AR078321A1 - Derivados de 2,4'-bipiridina como inhibidores de cinasa (cdk9) - Google Patents

Derivados de 2,4'-bipiridina como inhibidores de cinasa (cdk9)

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Publication number
AR078321A1
AR078321A1 ARP100103239A ARP100103239A AR078321A1 AR 078321 A1 AR078321 A1 AR 078321A1 AR P100103239 A ARP100103239 A AR P100103239A AR P100103239 A ARP100103239 A AR P100103239A AR 078321 A1 AR078321 A1 AR 078321A1
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AR
Argentina
Prior art keywords
carbon atoms
alkyl
haloalkyl
hydrogen
cycloalkyl
Prior art date
Application number
ARP100103239A
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English (en)
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Novartis Ag
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Publication date
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Publication of AR078321A1 publication Critical patent/AR078321A1/es

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    • 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
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Immunology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Communicable Diseases (AREA)
  • Psychiatry (AREA)
  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

También se proporciona un compuesto de la formula 1 para el tratamiento de una enfermedad o condicion mediada por un inhibidor de la cinasa dependiente de ciclina (CDK). Reivindicacion 1: Un compuesto de la formula 1 o una sal farmacéuticamente aceptable del mismo, en donde: R1 se selecciona a partir de -(CH2)0-2-heteroarilo, -(CH2)0-2-arilo, alquilo de 1 a 8 átomos de carbono, alquilo de 1 a 8 átomos de carbono ramificado, cicloalquilo de 1 a 8 átomos de carbono, y un grupo hetero-cicloalquilo de 4 a 8 miembros, en donde los grupos están cada uno opcionalmente sustituidos independientemente; R2 se selecciona a partir de hidrogeno, alcoxilo de 1 a 4 átomos de carbono, haloalquilo de 1 a 4 átomos de carbono, alquilo de 1 a 4 átomos de carbono, y halogeno; A1 es N; A4 es CR6; R4 se selecciona a partir de hidrogeno, halogeno, heterociclilo-R14 de 5 a 7 miembros, y A6-L-R9; R5 se selecciona a partir de hidrogeno, alquilo de 1 a 4 átomos de carbono, haloalquilo de 1 a 4 átomos de carbono, hidroxilo, CN, -O-alquilo de 1 a 4 átomos de carbono, -O-haloalquilo de 1 a 4 átomos de carbono, cicloalquilo de 3 a 4 átomos de carbono, halo-cicloalquilo de 3 a 4 átomos de carbono, y halogeno; R6 se selecciona a partir de hidrogeno, alquilo de 1 a 4 átomos de carbono, haloalquilo de 1 a 4 átomos de carbono, CN, -O- alquilo de 1 a 4 átomos de carbono, cicloalquilo de 3 a 4 átomos de carbono, halo-cicloalquilo de 3 a 4 átomos de carbono, -O-haloalquilo de 1 a 4 átomos de carbono, y halogeno; R7 se selecciona a partir de hidrogeno, alquilo de 1 a 4 átomos de carbono, haloalquilo de 1 a 4 átomos de carbono, O-alquilo de 1 a 3 átomos de carbono, y halogeno; A6 se selecciona a partir de O, SO2, y NR8; L se selecciona a partir de alquileno de 0 a 3 átomos de carbono, -CHD-, -CD2-, cicloalquilo de 3 a 6 átomos de carbono, halo-cicloalquilo de 3 a 6 átomos de carbono, hetero-cicloalquilo de 4 a 7 átomos de carbono, alquileno de 3 a 8 átomos de carbono ramificado, halo-alquileno de 3 a 8 átomos de carbono ramificado; R8 se selecciona a partir de hidrogeno, alquilo de 1 a 4 átomos de carbono, y alquilo de 3 a 8 átomos de carbono ramificado, y haloalquilo de 3 a 8 átomos de carbono ramificado; R9 se selecciona a partir de hidrogeno, alquilo de 1 a 6 átomos de carbono, cicloalquilo de 1 a 8 átomos de carbono, alquilo de 1 a 8 átomos de carbono ramificado, -(CH2)0-2-heteroarilo, (CH2)0-2-heterociclo-alquilo de 4 a 8 miembros, y (CH2)0-2-arilo, en donde los grupos están opcionalmente sustituidos; y R14 se selecciona a partir de hidrogeno, fenilo, halogeno, hidroxilo, alquilo de 1 a 4 átomos de carbono, alquilo de 3 a 6 átomos de carbono ramificado, haloalquilo de 1 a 4 átomos de carbono, CF3, =O, y O-alquilo de 1 a 4 átomos de carbono.
ARP100103239A 2009-09-04 2010-09-03 Derivados de 2,4'-bipiridina como inhibidores de cinasa (cdk9) AR078321A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US27593809P 2009-09-04 2009-09-04
US28496109P 2009-12-28 2009-12-28

