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51. 发明专利

NZ583495A COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY 未知
公开(公告)号：NZ583495A
公开(公告)日：2011-11-25
申请号：NZ58349508
申请日：2008-09-03
申请人： IRM LLC
发明人： WESTCOTT-BAKER LUCAS , NIKULIN VICTOR , MUTNICK DANIEL , MICHELLYS PIERRE-YVES , LELAIS GERALD , JIANG SONGCHUN , EPPLE ROBERT , COW CHRISTOPHER , AZIMIOARA MIHAI , ALPER PHILLIP
IPC分类号： C07D487/04 , A61K31/44 , A61K31/496 , A61K31/4965 , A61P3/10 , C07D401/10 , C07D401/14 , C07D413/06 , C07D413/14 , C07D417/14 , C07D491/048
摘要： Disclosed is a compound of Formula I e.g. 1-MethylcyclopropyI4-((5-(4-(methylsulfonyl)piperazin-1-yl)pyrazin-2-yloxy)methyl)piperidine-I-carboxylate, or the pharmaceutically acceptable salts thereof; in which: Q is a divalent or trivalent radical selected from aryl and heteroaryl; W1 and W2 are independently selected from CR21 and N; wherein R21 is selected from hydrogen, cyano, alkyl and -C(O)OR25; wherein R25 is selected from hydrogen and alkyl; ring A can have up to 2 ring carbons replaced by a group selected from -C(O)-,C(S)- and -C(=NOR30)- and can be partially unsaturated with up to 2 double bonds; wherein R30 is selected from hydrogen and alkyl; L is selected from alkylene, alkenylene, -OC(O)(CH2)n-, -NR26(CH2)n- and-O(CH2)n-; wherein R26 is selected from hydrogen and alkyl; wherein n is selected from 0, 1,2,3,4 and 5; q is selected from 0 and 1; t1 t2, t3 and t4 are each independently selected from 0, 1 and 2; R1 is selected from-X1S(O)0-2X26a, -X1S(O)0-2X2O6a, -X1S(O)0-2X2C(O)6a, -X1S(O)0-2X2C(O)O6a, -X1S(O)0-2X2OC(O)6a and -X1S(O)0-2NR6aRb, wherein X1 is selected from a bond, O, NR7a and alkylene, wherein R7a is selected from hydrogen and alkyl; X2 is selected from a bond and alkylene; 6a is selected from hydrogen, cyano, halo, alkyl, alkenyl, aryl, heteroaryl, heterocycloalkyl and cycloalkyl and 6b is selected from hydrogen and alkyl; R3 is selected from hydrogen, halo, hydroxyl, alkyl, halo-substituted-alkyl,hydroxy-substituted-alkyl, alkoxy, halo-substituted-alkoxy, -C(O)R23, andC(O)OR23; wherein R23 is selected from hydrogen and alkyl; R4 is selected from R8 and -C(O)OR8; wherein R8 is selected from alkyl, heteroaryl, cycloalkyl and heterocycloalkyl; R8 is selected from hydrogen, hydroxy-substituted-alkyl and alkoxy for treating coronary heart disease, ischemic stroke, restenosis after angioplasty, peripheral vascular disease, intermittent claudication, myocardial infarction, dyslipidemia, post-prandial lipemia, conditions of impaired glucose tolerance, conditions of impaired fasting plasma glucose, metabolic acidosis, ketosis, arthritis, osteoporosis, hypertension, congestive heart failure, left ventricular hypertrophy, peripheral arterial disease, diabetic retinopathy, macular degeneration, cataract, diabetic nephropathy, glomerulosclerosis, chronic renal failure, diabetic neuropathy, metabolic syndrome, syndrome X, premenstrual syndrome, coronary heart disease, angina pectoris, thrombosis, atherosclerosis, myocardial infarction, transient ischemic attacks, stroke, vascular restenosis, hyperglycemia, hyperinsulinemia, hyperlipidemia, hypertrygliceridemia, insulin resistance, impaired glucose metabolism, conditions of impaired glucose tolerance, conditions of impaired fasting plasma glucose, obesity, erectile dysfunction, skin and connective tissue disorders, foot ulcerations and ulcerative colitis, endothelial dysfunction and impaired vascular compliance.

