Настройки

Укажите год
-

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

Подробнее
-

Мониторинг СМИ

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

Подробнее

Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Укажите год
Укажите год

Применить Всего найдено 3399. Отображено 100.
26-01-2012 дата публикации

3-aminoxalyl-aminobenzamide derivatives and insecticidal and miticidal agents containing same as active ingredient

Номер: US20120022263A1
Принадлежит: Agro Kanesho Co Ltd

The present invention herein provides a 3-aminooxalylaminobenzamide derivative which is used as an insecticide or miticide. The 3-aminooxalylaminobenzamide derivative is one represented by the following general formula [1]: (R 1 and R 2 each represent, for instance, a C 1 to C 3 alkoxy group or a C 1 to C 3 haloalkoxy group; R 3 and R 4 each represent, for instance, a C 1 to C 8 alkyl group or a C 1 to C 8 haloalkyl group; R 5 represents, for instance, a C 1 to C 5 haloalkyl group; R 6 and R 7 each represent, for instance, a hydrogen atom or a C 1 to C 5 alkyl group; Y represents, for instance, a hydrogen atom or a halogen atom; Z represents, for instance, a hydrogen atom; n is an integer ranging from 0 to 4 and m is an integer ranging from 0 to 2).

Подробнее
28-06-2012 дата публикации

Amino- and amido-aminotetralin derivatives and related compounds as mu opioid receptor antagonists

Номер: US20120165360A1
Принадлежит: Theravance Inc

The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Подробнее
23-08-2012 дата публикации

New compounds, pharmaceutical compositions and uses thereof

Номер: US20120214785A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Подробнее
31-01-2013 дата публикации

Methods and compounds for the targeted delivery of agents to bone for interaction therewith

Номер: US20130029901A1

Bone targeted compounds and methods are provided. Compounds can include a Bone Targeting Portion (R T ), having an affinity for bone; a Bone Active Portion (R A ) for interacting with and affecting bone; and a Linking Portion (R L ) connecting the Bone Targeting Portion and the Bone Active Portion.

Подробнее
28-03-2013 дата публикации

Lipid Compounds Targeting VLA-4

Номер: US20130079383A1
Принадлежит: ARROWHEAD RESEARCH CORPORATION

The invention relates to the compounds of formula I: 8. A compound of wherein W is hydrogen and Y is methyl.9. A compound of wherein both W and Y are methyl.10. A compound of wherein Ris an alkyl having 9-20 carbon atoms.11. A compound of wherein Ris an alkyl having 16-20 carbon atoms.12. A compound of wherein Ris an alkyl having 18 carbon atoms.13. A compound of wherein Ris an alkyl having 19 carbon atoms.14. A compound of wherein Ris an alkyl having 20 carbon atoms.15. A compound of wherein n is 9-13.16. A compound of selected from the group consisting of:[2,3-bis(dodecyloxy)propyl][3-[[3-[2-[2-[2-[2-[2-[2-[2-[2-[[3-[[2-[1-[[[(S)-1-carboxy-2-[4-(2,6-dichloro-benzoylamino)phenyl]ethyl]amino]carbonyl]cyclopentyl]ethyl]amino]-3-oxopropyl]oxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]-1-oxopropyl]amino]propyl]dimethylaminium trifluoroacetate;[2,3-bis(dodecyloxy)propyl][3-[[4-[[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[[3-[[2-[1-[[[(S)-1-carboxy-2-[4-(2,6-dichloro-benzoylamino)phenyl]ethyl]amino]carbonyl]cyclopentyl]ethyl]amino]-3-oxopropyl]oxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethyl]amino]-1-4-dioxobutyl]amino]propyl]dimethylaminium trifluoroacetate;[[2,3-bis(hexadecyloxy)propyl][3-[[3-[2-[2-[2-[2-[2-[2-[2-[2-[[3-[[2-[1-[[[(S)-1-carboxy-2-[4-(2,6-dichloro-benzoylamino)phenyl]ethyl]amino]carbonyl]cyclopentyl]ethyl]amino]-3-oxopropyl]oxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]-1-oxopropyl]amino]propyl]dimethylaminium trifluoroacetate;[2,3-bis(hexadecyloxy)propyl][3-[[4-[[2-2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[[3-[[2-[1-[[[(S)-1-carboxy-2-[4-(2,6-dichloro-benzoylamino)phenyl]ethyl]amino]carbonyl]cyclopentyl]ethyl]amino]-3-oxopropyl]oxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethyl]amino]-1,4-dioxobutyl]amino]propyl]dimethylaminium trifluoroacetate;(S)-Alpha-[[[1-[2-[[3-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[[4-[[3-[[2,3-bis(hexadecyloxy)propyl]methylamino]propyl]amino]-1,4- ...

Подробнее
16-05-2013 дата публикации

HISTONE ACETYLTRANSFERASE ACTIVATORS AND USES THEREOF

Номер: US20130121919A1

The invention provides for a method for screening compounds that bind to and modulate a histone acetyltransferase protein. The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a HAT-activating compound to a subject. 8. A method for screening compounds of Formula (I) , Formula (II) , Formula (III) , or Formula (V) to treat conditions associated with accumulated amyloid-beta peptide deposits , the method comprising:a) administering a HAT Activator compound of Formula (I), Formula (II), Formula (III), or Formula (V) to an animal model of amyloid-beta peptide deposit accumulation; andb) selecting a HAT Activator compound of Formula (I), Formula (II), Formula (III), or Formula (V) that can modulate histone acetylation after administration of the HAT Activator compound in an animal model of amyloid-beta peptide deposit accumulation.9. A method for identifying a histone acetyltransferase (HAT) activator compound of Formula (I) , Formula (II) , Formula (III) , or Formula (V) to treat conditions associated with accumulated amyloid-beta peptide deposits , wherein the method comprises selecting a HAT Activator compound of Formula (I) , Formula (II) , Formula (III) , or Formula (V) having one or more of the following features:{'sub': '50', 'a) the ECof the compound is no more than about 1000 nM;'}b) the histone acetylation activity in vitro targets histone protein H2, H3, and/or H4; andc) the compound penetrates the blood brain barrier; or a combination thereof.10. The method of claim 9 , wherein the compound has a molecular mass less than about 500 Da claim 9 , has a polar surface area less than about 90 Å claim 9 , has less than 8 hydrogen bonds claim 9 , or a combination thereof claim 9 , in order to penetrate the blood brain barrier.12. The method of claim 11 , wherein the subject ...

Подробнее
16-05-2013 дата публикации

MODULATOR

Номер: US20130123356A1
Принадлежит: UNIVERSITY COLLEGE LONDON

The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, 2. A compound according to wherein Y is selected from CN claim 1 , OH claim 1 , COOR claim 1 , SONRR claim 1 , CONRR claim 1 , where each of Rand Ris independently H or a hydrocarbyl group.3. A compound according to wherein each of R claim 1 , R claim 1 , Rand Ris independently H claim 1 , an alkyl group claim 1 , an aryl group claim 1 , or a cycloalkyl group claim 1 , each of which may be optionally substituted.4. A compound according to wherein Y is selected from OH claim 1 , CN claim 1 , COOR claim 1 , CONRR claim 1 , where each of Rand Ris independently H or an optionally substituted alkyl group.5. A compound according to wherein Y is selected from OH claim 1 , CN claim 1 , COOMe claim 1 , COOH claim 1 , CONH claim 1 , CONHMe and CONMe.6. A compound according to wherein X—Y is selected from{'br': None, 'sub': 2', 'p, '—C≡C—(CH)—Y'}{'br': None, 'sup': 5', '6, 'sub': 2', 'q, '—C(R)═C(R)—(CH)—Y; and'}{'br': None, 'i': 'r', '—C(R5)(R6)C(R8)-(CH2)-Y;'}{'sup': 5', '6', '7', '8, 'wherein each of R, R, R, and Ris independently H or alkyl, and each of p, q and r is independently 2, 3, or 4.'}7. A compound according to wherein X—Y is selected from{'br': None, 'sub': 2', 'p, '—C≡C—(CH)—Y; and'}{'br': None, 'sub': 2', 'q, '—CH═CH—(CH)—Y;'}wherein each of p and q is independently 2, 3 or 4.8. A compound according to wherein X—Y is{'br': None, 'sup': 5', '6, 'sub': 2', 'q, 'i': 'q', 'cis-C(R)═C(R)—(CH)—Y and is 2, 3 or 4.'}9. A compound according to wherein X—Y is —C(Me)-CH—(CH)—Y and r is 2 claim 1 , 3 or 4.10. A compound according to wherein A is phenyl.11. A compound according to wherein Z is ORor NRRand each of Rand Ris independently H claim 1 , an alkyl or a cycloalkyl group claim 1 , each of which may be optionally substituted by one or more OH or halogen groups.12. A compound according to wherein Z is selected from OH claim 1 , OEt claim 1 , NHCHCHF claim 1 , NH- ...

Подробнее
30-05-2013 дата публикации

4-carboxybenzylamino derivatives as histone deacetylase inhibitors

Номер: US20130137690A1
Принадлежит: Individual

The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the 4-carboxybenzylamino derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the 4-carboxybenzylamino derivatives in vivo.

Подробнее
11-07-2013 дата публикации

Cannabinoid receptor modulators

Номер: US20130178457A1
Принадлежит: Lupin Ltd

Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors of Formula (I).

Подробнее
22-08-2013 дата публикации

NASAL FORMULATIONS OF METOCLOPRAMIDE

Номер: US20130213393A1
Принадлежит: Evoke Pharma, Inc.

Nasal formulations of metoclopramide, which remain stable and/or colorless upon storage over a period of time, are provided. Also provided are methods of treating disorders treatable with metoclopramide, comprising administering the nasal solutions to patients in need thereof. 110-. (canceled)11. A pharmaceutical composition comprising metoclopramide , or a pharmaceutically-acceptable salt thereof , a buffer , and benzalkonium chloride; wherein the composition is stable , substantially free of color , and/or substantially clear; and wherein the composition has a pH of above about 4.5.12. The composition of claim 11 , having a starting pH of at least about 4.6.13. The composition of claim 11 , wherein the composition remains stable claim 11 , substantially free of color and/or substantially clear on storage at a temperature of about 25° C. to about 40° C. for at least about 4 weeks claim 11 , at least about 6 weeks claim 11 , at least about 8 weeks claim 11 , at least about 10 weeks or at least about 12 weeks.14. The composition of claim 11 , wherein the buffer is selected from the group consisting of citric acid/phosphate claim 11 , acetate claim 11 , barbital claim 11 , borate claim 11 , Britton-Robinson claim 11 , cacodylate claim 11 , citrate claim 11 , collidine claim 11 , formate claim 11 , maleate claim 11 , McIlvaine claim 11 , phosphate claim 11 , Prideaux-Ward claim 11 , succinate claim 11 , citrate-phosphate-borate (Teorell-Stanhagen) claim 11 , veronal acetate claim 11 , MES (2-(N-morpholino)ethanesulfonic acid) claim 11 , BIS-TRIS (bis(2-hydroxyethyl)iminotris(hydroxymethyl)methane) claim 11 , AD(Original) A (N-(2-acetamido)-2-iminodiacetic acid) claim 11 , ACES (N-(carbamoylmethyl)-2-aminoethanesulfonaic acid) claim 11 , PIPES (piperazine-N claim 11 ,N′-bis(2-ethanesulfonic acid)) claim 11 , MOPSO (3-(N-morpholino)-2-hydroxypropanesulfonic acid) claim 11 , BIS-TRIS PROPANE (1 claim 11 ,3-bis(tris(hydroxymethyl)methylamino)propane) claim 11 , BES (N ...

Подробнее
05-09-2013 дата публикации

USE OF SQUARAMIDE IN THE PREVENTION AND/OR TREATMENT OF ROSACEA

Номер: US20130231393A1
Автор: AUBERT Jérôme
Принадлежит: GALDERMA RESEARCH & DEVELOPMENT

A compound of formula (I): 2. The compound of claim 1 , wherein R6 and R7 are joined together to form a 6 membered heterocycloalkyl ring claim 1 , that is substituted with one heteroatom.3. The compound of claim 2 , wherein the heteroatom is an oxygen.7. The compound of claim 1 , wherein the compound of formula (I) is selected from the group consisting of:1:2-Hydroxy-N,N-dimethyl-3-{2-[(R)-1-(5-methyl-furan-2-yl)-propylamino]-3,4-dioxo-cyclobut-1-enylamino}-benzamide;2:2-Hydroxy-N,N-dimethyl-3-{2-[(4-methyl-furan-2-ylmethyl)-amino]-3,4-dioxo-cyclobut-1-enylamino}benzamide;3:2-Hydroxy-N,N-dimethyl-3-{2-[(4-isopropyl-furan-2-ylmethyl)-amino]-3,4-dioxo-cyclobut-1-enylamino}-benzamide;4:3-{2-[(R)-1-(4-Ethyl-furan-2-yl)-ethylamino]-3,4-dioxo-cyclobut-1-enylamino}-2-hydroxy-N,N-dimethyl-benzamide;5:3-{2-[(R)-1-(4-Ethyl-furan-2-yl)-ethylamino]-3,4-dioxo-cyclobut-1-enylamino}-2-hydroxy-N,N-dimethyl-benzamide;6:3-[2-((R)-1-Furan-2-yl-ethylamino)-3,4-dioxo-cyclobut-1-enylamino]-2-hydroxy-N,N-dimethyl-benzamide;7:3-[3,4-Dioxo-2-((R)-1-phenyl-ethylamino)-cyclobut-1-enylamino]-2-hydroxy-N,N-dimethyl-benzamide;8:3-[3,4-Dioxo-2-((R)-1-phenyl-ethylamino)-cyclobut-1-enylamino]-2-hydroxy-N,N-dimethyl-benzamide;9:3-[3,4-Dioxo-2-((R)-1-phenyl-propylamino)-cyclobut-1-enylamino]-2-hydroxy-N,N-dimethyl-benzamide;10:3-[3,4-Dioxo-2-((R)-1-pyridin-2-yl-propylamino)-cyclobut-1-enylamino]-2-hydroxy-N,N-dimethyl-benzamide;11:3-[3,4-Dioxo-2-((R)-1-pyridin-3-yl-propylamino)-cyclobut-1-enylamino]-2-hydroxy-N,N-dimethyl-benzamide;12:3-[3,4-Dioxo-2-((R)-1-pyridin-4-yl-propylamino)-cyclobut-1-enylamino]-2-hydroxy-N,N-dimethyl-benzamide;13:3-(2-Hydroxy-phenylamino)-4-((R)-1-phenyl-propylamino)-cyclobut-3-ene-1,2- dione;14:3-(5-Fluoro-2-hydroxy-phenylamino)-4-((R)-1-phenyl-propylamino)-cyclobut-3-ene-1,2-dione;15:3-(4-Fluoro-2-hydroxy-phenylamino)-4-((R)-1-phenyl-propylamino)-cyclobut-3-ene-1,2-dione;16:3-[3,4-Dioxo-2-((R)-1-phenyl-propylamino)-cyclobut-1-enylamino]-N,N-diethyl-2-hydroxy-benzamide;17:3 ...

Подробнее
21-11-2013 дата публикации

Amide derivative, pest control agent containing the amide derivative, and use of the amide derivative

Номер: US20130310459A1
Принадлежит: Mitsui Chemicals Agro 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. In the following Formula (1), A represents a carbon atom, a nitrogen atom, or the like, and K represents a non-metal atomic group necessary for forming a cyclic linking group derived from benzene or a heterocyclic. X represents a halogen atom or the like; n represents an integer of from 0 to 4. R 1 and R 2 represent hydrogen atoms, alkyl groups, or the like. T represents —C(=G 1 )-Q 1 or —C(=G 1 )-G 2 Q 2 , and G 1 to G 3 each represent oxygen atoms or the like. Q 1 and Q 2 each represent a hydrogen atom, an alkyl group, an aryl group, or the like. Y 1 and Y 5 each represent a halogen atom or the like, Y 2 and Y 4 each represent a hydrogen atom or the like, and Y 3 represents a C2-C5 haloalkyl group.

Подробнее
26-12-2013 дата публикации

Substituted tetracycline compounds for treatment of inflammatory skin disorders

Номер: US20130345179A1
Принадлежит: PARATEK PHARMACEUTICALS, INC.

Methods and compositions for the treatment of skin disorders (e.g., acne, rosacea) are described. 1160-. (canceled)1631. The method according to claim , wherein the amount of substituted tetracycline compound administered to the subject is in a range of from 0.01 to 100 milligrams per kilogram of body weight of the subject.1642. The method according to claim , wherein the amount of substituted tetracycline compound administered to the subject is in a range of from 0.01 to 100 milligrams per kilogram of body weight of the subject.1651. The method according to claim , wherein the amount of substituted tetracycline compound administered to the subject is in a range of from 0.1 to 50 milligrams per kilogram of body weight of the subject.1662. The method according to claim , wherein the amount of substituted tetracycline compound administered to the subject is in a range of from 0.1 to 50 milligrams per kilogram of body weight of the subject.1671. The method according to claim , wherein the amount of substituted tetracycline compound administered to the subject is in a range of from 1 to 20 milligrams per kilogram of body weight of the subject.1682. The method according to claim , wherein the amount of substituted tetracycline compound administered to the subject is in a range of from 1 to 20 milligrams per kilogram of body weight of the subject.1691. The method according to claim , wherein the subject is a human.1702. The method according to claim , wherein the subject is a human. This application claims priority to U.S. Provisional Patent Application No. 60/876,434, filed Dec. 21, 2006. The contents of the foregoing application are hereby incorporated in their entirety.Acne is a disorder resulting from the actions of hormones on the sebaceous glands, which leads to plugged pores and outbreaks of lesions, commonly called pimples. Nearly 17 million people in the United States have acne, making it the most common skin disease. Severe acne can lead to disfiguring, ...

Подробнее
02-01-2014 дата публикации

COMPOUNDS AND COMPOSITIONS FOR USE AS MODULATORS OF TAU AGGREGATION AND ALLEVIATION OF TAUOPATHIES

Номер: US20140005240A1
Принадлежит:

This invention relates to the use of bis- and tris-dihydroxyaryl compounds as well as sulfonamides, heteroaryls, tricycloalkyl and their analogs and pharmaceutically acceptable salts, for modulating tau aggregation and alleviating tauopathies, such as Alzheimer's disease (AD), Pick's disease (PiD), progressive supranuclear palsy (PSP), corticobasal degeneration (CBD) and familial frontotemporal dementia/Parkinsonism linked to chromosome 17 (FTDP-17), amyotrophic lateral sclerosis/Parkinsonism-dementia complex, argyrophilic grain dementia, dementia pugilistic, diffuse neurofibrillary tangles with calcification, progressive subcortical gliosis and tangle only dementia. 2. The method of claim 1 , wherein the mammal is a human.3. The method of claim 1 , wherein the amount of the compound administered is between 0.1 mg/Kg/day and 1000 mg/Kg/day.4. The method of claim 1 , wherein the amount of compound administered is between 1 mg/Kg/day and 100 mg/Kg/day.5. The method of claim 1 , wherein the amount of compound administered is between 10 mg/Kg/day and 100 mg/Kg/day.6. The method of claim 1 , wherein the tauopathy is selected from the group consisting of Alzheimer's disease claim 1 , Pick's disease claim 1 , progressive supranuclear palsy claim 1 , corticobasal degeneration claim 1 , familial frontotemporal dementia/Parkinsonism linked to chromosome 17 claim 1 , amyotrophic lateral sclerosis/Parkinsonism-dementia complex claim 1 , argyrophilic grain dementia claim 1 , dementia pugilistic claim 1 , diffuse neurofibrillary tangles with calcification claim 1 , progressive subcortical gliosis and tangle only dementia.7. The method of wherein the compound administered is administered by one of routes selected from claim 1 , oral claim 1 , topical claim 1 , systemic or parenteral.8. A method of disrupting or causing the dissolution of tau aggregates in a mammal suffering from a tauopathy claim 1 , comprising administering to the mammal suffering from a tauopathy an effective ...

Подробнее
06-02-2014 дата публикации

NOVEL DRUG TARGET SITE WITHIN GP120 OF HIV

Номер: US20140038168A1
Принадлежит: KFLP BIOTECH, LLC

The present invention relates to a method of designing an inhibitor of the binding of HIV (human immunodeficiency virus) glycoprotein (gp)120 to a CD4-receptor or to the integrin alpha4 beta7 (a4b7). The inhibitor interacts with at least two amino acid residues comprised in six motifs within the 3-dimensional structure of gp120. Also provided are compounds, pharmaceutical compositions thereof and uses thereof in the development of an inhibitor of the binding of a HIV gp120 to a CD4-receptor or an integrin alpha4 beta7 (a4b7). The inhibitors are useful for the prevention or treatment of an HIV infection and/or diseases associated with an HIV infection. 1. A method of designing an inhibitor of the binding of HIV (human immunodeficiency virus) glycoprotein (gp)120 to a CD4-receptor or to the integrin alpha4 beta7 (a4b7) , the method comprising the molecular modelling of a compound such that the modelled compound interacts in silico with at least two amino acid residues comprised in six motifs within the 3-dimensional structure of said gp120 of HIV or within a peptidomimetic reflecting the 3-dimensional structure of said gp120 of HIV , wherein said interaction between said at least two amino acid residues and said compound is characterized by an interatomic distance of less than 8 Angströms ,wherein a first motif of said six motifs comprises the amino acid sequence DIISLWDQSLKPCVKLT (SEQ ID NOS 3 or 9) or a variant thereof;wherein a second motif of said six motifs comprises the amino acid sequence NVSTVQCTHGIRPVVSTQLLLNGSLAE (SEQ ID NOS 4 or 10) or a variant thereof;wherein a third motif of said six motifs comprises the amino acid sequence SGGDPEIVMHSFNCGGEFFYCN (SEQ ID NOS 5 or 11) or a variant thereof;wherein a fourth motif of said six motifs comprises the amino acid sequence CPKISFEP (SEQ ID NOS 6 or 14) or a variant thereof;wherein a fifth motif of said six motifs comprises the amino acid sequence FRPGGGDMRDNWSELYKYKVV (SEQ ID NO: 7) or a variant thereof; andwherein ...

