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1. 发明申请

WO2008137027A3 COMPOUNDS AS CRTH2 AND/OR PGD2 RECEPTORS MODULATORS AND THEIR USE FOR TREATING ASTHMA AND ALLERGIC INFLAMMATION 审中-公开
标题翻译：作为CRTH2和/或PGD2受体调节剂的化合物及其用于治疗哮喘和过敏性炎症的用途
公开(公告)号：WO2008137027A3
公开(公告)日：2009-01-15
申请号：PCT/US2008005611
申请日：2008-05-01
申请人： AMGEN INC , BROWN MATTHEW , JOHNSON MICHAEL G , LI AN-RONG , LIU JIWEN , LIVELY SARAH E , MEDINA JULIO , SHEN WANG , WANG XUEMEI , WANG YINGCAI
发明人： BROWN MATTHEW , JOHNSON MICHAEL G , LI AN-RONG , LIU JIWEN , LIVELY SARAH E , MEDINA JULIO , SHEN WANG , WANG XUEMEI , WANG YINGCAI
IPC分类号： C07D209/08 , A61P11/06 , A61P17/06 , A61P37/08 , C07D209/34 , C07D209/42 , C07D209/48 , C07D215/227 , C07D215/38 , C07D231/56 , C07D235/08 , C07D277/82 , C07D471/04
CPC分类号： C07D209/08 , C07D209/10 , C07D209/34 , C07D209/42 , C07D209/48 , C07D213/68 , C07D213/76 , C07D215/38 , C07D231/56 , C07D235/08 , C07D235/22 , C07D277/82 , C07D405/12 , C07D471/04
摘要： The present invention is directed to compounds, compositions and methods useful for treating inflammatory and immune-related diseases and conditions. The compounds are modulators of prostaglandin D2 (PGD2) receptors including CRTH2 and DP receptors. The subject compounds are carboxylic acid derivatives of formulae (II) and (III): Formula (II), (III), wherein, X represents a divalent linkage selected from -O-, -S(O)k-., -CRaRb-, -C(O)-, -NR8- and -C(NR9)- Y represents a divalent linkage selected from a single bond, -S(O)kNR10-, -C(O)NR10-, (C1-C4)alkylene, hetero(C2-C4)alkyIene, -N(R11)C(O)NR10- -N(R11)S(O)kNR10-, -N(R11)CO2-, -NR11-, -O- and -S(O)k-. Z represents -CO2R12, -C(O)NR12R13 or heteroaryl. L represents a divalent linkage selected from a single bond, (C1-C6)alkylene, (C2-C6)alkenylene, (C2-C6)alkynylene and (C2-C4)heteroalkylene.
摘要翻译：本发明涉及可用于治疗炎性和免疫相关疾病和病症的化合物，组合物和方法。这些化合物是前列腺素D2（PGD2）受体的调节剂，包括CRTH2和DP受体。本发明化合物是式（II）和（III）的羧酸衍生物：式（II），（III）其中X表示选自-O - ， - S（O）k - ， - CR a R b - ， - C（O） - ， - NR8-和-C（NR9）-Y表示选自单键，-S（O）kNR10 - ， - （O）NR10-，（C1-C4 ）亚烷基，杂（C 2 -C 4）烷基，-N（R 11）C（O）NR 10 -N（R 11）S（O）k NR 10 - ， - （R 11）CO 2 - ， - NR 11 - -S（O）K-。 Z表示-CO 2 R 12，-C（O）NR 12 R 13或杂芳基。 L表示选自单键，（C1-C6）亚烷基，（C2-C6）亚烯基，（C2-C6）亚炔基和（C2-C4）亚杂烷基的二价键。

2. 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).

3. 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.

