CN110198944A - 作为单酰基甘油脂肪酶抑制剂的杂环螺环化合物 - Google Patents

作为单酰基甘油脂肪酶抑制剂的杂环螺环化合物 Download PDF

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Publication number
CN110198944A
CN110198944A CN201880007992.7A CN201880007992A CN110198944A CN 110198944 A CN110198944 A CN 110198944A CN 201880007992 A CN201880007992 A CN 201880007992A CN 110198944 A CN110198944 A CN 110198944A
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formula
alkyl
group
compound
pharmaceutically acceptable
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Chinese (zh)
Inventor
M·A·布罗德尼
C·R·巴特勒
C·J·赫拉尔
L·A·麦卡利斯特
S·V·奥尼尔
P·R·费尔赫斯特
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SmithKline Beecham Ltd
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SmithKline Beecham Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/10—Spiro-condensed 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/438—The ring being spiro-condensed with carbocyclic or 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/20—Spiro-condensed ring systems
    • 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
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • 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
    • C07D493/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10—Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201880007992.7A 2017-01-23 2018-01-09 作为单酰基甘油脂肪酶抑制剂的杂环螺环化合物 Pending CN110198944A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762449242P 2017-01-23 2017-01-23
US62/449,242 2017-01-23
PCT/IB2018/050128 WO2018134698A1 (en) 2017-01-23 2018-01-09 Heterocyclic spiro compounds as magl inhibitors

Publications (1)

Publication Number Publication Date
CN110198944A true CN110198944A (zh) 2019-09-03

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CN201880007992.7A Pending CN110198944A (zh) 2017-01-23 2018-01-09 作为单酰基甘油脂肪酶抑制剂的杂环螺环化合物

Country Status (14)

Country Link
US (2) US20180208608A1 (https=)
EP (1) EP3571202B1 (https=)
JP (1) JP2020506903A (https=)
KR (1) KR20190097242A (https=)
CN (1) CN110198944A (https=)
AU (1) AU2018208848A1 (https=)
BR (1) BR112019014099A2 (https=)
CA (1) CA3050853A1 (https=)
IL (1) IL267781A (https=)
MX (1) MX2019008690A (https=)
RU (1) RU2726631C1 (https=)
SG (1) SG11201906427QA (https=)
TW (1) TWI665199B (https=)
WO (1) WO2018134698A1 (https=)

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WO2021228123A1 (zh) * 2020-05-12 2021-11-18 北京广为医药科技有限公司 调节nmda受体活性的化合物、其药物组合物及用途
WO2022135462A1 (zh) * 2020-12-22 2022-06-30 鲁南制药集团股份有限公司 Magl抑制剂的医药用途
CN115335365A (zh) * 2020-03-26 2022-11-11 詹森药业有限公司 氨基环丁烷作为单酰基甘油脂肪酶调节剂
CN116547274A (zh) * 2020-11-13 2023-08-04 H.隆德贝克有限公司 Magl抑制剂

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US10927105B1 (en) 2017-05-23 2021-02-23 Lundbeck La Jolla Research Center, Inc. Pyrazole MAGL inhibitors
BR112020005720A2 (pt) * 2017-09-29 2020-10-20 Takeda Pharmaceutical Company Limited composto ou sal, medicamento, métodos para inibir monoacilglicerol lipase e para a profilaxia ou o tratamento de doença de alzheimer, doença de parkinson, doença de huntington, esclerose lateral amiotrófica, esclerose múltipla, distúrbio de ansiedade, dor, epilepsia ou depressão, e, uso do composto ou sal.
US10662159B2 (en) * 2017-11-22 2020-05-26 Makscientific, Llc ABHD6 and dual ABHD6/MGL inhibitors and their uses
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MX2021000549A (es) * 2018-07-19 2021-03-25 Pfizer Compuestos espiro heterociclicos como inhibidores de magl.
RS67557B1 (sr) * 2018-08-24 2026-01-30 Pharmacosmos Holding As Unapređena sinteza 1,4-diazaspiro[5.5]undekan-3-ona
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WO2020065614A1 (en) 2018-09-28 2020-04-02 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators
KR20210097734A (ko) * 2018-11-28 2021-08-09 하. 룬드벡 아크티에셀스카브 Magl 저해제에 의해 질병을 치료하는 방법
CN109485656A (zh) * 2018-12-17 2019-03-19 上海药明康德新药开发有限公司 3-氧亚基-7-氧杂-2,10-二氮杂螺[4.6]十一烷-10-甲酸叔丁酯的制法
CA3125636A1 (en) * 2019-01-25 2020-07-30 H. Lundbeck A/S Methods of treating disease with magl inhibitors
BR112021026899A2 (pt) * 2019-07-09 2022-05-10 Hoffmann La Roche Compostos heterocíclicos
MX2022003819A (es) 2019-09-30 2022-05-11 Janssen Pharmaceutica Nv Ligandos de pet de mgl radiomarcados.
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