CN1235877C - 升高丙酮酸脱氢酶活性的取代的n－苯基2－羟基－2－甲基－3,3,3－三氟代丙酰胺衍生物 - Google Patents

升高丙酮酸脱氢酶活性的取代的n－苯基2－羟基－2－甲基－3,3,3－三氟代丙酰胺衍生物 Download PDF

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Publication number
CN1235877C
CN1235877C CNB008152446A CN00815244A CN1235877C CN 1235877 C CN1235877 C CN 1235877C CN B008152446 A CNB008152446 A CN B008152446A CN 00815244 A CN00815244 A CN 00815244A CN 1235877 C CN1235877 C CN 1235877C
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CN
China
Prior art keywords
hydroxy
optionally substituted
methyl
phenyl
trifluoropropionamide
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Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CNB008152446A
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English (en)
Chinese (zh)
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CN1387509A (zh
Inventor
R·J·布特林
J·E·佩斯
M·H·布洛克
T·诺瓦克
J·N·布罗斯
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AstraZeneca AB
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AstraZeneca AB
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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 CN1387509A publication Critical patent/CN1387509A/zh
Application granted granted Critical
Publication of CN1235877C publication Critical patent/CN1235877C/zh
Anticipated expiration legal-status Critical
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic 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
    • C07D295/16—Heterocyclic 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
    • C07D295/18—Heterocyclic 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
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C317/32—Sulfones; 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
    • C07C317/34—Sulfones; 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
    • C07C317/38—Sulfones; 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
    • C07C317/42—Y being a hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C07C317/48—Sulfones; 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
    • C07C317/50—Sulfones; 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/64—Thiols, 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
    • C07C323/65—Thiols, 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic 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
    • C07D295/04—Heterocyclic 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
    • C07D295/12—Heterocyclic 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
    • C07D295/135—Heterocyclic 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (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)
CNB008152446A 1999-09-04 2000-08-30 升高丙酮酸脱氢酶活性的取代的n－苯基2－羟基－2－甲基－3,3,3－三氟代丙酰胺衍生物 Expired - Fee Related CN1235877C (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB9920814.2 1999-09-04
GBGB9920814.2A GB9920814D0 (en) 1999-09-04 1999-09-04 Chemical compounds
GB0006641A GB0006641D0 (en) 2000-03-21 2000-03-21 Chemical compounds
GB0006641.5 2000-03-21

Publications (2)

Publication Number Publication Date
CN1387509A CN1387509A (zh) 2002-12-25
CN1235877C true CN1235877C (zh) 2006-01-11

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CNB008152446A Expired - Fee Related CN1235877C (zh) 1999-09-04 2000-08-30 升高丙酮酸脱氢酶活性的取代的n－苯基2－羟基－2－甲基－3,3,3－三氟代丙酰胺衍生物

Country Status (32)

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

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003508509A (ja) 1999-09-04 2003-03-04 アストラゼネカ アクチボラグ ピルビン酸デヒドロゲナーゼの阻害剤としてのアミド
GB0012012D0 (en) * 2000-05-19 2000-07-05 Astrazeneca Ab Chemical compound
GB0120471D0 (en) * 2001-08-23 2001-10-17 Astrazeneca Ab Chemical compounds
WO2003055850A1 (en) * 2001-12-27 2003-07-10 Daiichi Pharmaceutical Co., Ltd. β-AMYLOID PROTEIN PRODUCTION/SECRETION INHIBITORS
WO2012151448A1 (en) * 2011-05-03 2012-11-08 Agios Pharmaceuticals, Inc. Pyruvate kinase activators for use in therapy
US9458132B2 (en) 2012-11-08 2016-10-04 Agios Pharmaceuticals, Inc Therapeutic compounds and compositions and their use as PKM2 modulators
WO2014139144A1 (en) 2013-03-15 2014-09-18 Agios Pharmaceuticals, Inc. Therapeutic compounds and compositions
MX2020001832A (es) 2017-08-15 2020-07-22 Agios Pharmaceuticals Inc Activadores de piruvato quinasas para usar en el tratamiento de trastornos en la sangre.
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
CA3228249A1 (en) * 2021-09-01 2023-03-09 Maki YAMAKAWA Nitrogen-containing tricyclic compound and pharmaceutical use thereof

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DE2862100D1 (en) 1977-10-12 1983-01-05 Ici 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
LU88769I2 (fr) 1982-07-23 1996-11-05 Zeneca Ltd Bicalutamide et ses sels et esters pharmaceutiquement acceptables (Casodex (R))
GB8617653D0 (en) 1986-07-18 1986-08-28 Ici Plc Amide derivatives
GB8617652D0 (en) 1986-07-18 1986-08-28 Ici Plc Acylanilide derivatives
GB9214120D0 (en) * 1991-07-25 1992-08-12 Ici Plc Therapeutic amides
GB9116069D0 (en) * 1991-07-25 1991-09-11 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 having potassium channel activity, process for their preparation and pharmaceutical compositions containing them
GB9305295D0 (en) * 1993-03-15 1993-05-05 Zeneca Ltd Therapeutic compounds
GB9309716D0 (en) 1993-05-12 1993-06-23 Zeneca Ltd Heterocyclic derivatives
GB9310095D0 (en) 1993-05-17 1993-06-30 Zeneca Ltd Therapeutic compounds
GB9310069D0 (en) 1993-05-17 1993-06-30 Zeneca Ltd Heterocyclic compounds
GB2278054A (en) * 1993-05-18 1994-11-23 Zeneca Ltd Compounds for the treatment of urinary incontinence
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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

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CO5190690A1 (es) 2002-08-29
MXPA02002319A (es) 2002-07-30
NO20021040L (no) 2002-05-02
HK1045496B (en) 2004-10-21
ES2216940T3 (es) 2004-11-01
RU2255085C2 (ru) 2005-06-27
BR0013694A (pt) 2002-05-21
KR20020067498A (ko) 2002-08-22
IS2069B (is) 2005-11-15
TW577867B (en) 2004-03-01
IS6285A (is) 2002-02-26
EE200200113A (et) 2003-06-16
DE60009319T2 (de) 2005-03-31
ATE262507T1 (de) 2004-04-15
TR200200550T2 (tr) 2002-06-21
WO2001017956A1 (en) 2001-03-15
EE05080B1 (et) 2008-10-15
CZ2002773A3 (cs) 2002-06-12
PL353887A1 (en) 2003-12-15
RU2002108508A (ru) 2004-01-20
SK286774B6 (sk) 2009-05-07
SK3002002A3 (en) 2002-07-02
IL148111A (en) 2007-05-15
NO20021040D0 (no) 2002-03-01
MY127036A (en) 2006-11-30
DE60009319D1 (de) 2004-04-29
DK1214296T3 (da) 2004-07-05
JP2003508515A (ja) 2003-03-04
CA2381581A1 (en) 2001-03-15
NZ517147A (en) 2003-11-28
KR100692232B1 (ko) 2007-03-09
HK1045496A1 (en) 2002-11-29
AU760061B2 (en) 2003-05-08
HUP0202725A3 (en) 2005-04-28
EP1214296B1 (en) 2004-03-24
AU6854300A (en) 2001-04-10
HUP0202725A2 (hu) 2003-01-28
IL148111A0 (en) 2002-09-12
EP1214296A1 (en) 2002-06-19
AR035163A1 (es) 2004-05-05
PT1214296E (pt) 2004-08-31
US6689909B1 (en) 2004-02-10
CN1387509A (zh) 2002-12-25
BG65099B1 (bg) 2007-02-28
BG106520A (en) 2003-03-31

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