Abstract: The invention provides a pharmaceutically acceptable salt of 5-[[5-[4-(4-fluoro-1-methyl-4-piperidyl)-2-methoxy-phenyl]-1H-pyrazol-3-yl]amino]pyrazine-2-carbonitrile which is selected from maleate, tosylate, besylate and malonate salts. Also provided are particular crystalline forms of the salts, methods for the preparation of the salts, pharmaceutical compositions containing the salts and their therapeutic uses.

Abstract: The invention provides a novel synthetic route for the preparation of the Chk-1 inhibitor compound: as well as novel process intermediates per se.

Abstract: The present invention relates to (R)-4-[5-(4-chlorophenyl)-1-[2-(trifluoromethyl)-phenyl]pyrrol-2-yl]-N-[2-(dimethylamino)-ethyl]benzamide (+)-L-tartrate salt, methods for its preparation, pharmaceutical compositions containing it and its use in treating diseases such as cancer.

Abstract: The invention provides compounds of the formula (3): or a pharmaceutically acceptable salt or tautomer thereof, wherein: Z is a 5-membered heteroaryl ring containing one or two nitrogen ring members and optionally one further heteroatom ring member selected from N and O; ring X is a benzene or pyridine ring; ring Y is a benzene, pyridine, thiophene or furan ring; Ar1 is an optionally substituted benzene, pyridine, thiophene or furan ring; m is 0, 1 or 2; n is 0, 1 or 2; R1 is selected from various substituents: R2 is selected from hydrogen and a C1-4 hydrocarbon group; R3 is selected from hydrogen and a C1-4 hydrocarbon group; R4 is selected from various substituents; R5 is selected from various substituents; Ar2 is an optionally substituted phenyl, pyridyl or pyridone group; R6 is a group Q1-Ra—Rb; Q1 is absent or is a C1-3 saturated hydrocarbon linker; Ra is selected from O; C(O); C(O)O; CONRc; N(Rc)CO; N(Rc)CONRc, NRc; and SO2NRc; Rb is selected from hydrogen and various substituents; and Rb is selec

Abstract: This invention relates to compounds that inhibit or modulate the activity of Chk-1 kinase. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds.

Abstract: The invention provides a composition of matter which: (i) consists of at least 90% by weight of an atropisomer (2A) and 0-10% by weight of an atropisomer of formula (2B); or (ii) consists of at least 90% by weight of an atropisomer (2B) and 0-10% by weight of an atropisomer of formula (2A); wherein the atropisomer of formula (2A) and the atropisomer of formula (2B) are represented by: or are pharmaceutically acceptable salts or tautomers thereof, wherein ring X is a benzene or pyridine ring; ring Y is selected from a benzene ring, a pyridine ring and a thiophene ring; R1 is trifluoromethyl; R2 is hydrogen; R3 is hydrogen; m is 0 or 1; n is 0, 1 or 2; Ar1 is a monocyclic aromatic ring selected from benzene and pyridine; each monocyclic aromatic ring being unsubstituted or substituted with 1 or 2 substituents R5 as defined herein; and R4; R5 when present, R6 and R7 independently selected from various substituents as defined herein.

Abstract: The invention provides compounds of the formula (3): or a pharmaceutically acceptable salt or tautomer thereof, wherein: Z is a 5-membered heteroaryl ring containing one or two nitrogen ring members and optionally one further heteroatom ring member selected from N and O; ring X is a benzene or pyridine ring; ring Y is a benzene, pyridine, thiophene or furan ring; Ar1 is an optionally substituted benzene, pyridine, thiophene or furan ring; m is 0, 1 or 2; n is 0, 1 or 2; R1 is selected from various substituents: R2 is selected from hydrogen and a C1-4 hydrocarbon group; R3 is selected from hydrogen and a C1-4 hydrocarbon group; R4 is selected from various substituents; R5 is selected from various substituents; Ar2 is an optionally substituted phenyl, pyridyl or pyridone group; R6 is a group Q1-Ra—Rb; Q1 is absent or is a C1-3 saturated hydrocarbon linker; Ra is selected from O; C(O); C(O)O; CONRc; N(Rc)CO; N(Rc)CONRc, NRc; and SO2NRc; Rb is selected from hydrogen and various substituents; and Rb is selecte

