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101. 发明授权

US06320047B1 Substituted aryl or heteroarylamides having retinoid-like biological activity 失效
公开(公告)号：US06320047B1
公开(公告)日：2001-11-20
申请号：US09829310
申请日：2001-04-09
申请人： Min Teng , Tien T. Duong , Roshantha A. Chandraratna
发明人： Min Teng , Tien T. Duong , Roshantha A. Chandraratna
IPC分类号： C07D21302
CPC分类号： C07D213/82 , C07C233/81
摘要： Compounds of the formula wherein the symbols have the meaning described in the specification, have retinoid-like biological activity.

102. 发明授权

US06294657B1 Retinoid induced gene 失效
标题翻译：类视黄醇诱导基因
公开(公告)号：US06294657B1
公开(公告)日：2001-09-25
申请号：US08996533
申请日：1997-12-23
申请人： Sunil Nagpal , Daniel DiSepio , Roshantha A. Chandraratna
发明人： Sunil Nagpal , Daniel DiSepio , Roshantha A. Chandraratna
IPC分类号： C07H2102
CPC分类号： C07K14/82
摘要： A novel human cDNA, called TIG3 (Tazarotene Induced Gene 3), inducible by RAR-selective retinoids and structurally related to a known tumor suppressor gene. Methods of detecting the TIG3 polynucleotide.
摘要翻译：一种称为TIG3（他扎罗汀诱导的基因3）的新型人类cDNA，由RAR选择性类维生素A诱导，并与已知的肿瘤抑制基因结构相关。检测TIG3多核苷酸的方法。

103. 发明授权

US06172115B2 Method for preventing onset of restenosis after angioplasty employing an RXR-specific retinoid 失效
标题翻译：在使用RXR特异性类视黄醇的血管成形术后预防再狭窄发作的方法
公开(公告)号：US06172115B2
公开(公告)日：2001-01-09
申请号：US09005897
申请日：1998-01-12
申请人： Roshantha A. Chandraratna
发明人： Roshantha A. Chandraratna
IPC分类号： A01N3710
CPC分类号： A61K31/34 , A61K31/19 , A61K31/38
摘要： A method is provided for preventing or reducing the risk of restenosis following angioplasty by administering a retinoid, such as an RXR-selective retinoid, e.g. the compound of the formula: and pharmaceutically acceptable salts and esters and amides thereof.
摘要翻译：提供了一种通过施用类视黄醇（例如RXR-选择性类维生素A，例如紫杉醇）来预防或降低血管成形术后再狭窄的风险的方法。下式的化合物及其药学上可接受的盐和酯和酰胺。

104. 发明授权

US6166244A Oxygen, sulfur and nitrogen substituted cyclohexene and cyclohexane derivatives having retinoid-like biological activity 失效
公开(公告)号：US6166244A
公开(公告)日：2000-12-26
申请号：US307061
申请日：1999-05-07
申请人： Richard L. Beard , Diana F. Colon , Roshantha A. Chandraratna
发明人： Richard L. Beard , Diana F. Colon , Roshantha A. Chandraratna
IPC分类号： A61K31/325 , A61P17/00 , C07C69/52 , C07C69/76 , C07C69/84 , C07C69/86 , C07C333/00 , C07C403/18 , C07D213/06 , C07D237/02 , C07D333/16 , C07F7/08 , C07C69/64
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. ##STR1##

