公开(公告)号：US08163752B2

公开(公告)日：2012-04-24

申请号：US12602681

申请日：2008-06-03

申请人： Ian Bell ,  Craig A. Stump

发明人： Ian Bell ,  Craig A. Stump

IPC分类号： C07D401/12 ,  A61K31/437 ,  A61P25/06

CPC分类号： C07D519/00 ,  C07D471/06 ,  C07D487/06

摘要： Compounds of formula I: wherein variables A1, A2, B, m, n, J, R4, G1, G2, G3 and Y are as described herein, which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.

摘要翻译： 式I化合物：其中变量A1，A2，B，m，n，J，R4，G1，G2，G3和Y如本文所述，其是CGRP受体的拮抗剂，其可用于治疗或预防疾病 其中涉及CGRP，如偏头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。

公开(公告)号：US06610722B2

公开(公告)日：2003-08-26

申请号：US09828325

申请日：2001-04-06

申请人： Craig A. Stump ,  Theresa M. Williams

发明人： Craig A. Stump ,  Theresa M. Williams

IPC分类号： C07D49808

CPC分类号： C07D498/18 ,  A61K31/337 ,  A61K31/415 ,  A61K38/00 ,  A61K41/00 ,  A61K45/06 ,  A61K49/0002 ,  C07D513/18 ,  C07D515/18 ,  C07K5/06139 ,  C07K5/06191 ,  A61K2300/00

摘要： The present invention is directed to peptidomimetic macrocyclic compounds that inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

公开(公告)号：US20170158698A1

公开(公告)日：2017-06-08

申请号：US15128782

申请日：2015-03-23

申请人： 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.

发明人： 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分类号： 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分类号： 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

摘要： 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.

公开(公告)号：US20170114056A1

公开(公告)日：2017-04-27

申请号：US15129206

申请日：2015-03-23

申请人： Helen MITCHELL ,  Mark E. FRALEY ,  Andrew J. COOKE ,  Craig A. STUMP ,  Yi Heng CHEN ,  Douglas C. BESHORE ,  Xu-Fank ZHANG ,  Casey C. MCCOMAS ,  Kathy SCHIRRIPA ,  Melody MCWHERTER ,  Swati P. MERCER ,  Keith P. MOORE ,  Ping LIU ,  Harold B. WOOD ,  Chun Sing LI ,  Qinghua MAO ,  Merck Sharp & Dohme Corp.

发明人： 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分类号： C07D471/04 ,  C07D513/04

CPC分类号： C07D403/12 ,  C07D401/12 ,  C07D403/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

摘要： 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.

公开(公告)号：US20160229850A1

公开(公告)日：2016-08-11

申请号：US15023145

申请日：2014-09-17

申请人： Andrew J. COOKE ,  Craig A. STUMP ,  Xu-Fang ZHANG ,  Chun Sing LI ,  Qinghua MAO ,  MERCK SHARP & DOHME CORP.

发明人： Andrew J. Cooke ,  Craig A. Stump ,  Xu-Fang Zhang ,  Chun Sing Li ,  Qinghua Mao

IPC分类号： C07D471/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D231/40 ,  C07D239/42 ,  C07D261/14

CPC分类号： C07D471/04 ,  C07D213/16 ,  C07D231/40 ,  C07D239/42 ,  C07D261/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

摘要： 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.

公开(公告)号：US08778957B2

公开(公告)日：2014-07-15

申请号：US13256354

申请日：2010-03-08

申请人： Craig A. Stump ,  Amy G. Quigley

发明人： Craig A. Stump ,  Amy G. Quigley

IPC分类号： C07D471/20 ,  A61K31/437

CPC分类号： C07D471/20 ,  C07D471/10 ,  C07D519/00

摘要： Compounds of Formula (I) (wherein variables A1, A2, A3, ring-B, m, n, J, E1, E2, E3, R5, RPG and Y are as described herein), which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and the use of these compounds and compositions in the prevention or treatment of diseases in which CGRP receptors are involved.

