CN100379737C - 作为髓过氧化物酶抑制剂的硫代黄嘌呤衍生物 - Google Patents

作为髓过氧化物酶抑制剂的硫代黄嘌呤衍生物 Download PDF

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Publication number
CN100379737C
CN100379737C CNB038083558A CN03808355A CN100379737C CN 100379737 C CN100379737 C CN 100379737C CN B038083558 A CNB038083558 A CN B038083558A CN 03808355 A CN03808355 A CN 03808355A CN 100379737 C CN100379737 C CN 100379737C
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China
Prior art keywords
thioxanthine
methyl
compound
isobutyl
nmr
Prior art date
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Expired - Fee Related
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CNB038083558A
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English (en)
Chinese (zh)
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CN1646531A (zh
Inventor
S·汉松
G·诺德瓦尔
A·-K·蒂登
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AstraZeneca AB
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AstraZeneca AB
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Priority claimed from SE0201193A external-priority patent/SE0201193D0/xx
Priority claimed from SE0202239A external-priority patent/SE0202239D0/xx
Application filed by AstraZeneca AB filed Critical AstraZeneca AB
Publication of CN1646531A publication Critical patent/CN1646531A/zh
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    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/20—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two sulfur 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • 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
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
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    • A—HUMAN NECESSITIES
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    • 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
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    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P27/16—Otologicals
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/22—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one sulfur atom

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
CNB038083558A 2002-04-19 2003-04-15 作为髓过氧化物酶抑制剂的硫代黄嘌呤衍生物 Expired - Fee Related CN100379737C (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
SE0201193A SE0201193D0 (sv) 2002-04-19 2002-04-19 Novel use
SE02011930 2002-04-19
SE02022390 2002-07-17
SE0202239A SE0202239D0 (sv) 2002-07-17 2002-07-17 Novel use

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN2007101082174A Division CN101062037B (zh) 2002-04-19 2003-04-15 作为髓过氧化物酶抑制剂的硫代黄嘌呤衍生物的制法及其应用

Publications (2)

Publication Number Publication Date
CN1646531A CN1646531A (zh) 2005-07-27
CN100379737C true CN100379737C (zh) 2008-04-09

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CNB038083558A Expired - Fee Related CN100379737C (zh) 2002-04-19 2003-04-15 作为髓过氧化物酶抑制剂的硫代黄嘌呤衍生物

Country Status (21)

Country Link
US (2) US7425560B2 (enExample)
EP (2) EP2332541A1 (enExample)
JP (2) JP4649112B2 (enExample)
KR (3) KR101064092B1 (enExample)
CN (1) CN100379737C (enExample)
AR (1) AR039385A1 (enExample)
AT (1) ATE529428T1 (enExample)
AU (2) AU2003224548B2 (enExample)
BR (1) BR0309012A (enExample)
CA (2) CA2480452C (enExample)
ES (1) ES2373224T3 (enExample)
IL (1) IL164315A0 (enExample)
IS (1) IS7509A (enExample)
MX (1) MXPA04010055A (enExample)
MY (1) MY157949A (enExample)
NO (2) NO331002B1 (enExample)
NZ (1) NZ535406A (enExample)
PL (1) PL373197A1 (enExample)
RU (2) RU2323219C2 (enExample)
TW (1) TWI335918B (enExample)
WO (1) WO2003089430A1 (enExample)

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SE0302756D0 (sv) * 2003-10-17 2003-10-17 Astrazeneca Ab Novel Compounds
SE0402591D0 (sv) * 2004-10-25 2004-10-25 Astrazeneca Ab Novel use
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TW200806667A (en) * 2006-04-13 2008-02-01 Astrazeneca Ab New compounds
CN101472926A (zh) * 2006-04-13 2009-07-01 阿斯利康(瑞典)有限公司 硫代黄嘌呤衍生物以及它们作为髓过氧化物酶抑制剂的用途
EP2029603A1 (en) * 2006-06-05 2009-03-04 Astra Zeneca AB Pyrrolo[3,2-d]pyrimidin-4-one derivative as myeloperoxidase inhibitor
TW200804383A (en) 2006-06-05 2008-01-16 Astrazeneca Ab New compounds
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US20090054468A1 (en) * 2007-08-23 2009-02-26 Astrazeneca Ab New Use 938
US20090053176A1 (en) * 2007-08-23 2009-02-26 Astrazeneca Ab New Combination 937
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AU2010251930A1 (en) * 2009-05-27 2011-11-24 Universite Libre De Bruxelles 3-alkyl-5-fluoroindole derivatives as myeloperoxidase inhibitors
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WO2011133581A1 (en) 2010-04-19 2011-10-27 General Atomics Methods and compositions for assaying enzymatic activity of myeloperoxidase in blood samples
GB201021979D0 (en) 2010-12-23 2011-02-02 Astrazeneca Ab New compound
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US9616063B2 (en) 2014-12-01 2017-04-11 Astrazeneca Ab 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-ones as inhibitors of myeloperoxidase
CR20170498A (es) 2015-05-05 2018-01-26 Pfizer 2-tiopirimidinonas
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WO2020021300A1 (en) 2018-07-24 2020-01-30 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of myeloperoxidase (mpo) inhibitors for the treatment of chemoresistant acute myeloid leukemia (aml)
WO2021013942A1 (en) 2019-07-24 2021-01-28 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of myeloperoxidase inhibitors for the treatment of cardiovascular diseases in patients suffering from myeloproliferative neoplasms
JP2025528217A (ja) 2022-08-18 2025-08-26 アストラゼネカ・アクチエボラーグ ミエロペルオキシダーゼの阻害剤
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WO2025190901A1 (en) 2024-03-13 2025-09-18 Institut National de la Santé et de la Recherche Médicale Use of myeloperoxidase (mpo) inhibitors for promoting cd8+ t cell responses

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