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31.发明授权Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities 失效具有负激素和/或拮抗剂活性的类视黄醇化合物的合成和用途公开(公告)号：US06228848B1
公开(公告)日：2001-05-08
申请号：US09447082
申请日：1999-11-22
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： C07C6306
CPC分类号： C07D335/06 , 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 , C07C245/10 , C07C327/48 , C07C2602/10 , C07D213/55 , C07D277/30 , C07D307/54 , C07D333/24 , C07D409/04 , C07D417/04 , C07F7/081
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.
摘要翻译： 芳基取代的和芳基和（3-氧代-1-丙烯基）取代的苯并吡喃，苯并噻喃，1,2-二氢喹啉和5,6-二氢萘衍生物具有类视黄醇阴性激素和/或拮抗剂样生物活性。 本发明的RAR拮抗剂可以施用于包括人在内的哺乳动物，以预防或减少RAR激动剂在结合受体位点上的作用。 具体来说，RAR激动剂与类视黄醇药物一起施用或共同施用以预防或改善由类维生素A或维生素A或维生素A前体引起的毒性或副作用。 类视黄醇阴性激素可用于增强其他类维生素A和核受体激动剂的活性。 例如，称为AGN 193109的类视黄醇阴性激素有效地增加了体外反式激活测定中其他类维生素A和类固醇激素的有效性。 另外，反式激活测定可用于鉴定具有负激素活性的化合物。 这些测定是基于负激素下调修饰的具有组成型转录激活子结构域的嵌合维甲酸受体的活性的能力。
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32.发明授权
公开(公告)号：US5952345A
公开(公告)日：1999-09-14
申请号：US871093
申请日：1997-06-09
申请人： Elliot 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： Elliot 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 , C07D215/16
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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33.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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34.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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35.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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36.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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37.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：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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公开(公告)号：US06720425B2
公开(公告)日：2004-04-13
申请号：US10314758
申请日：2002-12-09
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： C07D21304
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.
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39.发明授权Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities 失效具有负激素和/或拮抗剂活性的类视黄醇化合物的合成和用途
公开(公告)号：US5958954A
公开(公告)日：1999-09-28
申请号：US998319
申请日：1997-12-24
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： A61K31/165 , A61K31/19 , A61K31/192 , A61K31/216 , A61K31/341 , A61K31/35 , A61K31/352 , A61K31/353 , A61K31/382 , A61K31/426 , A61K31/427 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4418 , A61K31/4433 , A61K31/4436 , A61K31/47 , A61K31/655 , A61P3/06 , A61P17/00 , A61P19/00 , A61P25/04 , A61P39/02 , C07C63/06 , C07C65/38 , C07C69/78 , C07C233/65 , C07D213/55 , C07D215/14 , C07D233/66 , C07D277/20 , C07D277/30 , C07D307/54 , C07D311/04 , C07D311/58 , C07D333/24 , C07D335/06 , C07D401/12 , C07D405/06 , C07D409/04 , C07D409/14 , C07D417/04 , C07F7/04
CPC分类号： C07D335/06 , C07D213/55 , C07D277/30 , C07D307/54 , C07D311/58 , C07D333/24 , C07D409/04 , C07D417/04
摘要： 2,2-Dialkyl-4-aryl-substituted benzopyran and benzothiopyran derivatives of the formula ##STR1## where the symbols have the meaning described in the specification, 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.
摘要翻译： 式中的2,2-二烷基-4-芳基取代的苯并吡喃和苯并噻喃衍生物，其中符号具有说明书中描述的含义，具有类视黄醇阴性激素和/或拮抗剂样生物活性。 本发明的RAR拮抗剂可以施用于包括人在内的哺乳动物，以预防或减少RAR激动剂在结合受体位点上的作用。 具体来说，RAR激动剂与类视黄醇药物一起施用或共同施用以预防或改善由类维生素A或维生素A或维生素A前体引起的毒性或副作用。 类视黄醇阴性激素可用于增强其他类维生素A和核受体激动剂的活性。
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40.发明授权Acetylenes disubstituted with a 5 alkyl, aryl or heteroaryl substituted dihydronaphthyl group and with an aryl or heteroaryl group having retinoid-like biological activity 失效用5个烷基，芳基或杂芳基取代的二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：US5808083A
公开(公告)日：1998-09-15
申请号：US854297
申请日：1997-05-12
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： 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 , C07D277/22 , C07D277/30 , C07D307/54 , C07D309/06 , C07D309/12 , C07D333/24 , C07D339/08 , C07F7/08 , C07F7/18 , C07D213/04 , C07D333/04 , C07D307/36
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## wherein the symbols have the meaning described in the specification, have retinoid-like biological activity.
摘要翻译： 其中符号具有说明书中描述的含义的式“IMAGE”的化合物具有类视黄醇样生物活性。
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