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WO/1994/026709A1 |
Guanidine derivatives of formula (I), wherein Y is N or C-R1 (in which R1 is hydrogen, lower alkyl, hydroxy, protected hydroxy, etc.), R2 is hydrogen, aryl which may have one suitable substituent, aryloxy, etc., R3 is hydrogen, lower alk...
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WO/1994/022807A1 |
A compound having formula (I) or a pharmaceutically acceptable salt thereof, wherein X and Z each independently are NH or CH2, at least one of X and Z being NH; Y is O, S, NCN, or NH; B, D, E and F each independently are C or N, at least...
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WO/1994/021602A1 |
Novel urea derivatives are provided which inhibit platelet aggregation. This invention also pertains to pharmaceutical compositions and methods of using such derivatives.
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WO/1994/021599A1 |
A compound with a platelet aggregation inhibitor activity, represented by the following general formula (I), and pharmacologically acceptable salt and solvate thereof. Examples of the compound are as in (II).
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WO/1994/020449A1 |
The salts of S(+) 2-(3-benzoylphenyl)propionic acid and of R(-) 2-(3-benzoylphenyl)propionic acid with an achiral, organic base such as tris-(hydroxymethyl)aminomethane or a chiral organic base such as D-lysine, L-lysine, L-arginine, (R)...
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WO/1994/019314A1 |
The invention aims at providing a device comprising lipids that act like the so-called cationic liposome and are reduced in toxicity and the lipids as the constituent of the device. The invention compounds are exemplified by 3-0-(4-dimet...
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WO/1994/018987A1 |
The invention aims at effectively utilizing a single-stranded nucleic acid copolymer, in particular, poly(adenylic acid-uridylic acid) and providing a drug composition having an antitumor effect. An example of the drug composition of the...
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WO/1994/017817A1 |
This invention relates to peptide aldehyde analogs that inhibit the thrombin or Factor Xa. The compounds are thought useful for preventing or treating conditions in mammal characterized by abnormal thrombosis.
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WO/1994/017034A1 |
Compounds are disclosed having the general formula (I) R1-(A)a-(B)b-(D)c-(CH2)m-N(R2)-(CH2)n-R3, in which A, B, D, R1 to R3 and a, b, c, m and n have the definitions given in the description, as well as a process for preparing the same a...
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WO/1994/017041A1 |
The present invention relates to a class of compounds represented by formula (I) which inhibit platelet aggregation. This invention also pertains to pharmaceutical compositions and methods of using such derivatives. In said formula, R is...
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WO/1994/017035A1 |
New aminoacid derivates have the general formula: T-Z-NR1-(R2CR3)-CO-Y-(CH2)n-R, in which R, R1 to R3, T, Z, Y and n are defined as in the first claim. They represent valuable NPY-antagonistic active substances. Also disclosed are their ...
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WO/1994/015909A1 |
Compounds which have one of structural formulae (I) or (II). AA is an amino acid residue or an amino acid chain of two or more amino acid residues, excluding the N-terminal and the C-terminal from said amino acid residue or amino acid ch...
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WO/1994/014755A1 |
A novel anti-active-oxygen agent which inhibits the generation of active oxygen species, is highly safe, can be preparated at a rather low cost, and contains an amino acid derivative represented by general formula (I) or a salt thereof a...
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WO/1994/013631A1 |
A propionic acid derivative represented by general formula (I) or a pharmaceutically acceptable acid-addition salt thereof, wherein A represents OH, C1-C8 lower alkoxy, -NR1R2, or C1-C8 lower alkoxy which may be substituted by halogen, o...
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WO/1994/012169A1 |
Novel carboxy-peptidyl compounds of formula (I) are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, peri...
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WO/1994/012654A1 |
A process for preparing clavulanic acid and other clavam derivatives from any one of S-arginine, compounds of formula (I), wherein R1 is (a) or (b), wherein R2 = H or C1-6alkyl; compounds of formula (II), wherein R1 is (c) or (d), where ...
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WO/1994/008941A1 |
The present invention is directed to novel arginine alpha-keto-amide derivatives, their pharmaceutically acceptable salts and compositions thereof which are useful as antithrombotic agents in mammals and also the use of these compounds a...