Abstract: The invention provides compounds of the formula (3): or a pharmaceutically acceptable salt or tautomer thereof, wherein: Z is a 5-membered heteroaryl ring containing one or two nitrogen ring members and optionally one further heteroatom ring member selected from N and O; ring X is a benzene or pyridine ring; ring Y is a benzene, pyridine, thiophene or furan ring; Ar1 is an optionally substituted benzene, pyridine, thiophene or furan ring; m is 0, 1 or 2; n is 0, 1 or 2; R1 is selected from various substituents: R2 is selected from hydrogen and a C1-4 hydrocarbon group; R3 is selected from hydrogen and a C1-4 hydrocarbon group; R4 is selected from various substituents; R5 is selected from various substituents; Ar2 is an optionally substituted phenyl, pyridyl or pyridone group; R6 is a group Q1-Ra—Rb; Q1 is absent or is a C1-3 saturated hydrocarbon linker; Ra is selected from O; C(O); C(O)O; CONRc; N(Rc)CO; N(Rc)CONRc, NRc; and SO2NRc; Rb is selected from hydrogen and various substituents;

Abstract: This invention relates to compounds that inhibit or modulate the activity of Chk-1 kinase. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds.

Abstract: This invention relates to compounds that inhibit or modulate the activity of Chk-1 kinase. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds.

Abstract: The invention provides compounds of the formula (3): or a pharmaceutically acceptable salt or tautomer thereof, wherein: Z is a 5-membered heteroaryl ring containing one or two nitrogen ring members and optionally one further heteroatom ring member selected from N and O; ring X is a benzene or pyridine ring; ring Y is a benzene, pyridine, thiophene or furan ring; Ar1 is an optionally substituted benzene, pyridine, thiophene or furan ring; m is 0, 1 or 2; n is 0, 1 or 2; R1 is selected from various substituents: R2 is selected from hydrogen and a C1-4 hydrocarbon group; R3 is selected from hydrogen and a C1-4 hydrocarbon group; R4 is selected from various substituents; R5 is selected from various substituents; Ar2 is an optionally substituted phenyl, pyridyl or pyridone group; R6 is a group Q1-Ra—Rb; Q1 is absent or is a C1-3 saturated hydrocarbon linker; Ra is selected from O; C(O); C(O)O; CONRc; N(Rc)CO; N(Rc)CONRc, NRc; and SO2NRc; Rb is selected from hydrogen and various substituents;

Abstract: The invention provides compound that inhibit or modulate the activity of p70S6 kinase, the compounds being of the formula (1): or a salt, tautomer or N-oxide thereof; wherein: one of Y and Z is R3 and the other is Ar2; Q1 is an optionally substituted C1-8 alkylene group; and wherein a carbon atom of the C1-8 alkylene group may optionally be replaced by a cyclopropane-1,1-diyl or cyclobutane-1,1-diyl group provided that the total number of carbon atoms in an alkylene group containing such a replacement does not exceed 8; Q2 is a bond or an optionally substituted C1-8 alkylene group R1 is selected from hydrogen, NRxRy and a group Cy1; Rx and Ry are each is selected from hydrogen, C1-4 hydrocarbyl or hydroxy-C1-4 hydrocarbyl; or NRxRy forms an optionally substituted 4 to 7-membered heterocyclic ring; Cy1 is an optionally substituted C-linked 3 to 7 membered monocyclic non-aromatic carbocyclic or heterocyclic; R2 and R4 are each is selected from hydrogen, fluorine, chlorine, optionally substituted C1-2 al

Abstract: The invention provides compound that inhibit or modulate the activity of p70S6 kinase, the compounds being of the formula (1): or a salt, tautomer or N-oxide thereof; wherein: one of Y and Z is R3 and the other is Ar2; Q1 is an optionally substituted C1-8 alkylene group; and wherein a carbon atom of the C1-8 alkylene group may optionally be replaced by a cyclopropane-1,1-diyl or cyclobutane-1,1-diyl group provided that the total number of carbon atoms in an alkylene group containing such a replacement does not exceed 8; Q2 is a bond or an optionally substituted C1-8 alkylene group R1 is selected from hydrogen, NRxRy and a group Cy1; Rx and Ry are each is selected from hydrogen, C1-4 hydrocarbyl or hydroxy-C1-4 hydrocarbyl; or NRxRy forms an optionally substituted 4 to 7-membered heterocyclic ring; Cy1 is an optionally substituted C-linked 3 to 7 membered monocyclic non-aromatic carbocyclic or heterocyclic; R2 and R4 are each is selected from hydrogen, fluorine, chlorine, optionally substituted C1-2 al

