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1. 发明申请

WO2005061498A1 SUBSTITUTED 1H-PYRROLO[3,2-B, 3,2-C, AND 2,3-C]PYRIDINE-2-CARBOXAMIDES AND RELATED ANALOGS AS INHIBITORS OF CASEIN KINASE I EPSILON 审中-公开
标题翻译：取代的1H-吡咯[3,2-B，3,2-C和2,3-C]吡啶-2-羧酸和作为CASEIN KINASE I EPSILON的抑制剂的相关模拟物
公开(公告)号：WO2005061498A1
公开(公告)日：2005-07-07
申请号：PCT/US2004/040080
申请日：2004-12-01
申请人： AVENTIS PHARMACEUTICALS INC. , METZ, William, A. , HALLEY, Frank , DUTRUC-ROSSET, Gilles , CHOI-SLEDESKI, Yong, Mi , POLI, Gregory, B. , FINK, David, M. , DOERFLINGER, Gilles , HUANG, Bao-Guo , GELORMINI, Ann, Marie , GAMBOA, Juan, A. , GIOVANNI, Andrew , ROEHR, Joachim, E. , TSAY, Joseph, T. , CAMACHO, Fernando , HURST, William, J. , HARNISH, Stephen, W. , CHIANG, Yulin
发明人： METZ, William, A. , HALLEY, Frank , DUTRUC-ROSSET, Gilles , CHOI-SLEDESKI, Yong, Mi , POLI, Gregory, B. , FINK, David, M. , DOERFLINGER, Gilles , HUANG, Bao-Guo , GELORMINI, Ann, Marie , GAMBOA, Juan, A. , GIOVANNI, Andrew , ROEHR, Joachim, E. , TSAY, Joseph, T. , CAMACHO, Fernando , HURST, William, J. , HARNISH, Stephen, W. , CHIANG, Yulin
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The present invention discloses and claims substituted 1H-pyrrolo[3,2-b]pyridine-2-carboxamides, 1H-pyrrolo[3,2-c]pyridine-2-carboxamides and 1H-pyrrolo[2,3-c]pyridine-2-carboxamides (compounds of formula (I)) as inhibitors of human casein kinase I Epsilon, and methods of using said compounds of formula (I) for treating central nervous system diseases and disorders including mood disorders and sleep disorders. Pharmaceutical compositions comprising compounds of formula (I) and methods for the preparation of compounds of formula (I) are also disclosed and claimed.
摘要翻译：本发明公开并要求取代的1H-吡咯并[3,2-b]吡啶-2-甲酰胺，1H-吡咯并[3,2-c]吡啶-2-甲酰胺和1H-吡咯并[2,3-c]吡啶 -2-甲酰胺（式（I）化合物）作为人酪蛋白激酶I Epsilon的抑制剂，以及使用所述式（I）化合物治疗中枢神经系统疾病和病症（包括情绪障碍和睡眠障碍）的方法。还公开并要求保护包含式（I）化合物和制备式（I）化合物的方法的药物组合物。

2. 发明申请

WO2008109786A2 REGIO-SELECTIVE ULLMANN SYNTHESIS OF 4-BROMO-3-METHYL-5-PROPOXY-THIOPHENE-2-CARBOXYLIC ACID 审中-公开
标题翻译： 4-BROMO-3-甲基-5-丙氧基-2-羟基乙酸的选择性ULLMANN合成
公开(公告)号：WO2008109786A2
公开(公告)日：2008-09-12
申请号：PCT/US2008/056112
申请日：2008-03-07
申请人： SANOFI-AVENTIS , AYERS, Timothy A. , GELORMINI, Ann Marie , SHAY, John J., Jr. , SLEDESKI, Adam W. , YU, Yong
发明人： AYERS, Timothy A. , GELORMINI, Ann Marie , SHAY, John J., Jr. , SLEDESKI, Adam W. , YU, Yong
CPC分类号： C07D333/38
摘要： This invention is directed to a two step regio-selective Ullmann synthesis of 4-bromo-3- methyl-5-propoxy-thiophene-2-carboxylic acid compound of formula 16 comprising the steps of brominating 3-methyl-thiophene-2-carboxylic acid to yield 4,5-dibromo-3-methyl- thiophene-2-carboxylic acid in appropriate bromination organic solvent, and then effecting the selective Ullmann coupling of the 4,5-dibromo-3-methyl-thiophene-2-carboxylic cid with alkali metal propoxide salt using copper catalyst in propanol to yield the compound of formula 16.
摘要翻译：本发明涉及式16的4-溴-3-甲基-5-丙氧基 - 噻吩-2-羧酸化合物的两步区域选择性Ullmann合成，包括以下步骤：将3-甲基 - 噻吩-2-羧酸酸，得到4,5-二溴-3-甲基 - 噻吩-2-羧酸在合适的溴化有机溶剂中，然后进行4,5-二溴-3-甲基 - 噻吩-2-羧酸的选择性Ullmann偶联与丙醇中使用铜催化剂的碱金属丙醇盐反应得到式16化合物。

