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91. 发明授权

US5036066A Tricyclic pyridine derivatives 失效
标题翻译：三环吡啶衍生物
公开(公告)号：US5036066A
公开(公告)日：1991-07-30
申请号：US422397
申请日：1989-10-16
申请人： Ulf Fischer , Fernand Schneider , Ulrich Widmer
发明人： Ulf Fischer , Fernand Schneider , Ulrich Widmer
IPC分类号： A61K20060101 , A61K31/435 , A61K31/54 , A61K31/55 , A61P21/02 , A61P25/20 , C07D20060101 , C07D205/04 , C07D333/38 , C07D455/02 , C07D455/06 , C07D471/04 , C07D495/04 , C07D495/14 , C07D501/14 , C07D513/04 , C07D513/14 , C07D513/18 , C07D513/22 , C07D519/00
CPC分类号： C07D495/04 , C07D205/04 , C07D333/38 , C07D455/02 , C07D455/06 , C07D495/14 , C07D513/04 , C07D513/14
摘要： The compounds are of the class of bi- and tricyclic pyridone derivatives of the formula ##STR1## wherein the various substituent are as described in the specification, useful in the control of prevention of muscle tensions stress conditions, insomnia, anxiety states and/or convulsions.

92. 发明授权

US4894369A Novel 2.beta.-morpholino-androstane derivatives 失效
标题翻译：新型2β-吗啉代 - 雄甾烷衍生物
公开(公告)号：US4894369A
公开(公告)日：1990-01-16
申请号：US181139
申请日：1988-04-13
申请人： Thomas Sleigh , David S. Savage , Ian C. Carlyle
发明人： Thomas Sleigh , David S. Savage , Ian C. Carlyle
IPC分类号： A61K31/58 , A61K31/565 , A61P21/02 , C07J43/00 , C07J71/00
CPC分类号： C07J43/003 , C07J71/001
摘要： Compounds having the formula: ##STR1## wherein R.sub.1 is H or an optionally substituted acyl group having 1-12 carbon atoms,R.sub.2 is H or an acyl group having 1-12 carbon atoms andR.sub.3 is C, N--CH.sub.3 or a direct bond;and mono- or bisquaternary ammonium compounds thereof and acid addition salts of the non- or mono-quaternary ammonium compounds. Process for the preparation of these compounds. Compositions comprising at least one of the above compounds as the active ingredient. The compounds are favorable neuromuscular blocking agents.

