Patent number: 9260504
Abstract: There is provided a novel series of synthetic analogs of hGH-RH(1-29)NH2 (SEQ ID NO: 1) and hGH-RH(1-30)NH2. Of particular interest are those carrying PhAc, N-Me-Aib, Dca, Ac-Ada, Fer, Ac-Amc, Me-NH-Sub, PhAc-Ada, Ac-Ada-D-Phe, Ac-Ada-Phe, Dca-Ada, Dca-Amc, Nac-Ada, Ada-Ada, or CH3—(CH2)10—CO-Ada, at the N-Terminus and ?-Ala, Amc, Apa, Ada, AE2A, AE4P, ?-Lys(?-NH2), Agm, Lys(Oct) or Ahx, at the C-terminus. These analogs inhibit the release of growth hormone from the pituitary in mammals as well as inhibit the proliferation of human cancers, and inhibit the hyperplastic and benign proliferative disorders of various organs, through a direct effect on the cancerous and non-malignant cells. The stronger inhibitory potencies of the new analogs, as compared to previously described ones, result from replacement of various amino acids.
Type:
Grant
Filed:
February 19, 2014
Date of Patent:
February 16, 2016
Assignees:
University of Miami, The United States of America, Represented by the Department of Veterans Affairs
Inventors:
Andrew V. Schally, Marta Zarandi, Jozsef L. Varga, Ren Zhi Cai
Publication number: 20140206836
Abstract: There is provided a novel series of synthetic analogs of hGH-RH(1-29)NH2 (SEQ ID NO: 1) and hGH-RH(1-30)NH2. Of particular interest are those carrying PhAc, N-Me-Aib, Dca, Ac-Ada, Fer, Ac-Amc, Me-NH-Sub, PhAc-Ada, Ac-Ada-D-Phe, Ac-Ada-Phe, Dca-Ada, Dca-Amc, Nac-Ada, Ada-Ada, or CH3—(CH2)10—CO-Ada, at the N-Terminus and ?-Ala, Amc, Apa, Ada, AE2A, AE4P, ?-Lys(?-NH2), Agm, Lys(Oct) or Ahx, at the C-terminus. These analogs inhibit the release of growth hormone from the pituitary in mammals as well as inhibit the proliferation of human cancers, and inhibit the hyperplastic and benign proliferative disorders of various organs, through a direct effect on the cancerous and non-malignant cells. The stronger inhibitory potencies of the new analogs, as compared to previously described ones, result from replacement of various amino acids.
Type:
Application
Filed:
February 19, 2014
Publication date:
July 24, 2014
Applicants:
U.S.A., represented by the Department of Veterans Affairs, University of Miami
Inventors:
Andrew V. SCHALLY, Marta ZARANDI, Jozsef L. VARGA, Ren Zhi CAI
Patent number: 8691942
Abstract: There is provided a novel series of synthetic analogs of hGH-RH(1-29)NH2 (SEQ ID NO: 1) and hGH-RH(1-30)NH2. Of particular interest are those carrying PhAc, N-Me-Aib, Dca, Ac-Ada, Fer, Ac-Amc, Me-NH-Sub, PhAc-Ada, Ac-Ada-D-Phe, Ac-Ada-Phe, Dca-Ada, Dca-Amc, Nac-Ada, Ada-Ada, or CH3—(CH2)10—CO-Ada, at the N-Terminus and ?-Ala, Amc, Apa, Ada, AE2A, AE4P, ?-Lys(?-NH2), Agm, Lys(Oct) or Ahx, at the C-terminus. These analogs inhibit the release of growth hormone from the pituitary in mammals as well as inhibit the proliferation of human cancers, and inhibit the hyperplastic and benign proliferative disorders of various organs, through a direct effect on the cancerous and non-malignant cells. The stronger inhibitory potencies of the new analogs, as compared to previously described ones, result from replacement of various amino acids.
Type:
Grant
Filed:
September 25, 2010
Date of Patent:
April 8, 2014
Assignees:
University of Miami, U.S.A. Represented by the Dept. of Veterans Affairs
Inventors:
Andrew V. Schally, Marta Zarandi, Jozsef L. Varga, Ren Zhi Cai
Publication number: 20130261055
Abstract: There is provided a novel series of synthetic analogs of hGH-RH(1-29)NH2 (SEQ ID NO: 96) and hGH-RH(1-30)NH2. Of particular interest are those carrying PhAc, N-Me-Aib, Dca, Ac-Ada, Fer, Ac-Amc, Me-NH-Sub, PhAc-Ada, Ac-Ada-D-Phe, Ac-Ada-Phe, Dca-Ada, Dca-Amc, Nac-Ada, Ada-Ada, or CH3—(CH2)10—CO-Ada, at the N-Terminus and ?-Ala, Amc, Apa, Ada, AE2A, AE4P, ?-Lys(?-NH2), Agm, Lys(Oct) or Ahx, at the C-terminus. These analogs inhibit the release of growth hormone from the pituitary in mammals as well as inhibit the proliferation of human cancers, and inhibit the hyperplastic and benign proliferative disorders of various organs, through a direct effect on the cancerous and non-malignant cells. The stronger inhibitory potencies of the new analogs, as compared to previously described ones, result from replacement of various amino acids.
Type:
Application
Filed:
September 25, 2010
Publication date:
October 3, 2013
Inventors:
Andrew V. Schally, Marta Zarandi, Jozsef L. Varga, Ren Zhi Cai