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公开(公告)号:US08466108B2
公开(公告)日:2013-06-18
申请号:US12643818
申请日:2009-12-21
申请人: Michael Dockal , Hartmut Ehrlich , Friedrich Scheiflinger , Ulf Reimer , Ulrich Reineke , Thomas Polakowski , Eberhard Schneider
发明人: Michael Dockal , Hartmut Ehrlich , Friedrich Scheiflinger , Ulf Reimer , Ulrich Reineke , Thomas Polakowski , Eberhard Schneider
IPC分类号: A61K38/36 , A61K38/37 , A61K38/10 , A61K38/00 , A61K38/04 , A61K38/16 , C07K14/745 , C07K14/755
CPC分类号: C07K14/4703 , A61K38/00 , A61K47/551 , A61K47/557 , A61K47/60 , C07K7/08 , C07K14/001 , Y02A50/463
摘要: The invention provides peptides that bind Tissue Factor Pathway Inhibitor (TFPI), including TFPI-inhibitory peptides, and compositions thereof. The peptides may be used to inhibit a TFPI, enhance thrombin formation in a clotting factor-deficient subject, increase blood clot formation in a subject, and/or treat a blood coagulation disorder in a subject.
摘要翻译: 本发明提供了结合组织因子途径抑制剂(TFPI),包括TFPI抑制肽的肽及其组合物。 肽可以用于抑制TFPI,增强凝血因子缺陷受试者中的凝血酶形成,增加受试者中的血块形成和/或治疗受试者的血液凝固障碍。
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公开(公告)号:US20100173847A1
公开(公告)日:2010-07-08
申请号:US12643818
申请日:2009-12-21
申请人: Michael Dockal , Hartmut Ehrlich , Friedrich Scheiflinger , Ulf Reimer , Ulrich Reineke , Thomas Polakowski , Eberhard Schneider
发明人: Michael Dockal , Hartmut Ehrlich , Friedrich Scheiflinger , Ulf Reimer , Ulrich Reineke , Thomas Polakowski , Eberhard Schneider
CPC分类号: C07K14/4703 , A61K38/00 , A61K47/551 , A61K47/557 , A61K47/60 , C07K7/08 , C07K14/001 , Y02A50/463
摘要: The invention provides peptides that bind Tissue Factor Pathway Inhibitor (TFPI), including TFPI-inhibitory peptides, and compositions thereof. The peptides may be used to inhibit a TFPI, enhance thrombin formation in a clotting factor-deficient subject, increase blood clot formation in a subject, and/or treat a blood coagulation disorder in a subject.
摘要翻译: 本发明提供了结合组织因子途径抑制剂(TFPI),包括TFPI抑制肽的肽及其组合物。 肽可以用于抑制TFPI,增强凝血因子缺陷受试者中的凝血酶形成,增加受试者中的血块形成和/或治疗受试者的血液凝固障碍。
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公开(公告)号:US08450275B2
公开(公告)日:2013-05-28
申请号:US13026070
申请日:2011-02-11
申请人: Michael Dockal , Rudolf Hartmann , Markus Fries , Friedrich Scheiflinger , Hartmut Ehrlich , Ulrich Reineke , Frank Osterkamp , Thomas Polakowski
发明人: Michael Dockal , Rudolf Hartmann , Markus Fries , Friedrich Scheiflinger , Hartmut Ehrlich , Ulrich Reineke , Frank Osterkamp , Thomas Polakowski
IPC分类号: A61K38/57
CPC分类号: A61K38/10 , A61K38/00 , A61K2121/00 , C07K1/14 , C07K7/08 , C07K14/00 , C07K14/8114 , G01N33/68 , G01N2333/745 , G01N2333/8114 , G01N2333/96444 , G01N2333/96447 , G01N2500/02 , G01N2500/04 , G01N2500/20 , G06F19/16 , G06F19/18
摘要: The invention provides peptides that bind Tissue Factor Pathway Inhibitor (TFPI), including TFPI-inhibitory peptides, and compositions thereof. The peptides may be used to inhibit a TFPI, enhance thrombin formation in a clotting factor-deficient subject, increase blood clot formation in a subject, treat a blood coagulation disorder in a subject, purify TFPI, and identify a TFPI-binding compound.
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公开(公告)号:US08410134B2
公开(公告)日:2013-04-02
申请号:US12532703
申请日:2008-03-22
申请人: Christoph Gibson , Thomas Tradler , Karsten Schnatbaum , Jochen Pfeifer , Elsa Locardi , Dirk Scharn , Matthias Paschke , Ulf Reimer , Uwe Richter , Gerd Hummel , Ulrich Reineke
发明人: Christoph Gibson , Thomas Tradler , Karsten Schnatbaum , Jochen Pfeifer , Elsa Locardi , Dirk Scharn , Matthias Paschke , Ulf Reimer , Uwe Richter , Gerd Hummel , Ulrich Reineke
IPC分类号: A61K31/04 , C07D215/38
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。
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公开(公告)号:US20110077381A1
公开(公告)日:2011-03-31
申请号:US12888556
申请日:2010-09-23
申请人: Frank Osterkamp , Heiko Hawlisch , Gerd Hummel , Tobias Knaute , Ulf Reimer , Ulrich Reineke , Uwe Richter , Bernadett Simon , Edgar Specker , Markus Woischnik , Mark R. Hellberg
发明人: Frank Osterkamp , Heiko Hawlisch , Gerd Hummel , Tobias Knaute , Ulf Reimer , Ulrich Reineke , Uwe Richter , Bernadett Simon , Edgar Specker , Markus Woischnik , Mark R. Hellberg
IPC分类号: C07K7/06
摘要: Disclosed are novel compounds having NPR-B agonistic activity. Preferred compounds are linear peptides containing 8-13 conventional or non-conventional L- or D-amino acid residues connected to one another via peptide bonds.
