Abstract: There is provided heterocyclic compounds of the following formula (I): 1

Abstract: The invention provides compounds which are potent inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to compounds having a structure according to the following Formula (I): wherein R1, R2, X, Z, m, and n are defined below. to This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. The compounds of the present invention are useful for the treatment of diseases and conditions which are characterized by unwanted metalloprotease activity. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for metalloprotease-related maladies using these compounds or the pharmaceutical compositions containing them.

Abstract: A crosslinking agent having reactive benzoxazine groups is provided. The crosslinking agent is the ungelled reaction product of a polyhydric aromatic compound and an aminotriazine compound having one or less non-alkylated NH bond per triazine ring. The crosslinking agent is essentially free of hydroxyl functionality and has a glass transition temperature of at least 10° C. Additionally provided is a method for preparing the crosslinking agent. Also provided is a curable powder coating composition including a solid particulate, film-forming mixture of a polymer having functional groups reactive with benzoxazine groups and the crosslinking agent. Further provided is a multilayer composite coating composition having a base coat layer deposited from a film-forming base coating composition and a topcoat layer deposited from the curable powder coating composition. Coated substrates are also provided.

Abstract: The present invention relates generally to cyclic carbamates and isoxazolidines or Formula (I) or their pharmaceutically acceptable salts thereof, which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.

Abstract: A 6-phenyltetrahydro-1,3-oxazin-2-one derivative having the formula (I): wherein, R1 is an unsubstituted or substituted C1 to C8 alkyl group; an unsubstituted or substituted C3 to C7 cycloalkyl group;, etc., R2 is a C1 to C4 alkyl group, R3 is H; an unsubstituted or substituted C1 to C5 alkyl group; etc., R4 is H; an unsubstituted or substituted C1 to C6 alkyl group, and R5 and R6 are independently a hydrogen atom; an unsubstituted or substituted C1 to C5 alkyl group; etc. an optical isomer thereof, or a pharmacologically acceptable salt thereof, or a hydrate or a solvate thereof and pharmaceutical compositions containing the same, in particular a drug for the prevention or treatment of inflammatory diseases and a drug for asthma. The above 6-phenyltetrahydro-1,3-oxazin-2-one derivative has a strong type IV PDE inhibitory activity and has a bronchiodilator and antiinflammatory effects.

Abstract: The present invention provides a compound of formula I Wherein R1 is C1-7 alkyl, optionally substituted by hydroxy or NR4R5; R2 is C1-7 alkyl substituted by hydroxy or NR4R5; R3 is H, F or C1-7 alkoxy; R4 and R5 together with N are a 5- or 6-membered heterocyclic moiety having 1-3 heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur in which sulfur may be substituted by one (1) or two (2) oxygen atoms; and pharmaceutically acceptable salts thereof Compounds of formula I of the present invention are useful as antiviral agents.

Abstract: A novel compound having the formula: wherein R is an alkyl group containing 1-5 carbon atoms or an aryl, substituted aryl, substituted or unsubstituted heteroaryl, alkyl-aryl, alkylether-aryl or O; R1 and R2 are hydrogen or a methyl group; X is O, NH, NR′ wherein R′ is an alkyl group containing 1-5 carbon atoms, or O—R″ or NR″ wherein O—R″ is O-alkyl-O or O-alkyl, NR″ is O-alkyl-ONH, wherein each instance alkyl contains 1-5 carbon atoms and n is 0 or 1. The compound of this invention is useful as a monomer which can be polymerized and/or copolymerized by catonic polymerization. Polymers and copolymers produced in this invention can be crosslinked and are useful in coatings, inks, overprint varnishes, and surface treatment applications.

Abstract: There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

Abstract: There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

Abstract: The present invention relates to mixtures comprising the compound I in a proportion of 65-95% by weight, the compound II in a proportion of 5-35% by weight and the compound III in a proportion of 0-10% by weight wherein the substituents are as defined in the description, and to mixtures with other compounds. The mixtures are suitable for stabilizing organic material against the effect of light and heat.

