Abstract: The compounds of the formula wherein R signifies halogen or lower alkyl; n signifies 0-3; R1 signifies lower alkyl; cycloalkyl; benzyl optionally substituted by hydroxy, halogen, lower alkoxy or lower alkyl; benzoyl optionally substituted by amino, lower alkylamino or di-lower alkylamino; acetyl or cycloalkyl-carbonyl; and signifies an aromatic 5-membered residue which is bonded via a N-atom and which contains further 1-3 N atoms in addition to the linking N atom, as well as their pharmaceutically acceptable salts as therapeutically active substances, especially for the control or prevention of acute and/or chronic neurological disorders.

Abstract: This invention relates to new processes for manufacturing 4-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]-N-methyl-3H-[1,2,3]triazole-5-carboxamide (compound I) as well as the following new intermediates useful in these synthetic processes. 2-benzenesulfonyl-N-methylacetamide (compound IV), 2-(benzenesulfonyl)-3-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]-N-methylacrylamide (compound II) and threo-2-[2-benzenesulfonyl-1-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-[(methylcarbamoyl)ethyl]]-5-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]-N-methyl-2H-[1,2,3]triazole-4-carboxamide (compound III).

Abstract: Compounds of the formula wherein R1 and R1′ are independently alkyl, aryl, alkenyl or alkynyl; R2 and R2′ are independently hydrogen, alkyl, aralkyl, alkoxyalkyl, hydroxyalkyl, haloalkyl, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, acylaminoalkyl, alkylsulphonylaminoalkyl, arylsulphonyl-aminoalkyl, mercaptoalkyl, alkylthioalkyl, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, alkylthio or alkylsulphinyl; R4, R5, R6, R7, R4′, R5′, R6′, and R7′ each independently are hydrogen, CO2R9, CH2OR10, CHO, CH2NR11R12, CON(R13)2, halogen, cyano, aryl, alkyl, hydroxy, alkoxy, aryloxy, haloalkyl, nitro, amino, aralkyloxy, acylamino, monoalkylamino, dialkylamino, thio, alkyl, alkylsulphinyl, alkylsulphonyl, arylsulphinyl, azide, phosphate or phosphonate provided that at least one of R4, R5, R6 and R7 and at least one of R4′, R5′, R6′, and R7′ are other than hydrogen, with the proviso that when R6 is methoxy, R5

Abstract: The present invention relates to novel p75 heterodimer specific anti-human IL-12 antibodies that are characterized by a higher potency and greater efficacy in neutralizing human IL-12 bioactivity than known heterodimer specific IL-12 monoclonal antibodies. The heterodimer specific antibodies recognize one or more epitopes of the human IL-12 p75 heterodimer, but do not bind to the p40 subunit alone. The heterodimer specific IL-12 antibodies neutralize rhesus monkey IL-12 bioactivity with a potency similar to their potency for neutralizing human IL-12 bioactivity making them useful IL-12 antagonists for in vivo studies in the rhesus monkey.

Abstract: Novel 5′-deoxy-cytidine derivatives represented by the general formula (I) wherein R1 is a hydrogen atom or a group easily hydrolyzable under physiological conditions; R2 is a hydrogen atom, or —CO—OR4 group [wherein R4 is a saturated or unsaturated, straight or branched hydrocarbon group consisting of one to fifteen carbon atoms, or a group of the formula —(CH2)n—Y (in which Y is cyclohexyl or phenyl; n is an integer from 0 to 4)]; R3 is a hydrogen atom, bromo, iodo, cyano, a C1-4 alkyl group [which may be substituted with halogen atom(s)], a vinyl or ethynyl group [which may be substituted with halogen atom(s), C1-4 alkyl, cycloalkyl, aralkyl, or aromatic ring which may have one or more hetero atom(s)], or an aralkyl group which may be substituted for use in medical therapy, especially tumor therapy.

Abstract: Compounds of the formula wherein R,R′, A,B,T and x have the meaning given in the specification possess uPA (urokinase-type plasminogen activator) antagonist activity and can be employed as antitumor and/or antimetastatic agents.

