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1. 发明申请

US20170197973A1 IMMUNOREGULATORY AGENTS 审中-公开
公开(公告)号：US20170197973A1
公开(公告)日：2017-07-13
申请号：US15469707
申请日：2017-03-27
申请人： Flexus Biosciences, Inc.
发明人： Hilary Plake Beck , Juan Carlos Jaen , Maksim Osipov , Jay Patrick Powers , Maureen Kay Reilly , Hunter Paul Shunatona , James Ross Walker , Mikhail Zibinsky , James Aaron Balog , David K. Williams , Jay A. Markwalder , Emily Charlotte Cherney , Weifang Shan , Audris Huang
IPC分类号： C07D487/04 , C07D215/14 , A61K31/416 , C07D231/56 , A61K45/06 , C07D215/233 , C07D471/04 , A61K31/437 , A61K31/517 , C07D239/74 , A61K31/4375 , A61K31/4709 , C07D405/12 , C07D401/12 , C07D417/12 , A61K31/496 , C07D401/14 , A61K31/519 , A61K31/506 , A61K31/47
CPC分类号： C07D215/12 , A61K31/416 , A61K31/437 , A61K31/4375 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/517 , A61K31/519 , A61K39/39558 , A61K45/06 , A61K2300/00 , A61P35/02 , C07D215/06 , C07D215/14 , C07D215/233 , C07D217/04 , C07D217/12 , C07D217/24 , C07D231/56 , C07D239/74 , C07D401/12 , C07D401/14 , C07D405/08 , C07D405/12 , C07D417/08 , C07D417/12 , C07D471/04 , C07D487/04
摘要： Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.

2. 发明授权

US09636339B2 Phenyl-dihydropyridine derivatives as aldosterone synthase inhibitors 有权
公开(公告)号：US09636339B2
公开(公告)日：2017-05-02
申请号：US15098738
申请日：2016-04-14
申请人： Hoffmann-La Roche Inc.
发明人： Johannes Aebi , Kurt Amrein , Robert Britton , Benoit Hornsperger , Bernd Kuhn , Hans P. Maerki , Rainer E. Martin , Alexander V. Mayweg , Xuefei Tan
IPC分类号： A61K31/472 , C07D217/02 , C07D217/18 , C07D401/06 , C07D401/12 , C07D413/12
CPC分类号： A61K31/472 , C07D217/02 , C07D217/12 , C07D217/18 , C07D401/06 , C07D401/12 , C07D413/12
摘要： The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A1 and n are as described herein, compositions including the compounds and methods of using the compounds.

3. 发明授权

US09604930B2 Tetrahydro- and dihydro-isoquinoline PRMT5 inhibitors and uses thereof 有权
公开(公告)号：US09604930B2
公开(公告)日：2017-03-28
申请号：US14654253
申请日：2013-12-20
申请人： Epizyme, Inc.
发明人： Kenneth W. Duncan , Richard Chesworth , Paula Ann Boriack-Sjodin , Michael John Munchhof , Lei Jin
IPC分类号： A61K31/00 , C07D217/04 , C07D401/14 , C07D217/12 , C07D401/12 , C07D405/12 , C07D405/14 , C07D413/12
CPC分类号： A61K31/506 , C07D217/04 , C07D217/12 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D413/12 , C12N9/1007
摘要： Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5 mediated disorders are also described.

4. 发明申请

US20150126517A1 ARYL, HETEROARYL, AND HETEROCYCLE SUBSTITUTED TETRAHYDROISOQUINOLINES AND USE THEREOF 有权
标题翻译： ARYL，HETEROARYL和HETEROCYCLE取代的四氢喹啉和其用途
公开(公告)号：US20150126517A1
公开(公告)日：2015-05-07
申请号：US14593750
申请日：2015-01-09
申请人： Albany Molecular Research, Inc.
发明人： Shuang Liu , Bruce F. Molino , Kassoum Nacro
IPC分类号： C07D217/14 , C07D413/04 , C07D471/04 , C07D401/04
CPC分类号： C07D401/04 , C07D217/02 , C07D217/12 , C07D217/14 , C07D413/04 , C07D471/04
摘要： Novel aryl, heteroaryl, and non-aromatic heterocyle substituted tetrahydroisoquinolines are described in the present invention. These compounds are used in the treatment of various neurological and physiological disorders. Methods of making these compounds are also described in the present invention.
摘要翻译：本发明描述了新的芳基，杂芳基和非芳族杂环取代的四氢异喹啉。这些化合物用于治疗各种神经和生理疾病。制备这些化合物的方法也在本发明中描述。

