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1. 发明授权

US5679518A Method for finding transcription activators of the NER steroid hormone receptor 失效
标题翻译：找到NER类固醇激素受体的转录激活因子的方法
公开(公告)号：US5679518A
公开(公告)日：1997-10-21
申请号：US330283
申请日：1994-10-27
申请人： Eitan Friedman , M. Katharine Holloway , Gideon A. Rodan , Su Jane Rutledge , Azriel Schmidt , Robert L. Vogel
发明人： Eitan Friedman , M. Katharine Holloway , Gideon A. Rodan , Su Jane Rutledge , Azriel Schmidt , Robert L. Vogel
IPC分类号： C07D307/68 , C07K14/72 , C12N15/12 , C12Q1/68 , G01N33/74
CPC分类号： C07K14/721 , C07D307/68 , C07K2319/00
摘要： The NER receptor is a novel member of the steroid hormone receptor superfamily and has been prepared by cDNA cloning from a human osteosarcoma SAOS-2/B10 cell library. The complete sequence of human NER complementary DNA (Seq. ID No. 1), expression systems including a COS stable expression system, the expressed protein (SEQ. ID No. 2) and an assay using the COS expression system are disclosed. The assay may be used to identify agents which activate transcription mediated by the NER receptor, and which are useful for potentiating the activity of a modulator of a G-protein coupled receptor wherein the G-protein coupled receptor is a member of the steroid hormone receptor superfamily.
摘要翻译： NER受体是类固醇激素受体超家族的新成员，并通过人骨肉瘤SAOS-2 / B10细胞库的cDNA克隆制备。公开了人NER互补DNA（Seq.ID No.1）的完整序列，包括COS稳定表达系统的表达系统，表达的蛋白质（SEQ ID NO：2）和使用COS表达系统的测定法。该测定可用于鉴定激活由NER受体介导的转录的试剂，其可用于增强G蛋白偶联受体调节剂的活性，其中G蛋白偶联受体是类固醇激素受体的成员超家族

2. 发明授权

US5607967A Treatment of alzheimer's disease with 5-(tetradecyloxy)-2-furan carboxylic acid 失效
标题翻译：用5-（十四烷氧基）-2-呋喃羧酸治疗阿尔茨海默病
公开(公告)号：US5607967A
公开(公告)日：1997-03-04
申请号：US330518
申请日：1994-10-27
申请人： Eitan Friedman , M. Katharine Holloway , Gideon A. Rodan , Azriel Schmidt , Robert L. Vogel
发明人： Eitan Friedman , M. Katharine Holloway , Gideon A. Rodan , Azriel Schmidt , Robert L. Vogel
IPC分类号： A61K45/00 , A61K31/00 , A61K31/341 , A61K31/55 , A61K31/714 , A61K38/18 , A61P21/00 , A61P25/18 , A61P25/28 , A61P27/02 , A61K31/34
CPC分类号： A61K31/55 , A61K31/00 , A61K31/341 , A61K38/185
摘要： Use of the novel receptor NER TOFA (5-(tetradecyloxy)-2-furan-carboxylic acid) to treat Alzheimer's disease.
摘要翻译：使用新的受体NER TOFA（5-（十四烷氧基）-2-呋喃羧酸）治疗阿尔茨海默病。

