Abstract: 2,2-Dialkyl-4-aryl-substituted benzopyran and benzothiopyran derivatives of the formula ##STR1## where the symbols have the meaning described in the specification, have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists.

Abstract: A red fluorescent material includes a compound of the formula: ##STR1## wherein: R.sub.1, and R.sub.2 are individually alkyl of from 1 to 20 carbon atoms, aryl, carbocyclic and other heterocyclic systems; andR.sub.3, and R.sub.4 are individually alkyl of from 1 to 10 carbon atoms, and a branched or unbranched 5 or 6 member substituent ring connecting with R.sub.1, R.sub.2 respectively; andR.sub.5 is alkyl of from 2-20 carbon atoms; sterically hindered aryl and heteroaryl; andR.sub.6 is alkyl of from 1 to 10 carbon atoms, and a 5 or 6-member carbocyclic ring connecting with R.sub.5.

Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or 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 optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.

Abstract: Certain N-acetonylbenzamides and their use as fungicides are disclosed. The N-acetonylbenzamides disclosed contain a heterocyclic ring fused to an aromatic ring. These compounds are particularly effective against phytopathogenic fungi of the class Oomycetes. Also disclosed is a method for controlling phytopathogenic fungi by applying one or more of the heterocyclic N-acetonylbenzamides of the present invention, optionally with one or more additional fungicidal compounds.

Abstract: Compounds of the formula ##STR1## which have antifungal activity.

Abstract: Nonlinear optical compounds which contain a heteroaromatic ring and may further comprise a tricyanovinyl group attached to the heteroaromatic ring.

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention.

Abstract: A compound having the structure: ##STR1## wherein (a) n is from 1 to about 3;(b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen;(e) W is hydrogen or straight, branched or cyclic alkyl, aryl, hydroxy or alkoxy; and(f) R.sub.1 and R.sub.2 are independently hydrogen or straight, branched or cyclic alkyl having from one to 10 carbon atoms, aryl, heterocyclyl, heteroaryl, hydroxy, or alkoxy; or R.sub.1 and R.sub.2 are bonded together to form a ring having from from 3 to about 7 atoms wherein one to three atoms may be heteroatoms.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.

Abstract: A method is provided for the regioselective, palladium catalyzed carbo- or heteroannulation of internal alkynes by aryl iodides containing o-substituted side chains to yield aromatic carbocyclic and heterocyclic ring systems.

Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

Abstract: A process for preparing compounds of the formula ##STR1## where a, b d, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein including condensation of a phenol of formula ##STR2## with an acetal of formula ##STR3## in the presence of a catalytic amount of a tertiary amine. The compounds of formula I are intermediates useful in the preparation of pyranyl cyanoguanidine derivatives.

Abstract: A process for producing chlorosulfate and sulfamate esters of 2,3:4,5-bis-O-(1-methylethylidene)-.beta.-D-fructopyranose and (1-methylcyclohexyl)methanol is disclosed. The process involves a two step procedure involving in the first step reacting of an alcohol with sulfuryl chloride in the presence of a tertiary or heterocyclic amine base in a solvent selected from the group consisting of toluene, t-butyl methyl ether or tetrahydrofuran to produce a chlorosulfate intermediate, which is preferably stabilized by an aqueous wash and/or treatment with a base, and in the second step reacting of the resulting intermediate with an amine in a solvent selected from the group consisting of t-butyl methyl ether, tetrahydrofuran and lower alkanol.

Abstract: Sulfamate derivatives having the following formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are as herein defined, have been found to exhibit anticonvulsant activity and are thus useful in the treatment of conditions such as epilepsy. Further, the present invention encompasses pharmaceutical compositions containing a compound of formula (I) as well as methods for their use and novel intermediates are disclosed.

Abstract: A trialkylamine derivative represented by the formula (1) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different from each other and each represents lower alkyl;R.sup.3, R.sup.4 and R.sup.5 may be the same or different from one another and each represents hydrogen, lower alkyl, lower alkoxy, lower alkoxycarbonyl or halogen;R.sup.6 and R.sup.7 may be the same or different from each other and each represents hydrogen or lower alkyl;R.sup.8 represents hydrogen, lower alkyl, lower alkoxy or halogen;X represents oxygen, sulfur, --CH.dbd.N-- or --CH.dbd.CH--;Y represents oxygen, sulfur, methylene, N--R.sup.11 (wherein R.sup.11 represents lower alkyl), SO or SO.sub.2 ;Z represents --OCO(CH.sub.2).sub.p .about. or --OCH.sub.2 (CH.sub.2).sub.p .about. (wherein p represents a number of 0 to 4 and symbol .about.

