Process for the preparation of a PDE4 inhibitor
US-9434691-B2 · Sep 6, 2016 · US
Process for the preparation of a PDE4 inhibitor
US9890122B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9890122-B2 |
| Application number | US-201615217468-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jul 22, 2016 |
| Priority date | Oct 22, 2013 |
| Publication date | Feb 13, 2018 |
| Grant date | Feb 13, 2018 |
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- Title
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Abstract
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The present invention relates to a process for the preparation of compounds endowed with phosphodiesterase (PDE4) inhibitory activity having formula (I). The invention also relates to the process for the isolation by crystallization of the compound (I) and to its use for the preparation of pharmaceutical compositions for inhalation in combination with suitable carriers or vehicles. The present invention also relates to solvates and crystal forms of a compound of formula (I). The synthesized product is suitable for use in pharmaceutical applications for instance in the treatment of respiratory diseases.
First claim
Opening claim text (preview).
The invention claimed is: 1. Crystal form A of 3-cyclopropylmethoxy-4-methanesulfonylamino-benzoic acid 1-(3-cyclopropylmethoxy-4-difluoromethoxy-phenyl)-2-(3,5-dichloro-1-oxy-pyridin-4-yl)-ethyl ester, which exhibits the following XRPD peaks: 7.93; 10.32; 13.51; 16.18; 20.2; and 24.87±0.2 degrees/2 theta (CuKα2). 2. Crystal form A of 3-cyclopropylmethoxy-4-methanesulfonylamino-benzoic acid 1-(3-cyclopropylmethoxy-4-difluoromethoxy-phenyl)-2-(3,5-dichloro-1-oxy-pyridin-4-yl)-ethyl ester according to claim 1 , which exhibits the following XRPD peaks: 7.93; 10.32; 12.72; 13.51; 16.18; 17.79; 18.94; 20.2; and 24.87±0.2 degrees/2 theta (CuKα2). 3. Crystal form A of 3-cyclopropylmethoxy-4-methanesulfonylamino-benzoic acid 1-(3-cyclopropylmethoxy-4-difluoromethoxy-phenyl)-2-(3,5-dichloro-1-oxy-pyridin-4-yl)-ethyl ester according to claim 1 , which exhibits the following XRPD peaks: 7.48; 7.93; 8.55; 10.32; 12.72; 13.51; 16.18; 17.79; 18.94; 20.2; 23.63; 24.87; and 25.82±0.2 degrees/2 theta (CuKα2). 4. A method of treating an inflammatory or obstructive respiratory disease selected from the group consisting of asthma and chronic obstructive pulmonary disease (COPD), which comprises the inhalatory administration of an effective amount of the crystal form A of 3-cyclopropylmethoxy-4-methanesulfonylamino-benzoic acid 1-(3-cyclopropylmethoxy-4-difluoromethoxy-phenyl)-2-(3,5-dichloro-1-oxy-pyridin-4-yl)-ethyl ester according to claim 1 to a subject in need thereof.
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Classifications
- A61K31/44Primary
Non condensed pyridines; Hydrogenated derivatives thereof · CPC title
- C07D213/61Primary
Halogen atoms or nitro radicals · CPC title
Pulmonary tract; Aromatherapy · CPC title
Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy; (nasal sprays A61K9/0043; inhalation of vapours of volatile or heated drugs, e.g. essential oils or nicotine, A61K9/007; devices A61M) · CPC title
- C07D213/89Primary
with hetero atoms directly attached to the ring nitrogen atom · CPC title
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- What does patent US9890122B2 cover?
- The present invention relates to a process for the preparation of compounds endowed with phosphodiesterase (PDE4) inhibitory activity having formula (I). The invention also relates to the process for the isolation by crystallization of the compound (I) and to its use for the preparation of pharmaceutical compositions for inhalation in combination with suitable carriers or vehicles. The present …
- Who is the assignee on this patent?
- Chiesi Farm Spa
- What technology area does this patent fall under?
- Primary CPC classification A61K31/44. Mapped technology areas include Human Necessities.
- When was this patent published?
- Publication date Tue Feb 13 2018 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 7 related publications on this page (citations in our corpus or others sharing the same primary CPC).