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Last Updated: April 23, 2024

Claims for Patent: 4,788,178

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Summary for Patent: 4,788,178

Title:	Use of gonadoliberin and gonadoliberin agonists for the treatment of climacteric complaints
Abstract:	The invention relates to the use of gonadoliberin and gonadoliberin agonists for the treatment of climacteric complaints and pathological conditions in which the level of parathyroid hormone is elevated, and to preparations containing this or these compounds(s).
Inventor(s):	Konig; Wolfgang (Hofheim am Taunus, DE)
Assignee:	Hoechst Aktiengesellschaft (Frankfurt, DE)
Application Number:	06/724,331
Patent Claims:	1. A method for the treatment of climacteric complaints and pathological conditions in which the level of parathyroid hormone is too high, comprising administering to a patient in need of treatment of said complaints and conditions, a pharmacologically effective amount of gonadoliberin or a pharmacologically effective amount of a gonadoliberin agonist of formula II: ##STR4## in which (a) Z denotes Gly--NH.sub.2, Y denotes Leu, and X denotes D-Nle, D-Nva, D-Abu, D-Phe, D-Ser, D-Met, D-Pgl, D-Lys, D-Leu, D-Arg, D-Ser(Bu.sup.t), D-Thr(Bu.sup.t), D-Cys(Bu.sup.t), D-Asp, D-Asp(OBu.sup.t), D-Glu(OBu.sup.t), D-Orn(Boc), D-Lys(Boc), D-Trp, D-Tyr, .epsilon.-lauryl-D-Lys or .epsilon.-dextran-D-Lys, D-His(Bzl) or (b) Z denotes Gly--NH.sub.2, NH--(C.sub.1 -C.sub.3)-alkyl or NH-cyclopropyl, which can be substituted by OH or F, Y denotes Leu, Ser(Bu.sup.t), Cys(Bu.sup.t), Glu(OBu.sup.t), Orn(Boc) or Lys (Boc), and X denotes D-Ser(Bu.sup.t), D-Cys(Bu.sup.t), O-Asp(OBu.sup.t), D-Glu(OBu.sup.t), D-Orn(Boc) or D-Lys(Boc), D-His(Bzl) or said, agonist wherein Ser.sup.4 is replaced by Ala or Thr, or wherein Tyr is replaced by Phe, or wherein Arg is replaced by Orn, Lys or homoarginine, or (c) Z denotes --NHCH.sub.3, --NH--CH.sub.2 --CH.sub.3, --NH--CH.sub.2 CH.sub.2 CH.sub.3, ##STR5## Y denotes Leu, and X denotes Gly or (d) Z denotes --NHC.sub.2 H.sub.5, Y denotes Leu, and X denotes D-Trp, D-Leu, D-Ala, D-Ser(Bu.sup.t), D-Tyr, D-Lys or D-His(Bzl) or (e) Z denotes Gly--NH.sub.2 or NH--C.sub.2 H.sub.5, Y denotes N-.alpha.-methyl-Leu, and X denotes Gly or (f) Z denotes NH-cycloporpyl, Y denotes Leu, and X denotes D-Leu or (g) Z denotes Gly--NH.sub.2, NH--(C.sub.1 -C.sub.3)-alkyl or NH-cyclopropyl, Y denotes Ser(Bu.sup.t), Cys(Bu.sup.t), Asp(OBu.sup.t), Glu(OBu.sup.t), Orn(Boc) or Lys(Boc), and X denotes Gly. 2. A method for the treatment of osteoporosis in which the level of parathyroid hormone is too high, comprising administering to a patient in need of treatment for said osteoporosis, a pharmacologically effective amount of gonadoliberin or a pharamacologically effective amount of a gondoliberin agonist of formula II: ##STR6## in which (a) Z denotes Gly--NH.sub.2, Y denotes Leu, and X denotes D-Nle, D-Nva, D-Abu, D-Phe, D-Ser, D-Met, D-Pgl, D-Leu, D-Arg, D-Ser(Bu.sup.t), D-Thr(Bu.sup.t), D-Cys(Bu.sup.t), D-Lys, D-Asp, D-Asp(OBu.sup.t), D-Glu(OBu.sub.t), D-Orn(Boc), D-Lys(Boc), D-Trp, D-Tyr, .epsilon.-lauryl-D-Lys or .epsilon.-dextran-D-Lys, D-His(Bzl) or (b) Z denotes Gly--NH.sub.2, NH--(C.sub.1 -C.sub.3)-alkyl or NH-cyclopropyl, which can be substituted by OH or F, Y denotes Leu, Ser(Bu.sup.t), Cys(Bu.sup.t), Glu(OBu.sup.t), Orn(Boc) or Lys(Boc), and X denotes D-Ser(Bu.sup.t), D-Cys(Bu.sup.t), D-Asp(OBu.sup.t), D-Glu(OBu.sup.t), D-Orn(Boc) or D-Lys(Boc), D-His(Bzl) or said agonist wherein Ser.sup.4 is replaced by Ala or Thr, or wherein Tyr is replaced by Phe, or wherein Arg is replaced by Orn, Lys or homoarginine, or (c) Z denotes --NHCH.sub.3, --NH--CH.sub.2 --CH.sub.3, --NH--CH.sub.2 CH.sub.2 CH.sub.3, ##STR7## Y denotes Leu, and X denotes Gly or (d) Z denotes --NHC.sub.2 H.sub.5, Y denotes Leu, and X denotes D-Trp, D-Ala, D-Ser(Bu.sup.t), D-Tyr, D-Lys or D-His(Bzl) (e) Z denotes Gly--NH.sub.2 or NH--C.sub.2 H.sub.5. Y denotes N-.alpha.