Title:
COMPOUND SERVING AS PRODRUG OF HYDROXAMIC ACID OR SALT OF SAID COMPOUND, FREEZE-DRIED MEDICINAL PREPARATION, LpxC INHIBITOR, AND ANTIBACTERIAL
Document Type and Number:
WIPO Patent Application WO/2018/143162
Kind Code:
A1
Abstract:
The present invention addresses the problem of providing: a compound which shows potent antibacterial activity and excellent solubility in water or a salt of the compound; and a freeze-dried medicinal preparation, an LpxC inhibitor, and an antibacterial each containing the compound or salt. According to the present invention, a compound represented by general formula [1] or a salt thereof is provided. [In formula [1], R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, etc.; R3 represents a hydrogen atom, etc.; R4 represents a hydrogen atom, etc.; and n is 0 or 1.]
Inventors:
SHOJI MUNEO (JP)
NAGATO YUSUKE (JP)
SUZUMURA YUKO (JP)
NAGATO YUSUKE (JP)
SUZUMURA YUKO (JP)
Application Number:
PCT/JP2018/002874
Publication Date:
August 09, 2018
Filing Date:
January 30, 2018
Export Citation:
Assignee:
TOYAMA CHEMICAL CO LTD (JP)
International Classes:
C07F9/09; A61K9/19; A61K31/661; A61P31/04; A61P43/00; C12N9/18
Domestic Patent References:
| WO2016039433A1 | 2016-03-17 | |||
| WO2014142298A1 | 2014-09-18 | |||
| WO2016039433A1 | 2016-03-17 | |||
| WO2011132712A1 | 2011-10-27 |
Foreign References:
| JP2006503831A | 2006-02-02 | |||
| US20160194351A1 | 2016-07-07 |
Other References:
"Textbook of Drug Design and Discovery", 2002, article LARSEN, C. S. ET AL.: "Chapter 14 Design and application of prodrugs. 14.4.3 Improvement of drug formulation.", pages: 460 - 514, XP055530665
MANTYLA, A. ET AL.: "Design, synthesis and in vitro evaluation of novel water-soluble prodrugs of buparvaquone", EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 23, 2004, pages 151 - 158, XP004580038
CHEMICAL SOCIETY OF JAPAN: "Chapter 4.3. Synthesis by addition reaction of alcohol to alkenyl ether", EXPERIMENTAL CHEMICAL LECTURE 14: SYNTHESIS OF ORGANIC COMPOUNDS II - ALCOHOL AND AMINE (5TH EDITION), 2007, pages 325 - 333, XP009515455, ISBN: 4-621-07313-3
GREENE, T. W. ET AL.: "PROTECTION FOR THE HYDROXYL GROUP, INCLUDING 1,2- AND 1, 3-DIOLS", PROTECTIVE GROUPS IN ORGANIC SYNTHESIS, 1999, pages 17 - 246, XP055474694
W. GREENE ET AL.: "Protective Groups in Organic Synthesis", 2007, JOHN WILEY & SONS, INC, pages: 934 - 299
"Greene's Protective Groups in Organic Synthesis", 2014, JOHN WILEY & SONS, INC, pages: 1203 - 1262
"Fourth Series of Experimental Chemistry", vol. 20, 1992, MARUZEN, pages: 344 - 345
"Seizai no tanni sousa to kikai (Unit operation and machine for formulation", vol. 11, 1988, HIROKAWA-SHOTEN LTD., article "Iyakuhin no jissai (Practice of pharmaceutical products", pages: 388 - 396
MANTYLA, A. ET AL.: "Design, synthesis and in vitro evaluation of novel water-soluble prodrugs of buparvaquone", EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 23, 2004, pages 151 - 158, XP004580038
CHEMICAL SOCIETY OF JAPAN: "Chapter 4.3. Synthesis by addition reaction of alcohol to alkenyl ether", EXPERIMENTAL CHEMICAL LECTURE 14: SYNTHESIS OF ORGANIC COMPOUNDS II - ALCOHOL AND AMINE (5TH EDITION), 2007, pages 325 - 333, XP009515455, ISBN: 4-621-07313-3
GREENE, T. W. ET AL.: "PROTECTION FOR THE HYDROXYL GROUP, INCLUDING 1,2- AND 1, 3-DIOLS", PROTECTIVE GROUPS IN ORGANIC SYNTHESIS, 1999, pages 17 - 246, XP055474694
W. GREENE ET AL.: "Protective Groups in Organic Synthesis", 2007, JOHN WILEY & SONS, INC, pages: 934 - 299
"Greene's Protective Groups in Organic Synthesis", 2014, JOHN WILEY & SONS, INC, pages: 1203 - 1262
"Fourth Series of Experimental Chemistry", vol. 20, 1992, MARUZEN, pages: 344 - 345
"Seizai no tanni sousa to kikai (Unit operation and machine for formulation", vol. 11, 1988, HIROKAWA-SHOTEN LTD., article "Iyakuhin no jissai (Practice of pharmaceutical products", pages: 388 - 396
Attorney, Agent or Firm:
SIKS & CO. (JP)
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