ES2178750T3 - 17-beta- iclopropil(amino/oxi)4-aza esteroides como inhibidores activos de la 5-alfa-reductasa y de c17-20-liasa de testosterona. - Google Patents
17-beta- iclopropil(amino/oxi)4-aza esteroides como inhibidores activos de la 5-alfa-reductasa y de c17-20-liasa de testosterona.Info
- Publication number
- ES2178750T3 ES2178750T3 ES97901995T ES97901995T ES2178750T3 ES 2178750 T3 ES2178750 T3 ES 2178750T3 ES 97901995 T ES97901995 T ES 97901995T ES 97901995 T ES97901995 T ES 97901995T ES 2178750 T3 ES2178750 T3 ES 2178750T3
- Authority
- ES
- Spain
- Prior art keywords
- compounds
- liasa
- aza
- testosterona
- iclopropil
- 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
- 150000000520 4-azasteroids Chemical class 0.000 title 1
- -1 AMINO Chemical class 0.000 title 1
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 239000003098 androgen Substances 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 230000001404 mediated effect Effects 0.000 abstract 3
- 229940030486 androgens Drugs 0.000 abstract 2
- JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 abstract 2
- 208000002874 Acne Vulgaris Diseases 0.000 abstract 1
- 206010006187 Breast cancer Diseases 0.000 abstract 1
- 208000026310 Breast neoplasm Diseases 0.000 abstract 1
- 208000014311 Cushing syndrome Diseases 0.000 abstract 1
- 206010060862 Prostate cancer Diseases 0.000 abstract 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 abstract 1
- 206010000496 acne Diseases 0.000 abstract 1
- 102000001307 androgen receptors Human genes 0.000 abstract 1
- 108010080146 androgen receptors Proteins 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 230000001419 dependent effect Effects 0.000 abstract 1
- MKXKFYHWDHIYRV-UHFFFAOYSA-N flutamide Chemical compound CC(C)C(=O)NC1=CC=C([N+]([O-])=O)C(C(F)(F)F)=C1 MKXKFYHWDHIYRV-UHFFFAOYSA-N 0.000 abstract 1
- 229960002074 flutamide Drugs 0.000 abstract 1
- 229960000890 hydrocortisone Drugs 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 201000009395 primary hyperaldosteronism Diseases 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 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
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/59—Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
-
- 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)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Steroid Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
LA INVENCION SE REFIERE A 4 - AZA - 17 BE - (CICLOPROPOXI) ANDROST - 5 AL - ANDROSTAN - 3 - ONA, 4 - AZA - 17 BE (CI CLOPROPILAMINO) - ANDROST - 4 - EN - 3 - ONA Y A COMPUESTOS RELACIONADOS Y A COMPOSICIONES QUE COMPRENDEN ESTOS COMPUESTOS, ASI COMO LA INHIBICION DE LIASA C 17-20), 5 AL - REDUCTASA Y C 17 AL - HIDROLASA Y AL USO DE ESTOS COMPUESTOS EN EL TRATAMIENTO DE TRASTORNOS MEDIADOS POR ANDROGENOS Y ESTROGENOS, INCLUIDA LA HIPERPLASIA PROSTATICA BENIGNA, CANCER DE PROSTATA MEDIADO POR ANDROGENOS, CANCER DE MAMA MEDIADO POR ESTROGENOS Y A TRASTORNOS MEDIADOS POR DHT TALES COMO EL ACNE. TAMBIEN SE INCLUYEN LOS TRASTORNOS RELATIVOS A LA SOBRESINTESIS DE CORTISOL, POR EJEMPLO, EL SINDROME DE CUSHING. EL TRATAMIENTO DE TRASTORNOS DEPENDIENTES DE ANDROGENOS TAMBIEN COMPRENDE UNA TERAPIA COMBINATORIA CON ANTAGONISTAS CONOCIDOS DEL RECEPTOR DE ANDROGENOS, TALES COMO LA FLUTAMIDA. LOS COMPUESTOS DE LA INVENCION TIENEN LA FORMULA GENERAL (I).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US60127896A | 1996-02-14 | 1996-02-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2178750T3 true ES2178750T3 (es) | 2003-01-01 |
Family
ID=24406899
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES97901995T Expired - Lifetime ES2178750T3 (es) | 1996-02-14 | 1997-01-09 | 17-beta- iclopropil(amino/oxi)4-aza esteroides como inhibidores activos de la 5-alfa-reductasa y de c17-20-liasa de testosterona. |
Country Status (17)
