公开(公告)号：EP1506193B1

公开(公告)日：2006-06-21

申请号：EP03727359.6

申请日：2003-04-25

申请人： Bayer HealthCare AG

发明人： ALONSO-ALIJA, Cristina ,  BISCHOFF, Erwin ,  MÜNTER, Klaus ,  STASCH, Johannes-Peter ,  STAHL, Elke ,  WEIGAND, Stefan ,  FEURER, Achim

IPC分类号： C07D471/04 ,  A61K31/506 ,  A61P9/02

CPC分类号： C07D471/04 ,  A61K31/506 ,  A61K45/06 ,  A61K2300/00

摘要： The invention relates to compounds of formula (I), wherein R1 represents -NR3C (=0) OR4, R2 represents hydrogen or NH2, R3 represents hydrogen or (C1-C4) alkyl and R4 represents (C1-C6) alkyl, which stimulate soluble guanylate cyclase and to their production and use as medicaments, in particular as medicaments for treating cardiovascular disease and/or sexual dysfunction.

公开(公告)号：EP1406908A1

公开(公告)日：2004-04-14

申请号：EP02745409.9

申请日：2002-06-25

申请人： Bayer HealthCare AG

发明人： FEURER, Achim ,  FLUBACHER, Dietmar ,  WEIGAND, Stefan ,  STASCH, Johannes-Peter ,  STAHL, ELke ,  SCHENKE, Thomas ,  ALONSO-ALIJA, Cristina ,  WUNDER, Frank ,  LANG, Dieter ,  DEMBOWSKY, Klaus ,  STRAUB, Alexander ,  PERZBORN, Elisabeth

IPC分类号： C07D519/00 ,  C07D471/04 ,  C07D498/08 ,  A61K31/5386 ,  A61P7/02 ,  A61P9/10

CPC分类号： C07D471/04

摘要： The invention relates to novel pyrazolopyridine derivatives of formula (I), wherein R1 represents (a) or (b) and n represents 1 or 2 and R2 represents H NH¿2?. The invention also relates to salts, isomers and hydrates thereof as stimulators for soluble guanylate cyclase and to their use as agents in the treatment of cardiovascular diseases, hypertonicity, thrombo-embolic diseases and ischemia, sexual dysfunction or inflammations and for the treatment of diseases of the central nervous system.

公开(公告)号：EP1339714B1

公开(公告)日：2006-10-18

申请号：EP01989460.9

申请日：2001-11-12

申请人： Bayer HealthCare AG

发明人： STASCH, Johannes-Peter ,  FEURER, Achim ,  WEIGAND, Stefan ,  STAHL, Elke ,  FLUBACHER, Dietmar ,  ALONSO-ALIJA, Cristina ,  WUNDER, Frank ,  LANG, Dieter ,  DEMBOWSKY, Klaus ,  STRAUB, Alexander ,  PERZBORN, Elisabeth

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P9/00 ,  A61P15/00 ,  C07D231/00 ,  C07D221/00

CPC分类号： C07D471/04

摘要： The invention relates to novel pyrazolopyridine derivatives of formula (I) wherein R1 represents H, Cl or NH¿2?, and R?2 and R3¿ form, together with the heteroatoms to which they are bonded, a five to six-membered heterocycle which can be saturated or partially unsaturated, can optionally contain at least one other heteroatom from the group N, O, S and can be optionally substituted. The invention also relates to salts, isomers and hydrates of said derivatives, in the form of stimulators of soluble guanylate cyclase and as agents for treating cardiovascular diseases, hypertonia, thrombo-embolic diseases and ischaemia, sexual dysfunction, inflammations, and diseases of the central nervous system.

公开(公告)号：EP1578418A2

公开(公告)日：2005-09-28

申请号：EP03813560.4

申请日：2003-12-06

申请人： Bayer HealthCare AG

发明人： ERGÜDEN, Jens ,  KRAHN, Thomas ,  SCHRÖDER, Christian ,  STASCH, Johannes, Peter ,  WEIGAND, Stefan ,  WILD, Hanno ,  BRANDS, Michael ,  SIEGEL, Stephan ,  HEIMBACH, Dirk ,  KELDENICH, Jörg ,  TAJIMI, Masaomi ,  TAKAGI, Hiroko

IPC分类号： A61K31/404 ,  A61K31/4439 ,  A61K31/405 ,  A61K31/433 ,  A61P13/00 ,  A61P13/08 ,  A61P13/10

CPC分类号： A61K31/433 ,  A61K31/404 ,  A61K31/405 ,  A61K31/4439

摘要： The present invention relates to the use of 2,5-diamidoindole derivatives for the preparation of medicaments for treating urological disorders in humans and/or animals, by virtue of their endothelin-converting enzyme (ECE) inhibitory activity.

