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91. 发明授权

US5773646A Meta-substituted phenylene derivatives 失效
标题翻译：元取代亚苯衍生物
公开(公告)号：US5773646A
公开(公告)日：1998-06-30
申请号：US825086
申请日：1997-03-27
申请人： Nizal Chandrakumar , Barbara B. Chen , Helen Y. Chen , Michael Clare , Alan F. Gasiecki , Richard A. Haack , James W. Malecha , Peter G. Ruminski , Mark A. Russell
发明人： Nizal Chandrakumar , Barbara B. Chen , Helen Y. Chen , Michael Clare , Alan F. Gasiecki , Richard A. Haack , James W. Malecha , Peter G. Ruminski , Mark A. Russell
IPC分类号： A61K31/00 , A61K31/195 , A61K31/196 , A61K31/215 , A61K31/216 , A61K31/415 , A61K31/4164 , A61K31/4168 , A61K31/4184 , A61K31/496 , A61K31/505 , A61P1/00 , A61P1/02 , A61P19/00 , A61P19/08 , A61P19/10 , A61P27/00 , A61P27/02 , A61P35/00 , A61P43/00 , C07C45/67 , C07C49/796 , C07C205/35 , C07C205/45 , C07C205/56 , C07C205/57 , C07C257/16 , C07C257/18 , C07C259/18 , C07C275/42 , C07C279/18 , C07C279/24 , C07C279/28 , C07C311/46 , C07C311/47 , C07C317/42 , C07C317/44 , C07C323/44 , C07C323/56 , C07C335/16 , C07C335/22 , C07C335/32 , C07D223/06 , C07D233/50 , C07D233/88 , C07D235/30 , C07D239/14 , C07D311/18 , C07D311/20 , C07D405/12 , C07C241/00 , C07C205/00 , C07C229/00 , C07C321/00
CPC分类号： C07C45/673 , C07C205/35 , C07C205/45 , C07C205/56 , C07C205/57 , C07C257/16 , C07C259/18 , C07C275/42 , C07C279/18 , C07C279/24 , C07C279/28 , C07C311/46 , C07C311/47 , C07C317/42 , C07C323/44 , C07C335/16 , C07C335/22 , C07C335/32 , C07C49/796 , C07D223/06 , C07D233/50 , C07D233/88 , C07D235/30 , C07D239/14 , C07D311/18 , C07D311/20 , C07D405/12
摘要： The present invention relates to a class of compounds represented by the Formula I ##STR1## or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the .alpha..sub.v .beta..sub.3 integrin.
摘要翻译：本发明涉及一类由式I表示的化合物或其药学上可接受的盐，包含式I化合物的药物组合物和选择性抑制或拮抗αvβ3整联蛋白的方法。

92. 发明授权

US5710149A Piperazine derivatives as 5-ht antagonists 失效
标题翻译：哌嗪衍生物作为5-ht拮抗剂
公开(公告)号：US5710149A
公开(公告)日：1998-01-20
申请号：US731953
申请日：1996-10-23
申请人： Ian Anthony Cliffe
发明人： Ian Anthony Cliffe
IPC分类号： A61K31/335 , A61K31/34 , A61K31/343 , A61K31/35 , A61K31/352 , A61K31/353 , A61K31/357 , A61K31/39 , A61K31/535 , A61K31/538 , A61K31/55 , A61P9/12 , A61P13/02 , A61P15/00 , A61P25/00 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07D265/36 , C07D295/10 , C07D307/79 , C07D311/08 , C07D311/20 , C07D311/22 , C07D311/58 , C07D317/46 , C07D317/66 , C07D319/18 , C07D319/20 , C07D321/10 , C07D327/06 , C07D405/02 , C07D405/04 , C07D411/02 , C07D413/02 , A61K31/495 , C07D405/10 , C07D405/14
CPC分类号： C07D319/18
摘要： This invention concerns compounds of formula (I) ##STR1## where A is a C.sub.1 or C.sub.2 alkylene chain optionally substituted by lower alkyl; Z is a bicyclic oxygen-containing aryl radical (e.g. 2,3-dihydro-1,4-benzodioxin-5-yl); R is hydrogen or lower alkyl; R.sup.1 is aryl or aryl(lower)alkyl; R.sup.2 is hydrogen or lower alkyl; and R.sup.3 is hydrogen, an alkyl group of 1 to 10 carbon atoms, cycloalkyl of 3 to 12 carbon atoms; cycloalkyl(lower)alkyl, aryl or aryl(lower)alkyl or R.sup.2 and R.sup.3 together with the nitrogen atom to which they are both attached represent a saturated heterocyclic ring which may contain a further hetero atom, and the pharmaceutically acceptable acid addition salts thereof. The compounds are 5-HT.sub.1A -antagonists which may be used, for example, in treating anxiety.
摘要翻译：本发明涉及式（I）的化合物：其中A是任选被低级烷基取代的C1或C2亚烷基链; Z是双环含氧芳基（例如2,3-二氢-1,4-苯并二恶英-5-基）; R是氢或低级烷基; R1是芳基或芳基（低级）烷基; R2是氢或低级烷基; R3为氢，碳原子数为1〜10的烷基，碳原子数为3〜12的环烷基，环烷基（低级）烷基，芳基或芳基（低级）烷基或R 2和R 3与它们所连接的氮原子一起表示可含有另外的杂原子的饱和杂环及其药学上可接受的酸加成盐。该化合物是可用于例如治疗焦虑症的5-HT 1A拮抗剂。

