Title:
アミノ含有生物活性剤のトリアルキルロック促進性重合体プロドラッグ
Document Type and Number:
Japanese Patent JP4728478
Kind Code:
B2
Abstract:
The present invention is directed to double prodrugs containing polymeric-based transport forms. These polymeric prodrugs are preferably of the formula: wherein: B is a leaving group or a residue of an amine-containing target moiety; G is or CH2; Y1-2 are independently O or S; M is X or Q; where X is an electron withdrawing group and Q is a moiety containing a free electron pair positioned three to six atoms from C(=Y2); R1, R4, R7, R8, R9, R10 and R13 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls; R2, R3, R5 and R6 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C1-6 alkoxy, phenoxy, C1-8 heteroalkyls, C1-8 heteroalkoxy, substituted C1-6 alkyls, C3-8 cycloalkyls, C3-8 substituted cycloalkyls, aralkyls, aryls, substituted aryls, such as aryls substituted with halo-, nitro- and cyano-; carboxy-, C1-6 carboxyalkyls and C1-6 alkyl carbonyls; (m) is zero or one; (n) is zero or a positive integer; (p) is zero, one or two; and R11 is a substantially non-antigenic polymer. The first prodrug is generated when the polymeric portion of the double prodrug is cleaved and the parent molecule is generated rapidly thereafter in vivo, as a result of a trialkyl lock type lactonization-type reaction.
Inventors:
Greenwald, Richard, Bee.
Cho, Yun, Yi.
Pendri, Annapurna
Cho, Yun, Yi.
Pendri, Annapurna
Application Number:
JP2000526236A
Publication Date:
July 20, 2011
Filing Date:
December 29, 1998
Export Citation:
Assignee:
Enzon Pharmaceuticals, Incorporated
International Classes:
A61K47/48; A61K31/135; A61K31/136; A61K31/65; A61K31/704; A61K31/7068; A61K38/00; A61K45/00; A61P43/00; C07C237/22; C07C271/16; C07C271/22; C08G65/329
Foreign References:
| WO1996023794A1 |
Other References:
Journal of Pharmaceutical Sciences,1997年 7月,Vol.86,pp.765-767
DDSの進歩 1995-96(Molecular Medicine別冊),1995年,82-94
DDSの進歩 1995-96(Molecular Medicine別冊),1995年,82-94
Attorney, Agent or Firm:
Yusuke Hiraki
Satoshi Fujita
Eiichi Arai
Natsuo Tanaka
Satoshi Fujita
Eiichi Arai
Natsuo Tanaka