Patent NZ-501613-A (NZ)
Title: Benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-4-(4-pyridinylacetyl) piperazine derivatives useful as inhibitors of farnesyl-protein transferase
Inventor: ROSENBLUM STUART B
IPC: C07D401/14
Filed: 1998-06-15
Abstract: A compound selected from: 1-(3-Bromo-6,11-dihydro-8,10-dimethoxy-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-4-(4-pyridinylacetyl)piperazine N4-oxide; 4-(6,11-Dihydro-10-methoxy-3,8-dimethyl-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-(4-pyridinylacetyl)piperidine N1-oxide; (+,-)-4-(3-Bromo-10-methoxy-8-methyl-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-(4-pyridinylacetyl)piperidine N1-oxide; (+,-)-4-(6,11-Dihydro-10-methoxy-8-methyl-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-(4-pyridinylacetyl)piperidine N1-oxide; (+,-)-4-(7-Chloro-5,6-dihydro-8-methyl-10-methoxy-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-(4-pyridinylacetyl)piperidine N1-oxide; (+,-)-4-(3-Bromo-10-hydroxy-8-methyl-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-(4-pyridinylacetyl)piperidine N1-oxide; 4-(5,6-Dihydro-10-methoxy-3,8-dimethyl-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-(4-pyridinylacetyl)piperidine N1-oxide; (+,-)-4-(3-Bromo-10-methoxy-8-methyl-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-(4-pyridinylacetyl)piperidine N1-oxide; (+,-)-4-(3-Bromo-10-hydroxy-8-methyl-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-(4-pyridinylacetyl)piperidine N1-oxide; (+,-)-1-(3-Bromo-10-methoxy-8-methyl-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-4-(4-pyridinylacetyl)piperazine N4-oxide; (+,-)-1-(3-Bromo-7-methyl-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)4-( 4-pyridinylacetyl)piperazine N4-oxide; (+,-)-1-(3-Bromo-7,10-dimethyl-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-4-(4-pyridinylacetyl)piperazine N4-oxide; (+,-)-1-(3-Bromo-8-methyl-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-4-(4-pyridinylacetyl)piperazine N4-oxide; (+,-)-1-(3-Bromo-6,11-dihydro-8-methoxy-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-4-(4-pyridinylacetyl)piperazine N4-oxide; (+,-)-1-(3-Bromo-6,11-dihydro-8,10-dimethyl-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-4-(4-pyridinylacetyl)piperazine N4-oxide; (-)-1-(3-Bromo-10-methoxy-8-methyl-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-4-(4-pyridinylacetyl)piperazine N4-oxide; (+)-1-(3-Bromo-10-methoxy-8-methyl-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-4-(4-pyridinylacetyl)piperazine N4-oxide; (+,-)-1-(3,10-Dibromo-6,11-dihydro-8-methyl-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-4-(4-pyridinylacetyl)piperazine N4-oxide; (+,-)-1-(3,8-Dibromo-6,11-dihydro-10-methyl-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-4-(4-pyridinylacetyl)piperazine N4-oxide; (+,-)-4-[6,11-Dihydro-3-(1-hydroxy-1-methylethyl)-10-methoxy-8-methyl-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl]-1-(4-pyridinylacetyl)piperidine N1-oxide; (+)-4-(3-Bromo-10-methoxy-8-methyl-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-(4-pyridinylacetyl)piperidine N1-oxide; (-)-4-(3-Bromo-10-methoxy-8-methyl-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-(4-pyridinylacetyl)piperidine N1-oxide; (+,-)-1-(3-Bromo-8-methoxy-10-methyl-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-4-(4-pyridinylacetyl)piperazine N4-oxide; 4-(3-Ethenyl-6,11-dihydro-10-methoxy-8-methyl-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-(4-pyridinylacetyl)piperidine N1-oxide; 4-(3-Ethenyl-6,11-dihydro-10-methoxy-8-methyl-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-(methylsulphonyl)piperidine; 4-(3-Ethyl-6,11-dihydro-10-methoxy-8-methyl-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-(4-pyridinylacetyl)piperidine N1-oxide; (+,-)-4-(3-Bromo-6,11-dihydro-8,10-dimethyl-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-(4-piperidinylacetyl)piperazine; (+,-)-4-(3-Bromo-6,11-dihydro-8,10-dimethyl-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-(4-piperidinylacetyl-N-carboxamido)piperazine; (+,-)-4-(3-Cyclopropyl-6,11-dihydro-10-methoxy-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-(4-pyridinylacetyl)piperidine; (+)-4-(3-Bromo-6,11-dihydro-10-bromo-8-methyl-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-(4-pyridinylacetyl)piperidine N1-oxide; (-)-4-(3-Bromo-6,11-dihydro-10-bromo-8-methyl-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-(4-pyridinylacetyl)piperidine N1-oxide; (+)-4-(3-Bromo-6,11-dihydro-11-hydroxy-10-bromo-8-methyl-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-(4-pyridinylacetyl)piperidine N1-oxide; (-)-4-(3-Bromo-6,11-dihydro-11-hydroxy-10-bromo-8-methyl-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-1-(4-pyridinylacetyl)piperidine N1-oxide; 4-(3-Bromo-5,6-dihydro-10-bromo-8-methyl-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-(4-pyridinylacetyl)piperidine N1-oxide or a pharmaceutically acceptable salt thereof is disclosed. A pharmaceutical composition thereof is useful for inhibiting the abnormal growth of cells in a patient such as inhibiting tumour cells expressing an activated ras oncogene.