专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US08618163B2 Derivatives of cycloalkyl- and cycloalkenyl-1,2-dicarboxylic acid compounds having formyl peptide receptor like-1 (FPRL-1) agonist or antagonist activity 有权
标题翻译：具有甲酰肽受体1（FPRL-1）激动剂或拮抗剂活性的环烯基和环烯基-1,2-二羧酸化合物的衍生物
公开(公告)号：US08618163B2
公开(公告)日：2013-12-31
申请号：US13168464
申请日：2011-06-24
申请人： Richard L. Beard , John E. Donello , Vidyasagar Vuligonda , Michael E. Garst
发明人： Richard L. Beard , John E. Donello , Vidyasagar Vuligonda , Michael E. Garst
IPC分类号： A61K31/21 , A61K31/16 , A01N37/18
CPC分类号： C07C323/40 , A61K31/16 , A61K31/167 , A61K31/192 , A61K31/195 , A61K31/215 , A61K31/216 , A61K31/4035 , A61K31/44 , C07C233/58 , C07C233/59 , C07C311/46 , C07C2603/94 , C07D213/75 , C07D493/08
摘要： The invention provides well defined compounds having FPRL-1 agonist or antagonist activity. As such, the compounds of the invention are useful for treating a variety of ocular disorders.
摘要翻译：本发明提供了具有FPRL-1激动剂或拮抗剂活性的明确定义的化合物。因此，本发明的化合物可用于治疗各种眼部疾病。

2. 发明申请

US20120238628A1 DIHYDRONAPHTHALENE AND NAPHTHALENE DERIVATIVES AS N-FORMYL PEPTIDE RECEPTOR LIKE-1 (FPRL-1) RECEPTOR MODULATORS 有权
标题翻译：作为N-甲基肽受体样-1（FPRL-1）受体调节剂的二氢萘和萘衍生物
公开(公告)号：US20120238628A1
公开(公告)日：2012-09-20
申请号：US13409228
申请日：2012-03-01
申请人： Vidyasagar Vuligonda , Richard L. Beard , Thong Vu , John E. Donello , Veena Viswanath , Michael E. Garst
发明人： Vidyasagar Vuligonda , Richard L. Beard , Thong Vu , John E. Donello , Veena Viswanath , Michael E. Garst
IPC分类号： A61K31/196 , A61P27/02 , A61P35/00 , A61P35/04 , A61P29/00 , A61P11/00 , A61P31/18 , A61P9/00 , A61P25/00 , A61P11/06 , A61P37/08 , A61P19/04 , A61P17/06 , A61P25/28 , A61P19/02 , A61P31/00 , A61P1/00 , A61P9/10 , A61P17/00 , A61P17/10 , A61P17/12 , A61P17/14 , A61P17/08 , C07C229/46
CPC分类号： C07C235/84 , C07C233/59 , C07C235/82 , C07C2602/10
摘要： The present invention relates to novel dihydronaphthalene and naphthalene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
摘要翻译：本发明涉及新型二氢萘和萘衍生物，其制备方法，含有它们的药物组合物及其作为N-甲酰基肽受体1（FPRL-1）受体调节剂的药物的用途。

3. 发明申请

US20070232682A1 Indole Compounds having sphingosine-1-phosphate (S1P) receptor antagonist 有权
标题翻译：具有鞘氨醇-1-磷酸（S1P）受体拮抗剂的吲哚化合物
公开(公告)号：US20070232682A1
公开(公告)日：2007-10-04
申请号：US11690637
申请日：2007-03-23
申请人： Richard L. Beard , John E. Donello , Haiqing Yuan , Vidyasagar Vuligonda , Tien T. Duong
发明人： Richard L. Beard , John E. Donello , Haiqing Yuan , Vidyasagar Vuligonda , Tien T. Duong
IPC分类号： A61K31/405 , C07D209/04
CPC分类号： C07D209/14 , C07D209/12 , C07D209/30 , C07D209/40 , C07D209/42 , C07D405/12 , C07D409/06 , C07D413/04 , C07F9/5728
摘要： The present invention provides novel compounds having the following general formula I wherein: A, B, X, Y, R1, R2, R3, R4, n, o and p are as defined in the specification. Such compounds are useful for treating a disease or condition selected from the group consisting of glaucoma, dry eye, angiogenesis, cardiovascular conditions or diseases and wound healing.
摘要翻译：本发明提供具有以下通式I的新化合物，其中：A，B，X，Y，R 1，R 2，R 3， >，R 4，n，o和p如说明书中所定义。这样的化合物可用于治疗选自青光眼，干眼症，血管发生，心血管疾病或疾病和伤口愈合的疾病或病症。

