CN106660968B - 吡唑衍生物及其作为大麻素受体介体的用途 - Google Patents

吡唑衍生物及其作为大麻素受体介体的用途 Download PDF

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CN106660968B
CN106660968B CN201580028788.XA CN201580028788A CN106660968B CN 106660968 B CN106660968 B CN 106660968B CN 201580028788 A CN201580028788 A CN 201580028788A CN 106660968 B CN106660968 B CN 106660968B
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CN106660968A (zh
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G·库诺斯
M·艾耶
R·西纳
K·C·赖斯
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    • 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
    • C07D231/06—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric 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
    • A61P3/04—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
    • 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
    • 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
    • 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings

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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)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201580028788.XA 2014-05-09 2015-05-08 吡唑衍生物及其作为大麻素受体介体的用途 Active CN106660968B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461991333P 2014-05-09 2014-05-09
US61/991,333 2014-05-09
PCT/US2015/029946 WO2015172059A1 (en) 2014-05-09 2015-05-08 Pyrazole derivatives and their use as cannabinoid receptor mediators

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CN106660968A CN106660968A (zh) 2017-05-10
CN106660968B true CN106660968B (zh) 2020-02-07

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US (1) US10329259B2 (enExample)
EP (1) EP3140288B1 (enExample)
JP (1) JP6762930B2 (enExample)
CN (1) CN106660968B (enExample)
AU (2) AU2015255765A1 (enExample)
CA (1) CA2948349C (enExample)
WO (1) WO2015172059A1 (enExample)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11155521B2 (en) 2012-11-13 2021-10-26 The United States Of America As Represented By The Secretary, Department Of Health And Human Services Cannabinoid receptor mediating compounds
EP2919779B1 (en) 2012-11-13 2021-01-06 The U.S.A. as represented by the Secretary, Department of Health and Human Services Cannabinoid receptor mediating compounds
AU2015255765A1 (en) 2014-05-09 2016-11-24 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Pyrazole derivatives and their use as cannabinoid receptor mediators
CN112511569B (zh) * 2021-02-07 2021-05-11 杭州筋斗腾云科技有限公司 网络资源访问请求的处理方法、系统及计算机设备
WO2025040089A1 (zh) * 2023-08-21 2025-02-27 德睿智药(苏州)新药研发有限公司 用于选择性调节大麻素cb1功能的新型杂环类化合物

Citations (6)

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CN1419546A (zh) * 2000-03-23 2003-05-21 索尔瓦药物有限公司 具有cb1－拮抗活性的4,5－二氢－1h－吡唑衍生物
CN1529595A (zh) * 2001-09-21 2004-09-15 ������ҩ�����޹�˾ 具有效cb1-拮抗活性的4,5-2氢-1h-吡唑衍生物
CN1555262A (zh) * 2001-09-21 2004-12-15 ������ҩ�����޹�˾ 具有cb1－拮抗活性的新的4,5－二氢－1h－吡唑衍生物
CN101823999A (zh) * 2004-01-30 2010-09-08 索尔瓦药物有限公司 具有cb1-拮抗活性的1，3，5-三取代的4，5-二氢-1h-吡唑衍生物
WO2011044370A1 (en) * 2009-10-07 2011-04-14 Jenrin Discovery Cannabinoid receptor antagonists/inverse agonists useful for treating metabolic disorders, including obesity and diabetes
CN103547263A (zh) * 2010-11-18 2014-01-29 詹里恩探索公司 对于治疗代谢性疾病，包括肥胖症和糖尿病有用的大麻素受体拮抗剂/反相激动剂

