KR102508739B1 - Magl 억제제의 결정형 - Google Patents

Magl 억제제의 결정형 Download PDF

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KR102508739B1
KR102508739B1 KR1020197017161A KR20197017161A KR102508739B1 KR 102508739 B1 KR102508739 B1 KR 102508739B1 KR 1020197017161 A KR1020197017161 A KR 1020197017161A KR 20197017161 A KR20197017161 A KR 20197017161A KR 102508739 B1 KR102508739 B1 KR 102508739B1
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crystalline
hexafluoropropan
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KR20190077561A (ko
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셰럴 에이 그라이스
토드 케이 존스
커트 지 그림
재클린 로레인 블랭크맨
채닝 로드니 빌스
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하. 룬드벡 아크티에셀스카브
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • 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
    • 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
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • 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]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13Dicarboxylic acids
    • C07C57/15Fumaric acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/16Heterocyclic 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
    • C07D295/20Heterocyclic 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
    • C07D295/205Radicals derived from carbonic acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1020197017161A 2016-11-16 2017-11-15 Magl 억제제의 결정형 Active KR102508739B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662423126P 2016-11-16 2016-11-16
US62/423,126 2016-11-16
PCT/US2017/061875 WO2018093953A1 (en) 2016-11-16 2017-11-15 Crystalline forms of a magl inhibitor

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KR20190077561A KR20190077561A (ko) 2019-07-03
KR102508739B1 true KR102508739B1 (ko) 2023-03-09

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EP (2) EP3541807B1 (https=)
JP (2) JP7042548B2 (https=)
KR (1) KR102508739B1 (https=)
CN (2) CN115093382A (https=)
AU (1) AU2017361257B2 (https=)
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JOP20190107A1 (ar) 2016-11-16 2019-05-09 Lundbeck La Jolla Research Center Inc مثبطات أحادي أسيل جليسرول ليباز (magl)
UA124884C2 (uk) 2016-11-16 2021-12-08 Лундбек Ла Джолла Ресеарч Центер, Інк. Фармацевтичні склади
MA46866B1 (fr) 2016-11-16 2021-11-30 H Lundbeck As Une forme cristalline d'un inhibiteur de magl
US10927105B1 (en) 2017-05-23 2021-02-23 Lundbeck La Jolla Research Center, Inc. Pyrazole MAGL inhibitors
DK3630744T3 (da) 2017-05-23 2023-03-06 H Lundbeck As Pyrazol-magl-inhibitorer
JP7257387B2 (ja) 2017-08-29 2023-04-13 ハー・ルンドベック・アクチエゼルスカベット スピロ環化合物並びにその作製及び使用方法
GEP20227443B (en) 2018-05-15 2022-11-25 H Lundbeck As Magl inhibitors
MX2021000549A (es) * 2018-07-19 2021-03-25 Pfizer Compuestos espiro heterociclicos como inhibidores de magl.
ES2986417T3 (es) 2018-08-13 2024-11-11 Hoffmann La Roche Nuevos compuestos heterocíclicos como inhibidores de la monoacilglicerol lipasa
ES2955037T3 (es) 2018-11-22 2023-11-28 Hoffmann La Roche Nuevos compuestos heterocíclicos
CA3125636A1 (en) * 2019-01-25 2020-07-30 H. Lundbeck A/S Methods of treating disease with magl inhibitors
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WO2021214550A1 (en) * 2020-04-21 2021-10-28 H. Lundbeck A/S Synthesis of a monoacylglycerol lipase inhibitor
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CA3242372A1 (en) 2021-12-29 2023-07-06 Psy Therapeutics, Inc. Inhibiting monoacylglycerol lipase (magl)
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
CN117665187B (zh) * 2023-11-23 2024-08-16 宁波大红鹰药业股份有限公司 一种舒林酸中间体杂质的测定方法

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WO2018093953A1 (en) 2018-05-24
MA46866B1 (fr) 2021-11-30
EP3541807B1 (en) 2021-09-29
MX389459B (es) 2025-03-20
PT3541807T (pt) 2021-12-09
IL266548A (en) 2019-07-31
RS62665B1 (sr) 2021-12-31
CN110291083A (zh) 2019-09-27
DOP2019000120A (es) 2019-09-30
NZ753241A (en) 2021-06-25
NI201900053A (es) 2019-10-30
JP7350117B2 (ja) 2023-09-25
SMT202100675T1 (it) 2022-01-10
UA124585C2 (uk) 2021-10-13
EP3541807A4 (en) 2020-04-22
EP3964503B1 (en) 2023-11-08
KR20190077561A (ko) 2019-07-03
MX2019005767A (es) 2019-12-05
LT3541807T (lt) 2021-12-27
CN110291083B (zh) 2022-06-17
US20200190063A1 (en) 2020-06-18
MA46866A (fr) 2021-06-02
JP2019537596A (ja) 2019-12-26
CL2019001340A1 (es) 2019-10-04
ES2900016T3 (es) 2022-03-15
AU2017361257A1 (en) 2019-05-30
PL3964503T3 (pl) 2024-04-02
BR112019010003A2 (pt) 2019-08-20
CR20190242A (es) 2019-07-09
RS65016B1 (sr) 2024-01-31
CY1126586T1 (el) 2026-02-25
US11142517B2 (en) 2021-10-12
HUE056973T2 (hu) 2022-04-28
EP3541807A1 (en) 2019-09-25
JOP20190109A1 (ar) 2019-05-09
US20220235037A1 (en) 2022-07-28
GEP20237559B (en) 2023-10-25
TN2019000151A1 (en) 2020-10-05
SMT202300494T1 (it) 2024-01-10
EP3964503A1 (en) 2022-03-09
JP2022084717A (ja) 2022-06-07
ZA201903093B (en) 2020-11-25
GEAP202315091A (en) 2023-05-10
JP7042548B2 (ja) 2022-03-28
HUE064559T2 (hu) 2024-03-28
HRP20211863T1 (hr) 2022-03-04
SI3541807T1 (sl) 2022-01-31
CY1124870T1 (el) 2022-11-25
RU2019116689A3 (https=) 2021-02-26
US11993588B2 (en) 2024-05-28
MA58133B1 (fr) 2024-02-29
EA201991086A1 (ru) 2019-11-29
DK3541807T3 (da) 2021-12-06
HRP20231697T1 (hr) 2024-03-15
JOP20190109B1 (ar) 2022-09-15
AU2017361257B2 (en) 2022-02-10
RU2019116689A (ru) 2020-12-17
ECSP19035171A (es) 2019-05-31
PE20191239A1 (es) 2019-09-16
CO2019005045A2 (es) 2019-05-31
ES2966939T3 (es) 2024-04-25
MY199386A (en) 2023-10-25
PL3541807T3 (pl) 2022-01-17
MX2022000249A (es) 2022-02-03
CA3043610A1 (en) 2018-05-24
PH12019501068A1 (en) 2019-08-19
CN115093382A (zh) 2022-09-23
EP3964503C0 (en) 2023-11-08

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