ES2080297T3 - Derivados 17-g(b)-sustituido-4-aza-5g(a)-androstan-3-ona y procedimiento de preparacion de estos. - Google Patents
Derivados 17-g(b)-sustituido-4-aza-5g(a)-androstan-3-ona y procedimiento de preparacion de estos.Info
- Publication number
- ES2080297T3 ES2080297T3 ES91903236T ES91903236T ES2080297T3 ES 2080297 T3 ES2080297 T3 ES 2080297T3 ES 91903236 T ES91903236 T ES 91903236T ES 91903236 T ES91903236 T ES 91903236T ES 2080297 T3 ES2080297 T3 ES 2080297T3
- Authority
- ES
- Spain
- Prior art keywords
- androstan
- ona
- aza
- derivatives
- 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 - Lifetime
Links
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
-
- 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
- A61P35/00—Antineoplastic agents
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
LA PRESENTE INVENCION SE REFIERE A INHIBIDORES DE 5ALFA-REDUCTASA ESTERODICA QUE TIENEN LA FORMULA (I) DONDE R SUB 1 ES HIDROGENO, UN GRUPO ALQUILO C SUB 1 C SUB 1 UFRE; W ES UN GRUPO (2) DONDE R SUB 2 Y R SUB 3 SE ELIGEN INDEPENDIENTEMENTE ENTRE EL GRUPO FORMADO POR HIDROGENO, ALQUILO C SUB 1 QUILO C SUB 6 ALQUILO, CICLOALQUILO, CICLOALQUILALQUILO Y ARILO PUEDE ESTAR NO-SUSTITUIDO O SUSTITUIDO POR UN SUSTITUTO -OR SUB 4 DONDE R SUB 4 ES HIDROGENO O ALQUILO C SUB 1 ICLOALQUILALQUILO C SUB 6 OS ALQUILO, CICLOALQUILO Y CICLOALQUILALQUILO, PUEDE ESTAR SUSTITUIDO O NO POR UN SUSTITUTO ELEGIDO ENTRE: A) -OR SUB 4 DONDE R SUB 4 ES COMO SE HA DEFINIDO ANTERIORMENTE, Y B) (3) DONDE BIEN R SUB 5 Y R SUB 6 SE ELIGEN INDEPENDIENTEMENTE ENTRE EL GRUPO FORMADO POR HIDROGENO, ALQUILO C SUB 1 QUILO C SUB 1 LO HETEROMONOCICLICO SATURADO PENTALOMICO O HEXATOMICO, CONTENIENDO OPCIONALMENTE AL MENOS UN HETEROATOMO ADICIONAL ELEGIDO ENTRE OXIGENO Y NITROGENO; Y EL SIMBOLO (----) REPRESENTA UN ENLACE SENCILLO ODOBLE, Y SUS SALES FARMACEUTICAMENTE ACEPTABLES. EN VISTA DE SU ACTIVIDAD INHIBIDORA DE 5ALFA-REDUCTASA, LOS COMPUESTOS DE LA INVENCION PUEDEN SER UTILES PARA EL TRATAMIENTO DE CONDICIONES DEPENDIENTES DE ANDROGENOS.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB909002922A GB9002922D0 (en) | 1990-02-09 | 1990-02-09 | 17 beta-substituted-4-aza-5 alpha-androstan-3-one derivatives and process for their preparation |
Publications (1)
Publication Number | Publication Date |
---|---|
ES2080297T3 true ES2080297T3 (es) | 1996-02-01 |
Family
ID=10670693
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES91903236T Expired - Lifetime ES2080297T3 (es) | 1990-02-09 | 1991-02-06 | Derivados 17-g(b)-sustituido-4-aza-5g(a)-androstan-3-ona y procedimiento de preparacion de estos. |
Country Status (26)
Country | Link |
---|---|
US (1) | US5155107A (es) |
EP (1) | EP0468012B1 (es) |
JP (1) | JPH04505462A (es) |
KR (1) | KR920701234A (es) |
CN (1) | CN1054771A (es) |
AT (1) | ATE128143T1 (es) |
AU (1) | AU642215B2 (es) |
CA (1) | CA2049318A1 (es) |
CZ (1) | CZ279484B6 (es) |
DE (1) | DE69113155T2 (es) |
DK (1) | DK0468012T3 (es) |
ES (1) | ES2080297T3 (es) |
FI (1) | FI914723A0 (es) |
GB (1) | GB9002922D0 (es) |
GR (1) | GR3017996T3 (es) |
HR (1) | HRP921221A2 (es) |
HU (1) | HUT59158A (es) |
IE (1) | IE910408A1 (es) |
IL (1) | IL97025A (es) |
MY (1) | MY105402A (es) |
NO (1) | NO913923L (es) |
NZ (1) | NZ237023A (es) |
PT (1) | PT96699A (es) |
RU (1) | RU2088589C1 (es) |
WO (1) | WO1991012261A1 (es) |
ZA (1) | ZA91918B (es) |
Families Citing this family (34)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB9115676D0 (en) * | 1991-07-19 | 1991-09-04 | Erba Carlo Spa | Process for the preparation of 17 beta substituted-4-aza-5 alpha-androstan-3-one derivatives |
