EP0000764B1 - Agent anticonceptionnel contenant une peptide - Google Patents

Agent anticonceptionnel contenant une peptide Download PDF

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Publication number
EP0000764B1
EP0000764B1 EP78100564A EP78100564A EP0000764B1 EP 0000764 B1 EP0000764 B1 EP 0000764B1 EP 78100564 A EP78100564 A EP 78100564A EP 78100564 A EP78100564 A EP 78100564A EP 0000764 B1 EP0000764 B1 EP 0000764B1
Authority
EP
European Patent Office
Prior art keywords
peptide
compound
anticonceptive
mcg
agent containing
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired
Application number
EP78100564A
Other languages
German (de)
English (en)
Other versions
EP0000764A1 (fr
Inventor
Marianne Dr. Von Der Ohe
Jürgen Kurt Dr. Sandow
Wolfrad Dr. Von Rechenberg
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Hoechst AG
Original Assignee
Hoechst AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoechst AG filed Critical Hoechst AG
Priority to DE8181103936T priority Critical patent/DE2862466D1/de
Publication of EP0000764A1 publication Critical patent/EP0000764A1/fr
Application granted granted Critical
Publication of EP0000764B1 publication Critical patent/EP0000764B1/fr
Expired legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08—Peptides having 5 to 11 amino acids
    • A61K38/09—Luteinising hormone-releasing hormone [LHRH], i.e. Gonadotropin-releasing hormone [GnRH]; Related peptides
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S930/00—Peptide or protein sequence
    • Y10S930/01—Peptide or protein sequence
    • Y10S930/13—Luteinizing hormone-releasing hormone; related peptides

Definitions

  • the invention relates to an anti-conception agent based on a peptide of the general formula in which X stands for D-serine tert-butyl ether.
  • the compound of formula I is prepared according to DOS 2 438 350. After a single dose in doses of 1.4-20 mcg (this corresponds to 20-300 ng / kg) intravenously (iv) 50-1000 mcg (this corresponds to 100-5000 ng / kg) intranasally (in) in test subjects the release of gonadotropins from the anterior pituitary lobe.
  • the dosage is z. B. 3 x 5 mcg daily. c., i. v. or I. m., but can be safely increased to a multiple, since the peptide is non-toxic. In practice one moves between 5-500 mcg daily. With intranasal use, this dose has to be increased by about 100 times because of the absorption of only approx. 1%.
  • the agent according to the invention can be used in men to temporarily suppress testosterone production and thus spermatogenesis, and in women to suppress ovulation.
  • the application for women begins. e.g. B. on the first day of the cycle and is continued for at least 14 days. In this way, ovulation is definitely prevented during the treatment period.
  • the LH level drops to basal values and stimulation of the pituitary gland is no longer possible. With short-term treatment, it is suppressed. The latter may also apply to the nidation, since both processes depend on the level of the FSH and LH levels.
  • the z. B. with steroid-containing contraceptives to be considered residue and metabolism problems.
  • the preparations according to the invention contain peptides that are easily broken down into amino acids in the body and excreted or metabolized via these amino acids in a physiological manner.
  • Compound of formula can be used e.g. B. in physiological saline intravenously, intramuscularly or subcutaneously.
  • aqueous or oily preparations for intranasal application are particularly suitable for long-term treatment.
  • rectal or vaginal use is also possible.
  • Testosterone levels were measured by radioimmunoassay. There was a reduction in the plasma testosterone level to approximately Y, the initial value. Testosterone levels were measured again 6 weeks after stopping treatment. They were back to normal.
  • Ovulation was postponed with short-term treatment, but was completely suppressed with longer treatment.
  • testicular atropy occurred in the course of treatment, but testicular size increased significantly 8 weeks after treatment was discontinued and the animals showed normal sex drive.
  • 500 mg of compound I are dissolved in 100 liters of physiological saline. It is filtered sterile and filled into ampoules of 1 ml each. This preparation can be used for intravenous, intramuscular or subcutaneous administration of the compound I.
  • 600 mg of compound I are dissolved in 100 I of isotonic aqueous mannitol solution and treated as in Example 1.
  • the ampouled solution is freeze-dried for use again in 1 ml of dist. Water dissolved.
  • 1 ml of solution is e.g. B. filled into a container that is provided with a dispensing metering valve that releases 0.05 ml of the solution per application.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Immunology (AREA)
  • Medicinal Chemistry (AREA)
  • Reproductive Health (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (1)

  1. Agent anticonceptionnel contenant un peptide - de formule 1
    Figure imgb0004
    dans laquelle X désigne l'éthertert-butylique de la D-sérine, pour l'administration intraveineuse, sous-cutanée, intramusculaire ou intranasale, caractérisé en ce qu'il est mis sous forme de doses pour au moins 4 jours, chaque dose quotidienne représentant plus de 2,5 mcg pour l'administration intraveineuse, sous-cutanée ou intramusculaire, ou plus de 100 mcg pour l'administration intranasale.
EP78100564A 1977-08-06 1978-08-01 Agent anticonceptionnel contenant une peptide Expired EP0000764B1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
DE8181103936T DE2862466D1 (en) 1977-08-06 1978-08-01 Use of a luteinising peptide as anti-contraceptive

