专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

11. 发明授权

US5959109A Compounds and methods for increasing endogenous levels of corticotropin-releasing factor 失效
标题翻译：增加促肾上腺皮质激素释放因子内源性水平的化合物和方法
公开(公告)号：US5959109A
公开(公告)日：1999-09-28
申请号：US645637
申请日：1996-05-15
申请人： Jeffrey P. Whitten , James R. McCarthy , Zhengyu Liu , Charles Q. Huang , Philip E. Erickson , Dominic P. Behan
发明人： Jeffrey P. Whitten , James R. McCarthy , Zhengyu Liu , Charles Q. Huang , Philip E. Erickson , Dominic P. Behan
IPC分类号： A61K31/00 , A61K31/35 , A61K31/352 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4168 , A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/433 , A61K31/505 , A61K31/513 , A61P5/00 , A61P43/00 , C07D239/62 , C07D239/66 , C07D311/56 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D473/08 , C07D487/04 , C07D239/02
CPC分类号： C07D409/14 , C07D239/62 , C07D239/66 , C07D311/56 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D473/08 , C07D487/04
摘要： Ligand inhibitors for increasing levels of free corticotropin-releasing factor (CRF) in the brain. Such ligand inhibitors cause release of CRF from the CRF/CRF-binding protein complex. Administration of the ligand inhibitors provide improvement in learning and memory, result in decreased food intake and/or provide treatment for diseases associated with low levels of CRF in the brain, notably Alzheimer's disease. The ligand inhibitor is represented by the formula: ##STR1##
摘要翻译：增加脑中游离促皮质激素释放因子（CRF）水平的配体抑制剂。这种配体抑制剂引起CRF / CRF结合蛋白复合物的CRF释放。配体抑制剂的施用提供了学习和记忆的改善，导致食物摄取减少和/或提供与脑中低水平CRF相关疾病，特别是阿尔茨海默氏病的治疗。配体抑制剂由下式表示：

12. 发明授权

US5512678A 5-(1-fluoro-vinyl)-1H-pyrimidine-2,4-dione derivatives useful as antineoplastic agents 失效
标题翻译：可用作抗肿瘤剂的5-（1-氟 - 乙烯基）-1H-嘧啶-2,4-二酮衍生物
公开(公告)号：US5512678A
公开(公告)日：1996-04-30
申请号：US236599
申请日：1994-04-29
申请人： James R. McCarthy , Donald P. Matthews , Jeffrey S. Sabol
发明人： James R. McCarthy , Donald P. Matthews , Jeffrey S. Sabol
IPC分类号： C07D239/54 , C07H19/06 , C07D405/04 , A61K31/505 , C07D239/02
CPC分类号： C07D239/54 , C07H19/06
摘要： The present invention provides novel 5-(1-fluorovinyl)-1H-pyrimidine-2,4-dione derivatives which are useful as antineoplastic agents by themselves or in conjunctive therapy with the antineoplastic agent 5-fluorouracil.
摘要翻译：本发明提供了新颖的5-（1-氟乙烯基）-1H-嘧啶-2,4-二酮衍生物，其自身可用作抗肿瘤剂，或与抗肿瘤药物5-氟尿嘧啶联合治疗。

13. 发明授权

US5147863A 2,2'-bi-1H-imidazoles 失效
标题翻译： 2,2'-联-1H-咪唑
公开(公告)号：US5147863A
公开(公告)日：1992-09-15
申请号：US600295
申请日：1990-10-17
申请人： Donald P. Matthews , Jeffrey P. Whitten , James R. McCarthy
发明人： Donald P. Matthews , Jeffrey P. Whitten , James R. McCarthy
IPC分类号： C07D233/06 , C07D233/54 , C07D233/68 , C07D233/90 , C07D521/00 , C07F7/08
CPC分类号： C07D233/64 , C07D231/12 , C07D233/06 , C07D233/56 , C07D233/68 , C07D233/90 , C07D249/08 , C07F7/0812
摘要： This invention relates to novel derivatives of 2,2'-bi-1H-imidazoles, to the processes and intermediates used in their preparation, to their ability to exert the pharmacologic effects of lowering high blood pressure and of increasing heart contractile force and to their use as chemotherpauetic agents useful in treating cardiac insufficiency and hypertension.
摘要翻译：本发明涉及2,2'-双-1H-咪唑的新型衍生物，其制备中使用的方法和中间体，其发挥降低高血压和增加心脏收缩力的药理作用及其增加心脏收缩力的能力用作治疗心功能不全和高血压的化学疗法。

