公开(公告)号：US08278300B2

公开(公告)日：2012-10-02

申请号：US12654787

申请日：2010-01-04

Applicant: Torsten Dunkern ,  Christian Schudt ,  Friedrich Grimminger ,  Hossein Ardeschir Ghofrani ,  Manfred Kaps ,  Bernhard Rosengarten

Inventor： Torsten Dunkern ,  Christian Schudt ,  Friedrich Grimminger ,  Hossein Ardeschir Ghofrani ,  Manfred Kaps ,  Bernhard Rosengarten

IPC: A01N43/58 ,  A01N43/54 ,  A61K31/495 ,  A61K31/535 ,  A61K31/517

CPC classification number: A61K31/53 ,  A61K31/5025 ,  A61K31/519

Abstract: The present invention is concerned with the use of PDE5 inhibitors in medicine.

Abstract translation: 本发明涉及在药物中使用PDE5抑制剂。

公开(公告)号：US09018175B2

公开(公告)日：2015-04-28

申请号：US13515214

申请日：2010-12-15

Applicant: Dieter Flockerzi ,  Thomas Stengel ,  Alexander Mann ,  Harald Ohmer ,  Ulrich Kautz ,  Steffen Weinbrenner ,  Stefan Fischer ,  Christof Zitt ,  Armin Hatzelmann ,  Torsten Dunkern ,  Christian Hesslinger ,  Thomas Maier ,  Hermann Tenor ,  Clemens Braun ,  Raimund Külzer ,  Degenhard Marx

Inventor： Dieter Flockerzi ,  Thomas Stengel ,  Alexander Mann ,  Harald Ohmer ,  Ulrich Kautz ,  Steffen Weinbrenner ,  Stefan Fischer ,  Christof Zitt ,  Armin Hatzelmann ,  Torsten Dunkern ,  Christian Hesslinger ,  Thomas Maier ,  Hermann Tenor ,  Clemens Braun ,  Raimund Külzer ,  Degenhard Marx

IPC: A61K31/56 ,  A61K31/519 ,  A61K31/5585 ,  C07D495/04 ,  C07D519/00

CPC classification number: C07D519/00

Abstract: The compounds of Formula (1), in which A, R1, R2, R3 and R5 have the meanings as given in the description, are novel effective inhibitors of type 4 and 5 phosphodiesterase.

Abstract translation: 其中A，R1，R2，R3和R5具有如说明书中给出的含义的式（1）化合物是4型和5型磷酸二酯酶的新型有效抑制剂。

公开(公告)号：US08816085B2

公开(公告)日：2014-08-26

申请号：US13390942

申请日：2010-08-24

Applicant: Josef Stadlwieser ,  Beate Schmidt ,  Heiko Bernsmann ,  Alexander Sudau ,  Torsten Dunkern ,  Ragna Hussong ,  Ewald Benediktus ,  Andreas Pahl

Inventor： Josef Stadlwieser ,  Beate Schmidt ,  Heiko Bernsmann ,  Alexander Sudau ,  Torsten Dunkern ,  Ragna Hussong ,  Ewald Benediktus ,  Andreas Pahl

IPC: A61K31/437 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: The compounds of Formula (I), wherein R1, R21, R22, R23, R24, Y and R3 have the meanings as given in the description, the salts thereof, the stereoisomers of the compounds and the salts thereof are effective inhibitors of the type 5 phosphodiesterase.

Abstract translation: 式（I）的化合物，其中R 1，R 21，R 22，R 23，R 24，Y和R 3具有在说明书中给出的含义，其盐，化合物及其盐的立体异构体是有效的类型的抑制剂 5磷酸二酯酶。

公开(公告)号：US20140113877A1

公开(公告)日：2014-04-24

申请号：US14124446

申请日：2012-06-12

Applicant: Dieter Flockerzi ,  Alexander Mann ,  Thomas Stengel ,  Harald Ohmer ,  Ulrich Kautz ,  Steffen Weinbrenner ,  Stefan Fischer ,  Hermann Tenor ,  Christof Zitt ,  Armin Hatzelmann ,  Torsten Dunkern ,  Christian Hesslinger ,  Clemens Braun ,  Ewald Benediktus ,  Andreas Pahl ,  Raimund Kuelzer ,  Degenhard Marx

Inventor： Dieter Flockerzi ,  Alexander Mann ,  Thomas Stengel ,  Harald Ohmer ,  Ulrich Kautz ,  Steffen Weinbrenner ,  Stefan Fischer ,  Hermann Tenor ,  Christof Zitt ,  Armin Hatzelmann ,  Torsten Dunkern ,  Christian Hesslinger ,  Clemens Braun ,  Ewald Benediktus ,  Andreas Pahl ,  Raimund Kuelzer ,  Degenhard Marx

IPC: C07D519/00 ,  A61K45/06 ,  A61K31/519

CPC classification number: C07D519/00 ,  A61K31/519 ,  A61K45/06 ,  C07D495/04

Abstract: The compounds of formula (1) in which A, X, R1, R2, R3 and R7 have the meanings as given in the description, are novel effective inhibitors of type 4 and type 5 phosphodiesterase.

