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Patent

Polyaryl antitumor agents

TL;DR: A compound of the formula: Ar.sub.1 -B--Ar.sub-2 where Ar 1 is unsubstituted or substituted phenyl, thienyl, furanyl, or pyrrolyl, in which each substituent of the substituted persons, such as phenyl and pyrronyl, independently, is aldehyde, acyl, ester, carboxyl, amido, nitrile, nitro, cyano, acetal, oxoalkyl, aminoalkyl and oxo-alkyl as discussed by the authors.
Abstract: A compound of the formula: Ar.sub.1 --B--Ar.sub.2 wherein Ar 1 is unsubstituted or substituted phenyl, thienyl, furanyl, or pyrrolyl, in which each substituent of the substituted phenyl, substituted thienyl, substituted furanyl, and substituted pyrrolyl, independently, is aldehyde, acyl, ester, carboxyl, amido, nitrile, nitro, cyano, acetal, ketal, oxoalkyl, aminoalkyl, hydroxyalkyl, haloalkyl, iminoalkyl, acid halide, aminoalkylaminoalkyl, aminoalkylaminoalkylamino, hydroxyalkylaminoalkyl, or hydroxyalkylaminoalkylaminoalkyl; B is, --CH═CH--, or --C C--, in which R is H, alkyl, hydroxyl, alkoxy, ester, aldehyde, hydroxyalkyl, aminoalkyl, carboxyl, --CH(OR 1 ) 2 , or NR 2 R 3 , where each R 1 , independently, is H, alkyl, or acyl; and each of R 2 and R 3 , independently, is H, alkyl, hydroxyalkyl, or aminoalkyl; and Ar 2 is substituted phenyl, substituted thienyl, substituted furanyl, or substituted pyrrolyl, in which each substituent of the substituted phenyl, substituted thienyl, substituted furanyl, and substituted pyrrolyl, independently, is amido, nitrile, nitro, cyano, acetal, ketal, oxoalkyl, aminoalkyl, haloalkyl, iminoalkyl, acid halide, aminoalkylaminoalkyl, aminoalkylaminoalkylamino, hydroxyalkylaminoalkyl, or hydroxyalkylaminoalkylaminoalkyl; or a salt thereof. Also disclosed is a composition which contains a pharmaceutical acceptable carrier and an effective amount of a compound of the above formula.
Citations
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Patent
15 Sep 2000
TL;DR: In this paper, the authors present methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain of function, ptc loss of function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to induce an abnormal growth state.
Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.

252 citations

Patent
07 Aug 2003
TL;DR: In this article, the authors define caracterises en ce que.bullet, i.e., oxygene ou soufre,.Bullet, and X represent oxygenes, NH ou -N(C1-C6)alkyle,, and Y represent pyridyle, aryle, cycloalkenyle.
Abstract: Composes de formule (I) caracterises en ce que .bullet. X represente oxygene ou soufre, .bullet. Y represente oxygene,-NH ou -N(C1-C6)alkyle, .bullet. Ra represente hydrogene, halogene, (C1-C3)alkyle, hydroxy, ou (C1-C3)alkoxy, .bullet. Rb represente hydrogene, halogene, ou (C1-C3)alkyle, .bullet. A represente phenyle, pyridyle, (C5-C6)cycloalkyle ou (C5-C6)cycloalkenyle, .bullet. R1 et R2 representent chacun un groupement choisi parmi hydrogene, halogene, cyano, nitro, halogenoalkyle, halogenoalkoxy, alkyle, alkenyle, alkynyle, -OR4, -NR4R5, -S(O)nR4, -C(O)R4, -C02R4, -OC(O)R4, -C(O)NR4R5, -NR5-C(O)R4, -NR5-S02R4, -T-CN, -T-OR4, -T-OCF3, -T-NR4R5, -TS(O)nR4, -TC(O)R4, -T-C02R4, -TOC(O)R4, -TC(O)NR4R5, -T-NR4-C(O)R5, -T-NR4-S02R5, -R6, et -T-R6 dans lesquels n, T, R4, R5 et R6 sont tels que definis dans la description, .bullet. R3 represente un groupement -R7 ou -U-R11, dans lesquels R7 represente hydrogene, alkyle, aryle, cycloalkyle ou heterocycle, U represente une chaine alkylene lineaire ou ramifiee, et R11, est tel que defini dans la description, leurs isomeres optiques ou leurs sels d'addition a un acide ou a une base pharmaceutiquement acceptable, et leur utilisation en tant qu'inhibiteur de metalloproteinase et plus specifiquement de la metalloproteinase -12.
References
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Journal ArticleDOI
TL;DR: In this article, the reaction of benzene solutions of arylacetylenes with 1 equiv of chloroacetone and 2 equiv. of Et3N, using a mixture of (PPh3)4 Pd and CuJ as catalyst, affords 1,4-diaryl-butadiynes in very good yields.

173 citations

Journal ArticleDOI
TL;DR: In this paper, the linear optical properties of poly(2,7]-2,2'-bithiophenylylene]-4,9-diphenyl-1,6-anthrazoline were investigated.
Abstract: Poly(2,7-[2,2'-bithiophenylylene]-4,9-diphenyl-1,6-anthrazoline) and poly(2,7-[2-thienylethynyl-2-thienyl]-4,9-diphenyl-1,6-anthrazoline) were prepared. These polymers showed significant changes in electronic structures as evidenced in the linear optical properties compared to the known poly(2,7-[p,p'-biphenylyl]-4,9-diphenyl-1,6-anthrazoline). Smaller band gaps (∼2 eV) were observed for these polymers.

153 citations

Patent
09 Jul 1991
TL;DR: In this article, a compound represented by the formula (16) is defined, wherein each of R 16-1 and R 16 -2 is a substituted or unsubstituted alkyl group or a substituted-or-uniform aromatic ring group; each of X is an oxygen atom, a sulfur atom, =C(CN) 2, and each of x is a halogen atom.
Abstract: 1. An electrophotographic photosensitive member comprising an electroconductive support and a photosensitive layer on said electroconductive support, said a compound represented by the formula (16) wherein each of R 16-1 and R 16-2 is a substituted or unsubstituted alkyl group or a substituted or unsubstituted aromatic ring group; each of R 16-3 and R 16-4 is a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aralkyl group or a substituted or unsubstituted aromatic ring group; X is an oxygen atom, a sulfur atom, =C(CN) 2 , each of R 16-5 and R 16-6 is a halogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aromatic ring group or a substituted or unsubstituted heterocyclic ring group; each of R 16-7 and R 16-8 is a hydrogen atom, a cyano group, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aromatic ring group or a substituted or unsubstituted heterocyclic ring group, provided that R 16-5 and R 16-6 as well as R 16-7 and R 16-8 are not hydrogen atoms at the same time.

139 citations