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United States patent granted to Cyclacel for cyclin dependent kinase inhibitor series.

Cyclacel Group plc (Dundee, Scotland), the cell cycle-based biopharmaceutical company, announced that it received a United States Patent (6,531,479) covering a novel series of pyrimidine small molecules shown to control the progress of cells through the cancer cell cycle. One group of these novel compounds works by inhibiting Cyclin Dependent Kinases (CDK), drug targets that control cancer cell division. Further groups of compounds within the series work by inhibiting alternative CDK target profiles and other cell cycle kinases. The patented compounds may be useful as therapeutics for proliferative diseases such as cancer, inflammatory and autoimmune diseases, in which cells divide out of control, and certain viral infections.

Cell cycle inhibitors are an area of growing interest to the pharmaceutical industry because of the importance of CDK and cyclin drug targets in cancer biology. Cyclacel is a world leader in this field. Seliciclib, its lead CDK inhibitor drug, is currently the only orally available CDK inhibitor in Phase II clinical trials. Seliciclib is a patented purine molecule as opposed to the recently patented agents which were designed on a pyrimidine chemical scaffold. Lead compounds from the new series demonstrated highly potent inhibition of CDK activity, with many at the subnanomolar level. Several pyrimidine drugs have passed the proof of concept stage as they have been shown to be active in in vivo models when taken by mouth and are progressing into preclinical development.

Dr. Robert Jackson, Chief Scientific Officer, said, "This patent validates the talent of our scientists who invented another novel drug series with multiple mechanisms of action. We used state-of-the-art technology based on target protein structures to design compounds that hit a variety of cell cycle targets resulting in multiple product opportunities. We have achieved significant improvements in activity over previous generations and many of the new compounds have drug-like physicochemical properties. Our objective is to progress one or more of these molecules into clinical trials as soon as possible."

Cyclacel is a biopharmaceutical company dedicated to the discovery, development and commercialization of novel, mechanism-targeted drugs to treat human cancers and other serious disorders. The company is currently evaluating seliciclib (CYC202), an orally-available Cyclin Dependent Kinase inhibitor, in Phase II clinical trials for the treatment of non-small cell lung cancer and B-cell hematological malignancies. CYC682 is an orally- available, cell cycle modulating nucleoside analog in Phase I clinical trials for the treatment of cancer. Cyclacel has eight additional programs at preclinical stages.

United States Patent 6,531,479 relates to 2-substituted 4-heteroaryl-pyrimidines, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders such as cancer, leukemia, psoriasis and the like.

Cancer is the second leading cause of death in the Western World. Solid tumors in particular represent a major public health issue with an incidence of over 2 million people. Breast, colorectal, lung, prostate cancer and leukemia are the most common cancers. Survival rates tend to be poor in many cancers and demographic changes and graying populations suggest that new cases of cancer are on the rise. Increased understanding of the molecular and genetic mechanism causing cancer have raised expectations that mechanism- targeted drugs may complement existing chemotherapies with the objective of increasing effectiveness and decreasing toxic side effects of modern cancer therapeutics.

Cyclin Dependent Kinase (CDK) Inhibitors are a novel class of drugs that act on the same CDK enzyme targets as the body's own cancer stopping genes. Tumor suppressor genes, such as p53 and p21, stop cancer cells at cell cycle checkpoints and cause them to commit suicide. The goal of cancer treatment with CDK inhibitors is to emulate tumor suppressor gene behavior and cause cancer cells to die. The discovery of CDKs and cyclins and their role in checkpoint control of the cancer cell cycle has been honored with the 2001 Nobel Prize for Medicine and Physiology.

Seliciclib (CYC202 or r-roscovitine) is novel cell cycle drug belonging to the Cyclin Dependent Kinase (CDK) inhibitor class. CDK inhibition is an important new approach in the quest for drugs that target the same molecular mechanisms as the body's own cancer stopping genes. By acting on different combinations of Cyclin Dependent Kinases it is possible to stop normal cells growing or to cause cancer cells to commit suicide, otherwise known as apoptosis. Recent publications have implied that seliciclib has activity in a wide variety of disease models including HIV and inflammatory diseases such as glomerulonephritis. Seliciclib has been tested in Phase I clinical trials in both cancer patients and healthy volunteers and is currently in Phase II clinical trials in patients with non small cell lung cancer or haematological (blood) cancers.

Robert Jackson, Ph.D., Chief Scientific Officer, 61, joined January 2001. He was previously Director of Research and Development and a member of the Board of Directors at Celltech Group plc. He was also the Executive Director of Research and Development, the Chief Operating Officer and a member of the Board of Directors at Chiroscience Group plc, which was acquired by Celltech in 1999. Before these appointments, he was Vice President of Research and Development at Agouron Pharmaceuticals, Inc., and headed cancer research at DuPont Pharmaceuticals and Warner-Lambert Company. He holds a B.A. from the University of Cambridge and a Ph.D. from the University of London, Institute of Cancer Research.

Cyclacel Group plc

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Title Annotation:Cell cycle inhibitors; Seliciclib (CYC202 or r-roscovitine)
Comment:United States patent granted to Cyclacel for cyclin dependent kinase inhibitor series.(Cell cycle inhibitors )(Seliciclib (CYC202 or r-roscovitine))
Publication:BIOTECH Patent News
Geographic Code:4EUUK
Date:Feb 1, 2005
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