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1. 发明授权

US5380746A Bis-(1H-indol-3-YL)-maleinimide derivatives, processes for the preparation thereof and pharmaceutical compositions containing them 失效
标题翻译：双（1H-吲哚-3-YL） - 马来酰亚胺衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5380746A
公开(公告)日：1995-01-10
申请号：US28528
申请日：1993-03-09
申请人： Hubert Barth , Johannes Hartenstein , Claus Rudolph , Christoph Schachtele , Hans-Jurgen Betche , Reinhard Reck , Hartmut Osswald
发明人： Hubert Barth , Johannes Hartenstein , Claus Rudolph , Christoph Schachtele , Hans-Jurgen Betche , Reinhard Reck , Hartmut Osswald
IPC分类号： C07D403/14 , C07D491/04 , C07D519/00 , C07D401/14 , A61K31/40 , A61K31/445 , A61K31/535 , C07D413/14
CPC分类号： C07D403/14 , C07D491/04
摘要： The present invention provides bis-(1H-indol-3-yl)maleinimide derivatives and the pharmacologically acceptable salts thereof, processes for the preparation of these compounds, and pharmaceutical compositions containing them for the treatment of heart and blood vessel diseases, such as thromboses, arteriosclerosis, hypertension, of inflammatory processes, allergies, cancer, and certain degenerative damages of the central nervous system, as well as of diseases of the immune system and viral diseases.
摘要翻译：本发明提供双 - （1H-吲哚-3-基）马来酰亚胺衍生物及其药学上可接受的盐，制备这些化合物的方法，以及含有它们的药物组合物，用于治疗心血管疾病如血栓形成，动脉硬化，高血压，炎症过程，过敏，癌症以及中枢神经系统的某些退行性损伤，以及免疫系统和病毒性疾病的疾病。

2. 发明授权

US4677108A 4-oxo-pyrido[2,3-d]pyrimidinone derivatives 失效
标题翻译： 4-氧代 - 吡啶并[2,3-d]嘧啶酮衍生物
公开(公告)号：US4677108A
公开(公告)日：1987-06-30
申请号：US787845
申请日：1985-10-16
申请人： Jurgen Kleinschroth , Gerhard Satzinger , Karl Mannhardt , Johannes Hartenstein , Hartmut Osswald , Gunter Weinheimer , Edgar Fritschi
发明人： Jurgen Kleinschroth , Gerhard Satzinger , Karl Mannhardt , Johannes Hartenstein , Hartmut Osswald , Gunter Weinheimer , Edgar Fritschi
IPC分类号： A61K31/505 , A61P3/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , C07D471/04 , A61K31/435
CPC分类号： C07D471/04
摘要： 4-Oxo-pyrido[2,3-d]pyrimidine derivatives are herein described as well as processes for their preparation.These compounds possess valuable pharmacological properties. As calcium antagonists they exert vasospasmolytic, vasodilatory, and antihypertensive activities. Surprisingly some of the compounds also have the effect of increasing contractility. They are therefore particularly suited for the treatment of vascular diseases.
摘要翻译：本文描述4-氧代 - 吡啶并[2,3-d]嘧啶衍生物及其制备方法。这些化合物具有有价值的药理学性质。作为钙拮抗剂，它们发挥血管痉挛，血管扩张和抗高血压活性。令人惊讶的是，一些化合物也具有增加收缩性的作用。因此，它们特别适用于治疗血管疾病。

3. 发明授权

US4612311A 1,2,4-benzothiadiazine oxide derivatives 失效
标题翻译： 1,2,4-苯并噻二嗪氧化物衍生物
公开(公告)号：US4612311A
公开(公告)日：1986-09-16
申请号：US772501
申请日：1985-09-04
申请人： Hubert Barth , Johannes Hartenstein , Gerhard Satzinger , Edgar Fritschi , Hartmut Osswald , Gerd Bartoszyk
发明人： Hubert Barth , Johannes Hartenstein , Gerhard Satzinger , Edgar Fritschi , Hartmut Osswald , Gerd Bartoszyk
IPC分类号： A61K31/395 , A61P25/24 , A61P25/26 , C07D513/04 , A61K31/54
CPC分类号： C07D513/04
摘要： 1,2,4-Benzothiadiazine oxide derivatives of the general Formula I ##STR1## in which R.sup.1 represents an unsubstituted or substituted aryl radical;R.sup.2 and R.sup.5, which may be the same or different, and represent hydrogen, halogen, or a nitro group, andR.sup.3 represents a hydrogen atom or a hydroxy radical, an alkyl, alkoxy alkyl or alkoxy carbonyl radical with up to four carbon atoms, unsubstituted or substituted by halogen, hydroxy, amino, alkyl amino or dialkyl amino radicals, or a phenyl radical, unsubstituted or substituted by halogen,are described as having anxiolytic effects on the central nervous system.
摘要翻译：其中R 1表示未取代或取代的芳基的通式I（I）的1,2,4-苯并噻二嗪氧化物衍生物; R 2和R 5可以相同或不同，表示氢，卤素或硝基，R 3表示氢原子或羟基，具有至多4个碳原子的烷基，烷氧基烷基或烷氧基羰基，被卤素，羟基，氨基，烷基氨基或二烷基氨基取代或被未取代或被卤素取代的苯基被描述为对中枢神经系统具有抗焦虑作用。

