PE20191146A1 - Inhibidores de magl - Google Patents

Inhibidores de magl

Info

Publication number
PE20191146A1
PE20191146A1 PE2019001015A PE2019001015A PE20191146A1 PE 20191146 A1 PE20191146 A1 PE 20191146A1 PE 2019001015 A PE2019001015 A PE 2019001015A PE 2019001015 A PE2019001015 A PE 2019001015A PE 20191146 A1 PE20191146 A1 PE 20191146A1
Authority
PE
Peru
Prior art keywords
hexafluoropropan
piperazin
oxy
carbonyl
phenyl
Prior art date
Application number
PE2019001015A
Other languages
English (en)
Inventor
Cheryl A Grice
Daniel J Buzard
Nicole S White
Donald L Hertzog
Original Assignee
Abide Therapeutics Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Abide Therapeutics Inc filed Critical Abide Therapeutics Inc
Publication of PE20191146A1 publication Critical patent/PE20191146A1/es

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    • 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
    • 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
    • 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
    • A61K31/4965Non-condensed pyrazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • 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
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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]
    • 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]
    • A61P29/02Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Se refiere a un compuesto de formula (I): En la que R1 es -N(R3)(R5) o -NH(R4); R2 puede ser un halogeno, alquilo C1-C6; -CN, haloalquilo C1-C6, entre otros; R3 es -CH2CO2H, -CH2CH2CO2H, o -CH(CH3)CO2H, entre otros; R4 es -(CH2)m-CO2H; R5 es H o alquilo C1-C3; n es 0, 1, 2, 3, o 4; y m es 3; o una sal solvato farmaceuticamente aceptable. Son compuestos preferidos acido 4-((2-((4-(((1,1,1,3,3,3-hexafluoropropan-2-il)oxi)carbonil)piperazin-1-il)metil)5(trifluorometil)fenil)amino)butanoico; (5-cloro-2-((4-(((1,1,1,3,3,3-hexafluoropropan-2-il)oxi)carbonil)piperazin-1-il)metil)fenil)glicina; acido3-((5-cloro-2-((4-(((1,1,1,3,3,3-hexafluoropropan-2-il)oxi)carbonil)piperazin-1-il)metil)-5-(trifluorometil)fenil)amino)propanoico. Tambien se refiere a una composicion farmaceutica. Dicho compuesto es modulador de la monoacilglicerol lipasa (MAGL), y es util en el tratamiento del dolor neuropatico, inflamatorio, trastornos convulsivos, esclerosis multiple, enfermedad de Alzheimer, entre otros.
PE2019001015A 2016-11-16 2017-11-15 Inhibidores de magl PE20191146A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201662423095P 2016-11-16 2016-11-16

Publications (1)

Publication Number Publication Date
PE20191146A1 true PE20191146A1 (es) 2019-09-02

Family

ID=62107273

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2019001015A PE20191146A1 (es) 2016-11-16 2017-11-15 Inhibidores de magl

Country Status (27)

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

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EP3294731A4 (en) 2015-05-11 2018-10-24 Abide Therapeutics, Inc. Methods of treating inflammation or neuropathic pain
EP3515897B1 (en) 2016-09-19 2021-08-18 H. Lundbeck A/S Piperazine carbamates as modulators of magl and/or abhd6 and their use
JOP20190107A1 (ar) * 2016-11-16 2019-05-09 Lundbeck La Jolla Research Center Inc مثبطات أحادي أسيل جليسرول ليباز (magl)
LT3541807T (lt) 2016-11-16 2021-12-27 H. Lundbeck A/S Magl inhibitoriaus kristalinė forma
JOP20190108B1 (ar) 2016-11-16 2023-09-17 H Lundbeck As تركيبات صيدلانية
JOP20190106A1 (ar) 2016-11-16 2019-05-09 Lundbeck La Jolla Research Center Inc مثبطات أحادي أسيل جليسرول ليباز (magl)
ES2952332T3 (es) 2017-08-29 2023-10-30 H Lundbeck As Compuestos espirocíclicos y sus métodos de preparación y uso
EP3704127A1 (en) * 2017-11-02 2020-09-09 AiCuris GmbH & Co. KG Novel, highly active amino-thiazole substituted indole-2-carboxamides active against the hepatitis b virus (hbv)
AR115092A1 (es) 2018-05-15 2020-11-25 Abide Therapeutics Inc Inhibidores de magl
US11702393B2 (en) * 2020-04-21 2023-07-18 H. Lundbeck A/S Synthesis of a monoacylglycerol lipase inhibitor
TW202229255A (zh) 2020-11-13 2022-08-01 丹麥商H 朗德貝克公司 Magl抑制劑

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Also Published As

Publication number Publication date
KR20190077087A (ko) 2019-07-02
TN2019000150A1 (en) 2020-10-05
CN110248947A (zh) 2019-09-17
IL266550A (en) 2019-07-31
RU2019116514A (ru) 2020-12-17
DOP2019000121A (es) 2019-09-30
PH12019501102A1 (en) 2019-08-19
EP3541822B1 (en) 2022-01-19
AU2017361250A1 (en) 2019-05-30
EP3541822A1 (en) 2019-09-25
CR20190243A (es) 2019-06-26
BR112019009991A2 (pt) 2019-08-27
CO2019005038A2 (es) 2019-05-31
WO2018093946A1 (en) 2018-05-24
EP3541822A4 (en) 2020-04-29
CA3043612A1 (en) 2018-05-24
MX2019005771A (es) 2019-12-05
US9981930B1 (en) 2018-05-29
TW201831458A (zh) 2018-09-01
MA46860A (fr) 2019-09-25
ES2908632T3 (es) 2022-05-03
US20180134675A1 (en) 2018-05-17
NI201900050A (es) 2019-10-30
JOP20190105A1 (ar) 2019-05-09
EA201991074A1 (ru) 2019-12-30
CL2019001335A1 (es) 2019-10-04
JP6987859B2 (ja) 2022-01-05
JP2020502047A (ja) 2020-01-23
ECSP19035377A (es) 2019-05-31
AR110088A1 (es) 2019-02-20
CN110248947B (zh) 2022-04-01

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