专利号:US-9295679-B2 优先权日:2008-03-25 标 题:Prodrugs of C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity 发明人:NJAR VINCENT; BRODIE ANGELA; GEDIYA LALJI K 权利人:UNIV MARYLAND 摘要:Prodrugs of steroidal C-17 benzoazoles, pyrimidinoazoles (az-abenzoazoles) and diazines. Methods of synthesis are also described, whereby a prodrug group is substituted for a functional group at A ring portion of the ABC ring structure of the steroid. Suitable pro-drug groups include amino acid groups, succinate groups, phosphate groups, or sulfamate groups. The prodrugs of the disclosed compounds allow for improved oral bioavailability of the compounds that are inhibitors of human CYP 17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds and the corresponding prodrugs are useful for the treatment of conditions such as human prostate cancer, breast cancer, and prostate hyperplasia.
专利号:US-10098896-B2 优先权日:2005-03-02 标 题:C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens, in vitro biological activities, pharmacokinetics and antitumor activity 发明人:BRODIE ANGELA; NJAR VINCENT C O 权利人:THE UNIV OF MARYLAND BALTIMORE; UNIV MARYLAND 摘要:Described are steroidal C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic “addition-eliminationâ€? substitution reaction of 3β-acetoxy-17-chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles and methods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3β-ol or analogs thereof with tributylstannyl diazines. The compounds are potent inhibitors of human CYP17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds are useful for the treatment of human prostate cancer.
专利号:US-11739082-B2 优先权日:2017-08-31 标 题 :Thiophene compounds, process for synthesis and use thereof 发明人:KOMIRISHETTY KASHINATH; VERMA MAHESH KUMAR; GANJU PARUL; PRASAD SUDHANAND 权利人:AHAMMUNE BIOSCIENCES PRIVATE LTD 摘要:The present invention relates to novel thiophene compounds of general Formula I, and their stereoisomers (diastereoisomers, enantiomers), pure or mixed, racemic mixtures, geometrical isomers, tautomers, pharmaceutically acceptable salts, hydrates, solvates, solid forms and mixtures thereof along with process for their preparation. The present invention discloses compounds that are useful in the treatment and prevention of autoimmune diseases.
专利号:US-2009137557-A1 优先权日:2005-11-22 标题 :Calcilytic Compounds 发明人:KU THOMAS WEN FU; LIN HONG; LUENGO JUAN I; MARQUIS JR ROBERT W; RAMANJULU JOSHI M; TROUT ROBERT; YAMASHITA DENNIS S 权利人:KU THOMAS WEN FU; LIN HONG; LUENGO JUAN I; MARQUIS JR ROBERT W; RAMANJULU JOSHI M; TROUT ROBERT; YAMASHITA DENNIS S 摘要:Novel calcilytic compounds, pharmaceutical compositions, methods of synthesis and methods of using them are provided.
专利号:US-9018198-B2 优先权日:2008-03-25 标题 :Prodrugs of C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity
专利号:US-7875599-B2 优先权日:2005-03-02 标题:C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens, in vitro biological activities, pharmacokinetics and antitumor activity 发明人:BRODIE ANGELA; NJAR VINCENT 权利人:UNIV MARYLAND 摘要:Described are steroidal C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic “addition-eliminationâ€? substitution reaction of 3β-acetoxy-17-chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles and methods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3β-ol or analogs thereof with tributylstannyl diazines. The compounds are potent inhibitors of human CYP 17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds are useful for the treatment of human prostate cancer.