公开(公告)号：US10080741B2

公开(公告)日：2018-09-25

申请号：US15497268

申请日：2017-04-26

Applicant: Enanta Pharmaceuticals, Inc.

Inventor： Yat Sun Or ,  Brett Granger ,  Ruichao Shen ,  Xuechao Xing ,  Bin Wang ,  Jun Ma ,  Jing He ,  Jiang Long ,  Yong He ,  Guoqiang Wang

IPC: C07D261/08 ,  C07D413/12 ,  A61K31/42 ,  C07D261/06 ,  C07D413/04

CPC classification number: A61K31/42 ,  C07D261/06 ,  C07D261/08 ,  C07D413/04 ,  C07D413/12

Abstract: The present invention provides compounds of Formula I: pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated as FXR modulators. Specifically, the present invention relates to isoxazole derivatives useful as agonists for FXR, and methods for their preparation and use.

公开(公告)号：US20160052935A1

公开(公告)日：2016-02-25

申请号：US14936949

申请日：2015-11-10

Applicant: Indiana University Research and Technology Corporation ,  The Brigham Women's Hospital, Inc. ,  The University of Massachusetts

Inventor： Elliot Androphy ,  Gregory D. Cuny ,  Jonathan Cherry ,  Marcie A. Glicksman

IPC: C07D493/04 ,  C07D413/12 ,  C07D261/14 ,  C07D231/14 ,  C07D285/135 ,  C07D277/46 ,  C07D263/48 ,  C07D233/88 ,  C07D239/47 ,  C07D417/12 ,  C07D215/44 ,  C07D471/04 ,  C07D417/04 ,  C07D215/227 ,  C07D487/04 ,  C07D221/10 ,  C07D405/04 ,  C07D401/04 ,  C07D239/82 ,  C07D267/14 ,  C07D261/18

CPC classification number: C07D493/04 ,  C07C311/37 ,  C07C2601/08 ,  C07C2603/20 ,  C07D213/75 ,  C07D215/227 ,  C07D215/44 ,  C07D221/10 ,  C07D231/14 ,  C07D233/88 ,  C07D239/47 ,  C07D239/82 ,  C07D261/06 ,  C07D261/14 ,  C07D261/18 ,  C07D263/48 ,  C07D267/14 ,  C07D277/46 ,  C07D285/135 ,  C07D401/04 ,  C07D405/04 ,  C07D405/12 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07K14/47

Abstract: Disclosed herein are compositions and methods for treatment of spinal muscular atrophy (SMA). In certain embodiments, compounds are provided that increase full-length survival of motor neuron (SMN) protein production by an SMN2 gene.

Abstract translation: 本文公开了用于治疗脊髓性肌萎缩（SMA）的组合物和方法。 在某些实施方案中，提供了通过SMN2基因增加运动神经元（SMN）蛋白质产生的全长存活的化合物。

公开(公告)号：US20100280073A1

公开(公告)日：2010-11-04

申请号：US12664137

申请日：2008-06-11

Applicant: Jay P. Powers ,  Daqing Sun ,  Xuelei Yan ,  Lisa Julian ,  Felix Gonzalez Lopez De Turiso

Inventor： Jay P. Powers ,  Daqing Sun ,  Xuelei Yan ,  Lisa Julian ,  Felix Gonzalez Lopez De Turiso

IPC: A61K31/454 ,  C07D263/32 ,  A61K31/421 ,  A61P3/10 ,  A61P3/04 ,  A61P15/00 ,  A61P3/06 ,  A61P9/12 ,  A61P9/10 ,  A61P25/28 ,  A61P25/24 ,  A61P17/06 ,  A61P27/06 ,  A61P19/10 ,  A61P31/12 ,  A61P37/00 ,  C12N5/02 ,  C07D413/04 ,  C07D261/08 ,  A61K31/42 ,  C07D277/24 ,  A61K31/426

CPC classification number: C07D231/10 ,  C07D261/06 ,  C07D263/30 ,  C07D277/20

Abstract: The present invention provides tricyclic compounds according to formula (I): (I) where R1, R2, R3, W, X, Y, Z, m, n, and p are as defined in the description; as well as pharmaceutical compositions comprising the same, methods of use of the compounds and compositions of the invention for the treatment of conditions associated with hydroxysteroid dehydrogenases (e.g., 11-HSD1), and the use of the compounds of the invention in the preparation of medicaments for the treatment of hydroxysteroid dehydrogenase-associated conditions.