105. 发明授权

US6075032A Method of preventing proliferation of retinal pigment epithelium by retinoic acid receptor agonists 失效
标题翻译：视黄酸受体激动剂预防视网膜色素上皮细胞增生的方法
公开(公告)号：US6075032A
公开(公告)日：2000-06-13
申请号：US875665
申请日：1998-01-23
申请人： Peter A. Campochiaro , Larry A. Wheeler , Roshantha A. Chandraratna , Sunil Nagpal , Eugene De Juan, Jr.
发明人： Peter A. Campochiaro , Larry A. Wheeler , Roshantha A. Chandraratna , Sunil Nagpal , Eugene De Juan, Jr.
IPC分类号： A61K9/127 , A61K9/14 , A61K31/19 , A61K31/192 , A61K31/455 , A61K31/465 , A61K45/00 , A61K47/24 , A61P27/02 , A61P35/00 , A61K31/435 , A61K31/07
CPC分类号： A61K31/455 , A61K31/192 , Y10S514/912
摘要： Proliferation of retinal pigment epithelium following surgery or trauma or resulting in ocular diseases associated with choroidal neovascularization, such as age related macular degeneration and histoplasmosis syndrome, is prevented by contacting retinal pigment epithelium cells with a therapeutic amount of a retinoic acid receptor (RAR agonist, preferably one with specific activity for retinoic acid receptors. Preferably the RAR agonist is also a potent antagonist of AP1-dependent gene expression. Alternatively, the proliferation of retinal pigment epithelium is ameliorated with a therapeutic amount of an AP-1 antagonist, alone or in combination with an RAR agonist. The drug can be administered by bolus injection into the vitreous cavity using a dosage from about 50 to 150 .mu.g. Or by slow release from liposomes or an oil tamponade injected into the vitreous cavity. Formulations for preventing proliferation of retinal pigment epithelium are also provided.
摘要翻译： PCT No.PCT / US96 / 01505 Sec。 371日期1998年1月23日 102（e）日期1998年1月23日PCT提交1996年1月31日PCT公布。公开号WO96 / 23498 日期1996年8月8日通过使视网膜色素上皮细胞与治疗量的视黄酸接触来预防手术或创伤后视网膜色素上皮细胞增生或与脉络膜新生血管形成相关的眼部疾病，如年龄相关性黄斑变性和组织胞浆菌病综合征受体（RAR激动剂，优选具有对视黄酸受体具有比活性的激动剂），优选地，RAR激动剂也是AP1依赖性基因表达的有效拮抗剂，或者，用治疗量的AP-1改善视网膜色素上皮的增殖拮抗剂，单独或与RAR激动剂组合，药物可以通过使用约50至150μg的剂量通过快速注射进入玻璃体腔中，或通过从脂质体缓慢释放或注入玻璃体腔的油栓塞来施用。还提供了用于防止视网膜色素上皮细胞增殖的制剂。

106. 发明授权

US6051713A Substituted aryl or heteroarylamides having retinoid-like biological activity 失效
标题翻译：具有类视黄醇样生物活性的取代的芳基或杂芳基酰胺
公开(公告)号：US6051713A
公开(公告)日：2000-04-18
申请号：US215509
申请日：1998-12-17
申请人： Min Teng , Tien T. Duong , Roshantha A. Chandraratna
发明人： Min Teng , Tien T. Duong , Roshantha A. Chandraratna
IPC分类号： C07D213/81 , A61K31/00 , A61K31/44 , A61P43/00 , C07C233/81 , C07C235/64 , C07D20060101 , C07D213/02 , C07D213/82 , C07D233/54 , C07D401/02 , C07D401/12 , C07D403/02 , C07D413/02 , C07D417/02
CPC分类号： C07D213/82 , C07C233/81
摘要： Compounds of the formula ##STR1## wherein the symbols have the meaning described in the specification, have retinoid-like biological activity.
摘要翻译：下式的化合物其中符号具有说明书中描述的含义，具有类视黄醇样生物活性。

