IP Library Granted Patent US 8,759,323
Granted Patent B2
US 8,759,323 · App. 13/123,166 · Granted Jun 24, 2014

Protein phosphatase inhibitor

Inventors: Kazuyasu Sakaguchi (Sapporo, JP); Keiji Tanino (Sapporo, JP); Yoshiro Chuman (Sapporo, JP); Fumihiko Yoshimura (Sapporo, JP); Hiroaki Yagi (Sapporo, JP)
Assignee: LSIP, LLC
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Quick Facts
Patent No.
US 8,759,323
App. No.
13/123,166
Granted
Jun 24, 2014
Kind
B2
Abstract

Provided is a novel protein phosphatase inhibitor. The protein phosphatase inhibitor contains, as an active ingredient, a silicon compound represented by the following general formula (1) or a salt thereof, wherein R 1 , R 2 and R 3 are the same or different and represent a hydrocarbon group having 1 to 12 carbon atoms; X represents an optionally substituted hydrocarbon group having 3 to 36 carbon atoms or an optionally substituted heterocyclic group; and n represents an integer of 0 or 1.

Claims (12)

1. A silicon compound represented by the formula (2) or a salt thereof:

wherein R 4 and R 5 are the same or different and represent a hydrogen atom or (R 1 )(R 2 )(R 3 )Si—, wherein at least one of R 4 and R 5 is (R 1 )(R 2 )(R 3 )Si—;

R 1 , R 2 , and R 3 are the same or different and represent a hydrocarbon group having 1 to 12 carbon atoms;

R 6 represents a hydrogen atom or optionally forms —O-(ether bond) together with the hydroxyl group of R 8 ; and

R 7 represents a hydrogen atom and R 8 represents a hydroxyl group, or R 7 and R 8 optionally together form an oxo group (═O).

2. The silicon compound or the salt thereof according to claim 1 , wherein the silicon compound is represented by the following formula (2-1), (2-2), or (2-3):

wherein R 4 , R 5 , R 6 and R 8 are as defined above, or a salt thereof.

3. The silicon compound or the salt thereof according to claim 1 , wherein R 1 , R 2 , and R 3 are the same or different and represent linear or branched alkyl group having 1 to 8 carbon atoms, an aromatic hydrocarbon group having 6 to 14 carbon atoms, or a C 6-10 aryl-C 1-6 alkyl group.

4. The silicon compound or the salt thereof according to claim 1 , wherein (R 1 )(R 2 )(R 3 )Si— is selected from the group consisting of a trimethylsilyl group, a triethylsilyl group, a tri(n-propyl)silyl group, a triisopropylsilyl group, a tri(n-butyl)silyl group, a tri(sec-butyl)silyl group, a triisobutylsilyl group, a tert-butyldimethylsilyl group, a dimethylphenylsilyl group, a methyldiphenylsilyl group, a triphenylsilyl group, and a tert-butyldiphenylsilyl group.

5. A composition comprising the silicon compound or the salt thereof according to claim 1 , and a pharmaceutically acceptable carrier.

6. A protein phosphatase inhibitor comprising the silicon compound or the salt thereof according to claim 1 .

7. The protein phosphatase inhibitor according to claim 6 , wherein the protein phosphatase inhibitor is a PPM1D inhibitor.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 7, 2011
From: SAKAGUCHI, KAZUYASU; TANINO, KEIJI; CHUMAN, YOSHIRO; YOSHIMURA, FUMIHIKO; YAGI, HIROAKI
To: LSIP, LLC
Reel/Frame 026403/0955 →
Priority Claims (1)
JP 2008-262646 · Oct 9, 2008 · national
Continuity (1)
Related Publication 20110288050A1 · Nov 24, 2011