Inhibition and dispersion of bacterial biofilms with imidazole-triazole derivatives
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
C07D-403/06
C07D-403/14
C07D-405/14
C07D-409/14
A61L-027/54
A61K-031/5377
A61K-031/4192
A61L-029/16
A61L-031/16
A01N-043/653
A01N-043/647
A01N-043/84
A61K-045/06
출원번호
US-0732620
(2013-01-02)
등록번호
US-9145395
(2015-09-29)
발명자
/ 주소
Melander, Christian
Rogers, Steven A.
Huigens, III, Robert W.
Reed, Catherine S.
출원인 / 주소
North Carolina State University
대리인 / 주소
Myers Bigel Sibley & Sajovec, P.A.
인용정보
피인용 횟수 :
0인용 특허 :
12
초록
Disclosure is provided for imidazole-triazole derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions comprising these compounds, devices comprising these compounds, and methods of using the same.
대표청구항▼
1. A method of controlling biofilm formation on a substrate comprising the step of contacting to said substrate in an amount effective to inhibit biofilm formation: a compound of Formula (II)(a): wherein: R1a and R1b are each H;R2, R3, R5 and are each independently H or alkyl;each occurrence of Rx,
1. A method of controlling biofilm formation on a substrate comprising the step of contacting to said substrate in an amount effective to inhibit biofilm formation: a compound of Formula (II)(a): wherein: R1a and R1b are each H;R2, R3, R5 and are each independently H or alkyl;each occurrence of Rx, Ry, Ru and Rv is present or absent (depending upon chain saturation), and are each independently H or alkyl;R6 is independently selected from the group consisting of H, hydroxy, acyl, alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclo, aryl, heteroaryl, alkoxy, amino, amide, thiol, sulfone, sulfoxide, oxo, oxy, nitro, carbonyl, carboxy, amino acid sidechain, amino acid and peptide;n=0 to 10; andm=0 to 20;or a pharmaceutically acceptable salt or prodrug thereof. 2. The method of claim 1, wherein said method comprises the step of reducing a preformed biofilm from said substrate by administering an effective amount of the compound to said substrate, wherein said effective amount will reduce the amount of said biofilm on said substrate. 3. A method for treating a chronic bacterial infection in a subject in need thereof, comprising administering to said subject in an amount effective to inhibit, reduce, or remove a biofilm component of said chronic bacterial infection: a compound of Formula (II)(a): wherein: R1a and R1b are each H;R2, R3, R5 and are each independently H or alkyl;each occurrence of Rx, Ry, Ru and Rv is present or absent (depending upon chain saturation), and are each independently H or alkyl;R6 is independently selected from the group consisting of: H, hydroxy, acyl, alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclo, aryl, heteroaryl, alkoxy, amino, amide, thiol, sulfone, sulfoxide, oxo, oxy, nitro, carbonyl, carboxy, amino acid sidechain, amino acid and peptide;n=0 to 10; andm=0 to 20;or a pharmaceutically acceptable salt or prodrug thereof. 4. The method of claim 3, wherein said chronic bacterial infection is selected from the group consisting of urinary tract infection, gastritis, respiratory infection, cystitis, pyelonephritis, osteomyelitis, bacteremia, skin infection, rosacea, acne, chronic wound infection, infectious kidney stones, bacterial endocarditis, and sinus infection. 5. The method of claim 3, wherein said compound is administered in combination with an antibiotic. 6. A medical device comprising: (a) a medical device substrate; and(b) an effective amount of a compound of Formula (II)(a): wherein: R1a and R1b are each H;R2, R3, R5 and are each independently H or alkyl;each occurrence of Rx, Ry, Ru and Ry is present or absent (depending upon chain saturation), and are each independently H or alkyl;R6 is independently selected from the group consisting of: H, hydroxy, acyl, alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclo, aryl, heteroaryl, alkoxy, amino, amide, thiol, sulfone, sulfoxide, oxo, oxy, nitro, carbonyl, carboxy, amino acid sidechain, amino acid and peptide;n=0 to 10; andm=0 to 20;or a pharmaceutically acceptable salt or prodrug thereof, either coating the substrate, or incorporated into the substrate, wherein said effective amount of said compound prevents or inhibits the growth of a biofilm thereon. 7. The medical device of claim 6, wherein said medical device substrate is selected from the group consisting of stents, fasteners, ports, catheters, scaffolds and grafts. 8. A medical device comprising: (a) a medical device substrate; and(b) an effective amount of a compound of Formula (II)(a): wherein: R1a and R1b are each H;R2, R3, R5 and are each independently H or alkyl;each occurrence of Rx, Ry, Ru and Rv is present or absent (depending upon chain saturation), and are each independently H or alkyl;R6 is independently selected from the group consisting of: H, hydroxy, acyl, alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclo, aryl, heteroaryl, alkoxy, amino, amide, thiol, sulfone, sulfoxide, oxo, oxy, nitro, carbonyl, carboxy, amino acid sidechain, amino acid and peptide;n=0 to 10; andm=0 to 20, wherein said compound is covalently coupled to said substrate. 9. The medical device of claim 6, wherein n=1 to 6. 10. The medical device of claim 9, wherein m=1 to 3. 11. The medical device of claim 10, wherein R6 is aryl. 12. The method of claim 1, wherein said compound is a compound of Formula (II)(a)(5)(D): 13. The method of claim 1, wherein said compound is 14. The method of claim 1, wherein m=1 to 10. 15. The method of claim 3, wherein m=1 to 10. 16. The medical device of claim 6, wherein m=1 to 10. 17. The medical device of claim 8, wherein m=1 to 10.
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이 특허에 인용된 특허 (12)
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Melander, Christian; Rogers, Steven A.; Huigens, III, Robert W.; Reed, Catherine S., Inhibition and dispersion of bacterial biofilms with imidazole-triazole derivatives.
Melander, Christian; Rogers, Steven A.; Huigens, III, Robert W.; Reed, Catherine S., Inhibition and dispersion of bacterial biofilms with imidazole-triazole derivatives.
Ulrich Peter (Old Tappan NJ) Cerami Anthony (Shelter Island NY) Wagle Dilip R. (Valley Cottage NY), Method for inhibiting advanced glycosylation of proteins using aminosubstituted imidazoles.
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