WO2001026603A3 - Mesoprogestines (modulateurs de recepteur de progesterone) comme composants de contraceptifs feminins - Google Patents

Mesoprogestines (modulateurs de recepteur de progesterone) comme composants de contraceptifs feminins Download PDF

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Publication number
WO2001026603A3
WO2001026603A3 PCT/IB2000/002053 IB0002053W WO0126603A3 WO 2001026603 A3 WO2001026603 A3 WO 2001026603A3 IB 0002053 W IB0002053 W IB 0002053W WO 0126603 A3 WO0126603 A3 WO 0126603A3
Authority
WO
WIPO (PCT)
Prior art keywords
mesoprogestins
female
progesterone receptor
component
contraception
Prior art date
Application number
PCT/IB2000/002053
Other languages
English (en)
Other versions
WO2001026603A2 (fr
Inventor
Kristof Chwalisz
Walter Elger
Gerd Schubert
Original Assignee
Jenapharm Gmbh
Kristof Chwalisz
Walter Elger
Gerd Schubert
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
Priority to PL00353994A priority Critical patent/PL353994A1/xx
Priority to MXPA02002186A priority patent/MXPA02002186A/es
Priority to SI200020043A priority patent/SI20853A/sl
Priority to EP00991299A priority patent/EP1605949A2/fr
Priority to AU32150/01A priority patent/AU781835B2/en
Priority to KR1020027002785A priority patent/KR20020038745A/ko
Priority to HU0202515A priority patent/HUP0202515A3/hu
Priority to SK298-2002A priority patent/SK2982002A3/sk
Priority to CA002383650A priority patent/CA2383650A1/fr
Priority to IL14841500A priority patent/IL148415A0/xx
Application filed by Jenapharm Gmbh, Kristof Chwalisz, Walter Elger, Gerd Schubert filed Critical Jenapharm Gmbh
Priority to UA2002032429A priority patent/UA77150C2/uk
Priority to BR0013711-1A priority patent/BR0013711A/pt
Priority to EA200200284A priority patent/EA006805B1/ru
Priority to EEP200200103A priority patent/EE200200103A/xx
Priority to NZ517470A priority patent/NZ517470A/en
Priority to JP2001529395A priority patent/JP2003511399A/ja
Publication of WO2001026603A2 publication Critical patent/WO2001026603A2/fr
Publication of WO2001026603A3 publication Critical patent/WO2001026603A3/fr
Priority to BG06441A priority patent/BG106441A/bg
Priority to NO20020998A priority patent/NO20020998L/no
Priority to HR20020265A priority patent/HRP20020265A2/hr

Links

Classifications

    • 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
    • A61K31/565—Compounds 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
    • A61K31/567—Compounds 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 substituted in position 17 alpha, e.g. mestranol, norethandrolone
    • 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
    • A61K31/565—Compounds 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
    • 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
    • A61P15/18—Feminine contraceptives
    • 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
    • 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
    • A61P5/30—Oestrogens

Landscapes

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

Abstract

La présente invention concerne l'utilisation de mésoprogestines destinée à la production d'un produit pharmaceutique pour contraception féminine, une préparation pharmaceutique destinée à la contraception féminine ainsi qu'un procédé de contraception féminine par administration de quantités effectives de mésoprogestine dans une contraception féminine recherchée. La mésoprogestine peut, éventuellement, être utilisée en combinaison avec un oestrogène. Les mésoprogestines sont définies comme des composés possédant à la fois des activités agonistes et antagonistes au récepteur de progestérone (PR) in vivo. Elles stabilisent la fonction du PR à un niveau intermédiaire d'activité agoniste et antagoniste. On ne peut pas obtenir des états fonctionnels correspondants avec des progestines ou des antiprogestines. Selon l'invention, les mésoprogestines préférées sont les J867, J912, J956 et J1042.
PCT/IB2000/002053 1999-08-31 2000-08-31 Mesoprogestines (modulateurs de recepteur de progesterone) comme composants de contraceptifs feminins WO2001026603A2 (fr)

Priority Applications (19)

