New pyridine analogues

A compound, C1-C12 technology, applied in the field of pyridine compounds, can solve the problems of acute thrombosis and high morbidity

Inactive Publication Date: 2008-09-10
ASTRAZENECA AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Although the process of platelet adhesion to the subendothelial surface may play an important role in repairing damaged vessel walls, the resulting platelet aggregation can contribute to acute thrombotic occlusion of vascular beds in vital organs, resulting in a high incidence of events such as myocardial infarction and unstable angina

Method used

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  • New pyridine analogues
  • New pyridine analogues
  • New pyridine analogues

Examples

Experimental program
Comparison scheme
Effect test

no. 2 approach

[0092] A second embodiment of formula I is defined as follows:

[0093] R 1 means R 6 OC(O), R 7 C(O), R 16 SC(O), R 17 S, R 18 C(S) or group gII:

[0094]

[0095] R 2 Indicates H, CN, NO 2 , (C optionally interrupted by oxygen and / or optionally substituted by OH, aryl, cycloalkyl, heterocyclyl or one or more halogen (F, Cl, Br, I) atoms 1 -C 6 ) alkyl; In addition, R 2 represents (C optionally substituted by one or more halogen (F, Cl, Br, I) atoms 1 -C 6 ) alkoxy; In addition, R 2 Indicates (C 3 -C 6 ) cycloalkyl, hydroxyl (C 1 -C 6 ) Alkyl, (C 1 -C 6 ) Alkyl C (O), (C 1 -C 6 ) Alkylthio C (O), (C 1 -C 6 ) Alkyl C(S), (C 1 -C 6 ) alkoxy C (O), (C 3 -C 6 ) cycloalkoxy, aryl, aryl C (O), aryl (C 1 -C 6 ) Alkyl C (O), heterocyclyl, heterocyclyl C (O), heterocyclyl (C 1 -C 6 ) Alkyl C (O), (C 1 -C 6 ) Alkylsulfinyl, (C 1 -C 6 ) Alkylsulfonyl, (C 1 -C 6 ) Alkylthio, (C 3 -C 6 ) cycloalkylthio, arylsulfinyl, arylsulfonyl, arylthio, aryl (C...

no. 3 approach

[0114] A third embodiment of formula I is defined as follows:

[0115] R 1 means R 6 OC(O), R 16 SC(O) or group gII:

[0116]

[0117] R 2 Indicates H, CN, NO 2 , (C optionally interrupted by oxygen and / or optionally substituted by OH, aryl, cycloalkyl, heterocyclyl or one or more halogen (F, Cl, Br, I) atoms 1 -C 6 ) alkyl; In addition, R 2 represents (C optionally substituted by one or more halogen (F, Cl, Br, I) atoms 1 -C 6 ) alkoxy; In addition, R 2 Indicates (C 3 -C 6 ) cycloalkyl, hydroxyl (C 1 -C 6 ) Alkyl, (C 1 -C 6 ) Alkyl C (O), (C 1 -C 6 ) Alkylthio C (O), (C 1 -C 6 ) Alkyl C(S), (C 1 -C 6 ) alkoxy C (O), (C 3 -C 6 ) cycloalkoxy, aryl, aryl C (O), aryl (C 1 -C 6 ) Alkyl C (O), heterocyclyl, heterocyclyl C (O), heterocyclyl (C 1 -C 6 ) Alkyl C (O) or formula NR a(2) R b(2) group, where R a(2) and R b(2) Independently represent H, (C 1 -C 6 ) Alkyl, (C 1 -C 6 ) alkyl C (O), or R a(2) and R b(2) together with a nitrogen atom rep...

no. 4 approach

[0132] A fourth embodiment of formula I is defined as follows:

[0133] R 1 means R 6 OC(O), R 16 SC(O) or group gII:

[0134]

[0135] R 2 represents H or (C optionally interrupted by oxygen and / or optionally substituted by OH, aryl, cycloalkyl, heterocyclyl or one or more halogen (F, Cl, Br, I) atoms 1 -C 6 ) alkyl; In addition, R 2 Expression NR a(2) R b(2) group, where R a(2) and R b(2) Independently represent H, (C 1 -C 6 ) Alkyl, (C 1 -C 6 ) alkyl C (O), or R a(2) and R b(2) together with a nitrogen atom represents piperidine, pyrrolidine, azetidine or aziridine;

[0136] R 3 Represents H or formula NR a(3) R b(3) group, where R a(3) and R b(3) Independently represent H, (C 1 -C 6 ) Alkyl, (C 1 -C 6 ) alkyl C (O), or R a(3) and R b(3) together with a nitrogen atom represents piperidine, pyrrolidine, azetidine or aziridine;

[0137] R 4 Indicates CN, halogen (F, Cl, Br, I), in addition, R 4 Indicates (C 1 -C 6 ) Alkyl C (O), (C 1 -C 6 ...

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Abstract

The present invention relates to certain new pyridin analogues of Formula (I) Chemical formula should be inserted here. Please see paper copy Formula (I) to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-trombotic agents etc, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.

Description

field of invention [0001] The present invention provides novel pyridine compounds, their use as medicaments, compositions comprising them and processes for their preparation. Background of the invention [0002] Platelet adhesion and aggregation are initiating events in arterial thrombosis. Although the process of platelet adhesion to the subendothelial surface may play an important role in repairing damaged vessel walls, the resulting platelet aggregation can contribute to acute thrombotic occlusion of vascular beds in vital organs, resulting in a high incidence of events such as myocardial infarction and unstable angina. The success of interventional treatments such as thrombolysis and angioplasty to prevent or alleviate these conditions is also compromised by platelet-mediated occlusion or re-occlusion. [0003] Hemostasis is controlled by a tight balance between platelet aggregation, coagulation, and fibrinolysis. Thrombosis under pathological conditions (eg rupture o...

Claims

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Application Information

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IPC IPC(8): C07D401/04A61P7/02A61K31/4427C07D401/14A61K31/4439C07D413/14A61K31/4545
Inventor S・安德森P・巴克K・布里克曼F・乔达尼托F・泽特伯格K・奥斯特伦德
Owner ASTRAZENECA AB
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