WO2002079220A2 - Aminosterol compounds, their use in the preparation of meiosis-regulating medicaments and method for their preparation - Google Patents

Aminosterol compounds, their use in the preparation of meiosis-regulating medicaments and method for their preparation Download PDF

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Publication number
WO2002079220A2
WO2002079220A2 PCT/EP2002/003148 EP0203148W WO02079220A2 WO 2002079220 A2 WO2002079220 A2 WO 2002079220A2 EP 0203148 W EP0203148 W EP 0203148W WO 02079220 A2 WO02079220 A2 WO 02079220A2
Authority
WO
WIPO (PCT)
Prior art keywords
pregna
methyl
substituted
unsubstituted
dien
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.)
Ceased
Application number
PCT/EP2002/003148
Other languages
English (en)
French (fr)
Other versions
WO2002079220A3 (en
Inventor
Thorsten Blume
Peter Esperling
Christa Hegele-Hartung
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.)
Bayer Pharma AG
Novo Nordisk AS
Original Assignee
Schering AG
Novo Nordisk AS
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 IL15727202A priority Critical patent/IL157272A0/xx
Priority to AU2002315260A priority patent/AU2002315260B2/en
Priority to EP02740430A priority patent/EP1401856A2/en
Priority to CA002438210A priority patent/CA2438210A1/en
Priority to KR10-2003-7012456A priority patent/KR20030088043A/ko
Priority to BR0208381-7A priority patent/BR0208381A/pt
Priority to UA2003109610A priority patent/UA75130C2/uk
Priority to JP2002577844A priority patent/JP2004534011A/ja
Priority to HU0303643A priority patent/HUP0303643A2/hu
Priority to HK05103729.7A priority patent/HK1070900B/xx
Application filed by Schering AG, Novo Nordisk AS filed Critical Schering AG
Priority to MXPA03008199A priority patent/MXPA03008199A/es
Publication of WO2002079220A2 publication Critical patent/WO2002079220A2/en
Priority to NO20034273A priority patent/NO20034273L/no
Anticipated expiration legal-status Critical
Publication of WO2002079220A3 publication Critical patent/WO2002079220A3/en
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • 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
    • C07J41/005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of only two carbon atoms, e.g. pregnane derivatives
    • 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
    • A61P15/08—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed

Definitions

  • novel steroid compounds have a number of chiral centers such that these compounds exist in several isomeric forms. All these isomeric forms are within the scope of the present invention unless otherwise described herein.
  • the phenyl and 1-naphthyl radical may also be substituted by halogen, C-i - C 4 alkoxy, hydroxy or Ci - C 4 alkyl, including the fluoroalkoxy and fluoroalkyl derivatives.
  • R 23 and R 23' independently, may further be e.g. 4-hydroxyphenyl, 4-methoxyphenyl, 2,4,6- trimethylphenyl, 2,4-dichlorophenyl, 4-fluorophenyl, 4-trifluoromethylphenyl and 2-pentafluoroethylphenyl.
  • the compound was added to culture media in 3 ⁇ M concentration and allowed to interact with the gamete prior to fertilization either to mediate or to improve the process of meiotic maturation.
  • the oocytes were fertilized in vitro, cultured in vitro and back-transferred to the patient uterus typically on day 3 after oocyte collection.
  • the patient was given progesterone (crinone vaginal gel, 1 doser per day) and/or oestradiol (oestradiol-valerate 2 mg/day) to improve implantation and render the uterus more receptive.
  • the compound added to culture medium significantly improved on the quality of oocyte maturation, which led to higher fertilization rates, higher pre-implantation development, higher implantation rates and ultimately a higher success rate of healthy born human infants.
  • Example 30 Treatment regimen for male contraception using a MAS antagonist blocking the process of meiosis in testis

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
PCT/EP2002/003148 2001-03-26 2002-03-20 Aminosterol compounds, their use in the preparation of meiosis-regulating medicaments and method for their preparation Ceased WO2002079220A2 (en)

Priority Applications (12)