Abstract: A method of producing a deuterated or undeuterated 11-nor-.DELTA..sup.8 -tetrahydrocannabinol (THC) glucuronide or deuterated or undeuterated 11-nor-.DELTA..sup.9 -THC glucuronide by reacting a blocked THC carboxylic acid precursor with a blocked sugar epoxide precursor is disclosed. Also disclosed are: deuterated 11-nor-.DELTA..sup.8 - or .DELTA..sup.9 -THC carboxylic acid glucuronide having a deuterated hydrocarbon chain; 5'-deuterated 11-nor-.DELTA..sup.8 - or .DELTA..sup.9 -THC-carboxylic acid or 5'-deuterated .DELTA..sup.8 - or .DELTA..sup.9 -THC glucuronide. The compositions are useful as GC-MS standards; in methods for preparing antibodies reactive with a THC glucuronide; and, in GC-MS diagnostic methods for THC metabolites.

Abstract: The isomer ratio of a cis-isomer against the corresponding trans-isomer with respect to the 5-6 double bond is improved in the production of prostaglandins, when a lactol is reacted with an ylide to cause simultaneously formation of the 5-double bond and an .alpha.-chain, whereby the ylide generated from a phosphonium salt with a potossium base, and a solvent which is liquid at the reaction temperature and has a dipole moment of 0.3 to 3.0D are used.

Abstract: Compounds of the general formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, n and p are as herein defined; exhibit anticonvulsant activity and are thus useful in the treatment of conditions such as epilepsy. Compounds of this class are also useful for the treatment of glaucoma, peptic ulcers, hypertension, congestive heart failure and other types of edema. Furthermore, pharmaceutical compositions containing a compound of formula (I) as well as methods for their use and novel intermediates are disclosed.

Abstract: Cyclic ethers are prepared by reacting an unsaturated olefin oligomer derived from an alpha-olefin monomer containing from about 6 to 20 carbon atoms with an aldehyde in the presence of an acid catalyst.

Abstract: The present invention relates to new substituted benzoxazepines and benzothiazepines of the general formula I ##STR1## in which X, R.sup.1, R.sup.2 and R.sup.3 have the meaning given in the description, processes for their preparation and their use in medicaments having vaso- and muscle-relaxing properties, in particular as circulatory agents.

Abstract: A process for the preparation of 15-pentadecanolide, wherein bis-(13-oxabicyclo[10.4.0]hexadec-12-yl)peroxide is subjected to a thermal treatment in an organic solvent, eventually followed by hydrogenation of the resulting reaction product, which treatment is carried out in an organic solvent having a boiling point comprised between about 170.degree. and 250.degree. C.

Abstract: Cyclic ethers are prepared by reacting an unsaturated olefin oligomer derived from an alpha-olefin monomer containing from about 6 to 20 carbon atoms with an aldehyde in the presence of an acid catalyst.

Abstract: Amines of the following formula: ##STR1## where the variables are defined in the specification are useful in the treatment of diseases associated with altered motility and/or tone of smooth muscle.

Abstract: A process for producing an optically active dihydropyran derivative represented by formula (1): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 each represents a hydrogen atom, a lower alkyl group, a tri-lower alkylsilylmethyl group, a lower alkoxycarbonylamino group, or an --OR.sup.5 group, wherein R.sup.5 represents a lower alkyl group, a lower acyl group, a lower alkoxycarbonyl group, a di-lower alkylcarbamoyl group, or a tri-lower alkylsilyl group, or R.sup.1 and R.sup.2 are taken together to form a 5- to 7-membered cyclic hydrocarbon group or to form a condensed heterocyclic group with an oxygen atom, or R.sup.2 and R.sup.3 are taken together to form a 5- to 7-membered cyclic hydrocarbon group or to form a condensed heterocyclic group with an oxygen atom, provided that all of R.sup.1, R.sup.2, R.sup.3, and R.sup.4 do not represent hydrogen atoms at the same time; and R.sup.6 represents a lower alkyl group, which comprises reacting a diene compound represented by formula (2): ##STR2## wherein R.