93. 发明授权

US5580990A Pt-containing compound, process for its preparation, and application of such compounds 失效
标题翻译：含Pt化合物，其制备方法和这些化合物的应用
公开(公告)号：US5580990A
公开(公告)日：1996-12-03
申请号：US975586
申请日：1993-10-29
申请人： Franciscus M. van den Berg , Edwin L. M. Lempers , Marieke J. Bloemink , Jan Reedijk
发明人： Franciscus M. van den Berg , Edwin L. M. Lempers , Marieke J. Bloemink , Jan Reedijk
IPC分类号： G01N33/53 , C07F15/00 , C07H21/00 , C07H23/00 , C07J51/00 , C09B11/04 , C12N15/09 , C12Q1/68 , G01N33/532 , G01N33/533 , G01N33/566 , G01N33/58 , C07D311/20 , C12Q1/70
CPC分类号： C09B11/04 , C07F15/0093 , C07J51/00 , C12Q1/6816
摘要： Pt-containing compound with the formula {Pt.sup.II (w)(x)(y)(z)} or {Pt.sup.IV (u)(v)(w)(x)(y)(z)}, wherein u, v, w, x, y and z represent whether or not the same whether or not interconnected ligands, of which at least one is a leaving ligand and at least one of the remaining ligands represents a detectable marker group. According to the invention (CH.sub.3).sub.2 SO, Cl or H.sub.2 O appears to be suitable as a leaving ligand while as detectable marker group a fluorescent group merits preference and is the ligand fluorescein or tetramethyl rhodamine. A suitable Pt-containing compounds is {Pt(ethylenediamine)(Me.sub.2 SO)(fluorescein-NH(CS)-NHCH.sub.3)} (PtF). Further, the invention comprises a process for the preparation of the Pt-containing compounds, where the Pt-containing compounds are prepared in a manner known per se for analogous compounds.
摘要翻译： PCT No.PCT / NL91 / 00126 Sec。 371日期：1993年10月29日 102（e）日期1993年10月29日PCT 1991年7月16日PCT公布。第WO92 / 01699号公报日期：1992年6月2日具有式{PtII（w）（x）（y）（z）}或{PtIV（u）（v）（w）（x）（y）（z）}的含Pt的化合物，其中u，v，w，x，y和z表示是否相互连接的配体（其中至少一个是离去配体）和至少一个剩余配体是否表示可检测标记基团是否相同。根据本发明（CH 3）2 SO，Cl或H 2 O似乎适合作为离去配体，而作为可检测的标记基团，荧光基团优先选择并且是配体荧光素或四甲基罗丹明。合适的含Pt化合物是{Pt（乙二胺）（Me 2 SO）（荧光素-NH（CS）-NHCH 3）}（PtF）。此外，本发明包括制备含Pt化合物的方法，其中以本身已知的类似化合物制备含Pt化合物。

