Abstract: The present invention relates to an improved process for the preparation of nicotinic acids represented by the following structural formula (I): ##STR1## which are prepared by reacting a nicotinic amide compound having the formula: ##STR2## under acidic conditions with a nitrite salt. In the process of the invention have the groups R.sup.1, R.sup.2, and R.sup.3, in the compounds are independently selected from the group consisting of hydrogen, and halogen atoms and R.sup.4 is selected from the group consisting of hydrogen, lower alkyl and aryl. The process provides the nicotinic acid compounds in improved yields.

Abstract: Pyridine derivatives of the formula ##STR1## wherein the ring A stands for an optionally further substituted benzene ring; the ring B stands for an optionally substituted pyridine ring; Q stands for hydroxyl group, or OQ.sup.1 or Q.sup.1 wherein Q.sup.1 stands for an optionally substituted aliphatic hydrocarbon group; and n denotes 0 or 1, or their salts, which have potassium.channel opening activity and are useful as therapeutic agents of circulatory diseases such as angina pectoris, hypertension, etc.

Abstract: HIV protease inhibitors, obtainable by chemical synthesis, block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and possibly other anti-vital agents as ingredients, are thus suitable for the treatment of the HIV virus known to cause AIDS.

Abstract: The reaction of cyanoolefins, aminocarbonylolefins or hydroxyiminoolefins with a Vilsmeier reagent leads to 2-halogenopyridines which bear aldehyde groups in the 3 and/or 5 position. These pyridinealdehydes are valuable intermediates for the preparation of pharmaceuticals and crop protection agents.

Abstract: A compound, composition, and method for controlling Take-all disease of plants by applying to the seed prior to planting, a fungicide of the formula: ##STR1## wherein Z.sub.1 and Z.sub.2 are C and are part of an aromatic ring which is pyridine; R and n are defined herein; A is selected from the group consisting of --C(O)--SR.sub.3, --NH--C(X)R.sub.4, --C(.dbd.NR.sub.3)--XR.sub.7, and --C(X)-amine wherein the amine is substituted with with an alkylaminocarbonyl and a hydrogen or wherein the amine has a first and a second amine substituent defined herein; B is --W.sub.m --Q(R.sub.2).sub.3 or selected from 0-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R.sub.4 ; Q is C, Si, Ge, or Sn; W is --C(R.sub.3).sub.p H.sub.(2-p) --; or when Q is C, W may also be selected from --N(R.sub.3).sub.m H(.sub.1-m)--, --S(O)p--, and --O--; X is O or S; n is 0, 1, 2, or 3; m is 0 or 1; p is 0, 1, or 2; each R.sub.

Abstract: Patients susceptible to or suffering from central nervous system are treated by administering an effective amount of an aryl substituted olefinic amine compound, such as (E)-metanicotine. (E)-metanicotine is provided from nicotine. Nicotine is reacted with ethyl chloroformate to produce ethyl N-methyl-N-[4-chloro-4-(3-pyridyl)butyl]carbamate, which then is reacted in the presence of potassium tert-butoxide, tetrahydrofuran and dimethylformamide to produce (E)-metanicotine N-ethyl carbamate, which then is subjected to hydrolysis using hydrochloric acid to produce a reaction mixture containing (E)-metanicotine. The reaction mixture containing (E)-metanicotine is adjusted to a slightly basic pH, and then contacted with dichloromethane. The resulting water immiscible phase then is separated from the aqueous phase. The aqueous phase, then is adjusted to a very basic pH, and then contacted with methyl tert-butyl ether.

Abstract: A process for the preparation of an aqueous medium of nicotinaldehyde by the catalytic reduction of 3-cyanopyridine under hydrogen in the presence of Raney-nickel.

