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1. RU0002638537 - ENZYMES INHIBITION

Office
Russian Federation
Application Number 2015104644
Application Date 10.07.2013
Publication Number 0002638537
Publication Date 14.12.2017
Grant Number
Grant Date 14.12.2017
Publication Kind C2
IPC
A61K 31/4196
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
41961,2,4-Triazoles
A61K 31/437
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
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
437the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61P 11/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
C07D 471/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
CPC
C07D 471/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61P 11/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
A61K 31/4196
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 being nitrogen, e.g. tetrazole
41961,2,4-Triazoles
A61K 31/437
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
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
437the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
Inventors КАПАЛЬДИ Кармелида (IT)
ХИЛД Роберт Эндрю (IT)
РЭЙ Николас Чарльз (IT)
САТТОН Джонатан Марк (IT)
KAPALDI Karmelida (IT)
KHILD Robert Endryu (IT)
REJ Nikolas Charlz (IT)
SATTON Dzhonatan Mark (IT)
Priority Data 12176079.7 12.07.2012 EP
13158756.0 12.03.2013 EP
Title
(EN) ENZYMES INHIBITION
(RU) ИНГИБИРОВАНИЕ ФЕРМЕНТОВ
Abstract
(EN) FIELD: pharmacology. SUBSTANCE: invention relates to the compound of the formula or its pharmaceutically acceptable salt. In the formula (I) R1 represents -CN; R2 is selected from (C1-C4)haloalkyl, (C1-C4)haloalkoxy; W represents the (i) 5-membered heteroaryl ring, where two or three ring-atoms represent the hetero-atom N, optionally substituted by one group, which is selected from the (C1-C4) alkyl, the group -NHR18, and from the group -COOR28; or (iii) phenyl group; R3 represents the group -CH2-R23; R5 represents the hydrogen; R6 represents the hydrogen; A1 represents the group -CR7=; A2 represents the group =CR8- or the group =N-; A3--A4 represents the group, which is selected from the group -CR4=N-, the group -CR4=CR9- and the group NR17-CO-; R4 represents the group, which is selected from the hydrogen, the (C1-C4) alkyl, -NR10R11, -NHCOR12, -NHCOO-R13, -NHCONR27-R14, the (C1-C4)alkoxy, -NH(CH2)n-SO2(C1-C4)alkyl, -(NH)q(CH2)n-(C6H4)-SO2(C1-C4)alkyl, -NHSO2(C1-C4) alkyl and -(NH)r(CH2)nCONR15R16; the other chemical groups value is indicated in the invention formula. The invention also relates to the pharmaceutical composition and to the method of the disease or state treatment, where HNE is implicated. EFFECT: there are new compounds of the formula that offer the inhibitors' properties of the human neutrophil elastase. 14 cl, 97 ex
(RU) Изобретение относится к соединению формулы (I) или его фармацевтически приемлемой соли . В формуле (I) R1 представляет собой -CN; R2 выбран из (С1-С4)галогеналкила, (С1-С4)галогеналкокси; W представляет собой (i) 5-членное гетероарильное кольцо, где два или три кольцевых атома представляют собой гетероатом N, необязательно замещенное одной группой, выбранной из (С1-С4)алкила, группы -NHR18, группы -COOR28; или (iii) фенильную группу; R3 представляет собой группу -CH2-R23; R5 представляет собой водород; R6 представляет собой водород; A1 представляет собой группу -CR7=; А2 представляет собой группу =CR8- или группу =N-; А3--А4 представляет собой группу, выбранную из группы -CR4=N-, группы -CR4=CR9- и группы -NR17-CO-; R4 представляет собой группу, выбранную из водорода, (C1-С4)алкила, -NR10R11, -NHCOR12, -NHCOO-R13, -NHCONR27-R14, (C1-С4)алкокси, -NH(CH2)n-SO2(C1-C4)алкила, -(NH)q(CH2)n-(C6H4)-SO2(C1-C4)алкила, -NHSO2(C1-C4)алкила и -(NH)r(CH2)nCONR15R16; значения остальных радикалов указаны в формуле изобретения. Изобретение также относится к фармацевтической композиции и к способу лечения заболевания или состояния, в котором участвует HNE. Технический результат: получены новые соединения формулы (I), обладающие свойствами ингибиторов человеческой нейтрофил-эластазы (NHE). 3 н. и 11 з.п. ф-лы, 97 пр.