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1. 发明申请

WO2009036996A3 SMALL MOLECULE BRADYKININ B1 RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2009036996A3
公开(公告)日：2009-03-26
申请号：PCT/EP2008/007919
申请日：2008-09-19
申请人： JERINI AG , LOCARDI, Elsa , DINKEL, Klaus , SCHAUDT, Marco , RICHTER, Uwe , SCHARN, Dirk , HUMMEL, Gerd , REINEKE, Ulrich , REIMER, Ulf
发明人： LOCARDI, Elsa , DINKEL, Klaus , SCHAUDT, Marco , RICHTER, Uwe , SCHARN, Dirk , HUMMEL, Gerd , REINEKE, Ulrich , REIMER, Ulf
IPC分类号： C07D207/06 , C07D207/20 , C07D213/82 , C07D213/89 , C07D239/42 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D417/12 , C07C209/00 , A61K31/506 , A61P29/00
摘要： Disclosed are compounds of formula (I) which are bradykinin B1 receptor (B1R) antagonists. These compounds are useful to treat diseases or relieve adverse symptoms associated with inflammation and pain. The invention encompasses novel compounds and acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases involving inflammation and pain.

2. 发明申请

WO2010031577A1 USE OF BRADYKININ B1 RECEPTOR ANTAGONISTS IN INTESTINAL FIBROSIS TREATMENT 审中-公开
标题翻译： BRADYKININ B1受体拮抗剂在炎性纤维化治疗中的应用
公开(公告)号：WO2010031577A1
公开(公告)日：2010-03-25
申请号：PCT/EP2009/006772
申请日：2009-09-18
申请人： JERINI AG , LOCARDI, Elsa , DINKEL, Klaus , SCHAUDT, Marco , SCHARN, Dirk , REIMER, Ulf , RICHTER, Uwe , HUMMEL, Gerd , REINEKE, Ulrich
发明人： LOCARDI, Elsa , DINKEL, Klaus , SCHAUDT, Marco , SCHARN, Dirk , REIMER, Ulf , RICHTER, Uwe , HUMMEL, Gerd , REINEKE, Ulrich
IPC分类号： A61K38/04 , A61K31/165 , A61K31/18 , A61K31/498 , A61K31/5513 , A61P1/00
CPC分类号： A61K38/08 , A61K31/165 , A61K31/18 , A61K31/498 , A61K31/5513
摘要： The present invention is related to a kinin B1 receptor antagonist for use in the treatment of a patient suffering from stricturing Crohn's Disease.
摘要翻译：本发明涉及用于治疗患有克罗恩病严重性的患者的激肽B1受体拮抗剂。

3. 发明申请

WO2010031589A1 SMALL MOLECULE BRADYKININ B2 RECEPTOR MODULATORS 审中-公开
标题翻译：小分子BRADYKININ B2受体调节剂
公开(公告)号：WO2010031589A1
公开(公告)日：2010-03-25
申请号：PCT/EP2009/006842
申请日：2009-09-22
申请人： JERINI AG , GIBSON, Christoph , SCHNATBAUM, Karsten , TRADLER, Thomas , PFEIFER, Jochen , SCHARN, Dirk , REIMER, Ulf , RICHTER, Uwe , HUMMEL, Gerd , REINEKE, Ulrich , LOCARDI, Elsa , PASCHKE, Matthias
发明人： GIBSON, Christoph , SCHNATBAUM, Karsten , TRADLER, Thomas , PFEIFER, Jochen , SCHARN, Dirk , REIMER, Ulf , RICHTER, Uwe , HUMMEL, Gerd , REINEKE, Ulrich , LOCARDI, Elsa , PASCHKE, Matthias
IPC分类号： C07D401/14 , C07D417/14 , A61K31/47 , A61P17/00
CPC分类号： C07D401/14 , C07D413/14 , C07D417/14
摘要： The present invention is related to a compound of the formula (I): or a pharmacologically acceptable salt, solvate, or hydrate thereof, wherein R 1 is: (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), (l), (m), (n), (o), (p), (q), (r), (s); R 2 is C1, F, or methoxy; R 3 is methyl, methoxy, hydroxymethyl, H, or absent; R 4 is methyl, ethyl, HO, H, or absent; A 1 is C or N; A 2 is C or N; R 6 is H or OH; R 5 is: (t), (u), (v), (w), (x), (y), (z).
摘要翻译：本发明涉及式（I）化合物或其药理学上可接受的盐，溶剂化物或水合物，其中R1为：（a），（b），（c），（d），（e），（g），（h），（i），（j），（k），（l），（m），（n），（o），（p），（q） r），（s）; R2是C1，F或甲氧基; R3是甲基，甲氧基，羟甲基，H或不存在; R4是甲基，乙基，HO，H或不存在; A1为C或N; A2为C或N; R6是H或OH; R5是：（t），（u），（v），（w），（x），（y），（z）。

