公开(公告)号：EP1756114B1

公开(公告)日：2014-11-19

申请号：EP05743968.9

申请日：2005-05-03

申请人： Merck Sharp & Dohme Corp.

发明人： 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分类号： C07D487/14 ,  A61K31/5025 ,  A61K31/4985

CPC分类号： A61K31/5025 ,  C07D487/14 ,  Y02A50/414

摘要： 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 R1, R2, R3, R4, R5, R6 and R7 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.

公开(公告)号：EP2638042B1

公开(公告)日：2014-09-24

申请号：EP11787987.4

申请日：2011-11-10

申请人： Merck Sharp & Dohme Corp.

发明人： 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分类号： C07D471/10 ,  A61K31/519 ,  A61K31/437 ,  A61P9/08

CPC分类号： A61K31/4545 ,  A61K31/435 ,  A61K31/438 ,  C07D471/10 ,  C07D471/20

摘要： 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.

公开(公告)号：EP2271346A2

公开(公告)日：2011-01-12

申请号：EP09725978.2

申请日：2009-03-24

申请人： Merck Sharp & Dohme Corp.

发明人： 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分类号： A61K31/54 ,  A61K31/44 ,  C07D487/00 ,  C07D211/00

CPC分类号： C07D471/10 ,  C07D403/06 ,  C07D471/20 ,  C07D519/00

摘要： 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.

公开(公告)号：EP2637656B1

公开(公告)日：2016-12-14

申请号：EP11840630.5

申请日：2011-11-10

申请人： Merck Sharp & Dohme Corp.

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

IPC分类号： C07D471/04 ,  C07D487/04 ,  A61K31/40 ,  A61K31/445 ,  A61K31/506

CPC分类号： C07D471/04 ,  A61K31/506 ,  C07D487/04

公开(公告)号：EP2340025A1

公开(公告)日：2011-07-06

申请号：EP09818345.2

申请日：2009-09-29

申请人： Merck Sharp & Dohme Corp.

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

IPC分类号： A61K31/55

CPC分类号： C07D498/20 ,  C07D498/04 ,  C07D498/10

摘要： 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.

公开(公告)号：EP2340025B1

公开(公告)日：2014-10-15

申请号：EP09818345.2

申请日：2009-09-29

申请人： Merck Sharp & Dohme Corp.

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

IPC分类号： A61K31/55 ,  C07D498/10 ,  C07D498/20 ,  A61P29/00

CPC分类号： C07D498/20 ,  C07D498/04 ,  C07D498/10

公开(公告)号：EP2271346B1

公开(公告)日：2014-01-01

申请号：EP09725978.2

申请日：2009-03-24

申请人： Merck Sharp & Dohme Corp.

发明人： 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分类号： A61K31/54 ,  A61K31/44 ,  C07D487/00 ,  C07D211/00

CPC分类号： C07D471/10 ,  C07D403/06 ,  C07D471/20 ,  C07D519/00

公开(公告)号：EP2638042A1

公开(公告)日：2013-09-18

申请号：EP11787987.4

申请日：2011-11-10

申请人： Merck Sharp & Dohme Corp.

发明人： 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分类号： C07D471/10 ,  A61K31/519 ,  A61K31/437 ,  A61P9/08

CPC分类号： A61K31/4545 ,  A61K31/435 ,  A61K31/438 ,  C07D471/10 ,  C07D471/20

摘要： 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.

摘要翻译： 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：EP2637656A1

公开(公告)日：2013-09-18

申请号：EP11840630.5

申请日：2011-11-10

申请人： Merck Sharp & Dohme Corp.

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

IPC分类号： A61K31/40 ,  A61K31/445

CPC分类号： C07D471/04 ,  A61K31/506 ,  C07D487/04

摘要： The present invention is directed to piperidinone carboxamide indane derivatives 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.

公开(公告)号：EP2341919A1

公开(公告)日：2011-07-13

申请号：EP09819658.7

申请日：2009-09-30

申请人： Merck Sharp & Dohme Corp.

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

IPC分类号： A61K38/00

CPC分类号： A61K31/00 ,  C07D471/10 ,  C07D491/107 ,  C07D491/20

摘要： 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.

摘要翻译： 式（I）化合物：其中变量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和Y和Z如本文所述）可用作CGRP受体的拮抗剂，并且可用于治疗或预防其中涉及CGRP受体的疾病，例如头痛，并且特别 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其中涉及CGRP受体的疾病中的用途。