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61. 发明授权

US4824840A Carbostyril derivatives and pharmaceutical preparations containing same 失效
标题翻译：卡波他汀衍生物和含有它们的药物制剂
公开(公告)号：US4824840A
公开(公告)日：1989-04-25
申请号：US25193
申请日：1987-03-12
申请人： Kazuo Banno , Takafumi Fujioka , Yasuo Oshiro , Kazuyuki Nakagawa
发明人： Kazuo Banno , Takafumi Fujioka , Yasuo Oshiro , Kazuyuki Nakagawa
IPC分类号： C07D215/06 , A61K31/4704 , A61K31/495 , A61P25/00 , A61P25/20 , A61P29/00 , A61P37/08 , A61P43/00 , C07D205/06 , C07D215/16 , C07D215/22 , C07D215/227 , C07D215/26 , C07D215/28 , C07D241/04 , C07D243/08 , C07D295/04 , C07D403/12 , C07D405/12 , C07D403/02
CPC分类号： C07D215/227 , C07D215/16 , C07D215/22 , C07D215/28
摘要： Carbostyril derivatives having antihistaminic action and central nervous controlling action are useful as antihistaminic agents or central nervous controlling agents. The derivatives are represented by the general formula, ##STR1## wherein R.sup.1 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an alkenyl group having 2 to 4 carbon atoms, an alkynyl group having 2 to 4 carbon atoms or a phenylalkyl group, an alkylene group containing 1 to 4 carbon atoms; R.sup.2 is a hydrogen atom, an alkyl group having 1 to 4 carbon atoms or a phenyl group; R.sup.3 is a hydrogen atom, a hydroxy group, an alkyl group having 1 to 4 carbon atoms, an alkanoyloxy group having 1 to 4 carbon atoms or a 3,4,5-trimethoxybenzoyloxy group; R.sup.4 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms; R.sup.5 is a cycloalkyl group having 3 to 8 carbon atoms, a phenyl group (which may have 1 to 3 substituted groups selected from the group consisting of halogen atoms, alkyl groups having 1 to 4 carbon atoms and alkoxy groups having 1 to 4 carbon atoms), an alkyl group having 1 to 4 carbon atoms (having one substituted group such as a hydroxy group, a phenyl group or an alkanoyloxy group having 1 to 4 carbon atoms), an alkanoyl group having 1 to 4 carbon atoms or benzoyl group; X is a halogen atom; n is 0, or an integer of 1 or 2; Q is an integer of 2 or 3, l and m are respectively an integer of 0 to 1-6, but the sum of l and m should not exceed 6; the carbon-carbon bond at the 3- and 4-positions in the carbostyril skeleton is a single or double bond and; the substituted position of the side chain of ##STR2## is any one of the 4-, 5-, 6-, 7- or 8-positions.
摘要翻译：具有抗组胺作用和中枢神经控制作用的卡波他特尔衍生物可用作抗组胺剂或中枢神经控制剂。衍生物由通式（1）表示，其中R 1是氢原子，具有1至6个碳原子的烷基，具有2至4个碳原子的烯基，具有2至4个碳原子的炔基原子或苯基烷基，含有1至4个碳原子的亚烷基; R2是氢原子，碳原子数1〜4的烷基或苯基; R3是氢原子，羟基，碳原子数1〜4的烷基，碳原子数1〜4的烷酰氧基或3,4,5-三甲氧基苯甲酰氧基。 R4是氢原子或碳原子数1〜4的烷基。 R5是具有3-8个碳原子的环烷基，苯基（其可以具有1至3个选自卤素原子，具有1至4个碳原子的烷基和具有1至4个碳原子的烷氧基的取代基）），碳原子数1〜4的烷基（具有羟基，苯基或碳原子数1〜4的烷酰氧基的一个取代基），碳原子数1〜4的烷酰基或苯甲酰基; X是卤原子; n为0或1或2的整数; Q为2或3的整数，l和m分别为0至1-6的整数，但l和m之和不应超过6; 喹诺酮骨架中3-和4-位的碳 - 碳键是单键或双键， “IMAGE”侧链的取代位置是4-，5-，6-，7-或8-位中的任何一个。

