公开(公告)号：US20240300980A1

公开(公告)日：2024-09-12

申请号：US18563357

申请日：2022-05-22

Applicant: SHANGHAI KECHOW PHARMA, INC.

Inventor： Hongqi Tian ,  Gongchao Huang ,  Xuguang Gao ,  Huanhuan Liu ,  Xingkai Wang

IPC: C07D519/00 ,  A61K31/4995 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5386 ,  A61K31/547 ,  A61P35/00 ,  C07D487/04 ,  C07D487/08

CPC classification number: C07D519/00 ,  A61K31/4995 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5386 ,  A61K31/547 ,  A61P35/00 ,  C07D487/04 ,  C07D487/08

Abstract: Disclosed is a compound of formula (I) and (II) or a pharmaceutically acceptable salt, prodrug, tautomer or stereoisomer, and solvate thereof. The compound can be applied to treatment of cancers and inflammations of mammals. Further disclosed are a preparation method for the compound of formula (I) and (II) and a pharmaceutical composition containing the compound.

公开(公告)号：US09725468B2

公开(公告)日：2017-08-08

申请号：US15021011

申请日：2014-09-08

Applicant: Merck Sharp & Dohme Corp.

Inventor： Jack D. Scott ,  Wen-Lian Wu ,  Jared N. Cumming

IPC: C07D513/10 ,  C07D519/00 ,  C07D417/12 ,  A61K31/547 ,  A61K45/06 ,  C07D471/04 ,  C07D279/16

CPC classification number: C07D513/10 ,  A61K31/547 ,  A61K45/06 ,  C07D279/16 ,  C07D417/12 ,  C07D471/04 ,  C07D519/00 ,  A61K2300/00

Abstract: In its many embodiments, the present invention provides certain C5-spiro iminothiadiazine dioxide compounds, including compounds Formula (I): or a tautomers and/or stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein RL, X, Y, R1A, R1B, R2, R3, m, and RA are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.

公开(公告)号：US09458181B2

公开(公告)日：2016-10-04

申请号：US14506760

申请日：2014-10-06

Applicant: Merck Sharp & Dohme Corp.

Inventor： Shawn Stachel ,  Daniel V. Paone ,  Jing Li ,  Kausik Nanda

IPC: A61K31/421 ,  C07D263/32 ,  C07D263/34 ,  C07D277/30 ,  C07D413/04 ,  C07D413/10 ,  C07D417/10 ,  C07D417/14 ,  C07D495/08 ,  C07F7/08 ,  A61K31/695 ,  A61K31/422 ,  A61K31/547 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/496 ,  C07D513/08 ,  A61K31/427 ,  A61K45/06 ,  C07D413/12

CPC classification number: C07F7/0807 ,  A61K31/421 ,  A61K31/422 ,  A61K31/427 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/547 ,  A61K31/695 ,  A61K45/06 ,  C07D263/32 ,  C07D263/34 ,  C07D277/30 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D417/14 ,  C07D495/08 ,  C07D513/08

Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

公开(公告)号：US20160222032A1

公开(公告)日：2016-08-04

申请号：US15021011

申请日：2014-09-08

Applicant: Jack D. SCOTT ,  Wen-Lian WU ,  Jared N. CUMMING ,  MERCK SHARP & DOHME CORP.

Inventor： Jack D. Scott ,  Wen-Lian Wu ,  Jared N. Cumming

IPC: C07D513/10 ,  A61K45/06 ,  C07D417/12 ,  A61K31/547 ,  C07D519/00

CPC classification number: C07D513/10 ,  A61K31/547 ,  A61K45/06 ,  C07D279/16 ,  C07D417/12 ,  C07D471/04 ,  C07D519/00 ,  A61K2300/00

Abstract: In its many embodiments, the present invention provides certain C5-spiro iminothiadiazine dioxide compounds, including compounds Formula (I): or a tautomers and/or stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein RL, X, Y, R1A, R1B, R2, R3, m, and RA are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.

Abstract translation: 在其许多实施方案中，本发明提供某些C5-螺亚氨基二氮嗪二氧化物化合物，包括式（I）化合物：或其互变异构体和/或立体异构体，以及所述化合物，所述互变异构体和所述立体异构体的药学上可接受的盐，其中RL， X，Y，R 1A，R 1B，R 2，R 3，m和RA如本文所定义。 本发明的新化合物可用作BACE抑制剂和/或用于治疗和预防与其相关的各种病症。 还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和使用方法，包括用于治疗阿尔茨海默氏病的药物组合物。

公开(公告)号：US08871758B2

公开(公告)日：2014-10-28

申请号：US14003080

申请日：2012-03-07

Applicant: Thomas Boehme ,  Christian Engel ,  Stefan Guessregen ,  Torsten Haack ,  Kurt Ritter ,  Georg Tschank

Inventor： Thomas Boehme ,  Christian Engel ,  Stefan Guessregen ,  Torsten Haack ,  Kurt Ritter ,  Georg Tschank

IPC: A61K31/51 ,  A61K45/06 ,  C07D419/12 ,  C07D515/20 ,  A61K31/541 ,  A61K31/547 ,  C07D515/10 ,  C07D291/02 ,  C07D291/06 ,  A61K31/54 ,  C07D291/08

CPC classification number: C07D291/06 ,  A61K31/54 ,  A61K31/541 ,  A61K31/547 ,  A61K45/06 ,  C07D291/02 ,  C07D291/08 ,  C07D419/12 ,  C07D515/10 ,  C07D515/20

Abstract: The invention relates to the compounds of formula (I) and to the physiologically acceptable salts thereof. Said compounds are suitable e.g. for the treatment of hyperglycemia.