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 |
ES2118222T3 (es) * | 1991-12-20 | 1998-09-16 | Glaxo Wellcome Inc | Inhibidores de 5-alfa-testosterona reductasa. |
EP0641204B1 (en) * | 1992-05-20 | 2000-08-16 | Merck & Co. Inc. | 17-ethers and thioethers of 4-aza-steroids |
WO1993023419A1 (en) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | NEW 7β-SUBSTITUTED-4-AZA-5α-CHOLESTAN-ONES AS 5α-REDUCTASE INHIBITORS |
WO1993023048A1 (en) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | 4-azasteroid 5-alpha-reductase inhibitors |
WO1993023038A1 (en) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | 17-AMINO SUBSTITUTED 4-AZASTEROID 5α-REDUCTASE INHIBITORS |
EP0649306B1 (en) * | 1992-05-20 | 2001-01-10 | Merck & Co. Inc. | Ester derivatives of 4-aza-steroids |
US5237064A (en) * | 1992-05-20 | 1993-08-17 | Merck & Co., Inc. | Process for producing 7β-substituted-aza-5αandrostan-3-ones |
UA35589C2 (uk) * | 1992-05-21 | 2001-04-16 | Андорешерш Інк. | ІНГІБІТОРИ ТЕСТОСТЕРОН 5-<font face="Symbol">a</font>-РЕДУКТАЗИ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ ТА СПОСІБ ІНГІБУВАННЯ АКТИВНОСТІ ТЕСТОСТЕРОН 5-<font face="Symbol">a</font>-РЕДУКТАЗИ |
GB9216284D0 (en) * | 1992-07-31 | 1992-09-16 | Erba Carlo Spa | Fluorinated 17beta-substituted 4-aza-5alpha-androstane-3-one derivatives |
GB9216329D0 (en) * | 1992-07-31 | 1992-09-16 | Erba Carlo Spa | 17beta-substituted 4-aza-5alpha-androstan-3-one derivatives |
GB9216280D0 (en) * | 1992-07-31 | 1992-09-16 | Erba Carlo Spa | Steroids with a fluorinated acylureidic type side chain |
US5302589A (en) * | 1992-08-07 | 1994-04-12 | Glaxo, Inc. | Heterocyclic inhibitors of 5-α-testosterone reductase |
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 |
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 |
US5359071A (en) * | 1993-03-12 | 1994-10-25 | Merck & Co., Inc. | 15-substituted 4-azasteroids |
AU6413594A (en) * | 1993-03-24 | 1994-10-11 | Merck & Co., Inc. | Substituted 3-phenanthridinone derivatives as 5alpha-reductase inhibitors |
WO1995000147A1 (en) * | 1993-06-28 | 1995-01-05 | Merck & Co., Inc. | 4-AZA-PREGNANE 5α-REDUCTASE ISOZYME 1 INHIBITORS |
TW369521B (en) * | 1993-09-17 | 1999-09-11 | Smithkline Beecham Corp | Androstenone derivative |
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 |
CN1072679C (zh) * | 1995-07-30 | 2001-10-10 | 重庆医科大学 | 一种氮杂甾体化合物、制备及其用途 |
GB9518858D0 (en) * | 1995-09-14 | 1995-11-15 | Pharmacia Spa | Phenylsubstituted 4-azasteroid fluoroderivatives |
CA2231434A1 (en) * | 1995-09-27 | 1997-04-03 | Glenn J. Gormley | Method of preventing androgenetic alopecia with 5-.alpha. reductase inhibitors |
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 |
CA2472475C (en) * | 2002-01-15 | 2010-05-18 | Merck & Co., Inc. | 17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators |
KR100503193B1 (ko) * | 2002-08-19 | 2005-07-25 | 한미약품 주식회사 | 3-옥소-4-아자-5α-안드로스탄 화합물의 선택적인 제조방법 |
EP1663199B1 (en) * | 2003-09-25 | 2013-04-03 | Tel Aviv University Future Technology Development L.P. | Compositions and methods using same for treating amyloid-associated diseases |
WO2005092341A1 (en) * | 2004-03-22 | 2005-10-06 | Ranbaxy Laboratories Limited | Combination therapy for lower urinary tract symptoms |
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 |
WO2023070071A2 (en) * | 2021-10-21 | 2023-04-27 | The Board Of Trustees Of The University Of Illinois | Small molecule activators of the immune system |
Family Cites Families (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA970692A (en) * | 1971-11-08 | 1975-07-08 | Walter Voigt | METHODS OF INHIBITING THE ACTIVITY OF TESTOSTERONE 5.alpha.-REDUCTASE |