3. 发明授权

US5939322A Human steroid receptor 失效
标题翻译：人类类固醇受体
公开(公告)号：US5939322A
公开(公告)日：1999-08-17
申请号：US646248
申请日：1996-05-14
申请人： Gideon A. Rodan , Su Jane Rutledge , Azriel Schmidt , Robert L. Vogel
发明人： Gideon A. Rodan , Su Jane Rutledge , Azriel Schmidt , Robert L. Vogel
IPC分类号： C07D307/68 , C07K14/72 , C12N15/12 , C07K14/705 , C12N15/63 , C12N15/85
CPC分类号： C07K14/721 , C07D307/68 , C07K2319/00
摘要： Through the use of the novel receptor NER in a screening procedure, TOFA (5-tetradecyloxy)-2-furan-carboxylic acid) has been found to modulate other receptors and to be a potent potentiator of other drugs. TOFA activates the NER receptor. The NER receptor is a novel member of the steroid hormone receptor family and has been prepared by cDNA cloning from a human osteosarcoma SAOS-2/B10 cell library. Also disclosed is the complete sequence of human NER cDNA; a COS stable expression system; the expressed NER protein; and an assay using the COS expression system. In addition, the invention relates to a method for identifying functional ligands of the NER receptor.
摘要翻译： PCT No.PCT / US95 / 13924 Sec。 371日期：1996年5月14日 102（e）日期1996年5月14日PCT提交1995年10月24日PCT公布。第WO96 / 13519号公报日期1996年5月9日通过在筛选程序中使用新型受体NER，已经发现TOFA（5-十四烷氧基）-2-呋喃羧酸）调节其他受体并成为其他药物的有效增强剂。 TOFA激活NER受体。 NER受体是类固醇激素受体家族的新成员，并通过人骨肉瘤SAOS-2 / B10细胞库的cDNA克隆制备。还公开了人NER cDNA的完整序列; COS稳定表达系统; 表达的NER蛋白; 和使用COS表达系统的测定法。另外本发明涉及一种鉴定NER受体功能性配体的方法。

4. 发明授权

US5530121A Carbamates of rapamycin 失效
公开(公告)号：US5530121A
公开(公告)日：1996-06-25
申请号：US451104
申请日：1995-05-25
申请人： Wenling Kao , Magid A. Abou-Gharbia , Robert L. Vogel
发明人： Wenling Kao , Magid A. Abou-Gharbia , Robert L. Vogel
IPC分类号： A61K31/395 , A61K31/44 , A61K31/675 , C07D491/06 , C07D498/04 , C07D498/16
CPC分类号： A61K31/70
摘要： A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, --CONH--[(CR.sup.3 R.sup.4).sub.m (--A--(CR.sup.5 R.sup.6).sub.n).sub.p ].sub.q --B; ##STR2## R.sup.3, R.sup.4, R.sup.5, R.sup.6, and B are each, independently, hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl, cycloalkyl, --OR.sup.7, --SR.sup.7, halogen, --CN, --NO.sub.2, --CF.sub.3, --COR.sup.7, --CO.sub.2 R.sup.7, --CONHR.sup.7, --SO.sub.2 R.sup.7, --OSO.sub.3 R.sup.7, --NR.sup.7 R.sup.8, --NHCOR.sup.7, --NHSO.sub.2 R.sup.7, or Ar;R.sup.7 and R.sup.8 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl;R.sup.9 and R.sup.10 are each, independently, alkyl , alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl, --CF.sub.3, --COR.sup.7, --CO.sub.2 R.sup.7, --CONHR.sup.7, --SO.sub.2 R.sup.7, or Ar;A is --CH.sub.2 --, --NR.sup.7, --O--, --S--, --SO--, --SO.sub.2 --, --PR.sup.7, --CO--, --NHCO--, --NHSO--, or --P(O)(R.sup.7)--;Ar is phenyl, naphthyl, pyridyl, quinolyl, isoquinolyl, quinoxalyl, thienyl, thionaphthyl, furyl, benzofuryl, benzodioxyl, benzoxazolyl, benzoisoxazolyl, indolyl, thiazolyl, isoxazolyl, pyrimidinyl, pyrazinyl, imidazolyl, benzopyranyl, benz[b]thiophenolyl, benzimidazolyl, benzthiazolyl, benzodioxolyl, piperidinyl, morpholinyl, piperazinyl, tetrahydrofuranyl, or pyrrolidinyl; wherein the Ar group may be optionally mono-, di-, or tri-substituted; ##STR3## is a nitrogen containing heterocycle that may be saturated, unsaturated, or partially unsaturated, and may be optionally mono-, di-, or tri- substituted; with the proviso that R.sup.1 and R.sup.2 are not both hydrogen;m=0-6;n=0-6;p=0-1;q=0-1;or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

