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1. 发明专利

CA2798634C PYRIDONE AND AZA-PYRIDONE COMPOUNDS AND METHODS OF USE 未知
公开(公告)号：CA2798634C
公开(公告)日：2019-04-16
申请号：CA2798634
申请日：2011-05-06
申请人： GILEAD CONNECTICUT INC , GENENTECH INC
发明人： BARBOSA ANTONIO J M , BLOMGREN PETER A , CURRIE KEVIN S , KRISHNAMOORTHY RAVI , KROPF JEFFREY E , LEE SEUNG H , MITCHELL SCOTT A , ORTWINE DANIEL , SCHMITT AARON C , WANG XIAOJING , XU JIANJUN , YOUNG WENDY , ZHANG HONGLU , ZHAO ZHONGDONG , ZHICHKIN PAVEL E
IPC分类号： C07D487/04 , A61K31/498 , A61K31/501 , A61K31/506 , A61K31/5383 , A61P35/00 , C07D495/04 , C07D519/00
摘要： Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

2. 发明专利

CA3034600C PYRIDONE AND AZA-PYRIDONE COMPOUNDS AND METHODS OF USE 未知
公开(公告)号：CA3034600C
公开(公告)日：2020-11-10
申请号：CA3034600
申请日：2011-05-06
申请人： GENENTECH INC , GILEAD CONNECTICUT INC
发明人： BARBOSA ANTONIO J M , BLOMGREN PETER A , CURRIE KEVIN S , KRISHNAMOORTHY RAVI , KROPF JEFFREY E , LEE SEUNG H , MITCHELL SCOTT A , ORTWINE DANIEL , SCHMITT AARON C , WANG XIAOJING , XU JIANJUN , YOUNG WENDY , ZHANG HONGLU , ZHAO ZHONGDONG , ZHICHKIN PAVEL E
IPC分类号： C07D519/00 , A61K31/33 , A61K31/497 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/5383 , A61K31/551 , C07D487/04 , C07D495/04
摘要： Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. (see formula I)

3. 发明专利

MY160349A PYRIDONE AND AZA-PYRIDONE COMPOUNDS AND METHODS OF USE 未知
公开(公告)号：MY160349A
公开(公告)日：2017-02-28
申请号：MYPI2012004877
申请日：2011-05-06
申请人： GILEAD CONNECTICUT INC , GENENTECH INC
发明人： BARBOSA ANTONIO J M , WANG XIAOJING , XU JIANJUN , YOUNG WENDY , ZHANG HONGLU , ZHAO ZHONGDONG , ZHICHKIN PAVEL E , BLOMGREN PETER A , CURRIE KEVIN S , KRISHNAMOORTHY RAVI , KROOPF JEFFREY E , LEE SEUNG H , MITCHELL SCOTT A , ORTWINE DANIEL , SCHMITT AARON C
IPC分类号： C07D487/04 , A61K31/498 , A61P35/00 , C07D495/04 , C07D498/04
摘要： PYRIDONE AND AZA-PYRIDONE COMPOUNDS OF FORMULA I ARE PROVIDED, INCLUDING STEREOISOMERS, TAUTOMER, AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, USEFUL FOR INHIBITING BTK KINASE, AND FOR TREATING IMMUNE DISORDERS SUCH AS INFLAMMATION MEDIATED BY BTK KINASE. METHODS OF USING COMPOUNDS OF FORMULA I FOR IN VITRO, IN SITU, AND IN VIVO DIAGNOSIS, AND TREATMENT OF SUCH DISORDERS IN MAMMALIAN CELLS, OR ASSOCIATED PATHOLOGICAL CONDITIONS, ARE DISCLOSED.

