公开(公告)号：US20190307753A1

公开(公告)日：2019-10-10

申请号：US16301935

申请日：2017-05-11

Applicant: Alan WHITEHEAD ,  Olga ORNOSKI ,  Subharekha RAGHAVAN ,  Raphaelle BERGER ,  Joie GARFUNKLE ,  Zhiqiang YANG ,  Gang JI ,  Falong JIANG ,  Jianmin FU ,  Merck Sharp & Dohme Corp.

Inventor： Alan Whitehead ,  Olga Ornoski ,  Subharekha Raghavan ,  Raphaelle Berger ,  Joie Garfunkle ,  Zhiqiang Yang ,  Gang JI ,  Falong Jiang ,  Jianmin Fu

IPC: A61K31/519 ,  C07D519/00 ,  A61P9/12

Abstract: The invention provides certain fused pyrazine compounds of the Formula (I) or a pharmaceutically acceptable salts thereof, wherein X, Y, R1, R3, R4a, R5a, R5b, R6, and the subscript t are as described herein. The compounds or their pharmaceutically acceptable salts can modulate the body's production of cyclic guanosine monophosphate (“cGMP”), and are generally suitable for the therapy and prophylaxis of diseases or disorders which are associated with a disturbed cGMP balance. The invention also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of the abovementioned diseases and disorders and for preparing pharmaceutical s for this purpose.

公开(公告)号：US20190175744A1

公开(公告)日：2019-06-13

申请号：US16083201

申请日：2017-03-13

Applicant: Anandan PALANI ,  Chunhui HUANG ,  Zhiqiang YANG ,  Lin YAN ,  Songnian LIN ,  Pei HUO ,  Qiaolin DENG ,  Elisabetta BIANCHI ,  Federica ORVIETO ,  Merck Sharp & Dohme Corp.

Inventor： Anandan Palani ,  Chunhui Huang ,  Zhiqiang Yang ,  Lin Yan ,  Songnian Lin ,  Pei Huo ,  Qiaolin Deng ,  Elisabetta Bianchi ,  Federica Orvieto

IPC: A61K47/64 ,  A61K38/28 ,  A61K38/26

Abstract: Insulin-incretin conjugates comprising a peptide having agonist activity at the glucagon-like 1 (GLP-1) receptor, the glucagon (GCG) receptor, and/or the gastric inhibitory protein (GIP) receptor conjugated to an insulin molecule having agonist activity at the insulin receptor and use of the conjugates for treatment of metabolic diseases, for example, Type 2 diabetes, are described.

公开(公告)号：US20100216841A1

公开(公告)日：2010-08-26

申请号：US11922399

申请日：2006-06-28

Applicant: James C. Barrow ,  Craig W. Lindsley ,  William D. Shipe ,  Zhiqiang Yang ,  David Wisnoski

Inventor： James C. Barrow ,  Craig W. Lindsley ,  William D. Shipe ,  Zhiqiang Yang ,  David Wisnoski

IPC: A61K31/445 ,  C07D211/34 ,  C07D405/06 ,  C07D403/06 ,  C07D413/06 ,  C07D417/06 ,  A61K31/453 ,  A61K31/454 ,  A61P25/00

CPC classification number: C07D211/38

Abstract: The present invention is directed to 4-fluoro-piperidine compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.

Abstract translation: 本发明涉及作为T型钙通道拮抗剂的4-氟哌啶化合物，其可用于治疗或预防涉及T型钙通道的神经和精神疾病及疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及T型钙通道的疾病中的用途。

公开(公告)号：US10780092B2

公开(公告)日：2020-09-22

申请号：US16301935

申请日：2017-05-11

Applicant: Merck Sharp & Dohme Corp. ,  Alan Whitehead ,  Olga Ornoski ,  Subharekha Raghavan ,  Raphaelle Berger ,  Joie Garfunkle ,  Zhiqiang Yang ,  Gang Ji ,  Falong Jiang ,  Jianmin Fu

