Title:
CLASS OF CARBOXYLIC ACID DERIVATIVES AND USE THEREOF IN PREPARATION OF PRODRUGS
Document Type and Number:
WIPO Patent Application WO/2015/120820
Kind Code:
A1
Abstract:
The present invention discloses a class of carboxylic acid derivatives and use thereof in preparation of prodrugs. The carboxylic acid derivatives have the general formula (I): R1 being H or an alkyl; X being H or F; Y being F or a fluoroalkyl; n being 0, 1, 2, 3, 4, 5, or 6; W being W1 or W2; W1 being NR2R3, NR2R3·A, formula (AA), or formula (BB); R2 and R3 each independently being H, an alkyl, a cycloalkyl, or an amino protecting group; m being 0, 1, 2, or 3; A being an acid; W2 being COOR4, OPO(OR4)2, or PO(OR4)2; R4 being H, or being a carboxyl or phosphate hydroxyl protecting group.
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Inventors:
LI QINGENG (CN)
WANG TAO (CN)
CHEN GANG (CN)
WANG YUANZHONG (CN)
MAO WEI (CN)
WU TONG (CN)
ZENG LINGGUO (CN)
WANG TAO (CN)
CHEN GANG (CN)
WANG YUANZHONG (CN)
MAO WEI (CN)
WU TONG (CN)
ZENG LINGGUO (CN)
Application Number:
PCT/CN2015/073165
Publication Date:
August 20, 2015
Filing Date:
February 16, 2015
Export Citation:
Assignee:
LI QINGENG (CN)
International Classes:
C07C229/20; C07C67/30; C07C69/63; C07C227/04; C07C227/18; C07C229/22; C07D203/02; C07D203/08; C07D295/15; C07D305/14; C07F9/09
Foreign References:
| CN101094840A | 2007-12-26 | |||
| CN102015621A | 2011-04-13 | |||
| CN1907954A | 2007-02-07 | |||
| CN101898978A | 2010-12-01 |
Other References:
HOOK, D.F. ET AL.: "Probing the Proteolytic Stability of beta-peptides Containing a-fluoro- and alpha-hydroxy-beta-amino Acids", vol. 5, 31 December 2004 (2004-12-31), pages 691 - 706, XP008143749
DESMOULIN ET AL.: "Metabolism of Capecitabine, An Oral Fluorouracil Prodrug: 19F NMR Studies in Animal Models and Human Urine", DRUG METABOLISM AND DISPOSITION, vol. 30, no. 11, 5 August 2002 (2002-08-05), pages 1221 - 1229, XP055357568
JURCIK, V. ET AL.: "Single Enantiomer Synthesis of alpha-(trifluoromethyl)-beta-lactam", BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY, vol. 7, no. 86, 6 June 2011 (2011-06-06), pages 759 - 766, XP055357577
See also references of EP 3109230A4
DESMOULIN ET AL.: "Metabolism of Capecitabine, An Oral Fluorouracil Prodrug: 19F NMR Studies in Animal Models and Human Urine", DRUG METABOLISM AND DISPOSITION, vol. 30, no. 11, 5 August 2002 (2002-08-05), pages 1221 - 1229, XP055357568
JURCIK, V. ET AL.: "Single Enantiomer Synthesis of alpha-(trifluoromethyl)-beta-lactam", BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY, vol. 7, no. 86, 6 June 2011 (2011-06-06), pages 759 - 766, XP055357577
See also references of EP 3109230A4
Attorney, Agent or Firm:
NTD UNIVATION INTELLECTUAL PROPERTY AGENCY LTD. (CN)
北京永新同创知识产权代理有限公司 (CN)
北京永新同创知识产权代理有限公司 (CN)
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