公开(公告)号：US10307407B2

公开(公告)日：2019-06-04

申请号：US15553593

申请日：2016-02-26

申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN

发明人： Shaomeng Wang ,  Yujun Zhao ,  Bing Zhou ,  Angelo Aguilar

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

摘要： 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：US20180036294A1

公开(公告)日：2018-02-08

申请号：US15553593

申请日：2016-02-26

申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN

发明人： Shaomeng WANG ,  Yujun ZHAO ,  Bing ZHOU ,  Angelo AGUILAR

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

CPC分类号： A61K31/437 ,  A61K31/519 ,  C07D231/38 ,  C07D261/06 ,  C07D471/04 ,  C07D487/04 ,  C07D487/14

摘要： 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

申请人： Industry-University Cooperation Foundation Hanyang University ERICA Campus

发明人： Jung-Mi Hah ,  Kyung Jin Jung

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

CPC分类号： A61K31/415 ,  C07C233/07 ,  C07C233/10 ,  C07D261/02 ,  C07D261/06 ,  C07D261/18 ,  C07D413/12

摘要： 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：US09133189B2

公开(公告)日：2015-09-15

申请号：US14212713

申请日：2014-03-14

申请人： Epizyme, Inc.

发明人： Richard Chesworth ,  Lorna Helen Mitchell ,  Gideon Shapiro ,  Oscar Miguel Moradei

IPC分类号： A61K31/415 ,  A61K31/437 ,  A61K31/428 ,  A61K31/4155 ,  A61K31/42 ,  C07D231/10 ,  C07D239/20 ,  C07D261/06 ,  C07D403/02 ,  C07D277/62 ,  C07D471/04 ,  C07D513/02 ,  C07D409/04 ,  C07D403/04 ,  C07D413/04 ,  C07D231/12 ,  C07D407/04 ,  C07D411/04

CPC分类号： C07D471/04 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/42 ,  A61K31/428 ,  A61K31/437 ,  C07D231/12 ,  C07D403/04 ,  C07D405/04 ,  C07D407/04 ,  C07D409/04 ,  C07D411/04 ,  C07D413/04 ,  C07D417/04

摘要： Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.

公开(公告)号：US20130072490A1

公开(公告)日：2013-03-21

申请号：US13499052

申请日：2010-09-29

申请人： Ryan Clark ,  Brian Andrew Stearns ,  Jill Melissa Scott ,  Heather Renee Coate ,  Lucy Zhao ,  Thomas Jon Seiders ,  Deborah Volkots ,  Jeannie Arruda ,  Nicholas Simon Stock ,  Yen Pham Truong ,  David Nathan Zalatan

发明人： Ryan Clark ,  Brian Andrew Stearns ,  Jill Melissa Scott ,  Heather Renee Coate ,  Lucy Zhao ,  Thomas Jon Seiders ,  Deborah Volkots ,  Jeannie Arruda ,  Nicholas Simon Stock ,  Yen Pham Truong ,  David Nathan Zalatan

IPC分类号： A61K31/42 ,  C07D413/14 ,  C07D413/04 ,  C07D261/14 ,  C07D413/06 ,  C07D261/06

CPC分类号： C07D231/38 ,  C07D261/08 ,  C07D261/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.

摘要翻译： 本文描述的是作为溶血磷脂受体拮抗剂的化合物。 还描述了包括本文所述化合物的药物组合物和药物，以及使用这些拮抗剂单独和与其它化合物组合用于治疗LPA依赖性或LPA介导的病症或疾病的方法。

公开(公告)号：US08258162B2

公开(公告)日：2012-09-04

申请号：US13002475

申请日：2009-06-26

申请人： Takehiro Ishikawa ,  Satoko Kobayashi ,  Hitoshi Inoue ,  Yasunori Ueno ,  Masako Yoshida ,  Nobuyuki Tanaka

发明人： Takehiro Ishikawa ,  Satoko Kobayashi ,  Hitoshi Inoue ,  Yasunori Ueno ,  Masako Yoshida ,  Nobuyuki Tanaka

IPC分类号： A61K31/04 ,  A61K31/426 ,  A61K31/42 ,  A61K31/381 ,  C07C205/06 ,  C07D277/20 ,  C07D261/06 ,  C07D333/02

CPC分类号： C07C205/61 ,  A61K31/192 ,  A61K31/24 ,  A61K31/277 ,  A61K31/351 ,  A61K31/381 ,  A61K31/40 ,  A61K31/42 ,  A61K31/425 ,  A61K31/4453 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/55 ,  A61K45/06 ,  C07C255/56 ,  C07C255/57 ,  C07C259/10 ,  C07C2601/14 ,  C07C2601/18 ,  C07D261/08 ,  C07D277/24 ,  C07D295/10 ,  C07D309/06 ,  C07D333/22 ,  A61K2300/00

