Abstract: The present invention relates to hydroxy alkyl piperidine compounds and pharmaceutical compositions thereof which can be used to treat diabetes.

Abstract: The present invention relates to substituted piperazinone derivatives (compounds of formula (1)) or stereoisomers, or pharmaceutically acceptable salts thereof and their use as tachykinin receptor antagonists. Such antagonists are useful in the treatment of tachykinin-mediated diseases and conditions disclosed herein including: asthma, cough, and bronchitis. The present invention also relates to intermediates useful in the preparation of compounds of formula (1).

Abstract: Compounds of formula (I) or a salt thereof: ##STR1## R.sup.1 is hydrogen, halogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, COC.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, hydroxyC.sub.1-6 alkyl, hydroxyC.sub.1-6 alkoxy, C.sub.1-6 alkoxyC.sub.1-6 alkoxy, acyl, nitro, trifluoromethyl, cyano, CHO, SR.sup.9, SOR.sup.9, SO.sub.2 R.sup.9, SO.sub.2 NR.sup.10 R.sup.11, CO.sub.2 R.sup.10, NR.sup.10 SO.sub.2 R.sup.11, CONR.sup.10 R.sup.11, CO.sub.2 NR.sup.10 R.sup.11, CONR.sup.10 (CH.sub.2).sub.p CO.sub.2 R.sup.11, (CH.sub.2).sub.p NR.sup.10 R.sup.11, (CH.sub.2).sub.p CONR.sup.10 R.sup.11, (CH.sub.2).sub.p NR.sup.10 COR.sup.11, (CH.sub.2).sub.p CO.sub.2 C.sub.1-6 alkyl, CO.sub.2 (CH.sub.2).sub.p OR.sup.10, CONHNR.sup.10 R.sup.11, NR.sup.10 R.sup.11, NR.sup.10 CO.sub.2 R.sup.11, NR.sup.10 CONR.sup.10 R.sup.11, CR.sup.10 .dbd.NOR.sup.11, CNR.sup.10 .dbd.NOR.sup.11, where R.sup.10 and R.sup.11 are independently hydrogen or C.sub.1-6 alkyl and p is 1 to 4;R.sup.2 and R.sup.3 are independently hydrogen, halogen, C.sub.

Abstract: This invention has for its object to provide a method of inducing a transition in crystalline state of a crystallizable medicinal substance with great ease and improved efficiency and uniformity on a high production scale. According to the invention, an extruder is used for inducing a transition from one crystalline state (.DELTA.) to another crystalline state in a crystallizable medicinal substance.

Abstract: The present invention provides therapeutic conjugates which comprise a therapeutic compound bound to one to three acyl groups derived from fatty acids. The therapeutic compounds are preferably non.about.steroidal anti.about.inflammatory agents which include a carboxylic acid group. The compounds involve the use of tromethamine or ethanolamine derivative to link the acyl groups derived from fatty acids to the therapeutic compounds.

Abstract: The present invention relates to a new N-cinnamoyl-2-methyl-5-methoxy-3-indoleacetic ester represented by the following general formula (I). It is manufactured by causing N-cinnamoyl-2-methyl-5-metboxy-3-indoleacetic acid represented by the following general formula (II) or a reactive derivative thereof to react with a compound represented by the following general formula (III) ##STR1## wherein, R is ##STR2## The inventive compounds are effective to the same extent as the existing cinmetacin, and are also excellent in greatly reducing fatal side effects like a gastric ulcer, that are associated with cinmetacin or an intestinal ulcer.

Abstract: Dye-donor element for thermal dye transfer comprising at least one magenta dye having extremely low side absorption in the blue and red regions of the spectrum, said dye corresponding to the general formula (I) : ##STR1## wherein R.sup.1 is H, (cyclo)alkyl, or aryl; X represents the atoms completing a heterocycle; Z is an electron-withdrawing group; Y is an electron-withdrawing group or --N(R.sup.2)R.sup.3 ; R.sup.2 and R.sup.3 together represent the atoms completing a heterocycle; or R.sup.2 and R.sup.3 together represent .dbd.C(R.sup.4)R.sup.5, or each of R.sup.2 and R.sup.3 represents (same or different) (cyclo) alkyl, aryl, or an electron-withdrawing group; each of R.sup.4 and R.sup.5 (same or different) represents H, (cyclo)alkyl, aryl, a heterocycle, SO.sub.2 R.sup.6, COR.sup.6, CSR.sup.6, POR.sup.6 R.sup.7, OR.sup.8, NR.sup.8 R.sup.9, SR.sup.8, or R.sup.4 and R.sup.5 together represent the atoms completing an aliphatic ring or a heterocycle, each of R.sup.6 and R.sup.

