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1. 发明申请

WO2020092667A1 2-AMINO-N-HETEROARYL-NICOTINAMIDES AS NAV1.8 INHIBITORS 审中-公开
公开(公告)号：WO2020092667A1
公开(公告)日：2020-05-07
申请号：PCT/US2019/058999
申请日：2019-10-31
申请人： MERCK SHARP & DOHME CORP. , ARASAPPAN, Ashok , BELL, Ian, M. , BRESLIN, Michael, J. , BUNGARD, Christopher James , BURGEY, Christopher, S. , CHOBANIAN, Harry, R. , COX, Jason, M. , GINNETTI, Anthony, T. , GUIADEEN, Deodial Guy , JONES, Kristen, L. G. , LAYTON, Mark, E. , LIU, Hong , LIU, Jian , PERKINS, James, J. , STACHEL, Shawn, J. , SUEN-LAI, Linda, M. , WU, Zhe
发明人： ARASAPPAN, Ashok , BELL, Ian, M. , BRESLIN, Michael, J. , BUNGARD, Christopher James , BURGEY, Christopher, S. , CHOBANIAN, Harry, R. , COX, Jason, M. , GINNETTI, Anthony, T. , GUIADEEN, Deodial Guy , JONES, Kristen, L. G. , LAYTON, Mark, E. , LIU, Hong , LIU, Jian , PERKINS, James, J. , STACHEL, Shawn, J. , SUEN-LAI, Linda, M. , WU, Zhe
IPC分类号： C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D491/04 , C07D495/04 , A61P29/00 , A61K31/4439 , A61K31/444 , C07D409/14
摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Nav1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Nav1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.

2. 发明申请

WO2021257418A1 2-OXO-OXAZOLIDINE-5-CARBOXAMIDES AS NAV1.8 INHIBITORS 审中-公开
公开(公告)号：WO2021257418A1
公开(公告)日：2021-12-23
申请号：PCT/US2021/037157
申请日：2021-06-14
申请人： MERCK SHARP & DOHME CORP. , ARASAPPAN, Ashok , BELL, Ian, M. , BUNGARD, Christopher James , BURGEY, Christopher, S. , COX, Jason, M. , GUIADEEN, Deodial Guy , KELLY, Michael, J., III , LAYTON, Mark, E. , LIU, Hong , LIU, Jian , OLSEN, James, T. , PERKINS, James, J. , SCHUBERT, Jeffrey, W. , SHAH, Akshay, A. , STACHEL, Shawn, J. , VANHEYST, Michael, D. , WU, Zhe
发明人： ARASAPPAN, Ashok , BELL, Ian, M. , BUNGARD, Christopher James , BURGEY, Christopher, S. , COX, Jason, M. , GUIADEEN, Deodial Guy , KELLY, Michael, J., III , LAYTON, Mark, E. , LIU, Hong , LIU, Jian , OLSEN, James, T. , PERKINS, James, J. , SCHUBERT, Jeffrey, W. , SHAH, Akshay, A. , STACHEL, Shawn, J. , VANHEYST, Michael, D. , WU, Zhe
IPC分类号： A61K31/4045 , A61K31/4155 , A61K31/4178
摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Nav1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Nav1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.

3. 发明申请

WO2020092187A1 2-AMINO-N-PHENYL-NICOTINAMIDES AS NAV1.8 INHIBITORS 审中-公开
公开(公告)号：WO2020092187A1
公开(公告)日：2020-05-07
申请号：PCT/US2019/058251
申请日：2019-10-28
申请人： MERCK SHARP & DOHME CORP. , BRESLIN, Michael, J. , BUNGARD, Christopher James , CHOBANIAN, Harry, R. , JONES, Kristen, L. G. , LAYTON, Mark, E. , LIU, Jian , PERKINS, James, J. , SCHUBERT, Jeffrey William , STACHEL, Shawn, J. , SUEN-LAI, Linda, M. , WU, Zhe
发明人： BRESLIN, Michael, J. , BUNGARD, Christopher James , CHOBANIAN, Harry, R. , JONES, Kristen, L. G. , LAYTON, Mark, E. , LIU, Jian , PERKINS, James, J. , SCHUBERT, Jeffrey William , STACHEL, Shawn, J. , SUEN-LAI, Linda, M. , WU, Zhe
IPC分类号： A61K31/4425 , A61K31/167 , A61K31/44 , C07D213/06 , C07D213/20
摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Na v 1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Na v 1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.

