+

WO2001018181A3 - Enzyme inhibitors - Google Patents

Enzyme inhibitors Download PDF

Info

Publication number
WO2001018181A3
WO2001018181A3 PCT/US2000/024713 US0024713W WO0118181A3 WO 2001018181 A3 WO2001018181 A3 WO 2001018181A3 US 0024713 W US0024713 W US 0024713W WO 0118181 A3 WO0118181 A3 WO 0118181A3
Authority
WO
WIPO (PCT)
Prior art keywords
component
bonded
polymer
enzyme
inhibitor component
Prior art date
Application number
PCT/US2000/024713
Other languages
French (fr)
Other versions
WO2001018181A2 (en
Inventor
Todd Laurence Underiner
Scott Edward Osborne
Timothy Bates
Garry Steven Garrett
Renae Dianna Fossum
Original Assignee
Procter & Gamble
Todd Laurence Underiner
Scott Edward Osborne
Timothy Bates
Garry Steven Garrett
Renae Dianna Fossum
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 Procter & Gamble, Todd Laurence Underiner, Scott Edward Osborne, Timothy Bates, Garry Steven Garrett, Renae Dianna Fossum filed Critical Procter & Gamble
Priority to JP2001522393A priority Critical patent/JP2003509538A/en
Priority to AU71270/00A priority patent/AU7127000A/en
Priority to EP00960050A priority patent/EP1212098A2/en
Publication of WO2001018181A2 publication Critical patent/WO2001018181A2/en
Publication of WO2001018181A3 publication Critical patent/WO2001018181A3/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Macromolecular Compounds Obtained By Forming Nitrogen-Containing Linkages In General (AREA)
  • Addition Polymer Or Copolymer, Post-Treatments, Or Chemical Modifications (AREA)
  • Polyethers (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

The present invention relates to polymer conjugates which inhibit protease or lipase enzyme, said polymer conjugates comprising a polymer component bonded to an enzyme inhibitor component having an acyl unit capable of inhibiting the activity of more than one protease or lipase enzymes, wherein said inhibitor component is directly bonded to said polymer component or is bonded by a linking unit, said linking unit capable of modulating the interaction of a target enzyme and said inhibitor component wherein said polymer component remains bonded to said inhibitor component after said acyl unit interacts with said target enzyme.
PCT/US2000/024713 1999-09-10 2000-09-08 Enzyme inhibitors WO2001018181A2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP2001522393A JP2003509538A (en) 1999-09-10 2000-09-08 Enzyme inhibitor
AU71270/00A AU7127000A (en) 1999-09-10 2000-09-08 Enzyme inhibitors
EP00960050A EP1212098A2 (en) 1999-09-10 2000-09-08 Enzyme inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US15347399P 1999-09-10 1999-09-10
US60/153,473 1999-09-10

Publications (2)

Publication Number Publication Date
WO2001018181A2 WO2001018181A2 (en) 2001-03-15
WO2001018181A3 true WO2001018181A3 (en) 2001-12-13

Family

ID=22547365

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2000/024713 WO2001018181A2 (en) 1999-09-10 2000-09-08 Enzyme inhibitors

Country Status (6)

Country Link
EP (1) EP1212098A2 (en)
JP (1) JP2003509538A (en)
AR (1) AR023272A1 (en)
AU (1) AU7127000A (en)
PE (1) PE20010588A1 (en)
WO (1) WO2001018181A2 (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1212097B1 (en) * 1999-09-10 2005-11-16 The Procter & Gamble Company Enzyme inhibitors
EP1446125B1 (en) * 2001-08-30 2009-04-29 Alizyme Therapeutics Limited Thieno-(1,3)-oxazin-4-ones with lipase inhibiting activity
US8907154B2 (en) 2001-10-01 2014-12-09 The Procter & Gamble Company Sanitary napkins with hydrophobic lotions
US20030143186A1 (en) * 2001-11-13 2003-07-31 The Procter & Gamble Company Protease enzyme inhibitors
US7064122B2 (en) * 2001-12-20 2006-06-20 Osi Pharmaceuticals, Inc. Pancreatic lipase inhibitor compounds, their synthesis and use
US9035123B2 (en) 2002-10-01 2015-05-19 The Procter & Gamble Company Absorbent article having a lotioned topsheet
US20050048105A1 (en) * 2003-08-29 2005-03-03 Mcnulty Amy K. Protease inhibitor compositions for prevention and treatment of skin conditions

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999034786A2 (en) * 1998-01-09 1999-07-15 Geltex Pharmaceuticals, Inc. Lipase inhibiting polymers
WO1999046316A2 (en) * 1998-03-12 1999-09-16 The Procter & Gamble Company Enzyme inhibitors
WO1999045973A1 (en) * 1998-03-12 1999-09-16 The Procter & Gamble Company Disposable absorbent article having a skin care composition containing an enzyme inhibitor
WO1999045974A1 (en) * 1998-03-12 1999-09-16 The Procter & Gamble Company Protease inhibitors in absorbent articles
WO2001017501A1 (en) * 1999-09-10 2001-03-15 The Procter & Gamble Company Enzyme inhibitors

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4665070A (en) * 1985-06-25 1987-05-12 Syntex (U.S.A.) Inc. 2-oxy-4H-3,1-benzoxazin-4-ones and pharmaceutical use
DE4342154A1 (en) * 1993-12-10 1995-06-14 Behringwerke Ag Amidinophenylalanine derivatives, process for their preparation, their use and agents containing them as anticoagulants

