Abstract:
The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.
Abstract:
A compound of formula (I) useful for the treatment of cancer, inflammation and inflammatory disorders, and a pharmaceutical composition containing the compound.
Abstract:
Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where V, W, R1, R2, R3 and R4 are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
Abstract:
Compounds having the formula or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L2—, and (i) heterocyclic-L2—; R2 is selected from (a) (b) —C(O)NH—CH(R14)—C(O)OR15, (d) —C(O)NH—CH(R14)—C(O)NHSO2R16, (e) —C(O)NH—CH(R14)-tetrazolyl, (f) —C(O)NH-heterocyclic, and (g) —C(O)NH—CH(R14)—C(O)NR17R18; R3 is substituted or unsubstituted heterocyclic or aryl, substituted or unsubstituted cycloalkyl or cycloalkenyl, and —P(W)RR3RR3′; R4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; L1 is absent or is selected from (a) —L4—N(R5)—L5—, (b) —L4—O—L5—, (c) —L4—S(O)n—L5— (d) —L4—L6—C(W)—N(R5)—L5—, (e) —L4—L6—S(O)m—N(R5)—L5 —, (f) —L4—N(R5)—C(W)—L7—L5—, (g) —L4—N(R5)—S(O)p—L7—L5—, (h) optionally substituted alkylene, (i) optionally substituted alkenylene, (j) optionally substituted alkynylene (k) a covalent bond, (l) and (m) are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases.
Abstract translation:具有式的化合物或其药学上可接受的盐,其中R 1是(a)氢,(b)低级烷基,(c)烯基,(d)烷氧基,(e)硫代烷氧基,(f)卤素,(g)卤代烷基,(h) 芳基-L2-和(i)杂环-L2-; R 2选自(a)(b)-C(O)NH-CH(R 14)-C(O)OR 15,(d)-C(O)NH-CH(R 14)-C(O)NHSO 2 R 16 e)-C(O)NH-CH(R14) - 四唑基,(f)-C(O)NH-杂环基和(g)-C(O)NH-CH(R14)-C(O)NR17R18; R 3是取代或未取代的杂环或芳基,取代或未取代的环烷基或环烯基,和-P(W)RR 3 R R 3'; R4是氢,低级烷基,卤代烷基,卤素,芳基,芳基烷基,杂环或(杂环)烷基; (a)-L4-N(R5)-L5-,(b)-L4-O-L5-,(c)-L4-S(O)n-L5-(d) - L4-L6-C(W)-N(R5)-L5-,(e)-L4-L6-S(O)mN(R5)-L5 - ,(f)-L4-N(R5)-C W)-L7-L5-,(g)-L4-N(R5)-S(O)p-L7-L5-,(h)任选取代的亚烷基,(i)任选取代的亚烯基,(j)任选取代的亚炔基 (k)共价键,(1)和(m)是蛋白质异戊二烯基转移酶的抑制剂。 还公开了蛋白质异戊二烯转移酶抑制组合物和抑制蛋白质异戊二烯转移酶的方法。
Abstract:
Heteroaromatic compounds of the formulae IA and IB ##STR1## where the dashed line is a double bond between the carbon atom and a Z atom, and the index and the substituents have the following meanings:R.sup.1alkyl, alkoxy, alkylaminoR.sup.2alkyl;Aa direct bond; alkylene, alkenylene, alkynylene;O, S, S-oxides, N and alkylene derivatives or oxime radicals thereofBhydrogen, halogen,alkyl, alkenyl, alkynyl;cycloalkyl, cycloalkenyl, cycloalkynyl, heterocyclyl, aryl, hetarylUCH.sub.2, CHCl, CHR.sup.2 or NOR.sup.2 ;Xhydrogen, cyano, nitro, halogen,alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, hetaryl; oxi- and thio derivatives thereof, carbonyl derivatives thereof, carbonyloxy derivatives thereof, amino derivatives thereof, oxime derivatives thereof,amino which may bear one or two of the abovementioned groups;m1 or 2,Yoxygen or sulfur;Z.sup.1 -Z.sup.2, Z.sub.3 -Z.sub.4,together with the carbon atom to which they are bonded, are the radical of a heteroaromatic, and fungicides containing these compounds.
Abstract:
Cephem derivatives of the general formula ##STR1## in which the R.sub.2 O group is in the syn-position, a process for their manufacture and pharmaceutical formulations which are active against bacterial infections and contain these compounds.
Abstract:
A cephalosporin intermediate of the formula ##STR1## where R.sub.3 is carboxyl, carboxylate, or a carboxylic acid ester group and,R.sub.8 and R.sub.9 are each independently hydrogen, halogen,(C.sub.1-4) alkyl, hydroxy, carboxamido,(C.sub.1-4) alkoxycarbonyl, amino,mono- (C.sub.1-4) alkylamino, di- (C.sub.1-4) alkylamino, ortogether are a 5 or 6-membered carbocyclic ring or an alkali metal, alkaline earth metal, or acid addition salt thereof. Valuable cephalosporin antibiotics can be produced from the cephalosporin intermediate products of formula I.