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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 10447. Отображено 100.
12-01-2012 дата публикации

Acetylene derivatives having mglur 5 antagonistic activity

Номер: US20120010263A1
Автор: Fabrizio Gasparini, Kasper Zimmerman, Silvio Ofner, Terance William Hart, Yves Auberson
Принадлежит: Individual

The invention provides compounds of formula I wherein n, A, R, R′, R″, R O , X and Y are as defined in the description, and their preparation. The compounds of formula I are useful as pharmaceuticals.

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Номер записи: 1
12-01-2012 дата публикации

Modulation of anxiety through blockade of anandamide hydrolysis

Номер: US20120010283A1
Автор: Andrea Duranti, Andrea Tontini, Daniele Piomelli, Giorgio Tarzia, Marco Mor
Принадлежит: Universita degli Studi di Parma, Universita degli Studi di Urbino "Carlo Bo", UNIVERSITY OF CALIFORNIA

Fatty acid amide hydrolase inhibitors of the Formula: are provided wherein X is NH, CH 2 , O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R 1 and R 2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R 1 and R 2 is absent, and that if Z is N, optionally R 1 and R 2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which they are each attached. Pharmaceutical compositions comprising the compounds of Formula I and methods of using them to inhibit FAAH and/or treat appetite disorders, glaucoma, pain, insomnia, and neurological and psychological disorders including anxiety disorders, epilepsy, and depression are provided.

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Номер записи: 2
23-02-2012 дата публикации

Diacylethylenediamine compound

Номер: US20120046292A1
Автор: Hiroki Fukudome, Hiroshi Moritani, Takahiro Nigawara, Takeshi Hanazawa, Tomoaki Kawano, Yasuhiro Yonetoku
Принадлежит: Astellas Pharma Inc

[Problem] A compound which is useful as an anti-obesity agent is provided. [Means for Solution] The present inventors have investigated a compound having a DGAT1 inhibitory action, which is promising as an active ingredient of a pharmaceutical composition for treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases, and as a result, they have found that the diacylethylenediamine compound of the present invention has an excellent DGAT1 inhibitory action, thereby completing the present invention. That is, the diacylethylenediamine compound of the present invention has a DGAT1 inhibitory action, and can be therefore used as an agent for preventing and/or treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases.

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Номер записи: 3
15-03-2012 дата публикации

Peptidomimetic protease inhibitors

Номер: US20120064034A1
Автор: Cristina Garcia-Paredes, Deqi Guo, Frantz Victor, Ivan Collado, Jason Eric Lamar, John Irvin Glass, LING Jin, Luc Farmer, Mark Joseph Tebbe, Nancy June Snyder, Q. May Wang, Raymond Samuel Parker, Iii, Robert B. Perni, Robert Edward Babine, Shu Hui Chen, Xicheng David Sun, Yvonne Yee Mai Yip
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.

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Номер записи: 4
22-03-2012 дата публикации

Methods for Treating Cognitive/Attention Deficit Disorders Using Tetrahydroindolone Analogues and Derivatives

Номер: US20120070385A1
Автор: Alvin J. Glasky, David B. Fick, David Helton
Принадлежит: Spectrum Pharmaceuticals Inc

The present specification discloses tetrahydroindolone derivatives or analogues and methods for treating cognitive/attention deficit disorders using such tetrahydroindolone derivatives and analogues.

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Номер записи: 5
22-03-2012 дата публикации

Estrogen receptor modulators and uses thereof

Номер: US20120071535A1
Автор: Andiliy G. Lai, Celine Bonnefous, Jackaline D. Julien, Johnny Y. Nagasawa, Mehmet Kahraman, Nicholas D. Smith, Steven P. Govek
Принадлежит: Aragon Pharmaceuticals Inc

Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

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Номер записи: 6
19-04-2012 дата публикации

Organic Compounds Having Cooling Properties

Номер: US20120095042A1
Автор: Stefan Michael Furrer
Принадлежит: Givaudan SA

Provided are compounds of formula (I) wherein m is 0, 1 or 2; R I is a mono- or bicyclic heterocyclic ring system including one, two or three heteroatoms selected from nitrogen, sulphur and oxygen; R 2 is selected from hydrogen, methyl and ethyl; I) R 3 is hydrogen, methyl, or ethyl; and R 4 and R 5 are independently selected from ethyl and isopropyl; and R 3 , R 4 and R 5 together have at least 6 carbon atoms: or II) any two or all of R 3 , R 4 and R 5 form together with the carbon atom to which they are attached 3-para-menthyl, bornyl, or adamantyl; having cooling properties, their use as cooling agent and compositions including them.

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Номер записи: 7
23-08-2012 дата публикации

New compounds, pharmaceutical compositions and uses thereof

Номер: US20120214785A1
Автор: Bernd Nosse, Gerald Juergen Roth, Heike Neubauer, Joerg Kley, Martin Fleck, Niklas Heine, Thorsten Lehmann-Lintz
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.

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Номер записи: 8
06-09-2012 дата публикации

Compositions and methods useful for treating diseases

Номер: US20120225851A1
Автор: Andrew F. Kolodziej, Michael H. Cardone, Xiang Y. Yu
Принадлежит: Eutropics Pharmaceuticals Inc

The present invention relates to a chemotherapeutic cancer treatment in which compounds of Formula Ia′, Ib′, Ic′, or II′ (referred to as a group as BH3Is) are administered to a mammal for the treatment of B-cell Lymphoma or other hematopoietic cancers, including diseases associated with MCL-1. In another aspect, the invention provides a method for treating particular types of hematopoietic cancers, such as B-cell lymphoma, using a combination of one or more compounds selected from the group consisting of compounds or Formula Ia, Ib, Ic, or II in combination with other therapies, for example, a class of therapeutics known as 26S proteosome inhibitors, such as, for example, Bortezomib. In another aspect the present invention relates to autoimmune treatment with pharmaceutical compositions comprising one or more compounds of Formula Ia′, Ib′, Ic′, or II′. In another aspect, this invention relates to methods for identifying compounds, for example, compounds of the BH3 mimic class, that have unique in vitro properties that predict in vivo efficacy against B-cell lymphoma tumors and other cancers as well as autoimmune disease.

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Номер записи: 9
08-11-2012 дата публикации

Association between 4-benzamide and an acetylcholinesterase inhibitor, and pharmaceutical compositions containing it

Номер: US20120283244A1
Автор: Aurore Sors, Caryn Trocme-Thibierge, Florence Keime-Guibert
Принадлежит: Laboratoires Servier SAS

Association between 4-{3-[cis-hexahydrocyclopenta[c]pyrrol-2(1H)-yl]propoxy}benzamide of formula (I): or an addition salt thereof with a pharmaceutically acceptable acid or base, and an acetylcholinesterase inhibitor. Medicinal products containing the same which are useful in the treatment of cognitive disturbances associated with cerebral ageing and with neurodegenerative diseases.

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Номер записи: 10
08-11-2012 дата публикации

[4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-[7-fluoro-1-(2-methoxy-ethyl)-4-trifluoromethoxy-1h-indol-3-yl]-methanone as an inhibitor of mast cell tryptase

Номер: US20120283445A1
Автор: Adam W. Sledeski, Gregory Bernard Poli, John J. Shay, Jr., Nakyen Choy, Patrick Wai-Kwok Shum, Yong Mi Choi-Sledeski
Принадлежит: SANOFI SA

The present invention is directed to an indole benzylamine compound of formula I: useful as an inhibitor of tryptase. In addition, the present invention is directed to the use of the compound for treating a patient suffering from, or subject to, a physiological condition in need of amelioration by inhibition of tryptase, comprising administering to the patient of a therapeutically effective amount of the compound, and to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula I, and a pharmaceutically acceptable carrier.

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Номер записи: 11
10-01-2013 дата публикации

Fluorine-free fused ring heteroaromatic photoacid generators and resist compositions containing the same

Номер: US20130011788A1
Автор: Pushkara R. Varanasi, Sen Liu
Принадлежит: International Business Machines Corp

The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.

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Номер записи: 12
10-01-2013 дата публикации

Fluorine-free fused ring heteroaromatic photoacid generators and resist compositions containing the same

Номер: US20130011793A1
Автор: Pushkara R. Varanasi, Sen Liu
Принадлежит: International Business Machines Corp

The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.

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Номер записи: 13
21-02-2013 дата публикации

Compositions and Methods for Enhancing Proteasome Activity

Номер: US20130045992A1
Автор: Byung-Hoon Lee, Daniel J. Finley, Min J. Lee, Randall W. King, Timothy C. Gahman
Принадлежит: Harvard College

Proteinopathies result from the proteasome not acting efficiently enough to eliminate harmful proteins and prevent the formation of the pathogenic aggregates. As described herein, inhibition of proteasome-associated deubiquitinase Usp 14 results in increased proteasome efficiency. The present invention therefore provides novel compositions and methods for inhibition of Usp14, enhancement of proteasome activity and treatment of proteinopathies.

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Номер записи: 14
28-03-2013 дата публикации

USES OF SELECTIVE INHIBITORS OF HDAC8 FOR TREATMENT OF INFLAMMATORY CONDITIONS

Номер: US20130078215A1
Автор: Balasubramanian Sriram, Buggy Joseph J., Steggerda Susanne M.
Принадлежит: Pharmacyclics, Inc.

Described herein are methods for treating a subject suffering from an inflammatory, autoimmune, or heteroimmune condition by administering to the subject a pharmaceutical composition containing a therapeutically effective amount of a compound that is a selective inhibitor of histone deacetylase 8. Also described herein are methods for decreasing secretion of pro-inflammatory cytokines by administering an HDAC8-selective inhibitor compound. Further described herein are methods for predicting responsiveness to treatments for inflammatory conditions. Methods for predicting efficacy of treatments for inflammatory conditions are also described. 1. A method for treating an inflammatory condition in a subject in need thereof , comprising administering to the subject a composition containing a therapeutically effective amount of a selective inhibitor of histone deacetylase 8 activity.2. The method of claim 1 , wherein (a) the secretion of IL-1β in a sample taken from the subject is inhibited by at least 40% claim 1 , and/or (b) the swelling on the skin of the subject decreases by at least 30% after administering the therapeutically effective amount of the selective inhibitor of histone deacetylase 8 activity.3. The method of claim 1 , wherein the inflammatory condition is a skin inflammatory condition claim 1 , autoimmune condition claim 1 , or heteroimmune condition.4. The method of claim 1 , wherein the inflammatory condition is rheumatoid arthritis or psoriasis.5. The method of claim 1 , wherein the subject is refractory or intolerant to at least one other treatment for an inflammatory condition.6. The method of claim 1 , wherein the composition is administered in combination with an additional anti-inflammatory agent.7. The method of claim 6 , wherein the additional anti-inflammatory agent is an immunosuppressant claim 6 , glucocorticoid claim 6 , non-steroidal anti-inflammatory drug claim 6 , Cox-2 specific inhibitor claim 6 , leflunomide claim 6 , gold thioglucose ...

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Номер записи: 15
04-04-2013 дата публикации

CATIONIC 6-AMINOINDOLINES, DYEING COMPOSITIONS CONTAINING THEM, PROCESSES AND USES THEREOF

Номер: US20130081213A1
Автор: Fadli Aziz
Принадлежит:

The present invention relates to a cationic 6-aminoindoline of general formula (I), the addition salts thereof with an acid and the solvates thereof: the present invention is also directed towards a method for synthesizing this cationic 6-aminoindoline, the compositions, the uses, the hair dyeing methods and the devices using this cationic 6-aminoindoline. 2. Cationic 6-aminoindoline according to claim 1 , in which the cationic radical is a tri(hydroxy)(C-C)alkylammonium radical selected from trimethylammonium claim 1 , triethylammonium claim 1 , dimethylethylammonium claim 1 , diethylmethylammonium claim 1 , diisopropylmethylammonium claim 1 , diethylpropylammonium claim 1 , beta-hydroxyethyldiethylammonium claim 1 , dimethyl-beta-hydroxyethylammonium claim 1 , di-beta-hydroxyethylmethylammonium and tri-beta-hydroxyethylammonium radicals.3. Cationic 6-aminoindoline according to claim 1 , in which the cationic radical is a cationic heterocyclic radical selected from imidazolium claim 1 , pyridinium claim 1 , piperazinium claim 1 , pyrrolidinium claim 1 , morpholinium claim 1 , pyrimidinium claim 1 , thiazolium claim 1 , benzimidazolium claim 1 , benzothiazolium claim 1 , oxazolium claim 1 , benzotriazolium claim 1 , pyrazolium claim 1 , triazolium claim 1 , benzoxazolium and piperidinium radicals.4. Cationic 6-aminoindoline according to claim 1 , in which B represents a covalent bond or a carbonyl radical CO claim 1 , AKrepresents a saturated linear C-Chydrocarbon-based chain claim 1 , p is equal to 0 claim 1 , and CAT is selected from imidazolium claim 1 , piperazinium claim 1 , pyrrolidinium claim 1 , morpholinium or piperidinium radicals claim 1 , optionally substituted with a C-Calkyl radical; the following radicals: piperidine claim 1 , pyrrolidine claim 1 , morpholine claim 1 , substituted with a methyltrimethylammonium claim 1 , methyldiethylmethylammonium claim 1 , methyl(N-methylpyrrolidinium) or trimethylammonium radical; and trimethylammonium claim 1 , ...

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Номер записи: 16
25-04-2013 дата публикации

BIARYL OXYACETIC ACID COMPOUNDS

Номер: US20130102609A1
Автор: Babu Suresh, Dong Guizhen, Duo Jingqi, Ho Koc-Kan, Le Thuy X.H., Mcguinness Brian F., Saionz Kurt W.
Принадлежит: LIGAND PHARMACEUTICALS INC.

The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin. The compounds provided include those of the general formula I: 2. A compound or salt according to wherein R claim 1 , R claim 1 , Rand Rare each independently selected from hydrogen and methyl.3. (canceled)4. A compound or salt according to claim 1 , wherein Ris selected from hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , propyl and isopropyl.5. (canceled)6. A compound or salt according to claim 1 , wherein Ris selected from aryl and heteroaryl claim 1 , each optionally substituted with one to four substituents independently selected from halogen claim 1 , cyano claim 1 , (C-C) haloalkyl claim 1 , (C-C) alkoxy claim 1 , (C-C) haloalkoxy claim 1 , (C-C) alkyl claim 1 , and (C-C) alkylsulfonyl.9. A compound or salt according to claim 8 , wherein Ris selected from hydrogen claim 8 , methyl claim 8 , fluoro claim 8 , chloro claim 8 , cyano claim 8 , —CFand methoxy; and Ris selected from hydrogen claim 8 , fluoro claim 8 , chloro claim 8 , methyl claim 8 , methoxy claim 8 , cyano claim 8 , —CFand —SOCH.10. A compound or salt according to wherein Rand Rare each independently selected from fluoro claim 9 , chloro claim 9 , methoxy and hydrogen.11. (canceled)13. A compound or salt according to wherein Ris selected from naphthyl claim 6 , pyridinyl and quinolinyl claim 6 , each optionally substituted with one to four substituents independently selected from halogen claim 6 , cyano claim 6 , (C-C) haloalkyl claim 6 , (C-C) alkoxy claim 6 , (C-C) haloalkoxy claim 6 , (C-C) alkyl and alkylsulfonyl.14. A compound or salt according to claim 1 , wherein Rand Rare each hydrogen.15. A compound or salt according to claim 1 , wherein A is selected from phenyl claim 1 , pyridinyl claim 1 , benzimidazolyl claim 1 , quinolinyl claim 1 , indolyl claim 1 , pyrimidinyl and imidazopyridinyl.16. A compound ...

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Номер записи: 17
25-04-2013 дата публикации

NOVEL CURING AGENTS

Номер: US20130102756A1
Автор: Cawse John
Принадлежит: Hexcel Composites Limited

A curable resin comprising a compound having the structure (I): wherein each carbon 2, together with either its carbon 1 or carbon 3, arc members of a fused cycloaliphatic ring, and when carbon 1 is a member of the ring so is N, and wherein each of the aliphatic or aromatic ring-member carbons may either be members of further fused cycloaliphatic rings or be bonded to a group selected from H or linear or branched Cto Calkyl. 2. A curable resin according to claim 1 , wherein any carbons forming part of any further fused cycloaliphatic rings are also bonded to either an H or linear or branched Cto Calkyl.3. A curable resin according to claim 1 , wherein each of the aliphatic or aromatic ring-member carbons claim 1 , which are not members of a fused cycloaliphatic ring claim 1 , are bonded to an H or linear or branched Cto Calkyl.4. A curable resin according to claim 1 , wherein the compound has a molecular weight of no greater than 600.5. A curable resin according to claim 1 , wherein the fused cycloaliphatic rings comprise five or six carbons.8. A curable resin according to claim 1 , wherein carbon 2 is a member of two fused cycloaliphatic rings claim 1 , one with carbon 1 and the other with carbon 3.9. A curable resin according to claim 1 , having a melting point of from 80° C. to 200° C.10. A curable resin according to claim 1 , wherein the resin is an epoxy or urethane.11. A curable resin according to claim 1 , comprising a fibre reinforcement.12. A curable resin according to claim 11 , which is a prepreg claim 11 ,13. A cured resin made by exposing a curable resin according to to elevated temperature.14. A cured resin according to claim 13 , which has a glass transition temperature of greater than 100° C.15. A cured resin according to which forms part of a structural member of an aerospace structure. The present invention relates to novel resin curing agents, particularly for epoxy and urethane resins.Curable resin systems are widely known and have a wide range ...

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Номер записи: 18
02-05-2013 дата публикации

GPR120 RECEPTOR AGONISTS AND USES THEREOF

Номер: US20130109734A1
Автор: Chen Xin, Ma Jingyuan, Nashashibi Imad Fayek, Novack Aaron, PHAM PHUONGLY, Rabbat Christopher J., Shi Dong Fang, Song Jiangao
Принадлежит: Metabolex, Inc.

GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control. 125.-. (canceled)26. A compound selected from the group consisting of:3-(4-((5-fluoro-1-(methoxycarbonyl)-2,2-dimethylindolin-7-yl)methoxy)-2,3-dimethylphenyl)propanoic acid;3-(4-((5-fluoro-2,2-dimethylindolin-7-yl)methoxy)-2,3-dimethylphenyl)propanoic acid; and3-(4-((5-fluoro-1,2,2-trimethylindolin-7-yl)methoxy)-2,3-dimethylphenyl)propanoic acid,or a pharmaceutically acceptable salt thereof.27. A composition comprising a compound of and a pharmaceutically acceptable carrier.28. A method of treating a disease or condition selected from the group consisting of Type I diabetes claim 26 , Type II diabetes and metabolic syndrome claim 26 , said method comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of .29. The method of claim 28 , wherein said disease is Type II diabetes.30. A method of lowering blood glucose in a mammal claim 26 , said method comprising administering a therapeutically effective amount of a compound of to a mammal in need of such treatment.31. The method of claim 30 , wherein said mammal is a human. Diabetes mellitus can be divided into two clinical syndromes, Type I and Type II diabetes mellitus. Type I diabetes, or insulin-dependent diabetes mellitus, is a chronic autoimmune disease characterized by the extensive loss of beta cells in the pancreatic islets of Langerhans (hereinafter referred to as “pancreatic islet cells” or “islet cells”), which produce insulin. As these cells are progressively destroyed, the amount of secreted insulin decreases, eventually leading to hyperglycemia (abnormally high level of glucose in the blood) when the amount secreted drops below the level required for euglycemia (normal blood glucose level). Although the exact trigger for this immune response is not known, patients with Type I ...

