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1. 发明专利

JP2011057681A C5a RECEPTOR ANTAGONIST 审中-公开
标题翻译： C5a受体拮抗剂
公开(公告)号：JP2011057681A
公开(公告)日：2011-03-24
申请号：JP2010230873
申请日：2010-10-13
申请人： Jerini Ag , イエリニ・アクチェンゲゼルシャフトJerini Ag
发明人： HUMMEL GERD , LOCARDI ELSA , POLAKOWSKI THOMAS , SCHARN DIRK , SCHNATBAUM KARSTEN
IPC分类号： C07K7/54 , A61K38/00 , A61P1/00 , A61P1/04 , A61P3/10 , A61P7/02 , A61P9/00 , A61P9/10 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P21/04 , A61P25/00 , A61P27/02 , A61P29/00 , A61P31/04 , A61P37/02 , A61P37/06 , A61P43/00 , C07K7/06 , C07K7/50 , C07K7/56 , C07K7/64 , C07K14/47 , C07K14/705
CPC分类号： C07K7/56 , C07K14/705
摘要： PROBLEM TO BE SOLVED: To provide a C5a receptor antagonist.
SOLUTION: The present invention relates to the C5a receptor antagonist represented by formula (I) [wherein, in one embodiment, X1 is a radical having a mass of about 1-300 and preferably selected from the group consisting of R5-, R5-CO-, R5-N(R6)-CO-, R5-O-CO-, R5-SO2-, R5-N(R6)-C(NH)-, wherein R5 and R6 are individually and independently selected from the group consisting of H, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, heterocyclyl, substituted heterocyclyl, aryl and substituted aryl; X2 and X6 are individually and independently aromatic amino acids, derivatives or analogs thereof, X5 and X7 are individually and independently hydrophobic amino acids, derivatives or analogs thereof].
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供C5a受体拮抗剂。解决方案：本发明涉及由式（I）表示的C5a受体拮抗剂[其中，在一个实施方案中，X 1为质量约1-300的基团，优选选自R5-， R5-CO-，R5-N（R6）-CO-，R5-O-CO-，R5-SO2-，R5-N（R6）-C（NH） - ，其中R5和R6各自独立地选自由H，烷基，取代的烷基，环烷基，取代的环烷基，杂环基，取代的杂环基，芳基和取代的芳基组成的基团; X 2和X 6各自独立地为芳族氨基酸，其衍生物或类似物，X5和X7各自独立地为疏水性氨基酸，其衍生物或类似物]。版权所有（C）2011，JPO＆INPIT

2. 发明申请

WO2009036996A2 SMALL MOLECULE BRADYKININ B1 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：小分子BRADYKININ B1受体拮抗剂
公开(公告)号：WO2009036996A2
公开(公告)日：2009-03-26
申请号：PCT/EP2008007919
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 , A61K31/506 , A61P29/00 , C07C209/00 , C07D207/20 , C07D213/82 , C07D213/89 , C07D239/42 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D417/12
CPC分类号： C07D403/12 , C07C237/42 , C07C281/06 , C07C2601/02 , C07D207/06 , C07D207/20 , C07D213/82 , C07D213/89 , C07D239/42 , C07D401/12 , C07D401/14 , C07D413/12 , C07D417/12
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.
摘要翻译：公开了式（I）化合物，其为缓激肽B1受体（B1R）拮抗剂。这些化合物可用于治疗疾病或缓解与炎症和疼痛相关的不良症状。本发明包括新型化合物及其可接受的衍生物，用于预防和治疗涉及炎症和疼痛的疾病的药物组合物和方法。

3. 发明申请

WO2005010030A2 C5A RECEPTOR ANTAGONISTS 审中-公开
标题翻译： C5a受体拮抗剂
公开(公告)号：WO2005010030A2
公开(公告)日：2005-02-03
申请号：PCT/EP2004008057
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： A61K38/00 , C07K7/06 , C07K7/50 , C07K7/56 , C07K14/47 , C07K14/705 , C07K7/00
CPC分类号： C07K7/56 , C07K14/705
摘要： The invention relates to a C5a receptor antagonist of structure (I), wherein X1 is a radical having a mass of about 1-300 and stands for 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-, R5-B(OH)- or R5-CH=N-O-CH2-CO-, wherein R5/R6 represent 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 or substituted aryloxyalkyl; X2 = radical (biological bonding properties of a mimicrying phenylalanine unit); X3/X4 = spacer (amino acids, amino-acid analogs and amino-acid derivatives); X5 = radical (biological bonding properties of a mimicrying cyclohexylalanine or homoleucine unit); X6 = radical (biological bonding properties of a mimicrying tryptophan unit); X7 = radical (biological bonding properties of a mimicrying norleucine or phenylalanine unit), a chemical bond being formed between X3 and X7.
摘要翻译： C5a受体拮抗剂，其具有结构（I），其中X为基团具有约1-300的质量，并且其中X 1是R 5 - ，R 5 -CO-，R 5-N（R6）-CO-，R5-O -CO-，R 5 -SO 2 - ，R 5-N（R 6）-SO 2 - ，R 5-N（R6） - ，R 5-N（R6） - CS-，R5-N（R 6）-C（NH） - ， - R5-CS-，R5-P（O）OH-，R 5-B（OH） - ，或R 5-CH = NO-CH 2 CO-，其中R 5 / R 6是H，F，羟基，烷基，取代的烷基，环烷基，取代环烷基，杂环基，取代的杂环基，芳基烷基，取代芳烷基，芳基，取代芳基，杂芳基，取代的杂芳基，酰基，取代酰基，烷氧基，烷氧基烷基，取代的烷氧基烷基，芳氧基烷基或取代的芳氧基，X2 =自由基（生物结合苯丙氨酸的特征部分mimikrierend），X3 / X4 =间隔（氨基酸，氨基酸类似物和氨基酸衍生物），X5 =自由基（生物结合的Cyclohexylalanin-或高亮氨酸单元mimikrierend的特性），X6 =自由基（生物结合色氨酸Einhe的特征它mimikrierend），X7 =正亮氨酸或苯丙氨酸单元mimikrierend的自由基（生物结合特征，一个化学键X3和X7）之间形成。