Abstract: The invention relates to a process for simultaneously N(2)-acylating piperazic acid or an ester thereof and forming a bicyclic ring structure. The invention also relates to the use of that process step in a method of synthesizing a bicyclic compound useful as an intermediate for the production of an inhibitor of a caspase, particularly an inhibitor of interleukin-1&bgr; converting enzyme (“ICE”).

Abstract: The present invention is concerned with a process for the manufacture of chiral succinic acid derivatives of formula (I) wherein R1 is (C1-C6) alkyl or benzyl, and the novel intermediates used therein.

Abstract: The invention relates to a process for synthesizing piperazic acid and similar, ring-containing acids. The invention also relates to a process for simultaneously N(2)-acylating piperazic acid or an ester thereof and forming a bicyclic ring structure. The invention also relates to the use of either or both processes in a method of synthesizing a bicyclic compound useful as an intermediate for the production of an inhibitor of a caspase, particularly an inhibitor of interleukin-1&bgr; converting enzyme (“ICE”).

Abstract: The invention is concerned with hydroxymethyl-imidazodiazepines and their esters of general formula I. These compounds can be used as anxiolytic and/or anticonvulsant and/or muscle relaxant and/or sedative-hypnotic active substances.

Abstract: The present invention relates to compounds of the formula ##STR1## wherein X is --O-- or --CH.sub.2 --;Y is --C(O)--, --(CH.sub.2).sub.n -- or --N(CH.sub.3)--;n is 1 or 2 orX and Y taken together are --CH.dbd.CH--Z is --NH--, --CH.sub.2 --, --O-- or .dbd.CH--;A.sup.1 is a group ##STR2## B is --(CH.sub.2).sub.m --; m is 0, 1 or 2;R.sup.1 and R.sup.2 are each independently hydrogen or lower alkyl;R.sup.3 is hydrogen or halogen;R.sup.4 is hydrogen or hydroxy andthe dotted line is (--CH.sub.2 --CH.sub.2 --).sub.n, and n' is 0 or 1 and to pharmaceutically acceptable acid addition salts thereof.The compounds of the present invention are antagonists of the OFQ receptor.

Abstract: Described herein is a toothpaste composition which comprises an orally acceptable vehicle, a polishing agent, a surface active agent and a binder, the binder containing kappa carrageenan and a cellulose gum, the percent by weight concentration of binder being in the range of about 0.30 to 0.80%, and the ratio of kappa carrageenan to cellulose gum being in the range of about 25:75 to 75:25. A preferred concentration of binder is in the range of about 0.45 to 0.65 and a preferred ratio of kappa carrageenan to cellulose gum is in the range of about 55:45 to 75:25. The toothpaste is surprisingly non-stringy, exhibits good consistency, transparency and physical stability.

Abstract: Compounds of formula (I) ##STR1## as defined by the specification. The compounds are useful in the treatment or prevention of vitamin D dependent disorders, particularly psoriasis, basal cell carcinomas, disorders of keratinization and keratosis, leukemia, osteoporosis, hyperparathyroidism accompanying renal failure, transplant rejection and graft vs. host disease.

Abstract: The invention provides novel azulene derivatives of general formula I ##STR1## wherein R.sub.1 to R.sub.6 have the significance given in the description, as well as their tautomers, enantiomers, diastereomers, racemates and physiologically compatible salts or esters and substances which are hydrolyzed or metabolized in vivo to compounds of formula I.The invention is also concerned with a process and intermediates for the manufacture of the above compounds, pharmaceutical compositions which contain such compounds as well as the use of these compounds in the treatment of inflammatory conditions.

