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1. 发明申请

WO2004041799A1 5- (SUBSTITUTED PHENYL) -THIADIAZOLIDINE-3-ONES AND THEIR USE AS PTP1B 审中-公开
标题翻译： 5-（取代苯基） - 二苯并唑-3-酮及其作为PTP1B的用途
公开(公告)号：WO2004041799A1
公开(公告)日：2004-05-21
申请号：PCT/GB2003/004721
申请日：2003-11-03
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , BIRCH, Alan, Martin , KENNY, Peter, Wedderburn , MORLEY, Andrew, David , RUSSELL, Daniel, John , TOADER, Dorin
发明人： BIRCH, Alan, Martin , KENNY, Peter, Wedderburn , MORLEY, Andrew, David , RUSSELL, Daniel, John , TOADER, Dorin
IPC分类号： C07D285/10
CPC分类号： C07D285/10 , C07D417/10
摘要： The invention concerns compounds of the formula (I) or pharmaceutically acceptable salts thereof (A chemical formula should be inserted here - please see paper copy enclosed herewith) wherein R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 have any of the meanings defined in the description. Processes for the manufacture of compounds of formula (I), compositions containing them, their use as inhibitors of protein tyrosine phosphatase PTP1B and their use for the treatment of diabetes mellitus are also described.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐（此处应插入化学式 - 请参见随附的纸质文本），其中R1，R2，R3，R4，R5和R6具有定义的任何含义在说明中。还描述了制备式（I）化合物，含有它们的组合物，它们作为蛋白质酪氨酸磷酸酶PTP1B抑制剂的用途及其用于治疗糖尿病的方法。

2. 发明申请

WO0164659A3 INDANE DERIVATIVES AND THEIR USE AS CELL ADHESION INHIBITORS 审中-公开
标题翻译： INDANE衍生物及其作为细胞粘附抑制剂的用途
公开(公告)号：WO0164659A3
公开(公告)日：2001-12-27
申请号：PCT/GB0100844
申请日：2001-02-28
申请人： AVENTIS PHARMA LTD , FENTON GARRY , MCCARTHY CLIVE , MACKENZIE ROBERT EDWARD , MORLEY ANDREW DAVID
发明人： FENTON GARRY , MCCARTHY CLIVE , MACKENZIE ROBERT EDWARD , MORLEY ANDREW DAVID
IPC分类号： A61K31/423 , A61P11/06 , A61P29/00 , C07D235/30 , C07D263/58 , A61K31/4184
CPC分类号： C07D263/58 , C07D235/30
摘要： The invention is directed to physiologically active compounds of general formula (I) wherein: R represents aryl, heteroaryl or a group R -L -Ar -L -; R represents hydrogen or lower alkyl; R represents aryl or heteroaryl; and Ar represents an optionally substituted saturated, partially saturated or fully unsaturated 8 to 10 membered bicyclic ring system containing at least one heteroatom selected from O, S or N; Y is carboxy or an acid bioisostere; and their corresponding N-oxides or prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their corresponding N-oxides or prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4( alpha 4 beta 1).
摘要翻译：本发明涉及通式（I）的生理活性化合物，其中：R 1表示芳基，杂芳基或基团R 3 -L 2 -Ar 1 -L 3 - ; R 2表示氢或低级烷基; R 3表示芳基或杂芳基; 并且Ar 1表示含有至少一个选自O，S或N的杂原子的任选取代的饱和，部分饱和或完全不饱和的8至10元双环体系; Y是羧基或酸性生物电子等排体; 及其相应的N-氧化物或前体药物，以及这些化合物及其相应的N-氧化物或前药的药学上可接受的盐和溶剂合物。这些化合物具有有价值的药物特性，特别是调节VCAM-1和纤连蛋白与整联蛋白VLA-4（α4β1）的相互作用的能力。

