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    • 11. 发明授权
    • Antipsychotic indolyl derivatives
    • 抗精神病药物吲哚衍生物
    • US06689792B2
    • 2004-02-10
    • US09976321
    • 2001-10-12
    • Michael G. KellyYoung H. Kang
    • Michael G. KellyYoung H. Kang
    • A61K31454
    • C07D209/42C07D209/08C07D209/34C07D403/12
    • Compounds of formula (1) are provided: wherein R1 and R2 are H, OH, F, Cl, Br, I, 1 to 6 carbon alkyl or alkenyl, 1 to 6 carbon alkoxy, aryl, OR5, nitro, amino, CF3 or R1 and R2 are taken together to form a fused ring at the 2,3- or 3,4-positions providing a fused phenyl group or a benzodioxane group, or a 4- or 7-substituted indole group, or a 5- or 8-substituted quinoline group; R3 represents a group selected from hydrogen, a 1 to 6 carbon alkyl, a 1 to 4 carbon alkoxy or a halogen; R4 represents a group selected from hydrogen, 1 to 6 carbon alkyl or R5; R5 is CH2Ph in which the phenyl ring can be optionally substituted by a group selected from OMe, halogen, CF3; X is selected from a group represented by C, CR4, [[CHR4]] and CHCH2; A is selected from a group represented by N, NH, CH and CH2; B is selected from a group represented by ═O, ═S, H and H2; or A and B may be concatenated together to form indole, benzimidazole, indolone or indoline moieties; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods of treating central nervous system disorders utilizing these compounds.
    • 提供式(1)化合物:其中R 1和R 2是H,OH,F,Cl,Br,I,1至6碳烷基或烯基,1至6个碳烷氧基,芳基,OR 5,硝基,氨基,CF 3或R 1 并且R 2一起在2,3或3,4位上形成稠环,提供稠合苯基或苯并二恶烷基,或4-或7-取代的吲哚基,或5-或8-取代的吲哚基, 取代的喹啉基; R 3表示选自氢,1至6个碳烷基,1至4个碳烷氧基或卤素的基团; R 4表示选自氢,1至6个碳烷基或R 5的基团; R 5是CH 2 Ph,其中 苯环可任选被选自OMe,卤素,CF 3的基团取代; X选自C,CR 4,[[CHR]]和CHCH 2表示的基团; A选自N,NH, CH和CH 2; B选自由= O,= S,H和H 2表示的基团;或者A和B可以连接在一起形成吲哚,苯并咪唑,吲哚酮或二氢吲哚部分; 或其药学上可接受的盐,以及利用这些化合物治疗中枢神经系统疾病的药物组合物和方法。
    • 13. 发明授权
    • Cycloalkyl-substituted aryl-piperazines, piperidines and tetrahydropyridines as serotonergic agents
    • 环烷基取代的芳基哌嗪,哌啶和四氢吡啶作为血清素能药
    • US06518272B2
    • 2003-02-11
    • US10107866
    • 2002-03-27
    • Wayne E. ChildersMichael G. KellyYvette L. PalmerEdward J. Podlesny
    • Wayne E. ChildersMichael G. KellyYvette L. PalmerEdward J. Podlesny
    • A61K3150
    • C07D239/42C07D209/08C07D211/22C07D213/74C07D217/22C07D277/82C07D295/125C07D295/13C07D319/20
    • This invention relates to compounds which have activity as 5-HT1A agonists and antagonists which may be useful for the treatment of anxiety, depression, cognitive deficits, and prostate cancer, having the formula wherein: X is a moiety selected from the group of: n is selected from the integers 1 through 5; R1 is optionally substituted aryl or mono or bicyclic heteroaryl, with a proviso that heteroaryl is not thiadiazole; R2 is H or alkyl; R3 is H, COR5, COOR5, and CONR5R6; R4 is H, alkyl, alkenyl, alkynyl, aryl, mono or bicyclic heteroaryl, aralkyl, and mono or bicyclic heteroaralkyl, wherein the aryl or heteroaryl groups are optionally substituted; R5 and R6 are H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, adamantyl, and noradamantyl or R5 and R6 taken together may form a 5-7 membered azacyclic ring, optionally containing an additional heteroatom selected from O, S, or NR4; when R5 or R6 are chosen from cycloalkyl or cycloalkenyl, the cyclic group may optionally be substituted at the 1-position with a C1-C3 alkyl group; or an optical isomer; or a pharmaceutically acceptable salt thereof.
