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1. 发明申请

US20050176799A1 Pyrazole derivatives, their preparation and their use in pharmaceuticals 有权
标题翻译：吡唑衍生物，其制备及其在药物中的应用
公开(公告)号：US20050176799A1
公开(公告)日：2005-08-11
申请号：US11104556
申请日：2005-04-13
申请人： Ursula Schindler , Karl Schonafinger , Hartmut Strobel
发明人： Ursula Schindler , Karl Schonafinger , Hartmut Strobel
IPC分类号： A61K31/415 , A61K31/00 , A61K31/34 , A61P1/00 , A61P1/16 , A61P3/00 , A61P3/10 , A61P9/00 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/00 , A61P13/12 , A61P25/28 , A61P43/00 , C07D231/56 , C07D307/34 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D417/14 , A61K31/416 , C07D43/04 , C07D45/04 , C07D49/04
CPC分类号： C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14
摘要： The present invention relates to pyrazole derivatives of the formula I, their preparation and their use in pharmaceuticals: in which X, R1, R1a, R2, R3, R4 and n are as defined in the claims, which are useful pharmaceutically active compounds for the therapy and prophylaxis of illnesses, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate “cGMP” and are generally suitable for the therapy and prophylaxis of illnesses which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned illnesses and for preparing pharmaceuticals for this purpose, and also to pharmaceutical preparations which comprise the compounds of the formula I.
摘要翻译：本发明涉及式I的吡唑衍生物及其制备及其在药物中的用途：其中X，R 1，R 1a，R 2， R 3，R 4，R 4和n如权利要求中所定义，它们是用于治疗和预防疾病的有用的药物活性化合物，例如心血管疾病如高血压，心绞痛，心功能不全，血栓形成或动脉粥样硬化。式I的化合物能够调节身体产生的环鸟苷酸“cGMP”，通常适用于治疗和预防与受干扰的cGMP平衡有关的疾病。本发明还涉及用于制备式I化合物的方法，其用于治疗和预防上述疾病和用于制备用于该目的的药物，还涉及包含式I化合物的药物制剂。

2. 发明授权

US5679704A Use of 2- (N-(2-aminoethyl)amino) acetic acid derivatives 失效
标题翻译：使用2-（N-（2-氨基乙基）氨基）乙酸衍生物
公开(公告)号：US5679704A
公开(公告)日：1997-10-21
申请号：US543395
申请日：1995-10-16
申请人： Karl Schonafinger , Ursula Schindler , Eckhard Schraven
发明人： Karl Schonafinger , Ursula Schindler , Eckhard Schraven
IPC分类号： A61K31/195 , A61K31/198 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/415 , A61K31/4172 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4406 , A61P3/08 , A61P3/10 , C07D233/64 , C07D277/22 , C07D307/54 , C07D333/24
CPC分类号： A61K31/4406 , A61K31/195 , A61K31/198 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/415 , A61K31/4172 , A61K31/425 , A61K31/426 , A61K31/44
摘要： The invention relates to the use of 2-(N-(2-aminoethyl)amino)acetic acid derivatives of the formula I ##STR1## in which R denotes, for example, phenyl or thienyl, and their pharmacologically acceptable acid addition salts as pharmacological active compounds.
摘要翻译：本发明涉及使用式I的2-（N-（2-（2-氨基乙基）氨基）乙酸衍生物，其中R表示例如苯基或噻吩基，以及它们的药理学上可接受的酸加成盐作为药理活性化合物。

3. 发明授权

US5424326A Phenyl-1,2,5-oxadiazolecarboxamide-2-oxides, their preparation and their use 失效
标题翻译：苯基-1,2,5-氧杂二环甲酰胺-2-氧化物，其制备及其应用
公开(公告)号：US5424326A
公开(公告)日：1995-06-13
申请号：US66986
申请日：1993-05-25
申请人： Karl Schonafinger , Helmut Bohn
发明人： Karl Schonafinger , Helmut Bohn
IPC分类号： A61K31/41 , A61K31/415 , A61K31/4245 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/496 , A61K31/505 , A61P9/00 , C07D271/08 , C07D413/04 , C07D413/12
CPC分类号： C07D413/12 , C07D271/08
摘要： The present invention relates to phenyl-1,2,5-oxadiazolecarboxamide-2-oxides of the general formula I ##STR1## in which one of the radicals R.sup.1 and R.sup.2 represents ##STR2## and the other represents ##STR3## and R.sup.3 and R.sup.4 are defined as indicated in claim 1, to processes for their preparation and to their use for the treatment of disorders of the cardiovascular system, including angina pectoris and erectile dysfunctions.
摘要翻译：本发明涉及通式Ⅰ（I）的苯基-1,2,5-氧杂双环唑酰胺-2-氧化物，其中基团R1和R2之一表示“IMAGE”，另一个表示和 R3和R4如权利要求1所述定义，用于其制备方法及其用于治疗心血管系统疾病的用途，包括心绞痛和勃起功能障碍。

