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1. 发明专利

AU2008302570B2 Compounds and compositions as modulators of GPR119 activity 未知
公开(公告)号：AU2008302570B2
公开(公告)日：2012-05-31
申请号：AU2008302570
申请日：2008-09-03
申请人： IRM LLC
发明人： EPPLE ROBERT , NIKULIN VICTOR , AZIMIOARA MIHAI , COW CHRISTOPHER , MICHELLYS PIERRE-YVES , MUTNICK DANIEL , LELAIS GERALD , ALPER PHILLIP , JIANG SONGCHUN , WESTCOTT-BAKER LUCAS
IPC分类号： C07D401/10 , A61K31/44 , A61K31/496 , A61K31/4965 , A61P3/10 , C07D401/14 , C07D413/06 , C07D413/14 , C07D417/14 , C07D487/04 , C07D491/048
摘要： The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.

2. 发明专利

CA2697551A1 COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY 未知
公开(公告)号：CA2697551A1
公开(公告)日：2009-03-26
申请号：CA2697551
申请日：2008-09-03
申请人： IRM LLC
发明人： ALPER PHILLIP , 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 , A61K31/44 , A61K31/496 , A61K31/4965 , A61P3/10 , C07D401/14 , C07D413/06 , C07D413/14 , C07D417/14 , C07D487/04 , C07D491/048
摘要： The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.

3. 发明专利

AU2008302570A1 Compounds and compositions as modulators of GPR119 activity 未知
公开(公告)号：AU2008302570A1
公开(公告)日：2009-03-26
申请号：AU2008302570
申请日：2008-09-03
申请人： IRM LLC
发明人： EPPLE ROBERT , NIKULIN VICTOR , AZIMIOARA MIHAI , COW CHRISTOPHER , MICHELLYS PIERRE-YVES , MUTNICK DANIEL , LELAIS GERALD , ALPER PHILLIP , JIANG SONGCHUN , WESTCOTT-BAKER LUCAS
IPC分类号： C07D401/10 , A61K31/44 , A61K31/496 , A61K31/4965 , A61P3/10 , C07D401/14 , C07D413/06 , C07D413/14 , C07D417/14 , C07D487/04 , C07D491/048
摘要： The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.

4. 发明申请

WO2008097428A3 COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY 审中-公开
标题翻译：作为GPR119活性调节剂的化合物和组合物
公开(公告)号：WO2008097428A3
公开(公告)日：2008-09-25
申请号：PCT/US2008000864
申请日：2008-01-22
申请人： IRM LLC , ALPER PHILLIP , AZIMIOARA MIHAI , COW CHRISTOPHER , EPPLE ROBERT , JIANG SONGCHUN , LELAIS GERALD , MICHELLYS PIERRE-YVES , NGUYEN TRUC NGOC , WESTCOTT-BAKER LUCAS , WU BAOGEN
发明人： ALPER PHILLIP , AZIMIOARA MIHAI , COW CHRISTOPHER , EPPLE ROBERT , JIANG SONGCHUN , LELAIS GERALD , MICHELLYS PIERRE-YVES , NGUYEN TRUC NGOC , WESTCOTT-BAKER LUCAS , WU BAOGEN
IPC分类号： C07D217/08 , A61K31/4725 , A61P3/04 , A61P3/10 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D409/14 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/10 , C07D487/04 , C07D495/04
CPC分类号： C07D401/12 , C07D217/08 , C07D401/06 , C07D401/10 , C07D401/14 , C07D409/14 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/10 , C07D487/04 , C07D495/04
摘要： The invention provides compounds, pharmaceutical compositions comprising compound of following formula (I), and methods of using such compounds to treat or prevent diseases or disorders associated with theactivity of GPR119 (G protein-coupled receptor 119) such as obesity, diabetes and hyperlipidemia.
摘要翻译：本发明提供化合物，包含下式（I）化合物的药物组合物，以及使用这些化合物治疗或预防与GPR119（G蛋白偶联受体119）的活性相关的疾病或障碍的方法，例如肥胖症，糖尿病和高脂血症。

