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81.发明申请Methods For The Prophylaxis And/or Treatment Of Thromboembolic Disorders By Combination Therapy With Substituted Oxazolidinones 审中-公开通过与取代的恶唑烷酮组合治疗预防和/或治疗血栓栓塞障碍的方法公开(公告)号：US20100267685A1
公开(公告)日：2010-10-21
申请号：US12766365
申请日：2010-04-23
申请人： Alexander Straub , Thomas Lampe , Josef Pernerstorfer , Elisabeth Perzborn , Jens Pohlmann , Susanne Röhrig , Karl-Heinz Schlemmer
发明人： Alexander Straub , Thomas Lampe , Josef Pernerstorfer , Elisabeth Perzborn , Jens Pohlmann , Susanne Röhrig , Karl-Heinz Schlemmer
IPC分类号： A61K31/397 , A61K31/5377 , A61K31/541 , A61K31/4365 , A61K31/428 , A61K31/496 , A61K31/444 , A61K31/454 , A61K31/422 , A61K31/423 , A61K31/538 , A61K31/4439 , A61K31/5355 , A61K31/427 , A61P9/08 , A61P7/02 , A61P9/10 , A61P3/06 , A61P9/00 , A61P9/04 , A61K31/5365
CPC分类号： A61K31/422 , A61K31/421 , A61K31/5377 , A61K45/06 , A61K2300/00
摘要： The invention relates to combinations of A) oxazolidinones of formula (I) and B) other active ingredients, to a method for producing said combinations and to the use thereof as medicaments, in particular for the treatment and/or prophylaxis of thrombo-embolic diseases.
摘要翻译： 本发明涉及式（I）的A）恶唑烷酮和B）其它活性成分的组合，用于制备所述组合的方法及其作为药物的用途，特别是用于治疗和/或预防血栓栓塞性疾病 。
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82.发明申请公开(公告)号：US20100137274A1
公开(公告)日：2010-06-03
申请号：US12494879
申请日：2009-06-30
申请人： Alexander Straub , Thomas Lampe , Jens Pohlmann , Susanne Rohrig , Elisabeth Perzborn , Karl-Heinz Schlemmer , Joseph Pernerstorfer
发明人： Alexander Straub , Thomas Lampe , Jens Pohlmann , Susanne Rohrig , Elisabeth Perzborn , Karl-Heinz Schlemmer , Joseph Pernerstorfer
IPC分类号： A61K31/422 , C07D413/14 , C07D417/14 , C07D495/04 , C07D498/04 , C12N5/00 , A61K31/5377 , A61K31/541 , A61K31/4365 , A61K31/428 , A61K31/496 , A61K31/444 , A61K31/4545 , A61K31/423 , A61K31/538
CPC分类号： C07D498/04 , A61K31/5377 , C07D333/38 , C07D409/12 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/14 , C07D495/04
摘要： The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.
摘要翻译： 本发明涉及血液凝固领域。 描述了通式（I）的新型恶唑烷酮衍生物的制备及其作为用于预防和/或治疗病症的药物活性化合物的用途。
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公开(公告)号：US07598378B2
公开(公告)日：2009-10-06
申请号：US10571364
申请日：2004-09-09
IPC分类号： C07D413/14 , C07D295/135
CPC分类号： C07D265/32 , C07D409/14
摘要： The present invention relates to a process for preparing 4-(4-aminophenyl)-3-morpholinone by reacting 4-(4-nitrophenyl)-3-morpholinone with hydrogen in the presence of a hydrogenation catalyst, characterized in that the reaction is effected in an aliphatic alcohol.
摘要翻译： 本发明涉及通过在氢化催化剂存在下使4-（4-硝基苯基）-3-吗啉酮与氢气反应来制备4-（4-氨基苯基）-3-吗啉酮的方法，其特征在于进行反应 在脂肪醇中。
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公开(公告)号：US07585860B2
公开(公告)日：2009-09-08
申请号：US12027553
申请日：2008-02-07
申请人： Alexander Straub , Thomas Lampe , Jens Pohlmann , Susanne Rohrig , Elisabeth Perzborn , Karl-Heinz Schlemmer , Joseph Pernerstorfer
发明人： Alexander Straub , Thomas Lampe , Jens Pohlmann , Susanne Rohrig , Elisabeth Perzborn , Karl-Heinz Schlemmer , Joseph Pernerstorfer
IPC分类号： A61K31/5377 , C07D409/14
CPC分类号： C07D498/04 , A61K31/5377 , C07D333/38 , C07D409/12 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/14 , C07D495/04
摘要： The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.