Abstract: A process for preparing a compound of general formula ##STR1## where Ar represents an optionally substituted aromatic or heteroaromatic group, the process comprising reacting a compound of general formulaAr--C(L.sup.1).sub.2 Cl (II)where each L.sup.1 independently represents a leaving group (preferably a chlorine atom), with water in the presence of a Lewis acid and a chlorocarbon solvent which includes at least two chlorine atoms, is disclosed.

Abstract: The invention provides UV-absorbing compounds of formula (I) ##STR1## and compositions, including sunscreens, containing compounds of formula (I).

Abstract: The invention relates to new pyridine derivatives of general formula I which have useful properties, e.g., as leukotriene-B.sub.4 -antagonists. Pharmaceutical compositions containing these compounds can be used to treat various diseases.

Abstract: A process is described for preparing trifluoromethyl ketones of the formula I ##STR1## where R has the given meanings, wherein an alcohol of the formula II ##STR2## is reacted with a compound of the formula IVYO.sub.n H (IV)where n has the given meaning.

Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning defined in the specification.

Abstract: This invention relates to a compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein X is oxygen, sulfur, --CH.dbd.CH--, or --CH.dbd.N--;wherein R.sup.1 is --CO.sub.2 R.sup.2 or tetrazole;wherein R.sup.2 is hydrogen, alkyl of 1 to 6 carbons or a pharmaceutically acceptable cation;wherein R is an alkyl of from 1 to 20 carbons, --(CH.sub.2).sub.p CF.sub.3 or --(CH.sub.2).sub.q R.sup.3 wherein R.sup.3 is alkoxy, phenoxy or alkoxy substituted phenoxy wherein the alkoxy group has from 1 to 8 carbons;wherein p and q are integers from 0 to 20;wherein n is 0 or 1; andwherein m is 0, 1, 2, or 3.

Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which R, R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification,and a medicinal product containing said compound for treating a disorder of the melatoninergic system.

Abstract: Disclosed are pyridinecarboximidamides having a vasodilating effect (hypotensive activity or antianginal activity), and acid adduct salts thereof. ##STR1## wherein when R.sup.1 represents an alkyl, hydroxyalkyl, carboxyl, amino, acylamino, alkylamino, dialkylamino, aralkylamino, alkylsulfonamide, bisalkylsulfonylamino or hydroxyl group, R.sup.2 represents a hydrogen atom and R.sup.3 represents a nitroxyl, 2-chlorophenyl or phenyl group; andwhen R.sup.1 represents a hydrogen atom, R.sup.2 represents an alkyl, hydroxyalkyl, carboxyl, amino, acylamino, alkylamino, dialkylamino, aralkylamino, alkylsulfonamide, bisalkylsulfonylamino or hydroxyl group and R.sup.3 represents a nitroxyl, 2-chlorophenyl or phenyl group.There is also disclosed the use of the compounds represented by the formula (I) for antihypertensive or antianginal purpose.

Abstract: Fluorine-containing, chiral liquid crystal compounds comprise (a) an aliphatic fluorocarbon terminal portion containing at least two catenary ether oxygen atoms; (b) a chiral, aliphatic hydrocarbon terminal portion; and (c) a central core connecting the terminal portions. The compounds have smectic mesophases or latent smectic mesophases and are useful, for example, in liquid crystal display devices.

Abstract: Substituted tetrahydropyridines and piperidinecarboxylic acids and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which muscarinic antagonists are useful as agents for inhibiting gastric acid release, for treating bradycardia, bronchoconstriction, urinary incontinence, atonic conditions of the gut and bladder, Parkinson's disease, dystonias, and Alzheimer's disease.

Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function. Use is in human and veterinary medicine and in cosmetics.

Abstract: Novel fabric conditioners based on pyridine carboxylic acid esters or amides are described. The compounds are effective fabric conditioners and are biodegradable. Compositions including the compounds and a method of using the compositions are also described.

Abstract: Compounds of the formula ##STR1## wherein the variables are defined in the specification. The compounds and their salts are soft anticholinergic/antisecretory agents especially useful as mydriatics and as antiperspirants.

