NOVEL 3,5-DIVINYL-PYRAZOLE DERIVATIVES FOR MEDICAL USE Russian patent published in 2019 - IPC C07D231/12 C07D403/10 C07D405/06 A61K31/415 A61K31/4155 A61K31/4178 A61P35/00 

Abstract RU 2695062 C2

FIELD: medicine; pharmacology.

SUBSTANCE: invention refers to pharmacology, and concerns new chemical compounds of general formula (I) or their pharmaceutically acceptable salts which are inhibitors of P-glycoprotein. In formula (I) R1, R2, R3, R4 independently represent H, halogen, NO2; Rx - is selected from -C(=S)NHRA, -C(=O)ORA, -S(=O)2NRARB, -C(=O) NRARB, 5-membered partially or completely unsaturated heterocycle containing 2 N atoms; RA is independently selected and represents C1-6-alkyl, partially or completely halogenated C1-8-alkyl; RB is independently selected and represents H, C1-8-alkyl or partially or completely halogenated C1-8-alkyl; alternatively, in case Rx is -C (= O) NRARB, RA and RB together with nitrogen atom, to which they are attached, can form saturated cycle containing 5 atoms; Rp is independently selected and represents C1-6-alkyl, partially or completely halogenated C1-6-alkyl; Rm is selected independently and is H, C1-6-alkyl, partially or completely halogenated C1-8-alkyl; alternatively neighbouring groups Rp and Rm together with two oxygen atoms, to which they are attached, and two carbon atoms of the benzene ring can form a non-aromatic ring containing 5 to 6 atoms. Given chemical compounds can be used to suppress multiple drug resistance in the patients receiving the various drugs for a long time. Invention also relates to the use of the above compounds and a pharmaceutical composition containing said compounds.

(I).

EFFECT: these compounds can be used in therapy of central nervous system diseases, infectious, allergic, autoimmune, oncological and other diseases.

9 cl

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RU 2 695 062 C2

Authors

Sagnou Marina

Alexiou Polyxeni

Novikov Fedor Nikolaevich

Chilov Germes Grigorevich

Stroganov Oleg Valentinovich

Strojlov Viktor Sergeevich

Zejfman Aleksej Aleksandrovich

Titov Ilya Yurevich

Sagnou Marina

Aleksiou Poliksenij

Dates

2019-07-19Published

2015-05-22Filed