EA201190287A1 - Бициклические и трициклические соединения в качестве ингибиторов kat ii - Google Patents

Бициклические и трициклические соединения в качестве ингибиторов kat ii

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Publication number
EA201190287A1
EA201190287A1 EA201190287A EA201190287A EA201190287A1 EA 201190287 A1 EA201190287 A1 EA 201190287A1 EA 201190287 A EA201190287 A EA 201190287A EA 201190287 A EA201190287 A EA 201190287A EA 201190287 A1 EA201190287 A1 EA 201190287A1
Authority
EA
Eurasian Patent Office
Prior art keywords
kat
bicyclic
inhibitors
tricyclic compounds
compounds
Prior art date
Application number
EA201190287A
Other languages
English (en)
Inventor
Майкл Мэри Клэффи
Эми Бет Доунэй
Синминь Гань
Мэттью Меррилл Хэйуорд
Суобао Рон
Джеймисон Брюс Туттл
Патрик Роберт Верхоэст
Original Assignee
Пфайзер Инк.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Пфайзер Инк. filed Critical Пфайзер Инк.
Publication of EA201190287A1 publication Critical patent/EA201190287A1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/58—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems with hetero atoms directly attached to the ring nitrogen atom
    • C07D215/60—N-oxides
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P13/10—Drugs for disorders of the urinary system of the bladder
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    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Otolaryngology (AREA)
  • Oncology (AREA)
  • Addiction (AREA)
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  • Anesthesiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Communicable Diseases (AREA)
  • Dermatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Соединения формулы X, где А, X, Y, Z, R, Rи Rтакие, как они определены в данном описании, и их фармацевтически приемлемые соли описаны как полезные для лечения когнитивных дефицитов, ассоциированных с шизофренией, и других нейродегенеративных и/или неврологических расстройств у млекопитающих, в том числе людей.
EA201190287A 2009-06-18 2010-05-26 Бициклические и трициклические соединения в качестве ингибиторов kat ii EA201190287A1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US21814909P 2009-06-18 2009-06-18
US33438910P 2010-05-13 2010-05-13
PCT/IB2010/052349 WO2010146488A1 (en) 2009-06-18 2010-05-26 Bicyclic and tricyclic compounds as kat ii inhibitors

Publications (1)

Publication Number Publication Date
EA201190287A1 true EA201190287A1 (ru) 2012-06-29

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US (1) US8183238B2 (ru)
EP (1) EP2443092B1 (ru)
JP (1) JP5643818B2 (ru)
KR (1) KR101390023B1 (ru)
CN (1) CN102482221B (ru)
AP (1) AP2012006071A0 (ru)
AR (1) AR077147A1 (ru)
AU (1) AU2010261399B2 (ru)
BR (1) BRPI1011784A2 (ru)
CA (1) CA2763960C (ru)
CO (1) CO6470895A2 (ru)
CR (1) CR20110625A (ru)
CU (1) CU20110234A7 (ru)
DK (1) DK2443092T3 (ru)
DO (1) DOP2011000381A (ru)
EA (1) EA201190287A1 (ru)
EC (1) ECSP11011539A (ru)
ES (1) ES2538386T3 (ru)
HK (1) HK1166980A1 (ru)
IL (1) IL216603A (ru)
MA (1) MA33407B1 (ru)
MX (1) MX2011013870A (ru)
PE (1) PE20120432A1 (ru)
SG (1) SG176288A1 (ru)
TW (1) TW201100082A (ru)
UY (1) UY32712A (ru)
WO (1) WO2010146488A1 (ru)
ZA (1) ZA201108964B (ru)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2702113C2 (ru) * 2014-04-23 2019-10-04 Мицубиси Танабе Фарма Корпорейшн Новое бициклическое или трициклическое гетероциклическое соединение

