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1. 发明授权

US07022709B2 Selective PDE 2 inhibitors as pharmaceuticals for improving perception 失效
公开(公告)号：US07022709B2
公开(公告)日：2006-04-04
申请号：US09911277
申请日：2001-07-23
申请人： Frank-Gerhard Böss , Martin Hendrix , Gerhard König , Ulrich Niewöhner , Karl-Heinz Schlemmer , Rudy Schreiber , Franz-Josef Van Der Staay , Dagmar Schauss
发明人： Frank-Gerhard Böss , Martin Hendrix , Gerhard König , Ulrich Niewöhner , Karl-Heinz Schlemmer , Rudy Schreiber , Franz-Josef Van Der Staay , Dagmar Schauss
IPC分类号： A61K31/519
CPC分类号： A61K31/505
摘要： The invention relates to the use of selective phosphodiesterase 2 (PDE 2) inhibitors for producing pharmaceuticals for improving perception, concentration, learning and/or memory.

2. 发明授权

US06573263B2 Substituted imidazotriazinones 失效
公开(公告)号：US06573263B2
公开(公告)日：2003-06-03
申请号：US10026310
申请日：2001-12-21
申请人： Ulrich Niewöhner , Dagmar Schauss , Martin Hendrix , Gerhard König , Frank-Gerhard Böss , Franz-Josef Van Der Staay , Rudy Schreiber , Karl-Heinz Schlemmer , Rolf Grosser
发明人： Ulrich Niewöhner , Dagmar Schauss , Martin Hendrix , Gerhard König , Frank-Gerhard Böss , Franz-Josef Van Der Staay , Rudy Schreiber , Karl-Heinz Schlemmer , Rolf Grosser
IPC分类号： C07D45704
CPC分类号： C07D487/04 , A61K31/53
摘要： The present invention relates to new substituted imidazotriazinones, processes for their preparation, and their use for the production of medicaments, in particular for improving perception, concentration power, learning power and/or memory power.

3. 发明申请

US20050009822A1 Novel substituted imidazotriazinones 失效
标题翻译：新型取代咪唑并三嗪酮
公开(公告)号：US20050009822A1
公开(公告)日：2005-01-13
申请号：US10468511
申请日：2002-02-11
申请人： Ulrich Niewohner , Maria Niewohner , Dagmar Schauss , Gerhard Konig , Martin Hendrix , Frank-Gerhard Boss , Franz-Josef Staay , Rudy Schreiber , Karl-Heinz Schlemmer , Toshiya Moriwaki
发明人： Ulrich Niewohner , Maria Niewohner , Dagmar Schauss , Gerhard Konig , Martin Hendrix , Frank-Gerhard Boss , Franz-Josef Staay , Rudy Schreiber , Karl-Heinz Schlemmer , Toshiya Moriwaki
IPC分类号： A61K31/53 , A61P25/00 , A61P25/28 , A61P43/00 , C07D253/07 , C07D487/04
CPC分类号： C07D253/07 , C07D487/04
摘要： The invention relates to novel substituted imidazotriazinones, to a method for their production and to the use thereof for producing medicaments, in particular to improve perception, powers of concentration, learning capacity and/or memory retentiveness.
摘要翻译：本发明涉及新的取代的咪唑并三嗪酮，其制备方法及其用于生产药物的方法，特别是改善感知力，浓度，学习能力和/或记忆保持性。

