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1.发明公开
公开(公告)号：EP1056745A2
公开(公告)日：2000-12-06
申请号：EP99936074.6
申请日：1999-02-18
发明人： DUMONT, Jennifer, A. , BITONTI, Alan, J. , BORCHERDING, David, R. , PEET, Norton, P. , MUNSON, H., Randall , SHUM, Patrick, W., K.
IPC分类号： C07D473/16 , A61K31/52
CPC分类号： C07D473/16
摘要： The present invention provides novel compounds of formula (I) wherein R is selected from the group consisting of R2, R2NH-, or H2N-R3- wherein R2 is selected from the group consisting of C1-C8 alkyl and formula (II), wherein Z is selected from the group consisting of phenyl, heterocycle and cycloalkyl, each R4 is independently hydrogen or C1-C4 alkyl, and n is an integer 1-8; wherein each C1-C8 alkyl and Z is optionally substituted with 1 to 3 substituents, which may be the same or different, selected from the group consisting of Hal, OH, and C1-C4 alkyl; R3 is C1-C8 alkylene; and R1 is selected from the group consisting of cyclopentyl and isopropyl, and the pharmaceutically acceptable salts, optical isomers, and hydrates thereof. In addition, the present invention provides a method of inhibiting cell cycle progression. More specifically, the present invention provides a method of inhibiting cyclin dependent kinases, particularly cdk-2. The present invention also provides a method of preventing apoptosis in neuronal cells and a method of inhibiting the development of neoplasms. In addition, the present invention provides a composition comprising an assayable amount of a compound of formula (I) in admixture or otherwise in association with an inert carrier. The present invention also provides a pharmaceutical composition comprising an effective inhibitory amount of a compound of formula (I) in admixture or otherwise in association with one or more pharmaceutically acceptable carriers or excipients.
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2.发明授权1-(2H-PYRAZOL-3-YL)-3-{4-[1-(BENZOYL)-PIPERIDIN-4-YLMETHYL]-PHENYL}-UREA DERIVATIVES AND RELATED COMPOUNDS AS INHIBITORS OF P38 KINASE AND/OR TNF INHIBITORS FOR THE TREATMENT OF INFLAMMATIONS 有权1-（2H-吡唑-3-基）-3- {4- [1-（苯甲酰基） - 哌啶-4-基甲基] - 苯基} -HARNSTOFFDERIVATE及相关化合物AS P38激酶和/或TNF用于治疗抑制剂 炎症
公开(公告)号：EP1622610B1
公开(公告)日：2006-12-20
申请号：EP04751319.7
申请日：2004-05-05
发明人： BORCHERDING, David, R. , GROSS, Alexandre , SHUM, Patrick, Wai-Kwok , WILLARD, Nicole , FREED, Brian, S.
IPC分类号： A61K31/4155 , C07D401/12 , C07D451/02 , A61P29/00
CPC分类号： C07D401/14 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D451/02 , C07D471/04
摘要： The present invention provides compounds of Formula (I) Wherein ( ) is an optional ethylene bridge; R1 is alkyl, cycloalkyl, aryl or aryl substituted with one or more substituents selected from alkyl, alkoxy and amino, or R1 is pyridyl or pyridyl substituted with one or more substituents selected from alkyl, alkoxy and amino; R2 is optionally substituted alkyl, alkoxyalkyl, optionally substituted cycloalkylalkyl, arylalkyl, or R2 is arylalkyl substituted with one or more substituents selected from alkyl, alkoxy; X is -C(O)-, -C(O)-CH2-, -S(O)2-, or NH-C(O)- ; and A is optionally substituted alkyl or other substituents as defined in claim 1. Pharmaceutical compositions comprising such compounds, their preparation, and their pharmaceutical use in the treatment of disease states capable of being modulated by the inhibition of p38 kinase and/or tumor necrosis factor (TNF), such as asthma or joint inflammation.
