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1. WO2022008918 - AZETIDINE DERIVATIVES FOR THE TREATMENT OF INTEGRIN ASSOCIATED DISEASES

Publication Number WO/2022/008918
Publication Date 13.01.2022
International Application No. PCT/GB2021/051742
International Filing Date 08.07.2021
IPC
C07D 471/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61P 9/10 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
10for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 11/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
A61P 19/10 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
08for bone diseases, e.g. rachitism, Paget's disease
10for osteoporosis
A61P 35/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61K 31/4375 2006.1
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
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
4375the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
Applicants
  • UNIVERSITY OF NOTTINGHAM [GB]/[GB]
Inventors
  • MCINALLY, Thomas
  • MACDONALD, Simon
  • MOODY, Christopher
  • HATLEY, Richard
  • BARRETT, Tim
  • WATSON, Morag
  • RICHIE, Timothy
Agents
  • JOANNA, Thurston
Priority Data
2010626.610.07.2020GB
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) AZETIDINE DERIVATIVES FOR THE TREATMENT OF INTEGRIN ASSOCIATED DISEASES
(FR) DÉRIVÉS D'AZÉTIDINE POUR LE TRAITEMENT DE MALADIES SE RAPPORTANT AUX INTÉGRINES
Abstract
(EN) The invention relates to novel compounds of formula (I), the compounds being capable of acting as avβ6 integrin antagonists, their use in the treatment of disease, their methods of manufacture and compositions comprising said compounds for such purposes (I) wherein R1 is selected from: R1a, -C(O)R1a, -C(O)OR1a -C(O)NHR1a, -C(O)N(R1a)2, -SO2R1a, wherein R1a are each independently selected from: alkyl, alkenyl, alkynyl, aryl, heteroaryl, alkylaryl or alkylheteroaryl, each of which may be optionally substituted; R2 is selected from: hydrogen, halogen, optionally substituted alkyl or optionally substituted alkoxyl; R2a are each independently selected from: hydrogen, halogen, optionally substituted alkyl or optionally substituted alkoxyl; R3 is selected from: hydrogen, optionally substituted alkyl or optionally substituted alkoxyl; R4 is hydroxyl; Ar1 is an optionally substituted heteroaryl or bicyclic heteroaryl; and L is a linker; or a pharmaceutically acceptable salt thereof.
(FR) L'invention concerne de nouveaux composés de formule (I), les composés étant aptes à agir en tant qu'antagonistes de l'intégrine α V β 6, leur utilisation dans le traitement de maladies, leurs procédés de fabrication et des compositions comprenant lesdits composés à de telles fins (I) R1 étant choisi parmi : R1a, -C(O)R1a, -C(O)OR1a -C(O)NHR1a, -C(O)N(R1a)2, -SO2R1a, R1a étant indépendamment respectivement choisis parmi : un alkyle, un alcényle, un alcynyle, un aryle, un hétéroaryle, un alkylaryle ou un alkylhétéroaryle, chacun d'eux pouvant être éventuellement substitué ; R2 est choisi parmi : l'hydrogène, un halogène, un alkyle éventuellement substitué ou un alcoxyle éventuellement substitué ; R2a sont chacun indépendamment choisis parmi : l'hydrogène, un halogène, un alkyle éventuellement substitué ou un alcoxyle éventuellement substitué ; R3 est choisi parmi : un hydrogène, un alkyle éventuellement substitué ou un alcoxyle éventuellement substitué ; R4 représente un hydroxyle ; Ar1 représente un hétéroaryle éventuellement substitué ou un hétéroaryle bicyclique ; et L est un liant ; ou un sel pharmaceutiquement acceptable de celui-ci.
Latest bibliographic data on file with the International Bureau