DE69313018D1 - Neue 7-Beta-substituierte-4-Aza-5-Alpha-Androstan-3-Onen als Inhibitoren 5-Alpha-Reduktases - Google Patents
Neue 7-Beta-substituierte-4-Aza-5-Alpha-Androstan-3-Onen als Inhibitoren 5-Alpha-ReduktasesInfo
- Publication number
- DE69313018D1 DE69313018D1 DE69313018T DE69313018T DE69313018D1 DE 69313018 D1 DE69313018 D1 DE 69313018D1 DE 69313018 T DE69313018 T DE 69313018T DE 69313018 T DE69313018 T DE 69313018T DE 69313018 D1 DE69313018 D1 DE 69313018D1
- Authority
- DE
- Germany
- Prior art keywords
- alpha
- aza
- beta
- ones
- substituted
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- 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
- C07C59/90—Unsaturated compounds containing keto groups containing singly bound oxygen-containing groups
-
- 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
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US88657292A | 1992-05-20 | 1992-05-20 |
Publications (2)
Publication Number | Publication Date |
---|---|
DE69313018D1 true DE69313018D1 (de) | 1997-09-18 |
DE69313018T2 DE69313018T2 (de) | 1998-02-19 |
Family
ID=25389283
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DE69313018T Expired - Fee Related DE69313018T2 (de) | 1992-05-20 | 1993-05-19 | Neue 7-Beta-substituierte-4-Aza-5-Alpha-Androstan-3-Onen als Inhibitoren 5-Alpha-Reduktases |
DE69333317T Expired - Fee Related DE69333317T2 (de) | 1992-05-20 | 1993-05-19 | Neue 7-beta-substituierte 4-Aza-5-alpha-Androstan-3-onen als Inhibitoren von 5-alpha-Reduktase |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DE69333317T Expired - Fee Related DE69333317T2 (de) | 1992-05-20 | 1993-05-19 | Neue 7-beta-substituierte 4-Aza-5-alpha-Androstan-3-onen als Inhibitoren von 5-alpha-Reduktase |
Country Status (14)
Country | Link |
---|---|
US (1) | US5710275A (de) |
EP (2) | EP0778284B1 (de) |
JP (1) | JPH06100587A (de) |
CN (1) | CN1087092A (de) |
AT (2) | ATE156838T1 (de) |
CA (1) | CA2096616A1 (de) |
DE (2) | DE69313018T2 (de) |
DK (1) | DK0572166T3 (de) |
ES (2) | ES2106965T3 (de) |
GR (1) | GR3024884T3 (de) |
IL (1) | IL105715A (de) |
MX (1) | MX9302932A (de) |
WO (1) | WO1993023420A1 (de) |
ZA (1) | ZA933497B (de) |
Families Citing this family (39)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
CA2135167A1 (en) * | 1992-05-20 | 1993-11-25 | Donald W. Graham | New 17-ester, amide, and ketone derivatives of 3-oxo-4- azasteroids as 5a-reductase inhibitors |
DE69313114T2 (de) * | 1992-05-20 | 1998-03-19 | Merck & Co Inc | NEUE DELTA-17 UND DELTA-20 UNGESÄTIGTE UND GESATIGTE 17--g(b)-SUBSTITUIERTE-4-AZA-5-g(a)-ANDROSTAN-3-ON VERBINDUNGEN ALS INHIBITOREN VON 5-ALPHA-REDUCTASE |
WO1993023039A1 (en) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | Substituted 4-aza-5a-androstan-ones as 5a-reductase inhibitors |
CA2135055A1 (en) * | 1992-05-20 | 1993-11-25 | Bruce E. Witzel | 4-azasteroid 5-alpha-reductase inhibitors |
ATE183193T1 (de) * | 1992-05-20 | 1999-08-15 | Merck & Co Inc | 17-amino-substituierte 4-azasteroide als 5-alpha- reductase inhibitoren |