4. 发明专利

CA2685215C COMPOUNDS AND METHODS USEFUL FOR TREATING ASTHMA AND ALLERGIC INFLAMMATION 未知
公开(公告)号：CA2685215C
公开(公告)日：2014-02-11
申请号：CA2685215
申请日：2008-05-01
申请人： AMGEN INC
发明人： BROWN MATTHEW , JOHNSON MICHAEL G , LI AN-RONG , LIU JIWEN , LIVELY SARAH ELIZABETH , MEDINA JULIO C , SHEN WANG , WANG XUEMEI , WANG YINGCAI
IPC分类号： C07D209/08 , A61K31/404 , A61K31/428 , A61K31/435 , C07D209/30 , C07D215/16 , C07D231/56 , C07D235/08 , C07D239/72 , C07D277/82 , C07D471/04
摘要： The present invention is directed to compounds, compositions and methods useful for treating inflammatory and immune-related diseases and conditions. The compounds are modulators of prostaglandin D2 (PGD2) receptors including CRTH2 and DP receptors. The subject compounds are carboxylic acid derivatives of formulae (II) and (III): Formula (II), (III), wherein, X represents a divalent linkage selected from -O-, -S(O)k-., -CRaRb-, -C(O)-, -NR8- and -C(NR9)- Y represents a divalent linkage selected from a single bond, -S(O)kNR10-, -C(O)NR10-, (C1-C4)alkylene, hetero(C2-C4)alkyIene, -N(R11)C(O)NR10- -N(R11)S(O)kNR10-, -N(R11)CO2-, -NR11-, -O- and -S(O)k-. Z represents -CO2R12, -C(O)NR12R13 or heteroaryl. L represents a divalent linkage selected from a single bond, (C1-C6)alkylene, (C2-C6)alkenylene, (C2-C6)alkynylene and (C2-C4)heteroalkylene.

5. 发明专利

AU2008248201B2 Compounds as CRTH2 and/or PGD2 receptors modulators and their use for treating asthma and allergic inflammation 未知
公开(公告)号：AU2008248201B2
公开(公告)日：2013-10-24
申请号：AU2008248201
申请日：2008-05-01
申请人： AMGEN INC
发明人： JOHNSON MICHAEL G , LIU JIWEN , SHEN WANG , LI AN-RONG , LIVELY SARAH E , WANG YINGCAI , WANG XUEMEI , MEDINA JULIO , BROWN MATTHEW
IPC分类号： C07D209/08 , A61P11/06 , A61P17/06 , A61P37/08 , 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.