14. 发明授权

US4868315A Novel aryloxycycloalkanolaminoalkylene aryl ketones 失效
标题翻译：新型芳氧基环烷醇基氨基亚烷基芳基酮
公开(公告)号：US4868315A
公开(公告)日：1989-09-19
申请号：US141737
申请日：1988-01-11
申请人： Michael E. LeTourneau , James R. McCarthy , Donald L. Trepanier
发明人： Michael E. LeTourneau , James R. McCarthy , Donald L. Trepanier
IPC分类号： C07C45/68 , C07C45/75 , C07C49/653 , C07C49/683 , C07C49/755 , C07D209/08 , C07D303/22 , C07D303/36 , C07D307/79 , C07D333/52 , C07D333/54 , C07D463/00
CPC分类号： C07D303/22 , C07C247/00 , C07C45/68 , C07C45/75 , C07C49/683 , C07C49/755 , C07D209/08 , C07D303/36 , C07D307/79 , C07D333/54
摘要： This invention relates to aryloxycycloalkanolaminoalkylene aryl ketones to the processes for their preparation and to their use as antihypertensive agents.
摘要翻译：本发明涉及芳氧基环烷醇氨基亚烷基芳基酮与其制备方法及其作为抗高血压剂的用途。

15. 发明授权

US4108853A N,15-Didehydro-15-deoxo-pyrimidino-(4,5-b)rifamycin S 失效
标题翻译： N，15-二氢-15-脱氧嘧啶并（4,5-b）利福霉素S
公开(公告)号：US4108853A
公开(公告)日：1978-08-22
申请号：US802214
申请日：1977-05-31
申请人： James R. McCarthy , Jimmie L. Moore
发明人： James R. McCarthy , Jimmie L. Moore
IPC分类号： C07D498/18 , C07D241/36 , A61K31/505
CPC分类号： C07D498/18
摘要： The subject compound is prepared by an activated manganese dioxide oxidation of N,15-didehydro-15-deoxo-3,15-epi(methano(imino)rifamycin SV. The new compound has antimicrobial utility.
摘要翻译：本发明化合物通过活化二氧化锰氧化N，15-二脱氢-15-脱氧-3,15-表（亚硝基）利福霉素SV制备。新化合物具有抗菌效用。

16. 发明授权

US06723721B2 CRF receptor antagonists and methods relating thereto 有权
标题翻译： CRF受体拮抗剂及其相关方法
公开(公告)号：US06723721B2
公开(公告)日：2004-04-20
申请号：US10027789
申请日：2001-12-20
申请人： Mustapha Haddach , Zhiqiang Guo , James R. McCarthy
发明人： Mustapha Haddach , Zhiqiang Guo , James R. McCarthy
IPC分类号： A61K31495
CPC分类号： C07D471/16 , C07D487/16
摘要： Compounds are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, including stroke. The compounds of this invention have the following structures: wherein n, m, R, R1, R2, X and Ar are as defined herein, including stereoisomes and pharmaceutically acceptable salts thereof.
摘要翻译：公开了可用于治疗多种疾病的化合物，包括治疗在温血动物（包括中风）中表现出CRF过度分泌的病症。本发明的化合物具有以下结构：其中n，m，R，R 1，R 2，X和Ar如本文所定义，包括立体异构体及其药学上可接受的盐。

