Title:
複素環式アスパルチルプロテアーゼインヒビター
Document Type and Number:
Japanese Patent JP2008523059
Kind Code:
A
Abstract:
Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(═S)—, —S(O)—, —S(O)2—, —C(═O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(═N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(═O)— or —C(═NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(═NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist.
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Inventors:
Ju, Chao Ninh
Macrickrick, brian
Sun, Chung-You
Ye, Yuan Trang Si.
Voight, Johannes H.
Strickland, Collie
Smith, Elizabeth M.
Andrew Stanford
Greenlee, William Jay.
Robert, Mazzola
John Caldwell
Cumming, jared
Wang, Lin Yang
Wu, Yushen
Iserlo, Würich
Guo, Tao
Les, Tui X. H.
Scions, Kurt W.
Bab, Suresh Dee.
Hunter, Rachel Sea.
Morris, Michael El.
Gu, Hoichon
Chien, gun
Tadesse, Dawitt
Macrickrick, brian
Sun, Chung-You
Ye, Yuan Trang Si.
Voight, Johannes H.
Strickland, Collie
Smith, Elizabeth M.
Andrew Stanford
Greenlee, William Jay.
Robert, Mazzola
John Caldwell
Cumming, jared
Wang, Lin Yang
Wu, Yushen
Iserlo, Würich
Guo, Tao
Les, Tui X. H.
Scions, Kurt W.
Bab, Suresh Dee.
Hunter, Rachel Sea.
Morris, Michael El.
Gu, Hoichon
Chien, gun
Tadesse, Dawitt
Application Number:
JP2007545436A
Publication Date:
July 03, 2008
Filing Date:
June 09, 2005
Export Citation:
Assignee:
Schering Corporation
International Classes:
C07D233/46; A61K31/4168; A61K31/4178; A61K31/4184; A61K31/422; A61K31/4245; A61K31/427; A61K31/428; A61K31/4375; A61K31/4425; A61K31/4439; A61K31/454; A61K31/4545; A61K31/4709; A61K31/4725; A61K31/497; A61K31/506; A61K31/513; A61K31/519; A61K31/5377; A61K31/5395; A61K31/541; A61K45/00; A61P9/00; A61P9/12; A61P13/12; A61P25/00; A61P25/28; A61P31/18; A61P33/02; A61P33/06; A61P35/00; A61P43/00; C07D233/88; C07D239/22; C07D271/06; C07D273/04; C07D401/04; C07D401/10; C07D401/12; C07D401/14; C07D403/04; C07D403/06; C07D403/12; C07D405/06; C07D409/04; C07D409/10; C07D409/14; C07D413/06; C07D413/10; C07D413/12; C07D417/06; C07D417/10; C07D417/12; C07D417/14; C07D471/04; C07D487/04; A61K31/192; A61K31/40
Domestic Patent References:
| JP2003522739A | 2003-07-29 |
Foreign References:
| WO1990004917A1 | 1990-05-17 |
Attorney, Agent or Firm:
Hidesaku Yamamoto
Takaaki Yasumura
Natsuki Morishita
Takaaki Yasumura
Natsuki Morishita