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1.Acetylenes disubstituted with a 5 OXO substituted tetrahydronaphthyl group and with an aryl or heteroaryl group having retinoid-like biological activity 失效
标题翻译: 用5 OXO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:US5618943A
公开(公告)日:1997-04-08
申请号:US366167
申请日:1994-12-29
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: C07C17/10 , C07C17/26 , C07C17/35 , C07C45/28 , C07C45/67 , C07C63/66 , 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 , C07D213/02 , C07C233/81
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 , 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## the symbols have the meaning described in the specification have retinoid-like biological activity.
摘要翻译: 化学式“IMAGE”符号具有本说明书中描述的含义,具有类视黄醇样生物活性。
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2.Oxo-substituted tetrahydronaphthalene derivatives having retinold and/or retinoid antagonist-like biological activity 失效
标题翻译: 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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3.Acetylenes disubstituted with a 5 substituted tetrahydronaphthyl group and with an aryl or heteroaryl group having retinoid-like biological activity 失效
标题翻译: 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:US5648503A
公开(公告)日:1997-07-15
申请号:US656134
申请日:1996-05-31
申请人: Vidyasagar Vuligonda , Richard L. Beard , Alan T. Johnson , Min Teng , Tae K. Song , Roshantha A. Chandraratna
发明人: Vidyasagar Vuligonda , Richard L. Beard , Alan T. Johnson , Min Teng , Tae K. Song , Roshantha A. Chandraratna
IPC分类号: C07C17/10 , C07C17/26 , C07C17/35 , C07C45/28 , C07C45/67 , C07C45/68 , C07C49/697 , C07C59/86 , C07C63/66 , 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 , C07D307/06 , C07D309/04 , C07D333/08 , C07D335/02
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 , C07C45/68 , C07C49/697 , C07C59/86 , C07C63/66 , 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## which have retinoid-like biological activity.
摘要翻译: 具有类视黄醇样生物活性的式“IMAGE”的化合物。
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4.Acetylenes disubstituted with a 5 substituted tetrahydronaphthyl group and with an aryl or heteroaryl group having retinoid-like biological activity 失效
标题翻译: 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:US5605915A
公开(公告)日:1997-02-25
申请号:US656135
申请日:1996-05-31
申请人: Vidyasagar Vuligonda , Richard L. Beard , Alan T. Johnson , Min Teng , Tae K. Song , Roshantha A. Chandraratna
发明人: Vidyasagar Vuligonda , Richard L. Beard , Alan T. Johnson , Min Teng , Tae K. Song , Roshantha A. Chandraratna
IPC分类号: C07C17/10 , C07C17/26 , C07C17/35 , C07C45/28 , C07C45/67 , C07C45/68 , C07C49/697 , C07C59/86 , C07C63/66 , 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 , A61K31/44 , C07D213/44
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 , C07C45/68 , C07C49/697 , C07C59/86 , C07C63/66 , 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 have the meaning defined in the specification.
摘要翻译: 式“IMAGE”的化合物,其中符号具有本说明书中定义的含义。
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5.Acetylenes disubstituted with a 5 substituted tetrahydronaphthyl group and with an aryl of heteroaryl group having retinoid-like biological activity 失效
标题翻译: 用5取代的四氢萘基和与类视黄醇样生物活性的杂芳基的芳基二取代的乙炔公开(公告)号:US5599967A
公开(公告)日:1997-02-04
申请号:US366169
申请日:1994-12-29
申请人: Vidyasagar Vuligonda , Richard L. Beard , Alan T. Johnson , Min Teng , Tae K. Song , Roshantha A. Chandraratna
发明人: Vidyasagar Vuligonda , Richard L. Beard , Alan T. Johnson , Min Teng , Tae K. Song , Roshantha A. Chandraratna
IPC分类号: C07C17/10 , C07C17/26 , C07C17/35 , C07C45/28 , C07C45/67 , C07C45/68 , C07C49/697 , C07C59/86 , C07C63/66 , 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 , C07C45/68 , C07C49/697 , C07C59/86 , C07C63/66 , 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 have the meaning defined in the specification have retinoid-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生物活性。
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6.Oxime substituted tetrahydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity 失效
标题翻译: 具有类视黄醇和/或类视黄醇拮抗剂的生物活性的肟取代的四氢萘衍生物公开(公告)号:US5723666A
公开(公告)日:1998-03-03
申请号:US667215
申请日:1996-06-21
申请人: Vidyasagar Vuligonda , Richard L. Beard , Alan T. Johnson , Min Teng , Tae K. Song , Roshantha A. Chandraratna
发明人: Vidyasagar Vuligonda , Richard L. Beard , Alan T. Johnson , Min Teng , Tae K. Song , 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 , C07C249/00 , C07C229/00 , C07C251/00 , C07C263/00 , C07C291/00 , C07F7/04
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## have retinoid-like or retinoid antagonist-like biological activity.