Abstract: Methods of inhibiting cell proliferation in a patient suffering from such disorder comprising the use of a styryl-substituted heteroaryl compound wherein the heteroaryl group is a monocyclic ring with 1 or 2 heteroatoms, or a bicyclic ring with 1 to about 4 heteroatoms, said compound optionally substituted or polysubstituted, with the proviso that when said ring is polysubstituted, the substituents do not have a common point of attachment to said ring, and those compounds wherein no substituent on the heteroaryl group is a carboxy group or an ester group, and pharmaceutical compositions comprising such compounds.

Abstract: Compounds of formula I ##STR1## wherein X, A, B, R.sup.1 and R.sup.2 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable ester thereof, processes for preparing the compounds and pharmaceutical compositions comprising them. The compounds are useful as potassium channel openers and as therapeutic agents in the treatment of urinary incontinence.

Abstract: Pyrido[2,3-d]pyridazin-5-one and pyrido[2,3-d]pyridazin-5-thione derivatives of general formula (I): ##STR1## wherein R and R.sup.1 independently represent hydrogen, optionally halogenated alkyl, alkenyl or alkynyl, optionally substituted heterocycle or a group --[CR.sup.41 R.sup.42 ].sub.n -(phenyl)-(R.sup.3).sub.q ;R.sup.2 represents halogen, optionally halogenated alkyl, alkenyl or alkynyl, CN; --CO.sub.2 R.sup.4 ; --S(O).sub.r R.sup.4 ; --NO.sub.2 ; --NR.sup.41 R.sup.42 ; --OH; --COR.sup.4, --S(O).sub.r R.sup.5, --CO.sub.2 R.sup.5, --OR.sup.5 ; --CONR.sup.41 R.sup.42, --OSO.sub.2 R.sup.5, --OSO.sub.2 R.sup.6, --OCH.sub.2 R.sup.5, --N(R.sup.41)COR.sup.6, --N(R.sup.41)SO.sub.2 R.sup.5, --N(R.sup.41)SO.sub.2 R.sup.6, --SO.sub.2 NR.sup.41 R.sup.42, optionally substituted phenyl, alkoxy or haloalkoxy;X represents oxygen or sulphur;R.sup.3 represents halogen, optionally halogenated alkyl, alkenyl, alkoxy, alkynyl, --OH, --S(O).sub.r R.sup.4, --CO.sub.2 R.sup.4, COR.sup.4, --CN, --NO.sub.2, --NR.sup.41 R.sup.

Abstract: Fluorine-containing, chiral and achiral liquid crystal compounds comprise (a) an aliphatic fluorocarbon terminal portion comprising a perfluorinated or partially-fluorinated alkylene group and a terminal hydrocarbon alkyl group, the groups optionally containing at least one catenary ether oxygen atom; (b) an aliphatic hydrocarbon terminal portion; and (c) a central core connecting the terminal portions. The compounds have smectic mesophases or latent smectic mesophases and are useful, for example, in liquid crystal display devices.

Abstract: The invention relates to nicotinic acid hydrazone derivatives of formula I: ##STR1## in which the various symbols are as defined in the description, and their use as herbicides or as intermediates in the synthesis of herbicides.

Abstract: A method for preparing a compound of the formula ##STR1## wherein Q is C--H or N; R.sup.1 is C.sub.1-C.sub.4 alkyl, benzyl or p-nitrobenzyl and X and Y are independently selected from fluoro and chloro comprising reacting a compound of the formula ##STR2## wherein Q is >C--H or N; X and Y are independently selected from fluoro and chloro; and Z is fluoro, chloro, 1-imidazolyl or substituted 1-imidazolyl, wherein the 1-imidazolyl group is substituted with one or two substituents independently selected from C.sub.1 to C.sub.4 alkyl, with a compound of the formula[M.sup.n+ ].sub.p [V.sup.p- ].sub.nwherein M is an alkaline earth metal, Cu or Mn, n is 2, V.sup.p-, wherein p is 1 or 2, is an anion of the formula ##STR3## or a dianion of the formula ##STR4## and R.sup.1 is C.sub.1 to C.sub.6 alkyl or paranitrobenzyl, with the proviso that when Z is 1-imidazolyl or substituted 1-imidazole, M is magnesium, copper or manganese and with the proviso that when Z is fluoro, chloro or bromo, V.sup.