5. 发明专利

ES2499018T3 Compuestos y composiciones como moduladores de la actividad de GPR119 未知
公开(公告)号：ES2499018T3
公开(公告)日：2014-09-26
申请号：ES08831608
申请日：2008-09-03
申请人： IRM LLC
发明人： ALPER PHILLIP , AZIMIOARA MIHAI , COW CHRISTOPHER , EPPLE ROBERT , JIANG SONGCHUN , LELAIS GERALD , MICHELLYS PIERRE-YVES , MUTNICK DANIEL , NIKULIN VICTOR , WESTCOTT-BAKER LUCAS
IPC分类号： A61K31/44 , C07D401/10 , A61K31/496 , A61K31/4965 , A61P3/10 , C07D401/14 , C07D413/06 , C07D413/14 , C07D417/14 , C07D487/04 , C07D491/048
摘要： Un compuesto de la Fórmula Ia:**Fórmula** en la que: Q es un radical seleccionado entre fenilo, piridinilo, pirazinilo, piridazinilo, pirimidinilo, 1,2,4-oxadiazolilo y tiazolilo; donde dicho fenilo, piridinilo, pirazinilo, piridazinilo, pirimidinilo y tiazolilo de Q está opcionalmente sustituido con hasta 3 radicales seleccionados independientemente entre halo, alquilo C1-6, alcoxi C1-6, alquilo C1-6, -C(O)OR20 y -C(O)R20 halo-sustituidos; donde R20 se selecciona entre hidrógeno y alquilo C1-6; en donde un carbono adyacente a W2 está conectado a través de un CR31 u O con un carbono de Q para formar un anillo de 5 miembros condensado con los anillos A y Q; donde R31 se selecciona entre hidrógeno y alquilo C1-6; W1 y W2 se seleccionan independientemente entre CR21 y N; donde R21 se selecciona entre hidrógeno, ciano, alquilo C1-6, -C(O)OR25, donde R25 se selecciona entre hidrógeno y alquilo C1-6; el anillo A puede tener hasta 2 carbonos del anillo sustituidos con un grupo seleccionado entre -C(O)-, - C(S)- y -C(>=NOR30)- y puede estar parcialmente insaturado con hasta 2 enlaces dobles; donde R30 se selecciona entre hidrógeno y alquilo C1-6; L se selecciona entre alquileno C1-6, alquenileno C2-6, -(CH2)nO-, -NR26(CH2)n-, -OC(O)(CH2)n-, -C(O)O(CH2)n- y -O(CH2)n-; donde R26 se selecciona entre hidrógeno y alquilo C1-6; en donde n se selecciona entre 1, 2, 3, 4 y 5; en donde cualquier alquilo de L puede estar opcionalmente sustituido con 1 a 3 radicales seleccionados independientemente entre halo, alquilo C1-6, alquilo C1-6 halo-sustituido, alcoxi C1-6, alcoxi C1-6 halosustituido, -C(O)R22 y -C(O)OR22; donde R22 se selecciona entre hidrógeno y alquilo C1-6; t1 y t2 se seleccionan cada uno independientemente entre 0, 1 y 2; q se selecciona entre 0, 1, 2, 3 y 4; R1 se selecciona entre -X1S(O)0-2X2R6a, -X1S(O)0-2X2OR6a, -X1S(O)0-2X2C(O)OR6a, - X1S(O)0-2X2OC(O)R6a y -X1S(O)0-2NR6aR6b; donde X1 se selecciona entre un enlace, O, NR7a y alquileno C1-4, donde R7a se selecciona independientemente entre hidrógeno y alquilo C1-6; X2 se selecciona entre un enlace y alquileno C1-4; R6a se selecciona entre hidrógeno, halo, alquilo C1-6, alquenilo C2-6, arilo C6-10, heteroarilo C1-10, heterocicloalquilo C3-8 y cicloalquilo C3-8; en donde dicho arilo, heteroarilo, cicloalquilo y heterocicloalquilo de R6a está opcionalmente sustituido con 1 a 3 radicales seleccionados independientemente entre hidroxi, halo, alquilo C1-6, alquilo C1-6 halo-sustituido, alquilo C1-6 hidroxi-sustituido, alquilo C1-6 ciano-sustituido, alcoxi C1-6, alcoxi C1-6 halo-sustituido y aril C6-10-alcoxi C1-4; y R6b se selecciona entre hidrógeno y alquilo C1-6; R3 se selecciona entre hidrógeno, halo, hidroxi, alquilo C1-6, alquilo C1-6 halo-sustituido, alquilo C1-6 hidroxi-sustituido, alcoxi C1-6, alcoxi C1-6 halosustituido, -C(O)R23 y -C(O)OR23; donde R23 se selecciona entre hidrógeno y alquilo C1-6; R4 se selecciona entre R8 y -C(O)OR8; donde R8 se selecciona entre alquilo C1-6, arilo C6-10, heteroarilo C1-10, cicloalquilo C3-8 y heterocicloalquilo C3-8; en donde dicho arilo, heteroarilo, cicloalquilo o heterocicloalquilo de R8 está opcionalmente sustituido con 1 a 3 radicales seleccionados independientemente entre halo, alquilo C1-6, cicloalquilo C3-8, heterocicloalquilo C3-8, alquilo C1-6 halo-sustituido, alquilo C1-6 hidroxi-sustituido, alcoxi C1-6 y alcoxi C1-6 halosustituido; R5 se selecciona entre hidrógeno, alquilo C1-6, alquilo C1-6 halo-sustituido, alquilo C1-6 hidroxi-sustituido, alcoxi C1-6 y alcoxi C1-6 halosustituido.

