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1. 发明授权

US10208064B2 Inhibitors of the renal outer medullary potassium channel 有权
公开(公告)号：US10208064B2
公开(公告)日：2019-02-19
申请号：US15323989
申请日：2015-07-09
申请人： MERCK SHARP & DOHME CORP. , Alexander Pasternak , Ian Davies , Fa-Xiang Ding , Jinlong Jiang , Shuzhi Dong , Xin Gu , Takao Suzuki , Joseph P. Vacca , Zhifa Pu , Shouning Xu
发明人： Alexander Pasternak , Ian Davies , Fa-Xiang Ding , Jinlong Jiang , Shuzhi Dong , Xin Gu , Takao Suzuki , Joseph P. Vacca , Zhifa Pu , Shouning Xu
IPC分类号： C07D513/10 , C07D519/00 , A61K45/06 , A61K31/435 , A61K31/4745 , A61K31/4375
摘要： The present invention provides compounds of Formula (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.

2. 发明申请

US20170197989A1 INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL 审中-公开
公开(公告)号：US20170197989A1
公开(公告)日：2017-07-13
申请号：US15323989
申请日：2015-07-09
申请人： Alexander PASTERNAK , Ian DAVIES , Fa-Xiang DING , Jinlong JIANG , Shuzhi DONG , Xin GU , Takao SUZUKI , Joseph P. VACCA , Zhifa PU , Shouning XU , Merck Sharp & Dohme Corp.
发明人： Alexander Pasternak , Ian Davies , Fa-Xiang Ding , Jinlong Jiang , Shuzhi Dong , Xin Gu , Takao Suzuki , Joseph P. Vacca , Zhifa Pu , Shouning Xu
IPC分类号： C07D519/00 , A61K31/4745 , A61K31/4375 , A61K31/435
CPC分类号： C07D519/00 , A61K31/435 , A61K31/4375 , A61K31/4745 , A61K45/06
摘要： The present invention provides compounds of Formula (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.

3. 发明申请

US20160324833A1 INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL 有权
标题翻译：肾脏外部药物通道的抑制剂
公开(公告)号：US20160324833A1
公开(公告)日：2016-11-10
申请号：US15101481
申请日：2014-12-19
申请人： Shuzhi DONG , Alexander PASTERNAK , Xin GU , Qinghong FU , Jinlong JIANG , Fa-Xiang DING , Haifeng TANG , Reynalda K. DEJESUS , Takao SUZUKI , MERCK SHARP & DOHME CORP.
发明人： Shuzhi Dong , Alexander Pasternak , Xin Gu , Qinghong Fu , Jinlong Jiang , Fa-Xiang Ding , Haifeng Tang , Reynalda K. DeJesus , Takao Suzuki
IPC分类号： A61K31/435 , C07D471/10 , A61K31/444 , A61K31/506 , A61K31/438 , C07D498/10 , A61K31/537 , A61K31/497 , C07D519/00 , A61K31/437 , A61K45/06 , A61K31/501
CPC分类号： A61K31/435 , A61K31/437 , A61K31/438 , A61K31/444 , A61K31/4545 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/537 , A61K45/06 , C07D471/10 , C07D498/10 , C07D519/00 , A61K2300/00
摘要： Novel spirocyclic compounds of formula I: and pharmaceutically acceptable salts thereof are disclosed as inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention. Pharmaceutical compositions and methods of treatment are also included.

4. 发明申请

US20160002259A1 INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL 有权
标题翻译：肾脏外部药物通道的抑制剂
公开(公告)号：US20160002259A1
公开(公告)日：2016-01-07
申请号：US14768245
申请日：2014-02-12
申请人： Alexander PASTERNAK , Reynalda Keh DE JESUS , Fa-xiang DING , Shuzhi DONG , Jessica FRIE , Xin GU , Jinlong JIANG , Aurash SHAHRIPOUR , Barbara PIO , Haifeng TANG , Shawn WALSH , MERCK SHARP & DOHME CORP.
发明人： Alexander Pasternak , Reynalda Keh DeJesus , Fa-Xiang Ding , Shuzhi Dong , Jessica L. Frie , Xin Gu , Jinlong Jiang , Aurash Shahripour , Barbara Pio , Haifeng Tang , Shawn Walsh
IPC分类号： C07D498/04 , A61K45/06 , A61K31/4985 , A61K31/5383 , C07D487/04
CPC分类号： C07D498/04 , A61K31/401 , A61K31/403 , A61K31/41 , A61K31/4178 , A61K31/4184 , A61K31/4422 , A61K31/4985 , A61K31/5383 , A61K31/55 , A61K31/675 , A61K45/06 , C07D487/04 , C07D519/00 , A61K2300/00
摘要： The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure, kidney disease, edema, and conditions associated with excessive salt and water retention.
摘要翻译：本发明提供式I化合物及其药学上可接受的盐，它们是ROMK（Kir1.1）通道的抑制剂。该化合物可以用作利尿剂和/或利尿钠剂，并用于治疗和预防包括心血管疾病如高血压，心力衰竭，肾脏疾病，水肿以及与过量的盐和水保留有关的病症的医学病症。