4. 发明授权

US5006540A Substituted 3-aminosydnonimines, processes for their preparation and their use 失效
标题翻译：取代的3-氨基亚氨基亚胺，其制备方法及其用途
公开(公告)号：US5006540A
公开(公告)日：1991-04-09
申请号：US422502
申请日：1989-10-17
申请人： Karl Schonafinger , Rudi Beyerle , Melitta Just , Helmut Bohn , Jorg Ostrowski
发明人： Karl Schonafinger , Rudi Beyerle , Melitta Just , Helmut Bohn , Jorg Ostrowski
IPC分类号： A61K31/41 , A61K31/4245 , A61P7/02 , A61P9/00 , C07D271/04 , C07D413/12
CPC分类号： C07D271/04
摘要： Substituted 3-aminosydnonimines of the formula I ##STR1## and their pharmacologically acceptable acid addition salts, wherein R.sup.1 denotes, for example, alkyl having 1 to 8 C atoms, R.sup.2 denotes hydrogen or the radical --COR.sup.3 and R.sup.3 denotes, for example, an aliphatic radical having 1 to 4 C atoms, are prepared, for example, by cyclization of a compound of the formula II ##STR2## and if appropriate subsequent acylation and have useful pharmacological properties.
摘要翻译：式I（I）的取代的3-氨基亚氨基亚胺及其药理学上可接受的酸加成盐，其中R 1表示例如具有1至8个C原子的烷基，R 2表示氢或基团-COR 3，R 3表示用于例如，具有1至4个C原子的脂族基团，例如通过使式II化合物（II）环化，并且如果合适，则随后进行酰化并具有有用的药理学性质。

5. 发明授权

US4452797A 3-Aminosydnonimines compounds and their use 失效
标题翻译： 3-氨基壬腈化合物及其用途
公开(公告)号：US4452797A
公开(公告)日：1984-06-05
申请号：US233055
申请日：1981-02-10
申请人： Karl Schonafinger , Rudi Beyerle , Rolf-Eberhard Nitz , Piero A. Martorana , Volker Fiedler
发明人： Karl Schonafinger , Rudi Beyerle , Rolf-Eberhard Nitz , Piero A. Martorana , Volker Fiedler
IPC分类号： C07D413/04 , A61K31/4245 , A61K31/425 , A61K31/495 , A61K31/496 , A61K31/54 , A61P9/00 , A61P9/12 , C07D271/04 , C07D295/28 , C07D413/06 , C07D417/04 , C07D403/04 , A61K31/38 , A61K31/41
CPC分类号： C07D295/30 , C07D271/04
摘要： Physiologically-acceptable 3-aminosydnonimines of the formula ##STR1## and their pharmacologically-acceptable acid-addition salts, when formulated into medicament dosage forms, are useful for reducing systemic blood pressure, pulmonary artery pressure and left ventricular end diastolic pressure when orally administered to patients in need of such pressure reduction. These compounds are prepared by cyclizing a compound which, in its free-base state, is of the formula ##STR2## to a corresponding product which, in its free-base state, is of the formula ##STR3## and, when R.sup.2 is other than -H, acylating that product.
摘要翻译：当配制成药物剂型时，式（I）的生理学上可接受的3-氨基亚氨基亚胺及其药理学上可接受的酸加成盐可用于降低全身血压，肺动脉压和左心室舒张末期压口服给予需要减压的患者。这些化合物通过将其游离碱状态为具有式（II）的化合物环化成相应的产物，其在其游离碱状态下具有式（Ia）并且当R2不是-H时，酰化该产物。

