EP2125858A2 - Sels pharmaceutiquement acceptables de dérivés de 11-(4-aminophenyl)-19-norpregna-4,9(10)-diène-3, 20-dione - Google Patents

Sels pharmaceutiquement acceptables de dérivés de 11-(4-aminophenyl)-19-norpregna-4,9(10)-diène-3, 20-dione

Info

Publication number
EP2125858A2
EP2125858A2 EP08713475A EP08713475A EP2125858A2 EP 2125858 A2 EP2125858 A2 EP 2125858A2 EP 08713475 A EP08713475 A EP 08713475A EP 08713475 A EP08713475 A EP 08713475A EP 2125858 A2 EP2125858 A2 EP 2125858A2
Authority
EP
European Patent Office
Prior art keywords
composition
patient
alkyl
administering
effective amount
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.)
Withdrawn
Application number
EP08713475A
Other languages
German (de)
English (en)
Inventor
Joseph Podolski
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.)
Repros Therapeutics Inc
Original Assignee
Repros Therapeutics Inc
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 Repros Therapeutics Inc filed Critical Repros Therapeutics Inc
Publication of EP2125858A2 publication Critical patent/EP2125858A2/fr
Withdrawn legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C225/00—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones
    • C07C225/22—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/136—Amines having aromatic rings, e.g. ketamine, nortriptyline having the amino group directly attached to the aromatic ring, e.g. benzeneamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/04—Drugs for genital or sexual disorders; Contraceptives for inducing labour or abortion; Uterotonics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18—Feminine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/36—Antigestagens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C221/00—Preparation of compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0077—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom
    • C07J41/0083—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom substituted in position 11-beta by an optionally substituted phenyl group not further condensed with other rings

Definitions

  • the present invention relates generally to compositions comprising steroids and, in particular, to compositions with potent antiprogestational activity, minimal antiglucocorticoid activity and improved stability, comprising a 19-norprogesterone I
  • the present invention provides new formulations with potent antiprogestational activity, minimal antiglucocorticoid activity and improved stability. [0006] More particularly, the present invention provides compositions comprising a pharmaceutically acceptable salt of a compound having the following general formula I:
  • compositions having antiprogestational activity may also be characterized by antagonizing the effects of progesterone.
  • the compositions may be of particular value in the control of hormonal irregularities in the menstrual cycle, for controlling endometriosis and dysmenorrhea, and for inducing menses.
  • the compositions can be used as a method of providing hormone therapy either alone or in combination with estrogenic substances in postmenopausal women, or in women whose ovarian hormone production is otherwise compromised.
  • Formulations for oral use can also be presented as hard gelatin capsules wherein the active ingredient is mixed with an inert solid diluent, for example calcium carbonate, calcium phosphate or kaolin, or as soft gelatin capsules wherein the active ingredient is mixed with water or an oil medium, such as peanut oil, liquid paraffin or olive oil.
  • an inert solid diluent for example calcium carbonate, calcium phosphate or kaolin
  • soft gelatin capsules wherein the active ingredient is mixed with water or an oil medium, such as peanut oil, liquid paraffin or olive oil.
  • Aqueous suspensions may contain the active materials in admixture with excipients suitable for the manufacture of aqueous suspensions.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Endocrinology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Epidemiology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

L'invention concerne des compositions ayant une stabilité améliorée, comprenant un sel pharmaceutiquement acceptable d'un composé associé à un stéroïde.
EP08713475A 2007-01-17 2008-01-03 Sels pharmaceutiquement acceptables de dérivés de 11-(4-aminophenyl)-19-norpregna-4,9(10)-diène-3, 20-dione Withdrawn EP2125858A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US88536307P 2007-01-17 2007-01-17
PCT/US2008/050128 WO2008088935A2 (fr) 2007-01-17 2008-01-03 Procédés pour une stabilité améliorée de dérivés de stéroïdes

Publications (1)

Publication Number Publication Date
EP2125858A2 true EP2125858A2 (fr) 2009-12-02

Family

ID=39387140

Family Applications (1)

Application Number Title Priority Date Filing Date
EP08713475A Withdrawn EP2125858A2 (fr) 2007-01-17 2008-01-03 Sels pharmaceutiquement acceptables de dérivés de 11-(4-aminophenyl)-19-norpregna-4,9(10)-diène-3, 20-dione

Country Status (16)

Country Link
EP (1) EP2125858A2 (fr)
JP (1) JP2010516686A (fr)
KR (1) KR20090105944A (fr)
CN (1) CN101616926A (fr)
AR (1) AR064947A1 (fr)
AU (1) AU2008206599A1 (fr)
BR (1) BRPI0806572A2 (fr)
CA (1) CA2674440A1 (fr)
CL (1) CL2008000138A1 (fr)
CR (1) CR10924A (fr)
EA (1) EA200970692A1 (fr)
EC (1) ECSP099537A (fr)
IL (1) IL199684A0 (fr)
MX (1) MX2009007313A (fr)
TW (1) TW200835503A (fr)
WO (1) WO2008088935A2 (fr)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI477276B (zh) * 2008-04-28 2015-03-21 Repros Therapeutics Inc 抗黃體素給藥方案
US8512745B2 (en) 2008-12-08 2013-08-20 Laboratoire Hra Pharma Ulipristal acetate tablets
HUP0900171A2 (hu) 2009-03-20 2010-12-28 Richter Gedeon Nyrt 17-acetoxi-11ß-[4-(dimetil-amino)-fenil]-21-metoxi-19-norpregna-4,9-dién-3,20-dion új kristályos módosulata és eljárás elõállítására
HUP0900487A2 (hu) 2009-08-05 2011-03-28 Richter Gedeon Nyrt 17-acetoxi-11ß-[4-(dimetil-amino)-fenil]-21-metoxi-19-norpregna-4,9-dién-3,20-dion új kristályos polimorf módosulata és eljárás elõállítására

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA8231B (en) * 1981-01-09 1982-11-24 Roussel Uclaf New 11 -substituted steroid derivatives, their preparation, their use as medicaments, the compositions containing them and the new intermediates thus obtained
US6020328A (en) * 1998-03-06 2000-02-01 Research Triangle Institute 20-keto-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties
US8044223B2 (en) * 2003-04-04 2011-10-25 Bridge Organics Co. Crystalline 19-norsteroids

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO2008088935A2 *

Also Published As

Publication number Publication date
JP2010516686A (ja) 2010-05-20
MX2009007313A (es) 2009-07-15
AR064947A1 (es) 2009-05-06
EA200970692A1 (ru) 2010-02-26
CR10924A (es) 2009-10-30
KR20090105944A (ko) 2009-10-07
BRPI0806572A2 (pt) 2014-05-06
TW200835503A (en) 2008-09-01
CL2008000138A1 (es) 2008-05-16
WO2008088935A2 (fr) 2008-07-24
CN101616926A (zh) 2009-12-30
ECSP099537A (es) 2009-08-28
AU2008206599A1 (en) 2008-07-24
CA2674440A1 (fr) 2008-07-24
IL199684A0 (en) 2010-04-15
WO2008088935A3 (fr) 2009-03-05

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EP2125858A2 (fr) Sels pharmaceutiquement acceptables de dérivés de 11-(4-aminophenyl)-19-norpregna-4,9(10)-diène-3, 20-dione
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