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1. WO2012129673 - INHIBITORS OF 17ß-HSD1, 17ß-HSD3 AND 17ß-HSD10

Publication Number WO/2012/129673
Publication Date 04.10.2012
International Application No. PCT/CA2012/000316
International Filing Date 26.03.2012
IPC
C07J 1/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
JSTEROIDS
1Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 17 beta by a carbon atom, e.g. oestrane, androstane
A61K 31/565 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
A61K 31/566 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
566having an oxo group in position 17, e.g. oestrone
A61K 31/58 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
58containing heterocyclic rings, e.g. aldosterone, danazol, stanozolol, pancuronium, digitogenin
A61K 31/675 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
66Phosphorus compounds
675having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61K 31/69 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
69Boron compounds
CPC
A61K 31/566
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
566having an oxo group in position 17, e.g. estrone
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
A61K 31/5685
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
568substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
5685having an oxo group in position 17, e.g. androsterone
A61K 31/58
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
58containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A61K 31/675
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
66Phosphorus compounds
675having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61K 31/69
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
69Boron compounds
Applicants
  • UNIVERSITE LAVAL [CA]/[CA] (AllExceptUS)
  • POIRIER, Donald [CA]/[CA] (UsOnly)
  • MALTAIS, René [CA]/[CA] (UsOnly)
  • ROY, Jenny [CA]/[CA] (UsOnly)
Inventors
  • POIRIER, Donald
  • MALTAIS, René
  • ROY, Jenny
Agents
  • BERESKIN & PARR LLP/S.E.N.C.R.L., S.R.L.
Priority Data
61/467,76425.03.2011US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) INHIBITORS OF 17ß-HSD1, 17ß-HSD3 AND 17ß-HSD10
(FR) INHIBITEURS DE 17SS-HSD1, 17SS-HSD3 ET 17SS-HSD10
Abstract
(EN)
The present application discloses 17β hydroxy steroid dehydrogenase (17β HSD) type 1, 3, 10 inhibitors and use thereof (alone and in combination) in the treatment of cancer and other afflictions. 17β HSDl inhibitors include estradiol derivatives with a nieta-carbamoylbenzyl substituent at C 16. 17β HSD3/HSD10 inhibitors include androsterone derivatives substituted at the C3 position with a sulfonamide piperazine. Also disclosed are compounds that are inhibitors of both 17β HSDl and 17β HSD3 that have a spiro-morpholine substituent at C20.
(FR)
La présente invention concerne des inhibiteurs de la 17β hydroxy stéroïde déshydrogénase (17β HSD) de type 1, 3, 10 et leur utilisation (individuellement ou en combinaison) dans le traitement du cancer et d'autres afflictions. Les inhibiteurs de 17β HSD1 comprennent des dérivés d'œstradiol ayant un substituant niéta-carbamoylbenzyle en C 16. Les inhibiteurs de 17β HSD3/HSD10 comprennent des dérivés d'androstérone substitués à la position C3 par une sulfonamide pipérazine. L'invention concerne également des composés qui sont des inhibiteurs à la fois de 17β HSD1 et 17β HSD3 qui possèdent un substituant spiro-morpholine en C 20.
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