公开(公告)号：EP1086091A1

公开(公告)日：2001-03-28

申请号：EP99926095.3

申请日：1999-06-01

申请人： Merck & Co., Inc. (a New Jersey corp.)

发明人： YOUNG, Steven, D. ,  WAI, John, S. ,  EMBREY, Mark, W. ,  FISHER, Thorsten, E.

IPC分类号： C07D333/74 ,  C07D333/56 ,  C07D333/22 ,  C07D277/04 ,  C07D277/18 ,  A61K31/38 ,  A61K31/425

CPC分类号： C07D409/12 ,  C07D277/42 ,  C07D333/24 ,  C07D333/32 ,  C07D333/34 ,  C07D333/36 ,  C07D333/60 ,  C07D333/74

摘要： Sulfur-containing heteroaryl dioxo-butyric acid derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

公开(公告)号：EP0944388A2

公开(公告)日：1999-09-29

申请号：EP97921256.0

申请日：1997-03-27

申请人： MERCK & CO., INC.

发明人： ANTHONY, Neville, J. ,  DINSMORE, Christopher ,  GOMEZ, Robert, P. ,  HUTCHINSON, John, H. ,  WAI, John, S. ,  WILLIAMS, Theresa, M. ,  BELL, Ian, M. ,  EMBREY, Mark, W. ,  FISHER, Thorsten, E.

IPC分类号： A61K31 ,  A61P9 ,  A61P13 ,  A61P27 ,  A61P31 ,  A61P35 ,  A61P43 ,  C07D211 ,  C07D401 ,  C07D413

CPC分类号： C07D401/06 ,  C07D211/62 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14

摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

公开(公告)号：EP2044068A1

公开(公告)日：2009-04-08

申请号：EP07796862.6

申请日：2007-07-13

申请人： Merck & Co., Inc.

发明人： WILLIAMS, Peter, D. ,  VENKATRAMAN, Shankar ,  LANGFORD, H. Marie ,  KIM, Boyoung ,  BOOTH, Theresa, M. ,  GROBLER, Jay, A. ,  STAAS, Donnette ,  RUZEK, Rowena, D. ,  EMBREY, Mark, W. ,  WISCOUNT, Catherine, M. ,  LYLE, Terry, A.

IPC分类号： C07D471/04

CPC分类号： C07D471/04

摘要： 1-Hydroxy naphthyridine compounds (e.g., 1-hydroxy naphthyridin-2(1H)-one compounds of Formula I are inhibitors of HIV integrase and/or HIV RNase H and inhibitors of HIV replication: (I) wherein X and R1-R6 are as defined herein. The compounds are useful in the prophylaxis and treatment of infection by HIV and in the prophylaxis, 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 anti-HIV agents such as HIV antivirals, immunomodulators, antibiotics and vaccines.

公开(公告)号：EP1725102A1

公开(公告)日：2006-11-29

申请号：EP05724457.6

申请日：2005-03-04

申请人： Merck & Co., Inc.

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

IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/495 ,  A61K31/54 ,  A61K31/50 ,  A61K31/535 ,  C07D279/00 ,  C07D285/00 ,  C07D295/00 ,  C07D417/00 ,  C07D413/00

CPC分类号： C07D487/04 ,  A61K31/495 ,  A61K31/50 ,  A61K31/535 ,  A61K31/54 ,  A61K45/06 ,  A61K2300/00

摘要： 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, R1, R2, R3 and R4 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：EP1677599A1

公开(公告)日：2006-07-12

申请号：EP04795564.6

申请日：2004-10-18

申请人： Merck & Co., Inc.

发明人： 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分类号： A01N43/58 ,  A01N43/60 ,  A61K31/495 ,  A61K31/50 ,  C07D239/00 ,  C07D471/00 ,  C07D487/00 ,  C07D491/00

CPC分类号： C07D471/14

摘要： 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, R1, R2, R3, R4, R5, R6, R7 and R8 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：EP1196384A1

公开(公告)日：2002-04-17

申请号：EP00944756.6

申请日：2000-06-21

申请人： Merck & Co., Inc. ,  TULARIK, INC.