4. 发明授权

US06589949B1 3-oxo-2,1-benzisoxazol-1(3H)-carboxamides for treatment of CNS diseases 失效
标题翻译： 3-氧代-2,1-苯并异恶唑-1（3H） - 甲酰胺，用于治疗CNS疾病
公开(公告)号：US06589949B1
公开(公告)日：2003-07-08
申请号：US10149658
申请日：2002-10-22
申请人： Toshiya Moriwaki , Chantal Fürstner , Bernd Riedl , Jens-Kerim Ergüden , Frank Böss , Bernard Schmidt , Franz-Josef van der Staay , Werner Schröder , Karl-Heinz Schlemmer , Nagahiro Yoshida
发明人： Toshiya Moriwaki , Chantal Fürstner , Bernd Riedl , Jens-Kerim Ergüden , Frank Böss , Bernard Schmidt , Franz-Josef van der Staay , Werner Schröder , Karl-Heinz Schlemmer , Nagahiro Yoshida
IPC分类号： A61K315377
CPC分类号： C07D261/20
摘要： The invention relates to novel 3-oxo-2,1-benzisomazol-1(3H)-carboxamides (I), where R1, R2 are the same or different and independently=H, halogen, C1 C6 alkyl C1 C6 alkoxy, C1 C3 perfluoroalkyl, or a group NR5R6; R3, R4 are the same or different and independently=C1 C8 alkyl, whose carbon chain is optionally interrupted by an O, S or NR7 and is optionally singly or severally substituted by C3 C6 cycloalkyl, C1 C4 alkoxy, OH, halogen or NR8R9; C3 C8 cycloalkyl whose carbon chain is optionally interrupted by an O, S or NR10 and is optionally singly or severally substituted by C1 C4 alkoxy, OH, halogen or NR11R12, or R3 and R4 together with a nitrogen atom form a saturated or partially unsaturated 3- to 10-membered mono- or bi-cyclic heteocycle, which, optionally, contains up to two further heteroatoms, from N, O or S and is, optionally, substituted by C1 C4 alkyl, C1 C4 alkoxy, OH, halogen, COOR13 or NR14R15 and X=O or S. The invention further relates to methods for production thereof and use thereof in the production of medicaments for the prophylaxis and/or treatment of diseases of the central nervous system, in particular, cognitive disorders, such as Alzheimer's disease and other forms of dementia, cerebral infarct, skull and brain trauma and pain.
摘要翻译：本发明涉及新的3-氧代-2,1-苯并异恶唑-1（3H） - 甲酰胺（I），其中R 1，R 2相同或不同且独立地为H，卤素，C 1 -C 6烷基C 1 -C 6烷氧基，C 1 C 3 全氟烷基或NR5R6基团; R 3，R 4相同或不同且独立地为C 1 -C 8烷基，其碳链任选地被O，S或NR 7中断，并且任选地被C 3 -C 6环烷基，C 1 -C 4烷氧基，OH，卤素或NR 8 R 9单独或多个取代; C 8 -C 8环烷基，其碳链任选地被O，S或NR 10中断，并且任选地被C 1 -C 4烷氧基，OH，卤素或NR 11 R 12单独或多个取代，或者R 3和R 4与氮原子一起形成饱和或部分不饱和的3 至10元单环或双环杂环，其任选地含有至多两个另外的N，O或S的杂原子，并且任选地被C 1 -C 4烷基，C 1 -C 4烷氧基，OH，卤素，COOR 13 或NR14R15和X = O或S.本发明还涉及其生产方法及其在生产用于预防和/或治疗中枢神经系统疾病的药物中的用途，特别是认知障碍，例如阿尔茨海默病疾病和其他形式的痴呆，脑梗塞，头骨和脑外伤和疼痛。

5. 发明申请

US20060293326A1 2-Heteroaryl-imidazotriazinones and their use in the treatment of inflammatory or immune diseases 审中-公开
标题翻译： 2-杂芳基 - 咪唑并三嗪酮及其在治疗炎症或免疫疾病中的应用
公开(公告)号：US20060293326A1
公开(公告)日：2006-12-28
申请号：US10480949
申请日：2002-05-21
申请人： Cristina Alonso-Alija , Heike Gielen , Martin Hendrix , Ulrich Niewohner , Maria Niewohner , Dagmar Schauss , Hilmar Bischoff , Nils Burkhardt , Volker Geiss , Karl-Heinz Schlemmer , Nigel Cuthbert , Mary Fitzgerald , Graham Sturton
发明人： Cristina Alonso-Alija , Heike Gielen , Martin Hendrix , Ulrich Niewohner , Maria Niewohner , Dagmar Schauss , Hilmar Bischoff , Nils Burkhardt , Volker Geiss , Karl-Heinz Schlemmer , Nigel Cuthbert , Mary Fitzgerald , Graham Sturton
IPC分类号： A61K31/53 , C07D487/04
CPC分类号： C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D417/04 , C07D487/04
摘要： The invention relates to 2-Heteroaryl-imidazotriazinones, processes for their preparation and their use in medicaments, esp. for the treatment and/or prophylaxis of inflammatory processes and/or immune diseases. The present invention relates to compounds of the general formula (I) in which R1 denotes 5- to 10-membered heteroaryl, which is optionally substituted by identical or different residues selected from the group consisting of halogen, (C1-C4)-alkyl, trifluoromthyl, cyano, nitro und trifluoromethoxy, denotes 3- to 10-membered carbocyclyl or carbon-bonded, 4- to 10-membered heterocyclyl, whereby carbocyclyl and heterocyclyl are optionally substituted by identical or different residues selected from the group consisting of (C1-C6)-aldyl, (C1-C6)-aldoxy, hydroxy, halogen, trifluoromethyl and oxo, or denotes (C2-C10)-alkyl, which is optionally substituted by identical or different residues selected from the group the group consisting of (C1-C6)-alkoxy, hydroxy, halogen, 3- to 10-membered carbocyclyl and oxo.
摘要翻译：本发明涉及2-杂芳基 - 咪唑并三嗪酮，其制备方法及其在药物中的应用，用于治疗和/或预防炎症过程和/或免疫疾病。本发明涉及通式（I）的化合物，其中R 1表示5至10元杂芳基，其任选被相同或不同的选自以下的残基所取代：卤素，（C 1 -C 4 - ） - 烷基，三氟甲基，氰基，硝基和三氟甲氧基，表示3-至10-元碳环基或碳键合，4-至10- 其中碳环基和杂环基任选被相同或不同的选自（C 1 -C 6 -C 6） - 烷基，（C 1 -C 6）（C 1 -C 6 -C 6） - 羟基，羟基，卤素，三氟甲基和氧代，或表示（C 2 -C 10） - 烷基，其任选被相同或不同的残基选择，所述残基选自（C 1 -C 6 -C 6） - 烷氧基，羟基，卤素，至10元碳环基和氧代。

