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1.发明申请公开(公告)号：US20050004165A1
公开(公告)日：2005-01-06
申请号：US10910688
申请日：2004-08-03
IPC分类号： C12N15/09 , A61K31/192 , A61K31/202 , A61K31/203 , A61K31/695 , A61P3/00 , A61P35/00 , A61P43/00 , A61K31/41
CPC分类号： A61K31/192 , A61K31/202 , A61K31/203 , A61K31/695
摘要： Methods for modulating the activity of the mammalian BAR/FXR receptor. The methods include methods of treating a hypocholesterolemic mammal comprising contacting the mammal with synthetic compounds able to modulate an activity characteristic of the BAR/FXR receptor. Other methods include a method of treating colon cancer in a mammal comprising administering a compound having a BAR/FXR antagonistic activity.
摘要翻译： 调节哺乳动物BAR / FXR受体活性的方法。 所述方法包括治疗低胆固醇血症哺乳动物的方法，包括使哺乳动物与能够调节BAR / FXR受体活性特征的合成化合物接触。 其他方法包括在哺乳动物中治疗结肠癌的方法，包括给予具有BAR / FXR拮抗活性的化合物。
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2.发明申请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：US20080004455A1
公开(公告)日：2008-01-03
申请号：US11728313
申请日：2007-03-23
申请人： Jayasree Vasudevan , Liming Wang , Xiaoxia Liu , Kwok Tsang , Ling Li , Janet Takeuchi , Thong Vu , Richard Beard , Smita Bhat , Vidyasagar Vuligonda , Roshantha Chandraratna
发明人： Jayasree Vasudevan , Liming Wang , Xiaoxia Liu , Kwok Tsang , Ling Li , Janet Takeuchi , Thong Vu , Richard Beard , Smita Bhat , Vidyasagar Vuligonda , Roshantha Chandraratna
IPC分类号： C07D311/96 , C07C229/44 , C07C63/331 , C07D311/04
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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![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/2005/05/05/US20050096380A1/abs.jpg.150x150.jpg)
3.发明申请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）-CHROM-3-EN-6-YL] - 庚酸和7 - [（3-烷氧基）-5,6-二氢萘-2-基] - 嘌呤酸衍生物具有减少血清葡萄糖 活动公开(公告)号：US20050096380A1
公开(公告)日：2005-05-05
申请号：US10696748
申请日：2003-10-29
申请人： Richard Beard , Tien Duong , Janet Takeuchi , Ling Li , Kwok Tsang , Xiaoxia Liu , Jayasree Vasudevan , Liming Wang , Santosh Sinha , Haiqing Yuan , Roshantha Chandraratna
发明人： Richard Beard , Tien Duong , Janet Takeuchi , Ling Li , Kwok Tsang , Xiaoxia Liu , Jayasree Vasudevan , Liming Wang , Santosh Sinha , Haiqing Yuan , Roshantha Chandraratna
IPC分类号： A61K31/21 , A61K31/335 , C07C59/72 , C07C69/587 , C07C69/734 , C07D311/58 , A61K31/353 , A61K31/192 , C07C65/105
CPC分类号： C07C69/734 , C07C59/72 , C07C2601/02 , C07C2602/28 , C07D311/58
摘要： Compounds of the formula where the variables 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： 其中变量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，而没有瞬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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5.发明申请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：US20050176689A1
公开(公告)日：2005-08-11
申请号：US11014460
申请日：2004-12-16
申请人： Jayasree Vasudevan , Liming Wang , Xiaoxia Liu , Kwok Tsang , Ling Li , Janet Takeuchi , Thong Vu , Richard Beard , Smita Bhat , Vidyasagar Vuligonda , Roshantha Chandraratna
发明人： Jayasree Vasudevan , Liming Wang , Xiaoxia Liu , Kwok Tsang , Ling Li , Janet Takeuchi , Thong Vu , Richard Beard , Smita Bhat , Vidyasagar Vuligonda , Roshantha Chandraratna
IPC分类号： C07C57/42 , C07C59/64 , C07C59/86 , C07C69/18 , C07C69/73 , C07C69/753 , C07C69/76 , C07C229/34 , C07C229/38 , C07C229/46 , C07C229/50 , C07C275/42 , C07D311/58 , C07D311/64 , C07D311/96 , A61K31/655 , A61K31/4747 , A61K31/497 , A61K31/502 , A61K31/506
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-[phenyl-tetrahydronaphthalene-2-yl dihydronaphthalen-2-yl and heteroaryl-cyclopropyl]-pentadienoic acid derivatives having serum glucose reducing activity](/abs-image/US/2005/01/06/US20050004213A1/abs.jpg.150x150.jpg)
6.发明申请5-[phenyl-tetrahydronaphthalene-2-yl dihydronaphthalen-2-yl and heteroaryl-cyclopropyl]-pentadienoic acid derivatives having serum glucose reducing activity 失效具有血清葡萄糖还原活性的5- [苯基 - 四氢萘-2-基二氢萘-2-基和杂芳基 - 环丙基] - 戊二烯酸衍生物公开(公告)号：US20050004213A1
公开(公告)日：2005-01-06
申请号：US10606603
申请日：2003-06-26
申请人： Santosh Sinha , Kwok Tsang , Smita Bhat , Roshantha Chandraratna
发明人： Santosh Sinha , Kwok Tsang , Smita Bhat , Roshantha Chandraratna
IPC分类号： A61P3/10 , C07C59/72 , C07C69/74 , A61K31/215
CPC分类号： C07C59/72
摘要： Compounds of the formula where the variables have the meaning defined in the specification are capable of reducing serum glucose levels in diabetic mammals without the undesirable side effects of reducing serum thyroxine levels and transiently increasing triglyceride levels.
