CO5200772A1 - Mesoprogestinas (moduladores de receptores de progesterona) para el trataiento y la prevencion de transtornos ginecolo- gicos benignos hormona-dependientes - Google Patents

Mesoprogestinas (moduladores de receptores de progesterona) para el trataiento y la prevencion de transtornos ginecolo- gicos benignos hormona-dependientes

Info

Publication number
CO5200772A1
CO5200772A1 CO00065515A CO00065515A CO5200772A1 CO 5200772 A1 CO5200772 A1 CO 5200772A1 CO 00065515 A CO00065515 A CO 00065515A CO 00065515 A CO00065515 A CO 00065515A CO 5200772 A1 CO5200772 A1 CO 5200772A1
Authority
CO
Colombia
Prior art keywords
progesterone
treatment
prevention
disorders
mcphail
Prior art date
Application number
CO00065515A
Other languages
English (en)
Inventor
Walter Elger
Chwalisz Kristof
Gerd Schubert
Original Assignee
Jenapharm Gmbh And Co Kg
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 Jenapharm Gmbh And Co Kg filed Critical Jenapharm Gmbh And Co Kg
Publication of CO5200772A1 publication Critical patent/CO5200772A1/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/04Drugs for genital or sexual disorders; Contraceptives for inducing labour or abortion; Uterotonics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32Antioestrogens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/34Gestagens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents

Landscapes

  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)

Abstract

La presente invención descubre el uso de mesoprogestinas, una nueva clase de moduladores de receptor de progesterona (MRP), para el tratamiento y la prevención de trastornos ginecológicos benignos hormona-dependientes: a) para el tratamiento de trastornos ginecológicos tales como la endometriosis, los fibromas uterinos, las adherencias peritoneales postoperatorias, la hemorragia disfuncional (metrorragia, menorragia) y la dismenorrea; b) para prevenir trastornos ginecológicos tales como las adherencias peritoneales postoperatorias, hemorragia uterina disfuncional (metrorragia, menorragia) y dismenorrea y c) un método para tratar y prevenir los trastornos antes mencionados en una hembra, preferentemente una hembra humana, que necesite tratamiento o prevención de uno o más de los mencionados trastornos con una cantidad efectiva de mesoprogestina. Las mesoprogestinas se definen como compuestos que disponen de actividad tanto agonística como antagonística en el receptor de progesterona (RP) in vivo. Estabilizan la función de PR en un nivel intermedio entre agonístico y antagonístico. Las progestinas y las antiprogestinas no permiten lograr los mismos estados funcionales. La dosis diaria de mesoprogestina es de 0.5 a 100 mg, preferentemente de 5,0 a 50 mg y más preferentemente de 10 a 25 mg. J867, J912, J956 y J1042 son las mesoprogestinas preferidas de acuerdo con la invención.Figuras 1A y 1BEfectos tipo progesterona (arriba, Figura 1A) yantagonísticos de progesterona (debajo, Figura 1B) de losmoduladores de RP en el útero de conejos inmaduros preparados con estrógeno (prueba de McPhail).Figura lA:Resultado de McPhail<EMI FILE="00065515_1" ID="1" IMF=JPEG >mg/animal/díavehículo - progesterona - RU486 - J867 - J956 - J1042Figura 1BResultado de McPhail<EMI FILE="00065515_2" ID="2" IMF=JPEG >mg/animal/día (dosis de sustancias de prueba + 1,0 mg de progesterona).
CO00065515A 1999-08-31 2000-08-31 Mesoprogestinas (moduladores de receptores de progesterona) para el trataiento y la prevencion de transtornos ginecolo- gicos benignos hormona-dependientes CO5200772A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US38614199A 1999-08-31 1999-08-31

Publications (1)

Publication Number Publication Date
CO5200772A1 true CO5200772A1 (es) 2002-09-27

Family

ID=23524338

Family Applications (1)