62. 发明授权

US4803225A Dihydroxy-phenethylamino compounds useful as pharmaceuticals 失效
标题翻译：用作药物的二羟基 - 苯乙基氨基化合物
公开(公告)号：US4803225A
公开(公告)日：1989-02-07
申请号：US127366
申请日：1987-12-02
申请人： John Dixon , Francis Ince
发明人： John Dixon , Francis Ince
IPC分类号： A61K31/135 , C07C43/174 , C07C43/23 , C07C45/51 , C07C65/24 , C07C237/00 , C07C275/28 , C07C323/25 , C07D215/22 , C07D215/227 , C07D215/26 , C07D263/14 , C07D319/08
CPC分类号： C07D215/227 , C07C205/37 , C07C205/44 , C07C255/00 , C07C275/28 , C07C323/00 , C07C323/25 , C07C43/174 , C07C43/23 , C07C45/515 , C07C65/24 , C07D215/26 , C07D263/14 , C07D319/08 , C07C2101/14 , Y10S514/821
摘要： There are provided compounds of formula I, ##STR1## and pharmaceutically acceptable derivatives thereof. There are also described the use of the compounds of formula I as pharmaceuticals, methods for making the compounds and pharmaceutical, e.g. cardiac, compositions containing the compounds.
摘要翻译：提供式I化合物，其药学上可接受的衍生物。还描述了式I化合物作为药物的用途，制备化合物的方法和药物，例如，心脏，含有化合物的组合物。

63. 发明授权

US4792559A 1,2,3,4-tetrahydroquinoline substituted 5-aminopentanenitrile compounds and their use as calcium modulators 失效
标题翻译： 1,2,3,4-四氢喹啉取代的5-氨基戊腈化合物及其作为钙调节剂的用途
公开(公告)号：US4792559A
公开(公告)日：1988-12-20
申请号：US911483
申请日：1986-09-25
申请人： Gilbert Regnier , Yves-Michel Gargouil , Jean-Paul Vilaine
发明人： Gilbert Regnier , Yves-Michel Gargouil , Jean-Paul Vilaine
IPC分类号： A61K31/275 , A61K31/335 , A61K31/357 , A61K31/47 , A61P3/00 , A61P3/14 , A61P9/08 , A61P9/10 , C07C67/00 , C07C253/00 , C07C255/42 , C07C255/43 , C07C313/00 , C07C315/04 , C07C317/48 , C07C319/20 , C07C323/63 , C07D215/26 , C07D263/54 , C07D317/00 , C07D317/60 , C07D319/00 , C07D319/18 , C07D405/12 , C07D413/12 , C07D417/12
CPC分类号： C07D405/12 , C07D215/26 , C07D317/60 , C07D319/18 , C07D413/12 , C07D417/12
摘要： 5-aminopentanenitrile compounds of the formula: ##STR1## in which: Ar represents ##STR2## in which: R.sub.1 is hydrogen, halogen trifluoromethyl or C.sub.1 -C.sub.5 -alkoxy, andR.sub.2 and R.sub.3, which are identical or different, each are hydrogen or C.sub.1 -C.sub.5 -alkoxy or together form --O--CH.dbd.CH--O-- or --O--CH.sub.2 --O--; or together form with the phenyl ring to which they are bound a benzoxazolyl, benzothiazolyl, benzothiadiazolyl or quinolyl radical;R is C.sub.3 -C.sub.15 -alkyl or ##STR3## in which: X is S or SO.sub.2 and Z is hydrogen, chlorine or C.sub.1 -C.sub.5 -alkyl or C.sub.1 -C.sub.5 -alkoxy;R' is C.sub.1 -C.sub.5 -alkyl, andAr' represents ##STR4## in which: R'.sub.1 is C.sub.1 -C.sub.5 -alkyl andR'.sub.2 is hydrogen or C.sub.1 -C.sub.4 -alkyl; and moreover when R is ##STR5## Ar' may be ##STR6## in which Y is C.sub.1 -C.sub.5 alkoxy andY' is hydrogen or C.sub.1 -C.sub.5 alkoxyThese compounds (I), and physiologically tolerable acid salts thereof may be used as medicines especially in the treatment of disorders requiring modulators of transmembrane and intracellular movements of calcium.
摘要翻译：其中：Ar表示，其中：R 1是氢，卤素三氟甲基或C 1 -C 5 - 烷氧基，R 2和R 3相同或不同，各自为氢或 C1-C5-烷氧基或一起形成-O-CH = CH-O-或-O-CH2-O-; 或与它们所结合的苯环一起形成苯并恶唑基，苯并噻唑基，苯并噻二唑基或喹啉基; R是C 3 -C 15 - 烷基或者其中：X是S或SO 2，Z是氢，氯或C 1 -C 5 - 烷基或C 1 -C 5 - 烷氧基; R'是C 1 -C 5 - 烷基，Ar'代表“IMA”，其中R 1是C 1 -C 5烷基，R 2是氢或C 1 -C 4 - 烷基; 此外，当R为 Ar'可以是其中Y为C1-C5烷氧基并且Y'为氢或C1-C5烷氧基的这些化合物（I）及其生理上可耐受的酸盐可用作药物特别是在需要调节剂的跨膜和细胞内运动的钙的治疗中。

