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1. 发明授权

US06452032B1 Organosilyl compounds having nuclear hormone receptor modulating activity 失效
标题翻译：具有核激素受体调节活性的有机甲硅烷基化合物
公开(公告)号：US06452032B1
公开(公告)日：2002-09-17
申请号：US09591042
申请日：2000-06-09
申请人： Richard L. Beard , Michael E. Garst , Roshantha A. Chandraratna
发明人： Richard L. Beard , Michael E. Garst , Roshantha A. Chandraratna
IPC分类号： C07F710
CPC分类号： C07F7/0807 , C07F7/081 , C07F7/0814
摘要： Silicone-containing organic compounds useful as modulators of mammalian nuclear hormone receptors, particularly the retinoid receptors and the farnesoid receptors.
摘要翻译：有机硅有机化合物可用作哺乳动物核激素受体的调节剂，特别是类视黄醇受体和法呢基受体。

2. 发明授权

US06759547B1 5,6,7,8-tetrahydronaphthalen-2-yl 2,6-difluoroheptatrienoic acid derivatives having serum glucose reducing activity 失效
标题翻译：具有血清葡萄糖还原活性的5,6,7,8-四氢萘-2-基2,6-二氟庚酸
公开(公告)号：US06759547B1
公开(公告)日：2004-07-06
申请号：US10341837
申请日：2003-01-14
申请人： Richard L. Beard , Haiqing Yuan , Yang-Dar Yuan , Roshantha A. Chandraratna
发明人： Richard L. Beard , Haiqing Yuan , Yang-Dar Yuan , Roshantha A. Chandraratna
IPC分类号： C07C6976
CPC分类号： C07C59/72 , C07C69/734 , C07C2602/10
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 effect of reducing serum thyroxine levels.
摘要翻译：所述变体具有本说明书中定义的含义的化合物能够降低糖尿病哺乳动物的血清葡萄糖水平，而没有降低血清甲状腺素水平的不良副作用。

3. 发明授权

US06465646B1 1-alkoxy and 1-acyloxy substituted cyclohex-1-ene compounds and sulfur and 1-alkoxycarbonyl analogs having retinoid-like biological activity 失效
标题翻译： 1-烷氧基和1-酰氧基取代的环己-1-烯化合物和具有类视黄醇样生物活性的硫和1-烷氧基羰基类似物
公开(公告)号：US06465646B1
公开(公告)日：2002-10-15
申请号：US09634726
申请日：2000-08-04
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： C07D23702
CPC分类号： C07C403/02 , C07C69/76 , C07C2601/16 , C07F7/081 , C07F7/0812 , C07F7/1804
摘要： Compounds of Formula 1 and of Formula 2 where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist or retinoid negative hormone 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的化合物具有类视黄醇，维生素A拮抗剂或类视黄醇阴性激素，如生物活性。

4. 发明授权

US06387950B2 Treatment of tumors with RAR&agr; selective retinoid compounds in combination with other anti-tumor agents 失效
标题翻译：用RARalpha选择性类视黄醇化合物与其他抗肿瘤剂联合治疗肿瘤
公开(公告)号：US06387950B2
公开(公告)日：2002-05-14
申请号：US09824111
申请日：2001-04-02
申请人： Alissar Nehme , Richard L. Beard , Roshantha A. Chandraratna
发明人： Alissar Nehme , Richard L. Beard , Roshantha A. Chandraratna
IPC分类号： A61K3145
CPC分类号： A61K31/165 , A61K31/167 , C07C235/66 , C07C2602/10
摘要： Compounds which are specific or selective agonists of RAR&agr; receptors in preference over RAR&bgr; and RAR&ggr; receptors, and particularly compounds of the formula where R is a H, lower alkyl of 1 to 6 carbons, or a pharmaceutically acceptable salt, are useful for treating a malignant disease or condition in a mammal. In treatment of solid tumors the compound exhibit synergistic anti-proliferative effect with human recombinant interferon.
摘要翻译：作为优选RARα和RARγ受体的RARα受体的特异性或选择性激动剂的化合物，特别是式R的化合物，其为H，1至6个碳的低级烷基或其药学上可接受的盐，可用于治疗恶性疾病或状况。在实体瘤治疗中，该化合物与人重组干扰素具有协同的抗增殖作用。

5. 发明授权

US6117987A Alkyl or aryl substituted dihydronaphthalene derivatives having retinoid and/or retinoid antagonist like biological activity 失效
标题翻译：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。

6. 发明授权

US5877207A Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities 失效
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.

7. 发明授权

US5808124A O- or S-substituted dihydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity 失效
标题翻译：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。

8. 发明授权

US5672710A Sulfides, sulfoxides and sulfones disubstituted with a tetrahydronaphthalenyl, chromanyl, thiochromanyl or tetrahydroquinolinyl and substituted phenyl or heteroaryl group, having retinoid-like biological activity 失效
标题翻译：用四氢萘基，苯并二氢吡喃基，硫代苯并二氢吡喃基或四氢喹啉基和取代的苯基或杂芳基二取代的硫化物，亚砜和砜，具有类视黄醇样生物活性
公开(公告)号：US5672710A
公开(公告)日：1997-09-30
申请号：US552965
申请日：1995-11-03
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： C07C317/44 , C07C323/62 , C07D213/80 , C07D277/36 , C07D277/56 , C07D277/24
CPC分类号： C07D213/80 , C07C317/44 , C07C323/62 , C07D277/56
摘要： ##STR1## wherein the symbols have the meaning described in the specification, are selective agonists of RXR retinoid receptors.
摘要翻译：其中符号具有说明书中描述的含义，是RXR类视黄醇受体的选择性激动剂。

