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1.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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公开(公告)号：US08236847B2
公开(公告)日：2012-08-07
申请号：US13081341
申请日：2011-04-06
申请人： Jack Z. Gougoutas , Mary F. Malley , John D. DiMarco , Xiaotian S. Yin , Chenkou Wei , Jurong Yu , Truc Chi Vu , Gregory Scott Jones , Scott A. Savage
发明人： Jack Z. Gougoutas , Mary F. Malley , John D. DiMarco , Xiaotian S. Yin , Chenkou Wei , Jurong Yu , Truc Chi Vu , Gregory Scott Jones , Scott A. Savage
IPC分类号： A61K31/403 , C07D209/02
CPC分类号： C07D209/52 , A61K31/403 , A61K45/06 , A61K2300/00
摘要： Physical crystal structures of a compound of the formula I: are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H2O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H2O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
摘要翻译： 提供式I化合物的物理晶体结构：包括其游离碱一水合物（形式H-1）及其盐酸盐，包括含有0.75当量H 2 O（H0.75-3）的盐酸盐和 含有2当量H 2 O（形式H2-1）的盐酸盐和盐酸盐图案P-5，优选基本上纯的形式，以及本文所述的其它形式，含有化合物I或IA的结构的药物组合物，制备方法 相同的，用于制备其的中间体，以及使用这种结构治疗疾病如糖尿病的方法。
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3.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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公开(公告)号：US20120283181A1
公开(公告)日：2012-11-08
申请号：US13546584
申请日：2012-07-11
申请人： Jack Z. Gougoutas , Mary F. Malley , John D. DiMarco , Xiaotian S. Yin , Chenkou Wei , Jurong Yu , Truc Chi Vu , Gregory Scott Jones , Scott A. Savage
发明人： Jack Z. Gougoutas , Mary F. Malley , John D. DiMarco , Xiaotian S. Yin , Chenkou Wei , Jurong Yu , Truc Chi Vu , Gregory Scott Jones , Scott A. Savage
IPC分类号： A61K31/403 , A61K38/26 , A61K38/28 , A61K31/702 , A61K31/70 , A61P3/10 , A61P3/04 , A61P27/02 , A61P9/10 , A61P25/00 , A61P29/00 , A61P17/06 , A61P37/06 , A61P3/06 , A61P19/02 , A61P15/08 , C07D209/52
CPC分类号： C07D209/52 , A61K31/403 , A61K45/06 , A61K2300/00
摘要： Physical crystal structures of a compound of the formula I: are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H2O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H2O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
摘要翻译： 提供式I化合物的物理晶体结构：包括其游离碱一水合物（形式H-1）及其盐酸盐，包括含有0.75当量H 2 O（H0.75-3）的盐酸盐和 含有2当量H 2 O（形式H2-1）的盐酸盐和盐酸盐图案P-5，优选基本上纯的形式，以及本文所述的其它形式，含有化合物I或IA的结构的药物组合物，制备方法 相同的，用于制备其的中间体，以及使用这种结构治疗疾病如糖尿病的方法。
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公开(公告)号：US20110257085A1
公开(公告)日：2011-10-20
申请号：US13081341
申请日：2011-04-06
申请人： Jack Z. Gougoutas , Mary F. Malley , John D. DiMarco , Xiaotian S. Yin , Chenkou Wei , Jurong Yu , Truc Chi Vu , Gregory Scott Jones , Scott A. Savage
发明人： Jack Z. Gougoutas , Mary F. Malley , John D. DiMarco , Xiaotian S. Yin , Chenkou Wei , Jurong Yu , Truc Chi Vu , Gregory Scott Jones , Scott A. Savage
IPC分类号： A61K31/403 , A61K31/702 , A61K31/445 , A61K31/4439 , A61K38/28 , A61K38/26 , A61K31/451 , A61K38/22 , A61K31/70 , A61K38/18 , A61K31/407 , A61K31/44 , A61K31/405 , A61K31/47 , A61P3/10 , A61P3/08 , A61P3/06 , A61P3/04 , A61P3/00 , A61P9/10 , A61P15/00 , A61P43/00 , A61P19/02 , A61P37/06 , A61P1/00 , A61P29/00 , A61P19/10 , A61K31/4965
CPC分类号： C07D209/52 , A61K31/403 , A61K45/06 , A61K2300/00
摘要： Physical crystal structures of a compound of the formula I: are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H2O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H2O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