Publications (1)

Publication Number Publication Date
AR078321A1 true AR078321A1 (es) 2011-11-02

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ID=43478200

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100103239A AR078321A1 (es) 2009-09-04 2010-09-03 Derivados de 2,4'-bipiridina como inhibidores de cinasa (cdk9)

Country Status (11)

Country Link
US (1) US20110130380A1 (es)
EP (1) EP2473499A1 (es)
KR (1) KR20120092586A (es)
CN (1) CN102471310A (es)
AR (1) AR078321A1 (es)
AU (1) AU2010291206A1 (es)
CA (1) CA2771563A1 (es)
MX (1) MX2012002761A (es)
TW (1) TW201113273A (es)
UY (1) UY32877A (es)
WO (1) WO2011026911A1 (es)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8415381B2 (en) 2009-07-30 2013-04-09 Novartis Ag Heteroaryl compounds and their uses
WO2012101064A1 (en) * 2011-01-28 2012-08-02 Novartis Ag N-acyl pyrimidine biaryl compounds as protein kinase inhibitors
EP2668162A1 (en) * 2011-01-28 2013-12-04 Novartis AG Substituted bi-heteroaryl compounds as cdk9 inhibitors and their uses
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
SG11201604820XA (en) 2014-01-14 2016-07-28 Millennium Pharm Inc Heteroaryls and uses thereof
EP3094326A4 (en) 2014-01-14 2017-07-26 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
MX2019003095A (es) 2016-09-19 2019-07-04 Novartis Ag Combinaciones terapeuticas que comprenden un inhibidor de raf y un inhibidor de erk.
EP3804724B1 (en) 2016-10-20 2022-12-07 Pfizer Inc. Cdk inhibitors for treating pah
PT3618875T (pt) 2017-05-02 2023-08-07 Novartis Ag Terapia de combinação que compreende um inibidor de raf e trametinib
AU2020401999B2 (en) * 2019-12-09 2024-01-18 Cspc Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd. Compound as cyclin-dependent kinase 9 inhibitor and use thereof
CN115381823A (zh) * 2021-05-24 2022-11-25 石药集团中奇制药技术（石家庄）有限公司 一种周期蛋白依赖性激酶9抑制剂的用途
CN115381824A (zh) * 2021-05-24 2022-11-25 石药集团中奇制药技术（石家庄）有限公司 周期蛋白依赖性激酶9抑制剂的用途
CN115448874A (zh) * 2021-06-09 2022-12-09 石药集团中奇制药技术（石家庄）有限公司 固体形式的周期蛋白依赖性激酶9抑制剂及其用途

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PT72878B (en) 1980-04-24 1983-03-29 Merck & Co Inc Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
EP1631260A2 (en) 2003-02-28 2006-03-08 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
WO2005040152A1 (en) * 2003-10-20 2005-05-06 E.I. Dupont De Nemours And Company Heteroyclylphenyl-and heterocyclylpyridyl-substituted azolecarboxamides as herbicides
CN101568529A (zh) * 2006-12-22 2009-10-28 诺瓦提斯公司 作为cdk抑制剂、用于治疗癌症、炎症和病毒感染的杂芳基-杂芳基化合物

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Publication number Publication date
WO2011026911A1 (en) 2011-03-10
TW201113273A (en) 2011-04-16
UY32877A (es) 2011-04-29
US20110130380A1 (en) 2011-06-02
KR20120092586A (ko) 2012-08-21
AU2010291206A1 (en) 2012-02-23
EP2473499A1 (en) 2012-07-11
WO2011026911A8 (en) 2011-04-21
CN102471310A (zh) 2012-05-23
MX2012002761A (es) 2012-04-19
CA2771563A1 (en) 2011-03-10

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