47 results about "Gonadotropin-releasing hormone receptor" patented technology

The present invention relates to Gonadotropin Releasing Hormone (GnRH, also known as Luteinizing Hormone Releasing Hormone) receptor antagonists.

The invention belongs to the pharmacological field of gene engineering, and provides a group of protein derivatives of human granzyme B by adopting gene engineering technology. The group of protein derivatives of the human granzyme B comprises GrB-G4S-GnRH (GrBLG) and mGrB-C4S-GnRH (mGrBLG) which are targeted fusion proteins formed by connecting human matured granzyme B (GrB) and mutagenic human matured granzyme B (mGrB) with human gonadotropin-releasing hormone (GnRH) through flexible connecting short peptide GlyGlyGlyGlySer (G4S) respectively and which can be combined with human GnRH receptors (GnRHR) on the surfaces of cells through ligand human GnRH. The mGrB eliminates the functions of the combination through a personal 'electrostatic exchange-absorption mode' and the entering into target cells of the prior GrB, and simultaneously reserves the enzymatic activity and the cytocidal function of the GrB. The invention provides experimental evidences for peculiarly targeted-killing GnRHR positive cells and minimizing toxic side effect by the fusion proteins, and shows the use of the group of protein derivatives of the human granzyme B in the targeted therapy on the positive adenocarcinoma of a type of gonadotropin-releasing hormone receptors.

GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure:wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, R7 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure, wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure:wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, R7 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

Spiroindoline derivatives, processes for their preparation and pharmaceutical compositions thereof, their use for the treatment of diseases, and their use for the manufacture of medicaments for the treatment of diseases, especially sex-hormone-related diseases in both men and women, in particularly those selected from the group of endometriosis, uterine leiomyoma (fibroids), polycystic ovarian disease, menorrhagia, dysmenorrhea, hirsutism, precocious puberty, gonadal steroid-dependent neoplasia such as cancers of the prostate, breast and ovary, gonadotrope pituitary adenomas, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hypertrophy, contraception, infertility and assisted reproductive therapy such as in vitro fertilization. The present application relates in particular to spiroindoline derivatives as gonadotropin-releasing hormone (GnRH) receptor antagonists.