摘要翻译： 式（I）化合物（其中变量A1，A2，A3，环-B，m，n，J，E1，E2，E3，R5，RPG和Y如本文所述），其可用作CGRP受体的拮抗剂 并且可用于治疗或预防涉及CGRP受体的疾病，例如头痛，特别是偏头痛和丛集性头痛。 本发明还涉及包含式（I）化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP受体的疾病中的用途。

公开(公告)号：US20130210804A1

公开(公告)日：2013-08-15

申请号：US13880171

申请日：2011-10-20

申请人： Neville J. Anthony ,  Robert P. Gomez ,  Jing Li ,  Swati P. Mercer ,  Anthony J. Roecker ,  Craig A. Stump ,  Theresa M. Williams

发明人： Neville J. Anthony ,  Robert P. Gomez ,  Jing Li ,  Swati P. Mercer ,  Anthony J. Roecker ,  Craig A. Stump ,  Theresa M. Williams

IPC分类号： C07D513/04 ,  C07D498/04 ,  C07D471/14 ,  C07D471/04

CPC分类号： C07D513/04 ,  C07D471/04 ,  C07D471/14 ,  C07D498/04

摘要： The present invention is directed to tricyclic compounds which are positive allosteric modulators of metabotropic glutamate receptors, particularly the mGluR5 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. 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 metabotropic glutamate receptors are involved.

摘要翻译： 本发明涉及三环化合物，其是代谢型谷氨酸受体，特别是mGluR5受体的正性变构调节剂，其可用于治疗或预防与谷氨酸功能障碍相关的神经和精神病症以及涉及代谢型谷氨酸受体的疾病 。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。

公开(公告)号：US20120010193A1

公开(公告)日：2012-01-12

申请号：US13256354

申请日：2010-03-08

申请人： Craig A. Stump ,  Amy G. Quigley ,  Cory R. Theberge ,  Michael R. Wood

发明人： Craig A. Stump ,  Amy G. Quigley ,  Cory R. Theberge ,  Michael R. Wood

IPC分类号： A61K31/435 ,  C07D471/10 ,  C07D491/107 ,  C07D498/20 ,  A61K31/4375 ,  A61P25/06 ,  A61K31/536 ,  A61K31/537 ,  A61K31/551 ,  A61K31/553 ,  A61K31/5377 ,  C07D471/20 ,  A61K31/496

CPC分类号： C07D471/20 ,  C07D471/10 ,  C07D519/00

摘要： Compounds of Formula (I) (wherein variables A1, A2, A3, ring-B, m, n, J, E1, E2, E3, R5, RPG and Y are as described herein), which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and the use of these compounds and compositions in the prevention or treatment of diseases in which CGRP receptors are involved.

摘要翻译： 式（I）化合物（其中变量A1，A2，A3，环-B，m，n，J，E1，E2，E3，R5，RPG和Y如本文所述），其可用作CGRP受体的拮抗剂 并且可用于治疗或预防涉及CGRP受体的疾病，例如头痛，特别是偏头痛和丛集性头痛。 本发明还涉及包含式（I）化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP受体的疾病中的用途。

公开(公告)号：US20110224230A1

公开(公告)日：2011-09-15

申请号：US13119534

申请日：2009-09-10

申请人： Craig A. Stump

发明人： Craig A. Stump

IPC分类号： A61K31/497 ,  C07D417/14 ,  A61K31/427 ,  A61P25/00 ,  C07D401/14 ,  A61K31/4439 ,  C07D403/12 ,  C07D401/12

CPC分类号： C07D417/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D491/107

摘要： Compounds of formula (I): wherein variables B, G1, G2, G3, G4, Ea, Eb, Ec, A1, A2, A3, A4, R6 and RPG and Y are as described herein, which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.

摘要翻译： 式（I）化合物：其中变量B，G1，G2，G3，G4，Ea，Eb，Ec，A1，A2，A3，A4，R6和RPG和Y如本文所述，它们是CGRP受体的拮抗剂， 其可用于治疗或预防涉及CGRP的疾病，例如偏头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。

公开(公告)号：US20100137328A1

公开(公告)日：2010-06-03

申请号：US12602681

申请日：2008-06-03

申请人： Ian Bell ,  Craig A. Stump

发明人： Ian Bell ,  Craig A. Stump

IPC分类号： A61K31/4985 ,  C07D221/20 ,  A61K31/438 ,  C07D245/04 ,  C07D241/52 ,  A61P25/06

CPC分类号： C07D519/00 ,  C07D471/06 ,  C07D487/06

摘要： Compounds of formula I: wherein variables A1, A2, B, m, n, J, R4, G1, G2, G3 and Y are as described herein, which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.

摘要翻译： 式I化合物：其中变量A1，A2，B，m，n，J，R4，G1，G2，G3和Y如本文所述，其是CGRP受体的拮抗剂，其可用于治疗或预防疾病 其中涉及CGRP，如偏头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。