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1. 发明申请

WO2010115836A4 SUBSTITUTED PIPERIDINES AS CCR3 ANTAGONISTS 审中-公开
公开(公告)号：WO2010115836A4
公开(公告)日：2010-10-14
申请号：PCT/EP2010/054396
申请日：2010-04-01
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , GRUNDL, Marc , DOLLINGER, Horst , GIOVANNINI, Riccardo , HOENKE, Christoph , HOFFMANN, Matthias , KRIEGL, Jan , MARTYRES, Domnic , RAST, Georg , SEITHER, Peter
发明人： GRUNDL, Marc , DOLLINGER, Horst , GIOVANNINI, Riccardo , HOENKE, Christoph , HOFFMANN, Matthias , KRIEGL, Jan , MARTYRES, Domnic , RAST, Georg , SEITHER, Peter
IPC分类号： C07D401/04 , C07D401/14 , C07D413/04 , C07D413/14 , C07D417/14 , A61K31/4523 , A61K31/454 , A61P31/00 , A61P35/00 , A61P37/00
摘要： Object of the present invention are novel substituted compounds of the formula 1, wherein A, R 1 , R 2 , R 3 and R 4 are defined as in the description. Another object of the present invention is to provide antagonists of CCR3, more particularly to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.

2. 发明申请

WO2010070032A1 CYCLIC PYRIMIDIN-4-CARBOXAMIDES AS CCR2 RECEPTOR ANTAGONISTS FOR TREATMENT OF INFLAMMATION, ASTHMA AND COPD 审中-公开
标题翻译： CYPIC PYRIMIDIN-4-CARBOXAMIDES作为CCR2受体拮抗剂用于治疗炎症，哮喘和COPD
公开(公告)号：WO2010070032A1
公开(公告)日：2010-06-24
申请号：PCT/EP2009/067378
申请日：2009-12-17
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , EBEL, Heiner , FRATTINI, Sara , GIOVANNINI, Riccardo , HOENKE, Christoph , TRIESELMANN, Thomas , TIELMANN, Patrick , SCHEUERER, Stefan , HOBBIE, Silke (Marie Katrin)
发明人： EBEL, Heiner , FRATTINI, Sara , GIOVANNINI, Riccardo , HOENKE, Christoph , TRIESELMANN, Thomas , TIELMANN, Patrick , SCHEUERER, Stefan , HOBBIE, Silke (Marie Katrin)
IPC分类号： C07D401/06 , C07D401/14 , C07D403/06 , C07D413/14 , A61K31/506 , A61P29/00 , C07D407/14 , C07D471/10
CPC分类号： C07D498/10 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/553 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D407/14 , C07D413/14 , C07D417/14 , C07D451/02 , C07D471/04 , C07D471/10 , C07D491/052 , Y02A50/385 , Y02A50/409 , Y02A50/411
摘要： The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD. Formula (I), wherein A is selected from among a single bond, =CH-, -CH 2 -, -O-, -S-, and -NH-; wherein n is 1, 2 or 3; wherein Z is C or N, the other variables are as defined in the claims, as well as in form of their acid addition salts with pharmacologically acceptable acids.
摘要翻译：本发明涉及CCR2（CC趋化因子受体2）的新型拮抗剂及其用于治疗疾病，特别是肺疾病如哮喘和COPD的药物的用途。式（I）其中A选自单键，= CH - ， - CH 2 - ， - O - ， - S - 和-NH-; 其中n为1,2或3; 其中Z是C或N，其它变量如权利要求中所定义，以及其与药理学上可接受的酸的酸加成盐的形式。

3. 发明申请

WO2007042250A1 PROLINAMIDE DERIVATIVES AS SODIUM CHANNEL MODULATORS 审中-公开
标题翻译：丙酰胺衍生物作为钠通道调节剂
公开(公告)号：WO2007042250A1
公开(公告)日：2007-04-19
申请号：PCT/EP2006/009746
申请日：2006-10-06
申请人： GLAXO GROUP LIMITED , ALVARO, Giuseppe , ANDREOTTI, Daniele , BERGAUER, Markus , GIOVANNINI, Riccardo , MARASCO, Agostino
发明人： ALVARO, Giuseppe , ANDREOTTI, Daniele , BERGAUER, Markus , GIOVANNINI, Riccardo , MARASCO, Agostino
IPC分类号： C07D207/22 , A61K31/401 , A61P25/24 , C07D211/60 , C07D401/04 , C07D487/04 , A61K31/451 , A61K31/407
CPC分类号： C07D487/04 , C07D207/22 , C07D211/60 , C07D401/04
摘要： This invention relates to novel -aminocarboxyamide derivatives of formula (I) for treating diseases and conditions mediated by modulation of use-dependent voltage-gated sodium channels.
摘要翻译：本发明涉及式（I）的新型氨基羧基酰胺衍生物，其用于治疗通过调节依赖于电压门控钠通道介导的疾病和病症。

