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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Мониторинг СМИ

Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

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Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 1560. Отображено 100.
03-05-2012 дата публикации

Novel microbiocides

Номер: US20120108645A1
Автор: Daniel Stierli, Harald Walter
Принадлежит: SYNGENTA CROP PROTECTION LLC

Compounds of formula (I) in which the substituents are as defined in claim 1, are suitable for use as microbiocides.

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Номер записи: 1
13-12-2012 дата публикации

Fibrillation-resistant insulin and insulin analogues

Номер: US20120316107A1
Автор: Michael Weiss
Принадлежит: CASE WESTERN RESERVE UNIVERSITY

A fibrillation-resistant insulin analogue may be a single-chain insulin analogue or a physiologically acceptable salt thereof, containing an insulin A chain sequence or an analogue thereof and an insulin B chain sequence or an analogue thereof connected by a polypeptide of 4-10 amino acids. The fibrillation-resistant insulin analogue preferably displays less than 1 percent fibrillation with incubation at 37° C. for at least 21 days. A single-chain insulin analogue displays greater in vitro insulin receptor binding than normal insulin while displaying less than or equal binding to IGFR than normal insulin. The fibrillation-resistant insulin may be used to treat a patient using an implantable or external insulin pump, due to its greater fibrillation resistance.

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Номер записи: 2
21-03-2013 дата публикации

COMPOUNDS WITH BOTH ANALGESIC AND ANTI-HYPERALGESIC EFFICACY

Номер: US20130072533A1
Автор: Dragoni Elisa, Ghelardini Carla, La Marca Giancarlo, Nativi Cristina
Принадлежит:

The present invention relates to molecules of formula (I), deriving from lipoic acid and camosine, their preparation and use as analgesics. 2. Compounds of formula (I) according to for use as a medicament.3. Compounds according to for use as analgesics.4. Compounds of formula (I) according to for the treatment of neuropathic pain.5. Compositions comprising at least one compound of formula (I) according to and at least one other pharmaceutically acceptable ingredient.6. Process for the preparation of compounds of formula (I) according to starting from lipoic acid and carnosine.8. Compounds of formula (II) as defined in . The present invention relates to the field of organic compounds containing heterocycles having pharmacological efficacy as analgesics.The World Health Organisation (W.H.O.) defines neuropathic pain as: “An unpleasant sensation and a negative-affective emotional experience, associated with actual or potential tissue damage, or described in terms of such damage”. The International Association for the Study of Pain (1ASP) defines it as: “An unpleasant sensory and emotional experience associated with actual or potential tissue damage, or described as such”.Neuropathic pain is a significant problem in neurology in that it occurs frequently and is often disabling due to its irritating and chronic character.Examples thereof are: post-herpetic pain, phantom limb pain which can arise after an amputation, pain present in peripheral neuropathy such as with diabetes or AIDS, so-called complex regional pain syndrome or reflex sympathetic dystrophy pain, and pain from lesions of the central nervous system. These latter can be sequelae of stroke, trauma, tumours or due to systemic diseases. In most cases, the pain often present in multiple sclerosis is of such origin. In recent years, interest has focussed on neuropathic pain induced by chemotherapy drugs (vincristine, paclitaxel, oxaliplatin, bortezomib, etc.)The characteristics of this pain vary from patient to ...

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Номер записи: 3
09-05-2013 дата публикации

PROCESS FOR THE PREPARATION OF 4-CARBONYL)AMINO]-3-FLUOROPHENOXY}-N-METHYLPYRIDINE-2-CARBOXAMIDE, ITS SALTS AND MONOHYDRATE

Номер: US20130116442A1
Автор: Gottfried Michael, Heilmann Werner, Lögers Michael, Rehse Joachim, Stiehl Juergen, Wichmann Saskia
Принадлежит: Bayer Intellectual Property GmbH

The present invention relates to a process for preparing 4-{4-[({[4-chloro-3-(trifluoromethyl)-phenyl]amino}carbonyl)amino]-3-fluorophenoxy}-N-methylpyridine-2-carboxamide, its salts and monohydrate. 2. The process of for preparing the monohydrate of the compound of the formula (I) wherein the salt of the compound of the formula (I) is then treated with an aqueous basic solution to precipitate the monohydrate of the compound of the formula (I).3. The process of wherein the monohydrate of the compound of the formula (I) precipitates at a temperature of from 35° C. to 45° C.4. The process of or for preparing of the compound of the formula (I) wherein the monohydrate is dried under reduced pressure until the compound of the formula (I) is formed.5. The process of any of to wherein the solution comprising the solved compound of the formula (I) and what from the salt of the compound of the formula (I) precipitates is the reaction mixture or is a separate solution of the compound of the formula (I) prepared after isolation of the compound of the formula (I) from the reaction mixture.6. The process of any of to wherein the acid is generated in situ in the reaction mixture after the compound of the formula (I) is formed by adding to the reaction mixture a protic substance and an acid precursor.7. The process of wherein the acid is generated in situ in the reaction mixture after the compound of the formula (I) is formed by adding to the reaction mixture an alcohol and an acylchloride.8. The process of wherein the alcohol is ethanol and the acylchloride is acetylchloride.11. The process of or wherein the compound of the formula (II) is used in a solution of a suitable organic solvent which solution is prepared by neutralization the hydrochloric acid salt of the compound of the formula (II) with a base.12. The process of any of to wherein the compound of the formula (II) it is solved in a suitable organic solvent claim 7 , treated with an acid which is generated in situ by ...

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Номер записи: 4
16-05-2013 дата публикации

AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS

Номер: US20130123233A1
Автор: Bian Haiyan, Chevalier Kristen, Clemente Jose, Connolly Pete, Flores Chris, LIN Shu-Chen, Liu Li, Mabus John, Macielag Mark, McDonnell Mark, Pitis Philip, Zhang Sui-Po, Zhang Yue-Mei, ZHU Bin
Принадлежит: Janssen Pharmaceutica NV

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: 117.-. (canceled)19. A pharmaceutical composition comprising a compound of and at least one of a pharmaceutically acceptable carrier claim 18 , a pharmaceutically acceptable excipient and a pharmaceutically acceptable diluent.20. A pharmaceutical composition of claim 19 , wherein the composition is a solid oral dosage form.21. A pharmaceutical composition of claim 19 , wherein the composition is a syrup claim 19 , an elixir or a suspension. This application claims priority to U.S. provisional patent application Nos. 61/171,658 and 61/171,649, each filed Apr. 22, 2009, which are hereby incorporated by reference in their entirety.The research and development of the invention described below was not federally sponsored.has been used for the treatment of pain for many years. Δ-tetrahydrocannabinol is a major active ingredient from and an agonist of cannabinoid receptors (Pertwee, 2008, 153, 199-215). Two cannabinoid G protein-coupled receptors have been cloned, cannabinoid receptor type 1 (CBMatsuda et al., Nature, 1990, 346, 561-4) and cannabinoid receptor type 2 (CBMunro et al., 1993, 365, 61-5). CBis expressed centrally in brain areas, such as the hypothalamus and nucleus accumbens as well as peripherally in the liver, gastrointestinal tract, pancreas, adipose tissue, and skeletal muscle (Di Marzo et al., 2007, 18, 129-140). CBis predominantly expressed in immune cells, such as monocytes (Pacher et al., 2008, 294, H1133-H1134), and under certain conditions, also in the brain (Benito et al., 2008, 153, 277-285) and in skeletal (Cavuoto et al., 2007, 364, 105-110) and cardiac (Hajrasouliha et al., 2008, 579, 246-252) muscle. An abundance of pharmacological, anatomical and electrophysiological data, using synthetic agonists, indicate that increased cannabinoid signaling through CB/ ...

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Номер записи: 5
23-05-2013 дата публикации

Fluro substituted Omega-Carboxyaryl Diphenyl Urea for the Treatment and Prevention of Diseases and Conditions

Номер: US20130131122A1
Автор: Boyer Stephen, Dumas Jacques, Riedl Bernd, Wilhelm Scott
Принадлежит: Bayer HealthCare LLC

A compound of Formula (I): 154-. (canceled)562. A compound claim where the methylamide group is substituted with a hydroxyl group.571. A pharmaceutical composition comprising a compound of claim and a physiologically acceptable carrier.581. A pharmaceutical composition for the treatment of a cancerous cell growth comprising a compound of claim and a physiologically acceptable carrier for treating cancer.605. A compound claim where either urea nitrogen atom of the compound of formula I is substituted with a hydroxyl group.627. A compound claim where the pyridine nitrogen atom is in the n-oxide form and the methylamide functionality is substituted with a hydroxyl group. This application is a continuation application of U.S. application Ser. No. 10/895,985 filed Jul. 22, 2004 which claims the benefit of the filing date of U.S. Provisional Application Ser. No. 60/489,102 filed Jul. 23, 2003 and U.S. Provisional Application Ser. No. 60/540,326 filed Feb. 2, 2004.This invention relates to novel compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating diseases and conditions mediated by abnormal VEGFR, PDGFR, raf, p38, and/or flt-3 kinase signaling, either alone or in combination with anti-cancer agents.Activation of the ras signal transduction pathway indicates a cascade of events that have a profound impact on cellular proliferation, differentiation, and transformation. Raf kinase, a downstream effector of ras, is recognized as a key mediator of these signals from cell surface receptors to the cell nucleus (Lowy, D. R.; Willumsen, B. M. 1993, 62, 851; Bos, J. L. 1989, 49, 4682). It has been shown that inhibiting the effect of active ras by inhibiting the raf kinase signaling pathway by administration of deactivating antibodies to raf kinase or by co-expression of dominant negative raf kinase or dominant negative MEK, the substrate of raf kinase, leads to the reversion of transformed cells to the normal ...

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Номер записи: 6
06-06-2013 дата публикации

TARGETED CORRECTION OF A GENETIC DEFECT IN CANCER THERAPY

Номер: US20130143933A1
Автор: BATIST Gérald, WU Jian Hui
Принадлежит: TRT Pharma Inc.

The present document describes a cancer mutation-selective chemosensitizer that comprise compounds for restoring association between mutated keap1 protein and Nrf2 protein, and inhibition of Nrf2 functions. The present document also describes composition of matter containing the compounds, as well as methods of medical treatment for treating diseases such as cancer with the compounds. 3. The mutation-selective chemosensitizer of claim 1 , wherein said compound corrects a Keap1 mutation to restore interaction between a mutated Keap1 protein and said Nrf2 protein.10. A pharmaceutical composition for the inhibition of a Nrf2 protein which comprises a therapeutically effective amount of a compound of formula (I) as defined in claim 1 , in association with a pharmaceutically acceptable carrier.11. A pharmaceutical composition for overcoming drug resistance in cancer chemotherapy and for the inhibition of tumor growth which comprises a therapeutically effective amount of a compound of formula (I) as defined in claim 1 , in association with a pharmaceutically acceptable carrier.12. A method of treating and/or preventing a disease which involves the abnormal activation or expression of a Nrf2 protein comprising administering a therapeutically effective amount of the compound of formula (I) as defined in of .13. A method of treating a cancer in a subject in need thereof comprising administering a therapeutically effective amount of a compound of formula (I) as defined in of .14. The method of claims 13 , wherein said cancer is chosen from liver cancer claims 13 , lung cancer claims 13 , breast cancer claims 13 , prostate cancer claims 13 , colon cancer claims 13 , neuroblastoma or leukemia. This application claims priority of U.S. provisional patent application U.S. 61/557,646, filed 9 Nov. 2011, the specification of which is hereby incorporated by reference.(a) FieldThe subject matter disclosed generally relates to a mutation-selective chemosensitizer for overcoming ...

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Номер записи: 7
13-06-2013 дата публикации

RATIONALLY IMPROVED ISONIAZID AND ETHIONAMIDE DERIVATIVES AND ACTIVITY THROUGH SELECTIVE ISOTOPIC SUBSTITUTION

Номер: US20130150415A1
Автор: Bishai William, Deretic Vojo P., Masters Sharon, Timmins Graham
Принадлежит:

The present invention relates to the use of isotopically labeled derivatives of isoniazid, ethionamide and related compounds as effective therapy for the treatment of mycobacterial diseases, including 144-. (canceled)46. The method according to wherein said NHNHgroup is isotopically labeled with two N atoms.47. The method according to wherein said compound contains at least one isotopically labeled atom selected from the group consisting of carbon-13 claim 45 , nitrogen-15 claim 45 , oxygen-17 and oxygen-18 in the exocyclic acyl hydrazide moiety of the compound.49. The method according to wherein said compound has an isotopically labeled carbon-13 claim 45 , oxygen-17 or oxygen-18 atom.50. The method according to wherein said compound has an isotopically labeled carbon-13 atom.51. The method according to wherein said compound has an isotopically labeled oxygen-17 atom.52. The method according to wherein said compound has an isotopically labeled oxygen-18 atom.53. The method according to wherein said compound has an isotopically labeled carbon-13 atom and an isotopically labeled oxygen-18 atom.54. The method according to wherein said compound has an isotopically labeled nitrogen-15 atom.55MycobacteriumMycobacterium tuberculosis.. The method according to wherein said infection is56. The method according to wherein said infection is latent.57. The method according to wherein said infection is active.58. The method according to wherein said infection is miliary.59. The method according to wherein said infection is extrapulmonary.60. The method according to wherein said infection is renal.62. The method according to wherein said compound is administered in pulmonary dosage form.63. The method according to wherein said compound is administered is oral dosage form.64. The method according to wherein said compound is administered in parenteral dosage form. This application claims the benefit of priority of U.S. provisional application Ser. No. 61/127,150, filed May 9, 2008 ...

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Номер записи: 8
13-06-2013 дата публикации

PROLINE SULFONAMIDE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS

Номер: US20130150424A1
Автор: Boss Christoph, Brotschi Christine, GATFIELD John, Gude Markus, Heidmann Bibia, Sifferlen Thierry, Williams Jodi T.
Принадлежит: ACTELION PHARMACEUTICALS LTD.

The present invention relates to (S)-proline sulfonamide compounds of formula (I) 2. A method according to claim 1 , wherein{'sup': '1', 'Rrepresents a group selected from the group consisting of 5-bromo-thiophen-2-yl, 4-chloro-phenyl, 3-chloro-phenyl, 4-bromo-phenyl, 3-bromo-phenyl, 3-chloro-4-methyl-phenyl, 2-bromo-4-methyl-phenyl, 4-bromo-2-methyl-phenyl, 4-vinyl-phenyl, 2,4-dimethylphenyl, 3,4-dichloro-phenyl, 4-bromo-2-chloro-phenyl, 3-methoxy-phenyl, 4-methoxy-phenyl, 4-chloro-2,5-dimethyl-phenyl, 4-n-propyl-phenyl, 2-methoxy-4-methyl-phenyl, 2-methoxy-5-methyl-phenyl, 4-trifluoromethyl-phenyl, 4-methanesulfonyl-phenyl, 2,5-dimethoxy-phenyl, 3,4-dimethoxy-phenyl, naphthalen-1-yl, naphthalen-2-yl, 4-methyl-3,4-dihydro-2H-benzo[1,4]oxazin-7-yl, 2-chloro-5-trifluoromethyl-phenyl, 2-chloro-4-trifluoromethyl-phenyl, and 4-chloro-3-trifluoromethyl-phenyl.'}3. A method according to claim 1 , wherein{'sup': '2', 'Rrepresents a group selected from the group consisting of phenyl, 3-chloro-phenyl, 3-bromo-phenyl, 3-methyl-phenyl, 3-methylthio-phenyl, 2-chloro-5-methyl-phenyl, 4-chloro-3-methyl-phenyl, 2-fluoro-5-methyl-phenyl, 4-fluoro-3-methyl-phenyl, 3-ethyl-phenyl, 3,5-dimethyl-phenyl, 3,4-dimethyl-phenyl, 3,4-dichloro-phenyl, 3,5-dichloro-phenyl, 3-chloro-4-fluoro-phenyl, 3,4-difluoro-phenyl, 3-methoxy-phenyl, 3-cyano-phenyl, 5-chloro-2-methoxy-phenyl, 2-chloro-5-methoxy-phenyl, 3-ethoxy-phenyl, 3-dimethylamino-phenyl, 3-trifluoromethyl-phenyl, 3,5-dimethoxy-phenyl, 1-naphthyl, 3-trifluoromethoxy-phenyl, 3,5-bistrifluoromethyl-phenyl, and indan-5-yl.'}5. A pharmaceutical composition according to claim 4 , wherein{'sup': '1', 'Arrepresents a group selected from the group consisting of 3-chloro-phenyl, 4-bromo-phenyl, 3-bromo-phenyl, 3-chloro-4-methyl-phenyl, 3,4-dichloro-phenyl, 3-methoxy-phenyl, 4-methoxy-phenyl, 3,4-dimethoxy-phenyl, and 4-chloro-3-trifluoromethyl-phenyl;'}or a pharmaceutically acceptable salt thereof.6. A pharmaceutical composition according to ...

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Номер записи: 9
13-06-2013 дата публикации

NOVEL SOLID FORMS OF TACEDINALINE

Номер: US20130150450A1
Автор: Holson Edward, Stahly G. Patrick, Wagner Florence F.
Принадлежит: THE BROAD INSTITUTE, INC.

Novel solid forms of tacedinaline (4-(acetylamino)-N-(2-aminophenyl)benzamide), including crystalline tacedinaline Forms A, B, and D, a novel crystalline tacedinaline TFA salt, and amorphous tacedinaline, are disclosed. Pharmaceutical compositions comprising crystalline tacedinaline Forms A, B, and D, the novel crystalline tacedinaline TFA salt, and/or amorphous tacedinaline, and methods of treating various conditions by administering those novel solid forms, are also disclosed. 14-. (canceled)5. A method of treating at least one of a neoplastic disease , memory loss , and a cognitive function disorder/impairment in a subject , said method comprising administering 4-(acetylamino)-N-(2-aminophenyl)benzamide comprising crystalline 4-(acetylamino)-N-(2-aminophenyl)benzamide Form A to said subject.6. A method of treating at least one of a neoplastic disease , memory loss , and a cognitive function disorder/impairment in a subject , said method comprising administering a pharmaceutical composition comprising crystalline 4-(acetylamino)-N-(2-aminophenyl)benzamide Form A to said subject.7. A method of treating at least one of a neoplastic disease , memory loss , and a cognitive function disorder/impairment in a subject , said method comprising administering 0.001 mg/kg to 50 mg/kg per day of 4-(acetylamino)-N-(2-aminophenyl)benzamide comprising crystalline 4-(acetylamino)-N-(2-aminophenyl)benzamide Form A to said subject , for at least two consecutive days.8. A method of treating at least one of a neoplastic disease , memory loss , and a cognitive function disorder/impairment in a subject , said method comprising administering up to 0.4 mg/kg per day of 4-(acetylamino)-N-(2-aminophenyl)benzamide crystalline 4-(acetylamino)-N-(2-aminophenyl)benzamide Form A to said subject , for up to 14 consecutive days.9. A method of treating at least one of a neoplastic disease , memory loss , and a cognitive function disorder/impairment in a subject , said method comprising ...

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Номер записи: 10
20-06-2013 дата публикации

PIPERAZINE-SUBSTITUTED BENZOTHIOPHENES FOR TREATMENT OF MENTAL DISORDERS

Номер: US20130158044A1
Автор: Ito Nobuaki, Kuroda Hideaki, Matsubara Jun, Miyamura Shin, Oshima Kunio, SHIMIZU Satoshi, Takahashi Haruka, Tanaka Tatsuyoshi, Yamashita Hiroshi
Принадлежит: OTSUKA PHARMACEUTICAL CO., LTD.

The present invention provides a heterocyclic compound represented by the general formula (1): The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety. 7. The heterocyclic compound of the formula (1) according to selected from the group consisting of:(1) 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one,(2) 7-[3-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)propoxy]-1H-quinolin-2-one,(3) 7-[3-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)propoxy]-3,4-dihydro-1H-quinolin-2-one,(4) 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-3,4-dihydro-1H-quinolin-2-one,(5) 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1-methyl-3,4-dihydro-1H-quinolin-2-one and(6) 6-[3-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)propoxy]-3,4-dihydro-1H-quinolin-2-one;or a salt thereof.8. The heterocyclic compound of the formula (1) according to selected from the group consisting of:(1) 7-[3-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)propoxy]-3,4-dihydro-2H-isoquinolin-1-one(2) 7-[3-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)propoxy]-2-methyl-3,4-dihydro-2H-isoquinolin-1-one,(3) 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-2-methyl-3,4-dihydro-2H-isoquinolin-1-one,(4) 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-3,4-dihydro-2H-isoquinoline-1-one,(5) 7-[3-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)propoxy]-2H-isoquinolin-1-one and(6) 7-[3-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)propoxy]-2-methyl-2H-isoquinolin-1-one;or a salt thereof.9. A pharmaceutical composition comprising a heterocyclic compound of the formula (1) or a salt thereof according to claim 1 , as an active ingredient and a pharmaceutically acceptable carrier.10. The pharmaceutical composition according to for treating or preventing central nervous system disorders.11. The pharmaceutical composition according to for treating or preventing central nervous system disorders selected from the group ...

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Номер записи: 11
18-07-2013 дата публикации

INSECTICIDAL COMPOUNDS

Номер: US20130184343A1
Автор: Jung Pierre, Lutz William, Maienfisch Peter, Pitterna Thomas, Renold Peter, Zambach Werner
Принадлежит:

A compound of formula (I): 2. A compound according to wherein Ais C—X—Ror C—R.3. A compound according to wherein Ais C—X—Ror C—R.4. A compound according to wherein Ais C—X—Ror C—R.5. A compound according to wherein Ais C—X—Ror C—R.6. A compound according to wherein one or two of A claim 1 , A claim 1 , Aand Aare C—X—R.7. A compound according to wherein Ris hydrogen claim 1 , methyl claim 1 , ethyl or acetyl.8. A compound according to wherein Ris hydrogen claim 1 , methyl claim 1 , ethyl or acetyl.9. A compound according to wherein Gis oxygen.10. A compound according to wherein Gis oxygen.11. A compound according to wherein each Ris independently hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , allyl claim 1 , phenyl or phenyl mono-substituted by halogen or methyl.12. A compound according to wherein each X is independently oxygen or sulfur.13. A compound according to wherein each Ris independently hydrogen or methyl.14. A compound according to wherein each Ris independently hydrogen claim 1 , fluoro claim 1 , methyl or trifluoromethyl.15. A compound according to any wherein Qis 5-bromo-furan-2-yl claim 1 , 2-bromo-phenyl claim 1 , 5-bromo-pyrid-3-yl claim 1 , 2-chloro-5-nitro-phenyl claim 1 , 2-chloro-phenyl claim 1 , 3-chloro-phenyl claim 1 , 2-chloro-pyrid-3-yl claim 1 , 2-chloro-pyrid-4-yl claim 1 , 6-chloro-pyrid-3-yl claim 1 , 5-chloro-thiophen-2-yl claim 1 , 3-chloro-5-trifluoromethyl-pyrid-2-yl claim 1 , 4-cyano-phenyl claim 1 , 2 claim 1 ,5-dichloro-phenyl claim 1 , 2 claim 1 ,3-difluoro-phenyl claim 1 , 1 claim 1 ,3-dimethyl-pyrazol-5-yl claim 1 , 4-fluoro-phenyl claim 1 , 2-fluoro-pyrid-3-yl claim 1 , 2-fluoro-3-trifluoromethyl-phenyl claim 1 , 2-methyl-phenyl claim 1 , 3-methyl-pyrid-2-yl claim 1 , 2-methylthio-pyrid-3-yl claim 1 , 4-nitro-phenyl claim 1 , phenyl claim 1 , 1 claim 1 ,2 claim 1 ,3-thiadiazol-4-yl and thiophen-2-yl.16. A compound according to wherein Qis a moiety of formula (II).17. A compound according to wherein Qis 2 ...

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Номер записи: 12
25-07-2013 дата публикации

QUINOLYLPIPERAZINO SUBSTITUTED THIOLACTONE COMPOUNDS AND PROCESS FOR THE PREPARATION THEREOF

Номер: US20130190489A1
Автор: Abdullah Sheikh Tasdug, Kamal Ahmed, Khan Inshad Ali, Malik Mohammed Shaheer, Ram Anshu Beulah, Shaik Ahmad Ali, Shaik Azeeza, Sharma Sandeep
Принадлежит:

The present invention provides compounds of general formulae A, useful as potential anti-tubercular agents against H37Rv, and drug-resistant and a process for the preparation thereof. Formula (A). 3. Quinolylpiperazino substituted thiolactone compounds as claimed in is represented by the group of the following compounds:3,5-dimethyl-4-[(5-4-[7-(trifluoromethyl)-4-quinolyl]piperazinopentyl)oxy]-5H-thiophen-2-one (3a).3,5-dimethyl-4-[(6-4-[7-(trifluoromethyl)-4-quinolyl]piperazinohexyl)oxy]-5H-thiophen-2-one (3b)3,5-dimethyl-4-[(8-4-[7-(trifluoromethyl)-4-quinolyl]piperazinooctyl)oxy]-5H-thiophen-2-one (3c).3,5-dimethyl-4-[(9-4-[7-(trifluoromethyl)-4-quinolyl]piperazinononyl)oxy]-5H-thiophen-2-one (3 d).3,5-dimethyl-4-[(10-4-[7-(trifluoromethyl)-4-quinolyl]piperazinodecyl)oxy]-5H-thiophen-2-one (3e).3,5-dimethyl-4-[(12-4-[7-(trifluoromethyl)-4-quinolyl]piperazinododecyl)oxy]-5H-thiophen-2-one (3f).3,5-dimethyl-4-(5-[4-(7-chloro-4-quinolyl)piperazino]pentyloxy)-5H-thiophen-2-one (4a).3,5-dimethyl-4-(6-[4-(7-chloro-4-quinolyl)piperazino]hexyloxy)-5H-thiophen-2-one (4b).3,5-dimethyl-4-(8-[4-(7-chloro-4-quinolyl)piperazino]octyloxy)-5H-thiophen-2-one (4c).3,5-dimethyl-4-(9-[4-(7-chloro-4-quinolyl)piperazino]nonyloxy)-5H-thiophen-2-one (4d).3,5-dimethyl-4-(10-[4-(7-chloro-4-quinolyl)piperazino]decyloxy)-5H-thiophen-2-one (4e).3,5-dimethyl-4-(12-[4-(7-chloro-4-quinolyl)piperazino]dodecyloxy)-5H-thiophen-2-one (4f).3,5-dimethyl-4-[(5-4-[7-(trifluoromethyl)-4-quinolyl]-1,4-diazepan-1-ylpentyl)oxy]-5H-thiophen-2-one 5a).3,5-dimethyl-4-[(6-4-[7-(trifluoromethyl)-4-quinolyl]-1,4-diazepan-1-ylhexyl)oxy]-5H-thiophen-2-one (5b).3,5-dimethyl-4-[(8-4-[7-(trifluoromethyl)-4-quinolyl]-1,4-diazepan-1-yloctyl)oxy]-5H-thiophen-2-one (5c).3,5-dimethyl-4-[(9-4-[7-(trifluoromethyl)-4-quinolyl]-1,4-diazepan-1-ylnonyl)oxy]-5H-thiophen-2-one (5d).3,5-dimethyl-4-[(10-4-[7-(trifluoromethyl)-4-quinolyl]-1,4-diazepan-1-yldecyl)oxy]-5H-thiophen-2-one (5e).3,5-dimethyl-4-[(12-4-[7-(trifluoromethyl)-4 ...