Подробнее
13-02-2014 дата публикации

Prolyl hydroxylase inhibitors and methods of use

Номер: US20140045899A1
Принадлежит: Akebia Therapeutics Inc

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.

Подробнее
20-02-2014 дата публикации

POLYCATIONIC COMPOUNDS AND USES THEREOF

Номер: US20140051762A1
Автор: Liu Dahui, Mousa Shaker
Принадлежит:

Aspects of the present invention relate to compounds and methods useful in modulating angiogenesis and methods of treating or preventing diseases associated with angiogenesis by administering a polycationic compound. The present invention relates to methods of use and compositions for inhibiting angiogenesis-mediated disorders in mammals including animals and humans. Additionally, this invention relates to the combined use of polycations with other anti-angiogenesis agents for the treatment of different angiogenesis-mediated disorders. Additionally, those polycationic compounds can be used with various anti-inflammatory and cytotoxic agents as well as with radio-therapeutic agents in cancer patients to prevent and treat tumor growth and metastasis. 1. A compound for inhibiting angiogenesis comprising a therapeutically effective amount of a polycationic compound.2. The compound of claim 1 , wherein said polycationic compound is an arylamide.6. The compound of claim 1 , wherein said polycationic compound is a hydrazide.8. The compound of claim 6 , wherein said hydrazide is:9. The compound of claim 1 , wherein said polycationic compound is a calixrene.12. The compound of claim 1 , wherein said polycationic compound is a salicylamide.16. A method of inhibiting angiogenesis in an animal in need thereof comprising administering to said animal a therapeutically effective amount of an polycationic compound.17. The method of claim 16 , wherein said polycationic compound is an arylamide.18. The method of claim 16 , wherein said polycationic compound is a hydrazide.19. The method of claim 16 , wherein said polycationic compound is a calixrene.20. The method of claim 16 , wherein said polycationic compound is a salicylamide.21. A method of treating or preventing a disease or disorder associated with angiogenesis in an animal in need thereof comprising administering to said animal a therapeutically effective amount of a polycationic compound.22. The method of claim 21 , wherein ...

Подробнее
13-03-2014 дата публикации

Benzamide derivatives as p2x7 receptor antagonists

Номер: US20140073651A1
Принадлежит: ACTELION PHARMACEUTICALS LTD

The invention relates to benzamide derivatives of formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , n and Y are as defined in the description, their preparation and their use as pharmaceutically active compounds.

Подробнее
04-01-2018 дата публикации

Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto

Номер: US20180000087A1
Принадлежит: DOW AGROSCIENCES LLC

This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”). 2. A molecule according to claim 1 , wherein Ris selected from the group consisting of H and Cl.3. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , Cl claim 1 , Br claim 1 , CH claim 1 , and CF.4. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , F claim 1 , Cl claim 1 , CH claim 1 , CF claim 1 , and OCF.5. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , CH claim 1 , and CF.6. A molecule according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare H.7. A molecule according to claim 1 , wherein Ris Cl.8. A molecule according to claim 1 , wherein Ris Cl.9. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , Cl claim 1 , and CF.10. A molecule according to claim 1 , wherein Ris selected from the group consisting of H and CH.11. A molecule according to claim 1 , wherein Ris selected from the group consisting of cyclopropyl claim 1 , cyclobutyl claim 1 , cyclopentyl claim 1 , cyclohexyl claim 1 , azetidinyl claim 1 , morpholinyl claim 1 , oxetanyl claim 1 , pyranyl claim 1 , tetrahydrothiophenyl claim 1 , thietanyl claim 1 , thietanyl-oxide claim 1 , and thietanyl-dioxide claim 1 ,{'sub': 3', '3', '3, 'wherein each cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, ...

Подробнее
05-01-2017 дата публикации

INSECTICIDAL COMPOUNDS

Номер: US20170000120A1
Принадлежит: SYNGENTA PARTICIPATIONS AG

The present invention relates to novel triazole derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests (I) wherein Y, X, X 2 and Q are as defined in claim ; or salts thereof. 3. A compound of formula (I) according to wherein{'sub': '1', 'Xis hydrogen, fluorine or methoxy'}{'sub': 2', '2', '1, 'Xis hydrogen or cyano, with the condition that if Xis cyano, then Xis hydrogen,'}R is hydrogen, methyl or ethyl.4. A compound of formula (I) according to wherein{'sub': 1', '2, 'Xis methoxy and Xis hydrogen.'}5. A compound of formula (I) according to wherein{'sub': 2', '1, 'Xis cyano and Xis hydrogen.'}7. A method of controlling insects claim 1 , acarines claim 1 , nematodes or molluscs which comprises applying to a pest claim 1 , to a locus of a pest claim 1 , or to a plant susceptible to attack by a pest an insecticidally claim 1 , acaricidally claim 1 , nematicidally or molluscicidally effective amount of a compound of formula (I) as defined in .8. An insecticidal claim 1 , acaricidal claim 1 , nematicidal or molluscicidal composition comprising an insecticidally claim 1 , acaricidally claim 1 , nematicidally or molluscicidally effective amount of a compound of formula (I) as defined in together with an agrochemically acceptable diluent or carrier.9. A composition according to which further comprises one or more additional insecticidal claim 8 , acaricidal claim 8 , nematicidal or molluscicidal compounds.10. A method of protecting useful plants from insects claim 1 , acarines claim 1 , nematodes or molluscs claim 1 , comprising applying to said plants claim 1 , to the locus thereof claim 1 , or to plant propagation material thereof claim 1 , an insecticidally claim 1 , acaricidally claim 1 , nematicidally or molluscicidally effective amount of ...

Подробнее
07-01-2016 дата публикации

AMIDE DERIVATIVES, PROCESS FOR PREPARATION THEREOF AND USE THEREOF AS INSECTICIDE

Номер: US20160002198A1
Принадлежит:

An object of the present invention is to provide a compound represented by Formula (1): 114-. (canceled) The present invention relates to a compound represented by Formula (1):wherein A, A, Aand Aeach represent a carbon atom, a nitrogen atom or an oxidized nitrogen atom;Rand Reach represent a hydrogen atom, an optionally substituted alkyl group or an optionally substituted C1-C4 alkylcarbonyl group;Gand Geach represent an oxygen atom or a sulfur atom;X, which may be identical or different, represents a hydrogen atom, a halogen atom, a C1-C3 alkyl group or a trifluoromethyl group;n is an integer of 0 to 4; andQand Qeach represent an optionally substituted phenyl group, an optionally substituted naphthyl group or an optionally substituted heterocyclic group,an insecticide comprising the compound as the active ingredient, and a process for preparation thereof and use thereof.International Publication WO 2000/55120 and U.S. Pat. No. 6,548,514 describe a compound similar to the compound of the present invention for the use as medicament, but they do not describe on the insecticidal activity of the compound. The compound clearly does not fall within the scope of claims of the present invention.International Publication WO 2000/7980 describes a compound similar to the compound of the present invention for the use as medicament, but it does not describe on the insecticidal activity of the compound. The compound clearly does not fall within the scope of claims of the present invention.US Patent Laid-Open No. 2002-032238 describes a compound similar to the compound of the present invention for the use as medicament, but it does not describe on the insecticidal activity of the compound. The compound clearly does not fall within the scope of claims of the present invention.The object of the present invention is to provide a pesticide having a high insecticidal efficacy. Another object of the present invention is to provide a compound represented by Formula (1), a process for ...

Подробнее
05-01-2017 дата публикации

COMPOUND, POLY(IMIDE-AMIDE) COPOLYMER, AND AN ARTICLE INCLUDING THE POLY(IMIDE-AMIDE) COPOLYMER

Номер: US20170001951A1
Принадлежит:

A compound represented by Chemical Formula 1: 2. The compound according to claim 1 , wherein Rand Rare the same or different claim 1 , and are each independently —CF claim 1 , —CCl claim 1 , —CBr claim 1 , —Cl claim 1 , —CF claim 1 , —CF claim 1 , —COOH claim 1 , —COOMe claim 1 , —COOEt claim 1 , —OMe claim 1 , —OEt claim 1 , —SF claim 1 , —F claim 1 , —Cl claim 1 , or —Br.3. The compound according to claim 1 , wherein both Rand Rare —CF claim 1 , and Rto Rare all hydrogens.5. The poly(imide-amide) copolymer according to claim 4 , wherein in Chemical Formula 9 claim 4 , Rand Rare the same or different claim 4 , and are each independently —CF claim 4 , —CCl claim 4 , —CBr claim 4 , —Cl claim 4 , —CF claim 4 , —CF claim 4 , —COOH claim 4 , —COOMe claim 4 , —COOEt claim 4 , —OMe claim 4 , —OEt claim 4 , —SF claim 4 , —F claim 4 , —Cl claim 4 , or —Br.6. The poly(imide-amide) copolymer according to claim 4 , wherein in Chemical Formula 8 claim 4 , 0.01≦x≦0.10.9. The poly(imide-amide) copolymer according to claim 4 , wherein in Chemical Formula 3-1 claim 4 , Rand Rare the same or different claim 4 , and are each independently selected from —CF claim 4 , —CCl claim 4 , —CBr claim 4 , —Cl claim 4 , —NO claim 4 , —CN claim 4 , —C(═O)CH claim 4 , and —COCH.10. The poly(imide-amide) copolymer according to claim 4 , wherein in Chemical Formula 4-1 claim 4 , Ris SO claim 4 , and both n9 and n10 are the integers of 0.11. An article comprising the poly(imide-amide) copolymer according to .12. An optical device comprising the article according to . This application is a division of U.S. patent application Ser. No. 14/341,981 which claims priority to Korean Patent Application No. 10-2013-0144124, filed on Nov. 25, 2013, and all the benefits accruing therefrom under 35 U.S.C. §119, the content of which are incorporated herein in their entirety by reference.1. FieldThis disclosure relates to a new compound, a poly(imide-amide) copolymer prepared using the new compound, and an article ...

Подробнее
02-01-2020 дата публикации

DUAL MECHANISM INHIBITORS FOR THE TREATMENT OF DISEASE

Номер: US20200002324A1
Принадлежит:

Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved. 121-. (canceled)23. A composition claim 22 , comprising the compound of .24. A pharmaceutical composition claim 22 , comprising the compound of and a pharmaceutically acceptable carrier.25. The pharmaceutical composition of claim 24 , wherein the pharmaceutically acceptable carrier is saline buffered to a pH of about 5.5 to about 6.5.26. A method of treating an eye disease in a subject in need thereof claim 22 , comprising administering to the subject an effective amount of the compound of .27. The method of claim 26 , wherein the eye disease comprises glaucoma.28. The method of claim 26 , wherein the eye disease comprises wet age-related macular degeneration claim 26 , dry age-related macular degeneration claim 26 , or diabetic macular edema.29. The method of claim 26 , wherein the eye disease comprises dry eye.30. The method of claim 26 , wherein the eye disease comprises ocular hypertension.31. The method of claim 26 , wherein the administration is topical administration to an eye of the subject.32. A method of treating an eye disease in a subject in need thereof claim 23 , comprising administering to the subject an effective amount of the composition of .33. The method of claim 32 , wherein the eye disease comprises glaucoma.34. The method of claim 32 , wherein the eye disease comprises wet age-related macular degeneration claim 32 , dry age-related macular degeneration claim 32 , or diabetic macular edema.35. The method of claim 32 , wherein the eye disease comprises dry eye.36. ...

Подробнее
01-01-2015 дата публикации

COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES

Номер: US20150005320A9
Принадлежит: Synta Pharmaceuticals Corp.

The invention relates to compounds of formula (I): 187-. (canceled)89. The compound of claim 88 , wherein Ais CH.90. (canceled)91. The compound of claim 88 , wherein Yis a substituted phenyl claim 88 , an optionally substituted pyridyl claim 88 , or an optionally substituted [1 claim 88 ,2 claim 88 ,3]-thiadiazolyl.92. The compound of claim 88 , wherein Yis a substituted phenyl.94. (canceled)95. A compound selected from the group consisting of:3-Fluoro-N-(2′-trifluoromethyl-biphenyl-4-yl)-isonicotinamide;3-Fluoro-N-(2′-methyl-biphenyl-4-yl)-isonicotinamide;3-Fluoro-N-(3′-trifluoromethyl-biphenyl-4-yl)-isonicotinamide;N-(2′-Trifluoromethyl-biphenyl-4-yl)-nicotinamide;N-(2′-Trifluoromethyl-biphenyl-4-yl)-isonicotinamide;4-Trifluoromethyl-N-(2′-trifluoromethyl-biphenyl-4-yl)-nicotinamide;Pyridine-2-carboxylic acid (2′-trifluoromethyl-biphenyl-4-yl)-amide;Pyrazine-2-carboxylic acid (2′-trifluoromethyl-biphenyl-4-yl)-amide;2-methyl-pyridine-3-carboxylic acid (2′,5′-bis-trifluoromethyl-biphenyl-4-yl)-amide;1-methyl-1H-imidazole-5-carboxylic acid (2′,5′-bis-trifluoromethyl-biphenyl-4-yl)-amide;3-methyl-pyridine-4-carboxylic acid (2′,5′-dimethoxy-biphenyl-4-yl)-amide;3-methyl-pyridine-4-carboxylic acid (2′,5′-bis-trifluoromethyl-biphenyl-4-yl)-amide;3-methyl-pyridine-4-carboxylic acid (2′-methoxy-5′-chlorobiphenyl-4-yl)-amide;3-fluoro-pyridine-4-carboxylic acid (2′,5′-dimethoxybiphenyl-4-yl)-amide;3-fluoro-pyridine-4-carboxylic acid (2′-methoxy-5′-chlorobiphenyl-4-yl)-amide;3-fluoro-pyridine-4-carboxylic acid (2′,5′-bis-trifluoromethylbiphenyl-4-yl)-amide;3-methyl-pyridine-4-carboxylic acid (2′-methoxy-5′-methylbiphenyl-4-yl)-amide;3-methyl-pyridine-4-carboxylic acid (2′,5′-dimethylbiphenyl-4-yl)-amide;4-methyl-[1,2,3]-thiadiazole-5-carboxylic acid (2′-methoxy-5′-acetylbiphenyl-4-yl)-amide;3-fluoro-pyridine-4-carboxylic acid (2′-difluoromethoxy-5′-chlorobiphenyl-4-yl)-amide;4-methyl-[1,2,3]-thiadiazole-5-carboxylic acid {2′-(N,N-dimethylamino)-5′-trifluoromethoxybiphenyl-4- ...

Подробнее
11-01-2018 дата публикации

Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto

Номер: US20180007911A1
Принадлежит: DOW AGROSCIENCES LLC

This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”). 2. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , F claim 1 , and Cl.3. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , F claim 1 , and Cl.4. A molecule according to claim 1 , wherein Ris F or Cl.5. A molecule according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare each independently H.6. A molecule according to claim 1 , wherein Ris selected from the group consisting of Cl and Br.7. A molecule according to claim 1 , wherein Ris selected from the group consisting of Cl and Br.8. A molecule according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , Cl claim 1 , and CF.9. A molecule according to claim 1 , wherein Ris selected from the group consisting of H and CH.10. A molecule according to claim 1 , wherein Ris selected from the group consisting of CH claim 1 , CHCH claim 1 , CHCHCH claim 1 , CHCHCHCH claim 1 , CHCHCHOCHCH claim 1 , CH claim 1 , CHCH claim 1 , CHCHCH claim 1 , CHCHCHCH claim 1 , CHCHCHCHCH claim 1 , CHCHCHCHCHCH claim 1 , CHCH(CH) claim 1 , CHcyclopropyl claim 1 , CHCHcyclopropyl claim 1 , CHcyclobutyl claim 1 , CHphenyl claim 1 , CHCHphenyl claim 1 , CHC═CH claim 1 , CHC═CH claim 1 , CHCF claim 1 , CHCHF claim 1 , CHCHCF claim 1 , CHCFCF claim 1 , CHCHCHCF claim 1 , CHCHCFCF claim 1 , CHCFCFCF claim 1 , CHCHCHCHF claim 1 , CHCHSCH ...

Подробнее
11-01-2018 дата публикации

THERAPEUTIC COMPOUNDS AND USES THEREOF

Номер: US20180009735A1
Принадлежит:

Provided herein are compounds of formula I: 23-. (canceled)4. The compound of claim 1 , wherein X is —CH— claim 1 , —CHCH— or —CHCHCH—.79-. (canceled)11. The compound of claim 1 , wherein X is or —N(R)C(R)—.1214-. (canceled)15. The compound of claim 1 , wherein Ris hydrogen claim 1 , halo claim 1 , heteroaryl claim 1 , —OR claim 1 , CN claim 1 , —C(O)—N(R)or —C(O)—OR claim 1 , wherein any heteroaryl of Ris optionally substituted with one or more Rgroups.1618-. (canceled)2022-. (canceled)2425-. (canceled)27. (canceled)2933-. (canceled)36. (canceled)40. (canceled)42. (canceled)43. A method of treating cancer in an animal comprising administering to the animal in need thereof a compound of formula I or a pharmaceutically acceptable salt thereof as described in .44. A method of treating an LSD1-mediated disorder in an animal comprising administering to the animal in need thereof a compound of formula I or a pharmaceutically acceptable salt thereof as described in .4549-. (canceled)50. A method of increasing efficacy of a cancer treatment comprising a cytotoxic agent in an animal comprising administering to the animal an effective amount of a compound of formula I or a pharmaceutically acceptable salt thereof as described in .51. (canceled)52. A method of delaying or preventing development of cancer resistance to a cytotoxic agent in an animal claim 1 , comprising administering to the animal a compound of formula I or a pharmaceutically acceptable salt thereof as described in .53. A method of extending the duration of response to a cancer therapy in an animal claim 1 , comprising administering to the animal undergoing the cancer therapy a compound of formula I or a pharmaceutically acceptable salt thereof claim 1 , as described in claim 1 , wherein the duration of response to the cancer therapy when the compound of formula I is administered is extended over the duration of response to the cancer therapy in the absence of the administration of the compound of formula I or ...

Подробнее
03-02-2022 дата публикации

Anionic-cationic-nonionic surfactant, production and use thereof

Номер: US20220033705A1

An anionic-cationic-nonionic surfactant as substantially represented by the formula (I) exhibits significantly improved interfacial activity and stability as compared with the prior art. With the present anionic-cationic-nonionic surfactant, a flooding fluid composition for tertiary oil recovery with improved oil displacement efficiency and oil washing capability as compared with the prior art could be produced. In the formula (I), each group is as defined in the specification.

Подробнее
18-01-2018 дата публикации

CYCLIC PROTEIN TYROSINE KINASE INHIBITORS

Номер: US20180016247A1
Принадлежит:

Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders. 2. A compound of claim 1 , wherein Ris hydrogen.3. A compound of claim 1 , wherein Ris hydrogen.4. A compound of claim 1 , wherein Ris hydrogen.69. A compound of claim claim 1 , wherein Ris aryl which is unsubstituted or independently substituted with one or more alkyl or halo.7. A pharmaceutical composition claim 1 , comprising a pharmaceutically acceptable vehicle ordiluent and at least one compound of .8. A pharmaceutical composition claim 8 , comprising a pharmaceutically acceptable vehicle ordiluent and at least one compound of . This application is a continuation of Ser. No. 15/163,750 filed May 25, 2016, now allowed, which is a continuation of Ser. No. 14/620,244, filed Feb. 12, 2015, now U.S. Pat. No. 9,382,219, which is a continuation of Ser. No. 14/226,868, filed Mar. 27, 2014, now U.S. Pat. No. 8,993,567, which is a continuation of Ser. No. 11/271,626, filed Nov. 10, 2005, now U.S. Pat. No. 8,716,323, which is a continuation of application Ser. No. 10/378,373 filed Mar. 3, 2003, which is a continuation of application Ser. No. 09/548,929 filed Apr. 13, 2000, now U.S. Pat. No. 6,596,746, which claims priority from provisional application No. 60/129,510 filed Apr. 15, 1999. The entire disclosure of each of the foregoing applications is herein incorporated by reference in its entirety.The present invention relates to cyclic compounds and salts thereof, to methods of using such compounds in treating protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders, and to pharmaceutical compositions containing such compounds.Protein tyrosine kinases (PTKs) are enzymes which, in conjuction with ATP as a substrate, phosphorylate tyrosine residues in peptides and proteins. These enzymes are key ...