Abstract: Compositions degrading by hydrolysis to release a bioactive compound having carboxylic acid moieties, which are organic acid anhydrides having the following formula: ##STR1## wherein R' is a residue of a therapeutic bioactive compound, for example, a non-steroidal anti-inflammatory agent; a penicillin or cephalosporin antibiotic; or bioactive compounds for non-therapeutic use, for example, herbicides, insecticides, fungicides, antimicrobials, pesticides, pheromones, and fertilizers; m is an integer of between 1 and 3; and R is a carrier. The resulting mixed anhydrides are characterized by having between one and three drug molecules attached to a single carrier molecule. The prodrugs are highly susceptibility to hydrolytic degradation in a predictable and controlled fashion, have variable solubilities in water and lipids, with increased biomembrane transport, elicit a bio-affecting/pharmacological response, and are less irritating to topical and gastric or intestinal mucosal membranes.

Abstract: The invention relates to compounds of the general formula AB, which may be a salt or an amide, wherein:A represents a cyclooxygenase inhibitor having an accessible acidic function andB represents the L-form of arginine analogues of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 represent various substituents, process for the preparation of such compounds and pharmaceutical composition thereof.

Abstract: The present invention provides a process for the preparation of a complex of indomethacin and a divalent metal comprising forming a solution by dissolving indomethacin and a salt of said divalent metal in a tertiary amide or cyclic tertiary amide, adding a C.sub.1-4 alkanol or C.sub.3-6 ketone to the solution to precipitate the complex, and separating the precipitated complex from the solution. The present invention also provides a method for the treatment of inflammation or pain in a mammal requiring such treatment, comprising administering to said mammal an anti-inflammatory or analgesically effective amount of a complex of indomethacin and a divalent metal, the complex having the formula [M].sub.2 [indomethacin].sub.4 [S].sub.n, wherein M is the divalent metal, S is a molecule of a tertiary amide or a cyclic tertiary amide, and n is 2 or 3, or of a pharmaceutical composition comprising said complex together with a pharmaceutically acceptable carrier, diluent and/or excipient.

Abstract: Compounds of the structures shown below are specific inhibitors of cyclooxygenase-2 useful in the treatment of cyclooxygenase-2 mediated disease states such as inflammation, pain and fever, and are non-ulcerogenic.

Abstract: The present invention provides a condensed heterocyclic derivative represented by a formula: ##STR1## wherein R.sup.1 represents a lower alkyl group, an alkenyl group, or the like, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 independently represent a hydrogen atom, a lower alkyl, or the like, W is represented by --OC(O)--, --SC(O)--, or the like, and Z represents a 2-indolyl group or the like. The present invention also provides an agricultural or horticultural fungicide which comprises an amount of the condensed derivative known to be effective as a fungicide. The agricultural or horticultural fungicide according to the present invention exhibits a superior control effect for downy mildew and late blight, without harm to nonfungal, photosynthesizing plants.

Abstract: The present invention provides a method for the treatment of inflammation and pain in a mammal requiring such treatment, comprising administering to said mammal an anti-inflammatory and analgesically effective amount of an indomethacin salt of a divalent metal capable of forming a stable complex with indomethacin, or of a pharmaceutical composition comprising said indomethacin salt together with a pharmaceutically acceptable carrier, diluent and/or excipient. The present invention also provides a process for the preparation of an indomethacin salt of a divalent metal capable of forming a stable complex with indomethacin comprising forming a solution by dissolving indomethacin and a salt of said divalent metal in a tertiary amide or cyclic tertiary amide, adding a C.sub.1-4 alkanol or C.sub.3-6 ketone to the solution to precipitate the indomethacin metal salt and separating the indomethacin metal salt precipitate from the solution.

Abstract: Indole derivatives of the following formula: ##STR1## wherein R.sup.1 is carboxy(lower)alkyl or protected carboxy(lower)alkyl,R.sup.2 is hydrogen, lower alkyl or halogen,R.sup.3 and R.sup.4 are each hydrogen or lower alkyl,R.sup.5 is ar(lower)alkyl which may have suitable substituent(s), andA is carbonyl, sulfonyl or lower alkylene, or a pharmaceutically acceptable salt thereof, which are useful as a testosterone 5.alpha.-reductase inhibitor.

