AU657579B2 - Novel 17beta-substituted aza-androstane derivatives - Google Patents
Novel 17beta-substituted aza-androstane derivatives Download PDFInfo
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- AU657579B2 AU657579B2 AU26261/92A AU2626192A AU657579B2 AU 657579 B2 AU657579 B2 AU 657579B2 AU 26261/92 A AU26261/92 A AU 26261/92A AU 2626192 A AU2626192 A AU 2626192A AU 657579 B2 AU657579 B2 AU 657579B2
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- 239000001257 hydrogen Substances 0.000 claims abstract description 24
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract description 24
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract description 19
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims abstract description 12
- 241001465754 Metazoa Species 0.000 claims abstract description 8
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims abstract description 7
- 239000003112 inhibitor Substances 0.000 claims abstract description 4
- 230000001225 therapeutic effect Effects 0.000 claims abstract description 4
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims abstract 3
- 238000000034 method Methods 0.000 claims description 37
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- 125000002947 alkylene group Chemical group 0.000 claims description 10
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- 238000002360 preparation method Methods 0.000 claims description 9
- 239000003814 drug Substances 0.000 claims description 7
- 229910052736 halogen Inorganic materials 0.000 claims description 7
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Classifications
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- 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
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CH297891 | 1991-10-09 | ||
| CH2978/91 | 1991-10-09 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2626192A AU2626192A (en) | 1993-04-22 |
| AU657579B2 true AU657579B2 (en) | 1995-03-16 |
Family
ID=4245915
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU26261/92A Ceased AU657579B2 (en) | 1991-10-09 | 1992-10-07 | Novel 17beta-substituted aza-androstane derivatives |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US5304562A (enExample) |
| EP (1) | EP0538192B1 (enExample) |
| JP (1) | JPH05213989A (enExample) |
| KR (1) | KR930007969A (enExample) |
| AT (1) | ATE152121T1 (enExample) |
| AU (1) | AU657579B2 (enExample) |
| CA (1) | CA2080054A1 (enExample) |
| DE (1) | DE59208383D1 (enExample) |
| DK (1) | DK0538192T3 (enExample) |
| ES (1) | ES2101073T3 (enExample) |
| FI (1) | FI924529A7 (enExample) |
| GR (1) | GR3024013T3 (enExample) |
| HU (1) | HUT62600A (enExample) |
| IL (1) | IL103361A (enExample) |
| MX (1) | MX9205792A (enExample) |
| NO (1) | NO923911L (enExample) |
| NZ (1) | NZ244640A (enExample) |
| TW (1) | TW263513B (enExample) |
| ZA (1) | ZA927747B (enExample) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5304562A (en) * | 1991-10-09 | 1994-04-19 | Ciba-Geigy Corporation | 17β-substituted Aza-androstane derivatives |
| WO1993023039A1 (en) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | Substituted 4-aza-5a-androstan-ones as 5a-reductase inhibitors |
| 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 |
| GB9210880D0 (en) * | 1992-05-21 | 1992-07-08 | Smithkline Beecham Corp | Compounds |
| GB9216284D0 (en) * | 1992-07-31 | 1992-09-16 | Erba Carlo Spa | Fluorinated 17beta-substituted 4-aza-5alpha-androstane-3-one derivatives |
| HU212459B (en) * | 1992-10-02 | 1996-06-28 | Richter Gedeon Vegyeszet | Process for producing new 17-beta-substituted 4-aza-androstane-derivatives and pharmaceutical compositions containing them |
| DE69329933T2 (de) * | 1992-10-06 | 2001-07-19 | Merck & Co., Inc. | 17-beta-carboxanilid derivate von 4-aza-5-alpha-androstan-3-one als 5-alpha-reduktase-hemmende arzneimittel |
| TW369521B (en) * | 1993-09-17 | 1999-09-11 | Smithkline Beecham Corp | Androstenone derivative |
| TW408127B (en) * | 1993-09-17 | 2000-10-11 | Glaxo Inc | Androstenones |
| US5470976A (en) * | 1994-09-07 | 1995-11-28 | Merck & Co., Inc. | Process for the stereoselective reduction of steroid enelactams |
| 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 |
| US5656613A (en) * | 1995-01-04 | 1997-08-12 | Merck & Co., Inc. | Treatment of hyperandrogenic conditions |