Application Number Priority Date Filing Date Title
HU0303643A HUP0303643A2 (hu) 2001-03-26 2002-03-20 Szteroid vegyületek, ezek felhasználása meiosis szabályozására alkalmas gyógyszerkészítmény előállítására és eljárás ezen vegyületek előállítására
EP02740430A EP1401856A2 (en) 2001-03-26 2002-03-20 Steroid compounds, use of these compounds for the preparation of meiosis-regulating medicaments and method for the preparation of these compounds
CA002438210A CA2438210A1 (en) 2001-03-26 2002-03-20 Steroid compounds, use of these compounds for the preparation of meiosis-regulating medicaments and method for the preparation of these compounds
KR10-2003-7012456A KR20030088043A (ko) 2001-03-26 2002-03-20 스테로이드 화합물, 이 화합물의 감수분열 조절 약제 제조용도 및 이 화합물의 제조 방법
BR0208381-7A BR0208381A (pt) 2001-03-26 2002-03-20 Compostos esteróides, utilização desses compostos para a preparação de medicamentos reguladores de meiose e processo para a preparação desses compostos
UA2003109610A UA75130C2 (en) 2001-03-26 2002-03-20 Steroid compounds, use of these compounds for obtaining medicament regulating meiosis and a method for producing these compounds (variants)
JP2002577844A JP2004534011A (ja) 2001-03-26 2002-03-20 ステロイド化合物類、減数分裂−調節薬剤の調製のためのそれらの化合物の使用、及びそれらの化合物の調製方法
IL15727202A IL157272A0 (en) 2001-03-26 2002-03-20 Steroid compounds, use of these compounds for the preparation of meiosis-regulating medicaments and method for the preparation of these compounds
AU2002315260A AU2002315260B2 (en) 2001-03-26 2002-03-20 Aminosterol compounds, their use in the preparation of meiosis-regulating medicaments and method for their preparation
HK05103729.7A HK1070900B (en) 2001-03-26 2002-03-20 Steroid compounds, use of these compounds for the preparation of meiosis-regulating medicaments and method for the preparation of these compounds
MXPA03008199A MXPA03008199A (es) 2001-03-26 2002-03-20 Compuestos esteroides, uso de estos compuestos para la preparacion de medicamentos que regulan la meiosis y metodo para la preparacion de estos compuestos.
NO20034273A NO20034273L (no) 2001-03-26 2003-09-25 Steroidforbindelser, anvendelse av disse forbindelsene til fremstilling avmeioseregulerende medikamenter og fremgangsmåte for fremstillingav disse forbindelsene

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP01250108A EP1245572A1 (en) 2001-03-26 2001-03-26 Aminosterol compounds, their use in the preparation of meiosis-regulating medicaments and method for their preparation
EP01250108.6 2001-03-26

Publications (2)

Publication Number Publication Date
WO2002079220A2 true WO2002079220A2 (en) 2002-10-10
WO2002079220A3 WO2002079220A3 (en) 2003-10-16

Family

ID=8181575

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2002/003148 Ceased WO2002079220A2 (en) 2001-03-26 2002-03-20 Aminosterol compounds, their use in the preparation of meiosis-regulating medicaments and method for their preparation

Country Status (18)

Country Link
US (1) US6916921B2 (https=)
EP (2) EP1245572A1 (https=)
JP (1) JP2004534011A (https=)
KR (1) KR20030088043A (https=)
CN (1) CN1332975C (https=)
AU (1) AU2002315260B2 (https=)
BR (1) BR0208381A (https=)
CA (1) CA2438210A1 (https=)
CZ (1) CZ20032578A3 (https=)
HU (1) HUP0303643A2 (https=)
IL (1) IL157272A0 (https=)
MX (1) MXPA03008199A (https=)
NO (1) NO20034273L (https=)
PL (1) PL369576A1 (https=)
RU (1) RU2289587C2 (https=)
UA (1) UA75130C2 (https=)
WO (1) WO2002079220A2 (https=)
ZA (1) ZA200308271B (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007500140A (ja) * 2003-07-28 2007-01-11 シエーリング アクチエンゲゼルシャフト チオモルホリノステロイド化合物、減数分裂調節薬剤を製造するためのそれらの使用、およびそれらの製造方法