6. 发明专利

ES2402987T3 Compuestos como moduladores de receptores de PGD2 y/o CRTH2 y su uso para tratar asma e inflamación alérgica 未知
公开(公告)号：ES2402987T3
公开(公告)日：2013-05-13
申请号：ES08743426
申请日：2008-05-01
申请人： AMGEN INC
发明人： BROWN MATTHEW , JOHNSON MICHAEL G , LI AN-RONG , LIU JIWEN , LIVELY SARAH E , MEDINA JULIO C , SHEN WANG , WANG XUEMEI , WANG YINGCAI
IPC分类号： C07D209/08 , A61P11/06 , A61P17/06 , A61P37/08 , C07D209/34 , C07D209/42 , C07D209/48 , C07D215/227 , C07D215/38 , C07D231/56 , C07D235/08 , C07D277/82 , C07D471/04
摘要： Compuesto que tiene la fórmula II: o una sal o solCompuesto que tiene la fórmula II: o una sal o solvato farmacéuticamente aceptable del mismo, en el vato farmacéuticamente aceptable del mismo, en el queB es un anillo de 5 miembros condensado que conqueB es un anillo de 5 miembros condensado que contiene 0, 1, 2 ó 3 heteroátomos seleccionados de N,tiene 0, 1, 2 ó 3 heteroátomos seleccionados de N, O yS; opcionalmente, B está sustituido con halóge O yS; opcionalmente, B está sustituido con halógeno, alquilo (C1-C3), haloalquilo (C1-C3), cicloalqno, alquilo (C1-C3), haloalquilo (C1-C3), cicloalquilo (C3-C5),cicloalquenilo (C3-C5), aminoalquilo uilo (C3-C5),cicloalquenilo (C3-C5), aminoalquilo (C1-C3), hidroxilo, oxo, -OR', -CONR'R", -N(R")C(O(C1-C3), hidroxilo, oxo, -OR', -CONR'R", -N(R")C(O)R', -CO2R', -CN,arilo o heteroarilo; X es un enla)R', -CO2R', -CN,arilo o heteroarilo; X es un enlace divalente seleccionado de -O-, -S(O)k-, -CRaRb-ce divalente seleccionado de -O-, -S(O)k-, -CRaRb-, -C(O)-, -NR8- y -C(NR9)-; Y es un enlace divalen, -C(O)-, -NR8- y -C(NR9)-; Y es un enlace divalente seleccionado de -SO2NH-, -SO2NMe-, -C(O)NH-, -Nte seleccionado de -SO2NH-, -SO2NMe-, -C(O)NH-, -NH-, -NHCO2- y -NHC(O)-NMe; Z es -CO2R12, -C(O)NR12H-, -NHCO2- y -NHC(O)-NMe; Z es -CO2R12, -C(O)NR12R13 o heteroarilo; L es un enlace divalente seleccR13 o heteroarilo; L es un enlace divalente seleccionado de metileno, etileno, clorometileno, hidroxionado de metileno, etileno, clorometileno, hidroximetileno y metilmetileno; R2 es un anillo de bencimetileno y metilmetileno; R2 es un anillo de benceno que no está sustituido o está sustituido con heno que no está sustituido o está sustituido con halógeno, -OR' o -R', en el que R'es alquilo (C1-C8alógeno, -OR' o -R', en el que R'es alquilo (C1-C8) o haloalquilo (C1-C8); R5 y R6 son independiente) o haloalquilo (C1-C8); R5 y R6 son independientemente hidrógeno, halógeno, alquilo (C1-C8), fluoromente hidrógeno, halógeno, alquilo (C1-C8), fluoroalquilo (C1-C4), heteroalquilo(C2-C8), arilo, hetealquilo (C1-C4), heteroalquilo(C2-C8), arilo, heteroarilo, arilalquilo (C1-C4), -NR'R", -OR', -NO2, roarilo, arilalquilo (C1-C4), -NR'R", -OR', -NO2, -CN, -C(O)R', -CO2R', -C(O)NR'R",alquilen (C1-C4)--CN, -C(O)R', -CO2R', -C(O)NR'R",alquilen (C1-C4)-C(O)NR'R", -S(O)mR', -S(O)kNR'R", -OC(O)OR', -OC(OC(O)NR'R", -S(O)mR', -S(O)kNR'R", -OC(O)OR', -OC(O)R', -OC(O)NR'R",N(R''')C(O)NR'R", -N(R")C(O)R', -)R', -OC(O)NR'R",N(R''')C(O)NR'R", -N(R")C(O)R', -N(R")S(O)kR' o -N(R")C(O)OR'; R8, R10 y R11 son inN(R")S(O)kR' o -N(R")C(O)OR'; R8, R10 y R11 son independientemente hidrógeno, alquilo (C1-C8), fluordependientemente hidrógeno, alquilo (C1-C8), fluoroalquilo (C1-C4), heteroalquilo (C2-C8),arilo, hetoalquilo (C1-C4), heteroalquilo (C2-C8),arilo, heteroarilo, arilalquilo (C1-C4), -C(O)R', -CO2R', -Ceroarilo, arilalquilo (C1-C4), -C(O)R', -CO2R', -C(O)NR'R", -S(O)mR' o -S(O)kNR'R";R9 es hidrógeno, (O)NR'R", -S(O)mR' o -S(O)kNR'R";R9 es hidrógeno, alquilo (C1-C6), heteroalquilo (C2-C6), arilalquilalquilo (C1-C6), heteroalquilo (C2-C6), arilalquilo (C1-C4), -OR' o -NR'R";R12 y R13 son independieno (C1-C4), -OR' o -NR'R";R12 y R13 son independientemente hidrógeno, alquilo (C1-C6), heteroalquilo temente hidrógeno, alquilo (C1-C6), heteroalquilo (C2-C6), arilo, arilalquilo (C1-C4)o heteroarilo; (C2-C6), arilo, arilalquilo (C1-C4)o heteroarilo; cada R14 es independientemente halógeno, alquilo (cada R14 es independientemente halógeno, alquilo (C1-C8), fluoroalquilo (C1-C4), alquenilo (C2-C5), C1-C8), fluoroalquilo (C1-C4), alquenilo (C2-C5), -OR',NR'R", -NO2, -CN, -C(O)R' o arilo; Ra y Rb so-OR',NR'R", -NO2, -CN, -C(O)R' o arilo; Ra y Rb son independientemente hidrógeno, alquilo (C1-C6), hn independientemente hidrógeno, alquilo (C1-C6), heteroalquilo (C2-C6), arilalquilo (C1-C4), -OR' o-eteroalquilo (C2-C6), arilalquilo (C1-C4), -OR' o-NR'R"; cada R', R" y R''' es independientemente hiNR'R"; cada R', R" y R''' es independientemente hidrógeno, alquilo (C1-C6), cicloalquilo (C3-C8), cidrógeno, alquilo (C1-C6), cicloalquilo (C3-C8), cicloalquenilo(C3C8), arilo o arilalquilo (C1-C4); ecloalquenilo(C3C8), arilo o arilalquilo (C1-C4); el subíndice k es 0, 1 ó 2; el subíndice m es 0, 1,l subíndice k es 0, 1 ó 2; el subíndice m es 0, 1, 2 ó 3; y el subíndice n es 0, 1, 2, 3 ó 4. 2 ó 3; y el subíndice n es 0, 1, 2, 3 ó 4.