Abstract: The invention relates to the use of azine derivatives, some of which are known, of the formula ##STR1## in which A represents substituted phenyl, or represents in each case optionally substituted naphthyl, pyridyl, thienyl or pyrazolyl;B represents hydrogen, alkyl or in each case optionally substituted phenyl, phenylalkyl, phenylalkenyl, phenoxyalkyl, phenylthioalkyl, phenylsulfinylalkyl or phenylsulfonylalkyl;D represents hydrogen or alkyl;E represents hydrogen, alkyl or in each case optionally substituted phenyl, phenylalkyl, phenoxyalkyl, phenylthioalkyl, phenylsulfinylalkyl or phenylsulfonylalkyl;G represents hydrogen or alkyl;J represents hydrogen or alkyl;K represents hydrogen, alkyl or optionally substituted phenyl; orB and D or D and G or E and G together represent optionally substituted alkanediyl, wherein one or two CH.sub.2 groups are optionally replaced by O and/or S; andW and Y are different and represent N, O or S, wherein the ring always contains an N atom,for combating animal pests.

Abstract: Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.

Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

Abstract: 4-Benzoylpyrazoles of the formula I ##STR1## useful for controlling harmful plants, are disclosed.

Abstract: The present invention relates to novel protein tyrosine phosphatase modulating compounds having the general structure shown in Formula (A1), to methods for their preparation, to compositions comprising the compounds, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phosphotyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganism, eukaryoic cells, whole animals and human being. R' and R" are independently selected from the group consisting of hydrogen, halo, cyano, nitro, trihalomethyl, alkyl, arylalkyl. R'" is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, arylalkyl. X is aryl. Y is selected from hydrogen or ##STR1## wherein (*) indicates a potential point of attachment to X.

Abstract: Chemiluminescent labeling compounds and chemiluminescent labeled conjugates are provided. The compounds comprise an acridan ring bearing an exocyclic double bond and further contain a labeling substituent which permits attachement to compounds of interest. The novel chemiluminescent compounds and labeled conjugates generated chemiluminescence rapidly after undergoing a reaction with an acid, an oxidant and a base. The compounds and conjugates are useful in assays of an analyte in a sample and in assays employing labeled specific binding pairs.

Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

Abstract: Compounds of the formula (I) and their salts ##STR1## in which R.sup.1 to R.sup.6, Y.sup.1, to Y.sup.2, Y.sup.3, m and n are as defined in claim 1 are suitable as herbicides and plant growth regulators. They can be prepared analogously to known processes using intermediates of the formula (V) (cf. claim 6).

Abstract: 1,3-Oxazin-4-one derivatives of formula (I): ##STR1## wherein Q represents --C(.dbd.O)--, --CH(OH)-- or --C(OR.sup.11)(OR.sup.11)--, in which R.sup.11 represents lower alkyl; or the two groups --OR.sup.11, together with the carbon atom to which they are attached, form a five or six membered cyclic ketal group; and their use as herbicides.

Abstract: 1,3-oxazin-4-ones of formula (I), ##STR1## wherein R.sup.1 represents phenyl optionally substituted; R.sup.2 represents: a straight- or branched-chain alkyl having from one to ten carbon atoms which is substituted by one or more groups R.sup.8 which may be the same or different; a straight- or branched-chain optionally halogenated alkenyl or alkynyl group having up to ten carbon atoms; or a group selected from cyano, --CHO, --COR.sup.7, --CO.sub.2 H, --CO.sub.2 R.sup.7, --COSR.sup.7, --CONR.sup.9 R.sup.10, --CH.dbd.NOH, --CH.dbd.NOR.sup.7, --CH.dbd.NOCOR.sup.7, --CH.dbd.NNR.sup.9 R.sup.10, --CH.sub.2 CN, --CH.sub.2 NO.sub.2 and oxiranyl; R.sup.3 represents phenyl optionally substituted or R.sup.3 represents a first five to seven membered heteroaromatic ring; said first ring being optionally fused and said first ring being linked to the nitrogen atom of the group NR.sup.6 via one of the ring carbon atoms; R.sup.4 and R.sup.5 independently represent lower alkyl; W represents --NR.sup.6 --; R.sup.

