Abstract: A fluorine-containing sulfonic acid salt or a compound having a fluorine-containing sulfonic acid group, either of which having a structure represented by the following general formula (1), is provided. Such a salt or compound can act as a suitable photo-acid generator, and can form a resist pattern having excellent sensitivity, resolution and mask-dependence. [In general formula (1), R represents a substituted or unsubstituted linear or branched monovalent hydrocarbon group having 1 to 30 carbon atoms, a substituted or unsubstituted monovalent hydrocarbon group having 3 to 30 carbon atoms and a cyclic or a partially cyclic structure, a substituted or unsubstituted aryl group having 6 to 30 carbon atoms, or a substituted or unsubstituted monovalent heterocyclic organic group having 4 to 30 carbon atoms.

Abstract: The subject of the invention is process for the preparation of the prostaglandin amides of the general formula I, where in the formula the bonds marked with dotted lines may be single or double bonds, in the case of double bounds at positions 5,6 and 13,14 they may be in cis or in trans orientation, Q stands for a hydroxyl-group and Z stands for a hydroxyl- or oxo-group, R1 and R2 independently represent hydrogen atom or a straight or branched C1-10 alkyl- or aralkyl- group, optionally substituted with —ONO2 group, or an aralkyl- or aryl- group, which contains heteroatom, R3 represents a straight or branched, saturated or unsaturated C4-6 hydrocarbon group, or a C4-10 alkylcycloalkyl- or cycloalkyl- group, or an optionally with alkyl group or halogen atom substituted phenyl-, C7-10 alkylaryl- or hetaryl- group, Y represents (CH2), group or 0 atom or S atom, and where n=0-3.

Abstract: An object of the present invention is to provide an auxin biosynthesis inhibitor superior to L-AOPP. The object can be attained by a compound represented by general formula (I): wherein, R1 to R5 and X are the same as defined in the specification or a salt or solvate thereof.

Abstract: Disclosed are two new crystalline forms, ? and ?, of perindopril erbumine. Those forms are suitable as therapeutic active substances for medicaments for the treatment of cardiovascular diseases, especially high blood pressure and heart failure. The ? crystalline form is obtained in the crystallization of perindopril erbumine at from 30 to 45° C., preferably from 34 to 45° C., from MTBE containing from 1.5 to 2.5% (v/v) water; the crystallization is advantageously carried out with stirring. If the water is then removed, advantageously by azeotropic distillation, preferably at from 35 to 37° C., and stirring is then continued for at least 15 h at from 30 to 45° C., preferably from 35 to 37° C., the ? crystalline form is converted to the ? crystalline form. The ? crystalline form can also be obtained by stirring the ? or ? crystalline form at from 33 to 38° C. in tert.-butyl methyl ether containing from 0.9 to 1.4% (v/v) water with seeding with the ? crystalline form.

Abstract: Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.

Abstract: Disclosed are two new crystalline forms, ? and ?, of perindopril erbumine. Those forms are suitable as therapeutic active substances for medicaments for the treatment of cardio-vascular diseases, especially high blood pressure and heart failure. The ? crystalline form is obtained in the crystallization of perindopril erbumine at from 30 to 45° C., preferably from 34 to 45° C., from MTBE containing from 1.5 to 2.5% (v/v) water; the crystallization is advantageously carried out with stirring. If the water is then removed, advantageously by azeotropic distillation, preferably at from 35 to 37° C., and stirring is then continued for at least 15 h at from 30 to 45° C., preferably from 35 to 37° C., the ? crystalline form is converted to the ? crystalline form. The ? crystalline form can also be obtained by stirring the ? or ? crystalline form at from 33 to 38° C. in tert.-butyl methyl ether containing from 0.9 to 1.4% (v/v) water with seeding with the ? crystalline form.

Abstract: Compounds having two reactive functional groups are described that can be used as a tethering compound to immobilize an amine-containing material to a substrate. The first reactive functional group can be used to provide attachment to a surface of a substrate. The second reactive functional group is a N-sulfonyldicarboximide group that can be reacted with an amine-containing material, particularly a primary aliphatic amine, to form a connector group between the substrate and the amine-containing material. The invention also provides articles and methods for immobilizing amine-containing materials to a substrate.

