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1.发明授权2-PHENOXY-N-(1,3,4-THIADIZOL-2-YL)PYRIDIN-3-AMINE DERIVATIVES AND RELATED COMPOUNDS AS P2Y1 RECEPTOR INHIBITORS FOR THE TREATMENT OF THROMBOEMBOLIC DISORDERS 有权2-苯氧基 - N-（1,3,4- THIADIZOL -2-基）吡啶-3-胺衍生物和相关化合物P2Y1受体抑制剂用于治疗血栓栓塞性病症
公开(公告)号：EP1954696B1
公开(公告)日：2011-02-23
申请号：EP06733718.8
申请日：2006-01-17
发明人： SUTTON, James, C. , PI, Zulan , RUEL, Rejean , L'HEUREUX, Alexandre , THIBEAULT, Carl , LAM, Patrick, Y., S.
IPC分类号： C07D417/12 , C07D413/12 , C07D401/12 , C07D213/74 , C07D417/14 , C07D277/42 , C07D277/56 , C07D513/04 , A61P7/02
CPC分类号： C07D213/74 , C07D213/75 , C07D213/80 , C07D277/42 , C07D277/56 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/04 , C07D513/04
摘要： The present invention provides novel heteroaryl compounds of formula (Ia) which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity. (Ia) or a stereoisomer, tautomer, pharmaceutically acceptable salt, or solvate thereof, wherein: ring A is a 5- to 6-membered heteroaryl comprising: carbon atoms and 1-4 ringheteroatoms selected from N, NR11, S(O)p, and O, wherein said heteroaryl is substituted with 0-4 R1; ring B is phenyl substituted with 0-4 R7, pyridyl substituted with 0-3 R7, or thienyi substituted with 0-2 R7; X is NH or NMe; Y is O or S; R5 is a -(CRfRf)n-C3-10 carbocycle substituted with 1-4 R5a, or a -(CRfRf)n-5- to 10-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, NR11, O, and S(O)p, wherein said heterocycle is substituted with 0-4 R5a; the other substituents and variables are defined in the claims.
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2.发明公开SULFONYLPYRROLODINE MODULATORS OF ANDROGEN RECEPTOR FUCTION AND METHOD 审中-公开Sulfonylpyrrolidinmodulatoren其制备的雄激素受体和方法
公开(公告)号：EP1718626A1
公开(公告)日：2006-11-08
申请号：EP05712320.0
申请日：2005-02-02
发明人： HAMANN, Lawrence, H. , BI, Yingzhi , MANFREDI, Mark, C. , NIRSCHL, Alexandra, A. , SUTTON, James, C.
IPC分类号： C07D285/06 , A61K31/433
CPC分类号： C07D285/14 , C07D207/48
摘要： Compounds are provided which are useful in the treatment of androgen receptor-associated conditions, such as age-related diseases, which compounds have the structure of formulae (I) or (II); whereinR1 is hydrogen (H), alkyl or substituted alkyl, alkenyl or substituted alkenyl, arylalkyl or substituted arylalkyl, CO2R4a, CONR4aR4b, and CH2OR4a; R2 is hydrogen (H), OR3, SR3, halo, NHR3, NHCOR4c1, NHCO2R4c1, NHCONR4cR4d and NHSO2R4c; R3 in each functional group is hydrogen (H), alkyl or substituted alkyl, CHF2, CF3 and COR4e; R4, R4a, R4b, R4c, R4c1, R4d, R4e, R4f, R4g, or R4h in each functional group are the same or different and are hydrogen(H), alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, arylalkyl or substituted arylalkyl, aryl or substituted aryl, or heteroaryl or substituted heteroaryl; R5 and R5 are the same or different and are hydrogen(H), alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, arylalkyl or substituted arylalkyl, aryl or substituted aryl, or heteroaryl or substituted heteroaryl, wherein at least one of R5 and R5 is hydrogen, or R5 and R5 taken together form a double bond with oxygen (O), sulfur (S), NR7 or CR7R7 ; where R7 and R7 are as defined herein; G is an aryl, heterocyclo or heteroaryl group, wherein said group is mono- or polycyclic, and which is optionally substituted; and n is an integer of 1 or 2, m is an integer of 1 or 2, Z is oxygen (-O-) or NR4h, a prodrug ester, all stereoisomers thereof and a pharmaceutically acceptable salt. A method for treating androgen receptor-associated conditions such as age-related diseases is also provided.
