# US 7,608,643 B2 · Compounds for inhibiting KSP kinesin activity

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- Number: US 7,608,643 B2
- Document ID: US7608643B2
- Status: Granted
- Kind: B2
- Application number: 11/370,005
- Filed: 2006-03-07
- Published: 2006-11-16
- Granted: 2009-10-27
- Earliest claimed: 2005-03-09
- Assignees: Schering Corporation
- Inventors: Ronald J. Doll; Ronald Herbst; Wolfgang Seghezzi; Emma M. Lees; William F. Estacio
- Web page: https://patentgrep.com/patent/US7608643B2

## CPC

- A61K 31/4743: condensed with ring systems having sulfur as a ring hetero atom
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

The present invention relates to compounds of Formula I or pharmaceutically acceptable salts or solvates thereof: The present invention provides compositions comprising these compounds that are useful for treating cellular proliferative diseases or disorders associated with KSP kinesin activity and for inhibiting KSP kinesin activity.

## Claims

### Claim 1

A pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I or a pharmaceutically acceptable salt thereof, in combination with a pharmaceutically acceptable carrier, adjuvant or vehicle:

### Claim 2 (depends on 1)

The composition of claim 1, wherein the compound is the (+)-enantiomer of
or a pharmaceutically acceptable salt thereof.

### Claim 3 (depends on 1)

The composition of claim 1, wherein the compound is the (−)-enantiomer of
or a pharmaceutically acceptable salt thereof.

### Claim 4 (depends on 1)

The pharmaceutical composition of claim 1, further comprising one or more compounds selected from the group consisting of an anti-cancer agent, a PPAR-γ agonist, a PPAR-δ agonist, an inhibitor of inherent multidrug resistance, an anti-emetic agent, and an immunologic-enhancing drug.

### Claim 5 (depends on 4)

The pharmaceutical composition of claim 4, wherein the anti-cancer agent is selected from the group consisting of an estrogen receptor modulator, an androgen receptor modulator, retinoid receptor modulator, a cytotoxic/cytostatic agent, an antiproliferative agent, a prenyl-protein transferase inhibitor, an HMG-CoA reductase inhibitor, an angiogenesis inhibitor, an inhibitor of cell proliferation and survival signaling, an agent that interferes with a cell cycle checkpoint, and an apoptosis inducing agent.

### Claim 6 (depends on 4)

The pharmaceutical composition of claim 4, further comprising one or more anti-cancer agents selected from the group consisting of cytostatic agents, cytotoxic agents, taxanes, topoisomerase II inhibitors, topoisomerase I inhibitors, tubulin interacting agents, hormonal agents, thymidilate synthase inhibitors, anti-metabolites, alkylating agents, farnesyl protein transferase inhibitors, signal transduction inhibitors, EGER kinase inhibitors, antibodies to EGER, C-abl kinase inhibitors, hormonal therapy combinations, and aromatase combinations.

### Claim 7 (depends on 4)

The pharmaceutical composition of claim 4, further comprising one or more agents selected from the group consisting of Uracil mustard, Chlormethine, Ifosfamide, Melphalan, Chlorambucil, Pipobroman, Triethylenemelamine, Triethylenethiophosphoramine, Busulfan, Carmustine, Lomustine, Streptozocin, Dacarbazine, Floxuridine, Cytarabine, 6-Mercaptopurine, 6-Thioguanine, Fludarabine phosphate, oxaliplatin, leucovirin, oxaliplatin, Pentostatine, Vinblastine, Vincristine, Vindesine, Bleomycin, Dactinomycin, Daunorubicin, Doxorubicin, Epirubicin, Idarubicin, Mithramycin, Deoxycoformycin, Mitomycin-C, L-Asparaginase, Teniposide 17α-Ethinylestradiol, Diethylstilbestrol, Testosterone, Prednisone, Fluoxymesterone, Dromostanolone propionate, Testolactone, Megestrolacetate, Methyipred nisolone, Methyltestosterone, Prednisolone, Triamcinolone, Chlorotrianisene, Hydroxyprogesterone, Aminoglutethimide, Estramustine, Medroxyprogesteroneacetate, Leuprolide, Flutamide, Toremifene, goserelin, Cisplatin, Carboplatin, Hydroxyurea, Amsacrine, Procarbazine, Mitotane, Mitoxantrone, Levamisole, Navelbene, Anastrazole, Letrazole, Capecitabine, Reloxafine, Droloxafine, Hexamethyl melamine, doxorubicin, cyclophosphamide, gemcitabine, interferons, pegylated interferons, Erbitux and mixtures thereof.