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1. WO2000042042 - HIGH AFFINITY INHIBITORS FOR TARGET VALIDATION AND USES THEREOF

Publication Number WO/2000/042042
Publication Date 20.07.2000
International Application No. PCT/US2000/000551
International Filing Date 11.01.2000
Chapter 2 Demand Filed 10.08.2000
IPC
C07D 487/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C12Q 1/48 2006.01
CCHEMISTRY; METALLURGY
12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
QMEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
1Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
48involving transferase
CPC
A61P 13/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
A61P 19/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
02for joint disorders, e.g. arthritis, arthrosis
C07D 487/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by C07D451/00 - C07D477/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C12Q 1/485
CCHEMISTRY; METALLURGY
12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
QMEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS
1Measuring or testing processes involving enzymes, nucleic acids or microorganisms
48involving transferase
485involving kinase
G01N 2333/9121
GPHYSICS
01MEASURING; TESTING
NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
2333Assays involving biological materials from specific organisms or of a specific nature
90Enzymes; Proenzymes
91Transferases (2.)
912transferring phosphorus containing groups, e.g. kinases (2.7)
91205Phosphotransferases in general
9121with an alcohol group as acceptor (2.7.1), e.g. general tyrosine, serine or threonine kinases
G01N 2500/04
GPHYSICS
01MEASURING; TESTING
NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
2500Screening for compounds of potential therapeutic value
04Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A)
Applicants
  • PRINCETON UNIVERSITY [US/US]; New South Building 5th floor P.O. Box 36 Princeton, NJ 08544-0036, US
Inventors
  • SHOKAT, Kevan, M.; US
Agents
  • VEITENHEIMER, Erich, E.; Morgan, Lewis & Bockius LLP 1800 M Street, N.W. Washington, DC 20036-5869, US
Priority Data
60/115,34011.01.1999US
60/145,42223.07.1999US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) HIGH AFFINITY INHIBITORS FOR TARGET VALIDATION AND USES THEREOF
(FR) INHIBITEURS DE HAUTE AFFINITE POUR LA VALIDATION DE CIBLES, ET LEURS UTILISATIONS
Abstract
(EN)
This invention provides general methods for discovering mutant inhibitors for any class of enzymes as well as the specific inhibitors so identified. More specifically, this invention provides general methods for discovering specific inhibitors for multi-substrate enzymes. Examples of such multi-substrate enzymes include, but are not limited to, kinases and transferases. The mutant inhibitors identified by the methods of this invention can be used to highly selectively disrupt cell functions such as oncogenic transformation. In one particular example, this invention provides an Src protein kinase inhibitor, pharmaceutical compositions thereof and methods of disrupting transformation in a cell that expresses the target v-scr comprising contacting the cell with the protein kinase inhibitor.
(FR)
L'invention concerne des méthodes générales permettant de découvrir des inhibiteurs mutants dans une classe d'enzymes, ainsi que les inhibiteurs spécifiques ainsi identifiés. Cette invention concerne plus particulièrement des méthodes générales permettant de découvrir des inhibiteurs spécifiques d'enzymes multi-substrats, les kinases et les transférases étant parmi les exemples d'enzymes multi-substrats. Les inhibiteurs mutants identifiés grâce aux méthodes de cette invention peuvent être utilisés pour détruire de manière sélective des fonctions cellulaires, comme la transformation oncogène. Dans un exemple précis, cette invention concerne un inhibiteur de la protéine kinase Src, des compositions pharmaceutiques de ce dernier, et des méthodes destinées à détruire la transformation d'une cellule exprimant l'enzyme v-scr cible, ces méthodes consistant notamment à mettre ladite cellule en présence de l'inhibiteur de protéine kinase.
Latest bibliographic data on file with the International Bureau