AR092536A1 - Inhibidores de la tirosina-quinasa de bruton - Google Patents

Inhibidores de la tirosina-quinasa de bruton

Info

Publication number
AR092536A1
AR092536A1 ARP130103257A ARP130103257A AR092536A1 AR 092536 A1 AR092536 A1 AR 092536A1 AR P130103257 A ARP130103257 A AR P130103257A AR P130103257 A ARP130103257 A AR P130103257A AR 092536 A1 AR092536 A1 AR 092536A1
Authority
AR
Argentina
Prior art keywords
alkyl
amino
cycloalkyl
optionally substituted
halogen
Prior art date
Application number
ARP130103257A
Other languages
English (en)
Inventor
E Brotherton-Pleiss Christine
Hilgenkamp Ramona
K Kondru Rama
Javier Lopez-Tapia Francisco
Lou Yan
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR092536A1 publication Critical patent/AR092536A1/es

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • 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
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Los compuestos son útiles además para tratar enfermedades inflamatorias y autoinmunes asociadas con la proliferación aberrante de las células B, por ejemplo la artritis reumatoide. Se describen también composiciones que contienen los compuestos de la fórmula (1) y por lo menos un vehículo, diluyente o excipiente. Reivindicación 1: Un compuesto de la fórmula (1), en la que: ⁻ ⁻ ⁻ ⁻ ⁻ es un enlace sencillo o un doble enlace; X es CH, CH₂ o N; R es H, -R¹, -R¹-R²-R³, -R¹-R³ o -R²-R³; R¹ es arilo, heteroarilo, heteroarilo bicíclico, cicloalquilo o heterocicloalquilo, cada uno de ellos está opcionalmente sustituido por uno o más alquilo inferior, hidroxi, hidroxialquilo inferior, alcoxi inferior, halógeno, nitro, amino, amido, ciano, oxo o haloalquilo inferior; R² es -C(=O), -C(=O)O, -C(=O)NR², -NHC(=O)O, -C(R²)₂, -O, -S, -C(=NH)NR² o -S(=O)₂; cada R² es con independencia H o alquilo inferior; R³ es H o R⁴; R⁴ es alquilo inferior, haloalquilo inferior, alcoxi inferior, amino, (alquilo inferior)-amino, cicloalquil-amino, di(alquilo inferior)-amino, arilo, arilalquilo, alquilarilo, heteroarilo, alquil-heteroarilo, heteroaril-alquilo, cicloalquilo, alquil-cicloalquilo, cicloalquil-alquilo, heterocicloalquilo, alquil-heterocicloalquilo, heterocicloalquilalquilo, cicloalquilo bicíclico, heterocicloalquilo bicíclico, espirocicloalquilo, espiroheterocicloalquilo o espiroheterocicloalquilo bicíclico, cada uno de ellos está opcionalmente sustituido por uno o más alquilo inferior, halógeno, (alquilo inferior)-amino, di(alquilo inferior)-amino, hidroxi, hidroxialquilo inferior, alcoxi inferior, alcanoílo inferior, halógeno, nitro, amino, amido, acilo, ciano, oxo, sulfonilo, alquilo inferior sulfonilo, guanidino, hidroxil-amino, carboxi, carbamoilo, carbamato, haloalcoxi inferior, heterocicloalquilo o haloalquilo inferior, en el que dos grupos alquilo inferior juntos pueden formar un anillo; Y⁴ es Y⁴ᵃ, Y⁴ᵇ, Y⁴ᶜ o Y⁴ᵈ; Y⁴ᵃ es H o halógeno; Y⁴ᵇ es alquilo inferior opcionalmente sustituido por uno o más sustituyentes elegidos entre el grupo formado por haloalquilo inferior, halógeno, hidroxi, amino, ciano y alcoxi inferior; Y⁴ᶜ es cicloalquilo inferior opcionalmente sustituido por uno o más sustituyentes elegidos entre el grupo formado por alquilo inferior, haloalquilo inferior, halógeno, hidroxi, amino, ciano y alcoxi inferior; e Y⁴ᵈ es amino opcionalmente sustituido por uno o más alquilo inferior, alcoxi alquilo inferior o hidroxialquilo inferior; o una sal farmacéuticamente aceptable del mismo.
ARP130103257A 2012-09-13 2013-09-12 Inhibidores de la tirosina-quinasa de bruton AR092536A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201261700373P 2012-09-13 2012-09-13

Publications (1)

