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1. WO2022008006 - DEUTERATED AND TRITIATED N-(4,5-DIMETHYLTHIAZOLO-2(3H)-YLIDEN)-2,2,3,3-TETRAMETHYLCYCLOPROPANE-1-CARBOXAMIDE DERIVATIVES AND THEIR USE

Publication Number WO/2022/008006
Publication Date 13.01.2022
International Application No. PCT/DE2021/100600
International Filing Date 09.07.2021
IPC
C07D 277/46 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
277Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
02not condensed with other rings
20having two or three double bonds between ring members or between ring members and non-ring members
32with 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 to ring carbon atoms
38Nitrogen atoms
44Acylated amino or imino radicals
46by carboxylic acids, or sulfur or nitrogen analogues thereof
A61P 25/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
C07B 59/00 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
59Introduction of isotopes of elements into organic compounds
A61K 31/426 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
425Thiazoles
4261,3-Thiazoles
Applicants
  • HELMHOLTZ-ZENTRUM DRESDEN-ROSSENDORF E.V. [DE]/[DE]
Inventors
  • MOLDOVAN, Rares-Petru
  • TEODORO, Rodrigo
  • TOUSSAINT, Magali
  • GÜNDEL, Daniel
  • DEUTHER-CONRAD, Winnie
  • BRUST, Peter
Agents
  • RIECHELMANN & CARLSOHN PATENTANWÄLTE PARTG MBB
Priority Data
10 2020 118 255.410.07.2020DE
Publication Language German (de)
Filing Language German (DE)
Designated States
Title
(DE) DEUTERIERTE UND TRITIIERTE N-(4,5-DIMETHYLTHIAZOL-2(3H)-YLIDEN)-2,2,3,3-TETRAMETHYLCYCLOPROPAN-1-CARBOXAMID-DERIVATE UND DEREN VERWENDUNG
(EN) DEUTERATED AND TRITIATED N-(4,5-DIMETHYLTHIAZOLO-2(3H)-YLIDEN)-2,2,3,3-TETRAMETHYLCYCLOPROPANE-1-CARBOXAMIDE DERIVATIVES AND THEIR USE
(FR) DÉRIVÉS DE N-(4,5-DIMÉTHYLTHIAZOLO -2(3H)-YLIDÈNE) -2,2,3,3-TÉTRAMÉTHYLCYCLOPROPANE-1-CARBOXAMIDE DEUTÉRÉS ET TRITIÉS ET LEUR UTILISATION
Abstract
(DE) Die Erfindung betrifft Verbindungen der allgemeinen Formel (I), worin X1 eine CD2-Gruppe oder eine CT2-Gruppe ist; X2 Sauerstoff oder eine Gruppe (CZ1Z2)n ist, wobei Z1 und Z2 bei jedem Auftreten unabhängig voneinander jeweils Wasserstoff, Deuterium oder Tritium sind und n eine Ganzzahl von 1 bis 12 ist; X3 eine CD2-Gruppe oder eine CT2-Gruppe ist; und R aus der Gruppe ausgewählt ist, die aus Hydroxy, -NO2, Halogen, einem Diazonium-Ion, einem Diazonium-Salz, einem Trialkylammonium-Ion, einem Trialkylammonium-Salz, einem Dialkoxyaren, einem Sulfoxid, einer Boronsäure, einem Boronsäureester, einer zinnorganischen Verbindung, einem Iodonium-Ion, einem Iodonium-Salz, einem Iodonium-Ylid und einem Sulfonat besteht.
(EN) The invention relates to compounds of the general formula (I) wherein X1 is a CD2 group or a CT2 group; X2 is oxygen or a group (CZ1Z2)n, with Z1 and Z2 independently of each other being hydrogen, deuterium or tritium and n being an integer from 1 to 12 at each instance; X3 is a CD2 group or a CT2 group; and R is selected from the group consisting of hydroxy, -NO2, halogen, a diazonium ion, a diazonium salt, a trialkyl ammonium ion, a trialkyl ammonium salt, a dialkoxyarene, a sulfoxide, a boronic acid, a boronic acid ester, a tin-organic compound, a iodonium ion, a iodonium salt, a iodonium ylide and a sulfonate.
(FR) L'invention concerne des composés de la formule générale (I), dans laquelle X1 représente un groupe CD2 ou un groupe CT2; X2 représente oxygène ou un groupe (CZ1Z2)n, Z1 et Z2 étant indépendamment l'un de l'autre hydrogène, deutérium ou tritium et n étant un entier de 1 à 12 à chaque occurrence; X3 représente un groupe CD2 ou un groupe CT2; et R est choisi dans le groupe consistant en hydroxy, -NO2, halogène, un ion diazonium, un sel de diazonium, un ion trialkyl ammonium, un sel de trialkyl ammonium, un dialcoxyarène, un sulfoxyde, un acide boronique, un ester d'acide boronique, un composé organique de l'étain, un ion iodonium, un sel d'iodonium, un ylure d'iodonium et un sulfonate.
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