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1. 发明授权

US06867300B2 Methods for the preparation of pyrrolotriazine compounds useful as kinase inhibitors 失效
标题翻译：制备用作激酶抑制剂的吡咯并三嗪化合物的方法
公开(公告)号：US06867300B2
公开(公告)日：2005-03-15
申请号：US10289010
申请日：2002-11-06
申请人： Jollie Duaine Godfrey, Jr. , John Hynes, Jr. , Alaric J. Dyckman , Katerina Leftheris , Zhongping Shi , Stephen T. Wrobleski , Wendel William Doubleday , John A. Grosso
发明人： Jollie Duaine Godfrey, Jr. , John Hynes, Jr. , Alaric J. Dyckman , Katerina Leftheris , Zhongping Shi , Stephen T. Wrobleski , Wendel William Doubleday , John A. Grosso
IPC分类号： A61P11/06 , A61P19/02 , A61P19/10 , C07D207/50 , C07D487/04 , C07D519/00 , A61K31/53
CPC分类号： C07D487/04 , C07D207/50
摘要： Methods of preparing kinase inhibiting pharmaceutical compounds having the formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein R1 through R6 and Z are as described in the specification. The methods according to the invention utilize an amination process, in which a pyrrole is reacted with a haloamine, preferably chloramine. This step is followed by cyclization to form the pyrrolotriazine core.
摘要翻译：制备具有式（I）的激酶抑制药物化合物或其药学上可接受的盐或溶剂化物的方法，其中R1至R6和Z如说明书所述。根据本发明的方法利用胺化方法，其中吡咯与卤胺，优选氯胺反应。该步骤之后环化形成吡咯并三嗪核心。

2. 发明申请

US20120108594A1 PROCESS FOR PREPARING SALTS OF 4-[[5-[(CYCLOPROPYLAMINO)CARBONYL]-2-METHYLPHENYL]AMINO]-5-METHYL-N-PROPYLPYRROLO[2,1-f][1,2,4]TRIAZINE-6-CARBOXAMIDE AND NOVEL STABLE FORMS PRODUCED THEREIN 审中-公开
标题翻译：制备4 - [[5 - [（环丙基氨基）羰基] -2-甲基苯基]氨基] -5-甲基-N-丙基吡咯并[2,1-f] [1,2,4]三氮杂- 碳酰胺和生产的新型稳定形式
公开(公告)号：US20120108594A1
公开(公告)日：2012-05-03
申请号：US13293204
申请日：2011-11-10
申请人： Soojin Kim , Mary F. Malley , Zhongping Shi
发明人： Soojin Kim , Mary F. Malley , Zhongping Shi
IPC分类号： A61K31/53 , A61P29/00 , A61P11/06 , A61P11/00 , A61P19/02 , A61P1/00 , A61P19/10 , A61P17/06 , A61P37/06 , A61P9/10 , C07D487/04 , A61P3/10
CPC分类号： C07D487/04
摘要： Processes are provided for selectively preparing novel stable crystalline salt forms, selectively and consistently, namely, preparing Form N-1 of the methanesulfonic acid salt, and Form N-1 and Form N-4 of the hydrochloric acid salt of the p38 kinase inhibitor 4-[[5-[(cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide. The processes preferably employ solvent systems including formic acid/acetone and formic acid/methylethyl ketone which produce crystals having suitable flow properties and desired particle size, and solvents such as N,N-dimethylformamide and N,N-dimethylacetamide may be employed as well.Novel Form N-1 crystals of the Form N-1 and Form N-4 crystals of the hydrochloride salt and Form N-1 crystals of the methanesulfonic acid salt of the above free base, pharmaceutical compositions containing such novel forms and a method of treating p38 kinase associated conditions, including rheumatoid arthritis are also provided.
摘要翻译：提供了选择性和一致地选择性制备新的稳定结晶盐形式的方法，即制备甲磺酸盐的N-1型，和p38激酶抑制剂4的盐酸盐的N-1和N-4型 - [[5 - [（环丙基氨基）羰基] -2-甲基苯基]氨基] -5-甲基-N-丙基吡咯并[2,1-f] [1,2,4]三嗪-6-甲酰胺。该方法优选使用包含甲酸/丙酮和甲酸/甲基乙基酮的溶剂体系，其产生具有合适流动性和所需粒径的晶体，并且也可以使用溶剂如N，N-二甲基甲酰胺和N，N-二甲基乙酰胺。上述游离碱的甲磺酸盐的盐酸盐形式的N-1型和N-4型结晶的新型N-1晶体和形式N-1晶体，含有这种新形式的药物组合物和治疗方法还提供p38激酶相关病症，包括类风湿性关节炎。