Abstract: Described are camphonyl spirocyclooxaoctane-containing compositions having the generic structures: ##STR1## and mixtures of same with substituted cyclopentenyl-oxabicyclooctanes defined according to the generic structures: ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 ' and R.sub.3 " each represents hydrogen or methyl and R.sub.4 ' represents hydrogen or C.sub.1 -C.sub.5 alkyl, processes for preparing same and uses thereof in augmenting or enhancing the aroma of perfume compositions, colognes and perfumed articles, e.g., solid or liquid anionic, cationic, nonionic or zwitterionic detergents, cosmetic preparations, fabric softener compositions, fabric softener articles, hair preparations and perfumed polymers.

Abstract: Described are cyclopentenyl-oxabicyclooctanes, cyclopentenyl-formylcyclohexenes and cyclopentylhydroxymethyl cyclohexenes having the generic structures: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 ', and R.sub.3 " each represents hydrogen or methyl with the provisos:(i) one or two or R.sub.1, R.sub.2, R.sub.3 ' and R.sub.3 " represents methyl;(ii) R.sub.1 and/or R.sub.2 are methyl;(iii) at least one of R.sub.3 ' and R.sub.3 " is hydrogen; and(iv) when R.sub.1 and R.sub.2 is methyl then each of R.sub.3 ' and R.sub.3 " is hydrogenwherein R.sub.4 ' is hydrogen or C.sub.1 -C.sub.5 alkyl, processes for preparing same and uses thereof in augmenting or enhancing the aroma of perfume compositions, colognes and perfumed articles, e.g., solid or liquid, anionic, cationic, nonionic or zwitterionic detergents, cosmetic preparations, fabric softener compositions, fabric softener articles, hair preparations and perfumed polymers.

Abstract: A compound of the formula: ##STR1## where in x-y is --CO--CH.sub.2 --, --COCR.sup.10-, --CHOHCHR.sup.8-, --CH.dbd.CR.sup.8 -- or ##STR2## and R.sup.9 is various, R.sup.1 and R.sup.8 are alkyl, R.sub.2 is H or alkyl and R.sup.1 and R.sup.2 are alkylene, are disclosed as useful as intermediates for cardiovascular agents.

Abstract: Described are alkyl-substituted tetra- or hexahydrobenzopyran derivatives defined according to one of the generic structures: ##STR1## wherein Z is a moiety in the alternative either ##STR2## wherein in the moiety having the structure: ##STR3## R' is methyl or ethyl and in the moiety having the structure: ##STR4## one of the dashed lines is a carbon-carbon double bond and each of the other of the dashed lines represent carbon-carbon single bonds; wherein R.sub.1 and R.sub.2 taken separately represent hydrogen or C.sub.1 -C.sub.3 lower alkyl (with the proviso that R.sub.1 and R.sub.2 are not both hydrogen) or R.sub.1 and R.sub.2 taken together complete a C.sub.5 or C.sub.

Abstract: The use of valepotriate hydrins in the prevention and treatment of disorders of the gastrointestinal tract is described, together with pharmaceutical compositions containing valepotriate hydrins and certain novel valepotriate hydrins per se.

Abstract: The use of valepotriate hydrins in the prevention and treatment of disorders of the gastrointestinal tract is described, together with pharmaceutical compositions containing valepotriate hydrins and certain novel valepotriate hydrins per se.

Abstract: A compound of the formula (I) ##STR1## wherein (1) when R.sub.1 is a C.sub.2-11 alkyl, a lower alkenyl, a lower alkynyl, a cycloalkyl, a lower alkoxyalkyl, an aralkyl which may be substituted, a lower haloalkyl or a 5 or 6 membered heterocycle;R.sub.2, R.sub.3 and R.sub.4 are the same or different, hydrogen, a halogen, cyano, nitro, amino, a lower alkyl, a lower haloalkyl, hydroxy, a lower alkoxy, an aryloxy, carboxy, or a lower alkoxycarbonyl;R.sub.5 is hydrogen, a halogen, a C.sub.1-11 alkyl, an aryl which may be substituted, an aralkyl which may be substituted;R.sub.6 is a C.sub.1-11 alkyl, a lower alkenyl, a lower alkynyl, a cycloalkyl, a lower alkoxyalkyl, an aryl which may be substituted, an aralkyl which may be substituted, a lower haloalkyl, or a 5 or 6 membered heterocycle; or R.sub.5 and R.sub.6 may be combined to form a group of --(CH.sub.2).sub.m -- (m is 3 or 4);(2) when R.sub.1 is an aryl which may be substituted;R.sub.2, R.sub.3, R.sub.4 and R.sub.5 have the same meanings as defined above; R.

