摘要:
This invention relates to tri- and tetra-substituted-oxetanes, e.g. (.+-.)-cis- and (.+-.)-trans-2-[(4-(4-isopropylpiperazin-1-yl)phenoxy)methyl]-4-(2,4-dihalophenyl)-4-[1H-1,2,4-triazol-1-yl)-methyl]oxetane and tri- and tetra-substituted-tetrahydrofurans, e.g. (.+-.)-cis- and (.+-.)-trans-1-[4-[[2-(2,4-dihalophenyl)tetrahydro-2-[(1H-azol-1-yl)methyl]-5-furanylmethoxy]phenyl]-4-yl-1-substituted piperazine-3-one and related derivatives which exhibit antifungal and antiallergy activities, pharmaceutical composition thereof, methods of their use in treating or preventing susceptible fungal infections and allergic reactions in a host including warm-blooded animals such as humans.
摘要:
A compound represented by formula I, Ar.sub.1 --O--M--O--Ar.sub.2, wherein Ar.sub.1 and Ar.sub.2 are independently substituted phenyl or substituted pyridinyl, the substituents on said phenyl or pyridinyl being independently selected from one, two or three of (C.sub.1 -C.sub.10) alkyl, (C.sub.1 -C.sub.10) alkoxy, halogen, carbamyl, (C.sub.1 -C.sub.10) alkoxycarbonyl, oxazoyl, and (C.sub.1 -C.sub.10) alkyl substituted by halogen, (C.sub.1 -C.sub.10) alkoxy, hydroxy, or (C.sub.1 -C.sub.10) alkoxycarbonyl; ##STR1## O is oxygen; R' is (C.sub.1 -C.sub.3 alkyl or H; A is oxygen or sulfur; Q is selected from hydrogen, halogen, nitro, (C.sub.1 -C.sub.6) alkyl, (C.sub.1 C.sub.6) perhaloalkyl, (C.sub.1 -C.sub.6) alkylthio (C.sub.1 -C.sub.6) or alkyl sulfonyl; the dotted lines in M-3 and M-4 between carbons, 2 and 3 and 3 and 4, and 4 and 5 mean that the bonds between carbons 2 and 3, and 3 and 4, and 5 and 6, may each be a single or double bond; n=1 or 2; m=1 or 2; p=0 or 1; or pharmaceutically acceptable salts thereof as well as pharmaceutical compositions containing such compounds and methods of treating or preventing viral infections, especially picornaviral infections using the compounds of formula I, 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 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.
摘要:
A method for treating a patient having chronic hepatitis C infection to eradicate detectable HCV-RNA involving a combination therapy using a therapeutically effective amount of ribavirin derivative of formula I and a therapeutically effective amount of interferon-alpha for a time period of from 20 up to 80 weeks.
摘要:
5′-Amino acid esters of ribavirin represented by formula I: wherein R is CH3CH(NH2)—CO—, CH3CH2(CH3)CHCH(NH2)—CO—or H2N(CH2)4CH(NH2)—CO—; preferably R is or a pharmaceutically acceptable salt thereof, e.g., trifluoroacetate, tosylate, mesylate, and chloride, pharmaceutical compositions containing them as well as methods of treating patients having susceptible viral infections, e.g., chronic hepatitis C infections by administering a therapeutically effective amount of a ribavirin derivative, alone or in combination with a therapeutically effective amount of interferon-alpha are disclosed.
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.