Abstract: Compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are pharmaceutical compositions comprising the compounds, and methods of using the compounds in the treatment of cancer.

Abstract: The present invention provides novel compounds of Chemical Formula I, a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, a preparation thereof and a composition for the alleviation, prevention or treatment of osteoporosis, comprising thereof in an effective amount, and a method for alleviating, preventing or treating osteoporosis.

Abstract: Compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are pharmaceutical compositions comprising the compounds, and methods of using the compounds in the treatment of cancer.

Abstract: A compound having Formula I wherein one of R1 and R2 is a group of the formula wherein R4 is selected from H and hydrocarbyl, R5 is a hydrocarbyl group and L is an optional linker group, or R1 and R2 together form a ring substituted with the group wherein R3 is H or a substituent, and wherein X is selected from S, O, NR6 and C(R7)(R8), wherein R6 is selected from H and hydrocarbyl groups, wherein each of R7 and R8 are independently selected from H and hydrocarbyl groups.

Abstract: The present invention relates to substituted pyrazoline compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.

Abstract: Modulators of PPAR? activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.

Abstract: Compounds of formula 1 modulate the activity of Rho C: wherein n is 2 to 5, inclusive; R1, R2, R3, R4, R5, R6, R7, R8, and R9 are each independently H, halo, lower alkyl, lower alkoxy, lower alkylamino, trifluoromethyl, nitro, lower alkylthio, or two adjacent residues form cycloalkyl, cycloalkenyl, aryl, or lower alkylenedioxy; and pharmaceutically acceptable salts thereof.

Abstract: A new nitro compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each lower alkyl or lower alkoxy(lower)-alkyl, or ##STR2## is cyclized to form ##STR3## X is --O--, --S-- or --NH--, m is an integer 0 or 1, andR.sup.3 is carbamoyl, lower alkylcarbamoyl, lower alkanoyl, di-lower alkylaminosulfonyl, lower alkylsulfonyl, oxamoyl or a group of the formula: --(Y).sub.n --R.sup.4 wherein Y is --CO--, --SO.sub.2 --, --COCH.sub.2 -- or ##STR4## n is an integer of 0 or 1, and R.sup.4 is heterocyclic group which is optionally substituted with one or more substituents selected from lower alkyl, lower alkoxy, phenyl, carbamoyl, halogen, amino, lower alkylthio, hydroxy, lower alkylsulfonylamino and carbamoylmethyl, and pharmaceutically acceptable salt thereof, which are useful as vasodilators.

Abstract: A process of synthesizing N-acyl auxiliary compounds is disclosed. A compound of the formula: ##STR1## is reacted with an anhydride in the presence of a lithium salt and an amine base to produce the N-acylated auxiliary.

Abstract: Compounds of general formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, n, X and A are defined in the description. Medicinal products containing the same are useful as antidepressives or anxiolytics due to their 5-HT1A receptor agonist activity.

Abstract: Combating fungi with nitro-substituted benzothiazolones of the formula ##STR1## in which R.sup.1 represents hydrogen, alkyl, alkenyl or alkynyl, cycloalkyl-alkyl, furylalkyl, alkylcarbonyl which is optionally substituted by halogen or alkoxy, benzoyl which is optionally substituted by halogen, nitro, alkyl, halogenoalkyl and/or alkoxy, alkoxycarbonyl, phenoxycarbonyl, alkylaminocarbonyl which is optionally substituted by halogen or alkoxy, dialkylaminocarbonyl, benzyloxycarbonyl, benzylaminocarbonyl which is optionally substituted by halogen, alkyl, halogenoalkyl and/or alkoxy, or phenethylaminocarbonyl which is optionally substituted by halogen, alkyl, halogenoalkyl and/or alkoxy, andR.sup.2 represents hydrogen, halogen, alkyl or halogenoalkyl.Some of the compounds and intermediates therefor are new.

Abstract: Fungicidal nitro-substituted benzothiazolones of the formula ##STR1## in which R represents alkyl which is monosubstituted or disubstituted by identical or different substituents from the group consisting of cyano, carboxyl, alkylcarbonyl, alkoxycarbonyl, and alkylaminocarbonyl or and phenyl or phenylcarbonyl in each case optionally monosubstituted to pentasubstituted by identical or different substituents from the group consisting of halogen, alkyl, halogenoalkyl and alkoxy, or R is the radical --CONHR.sup.1, in which R.sup.1 represents alkyl which is monosubstituted or disubstituted by identical or different substituents from the group consisting of cyano, carboxyl and alkoxycarbonyl, andX represents hydrogen, halogen, alkyl or halogenoalkyl.

Abstract: Herbicidally active pyrroles of the formula ##STR1## wherein R.sup.1 represents C.sub.1-4 alkyl, or one R.sup.1 together with the other R.sup.1 forms tetramethylene or butenylene,X represents hydrogen or halogen,Y represents O or S,n represents 0 or 1,R.sup.2 represents hydrogen or an organic radical.

Abstract: N-hetaryl imidazole derivatives of general Formula I ##STR1##are disclosed in whichHet represents an optionally substituted monocyclic or bicyclic heteroaromate,R.sup.3 represents hydrogen, a straight or branched C.sub.1-6 -alkyl group, or a C.sub.1-6 -alkoxy-alkyl group, andR.sup.4 represents --COOR.sup.5 --CONR.sup.6 R.sup.7 --CN, ##STR2##with R.sup.5 meaning hydrogen, a straight or branched C.sub.1-6 -alkyl group, R.sup.6 and R.sup.7 are the same of different and represent hydrogen or a straight, branched, or cyclic alkyl group with up to 7 carbon atoms or, together with the nitrogen atom, form a saturated five or six ring optionally containing another heteroatom and R.sup.8 means hydrogen or a straight, branched or cyclic alkyl group with up to 7 carbon atoms.