52. 发明专利

SMP200900058B Composti e composizioni come inibitori di proteinachinasi. 未知
公开(公告)号：SMP200900058B
公开(公告)日：2010-11-12
申请号：SM200900058
申请日：2009-07-02
申请人： IRM LLC
发明人： MICHELLYS PIERRE-YVES , PEI WEI , MARSILJE THOMAS H , LU WENSHUO , CHEN BEI , UNO TETSUO , JIN YUNHO , JIANG TAO

53. 发明专利

MX2010011069A COMPUESTOS Y COMPOSICIONES COMO INHIBIDORES DE CINASA. 未知
公开(公告)号：MX2010011069A
公开(公告)日：2010-11-12
申请号：MX2010011069
申请日：2009-04-03
申请人： IRM LLC
发明人： PEI WEI , WU BAOGEN , NGUYEN TRUC NGOC , MICHELLYS PIERRE-YVES , JIANG TAO , ZHU XUEFENG
IPC分类号： C07D471/04 , A61K31/519 , A61K31/53 , A61P31/00 , A61P35/00 , A61P37/00
摘要： La invención se refiere a derivados de triazina y pirimidina que tienen la fórmula (1) o (2): (ver fórmulas) y a métodos para utilizar estos compuestos. Por ejemplo, los compuestos de la invención se pueden utilizar para tratar, mitigar, o prevenir una condición que responda a la inhibición de la actividad de cinasa de linfoma anaplásico (ALK), del oncogén c-ros (ROS), del factor de crecimiento tipo insulina (IGF-1R), y/o del receptor de insulina (lnsR), o de una combinación de los mismos.

54. 发明专利

MX2010009203A COMPUESTOS Y COMPOSICIONES COMO MODULARES DE LA ACTIVIDAD DE GPR119. 未知
公开(公告)号：MX2010009203A
公开(公告)日：2010-11-10
申请号：MX2010009203
申请日：2009-02-20
申请人： IRM LLC
发明人： MUTNICK DANIEL , EPPLE ROBERT , MICHELLYS PIERRE-YVES , ALPER PHILLIP , NIKULIN VICTOR , PETRASSI MICHAEL J
IPC分类号： C07D209/42 , A61K31/343 , A61K31/4439 , A61P3/00 , A61P9/00 , C07D307/85 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12
摘要： La presente invención proporciona compuestos de la fórmula (I): composiciones farmacéuticas que comprenden tales compuestos y métodos para el uso de dichos compuestos en el tratamiento o prevención de enfermedades o trastornos asociados con la actividad de GPR119.

55. 发明专利

SMAP200900058A Composti e composizioni come inibitori di proteinachinasi 未知
公开(公告)号：SMAP200900058A
公开(公告)日：2010-01-19
申请号：SM200900058
申请日：2009-07-02
申请人： IRM LLC
发明人： MICHELLYS PIERRE-YVES , PEI WEI , MARSILJE THOMAS H , LU WENSHUO , CHEN BEI , UNO TETSUO , JIN YUNHO , JIANG TAO

56. 发明专利

AU2009233964A1 Compounds and compositions as protein kinase inhibitors 未知
公开(公告)号：AU2009233964A1
公开(公告)日：2009-10-15
申请号：AU2009233964
申请日：2009-04-03
申请人： IRM LLC , NOVARTIS AG
发明人： LI YUNCHENG , JIANG TAO , PEI WEI , MARSILJE THOMAS H III , MICHELLYS PIERRE-YVES , HUANG CHEN , WU BAOGEN , CHEN BEI , GAO ZHAOBO , GE YONGHUI , NGUYEN TRUC NGOC , ZHU XUEFENG
IPC分类号： C07D239/48 , A61K31/505 , A61K31/506 , A61K31/519 , A61P31/00 , A61P35/00 , A61P37/00 , C07D403/12 , C07D403/14 , C07D487/04
摘要： The invention provides novel pyrimidine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, c-ros oncogene (ROS), insulin-like growth factor (IGF-1R), and/or insulin receptor (InsR) or a combination thereof.

