Abstract: A naphthol derivative represented by the general formula (I), [wherein Y and Y′ indicate —(CONH)n—X or —COR; X is a phenyl group, a naphthyl group, an anthraquinonyl group, a benzimidazolonyl group or a carbazolyl group; R is a hydroxyl group, an alkoxy group having 1 to 6 carbon atoms, a halogen atom, a benzyloxy group, a phenyloxy group or a phenacyloxy group; R2 is a hydrogen atom, an alkaline metal, an alkyl group having 1 to 6 carbon atoms, an acyl group having 1 to 6 carbon atoms or a phenylalkyl group; Z is a group selected from the group consisting of a hydrogen atom, a halogen atom, a nitro group, a nitroso group and an amino group (Z may be substituted on any ring of the naphthalene ring); and n is an integer of 1 or 2; provided that R2 and Z do not simultaneously indicate a hydrogen atom when both R simultaneously indicate a hydroxyl group], and a process for producing the same.

Abstract: A method for manufacturing a color coupler used in a silver halide photographic light-sensitive material using an ammonium trihalide. Said method for manufacturing the color coupler comprising the following step: a step for halogenating a coupling position of a four equivalent coupler using a halogenating agent, wherein said halogenating agent is said ammonium trihalide.

Abstract: A nonlinear optical material which is characterized as having a relatively high macroscopic dipole moment achieved through the generally parallel packing of dipolar molecules in a relative orientation to reinforce their dipole moments. The nonlinear optical material may be a crystalline azine or imine bridged di-arene in which the arenyl groups, which can be the same or different, are substituted with an electron donor group on the first arenyl group Ar1 and A is an electron acceptor group which is substituted on the second arenyl group Ar2. B is an azine or imine bridge which extends between and interconnects the first and second arenyl groups. The nonlinear optical material has a dipole alignment factor of at least 0.1, more preferably, at least 0.5.

Abstract: Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.

Abstract: The subject of the invention is the products of formula (I): in which R1, R2, R3, R4, R5 and G are as defined in the description, the dotted lines represent an optional second bond, as well as the addition salts with acids and bases and the esters, their preparation process and the intermediates of this process, their use as medicines and the pharmaceutical compositions containing them.

Abstract: Dialkyl urea compounds are described which act as calcitonin mimetics. These compounds are useful in the treatment of diseases which are associated with bone resorption. The calcitonin mimetics of the present invention are also useful in assays for the determination of calcitonin receptor activity.

Abstract: Carboxylic acid ester derivatives of formula (1): wherein R is C1-C6 alkyl, R2 and R3 are independently hydrogen or C1-C3 alkyl, and Q is optionally substituted phenyl, can be easily converted by ring closing into pyridazin-3-one derivatives of formula (7): The carboxylic acids of formula (1) can be produced by reacting hydrazone compounds of formula (5): wherein R3 and Q are as defined above, with malonic acid monoester derivatives of formula (6): wherein R and R2 are as defined above, in the presence of a base.

Abstract: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.

Abstract: There is provided pharmaceutically useful compounds of formula I, ##STR1## wherein Ar.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 have meanings given in the description, which are useful as antagonists of neuropeptide Y and in particular in the treatment of cardiovascular diseases, for example vasoconstriction.

Abstract: A fungicidal compound of formula (I): or a stereoisomer thereof, wherein A is CH or N, B is OCH.sub.3 or NHCH.sub.3, E is --NR.sup.1 --C(CH.sub.3).dbd.N-- or --N.dbd.C(CH.sub.3)--NR.sup.1 --, R.sup.1 is H, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl or optionally substitute benzyl, R.sup.2 is H, C.sub.1-4 alkyl, halo(C.sub.1-4)alkyl, C.sub.3-6 cycloalkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl, and R.sup.3 is optionally substituted aryl or optionally substituted heterocyclyl.

Abstract: The 6-alkoxycarbonylpyridazin-3-one compounds given in the formula: ##STR1## wherein, X represents a hydrogen and so on, Y represents a halogen atom, R.sup.1 represents a C.sub.1 -C.sub.6 alkyl group, R.sup.2 represents a hydrogen and other groups as defind, R.sup.3 represents a C.sub.1 -C.sub.3 haloalkoxy group and B represents a hydrogen and other groups as defind,are intermediates to produce the pyridazin-3-one compounds given in the formula: ##STR2## wherein X represents a hydrogen atom and other groups as defind, Y represents a halogen atom, R.sup.2 represents a hydrogen atom and other groups as defind, R.sup.3 represents a C.sub.1 -C.sub.3 haloalkyl group and B represents a hydrogen atom and other groups as defined, which are herbicidal compounds.

