FI113778B - Menetelmä farmaseuttisesti käyttökelpoisten fluorattujen 17beta-substituoitujen 4-atsa-5alfa-androstan-3-oni-johdannaisten valmistamiseksi - Google Patents
Menetelmä farmaseuttisesti käyttökelpoisten fluorattujen 17beta-substituoitujen 4-atsa-5alfa-androstan-3-oni-johdannaisten valmistamiseksi Download PDFInfo
- Publication number
- FI113778B FI113778B FI941424A FI941424A FI113778B FI 113778 B FI113778 B FI 113778B FI 941424 A FI941424 A FI 941424A FI 941424 A FI941424 A FI 941424A FI 113778 B FI113778 B FI 113778B
- Authority
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- Finland
- Prior art keywords
- aza
- oxo
- carboxamide
- hydrogen
- ene
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- 238000000034 method Methods 0.000 title claims description 34
- 238000002360 preparation method Methods 0.000 title claims description 7
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- 239000001257 hydrogen Substances 0.000 claims abstract description 72
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- 125000001153 fluoro group Chemical group F* 0.000 claims abstract description 45
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- AKHNMLFCWUSKQB-UHFFFAOYSA-L sodium thiosulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=S AKHNMLFCWUSKQB-UHFFFAOYSA-L 0.000 description 1
- 235000019345 sodium thiosulphate Nutrition 0.000 description 1
- 238000012289 standard assay Methods 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 229940032147 starch Drugs 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 239000007940 sugar coated tablet Substances 0.000 description 1
- 238000009495 sugar coating Methods 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 230000002381 testicular Effects 0.000 description 1
- 229940095585 testosterone-5-alpha reductase inhibitors for benign prostatic hypertrophy Drugs 0.000 description 1
- UGNWTBMOAKPKBL-UHFFFAOYSA-N tetrachloro-1,4-benzoquinone Chemical compound ClC1=C(Cl)C(=O)C(Cl)=C(Cl)C1=O UGNWTBMOAKPKBL-UHFFFAOYSA-N 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 125000005270 trialkylamine group Chemical group 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
- 239000003039 volatile agent Substances 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- 239000008096 xylene Substances 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
- C07J73/001—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom
- C07J73/005—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom by nitrogen as hetero atom
-
- 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
- A61P17/08—Antiseborrheics
-
- 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
- A61P35/00—Antineoplastic agents
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Dermatology (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Glass Compositions (AREA)
- Percussion Or Vibration Massage (AREA)
- Lubricants (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB9216284 | 1992-07-31 | ||
| GB929216284A GB9216284D0 (en) | 1992-07-31 | 1992-07-31 | Fluorinated 17beta-substituted 4-aza-5alpha-androstane-3-one derivatives |
| EP9302037 | 1993-07-29 | ||
| PCT/EP1993/002037 WO1994003475A1 (en) | 1992-07-31 | 1993-07-29 | FLUORINATED 17β-SUBSTITUTED 4-AZA-5α-ANDROSTAN-3-ONE DERIVATIVES |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| FI941424A0 FI941424A0 (fi) | 1994-03-28 |
| FI941424A7 FI941424A7 (fi) | 1994-05-27 |
| FI113778B true FI113778B (fi) | 2004-06-15 |
Family
ID=10719598