Abstract translation: 本发明提供式（I）的三环化合物：（I）其中R 1，R 2，R 3，W，X，Y，Z，m，n和p如说明书中所定义; 以及包含其的药物组合物，使用本发明化合物和组合物的方法用于治疗与羟类固醇脱氢酶（例如，11-HSD1）相关的病症的用途，以及本发明化合物在制备 用于治疗羟基类固醇脱氢酶相关病症的药物。

公开(公告)号：US09150563B2

公开(公告)日：2015-10-06

申请号：US14177000

申请日：2014-02-10

Applicant: Daiichi Sankyo Company, Limited

Inventor： Keiko Suzuki ,  Takahiro Yamaguchi ,  Akihiro Tamura ,  Tomohiro Nishizawa ,  Mitsuhiro Yamaguchi

IPC: A61K31/427 ,  A61K31/422 ,  C07D277/20 ,  C07D261/06 ,  C07D417/12 ,  A61K31/40 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4245 ,  A61K31/4439 ,  C07D207/34 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14

CPC classification number: C07D417/12 ,  A61K31/40 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/4439 ,  C07D207/34 ,  C07D261/06 ,  C07D277/20 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14

Abstract: The present invention provides a compound having excellent regulating action on blood lipid level.The present invention provides a compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, etc., wherein A represents a 5-membered nitrogen-containing aromatic heterocyclyl group; R1 represents COOH or the like; each R2 represents an alkyl or the like; each R3 represents an optionally substituted phenyl, an optionally substituted phenylalkyl, or the like; m represents 0, 1, 2, or 3; n represents 0 or 1; each of R4, R5, R6, and R7 represents H, an alkyl, or the like; and B represents an optionally substituted naphthyl, an optionally substituted aromatic heterocyclyl, or a group represented by the following formula (II) wherein each of B1 and B2 represents an optionally substituted phenyl or an optionally substituted aromatic heterocyclyl.

Abstract translation: 本发明提供了对血脂水平具有优异调节作用的化合物。 本发明提供由以下通式（I）表示的化合物或其药学上可接受的盐等，其中A表示5元含氮芳族杂环基; R1表示COOH等; 每个R 2表示烷基等; 每个R 3表示任选取代的苯基，任选取代的苯基烷基等; m表示0,1,2或3; n表示0或1; R 4，R 5，R 6和R 7各自表示H，烷基等; 和B表示任选取代的萘基，任选取代的芳族杂环基或由下式（II）表示的基团，其中B1和B2各自表示任选取代的苯基或任选取代的芳族杂环基。

公开(公告)号：US20140193906A1

公开(公告)日：2014-07-10

申请号：US13941099

申请日：2013-07-12

Applicant: Indiana University Research and Technology Corporation ,  The University of Massachusetts ,  The Brigham Women's Hospital, Inc.

Inventor： Elliot Androphy ,  Gregory D. Cuny ,  Jonathan Cherry ,  Marcie A. Glicksman

IPC: C07K14/47

CPC classification number: C07D493/04 ,  C07C311/37 ,  C07C2601/08 ,  C07C2603/20 ,  C07D213/75 ,  C07D215/227 ,  C07D215/44 ,  C07D221/10 ,  C07D231/14 ,  C07D233/88 ,  C07D239/47 ,  C07D239/82 ,  C07D261/06 ,  C07D261/14 ,  C07D261/18 ,  C07D263/48 ,  C07D267/14 ,  C07D277/46 ,  C07D285/135 ,  C07D401/04 ,  C07D405/04 ,  C07D405/12 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07K14/47

Abstract: Disclosed herein are compositions and methods for treatment of spinal muscular atrophy (SMA). In certain embodiments, compounds are provided that increase full-length survival of motor neuron (SMN) protein production by an SMN2 gene.

Abstract translation: 本文公开了用于治疗脊髓性肌萎缩（SMA）的组合物和方法。 在某些实施方案中，提供了通过SMN2基因增加运动神经元（SMN）蛋白质产生的全长存活的化合物。

公开(公告)号：US20080269280A1

公开(公告)日：2008-10-30

申请号：US12048814

申请日：2008-03-14

Applicant: Penglie Zhang ,  Andrew M.K. Pennell ,  Lianfa Li ,  Edward J. Sullivan

Inventor： Penglie Zhang ,  Andrew M.K. Pennell ,  Lianfa Li ,  Edward J. Sullivan

IPC: A61K31/437 ,  C07D233/02 ,  C07D261/06 ,  C07D401/04 ,  A61K31/4166 ,  A61K31/422 ,  A61P37/02

CPC classification number: C07D233/32 ,  C07D261/06 ,  C07D401/04 ,  C07D413/06 ,  C07D413/14 ,  C07D471/04

Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Abstract translation: 提供了作为CCR1受体的有效拮抗剂并具有体内抗炎活性的化合物。 化合物通常是单环和双环化合物，并且可用于药物组合物，用于治疗CCR1介导的疾病的方法，以及用于鉴定竞争性CCR1拮抗剂的测定中的对照。

