MA29253B1 - Derives de pyrazole destines a inhiber les cdk et gsk - Google Patents

Derives de pyrazole destines a inhiber les cdk et gsk

Info

Publication number
MA29253B1
MA29253B1 MA30143A MA30143A MA29253B1 MA 29253 B1 MA29253 B1 MA 29253B1 MA 30143 A MA30143 A MA 30143A MA 30143 A MA30143 A MA 30143A MA 29253 B1 MA29253 B1 MA 29253B1
Authority
MA
Morocco
Prior art keywords
group
gsk
activity
inhibiting cdk
pyrazole derivatives
Prior art date
Application number
MA30143A
Other languages
English (en)
Inventor
Paul Graham Wyatt
Valerio Berdini
Adrian Liam Gill
Gary Trewartha
Andrew James Woodhead
Eva Figueroa Navarro
Michael Alistair O'brien
Theresa Rachel Phillips
Original Assignee
Astex Therapeutics 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 GB0501480A external-priority patent/GB0501480D0/en
Priority claimed from GB0501748A external-priority patent/GB0501748D0/en
Application filed by Astex Therapeutics Ltd filed Critical Astex Therapeutics Ltd
Publication of MA29253B1 publication Critical patent/MA29253B1/fr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P31/12—Antivirals
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • 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
    • A61P9/06—Antiarrhythmics
    • 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
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38—Nitrogen atoms
    • C07D231/40—Acylated on said nitrogen atom
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    • 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
    • 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
    • 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
    • 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
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
    • C07D417/14—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 three or more hetero rings

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  • 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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Psychology (AREA)
  • AIDS & HIV (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Molecular Biology (AREA)
  • Endocrinology (AREA)

Abstract

LA PRÉSENTE INVENTION CONCERNE DES COMPOSÉS DE FORMULE (I), OU LEURS SELS, TAUTOMÈRES, N-OXYDES OU SOLVATES, OÙ : R1 EST CHOISI PARMI : (A) LE 2,6-DICHLOROPHÉNYLE ; (B) LE 2,6-DIFLUOROPHÉNYLE; (C) UN GROUPE PHÉNYLE 2,3,6-TRISUBSTITUÉ DANS LEQUEL LES SUBSTITUANTS DU GROUPE PHÉNYLE SONT CHOISIS PARMI LE FLUOR, LE CHLORE, LE MÉTHYLE ET LE MÉTHOXY; (D) UN GROUPE R0; (E) UN GROUPE R1A ; (F) UN GROUPE R1B ; (G) UN GROUPE R1C ; (H) UN GROUPE R1D ; ET (J) UN 2,6-DIFLUOROPHÉNYLAMINO ; R0, R1A, R1B, R1C, R1D, R2A, R2B ET R3 ÉTANT TELS QUE DÉFINIS DANS LES REVENDICATIONS. CES COMPOSÉS PRÉSENTENT UNE ACTIVITÉ D'INHIBITION DE L'ACTIVITÉ DES KINASES CDK (TELLES QUE CDK1 OU CDK2) ET DE L'ACTIVITÉ DE LA GLYCOGÈNE SYNTHASE KINASE-3.
MA30143A 2005-01-21 2007-08-16 Derives de pyrazole destines a inhiber les cdk et gsk MA29253B1 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US64621705P 2005-01-21 2005-01-21
GB0501480A GB0501480D0 (en) 2005-01-22 2005-01-22 Pharmaceutical compounds
GB0501748A GB0501748D0 (en) 2005-01-27 2005-01-27 Pharmaceutical compounds
US65133905P 2005-02-09 2005-02-09

Publications (1)

Publication Number Publication Date
MA29253B1 true MA29253B1 (fr) 2008-02-01

Family

ID=35967182

Family Applications (3)

Application Number Title Priority Date Filing Date
MA30143A MA29253B1 (fr) 2005-01-21 2007-08-16 Derives de pyrazole destines a inhiber les cdk et gsk
MA30144A MA29254B1 (fr) 2005-01-21 2007-08-16 Derives de pyrazole servant a inhiber les kinases dependantes des cyclines (cdk) et les glycogene synthases kinases (gsk)
MA30145A MA29255B1 (fr) 2005-01-21 2007-08-16 Derives de pyrazole destines a inhiber les kinases dependantes des cyclines (cdk) et les glycogene synthases kinases (gsk)

Family Applications After (2)

Application Number Title Priority Date Filing Date
MA30144A MA29254B1 (fr) 2005-01-21 2007-08-16 Derives de pyrazole servant a inhiber les kinases dependantes des cyclines (cdk) et les glycogene synthases kinases (gsk)
MA30145A MA29255B1 (fr) 2005-01-21 2007-08-16 Derives de pyrazole destines a inhiber les kinases dependantes des cyclines (cdk) et les glycogene synthases kinases (gsk)

Country Status (15)

Country Link
US (2) US20080306069A1 (fr)
EP (3) EP1853600A1 (fr)
JP (3) JP2008528465A (fr)
KR (3) KR20070107049A (fr)
AR (3) AR053662A1 (fr)
AU (3) AU2006207316A1 (fr)
BR (2) BRPI0606107A2 (fr)
CA (3) CA2593656A1 (fr)
IL (3) IL184499A0 (fr)
MA (3) MA29253B1 (fr)
MX (3) MX2007008782A (fr)
NO (3) NO20073960L (fr)
PE (3) PE20060876A1 (fr)
TN (3) TNSN07279A1 (fr)
WO (3) WO2006077416A1 (fr)

Families Citing this family (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2532965C (fr) * 2003-07-22 2013-05-14 Astex Therapeutics Limited Composes 1h-pyrazole 3,4-disubstitues et leur utilisation en tant que kinases dependant des cyclines (cdk) et modulateurs de la glycogene synthase kinase-3 (gsk-3)
TW200533657A (en) 2004-02-17 2005-10-16 Esteve Labor Dr Substituted pyrazoline compounds, their preparation and use as medicaments
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
US20080139620A1 (en) * 2005-01-21 2008-06-12 Astex Therapeutics Limited Pyrazole Derivatives For The Inhibition Of Cdk's And Gsk's
CN101146532B (zh) * 2005-01-21 2012-05-09 阿斯泰克斯治疗有限公司 药物化合物
AR054425A1 (es) 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
EP1845975A1 (fr) * 2005-01-21 2007-10-24 Astex Therapeutics Limited Combinaisons d'inhibiteurs de pyrazole kinase et d'autres agents antitumoraux
AR053662A1 (es) * 2005-01-21 2007-05-16 Astex Therapeutics Ltd Compuestos de pirazol inhibidores de la actividad quinasa cdk y gsk
MX2007008781A (es) * 2005-01-21 2007-09-11 Astex Therapeutics Ltd Compuestos farmaceuticos.
US20090036607A1 (en) * 2005-03-03 2009-02-05 Mitsubishi Rayon Co., Ltd. Polymer particle, resin composition containing same, and molded body
EP1743892A1 (fr) 2005-07-15 2007-01-17 Laboratorios del Dr. Esteve S.A. Composés pyrazoline substitués, leur préparation et utilisation comme médicaments
EP1743890A1 (fr) 2005-07-15 2007-01-17 Laboratorios Del Dr. Esteve, S.A. Dérivés 4,5-dihydro-1H-pyrazole, leur, préparation et utilisation comme médicaments.
US7897589B2 (en) 2005-07-15 2011-03-01 Laboratorios Del Dr. Esteve, S.A. Substituted pyrazoline compounds, their preparation and use as medicaments
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