Patent classifications
C07D497/08
BENZOLACTAM COMPOUNDS AS PROTEIN KINASE INHIBITORS
- Valerio Berdini ,
- Ildiko Maria Buck ,
- James Edward Harvey Day ,
- Charlotte Mary Griffiths-Jones ,
- Thomas Daniel Heightman ,
- Steven Howard ,
- Christopher William Murray ,
- David Norton ,
- Marc O'Reilly ,
- Alison Jo-Anne Woolford ,
- Michael Liam Cooke ,
- David Cousin ,
- Stuart Thomas Onions ,
- Jonathan Martin Shannon ,
- John Paul Watts
The invention provides a compound of formula (0):
##STR00001## or a pharmaceutically acceptable salt, N-oxide or tautomer thereof; wherein: n is 1 or 2; X is CH or N; Y is selected from CH and C—F; Z is selected from C—R.sup.z and N; R.sup.1 is selected from: -(Alk.sup.1).sub.t-Cyc.sup.1; wherein t is 0 or 1; Optionally substituted C.sub.1-6 acyclic hydrocarbon groups R.sup.2 is selected from hydrogen; halogen; and C.sub.1-3 hydrocarbon groups optionally substituted with one or more fluorine atoms; R.sup.3 is hydrogen or a group L.sup.1-R.sup.7; R.sup.4 is selected from hydrogen; methoxy; and optionally substituted C.sub.1-3 alkyl; and R.sup.4a is selected from hydrogen and a C.sub.1-3 alkyl group; wherein R.sup.z, Alk.sup.1, Cyc.sup.1, L.sup.1 and R.sup.7 are defined herein; provided that the compound is other than 6-benzyl-3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and 3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and salts and tautomers thereof.
The compounds are inhibitors of ERK1/2 kinases and will be useful in the treatment of ERK1/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.
BENZOLACTAM COMPOUNDS AS PROTEIN KINASE INHIBITORS
- Valerio Berdini ,
- Ildiko Maria Buck ,
- James Edward Harvey Day ,
- Charlotte Mary Griffiths-Jones ,
- Thomas Daniel Heightman ,
- Steven Howard ,
- Christopher William Murray ,
- David Norton ,
- Marc O'Reilly ,
- Alison Jo-Anne Woolford ,
- Michael Liam Cooke ,
- David Cousin ,
- Stuart Thomas Onions ,
- Jonathan Martin Shannon ,
- John Paul Watts
The invention provides a compound of formula (0):
##STR00001## or a pharmaceutically acceptable salt, N-oxide or tautomer thereof; wherein: n is 1 or 2; X is CH or N; Y is selected from CH and C—F; Z is selected from C—R.sup.z and N; R.sup.1 is selected from: -(Alk.sup.1).sub.t-Cyc.sup.1; wherein t is 0 or 1; Optionally substituted C.sub.1-6 acyclic hydrocarbon groups R.sup.2 is selected from hydrogen; halogen; and C.sub.1-3 hydrocarbon groups optionally substituted with one or more fluorine atoms; R.sup.3 is hydrogen or a group L.sup.1-R.sup.7; R.sup.4 is selected from hydrogen; methoxy; and optionally substituted C.sub.1-3 alkyl; and R.sup.4a is selected from hydrogen and a C.sub.1-3 alkyl group; wherein R.sup.z, Alk.sup.1, Cyc.sup.1, L.sup.1 and R.sup.7 are defined herein; provided that the compound is other than 6-benzyl-3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and 3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and salts and tautomers thereof.
The compounds are inhibitors of ERK1/2 kinases and will be useful in the treatment of ERK1/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.
PYRIDINYL DERIVATIVES AS SODIUM CHANNEL ACTIVATORS
The present disclosure is directed to compounds of formula (I):
##STR00001##
wherein X, Y, Z, R.sup.1, R.sup.2a, R.sup.2b, R.sup.3, and L are as described herein, as stereoisomers, enantiomers, or tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates, or prodrugs thereof, and pharmaceutical compositions comprising the compounds of formula (I), as described herein, which are useful as voltage-gated sodium channel modulators and are therefore are useful in treating seizure disorders such as epilepsy.
PYRIDINYL DERIVATIVES AS SODIUM CHANNEL ACTIVATORS
The present disclosure is directed to compounds of formula (I):
##STR00001##
wherein X, Y, Z, R.sup.1, R.sup.2a, R.sup.2b, R.sup.3, and L are as described herein, as stereoisomers, enantiomers, or tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates, or prodrugs thereof, and pharmaceutical compositions comprising the compounds of formula (I), as described herein, which are useful as voltage-gated sodium channel modulators and are therefore are useful in treating seizure disorders such as epilepsy.