3. 发明申请

WO2008109786A3 REGIO-SELECTIVE ULLMANN SYNTHESIS OF 4-BROMO-3-METHYL-5-PROPOXY-THIOPHENE-2-CARBOXYLIC ACID 审中-公开
标题翻译：选择性雷蒙曼合成4-溴-3-甲基-5-丙氧基噻吩-2-羧酸
公开(公告)号：WO2008109786A3
公开(公告)日：2008-12-11
申请号：PCT/US2008056112
申请日：2008-03-07
申请人： SANOFI AVENTIS , AYERS TIMOTHY A , GELORMINI ANN MARIE , SHAY JOHN J JR , SLEDESKI ADAM W , YU YONG
发明人： AYERS TIMOTHY A , GELORMINI ANN MARIE , SHAY JOHN J JR , SLEDESKI ADAM W , YU YONG
IPC分类号： C07D333/38
CPC分类号： C07D333/38
摘要： This invention is directed to a two step regio-selective Ullmann synthesis of 4-bromo-3- methyl-5-propoxy-thiophene-2-carboxylic acid compound of formula 16 comprising the steps of brominating 3-methyl-thiophene-2-carboxylic acid to yield 4,5-dibromo-3-methyl- thiophene-2-carboxylic acid in appropriate bromination organic solvent, and then effecting the selective Ullmann coupling of the 4,5-dibromo-3-methyl-thiophene-2-carboxylic cid with alkali metal propoxide salt using copper catalyst in propanol to yield the compound of formula 16.
摘要翻译：本发明涉及式16的4-溴-3-甲基-5-丙氧基 - 噻吩-2-羧酸化合物的两步区域选择性乌尔曼合成，该方法包括溴化3-甲基 - 噻吩-2-羧酸在合适的溴化有机溶剂中生成4,5-二溴-3-甲基噻吩-2-羧酸，然后进行4,5-二溴-3-甲基噻吩-2-羧酸cid的选择性乌尔曼偶联与碱金属丙氧化物盐在丙醇中使用铜催化剂反应，得到式16化合物。

