JP7042468B2 - Ｍａｇｌ阻害剤 - Google Patents
Ｍａｇｌ阻害剤 Download PDFInfo
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- JP7042468B2 JP7042468B2 JP2019523671A JP2019523671A JP7042468B2 JP 7042468 B2 JP7042468 B2 JP 7042468B2 JP 2019523671 A JP2019523671 A JP 2019523671A JP 2019523671 A JP2019523671 A JP 2019523671A JP 7042468 B2 JP7042468 B2 JP 7042468B2
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- Prior art keywords
- pharmaceutically acceptable
- formula
- solvate
- compound
- acceptable salt
- Prior art date
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- 229940124530 sulfonamide Drugs 0.000 description 1
- 150000003456 sulfonamides Chemical class 0.000 description 1
- 150000003871 sulfonates Chemical class 0.000 description 1
- 150000003459 sulfonic acid esters Chemical class 0.000 description 1
- 230000004083 survival effect Effects 0.000 description 1
- 230000002194 synthesizing effect Effects 0.000 description 1
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- 239000006188 syrup Substances 0.000 description 1
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- 238000003419 tautomerization reaction Methods 0.000 description 1
- WZWYJBNHTWCXIM-UHFFFAOYSA-N tenoxicam Chemical compound O=C1C=2SC=CC=2S(=O)(=O)N(C)C1=C(O)NC1=CC=CC=N1 WZWYJBNHTWCXIM-UHFFFAOYSA-N 0.000 description 1
- 229960002871 tenoxicam Drugs 0.000 description 1
- AGYJKDRKBSJWLJ-UHFFFAOYSA-N tert-butyl 1,8-diazaspiro[4.5]decane-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCCC11CCNCC1 AGYJKDRKBSJWLJ-UHFFFAOYSA-N 0.000 description 1
- FYUVLZRRIRGSTE-UHFFFAOYSA-N tert-butyl 2,3,3a,4,6,6a-hexahydro-1h-pyrrolo[3,4-c]pyrrole-5-carboxylate Chemical compound C1NCC2CN(C(=O)OC(C)(C)C)CC21 FYUVLZRRIRGSTE-UHFFFAOYSA-N 0.000 description 1
- LXCFKRGUNOCAAR-UHFFFAOYSA-N tert-butyl 4-[2-formyl-5-(trifluoromethyl)phenoxy]butanoate Chemical compound C(=O)C1=C(OCCCC(=O)OC(C)(C)C)C=C(C=C1)C(F)(F)F LXCFKRGUNOCAAR-UHFFFAOYSA-N 0.000 description 1
- NCZATBPIZHRPEE-UHFFFAOYSA-N tert-butyl 4-amino-2,2-dimethylbutanoate Chemical compound NCCC(C(=O)OC(C)(C)C)(C)C NCZATBPIZHRPEE-UHFFFAOYSA-N 0.000 description 1
- WHRNULOCNSKMGB-UHFFFAOYSA-N tetrahydrofuran thf Chemical compound C1CCOC1.C1CCOC1 WHRNULOCNSKMGB-UHFFFAOYSA-N 0.000 description 1
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- 125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
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- 125000001984 thiazolidinyl group Chemical group 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 125000005985 thienyl[1,3]dithianyl group Chemical group 0.000 description 1
- 238000003354 tissue distribution assay Methods 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 229960004380 tramadol Drugs 0.000 description 1
- TVYLLZQTGLZFBW-GOEBONIOSA-N tramadol Natural products COC1=CC=CC([C@@]2(O)[C@@H](CCCC2)CN(C)C)=C1 TVYLLZQTGLZFBW-GOEBONIOSA-N 0.000 description 1
- LLPOLZWFYMWNKH-UHFFFAOYSA-N trans-dihydrocodeinone Natural products C1C(N(CCC234)C)C2CCC(=O)C3OC2=C4C1=CC=C2OC LLPOLZWFYMWNKH-UHFFFAOYSA-N 0.000 description 1
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- 206010044652 trigeminal neuralgia Diseases 0.000 description 1
- 125000005591 trimellitate group Chemical group 0.000 description 1
- YFTHZRPMJXBUME-UHFFFAOYSA-N tripropylamine Chemical compound CCCN(CCC)CCC YFTHZRPMJXBUME-UHFFFAOYSA-N 0.000 description 1
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- 235000019871 vegetable fat Nutrition 0.000 description 1
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- 229920002554 vinyl polymer Polymers 0.000 description 1
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- 239000000080 wetting agent Substances 0.000 description 1
- 229940093612 zein Drugs 0.000 description 1
- 239000005019 zein Substances 0.000 description 1
- 239000011701 zinc Chemical class 0.000 description 1
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Classifications
-
- 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
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
-
- 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
- A61P25/28—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]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Neurology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
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| US201662423102P | 2016-11-16 | 2016-11-16 | |
| US62/423,102 | 2016-11-16 | ||
| PCT/US2017/061870 WO2018093949A1 (en) | 2016-11-16 | 2017-11-15 | Magl inhibitors |