WO1995012398A1 (en) * | 1993-11-04 | 1995-05-11 | Merck & Co., Inc. | 7-substituted-4-aza-steroid derivatives as 5-alpha- reductase inhibitors |
US5693810A (en) * | 1992-10-06 | 1997-12-02 | Merck & Co., Inc. | 17 β-carboxanilides of 4-aza-5α-androstan-3-ones as 5α-reductase inhibitors |
JPH08504813A (ja) * | 1992-12-18 | 1996-05-28 | メルク エンド カンパニー インコーポレーテッド | 17β−N−モノ置換−カルバモイル−4−アザ−5α−アンドロスト−1−エン−3−オンを含む慢性前立腺炎の治療に有用な薬剤の製造法 |
CA2165077A1 (en) * | 1993-06-28 | 1995-01-05 | Philippe L. Durette | 4-aza-pregnane 5.alpha.-reductase isozyme 1 inhibitors |
US5438061A (en) * | 1993-07-16 | 1995-08-01 | Merck & Co., Inc. | 7-substituted-δ4-6-azasteroid derivatives as 5α-reductase inhibitors |
TW369521B (en) * | 1993-09-17 | 1999-09-11 | Smithkline Beecham Corp | Androstenone derivative |
TW408127B (en) * | 1993-09-17 | 2000-10-11 | Glaxo Inc | Androstenones |
US5525608A (en) * | 1994-04-20 | 1996-06-11 | Merck & Co., Inc. | 17b-aryl-4-aza-steroid derivatives useful as 5-alpha-reductase inhibitors |
GB9415178D0 (en) * | 1994-07-28 | 1994-09-21 | Erba Carlo Spa | 4-azasteroids with side-chain fluoroketones |
US5470976A (en) * | 1994-09-07 | 1995-11-28 | Merck & Co., Inc. | Process for the stereoselective reduction of steroid enelactams |
US5817818A (en) * | 1994-09-16 | 1998-10-06 | Glaxo Wellcome Inc. | Androstenones |
US5541322A (en) * | 1994-10-14 | 1996-07-30 | Glaxo Wellcome Inc. | Synthesis of 6-azaandrostenones |
US5656613A (en) * | 1995-01-04 | 1997-08-12 | Merck & Co., Inc. | Treatment of hyperandrogenic conditions |
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 |
US6365597B1 (en) | 1996-02-14 | 2002-04-02 | Aventis Pharmaceuticals Inc. | 4-aza steroids |
US5872126A (en) * | 1996-09-06 | 1999-02-16 | Merck & Co., Inc. | Methods and compositions for treating preterm labor |
JP2001523259A (ja) * | 1997-05-07 | 2001-11-20 | ノヴォファーム リミテッド | 4−アザ−ステロイド類 |
US5998427A (en) * | 1998-05-14 | 1999-12-07 | Glaxo Wellcome Inc. | Androstenones |
CA2472475C (en) * | 2002-01-15 | 2010-05-18 | Merck & Co., Inc. | 17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators |
US7351698B2 (en) * | 2003-05-07 | 2008-04-01 | Merck & Co., Inc. | Androgen receptor modulators and methods of use thereof |
CA2530048A1 (en) * | 2003-06-30 | 2005-01-20 | Merck & Co., Inc. | 17-acetamido-4-azasteroid derivatives as androgen receptor modulators |
US7482357B2 (en) | 2003-06-30 | 2009-01-27 | Merck & Co., Inc. | 17-acetamido-4-azasteroid derivatives as androgen receptor modulators |
WO2005009949A2 (en) * | 2003-06-30 | 2005-02-03 | Merck & Co., Inc. | 17-acetamido-4-azasteroid derivatives as androgen receptor modulators |
US7696217B2 (en) * | 2003-06-30 | 2010-04-13 | Merck Sharp & Dohme Corp. | 17-acetamido-4-azasteroid derivatives as androgen receptor modulators |
CA2537663A1 (en) | 2003-09-10 | 2005-03-24 | Merck & Co., Inc. | 17-heterocyclic-4-azasteroid derivatives as androgen receptor modulators |
AU2004272007B2 (en) * | 2003-09-10 | 2009-05-28 | Merck Sharp & Dohme Corp. | 17-heterocyclic-4-azasteroid derivatives as androgen receptor modulators |