4. 发明申请

WO2004005256A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2004005256A2
公开(公告)日：2004-01-15
申请号：PCT/EP2003/007127
申请日：2003-07-02
申请人： GLAXO GROUP LIMITED , ALVARO, Giuseppe , CARDULLO, Francesca , DI FABIO, Romano , GIOVANNINI, Riccardo , PIGA, Elisabetta , TRANQUILLINI, Maria, Elvira
发明人： ALVARO, Giuseppe , CARDULLO, Francesca , DI FABIO, Romano , GIOVANNINI, Riccardo , PIGA, Elisabetta , TRANQUILLINI, Maria, Elvira
IPC分类号： C07D211/34
CPC分类号： C07D211/34 , C07D211/64 , C07D223/04 , C07D223/06
摘要： The present invention relates to cyclic amine derivatives of formula(I) (I)whereinR represents halogen, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethyl or trifluoromethoxy;R1 represents hydrogen, halogen, C3-7cycloalkyl, hydroxy, nitro, cyano or C1-4 alkyl optionally substituted by halogen, cyano or C1-4 alkoxy;R2 represents hydrogen or C1-4 alkyl;R3 and R4 independently represent hydrogen, cyano, C1-4 alkyl or R3 together with R4 represents C3-7 cycloalkyl;R5 represents trifluoromethyl, S(O)t C 1-4 alkyl, C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy, halogen or cyano;R6 represents hydrogen or (CH2)rR7;R7 represents hydrogen, C3-7 cycloalkyl, NH(C1-4alkylOC1-4alkoxy), NH(C1-4alkyl), N(C1-4alkyl)2 , OC(O)NR9R8 , NR8C(O)R9 or C(O)NR9R8;R9 and R8 independently represent hydrogen, C1-4 alkyl or C3-7 cycloalkyl; m represents zero or an integer from 1 to 4;n represents 1 or 2;p is zero or an integer from 1 to 3;q is an integer from 1 to 3;r is an integer from 1 to 4;t is 0 , 1 or 2 ;provided that when m is 0, p is 2, q , r and n represent 1, R1, R2,R3, R4, R5 and R7 are hydrogen and R is chlorine, R5 is not iodine; and pharmaceutically acceptable salts and solvates thereof; process for their preparation and their use in the treatment of conditions mediated by tackykinins and/or by selective inhibition of serotonin reuptake transporter protein .
摘要翻译：本发明涉及式（I）（I）的环胺衍生物，其中R代表卤素，C 1-4烷基，氰基，C 1-4烷氧基，三氟甲基或三氟甲氧基; R 1代表氢，卤素，氰基或C1-4烷基; R2代表氢或C1-4烷基; R3和R4独立地代表氢，氰基，C1-4烷基或R3 与R 4一起代表C 3-7环烷基; R 5代表三氟甲基，S（O）t C 1-4烷基，C 1-4烷基，C 1-4烷氧基，三氟甲氧基，卤素或氰基; R 6代表氢或（CH 2）r R 7; R 7 （C 1-4烷基），N（C 1-4烷基）2，OC（O）NR 9 R 8，NR 8 C（O）R 9或C（O）NR 9 R 8; R9和R8独立地表示氢，C1-4烷基或C3-7环烷基; m表示0或1至4的整数; n表示1或2; p为0或1至3的整数; q为1至3的整数; r为1至4的整数; t为0， 1或2;条件是当m为0时，p为2，q，r和n表示1，R1，R2，R3，R4，R5和R7是氢并且R是氯，R5不是碘; 及其药学上可接受的盐和溶剂合物; 它们的制备方法以及它们在治疗由粘着激肽介导的病症和/或通过选择性抑制血清素再摄取转运蛋白中的用途。