Abstract: An intermediate, 5-Acyl-4,5,6,7-tetrahydrothieno [3,2-c ]pyridine- 2-carboxylic acid derivative of the following general formula (I): ##STR1## wherein R.sup.1 represents an acyl group and R.sup.2 represents a hydrogen atom or an alkyl group is useful for synthesizing ticlopidine hydrochloride from an inexpensive, easily available compound in short steps.

Abstract: The process for the production of the carboxylic acid chlorides of the aromatic nitrogen heterocycles of the series of the compounds of the general formulas: ##STR1## The hydroxy carboxylic acids of the aromatic nitrogen heterocycles from the series of the compounds of the general formulas: ##STR2## In the general formulas I to VI, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are the same or different and each is a hydrogen atom or a halogen atom. The chlorination is performed with a solution of phosphorous pentachloride in phosphoroxy chloride. The excess phosphorous pentachloride is converted into phosphoroxy chloride either with a C.sub.1 -C.sub.4 -carboxylic acid or with a silane of the general formula:(CH.sub.3).sub.3 --Si--OR.sub.9 VIIThen the product according to one of the general formulas I to III is isolated.

Abstract: The invention relates to sunscreen compounds of formula I ##STR1## wherein R.sup.1 is selected from alkyl, alkenyl, alkynyl substituted alkyl, substituted alkenyl, phenyl, substituted phenyl, substituted benzyl, cycloalkyl, cycloalkenyl, substituted cycloalkyl, substituted cycloalkenyl;R.sup.2 is selected from hydrogen, alkyl and alkoxy;R.sup.3 is selected from alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, phenyl, benzoyl, substituted phenyl, substituted benzyl, substituted benzoyl, cycloalkyl, substituted cycloalkyl, cycloalkenyl, substituted cycloalkenyl, alkanyoyl, substituted alkanoyl, the group OROROR.sup.9 wherein R is a bivalent hydrocarbon radical and R.sup.9 is alkyl, alkenyl, phenyl benzyl, substituted phenyl, substituted benzyl;R.sup.4 is alkyl or alkoxy;n is an integer from 0 to 4; andR.sup.5 and R.sup.6 are independently selected from alkyl, alkoxy, alkanoyl, alkanoyl substituted by hydroxyl or alkoxycarbonyl.

Abstract: There are disclosed various compounds of the formula below, ##STR1## where the parameters n, R.sub.1, R.sub.2 and X are as defined in the specification which are selective inhibitors of the reuptake of the serotonin and as such are useful for the treatment of depression and obsessive compulsive disorder.

Abstract: Pyridine derivatives of the formulae ##STR1## wherein W, X, Y and Z are each C--R.sup.4, N or N.fwdarw.O, with the proviso that the ring contains only one heteroatom, and the substituents R.sup.1, R.sup.2 and R.sup.3 have the following meanings:R.sup.1 is alkoxy, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl,R.sup.2 is hydrogen,R.sup.3 is formyl, 4,5-dihydrooxazol-2-yl or --CO--A--R.sup.5 or --CO--NR.sup.6.sup.R.sup.7, whereR.sup.

Abstract: Fluorine-containing liquid crystal compounds are provided. The compounds comprise a fluorocarbon terminal portion having at least one catenary ether oxygen and a hydrocarbon terminal portion, the terminal portion being connected by a central core, the compounds having smectic mesophases or having latent smectic mesophases.

