Title:
【発明の名称】インテグリンアンタゴニストとしての環状カルボン酸
Document Type and Number:
Japanese Patent JP2003531189
Kind Code:
A
Abstract:
Cyclic carboxylic acids (I) and their salts are new. Cyclic carboxylic acids of formula (I) and their salts are new. [Image] R1>e.g. a 4-9 membered heterocyclic residue containing 0-3 heteroatoms (N, O or S); where R1> is optionally annulated with a 4-8 membered cyclic residue, containing 0-2 heteroatoms (N, S or O); R2>e.g. H, 1-10C alkyl, 2-10C alkenyl, 2-10C alkynyl (all optionally substituted); R3>e.g. H, 1-10C alkyl, 2-10C alkenyl, 2-10C alkynyl (all optionally substituted); R4>e.g. H, 1-10C alkyl, 2-10C alkenyl, 2-10C alkynyl (all optionally substituted); R5>e.g. H, 1-10C alkyl, 2-10C alkenyl, 2-10C alkynyl (all optionally substituted); R6>e.g. phenyl or 5-6 membered aromatic heterocyclic residue; A : e.g. -C(O)-, -C(O)-C(O) , -SO-, -SO2-, -PO-, -PO2-, 2- or 4-pyrimidyl, or 2-pyridyl; X : -CRx1>Rx2>-; Rx1>, Rx2>e.g. H, 1-4C alkyl, 2-4C alkenyl or 2 4C alkynyl; Y : e.g. -C(O) , -S(O)-, -SO2-, -O- or -S-; D : N or CRD1>; RD1>e.g. a bond, H, 1-4C alkyl, 2-4C alkenyl or 2-4C alkynyl (all optionally substituted); with provisos. The full definitions are given in the DEFINITIONS (Full Definitions) Field. An independent claim is included for the preparation of protected compounds of formula (IV) comprising reacting a carboxylic acid of formula (II) with a carboxylic acid of formula (III), in the presence of a coupling agent and a base in inert solvent. [Image] PG : protecting group. - ACTIVITY : Antiarteriosclerotic; antiasthmatic; antiallergic; antiinflammatory; antidiabetic; neuroprotective; antirheumatic; antiarthritic; immunosuppressive. - MECHANISM OF ACTION : Integrin antagonists. In-vitro assays were carried out to determine adhesion of Jurkat or Ramos cells to immobilized VCAM-1 (domains 1-3). Test compounds typically had IC50 values less than 0.5 MicroM to 10 MicroM.
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Inventors:
Lehman, Thomas
Fisher, Liyudaigar
Albers, Marx
Lele, Thomas
Micheller, Gerhard
Hessler, Gerhard
Tajimi Masaomi
Carl Twigelbauer
Hiromi Okigami
Kevin, bacon
Haruki Hasegawa
Fisher, Liyudaigar
Albers, Marx
Lele, Thomas
Micheller, Gerhard
Hessler, Gerhard
Tajimi Masaomi
Carl Twigelbauer
Hiromi Okigami
Kevin, bacon
Haruki Hasegawa
Application Number:
JP2001578395A
Publication Date:
October 21, 2003
Filing Date:
April 09, 2001
Export Citation:
Assignee:
Bayer Aktiengesellschaft
International Classes:
C07D215/08; A61K31/185; A61K31/192; A61K31/198; A61K31/216; A61K31/222; A61K31/27; A61K31/405; A61K31/41; A61K31/426; A61K31/433; A61P1/04; A61P3/10; A61P9/00; A61P9/10; A61P11/06; A61P25/28; A61P29/00; A61P37/00; A61P37/04; A61P37/08; A61P43/00; C07C237/20; C07C271/22; C07C273/18; C07C275/42; C07D209/42; C07D215/48; C07D257/04; C07D277/20; C07D277/46; C07D285/12; C07D285/135; (IPC1-7): C07C275/42; A61K31/185; A61K31/192; A61K31/198; A61K31/216; A61K31/222; A61K31/27; A61K31/405; A61K31/41; A61K31/426; A61K31/433; A61P1/04; A61P3/10; A61P9/00; A61P9/10; A61P11/06; A61P25/28; A61P29/00; A61P37/00; A61P37/04; A61P37/08; A61P43/00; C07C273/18; C07D209/42; C07D215/08; C07D257/04; C07D277/46; C07D285/12
Attorney, Agent or Firm:
Heiyoshi Odashima
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