3. 发明申请

WO1995004046A1 COMPOUNDS AS PDE IV AND TNF INHIBITORS 审中-公开
标题翻译：作为PDE IV和TNF抑制剂的化合物
公开(公告)号：WO1995004046A1
公开(公告)日：1995-02-09
申请号：PCT/GB1994001631
申请日：1994-07-28
申请人： RHONE-POULENC RORER LIMITED , MORLEY, Andrew, David , PALFREYMAN, Malcolm, Norman , RATCLIFFE, Andrew, James , SHARP, Brian, William
发明人： RHONE-POULENC RORER LIMITED
IPC分类号： C07D213/75
CPC分类号： C07D213/75 , C07D213/89
摘要： This invention is directed to an [(ether or thioether)heteroaryl or aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.
摘要翻译：本发明涉及用于抑制TNF治疗患者的生产或生理作用的[（醚或硫醚）杂芳基或芳基]化合物或其N-氧化物或其药学上可接受的盐与肿瘤坏死因子（TNF）的生理有害过量相关的疾病状态。本发明范围内的化合物还抑制环AMP磷酸二酯酶，并且可用于治疗与通过抑制环AMP磷酸二酯酶调节的病理状况相关的疾病状态，所述疾病状态包括炎性和自身免疫性疾病，特别是IV型环AMP 磷酸二酯酶。因此，本发明涉及其用于抑制TNF和/或环AMP磷酸二酯酶的药理学用途，包含该化合物的药物组合物及其制备方法。

4. 发明申请

WO2003074532A1 HETEROCYCLIC AMIDE DERIVATIVES AS INHIBITORS OF GLYCOGEN PHOSPHORYLASE 审中-公开
标题翻译：作为GLYCOGEN PHOSPHORYLASE的抑制剂的杂环酰胺衍生物
公开(公告)号：WO2003074532A1
公开(公告)日：2003-09-12
申请号：PCT/GB2003/000877
申请日：2003-03-04
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , BIRCH, Alan, Martin , MORLEY, Andrew, David , STOCKER, Andrew , WHITTAMORE, Paul, Robert, Owen
发明人： BIRCH, Alan, Martin , MORLEY, Andrew, David , STOCKER, Andrew , WHITTAMORE, Paul, Robert, Owen
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： Heterocyclic amides of formula (1) wherein: X is N or CH; R 4 and R 5 together are either -S-C(R 6 )=C(R 7 )- or -C(R 7 )=C(R 6 )-S-; R 6 and R 7 are independently selected from, for example hydrogen, halo and C 1-4 alkyl; A is phenylene or heteroarylene; n is 0, 1 or 2; R 1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R 2 is hydrogen, hydroxy or carboxy; R 3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C 1-4 alkyl (optionally substituted by 1 or 2 R 8 groups); R 8 is selected from for example hydroxy, -COCOOR 9 , -C(O)N(R 9 )(R 10 ), -NHC(O)R 9 , (R 9 )(R 10 )N- and -COOR 9 ; R 9 and R 10 are selected from for example hydrogen, hydroxy, C 1-4 alkyl (optionally substituted by 1 or 2 R 13 ); R 13 is selected from hydroxy, halo, trihalomethyl and C 1-4 alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are described.
摘要翻译：式（1）的杂环酰胺其中：X是N或CH; R4和R5一起是-S-C（R6）= C（R7） - 或-C（R7）= C（R6）-S-; R 6和R 7独立地选自例如氢，卤素和C 1-4烷基; A是亚苯基或亚杂芳基; n为0,1或2; R 1选自例如卤素，硝基，氰基，羟基，羧基; R2是氢，羟基或羧基; R3选自例如氢，羟基，芳基，杂环基和C 1-4烷基（任选被1或2个R 8基团取代）; R8选自例如羟基，-COCOOR9，-C（O）N（R9）（R10），-NHC（O）R9，（R9）（R10）N-和-COOR9; R9和R10选自例如氢，羟基，C 1-4烷基（任选被1或2个R 13取代）; R 13选自羟基，卤代，三卤代甲基和C 1-4烷氧基; 或其药学上可接受的盐或前体药物; 具有糖原磷酸化酶抑制活性，因此具有与增加的糖原磷酸化酶活性相关的疾病状态的治疗价值。描述了制备所述杂环酰胺衍生物和含有它们的药物组合物的方法。

