发明名称 THIADIAZOLE AND OXADIAZOLE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS
摘要 A compound of formula (I) or a pharmaceutically acceptable salt or prodrug thereof: wherein X is an oxygen or sulphur atom A is CH(R<SUP>6</SUP>)-, -O- or NR<SUP>7 </SUP>or when A is NR<SUP>7</SUP>, then R<SUP>1</SUP> and NR<SUP>7</SUP> can together form a ring such that R<SUP>1</SUP> and R<SUP>7</SUP> are (CH<SUB>2</SUB>)<SUB>n</SUB>, where n is 2-4, preferably 2-3; Y is a bond, CH(R<SUP>6</SUP>)-, -O- or NR<SUP>7</SUP> or A and Y together form a single bond between the aromatic group and the carbonyl group but when A is-O- then Y is not -O-; R<SUP>1</SUP> and R<SUP>2</SUP> are independently hydrogen, halogen, OR<SUP>8</SUP>, NR<SUP>9</SUP>R<SUP>10</SUP>, NR<SUP>9</SUP>COR<SUP>11</SUP>, NR<SUP>9</SUP>SO<SUB>2</SUB>R<SUP>11</SUP> or C<SUB>1-6</SUB>alkyl optionally substituted by fluorine, hydroxyl, C<SUB>1-6</SUB> alkoxy or NR<SUP>9</SUP>R<SUP>10</SUP>; R<SUP>3 </SUP> is C<SUB>1-6</SUB> alkyl, C<SUB>3-8</SUB> cycloalkyl C<SUB>4-10</SUB> alkylcycloalkyl optionally substituted by hydroxyl, C<SUB>1-6</SUB> alkoxy or NR<SUP>9</SUP>R<SUP>10</SUP>; R<SUP>4</SUP> is hydrogen, halogen, CF<SUB>3</SUB>, OR<SUP>9</SUP>, NR<SUP>9</SUP>R<SUP>10</SUP>, NR<SUP>9</SUP>COR<SUP>11</SUP>, NR<SUP>9</SUP>SO<SUB>2</SUB>R<SUP>11</SUP> or C<SUB>1-6</SUB> alkyl optionally substituted by hydroxyl, C<SUB>1-6</SUB> alkoxy or NR<SUP>9</SUP>R<SUP>10</SUP>; R<SUP>5</SUP> is hydrogen, halogen, CF<SUB>3</SUB>, OR<SUP>8</SUP>, COOR<SUP>9</SUP>, CONR<SUP>9</SUP>R<SUP>10</SUP> or SO<SUB>2</SUB>R<SUP>11</SUP>; The compounds find use in the treatment of amyloid related diseases, such as Alzheimer disease.
申请公布号 WO2008107677(A3) 申请公布日期 2008.10.30
申请号 WO2008GB00761 申请日期 2008.03.06
申请人 SENEXIS LIMITED;SCOPES, DAVID, IAN, CARTER;CHEESERIGHT, TIMOTHY, JOHN;VINTER, JEREMY, GILBERT 发明人 SCOPES, DAVID, IAN, CARTER;CHEESERIGHT, TIMOTHY, JOHN;VINTER, JEREMY, GILBERT
分类号 C07D285/135;A61K31/433;A61P25/16;A61P25/28;C07D271/113 主分类号 C07D285/135
代理机构 代理人
主权项
地址