公开(公告)号：US20210188863A1

公开(公告)日：2021-06-24

申请号：US16755172

申请日：2018-10-08

Applicant: David Annunziato CANDITO ,  Thomas, H. GRAHAM ,  John ACTON ,  Ryan Wing-Kun CHAU ,  Joanna L. CHEN ,  J. Michael ELLIS ,  Peter H. FULLER ,  Anmol GULATI ,  Hakan GUNAYDIN ,  Solomon KATTAR ,  Mitchell Henry KEYLOR ,  Blair T. LAPOINTE ,  Ping LIU ,  Weiguo LIU ,  Joey L. METHOT ,  Santhosh F. NEELAMKAVIL ,  Vladimir SIMOV ,  Ling TONG ,  Harold B. WOOD ,  Merck Sharp & Dohme Corp.

Inventor： David Annunziato Candito ,  Thomas H. Graham ,  John Acton ,  Ryan Wing-Kun Chau ,  Joanna L. Chen ,  J. Michael Ellis ,  Peter H. Fuller ,  Anmol Gulati ,  Hakan Gunaydin ,  Solomon Kattar ,  Mitchell Henry Keylor ,  Blair T. Lapointe ,  Ping Liu ,  Weiguo Liu ,  Joey L. Methot ,  Santhosh F. Neelamkavil ,  Vladimir Simov ,  Ling Tong ,  Harold B. Wood

IPC: C07D491/10 ,  C07D403/14 ,  C07D487/08 ,  C07D405/14 ,  C07D401/14 ,  C07D413/14 ,  C07D498/10 ,  C07D519/00 ,  C07D498/04 ,  C07D403/04

Abstract: The present invention is directed to substituted certain reversed indazolyl-spiro[2.2]pentane-carbonitrile derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X, Y, and Z are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. 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 LRRK-2 kinase is involved.

公开(公告)号：US09815846B2

公开(公告)日：2017-11-14

申请号：US15128689

申请日：2015-03-23

Applicant: Merck Sharp & Dohme Corp. ,  MSD R & D (China) Co., LTD.

Inventor： Helen Mitchell ,  Mark E. Fraley ,  Andrew J. Cooke ,  Craig A. Stump ,  Yi-Heng Chen ,  Xu-Fang Zhang ,  Casey C. McComas ,  Kathy Schirripa ,  Melody McWherter ,  Swati P. Mercer ,  Kerim Babaoglu ,  Dongfang Meng ,  Jane Wu ,  Ping Liu ,  Harold B. Wood ,  Jianming Bao ,  Chun Sing Li ,  Qinghua Mao ,  Zhiqi Qi

IPC: C07D491/107 ,  C07C233/66 ,  C07D213/75 ,  C07D403/12 ,  C07D401/12 ,  C07D417/12 ,  C07D239/42 ,  C07D401/04 ,  C07D413/12 ,  C07D417/14 ,  C07D401/14 ,  C07D405/12 ,  C07D413/14 ,  C07D403/14 ,  C07D405/14 ,  C07D471/04 ,  C07D401/06 ,  C07D413/06 ,  C07D403/06

CPC classification number: C07D491/107 ,  C07C233/66 ,  C07D213/75 ,  C07D231/12 ,  C07D239/42 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

Abstract: The present invention is directed to six membered heteroaryl benzamide compounds of formula (I), which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.

公开(公告)号：US20150274664A1

公开(公告)日：2015-10-01

申请号：US14431366

申请日：2013-09-25

Applicant: John J. ACTON ,  Scott D. EDMONDSON ,  Ping LIU ,  Michael W. MILLER ,  Harold B. WOOD ,  Byron G. DUBOIS ,  William B. GEISS ,  MERCK SHARP & DOHME CORP.

Inventor： John J. Acton ,  Scott D. Edmondson ,  Ping Liu ,  Michael W. Miller ,  Harold B. Wood ,  Byron G. DuBois ,  William B. Geiss

IPC: C07D211/60 ,  C07D401/12 ,  C07D413/04 ,  C07D401/14 ,  C07D401/04

CPC classification number: C07D211/60 ,  A61K31/506 ,  C07D211/22 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D413/04 ,  C07D413/14

Abstract: Substituted cyclopropyl piperidinyl compounds and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.

Abstract translation: 公开了用于治疗或预防2型糖尿病和类似病症的取代的环丙基哌啶基化合物及其药学上可接受的盐。 该化合物可用作G蛋白偶联受体GPR-119的激动剂。 还包括药物组合物和治疗方法。

公开(公告)号：US09045467B2

公开(公告)日：2015-06-02

申请号：US14099142

申请日：2013-12-06

Applicant: Merck Sharp & Dohme Corp.

Inventor： Harry Chobanian ,  Linus S. Lin ,  Ping Liu ,  Marc D. Chioda ,  Robert J. DeVita ,  Ravi P. Nargund ,  Yan Guo

IPC: A01N43/40 ,  A61K31/44 ,  C07D413/14 ,  C07D263/46 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D417/14 ,  C07D271/06 ,  C07D271/10

CPC classification number: C07D413/14 ,  C07D263/46 ,  C07D271/06 ,  C07D271/10 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D417/14

Abstract: The present invention is directed to certain oxazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). 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）抑制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：US20140171437A1

公开(公告)日：2014-06-19

申请号：US14099142

申请日：2013-12-06

Applicant: Merck Sharp & Dohme Corp.

