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    • 1. 发明申请
    • Inhibitors of cancer cell, T-cell and keratinocyte proliferation
    • 癌细胞抑制剂,T细胞和角化细胞增殖
    • US20070037753A1
    • 2007-02-15
    • US11501722
    • 2006-08-10
    • Johann LebanMartin Kralik
    • Johann LebanMartin Kralik
    • A61K38/05A61K38/04C07K5/04C07D403/02
    • C07D233/72A61K38/00C07D403/12C07D405/12C07D409/12C07D417/14C07K5/0205C07K5/06078C07K5/06191Y02A50/409
    • The invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein Y is —NRaRb, —NRcC═ONRaRb, —NRcC═SNRaRb, —NRcC═NRdNaRb, heterocycle, —C═ONRaRb, heterocycle, or aryl; n is 0 to 8; m is 0, or 1; r is 0 to 3; t is 0 to 3; X is O or N; Z is CH2, C═O, C═S or a single bond; Z1 is CO—R2, CS—R2, (CH2)t—R2 or the side-chain of a naturally occuring amino acid;, Z2 is CO—R2, CS—R2 or (CH2)t—R3 or the side-chain of a naturally occuring amino acid; Z3 is CO—R2, CS—R2 or (CH2)t—R4 or the side-chain of a naturally occuring amino acid; Z4 is H, alkyl, alkoxy, or cycloalkyl; R1, R2, R3, and R4 are independently from each other H, OH, SH, NH2, CN, NO2, alkyl, cycloalkyl, heterocycloalkyl, haloalkyl, alkylthio, haloalkyloxy, hydroxyalkyl, hydroxyalkylamino, alkylamino, alkylaryl, alkylsulfinyl, alkylsulfonyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, alkoxyalkyl, alkoxy, aryloxy, heteroaryl, aryl, or halogen.
    • 本发明涉及通式(I)的化合物及其盐和生理功能衍生物,其中Y是-NR a,R b, C-ON< b> b<<< C> C-SNR< b> b C 1 -C 6卤代烷基,杂环基,C 1 -C 6 - 杂环或芳基;杂环或芳基; n为0〜8; m为0或1; r为0〜3; t为0〜3; X是O或N; Z是CH 2,C-O,C-S或单键; Z 1是CO-R 2,CS-R 2,(CH 2)2, / SUB> -R 2或天然存在的氨基酸的侧链; Z 2是CO-R 2,CS- R 2或(CH 2)2 -TH 3或天然存在的氨基酸的侧链 ; Z 3是CO-R 2,CS-R 2或(CH 2 CH 2) / SUB→4或天然存在的氨基酸的侧链; Z 4是H,烷基,烷氧基或环烷基; R 1,R 2,R 3和R 4彼此独立地为H,OH,SH ,NH 2,CN,NO 2,烷基,环烷基,杂环烷基,卤代烷基,烷硫基,卤代烷氧基,羟烷基,羟烷基氨基,烷基氨基,烷基芳基,烷基亚磺酰基,烷基磺酰基,烷硫基烷基,烷基亚磺酰基烷基 烷基磺酰基烷基,烷氧基烷基,烷氧基,芳氧基,杂芳基,芳基或卤素。
    • 2. 发明授权
    • Inhibitors of cancer cell, T-cell and keratinocyte proliferation
    • 癌细胞抑制剂,T细胞和角化细胞增殖
    • US07531517B2
    • 2009-05-12
    • US11501722
    • 2006-08-10
    • Johann LebanMartin Kralik
    • Johann LebanMartin Kralik
    • A61K38/05
    • C07D233/72A61K38/00C07D403/12C07D405/12C07D409/12C07D417/14C07K5/0205C07K5/06078C07K5/06191Y02A50/409
    • The invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein Y is —NRaRb, —NRcC═ONRaRb, —NRcC═SNRaRb, —NRcC═NRdNaRb, heterocycle, —C═ONRaRb, heterocycle, or aryl; n is 0 to 8; m is 0, or 1; r is 0 to 3; t is 0 to 3; X is O or N; Z is CH2, C═O, C═S or a single bond; Z1 is CO—R2, CS—R2, (CH2)t—R2 or the side-chain of a naturally occuring amino acid;, Z2 is CO—R2, CS—R2 or (CH2)t—R3 or the side-chain of a naturally occuring amino acid; Z3 is CO—R2, CS—R2 or (CH2)t—R4 or the side-chain of a naturally occuring amino acid; Z4 is H, alkyl, alkoxy, or cycloalkyl; R1, R2, R3, and R4 are independently from each other H, OH, SH, NH2, CN, NO2, alkyl, cycloalkyl, heterocycloalkyl, haloalkyl, alkylthio, haloalkyloxy, hydroxyalkyl, hydroxyalkylamino, alkylamino, alkylaryl, alkylsulfinyl, alkylsulfonyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, alkoxyalkyl, alkoxy, aryloxy, heteroaryl, aryl, or halogen.