5. 发明申请

WO2012110599A1 TRICYCLIC PYRIDINE DERIVATIVES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, THEIR USE AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译：三环吡啶衍生物，含有这些化合物的药物，其使用及其制备方法
公开(公告)号：WO2012110599A1
公开(公告)日：2012-08-23
申请号：PCT/EP2012/052687
申请日：2012-02-16
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , WAGNER, Holger , BERTA, Daniela , FUCHS, Klaus , GIOVANNINI, Riccardo , HAMPRECHT, Wolfgang , KONETZKI, Ingo , STREICHER, Ruediger , TRIESELMANN, Thomas
发明人： WAGNER, Holger , BERTA, Daniela , FUCHS, Klaus , GIOVANNINI, Riccardo , HAMPRECHT, Wolfgang , KONETZKI, Ingo , STREICHER, Ruediger , TRIESELMANN, Thomas
IPC分类号： C07D491/04 , A61P3/06 , A61P9/00 , A61K31/4741
CPC分类号： C07D491/048 , C07D491/107 , C07D491/18
摘要： The present invention relates to compounds defined by formula (I), wherein the variables R 1 -R 8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme.
摘要翻译：本发明涉及由式（I）定义的化合物，其中变量R1-R8如描述中所定义，具有有价值的药理学活性。特别地，化合物是胆固醇酯转移蛋白（CETP）的抑制剂，因此适用于治疗和预防可受该酶抑制影响的疾病。

6. 发明申请

WO2011018495A1 NEW COMPOUNDS FOR THE TREATMENT OF CNS DISORDERS 审中-公开
标题翻译：用于治疗CNS病症的新化合物
公开(公告)号：WO2011018495A1
公开(公告)日：2011-02-17
申请号：PCT/EP2010/061735
申请日：2010-08-12
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , HEINE, Niklas , DORNER-CIOSSEK, Cornelia , EICKMEIER, Christian , FIEGEN, Dennis , FOX, Thomas , FUCHS, Klaus , GIOVANNINI, Riccardo , ROSENBROCK, Holger , SCHAENZLE, Gerhard , BAERFACKER, Lars
发明人： HEINE, Niklas , DORNER-CIOSSEK, Cornelia , EICKMEIER, Christian , FIEGEN, Dennis , FOX, Thomas , FUCHS, Klaus , GIOVANNINI, Riccardo , ROSENBROCK, Holger , SCHAENZLE, Gerhard , BAERFACKER, Lars
IPC分类号： C07D487/04 , A61K31/522 , A61P25/28
CPC分类号： C07D487/04
摘要： The invention relates to novel pyrazolopyrimidinones according to formula (I). The new compounds shall be used for the manufacture of medicaments, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. The new compounds are also for the manufacture of medicaments for the treatment of Alzheimer's disease. Further aspects of the present invention refer to a process for the manufacture of the compounds and their use for producing medicaments.
摘要翻译：本发明涉及式（I）的新型吡唑并嘧啶酮。新化合物应用于制造药物，特别是用于治疗有关感知，集中，学习或记忆缺陷的病症的药物。新化合物也用于制备用于治疗阿尔茨海默氏病的药物。本发明的其它方面是指化合物的制造方法及其制造用药物的用途。

7. 发明申请

WO2010115836A1 SUBSTITUTED PIPERIDINES AS CCR3 ANTAGONISTS 审中-公开
标题翻译：作为CCR3拮抗剂的取代的哌啶
公开(公告)号：WO2010115836A1
公开(公告)日：2010-10-14
申请号：PCT/EP2010054396
申请日：2010-04-01
申请人： BOEHRINGER INGELHEIM INT , GRUNDL MARC , DOLLINGER HORST , GIOVANNINI RICCARDO , HOENKE CHRISTOPH , HOFFMANN MATTHIAS , KRIEGL JAN , MARTYRES DOMNIC , RAST GEORG , SEITHER PETER
发明人： GRUNDL MARC , DOLLINGER HORST , GIOVANNINI RICCARDO , HOENKE CHRISTOPH , HOFFMANN MATTHIAS , KRIEGL JAN , MARTYRES DOMNIC , RAST GEORG , SEITHER PETER
IPC分类号： C07D401/04 , A61K31/4523 , A61K31/454 , A61P31/00 , A61P35/00 , A61P37/00 , C07D401/14 , C07D413/04 , C07D413/14 , C07D417/14
CPC分类号： C07D401/04 , A61K31/4523 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/506 , A61K31/5355 , A61K31/56 , C07D401/14 , C07D413/04 , C07D413/14 , C07D417/14
摘要： Object of the present invention are novel substituted compounds of the formula 1, wherein A, R1, R2, R3 and R4 are defined as in the description. Another object of the present invention is to provide antagonists of CCR3, more particularly to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明的目的是式I的新型取代化合物，其中A，R 1，R 2，R 3和R 4如说明书中所定义。本发明的另一目的是提供CCR3的拮抗剂，更具体地说是提供包含药学上可接受的载体和治疗有效量的至少一种本发明化合物或其药学上可接受的盐的药物组合物。

