CN102459304B - 用于女性保健的取代16,17-稠合的类固醇化合物 - Google Patents
用于女性保健的取代16,17-稠合的类固醇化合物 Download PDFInfo
- Publication number
- CN102459304B CN102459304B CN201080026013.6A CN201080026013A CN102459304B CN 102459304 B CN102459304 B CN 102459304B CN 201080026013 A CN201080026013 A CN 201080026013A CN 102459304 B CN102459304 B CN 102459304B
- Authority
- CN
- China
- Prior art keywords
- compound
- methyl
- treatment
- group
- alkyl
- 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.)
- Expired - Fee Related
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J53/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by condensation with a carbocyclic rings or by formation of an additional ring by means of a direct link between two ring carbon atoms, including carboxyclic rings fused to the cyclopenta(a)hydrophenanthrene skeleton are included in this class
- C07J53/002—Carbocyclic rings fused
-
- 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
- A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- 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
-
- 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
- A61P5/32—Antioestrogens
-
- 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
- A61P5/34—Gestagens
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Reproductive Health (AREA)
- Physical Education & Sports Medicine (AREA)
- Gynecology & Obstetrics (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
Abstract
Description
分析法 | 化合物10 | Org 41621 |
体外数据 | ||
Erα ago EC50;eff | 1.8 nM;0.63 | 0.28 nM;095 |
Erα ant IC50;anteff | 10.0 nM;0.47 | > 1,000 nM |
Erβ ago EC50;eff | > 1,000 nM | > 100 nM |
Erβ ant IC50;anteff | 8.4 nM;0.83 | 3.8 nM;0.89 |
PR-B ago EC50;eff | 3.8 nM;0.49 | > 100 nM |
PR-B ant IC50;anteff | 3.7 nM;0.55 | 20.8 nM;0.74 |
PR-A ago EC50;eff | 30.0 nM;0.46 | > 100 nM |
PR-B ant IC50;anteff | 27.0 nM;0.54 | 58.3 nM;0.85 |
分析法 | EE | 化合物10 |
体内数据 | ||
Allen-Doisy(大鼠)MAD p.o. | 0.016 mg/kg .天 | 0.15 mg/kg .天 |
AOST BMD(大鼠)MAD p.o. | 0.020 mg/kg .天 | 0.12 mg/kg .天 |
脊柱前凸(大鼠)MAD p.o. | 0.035 mg/kg .天 | 0.14 mg/kg .天 |
抑制排卵(大鼠)MAD p.o. | 0.022 mg/kg .天 | 0.10 mg/kg .天 |
Claims (9)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP09162437 | 2009-06-10 | ||
EP09162437.9 | 2009-06-10 | ||
PCT/EP2010/058042 WO2010142705A1 (en) | 2009-06-10 | 2010-06-09 | Substituted 16,17-annellated steroid compounds for use in women's healthcare |
Publications (2)
Publication Number | Publication Date |
---|---|
CN102459304A CN102459304A (zh) | 2012-05-16 |
CN102459304B true CN102459304B (zh) | 2014-11-05 |
Family
ID=42752387
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201080026013.6A Expired - Fee Related CN102459304B (zh) | 2009-06-10 | 2010-06-09 | 用于女性保健的取代16,17-稠合的类固醇化合物 |
Country Status (9)
Country | Link |
---|---|
EP (1) | EP2440567B1 (zh) |
JP (1) | JP5658748B2 (zh) |
CN (1) | CN102459304B (zh) |
AR (1) | AR077027A1 (zh) |
AU (1) | AU2010257474B2 (zh) |
CA (1) | CA2764252A1 (zh) |
ES (1) | ES2414407T3 (zh) |
TW (1) | TW201109346A (zh) |
WO (1) | WO2010142705A1 (zh) |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0869132A1 (en) * | 1997-02-21 | 1998-10-07 | Akzo Nobel N.V. | "Steroid compounds having contraceptive and anti-osteoporosis activity" |
WO2002000682A1 (en) * | 2000-06-06 | 2002-01-03 | Akzo Nobel N.V. | 16, 17-carbocyclic condensed steroid compounds having selective estrogenic activity |
