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AR077977A1 - Compuestos y composiciones como inhibidores de cinasa de proteina - Google Patents

Compuestos y composiciones como inhibidores de cinasa de proteina

Info

Publication number
AR077977A1
AR077977A1 ARP100103125A ARP100103125A AR077977A1 AR 077977 A1 AR077977 A1 AR 077977A1 AR P100103125 A ARP100103125 A AR P100103125A AR P100103125 A ARP100103125 A AR P100103125A AR 077977 A1 AR077977 A1 AR 077977A1
Authority
AR
Argentina
Prior art keywords
carbon atoms
alkyl
halogen
substituted
cycloalkyl
Prior art date
Application number
ARP100103125A
Other languages
English (en)
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of AR077977A1 publication Critical patent/AR077977A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Las composiciones farmacéuticas de los mismos son utiles para el tratamiento de las enfermedades asociadas con B-Raf. Reivindicacion 1: Un compuesto de la formula (1) o (2): en donde: R1 es: (i) H, (ii) cicloalquilo (de 3 a 6 átomos de carbono) opcionalmente sustituido con ciano; (iii) alquilo (de 1 a 3 átomos de carbono) opcionalmente sustituido con ciano, -C(O)NH2, o hidroxilo, o (iv) -X1NHC(O)OR1a o -X1NHC(O)NHR1a, en donde X1 es alquileno (de 1 a 4 átomos de carbono) opcionalmente sustituido con 1 a 3 grupos, cada uno independientemente seleccionado a partir de halogeno, alquilo (de 1 a 4 átomos de carbono), o alquilo (de 1 a 4 átomos de carbono) sustituido por halogeno, y R1a es H, alquilo (de 1 a 4 átomos de carbono), o alquilo (de 1 a 4 átomos de carbono) sustituido por halogeno; R1b es H o metilo; R2 es H o halogeno; R3 es H, halogeno, alcoxilo (de 1 a 4 átomos de carbono), alquilo (de 1 a 4 átomos de carbono), alcoxilo (de 1 a 4 átomos de carbono) sustituido por halogeno, o alquilo (de 1 a 4 átomos de carbono) sustituido por halogeno; R4 es halogeno, H, o alquilo (de 1 a 4 átomos de carbono); R5 es alquilo (de 1 a 6 átomos de carbono), cicloalquilo (de 3 a 6 átomos de carbono), alquilo ramificado (de 3 a 8 átomos de carbono), alquilo (de 1 a 6 átomos de carbono) sustituido por halogeno, alquilo ramificado (de 3 a 8 átomos de carbono) sustituido por halogeno, cicloalquilo (de 3 a 6 átomos de carbono)-alquileno (de 1 a 3 átomos de carbono), o fenilo, en donde el fenilo está opcionalmente sustituido con 1 a 3 sustituyentes, cada uno independientemente seleccionado a partir de halogeno, CH3, o CF3; R6 es H, alquilo (de 1 a 4 átomos de carbono), o halogeno; y R7 es H, alquilo (de 1 a 6 átomos de carbono), cicloalquilo (de 3 a 6 átomos de carbono), 1-metil-cicloalquilo (de 3 a 6 átomos de carbono), alquilo ramificado (de 3 a 8 átomos de carbono), o fenilo, en donde el fenilo está opcionalmente sustituido con 1 a 3 sustituyentes seleccionados a partir de halogeno, alquilo (de 1 a 4 átomos de carbono) o alquilo (de 1 a 4 átomos de carbono) sustituido por halogeno; o una sal farmacéuticamente aceptable del mismo.
ARP100103125A 2009-08-28 2010-08-26 Compuestos y composiciones como inhibidores de cinasa de proteina AR077977A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US23808309P 2009-08-28 2009-08-28
US31306110P 2010-03-11 2010-03-11

Publications (1)

Publication Number Publication Date
AR077977A1 true AR077977A1 (es) 2011-10-05

Family

ID=42829939

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100103125A AR077977A1 (es) 2009-08-28 2010-08-26 Compuestos y composiciones como inhibidores de cinasa de proteina

Country Status (19)