Inventor： Harry Chobanian ,  Linus S. Lin ,  Ping Liu ,  Marc D. Chioda ,  Robert J. DeVita ,  Ravi P. Nargund ,  Yan Guo

IPC: C07D413/14 ,  C07D271/10 ,  C07D271/06 ,  C07D413/04 ,  C07D263/46

CPC classification number: C07D413/14 ,  C07D263/46 ,  C07D271/06 ,  C07D271/10 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D417/14

Abstract: The present invention is directed to certain oxazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). 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, Alzeimer Disease, and Parkinson's Disease.

Abstract translation: 本发明涉及可用作脂肪酸酰胺水解酶（FAAH）抑制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：US20220220117A1

公开(公告)日：2022-07-14

申请号：US17657515

申请日：2022-03-31

Applicant: Merck Sharp & Dohme Corp.

Inventor： 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: C07D487/04

Abstract: 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：US11161854B2

公开(公告)日：2021-11-02

申请号：US16755172

申请日：2018-10-08

Applicant: Merck Sharp & Dohme Corp. ,  David Annunziato Candito ,  Thomas H. Graham ,  John Acton ,  Ryan Wing-Kun Chau ,  Joanna L. Chen ,  J. Michael Ellis ,  Peter H. Fuller ,  Anmol Gulati ,  Hakan Gunaydin ,  Solomon Kattar ,  Mitchell Henry Keylor ,  Blair T. Lapointe ,  Ping Liu ,  Weiguo Liu ,  Joey L. Methot ,  Santhosh F. Neelamkavil ,  Vladimir Simov ,  Ling Tong ,  Harold B. Wood

Inventor： David Annunziato Candito ,  Thomas H. Graham ,  John Acton ,  Ryan Wing-Kun Chau ,  Joanna L. Chen ,  J. Michael Ellis ,  Peter H. Fuller ,  Anmol Gulati ,  Hakan Gunaydin ,  Solomon Kattar ,  Mitchell Henry Keylor ,  Blair T. Lapointe ,  Ping Liu ,  Weiguo Liu ,  Joey L. Methot ,  Santhosh F. Neelamkavil ,  Vladimir Simov ,  Ling Tong ,  Harold B. Wood

IPC: C07D491/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D487/08 ,  C07D498/04 ,  C07D498/10 ,  C07D519/00

Abstract: The present invention is directed to substituted certain reversed indazolyl-spiro[2.2]pentane-carbonitrile derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X, Y, and Z are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. 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 LRRK-2 kinase is involved.

公开(公告)号：US20210107904A1

公开(公告)日：2021-04-15

申请号：US16695367

申请日：2019-11-26

Applicant: Merck Sharp & Dohme Corp.

Inventor： 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: C07D487/04

Abstract: 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：US20160060256A1

公开(公告)日：2016-03-03

申请号：US14786466

申请日：2014-04-22

Applicant: Kenneth L. ARRINGTON ,  Byron DUBOIS ,  John S. DEBENHAM ,  Ping LIU ,  Alan B. NORTHRUP ,  Jason W. SZEWCZYK ,  Liping WANG ,  Ming WANG ,  MERCK SHARP & DOHME CORP.

Inventor： Kenneth L. Arrington ,  Byron DuBois ,  John S. Debenham ,  Ping Liu ,  Alan B. Northrup ,  Jason W. Szewczyk ,  Liping Wang ,  Ming Wang

IPC: C07D417/14 ,  C07D417/12 ,  A61K31/5377 ,  A61K31/506

CPC classification number: C07D417/14 ,  A61K31/427 ,  A61K31/506 ,  A61K31/5377 ,  C07D417/12

Abstract: The invention provides certain thiazole-substituted aminopyrimidine compounds of the Formula (I) (I), or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R5, R6, and the subscripts r, s, and t 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).

Abstract translation: 本发明提供了式（I）（I）的某些噻唑取代的氨基嘧啶化合物或其药学上可接受的盐，其中R1，R2，R3，R5，R6和下标r，s和t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：US20140329798A1

公开(公告)日：2014-11-06

申请号：US14358241

申请日：2012-11-09

Applicant: Merck Sharp & Dohme Corp.

Inventor： Scott Edmondson ,  Zhiyong Hu ,  Ping Liu ,  Gregori J. Morriello ,  Jason W. Szewczyk ,  Bowei Wang ,  Liping Wang ,  Harold B. Wood ,  Cheng Zhu ,  Yuping Zhu ,  Zhiqiang Guo

IPC: C07D513/04 ,  C07D239/42 ,  C07D405/12 ,  C07D409/12 ,  C07D498/04 ,  C07D487/04 ,  C07D403/14 ,  C07D401/14 ,  C07D403/12 ,  C07D471/04

CPC classification number: C07D513/04 ,  C07D239/42 ,  C07D401/04 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04

Abstract: Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included

Abstract translation: 披露式（I）的取代的环丙基化合物及其药学上可接受的盐可用于治疗或预防2型糖尿病和类似病状。 该化合物可用作G蛋白偶联受体GPR-119的激动剂。 还包括药物组合物和治疗方法