Abstract: Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented.

Abstract: The present invention relates to the use of creatine compounds for treating or preventing a metabolic disorder related to body weight control such as obesity, and it's associated diseases in a patient experiencing said disorder. The creatine compounds which can be used in the present method include (1) analogues of creatine which can act as substrates or substrate analogues for the enzyme creatine kinase; (2) compounds which can act as inhibitors of creatine kinase; (3) compounds which can modulate the creatine transporter (4) N-phosphocreatine analogues bearing transferable or non-transferable moieties which mimic the N-phosphoryl group. (5) compounds which modify the association of creatine kinase with other cellular components.

Abstract: The invention concerns combinations of alpha adrenergic agents such as brimonidine and its derivatives as represented by formula (I) below 1

Abstract: The present invention relates to acylguanidine derivatives of the formula I in which R1, R2, R4, Ar, X and n have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of the formula I are valuable pharmacologically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion. They inhibit, for example, bone resorption by osteoclasts and are suitable for the therapy and prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example osteoporosis. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceutical preparations, and pharmaceutical preparations comprising them.

Abstract: A compound selected from the group consisting of a compound of the formula wherein the substituents are defined as set forth in the specification and its salts with non-toxic pharmaceutically acceptable acids and bases useful for treating loss of bone matrix.

Abstract: The present invention relates to compounds of formula (I): wherein: Ar is an optionally substituted aromatic or heteroaromatic group, R1 is H, C1-6alkyl, CF3, phenyl, benzyl, carboC1-6alkoxy, carbamoyl, or methyl(N—C1-6alkylcarbamoyl) R2 is H, C1-6alkyl, aminoC1-6alkyl, hydroxyC1-6alkyl, (mono- or di- C1-6alkyl)aminoC1-6alkyl, (aminoC1-3alkylphenyl)C1-3alkyl, amidinothio C1-6alkyl, R3 is H or C1-6alkoxy, R4 is H or together with R2, forms an annulated ring which may be substituted by hydroxyC1-3alkyl or amidinothio C1-3alkyl, or aminoC1-3alkyl; and pharmaceutically acceptable salts thereof; and the use of such compounds in medical therapies.

Abstract: Methods of treating glaucoma or elevated pressure and other diseases with reduced side effects by treating a mammal in need thereof an agonist of the alpha 2B or alpha 2B/2C adrenergic receptor(s). Also described are compounds having such selective agonist activity.

Abstract: A compound of formula I in which: ring A is one of the five alternative multi-cyclic rings as shown wherein a dotted line adjacent to a bond indicates that a single bond or a double bond may be present at that position; X is nitrogen, oxygen or sulfur; R is hydrogen, lower straight or branched chain alkyl of 1 to 6 carbon atoms, or lower straight or branched chain alkenyl of 2 to 6 carbon atoms, a cycloaliphatic ring of 3 to 6 carbon atoms, phenyl optionally mono- or di-substituted with hydroxy, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 2 carbon atoms, or methylenedioxyphenyl; or a stereoisomer, or a pharmaceutically acceptable salt thereof. These compounds have &agr;2 receptor blocking activity and hence find use in the treatment or palliation of elevated intraocular pressure, non insulin-dependent diabetes, male impotence and obesity.

Abstract: The invention concerns combinations of alpha adrenergic agents such as brimonidine and its derivatives as represented by formula (I) below wherein each Y is independently selected from the group consisting of N, N—CH3, O, S and C—R1; R1 is hydrogen, lower alkyl or oxo; R2, R3 and R4 are independently selected from the group consisting of hydrogen, halogen, lower alkyl and lower alkenyl; n is an integer from 1 to 3; and a broken line beside a solid line indicates either a single or a double bond with the proviso that when n=1, both bonds from Y to C—R1 cannot be double bonds, and prostaglandins known in the art to cause lowering of intraocular pressure which are useful in compositions, methods of treatment and articles of manufacture for the treatment of glaucoma and alleviation of elevated intraocular pressure and providing neuroprotection.

Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

Abstract: Compounds of the formula wherein the substituents are as defined in the application and their pharmaceutically acceptable acid and base salts thereof which are useful for preventing loss of bone matrix.

Abstract: This invention relates to herbicidal compounds of formula (I), methods of making such herbicidal compounds and methods of using such herbicidal compounds. It has been found that compounds of formula (I) are useful as pre-emergent and post-emergent herbicides. Formula (I) is as follows: where Q, X, Y, n, and R are as described herein. This invention is also directed to intermediates used in the preparation of such herbicidal compounds.