    • 本发明涉及具有作为5-HT 1A激动剂和拮抗剂的活性的化合物,其可用于治疗具有下列基团的焦虑,抑郁,认知缺陷和前列腺癌:X是选自以下的部分:n是 从整数1到5中选择; R 1是任选取代的芳基或单或双环杂芳基,条件是杂芳基不是噻二唑; R2是H或烷基; R3是H,COR5,COOR5和CONR5R6; R 4是H,烷基,烯基,炔基,芳基,单或双环杂芳基,芳烷基和单或双环杂芳烷基,其中芳基或杂芳基任选被取代; R5和R6是H,烷基,烯基,炔基,环烷基,环烯基,金刚烷基和去月桂烷基或R5和R6一起可以形成5-7元的氮杂环,任选地含有选自O,S或NR4的另外的杂原子; 当R5或R6选自环烷基或环烯基时,环状基团可以任选在1-位被C1-C3烷基取代;或光学异构体; 或其药学上可接受的盐。
    • 15. 发明授权
    • Indolyl derivatives as serotonergic agents
    • 吲哚衍生物作为血清素能药
    • US06204274B1
    • 2001-03-20
    • US09298200
    • 1999-04-23
    • Michael G. KellyYoung H. Kang
    • Michael G. KellyYoung H. Kang
    • A61K31445
    • C07D401/14
    • The present invention provides compounds of the formula (1): wherein R1 and R2 each independently represent hydrogen, hydroxy, F, Cl, Br, I, CN, 1 to 6 carbon alkyl, 1 to 6 carbon alkoxy, nitro, CF3 and phenyloxy or benzyloxy, in which the aromatic ring can be optionally substituted by from 1 to 3 groups selected from C1-C6 alkoxy (preferably OMe), F, Cl, Br, I, and CF3; R3 and R4 are each independently a hydrogen, a 1 to 6 carbon alkyl or a CH2Ph in which the phenyl ring can be optionally substituted by from 1 to 3 groups selected from C1-C6 alkoxy (preferably OMe), F, Cl, Br, I, and CF3; Y is selected from CH2 or CH and, X is selected from a group represented by N, CR3, CHR3, CHCH; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods of using the compounds to treat central nervous system disorders, such as depression, anxiety, drug withdrawal, eating and sexual disorders and other conditions for which serotonin reuptake inhibitors are used.
    • 本发明提供式(1)的化合物:其中R 1和R 2各自独立地表示氢,羟基,F,Cl,Br,I,CN,1至6个碳原子的烷基,1至6个碳烷氧基,硝基,CF 3和苯氧基或 苄氧基,其中芳环可以任选被1至3个选自C 1 -C 6烷氧基(优选OMe),F,Cl,Br,I和CF 3的基团取代; R 3和R 4各自独立地为氢, 至6碳烷基或CH 2 Ph,其中苯环可以任选被1至3个选自C 1 -C 6烷氧基(优选OMe),F,Cl,Br,I和CF 3的基团取代; Y选自CH 2或 CH,X选自由N,CR 3,CHR 3,CHCH表示的基团;或其药学上可接受的盐,以及使用该化合物治疗中枢神经系统疾病如抑郁症,焦虑症, 药物戒断,饮食和性障碍以及使用5-羟色胺再摄取抑制剂的其他条件。
    • 18. 发明授权
    • Soil repellents derived from fluorinated acrylates and aromatic amines
    • 衍生自氟化丙烯酸酯和芳族胺的防污剂
    • US4550189A
    • 1985-10-29
    • US697293
    • 1985-02-01
    • Michael G. KellyJames H. Covill
    • Michael G. KellyJames H. Covill
    • C08K5/18C07C101/447
    • C08K5/18
    • Soil repellents derived from fluorinated acrylates and aromatic amines are disclosed which have excellent durability and resistance to laundering. The compounds are represented by the formula(R).sub.m --Ar--(NHCH.sub.2 CH(R.sub.1)CO.sub.2 R.sub.f).sub.nwherein n is 1 to 3 and m is 0 to 4, Ar is an aromatic radical containing from 1 to 3 benzene rings which may be fused together or linked through a single carbon-carbon bond or a linking group, R.sub.f is a fluorinated radical, R.sub.1 is H or CH.sub.3, and R is independently selected from lower alkyl, lower alkoxy, halogen, hydroxy, nitro, cyano, amino, lower alkylamino, lower acylamino, --CO.sub.2 R.sub.3 and --NHCH.sub.2 CH(R.sub.1)CO.sub.2 R.sub.3 wherein R.sub.3 is lower alkyl, --CH.sub.2 CH.sub.2 OH, or --CH.sub.2 CH(OH)CH.sub.2 Cl. Also disclosed are polyester and nylon fibers having these compounds incorporated therein.
    • 公开了从氟化丙烯酸酯和芳族胺衍生的防污剂,其具有优异的耐久性和耐洗涤性。 化合物由式(R)m-Ar-(NHCH 2 CH(R 1)CO 2 R f)n表示,其中n为1至3,m为0至4,Ar为含有1至3个苯环的芳族基团,其可以是 稠合在一起或通过单个碳 - 碳键或连接基团连接,Rf是氟化基团,R1是H或CH3,R独立地选自低级烷基,低级烷氧基,卤素,羟基,硝基,氰基,氨基, 低级烷基氨基,低级酰基氨基,-CO 2 R 3和-NHCH 2 CH(R 1)CO 2 R 3,其中R 3是低级烷基,-CH 2 CH 2 OH或-CH 2 CH(OH)CH 2 Cl。 还公开了具有这些化合物的聚酯和尼龙纤维。