公开(公告)号：WO2009120652A3

公开(公告)日：2009-12-30

申请号：PCT/US2009038013

申请日：2009-03-24

Applicant: MERCK & CO INC ,  SELNICK HAROLD G ,  BELL IAN M ,  MCWHERTER MELODY ,  STAAS DONNETTE D ,  STACHEL SHAWN J ,  STEELE THOMAS ,  STUMP CRAIG ,  WOOD MICHAEL R ,  ZARTMAN C BLAIR

Inventor： SELNICK HAROLD G ,  BELL IAN M ,  MCWHERTER MELODY ,  STAAS DONNETTE D ,  STACHEL SHAWN J ,  STEELE THOMAS ,  STUMP CRAIG ,  WOOD MICHAEL R ,  ZARTMAN C BLAIR

IPC: A61K31/54 ,  A61K31/44 ,  C07D211/00 ,  C07D487/00

CPC classification number: C07D471/10 ,  C07D403/06 ,  C07D471/20 ,  C07D519/00

Abstract: The present invention is directed to compounds of the formula (I) : (wherein variables A1, A2, A3, A4, A5, A6, A7, A8, G1, G2, G3, G4, J, Q, Ea, Eb, Ec, R6, R7, 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 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.

Abstract translation: 本发明涉及式（I）化合物：（其中变量A1，A2，A3，A4，A5，A6，A7，A8，G1，G2，G3，G4，J，Q，Ea，Eb，Ec ，R6，R7，RPG和Y如本文所述），它们是CGRP受体的拮抗剂并且可用于治疗或预防其中涉及CGRP的疾病，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的此类疾病中的用途。

公开(公告)号：WO2012064910A1

公开(公告)日：2012-05-18

申请号：PCT/US2011/060081

申请日：2011-11-10

Applicant: MERCK SHARP & DOHME CORP. ,  BELL, Ian, M. ,  FRALEY, Mark, E. ,  GALLICCHIO, Steven, N. ,  GINNETTI, Anthony ,  MITCHELL, Helen, J. ,  PAONE, Daniel, V. ,  STAAS, Donnette, D. ,  WANG, Cheng ,  ZARTMAN, C. Blair ,  STEVENSON, Heather, E.

Inventor： BELL, Ian, M. ,  FRALEY, Mark, E. ,  GALLICCHIO, Steven, N. ,  GINNETTI, Anthony ,  MITCHELL, Helen, J. ,  PAONE, Daniel, V. ,  STAAS, Donnette, D. ,  WANG, Cheng ,  ZARTMAN, C. Blair ,  STEVENSON, Heather, E.

IPC: C07D471/10 ,  A61K31/519 ,  A61K31/437 ,  A61P9/08

CPC classification number: A61K31/4545 ,  A61K31/435 ,  A61K31/438 ,  C07D471/10 ,  C07D471/20

Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives of formula I which are antagonists of CGRP receptors and 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.

Abstract translation: 本发明涉及作为CGRP受体的拮抗剂的式I的哌啶酮羧酰胺氮杂茚衍生物，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：WO2010042356A1

公开(公告)日：2010-04-15

申请号：PCT/US2009/058925

申请日：2009-09-30

Applicant: MERCK SHARP & DOHME CORP. ,  STAAS, Donnette, D. ,  BELL, Ian, M. ,  WOOD, Michael, R.

Inventor： STAAS, Donnette, D. ,  BELL, Ian, M. ,  WOOD, Michael, R.

IPC: A61K38/00

CPC classification number: A61K31/00 ,  C07D471/10 ,  C07D491/107 ,  C07D491/20

Abstract: Compounds of Formula (I): (wherein variables A 1 , A 2 , A 3 A 4 A 5 , A 6 , A 7 , A 8 , J, Q, R 4 , E a , E b , E c , R 6 , R 7 , R e , R f , R PG andY and Z are as described herein) 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 these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP receptors are involved.

Abstract translation: 式（I）的化合物（其中变量A1，A2，A3 A4 A5，A6，A7，A8，J，Q，R4，Ea，Eb，Ec，R6，R7，Re，Rf，RPG和Y和Z分别为 可用作CGRP受体的拮抗剂，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受体的疾病中的用途。

公开(公告)号：WO2010039673A1

公开(公告)日：2010-04-08

申请号：PCT/US2009/058711

申请日：2009-09-29

Applicant: MERCK SHARP & DOHME CORP. ,  STAAS, Donnette, D. ,  BELL, Ian, M. ,  SELNICK, Harold, G.

Inventor： STAAS, Donnette, D. ,  BELL, Ian, M. ,  SELNICK, Harold, G.

