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BRPI0415759A - compostos de pirimidin-4-il-3,4-tiona e uso dos mesmos na terapia - Google Patents

compostos de pirimidin-4-il-3,4-tiona e uso dos mesmos na terapia

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Publication number
BRPI0415759A
BRPI0415759A BRPI0415759-1A BRPI0415759A BRPI0415759A BR PI0415759 A BRPI0415759 A BR PI0415759A BR PI0415759 A BRPI0415759 A BR PI0415759A BR PI0415759 A BRPI0415759 A BR PI0415759A
Authority
BR
Brazil
Prior art keywords
independently
optionally substituted
compounds
cor
heteroaryl
Prior art date
Application number
BRPI0415759-1A
Other languages
English (en)
Inventor
Shudong Wang
Gavin Wood
Kenneth W Duncan
Christopher Meades
Darren Gibson
Janice J Mclachlan
Alex Perry
David Blake
Daniella I Zheleva
Peter Fischer
Original Assignee
Cyclacel 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 GB0324599A external-priority patent/GB0324599D0/en
Priority claimed from GB0330013A external-priority patent/GB0330013D0/en
Application filed by Cyclacel Ltd filed Critical Cyclacel Ltd
Publication of BRPI0415759A publication Critical patent/BRPI0415759A/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
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    • A61P3/00Drugs for disorders of the metabolism
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    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • A61P31/22Antivirals for DNA viruses for herpes viruses
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    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06Antimalarials
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00Drugs for disorders of the cardiovascular system
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Cardiology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
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Abstract

"COMPOSTOS DE PIRIMIDIN-4-IL-3,4-TIONA E USO DOS MESMOS NA TERAPIA". A presente invenção refere-se aos compostos da fórmula: (I) ou sais farmaceuticamente aceitáveis dos mesmos, em que R¬ 1¬ e R¬ 5¬ São Cada um independentemente H, C(OR¬ j¬<39>) ou um grupo hidrocarbila opcionalmente substituído por um ou mais grupos R¬ 6¬; R¬ 2¬, R¬ 3¬ e R¬ 4¬ São cada um independentemente H, alquila ou alquenila, cada um dos quais pode ser opcionalmente substituído por um ou mais grupos R¬ 7¬; R¬ 6¬ e R¬ 7¬ São cada um independentemente halogênio, NO~ 2~, CN, (CH~ 2~)~ m~OR¬ a¬, O(CH~ 2~)~ n~OR¬ b¬ (CH~ 2~)~ p~NR¬ c¬R¬ d¬, CF~ 3~, COOR¬ e¬CONR¬ f¬R¬ g¬, COR¬ h¬, SO~ 3~H, SO~ 2~R¬ i¬, SO~ 2~NR¬ j¬R¬ k¬, (CH~ 2~)~ q~NR¬ a¬<39>COR¬ g¬<39>, R¬ f¬, (CH~ 2~)~ r~NR¬ b¬<39>SO~ 2~R¬ h¬<39>, SO~ 2~NR¬ d¬<39>R¬ i¬<39>, SO~ 2~NR¬ e¬ <39>(CH~ 2~)~ s~OR¬ c¬<39>, heterociclila ou heteroarila, em que o dito heterociclila e heteroarila podem ser opcionalmente substituídos por um ou mais substituintes selecionados de aralquila, sulfonila, R¬ m¬ e COR¬ n¬; R¬ g¬<39>, R¬ h¬<39>, R¬ i¬<39> e R¬ j¬<39> são cada um independentemente selecionados de alquila, arila, aralquila e heteroarila, cada um dos quais pode ser opcionalmente substituído por um ou mais substituintes selecionados de halogênio, OH, NO~ 2~, NH~ 2~ CF~ 3~ e COOH; m, p, q e r são cada um independentemente 0, 1, 2 ou 3; n e s são cada um independentemente 1, 2 ou 3; e R¬ a-n¬ e R¬ a<39>-f¬ são cada um independentemente H ou alquila. Aspectos adicionais da invenção refere-sem a composições farmacêuticas que compreendem tais compostos e o seu uso na preparação de um medicamento para o tratamento de um ou mais dos seguintes: um distúrbio proliferativo, um distúrbio viral, um distúrbio do SNC, um derrame, alopecia e diabete.
BRPI0415759-1A 2003-10-21 2004-10-21 compostos de pirimidin-4-il-3,4-tiona e uso dos mesmos na terapia BRPI0415759A (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0324599A GB0324599D0 (en) 2003-10-21 2003-10-21 Compound
GB0330013A GB0330013D0 (en) 2003-12-24 2003-12-24 Compound
PCT/GB2004/004465 WO2005042525A1 (en) 2003-10-21 2004-10-21 Pyrimidin-4-yl-3, 4-thione compounds and their use in therapy

Publications (1)

Publication Number Publication Date
BRPI0415759A true BRPI0415759A (pt) 2006-12-19

Family

ID=34553788

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0415759-1A BRPI0415759A (pt) 2003-10-21 2004-10-21 compostos de pirimidin-4-il-3,4-tiona e uso dos mesmos na terapia

Country Status (8)

Country Link
US (1) US7902361B2 (pt)
EP (1) EP1678171B1 (pt)
JP (1) JP5164380B2 (pt)
AU (1) AU2004285745A1 (pt)
BR (1) BRPI0415759A (pt)
CA (1) CA2542880A1 (pt)
IL (1) IL174994A0 (pt)
WO (1) WO2005042525A1 (pt)

