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1. 发明申请

WO2003105837A1 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：WO2003105837A1
公开(公告)日：2003-12-24
申请号：PCT/EP2003/006195
申请日：2003-06-12
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , CHEN, Guang-Pei , KAPA, Prasad, Koteswara , SUTTON, Paul, Allen
发明人： CHEN, Guang-Pei , KAPA, Prasad, Koteswara , SUTTON, Paul, Allen
IPC分类号： A61K31/405
CPC分类号： C07D209/24
摘要： The present invention provides calcium salts of indole derived statins of the formula (IA) wherein R 1 , is alkyl, cycloalkyl or aralkyl; R 2 , R 3 and R 4 are independently hydrogen, halogen or alkyl; R 5 and R 6 are independently hydrogen, halogen, alkyl, cycloalkyl, aralkyl, alkoxy or aralkoxy; and the hydroxyl group at the 3position is in the R-configuration and at the 5position 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 R 1 , is isopropyl, R 2 is fluorine and R 3 , R 4 R 5 and R 6 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：本发明提供式（IA）的吲哚衍生的他汀类钙盐，其中R 1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; 并且3位上的羟基处于R-构型，在5-构型中为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。

2. 发明申请

WO2007009080A2 PPARα/γ AGONISTS AND PROCESSES OF PREPARING 审中-公开
标题翻译：的PPARα/？激励和准备过程
公开(公告)号：WO2007009080A2
公开(公告)日：2007-01-18
申请号：PCT/US2006/027441
申请日：2006-07-12
申请人： NOVARTIS AG , NOVARTIS PHARMA GmbH , GARRETT, Christine, E. , CHEN, Guang-Pei , LEE, George Tien-San , JIANG, Xinglong , GIRGIS, Michael, J. , VIVELO, James, Anthony , SWERYDA-KRAWIEC, Beata , PAPOUTSAKIS, Dimitris , KARPINSKI, Piotr , KAPA, Prasad, Koteswara , SKORODINSKY, Ada
发明人： GARRETT, Christine, E. , CHEN, Guang-Pei , LEE, George Tien-San , JIANG, Xinglong , GIRGIS, Michael, J. , VIVELO, James, Anthony , SWERYDA-KRAWIEC, Beata , PAPOUTSAKIS, Dimitris , KARPINSKI, Piotr , KAPA, Prasad, Koteswara , SKORODINSKY, Ada
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 R 1 is hydrogen or optionally substituted alkyl, n is zero or 1 and m is 1; wherein R is H, halogen, optionally substituted C 1-6 alkyl or C 1-6 alkoxy; 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)NR 6 - in which R 6 is hydrogen, optionally substituted alkyl or cycloalkyl; or Q is -NR 6 -, -NR 5 C(O)NH- or -NR 5 C(O)O- in which R 5 is hydrogen, alkyl or aralkyl provided that p is not 1; wherein W is cycloalkyl, aryl or heterocyclyl; or W and R 6 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。

3. 发明申请

WO2006107964A2 PROCESS TO PREPARE ORGANIC COMPOUNDS 审中-公开
标题翻译：制备有机化合物的方法
公开(公告)号：WO2006107964A2
公开(公告)日：2006-10-12
申请号：PCT/US2006/012498
申请日：2006-04-04
申请人： NOVARTIS AG , NOVARTIS PHARMA GmbH , CHEN, Guang-Pei , JIANG, Xinglong , KAPA, Prasad Koteswara , MCKENNA, Joseph , SHIEH, Wen-Chung , XUE, Song
发明人： CHEN, Guang-Pei , JIANG, Xinglong , KAPA, Prasad Koteswara , MCKENNA, Joseph , SHIEH, Wen-Chung , XUE, Song
CPC分类号： C07D471/04
摘要： The present invention provides efficient and cost effective ways to prepare 6-phenethyl-octahydro-pyrrolo[2,3-c]pyridine and related compounds of the following formula (I).
摘要翻译：本发明提供了制备6-苯乙基 - 八氢 - 吡咯并[2,3-c]吡啶和下式（I）的相关化合物的有效和成本有效的方法。

4. 发明申请

WO2003064382A3 PROCESS FOR THE MANUFACTURE OF ORGANIC COMPOUNDS 审中-公开
公开(公告)号：WO2003064382A3
公开(公告)日：2003-08-07
申请号：PCT/EP2003/000804
申请日：2003-01-27
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , CHEN, Guang-Pei , KAPA, Prasad, Koteswara , LOESER, Eric, M. , BEUTLER, Ulrich , ZAUGG, Werner , GIRGIS, Michael, J.
发明人： CHEN, Guang-Pei , KAPA, Prasad, Koteswara , LOESER, Eric, M. , BEUTLER, Ulrich , ZAUGG, Werner , GIRGIS, Michael, J.
IPC分类号： 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.

