AR104461A1 - Pirrolo[2,3-d]pirimidinil, pirrolo[2,3-b]pirazinil, pirrolo[2,3-b]piridinil acrilamidas y epóxidos de estas - Google Patents

Pirrolo[2,3-d]pirimidinil, pirrolo[2,3-b]pirazinil, pirrolo[2,3-b]piridinil acrilamidas y epóxidos de estas

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Publication number
AR104461A1
AR104461A1 ARP160101237A ARP160101237A AR104461A1 AR 104461 A1 AR104461 A1 AR 104461A1 AR P160101237 A ARP160101237 A AR P160101237A AR P160101237 A ARP160101237 A AR P160101237A AR 104461 A1 AR104461 A1 AR 104461A1
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AR
Argentina
Prior art keywords
straight
branched chain
chain alkyl
aryl
heteroaryl
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ARP160101237A
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English (en)
Inventor
Xi Liang Sidney
I TRUJILLO John
Jai Unwalla Rayomand
Telliez Jean
Merrill Baptiste - Hayward Matthew
Matthew Gilbert Adam
Edward Flanagan Mark
Che Ye
Casimiro-Garcia Agustin
Frank Brown Matthew
Thorarensen Atli
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Pfizer
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Publication of AR104461A1 publication Critical patent/AR104461A1/es

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    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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Abstract

Reivindicación 1: Un compuesto caracterizado porque tiene la estructura fórmula (1) o una sal o un solvato de aquel aceptables desde el punto de vista farmacéutico, o un enantiómero o un diastereómero de aquel, y en donde R² se selecciona del grupo que consiste en hidrógeno, deuterio, C₁₋₆ alquilo de cadena lineal o ramificada, C₃₋₆ cicloalquilo, C₆₋₁₀ arilo, heteroarilo monocíclico o bicíclico, que comprende anillos de 5 y/o 6 miembros, (aril)C₁₋₆ alquilo de cadena lineal o ramificada, (heteroaril)C₁₋₆ alquilo de cadena lineal o ramificada, (heterociclil)C₁₋₆ alquilo de cadena lineal o ramificada, (C₁₋₆ alquil de cadena lineal o ramificada)arilo, (C₁₋₆ alquil de cadena lineal o ramificada)heteroarilo, (C₁₋₆ alquil de cadena lineal o ramificada)heterociclilo, C₁₋₆ perfluoroalquilo de cadena lineal o ramificada, C₁₋₆ alcoxi de cadena lineal o ramificada, C₁₋₆ perfluoroalcoxi de cadena lineal o ramificada, halógeno, ciano, hidroxilo, amino, carboxi, aminocarbonilo, (C₁₋₆ alquil de cadena lineal o ramificada)aminocarbonilamino, (C₁₋₆ alquil de cadena lineal o ramificada)aminocarbonilo, -SOR¹², -SO₂R¹², -NR¹³SO₂R¹², -SO₂NR¹³R¹⁴ y -NR¹³SO₂NR¹⁴R¹⁵; en donde tal alquilo, arilo y heteroarilo se sustituyen, independientemente y de manera opcional, con uno o más sustituyentes seleccionados del grupo que consiste en halo, hidroxi, metoxi, amino, ciano, alquilamino, dialquilamino, CF₃, aminocarbonilo, (C₁₋₆ alquil de cadena lineal o ramificada)aminocarbonilo y C₃₋₆ cicloalquilo; las líneas punteadas al átomo O pueden estar presentes o ausentes, y si están presentes, el anillo resultante forma un epóxido, o si están ausentes, se obtiene un etileno; R³ se selecciona del grupo que consiste en hidrógeno, deuterio, C₁₋₆ alquilo de cadena lineal o ramificada, C₁₋₆ perfluoroalquilo de cadena lineal o ramificada, halógeno y ciano; R⁰ se selecciona de hidrógeno, C₁₋₆ alquilo de cadena lineal o ramificada y C₁₋₆ perfluoroalquilo de cadena lineal o ramificada; R¹, R⁴, R⁵, R⁴, R⁶, R⁷, R⁸, R⁹ y R¹⁰ se seleccionan independientemente de hidrógeno, C₁₋₆ alquilo de cadena lineal o ramificada, C₁₋₆ perfluoroalquilo de cadena lineal o ramificada, C₆₋₁₀ arilo, heteroarilo monocíclico o bicíclico, que comprende anillos de 5 y/o 6 miembros, (aril)C₁₋₆ alquilo de cadena lineal o ramificada, (heteroaril)C₁₋₆ alquilo de cadena lineal o ramificada, heteroarilo, halógeno, ciano, hidroxilo, C₁₋₆ alcoxi de cadena lineal o ramificada, amino, carboxi, aminocarbonilo, (heterociclil)C₁₋₆ alquilo de cadena lineal o ramificada, (C₁₋₆ alquil de cadena lineal o ramificada)arilo, (C₁₋₆ alquil de cadena lineal o ramificada)heteroarilo y (C₁₋₆ alquil de cadena lineal o ramificada)heterociclilo, en donde tal alquilo también se sustituye opcionalmente con uno o más sustituyentes seleccionados del grupo que consiste en halo, hidroxi, metoxi, amino, alquilamino, dialquilamino, CF₃ y C₃₋₆ cicloalquilo; en donde R⁸ y R⁹ juntos pueden formar un anillo de 3 - 6 miembros que contiene opcionalmente uno o dos átomos de O ó N; R¹¹ es hidrógeno o deuterio; R¹², R¹³, R¹⁴ y R¹⁵ se seleccionan independientemente de hidrógeno, C₁₋₆ alquilo de cadena lineal o ramificada, C₁₋₆ perfluoroalquilo de cadena lineal o ramificada, C₆₋₁₀ arilo, alquilarilo y (aril)C₁₋₆ alquilo de cadena lineal o ramificada; Y es O ó N, en donde cuando Y es N, el enlace punteado es un enlace simple, o N se sustituye con H o alquilo, y el enlace punteado a este está ausente, y cuando Y es O, el enlace punteado a este está ausente; y n y p son independientemente 0, 1 ó 2.
ARP160101237A 2015-05-01 2016-04-29 Pirrolo[2,3-d]pirimidinil, pirrolo[2,3-b]pirazinil, pirrolo[2,3-b]piridinil acrilamidas y epóxidos de estas AR104461A1 (es)