4. 发明申请

WO2008116620A1 8-OXY-QUINOLINE DERIVATIVES AS BRADYKININ B2 RECEPTOR MODULATORS 审中-公开
标题翻译： 8-O-喹啉衍生物作为BRADYKININ B2受体调节剂
公开(公告)号：WO2008116620A1
公开(公告)日：2008-10-02
申请号：PCT/EP2008/002316
申请日：2008-03-22
申请人： JERINI AG , GIBSON, Christoph , TRADLER, Thomas , SCHNATBAUM, Karsten , PFEIFER, Jochen , LOCARDI, Elsa , SCHARN, Dirk , PASCHKE, Matthias , REIMER, Ulf , RICHTER, Uwe , HUMMEL, Gerd , REINEKE, Ulrich
发明人： GIBSON, Christoph , TRADLER, Thomas , SCHNATBAUM, Karsten , PFEIFER, Jochen , LOCARDI, Elsa , SCHARN, Dirk , PASCHKE, Matthias , REIMER, Ulf , RICHTER, Uwe , HUMMEL, Gerd , REINEKE, Ulrich
IPC分类号： C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , A61K31/4709 , A61P29/00
CPC分类号： C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention is related to compound of the formula (I): or a pharmacologically acceptable salt, solvate, or hydrate thereof, wherein A is a 6-membered heteroaryl having from 1 to 3 heteroatoms, each independently selected from N or O and the other substituents are defined as in the claims.
摘要翻译：本发明涉及式（I）化合物或其药理学上可接受的盐，溶剂合物或水合物，其中A为具有1至3个杂原子的6元杂芳基，各自独立地选自N或O，且其它取代基如权利要求中所定义。