93. 发明授权

US4485112A N-[(Benzofuran-2-yl)(phenyl)methyl]-alkylene diamines useful in treating arrhythmic, histaminic and tussive conditions 失效
标题翻译： N - [（苯并呋喃-2-基）（苯基）甲基] - 亚烷基二胺可用于治疗心律失常，组织和咳嗽状况
公开(公告)号：US4485112A
公开(公告)日：1984-11-27
申请号：US468869
申请日：1983-02-22
申请人： Vittorio Pestellini , Mario Ghelardoni , Carlo Alberto Maggi , Gabrio Roncucci , Alberto Meli
发明人： Vittorio Pestellini , Mario Ghelardoni , Carlo Alberto Maggi , Gabrio Roncucci , Alberto Meli
IPC分类号： A61K31/34 , A61K31/343 , A61K31/443 , A61K31/445 , A61K31/495 , A61K31/535 , A61P3/06 , A61P9/06 , A61P21/02 , A61P25/02 , A61P43/00 , C07D307/80 , C07D307/81 , C07D307/86 , C07D307/92 , C07D405/12
CPC分类号： C07D307/92 , C07D307/80 , C07D307/81 , C07D307/86
摘要： A 2-substituted benzofuran derivative of general formula I or II ##STR1## in which R.sub.1 and R.sub.2, can be the same or different, and are a hydrogen atom, a halogen atom, an alkyl group containing 1 to 4 carbon atoms, an arylalkyl group, an aryl group, a hydroxyl group, an alkoxy group, or an NH.sub.2, NH-alkyl, N(alkyl).sub.2, NH(CO-alkyl), NH(CO-aryl) or NO.sub.2 group, or R.sub.1 and R.sub.2 can together form a ring of 5-8 carbon atoms; R.sub.3 is a hydrogen atom, an alkyl group containing 1 to 4 carbon atoms or an aryl group; R.sub.4 is a hydrogen atom, an alkyl group, an aryl or an arylalkyl group, R.sub.5 is a hydroxyl group, an alkoxy group, an OCO-aryl an OCO-alkyl, OCONH-alkyl or OCONH-aryl group, ##STR2## where n is a number between 1 and 4, R.sub.7 is a hydrogen atom or an alkyl group containing 1 to 4 carbon atoms, and R.sub.8 and R.sub.9, which can be the same or different, represent a hydrogen atom, an alkyl group, an aryl group, an alkoyl group, arylalkoyl group or an aroyl group, or can together form a heterocyclic ring which can contain supplementary heteratoms, and R.sub.6 is a hydrogen or halogen atom, an alkyl group, an arylalkyl group, an aryl group, a hydroxyl group, an alkoxy group, or an NH.sub.2, NH-alkyl, N(alkyl).sub.2, NHCO-alkyl, NHCO-aryl or NO.sub.2 group. The compounds are useful for treating arrhythmic, histaminic and tussive conditions.
摘要翻译：通式I或II的2-取代的苯并呋喃衍生物其中R 1和R 2可以相同或不同，并且是氢原子，卤素原子，烷基含有1至4个碳原子，芳基烷基，芳基，羟基，烷氧基或NH 2，NH-烷基，N（烷基）2，NH（CO-烷基），NH（CO-芳基）或NO 2基团，或者R 1和R 2可以一起形成5-8个碳原子的环; R3是氢原子，含有1至4个碳原子的烷基或芳基; R4是氢原子，烷基，芳基或芳基烷基，R5是羟基，烷氧基，OCO-芳基，OCO-烷基，OCONH-烷基或OCONH-芳基，IMA图像 >其中n是1至4之间的数，R 7是氢原子或含有1至4个碳原子的烷基，并且可以相同或不同的R 8和R 9表示氢原子，烷基，芳基，芳酰基或芳酰基，或者可以一起形成可以含有补充杂原子的杂环，R6是氢或卤素原子，烷基，芳基烷基，芳基，羟基基团，烷氧基或NH 2，NH-烷基，N（烷基）2，NHCO-烷基，NHCO-芳基或NO 2基团。该化合物可用于治疗心律失常，组织和咳嗽状况。

94. 发明授权

US4476061A 2'-(Orthochlorobenzoyl)-4'-chloroglycylanilides 失效
标题翻译： 2' - （邻氯苯甲酰基）-4'-氯草酰苯胺
公开(公告)号：US4476061A
公开(公告)日：1984-10-09
申请号：US409320
申请日：1982-08-18
申请人： Gilbert Mouzin , Henri Cousse , Antoine Stenger
发明人： Gilbert Mouzin , Henri Cousse , Antoine Stenger
IPC分类号： A61K31/165 , A61K31/535 , A61P21/02 , A61P25/18 , A61P25/20 , C07C231/12 , C07C237/04 , C07C237/06 , C07C275/38 , C07D295/15 , C07C103/737
CPC分类号： C07D295/15 , Y10S514/96 , Y10S514/962 , Y10S514/966
摘要： The present invention relates to 2'-(ortho-chlorobenzoyl)-4'-chloroglycylanilides, compositions thereof, and their use as medicaments, e.g., as anxiolytic agents.The compounds of the invention have the general formula I ##STR1## in which R represents hydrogen or alkyl,R.sub.1 and R.sub.2 may be identical or different and are selected from hydrogen, alkyl, hydroxyalkyl, alkenyl, and alkynyl, possibly substituted by alkyl, and cycloalkyl having three to six members, possibly substituted by alkyl, with the proviso that, when one of R.sub.1 and R.sub.2 represents hydrogen, the other is not lower alkyl or hydroxyalkyl; and with the further proviso that R.sub.1 and R.sub.2 may not simultaneously represent either hydrogen or lower-alkyl. R.sub.1 and R.sub.2 may furthermore form, with the nitrogen atom to which they are connected, a nitrogen heterocycle possibly containing a second heteroatom selected from oxygen and nitrogen.
摘要翻译：本发明涉及2' - （邻氯苯甲酰基）-4'-氯草酰苯胺，其组合物及其作为药物的用途，例如作为抗焦虑剂。本发明的化合物具有通式I（I）其中R表示氢或烷基，R 1和R 2可以相同或不同，并且选自氢，烷基，羟基烷基，烯基和炔基，可能被烷基和具有3至6个成员的环烷基，可能被烷基取代，条件是当R 1和R 2之一表示氢时，另一个不是低级烷基或羟烷基; 并且进一步的条件是R 1和R 2可以不同时表示氢或低级烷基。 R1和R2可以与它们所连接的氮原子形成可能含有选自氧和氮的第二杂原子的氮杂环。

