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AR063420A1 - Derivados de 2-ciano-4-pirimidinil sustituidos,proceso de preparacion de los mismos,medicamentos que los contienen y su uso para el tratamiento de la malaria. - Google Patents

Derivados de 2-ciano-4-pirimidinil sustituidos,proceso de preparacion de los mismos,medicamentos que los contienen y su uso para el tratamiento de la malaria.

Info

Publication number
AR063420A1
AR063420A1 ARP070104761A ARP070104761A AR063420A1 AR 063420 A1 AR063420 A1 AR 063420A1 AR P070104761 A ARP070104761 A AR P070104761A AR P070104761 A ARP070104761 A AR P070104761A AR 063420 A1 AR063420 A1 AR 063420A1
Authority
AR
Argentina
Prior art keywords
alkylene
alkyl
phenyl
ring
rest
Prior art date
Application number
ARP070104761A
Other languages
English (en)
Original Assignee
Glaxo Group Ltd
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
Priority claimed from EP06381045A external-priority patent/EP1918284A1/en
Priority claimed from EP07100630A external-priority patent/EP1947091A1/en
Priority claimed from EP07381060A external-priority patent/EP2030621A1/en
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of AR063420A1 publication Critical patent/AR063420A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • 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
    • A61P11/08—Bronchodilators
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • 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
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/08—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis for Pneumocystis carinii
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/10—Anthelmintics
    • A61P33/12—Schistosomicides
    • 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
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/02—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 two hetero rings
    • C07D403/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

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

Abstract

Compuesto de heteroarilnitrilo sustituido caracterizado porque es de formula (1) en la que: A representa CH2 y n representa 0 o 1; o A representa -O- o N(C(O)R1) y n representa 1; R1 representa alquilo C1-4 u OCH2fenilo; cuando A representa CH2, Rx representa un sustituyente metilo opcional sobre cualquier átomo de carbono del anillo al que está unido, y en cualquier otro caso Rx está ausente; R4 representa halo; a) cuando A representa CH2 y n representa 0 o 1; o A representa -O- o N(C(O)R1)) y n representa 1, R2 representa -B-alquileno C0-3-X; -B-alquileno C0-3-X-RJ, -B-alquileno C0-3-Y; - piridil-fenil-alquileno C0-3-X; o -piridil-fenil-alquileno C0-3-X-RJ; B representa i) fenilo; ii) un anillo heteroarilo de 6 miembros, que contiene uno o dos átomos de N; o iii) un anillo heteroarilo de 5 miembros, que contiene un átomo seleccionado entre N, O y S, o dos átomos seleccionados entre a) N y S o b) N y O; donde cualquier grupo fenilo de R2 está opcionalmente sustituido con al menos un grupo seleccionado independientemente entre halogeno o CF3; b) cuando A representa N(C(O)-alquilo C1-3), R2 representa, como alternativa, -OtBu; c) cuando A representa CH2, n representa 0 y Rx está presente y está tanto en la posicion 2 con respecto al punto de union del anillo al resto de la molécula como en la orientacion trans con respecto al punto de union del anillo al resto de la molécula entonces R2 representa, como alternativa, halofenil-; RJ representa Z, alquileno C1-4-Z o C(O)Z; X y Z representan independientemente un grupo hidrocarburo saturado, monocíclico, de 4, 5 o 6 miembros que contiene uno o dos átomos de nitrogeno y opcionalmente un átomo de oxigeno, que está opcionalmente sustituido con un grupo seleccionado entre: alquilo C1-4, OH y alquileno C1-4OH; Y representa -NRARB; RA representa alquilo C1-6; RB representa alquilo C1-8, -alquileno C2-6-fenilo; ciclohexilo; -alquileno C1-4CH(OH)-feniio; -C(O)-N(CH3)2, -alquileno C1-4-1,3-dioxolano; 3,3-dimetil-1,5- dioxaespiro[5.5]undec-9-il-; -alquileno C1-4NHC(O)O-alquilo C1-4 -(CHRc)1-4Rc, donde 1 o 2 casos de Rc representan OH y el resto representan hidrogeno; RD representa hidrogeno o alquilo C1-6 o un derivado farmacéuticamente aceptable del mismo.
ARP070104761A 2006-10-30 2007-10-26 Derivados de 2-ciano-4-pirimidinil sustituidos,proceso de preparacion de los mismos,medicamentos que los contienen y su uso para el tratamiento de la malaria. AR063420A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP06381045A EP1918284A1 (en) 2006-10-30 2006-10-30 Hydrazinopyrimidines as cysteine protease inhibitors
EP07100630A EP1947091A1 (en) 2007-01-16 2007-01-16 Pyrimidyl nitrile derivatives as cysteine protease inhibitors
EP07381060A EP2030621A1 (en) 2007-08-21 2007-08-21 Novel substituted pyrimidines as cysteine protease inhibitors