4. 发明授权

US5401875A 2-aminocarboxylic acids and their derivatives, processes for their preparation and their use as medicaments 失效
标题翻译： 2-氨基羧酸及其衍生物，其制备方法及其作为药物的用途
公开(公告)号：US5401875A
公开(公告)日：1995-03-28
申请号：US681500
申请日：1991-04-22
申请人： Uwe Trostmann , Johannes Hartenstein , Claus Rudolph , Christoph Schachtele , Hartmut Osswald , Gunter Weinheimer
发明人： Uwe Trostmann , Johannes Hartenstein , Claus Rudolph , Christoph Schachtele , Hartmut Osswald , Gunter Weinheimer
IPC分类号： A61K31/195 , A61K31/215 , A61K31/225 , A61P7/02 , A61P9/10 , A61P9/12 , A61P25/00 , A61P29/00 , A61P31/12 , A61P35/00 , A61P37/08 , A61P43/00 , C07C227/08 , C07C227/14 , C07C229/12 , C07C229/22 , C07C229/24 , C07C229/36
CPC分类号： C07C229/22 , C07C229/12 , C07C229/24 , C07C229/36
摘要： The invention concerns 2-aminocarboxylic acids and derivatives of formula ##STR1## processes for their preparation, as well as medicaments containing them for the inhibition of protein kinase C and thus for the prevention and/or treatment of heart and blood vessel diseases, such as thromboses, arterioscleroses, hypertension, of inflammatory processes, allergies, cancers, and certain degenerative damages of the central nervous system.
摘要翻译： PCT No.PCT / EP89 / 01293 Sec。 371日期1991年04月22日 102（e）日期1991年4月22日PCT提交1989年10月30日PCT公布。公开号WO90 / 05130 日期1990年5月17日本发明涉及2-氨基羧酸及其制备方法的衍生物，其制备方法以及含有它们用于抑制蛋白激酶C并因此用于预防和/或治疗心脏的药物以及诸如血栓形成，动脉硬化，高血压，炎症过程，过敏，癌症和中枢神经系统的某些退行性损伤的血管疾病。

5. 发明授权

US4762837A 4-alkoxy-pyrido[2,3-d]pyrimidine derivatives for treatment of myocardiac ischemia 失效
标题翻译： 4-烷氧基 - 吡啶并[2,3-d]嘧啶衍生物，用于治疗心肌缺血
公开(公告)号：US4762837A
公开(公告)日：1988-08-09
申请号：US55816
申请日：1987-05-29
申请人： Jurgen Kleinschroth , Gerhard Satzinger , Karl Mannhardt , Johannes Hartenstein , Hartmut Osswald , Gunter Weinheimer , Edgar Fritschi
发明人： Jurgen Kleinschroth , Gerhard Satzinger , Karl Mannhardt , Johannes Hartenstein , Hartmut Osswald , Gunter Weinheimer , Edgar Fritschi
IPC分类号： A61K31/435 , A61P3/00 , A61P3/14 , A61P9/00 , A61P9/10 , A61P25/02 , C07D471/04 , A61K31/505
CPC分类号： C07D471/04
摘要： 4-Alkoxy-pyrido[2,3-d]pyrimidine derivatives are described as well as processes for their preparation.For reason of their vasospasmolytic effects these compounds are mainly indicated for the treatment of cerebral, cardiac, and peripheral vascular diseases such as myocardiac ischemia, cerebral infarction, pulmonary thromboses, as well as in cases of arterioschlerosis and other stenotic disorders. They are therefore valuable agents for combating cardiovascular mortality.
摘要翻译：描述4-烷氧基 - 吡啶并[2,3-d]嘧啶衍生物及其制备方法。由于它们的血管痉挛分解作用，这些化合物主要用于治疗脑，心脏和外周血管疾病如心肌缺血，脑梗塞，肺血栓形成，以及动脉硬化和其他狭窄病变。因此，它们是抗心血管死亡率的有效药物。