57. 发明专利

AU2009233963A1 Compounds and compositions as kinase inhibitors 未知
公开(公告)号：AU2009233963A1
公开(公告)日：2009-10-15
申请号：AU2009233963
申请日：2009-04-03
申请人： IRM LLC
发明人： NGUYEN TRUC NGOC , PEI WEI , JIANG TAO , ZHU XUEFENG , MICHELLYS PIERRE-YVES , WU BAOGEN
IPC分类号： C07D471/04 , A61K31/519 , A61K31/53 , A61P31/00 , A61P35/00 , A61P37/00
摘要： The invention relates to triazine and pyrimidine derivatives having Formula (1) or (2), and methods for using such compounds. For example, the compounds of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, c-ros oncogene (ROS), insulin-like growth factor (IGF-IR), and/or insulin receptor (InsR) or a combination thereof.

58. 发明专利

NO20092472L 未知
公开(公告)号：NO20092472L
公开(公告)日：2009-09-02
申请号：NO20092472
申请日：2009-06-30
申请人： IRM LLC
发明人： JIANG TAO , MICHELLYS PIERRE-YVES , PEI WEI , MARSILJE THOMAS H , LU WENSHUO , CHEN BEI , UNO TETSUO , JIN YUNHO
IPC分类号： C07D213/74
摘要： The invention provides novel pyrimidine and pyridine derivatives of formula (I) and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 ZAP-70), insulin-like growth factor (IGF- 1R), or a combination thereof.

59. 发明专利

PE20090708A1 COMPUESTOS Y COMPOSICIONES COMO MODULADORES DE LA ACTIVIDAD GPR119 未知
公开(公告)号：PE20090708A1
公开(公告)日：2009-07-15
申请号：PE2008001646
申请日：2008-09-19
申请人： IRM LLC
发明人： ALPER PHILLIP B , AZIMIOARA MIHAI , COW CHRISTOPHER , EPPLE ROBERT , JIANG SONGCHUN , LELAIS GERALD , MICHELLYS PIERRE-YVES , MUTNICK DANIEL , NIKULIN VICTOR , WESTCOTT-BAKER LUCAS
IPC分类号： C07D401/10 , C07D401/14 , C07D413/06 , C07D413/14 , C07D417/14
摘要： REFERIDA A COMPUESTOS DE FORMULA (I) DONDE Q ES RADICAL DIVALENTE O TRIVALENTE DE ARILO C6-C10, CICLOALQLUILO C3-C8, HETEROCICLOALQUILO C3-C8, ENTRE OTROS; W1 Y W2 SON CADA UNO CR21 Y N; R21 ES H, CN, ALQUILO C1-C6, ENTRE OTROS; L ES ALQUILENO C1-C6, -(CH2)nO-, -OC(O)(CH2)n-, ENTRE OTROS; n ES DE 0-5; m Y q SON CADA UNO DE 0-4; t1, t2, t3 y t4 SON CADA UNO DE 0-2; R1 ES DE PREFERENCIA METILSULFONILPIPERAZIN-1-IL; R2 Y R3 SON CADA UNO H, HALO, OH, ALQUILO(C1-C4), ENTRE OTROS; R4 ES R8 O -C(O)OR8; R8 ES ALQUILO C1-C6, ARILO C6-C10, CICLOALQUILO C3-C8, ENTRE OTROS; R5 ES H, ALQUILO C1-C6, ALCOXI(C1-C6), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 1-METILCICLOPROPIL-4-((5-(4-(METILSULFONIL)PIPERAZIN-1-IL)PIRAZIN-2-ILOXI)METIL)PIPERIDIN-1-CARBOXILATO, ISOPROPIL 4-((4-((4-METANOSULFONILPIPERAZIN)-1-IL)FENOXI)METIL)PIPERIDIN-1-CARBOXILATO, ISOPROPIL 4-(2-(4-(4-(METANOSULFONIL)PIPERAZIN-1-IL)FENOXI)ETIL)PIPERIDIN-1-CARBOXILATO, ENTRE OTROS. DICHOS COMPUESTOS SON MODULADORES DE LA ACTIVIDAD DEL GPR119, UTILES EN EL TRATAMIENTO DE LA HIPERLIPIDEMIA, DIABETES TIPO I Y II, DIABETES DE LA GESTACION, DISLIPIDEMIA, ENTRE OTROS

