RO112427B1 - Procedeu pentru obtinerea derivatilor de 7-beta-substitut-4-aza-5alfa-androstan-3-ona - Google Patents
Procedeu pentru obtinerea derivatilor de 7-beta-substitut-4-aza-5alfa-androstan-3-ona Download PDFInfo
- Publication number
- RO112427B1 RO112427B1 RO94-01868A RO9401868A RO112427B1 RO 112427 B1 RO112427 B1 RO 112427B1 RO 9401868 A RO9401868 A RO 9401868A RO 112427 B1 RO112427 B1 RO 112427B1
- Authority
- RO
- Romania
- Prior art keywords
- compound
- inert
- general formula
- alk
- formula
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C59/40—Unsaturated compounds
- C07C59/76—Unsaturated compounds containing keto groups
- C07C59/80—Unsaturated compounds containing keto groups containing rings other than six-membered aromatic rings
- C07C59/82—Unsaturated compounds containing keto groups containing rings other than six-membered aromatic rings the keto group being part of a ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
- C07F7/1872—Preparation; Treatments not provided for in C07F7/20
- C07F7/1892—Preparation; Treatments not provided for in C07F7/20 by reactions not provided for in C07F7/1876 - C07F7/1888
-
- 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
- C07J1/0003—Androstane derivatives
- C07J1/0018—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa
- C07J1/0022—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US07/886,049 US5237064A (en) | 1992-05-20 | 1992-05-20 | Process for producing 7β-substituted-aza-5αandrostan-3-ones |
| PCT/US1993/004443 WO1993023376A1 (en) | 1992-05-20 | 1993-05-11 | NEW PROCESS FOR PRODUCING 7β-SUBSTITUTED-4-AZA-5α-ANDROSTAN-3-ONES |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RO112427B1 true RO112427B1 (ro) | 1997-09-30 |
Family
ID=25388268
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RO94-01868A RO112427B1 (ro) | 1992-05-20 | 1993-05-11 | Procedeu pentru obtinerea derivatilor de 7-beta-substitut-4-aza-5alfa-androstan-3-ona |
Country Status (11)
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SK137994A3 (en) * | 1992-05-20 | 1995-04-12 | Merck & Co Inc | 7-beta-substituted-4-aza-5-alpha-cholestan-ons their using for production of pharmaceutical agent and pharmaceutical agent containing them |
| US5237064A (en) * | 1992-05-20 | 1993-08-17 | Merck & Co., Inc. | Process for producing 7β-substituted-aza-5αandrostan-3-ones |
| WO1993023420A1 (en) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | NEW 7β-SUBSTITUTED-4-AZA-5α-ANDROSTAN-3-ONES AS 5α-REDUCTASE INHIBITORS |
| AU4251993A (en) * | 1992-05-20 | 1993-12-13 | Merck & Co., Inc. | Substituted 4-aza-5A-androstan-ones as 5A-reductase inhibitors |
| AU698696B2 (en) * | 1992-05-20 | 1998-11-05 | Merck & Co., Inc. | 7-substituted-4-aza-steroid derivatives as 5-alpha- reductase inhibitors |
| HUT71514A (en) * | 1992-05-21 | 1995-12-28 | Endorecherche Inc | Inhibitors of testosterone 5 alfa-reductase activity and pharmaceutical compositions containing the same |
