[EN] NITROGEN- HETEROCYCLIC COMPOUNDS AS PHOSPHODIESTERASE 10 INHIBITORS<br/>[FR] COMPOSÉS AZOTÉS HÉTÉROCYCLIQUES CONVENANT COMME INHIBITEURS DE LA PHOSPHODIESTÉRASE 10
申请人:AMGEN INC
公开号:WO2011143129A1
公开(公告)日:2011-11-17
Aryl- and heteroaryl-nitrogen heterocyclic compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDEIO, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.
The present invention relates to ester, ether and N-alkylcarbamoyl derivatives of compound (Ia) and pharmaceutically acceptable salts thereof. These compounds exhibit excellent antibacterial activity and are useful for the treatment or prevention of bacterial infections.
1
(wherein R
1
is a hydrogen atom or a methyl group; R
2
a
is a hydrogen atom, a protecting group for a hydroxy group, or a methyl group; R
3
is a hydrogen atom or a protecting group for a hydroxy group; R
4
a
is a hydrogen atom, a hydroxy group or a protected hydroxy group; R
5
is a hydrogen atom or a protecting group for a hydroxy group; and X is a methylene group or a sulfur atom). The invention also includes compounds which are related to the aforeidentified compounds.
ARYL- AND HETEROARYL- NITROGEN-HETEROCYCLIC COMPOUNDS AS PDE10 INHIBITORS
申请人:Allen Jennifer R.
公开号:US20110306590A1
公开(公告)日:2011-12-15
Aryl- and heteroaryl-nitrogen heterocyclic compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.
THIAZOLIDINONE COMPOUNDS OR ANGINA PECTORIS REMEDY OR PREVENTIVE CONTAINING THE SAME AS ACTIVE INGREDIENT
申请人:SANKYO COMPANY LIMITED
公开号:EP0798298A1
公开(公告)日:1997-10-01
[Constitution]
Thiazolidinone compounds having the general formula:
[wherein W represents a sulfur atom or an oxygen atom, and X represents a group having the formula: -N(R1)-; or
X represents a sulfur atom or an oxygen atom, and W represents a group having the formula: -N(R1)-;
R1 represents a hydrogen atom, an alkyl group or a substituted alkyl group;
R2 and R3 may be the same or different and each represents a hydrogen atom, an alkyl group, a substituted alkyl group, an aryl group or a 5- or 6-membered aromatic heterocyclic group;
R4 represents a hydrogen atom, an alkyl group or a substituted C1-C4 alkyl group;
R5 represents a substituted cycloalkyl group optionally containing a nitrogen atom [said substituent is essentially a group having the formula: -B-ONO2 (wherein B represents a single bond or an alkylene group) and optionally an alkyl group]; and
A represents a single bond or an alkylene group; ] or pharmacologically acceptable salts thereof.
[Effect]
The compounds have an excellent anti-angina pectoris action and are useful as a therapeutic or preventing agent for angina pectoris.
[组织结构]
通式如下的噻唑烷酮化合物
[其中 W 代表硫原子或氧原子,X 代表具有以下通式的基团:-N(R1)-;或
X 代表硫原子或氧原子,而 W 代表具有以下式子的基团:-N(R1)-;
R1 代表氢原子、烷基或取代烷基;
R2 和 R3 可以相同或不同,各自代表氢原子、烷基、取代烷基、芳基或 5 或 6 元芳香杂环基团;
R4 代表氢原子、烷基或取代的 C1-C4 烷基;
R5 代表可选含有一个氮原子的取代环烷基[所述取代基基本上是具有以下式子的基团:-B-ONO2(其中 B 代表单键或亚烷基)和可选的烷基];和
A 代表单键或亚烷基; ]或其药理学上可接受的盐。
效果
这些化合物具有很好的抗心绞痛作用,可作为心绞痛的治疗剂或预防剂。
Novel antibacterial compounds
申请人:Sankyo Company, Limited
公开号:EP1319406A1
公开(公告)日:2003-06-18
The use of compounds of formula (I), defined herein, or pharmaceutically acceptable salts thereof, or of pharmaceutically acceptable esters, ethers or N-alkylcarbamoyl derivatives of compounds of formula (Ia), defined herein, or phamaceutically acceptable salts thereof in the manufacture of a medicament for the treatment or prevention of a bacterial infection caused by Mycobacterium bacteria is disclosed. The invention further provides the use of capuramycin in the manufacture of a medicament for the treatment or prevention of a bacterial infection caused by Mycobacterium tuberculosis bacteria.