PHOSPHODIESTERASE-V MODULATOR DRUGS AND THEIR USES

WIPO Patent Application WO1999064033

A9

This invention relates to novel multibinding compounds that bind to the enzyme phosphodiesterase V (PDE V) and modulate its activity. The compounds of this invention comprise 2-10 PDE V modulator (particularly inhibitor) ligands covalently connected by a linker or linkers, wherein the ligands in their monovalent (i.e., unlinked) state bind to a PDE V enzyme. The manner of linking the ligands together is such that the multibinding agents thus formed demonstrate an increased biologic and/or therapeutic effect as compared to the same number of unlinked ligands made available for binding to PDE V. The invention also relates to methods of using such compounds and to methods of preparing them. The compounds of this invention are particularly useful for treating diseases and conditions of mammals that are mediated by PDE V. Accordingly, this invention also relates to pharmaceutical compositions comprising a pharmaceutically acceptable excipient and an effective amount of a compound of this invention.

KLEIN UWE (US)
ZHU YAN (US)
GRIFFIN JOHN H (US)

PCT/US1999/011800

July 27, 2000

June 07, 1999

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ADVANCED MEDICINE INC (US)
KLEIN UWE (US)
ZHU YAN (US)
GRIFFIN JOHN H (US)

C07D499/44; A01N57/34; A61K31/00; A61K31/357; A61K31/397; A61K31/407; A61K31/421; A61K31/424; A61K31/431; A61K31/439; A61K31/444; A61K31/4545; A61K31/496; A61K31/522; A61K31/536; A61K31/5377; A61K31/546; A61K31/551; A61K31/65; A61K31/7028; A61K31/7034; A61K31/7036; A61K31/7042; A61K31/7048; A61K31/7052; A61K31/7056; A61K31/7064; A61K31/7068; A61K31/7072; A61K38/00; A61K39/00; A61K39/395; A61K39/44; A61K47/48; A61K51/00; A61P31/04; A61P31/18; A61P43/00; C07C233/36; C07C233/78; C07C237/24; C07C237/26; C07C271/20; C07C275/42; C07C321/04; C07C323/12; C07C335/08; C07C335/32; C07D207/333; C07D211/58; C07D215/56; C07D233/90; C07D235/30; C07D263/28; C07D265/18; C07D401/06; C07D401/12; C07D401/14; C07D405/04; C07D413/14; C07D453/02; C07D471/04; C07D471/14; C07D473/00; C07D473/34; C07D475/04; C07D475/08; C07D477/00; C07D487/04; C07D487/06; C07D493/04; C07D493/06; C07D495/04; C07D498/04; C07D498/18; C07D501/20; C07D519/00; C07H15/236; C07H15/238; C07H15/26; C07H17/08; C07H19/06; C07H19/20; C07K2/00; C07K4/00; C12N9/99; C12P19/38; C12Q1/26; C12Q1/44; C12Q1/48; C12Q1/533; C40B30/04; C40B40/04; G01N33/15; G01N33/50; G01N33/53; G01N33/543; G01N33/566; G01N33/573; G01N33/68; G01N33/92; G01N37/00; C07B61/00; C07D207/32; (IPC1-7): A61K38/00; A61K39/00; A61K39/44; A61K39/395; A61K51/00; C07K2/00; C07K4/00; G01N33/53; G01N33/543; G01N33/566

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