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US4675189A (en) 1980-11-18 1987-06-23 Syntex (U.S.A.) Inc. Microencapsulation of water soluble active polypeptides
JPS60100516A (ja) 1983-11-04 1985-06-04 Takeda Chem Ind Ltd 徐放型マイクロカプセルの製造法
CA1256638A (en) 1984-07-06 1989-06-27 Motoaki Tanaka Polymer and its production
JP2551756B2 (ja) 1985-05-07 1996-11-06 武田薬品工業株式会社 ポリオキシカルボン酸エステルおよびその製造法
IL153508A (en) 2001-03-22 2008-07-08 Solvay Pharm Bv Derivatives of 4,5 - Dihydro-1H-pyrazole with antagonistic activity to the 1CB receptor
US20050239859A2 (en) 2003-09-03 2005-10-27 Solvay Pharmaceuticals Gmbh Novel medical uses of 4,5-dihydro-1h-pyrazole derivatives having cb1- antagonistic activity
EP1713475B1 (en) * 2004-01-30 2008-07-30 Solvay Pharmaceuticals B.V. 1,3,5-trisubstituted 4,5-dihydro-1h-pyrazole derivatives having cb1-antagonistic activity
EP1574211A1 (en) 2004-03-09 2005-09-14 Inserm Use of antagonists of the CB1 receptor for the manufacture of a composition useful for the treatment of hepatic diseases
WO2006060192A2 (en) 2004-11-30 2006-06-08 Bayer Pharmaceuticals Corporation Pyrazole derivatives
PL1902034T3 (pl) * 2005-06-02 2011-09-30 Glenmark Pharmaceuticals Sa Nowe ligandy receptorów kanabinoidowych, kompozycja farmaceutyczna je zawierająca oraz proces ich wytwarzania
CA2651385C (en) 2006-05-05 2015-02-03 John F. Mcelroy Cannabinoid receptor antagonists/inverse agonists useful for treating metabolic disorders, including obesity and diabetes
AU2007336219A1 (en) * 2006-12-20 2008-06-26 Solvay Pharmaceuticals B.V. Compounds with a combination of cannabinoid-CB1 antagonism and acetylcholinesterase inhibition
US7655685B2 (en) 2007-11-02 2010-02-02 Jenrin Discovery, Inc. Cannabinoid receptor antagonists/inverse agonists useful for treating metabolic disorders, including obesity and diabetes
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AR070898A1 (es) * 2008-03-18 2010-05-12 Solvay Pharm Bv Derivados de arilsulfonil pirazolin carboxamidina como antagonistas de 5-ht6
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EP2919779B1 (en) 2012-11-13 2021-01-06 The U.S.A. as represented by the Secretary, Department of Health and Human Services Cannabinoid receptor mediating compounds
US11155521B2 (en) 2012-11-13 2021-10-26 The United States Of America As Represented By The Secretary, Department Of Health And Human Services Cannabinoid receptor mediating compounds
AU2015255765A1 (en) 2014-05-09 2016-11-24 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Pyrazole derivatives and their use as cannabinoid receptor mediators
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Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1419546A (zh) * 2000-03-23 2003-05-21 索尔瓦药物有限公司 具有cb1－拮抗活性的4,5－二氢－1h－吡唑衍生物
CN1529595A (zh) * 2001-09-21 2004-09-15 ������ҩ�����޹�˾ 具有效cb1-拮抗活性的4,5-2氢-1h-吡唑衍生物
CN1555262A (zh) * 2001-09-21 2004-12-15 ������ҩ�����޹�˾ 具有cb1－拮抗活性的新的4,5－二氢－1h－吡唑衍生物
CN101823999A (zh) * 2004-01-30 2010-09-08 索尔瓦药物有限公司 具有cb1-拮抗活性的1，3，5-三取代的4，5-二氢-1h-吡唑衍生物
WO2011044370A1 (en) * 2009-10-07 2011-04-14 Jenrin Discovery Cannabinoid receptor antagonists/inverse agonists useful for treating metabolic disorders, including obesity and diabetes
CN103547263A (zh) * 2010-11-18 2014-01-29 詹里恩探索公司 对于治疗代谢性疾病，包括肥胖症和糖尿病有用的大麻素受体拮抗剂/反相激动剂

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AU2019227889B2 (en) 2021-03-04
EP3140288A1 (en) 2017-03-15
AU2015255765A1 (en) 2016-11-24
CN106660968A (zh) 2017-05-10
WO2015172059A8 (en) 2016-10-27
HK1232213A1 (en) 2018-01-05
AU2019227889A1 (en) 2019-09-26
WO2015172059A1 (en) 2015-11-12
JP6762930B2 (ja) 2020-09-30
CA2948349C (en) 2023-03-28
EP3140288B1 (en) 2023-01-25
US10329259B2 (en) 2019-06-25
CA2948349A1 (en) 2015-11-12
US20180179163A1 (en) 2018-06-28
JP2017515899A (ja) 2017-06-15

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