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公开(公告)号：US4816485A
公开(公告)日：1989-03-28
申请号：US31810
申请日：1987-03-30
IPC分类号： A61K31/165 , A61K20060101 , A61P31/12 , A61P35/00 , A61P37/06 , C07C20060101 , C07C231/00 , C07C231/02 , C07C233/65 , C07C237/40 , C07K1/113 , C07K5/08
CPC分类号： C07C237/40 , A61K31/165 , C07C231/02 , C07C231/12 , Y10S514/885
摘要： N-phenylbenzamide derivatives of the general formula I ##STR1## wherein the radicals R.sup.1, R.sup.2, and R.sup.3, which can be the same or different, are a hydrogen atom or a methyl radical, as well as the pharmacologically acceptable salts thereof for controlling malignant, proliferative and auto-immune diseases and for immunosuppressive therapy upon grafting are described.
摘要翻译： 通式I（I）的N-苯基苯甲酰胺衍生物，其中可以相同或不同的基团R 1，R 2和R 3是氢原子或甲基，以及其药理学上可接受的盐 描述了用于控制恶性，增殖性和自身免疫性疾病以及在接枝时的免疫抑制治疗。
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32.发明授权
公开(公告)号：US4563471A
公开(公告)日：1986-01-07
申请号：US608298
申请日：1984-05-08
IPC分类号： C07D317/50 , A61K31/425 , A61K31/426 , A61P21/02 , A61P25/00 , A61P25/08 , C07D277/20 , C07D277/34 , C07D417/12
CPC分类号： C07D277/34
摘要： 4-Oxothiazolidin-2-ylidene-acetamide derivatives, processes for their preparation, pharmaceutical compositions and a method for treating diseases of the central nervous system such as epilepsy are described.
摘要翻译： 描述了4-氧代噻唑烷-2-亚基 - 乙酰胺衍生物，其制备方法，药物组合物和治疗中枢神经系统疾病如癫痫的方法。
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33.发明授权2-Pyrrolin-3-carbonitrile derivatives, and pharmaceutical compositions containing them and their anti-inflammatory and ulcer protective activity 失效2-吡咯啉-3-腈衍生物和含有它们的药物组合物及其抗炎和溃疡保护活性
公开(公告)号：US4517185A
公开(公告)日：1985-05-14
申请号：US478762
申请日：1983-03-25
申请人： Hubert Barth , Edgar Fritschi , Volker Ganser , Johannes Hartenstein , Manfred Herrmann , Gerhard Satzinger
发明人： Hubert Barth , Edgar Fritschi , Volker Ganser , Johannes Hartenstein , Manfred Herrmann , Gerhard Satzinger
IPC分类号： C07D207/24 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/495 , A61K31/535 , A61P1/04 , A61P29/00 , C07D207/36 , C07D207/38 , C07D401/04 , C07D401/14 , C07D409/04
CPC分类号： C07D401/04 , C07D207/36 , C07D207/38 , C07D401/14 , C07D409/04
摘要： The present invention provides compounds of the general formula I ##STR1## wherein R.sup.1 and R.sup.2, which are the same or different, are unsubstituted or substituted aromatic rings, Alk is a straight-chained or branched lower hydrocarbon chain and Z is a hydrogen atom, with the proviso that when Alk is a straight-chained hydrocarbon chain, Z can also be a lower alkylamino radical of the general formula II ##STR2## in which R.sup.3 and R.sup.4 are the same or different and are hydrogen atoms or straight-chained or branched lower alkyl radicals or R.sup.3 and R.sup.4, together with the nitrogen atom to which they are attached, can also form a ring optionally containing further hetero atoms; and the pharmacologically acceptable salts thereof.The present invention also provides an inventive process for preparing these compounds, as well as pharmaceutical compositions containing them. The compounds I may be used in the therapy of inflammations and they are free of gastrointestinal side effects.
摘要翻译： 本发明提供了通式I（I）的化合物，其中R 1和R 2相同或不同，为未取代或取代的芳环，Alk为直链或支链低级烃链，Z为 氢原子，条件是当Alk是直链烃链时，Z还可以是通式II（II）的低级烷基氨基，其中R 3和R 4相同或不同，并且是氢原子 或直链或支链的低级烷基或R3和R4与它们所连接的氮原子一起也可以形成任选含有其它杂原子的环; 及其药理学上可接受的盐。 本发明还提供了制备这些化合物的本发明方法，以及含有它们的药物组合物。 化合物I可用于治疗炎症，并且它们没有胃肠道副作用。
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公开(公告)号：US4415495A
公开(公告)日：1983-11-15
申请号：US238501
申请日：1981-02-24
申请人： Gerhard Satzinger , Manfred Herrmann , Edgar Fritschi , Heinrich Bahrmann , Volker Ganser , Bernd Wagner , Wolfgang Steinbrecher
发明人： Gerhard Satzinger , Manfred Herrmann , Edgar Fritschi , Heinrich Bahrmann , Volker Ganser , Bernd Wagner , Wolfgang Steinbrecher
IPC分类号： C07D225/06 , A61K31/395 , A61K31/485 , A61P9/06 , C07D225/08 , A61K31/355
CPC分类号： C07D225/08
摘要： The present invention provides 5,6;8,9-tetrahydro-7H-dibenz(d,f)azonine derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2, which are the same or different, are hydrogen or halogen atoms or lower alkyl or alkoxy radicals, R.sup.3 is a hydrogen atom or a lower alkyl radical, R.sup.4 is a hydrogen atom or a lower alkyl or alkanoyl radical and n is 1 or 2; and the pharmaceutically acceptable salts thereof formed with inorganic and organic acids; but excluding 6-benzyl-2,12-dimethoxy-1-hydroxy-7-methyl-5,6;8,9-tetrahydro-7H-dibenz(d,f)azonine in which case R.sup.1, R.sup.2 and R.sup.4 are hydrogen, n is 1 and R.sup.3 is methyl. The lower alkyl, alkanoyl and alkoxy radicals are straight chained or branched radicals containing 1 to 5 carbon atoms.The present invention also provides a process for the preparation of these compounds, as well as pharmaceutical compositions containing them.
