Benzathine analogs
US-2019091222-A1 · Mar 28, 2019 · US
US10869866B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10869866-B2 |
| Application number | US-201916444879-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jun 18, 2019 |
| Priority date | Jun 8, 2012 |
| Publication date | Dec 22, 2020 |
| Grant date | Dec 22, 2020 |
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A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein X is a divalent linking moiety; and R 1 -R 10 are each individually H, optionally-substituted alkyl, optionally-substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, halogen, amino, or hydroxy, provided that at least one of R 3 or R 8 is an optionally-substituted alkyl, a substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, or halogen.
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What is claimed is: 1. A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of formula II: wherein X is an optionally-substituted aryldiyl; and R 1 -R 10 are each individually H, optionally-substituted alkyl, optionally-substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocycle, halogen, amino, or hydroxy, provided that at least one of R 3 or R 8 is an N-heterocycle selected from pyrrolyl, H-pyrrolyl, pyrrolinyl, pyrrolidinyl, oxazolyl, oxadiazolyl, isoxazolyl, furazanyl, thiazolyl, isothiazolyl, pyrazolyl, pyrazolinyl, pyrazolidinyl, imidazolyl, imidazolinyl, triazolyl, tetrazolyl, pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl, piperidinyl, morpholinyl, thiomorpholinyl, piperazinyl, or triazinyl. 2. The compound of claim 1 , wherein R 3 is an N-heterocycle and R 8 is an N-heterocycle. 3. The compound of claim 1 , wherein the N-heterocycle is selected from imidazolyl, pyridyl, pyrazolyl, oxadiazolyl, or pyrimidinyl. 4. The compound of claim 1 , wherein R 1 , R 2 , R 4 , R 5 , R 6 , R 7 , R 9 and R 10 are each H, and R 3 and R 8 are not H. 5. A pharmaceutical composition comprising at least one compound of claim 1 , and at least one pharmaceutically acceptable additive. 6. The compound of claim 1 , wherein X is phenylenediyl. 7. The compound of claim 1 , wherein the N-heterocycle is pyrazolidinyl. 8. The compound of claim 1 , wherein R 3 and R 8 are each pyrazolidinyl. 9. The compound of claim 6 , wherein R 3 and R 8 are each pyrazolidinyl. 10. The compound of claim 1 , wherein R 1 , R 2 , R 4 , R 5 , R 6 , R 7 , R 9 and R 10 are each H, and R 3 and R 8 are each pyrazolidinyl. 11. The compound of claim 2 , wherein X is phenylenediyl. 12. The compound of claim 10 , wherein X is phenylenediyl.
Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change · CPC title
having five-membered rings · CPC title
having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom · CPC title
linked by a chain containing hetero atoms as chain links · CPC title
not condensed and containing further heterocyclic rings · CPC title
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