Подробнее
28-01-2016 дата публикации

PPAR AGONISTS

Номер: US20160023991A1
Принадлежит:

Provided herein are compounds and compositions useful in increasing PPARδ activity. The compounds and compositions provided herein are useful for the treatment of PPARδ related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases). 2. The compound of claim 1 , wherein ring B is selected from phenyl claim 1 , pyridine claim 1 , thiophene claim 1 , thiazole claim 1 , pyrazole claim 1 , oxazole claim 1 , isoxazole claim 1 , benzo[b]furan claim 1 , indazole claim 1 , piperidine claim 1 , cyclohexane claim 1 , piperidin-2-one claim 1 , piperazine-2 claim 1 ,5-dione or quinazolin-4(3H)-one.6. The compound of claim 1 , wherein:{'sup': '3', 'Ris selected from aliphatic or alkyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; and/or'}{'sup': 2', '3', '4, 'L, Land Lare each independently selected from a bond or alkylene.'}7. The compound of claim 1 , wherein LRis isopropyl.8. The compound of claim 1 , wherein Ris furan-2-yl or furan-3-yl.11. The compound of claim 1 , wherein the compound is selected from6-(2-((N-isopropyl-[1,1′-biphenyl]-4-carboxamido)methyl)phenoxy)hexanoic acid;ethyl 6-(2-(1-(4-bromo-N-cyclopropylbenzamido)-2-(tert-butylamino)-2-oxoethyl)phenoxy)hexanoate;ethyl 6-(2-(2-(tert-butylamino)-1-(N-cyclopropyl-[1,1′-biphenyl]-4-carboxamido)-2-oxoethyl)phenoxy)hexanoate;ethyl 6-(2-(2-amino-1-(N-cyclopropyl-[1,1′-biphenyl]-4-carboxamido)-2-oxoethyl)phenoxy)hexanoate;6-(2-(2-amino-1-(N-cyclopropyl-[1,1′-biphenyl]-4-carboxamido)-2-oxoethyl)phenoxy)hexanoic acid;6-(2-(2-(tert-butylamino)-1-(N-cyclopropyl-[1,1′-biphenyl]-4-carboxamido)-2-oxoethyl)phenoxy)hexanoic acid;6-(2-((N-cyclopropyl-[1,1′-biphenyl]-4-carboxamido)methyl)phenoxy)hexanoic acid;N-(2-amino-1-(2-((6-(hydroxyamino)-6-oxohexyl)oxy)phenyl)-2-oxoethyl)-N-cyclopropyl-[1,1′-biphenyl]-4-carboxamide;6-(2-((N-cyclopropyl-4-(pyridin-4-yl)benzamido)methyl)phenoxy)hexanoic acid;6-(2-((N-cyclopropyl-4-(pyridin-3-yl)benzamido)methyl)phenoxy)hexanoic acid;6 ...

Подробнее
22-01-2015 дата публикации

HIF INHIBITORS AND USE THEREOF

Номер: US20150023868A1
Принадлежит: The General Hospital Corporation

The present invention is directed to HIF inhibitors and methods of preventing cell proliferation, reducing inflammation, and treating an angiogenic disease or disorders. 3. The method of claim 1 , wherein said contacting is in vivo.4. The method of claim 2 , wherein said contacting is in vivo.5. (canceled)6. (canceled)7. The method of claim 4 , wherein in vivo contacting is in a human.8. The method of claim 4 , wherein in vivo contacting is in a subject in need of treatment or prevention of a HIF related pathology.9. (canceled)11. The method of claim 10 , comprising pulsed or sustained release administration of said HIF inhibitor claim 10 , wherein pulse administration is administration of a single therapeutic dose in 5-30 individual doses.12. The method of claim 11 , wherein interval between individual pulse doses is 24 hours or greater.13. The method of claim 11 , wherein a single therapeutic dose occurs in about 5 to about 10 pulses or greater than 20 pulses.14. (canceled)15. (canceled)16. The method of claim 10 , comprising co-administering a second therapeutic agent selected from the group consisting of: an antibody claim 10 , antibiotic claim 10 , anti-inflammatory claim 10 , anti-oxidant claim 10 , analgesic claim 10 , radioisotope claim 10 , noscapine claim 10 , paclitaxel claim 10 , nocodazole claim 10 , buslfulan claim 10 , lomustine (CCNU) claim 10 , caboplatinum claim 10 , cisplatinum claim 10 , cytoxan claim 10 , daunorubicin claim 10 , dacarbazine (DTIC) claim 10 , 5-fluorouracil (5-FU) claim 10 , fludarabine claim 10 , hydroxyurea claim 10 , idarubicin claim 10 , ifosfamide claim 10 , methotrextrate claim 10 , mithramycin claim 10 , mitomycin claim 10 , mitoxantrone claim 10 , nitrogen mustard claim 10 , vinblastine claim 10 , vincristine claim 10 , CPT-11 claim 10 , cladribine claim 10 , vinorebne tartrate claim 10 , rituximab claim 10 , STI-571 claim 10 , docetaxel claim 10 , temozolomide claim 10 , topotecan claim 10 , capecitaine claim 10 , ...

Подробнее
17-04-2014 дата публикации

COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES

Номер: US20140107134A1
Принадлежит: Synta Pharmaceuticals Corp.

The invention relates to compounds of formula (I): 187-. (canceled)89. The compound of claim 88 , wherein Ais CH.90. (canceled)91. The compound of claim 88 , wherein Yis a substituted phenyl claim 88 , an optionally substituted pyridyl claim 88 , or an optionally substituted [1 claim 88 ,2 claim 88 ,3]-thiadiazolyl.92. The compound of claim 88 , wherein Yis a substituted phenyl.94. (canceled)95. A compound selected from the group consisting of:3-Fluoro-N-(2′-trifluoromethyl-biphenyl-4-yl)-isonicotinamide;3-Fluoro-N-(2′-methyl-biphenyl-4-yl)-isonicotinamide;3-Fluoro-N-(3′-trifluoromethyl-biphenyl-4-yl)-isonicotinamide;N-(2′-Trifluoromethyl-biphenyl-4-yl)-nicotinamide;N-(2′-Trifluoromethyl-biphenyl-4-yl)-isonicotinamide;4-Trifluoromethyl-N-(2′-trifluoromethyl-biphenyl-4-yl)-nicotinamide;Pyridine-2-carboxylic acid (2′-trifluoromethyl-biphenyl-4-yl)-amide;Pyrazine-2-carboxylic acid (2′-trifluoromethyl-biphenyl-4-yl)-amide;2-methyl-pyridine-3-carboxylic acid (2′,5′-bis-trifluoromethyl-biphenyl-4-yl)-amide;1-methyl-1H-imidazole-5-carboxylic acid (2′,5′-bis-trifluoromethyl-biphenyl-4-yl)-amide;3-methyl-pyridine-4-carboxylic acid (2′,5′-dimethoxy-biphenyl-4-yl)-amide;3-methyl-pyridine-4-carboxylic acid (2′,5′-bis-trifluoromethyl-biphenyl-4-yl)-amide;3-methyl-pyridine-4-carboxylic acid (2′-methoxy-5′-chlorobiphenyl-4-yl)-amide;3-fluoro-pyridine-4-carboxylic acid (2′,5′-dimethoxybiphenyl-4-yl)-amide;3-fluoro-pyridine-4-carboxylic acid (2′-methoxy-5′-chlorobiphenyl-4-yl)-amide;3-fluoro-pyridine-4-carboxylic acid (2′,5′-bis-trifluoromethylbiphenyl-4-yl)-amide;3-methyl-pyridine-4-carboxylic acid (2′-methoxy-5′-methylbiphenyl-4-yl)-amide;3-methyl-pyridine-4-carboxylic acid (2′,5′-dimethylbiphenyl-4-yl)-amide;4-methyl-[1,2,3]-thiadiazole-5-carboxylic acid (2′-methoxy-5′-acetylbiphenyl-4-yl)-amide;3-fluoro-pyridine-4-carboxylic acid (2′-difluoromethoxy-5′-chlorobiphenyl-4-yl)-amide;4-methyl-[1,2,3]-thiadiazole-5-carboxylic acid {2′-(N,N-dimethylamino)-5′-trifluoromethoxybiphenyl-4- ...

Подробнее
17-04-2014 дата публикации

Amide derivative, pest control agent containing the amide derivative, and pest controlling method

Номер: US20140107368A1
Принадлежит: Mitsui Chemicals Agro Inc

A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(=G 1 )-Q 1 (wherein G 1 and G 2 represent an oxygen atom or the like, Q 1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q 2 represents a phenyl group or the like, G 3 represents an oxygen atom or the like, and R 1 and R 2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R 1 or R 2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.

Подробнее
17-04-2014 дата публикации

Processes and intermediates for making sweet taste enhancers

Номер: US20140107370A1
Принадлежит: Senomyx Inc

The present invention includes methods/processes and intermediates for preparing compounds having structural Formula (I): wherein X is alkyl, substituted alkyl, alkenyl, substituted alkenyl, heteroalkyl, substituted heteroalkyl, heteroalkenyl, or substituted heteroalkenyl.

Подробнее
23-01-2020 дата публикации

SUBSTITUTED DIHYDROINDENE-4-CARBOXAMIDES AND ANALOGS THEREOF, AND METHODS USING SAME

Номер: US20200024226A1
Принадлежит: Arbutus Biopharma Corporation

The present invention includes novel substituted bicyclic compounds, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) infections in a patient. In certain embodiments, the compounds and compositions of the invention are capsid inhibitors. 2. The compound of claim 1 , wherein each occurrence of Ror Ris independently selected from the group consisting of —(CH)-(optionally substituted heteroaryl) claim 1 , —(CH)-(optionally substituted heterocyclyl) claim 1 , and —(CH)-(optionally substituted aryl).3. The compound of claim 1 , wherein each occurrence of optionally substituted alkyl claim 1 , optionally substituted heterocyclyl claim 1 , or optionally substituted cycloalkyl is independently optionally substituted with at least one substituent selected from the group consisting of C-Calkyl claim 1 , halo claim 1 , —OR claim 1 , optionally substituted phenyl claim 1 , optionally substituted heteroaryl claim 1 , optionally substituted heterocyclyl claim 1 , —N(R)C(═O)R claim 1 , —C(═O)NRR claim 1 , and —N(R)(R) claim 1 , wherein each occurrence of Ris independently H claim 1 , optionally substituted C-Calkyl claim 1 , optionally substituted C-Ccycloalkyl claim 1 , optionally substituted aryl claim 1 , or optionally substituted heteroaryl claim 1 , or two Rgroups combine with the N to which they are bound to form a heterocycle.4. The compound of claim 1 , wherein each occurrence of optionally substituted aryl or optionally substituted heteroaryl is independently optionally substituted with at least one substituent selected from the group consisting of C-Calkyl claim 1 , C-Chaloalkyl claim 1 , C-Chaloalkoxy claim 1 , halo claim 1 , —CN claim 1 , —OR claim 1 , —N(R)(R) claim 1 , —NO claim 1 , —S(═O)N(R)(R) claim 1 , acyl claim 1 , and C-Calkoxycarbonyl claim 1 , wherein each occurrence of Ris independently H claim 1 , C-Calkyl claim 1 , or C-Ccycloalkyl.5. The compound of claim 1 , wherein each occurrence of optionally ...

Подробнее
04-02-2016 дата публикации

INSECTICIDAL COMPOUNDS

Номер: US20160029623A1
Принадлежит: SYNGENTA PARTICIPATIONS AG

The present invention relates to novel triazole derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests wherein R, R, G, G, Qand Qare as defined in claim or salts thereof. 2. A compound of formula (I) according to characterized in that{'sup': '1', 'Qis 3-pyridyl or 1-oxidopyridin-1-ium-3-yl;'}{'sup': '1', 'Yis selected from Cl, Br, I, methyl, ethyl, methoxy, difluoromethoxy, trifluoromethoxy, or methoxymethyl'}{'sup': '5', 'Yis selected from Cl, Br, I, ethyl'}{'sup': '3', 'Yis heptafluoroprop-2-yl or nonafluorobut-2-yl'}X is hydrogen or F{'sup': '1', 'sub': 1', '8', '2', '8, 'Ris selected from C-Calkyl, C-Calkenyl;'}{'sup': '2', 'sub': 1', '8', '2', '8, 'Ris selected from hydrogen, C-Calkyl, C-Calkenyl; and'}{'sup': 1', '2, 'Gand Gare both oxygen;'}3. A compound of formula (I) according to characterized in that{'sup': '1', 'Qis 3-pyridyl or 1-oxidopyridin-1-ium-3-yl;'}{'sup': '1', 'Yis selected from Cl, Br, I, methyl, ethyl;'}{'sup': '5', 'Yis selected from Cl, Br, I, ethyl;'}{'sup': '3', 'Yis heptafluoroprop-2-yl'}X is hydrogen or F{'sup': '1', 'sub': 2', '4, 'Ris selected from C-Calkyl;'}{'sup': '2', 'sub': 1', '4, 'Ris selected from hydrogen, C-Calkyl; and'}{'sup': 1', '2, 'Gand Gare both oxygen;'}4. A compound of formula (I) according to characterized in that{'sup': '1', 'Qis 3-pyridyl or 1-oxidopyridin-1-ium-3-yl;'}{'sup': '1', 'Yis selected from Cl, Br, methyl, ethyl;'}{'sup': '5', 'Yis selected from Cl, Br, ethyl;'}{'sup': '3', 'Yis heptafluoroprop-2-yl'}X is hydrogen or F{'sup': '1', 'sub': 2', '4, 'Ris selected from C-Calkyl;'}{'sup': '2', 'sub': 1', '4, 'Ris selected from hydrogen, C-Calkyl; and'}{'sup': 1', '2, 'Gand Gare both oxygen;'}5. A compound of formula (I) according to characterized in that{'sup': '1', 'Qis 3-pyridyl ...

Подробнее
04-02-2016 дата публикации

INSECTICIDAL COMPOUNDS

Номер: US20160029624A1
Принадлежит: SYNGENTA PARTICIPATIONS AG

The present invention relates to novel triazole derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests wherein R, R, G, G, Qand Qare as defined in claim ; or salts thereof. 2. A compound of formula (I) according to characterized in that{'sup': '1', 'Qis 4-pyridyl or 1-oxidopyridin-1-ium-4-yl;'}{'sup': '1', 'Yis selected from Cl, Br, I, methyl, ethyl, methoxy, difluoromethoxy, trifluoromethoxy, or methoxymethyl'}{'sup': '5', 'Yis selected from Cl, Br, I, ethyl'}{'sup': '3', 'Yis heptafluoroprop-2-yl or nonafluorobut-2-yl'}X is hydrogen or F{'sup': '1', 'sub': 1', '8', '2', '8, 'Ris selected from C-Calkyl, C-Calkenyl;'}{'sup': '2', 'sub': 1', '8', '2', '8, 'Ris selected from hydrogen, C-Calkyl, C-Calkenyl; and'}{'sup': 1', '2, 'Gand Gare both oxygen;'}3. A compound of formula (I) according to characterized in that{'sup': '1', 'Qis 4-pyridyl or 1-oxidopyridin-1-ium-4-yl;'}{'sup': '1', 'Yis selected from Cl, Br, I, methyl, ethyl;'}{'sup': '5', 'Yis selected from Cl, Br, I, ethyl;'}{'sup': '3', 'Yis heptafluoroprop-2-yl'}X is hydrogen or F{'sup': '1', 'sub': 2', '4, 'Ris selected from C-Calkyl;'}{'sup': '2', 'sub': 1', '4, 'Ris selected from hydrogen, C-Calkyl; and'}{'sup': 1', '2, 'Gand Gare both oxygen;'}4. A compound of formula (I) according to characterized in that{'sup': '1', 'Qis 4-pyridyl or 1-oxidopyridin-1-ium-4-yl;'}{'sup': '1', 'Yis selected from Cl, Br, methyl, ethyl;'}{'sup': '5', 'Yis selected from Cl, Br, ethyl;'}{'sup': '3', 'Yis heptafluoroprop-2-yl'}X is hydrogen or F{'sup': '1', 'sub': 2', '4, 'Ris selected from C-Calkyl;'}{'sup': '2', 'sub': 1', '4, 'Ris selected from hydrogen, C-Calkyl; and'}{'sup': 1', '2, 'Gand Gare both oxygen;'}5. A compound of formula (I) according to characterized in that{'sup': '1', 'Qis 4-pyridyl ...

Подробнее
01-02-2018 дата публикации

3-CARBAMOYLPHENYL-4-CARBOXAMIDE AND ISOPHTALAMIDE DERIVATIVES AS INHIBITORS OF THE WNT SIGNALLING PATHWAY

Номер: US20180028507A1
Принадлежит: BAYER PHARMA AKTIENGESELLSCHAFT

The present invention relates to inhibitors of the Wnt signalling pathways of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative disorder, as a sole agent or in combination with other active ingredients, in which: Rrepresents a group selected from: C-C-alkoxy-C-C-alkyl-, (A), (B), (C), (D), (E), (F), (G) or (H); wherein * indicates the point of attachment to the rest of the molecule; Rrepresents a group selected from: (I), (J) or (K); wherein * indicates the point of attachment to the rest of the molecule. 2. A compound according to claim 1 , wherein:{'sup': '1', 'sub': 2', '2', '3', '2', '2', '2', '3', '2', '2', '2', '2', '3', '2', '2', '2', '3', '2, 'Rrepresents a group selected from: —CH—CH—O—CH, —CH—CH—CH—O—CH, —CH—CH—CH—O—CH—CH, and —CH—CH—CH—O—C(H)(CH).'}8. A compound according to claim 1 , which is selected from the group consisting of:N-[4-methoxy-3-(pyridin-4-ylcarbamoyl)phenyl]biphenyl-4-carboxamide,N-{4-methoxy-3-[(3-methoxypropyl)carbamoyl]phenyl}biphenyl-4-carboxamide,N-{4-methoxy-3-[(2-methylpyridin-4-yl)carbamoyl]phenyl}biphenyl-4-carboxamide,N-{4-methoxy-3-[(3-methoxypropyl)(methyl)carbamoyl]phenyl}biphenyl-4-carboxamide,N-{3-[(3-ethoxypropyl)carbamoyl]-4-methoxyphenyl}biphenyl-4-carboxamide,N-{3-[(3-isopropoxypropyl)carbamoyl]-4-methoxyphenyl}biphenyl-4-carboxamide,{'sup': 1', '3, 'N-(biphenyl-4-yl)-N-(pyridin-2-ylmethyl)-4-(trifluoromethoxy)isophthalamide,'}N-{3-[(3-fluoropyridin-4-yl)carbamoyl]-4-methoxyphenyl}biphenyl-4-carboxamide,N-{3-[(3-chloropyridin-4-yl)carbamoyl]-4-methoxyphenyl}biphenyl-4-carboxamide,{'sup': 1', '3, 'N-(biphenyl-4-yl)-N-(2-methylpyridin-4-yl)-4-(trifluoromethoxy)isophthalamide,'}{' ...

Подробнее
04-02-2016 дата публикации

OLIGO-BENZAMIDE COMPOUNDS AND THEIR USE IN TREATING CANCERS

Номер: US20160031803A1
Автор: Ahn Jung-Mo, RAJ Ganesh

The present invention includes bis- and tris-benzamide compounds that block AR signaling and have activity against prostate cancer. Uses for these compounds, and pharmaceutical compositions containing the same, also are provided. 2. The compound of claim 1 , wherein X is —NO.3. (canceled)4. The compound of claim 2 , wherein A claim 2 , A′ and A″ are each O.5. The compound of claim 1 , wherein RChydroxyalkyl.6. The compound of claim 1 , wherein Ris C-Carylalkyl.7. The compound of claim 1 , wherein Ris Calkyl.8. The compound of claim 1 , wherein Ris Calkyl.937.-. (canceled)38. A pharmaceutical composition comprising a compound as shown in claim 1 , dispersed in a pharmaceutically acceptable carrier claim 1 , buffer or diluent.3942.-. (canceled)43. The compound of claim 5 , wherein Ris 2-hydroxyethyl.44. The compound of claim 6 , wherein Ris 2-quinolylethyl.45. The compound of claim 7 , wherein Ris butyl.46. The compound of claim 7 , wherein Ris isobutyl.47. The compound of claim 8 , wherein Ris isobutyl.48. The compound of claim 1 , wherein X is —NHCOR′ wherein: R′ is C-Carylalkyl.49. The compound of claim 1 , wherein Y is —COOH.50. The compound of claim 1 , wherein Y is —CONHR claim 1 , wherein: Ris —H or C-Calkyl. This application is a continuation of U.S. application Ser. No. 14/259,644, filed Apr. 23, 2014, which will issue as U.S. Pat. No. 9,072,705, which is a continuation of U.S. application Ser. No. 13/683,932, filed Nov. 21, 2012, now U.S. Pat. No. 8,754,124, which claims benefit of priority to U.S. Provisional Application Ser. No. 61/563,437, filed Nov. 23, 2011, and 61/664,372, filed Jun. 26, 2012. The entire text of each of the above referenced disclosures is specifically incorporated herein by reference.The present invention relates in general to the field of peptidomimetics and specifically to compositions of matter, kits, methods of making oligo-benzamide peptidomimetic compounds, and methods of their use in prostate cancers.Androgen receptor (AR) ...