6. 发明授权

US4751228A 1,6-naphthyridine derivatives 失效
标题翻译： 1,6-萘啶衍生物
公开(公告)号：US4751228A
公开(公告)日：1988-06-14
申请号：US7691
申请日：1987-01-28
申请人： Jorgen Kleinschroth , Karl Mannhardt , Johannes Hartenstein , Gerhard Satzinger , Dieter Muster , Wolfgang Steinbrecher , Bernd Wagner , Hartmut Osswald
发明人： Jorgen Kleinschroth , Karl Mannhardt , Johannes Hartenstein , Gerhard Satzinger , Dieter Muster , Wolfgang Steinbrecher , Bernd Wagner , Hartmut Osswald
IPC分类号： A61K31/435 , A61P3/00 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , C07D213/80 , C07D471/04
CPC分类号： C07D213/80 , C07D471/04
摘要： The present invention provides 1,6-naphthyridine derivatives of formula ##STR1## wherein R.sup.1 is an unsubstituted or substituted aromatic or heteroaromatic ring or an unsubstituted or substituted condensed aromatic or heterocyclic ring system, R.sup.2 is a straight-chained or branched alkyl radical containing up to 4 carbon atoms, a benzyl radical or a straight-chained or branched, substituted or unsubstituted aminoalkyl radical containing up to 8 carbon atoms, R.sup.3 is a hydrogen atom, a straight-chained or branched alkyl radical or an alkoxycarbonyl radical, in each case containing up to 4 carbon atoms, R.sup.4 is a straight-chained or branched hydrocarbon radical containing up to 21 carbon atoms, which can also contain oxygen, sulphur, nitrogen or halogen atoms and is optionally substituted by carbocyclic or heterocyclic ring systems, or is an amino, cyano, formyl, halogenomethyl or dihalomethyl radical and R.sup.5 is an alkoxycarbonyl radical or an unsubstituted or substituted carboxamide radical with, in each case, up to 21 carbon atoms which can also contain oxygen, sulphur or nitrogen atoms and is optionally substituted by carbocyclic or heterocyclic ring systems or is a carboxyl or cyano group as well as the pharmaceutically acceptable salts thereof.The compounds are useful for blood vessel diseases.The present invention also provides processes for the preparation of these 1,6-naphthyridine derivatives, pharmaceutical compositions containing them, and methods for using them.
摘要翻译：本发明提供了式（I）的1,6-萘啶衍生物，其中R 1是未取代或取代的芳族或杂芳环或未取代或取代的稠合芳族或杂环系，R2是直链或支链烷基含有至多4个碳原子的基团，含有至多8个碳原子的苄基或直链或支链，取代或未取代的氨基烷基，R3是氢原子，直链或支链烷基或烷氧基羰基，在每种情况下最多含有4个碳原子，R4是含有至多21个碳原子的直链或支链烃基，其也可以含有氧，硫，氮或卤素原子，并且任选地被碳环或杂环系统取代，或者是氨基，氰基，甲酰基，卤代甲基或二卤甲基，R5是烷氧基羰基或未取代或取代的酰胺基团w 在每种情况下，最多21个碳原子，其也可以含有氧，硫或氮原子，并且任选被碳环或杂环系统取代，或者是羧基或氰基以及其药学上可接受的盐。这些化合物可用于血管疾病。本发明还提供制备这些1,6-萘啶衍生物的方法，含有它们的药物组合物及其使用方法。

7. 发明授权

US4681882A 4-alkoxy-pyrido[2,3-d]pyrimidine derivatives 失效
标题翻译： 4-烷氧基 - 吡啶并[2,3-d]嘧啶衍生物
公开(公告)号：US4681882A
公开(公告)日：1987-07-21
申请号：US787844
申请日：1985-10-16
申请人： Jorgen Kleinschroth , Gerhard Satzinger , Karl Mannhardt , Johannes Hartenstein , Hartmut Osswald , Gonter Weinheimer , Edgar Fritschi
发明人： Jorgen Kleinschroth , Gerhard Satzinger , Karl Mannhardt , Johannes Hartenstein , Hartmut Osswald , Gonter Weinheimer , Edgar Fritschi
IPC分类号： A61K31/435 , A61P3/00 , A61P3/14 , A61P9/00 , A61P9/10 , A61P25/02 , C07D471/04
CPC分类号： C07D471/04
摘要： 4-Alkoxy-pyrido[2,3-d]pyrimidine derivatives are described as well as processes for their preparation.For reason of their vasospasmolytic effects these compounds are mainly indicated for the treatment of cerebral, cardiac, and peripheral vascular diseases such as myocardiac ischemia, cerebral infarction, pulmonary thromboses, as well as in cases of arteriosclerosis and other stenotic disorders. They are therefore valuable agents for combating cardiovascular mortality.
摘要翻译：描述4-烷氧基 - 吡啶并[2,3-d]嘧啶衍生物及其制备方法。由于它们的血管痉挛分解作用，这些化合物主要用于治疗脑，心脏和外周血管疾病如心肌缺血，脑梗塞，肺血栓形成，以及动脉硬化和其他狭窄病变。因此，它们是抗心血管死亡率的有效药物。