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Номер записи: 13
15-08-2013 дата публикации

PHOTOLABILE CAGED TRANSITION METAL COMPLEXES AND METHODS OF USING THE SAME

Номер: US20130210793A1
Автор: Ciesienski Katie L., Franz Katherine J.
Принадлежит: Duke University

The present invention provides compounds of Formula I: 2. The compound of claim 1 , wherein Z is absent.3. The compound of claim 1 , wherein Z is a transition metal.4. The compound of claim 1 , wherein Z is a transition metal selected from the group consisting of copper claim 1 , platinum claim 1 , iron and zinc.5. The compound of claim 1 , wherein at least one adjacent pair of Rand Rtogether form a heteroaryl selected from the group consisting of pyrimidine claim 1 , thiazole claim 1 , thiophene claim 1 , isoquinoline claim 1 , imidazole claim 1 , and pyrroline.6. The compound of claim 1 , wherein Ris selected from the group consisting of: H claim 1 , alkyl claim 1 , alkoxy claim 1 , halo claim 1 , and sulfonate.7. The compound of claim 1 , wherein Ris selected from the group consisting of: H claim 1 , alkyl claim 1 , alkoxy claim 1 , halo claim 1 , and sulfonate.8. The compound of claim 1 , wherein Ris selected from the group consisting of: H claim 1 , alkyl claim 1 , alkoxy claim 1 , halo claim 1 , and sulfonate.9. The compound of claim 1 , wherein Ris selected from the group consisting of: H claim 1 , alkyl claim 1 , alkoxy claim 1 , halo claim 1 , and sulfonate.10. The compound of claim 1 , wherein Rand Rtogether form oxo.11. The compound of claim 1 , wherein each Ris independently selected from the group consisting of: H claim 1 , alkyl claim 1 , alkoxy claim 1 , halo claim 1 , and sulfonate.12. The compound of claim 1 , wherein each Ris independently selected from the group consisting of: H claim 1 , alkyl claim 1 , alkoxy claim 1 , halo claim 1 , and sulfonate.13. The compound of claim 1 , wherein each Ris independently selected from the group consisting of: H claim 1 , alkyl claim 1 , alkoxy claim 1 , and halo.14. The compound of claim 1 , wherein each Ris independently selected from the group consisting of: H claim 1 , alkyl claim 1 , alkoxy claim 1 , and halo.16. A composition comprising a compound of in a pharmaceutically acceptable carrier.1718-. ( ...

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Номер записи: 14
15-08-2013 дата публикации

SORAFENIB DIMETHYL SULPHOXIDE SOLVATE

Номер: US20130210865A1
Автор: Jaryal Jagdev Singh, Prasad Mohan, Sathyanarayana Swargam, Sinch Ajay Shankar, Thaper Rajesh Kumar, Zade Sachin Deorao
Принадлежит: RANBAXY LABORATORIES LIMITED

The present invention provides dimethyl sulphoxide solvate of 4-(4-{3-[4-chloro-3-(trifluoromethyl)phenyl]ureido}phenoxy)-N-methylpyridine-2-carboxamide, process for its preparation, pharmaceutical composition comprising it and its use for the treatment of cancer. The present invention also provides a novel HPLC method for the identification, quantification and isolation of related substances of sorafenib. 2. Sorafenib dimethyl sulphoxide solvate according to further characterized by X-ray diffraction peaks at d-spacing 5.36 claim 1 , 4.47 claim 1 , 4.44 claim 1 , 3.26 and 3.14 Å.3. Sorafenib dimethyl sulphoxide solvate of Formula III characterized by X-ray diffraction pattern as depicted in .4. Sorafenib dimethyl sulphoxide solvate of Formula III characterized by DSC thermogram having endotherms at about 123.69° C. and about 202.54° C.5. Sorafenib dimethyl sulphoxide solvate of Formula III characterized by DSC thermogram as depicted in .6. Sorafenib dimethyl sulphoxide solvate of Formula III characterized by X-ray diffraction pattern as depicted in and DSC thermogram as depicted in .7. Sorafenib dimethyl sulphoxide solvate of Formula III characterized by TGA as depicted in .8. Sorafenib dimethyl sulphoxide solvate of Formula III characterized by IR spectrum as depicted in .9. Sorafenib dimethyl sulphoxide solvate of Formula III having purity greater than 99% by HPLC.11. The process according to claim 10 , wherein Sorafenib free base of Formula I is contacted with dimethyl sulphoxide at a temperature of about 15° C. to the reflux temperature of dimethyl sulphoxide.13. The process according to claim 12 , wherein the solvent is selected from the group consisting of water claim 12 , chlorinated hydrocarbons claim 12 , alcohols claim 12 , ketones claim 12 , alkyl acetates claim 12 , ethers and mixtures thereof.14. The process according to claim 12 , wherein sorafenib dimethyl sulphoxide solvate of Formula III is contacted with a solvent at a temperature of about −5° C. ...

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Номер записи: 15
15-08-2013 дата публикации

ANTIVIRAL COMPOUNDS

Номер: US20130210915A1
Автор: Andersson Emma, Edlund Karin, Elofsson Mikael, Mei Ya-Fang, Öberg Christopher, Strand Marten, Wadell Göran
Принадлежит:

The present invention provides new antiviral compounds and pharmacological compositions comprising these new compounds and their use in the prophylaxis, prevention and treatment of viral infections, particularly adenovirus and herpes virus infections. 18-. (canceled)9. A compound selected from:Ethyl 2-[3-(benzoylamino)benzoylamino]benzoate2-[[3-(Benzoylamino)benzoyl]amino]benzoic acidEthyl 2-[4-(benzoylamino)benzoylamino]benzoate2-[2-(Acetylamino)benzoylamino]benzoic acid2-[2-(Trimethylacetylamino)benzoylamino]benzoic acid2-[[2-(Cyclohexanecarboxylamino)benzoyl]amino]benzoic acid2-[2-(4-Carboxybutanoylamido)benzoyl]aminobenzoic acid2-[2-(Benzylamino)benzoylamino]benzoic acid2-[2-(2-Fluorobenzoylamino)-benzoylamino]benzoic acid2-[2-(3-Fluorobenzoylamino)-benzoylamino]benzoic acid2-[2-(4-Fluorobenzoylamino)-benzoylamino]benzoic acidEthyl 2-[2-(benzoylamino)benzoylamino]benzoateEthyl 2-[2-(acetylamino)benzoylamino]benzoateEthyl 2-[2-(trimethylacetylamino)benzoylamino]benzoateEthyl 2-[[2-(cyclohexanecarboxylamino)benzoyl]amino]benzoateEthyl 2-[2-(phenylacetylamino)benzoylamino]benzoateEthyl 2-[2-(4-carboxybutanoylamido)benzoyl]aminobenzoateEthyl 2-[[2-(benzylamino)benzoyl]amino]benzoate2-[[2-(Benzoylamino)benzoyl]amino]benzoic acid2-[2-(Acetylamino)benzoylamino]benzoic acid2-[2-(Trimethylacetylamino)benzoylamino]benzoic acid2-[[2-(Cyclohexanecarboxylamino)benzoyl]amino]benzoic acid2-[2-(Phenylacetylamino)benzoylamino]benzoic acid2-[2-(4-Carboxybutanoylamido)benzoyl]aminobenzoic acid2-[2-(Benzylamino)benzoylamino]benzoic acid2-[2-(benzoylamino)benzoylamino]phenylacetic acid2-[2-(benzoylamino)phenylacetylamino]benzoic acid2-[2-(2-fluorobenzoylamino)-benzoylamino]-4-chlorobenzoic acid2-[2-(2-fluorobenzoylamino)benzoylamino]-5-chlorobenzoic acid2-[2-(2-fluorobenzoylamino)-benzoylamino]-4-methoxybenzoic acid2-[2-(2-fluorobenzoylamino)-benzoylamino]-5-methoxybenzoic acid2-[2-(2-fluorobenzoylamino)-benzoylamino]-4,5-difluorobenzoic acid2-[4-chloro-2-(2-fluorobenzoylamino)- ...

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Номер записи: 16
22-08-2013 дата публикации

PHENOXY-AZETIDINE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS

Номер: US20130217667A1
Автор: Chow Ken, CORPUZ EVELYN G., FANG WENKUI K., IM WHA-BIN, Wang Liming
Принадлежит: ALLERGAN, INC.

The present invention relates to novel phenoxy-azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. 2. A compound according to wherein Lis CH.3. A compound according to wherein Lis CH.4. A compound according to wherein a is 1 claim 1 , 2 or 3.9. A compound according to claim 1 , wherein:{'sup': '1', 'Ris H or halogen;'}{'sup': '2', 'Ris H or halogen;'}{'sup': '3', 'Ris H or halogen;'}{'sup': '4', 'Ris H or halogen;'}{'sup': '5', 'sub': '1-8', 'Ris H or Calkyl; and'}{'sup': '6', 'sub': '1-8', 'Ris H or Calkyl.'}10. A compound according to claim 1 , selected from:1-(4-{[5-(3-chlorophenyl)-6-(3,4-dimethylphenyl)hexyl]oxy}benzyl)azetidine-3-carboxylic acid;1-{4-[3-(3-chlorophenyl)-4-(3,4-dimethylphenyl)butoxy]benzyl}azetidine-3-carboxylic acid;1-(4-{[4-(3,5-difluorophenyl)-5-(3,4-dimethylphenyl)pentyl]oxy}benzyl)azetidine-3-carboxylic acid;1-(4-{[4-(3-chlorophenyl)-5-(3,4-dimethylphenyl)pentyl]oxy}benzyl)azetidine-3-carboxylic acid;1-(4-{[4-(3,4-difluorophenyl)-5-(3,4-dimethylphenyl)pentyl]oxy}benzyl)azetidine-3-carboxylic acid;1-(4-{[5-(3,4-dimethylphenyl)-4-(3-thienyl)pentyl]oxy}benzyl)azetidine-3-carboxylic acid; and1-(4-{[4-(2,3-difluorophenyl)-5-(3,4-dimethylphenyl)pentyl]oxy}benzyl)azetidine-3-carboxylic acid.11. A pharmaceutical composition comprising as active ingredient a therapeutically effective amount of a compound according to and a pharmaceutically acceptable adjuvant claim 1 , diluent or carrier.12. A pharmaceutical composition according to wherein the compound is selected from:1-(4-{[5-(3-chlorophenyl)-6-(3,4-dimethylphenyl)hexyl]oxy}benzyl)azetidine-3-carboxylic acid;1-{4-[3-(3-chlorophenyl)-4-(3,4-dimethylphenyl)butoxy]benzyl}azetidine-3-carboxylic acid;1-(4-{[4-(3,5-difluorophenyl)-5-(3,4-dimethylphenyl)pentyl]oxy}benzyl)azetidine-3-carboxylic acid;1-(4-{[4-(3-chlorophenyl)-5-(3,4-dimethylphenyl)pentyl]oxy}benzyl)azetidine-3 ...

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Номер записи: 17
29-08-2013 дата публикации

ANTICANCER COMPOUNDS AND PREPARATION METHODS THEREOF

Номер: US20130225641A1
Автор: Zhang Nan, Zhong Rong
Принадлежит:

Two new compounds with anticancer effects of N-[4-chloro-3-(trifluoromethyl)phenyl]-[4-(N-methyl-formamide)(4-pyridyloxy)phenyl]-thiourea and N-[4-chloro-3-(trifluoromethyl)phenyl]-[4-(N-methyl-formamide)(4-pyridylthio)phenyl]-thiourea, and salts thereof are disclosed. Preparation methods of the two new compounds and pharmaceutical compositions containing the new compounds are further disclosed. Experimental studies show that the two new compounds can effectively inhibit the activity of Raf and VEGFR protein kinase, widely inhibit growth of various types of human tumor cell lines and further induce apoptosis of tumor cells. Human tumor heterograft model investigation proves that the two new compounds are effective antineoplastic agents, and can sharply inhibit growth of human liver cancer cells, lung cancer cells and intestinal cancer cells in vivo. Furthermore, the anticancer effects of the compounds are much better than that of Sorafenib. 2. A method for preparing the compound of claim 1 , the method comprising:(1) adding dimethyl formamide dropwise to a solution of pyridine-2-carboxylic acid in thionyl chloride at 40° C., stirring, then heating to 72° C., and stirring overnight; and cooling to room temperature after the reaction is completed, removing thionyl chloride under reduced pressure, adding toluene, evaporating to dryness under reduced pressure, and then adding toluene again, to obtain a solution of 4-chloropyridyl-2-carbonyl chloride in toluene;(2) adding the solution of 4-chloropyridyl-2-carbonyl chloride in toluene dropwise to an aqueous methylamine solution cooled to −5° C., and stirring when the temperature is below 20° C.; and then adding ethyl acetate and water, washing the organic layer with saturated saline, drying it over anhydrous sodium sulfate, and then concentrating to an orange oil, to obtain 4-chloro(2-pyridyl)-N-methylcarboxamide;{'sup': '˜', '(3) Under the protection of nitrogen, dissolving 4-aminophenol in dimethylformamide, then adding ...

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Номер записи: 18
05-09-2013 дата публикации

Novel Process For The Preparation Of Roflumilast

Номер: US20130231374A1
Автор: KOHL Bernhard, Mueller Bernd, PALOSCH Walter
Принадлежит: NYCOMED GMBH

A composition comprising: roflumilast having a purity of greater than or equal to 99% by weight, and N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide present (relative to roflumilast) in an amount greater than zero and less than 0.1% by weight. 121.-. (canceled)22. A composition comprising: roflumilast having a purity of greater than or equal to 99% by weight , and N-(3 ,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide present (relative to roflumilast) in an amount greater than zero and less than 0.1% by weight.23. The composition of claim 22 , wherein said roflumilast has a purity of greater than or equal to 99.8% by weight.24. The composition of claim 22 , wherein said N-(3 claim 22 ,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide is present (relative to roflumilast) in an amount greater than zero and less than 0.05% by weight.25. A pharmaceutical composition claim 22 , comprising: roflumilast having a purity of greater than or equal to 99% by weight; N-(3 claim 22 ,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide present (relative to roflumilast) in an amount greater than zero and less than 0.1% by weight; and pharmaceutically acceptable auxiliaries and/or excipients.26. The pharmaceutical composition of claim 25 , wherein said roflumilast has a purity of greater than or equal to 99.8% by weight.27. The pharmaceutical composition of claim 25 , wherein said N-(3 claim 25 ,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide is present (relative to roflumilast) in an amount greater than zero and less than 0.05% by weight.28. A pharmaceutical dosage form claim 25 , comprising: roflumilast having a purity of greater than or equal to 99% by weight; N-(3 claim 25 ,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide present (relative to roflumilast) in an amount greater than zero and less than 0.1% by weight; and pharmaceutically acceptable auxiliaries and/or excipients.29. The pharmaceutical ...

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Номер записи: 19
05-09-2013 дата публикации

AMIDE DERIVATIVE, PEST CONTROL AGENT CONTAINING THE AMIDE DERIVATIVE, AND USE OF THE AMIDE DERIVATIVE

Номер: US20130231392A1
Автор: Aoki Yoji, Daido Hidenori, Fukazawa Yasuaki, Hirabayashi Atsushi, Hirose Mai, Katsuta Hiroyuki, KAWAHARA Atsuko, Kobayashi Yumi, Nomura Michikazu, Takahashi Yusuke, TSUKADA Hidetaka
Принадлежит: MITSUI CHEMICALS ARGO, INC.

An amide derivative represented by the following Formula (1) is provided as an amide derivative showing a significantly excellent effect for a pest control action. 4. The pest control agent according to claim 3 , wherein in Formula (8) claim 3 , Yrepresents a C3-C4 perfluoroalkyl group.5. The pest control agent according to claim 4 , wherein in Formula (8) claim 4 , Yand Yeach independently represent a chlorine atom claim 4 , a bromine atom claim 4 , an iodine atom claim 4 , a trifluoromethoxy group claim 4 , a trifluoromethyl group claim 4 , or a pentafluoroethyl group claim 4 , and Yand Yrepresent hydrogen atoms.6. The pest control agent according to claim 5 , wherein in Formula (8) claim 5 , Xand Xeach independently represent a hydrogen atom or a fluorine atom claim 5 , and Xand Xrepresent hydrogen atoms.7. The pest control agent according to claim 6 , wherein in Formula (8) claim 6 , Rand Reach independently represent a hydrogen atom or a methyl group.8. The pest control agent according to claim 7 , wherein in Formula (8) claim 7 , Qrepresents a phenyl group or a pyridyl group which may have a substituent selected from a group consisting of a halogen atom claim 7 , a C1 haloalkyl group claim 7 , a nitro group claim 7 , and a cyano group.9. The pest control agent according to claim 8 , wherein in Formula (8) claim 8 , the number of the substituents in Qis 1 or 2.10. The pest control agent according to claim 2 , wherein in Formula (7) claim 2 , Yrepresents a C2-C4 perfluoroalkyl group claim 2 , Yand Yrepresent hydrogen atoms claim 2 , Yand Yeach represent a halogen atom or a C1-C3 haloalkyl group claim 2 , and either Yor Yrepresents a C1-C3 haloalkyl group.11. The pest control agent according to claim 10 , wherein in Formula (7) claim 10 , Xto Xeach independently represent a hydrogen atom claim 10 , a halogen atom claim 10 , or a cyano group.13. The pest control agent according to claim 12 , wherein in Formula (9) claim 12 , Yrepresents a C2-C4 perfluoroalkyl ...

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Номер записи: 20
12-09-2013 дата публикации

SULFAMIDES AS TRPM8 MODULATORS

Номер: US20130237547A1
Автор: Matthews Jay M.
Принадлежит: Janssen Pharmaceutica, NV

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: 1. (canceled)312-. (canceled)17. A pharmaceutical composition comprising a compound of and at least one of a pharmaceutically acceptable carrier claim 2 , a pharmaceutically acceptable excipient claim 2 , and a pharmaceutically acceptable diluent.18. A pharmaceutical composition of claim 17 , wherein the composition is a solid claim 17 , oral dosage form.19. A pharmaceutical composition of claim 17 , wherein the composition is a syrup claim 17 , an elixir claim 17 , or a suspension.20. A method for treating neuropathic pain in a subject in need thereof claim 2 , comprising administering to the subject a therapeutically effective amount of a compound of .21. The method of wherein the neuropathic pain is due to cancer claim 20 , a neurological disorder claim 20 , spine or peripheral nerve surgery claim 20 , a brain tumor claim 20 , traumatic brain injury (TBI) claim 20 , spinal cord trauma claim 20 , a chronic pain syndrome claim 20 , fibromyalgia claim 20 , chronic fatigue syndrome claim 20 , a neuralgia claim 20 , lupus claim 20 , sarcoidosis claim 20 , peripheral neuropathy claim 20 , bilateral peripheral neuropathy claim 20 , diabetic neuropathy claim 20 , central pain claim 20 , neuropathies associated with spinal cord injury claim 20 , stroke claim 20 , ALS claim 20 , Parkinson's disease claim 20 , multiple sclerosis claim 20 , sciatic neuritis claim 20 , mandibular joint neuralgia claim 20 , peripheral neuritis claim 20 , polyneuritis claim 20 , stump pain claim 20 , phantom limb pain claim 20 , a bony fracture claim 20 , oral neuropathic pain claim 20 , Charcot's pain claim 20 , complex regional pain syndrome I and II (CRPS I/II) claim 20 , radiculopathy claim 20 , Guillain-barre syndrome claim 20 , meralgia paresthetica claim 20 , burning-mouth syndrome claim 20 , optic ...

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Номер записи: 21
19-09-2013 дата публикации

PROLYL HYDROXYLASE INHIBITORS AND METHOD OF USE

Номер: US20130245076A1
Автор: Boyer Angelique Sun, Evdokimov Artem G., Greis Kenneth D., Kawamoto Richard Masaru, Warshakoon Namal C., Wu Shengde
Принадлежит:

The present disclosure relates to HIF-1α prolyl hydroxylase inhibitors, compositions which comprise the HIF-1α prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. 2. The compound according to claim 1 , wherein Ris —OR.3. The compound according to claim 2 , wherein Ris hydrogen.4. The compound according to claim 2 , wherein Ris methyl.5. The compound according to claim 1 , wherein Ris —NRR.6. The compound according to claim 5 , wherein Rand Rare each independently hydrogen or methyl.7. The compound according to claim 6 , wherein R is —NH.8. The compound {[5-(3-fluorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid.10. The composition according to claim 9 , wherein Ris —OR.11. The composition according to claim 10 , wherein Ris hydrogen.12. The composition according to claim 10 , wherein Ris methyl.13. The composition according to claim 9 , wherein Ris —NRR.14. The composition according to claim 13 , wherein Rand Rare each independently hydrogen or methyl.15. The composition according to claim 14 , wherein R is —NH.16. The composition according to claim 9 , wherein the compound is {[5-(3-fluorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid.18. A method for treating anemia claim 1 , comprising administering to a subject a compound according to .19. A method for treating anemia claim 9 , comprising administering to a subject a composition according to .20. A method for treating anemia claim 17 , comprising administering to a subject a compound according to . This application is a Continuation application of U.S. application Ser. No. 13/681,876, filed Nov. 20, 2012, which is a Continuation application of U.S. application Ser. No. 12/860,073, filed Aug. 20, 2010, which is a Continuation application of U.S. application Ser. No. 11/821,936, now U.S. Pat. No. 7,811,595 B2, filed Jun. 26, 2007, which claims the benefit of ...

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Номер записи: 22
31-10-2013 дата публикации

INHIBITORS OF ALPHA4 MEDIATED CELL ADHESION

Номер: US20130289109A1
Автор: Kawaguchi Takayuki, KUME Toshiyuki, NOMURA Sumihiro, SIRCAR Ila, TSUKIMOTO Mikiko
Принадлежит:

The present invention relates to a phenylalanine derivative of Formula (I) wherein Xis a halogen atom, Xis a halogen atom, Q is a CHR— is a carboxyl group which may be esterified; or a pharmaceutically acceptable salt thereof. 2. The method according to claim 1 , wherein said condition is allergic condition or rejection after transplantation.3. The method according to claim 2 , wherein allergic condition is rhinitis.5. The method according to claim 4 , wherein Xis chlorine atom or fluorine atom claim 4 , Xis chlorine atom or fluorine atom claim 4 , and Y is a Calkyl group.6. The method according to claim 5 , wherein Xis chlorine atom or fluorine atom claim 5 , Xis chlorine atom or fluorine atom claim 5 , Q is a —CH— group claim 5 , Y is methyl group claim 5 , ethyl group claim 5 , or n-propyl group claim 5 , and COR is a carboxyl group claim 5 , methoxycarbonyl group claim 5 , ethoxycarbonyl group or tert-butoxycarbonyl group.7. The method according to claim 5 , wherein Xis fluorine atom claim 5 , Xis chlorine atom or fluorine atom claim 5 , Q is a —CH— group claim 5 , and Y is methyl group or ethyl group.8. The method according to claim 1 , wherein the compound is selected from the group consisting of N-(2 claim 1 ,6-difluorobenzoyl)-4-(2 claim 1 ,6-dimethoxy-4-ethoxymethylphenyl)-L-phenylalanine claim 1 , N-(2-chloro-6-fluorobenzoyl)-4-(2 claim 1 ,6-dimethoxy-4-ethoxymethylphenyl)-L-phenylalanine claim 1 , N-(2-chloro-6-fluorobenzoyl)-4-(2 claim 1 ,6-dimethoxy-4-methoxymethylphenyl)-L-phenylalanine claim 1 , and N-(2 claim 1 ,6-difluorobenzoyl)-4-(2 claim 1 ,6-dimethoxy-4-methoxymethylphenyl)-L-phenylalanine.9. The method according to claim 1 , wherein the compound is N-(2 claim 1 ,6-difluorobenzoyl)-4-(2 claim 1 ,6-dimethoxy-4-ethoxymethylphenyl)-L-phenylalanine. This application is a Divisional of co-pending application Ser. No. 12/962,707, filed Dec. 8, 2010, which is a Divisional of application Ser. No. 12/683,648, filed Jan. 7, 2010, which issued as U.S. Pat. ...

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Номер записи: 23
12-12-2013 дата публикации

Proteasome Inhibitors

Номер: US20130331595A1
Автор: Danca Mihaela Diana, Olhava Edward J.
Принадлежит: Millennium Pharmaceuticals, Inc.

The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. 2. The process of claim 1 , wherein the reaction of step (1) is conducted in the presence of a peptide coupling reagent.3. The process of claim 2 , wherein the peptide coupling reagent is selected from the group consisting of a carbodiimide reagent claim 2 , phosphonium reagent claim 2 , and uranium reagent.4. The process of claim 3 , wherein the peptide coupling reagent is selected from one or more of the group consisting of dicyclohexylcarbodiimide (DCC) claim 3 , 1-(3-dimethylaminopropyl-3-ethylcarbodiimide (EDC) claim 3 , benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate (BOP) claim 3 , O-(1H-benzotriazol-1-yl)-N claim 3 ,N claim 3 ,N′N′-tetramethyluronium tetrafluoroborate (TBTU) and N-Hydroxybenzotriazole (HOBt).5. The process of claim 1 , wherein the reaction of step (3) is conducted in the presence of a peptide coupling reagent.6. The process of claim 5 , wherein the peptide coupling reagent is selected from the group consisting of a carbodiimide reagent claim 5 , phosphonium reagent claim 5 , and uranium reagent.7. The process of claim 6 , wherein the peptide coupling reagent is selected from one or more of the group consisting of dicyclohexylcarbodiimide (DCC) claim 6 , 1-(3-dimethylaminopropyl-3-ethylcarbodiimide (EDC) claim 6 , benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate (BOP) claim 6 , O-(1H-benzotriazol-1-yl)-N claim 6 ,N claim 6 ,N′N′-tetramethyluronium tetrafluoroborate (TBTU) and N-Hydroxybenzotriazole (HOBt).8. The process of claim 1 , wherein the reaction of step (1) is conducted in the presence of a solvent comprising a polar aprotic solvent.9. The process of claim 8 , wherein the polar aprotic solvent is selected from one or more of the group ...

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Номер записи: 24
09-01-2014 дата публикации

POLYMERIZABLE MONOMER, POLYMERIC COMPOUND, CHARGE CONTROL AGENT CONTAINING THE POLYMERIC COMPOUND, AND DEVELOPER BEARING MEMBER AND TONER WHICH CONTAIN THE CHARGE CONTROL AGENT

Номер: US20140011129A1
Автор: Hirose Masashi, Inoue Kei, Murai Yasuaki, Murayama Ryuji, Sato Kazuyuki
Принадлежит: CANON KABUSHIKI KAISHA

A polymerizable monomer is provided which is represented by the following formula (1): 4. The polymeric compound according to claim 3 , wherein the unit represented by the formula (4) is a styrene derivative unit or an acrylate derivative unit.5. The polymeric compound according to claim 2 , which has a weight-average molecular weight of from 3 claim 2 ,000 to 100 claim 2 ,000.6. A charge control agent comprising the polymeric compound according to .7. A developer bearing member comprising in a surface layer thereof the charge control agent according to .8. A toner comprising a binder resin claim 6 , a colorant and the charge control agent according to .9. The toner according to claim 8 , which is produced by a suspension polymerization process.10. The toner according to claim 8 , which is produced by a suspension granulation process. The present invention relates to a novel polymerizable monomer having a salicylic acid unit, and a polymeric compound produced by polymerizing the same. The present invention also relates to a charge control agent used in recording methods making use of electrophotography or the like, and a developer bearing member and a toner which contain the same.In image forming methods as typified by an electrophotographic recording method, a developer charged electrostatically (hereinafter “toner”) flies to the surface of a photosensitive member by electrostatic force which accords with potential differences on the photosensitive member surface, and develops electrostatic latent images formed on the photosensitive member surface. Hence, it is necessary and indispensable to control charge characteristics of the toner. Then, as a method for providing the toner with proper charge characteristics, a method is known in which a binder resin of a developer bearing member (hereinafter also “developing roller”) is incorporated with a charge control agent or a method in which a charge control agent capable of providing the toner with positive charges or ...

