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1.发明授权Process for preparing 2-aminothiazole-5-aromatic carboxamides as kinase inhibitors 有权制备2-氨基噻唑-5-芳族羧酰胺作为激酶抑制剂的方法公开(公告)号：US08680103B2
公开(公告)日：2014-03-25
申请号：US13562399
申请日：2012-07-31
IPC分类号： A61K31/506 , C07D403/04
CPC分类号： C07D403/12 , C07D277/56 , C07D417/12
摘要： The invention relates to a pharmaceutical composition of a crystalline monohydrate of the compound of formula (IV) wherein the crystalline monohydrate is characterized by certain unit cell parameters.
摘要翻译： 本发明涉及式（IV）化合物的结晶一水合物的药物组合物，其中结晶一水合物的特征在于某些单位电池参数。
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2.发明授权Process for preparing 2-aminothiazole-5-aromatic carboxamides as kinase inhibitors 有权制备2-氨基噻唑-5-芳族羧酰胺作为激酶抑制剂的方法公开(公告)号：US08242270B2
公开(公告)日：2012-08-14
申请号：US12342141
申请日：2008-12-23
IPC分类号： C07D403/04
CPC分类号： C07D403/12 , C07D277/56 , C07D417/12
摘要： The invention relates to processes for preparing compounds having the formula, and crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R2, R3, R4, and R5, are as defined in the specification herein, which compounds are useful as kinase inhibitors, in particular, inhibitors of protein tyrosine kinase and p38 kinase.
摘要翻译： 本发明涉及制备具有下式的化合物及其结晶形式的方法，其中Ar为芳基或杂芳基，L为任选的亚烷基连接基，R2，R3，R4和R5如本说明书中所定义， 化合物可用作激酶抑制剂，特别是蛋白酪氨酸激酶和p38激酶的抑制剂。
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3.发明申请Process for preparing 2-aminothiazole-5-aromatic carboxamides as kinase inhibitors 审中-公开制备2-氨基噻唑-5-芳族羧酰胺作为激酶抑制剂的方法公开(公告)号：US20050215795A1
公开(公告)日：2005-09-29
申请号：US11051208
申请日：2005-02-04
申请人： Bang-Chi Chen , Roberto Droghini , Jean Lajeunesse , John Dimarco , Michael Galella , Ramakrishnan Chidambaram
发明人： Bang-Chi Chen , Roberto Droghini , Jean Lajeunesse , John Dimarco , Michael Galella , Ramakrishnan Chidambaram
IPC分类号： A61K31/426 , C07D277/56 , C07D417/02 , C07D417/12
CPC分类号： C07D277/56 , C07D417/12
摘要： The invention relates to processes for preparing compounds having the formula, and crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R2, R3, R4, and R5, are as defined in the specification herein, which compounds are useful as kinase inhibitors, in particular, inhibitors of protein tyrosine kinase and p38 kinase.
摘要翻译： 本发明涉及制备具有下式的化合物及其结晶形式的方法，其中Ar为芳基或杂芳基，L为任选的亚烷基连接基，R 2，R 3， R 4，R 5和R 5如本说明书中所定义，该化合物可用作激酶抑制剂，特别是蛋白酪氨酸激酶和p38激酶的抑制剂 。
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4.发明授权公开(公告)号：US08541444B2
公开(公告)日：2013-09-24
申请号：US13197273
申请日：2011-08-03
申请人： Jun Li , Jeffrey A. Robl , James J. Li , Lawrence J. Kennedy , Haixia Wang , Jie Jack Li , Chenkou Wei , Michael Galella
发明人： Jun Li , Jeffrey A. Robl , James J. Li , Lawrence J. Kennedy , Haixia Wang , Jie Jack Li , Chenkou Wei , Michael Galella
IPC分类号： C07D471/02 , C07D491/02 , C07D498/02 , A61K31/44
CPC分类号： C07D471/04
摘要： Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds of formula I: or stereoisomers or pharmaceutically acceptable salts thereof, wherein G, Q, X, Y, R3, R3a, and R3b are defined herein.
