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11. 发明授权

US5385910A Gem-distributed esters of rapamycin 失效
标题翻译：雷公藤分泌的酯
公开(公告)号：US5385910A
公开(公告)日：1995-01-31
申请号：US156334
申请日：1993-11-22
申请人： Timothy D. Ocain , Guy A. Schiehser
发明人： Timothy D. Ocain , Guy A. Schiehser
IPC分类号： C07D498/18 , A61K31/445 , C07D471/04
CPC分类号： C07D498/18
摘要： Compounds of the structure ##STR1## R and R.sup.1 are each, independently, hydrogen, or ##STR2## R.sup.2 and R.sup.3 are each, independently, alkyl, arylalkyl, or may be taken together to form a cycloalkyl ring;R.sup.4 and R.sup.5 are each, independently, hydrogen, alkyl, arylalkyl, or may be taken together to form a saturated heterocycle wherein the heterocyclic ring may be optionally mono-, di-, or tri-substituted;m=0-1; andn=0-6;with the proviso that R and R.sup.1 are not both hydrogen, or a pharmaceutically acceptable salt thereof, and ##STR3## R.sup.1 is ##STR4## R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, arylalkyl, or may be taken together to form a cycloalkyl ring;R.sup.4 and R.sup.5 are each, independently, hydrogen, alkyl, arylalkyl, or may be taken together to form a saturated heterocycle wherein the heterocyclic ring may be optionally mono-, di-, or tri-substituted;m=0-1; andn=0-6;or a pharmaceutically acceptable salt thereof which are useful as immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agents.
摘要翻译：结构式I R和R 1的化合物各自独立地为氢，或者R 2和R 3各自独立地为烷基，芳基烷基，或者可以一起形成环烷基环; R 4和R 5各自独立地为氢，烷基，芳基烷基，或者可以一起形成饱和杂环，其中杂环可以是任选的单，二或三取代; m = 0-1; 并且n = 0-6; 条件是R和R 1不是氢或其药学上可接受的盐，而R 2和R 3各自独立地为氢，烷基，芳基烷基，或者可以一起形成环烷基环; R 4和R 5各自独立地为氢，烷基，芳基烷基，或者可以一起形成饱和杂环，其中杂环可以是任选的单，二或三取代; m = 0-1; 并且n = 0-6; 或其药学上可接受的盐，其可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂。

12. 发明授权

US5064965A Renin inhibitors 失效
标题翻译：肾素抑制剂
公开(公告)号：US5064965A
公开(公告)日：1991-11-12
申请号：US614545
申请日：1990-11-16
申请人： Timothy D. Ocain , David D. Deininger
发明人： Timothy D. Ocain , David D. Deininger
IPC分类号： C07D207/26 , C07D207/27 , C07D209/46 , C07D209/48 , C07D221/14 , C07D263/22 , C07D403/12 , C07D471/04 , C07D487/04
CPC分类号： C07D207/27 , C07D209/46 , C07D209/48 , C07D221/14 , C07D263/22 , C07D403/12 , C07D471/04 , C07D487/04
摘要： A compound of the formula: ##STR1## wherein A is ##STR2## in which X is .dbd.CH-- or .dbd.N--; R.sup.2 is hydrogen, alky, phenyl, benzyl or phenylethyl; Y is --CH.sub.2 --, --NH-- or --O--; and Z is --H.sub.2 or O; b is His, Leu, Ile, Nva, Nle, Ala or Val; and R.sup.1 is hydrogen, alkyl, phenyl or phenylakyl; or a pharmaceutically acceptable salt thereof are renin inhibitors.
摘要翻译：下式的化合物：其中A是其中X为= CH-或= N-的 R2是氢，烷基，苯基，苄基或苯基乙基; Y是-CH 2 - ， - NH-或-O-; Z为-H 2或O; b是His，Leu，Ile，Nva，Nle，Ala或Val; R1是氢，烷基，苯基或苯基烷基; 或其药学上可接受的盐是肾素抑制剂。

13. 发明授权

US5023338A Renin inhibitors 失效
标题翻译：肾素抑制剂
公开(公告)号：US5023338A
公开(公告)日：1991-06-11
申请号：US490810
申请日：1990-03-08
申请人： Timothy D. Ocain , David D. Deininger
发明人： Timothy D. Ocain , David D. Deininger
IPC分类号： C07D207/26 , C07D207/27 , C07D209/46 , C07D209/48 , C07D221/14 , C07D263/22 , C07D403/12 , C07D471/04 , C07D487/04
CPC分类号： C07D207/27 , C07D209/46 , C07D209/48 , C07D221/14 , C07D263/22 , C07D403/12 , C07D471/04 , C07D487/04
摘要： A compound of the formula: ##STR1## wherein A is ##STR2## in which X is .dbd.CH-- or .dbd.N--; R.sup.2 is hydrogen, alky, phenyl, benzyl or phenethyl; Y is --CH.sub.2 --, --NH-- or --O--; and Z is --H.sub.2 or .dbd.O; B is His, Leu, Ile, Nva, Nle, Ala or Val; and R.sup.1 is hydrogen, alkyl, phenyl or phenylalkyl; or a pharmaceutically acceptable salt thereof are renin inhibitors.
摘要翻译：下式的化合物：其中A是其中X为= CH-或= N-的 R2是氢，烷基，苯基，苄基或苯乙基; Y是-CH 2 - ， - NH-或-O-; Z为-H2或= O; B是His，Leu，Ile，Nva，Nle，Ala或Val; 且R 1为氢，烷基，苯基或苯基烷基; 或其药学上可接受的盐是肾素抑制剂。

