BORONATE ESTER COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF

• Main Authors: ERIC L ELLIOTT, RAYMOND D SKWIERCZYNSKI, CSANAD M VARGA, VAITHIANATHAN PALANIAPPAN, DEBRA L MAZAIK, PETER N ZAWANEH, QUENTIN J MCCUBBIN, NOBEL T TRUONG, PHUONG M NGUYEN, ABU J FERDOUS, MICHAEL J KAUFMAN, SONJA A KOMAR
• Format: Patent
• Language: English; Japanese
• Published: 07.12.2017
• Subjects: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM; CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

PROBLEM TO BE SOLVED: To provide novel boronate ester compounds useful as proteasome inhibitors.SOLUTION: A pharmaceutical composition comprises a compound of formula (I) or a crystalline form thereof, and additional excipients. The composition is suitable for production of a lyophilized powder pharmaceutical dosage form. (Z1 and Z2 together form a moiety derived from an α-hydroxy carboxylic acid where the atom attached to B in each case is O; alternatively, Z1 and Z2 together form a moiety derived from a β-hydroxy carboxylic acid where the atom attached to B in each case is O.)SELECTED DRAWING: None 【課題】プロテアソーム阻害剤として有用な新規ボロン酸エステル化合物を提供。【解決手段】式（Ｉ）で表される化合物、又はその結晶形態、及び追加の賦形剤を含む、医薬組成物。前記組成物は、凍結乾燥粉末の医薬投薬形態を製造するのに好適である。（Ｚ１及びＺ２は共に、α−ヒドロキシカルボン酸に由来する部分を形成し、いずれの場合にもＢに結合する原子は、Ｏであるか、またはＺ１およびＺ２は共に、β−ヒドロキシカルボン酸に由来する部分を形成し、いずれの場合にもＢに結合する原子は、Ｏである）【選択図】なし