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1. 发明申请

WO1991012242A1 THIOFORMAMIDE DERIVATIVES 审中-公开
标题翻译：酪氨酸衍生物
公开(公告)号：WO1991012242A1
公开(公告)日：1991-08-22
申请号：PCT/EP1991000247
申请日：1991-02-08
申请人： RHONE-POULENC RORER S.A. , HART, Terance, William , VACHER, Bernard, Yvon, Jack
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07D213/59
CPC分类号： C07D213/59 , C07D215/14
摘要： Thioformamide derivatives of formula (I), wherein R represents alkyl; A represents optionally substituted pyrid-4-yl or quinolin-4-yl; Y represents ethylene or methylene or a direct bond and X represents an optionally substituted phenyl, pyridyl, furyl or thienyl group or optionally substituted alkyl, alkenyl or cycloalkyl , and salts thereof possess useful pharmacological properties.
摘要翻译：式（I）的硫代甲酰胺衍生物，其中R表示烷基; A表示任选取代的吡啶-4-基或喹啉-4-基; Y表示亚乙基或亚甲基或直接键，X表示任选取代的苯基，吡啶基，呋喃基或噻吩基或任选取代的烷基，烯基或环烷基及其盐具有有用的药理学性质。

2. 发明申请

WO2008040995A1 INDOLES FOR USE AS DPP-IV INHIBITORS 审中-公开
标题翻译：用作DPP-IV抑制剂的药物
公开(公告)号：WO2008040995A1
公开(公告)日：2008-04-10
申请号：PCT/GB2007003788
申请日：2007-10-04
申请人： PEAKDALE MOLECULAR LTD , MADDAFORD ADRIAN , GLEN REBECCA , LEESE DAVID PAUL , HART TERANCE WILLIAM
发明人： MADDAFORD ADRIAN , GLEN REBECCA , LEESE DAVID PAUL , HART TERANCE WILLIAM
IPC分类号： C07D487/04 , A61K31/416 , A61P3/10 , C07D403/06
CPC分类号： C07D487/04 , C07D403/06
摘要： The present invention relates to indazole derivatives useful as dipeptidyl peptidase IV (DPP-IV) inhibitors.
摘要翻译：本发明涉及可用作二肽基肽酶IV（DPP-IV）抑制剂的吲唑衍生物。

3. 发明申请

WO2007065888A1 CHROMONE DERIVATIVES USEFUL AS ANTAGONISTS OF VR1 RECEPTORS 审中-公开
标题翻译：用作VR1受体拮抗剂的色素衍生物
公开(公告)号：WO2007065888A1
公开(公告)日：2007-06-14
申请号：PCT/EP2006/069303
申请日：2006-12-05
申请人： NOVARTIS AG , NOVARTIS PHARMA GmbH , CULSHAW, Andrew James , BRAIN, Christopher Thomas , DZIADULEWICZ, Edward Karol , EDWARDS, Lee , HART, Terance William , RITCHIE, Timothy John
发明人： CULSHAW, Andrew James , BRAIN, Christopher Thomas , DZIADULEWICZ, Edward Karol , EDWARDS, Lee , HART, Terance William , RITCHIE, Timothy John
IPC分类号： C07D491/04 , C07D498/04 , A61K31/352 , A61P29/00
CPC分类号： C07D491/04
摘要： The invention relates to novel heterocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them. The compounds (I) are antagonists of VRl receptors.
摘要翻译：本发明涉及式（I）的新型杂环化合物，其中所有变量如本说明书中所定义，以游离形式或盐形式，其制备，用作药物和包含它们的药物。化合物（I）是VR1受体的拮抗剂。

4. 发明申请

WO0075107A3 BRADYKININ RECEPTOR ANTAGONISTS 审中-公开
标题翻译： BRADYKININ受体拮抗剂
公开(公告)号：WO0075107A3
公开(公告)日：2001-09-07
申请号：PCT/EP0005059
申请日：2000-06-02
申请人： NOVARTIS AG , NOVARTIS ERFIND VERWALT GMBH , BRAIN CHRISTOPHER THOMAS , CANTRELL WILLIAM , CULSHAW ANDREW JAMES , DZIADULEWICZ EDWARD KAROL , HART TERANCE WILLIAM , RITCHIE TIMOTHY JOHN , WAYKOLE LILADHAR
发明人： BRAIN CHRISTOPHER THOMAS , CANTRELL WILLIAM , CULSHAW ANDREW JAMES , DZIADULEWICZ EDWARD KAROL , HART TERANCE WILLIAM , RITCHIE TIMOTHY JOHN , WAYKOLE LILADHAR
IPC分类号： C07D295/18 , A61K31/4406 , A61K31/4409 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/63 , A61P1/04 , A61P1/18 , A61P7/10 , A61P9/02 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/10 , A61P15/00 , A61P15/06 , A61P17/00 , A61P17/02 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/04 , A61P19/06 , A61P21/00 , A61P21/02 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P27/02 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/08 , A61P41/00 , A61P43/00 , C07C311/44 , C07D211/34 , C07D211/62 , C07D211/82 , C07D213/38 , C07D261/08 , C07D277/28 , C07D295/192 , C07D295/26 , C07D333/20 , C07D401/12
CPC分类号： C07D295/192 , C07D211/34 , C07D211/62 , C07D295/26 , C07D401/12
摘要： Novel sulfonyl amine derivatives, of formula (IA) processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
摘要翻译：式（IA）的新型磺酰胺衍生物的制备方法，它们用作药物和包含它们的药物组合物。

