RU2015144372A - Антибактериальные сидерофор-аминопенициллиновые конъюгаты - Google Patents

Антибактериальные сидерофор-аминопенициллиновые конъюгаты Download PDF

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RU2015144372A
RU2015144372A RU2015144372A RU2015144372A RU2015144372A RU 2015144372 A RU2015144372 A RU 2015144372A RU 2015144372 A RU2015144372 A RU 2015144372A RU 2015144372 A RU2015144372 A RU 2015144372A RU 2015144372 A RU2015144372 A RU 2015144372A
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bacterial infection
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Марвин Дж. МИЛЛЕР
Чэн ЦЗИ
Патрисия А. МИЛЛЕР
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Юниверсити Оф Нотр Дам Дю Лак
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Claims (28)

1. Соединение формулы (I):
Figure 00000001
где X представляет собой антибиотик, ковалентно связанный с проиллюстрированной структурой формулы (I) посредством сложноэфирной или амидной связи;
m принимает значения 0 или 1-11;
каждый R1 независимо представляет собой H, -C(=O)алкил, -C(=O)арил или -C(=O)O-алкил;
каждый R2 независимо представляет собой H, алкил, алкокси, гидрокси, карбокси, галоген, нитро, амино или циано; и
каждый n независимо принимает значения 1, 2, или 3;
или фармацевтически приемлемые соли или их сольваты.
2. Соединение по п. 1, где каждый R1 представляет собой ацетил, пропаноил или бензоил.
3. Соединение по п. 1, где каждый R2 представляет собой H, алкил, алкокси или гидрокси.
4. Соединение по п. 1, где каждый R2 представляет собой H.
5. Соединение по п. 1, в котором каждый n принимает значение 1.
6. Соединение по п. 1, где m принимает значения 0, 1, 2 или 3.
7. Соединение по п. 1, в котором X представляет собой амикацин, амоксициллин, ампициллин, амфотерицин, азтреонам, бацилломицин, BAL30072, биапенем, карумонам, цефаклор, цефалотин, хлорамфеникол, хлортетрациклин, ципрофлоксацин, клиндамицин, клиндамицина фосфат, циклосерин, даптомицин, демеклоциклин, дорипенем, доксорубицин, доксициклин, эртапенем, эритромицин, этамбутол, эритромицин, гентамицин, имипенем, изониазид, канамицин, линкомицин, лоракарбеф, меропенем, метациклин, мупироцин, неомицин, нистатин, окситетрациклин, панипенем, пирролнитрин, рифампин, ролитетрациклин, стрептомицин, сульфацетамид, сульфабензамид, сульфадиазин, сульфадоксин, сульфамеразин, сульфаметазин, сульфаметизол, сульфаметоксазол, сульфизоксазол, тетрациклин или тигимонам.
8. Соединение по п. 1, в котором X представляет собой ампициллин или амоксициллин.
9. Соединение по п. 1, где соединение представляет собой
Figure 00000002
или
Figure 00000003
.
10. Композиция, содержащая соединение по п. 1 и фармацевтически приемлемый разбавитель или носитель.
11. Способ лечения бактериальной инфекции, вызванной грамотрицательной бактерией, включающий введение субъекту, нуждающемуся в этом, эффективного терапевтического количества соединения по п. 1 с обеспечением тем самым лечения указанной бактериальной инфекции.
12. Способ по п. 11, в котором указанная бактериальная инфекция вызвана устойчивой к антибиотику бактерией.
13. Способ по п. 11, в котором указанная бактериальная инфекция вызвана бактерией Pseudomonas.
14. Способ лечения бактериальной инфекции, вызванной грамотрицательной бактерией, включающий введение субъекту, нуждающегося в этом, эффективного терапевтического количества композиции по п. 10 с обеспечением тем самым лечения бактериальной инфекции.
15. Способ уничтожения или подавления роста грамотрицательной бактерии, включающий приведение указанной бактерии в контакт с эффективным летальным или ингибирующим количеством соединения по п. 1.
16. Способ по п. 15, в котором указанная бактериальная инфекция вызвана устойчивой к антибиотику бактерией.
17. Способ по п. 15, в котором указанная бактериальная инфекция вызвана бактерией Pseudomonas.
18. Способ по п. 15, в котором указанная бактериальная инфекция вызвана Pseudomonas aeruginosa, Escherichia coli, Acinetobacter baumannii или Salmonella typhimurium.
19. Способ уничтожения или подавления роста грамотрицательной бактерии, включающий приведение указанной бактерии в контакт с эффективным летальным, или ингибирующим количеством композиции по п. 10.
RU2015144372A 2013-04-18 2013-10-23 Антибактериальные сидерофор-аминопенициллиновые конъюгаты RU2015144372A (ru)

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