5. 发明申请

US20130040929A1 NOVEL PROLYLCARBOXYPEPTIDASE INHIBITORS 有权
公开(公告)号：US20130040929A1
公开(公告)日：2013-02-14
申请号：US13642646
申请日：2011-05-06
申请人： Jeffrey J. Hale , Jinlong Jiang , Dong-Ming Shen , Zhi-Cai Shi , Min Shu , Zhicai Wu , Cangming Yang
发明人： Jeffrey J. Hale , Jinlong Jiang , Dong-Ming Shen , Zhi-Cai Shi , Min Shu , Zhicai Wu , Cangming Yang
IPC分类号： A61K31/506 , C07D401/04 , A61K31/454 , A61K31/4545 , A61P3/00 , C07D413/14 , A61K31/5377 , A61K31/4985 , A61P3/04 , A61P3/10 , C07D401/14 , A61K31/497
CPC分类号： C07D401/04 , C07D401/14
摘要： Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.

6. 发明授权

US07345083B2 Hydroisoindoline tachykinin receptor antagonists 有权
标题翻译：羟基异吲哚啉速激肽受体拮抗剂
公开(公告)号：US07345083B2
公开(公告)日：2008-03-18
申请号：US11714352
申请日：2007-03-06
申请人： Jaime Lynn Bunda , Robert J. DeVita , Jinlong Jiang , Sander G. Mills
发明人： Jaime Lynn Bunda , Robert J. DeVita , Jinlong Jiang , Sander G. Mills
IPC分类号： A61K31/4035 , C07D209/44
CPC分类号： C07D209/44
摘要： The present invention is directed to certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
摘要翻译：本发明涉及可用作神经激肽-1（NK-1）受体拮抗剂，速激肽抑制剂，特别是物质P的某些加氢异吲哚啉化合物。本发明还涉及包含这些化合物作为活性成分的药物制剂和使用化合物及其制剂治疗某些疾病，包括呕吐，尿失禁，抑郁和焦虑。

7. 发明授权

US07084156B2 2-Aminoquinoline compounds 失效
标题翻译： 2-氨基喹啉化合物
公开(公告)号：US07084156B2
公开(公告)日：2006-08-01
申请号：US10496615
申请日：2002-11-22
申请人： Robert J. DeVita , Lehua Chang , Danny Chaung , MyLe Hoang , JinLong Jiang , Peter Lin , Andreas W. Sailer , Jonathan R. Young
发明人： Robert J. DeVita , Lehua Chang , Danny Chaung , MyLe Hoang , JinLong Jiang , Peter Lin , Andreas W. Sailer , Jonathan R. Young
IPC分类号： C07D215/38 , C07D215/16 , A61K31/47
CPC分类号： C07D215/227 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/04 , C07D417/14 , C07D491/04 , C07D495/10
摘要： The present invention is concerned with compounds of the general Formula I: and pharmaceutically acceptable salts thereof, which are useful as melanin concentrating hormone receptor antagonists, particularly MCH-1R antagonists. As such, compounds of the present invention are useful for the treatment or prevention of obesity or eating disorders associated with excessive food intake and complications thereof, osteoarthritis, certain cancers, AIDS wasting, cachexia, frailty (particularly in elderly), mental disorders stress, cognitive disorders, sexual function, reproductive function, kidney function, locomotor disorders, attention deficit disorder (ADD), substance abuse disorders and dyskinesias, Huntington's disease, epilepsy, memory function, and spinal muscular atrophy. Compounds of formula I may therefore be used in the treatment of these conditions, and in the manufacture of a medicament useful in treating these conditions. Pharmaceutical formulations comprising one of the compounds of formula (I) as an active ingredient are disclosed, as are processes for preparing these compounds.
摘要翻译：本发明涉及通式I的化合物及其药学上可接受的盐，其可用作黑色素浓缩激素受体拮抗剂，特别是MCH-1R拮抗剂。因此，本发明的化合物可用于治疗或预防与食物过量摄取及其并发症，骨关节炎，某些癌症，艾滋病消瘦，恶病质，虚弱（特别是老年人）相关的肥胖或进食障碍，精神障碍压力，认知障碍，性功能，生殖功能，肾功能，运动障碍，注意力缺陷障碍（ADD），药物滥用障碍和运动障碍，亨廷顿病，癫痫，记忆功能和脊髓性肌肉萎缩。因此，式I化合物可用于治疗这些病症，以及制备用于治疗这些病症的药物。作为制备这些化合物的方法，公开了包含式（I）化合物之一作为活性成分的药物制剂。

