EP1957515A2 - PRODRUGS ERbeta-SELEKTIVER SUBSTANZEN, VERFAHREN ZU DEREN HERSTELLUNG UND DIESE VERBINDUNGEN ENTHALTENDE PHARMAZEUTISCHE ZUSAMMENSETZUNGEN - Google Patents
PRODRUGS ERbeta-SELEKTIVER SUBSTANZEN, VERFAHREN ZU DEREN HERSTELLUNG UND DIESE VERBINDUNGEN ENTHALTENDE PHARMAZEUTISCHE ZUSAMMENSETZUNGENInfo
- Publication number
- EP1957515A2 EP1957515A2 EP06829357A EP06829357A EP1957515A2 EP 1957515 A2 EP1957515 A2 EP 1957515A2 EP 06829357 A EP06829357 A EP 06829357A EP 06829357 A EP06829357 A EP 06829357A EP 1957515 A2 EP1957515 A2 EP 1957515A2
- Authority
- EP
- European Patent Office
- Prior art keywords
- group
- triene
- estra
- vinyl
- sulfamoylbenzoate
- 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.)
- Withdrawn
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
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- 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
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- 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
-
- 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
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
-
- 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
-
- 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
- A61P5/28—Antiandrogens
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
Definitions
- the compounds of the invention have therapeutically favorable estrogenic activities, as far as they are mediated via the ER ß, especially in the central nervous system, in the circulatory system and in the bone.
- the substances according to the invention are preferably used for oral therapy.
- the compounds according to the invention have a markedly increased oral bioavailability compared to their parent estrogens, an increased systemic, but generally reduced hepatic estrogenicity. This dissociation of desired and undesired hormonal effects simultaneously enables therapeutically more effective and more compatible drugs compared to the prior art.
- the substances according to the invention are cleaved enzymatically or hydrolytically in the body, with no steroid sulphatases (STS) being required, for example for the cleavage of estradiol-3-sulphamate.
- STS steroid sulphatases
- C 3-8 -cycloalkyl group denotes a mono- or bicyclic group which may be substituted, for example, by halogens such as fluorine, chlorine or bromine, OH, CN, such as, for example, a cyclopropyl, cyclobutyl or cyclopentyl group. , Cyclohexyl or a hydroxycyclohexyl group.
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Physical Education & Sports Medicine (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Reproductive Health (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
Claims
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP08161982A EP2039702A2 (de) | 2005-11-29 | 2006-11-27 | Prodrugs erbeta-selektiver Substanzen, Verfahren zu deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE102005057224A DE102005057224A1 (de) | 2005-11-29 | 2005-11-29 | Prodrugs ERß-selektiver Substanzen, Verfahren zu deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
PCT/EP2006/011729 WO2007062877A2 (de) | 2005-11-29 | 2006-11-27 | PRODRUGS ERβ-SELEKTIVER SUBSTANZEN, VERFAHREN ZU DEREN HERSTELLUNG UND DIESE VERBINDUNGEN ENTHALTENDE PHARMAZEUTISCHE ZUSAMMENSETZUNGEN |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP08161982A Division EP2039702A2 (de) | 2005-11-29 | 2006-11-27 | Prodrugs erbeta-selektiver Substanzen, Verfahren zu deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
Publications (1)
Publication Number | Publication Date |
---|---|
EP1957515A2 true EP1957515A2 (de) | 2008-08-20 |
Family
ID=38037824
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP06829357A Withdrawn EP1957515A2 (de) | 2005-11-29 | 2006-11-27 | PRODRUGS ERbeta-SELEKTIVER SUBSTANZEN, VERFAHREN ZU DEREN HERSTELLUNG UND DIESE VERBINDUNGEN ENTHALTENDE PHARMAZEUTISCHE ZUSAMMENSETZUNGEN |
EP08161982A Withdrawn EP2039702A2 (de) | 2005-11-29 | 2006-11-27 | Prodrugs erbeta-selektiver Substanzen, Verfahren zu deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP08161982A Withdrawn EP2039702A2 (de) | 2005-11-29 | 2006-11-27 | Prodrugs erbeta-selektiver Substanzen, Verfahren zu deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
