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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：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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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：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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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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![7-[(7-Alkoxy)-chrom-3-en-6-yl]-heptatrienoic acid and 7-[(3-alkoxy)-5,6-dihydronaphthalen-2-yl]-heptatrienoic acid derivatives having serum glucose reducing activity](/abs-image/US/2005/05/03/US06887896B1/abs.jpg.150x150.jpg)
7.发明授权7-[(7-Alkoxy)-chrom-3-en-6-yl]-heptatrienoic acid and 7-[(3-alkoxy)-5,6-dihydronaphthalen-2-yl]-heptatrienoic acid derivatives having serum glucose reducing activity 失效7 - [（7-烷氧基） - 色烯-3-烯-6-基] - 庚三烯酸和具有血清葡萄糖降低的7 - [（3-烷氧基）-5,6-二氢萘-2-基] - 庚二酸衍生物 活动公开(公告)号：US06887896B1
公开(公告)日：2005-05-03
申请号：US10696748
申请日：2003-10-29
申请人： Richard L. Beard , Tien T. Duong , Janet A. Takeuchi , Ling Li , Kwok Yin Tsang , Xiaoxia Liu , Jayasree Vasudevan , Liming Wang , Santosh C. Sinha , Haiqing Yuan , Roshantha A. Chandraratna
发明人： Richard L. Beard , Tien T. Duong , Janet A. Takeuchi , Ling Li , Kwok Yin Tsang , Xiaoxia Liu , Jayasree Vasudevan , Liming Wang , Santosh C. Sinha , Haiqing Yuan , Roshantha A. Chandraratna
IPC分类号： A61K31/21 , A61K31/335 , C07C59/72 , C07C69/587 , C07C69/734 , C07D311/58 , A61K31/35 , A61K31/19 , A61K31/235
CPC分类号： C07C69/734 , C07C59/72 , C07C2601/02 , C07C2602/28 , C07D311/58
摘要： Compounds of the formula where the variations have the meaning defined in the specification are capable of reducing serum glucose levels in diabetic mammals without the undesirable side effects of transiently increasing triglyceride levels and reducing serum thyroxine levels.
摘要翻译： 其中变化具有本说明书中定义的含义的式的化合物能够降低糖尿病哺乳动物中的血清葡萄糖水平，而没有暂时增加甘油三酯水平和降低血清甲状腺素水平的不良副作用。
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![4-[(8-substituted)-6-chromanoyl]-and 4-[8-substituted)-chroman-6-YL-ethynyl]-benzoic and phenylacetic acids, their esters and salts having cytochrome P450RAI inhibitory activity](/abs-image/US/2008/04/01/US07351737B2/abs.jpg.150x150.jpg)
8.发明授权4-[(8-substituted)-6-chromanoyl]-and 4-[8-substituted)-chroman-6-YL-ethynyl]-benzoic and phenylacetic acids, their esters and salts having cytochrome P450RAI inhibitory activity 失效4 - [（8-取代的）-6-色酰基] - 和4- [8-取代的） - 苯并二氢吡喃-6-基] - 乙炔基] - 苯甲酸和苯乙酸，它们的酯和盐具有细胞色素P450RAI抑制活性公开(公告)号：US07351737B2
公开(公告)日：2008-04-01
申请号：US10389071
申请日：2003-03-14
申请人： Jayasree Vasudevan , Liming Wang , Xiaoxia Liu , Kwok-Yin Tsang , Yang-Dar Yuan , Roshantha A. Chandraratna
发明人： Jayasree Vasudevan , Liming Wang , Xiaoxia Liu , Kwok-Yin Tsang , Yang-Dar Yuan , Roshantha A. Chandraratna
IPC分类号： A61K31/352 , C07D311/76
CPC分类号： C07D311/58
摘要： Compounds of the formula where the variables are defined in the specification have cytochrome P450RAI-1 and P450RAI-2 inhibitory activity, and are suitable for treatment of mammals with conditions which are treatable with retinoids, or which are controlled by or responsive to the organism's native retinoic acid. Formulations containing the compounds of the invention can also be co-administered with retinoids and/or Vitamin A to enhance or prolong the effects of medications containing retinoids, Vitamin A, or of the organism's native retinoic acid.
摘要翻译： 其中变量在本说明书中定义的化合物具有细胞色素P450RAI-1和P450RAI-2抑制活性，并且适用于具有可用类视黄醇治疗的病症的哺乳动物的治疗，或由生物体的天然 视黄酸。 含有本发明化合物的制剂也可以与类维生素A和/或维生素A共同施用，以增强或延长含有类维生素A，维生素A或有机体天然视黄酸的药物的作用。
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公开(公告)号：US06380256B1
公开(公告)日：2002-04-30
申请号：US09651564
申请日：2000-08-29
IPC分类号： A61K3124
摘要： Compounds having Formula 4 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.
摘要翻译： 具有式4的化合物，其中符号具有本说明书中定义的含义是细胞色素P450RAI（视黄酸诱导型）酶的抑制剂，并且用于治疗响应于类视黄醇治疗的疾病。
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公开(公告)号：US06291677B1
公开(公告)日：2001-09-18
申请号：US09651001
申请日：2000-08-29
IPC分类号： C07D21514
CPC分类号： C07D221/20 , C07C59/72 , C07C65/28 , C07D215/14 , C07D217/04 , C07D311/58
摘要： Compounds having Formula 7 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.
摘要翻译： 具有式7的化合物，其中符号具有本说明书中定义的含义是细胞色素P450RAI（视黄酸诱导型）酶的抑制剂，并且用于治疗响应于类视黄醇治疗的疾病。
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