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Номер записи: 25
30-01-2014 дата публикации

CYCLIC SULFONIUM SALT, PROCESS FOR PRODUCTION OF SAME, AND alpha-GLUCOSIDASE INHIBITOR COMPRISING SAME

Номер: US20140031394A1
Автор: Muraoka Osamu, Tanabe Genzoh
Принадлежит:

Provided is a novel cyclic sulfonium salt compound which is useful for the prevention or treatment of diabetes and the like. The present invention relates to a novel cyclic sulfonium salt compound represented by general formula (I) or (II), an isomer or solvate of the compound, or a pharmaceutically acceptable salt of the compound or the isomer or solvate. The present invention also relates to an α-glucosidase inhibitor, a pharmaceutical composition for preventing or treating diabetes, and an anti-diabetes food, each of which comprises the compound represented by general formula (I) or (II) and the like. 3. The cyclic sulfonium salt compound or the isomer or the solvate thereof or the pharmaceutically acceptable salt thereof as claimed in or , wherein Ris hydrogen atom or —CHOH or —(CH)—CHOH).4. The cyclic sulfonium salt compound or the isomer or the solvate thereof or the pharmaceutically acceptable salt thereof as claimed in or , wherein Ris a C-Calkyl group or benzyl group , o- , m- or p-halobenzyl group , o- , m- or p-nitrobenzyl group , o- , m- or p-methylbenzyl group , o- , m- or p-trifluoromethylbenzyl group , hydroxymethylbenzyl group , naphthylmethyl group or pyridylmethyl group.5. The cyclic sulfonium salt compound or the isomer or the solvate thereof or the pharmaceutically acceptable salt thereof as claimed in or , wherein X is Cl or BF.6. The cyclic sulfonium salt compound or the isomer or the solvate thereof or the pharmaceutically acceptable salt thereof as claimed in or , wherein Ris hydrogen atom or —CHOH or —(CH)—CHOH) , and Ris a C-Calkyl group or benzyl group , o- , m- or p-halobenzyl group , o- , m- or p-nitrobenzyl group , o- , m- or p-methylbenzyl group , o- , m- or p-trifluoromethylbenzyl group , hydroxymethylbenzyl group , naphthylmethyl group or pyridylmethyl group.7. A medical composition for inhibition of α-glucosidase containing a cyclic sulfonium salt compound or the isomer or the solvate thereof or the pharmaceutically acceptable salt ...

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Номер записи: 26
20-02-2014 дата публикации

SYNTHESIS OF AN ANTIVIRAL COMPOUND

Номер: US20140051866A1
Автор: Liu Qi, Watkins William John
Принадлежит: Gilead Sciences, Inc.

The present disclosure provides a processes for the preparation of a compound of Formula I: 7. The process of claim 5 , wherein the N-arylation reaction conditions comprise a catalyst.8. The process of claim 7 , wherein the catalyst is a palladium claim 7 , platinum claim 7 , or copper based catalyst.9. The process of claim 8 , wherein the catalyst is selected from the group consisting of tris(dibenzylideneacetone)dipalladium(0) claim 8 , copper(I) chloride claim 8 , copper(II) chloride claim 8 , copper(I) bromide claim 8 , copper(II) bromide claim 8 , copper(I) acetate claim 8 , copper(II) acetate claim 8 , copper(II) acetylacetonate claim 8 , copper(I) trifluoromethanesulfonate claim 8 , copper(II) trifluoromethanesulfonate claim 8 , copper(I) thiophene-2-carboxylate claim 8 , and copper(I) iodide.10. The process of claim 7 , wherein the N-arylation reaction conditions further comprise a ligand.11. The process of claim 10 , wherein the ligand is selected from the group consisting of 5-(di-tert-butylphosphino)-1′ claim 10 ,3′ claim 10 ,5′-triphenyl-1′H-[1 claim 10 ,4′]bipyrazole claim 10 , 2-(di-tert-butyl-phosphino)-1-phenyl-1H-pyrrole claim 10 , 2-(di-tert-butylphosphino)-1-(2-methoxyphenyl)-1H-pyrrole claim 10 , acetylacetone claim 10 , acetylcyclohexanone claim 10 , isobutyrylcyclohexanone claim 10 , N claim 10 ,N-dimethylcyclohexane-1 claim 10 ,2-diamine claim 10 , L-proline claim 10 , BINAP claim 10 , and N claim 10 ,N-diethylsalicylamide.12. The process of claim 7 , wherein the N-arylation reaction conditions further comprise a base.13. The process of claim 12 , wherein the base is selected from the group consisting of potassium hydroxide claim 12 , sodium hydroxide claim 12 , sodium tert-amylate claim 12 , cesium carbonate claim 12 , cesium hydroxide claim 12 , potassium phosphate tribasic claim 12 , sodium tertbutoxide claim 12 , sodium methoxide claim 12 , and sodium ethoxide.14. The process of claim 4 , wherein the acylation reaction conditions comprise ...

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Номер записи: 27
20-02-2014 дата публикации

SYNTHESIS OF AN ANTIVIRAL COMPOUND

Номер: US20140051867A1
Автор: EVANS Jared Wayne, Fujimori Shinji, Huynh Grace M., Liu Qi, Teresk Martin Gerald
Принадлежит: Gilead Sciences, Inc.

The present disclosure provides processes for the preparation of a compound of Formula I: 5. The process of claim 3 , wherein the N-arylation reaction conditions comprise a catalyst.6. The process of claim 5 , wherein the catalyst is a palladium claim 5 , platinum claim 5 , or copper based catalyst.7. The process of claim 6 , wherein the catalyst is selected from the group consisting of tris(dibenzylideneacetone)dipalladium(0) claim 6 , copper(I) chloride claim 6 , copper(II) chloride claim 6 , copper(I) bromide claim 6 , copper(II) bromide claim 6 , copper(I) acetate claim 6 , copper(II) acetate claim 6 , copper(II) acetylacetonate claim 6 , copper(I) trifluoromethanesulfonate claim 6 , copper(II) trifluoromethanesulfonate claim 6 , copper(I) thiophene-2-carboxylate claim 6 , and copper(I) iodide.8. The process of claim 3 , wherein the N-arylation reaction conditions further comprise a ligand.9. The process of claim 8 , wherein the ligand is selected from the group consisting of 5-(di-tert-butylphosphino)-1′ claim 8 ,3′ claim 8 ,5′-triphenyl-1′H-[1 claim 8 ,4]bipyrazole claim 8 , 2-(di-tert-butyl-phosphino)-1-phenyl-1H-pyrrole claim 8 , 2-(di-tert-butylphosphino)-1-(2-methoxyphenyl)-1H-pyrrole claim 8 , acetylacetone claim 8 , acetylcyclohexanone claim 8 , isobutyrylcyclohexanone claim 8 , N claim 8 ,N-dimethylcyclohexane-1 claim 8 ,2-diamine claim 8 , L-proline claim 8 , BINAP claim 8 , and N claim 8 ,N-diethylsalicylamide.10. The process of claim 3 , wherein the N-arylation reaction conditions comprise a base.11. The process of claim 10 , wherein the base is selected from the group consisting of potassium hydroxide claim 10 , sodium hydroxide claim 10 , sodium tert-amylate claim 10 , cesium carbonate claim 10 , cesium hydroxide claim 10 , potassium phosphate tribasic claim 10 , sodium tertbutoxide claim 10 , sodium methoxide claim 10 , and sodium ethoxide.12. The process of claim 3 , wherein the N-arylation reaction conditions comprise a phase transfer catalyst. ...

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Номер записи: 28
27-02-2014 дата публикации

PROCESS FOR THE SYNTHESIS OF SUBSTITUTED GAMMA LACTAMS

Номер: US20140058117A1
Автор: Dinh Danny T., Garst Michael E., Gorin Boris, Lanthier Christopher M., Old David W., OUDENES Jan, Syage Elizabeth T.
Принадлежит: ALLERGAN, INC.

The present invention provides synthetic processes for the preparation of a variety of well-defined substituted gamma lactams. The compounds that can be prepared by the process of the invention are useful for treating a variety of conditions. In some embodiments of the invention, the compounds are useful for treating ocular disorders, such as, for example, glaucoma, lowering of elevated intraocular pressure, and the like. In other embodiments, the compounds are useful for treating irritable bowel disease. In further embodiments, the compounds are useful in promoting hair growth. In still further embodiments, the compounds are useful in promoting wound healing, scar reduction, and the like. 2. The process of claim 1 , wherein Ar is phenylene or naphthylene.3. The process of claim 1 , wherein Ar is phenylene.4. The process of wherein Ris Calkyl.5. The process of wherein Ris isopropyl.6. The process of wherein Ris linear Calkyl.7. The process of wherein m and n are 1.8. The process of claim 1 , wherein the protecting group is RRRSiCl claim 1 , wherein R claim 1 , R claim 1 , and Rare each independently C-Cstraight or branched chain alkyl.9. The process of claim 1 , wherein coupling step (b) is performed in the presence of a metal halide catalyst.10. The process of wherein the catalyst is a copper halide.11. The process of wherein the catalyst is CuI. This application claims the benefit of U.S. Provisional Ser. No. 61/691,559 filed on Aug. 21, 2012, which is incorporated by reference herein.This invention relates generally to the synthesis of substituted gamma lactams, which are useful as pharmaceutical compounds, e.g. as medicinal compounds useful for treating glaucoma and/or lower elevated intraocular pressure.The present invention provides synthetic processes for the preparation of a variety of well-defined substituted gamma lactams. The compounds that can be prepared by the process of the invention are useful for treating a variety of conditions. In some embodiments ...

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Номер записи: 29
13-03-2014 дата публикации

N-QUINOLIN-BENZENSULFONAMIDES AND RELATED COMPOUNDS FOR THE TREATMENT OF CANCER, AUTOIMMUNE DISORDERS AND INFLAMMATION

Номер: US20140073668A1
Автор: "OConnor Owen", Deng Shi-Xian, Kalac Matko, Landry Donald W., Rinderspacher Kristen Alison
Принадлежит: The Trustees of Columbia Unversity in the City of New York

The present invention relates to the NQBS class of molecules. It is based, at least in part, on the discovery that a representative group of compounds have been observed to inhibit nuclear translocation of NF-κB subunits. Without being bound by any particular theory, this inhibition of nuclear translocation may be mediated by either (i) binding of the NQBS or related compound to the C-terminus of the RHD, which specifically mediates the nuclear internalization; or (ii) NQBS-mediated stabilization of the dimer/IκB complex, disallowing dissociation of the active NF-κB monomers, and thus, inhibiting the generation of the subunits necessary to enter the nucleus. The NQBS class of molecules, and related molecules, may be used in therapeutic applications where inhibition of NF-κB translocation is beneficial, including but not limited to the treatment of cancer, autoimmune disorders, and inflammatory states. 1. A method for inhibiting the activity of a Nuclear factor-κB (NFκB) in a cell which comprises contacting the cell with a compound selected from the group consisting of compounds 47 , 55 , 69 , 74 , 75 and combinations thereof , in an amount effective to inhibit Nuclear factor-κB (NFκB) activity.2. The method of claim 1 , wherein the inhibition of Nuclear factor-κB (NFκB) activity reduces nuclear translocation of the Nuclear factor-κB (NFκB).3. The method of claim 1 , wherein the cell is a mammalian cell.4. The method of claim 1 , wherein the cell is contacted in vitro.5. A method for treating a disease related to dysfunction of cell proliferation claim 1 , the immune system claim 1 , and/or inflammation in an individual claim 1 , which method comprises administering to the individual an effective amount of a compound selected from the group consisting of compounds 47 claim 1 , 55 claim 1 , 69 claim 1 , 74 claim 1 , 75 and combinations thereof.6. The method of claim 5 , where the disease is cancer.7. The method of claim 6 , where the cancer is lymphoma.8. A ...

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Номер записи: 30
20-03-2014 дата публикации

FUSED CYCLIC COMPOUNDS

Номер: US20140080891A1
Автор: ITOU Masahiro, NEGORO Nobuyuki, YAMASHITA Masayuki, YASUMA Tsuneo
Принадлежит: Takeda Pharmaceutical Company Limited

The present invention provides a compound represented by the formula (I): 2. The compound of claim 1 , wherein Ris R—SO— (wherein Ris a substituent).3. The compound of claim 2 , wherein Ris a Calkyl group.4. The compound of claim 1 , wherein X is a Calkylene group.5. The compound of claim 1 , wherein Rand Rare the same or different and each is a hydrogen atom claim 1 , a halogen atom or a Calkyl group.6. The compound of claim 1 , wherein Rand Rare the same or different and each is a Calkyl group.7. The compound of claim 1 , wherein ring A is an unsubstituted benzene ring.8. The compound of claim 1 , wherein ring B is tetrahydrofuran.9. The compound of claim 1 , wherein Y is CH.10. The compound of claim 1 , wherein R is a hydroxy group.11. The compound of claim 1 , which is selected from[(3S)-6-({4′-[(4-hydroxy-1,1-dioxidotetrahydro-2H-thiopyran-4-yl)methoxy]-2′,6′-dimethylbiphenyl-3-yl}methoxy)-2,3-dihydro-1-benzofuran-3-yl]acetic acid,[(3S)-6-({2′,6′-dimethyl-4′-[3-(methylsulfonyl)propoxy]biphenyl-3-yl}methoxy)-2,3-dihydro-1-benzofuran-3-yl]acetic acid,[(3S)-6-({3′-fluoro-2′,6′-dimethyl-4′-[3-(methylsulfonyl)propoxy]biphenyl-3-yl}methoxy)-2,3-dihydro-1-benzofuran-3-yl]acetic acid,[(3S)-6-({3′-chloro-2′,6′-dimethyl-4′-[3-(methylsulfonyl)propoxy]biphenyl-3-yl}methoxy)-2,3-dihydro-1-benzofuran-3-yl]acetic acid,[(3S)-6-({3′,5′-dichloro-2′,6′-dimethyl-4′-[3-(methylsulfonyl)propoxy]biphenyl-3-yl}methoxy)-2,3-dihydro-1-benzofuran-3-yl]acetic acid, and[(3S)-6-({2′,6′-diethyl-4′-[3-(methylsulfonyl)propoxy]biphenyl-3-yl}methoxy)-2,3-dihydro-1-benzofuran-3-yl]acetic acid.12. A prodrug of the compound of .13. A GPR40 receptor function modulator comprising the compound of or a prodrug thereof.14. A pharmaceutical agent comprising the compound of or a prodrug thereof.15. The pharmaceutical agent of claim 14 , which is an agent for the prophylaxis or treatment of diabetes.16. A method for the prophylaxis or treatment of diabetes in a mammal claim 1 , which comprises administering ...

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Номер записи: 31
04-01-2018 дата публикации

PICOLINAMIDE COMPOUNDS WITH FUNGICIDAL ACTIVITY

Номер: US20180000075A1
Автор: Bravo-Altamirano Karla, Daeuble, DeKorver Kyle A., DeLorbe Johnathan E., Epp Jeffrey B., Herrick Jessica, Jones David M., Meyer Kevin G., SR. John F., Yao Chenglin
Принадлежит:

This disclosure relates to picolinamides of Formula I and their use as fungicides. 2. A compound according to claim 1 , wherein X and Y are hydrogen.3. A compound according to claim 2 , wherein Rand Rare independently chosen from hydrogen or alkyl.4. A compound according to claim 2 , wherein Rand Rare independently chosen from hydrogen or alkyl.5. A compound according to claim 2 , wherein Ris chosen from C-Calkyl claim 2 , aryl claim 2 , or alkenyl claim 2 , each optionally substituted with 0 claim 2 , 1 or multiple R.6. A compound according to claim 2 , wherein Ris chosen from alkyl or aryl claim 2 , each optionally substituted with 0 claim 2 , 1 or multiple R.7. A compound according to claim 2 , wherein Rand Rare independently chosen from hydrogen or alkyl claim 2 , Rand Rare independently chosen from hydrogen or alkyl claim 2 , Ris chosen from C-Calkyl claim 2 , aryl claim 2 , or alkenyl claim 2 , each optionally substituted with 0 claim 2 , 1 or multiple R claim 2 , and Ris chosen from alkyl or aryl claim 2 , each optionally substituted with 0 claim 2 , 1 or multiple R.8. A compound according to claim 1 , wherein X is C(O)Rand Y is hydrogen.9. A compound according to claim 8 , wherein Rand Rare independently chosen from hydrogen or alkyl.10. A compound according to claim 8 , wherein Rand Rare independently chosen from hydrogen or alkyl.11. A compound according to claim 8 , wherein Ris chosen from C-Calkyl claim 8 , aryl claim 8 , or alkenyl claim 8 , each optionally substituted with 0 claim 8 , 1 or multiple R.12. A compound according to claim 8 , wherein Ris chosen from alkyl or aryl claim 8 , each optionally substituted with 0 claim 8 , 1 or multiple R.13. A compound according to claim 8 , wherein Rand Rare independently chosen from hydrogen or alkyl claim 8 , Rand Rare independently chosen from hydrogen or alkyl claim 8 , Ris chosen from C-Calkyl claim 8 , aryl claim 8 , or alkenyl claim 8 , each optionally substituted with 0 claim 8 , 1 or multiple R claim 8 ...

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Номер записи: 32
11-01-2018 дата публикации

PROCESSES FOR THE PREPARATION OF 4-ALKOXY-3-(ACYL OR ALKYL)OXYPICOLINAMDES

Номер: US20180009755A1
Автор: Babij Nicholas R., Borromeo Peter, CHOY Nakyen, Hanley Patrick S., Hough Nicole, Knueppel Daniel I., Ober Matthias S., Roth Gary, Staton Tina, Wald Grant Von, Whiteker Gregory T.
Принадлежит: DOW AGROSCIENCES LLC

A fungicidal 4-methoxy-3-acetyloxypicolinamide may be conveniently prepared in processes that include the coupling together of 4-methoxy-3-acetyloxypicolinic acid or 4-methoxy-3-hydroxypicolinic acid with a key 2-aminopropanoate ester derived from a 1,1-bis(4-fluorophenyl)propane-1,2-diol. 2. The process of wherein the acylating agent is an alkyl chloroformate of the Formula ClCOR claim 1 , wherein R is a C-Calkyl or benzyl claim 1 , or an acid chloride of the Formula RCOCl claim 1 , wherein R is a C-Calkyl.3. The process of wherein the chlorinating agent is oxalyl chloride or thionyl chloride.4. The process of wherein the base may be selected from the group including triethylamine (TEA) claim 1 , diisopropylethylamine (DIPEA) claim 1 , pyridine claim 1 , potassium carbonate claim 1 , and mixtures thereof.5. The process of wherein the first mixture further comprises a solvent selected from the group including dichloromethane (DCM) claim 1 , 1 claim 1 ,2-dichloroethane (DCE) claim 1 , isopropyl acetate claim 1 , tetrahydrofuran (THF) claim 1 , 2-MeTHF claim 1 , acetonitrile (ACN) claim 1 , and mixtures thereof.7. The process of wherein the acylating agent is an alkyl chloroformate of the Formula ClCOR claim 6 , wherein R is a C-Calkyl or a benzyl.8. The process of wherein the first mixture further comprises a solvent selected from the group including dichloromethane (DCM) claim 6 , 1 claim 6 ,2-dichloroethane (DCE) claim 6 , acetonitrile (ACN) claim 6 , isopropyl acetate claim 6 , THF claim 6 , 2-MeTHF claim 6 , and mixtures thereof.9. The process of wherein the first base may be selected from the group including triethylamine (TEA) claim 6 , diisopropylethylamine (DIPEA) claim 6 , pyridine and potassium carbonate.10. The process of wherein about 3 equivalents of the first base and about 2 equivalents of the acylating agent are used.11. The process of wherein the alkali metal base may be selected from the group including LiOH claim 6 , NaOH claim 6 , KOH claim 6 , ...

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Номер записи: 33
17-01-2019 дата публикации

USE OF GUAIACOL FOR THE PREVENTION AND TREATMENT OF GLYCOGEN STORAGE DISEASE

Номер: US20190015355A1
Автор: AKMAN Hasan Orhan, DIMAURO Salvatore, KAKHLON Or
Принадлежит:

The current invention is a method of preventing and treating certain diseases by preventing the synthesis and/or breakdown of glycogen by the administration of an agent, guaiacol. Diseases that can be prevented and treated by the administration of guaiacol include but are not limited to glycogen storage disease type IV (GSD-IV), adult polyglucosan body disease (APBD), and Lafora disease (LD). The invention also includes methods and tools for screening for agents that prevent and treat these diseases as well as basic research, specifically in the form of cells and cell lines that produce detectable polyglucosan. 1. A method of treating and/or preventing a disease selected from a glycogen storage disease , a disease or disorder characterized by polyglucosan accumulation or abnormal glycogen accumulation , Lanora disease and diabetes , the method comprising administering to a subject in need thereof a therapeutically effective amount of guaiacol.2. The method of claim 1 , wherein the glycogen storage disease is chosen from the group consisting of types I-IX.3. The method of claim 1 , wherein the glycogen storage disease is a type IV glycogen storage disease.4. The method of claim 1 , wherein the glycogen storage disease is adult polyglucosan body disease.5. The method of claim 1 , wherein the subject in human.6. The method of claim 1 , wherein the guaiacol is administered orally.7. The method of claim 1 , wherein the guaiacol is administered in a dosage from about 22.5 to 45 milligrams of guaiacol per kilogram of the subject.8. The method of claim 1 , wherein the guaiacol is administered in a dosage from about 22.5 to 180 milligrams of guaiacol per kilogram of the subject.9. The method of claim 1 , wherein the guaiacol is administered in a dosage from about 22.5 to 720 milligrams of guaiacol per kilogram of the subject.1033.-. (canceled)34. A method for screening or identifying an agent for the prevention and/or treatment of a disease or disorder characterized by ...

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Номер записи: 34
26-01-2017 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20170022148A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 2. A molecule according to wherein R1 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , haloethyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , methoxy claim 1 , ethoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , halomethoxy claim 1 , haloethoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , and halo(C)alkoxy.3. A molecule according to wherein R2 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , haloethyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , methoxy claim 1 , ethoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , halomethoxy claim 1 , haloethoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , and halo(C)alkoxy.4. A molecule according to wherein R3 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , ...

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Номер записи: 35
10-02-2022 дата публикации

METHODS FOR SYNTHESIS OF OXYPICOLINAMIDES

Номер: US20220041555A1
Автор: CISMESIA Megan A., MUHUHI Joseck M.
Принадлежит: DOW AGROSCIENCES LLC

The present technology relates to processes, mixtures and intermediates useful for making fungicide, florylpicoxamid. Also disclosed herein are processes for addition reactions which suppress epimerization and/or racemization. 2. The process of wherein Pis hydrogen and Pis Pg claim 1 , where Pg is Calkoxycarbonyl or substituted Calkoxycarbonyl.4. The process of wherein Pis hydrogen and Pis Pg claim 1 , where Pg is tosyl (Ts).5. The process of wherein Pis hydrogen and Pis Pg claim 1 , where Pg is nosyl (Ns).6. The process of wherein Pis hydrogen and Pis Pg claim 1 , where Pg is silyl.11. The process of any one of - wherein the amount of acylation catalyst is from 0.5-20 mol % based on the amount of compound III.12. The process of any one of - wherein the mixing occurs under conditions further comprising an aprotic organic solvent.13. The process of wherein the solvent is heptanes.14. The process of any one of - wherein the mixing occurs under conditions further comprising heating the mixture to about 65° C.16. The process of any one of - wherein compound I is in 99% de.17. A mixture comprising two or more compounds of formula I; wherein one compound is in 97% de.18. A mixture comprising two or more compounds of formula I; wherein one compound is in 98% de.19. A mixture comprising two or more compounds of formula I; wherein one compound is in 99% de.20. A mixture comprising two or more compounds of formula I; wherein one compound is in 99.5% de. This is a national phase entry under 35 U.S.C § 371 of international patent application PCT/US19/55771, filed on Oct. 11, 2019 and published in English as international patent publication WO 2020/081382, which claims priority to the benefit of U.S. Provisional Patent Application Ser. No. 62/745,684 filed Oct. 15, 2018, the disclosure of which is hereby incorporated by reference in its entirety.Particular small molecules of the 4-methoxy-3-(acetyl or acetyloxymethyl) oxypicolinamide persuasion are of interest as being ...

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Номер записи: 36
29-01-2015 дата публикации

AMINOALKYL-SUBSTITUTED N-THIENYLBENZAMIDE DERIVATIVE

Номер: US20150031727A1
Автор: Hachiya Shunichiro, Isomura Mai, KAGA Daisuke, MIURA Masanori, Okuda Takao, Sato Ippei, Terada Yoh, Terai Kazuhiro, Watanuki Susumu
Принадлежит: Astellas Pharma Inc.

[Problem] To provide a compound that has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. 2. The compound or a salt thereof or hydrate thereof according to claim 1 , wherein in formula (I) claim 1 , Rrepresents lower alkyl or cycloalkyl.3. The compound or a salt thereof or hydrate thereof according to claim 2 , wherein in formula (I) claim 2 , n represents 1 claim 2 , and Rrepresents H claim 2 , lower alkyl claim 2 , or lower alkylene-OR.4. The compound or a salt thereof or hydrate thereof according to claim 3 , wherein in formula (I) claim 3 , Y represents lower alkylene which may be substituted with a hydroxyl group.5. The compound or a salt thereof or hydrate thereof according to claim 4 , wherein in formula (I) claim 4 , Xrepresents CH claim 4 , and k represents 1.6. The compound or a salt thereof or hydrate thereof according to claim 5 , wherein in formula (I) claim 5 , both the Xand Xrepresent CH.7. The compound of claim 1 , wherein said compound is selected from the group consisting of:4-(2-{4-[({2-[(3-{[{2-[(3-carboxypropanoyl)(methyl)amino]ethyl}(pentan-3-yl)amino]methyl}benzoyl)amino]-4,5,6,7-tetrahydro-1-benzothiophen-3-yl}carbonyl)amino]phenyl}ethyl)benzoic acid;4-(2-{4-[({2-[(3-{[{2-{[(carboxymethoxy)carbonyl](methyl)amino}ethyl)(pentan-3-yl)amino]methyl}benzoyl)amino]-4,5,6,7-tetrahydro-1-benzothiophen-3-yl}carbonyl)amino]phenyl}ethyl)benzoic acid;4-(2-{4-[({2-[(3-{[{2-[(4-carboxy-4-methylpentanoyl)(methyl)amino]ethyl}(pentan-3-yl)amino]methyl}benzoyl)amino]-4,5,6,7-tetrahydro-1-benzothiophen-3-yl}carbonyl)amino]phenyl}ethyl)benzoic acid;4-(2-{4-[({2-[(3-{[{3-[(3-carboxypropanoyl)(methyl)amino]propyl}(pentan-3-yl)amino]methyl}benzoyl)amino]-4,5,6,7-tetrahydro-1-benzothiophen-3-yl}carbonyl)amino]phenyl}ethyl)benzoic acid;4-(2-{4-[({2-[(3-{[{2-[(3-carboxypropanoyl)(2-methoxyethyl)amino]ethyl}(pentan-3-yl)amino]methyl}benzoyl)amino]-4,5,6,7- ...