14. 发明授权

US07897733B2 Rapamycin conjugates and antibodies 失效
标题翻译：雷帕霉素缀合物和抗体
公开(公告)号：US07897733B2
公开(公告)日：2011-03-01
申请号：US11272070
申请日：2005-11-14
申请人： Katherine L. Molnar-Kimber , Craig E. Caufield , Timothy D. Ocain
发明人： Katherine L. Molnar-Kimber , Craig E. Caufield , Timothy D. Ocain
IPC分类号： C07K16/00 , C07K1/04 , C12N5/00 , C12P21/08
CPC分类号： C07K16/14 , A61K31/435 , A61K47/643 , A61K47/6835 , C07K16/1292 , C12N9/0065 , G01N33/533 , G01N33/9446 , Y10S530/809
摘要： Provided are rapamycin conjugates which are useful as immunogenic molecules for the generation of antibodies specific for rapamycin, for measuring levels of rapamycin or derivatives thereof; for isolating rapamycin binding proteins; and detecting antibodies specific for rapamycin or derivatives thereof. This invention also provides a rapamycin specific monoclonal antibody.
摘要翻译：提供的雷帕霉素缀合物可用作产生雷帕霉素特异性抗体的免疫原性分子，用于测量雷帕霉素或其衍生物的水平; 用于分离雷帕霉素结合蛋白; 并检测对雷帕霉素或其衍生物特异的抗体。本发明还提供了雷帕霉素特异性单克隆抗体。

15. 发明授权

US07247438B1 Methods of identifying agents which enhance caspase activity 失效
标题翻译：鉴定增强半胱天冬酶活性的药物的方法
公开(公告)号：US07247438B1
公开(公告)日：2007-07-24
申请号：US08948124
申请日：1997-10-09
申请人： Ellis Reinherz , Linda Clayton , Timothy D. Ocain , Raymond J. Patch
发明人： Ellis Reinherz , Linda Clayton , Timothy D. Ocain , Raymond J. Patch
IPC分类号： G01N33/53
CPC分类号： C12N9/6475 , A61K38/00
摘要： Methods for identifying agents which enhance the activity of a caspase according to the invention are described, as well as methods for enhancing caspase activity and methods for enhancing apoptosis in a lymphocyte.
摘要翻译：本发明描述了提高半胱天冬酶活性的试剂的方法，以及增强半胱天冬酶活性的方法和增强淋巴细胞凋亡的方法。

16. 发明授权

US06632830B1 ACE-2 inhibiting compounds and methods of use thereof 失效
标题翻译： ACE-2抑制化合物及其使用方法
公开(公告)号：US06632830B1
公开(公告)日：2003-10-14
申请号：US09561759
申请日：2000-04-28
申请人： Susan L. Acton , Timothy D. Ocain , Alexandra E. Gould , Natalie A. Dales , Bing Guan , James A. Brown
发明人： Susan L. Acton , Timothy D. Ocain , Alexandra E. Gould , Natalie A. Dales , Bing Guan , James A. Brown
IPC分类号： A61K31194
CPC分类号： C07D231/12 , C07B2200/07 , C07C229/16 , C07C229/24 , C07C229/26 , C07C229/36 , C07C271/20 , C07C275/24 , C07C323/52 , C07C323/58 , C07C2601/02 , C07C2601/14 , C07D209/20 , C07D213/55 , C07D233/64 , C07D235/16 , C07D249/08 , C07D261/08 , C07D277/06 , C07D277/30 , C07D277/40 , C07D277/42 , C07D333/24 , C07D405/06
摘要： ACE-2 inhibiting compounds are disclosed. These compounds include compounds of formula (IV): wherein the variables are as described in the specification. Pharmaceutical compositions containing the compounds are also discussed. The pharmaceutical compositions may contain an effective amount of a compound of the invention to treat ACE-2 associated disorders such as a blood pressure related disease or disorder, cell proliferation disorder, kidney disorder, kinetensin associated disorder, inflammation associated disorder, or an allergic disorder.
摘要翻译：公开了ACE-2抑制化合物。这些化合物包括式（IV）的化合物：其中变量如说明书中所述。还讨论了含有这些化合物的药物组合物。药物组合物可以含有有效量的本发明化合物以治疗ACE-2相关疾病，例如与血压相关的疾病或病症，细胞增殖病症，肾脏疾病，激素相关病症，炎症相关疾病或过敏性疾病。

