EA200300333A1 - Новые тиадиазолы и оксадиазолы и их применение в качестве ингибиторов фосфодиэстеразы-7 - Google Patents

Новые тиадиазолы и оксадиазолы и их применение в качестве ингибиторов фосфодиэстеразы-7

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Publication number
EA200300333A1
EA200300333A1 EA200300333A EA200300333A EA200300333A1 EA 200300333 A1 EA200300333 A1 EA 200300333A1 EA 200300333 A EA200300333 A EA 200300333A EA 200300333 A EA200300333 A EA 200300333A EA 200300333 A1 EA200300333 A1 EA 200300333A1
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EA
Eurasian Patent Office
Prior art keywords
heterocycloalkyl
oxadiazoles
cycloalkyl
aryl
tiadiazoles
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EA200300333A
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English (en)
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EA007179B1 (ru
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Фабрис Вернье
Пьер Дюкро
Шарль Андрианжара
Патрик Бернарделли
Эдвиж Лортиуа
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УОРНЕР-ЛАМБЕРТ КОМПАНИ Эл-Эл-Си
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Publication of EA200300333A1 publication Critical patent/EA200300333A1/ru
Publication of EA007179B1 publication Critical patent/EA007179B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D285/00Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01Five-membered rings
    • C07D285/02Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/121,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C07D285/1251,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • C07D285/135Nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • 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
    • C07D417/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D453/00Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Virology (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Transplantation (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Neurology (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

Abstract

Согласно изобретению предложены 1,3,4-тиадиазолы и 1,3,4-оксадиазолы, имеющие формулу (I), в которой Y представляет собой S или O, R1 представляет собой алкил, алкенил, алкинил, циклоалкил, гетероциклоалкил, циклоалкенил, арил, гетероарил или полициклическую группу, возможно замещенные, R2 представляет собой алкил, алкенил, алкинил, циклоалкил, гетероциклоалкил, циклоалкенил или арил, возможно замещенные, R3 представляет собой X-R'3, где Xявляется связывающей группой, a R'3 представляет собой циклоалкил, гетероциклоалкил, цикпоалкенил, арил, гетероарил или полициклическую группу, возможно замещенные, или их фармацевтически приемлемые производные, способ их получения и их применение для производства лекарственного средства для лечения расстройств, для лечения которых релевантным является лечение ингибитором ФДЭ7.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200300333A 2000-10-02 2001-10-01 Тиадиазолы и оксадиазолы и их применение в качестве ингибиторов фосфодиэстеразы-7 EA007179B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP00402710A EP1193261A1 (en) 2000-10-02 2000-10-02 New thiadiazoles and their use as phosphodiesterase-7 inhibitors
PCT/EP2001/011330 WO2002028847A1 (en) 2000-10-02 2001-10-01 New thiadiazoles and oxadiazoles and their use as phosphodiesterase-7 inhibitors

Publications (2)

Publication Number Publication Date
EA200300333A1 true EA200300333A1 (ru) 2003-10-30
EA007179B1 EA007179B1 (ru) 2006-08-25

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EA200300333A EA007179B1 (ru) 2000-10-02 2001-10-01 Тиадиазолы и оксадиазолы и их применение в качестве ингибиторов фосфодиэстеразы-7

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US (1) US7122565B2 (ru)
EP (2) EP1193261A1 (ru)
JP (1) JP4177098B2 (ru)
KR (1) KR100614158B1 (ru)
CN (1) CN1639141A (ru)
AP (1) AP1541A (ru)
AR (1) AR035347A1 (ru)
AT (1) ATE304003T1 (ru)
AU (2) AU2001289945B2 (ru)
BG (1) BG107654A (ru)
BR (1) BR0114391A (ru)
CA (1) CA2424279A1 (ru)
CZ (1) CZ2003857A3 (ru)
DE (1) DE60113283T2 (ru)
DK (1) DK1326853T3 (ru)
DZ (1) DZ3440A1 (ru)
EA (1) EA007179B1 (ru)
EC (1) ECSP034534A (ru)
EE (1) EE200300134A (ru)
ES (1) ES2247166T3 (ru)
GE (1) GEP20053459B (ru)
GT (1) GT200100196A (ru)
HN (1) HN2001000217A (ru)
HR (1) HRP20030247A2 (ru)
HU (1) HUP0301248A3 (ru)
IL (1) IL155122A0 (ru)
IS (1) IS6759A (ru)
MA (1) MA25916A1 (ru)
MX (1) MXPA03002839A (ru)
NO (1) NO20031482D0 (ru)
NZ (1) NZ524852A (ru)
OA (1) OA12518A (ru)
PA (1) PA8529501A1 (ru)
PE (1) PE20020419A1 (ru)
PL (1) PL366332A1 (ru)
PT (1) PT1326853E (ru)
SI (1) SI1326853T1 (ru)
SK (1) SK3812003A3 (ru)
SV (1) SV2003000633A (ru)
TN (1) TNSN01139A1 (ru)
WO (1) WO2002028847A1 (ru)
YU (1) YU24503A (ru)
ZA (1) ZA200302346B (ru)