Publications (1)

Publication Number Publication Date
AR063420A1 true AR063420A1 (es) 2009-01-28

Family

ID=39092134

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070104761A AR063420A1 (es) 2006-10-30 2007-10-26 Derivados de 2-ciano-4-pirimidinil sustituidos,proceso de preparacion de los mismos,medicamentos que los contienen y su uso para el tratamiento de la malaria.

Country Status (8)

Country Link
US (1) US20100009956A1 (es)
EP (1) EP2077841A1 (es)
JP (1) JP2010508322A (es)
AR (1) AR063420A1 (es)
CL (1) CL2007003100A1 (es)
PE (1) PE20081471A1 (es)
TW (1) TW200825058A (es)
WO (1) WO2008052934A1 (es)

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Publication number Priority date Publication date Assignee Title
MX2010013559A (es) * 2008-06-11 2011-05-19 Irm Llc Compuestos y composiciones utiles para el tratamiento de malaria.
US8524710B2 (en) * 2010-11-05 2013-09-03 Hoffmann-La Roche Inc. Pyrrolidine derivatives
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
EP3495367B1 (en) 2012-06-13 2020-09-30 Incyte Holdings Corporation Substituted tricyclic compounds as fgfr inhibitors
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
MX2015005382A (es) * 2012-10-31 2015-07-21 Novozymes Bioag As Composiciones y metodos para fomentar el crecimiento vegetal.
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
EA035095B1 (ru) 2013-04-19 2020-04-27 Инсайт Холдингс Корпорейшн Бициклические гетероциклы в качестве ингибиторов fgfr
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
ES2751669T3 (es) 2015-02-20 2020-04-01 Incyte Corp Heterociclos bicíclicos como inhibidores FGFR
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
US11299478B2 (en) 2018-03-28 2022-04-12 Hanlim Pharmaceutical Co., Ltd. 2-cyanopyrimidin-4-yl carbamate or urea derivative or salt thereof, and pharmaceutical composition including same
CR20200590A (es) 2018-05-04 2021-04-26 Incyte Corp Formas sólidas de un inhibidor de fgfr y procesos para prepararlas
CR20200591A (es) 2018-05-04 2021-03-31 Incyte Corp Sales de un inhibidor de fgfr
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CR20220169A (es) 2019-10-14 2022-10-27 Incyte Corp Heterociclos bicíclicos como inhibidores de fgfr
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021089683A1 (en) 2019-11-06 2021-05-14 Bayer Aktiengesellschaft Inhibitors of adrenoreceptor adrac2
JP2023505257A (ja) 2019-12-04 2023-02-08 インサイト・コーポレイション Ｆｇｆｒ阻害剤の誘導体
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2022221170A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
JP2024522189A (ja) 2021-06-09 2024-06-11 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての三環式ヘテロ環

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070232586A1 (en) * 2004-04-21 2007-10-04 Kazuyuki Ohmoto Hydrazino-Substituted Heterocyclic Nitrile Compounds and Use Thereof
WO2006027211A1 (en) * 2004-09-07 2006-03-16 Glaxo Group Limited 2,4-substituted pyrimidines as cysteine protease inhibitors
WO2007025774A2 (en) * 2005-09-02 2007-03-08 Glaxo Group Limited Cysteine protease inhibitors

Also Published As

Publication number Publication date
JP2010508322A (ja) 2010-03-18
WO2008052934A1 (en) 2008-05-08
PE20081471A1 (es) 2008-12-31
EP2077841A1 (en) 2009-07-15
US20100009956A1 (en) 2010-01-14
CL2007003100A1 (es) 2008-04-18
TW200825058A (en) 2008-06-16

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