Abstract: A compound of the formula: ##STR1## wherein R is a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group, a C.sub.3 -C.sub.4 alkenyl group, a C.sub.3 -C.sub.4 alkynyl group, a halo(C.sub.1 -C.sub.4)alkyl group, a halo(C.sub.3 -C.sub.4)alkenyl group, a halo(C.sub.3 -C.sub.4)alkynyl group, a C.sub.1 -C.sub.2 alkoxy(C.sub.1 -C.sub.2) alkyl group, a C.sub.1 -C.sub.2 alkoxy(C.sub.1 -C.sub.2)alkoxy(C.sub.1 -C.sub.2)alkyl group, a cinnamyl group, a cyano(C.sub.1 -C.sub.3)alkyl group, a carboxy(C.sub.1 -C.sub.3)alkyl group, a C.sub.1 -C.sub.5 alkoxycarbonyl(C.sub.1 -C.sub.3)alkyl group, a halo(C.sub.1 -C.sub.5)alkoxycarbonyl(C.sub.1 -C.sub.3)alkyl group, a C.sub.1 -C.sub.2 alkoxyalkoxycarbonyl(C.sub. 1 -C.sub.3)alkyl group, a C.sub.1 -C.sub.2 alkoxy (C.sub.1 -C.sub.2)alkoxycarbonyl(C.sub.1 -C.sub.3)alkyl group, a C.sub.1 -C.sub.5 alkoxycarbonyl(C.sub.1 -C.sub.2)-alkoxycarbonyl(C.sub.1 -C.sub.3)alkyl group, a cyclo(C.sub.3 -C.sub.6)alkoxycarbonyl(C.sub.1 -C.sub.3)alkyl group, a C.sub.1 -C.sub.5 alkylaminocarbonyl(C.sub.1 -C.

Abstract: Compounds corresponding to Formula I ##STR1## wherein R.sup.1 denotes an acyl group andX denotes hydrogen, halogen, alkoxy, aroxy, SO.sub.3 H or a heterocyclic group attached through --O-- or --N<are prepared form a compound corresponding to Formula II ##STR2## wherein X has the meaning already indicated and Q denotes the group required for completing a dicarbonimide ringby reduction of the said compound to the amino compound and acylation into a compound corresponding to Formula III ##STR3## wherein X, Q and R.sup.1 have the meanings indicatedfollowed by conversion of the compound corresponding to Formula III into a compound corresponding to Formula I by hydrazinolytic or hydrolytic decomposition of the dicarbonimide ring.

Abstract: The 6-[D(-)-alpha(4-ethyl-2,3-dioxopiperazin-1-ylcarbonylamino)-alphaphenylace tamido]penicillanic acid and the salts thereof are prepared by synthetizing the novel intermediates, thioesters of D(-)-alpha-(4-ethyl-2,3-dioxopiperazin-1-ylcarbonylamino)-alpha-phenylacet ic acid, with mercaptoheterocycles and by converting them into the desired compound by reaction with 6-amino-penicillanic acid.

Abstract: Substituted N-phenylsulfonyl-N'-pyrimidinylureas and N-phenylsulfonyl-N'-triazinylureas of the general formula ##STR1## and the salts thereof with amines, alkali metal bases or alkaline earth metal bases, or with quaternary ammonium bases, have good pre- and postemergence selective herbicidal and growth regulating properties.In the above formula the symbols have the following meanings:R.sup.1 is hydrogen, halogen, nitro, cyano, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.1 -C.sub.4 alkylsulfinyl, --CO--R.sup.8, --NR.sup.9 R.sup.10, --CO--NR.sup.11 R.sup.12 or --SO.sub.2 --NR.sup.13 R.sup.14,R.sup.2 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl or C.sub.1 -C.sub.4 alkylsulfonyl,R.sup.3 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl or cyano,R.sup.4 is hydrogen or C.sub.1 -C.sub.4 alkyl,R.sup.5 is hydrogen, C.sub.

Abstract: The invention relates to compounds of the formula ##STR1## Y is O or S, *A is paraphenylene or *--(CH.sub.2).sub.n --(X).sub.m --(CH.sub.2).sub.r --, X is O, S or --CH.dbd.CH--, n or r, independently, are integers from 0 to 3, s is an integer from 0 to 1, m is an integer from 0 to 1, provided that when m is 1, n+s must be at least 2, R.sub.1 and R.sub.2, independently, are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, Het or aryl, *E is ##STR2## or --(CH.sub.2).sub.k -- wherein k is an integer from 0 to 4, R.sub.3, R.sub.4 and R.sub.8 are independently hydrogen or lower alkyl, R.sub.5 and R.sub.6, independently are hydrogen or lower alkyl, R.sub.

Abstract: A class of bicyclic nitrogen heterocyclic ether and thioether compounds exhibiting pharmacological activity including cytoprotective, H.sub.2 -antagonist, anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions are disclosed.

Abstract: 5-Hydroxy-2-benzothiazolesulfonamide is useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions including drops and inserts are disclosed.

Abstract: Thioacetonitriles and other derivatives of benzo- and azabenzothiazoles and their use as antiviral agents are disclosed.

Abstract: N-amides of 2-benzothiazolinone have been found to be effective in regulating the growth of leguminous plants.