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US201562155824P 2015-05-01 2015-05-01

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US (1) US10703756B2 (es)
EP (1) EP3288943B1 (es)
JP (1) JP6761815B2 (es)
AR (1) AR104461A1 (es)
CA (1) CA2984183C (es)
ES (1) ES2928757T3 (es)
TW (1) TW201706274A (es)
WO (1) WO2016178110A1 (es)

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EP3573964A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Benzothiophene and benzothiazole compounds and methods of use thereof
EP3573967A1 (en) * 2017-01-26 2019-12-04 Araxes Pharma LLC Fused hetero-hetero bicyclic compounds and methods of use thereof
US11957931B2 (en) * 2017-04-26 2024-04-16 Yale University Compositions and methods for treating vitiligo
WO2018218069A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant kras, hras or nras
TW201920150A (zh) 2017-08-01 2019-06-01 美商施萬生物製藥研發 Ip有限責任公司 作為jak激酶抑制劑之吡唑并及三唑并雙環化合物
PL3762368T3 (pl) 2018-03-08 2022-06-06 Incyte Corporation ZWIĄZKI AMINOPIRAZYNODIOLOWE JAKO INHIBITORY PI3K-γ
WO2020010003A1 (en) 2018-07-02 2020-01-09 Incyte Corporation AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS
CN112823005A (zh) 2018-08-10 2021-05-18 阿克拉瑞斯治疗股份有限公司 吡咯并嘧啶itk抑制剂
CA3125039A1 (en) * 2019-01-23 2020-07-30 Theravance Biopharma R&D Ip, Llc Imidazo[1,5-a]pyridine, 1,2,4-triazolo[4,3-a]pyridine and imidazo[1,5-a]pyrazine as jak inhibitors
CN112430235B (zh) * 2019-08-26 2024-04-05 东莞市东阳光仿制药研发有限公司 一种pf-06651600中间体的制备方法
KR102228668B1 (ko) * 2019-10-08 2021-03-17 (주)부흥산업사 메틸피퍼리딘 아미노피롤로 피리미딘의 제조방법
CN111407767B (zh) * 2020-03-28 2021-05-25 中山大学 一种磺胺间甲氧嘧啶衍生物在制备抗肿瘤药物中的应用
WO2023151069A1 (zh) * 2022-02-14 2023-08-17 湖南南新制药股份有限公司 吡咯并[2,3-d]六元杂芳环衍生物、其制备方法和药物用途

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