Abstract translation: 其中A，X，R1，R2，R3和R7具有说明书中给出的含义的式（1）化合物是4型和5型磷酸二酯酶的新型有效抑制剂。

公开(公告)号：US20120149721A1

公开(公告)日：2012-06-14

申请号：US13390940

申请日：2010-08-24

Applicant: Josef Stadlwieser ,  Beate Schmidt ,  Heiko Bernsmann ,  Torsten Dunkern ,  Ewald Benediktus ,  Andreas Pahl ,  Ragna Hussong ,  Olaf Nimz ,  Matthias Mueller ,  Martin Viertelhaus

Inventor： Josef Stadlwieser ,  Beate Schmidt ,  Heiko Bernsmann ,  Torsten Dunkern ,  Ewald Benediktus ,  Andreas Pahl ,  Ragna Hussong ,  Olaf Nimz ,  Matthias Mueller ,  Martin Viertelhaus

IPC: A61K31/519 ,  A61P11/00 ,  A61P1/16 ,  A61P11/08 ,  A61P9/12 ,  C07D487/04 ,  A61P11/06

CPC classification number: C07D487/04 ,  A61K2300/00

Abstract: The compounds of Formula (I), wherein R1, R2, R21, R22, R23, R24, Y and R3 have the meanings as given in the description, the salts thereof, the stereoisomers of the compounds and the salts thereof are effective inhibitors of the type 5 phosphodiesterase.

Abstract translation: 式（I）化合物，其中R 1，R 2，R 21，R 22，R 23，R 24，Y和R 3具有本说明书中给出的含义，其盐，化合物及其盐的立体异构体是有效的抑制剂 5型磷酸二酯酶。

公开(公告)号：US08445501B2

公开(公告)日：2013-05-21

申请号：US12918740

申请日：2009-02-25

Applicant: Josef Stadlwieser ,  Beate Schmidt ,  Heiko Bernsmann ,  Alexander Sudau ,  Torsten Dunkern ,  Degenhard Marx ,  Jörg Diefenbach

Inventor： Josef Stadlwieser ,  Beate Schmidt ,  Heiko Bernsmann ,  Alexander Sudau ,  Torsten Dunkern ,  Degenhard Marx ,  Jörg Diefenbach

IPC: C07D487/04 ,  A61K31/519 ,  A61P9/08 ,  A61P11/06

CPC classification number: C07D487/04

Abstract: The compounds of Formula (I), in which R1, R21, R22, R23, R24, Y and R3 have the meanings as given in the description, the salts thereof, the N-oxides of the compounds and the salts thereof and the stereoisomers of the compounds, the salts, the N-oxides of the compounds and the N-oxides of the salts thereof are effective inhibitors of the type 5 phosphodiesterase.

Abstract translation: 式（I）的化合物，其中R 1，R 21，R 22，R 23，R 24，Y和R 3具有本说明书中给出的含义，其盐，化合物的N-氧化物及其盐和立体异构体 的化合物，盐，化合物的N-氧化物及其盐的N-氧化物是5型磷酸二酯酶的有效抑制剂。

公开(公告)号：US20120196867A1

公开(公告)日：2012-08-02

申请号：US13445675

申请日：2012-04-12

Applicant: Torsten DUNKERN ,  Armin HATZELMANN ,  Christian SCHUDT ,  Friedrich GRIMMINGER ,  Hossein Ardeschir GHOFRANI

Inventor： Torsten DUNKERN ,  Armin HATZELMANN ,  Christian SCHUDT ,  Friedrich GRIMMINGER ,  Hossein Ardeschir GHOFRANI

IPC: A61K31/53 ,  A61K31/497 ,  A61P11/00 ,  A61K31/4985

CPC classification number: A61K45/06 ,  A61K31/205 ,  A61K31/44 ,  A61K31/505 ,  A61K31/522 ,  A61K31/53 ,  A61K2300/00

Abstract: The claimed subject matter relates to pharmaceutical compositions comprising a PDE4 inhibitor and a PDE5 inhibitor and the treatment of a disease in which phosphodiesterase 4 (PDE4) and/or phosphodiesterase 5 (PDE5) is detrimental.

