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WO/1991/019734A2 |
A thrombin inhibitor comprising a first bulky hydrophobic portion interacting with the catalytic site of thrombin responsible for proteolysis and a second portion at least maintaining the hydrophobic and acidic character of amino acids 5...
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WO/1991/018869A1 |
A phenyl 4-guanidinobenzoate derivative of general formula (I) and a pharmacologically acceptable acid addition salt thereof, each having an excellent protease inhibitor activity, wherein R1 represents hydrogen or halogen; R2 represents ...
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WO/1991/018868A1 |
The invention relates to a method for the treatment or prophylaxis of psychosis, depression, hypertension, or anxiety in an animal by administering an effective amount of an N,N'-disubstituted guanidine or 2-imino-imidazolidine having a ...
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WO/1991/013904A1 |
Disclosed is the identification, characterization, and purification of two chymotrypsin-like serine proteases characteristic of AD, called "chymase" and "multicatalytic protease". Both chymase and the multicatalytic protease have an enzy...
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WO/1991/013056A1 |
Disubstituted guanidines, e.g., bis-1,3-(o-isopropylphenyl) guanidine, bis-1, 3-(m-isopropylphenyl) guanidine, bis-1,3-(1-naphthyl)guanidine, bis-1,3-(m-methoxyphenyl)guanidine, N-(1-naphthyl)-N'-(o-iodophenyl)-guanidine, N-(1-naphthyl)-...
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WO/1991/012797A1 |
Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors o...
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WO/1991/011994A1 |
A pharmaceutical composition containing as the active ingredient a compound which presents low-density lipoproteins (LDL) represented by the compounds of formula (I) from being negatively charged. This composition inhibits the LDL from u...
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WO/1991/010442A1 |
Compounds of the formula A-(C)�b?-(D)�c?-M-(X)�e?-Y-Z wherein: A is BocNH, CbzNH, H, R'R''N, R''CONR', or if a, b and c are 0 and Y is a covalent bond, then A is H, Boc, Cbz, R'' or R''CO; C and D are the same or different and are ...
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WO/1991/006543A1 |
Peptides which include unnatural amino acids and which either inhibit or promote the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. Administration of an effective amount of such pepti...
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WO/1991/004746A1 |
Disclosed are novel peptides and pseudopeptides and pharmaceutical compositions thereof that inhibit platelet aggregation and thrombus formation in mammalian blood.
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WO/1991/003549A1 |
Light activated acyl-enzymes of formula (III) are disclosed. In the compounds of formula (III) ENZ is an enzyme, X is O or S, Y is -NR3R4, -OR5, or -SR5, and Z is a nucleophile; m is 0 to 3 and n is 1 or 2; Y is substituted on the ring a...
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WO/1991/000853A1 |
Polyamine compounds are used as agents regulating ionic conductances in cellular membranes. These polyamines are used in blocking, modulating or activating calcium and other cationic channels in neuronal cell membranes and in blocking, m...
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WO/1990/013536A1 |
Antimicrobial bis-(pyrrolidonyl alkylene) biguanides having the formula: A-Z-A where A is: (I); X is C2-C4 alkylene; and Z is a bivalent bridging group, and acid addition salts thereof, are provided herein.
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WO/1990/009405A1 |
The invention relates to a quaternary ammonium compound having the formula (1), said compound containing one or a plurality of biguanide groups, at least one radical R0, R6, R1,y or R2,y for y comprised between 0 and n, represents a radi...
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WO/1990/008130A1 |
The compounds of formula (I), wherein R1 is a C18-24 alkenyl containing at least two double bonds, X is O, NH or C1-4 alkyl-N, Y is CONH2, COOH or COOMe, wherein Me is metal, and R2 is a side chain of a natural amino acid at alpha-positi...