3. 发明授权

US07534881B2 Method for preparing pyrrolotriazine compounds 失效
标题翻译：吡咯并三嗪化合物的制备方法
公开(公告)号：US07534881B2
公开(公告)日：2009-05-19
申请号：US11168682
申请日：2005-06-28
申请人： Zhongping Shi , John Hynes , Luca Parlanti , Stephen T. Wrobleski
发明人： Zhongping Shi , John Hynes , Luca Parlanti , Stephen T. Wrobleski
IPC分类号： C07D487/04 , C07D207/30 , C07D207/50
CPC分类号： C07D487/04 , C07D487/14
摘要： A method for aminating pyrrole derivatives and for preparing pyrrolotriazine compounds having the formula V,
摘要翻译：用于胺化吡咯衍生物和制备具有式V的吡咯并三嗪化合物的方法，

4. 发明授权

US07034152B2 Process for preparing the antiviral agent [1S-(1alpha,3 alpha,4beta )]-2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-6H-purin-6-one 有权
标题翻译：制备抗病毒剂的方法[1S-（1α，3α，4beta）] - 2-氨基-1,9-二氢-9- [4-羟基-3-（羟甲基）-2-亚甲基环戊基] -6H-嘌呤 -6-one
公开(公告)号：US07034152B2
公开(公告)日：2006-04-25
申请号：US10734012
申请日：2003-12-11
申请人： Yadagiri R. Pendri , Chung-Pin H. Chen , Sunil S. Patel , Jeffrey M. Evans , Jing Liang , David R. Kronenthal , Gerald L. Powers , Siva Josyula Prasad , Jeffrey T. Bien , Zhongping Shi , Ramesh N. Patel , Amit Banerjee , Yeung Yu Chan , Sushil K. Rijhwani , Ambarish K. Singh , Shaopeng Wang , Milan Stojanovic , David J. Kucera , Richard P. Polniaszek , Charles Lewis , John Thottathil , Dhileepkumar Krishnamurty , Maotang X. Zhou , Purushotham Vemishetti
发明人： Yadagiri R. Pendri , Chung-Pin H. Chen , Sunil S. Patel , Jeffrey M. Evans , Jing Liang , David R. Kronenthal , Gerald L. Powers , Siva Josyula Prasad , Jeffrey T. Bien , Zhongping Shi , Ramesh N. Patel , Amit Banerjee , Yeung Yu Chan , Sushil K. Rijhwani , Ambarish K. Singh , Shaopeng Wang , Milan Stojanovic , David J. Kucera , Richard P. Polniaszek , Charles Lewis , John Thottathil , Dhileepkumar Krishnamurty , Maotang X. Zhou , Purushotham Vemishetti
IPC分类号： C07D473/18 , C07D7/08 , C07D473/40 , C07F7/10 , C07F7/18
CPC分类号： C07F7/083 , C07D473/18 , C07F7/081 , C07F7/0812 , C07F7/0814 , C07F7/0827 , C07F7/1804
摘要： Processes are disclosed for preparing the antiviral agent entecavir. A resin adsorption process for the isolation and purification of entecavir is also disclosed. Various intermediates useful in the preparation of entecavir are also disclosed.
摘要翻译：公开了制备抗病毒剂恩替卡韦的方法。还公开了用于恩替卡韦的分离和纯化的树脂吸附方法。还公开了可用于制备恩替卡韦的各种中间体。

