HUP0300335A2 - 8béta-hidrokarbil-szubsztituált ösztratriének mint szelektív hatású ösztrogének, alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények - Google Patents
8béta-hidrokarbil-szubsztituált ösztratriének mint szelektív hatású ösztrogének, alkalmazásuk és ezeket tartalmazó gyógyszerkészítményekInfo
- Publication number
- HUP0300335A2 HUP0300335A2 HU0300335A HUP0300335A HUP0300335A2 HU P0300335 A2 HUP0300335 A2 HU P0300335A2 HU 0300335 A HU0300335 A HU 0300335A HU P0300335 A HUP0300335 A HU P0300335A HU P0300335 A2 HUP0300335 A2 HU P0300335A2
- Authority
- HU
- Hungary
- Prior art keywords
- compounds
- betha
- hydrocarbyl
- pharmaceutical compositions
- compositions containing
- Prior art date
Links
- 150000002164 estratrienes Chemical class 0.000 title abstract 2
- 229940011871 estrogen Drugs 0.000 title 1
- 239000000262 estrogen Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 102000015694 estrogen receptors Human genes 0.000 abstract 2
- 108010038795 estrogen receptors Proteins 0.000 abstract 2
- 238000002360 preparation method Methods 0.000 abstract 2
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 abstract 1
- 125000006729 (C2-C5) alkenyl group Chemical group 0.000 abstract 1
- 108010072564 5-HT2A Serotonin Receptor Proteins 0.000 abstract 1
- 102000049773 5-HT2A Serotonin Receptor Human genes 0.000 abstract 1
- 108010078791 Carrier Proteins Proteins 0.000 abstract 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 abstract 1
- 210000000988 bone and bone Anatomy 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 abstract 1
- 238000000338 in vitro Methods 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- -1 prop-1-ynyl group Chemical group 0.000 abstract 1
- 210000002307 prostate Anatomy 0.000 abstract 1
- 230000004936 stimulating effect Effects 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
- 210000004291 uterus Anatomy 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
- C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
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- 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
-
- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- 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
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- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
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- A61P15/16—Masculine contraceptives
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0059—Estrane derivatives substituted in position 17 by a keto group
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0062—Estrane derivatives substituted in position 17 alfa not substituted in position 17 beta
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
- C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
- C07J1/0074—Esters
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- 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
- C07J41/0072—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the A ring of the steroid being aromatic
Abstract
A találmány új, (I) általános képletű 8b-szubsztituált ösztratriénekrevonatkozik, mely képletben R2, R3, R6, R6', R7, R7', R9, R11, R11',R12, R14, R15, R15', R16, R16', R17 és R17' jelentése a leírásbanmegadott és R8 egyenes vagy elágazó láncú, adott esetben részlegesenvagy teljesen halogénezett 1-5 szénatomos alkil- vagy 2-5 szénatomosalkenilcsoportot, etinil- vagy prop-l-inil-csoportot jelent. Ezek avegyületek felhasználhatók gyógyászati hatóanyagokként, amelyek invitro patkányprosztata ösztrogénreceptor-preparátumokon magasabbaffinitást mutatnak, mint patkányuterusz ösztrogénreceptor-preparátumokon és amelyek in vivo előnyösen inkább a csontokon hatnak,mint az uteruszon és/vagy kifejezett hatásuk az 5HT2a-receptor és -transzporter expressziójának stimulálását tekintve. A találmánytovábbá az új vegyületek terápiás alkalmazására és ezeket avegyületeket tartalmazó gyógyszerkészítményekre is vonatkozik. Ó