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WO/1990/003176A1 |
Polyoxometallate compounds which exhibit anti-retroviral activity, are disclosed. These compounds have the following general molecular formulas: (X+)n(H+)4-n(SiW12O40)4-, n = 0 - 4; (X+)n(H+)5-m(BW12O40)5-, m = 0 - 5; (X+)n(H+)4-n(W10O32...
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WO/1989/008127A1 |
A method for increasing the water-solubility of highly insoluble organic compounds by forming a complex product from the reaction between the organic compound and an aqueous solution of solid polyvinylpyrrolidone. The solubility of the o...
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WO/1989/007099A1 |
Novel 2,2-disubstituted glycerol compounds are disclosed for use as anti-allergic and anti-inflammatory compounds. The compounds are antagonists of platelet activating factor (''PAF''). Also disclosed are methods of synthesizing and usin...
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WO/1989/007098A1 |
The present invention concerns a compound having structure (I), wherein R1 is a branched- or unbranched-chain alkylamine having from 2 to 20 atoms in the chain and wherein each of R2, R3 and R4 is the same or different and is hydrogen or...
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WO/1989/004595A2 |
This invention concerns N,N,N',N'-tetramethyl-N''-(3,4-dichlorophenyl)guanidine; 2-[(2,4-dimethylphenyl)imino]-3-methyloxazolidine or N-(3-chloro-4-methylphenyl)-N',N'-dimethylacetamidine and its acid addition and quaternary salts; or a ...
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WO/1989/001930A1 |
The invention comprises compositions and methods for the treatment of psoriasis. The compositions comprise compounds of formula (I).
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WO/1989/000423A1 |
A compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 is hydrogen; R2 is (C1-C15)alkyl, (C3-C15)alkenyl, phenyl, substituted phenyl, (C7-C20)phenylalkyl, or substituted (C7-C20)phenylalkyl wherein the substi...
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WO/1989/000576A1 |
Non-hygroscopic, azithromycin (9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin) dihydrate and a process therefor.
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WO/1988/007990A1 |
The invention relates to an improved method for the preparation of an amidino-urea derivative of general formula (I), wherein R1, R2 and R3 each stand for hydrogen, halogen, lower alkyl, lower alkoxy, trifluoromethyl, nitro or optionally...
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WO/1988/000583A1 |
Formula (I), wherein R and R' are hydrocarbon groups, e.g., N,N'-dibutyl-guanidine, N,N'-diphenyl-guanidine, N,N'-di-o-tolyl-guanidine, N-o-tolyl-N'-p-azido-o-tolyl-guanidine and N-adamantyl-N'-o-tolyl-guanidine, are highly selective lig...
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WO/1988/000181A1 |
Antiviral organic guanidine derivatives compositions; a process of producing the antiviral compositions; and a method for inhibiting viruses utilizing the compositions. More particularly, the compositions are tubastrines derived from mar...
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WO/1987/004433A1 |
Process for the preparation of benzotriazine oxide by the cyclization of a defined class of guanidinyl compounds which themselves are prepared by reaction of a substituted nitro-benzene compound with a cyanamide. In one form of the inven...
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WO/1987/000437A1 |
Improved methods of disinfecting and/or preserving contact lenses comprises treating said lenses with an effective concentration of a solution comprising a biguanide or a water soluble salt of formula (I), wherein R1 and R3 are selected ...
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WO/1986/005782A1 |
Novel guanidine derivatives having a straight hydrocarbon chain as a molecular skeleton, a guanidino group, (I), on the primary carbon atoms of both ends, and an amino group on the central carbon atom possess excellent effects against va...
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WO/1986/004935A1 |
Improved process for the preparation of amidinoureas and for the preparation of liquid pharmaceutical compositions.
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WO/1986/000893A1 |
Novel amidine compounds represented by formula (I) (wherein R1 and R2 each represents hydrogen, a straight or branched chain alkyl group containing 1 to 6 carbon atoms, R3 represents a straight or branched chain alkyl group containing 1 ...
