CN110267963B - Magl抑制剂 - Google Patents
Magl抑制剂 Download PDFInfo
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- CN110267963B CN110267963B CN201780083663.6A CN201780083663A CN110267963B CN 110267963 B CN110267963 B CN 110267963B CN 201780083663 A CN201780083663 A CN 201780083663A CN 110267963 B CN110267963 B CN 110267963B
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- pharmaceutically acceptable
- acceptable salt
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- HCKVVRSCUWDSPI-UHFFFAOYSA-N tert-butyl 4-[[2-(4-ethoxy-3,3-dimethyl-4-oxobut-1-ynyl)-3-fluoro-4-methylphenyl]methyl]piperazine-1-carboxylate Chemical compound C(C)OC(C(C#CC1=C(CN2CCN(CC2)C(=O)OC(C)(C)C)C=CC(=C1F)C)(C)C)=O HCKVVRSCUWDSPI-UHFFFAOYSA-N 0.000 description 1
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- LHGSERYYEGVXOP-UHFFFAOYSA-N tert-butyl 4-[[3-hydroxy-5-(trifluoromethyl)phenyl]methyl]piperazine-1-carboxylate Chemical compound OC=1C=C(CN2CCN(CC2)C(=O)OC(C)(C)C)C=C(C=1)C(F)(F)F LHGSERYYEGVXOP-UHFFFAOYSA-N 0.000 description 1
- MWRBWPQBGGARAY-UHFFFAOYSA-M tert-butyl acetate;chlorozinc(1+) Chemical compound [Zn+]Cl.CC(C)(C)OC([CH2-])=O MWRBWPQBGGARAY-UHFFFAOYSA-M 0.000 description 1
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- 238000012360 testing method Methods 0.000 description 1
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- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
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- LLPOLZWFYMWNKH-UHFFFAOYSA-N trans-dihydrocodeinone Natural products C1C(N(CCC234)C)C2CCC(=O)C3OC2=C4C1=CC=C2OC LLPOLZWFYMWNKH-UHFFFAOYSA-N 0.000 description 1
- 230000009529 traumatic brain injury Effects 0.000 description 1
- PBIMIGNDTBRRPI-UHFFFAOYSA-N trifluoro borate Chemical compound FOB(OF)OF PBIMIGNDTBRRPI-UHFFFAOYSA-N 0.000 description 1
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- 235000019871 vegetable fat Nutrition 0.000 description 1
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- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
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- GTLDTDOJJJZVBW-UHFFFAOYSA-N zinc cyanide Chemical compound [Zn+2].N#[C-].N#[C-] GTLDTDOJJJZVBW-UHFFFAOYSA-N 0.000 description 1
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Classifications
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- 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
-
- 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
-
- 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
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- 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
- A61P25/28—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
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- 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
- 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
- C07D295/18—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 carboxylic acids, or sulfur or nitrogen analogues thereof
- C07D295/195—Radicals derived from nitrogen analogues of carboxylic acids
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (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)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662423099P | 2016-11-16 | 2016-11-16 | |
| US62/423,099 | 2016-11-16 | ||
| PCT/US2017/061868 WO2018093947A1 (en) | 2016-11-16 | 2017-11-15 | Magl inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN110267963A CN110267963A (zh) | 2019-09-20 |
| CN110267963B true CN110267963B (zh) | 2022-04-01 |
Family
ID=62106678
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201780083663.6A Expired - Fee Related CN110267963B (zh) | 2016-11-16 | 2017-11-15 | Magl抑制剂 |
Country Status (29)
| Country | Link |
|---|---|
| US (1) | US10093635B2 (enExample) |
| EP (1) | EP3541821A4 (enExample) |
| JP (1) | JP7042547B2 (enExample) |
| KR (1) | KR20190077544A (enExample) |
| CN (1) | CN110267963B (enExample) |
| AR (1) | AR110089A1 (enExample) |
| AU (1) | AU2017361251B2 (enExample) |
| BR (1) | BR112019009994A2 (enExample) |
| CA (1) | CA3043615A1 (enExample) |
| CL (1) | CL2019001339A1 (enExample) |
| CO (1) | CO2019005059A2 (enExample) |
| CR (1) | CR20190241A (enExample) |
| DO (1) | DOP2019000122A (enExample) |
| EA (1) | EA038090B1 (enExample) |
| EC (1) | ECSP19035077A (enExample) |
| GE (1) | GEP20237470B (enExample) |
| IL (1) | IL266523B (enExample) |
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| PL2800565T3 (pl) | 2012-01-06 | 2020-09-21 | Lundbeck La Jolla Research Center, Inc. | Związki karbaminianowe i sposoby ich wytwarzania oraz zastosowanie |
| AU2016262459A1 (en) | 2015-05-11 | 2017-12-21 | H. Lundbeck A/S. | Methods of treating inflammation or neuropathic pain |
| US10899737B2 (en) | 2016-09-19 | 2021-01-26 | Lundbeck La Jolla Research Center, Inc. | Piperazine carbamates and methods of making and using same |
| BR112019009992A2 (pt) | 2016-11-16 | 2019-08-27 | Abide Therapeutics Inc | formulações farmacêuticas |
| JOP20190107A1 (ar) | 2016-11-16 | 2019-05-09 | Lundbeck La Jolla Research Center Inc | مثبطات أحادي أسيل جليسرول ليباز (magl) |
| CA3043610A1 (en) | 2016-11-16 | 2018-05-24 | Abide Therapeutics, Inc. | Crystalline forms of a magl inhibitor |
| ES2940111T3 (es) | 2017-05-23 | 2023-05-03 | H Lundbeck As | Inhibidores de MAGL de pirazol |
| MA50041A (fr) | 2017-08-29 | 2020-07-08 | Lundbeck La Jolla Research Center Inc | Composés spirocycliques et procédés de préparation et d'utilisation de ceux-ci |
| SG11202011228TA (en) | 2018-05-15 | 2020-12-30 | Lundbeck La Jolla Research Center Inc | Magl inhibitors |
| SG11202108008PA (en) * | 2019-01-25 | 2021-08-30 | H Lundbeck As | Methods of treating disease with magl inhibitors |
| MX2022005864A (es) * | 2019-11-15 | 2022-08-16 | H Lundbeck As | Formas cristalinas de un inhibidor de magl. |
| IT202000007150A1 (it) * | 2020-04-03 | 2021-10-03 | Univ Pisa | Inibitori di monoacilglicerolo lipasi (magl) |
| BR112021025516A2 (pt) | 2020-04-21 | 2022-11-01 | H Lundbeck As | Processos para a fabricação de 4-(2-(pirrolidin-1-il)-4-(trifluorometil)benzil)piperazina-1-carboxilato de 1,1,1,3,3,3-hexafluoropropan-2-ila e da forma 2 do sal monocloridrato do mesmo |
| MX2024008337A (es) | 2021-12-29 | 2024-07-30 | Psy Therapeutics Inc | Inhibicion de la monoacilglicerol lipasa (magl). |
| CN119137114A (zh) | 2022-05-04 | 2024-12-13 | H.隆德贝克有限公司 | 作为单酰基甘油脂肪酶抑制剂的(s)-1-(哒嗪-3-基氨基甲酰基)-6-氮杂螺[2.5]辛烷-6-甲酸1,1,1,3,3,3-六氟丙-2-酯的结晶形式 |
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