60. 发明专利

PE14472008A1 COMPUESTOS Y COMPOSICIONES COMO INHIBIDORES DE LA PROTEINA CINASA 未知
公开(公告)号：PE14472008A1
公开(公告)日：2008-11-20
申请号：PE0017432007
申请日：2007-12-07
申请人： IRM LLC
发明人： MICHELLYS PIERRE-YVES , PEI WEI , MARSILJE THOMAS H , LU WENSHUO , CHEN BEI , UNO TETSUO , JIN YUNHO , JIANG TAO
IPC分类号： A61K31/505 , C07D213/38 , C07D239/48 , C12N9/99
CPC分类号： A61K31/506 , A61K31/5377 , A61K45/06 , C07D213/74 , C07D239/48 , C07D239/95 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/12 , C07D417/12 , C07D451/02 , C07D453/02 , C07D471/04 , C07D473/16 , C07D487/04 , C07D487/08
摘要： SE REFIERE A UN COMPUESTO DE FORMULA I, DONDE W ES II, A1 Y A4 SON C O N, A2 Y A3 SON C, PERO CUANDO R6 Y R7 FORMAN UN ANILLO UNO DE ELLOS ES N, R7 FORMA UN ANILLO, B Y C SON UN ANILLO CARBOCICLICO DE 5 A 7 MIEMBROS, ARILO, HETEROARILO O ANILLO HETEROCICLICO; Z1, Z2 Y Z3 SON NR11, C=O, CR-OR, (CR2)1-2 O C-R12; R1 Y R2 SON HALO, OR12, NR(R12), SR12 O ALQUILO C1-C6; R3 ES (CR2)0-2SO2R12, (CR2)0-2SO2NRR12, CIANO, ENTRE OTROS; R4, R6, R7 Y R10 SON CADA UNO ALQUILO C1-C6, ALQUENILO C2-C6 O ALQUINILO C2-C6, OR12, ENTRE OTROS; R12 ES UN ANILLO CARBOCICLICO SATURADO O PARCIALMENTE INSATURADO, H O ALQUILO C1-C6; R, R5 Y R5' SON CADA UNO H, ALQUILO C1-C6. SON PREFERIDOS (2-(5-CLORO-2-(2-ISOPROPOXI-5-METIL-4-(1-METILPIPERIDI-4-NIL)FENILAMINO)PIRIMIDI-4-NILAMINO)FENIL)(PIRROLIDI-1-NIL)METANONA, N2-(2-ISOPROPOXI-5-METIL-4-(PIPERIDI-4-NIL)FENIL)-N4-(2-ISOPROPILSULFONIL)FENIL)(5-METILPIRIMIDINA-2,4,6-TRIAMINA, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO DE PREPARACION Y COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA ACTIVIDAD LINFOMA ANAPLASICO CINASA, CINASA ASOCIADA CON CADENA ZETA 70 O FACTOR DE CRECIMIENTO SIMILAR A LA INSULINA

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