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Номер записи: 19
16-05-2013 дата публикации

ALLOSTERIC BINDING COMPOUNDS

Номер: US20130123326A1
Автор: Jensen Henrik Helligsø, Neubauer Henrik Amtoft, Wiborg Ove Kjaer
Принадлежит:

The present invention relates to allosteric binding compounds of formula (I), especially for the treatment of CNS disorders, together with pharmaceutical compositions and methods of treatment including these compounds. 2. The method according to claim 1 , comprising administering the compound of formula (I) wherein A is an aryl ring.35.-. (canceled)6. The method according to claim 1 , comprising administering the compound of formula (I) claim 1 , wherein B is a 6-membered cycloalkyl claim 1 , aryl claim 1 , or heteroaryl ring claim 1 , which ring together with A forms an annulated ring system.78.-. (canceled)9. The method according to claim 1 , comprising administering the compound of formula (I) claim 1 , wherein B is a 5-membered heteroaryl ring claim 1 , which ring together with A forms an annulated ring system.1011.-. (canceled)14. (canceled)15. The method according to claim 1 , comprising administering the compound of formula (I) claim 1 , wherein Lis selected from the group consisting of —O— claim 1 , —NH— claim 1 , and —NR—.16. The method according to claim 15 , wherein Ris Calkyl.17. The method according to claim 16 , wherein Ris selected from the group consisting of methyl claim 16 , ethyl claim 16 , propyl claim 16 , isopropyl claim 16 , butyl claim 16 , iso-butyl claim 16 , sec-butyl claim 16 , and tert-butyl.1821.-. (canceled)22. The method according to claim 1 , comprising administering the compound of formula (I) claim 1 , wherein Ris selected from the group consisting of Calkyl claim 1 , Calkoxy claim 1 , Calkenyl claim 1 , Calkynyl claim 1 , and —NH—Calkyl claim 1 , where any of these optionally is substituted with one or more substituents.23. (canceled)24. The method according to claim 22 , wherein Ris Calkyl claim 22 , wherein the alkyl optionally is substituted with one or more substituents.2527.-. (canceled)29. The method according to claim 28 , wherein Lis selected from the group consisting of —O— and —S—.3038.-. (canceled)39. The method ...

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Номер записи: 20
23-05-2013 дата публикации

CATIONIC LIPID

Номер: US20130129811A1
Автор: Era Tomohiro, Kuboyama Takeshi, Naoi Tomoyuki
Принадлежит:

The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) 2. The cationic lipid according to claim 1 , wherein Xand Xare combined together to form a single bond or alkylene.3. The cationic lipid according to claim 1 , wherein Lis a single bond claim 1 , Ris a hydrogen atom claim 1 , methyl claim 1 , pyrrolidin-3-yl claim 1 , piperidin-3-yl claim 1 , piperidin-4-yl claim 1 , or alkyl having 1 to 6 carbon atoms or alkenyl having 3 to 6 carbon atoms substituted with 1 to 3 substituent(s) claim 1 , which is(are) claim 1 , the same or different claim 1 , amino claim 1 , monoalkylamino claim 1 , dialkylamino claim 1 , trialkylammonio claim 1 , hydroxy claim 1 , alkoxy claim 1 , carbamoyl claim 1 , monoalkylcarbamoyl claim 1 , dialkylcarbamoyl claim 1 , pyrrolidinyl claim 1 , piperidyl or morpholinyl claim 1 , and Land Lare —O—.4. The cationic lipid according to claim 1 , wherein Lis —CO— or —CO—O— claim 1 , Ris pyrrolidin-3-yl claim 1 , piperidin-3-yl claim 1 , piperidin-4-yl claim 1 , or alkyl having 1 to 6 carbon atoms or alkenyl having 3 to 6 carbon atoms substituted with 1 to 3 substituent(s) claim 1 , which is(are) claim 1 , the same or different claim 1 , amino claim 1 , monoalkylamino claim 1 , dialkylamino claim 1 , trialkylammonio claim 1 , hydroxy claim 1 , alkoxy claim 1 , carbamoyl claim 1 , monoalkylcarbamoyl claim 1 , dialkylcarbamoyl claim 1 , pyrrolidinyl claim 1 , piperidyl or morpholinyl claim 1 , wherein at least one of the substituents is amino claim 1 , monoalkylamino claim 1 , dialkylamino claim 1 , trialkylammonio claim 1 , pyrrolidinyl claim 1 , piperidyl or morpholinyl claim 1 , and Land Lare identically —CO—O— or —O—CO—.5. The cationic lipid according to any one of to claim 1 , wherein Xis absent claim 1 , or is methyl.64. The cationic lipid according to any one of to claims 1 , wherein Land Lare —O— or —O—CO— claims 1 , and Rand Rare (Z)-hexadec-6-enyl or (Z)-hexadec ...

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Номер записи: 21
23-05-2013 дата публикации

Novel Estrogen Receptor Ligands

Номер: US20130131061A1
Автор: Apelqvist Theresa, Cheng Aiping, Kallin Elisabet, Rhönnstad Patrik, Wennerstål Mattias
Принадлежит: KARO BIO AB

The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R, R, R, Rand Rare as defined in the specification. 125.-. (canceled)27. A method as claimed in claim 26 , in which each Ris independently selected from the group consisting of hydrogen claim 26 , Calkyl claim 26 , Calkenyl claim 26 , Calkynyl claim 26 , Ccycloalkyl claim 26 , phenyl and benzyl.28. A method as claimed in claim 27 , in which each Rindependently represents hydrogen or Calkyl.29. A method as claimed in claim 26 , in which each Ris independently selected from the group consisting of hydrogen and Calkyl.30. A method as claimed in claim 26 , in which is selected from the group consisting of OR claim 26 , N(R) claim 26 , —C(O)Calkyl claim 26 , Calkyl claim 26 , Calkenyl claim 26 , Calkynyl claim 26 , haloCalkyl claim 26 , dihaloCalkyl claim 26 , trihaloCalkyl claim 26 , haloCalkenyl claim 26 , dihaloCalkenyl claim 26 , trihaloCalkenyl claim 26 , phenyl claim 26 , and 5-6 membered heterocyclyl claim 26 , wherein said phenyl or heterocyclyl group can either be unsubstituted or substituted by 1 to 3 substituents selected from the group consisting of OR claim 26 , halogen claim 26 , cyano claim 26 , —C(O)Calkyl claim 26 , Calkyl claim 26 , Calkenyl claim 26 , Calkynyl claim 26 , haloCalkyl claim 26 , dihaloCalkyl and trihaloCalkyl.31. A method as claimed in claim 30 , in which Ris selected from the group consisting of OR claim 30 , N(R) claim 30 , —C(O)Calkyl claim 30 , Calkyl claim 30 , Calkenyl claim 30 , Calkynyl claim 30 , phenyl claim 30 , and 5-6 membered heterocyclyl claim 30 , wherein said phenyl or ...

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Номер записи: 22
30-05-2013 дата публикации

BENZENE, PYRIDINE, AND PYRIDAZINE DERIVATIVES

Номер: US20130137686A1
Автор: Barta Thomas, Eaves Jeron, Geng Lifeng, Hanson Gunnar, Hinkley Lindsay, Huang Kenneth He, Veal James
Принадлежит:

Disclosed are compounds and pharmaceutically acceptable salts of Formula I 2. A compound according to claim 1 , wherein Qis C—R.3. A compound according to claim 1 , wherein Xis N.46-. (canceled)9. A compound according to claim 8 , wherein Xis N.10. A compound according to claim 9 , wherein{'sub': 3', '4', '1', 'Z1, 'claim-text': [{'sub': '1', 'Zis —O— or —NH—;'}, {'sub': Z1', '1', '14', '22', '2, 'claim-text': {'sub': Z1', '1', '10', '1', '10', '2', '10', '2', '10', '1', '6', '2', '1', '6', '2', '2', '2', '1', '6', '2', '2', '1', '6', '2', '1', '6', '2', '10', '2', '10', '1', '10', '1', '10', '23, 'wherein Ris optionally substituted at any available position with C-Calkyl, C-Chaloalkyl, C-Calkenyl, C-Calkynyl, hydroxy, carboxy, carboxamido, oxo, halo, amino, cyano, nitro, —SH, —S—(C-C)alkyl, —SO—(C-C)alkyl, —SONH, —SONH—(C-C)alkyl, —SONH-aryl, —SO-aryl, —SO—(C-C)alkyl, —SO-aryl, C-Calkoxy, C-Calkenyloxy, C-Calkynyloxy, mono- or di-(C-C)alkylamino, —OC-Calkyl-Z, or R.'}, 'Ris a C-Calkyl group where up to five of the carbon atoms in the alkyl group are optionally replaced independently by R, carbonyl, ethenyl, ethynyl or a moiety selected from N, O, S, SO, or SO, with the proviso that two O atoms, two S atoms, or an O and S atom are not immediately adjacent each other,'}], 'Rand Rare independently hydrogen, halo, or —ZR, wherein'}11. A compound according to claim 9 , wherein{'sub': '4', 'Ris H; and'}{'sub': 3', '1', 'Z1, 'claim-text': [{'sub': '1', 'Zis —O— or —NH—;'}, {'sub': Z1', '1', '14', '22', '2, 'claim-text': {'sub': Z1', '1', '10', '1', '10', '2', '10', '2', '10', '1', '6', '2', '1', '6', '2', '2', '2', '1', '6', '2', '2', '1', '6', '2', '1', '6', '2', '10', '2', '10', '1', '10', '1', '10', '23, 'wherein Ris optionally substituted at any available position with C-Calkyl, C-Chaloalkyl, C-Calkenyl, C-Calkynyl, hydroxy, carboxy, carboxamido, oxo, halo, amino, cyano, nitro, —SH, —S—(C-C)alkyl, —SO—(C-C)alkyl, —SONH, —SONH—(C—O)alkyl, —SONH-aryl, —SO-aryl, —SO—(C-C ...

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Номер записи: 23
06-06-2013 дата публикации

Novel hydroxamates as therapeutic agents

Номер: US20130142758A1
Автор: Chitra Baskaran, Erik J. Verner, James Robinson, Joseph J. Buggy, Martin Sendzik
Принадлежит: Pharmacyclics LLC

The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.

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Номер записи: 24
13-06-2013 дата публикации

Autotaxin inhibitors and uses thereof

Номер: US20130150326A1
Автор: Deborah Volkots, Jeffrey Roger Roppe, John Howard Hutchinson, Nicholas Simon Stock, Timothy Andrew Parr
Принадлежит: Amira Pharmaceuticals Inc

Described herein are compounds that are inhibitors of autotaxin. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such inhibitors, alone and in combination with other compounds, for treating autotaxin-dependent or autotaxin-mediated conditions or diseases.

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Номер записи: 25
20-06-2013 дата публикации

MANUFACTURE, COMPOSITIONS AND USES OF COAGULATION FACTOR VIIa MODULATOR

Номер: US20130158089A1
Автор: David Loury, Tarak Mody
Принадлежит: Pharmacyclics LLC

Treatment of cancer and thromboembolic disorders using inhibitors of Factor VIIa are disclosed herein using a compound of Formula I:

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Номер записи: 26
20-06-2013 дата публикации

(AZA)INDOLE DERIVATIVE SUBSTITUTED IN POSITION 5, PHARMACEUTICAL COMPOSITION COMPRISING IT, INTERMEDIATE COMPOUNDS AND PREPARATION PROCESS THEREFOR

Номер: US20130158269A1
Автор: ALISI Maria Alessandra, CAZZOLLA Nicola, Coletta Isabella, DRAGONE Patrizia, FURLOTTI Guido, Garofalo Barbara, GARRONE Beatrice, MANGANO Giorgina, MAUGERI Caterina
Принадлежит: AZIENDE CHIMICHE RIUNITE ANGELIN FRANCESCO A.C.R.A.F. S.P.A.

An (aza)indole derivative substituted in position 5, of formula (I) in which X, Y, Z, G1, G2, G3, R1, W, and R2 have the meanings given in the description, a pharmaceutical composition comprising it, and also intermediate compounds and a preparation process therefor. 125-. (canceled)27. An intermediate compound according to claim 26 , wherein R1 is:{'sub': 1', '3', '1', '3', '2', 'n', '2', 'n', '2', 'n', '2', 'n', '2', 'n', '2', '2', 'n', '2', '2', 'n', '2', '1', '3', '1', '3', '1', '3, 'sup': I', 'II', 'III', 'II', 'III', 'I', 'II', 'I', 'I', 'II', 'I', 'I', 'I', 'II', 'III, 'a (C-C)alkyl, (C-C)alkylOR, (CH)NRR, (CH)CONRR, (CH)COR, (CH)COOR, (CH)OCOR, SOR, (CH)NRSOR, or (CH)SORgroup, optionally substituted with 1 to 3 hydroxy groups, wherein n is an integer from 1 to 4, Ris a (C-C)alkyl or (C-C)alkylOH group, and Rand R, which may be identical or different, are a hydrogen atom or a (C-C)alkyl group; or'}{'sub': 1', '3', '1', '3', '2', 'n', '2', 'n', '2', 'n', '2', 'n', '2', '2', 'n', '2', '2', 'n', '2', '3', '2', '5', '2', '2', '4', '3', '2', '5, 'sup': I', 'II', 'III', 'I', 'II', 'I', 'I', 'II', 'I', 'I', 'I', 'II', 'III, 'a (C-C)alkyl, (C-CalkylOR, (CH)CONRR, (CH)COR, (CH)COOR, (CH)OCOR, SOR, (CH)NRSOR, or (CH)SORgroup, optionally substituted with 1 to 3 hydroxy groups, wherein n is an integer from 1 to 3, Ris a CH, CH, CHOH, a CHOH group, and Rand R, which may be identical or different, are a hydrogen atom or a CH, CHgroup.'}28. An intermediate compound according to claim 26 , wherein W is:{'sub': 1', '3', '1', '4', '1', '3', '2', '3', '2', 'p', '2', 'q', '2', 'p', '2', 'q, 'a σ bond, a (C-C)alkyl, (C-C)alkenyl, O(C-C)alkyl, O(C-C)alkenyl, C(O)NH, (CH)CO(CH), or (CH)C(OH)(CH)group, wherein p and q, which may be identical or different, are an integer from 1 to 3; or'}{'sub': 2', '2', '4', '2', '2', '4', '2', 'p', '2', 'q', '2', 'p', '2', 'q, 'a σ bond, a CH, CH, CH═CH, OCH, OCH, OCH═CH, C(O)NH, (CH)CO(CH), or (CH)C(OH)(CH)group, wherein p and q, which may be ...

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Номер записи: 27
18-07-2013 дата публикации

Methods for Treating Parkinson's Disease Using Pro-Neurogenic Compounds

Номер: US20130184271A1
Автор: De Brabander Jef K., McKnight Steven L., Pieper Andrew A., Ready Joseph M.
Принадлежит: Board of Regents of the University of Texas System

This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like. 2. The method of claim 1 , wherein when A is CRR claim 1 , the carbon attached to Rand Ris substituted with four different substituents claim 1 , and is (R) or (S) configured.3. The method of claim 2 , wherein the compound or salt is (+) (dextrorotatory) or (−) (levororotatory).4. The method of claim 1 , wherein the effective amount of the compound or salt stimulates neurogenesis.5. The method of claim 1 , wherein the effective amount of the compound or salt reduces neuron cell death.6. The method of claim 1 , wherein the compound is selected from:R-1-(3,6-Dibromo-9H-carbazol-9-yl)-3-(3-methoxyphenylamino)-propan-2-ol;S-1-(3,6-Dibromo-9H-carbazol-9-yl)-3-(3-methoxyphenylamino)-propan-2-ol;1-(3,6-dibromo-9H-carbazol-9-yl)-3-(2-iminopyridin-[(2H)-yl)propan-2-ol;1-(3,6-dibromo-9H-carbazol-9-yl)-3-(phenylthio)propan-2-ol;N-(3-(3,6-dibromo-9H-carbazol-9-yl)-2-hydroxypropyl)-N-(3-methoxyphenyl)acetamide;5-((3,6-dibromo-9H-carbazol-9-yl)methyl)-3-(3-methoxyphenyl)-oxazolidin-2-one;N-(3-(3,6-dibromo-9H-carbazol-9-yl)-2- ...

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Номер записи: 28
18-07-2013 дата публикации

Methods of Treating Post-Traumatic Stress Disorder Using Pro-Neurogenic Compounds

Номер: US20130184301A1
Автор: De Brabander Jef K., McKnight Steven L., Pieper Andrew A., Ready Joseph M.
Принадлежит: Board of Regents of the University of Texas System

This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protecting from neuron cell death. 2. The method of claim 1 , wherein when A is CRR claim 1 , the carbon attached to Rand Ris substituted with four different substituents claim 1 , and is (R) or (S) configured.3. The method of claim 2 , wherein the compound or salt is (+) (dextrorotatory) or (−) (levororotatory).4. The method of claim 1 , wherein the effective amount of the compound or salt stimulates neurogenesis.5. The method of claim 1 , wherein the effective amount of the compound or salt reduces neuron cell death.6. The method of claim 1 , wherein the compound is selected from:R-1-(3,6-Dibromo-9H-carbazol-9-yl)-3-(3-methoxyphenylamino)-propan-2-ol;S-1-(3,6-Dibromo-9H-carbazol-9-yl)-3-(3-methoxyphenylamino)-propan-2-ol;1-(3,6-dibromo-9H-carbazol-9-yl)-3-(2-iminopyridin-1(2H)-yl)propan-2-ol;1-(3,6-dibromo-9H-carbazol-9-yl)-3-(phenylthio)propan-2-ol;N-(3-(3,6-dibromo-9H-carbazol-9-yl)-2-hydroxypropyl)-N-(3-methoxyphenyl)acetamide;5-((3,6-dibromo-9H-carbazol-9-yl)methyl)-3-(3-methoxyphenyl)-oxazolidin-2-one;N-(3-(3,6-dibromo-9H-carbazol-9-yl)-2-fluoropropyl)-3-methoxyaniline;1-(3,6-dibromo-9H-carbazol-9-yl)-3-(3-methoxyphenylamino)-propan-2-one;N-(3-(3,6-dibromo-9H-carbazol-9-yl)-2-methoxypropyl)-3-methoxyaniline;1-(3,6-Dimethyl-9H-carbazol-9-yl)-3-(3-methoxyphenylamino)propan-2-ol;1-(3-Bromo-6-methyl-9H-carbazol-9-yl)-3-(3-methoxyphenylamino)-propan-2-ol;1-(3,6-Dichloro-9H-carbazol-9-yl)-3-(3-methoxyphenylamino)propan-2-ol;1-(5-bromo-2,3-dimethyl-1H-indol-1-yl)-3-(phenylamino)propan-2-ol;1-(3,6-Dibromo-9H-pyrido[3,4-b]indol-9-yl)-3-(phenylamino)propan-2-ol;1-(3-Azidophenylamino)-3-(3,6-dibromo-9H-carbazol-9-yl)propan-2-ol;1,3-Bis(3,6-dibromo-9H-carbazol-9-yl)propan-2-ol;1-(9H-Carbazol-9-yl)-3-(3,6-dibromo-9H-carbazol-9-yl)propan-2-ol;3-(3,6-Dibromo-9H-carbazol-9-yl)-2-hydroxy-N-(3-methoxyphenyl)-propanamide;Ethyl 5-(2-Hydroxy- ...

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Номер записи: 29
18-07-2013 дата публикации

Compounds acting at multiple prostaglandin receptors giving a general anti-inflammatory response

Номер: US20130184463A1
Автор: David F. Woodward, Jenny W. Wang, Jose L. Martos, Jussi J. Kangasmetsa, William R. Carling
Принадлежит: Allergan Inc

The present invention provides a compound, that is a 1-({halo-2-[(2-hydrocarbyl or substituted hydrocarbyl)oxy]phenyl}methyl)-(fused bicyclic nitrogen heteroaryl) carboxylic acid or an ester or sulfonamide thereof. The compound may be represented by the following formula Wherein R 1 , R 2 , R 3 , R 4 A, X, W, Z and Y are as defined in the specification. The compounds may be administered to treat DP, FP, EP1, TP and/or EP4 receptor-mediated diseases or conditions.

