SK121697A3 - 17-difluoromethylene-oestratrienes, method of producing the same and pharmaceutical composition containing the same - Google Patents
17-difluoromethylene-oestratrienes, method of producing the same and pharmaceutical composition containing the same Download PDFInfo
- Publication number
- SK121697A3 SK121697A3 SK1216-97A SK121697A SK121697A3 SK 121697 A3 SK121697 A3 SK 121697A3 SK 121697 A SK121697 A SK 121697A SK 121697 A3 SK121697 A3 SK 121697A3
- Authority
- SK
- Slovakia
- Prior art keywords
- difluoromethylene
- estra
- hydrogen atom
- methyl
- trien
- Prior art date
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- BSGPCYMUVXVZHZ-DCTDBFQOSA-N (9r,10s,13s)-17-(difluoromethylidene)-13-methyl-2,3,4,5,9,10,11,12-octahydro-1h-cyclopenta[a]phenanthrene Chemical class C([C@@H]1[C@H]2CC3)CCCC1C=CC2=C1[C@@]3(C)C(=C(F)F)C=C1 BSGPCYMUVXVZHZ-DCTDBFQOSA-N 0.000 title claims abstract description 18
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- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims abstract description 13
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- 125000001424 substituent group Chemical group 0.000 claims abstract description 5
- 125000004432 carbon atom Chemical group C* 0.000 claims description 14
- -1 17-difluoromethylene-8a-estra-1,3,5 (10) -trien-3-ol 17-difluoromethylene-3-methoxy-18-methyl-estra-1,3,5 (10) -triene Chemical compound 0.000 claims description 10
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- SIPUZPBQZHNSDW-UHFFFAOYSA-N diisobutylaluminium hydride Substances CC(C)C[Al]CC(C)C SIPUZPBQZHNSDW-UHFFFAOYSA-N 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 210000002889 endothelial cell Anatomy 0.000 description 1
- WKRLQDKEXYKHJB-HFTRVMKXSA-N equilin Chemical compound OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4C3=CCC2=C1 WKRLQDKEXYKHJB-HFTRVMKXSA-N 0.000 description 1
- 150000002164 estratrienes Chemical class 0.000 description 1
- 229940011871 estrogen Drugs 0.000 description 1
- 239000000262 estrogen Substances 0.000 description 1
- 238000006266 etherification reaction Methods 0.000 description 1
- 210000002196 fr. b Anatomy 0.000 description 1
- 210000003918 fraction a Anatomy 0.000 description 1
- 208000018685 gastrointestinal system disease Diseases 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 239000007943 implant Substances 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 238000010253 intravenous injection Methods 0.000 description 1
- 150000002500 ions Chemical class 0.000 description 1
- 208000028867 ischemia Diseases 0.000 description 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 150000002576 ketones Chemical class 0.000 description 1
- 208000017169 kidney disease Diseases 0.000 description 1
- 230000003902 lesion Effects 0.000 description 1
- 150000007517 lewis acids Chemical class 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 238000004811 liquid chromatography Methods 0.000 description 1
- 229910052744 lithium Inorganic materials 0.000 description 1
- OVEHNNQXLPJPPL-UHFFFAOYSA-N lithium;n-propan-2-ylpropan-2-amine Chemical compound [Li].CC(C)NC(C)C OVEHNNQXLPJPPL-UHFFFAOYSA-N 0.000 description 1
- 239000007937 lozenge Substances 0.000 description 1
- 230000001926 lymphatic effect Effects 0.000 description 1
- 229910001425 magnesium ion Inorganic materials 0.000 description 1
- 230000008018 melting Effects 0.000 description 1
- 238000002844 melting Methods 0.000 description 1
- 230000005012 migration Effects 0.000 description 1
- 238000013508 migration Methods 0.000 description 1
- 210000003205 muscle Anatomy 0.000 description 1
- 230000003387 muscular Effects 0.000 description 1
- 208000010125 myocardial infarction Diseases 0.000 description 1
- 208000031225 myocardial ischemia Diseases 0.000 description 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 201000001119 neuropathy Diseases 0.000 description 1
- 230000007823 neuropathy Effects 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 125000001181 organosilyl group Chemical group [SiH3]* 0.000 description 1
- 108010071584 oxidized low density lipoprotein Proteins 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 208000033808 peripheral neuropathy Diseases 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 230000023603 positive regulation of transcription initiation, DNA-dependent Effects 0.000 description 1
