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1. 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。

2. 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。

3. 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。

4. 发明授权

US4760081A 1,6-naphthyridine derivatives useful for treating diseases of the blood vessels 失效
标题翻译：可用于治疗血管疾病的1,6-萘啶衍生物
公开(公告)号：US4760081A
公开(公告)日：1988-07-26
申请号：US7686
申请日：1987-01-28
申请人： Gerhard Satzinger , Johannes Hartenstein , Karl Mannhardt , Jurgen Kleinschroth , Hartmut Osswald , Gunter Weinheimer , Edgar Fritschi
发明人： Gerhard Satzinger , Johannes Hartenstein , Karl Mannhardt , Jurgen Kleinschroth , Hartmut Osswald , Gunter Weinheimer , Edgar Fritschi
IPC分类号： C07D213/80 , C07D471/04 , A61K31/435
CPC分类号： C07D213/80 , C07D471/04
摘要： The present invention describes 1,6-naphthyridine derivatives of the general formula: ##STR1## wherein R.sup.1 is an unsubstituted or substituted aromatic or heteroaromatic ring, R.sup.2 is a straight-chained or branched alkyl radical containing up to four carbon atoms or a benzyl radical, R.sup.3 is a hydrogen atom, a straight-chained or branched alkyl radicals or an alkoxycarbonyl radical containing up to four carbon atoms, R.sup.4 is a straight-chained or branched alkyl radical containing up to four carbons and R.sup.5 is a carboxyl group or a straight-chained, branched or cyclic alkoxycarbonyl radical which contains up to 17 carbon atoms and optionally also contains an oxygen, sulphur or nitrogen atom; as well as the pharmacologically acceptable salts thereof, which are useful for treating diseases of the blood vessels.
摘要翻译：本发明描述了以下通式的1,6-萘啶衍生物：其中R 1是未取代或取代的芳族或杂芳族环，R 2是含有至多4个碳原子的直链或支链烷基或苄基 R3是氢原子，直链或支链烷基或含有最多四个碳原子的烷氧基羰基，R4是含有至多四个碳的直链或支链烷基，R5是羧基或直链链，支链或环状的烷氧基羰基，其含有至多17个碳原子，并且任选地还含有氧，硫或氮原子; 以及其药理学上可接受的盐，其可用于治疗血管疾病。

5. 发明授权

US4711901A 1-6-naphthyridine derivatives useful in the treatment of blood vessel diseases 失效
标题翻译：可用于治疗血管疾病的1-6-萘啶衍生物
公开(公告)号：US4711901A
公开(公告)日：1987-12-08
申请号：US891712
申请日：1986-07-30
申请人： Gerhard Satzinger , Johannes Hartenstein , Karl Mannhardt , Jurgen Kleinschroth , Hartmut Osswald , Gunter Weinheimer , Edgar Fritschi
发明人： Gerhard Satzinger , Johannes Hartenstein , Karl Mannhardt , Jurgen Kleinschroth , Hartmut Osswald , Gunter Weinheimer , Edgar Fritschi
IPC分类号： A61K31/435 , C07D213/80 , C07D471/04 , A61K31/44
CPC分类号： C07D213/80 , C07D471/04
摘要： The present invention describes 1,6-naphthyridine derivatives of the general formula: ##STR1## wherein R.sup.1 is an unsubstituted or substituted aromtic or heteroaromatic ring, R.sup.2 is a straight-chained or branched alkyl radical containing up to four carbon atoms or a benzyl radical, R.sup.3 is a hydrogen atom, a straight-chained or branched alkyl radical or an alkoxycarbonyl radical containing up to four carbon atoms, R.sup.4 is a straight-chained or branched alkyl radical containing up to four carbons and R.sup.5 is a carbonyl group or a straight-chained, branched or cyclic alkoxycarbonyl radical which contains up to 17 carbon atoms and optionally also contains an oxygen, sulphur or nitrogen atom; as well as the pharamacologically acceptable salts thereof, which are useful for treating diseases of the blood vessels.
摘要翻译：本发明描述了以下通式的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，R 2是含有至多4个碳原子的直链或支链烷基或苄基 R3是氢原子，直链或支链烷基或含有最多四个碳原子的烷氧基羰基，R4是含有至多四个碳的直链或支链烷基，R5是羰基或直链链，支链或环状的烷氧基羰基，其含有至多17个碳原子，并且任选地还含有氧，硫或氮原子; 以及其药学上可接受的盐，其可用于治疗血管疾病。