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Номер записи: 30
25-07-2013 дата публикации

Pro-Neurogenic Compounds

Номер: US20130190339A1
Автор: De Brabander Jef K., McKnight Steven L., Pieper Andrew A., Ready Joseph M.
Принадлежит: Board of Regents of the University of Texas System

This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protecting from neuron cell death. 2. The compound or salt of claim 1 , wherein A is:{'sup': A1', 'A2', 'A1', 'A2', '9', '9, 'sub': 1', '3', '1', '3', '1', '3, '(i) CRR, wherein each of Rand Ris independently selected from hydrogen, halo, C-Calkyl, and OR, wherein Ris hydrogen or C-Calkyl that is optionally substituted with hydroxyl or C-Calkoxy; or'}(ii) C═O.3. The compound or salt of claim 1 , wherein A is CRR claim 1 , wherein each of Rand Ris claim 1 , independently claim 1 , hydrogen claim 1 , halo claim 1 , C-Calkyl claim 1 , or OR.4. The compound or salt of claim 3 , wherein one of Rand Ris independently selected from hydrogen claim 3 , halo claim 3 , C-Calkyl claim 3 , and OR; and the other of Rand Ris independently selected from halo claim 3 , C-Calkyl claim 3 , and OR.5. The compound or salt of claim 4 , wherein one of Rand Ris halo claim 4 , and the other of Rand Ris hydrogen claim 4 , halo claim 4 , or C-Calkyl.6. The compound or salt of claim 5 , wherein one of Rand Ris fluoro claim 5 , and the other of Rand Ris hydrogen or fluoro.7. The compound or salt of claim 3 , wherein one of Rand Ris OR; and the other of Rand Ris C-Calkyl.8. The compound or salt of claim 7 , wherein one of Rand Ris OH; and the other of Rand Ris CH.9. The compound or salt of claim 3 , wherein the carbon attached to Rand Ris substituted with four different substituents claim 3 , and is (R) or (S) configured.10. The compound or salt of claim 9 , wherein the formula (I) compound is (+) (dextrorotatory) or (−) (levororotatory).11. The compound or salt of claim 1 , wherein Ris selected from halo claim 1 , hydroxyl claim 1 , sulfhydryl claim 1 , C-Calkoxy claim 1 , C-Cthioalkoxy claim 1 , C-Chaloalkoxy claim 1 , C-Cthiohaloalkoxy claim 1 , C-Calkyl claim 1 , C-Chaloalkyl claim 1 , C-Calkynyl claim 1 , cyclopropyl claim 1 , —N claim 1 , cyano claim 1 ...

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Номер записи: 31
25-07-2013 дата публикации

APOPTOSIS PROMOTERS

Номер: US20130190488A1
Автор: Bruncko Milan, Ding Hong, Elmore Steven, Kunzer Aaron, Lynch Christopher L., McClellan William, Mitten Michael, Park Cheol-Min, Petros Andrew, Shoemaker Alexander, Song Xiaohong, Tu Noah, Wang Xilu, WENDT Michael
Принадлежит: ABBOTT LABORATORIES

Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member. 19-. (canceled)10. A compound , or a therapeutically acceptable salt thereof , wherein the compound is selected from the group consisting of:N-(4-(4-((4′-chloro(1,1′-biphenyl)-2-yl)methyl)piperazin-1-yl(benzoyl)-4-(((1R)-3-(dimethylamino)-1-((phenylsulfanyl)methyl)propyl)amino)-3-(trifluoromethyl)benzenesulfonamide;N-(4-(4-((4′-chloro(1,1′-biphenyl)-2-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(morpholin-4-yl)-1-((phenylsulfanyl)methyl)propyl)amino)-3-(trifluoromethyl)benzenesulfonamide;N-(4-(4-((4′-chloro(1,1′-biphenyl)-2-yl)methyl)piperazin-1-yl(benzoyl)-4-(((1R)-3-(5,6-dihydro-1(4H)-pyrimidin-1-yl)-1-((phenylsulfanyl)methyl)propyl)amino)-3-(trifluoromethyl)benzenesulfonamide;N-(4-(4-((4′-chloro(1,1′-biphenyl)-2-yl)methyl)piperazin-1-yl(benzoyl)-4-(((1R)-3-(2,4-dimenthyl-4,5-dihydro-1H-imidazol-1-yl)-1-((phenylsulfanyl)methyl)propyl)amino)-3-(trifluoromethyl)benzenesulfonamide;N-(4-(4-((4′-chloro(1,1′-biphenyl)-2-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-methyl-4,5-dihydro-1H-imidazol-1-yl)-1-((phenylsulfanyl)methyl)propyl)amino)-3-(trifluoromethyl)benzenesulfonamide;N-(4-(4-((4′-chloro(1,1′-biphenyl)-2-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(4,4-dimethyl-4,5-dihydro-1H-imidazol-1-yl)-1-((phenylsulfanyl)methyl)propyl)amino)-3-(trifluoromethyl)benzenesulfonamide;N-(4-(4-((2-(4-chlorophenyl)-1-cyclohexen-1-yl)methyl)piperazin-1-yl(benzoyl)-4-(((1R)-3-(dimethylamino)-1-((phenylsulfanyl)methyl)propyl)oxy)-3-(trifluoromethyl)benzenesulfonamide;N-(4-(4-((2-(4-chlorophenyl)cyclohept-1-en-1-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(dimethylamino)-1-((phenylsulfanyl)methyl)propyl)amino)-3-(trifluoromethyl)benzenesulfonamide;4-(((1R)-3-(bis(2-methoxyethyl)amino)-1 ...

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Номер записи: 32
01-08-2013 дата публикации

Alkaloid aminoester derivatives and medicinal composition thereof

Номер: US20130196978A1
Автор: Antonio Caligiuri, Gabriele Amari, Mauro Riccaboni
Принадлежит: Chiesi Farmaceutici SpA

Alkaloid aminoester compounds which act as muscarinic receptor antagonists are useful for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases.

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Номер записи: 33
15-08-2013 дата публикации

Neo-tryptophan

Номер: US20130210740A1
Автор: Abdul Fauq, Bernadette Marie Cusack, Beth Marie Tyler, Daniel J. McCormick, Elliott Richelson, Mona Boules, Yuan-Ping Pang
Принадлежит: Mayo Foundation for Medical Education and Research

Methods of inducing antinociception in a human are described. The method includes the step of administering an effective dose of a polypeptide comprising L-neo-tryptophan to the human extracranially. The polypeptide containing L-neo-tryptophan could be, but is not limited to, NT64L, NT65L, NT66L, NT67L, NT69L, NT69L′, NT71, NT72, NT73, NT74, NT75, NT76, or NT77.

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Номер записи: 34
29-08-2013 дата публикации

Methods for Treating Cognitive/Attention Deficit Disorders Using Tetrahydroindolone Analogues and Derivatives

Номер: US20130225648A1
Автор: Fick David B., Glasky Alvin J., Helton David R.
Принадлежит: SPECTRUM PHARMACEUTICALS, INC.

Methods for treating cognitive/attention deficit disorders in general using tetrahydroindolone derivatives and analogues, particularly tetrahydroindolone derivatives or analogues in which the tetrahydroindolone derivative or analogue is covalently linked to another moiety to form a bifunctional conjugate are disclosed. More specifically, methods and compositions for treating attention deficit disorder and attention deficit hyperactivity disorders in adults and children as well as mild cognitive impairment and dementia are provided. The compounds used to treat and/or palliate cognitive/attention deficit disorders in general include a tetrahydroindolone derivative or analogue comprises a 9-atom bicyclic moiety, moiety A, linked through a linker L to a moiety B, where B is a carboxylic acid, a carboxylic acid ester, or a moiety of the structure N(Y)-D, where Ycan be one of a variety of substituents, including hydrogen or alkyl, and D is a moiety that enhances the pharmacological effects, promotes absorption or blood-brain barrier penetration of the derivative or analogue. The moiety A has a six-membered ring fused to a five-membered ring. The moiety A can have one, two, or three nitrogen atoms in the five membered ring. The moiety A can be a tetrahydroindolone moiety. The moiety B can be one of a variety of moieties, including moieties having nootropic activity or other biological or physiological activity. 2. The compound of claim 1 , wherein L has the structure —(CH)— wherein n is an integer from 1 to 6.3. The compound of claim 2 , wherein n is 2.4. The compound of claim 1 , wherein the moiety B is N(Y)-D.5. The compound of claim 4 , wherein Yis hydrogen.6. The compound of claim 4 , wherein Yis lower alkyl.7. The compound of claim 6 , wherein Yis methyl.11. The compound of claim 10 , wherein L has the structure —(CH)— wherein n is an integer from 1 to 6.12. The compound of claim 11 , wherein n is 2.13. The compound of claim 10 , wherein the moiety B is N(Y)-D.14. The ...

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Номер записи: 35
29-08-2013 дата публикации

Fluoroalkylation Methods And Reagents

Номер: US20130225815A1
Автор: Hiroyuki Morimoto, John F. Hartwig, Patrick Fier
Принадлежит: University of Illinois

A method of forming a fluorinated molecular entity includes reacting in a reaction mixture an aromatic halide, copper, a fluoroalkyl group, and a ligand. The aromatic halide includes an aromatic group and a halogen substituent bonded to the aromatic group. The ligand includes at least one group-V donor selected from phosphorus and an amine. The overall molar ratio of copper to aromatic halide in the reaction mixture is from 0.2 to 3. The method further includes forming a fluoroalkylarene including the aromatic group and the fluoroalkyl group bonded to the aromatic group. A composition, which may be used in the method, consists essentially of copper, the fluoroalkyl group, and the ligand, where the molar ratio of copper to the fluoroalkyl group is approximately 1.

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Номер записи: 36
05-09-2013 дата публикации

ESTROGEN RECEPTOR MODULATORS AND USES THEREOF

Номер: US20130231333A1
Автор: Bonnefous Celine, Douglas Karensa L., Govek Steven P., Herbert Mark R., Julien Jackaline D., Kahraman Mehmet, LAI Andiliy G., Nagasawa Johnny Y., Smith Nicholas D.
Принадлежит: ARAGON PHARMACEUTICALS, INC.

Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors. 2. The compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , or N-oxide thereof claim 1 , wherein:ring A is 5- or 6-membered monocyclic heteroaryl or 8-, 9- or 10-membered bicyclic heterocycle;ring B is phenyl, naphthyl, 5- or 6-membered monocyclic heteroaryl or 8-, 9- or 10-membered bicyclic heterocycle;ring C is phenyl, or 5- or 6-membered monocyclic heteroaryl;{'sup': 3', '8', '8′', '9', '9', '10', '10', '10', '9', '10', '10', '9', '9, 'sub': 2', '2', '2', '2', '2', '2', '1', '4', '2', '4', '2', '4', '1', '4', '1', '4', '1', '4', '1', '4, 'each Ris independently selected from H, halogen, —NRR, —CN, —OH, —OR, —SR, —S(═O)R, —S(═O)R, —NHS(═O)R, —S(═O)N(R), —C(═O)R, —OC(═O)R, —COR, —C(═O)N(R), C-Calkyl, C-Calkenyl, C-Calkynyl, C-Cfluoroalkyl, C-Cheteroalkyl, C-Cfluoroalkoxy, and C-Calkoxy;'}{'sup': 4', '8', '8′', '9', '9', '10', '10', '10', '9', '10', '10', '9', '10', '9', '9', '9', '9', '9', '10', '9', '10, 'sub': 2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '1', '6', '2', '6', '2', '6', '1', '6', '1', '6', '1', '6', '1', '6, 'each Ris independently selected from H, halogen, —NO, —NRR, —CN, —OH, —OR, —SR, —S(═O)R, —S(═O)R, —NHS(═O)R, —S(═O)N(R), —C(═O)R, —OC(═O)R, —COR, —OCOR, —C(═O)N(R), —OC(═O)N(R), —NRC(═O)N(R), —NRC(═O)R, —NRC(═O)OR, substituted or unsubstituted C-Calkyl, substituted or unsubstituted C-Calkenyl, substituted or unsubstituted C-Calkynyl, substituted or unsubstituted C-Cfluoroalkyl, substituted or unsubstituted C-Cheteroalkyl, substituted or unsubstituted C-Cfluoroalkoxy, substituted or unsubstituted C-Calkoxy, substituted or unsubstituted phenyl and ...

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Номер записи: 37
19-09-2013 дата публикации

ACRYLOMIDO DERIVATIVES USEFUL AS INHIBITORS OF THE MITOCHONDRIAL PERMEABILITY TRANSITION

Номер: US20130245019A1
Автор: Ballarini Marco, CAPPA Anna, CARENZI Giacomo, Fancelli Daniele, Minucci Saverio, PAIN Gilles, PLYTE Simon, Varasi Mario, VILLA Manuela
Принадлежит: CONGENIA SRL

Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R′, R″, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them. 110-. (canceled)12. The method according to claim 11 , for the prevention and/or treatment of a diseases resulting from ischemia/reperfusion damage or oxidative damage claim 11 , age-related diseases claim 11 , degenerative and neurodegenerative diseases.13. The method according to claim 12 , for the prevention and/or treatment of acute myocardial infarction claim 12 , heart failure claim 12 , organ ischemia claim 12 , ischemic and traumatic brain damage claim 12 , Duchenne muscular dystrophy claim 12 , Uilrich congenital muscular dystrophy claim 12 , Bentham myopathy claim 12 , amyotrophic lateral sclerosis claim 12 , Huntington's disease claim 12 , Alzheimer's disease claim 12 , Parkinson's disease claim 12 , diabetes type I and type II claim 12 , diabetic complications claim 12 , hyperglycemic tissue damage claim 12 , hypoglycemic tissue damage claim 12 , cholestasis claim 12 , or alcohol-induced damage.1415-. (canceled) The present invention relates to acrylamido derivatives and to their use as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising ...

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Номер записи: 38
03-10-2013 дата публикации

Compounds and methods for kinase modulation, and indications therefor

Номер: US20130261117A1
Автор: Chao Zhang, Gideon Bollag, Jianming Tsai, Jiazhong Zhang, Klaus-Peter Hirth, Prabha N. Ibrahim, Wayne Spevak
Принадлежит: Plexxikon Inc

Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.

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Номер записи: 39
17-10-2013 дата публикации

4-(Hetero)Aryl-Ethynyl-Octahydro-Indole-1-Esters

Номер: US20130274294A1
Автор: Carcache David, KOLLER Manuel, OFNER Silvio, ORAIN David, Renaud Johanne
Принадлежит:

The invention relates to compound of the formula (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it. 2. A compound of formula I according to claim 1 , wherein Ris Calkyl; or a salt thereof.3. A compound of formula I according to claim 1 , wherein m and n are both 0; and Rand Rare both hydrogen; or a salt thereof.4. A compound of formula I according to claim 1 , wherein X is hydroxy; or a salt thereof.5. A compound of formula I according to claim 1 , wherein A is A2; or a salt thereof.6. A compound of formula I according to claim 1 , wherein A is A5; or a salt thereof.7. A compound of formula I according to claim 1 , wherein Ris Calkyl; m and n are both 0;{'sub': 4', '5', '6', '7, 'Rand Rare both hydrogen; X is hydroxy; A is A2; wherein the bond marked with the asterisk is attached to the ethynyl-moiety; Ris chloro, methyl, fluoromethyl, difluoromethyl or trifluoromethyl; Ris fluoro; and n1 is 0, 1 or 2; or a salt thereof.'}8. A compound of formula I according to claim 1 , wherein said compound is selected from the group consisting of(3aR,4S,7aR)-methyl 4-((3-chlorophenyl)ethynyl)-4-hydroxyoctahydro-1H-indole-1-carboxylate;(3aR,4S,7aR)-methyl 4-hydroxy-4-((5-methylpyridin-3-yl)ethynyl)octahydro-1H-indole-1-carboxylate;(3aR,4S,7aR)-methyl 4-hydroxy-4-((2-methylpyridin-4-yl)ethynyl)octahydro-1H-indole-1-carboxylate;(3aR,4S,7aR)-methyl 4-hydroxy-4-((6-methylpyridin-2-yl)ethynyl)octahydro-1H-indole-1-carboxylate;(3aR,4S,7aR)-methyl 4-((2-chloropyridin-4-yl)ethynyl)-4-hydroxyoctahydro-1H-indole-1-carboxylate;(3aR,4S,7aR)-methyl 4-hydroxy-4-((4-methylpyridin-2-yl)ethynyl)octahydro-1H-indole-1-carboxylate;(3aR,4S,7aR)-methyl 4-hydroxy-4-((2-methylthiazol-4-yl)ethynyl)octahydro-1H-indole-1-carboxylate;(3aR,4S,7aR)-methyl 4-amino-4-(m-tolylethynyl)octahydro-1H-indole-1-carboxylate; and(3aR,4S,7aR)-ethyl 4-amino-4-(m-tolylethynyl)octahydro-1H-indole-1-carboxylate;or ...

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Номер записи: 40
24-10-2013 дата публикации

Indolin-2-one derivatives as protein kinase inhibitors

Номер: US20130281451A1
Автор: Ajit Dhananjay JAGTAP, Grace Shiahuy Chen, Hsiao-Chun Wang, Ji-Wang Chern
Принадлежит: Annji Pharmaceutical Co Ltd

A novel class of indoline-2-one derivatives are disclosed. These compounds are protein kinase inhibitors which are useful for treating hyperproliferative diseases such as cancer.

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Номер записи: 41
24-10-2013 дата публикации

PALLADIUM CATALYST, METHOD FOR ITS PREPARATION AND ITS USE

Номер: US20130281700A1
Автор: DALICZEK Zoltán, FINTA Zoltán, SOÓS Tibor, Timári Géza, Vlád Gábor
Принадлежит:

The invention relates to palladium(0)-tris{tri-[3,5-bis(trifluoromethyl)-phenyl]-phosphine} complex of formula (I), as well as to its preparation and use. 2. The composition of in a solid form.3. The composition of having a melting point of 220° C. as determined by DSC in inert atmosphere.4. The composition of claim 1 , having a decomposition point of 169.5° C. as determined by DSC in air under atmospheric pressure.5. A palladium(0) complex comprising three fluorinated phosphine compounds.6. The palladium(0) complex of exhibiting a stability characterized by no measurable decomposition on the basis of P claim 5 , F claim 5 , C and H NMR spectra following 4 months of storage in air at a temperature of 25° C.7. The palladium(0) complex of exhibiting a stability characterized by no measurable decomposition on the basis of P claim 5 , F claim 5 , C and H NMR spectra following 20 months of storage in air at room temperature.8. The palladium(0) complex of having a melting point in inert atmosphere of 220° C.9. The palladium(0) complex of exhibiting stability at any temperature below its melting point.10. The palladium(0) complex of exhibiting insolubility in water at industrially relevant temperatures and stability when stored in water.11. The palladium(0) complex of comprising a yellow solid.12. The palladium(0) complex of that dissolves at around 90° C. in aqueous alcohols.13. The palladium(0) complex of having catalytic activity in cross coupling reactions at a concentration of from 0.1 to 0.3 mole % of the substrate.14. A method for catalysing a C—C claim 5 , C-heteroatom claim 5 , or hydrogenation reaction comprising carrying out the C—C claim 5 , C-heteroatom or hydrogenation reaction in the presence of the palladium(0) complex of .15. The method of claim 14 , wherein the reaction is a C—C cross-coupling reaction.16. The method of claim 14 , wherein the C—C cross-coupling reaction is selected from the group consisting of: Suzuki coupling claim 14 , Heck coupling and ...

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Номер записи: 42
31-10-2013 дата публикации

Amination of Aryl Alcohol Derivatives

Номер: US20130289270A1
Автор: Garg Neil K., Quasdorf Kyle W., Ramgren Stephen D., Silberstein Amanda L.
Принадлежит: The Regents of the University of California

Embodiments of the invention provide methods and materials for chemical cross-coupling reactions that utilize aryl alcohol derivatives as cross-coupling partners. Embodiments of the invention include methods for the amination of aryl sulfamates and carbamates, which are attractive cross-coupling partners, particularly for use in multistep synthesis. Illustrative embodiments include versatile means to use simple derivatives of phenol as precursors to polysubstituted aryl amines, as exemplified by a concise synthesis of the antibacterial drug linezolid. 1. A method for making a cross-coupled compound comprising: combining together:an aryl alcohol derivative, wherein the aryl alcohol derivative comprises an aryl carbamate compound or an aryl sulfamate compound;an amine; anda transition metal catalyst, wherein the transition metallic catalyst comprises nickel or palladium;wherein the aryl alcohol derivative, the amine and the transition metal catalyst are combined so as to allow a cross-coupling reaction between the amine, the aryl alcohol derivative and the transition metal catalyst that results in the formation of the cross-coupled compound that comprises a C—N bond between a carbon atom present in the aryl alcohol derivative and a nitrogen atom present in the amine, in a yield of at least 25%;so that the cross-coupled compound is made.2. The method of claim 1 , wherein the cross-coupling reaction results in the formation of the cross-coupled compound in a yield of at least 50%.3. The method of claim 1 , wherein the aryl alcohol derivative comprises an aryl sulfamate compound.4. The method of claim 1 , wherein the amine comprises a secondary amine.5. The method of claim 1 , wherein the aryl alcohol derivative comprises a heteroatom.6. The method of claim 1 , wherein the transition metallic catalyst comprises nickel.7. The method of claim 1 , wherein the transition metal catalyst comprises an air stable Ni(II) precatalyst complex prior to its combination with the amine ...