Country Link
US (3) US8242260B2 (es)
EP (1) EP2470528B1 (es)
JP (1) JP5726190B2 (es)
KR (1) KR101714107B1 (es)
CN (1) CN102596937B (es)
AR (1) AR077977A1 (es)
AU (1) AU2010288455B2 (es)
BR (1) BR112012004448A2 (es)
CA (1) CA2771673C (es)
EA (1) EA020479B1 (es)
ES (1) ES2527176T3 (es)
IN (1) IN2012DN00869A (es)
JO (1) JO3007B1 (es)
MX (1) MX2012002542A (es)
PL (1) PL2470528T3 (es)
PT (1) PT2470528E (es)
TW (1) TWI487701B (es)
UY (1) UY32859A (es)
WO (1) WO2011023773A1 (es)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR077975A1 (es) 2009-08-28 2011-10-05 Irm Llc Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina
ES2576061T3 (es) 2010-02-25 2016-07-05 Dana-Farber Cancer Institute, Inc. Mutaciones de BRAF que confieren resistencia a inhibidores de BRAF
WO2013059634A1 (en) 2011-10-20 2013-04-25 The Regents Of The University Of California Use of cdk9 inhibitors to reduce cartilage degradation
BR112014011223A8 (pt) 2011-11-11 2023-01-31 Novartis Ag Método de tratar uma doença proliferativa
KR102091295B1 (ko) 2011-11-23 2020-03-19 어레이 바이오파마 인크. 제약 제제
US9408885B2 (en) 2011-12-01 2016-08-09 Vib Vzw Combinations of therapeutic agents for treating melanoma
US20150232452A1 (en) * 2012-09-19 2015-08-20 Ruga Corporation Novel raf kinase inhibitors
US9242969B2 (en) * 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
RU2015149937A (ru) 2013-05-30 2017-07-06 Плексксикон Инк. Соединения для модулирования киназы и показания к их применению
US9714234B2 (en) 2013-06-25 2017-07-25 Bristol-Myers Squibb Company Carbazole carboxamide compounds
TWI648272B (zh) 2013-06-25 2019-01-21 美商必治妥美雅史谷比公司 經取代之四氫咔唑及咔唑甲醯胺化合物
PL3038622T3 (pl) * 2013-08-28 2018-09-28 Medivation Technologies Llc Związki heterocykliczne i sposoby zastosowania
GB2517988A (en) * 2013-09-09 2015-03-11 Redx Pharma Ltd Compounds
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
US10300073B2 (en) 2014-10-14 2019-05-28 The Regents Of The University Of California Use of CDK9 and BRD4 inhibitors to inhibit inflammation
CN104402920B (zh) * 2014-11-27 2018-04-03 河南科技学院 一种合成2‑卤代‑3‑频那醇硼酸酯‑5‑氯苯胺的方法
EP3515446B1 (en) 2016-09-19 2023-12-20 Novartis AG Therapeutic combinations comprising a raf inhibitor and a erk inhibitor
EP3579872A1 (en) 2017-02-10 2019-12-18 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of cancers associated with activation of the mapk pathway
CN110494166B (zh) 2017-05-02 2022-11-08 诺华股份有限公司 组合疗法
JP7416716B2 (ja) 2017-12-28 2024-01-17 トラクト ファーマシューティカルズ インコーポレイテッド 円柱上皮幹細胞のための幹細胞培養系およびそれに関連した使用法
WO2020124397A1 (en) * 2018-12-19 2020-06-25 Inventisbio Shanghai Ltd. C-terminal src kinase inhibitors
KR102881316B1 (ko) 2019-05-13 2025-11-05 노파르티스 아게 암 치료를 위한 raf 억제제로서의 n-(3-(2-(2-하이드록시에톡시)-6-모르폴리노피리딘-4-일)-4-메틸페닐)-2 (트리플루오로메틸)이소니코틴아미드의 새로운 결정질 형태
US20230303551A1 (en) * 2020-08-13 2023-09-28 Albert Einstein College Of Medicine N-cyclyl-sulfonamides useful for inhibiting raf
EP4499634A1 (en) 2022-03-28 2025-02-05 Nikang Therapeutics, Inc. Sulfonamido derivatives as cyclin-dependent kinase 2 inhibitors
EP4536363A1 (en) 2022-06-08 2025-04-16 Nikang Therapeutics, Inc. Sulfamide derivatives as cyclin-dependent kinase 2 inhibitors
WO2025072462A1 (en) 2023-09-27 2025-04-03 Nikang Therapeutics, Inc. Sulfonamide derivatives as cyclin-dependent kinase 2 inhibitors