Abstract: Novel compounds of Formula 1 are useful to treat disorders responsive to openers of the large conductance calcium-activated potassium channels: wherein “Het” is one of a select group of heterocyclic moieties; Z is independently for each occurrence selected from O or S; Ra, Rb and Rc each are independently selected from hydrogen, halogen, OH, CF3, NO2, or provided Rc is not hydrogen; and when Ra and Rb are hydrogen, Rc may be a heterocyclic moiety selected from the group consisting of imidazol-1-yl, morpholinomethyl, N-methylimidazol-2-yl, and pyridin-2-yl; Rd and Re each are independently selected from hydrogen, halogen, CF3, NO2 or imidazol-1-yl; m, n and p each are independently selected from an integer of 0 or 1; and Rf and Rg each are independently hydrogen; C1-4 alkyl; or Rf and Rg, taken together with the nitrogen atom to which they are attached, is a heterocyclic moiety selected from the group consisting of N-methylpiperazine, morpholine, thiomorpholine,

Abstract: The invention relates to new diphenyl-substituted 5-ring heterocycles of general formula (I) wherein A, X and the groups R1, R2, R3, R4 and R5 are defined as in the claims, processes for preparing them and their use as pharmaceutical compositions.

Abstract: Disclosed are biocidal compositions comprising mixtures of formaldehyde-releasing imidazolidines, such as 1,3-dimethylol-5,3-dimethylhydantoin, and 3-isothiazolones stabilized with low levels of copper salts.

Abstract: Use of agonists and antagonists of the nicotinergic acetylcholine receptors of insects for the non-systemic control of parasitic insects, such as fleas, lice and flies, on humans and on animals.

Abstract: The present invention is directed to a foodstuff or a dietary supplement that includes biotin at a concentration of at least 0.2 mg/400 kcal and one or more B vitamins at a total concentration of biotin plus B vitamins of at least 33.2 mg/400 kcal. The present invention is also directed to the method of using and preparing the foodstuff or dietary supplement.

Abstract: The invention provides the use of an AT1 receptor antagonist, or a pharmaceutical salt thereof, for producing a pharmaceutical preparation for the stimulation of apoptosis and for the treatment of pathological symptoms which are substantially reduced, halted or prevented by apoptosis, and also corresponding pharmaceutical preparations.

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: Sympathetically maintained peripheral neuropathic pain syndromes are relieved by topically applying, to the affected region of a patient suffering from such pain, a pain relieving amount of an aqueous gel comprising clonidine, a water-gelling amount of a pharmaceutically acceptable gelling agent and having a physiologically tolerable pH value. Pain relief was achieved with applied amounts of clonidine in the range of about 2 milligrams per day to about 6 mg per day.

Abstract: This invention relates to a method for selecting PDE IV inhibitors which have a salutory therapeutic index, and to compounds having these properties.

Abstract: Combination of chemical compounds used as a medicament intended to suppress the dependence of individuals to opioids, the combination comprising a laxative or enema of irrigation, repeated doses of alpha-adrenergic agents, anticmetic agents, gastric protectors, optionally inhibitors of the proton pump, an anxiolytic compound, anaesthetic sleep inducing agent and determined doses of an opioid antagonist compound, such as nazalone or naltrexone.

Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors .alpha.v.beta.3, .alpha.v.beta.5 and/or .alpha.v.beta.6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, and tumor growth and metastasis.

Abstract: Compounds of the formula I ##STR1## and the pharmaceutically tolerated salts thereof, are described. A process for their preparation and their use as medicaments in cardiovascular diseases are also described.

Abstract: The invention relates to 2-mercaptoimidazole derivatives substituted in the 4(or 5)-position.These 2-mercaptoimidazole derivatives are of the general formula (I) below: ##STR1## wherein: R.sub.1, R.sub.2, R.sub.5, R.sub.7 and R.sub.8 are hydrogen, a lower alkyl, an aralkyl or a substituted aralkyl, wherein at least one of R.sub.1 and R.sub.2 is hydrogen;R.sub.3 is (CH.sub.2).sub.n COR.sub.4, --(CH.sub.2).sub.n N.sup.+ (R.sub.5 R.sub.6 R.sub.7).X.sup.- or --CH.sub.2 CH(COR.sub.4)N.sup.+ (R.sub.5 R.sub.6 R.sub.7).X.sup.- ;R.sub.4 is OR.sub.8, --NHR.sub.5, --.alpha.-amino acid,--NHCH.sub.2 CH.sub.2 SO.sub.3.sup.-.Y.sup.+, --NHCH.sub.2 CH.sub.2 CO.sub.2.sup.- Y.sup.+, --OCH.sub.2 CH.sub.2 N.sup.+ (CH.sub.3).sub.3.X.sup.- ; ##STR2## n=1 or 2; X.sup.31 is an anion of an acid acceptable in cosmetics, pharmaceuticals or foodstuffs; andY.sup.+ is a cation of a base acceptable in cosmetics, pharmaceuticals or foodstuffs.

