Compounds useful as cytotoxic agents are selected from the group consisting of compounds of Formula (I) and compounds of Formula (II), wherein: R1, R2, R3 and R4 are each independently selected from the group consisting of: hydrogen, alkyl, carboxy, alkoxy, hydroxyalkyl, alkylcarbonyl; alkylcarbonyloxy; alkyl substituted with alkylcarbonyloxy, thiophenylcarbonyl; nitro and cyano; thiophenyl and thiophenylthiophenyl, each of which may be unsubstituted or substituted with alkyl, carboxy, alkoxy, hydroxyalkyl, alkylcarbonyl; alkylcarbonyloxy; alkyl substituted with alkylcarbonyloxy, nitro or cyano; subject to the proviso that at least one of R1, R2, R3 and R4 is not hydrogen; A1 and A2 are each selected from the group consisting of: =O, alkyl, alkoxy, and alkylcarbonyloxy; and the pharmaceutically acceptable salts thereof. When A1 and A2 are =O, the center ring has only two, and not three, double bonds.

Naphtho- and dihydrobenzo-thiophene derivatives as cytotoxic antitumor agents

PURPOSE:To obtain optimum preheating and after glow times by forming a large diameter part at the upper end of a holding tube, caulking and fixing the large-diameter part to the inner wall of a housing, forming a predetermined gap between the outer periphery of a general part and the inner periphery of the housing, and burying a resistor within a holding tube filled with an insulator. CONSTITUTION:An insulator 5 is filled in a holding tube 1, and a resistor 4 is buried within the lower half part of the tube 1. A metal ring body 13 is brazed and fixed to the outer circumference of the upper end 12 of the holding tube 1 to form a large diameter part. The upper edge 212 of an upper end opening 21 of the housing 2 is caulked so that the upper edge 212 covers the outer periphery of the ring body 13, and the holding tube 1 is fixedly located within the housing 2. That is, the inner periphery of the opening part 21 beforehand has an annular shoulder 211. Under this condition, an interval C having a predetermined size obtained by subtracting a predetermined caulking depth from the difference between the outer diameter of the general part and the outer diameter of the ring body, is formed between the outer periphery of the general part 11 of the holding tube other than the upper end 12 and the inner periphery of the housing 2. In the case of varying the size of the gap, the inner diameter of the housing and the outer diameter of the ring body in accordance therewith are varied.

Self-control type glow plug

PURPOSE:To obtain an optimum exposure condition by comparing and deciding an image characteristic by plural deciding methods. CONSTITUTION:A negative reading part 8 is positioned in the pre-stage of a negative printing part 4, and a transmission density of a film 2 is read at every separate frame, and also, by a picture element unit. A negative discrimination processing part 9 inputs an image signal from the reading part 8, and decides an optimum printing condition. As for a deciding means, plural deciding means such as a means 91 by a statistical method, and a means 92 by a pattern recognitory method, etc. are provided. A condition determining means 94 discriminates a result of decision by the means 91, 92, etc. by the statistical method or an evaluating expression, and executes printing by one decided value. In case it has been decided that printing is impossible, an operator executes a decision. Not only an exposure correction value selected from plural negative decision result, but also a summing exposure correction quantity can be determine. In this way, the most desirable printing condition can be obtained.

Discriminating method for characteristic of film image

NEW MATERIAL:A compound (salt) shown by the formula I (one of X and Y is O, and the other is methylene or carbonyl; A is H, halogen, methyl, acetyl, cyanoethyl, etc.; B is H, halogen, methyl, alpha-cyanoethyl, methoxycarbonylmethyl, etc.; C is H, halogen, methyl, methoxycarbonylmethyl, etc.; D and E are H, halogen, or methyl; with the proviso that the case wherein X is O, Y is carbonyl, and A-E are H is omitted). EXAMPLE:9H-Thieno[3,2-b][1] benzopyran-2-propionic acid. USE:An antiphlogistic. PROCESS:For example, a 3-alkoxythiophene is reacted with o-anisoyl chloride to give a compound shown by the formula II, which is subjected to ring closure to give 9H-thieno[3,2-b][1] benzopyran shown by the formula III, which is further acetylated, converted into a nitrile group, and hydrolyzed, to give a compound shown by the formula I .

9h-thieno(3,2-b) or 4h-thieno(2,3-b)(1) benzopyran derivative

NEW MATERIAL:A compound expressed by formula I (R is H, 1-12C alkyl, 4-7C cycloalkyl or phenyl; A is cyclohexyl, 1- or 2-methyl-3-hexyl, 1- or 2- methylhexyl, 2-phenethyl, etc.; the double bond between the 4- and 5-positions is E or/and Z; the asymmetric center of A is R- or/and S-configuration). EXAMPLE:3-(4'-Carboxy-3'-cyclohexyl-trans-1'-propenyl)-7(R)-hy-droxy-(1S, 5S)-cis- bicyclo[3.3.0]oct-2-ene. USE:An ameliorant of circulation, e.g. ameliorant of blood stream, antithrombosis, etc., or antiulcer agent. PREPARATION:A compound expressed by formula II is passed through compounds expressed by formulas III-VI (R is any one of groups in R except H; formula VII is tert-butyldimethylsilyl; THP is tetrahydro-2-pyranyl) to give the compound expressed by formula I (R is R ), which is then hydrolyzed to afford the compound expressed by formula I (R is H).

Prostaglandin i2 analogous compound and pharmaceutical containing said compound

NEW MATERIAL:A compound of formula I [R is H, alkyl, aralkyl or (substituted) phenyl; R is H, alkyl, aralkyl, (substituted) phenyl or (substituted) naphthyl; X is H, acetyl, alpha-hydroxyethyl, vinyl, alpha-cyanoethyl or alpha-(hydroxycarbonyl)ethyl]. EXAMPLE:1, 3-Dimethyl-6-(alpha-hydroxycarbonylethyl)-1, 4-dihydro[1]benzopyrano[2, 3-c]pyrazole. USE:An anti-inflammatory agent useful also as an intermediate for preparing medicines and agricultural chemicals. PROCESS:A compound of formula II is reduced to give a compound of formula III, which is then subjected to the Friedel-Crafts reaction to afford a compound of formula IV. The resultant compound of formula IV is further reacted with p-tosylmethyl isocyanide to afford a compound of formula V, which is then hydrolyzed.

Hayashi Yoshio

Papers

9h-thieno(3,2-b) or 4h-thieno(2,3-b)(1) benzopyran derivative

Prostaglandin i2 analogous compound and pharmaceutical containing said compound

1,4-dihydro(1)benzopyrano(2,3-c)pyrazole derivative