Abstract: Compounds having two reactive functional groups are described that can be used as a tethering compound to immobilize an amine-containing material to a substrate. The first reactive functional group can be used to provide attachment to a surface of a substrate. The second reactive functional group is a N-sulfonyldicarboximide group that can be reacted with an amine-containing material, particularly a primary aliphatic amine, to form a connector group between the substrate and the amine-containing material. The invention also provides articles and methods for immobilizing amine-containing materials to a substrate.

Abstract: Compounds having two reactive functional groups are described that can be used as a tethering compound to immobilize an amine-containing material to a substrate. The first reactive functional group can be used to provide attachment to a surface of a substrate. The second reactive functional group is a N-sulfonyldicarboximide group that can be reacted with an amine-containing material, particularly a primary aliphatic amine, to form a connector group between the substrate and the amine-containing material. The invention also provides articles and methods for immobilizing amine-containing materials to a substrate.

Abstract: Compounds having two reactive functional groups are described that can be used as a tethering compound to immobilize an amine-containing material to a substrate. The first reactive functional group can be used to provide attachment to a surface of a substrate. The second reactive functional group is a N-sulfonyldicarboximide group that can be reacted with an amine-containing material, particularly a primary aliphatic amine, to form a connector group between the substrate and the amine-containing material. The invention also provides articles and methods for immobilizing amine-containing materials to a substrate.

Abstract: The present invention provides novel fluorescent compounds and covalent attachment chemistries which facilitate the use of these compounds as labels for ultrasensitive and quantitative flourescent detection of low levels of biomolecules. In a preferred embodiment, the flourescent labels of this invention are novel derivatives of the hydroxy-pyrene trisulphonic and disulphonic acids which may be used in any assay in which radioisotopes, colored dyes or other fluorescent molecules are currently used. Thus, for example, any assay using labeled antibodies, proteins, oligonucleotides or lipids, including fluorescent cell sorting, fluorescence microscopy (including dark-field microscopy), fluorescence polarization assays, ligand, receptor binding assays, receptor activation assays and diagnostic assays can benefit from use of the compounds disclosed herein.

Abstract: A pharmaceutical composition which comprises a compound of formula (I) or a pharmaceutically acceptable salt, ester or amide thereof, which is an inhibitor of monocyte chemoattractant protein-1, and wherein A and B form an optionally substituted alkylene chain so as to form a ring with the carbon atoms to which they are attached; X is CH2 or SO2, R1 is an optionally substituted aryl or heteroaryl ring; R2 is a specified organic group such as carboxy, and R3 is hydrogen or a specified organic group; in combination with a pharmaceutically acceptable carrier. Certain compounds of formula (I) are novel and are claimed as such.

Abstract: Oleamide is an endogenous fatty acid primary amide that possesses sleep-inducing properties in animals and has been shown to effect seratonergic systems and block gap junction communication in a structurally specific manner. Certain agents can serve both as an oleamide agonist and as an inhibitor of fatty acid amide hydrolase. Fatty acid amide hydrolase is responsible for the rapid inactivation of oleamide in vivo. The structural features of oleamide required for inhibition of gap junction-mediated chemical and electrical transmission in rat glial cells are defined. Effective inhibitors fall into two classes of fatty acid primary amides of which oleamide and arachidonamide are the prototypical members. Of these two, oleamide constitutes the most effective and its structural requirements for inhibition of the gap junction are well defined.

Abstract: The present invention relates to compounds that are inhibitors of interleukin-1.beta. converting enzyme that have the Formula II ##STR1## This invention also relates to a method of treatment of stroke, inflammatory diseases, septic shock, reperfusion injury, Alzheimer's disease, shigellosis, and to a pharmaceutically acceptable composition that contains a compound that is an inhibitor of interleukin-1.beta. converting enzyme.