64. 发明授权

US4599345A Chloromethyl quinoline derivatives and use thereof as analgesics 失效
标题翻译：氯甲基喹啉衍生物及其作为止痛剂的用途
公开(公告)号：US4599345A
公开(公告)日：1986-07-08
申请号：US557106
申请日：1983-12-01
申请人： Zoltan Salamon , Ilona Imre nee Virag , Magdolna Sebestyen
发明人： Zoltan Salamon , Ilona Imre nee Virag , Magdolna Sebestyen
IPC分类号： A61K31/47 , A61P25/04 , A61P29/00 , A61P31/04 , A61P31/10 , C07D215/18 , C07D215/20 , C07D215/26 , C07D215/12
CPC分类号： C07D215/20 , C07D215/18 , C07D215/26
摘要： A chlorinated quinoline derivative of formula (I) ##STR1## wherein R.sup.1 is --CCl.sub.3, --CF.sub.3, --CHCl.sub.2 or --CH.sub.2 Cl, R.sup.2 is hydrogen when R.sup.3 is not hydrogen, or is halogen, C.sub.1-4 alkoxy, C.sub.1-4 alkyl or R.sup.1, R.sup.3 is hydrogen when R.sup.2 is not hydrogen or is halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or CF.sub.3, R.sup.6 is hydrogen or halogen, X is halogen. The compounds are made by chlorination of selected compounds as disclosed and the new compounds can have antimicrobial, antifungal or analgesic effects.
摘要翻译：式（I）的氯化喹啉衍生物其中R 1为-CCl 3，-CF 3，-CHCl 2或-CH 2 Cl，R 2为氢时，R 3不为氢，或为卤素，C 1-4烷氧基， 4烷基或R 1，当R 2不是氢或卤素时，R 3是氢，C 1-4烷基，C 1-4烷氧基或CF 3，R 6是氢或卤素，X是卤素。化合物通过所公开的所选化合物的氯化制备，并且新化合物可具有抗微生物，抗真菌或镇痛作用。