| USRE39056E1 (en) * | 1995-09-15 | 2006-04-04 | Merck & Co, Inc. | 4-Azasteroids for treatment of hyperandrogenic conditions |
| EP0859761A4 (en) * | 1995-09-15 | 2000-01-26 | Merck & Co Inc | 4-AZASTEROIDS FOR TREATING HYPERANDROGEN STATES |
| US5998427A (en) * | 1998-05-14 | 1999-12-07 | Glaxo Wellcome Inc. | Androstenones |
| US6645974B2 (en) | 2001-07-31 | 2003-11-11 | Merck & Co., Inc. | Androgen receptor modulators and methods for use thereof |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4377584A (en) * | 1978-04-13 | 1983-03-22 | Merck & Co., Inc. | 4-Aza-17β-substituted-5α-androstan-3-one-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 |
| NZ211145A (en) * | 1984-02-27 | 1988-10-28 | Merck & Co Inc | 4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions |
| 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 |
| DE3780778T2 (de) * | 1986-11-20 | 1993-01-14 | Merck & Co Inc | Topisches arzneimittel enthaltend 17-beta-methoxy-carbonyl-4-methyl-4-aza-5-alpha-androst-1-en-3-one. |
| US4888336A (en) * | 1987-01-28 | 1989-12-19 | Smithkline Beckman Corporation | Steroid 5-alpha-reductase inhibitors |
| DE3888378T2 (de) * | 1987-04-03 | 1994-09-29 | Merck & Co Inc | Behandlung von Prostatacarcinoma mit 17-beta-n-monosubstituierten-Carbamoyl-4-aza-5-alpha-Androst-1-en-3-onen. |
| US5237061A (en) * | 1988-10-31 | 1993-08-17 | Merck & Co., Inc. | Methods of synthesizing benign prostatic hypertropic agents and their intermediates |
| ES2121570T3 (es) * | 1989-07-07 | 1998-12-01 | Endorecherche Inc | Derivados de androgenos para uso en la inhibicion de la actividad de los esteroides sexuales. |
| CA2023157A1 (en) * | 1989-08-21 | 1991-02-22 | Gary H. Rasmusson | 17 beta-acyl-4-aza-5 alpha-androst-1-ene-3-ones as 5 alpha-reductase inhibitors |
| US5120847A (en) * | 1990-08-27 | 1992-06-09 | Merck & Co., Inc. | Process for iodinating or brominating the α-methylenic carbon of a secondary amide |
| 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 |
-
1992
- 1992-09-30 US US07/954,081 patent/US5304562A/en not_active Expired - Fee Related
- 1992-10-05 IL IL103361A patent/IL103361A/xx not_active IP Right Cessation
- 1992-10-07 CA CA002080054A patent/CA2080054A1/en not_active Abandoned
- 1992-10-07 FI FI924529A patent/FI924529A7/fi not_active Application Discontinuation
- 1992-10-07 NZ NZ244640A patent/NZ244640A/en unknown
- 1992-10-07 AU AU26261/92A patent/AU657579B2/en not_active Ceased
- 1992-10-08 TW TW081108002A patent/TW263513B/zh active
- 1992-10-08 DE DE59208383T patent/DE59208383D1/de not_active Expired - Fee Related
- 1992-10-08 EP EP92810766A patent/EP0538192B1/de not_active Expired - Lifetime
- 1992-10-08 ES ES92810766T patent/ES2101073T3/es not_active Expired - Lifetime
- 1992-10-08 ZA ZA927747A patent/ZA927747B/xx unknown
- 1992-10-08 HU HU9203189A patent/HUT62600A/hu unknown
- 1992-10-08 MX MX9205792A patent/MX9205792A/es unknown
- 1992-10-08 DK DK92810766.3T patent/DK0538192T3/da active
- 1992-10-08 AT AT92810766T patent/ATE152121T1/de not_active IP Right Cessation
- 1992-10-08 KR KR1019920018464A patent/KR930007969A/ko not_active Abandoned
- 1992-10-08 NO NO92923911A patent/NO923911L/no unknown
- 1992-10-09 JP JP4271226A patent/JPH05213989A/ja active Pending
-
1993
- 1993-10-06 US US08/132,399 patent/US5378710A/en not_active Expired - Fee Related
-
1997
- 1997-07-08 GR GR970401668T patent/GR3024013T3/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2080054A1 (en) | 1993-04-10 |
| AU2626192A (en) | 1993-04-22 |
| IL103361A (en) | 1997-06-10 |
| ATE152121T1 (de) | 1997-05-15 |
| ES2101073T3 (es) | 1997-07-01 |
| EP0538192B1 (de) | 1997-04-23 |
| TW263513B (enExample) | 1995-11-21 |
| ZA927747B (en) | 1993-04-13 |
| FI924529A0 (fi) | 1992-10-07 |
| EP0538192A1 (de) | 1993-04-21 |
| JPH05213989A (ja) | 1993-08-24 |
| HU9203189D0 (en) | 1992-12-28 |
| US5378710A (en) | 1995-01-03 |
| KR930007969A (ko) | 1993-05-20 |
| MX9205792A (es) | 1993-08-01 |
| IL103361A0 (en) | 1993-03-15 |
| GR3024013T3 (en) | 1997-10-31 |
| NO923911D0 (no) | 1992-10-08 |
| NZ244640A (en) | 1994-12-22 |
| DE59208383D1 (de) | 1997-05-28 |
| FI924529A7 (fi) | 1993-04-10 |
| DK0538192T3 (da) | 1997-05-20 |
| US5304562A (en) | 1994-04-19 |
| NO923911L (no) | 1993-04-13 |
| HUT62600A (en) | 1993-05-28 |
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