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 |
US4220778A (en) * | 1978-10-30 | 1980-09-02 | G. D. Searle & Co. | 8-Aryl-1,2,3,4-tetrahydroisoquinoline and derivatives thereof |
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 |
US4396615A (en) * | 1981-06-24 | 1983-08-02 | Duke University | Method of treating androgen-related disorders |
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 |
NZ225100A (en) * | 1987-06-29 | 1991-09-25 | Merck & Co Inc | Reaction of steroids (including 4-azasteroids) with a silylating agent in the presence of a quinone to introduce a delta' double bond and silylated intermediates |
-
1990
- 1990-02-09 GB GB909002922A patent/GB9002922D0/en active Pending
-
1991
- 1991-01-24 IL IL9702591A patent/IL97025A/en not_active IP Right Cessation
- 1991-02-05 NZ NZ237023A patent/NZ237023A/xx unknown
- 1991-02-05 US US07/650,970 patent/US5155107A/en not_active Expired - Fee Related
- 1991-02-05 CZ CS91274A patent/CZ279484B6/cs unknown
- 1991-02-06 DK DK91903236.7T patent/DK0468012T3/da active
- 1991-02-06 EP EP91903236A patent/EP0468012B1/en not_active Expired - Lifetime
- 1991-02-06 ES ES91903236T patent/ES2080297T3/es not_active Expired - Lifetime
- 1991-02-06 JP JP3503895A patent/JPH04505462A/ja active Pending
- 1991-02-06 KR KR1019910701317A patent/KR920701234A/ko not_active Application Discontinuation
- 1991-02-06 HU HU913193A patent/HUT59158A/hu unknown
- 1991-02-06 WO PCT/EP1991/000228 patent/WO1991012261A1/en active IP Right Grant
- 1991-02-06 AU AU72307/91A patent/AU642215B2/en not_active Ceased
- 1991-02-06 RU SU915001903A patent/RU2088589C1/ru active
- 1991-02-06 AT AT91903236T patent/ATE128143T1/de not_active IP Right Cessation
- 1991-02-06 DE DE69113155T patent/DE69113155T2/de not_active Expired - Fee Related
- 1991-02-06 CA CA002049318A patent/CA2049318A1/en not_active Abandoned
- 1991-02-07 IE IE040891A patent/IE910408A1/en unknown
- 1991-02-07 ZA ZA91918A patent/ZA91918B/xx unknown
- 1991-02-07 PT PT96699A patent/PT96699A/pt unknown
- 1991-02-08 CN CN91100959A patent/CN1054771A/zh active Pending
- 1991-02-08 MY MYPI91000195A patent/MY105402A/en unknown
- 1991-10-07 FI FI914723A patent/FI914723A0/fi not_active Application Discontinuation
- 1991-10-07 NO NO91913923A patent/NO913923L/no unknown
-
1992
- 1992-11-11 HR HR921221A patent/HRP921221A2/hr not_active Application Discontinuation
-
1995
- 1995-11-08 GR GR950403105T patent/GR3017996T3/el unknown
Also Published As
Publication number | Publication date |
---|---|
CN1054771A (zh) | 1991-09-25 |
KR920701234A (ko) | 1992-08-11 |
EP0468012B1 (en) | 1995-09-20 |
IE910408A1 (en) | 1991-08-14 |
ZA91918B (en) | 1991-11-27 |
AU642215B2 (en) | 1993-10-14 |
RU2088589C1 (en) | 1997-08-27 |
GR3017996T3 (en) | 1996-02-29 |
NZ237023A (en) | 1993-01-27 |
HRP921221A2 (en) | 1995-12-31 |
DK0468012T3 (da) | 1995-11-06 |
NO913923L (no) | 1991-12-06 |
CS9100274A2 (en) | 1991-12-17 |
NO913923D0 (no) | 1991-10-07 |
CA2049318A1 (en) | 1991-08-10 |
ATE128143T1 (de) | 1995-10-15 |
PT96699A (pt) | 1991-10-31 |
IL97025A (en) | 1995-05-26 |
CZ279484B6 (cs) | 1995-05-17 |
GB9002922D0 (en) | 1990-04-04 |
JPH04505462A (ja) | 1992-09-24 |
IL97025A0 (en) | 1992-03-29 |
US5155107A (en) | 1992-10-13 |
HU913193D0 (en) | 1992-01-28 |
FI914723A0 (fi) | 1991-10-07 |
DE69113155T2 (de) | 1996-02-29 |
WO1991012261A1 (en) | 1991-08-22 |
AU7230791A (en) | 1991-09-03 |
DE69113155D1 (de) | 1995-10-26 |
EP0468012A1 (en) | 1992-01-29 |
MY105402A (en) | 1994-09-30 |
HUT59158A (en) | 1992-04-28 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FG2A | Definitive protection |
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