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1. WO2000041669 - BENZIMIDAZOLE VASCULAR DAMAGING AGENTS

Publication Number WO/2000/041669
Publication Date 20.07.2000
International Application No. PCT/GB2000/000099
International Filing Date 14.01.2000
Chapter 2 Demand Filed 03.08.2000
IPC
A61K 31/4184 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
41641,3-Diazoles
4184condensed with carbocyclic rings, e.g. benzimidazoles
A61K 31/675 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
66Phosphorus compounds
675having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
C07D 235/32 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
235Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
02condensed with carbocyclic rings or ring systems
04Benzimidazoles; Hydrogenated benzimidazoles
24with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
30Nitrogen atoms not forming part of a nitro radical
32Benzimidazole-2-carbamic acids, unsubstituted or substituted; Esters thereof; Thio-analogues thereof
C07F 9/6506 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
645having two nitrogen atoms as the only ring hetero atoms
6503Five-membered rings
6506having the nitrogen atoms in positions 1 and 3
CPC
A61K 31/4184
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
41641,3-Diazoles
4184condensed with carbocyclic rings, e.g. benzimidazoles
A61K 31/675
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
66Phosphorus compounds
675having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61P 17/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
06Antipsoriatics
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 235/32
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
235Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
02condensed with carbocyclic rings or ring systems
04Benzimidazoles; Hydrogenated benzimidazoles
24with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
30Nitrogen atoms not forming part of a nitro radical
32Benzimidazole-2-carbamic acids, unsubstituted or substituted; Esters thereof; Thio-analogues thereof
C07F 9/65068
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
645having two nitrogen atoms as the only ring hetero atoms
6503Five-membered rings
6506having the nitrogen atoms in positions 1 and 3
65068condensed with carbocyclic rings or carbocyclic ring systems
Applicants
  • ANGIOGENE PHARMACEUTICALS LTD. [GB/GB]; 14 Plowden Park Aston Rowant Watlington Oxfordshire OX9 5SW, GB (AllExceptUS)
  • DAVIS, Peter, David [GB/GB]; GB (UsOnly)
Inventors
  • DAVIS, Peter, David; GB
Agents
  • BAILLIE, Iain, C. ; Langner Parry 52-54 High Holborn London WC1V 6RR, GB
Priority Data
9900752.815.01.1999GB
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) BENZIMIDAZOLE VASCULAR DAMAGING AGENTS
(FR) AGENTS DE DEGRADATION VASCULAIRE AUX BENZIMIDAZOLES
Abstract
(EN)
5(6)-substituted benzimidazole-2-carbamates of formula (I) wherein Alk is an alkyl group, X is oxygen, sulphur, sulphinyl, sulphonyl, carbonyl (CO), thiocarbonyl (CS), sulphonyloxy, NH, iminomethylene (C=NH), N-hydroxyiminomethylene, N-alkoxyiminomethylene, dialkoxymethylene, 1,3-dioxolan-2yl, 1,1-ethenyl, a group CHR3 or a bond, R1 is hydrogen, alkylaminocarbonyl or alkoxycarbonyl, R2 is hydrogen, alkoxycarbonyl, cyanomethyl, cyanoethyl, alkoxymethyl or acetoxymethyl. R3 is hydrogen, hydroxy, alkoxy or amino, A is an optionally substituted aromatic, optionally substituted heteroaromatic, optionally substituted heterocycloalkyl, optionally substituted alkyl or optionally substituted cycloalkyl group and the pharmaceutically acceptable salt, solvates and hydrates thereof, can be used in the preparation of medicaments for the treatment of diseases involving neovascularisation.
(FR)
La présente invention concerne un groupe d'agents de dégradation vasculaire convenant à la péparation de médicaments destinés au traitement d'affections impliquant une néovascularisation. Ces molécules sont des benzimidazole-2-carbamates à substitution 5(6) représentés par la formule générale (I) ou certains de leurs sels, solvates et hydrates admis en pharmacie. Dans cette formule, 'alk' est un groupe alkyle. X est oxygène, soufre, sulphinyle, sulphonyle, carbonyle (CO), thiocarbonyle (CS), sulphonyloxy, NH, iminométhylène (C=NH), N-hydroxyiminométhylène, N-alcoxyiminométhylène, dialcoxyméthylène, 1,3-dioxolane-2yle, 1,1-éthényle, un groupe CHR3 ou une liaison. R1 est hydrogène, alkylaminocarbonyle ou alcoxycarbonyle. R2 est hydrogène, alcoxycarbonyle, cyanométhyle, cyanoéthyle, alcoxyméthyle ou acétoxyméthyle. R3 est hydrogène, hydroxy, alcoxy ou amino. A est un groupe éventuellement substitué, notamment aromatique, hétéroaromatique, hétérocycloalkyle, alkyle ou cycloalkyle. La plupart des composés de ce groupe entrent dans le cadre de l'invention, en particulier ceux dans lesquels A est un cycle aromatique ou hétéroaromatique à substituants, particulièrement des substituants qui sont phosphates ou alkylphosphates. L'invention concerne donc aussi bien les composés de l'invention que les compositions pharmaceutiques comportant des composés ressortissants de la définition au sens large.
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