EA201691673A1 - Замещенные циклопентаны, тетрагидрофураны и пирролидины как антагонисты орексиновых рецепторов - Google Patents

Замещенные циклопентаны, тетрагидрофураны и пирролидины как антагонисты орексиновых рецепторов

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Publication number
EA201691673A1
EA201691673A1 EA201691673A EA201691673A EA201691673A1 EA 201691673 A1 EA201691673 A1 EA 201691673A1 EA 201691673 A EA201691673 A EA 201691673A EA 201691673 A EA201691673 A EA 201691673A EA 201691673 A1 EA201691673 A1 EA 201691673A1
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EA
Eurasian Patent Office
Prior art keywords
tetrahydrofuranes
pyrrolidines
antagonists
orexin receptors
substituted cyclopentanes
Prior art date
Application number
EA201691673A
Other languages
English (en)
Other versions
EA031982B1 (ru
Inventor
Шарлотта Филдхаус
Анджела ГЛЕН
Татсухико Фудзимото
Джон Стивен Робинсон
Original Assignee
Такеда Фармасьютикл Компани Лимитед
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Publication date
Application filed by Такеда Фармасьютикл Компани Лимитед filed Critical Такеда Фармасьютикл Компани Лимитед
Publication of EA201691673A1 publication Critical patent/EA201691673A1/ru
Publication of EA031982B1 publication Critical patent/EA031982B1/ru

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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
    • A61K31/01Hydrocarbons
    • A61K31/015Hydrocarbons carbocyclic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/428Thiazoles condensed with carbocyclic rings
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61P25/04Centrally 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
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/28Drugs 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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

Abstract

Данное изобретение предлагает соединения формулы (I) и их фармацевтически приемлемые соли, где L, X, R, R, R, Rи Rимеют значения, определенные в описании, способы их получения, содержащие их фармацевтические композиции и их применение в терапии.
EA201691673A 2014-02-20 2015-02-19 Замещенные циклопентаны, тетрагидрофураны и пирролидины как антагонисты орексиновых рецепторов EA031982B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14156010 2014-02-20
PCT/GB2015/050482 WO2015124934A1 (en) 2014-02-20 2015-02-19 Subsituted cyclopentanes, tetrahydrofuranes and pyrrolidines as orexin receptor antagonists

Publications (2)

Publication Number Publication Date
EA201691673A1 true EA201691673A1 (ru) 2017-01-30
EA031982B1 EA031982B1 (ru) 2019-03-29

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
EA201691673A EA031982B1 (ru) 2014-02-20 2015-02-19 Замещенные циклопентаны, тетрагидрофураны и пирролидины как антагонисты орексиновых рецепторов

Country Status (20)

Country Link
US (1) US9790220B2 (ru)
EP (1) EP3107907A1 (ru)
JP (1) JP6466465B2 (ru)
KR (1) KR20160124188A (ru)
CN (1) CN106164064B (ru)
AU (1) AU2015220553B2 (ru)
CA (1) CA2940047A1 (ru)
CL (1) CL2016002085A1 (ru)
CR (1) CR20160373A (ru)
EA (1) EA031982B1 (ru)
EC (1) ECSP16074482A (ru)
GE (1) GEP20186909B (ru)
IL (1) IL247195A0 (ru)
MA (1) MA39229A1 (ru)
MX (1) MX2016010745A (ru)
PE (1) PE20161374A1 (ru)
PH (1) PH12016501625A1 (ru)
SG (1) SG11201606839SA (ru)
WO (1) WO2015124934A1 (ru)
ZA (1) ZA201604924B (ru)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201613864A (en) * 2014-02-20 2016-04-16 Takeda Pharmaceutical Novel compounds
CN106659750B (zh) 2014-04-17 2021-02-12 韩国生命工学研究院 用于预防或治疗慢性阻塞性肺疾病的药物组合物
AU2016360245B2 (en) 2015-11-23 2020-07-09 Sunshine Lake Pharma Co., Ltd. Octahydropyrrolo [3, 4-c] pyrrole derivatives and uses thereof
KR102298546B1 (ko) * 2018-10-18 2021-09-08 에이치케이이노엔 주식회사 신규한 n-(이소프로필-트리아졸릴)피리디닐)-헤테로아릴-카르복사미드 유도체 및 이의 용도

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4399256B2 (ja) * 2001-06-28 2010-01-13 スミスクライン ビーチャム ピー エル シー オレキシン受容体アンタゴニストとしてのn−アロイル環状アミン誘導体
WO2008038841A1 (fr) * 2006-09-30 2008-04-03 Japan Tobacco Inc. Dérivé de thiadiazolone et utilisation de celui-ci
EP2491034B1 (en) * 2009-10-23 2013-12-18 Janssen Pharmaceutica, N.V. Fused heterocyclic compounds as orexin receptor modulators
US20110144081A1 (en) * 2009-12-15 2011-06-16 Henner Knust Pyrrolidine derivatives
TWI570120B (zh) * 2012-06-04 2017-02-11 艾克泰聯製藥有限公司 苯并咪唑脯胺酸衍生物

Also Published As

Publication number Publication date
SG11201606839SA (en) 2016-09-29
CN106164064B (zh) 2019-03-22
WO2015124934A8 (en) 2016-07-21
PE20161374A1 (es) 2016-12-17
EP3107907A1 (en) 2016-12-28
ZA201604924B (en) 2019-04-24
WO2015124934A1 (en) 2015-08-27
JP6466465B2 (ja) 2019-02-06
ECSP16074482A (es) 2018-05-31
US9790220B2 (en) 2017-10-17
IL247195A0 (en) 2016-09-29
CL2016002085A1 (es) 2017-06-09
CA2940047A1 (en) 2015-08-27
AU2015220553A1 (en) 2016-07-21
PH12016501625A1 (en) 2016-11-07
MX2016010745A (es) 2017-02-02
CN106164064A (zh) 2016-11-23
EA031982B1 (ru) 2019-03-29
JP2017506239A (ja) 2017-03-02
US20170073340A1 (en) 2017-03-16
AU2015220553B2 (en) 2019-06-27
CR20160373A (es) 2016-12-02
MA39229A1 (fr) 2018-01-31
GEP20186909B (en) 2018-10-25
KR20160124188A (ko) 2016-10-26

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