N-HETEROARYL COMPOUNDS Russian patent published in 2016 - IPC C07D213/74 C07D215/46 C07D237/20 C07D239/42 C07D251/40 C07D471/04 C07D491/04 C07D495/04 A61K31/435 A61K31/47 A61P33/10 

Abstract RU 2596185 C2

FIELD: pharmaceutics.

SUBSTANCE: invention relates to N-heteroaryl compounds and pharmaceutically acceptable salts, solvates or N-oxides of general formula (I), where R1: halogen, C1-C6-alkyl, C1-C6-alkyloxy, C1-C6-alkylthio, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkoxy-C-1-C6-alkyl, C1-C6-alkyl-carbonyl, SF5, C1-C6-alkylsulphonyl, wherein each carbon-containing radical is optionally substituted with one or more halogen atoms, R2: hydrogen, C1-C6-alkyl, R3, R4 and R7 hydrogen, C1-C6-alkyl, R5: hydrogen, C1-C6-alkyl, C1-C6-acyl or C1-C6-alkyloxycarbonyl, R6: hydrogen, C1-C6-alkyl, C1-C6-alkyloxycarbonyl, phenyl, phenyl-C1-C6-alkyl, n=1-3, X: carbonyl, thiocarbonyl or sulphonyl group, A is a bond, E is a bond or NR9, where R9 - hydrogen, B is N, D is N or CR11, where R11 - hydrogen, Y1 is C or N, where C is substituted with R12, which is hydrogen, C1-C6-alkyl, C1-C6-galoalkilom, nitro, Y2 is C or N, where C is substituted with R13, which is hydrogen, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, nitrilo, di(C1-C6-alkyl)amino, N-pyrrolidinyl, C1-C6-alkylthio, C1-C6-alkylcarbonyl, aminocarbonyl, C1-C6-alkylamino-carbonyl, C1-C6-alkoxycarbonyl, Y3 is C, where C is substituted with R14, which is hydrogen, C1-C6-alkyl, C1-C6-alkoxy, amino, N-pyrrolidinyl, N-piperidinyl, N-morpholinyl, C1-C6-alkylcarbonyl, 1,3-dioxolane, which is unsubstituted or substituted with C1-C6-alkyl, Y4 is C or N, where C is substituted with R15, which is hydrogen, C1-C6-alkyl, wherein two of Y1, Y2 and Y4 can represent N, or Y3 and Y4 are bonded to form a ring system, selected from phenyl, thiophene, imidazole, pyridine, furan, 1,4-dioxane, triazole, and where at least one of B and D is a nitrogen atom. Invention also relates to a pharmaceutical composition based on compound of formula (I), intermediate compounds of formulae (1-IV), (3-IV), (4-II), method of treating helminth infection, compounds of formula (Ia), use of formula (I) and (Ia).

EFFECT: obtaining novel compounds effective in treating parasitic infections.

23 cl, 3 tbl, 18 ex

Similar patents RU2596185C2

Title Year Author Number
CONJUGATES OF BINDER (ADC) WITH KSP INHIBITORS 2014
  • Lerkhen Khans-Georg
  • Vittrok Sven
  • Gribenov Nils
  • Shtelte-Ludvig Beatriks
  • Zommer Anette
  • Berndt Zandra
  • Malert Kristof
  • Lobell Mario
  • Teryung Karsten
  • Greven Zimone
  • Kancho Grande Iolanda
RU2698697C2
METHOD OF PRODUCING OXAZOLES THROUGH CONDENSATION OF AROMATIC ALDEHYDES WITH ALPHA-KETOXIMES WITH FORMATION OF N-OXIDES AND SUBSEQUENT REACTION WITH ACTIVATED ACID DERIVATIVES 2005
  • Kholla Vol'Fgang
  • Kherljajn Rol'F-Ljudvig
  • Kulittssher Berndt
  • Lauks Vol'Fgang
  • Shtjudemann Tomas
  • Tapperttskhofen Kristof
  • Sheffer Robert Dzh. Kh.
RU2402537C2
SUBSTITUTED ISOQUINOLINE AND ISOQUINOLINONE DERIVATIVES AS Rho-KINASE INHIBITORS 2007
  • Plettenburg Oliver
  • Khofmajster Armin
  • Brendel' Joakhim
  • Len Mattias
RU2455302C2
SUBSTITUTED DERIVATIVES OF OXAZOL-BENZOISOTHIAZOLDIOXIDE, METHOD FOR MAKING AND APPLYING THEREOF 2005
  • Petri Shtefan
  • Tennagel'S Norbert
  • Kirsh Rajnkhard
  • Baringkhaus Karl-Khajnts
RU2377242C2
POLYCYCLIC THIAZOLIDINE-2-YLIDENE AMINES, MEDICINAL AGENTS CONTAINING THEREOF AND METHOD FOR PREPARING MEDICINAL AGENT 1999
  • Jene Gerkhard
  • Gajzen Karl
  • Lang Khans Jokhen
RU2236405C2
NOVEL DERIVATIVES OF BENZIMIDAZOLE AND THEIR USING AS MEDICAMENTS 2002
  • Puatu Lidi
  • Bro Valeri
  • Ferrandi Ehrik
  • Tjur'O Kristof
RU2294326C2
NOVEL FLUOROGLYCOSIDE DERIVATIVES OF PYRAZOLES, MEDICINE CONTAINING THEM, AND APPLICATION OF DERIVATIVES 2005
  • Brummerkhop Kharm
  • Frik Vendelin
  • Glombik Khajner
  • Plettenburg Oliver
  • Bikkel' Martin
  • Khojer Khubert
  • Tajs Shtefan
RU2370499C2
RUTHENIUM COMPLEXES CONTAINING PARACYCLOPHANE AND CARBONYL LIGANDS AND THEIR USE AS CATALYSTS 2012
  • Grejndzher Damian Mark
  • Nedden Khans Gyunter
  • Rouzblejd Stefen Dzhejms
RU2614415C2
DERIVATIVES OF PHENYLUREA SUBSTITUTED WITH CARBOXYLIC ACID AMIDE AND THEIR USING AS MEDICINAL AGENTS 2002
  • Defossa Ehlizabet
  • Klabunde Tomas
  • Burger Khans-Jorg
  • Kherling Andreas
  • Fon Redern Ehrikh
  • Pojkert Shtefan
  • Ehnsen Al'Fons
  • Bauehr Armin
  • Najzes Berd
  • Vendt Karl Ul'Rikh
RU2291858C2
SUBSTITUTED DERIVATIVES OF IMIDAZOLIDINE, METHOD FOR PREPARING AND PHARMACEUTICAL PREPARATION 1998
  • Vener Fol'Kmar
  • Shtil'Ts Khans Ul'Rikh
  • Shmidt Vol'Fgang
  • Zajffge Dirk
RU2239641C2

RU 2 596 185 C2

Authors

Berger Mikhael

Kern Kristofer

Ek Marko

Shreder Jorg

Dates

2016-08-27Published

2011-09-28Filed