发明人： PAYNE, Linda, S. ,  TRAN, Lekhanh, O. ,  ZHUANG, Linghang, H. ,  YOUNG, Steven, D. ,  EGBERTSON, Melissa, S. ,  WAI, John, S. ,  EMBREY, Mark, W. ,  FISHER, Thorsten, E. ,  GUARE, James, P. ,  LANGFORD, H., Marie ,  MELAMED, Jeffrey, Y. ,  CLARK, David, L.

IPC分类号： C07D213/30 ,  C07D233/64 ,  C07D241/14 ,  C07D249/12 ,  C07D257/04 ,  C07D277/24 ,  C07D401/06 ,  C07D401/14 ,  C07D417/06 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/427 ,  A61K31/4402 ,  A61K31/4427 ,  A61K31/4436 ,  A61K31/4965 ,  A61K31/497

CPC分类号： C07D213/30 ,  C07D213/50 ,  C07D213/61 ,  C07D213/643 ,  C07D213/65 ,  C07D213/68 ,  C07D213/74 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D239/26 ,  C07D241/12 ,  C07D249/08 ,  C07D277/24 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/10 ,  C07D403/14 ,  C07D405/04 ,  C07D409/06 ,  C07D409/10 ,  C07D417/06 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D473/00 ,  C07D473/04 ,  C07D473/08

摘要： Certain 1-(aromatic- or heteroaromatic-substituted)-3-(heteroaromatic substituted)-1,3-propanediones are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

公开(公告)号：EP1087770A1

公开(公告)日：2001-04-04

申请号：EP99928592.7

申请日：1999-06-11

申请人： MERCK & CO., INC.

发明人： EMBREY, Mark, W. ,  PERLOW, Debra, S. ,  WAI, John, S. ,  HOFFMAN, Jacob, M.

IPC分类号： A61K31/53 ,  A61K31/54 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14

CPC分类号： C07D401/06 ,  C07D471/10 ,  C07D513/10

摘要： The present invention is directed to conformationally constrained compounds which 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.

摘要翻译： 本发明涉及抑制异戊二烯基蛋白转移酶和癌基因蛋白Ras的异戊烯化的构象约束化合物。 本发明还涉及含有本发明化合物的化学治疗组合物以及用于抑制异戊二烯基蛋白转移酶和癌基因蛋白Ras的异戊烯基化的方法。

公开(公告)号：EP1082121A1

公开(公告)日：2001-03-14

申请号：EP99926094.6

申请日：1999-06-01

申请人： MERCK & CO., INC. ,  TULARIK, INC.

发明人： YOUNG, Steven, D. ,  EGBERTSON, Melissa ,  PAYNE, Linda, S. ,  WAI, John, S. ,  FISHER, Thorsten, E. ,  GUARE, James, P., Jr. ,  EMBREY, Mark, W. ,  TRAN, Lee ,  ZHUANG, Linghang ,  VACCA, Joseph, P. ,  LANGFORD, Marie ,  MELAMED, Jeffrey ,  CLARK, David, L. ,  MEDINA, Julio, C. ,  JAEN, Juan

IPC分类号： A61K31/535

CPC分类号： C07D213/64 ,  C07C59/84 ,  C07C59/86 ,  C07C59/88 ,  C07C59/90 ,  C07C69/738 ,  C07C217/60 ,  C07C229/34 ,  C07C229/42 ,  C07C233/63 ,  C07C235/60 ,  C07C255/41 ,  C07C271/16 ,  C07C271/28 ,  C07C323/62 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2602/08 ,  C07C2602/10 ,  C07D209/12 ,  C07D241/12 ,  C07D253/08 ,  C07D263/58 ,  C07D295/088 ,  C07D295/155 ,  C07D295/192 ,  C07D333/22

摘要： Certain six-membered aromatic and heteroaromatic-dioxo-butyric acid derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.