公开(公告)号：US20180036294A1

公开(公告)日：2018-02-08

申请号：US15553593

申请日：2016-02-26

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Shaomeng WANG ,  Yujun ZHAO ,  Bing ZHOU ,  Angelo AGUILAR

IPC: A61K31/437 ,  C07D487/14 ,  C07D231/38 ,  C07D471/04 ,  C07D261/06 ,  A61K31/519 ,  C07D487/04

CPC classification number: A61K31/437 ,  A61K31/519 ,  C07D231/38 ,  C07D261/06 ,  C07D471/04 ,  C07D487/04 ,  C07D487/14

Abstract: The present disclosure provides substituted 9H-pyrimido [4,5-b] indoles and 5H-pyrido [4,3-b] indoles and related analogs represented by Formula I and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, W, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains such as cancer. The present disclosure is also directed to the use of compound of Formula I as synthetic intermediates.

公开(公告)号：US09789086B1

公开(公告)日：2017-10-17

申请号：US15510755

申请日：2015-09-17

Applicant: Industry-University Cooperation Foundation Hanyang University ERICA Campus

Inventor： Jung-Mi Hah ,  Kyung Jin Jung

IPC: A61K31/415 ,  C07D261/06 ,  C07C233/07 ,  C07C233/10

CPC classification number: A61K31/415 ,  C07C233/07 ,  C07C233/10 ,  C07D261/02 ,  C07D261/06 ,  C07D261/18 ,  C07D413/12

Abstract: The present invention relates to N-(5-arylamido-2-methylphenyl)-5-methylisoquoxazole-4-carboxamide derivative, or a pharmaceutically acceptable salt thereof and a pharmaceutical composition comprising same. The compound according to the present invention exhibits an FMS kinase inhibitory activity and thus can be used as pharmaceutical composition for preventing and treating diseases associated therewith.

公开(公告)号：US08765788B2

公开(公告)日：2014-07-01

申请号：US12664137

申请日：2008-06-11

Applicant: Jay P. Powers ,  Daqing Sun ,  Xuelei Yan ,  Lisa Julian ,  Felix Gonzalez Lopez De Turiso

Inventor： Jay P. Powers ,  Daqing Sun ,  Xuelei Yan ,  Lisa Julian ,  Felix Gonzalez Lopez De Turiso

IPC: A61K31/445 ,  A61K31/425 ,  A61K31/42

CPC classification number: C07D231/10 ,  C07D261/06 ,  C07D263/30 ,  C07D277/20

Abstract: The present invention provides tricyclic compounds according to formula (I): (I) where R1, R2, R3, W, X, Y, Z, m, n, and p are as defined in the description; as well as pharmaceutical compositions comprising the same, methods of use of the compounds and compositions of the invention for the treatment of conditions associated with hydroxysteroid dehydrogenases (e.g., 11-HSD1), and the use of the compounds of the invention in the preparation of medicaments for the treatment of hydroxysteroid dehydrogenase-associated conditions.

Abstract translation: 本发明提供式（I）的三环化合物：（I）其中R 1，R 2，R 3，W，X，Y，Z，m，n和p如说明书中所定义; 以及包含其的药物组合物，使用本发明化合物和组合物的方法用于治疗与羟类固醇脱氢酶（例如，11-HSD1）相关的病症的用途，以及本发明化合物在制备 用于治疗羟基类固醇脱氢酶相关病症的药物。

公开(公告)号：US20240174614A1

公开(公告)日：2024-05-30

申请号：US18341613

申请日：2023-06-26

Applicant: Aldeyra Therapeutics, Inc.

Inventor： Thomas A. Jordan ,  John E. Dowling ,  John Clifford Chabala

IPC: C07D215/38 ,  A61K31/41 ,  A61K31/423 ,  A61K31/426 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/47 ,  A61K31/4706 ,  C07C215/68 ,  C07C229/56 ,  C07C229/60 ,  C07D261/06 ,  C07D275/00 ,  C07D277/40 ,  C07D277/56 ,  C07D333/04

CPC classification number: C07D215/38 ,  A61K31/41 ,  A61K31/423 ,  A61K31/426 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/47 ,  A61K31/4706 ,  C07C215/68 ,  C07C229/56 ,  C07C229/60 ,  C07D261/06 ,  C07D275/00 ,  C07D277/40 ,  C07D277/56 ,  C07D333/04

Abstract: Compositions and methods for treating macular degeneration and other forms of retinal disease whose etiology involves the accumulation of A2E and/or lipofuscin, and, more specifically, for preventing the formation and/or accumulation of A2E are disclosed