Abstract: The present invention provides a chemically modified form of hemoglobin that is stabilized and can efficiently bind and release oxygen. In addition the chemically modified hemoglobin may be polymerized to increase its molecular weight and increase its stability so that it will have a longer half life in the circulatory system and may be used as a stable oxygen transport mediator which is useful as the basis of a blood substitute.

Abstract: Benzylhydroxylamines I ##STR1## (X=--N(R.sup.7)--O--; Y=O, S; R.sup.1 =halogen, CN, NO.sub.2, CF.sub.3 ; R.sup.2 =H, halogen; R.sup.3 =H, NH.sub.2, CH.sub.3 ;R.sup.4 =H, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylsulfinyl or C.sub.1 -C.sub.6 -alkylsulfonyl;R.sup.5 =H, halogen, C.sub.1 -C.sub.6 -alkyl;R.sup.6 =H, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.2 -C.sub.6 -alkenyl;R.sup.7 =H, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, C.sub.1 -C.sub.6 -alkylcarbonyl, C.sub.3 -C.sub.6 -alkenylcarbonyl, C.sub.3 -C.sub.6 -alkynylcarbonyl, C.sub.1 -C.sub.6 -alkoxycarbonyl, C.sub.2 -C.sub.8 -alkenyloxycarbonyl, C.sub.2 -C.sub.6 -alkynyloxycarbonyl, C.sub.1 -C.sub.6 -alkylthiocarbonyl, C.sub.1 -C.sub.6 -alkylsulfonyl, C.sub.1 -C.sub.

Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.

Abstract: The present invention relates to a class of compounds represented by the Formula I ##STR1## or a pharmaceutically acceptable salt thereof, wherein A is ##STR2## pharmaceutical compositions thereof and methods of using such compounds and compositions as .alpha..sub.v .beta..sub.3 antagonists.

Abstract: The present invention relates to the synthesis of a hydrazone .beta.-keto ester by the reaction of an alkyl diazoester with a hydrazone aldehyde in the presence of a Lewis acid In a preferred embodiment, the hydrazone .beta.-keto ester is then converted into a pyridazinone compound by the reaction with an alkyl acid chloride in the presence of a base, followed by acidification. A process for the production of a hydrazone aldehyde, which comprises contacting a hydrazine and glyoxal, is also described.

Abstract: The present invention provides novel compounds of the formula I and II for the treatment of non-insulin dependent diabetes mellitius (NIDDM) and a new use of known compounds for this purpose.

Abstract: The present invention relates to compounds represented by the formula [I] and salts thereof, wherein R.sup.1 and R.sup.5 each represents carboxyl, phosphonic or a derivative thereof; R.sup.2 represents hydrogen, lower alkyl, (substituted) phenyl lower alkyl, lower alkoxy or (substituted) phenyl lower alkoxy; R.sup.3 represents lower alkyl or (substituted) phenyl lower alkyl; and R.sup.4 represents a group represented by the formula [XI], [XII] or [XIII]. The compounds of the present invention have endopeptidase 24.11 inhibitory activity and are useful for treating cardiovascular diseases such as heart failure and hypertension, renal diseases such as renal failure, gastroenteric disorders such as diarrhea and hyperchlorhydria, endocrine and metabolic diseases such as obesity, and autoimmune diseases such as rheumatic disease, and for mitigating myosalgia, migraine, etc.

Abstract: The present invention provides a chemically modified form of hemoglobin that is stabilized and can efficiently bind and release oxygen. In addition the chemically modified hemoglobin may be polymerized to increase its molecular weight and increase its stability so that it will have a longer half life in the circulatory system and may be used as a stable oxygen transport mediator which is useful as the basis of a blood substitute.

Abstract: The present invention provides an acetate ester compound of formula (III), ##STR1## a process for synthesizing compound (III), and a process for using that compound to prepare a pyrazolone compound, where the substituent definitions are as defined in the Summary of the Invention.

Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.

Abstract: The present application describes m-amidino phenyl analogs of formula I: ##STR1## wherein D can be amidino and E can be phenyl, which are useful as inhibitors of factor Xa.