17. 发明授权

US06613777B1 CRF antagonistic pyrazolo[4,3-b]pyridines 有权
标题翻译： CRF拮抗性吡唑并[4,3-b]吡啶
公开(公告)号：US06613777B1
公开(公告)日：2003-09-02
申请号：US09623634
申请日：2001-02-20
申请人： Chen Chen , Keith M. Wilcoxen , Charles Q. Huang , Mustapha Hadduch , James R. McCarthy
发明人： Chen Chen , Keith M. Wilcoxen , Charles Q. Huang , Mustapha Hadduch , James R. McCarthy
IPC分类号： A61K3144
CPC分类号： C07D471/04
摘要： This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R1 is C1-6alkyl, NR5R6, OR6 or SR6; R2 is C1-6alkyl, C1-6alkyloxy, or C1-6alkylthio; R3 is Ar1 or Het1; R4 is hydrogen or C1-6alkyl; R5 is hydrogen, C1-8alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxyC1-6alkyl, mono- or di(C1-6alkyl)amino-C1-6alkyl or C1-6alkyloxyC1-6alkyl; R6 is C1-8alkyl, mono- or di(C3-6cycloalkyl)methyl, Ar2C1-6alkyl, Ar2oxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, tetrahydrofuranylmethyl, C1-6alkylthioC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, or C1-6alkylcarbonylC1-6alkyl; or R5 and R6 taken together with the nitrogen atom to which they are attached may form a pyrrolidinyl, piperidinyl, homopiperidinyl, morpholinyl, or thiomorpholinyl group, optionally substituted with 1 or 2 substituents each independently selected from C1-6alkyl or C1-6alkyloxyC1-6alkyl; and and Ar1 and Ar2 are each optionally substituted phenyl; and Het1 is optionally substituted pyridinyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).
摘要翻译：本发明涉及包括其立体异构体及其药学上可接受的酸加成盐形式的化合物，其中R 1是C 1-6烷基，NR 5 R 6，OR 6或SR 6; R2是C1-6烷基，C1-6烷氧基或C1-6烷硫基; R3是Ar1或Het1; R4是氢或C1-6烷基; R5是氢，C1-8烷基，一或二（C3-6环烷基）甲基，C3-6环烷基，C3-6烯基，羟基C1-6烷基，C1-6烷基羰基氧基C 1-6烷基，单或二（C1-6烷基）氨基C1- C 1-6烷基或C 1-6烷氧基C 1-6烷基; R 6是C 1-8烷基，单或二（C 3-6环烷基）甲基，Ar 2 C 1-6烷基，Ar 2氧基C 1-6烷基，C 1-6烷氧基C 1-6烷基，羟基C 1-6烷基，C 3-6烯基，噻吩基甲基，呋喃基甲基，四氢呋喃基甲基，C 1-6烷硫基C 1-6烷基，单或二（C 1-6烷基）氨基C 1-6烷基，二（C 1-6烷基）氨基或C 1-6烷基羰基C 1-6烷基; 或者R 5和R 6与它们所连接的氮原子一起形成吡咯烷基，哌啶基，高哌啶基，吗啉基或硫代吗啉基，任选地被1或2个独立地选自C 1-6烷基或C 1-6烷氧基C 1-6烷基的取代基取代 ; 并且Ar 1和Ar 2各自为任选取代的苯基; Het1是任选取代的吡啶基; 具有CRF受体拮抗特性; 含有这些化合物作为活性成分的药物组合物; 通过施用有效量的式（I）化合物来治疗与CRF过度分泌有关的疾病的方法，例如抑郁症，焦虑症，药物滥用。

