HUP0300504A2 - 19-nor-17alpha-pregna-1,3,5(10)-trien-17betha-ols of a 21,16alpha-lactone ring, process for their preparation and pharmaceutical compositions containing them - Google Patents
19-nor-17alpha-pregna-1,3,5(10)-trien-17betha-ols of a 21,16alpha-lactone ring, process for their preparation and pharmaceutical compositions containing themInfo
- Publication number
- HUP0300504A2 HUP0300504A2 HU0300504A HUP0300504A HUP0300504A2 HU P0300504 A2 HUP0300504 A2 HU P0300504A2 HU 0300504 A HU0300504 A HU 0300504A HU P0300504 A HUP0300504 A HU P0300504A HU P0300504 A2 HUP0300504 A2 HU P0300504A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- pregna
- trien
- ols
- hydroxyl
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000005843 halogen group Chemical group 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 229920006395 saturated elastomer Chemical group 0.000 abstract 3
- 229940011871 estrogen Drugs 0.000 abstract 2
- 239000000262 estrogen Substances 0.000 abstract 2
- 238000004519 manufacturing process Methods 0.000 abstract 2
- -1 methoxy, ethoxy group Chemical group 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 150000002154 estra-1,3,5(10)-trienes Chemical class 0.000 abstract 1
- 229960005309 estradiol Drugs 0.000 abstract 1
- 229930182833 estradiol Natural products 0.000 abstract 1
- 102000015694 estrogen receptors Human genes 0.000 abstract 1
- 108010038795 estrogen receptors Proteins 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 125000001893 nitrooxy group Chemical group [O-][N+](=O)O* 0.000 abstract 1
- 125000006340 pentafluoro ethyl group Chemical group FC(F)(F)C(F)(F)* 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 125000003107 substituted aryl group Chemical group 0.000 abstract 1
- 125000003396 thiol group Chemical group [H]S* 0.000 abstract 1
- 125000004417 unsaturated alkyl group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
- C07J71/0005—Oxygen-containing hetero ring
-
- 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
-
- 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
- C07J41/0094—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Diabetes (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Toxicology (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
A találmány új (II) általános képletű 21,16a-laktongyűrűs 19-nor-17a-pregna-1,3,5(10)-trién-17b-olokkal, ezek előállításával és a nevezettvegyületeket tartalmazó gyógyszerkészítményekkel, valamint a 19-nor-17a-pregna-1,3,5(10)-trién-17b-olok előállításánál köztesanyagkéntszereplő 17a-ciano-metilezett ösztra-1,3,5(10)-triénekkel foglalkozik.A 19-nor-17a-pregna-1,3,5(10)-trién-17b-olok olyan új szelektívösztrogéneket képviselnek, melyek eltérően a hagyományosösztrogénektől, például az ösztradioltól, a két ismertösztrogénreceptor közül elsősorban az a-receptorhoz kötődnek. A (II)általános képletben R1 jelentése halogénatom, hidroxil-, metil-,trifluormetil-, metoxi-, etoxicsoport; R2 jelentése hidrogén-,halogénatom, hidrozil-, vagy telített vagy telítetlen alkoxicsoort; R7jelentése halogénatom vagy telített vagy telítetlen adott esetbenfluorozott alkil-, alkoxicsoport vagy helyettesített aril- vagyheteroarilcsoport; R8 jelentése hidrogénatom, telített vagy telítetlenalkilcsoport vagy cianocsoport R9 jelentése hidrogénatom, metil-,etil-, trifluormetil- vagy pentafluor-etilcsoport; R11 jelentésenitrooxi-csoport vagy hidroxil- vagy merkaptocsoport, halogénatom,adott esetben fluorozott alkil-, alkoxi-, alkiltiocsoport; R13 és R14jelentése metil-etilcsoport vagy adott esetben fluorozottalkilcsoport; ÓThe invention with new 21,16a-lactone ring 19-nor-17a-pregna-1,3,5(10)-trien-17b-ols of general formula (II), their production and pharmaceutical preparations containing the named compounds, as well as the 19-nor- It deals with 17a-cyanomethylated estra-1,3,5(10)-trienes, which act as intermediates in the production of 