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61. 发明专利

MX2009011412A COMPUESTOS MODULADORES DE RECEPTORES DE CRTH2 Y/O PGD2 Y SU USO PARA EL TRATAMIENTO DE ASMA E INFLAMACION ALERGICA. 未知
公开(公告)号：MX2009011412A
公开(公告)日：2009-11-05
申请号：MX2009011412
申请日：2008-05-01
申请人： AMGEN INC
发明人： SHEN WANG , MEDINA JULIO C , LIU JIWEN , WANG YINGCAI , LIVELY SARAH E , JOHNSON MICHAEL G , LI AN-RONG , WANG XUEMEI , BROWN MATTHEW
IPC分类号： A61P11/06 , C07D209/08 , A61P17/06 , A61P37/08 , C07D209/34 , C07D209/42 , C07D209/48 , C07D215/227 , C07D215/38 , C07D231/56 , C07D235/08 , C07D277/82 , C07D471/04
摘要： La presente invención se relaciona con compuestos, composiciones y métodos útiles para el tratamiento de enfermedades y afecciones inflamatorias e inmunes relacionadas. Los compuestos son moduladores de los receptores de prostaglandina D2 (PGD2) que incluyen los receptores de CRTH2 y DP. Los compuestos objetivo son derivados de ácidos carboxílicos de las fórmulas (II) y (III), en donde X representa un enlace divalente seleccionado de -O- -S(O)k-, _CRaRb_ -C(O)-, -NR8- y -C(NR9)-; Y es un enlace divalente seleccionado de un enlace simple, -S(O)kNR10-, -C(O)NR10-, alquileno (C1-C4), heteroalquileno (C2-C4), -N(R11)C(O)NR10-, -N(R11)S(O)kNR10-, -N(R11)CO2-, -NR11-, -O- y -S(O)k-; Z es -CO2R12, -C(O)NR12R13 o heteroarilo; L representa un enlace divalente seleccionado de un enlace simple, alquileno (C1-C6), alquenileno (C2-C6), alquinileno (C2-C6) y heteroalquileno (C2-C4).

62. 发明专利

CA2707789A1 PHENYL ACETIC ACID DERIVATIVES AS INFLAMMATION MODULATORS 未知
公开(公告)号：CA2707789A1
公开(公告)日：2009-07-09
申请号：CA2707789
申请日：2008-12-18
申请人： AMGEN INC
发明人： GRILLO MARK , LI AN-RONG , LIU JIWEN , MEDINA JULIO C , SU YONGLI , WANG YINGCAI , JONA JANAN , ALLGEIER ALAN , MILNE JACQUELINE , MURRY JERRY , PAYACK JOSEPH F , STORZ THOMAS
IPC分类号： C07C311/21 , A61K31/192 , A61P17/00 , A61P37/08 , C07C311/29
摘要： Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related diseases and conditions. In particular, the invention provides compounds which modulate the function and/or expression of proteins involved in atopic diseases, inflammatory conditions and cancer. The subject compounds are carboxylic acid derivatives of formula I wherein R1 is alkyl or cycloalkyl; R2 is halo, alky I, haloalkyl, alkoxy, haloalkoxy or cycloalkyl; and X is chloro or fluoro.

63. 发明专利

EA011087B1 СОЕДИНЕНИЯ И ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ ДЛЯ ЛЕЧЕНИЯ ВОСПАЛИТЕЛЬНЫХ ЗАБОЛЕВАНИЙ 未知
公开(公告)号：EA011087B1
公开(公告)日：2008-12-30
申请号：EA200501017
申请日：2003-12-19
申请人： AMGEN INC
发明人： FU ZICE , HUANG XI ALAN , LIU JIWEN , MEDINA JULIO C , SCHMITT MICHAEL J , TANG LUCY H , WANG YINGCAI , XU QINGGE
IPC分类号： A61K31/18 , A61K31/195 , A61K31/277 , A61K31/325 , A61K31/40 , A61K31/44 , C07C205/37 , C07C205/56 , C07C233/75 , C07C271/28 , C07C275/42 , C07C311/08 , C07C311/21 , C07C311/29 , C07D209/22 , C07D209/26 , C07D213/71 , C07D215/36 , C07D233/84 , C07D243/12 , C07D243/24 , C07D257/04 , C07D295/192 , C07D307/91 , C07D333/34 , C07D333/62
摘要： Предложенысоединения, фармацевтическиекомпозициии способы, которыеможноиспользоватьдлялечениявоспалительныхи связанныхс иммунитетомзаболеванийи состояний. Вчастности, внастоящемизобретениипредложенысоединения, которыемодулируютфункциии/илиэкспрессиюбелков, вовлеченныхв атопическиезаболевания, воспалительныесостоянияи раковыезаболевания. Предметомизобретенияявляютсясоединения - производныекарбоновойкислоты.