65. 发明授权

US4442109A 3-Methylthiomethyl-and 3-methylsulfinylmethyl-4-quinolinones useful for treating hypertension 失效
标题翻译：可用于治疗高血压的3-甲硫基甲基 - 和3-甲基亚磺酰基甲基-4-喹啉酮
公开(公告)号：US4442109A
公开(公告)日：1984-04-10
申请号：US303948
申请日：1981-09-21
申请人： Roy V. Davies
发明人： Roy V. Davies
IPC分类号： C07D215/18 , C07D215/22 , C07D215/233 , C07D215/26 , C07D215/36 , C07D215/56 , A61K31/47
CPC分类号： C07D215/233 , C07D215/18 , C07D215/26 , C07D215/36 , C07D215/56
摘要： Novel quinolones of the general formula ##STR1## wherein n is 0, 1 or 2; R.sub.1 is C.sub.1-4 alkyl; and R.sub.3 is hydrogen, C.sub.1-4 alkyl, methoxy, methylthio, halo or trifluoromethyl. These compounds have antihypertensive activity and may be used for treating hypertension in mammals.The quinolones are administered in novel therapeutic compositions comprising a quinolone of the above general formula together with a pharmaceutically acceptable carrier.Processes for making the novel quinolones are described.
摘要翻译：通式的新型喹诺酮类，其中n为0,1或2; R1是C1-4烷基; 并且R 3是氢，C 1-4烷基，甲氧基，甲硫基，卤素或三氟甲基。这些化合物具有抗高血压活性，可用于治疗哺乳动物的高血压。喹诺酮以包含上述通式的喹诺酮和药学上可接受的载体的新型治疗组合物给药。描述了制备新型喹诺酮类的方法。

66. 发明授权

US4317887A Metal complexing polymers 失效
标题翻译：金属络合聚合物
公开(公告)号：US4317887A
公开(公告)日：1982-03-02
申请号：US65751
申请日：1979-08-10
申请人： Abraham Warshawsky , Rami Kalir , Abraham Patchornik
发明人： Abraham Warshawsky , Rami Kalir , Abraham Patchornik
IPC分类号： C01G3/00 , C07D215/26 , C07F9/09 , C07F9/165 , C07F9/20 , C07F9/53 , C08F8/00 , C22B3/26 , C22B3/30 , C22B3/36 , C22B3/38 , B01J45/00
CPC分类号： C07F9/09 , C01G3/003 , C07D215/26 , C07F9/165 , C07F9/20 , C07F9/53 , C08F8/02 , C08F8/26 , C08F8/30 , C08F8/32 , C08F8/34 , C08F8/38 , C08F8/44 , C22B3/0017 , C22B3/0036 , C22B3/0052 , C22B3/0066 , C22B3/0067 , C22B3/007 , C22B3/0097 , C08F2810/20 , Y02P10/234
摘要： Novel polyfunctional compounds and polymers are disclosed of the general formula ##STR1## wherein Q designates -X' or -X-.epsilon.-R; where X' designates ##STR2## where .alpha. is --OH, or --SH;.beta. is --OH, --SH, --NH.sub.2, --NO.sub.2, --CO--R.sub.2, --R.sub.2 C.dbd.N--OH, --COOH, -hal, alkyl, aryl, or aralkyl; halogen being chlorine or bromine;.gamma. is a non-interfering substituent;where .beta. and .gamma. may form together a hydrocarbyl ring system;where .delta. is --(CH.sub.2).sub.n -- or --SO.sub.2 --;where X is --O--, --S--, --NH--, --N.sup.+ R.sub.2 R.sub.3 Cl.sup.- or --P--;where.epsilon. is --(CH.sub.2).sub.n --, --SO.sub.2 --, --NH-- or --CH.sub.2 (O-CH.sub.2 --CH.sub.2).sub.n --; ##STR3## wherein the upwardly directed bonds are connected to the R polymer molecule and the downwardly directed bonds are connected to .delta. groups;n is an integer of from 1 to 15 or zero;R is a polymeric backbone, alkyl or aralkyl; andR.sub.2, R.sub.3 and R.sub.4 which may be identical or different, each designates hydrogen, alkyl, aryl or aralkyl. These compounds are useful as ion-exchange agents, extractants, biocides, flameproofing agents, fire retardants, metal polishing agents and rust inhibitors. Metals may be selectively extracted from solution thereof by means of these compounds and polymers.
摘要翻译：公开了通式“IMAGE”的新型多官能化合物和聚合物，其中Q表示-X'或-X-ε-R; 其中X'表示 SP（S）（OR2）2; NH2; NHR2; NR2R3; N + R2R3R4Cl- 其中α是-OH或-SH; β是-OH，-SH，-NH 2，-NO 2，-CO-R 2，-R 2 C = N-OH，-COOH， - 卤素，烷基，芳基或芳烷基; 卤素是氯或溴; γ是非干扰取代基; 其中β和γ可以一起形成烃基环体系; 其中δ是 - （CH 2）n - 或-SO 2 - ; 其中X是-O - ， - S - ， - NH - ， - N + R2R3Cl-或-P-; 其中ε是 - （CH 2）n - ， - SO 2 - ， - NH-或-CH 2（O-CH 2 -CH 2）n - 其中向上指向的键连接到R聚合物分子并且向下指向的键连接到δ基团; n为1至15的整数或零; R是聚合物主链，烷基或芳烷基; 和R 2，R 3和R 4可以相同或不同，各自表示氢，烷基，芳基或芳烷基。这些化合物可用作离子交换剂，萃取剂，杀生物剂，防火剂，阻燃剂，金属抛光剂和防锈剂。金属可以通过这些化合物和聚合物从其溶液中选择性提取。