CHEMICALLY AMPLIFIED POSITIVE-TYPE PHOTOSENSITIVE RESIN COMPOSITION, PHOTOSENSITIVE DRY FILM, PRODUCTION METHOD FOR PHOTOSENSITIVE DRY FILM, PRODUCTION METHOD FOR PATTERNED RESIST FILM, COMPOUND, PHOTO-ACID GENERATOR, AND PRODUCTION METHOD FOR N-ORGANOSULFONYLOXY COMPOUND
A chemically amplified positive-type photosensitive resin composition in which the acid generator included has excellent solubility in a solvent and with which a resist pattern having excellent mask linearity is easily formed; a photosensitive dry film having a photosensitive layer formed from the composition; a method of manufacturing the photosensitive dry film; a method of manufacturing a patterned resist film using the composition; and a compound and an acid generator which can be added to the composition. The composition includes an acid generator which generates acid when irradiated with an active ray or radiation, and a resin whose solubility in alkali increases under action of an acid.
Benzolactam compounds as protein kinase inhibitors
- Valerio Berdini ,
- Ildiko Maria Buck ,
- James Edward Harvey Day ,
- Charlotte Mary Griffiths-Jones ,
- Thomas Daniel Heightman ,
- Steven Howard ,
- Christopher William Murray ,
- David Norton ,
- Marc O'Reilly ,
- Alison Jo-Anne Woolford ,
- Michael Liam Cooke ,
- David Cousin ,
- Stuart Thomas Onions ,
- Jonathan Martin Shannon ,
- John Paul Watts
The invention provides a compound of formula (0): ##STR00001## or a pharmaceutically acceptable salt, N-oxide or tautomer thereof; wherein: n is 1 or 2; X is CH or N; Y is selected from CH and CF; Z is selected from CR.sup.z and N; R.sup.1 is selected from: -(Alk.sup.1).sub.t-Cyc.sup.1; wherein t is 0 or 1; Optionally substituted C.sub.1-6 acyclic hydrocarbon groups R.sup.2 is selected from hydrogen; halogen; and C.sub.1-3 hydrocarbon groups optionally substituted with one or more fluorine atoms; R.sup.3 is hydrogen or a group L.sup.1-R.sup.7; R.sup.4 is selected from hydrogen; methoxy; and optionally substituted C.sub.1-3 alkyl; and R.sup.4a is selected from hydrogen and a C.sub.1-3 alkyl group; wherein R.sup.z, Alk.sup.1, Cyc.sup.1, L.sup.1 and R.sup.7 are defined herein; provided that the compound is other than 6-benzyl-3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and 3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and salts and tautomers thereof. The compounds are inhibitors of ERK1/2 kinases and will be useful in the treatment of ERK1/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.
Benzolactam compounds as protein kinase inhibitors
- Valerio Berdini ,
- Ildiko Maria Buck ,
- James Edward Harvey Day ,
- Charlotte Mary Griffiths-Jones ,
- Thomas Daniel Heightman ,
- Steven Howard ,
- Christopher William Murray ,
- David Norton ,
- Marc O'Reilly ,
- Alison Jo-Anne Woolford ,
- Michael Liam Cooke ,
- David Cousin ,
- Stuart Thomas Onions ,
- Jonathan Martin Shannon ,
- John Paul Watts
The invention provides a compound of formula (0): ##STR00001## or a pharmaceutically acceptable salt, N-oxide or tautomer thereof; wherein: n is 1 or 2; X is CH or N; Y is selected from CH and CF; Z is selected from CR.sup.z and N; R.sup.1 is selected from: -(Alk.sup.1).sub.t-Cyc.sup.1; wherein t is 0 or 1; Optionally substituted C.sub.1-6 acyclic hydrocarbon groups R.sup.2 is selected from hydrogen; halogen; and C.sub.1-3 hydrocarbon groups optionally substituted with one or more fluorine atoms; R.sup.3 is hydrogen or a group L.sup.1-R.sup.7; R.sup.4 is selected from hydrogen; methoxy; and optionally substituted C.sub.1-3 alkyl; and R.sup.4a is selected from hydrogen and a C.sub.1-3 alkyl group; wherein R.sup.z, Alk.sup.1, Cyc.sup.1, L.sup.1 and R.sup.7 are defined herein; provided that the compound is other than 6-benzyl-3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and 3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and salts and tautomers thereof. The compounds are inhibitors of ERK1/2 kinases and will be useful in the treatment of ERK1/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.