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6.8-OXY-QUINOLINE DERIVATIVES AS BRADYKININ B2 RECEPTOR MODULATORS 失效
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:US20100234344A1
公开(公告)日:2010-09-16
申请号:US12532703
申请日:2008-03-22
申请人: Christoph Gibson , Thomas Tradler , Karsten Schinatbaum , Jochen Pfeifer , Elsa Locardi , Dirk Scharn , Mathias Paschke , Ulf Reimer , Uwe Richter , Gerd Hummel , Ulrich Reineke
发明人: Christoph Gibson , Thomas Tradler , Karsten Schinatbaum , Jochen Pfeifer , Elsa Locardi , Dirk Scharn , Mathias Paschke , Ulf Reimer , Uwe Richter , Gerd Hummel , Ulrich Reineke
IPC分类号: A61K31/4709 , A61K31/541 , A61K31/5355 , A61K31/5377 , A61K31/496 , C07D417/14 , C07D413/14 , C07D401/14 , A61P9/00 , A61P1/18 , A61P13/12 , A61P1/16 , A61P3/00 , A61P37/08 , A61P5/00 , A61P35/00 , A61P7/00 , C12N5/071 , G01N33/53
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。
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公开(公告)号:US08546523B2
公开(公告)日:2013-10-01
申请号:US12888556
申请日:2010-09-23
申请人: Frank Osterkamp , Heiko Hawlisch , Gerd Hummel , Tobias Knaute , Ulf Reimer , Ulrich Reineke , Uwe Richter , Bernadett Simon , Edgar Specker , Markus Woischnik , Mark R. Hellberg
发明人: Frank Osterkamp , Heiko Hawlisch , Gerd Hummel , Tobias Knaute , Ulf Reimer , Ulrich Reineke , Uwe Richter , Bernadett Simon , Edgar Specker , Markus Woischnik , Mark R. Hellberg
IPC分类号: A61K38/00
摘要: Disclosed are novel compounds having NPR-B agonistic activity. Preferred compounds are linear peptides containing 8-13 conventional or non-conventional L- or D-amino acid residues connected to one another via peptide bonds.
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公开(公告)号:US08071810B2
公开(公告)日:2011-12-06
申请号:US11915892
申请日:2006-05-30
申请人: Karsten Schnatbaum , Dirk Scharn , Elsa Locardi , Thomas Polakowski , Uwe Richter , Ulrich Reineke , Gerd Hummel
发明人: Karsten Schnatbaum , Dirk Scharn , Elsa Locardi , Thomas Polakowski , Uwe Richter , Ulrich Reineke , Gerd Hummel
IPC分类号: C07C275/00 , C07C273/00
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, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, 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 (—CONH2), substituted carbamoyl, carboxyl, carbamate, alkoxycarbonyl, substituted alkoxycarbonyl, acylamino, substituted acylamino, sulfamoyl (—SO2NH2), 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,R10,R11,R12,R13,R14,R15, R16,R17,R18,R19,R20,R21和R22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,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) 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,取代的酰氨基,氨磺酰基(-SO2NH2),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。
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公开(公告)号:US20080220003A1
公开(公告)日:2008-09-11
申请号:US11915892
申请日:2006-05-30
申请人: Karsten Schnatbaum , Dirk Scharn , Elsa Locardi , Thomas Polakowski , Uwe Richter , Ulrich Reineke , Gerd Hummel
发明人: Karsten Schnatbaum , Dirk Scharn , Elsa Locardi , Thomas Polakowski , Uwe Richter , Ulrich Reineke , Gerd Hummel
IPC分类号: A61K38/13 , C07C275/28 , C07D213/02 , C07D235/24 , C07D209/14 , A61K31/17 , A61K31/436 , A61K31/57 , A61K39/395 , A61K31/196 , A61K31/65 , A61K31/4545 , A61K31/519 , A61K31/44 , A61K31/4184 , A61K31/4045 , A61K31/47 , A61P37/06 , A61P29/00
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, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, 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 (—CONH2), substituted carbamoyl, carboxyl, carbamate, alkoxycarbonyl, substituted alkoxycarbonyl, acylamino, substituted acylamino, sulfamoyl (—SO2NH2), 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,R10,R11,R12,R13,R14,R15, R16,R17,R18,R19,R20,R21和R22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,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。
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公开(公告)号:US20090104116A1
公开(公告)日:2009-04-23
申请号:US12162798
申请日:2007-01-31
申请人: Gunter Zischinsky , Roland Stragies , Frank Osterkamp , Dirk Scharn , Gerd Hummel , Holger Kalkhof , Grit Zahn , Doerte Vossmeyer , Claudia Christner-Albrecht , Ulrich Reineke
发明人: Gunter Zischinsky , Roland Stragies , Frank Osterkamp , Dirk Scharn , Gerd Hummel , Holger Kalkhof , Grit Zahn , Doerte Vossmeyer , Claudia Christner-Albrecht , Ulrich Reineke
IPC分类号: A61K51/04 , C07D401/12 , A61K31/4427 , C07D471/04 , A61K31/4375 , A61K49/04 , A61P35/00 , A61K49/10 , A61K31/535 , C07D265/08 , C12N9/00
CPC分类号: C07D401/12 , C07D471/04
摘要: The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; Ψ is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.
摘要翻译: 本发明涉及式(I)化合物,其中A是非芳族杂环,Ar不存在或亚苯基; Psi是式(II)的基团,R2是疏水部分; 并且G是含有一个或多个选自NH,OH和碱性部分的部分的基团。 化合物是整联蛋白的抑制剂,特别是纤连蛋白受体α5β1的拮抗剂,可用作抗血管生成剂。
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