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101. 发明授权

US4645838A Pyrazolopyridine compounds, and intermediates, useful as anxiolytic agents 失效
标题翻译：吡唑并吡啶化合物和中间体，可用作抗焦虑剂
公开(公告)号：US4645838A
公开(公告)日：1987-02-24
申请号：US624530
申请日：1984-06-25
申请人： Thomas M. Bare , Anthony F. Heald
发明人： Thomas M. Bare , Anthony F. Heald
IPC分类号： C07C51/09 , C07C53/21 , C07D207/38 , C07D231/38 , C07D401/12 , C07D403/12 , C07D471/04 , C07D471/14 , C07D491/14 , C07D491/147 , C07D491/22
CPC分类号： C07D231/38 , C07C51/09 , C07C53/21 , C07D207/38 , C07D401/12 , C07D403/12 , C07D471/04 , C07D471/14 , C07D491/14
摘要： Compounds of the formula (I): ##STR1## wherein R.sup.1, R.sup.3, R.sup.4, R.sup.7 and R.sup.8 are as described herein, D is oxygen, n is 1 or 2 and the physiologically acceptable salts thereof useful in reducing anxiety in an animal such as man. The compounds are potent anxiolytics having reduced side effects compared to known anxiolytics. Also pharmaceutical compositions, intermediates and methods of treatment and synthesis are described.

102. 发明授权

US4482556A Pyrimido (6,1-a)isoquinolin-4-one derivatives 失效
标题翻译：嘧啶（6,1-a）异喹啉-4-酮衍生物
公开(公告)号：US4482556A
公开(公告)日：1984-11-13
申请号：US134080
申请日：1980-03-26
申请人： Bansi Lal , Horst Dornauer , Bani K. Bhattacharya , Alihussein N. Dohadwalla , Noel J. de Souza
发明人： Bansi Lal , Horst Dornauer , Bani K. Bhattacharya , Alihussein N. Dohadwalla , Noel J. de Souza
IPC分类号： A61K31/505 , A61K31/535 , A61P9/12 , A61P11/08 , A61P37/08 , C07D217/14 , C07D471/04 , C07D491/14 , C07D491/147 , C07F9/60 , C07F9/6509 , C07F9/6561
CPC分类号： C07D471/04 , C07D217/14 , C07D491/14 , C07F9/650911 , C07F9/6561
摘要： What are disclosed are pyrimido (6,1-a)isoquinolin-4-one compounds useful as hypotensive agents, bronchodilators, and anti-allergenics, intermediates useful in their preparation, and methods for making the compounds and intermediates.
摘要翻译：公开的是嘧啶（6,1-a）异喹啉-4-酮化合物，其可用作降压剂，支气管扩张剂和抗过敏原，可用于其制备的中间体，以及制备化合物和中间体的方法。

103. 发明授权

US4465691A (3,4';4,5)-Pyrido (3,2-g)-furo coumarins or (3,4-h) pyrido psoralens process of preparation, applications in cosmetology and in therapeutics, and cosmetological and pharmaceutical compositions with them 失效
标题翻译：（3,4'; 4,5） - 吡啶（3,2-g） - 呋喃香豆素或（3,4-h）吡啶补骨脂素的制备方法，在美容和治疗中的应用，以及它们的美容和药物组合物
公开(公告)号：US4465691A
公开(公告)日：1984-08-14
申请号：US469454
申请日：1983-02-24
申请人： Emile Bisagni , Jacqueline Morin , Dietrich Averbeck , Dubertret Louis
发明人： Emile Bisagni , Jacqueline Morin , Dietrich Averbeck , Dubertret Louis
IPC分类号： A61K8/49 , A61P17/00 , A61P29/00 , A61P37/08 , C07D213/68 , C07D213/73 , C07D405/12 , C07D487/16 , C07D491/04 , C07D491/14 , C07D491/153 , A61K31/435
CPC分类号： C07D213/73 , C07D213/68 , C07D405/12 , C07D491/04 , C07D491/14
摘要： Pyrido (3,4', 4,5) furo (3,2-g) coumarins or pyrido (3,4-h) psoralens having formula I ##STR1## wherein R is a hydrogen radical or a lower alkyl group having from 1 to 4 carbon atoms and R" is a methyl group or a methoxy group. These compounds are photobiologically active and are useful or medicinals and pharmaceutical compositions in association with ultraviolet radiation for treating skin diseases and as cosmetic compositions for skin pigmentation.
摘要翻译：吡啶（3,4'，4,5）呋喃（3,2-g）香豆素或吡啶并（3,4-h）补骨脂素，其具有式I的化合物，其中R是氢原子或具有1 至4个碳原子，R“为甲基或甲氧基。这些化合物是光生物活性的，并且是有用的或与用于治疗皮肤疾病的紫外线辐射有关的药物和药物组合物以及用于皮肤色素沉着的化妆品组合物。