5. 发明申请

WO03074513A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO03074513A2
公开(公告)日：2003-09-12
申请号：PCT/GB0300893
申请日：2003-03-04
申请人： ASTRAZENECA AB , ASTRAZENECA UK LTD , BIRCH ALAN MARTIN , MORLEY ANDREW DAVID
发明人： BIRCH ALAN MARTIN , MORLEY ANDREW DAVID
IPC分类号： A61K31/4709 , A61K31/497 , A61K31/501 , A61K31/506 , A61P3/04 , A61P3/10 , A61P7/00 , A61P9/10 , A61P43/00 , C07D401/12 , C07D401/14 , C07D405/14 , C07D417/14 , A61K31/404
CPC分类号： C07D401/12 , C07D401/14 , C07D417/14
摘要： Heterocyclic amides of formula (1) wherein: is a single or double bond; A is phenylene or heteroarylene; m is 0, 1 or 2;n is 0, 1 or 2;R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 is hydrogen, hydroxy or carboxy;R3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C 1-4 alkyl(optionally substituted by 1 or 2 R8 groups);R4 is independently selected from for example hydrogen, halo, nitro, cyano, hydroxy, C 1-4 alkyl, and C 1-4 alkanoyl; R8 is selected from for example hydroxy, -COCOOR9, -C(O)N(R9)(R10), -NHC(O)R9 , (R9)(R10)N- and -COOR9;R9 and R10 are selected from for example hydrogen, hydroxy, C 1-4 alkyl (optionally substituted by 1 or 2 R13 );R13 is selected from hydroxy, halo, trihalomethyl and C 1-4 alkoxy;or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are described.
摘要翻译：式（1）的杂环酰胺其中：是单键或双键; A是亚苯基或亚杂芳基; m为0,1或2; n为0,1或2; R 1选自例如卤素，硝基，氰基，羟基，羧基; R 2是氢，羟基或羧基; R 3选自例如氢，羟基，芳基，杂环基和C 1-4烷基（任选被1或2个R 8基团取代）; R 4独立地选自例如氢，卤素，硝基，氰基，羟基，C 1-4烷基和C 1-4烷酰基; R8选自例如羟基，-COCOOR9，-C（O）N（R9）（R10），-NHC（O）R9，（R9）（R10）N-和-COOR9; R9和R10选自例如氢，羟基，C 1-4烷基（任选被1或2个R 13取代）; R 13选自羟基，卤素，三卤代甲基和C 1-4烷氧基;或其药学上可接受的盐或前体药物; 具有糖原磷酸化酶抑制活性，因此具有与增加的糖原磷酸化酶活性相关的疾病状态的治疗价值。描述了制备所述杂环酰胺衍生物和含有它们的药物组合物的方法。

6. 发明申请

WO03074485A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO03074485A2
公开(公告)日：2003-09-12
申请号：PCT/GB0300936
申请日：2003-03-04
申请人： ASTRAZENECA AB , ASTRAZENECA UK LTD , MORLEY ANDREW DAVID
发明人： MORLEY ANDREW DAVID
IPC分类号： A61K31/404 , A61P3/04 , A61P3/08 , A61P3/10 , A61P5/50 , A61P9/10 , A61P43/00 , C07D209/42
CPC分类号： C07D209/42
摘要： Heterocyclic amides of formula (1) (A chemical formula should be inserted here - please see paper copy enclosed herewith) (1) wherein: R1 is independently selected from, for example, C1-6alkyl, C5-7cycloalkyl, C5-7cycloalkylC1-3alkyl, C 1-6alkoxy, C5-7cycloalkoxy, C5-7cycloalkylC1-3alkoxy, heterocyclyl, heterocyclylC1-3alkyl, heterocyclyloxy or heterocyclylC1-3alkoxy;R2 is phenyl or heteroaryl; R3 is independently selected from hydrogen, halo, nitro, cyano, hydroxy, carboxy, carbamoyl, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, C1-4alkanoyl, fluoromethyl, difluoromethyl, trifluoromethyl and trifluoromethoxy; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are described.
摘要翻译：式（1）的杂环酰胺（在此应插入化学式 - 请参见随附的纸质复合物）（1）其中：R 1独立地选自例如C 1-6烷基，C 5-7环烷基，C 5-7环烷基C 1-3烷基 C 1-6烷氧基，C 5-7环烷氧基，C 5-7环烷基C 1-3烷氧基，杂环基，杂环基C 1-3烷基，杂环基氧基或杂环基C 1-3烷氧基; R 2是苯基或杂芳基; R 3独立地选自氢，卤素，硝基，氰基，羟基，羧基，氨基甲酰基，C 1-4烷基，C 2-4烯基，C 2-4炔基，C 1-4烷氧基，C 1-4烷酰基，氟甲基，二氟甲基，三氟甲基和三氟甲氧基; 或其药学上可接受的盐或前体药物; 具有糖原磷酸化酶抑制活性，因此具有与增加的糖原磷酸化酶活性相关的疾病状态的治疗价值。描述了制备所述杂环酰胺衍生物和含有它们的药物组合物的方法。