| Country | Link |
|---|---|
| EP (1) | EP0880540B1 (es) |
| JP (1) | JP2000505444A (es) |
| KR (1) | KR19990082543A (es) |
| CN (1) | CN1211256A (es) |
| AT (1) | ATE219100T1 (es) |
| AU (1) | AU710208B2 (es) |
| BR (1) | BR9708301A (es) |
| CA (1) | CA2244823A1 (es) |
| DE (1) | DE69713285T2 (es) |
| DK (1) | DK0880540T3 (es) |
| ES (1) | ES2178750T3 (es) |
| HU (1) | HUP9900955A3 (es) |
| IL (1) | IL125575A0 (es) |
| NO (1) | NO983724L (es) |
| NZ (1) | NZ327041A (es) |
| PT (1) | PT880540E (es) |
| WO (1) | WO1997030069A1 (es) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6187925B1 (en) | 1997-12-23 | 2001-02-13 | Merck & Co., Inc. | Intermediates and process for the synthesis of azasteroids |
| US7005428B1 (en) | 1998-06-11 | 2006-02-28 | Endorecherche, Inc. | Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors |
| US6465445B1 (en) | 1998-06-11 | 2002-10-15 | Endorecherche, Inc. | Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors |
| AU2002221080A1 (en) * | 2000-12-08 | 2002-06-18 | Masami Kusaka | Substituted thiazole derivatives bearing 3-pyridyl groups, process for preparingthe same and use thereof |
| AU2004238238C1 (en) | 2003-05-07 | 2010-01-14 | Merck Sharp & Dohme Corp. | Androgen receptor modulators and methods of use thereof |
| SG185930A1 (en) * | 2007-10-29 | 2012-12-28 | Takeda Pharmaceutical | Pyrrolo [1,2-c] imidazole derivatives for use in the prophylaxis or treatment of cancer which is refractory to known cancer therapies |
| EP2362872A4 (en) * | 2008-10-28 | 2012-05-30 | Biomarin Pharm Inc | DECAHYDRO-1H-INDENOCHINOLINONE AND DECAHYDRO-3H-CYCLOPENTAPHENANTHRIDINONE CYP17 HEMMER |
| US20110178065A1 (en) * | 2010-01-15 | 2011-07-21 | Biomarin Pharmaceutical Inc. | Novel cyp17 inhibitors |
| GB201102913D0 (en) | 2011-02-18 | 2011-04-06 | Univ Birmingham | Novel therapeutic |
| CN109438549B (zh) * | 2018-12-13 | 2022-01-04 | 湖北葛店人福药业有限责任公司 | 一种制备N-叔丁基-3-氧代-4-氮杂-5α-雄甾-17β-甲酰胺的方法 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5264427A (en) * | 1992-01-29 | 1993-11-23 | Research Corporation Technologies, Inc. | 20-substituted pregnene derivatives and their use as androgen synthesis inhibitors |
| SK140494A3 (en) * | 1992-05-21 | 1995-07-11 | Endorecherche Inc | Inhibitors of testosterone 5-alpha-reductase activity |
| US5486511A (en) * | 1993-05-25 | 1996-01-23 | Merrell Dow Pharmaceuticals Inc. | 4-amino-17β-(cyclopropyloxy)androst-4-en-3-one, 4-amino-17β-(cyclopropylamino)androst-4-en-3-one and related compounds as C17-20 lyase and 5α-reductase |
-
1997
- 1997-01-09 KR KR1019980706280A patent/KR19990082543A/ko not_active Application Discontinuation
- 1997-01-09 PT PT97901995T patent/PT880540E/pt unknown
- 1997-01-09 JP JP9529338A patent/JP2000505444A/ja active Pending
- 1997-01-09 NZ NZ327041A patent/NZ327041A/xx unknown
- 1997-01-09 AU AU15767/97A patent/AU710208B2/en not_active Ceased
- 1997-01-09 AT AT97901995T patent/ATE219100T1/de not_active IP Right Cessation
- 1997-01-09 WO PCT/US1997/000469 patent/WO1997030069A1/en not_active Application Discontinuation
- 1997-01-09 EP EP97901995A patent/EP0880540B1/en not_active Expired - Lifetime
- 1997-01-09 CN CN97192283A patent/CN1211256A/zh active Pending
- 1997-01-09 CA CA002244823A patent/CA2244823A1/en not_active Abandoned
- 1997-01-09 ES ES97901995T patent/ES2178750T3/es not_active Expired - Lifetime
- 1997-01-09 DE DE69713285T patent/DE69713285T2/de not_active Expired - Fee Related
- 1997-01-09 DK DK97901995T patent/DK0880540T3/da active
- 1997-01-09 BR BR9708301A patent/BR9708301A/pt not_active IP Right Cessation
- 1997-01-09 HU HU9900955A patent/HUP9900955A3/hu unknown
- 1997-01-09 IL IL12557597A patent/IL125575A0/xx unknown
-
1998
- 1998-08-13 NO NO983724A patent/NO983724L/no unknown
Also Published As
| Publication number | Publication date |
|---|---|
| DK0880540T3 (da) | 2002-10-07 |
| IL125575A0 (en) | 1999-03-12 |
