Abstract: A compound of formula (I) wherein R1 is phenyl substituted by one or more halogen atoms; R2 is —NH2; R3 is —NH2 or hydrogen; R4 is —CXNRaRb, —CXNH—(CH2)y—NRaRb; wherein X is ═O or +S; y is an integer zero, 1 or 2; Ra and Rb, which may be the same or different, are selected from hydrogen and C1-4 alkyl or together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered heterocycle containing one or two nitrogen heteroatoms, which heterocycle can be further substituted with one or more C1-4 alkyl groups; and pharmaceutically acceptable derivatives thereof.

Abstract: Compounds having Formulas 5 and 6 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.

Abstract: This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

Abstract: A process for the preparation of arylamides of heteroaromatic carboxylic acids of the formula: in which each An is nitrogen or CRn(n=1 to 5), with the proviso that at least one of the ring members is nitrogen and that two nitrogen atoms are not bonded directly to one another; R1 to R5, if present, independently of one another are hydrogen, C1-4-alkyl or aryl, one of the substituents R1 to R5 being a group of the formula —OR, in which R is an optionally substituted aromatic or heteroaromatic radical; R6 is hydrogen or C1-4-alkyl; and R7 is an optionally substituted aromatic or heteroaromatic radical. The amides are obtained from the corresponding heteroaromatic halogen compounds, the corresponding aromatic amines and carbon monoxide in the presence of a palladium phosphine complex. Compounds of this class are important herbicides.

Abstract: Compounds of the Formula I are inhibitors of the 5&agr;-reductase 1 isozyme, and are useful alone, or in combination with a 5&agr;-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.

Abstract: A compound of the general formula I: is disclosed as useful in treating disorders of the central nervous system. Pharmaceutical compositions, processes for preparing the compounds and methods of treatment are also disclosed.

Abstract: Compounds of the general structural formula I are selective NPY Y5 receptor antagonists. The compounds and compositions of the present invention are useful in the treatment of obesity and complications associated therewith.

Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.7, Q, X and Y are as defined herein.

Abstract: This invention relates to a novel oxirane carboxylic acid derivative and thereof manufacturing method. Based on thereof mechanism to inhibit the CPT I, oxirane carboxylic acid derivative of this invention has blood glucose lowering effects so that the derivative may be effectively used as an antidiabetic agent having remarkable antidiabetic activity and less side effects.

Abstract: Since a compound represented by general formula (1), its pharmaceutically acceptable salt and a hydrate of the pharmaceutically acceptable salt have high antipsychotic activity, they may be used as an active ingredient for preparation of an antipsychotic. ##STR1## Also provided are an optical resolution method of the above compound and an intermediate for preparation of the compound.

Abstract: Substituted pyrazine derivatives of the general formula I ##STR1## where X is an oxygen or sulfur atom or a sulfoxyl or sulfonyl group;n is 0, 1 or 2;Z is a group ##STR2## where Y is oxygen or sulfur, R.sup.6 is hydrogen, alkyl, alkoxy, halogen or haloalkyl and p is 0 or 1;and R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the meanings stated in claim 1,and agriculturally useful salts of the compounds I are useful in herbicides.

Abstract: A compound which inhibits human thrombin and where has the structure and pharmaceutically acceptable salts thereof, wherein such as ##STR1## which are useful for inhibiting formation of blood platelet aggregates in blood in a mammal.

Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning described in the specification, have retinoid-like biological activity.

Abstract: A process for the preparation of arylamides of heteroaromatic carboxylic acids of the formula: ##STR1## in which each A.sup.n is nitrogen or CR.sup.n (n=1 to 5), with the proviso that at least one of the ring members is nitrogen and that two nitrogen atoms are not bonded directly to one another; R.sup.1 to R.sup.5, if present, independently of one another are hydrogen, C.sub.1-4 -alkyl or aryl, one of the substituents R.sup.1 to R.sup.5 being a group of the formula --OR, in which R is an optionally substituted aromatic or heteroaromatic radical; R.sup.6 is hydrogen or C.sub.1-4 -alkyl; and R.sup.7 is an optionally substituted aromatic or heteroaromatic radical. The amides are obtained from the corresponding heteroaromatic halogen compounds, the corresponding aromatic amines and carbon monoxide in the presence of a palladium phosphine complex. Compounds of this class are important herbicides.

Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.6, Q, and X are as defined herein.

Abstract: This invention relates to substituted and unsubstituted ???(aryl- and heteroaryl-) alkyl-, alkyloxy-, alkylthio-, oxo-, thio-, and alkylamino!- heteroaryl and aryl!- alkylamino-, aminoalkyl-, alkyloxy-, and alkylthio!- aryl and heteroaryl compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are useful as antagonists of the pain enhancing effects of E-type prostaglandins, to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods for treating pain comprising the administration of such compounds.

