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1. 发明申请

WO2010071894A3 TFPI INHIBITORS AND METHODS OF USE 审中-公开
公开(公告)号：WO2010071894A3
公开(公告)日：2010-06-24
申请号：PCT/US2009/069060
申请日：2009-12-21
申请人： BAXTER INTERNATIONAL INC. , BAXTER HEALTHCARE S.A. , 3B PHARMACEUTICALS GMBH , COSMIX MOLECULAR BIOLOGICALS GMBH , DOCKAL, Michael , EHRLICH, Hartmut , SCHEIFLINGER, Friedrich , REIMER, Ulf , REINEKE, Ulrich , POLAKOWSKI, Thomas , SCHNEIDER, Eberhard
发明人： DOCKAL, Michael , EHRLICH, Hartmut , SCHEIFLINGER, Friedrich , REIMER, Ulf , REINEKE, Ulrich , POLAKOWSKI, Thomas , SCHNEIDER, Eberhard
IPC分类号： A61K38/00
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.

2. 发明申请

WO2011115712A2 TFPI INHIBITORS AND METHODS OF USE 审中-公开
标题翻译： TFPI抑制剂及其使用方法
公开(公告)号：WO2011115712A2
公开(公告)日：2011-09-22
申请号：PCT/US2011/024604
申请日：2011-02-11
申请人： BAXTER INTERNATIONAL INC , BAXTER HEAL THCARE S.A. , 3B PHARMACEUTICALS GMBH , DOCKAL, Michael , HARTMANN, Rudolf , FRIES, Markus , SCHEIFLINGER, Friedrich , EHRLICH, Hartmut , REINEKE, Ulrich , OSTERKAMP, Frank , POLAKOWSKI, Thomas
发明人： DOCKAL, Michael , HARTMANN, Rudolf , FRIES, Markus , SCHEIFLINGER, Friedrich , EHRLICH, Hartmut , REINEKE, Ulrich , OSTERKAMP, Frank , POLAKOWSKI, Thomas
IPC分类号： A61K38/18
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.
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，治疗受试者的血液凝固障碍，纯化TFPI和鉴定TFPI结合化合物。

3. 发明申请

WO2011075471A2 NOVEL NPR-B AGONISTS AND METHODS OF USE FOR THE TREATMENT OF C-TYPE NATRIURETIC PEPTIDE-MEDIATED DISORDERS 审中-公开
标题翻译：新型NPR-B激动剂和治疗C型脑脊液介导性疾病的方法
公开(公告)号：WO2011075471A2
公开(公告)日：2011-06-23
申请号：PCT/US2010/060263
申请日：2010-12-14
申请人： ALCON RESEARCH, LTD. , OSTERKAMP, Frank , HAWLISCH, Heiko , HUMMEL, Gerd , KNAUTE, Tobias , REIMER, Ulf , REINEKE, Ulrich , SIMON, Bernadett , RICHTER, Uwe , SPECKER, Edgar , WOISCHNIK, Markus
发明人： OSTERKAMP, Frank , HAWLISCH, Heiko , HUMMEL, Gerd , KNAUTE, Tobias , REIMER, Ulf , REINEKE, Ulrich , SIMON, Bernadett , RICHTER, Uwe , SPECKER, Edgar , WOISCHNIK, Markus
IPC分类号： A61K38/08
CPC分类号： A61K38/08 , A61K38/2242
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. Also disclosed are methods of treating C-type natriuretic peptide (CNP)-mediated disorders, including glaucoma and/or elevated intraocular pressure, in a subject using pharmaceutical compositions that include a novel NPR-B agonist as described herein.
摘要翻译：公开了具有NPR-B激动活性的新化合物。优选的化合物是含有通过肽键相互连接的8-13个常规或非常规的L-或D-氨基酸残基的线性肽。还公开了使用包含如本文所述的新型NPR-B激动剂的药物组合物治疗受试者的C型利钠肽（CNP）介导的疾病（包括青光眼和/或升高的眼内压）的方法。

4. 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）。

5. 发明申请

WO2011038061A2 NOVEL NPR-B AGONISTS 审中-公开
公开(公告)号：WO2011038061A2
公开(公告)日：2011-03-31
申请号：PCT/US2010/049912
申请日：2010-09-23
申请人： ALCON RESEARCH, LTD. , OSTERKAMP, Frank , HAWLISCH, Heiko , HUMMEL, Gerd , KNAUTE, Tobias , REIMER, Ulf , REINEKE, Ulrich , RICHTER, Uwe , SIMON, Bernadett , SPECKER, Edgar , WOISCHNIK, Markus , HELLBERG, Mark R.
发明人： OSTERKAMP, Frank , HAWLISCH, Heiko , HUMMEL, Gerd , KNAUTE, Tobias , REIMER, Ulf , REINEKE, Ulrich , RICHTER, Uwe , SIMON, Bernadett , SPECKER, Edgar , WOISCHNIK, Markus , HELLBERG, Mark R.
IPC分类号： C07K7/06
CPC分类号： C07K7/06 , C07K7/02 , C07K7/08
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.
摘要翻译：公开了具有NPR-B激动剂活性的新型化合物。优选的化合物是含有8-13个通过肽键相互连接的常规或非常规L-或D-氨基酸残基的线性肽。

6. 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.

7. 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。

8. 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。

9. 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。

10. 发明申请

WO2022148843A1 COMPOUNDS COMPRISING A FIBROBLAST ACTIVATION PROTEIN LIGAND AND USE THEREOF 审中-公开
公开(公告)号：WO2022148843A1
公开(公告)日：2022-07-14
申请号：PCT/EP2022/050280
申请日：2022-01-07
申请人： 3B PHARMACEUTICALS GMBH
发明人： OSTERKAMP, Frank , ZBORALSKI, Dirk , SCHNEIDER, Eberhard , HAASE, Christian , PASCHKE, Matthias , HÖHNE, Aileen , UNGEWISS, Jan , SMERLING, Christiane , REINEKE, Ulrich , BREDENBECK, Anne , VON HACHT, Jan Lennart
IPC分类号： C07K7/02 , A61K51/08 , C07K7/08 , C07K14/81 , C12N9/48 , G01N33/543 , A61K38/00
摘要： The present invention is related to a compound comprising a cyclic peptide of formula (I) and an N-terminal modification group A attached to Xaa1, wherein each and any one of Xaa1, Xaa2, Xaa3, Xaa4, Xaa5, Xaa6 and Xaa7 is a residue of an amino acid, and Yc is a structure of formula (X).

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