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 DISEASE

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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
Application number
CY20101101188T
Other languages
Greek (el)
Inventor
Angela Brodie
Vincent Njar
Original Assignee
University Of Maryland Baltimore
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Priority claimed from EP06736460A external-priority patent/EP1853619B1/en
Application filed by University Of Maryland Baltimore filed Critical University Of Maryland Baltimore
Publication of CY1116024T1 publication Critical patent/CY1116024T1/en

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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.

CY20101101188T 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 CY1116024T1 (en)

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

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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

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CY (2) CY1116024T1 (en)

Also Published As

Publication number Publication date
CY1115910T1 (en) 2017-01-25

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