104. 发明授权

US4400506A Processes for the manufacture of pyrimido[6,1-a]isoquinolinones 失效
标题翻译：制备嘧啶并[6,1-a]异喹啉酮的方法
公开(公告)号：US4400506A
公开(公告)日：1983-08-23
申请号：US314994
申请日：1981-10-26
申请人： Bansi Lal , Adolf D'Sa , Horst Dornauer , Noel J. de Souza
发明人： Bansi Lal , Adolf D'Sa , Horst Dornauer , Noel J. de Souza
IPC分类号： A61K31/505 , A61P9/12 , A61P11/08 , A61P37/08 , C07D471/04 , C07D491/14 , C07D491/147 , C07F9/6561
CPC分类号： C07D471/04 , C07D491/14 , C07F9/6561
摘要： What are disclosed are compounds of the formula ##STR1## wherein, X is oxygen, sulfur, or halogen, useful as intermediates in the preparation of certain pyrimido(6,1-a)isoquinolin-4-ones having pharmaceutical utilities, and methods for making said intermediates.
摘要翻译：所公开的是下式的化合物，其中X是氧，硫或卤素，可用作制备具有药物效用的某些嘧啶（6,1-a）异喹啉-4-酮的中间体，以及用于制造中间体。

105. 发明授权

US4293695A Furonaphthyridine compounds 失效
标题翻译：呋喃并吡啶化合物
公开(公告)号：US4293695A
公开(公告)日：1981-10-06
申请号：US191620
申请日：1980-09-29
申请人： Yoshiaki Tanaka , Isao Hayakawa
发明人： Yoshiaki Tanaka , Isao Hayakawa
IPC分类号： A61K31/435 , A61K49/00 , A61P31/04 , C07D213/65 , C07D213/73 , C07D213/74 , C07D471/04 , C07D491/14 , C07D491/147
CPC分类号： C07D213/73 , C07D213/65 , C07D213/74 , C07D471/04 , C07D491/14
摘要： 2,3,5,8-Tetrahydrofuro- and 5,8-dihydrofuro[3,2-b]-1,8-naphthyridine compounds of the formula (I) ##STR1## wherein R.sup.1 represents an alkyl group having 1 to 6 carbon atoms and M represents a hydrogen atom, an alkali metal or an alkaline earth metal having anti-bacterial activity.
摘要翻译：式（I）的2,3,5,8-四氢呋喃和5,8-二氢呋喃并[3,2-b] -1,8-萘啶化合物其中R 1表示具有1 至6个碳原子，M表示氢原子，具有抗菌活性的碱金属或碱土金属。

106. 发明授权

US4209620A Substituted 3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-one derivatives having antiallergy activity 失效
标题翻译：取代的具有抗过敏活性的3-（1H-四唑-5-基）-4H-吡啶并[1,2-a]嘧啶-4-酮衍生物
公开(公告)号：US4209620A
公开(公告)日：1980-06-24
申请号：US951437
申请日：1978-10-16
申请人： Peter F. Juby
发明人： Peter F. Juby
IPC分类号： C07D239/70 , C07D487/04 , C07D491/14 , C07D491/147 , A61K31/505 , C07D491/04
CPC分类号： C07D487/04 , C07D239/70 , C07D491/14 , Y10S514/826
摘要： A novel series of substituted 3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-ones is provided for use as inhibitors of allergic reactions. The compounds exhibit antiallergy activity by both oral and parenteral routes of administration.
摘要翻译：提供一系列取代的3-（1H-四唑-5-基）-4H-吡啶并[1,2-a]嘧啶-4-酮用作过敏反应的抑制剂。该化合物通过口服和肠胃外给药途径显示出抗炎活性。

107. 发明授权

US3987047A Tetrahydro-azepinoquinolines 失效
标题翻译：四氮唑腈
公开(公告)号：US3987047A
公开(公告)日：1976-10-19
申请号：US520965
申请日：1974-11-05
申请人： Gerhart Griss , Rudolf Hurnaus , Wolfgang Grell , Robert Sauter , Richard Reichl
发明人： Gerhart Griss , Rudolf Hurnaus , Wolfgang Grell , Robert Sauter , Richard Reichl
IPC分类号： C07D471/04 , C07D491/14 , C07D491/147
CPC分类号： C07D471/04 , C07D491/14 , Y10S514/96 , Y10S514/966
摘要： Compounds of the formula ##SPC1##Wherein ##EQU1## where R.sub.1 is hydrogen, straight or branched aliphatic acyl of 1 to 12 carbon atoms, methoxy-substituted straight or branched aliphatic acyl of 1 to 12 carbon atoms, benzoyl, halo-benzoyl, carbalkoxy of 2 to 7 carbon atoms, carbcycloalkoxy of 4 to 7 carbon atoms, benzyl, methylbenzyl, phenylsulfonyl, halo-phenylsulfonyl, tolylsulfonyl, alkenyl of 2 to 6 carbon atoms, phenyl, trifluoroacetyl, amidino, amido, thioamido, phenoxycarbonyl, benzyloxycarbonyl, methylsulfonyl or--B -- XwhereB is straight or branched alkylene of 1 to 6 carbon atoms, andX is hydrogen, hydroxyl, methoxy, carboxyl, cyano, dimethylaminocarbonyl, morpholino-carbonyl or carbalkoxy of 2 to 6 carbon atoms,R.sub.2 is hydrogen, hydroxyl, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms, alkanoyloxy of 1 to 3 carbon atoms, alkoxycarbonyloxy of 2 to 4 carbon atoms, amino, dimethylamino, morpholino or halogen,R.sub.3 is hydrogen, halogen, hydroxyl, carboxyl, straight or branched alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, alkoxy of 1 to 3 carbon atoms, phenyl-alkoxy of 1 to 3 carbon atoms, carbalkoxy of 2 to 4 carbon atoms -- alkoxy of 1 to 3 carbon atoms, carbalkoxy of 2 to 4 carbon atoms, hydroxymethyl, phenyl, phenoxy, amino, pyrrolidino or morpholino,R.sub.4, r.sub.5 and R.sub.6, which may be identical to or different from each other, are each hydrogen, halogen, methyl, hydroxyl, methoxy, cyano, amino, nitro, trifluoromethyl, carboxyl, acetyl or carbalkoxy of 2 to 4 carbon atoms, or any two of R.sub.4, R.sub.5 and R.sub.6 together are methylenedioxy, andX.sub.1 and X.sub.2 are hydrogen or together form a double bond,6-N-oxides thereof, and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as anoretics.

