Abstract: The invention provides a pharmaceutical composition comprising a particular physical form of N-[4-[5-(cyclopentyloxycarbonyl)amino-1-methylindol-3-yl-methyl]-3-methoxy benzoyl]-2-methylbenzenesulphonamide and polyvinylpyrrolidone. It also provides methods for preparing this physical form, and another physical form of N-[4-[5-(cyclopentyloxycarbonyl)amino-1-methylindol-3-yl-methyl]-3-methoxy benzoyl]-2-methylbenzenesulphonamide useful in the preparation of the first mentioned physical form. The compositions are useful in the treatment of diseases in which leukotrienes are implicated, for example asthma.

Abstract: There are described novel (N-phthalimidoalkyl) piperidine compounds which exhibit selective sigma-receptor antagonism and therefore are useful in the treatment of physiological or drug induced psychosis and dyskinesia in a mammal. Also described are pharmaceutical compositions containing sigma selective compounds and methods of using these compositions for treating physiological or drug induced psychosis or dyskinesia in a mammal. Further provided are methods for preparing the compounds of this invention.

Abstract: There are disclosed compounds ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently of one another hydrogen, a C.sub.1 -C.sub.12 alkyl group, a C.sub.1 -C.sub.12 alkoxy group, a C.sub.5 -C.sub.8 cycloalkyl group, a C.sub.5 -C.sub.8 cycloalkoxy group, a C.sub.5 -C.sub.8 cycloalkylthio group, a C.sub.6 -C.sub.10 aryl group, a C.sub.6 -C.sub.10 aryloxy group, a C.sub.6 -C.sub.10 arylthio group, nitro, halogen, cyano, --COOH, --COOR.sub.7, --NR.sub.8 R.sub.9 or --CONR.sub.8 R.sub.9, where R.sub.7 is C.sub.1 -C.sub.20 alkyl, C.sub.5 -C.sub.8 acycloalkyl, phenyl or phenyl-C.sub.1 -C.sub.4 alkyl, and R.sub.8 and R.sub.9 are each independently of the other hydrogen, C.sub.1 -C.sub.8 alkyl, phenyl or phenyl-C.sub.1 -C.sub.4 alkyl, X is nitrogen or CR.sub.4, Y is nitrogen or CR.sub.5 and Z is nitrogen or CR.sub.6, and R.sub.4, R.sub.5 and R.sub.6 are each independently of one another hydrogen, a straight-chain or branched C.sub.1 -C.sub.12 alkyl group or a C.sub.6 -C.sub.

Abstract: The invention concerns ether derivatives of the formula IQ.sup.1 --X--Ar--Q.sup.2 IwhereinQ.sup.1 is an optionally substituted 9-, 10- or 11-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;X is oxy, thio, sulphinyl or sulphonyl;Ar is optionally substituted phenylene, pyridinediyl, pyrimidinediyl, thiophenediyl, furandiyl, thiazolediyl, oxazoiediyl, thiadiazoiediyl or oxadiazolediyl; andQ.sup.2 is selected from the groups of the formulae II and III: ##STR1## wherein R.sup.1 is hydrogen, (2-5C)alkanoyl or optionally substituted benzoyl;R.sup.2 is (1-4C)alkyl; andR.sup.3 is hydrogen or (1-4C)alkyl;or R.sup.2 and R.sup.3 are linked to form a methylene, vinylene, ethylene or trimethylene group;or a pharmaceutically-acceptable salt thereof;processes for their preparation; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.

Abstract: The invention relates to cyclic urea derivatives of general formula ##STR1## wherein R.sub.a, R.sub.b, X and Y are as defined herein, pharmaceutical compositions containing the derivatives and processes for preparing them.

Abstract: The present patent application discloses compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.21 and R.sup.22 each independently are alkyl; andR.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.11, R.sup.12, R.sup.13, and R.sup.14 each independently are hydrogen, halogen, CF.sub.3, CN, or NO.sub.2.The compounds are useful as in vivo active glutamate antagonists.

Abstract: Method of synthesizing a 1,3,3 trinitroazetidine compound (TNAZ) comprising the steps of:selecting a compound of the formula I: ##STR1## wherein R' is one of hydrogen and an organic group and R is selected from the group consisting of electron withdrawing and electron donating groups; and,reacting the selected compound with a nitrolyzing agent such that a TNAZ compound is formed from the reaction.

Abstract: The present invention provides compounds having the structure: ##STR1## or having the structure: ##STR2## The present invention also provides a pharmaceutical compostion containing the compounds, methods of synthesizing the compounds, as well as methods of inhibiting growth of tumor cells and of treating a subject having a disease characterized by the proliferation of tumor cells.

Abstract: The present invention includes N-substituted maleimides (1(H)-Pyrrole-2,5-dione (Maleimide) analogs and succinimides which act as potent nonsteroidal anti-inflammatory drugs and are capable of dual inactivation or selective inactivation of the cyclooxygenase and the peroxidase activities of prostaglandin endoperoxide synthase (PGHS).

