Abstract: The present invention relates to a process of making a compound of formula (I): Wherein, R1, R2, R4 and X are as defined herein.

Abstract: The invention relates to a method for reducing the concentration of amines and salts thereof, wherein the amines have the general chemical formula I R1R2R3N and the salts have the formula II R1R2R3N—H, wherein the amines and salts thereof exist in aqueous solution or aqueous suspension and are brought into contact with clinoptilolitic or clinoptilolite-containing mixtures. The method itself is suitable for use in food preparation and in the manufacture of foods. The inventive idea of reducing the concentration of amines and salts thereof is also useful in the manufacture of medical products for absorbing and for removing amines from the intestinal tract or the skin area of humans and animals.

Abstract: Compounds of formula (I) or a pharmaceutically acceptable ester, amide, carbamate or salt thereof, including a salt of such an ester, amide or carbamate in which R1 to R9 have meanings as defined in the Specification, are useful as estrogen receptor ligands.

Abstract: The invention relates to the use of at least one compound selected from the class of the sulphoximines for enhancing plants' intrinsic defenses and/or for improving plant growth and/or for enhancing the resistance of plants to plant diseases which are caused by fungi, bacteria, viruses, MLOs (mycoplasma-like organisms) and/or RLOs (rickettsia-like organisms), and/or for enhancing the resistance of plants to abiotic stress factors.

Abstract: The present invention relates to a process of making a compound of formula (I): Wherein, R1, R2, R4 and X are as defined herein.

Abstract: The invention provides a method of detecting uracil. The method comprises reacting uracil with a compound represented by the formula (I) in the presence of an oxidant and a base to produce a fluorescent compound represented by the formula (II).

Abstract: This invention relates to a pharmaceutical composition containing 4-[(4-thiazolyl)phenoxyl]alkoxy-benzamidine derivatives expressed by the following formula 1 for the prophylaxis and treatment of osteoporosis and more particularly, to the use of 4-{5-[4-(5-isoproply-2-methyl-1,3-thiazol-4-yl)phenoxyl]pentoxy}-benzamidine or N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxyl]pentoxy}-benzamidine expressed by the following formula 1 as a pharmaceutical composition for the prophylaxis and treatment of osteoporosis.

Abstract: This invention is directed to a compound of formula (I): wherein R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising the compound, intermediates and processes for making said compounds, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma, chronic obstructive pulmonary disease (COPD) and age-related macular degeneration (AMD).

Abstract: A method of treating osteoporosis comprising administering to a subject a composition comprising a compound, 4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}-benzamidine or a salt thereof, is described. A method of inhibiting osteoclast activity and stimulating osteoblast activity in a subject also is described.

Abstract: Novel dioxazine- and oxdiazine-substituted arylamides of the formula (I) in which A1, A2, R1, R2, R3, R4 and R5 are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling pests, and also novel intermediates and processes for their preparation.

Abstract: Compounds of formula I: wherein X, R2, R3, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.

Abstract: The invention relates to compounds having an anti-parasitic, in particular antimalarial activity, characterized in that they correspond to general formula (I) Applications in particular as compounds with anti-parasitic activity.

Abstract: Semiconductor processing compositions comprising amidoxime compounds having two or more amidoxime functional groups and their use in semiconductor processing to remove photoresist, polymeric materials, etching residues and copper oxides from semiconductor substrates, particularly substrates comprising copper, low-k dielectric material, titanium nitride, and/or titanium oxynitride.

Abstract: The invention relates to a method for improving bioavailability of pharmaceutical substances and for allowing the pharmaceutical substances to permeate the blood-brain barrier, the pharmaceutical substances having at least one or more amidine, guanidine, N-hydroxyamidine (amidoxime) or N-hydroxyguanidine functions. The invention also relates to medicaments containing the correspondingly modified pharmaceutical substances.

Abstract: Novel fused ring dicationic anti-protozoan compounds. Representative protozoan species include but are not limited to Trypanosoma brucei rhodesiense (T.b.r.) and Plasmodium falciparum. Prodrugs of these compounds can be used as an oral treatment for malaria and human African trypanosomiasis.

Abstract: The present invention provides a class of chemical compounds useful in the treatment of sickle cell disease, diseases characterized by unwanted or abnormal cell proliferation and for the treatment of ocular disorders such as glaucoma. The active compounds are tri-(aryl or heteroaryl) methane compounds or analogues thereof which further comprise an imine moiety and where the tertiary carbon atom can be replaced with a different atom such as Si, Ge, N or P. The compounds enhance resistance to degradation in a biological medium, inhibit potassium flux in a cell, reduce mammalian cell proliferation, reduce the Gardos channel of erythrocytes, reduce sickle erythrocyte dehydration and/or delay the occurrence of erythrocyte sickling or deformation.

