CA2962569C - N-alkylaryl-5-oxyaryl-octahydro-cyclopenta[c]pyrrole negative allosteric modulators of nr2b - Google Patents

N-alkylaryl-5-oxyaryl-octahydro-cyclopenta[c]pyrrole negative allosteric modulators of nr2b Download PDF

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CA2962569C
CA2962569C CA2962569A CA2962569A CA2962569C CA 2962569 C CA2962569 C CA 2962569C CA 2962569 A CA2962569 A CA 2962569A CA 2962569 A CA2962569 A CA 2962569A CA 2962569 C CA2962569 C CA 2962569C
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alkyl
compound
pharmaceutically acceptable
tautomer
stereoisomer
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CA2962569A1 (en
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David R. Anderson
Robert A. Volkmann
Frank S. Menniti
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Novartis AG
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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
    • 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
    • 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
    • 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
    • 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
    • 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)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrrole Compounds (AREA)
CA2962569A 2014-09-26 2015-09-23 N-alkylaryl-5-oxyaryl-octahydro-cyclopenta[c]pyrrole negative allosteric modulators of nr2b Active CA2962569C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462056284P 2014-09-26 2014-09-26
US62/056,284 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 (2)

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CA2962569A1 CA2962569A1 (en) 2016-03-31
CA2962569C true CA2962569C (en) 2023-09-19

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CA2962569A Active CA2962569C (en) 2014-09-26 2015-09-23 N-alkylaryl-5-oxyaryl-octahydro-cyclopenta[c]pyrrole negative allosteric modulators of nr2b

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US (4) US10239835B2 (enExample)
EP (4) EP3683207B1 (enExample)
JP (5) JP6473227B2 (enExample)
KR (1) KR102479356B1 (enExample)
CN (1) CN106795111B (enExample)
AP (1) AP2017009832A0 (enExample)
AR (1) AR103199A1 (enExample)
AU (1) AU2015320721B2 (enExample)
BR (1) BR112017006093B1 (enExample)
CA (1) CA2962569C (enExample)
CL (1) CL2017000474A1 (enExample)
CO (1) CO2017002494A2 (enExample)
CR (1) CR20170114A (enExample)
CU (1) CU24482B1 (enExample)
CY (1) CY1123533T1 (enExample)
DK (1) DK3197868T3 (enExample)
EA (1) EA034937B1 (enExample)
EC (1) ECSP17025302A (enExample)
ES (3) ES2791327T3 (enExample)
GT (1) GT201700062A (enExample)
HR (1) HRP20200959T1 (enExample)
HU (1) HUE049698T2 (enExample)
IL (1) IL250909B (enExample)
JO (1) JO3579B1 (enExample)
LT (1) LT3197868T (enExample)
MX (1) MX374657B (enExample)
MY (1) MY182342A (enExample)
NZ (1) NZ729569A (enExample)
PE (1) PE20170893A1 (enExample)
PH (1) PH12017500513A1 (enExample)
PL (1) PL3197868T3 (enExample)
PT (1) PT3197868T (enExample)
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SG (1) SG11201702023QA (enExample)
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TN (1) TN2017000076A1 (enExample)
TW (1) TWI687407B (enExample)
UY (1) UY36326A (enExample)
WO (1) WO2016049165A1 (enExample)
ZA (1) ZA201701061B (enExample)

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WO2019089676A1 (en) 2017-10-31 2019-05-09 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
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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
CN116744922A (zh) * 2020-12-04 2023-09-12 诺华股份有限公司 Nr2b-nmda受体nam在治疗抑郁症中的剂量方案
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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
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CA3258070A1 (en) 2022-06-02 2023-12-07 Novartis Ag SUBCUTANEOUS ADMINISTRATION OF ONFASPRODIL AND DOSING METHODS INTENDED FOR USE IN THE TREATMENT OF DEPRESSIVE DISORDERS
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TW202539663A (zh) 2023-12-06 2025-10-16 瑞士商諾華公司 用於治療抑鬱障礙之組成物和方法

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GT201700062A (es) 2019-09-30
IL250909B (en) 2019-06-30
MX2017003940A (es) 2018-03-01
IL250909A0 (en) 2017-04-30
EP4282412A3 (en) 2024-01-17
MX374657B (es) 2025-03-06
EA034937B1 (ru) 2020-04-08
EP4282412A2 (en) 2023-11-29
AU2015320721A1 (en) 2017-03-30
SI3197868T1 (sl) 2020-10-30
JP2023052515A (ja) 2023-04-11
EP3197868A4 (en) 2018-04-25
HUE049698T2 (hu) 2020-10-28
PT3197868T (pt) 2020-05-21
CY1123533T1 (el) 2022-03-24
JP2025060835A (ja) 2025-04-10
US20190152912A1 (en) 2019-05-23
PE20170893A1 (es) 2017-07-12
BR112017006093B1 (pt) 2023-03-21
BR112017006093A2 (pt) 2017-12-19
CA2962569A1 (en) 2016-03-31
ES2791327T3 (es) 2020-11-03
CU24482B1 (es) 2020-03-04
CR20170114A (es) 2017-08-21
US12145909B2 (en) 2024-11-19
SG11201702023QA (en) 2017-04-27
EP3974420B1 (en) 2023-08-16
JO3579B1 (ar) 2020-07-05
JP2019077713A (ja) 2019-05-23
US20200369610A1 (en) 2020-11-26
KR20170063599A (ko) 2017-06-08
JP7612722B2 (ja) 2025-01-14
EP3974420A1 (en) 2022-03-30
PL3197868T3 (pl) 2020-11-02
CN106795111B (zh) 2020-04-07
JP6772307B2 (ja) 2020-10-21
WO2016049165A1 (en) 2016-03-31
CN106795111A (zh) 2017-05-31
US10781174B2 (en) 2020-09-22
EP3197868A1 (en) 2017-08-02
JP2017528502A (ja) 2017-09-28
TN2017000076A1 (en) 2018-07-04
EP3683207A1 (en) 2020-07-22
PH12017500513A1 (en) 2017-08-07
LT3197868T (lt) 2020-09-10
US10239835B2 (en) 2019-03-26
AR103199A1 (es) 2017-04-26
JP2021006554A (ja) 2021-01-21
CO2017002494A2 (es) 2017-08-31
AP2017009832A0 (en) 2017-03-31
RS60497B1 (sr) 2020-08-31
JP7216060B2 (ja) 2023-01-31
JP6473227B2 (ja) 2019-02-20
US20220274925A1 (en) 2022-09-01
CL2017000474A1 (es) 2017-08-18
EP3197868B1 (en) 2020-04-15
HRP20200959T1 (hr) 2020-10-02
KR102479356B1 (ko) 2022-12-19
ZA201701061B (en) 2019-07-31
ECSP17025302A (es) 2018-11-30
US20180111902A1 (en) 2018-04-26
EA201790713A1 (ru) 2017-07-31
ES2956546T3 (es) 2023-12-22
UY36326A (es) 2016-04-29
EP3683207B1 (en) 2021-12-29
MY182342A (en) 2021-01-20
CU20170037A7 (es) 2017-08-08
AU2015320721B2 (en) 2020-01-30
DK3197868T3 (da) 2020-06-22
TW201625528A (zh) 2016-07-16
TWI687407B (zh) 2020-03-11
NZ729569A (en) 2019-06-28
ES2911004T3 (es) 2022-05-17

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