Abstract: The invention provides compound that inhibit or modulate the activity of p70S6 kinase, the compounds being of the formula (1): or a salt, tautomer or N-oxide thereof; wherein: one of Y and Z is R3 and the other is Ar2; Q1 is an optionally substituted C1-8 alkylene group; and wherein a carbon atom of the C1-8 alkylene group may optionally be replaced by a cyclopropane-1,1-diyl or cyclobutane-1,1-diyl group provided that the total number of carbon atoms in an alkylene group containing such a replacement does not exceed 8; Q2 is a bond or an optionally substituted C1-8 alkylene group R1 is selected from hydrogen, NRxRy and a group Cy1; Rx and Ry are each is selected from hydrogen, C1-4 hydrocarbyl or hydroxy-C1-4 hydrocarbyl; or NRxRy forms an optionally substituted 4 to 7-membered heterocyclic ring; Cy1 is an optionally substituted C-linked 3 to 7 membered monocyclic non-aromatic carbocyclic or heterocyclic; R2 and R4 are each is selected from hydrogen, fluorine, chlorine, optionally substituted C1-2 al

Abstract: The invention provides compound that inhibit or modulate the activity of p70S6 kinase, the compounds being of the formula (1): or a salt, tautomer or N-oxide thereof; wherein: one of Y and Z is R3 and the other is Ar2; Q1 is an optionally substituted C1-8 alkylene group; and wherein a carbon atom of the C1-8 alkylene group may optionally be replaced by a cyclopropane-1,1-diyl or cyclobutane-1,1-diyl group provided that the total number of carbon atoms in an alkylene group containing such a replacement does not exceed 8; Q2 is a bond or an optionally substituted C1-8 alkylene group R1 is selected from hydrogen, NRxRy and a group Cy1; Rx and Ry are each is selected from hydrogen, C1-4 hydrocarbyl or hydroxy-C1-4 hydrocarbyl; or NRxRy forms an optionally substituted 4 to 7-membered heterocyclic ring; Cy1 is an optionally substituted C-linked 3 to 7 membered monocyclic non-aromatic carbocyclic or heterocyclic; R2 and R4 are each is selected from hydrogen, fluorine, chlorine, optionally substituted C1-2 alkyl

Abstract: The invention provides compounds for use in the treatment of a disease or condition selected from brain disorders and triple-negative breast cancer, the compounds being of the formula (1): or a salt or tautomer thereof; wherein: X1 is N or N+(O?); X2 is N or CH; Q is selected from a C1-3 alkylene group, cyclopropane-1,1-diyl and cyclobutane-1,1-diyl; R1 is selected from hydrogen and C1-4 alkyl; R2, R3 and R4 are the same or different and each is selected from hydrogen and fluorine; Ar1 is a benzene, thiophene, naphthyl or pyridine ring optionally substituted with 1, 2 or 3 substituents selected from fluorine; chlorine; bromine; C1-4 hydrocarbyl; C1-4 hydrocarbyloxy; trifluoromethyl; difluoromethyl; cyano; trifluoromethoxy; difluoromethoxy; Ar2 is a monocyclic 5- or 6-membered heteroaryl ring containing 1, 2 or 3 heteroatom ring members selected from O, N and S and being optionally substituted with 1, 2 or 3 substituents selected from fluorine; C1-4 hydrocarbyl; amino; mono-C1-4 hydrocarbylamino and di

Abstract: The invention provides compounds for use in the treatment of a disease or condition selected from brain disorders and triple-negative breast cancer, the compounds being of the formula (1): or a salt or tautomer thereof; wherein: X1 is N or N+(O?); X2 is N or CH; Q is selected from a C1-3 alkylene group, cyclopropane-1,1-diyl and cyclobutane-1,1-diyl; R1 is selected from hydrogen and C1-4 alkyl; R2, R3 and R4 are the same or different and each is selected from hydrogen and fluorine; Ar1 is a benzene, thiophene, naphthyl or pyridine ring optionally substituted with 1, 2 or 3 substituents selected from fluorine; chlorine; bromine; C1-4 hydrocarbyl; C1-4 hydrocarbyloxy; trifluoromethyl; difluoromethyl; cyano; trifluoromethoxy; difluoromethoxy; Ar2 is a monocyclic 5- or 6-membered heteroaryl ring containing 1, 2 or 3 heteroatom ring members selected from O, N and S and being optionally substituted with 1, 2 or 3 substituents selected from fluorine; C1-4 hydrocarbyl; amino; mono-C1-4 hydrocarbylamino and di-

Abstract: The invention provides compounds which inhibit or modulate the activity of Chk-1 kinase and which are useful in the treatment of cancer.

Abstract: The invention provides compounds which inhibit or modulate the activity of Chk-1 kinase and which are useful in the treatment of cancer. The compounds have the general formula (1): and salts, N-oxides and tautomers thereof, wherein m is 2, 3 or 4; n is 0 or 1; Q1 is selected from a bond; C(?O); S(O); SO2; and an alkylene chain of 1 to 4 carbon atoms in length between the moiety R4 and the nitrogen atom.

Abstract: A compound of the formula (I):