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| FI941424A FI113778B (fi) | 1992-07-31 | 1994-03-28 | Menetelmä farmaseuttisesti käyttökelpoisten fluorattujen 17beta-substituoitujen 4-atsa-5alfa-androstan-3-oni-johdannaisten valmistamiseksi |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US5407939A (cs) |
| EP (1) | EP0607400B1 (cs) |
| JP (1) | JP3325025B2 (cs) |
| KR (1) | KR100311547B1 (cs) |
| CN (1) | CN1041096C (cs) |
| AT (1) | ATE159951T1 (cs) |
| AU (1) | AU660562B2 (cs) |
| CA (1) | CA2120343A1 (cs) |
| CZ (1) | CZ286240B6 (cs) |
| DE (1) | DE69315050T2 (cs) |
| DK (1) | DK0607400T3 (cs) |
| ES (1) | ES2110620T3 (cs) |
| FI (1) | FI113778B (cs) |
| GB (1) | GB9216284D0 (cs) |
| GR (1) | GR3025546T3 (cs) |
| HU (2) | HUT67043A (cs) |
| IL (1) | IL106520A (cs) |
| MX (1) | MX9304579A (cs) |
| MY (1) | MY109633A (cs) |
| NO (1) | NO305401B1 (cs) |
| NZ (1) | NZ254787A (cs) |
| PH (1) | PH29938A (cs) |
| PL (1) | PL178591B1 (cs) |
| RU (1) | RU2125061C1 (cs) |
| TW (1) | TW286319B (cs) |
| UA (1) | UA41291C2 (cs) |
| WO (1) | WO1994003475A1 (cs) |
| ZA (1) | ZA935481B (cs) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE203162T1 (de) * | 1992-12-18 | 2001-08-15 | Merck & Co Inc | Verfahren zur behandlung von chronischer prostatitis mit 17-beta-n-tertbutylcarbamoyl-4- aza-5 alpha-androst-1-en-3-one |
| CA2166090C (en) * | 1993-06-24 | 2006-01-24 | Zoltan Tuba | Novel process for preparing 17.beta.-substituted 4-azaandrostane derivatives |
| TW369521B (en) * | 1993-09-17 | 1999-09-11 | Smithkline Beecham Corp | Androstenone derivative |
| RU2142956C1 (ru) * | 1993-10-21 | 1999-12-20 | Мерк Энд Ко., Инк. | 16-замещенные 4-аза-андростаны, соединения, способы ингибирования, фармацевтическая композиция |
| GB9415178D0 (en) * | 1994-07-28 | 1994-09-21 | Erba Carlo Spa | 4-azasteroids with side-chain fluoroketones |
| US5541322A (en) * | 1994-10-14 | 1996-07-30 | Glaxo Wellcome Inc. | Synthesis of 6-azaandrostenones |
| US5543417A (en) * | 1994-10-21 | 1996-08-06 | Merck & Co., Inc. | Combination method of treating acne using 4-AZA-5α-cholestan-ones and 4-AZA-5α-androstan-ones as selective 5α-reductase inhibitors with anti-bacterial, keratolytic, or anti-inflammatory agents |
| US5595996A (en) * | 1994-10-25 | 1997-01-21 | Merck & Co., Inc. | 7-substituted 4-aza cholanic acid derivatives and their use |
| IT1275594B1 (it) * | 1995-07-21 | 1997-08-06 | Pharmacia S P A Ora Pharmacia | Epimeri del (22rs)-n-(1,1,1-trifluoro-2-fenilprop-2-il)-3-osso -4-aza-5alfa-androst-1-ene-17beta-carbossammide |
| GB9518858D0 (en) * | 1995-09-14 | 1995-11-15 | Pharmacia Spa | Phenylsubstituted 4-azasteroid fluoroderivatives |
| GB9727522D0 (en) * | 1997-12-31 | 1998-02-25 | Pharmacia & Upjohn Spa | Process for preparing carboxamido-4-azasteroids |
| US6645974B2 (en) * | 2001-07-31 | 2003-11-11 | Merck & Co., Inc. | Androgen receptor modulators and methods for use thereof |
| HRP20040822A2 (en) * | 2002-03-13 | 2005-06-30 | Merck & Co. Inc. | Fluorinated 4-azasteroid derivatives as androgen receptor modulators |
| EP1660184A4 (en) | 2003-06-30 | 2008-05-14 | Merck & Co Inc | 17-ACETAMIDO-4-AZASTEROID DERIVATIVES AS MODULATORS OF THE ANDROGEN RECEPTOR |
| WO2005004807A2 (en) * | 2003-06-30 | 2005-01-20 | Merck & Co., Inc. | 17-acetamido-4-azasteroid derivatives as androgen receptor modulators |
| CN1816370A (zh) * | 2003-06-30 | 2006-08-09 | 麦克公司 | 用作雄激素受体调节剂的17－乙酰氨基－4－氮杂甾族化合物衍生物 |
| CN100528168C (zh) * | 2003-06-30 | 2009-08-19 | 麦克公司 | 作为雄激素受体调节剂的17-乙酰氨基-4-氮杂甾类衍生物 |
| WO2005025572A1 (en) * | 2003-09-10 | 2005-03-24 | Merck & Co., Inc. | 17-heterocyclic-4-azasteroid derivatives as androgen receptor modulators |