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3.发明公开1-(2H-PYRAZOL-3-YL)-3- 4-[1-(BENZOYL)-PIPERIDIN-4-YLMETHYL]-PHENYL -UREA DERIVATIVES AND RELATED COMPOUNDS AS INHIBITORS OF P38 KINASE AND/OR TNF INHIBITORS FOR THE TREATMENT OF INFLAMMATIONS 有权1-（2H-吡唑-3-基）-3- [1-（苯甲酰基） - 哌啶-4-基甲基] - 苯基 - 脲衍生物和作为P38激酶和/或TNF抑制剂用于治疗的抑制剂的相关化合物 炎症
公开(公告)号：EP1622610A1
公开(公告)日：2006-02-08
申请号：EP04751319.7
申请日：2004-05-05
发明人： BORCHERDING, David, R. , GROSS, Alexandre , SHUM, Patrick, Wai-Kwok , WILLARD, Nicole , FREED, Brian, S.
IPC分类号： A61K31/4155 , C07D401/12 , C07D451/02 , A61P29/00
CPC分类号： C07D401/14 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D451/02 , C07D471/04
摘要： The present invention provides compounds of Formula (I) Wherein ( ) is an optional ethylene bridge; R1 is alkyl, cycloalkyl, aryl or aryl substituted with one or more substituents selected from alkyl, alkoxy and amino, or R1 is pyridyl or pyridyl substituted with one or more substituents selected from alkyl, alkoxy and amino; R2 is optionally substituted alkyl, alkoxyalkyl, optionally substituted cycloalkylalkyl, arylalkyl, or R2 is arylalkyl substituted with one or more substituents selected from alkyl, alkoxy; X is -C(O)-, -C(O)-CH2-, -S(O)2-, or NH-C(O)- ; and A is optionally substituted alkyl or other substituents as defined in claim 1. Pharmaceutical compositions comprising such compounds, their preparation, and their pharmaceutical use in the treatment of disease states capable of being modulated by the inhibition of p38 kinase and/or tumor necrosis factor (TNF), such as asthma or joint inflammation.
摘要翻译： 本发明提供了式（I）的化合物，其中（）为任选的亚乙基桥; R1为被一个或多个选自烷基，烷氧基和氨基的取代基取代的烷基，环烷基，芳基或芳基，或者R1为被一个或多个选自烷基，烷氧基和氨基的取代基取代的吡啶基或吡啶基; R2是任选取代的烷基，烷氧基烷基，任选取代的环烷基烷基，芳基烷基，或R2是被一个或多个选自烷基，烷氧基的取代基取代的芳基烷基; X是-C（O） - ， - C（O）-CH 2 - ， - S（O）2 - 或NH-C（O） - ; 并且A是任选取代的烷基或权利要求1中定义的其它取代基。包含此类化合物的药物组合物，它们的制备及其在治疗能够通过抑制p38激酶和/或肿瘤坏死因子 （TNF），如哮喘或关节炎症。
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4.发明授权
公开(公告)号：EP1056745B1
公开(公告)日：2004-06-16
申请号：EP99936074.6
申请日：1999-02-18
发明人： DUMONT, Jennifer, A. , BITONTI, Alan, J. , BORCHERDING, David, R. , PEET, Norton, P. , MUNSON, H., Randall , SHUM, Patrick, W., K.
IPC分类号： C07D473/16 , A61K31/52
CPC分类号： C07D473/16
摘要： The present invention provides novel compounds of formula (I) wherein R is selected from the group consisting of R2, R2NH-, or H2N-R3- wherein R2 is selected from the group consisting of C1-C8 alkyl and formula (II), wherein Z is selected from the group consisting of phenyl, heterocycle and cycloalkyl, each R4 is independently hydrogen or C1-C4 alkyl, and n is an integer 1-8; wherein each C1-C8 alkyl and Z is optionally substituted with 1 to 3 substituents, which may be the same or different, selected from the group consisting of Hal, OH, and C1-C4 alkyl; R3 is C1-C8 alkylene; and R1 is selected from the group consisting of cyclopentyl and isopropyl, and the pharmaceutically acceptable salts, optical isomers, and hydrates thereof. In addition, the present invention provides a method of inhibiting cell cycle progression. More specifically, the present invention provides a method of inhibiting cyclin dependent kinases, particularly cdk-2. The present invention also provides a method of preventing apoptosis in neuronal cells and a method of inhibiting the development of neoplasms. In addition, the present invention provides a composition comprising an assayable amount of a compound of formula (I) in admixture or otherwise in association with an inert carrier. The present invention also provides a pharmaceutical composition comprising an effective inhibitory amount of a compound of formula (I) in admixture or otherwise in association with one or more pharmaceutically acceptable carriers or excipients.
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