108. 发明授权

US3959312A Synthesis of antitumor alkaloid deoxyharringtonine and its precursor 3'-0-(5-methyl-2-oxohexanoyl)-cephalotaxine 失效
标题翻译：合成抗肿瘤生物碱脱氧胡椒碱及其前体3 {40-（5-甲基-2-氧代己酰） - 头孢噻肟
公开(公告)号：US3959312A
公开(公告)日：1976-05-25
申请号：US534925
申请日：1974-12-20
申请人： Kenneth L. Mikolajczak , Cecil R. Smith, Jr.
发明人： Kenneth L. Mikolajczak , Cecil R. Smith, Jr.
IPC分类号： C07C59/185 , C07C59/21 , C07D491/14 , C07D491/20 , C07F1/02
CPC分类号： C07D491/14 , C07C59/185 , C07C59/21 , C07F1/02 , Y10S514/908
摘要： The alkaloid deoxyharringtonine and its precursor 3'-O-(5-methyl-2-oxohexanoyl)-cephalotaxine were synthesized according to the following preferred series of reactions: Ethyl t-butyl oxalate + 1-lithio-3-methylbut-1-yne .fwdarw. t-butyl 5-methyl-2-oxohex-3-ynoate .fwdarw. t-butyl 5-methyl-2-oxohexanoate .sup.-trifluoroacetic acid 5-methyl-2-oxohexanoic acid .sup.(COCl).sbsp.2 5-methyl-2-oxohexanoyl chloride .sup.cephalotaxine 3'-O-(5-methyl-2-oxohexanoyl)-cephalotaxine .sup.lithio methyl acetate deoxyharringtonine.
摘要翻译：根据以下优选的一系列反应合成生物碱脱氧胡椒碱及其前体3'-O-（5-甲基-2-氧代己酰基） - 头孢噻肟：草酸叔丁酯+ 1-锂三甲基丁-1-炔 - 叔丁基5-甲基-2-氧代己-3-炔酸叔丁酯5-甲基-2-氧代己酸三氟乙酸5-甲基-2-氧代己酸（COCl）+402 5-甲基-2- 氧代己酰氯头孢噻肟3'-O-（5-甲基-2-氧代己酰基） - 头孢噻肟酸锂乙酸甲酯脱氧胡椒碱。

109. 发明授权

US3657256A Dipyridylium quaternary dihalide halogen complexes 失效
公开(公告)号：US3657256A
公开(公告)日：1972-04-18
申请号：US3657256D
申请日：1971-01-15
申请人： GREAT LAKES CHEMICAL CORP
发明人： THOMAS ROBERT M , GERNS FRED R , SANDS JOHN L
IPC分类号： C07D213/22 , C07D491/14
CPC分类号： C07D213/22 , C07D491/14
摘要： HALOGEN COMPLEXES OF DIPYRIDYLIUM QUATERNARY DIHALIDES WHICH ARE BACTERIOCIDAL AND HERBICIDAL AGENTS AND USEFUL AS DEFOLIANTS AND DESICCANTS, PARTICULARLY AS COTTON DEFOLIANT-DESICCANTS.

110. 发明授权

US3493579A 1,4-ethano-5h-(1)benzopyrano (3,4-b)pyridines 失效
标题翻译： 1,4-ETHANO-5H-（1）苯甲酰（3,4-B）吡啶
公开(公告)号：US3493579A
公开(公告)日：1970-02-03
申请号：US3493579D
申请日：1967-05-29
申请人： LITTLE INC A
发明人： LYLE ROBERT E JR , RAZDAN RAJ K , GRANCHELLI FELIX E , PARS HARRY G
IPC分类号： C07D491/14 , C07D99/04 , A61K27/00
CPC分类号： C07D491/14

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