Abstract: The invention relates to indoles of general formula (I) ##STR1## wherein R.sub.0 represents a hydrogen atom or a C.sub.1-3 alkyl group; R.sub.1 represents a group R.sub.4 CONH--, R.sub.4 R.sub.5 NSO.sub.2 --, R.sub.4 SO.sub.2 NH-- or R.sub.4 R.sub.5 NCO-- (where R.sub.4 is a hydrogen atom or a C.sub.1-6 alkyl group, provided that R.sub.4 does not represent a hydrogen atom when R.sub.1 represents R.sub.4 SO.sub.2 NH--, and R.sub.5 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, phenyl or phen(C.sub.1-3)alkyl group in which the phenyl ring is optionally substituted by a halogen atom or a C.sub.1-4 alkoxy, hydroxy or C.sub.1-3 alkyl group); R.sub.2 is a hydrogen atom, a C.sub.1-3 alkyl, a C.sub.3-6 alkenyl, a phenyl or a phen(C.sub.1-3)alkyl group; R.sub.3 is a hydrogen atom, a C.sub.1-3 alkyl group or a group --CO.sub.2 R.sub.6, --COR.sub.6, --COCO.sub.2 R.sub.6 or --CONHR.sub. 6 where R.sub.6 is a hydrogen atom or a C.sub.1-4 alkyl, a C.sub.3-7 cycloalkyl, a C.sub.

Abstract: Disclosed herein are compounds referred to as "fused pyrrolocarbazoles" which possess a variety of functional activities. The disclosed compounds are represented by the following general formula: ##STR1## Methodologies for the synthetic production of fused pyrrolocarbazoles are also disclosed, as well as exemplary uses of the compounds.

Abstract: An L-proline derivative represented by: ##STR1## wherein R.sub.2 represents a lower alkyl group is prepared by reacting L-proline with a D-.alpha.-alkyl-.beta.-acylthiopropionic acid halide, ##STR2## wherein R.sub.1 represents an acyl group, X represents a halogen atom and R.sub.2 has the same meaning as defined above. The halide is added to an aqueous medium containing L-proline and a condensation agent for deacidification. The halide and L-proline are reacted while the reaction temperature and pH are maintained at 12.degree. C. or lower and within a range of 10.5-11.5, whereby a compound represented by: ##STR3## wherein R.sub.1 and R.sub.2 have the same meanings as defined above is obtained. The resulting compound is then subjected to deacylation under strong alkaline conditions without being isolated from the reaction mixture, thereby yielding the target L-proline derivative.

Abstract: A tetrahydroprotoberberine quaternary ammonium compound represented by the formula: ##STR1## wherein R.sub.1, R.sub.2, R' and X are as defined in the specification. A method of preparing the compound is provided. The compounds can suppress arrhythmia and ventricular fibrillation, protect against myocardial ischemia, and can be conveniently orally administered.

Abstract: Monomeric bisimides corresponding to the formula: ##STR1## wherein R is independently in each occurrence hydrogen, alkyl of from 1 to 20 carbons, aralkyl of from 1 to 20 carbons, halogen, or NO.sub.2 ; X' is F, Cl, OH, or NO.sub.2. These bisimides are useful in the production of various thermoplastic, polymeric materials such as polyetherimides, polyesterimides, and poly(carbonate imides).

Abstract: Process for the preparation of purified phthalimidoalkanecarboxylic acidsThe present invention relates to a process for the preparation of purified phthalimidoalkanecarboxylic acids which are contaminated with phthalic acid, lactam and/or water, including the following measures:a) fusing the contaminated phthalimidoalkanecarboxylic acid,b) holding the melt for a period and at a temperature sufficient for the impurities to have substantially departed from the melt andc) cooling the purified product melt.

Abstract: Disclosed are (R)- and (S)-isomers of the compounds of the Formulas II and III with at least 95% optical purity ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and represent a hydrogen atom, a lower alkyl, lower alkenyl or lower alkynyl group, a cycloalkyl group or a group (CH.sub.2).sub.m Ph, wherein m is 0-3 and Ph is a substituted or unsubstituted phenyl group.These compounds are intermediates in the stereoconservative synthesis of 1-substituted (S)- and (R)-2-aminomethylpyrrolidines.

Abstract: Functional K-252a derivatives are used to enhance trk phosphorylation and to potentiate the activity of neurotrophin-3 (NT-3). These compounds can be used to treat neurological disorders, alone or in combination with NT-3.

Abstract: This invention provides a process for optimizing the yield of a 1-(2,4-dichlorophenyl)-4,5-dihydro-1H-1,2,4-triazol-5-one by the chlorination in two steps of a 4,5-dihydro-1-phenyl-1H-1,2,4-triazol-5-one. The critical first step is the selective chlorination of the phenyl ring in the 4-position by addition of chlorine to a solution of the 4,5-dihydro-1-phenyl-1H-1,2,4-triazol-5-one in N,N-dimethylformamide. Chlorination of the product of the first step in acetic acid/water yields the 1-(2,4-dichlorophenyl)-4,5-dihydro-1H-1,2,4-triazol-5-one in high yield.

Abstract: Various 4,5-dimercapto-1,3-dithiolo-2-one or thione maleimides corresponding to the formula ##STR1## wherein R represents --H, phenyl, benzyl, phenethyl, a C.sub.1 -C.sub.10 straight or branched chain alkyl radical, a C.sub.3 -C.sub.10 cycloalkyl radical, a C.sub.1 -C.sub.10 straight or branched chain alkoxy radical, a C.sub.3 -C.sub.10 cycloalkoxy, an ester of the formula --CH.sub.2 CH.sub.2 O--C(O)--R.sup.1, wherein R.sup.1 represents a C.sub.1 -C.sub.5 straight or branched chain alkyl radical or a C.sub.3 -C.sub.5 cycloalkyl radical and Z represents oxygen or sulfur are disclosed.These compounds have been found to exhibit antimicrobial and marine antifouling activity in industrial and commercial applications and compositions containing these compounds are so employed.

Abstract: Peroxycarboxylic acids of formula (I) are disclosed wherein the substituents are defined by the disclosure. The peroxycarboxylic acids are useful for washing, bleaching and disinfecting, and methods for using them in such processes are also disclosed. Further, a process for preparing the peroxycarboxylic acids is disclosed.