95. 发明授权

US4362731A Myotonolytic use of 4,5,6,7-tetrahydroisoxazolo [5,4-c] pyridin-3-ol and derivatives thereof 失效
标题翻译： 4,5,6,7-四氢异恶唑并[5,4-c]吡啶-3-醇及其衍生物的溶栓使用
公开(公告)号：US4362731A
公开(公告)日：1982-12-07
申请号：US296327
申请日：1981-08-26
申请人： Ronald C. Hill
发明人： Ronald C. Hill
IPC分类号： C07D498/04 , A61K31/435 , A61K31/44 , A61P21/02
CPC分类号： A61K31/435
摘要： The myotonolytic use of compounds of formula I ##STR1## wherein R is hydrogen, acetyl or a group of formula IIR'--O--CO-- IIwherein R' is alkyl(C.sub.1-8); phenyl; phenyl substituted in the 4-position with halogen, alkoxy(C.sub.1-4) or alkyl(C.sub.1-4); phenylalkyl; or phenylalkyl in which the phenyl group is substituted in the 4-position with halogen, alkoxy(C.sub.1-4) or alkyl(C.sub.1-4).
摘要翻译：其中R是氢，乙酰基或式II的R'-O-CO-II基团，其中R'是烷基（C1-8）的式I化合物的肌质分解用途。苯基; 在4-位被卤素取代的苯基，烷氧基（C1-4）或烷基（C1-4）; 苯基烷基; 或其中苯基在4-位被卤素，烷氧基（C1-4）或烷基（C1-4）取代的苯基烷基。

96. 发明授权

US4297280A 4,1-Benzoxazepines 失效
标题翻译： 4,1-苯并氧氮杂
公开(公告)号：US4297280A
公开(公告)日：1981-10-27
申请号：US91814
申请日：1979-11-06
申请人： Kentaro Hirai , Shigeru Matsutani , Teruyuki Ishiba , Itsuo Makino
发明人： Kentaro Hirai , Shigeru Matsutani , Teruyuki Ishiba , Itsuo Makino
IPC分类号： A61K31/395 , A61K31/4196 , A61K31/55 , A61K31/553 , A61K31/554 , A61P21/02 , A61P25/00 , A61P25/02 , A61P25/08 , A61P25/20 , A61P25/22 , C07D249/08 , C07D249/10 , C07D267/14 , C07D273/00 , C07D281/10 , C07D285/36 , C07D498/04 , C07D513/04 , C07D521/00
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D249/10 , C07D267/14 , C07D273/00 , C07D285/36 , C07D513/04
摘要： 4,1-Benzoxazepines and thia analogs thereof of the formula: ##STR1## (wherein --A--B-- is the following group: ##STR2## (wherein R.sup.1 is hydrogen, C.sub.1 to C.sub.3 alkyl, or C.sub.7 to C.sub.9 aralkyl;R.sup.2 is C.sub.1 to C.sub.3 alkyl or C.sub.1 to C.sub.3 .alpha.-aminoalkyl;R.sup.3 is C.sub.2 to C.sub.6 dialkylamino;R.sup.4 is C.sub.2 to C.sub.6 dialkylamino or C.sub.5 to C.sub.7 alkylpiperazino;R.sup.5 is C.sub.1 to C.sub.3 alkyl; andQ is oxygen or sulfur);D is oxygen or sulfur;X is halogen or nitro;Y is hydrogen or halogen; andZ is hydrogen, C.sub.1 to C.sub.3 alkoxy, or C.sub.3 to C.sub.9 dialkylaminoalkoxy;with the proviso that when --A--B-- is ##STR3## Z is not hydrogen.) useful as novel central nervous system drugs are prepared by various synthetic routes.
摘要翻译：（其中-AB-是下列基团：其中R 1是氢，C 1至C 3烷基或C 7至C 9芳烷基） ; R2是C1-C3烷基或C1-C3α-氨基烷基; R3是C2-C6二烷基氨基; R4是C2-C6二烷基氨基或C5-C7烷基哌嗪基; R5是C1-C3烷基; Q是氧或硫）; D 是氧或硫; X是卤素或硝基; Y是氢或卤素; Z是氢，C 1至C 3烷氧基或C 3至C 9二烷基氨基烷氧基;条件是当-AB-不是氢时。）作为新型中枢神经系统药物通过各种合成途径制备。