64. 发明专利

EA011010B1 СОЕДИНЕНИЯ, МОДУЛИРУЮЩИЕ РЕЦЕПТОР GPR40, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СПОСОБ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЙ, ЧУВСТВИТЕЛЬНЫХ К МОДУЛИРОВАНИЮ РЕЦЕПТОРА GPR40 (ВАРИАНТЫ), СПОСОБ МОДУЛИРОВАНИЯ ФУНКЦИИ GPR40 (ВАРИАНТЫ) И СПОСОБ МОДУЛИРОВАНИЯ ЦИРКУЛИРУЮЩЕЙ КОНЦЕНТРАЦИИ ИНСУЛИНА 未知
公开(公告)号：EA011010B1
公开(公告)日：2008-12-30
申请号：EA200601388
申请日：2005-02-24
申请人： AMGEN INC
发明人： AKERMAN MICHELLE , HOUZE JONATHAN , LIN DANIEL C H , LIU JIWEN , LUO JIAN , MEDINA JULIO C , QIU WEI , REAGAN JEFFREY D , SCHMITT MICHAEL J , WANG YINGCAI , SHARMA RAJIV , SHUTTLEWORTH STEPHEN J , SUN YING , ZHANG JIAN , ZHU LIUSHENG , MA ZHIHUA , LIU JINQIAN
IPC分类号： C07C53/132 , A61K31/19 , A61K31/215 , A61K31/42 , A61P5/48 , C07C213/00 , C07C277/00 , C07D277/24 , C07D277/30
摘要： Внастоящемизобретениипредставленысоединения, используемые, например, длямодулированияуровнейинсулинау субъектаи охватываемыеобщейформулой I, вкоторойзначениягрупп Q, L, P, R, R, LиА раскрытыв описании. Внастоящемизобретениипредставленытакжефармацевтическаякомпозицияи способыприменениясоединений, например, длялечениядиабетатипа II.

65. 发明专利

AU2008248201A1 Compounds as CRTH2 and/or PGD2 receptors modulators and their use for treating asthma and allergic inflammation 未知
公开(公告)号：AU2008248201A1
公开(公告)日：2008-11-13
申请号：AU2008248201
申请日：2008-05-01
申请人： AMGEN INC
发明人： MEDINA JULIO , WANG YINGCAI , LI AN-RONG , JOHNSON MICHAEL G , WANG XUEMEI , SHEN WANG , LIU JIWEN , LIVELY SARAH E , BROWN MATTHEW
IPC分类号： A61P11/06 , A61P17/06 , A61P37/08 , C07D209/08 , C07D209/34 , C07D209/42 , C07D209/48 , C07D215/227 , C07D215/38 , C07D231/56 , C07D235/08 , C07D277/82 , C07D471/04
摘要： Compounds, compositions and methods that are useful in the treatment of inflammatory and immune-related diseases and conditions are provided herein. In particular, the invention provides compounds which modulate the function and/or expression of proteins involved in atopic diseases, inflammatory conditions and cancer. The subject compounds are carboxylic acid derivatives.