5. 发明申请

US20140243338A1 PHENYLPYRAZOLE DERIVATIVES AS POTENT ROCK1 AND ROCK2 INHIBITORS 有权
标题翻译：作为POTENT ROCK1和ROCK2抑制剂的苯基吡唑衍生物
公开(公告)号：US20140243338A1
公开(公告)日：2014-08-28
申请号：US14192955
申请日：2014-02-28
申请人： Bristol-Myers Squibb Company
发明人： Mimi L. Quan , Zilun Hu , Cailan Wang
IPC分类号： C07D231/12 , C07D401/12 , C07D417/12
CPC分类号： C07D231/12 , C07D217/12 , C07D231/56 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D513/04
摘要： The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
摘要翻译：本发明提供式（I）的化合物或其立体异构体，互变异构体或其药学上可接受的盐，其中所有变量如本文所定义。这些化合物是选择性的ROCK抑制剂。本发明还涉及包含这些化合物的药物组合物和使用其治疗心血管，平滑肌，肿瘤学，神经病理学，自身免疫性，纤维化和/或炎症性疾病的方法。

6. 发明授权

US08088772B2 Sulfonamides and their use as a medicament 失效
标题翻译：磺酰胺及其作为药物的用途
公开(公告)号：US08088772B2
公开(公告)日：2012-01-03
申请号：US12517691
申请日：2007-12-11
申请人： Gabriel Garcia , Pierre Daram , Barbara Froesch , Frank Jaschinski , Guy Lemaillet , Cornelia Marty-Ernst , Elena Marzi , Leonardo Scapozza
发明人： Gabriel Garcia , Pierre Daram , Barbara Froesch , Frank Jaschinski , Guy Lemaillet , Cornelia Marty-Ernst , Elena Marzi , Leonardo Scapozza
IPC分类号： A61K31/5375 , A61K31/44 , A61K31/415 , A61K31/18 , C07D295/00 , C07D231/10 , C07D213/00 , C07D309/00
CPC分类号： C07C311/38 , C07C311/21 , C07D207/335 , C07D209/40 , C07D213/24 , C07D213/53 , C07D215/12 , C07D217/12 , C07D231/12 , C07D233/64 , C07D271/12 , C07D295/096 , C07D295/135 , C07D295/155 , C07D333/58
摘要： The present invention relates to the use of a sulfonamide compound of formula (I): wherein R1 is selected from the group consisting of H, CN, halogen, trifluoromethyl, methyl, ethyl, hydroxy, methoxy, ethoxy, morpholino, R2 is selected from H, phenyl, substituted phenyl, CN, —SO2R, wherein R is phenyl or morpholino, —NC(O)Me, —NC(O)Et, —CH2C(O)OMe, CH2C(O)OEt, R3 is selected from the group consisting of H, NO2, NH2, halogen, —COOMe, —COOEt, RC(O)N—, morpholino, R4 is selected from the group consisting of H, a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, methoxy, ethoxy, propoxy, butoxy, a substituted or unsubstituted phenyl, alkinyl, Me2SO2—, COOR, wherein R is a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, -MeOC(O)—, a substituted or unsubstituted five or sixmembered aromatic or non-aromatic heterocyclic system with one, two or three heteroatoms, a hetaryl system, a condensed benzoheterocyclic system, X is a linker comprising 2 or 3 atoms, selected from the group consisting of —NH—NH—, —NH—NH—CH2—, ethinyl, —NH—C(O)—CH2—, —NH—NH—SO2—, —C(O)—NH—CH2—, —NH—N═CH—, —NH—N═C(Me)-, a —NH—N═CH— motif being part of a heterocyclic system, preferably a substituted or unsubstituted pyrazole or pyridazine system, and pharmaceutically active salts thereof. Further, the invention relates to the use of these compounds as a medicament, especially for the treatment of cancer.
摘要翻译：本发明涉及式（I）的磺酰胺化合物的用途：其中R 1选自H，CN，卤素，三氟甲基，甲基，乙基，羟基，甲氧基，乙氧基，吗啉代，R2选自其中R为苯基或吗啉代，-NC（O）Me，-NC（O）Et，-CH2C（O）OMe，CH2C（O）OEt，R3选自由H，NO 2，NH 2，卤素，-COOMe，-COOEt，RC（O）N-，吗啉代，R 4选自H，支链或非支链的甲基，乙基，丙基，丁基，戊基乙氧基，丙氧基，丁氧基，取代或未取代的苯基，炔基，Me2SO2-，COOR，其中R是支链或非支链的甲基，乙基，丙基，丁基，戊基，-MeOC（O） - ，取代或未取代的具有一个，两个或三个杂原子的五或六元芳族或非芳族杂环体系，杂芳基系统，稠合苯并杂环系统，X是包含2或3个选自-NH-NH-，-NH-NH-CH 2 - ，乙炔基，-NH-C（O）-CH 2 - ， - NH-NH-SO 2 - ， - C（O）-NH -CH 2 - ， - NH-N = CH - ， - NH-N = C（Me） - ，作为杂环系统的一部分的-NH-N = CH-基序，优选取代或未取代的吡唑或哒嗪系统，其药学活性盐。此外，本发明涉及这些化合物作为药物，特别是用于治疗癌症的用途。

