AR107041A1 - Inhibidores de la tirosina kinasa de bruton y métodos de su uso - Google Patents

Inhibidores de la tirosina kinasa de bruton y métodos de su uso

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Publication number
AR107041A1
AR107041A1 ARP160103788A ARP160103788A AR107041A1 AR 107041 A1 AR107041 A1 AR 107041A1 AR P160103788 A ARP160103788 A AR P160103788A AR P160103788 A ARP160103788 A AR P160103788A AR 107041 A1 AR107041 A1 AR 107041A1
Authority
AR
Argentina
Prior art keywords
6alkyl
group
6alq
6haloalkyl
phenyl
Prior art date
Application number
ARP160103788A
Other languages
English (en)
Original Assignee
Janssen Pharmaceutica Nv
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR107041A1 publication Critical patent/AR107041A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/16—Peri-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Abstract

Reivindicación 1: Un compuesto de la fórmula (1), y sales farmacéuticamente aceptables, estereoisómeros, isótopos, N-óxidos, o solvatos de estos, en donde R¹ es H o C₁₋₆ alquilo; R² se selecciona del grupo que consiste en: C₀₋₂alq-piperidinilo; C₀₋₂alq-pirrolidinilo; oxazepanilo; azetidinilo; azepanilo; quinuclidinilo; C₂alq-imidazolidinilo; C₂alq-piperazinilo; C₂alq-morfolinilo; tetrahidropiranilo; y C₀₋₁alq-tetrahidrofuranilo; en donde el R² se sustituye, opcionalmente, con 1, 2, ó 3 sustituyentes, cada uno se selecciona, independientemente, del grupo que consiste en: (C=O)-C(R³)=CR⁴(R⁵); oxo; halógeno; -OH; NH₂; CN; C₁₋₆ alquilo; C₁₋₆alq-OH; OC₁₋₆alquilo; C₁₋₆haloalquilo; C₃₋₆cicloalquilo; SO₂C₁₋₆alquilo; SO₂-C₂₋₆alquenilo; C₁₋₂alq-arilo; (C=O)H; (C=O)C₁₋₆alquilo; (C=O)C₁₋₆haloalquilo; (C=O)-C₂₋₆alquenilo; (C=O)-C₂₋₆alquinilo; (C=O)C₃₋₆cicloalquilo; (C=O)-fenilo; (C=O)-imidazolilo; (C=O)-C₁₋₆alqCN; (C=O)-C₁₋₆alq-OH; (C=O)-C₁₋₆alq-SO₂C₁₋₆alquilo; (C=O)-C₁₋₆alq-NR⁶R⁷; (C=O)-C₁₋₆alq-O-C₁₋₆alquilo, en donde el C₁₋₆alq- se sustituye, opcionalmente, con OH, OC₁₋₆alquilo, o NR⁶R⁷; (C=O)C₀₋₁alq-heterocicloalquilo, en donde el -alq- se sustituye, opcionalmente, con oxo y el heterocicloalquilo se sustituye, opcionalmente, con C₁₋₆alquilo; y NH(C=O)-C(R³)=CR⁴(R⁵); en donde R³ se selecciona del grupo que consiste en: H, CN, halógeno, C₁₋₆haloalquilo y C₁₋₆alquilo; R⁴ y R⁵ se seleccionan, independientemente cada uno, del grupo que consiste en: H; halógeno; C₁₋₆alquilo; CH₂OH; C₁₋₆alq-O-C₁₋₆alquilo; OC₁₋₆alquilo; C₁₋₄alq-NR⁶R⁷; C₃₋₆cicloalquilo sustituido con NH₂ o CH₃; oxetanilo sustituido con CH₃; 1-acetilpirrolidin-2-ilo; CH₂-pirrolidinilo; CH₂-piperidinilo; C(CH₃)₂-piperidinilo; CH₂-morfolinilo; C(CH₃)₂-morfolinilo; CH₂-(4aR,7aS)-tetrahidro-2H-[1,4]dioxino[2.3-c]pirrol-6(3H)-ilo; C(CH₃)₂NH(CH₂CH₂OCH₃); CH₂SO₂CH₃; CH₂NHSO₂CH₃; NH(C=O)C₁₋₆alquilo; y enlazador-PEG-biotina; y R⁶ y R⁷ se seleccionan, independientemente cada uno, del grupo que consiste en: H, C₁₋₆alquilo, ciclopropilo, (C=O)H, y CN; A se selecciona del grupo que consiste en: un enlace, fenilo; naftalenilo, piridilo; pirimidinilo; pirazinilo; piridazinilo; benzotiofenilo; y pirazolilo; en donde A se sustituye, opcionalmente, con 1, 2, ó 3 sustituyentes, cada uno se selecciona independientemente del grupo que consiste en: C₁₋₆alquilo, halógeno, OC₁₋₆alquilo, (C=O)C₁₋₆alquilo, y C₁₋₆haloalquilo; E se selecciona del grupo que consiste en: -O-, un enlace, (C=O)-NH, CH₂, y CH₂-O; y G se selecciona del grupo que consiste en: H, C₁₋₆alquilo; C₁₋₆haloalquilo; C₁₋₆alq-O-C₁₋₆alquilo; NR⁶R⁷; SO₂C₁₋₆alquilo; -OH; C₃₋₆cicloalquilo; fenilo; tiofenilo; pirimidinilo; piridilo; piridazinilo; benzofuranilo; heterocicloalquilo que contiene un heteroátomo de oxígeno; fenil-CH₂-O-fenilo; en donde el fenilo, tiofenilo, pirimidinilo, piridilo, piridazinilo, o benzofuranilo opcionalmente sustituido con 1, 2, ó 3 sustituyentes cada uno independientemente seleccionados del grupo que consiste en: halógeno, C₁₋₆alquilo, C₁₋₆haloalquilo, OC₁₋₆haloalquilo, OC₁₋₆alquilo, OC₁₋₆alquilo-OC₁₋₆alquilo, C₃₋₆cicloalquilo, CN, OH, NH₂, N(CH₃)₂, C₁₋₆alq-OC₁₋₆alquilo, SO₂C₁₋₆alquilo, (C=O)-NR⁶R⁷, SF₅, y (C=O)C₁₋₆alquilo; y estereoisómeros y variantes isotópicas de estos; y sales farmacéuticamente aceptables de este.
ARP160103788A 2015-12-10 2016-12-12 Inhibidores de la tirosina kinasa de bruton y métodos de su uso AR107041A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201562265780P 2015-12-10 2015-12-10

