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1. 发明授权

US07405229B2 Cathepsin cysteine protease inhibitors 有权
标题翻译：组织蛋白酶半胱氨酸蛋白酶抑制剂
公开(公告)号：US07405229B2
公开(公告)日：2008-07-29
申请号：US10560672
申请日：2004-06-28
申请人： Christopher Bayly , Cameron Black , Sheldon Crane , Daniel J. McKay , Renata Oballa , Joel Robichaud
发明人： Christopher Bayly , Cameron Black , Sheldon Crane , Daniel J. McKay , Renata Oballa , Joel Robichaud
IPC分类号： A61K31/44 , A61K31/445 , A61K31/417 , A61K31/4184 , C07D211/80 , C07D233/54 , C07D235/04
CPC分类号： C07D213/83 , C07C255/29 , C07C311/06 , C07C323/25 , C07C323/49 , C07C323/60 , C07C323/61 , C07C323/62 , C07C2601/02 , C07C2601/14 , C07D211/20 , C07D213/32 , C07D231/12 , C07D233/64 , C07D235/06 , C07D257/04
摘要： This invention relates to a class of compounds having the general formula (I) which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
摘要翻译：本发明涉及一类具有通式（I）的化合物，它是半胱氨酸蛋白酶抑制剂，包括但不限于组织蛋白酶K，L，S和B的抑制剂。这些化合物可用于治疗其中抑制骨的疾病表示吸收，如骨质疏松症。

2. 发明授权

US07371747B2 Cyanoalkylamino derivatives as protease inhibitors 失效
标题翻译：氰基烷基氨基衍生物作为蛋白酶抑制剂
公开(公告)号：US07371747B2
公开(公告)日：2008-05-13
申请号：US10495387
申请日：2002-11-13
申请人： Cameron Black , Sheldon N. Crane , Dana Davis , Eduardo L. Setti
发明人： Cameron Black , Sheldon N. Crane , Dana Davis , Eduardo L. Setti
IPC分类号： A61K31/535
CPC分类号： C07D213/40 , C07C317/44 , C07C323/60 , C07C323/65 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2602/02 , C07C2602/16 , C07C2602/20 , C07C2602/42 , C07C2602/50 , C07D211/58 , C07D213/32 , C07D213/70 , C07D213/74 , C07D213/81 , C07D213/82 , C07D233/84 , C07D239/38 , C07D263/58 , C07D277/16 , C07D277/42 , C07D277/74 , C07D307/38 , C07D333/20
摘要： The present invention is directed to novel cyanoalkylamino derivatives that are inhibitors of cysteine protease such as cathepsins K, S, B and L, in particular cathepsin K Pharmaceutical composition comprising these compounds, method of treating diseases mediated by unregulated cysteine protease activity, in particular cathepsin K utilizing these compounds and methods of preparing these compounds are also disclosed.
摘要翻译：本发明涉及新的氰基烷基氨基衍生物，其是半胱氨酸蛋白酶如组织蛋白酶K，S，B和L的抑制剂，特别是组织蛋白酶K包含这些化合物的药物组合物，治疗由不受调节的半胱氨酸蛋白酶活性介导的疾病的方法，特别是组织蛋白酶还公开了利用这些化合物的K和制备这些化合物的方法。

3. 发明申请

US20030065011A1 Substituted pyridines as selective cyclooxygenase-2 inhibitors 有权
标题翻译：取代的吡啶作为选择性环氧合酶-2抑制剂
公开(公告)号：US20030065011A1
公开(公告)日：2003-04-03
申请号：US10021187
申请日：2001-10-30
申请人： Merck Frosst Canada & Co.
发明人： Daniel Dube , Rejean Fortin , Richard Friesen , Zhaoyin Wang , Jacques Yves Gauthier
IPC分类号： A61K031/44 , C07D41/04 , C07D213/04
CPC分类号： C07D213/75 , C07D213/34 , C07D213/61 , C07D213/65 , C07D213/80 , C07D213/85 , C07D213/89
摘要： The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. 1 The invention also encompasses certain pharmaceutical compositions for treatment of COX-2 mediated diseases comprising compounds of Formula I.
摘要翻译：本发明包括式I的新化合物以及治疗COX-2介导的疾病的方法，包括向需要这种治疗无需治疗有效量的式I化合物的患者施用本发明还包括用于治疗包含式I化合物的COX-2介导的疾病的某些药物组合物。

