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1. 发明申请

WO2008125518A2 PROCESS FOR THE PREPARATION OF PIPERAZINE BENZOTHIAZOLES 审中-公开
标题翻译：制备哌嗪苯并噻唑的方法
公开(公告)号：WO2008125518A2
公开(公告)日：2008-10-23
申请号：PCT/EP2008/054055
申请日：2008-04-03
申请人： LABORATOIRES SERONO SA , SCHIAVO, Cesare , POMA, Marco , NADLER, William
发明人： SCHIAVO, Cesare , POMA, Marco , NADLER, William
IPC分类号： C07D295/18 , C07D417/06
CPC分类号： C07D417/06 , C07D295/185
摘要： The present invention discloses a process for the preparation of compounds of formula (I) where the groups and symbols are as defined in the description, said process comprising a) reacting a benzothiazol-2-ylacetonitrile bearing group R 1 with an activated pyrimidine, in a reaction medium; then treating the obtained derivative in said reaction medium with a weak base anion exchange resin; then, after removing said resin and isolating the reaction product, reacting it with a substituted piperazine -benzyl-alkyloxy. The final product can optionally be salified. The invention also relates to the preparation of N-acyl-substituted piperazine -benzyl- alkyloxy, comprising treating a bromide-alkyl-phenyl-4-ester wherein the ester group is selected from COOMe or COOEt with DIBAL to obtain (4- bromomethyl-phenyl)-methanol and reacting the latter with 1-piperazin-1-yl-acyl. The processes here disclosed present a number of advantages, for example, higher yield and purity of final product. Moreover, in case of piperazine group bearing hydrogen or an acyl group in position 4, the preparation of the intermediate substituted piperazine -benzyl-alkyloxy (V) need no protection/deprotection steps.
摘要翻译：本发明公开了一种制备式（I）化合物的方法，其中基团和符号如说明书中所定义，所述方法包括a）使具有基团R 1的苯并噻唑-2-基乙腈/ >与活化的嘧啶反应; 然后用弱碱阴离子交换树脂处理所得反应介质中的衍生物; 然后，在除去所述树脂并分离反应产物后，与取代的哌嗪 - 苄基 - 烷氧基反应。最终产品可以任选地成盐。本发明还涉及N-酰基取代的哌嗪 - 苄基 - 烷氧基的制备，包括用DIBAL处理酯基选自COOMe或COOEt的溴化烷基苯基-4-酯，得到（4-溴甲基 - 苯基） - 甲醇，并将其与1-哌嗪-1-基 - 酰基反应。这里公开的方法具有许多优点，例如最终产物的较高产率和纯度。此外，在位置4具有氢或酰基的哌嗪基的情况下，中间体取代的哌嗪 - 苄基 - 烷氧基（V）的制备不需要保护/脱保护步骤。

2. 发明申请

WO2003035077A1 N-SUBSTITUTED HYDROXYPYRIMIDINONE CARBOXAMIDE INHIBITORS OF HIV INTEGRASE 审中-公开
标题翻译：艾滋病毒整合剂的N-取代羟基嘧啶酮羧酰胺抑制剂
公开(公告)号：WO2003035077A1
公开(公告)日：2003-05-01
申请号：PCT/GB2002/004753
申请日：2002-10-21
申请人： ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI SPA , CRESCENZI, Benedetta , GARDELLI, Cristina , MURAGLIA, Ester , NIZI, Emanuela , ORVIETO, Federica , PACE, Paola , PESCATORE, Giovanna , PETROCCHI, Alessia , POMA, Marco , ROWLEY, Michael , SCARPELLI, Rita , SUMMA, Vincenzo
发明人： CRESCENZI, Benedetta , GARDELLI, Cristina , MURAGLIA, Ester , NIZI, Emanuela , ORVIETO, Federica , PACE, Paola , PESCATORE, Giovanna , PETROCCHI, Alessia , POMA, Marco , ROWLEY, Michael , SCARPELLI, Rita , SUMMA, Vincenzo
IPC分类号： A61K31/515
CPC分类号： C07D239/557 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D413/04 , C07D413/10 , C07D413/12 , C07D417/04 , C07D513/04
摘要： N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula (I): are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R 1 , R 2 , R 3 and R 4 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译：式（I）的N-取代的5-羟基嘧啶-6-酮-4-甲酰胺：描述为HIV整合酶的抑制剂和HIV复制抑制剂，其中R 1，R 2， / sp>，R 3和/或sp 4在本文中定义。这些化合物可用于预防和治疗艾滋病毒感染以及艾滋病的预防，延迟发作和治疗。这些化合物被用作抗HIV感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。还描述了预防，治疗或延缓AIDS发病的方法以及预防或治疗HIV感染的方法。