Abstract: Imines are synthesized by the hydrogenation of pyridinecarbonitriles with amines in the presence of a rhodium-loaded catalyst. The resulting imines are stable and may be transiminated and then hydrogenated to form selected secondary amine products or may be hydrolyzed to aldehydes.Further, a very useful class of unsymmetrical secondary amines represented by the formula RCH.sub.2 NHAr (in which R is not aliphatic and Ar is aromatic and not attached to R), which has heretofore been accessible only with some difficulty, can be synthesized by processes herein disclosed utilizing the reductive intermolecular coupling of nitriles and primary aromatic amines.

Abstract: N-1 and C-5 heterocyclic pyrazoles, a method of their preparation, compositions containing the same and methods of their use are disclosed. The pyrazoles are useful in alleviating inflammatory and cardiovascular disorders in mammals.

Abstract: This invention relates to substituted bicycloheptadione derivatives with high herbicidal activity which are represented by general formula (I) ##STR1## (where R.sup.1 is a lower alkyl group, a phenyl group which may be substituted, an aralkyl group which may be substituted, or a heterocyclic group which may be substituted;R.sup.2 is, same or different, a halogen, an alkoxy group, an alkylthio group, an alkylsulfonyl group, an alkyl group, an alkoxyalkyl group, or an alkoxylcarbonyl group, and n is 0 to 4;R.sup.3 and R.sup.4 are, same or different, hydrogen or a lower alkyl group).

Abstract: This invention relates to a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein X is oxygen, sulfur, --CH.dbd.CH--or --CH.dbd.N--; wherein R.sub.1 is alkyl, alkenyl or alkynyl of about 1 to 20 carbon atoms; wherein R is --CO.sub.2 R.sup.2, tetrazole, methylsulfonamide or benzenesulfonamide, wherein R.sup.2 is hydrogen, alkyl of 1 to 6 carbon atoms or a pharmaceutically acceptable cation and R.sup.3 is hydroxyl or halogen, having utility as LTB.sub.4 synthesis inhibitors.

Abstract: An improved process for the preparation of 2,6-dichloro-5-fluoronicotinoyl chloride is described where a 2,6-dihydroxy-5-fluoronicotinic acid ester is converted in one step using phosphorus oxychloride and a lithium reagent to 2,6-dichloro-5-fluoronicotinoyl chloride and subsequent basic hydrolysis affords 2,6-dichloro-5-fluoronicotinic acid.

Abstract: A compound having the structural formula ##STR1## wherein: Y is selected from O and S;R.sub.1 and R.sub.4 are independently selected from fluorinated methyl, chlorofluorinated methyl, and C.sub.1 -C.sub.4 alkyl, provided that not both R.sub.1 and R.sub.4 may be C.sub.1 -C.sub.4 alkyl;R.sub.2 is selected from hydrogen, lower alkyl, haloalkyl, alkenyl, alkynyl, haloalkenyl, and a cation;R.sub.3 is selected from C.sub.1 -C.sub.5 alkyl, cycloalkyl, cycloalkylalkyl, hydroxy, and alkoxy; andX is selected from ##STR2## in which R.sub.8 is selected from H, alkyl and CF.sub.3 and R.sub.10 is selected from F, Cl, --OR.sup.1, --SR.sup.1, --NHR.sup.1, --N(R.sup.1).sub.2, phenyl, substituted phenyl, and --P(OR.sup.1).sub.2where R.sup.1 is as defined above; ##STR3## wherein R.sup.1 is as defined above; ##STR4## wherein R.sub.14 and R.sub.15 are independently selected from hydrogen and alkyl; and --N.dbd.C.dbd.O and their use as herbicides.