4. 发明申请

WO2008121669A1 4-BROMO-3-METHYL-5-PROPOXYTHIOPHENE-2-CARBOXYLIC ACID 2,5-DIOXO-PYRROLIDIN-1-YL ESTER, ITS REGIO-SPECIFIC SYNTHESIS AND INTERMEDIATE THERETO 审中-公开
标题翻译： 4-溴-3-甲基-5-丙氧基-2-羟基乙酸2,5-二氧代吡咯烷-1-酮，其特异性合成和中间体
公开(公告)号：WO2008121669A1
公开(公告)日：2008-10-09
申请号：PCT/US2008/058346
申请日：2008-03-27
申请人： SANOFI-AVENTIS , GELORMINI, Ann, Marie , SHAY, John, Josephe, Jr. , SLEDESKI, Adam, W.
发明人： GELORMINI, Ann, Marie , SHAY, John, Josephe, Jr. , SLEDESKI, Adam, W.
IPC分类号： C07D409/06 , C07D409/12
CPC分类号： C07D409/06 , C07D409/12
摘要： The present invention is directed to 4-bromo-3-methyl-5-propoxythiophene-2-carboxylic acid 2,5-dioxo-pyrrolidin-1-yl ester, and intermediate, 3-methyl-5-propoxythiophene-2-carboxylic acid 2,5-dioxo-pyrrolidin-1-yl ester, thereto. The present invention is also directed to the regio-specific synthesis of 4-bromo-3-methyl-5-propoxythiophene-2-carboxylic acid 2,5-dioxo-pyrrolidin-1-yl ester compound comprising the steps of iodinating 3-methyl-thiophene with an iodinating agent in the presence of a strong base in an non-protic polar or hydrocarbon solvent to yield 2-iodo-4-methylthiophene; Ullmann coupling the 2-iodo-4-methylthiophene with an alkali metal propoxide salt using a copper catalyst in propanol to yield 4-methyl-2-propoxythiophene; coupling the 4-methyl-2-propoxythiophene with CO2 using strong base in an non-protic polar or hydrocarbon solvent to yield 3 methyl-5-propoxy-thiophene-2-carboxylic acid; esterifying the 3 methyl-5-propoxy-thiophene-2-carboxylic acid with N hydroxysuccinimide in the presence of a coupling agent in an non-protic polar, hydrocarbon or halohydrocarbon solvent to yield 3-methyl-5-propoxythiophene-2-carboxylic acid 2,5 dioxo-pyrrolidin-1-yl ester; and brominating the 3-methyl-5-propoxythiophene-2-carboxylic acid 2,5 dioxo-pyrrolidin-1-yl ester with a brominating agent in an inert solvent to yield 4-bromo-3-methyl-5-propoxythiophene-2-carboxylic acid 2,5-dioxo-pyrrolidin-1-yl ester.
摘要翻译：本发明涉及4-溴-3-甲基-5-丙氧基噻吩-2-羧酸2,5-二氧代 - 吡咯烷-1-基酯和中间体3-甲基-5-丙氧基噻吩-2-甲酸 2,5-二氧代 - 吡咯烷-1-基酯。本发明还涉及4-溴-3-甲基-5-丙氧基噻吩-2-羧酸2,5-二氧代 - 吡咯烷-1-基酯化合物的区域特异性合成，包括以下步骤：将3-甲基 - 噻吩与碘化剂在非质子极性或烃溶剂中在强碱存在下反应，得到2-碘-4-甲基噻吩; Ullmann使用铜催化剂在丙醇中将2-碘-4-甲基噻吩与碱金属丙醇盐偶联，得到4-甲基-2-丙氧基噻吩; 在非质子极性或烃溶剂中使用强碱将4-甲基-2-丙氧基噻吩与CO 2偶联，得到3甲基-5-丙氧基 - 噻吩-2-羧酸; 在非质子极性，烃或卤代烃溶剂中，在偶联剂存在下，用N羟基琥珀酰亚胺酯化3-甲基-5-丙氧基 - 噻吩-2-羧酸，得到3-甲基-5-丙氧基噻吩-2-羧酸 2,5-二氧代 - 吡咯烷-1-基酯; 并用溴化剂在惰性溶剂中溴化3-甲基-5-丙氧基噻吩-2-羧酸2,5二氧代 - 吡咯烷-1-基酯，得到4-溴-3-甲基-5-丙氧基噻吩-2-基酯羧酸2,5-二氧代 - 吡咯烷-1-基酯。