| ATE158301T1 (de) * | 1993-06-28 | 1997-10-15 | Merck & Co Inc | 4-aza-pregnan-5-alpha-reductase isozym 1 inhibitoren |
| IL111467A0 (en) * | 1993-11-12 | 1994-12-29 | Merck & Co Inc | Pharmaceutical compositions comprising 7 beta -substituted -4-aza 5 alpha -cholestan-3-ones and 5 alpha reductase 1 inhibitors |
| AU1097995A (en) * | 1993-11-18 | 1995-06-06 | Merck & Co., Inc. | Combination method for the treatment of patterned alopecia |
| US5470976A (en) * | 1994-09-07 | 1995-11-28 | Merck & Co., Inc. | Process for the stereoselective reduction of steroid enelactams |
| US5656613A (en) * | 1995-01-04 | 1997-08-12 | Merck & Co., Inc. | Treatment of hyperandrogenic conditions |
| US5585383A (en) * | 1995-05-03 | 1996-12-17 | Merck & Co., Inc. | Process for crystallizing a 4-azasteroid 5alpha-reductase inhibitor |
| JPH11513684A (ja) * | 1995-10-19 | 1999-11-24 | メルク エンド カンパニー インコーポレーテッド | 16−置換−6−アザ−ステロイド5α−レダクターゼ阻害剤 |
| US5763361A (en) * | 1995-10-23 | 1998-06-09 | Merck & Co., Inc. | 17-alkyl-7-substituted-4-aza steroid derivatives as 5-α-reductase inhibitors |
| CA2233862A1 (en) * | 1995-10-23 | 1997-05-01 | Merck & Co., Inc. | 17-alkyl-7-substituted-4-aza steroid derivatives |
| AU5791698A (en) * | 1996-12-09 | 1998-07-03 | Merck & Co., Inc. | Methods and compositions for preventing and treating bone loss |
| US5994334A (en) * | 1997-02-05 | 1999-11-30 | University Of Maryland | Androgen synthesis inhibitors |
| AU6462598A (en) * | 1997-03-17 | 1998-10-12 | Merck & Co., Inc. | Methods and compositions for treating polycystic ovary syndrome |
| US5994335A (en) * | 1997-10-17 | 1999-11-30 | The University Of Maryland, Baltimore | 17-azolyl steroids useful as androgen synthesis inhibitors |
| US6187925B1 (en) | 1997-12-23 | 2001-02-13 | Merck & Co., Inc. | Intermediates and process for the synthesis of azasteroids |
| DE60045751D1 (de) | 1999-09-30 | 2011-04-28 | Harbor Biosciences Inc | Therapeutische Behandlung androgenrezeptorbedingter Leiden |
| JP4776843B2 (ja) | 1999-10-01 | 2011-09-21 | イムノゲン インコーポレーティッド | 免疫複合体及び化学療法剤を用いる癌治療用組成物及び方法 |
| KR100503193B1 (ko) * | 2002-08-19 | 2005-07-25 | 한미약품 주식회사 | 3-옥소-4-아자-5α-안드로스탄 화합물의 선택적인 제조방법 |
| MXPA05004913A (es) * | 2002-11-06 | 2005-07-22 | Pharmacia & Upjohn Co Llc | Procedimientos para preparar esteroides sustituidos por carboxi en posicion 7. |
| CN1694896A (zh) * | 2002-11-07 | 2005-11-09 | 法马西亚和厄普乔恩公司 | 制备c-7取代的5-雄甾烯的方法 |
| WO2007004429A1 (en) * | 2005-07-06 | 2007-01-11 | Matsushita Electric Industrial Co., Ltd. | Brushless dc motor and electric device using the same |
| CN100355772C (zh) * | 2005-12-28 | 2007-12-19 | 天津大学 | 具有5α-还原酶抑制活性的甾体化合物及其制备方法 |
| US7847457B2 (en) * | 2007-05-09 | 2010-12-07 | Federal-Mogul World Wide, Inc | BLDC motor assembly |
| US20100048912A1 (en) | 2008-03-14 | 2010-02-25 | Angela Brodie | Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens, In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity |
| CN102686600A (zh) | 2009-02-05 | 2012-09-19 | 托凯药业股份有限公司 | 甾体cyp17抑制剂/抗雄激素物质的新型药物前体 |
