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1. WO2009042565 - INHIBITORS OF EPPIN/SEMENOGELIN BINDING AS MALE CONTRACEPTIVES

Publication Number WO/2009/042565
Publication Date 02.04.2009
International Application No. PCT/US2008/077312
International Filing Date 23.09.2008
IPC
A61K 31/567 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
56Compounds containing cyclopentahydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
565not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
567substituted in position 17 alpha, e.g. mestranol, norethandrolone
A61K 38/16 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
C07K 14/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
CPC
A61K 31/567
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives, e.g. steroids
565not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
567substituted in position 17 alpha, e.g. mestranol, norethandrolone
A61P 15/16
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15Drugs for genital or sexual disorders
16Masculine contraceptives
Applicants
  • THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL [US]/[US] (AllExceptUS)
  • O'RAND, Michael G. [US]/[US] (UsOnly)
  • WIDGREN, Esther Elaine [US]/[US] (UsOnly)
  • RICHARDSON, Richard [US]/[US] (UsOnly)
  • TEMPLE, Brenda [US]/[US] (UsOnly)
Inventors
  • O'RAND, Michael G.
  • WIDGREN, Esther Elaine
  • RICHARDSON, Richard
  • TEMPLE, Brenda
Agents
  • FIX, Amy H.
Priority Data
60/995,29326.09.2007US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) INHIBITORS OF EPPIN/SEMENOGELIN BINDING AS MALE CONTRACEPTIVES
(FR) INHIBITEURS DE LA LIAISON EPPINE-SÉMÉNOGÉLINE EN TANT QUE CONTRACEPTIFS MASCULINS
Abstract
(EN)
Compounds suitable for use in providing male contraception, an assay method for identifying such compounds, and methods of providing contraception using the compounds, are provided. The compounds described herein inhibit Eppin-semenogelin binding, and inhibit forward motility of sperm in humans and other primates. The assays identify compounds which both inhibit eppin-semenogelin binding and inhibit sperm motility, and can be carried out in a high throughput manner, using labeled recombinant Eppin and semenogelin. The compounds can be used in oral or transdermal compositions to temporarily and reversibly inhibit male fertility. They can also be used in addition to, or in place of, spermicides in spermicidal compositions, such as those used in conjunction with condoms, diaphragms, and spermicidal jellies.
(FR)
L'invention concerne des composés appropriés à utiliser dans la contraception masculine, un procédé de test d'identification de ces composés et des procédés assurant une contraception en utilisant les composés. Les composés décrits ici inhibent la liaison eppine-séménogéline et inhibent la motilité des spermatozoïdes chez l'être humain et autres primates. Les tests identifient les composés qui inhibent à la fois la liaison eppine-séménogéline et la motilité des spermatozoïdes, et peuvent être réalisés de façon à donner un rendement élevé en utilisant l'eppine et la séménogéline recombinantes marquées. Les composés peuvent être utilisés dans des compositions orales ou transdermiques pour inhiber temporairement et de façon réversible, la fertilité masculine. Ils peuvent également être utilisés en plus ou à la place de spermicides dans des compositions spermicides telles que celles utilisées en association avec les préservatifs, diaphragmes et gels spermicides.
Also published as
Latest bibliographic data on file with the International Bureau