公开(公告)号：EP1425283B1

公开(公告)日：2005-03-16

申请号：EP02796211.7

申请日：2002-08-09

申请人： Bayer HealthCare AG

发明人： BISCHOFF, Erwin ,  HAUSWALD, Markus ,  NELL, Peter ,  RÖHRIG, Susanne ,  SCHLEMMER, Karl-Heinz ,  STEINHAGEN, Henning ,  STOLTEFUSS, Jürgen ,  WEIGAND, Stefan

IPC分类号： C07D491/04 ,  A61K31/519 ,  A61P9/00

CPC分类号： C07D491/04

公开(公告)号：EP1339716B1

公开(公告)日：2004-11-03

申请号：EP01997487.2

申请日：2001-11-09

申请人： Bayer HealthCare AG

发明人： STASCH, Johannes-Peter ,  FEURER, Achim ,  WEIGAND, Stefan ,  STAHL, Elke ,  FLUBACHER, Dietmar ,  ALONSO-ALIJA, Cristina ,  WUNDER, Frank ,  LANG, Dieter ,  DEMBOWSKY, Klaus ,  STRAUB, Alexander ,  PERZBORN, Elisabeth

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P9/00 ,  A61P15/00 ,  A61P25/00

CPC分类号： C07D471/04

摘要： The invention relates to novel pyrazolopyridine derivatives of formula (I) wherein R1 represents NH¿2? or NHCO-C1-6-alkyl, and R?2¿ represents a radical of formula R3NCOR4 which is bonded to the radical of the molecule by means of the nitrogen atom, R?3 and R4¿ forming, together with the amide group to which they are bonded, a five to six-membered heterocycle which can be saturated or partially unsaturated, can optionally contain another heteroatom from the group N, O, S and can comprise between one and five other substituents from the group oxo, C1-6 alkyl, hydroxy, hydroxy-C¿1-6?-alkyl, halogen, or can be anellated to a C6-10 aryl ring or a C3-8 cycloalkyl ring in which optionally two carbon atoms are bonded to each other by means of an oxygen atom. The invention also relates to salts, isomers and hydrates of said derivatives, in the form of stimulators of soluble guanylate cyclase and as agents for treating cardiovascular diseases, hypertonia, thrombo-embolic diseases and ischaemia, sexual dysfunction, inflammations, and diseases of the central nervous system.

公开(公告)号：EP1425283A1

公开(公告)日：2004-06-09

申请号：EP02796211.7

申请日：2002-08-09

申请人： Bayer HealthCare AG

发明人： BISCHOFF, Erwin ,  HAUSWALD, Markus ,  NELL, Peter ,  RÖHRIG, Susanne ,  SCHLEMMER, Karl-Heinz ,  STEINHAGEN, Henning ,  STOLTEFUSS, Jürgen ,  WEIGAND, Stefan

IPC分类号： C07D491/04 ,  A61K31/519 ,  A61P9/00

CPC分类号： C07D491/04

摘要： The invention relates to compounds of formula (I), a method for the production thereof in addition to the use thereof as medicaments.

公开(公告)号：EP1432415B1

公开(公告)日：2005-12-28

申请号：EP02767488.6

申请日：2002-09-16

申请人： Bayer HealthCare AG

发明人： ERGÜDEN, Jens-Kerim ,  KRAHN, Thomas ,  SCHRÖDER, Christian ,  STASCH, Johannes-Peter ,  WEIGAND, Stefan ,  WILD, Hanno ,  BRANDS, Michael ,  SIEGEL, Stephan ,  HEIMBACH, Dirk ,  KELDENICH, Jörg

IPC分类号： A61K31/404 ,  A61K31/4439 ,  A61K31/4245 ,  A61K31/506 ,  A61K31/4178 ,  C07D209/42 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12 ,  C07D403/12 ,  C07D417/06

CPC分类号： C07D401/12 ,  C07D209/42

公开(公告)号：EP1509228A1

公开(公告)日：2005-03-02

申请号：EP03722593.5

申请日：2003-05-05

申请人： Bayer HealthCare AG

发明人： WEIGAND, Stefan ,  BISCHOFF, Erwin ,  MÜNTER, Klaus ,  STASCH, Johannes-Peter ,  STAHL, Elke

IPC分类号： A61K31/505 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P15/10 ,  C07D471/04

CPC分类号： C07D471/04

摘要： The invention relates to novel chemical compounds of formula (I), which stimulate soluble guanylate cyclase, to the production and use thereof as medicament, particularly in the treatment of cardiovascular diseases and/or sexual dysfunction (I), wherein R1' represents chlorine, cyano, trifluoromethyl or methoxy and R2 represents hydrogen or fluorine or R1 represents fluorine and R2 represents fluorine. The invention also relates to the salts, isomers and hydrates of said compounds.

摘要翻译： 本发明涉及刺激可溶性鸟苷酸环化酶的新型式（I）化学化合物，涉及其作为药物的生产和用途，特别是治疗心血管疾病和/或性功能障碍（I），其中R1'代表氯， 氰基，三氟甲基或甲氧基，R2代表氢或氟，或R1代表氟，R2代表氟。 本发明还涉及所述化合物的盐，异构体和水合物。

公开(公告)号：EP1799210A1

公开(公告)日：2007-06-27

申请号：EP05787684.9

申请日：2005-09-23

申请人： Bayer HealthCare AG

发明人： WEIGAND, Stefan ,  FREY, Reiner ,  STASCH, Johannes-Peter

IPC分类号： A61K31/437 ,  A61K31/197 ,  A61K33/00 ,  A61P11/06

CPC分类号： A61K31/197 ,  A61K31/437 ,  A61K33/00 ,  A61K2300/00

摘要： This invention relates to the use of a soluble guanylate cyclase stimulator in combination with gaseous nitric for treatment and prevention of asthma or other forms of bronchoconstriction or reversible pulmonary vasoconstriction in a mammal, especially in a newborn.