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    ПРОИЗВОДНЫЕ 5,6-ДИГИДРОИМИДАЗО[1,2-А]ПИРАЗИН-8-ИЛАМИНА, ПРИГОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (ВАСЕ)
    6.
    发明专利
    ПРОИЗВОДНЫЕ 5,6-ДИГИДРОИМИДАЗО[1,2-А]ПИРАЗИН-8-ИЛАМИНА, ПРИГОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (ВАСЕ) 未知

    公开(公告)号：EA022409B1

    公开(公告)日：2015-12-30

    申请号：EA201390932

    申请日：2011-12-21

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： TRABANCO-SUAREZ ANDRES AVELINO ,  DELGADO-JIMENEZ FRANCISCA ,  VEGA RAMIRO JUAN ANTONIO ,  TRESADERN GARY JOHN ,  GIJSEN HENRICUS JACOBUS MARIA ,  OEHLRICH DANIEL

    IPC: C07D487/04 ,  A61K31/5025 ,  A61P25/00

    Abstract: Настоящееизобретениеотноситсяк производным 5,6-дигидроимидазо[1,2-а]пиразин-8-иламинаформулы (I)гдезначения R, R, R, X-X, L и Ar определеныв формулеизобретения, вкачествеингибиторовбета-секретазы, такжеизвестнойкакферментрасщепленияамилоидапобета-сайту, ВАСЕ, ВАСЕ1, Asp2 илимемапсин 2. Изобретениетакжеотноситсяк фармацевтическимкомпозициям, содержащимтакиесоединения, способамполучениятакихсоединенийи композицийи кприменениютакихсоединенийи композицийдляпрофилактикии лечениязаболеваний, вкоторыевовлеченабета-секретаза, такихкакболезньАльцгеймера (AD), умеренныекогнитивныенарушения, деменция, деменцияс тельцамиЛеви, церебральнаяамилоиднаяангиопатия, мультиинфарктнаядеменция, деменция, ассоциированнаяс инсультом, деменция, ассоциированнаяс болезньюПаркинсона, илидеменция, ассоциированнаяс бета-амилоидом.

    4,7-dihydro-pyrazolo[1,5-a]pyrazin-6-ylamine derivatives useful as inhibitors of beta-secretase (bace)
    7.
    发明专利
    4,7-dihydro-pyrazolo[1,5-a]pyrazin-6-ylamine derivatives useful as inhibitors of beta-secretase (bace) 未知

    公开(公告)号：NZ606848A

    公开(公告)日：2015-01-30

    申请号：NZ60684811

    申请日：2011-09-20

    Applicant: JANSSEN PHARMACEUTICA NV

    Inventor： TRABANCO-SUÁREZ ANDRÉS AVELINO ,  TRESADERN GARY JOHN ,  DELGADO-JIMÉNEZ FRANCISCA

    IPC: C07D487/04 ,  A61K31/4162 ,  A61K31/4985 ,  A61P25/28

    Abstract: Disclosed are N-{ 3-[6-amino-4-methyl-2-(trifluoromethyl)-4,7-dihydropyrazolo[1,5-a]pyrazin-4-yl]-phenyl} -benzamide derivatives as represented by the general formula (I), or a tautomer or a stereoisomeric form thereof, wherein R1 and R2 are independently selected from the group consisting of hydrogen, fluoro, cyano, alkyl, mono- and polyhalo-alkyl, and cycloalkyl; or R1 and R2 taken together with the carbon atom to which they are attached may form a cycloalkanediyl ring; R3 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, mono- and polyhalo-alkyl, homoaryl and heteroaryl; X1, X2, X3, X4 are independently C(R4) or N, provided that no more than two thereof represent N; each R4 is selected from the group consisting of hydrogen, halo, alkyl, mono- and polyhalo-alkyl, cyano, alkyloxy, mono- and polyhalo-alkyloxy; L is a bond or -N(R5)CO-, wherein R5 is hydrogen or alkyl; R6 is hydrogen or trifluoromethyl; Ar is homoaryl or heteroaryl; homoaryl is phenyl or phenyl substituted with one, two or three substituents selected from the group consisting of halo, cyano, alkyl, alkyloxy, mono and polyhalo-alkyl; and mono- and polyhalo-alkyloxy; heteroaryl is selected from the group consisting of pyridyl, pyrimidyl, pyrazyl, pyridazyl, furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, triazolyl, thiazolyl, thiadiazolyl, oxazolyl, and oxadiazolyl, each optionally substituted with one, two or three substituents selected from the group consisting of halo, cyano, alkyl, alkyloxy, mono- and polyhalo-alkyl; and mono- and polyhalo-alkyloxy; or an addition salt or a solvate thereof. Representative compounds of formula (I) include N-{ 3-[6-amino-4-methyl-2-(trifluoromethyl)-4,7-dihydropyrazolo[1,5-a]pyrazin-4-yl]-4-fluorophenyl} -3,5-dichloropyridine-2-carboxamide, (R)-N-{ 3-[6-amino-4-cyclopropyl-4,7-dihydropyrazolo[1,5-a]pyrazin-4-yI]-4-fluorophenyl} -5-chloro-3-fluoropyridine-2-carboxamide, (R)-4-(3’-methoxybiphenyl-3-yl)-4-methyl-4,7-dihydropyrazolo[1,5-a]pyrazin-6-amine, (R)-4-(3-(3-methoxy-pyridin-5-yl)-phenyl)-4-methyl-4,7-dihydropyrazolo[1,5-a]pyrazin-6-amine and (S)-N-[3-(6-amino-4-methyl-4,7-dihydropyrazolo[1,5-a]pyrazin-4-yl)-4-fluorophenyl]-5-chloropyridine-2-carboxamide. Further disclosed is a pharmaceutical composition comprising a therapeutically effective amount of a compound as defined above and a pharmaceutically acceptable carrier for use in the treatment, prevention or prophylaxis of Alzheimer’s disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down’s syndrome, dementia associated with stroke, dementia associated with Parkinson’s disease or dementia associated with beta-amyloid.

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