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WO/1994/007815A2 |
Oligopeptide compounds or oligopeptide analogue compounds of the formula A-B-D are ligands for the anaphylatoxin receptor and are useful in the treatment of inflammatory disease states; also disclosed are anaphylatoxin receptor ligand co...
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WO/1994/005258A1 |
An antivirally active pharmaceutical oil-in-water emulsion containing 9-[(2-hydroxyethoxy)methyl]guanine (acyclovir) or a salt or ester thereof as an active ingredient in the continuous aqueous phase, said phase in addition to said activ...
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WO/1994/004172A1 |
A method of treating medical conditions with proteinase inhibitors of formula (I), wherein B is H or an amino acid blocking group for the N-terminal amino acid nitrogen; R1 is an optionally protected alpha-amino acid side chain such that...
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WO/1994/002453A1 |
(S)-N5-[Imino(methylamino)methyl]ornithine hydrochloride, pharmaceutical compositions containing it, its us in medicine and its preparation is described.
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WO/1993/024448A1 |
An amino acid derivative represented by general formula (I), a pharmacologically acceptable salt thereof, and a cancer metastasis inhibitor containing the same, wherein L?1¿ and L?2¿ represent each an amino acid residue, etc.; A?1¿ an...
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WO/1993/024126A1 |
Guanidine substituted arginines or homoarginines based on monoalkyl carbon substituted ornithines or lysines, having formula (I) wherein R is (CH2)yCH3 or H, R' is CH2 or C(H)(CH2)yCH3, and R" is CH2 or C(H)(CH2)yCH3, with y ranging from...
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WO/1993/019042A1 |
A process for the preparation of a substituted guanidine by reacting a substituted cyanamide with ammonia or a substituted amine in the presence of a Lewis acid catalyst. Also disclosed is a process for the preparation of a tri-substitut...
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WO/1993/017555A1 |
N,N'-disubstituted guanidines exhibiting a high binding affinity to phencyclidine (PCP) receptors are disclosed. These N,N'-disubstituted guanidine derivatives act as non-competitive inhibitors of glutamate induced responses generated vi...
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WO/1993/017017A1 |
The present invention is concerned with vasoconstrictive [(benzodioxan, benzofuran or benzopyran)alkylamino]alkyl substituted guanidines having formula (I), the pharmaceutically acceptable acid addition salts thereof, and the stereochemi...
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WO/1993/016037A1 |
There are provided compounds of formula (1) wherein R1 is a substituted or unsubstituted divalent aliphatic group of 1 to 16 carbon atoms; wherein the substituents are mono or poly and are selected from the group consisting of lower alky...
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WO/1993/015756A1 |
This invention relates to peptide aldehyde analogs that inhibit the thrombin or Factor Xa. The compounds are thought useful for preventing or treating conditions in mammal characterized by abnormal thrombosis.
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WO/1993/012777A1 |
Methods for regulating cation transport across cellular membranes possessing cation channels are provided. The cell membrane possessing a specific ion channel is exposed to a non-aromatic polyamine compound having a lysine- or arginine-b...
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WO/1993/011759A1 |
This invention relates to novel diaminoalkanoic acid derivatives that inhibit platelet aggregation and thrombus formation in mammalian blood thereby being useful in the prevention and treatment of thrombosis associated with disease state...
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WO/1993/011152A1 |
The invention relates to new competitive inhibitors of thrombin, their synthesis, pharmaceutical compositions containing the compounds as active ingredients, and the use of the compounds as anticoagulants for prophylaxis and treatment of...
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WO/1993/010168A1 |
A curing agent for epoxy resins having improved solubility characteristics has formula (I). Such bis-dicyandiamides are soluble in various solvents and do not require the use of undesirable solvents necessary with dicyandiamide.
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WO/1993/010102A1 |
Novel compounds having a guanidine structure of formula (I), in which R1 is an isopropyl radical, benzyl optionally substituted by one or more alkoxy (C1-C4) radicals or a radical (a); R2, R3 and R4 are the hydrogen atom or together can ...