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AR107041A1 true AR107041A1 (es) 2018-03-14

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US (3) US10689396B2 (es)
EP (1) EP3386992B1 (es)
JP (2) JP7110097B2 (es)
KR (1) KR20180094514A (es)
CN (2) CN109071563A (es)
AR (1) AR107041A1 (es)
AU (1) AU2016366546B2 (es)
BR (1) BR112018011525B1 (es)
CA (1) CA3007993C (es)
EA (1) EA038031B1 (es)
IL (1) IL259862B (es)
JO (1) JO3793B1 (es)
MX (1) MX2018007084A (es)
TW (1) TWI739779B (es)
UY (1) UY37016A (es)
WO (1) WO2017100668A1 (es)

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JO3793B1 (ar) 2015-12-10 2021-01-31 Janssen Pharmaceutica Nv مثبطات تيروزين كاينيز بروتون وأساليب استخدامها
JO3794B1 (ar) 2015-12-10 2021-01-31 Janssen Pharmaceutica Nv المركبات متعددة الحلقات كمثبطات لتيروزين كيناز بروتون
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CN110028525A (zh) * 2018-04-13 2019-07-19 太仓运通新材料科技有限公司 一种2-氟磷酰基乙酸三乙酯的合成方法
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CN111635368B (zh) * 2020-06-12 2021-06-29 东莞市东阳光仿制药研发有限公司 一种胺化合物的制备方法
CN114478346A (zh) * 2021-12-31 2022-05-13 和鼎（南京）医药技术有限公司 一种制备乌帕替尼中间体的方法

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KR20180094514A (ko) 2018-08-23
CN113105475B (zh) 2022-09-09
JP2018536684A (ja) 2018-12-13
EA038031B1 (ru) 2021-06-25
AU2016366546A1 (en) 2018-05-31
UY37016A (es) 2017-06-30
US10822348B2 (en) 2020-11-03
CN113105475A (zh) 2021-07-13
US10800792B2 (en) 2020-10-13
BR112018011525A2 (pt) 2018-11-21
JP7110097B2 (ja) 2022-08-01
TWI739779B (zh) 2021-09-21
EP3386992B1 (en) 2019-11-27
US20170283431A1 (en) 2017-10-05
IL259862A (en) 2018-07-31
US10689396B2 (en) 2020-06-23
US20190284204A1 (en) 2019-09-19
WO2017100668A1 (en) 2017-06-15
BR112018011525B1 (pt) 2023-10-24
IL259862B (en) 2022-04-01
JP7471348B2 (ja) 2024-04-19
TW201734020A (zh) 2017-10-01
AU2016366546B2 (en) 2021-08-12
JO3793B1 (ar) 2021-01-31
US20190284203A1 (en) 2019-09-19
CA3007993A1 (en) 2017-06-15
JP2022141851A (ja) 2022-09-29
CN109071563A (zh) 2018-12-21
EP3386992A1 (en) 2018-10-17
CA3007993C (en) 2024-01-16
MX2018007084A (es) 2018-11-09
EA201891379A1 (ru) 2018-12-28

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