Novel 4-cyano, 4-amino, and 4-aminomethyl Derivatives of Pyrazolo[1,5-a]pyridines, Pyrazolo[1,5-c]pyrimidines and 2-H-indazole Compounds and 5-cyano, 5-amino, and 5-aminomethyl Derivatives of Imidazo[1,2-a]pyridines, and Imidazo[1,5-a]pyrazines Compounds

MALLAMS, Alan, Vincent MADISON and Kamil PARUCH. Novel 4-cyano, 4-amino, and 4-aminomethyl Derivatives of Pyrazolo[1,5-a]pyridines, Pyrazolo[1,5-c]pyrimidines and 2-H-indazole Compounds and 5-cyano, 5-amino, and 5-aminomethyl Derivatives of Imidazo[1,2-a]pyridines, and Imidazo[1,5-a]pyrazines Compounds. 2007.

Basic information

• Original name: Novel 4-cyano, 4-amino, and 4-aminomethyl Derivatives of Pyrazolo[1,5-a]pyridines, Pyrazolo[1,5-c]pyrimidines and 2-H-indazole Compounds and 5-cyano, 5-amino, and 5-aminomethyl Derivatives of Imidazo[1,2-a]pyridines, and Imidazo[1,5-a]pyrazines Compounds
• Name in Czech: Novel 4-cyano, 4-amino, and 4-aminomethyl Derivatives of Pyrazolo[1,5-a]pyridines, Pyrazolo[1,5-c]pyrimidines and 2-H-indazole Compounds and 5-cyano, 5-amino, and 5-aminomethyl Derivatives of Imidazo[1,2-a]pyridines, and Imidazo[1,5-a]pyrazines Compounds
• Authors: MALLAMS, Alan, Vincent MADISON and Kamil PARUCH.
• Edition: Number: WO 2007/032936 A2, Publisher: World Intellectula Property Organization, Place of publication: USA, Owner's name: Schering-Plough, 2007.

Other information

• Original language: English
• Type of outcome: Patent
• Field of Study: 10401 Organic chemistry
• Country of publisher: United States of America
• Confidentiality degree: is not subject to a state or trade secret
• Organization unit: Faculty of Science
• Keywords (in Czech): cyclin dependent kinase; inhibitor
• Keywords in English: cyclin dependent kinase; inhibitor
• Tags: Cyclin dependent kinase, inhibitor

Abstract

The invention provides a class of bicyclic heterocyclic compds. of formulas I, II, and III as inhibitors of cyclin dependent kinases, methods of prepg. such compds., pharmaceutical compns. contg. one or more such compds., methods of prepg. pharmaceutical formulations comprising one or more such compds., and methods of treatment, prevention, inhibition, or amelioration of one or more diseases assocd. with the CDKs using such compds. or pharmaceutical compns. Compds. of formulas I, II, and III wherein X is C or N; Y is CH, NH2, and CH2NH2; R1 is H, halo, NH2, (un)substituted alkyl, alkenyl, (hetero)aryl, CF3, etc.; R2 is H, halo, NH2 and derivs., CO2H and derivs., CONH2 and derivs., alkyl, alkenyl, alkynyl, cycloalkyl, (hetero)aryl, etc.; R3 is halo, CN, amino, alkylamino, cycloalkylamino, arylakylamino, hydroxyalkylamino, etc.; R4 is H, halo, CN and alkyl; are claimed. Example compd. IV was prepd. by cyanation of 5-bromo-6-phenyl-8-(pyridin-3-ylmethylamino)imidazo[1,5-a]pyrazine with zinc cyanide. All the invention compds. were evaluated for their CDK inhibitory activity.

Abstract (in Czech)

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