MX2017003940A - Moduladores alostericos negativos de nr2b de n-alquilaril-5-oxiari l-octahidro-ciclopenta [c] pirrol. - Google Patents

Moduladores alostericos negativos de nr2b de n-alquilaril-5-oxiari l-octahidro-ciclopenta [c] pirrol.

Info

Publication number
MX2017003940A
MX2017003940A MX2017003940A MX2017003940A MX2017003940A MX 2017003940 A MX2017003940 A MX 2017003940A MX 2017003940 A MX2017003940 A MX 2017003940A MX 2017003940 A MX2017003940 A MX 2017003940A MX 2017003940 A MX2017003940 A MX 2017003940A
Authority
MX
Mexico
Prior art keywords
oxyaryl
alkylaryl
nr2b
allosteric modulators
negative allosteric
Prior art date
Application number
MX2017003940A
Other languages
English (en)
Inventor
R Anderson David
A Volkmann Robert
S Menniti Frank
Original Assignee
Luc 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 Luc Therapeutics Inc filed Critical Luc Therapeutics Inc
Publication of MX2017003940A publication Critical patent/MX2017003940A/es

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    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/52Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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

Abstract

La presente invención se refiere a moduladores alostéricos negativos de los receptores NR2B de N-alquilaril-5-oxiaril-octadih idrociclopent[c]pirrol que son útiles en el tratamiento de enfermedades neurológicas, que tienen la fórmula I: (ver Fórmula) en donde R1, R2, L1, L2, X, Y y Y' se describen en la presente. En un aspecto se describen los compuestos de fórmula I y las sales farmacéuticamente aceptables, profármacos, solvatos, hidratos, tautómeros o estereoisómeros de los mismos, en donde L1 es alquilo de C1-C5 lineal o ramificado, sustituido opcionalmente con uno o más sustituyentes seleccionados del grupo que consiste en OH, OR10, NH2, NHR10 y N(R10)(R10'), siempre que no más de un oxígeno o nitrógeno esté unido a cualquier carbono.
MX2017003940A 2014-09-26 2015-09-23 Moduladores alostericos negativos de nr2b de n-alquilaril-5-oxiari l-octahidro-ciclopenta [c] pirrol. MX2017003940A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462056284P 2014-09-26 2014-09-26
PCT/US2015/051694 WO2016049165A1 (en) 2014-09-26 2015-09-23 N-alkylaryl-5-oxyaryl-octahydro-cyclopenta[c]pyrrole negative allosteric modulators of nr2b

Publications (1)

Publication Number Publication Date
MX2017003940A true MX2017003940A (es) 2018-03-01

Family

ID=55581945

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2017003940A MX2017003940A (es) 2014-09-26 2015-09-23 Moduladores alostericos negativos de nr2b de n-alquilaril-5-oxiari l-octahidro-ciclopenta [c] pirrol.

Country Status (40)

Country Link
US (4) US10239835B2 (es)
EP (4) EP3197868B1 (es)
JP (4) JP6473227B2 (es)
KR (1) KR102479356B1 (es)
CN (1) CN106795111B (es)
AP (1) AP2017009832A0 (es)
AR (1) AR103199A1 (es)
AU (1) AU2015320721B2 (es)
BR (1) BR112017006093B1 (es)
CA (1) CA2962569C (es)
CL (1) CL2017000474A1 (es)
CO (1) CO2017002494A2 (es)
CR (1) CR20170114A (es)
CU (1) CU24482B1 (es)
CY (1) CY1123533T1 (es)
DK (1) DK3197868T3 (es)
EA (1) EA034937B1 (es)
EC (1) ECSP17025302A (es)
ES (3) ES2956546T3 (es)
GT (1) GT201700062A (es)
HR (1) HRP20200959T1 (es)
HU (1) HUE049698T2 (es)
IL (1) IL250909B (es)
JO (1) JO3579B1 (es)
LT (1) LT3197868T (es)
MX (1) MX2017003940A (es)
MY (1) MY182342A (es)
NZ (1) NZ729569A (es)
PE (1) PE20170893A1 (es)
PH (1) PH12017500513A1 (es)
PL (1) PL3197868T3 (es)
PT (1) PT3197868T (es)
RS (1) RS60497B1 (es)
SG (1) SG11201702023QA (es)
SI (1) SI3197868T1 (es)
TN (1) TN2017000076A1 (es)
TW (1) TWI687407B (es)
UY (1) UY36326A (es)
WO (1) WO2016049165A1 (es)
ZA (1) ZA201701061B (es)