97. 发明授权

US4175079A Benzodiazepine derivatives 失效
标题翻译：苯并二氮杂衍生物
公开(公告)号：US4175079A
公开(公告)日：1979-11-20
申请号：US295575
申请日：1972-10-06
申请人： Yutaka Kuwada , Hideaki Natsugari , Kanji Meguro
发明人： Yutaka Kuwada , Hideaki Natsugari , Kanji Meguro
IPC分类号： A61K31/55 , A61P21/02 , A61P25/08 , A61P25/20 , C07D487/04 , C07D499/62
CPC分类号： C07D487/04 , Y10S514/906 , Y10S514/96
摘要： The present invention relates to pyrimidobenzodiazepine derivatives of the formula (I) and 2-(N-acetoacetal)aminobenzodiazepine derivatives of the formula (II), which compounds have the following formulas: ##STR1## wherein R.sup.1 represents a hydrogen atom or a lower alkyl group, R.sup.2 represents a hydrogen atom, a lower alkyl group or an aryl group, and rings A and/or B are unsubstituted or substituted by one or more of a halogen, nitro, trifluoromethyl, lower alkyl or lower alkoxy group; including the cases wherein the nitrogen atom at the 6-position of the compound (I) or the 4-position of the compound (II) may be in the form of N-oxide and wherein compound (I) may be in the form of a pharmaceutically acceptable acid addition salt thereof. The present invention also relates to a method of producing these compounds. The compounds (I) and (II) are useful as muscle relaxants, anticonvulsants, sedatives, tranquilizers, etc.
摘要翻译：本发明涉及式（I）的嘧啶并二氮杂衍生物和式（II）的2-（N-乙酰乙缩醛）氨基苯并二氮杂衍生物，该化合物具有下式：其中R 1表示氢原子或低级烷基，R2表示氢原子，低级烷基或芳基，并且环A和/或B是未取代的或被一个或多个卤素，硝基，三氟甲基，低级烷基或低级烷氧基取代组; 包括其中化合物（I）的6位的氮原子或化合物（II）的4-位可以是N-氧化物的形式，其中化合物（I）可以是其药学上可接受的酸加成盐。本发明还涉及生产这些化合物的方法。化合物（I）和（II）可用作肌肉松弛剂，抗惊厥药，镇静剂，镇定剂等。

98. 发明授权

US4171306A Diepoxy-androstanes and a process for the preparation thereof 失效
标题翻译：二环氧 - 雄甾烷砜及其制备方法
公开(公告)号：US4171306A
公开(公告)日：1979-10-16
申请号：US762234
申请日：1977-01-25
申请人： Zoltan Tuba , Maria Marsai
发明人： Zoltan Tuba , Maria Marsai
IPC分类号： A61K31/565 , A61P21/02 , C07J1/00 , C07J11/00 , C07J13/00 , C07J31/00 , C07J41/00 , C07J71/00 , C07J21/00
CPC分类号： C07J41/0005 , C07J1/0011 , C07J11/00 , C07J13/005 , C07J31/006 , C07J71/001
摘要： 5.alpha., 17B-Diacetoxy-6 -chloro-2.alpha., 3.alpha.; 16.alpha., 17.alpha.-diepoxy-androstane; 5.alpha., 17B-Dicetoxy-6 -chloro-androsta-2,16-diene; 5.alpha.-Hydroxy-6 -chloro-17-oxo-androst-2-ene or a like intermediate in the production of curare-like compounds is produced by reacting 5.alpha., 6B-dihydroxy-17-oxo-androst-2-ene with an organic sulfonic acid chloride. The obtained 5.alpha.- hydroxy-6B-chloro-17-oxo-androst-2-ene can then be reacted with the enol acetate of a ketone having 3 to 5 carbon atoms to yield 5.alpha., 17B-diacetoxy-6B-chloro-androsta-2,16-diene. The latter is treated to yield the corresponding diepoxide.
摘要翻译： 5α，17B-二乙酰氧基-6-氯-2a，3α; 16α，17α-二环氧 - 雄甾烷; 5α，17B-二甲氧基-6-氯 - 雄甾-2,16-二烯; 通过5α，6B-二羟基-17-氧代 - 雄甾-2-烯的反应制备5α-羟基-6-氯-17-氧代 - 雄甾-2-烯或类似中间物，与有机磺酰氯。然后将所得的5α-羟基-166-氯-17-氧代 - 雄甾-2-烯与具有3至5个碳原子的酮的烯醇乙酸酯反应，得到5α，17B-二乙酰氧基-β- 雄甾-2,16-二烯。处理后者以产生相应的二环氧化物。

