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BG106520A - Заместени n-фенил 2-хидрокси-2-метил-3,3,3-трифлуоропропанамидни производни, които повишават активността на пируват дехидрогеназа - Google Patents

Заместени n-фенил 2-хидрокси-2-метил-3,3,3-трифлуоропропанамидни производни, които повишават активността на пируват дехидрогеназа

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Publication number
BG106520A
BG106520A BG106520A BG10652002A BG106520A BG 106520 A BG106520 A BG 106520A BG 106520 A BG106520 A BG 106520A BG 10652002 A BG10652002 A BG 10652002A BG 106520 A BG106520 A BG 106520A
Authority
BG
Bulgaria
Prior art keywords
methyl
hydroxy
phenyl
substituted
dehydrogenase activity
Prior art date
Application number
BG106520A
Other languages
English (en)
Other versions
BG65099B1 (bg
Inventor
Roger Butlin
Janet Pease
Michael Block
Thorsten Nowak
Jeremy Burrows
Original Assignee
Astrazeneca Ab
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
Priority claimed from GBGB9920814.2A external-priority patent/GB9920814D0/en
Priority claimed from GB0006641A external-priority patent/GB0006641D0/en
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of BG106520A publication Critical patent/BG106520A/bg
Publication of BG65099B1 publication Critical patent/BG65099B1/bg
Anticipated expiration legal-status Critical
Active legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182Radicals derived from carboxylic acids
    • C07D295/185Radicals derived from carboxylic acids from aliphatic carboxylic acids
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12Antidiuretics, e.g. drugs for diabetes insipidus
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00Sulfones; Sulfoxides
    • C07C317/26Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C317/32Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C07C317/34Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring
    • C07C317/38Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring with the nitrogen atom of at least one amino group being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfones
    • C07C317/42Y being a hetero atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00Sulfones; Sulfoxides
    • C07C317/44Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00Sulfones; Sulfoxides
    • C07C317/44Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C07C317/48Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C317/50Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/64Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton
    • C07C323/65Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton containing sulfur atoms of sulfone or sulfoxide groups bound to the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/135Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Neurosurgery (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)
  • Pyrrole Compounds (AREA)

Abstract

Изобретението се отнася до съединение с формула, в която n има стойност 1 или 2, R1 е хлор, флуор, бром, метил или метокси, R2 и R3 имат значенията, посочени в описанието, и R4 е водород или флуор, или до негова фармацевтично приемлива сол или in vivo хидролизиращ се естер. Изобретението се отнася и до използването на съединенията с формула I за усилване на PDH-активност в топлокръвни бозайници, например човек. Изброени са подробно фармацевтичнисъстави, методи и процеси за получаване на съединения с посочената формула.
BG106520A 1999-09-04 2002-03-14 Заместени n-фенил 2-хидрокси-2-метил-3,3,3-трифлуоропропанамидни производни, които повишават активността на пируват дехидрогеназа Active BG65099B1 (bg)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9920814.2A GB9920814D0 (en) 1999-09-04 1999-09-04 Chemical compounds
GB0006641A GB0006641D0 (en) 2000-03-21 2000-03-21 Chemical compounds

Publications (2)

Publication Number Publication Date
BG106520A true BG106520A (bg) 2003-03-31
BG65099B1 BG65099B1 (bg) 2007-02-28

Family

ID=26243905

Family Applications (1)

Application Number Title Priority Date Filing Date
BG106520A Active BG65099B1 (bg) 1999-09-04 2002-03-14 Заместени n-фенил 2-хидрокси-2-метил-3,3,3-трифлуоропропанамидни производни, които повишават активността на пируват дехидрогеназа

Country Status (32)

Country Link
US (1) US6689909B1 (bg)
EP (1) EP1214296B1 (bg)
JP (1) JP2003508515A (bg)
KR (1) KR100692232B1 (bg)
CN (1) CN1235877C (bg)
AR (1) AR035163A1 (bg)
AT (1) ATE262507T1 (bg)
AU (1) AU760061B2 (bg)
BG (1) BG65099B1 (bg)
BR (1) BR0013694A (bg)
CA (1) CA2381581A1 (bg)
CO (1) CO5190690A1 (bg)
CZ (1) CZ2002773A3 (bg)
DE (1) DE60009319T2 (bg)
DK (1) DK1214296T3 (bg)
EE (1) EE05080B1 (bg)
ES (1) ES2216940T3 (bg)
HK (1) HK1045496B (bg)
HU (1) HUP0202725A3 (bg)
IL (2) IL148111A0 (bg)
IS (1) IS2069B (bg)
MX (1) MXPA02002319A (bg)
MY (1) MY127036A (bg)
NO (1) NO20021040L (bg)
NZ (1) NZ517147A (bg)
PL (1) PL353887A1 (bg)
PT (1) PT1214296E (bg)
RU (1) RU2255085C2 (bg)
SK (1) SK286774B6 (bg)
TR (1) TR200200550T2 (bg)
TW (1) TW577867B (bg)
WO (1) WO2001017956A1 (bg)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE399753T1 (de) 1999-09-04 2008-07-15 Astrazeneca Ab Amide als pyruvatdehydrogenaseinhibitoren
GB0012012D0 (en) * 2000-05-19 2000-07-05 Astrazeneca Ab Chemical compound
GB0120471D0 (en) * 2001-08-23 2001-10-17 Astrazeneca Ab Chemical compounds
JP4329905B2 (ja) * 2001-12-27 2009-09-09 第一三共株式会社 βアミロイド蛋白産生・分泌阻害剤
US9388164B2 (en) 2011-05-03 2016-07-12 Agios Pharmaceuticals, Inc Methods of using pyruvate kinase activators
EA032007B1 (ru) 2012-11-08 2019-03-29 Аджиос Фармасьютикалз, Инк. Терапевтические соединения и композиции и их использование в качестве модуляторов пк-m2
WO2014139144A1 (en) 2013-03-15 2014-09-18 Agios Pharmaceuticals, Inc. Therapeutic compounds and compositions
DK3668512T3 (da) 2017-08-15 2023-05-22 Agios Pharmaceuticals Inc Pyruvatkinasemodulatorer og anvendelse deraf
CN109096186B (zh) * 2018-09-29 2020-08-04 中南大学 一种2-芳磺酰基喹啉衍生物的合成方法
KR20240055793A (ko) * 2021-09-01 2024-04-29 니뽄 다바코 산교 가부시키가이샤 질소 함유 3환성 화합물 및 그 의약 용도