4. 发明申请

US20010016595A1 Use of inhibitors of cyclooxygenase in the treatment of neurodegenerative diseases 失效
标题翻译：使用环氧合酶抑制剂治疗神经变性疾病
公开(公告)号：US20010016595A1
公开(公告)日：2001-08-23
申请号：US09796211
申请日：2001-02-28
申请人： Merck Frosst Canada Inc./Merck Frosst Canada & Co.
发明人： Yves Ducharme , Jacques Yves Gauthier , Petpiboon Prasit , Yves Leblanc , Zhaoyin Wang , Serge Leger , Michel Therien
IPC分类号： A61K031/425 , A61K031/38
CPC分类号： C07D275/02 , A61K31/10 , A61K31/341 , A61K31/381 , A61K31/425 , A61K31/426 , C07C311/29 , C07C311/46 , C07C311/49 , C07C317/24 , C07C2601/08 , C07D277/26 , C07D307/38 , C07D307/58 , C07D333/18 , C07D333/38 , C07D405/04
摘要： The present invention provides a method of treating a neurodegenerative disease and in particular Alzheimers disease which comprises administering to a human in need thereof a therapeutically effective amount of a non-steroid COX-II inhibitor. Although a wide range of COX-II inhibitors may be employed but it is preferred to employ compounds of the Formula I: 1
摘要翻译：本发明提供治疗神经变性疾病，特别是阿尔茨海默病的方法，其包括向有需要的人施用治疗有效量的非类固醇COX-II抑制剂。尽管可以使用大范围的COX-II抑制剂，但优选使用式I的化合物：

5. 发明授权

US6114132A Prosphatase binding assay 失效
标题翻译： Prosphatase结合测定
公开(公告)号：US6114132A
公开(公告)日：2000-09-05
申请号：US964313
申请日：1997-11-04
申请人： Sylvie Desmarais , Michael Gresser , Richard Friesen , Brian Kennedy , Don Nicholson , Kathryn Skorey , Chidambaran Ramachandran , Anthony Ford-Hutchinson
发明人： Sylvie Desmarais , Michael Gresser , Richard Friesen , Brian Kennedy , Don Nicholson , Kathryn Skorey , Chidambaran Ramachandran , Anthony Ford-Hutchinson
IPC分类号： G01N33/573 , C07K5/08 , C07K5/083 , C07K5/087 , C07K5/09 , C07K5/093 , C07K5/097 , C12N11/00 , C12N15/09 , C12Q1/34 , C12Q1/37 , C12Q1/42 , C12Q1/48 , C12N9/96
CPC分类号： G01N33/573 , C07K5/0827 , C12Q1/34 , C12Q1/37 , C12Q1/42 , G01N2333/96466
摘要： Disclosed is a binding assay for proteases and phosphatases, which contain cysteine in their binding sites or as a necessary structural component for enzymatic binding. The sulfhydryl group of cysteine is the nucleophilic group in the enzyme's mechanistic proteolytic and hydrolytic properties. The assay can be used to determine the ability of new, unknown ligands and mixtures of compounds to competitively bind with the enzyme versus a known binding agent for the enzyme, e.g., a known enzyme inhibitor. By the use of a mutant form of the natural or native wild-type enzyme, in which serine, or another amino acid, e.g., alanine, replaces cysteine, the problem of interference from extraneous oxidizing and alkylating agents in the assay procedure is overcome. The interference arises because of oxidation or alkylation of the sulfhydryl, --SH (or --S.sup.-), in the cysteine, which then adversely affects the binding ability of the enzyme. Specifically disclosed is an assay for tyrosine phosphatases and cysteine proteases, including caspases and cathepsins, e.g., Cathepsin K(O2), utilizing scintillation proximity assay (SPA) technology. The assay has important applications in the discovery of compounds for the treatment and study of, for example, diabetes, immunosuppression, cancer, Alzheimer's disease and osteoporosis. The novel feature of the use of a mutant enzyme can be extended to its use in a wide variety of conventional colorimetric, photometric, spectrophotometric, radioimmunoassay and ligand-binding competitive assays.
摘要翻译：公开了蛋白酶和磷酸酶的结合测定法，其在其结合位点含有半胱氨酸或作为酶结合的必需结构组分。半胱氨酸的巯基是酶的机理蛋白水解和水解性质中的亲核基团。该测定法可用于测定新的未知配体和化合物的混合物与酶竞争性结合的能力，与酶的已知结合剂，例如已知的酶抑制剂。通过使用天然或天然野生型酶的突变形式，其中丝氨酸或另一氨基酸例如丙氨酸取代半胱氨酸，克服了测定程序中来自外来氧化和烷化剂的干扰问题。干扰是由于半胱氨酸中巯基-SH（或-S-）的氧化或烷基化而产生的，其然后不利地影响酶的结合能力。具体公开的是利用闪烁近邻测定（SPA）技术的酪氨酸磷酸酶和半胱氨酸蛋白酶的测定法，包括胱天蛋白酶和组织蛋白酶，例如组织蛋白酶K（O 2）。该测定在发现用于治疗和研究例如糖尿病，免疫抑制，癌症，阿尔茨海默氏病和骨质疏松症的化合物中具有重要应用。使用突变酶的新颖特征可以扩展到其在各种常规比色，光度，分光光度，放射免疫测定和配体结合竞争性测定中的用途。

