CN110248947B - Magl抑制剂 - Google Patents

Magl抑制剂 Download PDF

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Publication number
CN110248947B
CN110248947B CN201780083635.4A CN201780083635A CN110248947B CN 110248947 B CN110248947 B CN 110248947B CN 201780083635 A CN201780083635 A CN 201780083635A CN 110248947 B CN110248947 B CN 110248947B
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China
Prior art keywords
pharmaceutically acceptable
acceptable salt
formula
solvate
compounds
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Expired - Fee Related
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CN201780083635.4A
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English (en)
Chinese (zh)
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CN110248947A (zh
Inventor
谢丽尔·A·格莱斯
丹尼尔·J·布扎德
尼科尔·S·怀特
唐纳德·L·赫佐格
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H Lundbeck AS
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H Lundbeck AS
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Expired - Fee Related legal-status Critical Current
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
    • C07D295/205—Radicals derived from carbonic acid
    • 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 or sparfloxacin
    • 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
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201780083635.4A 2016-11-16 2017-11-15 Magl抑制剂 Expired - Fee Related CN110248947B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662423095P 2016-11-16 2016-11-16
US62/423,095 2016-11-16
PCT/US2017/061867 WO2018093946A1 (en) 2016-11-16 2017-11-15 Magl inhibitors

Publications (2)

Publication Number Publication Date
CN110248947A CN110248947A (zh) 2019-09-17
CN110248947B true CN110248947B (zh) 2022-04-01

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CN201780083635.4A Expired - Fee Related CN110248947B (zh) 2016-11-16 2017-11-15 Magl抑制剂

Country Status (27)

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US (1) US9981930B1 (enExample)
EP (1) EP3541822B1 (enExample)
JP (1) JP6987859B2 (enExample)
KR (1) KR20190077087A (enExample)
CN (1) CN110248947B (enExample)
AR (1) AR110088A1 (enExample)
AU (1) AU2017361250A1 (enExample)
BR (1) BR112019009991A2 (enExample)
CA (1) CA3043612A1 (enExample)
CL (1) CL2019001335A1 (enExample)
CO (1) CO2019005038A2 (enExample)
CR (1) CR20190243A (enExample)
DO (1) DOP2019000121A (enExample)
EA (1) EA201991074A1 (enExample)
EC (1) ECSP19035377A (enExample)
ES (1) ES2908632T3 (enExample)
IL (1) IL266550A (enExample)
JO (1) JOP20190105A1 (enExample)
MA (1) MA46860A (enExample)
MX (1) MX2019005771A (enExample)
NI (1) NI201900050A (enExample)
PE (1) PE20191146A1 (enExample)
PH (1) PH12019501102A1 (enExample)
RU (1) RU2019116514A (enExample)
TN (1) TN2019000150A1 (enExample)
TW (1) TW201831458A (enExample)
WO (1) WO2018093946A1 (enExample)

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US10899737B2 (en) 2016-09-19 2021-01-26 Lundbeck La Jolla Research Center, Inc. Piperazine carbamates and methods of making and using same
JOP20190106A1 (ar) * 2016-11-16 2019-05-09 Lundbeck La Jolla Research Center Inc مثبطات أحادي أسيل جليسرول ليباز (magl)
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AU2017361254B2 (en) 2016-11-16 2021-09-23 H. Lundbeck A/S. Pharmaceutical formulations
KR102508739B1 (ko) 2016-11-16 2023-03-09 하. 룬드벡 아크티에셀스카브 Magl 억제제의 결정형
PE20200664A1 (es) 2017-08-29 2020-06-11 Lundbeck La Jolla Research Center Inc Compuestos espirociclicos y sus metodos de preparacion y uso
CN111448199A (zh) * 2017-11-02 2020-07-24 艾库里斯有限及两合公司 具有抗乙型肝炎病毒(hbv)活性的新的高活性的氨基-噻唑取代的吲哚-2-甲酰胺
TW201946906A (zh) 2018-05-15 2019-12-16 美商阿拜德生物製藥公司 Magl抑制劑
US11702393B2 (en) * 2020-04-21 2023-07-18 H. Lundbeck A/S Synthesis of a monoacylglycerol lipase inhibitor
UY39516A (es) 2020-11-13 2022-05-31 H Lundbeck As Composición para el tratamiento de una enfermedad vascular, composición para la prevención de una enfermedad vascular, composición para el tratamiento de la hipertensión, y composición para la prevención de la hipertensión
JP7777891B2 (ja) 2021-12-29 2025-12-01 サイ セラピューティクス インコーポレイテッド モノアシルグリセロールリパーゼ（ｍａｇｌ）の阻害
KR20250005229A (ko) 2022-05-04 2025-01-09 하. 룬드벡 아크티에셀스카브 모노아실글리세롤 리파제 억제제로서 1,1,1,3,3,3-헥사플루오로프로판-2-일 (s)-1-(피리다진-3-일카르바모일)-6 아자스피로[2.5]옥탄-6-카르복실레이트의 결정질 형태

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CR20190243A (es) 2019-06-26
ES2908632T3 (es) 2022-05-03
CO2019005038A2 (es) 2019-05-31
TN2019000150A1 (en) 2020-10-05
RU2019116514A (ru) 2020-12-17
EP3541822A1 (en) 2019-09-25
US9981930B1 (en) 2018-05-29
IL266550A (en) 2019-07-31
AR110088A1 (es) 2019-02-20
MX2019005771A (es) 2019-12-05
ECSP19035377A (es) 2019-05-31
NI201900050A (es) 2019-10-30
BR112019009991A2 (pt) 2019-08-27
JP2020502047A (ja) 2020-01-23
CN110248947A (zh) 2019-09-17
CA3043612A1 (en) 2018-05-24
AU2017361250A1 (en) 2019-05-30
JP6987859B2 (ja) 2022-01-05
MA46860A (fr) 2019-09-25
EP3541822B1 (en) 2022-01-19
CL2019001335A1 (es) 2019-10-04
DOP2019000121A (es) 2019-09-30
WO2018093946A1 (en) 2018-05-24
KR20190077087A (ko) 2019-07-02
US20180134675A1 (en) 2018-05-17
EA201991074A1 (ru) 2019-12-30
JOP20190105A1 (ar) 2019-05-09
EP3541822A4 (en) 2020-04-29
PH12019501102A1 (en) 2019-08-19
TW201831458A (zh) 2018-09-01
PE20191146A1 (es) 2019-09-02

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