Подробнее
17-02-2022 дата публикации

NOVEL INHIBITORS OF GUANOSINE MONOPHOSPHATE SYNTHETASE AS THERAPEUTIC AGENTS

Номер: US20220048866A1
Принадлежит:

The invention provides a series of GMPS enzyme inhibitors. The invention includes potent GMPS inhibitors that specifically and covalently bind to GMPS, exhibit broad anti-cancer activity, block the infection efficiency of viruses, and have the potentials to suppress undesired immune responses. These novel inhibitors of GMPS, and their derivatives, have tremendous potentials to be used as therapeutic agents for the treatment of cancers, viral infection and immune disorders. 5. The compound of wherein the compound is selected from the group consisting of 2-chloro-N-(4-((3-(prop-2-yn--yloxy)phenyl)amino)quinazolin-6-yl)acetamide; 2-chloro-N-(4-((3-methoxyphenyl)amino)quinazolin-6-yl)acetamide; and N-(4-((3-methoxyphenyl)amino)quinazolin-6-yl)acetamide.6. The compound of wherein the compound is selected from the group consisting of 3-(2-chloroacetamido)-N-(3-(prop-2-yn-l-yloxy)phenyl)benzamide and N-(3-(2-chloroacetamido)phenyl)-3-(prop-2-yn-1-yloxy)benzamide.9. The method of claim 7 , wherein the disease or disorder is cancer or viral infection.10. The method of claim 9 , wherein the cancer is selected from the group consisting of leukemia claim 9 , non-small cell lung cancer claim 9 , colon cancer claim 9 , central nervous system (CNS) cancer claim 9 , melanoma claim 9 , ovarian cancer claim 9 , renal cancer and breast cancer.11. The method of claim 9 , wherein the viral infection is selected from the group consisting of gastroenteritis claim 9 , fatal encephalitis claim 9 , encephalitis claim 9 , fever claim 9 , joint pain claim 9 , meningitis claim 9 , myocarditis claim 9 , paralysis claim 9 , hemorrhagic fever claim 9 , thrombocytopaenia claim 9 , common cold claim 9 , mononucleosis claim 9 , renal or respiratory syndrome claim 9 , hepatitis claim 9 , pneumonia claim 9 , diarrhea claim 9 , neurological disorder claim 9 , skin lesions claim 9 , skin lymphoma claim 9 , AIDS claim 9 , skin warts claim 9 , genital warts claim 9 , cervical cancer claim 9 , leukemia ...

Подробнее
30-01-2020 дата публикации

2-BENZOYLAMINOBENZAMIDE DERIVATIVES AS BCL-3 INHIBITORS

Номер: US20200031787A1
Принадлежит:

The invention relates to a compound of general formula (I): 2. A method according to claim 1 , wherein Ris halo claim 1 , nitro claim 1 , Calkyl claim 1 , Chaloalkyl or OR.3. A method according to claim 1 , wherein Ris hydrogen claim 1 , or methyl or ethyl claim 1 , either of which may optionally be substituted by one or more halo substituents.4. A method according to claim 1 , wherein Ris halo claim 1 , nitro claim 1 , methyl claim 1 , trifluoromethyl claim 1 , OH claim 1 , methoxy or trifluoromethoxy.5. A method according to claim 1 , wherein m is 1 or 2.6. A method according to claim 1 , wherein at least one Ris fluoro.7. A method according to claim 6 , wherein Ris 2-fluoro.8. A method according to claim 1 , wherein at least one Ris OR.9. A method according to claim 8 , wherein Ris Calkyl.10. A method according to claim 9 , wherein Ris methyl.11. A method according to claim 1 , wherein Ris morpholinyl.12. A method according to claim 1 , wherein p is 2 or 3.13. A method according to claim 1 , wherein Ris Calkyl or OR.14. A method according to claim 13 , wherein Ris methyl or methoxy.15. A method according to claim 1 , wherein n is 0 or 1.17. The method of claim 1 , wherein the cancer is leukaemia or lymphoma.18. The method of claim 1 , wherein the cancer is anaplastic large cell lymphoma (ALCLs) claim 1 , classic Hodgkin lymphoma (cHL) claim 1 , non-Hodgkin's lymphoma or solid tumour cancer.19. The method of claim 18 , wherein the cancer is a solid tumour cancer selected from the group consisting of: breast cancer claim 18 , melanoma claim 18 , lung cancer claim 18 , pancreatic cancer claim 18 , oesophageal cancer claim 18 , colorectal cancer claim 18 , nasopharyngeal carcinoma or hepatocarcinoma.20. The method according to claim 1 , wherein the treatment comprises the treatment or prevention of metastasis in cancers.21. The method according to claim 19 , wherein the cancer is breast cancer.22. The method according to claim 21 , wherein the cancer is triple ...

Подробнее
04-02-2021 дата публикации

FARNESOID X RECEPTOR AGONISTS AND USES THEREOF

Номер: US20210032195A1
Принадлежит:

Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity. 1131-. (canceled)134. The compound of claim 132 , or a pharmaceutically acceptable salt or solvate thereof claim 132 , wherein:ring B is phenyl; orring B is monocyclic 6-membered heteroaryl selected from pyridinyl, pyrimidinyl, pyrazinyl, and pyridazinyl.136. The compound of claim 134 , or a pharmaceutically acceptable salt or solvate thereof claim 134 , wherein:ring D is phenyl; orring D is monocyclic heteroaryl selected from furanyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, triazolyl, tetrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, and pyridazinyl; or{'sub': 2', '8, 'ring D is a monocyclic heterocycle that is a monocyclic C-Cheterocycloalkyl containing at least 1 N atom in the ring that is selected from aziridinyl, azetidinyl, pyrrolidinyl, pyrrolidinonyl, pyrrolidine-2,5-dionyl, piperidinyl, piperidin-2-onyl, piperazinyl, morpholinyl, thiomorpholinyl, and azepanyl.'}138. The compound of claim 136 , or a pharmaceutically acceptable salt or solvate thereof claim 136 , wherein:{'sup': 3', '10, 'Lis absent, —O—, —S—, —CH═CH—, —C≡C—, or —NR—.'}139. The compound of claim 132 , or a pharmaceutically acceptable salt or solvate thereof claim 132 , wherein:{'sub': 3', '8, 'ring A is C-Ccycloalkyl'}140. The compound of claim 132 , or a pharmaceutically acceptable salt or solvate thereof claim 132 , wherein:{'sub': 2', '8, 'ring A is C-Cheterocycloalkyl.'}141. The compound of claim 140 , or a pharmaceutically acceptable salt or solvate thereof claim 140 , wherein:{'sub': 2', '8', '5', '8', '5', '8', '5', '8', '5', '8, 'ring A is a monocyclic C-Cheterocycloalkyl or a bicyclic C-Cheterocycloalkyl ...

Подробнее
05-02-2015 дата публикации

Benzamides and nicotinamides as syk modulators

Номер: US20150038492A1
Принадлежит: Portola Pharmaceuticals LLC

The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.

Подробнее
08-02-2018 дата публикации

BENZAMIDES AND RELATED INHIBITORS OF FACTOR XA

Номер: US20180036296A1
Принадлежит:

Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders. 172.-. (canceled)74. The method of claim 73 , wherein the salt is the maleate salt.75. The method of claim 73 , wherein the compound is administered to the mammal in the form of a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier.76. The method of claim 75 , wherein the pharmaceutical composition is in capsule form.78. The method of claim 77 , wherein the salt is the maleate salt.79. The method of claim 77 , wherein the compound is administered to the mammal in the form of a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier.80. The method of claim 79 , wherein the pharmaceutical composition is in capsule form.82. The method of claim 81 , wherein the salt is the maleate salt.83. The method of claim 81 , wherein the compound is administered to the mammal in the form of a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier.84. The method of claim 83 , wherein the pharmaceutical composition is in capsule form. This invention relates to novel compounds which are potent and highly selective inhibitors of isolated factor Xa or when assembled in the prothrombinase complex. These compounds show selectivity for factor Xa versus other proteases of the coagulation (e.g. thrombin, fVIIa, fIXa) or the fibrinolytic cascades (e.g. plasminogen activators, plasmin). In another aspect, the present invention relates to novel monoamidino-containing compounds, their pharmaceutically acceptable salts, and pharmaceutically acceptable compositions thereof which are useful as potent and specific inhibitors of blood ...

Подробнее
12-02-2015 дата публикации

SUBSTITUTED TETRACYCLINE COMPOUNDS

Номер: US20150045329A1
Принадлежит: PARATEK PHARMACEUTICALS, INC.

The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds such as blocking tetracycline efflux and modulation of gene expression. 149-. (canceled)51. A pharmaceutical composition comprising the tetracycline compound of and a pharmaceutically acceptable carrier.53. The method of claim 52 , wherein said subject is a human.54. The method of claim 52 , wherein the tetracycline responsive state is not a bacterial infection.55. The method of claim 54 , wherein the tetracycline responsive state is an inflammatory disorder.56. The method of claim 55 , wherein the inflammatory disorder is rheumatoid arthritis.57. The method of claim 55 , wherein the inflammatory disorder is acute or chronic gastroenteritis and colitis. This patent application claims priority to U.S. Provisional Patent Application Ser. No. 60/530,123, filed Dec. 16, 2003; U.S. Provisional Patent Application Ser. No. 60/525,287, filed Nov. 25, 2003; and U.S. Provisional Patent Application Ser. No. 60/486,017, filed Jul. 9, 2003, all of which are entitled “Substituted Tetracycline Compounds.” The entire contents of each of the aforementioned applications are hereby incorporated herein by reference.The development of the tetracycline antibiotics was the direct result of a systematic screening of soil specimens collected from many parts of the world for evidence of microorganisms capable of producing bacteriocidal and/or bacteriostatic compositions. The first of these novel compounds was introduced in 1948 under the name chlortetracycline. Two years later, oxytetracycline became available. The elucidation of the chemical structure of these compounds confirmed their similarity and furnished the analytical basis for the production of a third member of this group in 1952, ...

Подробнее
25-02-2021 дата публикации

Insecticidal compounds

Номер: US20210051955A1
Принадлежит: SYNGENTA PARTICIPATIONS AG

The present invention relates to novel triazole derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests wherein Y, X 1 , X 2 and Q are as defined in claim 1 ; or salts thereof.

Подробнее
08-05-2014 дата публикации

Composition and Method for Making Oligo-Benzamide Compounds

Номер: US20140127285A1
Автор: Ahn Jung-Mo

The present invention includes compound compositions and methods of making compounds that include an oligo-benzamide compound having at least two optionally substituted benzamides. 212-. (canceled)14. The composition of claim 13 , further comprising one or more of diluents excipients claim 13 , active agents claim 13 , lubricants claim 13 , preservatives claim 13 , stabilizers claim 13 , wetting agents claim 13 , emulsifiers claim 13 , salts for influencing osmotic pressure claim 13 , buffers claim 13 , colorings claim 13 , flavorings claim 13 , aromatic substances claim 13 , penetration enhancers claim 13 , surfactants claim 13 , fatty acids claim 13 , bile salts claim 13 , chelating agents claim 13 , colloids and combinations thereof.15. The composition of claim 13 , wherein the pharmaceutical composition is in the form of a solution claim 13 , an emulsion claim 13 , a liposome-containing formulation claim 13 , a tablet claim 13 , a capsule claim 13 , a gel capsule claim 13 , a liquid syrup claim 13 , a soft gel claim 13 , a suppository claim 13 , an enema claim 13 , a patch claim 13 , an ointment claim 13 , a lotion claim 13 , a cream claim 13 , a gel claim 13 , a drop claim 13 , a spray claim 13 , a liquid or a powder.19. The compound of claim 18 , wherein R1 claim 18 , R2 claim 18 , R3 claim 18 , R4 claim 18 , R5 claim 18 , R6 claim 18 , R7 claim 18 , R8 claim 18 , and R9 may individually comprise an acetyl group or a t-butoxycarbonyl group claim 18 , a benzyl group claim 18 , a methyl group claim 18 , a substituted benzyl group claim 18 , a 4-fluorobenzyl group claim 18 , a 2-naphthylmethyl group claim 18 , or an amino acid claim 18 , an amino acid analogue claim 18 , an artificial amino acid claim 18 , a carbohydrate claim 18 , a lipid claim 18 , a nucleic acid claim 18 , a sugar claim 18 , or a linker.20. The compound of claim 18 , wherein R1 comprises an acetyl group claim 18 , R2 comprises a benzyl group claim 18 , R3 comprises an isopropyl claim 18 , and ...

Подробнее
14-02-2019 дата публикации

3,4-DISUBSTITUTED 3-CYCLOBUTENE-1,2-DIONES AND USE THEREOF

Номер: US20190047947A1
Принадлежит:

Described herein are compounds, or pharmaceutically acceptable salts thereof, of the following formula: 3. The compound or a pharmaceutically acceptable salt thereof of , wherein Ris Calkyl substituted with at least one group selected from ORhalo , —COR , and 3 to 11 membered cycloalkyl , and wherein R , R , R , R , R , R , and W are as defined in .4. The compound or a pharmaceutically acceptable salt thereof of , wherein Ris hydrogen , and wherein R , R , R , R , and R , and W are as defined in .5. The compound or a pharmaceutically acceptable salt thereof of , wherein Ris 6 to 12 membered aryl or Calkyl , and wherein R , R , R , and R , and W are as defined in .6. The compound or a pharmaceutically acceptable salt thereof of claim 2 , wherein Ris hydrogen or Calkyl.7. The compound or a pharmaceutically acceptable salt thereof of claim 6 , wherein Ris hydrogen.8. The compound or a pharmaceutically acceptable salt thereof of claim 6 , wherein Ris Calkyl claim 6 , and wherein R claim 6 , R claim 6 , R claim 6 , R claim 6 , R claim 6 , R claim 6 , and W are as defined in .9. The compound or a pharmaceutically acceptable salt thereof of claim 6 , wherein Ris hydrogen claim 6 , and wherein R claim 6 , R claim 6 , R claim 6 , R claim 6 , R claim 6 , and W are as defined in .10. The compound or a pharmaceutically acceptable salt thereof of claim 8 , wherein Ris 6 to 12 membered aryl.11. The compound or a pharmaceutically acceptable salt thereof of claim 8 , wherein Ris 5 to 12 membered heteroaryl optionally substituted with at least one Calkyl group.12. The compound or a pharmaceutically acceptable salt thereof of claim 8 , wherein Ris —C(O)NRR claim 8 , and wherein Rand Rare independently selected from hydrogen claim 8 , Calkyl claim 8 , and 3 to 11 membered cycloalkyl.13. The compound or a pharmaceutically acceptable salt thereof of claim 8 , wherein Ris Calkyl claim 8 , and wherein R claim 8 , R claim 8 , R claim 8 , R claim 8 , R claim 8 , and W are as defined in .14. ...

Подробнее
25-02-2016 дата публикации

Novel compounds

Номер: US20160052898A1
Принадлежит: Bayer Pharma AG

The present invention relates to substituted N-biphenyl-3-acetylamino-benzamides and N-[3-(acetylamino)phenyl]-biphenyl-carboxamides of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative disorder, as a sole agent or in combination with other active ingredients.

Подробнее
25-02-2021 дата публикации

KETONE INHIBITORS OF LYSINE GINGIPAIN

Номер: US20210053908A1
Принадлежит: Cortexyme, Inc.

The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium . Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with infection, including brain disorders such as Alzheimer's disease. 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group consisting of Ccycloalkyl claim 1 , Calkyl claim 1 , Caryl claim 1 , and 5- to 12-membered heteroaryl each of which is optionally substituted with one or more Rsubstituents claim 1 , and each Ris independently selected from the group consisting of halogen claim 1 , —N claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , Calkoxy claim 1 , Chaloalkoxy claim 1 , —N(R) claim 1 , —N(R) claim 1 , and —NRC(O)R.3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris Calkyl substituted with Calkoxy.5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris hydrogen.67-. (canceled)8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —CHR claim 1 , Ris —O—R claim 1 , and Ris Chaloalkyl.9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —CHR claim 1 , Ris —O—R claim 1 , and Ris 5- to 12-membered heteroaryl claim 1 , which is optionally substituted with one or more members independently selected from the group consisting of halogen and Calkyl.10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group consisting of —N(R) claim 1 , 5- to 12-membered heteroaryl claim 1 , and 3- to 12-membered heterocyclyl claim 1 , wherein:{'sub': 1-3', '1-3, '5- to 12-membered heteroaryl is optionally substituted with one or more members ...

Подробнее
25-02-2021 дата публикации

Novel antimicrobial compound and use thereof

Номер: US20210053909A1

The coralmycin A and B have very strong antimicrobial activity against antibiotic-resistant bacteria such as MRSA, QRSA, VRE, VISA, etc.; Acinetobacter baumannii, which is a multidrug-resistant microorganism; and also against gram-positive microorganisms and gram-negative microorganisms. Therefore, the present invention can be very useful for prevention, treatment and alleviation of various microbial infections, and thus can be widely applied to the medical supply, quasi-drug, food, and feed industries.

Подробнее
22-02-2018 дата публикации

USES OF HISTONE ACETYLTRANSFERASE ACTIVATORS

Номер: US20180050982A1
Принадлежит:

The invention provides methods for enhancing histone acylation, learning, memory and/or cognition in subjects with compound (I) or compositions comprising compound (I), or a pharmaceutically acceptable salt thereof. 125-. (canceled)27. The method of claim 26 , wherein the subject is not afflicted with a neurodegenerative condition or disease.28. The method of claim 27 , wherein the neurodegenerative condition or disease is selected from one or more of the group consisting of adrenoleukodystrophy (ALD) claim 27 , alcoholism claim 27 , Alexander's disease claim 27 , Alper's disease claim 27 , Alzheimer's disease claim 27 , amyotrophic lateral sclerosis (Lou Gehrig's Disease or ALS) claim 27 , ataxia telangiectasia claim 27 , batten disease (Spielmeyer-Vogt-Sjögren-Batten disease) claim 27 , bovine spongiform encephalopathy (BSE) claim 27 , canavan disease claim 27 , cockayne syndrome claim 27 , corticobasal degeneration claim 27 , Creutzfeldt-Jakob disease claim 27 , familial fatal insomnia claim 27 , frontotemporal lobar degeneration claim 27 , Huntington's disease claim 27 , HIV-associated dementia claim 27 , Kennedy's disease claim 27 , Krabbe's disease claim 27 , lewy body dementia claim 27 , neuroborreliosis claim 27 , Machado-Joseph disease (spinocerebellar ataxia type 3) claim 27 , multiple system atrophy claim 27 , multiple sclerosis claim 27 , narcolepsy claim 27 , Niemann Pick disease claim 27 , Parkinson's disease claim 27 , Pelizaeus-Merzbacher disease claim 27 , Pick's disease claim 27 , primary lateral sclerosis claim 27 , prion diseases claim 27 , progressive supranuclear palsy claim 27 , Rett's syndrome claim 27 , tau-positive frontotemporal dementia claim 27 , tau-negative frontotemporal dementia claim 27 , Refsum's disease claim 27 , sandhoff disease claim 27 , Schilder's disease claim 27 , subacute combined degeneration of spinal cord secondary to pernicious anaemia claim 27 , spinocerebellar ataxia (multiple types with varying characteristics) ...

Подробнее
10-03-2022 дата публикации

INHIBITORS OF CGAS ACTIVITY AS THERAPEUTIC AGENTS

Номер: US20220073470A1
Принадлежит:

This disclosure relates to compounds, pharmaceutical compositions comprising them, and methods of using the compounds and compositions for treating or preventing inappropriate activation of a type I interferon (IFN) response in a subject in need thereof. 2. The compound of claim 1 , wherein L is —N—.3. The compound of claim 1 , wherein L is —CR—.4. The compound of claim 3 , wherein Ris hydrogen claim 3 , C-Calkyl claim 3 , C-Chaloalkyl claim 3 , —NH claim 3 , —NH(C-Calkyl) claim 3 , —N(C-Calkyl) claim 3 , —OH claim 3 , C-Calkoxy claim 3 , C-Chaloalkoxy claim 3 , —C(O)OR claim 3 , —C(O)NRR claim 3 , aryl optionally substituted with one or more R claim 3 , heteroaryl optionally substituted with one or more R claim 3 , heterocycloalkyl optionally substituted with one or more R claim 3 , or C-Ccycloalkyl optionally substituted with one or more R.5. The compound of claim 3 , wherein Ris hydrogen claim 3 , C-Calkyl claim 3 , —C(O)OR claim 3 , aryl optionally substituted with one or more R claim 3 , or heteroaryl optionally substituted with one or more R.6. The compound of claim 3 , wherein Ris hydrogen claim 3 , phenyl claim 3 , or —C(O)OH.7. The compound of claim 3 , wherein Ris hydrogen.8. The compound of any of - claim 3 , wherein Ris heteroaryl optionally substituted with one or more R.9. The compound of any of - claim 3 , wherein Ris imidazol-1-yl optionally substituted with one or more R.10. The compound of any of - claim 3 , wherein Ris unsubstituted imidazol-1-yl.11. The compound of any of - claim 3 , wherein Ris hydrogen claim 3 , halogen claim 3 , C-Calkyl claim 3 , C-Chaloalkyl claim 3 , —NH claim 3 , —NH(C-Calkyl) claim 3 , —N(C-Calkyl) claim 3 , —OH claim 3 , C-Calkoxy claim 3 , C-Chaloalkoxy claim 3 , or phenyl.12. The compound of any of - claim 3 , wherein Ris hydrogen claim 3 , halogen claim 3 , C-Calkyl claim 3 , —NH claim 3 , C-Calkoxy claim 3 , or phenyl.13. The compound of any of - claim 3 , wherein Ris hydrogen claim 3 , methyl claim 3 , or methoxy.14 ...