4. 发明专利

NZ604004A Pyridone and aza-pyridone compounds and methods of use 未知
公开(公告)号：NZ604004A
公开(公告)日：2014-06-27
申请号：NZ60400411
申请日：2011-05-06
申请人： GILEAD CONNECTICUT INC , GENENTECH INC
发明人： BARBOSA ANTONIO J M , BLOMGREN PETER A , CURRIE KEVIN S , KRISHNAMOORTHY RAVI , KROPF JEFFREY E , LEE SEUNG H , MITCHELL SCOTT A , ORTWINE DANIEL , SCHMITT AARON C , WANG XIAOJING , XU JIANJUN , YOUNG WENDY , ZHANG HONGLU , ZHAO ZHONGDONG , ZHICHKIN PAVEL E
IPC分类号： C07D487/04 , A61K31/498 , A61P35/00 , C07D495/04 , C07D498/04
摘要： 604004 Disclosed herein is a compound of formula I, wherein the variables are defined herein, and a pharmaceutical composition comprising said compound, a method of making said pharmaceutical composition and the use in the treatment of immune disorders, cancer, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders, and neurological disorders, and wherein the medicament mediates the Bruton’s tyrosine kinase. Specific embodiments of the compound include the following: 5-[2-(hydroxymethyl)-3-[1-methyl-6-oxo-5-(pyrimidin-4-ylamino)-1,6-dihydropyridin-3-yl ]phenyl] -8-thia-5-azatricyclo[7.4.0.02,7]trideca-1(9),2(7)-dien-6-one; 2-(3-(5-(6,7-dihydro-4H-pyrazolo[5,1-c][1,4]oxazin-2-ylamino)-1-methyl-6-oxo-1,6-dihydropyidin-3-yl)-2-(hydroxymethyl)phenyl)-3,4,6,7,8,9-hexahydropyrazino[1,2-a]indol-1(2H)-one; and 2-(6-fluoro-2-(hydroxymethyl)-3-(1-methyl-5-(5-(4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-ylamino)-6-oxo-1,6-dihydropyridin-3-yl)phenyl)-3,4,6,7,8,9-hexahydropyrazino[1,2-a]indol-1(2H)-one.

6. 发明专利

MA34431B1 COMPOSÉS DE PYRIDONE ET D'AZA-PYRIDONE ET LEURS PROCÉDÉS D'UTILISATION 未知
公开(公告)号：MA34431B1
公开(公告)日：2013-08-01
申请号：MA35435
申请日：2012-12-07
申请人： GILEAD CONNECTICUT INC , GENENTECH INC
发明人： BARBOSA ANTONIO J M , BLOMGREN PETER A , CURRIE KEVIN S , KRISHNAMOORTHY RAVI , KROPF JEFFREY E , LEE SEUNG H , MITCHELL SCOTT A , ORTWINE DANIEL , SCHMITT AARON C , WANG XIAOJING , XU JIANJUN , YOUNG WENDY , ZHANG HONGLU , ZHAO ZHONGDONG , ZHICHKIN PAVEL E
IPC分类号： C07D487/04 , A61K31/498
摘要： LA PRÉSENTE INVENTION CONCERNE DES COMPOSÉS DE PYRIDONE ET D'AZA-PYRIDONE DE FORMULE I, Y COMPRIS LEURS STÉRÉOISOMÈRES, TAUTOMÈRES, ET LEURS SELS PHARMACEUTIQUEMENT ACCEPTABLES, UTILES POUR L'INHIBITION DE LA KINASE BTK, ET POUR LE TRAITEMENT DE TROUBLES IMMUNS TELS QUE L'INFLAMMATION MÉDIÉE PAR LA KINASE BTK. L'INVENTION CONCERNE ÉGALEMENT DES PROCÉDÉS D'UTILISATION DE COMPOSÉS DE FORMULE I POUR LE DIAGNOSTIC IN VITRO, IN SITU, ET IN VIVO, ET LE TRAITEMENT DE TELS TROUBLES DANS DES CELLULES MAMMALIENNES, OU DES CONDITIONS PATHOLOGIQUES ASSOCIÉES.

7. 发明专利

SG185462A1 PYRIDONE AND AZA-PYRIDONE COMPOUNDS AND METHODS OF USE 未知
公开(公告)号：SG185462A1
公开(公告)日：2012-12-28
申请号：SG2012082178
申请日：2011-05-06
申请人： GILEAD CONNECTICUT INC , GENENTECH INC
发明人： BARBOSA ANTONIO J M , BLOMGREN PETER A , CURRIE KEVIN S , KRISHNAMOORTHY RAVI , KROPF JEFFREY E , LEE SEUNG H , MITCHELL SCOTT A , ORTWINE DANIEL , SCHMITT AARON C , WANG XIAOJING , XU JIANJUN , YOUNG WENDY , ZHANG HONGLU , ZHAO ZHONGDONG , ZHICHKIN PAVEL E
摘要： Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