Abstract: Cyclohexenone derivative of the formula ##STR1## where A is oxygen or NOR.sup.8, where R.sup.8 is alkyl, alkenyl, alkynyl, haloalkyl or haloalkenyl, chlorothienyl or alkoxyalkylB is O, S, SO or SO.sub.2,X is hydrogen or methoxycarbonyl,R.sup.1 is hydrogen, carbonylalkyl, benzoyl or a cation,R.sup.2 is alkyl,R.sup.3 and R.sup.4 are hydroxyl, chlorine, bromine, thioalkylcarboxyl, thiocarbonylalkyl, alkylcarbonyloxy, alkoxy, or alkylthio, or R.sup.3 and R.sup.4 together epoxy,R.sup.5 and R.sup.6 are hydrogen or methyl or R.sup.5 and R.sup.6 are together methyleneoxyethylene, andR.sup.7 is hydrogen or methyl,and herbicides containing these compounds.

Abstract: The invention relates to novel interfuranylene-prostacyclin derivatives of the general formula (I) ##STR1## wherein R.sup.1 stands for hydrogen or a straight or branched chain C.sub.1-6 alkyl group, an inorganic cation or for the protonated form of a base containing an amino group;R.sup.2 stands for hydrogen, a C.sub.1-4 alkanoyl or benzoyl group, a monosubstituted benzoyl, trialkylsilyl or an alkoxyalkyl group;R.sup.3 stands for a straight or branched chain C.sub.1-6 alkyl group, a phenyl group optionally substituted by halogen or by a C.sub.1-4 alkyl group, a heteroaryl group optionally substituted by halogen or by a C.sub.1-4 alkyl group or a cycloalkyl group;A stands for an ethylene or for a cis- or trans-vinylene or --C.tbd.C-- group;B means a chemical bond, a --CHR.sup.5 --, --CHR.sup.5 --CH.sub.2 -- or a --CH.sub.2 --O-- group: andR.sup.5 means hydrogen or a C.sub.1-4 alkyl group.

Abstract: Cyclohexane-1,3-dione derivatives of the formula ##STR1## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the meanings stated in the description, are used for controlling undesirable plant growth.

Abstract: Cyclohexenone derivatives of the formula ##STR1## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the meanings stated in the description, herbicides which contain these compounds and a method for controlling undesirable plant growth.

Abstract: A cyclopentenone compound represented by the following formula: ##STR1## has an antitumor effect and can be produced from the antibiotic XK-213.

Abstract: Pyrazole sulfonylureas are useful as pre- and post-emergence herbicides. Typical of this group is 3-[[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]aminosulfonylmethyl]-1,5-di methyl-1H-pyrazole-4-carboxylic acid, ethyl ester.

Abstract: Sulfamates of the following formula (I): ##STR1## wherein X is O or CH.sub.2 and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as herein defined have been found to exhibit anticonvulsant activity and are thus useful in the treatment of conditions such as epilepsy. Further, pharmaceutical compositions containing a compound of formula (I) as well as methods for their use and intermediates form part of the present invention.

Abstract: Substituted cinnamyl-2,3-dihydrobenzofurans and analogs were prepared from the nucleophilic substitution of a cinnamylhalide with a 2,3-dihydrobenzofuran anion or an analog thereof. These compounds were found to be potent topical anti-inflammatory agents.

Abstract: Sulfamates of the following formula (I): ##STR1## wherein X is O or CH.sub.2 and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as herein defined have been found to exhibit anticonvulsant activity and are thus useful in the treatment of conditions such as epilepsy. Further, pharmaceutical compositions containing a compound of formula (I) as well as methods for their use and intermediates form part of the present invention.

Abstract: The invention relates to 13-oxabicyclo[10.3.0]pentadecanes alkylated in the 14-position and, optionally, in the 15-position and to 13-oxabicyclo[10.4.0]hexadecanes alkylated in the 14-position and, optionally, in the 16-position. The compounds according to the invention may be used as odorizers.

Abstract: Processes for preparing dihydro-prostacyclin analogs, which are 9-deoxy-5,9-cyclic ethers of prostaglandin F.sub.1 .alpha.-type compounds, illustrated, for example, by a compound of the formula ##STR1## wherein .about. indicates alpha or beta configuration; including the products and intermediates produced therein, said products having pharmacological utility.