摘要： The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen, lower acyl, lower alkoxycarbonyl or the like; R3 is lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or the like; R4 is cyano, lower alkoxycarbonyl, carboxy or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

摘要翻译： 本发明提供由通式（I）表示的化合物或其药学上可接受的盐，其中R 1和R 2各自为氢，低级酰基，低级烷氧基羰基等; R 3是低级烷基，卤素 - 低级烷基，环烷基，杂环烷基，任选取代的芳基，任选取代的杂芳基等; R4是氰基，低级烷氧基羰基，羧基等，其表现出强烈的COMT抑制活性。 本发明还提供含有所述化合物的药物组合物及其用途。

公开(公告)号：US08119667B2

公开(公告)日：2012-02-21

申请号：US11611997

申请日：2006-12-18

申请人： Tomasz W. Glinka ,  Dale Edward Shuster ,  Chander Shekher Celly ,  Robert D. Simmons ,  Jason Zhang

发明人： Tomasz W. Glinka ,  Dale Edward Shuster ,  Chander Shekher Celly ,  Robert D. Simmons ,  Jason Zhang

IPC分类号： A61K31/44 ,  A61K31/41 ,  A61K31/42 ,  A61K31/265 ,  C07D211/78 ,  C07D285/12 ,  C07D261/06 ,  C07C69/96

CPC分类号： C07C317/32 ,  A61K31/222 ,  A61K31/265 ,  A61K31/42 ,  A61K31/433 ,  A61K31/44 ,  A61K45/06 ,  C07B2200/07 ,  C07C233/18 ,  C07C2601/02 ,  C07C2601/14 ,  C07D213/40 ,  C07D213/84 ,  A61K2300/00

摘要： Novel fenicol compounds having useful properties as antibiotic prodrugs, are provided, together with methods of making and using these new compounds.

摘要翻译： 提供了具有作为抗生素前药的有用性质的新型芬西醇化合物，以及制备和使用这些新化合物的方法。

公开(公告)号：US20110152295A1

公开(公告)日：2011-06-23

申请号：US13060756

申请日：2009-09-02

申请人： Jean-Philippe Leclerc ,  Chun Sing Li ,  Yeeman K. Ramtohul

发明人： Jean-Philippe Leclerc ,  Chun Sing Li ,  Yeeman K. Ramtohul

IPC分类号： A61K31/506 ,  C07D277/30 ,  C07D401/14 ,  C07D257/04 ,  C07D271/06 ,  C07D417/14 ,  C07D261/06 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/41 ,  A61K31/4245 ,  A61K31/422 ,  A61P9/10

CPC分类号： A61K31/4192 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/506 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14

摘要： Heteroaromatic compounds of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.

摘要翻译： 结构式I的杂芳族化合物是相对于其它已知的硬脂酰辅酶A去饱和酶的硬脂酰辅酶Aδ-9去饱和酶（SCD1）的选择性抑制剂。 本发明的化合物可用于预防和治疗与脂质合成和代谢异常有关的病症，包括心血管疾病，如动脉粥样硬化; 肥胖; 糖尿病; 神经系统疾病; 代谢综合征; 胰岛素抵抗; 和肝脂肪变性。

公开(公告)号：US07951827B2

公开(公告)日：2011-05-31

申请号：US11415982

申请日：2006-05-02

申请人： Richard R. Tidwell ,  Svetlana M. Bakunova ,  Stanislav Bakunov ,  Donald A. Patrick

发明人： Richard R. Tidwell ,  Svetlana M. Bakunova ,  Stanislav Bakunov ,  Donald A. Patrick

IPC分类号： A61K31/42 ,  C07D261/06 ,  C07D413/02

CPC分类号： C07D261/08 ,  C07D413/10 ,  C07D413/14

摘要： Novel dicationic 3,5-diphenylisoxazole compounds are described. Synthetic routes to these novel compounds are provided. Several of the compounds displayed in vitro activity versus Trypanosoma brucei brucei and Plasmodium falciparum comparable to that of furamidine. A majority of the novel compounds also were less toxic to VERO cells than furamidine.

摘要翻译： 描述了新型的阳离子3,5-二苯基异恶唑化合物。 提供了这些新化合物的合成路线。 几种化合物显示体外活性与布鲁斯氏锥虫和恶性疟原虫相当，与呋喃丹相当。 大多数新型化合物对VERO细胞的毒性相对于呋脒更少。

公开(公告)号：US07863308B2

公开(公告)日：2011-01-04

申请号：US12100555

申请日：2008-04-10

申请人： Thomas G. Gant ,  Sepehr Sarshar

发明人： Thomas G. Gant ,  Sepehr Sarshar

IPC分类号： A61K31/422 ,  C07D261/06

CPC分类号： C07D413/14 ,  C07D413/12

摘要： Disclosed herein are substituted pyrimidine-based endothelin modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

摘要翻译： 本文公开了式I的取代的基于嘧啶的内皮素调节剂，其制备方法，其药物组合物及其使用方法。