摘要翻译： 提供了新的化合物，其为11-β-羟基类固醇脱氢酶I型抑制剂。 11-β-羟基类固醇脱氢酶I型抑制剂可用于治疗，预防或减缓需要11-β-羟基类固醇脱氢酶I型抑制剂治疗的疾病进展。 这些新颖的式I化合物或其立体异构体或其药学上可接受的盐，其中G，Q，X，Y，R 3，R 3a和R 3b在本文中定义。
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5.发明申请公开(公告)号：US20110288051A1
公开(公告)日：2011-11-24
申请号：US13197273
申请日：2011-08-03
申请人： Jun Li , Jeffrey A. Robl , James J. Li , Lawrence J. Kennedy , Haixia Wang , Jie Jack Li , Chenkou Wei , Michael Galella
发明人： Jun Li , Jeffrey A. Robl , James J. Li , Lawrence J. Kennedy , Haixia Wang , Jie Jack Li , Chenkou Wei , Michael Galella
IPC分类号： A61K31/695 , C07F7/10 , A61K31/437 , A61P3/00 , A61P5/08 , A61P19/02 , A61P27/06 , A61P19/08 , A61P3/10 , A61P3/04 , A61P3/06 , A61P25/00 , C07D471/02 , A61P9/12
CPC分类号： C07D471/04
摘要： Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds of formula I: or stereoisomers or pharmaceutically acceptable salts thereof, wherein G, Q, X, Y, R3, R3a, and R3b are defined herein.
摘要翻译： 提供了新的化合物，其为11-β-羟基类固醇脱氢酶I型抑制剂。 11-β-羟基类固醇脱氢酶I型抑制剂可用于治疗，预防或减缓需要11-β-羟基类固醇脱氢酶I型抑制剂治疗的疾病进展。 这些新颖的式I化合物或其立体异构体或其药学上可接受的盐，其中G，Q，X，Y，R 3，R 3a和R 3b在本文中定义。
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6.发明申请PROCESS FOR PREPARING 2-AMINOTHIAZOLE-5-AROMATIC CARBOXAMIDES AS KINASE INHIBITORS 有权制备2-氨基噻唑-5-芳族羧酰胺作为激酶抑制剂的方法公开(公告)号：US20120302750A1
公开(公告)日：2012-11-29
申请号：US13562399
申请日：2012-07-31
IPC分类号： C07D417/14
CPC分类号： C07D403/12 , C07D277/56 , C07D417/12
摘要： The invention relates to processes for preparing compounds having the formula, and crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R2, R3, R4, and R5, are as defined in the specification herein, which compounds are useful as kinase inhibitors, in particular, inhibitors of protein tyrosine kinase and p38 kinase.
摘要翻译： 本发明涉及制备具有下式的化合物及其结晶形式的方法，其中Ar为芳基或杂芳基，L为任选的亚烷基连接基，R2，R3，R4和R5如本说明书中所定义， 化合物可用作激酶抑制剂，特别是蛋白酪氨酸激酶和p38激酶的抑制剂。
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7.发明授权公开(公告)号：US08119658B2
公开(公告)日：2012-02-21
申请号：US12206801
申请日：2008-09-09
申请人： Jun Li , Jeffrey A. Robl , James J. Li , Lawrence J. Kennedy , Haixia Wang , Jie Jack Li , Xinhua Qian , Rajendra P. Deshpande , Laxma R. Kolla , Reginald O. Cann , Chenkou Wei , Michael Galella
发明人： Jun Li , Jeffrey A. Robl , James J. Li , Lawrence J. Kennedy , Haixia Wang , Jie Jack Li , Xinhua Qian , Rajendra P. Deshpande , Laxma R. Kolla , Reginald O. Cann , Chenkou Wei , Michael Galella
IPC分类号： A61K31/437 , C07D471/04 , A61P3/04 , A61P3/10 , A61P9/12 , A61P3/00
CPC分类号： C07D471/04
摘要： Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds of formula I: or stereoisomers or pharmaceutically acceptable salts thereof, wherein G, Q, X, Y, R3, R3a, and R3b are defined herein.