3. 发明申请

WO2008125518A3 PROCESS FOR THE PREPARATION OF PIPERAZINE BENZOTHIAZOLES 审中-公开
标题翻译：制备哌嗪苯并噻唑的方法
公开(公告)号：WO2008125518A3
公开(公告)日：2009-04-30
申请号：PCT/EP2008054055
申请日：2008-04-03
申请人： MERCK SERONO SA , SCHIAVO CESARE , POMA MARCO , NADLER WILLIAM
发明人： SCHIAVO CESARE , POMA MARCO , NADLER WILLIAM
IPC分类号： C07D295/18 , C07D417/06
CPC分类号： C07D417/06 , C07D295/185
摘要： The present invention discloses a process for the preparation of compounds of formula (I) where the groups and symbols are as defined in the description, said process comprising a) reacting a benzothiazol-2-ylacetonitrile bearing group R1 with an activated pyrimidine, in a reaction medium; then treating the obtained derivative in said reaction medium with a weak base anion exchange resin; then, after removing said resin and isolating the reaction product, reacting it with a substituted piperazine -benzyl-alkyloxy. The final product can optionally be salified. The invention also relates to the preparation of N-acyl-substituted piperazine -benzyl- alkyloxy, comprising treating a bromide-alkyl-phenyl-4-ester wherein the ester group is selected from COOMe or COOEt with DIBAL to obtain (4- bromomethyl-phenyl)-methanol and reacting the latter with 1-piperazin-1-yl-acyl. The processes here disclosed present a number of advantages, for example, higher yield and purity of final product. Moreover, in case of piperazine group bearing hydrogen or an acyl group in position 4, the preparation of the intermediate substituted piperazine -benzyl-alkyloxy (V) need no protection/deprotection steps.
摘要翻译：本发明公开了一种制备式（I）化合物的方法，其中基团和符号如说明书中所定义，所述方法包括a）使具有基团R 1的苯并噻唑-2-基乙腈与活化的嘧啶反应，反应介质; 然后用弱碱阴离子交换树脂处理所得反应介质中的衍生物; 然后，在除去所述树脂并分离反应产物后，与取代的哌嗪 - 苄基 - 烷氧基反应。最终产品可以任选地成盐。本发明还涉及N-酰基取代的哌嗪 - 苄基 - 烷氧基的制备，包括用DIBAL处理酯基选自COOMe或COOEt的溴化烷基苯基-4-酯，得到（4-溴甲基 - 苯基） - 甲醇，并将其与1-哌嗪-1-基 - 酰基反应。这里公开的方法具有许多优点，例如最终产物的较高产率和纯度。此外，在位置4具有氢或酰基的哌嗪基的情况下，中间体取代的哌嗪 - 苄基 - 烷氧基（V）的制备不需要保护/脱保护步骤。

4. 发明申请

WO2003035076A1 DIHYDROXYPYRIMIDINE CARBOXAMIDE INHIBITORS OF HIV INTEGRASE 审中-公开
标题翻译：艾滋病毒整合的二羟基嘧啶羧酰胺抑制剂
公开(公告)号：WO2003035076A1
公开(公告)日：2003-05-01
申请号：PCT/GB2002/004742
申请日：2002-10-21
申请人： ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI SPA , DI FRANCESCO, Maria, Emilia , GARDELLI, Cristina , HARPER, Steven , MATASSA, Victor, Giulio , MURAGLIA, Ester , NIZI, Emanuela , PACE, Paola , PACINI, Barbara , PETROCCHI, Alessia , POMA, Marco , SUMMA, Vincenzo
发明人： DI FRANCESCO, Maria, Emilia , GARDELLI, Cristina , HARPER, Steven , MATASSA, Victor, Giulio , MURAGLIA, Ester , NIZI, Emanuela , PACE, Paola , PACINI, Barbara , PETROCCHI, Alessia , POMA, Marco , SUMMA, Vincenzo
IPC分类号： A61K31/513
CPC分类号： C07D239/557 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/06 , C07D409/14 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/08 , C07D491/10
摘要： 4,5-Dihydroxypyrimidine-6-carboxamides of formula (I); are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R 1 , R 2 , R 3 and R 4 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译：式（I）的4,5-二羟基嘧啶-6-甲酰胺; 被描述为HIV整合酶和HIV复制抑制剂的抑制剂，其中R 1，R 2，R 3和R 4在本文中定义。这些化合物可用于预防和治疗艾滋病毒感染以及艾滋病的预防，延迟发作和治疗。这些化合物被用作抗HIV感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。还描述了预防，治疗或延缓AIDS发病的方法以及预防或治疗HIV感染的方法。