IPC: A61K31/55

CPC classification number: C07D498/20 ,  C07D498/04 ,  C07D498/10

Abstract: Compounds of Formula (I), (wherein variables A 1 , A 2 , A 3 , A 4 , A 5 , A 6 , A 7 , A 8 , L, J, Q, R 4 , E a , E b , E c , R 6 , R 7 , R e , R f , R PG , W, Y and Z are as described herein) 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 these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP receptors are involved.

Abstract translation: 式（I）化合物（其中变量A1，A2，A3，A4，A5，A6，A7，A8，L，J，Q，R4，Ea，Eb，Ec，R6，R7，Re，Rf， W，Y和Z如本文所述）可用作CGRP受体的拮抗剂，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受体的疾病中的用途。

公开(公告)号：WO2005041664A1

公开(公告)日：2005-05-12

申请号：PCT/US2004/034420

申请日：2004-10-18

Applicant: MERCK & CO., INC. ,  WAI, John, S. ,  FISHER, Thorsten, E. ,  ZHUANG, Linghang ,  STAAS, Donnette, D. ,  LYLE, Terry, A. ,  KIM, Boyoung ,  EMBREY, Mark, W. ,  WISCOUNT, Catherine, M. ,  TRAN, Lekhanh, O. ,  EGBERTSON, Melissa ,  SAVAGE, Kelly, L.

Inventor： WAI, John, S. ,  FISHER, Thorsten, E. ,  ZHUANG, Linghang ,  STAAS, Donnette, D. ,  LYLE, Terry, A. ,  KIM, Boyoung ,  EMBREY, Mark, W. ,  WISCOUNT, Catherine, M. ,  TRAN, Lekhanh, O. ,  EGBERTSON, Melissa ,  SAVAGE, Kelly, L.

IPC: A01N43/58

CPC classification number: C07D471/14

Abstract: Hydroxy-substituted pyridopyrrolopyrazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I): (I) wherein a, b, A, B, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Abstract translation: 羟基取代的吡啶并吡咯并吡嗪二酮化合物是HIV整合酶和HIV复制抑制剂的抑制剂。 在一个实施方案中，二酮化合物具有式（I）：（I）其中a，b，A，B，R 1，R 2，R 3，R 4，R 5， R 6，R 7和R 8如本文所定义。 这些化合物可用于预防和治疗艾滋病毒感染以及预防，延迟艾滋病的发病和治疗。 这些化合物被用作抗HIV感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 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：WO2009120652A2

公开(公告)日：2009-10-01

申请号：PCT/US2009/038013

申请日：2009-03-24

Applicant: MERCK & CO., INC. ,  SELNICK, Harold, G. ,  BELL, Ian, M. ,  MCWHERTER, Melody ,  STAAS, Donnette, D. ,  STACHEL, Shawn, J. ,  STEELE, Thomas ,  STUMP, Craig ,  WOOD, Michael, R. ,  ZARTMAN, C., Blair

Inventor： SELNICK, Harold, G. ,  BELL, Ian, M. ,  MCWHERTER, Melody ,  STAAS, Donnette, D. ,  STACHEL, Shawn, J. ,  STEELE, Thomas ,  STUMP, Craig ,  WOOD, Michael, R. ,  ZARTMAN, C., Blair

IPC: C07D491/10

CPC classification number: C07D471/10 ,  C07D403/06 ,  C07D471/20 ,  C07D519/00

Abstract: The present invention is directed to compounds of the formula (I) : (wherein variables A 1 , A 2 , A 3 , A 4 , A 5 , A 6 , A 7 , A 8 , G 1 , G 2 , G 3 , G 4 , J, Q, E a , E b , E c , R 6 , R 7 , R PG 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 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.

Abstract translation: 本发明涉及式（I）的化合物：（其中变量A1，A2，A3，A4，A5，A6，A7，A8，G1，G2，G3，G4，J，Q，Ea，Eb，Ec ，R6，R7，RPG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：WO2005110414A2

公开(公告)日：2005-11-24

申请号：PCT/US2005/015200

申请日：2005-05-03

Applicant: MERCK & CO., INC. ,  WAI, John, S. ,  VACCA, Joseph, P. ,  ZHUANG, Linghang ,  KIM, Boyoung ,  LYLE, Terry, A. ,  WISCOUNT, Catherine, M. ,  EGBERTSON, Melissa, S. ,  NEILSON, Lou Anne ,  EMBREY, Mark ,  FISHER, Thorsten, E. ,  STAAS, Donnette, D.

Inventor： WAI, John, S. ,  VACCA, Joseph, P. ,  ZHUANG, Linghang ,  KIM, Boyoung ,  LYLE, Terry, A. ,  WISCOUNT, Catherine, M. ,  EGBERTSON, Melissa, S. ,  NEILSON, Lou Anne ,  EMBREY, Mark ,  FISHER, Thorsten, E. ,  STAAS, Donnette, D.