7. 发明申请

US20100292242A1 ARYL, HETEROARYL, AND HETEROCYCLE SUBSTITUTED TETRAHYDROISOQUINOLINES AND USE THEREOF 有权
标题翻译： ARYL，HETEROARYL和HETEROCYCLE取代的四氢喹啉和其用途
公开(公告)号：US20100292242A1
公开(公告)日：2010-11-18
申请号：US12777728
申请日：2010-05-11
申请人： Shuang Liu , Bruce F. Molino , Kassoum Nacro
发明人： Shuang Liu , Bruce F. Molino , Kassoum Nacro
IPC分类号： A61K31/472 , C07D401/10 , A61K31/501 , A61K31/497 , C07D217/14 , A61K31/4725 , C07D471/04 , A61P25/00 , A61P25/24 , A61P15/00
CPC分类号： C07D401/04 , C07D217/02 , C07D217/12 , C07D217/14 , C07D413/04 , C07D471/04
摘要： Novel aryl, heteroaryl, and non-aromatic heterocyle substituted tetrahydroisoquinolines are described in the present invention. These compounds are used in the treatment of various neurological and physiological disorders. Methods of making these compounds are also described in the present invention.
摘要翻译：本发明描述了新的芳基，杂芳基和非芳族杂环取代的四氢异喹啉。这些化合物用于治疗各种神经和生理疾病。制备这些化合物的方法也在本发明中描述。

8. 发明申请

US20090253906A1 ARYL- AND HETEROARYL-SUBSTITUTED TETRAHYDROISOQUINOLINES AND USE THEREOF TO BLOCK REUPTAKE OF NOREPINEPHRINE, DOPAMINE, AND SEROTONIN 有权
标题翻译： ARYL-和HETEROARYL取代的四氢喹啉和其用于阻断肾上腺素，多巴胺和丝氨酸蛋白酶的重复使用
公开(公告)号：US20090253906A1
公开(公告)日：2009-10-08
申请号：US12417598
申请日：2009-04-02
申请人： Bruce F. MOLINO , Shuang LIU , Peter R. GUZZO , James P. BECK
发明人： Bruce F. MOLINO , Shuang LIU , Peter R. GUZZO , James P. BECK
IPC分类号： C07D413/14 , C07D401/14 , C07D401/04 , C07D403/14 , C07D409/14 , C07D409/04 , C07D413/04 , C07D417/14 , C07D417/04
CPC分类号： C07D417/04 , A61K31/4709 , A61K31/4741 , A61K31/4743 , A61K31/502 , A61K31/517 , A61K31/53 , C07D217/00 , C07D217/04 , C07D217/08 , C07D217/12 , C07D217/14 , C07D217/16 , C07D217/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/04 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3 -a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle optionally substituted with substituents (1 to 4 in number) as defined in R14; with R1, R2, R3, R4, R5, R6, R7, R8, and R14 defined herein.
摘要翻译：本发明的化合物由式（I）中所示的化学结构表示：其中：指定为*的碳原子为R或S构型; 并且X是选自苯并呋喃基，苯并[b]噻吩基，苯并异噻唑基，苯并异恶唑基，吲唑基，吲哚基，异吲哚基，吲嗪基，苯并咪唑基，苯并恶唑基，苯并噻唑基，苯并三唑基，咪唑并[1,2-a ]吡啶基，吡唑并[1,5-a]吡啶基，[1,2,4]三唑并[4,3-a]吡啶基，噻吩并[2,3-b]吡啶基，噻吩并[3,2-b] 二氢苯并噻吩基，二氢苯并呋喃基，二氢苯并噻吩基，四氢萘基，喹啉基，异喹啉基，4H-喹啉基，9H-喹啉基，喹唑啉基，噌啉基，酞嗪基，喹喔啉基，苯并[1,2,3]三嗪基，苯并[1,2,4]三嗪基，2H-色烯基，4H-色烯基和稠合的双环碳环或稠合双环杂环，其任选被如所定义的取代基（数目为1至4）在R14; 本文定义的R1，R2，R3，R4，R5，R6，R7，R8和R14。

