AU2001225380A1 - 2-thio-4h-3,1-benzoxazin-4-one derivatives for use as enzyme inhibitors - Google Patents

2-thio-4h-3,1-benzoxazin-4-one derivatives for use as enzyme inhibitors

Info

Publication number
AU2001225380A1
AU2001225380A1 AU2001225380A AU2538001A AU2001225380A1 AU 2001225380 A1 AU2001225380 A1 AU 2001225380A1 AU 2001225380 A AU2001225380 A AU 2001225380A AU 2538001 A AU2538001 A AU 2538001A AU 2001225380 A1 AU2001225380 A1 AU 2001225380A1
Authority
AU
Australia
Prior art keywords
reduced
formula
sup
inhibition
arylalkyl
Prior art date
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.)
Abandoned
Application number
AU2001225380A
Inventor
Robert Downham
Christopher Robert Dunk
Harold Francis Hodson
Richard Michael John Palmer
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Alizyme Therapeutics Ltd
Original Assignee
Alizyme Therapeutics Ltd
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 Alizyme Therapeutics Ltd filed Critical Alizyme Therapeutics Ltd
Publication of AU2001225380A1 publication Critical patent/AU2001225380A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/12—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
    • C07D265/14—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D265/24—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with hetero atoms directly attached in positions 2 and 4
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/536—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with carbocyclic ring systems
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • 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
    • A61P9/10—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
    • 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
    • A61P9/12—Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic 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)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Cosmetics (AREA)
  • Coloring Foods And Improving Nutritive Qualities (AREA)
  • Food Preservation Except Freezing, Refrigeration, And Drying (AREA)

Abstract

The use of a compound, comprising formula (I) or a salt, ester, amide of prodrug thereof in the inhibition of an enzyme whose preferred mode of action is to catalyse the hydrolysis of an ester functionality e.g. in the control and inhibition of unwanted enzymes in products and processes. The compounds are also useful in medicine e.g. in the treatment of obesity and related conditions. The invention also relates to novel compounds within formula (I), to processes for preparing them and pharmaceutical compositions containing them. In formula (I) A is an optionally substituted 6-membered aromatic or heteroaromatic ring; and R<SUP>1 </SUP>is a branched or unbranched alkyl (optionally interrupted by one or more oxygen atoms), alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, reduced arylalkyl, arylalkenyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl, reduced aryl, reduced heteroaryl, reduced heteroarylalkyl or a substituted derivative of any of the foregoing groups
AU2001225380A 2000-01-24 2001-01-17 2-thio-4h-3,1-benzoxazin-4-one derivatives for use as enzyme inhibitors Abandoned AU2001225380A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0001572 2000-01-24
GBGB0001572.7A GB0001572D0 (en) 2000-01-24 2000-01-24 Inhibitors
PCT/GB2001/000171 WO2001053278A1 (en) 2000-01-24 2001-01-17 2-thio-4h-3,1-benzoxazin-4-one derivatives for use as enzyme inhibitors

Publications (1)

Publication Number Publication Date
AU2001225380A1 true AU2001225380A1 (en) 2001-07-31

Family

ID=9884222

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2001225380A Abandoned AU2001225380A1 (en) 2000-01-24 2001-01-17 2-thio-4h-3,1-benzoxazin-4-one derivatives for use as enzyme inhibitors

Country Status (9)

Country Link
US (1) US6916808B2 (en)
EP (1) EP1255742B1 (en)
JP (1) JP2003520278A (en)
AT (1) ATE417835T1 (en)
AU (1) AU2001225380A1 (en)
DE (1) DE60137023D1 (en)
ES (1) ES2317887T3 (en)
GB (1) GB0001572D0 (en)
WO (1) WO2001053278A1 (en)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL368994A1 (en) * 2001-08-30 2005-04-04 Alizyme Therapeutics Limited Thieno-(1,3)-oxazin-4-ones with lipase inhibiting activity
EP1467978A4 (en) * 2001-12-20 2005-11-02 Osi Pharm Inc Pancreatic lipase inhibitor compounds, their synthesis and use
US8372430B2 (en) 2002-12-17 2013-02-12 The Procter & Gamble Company Compositions, methods, and kits useful for the alleviation of gastrointestinal effects
US20090082435A1 (en) * 2005-04-28 2009-03-26 The Regents Of The University Of California Methods, Compositions, And Compounds For Modulation Of Monoacylglycerol Lipase, Pain, And Stress-Related Disorders
US9039158B2 (en) * 2013-06-13 2015-05-26 Xerox Corporation Ink stick identification system
CN111763164B (en) * 2019-04-02 2023-03-10 中国医学科学院药物研究所 Preparation method and application of ortho-carbonyl amino substituted benzene derivatives

