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51.发明授权O- or S- substituted tetrahydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity 失效O-或S-取代的四氢萘衍生物，其具有类视黄醇和/或维生素A拮抗剂样生物活性公开(公告)号：US06187933B1
公开(公告)日：2001-02-13
申请号：US09492495
申请日：2000-01-27
申请人： Vidyasagar Vuligonda , Min Teng , Richard L. Beard , Alan T. Johnson , Yuan Lin , Roshantha A. Chandraratna
发明人： Vidyasagar Vuligonda , Min Teng , Richard L. Beard , Alan T. Johnson , Yuan Lin , Roshantha A. Chandraratna
IPC分类号： C07D30912
CPC分类号： C07D339/08 , C07C69/587 , C07C69/734 , C07C69/76 , C07C233/81 , C07C235/66 , C07C245/10 , C07C251/44 , C07C309/65 , C07C317/44 , C07C323/55 , C07C2602/10 , C07D277/30 , C07D309/12 , C07D317/20 , C07D317/24 , C07D317/26 , C07D333/24 , C07D409/10
摘要： Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
摘要翻译： 符号具有本申请中描述的含义的化合物具有类视黄醇样或类视黄醇拮抗剂样的生物活性。
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52.发明授权Alkylidene substituted tetrahydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity 失效具有类视黄醇和/或维生素A拮抗剂的生物活性的亚烷基取代的四氢萘衍生物
公开(公告)号：US5998655A
公开(公告)日：1999-12-07
申请号：US30353
申请日：1998-02-25
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： C07C69/587 , C07C69/76 , C07C233/81 , C07C245/10 , C07C251/44 , C07C309/65 , C07C317/44 , C07C323/55 , C07D277/30 , C07D309/12 , C07D317/20 , C07D317/24 , C07D317/26 , C07D333/24 , C07D339/08 , C07D409/10
CPC分类号： C07D409/10 , C07C233/81 , C07C245/10 , C07C251/44 , C07C309/65 , C07C317/44 , C07C323/55 , C07C69/587 , C07C69/76 , C07D277/30 , C07D309/12 , C07D317/20 , C07D317/24 , C07D317/26 , C07D333/24 , C07D339/08 , C07C2102/10
摘要： Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
摘要翻译： 符号具有本申请中描述的含义的式的化合物具有类视黄醇样或维生素A拮抗剂样生物活性。
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53.发明授权Alkyl or aryl substituted dihydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity 失效具有类视黄醇和/或维生素A拮抗剂的生物活性的烷基或芳基取代的二氢萘衍生物
公开(公告)号：US5773594A
公开(公告)日：1998-06-30
申请号：US667663
申请日：1996-06-21
申请人： Alan T. Johnson , Min Teng , Vidyasagar Vuligonda , Richard L. Beard , Samuel J. Gillett , Tien T. Duong , Roshantha A. Chandraratna
发明人： Alan T. Johnson , Min Teng , Vidyasagar Vuligonda , Richard L. Beard , Samuel J. Gillett , Tien T. Duong , Roshantha A. Chandraratna
IPC分类号： C07C69/587 , C07C69/76 , C07C233/81 , C07C245/10 , C07C251/44 , C07C309/65 , C07C317/44 , C07C323/55 , C07D277/30 , C07D309/12 , C07D317/20 , C07D317/24 , C07D317/26 , C07D333/24 , C07D339/08 , C07D409/10
CPC分类号： C07D409/10 , C07C233/81 , C07C245/10 , C07C251/44 , C07C309/65 , C07C317/44 , C07C323/55 , C07C69/587 , C07C69/76 , C07D277/30 , C07D309/12 , C07D317/20 , C07D317/24 , C07D317/26 , C07D333/24 , C07D339/08 , C07C2102/10
摘要： Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
摘要翻译： 符号具有本申请中描述的含义的式“IMAGE”的化合物具有类视黄醇样或维生素A拮抗剂样的生物活性。
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54.发明授权Aryl-and heteroarylcyclohexenyl substituted alkenes having retinoid agonist, antagonist or inverse agonist type biological activity 失效具有类视黄醇激动剂，拮抗剂或反向激动剂型生物活性的芳基和杂芳基环己烯基取代的烯烃