4. 发明专利

CA2607862A1 C5A RECEPTOR ANTAGONISTS 未知
公开(公告)号：CA2607862A1
公开(公告)日：2006-12-07
申请号：CA2607862
申请日：2006-05-30
申请人： JERINI AG
发明人： LOCARDI ELSA , RICHTER UWE , POLAKOWSKI THOMAS , SCHNATBAUM KARSTEN , SCHARN DIRK , REINEKE ULRICH , HUMMEL GERD
IPC分类号： C07C275/40 , A61K31/17
摘要： Phenyl amino compounds (I) (C5a receptor antagonist) are new. Phenyl amino compounds of formula (I) (C5a receptor antagonist) are new. R 1>-R 22>alkyl, alkenyl, alkynyl, (cyclo)alkyl, heterocyclyl, (hetero)aryl, (hetero)arylalkyl, alkoxyl, aryloxy, arylalkyloxy, acyloxy, acyl, alkylthio, amino, alkylamino, bisalkyl amino, cyclic amino, carbamoyl (CONH 2), sulfamoyl (SO 2NH 2) (all optionally substituted), H, halo, OH, NO 2, CN, mercapto, carboxyl, carbamate, alkoxycarbonyl, acylamino, haloalkyl, haloalkyloxy, C(O)H, trialkylsilyl or azido. An independent claim is included for a combination of an antagonist of the bradykinine receptor 2 and a C5a receptor antagonist for the therapy of severe burn injury. [Image] ACTIVITY : Immunosuppressive; Endocrine-Gen.; Muscular-Gen.; Immunomodulator; Neuroprotective; Gastrointestinal-Gen.; Antiulcer; Dermatological; Nephrotropic; CNS-Gen.; Thyromimetic; Hepatotropic; Virucide; Hemostatic; Auditory; Antiarthritic; Antirheumatic; Cardiovascular-Gen.; Analgesic; Antianginal; Antipruritic; Antibacterial; Vasotropic; Ophthalmological; Uropathic; Vulnerary; Antipyretic; Antipsoriatic; Antiinflammatory; Tranquilizer; Antimicrobial; Respiratory-Gen.; Cerebroprotective; Cardiant; Cytostatic; Antiasthmatic; Antidiabetic; Anticoagulant; Antiparasitic. MECHANISM OF ACTION : C5a receptor antagonist. The C5a receptor antagonistic activity of (I) was tested using biological assays. The results showed that (S)-3-(3-amino-5-chloro-2,6-diethyl-phenyl)-1-(4-isopropyl-phenyl)-1-(1-para-tolyl-ethyl)-urea exhibited the IC 5 0 value of 32 nM.

5. 发明专利

BRPI0809231A2 未知
公开(公告)号：BRPI0809231A2
公开(公告)日：2014-09-02
申请号：BRPI0809231
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 , A61K31/4709 , A61P29/00 , C07D405/14 , C07D409/14 , 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 A is a 6-membered heteroaryl having 1 heteroatom, wherein said heteroatom is N, and R 5 -R 8 ; R 17 are as defined in the claims, and their use as bradykinin B 2 receptor modulators.

6. 发明专利

CA2681206A1 SMALL MOLECULE BRADYKININ B2 RECEPTOR MODULATORS 未知
公开(公告)号：CA2681206A1
公开(公告)日：2008-10-02
申请号：CA2681206
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 , A61K31/4709 , A61P29/00 , 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.