Abstract: New compounds of general formula (I) are provided: ##STR1## which are explained in the specification can be prepared by a variety of methods. The compounds may be used in pharmaceutical compositions.

Abstract: A compound of the general formula (I) ##STR1## wherein A represents a group of general formula ##STR2## and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Q.sup.2, Q.sup.3, and n are as described in the specification. The compounds of formula (I) are useful as agricultural herbicides.

Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.7, Q, X and Y are as defined herein.

Abstract: Compounds of formula (I) are inhibitors of the 5.alpha.-reductase 1 isozyme, and are useful alone, or in combination with a 5.alpha.-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.

Abstract: Pyrimidine derivatives useful as a gastrointestinal prokinetic agent, represented by formula ##STR1## wherein X is O or NR.sup.5, Y is O, S or NR.sup.5 wherein R.sup.5 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or the like;R.sup.1 and R.sup.2 may be the same or different and each is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or the like;R.sup.3 is CN, or COOR.sup.6 wherein R.sup.6 is a C.sub.1 -C.sub.6 alkyl group, a C.sub.3 -C.sub.6 cycloalkyl group, an aryl group or the like;R.sup.4 is --SR.sup.7 or --NR.sup.8 R.sup.9 wherein R.sup.7 is a C.sub.1 -C.sub.6 alkyl group;R.sup.8 is a C.sub.1 -C.sub.6 alkyl group or the like;R.sup.9 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or the like, or R.sup.8 and R.sup.9 may represent, together with the nitrogen atom to which they are attached, an N-substituted piperazine ring of formula (X) ##STR2## wherein R.sup.10 represents a C.sub.1 -C.sub.6 alkyl group or the like or a pharmacologically acceptable salt 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 piperdine derivative having the formula (I) or a pharmacologically acceptable salt thereof:R.sup.1 --X--A--R.sup.2 (I)wherein R.sup.1 is selected from the group consisting of substituted or unsubstituted pyrazine, naphthalenedicarboxylic acid imide, bicyclo oct-5-ene-2,3-dicarboxylic acid imide and pyromellitimide;X is --(CH.sub.2).sub.n --, --O(CH.sub.2).sub.n --, --S(CH.sub.2).sub.n --, --NH(CH.sub.2).sub.n --, --SO.sub.1 NH(CH.sub.2).sub.n --, ##STR1## --CH.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## wherein n is an integer of 1 through 7 and R.sup.3 is hydrogen, lower alkyl or a benzyl, ##STR3## --O--CH.sub.2 CH.sub.2 CH.dbd. or ##STR4## R.sup.2 is hydrogen, lower alkyl, benzyl, benzyl substituted with hydroxy, methoxy or chlorine, benzoyl, benzyl with a fluorine substituent, pyridyl, 2-hydroxyethyl, pyridylmethyl or ##STR5## wherein Z represents a halogen atom.

Abstract: Compounds of formula (I), wherein A represents CH.dbd.CH; Q represents pyrazine having substituents R.sup.6 and R.sup.7 ; R.sup.1 represents H or C.sub.1-6 alkyl; R.sup.2 represents H, C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, C.sub.3-6 cycloalkyl or NH.sub.2 CH.sub.2 CO--; R.sup.3 represents H, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.4 and R.sup.5 independently represent H, OH, C.sub.1-6 alkoxy, C.sub.1-6 alkyl, halogen, trifluoromethyl or NR.sup.8 R.sup.9 ; R.sup.6 and R.sup.7 independently represent H, OH, C.sub.1-6 alkoxy, C.sub.1-6 alkyl, halogen, trifluoromethyl, C.sub.1-6 hydroxyalkyl, amidino, CONH.sub.2 or NR.sup.8 R.sup.9 ; in addition, R.sup.6 and R.sup.7 may independently represent O when substituted on N; R.sup.8 and R.sup.9 independently represent H or C.sub.1-6 alkyl; and pharmaceutically acceptable derivatives thereof. The compounds are useful as pharmaceuticals, in particular in the treatment of neurological disorders.

Abstract: Sulfonamidocarboxamides of the formula ##STR1## wherein A, M, Q, X and Y have the significance given in the description, as well as hydrates, solvates and salts thereof, which inhibit thrombin-induced blood platelet aggregation and clotting of fibrinogen in plasma, as described. The compounds of formula I can be prepared by amidination of a cyclic amino group standing for grouping X or by C(O)N(Q) amide formation.

