公开(公告)号：US20230285514A1

公开(公告)日：2023-09-14

申请号：US17785279

申请日：2020-12-18

申请人： Elisabetta BIANCHI ,  Paul E. CARRINGTON ,  Qiaolin DENG ,  Songnian LIN ,  Federica ORVIETO ,  Anandan PALANI ,  Antonello PESSI ,  Tomi K. SAWYER ,  Merck Sharp & Dohme LLC

发明人： Elisabetta Bianchi ,  Paul E. Carrington ,  Qiaolin Deng ,  Songnian Lin ,  Federica Orvieto ,  Anandan Palani ,  Antonello Pessi ,  Tomi K. Sawyer

IPC分类号： A61K38/26 ,  A61K38/28 ,  C07K14/605

CPC分类号： A61K38/26 ,  A61K38/28 ,  C07K14/605

摘要： The stapled peptides of the present invention, and pharmaceutically acceptable salts thereof, are co-agonists of the glucagon and GLP-1 receptors, and may be useful in the treatment, prevention and suppression of diseases mediated by the glucagon receptor and the GLP-1 receptor, including but not limited to, metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity.

公开(公告)号：US10793615B2

公开(公告)日：2020-10-06

申请号：US15759911

申请日：2016-10-21

申请人： Merck Sharp & Dohme Corp. ,  Anandan Palani ,  Ravi Nargund ,  Paul E. Carrington ,  Tomi Sawyer ,  Qiaolin Deng ,  Antonello Pessi ,  Elisabetta Bianchi ,  Federica Orvieto

发明人： Anandan Palani ,  Ravi Nargund ,  Paul E. Carrington ,  Tomi Sawyer ,  Qiaolin Deng ,  Antonello Pessi ,  Elisabetta Bianchi ,  Federica Orvieto

IPC分类号： A61K38/00 ,  A61K38/28 ,  A61P3/04 ,  A61P7/12 ,  A61P3/10 ,  C07K14/435 ,  C07K14/605

摘要： Long-acting co-agonists of the glucagon and GLP-1 receptors are described.

公开(公告)号：US20190338008A1

公开(公告)日：2019-11-07

申请号：US15759911

申请日：2016-10-21

申请人： Anandan PALANI ,  Ravi NARGUND ,  Paul E. CARRINGTON ,  Tomi SAWYER ,  Qiaolin DENG ,  Antonello PESSI ,  Elisabetta BIANCHI ,  Fe-derica ORYIETO ,  Merck Sharp & Dohme Corp.

发明人： Anandan Palani ,  Ravi Nargund ,  Paul E. Carrington ,  Tomi Sawyer ,  Qiaolin Deng ,  Antonello Pessi ,  Elisabetta Bianchi ,  Federica Orvieto

IPC分类号： C07K14/605 ,  A61P3/04 ,  A61K38/28

摘要： Long-acting co-agonists of the glucagon and GLP-1 receptors are described.

公开(公告)号：US20190175744A1

公开(公告)日：2019-06-13

申请号：US16083201

申请日：2017-03-13

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

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

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

摘要： 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：US12060357B2

公开(公告)日：2024-08-13

申请号：US17657515

申请日：2022-03-31

申请人： Merck Sharp & Dohme LLC

发明人： Matthew A. Larsen ,  Amjad Ali ,  Jared Cumming ,  Duane DeMong ,  Qiaolin Deng ,  Thomas H. Graham ,  Elisabeth Hennessy ,  Andrew J. Hoover ,  Ping Liu ,  Kun Liu ,  Umar Faruk Mansoor ,  Jianping Pan ,  Christopher W. Plummer ,  Aaron Sather ,  Uma Swaminathan ,  Huijun Wang ,  Yonglian Zhang

IPC分类号： C07D487/04 ,  C07K16/28

CPC分类号： C07D487/04 ,  C07K16/2818

摘要： In its many embodiments, the present invention provides certain 9-substituted amino triazolo quinazoline compounds of the structural Formula (I):




and pharmaceutically acceptable salts thereof, wherein, ring A, R1 and R2 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.