Abstract: The present invention relates to an indoleacetic acid derivative and a salt thereof expressed by the following formula (I): ##STR1## [wherein X denotes a piperidino group, 1-pyrrolidinyl group or 3-hydroxy-1-pyrrolidinyl group; Y denotes ##STR2## (wherein R.sup.1 denotes a hydrogen atom or a lower alkyl group, and 1 denotes 0, 1 2) or ##STR3## (wherein R.sup.2 denotes a hydrogen atom, a lower alkyl group or a hydroxyl group, m denotes 0, 1 or 2, and n denotes 1, 2 or 3)]. The present invention also relates to anti-inflammatory drugs, anti-rheumatic drugs and anti-ulcer drugs containing the above compounds as active ingredients. The compounds possess a strong antiinflammatory action while causing extremely reduced troubles of digestive organs which is a serious defect with conventional non-steroidal anti-inflammatory drugs, and possess an excellent anti-ulcer action as well.

Abstract: Novel ester derivatives of carboxylic acid medicaments of formula (I), wherein R--COO--represents the acyloxy residue of a carboxylic acid drug or medicament, n is an integrer from 1 to 3, and R.sub.1 and R.sub.2 are the same or different and are selected from a group consisting of an alkyl, an alkenyl, an aryl, an aralkyl, a cycloalkyl and which group may be unsubstituted or substituted, or R.sub.1 and R.sub.2 together with the N forms a 4-, 5-, 6- or 7-membered heterocyclic ring, which in addition to the nitrogen atom may contain one or two further heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur and which heterocyclic group may be substituted. These compounds are highly biolabile prodrug forms of the corresponding carboxylic acid compounds and are highly susceptible to undergoing enzymatic hydrolysis in vivo whereas they are highly stable in aqueous solution.

Abstract: A method for increasing the water-solubility of highly insoluble organic compounds by forming a novel complex product from the reaction between the organic compound and an oligomer of vinylpyrrolidone. The complex is highly stable and results in solubilities of the organic compounds in excess of 25-fold.

Abstract: This invention provides a series of novel heterocyclic amides of formula I in which the group >X-Y-Z< is selected from >C.dbd.CH--N<, >C.dbd.N--N<, >N--(CH.sub.2)--N<, >CH--CH.sub.2 --N< and >N--N.dbd.C< and the other radicals have the meanings defined in the following specification.The compounds of formula I are leukotriene antagonists. The invention also provides pharmaceutically acceptable salts of the formula I compounds: pharmaceutical compositions containing the formula I compounds, or their salts, for use in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.

Abstract: 1-(fluoro- or perfluoro lower alkyl-substituted benzoyl)-5-methoxy-2-methyl-1H-indole-3-acetic acid carboxymethyl ester is found to have antiinflammatory and analgestic activity with less side effects on gastrointestinal traces than its homologue, acematacin or indometacin.

Abstract: Novel esters of the general formula ##STR1## in which ##STR2## is the acyl residue of a non-steroidal anti-inflammatory compound containing a carboxylic acid function. The novel esters are prepared by reacting an acide R--COOH when R is as above, with 1-haloethyl ethyl carbonate. There are also provided pharmaceutical compositions containing any of the said novel esters.

Abstract: The compound characterized by the structural Formula I: ##STR1## is therapeutically useful as an anti-hypertensive agent. A process for the preparation of the compound having Formula I and their synthetic intermediates is described. One of the synthetic intermediates is the compound characterized by the structural Formula: ##STR2## which is also therapeutically useful as an anti-hypertensive agent.

Abstract: Amide derivatives of non-steroidal anti-inflammatory carboxylic acids which have anti-inflammatory activity in their own right as well as being effective as pro-drugs of the carboxylic acids.

Abstract: The new indole derivatives of the formula ##STR1## in which R.sup.1 and R.sup.2 are identical or different and denote hydrogen or lower alkyl,R.sup.3 denotes hydrogen, lower alkyl or halogen andR.sup.4 and R.sup.5 are identical or different and denote hydrogen, lower alkyl or optionally substituted aryl, and R.sup.4 and R.sup.5 can also represent lower alkenyl, andwhereinR.sup.2 and R.sup.5 can be linked by an alkylene bridge of the formula--CH.sub.2 --CH.sub.2 --CH.sub.2).sub.nin whichn represents the number 0 or 1, can be prepared by reacting an ammonium or phosphonium salt of the corresponding indolecarboxylic acid with a haloacetic acid allyl ester. The new compounds can be used to prepare acemetacin. The new indole derivatives possess a pharmacological action.

