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公开(公告)号：US09975888B2
公开(公告)日：2018-05-22
申请号：US15036274
申请日：2014-11-07
Applicant: MERCK SHARP & DOHME CORP.
Inventor： Craig A. Coburn , Milana M. Maletic , Yunfu Luo , Zhiqi Qi , Chun Sing Li , Tingting Yu
IPC: C07D417/14 , C07D417/12 , C07D487/04 , C07D401/12 , C07D405/14 , C07D403/10 , C07D401/14 , A61K45/06 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/4985 , C07D409/14 , C07D471/04 , A61K31/4178 , A61K31/5377
CPC classification number: C07D417/14 , A61K31/4178 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/4985 , A61K31/5377 , A61K45/06 , C07D401/12 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/14 , C07D417/12 , C07D471/04 , C07D487/04 , A61K2300/00
Abstract: The present invention relates to aryl linked imidazole and triazole derivatives, compositions comprising said compounds, alone or in combination with other drugs, and methods of using the compounds for improving the pharmacokinetics of a drug. The compounds of the invention are useful in human and veterinary medicine for inhibiting CYP3A4 and for improving the pharmacokinetics of a therapeutic compound that is metabolized by CYP3A4.
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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.
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公开(公告)号：US09896447B2
公开(公告)日：2018-02-20
申请号：US15023145
申请日：2014-09-17
Applicant: MERCK SHARP & DOHME CORP. , Andrew J. Cooke , Craig A. Stump , Xu-Fang Zhang , Chun Sing Li , Qinghua Mao
Inventor： Andrew J. Cooke , Craig A. Stump , Xu-Fang Zhang , Chun Sing Li , Qinghua Mao
IPC: C07D471/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D239/42 , C07D213/16 , C07D261/14 , C07D231/40
CPC classification number: C07D471/04 , C07D213/16 , C07D231/40 , C07D239/42 , C07D261/14 , C07D401/12 , C07D401/14 , C07D403/12
Abstract: The present invention is directed to benzyl urea compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be 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 Trk-A, Trk-B and/or Trk-C.
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公开(公告)号：US09718819B2
公开(公告)日：2017-08-01
申请号：US15012445
申请日：2016-02-01
Applicant: Merck Sharp & Dohme Corp.
Inventor： Kenneth L. Arrington , Christopher Burgey , Robert Gilfillan , Yongxin Han , Mehul Patel , Chun Sing Li , Yunfu Luo , Zhiyu Lei
IPC: A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D471/04 , A61K31/513 , A61K45/06 , C07D403/06 , C07D405/14 , C07D401/14 , C07D239/56 , C07D403/14 , C07D239/52 , C07D239/54
CPC classification number: C07D471/04 , A61K31/513 , A61K45/06 , C07D239/52 , C07D239/54 , C07D239/56 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14
Abstract: Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein R1, R2, RE, L, M and Z are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment 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.
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公开(公告)号：US20160229804A1
公开(公告)日：2016-08-11
申请号：US15023634
申请日：2014-09-17
Applicant: Andrew J. COOKE , Craig A. STUMP , Xu-Fang ZHANG , Chun Sing LI , Qinghua MAO , MERCK SHARP & DOHME CORP
Inventor： Andrew J. Cooke , Craig A. Stump , Xu-Fang Zhang , Chun Sing Li , Qinghua Mao
IPC: C07D213/75 , C07D405/12 , C07D239/42 , C07D498/04 , C07D231/40 , C07D261/14 , C07D471/04 , C07D233/88 , C07C275/28 , C07D257/04 , C07D249/08 , C07D295/135 , C07D401/04 , C07D487/04 , C07D271/10 , C07D285/12 , C07D405/04 , C07D263/32 , C07D403/04 , C07D277/48
CPC classification number: C07D213/75 , C07C275/28 , C07D231/40 , C07D233/88 , C07D239/42 , C07D249/08 , C07D257/04 , C07D261/14 , C07D263/32 , C07D271/10 , C07D277/44 , C07D277/48 , C07D285/12 , C07D295/135 , C07D311/88 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/12 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04
Abstract: The present invention is directed to benzyl urea compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be 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 Trk-A, Trk-B and/or Trk-C.