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Номер записи: 43
14-11-2013 дата публикации

4-Tolyl-ethynyl-octahydro-indole-1-ester derivatives

Номер: US20130303538A1
Автор: Dieter Oser, Joachim Nozulak
Принадлежит: Individual

The invention relates to compounds of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to their preparation, to their use as medicament and to medicaments comprising them.

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Номер записи: 44
14-11-2013 дата публикации

Thionating agent

Номер: US20130303767A1
Автор: Birgitta Pettersson, Jan Bergman, Per H Svensson, Vedran Hasimbegovic
Принадлежит: Vironova AB

A process for transforming a group >C═O (I) in a compound into a group >C═S (II) or into a tautomeric form of group (II) in a reaction giving a thionated reaction product, by use of crystalline P 2 S 5 .2 C 5 H 5 N as a thionating agent. A thionating agent which is crystalline P 2 S 5 .2 C 5 H 5 N.

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Номер записи: 45
05-12-2013 дата публикации

Indanyloxyphenylcyclopropanecarboxylic acids

Номер: US20130324514A1
Автор: Dieter Hamprecht, Iain Lingard, Sara Frattini, Stefan Peters
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to compounds of general formula I, wherein the groups R 1 , R 2 , R 3 , m and n are defined as in claim 1 , which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.

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Номер записи: 46
05-12-2013 дата публикации

INSECT ODORANT RECEPTOR ANTAGONISTS

Номер: US20130324522A1
Автор: NAKAGAWA Takao, VOSSHALL Leslie
Принадлежит: THE ROCKEFELLER UNIVERSITY

Insect repellent compositions are disclosed which are antagonists of insect odorant receptors. These compositions are useful as insect repellents and confusants. These insect repellent compositions may be suitable for topical application. Also disclosed are methods for interfering with the ability of an insect to detect odors. This is accomplished by exposing an insect to an olfactory-disrupting concentration of a compound. 2. (canceled)4. A method according to wherein A is chosen from oxazole claim 3 , thiazole claim 3 , isothiazole claim 3 , oxadiazole claim 3 , thiadiazole claim 3 , isoxazole claim 3 , imidazole claim 3 , pyrazole and triazole.5. (canceled)78-. (canceled)10. (canceled)12. (canceled)1415-. (canceled)1820-. (canceled)22. A method according to claim 21 , wherein:{'sub': '2', 'Z is CH;'}Ar is phenyl optionally substituted with halogen;{'sub': '2', 'Q is CHor C═O;'}{'sub': '2', 'Y is CHor C═O;'}{'sup': '1', 'sub': 1', '10, 'Ris (C-C)hydrocarbon; and'}{'sup': '2', 'sub': 1', '10, 'Ris (C-C)hydrocarbon or phenyl optionally substituted with halogen.'}2531-. (canceled)32. A method according to wherein{'sup': '24', 'D is NRor S;'}{'sup': '24', 'sub': '3', 'Ris H or CH;'}{'sup': '21', 'sub': 1', '10, 'Ris H or (C-C)hydrocarbon; and'}{'sup': 12', '13, 'sub': 1', '10, 'Rand Rare each independently selected from H and (C-C)hydrocarbon.'}3438-. (canceled)4042-. (canceled)43. A method according to wherein the substituents are selected from —N[(C-C)hydrocarbon] claim 39 , halogen claim 39 , cyano and methoxy.4446-. (canceled)4851-. (canceled)52. A method for interfering with the ability of an insect to detect odors claim 39 , the method comprising exposing said insect to an olfactory-disrupting concentration of a compound chosen from the compounds shown in the compound tables of the application.53. An insect repellent composition suitable for topical application comprising a topically acceptable carrier and a compound described in ; ora topically acceptable ...

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Номер записи: 47
12-12-2013 дата публикации

MINERALOCORTICOID RECEPTOR ANTAGONISTS

Номер: US20130331419A1
Автор: Beresis Richard, Crespo Alejandro, DeVita Robert J., Lan Ping, LIU Kun, Mal Rudrajit, Ogawa Anthony, Qi Changhe, Shen Dong-Ming, Shen Hong, Shu Min, Sinclair Peter J., Sun Zhongxiang, Tan John Qiang, Vande Bunte Ellen K., Wang Yuguang, Wu Zhicai
Принадлежит:

Disclosed are the compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof, which are useful for treating aldosterone-mediated diseases. The processes for preparing compounds of the Formula (I), the use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and the pharmaceutical compositions which comprise compounds of the formula (I) are disclosed too. 3. The compound of wherein Ris H.8. The compound of which is(R)—N-{1-[(2R)-2-(4-chlorophenyl)-1-hydroxybutan-2-yl]-1H-indol-4-yl}methanesulfonamide;N-(1-(1-(4-chlorophenyl)-1-(2-cyanocyclopropyl)propyl)-1H-indazol-4-yl)methanesulfonamide;N-(1-(1-(4-chlorophenyl)-1-(3-ethyl-1,2,4-oxadiazol-5-yl)propyl)-1H-indol-4-yl)methanesulfonamide;N-(1-(2-(4-chlorophenyl)-1-hydroxybutan-2-yl)-1H-indazol-4-yl)methanesulfonamide;N-(1-(1-(4-chlorophenyl)-1-(1-hydroxycyclopropyl)propyl)-1H-indol-4-yl)methanesulfonamide;N-(1-(3-(4-chlorophenyl)-2-hydroxypentan-3-yl)-6-fluoro-1H-indol-4-yl)methanesulfonamide;N-(1-(2-(4-chlorophenyl)-1-hydroxybutan-2-yl)indolin-4-yl)methanesulfonamide;N-{1-[3-(4-chlorophenyl)-2-hydroxypentan-3-yl]-1H-indazol-4-ylmethanesulfonamide;N-(1-(2-amino-3-(4-chlorophenyl)pentan-3-yl)-1H-indol-4-yl)methanesulfonamide;1-(1-(3-(4-chlorophenyl)-2-hydroxy-2-methylpentan-3-yl)-1H-indazol-4-yl)-3-methyl-sulfonylurea;methyl {4-[(methylsulfonyl)amino]-1H-indol-1-yl}(phenyl)acetate;N-(1-(3-(4-chlorophenyl)-2-hydroxy-2-methylpentan-3-yl)-6-fluoro-1H-indol-4-yl)methane sulfonamide;N-(1-(3-(4-chlorophenyl)-2-hydroxy-2-methylpentan-3-yl)-1H-indol-4-yl)methanesulfonamide;N-(1-(3-(4-chlorophenyl)-2-hydroxy-2-methylpentan-3-yl)-1H-indazol-4-yl)methanesulfonamide;N-(1-(2-hydroxy-2-methyl-3-(4-(trifluoromethyl)phenyl)pentan-3-yl)-1H-indazol-4-yl)methanesulfonamide;N-(1-(2-(4-chlorophenyl)-1-methoxybutan-2-yl)-1H-indol-4-yl)methanesulfonamide;N-(1-(3-(4-chlorophenyl)-2-oxopentan-3-yl)-1H-indazol-4-yl)methanesulfonamide;N-(1-(2-hydroxy-3-(4-( ...

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Номер записи: 48
12-12-2013 дата публикации

ACETYLENE DERIVATIVES HAVING MGLUR 5 ANTAGONISTIC ACTIVITY

Номер: US20130331568A1
Автор: Auberson Yves, Gasparini Fabrizio, Hart Terance W., OFNER Silvio, Zimmermann Kaspar
Принадлежит: NOVARTIS AG

The invention provides compounds of formula I 1. A compound of formula Im is 0 or 1,n is 0 or 1 andA is hydroxyX is hydrogen andY is hydrogen, orA forms a single bond with X or with Y;{'sub': 0', '1-4', '1-4', '1', '1', '1-4', '2', '2', '1-4, 'Ris hydrogen. (C)alkyl, (C)alkoxy, trifluoromethyl, halogen, cyano, nitro, —COORwherein Ris (C)alkyl or —CORwherein Ris hydrogen or (C)alkyl, and'}{'sub': 3', '3', '4', '5', '2', '6', '3', '1-4', '3-7', '4', '5', '1-4', '3', '1-4', '3-7, 'R is —COR, —COOR, —CONRRor —SOR, wherein Ris (C)alkyl, (C)cycloalkyl or optionally substituted phenyl, 2-pyridyl or 2-thienyl, Rand R, independently, are hydrogen or (C)alkyl and Ris (Calkyl, (C)cycloalkyl or optionally substituted phenyl,'}{'sub': '1-4', 'R′ is hydrogen or (C)alkyl and'}{'sub': '1-4', 'R″ is hydrogen or (C)alkyl, or'}{'sub': 2', '2', 'p, 'claim-text': 'wherein p is 0, 1 or 2, in which case one of n and p is different from 0,', 'R′ and R″ together form a group —CH—(CH)—'}whereinwith the proviso that Ris different from hydrogen, trifluoromethyl and methoxy when m is 1, n is 0, A is hydroxy, X and Y are both hydrogen, R is COOEt and R′ and R″ together form a group —(CH)—, The present invention relates to novel acetylene derivatives, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them.More particularly the invention provides a compound of formula IwhereinOn account of the asymmetrical carbon atoms present in the compounds of formula I and their salts, the compounds may exist in optically active form or in form of mixtures of optical isomers, e.g. in form of racemic mixtures. All optical isomers and their mixtures including the racemic mixtures are part of the present invention.In a further aspect, the invention provides a process for the production of the compounds of formula I and their salts, which comprises the step ofThe reaction of process a) can be effected according to conventional methods, e.g. as described in Examples 1 (step ...

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Номер записи: 49
02-01-2014 дата публикации

ANDROGEN RECEPTOR MODULATOR COMPOUNDS AND METHODS

Номер: US20140005186A1
Автор: Chen Jyun-Hung, HIGUCHI Robert I., Kallel E. Adam, Lau Thomas Lot Stevens, Miller Todd A., Pedram Bijan, Ruppar Daniel A., Van Oeveren Cornelis Arjan, Zhi Lin
Принадлежит: Ligand Pharmaceuticals Incorporated

Provided herein are compounds having a structure selected from among Formula (I), Formula (II), Formula (III), Formula (IV), Formula (V) and Formula (VI) that are androgen receptor modulators and/or androgen receptor binding agents. Also disclosed are methods of making and using such compounds, including, but not limited to, using such compounds for treating various conditions. 2. The method of claim 1 , wherein the androgen receptor is in a cell.3. The method of claim 1 , wherein the compound is an androgen receptor agonist.4. The method of claim 1 , wherein the compound is an androgen receptor antagonist.5. The method of claim 1 , wherein the compound is a compound of Formula II claim 1 , or a pharmaceutically acceptable salt claim 1 , ester claim 1 , amide or prodrug thereof.6. The method of claim 1 , wherein the compound is selected from:N,N-bis(2,2,2-trifluoroethyl)-3-methyl-4-nitroaniline;N,N-bis(2,2,2-trifluoroethyl)-4-nitroaniline;4-Bromo-N,N-bis(2,2,2-trifluoroethyl)-3-(trifluoromethyl)aniline;4-(Bis(2,2,2-trifluoroethyl)amino)-2-(trifluoromethyl)benzonitrile;(5R)—N-(4-nitrophenyl)-5-(dimethyl-tort-butylsilyloxymethyl)-2-pyrrolidone;(5R)—N-(4-nitrophenyl)-5-(hydroxymethyl)-2-pyrrolidone;(2R)—N-(4-nitro-3-trifluoromethylphenyl)-2-(dimethyl-tert-butylsilyloxymethyl)pyrrolidine (compound 106);(2R)—N-(4-nitro-3-trifluoromethylphenyl)-2-(hydroxymethyl)pyrrolidine;(2R)—N-(4-nitrophenyl)-2-(hydroxymethyl)pyrrolidine;(2R)—N-(3-Trifluoromethyl-4-nitrophenyl)-2-formylpyrrolidine;(2R)—N-(3-Trifluoromethyl-4-nitrophenyl)-2-(1-(S)-hydroxy-2,2,2-trifluoroethyl)pyrrolidine;(2R)—N-(3-Trifluoromethyl-4-nitrophenyl)-2-(1-(R)-hydroxy-2,2,2-trifluoroethyl)pyrrolidine;(2S)—N-(4-nitrophenyl)-2-(hydroxymethyl)pyrrolidine;(2R)—N-(4-nitrophenyl)-2-(1-(S)-hydroxy-2,2,2-trifluoroethyl)pyrrolidine;(2R)—N-(4-nitrophenyl)-2-(R)-(1-(R)-hydroxy-2,2,2-trifluoroethyl)pyrrolidine;(2S)—N-(4-nitrophenyl)-2-(1-(S)-hydroxy-2,2,2-trifluoroethyl);(2S)—N-(4-nitrophenyl)-2-(1-(R)-hydroxy-2,2,2- ...

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Номер записи: 50
02-01-2014 дата публикации

RING-FUSED COMPOUND

Номер: US20140005221A1
Автор: BABA Motoaki, FUJIOKA Shinichi, ITOH Yoshiki, KONDOH Eri, NAGAI Keita, NAGASAWA Koh, TAKAHASHI Hirobumi, Tanaka Kenichi
Принадлежит: SATO PHARMACEUTICAL CO., LTD.

The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below. 3. The compound according to claim 2 , wherein{'sup': 3', '4', '5, 'W, Wand Ware each independently a nitrogen atom, or a methine group that may have a substituent selected from the group consisting of a halogen atom and a lower alkyl group, or a pharmaceutically acceptable salt or ester of the compound.'}4. The compound according to claim 3 , wherein{'sup': 'X', 'X is a single bond, an oxygen atom, a carbonyl group, a vinylene group or a group represented by the general formula: —N(R)—, or a pharmaceutically acceptable salt or ester of the compound.'}5. The compound according to claim 4 , wherein{'sup': 1', '1', '1, 'Ris a group represented by a general formula -Q-A, or a pharmaceutically acceptable salt or ester of the compound.'}6. The compound according to claim 5 , wherein{'sup': '1', 'Qis a single bond or a lower alkylene group that may be substituted with a lower alkyl group, or a pharmaceutically acceptable salt or ester of the compound.'}7. The compound according to claim 6 , wherein{'sup': Yi', 'Yi′', 'Y1', 'Y1′', 'Y1', 'Y1′', 'Y1', 'Y1′', 'Y2', 'Y2′', 'Y1', 'Y1′', 'Y2', 'Y2′', 'Y3', 'Y3′', 'Y1', 'Y1′', 'Y2', 'Y2′', 'Y3', 'Y3′', 'Y4', 'Y4′', 'Y1', 'Y1′', 'Y2', 'Y2′', 'Y3', 'Y3′', 'Y4', 'Y4′', 'Y5', 'Y5′', 'Y1', 'Y′', 'Y2', 'Y2′', 'Y3', 'Y3′', 'Y4', 'Y4′', 'Y5', 'Y5′', 'Y6', 'Y6′', 'Y1', 'Y1′', 'Y2', 'Y2′', 'Y3', 'Y3′', 'Y4', 'Y4′', 'Y5', 'Y5′', 'Y6', 'Y6′, 'sub': n', 'n, 'Y is a single bond or (CRR)(herein n is any integer of 1 to 6, i is any integer of 1 to n, and (CRR)represents (CRR) when n=1; represents (CRR)—(CRR) when n=2; represents (CRR)—(CRR)—(CRR) when n=3; represents (CRR)—(CRR)—(CRR)—(CRR) when n=4; represents (CRR)—(CRR)—(CRR)—(CRR)—(CRR) when n=5; and ...

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Номер записи: 51
09-01-2014 дата публикации

New palladium catalyst, method for its preparation and its use

Номер: US20140012004A1
Автор: Gábor Vlád, Géza Timári, Tibor SOÓS, Zoltán DALICZEK, Zoltán Finta
Принадлежит: H4SEP KFT

The invention relates to palladium(0) tris{tri-[3,5-bis(trifluoromethyl)-phenyl]-phosphine} complex of formula (I), as well as to its preparation and use. This compound is outstandingly stable, and can be used as catalyst with excellent results.

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Номер записи: 52
09-01-2014 дата публикации

Process for preparing chiral amino acids

Номер: US20140012005A1
Автор: Benoit Folleas, Jean-Louis Brayer, Nicolas Lefevre, Sylvain Darses
Принадлежит: Diverchim SA

The present invention relates to a process for preparing chiral amino acids with excellent enantiomeric excesses.

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Номер записи: 53
16-01-2014 дата публикации

INDOLE DERIVATIVE, AND PHARMACOLOGICALLY ACCEPTABLE SALT THEREOF

Номер: US20140018335A1
Автор: Kawamura Naohiro, Kohno Yasushi, Kondo Atsushi, Kondo Tatsuhiro, SETO Shigeki, Tatani Kazuya
Принадлежит: KISSEI PHARMACEUTICAL CO., LTD.

The present invention provides a compound represented by the general formula (I) of the present invention, which has EPreceptor antagonism: 4. The compound as claimed in or a pharmaceutically acceptable salt thereof claim 3 , wherein Ris a group selected from the group consisting of the following o) claim 3 , r1) claim 3 , s1) claim 3 , and t1):{'sub': '3-6', 'o) a branched Calkyl group,'}{'sub': 1-6', '1-6', '1-6, 'r1) a phenyl group, in which the ring is unsubstituted or substituted with one group selected from the group consisting of the following: a halogen atom, a Calkyl group, a halo-Calkyl group, and a Calkoxy group,'}{'sub': 1-6', '1-6', '1-6, 's1) a 6-membered aromatic heterocyclic group, in which the ring is unsubstituted or substituted with one group selected from the group consisting of the following: a halogen atom, a Calkyl group, a halo-Calkyl group, and a Calkoxy group, and'}{'sub': 1-6', '1-6', '1-6, 't1) a 5-membered aromatic heterocyclic group, in which the ring is unsubstituted or substituted with one group selected from the group consisting of the following: a halogen atom, a Calkyl group, a halo-Calkyl group, and a Calkoxy group.'}5. The compound as claimed in or a pharmaceutically acceptable salt thereof claim 4 , wherein Rrepresents a halogen atom claim 4 , a Calkyl group claim 4 , a Calkoxy group claim 4 , or a Ccycloalkyl group.6. The compound as claimed in or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris a group selected from the group consisting of the following i) and m):{'sub': '2-', 'sup': '6', 'i) —C(═O)—NH—SOR; and'}m) an acidic 5-membered hetero ring group.7. The compound as claimed in or a pharmaceutically acceptable salt thereof claim 6 , wherein Ris —C(═O)—NH—SOR.8. The compound as claimed in claim 1 , which is the compound selected from the following group claim 1 , or a pharmaceutically acceptable salt thereof:N-(methanesulfonyl)-6-(5-methoxy-2-phenylindol-1-ylmethyl)pyridine-2-carboxamide,6-[6-fluoro-5- ...

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Номер записи: 54
16-01-2014 дата публикации

Lisofylline analogs and methods for use

Номер: US20140018355A1
Автор: Jerry L. Nadler, Peng Cui, Timothy L. MacDonald
Принадлежит: UNIVERSITY OF VIRGINIA PATENT FOUNDATION

The present invention provides analogs of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF.

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Номер записи: 55
23-01-2014 дата публикации

Indole compounds as an inhibitor of cellular necrosis

Номер: US20140024618A1
Автор: Dong Ook Seo, Eok Park, Heui Sul Park, Hyo Shin Kwak, Hyoung Jin Kim, Seung Hyun Yoon, Seung Yup Paek, Soon Ha Kim, Sun Young Koo, Sung Bae Lee
Принадлежит: LG Life Sciences Ltd

The present invention relates to new indole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole compounds as an active ingredient.

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Номер записи: 56
23-01-2014 дата публикации

Small molecule inhibitors of necroptosis

Номер: US20140024657A1
Автор: Emily S. Hsu, Junying Yuan
Принадлежит: Harvard College

The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-α) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-α induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.

