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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Expired - Fee Related
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CN201080028761.8A
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English (en)
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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    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2121/00—Preparations for use in therapy
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 (fr) 2009-04-22 2010-04-22 Pipérazinyl azétidinyl amides hétéroaromatiques et aromatiques en tant qu'inhibiteurs de la monoacylglycérol lipase

Publications (2)

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

Family

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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 (fr)
JP (1) JP2012524810A (fr)
KR (1) KR20120005517A (fr)
CN (1) CN102458407B (fr)
AU (1) AU2010238746B2 (fr)
BR (1) BRPI1014874A2 (fr)
CA (1) CA2759706A1 (fr)
IL (1) IL215797A0 (fr)
RU (1) RU2011147201A (fr)
TW (1) TW201103914A (fr)
WO (1) WO2010124122A1 (fr)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2760450A1 (fr) * 2011-09-30 2014-08-06 Janssen Pharmaceutica, N.V. Inhibiteurs de monoacylglycérol lipase pour le traitement de maladies métaboliques et de troubles apparentés
EP2935294A4 (fr) 2012-12-21 2016-08-31 Univ California Méthodes et compositions pour le traitement de la toxicité du cyanure et de sulfure d'hydrogène
JP6454349B2 (ja) * 2013-12-26 2019-01-16 武田薬品工業株式会社 モノアシルグリセロールリパーゼ（ｍａｇｌ）阻害剤としての４−（ピペラジン−１−イル）−ピロリジン−２−オン化合物
WO2016158956A1 (fr) * 2015-03-30 2016-10-06 武田薬品工業株式会社 Composé hétérocyclique
US10463753B2 (en) 2016-02-19 2019-11-05 Lundbeck La Jolla Research Center, Inc. Radiolabeled monoacylglycerol lipase occupancy probe
BR112018068538B1 (pt) 2016-03-31 2023-12-12 Takeda Pharmaceutical Company Limited Composto, medicamento, e, uso de um composto
WO2017170830A1 (fr) 2016-03-31 2017-10-05 武田薬品工業株式会社 Composé hétérocyclique
MX2020007318A (es) 2017-09-29 2020-08-24 Takeda Pharmaceuticals Co Compuesto heterociclico.
EP3717477B1 (fr) 2017-11-28 2022-07-20 F. Hoffmann-La Roche AG Nouveaux composés hétérocycliques
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
EP3856178A1 (fr) * 2018-09-28 2021-08-04 Janssen Pharmaceutica NV Modulateurs de la monoacylglycérol lipase

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 (fr) * 2008-10-09 2014-12-17 Janssen Pharmaceutica N.V. Forme cristalline alternative de la monoacylglycérol lipase (MGLL)

Also Published As

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

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