PE20120432A1 - Compuestos biciclicos y triciclicos como inhibidores de kat ii - Google Patents

Compuestos biciclicos y triciclicos como inhibidores de kat ii

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Publication number
PE20120432A1
PE20120432A1 PE2011002106A PE2011002106A PE20120432A1 PE 20120432 A1 PE20120432 A1 PE 20120432A1 PE 2011002106 A PE2011002106 A PE 2011002106A PE 2011002106 A PE2011002106 A PE 2011002106A PE 20120432 A1 PE20120432 A1 PE 20120432A1
Authority
PE
Peru
Prior art keywords
kat
inhibitors
hydroxy
amino
alkyl
Prior art date
Application number
PE2011002106A
Other languages
English (en)
Inventor
Michelle Marie Claffey
Amy Beth Dounay
Xinmin Gan
Mathew Merrill Hayward
Suobao Rong
Jamison Bryce Tuttle
Patrick Robert Verhoest
Original Assignee
Pfizer
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 Pfizer filed Critical Pfizer
Publication of PE20120432A1 publication Critical patent/PE20120432A1/es

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    • 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
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    • 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
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    • A61P25/20—Hypnotics; Sedatives
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • 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
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    • 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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    • 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)
  • Veterinary Medicine (AREA)
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  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Neurology (AREA)
  • Biomedical Technology (AREA)
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  • Pain & Pain Management (AREA)
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  • Gastroenterology & Hepatology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

REFERIDA A UN COMPUESTO HETEROCICLICO DE FORMULA (X), DONDE A ES N O CR1; X ES N O CR2; Y ES N O CR3; Z ES N O CR4; R1 ES H, ALQUILO C1-C10, ALCOXI C1-C10, CICLOPROPILO; R2, R3 Y R4 SON H, HALOGENO, ALQUILO C1-C10, ALCOXI C1-C10, ENTRE OTROS; R5 ES H, C(=O)R9, C(=O)OR9, ENTRE OTROS; R6a Y R6b SON H, METILO, F, HALOMETILO, ENTRE OTROS; R9 ES ALQUILO C1-C10, CICLALQUILO C6-C10, ARILO C6-C18, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 3-AMINO-7-CLORO-1-HIDROXI-3,4-DIHIDROQUINOLIN-2(1H)-ONA, 3-AMINO-1-HIDROXI-7-METIL-3,4-DIHIDROQUINOLIN-2(1H)-ONA, 3-AMINO-6-CLORO-1-HIDROXI-8-(TRIFLUOROMETIL)-3,4-DIHIDROQUINOLIN-2(1H)-ONA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA ENZIMA QUINURENINA AMINOTRANSFERASA II (KAT II) Y SON UTILES EN EL TRATAMIENTO DE DEFICITS COGNITIVOS ASOCIADOS A LA ESQUIZOFRENIA Y OTROS TRASTORNOS NEURODEGENERATIVOS Y/O NEUROLOGICOS
PE2011002106A 2009-06-18 2010-05-26 Compuestos biciclicos y triciclicos como inhibidores de kat ii PE20120432A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US21814909P 2009-06-18 2009-06-18
US33438910P 2010-05-13 2010-05-13

Publications (1)

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PE20120432A1 true PE20120432A1 (es) 2012-05-05

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PE2011002106A PE20120432A1 (es) 2009-06-18 2010-05-26 Compuestos biciclicos y triciclicos como inhibidores de kat ii

Country Status (28)

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

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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
KR102458990B1 (ko) 2014-04-23 2022-10-25 미쓰비시 타나베 파마 코퍼레이션 신규한 바이시클릭 또는 트리시클릭 헤테로시클릭 화합물
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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JPH0881443A (ja) * 1994-09-12 1996-03-26 Otsuka Pharmaceut Co Ltd 細胞外マトリックス金属プロテアーゼ阻害剤
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
EP1002535A1 (en) * 1998-10-28 2000-05-24 Hrissanthi Ikonomidou New use of glutamate antagonists for the treatment of cancer
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

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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
EA201190287A1 (ru) 2012-06-29
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
DK2443092T3 (en) 2015-04-27
JP5643818B2 (ja) 2014-12-17
AU2010261399A1 (en) 2012-01-12

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