Somatostatin analog and uses thereof

Abstract

Claimed is a somatostatin agonist according to formula (I), D-Phe-c(Cys-Tyr(I)-D-Trp-Lys-Val-Cys)-Thr-NH 2 ,  (I) or a pharmaceutically acceptable salt thereof, and uses thereof.

1 . A compound of the formula (I),  
       D-Phe-c(Cys-Tyr(I)-D-Trp-Lys-Val-Cys)-Thr-NH 2 ,  (I)  
     or a pharmaceutically acceptable salt thereof.  
   
   
       2 . A method of binding one or more of human somatostatin subtype receptors -1, -2, -3 and -5, which comprises the step of administering a compound of  claim 1 , or a pharmaceutically acceptable salt thereof, to a recipient in need thereof.  
   
   
       3 . A method of eliciting a somatostatin agonist effect, which comprises the step of administering a compound of  claim 1 , or a pharmaceutically acceptable salt thereof, to a recipient in need thereof.  
   
   
       4 . A method of treating a disease or condition in a human or other animal in need thereof, which comprises administering a compound of  claim 1 , or a pharmaceutically acceptable salt thereof, to said mammal, wherein said disease or condition is selected from the group consisting of Cushings Syndrome, gonadotropinoma, hyperparathyroidism, Paget's disease, VIPoma, nesidioblastosis, hyperinsulinism, gastrinoma, Zollinger-Ellison Syndrome, hypersecretory diarrhea, irritable bowel syndrome, pancreatitis, Crohn's Disease, systemic sclerosis, thyroid cancer, psoriasis, hypotension, panic attacks, sclerodoma, small bowel obstruction, gastroesophageal reflux, duodenogastric reflux, Graves' Disease, polycystic ovary disease, upper gastrointestinal bleeding, pancreatic pseudocysts, pancreatic ascites, leukemia, meningioma, cancer cachexia, acromegaly, restenosis, hepatoma, lung cancer, melanoma, inhibiting the accelerated growth of a solid tumor, decreasing body weight, treating insulin resistance, Syndrome X, prolonging the survival of pancreatic cells, fibrosis, hyperlipidemia, hyperamylinemia, hyperprolactinemia, prolactinomas, diabetic neuropathy, macular degeneration, hypercalcemia of malignancy, postprandial portal hypertension, and complications of portal hypertension.  
   
   
       5 . A method according to  claim 4 , wherein said disease or condition is acromegaly.  
   
   
       6 . A method of treating a disease or condition in a human or other animal in need thereof, which comprises administering a compound of  claim 1 , or a pharmaceutically acceptable salt thereof, to said mammal, wherein said disease or condition is selected from the group consisting of Grave's opthalmopathy, non-functioning pituitary tumors, angiogenesis, inflammation and inflammatory diseases, carcinoid syndrome, carcinoid tumors, retinopathy, and macular degeneration.  
   
   
       7 . A method according to  claim 4 , wherein said hypersecretory diarrhea is related to AIDS, to elevated gastrin-releasing peptide, to intestinal graft vs. host disease, or to chemotherapy.  
   
   
       8 . A method according to  claim 3 , wherein said somatostatin agonist effect comprises supression of growth hormone secretion.  
   
   
       9 . A method according to  claim 3 , wherein said somatostatin agonist effect comprises supression of prolactin secretion.  
   
   
       10 . A method according to  claim 2 , wherein said compound of formula (I) selectively binds to somatostatin subtype receptors -2 and -5.