Process for making arylomycin ring analogs
US-2020255476-A1 · Aug 13, 2020 · US
Macrocyclic broad spectrum antibiotics
US11208387B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-11208387-B2 |
| Application number | US-202016884679-A |
| Country | US |
| Kind code | B2 |
| Filing date | May 27, 2020 |
| Priority date | May 28, 2019 |
| Publication date | Dec 28, 2021 |
| Grant date | Dec 28, 2021 |
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- Title
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Abstract
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Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidases SpsB and/or LepB, an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
First claim
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What is claimed is: 1. A compound, or a pharmaceutically acceptable salt thereof, selected from the group consisting of: 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound is (8S,11S,14S)-18-hydroxy-11-methyl-14-[methyl-[(2S)-2-[[4-amino-2-(4-tert-butylphenyl)-6-methyl-pyrimidine-5-carbonyl]amino]-3-(sulfamoylamino)propanoyl]amino]-10,13-dioxo-3,17-bis[(2R)-3-amino-2-hydroxy-propoxy]-9,12-diazatricyclo[13.3.1.12,6]icosa-1(18),2(20),3,5,15(19),16-hexaene-8-carboxylic acid. 3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound is (8S,11S,14S)-18-hydroxy-11-methyl-14-[methyl-[(2S)-4-amino-2-[[4-amino-2-(4-tert-butylphenyl)-6-methyl-pyrimidine-5-carbonyl]amino]butanoyl]amino]-10,13-dioxo-3,17-bis[(2R)-3-amino-2-hydroxy-propoxy]-9,12-diazatricyclo[13.3.1.12,6]icosa-1(18),2(20),3,5,15(19),16-hexaene-8-carboxylic acid. 4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound is (8S,11S,14S)-18-hydroxy-11-methyl-14-[methyl-[(2S)-4-amino-2-[[4-methyl-2-[4-(1-methylcyclopropyl)phenyl]pyrimidine-5-carbonyl]amino]butanoyl]amino]-10,13-dioxo-3,17-bis[(2R)-3-amino-2-hydroxy-propoxy]-9,12-diazatricyclo[13.3.1.12,6]icosa-1(18),2(20),3,5,15(19),16-hexaene-8-carboxylic acid. 5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound is (8S,11S,14S)-18-hydroxy-11-methyl-14-[methyl-[(2S)-4-amino-2-[[2-(4-tert-butylphenyl)-4-amino-6-difluoromethyl-pyrimidine-5-carbonyl]amino]butanoyl]amino]-10,13-dioxo-3,17-bis[(2R)-3-amino-2-hydroxy-propoxy]-9,12-diazatricyclo[13.3.1.12,6]icosa-1(18),2(20),3,5,15(19),16-hexaene-8-carboxylic acid. 6. A pharmaceutical composition comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.
Assignees
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Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change · CPC title
linked by a chain containing hetero atoms as chain links · CPC title
- C07D245/02Primary
not condensed with other rings · CPC title
Bridged systems · CPC title
containing three or more hetero rings · CPC title
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Frequently asked questions
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- What does patent US11208387B2 cover?
- Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidases SpsB and/or LepB, an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
- Who is the assignee on this patent?
- Genentech Inc
- What technology area does this patent fall under?
- Primary CPC classification C07D245/02. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Dec 28 2021 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 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).