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Номер записи: 37
04-02-2021 дата публикации

TREATMENT OF POST-BARIATRIC HYPOGLYCEMIA USING MINI-DOSE STABLE GLUCAGON

Номер: US20210030847A1
Автор: NEWSWANGER Brett, PATTI Mary-Elizabeth, PRESTRELSKI Steven J.
Принадлежит:

Post-bariatric hypoglycemia (PBH) is an increasingly-recognized complication of gastric bypass surgery. Current therapeutic options have suboptimal efficacy. Small doses of stable liquid glucagon can be used to treat or prevent post-bariatric hypoglycemia. 135-. (canceled)36. A method of preventing or treating hypoglycemia in a post-bariatric surgery subject comprising:(a) determining whether or not the post-bariatric surgery subject is at risk of developing post-bariatric hypoglycemia (PBH); and(b) administering a therapeutic formulation comprising a glucagon peptide, a glucagon analog, or salts thereof to the subject if the subject is determined to be at risk of developing PBH.37. The method of claim 36 , further comprising monitoring the subject's blood glucose levels.38. The method of claim 36 , wherein the hypoglycemia is a post-prandial hypoglycemia episode.39. The method of claim 36 , wherein the hypoglycemia is a severe hypoglycemia episode.40. The method of claim 38 , wherein the subject's post-prandial blood glucose levels are decreasing and are below 100 claim 38 , 90 claim 38 , 80 claim 38 , 70 claim 38 , 60 claim 38 , or 50 mg/dL.41. The method of claim 40 , wherein the subject's blood glucose falls below 100 claim 40 , 90 claim 40 , 80 claim 40 , 70 claim 40 , 60 claim 40 , or 50 mg/dL within 90 claim 40 , 80 claim 40 , 70 claim 40 , 60 claim 40 , 50 claim 40 , 40 claim 40 , 30 claim 40 , 25 claim 40 , 20 claim 40 , 15 claim 40 , 10 claim 40 , 9 claim 40 , 8 claim 40 , 7 claim 40 , 6 claim 40 , 5 claim 40 , 4 claim 40 , 3 claim 40 , 2 claim 40 , or 1 minutes after a meal.42. The method of claim 36 , wherein the therapeutic formulation is administered 10 to 90 minutes after a meal.43. The method of claim 37 , wherein the therapeutic formulation is administered when the subject's blood glucose decreases by 0.5 to 10 mg/dL/min 90 claim 37 , 80 claim 37 , 70 claim 37 , 60 claim 37 , 50 claim 37 , 40 claim 37 , 30 claim 37 , 25 claim 37 , 20 claim 37 , 15 ...

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Номер записи: 38
30-01-2020 дата публикации

SUBSTITUTED PHENYLPROPIONIC ACID ENANTIOMER AND MANUFACTURING METHOD, COMPOSITION, AND APPLICATION OF SAME

Номер: US20200031771A1
Автор: Li Zhibin, LU Xianping, PAN Desi, SHAN Song, YU Jindi
Принадлежит: Shenzhen Chipscreen Biosciences Co., Ltd.

The present invention discloses an enantiomeric compound (−)-2-[(2-(4-fluorobenzoyl)phenyl)amine]-3-[(4-(2-carbazole-ethoxy)phenyl)]propionic acid as represented by formula (I), or a pharmaceutical salt thereof, and a manufacturing method of the compound and application of same. The enantiomeric compound demonstrates relatively better activation of RXR/PPAR-, RXR/PPAR- and RXR/PPAR-heterodimer expression and sugar reduction in a db/db mouse model compared to a (+)-enantiomer. 1. (−)-2-[(2-(4-fluorobenzoyl)phenyl)amino]-3-[(4-(2-carbazole-ethoxy)phenyl)]propionic acid or a pharmaceutically acceptable salt thereof.2. The (−)-2-[(2-(4-fluorobenzoyl)phenyl)amino]-3-[(4-(2-carbazole-ethoxy) phenyl)]propionic acid or a pharmaceutically acceptable salt thereof according to claim 1 , wherein the salt is an alkali metal salt claim 1 , an alkaline earth metal salt claim 1 , an ammonium salt or a quaternary ammonium salt.3. The (−)-2-[(2-(4-fluorobenzoyl)phenyl)amino]-3-[(4-(2-carbazole-ethoxy) phenyl)]propionic acid or a pharmaceutically acceptable salt thereof according to claim 2 , wherein the alkali metal salt is a sodium or potassium salt claim 2 , and/or the alkaline earth metal salt is a calcium or magnesium salt.4. A supercritical chromatography method for preparing the (−)-2-[(2-(4-fluorobenzoyl)phenyl)amino]-3-[(4-(2-carbazole-ethoxy)phenyl)]propionic acid according to claim 1 , comprising the steps of:dissolving 2-[(2-(4-fluorobenzoyl)phenyl)amino]-3-[(4-(2-carbazole-ethoxy)phenyl)] propionic acid in a solvent, loading the solution to a chiral chromatography column, eluting sequentially with a solvent mixture of organic solvent/carbon dioxide and a solvent mixture of organic solvent/carbon dioxide/aqueous ammonia and separating, to obtain (−)-2-[(2-(4-fluorobenzoyl)phenyl)amino]-3-[(4-(2-carbazole-ethoxy)phenyl)]propionic acid.5. Use of (−)-2-[(2-(4-fluorobenzoyl)phenyl)amino]-3-[(4-(2-carbazole-ethoxy)phenyl)]propionic acid or a pharmaceutically acceptable salt in ...

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Номер записи: 39
30-01-2020 дата публикации

CONDENSED THIOPHENE DERIVATIVES USEFUL AS NAPI-IIB INHIBITORS

Номер: US20200031813A1
Автор: Coates David Andrew, Fales Kevin Robert, II Jeffrey Michael, II John Rowley, Peterson Jeffrey Allen, Schkeryantz, Shen Quanrong `, Valli Matthew John, Wetterau, Wodka Dariusz Stanislaw, XU Yanping
Принадлежит:

The invention provides compounds of the formula: (A), pharmaceutically acceptable salts, pharmaceutical compositions thereof and methods of using these compounds, salts, or compositions to treat hyperphosphatemia, chronic kidney disease, and/or the cardiovascular disease associated with chronic kidney disease. 5. The compound of wherein R′ is —COH claim 4 , or a pharmaceutically acceptable salt thereof.14. A compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , selected from the group consisting of:4-[2-[2,6-difluoro-4-[[2-[[3-[(2,2,4-trimethylpiperazin-1-yl)methyl]benzoyl]amino]-4,5,6,7-tetrahydrobenzothiophene-3-carbonyl]amino]phenyl]ethyl]benzoic acid formic acid salt;4-[2-[4-[[2-[[3-[[2,2-dimethyl-4-(methylcarbamoyl)piperazin-1-yl]methyl]benzoyl]amino]-4,5,6,7-tetrahydrobenzothiophene-3-carbonyl]amino]-2,6-difluoro-phenyl]ethyl]benzoic acid;4-[2-[4-[[2-[[3-[[2,2-dimethyl-4-(methylcarbamothioyl)piperazin-1-yl]methyl]benzoyl]amino]-4,5,6,7-tetrahydrobenzothiophene-3-carbonyl]amino]-2,6-difluoro-phenyl]ethyl]benzoic acid;4-[2-[4-[[2-[[3-[[4-(2-carboxyethylcarbamoyl)-2,2-dimethyl-piperazin-1-yl]methyl]benzoyl]amino]-4,5,6,7-tetrahydrobenzothiophene-3-carbonyl]amino]-2,6-difluoro-phenyl]ethyl]benzoic acid;4-[2-[2,6-difluoro-4-[[2-[[3-[[8-(methylcarbamoyl)-3,8-diazabicyclo[3.2.1]octan-3-yl]methyl]benzoyl]amino]benzothiophene-3-carbonyl]amino]phenyl]ethyl]benzoic acid, formic acid salt;4-[2-[2,6-difluoro-4-[[2-[[3-[(4-methoxycarbonyl-2,2-dimethyl-piperazin-1-yl)methyl]benzoyl]amino]-4,5,6,7-tetrahydrobenzothiophene-3-carbonyl]amino]phenyl]ethyl]benzoic acid;4-(2,6-difluoro-4-(2-(3-(((1R,5S)-8-pentanoyl-3,8-diazabicyclo[3.2.1]octan-3-yl)methyl)benzamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamido)phenethyl)benzoic acid;4-[2-[4-[[2-[[3-[[2,2-dimethyl-4-(methyl sulfamoyl)piperazin-1-yl]methyl]benzoyl]amino]-4,5,6,7-tetrahydrobenzothiophene-3-carbonyl]amino]-2,6-difluoro-phenyl]ethyl]benzoic acid;4-[2-[2,6-difluoro-4-[[2-[[3-[[8-( ...

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Номер записи: 40
09-02-2017 дата публикации

PROCESS FOR PREPARING N-METHYL-4-BENZYLCARBAMIDOPYRIDINIUM CHLORIDE

Номер: US20170037011A1
Автор: Kostiuk Grygorii, Margitych Viktor, Vanat Mykhailo, Zhebrovska Filya
Принадлежит:

The present application relates to a new salt of N-methyl-4-benzylcarbami-dopyridine, a process for its preparation, a pharmaceutical composition comprising this compound and its use for the treatment or prevention of viral diseases. 2. The process according to wherein a solvent selected from the group consisting of 2-propanol claim 1 , aqueous ethanol and acetonitrile is used.3. The process of wherein the process is carried out at a temperature in the range of 50-120° C. and under pressure.4. The process according to wherein the reaction is carried out in acetonitrile with heating and permanent passing of chloromethane gas through the reaction mixture without any pressure application.5. The process of wherein the reaction time is in the range from 1-20 h.6. The process according to wherein the molar ratio between isonicotinic acid benzylamide and chloromethane is in the range of 1-1.5.7. The process according to wherein the solvent is ethanol 96% claim 2 , wherein the reaction is carried out at a pressure in the range of 0.1-1 MPa (1-10 bar) and wherein the molar ratio between isonicotinic acid benzylamide and chloromethane is in the range of 1-1.5.8. The process according to claim 1 , further comprising the step of recrystallisation of the raw product from ethanol 96%.917-. (canceled)18. The process of wherein the N-methyl-4-benzylcarbamidopyridinium chloride comprises impurities in the range of less than 0.5%.19. The process of wherein the N-methyl-4-benzylcarbamidopyridinium chloride comprises impurities in the range of less than 0.05%.20. The process of wherein the N-methyl-4-benzylcarbamidopyridinium has a melting temperature in the range of 198° C. to 203° C. The present invention relates to a process for the preparation of N-methyl-4-benzylcarbamidopyridinium chloride, to the compound obtained by this process, to pharmaceutical compositions comprising this compound and their use in the treatment or prevention of viral diseases.N-methyl-4- ...

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Номер записи: 41
14-02-2019 дата публикации

Anhydrate-Free Polymorphically Pure Micronized Crystalline Brexpiprazole Di-Hydrate For Use In Intramuscular Injectable Sustained Release Formulations

Номер: US20190047994A1
Автор: BORN Max, Langes Christoph, Lengauer Hannes
Принадлежит: HEXAL AG

The present invention relates to a brexpiprazole dihydrate crystalline form having a particle size distribution of d50 of at most 10 μm and less than 5% w/w of brexpiprazole anhydrate. The present invention also relates to a process for preparing this brexpiprazole dihydrate crystalline form and to pharmaceutical compositions thereof. The present invention also relates to a process for determining the absence of brexpiprazole anhydrate in this brexpiprazole dihydrate crystalline form. This brexpiprazole dihydrate crystalline form is used for the preparation of pharmaceutical compositions having delayed release properties upon intramuscular injection. 1. Brexpiprazole dihydrate in the form of crystalline material having a particle size distribution characterized by a d50 of at most 10 μm , the crystalline material comprising less than 5% w/w of brexpiprazole anhydrate in relation to the total amount of brexpiprazole.2. The brexpiprazole dihydrate of claim 1 , wherein the crystalline material comprises no detectable brexpiprazole anhydrate.3. The brexpiprazole dihydrate of claim 1 , characterized by having a PXRD wherein a peak at 10.0°+/−0.2° 2-Theta is absent.4. The brexpiprazole dihydrate according to claim 1 , characterized by having an PXRD comprising peaks at 2-theta angles of 8.1° claim 1 , 8.9° claim 1 , 15.1° claim 1 , 15.6° and 24.4° claim 1 , and further characterized by the absence of peaks at 2-theta angles of 6.8°+/−0.2° and 17.4°+/−0.2°.5. The brexpiprazole dihydrate according to claim 1 , characterized by a d90 of at most 25 μm.6. The brexpiprazole dihydrate according to claim 1 , which is obtainable or obtained by micronization.7. A process for the preparation of brexpiprazole dihydrate in the form of crystalline material having a particle size distribution characterized by a d50 of at most 10 μm comprising:(i) providing brexpiprazole dihydrate in the form of crystalline material having a particle size distribution characterized by a d50 of at least ...

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Номер записи: 42
13-02-2020 дата публикации

METHOD FOR PREPARING METHYL 4-[(4,5-DIHYDRO-3-METHOXY-4-METHYL-5-OXO-1H-1,2,4-TRIAZOL-1-YL)CARBONYL)SULFAMOYL]-5-METHYLTHIOPHENE-3-CARBOXYLATE

Номер: US20200048234A1
Автор: Ford Mark James, Funke Christian, Muehlthau Friedrich August, Neeff Arnd, PAZENOK Sergii, SCHIFFER Klaus-Ulrich
Принадлежит:

The invention relates to a method for preparing methyl 4-[(4,5-dihydro-3-methoxy-4-methyl-5-oxo-1H-1,2,4-triazol-1-yl)carbonyl)sulfamoyl]-5-methylthiophene-3-carboxylate from 4-methoxycarbonyl-2-methylthiophene-3-sulfonyl chloride in the presence of an imidazole base substituted in the 1-position or in the presence of a mixture of bases comprising an imidazole base substituted in the 1-position (N-alkylimidazole). 2. The method for preparing a compound of formula (I) according to claim 1 , wherein Ris an unsubstituted (C-C)-alkyl or an unsubstituted benzyl.3. The method for preparing a compound of formula (I) according to claim 2 , wherein Ris an unsubstituted (C-C)-alkyl.4. The method for preparing a compound of formula (I) according to claim 3 , wherein Ris methyl claim 3 , ethyl claim 3 , n-propyl or n-butyl.5. The method for preparing a compound of formula (I) according to claim 4 , wherein Ris methyl.6. The method for preparing a compound of formula (I) according to claim 1 , wherein Me in a compound of formula MeOCN (III) is Na or K.7. The method for preparing a compound of formula (I) according to claim 1 , wherein the reaction is carried out in a polar solvent selected from the group consisting of acetonitrile claim 1 , butyronitrile claim 1 , tetrahydrofuran (THF) claim 1 , methyl-THF claim 1 , dimethoxyethane claim 1 , sulfolane claim 1 , dimethylformamide and dimethylacetamide.8. The method for preparing a compound of formula (I) according to claim 1 , wherein the reaction is carried out in a solvent mixture comprising acetonitrile and THF.9. The method for preparing a compound of formula (I) according to claim 1 , wherein the reaction is conductedin a temperature range of 20° to 110° andin a reaction time of 3 hours to 24 hours.10. The method for preparing a compound of formula (I) according to claim 9 , wherein the reaction is conducted in a temperature range of 30° to 90°.11. The method for preparing a compound of formula (I) according to claim 10 , ...

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Номер записи: 43
08-05-2014 дата публикации

DEUTERATED OMEGA DIPHENYLUREA RELATED COMPOUNDS AND INTERMEDIATES

Номер: US20140128612A1
Автор: Dai Xiaojun, Feng Weidong, Gao Xiaoyong
Принадлежит: SUZHOU ZELGEN BIOPHARMACEUTICAL CO., LTD.

Methods and processes for preparation and production of deuterated ω-diphenylurea are disclosed. Especially, a kind of deuterated ω-diphenylurea compounds which can inhibit phosphokinase and the preparation method of N-(4-chloro-3-(trifluoromethyl)phenyl)-N′-(4-(2-(N-d3-methylcarbamoyl)-4-pridinyloxy)phenyl)urea are disclosed. The said deuterated diphenylurea compounds can be used for treating or preventing tumors and relative diseases. 2. The intermediate of formula (B) according to claim 1 , wherein Y is chlorine.4. A p-toluene sulfonate of a deuterated ω-diphenylurea compound being 4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl]ureido)-phenoxy)-N-(methyl-d)picolinamide p-toluenesulfonate (CM4307.TsOH). This application is a divisional of U.S. application Ser. No. 13/635,822, filed Sep. 19, 2012, which is a Section 371 of Internation Application No. PCT/CN2011/071926, filed Mar. 17, 2011, which was published in the Chinese language on Sep. 22, 2011, under Internation Publication No. WO 2011/113367 A1 the disclosure of which is incorporated herein by reference.This invention relates to the field of chemical synthesis, and particularly relates to the methods and processes for preparation and production of deuterated ω-diphenylurea.Ω-diphenylurea derivatives are known compounds with c-RAF kinase inhibition activity. For example, WO2000/042012 had disclosed a class of ω-carboxyl-aryl-substituted diphenylurea and the use thereof for treating cancer and related diseases.Initially, ω-diphenylurea compounds, such as Sorafenib, were firstly found as the inhibitor of c-RAF kinase. The other studies had shown that they could also inhibit the MEK and ERK signal transduction pathways and activities of tyrosine kinases including vascular endothelial growth factor receptor-2 (VEGFR-2), vascular endothelial growth factor receptor-3 (VEGFR-3), and platelet-derived growth factor receptor-β (PDGFR-β) (Curr Pharm Des 2002, 8, 2255-2257). Therefore, they were called multi-kinase ...

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Номер записи: 44
10-03-2022 дата публикации

Method for Preparing Indolenaphthopyrans

Номер: US20220073533A1
Автор: Stayshich Ryan, Walters Robert W.
Принадлежит:

Provided is a synthetic intermediate for the preparation of photochromic indolenaphthopyran compounds having the core skeletal structure of Formula (I): wherein m is 0 to 4, n is 0 to 4, Rand Rare each independently hydroxyl, cyano, (meth)acrylate, amino, halo, substituted or unsubstituted alkyl, boronic ester, boronic acid, polyether, polyester, polycarbonate, polyurethane, substituted or unsubstituted aryl, substituted or unsubstituted heterocycloaryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryloxy, substituted or unsubstituted alkylthio, substituted or unsubstituted arylthio, ketone, aldehyde, ester, carboxylic acid, carboxylate, amide, carbonate, carbamate, urea, siloxane, alkoxysilane, or polysiloxane; Ris substituted or unsubstituted 2-pyridyl or substituted or unsubstituted 2-quinolyl; and Ris hydrogen, substituted or unsubstituted alkyl, alkoxymethyl, substituted or unsubstituted silyl, or acyl. Also provided is a process for producing an indolenaphthol compound which includes cyclizing the phenylnaphthol compound of Formula (I) in the presence of a catalyst. 2. The phenylnaphthol compound of claim 1 , wherein each alkyl substituent claim 1 , each aryl substituent claim 1 , each heterocycloalkyl substituent claim 1 , each heteroaryl substituent claim 1 , each alkoxy substituent claim 1 , each aryloxy substituent claim 1 , each alkylthio substituent claim 1 , each arylthio substituent claim 1 , and each each silyl substituent is in each case independently selected from halogen claim 1 , cyano claim 1 , nitro claim 1 , alkyl claim 1 , alkenyl claim 1 , alkynyl claim 1 , haloalkyl claim 1 , perhaloalkyl claim 1 , heterocycloalkyl claim 1 , aryl claim 1 , heteroaryl claim 1 , alkoxy claim 1 , hydroxyl claim 1 , alkylthio claim 1 , arylthio claim 1 , ketone claim 1 , aldehyde claim 1 , ester claim 1 , carboxylic acid claim 1 , carboxylate claim 1 , siloxane claim 1 , alkoxysilane claim 1 , ...

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Номер записи: 45
02-03-2017 дата публикации

PROCESS FOR THE PREPARATION OF 4-CARBONYL)AMINO]-3-FLUOROPHENOXY}-N-ETHYLPYRIDINE-2-CARBOXAMIDE, ITS SALTS AND MONOHYDRATE

Номер: US20170057918A1
Автор: Gottfried Michael, Heilmann Werner, Lögers Michael, Rehse Joachim, Stiehl Juergen, Wichmann Saskia
Принадлежит: Bayer Intellectual Property GmbH

The present invention relates to a process for preparing 4-{4-[({[4-chloro-3-(trifluoromethyl)-phenyl]amino}carbonyl)amino]-3-fluorophenoxy}-N-methylpyridine-2-carboxamide, its salts and monohydrate. 2. The process of for preparing the monohydrate of the compound of the formula (I) wherein the salt of the compound of the formula (I) is then treated with an aqueous basic solution to precipitate the monohydrate of the compound of the formula (I).3. The process of wherein the monohydrate of the compound of the formula (I) precipitates at a temperature of from 35° C. to 45° C.4. The process of for preparing of the compound of the formula (I) wherein the monohydrate is dried under reduced pressure until the compound of the formula (I) is formed.5. The process of wherein the solution comprising the solved compound of the formula (I) and what from the salt of the compound of the formula (I) precipitates is the reaction mixture or is a separate solution of the compound of the formula (I) prepared after isolation of the compound of the formula (I) from the reaction mixture.6. The process of wherein the acid is generated in situ in the reaction mixture after the compound of the formula (I) is formed by adding to the reaction mixture a protic substance and an acid precursor.7. The process of wherein the acid is generated in situ in the reaction mixture after the compound of the formula (I) is formed by adding to the reaction mixture an alcohol and an acylchloride.8. The process of wherein the alcohol is ethanol and the acylchloride is acetylchloride.11. The process of wherein the compound of the formula (II) is used in a solution of a suitable organic solvent which solution is prepared by neutralization the hydrochloric acid salt of the compound of the formula (II) with a base.12. The process of wherein the compound of the formula (II) it is solved in a suitable organic solvent claim 9 , treated with an acid which is generated in situ by adding a protic substance and an acid ...

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Номер записи: 46
17-03-2022 дата публикации

AMIDE COMPOUNDS AND PREPARATION METHOD THEREFOR AND USE THEREOF

Номер: US20220081389A1
Автор: DU Yonglei, LIU Jiyong, LV Liang, NI Jueping, XIANG Juncheng, ZHOU Liqi
Принадлежит:

Provided are amide compounds and a preparation method therefor and the use thereof. The amide compounds have a structure represented by formula I. The amide compounds of the present invention have high insecticidal activity at a low dosage and have a good fast-acting property. The dosage of the pesticide will be reduced during application due to the good insecticidal activity of the amide compounds at low dosage, which is more conducive to environmental protection and has broad application prospect. 2. The amide compound according to claim 1 , wherein claim 1 , Z claim 1 , Z claim 1 , Z claim 1 , Z claim 1 , and Zare independently of each other H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , i-propyl claim 1 , c-propyl claim 1 , n-butyl claim 1 , t-butyl claim 1 , i-butyl claim 1 , n-pentyl claim 1 , 1-methylbutyl claim 1 , 2-methylbutyl claim 1 , 3-methylbutyl claim 1 , 1 claim 1 ,1-dimethylpropyl claim 1 , 1 claim 1 ,2-dimethylpropyl claim 1 , 2 claim 1 ,2-dimethylpropyl claim 1 , methoxyl claim 1 , ethoxyl claim 1 , n-propoxyl claim 1 , i-propoxyl claim 1 , t-butoxyl claim 1 , trifluoromethyl claim 1 , pentafluoroethyl claim 1 , heptafluoropropyl claim 1 , heptafluoroisopropyl claim 1 , difluoromethoxyl claim 1 , trifluoromethoxyl claim 1 , pentafluoroethoxyl claim 1 , methylsulfinyl claim 1 , trifluoromethylsulfinyl claim 1 , methylsulfonyl or trifluoromethylsulfonyl;{'sub': '2', 'Ris H, methyl, ethyl, n-propyl, i-propyl, n-butyl, i-butyl, t-butyl, n-pentyl, 2-pentyl, neopentyl, isopentyl, 4-methyl-2-pentyl, n-hexyl, monofluoromethyl, difluoromethyl, trifluoromethyl, monochloromethyl, dichloromethyl, trichloromethyl, pentafluoroethyl, heptafluoroisopropyl, cyclopropyl, cyclobutyl, cyclopentyl, perfluorocyclopropyl, perfluorocyclobutyl or perfluorocyclopentyl; and'}{'sub': '3', 'Ris H, F or Cl.'}3. The amide compound according to claim 1 , wherein claim 1 , Z claim 1 , Z ...

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Номер записи: 47
08-03-2018 дата публикации

DEUTERIUM-ENRICHED HYPOXIA-INDUCIBLE FACTOR PROLYL HYDROXYLASE ENZYME INHIBITORS

Номер: US20180065933A1
Автор: Hanselmann Roger
Принадлежит: Akebia Therapeutics, Inc.

Provided herein are deuterium-enriched compounds of Formula (I), Formula (II), Formula (III), Formula (IV), Formula (V), and Formula (VI). Pharmaceutical compositions comprising the isotope-enriched compounds, and methods of using such compounds are also provided. 2. The compound of claim 1 , wherein one of Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , and Yis isotopically enriched with deuterium claim 1 , and the others are non-enriched hydrogens.3. The compound of claim 1 , wherein two of Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , Y claim 1 , and Yare isotopically enriched with deuterium claim 1 , and the others are non-enriched hydrogens.4. The compound of claim 1 , wherein Y claim 1 , Y claim 1 , and Yare hydrogen.6. The compound of claim 5 , wherein one of Y claim 5 , Y claim 5 , Y claim 5 , Y claim 5 , Y claim 5 , Y claim 5 , Y claim 5 , Y claim 5 , YYand Yis isotopically enriched with deuterium claim 5 , and the others are non-enriched hydrogens.7. The compound of claim 5 , wherein two of Y claim 5 , Y claim 5 , Y claim 5 , Y claim 5 , Y claim 5 , Y claim 5 , Y claim 5 , Y claim 5 , Y claim 5 , Y claim 5 , and Yare isotopically enriched with deuterium claim 5 , and the others are non-enriched hydrogens.8. The compound of claim 5 , wherein Y claim 5 , Y claim 5 , and Yare hydrogen.10. The compound of claim 9 , wherein one of Y claim 9 , Y claim 9 , Y claim 9 , Y claim 9 , Y claim 9 , Y claim 9 , Y claim 9 , Y claim 9 , Y claim 9 , Yand Yis isotopically enriched with deuterium claim 9 , and the others are non-enriched hydrogens.11. The compound of claim 9 , wherein two of Y claim 9 , Y claim 9 , Y claim 9 , Y claim 9 , Y claim 9 , Y claim 9 , Y claim 9 , Y claim 9 , Y claim 9 , Y claim 9 , and Yare ...

