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PE20191144A1 - Inhibidores de magl - Google Patents

Inhibidores de magl

Info

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
Application number
PE2019001014A
Other languages
English (en)
Inventor
Cheryl A Grice
Daniel J Buzard
Michael B Shaghafi
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 PE20191144A1 publication Critical patent/PE20191144A1/es

Links

Classifications

    • 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
    • C07D295/18Heterocyclic 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
    • C07D295/195Radicals derived from nitrogen analogues of carboxylic acids
    • 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
    • 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
    • A61P25/28Drugs 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (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.
PE2019001014A 2016-11-16 2017-11-15 Inhibidores de magl PE20191144A1 (es)

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) MX391117B (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 (15)

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EP3698782B1 (en) 2012-01-06 2024-05-15 H. Lundbeck A/S Carbamate compounds for use in therapy
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EP3541385A4 (en) 2016-11-16 2020-06-24 Lundbeck La Jolla Research Center, Inc. PHARMACEUTICAL FORMULATIONS
JOP20190107A1 (ar) 2016-11-16 2019-05-09 Lundbeck La Jolla Research Center Inc مثبطات أحادي أسيل جليسرول ليباز (magl)
WO2018093953A1 (en) 2016-11-16 2018-05-24 Abide Therapeutics, Inc. Crystalline forms of a magl inhibitor
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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
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US12378219B2 (en) 2022-05-04 2025-08-05 H. Lundbeck A/S Crystalline forms of a MAGL inhibitor

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Also Published As

Publication number Publication date
WO2018093947A1 (en) 2018-05-24
NI201900051A (es) 2019-10-30
CL2019001339A1 (es) 2019-10-04
UA124542C2 (uk) 2021-10-05
DOP2019000122A (es) 2019-09-30
CR20190241A (es) 2019-09-02
TW201823216A (zh) 2018-07-01
IL266523A (en) 2019-07-31
JOP20190106A1 (ar) 2019-05-09
CN110267963A (zh) 2019-09-20
MA46857A (fr) 2019-09-25
JP7042547B2 (ja) 2022-03-28
TWI756299B (zh) 2022-03-01
CN110267963B (zh) 2022-04-01
AR110089A1 (es) 2019-02-20
MX391117B (es) 2025-03-21
EP3541821A1 (en) 2019-09-25
US20180134674A1 (en) 2018-05-17
CO2019005059A2 (es) 2019-05-31
KR20190077544A (ko) 2019-07-03
RU2754536C1 (ru) 2021-09-03
AU2017361251A1 (en) 2019-05-30
JP2020504707A (ja) 2020-02-13
EA038090B1 (ru) 2021-07-05
EP3541821A4 (en) 2020-04-22
US10093635B2 (en) 2018-10-09
ECSP19035077A (es) 2019-05-31
BR112019009994A2 (pt) 2019-08-27
RU2019116512A (ru) 2020-12-17
AU2017361251B2 (en) 2021-08-19
TN2019000153A1 (en) 2020-10-05
CA3043615A1 (en) 2018-05-24
GEP20237470B (en) 2023-02-10
IL266523B (en) 2022-09-01
PH12019501097A1 (en) 2019-08-19
NZ753264A (en) 2020-12-18
EA201991073A1 (ru) 2019-12-30
ZA201903100B (en) 2020-11-25
MX2019005776A (es) 2019-12-05

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