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1. 发明授权

US06835838B2 Process for the manufacture of organic compounds 有权
标题翻译：制备有机化合物的方法
公开(公告)号：US06835838B2
公开(公告)日：2004-12-28
申请号：US10350615
申请日：2003-01-24
申请人： Guang-Pei Chen , Prasad Koteswara Kapa , Eric M. Loeser , Ulrich Beutler , Werner Zaugg , Michael John Girgis
发明人： Guang-Pei Chen , Prasad Koteswara Kapa , Eric M. Loeser , Ulrich Beutler , Werner Zaugg , Michael John Girgis
IPC分类号： C07D21554
CPC分类号： C07D405/06 , C07D215/14
摘要： A method for preparing an alkali metal salt comprising: (a) condensing a disilyloxydiene with an aldehyde in the presence of a titanium (IV) catalyst in an inert solvent to form a 5(S)-hydroxy-3-ketoester; (b) reducing the 5(S)-hydroxy-3-ketoester to a 3(R),5(S)-dihydroxyester in the presence of a di(lower alkyl)methoxyborane; and (c) hydrolyzing the 3(R),5(S)-dihydroxyester in the presence of an aqueous base to form an alkali metal salt.
摘要翻译：一种制备碱金属盐的方法，包括：（a）在惰性溶剂中，在钛（IV）催化剂的存在下，使二脱氧二烯与醛缩合形成5（S） - 羟基-3-酮酯; （b）在二（低级烷基）甲氧基硼烷存在下将5（S） - 羟基-3-酮酯还原成3（R），（S） - 二羟基酯; 和（c）在碱水溶液存在下水解3（R），5（S） - 二羟基酯以形成碱金属盐。

2. 发明申请

US20090299065A1 PROCESS FOR THE MANUFACTURE OF ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物的制造方法
公开(公告)号：US20090299065A1
公开(公告)日：2009-12-03
申请号：US12497001
申请日：2009-07-02
申请人： Guang-Pei Chen , Prasad Koteswara Kapa , Eric M. Loeser , Ulrich Beutler , Werner Zaugg , Michael John Girgis
发明人： Guang-Pei Chen , Prasad Koteswara Kapa , Eric M. Loeser , Ulrich Beutler , Werner Zaugg , Michael John Girgis
IPC分类号： C07D239/42 , C07D215/14 , C07D213/55
CPC分类号： C07D405/06 , C07D215/14
摘要： A method for preparing an alkali metal salt comprising: (a) condensing a disilyloxydiene with an aldehyde in the presence of a titanium (IV) catalyst in an inert solvent to form a 5(S)-hydroxy-3-ketoester; (b) reducing the 5(S)-hydroxy-3-ketoester to a 3(R),5(S)-dihydroxyester in the presence of a di(lower alkyl)methoxyborane; and (c) hydrolyzing the 3(R),5(S)-dihydroxyester in the presence of an aqueous base to form an alkali metal salt.
摘要翻译：一种制备碱金属盐的方法，包括：（a）在惰性溶剂中，在钛（IV）催化剂的存在下，将二硅氧烷与醛缩合形成5（S） - 羟基-3-酮酯; （b）在二（低级烷基）甲氧基硼烷存在下将5（S） - 羟基-3-酮酯还原成3（R），（S） - 二羟基酯; 和（c）在碱水溶液存在下水解3（R），5（S） - 二羟基酯以形成碱金属盐。

