AR110089A1 - Inhibidores de magl - Google Patents

Inhibidores de magl

Info

Publication number
AR110089A1
AR110089A1 ARP170103184A ARP170103184A AR110089A1 AR 110089 A1 AR110089 A1 AR 110089A1 AR P170103184 A ARP170103184 A AR P170103184A AR P170103184 A ARP170103184 A AR P170103184A AR 110089 A1 AR110089 A1 AR 110089A1
Authority
AR
Argentina
Prior art keywords
6alkyl
cr6r7
independently selected
6haloalkyl
halogen
Prior art date
Application number
ARP170103184A
Other languages
English (en)
Inventor
Michael B Shaghafi
Daniel J Buzard
Cheryl A Grice
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 AR110089A1 publication Critical patent/AR110089A1/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)
  • 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)

Abstract

Reivindicación 1: Un compuesto, caracterizado porque presenta la estructura de la fórmula (1); en donde: R¹ es -R¹⁴, -OR³, -SR⁴, -S(O)₂R⁴, -N(R⁴)(R⁵), -NH(R⁴’) o -CºC-(CR⁶R⁷)-R⁸; cada R² se selecciona de manera independiente entre C₁₋₆alquilo, halógeno, -CN, C₁₋₆haloalquilo, -C₁₋₆alquil(heterocicloalquilo), -OR¹⁷ y -C(O)NR¹⁸R¹⁹; R³ es -(CR⁶R⁷)ₘ-R⁸, -(CR⁶R⁷)ₚ-Y-(CR⁶R⁷)q-R⁸ o -(CR⁶R⁷)ₜ-C₃₋₆cicloalquil-R⁸; R⁴ es -(CR⁶R⁷)ₘ-R⁸’, -(CR⁶R⁷)ᵛ-C(O)OH o -(CR⁶R⁷)ₚ-Y-(CR⁶R⁷)q-R⁸; R⁴’ es -(CR⁶R⁷)ₘ-R⁸’, -(CR⁶R⁷)ₚ-Y-(CR⁶R⁷)q-R⁸, -C₄₋₆alquil-C(O)OH, -C₃₋₆cicloalquil-C(O)OH o -C₁₋₆alquil-C₃₋₆cicloalquil-C(O)OH; Y es -O- o -N(R²²)-; R⁵ es C₁₋₆alquilo o -CH₂-fenilo sustituido opcionalmente con uno, dos o tres grupos seleccionados de manera independiente entre halógeno, C₁₋₆alquilo, C₁₋₆haloalquilo y C₁₋₆alcoxi; cada R⁶ y R⁷ se selecciona de manera independiente entre H, F y C₁₋₆alquilo; o R⁶ y R⁷ forman, junto con el carbono al cual están unidos, un anillo C₃₋₆cicloalquilo; R⁸ es -C(O)OR⁹, -C(O)R¹⁰ o -C(O)O-(CR¹²R¹³)-OC(O)R¹¹; R⁸’ es -C(O)OR⁹’, -C(O)R¹⁰’ o -C(O)O-(CR¹²R¹³)-OC(O)R¹¹; R⁹ es H o C₁₋₆alquilo; R⁹’ es C₁₋₆alquilo; R¹⁰ es C₁₋₆alquilo o -NHSO₂R²¹; R¹⁰’ es C₂₋₆alquilo o -NHSO₂R²¹; R¹¹ es C₁₋₆alquilo o C₁₋₆alcoxi; R¹² y R¹³ es, cada uno de manera independiente, H o C₁₋₆alquilo; R¹⁴ es -(CR¹⁵R¹⁶)ₘ-R⁸ o -(CR⁶R⁷)ₚ-Y-(CR⁶R⁷)q-R⁸; cada R¹⁵ y R¹⁶ se selecciona de manera independiente entre H, F y C₁₋₆alquilo; cada R¹⁷ se selecciona de manera independiente entre H, C₁₋₆alquilo, C₁₋₆haloalquilo y C₃₋₆cicloalquilo; cada R¹⁸ y R¹⁹ se selecciona de manera independiente entre H, C₁₋₆alquilo, C₃₋₆cicloalquilo, arilo y heteroarilo; o R¹⁸ y R¹⁹ forman, junto con el nitrógeno al cual están unidos, un anillo heterocicloalquilo sustituido opcionalmente con uno, dos o tres R²⁰; cada R²⁰ se selecciona de manera independiente entre halógeno, C₁₋₆alquilo, C₁₋₆haloalquilo, oxo, -CN y C₃₋₆cicloalquilo; R²¹ es C₁₋₆alquilo o C₃₋₆cicloalquilo; R²² es H, C₁₋₆alquilo o -SO₂R²³; R²³ es C₁₋₆alquilo; m es 1, 2, 3 ó 4; n es 0, 1, 2, 3 ó 4; p es 2, 3 ó 4; q es 1, 2 ó 3; t es 0, 1 ó 2; y v es 3 ó 4; o una sal o un solvato farmacéuticamente aceptable del mismo.
ARP170103184A 2016-11-16 2017-11-15 Inhibidores de magl AR110089A1 (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
AR110089A1 true AR110089A1 (es) 2019-02-20

