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公开(公告)号：EP1910360B1
公开(公告)日：2010-03-03
申请号：EP06787590.6
申请日：2006-07-17
申请人： Merck & Co., Inc.
发明人： SAGGAR, Sandeep, A. , SISKO, John, T. , TUCKER, Thomas, J. , TYNEBOR, Robert, M. , SU, Dai-Shi , ANTHONY, Neville, J.
IPC分类号： C07D471/04 , A61P31/12 , A61K31/437
CPC分类号： C07C311/46 , C07C255/54 , C07C255/60 , C07C307/06 , C07C317/40 , C07C2601/14 , C07D209/08 , C07D213/65 , C07D213/75 , C07D231/56 , C07D235/06 , C07D249/04 , C07D249/06 , C07D263/56 , C07D271/06 , C07D271/10 , C07D271/107 , C07D277/64 , C07D333/48 , C07D471/04
摘要： Compounds having the structure: are HIV reverse transcriptase inhibitors, wherein A, X, Y, Z, R1 and R2 are defined herein. The compounds and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
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公开(公告)号：EP0858262B1
公开(公告)日：2002-12-04
申请号：EP96936804.2
申请日：1996-10-21
申请人： MERCK & CO., INC.
发明人： LUMMA, William, C. , TUCKER, Thomas, J. , WITHERUP, Keith, M. , BRADY, Stephen, F. , WHITTER, Willie, L. , VACCA, Joseph, P. , COBURN, Craig , SHAFER, Jules, A.
IPC分类号： A01N43/34 , A01N43/64 , A01N43/82 , A61K31/165 , C07D207/08
CPC分类号： C07K5/06191 , A61K38/00 , C07D207/16 , C07K5/0222 , C07K5/06078 , C07K5/06139
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公开(公告)号：EP1158982A2
公开(公告)日：2001-12-05
申请号：EP00912071.8
申请日：2000-03-01
申请人： Merck & Co., Inc.
发明人： HARTMAN, George, D. , LUMMA, William, C., Jr. , SISKO, John, T. , SMITH, Anthony, M. , TUCKER, Thomas, J. , BERGMAN, Jeffrey, M
IPC分类号： A61K31/495 , A61K31/496 , A61K31/551 , C07D223/08 , C07D241/04 , C07D295/04 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14
CPC分类号： C07D233/64
摘要： The present invention comprises piperazine-containing compounds which inhibit prenyl-protein transferases, including farnesyl-protein transferase and geranylgeranyl-protein transferase type I. Such therapeutic compounds are useful in the treatment of cancer.
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公开(公告)号：EP1558609A2
公开(公告)日：2005-08-03
申请号：EP03779322.1
申请日：2003-10-24
申请人： Merck & Co., Inc.
IPC分类号： C07D417/12 , C07D417/14 , A61K31/427
CPC分类号： C07D417/12 , C07D417/14
摘要： The present invention relates to compounds which inhibit, regulate and/or modulate kinase signal transduction, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, retinal ischemia, macular edema, diabetic retinopathy, inflammatory diseases, and the like in mammals.
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公开(公告)号：EP1341540A2
公开(公告)日：2003-09-10
申请号：EP01991965.3
申请日：2001-11-30
申请人： Merck & Co., Inc.
发明人： BILODEAU, Mark, T. , HARTMAN, George, D. , HOFFMAN, Jacob, M., Jr. , LUMMA, William, C., Jr. , MANLEY, Peter, J. , RODMAN, Leonard , SISKO, John, T. , SMITH, Anthony, M. , TUCKER, Thomas, J.
IPC分类号： A61K31/5355 , A61K31/495 , A61K31/505 , A61K31/506 , A61P7/00
CPC分类号： C07D403/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D487/04 , C07D487/08 , C07D491/08
摘要： The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
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公开(公告)号：EP1165082A1
公开(公告)日：2002-01-02
申请号：EP00910377.1
申请日：2000-03-01
申请人： Merck & Co., Inc.