IPC: A61K31/502

CPC classification number: A61K31/5025 ,  C07D487/14 ,  Y02A50/414

Abstract: Hydroxy-substituted pyrazinopyrrolopyridazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Abstract translation: 羟基取代的吡嗪并吡咯并哒嗪二酮化合物是HIV整合酶和HIV复制抑制剂的抑制剂。 在一个实施方案中，二酮化合物具有式（I），其中R 1，R 2，R 3，R 4，R 5，R 6和R 7定义 于此。 这些化合物可用于预防和治疗艾滋病毒感染以及预防，延迟艾滋病的发病和治疗。 这些化合物被用作抗HIV感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 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：WO2004032834A3

公开(公告)日：2004-06-10

申请号：PCT/US0330867

申请日：2003-09-30

Applicant: MERCK & CO INC ,  STAAS DONNETTE D ,  LYLE TERRY A ,  WILLIAMS PETER D ,  SANDERSON PHILIP E J

Inventor： STAAS DONNETTE D ,  LYLE TERRY A ,  WILLIAMS PETER D ,  SANDERSON PHILIP E J

IPC: C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D417/12

CPC classification number: C07D417/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12

Abstract: Compounds of the invention (Formula I) are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: I.The compounds are useful for preventing or treating unstable angina, refractory angina, myocardial infarction, transient ischemic attacks, atrial fibrillation, thrombotic stroke, embolic stroke, deep vein thrombosis, disseminated intravascular coagulation, ocular build up of fibrin, and reocclusion or restenosis of recanalized vessels, in a mammal.

Abstract translation: 本发明的化合物（式I）可用于抑制具有以下结构的凝血酶和相关的血栓形成闭塞：I，该化合物可用于预防或治疗不稳定心绞痛，难治性心绞痛，心肌梗塞，短暂性脑缺血发作，心房纤颤，血栓形成中风 ，栓塞性中风，深静脉血栓形成，播散性血管内凝血，纤维蛋白的眼部积聚以及再通血管的再闭塞或再狭窄。

公开(公告)号：WO2002064559A3

公开(公告)日：2002-08-22

申请号：PCT/US2002/004658

申请日：2002-02-05

Applicant: MERCK & CO., INC. ,  SELNICK, Harold, G. ,  YOUNG, Mary Beth ,  NANTERMET, Philippe, G. ,  BARROW, James, C. ,  WILLIAMS, Peter, D. ,  LYLE, Terry, A. ,  STAAS, Donnette, D. ,  STAUFFER, Kenneth, J. ,  SANDERSON, Philip, E.

Inventor： SELNICK, Harold, G. ,  YOUNG, Mary Beth ,  NANTERMET, Philippe, G. ,  BARROW, James, C. ,  WILLIAMS, Peter, D. ,  LYLE, Terry, A. ,  STAAS, Donnette, D. ,  STAUFFER, Kenneth, J. ,  SANDERSON, Philip, E.

IPC: C07D403/12 ,  A61K31/41

Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure Formula (I): wherein u is CH or N; Q is 1)-N(R 25 )CH(R 30 )- wherein the nitrogen atom is attached to R 1 , and R 25 and R 30 are independently selected from the group consisting of hydrogen, C 3-6 cycloalkyl, and C 1-6 alkyl, or 2) wherein the nitrogen atom is attached to R 1 , and m is 0, 1, or 2.

公开(公告)号：WO2005092099A1

公开(公告)日：2005-10-06

申请号：PCT/US2005/006916

申请日：2005-03-04

Applicant: MERCK & CO., INC. ,  WILLIAMS, Peter, D. ,  WAI, John, S. ,  EMBREY, Mark, W. ,  STAAS, Donnette, D. ,  ZHUANG, Linghang ,  LANGFORD, H., Marie

Inventor： WILLIAMS, Peter, D. ,  WAI, John, S. ,  EMBREY, Mark, W. ,  STAAS, Donnette, D. ,  ZHUANG, Linghang ,  LANGFORD, H., Marie

IPC: A01N43/58

CPC classification number: C07D487/04 ,  A61K31/495 ,  A61K31/50 ,  A61K31/535 ,  A61K31/54 ,  A61K45/06 ,  A61K2300/00

Abstract: Bicyclic uracils and related compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the compounds are of Formula (I) wherein a, b, Y, R 1 , R 2 , R 3 and R 4 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Abstract translation: 双环尿嘧啶和相关化合物是HIV整合酶和HIV复制抑制剂的抑制剂。 在一个实施方案中，化合物为式（I），其中a，b，Y，R 1，R 2，R 3和R 4在本文中定义。 这些化合物可用于预防和治疗艾滋病毒感染以及预防，延迟艾滋病的发病和治疗。 这些化合物被用作抗HIV感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 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。