摘要翻译： 本发明提供下式的5,6,8,9-四氢-7H-二苯并（d，f）吖嗪衍生物：其中R 1和R 2相同或不同，为氢或卤原子或更低级 烷基或烷氧基，R3是氢原子或低级烷基，R4是氢原子或低级烷基或烷酰基，n是1或2; 和其与无机酸和有机酸形成的药学上可接受的盐; 但不包括6-苄基-2,12-二甲氧基-1-羟基-7-甲基-5,6; 8,9-四氢-7H-二苯并吖嗪（d，f）吖嗪，其中R1，R2和R4是氢 ，n为1，R 3为甲基。 低级烷基，烷酰基和烷氧基是含有1至5个碳原子的直链或支链基团。 本发明还提供了制备这些化合物的方法以及含有它们的药物组合物。
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公开(公告)号：US4259494A
公开(公告)日：1981-03-31
申请号：US83892
申请日：1979-10-11
申请人： Peter Stoss , Gerhard Satzinger , Manfred Herrmann
发明人： Peter Stoss , Gerhard Satzinger , Manfred Herrmann
IPC分类号： A61K31/38 , A61K31/381 , A61K31/382 , A61K31/385 , A61K31/39 , A61K31/445 , A61K31/54 , A61K31/5415 , A61P7/10 , A61P11/14 , A61P25/20 , A61P43/00 , C07D279/34 , C07D285/38 , C07D327/08 , C07D333/76 , C07D335/12 , C07D337/12 , C07D339/08 , C07D411/12
CPC分类号： C07D279/34 , C07D327/08 , C07D333/76 , C07D335/12 , C07D339/08
摘要： The present invention is concerned with novel tricyclic sulphoximides and with the preparation thereof. This family of compounds has been found to possess antihistaminic, antitussive, antiinflammatory, sedative, and diuretic properties.
摘要翻译： 本发明涉及新型三环磺酰亚胺及其制备方法。 已发现这一化合物族具有抗组胺，镇咳，抗炎，镇静，利尿等特性。
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36.发明授权
公开(公告)号：US4041166A
公开(公告)日：1977-08-09
申请号：US668159
申请日：1976-03-18
IPC分类号： A61K31/425 , C07D417/04 , A61K31/44
CPC分类号： C07D417/04 , A61K31/425
摘要： The present invention relates to novel thiazolidinone acetic acid derivatives and their preparation. These derivatives show diuretic properties when used as pharmaceuticals.
摘要翻译： 本发明涉及新型噻唑烷酮乙酸衍生物及其制备方法。 这些衍生物在用作药物时显示利尿特性。
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37.发明授权Process for the preparation of 4r-amino-1t-phenyl-1c-ethoxycarbonyl-cyclohexenes-(2) 失效制备4-氨基-1-苯基-c-乙氧基羰基 - 环己烯的方法（2）
公开(公告)号：US4008233A
公开(公告)日：1977-02-15
申请号：US528107
申请日：1974-11-29
IPC分类号： C07D211/14 , C07D211/34 , C07D295/155 , C07C101/38 , C07D295/14
CPC分类号： C07D295/155 , C07D211/14 , C07D211/34
摘要： This invention relates to 4r-amino-1t-phenyl-1c-ethoxycarbonyl-cyclohexenes-(2) of formula I: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and are hydrogen or alkyl having 1 to 4 carbon atoms, or one of the two groups is allyl, phenalkyl having 7 to 9 carbon atoms or .alpha.-methyl-.beta.-hydroxyethyl; or R.sub.1 and R.sub.2 together form a morpholino group, piperazino group substituted at the 4- position by methyl, benzyl, phenyl, 3-chlorophenyl, 4-chlorophenyl, 2-phenethyl or benzoyl, or a piperidino group substituted at the 4- position by hydroxyl, phenyl, 2-methoxyphenyl, 4-methoxyphenyl, methyl or benzyl and medically acceptable addition compounds derived from inorganic and organic acids or lower alkyl halides. The compounds of the present invention are prepared by separation of 4-amino-1-phenyl-1-ethoxycarbonyl-cyclohexenes-(2), described in U.S. Patent Application Ser. No. 226,509, filed Feb. 15, 1972, into the two possible geometrical isomers. The instant compounds, the 4r-amino-1t-phenyl-1c-ethoxycarbonyl-cyclohexenes-(2) of formula I, exhibit marked analgesic and neuroleptic activities and are useful for the alleviation and reduction of pain.
