EA201690790A1 - Серосодержащее бициклическое соединение - Google Patents

Серосодержащее бициклическое соединение

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Publication number
EA201690790A1
EA201690790A1 EA201690790A EA201690790A EA201690790A1 EA 201690790 A1 EA201690790 A1 EA 201690790A1 EA 201690790 A EA201690790 A EA 201690790A EA 201690790 A EA201690790 A EA 201690790A EA 201690790 A1 EA201690790 A1 EA 201690790A1
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Eurasian Patent Office
Prior art keywords
cognitive impairment
schizophrenia
cias
charcot
spasticity
Prior art date
Application number
EA201690790A
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English (en)
Other versions
EA029075B1 (ru
Inventor
Нобуюки Сираиси
Хироаки Хосии
Ватару Хамагути
Эрико Хондзо
Томофуми Такува
Юдзи Кондо
Такаюки Гото
Original Assignee
Астеллас Фарма Инк.
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Application filed by Астеллас Фарма Инк. filed Critical Астеллас Фарма Инк.
Publication of EA201690790A1 publication Critical patent/EA201690790A1/ru
Publication of EA029075B1 publication Critical patent/EA029075B1/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
    • A61K31/33Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5355Non-condensed oxazines 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/554Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
    • 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
    • A61P25/04Centrally 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
    • A61P25/18Antipsychotics, 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
    • A61P25/24Antidepressants
    • 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
    • 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
    • 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
    • A61P25/32Alcohol-abuse
    • 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]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/08Bridged systems
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    • C07DHETEROCYCLIC COMPOUNDS
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    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Предложено соединение, полезное в качестве фармацевтической композиции для предупреждения и/или лечения шизофрении, когнитивного нарушения, связанного с шизофренией (CIAS), когнитивного нарушения, синдрома ломкой Х-хромосомы, расстройства аутистического спектра, спастичности, тревожного расстройства, наркомании, боли, фибромиалгии, болезни Шарко-Мари-Тута или тому подобного. Проведено исследование фармацевтической композиции для предупреждения и/или лечения шизофрении, когнитивного нарушения, связанного с шизофренией (CIAS), когнитивного нарушения, синдрома ломкой X-хромосомы, расстройства аутистического спектра, спастичности, тревожного расстройства, наркомании, боли, фибромиалгии, болезни Шарко-Мари-Тута или тому подобного, обладающей действием позитивного аллостерического модулятора (РАМ-действием) GABA, и установлено, что серосодержащее бициклическое соединение является РАМ рецептора GABA, и тем самым завершено данное изобретение. Серосодержащее бициклическое соединение по настоящему изобретению обладает РАМ-действием GABAи может быть полезно в качестве средства для предупреждения и/или лечения шизофрении, CIAS, когнитивного нарушения, синдрома ломкой X-хромосомы, расстройства аутического спектра, спастичности, тревожного расстройства, наркомании, боли, фибромиалгии или болезни Шарко-Мари-Тута.
EA201690790A 2013-10-17 2014-10-17 Серосодержащее бициклическое соединение EA029075B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2013216332 2013-10-17
PCT/JP2014/077653 WO2015056771A1 (ja) 2013-10-17 2014-10-17 含硫黄二環式化合物

Publications (2)

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EA201690790A1 true EA201690790A1 (ru) 2016-08-31
EA029075B1 EA029075B1 (ru) 2018-02-28