公开(公告)号：US5760276A
公开(公告)日：1998-06-02
申请号：US810826
申请日：1997-03-06
申请人： Richard L. Beard , Alan T. Johnson , Min Teng , Vidyasagar Vuligonda , Roshantha A. Chandraratna
发明人： Richard L. Beard , Alan T. Johnson , Min Teng , Vidyasagar Vuligonda , Roshantha A. Chandraratna
IPC分类号： A61P3/02 , A61K31/192 , A61K31/215 , A61K31/216 , A61P9/00 , A61P17/02 , A61P17/06 , A61P17/10 , A61P25/00 , A61P37/00 , C07C63/33 , C07C63/66 , C07C69/76 , C07C309/65 , C07C66/76
CPC分类号： C07C403/02 , C07C309/65 , C07C69/76 , C07C2101/16
摘要： Compounds of the formula ##STR1## wherein the symbols have the meaning defined in the specification, have retinoid-like, retinoid antagonist or retinoid inverse agonist-like biological activity.
摘要翻译： 其中符号具有本说明书中定义的含义的式“IMAGE”的化合物具有类视黄醇样维生素A拮抗剂或类视色素反向激动剂样生物活性。
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55.发明授权Oxo-substituted tetrahydronaphthalene derivatives having retinold and/or retinoid antagonist-like biological activity 失效具有视黄醇和/或维生素A拮抗剂的生物活性的氧代取代的四氢萘衍生物
公开(公告)号：US5747542A
公开(公告)日：1998-05-05
申请号：US667666
申请日：1996-06-21
申请人： Vidyasagar Vuligonda , Alan T. Johnson , Richard L. Beard , Min Teng , Tae K. Song , Harold N. Wong , Roshantha A. Chandraratna
发明人： Vidyasagar Vuligonda , Alan T. Johnson , Richard L. Beard , Min Teng , Tae K. Song , Harold N. Wong , Roshantha A. Chandraratna
IPC分类号： C07C69/587 , C07C69/76 , C07C233/81 , C07C245/10 , C07C251/44 , C07C309/65 , C07C317/44 , C07C323/55 , C07D277/30 , C07D309/12 , C07D317/20 , C07D317/24 , C07D317/26 , C07D333/24 , C07D339/08 , C07D409/10 , A61K31/135 , A61K31/15 , A61K31/235 , A61K31/56 , C07C241/00 , C07D333/22
CPC分类号： C07D317/26 , C07C233/81 , C07C245/10 , C07C251/44 , C07C309/65 , C07C317/44 , C07C323/55 , C07C69/587 , C07C69/76 , C07D277/30 , C07D309/12 , C07D317/20 , C07D317/24 , C07D333/24 , C07D339/08 , C07D409/10 , C07C2102/10
摘要： Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
摘要翻译： 符号具有本申请中描述的含义的式“IMAGE”的化合物具有类视黄醇样或维生素A拮抗剂样生物活性。
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56.发明授权Benzo�1,2-g!-chrom-3-ene and benzo�1,2-g!-thiochrom-3-ene derivatives 失效苯并[1,2-g] - 色烯-3-烯和苯并[1,2-g] - 硫代色烯-3-烯衍生物
公开(公告)号：US5728846A
公开(公告)日：1998-03-17
申请号：US764466
申请日：1996-12-12
IPC分类号： A61K31/192 , A61K31/235 , A61K31/352 , A61K31/381 , A61K31/382 , A61K31/44 , A61P1/00 , A61P3/06 , A61P9/00 , A61P17/00 , A61P25/28 , A61P27/00 , A61P29/00 , A61P31/12 , A61P35/00 , A61P37/00 , A61P43/00 , C07C45/00 , C07C47/548 , C07C61/08 , C07C61/29 , C07C69/00 , C07C69/74 , C07C69/78 , C07C233/00 , C07D213/55 , C07D311/92 , C07D333/24 , C07D335/08 , C07D409/06 , C07D417/02 , C07F7/02 , C07F7/08 , C07D495/00 , A61K31/38 , C07D277/04 , C07D401/04
CPC分类号： C07C69/76 , C07C45/00 , C07C47/548 , C07D213/55 , C07D311/92 , C07D333/24 , C07D335/08 , C07D409/06 , C07C2103/24
摘要： Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist and/or retinoid inverse-agonist-like biological activity.
