AR064947A1 - Metodos para mejorar la estabilidad de derivados esteroides - Google Patents

Metodos para mejorar la estabilidad de derivados esteroides

Info

Publication number
AR064947A1
AR064947A1 ARP080100217A ARP080100217A AR064947A1 AR 064947 A1 AR064947 A1 AR 064947A1 AR P080100217 A ARP080100217 A AR P080100217A AR P080100217 A ARP080100217 A AR P080100217A AR 064947 A1 AR064947 A1 AR 064947A1
Authority
AR
Argentina
Prior art keywords
group
alkyl
alkoxy
salt
compound
Prior art date
Application number
ARP080100217A
Other languages
English (en)
Inventor
Joseph Podolski
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 AR064947A1 publication Critical patent/AR064947A1/es

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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Reproductive Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Gynecology & Obstetrics (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

Composiciones con estabilidad mejorada que comprenden una sal aceptable para uso farmacéutico de un compuesto relacionado con los esteroides. Reivindicacion 1: Una composicion caracterizada porque comprende una sal aceptable para uso farmacéutico de un compuesto con la formula general (1) donde: R1 es un grupo funcional básico que se selecciona entre el grupo que consiste en -N(CH3)2, -NHCH3, -NC4H8, -NC5H10, y -NC4H8O; R2 es un miembro que se selecciona entre el grupo que consiste en hidrogeno, halogeno, alquilo, acilo, hidroxi, alcoxi, aciloxi, carbonato de alquilo, cipioniloxi, S-alquilo, -SCN, S-acilo, y -OC(O)R6, donde R6 es un miembro que se selecciona entre el grupo que consiste en alquilo, alcoxi éster y alcoxi; R3 es un miembro que se selecciona entre el grupo que consiste en alquil-alcoxi, alcoxi y aciloxi; R4 es un miembro que se selecciona entre el grupo que consiste en hidrogeno y alquilo; X es un miembro que se selecciona entre el grupo que consiste en =O y =N- OR5, donde R5 es un miembro que se selecciona entre el grupo que consiste en hidrogeno y alquilo; donde dicha sal aceptable para uso farmacéutico tiene mayor estabilidad en comparacion con una cantidad equivalente de la base libre de dicho compuesto; y con la condicion de que cuando R1 es -N(CH3)2, R2 es metoxi, R3 es acetoxi, R4 es metilo y X es =O, la sal no es una sal de HCI o HBr. Reivindicacion 2: La composicion de la reivindicacion 1, caracterizada porque dicho compuesto es 17alfa-acetoxi-11beta-[4-(N,N-dimetilamino)fenil]-19-norpregna-4,9(10)-dieno-3,20-diona. Reivindicacion 8: Un método para producir un efecto antiprogestágeno en un paciente, caracterizado porque dicho método comprende administrar a dicho paciente una cantidad efectiva de la composicion de la reivindicacion 1 o la reivindicacion 6.
ARP080100217A 2007-01-17 2008-01-17 Metodos para mejorar la estabilidad de derivados esteroides AR064947A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US88536307P 2007-01-17 2007-01-17

Publications (1)

Publication Number Publication Date
AR064947A1 true AR064947A1 (es) 2009-05-06

Family

ID=39387140

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP080100217A AR064947A1 (es) 2007-01-17 2008-01-17 Metodos para mejorar la estabilidad de derivados esteroides

Country Status (16)

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

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

Also Published As

Publication number Publication date
IL199684A0 (en) 2010-04-15
BRPI0806572A2 (pt) 2014-05-06
TW200835503A (en) 2008-09-01
WO2008088935A3 (en) 2009-03-05
CL2008000138A1 (es) 2008-05-16
CR10924A (es) 2009-10-30
ECSP099537A (es) 2009-08-28
AU2008206599A1 (en) 2008-07-24
MX2009007313A (es) 2009-07-15
CA2674440A1 (en) 2008-07-24
EA200970692A1 (ru) 2010-02-26
KR20090105944A (ko) 2009-10-07
JP2010516686A (ja) 2010-05-20
WO2008088935A2 (en) 2008-07-24
CN101616926A (zh) 2009-12-30
EP2125858A2 (en) 2009-12-02

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