5. 发明申请

WO2006128670A1 C5A RECEPTOR ANTAGONISTS 审中-公开
标题翻译： C5A受体拮抗剂
公开(公告)号：WO2006128670A1
公开(公告)日：2006-12-07
申请号：PCT/EP2006/005141
申请日：2006-05-30
申请人： JERINI AG , SCHNATBAUM, Karsten , SCHARN, Dirk , LOCARDI, Elsa , POLAKOWSKI, Thomas , RICHTER, Uwe , REINEKE, Ulrich , HUMMEL, Gerd
发明人： SCHNATBAUM, Karsten , SCHARN, Dirk , LOCARDI, Elsa , POLAKOWSKI, Thomas , RICHTER, Uwe , REINEKE, Ulrich , HUMMEL, Gerd
IPC分类号： C07C275/40 , A61K31/17
CPC分类号： C07C275/40 , C07C235/40 , C07C275/26 , C07C275/30 , C07C2602/08 , C07C2602/10 , C07D207/327 , C07D213/40 , C07D213/61 , C07D215/40 , C07D235/06 , C07D237/08 , C07D239/42 , C07D241/42 , C07D311/20 , C07D335/02
摘要： The present invention is related to a compound, preferably a C5a receptor antagonist, having the following structure, Rl, R2, R3, R4, R5, R6, R7, R8, R9, Rl0, RI l, R12, R13, R14, R15, R16, Rl7, R18, Rl9, R20, R21 and R22 are individually and independently selected from the group comprising H, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, substituted cycloalkyl, heterocyclyl, substituted heterocyclyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl, substituted arylalkyl, heteroarylalkyl, substituted heteroarylalkyl, alkoxyl, substituted alkoxyl, aryloxy, substituted aryloxy, arylalkyloxy, substituted arylalkyloxy, acyloxy, substituted acyloxy, halogen, hydroxyl, nitro, cyano, acyl, substituted acyl, mercapto, alkylthio, substituted alkylthio, amino, substituted amino, alkylamino, substituted alkylamino, bisalkyl amino, substituted bisalkyl amino, cyclic amino, substituted cyclic amino, carbamoyl (-CONH 2 ), substituted carbamoyl, carboxyl, carbamate, alkoxycarbonyl, substituted alkoxycarbonyl, acylamino, substituted acylamino, sulfamoyl (-SO 2 NH 2 ), substituted sulfamoyl, haloalkyl, haloalkyloxy, -C(O)H, trialkylsilyl and azido.
摘要翻译：本发明涉及具有以下结构的化合物，优选C5a受体拮抗剂：R1，R2，R3，R4，R5，R6，R7，R8，R9，R1O，R1，R12，R13，R14，R15 ，R 16，R 17，R 18，R 19，R 20，R 21和R 22各自独立地选自H，烷基，取代的烷基，烯基，取代的烯基，炔基，取代的炔基，环烷基，取代的环烷基，杂环基，取代的杂环基，芳基，取代的芳基，杂芳基，取代的杂芳基，芳基烷基，取代的芳基烷基，杂芳基烷基，取代的杂芳基烷基，烷氧基，取代的烷氧基，芳氧基，取代的芳氧基，芳基烷氧基，取代的芳基烷氧基，酰氧基，取代的酰氧基，卤素，羟基，硝基，氰基，酰基，取代的酰基，巯基，烷硫基，取代的烷硫基，氨基，取代的氨基，烷基氨基，取代的烷基氨基，双烷基氨基，取代的双烷基氨基，环状氨基，取代的环状氨基，氨基甲酰基（-CONH 2 < 取代的氨基甲酰基，羧基，氨基甲酸酯，烷氧基羰基，取代的烷氧基羰基，酰氨基，取代的酰基氨基，氨磺酰基（-SO 2 NH 2），取代的氨磺酰基，卤代烷基，卤代烷氧基，-C（O）H，三烷基甲硅烷基和叠氮基。

6. 发明申请

WO2006074964A1 C5A RECEPTOR ANTAGONISTS 审中-公开
标题翻译： C5A受体拮抗剂
公开(公告)号：WO2006074964A1
公开(公告)日：2006-07-20
申请号：PCT/EP2006/000365
申请日：2006-01-17
申请人： JERINI AG , HUMMEL, Gerd , LOCARDI, Elsa , POLAKOWSKI, Thomas , SCHARN, Dirk , SCHNATBAUM, Karsten
发明人： HUMMEL, Gerd , LOCARDI, Elsa , POLAKOWSKI, Thomas , SCHARN, Dirk , SCHNATBAUM, Karsten
IPC分类号： C07K7/06 , C07K7/64 , C07K14/47 , C07K14/705 , C07K7/56
CPC分类号： C07K14/472 , C07K7/06 , C07K7/56 , C07K7/64
摘要： The present invention is related to a compound, preferably a C5a receptor antagonist, having the following structure: (I), whereby X1 is a radical having a mass of about 1-300, whereby X1 is preferably selected from the group comprising R5-, R5-CO-, R5-N(R6)-CO-, R5-O-CO-, R5-SO 2 -, R5-N(R6)-SO 2 -, R5-N(R6)-, R5-N(R6)-CS-, R5-N(R6)-C(NH)-, R5-CS-, R5-P(O)OH-5 R5-B(OH)-, and R5 -CH=N-O-CH 2 -CO-, whereby R5 and R6 are individually and independently selected from the group comprising H, F, hydroxy, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, heterocyclyl, substituted heterocyclyl, arylalkyl, substituted arylalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, acyl, substituted acyl, alkoxy, alkoxyalkyl, substituted alkoxyalkyl, aryloxyalkyl and substituted aryloxyalkyl, X2 is a radical that mimics the biological binding characteristics of a phenylalanine unit, X3 and X4 are individually and independently a spacer, whereby the spacer is preferably selected from the group comprising amino acids, amino acid analogs and amino acid derivates, X5 is a radical that mimics the biological binding characteristics of a cyclohexylalanine or homoleucine unit, X6 is a radical that mimics the biological binding characteristics of a tryptophane unit, X7 is a radical that mimics the biological binding characteristics of a norleucine or phenylalanine unit, a chemical bond X3 and X7 is formed, and the connecting lines - in formula (I) indicate chemical bonds, whereby the chemical bond is individually and independently selected from the group comprising covalent bonds, ionic bonds and coordinative bonds, whereby preferably the bond is a chemical bond and more preferably the chemical bond is a bond selected from the group comprising amide bonds, disulfide bonds, ether bonds, thioether bonds, oxime bonds and aminotriazine bonds, whereby the compound is in particular useful for the manufacture of a medicament for the treatment of autoimmune diseases.
摘要翻译：本发明涉及具有以下结构的化合物，优选C5a受体拮抗剂：（I），其中X1是质量约1-300的基团，其中X1优选选自包含R5-， R5-CO-，R5-N（R6）-CO-，R5-O-CO-，R5-SO2 - ，R5-N（R6）-SO2

