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91. 发明授权

US5514825A Acetylenes disubstituted with a 5 substituted tetrahydronaphthyl group and with an aryl or heteroaryl group having retinoid-like biological activity 失效
公开(公告)号：US5514825A
公开(公告)日：1996-05-07
申请号：US366168
申请日：1994-12-29
申请人： Vidyasagar Vuligonda , Min Teng , Richard L. Beard , Alan T. Johnson , Tien T. Duong , Yuan Lin , Roshantha A. Chandraratna
发明人： Vidyasagar Vuligonda , Min Teng , Richard L. Beard , Alan T. Johnson , Tien T. Duong , Yuan Lin , Roshantha A. Chandraratna
IPC分类号： C07C17/10 , C07C17/26 , C07C17/35 , C07C45/28 , C07C45/67 , C07C63/66 , C07C65/38 , C07C69/76 , C07C229/46 , C07C233/58 , C07C251/48 , C07C255/41 , C07C255/47 , C07C309/65 , C07C323/61 , C07C327/32 , C07D213/55 , C07D213/80 , C07D277/30 , C07D307/54 , C07D309/06 , C07D309/12 , C07D333/24 , C07D339/08 , C07F7/08 , C07F7/18 , C07C255/34 , C07C255/40
CPC分类号： C07D213/80 , C07C17/10 , C07C17/263 , C07C17/35 , C07C229/46 , C07C233/58 , C07C251/48 , C07C255/41 , C07C255/47 , C07C309/65 , C07C323/61 , C07C327/32 , C07C45/28 , C07C45/673 , C07C63/66 , C07C65/38 , C07C69/76 , C07D213/55 , C07D277/30 , C07D307/54 , C07D309/06 , C07D309/12 , C07D333/24 , C07D339/08 , C07F7/0818 , C07F7/1856 , C07C2102/10
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 10 carbons; R.sub.2 and R.sub.3 are hydrogen, or alkyl of 1 to 6 carbons and the substituted ethynyl group occupies either the 2 or the 3 position of the tetrahydronaphthalene nucleus; m is an integer having the value of 0-3; o is an integer having the value 0-4; Y is a phenyl group, or heteroaryl selected from a group consisting of pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, and imidazolyl, said groups being optionally substituted with one or two R.sub.2 groups; 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, CR.sub.7 OR.sub.13 O, or tri-lower alkylsilyl, 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 (trimethylsilyl)alkyl where the alkyl group has 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, and R.sub.19 is independently hydrogen, alkyl of 1 to 10 carbons, fluoro-substituted alkyl of 1 to 10 carbons, alkenyl of 2 to 10 carbons and having 1 to 3 double bonds, alkynyl having 2 to 10 carbons and 1 to 3 triple bonds, carbocyclic aryl selected from the group consisting of phenyl, C.sub.1 -C.sub.10 -alkylphenyl, naphthyl, C.sub.1 -C.sub.10 -alkylnaphthyl, phenyl-C.sub.1 -C.sub.10 alkyl, napthyl-C.sub.1 -C.sub.10 alkyl; CN, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, (CH.sub.2).sub.p CO.sub.2 R.sub.8, (CH.sub.2).sub.p CH.sub.2 OH, (CH.sub.2).sub.p CH.sub.2 OR.sub.11, (CH.sub.2).sub.p CH.sub.2 OCOR.sub.11, where p is an integer between 0 to 10, or the two R.sub.19 groups jointly represent 3 to 6 methylene groups which together with the alkylidene carbon complete a ring, have retinoid like biological activity.

92. 发明授权

US5498755A Disubstituted aryl and heteroaryl imines having retinoid-like biological activity 失效
标题翻译：具有类视黄醇样生物活性的二取代芳基和杂芳基亚胺
公开(公告)号：US5498755A
公开(公告)日：1996-03-12
申请号：US294901
申请日：1994-08-23
申请人： Roshantha A. Chandraratna , Min Teng
发明人： Roshantha A. Chandraratna , Min Teng
IPC分类号： C07C251/24 , C07D213/80 , C07D215/38 , C07D311/58
CPC分类号： C07D213/80 , C07C251/24 , C07D215/38 , C07D311/58
摘要： Compounds of the formula ##STR1## wherein the R.sub.1 groups independently are hydrogen, lower alkyl, or two geminal R.sub.1 groups jointly represent an oxo (.dbd.O) or a thio (.dbd.S) group; R.sub.2 is hydrogen or lower alkyl, or halogen; M is or --N.dbd.CR.sub.4 -- or --R.sub.4 C.dbd.N-- where R.sub.4 is hydrogen or lower alkyl; X is C(R.sub.1).sub.2 ; Y is phenyl optionally substituted with an R.sub.3 group which is lower alkyl or halogen; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl, cycloalkyl, alkenyl, alkynyl; 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.2OR.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R 1基团独立地为氢，低级烷基或两个偕R 1基团的式（ⅩⅧ）化合物共同表示氧代（= O）或硫代（= S）基团; R2是氢或低级烷基或卤素; M是或-N = CR 4 - 或-R 4 C = N-，其中R 4是氢或低级烷基; X为C（R 1）2; Y是任选被低级烷基或卤素的R 3基团取代的苯基; A是（CH 2）n，其中n是0-5，低级支链烷基，环烷基，烯基，炔基; 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是烷基，碳原子数为1〜5的环烷基或烯基，R8为碳原子数为1〜10的烷基或碳原子数为5〜10的环烷基，或R8为苯基或低级烷基苯基，R9和R10分别为氢，烷基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，具有类视黄醇类生物活性。

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