ATE502037T1 - Pyrimidin-4-yl-3,4-dihydro-2h-pyrroloä1, 2aüpyrazin-1-on verbindungen - Google Patents

Pyrimidin-4-yl-3,4-dihydro-2h-pyrroloä1, 2aüpyrazin-1-on verbindungen

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Publication number
ATE502037T1
ATE502037T1 AT06794699T AT06794699T ATE502037T1 AT E502037 T1 ATE502037 T1 AT E502037T1 AT 06794699 T AT06794699 T AT 06794699T AT 06794699 T AT06794699 T AT 06794699T AT E502037 T1 ATE502037 T1 AT E502037T1
Authority
AT
Austria
Prior art keywords
alkyl
independently
compounds
aryl
formula
Prior art date
Application number
AT06794699T
Other languages
English (en)
Inventor
Stuart Jones
Bob Westwood
Mark Thomas
Janice Mclachlan
Kenneth Duncan
Fred Scaerou
Daniella Zheleva
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
Application filed by Cyclacel Ltd filed Critical Cyclacel Ltd
Application granted granted Critical
Publication of ATE502037T1 publication Critical patent/ATE502037T1/de

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P31/10—Antimycotics
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • 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
    • 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
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • AIDS & HIV (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
AT06794699T 2005-10-14 2006-10-09 Pyrimidin-4-yl-3,4-dihydro-2h-pyrroloä1, 2aüpyrazin-1-on verbindungen ATE502037T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0520958.0A GB0520958D0 (en) 2005-10-14 2005-10-14 Compound
PCT/GB2006/003748 WO2007042784A2 (en) 2005-10-14 2006-10-09 Pyrimidin-4-yl-3, 4-dihydr0-2h- pyrrolo [1, 2a] pyrazin-1-one compounds

Publications (1)

Publication Number Publication Date
ATE502037T1 true ATE502037T1 (de) 2011-04-15

Family

ID=35451786

Family Applications (1)

Application Number Title Priority Date Filing Date
AT06794699T ATE502037T1 (de) 2005-10-14 2006-10-09 Pyrimidin-4-yl-3,4-dihydro-2h-pyrroloä1, 2aüpyrazin-1-on verbindungen

Country Status (12)

Country Link
US (1) US8404692B2 (de)
EP (1) EP1940846B9 (de)
JP (1) JP5266054B2 (de)
CN (1) CN101326188B (de)
AT (1) ATE502037T1 (de)
AU (1) AU2006301031A1 (de)
BR (1) BRPI0620968A2 (de)
DE (1) DE602006020755D1 (de)
GB (1) GB0520958D0 (de)
IL (1) IL190713A0 (de)
RU (1) RU2008118894A (de)
WO (1) WO2007042784A2 (de)

Families Citing this family (20)