8. 发明申请

WO2007042239A1 PROLINAMIDE DERIVATIVES AS SODIUM CHANNEL MODULATORS 审中-公开
标题翻译：丙酰胺衍生物作为钠通道调节剂
公开(公告)号：WO2007042239A1
公开(公告)日：2007-04-19
申请号：PCT/EP2006/009731
申请日：2006-10-06
申请人： GLAXO GROUP LIMITED , ALVARO, Giuseppe , BERGAUER, Markus , GIOVANNINI, Riccardo , PROFETA, Roberto
发明人： ALVARO, Giuseppe , BERGAUER, Markus , GIOVANNINI, Riccardo , PROFETA, Roberto
IPC分类号： C07D207/22 , A61K31/401 , A61P25/24
CPC分类号： C07D207/22
摘要： The invention provides a compound of formula (I), a solvate, a salt or prodrug thereof, useful in the treatment of diseases and conditions mediated by modulation of use-dependent voltage-gated sodium channels.
摘要翻译：本发明提供式（I）化合物，其溶剂合物，盐或前药，其可用于治疗通过调节依赖于电压门控钠通道介导的疾病和病症。

9. 发明申请

WO0125219A3 PIPERAZINE COMPOUNDS 审中-公开
标题翻译：哌嗪化合物
公开(公告)号：WO0125219A3
公开(公告)日：2001-12-13
申请号：PCT/EP0009722
申请日：2000-10-05
申请人： GLAXO GROUP LTD , ALVARO GIUSEPPE , FABIO ROMANO DI , GIOVANNINI RICCARDO , GUERCIO GIUSEPPE , ST DENIS YVES , URSINI ANTONELLA
发明人： ALVARO GIUSEPPE , DI FABIO ROMANO , GIOVANNINI RICCARDO , GUERCIO GIUSEPPE , ST-DENIS YVES , URSINI ANTONELLA
IPC分类号： A61K31/495 , A61K31/496 , A61P1/04 , A61P11/06 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P29/00 , C07D241/04 , C07D401/06 , C07D403/06
CPC分类号： C07D401/06 , A61K31/135 , A61K31/196 , A61K31/495 , A61K31/496 , C07D241/04 , C07D403/06 , A61K2300/00
摘要： The present invention relates to piperazine derivatives of formula (I) wherein R represents a halogen atom or a C1-4 alkyl group; R1 represents hydrogen or a C1-4 alkyl group; R2 represents hydrogen, a C1-4 alkyl, C2-6 alkenyl or a C3-7 cycloalkyl group; or R1 and R2 together with nitrogen and carbon atom to which they are attached respectively represent a 5-6 membered heterocyclic group; R3 represents a trifluoromethyl, a C1-4 alkyl, a C1-4 alkoxy, a trifluoromethoxy or a halogen group; R4 represents hydrogen, a (CH2)qR7 or a (CH2)rCO(CH2)pR7 group; R5 represents hydrogen, a C1-4 alkyl or a COR6 group; R6 represents hydrogen, hydroxy, amino, methylamino, dimethylamino a 5 membered heteroaryl group containing 1 to 3 heteroatoms selected from oxygen, sulphur and nitrogen or a 6 membered heteroaryl group containing 1 to 3 nitrogen atoms; R7 represents hydrogen, hydroxy or NR8R9 wherein R8 and R9 represent independently hydrogen or C1-4 alkyl optionally substituted by hydroxy, or by amino; R10 represents hydrogen, a C1-4 alkyl I group or R10 together with R2 represents a C3-7 cycloalkyl group; m is zero or an integer from 1 to 3; n is zero or an integer from 1 to 3; both p and r are independently zero or an integer from 1 to 4; q is an integer from 1 to 4; provided that, when R1 and R2 together with nitrogen and carbon atom to which they are attached respectively represent a 5 to 6 membered heterocyclic group, i) m is 1 or 2; ii) when m is 1, R is not fluorine and iii) when m is 2, the two substituents R are not both fluorine,and pharmaceutically acceptable salts and solvates thereof.
摘要翻译：本发明涉及式（I）的哌嗪衍生物，其中R表示卤素原子或C1-4烷基; R1表示氢或C1-4烷基; R 2表示氢，C 1-4烷基，C 2-6烯基或C 3-7环烷基; 或R 1和R 2与它们所连接的氮原子和碳原子分别表示5-6元杂环基; R3表示三氟甲基，C1-4烷基，C1-4烷氧基，三氟甲氧基或卤素基团; R4表示氢，（CH2）qR7或（CH2）rCO（CH2）pR7基团; R5代表氢，C1-4烷基或COR6基团; R 6表示氢，羟基，氨基，甲基氨基，二甲基氨基，含有1至3个选自氧，硫和氮的杂原子或含有1至3个氮原子的6元杂芳基的5元杂芳基; R 7表示氢，羟基或NR 8 R 9，其中R 8和R 9独立地表示氢或任选被羟基取代的C 1-4烷基或氨基; R 10表示氢，C 1-4烷基I基或R 10与R 2一起代表C 3-7环烷基; m为0或1〜3的整数; n为0或1〜3的整数; p和r分别独立为零或1至4的整数; q是1至4的整数; 条件是当R1和R2与它们所连接的氮原子和碳原子分别表示5至6元杂环基时，i）m为1或2; ii）当m为1时，R不为氟，iii）当m为2时，两个取代基R不同时为氟，其药学上可接受的盐和溶剂化物。