Abstract: Method for the preparation of N-alkoxy-(tetra- or hexahydro)-phthalimide according to formula I ##STR1## R.sub.1 being methyl or ethyl and R.sub.2 and R.sub.3 being each independently of one another hydrogen or alkyl with 1-4 C atoms or R.sub.2 and R.sub.3 together with the carbon atom to which they are bonded forming a ring with 5 or 6 C atoms, wherein the salt of the corresponding N-hydroxy-(tetrahydro- or hexahydro)-phthalimide according to formula II: ##STR2## with R.sub.2 and R.sub.3 as defined above and M being an alkali metal, is brought into contact with R.sub.1 Cl as alkylating agent, wherein R.sub.1 has the aforementioned meaning.The N-alkoxy-(tetra- or hexahydro)-phthalimide can afterwards be converted with the aid of hydroxylamine sulphate into the corresponding alkoxyamine after which the alkoxyamine obtained can be isolated. In this manner a simple and commercially attractive process for the preparation of O-(m)ethylhydroxylamine can be implemented.

Abstract: Fibrinogen receptor antagonists having the formula ##STR1## where L is L is (CH.sub.2).sub.p, where p is 1 or 2; and Z is --CR.sup.1 .dbd.CR.sup.

Abstract: Provided is a long chain carboxylic acid imide ester (I) represented by the following general formula (I) ##STR1## wherein W is a divalent long chain hydrocarbon group which may optionally be interrupted by one or more groups each independently selected from the group consisting of an oxygen atom, a sulfur atom, and a group of --N(R.sup.1)-- (R.sup.1 being a lower alkyl group) and X represents a divalent hydrocarbon group which may optionally be substituted, or salts thereof. The above long chain carboxylic acid imide ester or its salts is useful for modifying enzymes or proteins having biological activities to give their derivatives which have, while retaining most of the original biological activities, an extremely prolonged plasma half-life as compared with the proteins and have no antigenecities and can be administered to animals.

Abstract: A bisphosphonic acid derivative of the formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein A is ##STR2## each of R.sup.3 and R.sup.4, which may be the same or different, is (i) a hydrogen atom, (ii) a C.sub.1-6 alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a C.sub.1-6 alkyl-carbonyl group, a C.sub.2-6 alkenyl-carbonyl group, a C.sub.2-6 alkynyl-carbonyl group R.sup.5 and R.sup.6, which may be the same or different, is a hydrogen atom, a hydroxyl group, a halogen atom, a cyano group, a carbamoyl group, an aralkyl group, a substituted or unsubstituted phenyl group, a substituted or unsubstituted amino group, a C.sub.1-6 alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group;each of m and n is 0 or a positive integer, provided that (m+n) is from 2 to 5; andR is a hydrogen atom, a C.sub.1-8 alkyl group or a C.sub.7-15 aralkyl group.

Abstract: Water-soluble cyclic imide thione activated polyalkylene oxides having improved hydrolytic stability are disclosed. Methods of forming and conjugating the activated polyalkylene oxides with biologically active nucleophiles are also disclosed.

Abstract: Plant growth regulators comprising, as an active ingredient, a substituted dicarboxylic acid derivative having the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same as defined in the present specification, the substituted dicarboxylic acid derivatives, and processes for preparing the same, are disclosed. The plant growth regulators provided according to the present invention have a regulating activity on plant growth; more specifically, an action thereof of lowering the content of endogenous ethylene in a plant is utilized.

Abstract: Hydroxylamine derivatives have the general formula IAryl--A--O--B IwhereAryl is an unsubstituted or substituted, mononuclear or binuclear, isocyclic radical;A is a 1,4-butenylene group of the general formulae IIa or IIb ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -alkenyl;B is NH.sub.2 or a dicarboximide group of the general formula III ##STR2## where Z is unsubstituted or substituted phenylene, naphthylene, pyridinylene, cyclopentylene, cyclohexylene, cyclohexenylene, C.sub.2 -C.sub.4 -alkenylene or C.sub.2 -C.sub.4 -alkylene. The dicarboximides are intermediates for the compounds wherein B is NH.sub.2. The latter are used in synthesizing herbicidal compounds.

Abstract: Heterocyclic liquid crystal compounds containing the structural element ##STR1## wherein M is H, CN,, NCS, halogen or an alkyl group with 1-5 C atoms,X is CR.sup.4 or N,Y is CHR.sup.4, O, S or NR.sup.5,R.sup.4 is H, alkyl with 1-15 C atoms, halogen or cyano andR.sup.5 is H or alkyl with 1-15 C atoms,with the proviso that in the case where Y=CHR.sup.4, X is N, are suitable as components of liquid crystal phases.