6. 发明申请

US20050065153A1 Novel heterocycles 3 审中-公开
标题翻译：新的杂环3
公开(公告)号：US20050065153A1
公开(公告)日：2005-03-24
申请号：US10964380
申请日：2004-10-12
申请人： Cristina Alonso-Alija , Heike Gielen , Martin Hendrix , Ulrich Niewohner , Dagmar Schauss , Hilmar Bischoff , Nils Burkhardt , Volker Geiss , Karl-Heinz Schlemmer , Nigel Cuthbert , Mary Fitzgerald , Graham Sturton , Maria Niewohner
发明人： Cristina Alonso-Alija , Heike Gielen , Martin Hendrix , Ulrich Niewohner , Dagmar Schauss , Hilmar Bischoff , Nils Burkhardt , Volker Geiss , Karl-Heinz Schlemmer , Nigel Cuthbert , Mary Fitzgerald , Graham Sturton , Maria Niewohner
IPC分类号： C07D253/06 , A61K31/53 , A61P11/00 , A61P11/06 , A61P29/00 , A61P37/02 , C07D253/07 , C07D487/04
CPC分类号： C07D253/07 , C07D487/04
摘要： The invention relates to 7-(4-tert butyl-cyclohexyl)-imidazotriazinones, processes for their preparation and their use in medicaments, esp. for the treatment and/or prophylaxis of inflammatory processes and/or immune diseases.
摘要翻译：本发明涉及7-（4-叔丁基 - 环己基） - 咪唑并三嗪酮，其制备方法及其在药物中的应用，用于治疗和/或预防炎症过程和/或免疫疾病。

7. 发明授权

US06458796B1 Dihydro-[1,2,3]triazolo-[4,5-d]pyrimidin-7-one 失效
标题翻译：二氢 - [1,2,3]三唑并[4,5-d]嘧啶-7-酮
公开(公告)号：US06458796B1
公开(公告)日：2002-10-01
申请号：US09763808
申请日：2001-02-26
申请人： Helmut Haning , Ulrich Niewöhner , Ulrich Rosentreter , Thomas Schenke , Erwin Bischoff , Karl-Heinz Schlemmer
发明人： Helmut Haning , Ulrich Niewöhner , Ulrich Rosentreter , Thomas Schenke , Erwin Bischoff , Karl-Heinz Schlemmer
IPC分类号： C07D48704
CPC分类号： C07D487/04
摘要： The present invention relates to novel dihydro-[1,2,3]triazolo-[4,5-d]pyrimidin-7-one, to processes for their preparation and to their use as medicaments, in particular as inhibitors of cGMP-metabolizing phosphodiesterases.
摘要翻译：本发明涉及新的二氢 - [1,2,3]三唑并[4,5-d]嘧啶-7-酮，其制备方法及其作为药物的用途，特别是作为cGMP代谢抑制剂磷酸二酯酶。