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GB0012528D0 (en) * 2000-05-23 2000-07-12 Univ Palackeho Triterpenoid derivatives
GB0219052D0 (en) * 2002-08-15 2002-09-25 Cyclacel Ltd New puring derivatives
GB0226583D0 (en) * 2002-11-14 2002-12-18 Cyclacel Ltd Compounds
GB0226582D0 (en) * 2002-11-14 2002-12-18 Cyclacel Ltd Anti-viral compounds
GB0229581D0 (en) * 2002-12-19 2003-01-22 Cyclacel Ltd Use
GB0402653D0 (en) * 2004-02-06 2004-03-10 Cyclacel Ltd Compounds
GB0411791D0 (en) * 2004-05-26 2004-06-30 Cyclacel Ltd Compounds
CA2576159A1 (en) * 2004-08-27 2006-03-02 Cyclacel Limited Purine and pyrimidine cdk inhibitors and their use for the treatment of autoimmune diseases
DE602005023333D1 (de) 2004-10-15 2010-10-14 Takeda Pharmaceutical Kinaseinhibitoren
US20080207594A1 (en) 2005-05-04 2008-08-28 Davelogen Aktiengesellschaft Use of Gsk-3 Inhibitors for Preventing and Treating Pancreatic Autoimmune Disorders
EP2258357A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis with acetylcholinesterase inhibitor
CA2620333A1 (en) 2005-08-26 2007-03-01 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
GB0520958D0 (en) * 2005-10-14 2005-11-23 Cyclacel Ltd Compound
GB0520955D0 (en) * 2005-10-14 2005-11-23 Cyclacel Ltd Compound
CA2625153A1 (en) 2005-10-21 2007-04-26 Braincells, Inc. Modulation of neurogenesis by pde inhibition
AU2006308889A1 (en) 2005-10-31 2007-05-10 Braincells, Inc. GABA receptor mediated modulation of neurogenesis
WO2007054725A2 (en) * 2005-11-11 2007-05-18 Cyclacel Limited Combination of a cdk-inhibitor and a hdac-inhibitor
CA2628179A1 (en) 2005-11-15 2007-05-24 Vertex Pharmaceuticals Incorporated Azaindazoles useful as inhibitors of kinases
US7504513B2 (en) 2006-02-27 2009-03-17 Hoffman-La Roche Inc. Thiazolyl-benzimidazoles
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
WO2007134136A2 (en) 2006-05-09 2007-11-22 Braincells, Inc. Neurogenesis by modulating angiotensin
TW200815418A (en) * 2006-06-27 2008-04-01 Astrazeneca Ab New compounds I
TW200815417A (en) * 2006-06-27 2008-04-01 Astrazeneca Ab New compounds II
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
GEP20135728B (en) 2006-10-09 2013-01-25 Takeda Pharmaceuticals Co Kinase inhibitors
GB0805477D0 (en) * 2008-03-26 2008-04-30 Univ Nottingham Pyrimidines triazines and their use as pharmaceutical agents
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
EP2379543A2 (en) 2008-12-18 2011-10-26 F. Hoffmann-La Roche AG Thiazolyl-benzimidazoles
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
WO2013059634A1 (en) 2011-10-20 2013-04-25 The Regents Of The University Of California Use of cdk9 inhibitors to reduce cartilage degradation
WO2014069434A1 (ja) * 2012-10-30 2014-05-08 カルナバイオサイエンス株式会社 新規チアゾリジノン誘導体
EP3206749B1 (en) 2014-10-14 2021-09-08 The Regents of the University of California The cdk9 and brd4 inhibitors flavopiridol and jq1 to inhibit cartilage inflammation
CA2994023A1 (en) * 2015-08-04 2017-02-02 University Of South Australia N-(pyridin-2-yl)-4-(thiazol-5-yl)pyrimidin-2-amine derivatives as therapeutic compounds
WO2018005863A1 (en) 2016-07-01 2018-01-04 G1 Therapeutics, Inc. Pyrimidine-based compounds for the treatment of cancer
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 inhibitors

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GB9519275D0 (en) 1995-09-21 1995-11-22 Univ Dundee Substances and their therapeutic use
GB9523675D0 (en) * 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
JP4205165B2 (ja) 1996-05-08 2009-01-07 サイクラセル リミテッド Cdk4活性の阻害のための方法と手段
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ATE349443T1 (de) * 2001-09-28 2007-01-15 Cyclacel Ltd N-(4-(4-methylthiazol-5-yl)pyrimidin-2-yl)-n- phenylamine als antiproliferative verbindungen
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GB0226582D0 (en) * 2002-11-14 2002-12-18 Cyclacel Ltd Anti-viral compounds
GB0226583D0 (en) * 2002-11-14 2002-12-18 Cyclacel Ltd Compounds
GB0229581D0 (en) * 2002-12-19 2003-01-22 Cyclacel Ltd Use

Also Published As

Publication number Publication date
IL174994A0 (en) 2006-08-20
EP1678171B1 (en) 2016-09-14
US20070021452A1 (en) 2007-01-25
US7902361B2 (en) 2011-03-08
EP1678171A1 (en) 2006-07-12
AU2004285745A1 (en) 2005-05-12
JP5164380B2 (ja) 2013-03-21
CA2542880A1 (en) 2005-05-12
WO2005042525A1 (en) 2005-05-12
JP2007509117A (ja) 2007-04-12

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