Abstract: Cyclic amides of Formula I which are useful as fungicides: ##STR1## wherein A is N; G is N and the floating double bond is attached to A; W is O or S; X is OR.sup.1, S(O).sub.m R.sup.1 or halogen; R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y and Z are defined in the disclosure, are disclosed. Also, disclosed are fungicidal compositions containing these compounds and the use of these cyclic amide compounds for controlling plant diseases caused by fungal plant pathogens.

Abstract: The invention relates to compounds of the formula ##STR1## in which: A is a divalent radical selected from:A.sub.1) --O--CO--A.sub.2) --CH.sub.2 --O--CO--A.sub.3) --O--CH.sub.2 --CO--A.sub.4) --O--CH.sub.2 --CH.sub.2 --A.sub.5) --N(R.sub.1)--CO--A.sub.6) --N(R.sub.1)--CO--CO--A.sub.7) --N(R.sub.1)--CH.sub.2 --CH.sub.2 --A.sub.8) --O--CH.sub.2 --in which:R.sub.1 is a hydrogen or a (C.sub.1 -C.sub.4)-alkyl; andAm is a nitrogen-containing heterocycle.

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: Substituted 2-aminopyridine compounds of Formula (I) and pharmaceutically acceptable salts which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders.

Abstract: Heterocyclic compounds IR.sup.1 --X--L (I)whereL is a cyclic carbamate residue, a lactonoxy residue or a lactam residue,X is an oxygen-containing group ##STR1## where A is a linker, and R.sup.1 is an organic radical or a group L,are used as activators for inorganic peroxy compounds, in particular as cold bleach activators or optical brighteners in detergents, cleaners and bleaches and in disinfectants.

Abstract: The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R.sup.1, R.sup.1a, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4, R.sup.4a, R.sup.4b, R.sup.4c, R.sup.5, D, X, Y, n, x and y are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.

Abstract: Compounds of the following formula useful for inhibiting Ras function and therefore inhibiting or treating the abnormal growth of cells are disclosed: ##STR1## or an N-oxide thereof, or a pharmaceutically acceptable salt or solvate thereof, wherein:R and R.sup.2 are independently selected from halo;R.sup.1 and R.sup.3 are independently selected from the group consisting of H and halo, provided that at least one of R.sup.1 and R.sup.3 is H;R.sup.4 is ##STR2## or R.sup.5 ; R.sup.5 is ##STR3## and the remaining variables are as defined in the specification.

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: Compounds of the formula ##STR1## wherein Q is a hydrazone derivative;R.sup.1 is hydrogen, halogen, alkyl or alkoxy;R.sup.2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; andR.sup.6 is a substituted carboxamide, carbothioamide, phosphonosoamide, or phosphonothioamide,useful as anti-HIV agents.

Abstract: There has been found a new process for the preparation of 5,6-dihydro-1,3-oxazines, some of which are known, of the formula (I) ##STR1## in which A represents substituted phenyl, or represents in each case optionally substituted naphthyl, pyridyl, thienyl or pyrazolyl, andB represents hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl, halogenoalkyl, alkenyl, optionally substituted cycloalkyl, or in each case optionally substituted phenyl, phenylalkyl, phenylalkenyl, phenoxyalkyl, phenylthioalkyl, pyridyl or 2- or 3-pyrrolylby reacting amide derivatives of the formula (II) ##STR2## with ethylene in the presence of hydrogen chloride gas and of a catalyst. The new 5,6-dihydro-1,3-oxazines can be used for combatting animal pests.

Abstract: There is disclosed an azetidinone compound of the formula ?I!: ##STR1## wherein Ring B is a benzene ring which may have substituent(s), R.sup.1 is a hydroxy-substituted lower alkyl group which may have substituent(s), X is oxygen atom and the like, Y is oxygen atom and the like, and Z is a methylene group which may have substituent(s), which is useful as a synthetic intermediate of the 1 .beta.-methylcarbapenem-type antibacterial agent.

