Title:
P-セレクチン標的リガンドおよびその組成物
Document Type and Number:
Japanese Patent JP4771291
Kind Code:
B2
Abstract:
A P-selectin targeting ligand molecule (I) comprising target-recognizing group formed from a peptide, peptoid or its derivative, a spacer formed from water-soluble oligomer or polymer, and an anchoring moiety formed from an amphiphilic lipid consisting of one or more hydrophobic apolar moiety and a hydrophilic polar head group, is new. A P-selectin targeting ligand molecule (I) comprises a target-recognizing moiety, which is formed from a peptide, peptoid or its derivative, a spacer formed from a water-soluble oligomer or polymer, and an anchoring moiety, which is formed from an amphiphilic lipid consisting of one or more hydrophobic apolar moiety and a hydrophilic polar head group, where the target-recognizing moiety has an amino acid sequence X(A x) mA 3A 1A 2A 1Y, or its function equivalent, A 1D- or L-cysteine, D- or L-methionine, D- or L-valine, or its analog; A 2D- or L-aspartic acid or its analog; A 3D- or L-phenylalanine, D- or L-tyrosine, D- or L-tryptophan, or its analog; A xD- or L-amino acid; X : N-terminal side of the sequence (optionally substituted by R 1>-(Z) n-); Y : C-terminal side of the sequence (optionally substituted by R 1>-(Z) n-); X+Y : cyclic system (optionally substituted by R 1>-(Z) n-); Z : CO, O, NR 2>or CO-NR 2>; R 1>and R 2>H, 1-8C alkyl group, 2-8C alkyl group (in which one or more C-atom is replaced with N, O or S), 6-14C aryl group (optionally substituted with halogen), 1-6C alkyl, -CF 3, -OH, -O-1-6C alkyl, -COOH, -COO-1-6C alkyl, -NO 2, -NH 2, -NH-1-6C alkyl, -N(1-6C alkyl) 2or -SO 3H, heteroaryl (optionally substituted with one or more of halogen, 1-6C alkyl, -CF 3, -OH, -O-1-6C alkyl, -COOH, -COO-1-6C alkyl, -NO 2, -NH 2, -NH-1-6C alkyl, -N(1-6C alkyl) 2or -SO 3H), or an aralkyl group comprising an alkyl, aryl or heteroaryl group; and m and n : 0 or 1. Provided that n is not 0 when R 1>is H. Independent claims are also included for: (1) a pharmaceutical composition (II) comprising a carrier, and one or more (I) associated with the surface of the carrier; and (2) a kit for preparing (II), comprising a liquid and a solid component, where the liquid component is an aqueous composition, and the solid component comprises a colloidal carrier and one or more (I), being prepared by conventional methods and subsequent removal of water. ACTIVITY : Cardiant; Vasotropic; Anticoagulant; Thrombolytic; Cytostatic; Antiinflammatory; Antirheumatic; Antiarthritic; Gastrointestinal-Gen.; Neuroprotective; Antiarteriosclerotic; Nephrotropic; Vulnerary; Antibacterial; Immunosuppressive; Respiratory-Gen.; Cerebroprotective; Antiangiogenic. No biological data given. MECHANISM OF ACTION : Inactivates P-selectin; Counteracts inflammatory process within P-selectin activated cells.
Inventors:
Appeldoorn Chantal Catalina Maria
Van Berkel Theodorus Josephus Cornelis
Beesen Eric Anna Leonard Dus
Van Berkel Theodorus Josephus Cornelis
Beesen Eric Anna Leonard Dus
Application Number:
JP2006529953A
Publication Date:
September 14, 2011
Filing Date:
June 01, 2004
Export Citation:
Assignee:
Astellas Pharma Inc.
International Classes:
A61K38/00; A61K38/08; A61K9/10; A61K9/107; A61K9/127; A61K9/50; A61K9/51; A61K31/192; A61K31/198; A61K31/573; A61K31/7032; A61K47/08; A61K47/10; A61K47/12; A61K47/18; A61K47/24; A61K47/26; A61K47/28; A61K47/32; A61K47/34; A61K47/48; A61K49/00; A61P1/04; A61P7/00; A61P7/02; A61P9/00; A61P9/10; A61P11/00; A61P13/12; A61P25/00; A61P29/00; A61P31/04; A61P35/00; A61P35/04; A61P37/06; A61P43/00
Domestic Patent References:
| JP2002511446A | 2002-04-16 | |||
| JP2003506475A | 2003-02-18 |
Foreign References:
| WO2001060416A2 | 2001-08-23 | |||
| WO2002026776A2 | 2002-04-04 | |||
| WO2002055111A2 | 2002-07-18 | |||
| WO2003020753A1 | 2003-03-13 | |||
| WO2002098951A2 | 2002-12-12 |
Attorney, Agent or Firm:
Sadao Kumakura
Nobuo Ogawa
Atsushi Hakoda
Kenji Asai
Koji Hirayama
Nobuo Ogawa
Atsushi Hakoda
Kenji Asai
Koji Hirayama