Abstract: Compounds corresponding to the general formula (I) ##STR1## in which n represents 0 or 1, R.sub.1 represents a methyl group, in which case R.sub.2 represents a phenoxy(C.sub.1 -C.sub.4)alkyl group (in which the phenoxy group is optionally substituted), or else R.sub.1 and R.sub.2 together form, and with the nitrogen atom which carries them, a 4-(phenoxymethyl)piperid-1-yl group (in which the phenoxy group is optionally substituted) or a 4-phenylpiperazin-1-yl group (in which the phenyl group is optionally substituted), R.sub.3 represents a hydrogen atom or a methyl group, R.sub.4 represents a hydrogen atom and R.sub.5 represents a hydrogen atom or a group of general formula -CH.sub.2 -CH.sub.2 -NH-R.sub.6, R.sub.6 being a hydrogen atom or a tert-butyloxycarbonyl, 4-carbamoylpyrimidin-2-yl or 5-carbamoylpyrazin-2-yl group, are useful in the treatment of diseases and complaints involving hyperactivity of the .alpha.-adrenergic system at the level of the lower urinary apparatus.

Abstract: The present invention relates to 4(3H)-pteridinones represented by the formula: ##STR1## in which X is an oxygen atom or a sulphur atom, Y is a hydrogen atom, a lower alkyl radical, especially a methyl radical, at the 6-position or a hydroxyl group at the 7-position, R.sub.1 is a hydrogen atom, a lower alkyl radical, a substituted or unsubstituted phenyl radical, a benzyl radical, a methoxymethyl group, an acetyl group, a 2-acetoxyethyl group or a 2,2,2-trifluoroethyl group and R.sub.2 is a hydrogen atom or a lower alkyl radical, especially a methyl radical.Application of these compounds as anti-allergic drugs.

Abstract: A p-aminophenol derivative having anti-inflammatory activity, represented by the formula ##STR1## wherein each of R.sup.1 and R.sup.2 is independently a hydrogen atom or a C.sub.1-6 acyl group; Ar is a pyrazine, pyrazine N-oxide, thiazole, benzene, pyridine, pyridazine, pyrimidine or triazine ring; R.sup.3 is a hydrogen atom, a C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy-carbonyl-C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a halogen atom or a carboxy-C.sub.1-6 alkyl group; A is a C.sub.1-6 alkylene group; and B is a C.sub.1-6 alkyl group, or a salt thereof.

Abstract: This application relates to a process for preparing a N-t-alkyl-1,2-diacylhydrazine by reacting a 1,3,4-oxadiazole with a tertiary alkyl cation precursor in the presence of a strong acid catalyst. Preferably, the 1,3,4-oxadiazole is a 2,5-disubstituted-1,3,4-oxadiazole and more preferably a 2,5-diaryl-1,3,4-oxadiazole. The strong acid catalyst is preferably a sulfur containing acid and more preferably sulfuric acid.

Abstract: Pyrazinone derivatives useful as insecticides have the formula (I): ##STR1## wherein A is N or C-R.sup.1 ; R.sup.1 and R.sup.2 are independently selected from hydrogen, halogen, haloalkyl, cyano or nitro; R.sup.3 and R.sup.4 are independently selected from hydrogen, halogen, alkyl or cycloalkyl; R.sup.5 is cyano, halo, nitro, alkoxy, haloalkyl, haloalkoxy or --S(O).sub.n R.sup.10 ; R.sup.6 is halo, cyano, nitro, haloalkyl, haloalkoxy, alkoxycarbonyl or --S(O).sub.n R.sup.10 ; R.sup.7 is hydrogen, halogen, cyano, nitro, alkyl, alkoxy, alkylthio, haloalkylthio, alkoxycarbonyl, NR.sup.11 R.sup.12 or haloalkyl; R.sup.8 is H, halo, NR.sup.11 R.sup.12, alkyl, cycloalkyl or S(O).sub.n R.sup.10 ; and R.sup.9 is oxygen or sulphur; where n is 0, 1 or 2; and R.sup.10 is alkyl, haloalkyl or cycloalkyl and R.sup.11 and R.sup.12 are independently selected from hydrogen, alkyl, cycloalkyl, benzyl or substituted benzyl.

Abstract: Novel aminomethyloxooxazolidinyl arylbenzene derivatives, wherein the aryl includes the phenyl, substituted phenyl, pyridyl, and substituted pyridyl groups, such as (l)-N-{3-[4- (4'-pyridyl)phenyl]-2-oxooxazolidin-5-ylmethyl}acetamide, possess useful antibacterial activity.