5. 发明授权

US07271164B2 Cyclohepta[b][1,4]diazepino[6,7,1,-hi]indoles and derivatives 失效
标题翻译：环庚三烯[b] [1,4]二氮杂[6,7,1，-i]吲哚和衍生物
公开(公告)号：US07271164B2
公开(公告)日：2007-09-18
申请号：US10966227
申请日：2004-10-15
申请人： Annmarie L. Sabb , Robert L. Vogel
发明人： Annmarie L. Sabb , Robert L. Vogel
IPC分类号： A61K31/55 , A61P25/00 , A61P25/24 , C07D243/00
CPC分类号： C07D487/06
摘要： This invention provides compounds of the formula: wherein R1 and R2 are each, independently, H, alkyl, cycloalkyl, —CH2-cycloalkyl, alkoxy, halogen, fluorinated alkyl, —CN, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, or phenoyl or thiophenoyl; R3 and R4 are each, independently, H, alkyl or cycloalkyl; R5 is H or alkyl; R6 is H or; and the dashed line indicates an optional double bond; or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions and methods utilizing these compounds for the treatment or prevention of disorders including obsessive-compulsive disorder, depression, anxiety, generalized anxiety disorder, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.
摘要翻译：本发明提供下式的化合物：其中R 1和R 2各自独立地为H，烷基，环烷基，-CH 2 - 环烷基，烷氧基，卤素，氟化烷基，-CN，-NH-SO 2 - 烷基，-SO 2 -NH-烷基，烷基酰胺，氨基，烷基氨基，二烷基氨基，氟化烷氧基，酰基或酚酰基或噻吩甲酰基; R 3和R 4各自独立地为H，烷基或环烷基; R 5是H或烷基; R 6是H或; 虚线表示可选的双键; 或其药学上可接受的盐，以及利用这些化合物治疗或预防包括强迫症，抑郁症，焦虑症，广泛性焦虑症，精神分裂症，偏头痛，睡眠障碍，进食障碍，肥胖症，癫痫症，和脊髓损伤。

6. 发明授权

US5349060A Rapamycin 31-ester with N,N-dimethylglycine derivatives useful as immunosuppressive agents 失效
标题翻译：雷帕霉素31-酯与可用作免疫抑制剂的N，N-二甲基甘氨酸衍生物
公开(公告)号：US5349060A
公开(公告)日：1994-09-20
申请号：US58918
申请日：1993-05-06
申请人： Wenling Kao , Robert L. Vogel
发明人： Wenling Kao , Robert L. Vogel
IPC分类号： C07D498/18 , C07D491/16 , A61K31/395
CPC分类号： C07D498/18
摘要： A derivative of rapamycin of general formula (1) and (2) ##STR1## wherein ##STR2## or hydrogen; R.sup.2 =hydrogen, or lower alkyl having 1 to 6 carbon atoms; ##STR3## wherein X=hydrogen, lower alkyl having 1 to 6 carbon atoms, --CF.sub.3, --NO.sub.2, --OR.sup.2, NR.sup.2, SR.sup.2, or halogen; R.sup.4 =lower alkyl, alkenyl or alkynyl having 1 to 6 carbon atoms or an aromatic or heterocyclic moiety selected from the group consisting of phenyl, naphthyl, thiophenyl and quinolinyl;Y-=halide, methanesulfonate, toluene sulfonate or maleate; andZ=oxygen or OH and H.which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host versus graft disease, autoimmune diseases, and diseases of inflammation.
摘要翻译：（1）和（2）的雷帕霉素的衍生物其中图像或氢; R2 =氢或具有1至6个碳原子的低级烷基; 其中X =氢，具有1至6个碳原子的低级烷基，-CF 3，-NO 2，-OR 2，NR 2，SR 2或卤素; R4 =具有1至6个碳原子的低级烷基，烯基或炔基或选自苯基，萘基，噻吩基和喹啉基的芳族或杂环部分; Y- =卤化物，甲磺酸盐，甲苯磺酸盐或马来酸盐; Z =氧或OH和H.由于其免疫抑制活性可用于治疗移植排斥反应，宿主与移植物疾病，自身免疫性疾病和炎症疾病。

