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1. WO2020111956 - NOVEL L-PROLINE SULFONAMIDE DERIVATIVES COMPRISING PYRAZOLO[4,3- E]TETRAZOLO[4,5-B][1,2,4]TRIAZINE SYSTEM, METHOD OF MANUFACTURING THEREOF, USES THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

Publication Number WO/2020/111956
Publication Date 04.06.2020
International Application No. PCT/PL2019/000110
International Filing Date 27.11.2019
IPC
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07D 487/12 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
12in which the condensed system contains three hetero rings
A61K 31/4985 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
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
CPC
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07D 487/12
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
12in which the condensed system contains three hetero rings
Applicants
  • UNIWERSYTET MEDYCZNY W BIAŁYMSTOKU [PL]/[PL]
  • UNIWERSYTET PRZYRODNICZO-HUMANISTYCZNY W SIEDLCACH [PL]/[PL]
  • UNIWERSYTET MEDYCZNY W LUBLINIE [PL]/[PL]
Inventors
  • MOJZYCH, Mariusz
  • KOTWICA-MOJZYCH, Katarzyna
  • BIELAWSKA, Anna
  • BIELAWSKI, Krzysztof
  • PAWLAK, Dariusz
  • HERMANOWICZ, Justyna, Magdalena
  • TANKIEWICZ-KWEDLO, Anna
  • SZYMANOWSKA, Anna
Agents
  • KAWCZYŃSKA, Marta, Joanna
Priority Data
P.42799130.11.2018PL
Publication Language English (EN)
Filing Language Polish (PL)
Designated States
Title
(EN) NOVEL L-PROLINE SULFONAMIDE DERIVATIVES COMPRISING PYRAZOLO[4,3- E]TETRAZOLO[4,5-B][1,2,4]TRIAZINE SYSTEM, METHOD OF MANUFACTURING THEREOF, USES THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
(FR) NOUVEAUX DÉRIVÉS DE L-PROLINE SULFONAMIDE COMPRENANT LE SYSTÈME PYRAZOLO[4,3-E]TÉTRAZOLO[4,5-B][1,2,4]TRIAZINE, SON PROCÉDÉ DE FABRICATION, SES UTILISATIONS ET COMPOSITION PHARMACEUTIQUE LE COMPRENANT
Abstract
(EN)
The subject matter of the invention relates to novel sulfonamide derivatives of 7-methyl-5-phenyl-pyrazolo[4,3-e]tetrazolo[4,5-b] [1,2,4]triazine comprising L-proline or 4-hydroxy-L-proline in the sulfonamide group. The novel compounds exhibit cytostatic activity against gastric cancer cell (AGS) and colorectal cancer cell (DLD-1 and HT-29) lines and may be used as novel medicaments which have anticancer action. The subject matter of the invention also relates to a method of manufacturing such derivatives, as well as uses thereof and a pharmaceutical composition comprising the same.
(FR)
La présente invention concerne de nouveaux dérivés de sulfonamide de 7-méthyl-5-phényl-pyrazolo[4,3-e]tétrazolo[4,5-b][1,2,4]triazine comprenant de la L-proline ou de la 4-hydroxy-L-proline dans le groupe sulfonamide. Les nouveaux composés font preuve d'activité cytostatique contre les lignées cellulaires du cancer de l'estomac (AGS) et des cellules du cancer colorectal (DLD-1 et HT-29) et peuvent être utilisés en tant que nouveaux médicaments qui présentent une action anticancéreuse. L'invention concerne également un procédé de fabrication de tels dérivés, ainsi que leurs utilisations et une composition pharmaceutique les comprenant.
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