3. 发明申请

US20100249204A1 CALCIUM SALTS OF INDOLE DERIVED STATINS 审中-公开
标题翻译：单位衍生统计的钙盐
公开(公告)号：US20100249204A1
公开(公告)日：2010-09-30
申请号：US12768991
申请日：2010-04-28
申请人： Guang-Pei Chen , Prasad Koteswara Kapa , Paul Allen Sutton
发明人： Guang-Pei Chen , Prasad Koteswara Kapa , Paul Allen Sutton
IPC分类号： A61K31/404 , C07D209/18 , A61P9/00 , A61P9/10
CPC分类号： C07D209/24
摘要： The present invention provides calcium salts of indole derived statins of the formula wherein R1 is alkyl, cycloalkyl or aralkyl; R2, R3 and R4 are independently hydrogen, halogen or alkyl; R5 and R6 are independently hydrogen, halogen, alkyl, cycloalkyl, aralkyl, alkoxy or aralkoxy; and the hydroxyl group at the 3-position is in the R-configuration and at the 5-position in the S-configuration; or an enantiomer thereof; or a hydrate thereof; as obtainable by the methods of the present invention. More specifically, the invention provides a calcium salt of formula IA wherein R1 is isopropyl, R2 is fluorine and R3, R4, R5 and R6 are hydrogen, designated herein as Fluvastatin calcium, in a highly crystalline form. Furthermore, the present invention is directed to methods for the preparation of the crystalline Fluvastatin calcium, and to pharmaceutical compositions comprising the crystalline form.
摘要翻译：本发明提供下式的吲哚衍生的他汀类钙盐：其中R1是烷基，环烷基或芳烷基; R2，R3和R4独立地是氢，卤素或烷基; R5和R6独立地是氢，卤素，烷基，环烷基，芳烷基，烷氧基或芳烷氧基; 3位的羟基为R构型，S构型为5位; 或其对映体; 或其水合物; 如通过本发明的方法可获得的。更具体地，本发明提供式IA的钙盐，其中R 1是异丙基，R 2是氟，并且R 3，R 4，R 5和R 6是氢，在本文中称为氟伐他汀钙，为高度结晶形式。此外，本发明涉及制备结晶氟伐他汀钙的方法以及包含结晶形式的药物组合物。

4. 发明授权

US09193732B2 Salt(s) of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-D]pyrimidine-6-carboxylic acid dimethylamide and processes of making thereof 有权
标题翻译： 7-环戊基-2-（5-哌嗪-1-基 - 吡啶-2-基氨基）-7H-吡咯并[2,3-D]嘧啶-6-甲酸二甲基酰胺的盐及其制备方法
公开(公告)号：US09193732B2
公开(公告)日：2015-11-24
申请号：US13882353
申请日：2011-11-09
申请人： John Vincent Calienni , Guang-Pei Chen , Baoqing Gong , Prasad Koteswara Kapa , Vishal Saxena
发明人： John Vincent Calienni , Guang-Pei Chen , Baoqing Gong , Prasad Koteswara Kapa , Vishal Saxena
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00 , C07D401/12 , C07C55/10 , C07D213/74 , C07D213/73
CPC分类号： C07D487/04 , C07C55/10 , C07D213/73 , C07D213/74 , C07D239/42 , C07D401/12
摘要： This invention relates to (1) process of making 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and salts thereof; (2) novel salt(s) of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide; (3) pharmaceutical compositions comprising the same; and (4) methods of treatment using the same.
摘要翻译：本发明涉及（1）制备7-环戊基-2-（5-哌嗪-1-基 - 吡啶-2-基氨基）-7H-吡咯并[2,3-d]嘧啶-6-甲酸二甲基酰胺和的盐; （2）7-环戊基-2-（5-哌嗪-1-基 - 吡啶-2-基氨基）-7H-吡咯并[2,3-d]嘧啶-6-甲酸二甲基酰胺的新型盐; （3）包含其的药物组合物; 和（4）使用其的治疗方法。