9. 发明专利

ES2573716T3 Compuestos de piridona y aza-piridona y métodos de utilización 未知
公开(公告)号：ES2573716T3
公开(公告)日：2016-06-09
申请号：ES11731170
申请日：2011-05-06
申请人： GILEAD CONNECTICUT INC , GENENTECH INC
发明人： BARBOSA ANTONIO J M , BLOMGREN PETER A , CURRIE KEVIN S , KRISHNAMOORTHY RAVI , KROPF JEFFREY E , LEE SEUNG H , MITCHELL SCOTT A , ORTWINE DANIEL , SCHMITT AARON C , WANG XIAOJING , XU JIANJUN , YOUNG WENDY , ZHANG HONGLU , ZHAO ZHONGDONG , ZHICHKIN PAVEL E
IPC分类号： C07D487/04 , A61K31/498 , A61P35/00 , C07D495/04 , C07D498/04
摘要： Compuesto seleccionado de la fórmula I:**Fórmula** o estereoisómeros, tautómeros o sales farmacéuticamente aceptables del mismo, en el que: R1 es H, D, F, Cl, CN, -NH2, -NHCH3, -N(CH3)2, -OH, -OCH3, -OCH2CH3, -OCH2CH2OH, heteroarilo seleccionado de imidazolilo y pirazolilo, heterociclilo seleccionado de oxetanilo y azetidinilo, y alquilo de C1-C3; R2, R3 y R4 se seleccionan independientemente de H, D, F, Cl, -NH2, -NHCH3, -N(CH3)2, -OH, -OCH3, -OCH2CH3, -OCH2CH2OH, y alquilo de C1-C3; R5 es arilo de C6-C20 opcionalmente sustituido, carbociclilo de C3-C12, heterociclilo de C2-C20, heteroarilo de C1- C20, -(arilo de C6-C20)-(heterociclilo de C2-C20), -(heteroarilo de C1-C20)-(heterociclilo de C2-C20), -(heteroarilo de C1-C20)-(alquilo de C1-C6), o -(heteroarilo de C1-C20)-C(>=O)-(heterociclilo de C2-C20); R6 es H, F, -NH2, -OH, o alquilo de C1-C3 opcionalmente sustituido; X es S, S(>=O), S(>=O)2, N, NR6, O, o CR7; R7 se selecciona independientemente de entre H, D, F, Cl, -CH3, -CH2CH3, -CN, -CH2F, -CHF2, -CF3, -NH2, -OH, y -OCH3; Y1 e Y2 se seleccionan independientemente de CR6 y N; Z1, Z2, Z3, y Z4 se seleccionan independientemente de C, CR7, y N; Z5 se seleccionado de -C(R3)2-, -C(>=O)-, -N(R6)-, -C(R3)2C(R3)2-, -C(R3)2C(>=O)-, -CR3>=CR3-, -CR3>=N- , -N(R6)C(R3)2-, -N(R6)C(R3)2C(R3)2-, y -OC(R3)2C(R3)2-; uno de Z1 y Z2, o X y Z1, en el que X no es S, S(>=O), o S(>=O)2, forma un anillo arilo, carbociclilo, heterociclilo o heteroarilo de cinco, seis o siete miembros; en el que alquilo, carbociclilo, heterociclilo, arilo, y heteroarilo están opcionalmente sustituidos con uno o más grupos seleccionados independientemente de D, F, Cl, Br, I, -CH3, -CH2CH3, -CH2CH(CH3)2, - CH2OH, -CH2CH2OH, -C(CH3)2OH, -CH(OH)CH(CH3)2, -C(CH3)2CH2OH, -CH2CH2SO2CH3, -CH2OP(O)(OH)2, - CN, -CH2F, -CHF2, -CF3, -CO2H, -COCH3, -CO2CH3, -CO2C(CH3)3, -COCH(OH)CH3, -CONH2, - CONHCH3, -CON(CH3)2, -C(CH3)2CONH2, -NO2, -NH2, -NHCH3, -N(CH3)2, -NHCOCH3, -N(CH3)COCH3, - NHS(O)2CH3, -N(CH3)C(CH3)2CONH2, -N(CH3)CH2CH2S(O)2CH3, >=O, -OH, -OCH3, -OCH2CH2N(CH3)2, - OP(O)(OH)2, -S(O)2N(CH3)2, -SCH3, -CH2OCH3, -S(O)2CH3, ciclopropilo, azetidinilo, 1-metilazetidin-3-il)oxi, Nmetil- N-oxetan-3-ilamino, azetidin-1-ilmetilo, oxetanilo, y morfolino; y en el que el grupo:**Fórmula** forma las estructuras: en las que la línea ondulada indica el sitio de unión.

10. 发明专利

AU2011249912A1 Pyridone and aza-pyridone compounds and methods of use 未知
公开(公告)号：AU2011249912A1
公开(公告)日：2012-11-29
申请号：AU2011249912
申请日：2011-05-06
申请人： GENENTECH INC , GILEAD CONNECTICUT INC
发明人： BARBOSA ANTONIO J M , BLOMGREN PETER A , CURRIE KEVIN S , KRISHNAMOORTHY RAVI , KROPF JEFFREY E , LEE SEUNG H , MITCHELL SCOTT A , ORTWINE DANIEL , SCHMITT AARON C , WANG XIAOJING , XU JIANJUN , YOUNG WENDY , ZHANG HONGLU , ZHAO ZHONGDONG , ZHICHKIN PAVEL E
IPC分类号： C07D487/04 , A61K31/498 , A61P35/00 , C07D495/04 , C07D498/04
摘要： Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

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