| CN1211256A (zh) | 1999-03-17 |
| AU1576797A (en) | 1997-09-02 |
| HUP9900955A2 (hu) | 1999-07-28 |
| NZ327041A (en) | 1999-11-29 |
| NO983724D0 (no) | 1998-08-13 |
| EP0880540A1 (en) | 1998-12-02 |
| DE69713285T2 (de) | 2003-01-02 |
| KR19990082543A (ko) | 1999-11-25 |
| JP2000505444A (ja) | 2000-05-09 |
| PT880540E (pt) | 2002-10-31 |
| ATE219100T1 (de) | 2002-06-15 |
| HUP9900955A3 (en) | 2000-06-28 |
| NO983724L (no) | 1998-10-13 |
| CA2244823A1 (en) | 1997-08-21 |
| WO1997030069A1 (en) | 1997-08-21 |
| BR9708301A (pt) | 1999-08-03 |
| EP0880540B1 (en) | 2002-06-12 |
| AU710208B2 (en) | 1999-09-16 |
| DE69713285D1 (en) | 2002-07-18 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| MX2021011826A (es) | Composiciones y combinaciones farmacéuticas que comprenden inhibidores del receptor de andrógenos y usos de estas. | |
| ES2178750T3 (es) | 17-beta- iclopropil(amino/oxi)4-aza esteroides como inhibidores activos de la 5-alfa-reductasa y de c17-20-liasa de testosterona. | |
| UY26472A1 (es) | Compuestos de dihidropirimidina heterocíclicos | |
| PA8509901A1 (es) | Compuestos, composiciones farmaceuticas de indazol y metodos para mediar o inhibir la proliferacion celular. | |
| DK147086D0 (da) | Farmaceutisk komposition til kombinationsterapi af hormonafhaengige cancertyper | |
| UY28213A1 (es) | Nuevos derivados de cianopiridina útiles en el tratamiento de cáncer y otros trastornos. | |
| PE20020348A1 (es) | Exemestano como agente quimiopreventivo | |
| TW200500355A (en) | Methods and compositions using immunomodulatory compounds for treatment and management of cancers and other diseases | |
| UY26130A1 (es) | Compuestos para tratar la obesidad | |
| CR6565A (es) | Pirimidina-2,4,6-trionas inhibidores de metloproteinas | |
| ES2194495T3 (es) | Agentes androgenos en combinacion con agentes gestagenos para la compensacion de una deficiencia de testosterona con proteccion de la prostata. | |
| EP2004177A4 (en) | NITROFURAN COMPOUNDS FOR THE TREATMENT OF CANCER AND ANGIOGENESIS | |
| DE60040753D1 (de) | Therapeutische verwendungen von steroiden bei blutzellmangelzustaenden | |
| TR200200066T2 (tr) | Migrenin tedavisi için seçici iGluR5 reseptör antagonistleri | |
| AR029371A1 (es) | Urea-peptoides de indol e indazol como antagonistas del receptor de trombina, composicion farmaceutica y el uso. | |
| TR200103271T2 (tr) | İnflamasyon aracılığıyla gerçekleşen infeksiyon için anti-inflamatuar tedavi. | |
| SV2002000005A (es) | Heterociclos 2-arilimino substituidos y composiciones que los contienen para usar como agentes que ligan el receptor de la progesterona ref. 5048p1-sv | |
| WO2020141828A3 (en) | Anticancer compositions comprising immune checkpoint inhibitors | |
| CY1106713T1 (el) | Συνδυασμενη θεραπεια εναντιον καρκινωματων η οποια περιλαμβανει παραγωγα υποκαταστημενης ακρυλοϋλ δισταμυσινης και αλκυλιωτικους παραγοντες | |
| MX2020011826A (es) | Composiciones de combinacion que comprenden compuestos de bisfluoroalquil-1,4-benzodiazepinona y metodos de uso de las mismas. | |
| AR024907A1 (es) | Uso de inhibidores de la produccion y/o accion de la il-18 y composiciones farmaceuticas formuladas con dichos inhibidores para el tratamiento demetastasis de tumores. | |
| MX2019014677A (es) | Compuestos de estra-1,3,5(10)-trien-17-ona sustituida con 15.beta.-[3-propanamido] y sus 17-oximas para usarse en la inhibicion de 17.beta.-hidroxiesteroides deshidrogenasas. | |
| MX2022007595A (es) | Triterpenoides sinteticos con sustituyentes a base de nitrogeno en c-17 y metodos de uso de los mismos. | |
| AR048829A1 (es) | 17alfa - fluoroesteroides con actividad inhibidora de 5 alfa-reductasa; composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos para el tratamiento de enfermedades cancerosas influidas por androgenos. | |
| AR036257A1 (es) | Sulfamatos de 2-alcoxiestradiol de accion antitumoral |