摘要翻译： 其中变量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，而没有降低血清甲状腺素水平和短暂增加甘油三酯水平的不良副作用。
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![Aryl or heteroaryl substituted 3,4-dihydroanthracene and aryl or heteroaryl substituted benzo[1,2-g]-chrom-3-ene, benzo[1,2-g]-thiochrom-3-ene and benzo [1,2-g]-1,2-dihydroquinoline derivatives having retinoid antagonist or retinoid inverse agonist type biological activity](/abs-image/US/2007/11/15/US20070265449A1/abs.jpg.150x150.jpg)
7.发明申请Aryl or heteroaryl substituted 3,4-dihydroanthracene and aryl or heteroaryl substituted benzo[1,2-g]-chrom-3-ene, benzo[1,2-g]-thiochrom-3-ene and benzo [1,2-g]-1,2-dihydroquinoline derivatives having retinoid antagonist or retinoid inverse agonist type biological activity 审中-公开芳基或杂芳基取代的3,4-二氢蒽和芳基或杂芳基取代的苯并[1,2-g] - 色烯-3-烯，苯并[1,2-g] - 硫代色烯-3-烯和苯并[1,2- g] -1,2-二氢喹啉衍生物，其具有类视黄醇拮抗剂或类视黄醇反向激动剂型生物活性公开(公告)号：US20070265449A1
公开(公告)日：2007-11-15
申请号：US11643754
申请日：2006-12-21
IPC分类号： C07D211/06 , C07C25/22 , C07C323/56 , C07C333/08 , C07D335/08 , C07D311/92 , C07C47/546 , C07C69/78
CPC分类号： C07C69/76 , C07C45/00 , C07C47/548 , C07C2603/24 , C07D213/55 , C07D311/92 , C07D333/24 , C07D335/08 , C07D409/06
摘要： Compounds of the formula where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist and/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的化合物具有类视黄醇，类视黄醇拮抗剂和/或维甲酸反相激动剂样生物活性。
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8.发明申请Disubstituted chalcone oximes having RARy retinoid receptor antagonist activity 失效具有RARγ类视黄醇受体拮抗剂活性的二取代查耳酮肟公开(公告)号：US20050165095A1
公开(公告)日：2005-07-28
申请号：US11021471
申请日：2004-12-23
申请人： Kwok Tsang , Santosh Sinha , Xiaoxia Liu , Smita Bhat , Roshantha Chandraratna
发明人： Kwok Tsang , Santosh Sinha , Xiaoxia Liu , Smita Bhat , Roshantha Chandraratna
IPC分类号： A61K31/195 , A61K31/353 , A61K31/382 , A61K31/47 , A61K31/695 , C07C251/48 , C07D215/02 , C07D215/12 , C07D335/06
CPC分类号： C07D335/06 , C07C251/48 , C07C2602/08 , C07C2602/10 , C07D215/12
摘要： Compounds of the formula where the variables have the values described in the specification are antagonists of RARγ retinoid receptors.
摘要翻译： 变量具有本说明书中描述的值的式的化合物是RAR类视黄醇受体的拮抗剂。
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公开(公告)号：US20070054882A1
公开(公告)日：2007-03-08
申请号：US11503635
申请日：2006-08-14
IPC分类号： A61K31/695 , A61K31/47 , A61K31/382 , A61K31/353 , A61K31/195
CPC分类号： A61K31/382 , A61K31/00 , A61K31/192 , A61K31/195 , A61K31/196 , A61K31/203 , A61K31/353 , A61K31/47 , A61K31/695 , Y10S514/841
摘要： Methods and compositions for inhibiting or preventing spermatogenesis in a male mammal. Also disclosed are compounds and formulations for use in such methods.
摘要翻译： 用于抑制或预防雄性哺乳动物精子发生的方法和组合物。 还公开了用于这些方法的化合物和制剂。
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公开(公告)号：US20050171151A1
公开(公告)日：2005-08-04
申请号：US11016534
申请日：2004-12-17
IPC分类号： C07D335/06 , A61K31/00 , A61K31/196 , A61K31/202 , A61K31/235 , A61K31/352 , A61K31/382 , A61K45/00 , A61P3/06 , A61P9/10 , C07D311/58 , A61K31/47 , A61K31/353
CPC分类号： A61K31/382 , A61K31/00 , A61K31/196 , A61K31/202 , A61K31/352
摘要： The current invention relates to methods for treating hyperlipidemia in mammals, including humans. More specifically, the current invention relates to the use of retinoid or retinoid derivative that is able to act as an antagonist or inverse agonist of a retinoid receptor to treat hyperlipidemia.
摘要翻译： 本发明涉及用于治疗哺乳动物包括人类的高脂血症的方法。 更具体地，本发明涉及能够作为类视黄醇受体的拮抗剂或反向激动剂作用以治疗高脂血症的类视色素或类视色素衍生物的用途。
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