Pyrazolo[3,4-b]pyridine compounds, and their use as PDE4 inhibitors

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The Glaxo Group Limited patent solves the following problem:

US Pat. . Nos 3,979,399, 3,840,546, and 3,966,746 (ER Squibb & sons) disclose 4-amino pyrazolo [3,4-b] pyridine-5-carboxamide compounds of the following formula and salts thereof:

Our analysis of this patent is as follows:

Glaxo Group Limited’s patent US 7465743 B2 deals with Pyrazolo[3,4-b]pyridine compounds, and their use as PDE4 inhibitors.
The invention relates to a compound of formula (I) or a salt thereof: where: R1 is Et, n-Pr, i-Pr, C2fluoroalkyl, or CH2CH2OH; R2 is H, Me, Et, n-Pr, i-Pr, C1-2fluoroalkyl, cyclopropyl or (cyclopropyl) methyl; and NHR3 a sub-formula (nhr3): where R3A is methyl or ethyl; R3b is H, methyl or ethyl; R3C is H, methyl or ethyl, R3d is H, methyl or ethyl, and R3E is H or methyl, provided that: (a) R3B is methyl or ethyl; and / or (b) R3C and R3d independently methyl or ethyl; and provided that: (c) when R3C is ethyl and / or when R3d is ethyl and / or when R3E is methyl, then: R3A are methyl and / or R3B is hydrogen or methyl. These compounds are PDE4 inhibitor.

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Anticholinergic powder formulations for inhalation

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The Boehringer Ingelheim International Gmbh patent solves the following problem:

The compounds of Formula 1 is known from WO 02/32899 (corresponding to US Patent Application Pub. No. 2004/0087617, which is included in the discussion). They are valuable medicinal properties and provide therapeutic benefit as highly effective anticholinergics in the treatment of respiratory complaints, particularly in the treatment of inflammatory and / or obstructive diseases of the respiratory tract, especially for the treatment of asthma or chronic obstructive pulmonary disease ( COPD).

Our analysis of this patent is as follows:

Boehringer Ingelheim International Gmbh’s patent US 7462367 B2 deals with Anticholinergic powder formulations for inhalation.
An inhalable powder comprising: (a) an active substance consisting essentially of a compound of formula 1 wherein X is a pharmaceutically acceptable anion; and (b) a physiologically acceptable excipient with an average volume fraction of 10 m to 50 m, the process to prepare the inhalable powder, and methods of administration for the treatment of respiratory complaints, especially for the treatment of chronic obstructive pulmonary disease (COPD) and asthma.

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