- LPNYRYFBWFDTMA-UHFFFAOYSA-N potassium tert-butoxide Chemical compound [K+].CC(C)(C)[O-] LPNYRYFBWFDTMA-UHFFFAOYSA-N 0.000 description 1
- 238000011002 quantification Methods 0.000 description 1
- 239000013558 reference substance Substances 0.000 description 1
- 230000002040 relaxant effect Effects 0.000 description 1
- 230000004648 relaxation of smooth muscle Effects 0.000 description 1
- 230000010410 reperfusion Effects 0.000 description 1
- 206010039073 rheumatoid arthritis Diseases 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 230000007017 scission Effects 0.000 description 1
- 125000003808 silyl group Chemical group [H][Si]([H])([H])[*] 0.000 description 1
- 210000002460 smooth muscle Anatomy 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000012312 sodium hydride Substances 0.000 description 1
- 229910000104 sodium hydride Inorganic materials 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 208000010110 spontaneous platelet aggregation Diseases 0.000 description 1
- 238000013222 sprague-dawley male rat Methods 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 238000010254 subcutaneous injection Methods 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000001981 tert-butyldimethylsilyl group Chemical group [H]C([H])([H])[Si]([H])(C([H])([H])[H])[*]C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000000037 tert-butyldiphenylsilyl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1[Si]([H])([*]C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 210000005167 vascular cell Anatomy 0.000 description 1
- 229940124549 vasodilator Drugs 0.000 description 1
- 239000003071 vasodilator agent Substances 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/02—Halogenated hydrocarbons
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
- C07H15/20—Carbocyclic rings
- C07H15/203—Monocyclic carbocyclic rings other than cyclohexane rings; Bicyclic carbocyclic ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
- C07J13/007—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 17 (20)
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K9/00—Peptides having up to 20 amino acids, containing saccharide radicals and having a fully defined sequence; Derivatives thereof
- C07K9/001—Peptides having up to 20 amino acids, containing saccharide radicals and having a fully defined sequence; Derivatives thereof the peptide sequence having less than 12 amino acids and not being part of a ring structure
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biotechnology (AREA)
- Biophysics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Photoreceptors In Electrophotography (AREA)
- Exhaust-Gas Circulating Devices (AREA)
- Electrical Control Of Air Or Fuel Supplied To Internal-Combustion Engine (AREA)
- Saccharide Compounds (AREA)
- Vehicle Body Suspensions (AREA)
- Transition And Organic Metals Composition Catalysts For Addition Polymerization (AREA)
- Ceramic Products (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19509729A DE19509729A1 (de) | 1995-03-13 | 1995-03-13 | 17-Difluormethylen-Estratriene |
| PCT/EP1996/001069 WO1996028462A1 (de) | 1995-03-13 | 1996-03-13 | 17-difluormethylen-estratriene |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SK121697A3 true SK121697A3 (en) | 1998-02-04 |
Family
ID=7756963
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SK1216-97A SK121697A3 (en) | 1995-03-13 | 1996-03-13 | 17-difluoromethylene-oestratrienes, method of producing the same and pharmaceutical composition containing the same |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US6018062A (is) |
| EP (1) | EP0815120B1 (is) |
| JP (1) | JPH11501644A (is) |
| KR (1) | KR19980703002A (is) |
| AT (1) | ATE199159T1 (is) |
| AU (1) | AU693335B2 (is) |
| BR (1) | BR9612787A (is) |
| CA (1) | CA2215201A1 (is) |
| CZ (1) | CZ281097A3 (is) |
| DE (2) | DE19509729A1 (is) |
| HU (1) | HUP9801846A3 (is) |
| IL (1) | IL117497A (is) |
| IS (1) | IS4556A (is) |
| NO (1) | NO308306B1 (is) |
| PL (1) | PL322199A1 (is) |
| RU (1) | RU2155770C2 (is) |
| SI (1) | SI9620030A (is) |