5. 发明申请

WO2008040995A8 INDAZOLES FOR USE AS DPP-IV INHIBITORS 审中-公开
标题翻译：用作DPP-IV抑制剂的药物
公开(公告)号：WO2008040995A8
公开(公告)日：2008-10-23
申请号：PCT/GB2007003788
申请日：2007-10-04
申请人： PEAKDALE MOLECULAR LTD , MADDAFORD ADRIAN , GLEN REBECCA , LEESE DAVID PAUL , HART TERANCE WILLIAM
发明人： MADDAFORD ADRIAN , GLEN REBECCA , LEESE DAVID PAUL , HART TERANCE WILLIAM
IPC分类号： C07D487/04 , A61K31/416 , A61P3/10 , C07D403/06
CPC分类号： C07D487/04 , C07D403/06
摘要： The present invention relates to indazole derivatives useful as dipeptidyl peptidase IV (DPP-IV) inhibitors.
摘要翻译：本发明涉及可用作二肽基肽酶IV（DPP-IV）抑制剂的吲唑衍生物。

6. 发明申请

WO2004033435A1 QUINAZOLINONE DERIVATIVES USEFUL AS ANTI-HYPERALGESIC AGENTS 审中-公开
标题翻译：喹诺酮衍生物作为抗高血压药物有用
公开(公告)号：WO2004033435A1
公开(公告)日：2004-04-22
申请号：PCT/EP2003/011276
申请日：2003-10-10
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , CULSHAW, Andrew, James , DZIADULEWICZ, Edward, Karol , HALLETT, Allan , HART, Terance, William
发明人： CULSHAW, Andrew, James , DZIADULEWICZ, Edward, Karol , HALLETT, Allan , HART, Terance, William
IPC分类号： C07D239/90
CPC分类号： C07D403/14 , C07C229/56 , C07D239/90 , C07D239/95 , C07D405/04 , C07D405/14 , C07D413/04
摘要： The present invention relates to quinazolinones of formula (I) wherein R 1 is hal; a); b); or c); X is N or CR 8 ; R 2 is hal; nitro; C 1 -C 6 alkylcarbonyl; C 1 -C 6 alkyl or C 3 -C 6 cycloalkyl; R 3 is C 1 -C 6 alkyl; C 1 -C 6 alkoxy or amino; and wherein the further radicals have the meanings as defined in the specification, which compounds exhibit human vanilloid antagonistic activity; to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式（I）的喹唑啉酮，其中R 1为卤素; 一个）; 二）; 或c）; X是N或CR 8; R 2为卤素; 硝基; C1-C6alkylcarbonyl; C 1 -C 6烷基或C 3 -C 6环烷基; R 3是C 1 -C 6烷基; C1-C6烷氧基或氨基; 并且其中所述其它基团具有如说明书中所定义的含义，所述化合物表现出人类香草素拮抗活性; 其制备方法，它们作为药物的用途以及包含它们的药物组合物。

7. 发明申请

WO2008040974A1 INDOLES FOR USE AS DPP-IV INHIBITORS 审中-公开
标题翻译：用作DPP-IV抑制剂的药物
公开(公告)号：WO2008040974A1
公开(公告)日：2008-04-10
申请号：PCT/GB2007/003758
申请日：2007-10-04
申请人： PEAKDALE MOLECULAR LIMITED , MADDAFORD, Adrian , GLEN, Rebecca , LEESE, David, Paul , HART, Terance, William
发明人： MADDAFORD, Adrian , GLEN, Rebecca , LEESE, David, Paul , HART, Terance, William
IPC分类号： C07D487/04 , A61K31/4985 , A61P9/00
CPC分类号： C07D487/04 , C07D403/06
摘要： The present invention relates to indole derivatives useful as dipeptidyl peptidase IV (DPP-IV) inhibitors. Formula (I).
摘要翻译：本发明涉及用作二肽基肽酶IV（DPP-IV）抑制剂的吲哚衍生物。式（I）。