Inventor： Alan Whitehead ,  Olga Ornoski ,  Subharekha Raghavan ,  Raphaelle Berger ,  Joie Garfunkle ,  Zhiqiang Yang ,  Gang Ji ,  Falong Jiang ,  Jianmin Fu

IPC: C07D487/04 ,  C07D519/00 ,  A61K31/519 ,  A61P9/12

Abstract: The invention provides certain fused pyrazine compounds of the Formula (I) or a pharmaceutically acceptable salts thereof, wherein X, Y, R1, R3, R4a, R5a, R5b, R6, and the subscript t are as described herein. The compounds or their pharmaceutically acceptable salts can modulate the body's production of cyclic guanosine monophosphate (“cGMP”), and are generally suitable for the therapy and prophylaxis of diseases or disorders which are associated with a disturbed cGMP balance. The invention also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of the abovementioned diseases and disorders and for preparing pharmaceuticals for this purpose.

公开(公告)号：US09193697B2

公开(公告)日：2015-11-24

申请号：US13635303

申请日：2011-04-04

Applicant: ZhiQiang Yang ,  Philippe G. Nantermet ,  Constantine Kreatsoulas ,  Keith P. Moore ,  Evan Foster Shalen

Inventor： ZhiQiang Yang ,  Philippe G. Nantermet ,  Constantine Kreatsoulas ,  Keith P. Moore ,  Evan Foster Shalen

IPC: C07D263/46 ,  C07D413/14 ,  C07D413/04 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4439 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/437 ,  A61K31/422 ,  A61K31/541 ,  A61K31/433 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/421 ,  A61P19/02 ,  A61P29/00 ,  A61P25/00 ,  A61P25/06 ,  A61P25/20 ,  A61P25/28 ,  A61P25/16 ,  C07D471/04 ,  C07D491/08 ,  C07D417/14 ,  C07D487/04 ,  A61K31/506

CPC classification number: C07D263/46 ,  C07D413/04 ,  C07D413/14

Abstract: The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. 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 osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.

Abstract translation: 本发明涉及可用作脂肪酸酰胺水解酶（FAAH）和FAAH成像剂的调节剂的某些恶唑衍生物。 本发明还涉及包含这些化合物作为活性成分的药物制剂，以及这些化合物及其制剂在治疗某些疾病，包括骨关节炎，类风湿性关节炎，糖尿病性神经病变，带状疱疹后神经痛，ke肉肌痛和纤维肌痛等方面的用途。 作为急性疼痛，偏头痛，睡眠障碍，阿尔茨海默病和帕金森病。

公开(公告)号：US20080167329A1

公开(公告)日：2008-07-10

申请号：US11886053

申请日：2006-03-08

Applicant: James C. Barrow ,  Rowena V. Cube ,  Phung Le Ngo ,  Kenneth E. Rittle ,  Zhiqiang Yang ,  Steven D. Young

Inventor： James C. Barrow ,  Rowena V. Cube ,  Phung Le Ngo ,  Kenneth E. Rittle ,  Zhiqiang Yang ,  Steven D. Young

IPC: A61K31/517 ,  C07D239/80 ,  A61P43/00 ,  A61P25/08 ,  A61P25/02 ,  A61P25/16 ,  A61P25/00 ,  A61P25/18 ,  A61P25/20

CPC classification number: C07D239/82 ,  C07D401/06 ,  C07D405/06

Abstract: The present invention is directed to quinazolinone compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.

Abstract translation: 本发明涉及作为T型钙通道拮抗剂的喹唑啉酮化合物，其可用于治疗或预防其中涉及T型钙通道的疾病和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及T型钙通道的疾病中的用途。

公开(公告)号：US08501773B2

公开(公告)日：2013-08-06

申请号：US11922399

申请日：2006-06-28

Applicant: James C. Barrow ,  Craig W. Lindsley ,  William D. Shipe ,  Zhiqiang Yang ,  David Wisnoski

Inventor： James C. Barrow ,  Craig W. Lindsley ,  William D. Shipe ,  Zhiqiang Yang ,  David Wisnoski

IPC: A01N43/42 ,  A01N43/40 ,  A61K31/47 ,  A61K31/445 ,  C07D211/00 ,  C07D295/00 ,  C07D211/08 ,  C07D401/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D421/00

CPC classification number: C07D211/38

Abstract: The present invention is directed to 4-fluoro-piperidine compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.

