摘要:
Compounds of formula (1) are provided: (1) where R1 through R7 are defined herein. The compounds of formula (I) are 5HT2c agonists or partial agonists, and are useful for treating a variety of disorders.
摘要:
UCS1025 derivatives represented by general formula (I) which have an antitumor activity or an antibacterial activity or pharmacologically acceptable salts thereof, (I) wherein R1 represents hydrogen, lower alkyl, etc.; R2 represents hydrogen, or forms a bond, etc. together with R3 or forms -O(C=O)-, etc. together with R4; R3 represents hydrogen or forms a bond, etc. together with R2; R4 represents hydrogen or forms -(C=O)O-, etc. together with R2; R5 represents hydrogen, or forms a bond together with R6; R6 represents hydroxy, or forms a bond together with R5; R7 represents hydrogen, or forms =O together with R8; R8 represents hydroxy or forms =O together with R7; --- represents a single or double bond; and a represents a single bond (i.e., the two carbon atoms bonded to a form a single bond to each other) or an oxygen atom.
摘要:
Pyran derivatives represented by any of chemical formulae (1) to (3). They are highly sensitive to visible light and highly luminescent and hence are useful in various applications in photochemical polymerization, organic electroluminescence, and dye lasers. In chemical formulae (1) to (3), R1 and R2 each independently represents hydrogen, alkyl, alkenyl, or aryl (the alkyl and aryl may be substituted); R3 represents cyano, carboxyl, a carboxylic ester group, amido, or a five- or six-membered heterocycle optionally forming a fused ring; and R4 represents hydrogen, halogeno, cyano, carbonyl, or a substituent derived from carbonyl, provided that R1 and/or R2 may form a cyclic structure in cooperation with the benzene ring bonded thereto.
摘要:
Compounds represented by general formula (I) carrying a tricylic amine substituent optionally having various substituents, their salts, hydrates thereof or drugs containing these compounds as the active ingredient. Because of having favorable antibacterial activities on gram-negative and gram-positive bacteria and being excellent both in the dynamics in vivo and safety, these compounds are useful in treating infectious diseases. In said formula (I), Q represents a partial structure which is preferably represented by formula (a); or (b) and may have various substituents.
摘要:
UCS 1025 derivatives having antitumor activity or antibacterial activity which are represented by formula (I): wherein R 1 represents hydrogen, lower alkyl, etc.; R 2 represents hydrogen, or is combined with R 3 to represent a bond, etc., or is combined with R 4 to represent -O(C=O)-, etc.; R 3 represents hydrogen, etc., or is combined with R 2 to represent a bond, etc.; R 4 represents hydrogen, etc., or is combined with R 2 to represent -(C=O)O-, etc.; R 5 represents hydrogen or is combined with R 6 to represent a bond; R 6 represents hydrogen, etc., or is combined with R 5 to represent a bond; R 7 represents hydrogen or is combined with R 8 to represent =O; R 8 represents hydroxy or is combined with R 7 to represent =O; ---- represents a single bond or a double bond, and a represents a single bond (two carbon atoms to which a is bound are combined to form a single bond) or an oxygen atom, or pharmaceutically acceptable salts thereof.
摘要翻译:由式(I)表示的具有抗肿瘤活性或抗菌活性的UCS 1025衍生物:其中R 1表示氢,低级烷基等; R 2表示氢,或与R 3结合以表示键等,或与R 4结合以表示-O(C = O) - 等; R 3表示氢等,或与R 2结合以代表键等; R 4表示氢等,或与R 2结合代表 - (C = O)O-等; R 5表示氢或与R 6结合以表示键; R 6表示氢等,或与R 5结合以表示键; R 7代表氢或与R 8结合代表= O; R 8表示羟基或与R 7结合代表= O; ----表示单键或双键,a表示单键(键合有两个碳原子结合形成单键)或氧原子,或其药学上可接受的盐。
摘要:
Antibacterical coumpounds having formula (I) and the pharmaceutically acceptable salts, esters and amides thereof, preferred examples of which include those coumpounds wherein R1 is cycloalkyl of from three to eight carbon atoms or substituted phenyl; R2is selected from the group consisting of (a) halogen, (b) loweralkyl, (c) loweralkenyl, (d) cycloalkyl of from three to eight carbons, (e) cycloalkenyl of from four to eight carbons, (f) loweralkoxy, (g) aryloxy, (h) aryl(loweralkyl)oxy, (i) aryl(loweralkyl), (j) cycloalkyl(loweralkyl), (k) amino, (l) (loweralkyl)amino, (m) aryl(loweralkyl)amino, (n) hydroxy substituted (loweralkyl)amino, (o) phenyl, (p) substituted phenyl, (q) bicyclic nitrogen-containing heterocycle, (r) nitrogen-containingaromatic heterocycle, and (s) nitrogen-containing heterocycle having formula (Ia) where x is between zero and three; R3 is halogen; R4 is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group; R5 is hydrogen, loweralkyl, halo(loweralkyl), or -NR?13R14; and R6¿ is loweralkyl, as wellas pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.