Abstract translation: 本发明涉及式（I）化合物及其生理上可接受的盐。 所述化合物是合适的。 用于治疗高血糖症。

公开(公告)号：US20080312292A1

公开(公告)日：2008-12-18

申请号：US12010740

申请日：2008-01-29

Applicant: Kiyoshi Yasui ,  Yasuhide Morioka ,  Kohji Hanasaki

Inventor： Kiyoshi Yasui ,  Yasuhide Morioka ,  Kohji Hanasaki

IPC: A61K31/4412 ,  A61K31/435

CPC classification number: C07D213/69 ,  A61K31/00 ,  A61K31/255 ,  A61K31/426 ,  A61K31/435 ,  A61K31/436 ,  A61K31/4375 ,  A61K31/4412 ,  A61K31/4439 ,  A61K31/4523 ,  A61K31/4704 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/54 ,  A61K31/541 ,  A61K31/5415 ,  A61K31/547 ,  C07D213/70 ,  C07D213/75 ,  C07D213/82 ,  C07D215/38 ,  C07D215/54 ,  C07D217/26 ,  C07D221/04 ,  C07D221/12 ,  C07D221/22 ,  C07D263/46 ,  C07D277/18 ,  C07D279/06 ,  C07D279/08 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D405/12 ,  C07D405/14 ,  C07D411/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D455/06 ,  C07D471/04 ,  C07D493/04 ,  C07D513/04 ,  C07D513/10

Abstract: It is intended to provide antipruritics (drugs to control itching, antiitch agents and drugs to stop itching). It is found out that a compound having an agonistic activity to the cannabinoid receptor shows an antipruritics effect.

Abstract translation: 旨在提供止痒药（用于控制瘙痒的药物，止痒剂和药物以阻止瘙痒）。 发现对大麻素受体具有激动作用的化合物显示出止痒作用。

公开(公告)号：US20170253562A1

公开(公告)日：2017-09-07

申请号：US15287851

申请日：2016-10-07

Applicant: AbbVie Inc.

Inventor： Michael L. Curtin ,  Anil Vasudevan ,  Kevin Woller

IPC: C07D209/44 ,  C07D403/12 ,  C07D405/12 ,  C07D491/10 ,  A61K31/55 ,  A61K31/547 ,  A61K31/5377 ,  A61K31/501 ,  C07D491/107 ,  C07D491/048 ,  C07D487/04 ,  A61K31/551 ,  A61K31/4035 ,  A61K31/4178

CPC classification number: C07D209/44 ,  A61K31/4035 ,  A61K31/4178 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/547 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06 ,  C07D403/12 ,  C07D405/12 ,  C07D487/04 ,  C07D491/048 ,  C07D491/10 ,  C07D491/107 ,  A61K2300/00

Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.

公开(公告)号：US09233982B2

公开(公告)日：2016-01-12

申请号：US14401959

申请日：2013-05-10

Applicant: Ares Trading S.A.

Inventor： Anna Quattropani ,  Dominique Swinnen

IPC: C07D513/10 ,  C07D495/10 ,  C07D498/10 ,  A61K31/547 ,  A61K31/4188 ,  A61K31/4439 ,  A61K31/4245

CPC classification number: C07D513/10 ,  A61K31/4188 ,  A61K31/4245 ,  A61K31/4439 ,  A61K31/547 ,  C07D495/10 ,  C07D498/10

Abstract: The present invention provide compounds of Formula (I) used as BACE inhibitors for the treatment of neurodegenerative diseases.

Abstract translation: 本发明提供用作治疗神经变性疾病的BACE抑制剂的式（I）化合物。

公开(公告)号：US20150099719A1

公开(公告)日：2015-04-09

申请号：US14506760

申请日：2014-10-06

Applicant: Merck Sharp & Dohme Corp.

Inventor： Shawn Stachel ,  Daniel V. Paone ,  Jing Li ,  Kausik Nanda

IPC: C07F7/08 ,  A61K31/422 ,  A61K31/547 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/421 ,  C07D513/08 ,  C07D263/32 ,  C07D413/04 ,  C07D277/30 ,  C07D413/10 ,  A61K31/427 ,  A61K45/06 ,  A61K31/695

CPC classification number: C07F7/0807 ,  A61K31/421 ,  A61K31/422 ,  A61K31/427 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/547 ,  A61K31/695 ,  A61K45/06 ,  C07D263/32 ,  C07D263/34 ,  C07D277/30 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D417/14 ,  C07D495/08 ,  C07D513/08

Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

Abstract translation: 本发明涉及一类新的化合物，它们是半胱氨酸蛋白酶抑制剂，包括但不限于组织蛋白酶K，L，S和B的抑制剂。这些化合物可用于治疗其中指示抑制骨吸收的疾病，例如 骨质疏松症

公开(公告)号：US20090111837A1

公开(公告)日：2009-04-30

申请号：US11817528

申请日：2006-02-16

Applicant: Peter Cox ,  Ross Anderson Kinloch ,  Graham Nigel Maw

Inventor： Peter Cox ,  Ross Anderson Kinloch ,  Graham Nigel Maw

IPC: A61K31/527 ,  C07D239/72 ,  A61P25/02 ,  A61P25/00

CPC classification number: A61K31/527 ,  A61K31/357 ,  A61K31/537 ,  A61K31/547

Abstract: The present invention relates to the use of a phosphodiesterase 7 (PDE7) inhibitor in the manufacture of a medicament for the treatment of neuropathic pain and to a method of treating neuropathic pain using an inhibitor of PDE7.

Abstract translation: 本发明涉及磷酸二酯酶7（PDE7）抑制剂在制备用于治疗神经性疼痛的药物中的用途以及使用PDE7抑制剂治疗神经性疼痛的方法。