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US 7,119,089 B2Granted
Phenothiazine kinesin inhibitors
AssigneeCytokinetics, Inc.
InventorsJeffrey T. Finer, John C. Chabala
Life of this patent
Estimating the term…
Abstract
Phenothiazine derivatives of formula (I) are disclosed. The compounds are inhibitors of the mitotic kinesin KSP and are useful in the treatment of cellular proliferative diseases, such as cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation.
Claims10
A method of inhibiting KSP kinesin in vitro comprising contacting KSP kinesin with a compound of formula
- wherein
- R1 is hydrogen, halogen or CF3;
- R2 is chosen from hydrogen and lower alkyl;
- R5 is chosen from hydrogen, alkyl, substituted alkyl, alkylaryl, substituted alkylaryl, alkylheteroaryl and substituted alkylheteroaryl;
- or
- R3 and R4 taken together with the intervening atoms form five- to seven-membered heterocycloalkyl ring chosen from imidazoline, piperidine, piperazine, pyrrolidine, pyrazole, pyrrole, tetrazole, and morpholine, said ring optionally substituted with one or more alkyl, aryl, alkoxy, halo, alkylaryl or substituted alkylaryl substituents,
- or a pharmaceutically acceptable salt thereof.
4 more elements
A method of inhibiting KSP kinesin in vitro comprising contacting KSP kinesin with a compound of formula
- wherein
- R1 is hydrogen, halogen or CF3;
- R3 hydrogen;
- R5 is chosen from hydrogen, alkyl, substituted alkyl, alkylaryl, substituted alkylaryl, alkylheteroaryl and substituted alkylheteroaryl;
- and
- R2 and R4 taken together with the intervening atoms form a five- to seven-membered heterocycloalkyl ring chosen from imidazoline, piperidine, piperazine, pyrrolidine. pyrazole, pyrrole, and morpholine, said ring optionally substituted with one or more alkyl, aryl, alkoxy, halo, alkylaryl or substituted alkylaryl substituents,
- or a pharmaceutically acceptable salt thereof.
4 more elements
A method of inhibiting KSP kinesin in vitro comprising contacting KSP kinesin with a compound of formula
- wherein
- R1 is hydrogen, halogen or CF3;
- R4 and R5 are independently chosen from hydrogen, alkyl, substituted alkyl, alkylaryl, substituted alkylaryl, alkylheteroaryl and substituted alkylheteroaryl;
- and
- R2 and R3 taken together with the intervening atoms form a five- to seven-membered heterocycloalkyl ring chosen from imidazoline, piperidine, piperazine, pyrrolidine,morpholine, oxazoline, dioxane, and tetrahydrofuran, said ring optionally substituted with one or more alkyl, aryl, alkoxy, halo, alkylaryl or substituted alkylaryl substituents,
- or a pharmaceutically acceptable salt thereof.
3 more elements
Dependencies are inferred from the claim text.