Publication Number Publication Date
AR092536A1 true AR092536A1 (es) 2015-04-22

Family

ID=49118551

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP130103257A AR092536A1 (es) 2012-09-13 2013-09-12 Inhibidores de la tirosina-quinasa de bruton

Country Status (13)

Country Link
US (1) US9499548B2 (es)
EP (1) EP2895473A1 (es)
JP (1) JP2015531781A (es)
KR (1) KR20150054994A (es)
CN (1) CN104619696A (es)
AR (1) AR092536A1 (es)
BR (1) BR112015005361A2 (es)
CA (1) CA2881761A1 (es)
HK (1) HK1210461A1 (es)
MX (1) MX2015002901A (es)
RU (1) RU2015111133A (es)
TW (1) TW201416361A (es)
WO (1) WO2014040965A1 (es)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MA37830B1 (fr) 2012-08-10 2018-09-28 Boehringer Ingelheim Int Composés hétéroromatiques en tant qu'inhibiteurs de la tyrosine kinase de bruton (btk)
WO2014076104A1 (en) * 2012-11-16 2014-05-22 F. Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
US9663494B2 (en) * 2013-03-05 2017-05-30 Hoffmann-La Roche Inc. Inhibitors of bruton's tyrosine kinase
CN104177338B (zh) * 2013-05-22 2018-04-03 南京勇山生物科技有限公司 一类布鲁顿激酶抑制剂
CN111303159A (zh) * 2014-10-02 2020-06-19 豪夫迈·罗氏有限公司 用于治疗由布鲁顿酪氨酸激酶(btk)介导的疾病的吡唑甲酰胺化合物
WO2017123695A1 (en) * 2016-01-13 2017-07-20 Boehringer Ingelheim International Gmbh Isoquinolones as btk inhibitors
AU2019360928B2 (en) 2018-10-15 2023-11-09 Nurix Therapeutics, Inc. Bifunctional compounds for degrading BTK via ubiquitin proteosome pathway
CN114364667A (zh) 2019-04-09 2022-04-15 紐力克斯治疗公司 用于Cbl-b抑制的3-取代哌啶类化合物以及Cbl-b抑制剂与癌症疫苗和/或溶瘤病毒联合的用途
AU2020278592A1 (en) 2019-05-17 2021-12-02 Nurix Therapeutics, Inc. Cyano cyclobutyl compounds for Cbl-b inhibition and uses thereof
EP4055019A1 (en) * 2019-11-08 2022-09-14 Nurix Therapeutics, Inc. Bifunctional compounds for degrading btk via ubiquitin proteosome pathway
EP4069237A1 (en) 2019-12-04 2022-10-12 Nurix Therapeutics, Inc. Bifunctional compounds for degrading btk via ubiquitin proteosome pathway
WO2022206924A1 (zh) * 2021-04-02 2022-10-06 南京明德新药研发有限公司 含氮三并环双功能化合物及其制备方法和应用

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7683064B2 (en) * 2008-02-05 2010-03-23 Roche Palo Alto Llc Inhibitors of Bruton's tyrosine kinase
DK2242749T3 (da) * 2008-02-05 2013-06-17 Hoffmann La Roche Nye pyridinoner og pyridazinoner
EP2297142B1 (en) * 2008-06-24 2015-10-14 F. Hoffmann-La Roche AG Novel substituted pyridin-2-ones and pyridazin-3-ones
KR101320763B1 (ko) * 2008-07-02 2013-10-21 에프. 호프만-라 로슈 아게 키나아제 억제제로서의 신규 페닐피라지논
US8299077B2 (en) * 2009-03-02 2012-10-30 Roche Palo Alto Llc Inhibitors of Bruton's tyrosine kinase
AR082590A1 (es) * 2010-08-12 2012-12-19 Hoffmann La Roche Inhibidores de la tirosina-quinasa de bruton

Also Published As

Publication number Publication date
MX2015002901A (es) 2015-06-03
BR112015005361A2 (pt) 2017-07-04
EP2895473A1 (en) 2015-07-22
RU2015111133A (ru) 2016-11-10
HK1210461A1 (en) 2016-04-22
KR20150054994A (ko) 2015-05-20
CN104619696A (zh) 2015-05-13
US9499548B2 (en) 2016-11-22
CA2881761A1 (en) 2014-03-20
TW201416361A (zh) 2014-05-01
WO2014040965A1 (en) 2014-03-20
US20150210704A1 (en) 2015-07-30
JP2015531781A (ja) 2015-11-05

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