5. 发明专利

IL269667D0 Solid forms of (s)-[2-chloro-4-fluoro-5-(7-morpholin-4-ylquinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl) methanol, its preparation and pharmaceutical compositions containing them 未知
公开(公告)号：IL269667D0
公开(公告)日：2019-11-28
申请号：IL26966719
申请日：2019-09-25
申请人： MERCK PATENT GMBH , MAILLARD DAVID , FUCHSS THOMAS , POMA MARCO , BURINI EDOARDO , LANGE MICHAEL , KUEHN CLEMENS , BREUNING MARCEL
发明人： MAILLARD DAVID , FUCHSS THOMAS , POMA MARCO , BURINI EDOARDO , LANGE MICHAEL , KUEHN CLEMENS , BREUNING MARCEL
IPC分类号： C07D20060101
摘要： An anhydrous disordered crystalline (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)-phenyl]-(6-methoxy-pyridazin-3-yl)-methanol can be used in pharmaceutical compositions.

6. 发明专利

IL268928D0 Crystalline forms of 1-(4-{[6-amino-5-(4-phenoxy-phenyl)-pyrimidin-4-ylamino]-methyl}-piperidin-1-yl)-propenone and their use 未知
公开(公告)号：IL268928D0
公开(公告)日：2019-10-31
申请号：IL26892819
申请日：2019-08-26
申请人： MERCK PATENT GMBH , BECKER AXEL , POMA MARCO , BURINI EDOARDO , SAAL CHRISTOPH , THEUERKORN VEDAD
发明人： BECKER AXEL , POMA MARCO , BURINI EDOARDO , SAAL CHRISTOPH , THEUERKORN VEDAD
IPC分类号： C07D20060101
摘要： A solid form of 1-(4-{[6-Amino-5-(4-phenoxy-phenyl)-pyrimidin-4-ylamino]-methyl}-piperidin-1-yl)-propenone, or pharmaceutically acceptable salts thereof, are useful as BTK inhibitors.

7. 发明专利

IL235947D0 Solid state isonicotineamide derivatives and pharmaceutical compositions containing them 未知
公开(公告)号：IL235947D0
公开(公告)日：2015-02-01
申请号：IL23594714
申请日：2014-11-27
申请人： MERCK PATENT GMBH , BANKSTON DONALD , BECKER AXEL , SAAL CHRISTOPH , KUEHN CLEMENS , POMA MARCO
IPC分类号： C07D20060101
摘要： The invention relates to solid state forms of N—((S)-2,3-Dihydroxy-propyl)-3-(2-fluoro-4-iodo-phenylamino)-isonicotinamide, processes for their preparation, and medical uses thereof.

8. 发明专利

IL269666D0 Crystalline form of (s)-[2-chloro-4-fluoro-5-(7-morpholin-4-ylquinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)-methanol , its preparation and use 未知
公开(公告)号：IL269666D0
公开(公告)日：2019-11-28
申请号：IL26966619
申请日：2019-09-25
申请人： MERCK PATENT GMBH , MAILLARD DAVID , FUCHSS THOMAS , POMA MARCO , BURINI EDOARDO , LANGE MICHAEL , KUEHN CLEMENS , BREUNING MARCEL
发明人： MAILLARD DAVID , FUCHSS THOMAS , POMA MARCO , BURINI EDOARDO , LANGE MICHAEL , KUEHN CLEMENS , BREUNING MARCEL
IPC分类号： C07D20060101
摘要： A crystalline form of (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)-phenyl]-(6-methoxy-pyridazin-3-yl)-methanol can be prepared as a pharmaceutical composition.

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