67. 发明授权

US4298739A Novel carbostyril derivatives 失效
标题翻译：新型喹诺酮衍生物
公开(公告)号：US4298739A
公开(公告)日：1981-11-03
申请号：US142057
申请日：1980-04-21
申请人： Takao Nishi , Hiraki Ueda , Kazuyuki Nakagawa
发明人： Takao Nishi , Hiraki Ueda , Kazuyuki Nakagawa
IPC分类号： C07D215/22 , C07D215/227 , C07D215/26 , A61K31/47
CPC分类号： C07D215/227 , C07D215/26
摘要： Novel carbostyril derivatives having platelet aggregation inhibitory action, antiinflamatory action, antiulcer action, vasodilatory action and phosphodiesterase inhibitory action and are useful for preventing or curing thrombus, arteriosclerosis, hypertension, asthma and other like diseases, and also useful as an antiinflamatory or anti-ulcer agent, represented by the formula ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, phenyl-C.sub.1-4 alkyl-; R.sup.2 is hydrogen, a halogen atom, hydroxy, phenyl-C.sub.1-4 alkoxy; R.sup.3 is hydrogen, hydroxy, C.sub.1-4 alkyl; R.sup.4 is C.sub.3-8 cycloalkyl, substituted or unsubstituted phenyl, C.sub.3-8 cycloalkyl-C.sub.1-4 alkyl, 2-(3,4-dimethoxyphenyl)-ethyl, R.sup.5 is hydrogen, C.sub.1-8 alkyl, C.sub.2-4 alkenyl, phenyl, C.sub.3-8 cycloalkyl, phenyl-C.sub.1-4 alkyl, C.sub.3-8 cycloalkyl-C.sub.1-4 alkyl, m is an integer of 1 - 3, l and n which may be same or different, and are respectively 0 or an integer of 1 - 7 and the sum of l and n is not exceeding 7, the carbon-carbon bond at 3- and 4-positions in the carbostyril skelton is either single or double bond.
摘要翻译：具有血小板聚集抑制作用，抗炎作用，抗溃疡作用，血管扩张作用和磷酸二酯酶抑制作用的新型喹诺酮衍生物，可用于预防或治疗血栓，动脉硬化，高血压，哮喘等疾病，并且还可用作抗炎或抗溃疡其中R 1为氢，C 1-4烷基，C 2-4链烯基，苯基-C 1-4烷基 - ; R2是氢，卤素原子，羟基，苯基-C 1-4烷氧基; R3是氢，羟基，C1-4烷基; R4是C3-8环烷基，取代或未取代的苯基，C3-8环烷基-C1-4烷基，2-（3,4-二甲氧基苯基） - 乙基，R5是氢，C1-8烷基，C2-4烯基，苯基， C 3-8环烷基，苯基-C 1-4烷基，C 3-8环烷基-C 1-4烷基，m是1-3的整数，l和n可以相同或不同，分别为0或整数1 -7和n和n的总和不超过7，在喹诺酮骨架中3-和4-位的碳 - 碳键是单键或双键。

