HRP20020892B1 - 8c-hydrocarbyl-substituted estratrienes for use as selective estrogens - Google Patents
8c-hydrocarbyl-substituted estratrienes for use as selective estrogensInfo
- Publication number
- HRP20020892B1 HRP20020892B1 HR20020892A HRP20020892A HRP20020892B1 HR P20020892 B1 HRP20020892 B1 HR P20020892B1 HR 20020892 A HR20020892 A HR 20020892A HR P20020892 A HRP20020892 A HR P20020892A HR P20020892 B1 HRP20020892 B1 HR P20020892B1
- Authority
- HR
- Croatia
- Prior art keywords
- radical
- hydrogen atom
- group
- additional bond
- carbon atoms
- Prior art date
Links
- 150000002164 estratrienes Chemical class 0.000 title 1
- 229940011871 estrogen Drugs 0.000 title 1
- 239000000262 estrogen Substances 0.000 title 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 14
- -1 C1-C5-alkyl radical Chemical class 0.000 abstract 9
- 125000004432 carbon atom Chemical group C* 0.000 abstract 6
- 150000003254 radicals Chemical class 0.000 abstract 5
- 125000005843 halogen group Chemical group 0.000 abstract 4
- 229920006395 saturated elastomer Polymers 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 229930195734 saturated hydrocarbon Natural products 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 229930195735 unsaturated hydrocarbon Natural products 0.000 abstract 2
- CPEONABTMRSIKA-UHFFFAOYSA-N 1,4$l^{2}-oxazinane Chemical compound C1COCC[N]1 CPEONABTMRSIKA-UHFFFAOYSA-N 0.000 abstract 1
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 abstract 1
- PQGAHNJECSVDEI-UHFFFAOYSA-N [CH2]CCCCC Chemical compound [CH2]CCCCC PQGAHNJECSVDEI-UHFFFAOYSA-N 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 abstract 1
- 150000002154 estra-1,3,5(10)-trienes Chemical class 0.000 abstract 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 abstract 1
- 125000003187 heptyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 abstract 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 abstract 1
- 125000001972 isopentyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 abstract 1
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Physical Education & Sports Medicine (AREA)
- Biomedical Technology (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Heart & Thoracic Surgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Immunology (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Gynecology & Obstetrics (AREA)
- Psychiatry (AREA)
- Vascular Medicine (AREA)
- Anesthesiology (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Toxicology (AREA)
- Pregnancy & Childbirth (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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 (fr) | 2000-04-12 | 2001-04-12 | Estratrienes a substitution 8.beta-hydrocarbyle utilises comme oestrogenes a action selective |
Publications (2)
Publication Number | Publication Date |
---|---|
HRP20020892A2 HRP20020892A2 (en) | 2005-02-28 |
HRP20020892B1 true HRP20020892B1 (en) | 2011-08-31 |
Family
ID=26005365
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HR20020892A HRP20020892B1 (en) | 2000-04-12 | 2002-11-11 | 8c-hydrocarbyl-substituted estratrienes for use as selective estrogens |
Country Status (26)
Country | Link |
---|---|
US (3) | US20040029847A1 (fr) |
EP (2) | EP1272505B1 (fr) |
JP (2) | JP3828423B2 (fr) |
CN (1) | CN100453549C (fr) |
AT (2) | ATE302790T1 (fr) |
AU (3) | AU2001273945A1 (fr) |
BG (1) | BG107173A (fr) |
BR (1) | BR0109983A (fr) |
CA (1) | CA2406177C (fr) |
CZ (1) | CZ20023382A3 (fr) |
DE (1) | DE50112561D1 (fr) |
DK (2) | DK1272505T3 (fr) |
EA (1) | EA006299B1 (fr) |
EE (1) | EE200200589A (fr) |
ES (2) | ES2287127T3 (fr) |
HK (1) | HK1057219A1 (fr) |
HR (1) | HRP20020892B1 (fr) |
HU (1) | HUP0300335A2 (fr) |
IL (2) | IL152248A0 (fr) |
MX (1) | MXPA02010066A (fr) |
NO (2) | NO325337B1 (fr) |
NZ (1) | NZ543724A (fr) |
PL (1) | PL207488B1 (fr) |
PT (1) | PT1272504E (fr) |
SK (1) | SK14632002A3 (fr) |
WO (2) | WO2001077139A1 (fr) |
Families Citing this family (34)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
HUP0300335A2 (hu) * | 2000-04-12 | 2003-07-28 | Schering Ag. | 8béta-hidrokarbil-szubsztituált ösztratriének mint szelektív hatású ösztrogének, alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények |
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 |
ES2315455T3 (es) * | 2003-03-27 | 2009-04-01 | Pantarhei Bioscience B.V. | Uso de estrogenos para el tratamiento de infertilidad en maniferos machos. |
DE10318896A1 (de) * | 2003-04-22 | 2004-11-25 | Schering Ag | 8beta-Vinyl-11beta-(omega-substituierte)alkyl-estra-1,3,5(10)-triene |
PL1689410T3 (pl) * | 2003-11-26 | 2008-10-31 | Bayer Schering Pharma Ag | Sposób zapobiegania i leczenia nadciśnieniowych chorób serca za pomocą selektywnych estrogenów: 8ß-winylo-estra-1,3,5(10)-trien-3,17ß-diolu i 17ß-fluoro-9a-winylo-estra-1,3,5(10)-trien-3,16a-diolu |
US7534780B2 (en) | 2004-05-21 | 2009-05-19 | Bayer Schering Pharma Aktiengesellschaft | Estradiol prodrugs |
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 |
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 |
EP2014672A1 (fr) * | 2007-07-12 | 2009-01-14 | Bayer Schering Pharma Aktiengesellschaft | Estratriènes 8 bêta substitués servant d'oestrogènes sélectivement actifs |
US20110097405A1 (en) * | 2008-02-13 | 2011-04-28 | Bayer Schering Pharma Aktiengesellschaft | Estradiol-containing drug delivery system |
KR20100117603A (ko) * | 2008-02-13 | 2010-11-03 | 바이엘 쉐링 파마 악티엔게젤샤프트 | 안정화 효과를 갖는 약물 전달 시스템 |
EP2143432A1 (fr) | 2008-07-11 | 2010-01-13 | Bayer Schering Pharma AG | Dérivés d'estratriènes 9-alpha en tant que ligands sélectifs ER-beta pour la prévention et le traitement du cancer intestinal |
JP2012509286A (ja) * | 2008-11-21 | 2012-04-19 | バイエル ファーマ アクチエンゲゼルシャフト | 薬物送達システム |
BR112014012444B1 (pt) | 2011-11-23 | 2021-12-14 | Therapeuticsmd, Inc | Composição farmacêutica compreendendo estradiol solubilizado, progesterona e um agente de solubilização, bem como usos desta para tratar um sintoma relacionado à menopausa em uma mulher |
US9301920B2 (en) | 2012-06-18 | 2016-04-05 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
US20150196640A1 (en) | 2012-06-18 | 2015-07-16 | Therapeuticsmd, Inc. | Progesterone formulations having a desirable pk profile |
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