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2659739A (en) 1950-04-14 1953-11-17 Eastman Kodak Co 1-hydroxy-4-beta-cyanopropylamino-anthraquinone and process for preparing same
US6358932B1 (en) 1994-05-31 2002-03-19 Isis Pharmaceticals, Inc. Antisense oligonucleotide inhibition of raf gene expression
US6391636B1 (en) 1994-05-31 2002-05-21 Isis Pharmaceuticals, Inc. Antisense oligonucleotide modulation of raf gene expression
US6037136A (en) 1994-10-24 2000-03-14 Cold Spring Harbor Laboratory Interactions between RaF proto-oncogenes and CDC25 phosphatases, and uses related thereto
US5717100A (en) 1995-10-06 1998-02-10 Merck & Co., Inc. Substituted imidazoles having anti-cancer and cytokine inhibitory activity
GB2306108A (en) * 1995-10-13 1997-04-30 Merck & Co Inc Treatment of Raf-mediated cancers with imidazole derivatives
IL127210A0 (en) 1996-05-23 1999-09-22 Applied Research Systems Compounds inhibiting the binding of raf-1 or 13-3-3 proteins to the beta-chain of il-2 pharmaceutical compositions containing them and their use
AR012634A1 (es) 1997-05-02 2000-11-08 Sugen Inc Compuesto basado en quinazolina, composicion famaceutica que lo comprende, metodo para sintetizarlo, su uso, metodos de modulacion de la funcion deserina/treonina proteinaquinasa con dicho compuesto y metodo in vitro para identificar compuestos que modulan dicha funcion
US6187799B1 (en) 1997-05-23 2001-02-13 Onyx Pharmaceuticals Inhibition of raf kinase activity using aryl ureas
GB9716557D0 (en) 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
US6022884A (en) 1997-11-07 2000-02-08 Amgen Inc. Substituted pyridine compounds and methods of use
US6204467B1 (en) 1998-03-24 2001-03-20 Ford Global Technologies, Inc. Method and apparatus for resistive welding
RU2319693C9 (ru) 1999-01-13 2008-08-20 Байер Копэрейшн Производные мочевины (варианты), фармацевтическая композиция (варианты) и способ лечения заболевания, связанного с ростом раковых клеток (варианты)
US6756410B2 (en) 2000-08-30 2004-06-29 Kamal D. Mehta Induction of LDL receptor expression by extracellular-signal regulated kinase, ERK-1/2
MXPA04008893A (es) 2002-03-13 2005-06-20 Array Biopharma Inc Derivados de bencimidazol n3 alquilados como inhibidores de mek.
US6644516B1 (en) 2002-11-06 2003-11-11 Continental Afa Dispensing Company Foaming liquid dispenser
KR20070113252A (ko) 2005-02-25 2007-11-28 쿠도스 파마슈티칼스 리미티드 2,4-디아미노-피리도피리미딘 유도체 및 이의 mTOR억제제로서의 용도
EP1877388A2 (en) 2005-02-25 2008-01-16 Kudos Pharmaceuticals Ltd Hydrazinomethyl, hydrazonomethyl and 5-membered heterocylic compounds which act as mtor inhibitors and their use as anti cancer agents
JP5161102B2 (ja) 2005-11-22 2013-03-13 クドス ファーマシューティカルズ リミテッド mTOR阻害剤としてのピリドピリミジン、ピラゾピリミジンおよびピリミドピリミジン誘導体
US20110034454A1 (en) 2006-01-11 2011-02-10 Allan Paul Dishington Morpholino pyrimidine derivatives and their use in therapy
KR101438245B1 (ko) 2006-08-23 2014-09-04 쿠도스 파마슈티칼스 리미티드 Mtor 억제제로서의 2-메틸모르폴린 피리도-, 피라조- 및 피리미도-피리미딘 유도체
TW200922582A (en) 2007-08-20 2009-06-01 Organon Nv N-benzyl, N'-arylcarbonylpiperazine derivatives
US8129394B2 (en) * 2008-03-21 2012-03-06 Novartis Ag Heteroaryl-substituted imidazole compounds and uses thereof
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
BRPI0916356B1 (pt) * 2008-07-24 2022-08-23 Nerviano Medical Sciences S.R.L 3,4-diaril pirazois como inibidores da proteína quinase

Also Published As

Publication number Publication date
US20140011825A1 (en) 2014-01-09
CA2771673C (en) 2016-07-12
AU2010288455B2 (en) 2013-01-31
EA020479B1 (ru) 2014-11-28
EP2470528A1 (en) 2012-07-04
IN2012DN00869A (es) 2015-07-10
US20110052578A1 (en) 2011-03-03
JO3007B1 (ar) 2016-09-05
US20120225899A1 (en) 2012-09-06
UY32859A (es) 2011-03-31
KR20120092577A (ko) 2012-08-21
KR101714107B1 (ko) 2017-03-08
CN102596937B (zh) 2014-02-12
AU2010288455A1 (en) 2012-02-23
US8859548B2 (en) 2014-10-14
BR112012004448A2 (pt) 2017-05-30
JP5726190B2 (ja) 2015-05-27
US8563553B2 (en) 2013-10-22
WO2011023773A1 (en) 2011-03-03
CA2771673A1 (en) 2011-03-03
EA201200323A1 (ru) 2012-09-28
EP2470528B1 (en) 2014-10-01
ES2527176T3 (es) 2015-01-21
MX2012002542A (es) 2012-04-02
PT2470528E (pt) 2014-12-29
US8242260B2 (en) 2012-08-14
TW201111365A (en) 2011-04-01
TWI487701B (zh) 2015-06-11
CN102596937A (zh) 2012-07-18
PL2470528T3 (pl) 2015-03-31
JP2013503139A (ja) 2013-01-31

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