66. 发明专利

MX2008011615A DERIVADOS DE ACIDOS CARBOXILICOS BICICLICOS UTILES PARA TRATAR TRASTORNOS METABOLICOS. 未知
公开(公告)号：MX2008011615A
公开(公告)日：2008-09-22
申请号：MX2008011615
申请日：2007-03-12
申请人： AMGEN INC
发明人： SHARMA RAJIV , MEDINA JULIO C , LIU JIWEN , SCHMITT MICHAEL J , CARDOZO MARIO G , AKERMAN MICHELLE , WANG YINGCAI , ZHU LIUSHENG , LIU JINQIAN , MA ZHIHUA , LI AN-RONG , HOUZE JONATHAN B , SUN YING , WANG ZHONGYU
IPC分类号： C07D209/08 , A61K31/426 , A61P3/10 , C07C59/54 , C07C59/72 , C07D209/46 , C07D215/22 , C07D277/24 , C07D311/74 , C07D313/08 , C07D417/12 , C07D498/04
摘要： Compuestos que tienen la fórmula general I y/o la fórmula general II son útiles, por ejemplo, para tratar trastornos metabólicos en un sujeto, fórmula (I), (II) donde las variables se proporcionan en la presente. Se describen composiciones y métodos para usar los compuestos para preparar medicamentos y para tratar trastornos metabólicos tal como por ejemplo, diabetes tipo II.

67. 发明专利

NZ541234A Asthma and allergic inflammation modulators 未知
公开(公告)号：NZ541234A
公开(公告)日：2008-06-30
申请号：NZ54123403
申请日：2003-12-19
申请人： AMGEN INC
发明人： FU ZICE , HUANG XI ALAN , LIU JIWEN , MEDINA JULIO C , SCHMITT MICHAEL J , TANG LUCY H , WANG YINGCAI , XU QINGGE
IPC分类号： A61K31/18 , A61K31/195 , A61K31/277 , A61K31/325 , A61K31/40 , A61K31/44 , C07C205/37 , C07C205/56 , C07C233/75 , C07C271/28 , C07C275/42 , C07C311/08 , C07C311/21 , C07C311/29 , C07D209/22 , C07D209/26 , C07D213/71 , C07D215/36 , C07D233/84 , C07D243/12 , C07D243/24 , C07D257/04 , C07D295/192 , C07D307/91 , C07D333/34 , C07D333/62
摘要： Disclosed are carboxylic acid derivative compounds of formula XVI and pharmaceutical compositions containing these compounds which are useful in the treatment of inflammatory and immune-related diseases and conditions. The compounds modulate the function and/or expression of proteins involved in atopic diseases, inflammatory conditions and cancer.

68. 发明专利

CA2662242A1 BENZO-FUSED COMPOUNDS FOR USE IN TREATING METABOLIC DISORDERS 未知
公开(公告)号：CA2662242A1
公开(公告)日：2008-03-13
申请号：CA2662242
申请日：2007-09-06
申请人： AMGEN INC
发明人： DRANSFIELD PAUL JOHN , BROWN SEAN P , HOUZE JONATHAN B , SHARMA RAJIV , LIU JIWEN , LIU JINQIAN , WANG YINGCAI , SCHMITT MICHAEL J , PATTAROPONG VATEE , MA ZHIHUA , MEDINA JULIO C
IPC分类号： C07D213/55 , A61K31/192 , A61K31/40 , C07C59/72 , C07C233/65 , C07D207/327 , C07D231/12 , C07D233/64 , C07D239/26 , C07D249/10 , C07D257/04 , C07D261/08 , C07D263/32 , C07D277/587 , C07D285/12 , C07D333/24
摘要： The present invention provides compounds useful, for example, for treatin g metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables Q, L1, ~, L2, M, X, L3, and A are provided herein. The present invention also provides compositions that inclu de, and methods for using, the compounds in preparing medicaments and for tr eating metabolic disorders such as, for example, type II diabetes.

