公开(公告)号：US20050004207A1

公开(公告)日：2005-01-06

申请号：US10484369

申请日：2002-07-03

Applicant: Alexander Straub ,  Thomas Lampe ,  Jens Pohlmann ,  Susanne Rohrig ,  Stephan Jordan ,  Elisabeth Perzborn ,  Karl-Heinz Schlemmer

Inventor： Alexander Straub ,  Thomas Lampe ,  Jens Pohlmann ,  Susanne Rohrig ,  Stephan Jordan ,  Elisabeth Perzborn ,  Karl-Heinz Schlemmer

IPC: C07D473/00 ,  A61K31/4025 ,  A61K31/4035 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/422 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/506 ,  A61K31/52 ,  A61K31/5377 ,  A61P7/02 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P19/02 ,  A61P25/28 ,  A61P35/00 ,  C07D209/46 ,  C07D209/48 ,  C07D213/81 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D471/14 ,  C07D521/00 ,  A61K31/4015 ,  C07D207/40

CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D409/12 ,  C07D409/14 ,  C07D471/14

Abstract: The invention relates to the field of blood clotting, to novel compounds of formula (I), to a method for their production and to the use of these compounds as active ingredients in medicaments for preventing and/or treating diseases. The compounds are factor Xa inhibitors.

公开(公告)号：US06743798B1

公开(公告)日：2004-06-01

申请号：US09744830

申请日：2001-04-11

Applicant: Alexander Straub ,  Achim Feurer ,  Cristina Alonso-Alija ,  Johannes-Peter Stasch ,  Elisabeth Perzborn ,  Joachim Hütter ,  Klaus Dembowsky ,  Elke Stahl

Inventor： Alexander Straub ,  Achim Feurer ,  Cristina Alonso-Alija ,  Johannes-Peter Stasch ,  Elisabeth Perzborn ,  Joachim Hütter ,  Klaus Dembowsky ,  Elke Stahl

IPC: C07D40304

CPC classification number: C07D471/04

Abstract: The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which R1, R2, R3 and A are each as defined, and to processes for their preparation and to their use as medicaments, in particular as medicaments for the treatment of cardiovascular disorders.

Abstract translation: 本发明涉及通式（I）的新的取代的吡唑衍生物，其中R 1，R 2，R 3和A各自如上所定义，并且其制备方法及其用途 药物，特别是用于治疗心血管疾病的药物。

公开(公告)号：US06693102B2

公开(公告)日：2004-02-17

申请号：US10001569

申请日：2001-11-01

Applicant: Johannes-Peter Stasch ,  Achim Feurer ,  Stefan Weigand ,  Elke Stahl ,  Dietmar Flubacher ,  Cristina Alonso-Alija ,  Frank Wunder ,  Dieter Lang ,  Klaus Dembowsky ,  Alexander Straub ,  Elisabeth Perzborn

Inventor： Johannes-Peter Stasch ,  Achim Feurer ,  Stefan Weigand ,  Elke Stahl ,  Dietmar Flubacher ,  Cristina Alonso-Alija ,  Frank Wunder ,  Dieter Lang ,  Klaus Dembowsky ,  Alexander Straub ,  Elisabeth Perzborn

IPC: C07D47104

CPC classification number: C07D471/04 ,  A61K31/505 ,  A61K45/06 ,  A61K2300/00

Abstract: The present invention relates to new pyrazolopyridine derivatives of the formula (I) in which R1 represents 4-pyridinyl or 3-pyridinyl; R2 represents H, NH2 or halogen; and salts, isomers and hydrates thereof as stimulators of soluble guanylate cyclase and for use as agents for the treatment of cardiovascular disorders, hypertension, of thromboembolic disorders and ischaemia, sexual dysfunction or inflammation, and for the treatment of disorders of the central nervous system.

Abstract translation: 本发明涉及式（I）的新的吡唑并吡啶衍生物，其中R 1表示4-吡啶基或3-吡啶基; R 2表示H，NH 2或卤素; 其盐，异构体和水合物作为可溶性鸟苷酸环化酶的刺激剂，并用作治疗心血管疾病，高血压，血栓栓塞障碍和局部缺血，性功能障碍或炎症以及用于治疗中枢神经系统疾病的药剂。

公开(公告)号：US06414009B1

公开(公告)日：2002-07-02

申请号：US09648082

申请日：2000-08-25

Applicant: Alexander Straub ,  Chantal Fürstner ,  Ulrich Niewöhner ,  Thomas Jaetsch ,  Achim Feurer ,  Raimund Kast ,  Johannes-Peter Stasch ,  Elisabeth Perzborn ,  Joachim Hütter ,  Klaus Dembowsky ,  Dieter Arlt

Inventor： Alexander Straub ,  Chantal Fürstner ,  Ulrich Niewöhner ,  Thomas Jaetsch ,  Achim Feurer ,  Raimund Kast ,  Johannes-Peter Stasch ,  Elisabeth Perzborn ,  Joachim Hütter ,  Klaus Dembowsky ,  Dieter Arlt

IPC: A61K31416

CPC classification number: C07D401/04 ,  C07D263/32 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D417/04

Abstract: The present invention relates to new heterocyclylmethyl-substituted pyrazole derivatives, processes for their preparation and their use as medicaments, in particular as medicaments for treatment of cardiovascular diseases.