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Номер записи: 57
23-01-2014 дата публикации

CHEMICAL COMPOUNDS

Номер: US20140024694A1
Автор: CADILLA Rodolfo, TURNBULL Philip Stewart
Принадлежит: GlaxoSmithKline Intellectual Property (No.2) Limit ed

This invention relates to non-steroidal compounds that are modulators of androgen receptor, and also to the methods for the making and use of such compounds. 2. A pharmaceutical composition comprising a compound according to and one or more pharmaceutically acceptable excipients.3. A method of treating muscle wasting associated with chronic obstructive pulmonary disease (COPD) claim 1 , wherein said method comprises administering a compound according to to a human subject in need thereof.4. A method of treating muscle wasting associated with chronic kidney disease (CKD) claim 1 , wherein said method comprises administering a compound according to to a human subject in need thereof.5. A method of treating muscle wasting associated with chronic heart failure (CHF) claim 1 , wherein said method comprises administering a compound according to to a human subject in need thereof.6. A method of treating urinary incontinence claim 1 , wherein said method comprises administering a compound according to to a human subject in need thereof.7. A method of accelerating hip fracture repair and healing claim 1 , wherein said method comprises administering a compound according to to a human subject in need thereof.8. The method according to claim 3 , wherein 0.1-50 mgs of compound 1 is administered.9. The method according to claim 4 , wherein 0.1-50 mgs of compound 1 is administered.10. The method according to claim 5 , wherein 0.1-50 mgs of compound 1 is administered.11. The method according to claim 6 , wherein 0.1-50 mgs of compound 1 is administered.12. The method according to claim 7 , wherein 0.1-50 mgs of compound 1 is administered. This invention relates to non-steroidal compounds that are modulators of the androgen receptor and methods for their use in treatment.Steroidal nuclear receptor (NR) ligands are known to play important roles in the health of both men and women. Testosterone (T) and dihydrotestosterone (DHT) are endogenous steroidal ligands for the androgen ...

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Номер записи: 58
06-02-2014 дата публикации

ANTI-PARASITIC METHODS AND COMPOSITIONS UTILIZING DIINDOLYLMETHANE-RELATED INDOLES

Номер: US20140037577A1
Автор: Zeligs Michael A.
Принадлежит:

The present invention includes methods and compositions for the treatment and prevention of protozoal parasitic infections utilizing Diindolylmethane-related indoles. Additive and synergistic interaction of Diindolylmethane-related indoles with other known anti-parasitic and pro-apoptotic agents is believed to permit more effective therapy and prevention of protozoal parasitic infections. The methods and compositions described provide new treatment of protozoal parasitic diseases of mammals and birds including malaria, leishmaniasis, trypanosomiasis, trichomoniasis, neosporosis and coccidiosis. 1. A method of treating or reducing the risk of a protozoal disease comprising administering to a subject in need thereof a therapeutically effective amount of one or more DIM-related indoles and one or more anti-protozoal agents.2. The method of claim 1 , wherein said protozoal disease is leishmaniasis or trypanosomiasis.3. The method of claim 1 , wherein said protozoal disease is malaria claim 1 , toxoplasmosis claim 1 , cryptosporidiosis or bebesiosis.4Microsporidia, Trichomonas, Cyclospora, IsosporaBlastocystis.. The method of claim 1 , wherein said protozoal disease results from an infection from or5Neospora.. The method of claim 1 , wherein said protozoal disease results from an infection from6. The method of claim 1 , or claim 1 , wherein said subject is a human.7. The method of claim 6 , wherein said human is immunocompromised.8. The method of claim 3 , wherein said subject is a lamb claim 3 , calf claim 3 , pig claim 3 , rabbit or chicken.9. The method of claim 5 , wherein said subject is a non-human mammal selected from the group consisting of a dog claim 5 , cow claim 5 , sheep claim 5 , goat and horse.11. The method of claim 1 , wherein the one or more DIM-related indoles are selected from the group consisting of diindolylmethane claim 1 , hydroxylated DIMs claim 1 , methoxylated DIMs claim 1 , 2-(Indol-3-ylmethyl)-3 claim 1 ,3′-diindolylmethane (LTR) claim 1 , ...

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Номер записи: 59
20-02-2014 дата публикации

Substituted indole compounds having nos inhibitory activity

Номер: US20140051687A1
Автор: Jailall Ramnauth, Joanne Patman, Paul Renton, Shawn Maddaford, Subhash C. Annedi, Suman Rakhit
Принадлежит: Neuraxon Inc

The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.

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Номер записи: 60
20-02-2014 дата публикации

Modulators of atp-binding cassette transporters

Номер: US20140051724A1
Автор: Anna Hazlewood, Ashvani Singh, Fredrick Van Goor, Jason Mccartney, Jinglan Zhou, Peter Grootenhuis, Sara Hadida-Ruah
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

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Номер записи: 61
27-02-2014 дата публикации

SYSTEM FOR FLUORINATING ORGANIC COMPOUNDS

Номер: US20140058106A1
Автор: Furuya Takeru, Kaiser Hanns M., Ritter Tobias
Принадлежит:

Described herein are fluorinated organic compounds and methods of making fluorinated organic compounds, for example, using palladium complexes. Also described herein are compositions and kits containing compounds and palladium complexes described herein. 2. The palladium complex of claim 1 , wherein the palladium complex further comprises a negatively charged counterion X claim 1 , wherein X is selected from BF claim 1 , BPh claim 1 , PF claim 1 , [BArF] claim 1 , B(CF) claim 1 , SbF claim 1 , and CFSO.3. The palladium complex of claim 1 , wherein Z is —N(R)—.4. The palladium complex of claim 3 , wherein Ris —S(O)R.5. The palladium complex of claim 4 , wherein Ris optionally substituted aryl.7. The palladium complex of claim 1 , wherein Ris pyridyl.8. The palladium complex of claim 1 , wherein Ris halogen claim 1 , an optionally substituted heteroaryl claim 1 , or —OR.9. The palladium complex of claim 8 , wherein Ris —Cl or pyridyl.10. The palladium complex of claim 1 , wherein Ris —C(═O)Ror —S(O)R.11. The palladium complex of claim 10 , wherein Ris an optionally substituted aliphatic.12. The palladium complex of claim 11 , wherein Ris —C(═O)CHor —S(O)CF.15. The method of claim 14 , wherein the organic compound comprises an aryl group.16. The method of claim 14 , wherein the organic compound comprises a boron substituent.18. The method of claim 14 , wherein the fluorinating agent provides a source of F.20. The palladium complex of claim 19 , wherein Ris pyridyl.21. The palladium complex of claim 19 , wherein Ris halogen claim 19 , an optionally substituted heteroaryl claim 19 , or —OR.22. The palladium complex of claim 21 , wherein Ris —Cl or pyridyl.23. The palladium complex of claim 21 , wherein Ris —C(═O)Ror —S(O)R.24. The palladium complex of claim 23 , wherein Ris an optionally substituted aliphatic.25. The palladium complex of claim 24 , wherein Ris —C(═O)CHor —S(O)CF. The present application is a Continuation of U.S. application Ser. No. 12/865,703, which is ...

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Номер записи: 62
06-03-2014 дата публикации

S1P Receptors Modulators and Their Use Thereof

Номер: US20140066427A1
Автор: Damian W. Grobelny, Gurmit S. Gill
Принадлежит: Akaal Pharma Pty Ltd

The invention relates to novel compounds that have SIP receptor modulating activity. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with inappropriate SIP receptor modulating activity or expression, for example, autoimmune response. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate SIP receptor modulating activity or expression such as autoimmune response.

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Номер записи: 63
20-03-2014 дата публикации

Histone Deacetylase Inhibitors for Enhancing Activity of Antifungal Agents

Номер: US20140081017A1
Автор: Raeppel Franck, Raeppel Stéphane, Vaisburg Arkadii
Принадлежит: METHYLGENE INC.

The present invention relates to compositions and methods to selectively treat fungal infection. More particularly, the invention relates to compounds, compositions thereof, and methods for selectively enhancing fungal sensitivity to antifungal compounds. The compositions of the invention are comprised of a combination of a histone deacetylase inhibitor, or an N-oxide, hydrate, solvate, pharmaceutically acceptable salt, agricultural formulation, prodrug or complex thereof, and an antifungal agent, the histone deacetylase inhibitor being a compound of Formula (I): 119.-. (canceled)21. The inhibitor of claim 20 , where B is phenyl.24. The inhibitor of claim 20 , where the butyl group is substituted at one or more positions with one or two methyl claim 20 , ethyl claim 20 , fluoro claim 20 , chloro claim 20 , bromo claim 20 , or hydroxyl groups claim 20 , or one oxo claim 20 , amino claim 20 , or oxime group.25. The inhibitor of claim 24 , where the butyl group is substituted at one position with one methyl claim 24 , ethyl claim 24 , fluoro claim 24 , chloro claim 24 , bromo claim 24 , oxo claim 24 , amino claim 24 , oxime or hydroxyl group.26. The inhibitor of claim 24 , where the butyl group is substituted at the same position with two methyl claim 24 , ethyl claim 24 , fluoro claim 24 , chloro claim 24 , bromo or hydroxyl groups.27. The inhibitor of claim 20 , where the butyl group is unsubstituted.28. The inhibitor of claim 20 , where Rand Rare independently hydrogen or methyl.29. (canceled)30. (canceled)32. (canceled)34. A histone deacetylase inhibitor selected from the group consisting of:N-hydroxy-2-(2-(4-phenylbutyl)thiazol-4-yl)acetamide,N-hydroxy-2-(2-(4-phenylbutyl)thiazol-5-yl)acetamide,2-(4-(4-(2,4-difluorophenyl)butyl)phenyl)-N-hydroxyacetamide,N-hydroxy-2-(4-(4-p-tolylbutyl)phenyl)acetamide,2-(4-(4-(biphenyl-4-yl)butyl)phenyl)-N-hydroxyacetamide,N-hydroxy-2-(4-(4-(1-methyl-1H-indol-5-yl)butyl)phenyl)acetamide,2,2′-(4,4′-(butane-1,4-diyl)bis(4,1- ...

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Номер записи: 64
20-03-2014 дата публикации

METHODS OF PRODUCING MOLINDONE AND ITS SALTS

Номер: US20140081020A1
Автор: Figini Attilia, Fumagalli Tiziano, Hanbauer Martin, Hildebrand Peter, Liang Likan, Nazir Zarghun
Принадлежит:

The present invention is directed towards novel methods of synthesis of molindone, synthesis of the intermediates of molindone, and high-purity compositions of molindone. In particular, the invention relates to the methods of synthesis of molindone through the Mannich reaction. 1. A process for preparing a compound SUMO-3 comprising a step of reacting SUMO-2 with bismorpholinomethane.2. The process of further comprising at least one of the following steps:(a) removal of methylene SUMO-2 by filtration under acidic conditions;(b) adsorbing oligomeric compounds on charcoal;(c) filtering and crystallizing SUMO-3 free base from a solvent.3. The process of further comprising a step of formation and crystallization of a salt of SUMO-3.4. The process of wherein said salt is selected from the group consisting of molindone hydrochloride claim 3 , molindone sulfate claim 3 , molindone phosphate claim 3 , molindone monohydrogenphosphate claim 3 , molindone dihydrogenphosphate claim 3 , molindone bromide claim 3 , molindone iodide claim 3 , molindone acetate claim 3 , molindone propionate claim 3 , molindone decanoate claim 3 , molindone caprylate claim 3 , molindone formate claim 3 , molindone oxalate claim 3 , molindone malonate claim 3 , molindone succinate claim 3 , molindone fumarate claim 3 , molindone maleate claim 3 , molindone citrate claim 3 , molindone lactate claim 3 , molindone tartrate claim 3 , molindone methanesulfonate claim 3 , and molindone mandelate.5. The process of wherein the compound SUMO-2 is prepared by reacting SUMO-1 with 1 claim 1 ,3-cyclohexanedione.6. The process of wherein the compound SUMO-2 is prepared by reacting SUMO-1 with 1 claim 5 ,3-cyclohexanedione in the presence of a hydrogenation catalyst.7. The process of wherein the compound SUMO-2 is prepared by reacting SUMO-1 with 1 claim 5 ,3-cyclohexanedione in the presence of Zn in acetic acid.8. The process of wherein said catalyst comprises Pd/C.9. The process of wherein said catalyst ...

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Номер записи: 65
07-01-2016 дата публикации

Processes for recovering valuable components from a catalytic fast pyrolysis process

Номер: US20160002162A1
Автор: Charles M. Sorensen, Jr., Jeffrey P. WHITING, Marc E. SCHNEIDKRAUT, Michael TANZIO
Принадлежит: Anellotech Inc

Methods of separating products from the catalytic fast pyrolysis of biomass are described. In a preferred method, a portion of the products from a pyrolysis reactor are recovered and separated using a quench system and solvent contacting system that employs materials produced in the pyrolysis process.

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Номер записи: 66
07-01-2016 дата публикации

NOVEL COMPOUNDS AND COMPOSITIONS FOR INHIBITION OF FASN

Номер: US20160002188A1
Автор: Bair Kenneth W., JR. David R., Lancia, LI Hongbin, Loch James
Принадлежит:

The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below: 6. The compound of claim 2 , wherein A and B are 0.10. The compound of claim 2 , wherein Aris a substituted or unsubstituted 5-6 membered monocyclic aryl or heteroaryl.11. The compound of claim 10 , wherein Aris a substituted or unsubstituted 5 membered monocyclic aryl or heteroaryl and said heteroaryl has 1 or 2 heteroatoms which are independently S or N.13. The compound of claim 10 , wherein Aris a substituted or unsubstituted 6 membered monocyclic aryl or heteroaryl and said heteroaryl has 1 or 2 heteroatoms which are N.18. The compound of claim 2 , wherein Aris a substituted or unsubstituted 9 membered 6 claim 2 ,5-bicyclic heteroaryl and said heteroaryl has 1 claim 2 , 2 claim 2 , or 3 heteroatoms which are independently O claim 2 , S or N.20. The compound of claim 2 , wherein Ris a substituted or unsubstituted monocyclic or bicyclic 5-10 membered aryl or heteroaryl.21. The compound of claim 20 , wherein Ris a substituted or unsubstituted monocylic 6 membered aryl.23. The compound of claim 20 , wherein Ris a substituted or unsubstituted bicyclic 8-10 membered aryl or 8-10 membered heteroaryl.24. The compound of claim 23 , wherein Ris a substituted or unsubstituted 8 membered 5 claim 23 ,5 bicyclic heteroaryl and said heteroaryl has 1 claim 23 , 2 claim 23 , 3 claim 23 , or 4 heteroatoms and said heteroatoms are independently O claim 23 , S claim 23 , or N.26. The compound of claim 20 , wherein Ris a substituted or unsubstituted 9 membered 6 claim 20 ,5 bicyclic heteroaryl and said heteroaryl has 1 claim 20 , 2 claim 20 , 3 claim 20 , or 4 heteroatoms and said heteroatoms are independently O claim 20 , S claim 20 , or N.28. The compound of claim 20 , wherein Ris a substituted or unsubstituted 10 membered 6 claim 20 ,6 bicyclic aryl or heteroaryl and said heteroaryl has 1 claim ...

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Номер записи: 67
07-01-2016 дата публикации

NOVEL INDOLE DERIVATIVES USEFUL AS ANTI-DIABETIC AGENTS

Номер: US20160002224A1
Автор: Acton, Anand Rajan, Arasappan Ashok, Dang Qun, III John J., Pu Zhifa, Sebhat Iyassu, Suzuki Takao
Принадлежит:

Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension. 3. The compound according to claim 1 , wherein{'sup': '3', 'T is selected from —CR— and N;'}{'sup': '1', 'U is —CR—;'}{'sup': '2', 'V is —CR—; and'}{'sup': '4', 'W is selected from —CR— and N,'}{'sup': 1', '2, 'sub': 3', '1-6', '2-6', '2-6', '3', '1-6', '2-6', '2-6, 'provided that one of T and W is N, and further provided that if W is N, then Ris selected from hydrogen, halogen, —CN, —CF, —Calkyl, —Calkenyl and —Calkynyl, and if T is N then Ris selected from hydrogen, halogen, —CN, —CF, —Calkyl, —Calkenyl and —Calkynyl;'}or a pharmaceutically acceptable salt thereof.4. The compound according to claim 1 , wherein T is —CR— or N; U is —CR—; V is —CR—; and W is —CR—; or a pharmaceutically acceptable salt thereof.5. The compound according to claim 1 , wherein X is absent or selected from:{'sub': '2', '(1) —CH—,'}(2) —S—,(3) —S(O)—,{'sub': '2', '(4) —S(O)—,'}(5) —O—,{'sub': '2', '(6) —O—CH—,'}{'sub': '2', '(7) —CH—O—,'}{'sub': '2', '(8) —CH—S—,'}(9) —NH—,(10) —C(O)—, and(11) —C(O)NH—,{'sub': 2', '2', '1-6', '2', '2', '1-6', '1-6', '1-6', '2', '2', '1-6', '1-6, 'wherein each CHis unsubstituted or substituted with 1 or 2 substituents selected from: hydroxy, halogen, NH, Calkyl, COH, COCalkyl, and COCalkyl, and wherein each NH is unsubstituted or substituted with 1 substituent selected from: Calkyl, COH, COCalkyl, and COCalkyl;'}or a pharmaceutically acceptable salt thereof.6. The compound according to claim 4 , wherein X is —CH—; or a pharmaceutically acceptable salt thereof.8. The compound according to claim 6 , wherein Y is selected from:{'sub': '1-6', '(1) Calkyl,'}{'sub': '3-10', '(2) Ccycloalkyl, ...

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Номер записи: 68
07-01-2016 дата публикации

SYNTHESIS AND USE OF FLUORINATED COMPOUNDS

Номер: US20160002270A1
Автор: ARGINTARU Oana, MOLANDER Gary Alan
Принадлежит:

The invention is directed to the preparation of fluorinated compounds and their use in organic synthesis. In particular, the invention is directed to methods of reacting compounds of structure with R—CH═Nor (CF)C═Nto form a perfluoroalkylate or -arylated compounds, and products derived from these reactions, where X, Y, and Rare described herein. 3. A method of generating a compound having an aryl- or heteroaryl-α-trifluoromethyl group comprising reacting an aryl-B(OH)or heteroaryl-B(OH)with CF—CH═Nunder conditions sufficient to form a trifluoromethyl-containing compound.4. The method of claim 3 , further comprising reacting the compound having an aryl- or heteroaryl-α-trifluoromethyl group with KHF claim 3 , pinacol claim 3 , an oxidizing reagent claim 3 , or a protodeboronating agent.5. The method of claim 1 , wherein the CF—CH═Nis generated in situ.6. The method of wherein the:(a) compound of Formula (II) or Formula (III); and{'sub': 3', '2, '(b) CF—CH═N'}{'sub': 3', '2, 'are reacted with a molar ratio of boron to CF—CH═Nin a range of from about 1:1 to about 1:10.'}7. The method of claim 1 , wherein the:(a) compound of Formula (II) or Formula (III); and{'sub': 3', '2, '(b) CF—CH═N'}{'sub': 3', '2, 'are reacted with a molar ratio of boron to CFCH═Nin a range of from about 1:10 to about 1:200.'}8. The method of claim 1 , wherein n is 1 to 5.9. The method of claim 1 , wherein n is 6 to 10.10. The method of claim 1 , wherein n is 11 to 50.11. The method of claim 1 , wherein n is 1 or 2.12. The method of claim 1 , wherein n is 1.13. The method of claim 1 , wherein X is optionally substituted aryl.14. The method of claim 3 , wherein the aryl is optionally substituted phenyl claim 3 , naphthyl claim 3 , or fluorenyl.15. The method of claim 13 , wherein the aryl is substituted with 1 claim 13 , 2 claim 13 , or 3 substitutents independently selected from the group consisting of Calkyl; Calkenyl; Calkynyl claim 13 , —OCalkyl; —OCalkenyl; —C(O)Calkyl; —C(O)-aryl; —C(O)- ...