6. 发明专利

CA2697551C PIPERIDINE DERIVATIVES AS MODULATORS OF GPR119 ACTIVITY 未知
公开(公告)号：CA2697551C
公开(公告)日：2013-03-12
申请号：CA2697551
申请日：2008-09-03
申请人： IRM LLC
发明人： ALPER PHILLIP , 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 , A61K31/44 , A61K31/496 , A61K31/4965 , A61P3/10 , C07D401/14 , C07D413/06 , C07D413/14 , C07D417/14 , C07D487/04 , C07D491/048
摘要： The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119. Compounds of this invention are of general Formula I as follows. (see formula I)

7. 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.

8. 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

9. 发明专利

ZA201001111B Compounds and compositions as modulators of GPR119 activity 未知
公开(公告)号：ZA201001111B
公开(公告)日：2010-10-27
申请号：ZA201001111
申请日：2010-02-16
申请人： IRM LLC
发明人： ALPER PHILLIP , AZIMIOARA MIHAI , COW CHRISTOPHER , EPPLE ROBERT , JIANG SONGCHUN , LELAIS GERALD , MICHELLYS PIERRE-YVES , MUTNICK DANIEL , NIKULIN VICTOR , WESTCOTT-BAKER LUCAS
IPC分类号： A61K20060101 , A61P20060101 , C07D20060101

10. 发明专利

CR11292A COMPUESTOS Y COMPOSICIONES COMO MODULADORES DE LA ACTIVIDAD DE GPR119 未知
公开(公告)号：CR11292A
公开(公告)日：2010-03-22
申请号：CR11292
申请日：2010-02-23
申请人： IRM LLC
发明人： ALPER PHILLIP , AZIMORA MIHAI , COW CHRISTOPHER , EPPLE ROBERT , JIANG SONGCHUN , LELAIS GERALD , MICHELLYS PIERRE-YVES , MUTNICK DANIEL , NIKULIN VICTOR , WESTCOTT-BAKER LUCAS
IPC分类号： A61K31/44 , A61K31/496 , C07D401/10 , C07D401/14 , C07D413/06 , C07D491/048
摘要： La invencion da a conocer compuestos, composiciones farmaceuticas que comprenden dichos compuestos y metodos para usar dichos compuestos para el tratamiento o prevencion de enfermedades o trastornos asociados con la actividad de GPR119.

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