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IL310346A (en) 2017-10-20 2024-03-01 Univ Vanderbilt Muscarinic acetylcholine M4 receptor antagonists
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CN113950478B (zh) * 2019-06-04 2024-02-02 勃林格殷格翰国际有限公司 作为nr2b负向调节剂的嘌呤衍生物及其作为药物的用途,特别是用于治疗抑郁病症
CN111481543A (zh) * 2020-05-21 2020-08-04 苏州健雄职业技术学院 Nr2b负变构调节剂联合gaba受体调节剂在制备治疗阿尔兹海默症的药物中的用途
AU2021390209A1 (en) 2020-12-04 2023-06-22 Novartis Ag Dosage regimen for a nr2b-nmda receptor nam for the treatment of depression
JP2021058765A (ja) * 2021-01-19 2021-04-15 株式会社藤商事 遊技機
EP4313041A1 (en) * 2021-03-26 2024-02-07 Novartis AG Novel cyclopental[c]pyrrol negative allosteric modulators of nr2b
CN117120053A (zh) * 2021-03-26 2023-11-24 诺华股份有限公司 新的环戊二烯并[c]吡咯NR2B负变构调节剂
WO2023233357A1 (en) 2022-06-02 2023-12-07 Novartis Ag Subcutaneous administration of onfasprodil and dosing methods for use in the treatment of depression disorders

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SG11201702023QA (en) 2017-04-27
US20200369610A1 (en) 2020-11-26
PH12017500513A1 (en) 2017-08-07
EA201790713A1 (ru) 2017-07-31
EA034937B1 (ru) 2020-04-08
EP4282412A3 (en) 2024-01-17
DK3197868T3 (da) 2020-06-22
PT3197868T (pt) 2020-05-21
CU20170037A7 (es) 2017-08-08
ZA201701061B (en) 2019-07-31
IL250909B (en) 2019-06-30
JP6772307B2 (ja) 2020-10-21
AU2015320721A1 (en) 2017-03-30
CA2962569C (en) 2023-09-19
US20190152912A1 (en) 2019-05-23
PE20170893A1 (es) 2017-07-12
BR112017006093B1 (pt) 2023-03-21
IL250909A0 (en) 2017-04-30
CY1123533T1 (el) 2022-03-24
JP2023052515A (ja) 2023-04-11
EP3197868B1 (en) 2020-04-15
BR112017006093A2 (pt) 2017-12-19
EP3683207A1 (en) 2020-07-22
ECSP17025302A (es) 2018-11-30
EP4282412A2 (en) 2023-11-29
CL2017000474A1 (es) 2017-08-18
AU2015320721B2 (en) 2020-01-30
TN2017000076A1 (en) 2018-07-04
WO2016049165A1 (en) 2016-03-31
EP3683207B1 (en) 2021-12-29
JO3579B1 (ar) 2020-07-05
SI3197868T1 (sl) 2020-10-30
JP7216060B2 (ja) 2023-01-31
MY182342A (en) 2021-01-20
ES2956546T3 (es) 2023-12-22
ES2791327T3 (es) 2020-11-03
RS60497B1 (sr) 2020-08-31
AP2017009832A0 (en) 2017-03-31
TW201625528A (zh) 2016-07-16
TWI687407B (zh) 2020-03-11
CO2017002494A2 (es) 2017-08-31
US20180111902A1 (en) 2018-04-26
US20220274925A1 (en) 2022-09-01
UY36326A (es) 2016-04-29
GT201700062A (es) 2019-09-30
CA2962569A1 (en) 2016-03-31
JP2019077713A (ja) 2019-05-23
CN106795111B (zh) 2020-04-07
JP2021006554A (ja) 2021-01-21
EP3974420B1 (en) 2023-08-16
JP2017528502A (ja) 2017-09-28
US10781174B2 (en) 2020-09-22
EP3197868A1 (en) 2017-08-02
EP3974420A1 (en) 2022-03-30
CU24482B1 (es) 2020-03-04
PL3197868T3 (pl) 2020-11-02
HRP20200959T1 (hr) 2020-10-02
LT3197868T (lt) 2020-09-10
CR20170114A (es) 2017-08-21
KR102479356B1 (ko) 2022-12-19
EP3197868A4 (en) 2018-04-25
AR103199A1 (es) 2017-04-26
ES2911004T3 (es) 2022-05-17
CN106795111A (zh) 2017-05-31
HUE049698T2 (hu) 2020-10-28
NZ729569A (en) 2019-06-28
KR20170063599A (ko) 2017-06-08
JP6473227B2 (ja) 2019-02-20
US10239835B2 (en) 2019-03-26

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