Salt and crystal form of egfr inhibitor, and composition and use thereof
US-2024352053-A1 · Oct 24, 2024 · US
US9593136B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9593136-B2 |
| Application number | US-201214130384-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jun 29, 2012 |
| Priority date | Jul 1, 2011 |
| Publication date | Mar 14, 2017 |
| Grant date | Mar 14, 2017 |
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In particular, the compound is effective to inhibit Dxr in Mycobacterium tuberculosis (Mtb). The present invention relates to compounds having general formula (I) or (II) where X is an acidic group, such as carboxylate, phosphonate, sulfate, and tetrazole; Ar is a substituted or unsubstituted aromatic or heteroaromatic group; and n is 0, 1, 2, 3, or 4, preferably 2, 3, or 4. The compounds inhibits 1-deoxy-D-xylulose-5-phosphate reductoisomerase (Dxr), particularly Dxr in Mycobacterium tuberculosis (Mtb).
Opening claim text (preview).
What is claimed is: 1. A compound having the chemical structure of formula (II) wherein X is 1) a carboxylate, phosphonate, sulfate, an ester thereof, or a salt thereof, or 2) a tetrazole; Ar is a substituted or unsubstituted aromatic or heteroaromatic group; and n is 0, 1, 2, 3, or 4, wherein “n is 1” and are not simultaneously satisfied. 2. The compound of claim 1 , wherein Ar is a phenyl or a heteroaromatic group. 3. A compound having the chemical structure of formula (II) wherein X is 1) a carboxylate, phosphonate, sulfate, an ester thereof, or a salt thereof, or 2) a tetrazol; Ar is a substituted or unsubstituted aromatic or heteroaromatic group; and wherein n is 2, 3, or 4. 4. A compound having the chemical structure of formula (II) wherein X is a phosphonate, an ester thereof, or a salt thereof; Ar is a substituted or unsubstituted aromatic or heteroaromatic group; and n is 0, 1, 2, 3, or 4, wherein “n is 1” and are not simultaneously satisfied. 5. The compound of claim 1 , selected from the group consisting of: 6. A pharmaceutical composition comprising a compound having the chemical structure of formula (II) wherein X is 1) a carboxylate, phosphonate, sulfate, an ester thereof, or a salt thereof, or 2) tetrazole; Ar is a substituted or unsubstituted aromatic or heteroaromatic group; and n is 0, 1, 2, 3, or 4, wherein “n is 1” and are not simultaneously satisfied. 7. The composition of claim 6 , wherein Ar is a phenyl or a heteroaromatic group. 8. A pharmaceutical composition comprising a compound having the chemical structure of formula (II) where X is 1) a carboxylate, phosphonate, sulfate, an ester thereof, or a salt thereof, or 2) a tetrazole; Ar is a substituted or unsubstituted aromatic or heteroaromatic group; wherein n is 2, 3, or 4. 9. A pharmaceutical composition comprising the compound of claim 5 .
Phosphorus compounds · CPC title
N-acyl derivatives · CPC title
having aromatic rings {, e.g. ketamine, nortriptyline (methadone A61K31/137)} · CPC title
Esters of aromatic acids (P-C aromatic linkage) · CPC title
involving isomerase · CPC title
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