Abstract: A process for the preparation of a 3-amino-2-(het)aroyl-acrylic acid derivative fo the formula ##STR1## in which Y represents a nitrile, or an ester group, --COOR.sub.1, or an acetyl group, whereR.sup.1 denotes C.sub.1 -C.sub.4 -alkyl, andR denotes optionally substituted alkyl, cyclopropyl, alkoxy, phenyl or amino,A represents nitrogen or C--R.sub.2, whereR.sub.2 denotes hydrogen, methyl, halogen, nitro, methoxy or cyano,X.sub.1 and X.sub.2 are identical or different and denote halogen, andX.sub.3 denotes hydrogen, halogen or nitro andX.sub.4 denotes halogen, nitro, methoxy or methylthio, which comprises reacting a 3-dialkylamino-2-(het)aroyl-acrylic acid derivative of the formula ##STR2## in which R.sub.3 and R.sub.4 are the same or different and represent an alkyl group having 1 to 4 carbon atoms, or, together with the nitrogen atom to which they are bonded, form a ring,with a primary amine of the formula R--NH.sub.2 in the presence of at least one equivalent of an acid HX in a solvent or in excess acid.

Abstract: Pyridinecarboxylic acids and their acid chloride, aliphatic ester and alkylamide derivatives are prepared by passing vapors of a (trichloromethyl)pyridine compound, such as 2,3-dichloro-5-(trichloromethyl)pyridine over gamma-alumina at a temperature of about 250.degree. C. to 450.degree. C. to obtain a pyridinecarboxylic acid chloride compound, such as 2,3-dichloronicotinoyl chloride and, if desired, subsequently converting this compound to its acid, an ester, or an amide, such as 2,3-dichloronicotinic acid, methyl 2,3-dichloronicotinate, or N-methyl-2,3-dichloronicotinamide, by treatment with water, an aliphatic alcohol, or ammonia or an alkylamine, respectively.

Abstract: Described herein is a process for dehydration of substituted piperidine dicarbothioate compounds and a novel compound obtained thereby.

Abstract: A process for the preparation of 2,3-dichloro-5-acetylpyridine of the formula ##STR1## comprising decarboxylating a compound of the formula ##STR2## in which R.sup.1 stands for methyl or ethyl,in a mixture of water and a water miscible aprotic solvent.

Abstract: Processes for production of 2,6-substituted-3,5-pyridinedicarboxylic acids, esters, salts, amides, halides, and cyano compounds, useful as herbicides and as intermediates which provide herbicides.

Abstract: This invention relates to amine derivatives and salts thereof. These compounds have an anti-ulcer activity which is effective to human beings and animals. This disclosure relates to such compound, a process for the preparation thereof and an anti-ulcer agent containing the same.

Abstract: An optically active compound represented by formula (I): ##STR1## wherein R.sup.1 represents an alkyl group having from 6 to 18 carbon atoms or an alkoxy group having from 6 to 18 carbon atoms; A represents ##STR2## or ##STR3## wherein ring ##STR4## represents a nitrogen-containing hetero-aromatic ring; n and m each represents 0 or 1; R.sup.2 represents an alkyl group having from 1 to 12 carbon atoms; and C* is an asymmetric carbon atom. The compound of formula (I) exhibits excellent physicochemical stability, a low temperature range for the chiral smectic C phase when used either alone or in combination with other compounds, and a rapid response.

Abstract: A process for dehydration of a 4-(lower alkyl)-2,6-bis(trifluoromethyl)-2,6-bis(hydroxy)-piperidine-3,5-dicarboxyl ic acid thioesters and esters.

Abstract: Pyridine-3-peroxycarboxylic acid monopersulfate is herein disclosed, which has the formula: ##STR1## The process for its preparation and its use as bleaching agent.

Abstract: Herbicides of formula: ##STR1## in which: n=0,1, 2f=0,1A is chosen from the groups ##STR2## in which: Ar is chosen from the groups ##STR3## B is chosen from optionally substituted C.sub.1 -C.sub.10 alkyl and C.sub.3 -C.sub.

Abstract: A process for dehydrofluorination of a 2,6-(bis) trifluoromethyl-dihydropyridine-3,5-dicarbothioic acid ester.