US 6,441,212 B1Granted

Silanol enzyme inhibitors

AssigneeThe Research Foundation of State University of New York

InventorsScott McN. Sieburth, Alfred M. Mutahi, Chien-An Chen

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Abstract

Compounds of formula (I, II, or III), wherein X is OH; Y is OH, H, lower alkyl of one to six carbons or heteroatoms or F; Z and Z′ are independently H, lower alkyl or Q3Si where Q is lower alkyl or aryl; n is 3-50; n′ is 2-50, A and B are independently a) alkyl of one to ten carbons or heteroatoms, b) aryl of four to ten carbons or heteroatoms, c) cyclic of three to ten carbons or heteroatoms, or moieties of the formulas (d, e, or f); R1-R11 groups are each independently hydrogen, alkyl of one to ten carbons or heteoatoms aryl of 4 to 14 carbons or heteroatoms, arylalkyl of five to twenty carbons or heteroatoms; unsubstituted carbonyl or substituted carbonyl. Heteroatoms are nitrogen, oxygen, silicon or sulfur. At least one of A or B, or both A and B are d), e), or f). The compounds of formula (I) inhibit protease enzymes and can be used as pharmaceuticals.

Claims4

Dependent claims

A Human Immunodeficiency Virus (HIV) protease inhibitor of formula II

in which
n is 3 to 50;
formula II is a stable molecule;
each of A and B is independently
a) a C3-C10-alkyl, or a substituent obtained by substituting at least one carbon atom of a C3-C10-alkyl group with a heteroatom;
b) a C4-C7-aryl, or a substituent obtained by substituting at least one carbon atom of a C4-C7-aryl group with a heteroatom;
c) a C3-C10-carbocyclic moiety, or a 3-10-membered heterocyclic group;
or moieties of the formulas
wherein in d), e) and f), CH is bonded to silicon;
and
wherein R1 to R11 are independently hydrogen, alkyl of 1 to 10 carbons or heteroatoms, aryl of 4 to 14 carbons or heteroatoms, arylalkyl of 5 to 20 carbons or heteroatoms, or a substituted carbonyl;
wherein each of said heteroatoms is selected from the group consisting of nitrogen, oxygen, silicon and sulfur, and at least one of A and B, or both of A and B, are selected from a group consisting of d), e) and f).

9 more elements

Dependencies are inferred from the claim text.

Facts

Application: 09/194,715Filed 17 Dec 1998 · division
Priority: 12 Jul 1996
Granted: 27 Aug 2002
Term ends: Not estimatedThe source records don’t support an estimate.

Classification7 codes

C07F 7/0836
Compounds having one or more O-Si linkage: compounds with one or more Si-OH or Si-O-metal linkage
A61P 43/00
Drugs for specific purposes, not provided for in groups a61p1/00-a61p41/00
C07F 7/081
Compounds with Si-C or Si-Si linkages: comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
C07F 7/0838
Compounds having one or more O-Si linkage: compounds with one or more Si-O-Si sequences