| CN105682662A (zh) | 2013-03-14 | 2016-06-15 | 马里兰大学巴尔的摩校区 | 雄激素受体减量调节剂及其用途 |
| AU2014306698A1 (en) | 2013-08-12 | 2016-01-28 | Tokai Pharmaceuticals, Inc. | Biomarkers for treatment of neoplastic disorders using androgen-targeted therapies |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2227876A (en) * | 1937-10-16 | 1941-01-07 | Firm Of N V Organon | Steroid derivatives with nuclear substituted nitrogen |
| US3285918A (en) * | 1962-04-18 | 1966-11-15 | Norman J Doorenbos | 1', 4', 5', 6'-tetrahydropyrimidino[a-4, 3]-4-aza-5-cholestene |
| US3239417A (en) * | 1962-12-07 | 1966-03-08 | Smith Kline French Lab | Methods and compositions for inhibiting sterol biosynthesis |
| US3264301A (en) * | 1963-08-22 | 1966-08-02 | Norman J Doorenbos | Substituted-4-azasteroids |
| FR1465544A (fr) * | 1965-11-29 | 1967-01-13 | Roussel Uclaf | Dérivés stéroïdes aromatiques substitués par un atome d'azote endocyclique et procédé de préparation |
| CA970692A (en) * | 1971-11-08 | 1975-07-08 | Walter Voigt | METHODS OF INHIBITING THE ACTIVITY OF TESTOSTERONE 5.alpha.-REDUCTASE |
| US4139619A (en) * | 1976-05-24 | 1979-02-13 | The Upjohn Company | 6-Amino-4-(substituted amino)-1,2-dihydro-1-hydroxy-2-iminopyrimidine, topical compositions and process for hair growth |
| US4596812A (en) * | 1976-05-24 | 1986-06-24 | The Upjohn Company | Methods and solutions for treating male pattern alopecia |
| US4377584A (en) * | 1978-04-13 | 1983-03-22 | Merck & Co., Inc. | 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors |
| AU527030B2 (en) * | 1978-04-13 | 1983-02-10 | Merck & Co., Inc. | 4-aza-17-substituted-5a-androstan-3-ones |
| US4220775A (en) * | 1979-03-15 | 1980-09-02 | Merck & Co., Inc. | Preparation of 4-aza-17-substituted-5α-androstan-3-ones useful as 5α-reductase inhibitors |
| US4317817A (en) * | 1979-08-27 | 1982-03-02 | Richardson-Merrell Inc. | Novel steroid 5α-reductase inhibitors |
| NZ211145A (en) * | 1984-02-27 | 1988-10-28 | Merck & Co Inc | 4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions |
| US4859681A (en) * | 1984-02-27 | 1989-08-22 | Merck & Co., Inc. | 17 α-Acyl-4-aza-5a-androst-1-en-3-ones as 5 alpha-reductase inhibitors |
| EP0314199B1 (en) * | 1984-02-27 | 1991-09-18 | Merck & Co. Inc. | 17 beta-substituted-4-aza-5 alpha-androstenones and their use as 5 alpha-reductase inhibitors |
| US4760071A (en) * | 1984-02-27 | 1988-07-26 | Merck & Co., Inc. | 17β-N-monosubstituted carbamoyl-4-aza-5α-androst-1-en-3-ones which are active as testosterone 5α-reductase inhibitors |
| US5049562A (en) * | 1984-02-27 | 1991-09-17 | Merck & Co., Inc. | 17β-acyl-4-aza-5α-androst-1-ene-3-ones as 5α-reductase inhibitors |
| GB8505862D0 (en) * | 1985-03-07 | 1985-04-11 | Erba Farmitalia | Steroidic 5alpha-reductase inhibitors |
| US4845104A (en) * | 1986-11-20 | 1989-07-04 | Merck & Co., Inc. | Oxidized analogs of 17β-N-monosubstituted-carbamoyl-4-aza-5-α-androstan-3-ones |
| US5237065A (en) * | 1987-01-28 | 1993-08-17 | Smithkline Beecham Corporation | Steroid 5-alpha-reductase inhibitors |