Abstract: Photocrosslinkable polymers having an average molecular weight of at least 1,000 and side groups of the formula Ia and/or Ib ##STR1## in which R, R', R.sub.1, R.sub.2, A, E, Y and n are as defined in claim 1, are suitable, for example, for preparing solvent-resistant coatings on metals and, in particular, for preparing printing plates or printed circuits. The group of the formula Ia and/or Ib content is at least 0.5%, preferably 5-100%, based on the number of the polymer's recurring structural elements.

Abstract: A compound of the formula: ##STR1## wherein R is an isoproyl group or an n-amyloxycarbonylmethyl group, useful as a herbicide, is effectively produced by reacting a compound of the formula: ##STR2## wherein R is as defined above, with sulfuryl chloride or chlorine in a solvent in the presence of a dehydrohalogenating agent.

Abstract: The novel N-(dichlorofluoromethylthio)-3,6-endomethylene-.DELTA..sup.4 -tetrahydrophthalimides can be prepared from 3,6-endomethylene-.DELTA..sup.4 -tetrahydrophthalimide with dichlorofluoromethanesulphenyl chloride in the presence of an acid-binding agent in solution. They can be used as microbicidal agents.

Abstract: Process for the preparation of peptides including higher polypeptides utilizing indenylmethoxycarbonyl blocking groups and products produced thereby.

Abstract: Alkyl thiosalicylate prevulcanization inhibitors having a pleasant odor are described.Claimed compounds include those of the formula: ##STR1## in which X is an amide inhibitor moiety attached through the nitrogen atom derived from the group consisting of 2-benzimidazolinone, 2-imidazolidinone, 2-benzothiazolone, 2-thiazolone, phthalimide, succinimide, glutarimide, hexahydrophthalimide, maleimide, hydantoin, urea, napthalimide, oxamide, oxanilide, phenylcarbamic acid ester, formamide, formanilide, acetamide, benzamide, acetanilide, benzanilide, propionamide, butyramide, pivalamide, valeramide and hexanamide, R is alkyl of 1-8 carbon atoms, R' is alkyl of 1-8 carbon atoms, alkoxy of 1-8 carbon atoms, --CO.sub.2 --R, or halo, and n is 0, 1 or 2.

Abstract: A process for the production of 2,2-dimethyl-3-vinyl-cyclopropanecarboxylic acid derivative of the formula ##STR1## in which R.sup.1 is a hydrogen atom, an alkyl group or a radical of an alcohol which can be used in pyrethroids, andX.sup.1 and X.sup.2 each independently is a halogen atomor a fluorine-substituted alkyl radical, comprising adding (a) a polyhalogenoalkene of the formula ##STR2## in which X.sup.3 and X.sup.4 each independently is a halogen atom, to 1-chloro-3,3-dimethyl-pent-4-en-2-one of the formula ##STR3## in the presence of a catalyst which yields free radicals, or in the presence of a metal salt of the VIII main group or of the sub-group IVa, VIIa or Ib of the periodic system, thereby to obtain a mixture of compounds of the formula ##STR4## and (b) reacting either or both of such compounds with a base of a formula(R.sup.1 --O.sup..crclbar.).sub.n M.sup.n+in whichM is an alkali metal or alkaline earth metal, andn is 1 or 2.

Abstract: Provided is a long chain carboxylic acid imide ester (I) represented by the following general formula (I) ##STR1## wherein W is a divalent long chain hydrocarbon group which may optionally be interrupted by one or more groups each independently selected from the group consisting of an oxygen, atom, a sulfur atom, and a group of --N(R.sup.1)-- (R.sup.1 being a lower alkyl group) and X represents a divalent hydrocarbon group which may optionally be substituted, or salt thereof. The above long chain carboxylic acid imide ester or its salts is useful for modifying enzymes or proteins having biological activities to give their derivatives which have, while retaining most of the original biological activities, an extremely prolonged plasma half-life as compared with the proteins and have no antigenecities and can be administered to animals.