摘要翻译： 本发明涉及式I的4r-氨基-1t-苯基-c-乙氧基羰基 - 环己烯 - （2）：其中R 1和R 2相同或不同，为氢或具有1至4个碳原子的烷基， 或两个基团中的一个为烯丙基，具有7至9个碳原子的苯基烷基或α-甲基-β-羟乙基; 或R 1和R 2一起形成吗啉代基，在4-位上被甲基，苄基，苯基，3-氯苯基，4-氯苯基，2-苯乙基或苯甲酰基取代的哌嗪基或在4-位取代的哌啶子基， 羟基，苯基，2-甲氧基苯基，4-甲氧基苯基，甲基或苄基，以及衍生自无机和有机酸或低级烷基卤的医药上可接受的加成化合物。 本发明的化合物是通过分离美国专利申请序列号中描述的4-氨基-1-苯基-1-乙氧基羰基 - 环己烯 - （2）制备的。 1972年2月15日提交的226,509号的两种可能的几何异构体。 本发明化合物，式I的4r-氨基-1t-苯基1c-乙氧基羰基 - 环己烯 - （2）表现出明显的镇痛和精神安定活性，并且可用于缓解和减轻疼痛。
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38.发明授权Method for treating cardiovascular circulatory insufficiencies and hypotonia with 2-hydroxyphenyl-1-oxa-4-azaspiroalkane derivatives 失效用2-羟基苯基-1-氧杂-4-氮杂螺环烷衍生物治疗心血管循环功能不全和低血压的方法
公开(公告)号：US3989836A
公开(公告)日：1976-11-02
申请号：US557134
申请日：1975-03-10
IPC分类号： C07D263/52 , A61K31/42
CPC分类号： C07D263/52
摘要： Novel 2-hydroxy-phenyl-1-oxa-4-azaspiroalkane derivatives, the preparation thereof, and pharmaceutical compositions containing these 2-hydroxyphenyl-1-oxa-4-azaspiroalkane derivatives are disclosed. These derivatives possess unexpectedly valuable thereapeutic properties which make them outstandingly useful for the treatment of cardiovascular circulatory insufficiencies and hypotonic states.
摘要翻译： 公开了新的2-羟基 - 苯基-1-氧杂-4-氮杂螺环烷衍生物，其制备方法和含有这些2-羟基苯基-1-氧杂-4-氮杂螺环烷衍生物的药物组合物。 这些衍生物具有出人意料的有价值的治疗性质，使其在治疗心血管循环功能不全和低渗状态方面非常有用。
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公开(公告)号：US3971794A
公开(公告)日：1976-07-27
申请号：US553715
申请日：1975-02-27
IPC分类号： C07D277/20 , A61K31/425 , A61K31/427 , A61K31/445 , A61K31/4453 , A61P7/10 , C07D277/54 , C07D417/04 , C07D295/12
CPC分类号： C07D417/04 , A61K31/425 , Y10S514/869
摘要： The present invention relates to novel thiazolidinone acetic acid derivatives and their preparation. These derivatives show diuretic properties when used as pharmaceuticals.
摘要翻译： 本发明涉及新型噻唑烷酮乙酸衍生物及其制备方法。 这些衍生物在用作药物时显示利尿特性。
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40.发明授权Method for treating cardiovascular circulatory insufficiencies and hypotonia with 2-hydroxy-phenyl-1-oxa-4-azaspiroalkane derivatives 失效用2-羟基 - 苯基-1-氧杂-4-氮杂螺环烷衍生物治疗心血管循环功能不全和低血压的方法
公开(公告)号：US3931212A
公开(公告)日：1976-01-06
申请号：US484376
申请日：1974-06-28
IPC分类号： C07D263/52 , C07D263/06
CPC分类号： C07D263/52
摘要： 2-Hydroxy-phenyl-1-oxa-4-azaspiroalkane derivatives, the preparation thereof, and pharmaceutical compositions containing these 2-hydroxyphenyl-1-oxa-4-azaspiroalkane derivatives are disclosed. These derivatives possess unexpectedly valuable therapeutic properties which make them outstandingly useful for the treatment of cardiovascular circulatory insufficiencies and hypotonic states.
摘要翻译： 公开了2-羟基 - 苯基-1-氧杂-4-氮杂螺环烷衍生物，其制备方法和含有这些2-羟基苯基-1-氧杂-4-氮杂螺环烷衍生物的药物组合物。 这些衍生物具有意想不到的有价值的治疗性质，使其在治疗心血管循环功能不全和低渗状态方面非常有用。
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