BENZOLACTAM COMPOUNDS AS PROTEIN KINASE INHIBITORS
- Valerio Berdini ,
- Ildiko Maria Buck ,
- James Edward Harvey Day ,
- Charlotte Mary Griffiths-Jones ,
- Thomas Daniel Heightman ,
- Steven Howard ,
- Christopher William Murray ,
- David Norton ,
- Marc O'Reilly ,
- Alison Jo-Anne Woolford ,
- Michael Liam Cooke ,
- David Cousin ,
- Stuart Thomas Onions ,
- Jonathan Martin Shannon ,
- John Paul Watts
The invention provides a compound of formula (0):
##STR00001## or a pharmaceutically acceptable salt, N-oxide or tautomer thereof; wherein: n is 1 or 2; X is CH or N; Y is selected from CH and CF; Z is selected from CR.sup.z and N; R.sup.1 is selected from: -(Alk.sup.1).sub.t-Cyc.sup.1; wherein t is 0 or 1; Optionally substituted C.sub.1-6 acyclic hydrocarbon groups R.sup.2 is selected from hydrogen; halogen; and C.sub.1-3 hydrocarbon groups optionally substituted with one or more fluorine atoms; R.sup.3 is hydrogen or a group L.sup.1-R.sup.7; R.sup.4 is selected from hydrogen; methoxy; and optionally substituted C.sub.1-3 alkyl; and R.sup.4a is selected from hydrogen and a C.sub.1-3 alkyl group; wherein R.sup.z, Alk.sup.1, Cyc.sup.1, L.sup.1 and R.sup.7 are defined herein; provided that the compound is other than 6-benzyl-3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and 3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and salts and tautomers thereof.
The compounds are inhibitors of ERK1/2 kinases and will be useful in the treatment of ERK1/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.
BENZOLACTAM COMPOUNDS AS PROTEIN KINASE INHIBITORS
- Valerio Berdini ,
- Ildiko Maria Buck ,
- James Edward Harvey Day ,
- Charlotte Mary Griffiths-Jones ,
- Thomas Daniel Heightman ,
- Steven Howard ,
- Christopher William Murray ,
- David Norton ,
- Marc O'Reilly ,
- Alison Jo-Anne Woolford ,
- Michael Liam Cooke ,
- David Cousin ,
- Stuart Thomas Onions ,
- Jonathan Martin Shannon ,
- John Paul Watts
The invention provides a compound of formula (0):
##STR00001## or a pharmaceutically acceptable salt, N-oxide or tautomer thereof; wherein: n is 1 or 2; X is CH or N; Y is selected from CH and CF; Z is selected from CR.sup.z and N; R.sup.1 is selected from: -(Alk.sup.1).sub.t-Cyc.sup.1; wherein t is 0 or 1; Optionally substituted C.sub.1-6 acyclic hydrocarbon groups R.sup.2 is selected from hydrogen; halogen; and C.sub.1-3 hydrocarbon groups optionally substituted with one or more fluorine atoms; R.sup.3 is hydrogen or a group L.sup.1-R.sup.7; R.sup.4 is selected from hydrogen; methoxy; and optionally substituted C.sub.1-3 alkyl; and R.sup.4a is selected from hydrogen and a C.sub.1-3 alkyl group; wherein R.sup.z, Alk.sup.1, Cyc.sup.1, L.sup.1 and R.sup.7 are defined herein; provided that the compound is other than 6-benzyl-3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and 3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and salts and tautomers thereof.
The compounds are inhibitors of ERK1/2 kinases and will be useful in the treatment of ERK1/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.
BENZOLACTAM COMPOUNDS AS PROTEIN KINASE INHIBITORS
- Valerio Berdini ,
- Ildiko Maria Buck ,
- James Edward Harvey Day ,
- Charlotte Mary Griffiths-Jones ,
- Thomas Daniel Heightman ,
- Steven Howard ,
- Christopher William Murray ,
- David Norton ,
- Marc O'Reilly ,
- Alison Jo-Anne Woolford ,
- Michael Liam Cooke ,
- David Cousin ,
- Stuart Thomas Onions ,
- Jonathan Martin Shannon ,
- John Paul Watts
The invention provides a compound of formula (0):
##STR00001## or a pharmaceutically acceptable salt, N-oxide or tautomer thereof; wherein: n is 1 or 2; X is CH or N; Y is selected from CH and CF; Z is selected from CR.sup.z and N; R.sup.1 is selected from: -(Alk.sup.1).sub.t-Cyc.sup.1; wherein t is 0 or 1; Optionally substituted C.sub.1-6 acyclic hydrocarbon groups R.sup.2 is selected from hydrogen; halogen; and C.sub.1-8 hydrocarbon groups optionally substituted with one or more fluorine atoms; R.sup.3 is hydrogen or a group L.sup.1-R.sup.7; R.sup.4 is selected from hydrogen; methoxy; and optionally substituted C.sub.1-3 alkyl; and R.sup.4a is selected from hydrogen and a C.sub.1-3 alkyl group; wherein R.sup.z, Alk.sup.1, Cyc.sup.1, L.sup.1 and R.sup.7 are defined herein; provided that the compound is other than 6-benzyl-3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and 3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and salts and tautomers thereof.
The compounds are inhibitors of ERK1/2 kinases and will be useful in the treatment of ERK1/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.