Imidazoquinoxaline compounds as immunomodulators
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/50
A61K-039/02
A61K-039/12
A61K-039/00
C07D-471/00
C07D-487/00
출원번호
US-0294233
(2007-03-23)
등록번호
US-8173657
(2012-05-08)
국제출원번호
PCT/US2007/064858
(2007-03-23)
§371/§102 date
20090210
(20090210)
국제공개번호
WO2007/109813
(2007-09-27)
발명자
/ 주소
Sutton, James
Xu, Feng
Valiante, Nicholas
Lan, Jiong
출원인 / 주소
Novartis AG
대리인 / 주소
Lee, Helen
인용정보
피인용 횟수 :
0인용 특허 :
64
초록▼
The invention provides novel compositions comprising imidazoquinoxaline compounds of formula (I) and analogs thereof. Also provided are methods of administering the compositions in an effective amount to enhance the immune response of a subject. Further provided are novel compositions and methods of
The invention provides novel compositions comprising imidazoquinoxaline compounds of formula (I) and analogs thereof. Also provided are methods of administering the compositions in an effective amount to enhance the immune response of a subject. Further provided are novel compositions and methods of administering the compositions in combination with (an) other agent(s).
대표청구항▼
1. A compound of Formula (I): wherein:R1 is selected from the group consisting of C1-C12 alkyl, substituted C1-C12 alkyl, C2-C12 alkenyl, substituted C2-C12 alkenyl, C2-C12 alkynyl, substituted C2-C12 alkynyl, C3-C12 cycloalkyl, substituted C3-C12 cycloalkyl, hydroxy, hydroxyalkyl, halo, haloalkyl,
1. A compound of Formula (I): wherein:R1 is selected from the group consisting of C1-C12 alkyl, substituted C1-C12 alkyl, C2-C12 alkenyl, substituted C2-C12 alkenyl, C2-C12 alkynyl, substituted C2-C12 alkynyl, C3-C12 cycloalkyl, substituted C3-C12 cycloalkyl, hydroxy, hydroxyalkyl, halo, haloalkyl, amino, —OR3, —N(R3)(R4), —NR3C(═O)R4, —NR3S(═O)pR4, —NR3C(═O)NR4R5, —NR3S(═O)pNR4R5, —C(═O)R4, —S(═O)pR4, —C(═O)NR3R4, —S(═O)pNR3R4 and —C(═O)OR4;R2 is selected from the group consisting of hydrogen, C1-C12 alkyl, substituted C1-C12 alkyl, C2-C12 alkenyl, substituted C2-C12 alkenyl, C2-C12 alkynyl, substituted C2-C12 alkynyl, C3-C12 cycloalkyl, substituted C3-C12 cycloalkyl, aryl, substituted aryl, heterocyclyl, substituted heterocyclyl, heteroaryl, substituted heteroaryl, hydroxy, hydroxyalkyl, halo, haloalkyl, amino, —OR3, —N(R3)(R4), —NR3C(═O)R4, —NR3S(═O)pR4, —NR3C(═O)NR4R5, —NR3S(═O)pNR4R5, —C(═O)R4, —S(═O)pR4, —C(═O)NR3R4, —S(═O)pNR3R4 and —C(═O)OR4;R3, R4 and R5 are each independently selected from the group consisting of hydrogen, C1-C12 alkyl, substituted C1-C12 alkyl, C2-C12 alkynyl, substituted C2-C12 alkynyl, C2-C12 alkenyl, substituted C2-C12 alkenyl, C3-C12 cycloalkyl, substituted C3-C12 cycloalkyl, aryl, substituted aryl, heterocyclyl, substituted heterocyclyl, heteroaryl, substituted heteroaryl, hydroxy, hydroxyalkyl, halo and haloalkyl;R6 is selected from the group consisting of hydrogen, halogen, hydroxy, —OR3, —N(R3)(R4), C1-3 haloalkyl, —O—C1-3 haloalkyl, C1-3 perhaloalkyl, —O—C1-3 perhaloalkyl, C1-3 hydroxyalkyl, —O—C1-3 hydroxyalkyl, CN, —(CH2)qC(═O)R7, —O—(CH2)qC(═O)R7, —(CH2)qN(R8)(R9), —S—C1-3 alkyl, —S(═O)2—R10 and —S(═O)2N(R8)(R9);q is 0, 1, 2 or 3;R7 is selected from hydrogen, hydroxy, C1-3 alkyl or C1-3 alkoxy; andR8, R9 and R10 are each independently hydrogen or C1-3 alkyl;or a pharmaceutically acceptable salt thereof; a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. 2. A compound of claim 1, wherein R1 is —N(R3)(R4), C1-C12 alkyl, substituted C1-C12 alkyl, C2-C12 alkenyl, or substituted C2-C12 alkenyl. 3. A compound of claim 1, wherein R1 is C1-C12 alkyl or substituted C1-C12 alkyl. 4. A compound of claim 1, wherein R1 is C1-C6 alkyl. 5. A compound of claim 1, wherein R2 is hydrogen, C1-C12 alkyl, substituted C1-C12 alkyl, C2-C12 alkenyl, substituted C2-C12 alkenyl, or hydroxyalkyl. 6. A compound of claim 1, wherein R2 is hydroxyalkyl. 7. A compound of claim 1, wherein: R1 is —CH2—CH(CH3)2; andR2 is hydrogen or hydroxyalkyl. 8. A compound of claim 1, wherein R6 is hydrogen. 9. A compound of claim 1, wherein said compound is: or a pharmaceutically acceptable salt thereof. 10. A compound of claim 1, wherein said compound is: or a pharmaceutically acceptable salt thereof. 11. A method of inducing an immune response in a subject, comprising: administering a compound of claim 1 to the subject in an amount sufficient to induce an immune response in the subject. 12. The method of claim 11, wherein the subject is suffering from a microbial infection. 13. The method of claim 11, wherein the subject is suffering from a viral infection. 14. The method of claim 11, wherein the subject is suffering from abnormal cellular proliferation or cancer. 15. The method of claim 11, wherein the subject is suffering from allergic diseases. 16. The method of claim 11, wherein the subject is suffering from asthma. 17. The method of claim 11, wherein the subject is suffering from precancerous lesions, wherein the precancerous lesions are actinic keratosis. 18. The method of claim 11 wherein the compound is administered topically. 19. A method of enhancing the immune response to an antigen in a subject, comprising: administering to the subject a composition comprising a compound of claim 1 and an antigen, wherein the immune response to the antigen in the subject is enhanced. 20. A pharmaceutical composition, comprising: the compound of claim 1 and a pharmaceutically acceptable excipient. 21. A composition comprising the compound of claim 1 and an additional immunogenic composition or an antigen. 22. The composition of claim 21, further comprising an adjuvant, wherein the adjuvant is MF59. 23. The composition of claim 21, further comprising poly(lactide-co-glycolide) (PLG). 24. The composition of claim 21, wherein the antigen is a bacterial antigen or a viral antigen. 25. The composition of claim 24, wherein the antigen is a viral antigen from a virus selected from the group consisting of Hepatitis C virus, Human Immunodeficiency virus, Hepatitis B virus, Human Papilloma virus and Influenza virus. 26. The composition of claim 25, wherein the antigen is an influenza antigen, and wherein the influenza antigen comprises haemagglutinin and/or neuraminidase surface proteins. 27. An immunogenic composition comprising an antigen and the compound of claim 1 effective to stimulate a cell mediated immune response to said antigen.
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