Abstract: This invention relates to a pharmaceutical composition containing 4-[(4-thiazolyl)phenoxyl]alkoxy-benzamidine derivatives expressed by the following formula 1 for the prevention and treatment of osteoporosis and more particularly, to the use of 4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxyl]pentoxy}-benzamidine or N-hydroxy-4-{5-[4-(5-iso-propyl-2-methyl-1,3-thiazol-4-yl)phenoxyl]pentoxy}-benzamidine expressed by the following formula 1, which is known as an antagonist of leukotriene-B4 receptor, as a pharmaceutical composition for the prevention and treatment of osteoporosis. [Formula 1], wherein, R is a hydrogen atom or a hydroxy group.

Abstract: Novel dioxazine- and oxdiazine-substituted arylamides of the formula (I) in which A1, A2, R1, R2, R3, R4 and R5 are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling pests, and also novel intermediates and processes for their preparation.

Abstract: The present invention is directed to amidino heterocyclic compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as to pharmaceutical compositions comprising such compounds and to pharmaceutical methods of treatment comprising administration of such compounds and pharmaceutical compositions.

Abstract: An N-hydroxyformamidine compound of the following formula or a pharmaceutically acceptable salt thereof: wherein R1, A and R are as defined herein. The compounds inhibit 20-HETE-producing enzymes, 20-HETE being involved in the effects of causing microvascular constriction or dilation in major organs (e.g., kidneys, cerebral blood vessels) or of inducing cell proliferation.

Abstract: The present invention relates to the use of amidine compounds in the treatment of amyloid-related diseases. In particular, the invention relates to a method of treating or preventing an amyloid-related disease in a subject comprising administering to the subject a therapeutic amount of an amidine compound.

Abstract: A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof [wherein R1 represents a substituted morpholino group, a substituted piperidino group, a piperazin-1-yl group, a substituted piperazin-1-yl group, a thiomorpholin-1-yl group, a perhydroazepin-1-yl group, a perhydroazocin-1-yl group, a tetrahydropyridin-1-yl group, a pyrrolin-1-yl group, etc.; X represents a nitrogen atom or a group represented by CR5; and R2 to R5 are the same or different and each represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, a trifluoromethyl group or a halogen atom.] There is provided a drug which inhibits an enzyme producing 20-HETE participating in a contracting or dilating action for microvessels and an inducing action for cell proliferation in main organs such as kidney and cerebrovascular vessels.

Abstract: A pharmaceutical composition an inclusion complex and methods for treating patients and preparing said complex disclosed for transmucosal delivery comprising an inclusion complex of (a) alprazolam and (b) a water soluble 2-hydroxypropyl-beta-cyclodextrin, and a pharmaceutically acceptable carrier therefor, wherein all the alprazolam is present in ring-closed form.

Abstract: Novel benzamidoxime derivatives, processes and intermediates for their preparation and their use as fungicides are described. In the context of the present invention, benzamidoxime derivatives are compounds of the formula I where: A is an aryl or hetaryl radical; Y is a straight-chain or branched C1–C4-alkylene group, where one carbon can be replaced by oxygen, nitrogen or sulfur or by a cyclopropyl group; Rn1 are one to five identical or different radicals from the group consisting of: hydrogen, halogen, C1–C6-alkyl, C1–C6-alkoxy, C1–C4-haloalkyl, C1–C4-haloalkoxy, C1–C4-alkylthio, C1–C4-alkoxyalkoxy; R2 is unsubstituted or substituted phenyl-C1–C6-alkyl, thienyl-C1–C4-alkyl, or pyrazolyl-C1–C4-alkyl, Rp3 are one to five identical or different radicals from the group consisting of: hydrogen, halogen, C1–C6-alkyl, C1–C6-alkoxy, C1–C4-haloalkyl, C1–C4-haloalkoxy, C1–C4-alkylthio, C1–C4-alkoxyalkoxy, C1–C6-alkylcarbonyl; n is 0–5; p is, depending on the number of free valencies, 0–4.

Abstract: The invention refers to novel propenecarboxylic acid amidoxime derivatives furthermore N-oxides and/or geometrical isomers and/or optical isomers and/or pharmaceutically suitable acid addition salts and/or quaternary derivatives thereof. The novel compounds are suitable for the treatment of a state connected with oxygen deficit and/or energy deficit, or a disease based on PARP inhibition, especially an autoimmune or neurodegenerative disease, and/or a viral disease, and/or a disease caused by a toxic effect.

