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1.发明授权Tetrahdroquinolin-2-one 6 or 7-yl, tetrahdroquinilin-2-thione 6 or 7-yl pentadienoic acid and related derivatives having retinoid-like biological activity 失效四氢喹啉-2-酮6或7-基，四氢喹啉-2-硫酮6或7-基戊二烯酸以及类视黄醇样生物活性的相关衍生物
公开(公告)号：US6048873A
公开(公告)日：2000-04-11
申请号：US164949
申请日：1998-10-01
IPC分类号： C07D215/12 , A61K20060101 , A61K31/47 , A61P1/04 , A61P3/00 , A61P3/06 , A61P5/10 , A61P9/00 , A61P17/00 , A61P17/14 , A61P25/00 , A61P25/16 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/12 , A61P35/00 , A61P37/02 , A61P39/02 , A61P43/00 , C07D20060101 , C07D215/00 , C07D215/22 , C07D215/36 , F61K31/47
CPC分类号： C07D215/12 , C07D215/22 , C07D215/36 , C07D405/04
摘要： Compounds of Formula 1 ##STR1## where Y is a bivalent radical having Formula 2 or Formula 3 where o is an integer from 1 to 4 ##STR2## where the remaining symbols have the meaning described in the specification are selective agonists of RXR retinoid receptors.
摘要翻译： 式1的化合物，其中Y是具有式2或式3的二价基团，其中o是1至4的整数，其中其余符号具有本说明书中描述的含义是RXR类视黄醇受体的选择性激动剂。
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2.发明授权2,4-pentadienoic acid derivatives having selective activity for retinoid X (RXR) receptors 失效对类视黄醇X（RXR）受体具有选择性活性的2,4-戊二烯酸衍生物公开(公告)号：US06403638B1
公开(公告)日：2002-06-11
申请号：US09532677
申请日：2000-03-21
IPC分类号： A61K3121
CPC分类号： C07D311/58 , C07C57/48 , C07C57/50 , C07C69/618 , C07C2601/02 , C07C2602/10 , C07C2603/74
摘要： Compounds having the formulas below, where R is H, lower alkyl, or a pharmaceutically acceptable salt, and where R1 represents i-propyl, t-butyl or n-butyl groups, have selective RXR retionoid agonist activity.
摘要翻译： 具有下式的化合物，其中R为H，低级烷基或其药学上可接受的盐，并且其中R 1表示异丙基，叔丁基或正丁基，具有选择性RXR铰链型激动剂活性。
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3.发明授权2,4-pentadienoic acid derivatives having selective activity for retinoid X (RXR) receptors 失效对类视黄醇X（RXR）受体具有选择性活性的2,4-戊二烯酸衍生物
公开(公告)号：US6147224A
公开(公告)日：2000-11-14
申请号：US164950
申请日：1998-10-01
IPC分类号： A61K31/201 , A61K31/231 , A61K31/352 , A61P1/00 , A61P3/02 , A61P3/06 , A61P5/06 , A61P9/00 , A61P11/00 , A61P17/00 , A61P17/04 , A61P17/06 , A61P17/10 , A61P17/14 , A61P17/16 , A61P25/16 , A61P25/28 , A61P27/02 , A61P35/00 , A61P37/02 , A61P43/00 , C07C57/48 , C07C57/50 , C07C69/00 , C07C69/618 , C07D311/58 , C07D295/00 , C07D233/00 , C07D303/08 , C07D311/80 , C07D45/00
CPC分类号： C07D311/58 , C07C57/48 , C07C57/50 , C07C69/618 , C07C2101/02 , C07C2102/10 , C07C2103/74
摘要： Compounds of Formula 1, Formula 2 or Formula 3 where X is O, S, or (CR.sub.1 R.sub.1).sub.n where n is 0, 1 or 2; Y is a bivalent radical having Formula 4 or Formula 5 where o is an integer from 1 to 4 ##STR1## or Y is a bivalent aryl or 5 or 6 membered heteroaryl radical having 1 to 3 heteroatoms selected from N, S and O, said aryl or heteroaryl groups being unsubstituted, or substituted with 1 to 3 C.sub.1-6 alkyl or with 1 to 3 C.sub.1-6 fluoroalkyl groups; and the remaining symbols have the meaning described in the specification, have RXR selective retinoid agonist-like activity.