5. 发明申请

US20050107462A1 Methods for the preparation of pyrrolotriazine compounds useful as kinase inhibitors 有权
标题翻译：制备用作激酶抑制剂的吡咯并三嗪化合物的方法
公开(公告)号：US20050107462A1
公开(公告)日：2005-05-19
申请号：US11019788
申请日：2004-12-22
申请人： Jollie Godfrey , John Hynes , Alaric Dyckman , Katerina Leftheris , Zhongping Shi , Stephen Wrobleski , Wendel William Doubleday , John Grosso
发明人： Jollie Godfrey , John Hynes , Alaric Dyckman , Katerina Leftheris , Zhongping Shi , Stephen Wrobleski , Wendel William Doubleday , John Grosso
IPC分类号： A61P11/06 , A61P19/02 , A61P19/10 , C07D207/50 , C07D487/04 , C07D519/00 , A61K31/4015 , A61K31/401 , A61K31/4025
CPC分类号： C07D487/04 , C07D207/50
摘要： Methods of preparing kinase inhibiting pharmaceutical compounds having the formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein R1 through R6 and Z are as described in the specification. The methods according to the invention utilize an amination process, in which a pyrrole is reacted with a haloamine, preferably chloramine. This step is followed by cyclization to form the pyrrolotriazine core.
摘要翻译：制备具有式（I）的激酶抑制药物化合物或其药学上可接受的盐或溶剂化物的方法，其中R 1至R 6和Z如规范。根据本发明的方法利用胺化方法，其中吡咯与卤胺，优选氯胺反应。该步骤之后环化形成吡咯并三嗪核心。

6. 发明授权

US07211666B2 Methods for the preparation of pyrrolotriazine compounds useful as kinase inhibitors 有权
标题翻译：制备用作激酶抑制剂的吡咯并三嗪化合物的方法
公开(公告)号：US07211666B2
公开(公告)日：2007-05-01
申请号：US11019788
申请日：2004-12-22
申请人： Jollie Duaine Godfrey, Jr. , John Hynes, Jr. , Alaric J. Dyckman , Katerina Leftheris , Zhongping Shi , Stephen T. Wrobleski , Wendel William Doubleday , John A. Grosso
发明人： Jollie Duaine Godfrey, Jr. , John Hynes, Jr. , Alaric J. Dyckman , Katerina Leftheris , Zhongping Shi , Stephen T. Wrobleski , Wendel William Doubleday , John A. Grosso
IPC分类号： C07D487/04 , C07D207/36
CPC分类号： C07D487/04 , C07D207/50
摘要： Methods of preparing kinase inhibiting pharmaceutical compounds having the formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein R1 through R6 and Z are as described in the specification. The methods according to the invention utilize an amination process, in which a pyrrole is reacted with a haloamine, preferably chloramine. This step is followed by cyclization to form the pyrrolotriazine core.
摘要翻译：制备具有式（I）的激酶抑制药物化合物或其药学上可接受的盐或溶剂化物的方法，其中R 1至R 6和Z如规范。根据本发明的方法利用胺化方法，其中吡咯与卤胺，优选氯胺反应。该步骤之后环化形成吡咯并三嗪核心。

7. 发明授权

US07074921B2 Process for the preparation of 3,7-disubstituted-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine compounds 失效
公开(公告)号：US07074921B2
公开(公告)日：2006-07-11
申请号：US10292093
申请日：2002-11-12
申请人： David R. Kronenthal , Rao S. Bhandaru , Zhongping Shi , Boguslaw M. Mudryk
发明人： David R. Kronenthal , Rao S. Bhandaru , Zhongping Shi , Boguslaw M. Mudryk
IPC分类号： C07D243/14 , A61K31/55 , A61P35/00
CPC分类号： C07D233/64 , C07C255/58 , C07C255/61 , C07D243/14 , C07D333/34 , C07D403/06 , C07D409/12 , C07D409/14 , C07F7/1804
摘要： Methods for the synthesis of benzodiazepine compounds having farnesyl protein transferase inhibitory activity.

8. 发明申请

US20060003967A1 Method for preparing pyrrolotriazine compounds 失效
公开(公告)号：US20060003967A1
公开(公告)日：2006-01-05
申请号：US11168682
申请日：2005-06-28
申请人： Zhongping Shi , John Hynes , Luca Parlanti , Stephen Wrobleski
发明人： Zhongping Shi , John Hynes , Luca Parlanti , Stephen Wrobleski
IPC分类号： A61K31/675 , C07D487/14 , A61K31/53
CPC分类号： C07D487/04 , C07D487/14
摘要： A method for aminating pyrrole derivatives and for preparing pyrrolotriazine compounds having the formula V,

