CN107531721B - 用于调节法尼醇x受体的稠合的三环吡唑衍生物 - Google Patents

用于调节法尼醇x受体的稠合的三环吡唑衍生物 Download PDF

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Publication number
CN107531721B
CN107531721B CN201680023961.1A CN201680023961A CN107531721B CN 107531721 B CN107531721 B CN 107531721B CN 201680023961 A CN201680023961 A CN 201680023961A CN 107531721 B CN107531721 B CN 107531721B
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Prior art keywords
methyl
chromeno
pyrazol
chloro
carboxamido
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Expired - Fee Related
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CN201680023961.1A
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English (en)
Chinese (zh)
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CN107531721A (zh
Inventor
D·基亚内利
刘晓东
V·莫尔泰尼
J·内尔森
J·罗兰
P·V·鲁克尔
D·C·塔利
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Novartis AG
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Novartis AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • 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
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
    • 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
    • A61K31/635—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
    • 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
    • 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
    • A61P1/12—Antidiarrhoeals
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201680023961.1A 2015-04-30 2016-04-29 用于调节法尼醇x受体的稠合的三环吡唑衍生物 Expired - Fee Related CN107531721B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562154862P 2015-04-30 2015-04-30
US62/154,862 2015-04-30
PCT/IB2016/052424 WO2016174616A1 (en) 2015-04-30 2016-04-29 Fused tricyclic pyrazole derivatives useful for modulating farnesoid x receptors

Publications (2)

Publication Number Publication Date
CN107531721A CN107531721A (zh) 2018-01-02
CN107531721B true CN107531721B (zh) 2020-07-17

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CN201680023961.1A Expired - Fee Related CN107531721B (zh) 2015-04-30 2016-04-29 用于调节法尼醇x受体的稠合的三环吡唑衍生物

Country Status (6)

Country Link
US (1) US10351576B2 (enExample)
EP (1) EP3288948B1 (enExample)
JP (1) JP6691552B2 (enExample)
CN (1) CN107531721B (enExample)
ES (1) ES2770128T3 (enExample)
WO (1) WO2016174616A1 (enExample)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG11201603026PA (en) 2013-11-05 2016-05-30 Novartis Ag Compositions and methods for modulating farnesoid x receptors
TW201808283A (zh) * 2016-08-05 2018-03-16 廣東東陽光藥業有限公司 含氮三環化合物及其在藥物中的應用
JP7599014B2 (ja) * 2020-06-30 2024-12-12 オクヴィルク，ゼレン グアニル酸シクラーゼｃ（ｇｕｃｙ２ｃ）アゴニストおよび短鎖脂肪酸またはそのプロドラッグの組み合わせを含む医薬組成物

Citations (3)

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Publication number Priority date Publication date Assignee Title
CN101448791A (zh) * 2006-05-24 2009-06-03 伊莱利利公司 Fxr激动剂
WO2010049366A1 (en) * 2008-10-27 2010-05-06 Glaxo Group Limited Tricyclic compounds as glutamate receptor modulators
WO2015069666A1 (en) * 2013-11-05 2015-05-14 Irm Llc Compositions and methods for modulating farnesoid x receptors

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PT72878B (en) 1980-04-24 1983-03-29 Merck & Co Inc Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
EP0463090A1 (en) * 1989-03-09 1992-01-02 E.I. Du Pont De Nemours And Company Arthropodicidal tetrahydrobenzopyranopyrazoles
JP3006925B2 (ja) * 1990-09-14 2000-02-07 協和醗酵工業株式会社 ピラゾロキノリン誘導体
WO2004078163A2 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
US20040259887A1 (en) * 2003-06-18 2004-12-23 Pfizer Inc Cannabinoid receptor ligands and uses thereof
CA2586011C (en) * 2004-07-12 2011-07-19 Cadila Healthcare Limited Tricyclic pyrazole derivatives as cannabinoid receptor modulators
CA2603254C (en) * 2005-04-12 2013-10-29 Vicore Pharma Ab New bicyclic angiotensin ii agonists
IT1394400B1 (it) * 2009-02-25 2012-06-15 Neuroscienze Pharmaness S C Ar L Composizioni farmaceutiche
IT1393930B1 (it) * 2009-02-25 2012-05-17 Neuroscienze Pharmaness S C A R L Composti farmaceutici
IT1395724B1 (it) * 2009-02-25 2012-10-19 Neuroscienze Pharmaness S C A R L Composti farmaceutici
US8071589B2 (en) * 2009-07-31 2011-12-06 N. V. Organon Dihydrobenzoindazoles
TWI423980B (zh) * 2009-09-28 2014-01-21 Hoffmann La Roche 苯并氧氮呯ｐｉ３ｋ抑制劑化合物及使用方法
RU2663898C2 (ru) * 2013-06-24 2018-08-13 Мерк Патент Гмбх Пиразольные соединения в качестве модуляторов fshr и их применение

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101448791A (zh) * 2006-05-24 2009-06-03 伊莱利利公司 Fxr激动剂
WO2010049366A1 (en) * 2008-10-27 2010-05-06 Glaxo Group Limited Tricyclic compounds as glutamate receptor modulators
WO2015069666A1 (en) * 2013-11-05 2015-05-14 Irm Llc Compositions and methods for modulating farnesoid x receptors
CN105682656A (zh) * 2013-11-05 2016-06-15 诺华股份有限公司 调节法尼醇x受体的组合物和方法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
检索记录;吴永英;《Registry》;20071012;CAS-RN为950419-77-9、950397-44-1、950303-22-7、902854-20-0、902854-18-6、902854-16-4、902854-12-0的化合物 *

Also Published As

Publication number Publication date
EP3288948A1 (en) 2018-03-07
US10351576B2 (en) 2019-07-16
ES2770128T3 (es) 2020-06-30
US20180298018A1 (en) 2018-10-18
WO2016174616A1 (en) 2016-11-03
JP6691552B2 (ja) 2020-04-28
EP3288948B1 (en) 2019-11-20
CN107531721A (zh) 2018-01-02
JP2018519252A (ja) 2018-07-19

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