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    • 2. 发明专利
      IL250709A Aminopyrimidinyl compounds as jak inhibitors 未知
    • Aminopyrimidinyl compounds as jak inhibitors
    • IL250709A
    • 2019-05-30
    • IL25070917
    • 2017-02-21
    • PFIZER , EDDINE SAIAH , ZHAO KUI WAN , LI XING , JEAN BAPTISTE TELLIEZ , JOHN I TRUJILLO , ANDREW FENSOME , ARIAMALA GOPALSAMY , BRIAN S GERSTENBERGER , IVAN VIKTOROVICH EFREMOV , BETSY PIERCE , LIYING ZHANG
    • EDDINE SAIAH , ZHAO-KUI WAN , LI XING , JEAN-BAPTISTE TELLIEZ , JOHN I TRUJILLO , ANDREW FENSOME , ARIAMALA GOPALSAMY , BRIAN S GERSTENBERGER , IVAN VIKTOROVICH EFREMOV , BETSY PIERCE , LIYING ZHANG
    • A61P9/00 , A61K31/506 , A61P17/00 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/02
    • A compound compound having the structure:or a pharmaceutically acceptable salt thereof, wherein X is N or CR, where R is hydrogen, deuterium, C1-C4 alkyl, C1-C4 alkoxy, C3-C6 cycloalkyl, aryl, heteroaryl, aryl(C1-C6 alkyl), CN, amino, alkylamino, dialkylamino, CF3, or hydroxyl; A is selected from the group consisting of a bond, C═O, —SO2—, —(C═O)NR0—, and —(CRaRb)q—, where R0 is H or C1-C4 alkyl, and Ra and Rb are independently hydrogen, deuterium, C1-C6 alkyl, C3-C6 cycloalkyl, aryl, aryl(C1-C6 alkyl), heteroaryl, (C1-C6 alkyl)heteroaryl, etc.; A′ is selected from the group consisting of a bond, C═O, —SO2—, —(C═O)NR0′, —NR0′(C═O)—, and —(CRa′Rb′)q—, where R0′ is H or C1-C4 alkyl, and Ra′ and Rb′ are independently hydrogen, deuterium, C1-C6 alkyl, C3-C6 cycloalkyl, aryl, aryl(C1-C6 alkyl), heteroaryl, (C1-C6 alkyl)heteroaryl, heteroaryl(C1-C6 alkyl), and heterocyclic(C1-C6 alkyl); Z is —(CH2)h— or a bond, where one or more methylene units are optionally substituted by one or more C1-C3 alkyl, CN, OH, methoxy, or halo, and where said alkyl may be substituted by one or more fluorine atoms; R1 and R1′ are independently selected from the group consisting of hydrogen, deuterium, C1-C4 alkyl, C3-C6 cycloalkyl, aryl, heteroaryl, aryl(C1-C6 alkyl), CN, etc., wherein said alkyl, aryl, cycloalkyl, heterocyclic, or heteroaryl is further optionally substituted with one or more substituents selected from the group consisting of C1-C6 alkyl, halo, CN, C1-C4 alkylamino, C3-C6 cycloalkyl, etc.; R2 is selected from the group consisting of hydrogen, deuterium, C1-C6 alkyl, C3-C6 cycloalkyl, halo, and cyano, where said alkyl may be substituted by one or more fluorine atoms; R3 is selected from the group consisting of hydrogen, deuterium, and amino; R4 is monocyclic or bicyclic aryl or monocyclic or bicyclic heteroaryl wherein said aryl or heteroaryl is optionally substituted with one or more substituents selected from the group consisting of C1-C6 alkyl, heterocycloalkyl, halo, C3-C6 cycloalkyl, etc., where said alkyl, cycloalkyl, alkoxy, or heterocycloalkyl may be substituted by one or more C1-C6 alkyl, halo, CN, OH, alkoxy, amino, —CO2H, —(CO)NH2, —(CO)NH(C1-C6 alkyl), or —(CO)N(C1-C6 alkyl)2, and where said alkyl may be further substituted by one or more fluorine atoms; R5 is independently selected from the group consisting of hydrogen, C1-C6 alkyl, C1-C6 alkoxy, and hydroxyl; h is 1, 2 or 3; j and k are independently 0, 1, 2, or 3; m and n are independently 0, 1 or 2; and, q is 0, 1 or 2. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations with other therapeutic agents.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 3. 发明专利