Abstract: Novel 5'-deoxy-cytidine derivatives represented by the general formula (I) ##STR1## wherein R.sup.1 is a hydrogen atom or a group easily hydrolyzable under physiological conditions; R.sup.2 is a hydrogen atom, or --CO--OR.sup.4 group [wherein R.sup.4 is a saturated or unsaturated, straight or branched hydrocarbon group consisting of one to fifteen carbon atoms, or a group of the formula --(CH.sub.2).sub.n --Y (in which Y is cyclohexyl or phenyl; n is an integer from 0 to 4)]; R.sup.3 is a hydrogen atom, bromo, iodo, cyano, a C.sub.1-4 alkyl group [which may be substituted with halogen atom(s)], a vinyl or ethynyl group [which may be substituted with halogen atom(s), C.sub.1-4 alkyl, cycloalkyl, aralkyl, or aromatic ring which may have one or more hetero atom(s)], or an aralkyl group which may be substituted for use in medical therapy, especially tumor therapy.

Abstract: The present invention relates to the use of tetrahydroisoquinoline derivatives of the general formula: ##STR1## wherein: A is arylR.sup.1 is hydrogen, hydroxy, lower alkyl, lower alkoxy, R--CO-- or R--COO--, wherein R is lower alkyl;R.sup.2 is hydrogen, lower alkyl or cycloalkylR.sup.3 -R.sup.7 are independently hydrogen, lower alkyl, lower alkoxy, hydroxy orR.sup.3 and R.sup.4 taken together are --(CH.sub.2).sub.n -- orR.sup.6 and R.sup.7 taken together are --OCH.sub.2 O-- andn is 3 or 4,as well as pharmaceutically acceptable salts for the manufacture of medicaments for the control or treatment of diseases which represent therapeutic indications for NMDA receptor subtype specific blockers.

Abstract: The compounds of the formula ##STR1## wherein R signifies halogen or lower alkyl;n signifies 0-3;R.sup.1 signifies lower alkyl; cycloalkyl; benzyl optionally substituted by hydroxy, halogen, lower alkoxy or lower alkyl; benzoyl optionally substituted by amino, lower alkyl-amino or di-lower alkylamino; acetyl or cycloalkyl-carbonyl; and ##STR2## signifies an aromatic 5-membered residue which is bonded via a N-atom and which contains further 1-3 N atoms in addition to the linking N atom,as well as their pharmaceutically acceptable salts as therapeutically active substances, especially for the control or prevention of acute and/or chronic neurological disorders.

Abstract: The present invention relates to vitamin D derivatives of the formula I ##STR1## wherein X is C.dbd.CH.sub.2 or CH.sub.2 ;Y is hydrogen, fluorine or hydroxyZ is hydroxyn is 1 or 2R.sup.1 is lower alkyl,R.sup.2 is a branched alkyl having 3 to 8 carbon atoms which is unsubstituted or substituted with one or more halogen or OH substituents, or is a phenyl group which is unsubstituted or substituted with a branched alkyl having 3 to 8 carbon atoms which is unsubstituted or substituted with one or more halogen or OH substituents;and the dotted carbon-carbon bond in ring D is --C--C-- or --C.dbd.C--; or a pharmaceutically usable salt thereof.

Abstract: Novel herbicidal compounds, compositions containing them, and methods for their preparation and use in controlling weeds are disclosed. The novel herbicidal compounds are 3-(pyrazolylphenyl)propanoic acids and derivatives having the formula: wherein X is H or halogen; Y is halogen, trihaloalkyl or cyano; Z and R are halogen; R1 is carboxyl or agriculturally acceptable salt thereof, cyano, alkoxycarbonyl, alkylthiocarbonyl, alkoxyalkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, or alkylsulfonylaminocarbonyl; and R2 is hydrogen or lower alkyl.

Abstract: It has now been found that certain novel (oxaalkyl)phenyl-substituted heterocycles are useful as pre-emergent and post-emergent herbicides. These compounds are represented by formula I: ##STR1## where Q is a heterocycle and X, Y, R, R.sup.1, R.sup.2, and R.sup.3 are substituents as described in the specification. Preferred are those compounds where Y and R are chloro; R.sup.1 and R.sup.2 are hydrogen or methyl; R.sup.3 is hydrogen or alkylaminocarbonyl; X is fluorine; and Q is a 1-substituted-6-trifluoromethyl-2,4(1H,3H)-pyrimidinedion-3-yl.