BR112017025023A2 - Compostos heterocíclicos de carbamato de 3,3- difluoropiperidina como antagonistas do receptor nmda nr2b - Google Patents

Compostos heterocíclicos de carbamato de 3,3- difluoropiperidina como antagonistas do receptor nmda nr2b

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Publication number
BR112017025023A2
BR112017025023A2 BR112017025023A BR112017025023A BR112017025023A2 BR 112017025023 A2 BR112017025023 A2 BR 112017025023A2 BR 112017025023 A BR112017025023 A BR 112017025023A BR 112017025023 A BR112017025023 A BR 112017025023A BR 112017025023 A2 BR112017025023 A2 BR 112017025023A2
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BR
Brazil
Prior art keywords
difluoropiperidine
receptor antagonists
heterocyclic compounds
nr2b receptor
formula
Prior art date
Application number
BR112017025023A
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English (en)
Other versions
BR112017025023B1 (pt
Inventor
Shapiro Gideon
Original Assignee
Rugen Holdings Cayman Ltd
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Publication date
Application filed by Rugen Holdings Cayman Ltd filed Critical Rugen Holdings Cayman Ltd
Publication of BR112017025023A2 publication Critical patent/BR112017025023A2/pt
Publication of BR112017025023B1 publication Critical patent/BR112017025023B1/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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

Abstract

são divulgadas entidades químicas da fórmula (i), em que r1 e z são definidos neste documento como antagonistas seletivos do receptor subtipo nr2b. também são divulgadas composições farmacêuticas que compreendem uma entidade química da fórmula (i), e métodos de tratamento de diversas doenças e distúrbios associados ao antagonismo de nr2b, por exemplo, doenças e distúrbios do snc, tais como depressão, através da administração de uma entidade química da fórmula (i).
BR112017025023-3A 2015-06-01 2016-05-31 Compostos heterocíclicos de carbamato de 3,3-difluoropiperidina, seu uso como antagonistas do receptor nmda nr2b e composição farmacêutica que os compreende BR112017025023B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562169107P 2015-06-01 2015-06-01
US62/169,107 2015-06-01
PCT/US2016/035098 WO2016196513A1 (en) 2015-06-01 2016-05-31 3,3-difluoropiperidine carbamate heterocyclic compounds as nr2b nmda receptor antagonists

Publications (2)

Publication Number Publication Date
BR112017025023A2 true BR112017025023A2 (pt) 2018-08-07
BR112017025023B1 BR112017025023B1 (pt) 2024-01-30

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BR112017025023-3A BR112017025023B1 (pt) 2015-06-01 2016-05-31 Compostos heterocíclicos de carbamato de 3,3-difluoropiperidina, seu uso como antagonistas do receptor nmda nr2b e composição farmacêutica que os compreende

Country Status (18)

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US (4) US10584127B2 (pt)
EP (1) EP3303323B1 (pt)
JP (1) JP6876625B2 (pt)
KR (1) KR102613179B1 (pt)
CN (1) CN107849010B (pt)
AR (1) AR104837A1 (pt)
AU (1) AU2016270677B2 (pt)
BR (1) BR112017025023B1 (pt)
CA (1) CA2987606C (pt)
DK (1) DK3303323T3 (pt)
ES (1) ES2784398T3 (pt)
HK (1) HK1253023A1 (pt)
IL (1) IL255937B (pt)
MX (1) MX2017015370A (pt)
RU (1) RU2735277C2 (pt)
TW (1) TWI721987B (pt)
WO (1) WO2016196513A1 (pt)
ZA (1) ZA201708006B (pt)

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ES2723436T3 (es) 2014-09-15 2019-08-27 Rugen Holdings Cayman Ltd Derivados de pirrolopirimidina como antagonistas del receptor NMDA NR2B
WO2016126869A1 (en) 2015-02-04 2016-08-11 Rugen Holdings (Cayman) Limited 3,3-difluoro-piperidine derivatives as nr2b nmda receptor antagonists
TWI721987B (zh) 2015-06-01 2021-03-21 開曼群島商盧郡控股（開曼）有限公司 做為nr2b nmda受體拮抗劑之3,3-二氟哌啶胺基甲酸酯雜環化合物
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EP3544610A1 (en) 2016-11-22 2019-10-02 Rugen Holdings (Cayman) Limited Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders
CN116134048A (zh) 2020-04-17 2023-05-16 Hb生物科技有限公司 用于治疗神经精神障碍的组合物和方法

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TWI721987B (zh) 2015-06-01 2021-03-21 開曼群島商盧郡控股（開曼）有限公司 做為nr2b nmda受體拮抗劑之3,3-二氟哌啶胺基甲酸酯雜環化合物
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IL255937A (en) 2018-01-31
KR20180032533A (ko) 2018-03-30
MX2017015370A (es) 2018-03-15
KR102613179B1 (ko) 2023-12-14
JP2018522831A (ja) 2018-08-16
EP3303323A4 (en) 2019-01-02
WO2016196513A1 (en) 2016-12-08
ZA201708006B (en) 2021-07-28
CN107849010B (zh) 2021-11-09
ES2784398T3 (es) 2020-09-24
US11136328B2 (en) 2021-10-05
IL255937B (en) 2021-06-30
HK1253023A1 (zh) 2019-06-06
RU2017142005A3 (pt) 2019-11-19
US10294230B2 (en) 2019-05-21
AU2016270677B2 (en) 2020-11-12
AU2016270677A1 (en) 2017-12-14
DK3303323T3 (da) 2020-03-23
US20200299300A1 (en) 2020-09-24
US20180170935A1 (en) 2018-06-21
CA2987606C (en) 2024-02-20
CA2987606A1 (en) 2016-12-08
JP6876625B2 (ja) 2021-05-26
BR112017025023B1 (pt) 2024-01-30
TW201710248A (zh) 2017-03-16
US20220024937A1 (en) 2022-01-27
TWI721987B (zh) 2021-03-21
EP3303323B1 (en) 2020-01-08
AR104837A1 (es) 2017-08-16
US10584127B2 (en) 2020-03-10
US20180346476A1 (en) 2018-12-06
RU2017142005A (ru) 2019-07-09
EP3303323A1 (en) 2018-04-11
RU2735277C2 (ru) 2020-10-29
CN107849010A (zh) 2018-03-27

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