公开(公告)号：US20230270825A1

公开(公告)日：2023-08-31

申请号：US17785772

申请日：2020-12-18

申请人： Merck Sharp & Dohme LLC

发明人： Elisabetta Bianchi ,  Qiaolin Deng ,  Songnian Lin ,  Federica Orvieto ,  Anandan Palani ,  Antonello Pessi ,  Tomi K. Sawyer

IPC分类号： A61K38/26 ,  C07K14/605 ,  A61K38/28 ,  C07K1/107

CPC分类号： A61K38/26 ,  A61K38/28 ,  C07K1/1077 ,  C07K14/605

摘要： The stapled peptides of the present invention, and pharmaceutically acceptable salts thereof, are co-agonists of the glucagon and GLP-1 receptors, and may be useful in the treatment, prevention and suppression of diseases mediated by the glucagon receptor and the GLP-1 receptor, including but not limited to, metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity.

公开(公告)号：US20230063794A1

公开(公告)日：2023-03-02

申请号：US17785287

申请日：2020-12-18

申请人： Merck Sharp & Dohme LLC

发明人： Elisabetta Bianchi ,  Qiaolin Deng ,  Songnian Lin ,  Federica Orvieto ,  Anandan Palani ,  Antonello Pessi ,  Tomi K. Sawyer

IPC分类号： A61K38/26 ,  C07K14/605 ,  A61K38/28

摘要： The stapled peptides of the present invention, and pharmaceutically acceptable salts thereof, are co-agonists of the glucagon and GLP-1 receptors, and may be useful in the treatment, prevention and suppression of diseases mediated by the glucagon receptor and the GLP-1 receptor, including but not limited to, metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity.

公开(公告)号：US20070299101A1

公开(公告)日：2007-12-27

申请号：US11666966

申请日：2005-10-31

申请人： Steven Colletti ,  Richard Beresis ,  Weichun Chen ,  James Tata ,  Hong Shen ,  Daria Marley ,  Qiaolin Deng ,  Jessica Frie ,  Fa-Xiang Ding

发明人： Steven Colletti ,  Richard Beresis ,  Weichun Chen ,  James Tata ,  Hong Shen ,  Daria Marley ,  Qiaolin Deng ,  Jessica Frie ,  Fa-Xiang Ding

IPC分类号： A61K31/47 ,  A61K31/195 ,  A61K31/403 ,  A61K31/41 ,  A61P3/10 ,  C07C233/64 ,  C07D215/02 ,  C07D257/04 ,  C07D487/00 ,  C07D513/00 ,  C07D471/02 ,  C07D217/00 ,  C07D209/56 ,  A61P9/00 ,  A61K31/425 ,  A61K31/428 ,  A61K31/437

CPC分类号： C07C233/55 ,  C07C235/38 ,  C07C237/20 ,  C07C237/22 ,  C07C255/57 ,  C07C259/10 ,  C07C271/30 ,  C07C271/58 ,  C07C275/42 ,  C07C311/08 ,  C07C311/13 ,  C07D213/80 ,  C07D215/14 ,  C07D215/18 ,  C07D215/20 ,  C07D215/227 ,  C07D215/38 ,  C07D217/02 ,  C07D217/24 ,  C07D231/54 ,  C07D231/56 ,  C07D235/30 ,  C07D257/04 ,  C07D261/20 ,  C07D277/82 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

摘要： The present invention relates to niacin receptor agonists of formula: (I); as well as pharmaceutically acceptable salts and solvates. The compounds are useful for treating dyslipidemias, and in particular, reducing serum LDL, VLDL and triglycerides, and raising HDL levels. Pharmaceutical compositions and methods of treatment are also included.

