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Claims for Patent: 6,833,384

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Claims for Patent: 6,833,384

Title: Deacetylase inhibitors
Abstract:The present invention provides hydroxamate compounds which are deacetylase inhibitors. The compounds are suitable for pharmaceutical compositions having anti-proliferative properties.
Inventor(s): Remiszewski; Stacy William (Washington Township, NJ), Bair; Kenneth Walter (Mountain Lakes, NJ), Versace; Richard William (Wanaque, NJ), Perez; Lawrence Blas (Hackettstown, NJ), Green; Michael Alan (Easton, PA), Sambucetti; Lidia Cristina (Pacifica, CA), Sharma; Sushil (West Orange, NJ)
Assignee: Novartis AG (Basel, CH)
Application Number:10/299,518
Patent Claims: 1. A compound selected from N-hydroxy-3-[4-[[[2-(2-methyl-1H-indol-3-yl)-ethyl]-amino]methyl]phenyl]-2 E-2-propenamide, or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition, which comprises a therapeutically effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier.

3. A method of treating a proliferative disorder in a mammal which comprises administering to said mammal a therapeutically effective amount of a compound of claim 1 wherein the proliferative disorder is selected from breast cancer, genitourinary cancer, lung cancer, gastrointestinal cancer, epidermoid cancer, melanoma, ovarian cancer, pancreas cancer, neuroblastoma, head and/or neck cancer or bladder cancer; renal, brain or gastric cancer; epidermoid head and/or neck tumor or a mouth tumor; a lung tumor, for example a small cell or non-small cell lung tumor; a gastrointestinal tumor, a colorectal tumor; a genitourinary tumor, a prostate tumor; a hormone-refractory prostate tumor; a proliferative disease that is refractory to the treatment with other chemotherapeutics; a tumor that is refractory to treatment with other chemotherapeutics due to multidrug resistance; hyperproliferative conditions such as leukemias, hyperplasias, fibrosis, pulmonary fibrosis, renal fibrosis, angiogenesis, psoriasis, atherosclerosis and smooth muscle proliferation in the blood vessels, stenosis or restenosis following angioplasty.

4. A compound selected from N-hydroxy-3-[4-[[[2-(1H-indol-3-yl)ethyl]-amino]methyl]phenyl]-2E-2-propen amide, or a pharmaceutically acceptable salt thereof.

5. A pharmaceutical composition which comprises a therapeutically effective amount of a compound of claim 4 and a pharmaceutically acceptable carrier.

6. A method of treating a proliferative disorder in a mammal which comprises administering to said mammal a therapeutically effective amount of a compound of claim 4 wherein the proliferative disorder is selected from breast cancer, genitourinary cancer, lung cancer, gastrointestinal cancer, epidermoid cancer, melanoma, ovarian cancer, pancreas cancer, neuroblastoma, head and/or neck cancer or bladder cancer; renal, brain or gastric cancer; epidermoid head and/or neck tumor or a mouth tumor; a lung tumor, for example a small cell or non-small cell lung tumor; a gastrointestinal tumor, a colorectal tumor; a genitourinary tumor, a prostate tumor; a hormone-refractory prostate tumor; a proliferative disease that is refractory to the treatment with other chemotherapeutics; a tumor that is refractory to treatment with other chemotherapeutics due to multidrug resistance; hyperproliferative conditions such as leukemias, hyperplasias, fibrosis, pulmonary fibrosis, renal fibrosis, angiogenesis, psoriasis, atherosclerosis and smooth muscle proliferation in the blood vessels, stenosis or restenosis following angioplasty.

7. A method of treating a proliferative disorder in a mammal according to claim 3 wherein the proliferative disorder is selected from lung cancer or tumors, non-small cell lung cancer or tumors, colon cancer or tumors, or fibroblasts.

8. A method of treating a proliferative disorder in a mammal according to claim 6 wherein the proliferative disorder is selected from lung cancer or tumors, non-small cell lung cancer or tumors, colon cancer or tumors, or fibroblasts.
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