Abstract: Novel benzamidoxime derivatives, processes and intermediates for their preparation and their use as fungicides are described. In the context of the present invention, benzamidoxime derivatives are compounds of the formula I where: A is an aryl or hetaryl radical; Y is a straight-chain or branched C1-C4-alkylene group, where one carbon can be replaced by oxygen, nitrogen or sulfur or by a cyclopropyl group; Rn1 are one to five identical or different radicals from the group consisting of: hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-alkylthio, C1-C4-alkoxyalkoxy; R2 is unsubstituted or substituted phenyl-C1-C6-alkyl, thienyl-C1-C4-alkyl, or pyrazolyl-C1-C4-alkyl, Rp3 are one to five identical or different radicals from the group consisting of: hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-alkylthio, C1-C4-alkoxyalkoxy, C1-C6-alkylcarbonyl; n is 0-5; p is, depending on the number of free valencies, 0-4.

Abstract: The present invention provides a pharmaceutical composition comprising N-(3-chloro-4-morpholin-4-yl)phenyl-N′-hydroxyimidoformamidine and sulfobutyl ether &bgr;-cyclodextrin or a salt thereof, wherein sulfobutyl ether &bgr;-cyclodextrin increases the solubility of N-(3-chloro-4-morpholin-4-yl)phenyl-N′-hydroxyimidoformamidine and improves the photostability.

Abstract: This invention relates to a method for producing compounds of the formula (I) or their salts: wherein each of R1 and R2 is hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted alkynyl, unsubstituted or substituted aryl, unsubstituted or substituted heteroaryl, OR3, SR3, COR3, COOR3 or cyano; R1 and R2 may combine together with the adjacent carbon atom of ═CR1R2 to form an unsubstituted or substituted cyclic ring; each of R4 and R5 is hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted alkynyl, unsubstituted or substituted aryl, unsubstituted or substituted heteroaryl, NR6R7, OR8 or SR9; R4 and R5 may combine together with the adjacent skeleton of C/N bond to form a heterocyclic ring; which comprises rearranging compounds of the formula (II) or their salts: wherein R1, R2, R4 and R5 are as defined above.

Abstract: The invention provides triamine derivative melanocortin receptor ligands of the formula: wherein R1 to R8 and n have the meanings provided herein. The invention further provides methods of using the ligands to alter or regulate the activity of a melanocortin receptor.

Abstract: Bis-aryl diamidoxime compounds, such as 2,5-bis[4-hydroxy and 4-O-alkylamidinophenyl]furans, can be prepared from 2,5-bis tri-alkylstannanes via a one step palladium-catalyzed cross reaction. Bis-aryl diamidoxime compounds, such as 2,5-bis[4-hydroxy and 4-O-alkylamidinophenyl]furans, are useful as therapeutic compounds. The disclosed process is scalable, simpler, more economic and more feasible than other presently known methods of preparing 2,5-bis[4-hydroxy and 4-O-alkylamidinophenyl]furans and other bis-aryl diamidoxime compounds.

Abstract: Biguanide and dihydrotriazine derivatives, preferably substituted asymmetrical imidodicarbonimidic diamides derived from hydroxylamines, and compositions containing biguanide and dihydrotriazine derivatives are disclosed. In addition, methods of using the biguanide and dihydrotriazine derivatives, inter alia, as antimicrobial agents and methods of using the dihydrotriazine derivatives in biological assays are disclosed. Methods of making the biguanide and dihydrotriazine derivatives are also disclosed.

Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.

Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.

Abstract: Compounds of the formulae are disclosed. A method of protecting subjects from infections caused by an organism of the group: Plasmodium sp. Mycobacterium sp., P. falciparum, and Pneumocystis carinii by administering to the subjects liable to infections, a prophylactically effective amount of a compound of the foregoing formulae; and a method of reducing the level of infection in subjects caused by the above-listed organism by administering to the subjects an infection reductively effective amount of a compound of the foregoing formulae are also disclosed.

Abstract: A method of increasing expression of a molecular chaperon by a cell and/or enhancing the activity of a molecular chaperon in cells is provided. The method comprises treating a cell that is exposed to a physiological stress which induces expression of a molecular chaperon by the cell with an effective amount of a certain hydroxylamine derivative to increase the stress. Alternatively; an hydroxylamine derivative can be administrated to a cell before it is exposed to a physiological stress which induces expression of a molecular chaperon by the cell. Preferably, the cell to which an hydroxylamine derivative is administered is an eukaryotic cell. The hydroxylamine derivative corresponds to the formulae (I) or (II). The invention also provides novel hydroxyl amine derivatives falling within the scope of the formulae (I) and (II) as well as pharmaceutical and/or cosmetical compositions comprising the said compounds.

Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.

Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: 1

Abstract: The invention refers to novel propenecarboxylic acid amidoxime derivatives furthermore N-oxides and/or geometrical isomers and/or optical isomers and/or pharmaceutically suitable acid addition salts and/or quaternary derivatives thereof. The novel compounds are suitable for the treatment of a state connected with oxygen deficit and/or energy deficit, or a disease based on PARP inhibition, especially an autoimmune or neurodegenerative disease, and/or a viral disease, and/or a disease caused by a toxic effect.

Abstract: Compounds of the formulae 1

Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.

Abstract: Benzamidoxime derivatives of the formula I where R1 is difluoromethyl or trifluoromethyl R2 is hydrogen or fluorine R3 is C1-C4-alkyl which may be substituted by cyano, C1-C4-haloalkyl, C1-C4-alkoxy-C1-C4-alkyl, C3-C6-alkenyl, C3-C6-haloalkenyl, C3-C6-alkynyl, C3-C8-cycloalkyl-C1-C4-alkyl R4 is phenyl-C1-C6-alkyl which may carry one or more substitutents selected from the group consisting of halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy and C1-C4-haloalkoxy on the phenyl ring, or is thienyl-C1-C4-alkyl which may carry one or more substituents selected from the group consisting of halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy and C1-C4-haloalkoxy on the thienyl ring, or is pyrazolyl-C1-C4-alkyl which may carry one or more substituents selected from the group consisting of halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy and C1-C4-haloalkoxy on the pyrazole ring, are prepared, and intermediates for their preparation and their use as fungicides are described.

Abstract: The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula: wherein: A is O, S, or NR4; B is a bond between A and C═Q, or the moiety CR5R6; R4, R5, R5 are independently selected from H or optionally substituted C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alknyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, or heterocyclic groups, or cyclic alkyl constructed by fusing R4 and R5 to from a 5 to 7 membered ring; R1 is selected from H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, substituted alknyl, —COH, or optionally substituted —CO(C1 to C3 alkyl), —CO(aryl), —CO(C1 to C3 alkoxy), or —CO(C1 to C3 aminoalkyl) groups; R2 is selected from H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl groups; R3 is selected from a trisubstitut

Abstract: A method of treating Pneumocystis carinii pneumonia in a subject in need of such treatment is disclosed. The method comprises orally administering to the subject a bis-benzamidoxime, or a pharmaceutically acceptable salt thereof, that is reduced in the subject to produce a benzamidine having anti-P. carinii activity. The method of the present invention may alternatively comprise intravenously administering to the subject an active compound as disclosed herein. Pharmaceutical formulations and active compounds useful in the practice of the present invention are also disclosed.

Abstract: Novel benzamidines, having LTB4-antagonistic activity, of the formula methods for their preparation, their and their use as medicaments.

Abstract: The present invention provides therapeutically useful substituted guanidines of the following Formula: ##STR1## and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.

Abstract: The present invention provides therapeutically useful substituted guanidines of the following Formula: ##STR1## and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.

Abstract: The invention relates to the use of agmatine, in the treatment of acute neurotrauma (such as stroke) and degenerative disorders of the central and peripheral nervous system (such as dementia).The invention further provides novel compounds of general formula I (which are quinuclidine derivatives), formula II (which are norbornane derivatives), formula III (which are adamantane derivatives), and formula IV (which are phenothiazine derivatives): ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, hydroxy, substituted or unsubstituted C.sub.1-4 alkyl, substituted or unsubstituted C.sub.1-4 alkoxy, halogeno, amino, phenyl, or R.sub.4 NR.sub.5 ; R.sub.4 and R.sub.5 are each independently hydrogen, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--(NR.sub.7 .dbd.)CNHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH(NR.sub.7 .dbd.)CNHR.sub.6 wherein n is from 0-5, y is from 0-5 and each x is independently from 1-5; R.

Abstract: The present invention provides compounds having the structureAr.sub.1 --Q--Ar.sub.2 --O--(CH.sub.2).sub.n --Zand pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.

Abstract: A method of treating Pneumocystis carinii pneumonia in a subject in need of such treatment is disclosed. The method comprises orally administering to the subject a bis-benzamidoxime, or a pharmaceutically acceptable salt thereof, that is reduced in the subject to produce a benzamidine having anti-P. carinii activity. The method of the present invention may alternatively comprise intravenously administering to the subject an active compound as disclosed herein. Pharmaceutical formulations and active compounds useful in the practice of the present invention are also disclosed.

Abstract: The present invention provides therapeutically useful substituted guanidines and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.