Abstract: The invention relates to new competitive tripeptide inhibitors of trypsin-like serine proteases, their synthesis, pharmaceutical compositions containing the compounds as active ingredients, and the use of the compounds as thrombin inhibitors, anticoagulants and antiinflammatory inhibitors for prophylaxis and treatment of related diseases.

Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.

Abstract: Aminophenol derivatives represented by the following formula (1): ##STR1## wherein X is O or S; A is alkylene, R.sup.1 is phenyl, etc., R.sup.2 and R.sup.3 are H or alkyl; R.sup.4 is substituted carbamoylalkyl, etc.; R.sup.5 is substituted amino, etc.; their salts, and optical isomers of the derivatives and salts. Also disclosed are gastrin receptor antagonists, cholecystokinin receptor antagonists, and medicines for digestive diseases. The compounds have strong binding inhibition against gastrin receptor or CCK-A receptor and also they have higher selectivity to either group of CCK-A receptor or gastrin receptor, and therefore, the compounds are useful for preventing and treating gastrointestinal diseases including peptic ulcers as well as central nervous system diseases.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: The present invention related to compounds represented by the following formula (I) and salts thereof, ##STR1## wherein R.sup.1 and R.sup.4 each represents a carboxyl or a carboxyl which is converted into an ester, an amide or hydroxamic acid; R.sup.2 represents a lower alkyl or a phenyl-lower alkyl; R.sup.3 represents a hydrogen atom, a lower alkyl, an amino-lower alkyl, a lower alkylamino-lower alkyl, a hydroxy-lower alkyl, a mercapto-lower alkyl, a carboxy-lower alkyl, a lower alkoxycarbonyl-lower alkyl, an imidazolyl-lower alkyl, an indolyl-lower alkyl, a (substituted) phenyl group, a (substituted) phenyl-lower alkyl group, a (substituted) naphthyl group, or a (substituted) naphtyl-lower group. The compounds of the present invention have inhibitory effects on endopeptidase 24.

Abstract: Substituted amidinonaphthyl ester compounds effective for treatment of thrombosis are represented by the following formula (I) and pharmaceutically acceptable acid addition salts thereof: ##STR1## wherein R.sub.1 represents (4,5-dihydro-1H-imidazol-2-yl)amino group, (4,5-dihydro-1,3-thiazol-2-yl)amino group, amidino group, morpholinomethyl group, nitro group, amino group, dimethylamino group, ##STR2## R.sub.3 represents hydrogen, methoxy group, hydroxyl group, acetylamino group, morpholino group, piperidino group, 1-pyrrolidinyl group or dimethylamino group,m represents 0-4,R.sub.4 represents hydrogen or methyl group,R.sub.2 represents NH.sub.2 CO(CH.sub.2).sub.n --, 2-(carbamoyl)vinyl group or R.sub.5 OOC(CH.sub.2).sub.n --,R.sub.5 represents dimethylcarbamoylmethyl group, hydrogen or lower alkyl group, andn represents 0-2.

Abstract: There is provided a 3-(3-aryloxyphenyl)-1-(substituted methyl)-s-triazine-2,4,6-oxo or thiotrione compound having the structural formula I ##STR1## Further provided are a composition and a method comprising that compound for the control of undesirable plant species.

Abstract: Boron compound completing reagents, intermediate reagents of those reagents and methods of synthesizing these reagents. These reagents, including those shown as General Formula CII may be used, after further reactions described herein, to complex with boronic compounds, such as phenylboronic acid or derivatives thereof. ##STR1## In one embodiment, group Z comprises a spacer selected from a saturated or unsaturated chain up to about 0 to 6 carbon equivalents in length, an unbranched saturated or unsaturated chain of from about 6 to 18 carbon equivalents in length with at least one of intermediate amide and disulfide moieties, and a polyethylene glycol chain of from 3 to 12 carbon equivalents in length; group R.sub.2 is one of an alkyl and a methylene with an electronegative moiety; and BAS is a biologically active species.

