- METHODS AND COMPOUNDS FOR RESTORING MUTANT p53 FUNCTION
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Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods to recover wild-type function to p53 mutants. The compounds of the present disclosure can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.
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Paragraph 01022
(2021/11/20)
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- IMIDAZOPIPERAZINONE INHIBITORS OF TRANSCRIPTION ACTIVATING PROTEINS
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The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of transcription activating proteins such as CBP and P300 for the treatment or prevention of diseases such as proliferative diseases, inflammatory disorders, autoimmune diseases, and fibrotic diseases.
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Paragraph 0791; 0792
(2019/10/20)
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- 4-substituted or unsubstituted tetrahydropyran-4-carboxylic acid or its ester compound compd.
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A process for producing a 4-(un)substituted tetrahydropyran-4-carboxylic acid compound or an ester compound thereof which are represented by the formula (1): (1) (wherein R represents hydrogen or a hydrocarbon group; R represents hydrogen or an optionally substituted hydrocarbon group; and R represents hydrogen or a hydrocarbon group), characterized by reacting a 4-(un)substituted 4-cyanotetrahydropyran compound represented by the formula (2): (2) (wherein R and R are the same as defined above) with water or an alcohol which are represented by the formula (3): ROH (3) (wherein R is the same as defined above) in the presence of an acid or base.
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Paragraph 0070
(2016/12/16)
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- SUBSTITUTED TETRAHYDRONAPHTHALENES, METHOD FOR THE PRODUCTION THEREOF, AND USE THEREOF AS DRUGS
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The invention relates to substituted tetrahydronaphthalenes, to derivatives thereof, to physiologically acceptable salts thereof, to physiologically functional derivatives, to the production thereof, to drugs containing at least one substituted tetrahydronaphthalene according to the invention or derivative thereof, and to the use of the substituted tetrahydronaphthalenes according to the invention and to derivatives thereof as MCH antagonists.
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Page/Page column 51
(2012/02/01)
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- NOVEL SUBSTITUTED INDANES, METHOD FOR THE PRODUCTION THEREOF, AND USE THEREOF AS DRUGS
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The invention relates to substituted indanes and derivatives thereof, to physiologically acceptable salts and physiologically functional derivatives thereof, to the production thereof, to drugs containing at least one substituted indane according to the invention or derivative thereof, and to the use of the substituted indanes according to the invention and to derivatives thereof as MCH antagonists.
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Page/Page column 64
(2012/02/03)
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- PHENYL-HETEROARYL AMINE COMPOUNDS AND THEIR USES
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The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds of Formula I, and pharmaceutical compositions comprising such compounds
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Page/Page column 80
(2012/06/01)
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- 3-(AMINOARYL)-PYRIDINE COMPOUNDS
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The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided are pharmaceutical compositions containing these compounds and methods of treating a disease or condition mediated by CDK9 using these compounds and compositions.
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Page/Page column 87-88
(2012/06/01)
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- N-ACYL PYRIDINE BIARYL COMPOUNDS AND THEIR USES
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The present invention provides a compound of general formula:wherein Z2-Z6 include one or two nitrogen atoms as described herein, including pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds of Formula I and isomers thereof, and pharmaceutical compositions comprising such compounds.
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Page/Page column 113
(2012/08/08)
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- PYRIDINE BIARYL AMINE COMPOUNDS AND THEIR USES
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The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds of Formula I and isomers thereof, and pharmaceutical compositions comprising such compounds.
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Page/Page column 95-96; 163
(2012/08/08)
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- N-ACYL PYRIMIDINE BIARYL COMPOUNDS AS PROTEIN KINASE INHIBITORS
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The present invention provides a compound of the general formula (1): wherein one of X and Y is N and the other is an optionally substituted carbon atom, and Z2-Z5 represent one or two nitrogen atoms, as further described herein, including pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals and as components of pharmaceutical compositions. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds described herein or pharmaceutical compositions comprising such compounds.
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Page/Page column 154
(2012/08/08)
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- PYRIMIDINE BIARYL AMINE COMPOUNDS AND THEIR USES
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The present invention provides a pyrimidine compound of formula (I): wherein one of X and Y but not both is N, and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tantomers, diastereomers, deuterated versions, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds of Formula I and isomers thereof, and pharmaceutical compositions comprising such compounds
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Page/Page column 84
(2012/08/08)
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- PYRAZINYLPYRIDINES USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISEASES
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The present invention provides a compound of Formula (I) and pharmaceutically acceptable salts thereof. Also provided is a method of using a compound of Formula I for treating a disease or condition mediated by a CDK inhibitor.
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Page/Page column 62
(2011/04/14)
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- HETEROARYL COMPOUNDS AS KINASE INHIBITORS
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The present invention provides a compound of Formula (I): and pharmaceutically acceptable salts thereof. Also provided is a method of using a compound of Formula I for treating a disease or condition mediated by a CDK inhibitor
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Page/Page column 62-63
(2011/04/14)
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