7. 发明申请

WO0147922A3 AZAINDOLES 审中-公开
标题翻译：氮杂吲哚
公开(公告)号：WO0147922A3
公开(公告)日：2002-01-17
申请号：PCT/GB0004993
申请日：2000-12-27
申请人： AVENTIS PHARMA LTD , COX PAUL JOSEPH , MAJID TAHIR NADEEM , LAI JUSTINE YEUN QUAI , MORLEY ANDREW DAVID , AMENDOLA SHELLEY , DEPRETS STEPHANIE , EDLIN CHRIS
发明人： COX PAUL JOSEPH , MAJID TAHIR NADEEM , LAI JUSTINE YEUN QUAI , MORLEY ANDREW DAVID , AMENDOLA SHELLEY , DEPRETS STEPHANIE , EDLIN CHRIS
IPC分类号： A61K31/437 , A61K31/4985 , A61K31/5377 , A61P1/04 , A61P3/10 , A61P9/10 , A61P9/14 , A61P11/00 , A61P11/02 , A61P11/06 , A61P17/06 , A61P19/02 , A61P19/06 , A61P25/28 , A61P27/14 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D471/04 , C07D487/04 , C07D519/00
CPC分类号： A61K31/4985 , A61K31/437 , C07D471/04 , C07D487/04
摘要： The invention is directed to compositions containing physiologically active compounds of general formula (I) wherein R is aryl or heteroaryl; R represents hydrogen, acyl, cyano, halo, lower alkenyl or lower alkyl optionally substituted by a substituent selected from cyano, heteroaryl, heterocycloalkyl, -Z R ,-C(=O)-NY Y ,-CO2R ,-NY Y ,-N(R )-C(=O)-R , -N(R )-C(=O)-NY Y ,-N(R )-C(=O)-OR , -N(R )-SO2-R ,-N(R )-SO2-NY Y and one or more halogen atoms; R represents hydrogen, aryl, cyano, halo, heteroaryl, lower alkyl, -C(=O)-OR or -C(=O)-NY Y; and X represents N, CH, C-halo, C-CN, C-R , C-NY Y , C-OH, C-Z R , C-C(=O)-OR , C-C(=O)-NY Y , C-N(R )-C(=O)-R , C-SO2-NY Y , C-N(R )-SO2-R , C-alkenyl, C-alkynyl or C-NO2; and their produgs, and pharmaceutically acceptable salts and solvates of such compounds and their produgs, as well as to novel compounds within the scope of fomula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit protein kinases.
摘要翻译：本发明涉及含有通式（I）的生理活性化合物的组合物，其中R 1是芳基或杂芳基; R 2表示氢，酰基，氰基，卤素，低级烯基或任选被选自氰基，杂芳基，杂环烷基，-Z 1 R 8，-C（= O）-NY （R 6）-C（= O）-R 7，-N（R 6）3，Y 3，）-C（= O）-NY 3 Y 4，-N（R 6）-C（= O）-OR 7，-N（R 6）-SO 2 -R 7，-N（R 6）-SO 2 -NY 3 Y 4和一个或多个卤素原子; R 3表示氢，芳基，氰基，卤素，杂芳基，低级烷基，-C（= O）-OR 5或-C（= O）-NY 3 Y; 并且X 1表示N，CH，C - 卤素，C-CN，CR 7，C-NY 3 Y 4，C-OH，CZ 2 R 7，CC（= O）-OR 5，CC（= O）-NY 3 Y 4，CN（R 8）-C（= O）-R 7，C-SO 2 -YN 3， Y 4，CN（R 8）-SO 2 -R 7，C-烯基，C - 炔基或C-NO 2; 及其制品，以及这些化合物及其制品的药学上可接受的盐和溶剂合物，以及在（I）范围内的新化合物。这些化合物和组合物具有有价值的药物特性，特别是抑制蛋白激酶的能力。