Abstract: Compounds of formula (I) and salts, esters and amides thereof, wherein R.sup.1 is a C.sub.1-6 straight or branched chain alkyl group, a C.sub.3-6 cycloalkyl group, a thiol group optionally substituted by a C.sub.1-6 alkyl group, or an amino group optionally substituted by one or two alkyl or alkenyl groups; R.sup.2 is H, C.sub.1-7 straight or branched chain alkyl, C.sub.3-6 cycloalkyl, C.sub.2-7 alkenyl or benzyl; A is a 5 or 6 membered aromatic carbocyclic or heterocyclic ring which may optionally be substituted by one or more suitable substituents such as C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, halo, nitro, cyano, trifluoro C.sub.1-6 alkyl, amino, C.sub.1-6 alkylamino or di C.sub.1-6 alkylamino; r is 0, 1 or 2; their use in medicine and in particular for conditions requiring inhibition of the NO Synthase enzyme, pharmaceutical formulations and processes for the preparation thereof are disclosed.

Abstract: Boron compound complexing reagents, intermediate reagents of those reagents, and methods of synthesizing these reagents are disclosed. These reagents, including those shown as General Formula II may be used, after further reactions described herein, to complex with boronic compounds, such as phenylboronic acid or derivatives thereof. ##STR1## In one embodiment, group Z comprises a spacer selected from a saturated or unsaturated chain of up to about 6 carbon equivalents in length, an unbranched saturated or unsaturated chain from about 6 to 18 carbon equivalents in length with at least one intermediate amide or disulfide moieties, and a polyethylene glycol chain of from about 3 to 12 carbon equivalents in length; group R.sub.2 is one of an alkyl and a methylene group with an electronegative moiety; and BAS is a biologically active species.

Abstract: Disclosed herein are substituted vinylurea derivatives represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.3 are independently a phenyl group which may be substituted, R.sup.2 is a phenyl group which may be substituted, or a cycloalkyl group, and wave lines mean that the bonding state may be either E or Z, with the proviso that the cases where R.sup.1, R.sup.2 and R.sup.3 are unsubstituted phenyl groups, and where R.sup.1 and R.sup.2 are unsubstituted phenyl groups and R.sup.3 is a 4-ethoxyphenyl group are excluded, or salt thereof, and medicines comprising such a derivative as an active ingredient as well as a method of preventing and treating arteriosclerosis with such a medicine. The derivatives or salts thereof selectively and strongly inhibit ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.

Abstract: Disclosed are a phenol compound represented by the formula (1): ##STR1## wherein R.sup.0 represents H, alkyl or alkyloxy; R.sup.1 represents alkyl; R.sup.2 represents alkyl or alkyloxy; OR.sup.3 represents OH; R.sup.4 represents H, lower alkyl or acyl, each of the above substituents may be substituted; W represents O, S or NR.sup.7 ; where R.sup.7 represents H, alkyl, aryl, OH or alkyloxy, a group of the formula (2): ##STR2## represents an amino which may be mono- or di-substituted or heterocyclic group containing N atom,or a pharmaceutically acceptable salt thereof, and a process for preparing the same.

Abstract: Boron compound complexing reagents and methods of synthesizing these reagents are disclosed. These reagents, including those shown as General Formula I and General Formula II may be used, after further reactions described herein, to complex with boronic compounds, such as phenylboronic acid or derivatives thereof.

Abstract: Carbamates of the formula I ##STR1## where the substituents have the following meanings: Z is methoxy, NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2, CH.sub.3, C.sub.2 H.sub.5, CF.sub.3 or CCl.sub.3,X and Y are identical or different and each is hydrogen, F, Cl, Br, CF.sub.3, CN, NO.sub.2, alkoxy, alkenyloxy, alkynyloxy, alkyl, alkenyl or alkynyl or may be condensed together to form a substituted or unsubstituted aromatic or heteroaromatic, alicyclic or heterocyclic, partially or completely hydrogenated ring,R.sup.1 may also be substituted or unsubstituted and is O-alkyl, O-alkenyl, O-alkynyl, O-cycloalkyl, O-cycloalkenyl or O--CO.sub.2 -alkyl,A is --O--, --S--, --CR.sup.2 .dbd.CR.sup.3 --, CHR.sup.2 --O--, --CHR.sup.2 --S--, --CHR.sup.2 --O--N.dbd.C(R.sup.4)--, --CR.sup.2 .dbd.N--O--, --O--N.dbd.C(R.sup.4)--, --C.tbd.C--, --CHR.sup.2 --CHR.sup.3 --, --CHR.sup.2 --O--CO--, --O--CHR.sup.