Подробнее
15-05-2014 дата публикации

PROCESS FOR THE PREPARATION OF PROTECTED L-ALANINE DERIVATIVES

Номер: US20140135525A1
Принадлежит:

The present invention is directed to a novel process for the preparation of protected L-alanine derivatives, useful as intermediates in the synthesis of compounds useful as mu/delta opioid modulators. 2. The process as in claim 1 , wherein the oxidizing agent is selected from the group consisting of hydrogen peroxide claim 1 , LiOH and LiOOH.3. The process as in claim 2 , wherein the oxidizing agent is hydrogen peroxide.4. The process as in claim 1 , wherein the oxidizing agent is 30% hydrogen peroxide and is present in an excess amount.5. The process as in claim 1 , wherein the inorganic base is potassium carbonate.6. The process as in claim 1 , wherein the inorganic base is present in an amount in the range of from about 1.0 to about 3.0 molar equivalents.7. The process as in claim 1 , wherein the third organic solvent is DMSO.8. The process as in claim 1 , wherein the compound of formula (I-B) is reacted with the oxidizing agent at a temperature in the range of from about room temperature to about 60° C.9. A compound prepared according to a process as in . This application is a divisional of U.S. Ser. No. 12/606,730, filed Oct. 27, 2009, (now allowed), which is derived from and claims priority to U.S. Provisional App. No. 61/108,649, filed Oct. 27, 2008, the entire contents of each of which are incorporated by reference herein.The present invention is directed to a novel process for the preparation of protected L-alanine derivatives, useful as intermediates in the synthesis of compounds useful as mu/delta opioid modulators.The opioid receptors were identified in the mid-1970's, and were quickly categorized into three sub-sets of receptors (mu, delta and kappa). More recently the original three types of receptors have been further divided into sub-types. Also known is that the family of opioid receptors are members of the G-protein coupled receptor (GPCR) super-family. More physiologically pertinent are the well established facts that opioid receptors are found ...

Подробнее
05-03-2015 дата публикации

METHOD FOR PRODUCING ALKYLATED AROMATIC AMIDE DERIVATIVE

Номер: US20150065721A1
Автор: Okura Hironari
Принадлежит: MITSUI CHEMICALS AGRO, INC.

Provided is a method for producing an aromatic amide derivative represented by Formula (4), the method including a process in which an aromatic amide derivative represented by Formula (1) and a haloalkyl compound represented by Formula (3) are reacted with each other in the presence of a base and a metal or metal salt. In the formulae, each of X and Y represents a hydrogen atom, a halogen atom, or the like. A represents a hydrogen atom, an alkyl group, a group represented by Formula (2), or the like. Each of Gand Grepresents an oxygen atom or the like. Qrepresents a phenyl group or the like. Rrepresents a hydrogen atom, an alkyl group, or the like. Zrepresents a haloalkyl group or the like. Xa represents an iodine atom or the like. m represents a number of from 1 to 4, n1 represents a number from 1 to 5, and n2 represents a number of from 1 to 4. 7. The alkylated aromatic amide derivative according to claim 6 , wherein claim 6 , in Formula (9) claim 6 , Yrepresents a C1-C2 haloalkyl group claim 6 , each of Yand Yrepresents a hydrogen atom claim 6 , Zrepresents a C1-C6 haloalkyl group claim 6 , and X represents a halogen atom. The present invention relates to a method for producing an alkylated aromatic amide derivative.International Publication WO 2005/73165, International Publication WO 2006/137376, and International Publication WO 2010/18714 disclose various compounds as amide derivatives having pest control effects, and disclose that an amide derivative having a perfluoroalkylated phenyl group is useful in the production of the amide derivative.As a method for producing an aniline having a perfluoroalkylated phenyl group, a production method in which a perfluoroalkyl halogen compound is reacted in the presence of a reducing agent is known (see, for example, Japanese Patent Application Laid-Open (JP-A) No. 2001-122836). Further, as a method for producing an amide derivative having a perfluoroalkylated phenyl group, the method described in the Journal of Fluorine ...

Подробнее
22-05-2014 дата публикации

MEDICAMENT FOR LIVER REGENERATION AND FOR TREATMENT OF LIVER FAILURE

Номер: US20140141510A1
Принадлежит:

The present invention relates to the use of a compound which inhibits the activity of MKK4 as a medicament for the treatment of a patient suffering from an impaired liver function, to the use of a compound as a medicament for the treatment of liver failure, including acute/fulminant or chronic liver failure and/or for increasing the regeneration of liver tissue in a patient. 1. Compound , which is an inhibitor of the activity of MKK4 , MKK4 being encoded by the mRNA of SEQ ID NO: 1204 , for use as a medicament in the treatment of liver failure and/or for the protection of hepatocytes against apoptosis and/or for the regeneration of hepatocytes.2. Compound according to claim 1 , characterized in that the compound is an siRNA containing an oligonucleotide having a nucleotide sequence hybridizing under physiological conditions to the mRNA of SEQ ID NO: 1204.3. Compound according to claim 2 , characterized in that the oligonucleotide is selected from the group comprising miR-15b claim 2 , miR-24 claim 2 , miR-25 claim 2 , miR-141 claim 2 , and SEQ ID NO: 1 to SEQ ID NO: 1203.4. Compound according to claim 2 , characterized in that the oligonucleotide is comprised as a first section in a nucleic acid construct which contains a second section which is reverse complementary to the first section.5. Compound according to claim 2 , characterized in that the oligonucleotide is arranged under the control of a promoter in an expression cassette.6. Compound according to claim 2 , characterized in that the oligonucleotide is contained in a liposome formulation and/or in a viral vector which is packaged in a viral particle or in a virus-like particle.7. Compound according to claim 1 , characterized in that the compound is selected from the group consisting of SP600125 claim 1 , myricitine claim 1 , Genistein claim 1 , PD98059 claim 1 , and the compounds of Table 1.8. Compound according to claim 1 , characterized in that the compound is formulated as liposomes or lipid nanoparticles ...

Подробнее
17-03-2022 дата публикации

FARNESOID X RECEPTOR AGONISTS AND USES THEREOF

Номер: US20220081390A1
Принадлежит:

Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity. 4. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:ring B is phenyl.5. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:ring B is monocyclic 6-membered heteroaryl selected from pyridinyl, pyrimidinyl, pyrazinyl, and pyridazinyl.7. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:ring D is phenyl.8. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:ring D is monocyclic heteroaryl selected from furanyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, triazolyl, tetrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, and pyridazinyl.11. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:{'sub': 2', '8, 'ring D is a monocyclic heterocycle that is a monocyclic C-Cheterocycloalkyl containing at least 1 N atom in the ring that is selected from aziridinyl, azetidinyl, pyrrolidinyl, pyrrolidinonyl, pyrrolidine-2,5-dionyl, piperidinyl, piperidin-2-onyl, piperazinyl, morpholinyl, thiomorpholinyl, and azepanyl.'}12. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:{'sup': 3', '2', '4', '4', '2, 'Lis —X-L- or -L-X—;'}{'sup': 2', '10', '10', '10', '10', '10, 'sub': 2', '2', '2', '2, 'Xis absent, —O—, —S—, —S(═O)—, —S(═O)—, —S(═O)NR—, —CH—, —CH═CH—, —C≡C—, —C(═O)—, —C(═O)O—, —OC(═O)—, —C(═O)NR—, —NRC(═O)—, —NRS(═O)—, or —NR—;'}{'sup': '4', 'sub': '2', 'Lis absent or —CH—.'}13. The compound of any one of - , or a pharmaceutically ...

Подробнее
16-03-2017 дата публикации

Nasal formulations of metoclopramide

Номер: US20170071885A1
Принадлежит: Evoke Pharma Inc

Nasal formulations of metoclopramide, which remain stable and/or colorless upon storage over a period of time, are provided. Also provided are methods of treating disorders treatable with metoclopramide, comprising administering the nasal solutions to patients in need thereof.

Подробнее
15-03-2018 дата публикации

INHIBITORS OF HISTONE DEACETYLASE

Номер: US20180072671A1
Принадлежит:

The present invention relates to compounds of formula (I): 2. A compound of or a pharmaceutically acceptable salt claim 1 , hydrate claim 1 , solvate claim 1 , or prodrug thereof claim 1 , wherein{'sub': 1', '2', '3', '4', '1', '2', '3', '4, 'W, W, W, and Ware each independently selected from hydrogen, chlorine, fluorine, and deuterium, provided that at least one of W, W, W, and Wis not hydrogen;'}{'sub': 1', '5', '1', '3, 'Xand Xare each independently selected from hydrogen, halogen and C-Calkyl;'}{'sub': 2', '3', '4', 'p', 'p', '1', '8', '2', '8', '2', '8', '3', '8', '4', '8', '2', '3', '4, 'sup': 5', '6', '7', '1', '7', '3', '4', '1', '2', 'a, 'X, X, and Xare each independently selected from hydrogen, halogen, OR, C(O)R, OS(O)R, NRS(O)R, NRR, NRC(O)R, C-Calkyl, C-Calkenyl, C-Calkynyl, C-Ccycloalkyl, C-Ccycloalkenyl, aromatic ring, 3-8 membered heteroaromatic ring, and 3-8 membered saturated or partially saturated heterocyclic ring, wherein said alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aromatic ring, heteroaromatic ring, and heterocyclic ring is unsubstituted or substituted with one or more Rand one or two of X, X, and Xis hydrogen;'}{'sup': a', '25', '26', '27', '28', '29, 'sub': 1', '8', '3', '2', '2, 'Ris selected from halogen, OR, C-Calkyl, CF, CHF, CHF, NRC(O)R, and NRR; or'}{'sup': 1', '26, 'sub': 1', '8, 'Rand Rare each independently selected from hydrogen and C-Calkyl;'}{'sup': 2', 'b, 'sub': 1', '8', '2', '8', '3', '8', '3', '8', '4', '8, 'Ris selected from hydrogen, C-Calkyl, C-Calkenyl, C-Calkynyl, C-Ccycloalkyl, C-Ccycloalkenyl, aromatic ring, 3-8 membered heteroaromatic ring, and 3-8 membered saturated or partially saturated heterocyclic ring, wherein said alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aromatic ring, heteroaromatic ring, and heterocyclic ring are unsubstituted or substituted with one or more R;'}{'sup': 27', 'b, 'sub': 1', '8', '3', '8', '3', '8', '4', '8, 'Ris selected from hydrogen, C-Calkyl, C-Calkynyl, C-Ccycloalkyl, ...

Подробнее
07-03-2019 дата публикации

PROCESS FOR THE PREPARATION OF IOPAMIDOL

Номер: US20190071392A1
Принадлежит: BRACCO IMAGING S.P.A.

The present invention discloses a process for the preparation of Iopamidol of formula (II) and comprising the following steps: a) reacting the Compound (I) wherein X is OR2 or R3, and wherein R2 and R3 are a Ci-C6 linear or branched alkyl, C3-C6 cycloalkyl, C6 aryl, optionally substituted with a group selected from the group consisting of methyl, ethyl, n-propyl, i-propyl, n-butyl, sec-butyl, t-butyl and phenyl, with the acylating agent (S)-2-(acetyloxy)propanoyl chloride in a reaction medium to provide the acetyloxy derivative of Compound (I); b) hydrolyzing the intermediate from step a) with an aqueous solution at a pH comprised from 0 to 7, by adding water or a diluted alkaline solution such as sodium hydroxide or potassium hydroxide, freeing the hydroxyls from the boron-containing protective groups, obtaining the N—(S)-2-(acetyloxy)propanoyl derivative of Compound (II); c) alkaline N hydrolysis to restore the (S)-2-(hydroxy)propanoyl group and to obtain Iopamidol (II) and optional recovery of the boron derivative from the solution obtained in step b). The boron-containing protective group is versatile, efficient and recyclable. A one-pot synthesis, without intermediate isolation is provided, leading to a decreasing of recovered and recycled solvents and a significant increasing in the yield, representing a significant advantage in terms of cost-effectiveness of the entire process and environmental awareness. 122-. (canceled)23. A process for recovery of a boronic acid of formula R—B(OH) , wherein Ris selected from the group consisting of C-Clinear or branched alkyl , C-Ccycloalkyl , and Caryl , optionally substituted with a group selected from the group consisting of methyl , ethyl , n-propyl , i-propyl , n-butyl , sec-butyl , t-butyl , and phenyl , from an aqueous mixture optionally comprising a polar solvent , said process comprising the following steps:admixing the aqueous mixture with a water-immiscible organic solvent in a weight ratio between the boronic ...

Подробнее
07-03-2019 дата публикации

NOVEL COMPOUND HAVING BLT INHIBITORY ACTIVITY AND COMPOSITION, FOR PREVENTING OR TREATING INFLAMMATORY DISEASES, COMPRISING SAME AS ACTIVE INGREDIENT

Номер: US20190071395A1
Принадлежит:

The present invention relates to a novel compound showing leukotriene B4 receptor 2 (BLT2) inhibitory activity and a pharmaceutical composition, for preventing or treating inflammatory diseases, having same as an active ingredient. The inventors identified a novel compound containing BTL2 inhibitory activity, and experimentally confirmed that the present novel compound had an excellent effect on the enhancement of the cancer cell death, on the inhibition of the metastasis and chemotactic mobility, and on the anti-asthma activity. Therefore, the present novel compound can be used as a very effective pharmaceutical component for treating the inflammatory-related diseases. 3. The method of claim 1 , wherein the compound represented by Formula 1 is selected from the group consisting of:tert-butyl 4-(4-(3-(N-phenylpentaneamido)prop-1-ynyl)benzoyl)piperazine-1-carboxylate;N-phenyl-N-(3-(4-(piperazine-1-carbonyl)phenyl)prop-2-ynyl)pentaneamide;N-(3-(4-(4-methylpiperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;N-(3-(4-(4-ethylpiperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;N-(3-(4-(4-isopropylpiperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;N-(3-(4-(4-(2-hydroxyethyl)piperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;N-(3-(4-(4-(cyclopropylmethyl)piperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;N-(3-(4-(4-cyclohexylpiperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;N-(3-(4-(4-(cyclohexylmethyl)piperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;N-(3-(4-(4-isobutylpiperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;N-phenyl-N-(3-(4-(4-(prop-2-ynyl)piperazine-1-carbonyl)phenyl)prop-2-ynyl)pentaneamide;N-(3-(4-(4-cyanopiperazine-1-carbonyl)phenyl)prop-2-ynyl)-N-phenylpentaneamide;tert-butyl 4-(4-(3-(N-(3-fluorophenyl)pentaneamido)prop-1-ynyl)benzoyl)piperazine-1-carboxylate;N-(3-fluorophenyl)-N-(3-(4-(piperazine-1-carbonyl)phenyl)prop-2-ynyl)pentaneamide;N-(3-fluorophenyl)-N-( ...

Подробнее
16-03-2017 дата публикации

BETA- AND GAMMA-AMINO-ISOQUINOLINE AMIDE COMPOUNDS AND SUBSTITUTED BENZAMIDE COMPOUNDS

Номер: US20170073325A1
Принадлежит:

Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds. 2. The compound according to claim 1 , wherein n is 1 to 3.3. The compound according to claim 2 , wherein n is 2.4. The compound according to claim 1 , wherein one Ris claim 1 , independently claim 1 , C-Calkyl claim 1 , cycloalkyl claim 1 , heterocycloalkyl claim 1 , aryl claim 1 , or heteroaryl.5. The compound according to claim 1 , wherein Xand Xare claim 1 , independently claim 1 , hydrogen or chloro or fluoro.6. The compound according to claim 1 , wherein Ris hydrogen.7. The compound according to claim 1 , wherein n is 2; wherein one Ris aryl or heteroaryl; wherein Xand Xare claim 1 , independently claim 1 , hydrogen claim 1 , chloro or fluoro; and wherein Ris hydrogen.8. The compound according to claim 7 , wherein the other Rgroups are hydrogen.9. The compound according to claim 1 , wherein one Ris aryl or heteroaryl.10. The compound according to claim 9 , wherein one Ris thienyl.11. The compound according to claim 9 , wherein one Ris monosubstituted phenyl or monosubstituted thienyl.12. The compound according to claim 11 , wherein the substituent is fluoro claim 11 , chloro claim 11 , or cyano.13. The compound according to claim 9 , wherein one Ris unsubstituted phenyl or unsubstituted thienyl.14. The compound according to claim 1 , wherein Xand Xare hydrogen.16. The compound according to claim 1 , wherein n is 2; Rand Rare claim 1 , ...

Подробнее
14-03-2019 дата публикации

INSECTICIDAL COMPOUNDS

Номер: US20190075792A1
Принадлежит: SYNGENTA PARTICIPATIONS AG

The present invention relates to novel triazole derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests 3. A compound of formula (I) according to characterized in thatR is hydrogen or ethyl.4. A compound of formula (I) according to characterized in that Y is chlorine claim 1 , bromine or iodine.5. A compound of formula (I) according to characterized in that Q is a group selected from Q2 claim 1 , Q3 claim 1 , Q4 and Q5.6. A method of controlling insects claim 1 , acarines claim 1 , nematodes or molluscs which comprises applying to a pest claim 1 , to a locus of a pest claim 1 , or to a plant susceptible to attack by a pest an insecticidally claim 1 , acaricidally claim 1 , nematicidally or molluscicidally effective amount of a compound of formula (I) as defined in .7. An insecticidal claim 1 , acaricidal claim 1 , nematicidal or molluscicidal composition comprising an insecticidally claim 1 , acaricidally claim 1 , nematicidally or molluscicidally effective amount of a compound of formula (I) as defined in together with an agrochemically acceptable diluent or carrier.8. A composition according to which further comprises one or more additional insecticidal claim 7 , acaricidal claim 7 , nematicidal or molluscicidal compounds.9. A method of protecting useful plants from insects claim 1 , acarines claim 1 , nematodes or molluscs claim 1 , comprising applying to said plants claim 1 , to the locus thereof claim 1 , or to plant propagation material thereof claim 1 , an insecticidally claim 1 , acaricidally claim 1 , nematicidally or molluscicidally effective amount of a compound of formula (I) as defined in . This application is a continuation of U.S. patent application Ser. No. 15/824,099, filed 28 Nov. 2017, which is a divisional of U.S. ...

Подробнее
22-03-2018 дата публикации

INSECTICIDAL COMPOUNDS

Номер: US20180077930A1
Принадлежит: SYNGENTA PARTICIPATIONS AG

The present invention relates to novel triazole derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests 3. A compound of formula (I) according to wherein{'sub': '1', 'Xis hydrogen, fluorine or methoxy'}{'sub': 2', '2', '1, 'Xis hydrogen or cyano, with the condition that if Xis cyano, then Xis hydrogen,'}R is hydrogen, methyl or ethyl.4. A compound of formula (I) according to wherein{'sub': 1', '2, 'Xis methoxy and Xis hydrogen.'}5. A compound of formula (I) according to wherein{'sub': 2', '1, 'Xis cyano and Xis hydrogen.'}7. A method of controlling insects claim 4 , acarines claim 4 , nematodes or molluscs which comprises applying to a pest claim 4 , to a locus of a pest claim 4 , or to a plant susceptible to attack by a pest an insecticidally claim 4 , acaricidally claim 4 , nematicidally or molluscicidally effective amount of a compound of formula (I) as defined in 1.8. An insecticidal claim 4 , acaricidal claim 4 , nematicidal or molluscicidal composition comprising an insecticidally claim 4 , acaricidally claim 4 , nematicidally or molluscicidally effective amount of a compound of formula (I) as defined in 1 together with an agrochemically acceptable diluent or carrier.9. A composition according to which further comprises one or more additional insecticidal claim 8 , acaricidal claim 8 , nematicidal or molluscicidal compounds.10. A method of protecting useful plants from insects claim 1 , acarines claim 1 , nematodes or molluscs claim 1 , comprising applying to said plants claim 1 , to the locus thereof claim 1 , or to plant propagation material thereof claim 1 , an insecticidally claim 1 , acaricidally claim 1 , nematicidally or molluscicidally effective amount of a compound of formula I in . This application is a U.S. divisional ...

Подробнее
14-03-2019 дата публикации

PROCESS FOR THE PREPARATION OF IOPAMIDOL

Номер: US20190077745A1
Принадлежит: BRACCO IMAGING S.P.A.