摘要翻译： 提供了新的化合物，其为11-β-羟基类固醇脱氢酶I型抑制剂。 11-β-羟基类固醇脱氢酶I型抑制剂可用于治疗，预防或减缓需要11-β-羟基类固醇脱氢酶I型抑制剂治疗的疾病进展。 这些新颖的式I化合物或其立体异构体或其药学上可接受的盐，其中G，Q，X，Y，R 3，R 3a和R 3b在本文中定义。
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8.发明申请PROCESS FOR PREPARING 2-AMINOTHIAZOLE-5-AROMATIC CARBOXAMIDES AS KINASE INHIBITORS 有权制备2-氨基噻唑-5-芳族羧酰胺作为激酶抑制剂的方法公开(公告)号：US20090149650A1
公开(公告)日：2009-06-11
申请号：US12342141
申请日：2008-12-23
申请人： Bang-Chi Chen , Roberto Droghini , Jean Lajeunesse , John D. Dimarco , Michael Galella , Ramakrishnan Chidambaram
发明人： Bang-Chi Chen , Roberto Droghini , Jean Lajeunesse , John D. Dimarco , Michael Galella , Ramakrishnan Chidambaram
IPC分类号： C07D403/04
CPC分类号： C07D403/12 , C07D277/56 , C07D417/12
摘要： The invention relates to processes for preparing compounds having the formula, and crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R2, R3, R4, and R5, are as defined in the specification herein, which compounds are useful as kinase inhibitors, in particular, inhibitors of protein tyrosine kinase and p38 kinase.
摘要翻译： 本发明涉及制备具有下式的化合物及其结晶形式的方法，其中Ar为芳基或杂芳基，L为任选的亚烷基连接基，R2，R3，R4和R5如本说明书中所定义， 化合物可用作激酶抑制剂，特别是蛋白酪氨酸激酶和p38激酶的抑制剂。
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9.发明申请公开(公告)号：US20060142319A1
公开(公告)日：2006-06-29
申请号：US11301433
申请日：2005-12-13
申请人： Bang-Chi Chen , Albert Delmonte , T.G. Dhar , Michael Galella , Margaret Gleeson , Jack Gougoutas , Douglas McLeod , Huiping Zhang
发明人： Bang-Chi Chen , Albert Delmonte , T.G. Dhar , Michael Galella , Margaret Gleeson , Jack Gougoutas , Douglas McLeod , Huiping Zhang
IPC分类号： A61K31/4747 , C07D487/10
CPC分类号： C07D487/10
摘要： The invention provides crystalline forms of 6-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-yl]nicotinic acid, its pharmaceutically acceptable salts, or solvates, thereof Further, a process is provided for preparing substituted spiro-hydantoin compounds of the formula I wherein Z is N or CR4b; K and L are independently O or S; Ar is an optionally substituted aryl or heteroaryl; A1, A2, G, and Q are linkers; and R2, R4a, R4c, and R16 are defined in the specification. The process includes the reaction of N-substituted glycine compound and methylene precursor compound with an alkene compound. The substituted spiro-hydantoin compounds of formulae I and II are useful in the treatment of immune and/or inflammatory diseases.
摘要翻译： 本发明提供6 - [（5S，9R）-9-（4-氰基苯基）-3-（3,5-二氯苯基）-1-甲基-2,4-二氧代-1,3,7-三氮杂螺[ [4.4]非7-基]烟酸，其药学上可接受的盐或溶剂化物。此外，提供了制备式I的取代的螺 - 乙内酰脲化合物的方法，其中Z是N或CR 4b， SUB>; K和L独立地为O或S; Ar是任选取代的芳基或杂芳基; A 1，A 2，G和Q是连接体; 和R 2，R 4a，R 4c和R 16在本说明书中定义。 该方法包括N-取代的甘氨酸化合物和亚甲基前体化合物与烯烃化合物的反应。 式I和II的取代的螺 - 乙内酰脲化合物可用于治疗免疫和/或炎性疾病。
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公开(公告)号：US20060063815A1
公开(公告)日：2006-03-23
申请号：US11271456
申请日：2005-11-10
申请人： John DiMarco , Jack Gougoutas , Imre Vitez , Martha Davidovich , Michael Galella , Timothy Malloy , Zhenrong Guo , Denis Favreau
发明人： John DiMarco , Jack Gougoutas , Imre Vitez , Martha Davidovich , Michael Galella , Timothy Malloy , Zhenrong Guo , Denis Favreau
IPC分类号： A61K31/427
CPC分类号： C07D491/04 , C07D417/06
摘要： There are provided in accordance with the present invention two crystalline polymorphs, designated Form A and Form B, respectively, as well as mixtures thereof, of an epothilone analog represented by the formula Also provided are methods of forming the novel polymorphs, therapeutic methods utilizing them and pharmaceutical dosage forms containing them.
摘要翻译： 根据本发明，提供分别由式（I）和式（B）表示的两个结晶多晶型物及其混合物，其由式
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