CN103153999B - 作为大麻素受体-1抑制剂的化合物 - Google Patents

作为大麻素受体-1抑制剂的化合物 Download PDF

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Publication number
CN103153999B
CN103153999B CN201180049022.1A CN201180049022A CN103153999B CN 103153999 B CN103153999 B CN 103153999B CN 201180049022 A CN201180049022 A CN 201180049022A CN 103153999 B CN103153999 B CN 103153999B
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base
pyrimidine
methanol
pyrrolidin
methyl
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Chinese (zh)
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CN103153999A (zh
Inventor
申松锡
洪勇德
卞庚姬
朴美渶
崔镇圭
朴俍姬
裵日弘
朱泳协
林庆珉
朴永镐
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Amorepacific Corp
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Amorepacific Corp
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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
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
  • Epidemiology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN201180049022.1A 2010-08-31 2011-08-31 作为大麻素受体-1抑制剂的化合物 Expired - Fee Related CN103153999B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
KR20100085042 2010-08-31
KR10-2010-0085042 2010-08-31
PCT/KR2011/006474 WO2012030170A2 (ko) 2010-08-31 2011-08-31 카나비노이드 1 수용체 저해제로 작용하는 신규 화합물

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CN103153999A CN103153999A (zh) 2013-06-12
CN103153999B true CN103153999B (zh) 2016-06-01

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Country Link
US (1) US8975264B2 (https=)
EP (1) EP2617723A4 (https=)
JP (1) JP5859544B2 (https=)
KR (1) KR101914161B1 (https=)
CN (1) CN103153999B (https=)
WO (1) WO2012030170A2 (https=)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2020531519A (ja) 2017-08-21 2020-11-05 ナビゲン，インコーポレーテッド Ａｒｆ６阻害剤及び関連する方法
CN109856394B (zh) * 2019-04-16 2022-04-19 浙江诺迦生物科技有限公司 一种基于细胞多巴胺释放效应的大麻素类活性物质的检测方法及其检测试剂盒
WO2020232350A1 (en) * 2019-05-15 2020-11-19 The Regents Of The University Of Colorado, A Body Corporate Assays for synthetic cannabinoids
CN112007156A (zh) * 2019-05-30 2020-12-01 复旦大学 大麻素受体药物在制备治疗心肌细胞坏死性凋亡药剂中的应用
CN112755189A (zh) * 2019-11-02 2021-05-07 复旦大学 1型大麻素受体拮抗剂在制备治疗心肌细胞焦亡药剂中的应用
TWI907472B (zh) * 2020-08-05 2025-12-11 匈牙利商羅特格登公司 具藥理活性之經雜環取代的吡唑并〔１，５－ａ〕嘧啶衍生物
KR102912267B1 (ko) * 2023-04-20 2026-01-15 한국화학연구원 신규한 헤테로고리 화합물 또는 이의 약학적으로 허용가능한 염 및 이를 유효성분으로 포함하는 바이러스성 질환의 예방 또는 치료용 약학적 조성물

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004069838A1 (en) * 2003-02-10 2004-08-19 Pfizer Products Inc. Cannabinoid receptor ligands and uses thereof
WO2008004698A2 (en) * 2006-07-05 2008-01-10 Mitsubishi Tanabe Pharma Corporation Pyrazolo [1, 5-a] pyrimidine compounds as cb1 receptor antagonist
CN101671336A (zh) * 2009-09-23 2010-03-17 辽宁利锋科技开发有限公司 芳杂环并嘧啶衍生物和类似物及其制备方法和用途

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0515026D0 (en) * 2005-07-21 2005-08-31 Novartis Ag Organic compounds
TW201345908A (zh) * 2006-07-05 2013-11-16 Mitsubishi Tanabe Pharma Corp 吡唑并〔１，５-ａ〕嘧啶化合物

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004069838A1 (en) * 2003-02-10 2004-08-19 Pfizer Products Inc. Cannabinoid receptor ligands and uses thereof
WO2008004698A2 (en) * 2006-07-05 2008-01-10 Mitsubishi Tanabe Pharma Corporation Pyrazolo [1, 5-a] pyrimidine compounds as cb1 receptor antagonist
CN101671336A (zh) * 2009-09-23 2010-03-17 辽宁利锋科技开发有限公司 芳杂环并嘧啶衍生物和类似物及其制备方法和用途

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
AM630, A COMPETITIVE CANNABINOID RECEPTOR ANTAGONIST;Roger Pertwee，等;《Life Sciences》;19951231;第56卷(第23/24期);第1949-1955页 *
BIOCHEMICAL AND PHARMACOLOGICAL CHARACTERISATION OF SR141716A, THE FIRST POTENT AND SELECTIVE BRAIN CANNABINOID RECEPTOR ANTAGONIST;Murielle Rinaldi-Carmona，等;《Life Sciences》;19951231;第56卷(第23/24期);第1941-1947页 *
Evaluation of Cannabinoid Receptor Agonists and Antagonists Using the Guanosine-59-O-(3-[35S]thio)-triphosphate Binding Assay in Rat Cerebellar Membranes;GRAEME GRIFFIN，等;《THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS》;19980120;第285卷(第2期);第553-560页 *
Fluoro-containing Heterocycles: V.* Cyclization of 3-Azolylamino-2-polyfluorobenzoylacrylates;G.N.Lipunova，等;《Russian Journal of Organic Chemistry》;20011231;第37卷(第4期);第570-576页 *
Synthesis of Pyrazolo[1,5-a]-, 1,2,4-Triazolo[1,5-a]- and Imidazo[1,2-a]pyrimidines Related to Zaleplon, a New Drug for the Treatment of Insomnia;Carlo Mustazza，等;《J. Heterocyclic Chem.》;20011031;第38卷(第5期);第1119-1129页 *

Also Published As

Publication number Publication date
KR20130099930A (ko) 2013-09-06
EP2617723A2 (en) 2013-07-24
EP2617723A4 (en) 2014-07-02
CN103153999A (zh) 2013-06-12
KR101914161B1 (ko) 2018-11-02
JP5859544B2 (ja) 2016-02-10
US20130158025A1 (en) 2013-06-20
WO2012030170A2 (ko) 2012-03-08
JP2013536836A (ja) 2013-09-26
WO2012030170A3 (ko) 2012-06-28
US8975264B2 (en) 2015-03-10

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