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Номер записи: 69
04-01-2018 дата публикации

BIS(SULFONAMIDE) DERIVATIVES AND THEIR USE AS MPGES INHIBITORS

Номер: US20180002278A1
Автор: BYLUND Johan, EK Maria, HALLBERG Jesper, HETTMAN Andreas, HÖGDIN Katharina, KERS Annika, NORD Johan, ÖHBERG Liselott, Soderman Peter, SVENSSON Mats A.
Принадлежит:

The present invention relates to bis(sulfonamide) compounds and pharmaceutically acceptable salts thereof. The present invention also relates to pharmaceutical compositions comprising these compounds and to their use as a medicament for the treatment and/or prevention of a disease, disorder or condition in which modulation of microsomal prostaglandin E synthase-1 activity is beneficial, such as pain, inflammation and cancer. 2. The compound of formula (I) according to claim 1 , whereinA is phenyl, indolyl or dihydroindolyl;{'sup': '1', 'sub': '2', 'Ris H or —CHOH;'}{'sup': 2', '4, 'sub': 1-4', '1-4, 'Ris H, bromine, chlorine, fluorine, C-alkyl, fluoro-C-alkyl or —C≡C—R;'}{'sup': '3', 'sub': 1-4', '1-4, 'Ris H, bromine, chlorine, fluorine, C-alkyl, C-alkoxy, cyano or oxo; and'}{'sup': '4', 'sub': 1-4', '3-7', '1-4, 'Ris C-alkyl, C-cycloalkyl or phenyl, wherein phenyl is optionally substituted with C-alkyl.'}3. The compound of formula (I) according to claim 1 , whereinA is phenyl, indolyl or dihydroindolyl;{'sup': '1', 'Ris H;'}{'sup': '2', 'Ris chlorine; and'}{'sup': '3', 'sub': 1-2', '1-2, 'Ris H, C-alkyl, C-alkoxy, cyano or oxo.'}4. The compound of formula (I) according to claim 1 , whereinA is phenyl;{'sup': '1', 'sub': '2', 'Ris H or —CHOH;'}{'sup': '2', 'sub': 1-4', '1-4, 'Ris H, chlorine, C-alkyl or fluoro-C-alkyl; and'}{'sup': '3', 'sub': 1-2', '1-2, 'Ris H, C-alkyl, C-alkoxy, cyano or oxo.'}5. The compound of formula (I) according to claim 1 , wherein A is phenyl and Ris H.6. The compound of formula (I) according to claim 1 , wherein A is indolyl or dihydroindolyl and Ris H.7. The compound of formula (I) according to claim 1 , wherein Ris chlorine.8. A compound claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , selected from the group consisting of2-(2-(4-chloro-2-phenethoxyphenyl)ethylsulfonamido)benzenesulfonamide,2-(2-(4-chloro-2-(2-methoxyphenethoxy)phenyl)ethylsulfonamido)benzenesulfonamide,2-(2-(4-chloro-2-(3-methoxyphenethoxy)phenyl) ...

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Номер записи: 70
04-01-2018 дата публикации

Diindole Compounds Useful In Treatment of Nervous System Disorders

Номер: US20180002283A1
Автор: King Roberta S., Scully Kyle Robert, Worthen David R.
Принадлежит:

The invention provides bridged diindole compounds, related pharmaceutical compositions and methods of use thereof, for the prevention, palliation and/or treatment of nervous system disorders. 2. The compound of claim 1 , comprising a thiodiindole.3. The compound of claim 1 , comprising an ethylenediindole.4. The compound of claim 1 , wherein the compound effectively inhibits a function of a N-methyl-D-aspartate receptor (NMDAR) in an animal.5homo sapiens.. The compound of claim 4 , wherein the animal is6. The compound of claim 4 , wherein the compound binds at least one of NMDAR's subunit isoforms claim 4 , the NR2A and NR2B subunits.7. A pharmaceutical composition claim 1 , comprising the compound of claim 1 , and a pharmaceutically acceptable excipient claim 1 , carrier claim 1 , or diluent.8. The pharmaceutical composition of claim 7 , comprising a thiodiindole.9. The pharmaceutical composition of claim 7 , comprising an ethylenediindole.10. A method of treating a disorder or condition claim 7 , the method comprising administering to a subject in need thereof a therapeutically effective amount of the pharmaceutical composition of .11. The method of claim 10 , wherein the disorder or condition is selected from the group consisting of epilepsies claim 10 , seizures claim 10 , conduction disturbances and electroconvulsive disorders claim 10 , pain claim 10 , fibromyalgia claim 10 , affective disorders such as bipolar disorder and depression claim 10 , autism claim 10 , schizophrenia claim 10 , Parkinson's disease claim 10 , Alzheimer's disease and other dementias claim 10 , attention deficit disorder claim 10 , attention deficit hyperactivity disorder claim 10 , and neurodegeneration of all types claim 10 , manifestations and origins.12. The method of claim 10 , wherein the therapeutically effective amount of the pharmaceutical composition effectively inhibits a function of a N-methyl-D-aspartate receptor (NMDAR) in the subject.13. The method of claim 10 , wherein ...

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Номер записи: 71
03-01-2019 дата публикации

IDO INHIBITORS

Номер: US20190002402A1
Автор: Balog James Aaron, Cherney Emily Charlotte, Markwalder Jay A., Shan Weifang, Williams David K.
Принадлежит:

There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention. 2. The compound according to wherein Rand Rare independently H claim 1 , Cto Calkyl claim 1 , Cto Calkoxy claim 1 , or join together to form cyclopropyl or cyclobutyl.3. The compound according to wherein Z is —NH— and Ris —SOR claim 1 , halo (C-Calkyl) claim 1 , thiazolyl or oxazolyl claim 1 , wherein Ris Cto Calkyl claim 1 , Cto Ccycloalkyl4. The compound according to wherein Z is O and Ris H.5. The compound according to wherein Ris —COR.6. The compound according to wherein Ris a 5 membered heterocycle containing from 1 to 4 heteroatoms selected from N claim 1 , O claim 1 , and S.7. The compound according to wherein Ris H and Ris —CORor —CONRR; Ris H claim 1 , and Ris phenyl claim 1 , pyridyl claim 1 , isoxazolyl claim 1 , thiadiazolyl claim 1 , indolinyl claim 1 , or benzyl claim 1 , wherein Rmay optionally be substituted with from 1 to 3 substituents selected from the group consisting of halo claim 1 , amino claim 1 , phenoxy claim 1 , benzoxy claim 1 , isoxalyl claim 1 , Cto Calkoxy claim 1 , Cto Calkyl claim 1 , halo-Cto Calkyl claim 1 , and CN.8. The compound according to wherein Ris Cto Ccycloalkyl optionally substituted with halo claim 1 , —OH or Cto Calkoxy; Cto Calkyl optionally substituted with halo claim 1 , —OH or phenyl claim 1 , wherein said phenyl is optionally substituted with Cto Chaloalkyl claim 1 , Cto Calkoxy claim 1 , halo or Cto Calkyl; Cto Calkenyl; Cto Calkoxy; or benzyl optionally substituted with Cto Calkyl claim 1 , halo claim 1 , Cto Calkoxy claim 1 , or haloalkyl.9. The compound according to wherein Ris a Cto Cheterocycloalkyl containing from 1 to 4 heteroatoms selected from O claim 1 , N or S.10. The compound ...

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Номер записи: 72
04-01-2018 дата публикации

SYNTHESIS OF CYCLOPROPYL INDOLES AND CYCLOHEPTA[B]INDOLES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND METHOD OF USING THEM

Номер: US20180002318A1
Автор: LI Xiaoxun, Tang Weiping
Принадлежит:

Methods of making indole analogs using a rhodium-containing catalyst are described, along with methods of using the compounds to treat hyperglycemic, hyperlipidemic, or autoimmune disorders in mammals, and corresponding pharmaceutical compositions. Disclosed herein is a method of making indoles. The method comprises contacting a reactant of formula I wherein E is a protecting group, —SO2-Aryl, or —SO2-substituted-Aryl; and R and R2 are independently selected from the group consisting of hydrogen, halo, C1-C12-alkyl and aryl; with a rhodium(l)-containing catalyst. 2. The method of claim 1 , which yields a product mixture comprising a compound of formula (II).3. The method of claim 1 , which yields a product mixture comprising a compound of formula (III).4. The method of claim 1 , which yields a product mixture comprising a compound of formula (IV).5. The method of claim 1 , conducted in the absence of the alpha-alkene-containing co-reactant.7. The method of claim 1 , wherein the rhodium(I)-containing catalyst comprises [Rh(CO)Cl].8. The method of claim 7 , which yields a product mixture comprising a compound of formula (II).9. The method of claim 7 , which yields a product mixture comprising a compound of formula (III).10. The method of claim 7 , which yields a product mixture comprising a compound of formula (IV).11. The method of claim 7 , conducted in the absence of the alpha-alkene-containing co-reactant.13. The method of claim 1 , wherein the reactant of formula I is contacted with the catalyst in the presence of carbon monoxide.14. The method of claim 13 , which yields a product mixture comprising a compound of formula (II).15. The method of claim 13 , which yields a product mixture comprising a compound of formula (III).16. The method of claim 13 , which yields a product mixture comprising a compound of formula (IV).17. The method of claim 13 , conducted in the absence of the alpha-alkene-containing co-reactant.20. A pharmaceutical composition for treating ...

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Номер записи: 73
01-01-2015 дата публикации

PRIMARY CARBOXAMIDES AS BTK INHIBITORS

Номер: US20150005279A1
Автор: Bonafoux Dominique, Davis Heather M., Frank Kristine E., Friedman Michael M., Herold J. Martin, Hoemann Michael Z., Huntley Raymond, Osuma Augustine, Sheppard George, Somal Gagandeep K., Van Camp Jennifer, Van Epps Stacy A., Vasudevan Anil, Wallace Grier A., Wang Lu, Wang Zhi, Wilson Noel S.
Принадлежит: AbbVie Inc.

The invention provides compounds of Formula (I) 2. The compound according to claim 1 , wherein Y is CRand Rof Y is H claim 1 , optionally substituted ethenyl claim 1 , optionally substituted ethyl claim 1 , optionally substituted methyl claim 1 , optionally substituted 2 claim 1 ,3-dihydrobenzofuranyl claim 1 , optionally substituted 1 claim 1 ,4-dioxanyl claim 1 , optionally substituted 3 claim 1 ,4-dihydro-2H-benzo[b.][1 claim 1 ,4]oxazinyl claim 1 , optionally substituted 6 claim 1 ,7-dihydro-4H-pyrazolo[5 claim 1 ,1-c][1 claim 1 ,4]oxazinyl claim 1 , optionally substituted chromanyl claim 1 , optionally substituted cyclohexenyl claim 1 , optionally substituted cyclopropyl claim 1 , optionally substituted tetrahydrofuranyl claim 1 , optionally substituted isochromanyl claim 1 , optionally substituted 1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydro-isoquinolinyl claim 1 , optionally substituted isoxazolyl claim 1 , optionally substituted morpholinyl claim 1 , optionally substituted oxetanyl claim 1 , optionally substituted phenyl claim 1 , optionally substituted piperidinyl claim 1 , optionally substituted piperazinyl claim 1 , optionally substituted 3 claim 1 ,6-dihydro-2H-pyranyl claim 1 , optionally substituted pyrano[4 claim 1 ,3-b]pyridinyl claim 1 , optionally substituted pyrazolyl claim 1 , optionally substituted pyridinyl claim 1 , optionally substituted 3H-pyridin-1-one claim 1 , optionally substituted 1 claim 1 ,2 claim 1 ,3 claim 1 ,6-tetrahydropyridinyl claim 1 , optionally substituted pyrimidinyl claim 1 , optionally substituted pyrrolidinyl claim 1 , optionally substituted 2 claim 1 ,5-dihydropyrrolyl claim 1 , optionally substituted tetrahydropyranyl or optionally substituted tetrahydro-2H-thiopyranyl.3. The compound according to wherein Ris H or Ris optionally substituted by one or more substituents independently selected from the group consisting of CN claim 2 , OH claim 2 , ═O claim 2 , halogen claim 2 , (C-C)alkyl claim 2 , (C-C)alkoxy claim 2 , — ...

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Номер записи: 74
01-01-2015 дата публикации

PROCESSES FOR PREPARING INDOLES

Номер: US20150005494A1
Автор: Wei Ye, Yoshikai Naohiko
Принадлежит:

Methods for the synthesis of an indole in provided. Methods comprise oxidizing a N-aryl imine in the presence of a palladium-based catalyst, an oxidant, and a solvent. 128.-. (canceled)30. The method according to claim 29 , wherein Rat each occurrence is independently selected from the group consisting of hydrogen claim 29 , alkyl claim 29 , —O-alkyl claim 29 , and halogen.31. The method according to claim 29 , wherein Rat each occurrence is independently selected from the group consisting of —H claim 29 , —OCH claim 29 , and —Cl.32. The method according to claim 29 , wherein Ris positioned on the phenyl ring in 4-position with respect to the bond linking the phenyl to the —N—H group according to Formula (I) or the —N═C group according to Formula (II).34. The method according to claim 29 , wherein Ris hydrogen or phenyl.35. The method according to claim 29 , wherein the indole is 2-aryl indole claim 29 , 2-alkenyl indole claim 29 , 2 claim 29 ,3-diaryl indole claim 29 , 2-aryl-3-alkenyl indole claim 29 , 2-alkenyl-3-aryl indole claim 29 , 2 claim 29 ,3-dialkenyl indole claim 29 , 2-aryl-3-alkyl indole claim 29 , or 2-alkenyl-3-alkyl indole.37. The method according to claim 29 , wherein the palladium-based catalyst is selected from the group consisting of palladium metal claim 29 , palladium (II) acetate claim 29 , sodium palladium (II) chloride claim 29 , palladium (II) acetylacetonate claim 29 , palladium(II) trifluoroacetate claim 29 , palladium hydroxide claim 29 , palladium(II) bromide claim 29 , palladium (II) chloride claim 29 , palladium(II) cyanide claim 29 , palladium(II) hexafluoroacetylacetonate claim 29 , palladium(II) iodide claim 29 , palladium(II) nitrate dehydrate claim 29 , palladium(II) nitrate hydrate claim 29 , palladium(II) oxide claim 29 , palladium (II) propionate claim 29 , palladium (II) sulfate claim 29 , palladium (II) sulfide claim 29 , or mixtures thereof.38. The method according to claim 37 , wherein the palladium-based catalyst ...

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Номер записи: 75
01-01-2015 дата публикации

NOVEL RUTHENIUM CATALYSTS AND THEIR USE FOR ASYMMETRIC REDUCTION OF KETONES

Номер: US20150005500A1
Автор: HADDAD Nizar, LEE Heewon, QU Bo, RODRIGUEZ Sonia, SENANAYAKE Chris Hugh
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Disclosed are novel ruthenium compounds of formula (Ia) and (Ib): 2. The compound of formula (Ia) or (Ib) according to claim 1 , wherein Ris —H.3. The compound of formula (Ia) or (Ib) according to claim 1 , wherein Ris —CH.4. The compound of formula (Ia) or (Ib) according to claim 1 , wherein Ris —OCH.5. The compound of formula (Ia) or (Ib) according to claim 1 , wherein the diamine ligand is compound 4.6. The compound of formula (Ia) or (Ib) according to claim 1 , wherein the diamine ligand is compound 5.7. The compound of formula (Ia) or (Ib) according to claim 1 , wherein the diamine ligand is compound 6.8. The compound of formula (Ia) or (Ib) according to claim 1 , wherein the diamine ligand is compound 7.9. The compound of formula (Ia) or (Ib) according to claim 1 , wherein the diamine ligand is compound 9.10. The compound of formula (Ia) or (Ib) according to claim 1 , wherein the diamine ligand is compound 12.11. The compound of formula (Ia) or (Ib) according to claim 1 , wherein Ris —OCH.12. The compound of formula (Ia) or (Ib) according to claim 1 , wherein the diamine ligand is compound 8.13. The compound of formula (Ia) or (Ib) according to claim 12 , wherein Ris —H.14. The compound of formula (Ia) or (Ib) according to claim 12 , wherein Ris —CH.15. The compound of formula (Ia) or (Ib) according to claim 12 , wherein Ris —OCH.16. The compound of formula (Ia) according to .17. The compound of formula (Ib) according to . The invention relates to a new family of amine-tunable ruthenium catalysts based on chiral bisdihydrobenzooxaphosphole ligands (BIBOP ligands). The catalysts are useful for asymmetric hydrogenation and transfer hydrogenation of a variety of highly challenging ketones, including heteroaryl cyclic ketones.Asymmetric reduction of ketones is a key transformation in the pharmaceutical industry for the preparation of enantiomerically pure alcohols, particularly those bearing heterocycles (see, e.g., (Eds.: J. G. De Vries, C. J. Elsevier), Willey- ...

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Номер записи: 76
04-01-2018 дата публикации

SPIRO-TYPE COMPOUND AND ORGANIC LIGHT EMITTING ELEMENT COMPRISING SAME

Номер: US20180006233A1
Автор: Cha Yongbum, Kim Jin Joo, KIM Jungbum, Suh Sang Duk
Принадлежит: LG CHEM, LTD.

The present specification provides a compound having a spiro structure, and an organic light emitting device including the same. 3. The compound of claim 1 , wherein HAr is a substituted or unsubstituted pyridyl group; a substituted or unsubstituted pyrimidyl group; a substituted or unsubstituted triazinyl group; a substituted or unsubstituted furan group; a substituted or unsubstituted thiophene group; a substituted or unsubstituted oxadiazole group; a substituted or unsubstituted thiadiazole group; a substituted or unsubstituted phenanthroline group; a substituted or unsubstituted quinolinyl group; a substituted or unsubstituted isoquinolinyl group; a substituted or unsubstituted quinazoline group; a substituted or unsubstituted benzoxazole group; a substituted or unsubstituted benzothiazole group; a substituted or unsubstituted benzimidazole group; a substituted or unsubstituted phenoxazine group; a substituted or unsubstituted phenothiazine group; a substituted or unsubstituted dibenzofuran group; a substituted or unsubstituted dibenzothiophene group; a substituted or unsubstituted carbazole group; or a substituted or unsubstituted diarylphosphine oxide group.7. An organic light emitting device comprising:a first electrode;a second electrode provided opposite to the first electrode; andone or more organic material layers provided between the first electrode and the second electrode,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein one or more layers of the organic material layers include the compound of .'}8. The organic light emitting device of claim 7 , wherein the organic material layer includes a light emitting layer claim 7 , and the light emitting layer includes the compound.9. The organic light emitting device of claim 8 , wherein the light emitting layer further includes a light emitting dopant.10. The organic light emitting device of claim 7 , wherein the organic material layer includes an electron injection layer claim 7 , an electron transfer ...

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Номер записи: 77
14-01-2021 дата публикации

BICYCLIC COMPOUNDS AND THEIR USE IN THE TREATMENT OF CANCER

Номер: US20210008046A1
Автор: BRAVO Yalda, BURCH Jason David, Chen Austin Chih-Yu, NAGAMIZO Joe Fred
Принадлежит:

The present disclosure is directed to novel compounds of Formula I and pharmaceutically acceptable salts, solvates, solvates of the salt and prodrugs thereof, useful in the prevention (e.g., delaying the onset of or reducing the risk of developing) and treatment (e.g., controlling, alleviating, or slowing the progression of) of cancer, including glioblastoma, bone cancer, head and neck cancer, melanoma, basal cell carcinoma, squamous cell carcinoma, adenocarcinoma, oral cancer, esophageal cancer, gastric cancer, intestinal cancer, colon cancer, bladder cancer, hepatocellular carcinoma, renal cell carcinoma, pancreatic cancer, ovarian cancer, cervical cancer, lung cancer, breast cancer, and prostate cancer. The compounds of the disclosure are selective antagonists of the EP4 receptor and useful treatment of various diseases that may be ameliorated with blockade of PGE2-mediated signaling. 2. A compound of wherein Ar is aryl or heteroaryl optionally substituted with 1 to 3 substituents independently selected from:(a) halogen,(b) cyano,{'sub': 1', '6, '(c) C-Calkyl,'}{'sub': '5', '(d) SF,'}{'sub': 1', '6, '(e) C-Chaloalkyl,'}{'sup': b', 'b, 'sub': 1', '6', '3', '6', '1', '6, '(f) ORwherein Ris C-Calkyl, aryl, heteroaryl, C-Ccycloalkyl or C-Chaloalkyl;'}(g) heterocycle,(h) aryl, and(i) heteroaryl.3. A compound of or wherein Ar is phenyl.4. A compound any one of to wherein each of X claim 1 , X claim 1 , X claim 1 , Xand Xis independently C—R claim 1 , or one of X claim 1 , X claim 1 , X claim 1 , Xand Xis N claim 1 , and the others are each independently C—R.5. A compound of wherein each of X claim 4 , X claim 4 , X claim 4 , Xand Xis independently C—R.6. A compound of any of to wherein Ris H or a halogen atom.7. A compound of any of to wherein W is selected from the group consisting of:{'sub': '2', '(a) COH; and'}(b) 1H-tetrazole.8. A compound of any of to wherein Z is —CH—.9. A compound of any of to wherein Y is a bond or —CH—.10. A compound of any of to wherein Rand ...