5. 发明申请

US20080221336A1 Pparalpha/Gamma Agonists and Processes of Preparing 审中-公开
标题翻译： Pparalpha / Gamma激动剂和制备方法
公开(公告)号：US20080221336A1
公开(公告)日：2008-09-11
申请号：US11995261
申请日：2006-07-12
申请人： Christine E. Garrett , Guang-Pei Chen , George Tien-San Lee , Xinglong Jiang , Michael J. Girgis , James Anthony Vivelo , Beata Sweryda-Krawiec , Dimitris Papoutsakis , Piotr Karpinski , Prasad Koteswara Kapa , Ada Skorodinsky
发明人： Christine E. Garrett , Guang-Pei Chen , George Tien-San Lee , Xinglong Jiang , Michael J. Girgis , James Anthony Vivelo , Beata Sweryda-Krawiec , Dimitris Papoutsakis , Piotr Karpinski , Prasad Koteswara Kapa , Ada Skorodinsky
IPC分类号： C07D263/32
CPC分类号： C07D413/12
摘要： This invention provides a method for preparing compounds having the structure [Formula (I)] wherein L is [Formula (A)] or [Formula (B)] in which R1 is hydrogen or optionally substituted alkyl, n is zero or 1 and m is 1; wherein R is H, halogen, optionally substituted C1-6alkyl or C1-6alkoxy; wherein Z is a bond, O or S; wherein p is an integer from 1 to 5; wherein Q is a bond provided that Z is not a bond when p is 1; or Q is O, S or —C(O)NR6— in which R6 is hydrogen, optionally substituted alkyl or cycloalkyl; or Q is —NR6—, —NR5C(O)NH— or —NR5C(O)O— in which R5 is hydrogen, alkyl or aralkyl provided that p is not 1; wherein W is cycloalkyl, aryl or heterocyclyl; or W and R6 form a 9- to 10-membered bicyclic ring, which may be optionally substituted or may contain oxygen, nitrogen or sulfur.
摘要翻译：本发明提供了制备具有结构[式（I）]的化合物的方法，其中L是[式（A）]或[式（B）]，其中R 1是氢或任选取代的烷基，n为0或1，m为1; 其中R是H，卤素，任选取代的C 1-6烷基或C 1-6烷氧基; 其中Z是键，O或S; 其中p是1至5的整数; 其中Q是键，条件是当p是1时Z不是键; 或Q是O，S或-C（O）NR 6 - ，其中R 6是氢，任选取代的烷基或环烷基; 或Q是-NR 6 - ， - NR 5 C（O）NH-或-NR 5 C（O）O-，其中 R 5是氢，烷基或芳烷基，条件是p不是1; 其中W是环烷基，芳基或杂环基; 或W和R 6形成9至10元双环，其可任选被取代或可含有氧，氮或硫。

6. 发明申请

US20110251171A1 HETEROCYCLIC COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：杂环化合物和使用方法
公开(公告)号：US20110251171A1
公开(公告)日：2011-10-13
申请号：US13166663
申请日：2011-06-22
申请人： Andrew Thomas Bach , Prasad Koteswara Kapa , George Tien-San Lee , Eric M. Loeser , Michael Lloyd Sabio , James Lawrence Stanton , Thalaththani Ralalage Vedananda
发明人： Andrew Thomas Bach , Prasad Koteswara Kapa , George Tien-San Lee , Eric M. Loeser , Michael Lloyd Sabio , James Lawrence Stanton , Thalaththani Ralalage Vedananda
IPC分类号： A61K31/397 , A61K31/5415 , A61K31/4725 , C07D417/12 , A61K31/422 , A61K31/404 , A61K31/427 , A61K31/40 , A61P3/10 , A61K31/538 , C07D401/12 , C07D411/12 , C07D413/12 , C07D209/30 , C07D207/48 , C07D205/04 , A61P9/12 , A61P9/00 , A61P11/00 , A61P27/02 , A61P25/28 , A61P1/00 , A61P17/00 , A61P3/06
CPC分类号： C07D205/04 , C07D207/16 , C07D209/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： Compounds of the formula provide pharmacological agents which are potent agonists of Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases, ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X. Preferred are the compounds of the invention which are dual agonists of PPARα and PPARγ receptors.
摘要翻译：配方的化合物提供作为过氧化物酶体增殖物激活受体（PPARs）的有效激动剂的药理学试剂。因此，本发明的化合物可用于治疗由哺乳动物中的PPAR受体活性介导的病症。这些病症包括血脂异常，高脂血症，高胆固醇血症，动脉粥样硬化，高甘油三酯血症，心力衰竭，心肌梗死，血管疾病，心血管疾病，高血压，肥胖症，炎症，关节炎，癌症，阿尔茨海默病，皮肤病，呼吸系统疾病，眼科疾病，炎症性肠病，溃疡性结肠炎和克罗恩病。本发明的化合物在哺乳动物中特别可用作降血糖药，用于治疗和预防葡萄糖耐量降低，高血糖症和胰岛素抵抗等疾病，如1型和2型糖尿病，以及X综合征。是PPARα和PPARγ受体的双重激动剂的本发明化合物。