Abstract: Compounds of the formula: ##STR1## wherein: X is O, NH or NR.sup.1 ; R.sup.1 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.4)alkyl, aryl or aryl (C.sub.1 -C.sub.4)alkyl; wherein the C.sub.1 -C.sub.6 alkyl group is optionally substituted by fluorine and the C.sub.3 -C.sub.7 cycloalkyl or C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.4 )alkyl group is optionally substituted in the cycloalkyl ring by up to two substituents each independently selected from halo, C.sub.1 -C.sub.4 alkoxy or halo(C.sub.1 -C.sub.4)alkoxy; R.sup.2 is phenyl optionally substituted with one or two halo substituents, indolyl or thienyl; R.sup.3 is NH.sub.2, --NR.sup.4 SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --NR.sup.4 SO.sub.2 aryl, --NR.sup.4 CO(C.sub.1 -C.sub.6 alkyl), --NR.sup.4 CO aryl or a 5 to 7-membered N-linked cyclic group incorporating W in the ring wherein W is O, NR.sup.5, CH(OH), CHCO.sub.2 H, CHN(R.sup.4).sub.2, CHF, CF.sub.2, C.dbd.O or CH.sub.2 ; R.sup.4 is H or C.sub.1 -C.sub.

Abstract: The invention relates to new substituted pyrazol derivatives of general formula (I) in which: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 have the meanings given in the description, agents with herbicidal action containing at least one compound of formula (I), and their use as herbicides.

Abstract: Disclosed herein are herbicidal pyridine compounds substituted at the 2- or 6-position with an OR.sub.2 moiety where R.sub.2 is hydrogen, lower alkyl, halomethyl, lower cyanoalkyl, alkenyl or alkynyl, as well as herbicidal compositions and herbicidal use of these compounds.

Abstract: Disclosed are compounds of the formula ##STR1## wherein Ar represents an aryl or heteroaryl group; andR.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 represent organic or inorganic substituents,which compounds are highly selective partial agonists or antagonists at human CRF1 receptors and, thus, are useful in the diagnosis and treatment of treating stress related disorders such as post trumatic stress disorder (PTSD) as well as depression, headache and anxiety.

Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

Abstract: The invention relates to compounds of the formula ##STR1## in which: A is a divalent radical selected from:A.sub.1) --O--CO--A.sub.2) --CH.sub.2 --O--CO--A.sub.3) --O--CH.sub.2 --CO--A.sub.4) --O--CH.sub.2 --CH.sub.2 --A.sub.5) --N(R.sub.1)--CO--A.sub.6) --N(R.sub.1)--CO--CO--A.sub.7) --N(R.sub.1)--CH.sub.2 --CH.sub.2 --A.sub.8) --O--CH.sub.2 --in which:R.sub.1 is a hydrogen or a (C.sub.1 -C.sub.4)-alkyl; andAm is a nitrogen-containing heterocycle.

Abstract: The present invention relates to a novel pyrazolopyridine compound of the following formula: ##STR1## wherein R.sup.1 is aryl, andR.sup.2 is cyclo(lower)alkyl which may have one or more suitable substituent(s), etc; and a pharmaceutically acceptable salt thereof, which is useful as a medicament; the processes for the preparation of said pyrazolopyridine compound or a salt thereof; a pharmaceutical composition comprising said pyrazolopyridine compound or a pharmaceutically acceptable salt thereof; etc.

Abstract: The present invention is directed to certain novel compounds identified as 4-heterocycle substituted piperidines of the general structural formula: ##STR1## wherein R.sup.1, R.sup.4, R.sup.5, A, R.sup.3 and the dashed line are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.

Abstract: A compound represented by the chemical formula ?1!: ##STR1## wherein Z is oxygen or sulfur, Y is halogen, optionally substituted alkyl, optionally substituted alkoxycarbonyl, optionally substituted alkoxy, S(O).sub.p r.sup.1 wherein p denotes an integer from 0 to 2, r.sup.1 is optionally substituted alkyl, nitro, cyano or optionally substituted amino, m denotes an integer from 1 to 3, R.sub.1, R.sub.2 and R.sub.4 are same or different one another and each independently hydrogen, optionally substituted alkyl or optionally substituted phenyl, R.sub.3 is alkyl, alkenyl, aralkyl, cycloalkyl, phenyl, naphthyl, pyridyl, furyl or thienyl, those which substituents can be further optionally substituted by halogen, hydroxy, optionally substituted alkyl or the like, and a chemical agent for controlling pests.