5. 发明申请

WO2012064805A1 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-哌啶-1-基 - 吡啶-2-基）氨基] -7H-吡咯并[2,3-D]嘧啶-6-羧酸二甲酰胺的盐（S）及其制备方法
公开(公告)号：WO2012064805A1
公开(公告)日：2012-05-18
申请号：PCT/US2011/059890
申请日：2011-11-09
申请人： NOVARTIS AG , ASTEX THERAPEUTICS LTD , CALIENNI, John Vincent , CHEN, Guang-Pei , GONG, Baoqing , KAPA, Prasad Koteswara , SAXENA, Vishal
发明人： CALIENNI, John Vincent , CHEN, Guang-Pei , GONG, Baoqing , KAPA, Prasad Koteswara , SAXENA, Vishal
IPC分类号： C07D401/12 , A61K31/519 , A61P35/00
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。

6. 发明申请

WO2008119734A2 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：WO2008119734A2
公开(公告)日：2008-10-09
申请号：PCT/EP2008/053641
申请日：2008-03-27
申请人： NOVARTIS AG , BEBERNITZ, Gregory, Raymond , LEE, George, Tien-San , KAPA, Prasad, Koteswara , JIANG, Xinglong , SCHUSTER, Herbert, Franz , KIRMAN, Louise , BAJWA, Joginder, S. , CHEN, Guang-Pei , SCLAFANI, Joseph
发明人： BEBERNITZ, Gregory, Raymond , LEE, George, Tien-San , KAPA, Prasad, Koteswara , JIANG, Xinglong , SCHUSTER, Herbert, Franz , KIRMAN, Louise , BAJWA, Joginder, S. , CHEN, Guang-Pei , SCLAFANI, Joseph
CPC分类号： C07D513/04
摘要： The present invention relates to a process for the preparation of a (R)-3-Cycloalkyl-2-[4-(4-substitued amine-1-sulfonyl)-phenyl]-N-(5-substituent-yl-thiazolo[5,4- b ]pyridin-2-yl)-propionamide comprising: (a) taking a chiral compound a formula 6 and forming an acid chloride in situ; (b) reacting the acid chloride of step (a) with a compounds of formula 6a in the presence of a base to form a compound of formula 7; (c) reacting the compound of formula 7 with chlorosulfonic acid in an aprotic solvent to form a compound of formula 8 in situ; (d) reacting the compound formed in step (c) without isolation with a secondary amine; (e) recovering a compound of formula 10 in free form or in acid addition salt form,
摘要翻译：本发明涉及制备（R）-3-环烷基-2- [4-（4-取代的胺-1-磺酰基） - 苯基] -N-（5-取代基 - 噻唑并[ 包括：（a）获得式6的手性化合物并原位形成酰氯; （b）在碱的存在下使步骤（a）的酰氯与式6a的化合物反应以形成式7的化合物; （c）将式7的化合物与非对照溶剂中的氯磺酸反应以原位形成式8的化合物; （d）使步骤（c）中形成的化合物与仲胺不分离; （e）以游离形式或以酸加成盐形式回收式10的化合物，

7. 发明申请

WO2005000835A1 PROCESS FOR PREPARING INTERMEDIATES USEFUL TO PREPARE CERTAIN ANTIBACTERIAL N-FORMYL HYDROXYLAMINES 审中-公开
标题翻译：制备中间体的方法可用于制备某些抗菌N-甲酰羟胺
公开(公告)号：WO2005000835A1
公开(公告)日：2005-01-06
申请号：PCT/EP2004/006915
申请日：2004-06-25
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , SLADE, Joel , VIVELO, James, Anthony , CHEN, Guang-Pei , BAJWA, Joginder, Singh , PARKER, David, John
发明人： SLADE, Joel , VIVELO, James, Anthony , CHEN, Guang-Pei , BAJWA, Joginder, Singh , PARKER, David, John
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07C239/20 , C07C259/06 , C07D263/26 , C07F7/1892
摘要： The present invention is directed to a process for preparing intermediates that are useful to prepare certain antibacterial N -formyl hydroxylamine compounds which are peptide deformylase inhibitors.
摘要翻译：本发明涉及一种制备中间体的方法，其可用于制备作为肽去甲酰化酶抑制剂的某些抗菌N-甲酰基羟胺化合物。

8. 发明授权

EP1515717B8 CALCIUM SALTS OF INDOLE DERIVED STATINS 有权
标题翻译：他汀类药物的钙盐OFF吲哚
公开(公告)号：EP1515717B8
公开(公告)日：2009-12-16
申请号：EP03740234.4
申请日：2003-06-12
申请人： Novartis AG , Novartis Pharma GmbH
发明人： CHEN, Guang-Pei , KAPA, Prasad, Koteswara , SUTTON, Paul, Allen
IPC分类号： A61K31/405 , C07D209/24
CPC分类号： C07D209/24
摘要： The present invention provides calcium salts of indole derived statins of the formula (IA) 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 3position is in the R-configuration and at the 5position 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.

9. 发明公开

EP1912978A2 PPAR / AGONISTS AND PROCESSES OF PREPARING 审中-公开
标题翻译： PPAR激动剂及其制造方法
公开(公告)号：EP1912978A2
公开(公告)日：2008-04-23
申请号：EP06787361.2
申请日：2006-07-12
申请人： Novartis AG , NOVARTIS-PHARMA GMBH
发明人： GARRETT, Christine, E. , CHEN, Guang-Pei , LEE, George Tien-San , JIANG, Xinglong , GIRGIS, Michael, J. , VIVELO, James, Anthony , SWERYDA-KRAWIEC, Beata , PAPOUTSAKIS, Dimitris , KARPINSKI, Piotr , KAPA, Prasad, Koteswara , SKORODINSKY, Ada
IPC分类号： C07D413/12 , A61P3/06 , A61K31/422
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.

10. 发明授权

EP1515717B1 CALCIUM SALTS OF INDOLE DERIVED STATINS 有权
标题翻译：他汀类药物的钙盐OFF吲哚
公开(公告)号：EP1515717B1
公开(公告)日：2008-10-01
申请号：EP03740234.4
申请日：2003-06-12
申请人： Novartis AG , Novartis Pharma GmbH
发明人： CHEN, Guang-Pei , KAPA, Prasad, Koteswara , SUTTON, Paul, Allen
IPC分类号： A61K31/405 , C07D209/24
CPC分类号： C07D209/24

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