68. 发明授权

US4297358A Novel 4,7-phenanthroline derivatives and pharmaceutical compositions containing them and their use 失效
标题翻译：新颖的4,7-菲咯啉衍生物和含有它们的药物组合物及其用途
公开(公告)号：US4297358A
公开(公告)日：1981-10-27
申请号：US109715
申请日：1980-01-04
申请人： Georges Haas , Knut A. Jaeggi , Alberto Rossi , Alex Sele
发明人： Georges Haas , Knut A. Jaeggi , Alberto Rossi , Alex Sele
IPC分类号： A61K31/47 , A61P37/08 , C07D215/26 , C07D215/38 , C07D471/04 , C07D487/04 , A61K31/435
CPC分类号： C07D215/38 , C07D215/26 , C07D471/04
摘要： New 4,7-phenanthroline derivatives of the formula (I) ##STR1## in which Ch represents an optionally substituted 5,6-quinolinylene radical of which the 6-position is joined to the --N(R.sub.E)-- group, andR represents an optionally esterified or amidated carboxy group,and in which eitherR.sub.A and R.sub.B together represent oxo,R.sub.C and R.sub.D together represent an additional link, andR.sub.E represents a radical R.sub.1 which is hydrogen, or an aliphatic, cycloaliphatic, araliphatic or heterocyclic-aliphatic radical, orR.sub.A represents an optionally etherified hydroxy group andR.sub.B together with R.sub.C and R.sub.D together with R.sub.E in each case represents an additional link,and salts of salt-forming compounds of the formula (I), compounds of the formula (I) or the salts thereof have anti-allergic properties. They can be prepared in accordance with processes known per se and may be used as active substances in pharmaceutical preparations.
摘要翻译：式（I）的新的4,7-菲咯啉衍生物其中Ch表示6位与-N（RE） - 基团连接的任意取代的5,6-喹啉基，并且R表示任选酯化或酰胺化的羧基，并且其中RA和RB一起表示氧代，RC和RD一起表示另外的连接，并且RE表示基团R 1，其为氢或脂族，脂环族，芳脂族或杂环脂族基团，或RA表示任选醚化的羟基，RB与RC和RD一起连同RE一起代表另外的连接，式（I）的成盐化合物的盐，式（I）的化合物）或其盐具有抗过敏性质。它们可以根据本身已知的方法制备，并且可以用作药物制剂中的活性物质。