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US (2) US9051339B2 (ru)
EP (1) EP3059239B1 (ru)
JP (1) JP6477484B2 (ru)
KR (1) KR102248450B1 (ru)
CN (1) CN105636965B (ru)
AR (1) AR098070A1 (ru)
AU (1) AU2014335304B2 (ru)
BR (1) BR112016008654B8 (ru)
CA (1) CA2927518C (ru)
CY (1) CY1120880T1 (ru)
DK (1) DK3059239T3 (ru)
EA (1) EA029075B1 (ru)
ES (1) ES2685070T3 (ru)
HK (1) HK1220192A1 (ru)
HR (1) HRP20181183T1 (ru)
HU (1) HUE040208T2 (ru)
IL (1) IL244953B (ru)
LT (1) LT3059239T (ru)
MX (1) MX367857B (ru)
MY (1) MY177271A (ru)
NZ (1) NZ719149A (ru)
PH (1) PH12016500625B1 (ru)
PL (1) PL3059239T3 (ru)
PT (1) PT3059239T (ru)
RS (1) RS57532B1 (ru)
SA (1) SA516370956B1 (ru)
SG (1) SG11201602926UA (ru)
SI (1) SI3059239T1 (ru)
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HU231058B1 (hu) 2017-03-13 2020-04-28 Richter Gedeon Nyrt. Gyógyászatilag hatékony aliciklusos-szubsztituált pirazolo[1,5-a]pirimidin származékok
US20210346392A1 (en) 2018-08-31 2021-11-11 Astellas Pharma Inc. Pharmaceutical composition for oral administration
TW202220992A (zh) 2020-08-05 2022-06-01 匈牙利商羅特格登公司 具藥理活性之經雜環取代的吡唑并〔1,5-a〕嘧啶衍生物
WO2023028519A2 (en) 2021-08-27 2023-03-02 Astellas Pharma Global Development, Inc. Methods of treating substance use disorder
WO2024048714A1 (ja) * 2022-09-01 2024-03-07 アステラス製薬株式会社 6-(4,4-ジメチルシクロヘキシル)-4-[(1,1-ジオキソ-1λ6-チオモルホリン-4-イル)メチル]-2-メチルチエノ[2,3-d]ピリミジンまたはその塩の製造方法

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JP2001097979A (ja) 1999-07-28 2001-04-10 Takeda Chem Ind Ltd 縮合複素環化合物、その製造法および用途
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Publication number Publication date
MY177271A (en) 2020-09-10
PH12016500625A1 (en) 2016-05-23
AR098070A1 (es) 2016-04-27
CA2927518A1 (en) 2015-04-23
US9051339B2 (en) 2015-06-09
BR112016008654B8 (pt) 2023-02-14
BR112016008654B1 (pt) 2022-12-06
LT3059239T (lt) 2018-09-10
PL3059239T3 (pl) 2018-10-31
RS57532B1 (sr) 2018-10-31
JPWO2015056771A1 (ja) 2017-03-09
TWI648281B (zh) 2019-01-21
WO2015056771A1 (ja) 2015-04-23
ES2685070T3 (es) 2018-10-05
US20150231138A1 (en) 2015-08-20
EA029075B1 (ru) 2018-02-28
HRP20181183T1 (hr) 2018-10-19
IL244953A0 (en) 2016-05-31
CA2927518C (en) 2022-04-12
MX2016004944A (es) 2016-07-11
CN105636965A (zh) 2016-06-01
EP3059239B1 (en) 2018-06-27
JP6477484B2 (ja) 2019-03-06
PH12016500625B1 (en) 2016-05-23
KR20160071408A (ko) 2016-06-21
SI3059239T1 (en) 2018-08-31
MX367857B (es) 2019-09-09
NZ719149A (en) 2019-09-27
HUE040208T2 (hu) 2019-02-28
KR102248450B1 (ko) 2021-05-06
UA116042C2 (uk) 2018-01-25
EP3059239A1 (en) 2016-08-24
PT3059239T (pt) 2018-10-09
DK3059239T3 (en) 2018-08-13
BR112016008654A2 (ru) 2017-08-01
SG11201602926UA (en) 2016-05-30
SA516370956B1 (ar) 2019-04-04
CY1120880T1 (el) 2020-05-29
CN105636965B (zh) 2017-11-24
US9642852B2 (en) 2017-05-09
TW201607951A (zh) 2016-03-01
HK1220192A1 (zh) 2017-04-28
AU2014335304B2 (en) 2018-03-01
EP3059239A4 (en) 2017-04-26
US20150111876A1 (en) 2015-04-23
IL244953B (en) 2019-01-31

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