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR022204A1 (en) * 1999-01-08 2002-09-04 Norgine Bv COMPOUND, PROCESS FOR PREPARATION, PHARMACEUTICAL COMPOSITION AND EDIBLE PRODUCT THAT UNDERSTANDS IT.
GB9900416D0 (en) 1999-01-08 1999-02-24 Alizyme Therapeutics Ltd Inhibitors

Also Published As

Publication number Publication date
ATE417835T1 (en) 2009-01-15
EP1255742A1 (en) 2002-11-13
ES2317887T3 (en) 2009-05-01
US20030176429A1 (en) 2003-09-18
GB0001572D0 (en) 2000-03-15
DE60137023D1 (en) 2009-01-29
US6916808B2 (en) 2005-07-12
EP1255742B1 (en) 2008-12-17
WO2001053278A1 (en) 2001-07-26
JP2003520278A (en) 2003-07-02

Similar Documents

Publication Publication Date Title
WO2000040569A8 (en) 2-amino-benzoxazinone derivatives for the treatment of obesity
MXPA01006921A (en) 2-amino-4h-3,1-benzoxazin-4-one derivatives for the treatment of obesity.
EP1090908A3 (en) Cyclobutane derivatives as inhibitors of protein farnesyltransferase
DK1018511T3 (en) Isochroman compounds and processes for their preparation
ES474288A1 (en) 3-Substituted-6-substituted-7-oxo-1-azabicyclo (3.2.0)-hept-2-ene-2-carboxylic acid, its preparation and pharmaceutical compositions containing it.
AU7517400A (en) N-substituted 4-aminopteridines, synthesis and use thereof as pharmaceutical agent
AU2001225380A1 (en) 2-thio-4h-3,1-benzoxazin-4-one derivatives for use as enzyme inhibitors
AU2152899A (en) Pyranones, method for the production and use thereof
AU2603697A (en) Thiadiazolyl(thio)ureas useful as matrix metalloprotease inhibitors
MX9800704A (en) Esters and amides as pla2 inhibitors.
AU1466295A (en) Amino acid derivatives and their use as phospholipase a2 inhibitors
NO20010559L (en) Process for the synthesis of (1H) -benzo [c] quinolizin-3-ones derivatives
AU5999798A (en) Heterocyclic compounds useful as oxido-squalene cyclase inhibitors
AU6731100A (en) Integrase inhibitors containing aromatic heterocycle derivatives
AU6889096A (en) Pyrimidine derivatives
IL151167A0 (en) Pyrrolopyridazine derivatives and pharmaceutical compositions containing the same
MY139608A (en) Thieno-(1,3)-oxazin-4-ones with lipase inhibiting activity
DE69608704D1 (en) MANUFACTURE OF DERIVATIVES OF ALLYLBERSTONIC ACID AND STARTING PRODUCTS THEREFOR
ZA937317B (en) Process for the stereoselective preparation of a beta-phenylisoserine derivative and its use for the preparation of taxane derivatives
TH59783B (en) Deterrent
TW200502204A (en) Oligo acid derivatives
AU1712601A (en) Novel amidine derivatives, preparation and use thereof as medicines
PT868428E (en) PHOSPHONIC ACID DERIVATIVES HAVING METALOPEPTIDASE INHIBITING ACTIVITY
MX9708077A (en) Cyclobutane derivatives as inhibitors of squalene synthase and protein farnesyltransferase.
MX9604347A (en) Organic compounds.