Application Number Title Priority Date Filing Date
CO00065515A CO5200772A1 (es) 1999-08-31 2000-08-31 Mesoprogestinas (moduladores de receptores de progesterona) para el trataiento y la prevencion de transtornos ginecolo- gicos benignos hormona-dependientes

Country Status (34)

Country Link
EP (1) EP1229906B1 (es)
JP (1) JP2003535029A (es)
KR (3) KR100755109B1 (es)
AR (1) AR025457A1 (es)
AT (1) ATE375160T1 (es)
AU (1) AU781840B2 (es)
BG (1) BG65817B1 (es)
BR (1) BR0014161A (es)
CA (1) CA2382580C (es)
CO (1) CO5200772A1 (es)
CZ (1) CZ2002704A3 (es)
DE (1) DE60036723T2 (es)
DK (1) DK1229906T3 (es)
EA (1) EA007854B1 (es)
EE (1) EE05172B1 (es)
ES (1) ES2295050T3 (es)
HR (1) HRP20020267A2 (es)
HU (1) HUP0202429A3 (es)
IL (1) IL148416A0 (es)
LT (1) LT5034B (es)
LV (1) LV12941B (es)
ME (1) MEP13808A (es)
MX (1) MXPA02002191A (es)
NO (1) NO20020999L (es)
NZ (1) NZ517471A (es)
PE (1) PE20010578A1 (es)
PL (1) PL198790B1 (es)
PT (1) PT1229906E (es)
RO (1) RO122179B1 (es)
RS (1) RS50283B (es)
SI (1) SI20852B (es)
SK (1) SK287192B6 (es)
UA (1) UA78184C2 (es)
WO (1) WO2001015679A2 (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2003255355A1 (en) * 2002-08-02 2004-02-25 Schering Aktiengesellschaft Progesterone receptor modulators having an increased antigonadotropic activity for use in female fertility testing and hormone replacement therapy
DE10236405A1 (de) 2002-08-02 2004-02-19 Schering Ag Progesteronrezeptormodulatoren mit erhöhter antigonadotroper Aktivität für die weibliche Fertilitätskontrolle und Hormonersatztherapie
US20040097591A1 (en) * 2002-11-18 2004-05-20 Kristof Chwalisz Use of selective progesterone receptor modulators for the treatment of androgen deficiency
DE102007011105A1 (de) 2007-03-02 2008-09-04 Bayer Schering Pharma Aktiengesellschaft Mineralcorticoid-Rezeptor-Antagonisten zur Behandlung von Endometriose
WO2010147184A1 (ja) * 2009-06-17 2010-12-23 国立大学法人熊本大学 月経困難症の予防及び/又は治療薬
US8399432B2 (en) * 2009-10-27 2013-03-19 Lipogen Ltd. Compositions and methods of treatment for alleviating premenstrual syndrome symptoms
JP2022548314A (ja) * 2019-09-23 2022-11-17 ザ ボード オブ トラスティーズ オブ ザ レランド スタンフォード ジュニア ユニバーシティー 妊娠を遷延させるためおよび月経または妊娠の合併症の処置の方法