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Номер записи: 48
09-03-2017 дата публикации

DIHYDRATE OF BENZOTHIOPHENE COMPOUND OR OF A SALT THEREOF, AND PROCESS FOR PRODUCING THE SAME

Номер: US20170066752A1
Автор: ETO Ryohei, HOSHIKA Yusuke, IKEBUCHI Takuma, Ito Nobuaki, KAWANO Shuuji, MINOWA Takuya, MORIYAMA Kei, Nakamura Takayuki, SATO Tetsuya, SOTA Masahiro, TOYOFUKU Hidekazu, Yamaguchi Tetsuya, Yamashita Hiroshi
Принадлежит: OTSUKA PHARMACEUTICAL CO., LTD.

An object of the present invention is to provide a compound that can be used as a more superior therapeutic agent for central nervous system diseases. The present invention provides a dihydrate of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or of a salt thereof, and a process for producing the same. 1. A dihydrate of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or of a salt thereof.2. The dihydrate according to which has characteristic peaks at diffraction angles (2θ) of 8.1° claim 1 , 8.9° claim 1 , 15.1° claim 1 , 15.6° claim 1 , and 24.4° in an X-ray powder diffraction pattern measured by copper radiation of λ=1.5418 Å through a monochromator.3. The dihydrate according to which has characteristic peaks at 3509 cm claim 1 , 2934 cm claim 1 , 2812 cm claim 1 , 1651 cm claim 1 , 1626 cm claim 1 , 1447 cm claim 1 , 1223 cm claim 1 , and 839 cmin an infrared absorption spectrum as measured by a potassium bromide tablet method.4. The dihydrate according to which has characteristic peaks at 1497 cm claim 1 , 1376 cm claim 1 , 1323 cm claim 1 , 1311 cm claim 1 , 1287 cm claim 1 , 1223 cm claim 1 , and 781 cmin a Raman spectrum.5. The dihydrate according to which contains water in an amount of 6.5 to 8.8 wt. %.6. The dihydrate according to which has peaks in a H-NMR spectrum at:1.64 ppm (tt, J=7.4 Hz, J=7.4 Hz, 2H),1.80 ppm (tt, J=7.0 Hz, J=7.0 Hz, 2H),2.44 ppm (t, J=7.5 Hz, 2H),2.62 ppm (br, 4H),3.06 ppm (br, 4H),{'sub': '2', '3.32 ppm (s, 4H+HO),'}4.06 ppm (t, J=6.5 Hz, 2H),6.29 ppm (d, J=9.5 Hz, 1H),6.80 ppm (d, J=2.5 Hz, 1H),6.80 ppm (dd, J=2.5 Hz, J=9.0 Hz, 1H),6.88 ppm (d, J=7.5 Hz, 1H),7.27 ppm (dd, J=7.8 Hz, J=7.8 Hz, 1H),7.40 ppm (dd, J=5.5 Hz, 1H),7.55 ppm (d, J=9.0 Hz, 1H),7.61 ppm (d, J=8.0 Hz, 1H),7.69 ppm (d, J=5.5 Hz, 1H),7.80 ppm (d, J=9.5 Hz, 1H), and11.57 ppm (s, 1H),7. A process for producing a dihydrate of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or of a salt thereof ...

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Номер записи: 49
11-03-2021 дата публикации

Process for Preparing 2-[[5-(3-Chlorophenyl)-3-Hydroxypyridine-2-Carbonyl]Amino]Acetic Acid

Номер: US20210070709A1
Автор: Copp James Densmore, Gonzalez Javier, Gorin Boris I., Lanthier Christopher M., Luong Anne Buu Chau
Принадлежит:

Disclosed herein are methods and processes of preparing vadadustat and pharmaceutically acceptable salts thereof, and intermediates of formula (I) and their salts useful for the synthesis of vadadustat. 2. The process of claim 1 , wherein Ris t-butyl.3. The process of or claim 1 , wherein Ris methyl.4. The process of any one of - claim 1 , wherein the hydrolyzing agent comprises an acid.5. The process of any one of - claim 1 , wherein the hydrolyzing agent comprises a base.6. The process of claim 5 , wherein the base is an alkali metal hydroxide claim 5 , alkali metal carbonate claim 5 , Polymer-SK or tetrabutylammonium fluoride (TBAF).7. The process of claim 5 , wherein the base is an alkali metal hydroxide selected from lithium hydroxide (LiOH) claim 5 , sodium hydroxide (NaOH) claim 5 , potassium hydroxide (KOH) claim 5 , cesium hydroxide (CsOH) claim 5 , and any combination thereof.8. The process of claim 5 , wherein the base is an alkali metal carbonate selected from lithium carbonate (LiCO) claim 5 , sodium carbonate (NaCO) claim 5 , potassium carbonate (KCO) claim 5 , cesium carbonate (CsCO) claim 5 , and any combination thereof.9. The process of claim 7 , wherein the alkali metal hydroxide is potassium hydroxide (KOH).10. The process of any one of - claim 7 , which occurs in presence of a solvent comprising N claim 7 ,N-dimethylformide (DMF) claim 7 , t-butanol claim 7 , dimethoxyethane (DME) claim 7 , acetonitrile claim 7 , dichloromethane (DCM) claim 7 , tetrahydrofuran (THF) claim 7 , 2-methyltetrahydrofuran (ME-THF) claim 7 , isopropyl alcohol claim 7 , methanol claim 7 , ethanol claim 7 , or any combination thereof.11. The process of claim 10 , wherein the solvent comprises 2-methyltetrahydrofuran (ME-THF).12. The process of any one of - claim 10 , wherein the purity of the compound of Formula (8) is at least 99%.14. The process of claim 13 , wherein step c) is required.15. The process of or claim 13 , wherein the compound of Formula (I) comprises less ...

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Номер записи: 50
24-03-2022 дата публикации

FLUORINE-CONTAINING SUBSTITUTED BENZOTHIOPHENE COMPOUND, AND PHARMACEUTICAL COMPOSITION AND APPLICATION THEREOF

Номер: US20220089561A1
Автор: Ding Chunyong, DING Jian, Geng Meiyu, SHEN Ancheng, WANG Xiyuan, XIE Zuoquan, Zhang Ao, Zhang Yan
Принадлежит:

A fluorine-containing substituted benzothiophene compound and a pharmaceutical composition and an application thereof are described. The compound has the structure as shown in formula (I), in which the definitions of each group and substituent are as described in the description. A preparation method of the compound and an anti-tumor application thereof are also described. 2. The compound claim 1 , or its isomer claim 1 , prodrug claim 1 , solvate claim 1 , hydrate or pharmaceutically acceptable salt thereof according to claim 1 , wherein Xis halogen.3. The compound claim 2 , or its isomer claim 2 , prodrug claim 2 , solvate claim 2 , hydrate or pharmaceutically acceptable salt thereof according to claim 2 , wherein Xis hydrogen or fluorine.4. The compound claim 1 , or its isomer claim 1 , prodrug claim 1 , solvate claim 1 , hydrate or pharmaceutically acceptable salt thereof according to claim 1 , wherein n is an integer selected from 0 claim 1 , 1 or 2.5. The compound claim 1 , or its isomer claim 1 , prodrug claim 1 , solvate claim 1 , hydrate or pharmaceutically acceptable salt thereof according to claim 1 , wherein Y is selected from the group consisting of —OR claim 1 , and —N(XR)R claim 1 ,wherein,{'sup': '4', 'Xis selected from the group consisting of: O, and NH;'}{'sup': '3', 'Ris selected from the substituted or unsubstituted group consisting of H, carboxy, sulfonic acid group, phosphoryl group, C1-C6 alkyl, C3-C8 cycloalkyl, C6-C10 aryl, 3-10 membered heteroaryl containing 1 to 3 heteroatoms selected from N, O or S, and 3-8 membered heterocycloalkyl containing 1 to 3 heteroatoms selected from N, O or S;'}{'sup': 4', '5, 'Rand Rare independently selected from the substituted or unsubstituted group consisting of H, carboxy, sulfonic acid group, phosphoryl group, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C8 cycloalkyl, C1-C6 alkoxy, C3-C8 cycloalkoxy, C6-C10 aryloxy, C6-C10 aryl, 3-8 membered heterocycloalkyl containing 1 to 3 heteroatoms selected from N ...

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Номер записи: 51
19-03-2015 дата публикации

PHARMACEUTICAL COMPOSITION CONTAINING CRYSTALLINE SORAFENIB TOSYLATE

Номер: US20150080435A1
Автор: Degendorfer Heiko, Raneburger Johannes, Scheler Stefan, Schwarz Franz
Принадлежит: SANDOZ AG

The present invention relates to an oral solid dosage form, in particular a tablet, comprising sorafenib tosylate polymorphic form III. 1. An oral solid dosage form , comprising a crystalline sorafenib tosylate characterized by an X-ray powder diffraction pattern showing peak maxima at 2 theta/° values of 7.7±0.2 , 12.0±0.2 , 19.9±0.2 , and 21.6±0.2 , the X-ray powder diffraction pattern being determined at a temperature of about 22° C. using copper-Kalpha1/2 radiation having a wavelength of 0.15419 nm , and at least one excipient.215-. (canceled)16. The dosage form of claim 1 , comprising a crystalline sorafenib tosylate characterized by a Raman spectrum showing peak maxima at Raman shift/cmvalues of 1715±5 claim 1 , 1601±5 claim 1 , 1334±5 claim 1 , 1268±5 claim 1 , 1033±5 claim 1 , and 1011±5 claim 1 , the Raman spectrum being determined using a laser having a wavelength of 532 nm wherein the exposure time of the sample is 2 s claim 1 , and at least one excipient.17. The dosage form according to claim 1 , comprising at least 90% by weight claim 1 , relative to the total amount of sorafenib tosylate claim 1 , of the crystalline sorafenib tosylate according to18. The dosage form of claim 1 , comprising at most 5% by weight claim 1 , relative to the crystalline sorafenib tosylate according to claim 1 , of a crystalline sorafenib tosylate characterized by an X-ray powder diffraction pattern showing peak maxima at 2 theta/° values of 4.3±0.2 claim 1 , 11.0±0.2 claim 1 , 14.8±0.2 claim 1 , 17.9±0.2 claim 1 , 19.3±0.2 claim 1 , 20.5±0.2 and 20.8±0.2 claim 1 , 21.5±0.2 claim 1 , 22.9±0.2 claim 1 , 24.5±0.2 claim 1 , the X-ray powder diffraction pattern being determined at a temperature of about 22° C. using copper-Kalpha1/2 radiation having a wavelength of 0.15419 nm claim 1 , and/or of a crystalline sorafenib tosylate characterized by a Raman spectrum showing peak maxima at Raman shift/cmvalues of 1688±5 claim 1 , 1612±5 claim 1 , 1601±5 claim 1 , 1325±5 claim 1 , 1310± ...

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Номер записи: 52
24-03-2016 дата публикации

FATTY ACID ACYLATED SALICYLATES AND THEIR USES

Номер: US20160083336A1
Автор: Bemis Jean E., Jirousek Michael R., Milne Jill C., Smith Jesse J., Vu Chi B.
Принадлежит:

The invention relates to fatty acid acylated salicylate derivatives; compositions comprising an effective amount of a fatty acid acylated salicylate derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a fatty acid acylated salicylate derivative. 1. (canceled)3. (canceled)7. (canceled)8. A compound of claim 2 , wherein Q is Z.10. A compound of claim 2 , wherein m is 1 and L is —S—S— or —O—.1138-. (canceled)39. The compound of claim 2 , wherein r is 3 claim 2 , s is 5 and w is 1.40. A method of treating inflammation associated with a metabolic disorder claim 2 , the method comprising administering to a patient in need thereof an effective amount of a compound of .41. The method of claim 40 , wherein the inflammation is associated with inflammatory bowel disease.42. The method of claim 40 , wherein the inflammation is associated with muscular dystrophy.43. The method of claim 40 , wherein the inflammation is associated with cachexia.44. The method of claim 40 , wherein the inflammation is associated with Crohn's disease.45. The method of claim 40 , wherein the inflammation is associated with Type II diabetes.46. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier. This application is a continuation-in-part of U.S. application Ser. No. 12/499,779, filed Jul. 8, 2009, and claims the benefit of U.S. Provisional Application No. 61/148,658, filed Jan. 30, 2009, U.S. Provisional Application No. 61/104,363, filed Oct. 10, 2008, U.S. Provisional Application No. 61/104,364, filed Oct. 10. 2008, U.S. Provisional Application No. 61/104,366, filed Oct. 10, 2008, and U.S. Provisional Application No. 61/078,983, filed Jul. 8, 2008. The entire disclosures of those applications are relied on and incorporated into this application by reference.The invention relates to fatty acid acylated salicylate derivatives, fatty acid acylated diflunisal derivatives, and fatty ...

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Номер записи: 53
12-06-2014 дата публикации

STILBENE-BASED REACTIVE COMPOUNDS, POLYMERIC MATRICES FORMED THEREFROM, AND ARTICLES VISUALIZABLE BY FLUORESCENCE

Номер: US20140162083A1
Автор: Jelle Bruce M., Kurdyumov Aleksey V., Lockwood Nathan A., Swan Dale G.
Принадлежит: SURMODICS, INC.

The invention is directed to latent reactive and polymerizable derivatives of fluorescent stilbene-based compounds. The compounds can be used to provide articles with a fluorescence property, such as medical devices (e.g., catheters). The fluorescent compounds can be used in association with polymers, or can be incorporated into polymers, and the polymers used in a coating composition on the article surface. The compounds allow for visual or machine inspection of coating properties such as uniformity of coverage. 7. The compound of wherein Ris a C1-C4 hydrocarbylene group claim 1 , or a C2 hydrocarbylene group; wherein Ris —OH; or wherein R and R are phenyl.11. The compound of wherein Ris —C(O)—.13. The compound of where claim 1 , in subformula Ic claim 1 , RRis —C(O)R—.14. The compound of wherein Ris —NR— claim 13 , or —NRN— claim 13 , wherein Ris a C1-C8 hydrocarbylene group.16. The compound of wherein Ris NRN claim 15 , a C1-C4 hydrocarbylene group claim 15 , or —NHCHCHNH—.17. A polymer comprising the compound of .18. A polymeric matrix comprising the compound of .19. A medical device comprising a hydrophilic coating comprising the polymeric matrix of .20. A medical device comprising a hydrophilic coating claim 18 , the hydrophilic coating comprising an aryl ketone derivative of a triazinylaminostilbenesulfonic acid. The present non-provisional application claims the benefit of commonly owned provisional Application having Ser. No. 61/736,436, filed on Dec. 12, 2012, entitled STILBENE-BASED REACTIVE COMPOUNDS, POLYMERIC MATRICES FORMED THEREFROM, AND ARTICLES VISUALIZABLE BY FLUORESCENCE, which application is incorporated herein by reference in its entirety.The invention relates to hydrophilic polymeric coatings for surfaces of medical articles and hydrophilic polymer coatings that can be visualized with light.Developments in medicine have enabled the use of many non-classical surgical techniques in the treatment of diseases and disorders. For example, ...

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Номер записи: 54
26-03-2015 дата публикации

DIHYDRATE OF BENZOTHIOPHENE COMPOUND OR OF A SALT THEREOF, AND PROCESS FOR PRODUCING THE SAME

Номер: US20150087655A1
Автор: ETO Ryohei, HOSHIKA Yusuke, IKEBUCHI Takuma, Ito Nobuaki, KAWANO Shuuji, MINOWA Takuya, MORIYAMA Kei, Nakamura Takayuki, SATO Tetsuya, SOTA Masahiro, TOYOFUKU Hidekazu, YAMAGUCHI Tatsuya, Yamashita Hiroshi
Принадлежит:

An object of the present invention is to provide a compound that can be used as a more superior therapeutic agent for central nervous system diseases. The present invention provides a dihydrate of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or of a salt thereof, and a process for producing the same. 1. A dihydrate of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or of a salt thereof.2. The dihydrate according to which has characteristic peaks at diffraction angles (2θ) of 8.1° claim 1 , 8.9° claim 1 , 15.1° claim 1 , 15.6° claim 1 , and 24.4° in an X-ray powder diffraction pattern measured by copper radiation of λ=1.5418 Å through a monochromator.3. The dihydrate according to which has characteristic peaks at 3509 cm claim 1 , 2934 cm claim 1 , 2812 cm claim 1 , 1651 cm claim 1 , 1626 cm claim 1 , 1447 cm claim 1 , 1223 cm claim 1 , and 839 cmin an infrared absorption spectrum as measured by a potassium bromide tablet method.4. The dihydrate according to which has characteristic peaks at 1497 cm claim 1 , 1376 cm claim 1 , 1323 cm claim 1 , 1311 cm claim 1 , 1287 cm claim 1 , 1223 cm claim 1 , and 781 cmin a Raman spectrum.5. The dihydrate according to which contains water in an amount of 6.5 to 8.8 wt. %.6. The dihydrate according to which has peaks in a H-NMR spectrum at:1.64 ppm (tt, J=7.4 Hz, J=7.4 Hz, 2H),1.80 ppm (tt, J=7.0 Hz, J=7.0 Hz, 2H),2.44 ppm (t, J=7.5 Hz, 2H),2.62 ppm (br, 4H),3.06 ppm (br, 4H),{'sub': '2', '3.32 ppm (s, 4H+HO),'}4.06 ppm (t, J=6.5 Hz, 2H),6.29 ppm (d, J=9.5 Hz, 1H),6.80 ppm (d, J=2.5 Hz, 1H),6.80 ppm (dd, J=2.5 Hz, J=9.0 Hz, 1H),6.88 ppm (d, J=7.5 Hz, 1H),7.27 ppm (dd, J=7.8 Hz, J=7.8 z, 1H),7.40 ppm (dd, J=0.5 Hz, J=5.5 Hz, 1H),7.55 ppm (d, J=9.0 Hz, 1H),7.61 ppm (d, J=8.0 Hz, 1H),7.69 ppm (d, J=5.5 Hz, 1H),7.80 ppm (d, J=9.5 Hz, 1H), and11.57 ppm (s, 1H).7. A process for producing a dihydrate of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or of a salt ...

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Номер записи: 55
26-03-2015 дата публикации

Thermoplastic polymer composition

Номер: US20150087758A1
Автор: Darin L. Dotson, Eduardo Torres, Francisco Alvarez, Haihu Qin, Sanjeev K. DEY
Принадлежит: Milliken and Co

The invention provides a compound conforming to the structure of Formula (CX) The invention also provides a thermoplastic polymer composition comprising a polyolefin polymer and a compound conforming to the structure of Formula (CX) as a nucleating agent.

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Номер записи: 56
25-03-2021 дата публикации

PREPARATION AND APPLICATION OF GRAIN WORM FOR TREATING DIABETES

Номер: US20210085727A1
Автор: HUA XIANGRONG, Huang Amy Y.
Принадлежит:

This invention discloses the preparation and the application of Grain Worm for treating diabetes or regulating blood insulin level. The Grain Worm can be in the form of dry powder, tincture, or extracts by itself or in a compound. 1. A method of regulating blood insulin levels in an individual comprising administering to the individual an effective amount of a composition comprising Grain Worm.2. The method of wherein said effective amount of said composition comprising Grain Worm treats diabetes.3. The method of wherein said composition comprising Grain Worm is ingested by the individual.4. The method of wherein said composition comprising Grain Worm comprises a dietary supplement.5. The method of wherein said composition comprising Grain Worm comprises dry powder Grain Worm.6. The method of wherein said composition comprising Grain Worm comprises a Grain Worm tincture.7. The method of wherein said composition comprising Grain Worm comprises a Grain Worm extract.8. The method of wherein said composition comprising Grain Worm comprises a lyophilized powder.9. The method of wherein said composition comprising grain worm is structured to be injected.10. The method of further comprising:conducting a treatment course of 1-6 cycles wherein each cycle has a duration of approximately three months and comprises administering said composition comprising Grain Worm at least once per day during each of said cycles.11. The method of wherein said composition comprising said Grain Worm comprises between approximately 2 g to 30 g of said Grain Worm.12. The method of wherein said composition comprising said Grain Worm is administered between two to three times per day.13. The method of comprising conducting a treatment course to treat pre-diabetes claim 2 , said pre-diabetes treatment course comprising 1-2 cycles claim 2 , wherein each cycle has a duration of approximately three months and comprises administering said composition comprising a total dosage of 2 g to 15 g of said ...

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Номер записи: 57
12-03-2020 дата публикации

Isolation Of Bona Fide Pancreatic Progenitor Cells

Номер: US20200080062A1
Автор: Ameri Jacqueline, Semb Henrik
Принадлежит:

The present invention relates to a method for isolating bona fide pancreatic progenitor cells and to cell populations enriched for bona fide pancreatic progenitor cells. 2. The method according to claim 1 , wherein the ligands is an antibody or fragment thereof.3. The method according to claim 1 , wherein the cells are removed or selected by flow cytometry.4. The method according to claim 2 , wherein the ligand is an antibody or fragment thereof directed against GP2.5. The method according to claim 4 , further comprising exposing the cell population to an antibody or fragment thereof directed against CD49d and selecting the cells that do not bind to the antibody or fragment thereof directed against CD49d from the cells that do bind the antibody or fragment thereof directed against CD49d prior to exposing the cell population to an antibody directed against GP2.6. The method according to claim 1 , wherein the bona fide pancreatic progenitor cells are derived from cells capable of differentiation selected from human iPS cells (hIPSCs) claim 1 , human ES cells (hESCs) or naive human stem cells (NhSCs).7. The method according to claim 6 , wherein the cells capable of differentiation are derived from cells isolated from an individual.8. The method according to claim 1 , wherein at least one cell of the cell population enriched for bona fide pancreatic progenitor cells has the capability to differentiate further into pancreatic hormone-producing cells.9. The method according to claim 1 , wherein CDKN1a or CDKN2a is inactivated in the cell population provided in i).10. The method according to claim 9 , wherein CDKN1a and/or CDKN2a is inactivated by knock-down claim 9 , deletion claim 9 , silencing or repression.11. The method according to claim 1 , wherein the starting cell population is a pancreatic progenitor population expressing PDX1.12. The method according to claim 11 , wherein inactivation of CDKN1a and/or CDKN2a results in an increase in the proportion of cells ...

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Номер записи: 58
31-03-2016 дата публикации

COMPOSITIONS AND METHODS FOR THE TREATMENT OF EPILEPSY AND NEUROLOGICAL DISORDERS

Номер: US20160090379A1
Автор: Kandula Mahesh
Принадлежит:

The invention relates to the compounds of formula I and formula Ia or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of formula I or formula Ia; and methods for treating or preventing epilepsy, seizures and convulsions may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of epilepsy, seizures and convulsions. 3. A Pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.4. A Pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.5. The pharmaceutical composition of claim 3 , which is formulated to treat the underlying etiology with an effective amount administering the patient in need by oral administration claim 3 , delayed release or sustained release claim 3 , transmucosal claim 3 , syrup claim 3 , topical claim 3 , parenteral administration claim 3 , injection claim 3 , subdermal claim 3 , oral solution claim 3 , rectal administration claim 3 , buccal administration or transdermal administration.6. The pharmaceutical composition of claim 4 , which is formulated to treat the underlying etiology with an effective amount administering the patient in need by oral administration claim 4 , delayed release or sustained release claim 4 , transmucosal claim 4 , syrup claim 4 , topical claim 4 , parenteral administration claim 4 , injection claim 4 , subdermal claim 4 , oral solution claim 4 , rectal administration claim 4 , buccal administration or transdermal administration.7. Compounds and compositions of are formulated for the treatment of epilepsy claim 5 , seizures claim 5 , convulsions and neurological diseases.8. Compounds and compositions of are formulated for the treatment of epilepsy claim 6 , seizures claim 6 , convulsions and neurological ...

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Номер записи: 59
21-03-2019 дата публикации

INDIRECT ASSESSMENT OF INSULIN RELEASE IN A CELL

Номер: US20190086390A1
Автор: COLLIER JASON, Rogers Richard C.
Принадлежит: Board of Supervisors of Louisiana State University and Agricultural and Mechanical College

Provided herein are compositions, systems, kits, and methods of indirectly assessing insulin release in a cell. 1. A method to indirectly assess insulin release in a cell in response to a test composition , the method comprising:culturing pancreatic beta cells;incubating the cells with a calcium sensitive indicator for an amount of time;contacting the cells with the test composition;stimulating the cells with glucose; andmeasuring a signal from the calcium sensitive indicator.23.-. (canceled)4. The method of claim 1 , wherein the test composition is a pharmaceutical composition.5. The method of claim 1 , wherein the test composition is a chemical compound.6. The method of claim 1 , wherein the test composition is a biologic compound.7. The method of claim 1 , wherein the pancreatic beta cells are obtained from a subject in need thereof.8. The method of claim 1 , wherein the subject in need thereof has diabetes.9. The method of claim 1 , wherein the calcium sensitive indicator is a fluorescent indicator.10. The method of claim 9 , wherein the calcium sensitive indicator is selected from the group consisting of: fura-2 claim 9 , indo-1 claim 9 , fluo-3 claim 9 , fluo-4 claim 9 , calcium green-1 claim 9 , and a calcium binding fluorescent protein.11. The method of any claim 1 , wherein the step of measuring a signal comprises the step of microscopically visualizing the pancreatic beta cells.12. The method of claim 11 , wherein the step of measuring a signal further comprises detecting a wavelength of light emitted by the calcium sensitive indicator.13. The method of claim 1 , wherein the step of measuring a signal comprises detecting a wavelength of light emitted by the calcium sensitive indicator.14. The method of claim 13 , wherein the wavelength of light is detected by a plate reader.15. The method of claim 1 , wherein during the step of incubating the cells with a calcium sensitive indicator for an amount of time claim 1 , the cells are also incubated with a ...

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Номер записи: 60
19-06-2014 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20140171310A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 2. A molecule according to wherein R1 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , haloethyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , methoxy claim 1 , ethoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , halomethoxy claim 1 , haloethoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , and halo(C)alkoxy.3. A molecule according to wherein R2 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , haloethyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , methoxy claim 1 , ethoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , halomethoxy claim 1 , haloethoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , and halo(C)alkoxy.4. A molecule according to wherein R3 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , ...

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Номер записи: 61
19-06-2014 дата публикации

REDUCED CENTRAL CORNEAL THICKENING BY USE OF HYDROPHILIC ESTER PRODRUGS OF BETA-CHLOROCYCLOPENTANES

Номер: US20140171661A1
Автор: Burk Robert M., Im Wha Bin
Принадлежит: ALLERGAN, INC.