7. 发明申请

WO2005010030A3 C5a-REZEPTOR-ANTAGONISTEN 审中-公开
公开(公告)号：WO2005010030A3
公开(公告)日：2005-02-03
申请号：PCT/EP2004/008057
申请日：2004-07-19
申请人： JERINI AG , HUMMEL, Gerd , LOCARDI, Elsa , POLAKOWSKI, Thomas , SCHARN, Dirk , SCHNATBAUM, Karsten
发明人： HUMMEL, Gerd , LOCARDI, Elsa , POLAKOWSKI, Thomas , SCHARN, Dirk , SCHNATBAUM, Karsten
IPC分类号： C07K7/06 , C07K14/47 , C07K14/705 , C07K7/50
摘要： C5a-Rezeptor-Antagonist, der Struktur (I), wobei X1 ein Radikal mit einer Masse von etwa 1-300 ist und wobei X1 gleich R5-, R5-CO-, R5-N(R6)-CO-, R5-O-CO-, R5-SO 2 -, R5-N(R6)-SO 2 -, R5-N(R6)-, R5-N(R6)-CS-, R5-N(R6)-C(NH)-, R5-CS-, R5-P(O)OH-, R5-B(OH)-, oder R5-CH=N-O-CH 2 -CO-, wobei R5 / R6 gleich H, F, Hydroxy, Alkyl, substituiertes Alkyl, Cycloalkyl, substituiertes Cycloalkyl, Heterocyclyl, substituiertes Heterocyclyl, Arylalkyl, substituiertes Arylalkyl, Aryl, substituiertes Aryl, Heteroaryl, substituiertes Heteroaryl, Acyl, substituiertes Acyl, Alkoxy, Alkoxyalkyl, substituiertes Alkoxyalkyl, Aryloxyalkyl oder substituiertes Aryloxyalkyl, X2 = Radikal (biologische Bindungseigenschaften einer Phenylalanin-Einheit mimikrierend), X3 / X4 = Spacer (Aminosäuren, Aminosäure-Analoga und Aminosäure-Derivate), X5 = Radikal (biologische Bindungseigenschaften einer Cyclohexylalanin- oder Homoleucin-Einheit mimikrierend), X6 = Radikal (biologische Bindungseigenschaften einer Tryptophan-Einheit mimikrierend), X7 = Radikal (biologische Bindungseigenschaften einer Norleucin- oder Phenylalanin-Einheit mimikrierend), eine chemische Bindung zwischen X3 und X7 ausgebildet ist.