8. 发明授权

US06362178B1 2-phenyl substituted imidazotriazinones as phosphodiesterase inhibitors 有权
标题翻译： 2-苯基取代的咪唑并三嗪酮作为磷酸二酯酶抑制剂
公开(公告)号：US06362178B1
公开(公告)日：2002-03-26
申请号：US09554162
申请日：2000-07-21
申请人： Ulrich Niewöhner , Mazen Es-Sayed , Helmut Haning , Thomas Schenke , Karl-Heinz Schlemmer , Jörg Keldenich , Erwin Bischoff , Elisabeth Perzborn , Klaus Dembowsky , Peter Serno , Marc Nowakowski
发明人： Ulrich Niewöhner , Mazen Es-Sayed , Helmut Haning , Thomas Schenke , Karl-Heinz Schlemmer , Jörg Keldenich , Erwin Bischoff , Elisabeth Perzborn , Klaus Dembowsky , Peter Serno , Marc Nowakowski
IPC分类号： A01N4362
CPC分类号： C07D487/04 , C07F9/6561
摘要： The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of cardiovascular and cerebrovascular disorders and/or disorders of the urogenital system, in particular for the treatment of erectile dysfunction.
摘要翻译：通过氯磺化和随后与胺的反应，由相应的2-苯基 - 咪唑并三嗪酮制备在9-位上具有短的非支链烷基的2-苯基取代的咪唑并三嗪酮。所述化合物抑制cGMP代谢磷酸二酯酶，并且适合用作药物中的活性化合物，用于治疗心血管和脑血管障碍和/或泌尿生殖系统疾病，特别是用于治疗勃起功能障碍。

9. 发明申请

US20110009367A1 2-PHENYL SUBSTITUTED IMIDAZOTRIAZINONES AS PHOSPHODIESTERASE INHIBITORS 审中-公开
标题翻译：作为磷酸二酯酶抑制剂的2-苯基取代的咪达唑仑
公开(公告)号：US20110009367A1
公开(公告)日：2011-01-13
申请号：US12717443
申请日：2010-03-04
申请人： Ulrich Niewöhner , Maria Niewöhner , Mazen Es-Sayed , Helmut Haning , Thomas Schenke , Karl-Heinz Schlemmer , Jörg Keldenich , Erwin Bischoff , Elisabeth Perzborn , Klaus Dembowsky , Peter Serno , Marc Nowakowski
发明人： Ulrich Niewöhner , Maria Niewöhner , Mazen Es-Sayed , Helmut Haning , Thomas Schenke , Karl-Heinz Schlemmer , Jörg Keldenich , Erwin Bischoff , Elisabeth Perzborn , Klaus Dembowsky , Peter Serno , Marc Nowakowski
IPC分类号： A61K31/53 , C07D487/04 , A61K31/5377 , C07D491/113 , A61K31/683 , A61K31/551 , A61P9/00 , A61P13/00
CPC分类号： C07D487/04 , C07F9/6561
摘要： The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of cardiovascular and cerebrovascular disorders and/or disorders of the urogenital system, in particular for the treatment of erectile dysfunction.
摘要翻译：通过氯磺化和随后与胺的反应，由相应的2-苯基 - 咪唑并三嗪酮制备在9-位上具有短的非支链烷基的2-苯基取代的咪唑并三嗪酮。所述化合物抑制cGMP代谢磷酸二酯酶，并且适合用作药物中的活性化合物，用于治疗心血管和脑血管障碍和/或泌尿生殖系统疾病，特别是用于治疗勃起功能障碍。

10. 发明授权

US07514565B2 3,5-Difluoropyridines 有权
标题翻译： 3,5-二氟吡啶
公开(公告)号：US07514565B2
公开(公告)日：2009-04-07
申请号：US11639955
申请日：2006-12-15
申请人： Jürgen Stoltefuβ , Siegfried Goldmann , Thomas Krämer , Karl-Heinz Schlemmer , Ulrich Niewöhner , Maria Niewöhner , Arnold Paeβens , Erwin Graef , Stefan Lottmann , Karl Deres , Olaf Weber , Jörn Stölting
发明人： Jürgen Stoltefuβ , Siegfried Goldmann , Thomas Krämer , Karl-Heinz Schlemmer , Ulrich Niewöhner , Maria Niewöhner , Arnold Paeβens , Erwin Graef , Stefan Lottmann , Karl Deres , Olaf Weber , Jörn Stölting
IPC分类号： C07D213/58
CPC分类号： C07D239/22 , C07D213/78 , C07D213/84 , C07D401/04 , C07D401/14
摘要： The invention relates to compounds of the formule
摘要翻译：本发明涉及形式的化合物

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