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100689260B1 (ko) * 2005-05-24 2007-03-02 삼원산업주식회사 항산화성 스틸벤계 형광증백제 및 이의 합성방법

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1095167A (en) * 1963-12-05 1967-12-13 Shalom Sarel Amino-steroids
US3419661A (en) * 1964-01-13 1968-12-31 Univ Missouri Oral contraceptive for birds
DE1643004A1 (de) * 1967-02-07 1971-04-08 Schering Ag Bisnorcholenderivate und Verfahren zu ihrer Herstellung
DE1930473A1 (de) * 1969-06-14 1970-12-17 Schering Ag 22-N-substituierte (20R)-23,24-dinor-cholanderivate
US5716777A (en) 1994-06-23 1998-02-10 Novo Nordisk A/S Regulation of meiosis using sterols
HUP9800731A3 (en) * 1995-03-06 2000-03-28 Novo Nordisk As Stimulation of meiosis
CA2224866A1 (en) 1995-06-23 1997-01-09 Novo Nordisk A/S Meiosis regulating compounds
JP2001506656A (ja) 1996-12-20 2001-05-22 ノボ ノルディスク アクティーゼルスカブ 減数分裂調節化合物
WO1999058549A1 (en) * 1998-05-13 1999-11-18 Novo Nordisk A/S Meiosis regulating compounds
EP1098652A2 (en) 1998-05-26 2001-05-16 Schering Aktiengesellschaft Treatment of infertility with camp-increasing compounds alone or in combination with at least one meiosis-stimulating compound
CN1353617A (zh) 1999-02-24 2002-06-12 诺沃挪第克公司 不孕症的治疗
AU2794000A (en) 1999-02-24 2000-09-14 Novo Nordisk A/S Treatment of infertility
CZ20012671A3 (cs) 1999-02-26 2002-01-16 Novo Nordisk A/S Způsob in vitro oplodnění s pouľitím kultivačního média obsahujícího sterol aktivující meiosu
CA2382908A1 (en) 1999-09-16 2001-03-22 Novo Nordisk A/S Composition for ivf
WO2001062260A2 (en) 2000-02-25 2001-08-30 Schering Aktiengesellschaft Improvement of implantation rate
ATE386495T1 (de) * 2001-02-06 2008-03-15 Novo Nordisk As Behältnis mit niedrigem sauerstoffgehalt, das ff- mas enthält
US6988613B2 (en) * 2001-02-06 2006-01-24 Novo Nordisk A/S Composition for IVF

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007500140A (ja) * 2003-07-28 2007-01-11 シエーリング アクチエンゲゼルシャフト チオモルホリノステロイド化合物、減数分裂調節薬剤を製造するためのそれらの使用、およびそれらの製造方法

Also Published As

Publication number Publication date
RU2003130228A (ru) 2005-04-10
ZA200308271B (en) 2005-01-24
PL369576A1 (en) 2005-05-02
IL157272A0 (en) 2004-02-19
JP2004534011A (ja) 2004-11-11
CA2438210A1 (en) 2002-10-10
NO20034273L (no) 2003-11-25
NO20034273D0 (no) 2003-09-25
CZ20032578A3 (cs) 2003-12-17
UA75130C2 (en) 2006-03-15
CN1332975C (zh) 2007-08-22
US6916921B2 (en) 2005-07-12
EP1245572A1 (en) 2002-10-02
AU2002315260B2 (en) 2008-04-03
HUP0303643A2 (hu) 2004-03-01
WO2002079220A3 (en) 2003-10-16
CN1543473A (zh) 2004-11-03
MXPA03008199A (es) 2004-01-29
US20020188143A1 (en) 2002-12-12
KR20030088043A (ko) 2003-11-15
HK1070900A1 (en) 2005-06-30
RU2289587C2 (ru) 2006-12-20
EP1401856A2 (en) 2004-03-31
BR0208381A (pt) 2004-06-15

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