发明人： HARTMAN, George, D. , LUMMA, William, C., Jr. , SISKO, John, T. , SMITH, Anthony, M. , TUCKER, Thomas, J. , STOKKER, Gerald, E.
IPC分类号： A61K31/495 , A61K31/496 , A61K31/499 , A61K31/551 , C07D403/04 , C07D403/06
CPC分类号： C07D233/64 , C07D401/12 , C07D405/12
摘要： The present invention comprises piperazine-containing compounds which inhibit prenyl-protein transferases, including farnesyl-protein transferase and geranylgeranyl-protein transferase type I. Such therapeutic compounds are useful in the treatment of cancer.
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公开(公告)号：EP1019391A1
公开(公告)日：2000-07-19
申请号：EP98952003.6
申请日：1998-10-01
申请人： Merck & Co., Inc.
发明人： DESOLMS, S., Jane , SHAW, Anthony, W. , LUMMA, William, C., Jr. , SISKO, John, T. , TUCKER, Thomas, J.
IPC分类号： C07D401/02 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , A61K31/415 , A61K31/44 , A61K31/445
CPC分类号： C07D401/06
摘要： The present invention is directed to compounds which inhibit prenyl-protein transferase (FTase) 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.
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公开(公告)号：EP0858262A1
公开(公告)日：1998-08-19
申请号：EP96936804.0
申请日：1996-10-21
申请人： MERCK & CO., INC.
发明人： LUMMA, William, C. , TUCKER, Thomas, J. , WITHERUP, Keith, M. , BRADY, Stephen, F. , WHITTER, Willie, L. , VACCA, Joseph, P. , COBURN, Craig , SHAFER, Jules, A.
CPC分类号： C07K5/06191 , A61K38/00 , C07D207/16 , C07K5/0222 , C07K5/06078 , C07K5/06139
摘要： A compound which inhibits human thrombin and where has the structure (I) such as (II).
摘要翻译： 抑制人凝血酶的化合物，其中具有结构（I）如（II）的化合物。
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公开(公告)号：EP0639184A1
公开(公告)日：1995-02-22
申请号：EP93910860.0
申请日：1993-04-28
申请人： MERCK & CO. INC.
CPC分类号： C07D401/06 , C07D239/80 , C07D401/12 , C07D403/06 , C07D405/12
摘要： Compounds having a quinazolin-2-one nucleus with a substituted alkynyl or substituted alkenyl at the 4-position are described. These compounds are useful in the inhibition of HIV reverse transcriptase (including its resistant varieties), 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.
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公开(公告)号：EP1912935A2
公开(公告)日：2008-04-23
申请号：EP06787584.9
申请日：2006-07-17
申请人： Merck & Co., Inc.
发明人： SAGGAR, Sandeep, A. , SISKO, John, T. , TUCKER, Thomas, J. , TYNEBOR, Robert, M. , SU, Dai-Shi , ANTHONY, Neville, J.
IPC分类号： C07C311/29 , C07C311/59 , C07C253/30 , A61P31/12
CPC分类号： C07C311/46 , C07C255/54 , C07C255/60 , C07C307/06 , C07C317/40 , C07C2601/14 , C07D209/08 , C07D213/65 , C07D213/75 , C07D231/56 , C07D235/06 , C07D249/04 , C07D249/06 , C07D263/56 , C07D271/06 , C07D271/10 , C07D271/107 , C07D277/64 , C07D333/48 , C07D471/04
摘要： Compounds having the structure: are HIV reverse transcriptase inhibitors, wherein A, X, Y, Z, R1 and R2 are defined herein. The compounds and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译： 具有以下结构的化合物是HIV逆转录酶抑制剂，其中A，X，Y，Z，R1和R2如本文所定义。 这些化合物及其药学上可接受的盐可用于抑制HIV逆转录酶，预防和治疗HIV感染以及预防，延迟发作和治疗AIDS。 化合物及其盐可以用作药物组合物中的成分，任选地与其他抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。
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