7. 发明授权

US5508399A Carbamates of rapamycin 失效
公开(公告)号：US5508399A
公开(公告)日：1996-04-16
申请号：US450835
申请日：1995-05-25
申请人： Wenling Kao , Magid A. Abou-Gharbia , Robert L. Vogel
发明人： Wenling Kao , Magid A. Abou-Gharbia , Robert L. Vogel
IPC分类号： A61K31/395 , A61K31/44 , A61K31/675 , C07D491/06 , C07D498/04 , C07D498/16
CPC分类号： A61K31/70
摘要： A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, --CONH--[(CR.sup.3 R.sup.4).sub.m (--A--(CR.sup.5 R.sup.6).sub.n).sub.p ].sub.q --B; ##STR2## R.sup.3, R.sup.4, R.sup.5, R.sup.6, and B are each, independently, hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl, cycloalkyl, --OR.sup.7, --SR.sup.7, halogen, --CN, --NO.sub.2, --CF.sub.3, --COR.sup.7, --CO.sub.2 R.sup.7, --CONHR.sup.7, --SO.sub.2 R.sup.7, --OSO.sub.3 R.sup.7, --NR.sup.7 R.sup.8, --NHCOR.sup.7, --NHSO.sub.2 R.sup.7, or Ar;R.sup.7 and R.sup.8 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloallcyl;R.sup.9 and R.sup.10 are each, independently, alkyl , alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl,, --CF.sub.3, --COR.sup.7, --CO.sub.2 R.sup.7, --CONHR.sup.7, --SO.sub.2 R.sup.7, or Ar;A is --CH.sub.2 --, --NR.sup.7 --, --O--, --S--, --SO--, --SO.sub.2 --, --PR.sup.7 --, --CO--, --NHCO--, --NHSO--, or --P(O)(R.sup.7)--;Ar is phenyl, naphthyl, pyridyl, quinolyl, isoquinolyl, quinoxalyl, thienyl, thionaphthyl, furyl, benzofuryl, benzodioxyl, benzoxazolyl, benzoisoxazolyl, indolyl, thiazolyl, isoxazolyl, pyrimidinyl, pyrazinyl, imidazolyl, benzopyranyl, benz[b]thiophenolyl, benzimidazolyl, benzthiazolyl, benzodioxolyl, piperidinyl, morpholinyl, piperazinyl, tetrahydrofuranyl, or pyrrolidinyl; wherein the Ar group may be optionally mono-, di-, or tri-substituted; ##STR3## is a nitrogen containing heterocycle that may be saturated, unsaturated, or partially unsaturated, and may be optionally mono-, di-, or tri- substituted; with the proviso that R.sup.1 and R.sup.2 are not both hydrogen;m=0-6;n=0-6;p=0-1;q=0-1;or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

8. 发明授权

US5260299A Rapamycin 42-sulfonates and 42-(N-Carboalkoxy)Sulfamates Useful as Immunosuppressive Agents 失效
标题翻译：雷帕霉素42-磺酸盐和42-（N-羧基烷氧基）磺酸盐可用作免疫抑制剂
公开(公告)号：US5260299A
公开(公告)日：1993-11-09
申请号：US917555
申请日：1992-07-21
申请人： Amedeo A. Failli , Wenling Kao , Robert J. Steffan , Robert L. Vogel
发明人： Amedeo A. Failli , Wenling Kao , Robert J. Steffan , Robert L. Vogel
IPC分类号： C07D498/18 , A61K31/395
CPC分类号： C07D498/18
摘要： A derivative of rapamycin of general formula (I) ##STR1## where R.sup.1 is alkyl, alkenyl, or alkynyl containing 1 to 6 carbon atoms; or an aromatic moiety selected from the group consisting of phenyl and naphthyl or a heterocyclic moiety selected from the group consisting of thiophenyl and quinolinyl or NHCO.sub.2 R.sup.2 wherein R.sup.2 is lower alkyl containing 1 to 6 carbon atoms or a pharmaceutically acceptable salt thereof, which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host versus graft disease, autoimmune diseases, and diseases of inflammation.
摘要翻译：通式（I）的雷帕霉素的衍生物其中R 1是含有1至6个碳原子的烷基，烯基或炔基; 或选自苯基和萘基的芳族部分或选自噻吩基和喹啉基或NHCO 2 R 2的杂环部分，其中R 2是含有1至6个碳原子的低级烷基或其药学上可接受的盐，其由于其免疫抑制活性可用于治疗移植排斥反应，宿主与移植物疾病，自身免疫疾病和炎症疾病。