4. 发明申请

WO2021257490A1 2-OXOIMIDAZOLIDINE-4-CARBOXAMIDES AS NAV1.8 INHIBITORS 审中-公开
公开(公告)号：WO2021257490A1
公开(公告)日：2021-12-23
申请号：PCT/US2021/037303
申请日：2021-06-15
申请人： MERCK SHARP & DOHME CORP. , ARASAPPAN, Ashok , BELL, Ian, M. , BUNGARD, Christopher, James , BURGEY, Christopher, S. , COX, Jason, M. , KELLY, Michael, J., III , LAYTON, Mark, E. , LIU, Hong , LIU, Jian , PERKINS, James, J. , SHAH, Akshay, A. , VANHEYST, Michael, David , WU, Zhe
发明人： ARASAPPAN, Ashok , BELL, Ian, M. , BUNGARD, Christopher, James , BURGEY, Christopher, S. , COX, Jason, M. , KELLY, Michael, J., III , LAYTON, Mark, E. , LIU, Hong , LIU, Jian , PERKINS, James, J. , SHAH, Akshay, A. , VANHEYST, Michael, David , WU, Zhe
IPC分类号： C07D233/32 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D513/04 , C07D401/14 , C07D471/08
摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Nav1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Nav1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.

5. 发明申请

WO2016032921A1 TETRAHYDRONAPHTHYRIDINE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE 审中-公开
标题翻译：作为mGluR2阴性单体调节剂，组合物及其用途的四氢萘啶衍生物
公开(公告)号：WO2016032921A1
公开(公告)日：2016-03-03
申请号：PCT/US2015/046458
申请日：2015-08-24
申请人： MERCK SHARP & DOHME CORP. , MERCK CANADA INC. , ARASAPPAN, Ashok , BUNGARD, Christopher James , FRIE, Jessica, L. , HAN, Yongxin , HOYT, Scott, B. , MANLEY, Peter, J. , MEISSNER, Robert, S. , PERKINS, James, J. , SEBHAT, Iyassu, K. , WILKENING, Robert, R. , LEAVITT, Kenneth, J.
发明人： ARASAPPAN, Ashok , BUNGARD, Christopher James , FRIE, Jessica, L. , HAN, Yongxin , HOYT, Scott, B. , MANLEY, Peter, J. , MEISSNER, Robert, S. , PERKINS, James, J. , SEBHAT, Iyassu, K. , WILKENING, Robert, R. , LEAVITT, Kenneth, J.
IPC分类号： A61K31/4375
CPC分类号： C07D471/04 , A61K31/4375
摘要： The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , L, X 1 , X 2 , and X 3 , are as defined herein. The compounds of the invention, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising them, are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a person in need thereof for diseases or disorders in which the mGluR2-NAM receptor plays a causative role, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders.
摘要翻译：本发明提供式（I）的喹啉羧酰胺和喹啉腈化合物或其药学上可接受的盐，其中R1，R2，L，X1，X2和X3如本文所定义。本发明的化合物及其药学上可接受的盐和包含它们的药物组合物可用作非竞争性mGluR2拮抗剂或mGluR2负变构调节剂（NAM），并且可用于治疗有需要的人的方法其中mGluR2-NAM受体起作用的疾病或障碍，例如阿尔茨海默病，认知障碍，精神分裂症和其他情绪障碍，疼痛障碍和睡眠障碍。

6. 发明申请

WO2011053574A1 2- [1-PHENYL-5-HYDROXY-4a-SUBSTITUTED-HEXAHYDROCYCLOPENTA [F] INDAZOL-5-YL] ETHYL PHENYL DERIVATIVES AS GLUCOCORTICOID RECEPTOR LIGANDS 审中-公开
标题翻译： 2- [1-苯基-5-羟基-4a-取代的六氢环戊二烯并[F]吲哚-5-基]乙基苯基衍生物作为葡萄糖激动剂受体配体
公开(公告)号：WO2011053574A1
公开(公告)日：2011-05-05
申请号：PCT/US2010/054052
申请日：2010-10-26
申请人： MERCK SHARP & DOHME CORP. , BUNGARD, Christopher, James , PERKINS, James, J. , MANIKOWSKI, Jesse, J. , DE LEON, Pablo , MEISSNER, Robert, S.
发明人： BUNGARD, Christopher, James , PERKINS, James, J. , MANIKOWSKI, Jesse, J. , DE LEON, Pablo , MEISSNER, Robert, S.
IPC分类号： A01N43/38 , A61K31/40
CPC分类号： C07D401/06 , C07D231/54 , C07D401/04
摘要： The present invention encompasses compounds of Formula I: or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.
摘要翻译：本发明包括式I化合物或其药学上可接受的盐或水合物，其可用作治疗各种自身免疫性和炎性疾病或病症的选择性糖皮质激素受体配体。还包括药物组合物和使用方法。

