CY1116024T1 - 3-BETA-HYDROXY-17- (1H-BENZIMIDAZOL-1-YL) ANDROSTA-5,16-DIAGNOSIS FOR USE IN TREATMENT OF A PROTECTIVE DISEASE - Google Patents
3-BETA-HYDROXY-17- (1H-BENZIMIDAZOL-1-YL) ANDROSTA-5,16-DIAGNOSIS FOR USE IN TREATMENT OF A PROTECTIVE DISEASEInfo
- Publication number
- CY1116024T1 CY1116024T1 CY20101101188T CY101101188T CY1116024T1 CY 1116024 T1 CY1116024 T1 CY 1116024T1 CY 20101101188 T CY20101101188 T CY 20101101188T CY 101101188 T CY101101188 T CY 101101188T CY 1116024 T1 CY1116024 T1 CY 1116024T1
- Authority
- CY
- Cyprus
- Prior art keywords
- treatment
- methods
- androsta
- benzimidazol
- diagnosis
- Prior art date
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Εδώ περιγράφονται στεροειδικά C-17 βενζοαζόλια, πυριμιδινοαζόλια (αζαβενζοαζόλια) και διαζίνες. Επίσης περιγράφονται μέθοδοι για τη σύνθεση τους, οι οποίες περιλαμβάνουν μεθόδους που έχουν ένα στάδιο αντίδρασης πυρηνόφιλης βινυλικής υποκατάστασης «προσθήκης-απόσπασης» του 3β-ακετοξυ-17-χλωρο-16-φορμυλανδροστα-5,16-διενίου ή αναλόγων αυτού και πυρηνόφιλων βενζοαζολίου ή πυριμιδινο-αζολίου και μεθόδους που έχουν μια καταλυόμενη από παλλάδιο αντίδραση διασταυρούμενης σύζευξης της 17-ιωδοανδροστα-5,16-διεν-3β-όλης ή αναλόγων αυτής με τριβουτυλοσταννυλοδιαζίνες. Οι ενώσεις είναι ισχυροί αναστολείς του ανθρώπινου ενζύμου CYP 17 καθώς και ισχυροί ανταγωνιστές αμφοτέρων των άγριου τύπου και μεταλλαγμένων υποδοχέων ανδρογόνων (AR). Οι ενώσεις είναι χρήσιμες για τη θεραπευτική αγωγή καρκίνου του ανθρώπινου προστάτη.Steroid C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines are described herein. Also described are methods for their synthesis, which comprise methods having a reaction step of "addition-removal" of 3β-acetoxy-17-chloro-16-formylandrosta-5,16-diene or its nucleophilic and nucleophilic reaction pyrimidine-azole and methods having a palladium-catalyzed cross-coupling reaction of 17-iodoandrost-5,16-dien-3β-ol or tributylsanthenyl diazines analogs. The compounds are potent inhibitors of the human CYP 17 enzyme as well as potent antagonists of both wild-type and mutated androgen receptors (AR). The compounds are useful for the treatment of human prostate cancer.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US65739005A | 2005-03-02 | 2005-03-02 | |
EP06736460A EP1853619B1 (en) | 2005-03-02 | 2006-03-02 | 3-beta-hydroxy-17-(1h-benzimidazol-1-yl)androsta-5,16-diene for use in the treatment of a prostate disease |
Publications (1)
Publication Number | Publication Date |
---|---|
CY1116024T1 true CY1116024T1 (en) | 2017-01-25 |
Family
ID=58457185
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CY20101101188T CY1116024T1 (en) | 2005-03-02 | 2010-12-23 | 3-BETA-HYDROXY-17- (1H-BENZIMIDAZOL-1-YL) ANDROSTA-5,16-DIAGNOSIS FOR USE IN TREATMENT OF A PROTECTIVE DISEASE |
CY20151100054T CY1115910T1 (en) | 2005-03-02 | 2015-01-20 | PHARMACEUTICAL COMPOSITION CONTAINING 3-BETA-HYDROXY-17- (l-HBENZIMIDAZOLE-1-YL) ANDROSTA-5,16-DIENE |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CY20151100054T CY1115910T1 (en) | 2005-03-02 | 2015-01-20 | PHARMACEUTICAL COMPOSITION CONTAINING 3-BETA-HYDROXY-17- (l-HBENZIMIDAZOLE-1-YL) ANDROSTA-5,16-DIENE |
Country Status (1)
Country | Link |
---|---|
CY (2) | CY1116024T1 (en) |
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2010
- 2010-12-23 CY CY20101101188T patent/CY1116024T1/en unknown
-
2015
- 2015-01-20 CY CY20151100054T patent/CY1115910T1/en unknown
Also Published As
Publication number | Publication date |
---|---|
CY1115910T1 (en) | 2017-01-25 |
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