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51.发明授权Synthesis and use of retinoid compounds having negative hormone and/or anatgonist activities 失效合成和使用具有负激素和/或阴离子活性的类视黄醇化合物公开(公告)号：US06469028B1
公开(公告)日：2002-10-22
申请号：US09821673
申请日：2001-03-28
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： C07D21514
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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52.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：US06465663B2
公开(公告)日：2002-10-15
申请号：US09900593
申请日：2001-07-06
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： C07D40900
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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53.发明授权Oxygen, sulfur and nitrogen substituted cyclohexene and cyclohexane derivatives having retinoid-like biological activity 失效氧，硫和氮取代的环己烯和具有类视黄醇样生物活性的环己烷衍生物公开(公告)号：US06465647B1
公开(公告)日：2002-10-15
申请号：US09634727
申请日：2000-08-04
IPC分类号： C07D23702
CPC分类号： C07C403/02 , C07C69/76 , C07C2601/14 , C07F7/081 , C07F7/0812
摘要： Compounds of the Formula 1, Formula 2, Formula 3 and Formula 4 wherein the symbols have the meaning assigned to them in the disclosure have retinoid-like biological activity.
摘要翻译： 式1，式2，式3和式4的化合物，其中符号具有本公开中赋予它们的含义具有类视色素样生物活性。
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54.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 WITH AN ARYL OR HETEROARYL GROUP HAVING RETINOID-LIKE BIOLOGICAL ACTIVITY 失效用5种亚烷基，芳基或杂芳基取代的二氢噻吩基团和与具有类似生物活性的芳族或异构体具有类似性的ARYL或HETEROARYL类发生的乙酰胺公开(公告)号：US06355806B1
公开(公告)日：2002-03-12
申请号：US09398613
申请日：1999-09-16
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： C07D21170
CPC分类号： C07D213/80 , C07C17/10 , C07C17/263 , C07C17/35 , C07C45/28 , C07C45/673 , C07C63/66 , C07C69/76 , C07C229/46 , C07C233/58 , C07C251/48 , C07C255/41 , C07C255/47 , C07C309/65 , C07C323/61 , C07C327/32 , C07C2602/10 , C07D213/55 , C07D277/30 , C07D307/54 , C07D309/06 , C07D309/12 , C07D333/24 , C07D339/08 , C07F7/081 , C07F7/1804 , C07C25/22 , C07C25/24 , C07C49/697 , C07C49/683
摘要： Compounds of the formula wherein the symbols have the meaning described in the specification, have retinoid-like biological activity.
摘要翻译： 符号表示的化合物具有说明书中描述的含义，具有类视黄醇样生物活性。
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55.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：US06344561B2
公开(公告)日：2002-02-05
申请号：US09735172
申请日：2000-12-11
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： C07D21170
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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56.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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57.发明授权Amines substituted with a tetrahydroquinolinyl group an aryl or heteroaryl group and an alkyl group, having retinoid-like biological activity 失效被四氢喹啉基取代为具有类视黄醇样生物活性的芳基或杂芳基和烷基的胺
公开(公告)号：US6127382A
公开(公告)日：2000-10-03
申请号：US375846
申请日：1999-08-16
IPC分类号： A61K31/47 , A61K31/4704 , A61P1/00 , A61P1/04 , A61P3/06 , A61P3/10 , A61P5/06 , A61P5/44 , A61P11/00 , A61P17/00 , A61P17/02 , A61P17/06 , A61P17/12 , A61P17/14 , A61P25/16 , A61P25/28 , A61P27/02 , A61P29/00 , A61P35/00 , A61P37/04 , A61P37/06 , A61P43/00 , C07D215/38 , C07D215/00 , C07D215/16 , C07D215/20 , C07D401/00
CPC分类号： C07D215/38
摘要： Compound of Formula 1 ##STR1## where the symbols have the meaning described in the specification, have retinoid-like biological activity.
摘要翻译： 符号具有说明书中描述的含义的式1化合物具有类视黄醇样生物活性。
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58.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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59.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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60.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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