Application Number Priority Date Filing Date Title
UA2002032429A UA77150C2 (en) 1999-08-31 2000-08-31 Use of mesoprogestins j867, j912, or j1042 for female contraception, pharmaceutical composition and kit (variants)
MXPA02002186A MXPA02002186A (es) 1999-08-31 2000-08-31 Mesoprogestinas (moduladores del receptor de progesterona) como un componente de los anticonceptivos femeninos.
EP00991299A EP1605949A2 (fr) 1999-08-31 2000-08-31 Mesoprogestines (modulateurs de recepteur de progesterone) comme composants de contraceptifs feminins
AU32150/01A AU781835B2 (en) 1999-08-31 2000-08-31 Mesoprogestins (progesterone receptor modulators) as a component of female contraceptives
KR1020027002785A KR20020038745A (ko) 1999-08-31 2000-08-31 여성 피임제 성분으로서의 메조프로게스틴 (프로게스테론수용체 조절물질)
HU0202515A HUP0202515A3 (en) 1999-08-31 2000-08-31 Mesoprogestins (progesterone receptor modulators) as a component of female contraceptives
SK298-2002A SK2982002A3 (en) 1999-08-31 2000-08-31 Mesoprogestins (progesterone receptor modulators) as a component of female contraceptives
BR0013711-1A BR0013711A (pt) 1999-08-31 2000-08-31 Mesoprogestinas (moduladores de receptores de progesterona) como um componente de contraceptivos femininos
IL14841500A IL148415A0 (en) 1999-08-31 2000-08-31 Mesoprogestins (progesterone receptor modulators) as a component of female contraceptives
PL00353994A PL353994A1 (en) 1999-08-31 2000-08-31 Mesoprogestins (progesterone receptor modulators) as a component of female contraceptives
SI200020043A SI20853A (sl) 1999-08-31 2000-08-31 Mezoprogestini (modulatorji receptorja progesterona) kot sestavina ženskih kontraceptivov
CA002383650A CA2383650A1 (fr) 1999-08-31 2000-08-31 Mesoprogestines (modulateurs de recepteur de progesterone) comme composants de contraceptifs feminins
EA200200284A EA006805B1 (ru) 1999-08-31 2000-08-31 Мезопрогестины (модуляторы рецептора прогестерона) в качестве компонента женских контрацептивов
EEP200200103A EE200200103A (et) 1999-08-31 2000-08-31 Mesoprogestiinid (progesterooniretseptori modulaatorid) naise kontratseptiivide komponendina
NZ517470A NZ517470A (en) 1999-08-31 2000-08-31 Mesoprogestins (progesterone receptor modulators) as a component of female contraceptives
JP2001529395A JP2003511399A (ja) 1999-08-31 2000-08-31 女性避妊薬の成分としてのメソプロゲスチン（プロゲステロン受容体モジュレーター）
BG06441A BG106441A (bg) 1999-08-31 2002-02-26 Мезопрогестини (модулатори на прогестероновия рецептор) като компоненти на женски контрацептиви
NO20020998A NO20020998L (no) 1999-08-31 2002-02-28 Mesoprogestiner (progesteronreseptormodulater) som en komponent i svangerskapsforebyggelse for kvinner
HR20020265A HRP20020265A2 (en) 1999-08-31 2002-03-28 Mesoprogestins (progesterone receptor modulators) as a component of female contraceptives

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US38613399A 1999-08-31 1999-08-31
US09/386,133 1999-08-31

Publications (2)

Publication Number Publication Date
WO2001026603A2 WO2001026603A2 (fr) 2001-04-19
WO2001026603A3 true WO2001026603A3 (fr) 2002-01-17

Family

ID=23524305

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2000/002053 WO2001026603A2 (fr) 1999-08-31 2000-08-31 Mesoprogestines (modulateurs de recepteur de progesterone) comme composants de contraceptifs feminins

Country Status (28)