The present invention discloses a process for the preparation of Iopamidol of formula (II) 2. The method according to claim 1 , wherein X is OR.3. The method according to claim 1 , wherein X is R.5. The method according to claim 4 , wherein the boronic acid is selected from the group consisting of: phenylboronic acid claim 4 , tolylboronic acid and butylboronic acid or the boroxine (III) is selected from the group consisting of tri-phenylboroxine and tri-methylboroxine.8. The method according to claim 1 , further comprising the purification and isolation of Iopamidol (II).9. The method according to claim 8 , wherein said purification is to pharmaceutical grade. The present invention relates to the field of organic chemistry, in particular to the synthesis of iodinated contrast agents, more in particular to the use of boron oxyacids and derivatives thereof as protecting groups. The present invention provides also compounds useful as intermediates in the above synthesis.Contrast agents, or contrast media, are substances that can alter the way in which a region is analyzed in medical imaging. In particular, they are able to change the contrast of an organ, an injury, or any other surrounding structure, to make visible such details that otherwise would be difficult to detect or appreciate.Contrast agents are primarily used in the radiological or in the nuclear magnetic resonance diagnostic fields. Depending on the field of application, these derivatives present structural features, such as, in the case of molecules useful as contrast agents for X-rays analysis, the presence of one or more atom with high atomic number (e.g. iodine or barium).Iopamidol (N,N′-bis[2-hydroxy-1-(hydroxymethyl)ethyl]-5-[(2S)(2-hydroxy-1-oxopropyl)amino]-2,4,6-triiodo-1,3-benzendicarboxamide) (II), whose structural formula is indicated below, is one of the numerous tri-iodinated diagnostic agents, commercially available and widely used for this purpose:The widespread use of this compound in ...

Подробнее
22-03-2018 дата публикации

ANTI-PCSK9 COMPOUNDS AND METHODS FOR THE TREATMENT AND/OR PREVENTION OF CARDIOVASCULAR DISEASES

Номер: US20180079730A1
Принадлежит:

Disclosed are compounds that modulate the physiological action of the proprotein convertase subtilisin kexin type 9 (PCSK9), and methods of using these modulators to reduce LDL-cholesterol levels and/or for the treatment and/or prevention of cardiovascular disease (CVD), including treatment of hypercholesterolemia. 8. The method of claim 2 , wherein the compound is selected from the group consisting of [(3-chloro-4-methylphenyl)carbamoyl](phenyl)methyl 4-(carbamoylamino)benzoate (SBC-110 claim 2 ,686); N-(3-chloro-4-methylphenyl)-2-[(4-acetamidophenyl)formamido]-2-phenylacetamide (SBC-110 claim 2 ,720); and [(3-chloro-4-methylphenyl)carbamoyl](phenyl)methyl 4-acetamidobenzoate (SBC-110 claim 2 ,721).9. The method of claim 2 , wherein the compound is N-{4-[4-(4-methylphenyl)-2-phenylpiperazine-1-carbonyl]phenyl}acetamide (SBC-110 claim 2 ,736) or {4-[4-(3-chloro-4-methylphenyl)-2-phenylpiperazine-1-carbonyl]phenyl}urea (SBC-110 claim 2 ,733).10. The method of claim 2 , further comprising administering to said patient a therapeutically effective amount of a low density lipoprotein (LDL) lowering drug.11. The method of claim 10 , wherein said LDL lowering drug is a statin.12. The method of claim 6 , further comprising administering to said patient a therapeutically effective amount of a low density lipoprotein (LDL) lowering drug.13. The method of claim 12 , wherein said LDL lowering drug is a statin. This application claims the benefit of U.S. Provisional Application No. 61/789,867, filed Mar. 15, 2013, the entirety of which is incorporated herein by reference.The present invention was made with support from the National Heart, Lung and Blood Institute (NHLBI) under SBIR Grant No. HL092712. The U.S. Government has certain rights in this invention.The present invention relates to compounds that modulate the physiological action of the proprotein convertase subtilisin kexin type 9 (PCSK9), including its interaction with the low density lipoprotein receptor (LDLR). More ...

Подробнее
24-03-2016 дата публикации

Compounds which have a protective activity with respect to the action of toxins and of viruses with an intracellular mode of action

Номер: US20160083355A1

The subject matter of the present invention is novel families of compounds which are aromatic amine, imine, aminoadamantane and benzodiazepine derivatives, medicaments comprising same and the use thereof as inhibitors of the toxic effects of toxins with intracellular activity, such as, for example, ricin, and of viruses that use the internalization pathway for infecting cells.

Подробнее
23-03-2017 дата публикации

NOVEL KCNQ POTASSIUM CHANNEL AGONISTS, METHOD OF PREPARATION AND METHOD OF USE THEREOF

Номер: US20170081301A1
Принадлежит:

The present invention provides a compound represented by general formula I or a pharmaceutical acceptable salt thereof, the preparation method therefor and the use thereof in preparing a medicine for treating a neurological disease, such as epilepsy, convulsion, neuropathic pain, acute ischemic stroke, and a neurodegenerative disease. The compound according to present invention has a better absorption in brain tissue when compared with RTG. In addition, the compound provided by present invention has not only a greatly enhanced efficacy, but also a neurotoxicity greatly lower than that of RTG, and thus possesses a wider safety window. 4. The compound or pharmaceutical acceptable salt thereof according to claim 1 , wherein one of Rand Ris methyl claim 1 , and the other is H or methyl.6. The compound or pharmaceutical acceptable salt thereof according to claim 1 , wherein the pharmaceutical acceptable salts are salts formed by the compound with an acid claim 1 , and for example claim 1 , the acid is selected from a group consisting of maleic acid claim 1 , succinic acid claim 1 , citric acid claim 1 , tartaric acid claim 1 , fumaric acid claim 1 , formic acid claim 1 , acetic acid claim 1 , propanoic acid claim 1 , propandioic acid claim 1 , oxalic acid claim 1 , benzoic acid claim 1 , phthalic acid claim 1 , methanesulfonic acid claim 1 , benzenesulfonic acid claim 1 , toluenesulfonic acid claim 1 , naphthalenesulfonic acid claim 1 , 1 claim 1 ,5-naphthalenedisulfonic acid claim 1 , camphoric acid claim 1 , camphor sulfonic acid claim 1 , salicylic acid claim 1 , acetyl salicylic acid claim 1 , aspartic acid claim 1 , glutamic acid claim 1 , lactic acid claim 1 , gluconic acid claim 1 , ascorbic acid claim 1 , gallic acid claim 1 , amygdalic acid claim 1 , malic acid claim 1 , sorbic acid claim 1 , trifloroacetic acid claim 1 , taurine claim 1 , homotaurine claim 1 , isethionic acid claim 1 , cinnamic acid claim 1 , hydrochloric acid claim 1 , hydrobromic acid claim 1 ...

Подробнее
12-06-2014 дата публикации

Antagonizing Heparin With Salicylamide Compounds And Histamine Blocking Agents

Номер: US20140162955A1
Принадлежит: CELLCEUTIX CORPORATION

The present disclosure provides combinations of salicylamide compounds, or pharmaceutically acceptable salts thereof, and histamine blocking agents, or pharmaceutically acceptable salts thereof, for antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative. 2. The pharmaceutical composition of wherein n is 3 to 8.3. The pharmaceutical composition of wherein n is 3 to 5.4. The pharmaceutical composition of wherein n is 3 or 4.5. The pharmaceutical composition of wherein Ris H.9. The pharmaceutical composition of wherein each Ris claim 1 , independently claim 1 , Cto Cstraight or branched alkyl.10. The pharmaceutical composition of wherein each Ris claim 1 , independently claim 1 , Cto Cstraight alkyl.12. The pharmaceutical composition of wherein Ris OH or NH.17. The pharmaceutical composition of wherein the histamine blocking agent is chosen from diphenhydramine (Benadryl) claim 1 , cimetidine (Tagamet) claim 1 , loratadine (Claritin) claim 1 , fexofenadine (Allegra) claim 1 , chlorpheniramine (Chlor-Tripalon) claim 1 , brompheniramine (Dimetane) claim 1 , dimenhydrinate (Gravol) claim 1 , promethazine (Phenergan) claim 1 , hydroxyzine (Atarax) claim 1 , cyproheptadine (Periactin) claim 1 , azatadine (Zadine) claim 1 , and cetirizine (Reactine) claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or any combination thereof.18. The pharmaceutical composition of wherein the histamine blocking agent is diphenhydramine or cimetidine claim 1 , or a combination thereof.19. The pharmaceutical composition of wherein the salicylamide compound is present as a unit dose amount from about 5 mg to about 60 mg claim 1 , and the histamine blocking agent is present as a unit dose amount from about 10 mg to about 50 mg.20. The pharmaceutical composition of wherein the salicylamide compound is present as a unit dose amount from about 10 mg to about 50 mg claim 1 , and the histamine blocking agent is present as ...

Подробнее
12-06-2014 дата публикации

ENZYME INHIBITORS

Номер: US20140163042A1
Принадлежит: Chroma Therapeutics Ltd.

Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers, wherein Ris a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; Ris the side chain of a natural or non-natural alpha amino acid; Y is a bond, —C(═O), —S(═O)—, —C(═O)O—, —C(O)NR—, —C(═S)—NR, —C(═NH)NRor —S(═O)NR— wherein Ris hydrogen or optionally substituted C-Calkyl; Lis a divalent radical of formula -(Alk)(Q)(Alk)- wherein m, n and p are independently 0 or 1, Q is (i) an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members, or (ii), in the case where both m and p are 0, a divalent radical of formula —X-Q- or -Q-X— wherein Xis —O—, S— or NR— wherein Ris hydrogen or optionally substituted C-Calkyl, and Qis an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members, Alkand Alkindependently represent optionally substituted divalent C-Ccycloalkyl radicals, or optionally substituted straight or branched, C-Calkylene, C-Calkenylene, or C-Calkynylene radicals which may optionally contain or terminate in an ether (—O—), thioether (—S—) or amino (—NR—) link wherein Ris hydrogen or optionally substituted C-Calkyl; Xrepresents a bond; —C(═O); or —S(═O)—; —NRC(═O)—, —C(═O)NR—, —NRC(═O)NR—, —NRS(═O)—, or —S(═O)NR— wherein Rand Rare independently hydrogen or optionally substituted C-Calkyl; z is 0 or 1; A represents an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system wherein the radicals RRNH—Y-L-X-[CH]— and HONHCO-[LINKER]- are attached different ring atoms; and -[Linker]- represents a divalent linker radical linking a ring atom in A with the hydroxamic acid group CONIIOII, the length of the linker radical, from the terminal atom linked to the ring atom of A to the terminal atom linked to the ...

Подробнее
01-04-2021 дата публикации

NASAL FORMULATIONS OF METOCLOPRAMIDE

Номер: US20210093590A1
Принадлежит:

Nasal formulations of metoclopramide, which remain stable and/or colorless upon storage over a period of time, are provided. Also provided are methods of treating disorders treatable with metoclopramide, comprising administering the nasal solutions to patients in need thereof. 1. A pharmaceutical composition comprising metoclopramide , or a pharmaceutically-acceptable salt thereof , and a buffer , wherein the pharmaceutical composition has a pH of above about 4.5 , and wherein the pharmaceutical composition has less than about 2% average change in percent optical density (O.D.) per week per 200 mg/mL of metoclopramide when stored at a temperature of 40° C. and 75% relative humidity.2. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition further comprises benzalkonium chloride.3. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition has a pH of at least about 4.6.4. The pharmaceutical composition of claim 1 , wherein the buffer is selected from the group consisting of citric acid/phosphate claim 1 , acetate claim 1 , barbital claim 1 , borate claim 1 , Britton-Robinson claim 1 , cacodylate claim 1 , citrate claim 1 , collidine claim 1 , formate claim 1 , maleate claim 1 , McIlvaine claim 1 , phosphate claim 1 , Prideaux-Ward claim 1 , succinate claim 1 , citrate-phosphate-borate (Teorell-Stanhagen) claim 1 , veronal acetate claim 1 , MES (2-(N-morpholino)ethanesulfonic acid) claim 1 , BIS-TRIS (bis(2-hydroxyethyl)iminotris(hydroxymethyl)methane) claim 1 , ADA (N-(2-acetamido)-2-iminodiacetic acid) claim 1 , ACES (N-(carbamoylmethyl)-2-aminoethanesulfonaic acid) claim 1 , PIPES (piperazine-N claim 1 ,N′-bis(2-ethanesulfonic acid)) claim 1 , MOPSO (3-(N-morpholino)-2-hydroxypropanesulfonic acid) claim 1 , BIS-TRIS PROPANE (1 claim 1 ,3-bis(tris(hydroxymethyl)methylamino)propane) claim 1 , BES (N claim 1 ,N-bis(2-hydroxyethyl)-2-aminoethanesulfonaic acid) claim 1 , MOPS (3-(N-morpholino)propanesulfonic acid) ...

Подробнее
28-03-2019 дата публикации

Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto

Номер: US20190090488A1
Принадлежит: DOW AGROSCIENCES LLC

This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”). 2. A process to control a pest claim 1 , said process comprising claim 1 , applying to a locus claim 1 , a pesticidally effective amount of a molecule according to . This Application is a continuation of, and claims the benefit of, U.S. nonprovisional application Ser. No. 15/679,415, which was filed Aug. 17, 2017, and which is now allowed; Ser. No. 15/679,415 is a divisional of, and claims the benefit of, U.S. nonprovisional application Ser. No. 15/092,650, which was filed Apr. 7, 2016, and is now U.S. Pat. No. 9,781,935; Ser. No. 15/092,650 claims the benefit of, and priority from, U.S. provisional application Ser. Nos. 62/148,809; 62/148814; 62/148818; 62/148824; 62/148830; and 62/148,837; all of which were filed on Apr. 17, 2015. The entire contents of all of the above-identified applications are hereby incorporated by reference into this Application.This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides.“Many of the most dangerous human diseases are transmitted by insect vectors” (Rivero et al.). “Historically, malaria, dengue, yellow ...

Подробнее
01-04-2021 дата публикации

CARBOXAMIDES AS MODULATORS OF SODIUM CHANNELS

Номер: US20210094906A1
Принадлежит:

Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain. 4. The compound of or , or a pharmaceutically acceptable salt thereof , wherein L is O.5. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein each R is H.6. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris H , halo , OH , C-Calkyl , or C-Calkoxy.7. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris H or halo.8. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris H or C-Calkyl.9. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris H , halo , C-Calkyl , C-Chaloalkyl , or C-Calkoxy.10. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris H , halo , C-Calkyl , C-Chaloalkyl , C-Calkoxy , C-Chaloalkoxy , or —W—(CH)—R.11. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris H , halo , C-Calkyl , C-Chaloalkyl , C-Calkoxy , or —W—(CH)—R.12. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris H or OCHPh.13. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris H , halo , OH , C-Calkyl , C-Calkoxy , or —W—(CH)—R.14. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris H , halo , OH , or C-Calkoxy.15. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris H , halo , C-Calkoxy , or C-Chaloalkoxy.16. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris H , ...

Подробнее
01-04-2021 дата публикации

DRUG FOR TREATING TUMOR DISEASES AND HAVING ANTIBACTERIAL ANTIVIRUS ANTI-INFLAMMATORY EFFECTS

Номер: US20210094910A1
Автор: Qi Baowen, Shi Jianyou
Принадлежит:

The present disclosure describes an anti-cancer drug for treating tumor diseases and providing antibacterial, antivirus, and anti-inflammatory effects. The drug contains a naphthalene dicarboxamide compound with a structural formula as shown in Formula I or a biologically acceptable salt or ester form of the compound with the formula I as an active ingredient. The drug is able to help inhibit the growth of tumor cells and possesses certain antibacterial, antivirus, and anti-inflammatory effects. 2. The compound of Claim 1 , wherein the X can be carbonyl Claim 1 , thiocarbonyl Claim 1 , or sulfonyl group; Y can be carbonyl Claim 1 , thiocarbonyl Claim 1 , or sulfonyl group.3. The compound of Claim 1 , wherein X substituents are in the P position of the naphthalene ring and N substituents (connected to Y Claim 1 , shown in the formula) are in the non-substituted para-position of the naphthalene ring.4. The compound of Claim 1 , wherein R Claim 1 , Rand nitrogen atoms connected to them can form a pyrrole ring Claim 1 , tetrahydropyrrole ring Claim 1 , pyridine ring Claim 1 , tetrahydropyridine ring Claim 1 , piperidine ring Claim 1 , piperazine ring Claim 1 , oxazine ring Claim 1 , tetrahydroxazine ring Claim 1 , and morpholine ring; and when R Claim 1 , Rand annular atoms connected to them form a substituted ring structure with 3-8 ring atoms Claim 1 , the formed ring structure should be 4-methyl-piperazinyl or N-morpholinyl; or Rand Rare selected independently from hydrogen Claim 1 , Calkyl Claim 1 , Calkoxy Claim 1 , cyclopropane Claim 1 , cyclohexane Claim 1 , Calkoxycarbonyl Claim 1 , Calkylcarbonyl Claim 1 , aminocarbonyl Claim 1 , Calkylaminocarbonyl Claim 1 , nitro Claim 1 , oxazolyl Claim 1 , thiazolyl Claim 1 , pyridyl Claim 1 , dihydropyridyl Claim 1 , tetrahydropyridyl Claim 1 , piperidinyl Claim 1 , thiazinyl Claim 1 , pyrrolyl Claim 1 , imidazolyl Claim 1 , pyrazolyl Claim 1 , pyrimidinyl Claim 1 , piperazinyl Claim 1 , morpholinyl Claim 1 , furanyl Claim ...

Подробнее
28-03-2019 дата публикации

MEDICAMENT FOR LIVER REGENERATION AND FOR TREATMENT OF LIVER FAILURE

Номер: US20190091265A1
Принадлежит:

The present invention relates to the use of a compound which inhibits the activity of MKK4 as a medicament for the treatment of a patient suffering from an impaired liver function, to the use of a compound as a medicament for the treatment of liver failure, including acute/fulminant or chronic liver failure and/or for increasing the regeneration of liver tissue in a patient. 1. A method of treatment of liver failure and/or for the treatment of impaired liver function and/or for the protection of hepatocytes against apoptosis and/or for the regeneration of hepatocytes , the method comprising a step of administering to a patient in need of treatment a compound , which is an inhibitor of the activity of MKK4 , wherein said MKK4 is encoded by mRNA with SEQ ID NO: 1204 , wherein the compound is not SP600125 , myricitine , PD98059 , genistein , or ZM 336372.3. The method according to claim 1 , wherein the compound is formulated as liposomes or lipid nanoparticles.4. The method according to claim 1 , wherein the patient is a human patient.5. A cultivated hepatocyte for treatment of liver failure and/or for treatment of impaired liver function and/or for blood purification claim 1 , characterized in that the hepatocyte contains a compound which is an inhibitor of the activity of MKK4 claim 1 , wherein said MKK4 encoded by SEQ ID NO: 1204 and the compound is not SP600125 claim 1 , myricitine claim 1 , PD98059 claim 1 , genistein claim 1 , or ZM 336372.6. A medicament comprising the cultivated hepatocyte of .7. The cultivated hepatocyte of claim 5 , wherein the hepatocyte is arranged in a vessel having an entry port for entry of blood of a patient and an exit port for recirculating the blood to the patient.8. The cultivated hepatocyte of claim 5 , wherein the compound is one or more of the compounds of . This application is a continuation of U.S. patent application Ser. No. 14/875,879 filed Oct. 6, 2015, pending, which is a continuation of U.S. patent application Ser. No. 14/ ...

Подробнее
12-04-2018 дата публикации

Molecules haveing pesticidal utiliy and intermediates, compositions and processes related thereto

Номер: US20180098541A1
Принадлежит: DOW AGROSCIENCES LLC

This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).

Подробнее
04-04-2019 дата публикации

Medicament for liver regeneration and for treatment of liver failure

Номер: US20190099453A1

The present invention relates to the use of a compound which inhibits the activity of MKK4 as a medicament for the treatment of a patient suffering from an impaired liver function, to the use of a compound as a medicament for the treatment of liver failure, including acute/fulminant or chronic liver failure and/or for increasing the regeneration of liver tissue in a patient.

Подробнее
19-04-2018 дата публикации

Tricyclic Amino Containing Compounds for Treatment or Prevention of Symptoms Associated with Endocrine Dysfunction

Номер: US20180104243A1
Принадлежит:

The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes. 2. The method of claim 1 , wherein the subject is menopausal or perimenopausal woman.3. The method of claim 1 , wherein the subject is menstruating or expecting to menstruate with a week.4. The method of claim 1 , wherein the subject is a woman diagnosed with vulvodynia.5. The method of claim 1 , wherein the pharmaceutical composition is administered in combination with another active agent.6. The method of claim 1 , wherein the pharmaceutical composition is administered in combination with an agonist or antagonist of an estrogen receptor.7. The method of claim 1 , wherein the pharmaceutical composition is administered in combination with tamoxifen.8. The method of claim 1 , wherein the pharmaceucial composition is administered in combination with an antiandrogen.9. The method of claim 1 , wherein the subject is a man with prostate cancer.10. The method of Claim claim 1 , wherein the pharmaceutical composition is administered in combination with spironolactone claim 1 , cyproterone claim 1 , flutamide claim 1 , nilutamide claim 1 , bicalutamide claim 1 , finasteride claim 1 , or dutasteride.11. The method of claim 1 , wherein said compound is N-(4-((pyrimidin-2-ylamino)methyl)benzyl)-pyrimidin-2-amine or pharmaceutically acceptable salt thereof12. The method of claim 1 , further comprising the step of administering the pharmaceutical composition to the subject after claim 1 , before claim 1 , or during a surgery selected from a hysterectomy claim 1 , oophorectomy claim 1 , partial oophorectomy claim 1 , unilateral salpingo-oophorectomy claim 1 , bilaterial salpingo-oophorectomy or combination thereof.13. The use of a compound of in the production of a medicament for the treatment or prevention of hot flashes. This application claims priority to U.S. Provisional Application Number 61/ ...

