Title:
TRYPTASE INHIBITORS
Document Type and Number:
WIPO Patent Application WO1999040073
Kind Code:
A3
Abstract:
The invention relates to bifunctional inhibitors of human tryptase of formula (I), to human tryptase in crystalline form, to a method for producing human tryptase in crystalline form, to pharmaceutical compositions comprising a bifunctional inhibitor of human tryptase, and to a method for developing and identifying tryptase inhibitors. The tryptase inhibitors are characterized in that both head groups K1 and K2 are the same or different and each comprises a group Q which can interact with a carboxylate group. The linker L can assume a conformation such that the groups Q of both head groups are situated at a distance ranging from 20 to 45 ANGSTROM , such that the dimension of the head groups and of the linker permit the inhibitor to penetrate into a cavity with the dimensions 52 ANGSTROM X 32 ANGSTROM X 40 ANGSTROM , and such that L represents formula (II) wherein A1 and A2 are the same or different, and represent -C(O)-, NH-, -O- (oxygen), -S- (sulfur), -S(O)2-, -S(O)2-NH-, -NH-S(O)2-, -C(O)-NH-, -NH-C(O)-, -O-C(O)-, -C(O)-O- or a bond. A3 and A4 are the same or different and represent -C(O)-, -C(S)-, -O-, -S-, -NH-, -O-C(O)-, -C(O)-O-, -C(O)-NH-, -NH-C(O)- or a bond, or are selected from the group A5, A6, M, B1-B6 as stated in the description.
Inventors:
BODE WOLFRAM (DE)
MORODER LUIS (DE)
PEREIRA PEDRO JOSE BARBOSA (DE)
BERGNER ANDREAS (DE)
HUBER ROBERT (DE)
SOMMERHOFF CHRISTIAN (DE)
SCHASCHKE NORBERT (DE)
BAER THOMAS (DE)
MARTIN THOMAS (DE)
STADLWIESER JOSEF (DE)
ULRICH WOLF-RUEDIGER (DE)
DOMINIK ANDREAS (DE)
THIBAUT ULRICH (DE)
BUNDSCHUH DANIELA (DE)
BEUME ROLF (DE)
GOEBEL KARL-JOSEF (DE)
MORODER LUIS (DE)
PEREIRA PEDRO JOSE BARBOSA (DE)
BERGNER ANDREAS (DE)
HUBER ROBERT (DE)
SOMMERHOFF CHRISTIAN (DE)
SCHASCHKE NORBERT (DE)
BAER THOMAS (DE)
MARTIN THOMAS (DE)
STADLWIESER JOSEF (DE)
ULRICH WOLF-RUEDIGER (DE)
DOMINIK ANDREAS (DE)
THIBAUT ULRICH (DE)
BUNDSCHUH DANIELA (DE)
BEUME ROLF (DE)
GOEBEL KARL-JOSEF (DE)
Application Number:
PCT/EP1999/000727
Publication Date:
November 11, 1999
Filing Date:
February 04, 1999
Export Citation:
Assignee:
MAX PLANCK GESELLSCHAFT (DE)
BYK GULDEN LOMBERG CHEM FAB (DE)
BODE WOLFRAM (DE)
MORODER LUIS (DE)
PEREIRA PEDRO JOSE BARBOSA (DE)
BERGNER ANDREAS (DE)
HUBER ROBERT (DE)
SOMMERHOFF CHRISTIAN (DE)
SCHASCHKE NORBERT (DE)
BAER THOMAS (DE)
MARTIN THOMAS (DE)
STADLWIESER JOSEF (DE)
ULRICH WOLF RUEDIGER (DE)
DOMINIK ANDREAS (DE)
THIBAUT ULRICH (DE)
BUNDSCHUH DANIELA (DE)
BEUME ROLF (DE)
GOEBEL KARL JOSEF (DE)
BYK GULDEN LOMBERG CHEM FAB (DE)
BODE WOLFRAM (DE)
MORODER LUIS (DE)
PEREIRA PEDRO JOSE BARBOSA (DE)
BERGNER ANDREAS (DE)
HUBER ROBERT (DE)
SOMMERHOFF CHRISTIAN (DE)
SCHASCHKE NORBERT (DE)
BAER THOMAS (DE)
MARTIN THOMAS (DE)
STADLWIESER JOSEF (DE)
ULRICH WOLF RUEDIGER (DE)
DOMINIK ANDREAS (DE)
THIBAUT ULRICH (DE)
BUNDSCHUH DANIELA (DE)
BEUME ROLF (DE)
GOEBEL KARL JOSEF (DE)
International Classes:
A61K31/165; A61K31/44; A61K31/4402; A61K31/4418; A61K31/4427; A61K31/445; A61K31/4468; A61K31/4545; A61K31/495; A61K31/496; A61K31/4985; C07D295/20; A61P1/02; A61P11/06; A61P17/00; A61P17/06; A61P19/06; A61P27/16; A61P29/00; A61P37/08; A61P43/00; C07C237/10; C07C237/22; C07C279/16; C07C279/18; C07D211/58; C07D213/81; C07D213/82; C07D241/08; C07D295/185; C07D295/215; C07D401/14; C07D487/14; (IPC1-7): C07D295/20; A61K31/495; C07D211/58; A61K31/445; C07C279/18; A61K31/155; C07C237/10; A61K31/16; C07D213/81; A61K31/44; C07D213/82
Domestic Patent References:
| WO1998004537A1 | 1998-02-05 | |||
| WO1997037969A1 | 1997-10-16 | |||
| WO1995032945A1 | 1995-12-07 | |||
| WO1996009297A1 | 1996-03-28 |
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