99. 发明授权

US4125726A Imidazo[1,5-a][1,4]benzodiazepines 失效
标题翻译：咪唑并[8,1-a {9 {8,4 {9苯并二氮杂卓
公开(公告)号：US4125726A
公开(公告)日：1978-11-14
申请号：US776820
申请日：1977-03-11
申请人： Armin Walser , Rodney I. Fryer , Louis Benjamin
发明人： Armin Walser , Rodney I. Fryer , Louis Benjamin
IPC分类号： A61K31/55 , A61P21/02 , A61P25/20 , A61P25/26 , C07D243/16 , C07D487/04
CPC分类号： C07D487/04 , C07D243/16
摘要： Compounds are disclosed of the formula ##STR1## wherein R.sub.1 is hydrogen, halogen or trifluoromethyl; R.sub.2 is selected from the group consisting of lower alkylthio together with the sulfoxide and sulfone thereof, halo, lower alkylamino or lower alkoxy; Y is oxo or thio; R.sub.3 is selected from the group consisting of hydrogen, --COOR.sub.4 wherein R.sub.4 is hydrogen or lower alkyl, --CONR.sub.6 R.sub.5 wherein R.sub.5 and R.sub.6 are hydrogen or lower alkyl; X is hydrogen or halogen; and R.sub.7 is lower alkyl or hydrogen and the pharmaceutically acceptable salts and N-oxides thereof.Also presented are processes to produce the above compounds and intermediates therefor and derivatives thereof.
摘要翻译：公开了化学式为“IMAGE”和“IMAGE”，其中R 1是氢，卤素或三氟甲基; R2选自低级烷硫基及其亚砜和砜，卤素，低级烷基氨基或低级烷氧基; Y是氧代或硫代; R 3选自氢，-COOR 4，其中R 4是氢或低级烷基，-CONR 6 R 5，其中R 5和R 6是氢或低级烷基; X是氢或卤素; 并且R 7为低级烷基或氢及其药学上可接受的盐和N-氧化物。

100. 发明授权

US4111931A 1,2,3,5-Tetrahydro-4H-1,5-benzodiazepine-4-ones 失效
标题翻译： 1,2,3,5-四氢-4H- 1,5-BENZODIAZEPINE-4-ONES
公开(公告)号：US4111931A
公开(公告)日：1978-09-05
申请号：US874074
申请日：1978-02-01
申请人： Armin Walser , Rodney Ian Fryer
发明人： Armin Walser , Rodney Ian Fryer
IPC分类号： A61K31/55 , A61P21/02 , A61P25/20 , C07D243/12 , C07D487/04
CPC分类号： C07D487/04 , C07D243/12 , Y10S514/906
摘要： The present invention concerns compounds of the formula ##STR1## wherein X is hydrogen or halogen; R.sub.1 is hydrogen, halogen or trifluoromethyl; R.sub.2 is hydrogen or lower alkyl; and R.sub.3 is hydrogen, --COO lower alkyl or CON(R.sub.4).sub.2 wherein R.sub.2 is lower alkyl or hydrogen and may be differentand the pharmaceutically acceptable salts thereof.Also provided are methods for the preparation of these compounds as well as pharmaceutical formulations which contain the active compounds of this invention. The compounds of the formula illustrated above are useful as anxiolytics, anticonvulsants, muscle relaxants and sedative agents.

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