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE2735515 1977-08-06
DE19772735515 DE2735515A1 (de) 1977-08-06 1977-08-06 Verwendung von lh-rh-peptiden als antikonzeptive

Related Child Applications (1)

Application Number Title Priority Date Filing Date
EP81103936.1 Division-Into 1981-05-22

Publications (2)

Publication Number Publication Date
EP0000764A1 EP0000764A1 (fr) 1979-02-21
EP0000764B1 true EP0000764B1 (fr) 1982-05-05

Family

ID=6015797

Family Applications (2)

Application Number Title Priority Date Filing Date
EP81103936A Expired EP0037127B1 (fr) 1977-08-06 1978-08-01 Utilisation d'un peptide lutéinisant en tant qu'agent anticonceptionnel
EP78100564A Expired EP0000764B1 (fr) 1977-08-06 1978-08-01 Agent anticonceptionnel contenant une peptide

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EP81103936A Expired EP0037127B1 (fr) 1977-08-06 1978-08-01 Utilisation d'un peptide lutéinisant en tant qu'agent anticonceptionnel

Country Status (5)

Country Link
US (1) US4263282A (fr)
EP (2) EP0037127B1 (fr)
JP (1) JPS5428831A (fr)
DE (3) DE2735515A1 (fr)
IT (1) IT1097629B (fr)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4652443A (en) * 1983-06-07 1987-03-24 Japan Atomic Energy Research Institute Slow-release composite and process for producing the same
DE3414595A1 (de) * 1984-04-18 1985-10-31 Hoechst Ag, 6230 Frankfurt Verwendung von gonadoliberin und gonadoliberinagonisten zur behandlung klimakterischer beschwerden
DE3581428D1 (de) * 1984-06-13 1991-02-28 Roehm Gmbh Verfahren zum ueberziehen von arzneiformen.
US4762717A (en) * 1986-03-21 1988-08-09 The General Hospital Corporation Continuous delivery of luteinizing hormone releasing hormone compositions in combination with sex steroid delivery for use as a contraceptive
JPS6311675A (ja) * 1986-07-03 1988-01-19 Nippon Mining Co Ltd アルミナ基板への無電解めつき方法
US4975420A (en) * 1987-09-30 1990-12-04 University Of Saskatchewan Agents and procedures for provoking an immune response to GnRH and immuno sterilizing mammals
CA2029018A1 (fr) * 1989-11-01 1991-05-02 Robert P. Millar Analogues de l'hormone liberant de la gonadotrophine
US5433219A (en) * 1992-09-23 1995-07-18 Spery; Nanette S. Receptive condom assembly

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CS180644B2 (en) * 1973-09-29 1978-01-31 Takeda Chemical Industries Ltd Process for preparing nonapeptides
US3914412A (en) * 1973-10-11 1975-10-21 Abbott Lab {8 Des{13 Gly{9 {0 10 -Gn{13 RH nonapeptide amide analogs in position 6 having ovulation-inducing activity
DE2438350C3 (de) * 1974-08-09 1979-06-13 Hoechst Ag, 6000 Frankfurt Peptide mit starker LH-RH/FSH-RH-Wirkung, Verfahren zu ihrer Herstellung und diese enthaltende pharmazeutische Zubereitungen
US3928307A (en) * 1974-11-04 1975-12-23 American Home Prod P-Glu-D-Phe-Trp-Ser-Tyr-D-Phee-Leu-Arg-Pro-Gly-NH2 and intermediates
US4010261A (en) * 1974-11-25 1977-03-01 Abbott Laboratories Method to prevent reproduction with [Des-Gly]10 -GN-RH nonadeptide amide analogs in position
US4010256A (en) * 1975-07-30 1977-03-01 Professional Staff Association Of The Los Angeles County Harbor General Hospital Male contraceptive and method of achieving male contraception
US4034082A (en) * 1976-03-01 1977-07-05 Abbott Laboratories Method to prevent reproduction in warm-blooded female animals with nonapeptides
DE2617646C2 (de) * 1976-04-22 1986-07-31 Hoechst Ag, 6230 Frankfurt Nonapeptid-amide und Decapeptid-amide mit Gonadoliberin-Wirkung, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende pharmazeutische Präparate

Also Published As

Publication number Publication date
EP0000764A1 (fr) 1979-02-21
EP0037127B1 (fr) 1985-05-22
US4263282A (en) 1981-04-21
DE2735515A1 (de) 1979-02-22
IT7826535A0 (it) 1978-08-04
JPS5428831A (en) 1979-03-03
IT1097629B (it) 1985-08-31
EP0037127A1 (fr) 1981-10-07
JPH0130808B2 (fr) 1989-06-22
DE2861783D1 (en) 1982-06-24
DE2862466D1 (en) 1985-06-27

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