6. 发明授权

US5958723A DNA encoding prostaglandin receptor DP 失效
标题翻译：编码前列腺素受体DP的DNA
公开(公告)号：US5958723A
公开(公告)日：1999-09-28
申请号：US812203
申请日：1997-03-06
申请人： Mark Abramovitz , Yves Boie , Kathleen Metters , Nicole Sawyer , Deborah M. Slipetz
发明人： Mark Abramovitz , Yves Boie , Kathleen Metters , Nicole Sawyer , Deborah M. Slipetz
IPC分类号： G01N33/15 , A61K38/00 , C07K14/72 , C07K16/28 , C12N5/10 , C12N15/09 , C12N15/12 , C12P21/02 , C12P21/04 , C12Q1/02 , C12R1/91 , C07K14/705
CPC分类号： C07K14/72 , A61K38/00 , C12N2799/026
摘要： A novel human DP prostaglandin receptor has been identified and DNA encoding the receptor has been isolated, purified, sequenced and expressed in host cells. This DNA encoding the novel prostaglandin receptor and host cells expressing the receptor are used to identify modulators of the prostaglandin receptor.
摘要翻译：已经鉴定了新的人DP前列腺素受体，并且已经分离，纯化，测序并在宿主细胞中表达编码受体的DNA。编码新型前列腺素受体的DNA和表达受体的宿主细胞用于鉴定前列腺素受体的调节剂。

7. 发明授权

US07365196B2 Sulphonamido-substituted bridged bicycloalkyl derivatives 有权
标题翻译：磺酰氨基取代的桥连双环烷基衍生物
公开(公告)号：US07365196B2
公开(公告)日：2008-04-29
申请号：US10239233
申请日：2001-03-15
申请人： Patrice Charles Belanger , Ian James Collins , Joanne Claire Hannam , Timothy Harrison , Stephen John Lewis , Andrew Madin , Edward Giles McIver , Alan John Nadin , Joseph George Neduvelil , Mark Steven Shearman , Adrian Leonard Smith , Timothy Jason Sparey , Graeme Irvine Stevenson , Martin Richard Teall
发明人： Patrice Charles Belanger , Ian James Collins , Joanne Claire Hannam , Timothy Harrison , Stephen John Lewis , Andrew Madin , Edward Giles McIver , Alan John Nadin , Joseph George Neduvelil , Mark Steven Shearman , Adrian Leonard Smith , Timothy Jason Sparey , Graeme Irvine Stevenson , Martin Richard Teall
IPC分类号： C07D413/14 , C07D413/12 , C07D213/71 , C07D213/52 , C07D333/34 , C07D409/14 , C07D409/12 , C07D249/12 , C07D233/84 , C07D207/48 , C07D277/16 , C07D307/64 , A61P25/28
CPC分类号： C07D213/30 , A61K31/18 , A61K31/40 , C07C311/07 , C07C311/09 , C07C311/11 , C07C311/14 , C07C311/20 , C07C311/24 , C07C323/67 , C07C2601/08 , C07C2601/14 , C07C2602/44 , C07C2602/46 , C07C2603/72 , C07C2603/78 , C07D207/36 , C07D211/14 , C07D211/18 , C07D213/71 , C07D213/81 , C07D215/12 , C07D223/32 , C07D231/12 , C07D233/56 , C07D249/08 , C07D271/107 , C07D277/36 , C07D285/14 , C07D285/16 , C07D295/088 , C07D295/135 , C07D295/26 , C07D307/64 , C07D307/81 , C07D319/18 , C07D333/34 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D487/04 , C07D487/08 , C07D491/08 , C07D491/10 , C07D513/10
摘要： A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.
摘要翻译：公开了一类化合物，其包含磺酰氨基取代的桥连双环烷基结构。这些化合物是γ-分泌酶的抑制剂，因此可用于治疗和/或预防阿尔茨海默氏病。