Compositions and methods for treating glaucoma are provided. In particular hydrophilic ester prodrugs and their use to reduce central corneal thickening is provided. 2. The compound of wherein the X is CHCH.3. The compound of wherein Y is thiophene.4. The compound of wherein Z is a single bond.5. The compound of wherein Ris —OH and Ris H or CHand n is 1 and Yis a single bond claim 4 , Zis —OH and n1 is 0.6. The compound of wherein U is H—Cl.7. The compound of wherein Ar is aryl and is disubstituted by Cl.8. The compound of wherein Rand Rare H claim 4 , n is 0 claim 4 , Yis C═O claim 4 , Zis N Ris CHCHOH claim 4 , and n1 is 2.9. The compound of wherein Ar is aryl and is disubstituted by Cl and U is H—Cl.11. The compound of wherein Ar is aryl and is disubstituted by Cl and U is H—Cl.12. The compound of wherein Rand Rare CH—OH claim 4 , n is 1 claim 4 , Yis C═O claim 4 , Zis NH claim 4 , n1 is 0 and Ar is aryl and is disubstituted by Cl and U is Cl.13. The compound of wherein Rand Rare CH—OH claim 4 , n is 2 claim 4 , Yis C═O claim 4 , Zis NH claim 4 , n1 is 0 and Ar is aryl and is disubstituted by Cl and U is Cl.14. The compound of wherein Rand Rare CH—OH claim 4 , n is 3 claim 4 , Yis C═O claim 4 , Zis NH claim 4 , n1 is 0 and Ar is aryl and is disubstituted by Cl and U is Cl.17. A compound according to wherein X is CHCH claim 16 , Y is thiophene claim 16 , and Z is a single bond.18. The compound of wherein Ris —OH and Ris H or CHand n is 0 and Yis a single bond claim 16 , Zis —OH and n1 is 0.19. The compound of wherein Rand Rare CH—OH claim 16 , n is 1-3 claim 16 , Yis C═O claim 16 , Zis NH claim 16 , n1 is 0 and Ar is aryl and is disubstituted by Cl and U is Cl. This application is a continuation-in-part of U.S. application Ser. No. 13/974,975, filed Aug. 23, 2013, which claims the benefit of U.S. provisional application Ser. No. 61/693,437, filed on Aug. 27, 2012, all of which applications are incorporated herein by reference in their entireties.The present ...

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Номер записи: 62
09-04-2015 дата публикации

HETEROARYLCARBOXYLIC ACID ESTER DERIVATIVE

Номер: US20150099733A1
Автор: Ichimaru Taisuke, Koshiba Takahiro, Matsumoto Kayo, Nakagawa Tadakiyo, Ohsumi Koji, Suzuki Tamotsu, Tokumasu Munetaka, Yamada Tatsuhiro
Принадлежит: AJINOMOTO CO., INC.

Compounds represented by the following formula (I); 2. A method according to claim 1 , wherein X is —NRRor a group represented by formula (II) claim 1 , wherein R claim 1 , Rand Rare each independently a hydrogen atom or a Calkyl group.3. A method according to claim 1 , wherein X is —NRR claim 1 , wherein Rand Rtogether with the nitrogen atom to which they are bonded form a Cheterocycle substituted by a hydrogen atom claim 1 , a halogen atom claim 1 , a carboxyl group claim 1 , a carboxyl Calkyl group or a hydroxyl group.4. A method according to claim 1 , wherein X is a group represented by formula (II) claim 1 , wherein p=1 or 2 claim 1 , and q=0.5. A method according to claim 1 , wherein X is a group represented by formula (II) claim 1 , wherein p=0 and q=1.6. A method according to claim 1 , wherein X is a group represented by formula (II) claim 1 , wherein p=1 claim 1 , q=1 claim 1 , and Ra and Rb are the same or different and each is independently a hydrogen atom or a Calkyl group claim 1 , or Ra and Rb together with the atom(s) to which they are bonded form a Ccycloalkane ring claim 1 , wherein said Calkyl group and said Ccycloalkane ring may substituted with a group selected from the group consisting of a hydrogen atom claim 1 , a carboxyl group claim 1 , a carbamoyl group claim 1 , a hydroxyl group claim 1 , a phenyl group and a Ccycloalkyl group.7. A method according to claim 1 , wherein Rand Rare the same or different and each is independently a methyl group claim 1 , an ethyl group or a propyl group claim 1 , or Rand Rtogether with the carbon atom to which they are bonded form a cyclobutane ring or a cyclopentane ring.8. A method according to claim 1 , wherein X is a group represented by formula (II) claim 1 , wherein q=1 claim 1 , and Ring A is a benzene ring claim 1 , a pyridine ring claim 1 , or a Cheterocycle containing 1-4 oxygen atoms.9. A method according to claim 1 , wherein X is a group represented by formula (II) claim 1 , wherein q=1 claim 1 , ...

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Номер записи: 63
26-03-2020 дата публикации

BIODEGRADABLE DIETHANOLAMINE DERIVATIVE CHELATING AGENT AND PREPARATION PROCESS THEREOF

Номер: US20200095192A1
Автор: KAEOTHIP SOPHON, PORNSURIYASAK PAPAPIDA
Принадлежит: PTT Global Chemical Public Company Limited

The present invention relates to a new diethanolamine derivative chelating agent having a high water solubility, a good chelating property, and biological degradation. The said new chelating agent can be prepared from reaction of diethanolamine and cyclic anhydride compound using lewis acid as the catalyst. The said process is uncomplicated, and does not use a severe condition, and also reduces the use of harmful chemicals. 4. The diethanolamine derivative chelating agent according to claim 3 , wherein n is 1.6. A process for preparing the diethanolamine derivative chelating agent according to claim 1 , wherein said process comprises the following steps:a) mixing diethanolamine and cyclic anhydride compound in equivalent mole ratio from 1:1 to 1:5 in organic solvent; andb) adding lewis acid catalyst into mixture obtained from a).7. The process for preparing the diethanolamine derivative chelating agent according to claim 6 , wherein the organic solvent in step a) can be selected from 1 claim 6 ,4-dioxane claim 6 , 1 claim 6 ,2-dichloroethane claim 6 , dichloromethane claim 6 , or mixture thereof.8. The process for preparing the diethanolamine derivative chelating agent according to claim 7 , wherein the organic solvent in step a) is dichloromethane.9. The process for preparing the diethanolamine derivative chelating agent according to claim 6 , wherein the cyclic anhydride compound in step a) is selected from maleic anhydride claim 6 , succinic anhydride claim 6 , glutaric anhydride claim 6 , or phthalic anhydride.10. The process for preparing the diethanolamine derivative chelating agent according to claim 9 , wherein the cyclic anhydride compound is selected from maleic anhydride claim 9 , succinic anhydride claim 9 , or phthalic anhydride.11. The process for preparing the diethanolamine derivative chelating agent according to claim 6 , wherein the equivalent mole ratio between diethanolamine and cyclic anhydride compound is from 1:2 to 1:5.12. The process for ...

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Номер записи: 64
26-03-2020 дата публикации

NOVEL CRYSTALLINE FORMS OF {[5-(3-CHLOROPHENYL)-3-HYDROXYPYRIDINE-2-CARBONYL] AMINO} ACETIC ACID AND PROCESSES FOR PREPARATION THEREOF

Номер: US20200095203A1
Автор: Chen Minhua, WANG Jinqiu, Zhang Xiaoyu, ZHANG Yanfeng, ZOU Po
Принадлежит:

The present disclosure relates to novel crystalline forms of {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl] amino} acetic acid and processes for preparation and uses thereof. Crystalline form CS1, form CS2 and form CS8 of the present disclosure can be used for preparing drugs treating anemia, which providing new choices for preparing drugs of {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl] amino} acetic acid, and having very important value for drug development. 1. A crystalline form CS1 of {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl] amino} acetic acid , wherein the X-ray powder diffraction pattern shows characteristic peaks at 2theta values of 13.9°±0.2° , 15.3°±0.2° , 15.6°±0.2° and 26.8°±0.2° using CuKα radiation.2. The crystalline form CS1 according to claim 1 , wherein the X-ray powder diffraction pattern shows one or more characteristic peaks at 2theta values of 17.0°±0.2° claim 1 , 19.1°±0.2° claim 1 , 23.5°±0.2° and 25.6°±0.2° using CuKα radiation.3. A process for preparing crystalline form CS1 according to claim 1 , wherein crystalline form CS1 can be obtained from either one of the following methods:1) Dissolving {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl] amino} acetic acid into ethers and then evaporating at room temperature to obtain solids; or2) Dissolving {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl] amino} acetic acid into tetrahydrofuran, and then adding water slowly into the solution or adding the solution into water; Stirring at room temperature for a period of time; Filtering and drying to obtain solids.4. The process for preparing crystalline form CS1 according to claim 3 , wherein said ether is methyl tert-butyl ether; said stirring time is 1-48 h.5. A crystalline form CS2 of {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl] amino} acetic acid claim 3 , wherein the X-ray powder diffraction pattern shows characteristic peaks at 2theta values of 14.1°±0.2° claim 3 , 15.0°±0.2° and 18.3°±0.2° using CuKα radiation.6. The ...

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Номер записи: 65
13-04-2017 дата публикации

Pyridone compounds, pharmaceutical compositions thereof, and their therapeutic use for treating proliferative diseases

Номер: US20170101379A1
Автор: Frank Mercurio, Kyle W.H. Chan, Leah Fung, Robert Sullivan, Sara Howard
Принадлежит: BioTheryX Inc

Provided herein are pyridone compounds, for example, a compound of Formula I, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.

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Номер записи: 66
23-04-2015 дата публикации

PROCESS FOR PREPARING CRYSTALLINE SORAFENIB TOSYLATE

Номер: US20150111929A1
Автор: Purohit Prashant, Rampalli Sriram, Upalla Lavkumar, Vijaya Murali Mohanrao Seshagiri
Принадлежит:

The present invention provides an industrially suitable process for the preparation of substantially pure 4-{4-[({[4-chloro-3-(trifluoromethyl)-phenyl]amino}carbonyl)amino]phenoxy}-N-methylpyridine-2-carboxamide or Sorafenib and its tosylate salt, with a suitable impurity profile and without requirement of any additional purification steps. The present invention also provides Sorafenib base (II) as stable crystalline Form-SSB. 2. A process for the preparation of crystalline Sorafenib base-Form-SSB according to claim 1 , wherein the high boiling organic solvent is selected from Cketones or a mixture thereof.3. A process for the preparation of crystalline Sorafenib base-Form-SSB according to claim 1 , wherein Cketone is selected from methyl ethyl ketone (MEK) or methyl isobutyl ketone (MIBK).4. A process for the preparation of crystalline Sorafenib base-Form-SSB according to claim 1 , wherein reaction of 4-(4-aminophenoxy)-N-methylpicolinamide (III) with 4-chloro-3-(trifluoromethyl)phenylisocyanate (IV) claim 1 , is carried out at temperature ranging between 75-90° C.5. A process for the preparation of crystalline Sorafenib base-Form-SSB according to claim 1 , wherein crystalline Sorafenib base-Form-SSB obtained is characterized by X-ray powder diffraction pattern substantially according to and DSC isothermal pattern substantially according to .6. Crystalline Sorafenib base-Form-SSB claim 1 , characterized by X-ray powder diffraction pattern comprising at least 5 characteristic 2θ° peaks selected from the XRPD peak set of 9.9 claim 1 , 11.4 claim 1 , 12.6 claim 1 , 14.6 claim 1 , 15.2 claim 1 , 15.6 claim 1 , 18.1 claim 1 , 18.6 claim 1 , 21.8 claim 1 , 22.5 claim 1 , 22.9 claim 1 , 23.6 claim 1 , 24.8 claim 1 , 25.2±0.20 2θ° and DSC isotherm comprising a single endothermic peak ranging between 202 to 212° C.7. Crystalline Sorafenib base-Form-SSB according to claim 6 , characterized by X-ray powder diffraction pattern substantially according to and DSC isothermal ...

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Номер записи: 67
19-04-2018 дата публикации

PYRIDYL BENZOTHIOPHENES AS KINASE INHIBITORS

Номер: US20180105515A1
Автор: Boral Sougato, Malone Thomas C., WANG Shimiao
Принадлежит:

This invention is directed to compounds, which are useful as protein kinase (PK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders, metabolic diseases inflammatory disorders and neurodegenerative disorders. 2. A pharmaceutical composition comprising as active ingredient a therapeutically effective amount of a compound according to and a pharmaceutically acceptable adjuvant claim 1 , diluent or carrier. This application is a continuation of U.S. patent application Ser. No. 15/162,172, filed May 23, 2016, which is a continuation of U.S. patent application Ser. No. 14/511,112, filed Oct. 9, 2014, now U.S. Pat. No. 9,371,314, issued Jun. 21, 2016, the disclosures of which are hereby incorporated by reference in their entireties and serve as the basis of a priority and/or benefit claim for the present application.The invention relates to inhibitors of VEGFR2 kinase or VEGFR, PDGFR kinases or PDGFR and Protein Kinase R (EIF2AK2), and methods of using such compounds. The present invention is also directed to methods of regulating, modulating or inhibiting protein kinases, whether of the receptor or non-receptor class, for the prevention and/or treatment of disorders related to unregulated protein kinase signal transduction, including cell growth, metabolic, and blood vessel proliferative disorders.Protein kinases (PKs) comprise a large and diverse class of proteins having enzymatic activity which catalyzes the transfer of the terminal phosphate of ATP to the hydroxyl group of a serine, threonine or tyrosine group in a protein. Protein kinases (PKs) are involved in numerous diseases which result from dysregulation of their normal function.There are numerous examples where protein kinases, have been found to be involved in cellular signaling pathways leading to pathological conditions. In the VEGFR2 kinase protein kinase, which is a receptor tyrosine kinase, ...

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Номер записи: 68
03-07-2014 дата публикации

METHOD FOR PRODUCING BENZO[B]THIOPHENE COMPOUND

Номер: US20140187782A1
Автор: Fujieda Shigeo, Ogasawara Shin, SHINHAMA Koichi, SOTA Masahiro, UTSUMI Naoto
Принадлежит: OTSUKA PHARMACEUTICAL CO., LTD.

The present invention provides a method for producing a compound of Formula (4): wherein Ris a hydrogen atom etc. by reacting a compound of Formula (2): wherein Xis a leaving group, with a compound of Formula (3): wherein Ris as defined above, in the presence of (a) a palladium compound and a tertiary phosphine or (b) a palladium carbene complex, in an inert solvent or without a solvent. The present invention can produce the compound of Formula (4), with high purity and high yield, and by a simple operation. 2. The method according to claim 1 , wherein the tertiary phosphine is at least one member selected from the group consisting of tri-tert-butylphosphine claim 1 , 2-(di-tert-butylphosphino)-1 claim 1 ,1′-biphenyl claim 1 , 2-(di-tert-butylphosphino)-2′-methyl-1 claim 1 ,1′-biphenyl claim 1 , 2-(di-tert-butylphosphino)1 claim 1 ,1′-binaphthyl claim 1 , 2-dicyclohexylphosphino-2′ claim 1 ,6′-dimethoxy-1 claim 1 ,1′-biphenyl claim 1 , 2-dicyclohexylphosphino-2′ claim 1 ,6′-di-iso-propoxy-1 claim 1 ,1′-biphenyl claim 1 , N-phenyl-2-(di-tert-butylphosphino)pyrrole claim 1 , and 1-phenyl-2-(di-tert-butylphosphino)-1H-indene.3. The method according to claim 1 , wherein the palladium carbene complex is at least one member selected from the group consisting of (1 claim 1 ,4-naphthoquinone)-[1 claim 1 ,3-bis(2 claim 1 ,6-diisopropylphenyl)imidazol-2-ylidene]palladium (0) claim 1 , allylchloro-[1 claim 1 ,3-bis(2 claim 1 ,6-diisopropylphenyl)imidazol-2-ylidene]palladium (II) claim 1 , allylchloro-[1 claim 1 ,3-bis(2 claim 1 ,6-diisopropylphenyl)-4 claim 1 ,5-dihydroimidazol-2-ylidene]palladium (II) claim 1 , and (3-phenylallylchloro)-[1 claim 1 ,3-bis(2 claim 1 ,6-diisopropylphenyl)-4 claim 1 ,5-dihydroimidazol-2-ylidene]palladium (II).6. The method according to claim 5 , further comprising:step E: reacting the hydrochloride of the compound represented by Formula (1) obtained in the step D in the presence of a basic compound to obtain the compound represented by Formula (1 ...

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Номер записи: 69
20-04-2017 дата публикации

PYRIDYL BENZOTHIOPHENES AS KINASE INHIBITORS

Номер: US20170107210A1
Автор: Boral Sougato, Malone Thomas C., WANG Shimiao
Принадлежит:

This invention is directed to compounds, which are useful as protein kinase (PK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders, metabolic diseases inflammatory disorders and neurodegenerative disorders. 29.-. (canceled)11. (canceled)1317.-. (canceled)18. A compound according to claim 1 , selected from:{'sup': '4', '6-amino-N-[dimethyl(oxido)-λ-sulfanylidene]-5-{5-[(3-methyl-2-furoyl)amino]-1-benzothien-2-yl}nicotinamide;'}methyl 6-amino-5-{5-[(3-methyl-2-furoyl)amino]-1-benzothien-2-yl}nicotinate;methyl 6-amino-5-{5-[(1-benzofuran-2-ylcarbonyl)amino]-1-benzothien-2-yl}nicotinate;2-(2-aminopyridin-3-yl)-N-(5-tert-butylisoxazol-3-yl)-1-benzothiophene-5-carboxamide;2-(2-aminopyridin-3-yl)-N-(3-methylbenzyl)-1-benzothiophene-5-carboxamide;19. A pharmaceutical composition comprising as active ingredient a therapeutically effective amount of a compound according to and a pharmaceutically acceptable adjuvant claim 1 , diluent or carrier.20. (canceled)22. A compound according to claim 21 , selected from:{'sup': '4', '6-amino-N-[dimethyl(oxido)-λ-sulfanylidene]-5-[4-({[(2-fluoro-5-methylphenyl) amino]carbonyl}amino)phenyl]nicotinamide;'}{'sup': '4', '6-amino-N-[dimethyl(oxido)-λ-sulfanylidene]-5-[4-({[(2-fluoro-5-methylphenyl)amino]carbonyl}amino)phenyl]nicotinamide;'}[6-amino-5-(4-{[(2-fluoro-5-methylphenyl)carbamoyl]amino}phenyl)pyridin-3-yl]boronic acid;1-{4-[2-amino-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-3-yl]phenyl}-3-(2-fluoro-5-methylphenyl)urea;1-{4-[2-amino-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-3-yl]phenyl}-3-phenylurea;dimethyl {6-amino-5-[4-({[3-(trifluoromethyl)phenyl]carbamoyl}amino) phenyl]pyridin-3-yl}phosphonate;diethyl [6-amino-5-(4-{[(2-fluoro-5-methylphenyl)carbamoyl]amino}phenyl) pyridin-3-yl]phosphonate;dimethyl {6-amino-5-[4-({[2-fluoro-5-(trifluoromethyl)phenyl]carbamoyl}amino) phenyl]pyridin-3-yl}phosphonate; ...

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Номер записи: 70
29-04-2021 дата публикации

PRO-DRUG PEPTIDE WITH IMPROVED PHARMACEUTICAL PROPERTIES

Номер: US20210122800A1
Автор: Fremaux Juliette, Goudreau Sebastien, Guichard Gilles, Venin Claire, Zimmer Robert H.
Принадлежит:

The present disclosure relates to a pro-drug peptide, or a salt thereof, having improvement for at least one biological property relative to a parent peptide or peptidomimetic, wherein the biological property is selected from the group consisting of therapeutic index, stability, solubility, toxicity, adsorption, and pre-systemic metabolism. The pro-drug peptide comprising the following structure: Z-pep, wherein: pep is the parent peptide or peptidomimetic; Z is a sequence of n amino acids, Z is cleaved in vivo releasing pep; n≥2 amino acids. The present disclosure also relates to methods of making and using the pro-drug peptide of the present disclosure. For example, the present disclosure describes a pro-drug peptide that may be used to prevent, treat, or ameliorate at least one symptom of hypoglycemia or a hypoglycemia-related disease or disorder. 1. A pro-drug peptide or salt thereof having improvement for at least one biological property relative to a parent peptide or peptidomimetic , wherein the biological property is selected from the group consisting of therapeutic index , stability , solubility , toxicity , adsorption , and pre-systemic metabolism , the pro-drug peptide comprising the following structure:{'br': None, 'sub': 'n', 'Z-pep,'} pep is the parent peptide or peptidomimetic;', 'Z is a sequence of n amino acids, which is cleaved in vivo releasing pep; and', 'n is an integer ≥2., 'wherein2. The pro-drug peptide of claim 2 , wherein the Z has the following structure: (Glu-Pro)or (Lys-Pro) claim 2 , wherein X is an integer ≥1.3. The pro-drug peptide of claim 1 , wherein the Z is selected from the group consisting of EP claim 1 , KP claim 1 , EPEP claim 1 , KPKP claim 1 , EPEPEP claim 1 , and KPKPKP.4. The pro-drug peptide of claim 2 , wherein at least the first Lys of Z is functionalized with a soluble compound or moiety.5. The pro-drug peptide of claim 2 , wherein at least two Lys of Z are functionalized with the soluble compound or moiety.6. The pro- ...

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Номер записи: 71
28-04-2016 дата публикации

Process for the manufacture of n-acylbiphenyl alanine

Номер: US20160115118A1
Автор: Desong Shi, Fengfeng Tao, Guoliang Zhu, Junhui Wei
Принадлежит: Individual

The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors.

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Номер записи: 72
10-07-2014 дата публикации

SUBSTITUTED 3-HETEROAROYLAMINO-PROPIONIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS

Номер: US20140194445A1
Автор: BUNING Christian, RUF Sven, SADOWSKI Thorsten, SCHREUDER Herman, WIRTH Klaus
Принадлежит: SANOFI

The present invention relates to compounds of the formula I, 2. A compound of the formula I in any of its stereoisomeric forms or a mixture of stereoisomeric forms in any ratio claim 1 , or a physiologically acceptable salt thereof claim 1 , or a physiologically acceptable solvate of any of them claim 1 , as claimed in claim 1 , wherein{'sup': 71', '72', '73, 'G is selected from the group consisting of R—O—C(O)— and R—N(R)—C(O)—;'}{'sup': 30', '32, 'sub': u', '2u, 'Ris R—CH—, wherein u is 0 or 1;'}{'sup': 32', '33', '33', '33', '1, 'sub': 1', '6', '3', '7', '1', '6', '1', '4', '2', '2', '1', '6', 'n', '1', '4', '2', '2', '1', '6', '1', '4, 'Ris selected from the group consisting of phenyl and an aromatic 6-membered monocyclic heterocycle which comprises one or two nitrogen atoms as ring heteroatoms, wherein the phenyl and the heterocycle all are optionally substituted by one or more identical or different substituents selected from the group consisting of halogen, (C-C)-alkyl, (C-C)-cycloalkyl, R, HO—, (C-C)-alkyl-O—, R—O—, R—(C-C)-alkyl-O—, —O—CH—O—, —O—CF—O—, (C-C)-alkyl-S(O)—, di((C-C)-alkyl)N—S(O)—, HN—, di((C-C)-alkyl)N—, Het, (C-C)-alkyl-C(O)—NH—, Ar—C(O)—NH— and NC—;'}{'sup': '33', 'sub': 1', '6', '3', '7', '1', '6', '1', '6', 'n', '2', '2', '1', '4', '2, 'Ris selected from the group consisting of phenyl and an aromatic 6-membered monocyclic heterocycle which comprises one or two nitrogen atoms as ring heteroatoms, wherein the phenyl and the heterocycle all are optionally substituted by one or more identical or different substituents selected from the group consisting of halogen, (C-C)-alkyl, (C-C)-cycloalkyl, HO—, (C-C)-alkyl-O—, (C-C)-alkyl-S(O)—, HN—S(O)—, di((C-C)-alkyON—S(O)— and NC—; and'}{'sup': '40', 'Ris hydrogen.'}3. A compound of the formula I in any of its stereoisomeric forms or a mixture of stereoisomeric forms in any ratio claim 1 , or a physiologically acceptable salt thereof claim 1 , or a physiologically acceptable solvate of any of them ...

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Номер записи: 73
26-04-2018 дата публикации

PYRIDYL BENZOTHIOPHENES AS KINASE INHIBITORS

Номер: US20180111921A1
Автор: Boral Sougato, Malone Thomas C., WANG Shimiao
Принадлежит:

This invention is directed to compounds, which are useful as protein kinase (PK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders, metabolic diseases inflammatory disorders and neurodegenerative disorders. 2. A compound according to claim 1 , selected from:{'sup': '4', '6-amino-N-[-dimethyl(oxido)-λ-sulfanylidene]-5-[4-({[(2-fluoro-5-methylphenyl) amino]carbonyl}amino)phenyl]nicotinamide;'}{'sup': '4', '6-amino-N[-dimethyl(oxido)-λ-sulfanylidene]-5-[4-({[(2-fluoro-5-methylphenyl)amino]carbonyl}amino)phenyl]nicotinamide;'}[6-amino-5-(4-{[(2-fluoro-5-methylphenyl)carbamoyl]amino}phenyl)pyridin-3-yl]boronic acid;1-{4-[2-amino-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-3-yl]phenyl}-3-(2-fluoro-5-methylphenyl)urea;1-{4-[2-amino-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-3-yl]phenyl}-3-phenylurea;dimethyl {6-amino-5-[4-({[3-(trifluoromethyl)phenyl]carbamoyl}amino) phenyl]pyridin-3-yl}phosphonate;diethyl [6-amino-5-(4-{[(2-fluoro-5-methylphenyl)carbamoyl]amino}phenyl) pyridin-3-yl]phosphonate;dimethyl {6-amino-5-[4-({[2-fluoro-5-(trifluoromethyl)phenyl]carbamoyl}amino) phenyl]pyridin-3-yl}phosphonate;dimethyl [6-amino-5-(4-{[(2-fluoro-5-methylphenyl)carbamoyl]amino}phenyl) pyridin-3-yl]phosphonate;dimethyl (6-amino-5-{4-[(phenylcarbamoyl)amino]phenyl}pyridin-3-yl)phosphonate;{'sup': '6', '6-amino-N-[bis(3-hydroxypropyl)(oxido)-λ-sulfanylidene]-5-(4-{[(3-methylphenyl)carbamoyl]amino}phenyl)pyridine-3-carboxamide;'}dimethyl 5,5′-(N-{[6-amino-5-(4-{[(3-methylphenyl)carbamoyl]amino} phenyl)pyridin-3-yl]carbonyl}sulfonimidoyl)dipentanoate;dimethyl 5,5′-(N-{[6-amino-5-(4-{[(2-fluoro-5-methylphenyl)carbamoyl]amino}phenyl)pyridin-3-yl]carbonyl}sulfonimidoyl)dipentanoate; anddimethyl 5, 5′-]N-({6-amino-5-[4-({[3-(trifluoromethyl)phenyl]carbamoyl}amino)phenyl]pyridin-3-yl}carbonyl)sulfonimidoyl]dipentanoate;methyl 6-amino-5-[4-({[2-fluoro-5-( ...

