CN102458407B - 用作单酰甘油脂肪酶抑制剂的杂芳族和芳族哌嗪基氮杂环丁基酰胺 - Google Patents

用作单酰甘油脂肪酶抑制剂的杂芳族和芳族哌嗪基氮杂环丁基酰胺 Download PDF

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Publication number
CN102458407B
CN102458407B CN201080028761.8A CN201080028761A CN102458407B CN 102458407 B CN102458407 B CN 102458407B CN 201080028761 A CN201080028761 A CN 201080028761A CN 102458407 B CN102458407 B CN 102458407B
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China
Prior art keywords
compound
disease
methyl
phenyl
isobutyl group
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CN201080028761.8A
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Chinese (zh)
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CN102458407A (zh
Inventor
C·M·弗罗尔斯
M·I·内伦
E·L·努尔顿
S·普罗蒂
M·托德
S-P·张
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Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/06Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2121/00Preparations for use in therapy

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201080028761.8A 2009-04-22 2010-04-22 用作单酰甘油脂肪酶抑制剂的杂芳族和芳族哌嗪基氮杂环丁基酰胺 Expired - Fee Related CN102458407B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US17166109P 2009-04-22 2009-04-22
US61/171661 2009-04-22
US61/171,661 2009-04-22
PCT/US2010/032100 WO2010124122A1 (en) 2009-04-22 2010-04-22 Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors

Publications (2)

Publication Number Publication Date
CN102458407A CN102458407A (zh) 2012-05-16
CN102458407B true CN102458407B (zh) 2014-03-05

Family

ID=42226535

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201080028761.8A Expired - Fee Related CN102458407B (zh) 2009-04-22 2010-04-22 用作单酰甘油脂肪酶抑制剂的杂芳族和芳族哌嗪基氮杂环丁基酰胺

Country Status (11)

Country Link
EP (1) EP2421535A1 (de)
JP (1) JP2012524810A (de)
KR (1) KR20120005517A (de)
CN (1) CN102458407B (de)
AU (1) AU2010238746B2 (de)
BR (1) BRPI1014874A2 (de)
CA (1) CA2759706A1 (de)
IL (1) IL215797A0 (de)
RU (1) RU2011147201A (de)
TW (1) TW201103914A (de)
WO (1) WO2010124122A1 (de)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2849782A1 (en) * 2011-09-30 2013-04-04 Janssen Pharmaceutica Nv Monoacylglycerol lipase inhibitors for the treatment of metabolic diseases and related disorders
WO2014100834A1 (en) * 2012-12-21 2014-06-26 The Regents Of The University Of California Methods and compositions for treatment of cyanide and hydrogen sulfide toxicity
EP3087067B1 (de) 2013-12-26 2018-10-24 Takeda Pharmaceutical Company Limited 4-(piperrazin-1-yl)-pyrrolidin-2-on-verbindungen als monoacylglycerinlipase(magl)inhibitoren
EP3279191B1 (de) 2015-03-30 2020-09-02 Takeda Pharmaceutical Company Limited Heterocyclische verbindung
US10463753B2 (en) 2016-02-19 2019-11-05 Lundbeck La Jolla Research Center, Inc. Radiolabeled monoacylglycerol lipase occupancy probe
US10610520B2 (en) 2016-03-31 2020-04-07 Takeda Pharmaceutical Company Limited Heterocyclic compound
US10323026B2 (en) 2016-03-31 2019-06-18 Takeda Pharmaceutical Company Limited Heterocyclic compound
MX2020007318A (es) 2017-09-29 2020-08-24 Takeda Pharmaceuticals Co Compuesto heterociclico.
TW201936602A (zh) 2017-11-28 2019-09-16 瑞士商赫孚孟拉羅股份公司 新雜環化合物
TW201930300A (zh) * 2017-12-15 2019-08-01 瑞士商赫孚孟拉羅股份公司 新雜環化合物
EA202190886A1 (ru) * 2018-09-28 2021-09-07 Янссен Фармацевтика Нв Модуляторы моноацилглицерин-липазы

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2915199B1 (fr) * 2007-04-18 2010-01-22 Sanofi Aventis Derives de triazolopyridine-carboxamides et triazolopyrimidine-carboxamides, leur preparation et leur application en therapeutique.
EP2180048B1 (de) * 2008-10-09 2014-12-17 Janssen Pharmaceutica N.V. Alternative Kristallform von Monoacylglycerinlipase (MGLL)

Also Published As

Publication number Publication date
RU2011147201A (ru) 2013-05-27
AU2010238746B2 (en) 2015-02-19
CN102458407A (zh) 2012-05-16
TW201103914A (en) 2011-02-01
AU2010238746A1 (en) 2011-11-10
EP2421535A1 (de) 2012-02-29
CA2759706A1 (en) 2010-10-28
KR20120005517A (ko) 2012-01-16
IL215797A0 (en) 2012-01-31
WO2010124122A1 (en) 2010-10-28
JP2012524810A (ja) 2012-10-18
BRPI1014874A2 (pt) 2016-04-12

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