Protein kinase C inhibitor

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

Patent

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

540469, 514185, A61K 31395, C07D41900

Patent

active

057101450

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.

REFERENCES:
patent: 5057614 (1991-10-01), Davis et al.
patent: 5292747 (1994-03-01), Davis et al.
patent: 5552396 (1996-09-01), Heath, Jr. et al.
DeFronzo, R.A., "Diabetic Nephropathy: Etiologic and Therapeutic Considerations", Diabetes Reviews, vol. 3, No. 3, 510-564, 1995.
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 control by islet cell transplantation:", Proc. Natl. Acad. Sci. USA, vol. 89, 11059-11063, Nov. 1992.
Ishii, et al., "Amelioration of Vascular Dysfunctions in Diabetic Rats by an Oral PKC b Inhibitor:", Science, vol. 272, 728-731, 3 May 1996.
Porte, et al., "Diabetes Complications: Why is Glucose Potentially Toxic?", Science, vol. 272, 699-700, 3 May 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, 86: 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.

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Protein kinase C inhibitor does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Protein kinase C inhibitor, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Protein kinase C inhibitor will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-725485

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.