18. 发明授权

US06348466B1 CRF receptor antagonists and methods relating thereto 失效
标题翻译： CRF受体拮抗剂及其相关方法
公开(公告)号：US06348466B1
公开(公告)日：2002-02-19
申请号：US09439841
申请日：1999-11-12
申请人： Mustapha Haddach , Zhiqiang Guo , James R. McCarthy
发明人： Mustapha Haddach , Zhiqiang Guo , James R. McCarthy
IPC分类号： A61K31495
CPC分类号： C07D471/16 , C07D487/16
摘要： Compounds are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, including stroke. The compounds of this invention have the following structures: wherein n, m, R, R1, R2, X and Ar are as defined herein, including stereoisomes and pharmaceutically acceptable salts thereof.
摘要翻译：公开了可用于治疗多种疾病的化合物，包括治疗在温血动物（包括中风）中表现出CRF过度分泌的病症。本发明的化合物具有以下结构：其中n，m，R，R 1，R 2，X和Ar如本文所定义，包括立体异构体及其药学上可接受的盐。

19. 发明授权

US5589587A Process for the preparation of ribonucleotide reductase inhibitors 失效
标题翻译：制备核糖核苷酸还原酶抑制剂的方法
公开(公告)号：US5589587A
公开(公告)日：1996-12-31
申请号：US419315
申请日：1995-04-10
申请人： James R. McCarthy , Donald P. Matthews , Jeffrey S. Sabol , James R. McConnell , Richard E. Donaldson , Robert Duquid
发明人： James R. McCarthy , Donald P. Matthews , Jeffrey S. Sabol , James R. McConnell , Richard E. Donaldson , Robert Duquid
IPC分类号： C07D405/04 , C07H1/00 , C07H19/06 , C07H23/00
CPC分类号： C07D405/04 , C07H19/06 , C07H23/00
摘要： The present invention is directed toward a novel process of preparing 2'-exocyclic vinylfluoride derivatives of cytidine analogues for use as ribonucleotide reductase inhibitors. The novel process of the present invention utilizes a cytidine derivative as the required starting material and provides the ribonucleotide reductase inhibitor in a more efficient than the reaction sequence. The process is more efficient than the process disclosed by McCarthy et al. in European Patent Application Publication No. 0 372 268 published Jun. 13, 1990, in that it requires fewer chromatographies and results in an overall yield of greater than 25% for the five steps. The present invention further provides the ribonucleotide reductase inhibitor in a four step reaction sequence and results in an overall yield of greater than 35%.
摘要翻译：本发明涉及制备用作核糖核苷酸还原酶抑制剂的胞苷类似物的2'-环状氟代乙烯衍生物的新方法。本发明的新方法利用胞苷衍生物作为所需的原料，并且比反应顺序更有效地提供核糖核苷酸还原酶抑制剂。该过程比McCarthy等人公开的方法更有效。在1990年6月13日公布的欧洲专利申请公开号0 372 268中，其需要较少的色谱和结果，五个步骤的总产率大于25％。本发明还提供了四步反应序列中的核糖核苷酸还原酶抑制剂，其总产率大于35％。

20. 发明授权

US5473104A Process for the preparation of L-carnitine 失效
标题翻译：制备左旋肉碱的方法
公开(公告)号：US5473104A
公开(公告)日：1995-12-05
申请号：US306502
申请日：1994-09-13
申请人： James R. McCarthy
发明人： James R. McCarthy
IPC分类号： C07C227/32 , C07C229/12
CPC分类号： C07C227/32
摘要： There is disclosed a process for preparation of L-carnitine from (S)-3-hydroxybutyrolactone. The process is a two-step preparation in which (S)-3-hydroxybutyrolactone is first converted to a hydroxy-activated form and subsequently transformed to L-carnitine by treatment of the hydroxy-activated (S)-3-hydroxybutyrolactone with trimethylamine in water.
摘要翻译：公开了从（S）-3-羟基丁内酯制备L-肉碱的方法。该方法是两步制备，其中（S）-3-羟基丁内酯首先转化为羟基活化形式，随后通过用三甲胺处理羟基活化（S）-3-羟基丁内酯，随后转化成L-肉毒碱水。

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