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Номер записи: 74
30-04-2015 дата публикации

PROLYL HYDROXYLASE INHIBITORS AND METHODS OF USE

Номер: US20150119425A1
Автор: Boyer Angelique Sun, Evdokimov Artem G., Greis Kenneth D., Kawamoto Richard Masaru, Warshakoon Namal C., Wu Shengde
Принадлежит:

The present disclosure relates to HIF-1α prolyl hydroxylase inhibitors, compositions which comprise the HIF-1α prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. 132-. (canceled)36. The method of claim 34 , wherein the compound is selected from:{[5-(3-Chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid methyl ester;{[5-(3-Chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid;5-(3-Chlorophenyl)-N-(2-amino-2-oxoethyl)-3-hydroxylpyridin-2-yl amide;5-(3-Chlorophenyl)-N-(2-methylamino-2-oxoethyl)-3-hydroxylpyridin-2-yl amide; and5-(3-Chlorophenyl)-N-(2-dimethylamino-2-oxoethyl)-3-hydroxylpyridin-2-yl amide.or a pharmaceutically acceptable salt thereof. This application is a Continuation Application of U.S. application Ser. No. 11/821,936, filed Jun. 26, 2007, which claims the benefit of Provisional Application Ser. No. 60/816,522 filed on Jun. 26, 2006, and the entire disclosures of Provisional Application Ser. No. 60/816,522 and U.S. application Ser. No. 11/821,936 are incorporated herein by reference in its entirety.The present disclosure relates, in some aspects, to HIF-1α prolyl hydroxylase inhibitor compounds and pharmaceutically acceptable salts thereof, compositions comprising the HIF-1α prolyl hydroxylase inhibitor compounds, and to methods for treating or controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.HIF-1α under normal healthy conditions wherein the cells have a sufficient supply of oxygen is readily converted to a degraded form by one of several prolyl hydroxylase enzymes, inter alia, EGLIN. When cells undergo hypoxia, this enzymatic transformation is slow or entirely stopped and HIF-1α begins to build up in the cell. When this build up of HIF-1α occurs, this protein combines with another factor, HIF-1β which together form ...

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Номер записи: 75
27-04-2017 дата публикации

COMPOSITIONS AND METHODS FOR TREATING ESTROGEN-RELATED MEDICAL DISORDERS

Номер: US20170114052A1
Автор: Siklos Marton, Thatcher Gregory R., Xiong Rui
Принадлежит:

Disclosed is a compound of formula (I). or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions including the compound of formula (I) and methods of using the compound of formula (I). 111-. (canceled)13. The compound of claim 12 , selected from the group consisting of:(2-(4-fluorophenyl)-6-hydroxybenzo[b]thiophen-3-yl)(4-(trifluoromethyl)phenyl)methanone;(3-(4-fluorophenyl)-6-hydroxybenzo[b]thiophen-2-yl)(4-(trifluoromethyl)phenyl)methanone;cyclopropyl(2-(4-fluorophenyl)-6-hydroxybenzo[b]thiophen-3-yl)methanone;cyclopropyl(3-(4-fluorophenyl)-6-hydroxybenzo[b]thiophen-2-yl)methanone;(2-(4-fluorophenyl)-6-hydroxybenzo[b]thiophen-3-yl)(pyridin-4-yl)methanone;(3-(4-fluorophenyl)-6-hydroxybenzo[b]thiophen-2-yl)(pyridin-4-yl)methanone;1-(2-(4-fluorophenyl)-6-hydroxybenzo[b]thiophen-3-yl)-2-methylpropan-1-one;1-(3-(4-fluorophenyl)-6-hydroxybenzo[b]thiophen-2-yl)-2-methylpropan-1-one;(4-ethynylphenyl)(2-(4-fluorophenyl)-6-hydroxybenzo[b]thiophen-3-yl)methanone;(4-ethynylphenyl)(3-(4-fluorophenyl)-6-hydroxybenzo[b]thiophen-2-yl)methanone;(2-(4-fluorophenyl)-6-hydroxybenzo[b]thiophen-3-yl)(p-tolyl)methanone;(3-(4-fluorophenyl)-6-hydroxybenzo[b]thiophen-2-yl)(p-tolyl)methanone;(4-(1-(4-fluorophenyl)-1H-1,2,3-triazol-4-yl)phenyl)(2-(4-fluorophenyl)-6-hydroxybenzo[b]thiophen-3-yl)methanone;(4-(1-(4-fluorophenyl)-1H-1,2,3-triazol-4-yl)phenyl)(3-(4-fluorophenyl)-6-hydroxybenzo[b]thiophen-2-yl)methanone;(3r,5r,7r)-adamantan-1-yl(2-(4-fluorophenyl)-6-hydroxybenzo[b]thiophen-3-yl)methanone; and(3r,5r,7r)-adamantan-1-yl(3-(4-fluorophenyl)-6-hydroxybenzo[b]thiophen-2-yl)methanone;or a pharmaceutically acceptable salt thereof.14. A method for treatment of an estrogen-related medical disorder claim 12 , the method comprising administering to a subject in need of such treatment a composition comprising a therapeutically effective amount of at least one compound of formula (II) as claimed in claim 12 , or a pharmaceutically acceptable salt thereof.15. ...

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Номер записи: 76
13-05-2021 дата публикации

Recrystallized HI-6 Dimethylsulfate

Номер: US20210138359A1
Автор: BLUMBERG Shawn T., MIGUEL Paul W.
Принадлежит:

The present invention is directed at the synthesis and characterization of recrystallized HI-6 dimethylsulfate (DMS). The method can comprise dissolving HI-6 DMS in an alkyl-based glycol and adding an antisolvent to recrystallize HI-6 DMS or dissolving HI-6 DMS in methanol and adding dimethoxy ethane or dimethyl formamide as the antisolvent to recrystallize HI-6 DMS. The recrystallized HI-6 DMS indicates a resistance to moisture absorption and/or a DSC melting point onset (MP Onset) at least at or above 160.0° C. 1. A method for recrystallizing HI-6 DMS comprising:dissolving HI-6 DMS in an alkyl-based glycol and adding an antisolvent to recrystallize HI-6 DMS.2. The method of wherein said alkyl-based glycol comprises ethylene glycol.3. The method of wherein said alkyl-based glycol comprises 1 claim 1 ,2-propane diol.4. The method of wherein said antisolvent is selected from tert-butanol.5. The method of wherein said antisolvent is selected from acetonitrile.6. The method of wherein said antisolvent is selected from ethanol.7. The method of wherein said antisolvent is selected from dimethoxy ethane.8. The method of wherein said alkyl-based glycol comprises 1 claim 1 ,2-propane diol and said recrystallized HI-6 DMS indicates a DSC melting point onset (MP Onset) at least at or above 160.0° C.9. The method of wherein said alkyl-based glycol comprises 1 claim 1 ,2-propane diol and said recrystallized HI-6 DMS indicates a DSC melting point at least at or above 165.0° C.10. The method of wherein said alkyl-based glycol comprises ethylene glycol and said antisolvent comprises tert-butanol.11. The method of wherein said recrystallized HI-6 DMS does not absorb water over a seven-day period under ambient temperature and humidity conditions.12. The method of wherein said alkyl-based glycol comprises 1 claim 1 ,2-propane diol and said antisolvent comprises tert-butanol.13. The method of wherein said recrystallized HI-6 DMS does not absorb water over a seven-day period under ...

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Номер записи: 77
13-05-2021 дата публикации

PRODUCTION METHOD OF ORGANIC COMPOUND

Номер: US20210139390A1
Автор: FUKUBAYASHI Yumeto, Nakai Makoto, YANAKA Ayumi
Принадлежит: UNITIKA LTD.

The present invention provides a production method of an organic compound, in which a reaction is performed between functional groups without using any solvents. The present invention relates to a production method of an organic compound, in which a reaction is performed between functional groups by using a mechanochemical effect. 138-. (canceled)39. A production method of an organic compound , wherein a reaction is performed between functional groups by using , a mechanochemicai effect , and wherein the organic compound is a high-molecular compound containing a repeating unit and the high-molecular compound is a polyamic acid-based compound , a polyimide-based compound , or a polyamide-imide-based compound.40. The production method of an organic compound of claim 39 , wherein the reaction is performed in a presence of a terminal blocking agent.41. The production method of an organic compound of claim 39 , wherein the polyamic acid-based compound claim 39 , the polyimide-based compound claim 39 , or a mixture thereof is produced as the organic compound by performing a reaction of a tetracarboxylic dianhydride component with a diamine component or a diisocyanate component claim 39 , as the reaction.42. The production method of an organic compound of claim 41 , wherein the components are used in an amount such that one component has a molar amount of 0.8 to 11 times that of the other component.43. The production method of an organic compound of claim 39 , Wherein the polyaniide-imide-based compound is produced as the organic compound by performing a reaction of a tricarboxylic acid anhydride component or its acid halide component with a diamine component or a diisocyanate component claim 39 , as the reaction.44. The production method of an organic compound of claim 43 , wherein the components are used in an amount such that one component has a molar amount of 0.8 to L2 times that of the other component.45. A production method of an organic compound claim 43 , wherein ...

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Номер записи: 78
07-05-2015 дата публикации

COMPOSITIONS AND METHODS FOR THE TREATMENT OF ASTHMA AND ALLERGY

Номер: US20150126593A1
Автор: Kandula Mahesh
Принадлежит:

The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of asthma and allergy may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of respiratory diseases, respiratory disorders, COPD, bronchitis, brain injury, inflammation, inflammatory skin diseases, asthma, allergic reactions, infections due to acute allergy, bronchospasm, respiratory distress, acute asthma, leukotrienes over activity, 5-LO enzyme activity and cancer. 2. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.3. The pharmaceutical composition of claim 2 , wherein said pharmaceutical composition is formulated to treat the underlying etiology with an effective amount administering the patient in need by oral administration claim 2 , delayed release or sustained release claim 2 , transmucosal claim 2 , syrup claim 2 , topical claim 2 , parenteral administration claim 2 , injection claim 2 , subdermal claim 2 , oral solution claim 2 , rectal administration claim 2 , buccal administration or transdermal administration.4. A method of treating asthma and allergy related diseases as the underlying etiology claim 3 , wherein said method comprises administering to a patient in need thereof an effective amount of .5. The method of claim 4 , wherein the asthma and allergy as the underlying etiology is selected from respiratory diseases claim 4 , respiratory disorders claim 4 , COPD claim 4 , bronchitis claim 4 , brain injury claim 4 , inflammation claim 4 , allergic rhinitis claim 4 , inflammatory skin diseases claim 4 , asthma claim 4 , allergic reactions claim 4 , infections due to acute allergy claim 4 , ...

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Номер записи: 79
25-08-2022 дата публикации

MICROBIOCIDAL PICOLINAMIDE DERIVATIVES

Номер: US20220264877A1
Автор: BEAUDEGNIES Renaud, BLUM Mathias, Lamberth Clemens, Pouliot Martin, RENDINE Stefano
Принадлежит: SYNGENTA CROP PROTECTION AG

Compounds of the formula (I) wherein the substituents are as defined in claim , useful as pesticides, and especially fungicides. 2. The compound according to claim 1 , wherein Ris hydrogen claim 1 , formyl claim 1 , C-Calkylcarbonyl claim 1 , C-Calkoxycarbonyl claim 1 , or C-CalkoxyC-Calkylcarbonyl.3. The compound according to claim 1 , wherein Ris hydroxyl claim 1 , C-Cacyloxy claim 1 , C-CalkoxyC-Calkoxy claim 1 , or C-CacyloxyC-Calkoxy.4. The compound according to claim 1 , wherein Ris C-Calkyl claim 1 , C-Calkoxy or C-Ccycloalkyl.5. The compound according to claim 1 , wherein Ris hydrogen.6. The compound according to claim 1 , wherein Rand Rare each independently C-Calkyl claim 1 , C-Ccycloalkyl or C-Chaloalkyl.7. The compound according to claim 1 , wherein Rand Rare both C-Calkyl.8. The compound according to claim 1 , wherein Ris C-Calkyl claim 1 , C-Ccycloalkyl claim 1 , phenyl or heteroaryl claim 1 , wherein the heteroaryl moiety is a 5- or 6-membered aromatic ring which comprises 1 claim 1 , 2 or 3 heteroatoms individually selected from N claim 1 , O and S claim 1 , and wherein the phenyl and heteroaryl moieties are optionally substituted by 1 claim 1 , 2 or 3 substituents claim 1 , which may be the same or different claim 1 , selected from R.9. The compound according to claim 1 , wherein Ris phenyl claim 1 , phenoxy claim 1 , heteroaryl or heteroaryloxy claim 1 , wherein the heteroaryl moiety is a 5- or 6-membered aromatic ring which comprises 1 claim 1 , 2 or 3 heteroatoms individually selected from N claim 1 , O and S claim 1 , and wherein the phenyl and heteroaryl moieties are optionally substituted by 1 claim 1 , 2 or 3 substituents claim 1 , which may be the same or different claim 1 , selected from R.10. The compound according to claim 1 , wherein Ris hydroxyl claim 1 , halogen claim 1 , cyano claim 1 , Calkyl claim 1 , or Chaloalkyl.11. The compound according to selected from:[4-amino-2-[[(1S)-2-[2,2-bis(4-fluorophenyl)-1-methyl-ethoxy]-1-methyl-2- ...

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Номер записи: 80
24-07-2014 дата публикации

METHODS FOR PREPARATION OF THIOPHENE COMPOUNDS

Номер: US20140206888A1
Автор: Guerette Dahrika Milfred Yap, Jurkauskas Valdas, Kline Billie J., Luong Hoa Q., Roeper Stefanie, Ruggiero Piero L., Waldo Michael, Willcox David
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

A method of preparing Compound (1): 2. The method of wherein the reaction of Compound (A) and 3 claim 1 ,3-dimethylbut-1-yne in the presence of said one or more palladium and copper catalysts in step a) is performed in the presence of EtN or PrNH claim 1 , wherein Et is ethyl and Pr is propyl.37-. (canceled)8. The method of wherein the reaction of Compound (A) and 3 claim 1 ,3-dimethylbut-1-yne in the presence of said one or more palladium and copper catalysts in step a) is performed at a temperature in a range of 18° C.-30° C.9. (canceled)10. The method of claim 1 , wherein the reaction of Compound (A) and 3 claim 1 ,3-dimethylbut-1-yne in the presence of said one or more palladium and copper catalysts in step a) is performed in a solvent system that includes 2-methyl tetrahydrofuran claim 1 , 2-butanone claim 1 , or methyl t-butyl ether.11. (canceled)12. The method of claim 1 , wherein the acid for step b) is HCl.1315-. (canceled)16. The method of wherein the reduction of the cyclohexanone of Compound (C) to cyclohexanol is carried out by the use of LiAlH(OBu) claim 1 , wherein Bu is tert-butyl.17. The method of wherein the base of step d) is selected from NaOH claim 1 , LiOH claim 1 , BuNOH claim 1 , or NaOMe claim 1 , or a combination thereof claim 1 , wherein Bu is n-butyl and Me is methyl.18. (canceled)19. The method of further comprising crystallization of Compound (C) from a mixture of acetone claim 1 , 2-butanone claim 1 , and water prior to step c).2022-. (canceled)23. The method of claim 19 , wherein the crystallization of Compound (1) is performed: in ethylacetate at a temperature in a range of 45° C. to 47° C.; in n-butylacetate at a temperature in a range of 35° C. to 47° C.; or in a mixture of n-butyl acetate and acetone at a temperature in a range of 30° C. to 47° C.25. (canceled)28. (canceled)29. (canceled)3136-. (canceled)38. (canceled)39. The method of wherein the step a) is performed in a solvent system that includes THF and/or 2-MeTHF.41. The ...

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Номер записи: 81
12-05-2016 дата публикации

ENHANCER OF ZESTE HOMOLOG 2 INHIBITORS

Номер: US20160130261A1
Автор: Burgess Joelle Lorraine, Knight Steven David
Принадлежит:

This invention relates to novel compounds according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers. 25-. (canceled)79-. (canceled)10. The compound according to claim 1 , wherein Rand Rare each independently (C-C)alkyl claim 1 , or a pharmaceutically acceptable salt thereof.11. The compound according to claim 6 , wherein:{'sup': 1', '2, 'sub': 1', '4, 'Rand Rare each methyl, independently (C-C)alkyl;'}{'sup': '3', 'Ris hydrogen;'}{'sup': '4', 'sub': 1', '3, 'Ris selected from the group consisting of (C-C)alkyl and halogen;'}{'sup': 5', 'a', 'b, 'Ris —NRR;'}{'sup': '6', 'sub': 1', '4', '1', '4, 'Ris hydrogen, halogen, (C-C)alkyl, or (C-C)alkoxy;'}{'sup': 'a', 'sub': 1', '4, 'Ris azetidinyl, oxetanyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, or tetrahydropyranyl, each of which is optionally substituted 1 or 2 times, independently, by (C-C)alkyl; or'}{'sup': 'a', 'sub': 1', '4', '1', '4', '2, 'Ris cyclopentyl or cyclohexyl, each of which is optionally substituted by amino, —NH(C-C)alkyl, or —N((C-C)alkyl), and'}{'sup': 'b', 'sub': 1', '4, 'Ris hydrogen or (C-C)alkyl;'}or a pharmaceutically acceptable salt thereof.12. The compound according to claim 1 , wherein Ris hydrogen claim 1 , or a pharmaceutically acceptable salt thereof.13. (canceled)14. The compound according to claim 1 , wherein Ris selected from the group consisting of (C-C)alkyl and halogen claim 1 , or a pharmaceutically acceptable salt thereof.1516-. (canceled)17. The compound according to claim 1 , wherein Ris selected from the group consisting of (C-C)alkoxy claim 1 , (C-C)cycloalkyloxy- claim 1 , heterocycloalkyloxy- claim 1 , heterocycloalkyl claim 1 , —NH((C-C)cycloalkyl) claim 1 , —N((C-C)alkyl)((C-C)cycloalkyl) claim 1 , —NH(heterocycloalkyl) claim 1 , and —N((C-C)alkyl)(heterocycloalkyl) claim 1 , ...

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Номер записи: 82
14-05-2015 дата публикации

Process for sorafenib tosylate polymorph iii

Номер: US20150133670A1
Автор: BANDI Parthasaradhi Reddy, Bandi Vamsi Krishna, Dasari Muralidhara Reddy, KURA Rathnakar Reddy, Thungathurthy Srinivasa Rao
Принадлежит: HETERO RESEARCH FOUNDATION

The present invention provides a novel process for the preparation of sorafenib tosylate polymorph III.

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Номер записи: 83
10-05-2018 дата публикации

SYNTHESIS OF NON-CYCLIC AMIDE AND THIOAMIDE BASED IONIC LIQUIDS

Номер: US20180127352A1
Автор: Bhattacharyya Alakananda, Broderick Erin M., Buchbinder Avram M.
Принадлежит:

Non-cyclic amide or thioamide based ionic liquids and methods of making them are disclosed. The non-cyclic amide or thioamide based ionic liquid comprises a cation and an anion and has the formula: 2. The ionic liquid of wherein the anion is a carboxylate claim 1 , a nitrate claim 1 , a phosphate claim 1 , a phosphinate claim 1 , a phosphonate claim 1 , an imide claim 1 , a cyanate claim 1 , a borate claim 1 , a sulfate claim 1 , a sulfonate claim 1 , an acetate claim 1 , a halide claim 1 , a halometallate claim 1 , and combinations thereof.3. The ionic liquid of wherein the anion is the halide and wherein the halide is bromide claim 1 , chloride claim 1 , iodide claim 1 , fluoride claim 1 , or combinations thereof.4. The ionic liquid of wherein the anion is the halometallate claim 1 , wherein the metal in the halometallate comprises Sn claim 1 , Al claim 1 , Zn claim 1 , Mn claim 1 , Fe claim 1 , Ga claim 1 , Cu claim 1 , Ni claim 1 , Co claim 1 , In claim 1 , or combinations thereof claim 1 , and wherein the halide in the halometallate comprises bromide claim 1 , chloride claim 1 , iodide claim 1 , fluoride claim 1 , or combinations thereof claim 1 , and wherein the halometallate optionally includes an —OH group.5. The ionic liquid of wherein the anion is the halometallate claim 1 , and wherein the halometallate comprises AlCl claim 1 , AlCl claim 1 , AlCl claim 1 , AlClBr claim 1 , AlClBr claim 1 , AlClBr claim 1 , AlBr claim 1 , AlBr claim 1 , AlBr claim 1 , GaCl claim 1 , GaCl claim 1 , GaCl claim 1 , GaClBr claim 1 , GaClBr claim 1 , GaClBr claim 1 , CuCl claim 1 , CuCl claim 1 , CuCl claim 1 , ZnCl claim 1 , FeCl claim 1 , FeCl claim 1 , FeCl claim 1 , InCl claim 1 , InCl claim 1 , InCl claim 1 , or combinations thereof.6. The ionic liquid of wherein the cation comprises N claim 1 ,N-dimethylacetamidium claim 1 , acetamidium claim 1 , carbonyl diamidium claim 1 , thioamidium claim 1 , N-methylthioacetamidium claim 1 , N claim 1 ,N-dimethylthioacetamidium ...

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Номер записи: 84
10-05-2018 дата публикации

ISOLATION OF BONA FIDE PANCREATIC PROGENITOR CELLS

Номер: US20180127724A1
Автор: Ameri Jacqueline, Semb Henrik
Принадлежит:

The present invention relates to a method for isolating bona fide pancreatic progenitor cells and to cell populations enriched for bona fide pancreatic progenitor cells. 1. A method for isolating a population enriched for bona fide pancreatic progenitor cell , said method comprising the steps of:i) providing a cell population comprising at least one bona fide pancreatic progenitor cell, wherein the bona fide pancreatic progenitor cell expresses PDX1 and NKX6-1; and a) a first ligand which binds to a first marker specific for PDX1− cells and selecting the cells that do not bind to said first ligand from said cell population, thereby enriching the cell population for PDX1+ cells;', 'and/or', 'b) a second ligand which binds to a second marker specific for PDX1+ cells and selecting the cells that bind to said second ligand from the cells that do not bind to said second ligand, thereby enriching the cell population for PDX1+ cells;', 'and/or', 'c) a third ligand which binds to a third marker specific for PDX1+ NKX6-1+ cells and selecting the cells that bind to said third ligand from the cells that do not bind to said third ligand, thereby enriching the cell population for PDX1+ NKX6-1+ cells;, 'ii) exposing said cell population tothereby obtaining a cell population enriched for bona fide pancreatic progenitor cells.2. The method according to claim 1 , wherein at least one of the first claim 1 , second and third ligands is an antibody or fragment thereof.3. The method according to any one of the preceding claims claim 1 , wherein the antibody is a monoclonal or polyclonal antibody.4. The method according to any one of the preceding claims claim 1 , wherein at least one of the first claim 1 , second and third ligand binds to a cell surface marker of the bona fide pancreatic progenitor cell.5. The method according to any one of the preceding claims claim 1 , wherein at least one of the first claim 1 , second and third ligand is conjugated to a label.6. The method according ...

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Номер записи: 85
21-05-2015 дата публикации

SOLID FORMS OF ACETIC ACID, COMPOSITIONS, AND USES THEREOF

Номер: US20150141467A1
Автор: Copp James Densmore, Luong Anne, Newman Ann W.
Принадлежит:

Provided herein are solid forms comprising {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders. 2. The crystalline compound of claim 1 , wherein the crystalline compound comprises less than 15% by weight of any other crystalline Compound (I).3. The crystalline compound of claim 2 , wherein the crystalline compound comprises less than 10% by weight of any other crystalline Compound (I).4. The crystalline compound of claim 3 , wherein the crystalline compound comprises less than 5% by weight of any other crystalline Compound (I).6. The crystalline compound of claim 5 , wherein the crystalline compound comprises less than 15% by weight of amorphous Compound (I).7. The crystalline compound of claim 6 , wherein the crystalline compound comprises less than 10% by weight of amorphous Compound (I).8. The crystalline compound of claim 7 , wherein the crystalline compound comprises less than 5% by weight of amorphous Compound (I).10. The crystalline compound of claim 9 , which has an X-ray powder diffraction pattern comprising one claim 9 , two claim 9 , three claim 9 , four claim 9 , or five peaks at approximately 18.1 claim 9 , 20.3 claim 9 , 22.9 claim 9 , 24.0 claim 9 , and 26.3° 2θ.11. The crystalline compound of claim 10 , wherein the crystalline compound comprises less than 100 ppm of a compound of Formula (II).12. The crystalline compound of claim 11 , wherein the crystalline compound comprises less than 50 ppm of a compound of Formula (II).13. The crystalline compound of claim 12 , wherein the crystalline compound comprises less than 10 ppm of a compound of Formula (II).14. The crystalline compound of claim 13 , wherein the crystalline compound comprises less than 1 ppm of a compound of Formula (II).16. The crystalline compound of claim 15 , wherein the crystalline Compound (I) is at least 99.6% ...

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Номер записи: 86
07-08-2014 дата публикации

PROCESS FOR THE PREPARATION OF 4-CARBONYL)AMINO]-3-FLUOROPHENOXY}-N-ETHYLPYRIDINE-2-CARBOXAMIDE, ITS SALTS AND MONOHYDRATE

Номер: US20140221661A1
Автор: Gottfried Michael, Heilmann Werner, L.GERS Michael, Rehse Joachim, Stiehl Juergen, Wichmann Saskia
Принадлежит: Bayer Intellectual Property GmbH

The present invention relates to a process for preparing 4-(4-[({[4-chloro-3-(trifluoromethyl)-phenyl]amino}carbonyl)amino]-3-fluorophenoxy)-N-methylpyridine-2-carboxamide, its salts and monohydrate. 1. (canceled)2. (canceled)3. (canceled)4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. (canceled)9. (canceled)10. (canceled)11. (canceled)12. (canceled)13. (canceled)15. The compound of wherein the compound of the formula (I) claim 14 , its monohydrate or salt is contaminated with 4-amino-3-fluorophenol and/or 4-(4-amino-3-fluorophenoxy)pyridine-2-carboxylic acid methylamide each in an amount of from 0.0001% to a maximum of 0.05% by weight based on the amount of the compound of the formula (I).17. The composition of which comprises 4-amino-3-fluorophenol and/or 4-(4-amino-3-fluorophenoxy)pyridine-2-carboxylic acid methylamide each in an amount of from 0.0001% to a maximum of 0.05% by weight based on the combined weight of the compound of the formula (I) claim 16 , the monohydrate of the compound of formula (I) claim 16 , and salts of the compound of formula (I) within the composition. The present invention relates to a process for preparing 4-{4-[({[4-chloro-3-(trifluoromethyl)-phenyl]amino}carbonyl)amino]-3-fluorophenoxy}-N-methylpyridine-2-carboxamide, its salts and monohydrate.4-{4-[({[4-chloro-3-(trifluoromethyl)phenyl]amino}carbonyl)amino]-3-fluorophenoxy})-N-methylpyridine-2-carboxamide is mentioned in WO 05/009961 and corresponds to the compound of the formula (I):The monohydrate of the compound of formula (I) is mentioned in WO 08/043,446. Furthermore salts of the compound of formula (I) such as its hydrochloride, mesylate and phenylsulfonate are mentioned in WO 05/009961 and can be formed by treating the compound of the formula (I) with the corresponding acid. The compound of formula (I) is described for treating hyper-proliferative disorders such as cancers, tumors, lymphomas, sarcomas and leukemias.WO 05/009961 describes a process for preparing the ...