摘要翻译： X为O，S或（CR1R1）n的式1，式2或式3化合物，其中n为0,1或2; Y是具有式4或式5的二价基团，其中o是1至4的整数或Y是二价芳基或具有1至3个选自N，S和O的杂原子的5或6元杂芳基，所述芳基或杂芳基 取代的基团，或被1至3个C 1-6烷基或1至3个C 1-6氟烷基取代; 并且其余符号具有说明书中描述的含义，具有RXR选择性类维生素A激动剂样活性。
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4.发明授权Compounds having selective cytochrome P450RAI-1 or selective cytochrome P450RAI-2 inhibitory activity and methods of obtaining the same 失效具有选择性细胞色素P450RAI-1或选择性细胞色素P450RAI-2抑制活性的化合物及其获得方法公开(公告)号：US07638648B2
公开(公告)日：2009-12-29
申请号：US11728313
申请日：2007-03-23
申请人： Jayasree Vasudevan , Liming Wang , Xiaoxia Liu , Kwok Yin Tsang , Ling Li , Janet A. Takeuchi , Thong Vu , Richard Beard , Smita Bhat , Vidyasagar Vuligonda , Roshantha A. Chandraratna
发明人： Jayasree Vasudevan , Liming Wang , Xiaoxia Liu , Kwok Yin Tsang , Ling Li , Janet A. Takeuchi , Thong Vu , Richard Beard , Smita Bhat , Vidyasagar Vuligonda , Roshantha A. Chandraratna
IPC分类号： C07D265/06 , C07D263/02 , C07D277/02 , C07D213/02 , C07D333/04 , C07D307/34 , C07C229/34
CPC分类号： C07C69/73 , C07C57/42 , C07C59/64 , C07C59/86 , C07C69/753 , C07C69/76 , C07C229/34 , C07C229/38 , C07C229/46 , C07C229/50 , C07C275/42 , C07C2601/02 , C07C2602/10 , C07D311/58 , C07D311/64 , C07D311/96
摘要： Compounds of formulas 1 through 17 provided in the specification specifically or selectively inhibit either the cytochrome P450RAI-1 enzyme or the cytochrome P450RAI-2 enzyme.
摘要翻译： 本说明书中提供的式1至17的化合物具体地或选择性地抑制细胞色素P450RAI-1酶或细胞色素P450RAI-2酶。
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5.发明授权Compounds having selective cytochrome P450RAI-1 or selective cytochrome P450RAI-2 inhibitory activity and methods of obtaining the same 失效具有选择性细胞色素P450RAI-1或选择性细胞色素P450RAI-2抑制活性的化合物及其获得方法公开(公告)号：US07226951B2
公开(公告)日：2007-06-05
申请号：US11014460
申请日：2004-12-16
申请人： Jayasree Vasudevan , Liming Wang , Xiaoxia Liu , Kwok Yin Tsang , Ling Li , Janet A. Takeuchi , Thong Vu , Richard Beard , Smita Bhat , Vidyasagar Vuligonda , Roshantha A. Chandraratna
发明人： Jayasree Vasudevan , Liming Wang , Xiaoxia Liu , Kwok Yin Tsang , Ling Li , Janet A. Takeuchi , Thong Vu , Richard Beard , Smita Bhat , Vidyasagar Vuligonda , Roshantha A. Chandraratna
IPC分类号： A61K31/135 , C07C62/00 , C07C69/52 , C07C211/16
CPC分类号： C07C69/73 , C07C57/42 , C07C59/64 , C07C59/86 , C07C69/753 , C07C69/76 , C07C229/34 , C07C229/38 , C07C229/46 , C07C229/50 , C07C275/42 , C07C2601/02 , C07C2602/10 , C07D311/58 , C07D311/64 , C07D311/96
摘要： Compounds of formulas 1 through 17 provided in the specification specifically or selectively inhibit either the cytochrome P450RAI-1 enzyme or the cytochrome P450RAI-2 enzyme.
摘要翻译： 在说明书中提供的式1至17的化合物具体地或选择性地抑制细胞色素P450RAI-1酶或细胞色素P450RAI-2酶。
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6.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：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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7.发明授权
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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8.发明授权O- or S-substituted dihydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity 失效具有类视黄醇和/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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9.发明授权Amines substituted with a dihydronaphthalenyl, chromenyl, or thiochromenyl group, a pyridyl group and an alkyl group, having retinoid-like biological activity 失效被二氢萘基，色烯基或硫代色烯基取代的胺，吡啶基和烷基，具有类视黄醇样生物活性公开(公告)号：US07026487B2
公开(公告)日：2006-04-11
申请号：US10612667
申请日：2003-07-02
申请人： Richard L. Beard , Thong Vu , Diana F. Colon , Vidyasagar Vuligonda , Roshantha A. Chandraratna
发明人： Richard L. Beard , Thong Vu , Diana F. Colon , Vidyasagar Vuligonda , Roshantha A. Chandraratna
IPC分类号： C07D213/74 , C07D407/12 , C07D409/12
CPC分类号： C07D335/06 , C07C229/60 , C07C2602/10 , C07D311/20
摘要： Compounds of the formula where the symbols are as defined in the specification, have retinoid agonist, antagonist or negative hormone-like biological activity.
摘要翻译： 其中符号如说明书中所定义的式的化合物具有类视黄醇激动剂，拮抗剂或负激素样生物活性。
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10.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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