      IL250709D0 Aminopyrimidinyl compounds as jak inhibitors 未知
    • Aminopyrimidinyl compounds as jak inhibitors
    • IL250709D0
    • 2017-04-30
    • IL25070917
    • 2017-02-21
    • PFIZER , EDDINE SAIAH , ZHAO-KUI WAN , LI XING , JEAN-BAPTISTE TELLIEZ , JOHN I TRUJILLO , ANDREW FENSOME , ARIAMALA GOPALSAMY , BRIAN S GERSTENBERGER , IVAN VIKTOROVICH EFREMOV , BETSY PIERCE , LIYING ZHANG
    • EDDINE SAIAH , ZHAO-KUI WAN , LI XING , JEAN-BAPTISTE TELLIEZ , JOHN I TRUJILLO , ANDREW FENSOME , ARIAMALA GOPALSAMY , BRIAN S GERSTENBERGER , IVAN VIKTOROVICH EFREMOV , BETSY PIERCE , LIYING ZHANG
    • C07D20060101
    • A compound compound having the structure:or a pharmaceutically acceptable salt thereof, wherein X is N or CR, where R is hydrogen, deuterium, C1-C4 alkyl, C1-C4 alkoxy, C3-C6 cycloalkyl, aryl, heteroaryl, aryl(C1-C6 alkyl), CN, amino, alkylamino, dialkylamino, CF3, or hydroxyl; A is selected from the group consisting of a bond, C═O, —SO2—, —(C═O)NR0—, and —(CRaRb)q—, where R0 is H or C1-C4 alkyl, and Ra and Rb are independently hydrogen, deuterium, C1-C6 alkyl, C3-C6 cycloalkyl, aryl, aryl(C1-C6 alkyl), heteroaryl, (C1-C6 alkyl)heteroaryl, etc.; A′ is selected from the group consisting of a bond, C═O, —SO2—, —(C═O)NR0′, —NR0′(C═O)—, and —(CRa′Rb′)q—, where R0′ is H or C1-C4 alkyl, and Ra′ and Rb′ are independently hydrogen, deuterium, C1-C6 alkyl, C3-C6 cycloalkyl, aryl, aryl(C1-C6 alkyl), heteroaryl, (C1-C6 alkyl)heteroaryl, heteroaryl(C1-C6 alkyl), and heterocyclic(C1-C6 alkyl); Z is —(CH2)h— or a bond, where one or more methylene units are optionally substituted by one or more C1-C3 alkyl, CN, OH, methoxy, or halo, and where said alkyl may be substituted by one or more fluorine atoms; R1 and R1′ are independently selected from the group consisting of hydrogen, deuterium, C1-C4 alkyl, C3-C6 cycloalkyl, aryl, heteroaryl, aryl(C1-C6 alkyl), CN, etc., wherein said alkyl, aryl, cycloalkyl, heterocyclic, or heteroaryl is further optionally substituted with one or more substituents selected from the group consisting of C1-C6 alkyl, halo, CN, C1-C4 alkylamino, C3-C6 cycloalkyl, etc.; R2 is selected from the group consisting of hydrogen, deuterium, C1-C6 alkyl, C3-C6 cycloalkyl, halo, and cyano, where said alkyl may be substituted by one or more fluorine atoms; R3 is selected from the group consisting of hydrogen, deuterium, and amino; R4 is monocyclic or bicyclic aryl or monocyclic or bicyclic heteroaryl wherein said aryl or heteroaryl is optionally substituted with one or more substituents selected from the group consisting of C1-C6 alkyl, heterocycloalkyl, halo, C3-C6 cycloalkyl, etc., where said alkyl, cycloalkyl, alkoxy, or heterocycloalkyl may be substituted by one or more C1-C6 alkyl, halo, CN, OH, alkoxy, amino, —CO2H, —(CO)NH2, —(CO)NH(C1-C6 alkyl), or —(CO)N(C1-C6 alkyl)2, and where said alkyl may be further substituted by one or more fluorine atoms; R5 is independently selected from the group consisting of hydrogen, C1-C6 alkyl, C1-C6 alkoxy, and hydroxyl; h is 1, 2 or 3; j and k are independently 0, 1, 2, or 3; m and n are independently 0, 1 or 2; and, q is 0, 1 or 2. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations with other therapeutic agents.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 9. 发明专利
      AR101599A1 COMPUESTOS AMINOPIRIMIDINILO 未知
    • COMPUESTOS AMINOPIRIMIDINILO
    • AR101599A1
    • 2016-12-28
    • ARP150102681
    • 2015-08-20
    • PFIZER