94. 发明授权

US5545646A 4-bicyclically substituted dihydropyridines and their use in medicaments 失效
标题翻译： 4-双环取代的二氢吡啶类及其在药物中的用途
公开(公告)号：US5545646A
公开(公告)日：1996-08-13
申请号：US261585
申请日：1994-06-17
申请人： Alexander Straub , Siegfried Goldmann , J urgen Stoltefuss , Martin Bechem , Klaus Dembowsky , Rainer Gross , Siegbert Hebisch , Joachim H utter , Howard-Paul Rounding
发明人： Alexander Straub , Siegfried Goldmann , J urgen Stoltefuss , Martin Bechem , Klaus Dembowsky , Rainer Gross , Siegbert Hebisch , Joachim H utter , Howard-Paul Rounding
IPC分类号： A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/455 , A61K31/495 , A61P9/08 , A61P9/10 , C07C45/71 , C07C45/74 , C07C47/546 , C07C47/575 , C07C49/835 , C07C323/09 , C07C323/62 , C07D209/08 , C07D209/44 , C07D209/48 , C07D211/84 , C07D211/90 , C07D215/14 , C07D241/42 , C07D241/48 , C07D307/79 , C07D311/04 , C07D311/08 , C07D311/18 , C07D311/20 , C07D311/22 , C07D311/32 , C07D311/42 , C07D311/58 , C07D311/76 , C07D333/54 , C07D333/62 , C07D335/06 , C07D401/04 , C07D405/04 , C07D409/04 , C07D471/04 , C07D491/04 , C07D491/048 , C07D495/04 , C07D519/00 , C07F9/24
CPC分类号： C07D307/79 , C07C323/62 , C07C45/71 , C07C45/74 , C07C47/575 , C07C49/835 , C07D209/48 , C07D211/90 , C07D215/14 , C07D241/48 , C07D311/18 , C07D311/32 , C07D311/58 , C07D311/76 , C07D333/54 , C07D333/62 , C07D335/06 , C07D401/04 , C07D405/04 , C07D409/04 , C07D471/04 , C07D491/04 , C07D495/04 , C07F9/242
摘要： The invention relates to new 4-bicyclically substituted dihydropyridines of the general formula (I) ##STR1## in which R.sub.1 to R.sub.5 have the meaning given in the description, processes for their preparation and their use in medicaments, in particular in agents for the treatment of cardiovascular diseases.
摘要翻译：本发明涉及在描述中给出的通式（I）的新的4-双环取代的二氢吡啶，其制备方法及其在药物中的用途，特别是用于治疗心血管疾病的药剂。