7. 发明专利

CA2685215A1 COMPOUNDS AND METHODS USEFUL FOR TREATING ASTHMA AND ALLERGIC INFLAMMATION 未知
公开(公告)号：CA2685215A1
公开(公告)日：2008-11-13
申请号：CA2685215
申请日：2008-05-01
申请人： AMGEN INC
发明人： WANG XUEMEI , WANG YINGCAI , LIU JIWEN , SHEN WANG , MEDINA JULIO C , BROWN MATTHEW , LI AN-RONG , LIVELY SARAH ELIZABETH , JOHNSON MICHAEL G
IPC分类号： C07D209/08 , A61P11/06 , A61P17/06 , A61P37/08 , C07D209/34 , C07D209/42 , C07D209/48 , C07D215/227 , C07D215/38 , C07D231/56 , C07D235/08 , C07D277/82 , C07D471/04
摘要： The present invention is directed to compounds, compositions and methods useful for treating inflammatory and immune-related diseases and conditions. The compounds are modulators of prostaglandin D2 (PGD2) receptors including CRTH2 and DP receptors. The subject compounds are carboxylic acid derivativ es of formulae (II) and (III): Formula (II), (III), wherein, X represents a divalent linkage selected from -O-, -S(O)k-., -CRaRb-, -C(O)-, -NR8- and -C( NR9)- Y represents a divalent linkage selected from a single bond, -S(O)kNR1 0-, -C(O)NR10-, (C1-C4)alkylene, hetero(C2-C4)alkyIene, -N(R11)C(O)NR10- -N( R11)S(O)kNR10-, -N(R11)CO2-, -NR11-, -O- and -S(O)k-. Z represents -CO2R12, -C(O)NR12R13 or heteroaryl. L represents a divalent linkage selected from a single bond, (C1-C6)alkylene, (C2-C6)alkenylene, (C2-C6)alkynylene and (C2-C 4)heteroalkylene.

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