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WO/1985/003076A1 |
Compounds of the formula (I), and pharmaceutically acceptable salts, wherein R1 is hydrogen or methyl and R2 is hydrogen or C1-4alkyl. These compounds have inotropic, vasodilator, bronchodilating and platelet aggregation inhibiting prope...
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WO/1984/004247A1 |
A class of bicyclic benzenoid aminoalkylene ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods fo...
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WO/1984/004245A1 |
A class of naphthalene aminoalkylene ether and thioether compounds exhibiting pharmacological activity including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the tr...
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WO/1984/000875A1 |
Methods for the treatment of physiological disorders, including protozoal infections in mammalian and avian species and gastrointestinal and cardiovascular disorders in mammalian species by administering a class of aralkyl- and aralkenyl...
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WO/1984/000105A1 |
The medicinal preparation having an antitumoral effect consists of an active substance-polyhexamethylene guanidine- of the formula (I):$(7,)$and contains a pharmaceutical diluent.
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WO/1982/001367A1 |
Guanidine derivatives of formula: (FORMULA) their isomers at the guanidine groups and pharmaceutically acceptable salts of such compounds, wherein one of X and Y is CR5 and the other is CH or N; R1 is hydrogen, halogen, nitro, amino, NHC...
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WO/1980/001694A1 |
Cyano-guanidins having the formula: (FORMULA) wherein: R1 is (a) the remains HS-CH2-CH2-, (b) the remains HO-CH2-CH2-, (c) the remains (FORMULA) (d) the remains (FORMULA) and several processes of the respective preparation thereof. The c...
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JP7464280B2 |
Provided are an environmentally-friendly high-efficiency method of manufacturing an ester compound based on an esterification reaction using a salt ion-exchange method and an ester compound manufactured thereby. In the conventional ester...
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JP2024038014A |
The present invention provides a novel lipid and a composition containing the same. The nanoparticle compositions of the present disclosure include novel lipids and additional lipids such as phospholipids, structured lipids, and PEG lipi...
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JP7447005B2 |
The present invention relates to an improved process for the preparation of metformin hydrochloride, an important drug in the first line treatment of Type II Diabetes.
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JP2024027144A |
The present invention provides lipids and compositions that can effectively deliver introduced compounds such as nucleic acids to target cells or tissues in vivo. The lipid of the present invention is a lipid represented by the following...
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JP2024505327A |
This disclosure describes compositions, preparations, nanoparticles (such as lipid nanoparticles), and/or nanomaterials, and methods of using them. [Selection diagram] None
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JP2024504532A |
The present invention relates to a novel co-crystal, a pharmaceutical composition containing the same, and a method for producing the same, and utilizes the co-crystal of the present invention to effectively prevent and/or prevent cancer...
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JP2024009811A |
The present invention provides creatine prodrug analogs and compositions thereof useful for treating creatine deficiency. [Solution] Compound of formula (I): (In the formula, R is -CH3,-CH2D,-CHD2, or -CD3;R1is straight-chain or branched...
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JP2024001077A |
The present invention provides novel compounds containing biguanidyl radicals that are more potent than metformin in the treatment of cancer. [Solution] The present invention provides formula (I) Novel compounds of the invention and thei...
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JP7403624B2 |
The present invention relates to a novel crystal modification of N-(aminoiminomethyl)-2-aminoacetic acid, crystal mixtures, and a process for preparing said crystal modification and said crystal mixtures.
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JP7400658B2 |
A resist composition comprising a base polymer and a salt is provided. The salt consisting of an anion derived from an iodized or brominated phenol and a cation derived from a 2,5,8,9-tetraaza-1-phosphabicyclo[3.3.3]undecane, biguanide o...
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JP7399996B2 |
The present disclosure provides purified forms of iobenguane and preparations of a precursor to iobenguane, such as a polymer, the polymer comprising a monomer of formula (I) or a pharmaceutically acceptable salt thereof, the preparation...
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JP7386383B2 |
The invention concerns a compound according to following formulawherein R1 is a halogen residue.
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