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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)
1.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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2.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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![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)
3.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.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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5.发明授权Methods for treating retinoid responsive disorders using selective inhibitors of CYP26A and CYP26B 失效使用CYP26A和CYP26B的选择性抑制剂治疗类视黄醇应答障碍的方法公开(公告)号：US07468391B2
公开(公告)日：2008-12-23
申请号：US11010953
申请日：2004-12-13
申请人： Jayasree Vasudevan , Rong Yang , Liming Wang , Xiaoxia Liu , Kwok-Yin Tsang , Ling Li , Janet Takeuchi , Thong Vu , Richard Beard , Smita Bhat , Roshantha A. Chandraratna
发明人： Jayasree Vasudevan , Rong Yang , Liming Wang , Xiaoxia Liu , Kwok-Yin Tsang , Ling Li , Janet Takeuchi , Thong Vu , Richard Beard , Smita Bhat , Roshantha A. Chandraratna
IPC分类号： A01N31/00 , A61K9/00 , A61K31/415 , A61K9/20 , A61K9/48
CPC分类号： A61K31/19 , A61K31/192 , A61K31/35 , A61K31/38
摘要： The invention provides methods for treating an individual having a retinoid responsive disorder. In one embodiment, a method involves administering to the individual an effective amount of a selective CYP26B inhibitor, the selective CYP26B inhibitor having at least 10-fold selectivity for CYP26B relative to CYP26A. In another embodiment, a method involves administering to the individual an effective amount of a selective CYP26A inhibitor, the selective CYP26A inhibitor having a chemical formula set forth in the specification. The invention further provides screening methods for identifying a selective CYP26A inhibitor or selective CYP26B inhibitor.
摘要翻译： 本发明提供了治疗患有类视黄醇反应性障碍的个体的方法。 在一个实施方案中，一种方法涉及向个体施用有效量的选择性CYP26B抑制剂，所述选择性CYP26B抑制剂相对于CYP26A对CYP26B具有至少10倍的选择性。 在另一个实施方案中，一种方法包括向个体施用有效量的选择性CYP26A抑制剂，该选择性CYP26A抑制剂具有说明书中阐述的化学式。 本发明还提供用于鉴定选择性CYP26A抑制剂或选择性CYP26B抑制剂的筛选方法。
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![4-[(8-ETHYNYL, 8-VINYL OR 8-ETHYNYL-METHYL)-6-CHROMANOYL]-BENZOIC AND 2-[4-[(8-ETHYNYL, 8-VINYL OR 8-ETHYNYL-METHYL)-6-CHROMANOYL]-PHENYL]-ACETIC ACID, THEIR ESTERS AND SALTS HAVING CYTOCHROME P450RAI INHIBITORY ACTIVITY](/abs-image/US/2004/05/25/US06740676B2/abs.jpg.150x150.jpg)
6.发明授权4-[(8-ETHYNYL, 8-VINYL OR 8-ETHYNYL-METHYL)-6-CHROMANOYL]-BENZOIC AND 2-[4-[(8-ETHYNYL, 8-VINYL OR 8-ETHYNYL-METHYL)-6-CHROMANOYL]-PHENYL]-ACETIC ACID, THEIR ESTERS AND SALTS HAVING CYTOCHROME P450RAI INHIBITORY ACTIVITY 失效4 - [（8-乙基，8-乙烯基或8-乙酰基 - 甲基）-6-氯苯基] - 苯基和2- [4 - [（8-乙酰基，8-乙烯基或8-乙酰基 - 甲基） 色氨酸] - 苯甲酸，其酯和具有细胞色素P450RAI抑制活性的盐公开(公告)号：US06740676B2
公开(公告)日：2004-05-25
申请号：US10100638
申请日：2002-03-19
申请人： Jayasree Vasudevan , Liming Wang , Xiaoxia Liu , Kwok-Yin Tsang , Yang-Dar Yuan , Roshantha S. Chandraratna
发明人： Jayasree Vasudevan , Liming Wang , Xiaoxia Liu , Kwok-Yin Tsang , Yang-Dar Yuan , Roshantha S. Chandraratna
IPC分类号： A61K3135
CPC分类号： C07D311/58
摘要： Compounds of Formula 1: wherein 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： 式1的化合物：其中变量在本说明书中定义为具有细胞色素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或由生物体 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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7.发明申请Methods for treating retinoid responsive disorders using selective inhibitors of CYP26A and CYP26B 失效使用CYP26A和CYP26B的选择性抑制剂治疗类视黄醇应答障碍的方法公开(公告)号：US20050187298A1
公开(公告)日：2005-08-25
申请号：US11010953
申请日：2004-12-13
申请人： Jayasree Vasudevan , Rong Yang , Liming Wang , Xiaoxia Liu , Kwok-Yin Tsang , Ling Li , Janet Takeuchi , Thong Vu , Richard Beard , Smita Bhat , Roshantha Chandraratna
发明人： Jayasree Vasudevan , Rong Yang , Liming Wang , Xiaoxia Liu , Kwok-Yin Tsang , Ling Li , Janet Takeuchi , Thong Vu , Richard Beard , Smita Bhat , Roshantha Chandraratna
IPC分类号： A61K31/19 , A61K31/192 , A61K31/35 , A61K31/38
CPC分类号： A61K31/19 , A61K31/192 , A61K31/35 , A61K31/38
摘要： The invention provides methods for treating an individual having a retinoid responsive disorder. In one embodiment, a method involves administering to the individual an effective amount of a selective CYP26B inhibitor, the selective CYP26B inhibitor having at least 10-fold selectivity for CYP26B relative to CYP26A. In another embodiment, a method involves administering to the individual an effective amount of a selective CYP26A inhibitor, the selective CYP26A inhibitor having a chemical formula set forth in the specification. The invention further provides screening methods for identifying a selective CYP26A inhibitor or selective CYP26B inhibitor.
摘要翻译： 本发明提供了治疗患有类视黄醇反应性障碍的个体的方法。 在一个实施方案中，一种方法涉及向个体施用有效量的选择性CYP26B抑制剂，所述选择性CYP26B抑制剂相对于CYP26A对CYP26B具有至少10倍的选择性。 在另一个实施方案中，一种方法包括向个体施用有效量的选择性CYP26A抑制剂，该选择性CYP26A抑制剂具有说明书中阐述的化学式。 本发明还提供用于鉴定选择性CYP26A抑制剂或选择性CYP26B抑制剂的筛选方法。
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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：US06713647B2
公开(公告)日：2004-03-30
申请号：US10364225
申请日：2003-02-11
IPC分类号： C07C22946
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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10.发明授权1-imidazolyl substituted tetrahydronaphthalene derivatives as inhibitors of eytochrome P450RAI 失效1-咪唑基取代的四氢萘衍生物作为眼睛色素P450RAI的抑制剂公开(公告)号：US06603019B2
公开(公告)日：2003-08-05
申请号：US10079993
申请日：2002-02-21
IPC分类号： C07D23364
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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