SUBSTITUTED DIAMINO-CARBOXAMIDE AND DIAMINO-CARBONITRILE PYRIMIDINE DERIVATIVES, THEIR COMPOSITIONS AND METHODS OF TREATMENT USING THEM Russian patent published in 2017 - IPC C07D239/48 C07D405/14 C07D401/04 A61K31/505 A61K31/506 A61P3/10 A61P35/00 A61P1/16 

Abstract RU 2625309 C2

FIELD: pharmacology.

SUBSTANCE: in formula (I)

,

R1 and R2 independently represent unsubstituted C1-8alkyl; C1-8alkyl substituted with one or more halogen atoms, hydroxy, C1-3alkoxy, C1-3alkoxy, C1-3alkyl, halogenC1-3alkoxy or hydroxyC1-3alkyl; unsubstituted saturated 3-7-membered monocycloalkyl or 5-8-membered bicycloalkyl; substituted saturated 3-7-membered monocycloalkyl or 5-8-membered bicycloalkyl, wherein the substituents are selected from halogen, C1-6alkyl, hydroxy, oxo, C1-3alkoxy, C1-3alkoxyC1-3alkyl, halogenC1-3alkyl, halogenC1-3alkoxy, hydroxyC1-3alkyl, aminoC1-3alkyl, O-cyclopropyl, NH2, NH(C1-3)alkyl, N(C1-3alkyl)2, C(O)-C1-3alkyl, NHC(O)-C1-3alkyl, C(O) NH2, C(O) NHC1-3alkyl, C(O)N(C1-3alkyl)2 and NHSO2(C1-3alkyl) and pyrrolidine; unsubstituted C1-3alkyl-C3-6cycloalkyl; 4-6-membered nonaromatic monocyclic heterocyclyl, optionally N-substituted with group of C1-3alkyl-C(O) or optionally substituted with C1-3alkyl, oxo or hydroxy, wherein heteroatoms are selected from 1-2 oxygen atoms or 1 nitrogen atom, or dioxaspirodecanyl.

EFFECT: compounds can be used for the treatment or prevention of fibrotic liver diseases or metabolic syndrome, which lead to the development of fibrotic liver diseases such as: nonalcoholic steatohepatitis, steatosis, cirrhosis, primary sclerosing cholangitis, primary biliary cirrhosis, hepatitis, hepatocellular carcinoma or liver fibrosis, connected with chronic or recurrent alcohol consumption, infection, liver transplantation or liver injury caused by taking drugs, and as well as for treatment or prevention of interstitial pulmonary fibrosis.

67 cl, 3 tbl, 62 ex

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RU 2 625 309 C2

Authors

Bennett Brajdon L.

Elsner Yan

Erdman Pol

Khilgraf Robert

Lebren Lori Enn

Makkarrik Meg

Mogkhaddam Mekhran F.

Nejdzhi Mark A.

Norris Stefan

Pejzner Devid A.

Sloss Meriann

Romanov Uilliam Dzh.

Satokh Jositaka

Tike Dzhejeshri

Joon Von Khiung

Delgado Mersedes

Dates

2017-07-13Published

2012-04-20Filed