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3.发明授权ADAMANTYLGLYCINE- BASED INHIBITORS OF DIPEPTIDYL PEPTIDASE IV FOR THE TREATMENT OF DIABETES 有权抑制剂DEP DIPEPTIDYPEPTIDASE IV AUF ADAMANTYLGLYCINBASIS ZUR BEHANDLUNG VON DIABETES
公开(公告)号：EP1658066B1
公开(公告)日：2009-09-30
申请号：EP04779352.6
申请日：2004-07-28
发明人： HAMANN, Lawrence, G. , KHANNA, Ashish , KIRBY, Mark, S. , MAGNIN, David, R. , SIMPKINS, Ligaya, M. , SUTTON, James, C. , ROBL, Jeffrey
IPC分类号： A61K31/40
CPC分类号： C07C255/46 , C07C255/47 , C07C2601/08 , C07C2602/18 , C07C2603/74 , C07D207/16 , C07D209/52 , C07D277/04 , C07D295/185
摘要： Compounds are provided having the formula (I) wherein: n is 0, 1 or 2; m is 0, 1 or 2; the sum of n + m less then or equal to 2; the dashed bonds forming a cyclopropyl ring can only be present when Y is CH; X is H or CN; Y is CH, CH2, CHF, CF2, O, S, SO, or SO2; and A is adamantyl. The compounds are inhibitors of dipeptidyl peptidase IV (DPP-IV) and are useful for the treatment of diabetes and related diseases.
摘要翻译： 本发明的化合物是二肽基肽酶IV（DPP-IV）的基于金刚烷基甘氨酸的抑制剂，可用于治疗糖尿病和相关疾病。
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公开(公告)号：EP1722793A1
公开(公告)日：2006-11-22
申请号：EP05724717.3
申请日：2005-03-03
发明人： NIRSCHL, Alexandra, A. , SUTTON, James, C. , HAMANN, Lawrence , WANG, Tammy , ZOU, Yan , SUN, Chongqing
IPC分类号： A61K31/44 , A61K31/425 , C07D263/60 , C07D471/02
CPC分类号： C07D487/04 , C07D498/04 , C07D513/04
摘要： The present invention relates to bicyclic compounds according to formula (I), pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of androgen receptor-associated conditions, such as age-related diseases, for example sarcopenia, wherein R1, R2, R5, X, Y and n are defined herein.
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公开(公告)号：EP1089973A1
公开(公告)日：2001-04-11
申请号：EP99930402.5
申请日：1999-06-18
发明人： BISACCHI, Gregory , SLUSARCHYK, William, A. , TREUNER, Uwe , SUTTON, James, C. , ZAHLER, Robert , SEILER, Steven , KRONENTHAL, David, R. , RANDAZZO, Michael, E. , XU, Zhongmin , SHI, Zhongping , SCHWINDEN, Mark, D.
IPC分类号： C07D205/08 , C07D205/09
CPC分类号： C07D403/12 , C07D205/08
摘要： Compounds of formulae (I), (II), (III).
摘要翻译： 式（I），（II），（III）的化合物。
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6.发明授权ADAMANTYLGLYCINE- BASED INHIBITORS OF DIPEPTIDYL PEPTIDASE IV FOR THE TREATMENT OF DIABETES 有权二肽基肽酶IV抑制剂对糖尿病ADAMANTYLGLYCINBASIS处理成
公开(公告)号：EP1658066B9
公开(公告)日：2010-02-24
申请号：EP04779352.6
申请日：2004-07-28
发明人： HAMANN, Lawrence, G. , KHANNA, Ashish , KIRBY, Mark, S. , MAGNIN, David, R. , SIMPKINS, Ligaya, M. , SUTTON, James, C. , ROBL, Jeffrey
IPC分类号： A61K31/40
CPC分类号： C07C255/46 , C07C255/47 , C07C2601/08 , C07C2602/18 , C07C2603/74 , C07D207/16 , C07D209/52 , C07D277/04 , C07D295/185
摘要： Compounds are provided having the formula (I) wherein: n is 0, 1 or 2; m is 0, 1 or 2; the sum of n + m less then or equal to 2; the dashed bonds forming a cyclopropyl ring can only be present when Y is CH; X is H or CN; Y is CH, CH2, CHF, CF2, O, S, SO, or SO2; and A is adamantyl. The compounds are inhibitors of dipeptidyl peptidase IV (DPP-IV) and are useful for the treatment of diabetes and related diseases.