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AU2003282087A1 (en) * 2002-11-13 2004-06-03 Bayer Healthcare Ag DIAGNOSTICS AND THERAPEUTICS FOR DISEASES ASSOCIATED WITH HUMAN PHOSPHODIESTERASE 7A1 (PDE7a1)
ES2217956B1 (es) * 2003-01-23 2006-04-01 Almirall Prodesfarma, S.A. Nuevos derivados de 4-aminotieno(2,3-d)pirimidin-6-carbonitrilo.
JP2006219373A (ja) 2003-06-13 2006-08-24 Daiichi Asubio Pharma Co Ltd Pde7阻害作用を有するピリジニルピラゾロピリミジノン誘導体
JP2006219374A (ja) 2003-06-13 2006-08-24 Daiichi Asubio Pharma Co Ltd Pde7阻害作用を有するイミダゾトリアジノン誘導体
DK1775298T3 (da) 2004-07-01 2013-05-21 Daiichi Sankyo Co Ltd Thienopyrazolderivat med PDE7-inhibitorisk aktivitet
WO2007025177A2 (en) 2005-08-26 2007-03-01 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
EP2258359A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis by muscarinic receptor modulation with sabcomelin
WO2007047978A2 (en) 2005-10-21 2007-04-26 Braincells, Inc. Modulation of neurogenesis by pde inhibition
US20070112017A1 (en) 2005-10-31 2007-05-17 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
JP2009536669A (ja) 2006-05-09 2009-10-15 ブレインセルス,インコーポレイティド アンジオテンシン調節による神経新生
EP2026813A2 (en) 2006-05-09 2009-02-25 Braincells, Inc. 5 ht receptor mediated neurogenesis
BRPI0716604A2 (pt) 2006-09-08 2013-04-09 Braincells Inc combinaÇÕes contendo um derivado de 4-acilaminopiridina
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MD3995C2 (ru) * 2009-05-11 2010-07-31 Государственный Университет Молд0 Использование ди(µ-Oфенокси)-ди{[2-(4-аминобензолсульфамидо)-5-этил-1,3,4-тиадиазол]-3,5-дибромсалицилидентиосемикарбазоната(-1) меди} в качестве ингибитора роста и размножения клеток Т-47D рака молочной железы
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US9220715B2 (en) 2010-11-08 2015-12-29 Omeros Corporation Treatment of addiction and impulse-control disorders using PDE7 inhibitors
NZ628055A (en) 2010-11-08 2016-03-31 Omeros Corp Treatment of addiction and impulse-control disorders using pde7 inhibitors
CN102276625B (zh) * 2011-08-24 2013-07-17 天津药物研究院 噻二唑衍生物
US20150119399A1 (en) 2012-01-10 2015-04-30 President And Fellows Of Harvard College Beta-cell replication promoting compounds and methods of their use
CN103288777A (zh) * 2013-05-28 2013-09-11 浙江禾田化工有限公司 特丁噻草隆关键中间体2-甲基氨基-5-叔丁基-1,3,4-噻二唑的合成方法
US9416652B2 (en) 2013-08-08 2016-08-16 Vetco Gray Inc. Sensing magnetized portions of a wellhead system to monitor fatigue loading
US20180284095A1 (en) * 2015-06-12 2018-10-04 Oryzon Genomics, S.A. Biomarkers associated with lsd1 inhibitors and uses thereof
CN107674042B (zh) * 2017-09-28 2020-09-25 河南科技大学 一种超声波无溶剂合成噻二唑类化合物的方法
CN113480486B (zh) * 2021-07-30 2022-05-24 赣南师范大学 一种3-胺基-1,2,4-三唑类衍生物及其制备方法和应用
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Publication number Publication date
BG107654A (bg) 2003-12-31
DZ3440A1 (fr) 2002-04-11
EP1326853B1 (en) 2005-09-07
DE60113283D1 (de) 2005-10-13
HRP20030247A2 (en) 2005-04-30
US7122565B2 (en) 2006-10-17
PA8529501A1 (es) 2003-06-30
TNSN01139A1 (en) 2005-11-10
AP2003002764A0 (en) 2003-03-31
EA007179B1 (ru) 2006-08-25
AR035347A1 (es) 2004-05-12
WO2002028847A1 (en) 2002-04-11
DE60113283T2 (de) 2006-06-08
ES2247166T3 (es) 2006-03-01
AP1541A (en) 2006-01-11
SV2003000633A (es) 2003-04-03
ATE304003T1 (de) 2005-09-15
PE20020419A1 (es) 2002-07-18
MA25916A1 (fr) 2003-10-01
AU2001289945B2 (en) 2005-12-22
KR100614158B1 (ko) 2006-08-21
CZ2003857A3 (cs) 2004-02-18
ECSP034534A (es) 2003-07-25
HUP0301248A2 (hu) 2003-10-28
HUP0301248A3 (en) 2005-06-28
NO20031482L (no) 2003-04-01
AU8994501A (en) 2002-04-15
BR0114391A (pt) 2003-06-24
EP1326853A1 (en) 2003-07-16
US20030045557A1 (en) 2003-03-06
NZ524852A (en) 2004-09-24
PL366332A1 (en) 2005-01-24
EE200300134A (et) 2003-08-15
GEP20053459B (en) 2005-02-25
NO20031482D0 (no) 2003-04-01
IS6759A (is) 2003-03-27
PT1326853E (pt) 2005-11-30
SI1326853T1 (sl) 2005-12-31
CN1639141A (zh) 2005-07-13
JP2004510769A (ja) 2004-04-08
CA2424279A1 (en) 2002-04-11
EP1193261A1 (en) 2002-04-03
SK3812003A3 (en) 2004-05-04
YU24503A (sh) 2006-03-03
OA12518A (en) 2006-05-29
IL155122A0 (en) 2003-10-31
DK1326853T3 (da) 2005-12-12
JP4177098B2 (ja) 2008-11-05
KR20030068542A (ko) 2003-08-21
MXPA03002839A (es) 2004-09-10
ZA200302346B (en) 2004-08-04
HN2001000217A (es) 2002-06-13
GT200100196A (es) 2002-07-18

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