Abstract: Compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof, which have .beta..sub.2 -adrenoreceptor stimulant activity. They may be used in the treatment of diseases associated with reversible airways obstruction, such as asthma and chronic bronchitis.In preferred embodiments, Q represents a chlorine atom or a trifluoromethyl group, X represents a C.sub.3-4 alkylene chain, Y a C.sub.1-5 alkylene chain, R, R.sup.1 and R.sup.2 are each preferably a hydrogen atom or a methyl group and Het represents a pyrimidinyl pyrazinyl, triazinyl, thiazolyl, quinolinyl, benzimidazolyl, benzothiazolyl, benzoxazolyl or pyridyl group.

Abstract: Certain gem-dimethyl substituted bicyclic phenolic pyrazines of formula III possess eukalemic diuretic properties. They are of value in treating those diseases and conditions in which a eukalemic diuretic effect is required, for example in treating edema, hypertension and/or related conditions.

Abstract: Compounds possessing both a hindered amine moiety, such as a derivative of 2,2,6,6-tetramethylpiperidine, and a nitrone moiety are valuable stabilizers for protecting polymer compositions against the deleterious effects of actinic light and from the adverse effects of high temperature polymer processing environments. Additionally, the instant compounds present the opportunity for grafting onto preformed polymer backbones.

Abstract: Certain amine containing phenolic pyrazines of formula III possess eukalemic diuretic properties and are of value in treating diseases and conditions in which a eukalemic diuretic effect is required, for example in treating edema, hypertension and/or related conditions.

Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## wherein A is pyridyl, furyl, thienyl, pyridazinyl, pyrimidinyl or pyrazinyl; n is 0-5; and B is H, --COOH and its esters, amides and pharmaceutically acceptable salts, --CHO and its acetal derivatives, --COR.sub.1 and its ketal derivatives where R.sub.1 is --(CH.sub.2).sub.n CH.sub.3 where n is defined above, or --CH.sub.2 OH and its ether and acyl ester derivatives; or a pharmaceutically acceptable salt.

Abstract: This invention comprises novel pyrazine amides which are useful as eukalemic diuretics.

Abstract: Novel pyrazine amides of Formula III (set out hereinafter) are disclosed which are useful as eukalemic diuretics.

Abstract: Processes for preparing bicyclic compounds useful as anti-allergic, anti-inflammatory and/or cytoprotective agents are described, together with a process for preparing intermediates thereof.

Abstract: The invention provides methods of treating diseases characterized by hyperexcitability of neurons. An amount of a substituted pyrazinoylguanidine compound effective to regulate excitability of the neurons is administered. Substituted pyrazinoylguanidines having the formula ##STR1## wherein R is halogen and R.sup.1 is a member of the group consisting of hydrogen, benzyl and optionally substituted benzyl are useful in the invention. The invention also discloses a method of treating neurons having hyperexcitable cell membranes.

Abstract: Heteroaryloxy-.beta.-carboline derivatives of general Formula I ##STR1## wherein R.sup.1 is an optionally substituted heteroaryl residue,R.sup.2 is hydrogen, lower alkyl or lower alkoxyalkyl,X is a COOR.sup.3 -group wherein R.sup.3 means H or lower alkyl, or represents a CONR.sup.4 R.sup.5 -group wherein R.sup.4 and R.sup.5 mean respectively hydrogen or lower alkyl, R.sup.4 and R.sup.5 being capable of forming, together with the nitrogen atom, a 5- to 6-membered heterocycle, or means an oxadiazolyl residue of the formula ##STR2## wherein R.sup.6 means hydrogen, lower alkyl or cycloalkyl, are valuable pharmaceuticals.

Abstract: The synthesis of 7-n-alkyl-imidazolium[4,5-d]-pyrimidines, 6-substituted-3n-alkyl-benzimidazolium- and 3n-alkyl-5,6-substituted-benzthiazolium salts are described. There N.sup.+ -surfactants having a substituted heterocycle as a head group have distinguished small critical micelle concentrations (CMC) in the range of 10.sup.-5 -10.sup.-7 Mol/Liter. The size and shape of these micelles in watery solutions are determined by the nature of the anion. The N-surfactants can be used as pharmaceuticals as well as reporter groups in fluorescence studies including immunological assays.