EP1550447A1 (en) * | 2004-01-02 | 2005-07-06 | Schering Aktiengesellschaft | Menstrual cycle control and improvement of conception rates in females |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6670347B2 (en) * | 2000-09-27 | 2003-12-30 | Schering Ag | 19-nor-17α-pregna-1,3,5(10)-trien-17β-ols with a 21,16α-lactone ring |
-
2010
- 2010-05-27 TW TW099117011A patent/TW201109346A/zh unknown
- 2010-06-09 WO PCT/EP2010/058042 patent/WO2010142705A1/en active Application Filing
- 2010-06-09 AU AU2010257474A patent/AU2010257474B2/en not_active Ceased
- 2010-06-09 EP EP10724830A patent/EP2440567B1/en active Active
- 2010-06-09 CA CA2764252A patent/CA2764252A1/en not_active Abandoned
- 2010-06-09 AR ARP100102017A patent/AR077027A1/es unknown
- 2010-06-09 JP JP2012514456A patent/JP5658748B2/ja not_active Expired - Fee Related
- 2010-06-09 CN CN201080026013.6A patent/CN102459304B/zh not_active Expired - Fee Related
- 2010-06-09 ES ES10724830T patent/ES2414407T3/es active Active
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0869132A1 (en) * | 1997-02-21 | 1998-10-07 | Akzo Nobel N.V. | "Steroid compounds having contraceptive and anti-osteoporosis activity" |
WO2002000682A1 (en) * | 2000-06-06 | 2002-01-03 | Akzo Nobel N.V. | 16, 17-carbocyclic condensed steroid compounds having selective estrogenic activity |
EP1550447A1 (en) * | 2004-01-02 | 2005-07-06 | Schering Aktiengesellschaft | Menstrual cycle control and improvement of conception rates in females |
Also Published As
Publication number | Publication date |
---|---|
AU2010257474A1 (en) | 2012-01-12 |
AR077027A1 (es) | 2011-07-27 |
JP5658748B2 (ja) | 2015-01-28 |
WO2010142705A1 (en) | 2010-12-16 |
EP2440567A1 (en) | 2012-04-18 |
EP2440567B1 (en) | 2013-04-03 |
CN102459304A (zh) | 2012-05-16 |
AU2010257474B2 (en) | 2014-08-28 |
ES2414407T3 (es) | 2013-07-19 |
CA2764252A1 (en) | 2010-12-16 |
TW201109346A (en) | 2011-03-16 |
JP2012529466A (ja) | 2012-11-22 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
C06 | Publication | ||
PB01 | Publication | ||
C10 | Entry into substantive examination | ||
SE01 | Entry into force of request for substantive examination | ||
ASS | Succession or assignment of patent right |
Owner name: MERCK SHARP + DOHME CORP. Free format text: FORMER OWNER: ORGANON BIOSCIENCES NEDERLAND B. V. Effective date: 20130701 Owner name: MSD OUSI CO., LTD. Free format text: FORMER OWNER: ORGANON NV Effective date: 20130701 Owner name: ORGANON BIOSCIENCES NEDERLAND B. V. Free format text: FORMER OWNER: MSD OUSI CO., LTD. Effective date: 20130701 |
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C41 | Transfer of patent application or patent right or utility model | ||
TA01 | Transfer of patent application right |
Effective date of registration: 20130701 Address after: Haarlem Applicant after: MERCK SHARP & DOHME B.V. Address before: Holland Applicant before: Organic agricultural biological sciences Holland Co.,Ltd. Effective date of registration: 20130701 Address after: Holland Applicant after: Organic agricultural biological sciences Holland Co.,Ltd. Address before: Holland Applicant before: N.V. Organon Effective date of registration: 20130701 Address after: Holland Applicant after: N.V. Organon Address before: Holland Applicant before: Organon AG |
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C14 | Grant of patent or utility model | ||
GR01 | Patent grant | ||
CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20141105 Termination date: 20170609 |
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CF01 | Termination of patent right due to non-payment of annual fee |