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EP0002309B1 (en) 1977-10-12 1982-12-01 Imperial Chemical Industries Plc Acylanilides, process for their manufacture and pharmaceutical and veterinary compositions containing them
US4191775A (en) 1977-12-15 1980-03-04 Imperial Chemical Industries Limited Amide derivatives
NZ197008A (en) 1980-05-22 1984-10-19 Ici Ltd Acylanilide derivatives and pharmaceutical compositions
AU8961382A (en) 1981-11-06 1983-05-12 Imperial Chemical Industries Plc Amide derivatives
US4537618A (en) 1982-05-26 1985-08-27 Ciba Geigy Corporation N-phenylsulfonyl-N'-pyrimidinylureas
DE3372965D1 (en) 1982-07-23 1987-09-17 Ici Plc Amide derivatives
GB8617652D0 (en) 1986-07-18 1986-08-28 Ici Plc Acylanilide derivatives
GB8617653D0 (en) 1986-07-18 1986-08-28 Ici Plc Amide derivatives
GB9214120D0 (en) 1991-07-25 1992-08-12 Ici Plc Therapeutic amides
EP0539329A1 (de) 1991-10-25 1993-04-28 Ciba-Geigy Ag Acetylen-Verbindungen, verwendbar als Leukotrien-Antagonisten
SE9103397D0 (sv) 1991-11-18 1991-11-18 Kabi Pharmacia Ab Nya substituerade salicylsyror
IL105558A (en) 1992-05-18 1998-04-05 Zeneca Ltd Tertiary carbinols with channel activity potassium process for their preparation and pharmaceutical preparations containing them
GB9305295D0 (en) * 1993-03-15 1993-05-05 Zeneca Ltd Therapeutic compounds
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GB9310069D0 (en) 1993-05-17 1993-06-30 Zeneca Ltd Heterocyclic compounds
GB9310095D0 (en) 1993-05-17 1993-06-30 Zeneca Ltd Therapeutic compounds
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GB9805520D0 (en) 1998-03-17 1998-05-13 Zeneca Ltd Chemical compounds
GB9811427D0 (en) 1998-05-29 1998-07-22 Zeneca Ltd Chemical compounds

Also Published As

Publication number Publication date
DE60009319T2 (de) 2005-03-31
JP2003508515A (ja) 2003-03-04
IL148111A0 (en) 2002-09-12
MY127036A (en) 2006-11-30
CO5190690A1 (es) 2002-08-29
BG65099B1 (bg) 2007-02-28
TW577867B (en) 2004-03-01
RU2002108508A (ru) 2004-01-20
AU760061B2 (en) 2003-05-08
KR20020067498A (ko) 2002-08-22
ATE262507T1 (de) 2004-04-15
IS2069B (is) 2005-11-15
KR100692232B1 (ko) 2007-03-09
BR0013694A (pt) 2002-05-21
PL353887A1 (en) 2003-12-15
CN1235877C (zh) 2006-01-11
DE60009319D1 (de) 2004-04-29
EE200200113A (et) 2003-06-16
SK286774B6 (sk) 2009-05-07
EP1214296A1 (en) 2002-06-19
EE05080B1 (et) 2008-10-15
WO2001017956A1 (en) 2001-03-15
RU2255085C2 (ru) 2005-06-27
PT1214296E (pt) 2004-08-31
CA2381581A1 (en) 2001-03-15
NO20021040D0 (no) 2002-03-01
US6689909B1 (en) 2004-02-10
HK1045496B (zh) 2004-10-21
MXPA02002319A (es) 2002-07-30
ES2216940T3 (es) 2004-11-01
SK3002002A3 (en) 2002-07-02
NO20021040L (no) 2002-05-02
CZ2002773A3 (cs) 2002-06-12
AR035163A1 (es) 2004-05-05
CN1387509A (zh) 2002-12-25
NZ517147A (en) 2003-11-28
HUP0202725A3 (en) 2005-04-28
DK1214296T3 (da) 2004-07-05
EP1214296B1 (en) 2004-03-24
HUP0202725A2 (hu) 2003-01-28
IS6285A (is) 2002-02-26
TR200200550T2 (tr) 2002-06-21
HK1045496A1 (en) 2002-11-29
AU6854300A (en) 2001-04-10
IL148111A (en) 2007-05-15

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