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CA2819106C (en) * 2010-12-01 2015-12-29 Pfizer Inc. Kat ii inhibitors
MX2013005773A (es) * 2010-12-01 2013-06-18 Pfizer Inhibidores de kat ii.
CN103796986B (zh) * 2011-07-07 2015-08-19 庵原化学工业株式会社 硝基苯化合物的制备方法
RU2014146509A (ru) * 2012-06-15 2016-08-10 Пфайзер Инк. Ингибиторы кат ii
JP6440625B2 (ja) 2012-11-14 2018-12-19 ザ・ジョンズ・ホプキンス・ユニバーシティー 精神分裂病を処置するための方法および組成物
EP2746250B1 (en) * 2012-12-21 2017-09-27 ABX Advanced Biochemical Compounds GmbH Precursors and process for the production of 18F-labelled amino acids
JPWO2014174745A1 (ja) * 2013-04-26 2017-02-23 国立大学法人京都大学 Ｅｇ５阻害剤
CN104592333B (zh) * 2014-07-23 2017-06-27 江西科技师范大学 一种合成5‑羧基‑2’‑脱氧胞苷的方法
US10793582B2 (en) 2015-10-22 2020-10-06 Mitsubishi Tanabe Pharma Corporation Bicyclic heterocyclic compound
GB201613163D0 (en) * 2016-07-29 2016-09-14 Autifony Therapeutics Ltd Novel compounds
WO2018155260A1 (ja) * 2017-02-23 2018-08-30 株式会社Ihi Ｏｈラジカル検出プローブ、ｏｈラジカル測定装置、および、ｏｈラジカル測定方法
US11911376B2 (en) 2020-03-30 2024-02-27 The Regents Of The University Of Colorado Methods for preventing and treating retinal damage
CN115872970A (zh) * 2022-12-08 2023-03-31 青岛普力机电工程有限公司 一种从乳酸原料到高纯丙交酯连续生产的方法

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US5801183A (en) * 1995-01-27 1998-09-01 State Of Oregon, Acting By And Through The Oregon State Board Of Higher Education, Acting For And On Behalf Of The Oregon Health Sciences University And The University Of Oregon Aza and aza (N-oxy) analogs of glycine/NMDA receptor antagonists
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WO2005007628A1 (en) * 2003-07-11 2005-01-27 Bristol-Myers Squibb Company Tetrahydroquinoline derivatives as cannabinoid receptor modulators
GT200500186A (es) 2004-07-07 2006-03-02 Regimenes anticonceptivos con antagonistas del receptor de progesterona y kits
US20100273787A1 (en) * 2007-11-15 2010-10-28 Robert Schwarcz Kynurenine-aminotransferase inhibitors

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2702113C2 (ru) * 2014-04-23 2019-10-04 Мицубиси Танабе Фарма Корпорейшн Новое бициклическое или трициклическое гетероциклическое соединение

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JP2012530129A (ja) 2012-11-29
BRPI1011784A2 (pt) 2016-03-22
CO6470895A2 (es) 2012-06-29
EP2443092A1 (en) 2012-04-25
UY32712A (es) 2011-01-31
AR077147A1 (es) 2011-08-03
CR20110625A (es) 2012-02-24
CN102482221A (zh) 2012-05-30
CN102482221B (zh) 2014-10-22
AP2012006071A0 (en) 2012-02-29
ZA201108964B (en) 2012-08-29
CA2763960A1 (en) 2010-12-23
ECSP11011539A (es) 2012-01-31
ES2538386T3 (es) 2015-06-19
US20100324043A1 (en) 2010-12-23
KR101390023B1 (ko) 2014-04-29
CA2763960C (en) 2014-07-08
HK1166980A1 (en) 2012-11-16
IL216603A0 (en) 2012-02-29
AU2010261399B2 (en) 2014-07-17
SG176288A1 (en) 2012-01-30
IL216603A (en) 2015-07-30
CU20110234A7 (es) 2012-06-21
TW201100082A (en) 2011-01-01
DOP2011000381A (es) 2012-02-29
KR20120027480A (ko) 2012-03-21
WO2010146488A1 (en) 2010-12-23
MA33407B1 (fr) 2012-07-03
MX2011013870A (es) 2012-02-01
EP2443092B1 (en) 2015-04-08
US8183238B2 (en) 2012-05-22
PE20120432A1 (es) 2012-05-05
DK2443092T3 (en) 2015-04-27
JP5643818B2 (ja) 2014-12-17
AU2010261399A1 (en) 2012-01-12

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