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Номер записи: 78
12-01-2017 дата публикации

METHOD FOR PRODUCING OPTICALLY ACTIVE CARBOXYLIC ACID ESTER

Номер: US20170008820A1
Автор: Shiina Isamu
Принадлежит:

Provided is a method for producing an optically active carboxylic acid ester at a high yield and with high enantioselectivity using dynamic kinetic resolution, said optically active carboxylic acid ester having an α-nitrogen substituent. This method for producing an optically active carboxylic acid ester includes a step in which racemic carboxylic acid represented by formula (a) and a specific alcohol or phenol derivative are reacted in a polar solvent having a dipole moment of at least 3.5 in the presence of an acid anhydride and an asymmetric catalyst, one enantiomer of the racemic carboxylic acid is selectively esterified, and the other enantiomer is racemized. In formula (a), Ra1 represents a nitrogen-containing heteroaromatic ring group bonded to an assymetric carbon via a nitrogen atom constituting a ring, and Ra2 is an organic group. 3. The method for producing an optically active carboxylic acid ester according to claim 1 , wherein Rin formula (a) is a 1H-pyrrol-1-yl group.4. The method for producing an optically active carboxylic acid ester according to claim 1 , wherein the polar solvent having a dipole moment of 3.5 or more is dimethylacetamide claim 1 , dimethylformamide claim 1 , 1 claim 1 ,3-dimethyl-2-imidazolidinone claim 1 , N-methylpyrrolidone claim 1 , or dimethyl sulfoxide.5. The method for producing an optically active carboxylic acid ester according to claim 1 , wherein the step is performed in the presence of a base.7. The method for producing an optically active carboxylic acid ester according to claim 6 , wherein at least one of R claim 6 , R claim 6 , or Ris a methyl group.8. The method for producing an optically active carboxylic acid ester according to claim 6 , wherein the base is diisopropylethylamine claim 6 , triethylamine claim 6 , dimethylethylamine claim 6 , dimethylisopropylamine claim 6 , diethylmethylamine claim 6 , or diisopropylmethylamine.10. The method for producing an optically active carboxylic acid ester according to ...

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Номер записи: 79
14-01-2016 дата публикации

BCL-2-SELECTIVE APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE DISEASES

Номер: US20160009687A1
Автор: Ding Hong, Elmore Steven W., Hasvold Lisa, Hexamer Laura A., Kunzer Aaron R., McClellan William J., Souers Andrew J., Sullivan Gerard M., Tao Zhi-Fu, Wendt Michael D.
Принадлежит:

Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein. 114-. (canceled)15. A compound , or a therapeutically acceptable salt thereof , wherein the compound is selected from the group consisting of:2-(benzyloxy)-4-(4-((4′-chloro-1,1-′-biphenyl-2-yl)methyl)piperazin-1-yl)-N-((3-nitro-4-((tetrahydro-2H-pyran-4-ylmethyl)amino)phenyl)sulfonyl)benzamide;4-(4-((4′-chloro-1,1′-biphenyl-2-yl)methyl)piperazin-1-yl)-N-((3-nitro-4-((tetrahydro-2H-pyran-4-ylmethyl)amino)phenyl)sulfonyl)-2-(2-phenylethoxy)benzamide;2-benzyl-4-(4-((4′-chloro-1,1′-biphenyl-2-yl)methyl)piperazin-1-yl)-N-((3-nitro-4-((tetrahydro-2H-pyran-4-ylmethyl)amino)phenyl)sulfonyl)benzamide;2-benzyl-4-(4-((4′-chloro-1,1′-biphenyl-2-yl)methyl)piperazin-1-yl)-N-((4-((tetrahydro-2H-pyran-4-ylmethyl)amino)phenyl)sulfonyl)benzamide;2-benzyl-4-(4-((4′-chloro-1,1′-biphenyl-2-yl)methyl)piperazin-1-yl)-N-((4-((3-morpholin-4-ylpropyl)amino)-3-nitrophenyl)sulfonyl)benzamide;4-(4-((4′-chloro-1,1′-biphenyl-2-yl)methyl)piperazin-1-yl)-N-((3-nitro-4-((tetrahydro-2H-pyran-4-ylmethyl)amino)phenyl)sulfonyl)-2-(2-phenylethyl)benzamide;2-(benzylamino)-4-(4-((4′-chloro-1,1′-biphenyl-2-yl)methyl)piperazin-1-yl)-N-((3-nitro-4-((tetrahydro-2H-pyran-4-ylmethyl)amino)phenyl)sulfonyl)benzamide;4-(4-((4′-chloro-1,1′-biphenyl-2-yl)methyl)piperazin-1-yl)-2-methoxy-N-((3-nitro-4-((tetrahydro-2H-pyran-4-ylmethyl)amino)phenyl)sulfonyl)benzamide;4-(4-((4′-chloro-1,1′-biphenyl-2-yl)methyl)piperazin-1-yl)-N-((4-((3-(dimethylamino)propyl)amino)-3-nitrophenyl)sulfonyl)-2-(1H-indol-6-yloxy)benzamide;N-[(3-{[chloro(difluoro)methyl]sulfonyl}-4-{[3-(dimethylamino)propyl]amino}phenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-indol-4-yloxy)benzamide;4-(4-((4′-chloro-1,1′-biphenyl-2-yl)methyl)piperazin-1-yl)-N-((3-nitro-4-((tetrahydro-2H ...

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Номер записи: 80
11-01-2018 дата публикации

Ligand-Enabled meta-C-H Activation Using a Transient Mediator

Номер: US20180009739A1
Автор: YU JIN-QUAN
Принадлежит:

An alternative approach to formation of a C-C bond at a meta-position of an aromatic compound is disclosed that employs an ethylenically unsaturated bicyclic compound as a transient mediator to achieve meta-selective C-H activation with a simple and common ortho-directing group. The use of a pyridine-based ligand assists in relaying the palladium catalyst to the meta-position by the unsaturated bicyclic compound following initial ortho-C-H activation. 2. The method according to claim 1 , wherein circled Ar is carbocyclic.3. The method according to claim 2 , wherein one or both of Vand Vare other than hydrido.4. The method according to claim 3 , wherein Z is C.5. The method according to claim 4 , wherein W is C and X is ═O.6. The method according to claim 4 , wherein Ris a 4-(CF)CFNH— group.7. The method according to claim 4 , wherein Ris H.8. The method according to claim 4 , wherein Ris HY.9. The method according to claim 4 , wherein Ris HR.10. The method according to claim 1 , wherein W is nitrogen that is a ring atom of an aromatic ring system that contains at least one additional nitrogen atom that is adjacent to W in the aromatic ring.11. The method according to claim 1 , wherein W is the carbon of a >CH— group claim 1 , X is a N-sulfonamido or N-carboxamido group claim 1 , and Ris a C-C-hydrocarbyl carboxylate group.12. The method according to claim 1 , wherein W is C and W claim 1 , X and Rtogether form a heteroaromatic ring structure that contains one ring or two fused rings that each contains 5- or 6-members and a total of one to four heteroatoms that are independently nitrogen claim 1 , oxygen or sulfur.13. The method according to claim 1 , wherein said reactive coupling agent is an aromatic claim 1 , benzylic or aliphatic bromide or iodide compound of the Formula R-Q claim 1 , wherein Ris an aromatic group claim 1 , a straight claim 1 , branched or cyclic aliphatic C-C-hydrocarbyl group claim 1 , or a benzylic group claim 1 , and Q is bromo or iodo.14. ...

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Номер записи: 81
14-01-2021 дата публикации

METHODS FOR TREATING PROTOZOAN INFECTIONS

Номер: US20210009552A1
Автор: Abraham Rebecca, Keenan Martine, McCluskey Adam, Page Stephen, Stevens Andrew
Принадлежит:

The invention provides compounds of Formula (I), and their use in methods for treating or preventing a protozoan infection in a subject using a compound of Formula (I). The invention also provides the use of a compound of Formula (I) in the manufacture of a medicament for the treatment of a protozoan infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a protozoan infection in a subject and to a medical device comprising the composition of the invention. 141.-. (canceled)43. A composition comprising the compound of .44. A pharmaceutical or veterinarian composition comprising the compound of and a pharmaceutically acceptable excipient.45. The compound of claim 42 , wherein the compound is 4 claim 42 ,6-bis(2-((E)-(6-chloropyridin-3-yl)methylene)hydrazinyl)pyrimidin-2-amine or a stereoisomer claim 42 , tautomer claim 42 , pharmaceutically acceptable salt thereof.46. The compound of claim 42 , wherein the compound is 4 claim 42 ,6-bis(2-((E)-pyridin-3-ylmethylene)hydrazinyl)pyrimidin-2-amine or a stereoisomer claim 42 , tautomer claim 42 , pharmaceutically acceptable salt thereof.47. The compound of claim 42 , wherein the compound is 4 claim 42 ,6-bis(2-((E)-pyridin-2-ylmethylene)hydrazinyl)pyrimidin-2-amine or a stereoisomer claim 42 , tautomer claim 42 , pharmaceutically acceptable salt thereof.48. The compound of claim 42 , wherein the compound is 4 claim 42 ,6-bis(2-((E)-pyridin-4-ylmethylene)hydrazinyl)pyrimidin-2-amine or a stereoisomer claim 42 , tautomer claim 42 , pharmaceutically acceptable salt thereof.49. The compound of claim 42 , wherein the compound is 4 claim 42 ,6-bis(2-((E)-2 claim 42 ,5-dihydroxybenzylidene)hydrazinyl)pyrimidin-2-aminium 2-formyl-4-hydroxyphenolate or a stereoisomer claim 42 , tautomer claim 42 , pharmaceutically acceptable salt thereof.50. The compound of claim 42 , wherein the compound is 4 claim 42 ,6-bis(2-((E)-3 claim 42 ,4-dihydroxybenzylidene)hydrazinyl) ...

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Номер записи: 82
09-01-2020 дата публикации

FLOW BATTERIES INCORPORATING A NITROXIDE COMPOUND WITHIN AN AQUEOUS ELECTROLYTE SOLUTION

Номер: US20200014054A1
Автор: Humbarger Scott Thomas, MILLARD Matthew, NELSON Emily Grace, Norman Zachariah M.
Принадлежит:

Flow batteries can include a first half-cell containing a first aqueous electrolyte solution, a second half-cell containing a second aqueous electrolyte solution, and a separator disposed between the first half-cell and the second half-cell. The first aqueous electrolyte solution contains a first redox-active material, and the second aqueous electrolyte solution contains a second redox-active material. At least one of the first redox-active material and the second redox-active material is a nitroxide compound or a salt thereof. Particular nitroxide compounds can include a doubly bonded oxygen contained in a ring bearing the nitroxide group, a doubly bonded oxygen appended to a ring bearing the nitroxide group, sulfate or phosphate groups appended to a ring bearing the nitroxide group, various heterocyclic rings bearing the nitroxide group, or acyclic nitroxide compounds. 2. The flow battery of claim 1 , wherein each Ris H claim 1 , and R-Rare each methyl.3. The flow battery of claim 1 , wherein Ais of S(═O) claim 1 , S(═O) claim 1 , P(═O)R claim 1 , or P(═O)OR.4. The flow battery of claim 3 , wherein Ais S(═O).6. The flow battery of claim 5 , wherein each Ris H claim 5 , and R-Rare each methyl.7. The flow battery of claim 5 , wherein Ais S(═O)OH claim 5 , S(═O)R claim 5 , S(═O)R claim 5 , S(═O)NRR claim 5 , OS(═O)OR claim 5 , NRC(═O)NRR claim 5 , NRC(═S)NRR claim 5 , or NRS(═O)R.8. The flow battery of claim 7 , wherein Ais S(═O)NRRor NRC(═S)NRR claim 7 , and at least one Rbound to N is H.9. The flow battery of claim 7 , wherein Ais OS(═O)OR.10. The flow battery of claim 9 , wherein Ris H.11. A flow battery comprising:a first half-cell containing a first aqueous electrolyte solution;a second half-cell containing a second aqueous electrolyte solution; anda separator disposed between the first half-cell and the second half-cell;wherein at least one of the first redox-active material and the second redox-active material comprises a nitroxide compound or a salt thereof ...

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Номер записи: 83
17-01-2019 дата публикации

Selective androgen receptor degrader (sard) ligands and methods of use thereof

Номер: US20190015387A1
Автор: Dong-Jin Hwang, Duane D. Miller, Ramesh Narayanan, Thamarai Ponnusamy, Yali He
Принадлежит: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION

This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including heterocyclic anilide rings and their synthetic precursors, R-isomers, and non-hydroxylated and/or non-chiral propanamides, and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

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Номер записи: 84
21-01-2016 дата публикации

COMPOUNDS FOR TREATING INFLAMMATORY AND HYPERPROLIFERATIVE DISEASES

Номер: US20160016931A1
Автор: BORNMANN William G., FORD, JR. Richard J., Maxwell David, PAL Ashutosh, PENG Zhenghong, PHAM Lan V., TAMAYO Archito
Принадлежит:

Compounds are provided that can exhibit anti-cancer and/or anti-inflammatory properties, in some aspects, methods of treating an inflammatory disease or a hyperproliferative disease, such as cancer, with the compounds are provided.

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Номер записи: 85
15-01-2015 дата публикации

N-(2-(HETARYL)ARYL)ARYLSULFONAMIDES AND N-(2-(HETARYL)HETARYL)ARYLSULFONAMIDES

Номер: US20150018337A1
Автор: Charvat Trevor T., Hu Cheng, Melikian Anita, Novack Aaron, Pennell Andrew M.K., Powers Jay, Punna Sreenivas, Sullivan Edward J., Thomas William D., Ungashe Solomon, Zhang Penglie
Принадлежит:

Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists. 138-. (canceled)45. The compound of claim 44 , or a salt thereof.52. The compound of claim 39 , wherein said compound is selected from the group consisting of:N-(2-(1H-[1,2,3]triazolo[4,5-b]pyridin-1-yl)-4-chlorophenyl)-4-(1-(methoxyimino)ethyl)benzenesulfonamide;N-(2-(1H-[1,2,3]triazolo[4,5-b]pyridin-1-yl)-4-chlorophenyl)-4-(1-aminoethyl)benzenesulfonamide;N-(2-(1H-[1,2,3]triazolo[4,5-b]pyridin-1-yl)-4-chlorophenyl)-4-(1-(methylamino)ethyl)benzenesulfonamide;N-(2-(1H-[1,2,3]triazolo[4,5-b]pyridin-1-yl)-4-chlorophenyl)-4-(1-(dimethylamino)ethyl)benzenesulfonamide;N-(2-(1H-[1,2,3]triazolo[4,5-b]pyridin-1-yl)-4-chlorophenyl)-4-(1-morpholinoethyl)benzenesulfonamide;N-(4-Chloro-2[1,2,3]triazolo[4,5-b]pyridin-1-yl-phenyl)-4-(1-hydroxy-1-methyl-ethyl)-benzene-sulfonamide;N-(2-(1H-[1,2,3]triazolo[4,5-b]pyridin-1-yl)-4-chlorophenyl)-4-(1-(ethoxyimino)ethyl)benzenesulfonamide;N-(2-(1H-[1,2,3]triazolo[4,5-b]pyridin-1-yl)-4-chlorophenyl)-4-(1-(allyloxyimino)ethyl)benzenesulfonamide;N-(2-(1H-[1,2,3]triazolo[4,5-b]pyridin-1-yl)-4-chlorophenyl)-4-(1-(tert-butoxyimina)ethyl)benzenesulfonamide;2-(1-(4-(N-(2-(1H-[1,2,3]triazolo[4,5-b]pyridin-1-yl)-4-chlorophenyl)sulfamoyl)phenyl)ethylideneaminooxy)acetic acid;N-(2-(1H-[1,2,3]triazolo[4,5-b]pyridin-1-yl)-4-chlorophenyl)-4-(1-hydroxy-2-methylpropan-2-yl)benzenesulfonamide;methyl 2-(4-(N-(2-(1H-[1,2,3]triazolo[4,5-b]pyridin-1-yl)-4-chlorophenyl)sulfamoyl)phenyl)-2-methylpropanoate;N-(2-(1H-[1,2,3]triazolo[4,5-b]pyridin-1-yl)-4-chlorophenyl)-4-isopropylbenzenesulfonamide;N-(2-(1H-[1,2,3]triazolo[4,5-b]pyridin-1-yl)-4- ...

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Номер записи: 86
15-01-2015 дата публикации

HIGHLY SELECTIVE SIGMA RECEPTOR LIGANDS

Номер: US20150018339A1
Автор: Abdelazeem Ahmed Hassan Amin, Avery Bonnie Ann, CHIN FREDERICK T., MCCURDY Christopher R., Mesangeau Christophe, Poupaert Jacques Henri
Принадлежит:

Compounds having the general formula II, III, or IV 6. The compounds of claim 1 , wherein Y=O and Z=O.7. The compounds of claim 1 , wherein Y=S and Z=S.8. The compounds of claim 1 , where Y=CHor Y=CH.10. The compounds of claim 1 , wherein X is fluoro.11. The compounds of claim 1 , wherein X is trifluoromethyl.12. The compounds of claim 1 , wherein the alkylene bridging moiety is substituted by methyl or trifluoromethyl.13. A method of treating a subject for alleviation of affects in the subject resulting from drug intake or drug abuse by the subject comprising administering to the subject a therapeutically effective amount of at least one compound according to .14. A method according to wherein the drug abuse or drug intake results from methamphetamine intake or methamphetamine abuse by the subject.15. A method according to wherein the drug intake or drug intake results from cocaine abuse or cocaine intake by the subject.16. A method of treating a subject having a need for therapy involving sigma receptors comprising administering to the subject an effective amount of at least one compound of .17. A method of treating a subject to prevent neurotoxic effects resulting from drug abuse or drug intake by the subject comprising administering to the subject a therapeutically effective amount of at least one compound according to .18. A radioligand composition comprising at least one compound according to wherein at least one compound contains a radioactive element.19. A pharmaceutical composition comprising at least one compound according to and an acceptable carrier or excipient.22. A method of treating a subject for alleviation of affects in the subject resulting from drug intake or drug abuse by the subject comprising administering to the subject a therapeutically effective amount of the compound according to .23. A method according to wherein the drug abuse or drug intake results from methamphetamine intake or methamphetamine abuse by the subject.24. A method ...

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Номер записи: 87
18-01-2018 дата публикации

BLUE FLUORESCENT EMITTERS

Номер: US20180016493A1
Автор: Hofmann Simone, Leo Karl, Lygaitis Ramunas, Oberlaender Martin, Reineke Sebastian, Scholz Reinhard, Zeika Olaf
Принадлежит:

The present invention relates to compounds of the formula (I) 8. Use of at least one compound according to in an optoelectronic component from the group comprising: an organic electroluminescent device (OLED) claim 1 , an organic integrated circuit (O-IC) claim 1 , an organic field-effect transistor (O-FET) claim 1 , an organic thin-film transistor (O-TFT) claim 1 , an organic light-emitting transistor (O-LET) claim 1 , an organic solar cell (O-SC) claim 1 , an organic optical detector claim 1 , an organic photoreceptor claim 1 , an organic field-quench device (O-FQD) claim 1 , a light-emitting electrochemical cell (LEC) claim 1 , or an organic laser diode (O-laser).9. An optoelectronic component comprising at least one compound according to . The present application is a national stage entry according to 35 U.S.C. §371 of PCT Application No. PCT/EP2016/052413 filed on Feb. 4, 2016, which claims priority to German Patent Application No. 10 2015 101 767.9, filed on Feb. 6, 2015; both of which are herein incorporated by reference in their entirety.The subject matter herein generally provides compounds of formula (I) as defined herein, as well as their use as emitter or carrier material in an optoelectronic component.The development of novel functional compounds for use in electronic devices is currently the subject of intensive research. The aim here is the development and study of compounds which have not been used to date in electronic devices, and the development of compounds which enable an improved profile of properties of the devices.According to a non-limiting embodiment, the term “optoelectronic component” is understood to mean inter alia organic integrated circuits (OICs), organic field-effect transistors (OFETs), organic thin-film transistors (OTFTs), organic light-emitting transistors (OLETs), organic solar cells (OSCs), organic optical detectors, organic photoreceptors, organic field-quench devices (OFQDs), organic light-emitting electrochemical cells ( ...