4. 发明授权

US06538149B1 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 失效
标题翻译：芳基或杂芳基取代的3,4-二羟基乙腈和芳基或取代的苄基[1,2-G] CH 3 -3-烯，苯并[1,2-G] - 噻唑酮-3-烯和苯并[1,2-G ] -1,2-二氢喹啉衍生物具有抗原拮抗剂或反义抗体激动剂类型生物活性
公开(公告)号：US06538149B1
公开(公告)日：2003-03-25
申请号：US09482700
申请日：2000-01-13
申请人： Vidyasagar Vuligonda , Alan T. Johnson , Roshantha A. Chandraratna
发明人： Vidyasagar Vuligonda , Alan T. Johnson , Roshantha A. Chandraratna
IPC分类号： C07C6974
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：符号具有本说明书中定义的含义的化合物具有类视黄醇，维生素A拮抗剂和/或类视黄醇反相激动剂样生物活性。

5. 发明授权

US06403638B1 2,4-pentadienoic acid derivatives having selective activity for retinoid X (RXR) receptors 失效
标题翻译：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
申请人： Vidyasagar Vuligonda , Kwok Yin Tsang , Jayasree Vasudevan , Roshantha A. Chandraratna
发明人： Vidyasagar Vuligonda , Kwok Yin Tsang , Jayasree Vasudevan , Roshantha A. Chandraratna
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。

6. 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。

7. 发明授权

US6114533A 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：US6114533A
公开(公告)日：2000-09-05
申请号：US390825
申请日：1999-09-07
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 Formula 3, ##STR2## Y is cycloalkyl or cycloalkenyl of 3 to 8 carbons optionally substituted with one or two R.sub.4 groups, or Y is phenyl, 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 a 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.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是式3，Y是任选被一个或两个R 4基团取代的3至8个碳的环烷基或环烯基，或Y是苯基，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，a是氢，COOH或其药学上可接受的盐，COOR8，CONR9R10，-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。

8. 发明授权

US6025388A Method for inhibiting gene expression promoted by AP1 protein with RAR.beta. selective retinoids and method for treatment of diseases and conditions with such retinoids 失效
标题翻译：用RARβ选择性类维生素A抑制AP1蛋白促进基因表达的方法和用这种类维生素A治疗疾病和病症的方法
公开(公告)号：US6025388A
公开(公告)日：2000-02-15
申请号：US428957
申请日：1995-04-26
申请人： Sunil Nagpal , Tae K. Song , Vidyasagar Vuligonda , Jyoti Athanikar , Roshantha A. Chandraratna
发明人： Sunil Nagpal , Tae K. Song , Vidyasagar Vuligonda , Jyoti Athanikar , Roshantha A. Chandraratna
IPC分类号： C07D309/12 , A61K31/35 , A61K31/351 , A61K31/443 , A61K31/455 , A61P9/10 , A61P17/00 , A61P35/02 , A61P43/00 , C07D405/12 , A01N43/16 , A01N43/40
CPC分类号： A61K31/351 , A61K31/455
摘要： Retinoid compounds which repress expression of the gene promoted by AP1 protein but which do not significantly activate expression of the genes having RA-responsive elements in their promoter region through RAR.alpha. and RAR.GAMMA. receptor subtypes, are used, with reduced side effects, for treating diseases and conditions which are responsive to therapy with retinoids.
摘要翻译：使用抑制由AP1蛋白促进的基因表达而不通过RARα和RAR GAMMA受体亚型显着激活其启动子区域中具有RA应答元件的基因的表达的类视黄醇化合物，具有减少的副作用，用于治疗对类维生素A治疗有反应的疾病和病症。

9. 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.

10. 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。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式