Family

ID=62106678

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP170103184A AR110089A1 (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)

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PT3541807T (pt) 2016-11-16 2021-12-09 H Lundbeck As Uma forma cristalina de um inibidor de magl
JOP20190107A1 (ar) 2016-11-16 2019-05-09 Lundbeck La Jolla Research Center Inc مثبطات أحادي أسيل جليسرول ليباز (magl)
JOP20190108B1 (ar) 2016-11-16 2023-09-17 H Lundbeck As تركيبات صيدلانية
FI3630744T3 (fi) 2017-05-23 2023-03-21 H Lundbeck As MAGL:n pyratsoli-inhibiittoreita
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
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CN113330005A (zh) * 2019-01-25 2021-08-31 H.隆德贝克有限公司 用magl抑制剂治疗疾病的方法
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)
WO2021214550A1 (en) 2020-04-21 2021-10-28 H. Lundbeck A/S Synthesis of a monoacylglycerol lipase inhibitor

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Also Published As

Publication number Publication date
MA46857A (fr) 2019-09-25
NI201900051A (es) 2019-10-30
JOP20190106A1 (ar) 2019-05-09
EA038090B1 (ru) 2021-07-05
CL2019001339A1 (es) 2019-10-04
AU2017361251B2 (en) 2021-08-19
TW201823216A (zh) 2018-07-01
DOP2019000122A (es) 2019-09-30
ZA201903100B (en) 2020-11-25
CA3043615A1 (en) 2018-05-24
EA201991073A1 (ru) 2019-12-30
US20180134674A1 (en) 2018-05-17
CR20190241A (es) 2019-09-02
IL266523B (en) 2022-09-01
CN110267963B (zh) 2022-04-01
BR112019009994A2 (pt) 2019-08-27
UA124542C2 (uk) 2021-10-05
MX2019005776A (es) 2019-12-05
GEP20237470B (en) 2023-02-10
PE20191144A1 (es) 2019-09-02
TN2019000153A1 (en) 2020-10-05
IL266523A (en) 2019-07-31
CO2019005059A2 (es) 2019-05-31
KR20190077544A (ko) 2019-07-03
JP2020504707A (ja) 2020-02-13
RU2754536C1 (ru) 2021-09-03
WO2018093947A1 (en) 2018-05-24
RU2019116512A (ru) 2020-12-17
CN110267963A (zh) 2019-09-20
EP3541821A4 (en) 2020-04-22
US10093635B2 (en) 2018-10-09
TWI756299B (zh) 2022-03-01
NZ753264A (en) 2020-12-18
ECSP19035077A (es) 2019-05-31
EP3541821A1 (en) 2019-09-25
PH12019501097A1 (en) 2019-08-19
AU2017361251A1 (en) 2019-05-30
JP7042547B2 (ja) 2022-03-28

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