Abstract: The invention discloses a novel process for the preparation of a compound of formula II ##STR1## wherein R.sub.1 is C.sub.1-5 alkyl,R.sub.2 is hydrogen or C.sub.1-5 alkyl, andR.sub.3 is optionally substituted phenyl,comprising the reaction of a 4-hydroxypyrazole of formula III ##STR2## wherein R.sub.1 and R.sub.2 are as defined for formula II, with a benzylhalide of formula IVHal--CH.sub.2 --R.sub.3 (IV)wherein Hal is halogen, preferably bromine or chlorine, and R.sub.3 is as defined for formula II, in the presence of a base. The invention further comprises a novel process for the preparation of the 4-hydroxypyrazole of formula III. The compounds of formulae II and III are intermediates for highly effective systemic fungicides of the class of pyrazolyl acetic acid derivatives.

Abstract: Boron compound complexing reagents, intermediate reagents of those reagents and methods of synthesizing these reagents are disclosed. These reagents, including those shown as General Formula I and General Formula II may be used, after further reactions described herein, to complex with boronic compounds, such as phenylboronic acid or derivatives thereof.

Abstract: The present invention provides novel highly branched macromolecule polymers that have highly controlled molecular architectures, and having the formula: ##STR1## wherein R.sub.4, R.sub.5, and R.sub.6 are defined herein.

Abstract: The present invention relates to a class of compounds represented by the Formula I ##STR1## or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the .alpha..sub.v .beta..sub.3 integrin.

Abstract: The present invention relates to a class of compounds represented by the Formula I ##STR1## or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the .alpha..sub.v .beta..sub.3 integrin.

Abstract: Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.

Abstract: The invention concerns acid derivatives of formula IR.sup.1 --CON(R.sup.2)--N(R.sup.3)CO--X.sup.1 --Q--X.sup.2 --G(I)and pharmaceutically acceptable metabolically labile esters or amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.1, R.sup.2, R.sup.3, X.sup.1, Q, X.sup.2 and G have the meanings given in the specification. The invention also concerns processes for the preparation of the acid derivatives of formula I, pharmaceutical compositions containing them their use as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa.

Abstract: A compound of the formula (I): ##STR1## wherein R.sub.1 is a hydrogen atom or lower alkyl; R.sub.2 is a lower alkoxy, lower alkylamino, lower cycloalkyl, optionally substituted phenyl or optionally substituted heterocyclic group; R.sub.3 is an optionally substituted phenyl; R.sub.4 is an optionally substituted phenyl, optionally substituted cycloalkyl, optionally substituted alkyl or optionally substituted heterocyclic group, or a pharmaceutically acceptable salt thereof, which has a high affinity for gastrin receptors and/or CCK-B receptors but not for CCK-A receptors, and is useful for treating diseases associated with gastrin receptors and/or CCK-B receptors without inducing the side effects associated with CCK-A receptors.

Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.

Abstract: A compound which comprises a prodrug of a protein tyrosine kinase inhibitor (PTKi) linked to a protecting group which is capable of being cleaved from the compound to release the PTKi, said PTKi prodrugs including tyrphostins, of formula (I), ##STR1## where X represents C, N or a group N.fwdarw.O, n is 1 to 3; each group R.sup.1, which may be the same or different is H, OH, mercapto, carboxy, formyl, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, carboxyC.sub.1-4 alkyl, carboxyC.sub.2-4 alkenyl, C.sub.1-4 alkylsulphoxy, halo, nitro, amino, C.sub.1-4 alkylamino, or C.sub.1-4 dialkylamino, or when n is 2 or 3 two R.sup.1 groups may together form a methylenedioxy or ethylenedioxy group; R.sup.2 is H, OH, C.sub.1-4 alkyl or together with position 2 of the ring to which the group(s) R.sup.1 is (are) attached forms a 5 or 6 membered aliphatic or heterocyclic ring, optionally containing a ketone group; and R.sup.3 is cyano, carboxy, carbamoyl, thiocarbamoyl, C(O)HNCH.sub.2 CN, C(NH.sub.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: Phthalazinedione compounds and pharmaceutical compositions are described. The compositions are useful in treating human or animal patients to alleviate or cure disease or disease symptoms caused by nuclear ADP-ribosyl and similar transferases.

Abstract: The invention relates to bicyclo?3.3.0!octane compounds of formula I, ##STR1## wherein the variable are defined in this specification, as well as their enantiomers, and their salts with physiologically compatible bases. .alpha.-, .beta.-, or .tau.-Cyclodextrin clathrates of the compounds and the compounds encapsulated with liposomes are also included. The invention is further directed to processes for production of the compounds and their pharmaceutical use.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.