9. 发明授权

US5177203A Rapamycin 42-sulfonates and 42-(N-carboalkoxy) sulfamates useful as immunosuppressive agents 失效
标题翻译：雷帕霉素42-磺酸盐和42-（N-烷氧羰基）氨基磺酸盐可用作免疫抑制剂
公开(公告)号：US5177203A
公开(公告)日：1993-01-05
申请号：US846637
申请日：1992-03-05
申请人： Amedeo A. Failli , Wenling Kao , Robert J. Steffan , Robert L. Vogel
发明人： Amedeo A. Failli , Wenling Kao , Robert J. Steffan , Robert L. Vogel
IPC分类号： C07D498/18
CPC分类号： C07D498/18
摘要： A derivative of rapamycin of general formula (I) ##STR1## where R.sup.1 is alkyl, alkenyl, or alkynyl containing 1 to 6 carbon atoms; or an aromatic moiety selected from the group consisting of phenyl and naphthyl or a heterocyclic moiety selected from the group consisting of thiophenyl and quinolinyl or NHCO.sub.2 R.sup.2 wherein R.sup.2 is lower alkyl containing 1 to 6 carbon atoms or a pharmaceutically acceptable salt thereof, which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host versus graft disease, autoimmune diseases, and diseases of inflammation.
摘要翻译：通式（I）的雷帕霉素的衍生物其中R 1是含有1至6个碳原子的烷基，烯基或炔基; 或选自苯基和萘基的芳族部分或选自噻吩基和喹啉基或NHCO 2 R 2的杂环部分，其中R 2是含有1至6个碳原子的低级烷基或其药学上可接受的盐，其由于其免疫抑制活性可用于治疗移植排斥反应，宿主与移植物疾病，自身免疫疾病和炎症疾病。

10. 发明授权

US5118678A Carbamates of rapamycin 失效
标题翻译：雷帕霉素的氨基甲酸酯
公开(公告)号：US5118678A
公开(公告)日：1992-06-02
申请号：US686728
申请日：1991-04-17
申请人： Wenling Kao , Robert L. Vogel , John H. Musser
发明人： Wenling Kao , Robert L. Vogel , John H. Musser
IPC分类号： C07D498/18
CPC分类号： C07D498/18
摘要： A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or --CONH(CR.sup.3 R.sup.4).sub.n --X;R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, aralkyl, cycloalkyl, halogen, or trifluoromethyl;X ix hydrogen, lower alkyl, cycloalkyl, trifluoromethyl, nitro, alkoxy, carboalkoxy, aralkyl, halo, dialkylamino, thioalkyl, or Y;Y is a phenyl group which may be optionally mono-, di-, or tri- substituted with a group selected from alkyl, aralkyl, alkoxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, dialkylamino, or alkylthio;n=0-5;with the proviso that R.sup.1 and R.sup.2 are not both hydrogen and when n=0, X is lower alkyl, cycloalkyl, aralkyl, or Y;or a pharmaceutically acceptable salt thereof when X is dialkylamino, which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases and diseases of inflammation; by virtue of its antitumor activity is useful in treating solid tumors; and by virtue of its antifungal activity is useful in treating fungal infections.
摘要翻译：结构的化合物，其中R 1和R 2各自独立地为氢或-CONH（CR 3 R 4）n -X; R 3和R 4各自独立地为氢，烷基，芳烷基，环烷基，卤素或三氟甲基; 硝基，烷氧基，烷氧基，芳烷基，卤素，二烷基氨基，硫代烷基或Y; Y是可以任选被选自烷基，芳烷基，烷氧基，氰基，卤素，硝基，烷氧基，三氟甲基，二烷基氨基或烷硫基中的基团单，二或三取代的苯基。 n = 0-5; 条件是R1和R2不同时为氢，当n = 0时，X为低级烷基，环烷基，芳烷基或Y; 当X是二烷基氨基时，或其药学上可接受的盐，其由于其免疫抑制活性可用于治疗移植排斥反应，宿主与移植物疾病，自身免疫疾病和炎症疾病; 由于其抗肿瘤活性可用于治疗实体瘤; 并且由于其抗真菌活性可用于治疗真菌感染。

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