6. 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。

7. 发明授权

US4698341A Use of 1,6-naphthyridinone derivatives in treating pulmonary thrombosis 失效
标题翻译：使用1,6-萘啶酮衍生物治疗肺血栓形成
公开(公告)号：US4698341A
公开(公告)日：1987-10-06
申请号：US753758
申请日：1985-07-11
申请人： Gerhard Satzinger , Johannes Hartenstein , Karl Mannhardt , Jurgen Kleinschroth , Manfred Herrmann , Edgar Fritschi , Horst-Dietmar Tauschel , Bernd Wagner , Gunter Wolf
发明人： Gerhard Satzinger , Johannes Hartenstein , Karl Mannhardt , Jurgen Kleinschroth , Manfred Herrmann , Edgar Fritschi , Horst-Dietmar Tauschel , Bernd Wagner , Gunter Wolf
IPC分类号： C07D211/90 , C07D471/04 , A61K31/455 , A61K31/535
CPC分类号： C07D471/04 , C07D211/90
摘要： New 1,6-naphthyridinone derivatives of the formula I ##STR1## are herein described wherein R.sup.1 represents an unsubstituted or substituted aromatic or heteroaromatic ring;R.sup.2 is hydrogen, a straight-chained or branched alkyl, alkoxyalkyl, or a substituted or unsubstituted aminoalkyl group with up to ten carbon atoms;R.sup.3 is hydrogen, a straight-chained or branched alkyl group, or an alkoxycarbonyl radical with up to four carbon atoms;R.sup.4 is hydrogen, or a morpholinoethyl group;R.sup.5 is a straight-chained or branched alkyl group with up to four carbon atoms, or an amino group; andR.sup.6 is a carboxyl group, or an alkyl- or alkyloxyalkyl carbonyl radical, containing up to 12 carbon atoms and optionally interrupted by an oxygen, sulphur, or nitrogen atom;as well as optionally the pharmacologically acceptable salts thereof; processes for the preparation of these derivatives and their use in the control of vascular diseases.
摘要翻译：本文描述了式I（I）的新的1,6-萘啶酮衍生物，其中R 1表示未取代或取代的芳族或杂芳族环; R2是氢，直链或支链烷基，烷氧基烷基或具有至多10个碳原子的取代或未取代的氨基烷基; R3是氢，直链或支链烷基或具有至多四个碳原子的烷氧基羰基; R4是氢或吗啉代乙基; R5是具有至多4个碳原子的直链或支链烷基或氨基; 并且R 6是含有至多12个碳原子并任选被氧，硫或氮原子中断的羧基或烷基 - 或烷氧基烷基羰基; 以及任选地其药理学上可接受的盐; 这些衍生物的制备方法及其在血管疾病控制中的应用。

8. 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。

9. 发明授权

US4626546A 3-aryl-3-pyrroline derivatives 失效
标题翻译： 3-芳基-3-吡咯啉衍生物
公开(公告)号：US4626546A
公开(公告)日：1986-12-02
申请号：US637351
申请日：1984-08-03
申请人： Gerhard Satzinger , Karl Mannhardt , Johannes Hartenstein , Manfred Herrmann , Edgar Fritschi , Wolfgang Steinbrecher
发明人： Gerhard Satzinger , Karl Mannhardt , Johannes Hartenstein , Manfred Herrmann , Edgar Fritschi , Wolfgang Steinbrecher
IPC分类号： A61K31/40 , A61P9/08 , A61P9/10 , C07D207/20
CPC分类号： C07D207/20
摘要： The invention is concerned with partially new compounds of the general formula ##STR1## wherein R.sup.1 is a hydrogen atom or an alkyl group with up to four carbon atoms and R.sup.2 a substituted phenyl radical and the pharmacologically acceptable salts thereof.The compounds can be prepared according to known procedures and show surprisingly a cardiovascular efficacy. They are capable of decompensating cardiac insufficiencies to a large extent. In addition to the new compounds, claim is also made for pharmaceutical compositions which contain compounds according to the general formula and their application for controlling cardiac and vascular diseases.
摘要翻译：本发明涉及通式“IMAGE”的部分新化合物，其中R 1为氢原子或具有至多4个碳原子的烷基，R 2为取代的苯基及其药理学上可接受的盐。这些化合物可以根据已知的方法制备并令人惊奇地显示出心血管功能。它们能够在很大程度上失代偿心脏功能不全。除了新化合物之外，还提出了含有根据通式的化合物及其用于控制心脏和血管疾病的应用的药物组合物。

10. 发明授权

US4587263A Cycloaliphatic aminosulfonic acid derivatives 失效
标题翻译：环脂族氨基磺酸衍生物
公开(公告)号：US4587263A
公开(公告)日：1986-05-06
申请号：US634839
申请日：1984-07-26
申请人： Gerhard Satzinger , Johannes Hartenstein , Edgar Fritschi , Wolf-Dieter Vigelius
发明人： Gerhard Satzinger , Johannes Hartenstein , Edgar Fritschi , Wolf-Dieter Vigelius
IPC分类号： A61K31/185 , A61P9/06 , A61P9/12 , C07C67/00 , C07C301/00 , C07C303/02 , C07C303/24 , C07C309/19 , C07C143/21
CPC分类号： C07C309/19 , C07C2101/08 , C07C2101/14 , C07C2101/18
摘要： New aminosulfonic acids of the general formula I ##STR1## wherein n represents the figures 4, 5, or 6, prepared according to previously known processes and characterized by very good tolerance and valuable cardiovascular properties, serve for the therapy of dysrhythmia and are superior to procaine.
摘要翻译：通式I的新的氨基磺酸（I）其中n代表按照先前已知的方法制备并以非常好的耐受性和有价值的心血管特性为特征的图4,5或6，用于治疗心律失常和优于普鲁卡因。

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