5. 发明申请

WO2008121666A1 USE OF 4-BROMO-3-METHYL-5-PROPOXYTHIOPHENE-2-CARBOXYLIC ACID 2,5-DIOXO-PYRROLIDIN-1-YL ESTER FOR PREPARING THE TRYPTASE INHIBITOR [4-(5-AMINOMETHYL-2-FLUORO-PHENYL)-PIPERIDIN-1-YL]-(4-BROMO-3-METHYL-5-PROPOXY-THIOPHEN-2-YL)-METHANONE 审中-公开
标题翻译： 4-溴-3-甲基-5-丙氧基-2-羧酸的制备用于制备TRYPTASE抑制剂[4-（5-氨基乙基-2-氟 - 苯基）] - 的二氧杂环戊烯-2-酮哌啶-1-基] - （4-溴-3-甲基-5-丙氧基 - 噻吩-2-基） - 甲
公开(公告)号：WO2008121666A1
公开(公告)日：2008-10-09
申请号：PCT/US2008/058341
申请日：2008-03-27
申请人： SANOFI-AVENTIS , GELORMINI, Ann, Marie , SLEDESKI, Adam, W. , SHAY, John, Joseph, Jr.
发明人： GELORMINI, Ann, Marie , SLEDESKI, Adam, W. , SHAY, John, Joseph, Jr.
IPC分类号： C07D409/06
CPC分类号： C07D409/06
摘要： This invention is directed to a five step regio-specific synthesis of 4-bromo-3-methyl-5-propoxy-thiophene-2-carboxylic acid compound of formula 16 comprising the steps of acetalating 3-methyl-thiophene-2-carbaldehyde in an alcohol solvent; iodinating the acetalated 3-methyl-thiophene-2-carbaldehyde in an non-protic polar or hydrocarbon solvent to yield the corresponding iodinated and acetalated 3-methyl-thiophene-2-carbaldehyde product; treating the iodinated and acetalated product with water to yield the corresponding 5-iodo-3-methyl-thiophene-2-carbaldehyde; oxidizing the 5-iodo-3-methyl-thiophene-2-carbaldehyde to the corresponding 5-iodo-3-methyl-thiophene-2-carboxylic acid in ketone solvent; Ullmann coupling of the 5-iodo-3-methyl-thiophene-2-carboxylic acid with alkali metal propoxide salt using a copper catalyst in propanol to yield 3-methyl-5-propoxy-thiophene-2-carboxylic acid; esterifying 3-methyl-5-propoxy-thiophene-2-carboxylic acid to yield the corresponding alkyl 3-methyl-5-propoxy-thiophene-2-carboxylate; brominating the 3-methyl-5-propoxy-thiophene-2-carboxylic acid to yield the corresponding alkyl 4-bromo-3-methyl-5-propoxy-thiophene-2-carboxylate; and basic hydrolyzing the alkyl 4-bromo-3-methyl-5-propoxy-thiophene-2-carboxylate with base to yield 4-bromo-3-methyl-5-propoxy-thiophene-2-carboxylic acid.
摘要翻译：本发明涉及式16的4-溴-3-甲基-5-丙氧基 - 噻吩-2-羧酸化合物的五步区域特异性合成，包括以下步骤：将3-甲基 - 噻吩-2-甲醛缩醛醇溶剂; 在非质子极性或烃溶剂中碘化缩醛化的3-甲基 - 噻吩-2-甲醛，得到相应的碘化和缩醛化的3-甲基 - 噻吩-2-甲醛产物; 用水处理碘化和缩醛产物，得到相应的5-碘-3-甲基 - 噻吩-2-甲醛; 在酮溶剂中将5-碘-3-甲基 - 噻吩-2-甲醛氧化成相应的5-碘-3-甲基 - 噻吩-2-羧酸; 使用铜催化剂在丙醇中的5-碘-3-甲基 - 噻吩-2-羧酸与碱金属丙醇盐的Ullmann偶联，得到3-甲基-5-丙氧基 - 噻吩-2-羧酸; 酯化3-甲基-5-丙氧基 - 噻吩-2-羧酸，得到相应的3-甲基-5-丙氧基 - 噻吩-2-甲酸烷基酯; 溴化3-甲基-5-丙氧基 - 噻吩-2-羧酸，得到相应的4-溴-3-甲基-5-丙氧基 - 噻吩-2-羧酸烷基酯; 并用碱碱性水解4-溴-3-甲基-5-丙氧基 - 噻吩-2-羧酸烷基酯，得到4-溴-3-甲基-5-丙氧基 - 噻吩-2-羧酸。

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