9. 发明申请

US20090105278A1 Selective inhibitors of human corticosteroid syntheses 审中-公开
标题翻译：人类皮质类固醇合成的选择性抑制剂
公开(公告)号：US20090105278A1
公开(公告)日：2009-04-23
申请号：US11658048
申请日：2005-07-21
申请人： Rolf Hartmann , Sarah Ulmschneider , Ursula Muller-Viera , Rita Bernhardt , Mattas Bureik
发明人： Rolf Hartmann , Sarah Ulmschneider , Ursula Muller-Viera , Rita Bernhardt , Mattas Bureik
IPC分类号： A61K31/505 , C07D213/06 , C07D213/26 , C07D213/30 , C07D215/12 , C07D217/02 , A61K31/472 , A61P3/10 , A61K31/47 , A61K31/426 , C07D239/26 , C07D277/22 , A61P9/00 , A61K31/44
CPC分类号： C07D213/04 , A61K31/122 , A61K31/4164 , A61K31/44 , A61K31/505 , C07D213/16 , C07D213/26 , C07D213/30 , C07D217/12 , C07D233/64 , C07D239/26
摘要： The invention relates to compounds for selectively inhibiting human corticosteroid syntheses CYP11B1 and CYP11B2, to the production thereof and to their use for treating hypercortisolism and diabetes mellitus or insufficiency of the heart and myocardial fibrosis.
摘要翻译：本发明涉及用于选择性抑制人类皮质类固醇合成CYP11B1和CYP11B2的化合物及其用于治疗高皮质醇血症和糖尿病或心脏和心肌纤维化不足的用途。

10. 发明申请

US20070054916A1 Aryl nitrogen-containing bicyclic compounds and methods of use 审中-公开
标题翻译：芳基含氮双环化合物及其使用方法
公开(公告)号：US20070054916A1
公开(公告)日：2007-03-08
申请号：US11240590
申请日：2005-09-30
申请人： Vinod Patel , Joseph Kim , Stephanie Geuns-Meyer , Stuart Chaffee , Victor Cee , Brian Hodous , Steven Bellon , Jean-Christophe Harmange , Philip Olivieri , Maya Thaman , Erin DiMauro , John Buchanan , David McGowan , Brian Albrecht , Holly Deak , Jean Bemis , Ryan White , Matthew Martin , Gregory Habgood , Paul Tempest , Craig Masse , William Buckner , Bradley Herberich , Russell Graceffa , Dawei Zhang , Shimin Xu , Kelvin Sham , Robert Rzasa , James Falsey , Partha Chakrabarti , Guo-Qiang Cao , Susan Tomlinson , Liping Pettus , Adrian Smith , Nick Paras , Gang Liu , Frenel DeMorin , Andrew Tasker , Anthony Reed
发明人： Vinod Patel , Joseph Kim , Stephanie Geuns-Meyer , Stuart Chaffee , Victor Cee , Brian Hodous , Steven Bellon , Jean-Christophe Harmange , Philip Olivieri , Maya Thaman , Erin DiMauro , John Buchanan , David McGowan , Brian Albrecht , Holly Deak , Jean Bemis , Ryan White , Matthew Martin , Gregory Habgood , Paul Tempest , Craig Masse , William Buckner , Bradley Herberich , Russell Graceffa , Dawei Zhang , Shimin Xu , Kelvin Sham , Robert Rzasa , James Falsey , Partha Chakrabarti , Guo-Qiang Cao , Susan Tomlinson , Liping Pettus , Adrian Smith , Nick Paras , Gang Liu , Frenel DeMorin , Andrew Tasker , Anthony Reed
IPC分类号： A61K31/525 , A61K31/519 , A61K31/517
CPC分类号： C07D215/38 , C07C205/37 , C07D215/12 , C07D217/12 , C07D217/22 , C07D217/26 , C07D239/26 , C07D239/84 , C07D239/94 , C07D239/95 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要： The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I wherein A1, A2, A3, B, R1, R2, R3 and R4 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.
摘要翻译：本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病，包括炎症，癌症和相关病症的化合物。化合物具有通式I，其中A 1，A 2，A 3，B，R 1， R 2，R 3和R 4在本文中定义。因此，本发明还包括含有本发明化合物的药物组合物，使用本发明化合物和组合物预防和治疗激酶介导的疾病的方法，以及可用于制备本发明化合物的中间体和方法。

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