-methyl-Leu, and X deontes Gly (f) Z denotes NH-cyclopropyl, Y denotes Leu, and X denotes D-Leu or (g) Z denotes Gly--NH.sub.2, NH--(C.sub.1 -C.sub.3)-alkyl or NH-cyclopropyl, Y denotes Ser(Bu.sup.t), Cys(Bu.sup.t), Asp(OBu.sup.t), Glu(OBu.sup.t), Orn(Boc) or Lys (Boc), and X denotes Gly. 3. A method for the treatment of renal insufficiency in which the level of parathyroid hormone is too high, comprising adminstering to a patient in need of treatment for said renal insufficiency a pharamcologically effective amount of gonadoliberin or a pharamcologically effective amount of a gonadoliberin agonist of formula II: ##STR8## in which (a) Z denotes Gly--NH.sub.2, Y denotes Leu, and X denotes D-Nle, D-Abu, D-Phe, D-Ser, D-Met, D-Pgl, D-Lys, D-Leu, D-Arg, D-Ser(Bu.sup.t), D-Thr(Bu.sup.t), D-Cys(Bu.sup.t), D-Asp, D-Asp(OBu.sup.t), D-Glu(OBu.sup.t), D-Orn(Boc), D-Lys(Boc), D-Trp, D-Tyr, .epsilon.-lauryl-D-Lys or .epsilon.-dextran-D-Lys, D-His(Bzl) or (b) Z denotes Gly--NH.sub.2, NH--(C.sub.1 -C.sub.3)-alkyl or NH-cyclopropyl, which can be substituted by OH or F, Y denotes Leu, Ser(Bu.sup.t), Cys(Bu.sup.t), Glu(OBu.sup.t), Orn(Boc) or Lys(Boc), and X denotes D-Ser(Bu.sup.t), D-Cys(Bu.sup.t), D-Asp(OBu.sup.t), D-Glu(OBu.sup.t), D-Orn(Boc) or D-Lys(Boc), D-His(Bzl) or said agonist wherein Ser.sup.4 is replaced by Ala or Thr, or wherein Tyr is replaced by Phe, or wherein Arg is replaced by Orn, Lys or homoarginine, or (c) Z denotes --NHCH.sub.3, --NH--CH.sub.2 --CH.sub.3, --NH--CH.sub.2 CH.sub.2 CH.sub.3, ##STR9## Y denotes Leu, and X denotes Gly or (d) Z denotes --NHC.sub.2 H.sub.5, Y denotes Leu, and X denotes D-Trp, D-Leu, D-Ala, D-Ser(Bu.sup.t), D-Tyr, D-Lys or D-His(Bzl) or (e) Z denotes Gly--NH.sub.2 or NH--C.sub.2 H.sub.5, Y denotes N-.alpha.-methyl-Leu, and X denotes Gly or (f) Z denotes NH-cyclopropyl, Y denotes Leu, and X denotes D-Leu or (g) Z denotes Gly--NH.sub.2, NH--(C.sub.1 -C.sub.3)-alkyl or NH-cyclopropyl, Y denotes Ser(Bu.sup.t), Cys(Bu.sup.t), Asp(OBu.sup.t), Glu(OBu.sup.t), Orn(Boc) or Lys(Boc), and X denotes Gly. 4. The method of claim 1 wherein said administering comprises parenterally administering 6 to 60 ng/kg of gonadoliberin pre single dose or an equally effective amount of said gonadoliberin agonist of formula II to said patient. 5. The method of claim I wherein said administering comprises administering 0.12 to 2.4 micrograms/kilogram of gonadoliberin pre single dose or an equally effective amount of said gonadoliberin agonist of formula II onto the mucosa of said patient. 6. The method of claim 2 wherein said administering comprises parenterally administering 6 to 60 ng/kg of gonadoliberin per single dose or an equally effective amount of said gondoliberin agonist of formula II to said patient. 7. The method of claim 2 wherein said administering comprises administering 0.12 to 2.4 micrograms/kilogram of gonadoliberin per single dose or an equally effective amount of said gonadoliberin agonist of formula II onto the mucosa of said patient. 8. The method of claim 3 wherein said administering comprises parenterally administering 6 to 60 ng/kg of gonadoliberin per single dose or an equally effective amount of said gonadoliberin agonist of formula II to said patient. 9. The method of claim 3 wherein said administering comprises administering 0.12 to 2.4 micrograms/kilogram of gonadoliberin per single dose or an equally effective amount of said gonadoliberin agonist of formula II onto the mucosa of said patient.

Details for Patent 4,788,178

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Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Nps Pharmaceuticals, Inc.	NATPARA	parathyroid hormone	For Injection	125511	01/23/2015	⤷ Try a Trial	2005-11-29
>Applicant	>Tradename	>Biologic Ingredient	>Dosage Form	>BLA	>Approval Date	>Patent No.	>Expiredate

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