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21.发明授权Tetrahydronaphthalene derivatives substituted in the 8 position with alkyhidene groups having retinoid and/or retinoid antagonist-like biological activity 失效在八位上被取代为具有类视黄醇和/或维生素A拮抗剂样生物活性的亚烷基的四氢萘衍生物
公开(公告)号：US5763635A
公开(公告)日：1998-06-09
申请号：US667665
申请日：1996-06-21
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 , C07F7/04 , C07C229/60 , C07C233/65
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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22.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：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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23.发明授权Acetylenes disubstituted with a phenyl or heteroaryl group and a 2-thio-1,2,3,4-tetrahdroquinolinyl, 2-alkylthio-3,4-dihydroquinolinyl or 2-alkoxy-3,4-dihydroquinolinyl group having retinoid-like biological activity 失效具有类视黄醇样生物活性的苯基或杂芳基二取代的2-乙烯基和2-硫代-1,2,3,4-四氢喹啉基，2-烷硫基-3,4-二氢喹啉基或2-烷氧基-3,4-二氢喹啉基
公开(公告)号：US5616712A
公开(公告)日：1997-04-01
申请号：US442223
申请日：1995-05-16
IPC分类号： C07D215/22 , A61K31/47 , A61P3/02 , C07D215/227 , C07D215/36 , C07D215/38
CPC分类号： C07D215/227 , C07D215/36
摘要： Compounds of the formula ##STR1## where the symbols are defined as in the specification.
摘要翻译： 其中符号在说明书中定义的式“IMAGE”的化合物。
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24.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：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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25.发明授权Acetylenes disubstituted with a 5 substituted tetrahydronaphthyl group and with an aryl of heteroaryl group having retinoid-like biological activity 失效用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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26.发明授权Oxiranyls disubstituted with a phenyl group and a substituted chromanyl or tetrahydroquinolinyl group having retinoid like activity 失效被苯基二取代的环氧乙烷基和具有类视黄醇样活性的取代的色满基或四氢喹啉基
公开(公告)号：US5556996A
公开(公告)日：1996-09-17
申请号：US366174
申请日：1994-12-29
IPC分类号： C07D311/04 , C07D407/04 , C07D311/58
CPC分类号： C07D407/04 , C07D311/04
摘要： Compounds of the formula ##STR1## wherein all the symbols in the formula are as defined in the specification, have retinoid-like activity.
摘要翻译： 其中式中所有符号如说明书中所定义的式“IMAGE”的化合物具有类视黄醇样活性。
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27.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：US06818775B2
公开(公告)日：2004-11-16
申请号：US10731448
申请日：2003-12-09
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： C07D1172
CPC分类号： C07D317/24 , C07C69/587 , C07C69/76 , C07C233/81 , C07C245/10 , C07C251/44 , C07C309/65 , C07C317/44 , C07C323/55 , C07C2602/10 , C07D277/30 , C07D309/12 , C07D317/20 , C07D317/26 , C07D333/24 , C07D339/08 , 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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公开(公告)号：US06653483B1
公开(公告)日：2003-11-25
申请号：US09550952
申请日：2000-04-17
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： C07D21372
CPC分类号： C07D409/10 , C07C69/587 , C07C69/76 , C07C233/81 , C07C245/10 , C07C251/44 , C07C309/65 , C07C317/44 , C07C323/55 , C07C2602/10 , C07D277/30 , C07D309/12 , C07D317/20 , C07D317/24 , C07D317/26 , C07D333/24 , C07D339/08
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.
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29.发明授权Amines substituted with a dihydro-benzofuranyl or with a dihydro-isobenzofuranyl group, an aryl or heteroaryl group and an alkyl group, having retinoid-like biological activity 失效被二氢苯并呋喃基或与二氢异苯并呋喃基，芳基或杂芳基和烷基取代的胺具有类视黄醇样生物活性
公开(公告)号：US6093838A
公开(公告)日：2000-07-25
申请号：US375845
申请日：1999-08-16
IPC分类号： A61K31/343 , A61P1/00 , A61P5/38 , A61P7/00 , A61P9/00 , A61P11/00 , A61P13/00 , A61P15/00 , A61P17/00 , A61P17/06 , A61P17/10 , A61P17/12 , A61P27/02 , A61P31/04 , A61P35/00 , A61P37/08 , A61P43/00 , C07D307/79 , C07D307/87 , C07D307/78 , C07D409/00
CPC分类号： C07D307/79 , C07D307/87
摘要： Compounds of Formula 1 and of Formula 2 ##STR1## where the symbols have the meaning defined in the specification, have retinoid-like biological activity.
摘要翻译： 符号具有本说明书中定义的含义的式1和式2化合物具有类视黄醇样生物活性。
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30.发明授权
公开(公告)号：US6090810A
公开(公告)日：2000-07-18
申请号：US222984
申请日：1998-12-30
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： A61K31/165 , A61K31/19 , A61K31/216 , A61K31/35 , A61K31/353 , A61K31/38 , A61K31/382 , A61K31/47 , A61K31/495 , A61K31/655 , C07C57/50 , C07C63/06 , 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 , C07C245/10 , C07C327/48 , C07D213/55 , C07D215/14 , C07D277/30 , C07D307/54 , C07D311/04 , C07D311/58 , C07D333/24 , C07D335/06 , C07D401/12 , C07D405/06 , C07D409/14 , C07F7/04 , C07F7/08
CPC分类号： C07C57/50 , C07C233/81 , 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 , C07D333/24 , C07D335/06 , C07D409/04 , C07D417/04 , C07F7/0818 , C07C2102/10
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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