Abstract translation: 本发明涉及式（I）的苄基脲化合物，其是原肌球蛋白相关激酶（Trk）家族蛋白激酶抑制剂，因此可用于治疗疼痛，炎症，癌症，再狭窄，动脉粥样硬化，牛皮癣，血栓形成 与神经生长因子（NGF）受体Trk-A，Trk-B和/或Trk-C的异常活动相关的疾病，失调，损伤或与异常髓鞘或脱髓鞘相关的疾病或障碍。
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Patent Agency Ranking
公开(公告)号：US10556900B2
公开(公告)日：2020-02-11
申请号：US15562617
申请日：2016-04-04
Applicant: Merck Sharp & Dohme Corp.
Inventor： Craig A. Stump , Yi Heng Chen , Ping Liu , Dongfang Meng , Jane Yang Wu , Chun Sing Li , Zhiqi Qi
IPC: C07D471/04 , C07D487/04 , C07D403/12 , C07D417/12 , A61P7/02 , A61P17/06 , A61P9/10 , A61P25/00 , A61P35/00
Abstract: The present invention is directed to bicyclic heteroaryl benzamide compounds of formulas (I): which are tropomyos-in-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.
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公开(公告)号：US09914736B2
公开(公告)日：2018-03-13
申请号：US15128782
申请日：2015-03-23
Applicant: Merck Sharp & Dohme Corp.
Inventor： Helen Mitchell , Mark E. Fraley , Andrew J. Cooke , Craig A. Stump , Xu-Fang Zhang , Casey C. McComas , Kathy Schirripa , Melody McWherter , Ping Liu , Dann Parker , Chun Sing Li , Qinghua Mao
IPC: A61K31/40 , C07D487/04 , C07D277/46 , C07D231/40 , C07D417/12 , C07D401/04 , C07D417/14 , C07D403/14 , C07D401/14 , C07D403/04 , C07D403/12 , C07D413/12 , C07D413/14 , C07D471/04
CPC classification number: C07D487/04 , C07D231/40 , C07D277/46 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
Abstract: The present invention is directed to substituted five membered heteroaryl benzamide compounds of formula (I) (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.
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公开(公告)号：US09862716B2
公开(公告)日：2018-01-09
申请号：US15129206
申请日：2015-03-23
Applicant: Merck Sharp & Dohme Corp.
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 , Keith P. Moore , Ping Liu , Harold B. Wood , Chun Sing Li , Qinghua Mao , Douglas C. Beshore
IPC: C07D471/04 , C07D513/04
CPC classification number: C07D403/12 , C07D401/12 , C07D403/14 , C07D471/04 , C07D487/04 , C07D513/04
Abstract: The present invention is directed to a bicyclic 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.
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公开(公告)号：US09862707B2
公开(公告)日：2018-01-09
申请号：US15128793
申请日：2015-03-23
Applicant: Merck Sharp & Dohme Corp.
Inventor： Helen Mitchell , Harold B. Wood , Chun Sing Li , Qinghua Mao , Zhiqi Qi
IPC: C07D403/12 , C07D471/04 , C07D403/14 , C07D487/04 , C07D401/12
CPC classification number: C07D403/12 , C07D401/12 , C07D403/14 , C07D471/04 , C07D487/04 , C07D513/04
Abstract: The present invention is directed to a bicyclic 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.
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公开(公告)号：US20170158698A1
公开(公告)日：2017-06-08
申请号：US15128782
申请日：2015-03-23
Applicant: Helen MITCHELL , Mark E. FRALEY , Andrew J. COOKE , Craig A. STUMP , Xu-Fang ZHANG , Casey C. MCCOMAS , Kathy SCHIRRIPA , Melody MCWHERTER , Ping LIU , Dann PARKER , Chun Sing LI , Qinghua MAO , Merck Sharp & Dohme Corp.
Inventor： Helen Mitchell , Mark E. Fraley , Andrew J. Cooke , Craig A. Stump , Xu-Fang Zhang , Casey C. McComas , Kathy Schirripa , Melody McWherter , Ping Liu , Dann Parker , Chun Sing Li , Qinghua Mao
IPC: C07D487/04 , C07D231/40 , C07D417/12 , C07D401/04 , C07D417/14 , C07D471/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D413/12 , C07D413/14 , C07D277/46 , C07D403/14
CPC classification number: C07D487/04 , C07D231/40 , C07D277/46 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
Abstract: The present invention is directed to substituted five membered heteroaryl benzamide compounds of formula (I) (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.
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