摘要:
Novel tricyclic N-cyanoimine compounds and pharmaceutical compositions of formula (1.0) ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein a, b, c, d, R.sup.1 -R.sup.8, X and Z are defined herein. Such compounds are inhibitors of the enzyme, farnesyl protein transferase. The compounds are useful for inhibiting Ras function and therefore inhibiting the abnormal growth of cells, in a mammals such as a human.
摘要:
Novel compounds of formula are disclosed. Also disclosed is a method of inhibiting farnesyl protein transferase function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the above formula to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being. Also disclosed is a method of effecting an anti-allergic response by administering the compounds.
摘要:
Novel compounds of the formula: or a pharmaceutically acceptable salt or solvate thereof, wherein: a represents N or NO−; R1 and R3 are the same or different and each represents halo; R2 and R4 are the same or different and each is selected from H and halo, provided that at least one of R2 and R4 is H; T is a substituent selected from SO2R or Z is O or S; n is zero or an integer from 1 to 6; R is alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, heterocycloalkyl, or N(R5)2; R5 is H, alkyl, aryl, heteroaryl or cycloalkyl. Also disclosed are methods of inhibiting farnesyl protein transferase and methods for treating tumor cells.
摘要翻译:新的下式化合物或其药学上可接受的盐或溶剂化物,其中:a表示N或NO - ; R 1和R 3相同或不同,各自表示卤素; R 2和 R 4相同或不同,各自选自H和卤素,条件是R 2和R 4中的至少一个为H; T为选自SO 2 R或Z的取代基为O或S; n R为烷基,芳基,芳基烷基,杂芳基,杂芳基烷基,环烷基,杂环烷基或N(R 5)2; R 5为H,烷基,芳基,杂芳基或环烷基 还公开了抑制法呢基蛋白转移酶的方法和治疗肿瘤细胞的方法。
摘要:
Novel compounds of the formula: or a pharmaceutically acceptable salt or solvate thereof, wherein: a represents N or NO−; R1 and R3 are the same or different and each represents halo; R2 and R4 are the same or different and each is selected from H and halo, provided that at least one of R2 and R4 is H; T is a substituent selected from SO2R or: Z is O or S; n is zero or an integer from 1 to 6; R is alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, heterocycloalkyl, or N(R5)2; R5 is H, alkyl, aryl, heteroaryl or cycloalkyl. Also disclosed are methods of inhibiting farnesyl protein transferase and methods for treating tumor cells.
摘要翻译:新的下式化合物或其药学上可接受的盐或溶剂合物,其中:a表示N或NO-; R 1和R 3相同或不同,各自表示卤素; R 2和R 4相同或不同,各自选自 H和卤素,条件是R 2和R 4中的至少一个是H; T是选自SO 2 R的取代基或:Z是O或S; n是0或1-6的整数; R是烷基,芳基,芳基烷基, 杂芳基,杂芳基烷基,环烷基,杂环烷基或N(R5)2; R5是H,烷基,芳基,杂芳基或环烷基。还公开了抑制法呢基蛋白转移酶的方法和治疗肿瘤细胞的方法。
摘要:
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
摘要:
The lactic acid�CH.sub.3 CH(OH)CO.sub.2 H! addition salt of the compound of formula I ##STR1## wherein the molar ratio of lactic acid, preferably L-lactic acid, to the compound of formula I is preferably about 1:1, pharmaceutical compositions of the lactic acid addition salt in an aqueous lactic acid carrier suitable for intravenous administration, and methods of using either of them to treat and/or prevent susceptible fungal infections in a host such as a mammal are disclosed.
摘要:
Disclosed is a process for preparing chiral compounds of the formula (I) ##STR1## wherein: X.sup.1 and X.sup.2 are independently F or Cl; and E is --SO.sub.2 R.sup.2, wherein R.sup.2 is C.sub.1 -C.sub.6 alkyl, --C.sub.6 H.sub.4 CH.sub.3 or --CF.sub.3 ; its enantiomer and racemates thereof, useful in the synthesis of tetrahydrofuran azole antifungals. Novel compounds of the formula ##STR2## wherein: X.sup.1 and X.sup.2 are independently F or Cl; B represents --C(O)Q* or --CH.sub.2 OR"; Q* represents a chiral auxiliary group; R" represents a hydroxy protecting group selected from --CH.sub.2 C.sub.6 H.sub.5, or --C(O)R.sup.1, wherein R.sup.1 is C.sub.1 -C.sub.6 alkyl; and A represents Cl, Br, I or triazolyl; are also disclosed.
摘要翻译:公开了制备式(I)的手性化合物(I)的方法,其中:X 1和X 2独立地是F或Cl; 并且E是-SO 2 R 2,其中R 2是C 1 -C 6烷基,-C 6 H 4 CH 3或-CF 3; 其对映体和外消旋体,可用于四氢呋喃唑类抗真菌剂的合成。 新颖的式(III)化合物或其成分:其中:X 1和X 2独立地为F或Cl; B表示-C(O)Q *或-CH 2 OR“; Q *表示手性辅助基团; R“表示选自-CH 2 C 6 H 5或-C(O)R 1的羟基保护基,其中R 1是C 1 -C 6烷基; A表示Cl,Br,I或三唑基; 也被披露。
摘要:
Ribavirin derivatives represented by formula I wherein at least one of R2, R3 or R5 is a straight or branched chain polyalkylene oxide polymer conjugate, and pharmaceutical compositions containing them as well as their use to treat patients having susceptible viral infections, alone and in combination with a therapeutically effective amount of interferon-alpha are disclosed.
摘要:
A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) alkyl group substituted by one or two groups convertible in vivo into hydroxy moieties, (e.g., a polyether ester, amino acid ester or phosphate ester) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.
摘要:
Ribavirin derivatives represented by the formula II, pharmaceutical compositions containing them as well as methods of using the ribavirin derivatives represented by the formula II for the treatment of susceptible viral infections, for example, chronic hepatitis C infections administrating, the ribavirin derivatives being represented by formula II are disclosed.