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WO/1993/009795A1 |
Non-peptidic RXD analogues are provided that inhibit biological cellular and molecular interactions which are dependent on RXD recognition, wherein X is one of the amino acid residues G, E, Y, A or F. In particular, RGD surrogates are pr...
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WO/1993/009132A1 |
Compounds of formula (I) wherein R1 and A are amino terminal groups: Z is O or N-R2; M is a dipeptide isostere; and D1 and D2 are optionally absent or amino acids; and pharmaceutically acceptable salts thereof, are potent inhibitors of t...
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WO/1993/004032A1 |
A compound having a high insecticidal activity, represented by general formula (I), or a salt thereof wherein R¿1? represents optionally substituted alkyl; R¿2? represents hydrogen, optionally substituted alkyl or COR¿3? wherein R¿3?...
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WO/1993/004373A1 |
Method and composition useful for treating a patient having a disease characterized by an abnormal level of one or more components, the activity of which is regulated or affected by activity of one or more Ca?2+¿ receptors. Novel compou...
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WO/1992/019643A1 |
A method for preparing peptides, wherein the peptide bond is formed by condensing a first amino acid or peptide derivative in which the amine function at alpha is protected by a group Boc, Fmoc, Moz, Ddz or Nps and in which the functiona...
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WO/1992/018117A1 |
Disclosed are novel peptide and pseudopeptide derivatives that inhibit platelet aggregation and thrombos formation in mammalian blood thereby being useful in the prevention and treatment of thrombosis associated with certain disease stat...
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WO/1992/017025A2 |
Peptides which include unnatural amino acids and which inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. The peptides are analogs of the decapeptide GnRH wherein there is at ...
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WO/1992/015546A1 |
Compounds and a method useful for protection of tissue cells in a mammalian body from irreversible damages due to lactic acidosis caused by oxygen deficiency. The protection is achieved by administering a compound having a cell membrane ...
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WO/1992/015555A2 |
Fluorinated alkene compounds useful for and methods of controlling nematodes, insects, and acarids that prey on agricultural crops. Polar compounds, for example, 3,4,4-trifluoro-3-butene-1-amine or 3,4,4-trifluoro-3-butenoic acid, are pa...
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WO/1992/014697A1 |
Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N, N', N", N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are metho...
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WO/1992/013552A1 |
This invention relates to compounds of the formula D-E-Asp-Q-Y, wherein: Q is NH, NCH3 or O; Y is phenyl, naphthyl or Het, unsubstituted or substituted by one to three C1-6alkyl, trifluoromethyl, halogen, OR', SR', (CH2)nAr, CONR1R2, CO2...
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WO/1992/011847A1 |
The invention relates to the use of a compound according to formula (I) in which x is an integer of from 2 to 5 and A signifies -NH-C(=NH)-NH2,-CH2-NH2 or -CO-NH2 or agmatin, for the preparation of a medicament for treatment of endotoxin...
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WO/1992/012140A1 |
Peptides ketoamides, ketoacids, and ketoesters, their use in inhibiting serine proteases and cysteine proteases.
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WO/1992/011233A1 |
N-(3-Chloro-5-cyanophenyl)-N'-cyano-N''-t-pentylguanidine remarkably useful as a potassium channel opening agent, particularly as a remedy for hypertension.
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WO/1992/008464A1 |
Substituted urea, thiourea and guanidino compounds, and related compounds and salts, useful as cell receptor antagonists for modulating cell adhesion via integrin receptors and/or fibronectin receptors, are disclosed. Methods for synthes...
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WO/1992/001726A1 |
A curing agent for epoxy resins having improved solubility characteristics has formula (I) where R is -C6H5X, -CH2C6H4X, -CH2CH2C6H4X, or -CnH2n-1, and X is either -H, -CH3, -OCH3, -OH, or -NY, where Y is -H or CH3 and where n is 1 to 12...
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WO/1992/000273A1 |
Compounds of formula (I) and their salts in which R1 is optionally substituted phenyl, R2 is alkyl, cycloalkyl or optionally substituted amino, or R2 and R3 together with the nitrogen and carbon atoms to which they are attached form an o...
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