Protein kinase C inhibitor

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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Details

514185, 514410, 540469, A01N 4300, A61K 31555, C07D26722

Patent

active

061178616

ABSTRACT:
This invention provides novel bis-indolylmaleimide macrocycle derivatives of the formula: ##STR1## and solvates thereof. The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.

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patent: 5552396 (1996-09-01), Heath, Jr. et al.
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Inoguchi, et al., Preferential Elevation of Protein Kinase C Isoform bII and Diacylglycerol Levels in the aorta and heart of diabetic rate: Differential reversibility to glycemic controls by islet cell transplantation:, Proc. Natl. Acad. Sci., USA, vol. 89, pp. 11059-11063 (Nov. 1992).
Ishii, et al., Amelioration of Vascular Dysfunctions in Diabetic Rats by an Oral PKC b Inhibitor:, Science, vol. 272, pp. 728-731 (May 3, 1996).
Porte, et al., "Diabetes Complications: Why is Glucose Potentially Toxic?", Science, vol. 272, pp. 699-700 (May 3, 1996).
Kowluru, et al., "Diabetes-Induced Disorders of Retinal Protein Kinase C and Na, K-ATPase are Inhibited by LY333531", Abstract, American Diabetes Association Meeting, Jun. 8-11, 1996.
Ishii, et al., "Treatment with Protein Kinase C b Isoform Inhibitor Normalized Urinary Albumin Excretion and Glomerular Filtration Rate in Diabetic Rats", Abstract, American Diabetes Association Meeting, Jun. 8-11, 1996.
Lee, et al., "Activation of Protein Kinase C by elevation of glucose concentration: Proposal for a mechanism in the development of diabetic vascular complications", Proc. Natl. Acad. Sci. USA, vol. 86, pp. 5141-5145 (1989).
Murray, et al., "Protein Kinases and Phosphates: Structural Biology and Synthetic Inhibitors", Annual Reports in Medicinal Chemistry, San Diego: Academic Press, 1994, vol. 29, Chapter 26, pp. 255-264.

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