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE10019167A DE10019167A1 (de) | 2000-04-12 | 2000-04-12 | Substituierte Estratriene als selektiv wirksame Estrogene |
US20737000P | 2000-05-26 | 2000-05-26 | |
PCT/EP2001/004290 WO2001077139A1 (de) | 2000-04-12 | 2001-04-12 | 8.beta.-hydrocarbyl-substituierte estratriene als selektiv wirksame estrogene |
Publications (1)
Publication Number | Publication Date |
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HUP0300335A2 true HUP0300335A2 (hu) | 2003-07-28 |
Family
ID=26005365
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0300335A HUP0300335A2 (hu) | 2000-04-12 | 2001-04-12 | 8béta-hidrokarbil-szubsztituált ösztratriének mint szelektív hatású ösztrogének, alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények |
Country Status (26)
Country | Link |
---|---|
US (3) | US7378404B2 (hu) |
EP (2) | EP1272505B1 (hu) |
JP (2) | JP3828423B2 (hu) |
CN (1) | CN100453549C (hu) |
AT (2) | ATE363487T1 (hu) |
AU (3) | AU2001273945A1 (hu) |
BG (1) | BG107173A (hu) |
BR (1) | BR0109983A (hu) |
CA (1) | CA2406177C (hu) |
CZ (1) | CZ20023382A3 (hu) |
DE (1) | DE50112561D1 (hu) |
DK (2) | DK1272504T3 (hu) |
EA (1) | EA006299B1 (hu) |
EE (1) | EE200200589A (hu) |
ES (2) | ES2287127T3 (hu) |
HK (1) | HK1057219A1 (hu) |
HR (1) | HRP20020892B1 (hu) |
HU (1) | HUP0300335A2 (hu) |
IL (2) | IL152248A0 (hu) |
MX (1) | MXPA02010066A (hu) |
NO (2) | NO325337B1 (hu) |
NZ (1) | NZ543724A (hu) |
PL (1) | PL207488B1 (hu) |
PT (1) | PT1272504E (hu) |
SK (1) | SK14632002A3 (hu) |
WO (2) | WO2001077139A1 (hu) |
Families Citing this family (34)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DK1272504T3 (da) * | 2000-04-12 | 2007-10-01 | Bayer Schering Pharma Ag | 8.Beta-hydrocarbylsubstituerede östradiener til anvendelse som selektive östrogener |
DE10027887A1 (de) | 2000-05-31 | 2001-12-13 | Jenapharm Gmbh | Verbindungen mit einer Sulfonamidgruppe und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
DE10039199A1 (de) * | 2000-08-10 | 2002-02-21 | Schering Ag | Kombinationspräparate aus einem ERß selektiven Estrogen und einem SERM oder Antiestrogen |
GB0020498D0 (en) * | 2000-08-18 | 2000-10-11 | Sterix Ltd | Compound |
DE10151363A1 (de) * | 2001-10-17 | 2003-05-08 | Schering Ag | Somatotrope Therapie |
DE10226326A1 (de) * | 2002-06-11 | 2004-01-15 | Schering Ag | 9-alpha-substiuierte Estratriene als selektiv wirksame Estrogene |
EP1468690B1 (en) * | 2003-03-27 | 2008-10-08 | Pantarhei Bioscience B.V. | Use of estrogens for the treatment of infertility in male mammals |
DE10318896A1 (de) * | 2003-04-22 | 2004-11-25 | Schering Ag | 8beta-Vinyl-11beta-(omega-substituierte)alkyl-estra-1,3,5(10)-triene |
PT1689410E (pt) * | 2003-11-26 | 2008-08-18 | Bayer Schering Pharma Ag | Prevenção e tratamento de doenças cardíacas hipertensivas pelos estrogénios selectivos 8beta-vinil-estra-1,3,5(10)-trieno-3,17beta-diol e 17beta-fluoro-9alfa-vinil-estra-1,3,5(10)-trieno-3,16alfa-diol |
US7534780B2 (en) | 2004-05-21 | 2009-05-19 | Bayer Schering Pharma Aktiengesellschaft | Estradiol prodrugs |
DE102005057225A1 (de) * | 2005-11-29 | 2007-05-31 | Bayer Schering Pharma Ag | Prodrugs ERß-selektiver Substanzen, Verfahren zu deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
DE102005057224A1 (de) * | 2005-11-29 | 2007-05-31 | Bayer Schering Pharma Ag | Prodrugs ERß-selektiver Substanzen, Verfahren zu deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
EP2014672A1 (en) * | 2007-07-12 | 2009-01-14 | Bayer Schering Pharma Aktiengesellschaft | 8-beta-substituted estratrienes as selectively active estrogens |