Подробнее
19-04-2018 дата публикации

CYCLIC VINYLOGOUS AMIDES AS BROMODOMAIN INHIBITORS

Номер: US20180105485A1
Принадлежит: ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI

Cyclic vinylogous amides of Formula I are disclosed 137-. (canceled)39. The method of claim 38 , wherein the disease or disorder is chronic inflammation.40. The method of wherein the disease or disorder is inflammatory colitis.41. The method of claim 38 , wherein the treatment of a disease or a disorder further comprises administering an additional therapeutic agent.43. The method of claim 38 , wherein the disease or disorder is autoimmune disease.44. The method of claim 38 , wherein the disease or disorder is cancer.45. The method of claim 44 , wherein the cancer is selected from breast cancer claim 44 , triple negative breast cancer claim 44 , prostate cancer claim 44 , acute leukemia claim 44 , chronic leukemia claim 44 , chronic lymphocytic leukemia claim 44 , colon cancer claim 44 , colorectal cancer claim 44 , multiple myeloma claim 44 , glioblastoma claim 44 , lung cancer claim 44 , and liver cancer.46. The method of claim 39 , wherein the disease or disorder is selected from multiple sclerosis claim 39 , inflammatory bowel disease claim 39 , Crohn's disease claim 39 , ulcerative colitis claim 39 , type I diabetes claim 39 , rheumatoid arthritis claim 39 , AIDS claim 39 , and asthma. This application claims priority from U.S. provisional application 61/872,303, filed Aug. 30, 2013, the entire disclosure of which is incorporated herein by reference.This invention was made with U.S. Government support under R01HG004508, R01CA87658 and R33DA029963 awarded by National Institutes of Health. The U.S. Government has certain rights in the invention.The present application relates generally to compositions for treating diseases that arise from inappropriate activity of proteins containing an acetyl-lysine. The compositions comprise a genus of cyclic vinylogous amides that are inhibitors of bromodomain.BRD4 is a member of the bromodomains and extra terminal domain (BET) family of proteins that recognize acetylated chromatin structures through their bromodomains and act ...

Подробнее
03-07-2014 дата публикации

DUAL MECHANISM INHIBITORS FOR THE TREATMENT OF DISEASE

Номер: US20140187617A1
Принадлежит: AERIE PHARMACEUTICALS, INC.

Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved. 3. A compound according to claim 1 , wherein Z is a bond or —CH—.4. A compound according to claim 1 , wherein X claim 1 , Xand Xare each hydrogen.5. A compound according to claim 1 , wherein A is —CHCH—.6. A compound according to claim 1 , wherein Rand Rare independently hydrogen or methyl.7. A compound according to claim 1 , wherein Ris hydrogen or C-Calkyl.8. A pharmaceutical composition comprising a compound according to and a pharmaceutically acceptable carrier.9. A method for treating a disease in a subject comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'administering to a subject an effective amount of a compound according to ; wherein the disease comprises eye disease.'}10. The method of claim 9 , wherein the eye disease comprises glaucoma or a neurodegenerative eye disease.11. A method of modulating kinase activity comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'contacting a cell with a compound according to in an amount effective to modulate kinase activity.'}12. The method of claim 11 , wherein the cell is in a subject.13. A method of reducing intraocular pressure comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'contacting a cell with a compound according to in an amount effective to reduce intraocular pressure.'}14. The method of claim 13 , wherein the cell is in a subject. This application is a continuation of U.S. patent application Ser. No. 13/768,594 filed Feb. 15, 2013 which is a divisional of U.S. patent application Ser. No. 12/ ...

Подробнее
02-04-2020 дата публикации

Histone acetyltransferase activators and uses thereof

Номер: US20200101078A1
Принадлежит: Columbia University of New York

The invention provides compounds and compositions comprising compounds that modulate histone acyl transferase (HAT). The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tan protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a compound that modulates HAT to a subject.

Подробнее
29-04-2021 дата публикации

ARYL-N-ARYL DERIVATIVES FOR TREATING A RNA VIRUS INFECTION

Номер: US20210122732A1
Принадлежит:

A compound of formula (Ie): 115-. (canceled)18. The compound of formula (Ie) according to claim 16 , wherein R″ is a hydrogen atom or any of its pharmaceutically acceptable salt.19. The compound of formula (Ie) according to claim 16 , wherein{'sup': '1', 'sub': 1', '4', '1', '5, 'Yrepresents an aryl group selected from a phenyl group, a pyridyl group, a pyrazinyl group, a pyridazinyl or a pyrimidinyl group, the aryl group being optionally substituted by one or two substituent(s) selected from a halogen atom, a (C-C)alkyl group, a cyano group, a (C-C)alkoxy group, a trifluoromethyl group, a trifluoromethoxy group,'}or any of its pharmaceutically acceptable salt.20. The compound of formula (Ie) according to claim 16 , wherein{'sup': '2', 'Xrepresents'}a —O— group,a —NH— group,a —S— group,a —CO—NH— group,a —NH—CO—NH— group,a —NH—CO— group,a divalent 5-membered heteroaromatic ring comprising 1, 2, 3 or 4 heteroatoms such as a triazole, a tetrazole or an oxadiazole,{'sub': '2', 'a —SO— group,'}or{'sub': '2', 'a —SO—NH— group,'}or any of its pharmaceutically acceptable salt.21. The compound of formula (Ie) according to claim 16 , wherein{'sup': '2', 'Yrepresents'}a hydrogen atom,a hydroxyl group,{'sub': f', 'f', 'f', 'f', '1', '4, 'a —PO(OR)(R′) group, wherein Rand R′independently represents a hydrogen atom or a (C-C)alkyl group,'}or{'sup': 1', '2', '3', '1', '2', '3', '1', '2', '3', '1', '2', '1', '2, 'sub': 1', '4', '3', '5', '3', '5', '1', '4', '1', '4', '3', '8, 'a —CRRRgroup, wherein R, Rand Rindependently represent a hydrogen atom, a fluorine atom or a (C-C)alkyl group, being understood that no more than one of R, Rand Ris a hydrogen atom, or Rand Rform together with the carbon atom bearing them a (C-C)cycloalkyl group, the (C-C)cycloalkyl group being optionally substituted by one or two (C-C)alkyl group, halogen atom or (C-C)alkoxy group and the (C-C)cycloalkyl group being optionally interrupted on the Rand/or Rby an oxygen atom,'}or any of its pharmaceutically ...

Подробнее
13-05-2021 дата публикации

PROLYL HYDROXYLASE INHIBITORS AND METHODS OF USE

Номер: US20210137901A1
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 process of claim 33 , wherein the catalyst is [1 claim 33 ,1′-bis (diphenylphosphino)ferrocine]dichloro palladium(II).37. The process of claim 33 , wherein the reaction is conducted in the presence of a base that is KPO.38. The process of claim 34 , wherein the coupling reagents in step (c) are 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (EDCI) and 1-hydroxybenzotriazole (HOBt).39. The process of claim 34 , wherein the catalyst in step (d) is Pd/C.42. The process of claim 40 , wherein the catalyst in step (a) is [1 claim 40 ,1-bis (diphenylphosphino)ferrocine]dichloro palladium(II).43. The process of claim 40 , wherein the reaction in step (a) is conducted in the presence of a base that is KPO.44. The process of claim 40 , wherein the coupling reagents in step (c) are 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (EDCI) and 1-hydroxybenzotriazole (HOBt). This application is a Continuation Application of Ser. No. 14/854,080, filed Sep. 15, 2015, now U.S. Pat. No. 9,598,370, which is a Continuation Application of U.S. application Ser. No. 14/568,200, filed on Dec. 12, 2014, which is a Continuation Application of U.S. application Ser. No. 14/062,011, filed Oct. 24, 2013, now U.S. Pat. No. 8,940,773, which is a Divisional Application of U.S. application Ser. No. 13/681,876, filed on Nov. 20, 2012, now U.S. Pat. No. 8,598,210, which is a Continuation of U.S. application Ser. No. 12/860,073, filed on Aug. 20, 2010, now U.S. Pat. No. 8,343,952, which is a Continuation Application of U.S. application Ser. No. 11/821,936, filed Jun. 26, 2007, now U.S. Pat. No. 7,811,595, which claims the benefit of Provisional Application Ser. No. 60/816,522 filed ...

Подробнее
05-05-2016 дата публикации

Compositions and methods for the treatment of inflammatory bowel disease

Номер: US20160120838A1
Автор: Mahesh KANDULA
Принадлежит: Individual

The invention relates to the compounds of formula I and formula II 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 or formula II; and methods for treating or preventing inflammatory bowel disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of gastrointestinal diseases and inflammation such as inflammatory bowel disease, ulcerative colitis, mild-to-moderate Crohn's disease, rheumatoid arthritis, inflammatory arthritis, psoriatic arthritis, liver cirrhosis and idiopathic urticaria.

Подробнее
03-05-2018 дата публикации

SMALL MOLECULE COMPOUNDS TARGETING PBX1 TRANSCRIPTIONAL COMPLEX

Номер: US20180118688A1
Принадлежит:

In accordance with one or more embodiments, the present invention provides a compound of formulas I, II, and III, for use in methods of inhibition of PBX1-DNA interaction in a mammalian cell or population of cells, and for use in the treatment of medical conditions including but not limited to cancers, developmental disorders, inflammatory disorders, autoimmune diseases, or neuro-degenerative disorders. 7. A pharmaceutical composition comprising the compound of claim 1 , and a pharmaceutically acceptable carrier.8. A method for inhibition of PBX1-DNA interaction in a mammalian cell or population of cells claim 1 , comprising contacting the cell or population of cells with an effective amount of the compound of .9. A method for treating medical conditions in a subject in need thereof claim 1 , including but not limited to cancers claim 1 , developmental disorders claim 1 , inflammatory disorders claim 1 , autoimmune diseases claim 1 , or neuro-degenerative disorders comprising administering to the subject an effective amount of the compound of .10. A method for treating medical conditions in a subject in need thereof claim 1 , including but not limited to cancers claim 1 , developmental disorders claim 1 , inflammatory disorders claim 1 , autoimmune diseases claim 1 , or neuro-degenerative disorders comprising administering to the subject an effective amount of the compound of and an effective amount of at least one other biologically active agent.11. A method for treating medical conditions in a subject in need thereof claim 2 , including but not limited to cancers claim 2 , developmental disorders claim 2 , inflammatory disorders claim 2 , autoimmune diseases claim 2 , or neuro-degenerative disorders comprising administering to the subject an effective amount of the compound of .12. A method for treating medical conditions in a subject in need thereof claim 4 , including but not limited to cancers claim 4 , developmental disorders claim 4 , inflammatory disorders ...

Подробнее
03-05-2018 дата публикации

COMPOUNDS FOR TREATING PARASITIC INFECTIONS

Номер: US20180118704A1
Автор: HAMZA Iqbal, XUA Fengtian
Принадлежит:

Compounds and compositions comprising them are provided. The compounds and compositions are useful for inhibiting transport of heme across membranes in parasitic heme auxotrophic organisms, thereby limiting their growth or killing the parasites. 13Leishmania.. The method of claim 7 , wherein the parasitic heme auxotrophic organism is14Leishmania. The method of claim 13 , wherein is a promastigote or an amastigote.15. The method of claim 7 , wherein the inhibiting the transport of the heme is lethal to the parasitic heme auxotrophic organism.16. The method of claim 10 , wherein the inhibiting the transport of the heme is lethal to the parasitic heme auxotrophic organism.17. The method of claim 11 , wherein the inhibiting the transport of the heme is lethal to the parasitic heme auxotrophic organism.18. The method of claim 13 , wherein the inhibiting the transport of the heme is lethal to the parasitic heme auxotrophic organism20. The kit of claim 19 , further comprising instructions for using the compounds to inhibit the growth of or kill a parasitic heme auxotrophic organism.21Leishmania.. The kit of claim 19 , wherein the instructions comprise an indication that the parasitic heme auxotrophic organism is22. The method of claim 8 , wherein the inhibiting the transport of the heme is lethal to the parasitic heme auxotrophic organism.23. The method of claim 9 , wherein the inhibiting the transport of the heme is lethal to the parasitic heme auxotrophic organism.24. The method of claim 12 , wherein the inhibiting the transport of the heme is lethal to the parasitic heme auxotrophic organism. This application claims priority to U.S. patent application No. 62/157,870, filed May 6, 2015, the disclosure of which is incorporated herein by reference.The present disclosure relates generally to compounds and methods for using the compounds to kill or inhibit the growth of parasites, and more specifically for killing or inhibiting growth of parasites that are heme auxotrophs. ...

Подробнее
03-05-2018 дата публикации

SELECTIVE HDAC6 INHIBITORS

Номер: US20180118709A1
Принадлежит:

The present invention provides a compound having the structure: 3. The compound of claim 1 ,wherein{'sub': 1', '5', '6', '5', '6', '2', '7, 'claim-text': {'sub': 5', '6', '7', '1-5', '2-5', '2-5', '1-5', '1-5, 'wherein R, R, and Rand are each, independently, H, Calkyl, Calkenyl, Calkynyl, heteroalkyl, hydroxyalkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, Calkyl-aryl, or Calkyl-NH-aryl.'}, 'Ris —C(═O)—NRR, —NR—C(═O)—R, or —COR,'}4. The compound of claim 3 ,wherein{'sub': 1', '5', '6', '5', '6', '2', '1, 'claim-text': {'sub': 5', '6', '7', '1-5', '1-5', '1-5, 'wherein R, R, and Rand are each, independently, H, Calkyl, hydroxyalkyl, aryl, heteroaryl, Calkyl-aryl, or Calkyl-NH-aryl.'}, 'Ris —C(═O)—NRR, —NR—C(═O)—R, or —COR,'}5. The compound of claim 4 ,wherein{'sub': 1', '5', '6', '5', '6', '2', '7, 'claim-text': wherein', {'sub': 5', '1-5, 'Ris Calkyl, hydroxyalkyl, aryl or heteroaryl;'}, {'sub': 6', '1-5, 'Ris Calkyl, hydroxyalkyl, aryl or heteroaryl; and'}, {'sub': 7', '1-5', '1-5, 'Ris Calkyl, hydroxyalkyl, aryl, heteroaryl, or Calkyl-NH-aryl.'}], 'Ris —C(═O)—NRR, —NR—C(═O)—R, or —COR,'}6. The compound of claim 4 ,wherein{'sub': 1', '5', '6', '5', '6', '2', '7, 'claim-text': {'sub': 5', '6', '7', '2', '2', '2', '2', '2, 'wherein R, R, and Rand are each, independently, phenyl, —CHCHOH, —CH-phenyl, or —CHCHN(H)-phenyl.'}, 'Ris —C(═O)—NRR, —NR—C(═O)—R, or —COR,'}14. A pharmaceutical composition comprising the compound of any one of - and a pharmaceutically acceptable carrier.15. A method of inhibiting the activity of a histone deacetylase in a cell comprising contacting the histone deacetylase with the compound of any one of - so as to inhibit the activity of the histone deacetylase.16. The method of claim 15 , wherein the histone deacetylase is HDAC6.17. A method of treating a neurodegenerative disease in a subject comprising administering an effective amount of the compound of any one of - to the subject so as to treat the neurodegenerative disease in the ...

Подробнее
16-04-2020 дата публикации

HISTONE ACETYLTRANSFERASE ACTIVATORS AND USES THEREOF

Номер: US20200115325A1
Принадлежит:

The invention provides for a method for screening compounds that bind to and modulate a histone acetyltransferase protein. The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a HAT-activating compound to a subject. 2. The method of claim 1 , wherein the subject exhibits abnormally elevated levels of amyloid beta plaques.3. The method of claim 1 , wherein the subject is afflicted with Alzheimer's disease claim 1 , Lewy body dementia claim 1 , inclusion body myositis claim 1 , or cerebral amyloid angiopathy.4. The method of claim 1 , wherein the Aβ protein deposit comprises an Aβ40 isomer claim 1 , an Aβ42 isomer claim 1 , or a combination thereof.6. A method for treating Alzheimer's Disease claim 1 , the method comprising administering to a subject a therapeutic amount of a pharmaceutical composition comprising a HAT activator compound.13. A method for ameliorating symptoms of Parkinson's Disease claim 1 , the method comprising administering to a subject a therapeutic amount of a pharmaceutical composition comprising a HAT activator compound.15. A method for treating Huntington's Disease claim 1 , the method comprising administering to a subject a therapeutic amount of a pharmaceutical composition comprising a HAT activator compound.16. The method of claim 1 , wherein the effective amount is at least about 1 mg/kg body weight claim 1 , at least about 2 mg/kg body weight claim 1 , at least about 3 mg/kg body weight claim 1 , at least about 4 mg/kg body weight claim 1 , at least about 5 mg/kg body weight claim 1 , at least about 6 mg/kg body weight claim 1 , at least about 7 mg/kg body weight claim 1 , at least about 8 mg/kg body weight claim 1 , at least about 9 mg/kg body weight claim 1 , at least about 10 mg/kg body weight claim 1 , at least about 15 mg/kg body weight claim 1 ...

Подробнее
16-04-2020 дата публикации

COMPOUNDS AND METHODS OF TREATING RNA-MEDIATED DISEASES

Номер: US20200115372A1
Принадлежит:

The present invention provides compounds, compositions thereof, and methods of using the same. 4. The compound of claim 2 , wherein Ligand is selected from the group consisting of a macrolide claim 2 , an alkaloid claim 2 , an aminoglycoside claim 2 , a tetracycline claim 2 , a SMN2 ligand selected from those shown in claim 2 , a pleuromutilin claim 2 , theophylline or an analogue thereof claim 2 , ribocil or an analogue thereof claim 2 , a substituted anthracene claim 2 , a substituted triptycene claim 2 , an oxazolidinone claim 2 , and CPNQ or an analogue thereof; wherein Ligand may be optionally substituted with one or more substituents.5. The compound of claim 2 , wherein Ligand is selected from the group consisting of erythromycin claim 2 , azithromycin claim 2 , berberine claim 2 , palmatine claim 2 , a paromomycin claim 2 , a neomycin claim 2 , a kanamycin claim 2 , doxycycline claim 2 , oxytetracycline claim 2 , pleuromutilin claim 2 , theophylline or an analogue thereof claim 2 , ribocil or an analogue thereof claim 2 , NVS-SM1 claim 2 , a substituted anthracene claim 2 , a substituted triptycene claim 2 , linezolid claim 2 , tedizolid claim 2 , and CPNQ or an analogue thereof; wherein Ligand may be optionally substituted with 1 claim 2 , 2 claim 2 , 3 claim 2 , or 4 substituents.6. The compound of claim 4 , wherein Tis selected from those shown in .7. The compound of claim 4 , wherein Tis selected from a polyethylene glycol (PEG) group claim 4 , an optionally substituted Caliphatic group claim 4 , or a peptide comprising 1-8 amino acids.8. The compound of claim 3 , wherein Tis selected from those shown in .9. The compound of claim 2 , wherein Ris selected from sulfonyl halides claim 2 , arenecarbonyl imidazoles claim 2 , active esters claim 2 , epoxides claim 2 , oxiranes claim 2 , oxidizing agents claim 2 , aldehydes claim 2 , alkyl halides claim 2 , benzyl halides claim 2 , or isocyanates; wherein Rreacts with an unconstrained 2′-hydroxyl group of a ...

Подробнее
12-05-2016 дата публикации

CYCLOPROPANEAMINE COMPOUND

Номер: US20160130215A1
Принадлежит:

The present invention provides a compound having a lysine-specific demethylase 1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for cancer, and central nervous system diseases, and the like. The present invention relates to a compound represented by the formula 2. The compound according to claim 1 , whereinA is{'sub': '3-8', '(1) a Ccycloalkyl group optionally having substituent(s),'}{'sub': '6-14', '(2) a Caryl group optionally having substituent(s),'}{'sub': 6-14', '1-6, '(3) a Caryl Calkyl group optionally having substituent(s),'}{'sub': 6-14', '1-6', '6-14, '(4) a Caryl Calkyl Caryl group optionally having substituent(s),'}(5) a 4- to 11-membered heterocyclic group containing, as a ring-constituting atom besides carbon atom, 1 to 3 hetero atoms selected from a nitrogen atom, a sulfur atom and an oxygen atom, and optionally having substituent(s), or{'sub': '10-14', '(6) a Ccyclic hydrocarbon group optionally having substituent(s);'}{'sub': '1-6', 'R is a hydrogen atom or a Calkyl group optionally having substituent(s); or'}A and R are optionally bonded to each other to form a 4- to 10-membered heterocycle optionally having substituent(s), or a salt thereof.3. The compound according to claim 1 , wherein{'sup': '1', 'sub': '1-6', 'Qis a hydrogen atom or a Calkyl group, and'}{'sup': 2', '3', '4, 'Q, Qand Qare each a hydrogen atom,'}or a salt thereof.4. The compound according to claim 1 , wherein{'sub': '1-6', 'X is a hydrogen atom or an optionally substituted Calkyl group;'}{'sup': 1', '2', '3, 'Y, Yand Yare each independently'}(1) a hydrogen atom,{'sub': '1-20', '(2) a Calkyl group optionally having substituent(s),'}{'sub': '3-8', '(3) a Ccycloalkyl group optionally having substituent(s),'}{'sub': '6-14', '(4) a Caryl group optionally having substituent(s),'}{'sub': 6-14', '1-6, '(5) a Caryl Calkyl group optionally having substituent(s),'}(6) a 5- to 7-membered monocyclic aromatic heterocyclic group containing, as a ring- ...