Abstract: The invention provides a method of treating heart failure. The method comprises administering a positive inotropic agent and a .beta.-adrenergic receptor antagonist in a specific manner.

Abstract: The present invention relates to the use of creatine compounds for treating or preventing a metabolic disorder related to body weight control such as obesity, and it's associated diseases in a patient experiencing said disorder. The creatine compounds which can be used in the present method include (1) analogues of creatine which can act as substrates or substrate analogues for the enzyme creatine kinase; (2) compounds which can act as inhibitors of creatine kinase; (3) compounds which can modulate the creatine transporter (4) N-phosphocreatine analogues bearing transferable or non-transferable moieties which mimic the N-phosphoryl group. (5) compounds which modify the association of creatine kinase with other cellular components.

Abstract: A process for the treatment of anxiety and tension, which comprises administering to a patient in need therefor an anxiolytically effective amount of a compound of the formula ##STR1## wherein X is hydrogen, a C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl residue, or halogen; R.sup.1 and R.sup.2 are independently of each other a C.sub.1-4 alkyl, cycloalkyl, C.sub.2-4 hydroxyalkyl, or heteroalkyl residue, or R.sup.1 and R.sup.2 together form a C.sub.2-6 alkylene residue in which one --CH.sub.2 -- group can be replaced by oxygen, nitrogen or sulfur; n is 0 or 1, and m is 0 or a cardinal number from 1-5, or a pharmaceutically acceptable salt of the compound.

Abstract: The present invention relates to salts of imidazoline derivatives of the formula I ##STR1## in which R represents hydrogen or alkyl,Y represents nitro or cyano,W represents an optionally substituted 5- or 6-membered heterocyclic radical andZ represents one equivalent of an alkali metal or alkaline earth metal or of an [NR.sup.1 R.sup.2 R.sup.3 R.sup.4 ] grouping, whereinR.sup.1, R.sup.2, R.sup.3 and R.sup.4 are identical or different and represent hydrogen, alkyl, optionally substituted cycloalkyl or optionally substituted benzyl,and to their preparation and their use as agents for controlling pests.

Abstract: Stable solid forms of preservative and embalming compositions are described which can be prepared by adding a sufficient amount of a chemical or chemicals containing at least one polar group capable of forming hydrogen and Van der Waal bonds with the reactive moieties of the aldehydes and antimicrobial agents in the preservative and embalming compositions. The amount of polar chemical(s) necessary to stabilize the reactive aldehydes and antimicrobial compounds/agents is based on a molar ratio of (i) polar groups in the stabilizing chemicals to (ii) reactive groups in the active preservative ingredient of at least 0.8.

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

Abstract: The present invention relates to a thrombolytic agent capable of being orally administered, said agent comprising 6-amidino-2-naphthyl 4-?(4,5-dihydro-1H-imidazole-2-yl)amino!benzoate or a pharmaceutically acceptable acid addition salt thereof.

Abstract: The present invention relates to a novel arylsulfonylimidazolone derivative represented by the following formula (I) which shows a superior antineoplastic activity in contrast to the known sulfonylurea antitumor agents as well as little side effect: ##STR1## and its pharmaceutically acceptable salt and stereoisomer, in which ----, R.sub.1, and R.sub.2 are as defined in the specification.

Abstract: A compound of the formula: ##STR1## is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

Abstract: Carboxyalkyl heterocyclic derivatives, pharmaceutically acceptable salts thereof, and therapeutic agents containing said compounds as an effective component are useful pharmaceuticals for the treatment of diabetic complications such as diabetic neuropathy, diabetic cataracts and retinopathy, diabetic nephropathy, diabetic dermopathy, and other diabetic microangiopathy. The compounds of the present invention are represented by the following general formula (A): ##STR1## The compounds of the present invention exhibit excellent inhibitory action towards aldose reductase with a high enzyme selectivity. Accordingly, they are useful as drugs for the therapy and prevention of various types of diabetic complications without substantially inhibiting aldehyde reductase.