摘要翻译: 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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7.Alkyl or aryl substituted dihydronaphthalene derivatives having retinoid and/or retinoid antagonist like biological activity 失效
标题翻译: 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:US6117987A
公开(公告)日:2000-09-12
申请号:US57386
申请日:1998-04-08
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 describedin 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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8.
公开(公告)号:US5877207A
公开(公告)日:1999-03-02
申请号:US880823
申请日:1997-06-24
申请人: Elliott S. Klein , Alan T. Johnson , Andrew M. Standeven , Richard L. Beard , Samuel J. Gillett , Tien T. Duong , Sunil Nagpal , Vidyasagar Vuligonda , Min Teng , Roshantha A. Chandraratna
发明人: Elliott S. Klein , Alan T. Johnson , Andrew M. Standeven , Richard L. Beard , Samuel J. Gillett , Tien T. Duong , Sunil Nagpal , Vidyasagar Vuligonda , Min Teng , Roshantha A. Chandraratna
IPC分类号: C07D333/24 , A61K31/245 , A61K31/353 , A61K31/381 , A61P3/10 , A61P17/16 , A61P19/08 , A61P39/02 , A61P43/00 , C07C57/50 , C07C63/33 , C07C63/49 , C07C63/66 , C07C63/72 , C07C63/74 , C07C65/19 , C07C65/28 , C07C65/38 , C07C69/618 , C07C69/76 , C07C69/90 , C07C69/94 , C07C233/81 , C07C233/87 , C07C245/10 , C07C327/48 , C07D213/55 , C07D277/30 , C07D307/54 , C07D311/58 , C07D335/06 , C07F7/08 , C07F7/18 , A61K31/35 , C07D311/04
CPC分类号: C07C57/50 , C07C233/81 , C07C233/87 , C07C245/10 , C07C327/48 , C07C63/33 , C07C63/49 , C07C63/66 , C07C63/72 , C07C63/74 , C07C65/19 , C07C65/28 , C07C65/38 , C07C69/618 , C07C69/76 , C07C69/90 , C07C69/94 , C07D213/55 , C07D277/30 , C07D307/54 , C07D311/58 , C07D333/24 , C07D335/06 , C07F7/0818 , C07C2102/10 , C07C2102/28
摘要: Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity. These assays are based on the ability of negative hormones to down-regulate the activity of chimeric retinoid receptors engineered to possess a constitutive transcription activator domain.
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9.O- or S-substituted dihydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity 失效
标题翻译: 具有类视黄醇和/或类视黄醇拮抗剂的生物活性的O-或S-取代的二氢萘衍生物公开(公告)号:US5808124A
公开(公告)日:1998-09-15
申请号:US667216
申请日:1996-06-21
申请人: Richard L. Beard , Min Teng , Alan T. Johnson , Vidyasagar Vuligonda , Roshantha A. Chandraratna
发明人: Richard L. Beard , Min Teng , Alan T. Johnson , Vidyasagar Vuligonda , 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 , C07F7/04 , C07F7/08 , C07F7/10
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拮抗剂样的生物活性。
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10.O- or S-substituted tetrahydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity 失效
标题翻译: 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:US06855832B2
公开(公告)日:2005-02-15
申请号:US10269270
申请日:2002-10-11
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: A01N33/26 , A61K31/655 , C07C61/10 , C07C61/16 , C07C62/00 , C07C69/02 , C07C69/587 , C07C69/76 , C07C69/95 , C07C233/81 , C07C245/10 , C07C251/44 , C07C291/00 , C07C309/65 , C07C317/44 , C07C323/55 , C07D211/70 , C07D211/78 , C07D211/82 , C07D277/30 , C07D309/12 , C07D311/00 , C07D311/04 , C07D317/20 , C07D317/24 , C07D317/26 , C07D333/24 , C07D335/04 , C07D339/08 , C07D409/10 , C09B29/033 , C09B29/09 , C09B29/22 , C09B29/36
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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