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3633244A1 (de) 1986-09-26 1988-03-31 Schering Ag Antigestagene zur hemmung der uterinen prostaglandinsynthese
DE4332283A1 (de) * 1993-09-20 1995-04-13 Jenapharm Gmbh Neue 11-Benzaldoximestradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel
DE4332284C2 (de) 1993-09-20 1997-05-28 Jenapharm Gmbh 11-Benzaldoxim-17beta-methoxy-17alpha-methoxymethyl-estradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel
US5681817A (en) * 1994-02-04 1997-10-28 The Medical College Of Hampton Roads Treatment of ovarian estrogen dependent conditions
US5576310A (en) * 1994-09-20 1996-11-19 Jenapharm Gmbh 11-benzaldoxime-17β-methoxy-17α-methoxymethyl-estrasdiene derivatives, methods for their production and pharmaceuticals containing such compounds
US5696133A (en) * 1994-12-22 1997-12-09 Ligand Pharmaceuticals Incorporated Steroid receptor modulator compounds and methods
ES2208699T3 (es) * 1994-12-22 2004-06-16 Ligand Pharmaceuticals Incorporated Compuestos y metodos moduladores de receptores de esteroides.
KR100370908B1 (ko) 1995-02-02 2003-04-10 쉐링 악티엔게젤샤프트 기능부전성자궁출혈치료용약제의제조에유용한프로게스테론길항제
DE19604231A1 (de) * 1996-01-29 1997-07-31 Schering Ag Pharmazeutisches Kombinationspräparat und seine Verwendung zur Behandlung von gynäkologischen Störungen
US6861415B2 (en) * 1996-05-01 2005-03-01 The United States Of America As Represented By The Department Of Health And Human Services 21-substituted progesterone derivatives as new antiprogestational agents
WO1998005679A2 (en) * 1996-08-05 1998-02-12 Duke University Mixed agonists of the progesterone receptor and assays therefor
DE19809845A1 (de) * 1998-03-03 1999-09-09 Jenapharm Gmbh S-substituierte 11beta-Benzaldoxim-estra-4,9-dien-kohlensäurethiolester, Verfahren zu deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zubereitungen
CA2359562A1 (en) * 1999-01-14 2000-07-20 Bayer Corporation Substituted 2-arylimino heterocycles and compositions containing them, for use as progesterone receptor binding agents
AU4501800A (en) * 1999-05-04 2000-11-17 American Home Products Corporation Tetracyclic progesterone receptor modulator compounds and methods

Also Published As

Publication number Publication date
AU781840B2 (en) 2005-06-16
AU6946600A (en) 2001-03-26
EA007854B1 (ru) 2007-02-27
LT5034B (lt) 2003-07-25
EP1229906B1 (en) 2007-10-10
NZ517471A (en) 2004-02-27
HUP0202429A3 (en) 2004-04-28
WO2001015679A2 (en) 2001-03-08
SK287192B6 (sk) 2010-02-08
IL148416A0 (en) 2002-09-12
NO20020999L (no) 2002-03-14
ATE375160T1 (de) 2007-10-15
ES2295050T3 (es) 2008-04-16
RO122179B1 (ro) 2009-02-27
PE20010578A1 (es) 2001-06-04
DE60036723D1 (de) 2007-11-22
BG106442A (bg) 2002-09-30
KR20080066095A (ko) 2008-07-15
HRP20020267A2 (en) 2004-04-30
EE200200104A (et) 2003-04-15
PT1229906E (pt) 2008-01-18
JP2003535029A (ja) 2003-11-25
HUP0202429A2 (en) 2002-10-28
SI20852A (sl) 2002-10-31
RS50283B (sr) 2009-09-08
CA2382580C (en) 2009-05-19
DE60036723T2 (de) 2008-07-17
KR20020027616A (ko) 2002-04-13
PL198790B1 (pl) 2008-07-31
CA2382580A1 (en) 2001-03-08
BR0014161A (pt) 2002-05-21
LT2002031A (en) 2003-02-25
EA200200282A1 (ru) 2002-10-31
DK1229906T3 (da) 2008-02-11
BG65817B1 (bg) 2010-01-29
NO20020999D0 (no) 2002-02-28
EP1229906A2 (en) 2002-08-14
KR100864547B1 (ko) 2008-10-20
WO2001015679A3 (en) 2001-11-22
SK2992002A3 (en) 2002-07-02
CZ2002704A3 (cs) 2003-02-12
PL353930A1 (en) 2003-12-15
UA78184C2 (en) 2007-03-15
MXPA02002191A (es) 2002-09-30
SI20852B (sl) 2009-06-30
LV12941B (en) 2003-06-20
EE05172B1 (et) 2009-06-15
KR100755109B1 (ko) 2007-09-04
KR20070058023A (ko) 2007-06-07
MEP13808A (en) 2010-06-10
AR025457A1 (es) 2002-11-27
YU14002A (sh) 2006-01-16

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