Подробнее
14-05-2015 дата публикации

COMPOSITIONS AND METHODS FOR THE TREATMENT OF RESPIRATORY DISORDERS

Номер: US20150133407A1
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 respiratory disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of viscid or excessive mucus, cough, inflammation, redness in sore throat, infection in the throat, sore throat, abnormal mucus secretion, impaired mucus transport, allergic rhinitis, asthma, COPD, respiratory muscular disorders and pain in acute sore throat. 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 respiratory disorders related diseases as the underlying etiology claim 3 , wherein the method comprises administering to a patient in need thereof an effective amount of .5. The method of claim 4 , wherein the respiratory disorders as the underlying etiology is selected from viscid or excessive mucus claim 4 , cough claim 4 , inflammation claim 4 , redness in sore throat claim 4 , infection in the throat claim 4 , sore throat claim 4 , abnormal mucus secretion claim 4 , impaired mucus transport claim 4 , allergic rhinitis claim 4 , asthma claim 4 , COPD claim 4 , respiratory muscular ...

Подробнее
03-06-2021 дата публикации

MOLECULES HAVING PESTICIDAL UTILITY, AND INTERMEDIATES, COMPOSITIONS, AND PROCESSES, RELATED THERETO

Номер: US20210161144A1
Принадлежит: DOW AGROSCIENCES LLC

This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”). 2. A composition according to wherein said active ingredient is Abamectin.3. A composition according to wherein said active ingredient is Acephate.4. A composition according to wherein said active ingredient is Acetamiprid.5. A composition according to wherein said active ingredient is Afidopyropen.6. A composition according to wherein said active ingredient is Bifenthrin.7. A composition according to wherein said active ingredient is Chlorantraniliprole.8. A composition according to wherein said active ingredient is Chlorfenapyr.9. A composition according to wherein said active ingredient is Cyantraniliprole.10. A composition according to wherein said active ingredient is Dinotefuran.11. A composition according to wherein said active ingredient is Emamectin Benzoate.12. A composition according to wherein said active ingredient is Ethiprole.13. A composition according to wherein said active ingredient is Fluxametamide.14. A composition according to wherein said active ingredient is Imidacloprid.15. A composition according to wherein said active ingredient is Methoxyfenozide.16. A composition according to wherein said active ingredient is Oxamyl.17. A composition according to wherein said active ingredient is Pyriproxyfen.18. A composition according to wherein said active ingredient is Spinetoram.19. A composition according to wherein said active ingredient is Spiromesifen.20. A composition according to wherein said active ingredient is ...

Подробнее
02-05-2019 дата публикации

BETA- AND GAMMA-AMINO-ISOQUINOLINE AMIDE COMPOUNDS AND SUBSTITUTED BENZAMIDE COMPOUNDS

Номер: US20190127346A1
Принадлежит:

Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds. 125-. (canceled)27. The method of claim 26 , wherein one of Rand Ris aryl or heteroaryl.28. The method of claim 26 , wherein the eye disease comprises glaucoma.29. The method of claim 26 , wherein the eye disease comprises a neurodegenerative eye disease.30. The method of claim 26 , wherein the composition is a pharmaceutical composition further comprising a pharmaceutically acceptable carrier.31. The method of claim 30 , wherein the pharmaceutically acceptable carrier is saline buffered to a pH of about 5.5 to about 6.5.32. The method of claim 30 , wherein one of Rand Ris aryl or heteroaryl.33. The method of claim 30 , wherein the eye disease comprises glaucoma.34. The method of claim 30 , wherein the eye disease comprises a neurodegenerative eye disease.36. The compound of claim 35 , wherein one of Rand Ris aryl or heteroaryl.37. The method of claim 35 , wherein the cell is in a subject.38. The method of claim 35 , wherein the composition is a pharmaceutical composition further comprising a pharmaceutically acceptable carrier.39. The method of claim 38 , wherein the pharmaceutically acceptable carrier is saline buffered to a pH of about 5.5 to about 6.5.40. The compound of claim 38 , wherein one of Rand Ris aryl or heteroaryl.41. The method of claim 38 , wherein the cell is in a subject.43. The compound of claim 42 , wherein one of Rand ...

Подробнее
03-06-2021 дата публикации

OPIOID RECEPTOR MODULATORS AND PRODUCTS AND METHODS RELATED THERETO

Номер: US20210163402A1
Принадлежит:

Compounds are provided having the structure of Formula (I): 1100-. (canceled)102. The compound of claim 101 , or a pharmaceutically acceptable isomer claim 101 , racemate claim 101 , hydrate claim 101 , solvate claim 101 , isotope claim 101 , or salt thereof claim 101 , wherein:ring A is phenyl, pyridinyl, or pyrazinyl;{'sub': 3', '7, 'sup': '7', 'ring C is a C-Ccycloalkyl or 3-7 membered heterocycloalkyl, substituted with 0-5 R;'}{'sup': 1', '2, 'Rand Rare each, independently, H, methyl, ethyl, isopropyl or cyclopropyl, substituted with 0-3 halo;'}{'sup': 3', '4, 'sub': 1', '6', '1', '6, 'Rand Rare each, independently, H, (C-C)alkyl, (C-C)haloalkyl, or cyclopropylmethyl;'}{'sup': 5', '1', '2', '3', '5, 'sub': 1', '6', '1', '6', '1', '6, 'each Ris independently —C(O)NRR, —OH, halo, (C-C)alkyl, (C-C)haloalkyl, (C-C)alkoxy, or carbocycle; or Rand one R, together with the atoms to which they are connected, form a 5-7 membered heterocycle;'}{'sup': '6', 'sub': 1', '6', '1', '6', '1', '6, 'each Ris independently halo, (C-C)alkyl, (C-C)haloalkyl, (C-C)alkoxy, or carbocycle;'}{'sup': '7', 'sub': 1', '6', '1', '6', '1', '6, 'each Ris independently halo, (C-C)alkyl, (C-C)haloalkyl, (C-C)alkoxy, or carbocycle;'}{'sup': '8', 'Ris H;'}m is 1-3; andn is 0-3.103. The compound of claim 102 , or a pharmaceutically acceptable isomer claim 102 , racemate claim 102 , hydrate claim 102 , solvate claim 102 , isotope claim 102 , or salt thereof claim 102 , wherein ring A is phenyl.104. The compound of claim 103 , or a pharmaceutically acceptable isomer claim 103 , racemate claim 103 , hydrate claim 103 , solvate claim 103 , isotope claim 103 , or salt thereof claim 103 , wherein ring B is phenyl claim 103 , indazolyl claim 103 , 2 claim 103 ,3-dihydrobenzoxazolyl claim 103 , benzoxazolonyl claim 103 , or pyrazolopyridinyl.105. The compound of claim 104 , or a pharmaceutically acceptable isomer claim 104 , racemate claim 104 , hydrate claim 104 , solvate claim 104 , isotope claim 104 , or ...

Подробнее
17-05-2018 дата публикации

NOVEL KCNQ POTASSIUM CHANNEL AGONIST, AND PREPARATION METHOD THEREFOR AND USE THEREOF

Номер: US20180134677A1
Принадлежит:

The present invention provides a compound represented by general formula I or a pharmaceutical acceptable salt thereof, the preparation method therefor and the use thereof in preparing a medicine for treating a neurological disease, such as epilepsy, convulsion, neuropathic pain, acute ischemic stroke, and a neurodegenerative disease. The compound according to present invention has a better absorption in brain tissue when compared with RTG. In addition, the compound provided by present invention has not only a greatly enhanced efficacy, but also a neurotoxicity greatly lower than that of RTG, and thus possesses a wider safety window. 2. The method according to claim 1 , wherein claim 1 ,{'sub': 2', '3', '2', '3, 'Rand Rare each independently selected from a group consisting of H and D, or Rand Rtogether with the carbon atom to which they attached form cyclopropyl;'}{'sub': 4', '5', '1', '4', '1', '4, 'one of Rand Ris C-Calkyl, and the other is H or C-Calkyl.'}4. The method according to claim 3 , wherein claim 3 ,{'sub': '1', 'Ris H or fluorine;'}{'sub': 2', '3', '2', '3, 'Rand Rare each independently selected from a group consisting of H and D, or Rand Rtogether with the carbon atom to which they attached form cyclopropyl;'}{'sub': 4', '5', '1', '4', '1', '4, 'one of Rand Ris C-Calkyl, and the other is H or C-Calkyl.'}8. The method according to claim 1 , wherein one of Rand Ris methyl claim 1 , and the other is H or methyl.9. The method according to claim 1 , wherein the pharmaceutical acceptable salt is a salt formed by reacting the compound with an acid.10. The method according to claim 9 , wherein the acid is selected from a group consisting of maleic acid claim 9 , succinic acid claim 9 , citric acid claim 9 , tartaric acid claim 9 , fumaric acid claim 9 , formic acid claim 9 , acetic acid claim 9 , propanoic acid claim 9 , propandioic acid claim 9 , oxalic acid claim 9 , benzoic acid claim 9 , phthalic acid claim 9 , methanesulfonic acid claim 9 , ...

Подробнее
17-05-2018 дата публикации

AMIDE DERIVATIVES, PROCESS FOR PREPARATION THEREOF AND USE THEREOF AS INSECTICIDE

Номер: US20180134681A1
Принадлежит:

An object of the present invention is to provide a compound represented by Formula (1): 114-. (canceled) The present invention relates to a compound represented by Formula (1):wherein A, A, Aand Aeach represent a carbon atom, a nitrogen atom or an oxidized nitrogen atom;Rand Reach represent a hydrogen atom, an optionally substituted alkyl group or an optionally substituted C1-C4 alkylcarbonyl group;Gand Geach represent an oxygen atom or a sulfur atom;X, which may be identical or different, represents a hydrogen atom, a halogen atom, a C1-C3 alkyl group or a trifluoromethyl group;n is an integer of 0 to 4; andQand Qeach represent an optionally substituted phenyl group, an optionally substituted naphthyl group or an optionally substituted heterocyclic group,an insecticide comprising the compound as the active ingredient, and a process for preparation thereof and use thereof.International Publication WO 2000/55120 and U.S. Pat. No. 6,548,514 describe a compound similar to the compound of the present invention for the use as medicament, but they do not describe on the insecticidal activity of the compound. The compound clearly does not fall within the scope of claims of the present invention.International Publication WO 2000/7980 describes a compound similar to the compound of the present invention for the use as medicament, but it does not describe on the insecticidal activity of the compound. The compound clearly does not fall within the scope of claims of the present invention.US Patent Laid-Open No. 2002-032238 describes a compound similar to the compound of the present invention for the use as medicament, but it does not describe on the insecticidal activity of the compound. The compound clearly does not fall within the scope of claims of the present invention.The object of the present invention is to provide a pesticide having a high insecticidal efficacy. Another object of the present invention is to provide a compound represented by Formula (1), a process for ...

Подробнее
17-05-2018 дата публикации

COMPOUNDS AND METHODS OF TREATING OCULAR DISORDERS

Номер: US20180134714A1
Принадлежит:

A method of treating an ocular disorder in a subject associated with aberrant all-trans-retinal clearance in the retina, the method comprising administering to the subject a therapeutically effective amount of a primary amine compound of formula: 2. The method of claim 1 , wherein Ris an aliphatic compound.3. The method of claim 1 , wherein Ris an aromatic compound.4. The method of claim 1 , wherein the primary amine compound does not inhibit RPE65 enzymatic activity or any other proteins involved in retinoid metabolism in the eye of the subject.5. The method of claim 1 , wherein the primary amine compound reduces the formation of A2E and/or retinal dimer in the subject's retina.6. The method of claim 1 , wherein the primary amine compound is delivered to the subject by at least one of topical administration claim 1 , systemic administration claim 1 , intravitreal injection claim 1 , oral administration claim 1 , and intraocular delivery.7. The method of claim 1 , wherein the primary amine compound does not cause night blindness in the subject.13. The method of claim 1 , wherein the primary amine compound is selected from the group consisting of (S)-3-(Aminomethyl)-5-methylhexanoic acid claim 1 , (R)-3-(Aminomethyl)-5-methylhexanoic acid claim 1 , and racemic mixtures thereof.14. The method of claim 1 , wherein the primary amine compound administered to the subject includes less than about 1% by weight (S)-3-(Aminomethyl)-5-methylhexanoic acid and greater than about 99% by weight (R)-3-(Aminomethyl)-5-methylhexanoic acid.15. The method of claim 1 , wherein the primary amine compound administered to the subject includes less than about 1% by weight (R)-3-(Aminomethyl)-5-methylhexanoic acid and greater than about 99% by weight (S)-3-(Aminomethyl)-5-methylhexanoic acid.16. The method of claim 1 , wherein the retinal pathology is macular degeneration claim 1 , Stargardt's disease claim 1 , geographic atrophy claim 1 , Leber's congenital amaurosis claim 1 , and retinitis ...

Подробнее
18-05-2017 дата публикации

6-AMINO-5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL OR 3-AMINOCHROMAN-7-YL DERIVATIVES

Номер: US20170137416A1
Принадлежит: Hoffmann-La Roche Inc.

The present invention relates to compounds TAAR receptor antagonists of formula I wherein X, R, L, Ar and Rare as described herein, compositions containing compounds of formula I, methods of manufacture of compounds of formula I and methods of treating psychiatric disorders with compounds of formula I. 2. The compound according to wherein L is —C(O)NH—.3. The compound according to claim 2 , said compound selected from the group consisting of:N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-2-(trifluoromethyl)isonicotinamide;N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-4-bromo-5-cyclopropyl-1H-pyrazole-3-carboxamide;N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-1-(2,2-difluoroethyl)-5-propyl-1H-pyrazole-3-carboxamide;(R)—N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-1-(2,2-difluoroethyl)-5-propyl-1H-pyrazole-3-carboxamide;(S)—N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-1-(2,2-difluoroethyl)-5-propyl-1H-pyrazole-3-carboxamide;(R)—N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-6-methyl-2-(trifluoromethyl)-pyrimidine-4-carboxamide;(S)—N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-6-methyl-2-(trifluoromethyl)-pyrimidine-4-carboxamide;N-(3-aminochroman-7-yl)-1-(2,2-difluoroethyl)-5-propyl-1H-pyrazole-3-carboxamide;N-(3-aminochroman-7-yl)-6-methyl-2-(trifluoromethyl)pyrimidine-4-carboxamide;(R)—N-(3-aminochroman-7-yl)-1-(2,2-difluoroethyl)-5-propyl-1H-pyrazole-3-carboxamide;(S)—N-(3-aminochroman-7-yl)-1-(2,2-difluoroethyl)-5-propyl-1H-pyrazole-3-carboxamide;(R)—N-(3-aminochroman-7-yl)-6-methyl-2-(trifluoromethyl)pyrimidine-4-carboxamide;(S)—N-(3-aminochroman-7-yl)-6-methyl-2-(trifluoromethyl)pyrimidine-4-carboxamide;(R)—N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-4-chlorobenzamide;(R)—N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-2-chlorobenzamide;(S)—N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-2-methylisonicotinamide;(S)-2-acetamido-N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)isonicotinamide;(S)—N-(6-amino-5,6,7,8-tetrahydronaphthalen-2-yl)-2-ethoxyisonicotinamide;(S ...

Подробнее
07-08-2014 дата публикации

NOVEL HISTONE DEACETYLASE INHIBITOR OF BENZAMIDES AND USE THEREOF

Номер: US20140221431A1
Принадлежит:

Disclosed in the present invention is a novel histone deacetylase inhibitor of benzamides and use thereof. The inhibitor has good efficacy in treating diseases caused by abnormal gene expression, such as tumours, endocrine disorders, immune system diseases, genetic diseases and nerve system diseases. The histone deacetylase inhibitor of benzamides is a compound of the following general chemical structural formula (I) or a salt thereof. 2. The novel histone deacetylase inhibitor of benzamides according to claim 1 , characterized in that claim 1 , the C-Calkyl is methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , n-butyl claim 1 , isobutyl or tert-butyl.3. The novel histone deacetylase inhibitor of benzamides according to claim 1 , characterized in that claim 1 , the C-Calkoxy is methoxy claim 1 , ethoxy claim 1 , n-propoxy claim 1 , isopropoxy claim 1 , n-butoxy or isobutoxy.4. The novel histone deacetylase inhibitor of benzamides according to claim 1 , characterized in that claim 1 , the C-Caminoalkyl is aminoethyl claim 1 , 1-aminopropyl or 2-aminopropyl.5. The novel histone deacetylase inhibitor of benzamides according to claim 1 , characterized in that claim 1 , the C-Calkylamino is N-methylamino claim 1 , N-ethylamino or N-isopropylamino.6. The novel histone deacetylase inhibitor of benzamides according to claim 1 , characterized in that claim 1 , the C-Cacyl is acetyl claim 1 , propionyl or isobutyryl.7. The novel histone deacetylase inhibitor of benzamides according to claim 1 , characterized in that claim 1 , the C-Camido is acetamido claim 1 , propionamido claim 1 , butanamido or isobutanamido.8. The novel histone deacetylase inhibitor of benzamides according to claim 1 , characterized in that claim 1 , the C-Cthioalkyl is methylthio claim 1 , ethylthio or propylthio.9. The novel histone deacetylase inhibitor of benzamides according to claim 1 , characterized in that claim 1 , the C-Calkyl is methyl claim 1 , ethyl claim 1 , n-propyl ...

Подробнее
08-09-2022 дата публикации

COMPOUNDS AND METHODS OF TREATING RNA-MEDIATED DISEASES

Номер: US20220281860A1
Принадлежит:

The present invention provides compounds, compositions thereof, and methods of using the same. 117-. (canceled)19. The method of claim 18 , wherein the Ligand is a kanamycin claim 18 , a paromomycin claim 18 , or a neomycin claim 18 , or an analog thereof claim 18 , wherein the Ligand is optionally substituted with 1 claim 18 , 2 claim 18 , or 3 substituents.20. The method of claim 18 , wherein the Ligand is kanamycin A claim 18 , paromomycin claim 18 , or neomycin B claim 18 , or an analog thereof claim 18 , wherein the Ligand is optionally substituted with 1 claim 18 , 2 claim 18 , or 3 substituents.22. The method of claim 18 , wherein Tis selected from a polyethylene glycol (PEG) group claim 18 , an optionally substituted Caliphatic group claim 18 , or a peptide comprising 1-8 amino acids.23. The method of claim 18 , wherein Ris selected from sulfonyl halides claim 18 , acyl imidazoles claim 18 , aryl esters claim 18 , heteroaryl esters claim 18 , epoxides claim 18 , alkyl halides claim 18 , benzyl halides claim 18 , and isocyanates.24. The method of claim 18 , wherein Ris selected from 1-methyl-7-nitroisatoic anhydride (1M7) claim 18 , benzoyl cyanide (BzCN) claim 18 , 2-methylnicotinic acid imidazolide (NAI) claim 18 , and 2-methyl-3-furoic acid imidazolide (FAI).26. The method of claim 25 , wherein the target RNA is an mRNA claim 25 , and the method comprises modulating the downstream protein expression associated with the mRNA.27. The method of claim 26 , wherein the compound irreversibly inhibits the activity of the mRNA.28. The method of claim 26 , wherein the Ligand is a kanamycin claim 26 , a paromomycin claim 26 , or a neomycin claim 26 , or an analog thereof claim 26 , wherein the Ligand is optionally substituted with 1 claim 26 , 2 claim 26 , or 3 substituents.29. The method of claim 26 , wherein the Ligand is kanamycin A claim 26 , paromomycin claim 26 , or neomycin B claim 26 , or an analog thereof claim 26 , wherein the Ligand is optionally ...

Подробнее
30-04-2020 дата публикации

DUAL MECHANISM INHIBITORS FOR THE TREATMENT OF DISEASE

Номер: US20200131171A1
Принадлежит:

Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved. 1. A method of treating glaucoma or ocular hypertension , comprising administration of a composition comprising a Rho kinase inhibitor and a pharmaceutically acceptable carrier to a subject in need thereof ,wherein the administration is daily administration, weekly administration, or monthly administration.2. The method of claim 1 , wherein the administration is ocular administration.3. The method of claim 1 , wherein the amount of the Rho kinase inhibitor administered is about 0.001 to about 100 mg/kg subject body weight.4. The method of claim 1 , wherein the administration is daily administration once daily claim 1 , twice per day claim 1 , or 4 times per day.5. The method of claim 2 , wherein the administration is daily administration once daily claim 2 , twice per day claim 2 , or 4 times per day.6. The method of claim 3 , wherein the administration is daily administration once daily claim 3 , twice per day claim 3 , or 4 times per day.7. The method of claim 1 , wherein the administration is weekly administration once weekly or twice weekly.8. The method of claim 2 , wherein the administration is weekly administration once weekly or twice weekly.9. The method of claim 3 , wherein the administration is weekly administration once weekly or twice weekly.10. The method of claim 1 , wherein the administration is monthly administration once a month.11. The method of claim 2 , wherein the administration is monthly administration once a month.12. The method of claim 3 , wherein the ...

Подробнее