8. 发明申请

US20050130203A1 Novel GABAB receptor DNA sequences 审中-公开
标题翻译：新型GABAB受体DNA序列
公开(公告)号：US20050130203A1
公开(公告)日：2005-06-16
申请号：US10983198
申请日：2004-11-04
申请人： Qingyun Liu , Terrence McDonald , Timothy Bonnert , Gordon Ng , Lee Kolakowski , Janet Clark , Tom Bonner
发明人： Qingyun Liu , Terrence McDonald , Timothy Bonnert , Gordon Ng , Lee Kolakowski , Janet Clark , Tom Bonner
IPC分类号： G01N33/53 , C07K14/705 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N15/09 , C12P21/02 , G01N33/566 , C12Q1/68 , C07H21/04
CPC分类号： C07K14/70571 , C07K2319/00
摘要： DNA encoding a novel human GABAB receptor subunit, HG20, as well as the protein encoded by the DNA, is provided. Also provided is DNA encoding a novel murine GABAB receptor subunit, GABABR1a, as well as the protein encoded by the DNA. Heterodimers of HG20 protein and GABABR1a protein that form a functional GABAB receptor are disclosed. Methods of identifying agonists and antagonists of the GABAB receptor are also provided.
摘要翻译：提供编码新型人GABA B受体亚基HG20的DNA以及由DNA编码的蛋白质。还提供了编码新型鼠GABA B受体亚基，GABA B Rαa以及由DNA编码的蛋白质的DNA。公开了形成功能性GABA B受体的HG20蛋白和GABA BIA1a蛋白的异源二聚体。还提供鉴定GABA B受体的激动剂和拮抗剂的方法。

9. 发明申请

US20030032789A1 High level expression of human cyclooxygenase-2 失效
公开(公告)号：US20030032789A1
公开(公告)日：2003-02-13
申请号：US10027961
申请日：2001-10-25
申请人： Merck Frosst Canada & Co.
发明人： Gary P. O'Neill , Joseph A. Mancini
IPC分类号： C07H021/04 , C12N015/00 , C12N009/02 , C12N005/06 , C12P021/02
CPC分类号： C12N9/0083 , C07K2319/00 , C12Q1/26 , C12Y114/99001 , G01N33/5005
摘要： The invention discloses a cDNA consisting of human cyclooxygenase-2 cDNA attached to 3null flanking sequence of human cyclooxygenase-1 methods for increasing the expression of human cyclooxygenase-2 in transformed cells and assays for preferentially and independently measuring cyclogenase-2 in samples.

10. 发明授权

US6110701A DNA encoding precursor of interleukin-1.beta. converting enzyme--related cysteine proteinase II (ICE.sub.rel -II) 失效
标题翻译：编码白细胞介素-1β转换酶相关半胱氨酸蛋白酶II（ICErel-II）的前体的DNA
公开(公告)号：US6110701A
公开(公告)日：2000-08-29
申请号：US225487
申请日：1994-04-08
申请人： Donald W. Nicholson , Ambereen Ali , Neil A. Munday , John P. Vaillancourt
发明人： Donald W. Nicholson , Ambereen Ali , Neil A. Munday , John P. Vaillancourt
IPC分类号： C12N15/09 , A61K38/00 , A61K38/46 , A61K48/00 , A61P3/00 , A61P9/00 , A61P25/00 , A61P25/28 , A61P31/04 , A61P35/00 , A61P43/00 , C07K16/40 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N9/64 , C12N15/57 , C12Q1/37 , C12Q1/68 , C12R1/19 , C12R1/91 , C12N15/00 , C07H21/04 , C12N1/20 , C12N15/63
CPC分类号： C12N9/6475 , A61K38/00
摘要： A complementary DNA (cDNA) encoding full length form of ICE.sub.rel -II is identified, sequenced and isolated. The cDNA is cloned into expression vectors for expression in recombinant hosts. The cDNA is useful to produce recombinant full length ICE.sub.rel -II. The cDNA and the recombinant ICE.sub.rel -II protein derived therefrom are useful in diagnostic kits, laboratory reagents and assays. The cDNA and the recombinant ICE.sub.rel -II protein may be used to identify compounds that affect ICE.sub.rel -II function, inflammation and cell apoptosis. ICE.sub.rel -II function, inflammation and cell apoptosis may also be modulated by ICE.sub.rel -II antisense or gene therapy.
摘要翻译：鉴定，测序和分离编码全长形式的ICErel-II的互补DNA（cDNA）。将cDNA克隆到表达载体中用于在重组宿主中表达。该cDNA可用于产生重组全长ICErel-II。 cDNA及其衍生的重组型ICErel-II蛋白质可用于诊断试剂盒，实验室试剂和测定。 cDNA和重组体ICErel-II蛋白可用于鉴定影响ICErel-II功能，炎症和细胞凋亡的化合物。 ICErel-II功能，炎症和细胞凋亡也可通过ICErel-II反义或基因治疗来调节。

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