10. 发明申请

WO2013017657A1 PHENYL-3-AZA-BICYCLO[3.1.0]HEX-3-YL-METHANONES AND THE USE THEREOF AS MEDICAMENT 审中-公开
标题翻译：苯基-3-氮杂双环[3.1.0] HEX-3-YL-甲烷及其作为药物的用途
公开(公告)号：WO2013017657A1
公开(公告)日：2013-02-07
申请号：PCT/EP2012/065140
申请日：2012-08-02
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , GIOVANNINI, Riccardo , BERTANI, Barbara , FERRARA, Marco , LINGARD, Iain , MAZZAFERRO, Rocco , ROSENBROCK, Holger
发明人： GIOVANNINI, Riccardo , BERTANI, Barbara , FERRARA, Marco , LINGARD, Iain , MAZZAFERRO, Rocco , ROSENBROCK, Holger
IPC分类号： C07D401/04 , C07D403/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , A61K31/421 , A61K31/427 , A61K31/437 , A61K31/4439 , A61P25/18 , A61P25/28
CPC分类号： C07D413/04 , C07D209/52 , C07D401/04 , C07D403/04 , C07D413/14 , C07D417/04 , C07D471/04
摘要： The present inventions relates to substituted phenyl-3-aza-bicyclo[3.1.0]hex-3-yl- methanones of general formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as herein described or salts thereof, preferably pharmaceutically acceptable salts thereof. The invention further relates to the manufacture of said compounds, pharmaceutical compositions comprising a compound according to general formula (I), and the use of said compounds for the treatment of various conditions such as conditions concerning positive and negative symptoms of schizophrenia as well as cognitive impairments associated with schizophrenia, Alzheimers Disease and other neurological and psychiatric disorders. The compounds of the invention show glycine transporter-1 (GlyT1) inhibiting properties.
摘要翻译：本发明涉及通式（I）的取代的苯基-3-氮杂 - 双环[3.1.0]己-3-基 - 甲酮，其中R 1，R 2，R 3，R 4，R 5和R 6如本文所述或其盐，优选其药学上可接受的盐。本发明进一步涉及所述化合物的制造，包含根据通式（I）的化合物的药物组合物，以及所述化合物用于治疗各种病症的用途，例如关于精神分裂症的正和负症状的症状以及认知与精神分裂症，阿尔茨海默病和其他神经和精神疾病有关的损伤。本发明化合物显示甘氨酸转运体-1（GlyT1）抑制性质。

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