6. 发明授权

US4436743A 3-[N-(Lower alkyl)-N-(tetrahydro-3-thienyl 5,5-dioxide)]sydnonimines 失效
标题翻译： 3- [N-（低级烷基）-N-（四氢-3-噻吩基-5,5-二氧化物）]脱水亚胺
公开(公告)号：US4436743A
公开(公告)日：1984-03-13
申请号：US350366
申请日：1982-02-19
申请人： Karl Schonafinger , Rudi Beyerle , Helmut Bohn , Melitta Just , Piero A. Martorana , Rolf-Eberhard Nitz
发明人： Karl Schonafinger , Rudi Beyerle , Helmut Bohn , Melitta Just , Piero A. Martorana , Rolf-Eberhard Nitz
IPC分类号： C07D409/12 , A61K31/41 , A61K31/4245 , A61K31/495 , A61K31/496 , A61P9/00 , A61P9/12 , C07D271/04 , C07D413/12
CPC分类号： C07D271/04
摘要： Pharmacologically-active 3-aminosydnonimines (which are optionally substituted in the N.sup.6 -position) and their physiologically-acceptable acid-addition salts are compounded into standard dosage-form medicament compositions and are useful for prophylaxis for and treatment of cardiovascular-system disorders, such as high blood pressure and angina pectoris. The 3-aminosydnonimines are 3-[4-(lower alkoxy)carbonylpiperazin-1-yl]sydnonimines and 3-[N-(lower alkyl)-N-(tetrahydro-3-thienyl S,S-dioxide)]-sydnonimines.
摘要翻译：将药理学活性的3-氨基二氢亚胺（其在N6位任选被取代）及其生理上可接受的酸加成盐复合到标准剂型药物组合物中，并且可用于预防和治疗心血管系统疾病，例如作为高血压和心绞痛。 3-氨基二膦酰亚胺是3- [4-（低级烷氧基）羰基哌嗪-1-基]次氨基亚胺和3- [N-（低级烷基）-N-（四氢-3-噻吩基S，S-二氧化物）] - 二氢亚胺。

7. 发明授权

US5382585A Pyrimidofuroxans, their preparation and their use 失效
标题翻译：吡嘧霉酮，其制备及其用途
公开(公告)号：US5382585A
公开(公告)日：1995-01-17
申请号：US66904
申请日：1993-05-25
申请人： Joachim Brendel , Karl Schonafinger , Helmut Bohn
发明人： Joachim Brendel , Karl Schonafinger , Helmut Bohn
IPC分类号： A61K31/505 , A61P9/00 , A61P13/02 , A61P15/00 , C07D498/04 , A61K31/495 , A61K31/50 , C07D413/00 , C07D413/02
CPC分类号： C07D498/04
摘要： The present invention relates to pyrimidofuroxans of the general formula I ##STR1## in which A denotes ##STR2## where in each case the nitrogen atom is bonded via the C-4 and the carbon atom via the C-3 of the furoxan ring and the R radicals are defined as indicated in Claim 1, processes for their preparation and their use for the control and prevention of disorders of the cardiovascular system, in particular for the control and prevention of angina pectoris, and for the treatment of erectile dysfunctions.
摘要翻译：本发明涉及通式I的嘧啶酮，其中A表示“IMAGE”，其中在每种情况下，氮原子通过C-4和碳原子通过C-3的C-3键合呋喃环和R基团如权利要求1所述定义，其制备方法及其用于控制和预防心血管系统疾病，特别是用于控制和预防心绞痛以及治疗勃起功能的用途功能障碍

8. 发明授权

US5015659A Thienylacetic acid derivatives, process for the preparation thereof, the use thereof, and pharmaceuticals containing these and the preparation thereof 失效
标题翻译：噻吩乙酸衍生物，其制备方法，其用途和含有它们的药物及其制备方法
公开(公告)号：US5015659A
公开(公告)日：1991-05-14
申请号：US495439
申请日：1990-03-14
申请人： Karl Schonafinger , Rudi Beyerle , Ursula Schindler , Bernd Jablonka , Jeffery Troke
发明人： Karl Schonafinger , Rudi Beyerle , Ursula Schindler , Bernd Jablonka , Jeffery Troke
IPC分类号： A61K31/00 , A61K31/38 , A61K31/381 , A61P25/00 , A61P25/28 , C07D333/24
CPC分类号： C07D333/24
摘要： The present invention relates to thienylacetic acid derivatives of the general formula I ##STR1## in which X denotes --O-- or --NH--;R.sup.1 denotes hydrogen, the group --CH.sub.2 --CO--R.sup.3 or the group --CO--CH.sub.2 --NH.sub.2 ;R.sup.2 denotes hydrogen, (C.sub.1 -C.sub.4)-alkyl or the radical R.sup.1 andR.sup.3 denotes (C.sub.1 -C.sub.4)-alkoxy, hydroxyl or amino, it not being possible for both R.sup.1 and R.sup.2 to represent hydrogen when X denotes O,as well as the pharmaceutically tolerated salts thereof, process for the preparation thereof, the use thereof, and pharmaceuticals containing these and the preparation thereof.
摘要翻译：本发明涉及通式I（I）的噻吩乙酸衍生物，其中X表示-O-或-NH-; R1表示氢，基团-CH2-CO-R3或基团-CO-CH2-NH2; R 2表示氢，（C 1 -C 4） - 烷基或基团R 1和R 3表示（C 1 -C 4） - 烷氧基，羟基或氨基，当X表示O时，R 1和R 2都不可能表示氢，其药学上可接受的盐，其制备方法，其用途和含有它们的药物及其制备方法。