Abstract translation: 本发明涉及作为T型钙通道拮抗剂的4-氟哌啶化合物，其可用于治疗或预防涉及T型钙通道的神经和精神疾病及疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及T型钙通道的疾病中的用途。

公开(公告)号：US20100261741A1

公开(公告)日：2010-10-14

申请号：US12824702

申请日：2010-06-28

Applicant: James C. Barrow ,  Rowena V. Cube ,  Phung Le Ngo ,  Kenneth E. Rittle ,  Zhiqiang Yang ,  Steven D. Young

Inventor： James C. Barrow ,  Rowena V. Cube ,  Phung Le Ngo ,  Kenneth E. Rittle ,  Zhiqiang Yang ,  Steven D. Young

IPC: A61K31/517 ,  C07D239/82 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/30 ,  C07D239/80

CPC classification number: C07D239/82 ,  C07D401/06 ,  C07D405/06

Abstract: The present invention is directed to quinazolinone compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.

公开(公告)号：US20160200715A1

公开(公告)日：2016-07-14

申请号：US14912212

申请日：2014-08-18

Applicant: Zhiqiang YANG ,  Guizhen DONG ,  Milana MALETIC ,  MERCK SHARP & DOHME CORP.

Inventor： Zhiqiang Yang ,  Guizhen Dong ,  Milana Maletic

IPC: C07D413/14 ,  A61K31/444 ,  C07D405/14 ,  A61K31/4439 ,  A61K45/06

CPC classification number: A61K31/60 ,  A61K31/4155 ,  A61K31/4245 ,  A61K31/4365 ,  A61K31/4439 ,  A61K31/444 ,  A61K45/06 ,  C07D405/14 ,  C07D413/14 ,  A61K2300/00

Abstract: The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof wherein: R1 is W is and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ASC, secondary prevention of myocardial infarction or stroke, or PAD.

Abstract translation: 本发明涉及下式的双环烟肼衍生物或其药学上可接受的盐，其中：R1是W，其余变量在本文中描述。 本发明的化合物是PAR-1受体的有效抑制剂。 本发明化合物可用于治疗或预防疾病状态如ASC，二次预防心肌梗塞或中风或PAD。

公开(公告)号：US20100081428A1

公开(公告)日：2010-04-01

申请号：US12238611

申请日：2008-09-26

Applicant: Harunobu Maejima ,  Vijay Sundar Rajaram ,  Zhiqiang Yang ,  Hitoshi Takanashi

Inventor： Harunobu Maejima ,  Vijay Sundar Rajaram ,  Zhiqiang Yang ,  Hitoshi Takanashi

IPC: H04W4/00 ,  H04W36/00 ,  H04M1/00

CPC classification number: H04W36/0055 ,  H04L65/1006 ,  H04L65/1093

Abstract: A technique to transfer a first telephony session between a first telephony device and a second telephony device from being conducted through a first network interface of the first telephony device to being conducted through a second network interface of the first telephony device includes the following. A second telephony session between the first network interface and the second network interface is initiated, and subsequently a media termination point of the first telephony session is changed from the first network interface to the second network interface. The technique further includes changing a media termination point of the second telephony session from the first network interface to a location associated with the second telephony device.

Abstract translation: 将在第一电话设备和第二电话设备之间传送第一电话会话的技术从通过第一电话设备的第一网络接口传导到通过第一电话设备的第二网络接口进行的技术包括以下。 启动第一网络接口和第二网络接口之间的第二电话会话，随后第一电话会话的媒体终止点从第一网络接口改变到第二网络接口。 该技术还包括将第二电话会话的媒体终止点从第一网络接口改变为与第二电话设备相关联的位置。