7. 发明申请

WO2013066736A1 QUINOLINE CARBOXAMIDE AND QUINOLINE CARBONITRILE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE 审中-公开
标题翻译：喹啉羧酰胺和喹啉衍生物作为mGluR2负离子调节剂，组合物及其用途
公开(公告)号：WO2013066736A1
公开(公告)日：2013-05-10
申请号：PCT/US2012/062027
申请日：2012-10-26
申请人： MERCK SHARP & DOHME CORP. , BUNGARD, Christopher James , CONVERSO, Antonella , DE LEON, Pablo , HANNEY, Barbara , HARTINGH, Timothy John , MANIKOWSKI, Jesse Josef , MANLEY, Peter, J. , MEISSNER, Robert , MENG, Zhaoyang , PERKINS, James, J. , RUDD, Michael, T. , SHU, Youheng
发明人： BUNGARD, Christopher James , CONVERSO, Antonella , DE LEON, Pablo , HANNEY, Barbara , HARTINGH, Timothy John , MANIKOWSKI, Jesse Josef , MANLEY, Peter, J. , MEISSNER, Robert , MENG, Zhaoyang , PERKINS, James, J. , RUDD, Michael, T. , SHU, Youheng
IPC分类号： A01N43/42
CPC分类号： C07D413/14 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/541 , C07D215/48 , C07D401/04 , C07D401/06 , C07D401/14 , C07D409/04 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04 , C07D491/10
摘要： The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, R Q , -L-, R 1 , n, R 2 , and R 3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or more additional active ingredients), and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.
摘要翻译：本发明提供式（I）的喹啉羧酰胺和喹啉腈化合物，其中环A，RQ，-L-，R1，n，R2和R3如本文所定义。本发明的化合物可用作非竞争性mGluR2拮抗剂或mGluR2负变构调节剂（NAM），以及用于治疗患有（其中涉及mGluR2-NAM受体的疾病或病症）的患者（优选人）的方法，例如作为阿尔茨海默病，认知障碍，精神分裂症和其他情绪障碍，疼痛障碍和睡眠障碍，通过向患者施用治疗有效量的本发明化合物或其药学上可接受的盐。本发明还涉及包含本发明化合物或其药学上可接受的盐（任选与一种或多种另外的活性成分组合）和药学上可接受的载体的药物组合物，以及该化合物和药物组合物的用途的本发明治疗这些疾病。

9. 发明授权

EP1755572B1 N- (2-BENZYL) -2-PHENYLBUTANAMIDES AS ANDROGEN RECEPTOR MODULATORS 有权
标题翻译： N-（2-苄氧基）-2-苯基丁酰胺和去氧肾上腺素
公开(公告)号：EP1755572B1
公开(公告)日：2012-02-15
申请号：EP05756622.6
申请日：2005-06-03
申请人： Merck Sharp & Dohme Corp.
发明人： HANNEY, Barbara , KIM, Yuntae , KROUT, Michael, R. , MEISSNER, Robert, S. , MITCHELL, Helen, J. , MUSSELMAN, Jeffrey , PERKINS, James, J. , WANG, Jiabing
IPC分类号： C07D213/61 , C07C235/06 , C07C233/13 , A61K31/165 , A61P5/26
CPC分类号： C07D295/205 , C07C233/13 , C07C235/34 , C07C255/60 , C07C271/12 , C07C271/22 , C07C2601/02 , C07D213/61 , C07D213/73
摘要： Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), abdominal adiposity, metabolic syndrome, type II diabetes, cancer cachexia, Alzhheiner’s disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.
摘要翻译：结构式I的化合物是以组织选择性方式的雄激素受体（AR）的调节剂。这些化合物可用于增强减弱的肌肉紧张度和治疗由雄激素缺乏引起的疾病或可由雄激素给药改善的疾病，包括骨质疏松症，骨质减少症，糖皮质激素诱导的骨质疏松症，牙周病，骨折，骨重建后的骨损伤手术，肌营养不良，虚弱，衰老皮肤，男性性腺机能减退，女性绝经后症状，动脉粥样硬化，高胆固醇血症，高脂血症，肥胖，再生障碍性贫血和其他造血障碍，炎症性关节炎和关节修复，艾滋病毒消耗，前列腺癌，良性前列腺增生），腹部肥胖，代谢综合征，II型糖尿病，癌症恶病质，阿尔茨海默病，肌营养不良症，认知衰退，性功能障碍，睡眠呼吸暂停，抑郁症，卵巢早衰，自身免疫性疾病，单独或与其他活性剂组合。

10. 发明授权

EP1940407B1 N-(4-OXO-3,4-DIHYDROQUINAZOLIN-2-YL)BUTANAMIDES AS ANDROGEN RECEPTOR MODULATORS 有权
标题翻译： N-（4-氧代-3,4-二氢喹唑啉-2-基）丁酰胺ALS雄激素受体调节
公开(公告)号：EP1940407B1
公开(公告)日：2010-11-10
申请号：EP06825101.6
申请日：2006-09-22
申请人： Merck Sharp & Dohme Corp.
发明人： HANNEY, Barbara , KIM, Yuntae , MITCHELL, Helen, J. , MUSSELMAN, Jeffrey, D. , PERKINS, James, J.
IPC分类号： A61K31/517 , C07D239/90 , C07D409/12 , A61P15/00 , A61P19/00 , A61P25/00 , A61P35/00 , A61P3/00 , A61P5/00
CPC分类号： C07D403/06 , C07D239/90 , C07D409/12
摘要： The invention relates to substituted N-(4-oxo-3,4-dihydroquinazolin-2-yl)butanamid derivatives which modulate androgen receptors to treat conditions such as: osteoporosis, peridontal disease, bone fracture, frailty, and sarcopenia.

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