PE20191144A1 - Inhibidores de magl - Google Patents
Inhibidores de maglInfo
- Publication number
- PE20191144A1 PE20191144A1 PE2019001014A PE2019001014A PE20191144A1 PE 20191144 A1 PE20191144 A1 PE 20191144A1 PE 2019001014 A PE2019001014 A PE 2019001014A PE 2019001014 A PE2019001014 A PE 2019001014A PE 20191144 A1 PE20191144 A1 PE 20191144A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- hexafluoropropan
- trifluoromethyl
- cr6r7
- oxobutyl
- Prior art date
Links
Classifications
-
- 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
-
- 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
-
- 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
- A61P25/28—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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (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)
Abstract
Se refiere a un compuesto de Formula ( I), en la que: R1 es -R14, -OR3, -SR4, entre otros; R2 puede ser alquilo C1-C6, halogeno, -CN, haloalquilo C1-C6, entre otros; R3 puede ser -(CR6R7)m-R8, entre otros; R4 puede ser -(CR6R7)m-R8; cada R6 y R7 pueden ser H, F, y alquilo C1-C6; o R6 y R7, junto con el carbono al cual se unen forman un anillo cicloalquilo C3-C6; R14 es -(CR15R16)m-R8; R8 puede ser H, alquilo C1-C6, cicloalquilo C3-C6, arilo y heteroarilo, entre otros; m es 1, 2, 3 o 4; n es 0, 1, 2, 3 o 4; R15 y R16 pueden ser H, F, y alquilo C1-C6. Son compuestos preferidos 4-(2-((4-etoxi-4-oxobutil)amino)-4-(trifluorometil)bencil)piperazina-1-carboxilato de 1,1,1,3,3,3-hexafluoropropan-2-ilo; acido 4-(2-((4-(((1,1,1,3,3,3-hexafluoropropan-2-il)oxi)carbonil)piperazin-1-il)metil)-5-(trifluorometil)fenoxi)butanoico; 4-(2-((4-(1-((etoxicarbonil)oxi)etoxi)-4-oxobutil)amino)-4-(trifluorometil)bencil)piperazina-1-carboxilato de 1,1,1,3,3,3-hexafluoropropan-2-ilo. Dicho compuesto modula la monoacilglicerol lipasa (MAGL), enzima responsable de hidrolizar endocannabinoides tal como el 2-AG, y es util en el tratamiento del dolor neuropatico, enfermedad de Alzheimer, esclerosis multiple, sindrome de Tourette, dolor neuropatico, dolor inflamatorio, entre otros.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662423099P | 2016-11-16 | 2016-11-16 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20191144A1 true PE20191144A1 (es) | 2019-09-02 |
Family
ID=62106678
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2019001014A PE20191144A1 (es) | 2016-11-16 | 2017-11-15 | Inhibidores de magl |
Country Status (29)
| Country | Link |
|---|---|
| US (1) | US10093635B2 (es) |
| EP (1) | EP3541821A4 (es) |
| JP (1) | JP7042547B2 (es) |
| KR (1) | KR20190077544A (es) |
| CN (1) | CN110267963B (es) |
| AR (1) | AR110089A1 (es) |
| AU (1) | AU2017361251B2 (es) |
| BR (1) | BR112019009994A2 (es) |
| CA (1) | CA3043615A1 (es) |
| CL (1) | CL2019001339A1 (es) |
| CO (1) | CO2019005059A2 (es) |
| CR (1) | CR20190241A (es) |
| DO (1) | DOP2019000122A (es) |
| EA (1) | EA038090B1 (es) |
| EC (1) | ECSP19035077A (es) |
| GE (1) | GEP20237470B (es) |
| IL (1) | IL266523B (es) |
| JO (1) | JOP20190106A1 (es) |
| MA (1) | MA46857A (es) |
| MX (1) | MX2019005776A (es) |
| NI (1) | NI201900051A (es) |
| PE (1) | PE20191144A1 (es) |
| PH (1) | PH12019501097A1 (es) |
| RU (1) | RU2754536C1 (es) |
| TN (1) | TN2019000153A1 (es) |
| TW (1) | TWI756299B (es) |
| UA (1) | UA124542C2 (es) |
| WO (1) | WO2018093947A1 (es) |