9. 发明授权

US5618836A [4-(1,2-epoxycyclohexanyl)but-3-en-1-ynyl]aromatic and heteroaromatic acids and derivatives having retinoid-like biological activity 失效
标题翻译： [4-（1,2-环氧环己烷基）丁-3-烯-1-炔基]芳族和杂芳族酸和具有类视黄醇样生物活性的衍生物
公开(公告)号：US5618836A
公开(公告)日：1997-04-08
申请号：US419626
申请日：1995-04-10
申请人： Roshantha A. Chandraratna , Richard L. Beard
发明人： Roshantha A. Chandraratna , Richard L. Beard
IPC分类号： C07D303/38 , C07D303/40 , C07D405/06 , C07D407/06 , C07D409/06 , A61K31/38 , A61K31/34
CPC分类号： C07D303/38 , C07D303/40 , C07D405/06 , C07D407/06 , C07D409/06
摘要： Compounds of Formula 1 ##STR1## where R.sub.1 -R.sub.7 are hydrogen, lower alkyl of 1-6 carbons, or halogen;Y is phenyl, pyridyl, furyl, thienyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl or oxazolyl;A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds;B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.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.14, CR.sub.14 (OR.sub.12).sub.2, or CR.sub.14 OR.sub.13 O, where R.sub.8 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 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, R.sub.13 is divalent alkyl radical of 2-5 carbons and R.sub.14 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, have retinoid-like biological activity.
摘要翻译：式1化合物其中R 1 -R 7是氢，1-6个碳的低级烷基或卤素; Y是苯基，吡啶基，呋喃基，噻吩基，哒嗪基，嘧啶基，吡嗪基，噻唑基或恶唑基; A是（CH 2）n，其中n是0-5，具有3-6个碳的低级支链烷基，具有3-6个碳的环烷基，具有2-6个碳的烯基和1或2个双键，具有2-6个碳原子的炔基和 1或2个三键; B是氢，COOH或其药学上可接受的盐，COOR8，CONR9R10，-CH2OH，CH2OR11，CH2OCOR11，CHO，CH（OR12）2，CHOR13O，-COR14，CR14（OR12）2或CR14OR13O，其中R8是烷基 1〜10个碳原子的烷基或碳原子数为5〜10的环烷基，或R8为苯基或低级烷基苯基，R9和R10分别独立地为氢，碳原子数1〜10的烷基或5-10个碳原子的环烷基或苯基或低级烷基苯基，R 11为低级烷基，苯基或低级烷基苯基，R 12为低级烷基，R 13为2-5个碳原子的二价烷基，R 14为含有1至5个碳原子的烷基，环烷基或烯基，具有类视黄醇类生物活性。

10. 发明授权

US5426118A [4-(1,2-epoxycyclohexanyl)but-3-en-1-ynyl]aromatic and heteroaromatic acids and derivatives having retinoid-like biological activity 失效
标题翻译： [4-（1,2-环氧环己烷基）丁-3-烯-1-炔基]芳族和杂芳族酸和具有类视黄醇样生物活性的衍生物
公开(公告)号：US5426118A
公开(公告)日：1995-06-20
申请号：US177620
申请日：1993-12-30
申请人： Roshantha A. Chandraratna , Richard L. Beard
发明人： Roshantha A. Chandraratna , Richard L. Beard
IPC分类号： C07D303/38 , C07D303/40 , C07D405/06 , C07D407/06 , C07D409/06 , A61K31/44
CPC分类号： C07D303/38 , C07D303/40 , C07D405/06 , C07D407/06 , C07D409/06
摘要： Compounds of Formula 1 ##STR1## where R.sub.1 -R.sub.7 are hydrogen, lower alkyl of 1-6 carbons, or halogen;Y is phenyl, pyridyl, furyl, thienyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl or oxazolyl;A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds;B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.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.14, CR.sub.14 (OR.sub.12).sub.2, or CR.sub.14 OR.sub.13 O, where R.sub.8 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 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, R.sub.13 is divalent alkyl radical of 2-5 carbons and R.sub.14 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, have retinoid-like biological activity.
摘要翻译：式1化合物其中R 1 -R 7是氢，1-6个碳的低级烷基或卤素; Y是苯基，吡啶基，呋喃基，噻吩基，哒嗪基，嘧啶基，吡嗪基，噻唑基或恶唑基; A是（CH 2）n，其中n是0-5，具有3-6个碳的低级支链烷基，具有3-6个碳的环烷基，具有2-6个碳的烯基和1或2个双键，具有2-6个碳原子的炔基和 1或2个三键; B是氢，COOH或其药学上可接受的盐，COOR8，CONR9R10，-CH2OH，CH2OR11，CH2OCOR11，CHO，CH（OR12）2，CHOR13O，-COR14，CR14（OR12）2或CR14OR13O，其中R8是烷基 1〜10个碳原子的烷基或碳原子数为5〜10的环烷基，或R8为苯基或低级烷基苯基，R9和R10分别独立地为氢，碳原子数1〜10的烷基或5-10个碳原子的环烷基或苯基或低级烷基苯基，R 11为低级烷基，苯基或低级烷基苯基，R 12为低级烷基，R 13为2-5个碳原子的二价烷基，R 14为含有1至5个碳原子的烷基，环烷基或烯基，具有类视黄醇类生物活性。

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