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US8394802B2 (en) 2008-09-19 2013-03-12 Nerviano Medical Sciences S.R.L. 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one derivatives for the modulation of the activity of protein kinases
WO2013050446A1 (en) * 2011-10-07 2013-04-11 Nerviano Medical Sciences S.R.L. SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-a]PYRAZIN-1(2H)-ONE DERIVATIVES AS KINASES INHIBITORS
ES2660265T3 (es) 2011-10-07 2018-03-21 Nerviano Medical Sciences S.R.L. Derivados de 3,4-dihidropirrolo[1,2-a]pirazin-1(2h)-ona 4-alquil-sustituidos como inhibidores de cinasa
WO2013059634A1 (en) 2011-10-20 2013-04-25 The Regents Of The University Of California Use of cdk9 inhibitors to reduce cartilage degradation
US10300073B2 (en) 2014-10-14 2019-05-28 The Regents Of The University Of California Use of CDK9 and BRD4 inhibitors to inhibit inflammation
WO2016100166A1 (en) 2014-12-15 2016-06-23 Bristol-Myers Squibb Company SUBSTITUTED DIHYDRO-1H-PYRROLO[3,2-c]PYRIDIN-4(5H)-ONES AS RIPK3 INHIBITORS
WO2016162325A1 (en) 2015-04-07 2016-10-13 Astrazeneca Ab Substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1 (2h)-one derivatives as kinase inhibitors
WO2016192063A1 (en) * 2015-06-03 2016-12-08 Changzhou Jiekai Pharmatech Co. Ltd Heterocyclic compounds as erk inhibitors
WO2016192064A1 (en) 2015-06-03 2016-12-08 Js Innopharm (Shanghai) Ltd. Heterocyclic compounds for treating psoriasis
WO2017080980A1 (en) * 2015-11-09 2017-05-18 Astrazeneca Ab Dihydropyrrolopyrazinone derivatives useful in the treatment of cancer
SMT202000152T1 (it) * 2015-11-09 2020-05-08 Astrazeneca Ab Derivati di diidroimidazopirazinone utili nel trattamento di cancro
GB201705263D0 (en) * 2017-03-31 2017-05-17 Probiodrug Ag Novel inhibitors
EP4194450A4 (de) * 2020-08-07 2024-10-30 Pharmablock Sciences (Nanjing), Inc. Cdk9-inhibitor und verwendung davon
CA3196620A1 (en) 2020-10-05 2022-04-14 Enliven Therapeutics, Inc. 5- and 6-azaindole compounds for inhibition of bcr-abl tyrosine kinases
TW202329937A (zh) 2021-12-03 2023-08-01 美商英塞特公司 雙環胺ck12抑制劑
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 inhibitors
WO2024035194A1 (ko) * 2022-08-11 2024-02-15 환인제약 주식회사 신규한 헤테로아릴 치환 유도체 및 이를 포함하는 신경퇴행성 질환, 암, 및 염증성 질환의 예방 또는 치료용 조성물
KR102651320B1 (ko) * 2022-08-11 2024-03-28 환인제약 주식회사 신규한 헤테로아릴 치환 유도체 및 이를 포함하는 신경퇴행성 질환, 암, 및 염증성 질환의 예방 또는 치료용 조성물
CN117946098A (zh) * 2022-10-28 2024-04-30 上海深势唯思科技有限责任公司 一种嘧啶类plk1抑制剂及其制备方法和用途
WO2026024674A1 (en) 2024-07-22 2026-01-29 Genesis Therapeutics, Inc. Methods of treating skp2-associated cancers

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SG47583A1 (en) 1986-01-13 1998-04-17 American Cyanamid Co 4,5,6-Substituted-n- (substituted-phenyl) -2- pyrimidinamines
US5516775A (en) 1992-08-31 1996-05-14 Ciba-Geigy Corporation Further use of pyrimidine derivatives
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GB2361236B (en) * 2000-03-29 2002-04-24 Cyclacel Ltd Pyrimidines useful against proliferative disorders
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BRPI0415759A (pt) * 2003-10-21 2006-12-19 Cyclacel Ltd compostos de pirimidin-4-il-3,4-tiona e uso dos mesmos na terapia

Also Published As

Publication number Publication date
BRPI0620968A2 (pt) 2011-11-29
US20100035870A1 (en) 2010-02-11
JP5266054B2 (ja) 2013-08-21
CN101326188B (zh) 2013-04-24
WO2007042784A2 (en) 2007-04-19
EP1940846B9 (de) 2012-09-12
EP1940846A2 (de) 2008-07-09
US8404692B2 (en) 2013-03-26
EP1940846B1 (de) 2011-03-16
JP2009511555A (ja) 2009-03-19
DE602006020755D1 (de) 2011-04-28
AU2006301031A8 (en) 2008-05-08
GB0520958D0 (en) 2005-11-23
CN101326188A (zh) 2008-12-17
WO2007042784A3 (en) 2007-06-28
IL190713A0 (en) 2008-11-03
AU2006301031A1 (en) 2007-04-19
RU2008118894A (ru) 2009-11-20

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