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1. WO2022003377 - THIENO[3,4-C]PYRAZOL-3-YL ACETAMIDES AS AUTOTAXIN INHIBITORS

Publication Number WO/2022/003377
Publication Date 06.01.2022
International Application No. PCT/GR2021/000045
International Filing Date 02.07.2021
IPC
A61K 31/4162 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4151,2-Diazoles
4162condensed with heterocyclic ring systems
A61K 31/4439 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
44Non-condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
4439containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/497 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
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
4965Non-condensed pyrazines
497containing further heterocyclic rings
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 35/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
Applicants
  • UNI-PHARMA KLEON TSETIS PHARMACEUTICAL LABORATORIES S.A. [GR]/[GR]
  • B.S.R.C. "ALEXANDER FLEMING" [GR]/[GR]
Inventors
  • AIDINIS, Vassilios
  • MATRALIS, Alexios
Priority Data
2020010039102.07.2020GR
2021010042224.06.2021GR
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) THIENO[3,4-C]PYRAZOL-3-YL ACETAMIDES AS AUTOTAXIN INHIBITORS
(FR) THIÉNO[3,4-C]PYRAZOL-3-YL ACÉTAMIDES UTILISÉS EN TANT QU'INHIBITEURS DE L'AUTOTAXINE
Abstract
(EN) A pharmaceutical compound or pharmaceutically acceptable salt thereof, for use in the treatment of pulmonary fibrosis, pulmonary allograft fibrosis, hepatic fibrosis, renal fibrosis, cardiac fibrosis, pneumonia, COVID-19 disease, bacterial infection, rheumatoid arthritis, neurodegenerative diseases, diseases related to metabolic syndrome and cancer, due to autotaxin inhibition, having the chemical formula (A), wherein: - R1 is selected from a heterocyclic group, or a heteroaromatic group, or an aromatic group which is selected from 4-bromophenyl, 4-carboxyphenyl- or 4-nitrophenyl-groups, R2 is independently selected from an alkyl carbon chain or from a cyclic hydrocarbon or from one or more heterocyclic, aromatic or heteroaromatic rings, wherein each ring may carry one or more substituents selected from hydrogen, halogen, nitro-, methoxy-, and carboxylic-group or from a group -CR3R4Ar, wherein R3, R4 are selected from hydrogen, (C1-6)alkyl-, trifluoromethyl-, methoxy-, trifluoromethoxy- or (C3-7)cycloalkane and Ar is an aromatic or a heteroaromatic ring.
(FR) L'invention concerne un composé pharmaceutique ou un sel pharmaceutiquement acceptable de celui-ci, destiné à être utilisé pour traiter la fibrose pulmonaire, la fibrose pulmonaire d'allogreffe, la fibrose hépatique, la fibrose rénale, la fibrose cardiaque, la pneumonie, la COVID-19, une infection bactérienne, la polyarthrite rhumatoïde, les maladies neurodégénératives, les maladies liées au syndrome métabolique et au cancer, en raison de l'inhibition de l'autotaxine, ayant la formule chimique (A), dans laquelle : - R1 est sélectionné parmi un groupe hétérocyclique, ou un groupe hétéroaromatique, ou un groupe aromatique qui est sélectionné parmi des groupes 4-bromophényle, 4-carboxyphényle ou 4-nitrophényle, R2 est indépendamment sélectionné parmi une chaîne carbonée d'alkyle ou parmi un hydrocarbure cyclique ou parmi un ou plusieurs cycles hétérocycliques, aromatiques ou hétéroaromatiques, chaque cycle pouvant porter un ou plusieurs substituants sélectionnés parmi hydrogène, halogène, nitro-, méthoxy-, et un groupe carboxylique ou parmi un groupe -CR3R4Ar, dans lequel R3, R4 sont sélectionnés parmi hydrogène, (C1-6)alkyl-, trifluorométhyl-, méthoxy-, trifluorométhoxy- ou (C3-7)cycloalcane et Ar est un cycle aromatique ou hétéroaromatique.
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