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Номер записи: 87
04-06-2015 дата публикации

SOLID STATE FORMS OF N-((S)-2,3-DIHYDROXY-PROPYL)-3-(2-FLUORO-4-IODO-PHENYLAMINO)-ISONICOTINAMIDE

Номер: US20150152059A1
Автор: Bankston Donald, Becker Axel, Kuehn Clemens, Poma Marco, Saal Christoph
Принадлежит: Merck Patent GmBH

The invention relates to solid state forms of N—((S)-2,3-Dihydroxy-propyl)-3-(2-fluoro-4-iodo-phenylamino)-isonicotinamide, processes for their preparation, and medical uses thereof. 1. A solid state form of N—((S)-2 ,3-Dihydroxy-propyl)-3-(2-fluoro-4-iodo-phenylamino)-isonicotinamide or its pharmaceutically acceptable salts.2. The solid state form according to claim 1 , in which the solid state form or its pharmaceutically acceptable salt is a crystalline form.3. The solid state form according to claim 2 , in which the pharmaceutically acceptable salt is the mono hydrochloride.4. The solid state form according to claim 2 , which is the free base of N—((S)-2 claim 2 ,3-Dihydroxy-propyl)-3-(2-fluoro-4-iodo-phenylamino)-isonicotinamide.5. A solid state form A1 according to claim 3 , having characteristic Cu-KαX-ray peaks at 2θ angles corresponding to 5.5±0.2 claim 3 , 16.8±0.2 claim 3 , 18.5±0.2 claim 3 , 19.1±0.2 claim 3 , 22.6±0.2 claim 3 , 23.0±0.2 claim 3 , 24.9±0.2 claim 3 , 25.2±0.2 claim 3 , 28.4±0.2 claim 3 , 29.2±0.2 degrees.6. A solid state form A1 according to claim 3 , having characteristic Cu-KαX-ray peaks at 2θ angles corresponding to one or more of the following lists of peaks:a) 5.5±0.2, 16.8±0.2, 19.5±0.2, 23.0±0.2 degrees;b) 5.5±0.2, 18.5±0.2, 19.1±0.2, 28.4±0.2, 29.6±0.2 degrees;c) 15.9±0.2, 19.1±0.2, 24.9±0.2 degrees.7. A solid state form A1 according to claim 3 , having the space group P2with the lattice parameters a=9.6±0.1 Å claim 3 , b=11.2±0.1 Å claim 3 , c=16.6±0.1 Å claim 3 , and β=104.4±0.5° (α=γ=90°) when measured at 301 K.8. A solid state form A2 according to claim 3 , having characteristic Cu-KαX-ray peaks at 2θ angles corresponding to 5.4±0.2 claim 3 , 9.6±0.2 claim 3 , 18.4±0.2 claim 3 , 18.6±0.2 claim 3 , 20.9±0.2 claim 3 , 21.6±0.2 claim 3 , 23.9±0.2 claim 3 , 24.4±0.2 claim 3 , 25.0±0.2 claim 3 , 26.0±0.2 degrees.9. A solid state form A2 according to claim 3 , having characteristic Cu-KαX-ray peaks at 2θ angles corresponding to one ...

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Номер записи: 88
04-06-2015 дата публикации

BENZOTHIOPHENE SULFONAMIDES DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS

Номер: US20150152080A1
Автор: Beard Richard L., Liu Xiaoxia, Yuan Haiqing
Принадлежит:

The present invention relates to benzothiophene sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors. 2. A compound according to wherein:n is 0.3. A compound according to wherein:X is CR; andR is hydrogen.4. A compound according to wherein:X is CR;R is hydrogen; andn is 0.5. A compound according to selected from:methyl 2-[({2-[(1-benzothiophen-2-ylsulfonyl)amino]-4-fluorophenyl}sulfanyl)methyl]benzoate;2-[({2-[(1-benzothiophen-2-ylsulfonyl)amino]-4-fluorophenyl}sulfanyl)methyl]benzoic acid;N-[2-(Benzylsulfinyl)pyridin-3-yl]-1-benzothiophene-2-sulfonamide;N-[2-(Benzylsulfonyl)pyridin-3-yl]-1-benzothiophene-2-sulfonamide;N-[2-(Benzylsulfanyl)pyridin-3-yl]-1-benzothiophene-2-sulfonamide;2-[({2-[(1-Benzothiophen-2-ylsulfonyl)amino]-5-methylphenyl}sulfanyl)methyl]benzoic acid;Methyl 2-[({2-[(1-Benzothiophen-2-ylsulfonyl)amino]-5-methylphenyl}sulfanyl) methyl]benzoate;N-{2-[(3-Aminobenzyl)sulfonyl]-5-chlorophenyl}-1-benzothiophene-2-sulfonamide;2-[({2-[(1-Benzothiophen-2-ylsulfonyl)amino]-4-methylphenyl}sulfanyl)methyl]benzoic acid;N-(5-Chloro-2-((3-nitrobenzyl)thio)phenyl)benzo[b]thiophene-2-sulfonamide;N-(5-Chloro-2-((3-nitrobenzyl)sulfonyl)phenyl)benzo[b]thiophene-2-sulfonamide;Methyl 2-[({2-[(1-benzothiophen-2-ylsulfonyl)amino]-4-methylphenyl}sulfanyl) methyl]benzoate;2-[({2-[(1-Benzothiophen-2-ylsulfonyl)amino]-4-chlorophenyl}sulfanyl)methyl]benzoic acid; andMethyl 2-[({2-[(1-benzothiophen-2-ylsulfonyl)amino]-4-chlorophenyl}sulfanyl) methyl]benzoate.6. A pharmaceutical composition comprising as active ingredient a therapeutically effective amount of a compound according to and a pharmaceutically acceptable adjuvant claim 1 , diluent or carrier.7. A pharmaceutical composition according to wherein the compound is selected from:methyl 2-[({2-[(1-benzothiophen-2-ylsulfonyl)amino]-4-fluorophenyl}sulfanyl)methyl]benzoate;2-[({2-[(1-benzothiophen-2-ylsulfonyl) ...

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Номер записи: 89
25-05-2017 дата публикации

PROCESSES FOR PREPARING BREXPIPRAZOLE

Номер: US20170145001A1
Автор: GUO Jiunn-Cheh, HUANG Shu Ting, Kuo Lung-Huang, Lee Chia-Ying, Liao Yuan-Xiu, WANG Hsin-Chi
Принадлежит:

The present disclosure provides processes for preparing brexpiprazole. The present disclosure also provides processes for the purification of brexpiprazole. The processes for preparing and purifying brexpiprazole of the present invention provide substantial improvements over currently known methods. In certain embodiments, the conversion of Formula XI and XII to form XIII provides increased selectivity over previously reported methods. This offers increased yield and purity. The improved process for purifying brexpiprazole disclosed herein provides brexpiprazole with superior purity and is also more suitable for industrial production. 3. The process of claim 1 , further comprising(3-i) contacting brexpiprazole, the organic solvent, and the reducing agent with an metal hydroxide to form solid brexpiprazole;(3-ii) separating solid brexpiprazole to form isolated brexpiprazole.4. The process of claim 3 , wherein the metal hydroxide is NaOH.5. The process of claim 1 , wherein the reducing agent is selected from the group consisting of sodium cyanoborohydride claim 1 , sodium borohydride claim 1 , sodium triacetoxy-borohydride claim 1 , and 2-methylpyridine borane complex.6. The process of claim 5 , wherein the reducing agent is sodium triacetoxy-borohydride.7. The process of claim 1 , wherein the organic solvent is selected from the group consisting of dimethyl sulfoxide (DMSO) claim 1 , dimethylacetate (DMAc) claim 1 , dichloromethane claim 1 , and acetone.8. The process of claim 7 , wherein the organic solvent is DMSO.10. The process of claim 9 , wherein the acid is selected from the group consisting of HCl claim 9 , HBr claim 9 , HI claim 9 , HSO claim 9 , HPO claim 9 , and acetic acid.11. The process of claim 10 , wherein the acid is HCl.12. The process of claim 11 , wherein the final concentration of acid in step (2) is from 5-40% (v/v).13. The process of claim 12 , wherein the final concentration of acid in step (2) is from 5-20% (v/v).14. The process of claim 13 , ...

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Номер записи: 90
14-08-2014 дата публикации

ALKENE AZETIDINE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS

Номер: US20140228344A1
Автор: Chow Ken, CORPUZ EVELYN G., FANG WENKUI K.
Принадлежит: ALLERGAN, INC.

The present invention relates to alkene azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. 6. The compound of in an E geometrical configuration.7. The compound of in an mixture of E and Z geometrical configuration.8. A compound according to wherein Lis S(O).9. A compound according to wherein Lis S.10. A compound according to wherein Lis O.11. A compound according to claim 1 , selected from:1-(4-{[(5E)-5-(3,5-difluorophenyl)-6-(3,4-dimethylphenyl)hex-5-en-1-yl]sulfanyl}benzyl)azetidine-3-carboxylic acid;1-(4-{[(4E)-4-(3,5-difluorophenyl)-5-(3,4-dimethylphenyl)pent-4-en-1-yl]sulfinyl}benzyl)azetidine-3-carboxylic acid;1-(4-{[(4E)-4-(3,5-difluorophenyl)-5-(3,4-dimethylphenyl)pent-4-en-1-yl]oxy}benzyl)azetidine-3-carboxylic acid;1-(4-{[(4E)-4-(3-chlorophenyl)-5-(3,4-dimethylphenyl)pent-4-en-1-yl]oxy}benzyl)azetidine-3-carboxylic acid;1-(4-{[(4E)-4-(2,3-difluorophenyl)-5-(3,4-dimethylphenyl)pent-4-en-1-yl]oxy}benzyl)azetidine-3-carboxylic acid;1-(4-{[5-(3,4-dimethylphenyl)-4-(3-thienyl)pent-4-en-1-yl]oxy}benzyl)azetidine-3-carboxylic acid; and1-(4-{[3-(3,5-difluorophenyl)-4-(3,4-dimethylphenyl)but-3-en-1-yl]thio}benzyl)azetidine-3-carboxylic acid.12. A pharmaceutical composition comprising as active ingredient a therapeutically effective amount of a compound according to and a pharmaceutically acceptable adjuvant claim 1 , diluent or carrier.13. A pharmaceutical composition according to wherein the compound is selected from1-(4-{[(5E)-5-(3,5-difluorophenyl)-6-(3,4-dimethylphenyl)hex-5-en-1-yl]sulfanyl}benzyl)azetidine-3-carboxylic acid;1-(4-{[(4E)-4-(3,5-difluorophenyl)-5-(3,4-dimethylphenyl)pent-4-en-1-yl]sulfinyl}benzyl)azetidine-3-carboxylic acid;1-(4-{[(4E)-4-(3,5-difluorophenyl)-5-(3,4-dimethylphenyl)pent-4-en-1-yl]oxy}benzyl)azetidine-3-carboxylic acid;1-(4-{[(4E)-4-(3-chlorophenyl)-5-(3,4-dimethylphenyl)pent-4-en-1-yl]oxy}benzyl) ...

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Номер записи: 91
15-09-2022 дата публикации

COMPOSITIONS AND METHODS FOR THE TREATMENT AND PREVENTION OF HYPOGLYCEMIC COMPLICATIONS

Номер: US20220288169A1
Автор: McDougal David
Принадлежит:

This invention is directed to compositions and methods for the treatment and prevention of hypoglycemic complications. Specifically, aspects of the invention are drawn to the use of leptin for the treatment and prevention of hypoglycemic complications. 1. A method of preventing a hypoglycemia-associated complication , the method comprising administering to a subject in need thereof a therapeutically effective amount of a composition comprising leptin , a fragment thereof , and/or a leptin receptor agonist.2. A method of treating a hypoglycemia-associated complication , the method comprising administering to a subject in need thereof a therapeutically effective amount of a composition comprising leptin , a fragment thereof , and/or a leptin receptor agonist.3. The method of or , wherein the hypoglycemia-associated complication is HAAF.4. The method of or , wherein the composition is administered prior to the onset of severe hypoglycemia.5. The method of or , wherein the composition is administered at about the same time as the onset of severe hypoglycemia.6. The method of or , wherein the leptin comprises human recombinant leptin.7. The method of or , wherein the method comprises administering a short course of leptin.8. The method of or , wherein the method comprises chronic administration of leptin.9. The method of or , wherein the subject in need thereof is afflicted with diabetes.10. The method of or , wherein the composition further comprises insulin.11. A therapeutic combination composition comprising leptin , a fragment thereof , or a leptin receptor agonist , and at least one additional active agent.12. The therapeutic combination composition of claim 11 , wherein the composition further comprises a pharmaceutically acceptable carrier claim 11 , diluent claim 11 , or excipient.13. The therapeutic combination composition of claim 11 , wherein the at least one additional active agent comprises insulin or an insulin secretagogue.14. The therapeutic combination ...

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Номер записи: 92
02-06-2016 дата публикации

Quinone derivative and electrophotographic photosensitive member

Номер: US20160152556A1
Автор: Fumio Sugai, Hideki Okada, Kensuke Kojima
Принадлежит: Kyocera Document Solutions Inc

A quinone derivative represented by general formula (1) where, in the general formula (1), chemical groups R 1 each represent, independently of one another, an alkyl group, a cycloalkyl group, an alkoxy group, an aralkyl group, or an aryl group, and R 2 represents an alkyl group, an aralkyl group, a cycloalkyl group, an alkoxy group, an aryl group, or a heterocyclic group.

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Номер записи: 93
16-05-2019 дата публикации

Process for the Preparation of 4-(4-amino-3-fluorophenoxy)-N-methylpyyridine-2-carboxamide

Номер: US20190144391A1
Автор: Gottfried Michael, Heilmann Werner, Lögers Michael, Rehse Joachim, Stiehl Juergen, Wichmann Saskia
Принадлежит: Bayer HealthCare LLC

The present invention relates to a process for preparing 4-(4-[({[4-chloro-3-(trifluoromethyl)-phenyl]amino}carbonyl)amino]-3-fluorophenoxy}-N-methylpyridine-2-carboxamide, its salts and monohydrate. 115.-. (canceled)18. A process according to claim 17 , wherein said organic solvent is 1-methyl-2-pyrrolidinone claim 17 , dimethylformamide claim 17 , N claim 17 ,N-dimethylacetamid claim 17 , dimethyl sulfoxide claim 17 , sulfolane or mixtures thereof.19. A process according to claim 18 , wherein said organic solvent is 1-methyl-2-pyrrolidinone and/or dimethylformamide.20. A process according to claim 17 , wherein said base is an alkali metal hydroxide or an alkali metal alkoxide.21. A process according to claim 17 , wherein said base is potassium tert-butoxide.22. A process according to claim 17 , wherein said base is potassium tert-butoxide in a tetrahydrofuran solution.23. A process according to claim 17 , wherein the reaction mixture of the compound of formula II and a compound of formula III is heated to a temperature of from 50° C. to 150° C. and acetic acid in water is added.24. A process according to claim 17 , wherein the reaction mixture is heated to a temperature of from 80° C. to 120° C. and after 2-4 hours the temperature is adjusted to between 50° C. to 90° C.25. A process according to claim 17 , wherein Rand Rare independently selected from the group consisting of hydrogen claim 17 , methyl claim 17 , ethyl claim 17 , n-propyl claim 17 , iso-propyl claim 17 , n-butyl claim 17 , iso-butyl claim 17 , sec-butyl claim 17 , tert-butyl claim 17 , n-pentyl claim 17 , 2-pentyl claim 17 , 3-pentyl claim 17 , neopentyl claim 17 , n-hexyl claim 17 , 2-hexyl and 3-hexyl.26. A process according to claim 17 , wherein Rand Rare joined and claim 17 , taken together with the carbon atom to which they are attached claim 17 , form a 4- to 7-membered cycloalkyl ring.28. The method of claim 27 , wherein the precipitated purified salt of 4-chloro-N-methyl-2- ...

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Номер записи: 94
31-05-2018 дата публикации

CHARGE-TRANSPORTING VARNISH, AND ORGANIC ELECTROLUMINESCENT ELEMENT

Номер: US20180151805A1
Автор: ENDO Toshiyuki, NAKAZAWA Taichi
Принадлежит: NISSAN CHEMICAL INDUSTRIES, LTD.

Provided are: a charge-transporting varnish that contains a charge-transporting substance comprising an oligoaniline derivative represented by formula (1), a charge transporting substance that does not contain fluorine atoms, and an organic solvent; and an organic electroluminescent element including a thin film obtained from the varnish. 2. The charge-transporting varnish of claim 1 , wherein letter A is a fluoroalkyl group having 1 to 20 carbon atoms which may be substituted with a cyano group claim 1 , chlorine atom claim 1 , bromine atom claim 1 , iodine atom claim 1 , nitro group or fluoroalkoxy group having 1 to 20 carbon atoms; a fluoroaryl group having 6 to 20 carbon atoms which may be substituted with a cyano group claim 1 , chlorine atom claim 1 , bromine atom claim 1 , iodine atom claim 1 , nitro group claim 1 , alkyl group having 1 to 20 carbon atoms claim 1 , fluoroalkyl group having 1 to 20 carbon atoms or fluoroalkoxy group having 1 to 20 carbon atoms; or an aryl group having 6 to 20 carbon atoms is substituted with a fluoroalkyl group having 1 to 20 carbon atoms claim 1 , fluorocycloalkyl group having 3 to 20 carbon atoms claim 1 , fluorobicycloalkyl group having 4 to 20 carbon atoms claim 1 , fluoroalkenyl group having 2 to 20 carbon atoms or fluoroalkynyl group having 2 to 20 carbon atoms claim 1 , and may be substituted with a cyano group claim 1 , halogen atom claim 1 , or fluoroalkoxy group having 1 to 20 carbon atoms.3. The charge-transporting varnish of claim 2 , wherein letter A is a phenyl group which is substituted with at least 3 fluorine atoms claim 2 , and may be substituted with a cyano group claim 2 , chlorine atom claim 2 , bromine atom claim 2 , iodine atom claim 2 , nitro group claim 2 , alkyl group having 1 to 20 carbon atoms claim 2 , fluoroalkyl group having 1 to 20 carbon atoms or fluoroalkoxy group having 1 to 20 carbon atoms; or a phenyl group which is substituted with a fluorocycloalkyl group having 3 to 20 carbon atoms claim ...

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Номер записи: 95
09-06-2016 дата публикации

FUSED HETEROCYCLIC COMPOUND

Номер: US20160159743A1
Автор: Ito Mai, Nokura Yoshihiko, TAKAHASHI Masaki, Tanabe Takamasa
Принадлежит:

There is provided a compound having an excellent controlling effect on pests represented by the formula (1): 122.-. (canceled)241. The compound according to claim , wherein Ais —NR— in the formula (M20-1). The present application is filed claiming the priority of the Japanese Patent Application Nos. 2011-170833, 2012-079323 and 2012-122837, the entire contents of which are herein incorporated by reference.The present invention relates to a fused heterocyclic, compound and the use thereof for pest control.For controlling pests, various compounds have been developed and used practically.Further, some fused heterocyclic compounds are known (see, Patent Literature 1).An object of the present invention is to provide a novel compound having an excellent controlling effect on pests and a method for controlling pests with said compound.The inventors of the present invention have intensively studied, and as a result, they have found that a fused heterocyclic compound represented by the following formula (1) has an excellent controlling effect on pests. Thus, the present invention has been completed.The present invention includes the followings:[1] A fused heterocyclic compound represented by the formula (1):wherein Arepresents —NR—, an oxygen atom or a sulfur atom, Arepresents a nitrogen atom or ═CR—, Arepresents a nitrogen atom or ═CR—, Rrepresents a C1-C6 chain hydrocarbon group optionally substituted by one or more atoms or groups selected from Group X or a C3-C6 alicyclic hydrocarbon group optionally substituted by one or more atoms or groups selected from R, Rand Rare the same or different and each represents a C1-C6 chain hydrocarbon group optionally substituted by one or more atoms or groups selected from Group X, a phenyl group optionally substituted by one or more atoms or groups selected from Group Z, a 5- or 6-membered heterocyclic group optionally substituted by one or more atoms or groups selected from Group Z, —OR, —S(O)R, —S(O)NRR, —NRR, —NRCOR, —NRC(O)R, —COR ...

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Номер записи: 96
28-08-2014 дата публикации

REDUCTION OF HMF ETHERS WITH METAL CATALYST

Номер: US20140239230A1
Автор: Bloom Paul, Sanborn Alexandra
Принадлежит: ARCHER DANIELS MIDLAND COMPANY

Methods of making reduced derivatives of hydroxymethyl furfural using metal catalysts are described. The derivatives may have tetrahydrofuran or furan nucleus with alkoxymethyl ether or ester moieties on the 5′ carbon and methanol on the 2′ carbon. Suitable metal catalyst include Raney nickel, a nickel catalyst with a zirconium promoter, a chromite catalyst with a barium, a palladium catalyst, such as palladium on carbon, or a ruthenium catalyst. Also provided are a new class of compounds, which are n-alkoxy hexane diols (i.e., 1,2 or 1,5 hexane diol ethers) and methods of making the same by reduction of furan or tetrahydrofuran derivatives. 2. The method of claim 1 , where the source contains at least 40% of the R-5′acyloxymethylfurfural ester as a fraction of dissolved solutes in the source and the desired compound formed is predominantly the (5-acyloxymethyl)-tetrahydrofuran-2-methanol.3. The method of claim 1 , where the source contains at least 40% of the R-5′acyloxymethylfurfural ester as a fraction of dissolved solutes in the source and the desired compound formed is predominantly the (5-acyloxymethyl)-furan-2-methanol.4. The method of claim 1 , where the source contains less than 40% of the R-5′acyloxymethylfurfural ester as a fraction of dissolved solutes in the source and additionally contains at least 20% of at least one compounds selected from the group consisting of alkyl levulinates and humins as a fraction of dissolved solutes in the source and the desired compound formed is predominantly the (5-acyloxymethyl)-furan-2-methanol.5. The method of claim 1 , wherein the temperature is 140-250° C. claim 1 , the pressure is 500-1500 psi claim 1 , the time is 30 min to 14 hours claim 1 , the source is greater than 80% pure claim 1 , and the reaction converts the acyloxymethylfurfural ester to the (5-acyloxymethyl)-tetrahydrofuran-2-methanol compound.6. The method of claim 1 , wherein the temperature is 170-205° C. claim 1 , the source is less than 80% pure ...

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Номер записи: 97
16-06-2016 дата публикации

Pyridine-2-carboxamides as nematocides

Номер: US20160165887A1
Автор: André Jeanguenat, Olivier Loiseleur, Régis Jean Georges MONDIERE
Принадлежит: SYNGENTA PARTICIPATIONS AG

Compounds of the formula (I), in which the substituents are as defined in claim 1 , are suitable for use as nematicides.

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Номер записи: 98
04-09-2014 дата публикации

OPTICALLY ACTIVE FLUCONAZOLE ANALOGUES CONTAINING THIOPHENES AS ANTIFUNGAL AGENTS

Номер: US20140249194A1
Автор: Borate Hanumant Bapurao, Chandavarkar Mohan Anand, Chavan Subhash Prataprao, IYER RAMAKRISHNAN RAMACAHNDRAN, Rao Deepali Damodar, SAWARGAVE SANGESHWER PRABHAKAR, Tawte Amit Chandrakant
Принадлежит:

The invention discloses optically active compounds of Formula (1a) or Formula (1b), 3. The optically active antifungal compound of claim 2 , having an enantiomeric excess of between about 97.5% and about 99.9%.5. The process as claimed in claim 4 , wherein the base is selected from the group consisting of at least one organic base claim 4 , at least one inorganic base claim 4 , and mixtures thereof.6. The process as claimed in claim 5 , wherein the inorganic base is selected from the group consisting of potassium carbonate claim 5 , sodium carbonate claim 5 , and cesium carbonate.7. The process as claimed in claim 4 , wherein the catalyst is a quaternary ammonium phase transfer catalyst.8. The process as claimed in claim 4 , wherein the catalyst is a phase transfer catalyst selected from the group consisting of tetrabutylammonium bromide claim 4 , tertrabutylammonium chloride claim 4 , triethylbenzylammonium chloride and cetyltrimethylammonium bromide.9. A process for preparation of the optically active antifungal compound of claim 1 , comprising:separating a mixture of a compound of Formula (1a) and a compound of Formula (1b) by High Performance Liquid Chromatography (HPLC) using a chiral HPLC column.10. The process of claim 9 , wherein the mixture is a racemic mixture.11. The process of claim 9 , wherein said chiral HPLC column is a chiral HPLC column selected from the group consisting of:cellulose tris(3,5-dimethylphenylcarbamate) coated on silica-gel,cellulose tris(4-methylbenzoate) coated on silica-gel; andtris-(3,5-dimethylphenyl)-carbamoyl amylose coated on silica-gel.12. The process of claim 9 , wherein said chiral HPLC column is a chiral preparative HPLC column.13. The process of claim 9 , wherein said separating is carried out using a mobile phase comprising at least one hydrocarbon claim 9 , at least one alcohol claim 9 , and an optional acid.14. The process of claim 9 , wherein said separating is carried out using a mobile phase comprising from 40% to 90 ...

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Номер записи: 99
15-06-2017 дата публикации

BENZOTHIOPHENE-BASED SELECTIVE ESTROGEN RECEPTOR DOWNREGULATOR COMPOUNDS

Номер: US20170166551A1
Автор: Thatcher Gregory R., Tonetti Debra A., Xiong Rui, Zhao Jiong
Принадлежит: The Board of Trustees of the University of Illinois

This invention is benzothiophene-based estrogen receptor downregulators and their compositions and uses to treat estrogen-related medical disorders. 2. The compound of claim 1 , wherein Xis —O—.3. The compound of claim 1 , wherein Xis —S—.4. The compound of claim 2 , wherein Ris selected from hydroxyl and —O(C-Calkyl).5. The compound of claim 4 , wherein Ris selected from —COOH claim 4 , —NH(CO)COOH and —CH═CHCOOH.6. The compound of claim 5 , wherein Ring D is phenyl claim 5 , naphthyl or quinolinyl and Ring E is phenyl or thienyl.8. The compound of claim 7 , wherein Ris independently selected at each occurrence from hydrogen claim 7 , halogen claim 7 , and C-Calkyl claim 7 , wherein C-Calkyl is methyl.10. The compound of claim 9 , wherein Ris independently selected at each occurrence from hydrogen claim 9 , halogen claim 9 , and C-Calkyl claim 9 , wherein C-Calkyl is methyl.13. The compound of claim 12 , wherein Ris independently selected at each occurrence from hydrogen claim 12 , halogen claim 12 , and C-Calkyl claim 12 , wherein C-Calkyl is methyl.18. A pharmaceutical composition comprising a compound according to and a pharmaceutically acceptable carrier or excipient.19. A method of treating an estrogen-related disorder in a subject comprising administering to a subject in need thereof a therapeutically effective amount of a compound or pharmaceutical composition according to or a pharmaceutically acceptable salt thereof.20. The method of claim 19 , wherein the estrogen-related disorder is a cancer.21. The method of claim 20 , wherein the cancer is selected from the group consisting of breast cancer claim 20 , ovarian cancer claim 20 , endometrial cancer claim 20 , prostate cancer claim 20 , and lung cancer.22. The method of claim 20 , wherein the cancer is selected from the group consisting of breast cancer claim 20 , ovarian cancer claim 20 , and endometrial cancer.23. The method of claim 20 , wherein the cancer is breast cancer.24. The method of claim 23 , ...

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Номер записи: 100