69. 发明专利

AR057815A1 ACIDOS PROPANOICOS SUSTITUIDOS POR 3-(4-HIDROXI-FENILO) CON RESTRICCIONES CONFORMACIONALES QUE RESULTAN DE UTILIDAD PARA EL TRATAMIENTO DE TRASTORNOS METABOLICOS 未知
公开(公告)号：AR057815A1
公开(公告)日：2007-12-19
申请号：ARP060104016
申请日：2006-09-14
申请人： AMGEN INC
发明人： BROWN SEAN , LIU JINQIAN , SCHMITT MICHAEL J , WANG YINGCAI , HOUZE JONATHAN B , SHARMA RAJIV , ZHU LIUSHENG , MA ZHIHUA , QIU WEI , LIU JIWEN , AKERMAN MICHELLE , MEDINA JULIO C
IPC分类号： C07C59/72 , A61K31/381 , A61P3/10
摘要： Reivindicacion 1: Un compuesto que tiene la formula (1) o uno de sus solvatos, estereoisomeros, profármacos o sales farmacéuticamente aceptables, donde Q es hidrogeno, arilo, heteroarilo, alquilo C1-6 o heteroalquilo C2-6; L1 es un enlace, alquileno C1-4, heteroalquileno C2-4, O, S(O)k, N(Ra), C(O)-heterocicloalquileno C5-7, alquileno C1-4-SO2N(Rb), alquileno C1-4-N(Rb)SO2 o C(O)N(Rb); P representa un anillo ciclohexano o un anillo cicloalcano C5-8 fusionado con benzo; L2 es un enlace, alquileno C1-6, heteroalquileno C2-6, oximetileno, O, S(O)k, N(Ra), C(O)N(Rb), SO2N(Rb), alquileno C1-4-C(O)N(Rb), alquileno C1-4-N(Rb)C(O), alquenileno C2-4-C(O)N(Rb), alquenileno C2-4-N(Rb)C(O), alquileno C1-4-SO2N(Rb), alquileno C1-4-N(Rb)SO2, alquenileno C2-4-SO2N(Rb) o alquenileno C2-4-N(Rb)SO2; M es un anillo aromático, un anillo heteroaromático, cicloalquileno C5-8, arilalquileno C1-4 o heteroarilalquileno C1-4; X es CR1R1', N(R1"), O o S(O)k; L3 es un alquileno C1-5 o es un heteroalquileno C2-5; A es -CO2H, tetrazol-5-ilo, -SO3H, -PO3H2, -SO2NH2, -C(O)NHSO2CH3, -CHO, tiazolidinedionilo, hidroxifenilo o piridilo; Ra es hidrogeno, alquilo C1-6, arilalquilo C1-3 o heteroalquilo C2-6; Rb es hidrogeno, alquilo C1-6 o heteroalquilo C2-6; R1 es ciano, arilo, heteroarilo, alquenilo C2-8, alquenilo C3-8, alquinilo C2-8, alquinilo C3-8 o -C(O)NR2R3; R1' es hidrogeno, ciano, arilo, heteroarilo, alquilo C1-8, alquenilo C2-8 o alquinilo C2-8; R1'' es hidrogeno, arilo, heteroarilo, alquilo C1-8, alquenilo C2-8, alquinilo C2-8 o cicloalquilo C3-8; R2 y R3 se seleccionan, en forma independiente, de hidrogeno, arilo, heteroarilo, alquilo C1-8, heteroalquilo C2-8, cicloalquilo C3-8 o heterocicloalquilo C3-8; de manera optativa, R2 y R3 se combinan para formar un anillo de 4, 5, 6 o 7 miembros que contienen el átomo de nitrogeno al cual está unidos y comprenden de 0 a 2 heteroátomos adicionales que se seleccionan de N, O o S; y el subíndice k es 0, 1 o 2.

70. 发明专利

TNSN06263A1 COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USE IN TREATING METABOLIC DISORDERS 未知
公开(公告)号：TNSN06263A1
公开(公告)日：2007-12-03
申请号：TNSN06263
申请日：2006-08-28
申请人： AMGEN INC
发明人： HOUZE JONATHAN , LIN DANIEL C H , JIWEN LIU , LUO JIAN , MEDINA JULIO C , QIU WEI , REAGAN JEFFREY D , SHARMA RAJIV , SCHMITT MICHAEL J , SHUTTLEWORTH STEPHEN J , SUN YING , WANG YINGCAI , ZHANG JIAN , ZHU LIUSHENG , AKERMAN MICHELLE , LIU JINQIAN , MA ZHIHUA
IPC分类号： A61K31/19 , A61K31/215 , A61K31/42 , C07C53/132 , C07C213/00 , C07C277/00
摘要： The present invention provides compounds useful, for example, for modulating insulin levels in a subject and that have the general formula Q-L1-P-L2-M-X-L3-A wherein the definitions of the variables Q, L1, P, L2, M, X, L3 and A are provided herein. The present invention also provides compositions and methods for use of the compounds, for instance, for treatment of type II diabetes.

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