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85.发明授权Substituted 2-oxo-3-phenyl-5-carbonylaminomethyl-1,3-oxazolines and their use as anticoagulant and antithrombotics 失效取代的2-氧代-3-苯基-5-羰基氨基甲基-1,3-恶唑啉及其作为抗凝血和抗血栓的用途公开(公告)号：US07582666B2
公开(公告)日：2009-09-01
申请号：US11394543
申请日：2006-03-31
申请人： Alexander Straub , Thomas Lampe , Josef Pernerstorfer , Elisabeth Perzborn , Jens Pohlmann , Susanne Rohrig , Karl-Heinz Schlemmer
发明人： Alexander Straub , Thomas Lampe , Josef Pernerstorfer , Elisabeth Perzborn , Jens Pohlmann , Susanne Rohrig , Karl-Heinz Schlemmer
IPC分类号： A61K31/422 , A61K31/5377 , C07D413/10 , C07D413/14 , C07D263/20
CPC分类号： C07D413/10 , C07D413/14
摘要： The invention relates to the field of blood coagulation, more particularly, to novel compounds of general formula (I), to a method for producing the compounds and to their use as active ingredients in medicaments for the prevention and/or the treatment of diseases.
摘要翻译： 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。
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公开(公告)号：US20070066611A1
公开(公告)日：2007-03-22
申请号：US10571364
申请日：2004-09-09
IPC分类号： C07D413/14 , A61K31/5377
CPC分类号： C07D265/32 , C07D409/14
摘要： The present invention relates to a process for preparing 4-(4-aminophenyl)-3-morpholinone by reacting 4-(4-nitrophenyl)-3-morpholinone with hydrogen in the presence of a hydrogenation catalyst, characterized in that the reaction is effected in an aliphatic alcohol.
摘要翻译： 本发明涉及通过在氢化催化剂存在下使4-（4-硝基苯基）-3-吗啉酮与氢气反应来制备4-（4-氨基苯基）-3-吗啉酮的方法，其特征在于进行反应 在脂肪醇中。
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87.发明授权公开(公告)号：US07157456B2
公开(公告)日：2007-01-02
申请号：US10181051
申请日：2000-12-11
申请人： Alexander Straub , Thomas Lampe , Jens Pohlmann , Susanne Röhrig , Elisabeth Perzborn , Karl-Heinz Schlemmer , Joseph Pernerstorfer
发明人： Alexander Straub , Thomas Lampe , Jens Pohlmann , Susanne Röhrig , Elisabeth Perzborn , Karl-Heinz Schlemmer , Joseph Pernerstorfer
IPC分类号： A61K31/5377 , C07D409/14
CPC分类号： C07D498/04 , A61K31/5377 , C07D333/38 , C07D409/12 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/14 , C07D495/04
摘要： The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.
摘要翻译： 本发明涉及血液凝固领域。 描述了通式（I）的新型恶唑烷酮衍生物的制备及其作为用于预防和/或治疗病症的药物活性化合物的用途。
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88.发明申请公开(公告)号：US20060183914A1
公开(公告)日：2006-08-17
申请号：US11403514
申请日：2006-04-13
申请人： Alexander Straub
发明人： Alexander Straub
IPC分类号： C07D277/36
CPC分类号： A01N43/78 , C07C331/04 , C07C333/20 , C07D277/36
摘要： The present invention relates to a process for preparing compounds of formula (IV) where R is H or F, by reacting a compound of formula (II) where where R is H or F, and X is bromine, chlorine, mesylate, or tosylate, with a thiocyanate salt of formula (III) M+SCN− (III) where M+ is hydrogen, an ammonium ion, a tetraalkylammonium ion, or an alkali metal or alkaline earth metal ion, optionally in the presence of a reaction auxiliary and optionally in the presence of a diluent.