95. 发明授权

US5399561A Acetylenes disubstituted with a phenyl or heteroaryl group and a 2-oxochromanyl, 2-oxothiochromanyl or 2-oxo-1,2,3,4-tetrahydro-quinolinyl group having retinoid-like biological activity 失效
标题翻译：具有类视黄醇样生物活性的苯基或杂芳基和2-氧代氧杂苯并二氢吡喃基或2-氧代-1,2,3,4-四氢 - 喹啉基二取代的乙炔
公开(公告)号：US5399561A
公开(公告)日：1995-03-21
申请号：US178714
申请日：1994-01-07
申请人： Roshantha A. Chandraratna
发明人： Roshantha A. Chandraratna
IPC分类号： A61K31/35 , A61K31/352 , A61K31/443 , A61K31/455 , A61K31/47 , A61K31/695 , A61P3/06 , A61P9/10 , A61P13/02 , A61P15/00 , A61P17/00 , A61P35/00 , C07D215/22 , C07D215/227 , C07D311/18 , C07D311/20 , C07D311/58 , C07D335/06 , C07D401/06 , C07D405/06 , C07D409/06 , C07F7/08 , A61K31/165 , A61K31/38
CPC分类号： C07D215/227 , C07D311/20 , C07D311/58 , C07D335/06 , C07D401/06 , C07D405/06 , C07D409/06 , C07F7/0812
摘要： Compounds of the formula ##STR1## where R.sub.1 and R.sub.2 are hydrogen, lower alkyl of 1-6 carbons, or halogen; R.sub.3 is hydrogen, lower alkyl of 1-6 carbons, halogen, OR.sub.11, SR.sub.11, OCOR.sub.11, SCOR.sub.11, NH.sub.2, NHR.sub.11, N(R.sub.11).sub.2, NHCOR.sub.11 or NR.sub.11 COR.sub.11 ; X is O, S or NR' where R' is hydrogen or lower alkyl of 1-6 carbons; Y is phenyl or a heteroaryl group selected from a group consisting of pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl and oxazolyl; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub. 12).sub.2, or CR.sub.7 OR.sub.13 O, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R.sub.11 is lower alkyl, phenyl or lower alkylphenyl, R.sub.12 is lower alkyl, and R.sub.13 is divalent alkyl radical of 2-5 carbons, have retinoid-like biological activity.
摘要翻译：其中R1和R2是氢，1-6个碳的低级烷基或卤素的式“IMAGE”的化合物; R3是氢，1-6个碳的低级烷基，卤素，OR11，SR11，OCOR11，SCOR11，NH2，NHR11，N（R11）2，NHCOR11或NR11COR11; X是O，S或NR'，其中R'是氢或1-6个碳的低级烷基; Y是苯基或选自吡啶基，噻吩基，呋喃基，哒嗪基，嘧啶基，吡嗪基，噻唑基和恶唑基的杂芳基; A是（CH 2）n，其中n是0-5，具有3-6个碳的低级支链烷基，具有3-6个碳的环烷基，具有2-6个碳的烯基和1或2个双键，具有2-6个碳原子的炔基和 1或2个三键; B是氢，COOH或其药学上可接受的盐，COOR8，CONR9R10，-CH2OH，CH2OR11，CH2OCOR11，CHO，CH（OR12）2，CHOR13O，-COR7，CR7（OR12）2或CR7OR13O，其中R7是含有1至5个碳的烷基，环烷基或链烯基，R 8为碳原子数为1至10的烷基或碳原子数为5至10的环烷基，或R 8为苯基或低级烷基苯基，R 9和R 10独立地为氢，苯基或低级烷基苯基，R11为低级烷基，苯基或低级烷基苯基，R12为低级烷基，R13为2-5个碳原子的二价烷基，具有类视黄醇样生物活性。

96. 发明授权

US5296492A Certain chroman derivatives useful for treating symptoms caused by contraction of smooth muscles, circulatory diseases or epilepsy 失效
标题翻译：某些苯并二氢吡喃衍生物可用于治疗由平滑肌，循环系统疾病或癫痫的收缩引起的症状
公开(公告)号：US5296492A
公开(公告)日：1994-03-22
申请号：US893403
申请日：1992-06-03
申请人： Akira Shiozawa , Atsuro Inubushi , Kazuhisa Narita , Yukihiro Sagawa , Makoto Hosono , Masashi Iida
发明人： Akira Shiozawa , Atsuro Inubushi , Kazuhisa Narita , Yukihiro Sagawa , Makoto Hosono , Masashi Iida
IPC分类号： A61K31/35 , A61K31/353 , A61K31/44 , A61K31/4433 , A61P9/00 , A61P21/00 , C07D213/50 , C07D213/64 , C07D311/20 , C07D311/68 , C07D405/04 , C07F7/18 , C07D407/04 , C07F7/02 , A61K31/695
CPC分类号： C07D405/04 , C07F7/1856
摘要： A chroman derivative represented by the following general formula [1]: ##STR1## wherein R.sub.1 represents cyano group, nitro group, halogenomethyl group or --SO.sub.2 --X group (X represents lower alkyl group having 1-6 carbon atoms or aryl group); R.sub.2 represents hydrogen atom or OA group (A represents hydrogen atom, nitro group, lower acyl group having 1-6 carbon atoms, arylcarbonyl group, lower alkylsulfonyl group having 1-6 carbon atoms, arylsulfonyl group, arylalkyl group, tetrahydropyranyl group, lower alkoxycarbonyl group having 1-6 carbon atoms, arylalkoxycarbonyl group or silyl derivative group); R.sub.3 singly represents a hydrogen atom; or R.sub.3 forms a bond jointly with R.sub.2 ; and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 each represent hydrogen atom, vinyl group, formyl group, --Y--(OA).sub.n group (Y represents straight or branched chain alkylene group having 1-6 carbon atoms or lower alkenyl group having 1-6 carbon atoms, A is as defined above, and n represents an integer of 1-3.The compound of this invention is expected to be effectively usable as an agent for treatment of various symptoms due to the contraction of smooth muscles, for treatment of the diseases of the circulatory system and for treatment of epilepsy.
摘要翻译：由下列通式（1）表示的苯并二氢吡喃衍生物：（*化学结构*）（1）其中R1表示氰基，硝基，卤代甲基或-SO2-X基（X表示具有1-6个碳原子的低级烷基原子或芳基）; R2表示氢原子或OA基（A表示氢原子，硝基，具有1-6个碳原子的低级酰基，芳基羰基，具有1-6个碳原子的低级烷基磺酰基，芳基磺酰基，芳基烷基，四氢吡喃基，低级烷氧基羰基具有1-6个碳原子的基团，芳基烷氧基羰基或甲硅烷基衍生物基团）; R3单独表示氢原子; 或R3与R2一起形成键; 和R 4，R 5，R 6和R 7各自表示氢原子，乙烯基，甲酰基，-Y-（OA）n基（Y表示具有1-6个碳原子的直链或支链亚烷基或具有1-6个碳原子的低级链烯基碳原子，A如上所定义，n表示1-3的整数。预期本发明化合物可有效地用作治疗由于平滑肌收缩引起的各种症状的药剂，用于治疗循环系统疾病和治疗癫痫。