JP2007532550A (ja) * | 2004-04-08 | 2007-11-15 | メルク エンド カムパニー インコーポレーテッド | アンドロゲン受容体モジュレーターとしての17−β−アセトアミド−4−アザステロイド |
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 |
JP5684895B2 (ja) * | 2010-04-20 | 2015-03-18 | シンジェンタ パーティシペーションズ アクチェンゲゼルシャフト | ピラゾールカルボン酸アミドの調製方法 |
CN111175410A (zh) * | 2020-02-12 | 2020-05-19 | 武汉大学 | N-甲基苯乙胺及其同位素试剂在羧基化合物检测中的应用 |
CA3223165A1 (en) * | 2021-06-16 | 2022-12-22 | Universite Laval | Novel inhibitors of 17.beta.-hsd7 and uses thereof |
Family Cites Families (26)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU527030B2 (en) * | 1978-04-13 | 1983-02-10 | Merck & Co., Inc. | 4-aza-17-substituted-5a-androstan-3-ones |
US4377584A (en) * | 1978-04-13 | 1983-03-22 | Merck & Co., Inc. | 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors |
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 |
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 (de) * | 1984-02-27 | 1991-09-18 | Merck & Co. Inc. | 17-Beta-substituierte-4-aza-5-alpha-Androstenone und ihre Anwendung als 5-Alpha-Reduktase-Inhibitoren |
NZ211145A (en) * | 1984-02-27 | 1988-10-28 | Merck & Co Inc | 4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions |
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 |
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 |
US5138063A (en) * | 1984-02-27 | 1992-08-11 | Merck & Co., Inc. | 17β-methoxycarbonyl-4-aza-androsten-1-en-3-ones |
US4888336A (en) * | 1987-01-28 | 1989-12-19 | Smithkline Beckman Corporation | Steroid 5-alpha-reductase inhibitors |
US5026882A (en) * | 1988-12-23 | 1991-06-25 | Smithkline Beecham Corporation | Phosphinic acid substituted steroids as inhibitors of steroid 5α-reductase |
US5032586A (en) * | 1989-08-24 | 1991-07-16 | Smithkline Beecham Corporation | 7-keto or hydroxy 3,5-diene steroids as inhibitors of steroid 5-alpha reductase |
US5300294A (en) * | 1990-06-27 | 1994-04-05 | Smithkline Beecham Corporation | Method of treating prostatic adenocarcinoma |
IE76452B1 (en) * | 1990-10-29 | 1997-10-22 | Sankyo Co | Azasteroid compounds for the treatment of prostatic hypertrophy their preparation and use |
CA2084799C (en) * | 1991-12-17 | 2003-01-28 | Glenn J. Gormley | Method of prevention of prostatic carcinoma with 17 beta-n-monosubstituted-carbamoyl-4-aza-5 alpha-androst-1 -en-3-ones |
US5543406A (en) * | 1991-12-20 | 1996-08-06 | Glaxo Wellcome, Inc. | Inhibitors of 5-α-testosterone reductase |
US5215894A (en) * | 1992-02-25 | 1993-06-01 | Merck & Co., Inc. | Biological process for producing 17β-N-monosubstituted carbamoyl-11-oxo-4-aza-5-α-androst-3-one testosterone-5-α reductase inhibitors |
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 |
AU668180B2 (en) * | 1992-05-20 | 1996-04-26 | Merck & Co., Inc. | 17-ethers and thioethers of 4-aza-steroids |
DE69313114T2 (de) * | 1992-05-20 | 1998-03-19 | Merck & Co Inc | NEUE DELTA-17 UND DELTA-20 UNGESÄTIGTE UND GESATIGTE 17--g(b)-SUBSTITUIERTE-4-AZA-5-g(a)-ANDROSTAN-3-ON VERBINDUNGEN ALS INHIBITOREN VON 5-ALPHA-REDUCTASE |