摘要翻译： 本发明涉及式（I）的烟酸受体激动剂： 以及药学上可接受的盐和溶剂合物。 该化合物可用于治疗血脂异常，特别是降低血清LDL，VLDL和甘油三酸酯，并提高HDL水平。 还包括药物组合物和治疗方法。

公开(公告)号：US20160060255A1

公开(公告)日：2016-03-03

申请号：US14786464

申请日：2014-04-22

申请人： Neville J. ANTHONY ,  Brain M. ANDERSEN ,  Alan B. NORTHRUP ,  Kaleen K. CHILDERS ,  Anthony FRIO ,  Thomas A. MILLER ,  Yuan LIU ,  Michelle R. MACHACEK ,  Hyun Chong WOO ,  Kerrie B. SPENCER ,  John Michael ELLIS ,  Micheal D. ALTMAN ,  Eric T. ROMEO ,  Daniel GUAY ,  Jonathan GRIMM ,  Marie-Eve LEBRUN ,  Joel S. ROBICHAUD ,  Liping WANG ,  Byron DUBOIS ,  Qiaolin DENG ,  MERICK SHARP & DOHNE CORP. ,  MERCK CANADA INC.

发明人： Neville J. Anthony ,  Brian M. Andresen ,  Alan B. Northrup ,  Kaleen K. Childers ,  Anthony Donofrio ,  Thomas A. Miller ,  Yuan Liu ,  Michelle R. Machacek ,  Hyun Chong Woo ,  Kerrie B. Spencer ,  John Michael Ellis ,  Michael D. Altman ,  Eric T. Romeo ,  Daniel Guay ,  Jonathan Grimm ,  Marie-Eve Lebrun ,  Joel S. Robichaud ,  Liping Wang ,  Byron DuBois ,  Qiaolin Deng

IPC分类号： C07D417/14 ,  A61K31/53 ,  A61K31/4439 ,  A61K31/501 ,  A61K31/506 ,  A61K31/497

CPC分类号： C07D417/14 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/53 ,  C07D417/12

摘要： The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, and R4 are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).

摘要翻译： 本发明提供式（I）的某些噻唑取代的氨基杂芳基化合物或其药学上可接受的盐，其中X 1，X 2，X 3，X 4，Y 1，Y 2，Y 3，Y 4和R 4如本文所定义。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗由脾脏酪氨酸激酶（Syk）介导的疾病或病症的方法。

公开(公告)号：US08193365B2

公开(公告)日：2012-06-05

申请号：US12815146

申请日：2010-06-14

申请人： Amjad Ali ,  Joann Bohn ,  Qiaolin Deng ,  Zhijian Lu ,  Peter J. Sinclair ,  Gayle Taylor ,  Christopher Thompson ,  Nazia Quraishi

发明人： Amjad Ali ,  Joann Bohn ,  Qiaolin Deng ,  Zhijian Lu ,  Peter J. Sinclair ,  Gayle Taylor ,  Christopher Thompson ,  Nazia Quraishi

IPC分类号： C07D261/02 ,  C07D209/04 ,  C07D307/93 ,  A01N57/26 ,  A01N57/00

CPC分类号： A61K31/343 ,  A61K31/381 ,  A61K31/404 ,  A61K31/42 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/455 ,  A61K31/47 ,  A61K31/472 ,  A61K38/00 ,  A61K45/06 ,  C07C233/16 ,  C07C271/16 ,  C07C271/20 ,  C07C271/22 ,  C07C275/32 ,  C07C311/04 ,  C07C311/08 ,  C07C317/32 ,  C07D209/08 ,  C07D213/54 ,  C07D215/12 ,  C07D217/02 ,  C07D261/08 ,  C07D271/10 ,  C07D307/14 ,  C07D307/79 ,  C07D333/20 ,  C07D333/22 ,  C07D333/28 ,  A61K2300/00

摘要： Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula 1, A1 and A2 are each an aromatic ring, a 5-6-membered heterocyclic ring, an aromatic ring fused to a heterocyclic ring, a phenyl ring fused to a heterocyclic ring, or a cycloalkyl ring.

摘要翻译： 式I化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于培养HDL-胆固醇，降低LDL-胆固醇，以及治疗或预防动脉粥样硬化。 在式1化合物中，A1和A2各自为芳环，5-6元杂环，稠合于杂环的芳环，稠合于杂环的苯环或环烷基环。