公开(公告)号：US5629320A

公开(公告)日：1997-05-13

申请号：US448930

申请日：1995-05-25

Applicant: J urgen Stoltefuss ,  Siegfried Goldmann ,  Alexander Straub ,  Martin Bechem ,  Rainer Gross ,  Siegbert Hebisch ,  Joachim H utter ,  Howard-Paul Rounding

Inventor： J urgen Stoltefuss ,  Siegfried Goldmann ,  Alexander Straub ,  Martin Bechem ,  Rainer Gross ,  Siegbert Hebisch ,  Joachim H utter ,  Howard-Paul Rounding

IPC: A61K31/47 ,  C07C47/06 ,  C07D215/20 ,  C07D215/36 ,  C07D215/48 ,  C07D401/04 ,  C07D401/14 ,  C07D491/04 ,  C07D491/048 ,  A61K31/395

CPC classification number: C07D401/04 ,  C07D401/14 ,  C07D491/04

Abstract: This invention relates to 3-quinolyl-substituted dihydropyridine derivatives, such as ##STR1## or a pharmaceutically acceptable salt thereof. These compounds are used in treating cardiovascular disease.

Abstract translation: 本发明涉及3-喹啉基取代的二氢吡啶衍生物，例如“IMAGE”或其药学上可接受的盐。 这些化合物用于治疗心血管疾病。

公开(公告)号：US5550245A

公开(公告)日：1996-08-27

申请号：US450461

申请日：1995-05-25

Applicant: J urgen Stoltefuss ,  Siegfried Goldmann ,  Alexander Straub ,  Martin Bechem ,  Rainer Gross ,  Siegbert Hebisch ,  Joachim H utter ,  Howard-Paul Rounding

Inventor： J urgen Stoltefuss ,  Siegfried Goldmann ,  Alexander Straub ,  Martin Bechem ,  Rainer Gross ,  Siegbert Hebisch ,  Joachim H utter ,  Howard-Paul Rounding

IPC: A61K31/47 ,  C07C47/06 ,  C07D215/20 ,  C07D215/36 ,  C07D215/48 ,  C07D401/04 ,  C07D401/14 ,  C07D491/04 ,  C07D491/048 ,  C07D403/92

CPC classification number: C07D401/04 ,  C07D401/14 ,  C07D491/04

Abstract: Intermediate of the formula ##STR1## wherein R.sup.5 represents a cyclic, straight-chain or branched, saturated or unsaturated hydrocarbon radical having up to 12 carbon atoms, which is optionally interrupted up to twice in an identical or different manner by oxygen or sulphur, as intermediates for substituents on novel dihydropyridine cardiovascular compounds.

Abstract translation: 式（XVIII）的中间体，其中R 5表示具有至多12个碳原子的环状，直链或支链，饱和或不饱和的烃基，其任选地以相同或不同的方式被氧或两次中断 硫，作为新型二氢吡啶心血管化合物上取代基的中间体。

公开(公告)号：US5514803A

公开(公告)日：1996-05-07

申请号：US230178

申请日：1994-04-20

Applicant: Jurgen Stoltefuss ,  Siegfried Goldmann ,  Alexander Straub ,  Martin Bechem ,  Rainer Gross ,  Siegbert Hebisch ,  Joachim Hutter ,  Howard-Paul Rounding

Inventor： Jurgen Stoltefuss ,  Siegfried Goldmann ,  Alexander Straub ,  Martin Bechem ,  Rainer Gross ,  Siegbert Hebisch ,  Joachim Hutter ,  Howard-Paul Rounding

IPC: A61K31/47 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D491/04 ,  C07D491/048 ,  C07F9/58 ,  C07D403/02

CPC classification number: C07D401/04 ,  C07D491/04

Abstract: The invention relates to new 2,6-disubstituted 4-quinolyl-dihydropyridines ##STR1## in which R.sub.1 to R.sub.5 have the meaning indicated in the description,processes for their preparation and their use in medicaments, in particular in compositions for the treatment of cardiovascular disorders.