CA2135167A1 (en) * | 1992-05-20 | 1993-11-25 | Donald W. Graham | New 17-ester, amide, and ketone derivatives of 3-oxo-4- azasteroids as 5a-reductase inhibitors |
CZ283894A3 (en) * | 1992-05-20 | 1995-09-13 | Merck & Co Inc | 7beta-substituted 4-aza-5alpha-cholestanones, their use for the preparation of pharmaceutical preparations and pharmaceutical compositions containing thereof |
HUT71514A (en) * | 1992-05-21 | 1995-12-28 | Endorecherche Inc | Inhibitors of testosterone 5 alfa-reductase activity and pharmaceutical compositions containing the same |
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 |
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 |
-
1993
- 1993-05-14 WO PCT/US1993/004643 patent/WO1993023420A1/en active Application Filing
- 1993-05-14 US US08/341,602 patent/US5710275A/en not_active Expired - Fee Related
- 1993-05-17 IL IL105715A patent/IL105715A/xx not_active IP Right Cessation
- 1993-05-19 DE DE69313018T patent/DE69313018T2/de not_active Expired - Fee Related
- 1993-05-19 ZA ZA933497A patent/ZA933497B/xx unknown
- 1993-05-19 AT AT93303882T patent/ATE156838T1/de not_active IP Right Cessation
- 1993-05-19 DE DE69333317T patent/DE69333317T2/de not_active Expired - Fee Related
- 1993-05-19 AT AT96202933T patent/ATE255125T1/de not_active IP Right Cessation
- 1993-05-19 EP EP96202933A patent/EP0778284B1/de not_active Expired - Lifetime
- 1993-05-19 EP EP93303882A patent/EP0572166B1/de not_active Expired - Lifetime
- 1993-05-19 DK DK93303882.0T patent/DK0572166T3/da active
- 1993-05-19 MX MX9302932A patent/MX9302932A/es not_active IP Right Cessation
- 1993-05-19 CN CN93107704A patent/CN1087092A/zh active Pending
- 1993-05-19 ES ES93303882T patent/ES2106965T3/es not_active Expired - Lifetime
- 1993-05-19 ES ES96202933T patent/ES2210336T3/es not_active Expired - Lifetime
- 1993-05-19 CA CA002096616A patent/CA2096616A1/en not_active Abandoned
- 1993-05-20 JP JP5154097A patent/JPH06100587A/ja active Pending
-
1997
- 1997-09-30 GR GR970402529T patent/GR3024884T3/el unknown
Also Published As
Publication number | Publication date |
---|---|
US5710275A (en) | 1998-01-20 |
CN1087092A (zh) | 1994-05-25 |
MX9302932A (es) | 1995-01-31 |
EP0572166A1 (de) | 1993-12-01 |
EP0572166B1 (de) | 1997-08-13 |
AU3869893A (en) | 1993-11-25 |
WO1993023420A1 (en) | 1993-11-25 |
DE69333317D1 (de) | 2004-01-08 |
CA2096616A1 (en) | 1993-11-21 |
ES2210336T3 (es) | 2004-07-01 |
AU662224B2 (en) | 1995-08-24 |
IL105715A0 (en) | 1993-09-22 |
EP0778284B1 (de) | 2003-11-26 |
DK0572166T3 (da) | 1997-09-01 |
IL105715A (en) | 1997-07-13 |
ES2106965T3 (es) | 1997-11-16 |
GR3024884T3 (en) | 1998-01-30 |
ZA933497B (en) | 1993-12-14 |
DE69313018T2 (de) | 1998-02-19 |
ATE156838T1 (de) | 1997-08-15 |
ATE255125T1 (de) | 2003-12-15 |
DE69333317T2 (de) | 2004-08-19 |
EP0778284A3 (de) | 1997-08-13 |
JPH06100587A (ja) | 1994-04-12 |
EP0778284A2 (de) | 1997-06-11 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
8364 | No opposition during term of opposition | ||
8339 | Ceased/non-payment of the annual fee |