    • 本发明涉及通式(I)的化合物及其盐和生理功能衍生物,其中Y为-NR a R b,-NR c C -ONR a R b,-NR c C -R SNR a R b,-NR c C-NR d N a R b,杂环,-C-ONR a R b,杂环, 或芳基; n为0〜8; m为0或1; r为0〜3; t为0〜3; X是O或N; Z是CH 2,C-O,C-S或单键; Z1是CO-R2,CS-R2,(CH2)t-R2或天然存在的氨基酸的侧链; Z2是CO-R2,CS-R2或(CH2)t-R3或侧链 的天然存在的氨基酸; Z3是CO-R2,CS-R2或(CH2)t-R4或天然存在的氨基酸的侧链; Z4是H,烷基,烷氧基或环烷基; R 1,R 2,R 3和R 4彼此独立地是H,OH,SH,NH 2,CN,NO 2,烷基,环烷基,杂环烷基,卤代烷基,烷硫基,卤代烷氧基,羟烷基,羟烷基氨基,烷基氨基,烷基芳基,烷基亚磺酰基,烷基磺酰基, 烷基亚磺酰基烷基,烷基磺酰基烷基,烷氧基烷基,烷氧基,芳氧基,杂芳基,芳基或卤素。
    • 3. 发明授权
    • Compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents
    • 化合物作为抗炎,免疫调节和抗增殖剂
    • US07071355B2
    • 2006-07-04
    • US10736711
    • 2003-12-17
    • Johann LebanMartin Kralik
    • Johann LebanMartin Kralik
    • C07C61/20C07C61/22A61K31/20
    • C07D221/04C07C233/58C07C233/60C07C235/40C07C259/08C07C2601/10C07D237/26C07D239/70C07D307/68C07D333/38C07D491/04C07D495/04
    • The present invention relates to compounds of the general formula (I) and salt and physiologically functional derivatives thereof, wherein A is a non-aromatic ring system containing 4 to 8 carbon atoms, wherein the ring system comprises at least one double bond and wherein one or more of the carbon atoms in the ring can be replaced by a group X, wherein X is selected from the group consisting of S, O, N, NR4, SO, CO or SO2; D is O, S, SO2, NR4 or CH2; Z1 and Z2 are independent from each other O, S, or NR5; R2 is H, OR6, or NHR7; E is an alkyl or cycloalkyl group or a monocyclic or polycyclic substituted or unsubstituted ring system which may contain one or more groups X and which contains at least one aromatic ring; Y is hydrogen, halogen, haloalkyl, haloalkyloxy, alkyl, cycloalkyl, a monocyclic or polycyclic substituted or unsubstituted ring system for the use as a medicament.
    • 本发明涉及通式(I)的化合物及其盐和生理功能衍生物,其中A是含有4-8个碳原子的非芳族环系,其中该环系包括至少一个双键,并且其中一个 或更多的碳原子可以被X基团取代,其中X选自S,O,N,NR 4,SO,CO或SO 3, 2 D是O,S,SO 2,NR 4或CH 2; Z 1和Z 2彼此独立地为O,S或NR 5; R 2是H,OR 6或NHR 7; E是烷基或环烷基或单环或多环取代或未取代的环系,其可以含有一个或多个基团X并且含有至少一个芳环; Y是氢,卤素,卤代烷基,卤代烷氧基,烷基,环烷基,单环或多环取代或未取代的环系统,用作药物。
    • 4. 发明申请
    • INHIBITORS OF CANCER CELL, T-CELL AND KERATINOCYTE PROLIFERATION
    • 癌细胞,T细胞和KERATINOCYTE增殖抑制剂
    • US20090176716A1
    • 2009-07-09
    • US12400680
    • 2009-03-09
    • Johann LebanMartin Kralik
    • Johann LebanMartin Kralik
    • A61K38/06C07K7/00C07D233/88C07D403/12C07D409/12A61K31/427A61K31/4166A61K31/4178A61K31/506A61P35/00A61P31/12
    • C07D233/72A61K38/00C07D403/12C07D405/12C07D409/12C07D417/14C07K5/0205C07K5/06078C07K5/06191Y02A50/409
    • The invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein Y is —NRaRb, —NRcC═ONRaRb, —NRcC═SNRaRb, —NRcC═NRdNaRb, heterocycle, —C═ONRaRb, heterocycle, or aryl; n is 0 to 8; m is 0, or 1; r is 0 to 3; t is 0 to 3; X is O or N; Z is CH2, C═O, C═S or a single bond; Z1 is CO—R2, CS—R2, (CH2)t—R2 or the side-chain of a naturally occurring amino acid; Z2 is CO—R2, CS—R2 or (CH2)t—R3 or the side-chain of a naturally occurring amino acid; Z3 is CO—R2, CS—R2 or (CH2)t—R4 or the side-chain of a naturally occurring amino acid; Z4 is H, alkyl, alkoxy, or cycloalkyl; R1, R2, R3, and R4 are independently from each other H, OH, SH, NH2, CN, NO2, alkyl, cycloalkyl, heterocycloalkyl, haloalkyl, alkylthio, haloalkyloxy, hydroxyalkyl, hydroxyalkylamino, alkylamino, alkylaryl, alkylsulfinyl, alkylsulfonyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, alkoxyalkyl, alkoxy, aryloxy, heteroaryl, aryl, or halogen.
    • 本发明涉及通式(I)的化合物及其盐和生理功能衍生物,其中Y为-NR a R b,-NR c C -ONR a R b,-NR c C -R SNR a R b,-NR c C-NR d N a R b,杂环,-C-ONR a R b,杂环, 或芳基; n为0〜8; m为0或1; r为0〜3; t为0〜3; X是O或N; Z是CH 2,C-O,C-S或单键; Z1是CO-R2,CS-R2,(CH2)t-R2或天然氨基酸的侧链; Z2是CO-R2,CS-R2或(CH2)t-R3或天然氨基酸的侧链; Z3是CO-R2,CS-R2或(CH2)t-R4或天然氨基酸的侧链; Z4是H,烷基,烷氧基或环烷基; R 1,R 2,R 3和R 4彼此独立地是H,OH,SH,NH 2,CN,NO 2,烷基,环烷基,杂环烷基,卤代烷基,烷硫基,卤代烷氧基,羟烷基,羟烷基氨基,烷基氨基,烷基芳基,烷基亚磺酰基,烷基磺酰基, 烷基亚磺酰基烷基,烷基磺酰基烷基,烷氧基烷基,烷氧基,芳氧基,杂芳基,芳基或卤素。