Abstract: This invention relates to novel heterocycles including 3-?1-?3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzylo xycarbonylamino)propionic acid, which are useful as antagonists of the .alpha..sub.v .beta..sub.3 integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.

Abstract: The subject invention relates to 5-Substituted trans-1-piperazinoindan derivatives having general formula (I), ##STR1## wherein X is halogen, trifluromethyl, alkyl, alkylthio, alkyloxy, hydroxy, alkylsulphonyl, alkyl- or dialkylamino, triflouromethylthio or cyano; R is hydrogen, or alkyl, alkenyl, cycloalkyl, cycloalkyl lower alkyl, optionally substituted with hydroxy, or R is a substituent, ##STR2## wherein n is an integer from 1 to 6; U is CH or N; Y is, CH.sub.2, O, S or N-R.sup.1, R.sup.1 being hydrogen or cycloalkyl, cycloalkylmethyl, alkyl or alkenyl optionally substituted with hydroxy or an optionally substituted phenyl group; W is O or S; Z is --(CH.sub.2).sub.4 --, ##STR3## where R.sup.2 and R.sup.3 are hydrogen or lower alkyl, --CH.dbd.CH--, --CH.dbd.CH--CH.sub.2 --, optionally substituted 1,2-phenylene, 1,2-C.sub.6 H.sub.4 CH.sub.2 -- (to form a quinazolidinone or -thione ring system) or 1,2-C.sub.6 H.sub.

Abstract: The invention relates to neurokinin receptor antagonist compounds of the formula ##STR1## in which: A is a divalent radical selected from:A.sub.1) --O--CO--A.sub.2) --CH.sub.2 --O--CO--A.sub.3) --O--CH.sub.2 --CO--A.sub.4) --O--CH.sub.2 --CH.sub.2 --A.sub.5) --N(R.sub.1)--CO--A.sub.6) --N(R.sub.1)--CO--CO--A.sub.7) --N(R.sub.1)--CH.sub.2 --CH.sub.2 --A.sub.8) --O--CH.sub.2 --in which:R.sub.1 is a hydrogen or a (C.sub.1 -C.sub.4)-alkyl; andAm is a nitrogen-containing heterocycleAPPLICATION: Neurokinin receptor antagonists.

Abstract: Method of preparation of 6-fluoro-2-halogen quinoline of general formula (I) wherein R is a hydrogen atom or an alkyl radical and Hal and Hal' are identical or different halogen atoms. The invention is characterized in that a halogenating agent is made to act on hydroxy-1 quinoline of general formula (II) wherein Hal is defined as above and R.sub.1 is defined as R excepting a hydrogen atom, the acid function being optionally released if a 6-fluoro-2-halogen quinoline is to be obtained for which R is a hydrogen atom.

Abstract: Disclosed are novel cyanoguanidine derivatives which are usable as an epoxy resin curing agent and are represented by the following general formula (1). A thermosetting resin composition and a photocurable and thermosetting resin composition containing the following cyanoguanidine derivatives and other derivatives as the epoxy resin curing agent are also disclosed. ##STR1## wherein R.sup.1 represents a substituent selected from the group consisting of the following substituents (a) through (k).

Abstract: Compounds of formula (I): ##STR1## [wherein: R.sup.1 is a cyclic amino group, or a dialkylamino group; R.sup.2 a group of formula --NHCHR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 are each alkyl aryl or aralkyl, or together form a cycloalkyl group, or R.sup.2 is an aromatic heterocyclic group, or a group of formula --B--S(O).sub.m --R.sup.5 wherein R.sup.5 is a substituted alkyl group, or an aromatic heterocyclic group; B is an alkylene or alkylidene group; m is 0, 1 or 2; A is a group of formula --CH.dbd.CH-- or --(CH.sub.2).sub.n --, where n is 1, 2 or 3]; and salts thereof have valuable anti-ulcer activity.

Abstract: This invention relates to L-Arginine aldehyde derivatives, pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents.