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    PYRAZINE COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
    2.
    发明专利
    PYRAZINE COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE 未知

    公开(公告)号：NZ593316A

    公开(公告)日：2013-06-28

    申请号：NZ59331609

    申请日：2009-11-10

    Applicant: VERTEX PHARMA

    Inventor： CHARRIER JEAN-DAMIEN ,  DURRANT STEVEN ,  KAY DAVID ,  O DONNELL MICHAEL ,  KNEGTEL RONALD ,  MACCORMICK SOMHAIRLE ,  PINDER JOANNE ,  VIRANI ANISA ,  YOUNG STEPHEN ,  BINCH HAYLEY ,  CLEVELAND THOMAS ,  FANNING LEV T

    IPC: C07D413/04 ,  A61K31/4965 ,  A61P35/00 ,  C07D401/04 ,  C07D403/04

    Abstract: 593316 The present disclosure relates to pyrazine compounds of formula (Ia) wherein L, n, R1, and R2 are as described in the specification. These compounds are useful as inhibitors of ATR protein kinase. The disclosure also relates to pharmaceutically acceptable compositions comprising the compounds of the disclosure; methods of treating of various diseases, disorders, and conditions using the compounds of the disclosure; processes for preparing the compounds of the disclosure; intermediates for the preparation of the compounds of the disclosure; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. Compounds of the present disclosure include: 2-[5-Amino-6-[5-[4-(methylaminomethyl)phenyl]-1,3,4-oxadiazol-2-yl]pyrazin-2-yl]-N-ethyl-cyclopropanecarboxamide, 1-(4-(5-Amino-6-(5-( 4-((methylamino)methyl)phenyl)-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)piperidin-1-yl)propan-1-one, 1-(7-(5-Amino-6-(5-( 4-CCmethylamino)methy])phenyl)-I,3A-oxadiazol-2-y])pyrazin-2-y])-2,7-diazaspiro[4,4]nonan-2-y])propan-1-one, 1-{ 7-(5-Amino-6-(5-(4-((methylamino)methyllphenyl)-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)-2,7-diazaspiro[4,4]nonan-2-yl} propan-1-one, 1-[S-amino-6-(S-phenyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yI]-3 ,6-dihydro-2H-pyridine-4-carboxylic acid, 3-{ [1,2,4(triazolo[1,S-alpyridin-2-y])-S-(1-(ethylsulfony])-1,2,3,6-tetrahydropyridin-4-y])pyrazin-2-amine, 3-amino-N-(pyridin-2-yl)-6-(4-(thiophen-3-ylsulfonyl)piperazin-1-yl)pyrazine-2-carboxamide, 3-amino-6-(4-(phenylcarbonyl)piperazin-1-yl)-N-(pyridin-2-yl)pyrazine-2-carboxamide, 3-(1H-benzo[d]imidazol-2-yl)-5-(1-(thiophen-2-ylsulfonyl)-1,2,3,6-tetrahydropyridin-4-yl)pyrazin-2-amine and 4-(5-amino-6-(3H-imidazo[4,5-b]pyridin-2-yl)pyrazin-2-yl)-N,N-dimethyl-5,6-dihydropyridine-1(2H)-sulfonamide

    MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
    5.
    发明专利
    MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR 未知

    公开(公告)号：NZ592687A

    公开(公告)日：2013-04-26

    申请号：NZ59268709

    申请日：2009-10-23

    Applicant: VERTEX PHARMA

    Inventor： BINCH HAYLEY ,  FANNING LEV T

    IPC: C07D487/08 ,  A61K31/4709 ,  A61P11/00 ,  A61P43/00

    Abstract: 592687 Disclosed herein is a compound of Formula I wherein: Ring A is a 7-azanorbornanyl or 8-azabicyclo(3.2.1)octanyl ring system R1 is -CH3, -CF3 or -CN, R2 is hydrogen, -CH3, -CF3, -OH, or -CH2OH, R3 is hydrogen, -CH3, -OCH3, or -CN; provided that both R2 and R3 are not simultaneously hydrogen, Ra is hydrogen or a silyl protecting group, and one of X and Y is nitrogen and the other is carbon; the use thereof in the treatment of a disease, such as cystic fibrosis or a disease associated with modulation of CFTR activity; and a process for the preparation thereof comprising: reacting a compound of formula 2a with an amine of formula 3 to provide a compound of formula 2b, converting the compound of formula 2b to the amine of formula 2e via hydrogenation, reacting the amine of formula 2c with an acid of formula Id to provide a compound of formula Ic, and optionally further comprising a deprotection step wherein Ra is a silyl protecting group. Exemplary compounds include: N-(6-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)pyridin-3-yl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide, and N-(6-(7-azabicyclo[2.2.1]heptan-7-yl)-4-methylpyridin-3-yl)-S-methyl-4-oxo-1,4-dihydroquinohne-3-carboxamide hydrochloride.

    MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
    6.
    发明专利
    MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR 未知

    公开(公告)号：NZ592685A

    公开(公告)日：2013-04-26

    申请号：NZ59268509

    申请日：2009-10-23

    Applicant: VERTEX PHARMA

    Inventor： BINCH HAYLEY ,  FANNING LEV T

    IPC: C07D451/02 ,  A61K31/439 ,  A61P11/00

    Abstract: 592685 Disclosed is a compound of formula (I) which is an azabicyclic substituted on a phenyl group which in turn is substituted on a dihydroquinoline. Examples of compounds of formula (I) are: N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2- (trifluoromethyl)phenyl)-4-oxo-5-( trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide; N-(4-(7-azabicydo[2.2.1]heptan-7-yl)-2-cyanophenyl)-5-methyl-4-oxo-1,4-dihydroquinoline-3-carboxamide and N-[4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(3-dimethylaminoprop-1-ynyl)phenyl]-4-oxo-5-(trifluoromethyl)-1H -quinoline-3-carboxamide. Also disclosed are pharmaceutical compositions and kits comprising a compound of formula (I) Further disclosed is the use of a compound of formula (I) in the manufacture of a medicament for the treatment of diseases such as cystic fibrosis, COPD, liver diseases and Alzheimer's disease.

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