69. 发明授权

US4216220A Platelet aggregation inhibiting 2-oxyindoles, their compositions and method of use 失效
标题翻译：抑制2-羟基吲哚的血小板聚集体，其组成和使用方法
公开(公告)号：US4216220A
公开(公告)日：1980-08-05
申请号：US806926
申请日：1977-06-15
申请人： Kazuyuki Nakagawa , Minoru Uchida , Kimiaki Oka
发明人： Kazuyuki Nakagawa , Minoru Uchida , Kimiaki Oka
IPC分类号： C07D209/34 , C07D215/22 , C07D215/227 , C07D215/26 , C07D209/04
CPC分类号： C07D215/227 , C07D209/34 , C07D215/26 , Y10S514/822
摘要： 2-Oxyindole derivatives represented by the following general formula: ##STR1## where R.sub.1 is selected from the group consisting of hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, benzyl and phenethyl; A is --CH.dbd.CH-- or ##STR2## wherein R.sub.2 or R.sub.3 may be the same or different and are selected from the group consisting of hydrogen and C.sub.1-4 alkyl; R.sub.4 is --OR.sub.5, wherein R.sub.5 is selected from the group consisting of hydrogen, C.sub.1-8 alkyl, cyclohexyl, benzyl and phenethyl, or ##STR3## wherein R.sub.6 and R.sub.7 may be the same or different and are selected from the group consisting of hydrogen, C.sub.1-4 alkyl, benzyl, phenethyl and together with the nitrogen atom, a heterocyclic group selected from the group consisting of a piperidino, morpholino, piperazino or thiazolino group; and m and n each are zero or a positive integer with m+n being no more than 11. The 2-oxyindole derivatives have excellent effects on the inhibition of platelet aggregation.
摘要翻译：由下列通式表示的2-氧吲哚衍生物：其中R 1选自氢，C 1-4烷基，C 2-4链烯基，苄基和苯乙基; A是-CH = CH-或其中R 2或R 3可以相同或不同，并且选自氢和C 1-4烷基; R 4是-OR 5，其中R 5选自氢，C 1-8烷基，环己基，苄基和苯乙基，或其中R 6和R 7可以相同或不同，并且选自氢，C 1-4烷基，苄基，苯乙基和氮原子一起选自哌啶子基，吗啉代，哌嗪基或噻唑基的杂环基; m和n各自为零或m + n不大于11的正整数。2-氧吲哚衍生物对抑制血小板聚集具有优异的效果。

70. 发明授权

US4187310A 1,2-Dihydro-2-oxoquinol-4-ylacetic acid derivatives and pharmaceutical compositions 失效
标题翻译： 1,2-二氢-2-氧代喹啉-4-基乙酸衍生物和药物组合物
公开(公告)号：US4187310A
公开(公告)日：1980-02-05
申请号：US945596
申请日：1978-09-25
申请人： David R. Brittain , Edward D. Brown , Walter Hepworth , Gilbert J. Stacey
发明人： David R. Brittain , Edward D. Brown , Walter Hepworth , Gilbert J. Stacey
IPC分类号： C07D215/22 , C07D215/227 , C07D215/26 , C07D215/36 , C07D215/38 , A61K31/545
CPC分类号： C07D215/227 , C07D215/26 , C07D215/36 , C07D215/38
摘要： Novel 1,2-dihydro-2-oxoquinol-4-ylalkanoic acid derivatives bearing a variety of substituents on the quinoline nucleus but including, at position 1, an aromatic radical linked directly or through a C.sub.1-4 -alkylene or a C.sub.2-4 -alkenylene radical. Representative compounds of the invention are 1-(3,4-dichlorobenzyl)-3-methyl-1,2-dihydro-2-oxoquinol-4-ylacetic acid and .alpha.-(1-benzyl-1,2-dihydro-2-oxoquinol-4-yl)propionic acid. The compounds possess anti-inflammatory or analgesic properties, or are inhibitors of the enzyme aldose reductase.
摘要翻译：在喹啉核上带有各种取代基的新型1,2-二氢-2-氧代喹啉-4-基链烷酸衍生物，但在第1位包括直接或通过C 1-4 - 亚烷基或C 2-4的芳族基团亚烯基。本发明的代表性化合物是1-（3,4-二氯苄基）-3-甲基-1,2-二氢-2-氧代喹啉-4-基乙酸和α-（1-苄基-1,2-二氢-2- 氧代喹啉-4-基）丙酸。该化合物具有抗炎或镇痛特性，或是醛糖还原酶的抑制剂。

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