Country Link
EP (1) EP1605949A2 (fr)
JP (1) JP2003511399A (fr)
KR (1) KR20020038745A (fr)
CN (1) CN1384748A (fr)
AR (1) AR025455A1 (fr)
AU (1) AU781835B2 (fr)
BG (1) BG106441A (fr)
BR (1) BR0013711A (fr)
CA (1) CA2383650A1 (fr)
CO (1) CO5190694A1 (fr)
CZ (1) CZ2002707A3 (fr)
EA (1) EA006805B1 (fr)
EE (1) EE200200103A (fr)
HR (1) HRP20020265A2 (fr)
HU (1) HUP0202515A3 (fr)
IL (1) IL148415A0 (fr)
LT (1) LT5001B (fr)
LV (1) LV12940B (fr)
MX (1) MXPA02002186A (fr)
NO (1) NO20020998L (fr)
NZ (1) NZ517470A (fr)
PE (1) PE20010579A1 (fr)
PL (1) PL353994A1 (fr)
SI (1) SI20853A (fr)
SK (1) SK2982002A3 (fr)
UA (1) UA77150C2 (fr)
WO (1) WO2001026603A2 (fr)
YU (1) YU13902A (fr)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10236405A1 (de) 2002-08-02 2004-02-19 Schering Ag Progesteronrezeptormodulatoren mit erhöhter antigonadotroper Aktivität für die weibliche Fertilitätskontrolle und Hormonersatztherapie
DK1525215T3 (da) * 2002-08-02 2007-01-15 Schering Ag Modulatorer for receptoren for progesteron med forhöjet anti-gonadotrop aktivitet til fertilitetskontrol hos kvinder og ved terapi til erstatning af hormoner
US7772219B2 (en) * 2003-05-02 2010-08-10 Teva Women's Health, Inc. Methods of hormonal treatment utilizing extended cycle contraceptive regimens
US20050215535A1 (en) * 2004-03-24 2005-09-29 Kristof Chwalisz Sequential SPRM/progestin treatment
EP1773344A1 (fr) * 2004-07-07 2007-04-18 Wyeth a Corporation of the State of Delaware Schémas cycliques de progestérone et trousses d"administration
DE102005050729A1 (de) * 2005-10-19 2007-04-26 Schering Ag Verfahren zur präventiven bedarfsweisen hormonalen Kontrazeption
JP5951480B2 (ja) * 2009-04-14 2016-07-13 ラボラトワール・アシュエールア−ファルマＬａｂｏｒａｔｏｉｒｅ Ｈｒａ−Ｐｈａｒｍａ オンデマンド避妊方法
CN110548034A (zh) * 2019-07-12 2019-12-10 广州莎蔓生物科技有限公司 一种怀孕阻断药物

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0309263A2 (fr) * 1987-09-24 1989-03-29 Jencap Research Limited Composition d'hormones et application
DE4332284A1 (de) * 1993-09-20 1995-03-23 Jenapharm Gmbh Neue 11-Benzaldoxim-17beta-methoxy-17alpha-methoxymethyl-estradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel
WO1996012494A1 (fr) * 1994-10-24 1996-05-02 Schering Aktiengesellschaft Antagonistes competitifs de la progesterone permettant de reguler a la demande la fecondite feminine
WO1997041866A1 (fr) * 1996-05-07 1997-11-13 Schering Aktiengesellschaft Augmentation du taux d'implantation apres fecondation in vitro
US5693628A (en) * 1993-09-20 1997-12-02 Jenapharm Gmbh 11-benzaldoxime-estra-diene derivatives, methods for their production and pharmaceuticals containing these compounds
WO1997049407A1 (fr) * 1996-06-25 1997-12-31 Akzo Nobel N.V. Schemas posologiques de progestogene et anti-progestogene
WO1998005679A2 (fr) * 1996-08-05 1998-02-12 Duke University Antagonistes mixtes du recepteur progesterone et techniques de dosage associees
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
WO2000066590A2 (fr) * 1999-05-04 2000-11-09 Ligand Pharmaceuticals, Inc. Composes modulateurs de recepteur de progesterone tetracycliques et procedes

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US2054271A (en) 1932-05-17 1936-09-15 Schering Kahlbaum Ag Production of crystallized hormone esters
DE699310C (de) 1936-11-20 1940-11-27 Chemische Ind Ges Verfahren zur Herstellung von in 3-Stellung veresterten Verbindungen vom Typus des Oestradiols
US2225419A (en) 1937-03-01 1940-12-17 Schering Corp Process for the conversion of 17-cisalcohols of the cyclopentanopolyhydrophenanthrene series into the corresponding 17-trans-alcohols
US2611773A (en) 1951-08-21 1952-09-23 Upjohn Co Estradiol 17-cyclopenetanepropionate
US2990414A (en) 1957-03-26 1961-06-27 Syntex Sa 17-undecenoate of estradiol
DE3337450A1 (de) 1983-10-12 1985-04-25 Schering AG, 1000 Berlin und 4709 Bergkamen Prostaglandine und antigestagene fuer den schwangerschaftsabbruch
US5439913A (en) 1992-05-12 1995-08-08 Schering Aktiengesellschaft Contraception method using competitive progesterone antagonists and novel compounds useful therein
US5516769A (en) 1993-02-19 1996-05-14 The Medical College Of Hampton Roads Method of inhibiting fertilization
DE4429397C2 (de) 1994-08-09 2003-11-20 Jenapharm Gmbh Estra-1,3,5(10)-trien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen
DE4429398C2 (de) 1994-08-09 1997-09-11 Jenapharm Gmbh Verwendung von Estra-1,3,5(10)-trien-Derivaten zur hormonalen Kontrazeption