CA2714340A1 (en) * | 2008-02-13 | 2009-08-20 | Bayer Schering Pharma Aktiengesellschaft | Estradiol-containing drug delivery system |
WO2009100871A2 (en) * | 2008-02-13 | 2009-08-20 | Bayer Schering Pharma Aktiengesellschaft | Drug delivery system with stabilising effect |
EP2143432A1 (en) | 2008-07-11 | 2010-01-13 | Bayer Schering Pharma AG | 9-alpha estratriene derivatives as ER-beta selective ligands for the prevention and treatment of intestinal cancer |
EP2358351A1 (en) * | 2008-11-21 | 2011-08-24 | Bayer Pharma Aktiengesellschaft | Drug delivery system |
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US20150196640A1 (en) | 2012-06-18 | 2015-07-16 | Therapeuticsmd, Inc. | Progesterone formulations having a desirable pk profile |
US20130338122A1 (en) | 2012-06-18 | 2013-12-19 | Therapeuticsmd, Inc. | Transdermal hormone replacement therapies |
US10806697B2 (en) | 2012-12-21 | 2020-10-20 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
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US9180091B2 (en) | 2012-12-21 | 2015-11-10 | Therapeuticsmd, Inc. | Soluble estradiol capsule for vaginal insertion |
US10568891B2 (en) | 2012-12-21 | 2020-02-25 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
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AR100562A1 (es) | 2014-05-22 | 2016-10-12 | Therapeuticsmd Inc | Composición farmacéutica de estradiol y progesterona para terapia de reemplazo hormonal |
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Family Cites Families (15)
Publication number | Priority date | Publication date | Assignee | Title |
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FR2743E (fr) * | 1902-01-11 | 1904-12-15 | Adolphe Ernest Pointe | Panification augmentant le rendement et la digestibilité |
JPS454059Y1 (hu) * | 1967-11-04 | 1970-02-25 | ||
JPS454060Y1 (hu) * | 1967-12-11 | 1970-02-25 | ||
US3501530A (en) * | 1968-02-27 | 1970-03-17 | American Cyanamid Co | Substituted naphthalenones,naphthalenediones and d-homo - beta - nor estra-1,3,5(10),9(11)-tetraenes |
US3681407A (en) * | 1969-06-18 | 1972-08-01 | American Cyanamid Co | 3-methoxy 8{62 -methylestra 1,3,5(10),9(11)-tetraene-17{62 -carboxylic acid lower alkyl ester and intermediates in the preparation thereof |
US3806546A (en) * | 1969-06-18 | 1974-04-23 | American Cyanamid Co | Steroid-like compounds and method of synthesis |
US3709878A (en) * | 1970-07-20 | 1973-01-09 | Sandoz Ag | 8 alpha-methyl-substituted-steroids |
US3736345A (en) * | 1971-05-18 | 1973-05-29 | American Cyanamid Co | Steroid-like compounds and method of synthesis |
US4961931A (en) * | 1982-07-29 | 1990-10-09 | Alza Corporation | Method for the management of hyperplasia |
DE4018828C2 (de) * | 1989-06-08 | 1999-05-12 | Schering Ag | Verfahren zur Herstellung C7-alpha-substituierter 8alpha- und 8ß-Estra-1,3,5(10)-triene und C8-alpha-substituierter Estra-1,3,5(10)-triene sowie neue Zwischenprodukte für dieses Verfahren |
ATE194358T1 (de) * | 1996-05-01 | 2000-07-15 | Us Gov Health & Human Serv | 21-substituierte progesteron derivate als antigestagene |
ATE222922T1 (de) * | 1998-11-20 | 2002-09-15 | Akzo Nobel Nv | Estrogenische estra-1,3,5(10)-trien verbindungen mit verschiedenen wirkungen auf estrogenrezeptor alpha und beta mit einer unverzweigten kohlenwasserstoffkette von 5-9 kohlenstoffatomen in position 11 |
DE10019167A1 (de) * | 2000-04-12 | 2001-10-18 | Schering Ag | Substituierte Estratriene als selektiv wirksame Estrogene |
DK1272504T3 (da) * | 2000-04-12 | 2007-10-01 | Bayer Schering Pharma Ag | 8.Beta-hydrocarbylsubstituerede östradiener til anvendelse som selektive östrogener |
DE10318896A1 (de) * | 2003-04-22 | 2004-11-25 | Schering Ag | 8beta-Vinyl-11beta-(omega-substituierte)alkyl-estra-1,3,5(10)-triene |
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2001
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