| US4888336A (en) * | 1987-01-28 | 1989-12-19 | Smithkline Beckman Corporation | Steroid 5-alpha-reductase inhibitors |
| US4910226A (en) * | 1987-04-29 | 1990-03-20 | Smithkline Beckman Corporation | Steroid 5-alpha-reductase inhibitors |
| CA1331457C (en) * | 1988-05-25 | 1994-08-16 | Dennis Alan Holt | Aromatic steroid 5--reductase inhibitors |
| US4882319A (en) * | 1988-12-23 | 1989-11-21 | Smithkline Beckman Corporation | Phosphonic acid substituted aromatic steroids as inhibitors of steroid 5-α-reductase |
| US4937237A (en) * | 1988-12-23 | 1990-06-26 | Smithkline Beckman Corporation | Phosphinic acid substituted aromatic steroids as inhibitors of steroid 5-60 -reductase |
| US4970205A (en) * | 1988-12-23 | 1990-11-13 | Smithkline Beecham Corporation | Sulfonic acid substituted aromatic steroids as inhibitors of steroid 5-α-reductase |
| US5026882A (en) * | 1988-12-23 | 1991-06-25 | Smithkline Beecham Corporation | Phosphinic acid substituted steroids as inhibitors of steroid 5α-reductase |
| 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 |
| US5237064A (en) * | 1992-05-20 | 1993-08-17 | Merck & Co., Inc. | Process for producing 7β-substituted-aza-5αandrostan-3-ones |
| WO1993023420A1 (en) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | NEW 7β-SUBSTITUTED-4-AZA-5α-ANDROSTAN-3-ONES AS 5α-REDUCTASE INHIBITORS |
| US5278159A (en) * | 1992-10-06 | 1994-01-11 | Merck & Co., Inc. | Aryl ester derivatives of 3-oxo-4-aza-androstane 17-β-carboxylates as 5-α-reductase inhibitors |
-
1992
- 1992-05-20 US US07/886,049 patent/US5237064A/en not_active Expired - Fee Related
-
1993
- 1993-05-11 CZ CZ942837A patent/CZ283794A3/cs unknown
- 1993-05-11 SK SK1378-94A patent/SK137894A3/sk unknown
- 1993-05-11 RU RU94046041A patent/RU2114117C1/ru active
- 1993-05-11 AU AU42439/93A patent/AU4243993A/en not_active Abandoned
- 1993-05-11 FI FI945441A patent/FI945441A0/fi not_active Application Discontinuation
- 1993-05-11 US US08/335,791 patent/US5578726A/en not_active Expired - Fee Related
- 1993-05-11 HU HU9403313A patent/HUT68232A/hu unknown
- 1993-05-11 WO PCT/US1993/004443 patent/WO1993023376A1/en not_active Application Discontinuation
- 1993-05-11 RO RO94-01868A patent/RO112427B1/ro unknown
- 1993-05-15 TW TW082103833A patent/TW234129B/zh active
- 1993-05-19 CN CN93107228A patent/CN1084519A/zh active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| SK137894A3 (en) | 1995-05-10 |
| FI945441A7 (fi) | 1994-11-18 |
| US5578726A (en) | 1996-11-26 |
| WO1993023376A1 (en) | 1993-11-25 |
| CZ283794A3 (en) | 1995-10-18 |
| TW234129B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) | 1994-11-11 |
| RU2114117C1 (ru) | 1998-06-27 |
| CN1084519A (zh) | 1994-03-30 |
| FI945441L (fi) | 1994-11-18 |
| US5237064A (en) | 1993-08-17 |
| HUT68232A (en) | 1995-06-28 |
| AU4243993A (en) | 1993-12-13 |
| RU94046041A (ru) | 1996-10-10 |
| FI945441A0 (fi) | 1994-11-18 |
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