Abstract: Disclosed are compounds of the formula ##STR1## wherein: R.sup.1 is a lower alkyl group;R.sup.2 and R.sup.3 are each hydrogen or lower alkyl or R.sup.2 and R.sup.3 taken together may form --(CH.sub.2 (.sub.4)-- or --CH.dbd.CH--CH.dbd.CH--;.alpha. is a 5- or 6-membered heteroaromatic ring group containing 1 to 3 hetero-atoms selected from the group consisting of nitrogen, oxygen and sulfur, or a pyrazine-N-oxide ring, pyridazine-N-oxide ring or pyrimidine-N-oxide ring group, wherein each of these heteroaromatic ring groups may optionally have 1 to 3 substituents selected from the group consisting of a lower alkyl, halogen, phenyl, lower alkoxycarbonyl, amino, lower alkoxy and hydroxy-lower alkyl, with the proviso that said 5- or 6-membered heteroaromatic ring group is not thiazolyl, isothiazolyl, pyridyl or 1,3,5-triazinyl group; or salts thereof. These compounds and salts thereof have anti-inflammatory activity and lipoxygenase-inhibitory activity.

Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein: Het is monocyclic heteroaryl having two adjacent carbon atoms, a and b, depicted in formula (I); p1 R.sub.1 and R.sub.2 are independently selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl and C.sub.1-6 Alkoxy;R.sub.3 is hydroxy, C.sub.1-6 alkoxy, C.sub.3-7 alkenyl-methoxy, phenoxy or phenyl C.sub.1-4 alkoxy in which either phenyl moiety may be substituted by one or two C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halo; CO.sub.2 R.sub.6 wherein R.sub.6 is hydrogen or C.sub.1-6 alkyl, CONR.sub.7 R.sub.8 or SO.sub.2 NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are independently hydrogen or C.sub.1-6 alkyl or together are C.sub.4-6 polymethylene, NO.sub.2, (CH.sub.2).sub.m OR.sub.9 wherein m is 1 or 2 and R.sub.9 is C.sub.1-6 alkyl or S(O).sub.n R.sub.10 wherein n is 0, 1 or 2 and R.sub.10 is C.sub.

Abstract: Acylpyrazines useful in the treatment of hypertension are disclosed.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: one of R.sub.1 and R.sub.2 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl or R.sub.1 and R.sub.2 together are C.sub.2-5 -polymethylene;either R.sub.3 is hydrogen, hydroxy, C.sub.1-6 alkoxy or C.sub.1-7 acyloxy and R.sub.4 is hydrogen or R.sub.3 and R.sub.4 together are a bond;R.sub.5 is hydrogen C.sub.1-6 alkyl optionally substituted by halogen hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkoxycarbonyl, carboxy or amino optionally substituted by one or two independent C.sub.1-6 alkyl groups, or C.sub.2-6 alkenyl, amino optionally substituted by a C.sub.1-6 alkyl or C.sub.1-6 alkenyl group or by a C.sub.1-6 alkanoyl group optionally substituted by up to three halo atoms, by a phenyl group optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen, or aryl or hetroaryl, either being optionally substituted by one or more groups or atoms selected from the class of C.sub.1-6 alkyl, C.sub.

Abstract: 2-Amino-3-cyano-5-dialkoxymethylpyrazine derivatives of the general formula III ##STR1## where R.sup.1 and R.sup.2 are each hydrogen or a protective group usually employed for amino groups and R.sup.5 and R.sup.6 are each alkyl of 1 to 4 carbon atoms, or together form an ethylene or propylene radical which is unsubstituted or substituted by methyl, are prepared starting from a novel 3-halomethyl-5-dihalomethyl-2-aminopyrazine derivative of the formula IV ##STR2## where X is Cl or Br, via a novel intermediate of the general formula I ##STR3## where R.sup.3 is --CH.sub.2 --O--CO--CH.sub.3 (a), --CH.sub.2 OH (b), ##STR4## or --C.tbd.N (d) and R.sup.4 is --CHCl.sub.2 or --CHBr.sub.2 or, where R.sup.1 and R.sup.2 are each a protective group, R.sup.4 may furthermore be ##STR5##The compounds according to the invention are useful intermediates for the preparation of folic acid and active compounds derived from this.

Abstract: 2,6-Disubstituted derivatives of 3-nitropyrazine are disclosed to have activity in increasing the sensitivity of tumor cells to radiation. Also disclosed are methods of preparing such compounds and pharmaceutical compositions including such compounds.

Abstract: 2,6-Disubstituted derivatives of 3-nitropyrazine are disclosed to have activity in increasing the sensitivity of tumor cells to radiation. Also disclosed are methods of preparing such compounds and pharmaceutical compositions including such compounds.

Abstract: Certain 2-substituted-2-penem-3-carboxylic acid compounds and pharmaceutically-acceptable salts thereof can be prepared from the appropriate xanthate or trithiocarbonate by desulfurization and addition of an electrophilic sulfur compound followed by halogenation and ring closure. The corresponding desulfurized and halogenated olefinic intermediates are disclosed.