公开(公告)号：US20220235041A1

公开(公告)日：2022-07-28

申请号：US17619338

申请日：2020-06-02

申请人： Brendan M. CROWLEY ,  Philippe NANTERMET ,  David OLSEN ,  Takao SUZUKI ,  Merck Sharp & Dohme Corp.

发明人： Brendan M. Crowley ,  Philippe Nantermet ,  David Olsen ,  Takao Suzuki

IPC分类号： C07D413/14 ,  C07D413/12 ,  C07D417/10 ,  A61K31/422 ,  A61K31/541 ,  C07D471/04 ,  A61K31/437 ,  C07D413/10 ,  A61K45/06 ,  A61P31/06 ,  A61P31/08

摘要： Disclosed are dihydroisoxazole compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, E, and R1 are as defined herein. Also disclosed are compositions which comprise at least one of these dihydroisoxazole compounds, methods for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis comprising administering a therapeutically effective amount of these dihydroisoxazole compounds and/or a pharmaceutically acceptable salt thereof, or a composition comprising such compound and/or salt.

公开(公告)号：US20220081403A1

公开(公告)日：2022-03-17

申请号：US17422308

申请日：2019-12-19

申请人： Randall R. MILLER ,  Joseph A. KOZLOWSKI ,  Philippe NANTERMET ,  David B. OLSEN ,  Jing SU ,  Uihu YANG ,  Takao SUZUKI ,  Brendan M. CROWLEY ,  Nengxue WANG ,  Lanying YOU ,  Merck Sharp & Dohme Corp.

发明人： Randall R. Miller ,  Joseph A. Kozlowski ,  Philippe Nantermet ,  David B. Olsen ,  Jing Su ,  Lihu Yang ,  Takao Suzuki ,  Brendan Crowley ,  Negxue Wang ,  Lanying You

IPC分类号： C07D263/06 ,  C07D471/04 ,  C07D413/12 ,  C07D495/04 ,  C07F9/653 ,  C07F9/6553 ,  A61K31/422 ,  A61K31/421 ,  A61K31/437 ,  A61K31/498 ,  A61K31/4439 ,  A61K31/541 ,  A61P31/06 ,  A61K45/06

摘要： The present invention discloses oxazolidinone compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A and E, are as defined herein. The present invention also relates to compositions which comprise at least one oxazolidinone compound of the invention. The invention also provides methods for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis comprising administering a therapeutically effective amount of an oxazolidinone of the invention and/or a pharmaceutically acceptable salt thereof, or a composition comprising such compound and/or salt.

公开(公告)号：US10519147B2

公开(公告)日：2019-12-31

申请号：US16061815

申请日：2016-12-15

申请人： Merck Sharp & Dohme Corp. ,  Thomas J. Greshock ,  James Mulhearn ,  Liangqin Guo ,  Ting Zhang ,  Deping Wang ,  Ronald M. Kim ,  Mark E. Layton ,  Michael J. Kelly, III ,  Rajan Anand ,  Philippe Nantermet ,  Tianying Jian ,  Anthony J. Roecker ,  Walter Won ,  Gang Zhou

发明人： Thomas J. Greshock ,  James Mulhearn ,  Liangqin Guo ,  Ting Zhang ,  Deping Wang ,  Ronald M. Kim ,  Mark E. Layton ,  Michael J. Kelly, III ,  Rajan Anand ,  Philippe Nantermet ,  Tianying Jian ,  Anthony J. Roecker ,  Walter Won ,  Gang Zhou

IPC分类号： C07D417/12 ,  A61K45/06 ,  C07D277/52 ,  C07D285/135 ,  A61P25/02 ,  A61P25/04 ,  A61P11/14 ,  A61P17/04

摘要： Disclosed are compounds of Formula A, or a salt thereof, where Q, X, R1 and R2 are as defined herein, which compounds have properties for inhibiting Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain (acute, post-operative, neuropathic), or cough or itch disorders using the same.

公开(公告)号：US20180362518A1

公开(公告)日：2018-12-20

申请号：US16061815

申请日：2016-12-15

申请人： Thomas J. GRESHOCK ,  James MULHEARN ,  Liangqin GUO ,  Ting ZHANG ,  Deping WANG ,  Ronald M. KIM ,  Mark E. LAYTON ,  Michael J. KELLY, III ,  Rajan ANAND ,  Tianying JIAN ,  Philippe NANTERMET ,  Anthony J. ROECKER ,  Walter WON ,  Gang ZHOU ,  Merck Sharp & Dohme Corp.