8. 发明授权

US06395256B1 Adenosine detection in small samples 失效
标题翻译：小样本中的腺苷检测
公开(公告)号：US06395256B1
公开(公告)日：2002-05-28
申请号：US09582150
申请日：2000-06-21
申请人： Hartmut Osswald , Doris Kloor
发明人： Hartmut Osswald , Doris Kloor
IPC分类号： A61K5100
CPC分类号： C12Q1/37 , G01N33/5308
摘要： The invention relates to a method for detecting adenosine with the inactive S-adenosyl homocysteine hydrolase's enzyme which selectively and only binds adenosine with high affinity. The inventive method enables adenosine to be determined in small sample volumes without the need for additional purification of said sample.
摘要翻译：本发明涉及一种利用非活性S-腺苷同型半胱氨酸水解酶检测腺苷的方法，该方法选择性且仅以高亲和力结合腺苷。本发明的方法使得能够以小的样品体积确定腺苷，而不需要额外纯化所述样品。

9. 发明授权

US5516915A Bis-(1H-indol-3-yl)-maleinimide derivatives, processes for the preparation thereof and pharmaceutical compositions containing them 失效
标题翻译：双（1H-吲哚-3-基） - 马来酰亚胺衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5516915A
公开(公告)日：1996-05-14
申请号：US304740
申请日：1994-09-12
申请人： Hubert Barth , Johannes Hartenstein , Claus Rudolph , Christoph Schachtele , Hans-Jurgen Betche , Reinhard Reck , Hartmut Osswald
发明人： Hubert Barth , Johannes Hartenstein , Claus Rudolph , Christoph Schachtele , Hans-Jurgen Betche , Reinhard Reck , Hartmut Osswald
IPC分类号： C07D403/14 , C07D491/04 , C07D519/00 , C07D401/14 , C07D413/14
CPC分类号： C07D403/14 , C07D491/04
摘要： The present invention provides bis-(1H-indol-3-yl)maleinimide derivatives and the pharmacologically acceptable salts thereof, processes for the preparation of these compounds, and pharmaceutical compositions containing them for the treatment of heart and blood vessel diseases, such as thromboses, arteriosclerosis, hypertension, of inflammatory processes, allergies, cancer, and certain degenerative damages of the central nervous system, as well as of diseases of the immune system and viral diseases.
摘要翻译：本发明提供双 - （1H-吲哚-3-基）马来酰亚胺衍生物及其药学上可接受的盐，制备这些化合物的方法，以及含有它们的药物组合物，用于治疗心血管疾病如血栓形成，动脉硬化，高血压，炎症过程，过敏，癌症以及中枢神经系统的某些退行性损伤，以及免疫系统和病毒性疾病的疾病。

10. 发明授权

US5034382A Topical composition for treating herpes with adenosine 失效
标题翻译：用腺苷治疗疱疹的局部组合物
公开(公告)号：US5034382A
公开(公告)日：1991-07-23
申请号：US357691
申请日：1989-05-25
申请人： Hartmut Osswald
发明人： Hartmut Osswald
IPC分类号： C07H19/167 , A61K8/60 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61P17/00 , A61P31/12 , A61Q19/00 , C07H19/16
CPC分类号： A61K31/70 , A61K8/606 , A61Q19/00 , A61Q19/001
摘要： The invention is concerned with the application of adenosine in the form of topically applicable pharmaceutical preparations for controlling herpes, in particular herpes labialis, herpes zoster, and herpes genitalis. The preparations are applied thinly several times daily to the affected skin or mucous areas. The active substance concentration should be in the region of 5-30%. Anhydrous preparations such as powder or anhydrous ointments have proven to be particularly effective and are surprisingly rapid in promoting healing.
摘要翻译：本发明涉及用于控制疱疹，特别是唇疱疹，带状疱疹和生殖疱疹的局部适用的药物制剂形式的腺苷的应用。每天将这些制剂每天稀释至受影响的皮肤或粘液区域。活性物质浓度应在5-30％的范围内。已经证明无水制剂如粉末或无水软膏特别有效，并且在促进愈合方面令人惊讶地快速。

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