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0309263A2 (fr) * 1987-09-24 1989-03-29 Jencap Research Limited Composition d'hormones et application
DE4332284A1 (de) * 1993-09-20 1995-03-23 Jenapharm Gmbh Neue 11-Benzaldoxim-17beta-methoxy-17alpha-methoxymethyl-estradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel
US5693628A (en) * 1993-09-20 1997-12-02 Jenapharm Gmbh 11-benzaldoxime-estra-diene derivatives, methods for their production and pharmaceuticals containing these compounds
WO1996012494A1 (fr) * 1994-10-24 1996-05-02 Schering Aktiengesellschaft Antagonistes competitifs de la progesterone permettant de reguler a la demande la fecondite feminine
WO1997041866A1 (fr) * 1996-05-07 1997-11-13 Schering Aktiengesellschaft Augmentation du taux d'implantation apres fecondation in vitro
WO1997049407A1 (fr) * 1996-06-25 1997-12-31 Akzo Nobel N.V. Schemas posologiques de progestogene et anti-progestogene
WO1998005679A2 (fr) * 1996-08-05 1998-02-12 Duke University Antagonistes mixtes du recepteur progesterone et techniques de dosage associees
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
WO2000066590A2 (fr) * 1999-05-04 2000-11-09 Ligand Pharmaceuticals, Inc. Composes modulateurs de recepteur de progesterone tetracycliques et procedes

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CONRAD, CONRAD PROGRAM BIENNIAL REPORT 1998-1999, XP002170202, Retrieved from the Internet <URL:http://www.conrad.org/bi-annual_Report.pdf> [retrieved on 20010620] *
JEWGENOW K ET AL: "Comparative binding affinity study of progestins to the cytosol progestin receptor of endometrium in different mammals.", GENERAL AND COMPARATIVE ENDOCRINOLOGY, vol. 110, no. 2, May 1998 (1998-05-01), pages 118 - 124, XP001006069, ISSN: 0016-6480 *
QUEST M ET AL: "Antigestagens - a new contraceptive method in captive bears?", REPRODUCTION IN DOMESTIC ANIMALS, vol. 34, no. 1, February 1999 (1999-02-01), 32nd Conference on Physiology and Pathology of Reproduction;Hannover, Germany; February 18-19, 1999, pages 32, XP001006070, ISSN: 0936-6768 *

Also Published As

Publication number Publication date
SI20853A (sl) 2002-10-31
NO20020998D0 (no) 2002-02-28
LT5001B (lt) 2003-03-25
EA006805B1 (ru) 2006-04-28
LV12940B (en) 2003-06-20
BG106441A (bg) 2002-09-30
KR20020038745A (ko) 2002-05-23
MXPA02002186A (es) 2002-09-02
CZ2002707A3 (cs) 2002-11-13
CN1384748A (zh) 2002-12-11
YU13902A (sh) 2006-01-16
PE20010579A1 (es) 2001-06-04
CO5190694A1 (es) 2002-08-29
JP2003511399A (ja) 2003-03-25
SK2982002A3 (en) 2002-07-02
PL353994A1 (en) 2003-12-15
WO2001026603A2 (fr) 2001-04-19
AR025455A1 (es) 2002-11-27
EE200200103A (et) 2003-04-15
LT2002035A (lt) 2002-10-25
EP1605949A2 (fr) 2005-12-21
HUP0202515A3 (en) 2004-06-28
HRP20020265A2 (en) 2004-02-29
CA2383650A1 (fr) 2001-04-19
IL148415A0 (en) 2002-09-12
NZ517470A (en) 2004-03-26
HUP0202515A2 (hu) 2002-12-28
EA200200284A1 (ru) 2002-10-31
AU3215001A (en) 2001-04-23
BR0013711A (pt) 2002-05-07
NO20020998L (no) 2002-03-14
UA77150C2 (en) 2006-11-15
AU781835B2 (en) 2005-06-16

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