摘要翻译： 提供式I化合物的物理晶体结构：包括其游离碱一水合物（形式H-1）及其盐酸盐，包括含有0.75当量H 2 O（H0.75-3）的盐酸盐和 含有2当量H 2 O（形式H2-1）的盐酸盐和盐酸盐图案P-5，优选基本上纯的形式，以及本文所述的其它形式，含有化合物I或IA的结构的药物组合物，制备方法 相同的，用于制备其的中间体，以及使用这种结构治疗疾病如糖尿病的方法。
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公开(公告)号：US20090054303A1
公开(公告)日：2009-02-26
申请号：US12105316
申请日：2008-04-18
申请人： Jack Z. Gougoutas , Mary F. Malley , John D. DiMarco , Xiaotian S. Yin , Chenkou Wei , Jurong Yu , Truc Chi Vu , Gregory Scott Jones , Scott A. Savage
发明人： Jack Z. Gougoutas , Mary F. Malley , John D. DiMarco , Xiaotian S. Yin , Chenkou Wei , Jurong Yu , Truc Chi Vu , Gregory Scott Jones , Scott A. Savage
IPC分类号： A61K38/28 , C07D209/52 , A61K31/403 , A61P3/04 , A61K38/17
CPC分类号： C07D209/52 , A61K31/403 , A61K45/06 , A61K2300/00
摘要： Physical crystal structures of a compound of the formula I: are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H2O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H2O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
摘要翻译： 提供式I化合物的物理晶体结构：包括其游离碱一水合物（形式H-1）及其盐酸盐，包括含有0.75当量H 2 O（H0.75-3）的盐酸盐和 含有2当量H 2 O（形式H2-1）的盐酸盐和盐酸盐图案P-5，优选基本上纯的形式，以及本文所述的其它形式，含有化合物I或IA的结构的药物组合物，制备方法 相同的，用于制备其的中间体，以及使用这种结构治疗疾病如糖尿病的方法。
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7.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：US07491725B2
公开(公告)日：2009-02-17
申请号：US11192867
申请日：2005-07-29
IPC分类号： A61K31/506 , 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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8.发明授权Methods for the preparation, isolation and purification of epothilone B, and X-ray crystal structures of epothilone B 有权埃坡霉素B的制备，分离和纯化方法以及埃坡霉素B的X射线晶体结构公开(公告)号：US07241899B2
公开(公告)日：2007-07-10
申请号：US10805724
申请日：2004-03-22
IPC分类号： A61K31/724 , C12P17/14 , C07D417/02
CPC分类号： C07D493/04 , C12N1/20 , C12N1/38 , C12P17/181 , C12R1/01
摘要： The present invention relates to improved methods for the production, isolation and purification of epothilone B. These methods include, for example, a fermentation process for the production of epothilone B, isolation via adsorption onto a resin, and subsequent purification.
摘要翻译： 本发明涉及埃坡霉素B的生产，分离和纯化的改进方法。这些方法包括例如用于生产埃坡霉素B的发酵方法，通过吸附到树脂上进行分离和随后的纯化。
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公开(公告)号：US07153879B2
公开(公告)日：2006-12-26
申请号：US11271456
申请日：2005-11-10
申请人： John D. DiMarco , Jack Z. Gougoutas , Imre M. Vitez , Martha Davidovich , Michael A. Galella , Timothy M. Malloy , Zhenrong Guo , Denis Favreau
发明人： John D. DiMarco , Jack Z. Gougoutas , Imre M. Vitez , Martha Davidovich , Michael A. Galella , Timothy M. Malloy , Zhenrong Guo , Denis Favreau
IPC分类号： C07D493/04 , A61K31/42 , A61P35/00
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.
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公开(公告)号：US06982276B2
公开(公告)日：2006-01-03
申请号：US10773819
申请日：2004-02-06
申请人： John D. DiMarco , Jack Z. Gougoutas , Imre M. Vitez , Martha Davidovich , Michael A. Galella , Timothy M. Malloy , Zhenrong Guo , Denis Favreau
发明人： John D. DiMarco , Jack Z. Gougoutas , Imre M. Vitez , Martha Davidovich , Michael A. Galella , Timothy M. Malloy , Zhenrong Guo , Denis Favreau
IPC分类号： C07D493/04 , A61K31/42
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.
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