17. 发明授权

US5234936A Pyrimidocycloalkanes as a II antagonists 失效
公开(公告)号：US5234936A
公开(公告)日：1993-08-10
申请号：US782017
申请日：1991-10-24
申请人： John L. Primeau , Lloyd M. Garrick , Timothy D. Ocain , Richard M. Soll , Paul J. Dollings
发明人： John L. Primeau , Lloyd M. Garrick , Timothy D. Ocain , Richard M. Soll , Paul J. Dollings
IPC分类号： C07D239/74 , A61K31/505 , A61K31/517 , A61P3/06 , A61P9/00 , A61P9/12 , C07D239/70 , C07D239/78 , C07D239/80 , C07D239/94 , C07D239/95 , C07D403/12
CPC分类号： C07D403/12 , C07D239/70 , C07D239/94
摘要： There are disclosed compounds of the general formula I: ##STR1## wherein X is H, NR.sup.12 R.sup.13, OR.sup.14, CN, F, Cl, I, Br, perfluoroalkyl, alkyl, alkoxy, alkyl-OH, alkoxyalkyl, --(CH.sub.2).sub.n CO.sub.2 R.sup.14, --(CH.sub.2).sub.n CONR.sup.12 R.sup.13 ;Y is NR.sup.15, NR.sup.18 CR.sup.16 R.sup.17, CR.sup.16 R.sup.17 NR.sup.15 ;R.sup.1 is 5-tetrazolyl, CO.sub.2 R.sup.14, SO.sub.3 H, NHSO.sub.2 CH.sub.3, NHSO.sub.2 CF.sub.3 ;R.sup.2, R.sup.3 is H, alkyl, alkoxy, alkoxyalkyl, alkyl-OH perfluoroalkyl, aralkyl, CN, NO.sub.2, SO.sub.2 R.sup.19, --(CH.sub.2).sub.n CO.sub.2 R.sup.14, --(CH.sub.2).sub.n CONR.sup.12 R.sup.13, OR.sup.14, F, Cl, Br, I, NR.sup.12 R.sup.13 ;R.sup.4 -R.sup.11 is H, F, alkyl, alkoxy, alkoxyalkyl, --OCOR.sup.14, alkyl-OH, perfluoroalkyl, aralkyl, aryl, CN, NO.sub.2, SO.sub.2 R.sup.19, --(CH.sub.2).sub.n CO.sub.2 R.sup.14, --(CH.sub.2).sub.n CONR.sup.12 R.sup.13, OH, OR.sup.14, --NR.sup.12 R.sup.13, any two geminal groups can be O or CH.sub.2 ;R.sup.12, R.sup.13 is H, alkyl, aralkyl;R.sup.14 is H, alkyl, aralkyl, alkoxyalkyl;R.sup.15 is H, alkyl, --(CH.sub.2).sub.n CO.sub.2 R.sup.14, alkoxyalkyl, aralkyl, --(CH.sub.2).sub.n CONR.sup.12 R.sup.13, OR.sup.14, perfluoroalkyl, alkyl-OH, --COR.sup.14, --CONR.sup.12 R.sup.13 ;R.sup.16, R.sup.17 is H, alkyl, alkoxyalkyl, alkyl-OH, perfluoroalkyl, aralkyl, CN, NO.sub.2, SO.sub.2 R.sup.19, --(CH.sub.2).sub.n CO.sub.2 R.sup.14, --(CH.sub.2).sub.n CONR.sup.12 R.sup.13 ;R.sup.18 is H, alkoxyalkyl, alkyl-OH, perfluoroalkyl, aralkyl, OR.sup.14, --(CH.sub.2).sub.n CO.sub.2 R.sup.14, --(CH.sub.2).sub.n CONR.sup.12 R.sup.13, alkyl, --COR.sup.14, --CONR.sup.12 R.sup.13 ;R.sup.19 is alkyl, aralkyl;n is 0, 1, 2 or 3;m is 1-5;wherein alkyl is defined as 1-8 carbons, branched or straight chain; perfluoroalkyl is defined as 1-6 carbons; aralkyl is defined as 7-12 carbons or 7-12 carbons substituted with fluorine, bromine or chlorine; aryl is defined as 6-10 carbons or 6-10 carbons substituted with fluorine, bromine or chlorine and the pharmaceutically acceptable salts, solvates and hydrates thereof, which by virtue of their ability to antagonize angiotensin II are useful for the treatment of hypertension and congestive heart-failure. The compounds are also useful for reducing lipid levels in the blood plasma and are thus useful for treating hyperlipidemia and hypercholesterolemia. Also disclosed are processes for the production of said compounds and pharmaceutical compositions containing said compounds.

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