Abstract translation: 所要求保护的主题涉及包含PDE4抑制剂和PDE5抑制剂的药物组合物和其中磷酸二酯酶4（PDE4）和/或磷酸二酯酶5（PDE5）是有害的疾病的治疗。

公开(公告)号：US20110021479A1

公开(公告)日：2011-01-27

申请号：US12918740

申请日：2009-02-25

Applicant: Josef Stadlwieser ,  Beate Schmidt ,  Heiko Bernsmann ,  Alexander Sudau ,  Torsten Dunkern ,  Degenhard Marx ,  Jörg Diefenbach

Inventor： Josef Stadlwieser ,  Beate Schmidt ,  Heiko Bernsmann ,  Alexander Sudau ,  Torsten Dunkern ,  Degenhard Marx ,  Jörg Diefenbach

IPC: A61K31/573 ,  C07D487/04 ,  A61K31/519 ,  C07D413/14 ,  A61K31/5377 ,  A61K31/397 ,  A61P11/00 ,  A61P1/16

CPC classification number: C07D487/04

Abstract: The compounds of Formula (I), in which R1, R21, R22, R23, R24, Y and R3 have the meanings as given in the description, the salts thereof, the N-oxides of the compounds and the salts thereof and the stereoisomers of the compounds, the salts, the N-oxides of the compounds and the N-oxides of the salts thereof are effective inhibitors of the type 5 phosphodiesterase.

Abstract translation: 式（I）的化合物，其中R 1，R 21，R 22，R 23，R 24，Y和R 3具有本说明书中给出的含义，其盐，化合物的N-氧化物及其盐和立体异构体 的化合物，盐，化合物的N-氧化物及其盐的N-氧化物是5型磷酸二酯酶的有效抑制剂。

公开(公告)号：US20100120730A1

公开(公告)日：2010-05-13

申请号：US12449173

申请日：2008-01-30

Applicant: Steffen Weinbrenner ,  Torsten Dunkern ,  Degenhard Marx ,  Beate Schmidt ,  Thomas Stengel ,  Dieter Flockerzi ,  Ulrich Kautz ,  Daniela Hauser ,  Jörg Diefenbach ,  Johannes A.M. Christiaans ,  Wiro M.P.B. Menge

Inventor： Steffen Weinbrenner ,  Torsten Dunkern ,  Degenhard Marx ,  Beate Schmidt ,  Thomas Stengel ,  Dieter Flockerzi ,  Ulrich Kautz ,  Daniela Hauser ,  Jörg Diefenbach ,  Johannes A.M. Christiaans ,  Wiro M.P.B. Menge

IPC: A61K31/475 ,  C07D471/04 ,  A61K31/56 ,  A61P11/00 ,  A61P1/16 ,  A61P9/12

CPC classification number: C07D471/04

Abstract: The compounds of formula (I) wherein R1 to R8 and R11 have the meanings as given in the description, the salts thereof, the N-oxides of the compounds and the salts thereof, and the stereoisomers of the compounds, the salts, the N-oxides of the compounds and the N-oxides of the salts thereof are effective inhibitors of the type 5 phosphodiesterase.

Abstract translation: 其中R1至R8和R11具有如本说明书中给出的含义的式（I）化合物，其盐，化合物的N-氧化物及其盐，以及化合物，盐，N的立体异构体 化合物的氧化物及其盐的N-氧化物是5型磷酸二酯酶的有效抑制剂。

公开(公告)号：US20120142633A1

公开(公告)日：2012-06-07

申请号：US13390942

申请日：2010-08-24

Applicant: Josef Stadlwieser ,  Beate Schmidt ,  Heiko Bernsmann ,  Alexander Sudau ,  Torsten Dunkern ,  Ragna Hussong ,  Ewald Benediktus ,  Andreas Pahl

Inventor： Josef Stadlwieser ,  Beate Schmidt ,  Heiko Bernsmann ,  Alexander Sudau ,  Torsten Dunkern ,  Ragna Hussong ,  Ewald Benediktus ,  Andreas Pahl

IPC: A61K31/437 ,  C07F7/02 ,  A61K31/695 ,  A61P1/16 ,  A61P11/06 ,  A61P11/08 ,  A61P9/12 ,  C07D471/04 ,  A61P11/00

CPC classification number: C07D471/04

Abstract: The compounds of Formula (I), wherein R1, R21, R22, R23, R24, Y and R3 have the meanings as given in the description, the salts thereof, the stereoisomers of the compounds and the salts thereof are effective inhibitors of the type 5 phosphodiesterase.

Abstract translation: 式（I）的化合物，其中R 1，R 21，R 22，R 23，R 24，Y和R 3具有在说明书中给出的含义，其盐，化合物及其盐的立体异构体是有效的类型的抑制剂 5磷酸二酯酶。