107. 发明授权

US6043381A Process for preparing substituted benzo[1,2-g]-chrom-3-ene, benzo[1,2-g]-thiochrom-3-ene and benzo[1,2-g]-1,2-dihydroquinoline derivatives 失效
标题翻译：取代苯并[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的制备方法
公开(公告)号：US6043381A
公开(公告)日：2000-03-28
申请号：US307062
申请日：1999-05-07
申请人： Vidyasagar Vuligonda , Roshantha A. Chandraratna
发明人： Vidyasagar Vuligonda , Roshantha A. Chandraratna
IPC分类号： C07D307/92 , C07D311/92
CPC分类号： C07D307/92
摘要： Compounds of Formula 1 ##STR1## where the symbols have the meaning disclosed in the specification are prepared by reaction of a compound of Formula 2 ##STR2## with an organometal reagent R--M to provide a compound of Formula 3 ##STR3## that is reacted with the reagent X.sub.3 --Y(R.sub.2)--A--B in the presence of a catalyst to provide the compounds of Formula 1.
摘要翻译：通过式2的化合物与有机金属试剂RM的反应制备符号具有本说明书中公开的含义的式1化合物，得到与试剂X3-Y（R2）-AB反应的式3化合物在催化剂的存在下提供式1的化合物。

108. 发明授权

US6037488A Trisubstituted phenyl derivatives having retinoid agonist, antagonist or inverse agonist type biological activity 失效
标题翻译：具有类视黄醇激动剂，拮抗剂或反向激动剂型生物活性的三取代苯基衍生物
公开(公告)号：US6037488A
公开(公告)日：2000-03-14
申请号：US845019
申请日：1997-04-19
申请人： Tae K. Song , Min Teng , Roshantha A. Chandraratna
发明人： Tae K. Song , Min Teng , Roshantha A. Chandraratna
IPC分类号： A61P3/06 , A61K31/192 , A61K31/216 , A61P7/02 , A61P9/08 , A61P17/00 , A61P17/02 , A61P17/06 , A61P17/10 , A61P17/14 , A61P17/16 , A61P29/00 , A61P31/02 , A61P35/00 , C07C45/46 , C07C45/54 , C07C45/67 , C07C45/71 , C07C63/66 , C07C65/19 , C07C65/28 , C07C65/40 , C07C69/76 , C07C69/94 , C07F7/18
CPC分类号： C07C69/94 , C07C45/46 , C07C45/54 , C07C45/673 , C07C45/71 , C07C63/66 , C07C65/19 , C07C65/28 , C07C65/40 , C07C69/76
摘要： Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification, have retinoid, retinois antagonist or retinoid inverse agonist type biological activity.
摘要翻译：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，视黄醇拮抗剂或维甲酸反向激动剂型生物活性。

