专利号:US-7700654-B2 优先权日:2005-02-05 标 题:Isolation of N-butylbenzenesulfonamide, synthesis of benzenesulfonamide derivatives, and use of N-butylbenzenesulfonamide and benzenesulfonamide derivatives for treating benign prostatic hyperplasia and/or prostate carcinoma 发明人:HOFFMANN HANS-RAINER; MATUSCH RUDOLF; BANIAHMAD ARIA 权利人:LOHMANN THERAPIE SYST LTS 摘要:A process for isolating N-butylbenzenesulfonamide (NBBS) from biological material, the chemical synthesis of benzenesulfonamide derivatives, the use of NBBS and benzenesulfonamide derivatives for treating benign prostatic hyperplasia and/or prostate carcinoma, the production of medicaments for the treatment thereof, and the use of NBBS and benzenesulfonamide derivatives as a lead substance in the development of active substances for treating benign prostatic hyperplasia and/or prostate carcinoma are provided.
专利号:US-8481519-B2 优先权日:2005-02-05 标题 :Isolation of atraric acid, synthesis of atraric acid derivatives, and use of atraric acid and the derivatives thereof for the treatment of benign prostatic hyperplasia, prostate carcinoma and spinobulbar muscular atrophy 发明人:HOFFMANN HANS-RAINER; MATUSCH RUDOLF; BANIAHMAD ARIA 权利人:HOFFMANN HANS-RAINER; MATUSCH RUDOLF; BANIAHMAD ARIA; LOHMANN THERAPIE SYST LTS 摘要:A method for isolating atraric acid from biological material, atraric acid derivatives, the chemical synthesis thereof, and the use of atraric acid and the derivatives thereof for treating or producing a medicament for treating benign prostate hyperplasia, prostate carcinoma or spinobulbar muscular atrophy is provided. In addition, a basic substance for the development of other agents used for treating benign prostate hyperplasia, prostate carcinoma, or spinobulbar muscular atrophy is provided.
专利号:US-9884067-B2 优先权日:2013-03-14 标 题:Androgen receptor down-regulating agents and uses thereof 发明人:NJAR VINCENT C O; GEDIYA LALJI K; PURUSHOTTAMACHAR PURANIK; GODBOLE ABHIJIT; KWEGYIR AFFUL ANDREW; VASAITIS TADAS 权利人:UNIV OF MARYLAND EASTERN SHORE; UNIV JEFFERSON; UNIV MARYLAND 摘要:The present disclosure provides the design and synthesis of novel steroidal compounds that cause down-regulation of the androgen receptor (AR), both full length and splice variant. The compounds are potential agents for the treatment of all forms of prostate cancer and other diseases that depend on functional AR.
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-2009143466-A1 优先权日:2005-02-05 标题 :Isolation of Atraric Acid, Synthesis of Atraric Acid Derivatives, and Use of Atraric Acid and the Derivatives Thereof for the Treatment of Benign Prostatic Hyperplasia, Prostate Carcinoma and Spinobulbar Muscular Atrophy
专利号:US-2008177107-A1 优先权日:2005-02-05 标题 :Isolation of N-Butylbenzenesulfonamide, Synthesis of Benzenesulfonamide Derivatives, and Use of N-Butylbenzenesulfonamide and Benzenesulfonamide Derivatives for Treating Benign Prostatic Hyperplasia and/or Prostate Carcinoma
参考文献:10.1038/onc.2011.273 摘要:Rao S, Lyons LS, Fahrenholtz CD, Wu F, Farooq A, Balkan W, Burnstein KL. A novel nuclear role for the Vav3 nucleotide exchange factor in androgen receptor coactivation in prostate cancer. Oncogene. 2012 Feb 09;31(6):716–27. 参考文献:10.1007/s13277-011-0209-y 摘要:Otsuka T, Iguchi K, Fukami K, Ishii K, Usui S, Sugimura Y, Hirano K. Androgen receptor W741C and T877A mutations in AIDL cells, an androgen-independent subline of prostate cancer LNCaP cells. Tumour Biol. 2011 Dec;32(6):1097–102. doi: 10.1007/s13277-011-0209-y.