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999034786A2 (en) * 1998-01-09 1999-07-15 Geltex Pharmaceuticals, Inc. Lipase inhibiting polymers
WO1999046316A2 (en) * 1998-03-12 1999-09-16 The Procter & Gamble Company Enzyme inhibitors
WO1999045973A1 (en) * 1998-03-12 1999-09-16 The Procter & Gamble Company Disposable absorbent article having a skin care composition containing an enzyme inhibitor
WO1999045974A1 (en) * 1998-03-12 1999-09-16 The Procter & Gamble Company Protease inhibitors in absorbent articles
WO2001017501A1 (en) * 1999-09-10 2001-03-15 The Procter & Gamble Company Enzyme inhibitors

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
JARVEST R L ET AL: "Potent selective thienoxazinone inhibitors of herpes proteases", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,GB,OXFORD, vol. 7, no. 13, 8 July 1997 (1997-07-08), pages 1733 - 1738, XP004136290, ISSN: 0960-894X *
PINTO I L ET AL: "Inhibition of human cytomegalovirus protease by enedione derivatives of thieno[2,3-d]oxazinones through a novel dual acylation/alkylation mechanism", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,GB,OXFORD, vol. 9, no. 3, 8 February 1999 (1999-02-08), pages 449 - 452, XP004157245, ISSN: 0960-894X *
TAKERKART G ET AL: "PREPARATON AND PROPERTIES OF ORGANOPHILIC TRYPSIN MACRO-INHIBITORS DIAMIDINO-ALPHA,OMEGA-DIPHENYLCARBAMYL-POLY(ETHYLENE GLYCOL)", FEBS LETTERS,XX,XX, vol. 42, no. 2, June 1974 (1974-06-01), pages 214 - 220, XP000870353, ISSN: 0014-5793 *

Also Published As

Publication number Publication date
AU7127000A (en) 2001-04-10
EP1212098A2 (en) 2002-06-12
WO2001018181A2 (en) 2001-03-15
PE20010588A1 (en) 2001-06-23
JP2003509538A (en) 2003-03-11
AR023272A1 (en) 2002-09-04

Similar Documents

Publication Publication Date Title
EP1818396A3 (en) Alpha-Amylase variants
WO2006133079A3 (en) Increasing perhydrolase activity in esterases and/or lipases
WO2001083770A3 (en) Lipolytic enzyme variant
WO1999043651A3 (en) Inhibitors of phospholipase enzymes
EP2204181A3 (en) Protease inhibitors
WO2001066711A8 (en) Xylanase variants having altered sensitivity to xylanase inhibitors
AU3665199A (en) Inhibitors of impdh enzyme
AU2003263842A1 (en) Novel variant hyprocrea jecorina cbh1 cellulases
ZA973397B (en) Inhibitors of IMPDH enzyme.
LV11986A (en) Inhibitors of rotamase enzyme activity
AU5498296A (en) Transdermally administrable medicament with ACE inhibitors
AU5920999A (en) Pesticidal compositions containing essential oils with enzyme inhibitors
AU5597098A (en) Inhibitors of the enzymatic activity of psa
WO2003061718A3 (en) Medical articles having enzymatic surfaces for localized therapy
WO2001018181A3 (en) Enzyme inhibitors
AU4976699A (en) Novel fluorogenic substrates for hydrolytic enzymes
PL342661A1 (en) Application of thiadiazole compounds as inhibitors of enzymes being dependent on cystein activity
EP1297834A4 (en) Inhibitor for enzyme having two divalent metal ions as active centers
WO2001042491A3 (en) Novel enzymatic substrates for detecting pseudomonas aeruginosa
DE60038350D1 (en) Angiotensin-converting enzyme inhibitors
AU6839300A (en) Nucleic acids which code for the enzyme activities of the spinosyn biosynthesis
AU7125700A (en) Enzyme inhibitors
PT996709E (en) CELLULITIS, XYLANOLITIC AND BETAGLUCANOLYTIC ENZYMES INHIBITORS
WO2004009804A3 (en) Feruloyl esterase and uses thereof
AU4906300A (en) Assay for detecting the enzymatic activity of a phosphorylation enzyme using enhanced signal generation

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AT AU AZ BA BB BG BR BY BZ CA CH CN CR CU CZ CZ DE DE DK DK DM DZ EE EE ES FI FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ PL PT RO RU SD SE SG SI SK SK SL TJ TM TR TT TZ UA UG US UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
121 Ep: the epo has been informed by wipo that ep was designated in this application
AK Designated states

Kind code of ref document: A3

Designated state(s): AE AG AL AM AT AT AU AZ BA BB BG BR BY BZ CA CH CN CR CU CZ CZ DE DE DK DK DM DZ EE EE ES FI FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ PL PT RO RU SD SE SG SI SK SK SL TJ TM TR TT TZ UA UG US UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: A3

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

WWE Wipo information: entry into national phase

Ref document number: 10070201

Country of ref document: US

ENP Entry into the national phase

Ref country code: JP

Ref document number: 2001 522393

Kind code of ref document: A

Format of ref document f/p: F

WWE Wipo information: entry into national phase

Ref document number: 2000960050

Country of ref document: EP

WWP Wipo information: published in national office

Ref document number: 2000960050

Country of ref document: EP

REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

WWW Wipo information: withdrawn in national office

Ref document number: 2000960050

Country of ref document: EP

点击 这是indexloc提供的php浏览器服务，不要输入任何密码和下载