8. 发明申请

US20050165083A1 Hydroisoindoline tachykinin receptor antagonists 有权
标题翻译：羟基异吲哚啉速激肽受体拮抗剂
公开(公告)号：US20050165083A1
公开(公告)日：2005-07-28
申请号：US11043213
申请日：2005-01-26
申请人： Jaime Bunda , Robert DeVita , Jinlong Jiang , Sander Mills
发明人： Jaime Bunda , Robert DeVita , Jinlong Jiang , Sander Mills
IPC分类号： C07D209/44 , A61K31/4035
CPC分类号： C07D209/44
摘要： The present invention is directed to certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
摘要翻译：本发明涉及可用作神经激肽-1（NK-1）受体拮抗剂，速激肽抑制剂，特别是物质P的某些加氢异吲哚啉化合物。本发明还涉及包含这些化合物作为活性成分的药物制剂和使用化合物及其制剂治疗某些疾病，包括呕吐，尿失禁，抑郁和焦虑。

9. 发明授权

US6150352A Antagonists of gonadotropin releasing hormone 失效
标题翻译：促性腺激素释放激素的拮抗剂
公开(公告)号：US6150352A
公开(公告)日：2000-11-21
申请号：US180662
申请日：1998-11-12
申请人： Mark Goulet , Eric E Allen , Matthew J. Wyvratt, Jr. , Jinlong Jiang , Richard B. Toupence , Thomas F Walsh , Feroze Ujjainwalla , Jonathan R Young , Robert J. Devita
发明人： Mark Goulet , Eric E Allen , Matthew J. Wyvratt, Jr. , Jinlong Jiang , Richard B. Toupence , Thomas F Walsh , Feroze Ujjainwalla , Jonathan R Young , Robert J. Devita
IPC分类号： C07D473/00 , A61K31/00 , A61K31/47 , A61K31/4709 , A61K31/472 , A61K31/4725 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/50 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/52 , A61K31/529 , A61P5/00 , A61P5/06 , A61P5/24 , A61P15/00 , A61P25/20 , A61P35/00 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D451/02 , C07D453/02 , C07D473/32 , C07D487/04 , C07D487/08 , C07D495/04 , C07D31/47
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D451/02 , C07D473/32 , C07D487/04 , C07D495/04
摘要： There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related conditions in both men and women.
摘要翻译： PCT No.PCT / US97 / 08432 Sec。 371日期：1998年11月12日 102（e）1998年11月12日日期PCT提交1997年5月16日PCT公布。公开号WO97 / 44339 日期1997年11月27日公开了可用作GnRH拮抗剂的式（I）化合物及其药学上可接受的盐，因此可用于治疗男性和女性中各种性激素相关病症。

10. 发明申请

US20190276443A1 INDOLE DERIVATIVES USEFUL AS INHIBITORS OF DIACYLGLYCERIDE O-ACYLTRANSFERASE 2 审中-公开
公开(公告)号：US20190276443A1
公开(公告)日：2019-09-12
申请号：US16461880
申请日：2017-11-13
申请人： Dong-Ming SHEN , Thomas H. GRAHAM , Jinlong JIANG , Fa-Xiang DING , Clare TUDGE , Merck Sharp & Dohme Corp.
发明人： Dong-Ming Shen , Thomas H. Graham , Jinlong Jiang , Fa-Xiang Ding , Clare Tudge
IPC分类号： C07D409/12 , A61P1/16 , C07D209/08 , C07D401/12 , C07D413/12 , C07D409/14
摘要： The present invention relates to a compound represented by formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, nonalcoholic steatohepatitis (NASH), cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.

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