9. 发明授权

US06335324B1 Beta lactam compounds and their use as inhibitors of tryptase 有权
标题翻译： β-内酰胺化合物及其作为类胰蛋白酶抑制剂的用途
公开(公告)号：US06335324B1
公开(公告)日：2002-01-01
申请号：US09458847
申请日：1999-12-13
申请人： Gregory S. Bisacchi , William A. Slusarchyk , Uwe Treuner , James C. Sutton , Robert Zahler , Steven Seiler , David R. Kronenthal , Michael E. Randazzo , Mark D. Schwinden , Zhongmin Xu , Zhongping Shi
发明人： Gregory S. Bisacchi , William A. Slusarchyk , Uwe Treuner , James C. Sutton , Robert Zahler , Steven Seiler , David R. Kronenthal , Michael E. Randazzo , Mark D. Schwinden , Zhongmin Xu , Zhongping Shi
IPC分类号： C07D4014
CPC分类号： C07D403/12 , C07D205/08
摘要： Compounds of the formulas: are disclosed. These compounds inhibit tryptase as well as other enzyme systems or are selective tryptase inhibitors and are useful as antiinflammatory agents particularly in the treatment of chronic asthma.
摘要翻译：公开了下列化合物：这些化合物抑制类胰蛋白酶以及其他酶系统或选择性类胰蛋白酶抑制剂，并且可用作抗炎剂，特别是用于治疗慢性哮喘。

10. 发明申请

US20090312331A1 PROCESS FOR PREPARING SALTS OF 4-[[5-[(CYCLOPROPYLAMINO)CARBONYL]-2-METHYLPHENYL]AMINO]-5-METHYL-N-PROPYLPYRROLO[2,1-f][1,2,4]TRIAZINE-6-CARBOXAMIDE AND NOVEL STABLE FORMS PRODUCED THEREIN 审中-公开
标题翻译：制备4 - [[5 - [（环丙基氨基）羰基] -2-甲基苯基]氨基] -5-甲基-N-丙基吡咯并[2,1-f] [1,2,4]三氮杂- 碳酰胺和生产的新型稳定形式
公开(公告)号：US20090312331A1
公开(公告)日：2009-12-17
申请号：US12478210
申请日：2009-06-04
申请人： Soojin Kim , Mary F. Malley , Zhongping Shi
发明人： Soojin Kim , Mary F. Malley , Zhongping Shi
IPC分类号： A61K31/53 , C07D487/04
CPC分类号： C07D487/04
摘要： Processes are provided for selectively preparing novel stable crystalline salt forms, selectively and consistently, namely, preparing Form N-1 of the methanesulfonic acid salt, and Form N-1 and Form N-4 of the hydrochloric acid salt of the p38 kinase inhibitor 4-[[5-[(cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide. The processes preferably employ solvent systems including formic acid/acetone and formic acid/methylethyl ketone which produce crystals having suitable flow properties and desired particle size, and solvents such as N,N-dimethylformamide and N,N-dimethylacetamide may be employed as well.Novel Form N-1 crystals of the Form N-1 and Form N-4 crystals of the hydrochloride salt and Form N-1 crystals of the methanesulfonic acid salt of the above free base, pharmaceutical compositions containing such novel forms and a method of treating p38 kinase associated conditions, including rheumatoid arthritis are also provided.
摘要翻译：提供了选择性和一致地选择性制备新的稳定结晶盐形式的方法，即制备甲磺酸盐的N-1型，和p38激酶抑制剂4的盐酸盐的N-1和N-4型 - [[5 - [（环丙基氨基）羰基] -2-甲基苯基]氨基] -5-甲基-N-丙基吡咯并[2,1-f] [1,2,4]三嗪-6-甲酰胺。该方法优选使用包含甲酸/丙酮和甲酸/甲基乙基酮的溶剂体系，其产生具有合适流动性和所需粒径的晶体，并且也可以使用溶剂如N，N-二甲基甲酰胺和N，N-二甲基乙酰胺。上述游离碱的甲磺酸盐的盐酸盐形式的N-1型和N-4型结晶的新型N-1晶体和形式N-1晶体，含有这种新形式的药物组合物和治疗方法还提供p38激酶相关病症，包括类风湿性关节炎。

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