97. 发明授权

US5280323A Development apparatus employing magnetic field shapers 失效
标题翻译：采用磁场成形机的显影装置
公开(公告)号：US5280323A
公开(公告)日：1994-01-18
申请号：US814171
申请日：1991-12-30
申请人： Jorge A. Alvarez , Gary A. Denton , Peter J. McGuire , Francisco Zirilli
发明人： Jorge A. Alvarez , Gary A. Denton , Peter J. McGuire , Francisco Zirilli
IPC分类号： A61K20060101 , C07C20060101 , C07C57/50 , C07D307/83 , C07D311/20 , C07D311/22 , C07D311/24 , C07D311/74 , C07D311/76 , C07D405/12 , C07D407/12 , G03G15/09
CPC分类号： C07C57/50 , C07D307/83 , C07D311/22 , C07D311/24 , C07D311/76 , C07D405/12 , C07D407/12
摘要： An electrophotographic printing machine in which an electrostatic latent image is recorded on a photoconductive surface by charging the appropriate areas of the surface to predetermined polarities. The latent image is a developed with toners of a preselected color and predetermined polarity by a developer unit. The developer unit includes a bead removal device which magnetically attracts carrier beads off the photoconductive surface and deposits these beads in a sump or reservoir of developer. The bead removal device includes a magnet and magnetic field shapers to enhance the magnetic fields which attract the beads in the zone between the surface and the bead removal device and attenuates the magnetic fields in the zone between the bead removal device and the sump or reservoir to reduce the attraction between the beads and the bead removal device in this zone. The invention also provides magnetic brush rollers for the delivery of toner to the photoconductive surface which have magnetic field shapers which attenuate the magnetic fields to encourage bead release from the roller and reduce attraction of beads to the roller in reverse rotation of the roller.
摘要翻译：一种电子照相印刷机，其中通过将表面的适当区域充电至预定极性，将静电潜像记录在光电导表面上。潜像是用显影剂单元开发出的具有预选颜色和预定极性的调色剂。显影剂单元包括珠粒去除装置，其磁吸引载体珠子离开光电导表面并将这些珠子沉积在显影剂的贮槽或贮存器中。珠去除装置包括磁体和磁场成形器，以增强吸引表面和珠粒移除装置之间的区域中的珠粒的磁场，并且使珠粒移除装置和贮槽或储存器之间的区域中的磁场衰减减少该区域中的珠粒和珠粒去除装置之间的吸引力。本发明还提供了用于将调色剂输送到光电导表面的磁刷辊，其具有磁场成形器，该磁场成形器使磁场衰减，以促进从滚筒释放珠子，并减少滚珠反向滚动时珠子对辊的吸引。