8. 发明公开

EP1838725A1 C5A RECEPTOR ANTAGONISTS 审中-公开
标题翻译： C5A受体拮抗剂
公开(公告)号：EP1838725A1
公开(公告)日：2007-10-03
申请号：EP06706265.3
申请日：2006-01-17
申请人： Jerini AG
发明人： HUMMEL, Gerd , LOCARDI, Elsa , POLAKOWSKI, Thomas , SCHARN, Dirk , SCHNATBAUM, Karsten
IPC分类号： C07K7/06 , C07K7/64 , C07K14/47 , C07K14/705 , C07K7/56
CPC分类号： C07K14/472 , C07K7/06 , C07K7/56 , C07K7/64
摘要： The present invention is related to a compound, preferably a C5a receptor antagonist, having the following structure: (I), whereby X1 is a radical having a mass of about 1-300, whereby X1 is preferably selected from the group comprising R5-, R5-CO-, R5-N(R6)-CO-, R5-O-CO-, R5-SO2-, R5-N(R6)-SO2-, R5-N(R6)-, R5-N(R6)-CS-, R5-N(R6)-C(NH)-, R5-CS-, R5-P(O)OH-5 R5-B(OH)-, and R5 -CH=N-O-CH2-CO-, whereby R5 and R6 are individually and independently selected from the group comprising H, F, hydroxy, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, heterocyclyl, substituted heterocyclyl, arylalkyl, substituted arylalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, acyl, substituted acyl, alkoxy, alkoxyalkyl, substituted alkoxyalkyl, aryloxyalkyl and substituted aryloxyalkyl, X2 is a radical that mimics the biological binding characteristics of a phenylalanine unit, X3 and X4 are individually and independently a spacer, whereby the spacer is preferably selected from the group comprising amino acids, amino acid analogs and amino acid derivates, X5 is a radical that mimics the biological binding characteristics of a cyclohexylalanine or homoleucine unit, X6 is a radical that mimics the biological binding characteristics of a tryptophane unit, X7 is a radical that mimics the biological binding characteristics of a norleucine or phenylalanine unit, a chemical bond X3 and X7 is formed, and the connecting lines - in formula (I) indicate chemical bonds, whereby the chemical bond is individually and independently selected from the group comprising covalent bonds, ionic bonds and coordinative bonds, whereby preferably the bond is a chemical bond and more preferably the chemical bond is a bond selected from the group comprising amide bonds, disulfide bonds, ether bonds, thioether bonds, oxime bonds and aminotriazine bonds, whereby the compound is in particular useful for the manufacture of a medicament for the treatment of autoimmune diseases.

9. 发明公开

EP2344176A1 USE OF BRADYKININ B1 RECEPTOR ANTAGONISTS IN INTESTINAL FIBROSIS TREATMENT 审中-公开
标题翻译：缓激肽B1受体的ANTAGONITEN肠纤维化的治疗用途
公开(公告)号：EP2344176A1
公开(公告)日：2011-07-20
申请号：EP09778615.6
申请日：2009-09-18
申请人： Jerini AG
发明人： LOCARDI, Elsa , DINKEL, Klaus , SCHAUDT, Marco , SCHARN, Dirk , REIMER, Ulf , RICHTER, Uwe , HUMMEL, Gerd , REINEKE, Ulrich
IPC分类号： A61K38/04 , A61K31/165 , A61K31/18 , A61K31/498 , A61K31/5513 , A61P1/00
CPC分类号： A61K38/08 , A61K31/165 , A61K31/18 , A61K31/498 , A61K31/5513
摘要： The present invention is related to a kinin B1 receptor antagonist for use in the treatment of a patient suffering from stricturing Crohn's Disease.

10. 发明授权

EP2144897B1 8-OXY-QUINOLINE DERIVATIVES AS BRADYKININ B2 RECEPTOR MODULATORS 有权
标题翻译： 8 OXYCHINOLINDERIVATE作为缓激肽B2受体的调节剂
公开(公告)号：EP2144897B1
公开(公告)日：2010-10-20
申请号：EP08716679.9
申请日：2008-03-22
申请人： Jerini AG
发明人： GIBSON, Christoph , TRADLER, Thomas , SCHNATBAUM, Karsten , PFEIFER, Jochen , LOCARDI, Elsa , SCHARN, Dirk , PASCHKE, Matthias , REIMER, Ulf , RICHTER, Uwe , HUMMEL, Gerd , REINEKE, Ulrich
IPC分类号： C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , A61K31/4709 , A61P29/00
CPC分类号： C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention is related to compound of the formula (I): or a pharmacologically acceptable salt, solvate, or hydrate thereof, wherein A is a 6-membered heteroaryl having from 1 to 3 heteroatoms, each independently selected from N or O and the other substituents are defined as in the claims.

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