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7.发明公开2-PHENOXY-N-(1,3,4-THIADIZOL-2-YL)PYRIDIN-3-AMINE DERIVATIVES AND RELATED COMPOUNDS AS P2Y1 RECEPTOR INHIBITORS FOR THE TREATMENT OF THROMBOEMBOLIC DISORDERS 有权2-苯氧基 - N-（1,3,4- THIADIZOL -2-基）吡啶-3-胺衍生物和相关化合物P2Y1受体抑制剂用于治疗血栓栓塞性病症
公开(公告)号：EP1954696A2
公开(公告)日：2008-08-13
申请号：EP06733718.8
申请日：2006-01-17
发明人： SUTTON, James, C. , PI, Zulan , RUEL, Rejean , L'HEUREUX, Alexandre , THIBEAULT, Carl , LAM, Patrick, Y., S.
IPC分类号： C07D417/12 , C07D413/12 , C07D401/12 , C07D213/74 , C07D417/14 , C07D277/42 , C07D277/56 , C07D513/04 , A61P7/02
CPC分类号： C07D213/74 , C07D213/75 , C07D213/80 , C07D277/42 , C07D277/56 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/04 , C07D513/04
摘要： The present invention provides novel heteroaryl compounds of formula (Ia) which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity. (Ia) or a stereoisomer, tautomer, pharmaceutically acceptable salt, or solvate thereof, wherein: ring A is a 5- to 6-membered heteroaryl comprising: carbon atoms and 1-4 ringheteroatoms selected from N, NR11, S(O)p, and O, wherein said heteroaryl is substituted with 0-4 R1; ring B is phenyl substituted with 0-4 R7, pyridyl substituted with 0-3 R7, or thienyi substituted with 0-2 R7; X is NH or NMe; Y is O or S; R5 is a -(CRfRf)n-C3-10 carbocycle substituted with 1-4 R5a, or a -(CRfRf)n-5- to 10-membered heterocycle comprising: carbon atoms and 1-4 heteroatoms selected from N, NR11, O, and S(O)p, wherein said heterocycle is substituted with 0-4 R5a; the other substituents and variables are defined in the claims.
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8.发明公开ADAMANTYLGLYCINE- BASED INHIBITORS OF DIPEPTIDYL PEPTIDASE IV FOR THE TREATMENT OF DIABETES 有权二肽基肽酶IV抑制剂对糖尿病ADAMANTYLGLYCINBASIS处理成
公开(公告)号：EP1658066A2
公开(公告)日：2006-05-24
申请号：EP04779352.6
申请日：2004-07-28
发明人： HAMANN, Lawrence, G. , KHANNA, Ashish , KIRBY, Mark, S. , MAGNIN, David, R. , SIMPKINS, Ligaya, M. , SUTTON, James, C. , ROBL, Jeffrey
IPC分类号： A61K31/40
CPC分类号： C07C255/46 , C07C255/47 , C07C2601/08 , C07C2602/18 , C07C2603/74 , C07D207/16 , C07D209/52 , C07D277/04 , C07D295/185
摘要： Compounds are provided having the formula (I) wherein: n is 0, 1 or 2; m is 0, 1 or 2; the sum of n + m less then or equal to 2; the dashed bonds forming a cyclopropyl ring can only be present when Y is CH; X is H or CN; Y is CH, CH2, CHF, CF2, O, S, SO, or SO2; and A is adamantyl. The compounds are inhibitors of dipeptidyl peptidase IV (DPP-IV) and are useful for the treatment of diabetes and related diseases.
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公开(公告)号：EP1089973B1
公开(公告)日：2005-11-09
申请号：EP99930402.5
申请日：1999-06-18
发明人： BISACCHI, Gregory , SLUSARCHYK, William, A. , TREUNER, Uwe , SUTTON, James, C. , ZAHLER, Robert , SEILER, Steven , KRONENTHAL, David, R. , RANDAZZO, Michael, E. , XU, Zhongmin , SHI, Zhongping , SCHWINDEN, Mark, D.
IPC分类号： C07D205/08 , C07D205/09 , C07D403/12 , C07D401/06 , C07D403/06 , A61K31/395
CPC分类号： C07D403/12 , C07D205/08
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