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)
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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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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/02Heterocyclic 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
    • C07D513/10Spiro-condensed systems
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/438The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53861,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D221/00Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02Heterocyclic 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
    • C07D221/20Spiro-condensed ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/10Spiro-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)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (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

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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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JP7697934B2 (ja) 2019-09-30 2025-06-24 ヤンセン ファーマシューティカ エヌ.ベー. 放射線標識されたmgl petリガンド
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JAYENDRA Z. PATEL 等: "Loratadine analogues as MAGL inhibitors", 《BIOORGANIC & MEDICINAL CHEMISTRY LETTERS》 *

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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
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
CN113966337A (zh) * 2020-05-12 2022-01-21 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
CN113966337B (zh) * 2020-05-12 2024-01-02 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
CN116547274A (zh) * 2020-11-13 2023-08-04 H.隆德贝克有限公司 Magl抑制剂
CN116547274B (zh) * 2020-11-13 2026-02-13 H.隆德贝克有限公司 Magl抑制剂
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

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US10858373B2 (en) 2020-12-08
EP3571202A1 (en) 2019-11-27
EP3571202B1 (en) 2021-06-30
BR112019014099A2 (pt) 2020-02-11
WO2018134698A1 (en) 2018-07-26
AU2018208848A1 (en) 2019-07-18
TWI665199B (zh) 2019-07-11
US20180208608A1 (en) 2018-07-26
IL267781A (en) 2019-09-26
SG11201906427QA (en) 2019-08-27
CA3050853A1 (en) 2018-07-26
MX2019008690A (es) 2019-09-18
TW201838995A (zh) 2018-11-01
KR20190097242A (ko) 2019-08-20
US20190292203A1 (en) 2019-09-26
RU2726631C1 (ru) 2020-07-15

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