7. 发明申请

US20090118160A1 HETEROCYCLIC COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：杂环化合物和使用方法
公开(公告)号：US20090118160A1
公开(公告)日：2009-05-07
申请号：US12349239
申请日：2009-01-06
申请人： Andrew Thomas Bach , Prasad Koteswara Kapa , George Tien-San Lee , Eric M. Loeser , Michael Lloyd Sabio , James Lawrence Stanton , Thalaththani Ralalage Vedananda
发明人： Andrew Thomas Bach , Prasad Koteswara Kapa , George Tien-San Lee , Eric M. Loeser , Michael Lloyd Sabio , James Lawrence Stanton , Thalaththani Ralalage Vedananda
IPC分类号： A61K38/28 , C07D209/04 , A61K31/404 , C07D413/02 , A61K31/422 , C07D205/04 , A61K31/397 , A61P9/04 , C07D403/02 , A61P9/00 , C07D401/02 , A61K31/4709 , A61P9/12 , A61K31/423 , A61P19/02 , A61K31/538 , C07D417/02 , A61K31/427 , C07D263/30 , A61P3/04 , A61P35/00 , A61P25/28 , A61P1/00 , A61P3/10 , A61P17/00 , A61P11/00 , A61P27/02
CPC分类号： C07D205/04 , C07D207/16 , C07D209/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： Compounds of the formula provide pharmacological agents which are potent agonists of Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases, ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X. Preferred are the compounds of the invention which are dual agonists of PPARα and PPARγ receptors.
摘要翻译：配方的化合物提供作为过氧化物酶体增殖物激活受体（PPARs）的有效激动剂的药理学试剂。因此，本发明的化合物可用于治疗由哺乳动物中的PPAR受体活性介导的病症。这些病症包括血脂异常，高脂血症，高胆固醇血症，动脉粥样硬化，高甘油三酯血症，心力衰竭，心肌梗死，血管疾病，心血管疾病，高血压，肥胖症，炎症，关节炎，癌症，阿尔茨海默病，皮肤病，呼吸系统疾病，眼科疾病，炎症性肠病，溃疡性结肠炎和克罗恩病。本发明的化合物在哺乳动物中特别可用作降血糖药，用于治疗和预防葡萄糖耐量降低，高血糖症和胰岛素抵抗等疾病，如1型和2型糖尿病，以及X综合征。是本发明的化合物，它们是PPARα和PPARγ受体的双重激动剂。

8. 发明授权

US09868739B2 Salt(s) of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and processes of making thereof 有权
公开(公告)号：US09868739B2
公开(公告)日：2018-01-16
申请号：US14887790
申请日：2015-10-20
申请人： John Vincent Calienni , Guang-Pei Chen , Baoqing Gong , Prasad Koteswara Kapa , Vishal Saxena
发明人： John Vincent Calienni , Guang-Pei Chen , Baoqing Gong , Prasad Koteswara Kapa , Vishal Saxena
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00 , C07D401/12 , C07C55/10 , C07D213/74 , C07D213/73 , C07D239/42
CPC分类号： C07D487/04 , C07C55/10 , C07D213/73 , C07D213/74 , C07D239/42 , C07D401/12
摘要： This invention relates to (1) process of making 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and salt(s) thereof; (2) novel salt(s) of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide; (3) pharmaceutical compositions comprising the same; and (4) methods of treatment using the same.