Abstract: Processes for preparing dihydro-prostacyclin analogs, which are 9-deoxy-5,9-cyclic ethers of prostaglandin F.sub.1 .alpha.-type compounds, illustrated, for example, by a compound of the formula ##STR1## wherein .about. indicates alpha or beta configuration; including the products and intermediates produced therein, said products having pharmacological utility.

Abstract: Processes for preparing dihydro-prostacyclin analogs, which are 9-deoxy-5,9-cyclic ethers of prostaglandin F.sub.1 .alpha.-type compounds, illustrated, for example, by a compound of the formula ##STR1## wherein .about. indicates alpha or beta configuration; including the products and intermediates produced therein, said products having pharmacological utility.

Abstract: The present invention provides novel 19-hydroxy-7a-homo-PGI.sub.1 19-hydroxy-19-methyl-7a-homo-PGI.sub.1 compounds which are useful for pharmacological purposes, e.g., anti-asthmatic indications.

Abstract: Single enanitiomers of 6-(2-hydrocarbyl-substituted ethenyl)-bearing, 4-hydroxy tetrahydro-2H-pyran-2-ones, e.g., 6.alpha.-[2-(2-methyl-1-naphthyl)ethenyl]-3,4,5,6-tetrahydro-4.beta.-hydro xy-2H-pyran-2-one (4R,6S) are obtained by a multi-step process which includes protecting and deprotecting hydroxy groups at various stages.

Abstract: There are described novel dihydropyrones of the formula I ##STR1## wherein R.sub.1 and R.sub.2 independently of one another are each a C.sub.1 -C.sub.4 -alkyl group, or one of the two substituents is also hydrogen, or R.sub.1 and R.sub.2 jointly form a C.sub.2 -C.sub.6 -alkylene bridge, R.sub.3 is C.sub.1 -C.sub.4 -alkoxy, C.sub.2 -C.sub.6 -alkenyloxy, C.sub.2 -C.sub.4 -alkynyloxy, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.3 -C.sub.5 -alkoxyalkoxy or hydroxyl, and X, Y and Z independently of one another are each hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, --S(O).sub.n -C.sub.1 -C.sub.4 -alkyl, --S(O).sub.n -C.sub.1 -C.sub.4 -haloalkyl, where n is 0, 1 or 2, or they are each C(O)OR.sub.4, where R.sub.4 is hydrogen or C.sub.1 -C.sub.4 -alkyl, or they are each NO.sub.2, CN or NR.sub.5 R.sub.6, where R.sub.5 and R.sub.6 independently of one another are each hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.

Abstract: Reactive iridoid derivates represented by the following general formula ##STR1## (wherein R represents a hydrogen atom, an alkyl group with 1 to 5 carbon atoms, an acyl group with 2 to 6 C atoms, an unsubstituted aralkyl group with 7 to 12 C atoms, a methanesulfonyl- or toluenesulfonyl group, a benzoyl-, a preferably para-substituted nitrobenzoyl- or chlorobenzoyl group, or a tetrahydropyranyl group), process for the manufacture of said derivatives starting from catapol as an easily obtainable natural substance and use of said derivatives as intermediates for the manufacture of prostanoids.

Abstract: Maltol (3-hydroxy-2-methyl-gamma-pyrone) is prepared from furfural through intermediates (a) 1-(2-furyl)-1-ethanol; (b) 2-(1-hydroxyethyl)-2,5-dialkoxy-2,5-dihydrofuran; (c) alkyl or aralkyl-2-methyl-2H-pyran-3(6H)-one; and (d) 2-alkyl or aralkyl-4-methyl-3,7-dioxabicyclo[4.1.0]heptan-5-one.Pyromeconic acid (3-hydroxy-gamma-pyrone), ethyl maltol (3-hydroxy-2-ethyl-gamma-pyrone) and other valuable 2-substituted-3-hydroxy-gamma-pyrones are prepared in an analogous manner from furfural.

Abstract: The present invention provides 2,5-inter-o-phenylene-3,4-dinor-5,9.alpha.-epoxy-6-iodo-PGF.sub.1 amides. These compounds are intermediates for preparing 2,5-inter-o-phenylene-3,4-dinor-prostacyclin analogs, which are useful for pharmacological purposes, e.g., as antithrombotic agents.

Abstract: The present invention provides 2,5-inter-o-phenylene-3,4-dinor-5,9.alpha.-epoxy-PGF.sub.1 amides. These compounds are useful for a wide variety of pharmacological and therapeutical purposes, e.g., as antithrombotic agents.