    • LI XING , LIYING ZHANG , JOHN I TRUJILLO , JEAN TELLIEZ , BETSY BAPTISTE - PIERCE , ZHAO WAN , IVAN VIKTOROVICH KUI - EFREMOV , BRIAN S GERSTENBERGER , ARIAMALA GOPALSAMY , ANDREW FENSOME
    • C07D471/08 , A61K31/439 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/00
    • Reivindicación 1: Un compuesto caracterizado porque tiene la estructura de fórmula (1), o una sal farmacéuticamente aceptable del mismo, en donde X es N o CR, donde R es hidrógeno, deuterio, alquilo C₁₋₄, alcoxi C₁₋₄, cicloalquilo C₃₋₆, arilo, heteroarilo, aril(alquilo C₁₋₆), CN, amino, alquilamino, dialquilamino, CF₃, o hidroxilo; A se selecciona del grupo que consiste de un enlace, C=O, -SO₂--, -(C=O)NR⁰--, y --(CRᵃRᵇ)q--, donde R⁰ es H o alquilo C₁₋₄, y Rᵃ y Rᵇ son independientemente hidrógeno, deuterio, alquilo C₁₋₆, cicloalquilo C₃₋₆, arilo, aril(alquilo C₁₋₆), heteroarilo, (alquilo C₁₋₆)heteroarilo, heteroaril(alquilo C₁₋₆), y heterociclil(alquilo C₁₋₆); A se selecciona del grupo que consiste de un enlace, C=O, --SO₂--, --(C=O)NR⁰, --NR⁰(C=O)--, y --(CRᵃRᵇ)q--, donde R⁰ es H o alquilo C₁₋₄, y Rᵃ y Rᵇ son independientemente hidrógeno, deuterio, alquilo C₁₋₆, cicloalquilo C₃₋₆, arilo, aril(alquilo C₁₋₆), heteroarilo, (alquilo C₁₋₆)heteroarilo, heteroaril(alquilo C₁₋₆), y heterociclil(alquilo C₁₋₆); Z es --(CH₂)ₕ-- o un enlace, donde una o más unidades de metileno se sustituyen opcionalmente por uno o más de alquilo C₁₋₃, CN, OH, metoxi, o halo, y donde el alquilo puede sustituirse por uno o más átomos de flúor; R¹ y R¹ se seleccionan independientemente del grupo que consiste de hidrógeno, deuterio, alquilo C₁₋₄, cicloalquilo C₃₋₆, arilo, heteroarilo, aril(alquilo C₁₋₆), CN, amino, alquilamino, dialquilamino, alcoxi, heteroaril(alquilo C₁₋₆), y heterociclil(alquilo C₁₋₆), en donde el alquilo, arilo, cicloalquilo, heterociclilo, o heteroarilo se sustituyen además opcionalmente con uno o más sustituyentes seleccionados del grupo que consiste de alquilo de C₁₋₆, halo, CN, hidroxi, metoxi, amino, alquilamino C₁₋₄, di(alquilo C₁₋₄)amino, CF₃, -SO₂-(alquilo C₁₋₆), y cicloalquilo C₃₋₆; R² se selecciona del grupo que consiste de hidrógeno, deuterio, alquilo C₁₋₆, cicloalquilo C₃₋₆, halo, y ciano, donde el alquilo puede sustituirse por uno o más átomos de flúor; R³ se selecciona del grupo que consiste de hidrógeno, deuterio, y amino; R⁴ es arilo monocíclico o bicíclico o heteroarilo monocíclico o bicíclico en donde el arilo o heteroarilo se sustituyen opcionalmente con uno o más sustituyentes seleccionados del grupo que consiste de alquilo C₁₋₆, heterocicloalquilo, halo, CN, hidroxi, --CO₂H, alcoxi C₁₋₆, amino, --N(alquilo C₁₋₆)(CO)(alquilo C₁₋₆), --NH(CO)(alquilo C₁₋₆), --(CO)NH₂, --(CO)NH(alquilo C₁₋₆), --(CO)N(alquilo C₁₋₆)₂, --(alquilo C₁₋₆)amino, --N(alquilo C₁₋₆)₂, --SO₂-(alquilo C₁₋₆), --(SO)NH₂, y cicloalquilo C₃₋₆, donde el alquilo, cicloalquilo, alcoxi, o heterocicloalquilo pueden sustituirse por uno o más de alquilo de C₁₋₆, halo, CN, OH, alcoxi, amino, --CO₂H, --(CO)NH₂, --(CO)NH(alquilo C₁₋₆), o --(CO)N(alquilo C₁₋₆)₂, y donde el alquilo puede sustituirse adicionalmente por uno o más átomos de flúor; R⁵ se selecciona independientemente del grupo que consiste de hidrógeno, alquilo C₁₋₆, alcoxi C₁₋₆, e hidroxilo; h es 1, 2 ó 3; j y k son independientemente 0, 1, 2, ó 3; m y n son independientemente 0, 1 ó 2; y, q es 0, 1 ó 2.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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