Abstract: The invention relates to the use of inhibitors of phosphodiesterase IV for the modulation of the motility and peristalsis of the hollow organs of the urogenital and gastrointestinal tract.

Abstract: The invention provides a method of preventing or treating malaria comprising administering a therapeutically effective amount of serotonin receptor ligand to reduce the pathological consequences of malaria infection in a patient, said serotonin receptor ligand characterized by an ability to displace an identifying ligand which defines the serotonin receptor subtype 5HT1a or 5HT2/5HT1c.In addition, the invention provides a method of identifying a serotonin receptor ligand capable of reducing the pathological consequences of malarial infection in a patient comprising the step of sequentially assaying potential ligands to identify a ligand characterized by an ability to displace an identifying ligand which defines the serotonin receptor subtype 5HT1a or 5HT2/5HT1c.

Abstract: Compounds having anticonsulive activity, of the formula 1 ##STR1## in which X is hydrogen, a C.sub.1-4 -alkyl, C.sub.1-4 alkoxy, trifluoromethyl, or halogen residue, R.sup.1 and R.sup.2 are independently of each other C.sub.1-4 -alkyl, C.sub.2-4 hydroxyalkyl, cycloalkyl or heteroalkyl, or R.sup.1 and R.sup.2 are together a C.sub.2-6 alkylene reside in which a--CH.sub.2 --group is optionally replaced by oxygen, nitrogen or sulfur, m is 0 or 1, and n is 0 or a cardinal number from 1 to 5, and their pharmaceutically acceptable salts. The application also relates to a process for making the compound of formula (I).

Abstract: N,N-di(aryl) cyclic urea derivatives, such as the compounds of the following formula: ##STR1## wherein R.sup.1 is --C(NH)NH.sub.2, --C(NH)N(H)OR.sup.11, --C(NH)N(H)C(O)R.sup.9, or --C(NH)N(H)C(O)OR.sup.11 ;R.sup.2 and R.sup.3 are independently hydrogen, halo, lower alkyl, lower haloalkyl, aryl, --OR.sup.11, --C(O)OR.sup.11, --C(O)N(R.sup.11)R.sup.12, --N(R.sup.11)R.sup.12, --N(H)C(O)R.sup.11, or --N(H)S(O).sub.2 R.sup.11 ;R.sup.4 is halo, lower haloalkyl, imidazolyl, --C(NH)NH.sub.2, --C(NH)NHOR.sup.11, --C(NH)N(H)C(O)R.sup.9, --C(NH)N(H)C(O)OR.sup.11, --OR.sup.11, --C(O)R.sup.13, --(CH.sub.2).sub.n C(O)OR.sup.11 (where n is 0 to 6), --C(O)N(R.sup.11)R.sup.12, or --N(R.sup.11)R.sup.12 ;R.sup.7 and R.sup.8 are independently hydrogen, lower alkyl, lower haloalkyl, 4-pyridinyl, --C(O)OR.sup.11, --C(O)N(R.sup.11)R.sup.12, or aryl (optionally substituted by one or more substituents selected from the group consisting of halo, hydroxy, lower alkyl, lower haloalkyl, lower alkoxy and --N(R.sup.11)R.sup.12);R.sup.

Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the group R6 represents a variety of possible substituent groups on the carbon chain between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12 ; and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.

Abstract: Methods are provided for treating sepsis/endotoxin-induced acute renal failure, and renal vasoconstriction and catecholamine-induced renal and mesenteric vasconstriction by administering to a patient a therapeutically effective amount of a composition comprising at least one drug with Type IV phosphodiesterase inhibiting activity or any combination thereof and a pharmaceutically acceptable carrier.

Abstract: The present invention is a method of preventing or ameliorating the episodic recurrence of MS, comprising administering an effective amount of selective phosphodiesterase inhibitors of Type IV, e.g., Rolipram, e.g., wherein the severity of the episodic recurrences is ameliorated or the time period between episodes is lengthened.

Abstract: Herein is described an ocular composition comprising an ocular decongestant such as phenylephrine and certain labdane derivatives which are intraocular pressure lowering agents. The composition not only markedly reduces the ocular reddening otherwise produced by such labdane compounds, but also unexpectedly prolongs and frequently potentiates their intraocular pressure lowering effect. Both of these effects are very beneficial to the use of such labdanes for the treatment of glaucoma.Also described herein is an ocular composition comprising para-aminoclonidine (an .alpha..sub.2 -adrenoreceptor agonist) and certain labdane derivatives mentioned above. The composition reduces the ocular reddening and lacrimation, and also potentiates the intraocular pressure lowering effect.