Abstract translation: 本发明涉及新的2,6-二取代的4-喹啉基 - 二氢吡啶（I），其中R1至R5具有说明书中所示的含义，其制备方法及其在药物中的用途，特别是用于 治疗心血管疾病。

公开(公告)号：US5434153A

公开(公告)日：1995-07-18

申请号：US230468

申请日：1994-04-20

Applicant: Alexander Straub ,  Siegfried Goldmann ,  Jurgen Stoltefuss ,  Martin Bechem ,  Rainer Gross ,  Siegbert Hebisch ,  Joachim Hutter ,  Howard-Paul Rounding

Inventor： Alexander Straub ,  Siegfried Goldmann ,  Jurgen Stoltefuss ,  Martin Bechem ,  Rainer Gross ,  Siegbert Hebisch ,  Joachim Hutter ,  Howard-Paul Rounding

IPC: A61K31/455 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/495 ,  A61K31/50 ,  A61K31/502 ,  A61P9/00 ,  A61P9/04 ,  C07D237/28 ,  C07D401/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  C07D519/00 ,  C07F9/59 ,  A61K31/435

CPC classification number: C07D409/04 ,  C07D417/04 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04

Abstract: The present invention relates to new 2-amino-4-hetero-aryl-1,4-dihydropyridines of the general formula (I) ##STR1## in which R.sub.1 to R.sub.4 have the meaning given in the description, processes for their preparation and their use in medicaments, in particular in compositions for the treatment of cardiovascular disorders.

Abstract translation: 本发明涉及通式（I）的新的2-氨基-4-杂芳基-1,4-二氢吡啶，其中R1至R4具有说明书中给出的含义， 制剂及其在药物中的用途，特别是用于治疗心血管疾病的组合物。

公开(公告)号：US5432282A

公开(公告)日：1995-07-11

申请号：US298013

申请日：1994-08-30

Applicant: Jurgen Stoltefuss ,  Siegfried Goldmann ,  Alexander Straub ,  Horst Boshagen ,  Martin Bechem ,  Rainer Gross ,  Siegbert Hebisch ,  Joachim Hutter ,  Howard-Paul Rounding

Inventor： Jurgen Stoltefuss ,  Siegfried Goldmann ,  Alexander Straub ,  Horst Boshagen ,  Martin Bechem ,  Rainer Gross ,  Siegbert Hebisch ,  Joachim Hutter ,  Howard-Paul Rounding

IPC: A61K31/47 ,  A61K31/445 ,  A61K31/4709 ,  A61P9/00 ,  A61P9/04 ,  C07D20060101 ,  C07D211/90 ,  C07D215/12 ,  C07D215/14 ,  C07D215/48 ,  C07D261/06 ,  C07D261/08 ,  C07D401/04 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D211/84

CPC classification number: C07D401/04 ,  C07D215/14

Abstract: The present invention relates to new 2-amino-5-cyano-4-quinoline-1,4-dihydropyridines, processes for their preparation and their use in medicaments, in particular in agents for the treatment of cardiovascular diseases.

Abstract translation: 本发明涉及新的2-氨基-5-氰基-4-喹啉-1,4-二氢吡啶，其制备方法及其在药物中的用途，特别是用于治疗心血管疾病的药剂。

公开(公告)号：US5254692A

公开(公告)日：1993-10-19

申请号：US961289

申请日：1992-10-15

Applicant: Siegfried Goldmann ,  Horst Boshagen ,  Jurgen Stoltefuss ,  Alexander Straub ,  Rainer Gross ,  Joachim Hutter ,  Siegbert Hebisch ,  Martin Bechem

Inventor： Siegfried Goldmann ,  Horst Boshagen ,  Jurgen Stoltefuss ,  Alexander Straub ,  Rainer Gross ,  Joachim Hutter ,  Siegbert Hebisch ,  Martin Bechem

IPC: C07D263/56 ,  C07D263/57 ,  C07D277/66 ,  C07D413/04 ,  C07D417/04 ,  C07D491/04 ,  C07D277/64

CPC classification number: C07D263/57 ,  C07D277/66 ,  C07D413/04 ,  C07D417/04 ,  C07D491/04

Abstract: 2,6-dialkyl-4-(benzothiazol- or benzoxazol-7-yl)-1,4-dihydropyridines which exhibit positive inotropic action with largely neutral vascular behavior, of the formula ##STR1## in which R.sup.1 and R.sup.5 are identical or different and represent straight-chain or branched alkyl having up to 8 carbon atoms,R.sup.2 represents nitro or cyano, orR.sup.1 and R.sup.2 together form a lactone ring of the formula ##STR2## R.sup.3 represents a radical of the formula ##STR3## and R.sup.4 represents hydrogen, orand physiologically acceptable salts thereof.

Abstract translation: 表现出具有大量中性血管行为的正性肌力作用的2,6-二烷基-4-（苯并噻唑基或苯并恶唑-7-基）-1,4-二氢吡啶，其中R1和R5是 相同或不同，代表具有至多8个碳原子的直链或支链烷基，R2代表硝基或氰基，或R1和R2一起形成下式的内酯环R3表示下式的基团： 图像> ，R4代表氢或其生理上可接受的盐。