Title:
【発明の名称】タンパク質イソプレニルトランスフェラーゼの阻害剤
Document Type and Number:
Japanese Patent JP2002518985
Kind Code:
A
Abstract:
Compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L2-, and (i) heterocyclic -L2-; R2 is selected from (a) Formula (Ia), (b) -C(O)NH-CH(R14)-C(O)OR15, (c) Formula (Ib), (d) -C(O)NH-CH(R14)-C(O)NHSO2R16, (e) -C(O)NH-CH(R14)-tetrazolyl, (f) -C(O)NH-heterocyclic, and (g) -C(O)NH-CH(R14)-C(O)NR17R18; R3 is heterocyclic, aryl, substituted or unsubstituted cycloalkyl; R4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylalkyl, heterocyclic, or (heterocyclic)alkyl; L1 is absent or is selected from (a) -L4-N(R5)-L5-, (b) -L4-O-L5-, (c) -L4-S(O)n-L5-, (d) -L4-L6-C(W)-N(R5)-L5-, (e) -L4-L6-S(O)m-N(R5)-L5-, (f) -L4-N(R5)-C(W)-L7-L5-, (g) -L4-N(R5)-S(O)p-L7-L5-, (h) optionally substituted alkylene, (i) optionally substituted alkenylene, and (j) optionally substituted alkynylene are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases.
Inventors:
Sebuchi, Sed M
Hamilton, Andrew Dee
Augeri, David Jay
Bar, Kenneth Jay
Donor Bernard Gee
Fak Holy, Stephen A
Yanovic, David A
Calvin, Douglas M
Larsen, John Jay
Riu, cancer
O'Connor, Stephen Jay
Rosenberg, Saul H
Shen, Wan
Swenson, Rolf Yee
Sorensen, Brian Kay
Sullivan, Gerrard M
Suzuze Pankey Bits, Bruce Gee
Tasker, Andrew S
Wassic, James Eye
Win, martin
Hamilton, Andrew Dee
Augeri, David Jay
Bar, Kenneth Jay
Donor Bernard Gee
Fak Holy, Stephen A
Yanovic, David A
Calvin, Douglas M
Larsen, John Jay
Riu, cancer
O'Connor, Stephen Jay
Rosenberg, Saul H
Shen, Wan
Swenson, Rolf Yee
Sorensen, Brian Kay
Sullivan, Gerrard M
Suzuze Pankey Bits, Bruce Gee
Tasker, Andrew S
Wassic, James Eye
Win, martin
Application Number:
JP54848098A
Publication Date:
June 25, 2002
Filing Date:
May 07, 1998
Export Citation:
Assignee:
University of Pittsburgh
International Classes:
C07D295/12; A61K31/198; A61K31/223; A61K31/341; A61K31/343; A61K31/357; A61K31/36; A61K31/381; A61K31/40; A61K31/404; A61K31/415; A61K31/4152; A61K31/4184; A61K31/42; A61K31/423; A61K31/426; A61K31/4402; A61K31/4406; A61K31/445; A61K31/4453; A61K31/4458; A61K31/472; A61K31/4965; A61K31/4985; A61K31/505; A61K31/5375; A61K31/7028; A61P9/10; A61P35/00; A61P43/00; C07C237/36; C07C239/20; C07C271/22; C07C317/50; C07C323/16; C07C323/59; C07C323/60; C07C327/42; C07D205/04; C07D207/08; C07D207/09; C07D207/10; C07D207/12; C07D207/14; C07D207/16; C07D207/26; C07D207/267; C07D209/14; C07D209/40; C07D209/48; C07D211/14; C07D211/22; C07D211/42; C07D211/52; C07D211/58; C07D211/60; C07D211/90; C07D213/30; C07D213/32; C07D213/36; C07D213/38; C07D213/56; C07D213/64; C07D213/65; C07D213/68; C07D213/70; C07D213/71; C07D213/74; C07D213/75; C07D213/76; C07D217/26; C07D231/38; C07D231/48; C07D233/54; C07D233/64; C07D235/06; C07D235/08; C07D237/14; C07D237/20; C07D239/26; C07D239/42; C07D241/04; C07D241/12; C07D241/18; C07D241/20; C07D241/24; C07D253/06; C07D257/04; C07D261/02; C07D261/14; C07D263/22; C07D263/24; C07D263/32; C07D265/30; C07D275/02; C07D277/04; C07D277/06; C07D277/20; C07D277/22; C07D277/26; C07D277/28; C07D277/30; C07D277/34; C07D277/36; C07D277/42; C07D277/46; C07D277/48; C07D277/50; C07D277/66; C07D279/12; C07D285/12; C07D285/135; C07D295/084; C07D295/13; C07D295/155; C07D295/185; C07D307/52; C07D307/54; C07D307/66; C07D307/81; C07D309/04; C07D309/14; C07D317/30; C07D317/58; C07D317/60; C07D317/66; C07D319/06; C07D319/08; C07D319/18; C07D333/18; C07D333/20; C07D333/24; C07D335/04; C07D471/04; C07D487/08; C07F9/53; C07H15/18; (IPC1-7): C07C323/59; A61K31/198; A61K31/223; A61K31/341; A61K31/343; A61K31/357; A61K31/36; A61K31/381; A61K31/40; A61K31/404; A61K31/415; A61K31/4152; A61K31/4184; A61K31/42; A61K31/423; A61K31/426; A61K31/4402; A61K31/4406; A61K31/445; A61K31/4453; A61K31/4458; A61K31/472; A61K31/4965; A61K31/4985; A61K31/505; A61K31/5375; A61K31/7028; A61P9/10; A61P35/00; A61P43/00; C07C317/50; C07C323/16; C07C323/60; C07D207/09; C07D207/12; C07D207/14; C07D207/16; C07D207/26; C07D209/14; C07D209/40; C07D211/22; C07D211/58; C07D211/60; C07H15/18
Domestic Patent References:
| JP2001501577A | 2001-02-06 | |||
| JP2001500118A | 2001-01-09 | |||
| JP2001509156A | 2001-07-10 | |||
| JP2000500745A | 2000-01-25 |
Foreign References:
| WO1997006138A1 | 1997-02-20 | |||
| WO1996021456A1 | 1996-07-18 | |||
| WO1995025086A1 | 1995-09-21 |
Attorney, Agent or Firm:
Takehiko Suzue (4 outside)