| ZA (1) | ZA201903100B (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3698782B1 (en) | 2012-01-06 | 2024-05-15 | H. Lundbeck A/S | Carbamate compounds for use in therapy |
| KR20180004263A (ko) | 2015-05-11 | 2018-01-10 | 어바이드 테라퓨틱스, 인크. | 염증 또는 신경병성 통증의 치료 방법 |
| JP7042804B2 (ja) | 2016-09-19 | 2022-03-28 | ルンドベック ラ ホーヤ リサーチ センター，インク． | ピペラジンカルバメート、及びその製造と使用の方法 |
| 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) |
| SI3541807T1 (sl) | 2016-11-16 | 2022-01-31 | H. Lundbeck A/S | Kristalinična oblika zaviralca MAGL |
| PL3630744T3 (pl) | 2017-05-23 | 2023-05-15 | H. Lundbeck A/S | Pirazolowe inhibitory magl |
| MX2020002251A (es) | 2017-08-29 | 2020-07-20 | Lundbeck La Jolla Research Center Inc | Compuestos espirociclicos y sus metodos de preparacion y uso. |
| US10570106B2 (en) | 2018-05-15 | 2020-02-25 | Lundbeck La Jolla Research Center, Inc. | MAGL inhibitors |
| EP3914589A4 (en) * | 2019-01-25 | 2022-11-30 | H. Lundbeck A/S | METHODS OF TREATING A DISEASE USING MAGL INHIBITORS |
| CA3159391A1 (en) * | 2019-11-15 | 2021-05-20 | H. Lundbeck A/S | Crystalline forms of a magl inhibitor |
| IT202000007150A1 (it) * | 2020-04-03 | 2021-10-03 | Univ Pisa | Inibitori di monoacilglicerolo lipasi (magl) |
| JP2023523219A (ja) | 2020-04-21 | 2023-06-02 | ハー・ルンドベック・アクチエゼルスカベット | モノアシルグリセロールリパーゼ阻害剤の合成 |
Family Cites Families (39)
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| FR1593586A (es) | 1967-10-17 | 1970-06-01 | ||
| JPS6183073A (ja) | 1984-10-01 | 1986-04-26 | Oki Electric Ind Co Ltd | 印字装置の用紙送り方法 |
| WO1989011794A1 (en) | 1988-06-07 | 1989-12-14 | Rikagaku Kenkyusho | Plant growth inhibitor |
| EP0619804B1 (en) | 1991-11-27 | 1996-05-22 | E.I. Du Pont De Nemours And Company | Herbicidal acylated amino-(phenyl- or pyridinyl- or thienyl-)-phenyl derivatives |
| DE69408873T2 (de) | 1993-12-22 | 1998-07-09 | Shell Int Research | Verfahren zur herstellung von carbamaten |
| WO1997018196A1 (en) | 1995-11-15 | 1997-05-22 | Zeneca Limited | Herbicidal substituted pyrazole compounds |
| WO1998000408A1 (en) | 1996-07-02 | 1998-01-08 | Novartis Ag | N-phenylimino heterocyclic derivatives and their use as herbicides |
| RU2167150C2 (ru) | 1998-03-25 | 2001-05-20 | Фокин Александр Васильевич | Полифторалкил-n-арилкарбаматы, обладающие антимикробной активностью |
| CA2386540A1 (en) | 1999-10-04 | 2001-04-12 | University Of Medicine And Dentistry Of New Jersey | Novel carbamates and ureas |
| EP1201298A1 (en) | 2000-10-24 | 2002-05-02 | Urea Casale S.A. | Carbamate condensation unit |
| DE10348022A1 (de) | 2003-10-15 | 2005-05-25 | Imtm Gmbh | Neue Dipeptidylpeptidase IV-Inhibitoren zur funktionellen Beeinflussung unterschiedlicher Zellen und zur Behandlung immunologischer, entzündlicher, neuronaler und anderer Erkrankungen |
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| AU2003300702A1 (en) | 2003-12-31 | 2005-07-21 | Council Of Scientific And Industrial Research | Process for preparing carbamates |
| KR20070026382A (ko) | 2004-02-18 | 2007-03-08 | 아스트라제네카 아베 | 아세틸린성 피페라진 화합물 및 대사성 글루타메이트수용체 길항제로서 이들의 용도 |
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| JP2009523729A (ja) | 2006-01-13 | 2009-06-25 | ピーティーシー セラピューティクス，インコーポレーテッド | Ｃ型肝炎の治療方法 |
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| EP2421848A1 (en) | 2009-04-22 | 2012-02-29 | Janssen Pharmaceutica N.V. | Azetidinyl diamides as monoacylglycerol lipase inhibitors |
| UA107791C2 (en) | 2009-05-05 | 2015-02-25 | Dow Agrosciences Llc | Pesticidal compositions |