摘要:
Novel compounds are disclosed having formula (I) as well as pharmaceutically acceptable salts, esters and amides thereof, wherein R1 is selected from (a) loweralkyl, (b) loweralkenyl, (c) halo(loweralkyl), (d) loweralkoxy, (e) cycloalkyl of from 3 to 8 carbons, (f) phenyl, (g) halo, (h) cyano, (i) nitro, (j) bicycloalkyl, (k) loweralkynyl, (l) alkoxycarbonyl, (m) nitrogen-containing aromatic heterocycle and (n) a group of the formula -NR7R8; R2 is selected from the group consisting of halogen, loweralkoxy, carbocyclic aryloxy or carbocyclic aryl(loweralkyl)oxy, loweralkyl, loweralkenyl, cycloalkyl of from 3 to 8 carbons, cycloalkenyl of from 4 to 8 carbons, carbocyclic aryl(loweralkyl), cycloalkyl(loweralkyl), phenyl, amino, (loweralkyl)amino, carbocyclic aryl(loweralkyl)amino, hydroxy-substituted (loweralkyl)amino, nitrogen-containing aromatic heterocycle, bicyclic nitrogen-containing heterocycle and nitrogen-containing heterocycle having formula (II), wherein x is 0 to 3; R9 is selected from (a)-(CH¿2?)m-, wherein m is 1, 2 or 3, and (b) -(CH2)nR?10(CH¿2)p-, wherein R10 is selected from S, O and N, n is 1 or 2, and p is 1 or 2; and Y is a non-hydrogen substituent independently selected from loweralkyl, halo(loweralkyl), loweralkoxy, hydroxy-substituted loweralkyl, hydroxy, amino(loweralkyl), halogen and a group having the formula -NR?11R12; R3¿ is hydrogen, halogen or loweralkoxy; R4 is selected from the group consisting of hydrogen, loweralkyl, a pharmaceutically acceptable cation and a prodrug ester group; R5 is selected from the group consisting of hydrogen, halogen, hydroxy, loweralkyl, halo(loweralkyl), loweralkoxy and a group having the formula -NR13R14; and A is N or CR6, wherein R6 is selected from hydrogen, halogen, loweralkyl, halo(loweralkyl), hydroxy-substituted loweralkyl, loweralkoxy(loweralkyl), loweralkoxy and amino(loweralkyl) or, alternatively, R?1 and R6¿, taken together with the atoms to which they are attached, form a 6-membered saturated ring which may contain an oxygen or a sulfur atom and which may be substituted with loweralkyl; with the proviso that when R5 is hydrogen and A is CH then either (a) R?1 is NR7R8¿, or (b) R2 is a group having formula (III), wherein x is 1-3 and R9 and Y are as defined above.
摘要:
Novel fused polycyclic heterocycle derivatives having excellent antitumor effects and a process for producing the same. A compound represented by the following general formula (I) or pharmacologically acceptable salts thereof: wherein the ring A represents an optionally substituted monocyclic aromatic ring or a dicyclic fused ring in which at least one of the rings is an aromatic ring; the ring B represents pyrrole, 4H-1,4-oxazine, 4H-1,4-thiazine or 4(1H)-pyridone; the ring C represents an optionally substituted, monocyclic or dicyclic fused aromatic ring; and Y represents a group represented by the formula -e-f (wherein e represents a lower alkylene; and f represents amidino, guanidino or amino optionally substituted by optionally hydroxylated or optionally lower-alkylaminated lower alkyl; provided that the cases where the rings A and B are both optionally substituted monocyclic aromatic rings are excluded. Which has an excellent antitumor activity.