Abstract: 1-(4-Chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetic acid carboxymethyl ester as known per se is obtainable by a novel and more simple method comprising mild acid hydrolysis of 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetoxyacetic tetrahydropyran-2-yl ester. The final product is a valuable drug having antiinflammatory activity.

Abstract: A novel anti-inflammatory drug, which exhibits rapidly a pharmacological activity, maintains the activity for a long time, and is free from a side effect such as a gastrointestinal disorder or a central nervous disturbance is disclosed.The drug comprises a compound of an alkylcarbonyloxyalkylester or alkenylcarbonyloxyalkylester derivative of indolylacetic acid or anilinophenylacetic acid.The compound is prepared by an esterification reaction.

Abstract: New acyl derivatives of p-aminophenol and esters of same useful as pharmacologically active ingredients and process for their preparation.

Abstract: Convenient intermediates for preparing 3-substituted-2-hydroxypropyl aryl ether .beta.-blockers, a reaction to the intermediates of the following formula and a conversion to obtain the said .beta.-blockers are disclosed. ##STR1## (wherein X is hydrogen or halogen;Y is halogen, hydroxy, lower acyloxy, amino, lower alkylamino, lower aralkylamino, lower acylamino, di-lower alkylamino, lower alkyleneamino, N-lower alkyl-N-lower aralkylamino, di-lower acylamino, N-lower alkyl-N-lower acylamino or N-tri-lower alkylsilylamino;one of P and R combined together with Q represents lower alkylene or alkenylene optionally interrupted by O, N or S and optionally substituted by lower alkyl, lower aralkyl, lower carboxylic acyl, carboxy, protected carboxy; hydroxy, lower alkoxy, lower acyloxy, oxo; amino, lower alkylamino, lower acylamino, nitro, nitroso, lower alkylthio, lower sulfonic acyl or halogen;and the remaining R or P is hydrogen or halogen;and dotted line represents the presence of one or two double bonds).

Abstract: 1-(4-Chlorobenzoyl)-5-methoxy-2-methyl-3-indole acetic acid as known per se is obtainable by means of a novel and more simple method. This method comprises hydrolizing 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-3-indole acetic acid tetrahydropyranyl ester, which ester is a novel compound. The final product obtained is a valuable drug having antiinflammatory activity.

Abstract: A process for the production of an ergot alkaloid comprising intramolecularly cyclizing a 3-iminoethyl-4-trans-buta-1',3'-dienylindole to produce an 8-ergolene and as necessary converting the resultant ergolene into the desired ergot alkaloid.

Abstract: The (5-R-2-oxo-1,3-dioxolen-4-yl)methyl moiety: ##STR1## wherein R is loweralkyl of 1-6 carbon atoms, especially methyl or t-butyl; when utilized as an ester on a pharmaceutical having a carboxylic acid functionality, enhances oral absorption of the pharmaceutical. This effect is applicable to a broad range of pharmaceutically active substances, including antibiotics, and antihypertensives as well as other classes of therapeutic agents.

Abstract: The invention relates to a process for the preparation of the known 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-3-indoleacetoxyacetic acid which comprises reacting an indolecarboxylic acid ester of Formula (II) or its derivative with an alcohol of Formula (III). The final product is known to have antiinflammatory activity.

Abstract: Non-steroidal, anti-inflammatory drugs are disclosed which are polyprenyl alcohol esters of indolyl lower carboxylic acids, phenyl lower carboxylic acids, acetyl salicylic acid, anthranilic acid and derivatives thereof.

Abstract: This invention relates to compounds and methods of using said compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, alkyl, alkenyl or alkoxycarbonylalkyl; Y is O or S; m is an integer of 1 to 3 and n is an integer of 0 to 1 which compounds are insect repellents.

Abstract: Novel prodrug forms of known non-steroidal anti-inflammatory agents are disclosed, said prodrugs having the structural formula ##STR1##

Abstract: Compounds of the formula:R'--CH.sub.2 --S--Awherein:R' is hydrogen, alkyl, --COOH or its pharmaceutically acceptable salts, --alkylene--COOH or its pharmaceutically acceptable salts, --alkylene-SO.sub.2 H or its pharmaceutically acceptable salts, --alkylene-SO.sub.3 H or its pharmaceutically acceptable salts, or --alkylene CH.sub.2 OH; andA is the acyl moiety of a pharmaceutically acceptable carboxylic acid, said acid having antiinflammatory properties;are gastrointestinal tract sparing drugs for antiinflammatory pharmaceuticals.