109. 发明授权

US6034242A 2,4-pentadienoic acid derivatives having retinoid-like biological activity 失效
标题翻译：具有类视黄醇样生物活性的2,4-戊二烯酸衍生物
公开(公告)号：US6034242A
公开(公告)日：2000-03-07
申请号：US165917
申请日：1998-10-02
申请人： Vidyasagar Vuligonda , Roshantha A. Chandraratna
发明人： Vidyasagar Vuligonda , Roshantha A. Chandraratna
IPC分类号： A61K31/35 , A61K31/20 , A61K31/23 , A61K31/38 , A61K31/47 , A61P17/00 , A61P43/00 , C07C57/50 , C07C69/618 , C07C215/02 , C07C215/18 , C07C311/58 , C07C335/06 , C07C403/00 , C07D277/22 , C07D311/58 , C07D333/54 , C07D335/06 , C07D215/06 , C07D215/12
CPC分类号： C07D333/54 , A61K31/20 , A61K31/23 , C07C57/50 , C07C69/618 , C07D311/58 , C07D335/06
摘要： Compounds of Formula 1 ##STR1## wherein Z is selected from the group consisting of the radicals shown in Formula 3, ##STR2## Y is cycloalkyl or cycloalkenyl of 3 to 8 carbons optionally substituted with one or two R.sub.4 groups, said groups being optionally substituted with one or two R.sub.4 groups, the divalent Y radical being substituted by the Z and --CR.sub.1 .dbd.CR.sub.1 --CR.sub.1 .dbd.CR.sub.1 groups on adjacent carbons; X is NR.sub.5 ; R.sub.1 and R.sub.2 independently are H, lower alkyl or fluoroalkyl; R.sub.3 is hydrogen, lover alkyl, Cl or Br; R.sub.4 is lower alkyl, fluoroalkyl or halogen; R.sub.5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CO.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, CR.sub.7 OR.sub.13 O, or tri-lower alkylsilyl, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons, a cycloalkyl group of 5 to 10 carbons or trimethylsilylalkyl where the alkyl group has 1 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R.sub.11 is lower alkyl, phenyl or lower alkylphenyl, R.sub.12 is lower alkyl, and R.sub.13 is divalent alkyl radical of 2-5 carbons, have retinoid like biological activity.
摘要翻译：式1的化合物，其中Z选自式3中所示的基团，Y是任选被一个或两个R 4基团取代的碳原子数为3至8的环烷基或环烯基，所述基团任选被一个或两个R 4基团取代，二价Y基团被相邻碳上的Z和-CR1 = CR1-CR1 = CR1基团取代; X是NR5; R1和R2独立地为H，低级烷基或氟代烷基; R3是氢，有情人烷基，Cl或Br; R4是低级烷基，氟烷基或卤素; R5是H或低级烷基，B是氢，COOH或其可药用盐，COOR8，CO9R10，-CH2OH，CH2OR11，CH2OCOR11，CHO，CH（OR12）2，CHOR13O，-COR7，CR7（OR12） CR 7OR 13 O或三低级烷基甲硅烷基，其中R 7为含有1至5个碳的烷基，环烷基或烯基，R 8为碳原子数1至10的烷基，碳原子数为5至10的环烷基或烷基具有的三甲基甲硅烷基烷基 1至10个碳，或R8为苯基或低级烷基苯基，R9和R10独立地为氢，1-10个碳原子的烷基或5-10个碳原子的环烷基，或苯基或低级烷基苯基，R11为低级烷基，苯基或低级烷基苯基，R12为低级烷基，R13为2-5个碳原子的二价烷基，具有类视黄醇类生物活性。

110. 发明授权

US5917082A 2,4-pentadienoic acid derivatives having retinoid-like biological activity 失效
标题翻译：具有类视黄醇样生物活性的2,4-戊二烯酸衍生物
公开(公告)号：US5917082A
公开(公告)日：1999-06-29
申请号：US918735
申请日：1997-08-20
申请人： Vidyasagar Vuligonda , Roshantha A. Chandraratna
发明人： Vidyasagar Vuligonda , Roshantha A. Chandraratna
IPC分类号： A61K31/35 , A61K31/20 , A61K31/23 , A61K31/38 , A61K31/47 , A61P43/00 , C07C57/50 , C07C69/618 , C07C215/02 , C07C215/18 , C07C311/58 , C07C335/06 , C07C403/00 , C07D311/58 , C07D333/54 , C07D335/06 , C07C69/76 , C07C63/36
CPC分类号： C07D311/58 , A61K31/20 , A61K31/23 , C07C57/50 , C07C69/618 , C07D333/54 , C07D335/06
摘要： Enantiomerically substantially pure compounds of the formula ##STR1## where R is H or lower alkyl of 1 to 6 carbons, or pharmaceutically acceptable salts thereof have retinoid-like biological activity. The enantimerically pure or substantially pure compound of the above formula where R is H, or a pharmaceutically acceptable salt thereof, is highly specific agonist of RXR retinoid receptors in preference over RAR receptors.
摘要翻译：对映异构基本上纯的下式化合物其中R是H或1至6个碳的低级烷基或其药学上可接受的盐具有类视黄醇样生物活性。其中R是H的上述式的对映体纯的或基本上纯的化合物或其药学上可接受的盐是优先于RAR受体的RXR类视黄醇受体的高度特异性激动剂。

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