| TWI506011B (zh) | 2009-11-03 | 2015-11-01 | Bayer Materialscience Ag | 在光聚合物調配物中作為添加劑之氟胺基甲酸酯 |
| FR2960875B1 (fr) | 2010-06-04 | 2012-12-28 | Sanofi Aventis | Derives de carbamates d'hexafluoroisopropyle, leur preparation et leur application en therapeutique |
| EP3698782B1 (en) | 2012-01-06 | 2024-05-15 | H. Lundbeck A/S | Carbamate compounds for use in therapy |
| CN115536635A (zh) | 2012-01-06 | 2022-12-30 | 法国施维雅药厂 | 治疗活性化合物及其使用方法 |
| CA2866302A1 (en) | 2012-03-19 | 2013-09-26 | Abide Therapeutics, Inc. | Carbamate compounds and of making and using same |
| JP2014005245A (ja) | 2012-06-26 | 2014-01-16 | Dainippon Sumitomo Pharma Co Ltd | 二環性ピリミジン誘導体を含有する医薬組成物 |
| US9551036B2 (en) | 2013-02-25 | 2017-01-24 | Whitehead Institute For Biomedical Research | Metabolic gene mesenchymal signatures and uses thereof |
| WO2015003002A1 (en) * | 2013-07-03 | 2015-01-08 | Abide Therapeutics, Inc. | Pyrrolo-pyrrole carbamate and related organic compounds, pharmaceutical compositions, and medical uses thereof |
| WO2016014975A2 (en) * | 2014-07-25 | 2016-01-28 | Northeastern University | Urea/carbamates faah magl or dual faah/magl inhibitors and uses thereof |
| CA2979537C (en) | 2015-03-18 | 2023-08-29 | Abide Therapeutics, Inc. | Piperazine carbamates and methods of making and using same |
| JP7042804B2 (ja) | 2016-09-19 | 2022-03-28 | ルンドベック ラ ホーヤ リサーチ センター，インク． | ピペラジンカルバメート、及びその製造と使用の方法 |
| JOP20190105A1 (ar) | 2016-11-16 | 2019-05-09 | Lundbeck La Jolla Research Center Inc | مثبطات أحادي أسيل جليسرول ليباز (magl) |
-
2017
- 2017-06-16 JO JOP/2019/0106A patent/JOP20190106A1/ar unknown
- 2017-11-15 CA CA3043615A patent/CA3043615A1/en active Pending
- 2017-11-15 EP EP17871753.4A patent/EP3541821A4/en not_active Withdrawn
- 2017-11-15 WO PCT/US2017/061868 patent/WO2018093947A1/en active Application Filing
- 2017-11-15 UA UAA201905620A patent/UA124542C2/uk unknown
- 2017-11-15 AU AU2017361251A patent/AU2017361251B2/en active Active
- 2017-11-15 IL IL266523A patent/IL266523B/en unknown
- 2017-11-15 RU RU2019116512A patent/RU2754536C1/ru active
- 2017-11-15 MX MX2019005776A patent/MX2019005776A/es unknown
- 2017-11-15 PE PE2019001014A patent/PE20191144A1/es unknown
- 2017-11-15 CR CR20190241A patent/CR20190241A/es unknown
- 2017-11-15 TN TNP/2019/000153A patent/TN2019000153A1/en unknown
- 2017-11-15 CN CN201780083663.6A patent/CN110267963B/zh active Active
- 2017-11-15 GE GEAP201715088A patent/GEP20237470B/en unknown
- 2017-11-15 BR BR112019009994A patent/BR112019009994A2/pt unknown
- 2017-11-15 US US15/814,322 patent/US10093635B2/en active Active
- 2017-11-15 MA MA046857A patent/MA46857A/fr unknown
- 2017-11-15 EA EA201991073A patent/EA038090B1/ru unknown
- 2017-11-15 JP JP2019523587A patent/JP7042547B2/ja active Active
- 2017-11-15 KR KR1020197016924A patent/KR20190077544A/ko active IP Right Grant
- 2017-11-15 AR ARP170103184A patent/AR110089A1/es unknown
- 2017-11-16 TW TW106139775A patent/TWI756299B/zh active
-
2019
- 2019-05-16 PH PH12019501097A patent/PH12019501097A1/en unknown
- 2019-05-16 CO CONC2019/0005059A patent/CO2019005059A2/es unknown
- 2019-05-16 DO DO2019000122A patent/DOP2019000122A/es unknown
- 2019-05-16 NI NI201900051A patent/NI201900051A/es unknown
- 2019-05-16 EC ECSENADI201935077A patent/ECSP19035077A/es unknown
- 2019-05-16 CL CL2019001339A patent/CL2019001339A1/es unknown
- 2019-05-17 ZA ZA201903100A patent/ZA201903100B/en unknown
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