9. 发明授权

US4942168A Hydroxyquinoline amines, and method of enhancing memory in mammals 失效
标题翻译：羟基喹啉胺，以及增强哺乳动物记忆的方法
公开(公告)号：US4942168A
公开(公告)日：1990-07-17
申请号：US164596
申请日：1988-03-07
申请人： Karl Schonafinger , Helen H. Ong
发明人： Karl Schonafinger , Helen H. Ong
IPC分类号： C07D498/04
CPC分类号： C07D498/04
摘要： There are disclosed novel compounds of the formula ##STR1## where X is hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, nitro or trifluoromethyl; R.sub.1 is hydrogen or loweralkyl; R.sub.2 is hydrogen, loweralkyl, arylloweralkyl or --(CH.sub.2).sub.m R.sub.7 wherein m is 1, 2 or 3 and R.sub.7 is cyano or amino; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R.sub.5 and R.sub.6 are independently hydrogen or loweralkyl, or R.sub.5 +R.sub.6 taken together with the carbon atom to which they are attached constitute a cyclobutane, cyclopentane, cyclohexane, cycloheptane, pyrrolidine, piperidine, morpholine or thiomorpholine ring, or R.sub.5 is hydrogen and R.sub.6 is aryl or --CH.sub.2 OR.sub.8 wherein R.sub.8 is hydrogen, loweralkyl or loweralkylcarbonyl, which are useful for enhancing memory.
摘要翻译：公开了下式的新化合物：其中X是氢，低级烷基，低级烷氧基，羟基，卤素，硝基或三氟甲基; R1是氢或低级烷基; R2是氢，低级烷基，芳基低级烷基或 - （CH2）mR7，其中m是1,2或3，R7是氰基或氨基; R3和R4独立地是氢或低级烷基; R5和R6独立地是氢或低级烷基，或者R5 + R6与它们所连接的碳原子一起构成环丁烷，环戊烷，环己烷，环庚烷，吡咯烷，哌啶，吗啉或硫代吗啉环，或R 5是氢，R 6是芳基或-CH 2 OR 8，其中R 8是氢，低级烷基或低级烷基羰基，其可用于增强记忆。

10. 发明授权

US4743601A Dihydro-1,4-oxazino(2,3-C)quinolines 失效
标题翻译：二氢-1,4-恶嗪（2,3-C）喹啉
公开(公告)号：US4743601A
公开(公告)日：1988-05-10
申请号：US72832
申请日：1987-07-13
申请人： Karl Schonafinger , Helen H. Ong
发明人： Karl Schonafinger , Helen H. Ong
IPC分类号： C07D498/04 , A61K31/535 , A61K31/54 , C07D513/20
CPC分类号： C07D498/04
摘要： There are disclosed novel compounds of the formula ##STR1## where X is hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, nitro or trifluoromethyl; R.sub.1 is hydrogen or loweralkyl; R.sub.2 is hydrogen, loweralkyl, arylloweralkyl or --(CH.sub.2).sub.m R.sub.7 wherein m is 1, 2 or 3 and R.sub.7 is cyano or amino; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R.sub.5 and R.sub.6 are independently hydrogen or loweralkyl, or R.sub.5 +R.sub.6 taken together with the carbon atom to which they are attached constitute a cyclobutane, cyclopentane, cyclohexane, cycloheptane, pyrrolidine, piperidine, morpholine or thiomorpholine ring, or R.sub.5 is hydrogen and R.sub.6 is aryl or --CH.sub.2 OR.sub.8 wherein R.sub.8 is hydrogen, loweralkyl or loweralkylcarbonyl, which are useful for enhancing memory.

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