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| JP2020500178A JP2020500178A (ja) | 2020-01-09 |
| JP2020500178A5 JP2020500178A5 (enExample) | 2020-12-24 |
| JP7042468B2 true JP7042468B2 (ja) | 2022-03-28 |
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| MA (1) | MA46855A (enExample) |
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| PE (1) | PE20191145A1 (enExample) |
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| RU (1) | RU2019115784A (enExample) |
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| WO2017197192A1 (en) * | 2016-05-12 | 2017-11-16 | Abide Therapeutics, Inc. | Spirocycle compounds and methods of making and using same |
| JOP20190107A1 (ar) | 2016-11-16 | 2019-05-09 | Lundbeck La Jolla Research Center Inc | مثبطات أحادي أسيل جليسرول ليباز (magl) |
| AU2017361257B2 (en) | 2016-11-16 | 2022-02-10 | H. Lundbeck A/S. | Crystalline forms of a MAGL inhibitor |
| JOP20190105A1 (ar) * | 2016-11-16 | 2019-05-09 | Lundbeck La Jolla Research Center Inc | مثبطات أحادي أسيل جليسرول ليباز (magl) |
| WO2018093950A1 (en) | 2016-11-16 | 2018-05-24 | Abide Therapeutics, Inc. | Pharmaceutical formulations |
| US10927105B1 (en) | 2017-05-23 | 2021-02-23 | Lundbeck La Jolla Research Center, Inc. | Pyrazole MAGL inhibitors |
| LT3630744T (lt) | 2017-05-23 | 2023-03-10 | H. Lundbeck A/S | Pirazolo magl inhibitoriai |
| MX2020002251A (es) | 2017-08-29 | 2020-07-20 | Lundbeck La Jolla Research Center Inc | Compuestos espirociclicos y sus metodos de preparacion y uso. |
| US11161856B2 (en) | 2017-08-29 | 2021-11-02 | H. Lundbeck A/S | Spirocycle compounds and methods of making and using same |
| JP2021531287A (ja) * | 2018-07-19 | 2021-11-18 | ファイザー・インク | Ｍａｇｌ阻害剤としての複素環式スピロ化合物 |
| BR112021002298A2 (pt) | 2018-08-13 | 2021-05-04 | F. Hoffmann-La Roche Ag | compostos heterocíclicos como inibidores da monoacilglicerol lipase |
| IL297470A (en) | 2020-04-21 | 2022-12-01 | H Lundbeck As | 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 |
| US20250084065A1 (en) | 2021-12-29 | 2025-03-13 | Psy Therapeutics, Inc. | Inhibiting monoacylglycerol lipase (magl) |
| US12378219B2 (en) | 2022-05-04 | 2025-08-05 | H. Lundbeck A/S | Crystalline forms of a MAGL inhibitor |
| WO2024168426A1 (en) | 2023-02-13 | 2024-08-22 | Apogee Pharmaceuticals, Inc. | Small molecules as monoacylglycerol lipase (magl) inhibitors, compositions and use thereof |
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-
2017
- 2017-06-16 JO JOP/2019/0107A patent/JOP20190107A1/ar unknown
- 2017-11-15 RU RU2019115784A patent/RU2019115784A/ru unknown
- 2017-11-15 KR KR1020197017201A patent/KR20190080935A/ko not_active Ceased
- 2017-11-15 ES ES17871458T patent/ES2952582T3/es active Active
- 2017-11-15 WO PCT/US2017/061870 patent/WO2018093949A1/en not_active Ceased
- 2017-11-15 CR CR20190239A patent/CR20190239A/es unknown
- 2017-11-15 PE PE2019001017A patent/PE20191145A1/es unknown
- 2017-11-15 MA MA046855A patent/MA46855A/fr unknown
- 2017-11-15 US US16/349,047 patent/US11059822B2/en active Active
- 2017-11-15 JP JP2019523671A patent/JP7042468B2/ja active Active
- 2017-11-15 BR BR112019009880A patent/BR112019009880A2/pt not_active IP Right Cessation
- 2017-11-15 EP EP17871458.0A patent/EP3541820B1/en active Active
- 2017-11-15 TN TNP/2019/000149A patent/TN2019000149A1/en unknown
- 2017-11-15 EA EA201991029A patent/EA038150B1/ru unknown
- 2017-11-15 MX MX2019005773A patent/MX389627B/es unknown
- 2017-11-15 CN CN201780083651.3A patent/CN110267962B/zh active Active
- 2017-11-15 CA CA3043617A patent/CA3043617A1/en not_active Abandoned
- 2017-11-15 UA UAA201905617A patent/UA125523C2/uk unknown
- 2017-11-15 AU AU2017361253A patent/AU2017361253B2/en not_active Ceased
-
2019
- 2019-05-12 IL IL266547A patent/IL266547B/en unknown
- 2019-05-14 DO DO2019000118A patent/DOP2019000118A/es unknown
- 2019-05-14 CO CONC2019/0004945A patent/CO2019004945A2/es unknown
- 2019-05-15 PH PH12019501079A patent/PH12019501079A1/en unknown
- 2019-05-15 EC ECSENADI201934535A patent/ECSP19034535A/es unknown
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- 2019-05-16 CL CL2019001336A patent/CL2019001336A1/es unknown
- 2019-05-17 ZA ZA2019/03099A patent/ZA201903099B/en unknown
-
2021
- 2021-06-09 US US17/343,227 patent/US11691975B2/en active Active
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| EP3675848B1 (en) | Spirocycle compounds and methods of making and using same | |
| JP6987859B2 (ja) | Ｍａｇｌ阻害剤 | |
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