8. 发明申请

WO2003066603A1 QUINAZOLINONE DERIVATIVES AND THEIR USE AS CB AGONISTS 审中-公开
标题翻译：喹诺酮衍生物及其作为CB激动剂的用途
公开(公告)号：WO2003066603A1
公开(公告)日：2003-08-14
申请号：PCT/EP2003/001140
申请日：2003-02-05
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BRAIN, Christopher, Thomas , DZIADULEWICZ, Edward, Karol , HART, Terance, William
发明人： BRAIN, Christopher, Thomas , DZIADULEWICZ, Edward, Karol , HART, Terance, William
IPC分类号： C07D239/91
CPC分类号： C07D239/91
摘要： Novel quinazolinone derivatives of formula (I) wherein R 1 -R 9 are as defined in the description, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
摘要翻译：式I的新型喹唑啉酮衍生物，其中R 1 -R 9如说明书中所定义，其制备方法，其作为药物的用途和包含它们的药物组合物。

9. 发明申请

WO2002092556A1 SULFONAMIDE DERIVATIVES 审中-公开
标题翻译：磺酰胺衍生物
公开(公告)号：WO2002092556A1
公开(公告)日：2002-11-21
申请号：PCT/EP2002/005240
申请日：2002-05-13
申请人： NOVARTIS AG , NOVARTIS-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , HART, Terance, William , RITCHIE, Timothy, John
发明人： HART, Terance, William , RITCHIE, Timothy, John
IPC分类号： C07C311/19
CPC分类号： C07C311/19 , C07C311/48 , C07C2602/08 , C07D213/55 , C07D239/26 , C07D257/04
摘要： Sulfonamide derivatives of the formula I wherein R 1 -R 6 are as defined in the description, processes for their production, their use as pharmaceuticals, particularly for use in the treatment or prevention of diseases in which bradykinin B 1 receptor activation plays a role or is implicated, and pharmaceutical compositions comprising them.
摘要翻译：式I的磺酰胺衍生物，其中R 1 -R 6如说明书中所定义，其制备方法，其作为药物的用途，特别是用于治疗或预防缓激肽B1受体活化的疾病作用或牵连，以及包含它们的药物组合物。

10. 发明申请

WO1997042216A1 AUTO-DECONVOLUTING COMBINATORIAL LIBRARIES 审中-公开
标题翻译：自动解除组合图书馆
公开(公告)号：WO1997042216A1
公开(公告)日：1997-11-13
申请号：PCT/GB1997001158
申请日：1997-04-24
申请人： PEPTIDE THERAPEUTICS LIMITED , QUIBELL, Martin , JOHNSON, Tony , HART, Terance
发明人： PEPTIDE THERAPEUTICS LIMITED
IPC分类号： C07K01/04
CPC分类号： C07K7/06 , B01J19/0046 , B01J2219/00315 , B01J2219/00504 , B01J2219/0072 , C07K1/047 , C07K5/06043 , C07K5/06191 , C07K7/02 , C40B60/14 , G01N33/68
摘要： The present invention relates to the field of apparatus and methods which provide the rapid generation of structure/activity relationships using auto-deconvoluting combinatorial libraries, which facilitate the invention of novel active compounds. The invention provides apparatus and methods which can be used for the rapid generation of structure/activity relationship (SAR) data, and, therefore, the characterisation of the active motif of any group of compounds. The invention provides libraries of compounds which interact with an active moiety, and apparatus and methods to identify such compounds. The active moieties may be (but are not limited to) enzymes, receptors, antibodies, etc. The interaction of the active moiety with the compounds of the library may be (but is not limited to) the interaction of a substrate or inhibitor with an enzyme, the interaction of a ligand with a receptor, the interaction of an antigen or antigenic epitope with an antibody, etc.
摘要翻译：本发明涉及使用自动去卷积组合库快速产生结构/活性关系的装置和方法领域，其促进了新型活性化合物的发明。本发明提供了可用于快速产生结构/活性关系（SAR）数据的装置和方法，并因此用于表征任何一组化合物的活性基序。本发明提供了与活性部分相互作用的化合物文库，以及鉴定这些化合物的装置和方法。活性部分可以是（但不限于）酶，受体，抗体等。活性部分与文库化合物的相互作用可以是（但不限于）底物或抑制剂与酶，配体与受体的相互作用，抗原或抗原表位与抗体的相互作用等

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