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Номер записи: 88
19-01-2017 дата публикации

NEAR-INFRARED CUT FILTER AND IMAGING DEVICE

Номер: US20170017024A1
Автор: Hasegawa Makoto, Sugiyama Takashi
Принадлежит: Asahi Glass Company, Limited

A near-infrared cut filter has an absorption layer and a reflection layer and satisfies following requirements: 1. A near-infrared cut filter comprising an absorption layer and a reflection layer and satisfying following requirements (1) to (3):(1) average transmittance (R) in the wavelength range of 620 to 750 nm is 20% or less and average transmittance (G) in the wavelength range of 495 to 570 nm is 90% or more in a spectral transmittance curve at an incident angle of 0°, and the ratio (R)/(G) of the average transmittance is 0.20 or less;{'sub': 0(600-725)', '30(600-725)', '0(600-725)', '30(600-725), '(2) difference T−T| between an integral value Tof transmittance in the wavelength range of 600 to 725 nm in the spectral transmittance curve at an incident angle of 0°, and an integral value Tof transmittance in the wavelength range of 600 to 725 nm in a spectral transmittance curve at an incident angle of 30° is 3%-nm or less; and'}{'sub': T(80)', 'T(50)', 'T(20)', 'T(80)', 'T(50)', 'T(20), 'claim-text': [{'br': None, 'sub': T(80)', 'T(80), '0≦λIR−λ≦30 nm\u2003\u2003(a),'}, {'br': None, 'sub': T(50)', 'T(50), '0≦λIR−λ≦35 nm\u2003\u2003(b),'}, {'br': None, 'sub': T(20)', 'T(20), '0≦λIR−λ≦37 nm\u2003\u2003(c),'}], '(3) the near-infrared cut filter has a wavelength λIRat which transmittance becomes 80%, a wavelength λIRat which transmittance becomes 50%, and a wavelength λIRat which transmittance becomes 20% in the wavelength range of 550 to 750 nm in the spectral transmittance curve at an incident angle of 0° normalized by maximum transmittance in the wavelength range of 450 to 650 nm, and the wavelengths λIR, λIR, and λIRsatisfy following formulae (a), (b) and (c), respectively{'sub': T(80)', 'T(50)', 'T(20), 'where λ, λand λare wavelengths on a long wavelength side where relative visibility of 0.8, 0.5 and 0.2 is exhibited in a relative visibility curve, respectively.'}2. The near-infrared cut filter according to claim 1 , wherein the wavelengths λIR claim 1 , λIR ...

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Номер записи: 89
17-01-2019 дата публикации

TRIFLUOROMETHOXYLATION OF ARENES VIA INTRAMOLECULAR TRIFLUOROMETHOXY GROUP MIGRATION

Номер: US20190016670A1
Автор: Hojczyk Katarzyna N., Ngai Ming-Yu
Принадлежит: The Research Foundation for The State University of New York

The present invention provides a process of producing a trifluoromethoxylated aryl or trifluoromethoxylated heteroaryl having the structure: 19-. (canceled)11. The process of claim 10 , wherein the second suitable solvent is chloroform claim 10 , dichloromethane claim 10 , nitromethane claim 10 , dimethylforamide claim 10 , diethyl ether claim 10 , tetrahydrofuran claim 10 , dioxane claim 10 , dichloroethane claim 10 , or hexane.12. The process of claim 10 , wherein step (b) is carried out at room temperature.13. The process of claim 10 , wherein step (b) is carried out at a temperature of 50-140° C.14. The process of claim 10 , wherein the compound is maintained in the second suitable solvent for 10-50 hours.15. The process of claim 10 , wherein A is a phenyl or pyridine.16. The process of claim 10 , wherein A is a furan claim 10 , thiophene claim 10 , pyrrole claim 10 , thiazole claim 10 , imidazole claim 10 , pyrazole claim 10 , isooxazole claim 10 , isothiazole claim 10 , naphthalene claim 10 , anthracene claim 10 , pyrimidine claim 10 , pyrazine claim 10 , pyridazine claim 10 , indole claim 10 , indoline claim 10 , benzofuran claim 10 , benzothiophene claim 10 , or quinolone.2037-. (canceled) This application claims priority of U.S. Provisional Application Nos. 62/192,789, filed Jul. 15, 2015; 62/192,462, filed Jul. 14, 2015; 62/063,246, filed Oct. 13, 2014; and 62/062,508, filed Oct. 10, 2014, the contents of each of which are hereby incorporated by reference.Throughout this application various publications are referenced. The disclosures of these documents in their entireties are hereby incorporated by reference into this application in order to more fully describe the state of the art to which this invention pertains.Fluorine atoms are often introduced into organic molecules to enhance their pharmacological properties such as solubility, metabolic and oxidative stability, lipophilicity, and bioavailability. Among the fluorine containing functional groups, ...

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Номер записи: 90
21-01-2021 дата публикации

ORGANIC REACTIONS CARRIED OUT IN AQUEOUS SOLUTION IN THE PRESENCE OF A HYDROXYALKYL(ALKYL)CELLULOSE OR AN ALKYLCELLULOSE

Номер: US20210017100A1
Автор: Braje Wilfried, BRITZE Katarina, Dietrich Justin D., JOLIT Anais, KASCHEL Johannes, KLEE Johanna, Lindner Tanja
Принадлежит:

The present invention relates to a method of carrying out an organic reaction in aqueous solution in the presence of a hydroxyalkyl(alkyl)cellulose or an alkylcellulose. 1. A method of carrying out an organic reaction in a solvent containing at least 90% by weight , based on the total weight of the solvent , of water , which method comprises reacting the reagents in said solvent in the presence of a cellulose derivative as a surfactant which is selected from the group consisting of cellulose modified with one or more alkylene oxides or other hydroxyalkyl precursors , and alkylcellulose;where the organic reaction is not a polymerization or oligomerization reaction of olefinically unsaturated compounds; and [ a transition metal catalyzed C—C coupling reaction:', 'a transition metal catalyzed reaction involving C—N bond formation which is an Au-catalyzed cyclodehydratization of α,β-amino alcohols containing a C—C triple bond:', 'a transition metal catalyzed reaction involving C—O bond formation:', 'a transition metal catalyzed reaction involving C—S bond formation:', 'a transition metal catalyzed reaction involving C—B bond formation: or', 'a transition metal catalyzed reaction involving C-halogen bond formation; or, 'a transition metal catalyzed reaction in which a transition metal catalyst is used; where the transition metal catalyzed reaction is'}, 'a C—C coupling reaction not requiring transition metal catalysis which is selected from the group consisting of reactions of carbonyl or nitrile compounds and pericyclic reactions;, 'where the organic reaction is'}a nucleophilic substitution reaction;a reduction or an oxidation reaction; oran ester formation reaction or an ester hydrolysis reaction.2. The method as claimed in claim 1 , where the cellulose derivative has a viscosity of from 1 to 150000 mPa·s claim 1 , determined as a 2% by weight aqueous solution claim 1 , relative to the weight of water.3. The method as claimed in claim 1 , where in the cellulose ...

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Номер записи: 91
16-01-2020 дата публикации

NOVEL COMPOUNDS AND COMPOSITIONS FOR INHIBITION OF FASN

Номер: US20200017458A1
Автор: Bair Kenneth W., JR. David R., Lancia, LI Hongbin, Loch James, Lu Wei, Martin Matthew W., Millan David S., Schiller Shawn E.R., TEBBE Mark J.
Принадлежит:

The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below: 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris a C-Chydroxyl-alkyl either unsubstituted or substituted with —CHor CHF.3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris a 5-membered cycloalkyl either unsubstituted or substituted with substituents selected from the group consisting of —R claim 1 , —OR claim 1 , —NHRand —NRR1.4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris a 3 membered cycloalkyl wherein said 3 membered cycloalkyl is either unsubstituted or optionally substituted with substituents selected from the group consisting of deuterium claim 1 , —R claim 1 , —OR claim 1 , —NHR claim 1 , and —NRR.5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris a 4 membered cycloalkyl wherein said 3 membered cycloalkyl is either unsubstituted or optionally substituted with substituents selected from the group consisting of deuterium claim 1 , —R claim 1 , —OR claim 1 , —NHR claim 1 , and —NRR.6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris a substituted or unsubstituted 9-membered 6 claim 1 ,5 bicyclic heteroaryl and said heteroaryl has 1 claim 1 , 2 claim 1 , 3 claim 1 , or 4 heteroatoms and said heteroatoms are independently O claim 1 , S claim 1 , or N.7. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein Ris a substituted or unsubstituted 9-membered 6 claim 2 ,5 bicyclic heteroaryl and said heteroaryl has 1 claim 2 , 2 claim 2 , 3 claim 2 , or 4 heteroatoms and said heteroatoms are independently O claim 2 , S claim 2 , or N.8. The compound of claim 3 , or a pharmaceutically acceptable salt thereof claim 3 , ...

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Номер записи: 92
17-04-2014 дата публикации

Dyes and Labeled Molecules

Номер: US20140106349A1
Автор: Fei Mao, Wai-Yee Leung, XING Xin
Принадлежит: AlleLogic Biosciences Corp, Biotium Inc

Dimeric and trimeric nucleic acid dyes, and associated systems and methods are provided. Such a dye may form a hairpin-like structure that enables it to stain nucleic acids via a release-on-demand mechanism, for example. Such a dye may have low background fluorescence in the absence of nucleic acids and high fluorescence in the presence of nucleic acids, upon binding therewith, for example. A dye provided herein may be useful in a variety of applications, such as in DNA quantitation in real-time PCR, for example.

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Номер записи: 93
28-01-2016 дата публикации

OCTAHYDROCYCLOPENTAPYRROLES, THEIR PREPARATION AND USE

Номер: US20160024007A1
Автор: Chen Ping, Cioffi Christopher, Conlon Michael, DOBRI Nicoleta, Freeman Emily, Johnson Graham, Petrukhin Konstantin, Zhu Lei
Принадлежит: The Trustees of Columbia University in the City of New York

The present invention provides Octahydrocyclopentapyrrole compounds having the structure: (structurally represented) wherein psi is absent or present, and when present is a bond; R1, R2, R3, R4, and R5 are each independently H, halogen, CF, or C1-C4 alkyl; R6 is absent or present, and when present is H, OH, or halogen; A is absent or present, and when present is C(O) or C(O)NH; B is substituted or unsubstituted monocycle, bicycle, heteromonocycle, heterobicycle, benzyl, CO2H or (C1-C4 alkyl)-CO2H, wherein when B is CO2H, then A is present and is C(O); and when psi is present, then R6 is absent and when psi is absent, then R6 is present, or a pharmaceutically acceptable salt thereof, for treatment of diseases characterized by excessive lipofuscin accumulation in the retina. 1114.-. (canceled)117. The compound of claim 116 , wherein B is a substituted or unsubstituted heterobicycle.126. The compound of claim 116 , wherein B is a substituted or unsubstituted monocycle or heteromonocycle.133. A pharmaceutical composition comprising the compound of and a pharmaceutically acceptable carrier.134. A method for treating a disease characterized by excessive lipofuscin accumulation in the retina in a mammal afflicted therewith comprising administering to the mammal an effective amount of the compound of . This application claims priority of U.S. Provisional Application No. 61/785,288, filed Mar. 14, 2013, the contents of which are hereby incorporated by reference.Throughout this application, certain publications are referenced in parentheses. Full citations for these publications may be found immediately preceding the claims. The disclosures of these publications in their entireties are hereby incorporated by reference into this application in order to describe more fully the state of the art to which this invention relates.The invention was made with government support under Grant numbers NS067594 and NS074476 awarded by the National Institutes of Health. The government has ...

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Номер записи: 94
24-01-2019 дата публикации

PLATELET STORAGE METHODS AND COMPOSITIONS FOR SAME

Номер: US20190021307A1
Автор: Cancelas Jose, Zheng Yi
Принадлежит:

Disclosed are compositions and methods for slowing, preventing, or reversing platelet damage, particularly as may occur during blood banking or during refrigeration of platelets. The composition may include one or more of a RAC inhibitor, a CDC42 inhibitor, a RHOA inhibitor, or a combination thereof. The compositions may further include a pharmaceutically acceptable carrier. 132.-. (canceled)34. The method of claim 33 , wherein said RHOA inhibitor is present at a concentration of from about 1 μM to about 500 μM.35. The method of claim 33 , wherein the platelets are stored in the presence of the RHOA inhibitor at a temperature of from about 1° C. to about 25° C.36. The method of claim 33 , wherein the platelets are stored in the presence of the RHOA inhibitor for a period of time of from about 3 to 20 days.37. The method of claim 33 , wherein the platelets are further contacted with a physiologically acceptable carrier.38. The method of claim 37 , wherein said physiologically acceptable carrier is selected from saline claim 37 , phosphate buffered saline claim 37 , Tris buffered saline claim 37 , Hank's buffered saline claim 37 , water claim 37 , or a combination thereof.39. The method according to claim 37 , wherein said physiologically acceptable carrier comprises an electrolyte solution.41. The method of claim 40 , wherein said RHOA inhibitor is present at a concentration of from about 1 μM to about 500 μM.42. The method of claim 40 , wherein the platelets are stored in the presence of the RHOA inhibitor at a temperature of from about 1° C. to about 25° C.43. The method of claim 40 , wherein the platelets are stored in the presence of the RHOA inhibitor for a period of time of from about 3 to 20 days.44. The method of claim 40 , wherein wherein claim 40 , prior to said infusing claim 40 , the platelets have further been contacted with a physiologically acceptable carrier.45. The method of claim 44 , wherein said physiologically acceptable carrier is selected from ...

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Номер записи: 95
22-01-2015 дата публикации

ANTIVIRAL DRUGS FOR TREATMENT OF ARENAVIRUS INFECTION

Номер: US20150023916A1
Автор: Amberg Sean M., Burgeson James R., Dai Dongcheng, Hruby Dennis E.
Принадлежит: SIGA TECHNOLOGIES INC.

Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever. 2. The compound of claim 1 , wherein each of E and J is N.3. The compound of claim 1 , wherein each of G claim 1 , M claim 1 , Q and L is C—R.4. The compound of claim 1 , wherein K is C.5. The compound of claim 1 , wherein D-A is RC═CRand each of Rand Rare H and the double bond in RC═CRhas a cis configuration.6. The compound of claim 1 , wherein D-A is O—CRRand each of Rand Rare H.7. The compound of selected from the group consisting of: 5-[(Z)-2-(4-tert-butylphenyl)vinyl]-1-(4-isopropoxyphenyl)-benzimidazole; 1-(4-ethoxyphenyl)-5-[(4-ethylphenyl)-methoxy]benzimidazole; and 2-[4-[(Z)-2-[1-(4-isopropoxyphenyl)benzimidazol-5-yl]vinyl]phenyl]-propan-2-ol.10. The composition of claim 9 , wherein each of E and J is N.11. The composition of claim 9 , wherein each of G claim 9 , M claim 9 , Q and L is C—R.12. The composition of claim 9 , wherein K is C.13. The composition of claim 9 , wherein D-A is RC═CRand each of Rand Rare H and the double bond in RC═CRhas a cis configuration.14. The composition of claim 9 , wherein D-A is O—CRRand each of Rand Rare H.15. The composition of claim 9 , wherein the compound of Formula I is selected from the group consisting of: 5-[(Z)-2-(4-tert-butylphenyl)vinyl]-1-(4-isopropoxyphenyl)-benzimidazole; 1-(4-ethoxyphenyl)-5-[(4-ethylphenyl)-methoxy]benzimidazole; and 2-[4-[(Z)-2-[1-(4-isopropoxyphenyl)benzimidazol-5-yl]vinyl]phenyl]-propan-2-ol.18. The method of claim 17 , wherein each of E and J is N.19. The method of claim 17 , ...

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Номер записи: 96
26-01-2017 дата публикации

Substituted 3-phenylpropylamine derivatives for the treatment of ophthalmic diseases and disorders

Номер: US20170022180A1
Автор: Feng Hong, Mark W. Orme, Ryo Kubota, Vladimir A. Kuksa
Принадлежит: Acucela Inc

The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted 3-phenylpropylamine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

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Номер записи: 97
28-01-2016 дата публикации

MULTI-TIERED, HIGH THROUGH-PUT SCREEN FOR COMPOUNDS EFFECTIVE AGAINST BACTERIAL BIOFILM COMPOUNDS EFFECTIVE FOR INHIBITING AND ERADICATING BACTERIAL BIOFILM

Номер: US20160024551A1
Автор: Hassett Daniel J., Lamkin Thomas J., Panmanee Warunya, Shea Chioe J.A., Taylor Deborah E.
Принадлежит:

A high through-put screening method for identifying agents effective for inhibiting biofilm formation and/or killing established biofilm are disclosed. The method includes three tiers, and each tier includes three specific biological process assays. The tier levels are a primary screen, a confirmation screen, and a dose-response screen, and the biological process assays include as says for total bacterial growth, bacterial metabolic activity, and biofilm formation. 1. A high through-put screening method for identifying agents from a library of compounds , said agents effective for inhibiting biofilm formation and/or killing established biofilm , the method comprising: (A) primary screen,', '(B) confirmation screen,', '(C) dose-response screen;, 'conducting three tiers of three assays; the tiers comprising'} (a) total bacterial growth assay', '(b) bacterial metabolic activity assay', '(c) biofilm formation assay,, 'the assays comprising'}wherein the library of compounds is subject to tier A and only compounds meeting a primary parameter advance to tier B, and only tier B compounds meeting a confirmation parameter advance to tier C, and only tier C compounds meeting a dose-response parameter are identified as putative agents effective for inhibiting and/or eradicating a biofilm, further wherein the assays are conducted for each compound subject to the respective tier.2. The high through-put screening method according to claim 1 , wherein the total bacterial growth assay according to (a) comprises optical density measurement claim 1 , the bacterial metabolic activity assay according to (b) comprises resazurin indicator claim 1 , and the biofilm formation assay according to (c) comprises crystal violet staining claim 1 , each assay being conducted in the presence of a concentration of a compound subject to a tier.3. The high through-put screening method according to claim 2 , wherein the primary parameter is one of ≧80% inhibition in (a) claim 2 , ≧80% inhibition in (b) ...

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Номер записи: 98
17-04-2014 дата публикации

3-aminocarbazole compound, pharmaceutical composition containing it and preparation method therefor

Номер: US20140107174A1
Автор: Angelo Guglielmotti, Barbara Garofalo, Caterina Maugeri, Giorgina Mangano, Guido Furlotti, Isabella Coletta, Maria Alessandra Alisi, Nicola Cazzolla, Patrizia Dragone
Принадлежит: Aziende Chimiche Riunite Angelini Francesco ACRAF SpA

The present invention relates to novel benzoyl derivatives of 3-aminocarbazole, to a pharmaceutical composition containing them, to a method for preparing them and to the use of such compounds for the production of a drug that is useful in the treatment or prevention of disturbances associated with the production of prostaglandin E 2 (PGE 2 ), for instance inflammatory processes, pain, fever, tumours, Alzheimer's disease and atherosclerosis.

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Номер записи: 99
17-04-2014 дата публикации

Triple reuptake inhibitors and methods of their use

Номер: US20140107175A1
Автор: Fengjiang Wang, Liming Shao, Michael C. Hewitt, Scott C. Malcolm
Принадлежит: SUNOVION PHARMACEUTICALS INC

Provided herein are bicyclic compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders. Compounds provided herein inhibit re-uptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine (e.g., from the synaptic cleft) and modulate one or more monoamine transporter. Pharmaceutical formulations containing the compounds are also provided.

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Номер записи: 100