| EP1670483A4 (en) | 2003-09-10 | 2010-02-17 | Merck & Co Inc | 17-heterocyclic 4-azasteroid derivatives as androgen receptor modules |
| CA2562132A1 (en) * | 2004-04-08 | 2005-10-27 | Merck & Co., Inc. | 17 beta-acetamide-4-azasteroids as androgen receptor modulators |
| US20100105700A1 (en) * | 2008-10-28 | 2010-04-29 | Lead Therapeutics, Inc. | Decahydro-1h-indenoquinolinone and decahydro-3h-cyclopentaphenanthridinone cyp17 inhibitors |
| KR102541494B1 (ko) | 2019-09-11 | 2023-06-08 | 주식회사 엘지화학 | 고흡수성 수지의 제조 방법 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL74365A (en) * | 1984-02-27 | 1990-07-26 | Merck & Co Inc | 17beta-(n-t.-butylcarbamoyl)-4-aza-5alpha-androst-1-en-3-one and pharmaceutical compositions containing it |
| GB8505862D0 (en) * | 1985-03-07 | 1985-04-11 | Erba Farmitalia | Steroidic 5alpha-reductase inhibitors |
| GB9002922D0 (en) * | 1990-02-09 | 1990-04-04 | Erba Carlo Spa | 17 beta-substituted-4-aza-5 alpha-androstan-3-one derivatives and process for their preparation |
| IE76452B1 (en) * | 1990-10-29 | 1997-10-22 | Sankyo Co | Azasteroid compounds for the treatment of prostatic hypertrophy their preparation and use |
| US5304562A (en) * | 1991-10-09 | 1994-04-19 | Ciba-Geigy Corporation | 17β-substituted Aza-androstane derivatives |
| AUPP930799A0 (en) * | 1999-03-18 | 1999-04-15 | University Of Sydney, The | Optical planar waveguide device and method of its fabrication |
-
1992
- 1992-07-31 GB GB929216284A patent/GB9216284D0/en active Pending
-
1993
- 1993-07-28 CZ CZ19931538A patent/CZ286240B6/cs not_active IP Right Cessation
- 1993-07-29 RU RU94021145A patent/RU2125061C1/ru not_active IP Right Cessation
- 1993-07-29 KR KR1019940701034A patent/KR100311547B1/ko not_active Expired - Fee Related
- 1993-07-29 MX MX9304579A patent/MX9304579A/es not_active IP Right Cessation
- 1993-07-29 HU HU9400914A patent/HUT67043A/hu unknown
- 1993-07-29 DE DE69315050T patent/DE69315050T2/de not_active Expired - Fee Related
- 1993-07-29 AU AU47048/93A patent/AU660562B2/en not_active Ceased
- 1993-07-29 UA UA94005429A patent/UA41291C2/uk unknown
- 1993-07-29 US US08/098,729 patent/US5407939A/en not_active Expired - Fee Related
- 1993-07-29 PL PL93303048A patent/PL178591B1/pl not_active IP Right Cessation
- 1993-07-29 IL IL106520A patent/IL106520A/xx not_active IP Right Cessation
- 1993-07-29 CA CA002120343A patent/CA2120343A1/en not_active Abandoned
- 1993-07-29 ES ES93917705T patent/ES2110620T3/es not_active Expired - Lifetime
- 1993-07-29 ZA ZA935481A patent/ZA935481B/xx unknown
- 1993-07-29 CN CN93109305A patent/CN1041096C/zh not_active Expired - Fee Related
- 1993-07-29 NZ NZ254787A patent/NZ254787A/en unknown
- 1993-07-29 EP EP93917705A patent/EP0607400B1/en not_active Expired - Lifetime
- 1993-07-29 PH PH46606A patent/PH29938A/en unknown
- 1993-07-29 AT AT93917705T patent/ATE159951T1/de not_active IP Right Cessation
- 1993-07-29 MY MYPI93001489A patent/MY109633A/en unknown
- 1993-07-29 TW TW082106069A patent/TW286319B/zh active
- 1993-07-29 DK DK93917705.1T patent/DK0607400T3/da active
- 1993-07-29 WO PCT/EP1993/002037 patent/WO1994003475A1/en active IP Right Grant
- 1993-07-29 JP JP50499494A patent/JP3325025B2/ja not_active Expired - Fee Related
-
1994
- 1994-03-24 NO NO941080A patent/NO305401B1/no unknown
- 1994-03-28 FI FI941424A patent/FI113778B/fi not_active IP Right Cessation
-
1995
- 1995-06-30 HU HU95P/P00706P patent/HU211238A9/hu unknown
-
1997
- 1997-12-02 GR GR970403195T patent/GR3025546T3/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| GB | Transfer or assigment of application |
Owner name: PHARMACIA & UPJOHN S.P.A. |
|
| MA | Patent expired |