Country Status (14)
Country | Link |
---|---|
EP (2) | EP1957515A2 (de) |
JP (1) | JP2009517427A (de) |
KR (1) | KR20080070839A (de) |
CN (1) | CN101316857A (de) |
AU (1) | AU2006319383A1 (de) |
BR (1) | BRPI0619065A2 (de) |
CA (1) | CA2629587A1 (de) |
CR (1) | CR9981A (de) |
DE (1) | DE102005057224A1 (de) |
EA (1) | EA200801352A1 (de) |
EC (1) | ECSP088481A (de) |
NO (1) | NO20082913L (de) |
WO (1) | WO2007062877A2 (de) |
ZA (1) | ZA200805656B (de) |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2143432A1 (de) | 2008-07-11 | 2010-01-13 | Bayer Schering Pharma AG | 9-Alpha-Estratrien-Derivate als ER-Beta-selektive Liganden zur Prävention und Behandlung von Darmkrebs |
CN101708338B (zh) * | 2008-12-26 | 2014-06-04 | 中国人民解放军军事医学科学院放射与辐射医学研究所 | 含甾体结构的前药及其高度分散制剂 |
Family Cites Families (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB8813353D0 (en) | 1988-06-06 | 1988-07-13 | Ici Plc | Therapeutic product |
DE19833786A1 (de) | 1998-07-18 | 2000-01-20 | Schering Ag | Benzocycloheptene, Verfahren zu ihrer Herstellung, pharmazeutische Präparate, die diese enthalten, sowie deren Verwendung zur Herstellung von Arzneimitteln |
AU2001273945A1 (en) * | 2000-04-12 | 2001-10-23 | Schering Aktiengesellschaft | 8beta-substituted-11beta-pentyl- and 11beta-hexyl-estra-1,3,5(10)-triene derivatives |
DE10027887A1 (de) * | 2000-05-31 | 2001-12-13 | Jenapharm Gmbh | Verbindungen mit einer Sulfonamidgruppe und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
DE10226326A1 (de) * | 2002-06-11 | 2004-01-15 | Schering Ag | 9-alpha-substiuierte Estratriene als selektiv wirksame Estrogene |
JP2007512279A (ja) * | 2003-11-26 | 2007-05-17 | シエーリング アクチエンゲゼルシャフト | 選択的エストロゲン8β−ビニル−エストラ−1,3,5(10)−トリエン−3,17β−ジオール、及び17β−フルオル−9α−ビニル−エストラ−1,3,5(10)−トリエン−3,16α−ジオールによる高血圧性心疾患の予防及び治療 |
DE102004025985A1 (de) * | 2004-05-21 | 2005-12-15 | Schering Ag | Estriol- und Estetrol-Prodrugs |
DE102004025966A1 (de) * | 2004-05-21 | 2005-12-15 | Schering Ag | Estradiol-Prodrugs |
DE102004025986A1 (de) * | 2004-05-21 | 2005-12-15 | Schering Ag | Steroid-Prodrugs mit androgener Wirkung |
-
2005
- 2005-11-29 DE DE102005057224A patent/DE102005057224A1/de not_active Ceased
-
2006
- 2006-11-27 CA CA002629587A patent/CA2629587A1/en not_active Abandoned
- 2006-11-27 EA EA200801352A patent/EA200801352A1/xx unknown
- 2006-11-27 WO PCT/EP2006/011729 patent/WO2007062877A2/de active Application Filing
- 2006-11-27 AU AU2006319383A patent/AU2006319383A1/en not_active Abandoned
- 2006-11-27 JP JP2008542681A patent/JP2009517427A/ja active Pending
- 2006-11-27 BR BRPI0619065-0A patent/BRPI0619065A2/pt not_active IP Right Cessation
- 2006-11-27 KR KR1020087012803A patent/KR20080070839A/ko not_active Application Discontinuation
- 2006-11-27 CN CNA2006800448628A patent/CN101316857A/zh active Pending
- 2006-11-27 EP EP06829357A patent/EP1957515A2/de not_active Withdrawn
- 2006-11-27 EP EP08161982A patent/EP2039702A2/de not_active Withdrawn
-
2008
- 2008-05-16 CR CR9981A patent/CR9981A/es not_active Application Discontinuation
- 2008-05-29 EC EC2008008481A patent/ECSP088481A/es unknown
- 2008-06-27 ZA ZA200805656A patent/ZA200805656B/xx unknown
- 2008-06-27 NO NO20082913A patent/NO20082913L/no not_active Application Discontinuation
Non-Patent Citations (1)
Title |
---|
See references of WO2007062877A2 * |
Also Published As
Publication number | Publication date |
---|---|
WO2007062877A2 (de) | 2007-06-07 |
EP2039702A2 (de) | 2009-03-25 |
CN101316857A (zh) | 2008-12-03 |
CA2629587A1 (en) | 2007-06-07 |
NO20082913L (no) | 2008-07-29 |
ZA200805656B (en) | 2009-11-25 |
BRPI0619065A2 (pt) | 2011-09-20 |
EA200801352A1 (ru) | 2008-10-30 |
DE102005057224A1 (de) | 2007-05-31 |
JP2009517427A (ja) | 2009-04-30 |
ECSP088481A (es) | 2008-06-30 |
WO2007062877A3 (de) | 2007-11-08 |
CR9981A (es) | 2008-09-22 |
AU2006319383A1 (en) | 2007-06-07 |
KR20080070839A (ko) | 2008-07-31 |
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Inventor name: WYRWA, RALF Inventor name: KOSEMUND, DIRK Inventor name: MUELLER, GERD |
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Owner name: BAYER PHARMA AKTIENGESELLSCHAFT |
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