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Pyrazolo (3, 4-b) pyridine derivatives as phosphodiesterase inhibitors

一种吡唑并、4-b的技术，应用在制备所公开的化合物领域，能够解决难以克服、剂量依赖性副作用、限制等问题

Inactive Publication Date: 2010-08-11
RANBAXY LAB LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Current approaches to target PDE4 to alleviate chronic inflammation associated with COPD are limited by dose-dependent side effects that are difficult to overcome

Method used

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  • Pyrazolo (3, 4-b) pyridine derivatives as phosphodiesterase inhibitors
  • Pyrazolo (3, 4-b) pyridine derivatives as phosphodiesterase inhibitors
  • Pyrazolo (3, 4-b) pyridine derivatives as phosphodiesterase inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1a

[0618] Example 1a: Preparation 1- ( 4-methoxybenzyl)-1H-pyrazol-5-amine

[0619] The compound is according to Bioorganic and medicinal chemistry letters (bioorganic and medicinal chemistry), 13， 1133-1136 (2003) described method is synthesized.

Embodiment 1b

[0620] Example 1b: Preparation of 1-ethyl-3-methyl-1H-pyrazol-5-amine

[0621] The compound according to Chem.Pharm.Bull. 52 (9), 1098-1104 (2004) described in the method for synthesis.

Embodiment 1c

[0622] Example 1c: Preparation of tetrahydro-2H-pyran-4-amine hydrochloride

[0623] The compound according to Tetrahedron letters, 42 , 4257-4259, (2001) described in the method for synthesis.

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PUM

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Abstract

The present invention relates to phosphodiesterase (PDE) type 4, phosphodiesterase (PDE) type 7 and dual PDE type 4 / PDE type 7 inhibitors. Compounds disclosed herein having the structure of Formura 1: can be useful in the treatment, prevention, inhibition or suppression of CNS diseases, for example, multiple sclerosis; various pathological conditions such as diseases affecting the immune system, including AIDS, rejection of transplant, auto-immune disorders such as T-cell related diseases, for example, rheumatoid arthritis; inflammatory diseases such as respiratory inflammation diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchitis, allergic rhinitis, adult respiratory distress syndrome (ARDS) and other inflammatory diseases including but not limited to psoriasis, shock, atopic dermatitis, eosinophilic granuloma, allergic conjunctivitis, osteoarthritis; gastrointestinal inflammation diseases such as Crohn's disease, colitis, pancreatitis as well as different types of cancers including leukaemia; especially in humans. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as PDE type 4, PDE type 7 and dual PDE type 4 / PDE type 7 inhibitors are provided.

Description

field of invention [0001] The invention relates to type 4 phosphodiesterase (PDE), type 7 phosphodiesterase (PDE) and type 4 PDE / type 7 PDE dual inhibitors. [0002] The compounds disclosed herein are useful for treating, preventing, inhibiting or suppressing CNS diseases such as multiple sclerosis; various pathological conditions such as diseases affecting the immune system including AIDS, graft rejection, autoimmune diseases such as T-cell related Diseases such as rheumatoid arthritis; inflammatory diseases such as respiratory inflammatory diseases, including chronic obstructive pulmonary disease (COPD), asthma, bronchitis, allergic rhinitis, adult respiratory distress syndrome (ARDS) and other inflammatory diseases, Including but not limited to psoriasis, shock, atopic dermatitis, eosinophilic granuloma, allergic conjunctivitis, osteoarthritis; gastrointestinal inflammatory diseases such as Crohn's disease, colitis, pancreatitis; and various types cancer, including leukemi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/437A61P11/00A61P17/00A61P19/00A61P35/00C07D471/04C07D519/00
CPCC07D519/00C07D471/04A61P1/00A61P1/04A61P1/18A61P11/00A61P11/02A61P11/06A61P17/00A61P17/04A61P17/06A61P19/00A61P19/02A61P19/08A61P25/00A61P27/14A61P29/00A61P31/18A61P35/00A61P37/02A61P37/06A61P43/00A61P7/00A61K31/437
Inventor S·鲁德拉N·古普塔L·K·巴里加玛R·阿加瓦尔V·V·卡尔纳M·R·拉玛亚V·P·帕勒S·巴拉钱德拉A·康达斯卡M·萨拉A·雷S·G·达斯蒂达L·维贾克里斯南
Owner RANBAXY LAB LTD