摘要翻译： 符号具有本说明书中定义的含义的式“IMAGE”的化合物具有类视黄醇，维生素A拮抗剂和/或维甲酸反相激动剂样生物活性。
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57.发明授权Acetylenes disubstituted with a 5 substituted tetrahydronaphthyl group and with an aryl or heteroaryl groups having retinoid-like biological activity 失效用5取代的四氢萘基和具有类视黄醇样生物活性的芳基或杂芳基二取代的乙炔
公开(公告)号：US5723620A
公开(公告)日：1998-03-03
申请号：US552813
申请日：1995-11-03
申请人： Vidyasagar Vuligonda , Min Teng , Richard L. Beard , Alan T. Johnson , Yuan Lin , Roshantha A. Chandraratna
发明人： Vidyasagar Vuligonda , Min Teng , Richard L. Beard , Alan T. Johnson , Yuan Lin , Roshantha A. Chandraratna
IPC分类号： C07C17/10 , C07C17/26 , C07C17/35 , C07C45/28 , C07C45/67 , C07C63/66 , C07C65/19 , C07C65/28 , 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 , C07D405/02
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 , C07C65/19 , C07C65/28 , 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： A compound of the formula ##STR1## wherein all variables are as defined in the specification having retinoid-like activity.
摘要翻译： 式（IMAGE）的化合物，其中所有变量如说明书中具有类视黄醇样活性的定义。
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58.发明授权Acetylenes disubstituted with a 5 substituted tetrahydronaphthyl group and with an aryl or heteroaryl groups having retinoid-like biological activity 失效用5取代的四氢萘基和具有类视黄醇样生物活性的芳基或杂芳基二取代的乙炔
公开(公告)号：US5654469A
公开(公告)日：1997-08-05
申请号：US656127
申请日：1996-05-31
申请人： Vidyasagar Vuligonda , Min Teng , Richard L. Beard , Alan T. Johnson , Yuan Lin , Roshantha A. Chandraratna
发明人： Vidyasagar Vuligonda , Min Teng , Richard L. Beard , Alan T. Johnson , Yuan Lin , Roshantha A. Chandraratna
IPC分类号： C07C17/10 , C07C17/26 , C07C17/35 , C07C45/28 , C07C45/67 , C07C63/66 , C07C65/19 , C07C65/28 , 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
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 , C07C65/19 , C07C65/28 , 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 Formula I ##STR1## wherein the symbols are as defined in the specification.
摘要翻译： 式Ⅰ化合物其中符号如说明书中所定义。
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59.发明授权Acetylenes disubstituted with a 5 substituted tetrahydronaphthyl group and with an aryl or heteroaryl group having retinoid-like biological activity 失效用5取代的四氢萘基和具有类视黄醇样生物活性的芳基或杂芳基二取代的乙炔
公开(公告)号：US5591858A
公开(公告)日：1997-01-07
申请号：US607737
申请日：1996-02-27
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 , C07D307/46 , C07D333/22
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 the symbols R.sub.1, R.sub.2, R.sub.3, R.sub.19, Y, A, B, m and o have the meaning described in the specification have retinoid like biological activity.
摘要翻译： 其中符号R1，R2，R3，R19，Y，A，B，m和o具有本说明书中描述的含义的式“IMAGE”的化合物具有类视黄醇类生物学活性。
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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.
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