发明人： Thomas J. Greshock ,  James Mulhearn ,  Liangqin Guo ,  Ting Zhang ,  Deping Wang ,  Ronald M. Kim ,  Mark E. Layton ,  Michael J. Kelly, III ,  Rajan Anand ,  Philippe Nantermet ,  Tianying Jian ,  Anthony J. Roecker ,  Walter Won ,  Gang Zhou

IPC分类号： C07D417/12 ,  C07D285/135 ,  C07D277/52 ,  A61P11/14 ,  A61P17/04 ,  A61P25/04 ,  A61P25/02

CPC分类号： C07D417/12 ,  A61K45/06 ,  A61P11/14 ,  A61P17/04 ,  A61P25/02 ,  A61P25/04 ,  C07D277/52 ,  C07D285/135

摘要： Disclosed are compounds of Formula A, or a salt thereof, where Q, X, R1 and R2 are as defined herein, which compounds have properties for inhibiting Na 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain (acute, post-operative, neuropathic), or cough or itch disorders using the same.

公开(公告)号：US20190233406A1

公开(公告)日：2019-08-01

申请号：US16246068

申请日：2019-01-11

申请人： Merck Sharp & Dohme Corp.

发明人： Thomas J. Greshock ,  James Mulhearn ,  Junying Zheng ,  Ronald M. Kim ,  Ting Zhang ,  Anthony J. Roecker ,  Walter Won ,  Philippe Nantermet ,  Rajan Anand ,  Gang Zhou ,  Deping Wang ,  Liangqin Guo

IPC分类号： C07D417/12 ,  A61K31/426 ,  A61K31/433 ,  A61K31/427 ,  A61K31/551 ,  C07D277/52 ,  C07D285/08 ,  A61K45/06

CPC分类号： C07D417/12 ,  A61K31/426 ,  A61K31/427 ,  A61K31/433 ,  A61K31/551 ,  A61K45/06 ,  C07D277/52 ,  C07D285/08 ,  A61K2300/00

摘要： Disclosed are compounds of Formula A, or a salt thereof: wherein R1, R2, and E are defined herein, which compounds have properties for inhibiting Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain disorders, cough, and itch using the same.

公开(公告)号：US20220064147A1

公开(公告)日：2022-03-03

申请号：US17413882

申请日：2019-12-13

申请人： Merck Sharp & Dohme Corp.

发明人： Antonella Converso ,  Abdellatif El Marrouni ,  Ashley Forster ,  Jessica L. Frie ,  David N. Hunter ,  Scott D. Kuduk ,  Helen J. Mitchell ,  Philippe Nantermet ,  Deyou Sha ,  William Daniel Shipe ,  Cheng Wang ,  Deping Wang

IPC分类号： C07D403/06 ,  A61K45/06

摘要： The present disclosure is directed to pyrimidone derivatives of Formula I and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV nave cells, and for the treatment or prophylaxis of infection by HIV, or for the treatment, prophylaxis or delay in the onset or progression of AIDS or AIDS Related Complex (ARC).

公开(公告)号：US10221167B2

公开(公告)日：2019-03-05

申请号：US15378465

申请日：2016-12-14

申请人： Merck Sharp & Dohme Corp.

发明人： Thomas J. Greshock ,  James Mulhearn ,  Junying Zheng ,  Ronald M. Kim ,  Ting Zhang ,  Anthony J. Roecker ,  Walter Won ,  Philippe Nantermet ,  Rajan Anand ,  Gang Zhou ,  Deping Wang ,  Liangqin Guo

IPC分类号： C07D417/12 ,  C07D285/08 ,  C07D277/52 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/4168 ,  A61K31/426 ,  A61K31/427 ,  A61K31/433 ,  A61K31/551 ,  A61K45/06

摘要： Disclosed are compounds of Formula A, or a salt thereof: wherein R1, R2, and E are defined herein, which compounds have properties for inhibiting Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain disorders, cough, and itch using the same.

公开(公告)号：US20170174674A1

公开(公告)日：2017-06-22

申请号：US15378465

申请日：2016-12-14

申请人： Merck Sharp & Dohme Corp.

发明人： Thomas J. Greshock ,  James Mulhearn ,  Junying Zheng ,  Ronald M. Kim ,  Ting Zhang ,  Anthony J. Roecker ,  Walter Won ,  Philippe Nantermet ,  Rajan Anand ,  Gang Zhou ,  Deping Wang ,  Liangqin Guo

IPC分类号： C07D417/12 ,  C07D277/52 ,  A61K31/551 ,  A61K31/427 ,  A61K31/433 ,  A61K31/426 ,  C07D285/08 ,  A61K45/06

CPC分类号： C07D417/12 ,  A61K31/426 ,  A61K31/427 ,  A61K31/433 ,  A61K31/551 ,  A61K45/06 ,  C07D277/52 ,  C07D285/08 ,  A61K2300/00

摘要： Disclosed are compounds of Formula A, or a salt thereof: wherein R1, R2, and E are defined herein, which compounds have properties for inhibiting Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain disorders, cough, and itch using the same.