8. 发明申请

WO2004063185A8 THIOPHENE CARBOXAMIDES AS INHIBITORS OF THE ENZYME IKK-2 审中-公开
标题翻译：作为ENKYME IKK-2的抑制剂的THIOPHENE CARBOXAMIDES
公开(公告)号：WO2004063185A8
公开(公告)日：2004-09-23
申请号：PCT/GB2004000106
申请日：2004-01-13
申请人： ASTRAZENECA AB , ASTRAZENECA UK LTD , MORLEY ANDREW DAVID , POYSER JEFFREY PHILIP
发明人： MORLEY ANDREW DAVID , POYSER JEFFREY PHILIP
IPC分类号： A61P29/00 , C07D333/38 , C07D409/12 , A61K31/4436
CPC分类号： C07D409/12 , C07D333/38
摘要： The invention relates to thiophene carboxamides of formula (I) wherein Ar, R1, R2, R3, R4, R5, m and n are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
摘要翻译：本发明涉及式（I）的噻吩甲酰胺，其中Ar，R 1，R 2，R 3，R 4，R 5，m和n如说明书中所定义，其制备中使用的方法和中间体，含有它们的药物组合物及其用途治疗。

9. 发明申请

WO2004063186A1 THIOPHENE-CARBOXAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF THE ENZIME IKK-2 审中-公开
标题翻译：硫代羧酰胺衍生物及其作为ENKIME IKK-2的抑制剂的用途
公开(公告)号：WO2004063186A1
公开(公告)日：2004-07-29
申请号：PCT/GB2004/000096
申请日：2004-01-13
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , FAULL, Alan, Wellington , JOHNSTONE, Craig , MORLEY, Andrew, David , POYSER, Jeffrey, Philip
发明人： FAULL, Alan, Wellington , JOHNSTONE, Craig , MORLEY, Andrew, David , POYSER, Jeffrey, Philip
IPC分类号： C07D333/38
CPC分类号： C07D409/12 , C07D333/38 , C07D333/44 , C07D413/12
摘要： The invention relates to thiophene carboxamides of formula (I), wherein A, R 1 , R 2 , R 3 , R 4 , R 5 and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy .
摘要翻译：本发明涉及式（I）的噻吩甲酰胺，其中A，R 1，R 2，R 3，R 4，R 5和X如说明书中所定义，用于制备的中间体，含有它们的药物组合物及其在治疗中的应用<>。

10. 发明申请

WO2004050646A1 1, 2, 5-THIADIAZOLIDIN-3-ONE 1, 1 DIOXIDE DERIVATIVES AS INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE PTP1B 审中-公开
标题翻译： 1,2,5-噻二唑-3-酮1,1-二氧化物衍生物作为蛋白酪氨酸磷酸酯酶PTP1B的抑制剂
公开(公告)号：WO2004050646A1
公开(公告)日：2004-06-17
申请号：PCT/GB2003/005120
申请日：2003-11-26
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , KENNY, Peter, Wedderburn , MORLEY, Andrew, David , RUSSELL, Daniel, John , TOADER, Dorin
发明人： KENNY, Peter, Wedderburn , MORLEY, Andrew, David , RUSSELL, Daniel, John , TOADER, Dorin
IPC分类号： C07D285/10
CPC分类号： C07D285/10
摘要： The invention concerns compounds of the formula (I) or pharmaceutically acceptable salts thereof wherein R 1 , R 2 , R 3 , R 4 , and R 5 have any of the meanings defined in the description.Processes for the manufacture of compounds of formula (I), compositions containing them, their use as inhibitors of protein tyrosine phosphatase PTP1B and their use for the treatment of diabetes mellitus are also described.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中R1，R2，R3，R4和R5具有本说明书中定义的任何含义。制备式（I）化合物的方法，含它们也被用作蛋白酪氨酸磷酸酶PTP1B的抑制剂及其用于治疗糖尿病的用途。

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