Abstract: The present invention contemplates a compound defined by the following formula: ##STR1## that inhibits the binding between the VLA-4 and the fibronectin CS-1 compound. Pharmaceutical compositions containing a contemplated compound and methods for treating immunoinflammatory conditions using the compound are also disclosed.

Abstract: Combinations of at least one clonidine derivative and at least one prostaglandin are used to treat glaucoma and ocular hypertension without some of the side effects typically associated with topical administration of prostaglandins.

Abstract: This invention provides methods for intraspinal administration of therapeutically-effective amounts of clonidine for alleviating acute and chronic pain.

Abstract: 3-Substituted 1-arylindole compounds are provided having general formula (I) ##STR1## wherein Ar is an optionally substituted aryl group; X represents a divalent hydrocarbon group, methyleneoxy or -thioxo; R.sup.1 -R.sup.4 are hydrogen or other substituents; R.sup.5 is hydrogen, alkyl, alkenyl, etc.; R.sup.6 and R.sup.7 are independently hydrogen, alkyl, alkenyl, etc.; R.sup.8 is alkyl, alkenyl or R.sup.8 represents a group of formula 1a or 1b; wherein n is an integer from 2-8; W is O or S; U is N or CH; Z is (CH.sub.2).sub.m, m being 2 or 3, 1,2-phenylene optionally substituted with halogen or trifluoromethyl, CH.dbd.CH, COCH.sub.2 or CSCH.sub.2 ; V is O, S, CH.sub.2 or NR.sup.10, wherein R.sup.10 is hydrogen, alkyl, alkenyl, cycloalkyl, etc.; U.sup.1 is O, S, CH.sub.2 or a group NR.sup.11, wherein R.sup.11 is hydrogen, alkyl, alkenyl, etc.; and V.sup.1 is NR.sup.12 R.sup.13, OR.sup.14, SR.sup.15 or CR.sup.16 R.sup.17 R.sup.18, where R.sup.12 -R.sup.18 are as the R.sup.10 substituents; R.sup.

Abstract: The present invention contemplates a compound defined by the following formula: ##STR1## that inhibits the binding between the VLA-4 and the fibronectin CS-1 compound. Pharmaceutical compositions containing a contemplated compound and methods for treating immunoinflammatory conditions using the compound are also disclosed.

Abstract: The present invention relates to substituted cyclic ureas and analogs thereof of formula (I): ##STR1## wherein, T is selected from: --N(R.sup.22)C(.dbd.Z)N(R.sup.23)--; --N(R.sup.22)C(.dbd.Z)C(.dbd.Z)N(R.sup.23)--; --N(R.sup.22)S(.dbd.Z')N(R.sup.23)--; --N(R.sup.22)S(.dbd.Z').sub.2 N(R.sup.23)--; or --N(R.sup.22)P(.dbd.O)(R.sup.24a)N(R.sup.23)--;Z is O, S, NR.sup.24 ; and,Z' is O or NR.sup.24 ;or pharmaceutically acceptable salt forms or prodrugs thereof, which are useful as retroviral protease inhibitors, and to pharmaceutical compositions comprising such compounds and methods of using the same for treating viral infection.

Abstract: This invention relates to compounds of formula ##STR1## or a salt, or metabolically labile ester thereof wherein R represents a group selected from halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, hydroxy, trifluoromethyl, trifluoromethoxy, nitro, cyano, SO.sub.2 R.sub.2 or COR.sub.2 wherein R.sub.2 represents hydroxy, methoxy, amino, alkylamino, or dialkylamino; m is zero or an integer 1 or 2;R.sub.1 represents a cycloalkyl, bridged cycloalkyl, heteroaryl, bridged heterocyclic or optionally substituted phenyl or fused bicyclic carbocylic group;A represents a C.sub.1-4 alkylene chain or the chain (CH.sub.2).sub.p Y(CH.sub.2).sub.q wherein Y is O, S(O)n or NR.sub.3 and which chains may be substituted by one or two groups selected from C.sub.1-6 alkyl optionally substituted by hydroxy, amino, alkylamino or dialkylamino, or which chains may be substituted by the group .dbd.O;R.sub.