公开(公告)号：US07189738B2

公开(公告)日：2007-03-13

申请号：US10485412

申请日：2002-07-17

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

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

IPC: A61K31/454 ,  A61K31/4545 ,  C07D211/22 ,  C07D401/14

CPC classification number: C07D209/48 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D403/12 ,  C07D409/12 ,  C07D409/14 ,  C07D495/04

Abstract: The invention relates to coagulation of the blood. Disclosed are novel compounds of formula (I), a method for the production of these compounds, pharmaceutical compositions containing them, and methods of using them for the prevention and/or treatment of various diseases.

Abstract translation: 本发明涉及血液凝固。 公开了式（I）的新型化合物，这些化合物的制备方法，含有它们的药物组合物及其用于预防和/或治疗各种疾病的方法。

公开(公告)号：US20060183915A1

公开(公告)日：2006-08-17

申请号：US11403743

申请日：2006-04-13

Applicant: Alexander Straub

Inventor： Alexander Straub

IPC: C07D277/36

CPC classification number: A01N43/78 ,  C07C331/04 ,  C07C333/20 ,  C07D277/36

Abstract: The present invention relates to a process for preparing a compound of formula (V) where R is H or F, by reacting a compound of formula (IV) where R is H or F, with hydrogen sulphide or salts thereof, optionally in the presence of a reaction auxiliary and optionally in the presence of a diluent.

Abstract translation: 本发明涉及制备其中R为H或F的式（Ⅴ）化合物的方法，其中R为H或F的式（Ⅳ）化合物与其硫化氢或其盐， 的反应助剂，任选地在稀释剂的存在下。

公开(公告)号：US20060173047A1

公开(公告)日：2006-08-03

申请号：US11394543

申请日：2006-03-31

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

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

IPC: A61K31/4439 ,  A61K31/427 ,  A61K31/422 ,  A61K31/421 ,  C07D417/02 ,  C07D413/02

CPC classification number: C07D413/10 ,  C07D413/14

Abstract: The invention relates to the field of blood coagulation, more particularly, to novel compounds of general formula (I), to a method for producing said compounds and to their use as active ingredients in medicaments for the prevention and/or the treatment of diseases.

Abstract translation: 本发明涉及血液凝固领域，更具体地说，涉及通式（I）的新型化合物，涉及用于制备所述化合物的方法及其作为用于预防和/或治疗疾病的药物中的活性成分的用途。

公开(公告)号：US07078527B2

公开(公告)日：2006-07-18

申请号：US10501115

申请日：2003-01-03

Applicant: Alexander Straub

Inventor： Alexander Straub

IPC: C07D277/12

CPC classification number: A01N43/78 ,  C07C331/04 ,  C07C333/20 ,  C07D277/36

Abstract: The present invention relates to a process for preparing compounds of the formula (I) where R is H or F, by (a) reacting a compound of the formula (II) where X is halogen, mesylate or tosylate with a thiocyanate, (b) reacting the resultant product with H2S or one of its salts to give a dithiocarbamate, and (c) reacting the dithiocarbamate with acetaldehyde, chloroacetaldehyde or an acetal thereof, and further relates to intermediates used in this process.

Abstract translation: 本发明涉及制备其中R为H或F的式（I）化合物的方法，通过以下步骤：使式（II）化合物（其中X为卤素，甲磺酸酯基或甲苯磺酸酯）与硫氰酸酯反应，（b） ）使所得产物与H 2 S或其盐之一反应，得到二硫代氨基甲酸酯，和（c）使二硫代氨基甲酸酯与乙醛，氯乙醛或其缩醛反应，并且还涉及此中使用的中间体 处理。

公开(公告)号：US07034017B2

公开(公告)日：2006-04-25

申请号：US10470861

申请日：2002-01-28

Applicant: Alexander Straub ,  Thomas Lampe ,  Josef Pernerstorfer ,  Elisabeth Perzborn ,  Jens Pohlmann ,  Susanne Röhrig ,  Karl-Heinz Schlemmer

Inventor： Alexander Straub ,  Thomas Lampe ,  Josef Pernerstorfer ,  Elisabeth Perzborn ,  Jens Pohlmann ,  Susanne Röhrig ,  Karl-Heinz Schlemmer

IPC: A61K31/5377 ,  C07D413/10

CPC classification number: C07D413/10 ,  C07D413/14

Abstract: This invention relates to compounds of formula (I) wherein R1 represents optionally substituted phenyl, R2 represents optionally substituted and the remaining “R” groups are as defined in the specification and claims, as well as a method for making such materials, pharmaceutical compositions containing such materials, and methods of using such materials in medical treatment.

Abstract translation: 本发明涉及式（I）化合物，其中R 1表示任选取代的苯基，R 2表示任选取代的，其余的“R”基团如本说明书中所定义 权利要求书，以及制造这种材料的方法，含有这些材料的药物组合物，以及在医疗中使用这些材料的方法。

公开(公告)号：US20050261323A1

公开(公告)日：2005-11-24

申请号：US11192961

申请日：2005-07-29

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: A61K31/506 ,  A61K31/5377 ,  A61K45/00 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P15/00 ,  A61P25/00 ,  A61P29/00 ,  C07B61/00 ,  C07D471/04 ,  A61K31/513 ,  C07D471/02

CPC classification number: C07D471/04

Abstract: This invention relates to methods for treating thromboembolic disorders and ischemias, sexual dysfunction, inflammation, disorders of the central nervous system, and cardiovascular disorders other than hypertension by administering a compound of the formula wherein R1 is H or a di-C1-6-alkylaminocarbonyl radical, and R2 is a radical of the formula —O—C(X)—NR3R4 wherein X is O or S. The compound may also be administered in combination with at least one organic nitrate or NO donor, or in combination with at least one compound which inhibits the breakdown of cyclic guanosine monophosphate (cGMP).