9. 发明申请

US20160039832A1 SALT(S) OF 7-CYCLOPENTYL-2-(5-PIPERAZIN-1-YL-PYRIDIN-2-YLAMINO)-7H-PYRROLO[2,3-D]PYRIMIDINE-6-CARBOXYLIC ACID DIMETHYLAMIDE AND PROCESSES OF MAKING THEREOF 审中-公开
标题翻译： 7-环戊基-2-（5-哌嗪-1-基 - 吡啶-2-基）氨基] -7H-吡咯并[2,3-d]嘧啶-6-羧酸二甲基胺的盐（S）及其制备方法
公开(公告)号：US20160039832A1
公开(公告)日：2016-02-11
申请号：US14887790
申请日：2015-10-20
申请人： John Vincent Calienni , Guang-Pei Chen , Baoqing Gong , Prasad Koteswara Kapa , Vishal Saxena
发明人： John Vincent Calienni , Guang-Pei Chen , Baoqing Gong , Prasad Koteswara Kapa , Vishal Saxena
IPC分类号： C07D487/04 , C07D239/42 , C07D213/73 , C07C55/10
CPC分类号： C07D487/04 , C07C55/10 , C07D213/73 , C07D213/74 , C07D239/42 , C07D401/12
摘要： This invention relates to (1) process of making 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and salt(s) thereof; (2) novel salt(s) of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-carboxylic acid dimethylamide; (3) pharmaceutical compositions comprising the same; and (4) methods of treatment using the same.
摘要翻译：本发明涉及（1）制备7-环戊基-2-（5-哌嗪-1-基 - 吡啶-2-基氨基）-7H-吡咯并[2,3-d]嘧啶-6-甲酸二甲基酰胺和其盐; （2）7-环戊基-2-（5-哌嗪-1-基 - 吡啶-2-基氨基）-7H-吡咯并[2,3-d]嘧啶 - 羧酸二甲基酰胺的新型盐; （3）包含其的药物组合物; 和（4）使用其的治疗方法。

10. 发明申请

US20150099760A1 SALT(S) OF 7-CYCLOPENTYL-2-(5-PIPERAZIN-1-YL-PYRIDIN-2-YLAMINO)-7H-PYRROLO[2,3-D]PYRIMIDINE-6-CARBOXYLIC ACID DIMETHYLAMIDE AND PROCESSES OF MAKING THEREOF 审中-公开
标题翻译： 7-环戊基-2-（5-哌嗪-1-基 - 吡啶-2-基）氨基] -7H-吡咯并[2,3-d]嘧啶-6-羧酸二甲基胺的盐（S）及其制备方法
公开(公告)号：US20150099760A1
公开(公告)日：2015-04-09
申请号：US14307901
申请日：2014-06-18
申请人： John Vincent Calienni , Guang-Pei Chen , Baoqing Gong , Prasad Koteswara Kapa , Vishal Saxena
发明人： John Vincent Calienni , Guang-Pei Chen , Baoqing Gong , Prasad Koteswara Kapa , Vishal Saxena
IPC分类号： C07D487/04 , C07D213/73 , C07C55/10
CPC分类号： C07D487/04 , C07C55/10 , C07D213/73 , C07D213/74 , C07D239/42 , C07D401/12
摘要： This invention relates to (1) process of making 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and salts thereof; (2) novel salt(s) of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide; (3) pharmaceutical compositions comprising the same; and (4) methods of treatment using the same.
摘要翻译：本发明涉及（1）制备7-环戊基-2-（5-哌嗪-1-基 - 吡啶-2-基氨基）-7H-吡咯并[2,3-d]嘧啶-6-甲酸二甲基酰胺和的盐; （2）7-环戊基-2-（5-哌嗪-1-基 - 吡啶-2-基氨基）-7H-吡咯并[2,3-d]嘧啶-6-甲酸二甲基酰胺的新型盐; （3）包含其的药物组合物; 和（4）使用其的治疗方法。

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