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US-2024400552-A1 · Dec 5, 2024 · US
Benzazepine dicarboxamide compounds
US9822065B1 · US · B1
| Field | Value |
|---|---|
| Publication number | US-9822065-B1 |
| Application number | US-201715432859-A |
| Country | US |
| Kind code | B1 |
| Filing date | Feb 14, 2017 |
| Priority date | Mar 6, 2015 |
| Publication date | Nov 21, 2017 |
| Grant date | Nov 21, 2017 |
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- Title
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- Abstract
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Abstract
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This invention relates to novel benzazepine dicarboxamide compounds of the formula wherein R 1 to R 4 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are TLR agonists and may therefore be useful as medicaments for the treatment of diseases such as cancer, autoimmune diseases, inflammation, sepsis, allergy, asthma, graft rejection, graft-versus-host disease, immunodeficiencies, and infectious diseases.
First claim
Opening claim text (preview).
The invention claimed is: 1. A process for the preparation of 2-amino-8-methoxycarbonyl-3H-1-benzazepine-4-carboxylic acid (I) comprising the step of deprotection of 4-tert-butyl 8-methyl 2-amino-3H-benzo[b]azepine-4,8-dicarboxylate (II) under acidic conditions. 2. The process according to claim 1 said process further comprising the step of reductive cyclization of compound (III) by treating compound (III) with iron and acetic acid. 3. The process according to claim 2 said process further comprising condensation of tert-butyl 3-cyano-2-(triphenylphosphoranylidene)propanoate with methyl 4-formyl-3-nitrobenzoate under basic conditions to afford methyl 4-(3-(tert-butoxy)-2-(cyanomethyl)-3-oxoprop-1-en-1-yl)-3-nitrobenzoate 4. A process for the preparation compound according to formula (VI) comprising condensation of VIII with VII basic conditions to afford methyl 4-(3-(tert-butoxy)-2-(cyanomethyl)-3-oxoprop-1-en-1-yl)-3-nitrobenzoate wherein R a and R b are C 1-6 alkyl or benzyl. 5. A compound which compound is 2-amino-8-methoxycarbonyl-3H-1-benzazepine-4-carboxylic acid, 4-tert-butyl 8-methyl 2-amino-3H-benzo[b]azepine-4,8-dicarboxylate or tert-butyl 3-cyano-2-(triphenylphosphoranylidene)propanoate.
Assignees
Inventors
Classifications
Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title
Immunomodulators · CPC title
specific for metastasis · CPC title
Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14) · CPC title
Immunosuppressants, e.g. drugs for graft rejection · CPC title
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- What does patent US9822065B1 cover?
- This invention relates to novel benzazepine dicarboxamide compounds of the formula wherein R 1 to R 4 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are TLR agonists and may therefore be useful…
- Who is the assignee on this patent?
- Hoffmann La Roche
- What technology area does this patent fall under?
- Primary CPC classification A61K31/55. Mapped technology areas include Human Necessities.
- When was this patent published?
- Publication date Tue Nov 21 2017 00:00:00 GMT+0000 (Coordinated Universal Time) (B1). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).