17a-pregna-1,3,5(10)-trien-17b-ols. 19-nor-17a-pregna-1, 3,5(10)-trien-17b-ols represent new selective estrogens that, unlike traditional estrogens, e.g. estradiol, primarily bind to the α-receptor of the two known estrogen receptors. In the general formula (II), R1 is a halogen atom, a hydroxyl, methyl, trifluoromethyl, methoxy, ethoxy group; R2 is hydrogen, halogen, hydroxyl, or saturated or unsaturated alkoxy; R7 is a halogen atom or a saturated or unsaturated optionally fluorinated alkyl, alkoxy group or a substituted aryl or heteroaryl group; R 8 is a hydrogen atom, a saturated or unsaturated alkyl group or a cyano group R 9 is a hydrogen atom, a methyl, ethyl, trifluoromethyl or pentafluoroethyl group; R11 is a nitrooxy group or a hydroxyl or mercapto group, a halogen atom, optionally a fluorinated alkyl, alkoxy, alkylthio group; R13 and R14 mean a methylethyl group or optionally a fluorinated alkyl group; HE
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10048634A DE10048634A1 (en) | 2000-09-27 | 2000-09-27 | 19-Nor-17alpha-pregna-1,3,5 (10) -trien-17beta-ole with a 21, 16alpha lactone ring |
| PCT/EP2001/011061 WO2002026763A1 (en) | 2000-09-27 | 2001-09-25 | 19-NOR-17α-PREGNA-1,3,5 (10)-TRIEN-17β-OLS OF A 21,16α-LACTONE RING |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0300504A2 true HUP0300504A2 (en) | 2003-06-28 |
| HUP0300504A3 HUP0300504A3 (en) | 2003-12-29 |
Family
ID=7658321
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0300504A HUP0300504A3 (en) | 2000-09-27 | 2001-09-25 | 19-nor-17alpha-pregna-1,3,5(10)-trien-17betha-ols of a 21,16alpha-lactone ring, process for their preparation and pharmaceutical compositions containing them |
Country Status (7)
| Country | Link |
|---|---|
| EP (1) | EP1322662A1 (en) |
| AU (1) | AU2001293843A1 (en) |
| DE (1) | DE10048634A1 (en) |
| HU (1) | HUP0300504A3 (en) |
| IL (1) | IL151782A0 (en) |
| NO (1) | NO20025201D0 (en) |
| WO (1) | WO2002026763A1 (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10214180A1 (en) * | 2002-03-27 | 2003-10-16 | Schering Ag | 11beta-lankgettig-substituted 19-nor-17alpha-pregna-1,3,5 (10) -triene-17beta-ols with a 21,16alpha lactone ring |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3920634A (en) * | 1974-08-30 | 1975-11-18 | Lilly Co Eli | 2,3-Dihydroestra-1,3,5(10)-trieno (16{60 ,17{60 -{62 ) furan-17{62 ols |
| DE19906159A1 (en) * | 1999-02-09 | 2000-08-10 | Schering Ag | 16-hydroxyestratrienes as selectively active estrogens |
| DE19917930A1 (en) * | 1999-04-15 | 2000-10-19 | Schering Ag | Treating estrogen deficiency associated disorders, e.g. menopausal problems, osteoporosis, neoplasia or neurodegenerative disease, using new or known ent-steroids having bone-selective estrogenic activity |
| DE19954105A1 (en) * | 1999-11-02 | 2001-05-17 | Schering Ag | Treatment of estrogen deficiency-associated conditions, e.g. menopausal syndrome, osteoporosis, infertility or prostatic hypertrophy, using new or known gonatrienes having tissue-selective estrogenic activity |
-
2000
- 2000-09-27 DE DE10048634A patent/DE10048634A1/en not_active Ceased
-
2001
- 2001-09-25 IL IL15178201A patent/IL151782A0/en unknown
- 2001-09-25 EP EP01974292A patent/EP1322662A1/en not_active Withdrawn
- 2001-09-25 HU HU0300504A patent/HUP0300504A3/en unknown
- 2001-09-25 AU AU2001293843A patent/AU2001293843A1/en not_active Abandoned
- 2001-09-25 WO PCT/EP2001/011061 patent/WO2002026763A1/en not_active Application Discontinuation
-
2002
- 2002-10-30 NO NO20025201A patent/NO20025201D0/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| AU2001293843A1 (en) | 2002-04-08 |
| EP1322662A1 (en) | 2003-07-02 |
| HUP0300504A3 (en) | 2003-12-29 |
| DE10048634A1 (en) | 2002-04-18 |
| IL151782A0 (en) | 2003-04-10 |
| NO20025201L (en) | 2002-10-30 |
| WO2002026763A1 (en) | 2002-04-04 |
| NO20025201D0 (en) | 2002-10-30 |
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