摘要翻译： 本发明涉及制备其中R为H或F的式（Ⅳ）化合物的方法，其中R为H或F，X为溴，氯，甲磺酸酯或甲苯磺酸的式（Ⅱ）化合物 与式（III）的硫氰酸盐进行比较<？in-line-formula description =“In-line Formulas”end =“lead”→>> （III）<？in-line-formula description =“In-line formula”end =“tail”？>其中M +为氢，铵离子，四烷基铵离子或碱金属 或碱土金属离子，任选地在反应助剂存在下，任选地在稀释剂存在下。
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公开(公告)号：US06903089B1
公开(公告)日：2005-06-07
申请号：US10432740
申请日：2001-11-09
申请人： Johannes-Peter Stasch , Achim Feurer , Stefan Weigand , Elke Stahl , Dietmar Flubacher , Cristina Alonso-Alija , Frank Wunder , Dieter Lang , Klaus Dembowsky , Alexander Straub , Elisabeth Perzborn
发明人： 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分类号： A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/00 , A61P1/00 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/06 , A61P13/00 , A61P13/08 , A61P15/00 , A61P15/08 , A61P15/10 , A61P19/10 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P29/00 , A61P43/00 , C07D471/04 , C07D519/00 , A61K31/437
CPC分类号： C07D471/04
摘要： The invention relates to novel pyrazolopyridine derivatives of formula (I) wherein R1 represents NH2 or NHCO-C1-6-alkyl, and R2 represents a radical of formula R3NCOR4 which is bonded to the remainder of the molecule by means of the nitrogen atom, R3 and R4 forming, together with the amide group to which they are bonded, a five to seven-membered heterocycle which may be saturated or partially unsaturated, may optionally contain a further heteroatom selected from the group N, O, and S and may comprise between one and five other substituents chosen from oxo, C1-6alkyl, hydroxyl, hydroxy-C1-6-alkyl, halogen, or may be fused 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 the 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. Processes for preparing these materials, and pharmaceutical compositions containing them are also disclosed and claimed.
摘要翻译： 本发明涉及式（I）的新的吡唑并吡啶衍生物，其中R 1表示NH 2或NHCO-C 1-6 - 烷基，以及 R 2表示通过氮原子与分子的其余部分键合的式R 3 NCOR 4的基团， 与它们所键合的酰胺基一起形成可以是饱和或部分不饱和的五元至七元的杂环，可以任选地含有另外 选自N，O和S的杂原子，并且可以包含一个和五个其它选自氧代，C 1-6烷基，羟基，羟基-C 1-6的取代基， 或者可以与C 6〜10芳基环或C 3〜C 8环烷基环稠合，其中任选地两个碳原子键合到 彼此借助于氧原子。 本发明还涉及可溶性鸟苷酸环化酶刺激剂形式的衍生物的盐，异构体和水合物，以及用于治疗心血管疾病，高血压，血栓栓塞性疾病和局部缺血，性功能障碍，炎症和中枢神经疾病的药剂 系统。 制备这些材料的方法和含有它们的药物组合物也被公开并要求保护。
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公开(公告)号：US06462068B1
公开(公告)日：2002-10-08
申请号：US09644305
申请日：2000-08-23
申请人： Alexander Straub , Chantal Fürstner , Ulrich Niewöhner , Thomas Jaetsch , Achim Feurer , Raimund Kast , Johannes-Peter Stasch , Elisabeth Perzborn , Joachim Hütter , Klaus Dembowsky , Dieter Arlt
发明人： Alexander Straub , Chantal Fürstner , Ulrich Niewöhner , Thomas Jaetsch , Achim Feurer , Raimund Kast , Johannes-Peter Stasch , Elisabeth Perzborn , Joachim Hütter , Klaus Dembowsky , Dieter Arlt
IPC分类号： A61K31416
CPC分类号： C07D401/04 , C07D263/32 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/04
摘要： 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.
摘要翻译： 本发明涉及新的杂环基甲基取代的吡唑衍生物，其制备方法及其作为药物的用途，特别是用于治疗心血管疾病的药物。
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