Abstract translation: 本发明涉及治疗血栓栓塞障碍和缺血性疾病，性功能障碍，炎症，中枢神经系统紊乱以及高血压以外的心血管疾病的方法，其通过给予下式化合物其中R 1是H或 二-C 1-6烷基氨基羰基，R 2是式-OC（X）-NR 3 R 3的基团， 其中X为O或S.化合物还可与至少一种有机硝酸盐或NO供体组合施用，或与至少一种抑制环鸟苷酸单磷酸化合物的化合物组合施用 cGMP）。

公开(公告)号：US20050124816A1

公开(公告)日：2005-06-09

申请号：US10501115

申请日：2003-01-03

Applicant: Alexander Straub

Inventor： Alexander Straub

IPC: C07D277/20 ,  A01N43/78 ,  C07C331/04 ,  C07C333/00 ,  C07C333/20 ,  C07D277/36 ,  C07D277/16

CPC classification number: A01N43/78 ,  C07C331/04 ,  C07C333/20 ,  C07D277/36

Abstract: The present invention relates to a process for preparing compounds of the formula (I) where R is H or F, by (a) reacting a compound of the formula (II) where X is halogen, mesylate or tosylate with a thiocyanate, (b) reacting the resultant product with H2S or one of its salts to give a dithiocarbamate, and (c) reacting the dithiocarbamate with acetaldehyde, chloroacetaldehyde or an acetal thereof, and further relates to intermediates used in this process.

Abstract translation: 本发明涉及制备其中R为H或F的式（I）化合物的方法，通过以下步骤：使式（II）化合物（其中X为卤素，甲磺酸酯基或甲苯磺酸酯）与硫氰酸酯反应，（b） ）使所得产物与H 2 S或其盐之一反应，得到二硫代氨基甲酸酯，和（c）使二硫代氨基甲酸酯与乙醛，氯乙醛或其缩醛反应，并且还涉及此中使用的中间体 处理。

公开(公告)号：US20050080081A1

公开(公告)日：2005-04-14

申请号：US10470861

申请日：2002-01-28

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

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

IPC: A61K31/422 ,  A61K31/5377 ,  A61P7/02 ,  A61P9/10 ,  A61P19/02 ,  A61P25/28 ,  A61P35/00 ,  C07D413/10 ,  C07D413/14 ,  C07D413/02 ,  A61K31/421 ,  A61K31/454 ,  A61K31/496

CPC classification number: C07D413/10 ,  C07D413/14

Abstract: The invention relates to the field of blood coagulation, more particularly, to novel compounds of general formula (I), to a method for producing said compounds and to their use as active ingredients in medicaments for the prevention and/or the treatment of diseases.

Abstract translation: 本发明涉及血液凝固领域，更具体地说，涉及通式（I）的新型化合物，涉及用于制备所述化合物的方法及其作为用于预防和/或治疗疾病的药物中的活性成分的用途。

公开(公告)号：US5708177A

公开(公告)日：1998-01-13

申请号：US697467

申请日：1996-08-26

Applicant: Alexander Straub

Inventor： Alexander Straub

IPC: A61K31/435 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  C07D211/90 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D491/04 ,  C07D491/048 ,  C07D211/82 ,  C07D211/84

CPC classification number: C07D491/04 ,  C07D211/90

Abstract: The invention relates to a process for the preparation of optically active ortho-substituted 4-aryl- or heteroaryl-1,4-dihydropyridines by oxidation and subsequent reduction from their opposite enantiomers.

Abstract translation: 本发明涉及通过氧化并随后从其相反对映异构体还原制备光学活性的邻位取代的4-芳基 - 或杂芳基-1,4-二氢吡啶的方法。

公开(公告)号：US5436342A

公开(公告)日：1995-07-25

申请号：US231010

申请日：1994-04-20

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

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

IPC: A61K31/47 ,  A61K31/435 ,  A61P9/00 ,  A61P9/04 ,  C07D401/04 ,  C07D401/14 ,  C07D409/14 ,  C07D495/04 ,  A61K31/495 ,  C07D403/12

CPC classification number: C07D401/04 ,  C07D495/04

Abstract: The invention relates to novel, condensed 4-quinolyl-dhydropyridines of the general formula (I) ##STR1## in which A, R.sub.1, R.sub.2 and R.sub.3 have the meaning given in the description, to processes for their preparation and to their use in medicaments, in particular in agents for treating angiocardiopathies.

Abstract translation: 本发明涉及通式（I）的化合物，其中A，R 1，R 2和R 3具有本说明书给出的含义，其制备方法及其制备方法 用于药物，特别是用于治疗血管性心脏病的药剂中。