98. 发明授权

US5237075A Process for producing 3,4-dihydrocoumarin derivatives 失效
标题翻译： 3,4-二氢香豆素衍生物的制备方法
公开(公告)号：US5237075A
公开(公告)日：1993-08-17
申请号：US839285
申请日：1992-02-24
申请人： Tamio Shirafuji , Kiyomi Sakai , Kensen Okusako , Itaru Kawata , Yasumoto Simazu , Tetuya Suzuta
发明人： Tamio Shirafuji , Kiyomi Sakai , Kensen Okusako , Itaru Kawata , Yasumoto Simazu , Tetuya Suzuta
IPC分类号： C07D311/10 , C07D311/20
CPC分类号： C07D311/10 , C07D311/20
摘要： A process for producing a 3,4-dihydrocoumarin compound represented by formula (II): ##STR1## wherein R.sub.1 to R.sub.4 are as defined in the specification, comprising the steps of:(1) heating a 3-(2-cyclohexanoyl)propionic acid ester compound represented by formula (I): ##STR2## wherein R.sub.1 R.sub.5 are as defined in the specification, in the presence of at least one solid metal catalyst, thereby to allow said compound of formula (I) to undergo ring formation and dehydrogenation to yield said 3,4-dihydrocoumarin compound of formula (II) and, as a by-product, a coumarin compound represented by formula (III): ##STR3## wherein R.sub.1 to R.sub.4 are as defined above; (2) adding a catalyst which is as defined above to said reaction mixture, or bringing said reaction mixture into contact with oxygen to activate said catalyst used in said ring formation and dehydrogenation, without separating said coumarin compound from the reaction mixture that has undergone said ring formation and dehydrogenation; and(3) partially hydrogenating said by-product coumarin compound in said reaction mixture with hydrogen so as to convert said coumarin compound to a 3,4-dihydrocoumarin compound.
摘要翻译：制备由式（II）表示的3,4-二氢香豆素化合物的方法：其中R 1至R 4如说明书中所定义，其包括以下步骤：（1）加热3-（2- 环己酰基）丙酸酯化合物：其中R1 R5如说明书中所定义，在至少一种固体金属催化剂存在下，从而使所述式（I）化合物与式进行环形成和脱氢，得到式（II）的3,4-二氢香豆素化合物，作为副产物，由式（III）表示的香豆素化合物：其中R 1至R 4为以上定义（2）向所述反应混合物中加入如上定义的催化剂，或使所述反应混合物与氧接触以活化所述环形成和脱氢中使用的所述催化剂，而不将所述香豆素化合物与已经经历所述反应混合物的反应混合物分离环形成和脱氢; 和（3）用氢将所述反应混合物中的所述副产物香豆素化合物部分氢化，以将所述香豆素化合物转化为3,4-二氢香豆素化合物。