公开(公告)号：US20100093811A1

公开(公告)日：2010-04-15

申请号：US12523200

申请日：2008-09-22

申请人： Craig A. Coburn ,  Joseph P. Vacca ,  Hemaka A. Rajapakse ,  Kristen L.G. Jones ,  Philippe Nantermet ,  James C. Barrow ,  Keith P. Moore ,  Steven S. Sharik ,  Cory Theberge ,  Abbas M. Walji

发明人： Craig A. Coburn ,  Joseph P. Vacca ,  Hemaka A. Rajapakse ,  Kristen L.G. Jones ,  Philippe Nantermet ,  James C. Barrow ,  Keith P. Moore ,  Steven S. Sharik ,  Cory Theberge ,  Abbas M. Walji

IPC分类号： A61K31/44 ,  C07C311/15 ,  A61K31/18 ,  C07C271/06 ,  A61K31/27 ,  C07D277/62 ,  A61K31/426 ,  C07D213/55 ,  A61P31/18

CPC分类号： C07C311/41 ,  C07C311/18 ,  C07C311/29 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2603/32 ,  C07D213/30 ,  C07D277/64

摘要： Compounds of Formula I are disclosed: (I), wherein XA, k, R1, R2, R3, R4, R5, R5A, R6, R6A, R7 and R8 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

摘要翻译： 公开了式I的化合物：其中XA，k，R1，R2，R3，R4，R5，R5A，R6，R6A，R7和R8如本文所定义。 式I所包括的化合物包括可以在体内代谢为HIV蛋白酶抑制剂的HIV蛋白酶抑制剂和其它化合物的化合物。 化合物及其药学上可接受的盐可用于预防或治疗HIV感染以及预防，治疗或延迟艾滋病的发病。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

公开(公告)号：US20070060569A1

公开(公告)日：2007-03-15

申请号：US11591861

申请日：2006-11-02

申请人： Roger Fujimoto ,  Leslie McQuire ,  Lauren Monovich ,  Philippe Nantermet ,  David Parker ,  Leslie Robinson ,  Jerry Skiles ,  Ruben Tommasi

发明人： Roger Fujimoto ,  Leslie McQuire ,  Lauren Monovich ,  Philippe Nantermet ,  David Parker ,  Leslie Robinson ,  Jerry Skiles ,  Ruben Tommasi

IPC分类号： A61K31/55 ,  A61K31/501 ,  A61K31/454 ,  A61K31/4545 ,  C07D409/02 ,  C07D417/02 ,  C07D405/02 ,  C07D403/02

CPC分类号： C07D401/12 ,  C07D211/34 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12

摘要： Compound of the formula wherein R represents OH or NHOH; R1 represents hydrogen, optically substituted lower alkyl, aryl-lower alkyl, cycloalkyl-lower alkyl, or acyl derived from a carboxylic acid, from a carbonic acid, from a carbamic acid or from a sulfonic acid; R2 represents biarylsulfonyl or aryloxyrylsulfonyl; R3 represents hydrogen, optionally substituted lower alkyl, aryl-lower alkyl, cycloalkyl-lower alkyl or acyl derived from a carboxylic acid, from a carbonic acid or from a carbamic acid; R4 and R5 represent independently hydrogen, lower alkyl, lower alkoxycarbonyl, aryl-lower alkyl or cycloalkyl-lower alkyl; m is zero, 1, 2 or 3; pharmaceutically acceptable prodrug derivatives thereof; pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; and their use for inhibiting matrix degrading metalloproteinases and preventing or treating matrix metalloproteinase dependent conditions in mammals.

摘要翻译： 下式的化合物其中R表示OH或NHOH; R 1表示氢，光取代的低级烷基，芳基 - 低级烷基，环烷基 - 低级烷基或衍生自羧酸的酰基，来自碳酸，氨基甲酸或磺酸; R 2表示联芳基磺酰基或芳氧基酰基磺酰基; R 3表示氢，任选取代的低级烷基，芳基 - 低级烷基，环烷基 - 低级烷基或衍生自羧酸的酰基，来自碳酸或氨基甲酸; R 4和R 5独立地表示氢，低级烷基，低级烷氧基羰基，芳基 - 低级烷基或环烷基 - 低级烷基; m为零，1,2或3; 其药学上可接受的前药衍生物; 其药学上可接受的盐; 包含所述化合物的药物组合物; 以及它们用于抑制基质降解金属蛋白酶和预防或治疗哺乳动物中基质金属蛋白酶依赖性条件的用途。