7. 发明专利

MX2007015092A ANTAGONISTAS DEL RECEPTOR C5A. 未知
公开(公告)号：MX2007015092A
公开(公告)日：2008-04-14
申请号：MX2007015092
申请日：2006-05-30
申请人： JERINI AG
发明人： HUMMEL GERD , REINEKE ULRICH , LOCARDI ELSA , POLAKOWSKI THOMAS , SCHARN DIRK , SCHNATBAUM KARSTEN , RICHTER UWE
IPC分类号： A61K31/17 , C07C275/40
摘要： La presente invencion se refiere a un compuesto, de preferencia un antagonista del receptor C5a, que tiene la siguiente estructura, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21 y R22 se seleccionan individualmente e independientemente del grupo que comprende H, alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, cicloalquilo, cicloalquilo sustituido, heterociclilo, heterociclilo sustituido, arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, arilalquilo, arilalquilo sustituido, heteroarilalquilo, heteroarilalquilo sustituido, alcoxilo, alcoxilo sustituido, ariloxi, ariloxi sustituido, arilalquiloxi, arilalquiloxi sustituido aciloxi, aciloxi sustituido, halogeno, hidroxilo, nitro, ciano, acilo, acilo sustituido, mercapto, alquiltio, alquiltio sustituido, amino, amino sustituido, alquilamino, alquilamino sustituido, bisalquilamino, bisalquilamino sustituido, amino ciclico, amino ciclico sustituido, carbamoilo (-CONH2), carbamoilo sustituido, carboxilo, carbamato, alcoxicarbonilo, alcoxicarbonilo sustituido, acilamino, acilamino sustituido, sulfamoilo (-SO2NH2), sulfamoilo sustituido, haloalquilo, haloalquiloxi, C(O)H, trialquilsililo y azido.

8. 发明专利

CA2681206C 8-(HETEROARYLMETHOXY)QUINOLINE COMPOUNDS AS BRADYKININ B2 RECEPTOR MODULATORS 未知
公开(公告)号：CA2681206C
公开(公告)日：2014-04-29
申请号：CA2681206
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 , A61K31/4709 , A61P29/00 , 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.

9. 发明专利

BRPI0610875A2 未知
公开(公告)号：BRPI0610875A2
公开(公告)日：2010-08-03
申请号：BRPI0610875
申请日：2006-05-30
申请人： JERINI AG
发明人： SCHNATBAUM KARSTEN , LOCARDI ELSA , POLAKOWSKI THOMAS , RICHTER UWE , SCHARN DIRK , REINEKE ULRICH , HUMMEL GERD
IPC分类号： C07C275/40 , A61K31/17
摘要： Phenyl amino compounds (I) (C5a receptor antagonist) are new. Phenyl amino compounds of formula (I) (C5a receptor antagonist) are new. R 1>-R 22>alkyl, alkenyl, alkynyl, (cyclo)alkyl, heterocyclyl, (hetero)aryl, (hetero)arylalkyl, alkoxyl, aryloxy, arylalkyloxy, acyloxy, acyl, alkylthio, amino, alkylamino, bisalkyl amino, cyclic amino, carbamoyl (CONH 2), sulfamoyl (SO 2NH 2) (all optionally substituted), H, halo, OH, NO 2, CN, mercapto, carboxyl, carbamate, alkoxycarbonyl, acylamino, haloalkyl, haloalkyloxy, C(O)H, trialkylsilyl or azido. An independent claim is included for a combination of an antagonist of the bradykinine receptor 2 and a C5a receptor antagonist for the therapy of severe burn injury. [Image] ACTIVITY : Immunosuppressive; Endocrine-Gen.; Muscular-Gen.; Immunomodulator; Neuroprotective; Gastrointestinal-Gen.; Antiulcer; Dermatological; Nephrotropic; CNS-Gen.; Thyromimetic; Hepatotropic; Virucide; Hemostatic; Auditory; Antiarthritic; Antirheumatic; Cardiovascular-Gen.; Analgesic; Antianginal; Antipruritic; Antibacterial; Vasotropic; Ophthalmological; Uropathic; Vulnerary; Antipyretic; Antipsoriatic; Antiinflammatory; Tranquilizer; Antimicrobial; Respiratory-Gen.; Cerebroprotective; Cardiant; Cytostatic; Antiasthmatic; Antidiabetic; Anticoagulant; Antiparasitic. MECHANISM OF ACTION : C5a receptor antagonist. The C5a receptor antagonistic activity of (I) was tested using biological assays. The results showed that (S)-3-(3-amino-5-chloro-2,6-diethyl-phenyl)-1-(4-isopropyl-phenyl)-1-(1-para-tolyl-ethyl)-urea exhibited the IC 5 0 value of 32 nM.

10. 发明专利

BRPI0606647A2 未知
公开(公告)号：BRPI0606647A2
公开(公告)日：2009-07-14
申请号：BRPI0606647
申请日：2006-01-17
申请人： JERINI AG
发明人： HUMMEL GERD , SCHARN DIRK , LOCARDI ELSA , POLAKOWSKI THOMAS , SCHNATBAUM KARSTEN
IPC分类号： C07K7/06 , C07K7/56 , C07K7/64 , C07K14/47 , C07K14/705
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.

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