99. 发明授权

US5192799A Coumaran group containing amine compounds and their acid addition salts and quaternary ammonium salts and the use thereof as anti arrhythmic agents and as psychotropic agents 失效
标题翻译：含有胺化合物的香豆素基团及其酸加成盐和季铵盐及其作为抗心律失常剂和作为精神药物的用途
公开(公告)号：US5192799A
公开(公告)日：1993-03-09
申请号：US895417
申请日：1992-06-05
申请人： Ikuo Tomino , Masaharu Ishiguro , Takumi Kitahara , Keiichi Yokoyama , Noriaki Kihara , Joji Kamiya , Kanji Yoshihara , Masaaki Ishii , Akira Mizuchi , Kazutoshi Horikomi , Akira Awaya , Takuo Nakano
发明人： Ikuo Tomino , Masaharu Ishiguro , Takumi Kitahara , Keiichi Yokoyama , Noriaki Kihara , Joji Kamiya , Kanji Yoshihara , Masaaki Ishii , Akira Mizuchi , Kazutoshi Horikomi , Akira Awaya , Takuo Nakano
IPC分类号： A61K31/34 , A61K31/35 , C07C217/18 , C07C217/22 , C07C217/32 , C07D209/08 , C07D209/48 , C07D211/14 , C07D215/04 , C07D217/02 , C07D217/24 , C07D235/06 , C07D265/36 , C07D307/78 , C07D307/79 , C07D307/80 , C07D307/83 , C07D307/86 , C07D307/91 , C07D311/04 , C07D311/08 , C07D311/14 , C07D311/16 , C07D311/18 , C07D311/20 , C07D311/22 , C07D311/24 , C07D311/58 , C07D311/74 , C07D317/06 , C07D317/46 , C07D317/48 , C07D327/04 , C07D401/12 , C07D405/12 , C07D407/12 , C07D471/10 , C07D487/04 , C07D487/22 , C07D491/10
CPC分类号： C07D209/48 , C07C217/18 , C07C217/22 , C07C217/32 , C07D209/08 , C07D211/14 , C07D215/04 , C07D217/02 , C07D217/24 , C07D235/06 , C07D265/36 , C07D307/78 , C07D307/79 , C07D307/80 , C07D307/83 , C07D307/86 , C07D307/91 , C07D311/04 , C07D311/14 , C07D311/16 , C07D311/18 , C07D311/20 , C07D311/22 , C07D311/24 , C07D311/58 , C07D317/46 , C07D317/48 , C07D327/04 , C07D401/12 , C07D405/12 , C07D407/12 , C07D471/10 , C07D487/04 , C07D491/10 , C07C2102/08
摘要： Amine represented by the following formula (1), or their acid addition salts or their quaternary ammonium salts. ##STR1## The amines of formula (1) or their pharmaceutically acceptable acid addition salts or quaternary ammonium salts are useful for the treatment and prevention of heart diseases of animals, particularly arrhythima, myocardial infarction, angina pectoris and heart failure and psychoneurological diseases.
摘要翻译：由下式（1）表示的胺或其酸加成盐或其季铵盐。（1）式（1）的胺或其药学上可接受的酸加成盐或季铵盐可用于治疗和预防动物的心脏病，特别是心律不齐，心肌梗塞，心绞痛和心力衰竭以及心理学疾病

100. 发明授权

US5162546A Acetylenes disubstituted with a phenyl group and a 2-substituted chromanyl, thiochromanyl or 1,2,3,4-tetrahydroquinolinyl group having retinoid-like activity 失效
标题翻译：与苯基和2-取代的CHROMANYL，噻喃酮或具有类似活性的1,2,3,4-四氢喹啉啉类分离的乙酰胺
公开(公告)号：US5162546A
公开(公告)日：1992-11-10
申请号：US749747
申请日：1991-08-26
申请人： Roshantha A. S. Chandraratna
发明人： Roshantha A. S. Chandraratna
IPC分类号： C07D311/14 , C07D311/16 , C07D311/58 , C07D335/06 , C07D311/20
CPC分类号： C07D335/06 , C07D311/14 , C07D311/16 , C07D311/58
摘要： Retinold-like activity is exhibited by compounds of the formula ##STR1## where X is S, O; R.sub.1, R.sub.2 and R.sub.3 are hydrogen or lower alkyl; R.sub.4 and R.sub.5 are hydrogen or lower alkyl with the proviso that R.sub.4 and R.sub.5 cannot both be hydrogen, R.sub.6 is hydrogen, lower alkyl, lower alkenyl, lower cycloalkyl or halogen; n is 0-5, and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR.sub.1 or a ketal derivative where R.sub.1 l is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4, or a pharmaceutically acceptable salt thereof.
摘要翻译：视黄醇样活性由下式化合物显示：其中X为S，O; R1，R2和R3是氢或低级烷基; R4和R5是氢或低级烷基，条件是R4和R5不能都是氢，R6是氢，低级烷基，低级烯基，低级环烷基或卤素; n为0-5，B为H，-COOH或其药学上可接受的盐，酯或酰胺，-CH 2 OH或醚或酯衍生物，或-CHO或缩醛衍生物，或-COR1或缩酮衍生物，其中R1 l是 - （CH 2）m CH 3，其中m是0-4，或其药学上可接受的盐。

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