| SK (1) | SK121697A3 (is) |
| TR (1) | TR199700950T1 (is) |
| WO (1) | WO1996028462A1 (is) |
| ZA (1) | ZA962037B (is) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU703814B2 (en) * | 1995-12-04 | 1999-04-01 | Wyeth | Antioxidant |
| US5773432A (en) * | 1996-10-30 | 1998-06-30 | Schering Aktiengesellschaft | Method for lowering plasma levels of lipoprotein(a) |
| CA2534497A1 (en) * | 2003-08-11 | 2005-02-17 | Industria Chimica Reggiana I.C.R. S.P.A. | Chemical composition and method of polymerisation thereof for use on vehicle bodywork repair |
| JP2008504329A (ja) * | 2004-06-29 | 2008-02-14 | ヤド テクノロジーズ ゲゼルシャフト ミット ベシュレンクテル ハフツング | 脂質ラフト内の病理プロセスに関係する障害を治療するためのステロイド由来の医薬組成物の使用 |
| US8030298B2 (en) | 2005-05-26 | 2011-10-04 | Abbott Products Gmbh | 17β-HSD1 and STS inhibitors |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3741800A1 (de) * | 1987-12-07 | 1989-06-15 | Schering Ag | 17-halogenmethylen-estratriene |
| US5783571A (en) * | 1991-01-07 | 1998-07-21 | Pherin Corporation | Method of altering hypothalamic function by nasal administration of estrene steroids |
| US5883087A (en) * | 1991-01-07 | 1999-03-16 | Pherin Corporation | Androstane steroids as neurochemical initiators of change in human hypothalamic function and related pharmaceutical compositions and methods |
| US5969168A (en) * | 1991-01-07 | 1999-10-19 | Pherin Corporation | Androstanes for inducing hypothalamic effects |
| US5773432A (en) * | 1996-10-30 | 1998-06-30 | Schering Aktiengesellschaft | Method for lowering plasma levels of lipoprotein(a) |
-
1995
- 1995-03-13 DE DE19509729A patent/DE19509729A1/de not_active Withdrawn
-
1996
- 1996-03-13 TR TR97/00950T patent/TR199700950T1/xx unknown
- 1996-03-13 SK SK1216-97A patent/SK121697A3/sk unknown
- 1996-03-13 JP JP8527276A patent/JPH11501644A/ja active Pending
- 1996-03-13 US US08/913,325 patent/US6018062A/en not_active Expired - Fee Related
- 1996-03-13 ZA ZA962037A patent/ZA962037B/xx unknown
- 1996-03-13 BR BR9612787-2A patent/BR9612787A/pt not_active Application Discontinuation
- 1996-03-13 CA CA002215201A patent/CA2215201A1/en not_active Abandoned
- 1996-03-13 PL PL96322199A patent/PL322199A1/xx unknown
- 1996-03-13 RU RU97116513/04A patent/RU2155770C2/ru active
- 1996-03-13 AU AU51078/96A patent/AU693335B2/en not_active Ceased
- 1996-03-13 AT AT96907453T patent/ATE199159T1/de not_active IP Right Cessation
- 1996-03-13 EP EP96907453A patent/EP0815120B1/de not_active Expired - Lifetime
- 1996-03-13 KR KR1019970706410A patent/KR19980703002A/ko not_active Application Discontinuation
- 1996-03-13 WO PCT/EP1996/001069 patent/WO1996028462A1/de not_active Application Discontinuation
- 1996-03-13 DE DE59606435T patent/DE59606435D1/de not_active Expired - Fee Related
- 1996-03-13 SI SI9620030A patent/SI9620030A/sl unknown
- 1996-03-13 HU HU9801846A patent/HUP9801846A3/hu unknown
- 1996-03-13 CZ CZ972810A patent/CZ281097A3/cs unknown
- 1996-03-14 IL IL11749796A patent/IL117497A/xx not_active IP Right Cessation
-
1997
- 1997-09-08 IS IS4556A patent/IS4556A/is unknown
- 1997-09-12 NO NO974206A patent/NO308306B1/no unknown
-
1999
- 1999-03-08 US US09/263,062 patent/US6136800A/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| CA2215201A1 (en) | 1996-09-19 |
| DE59606435D1 (de) | 2001-03-22 |
| SI9620030A (sl) | 1998-02-28 |
| HUP9801846A3 (en) | 1999-03-01 |
| RU2155770C2 (ru) | 2000-09-10 |
| US6136800A (en) | 2000-10-24 |
| NO974206L (no) | 1997-11-13 |
| NO974206D0 (no) | 1997-09-12 |
| CZ281097A3 (cs) | 1998-02-18 |
| AU693335B2 (en) | 1998-06-25 |
| WO1996028462A1 (de) | 1996-09-19 |
| ATE199159T1 (de) | 2001-02-15 |
| TR199700950T1 (xx) | 1998-02-21 |
| US6018062A (en) | 2000-01-25 |
| BR9612787A (pt) | 1999-11-23 |
| DE19509729A1 (de) | 1996-09-19 |
| ZA962037B (en) | 1996-09-25 |
| MX9707006A (es) | 1997-11-29 |
| PL322199A1 (en) | 1998-01-19 |
| IS4556A (is) | 1997-09-08 |
| AU5107896A (en) | 1996-10-02 |
| EP0815120A1 (de) | 1998-01-07 |
| IL117497A0 (en) | 1996-07-23 |
| JPH11501644A (ja) | 1999-02-09 |
| IL117497A (en) | 1999-12-22 |
| EP0815120B1 (de) | 2001-02-14 |
| NO308306B1 (no) | 2000-08-28 |
| HUP9801846A2 (hu) | 1998-12-28 |
| KR19980703002A (ko) | 1998-09-05 |
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