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WO/1994/028901A1 |
An amino acid derivative having an angiotensin I-converting enzyme inhibitor activity, a vasopressin antagonism and an atrial natriuretic peptide hydrolase inhibitor activity, and represented by general formula (I) wherein R1 represents ...
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WO/1994/026723A2 |
Benzodiazepine derivatives are disclosed that act as potent inhibitors of ras farnesyl:protein transferase. Pharmaceutical compositions containing these benzodiazepines are provided for treatment of diseases for which inhibition of the r...
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WO/1994/025445A1 |
Compounds of formula (I) wherein R1 represents a C3-7cycloalkyl, C7-11 bridged cycloalkyl or C1-6alkyl group which alkyl group may be substituted by a hydroxy, C1-4alkoxy, phenyl, C1-6alkoxycarbonyl, C3-7cycloalkyl, or C7-11 bridged cycl...
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WO/1994/025444A1 |
Compounds of formula (I), wherein R1 represents a phenyl, C3-7cycloalkyl, C7-11 bridged cycloalkyl or C1-6alkyl group which alkyl group may be susbtituted by a hydroxy, phenyl, C1-6alkoxycarbonyl, C3-7cycloalkyl or C7-11 bridged cycloalk...
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WO/1994/024149A1 |
Novel benzodiazepine compounds of formula (1) which exhibit agonistic activity for CCK-A receptors enabling them to modulate the hormones gastrin and cholecystokinin (CCK) in mammals for use in medicine as anorectic agents in the regulat...
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WO/1994/022840A1 |
This invention relates to novel substituted caprolactams, including 4-azacaprolactams such as those of formula (Ic) in which R4, R7, R22, and R27 are as defined in the description, and derivatives thereof which inhibit HIV protease and a...
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WO/1994/022825A1 |
Fibrinogen receptor antagonists of formula (I) are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets, for example (A).
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WO/1994/020473A1 |
A dihydrobenzazepine derivative of general formula (I-A), a tetrahydrobenzodiazepine derivative of general formula (I-B) or a tetrahydrobenzazepine derivative of general formula (I-C), a pharmaceutically acceptable salt thereof, and a ph...
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WO/1994/019329A1 |
This invention relates to substituted cyclic carbonyls and derivatives thereof useful as Human Immnunodeficiency Virus (HIV) protease inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of using these com...
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WO/1994/015924A1 |
Benzodiazepine analogs of formula (I) are disclosed, which are antagonists of gastrin and cholecystokinin (CCK).
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WO/1994/014776A2 |
This invention relates to compounds of formulae (I), (II), (II), wherein A1 is O, S, N-R1 or CHR1; A4 is N-R4 or CHR4; R2 is a sidechain containing an acid or ester group; R1, R4 and R5 are substituents such as H, alkyl and aryl alkyl, a...
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WO/1994/013648A1 |
Compounds of general formula (I) and physiologically acceptable salts thereof; wherein R1 represents CH2CONR5R6 or CH2COR7; R2 represents a phenyl group optionally substituted by 1 or 2 substituents selected from halogen, alkyl, nitro, c...
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WO/1994/011490A2 |
A solution of one or two molecules of aminoguanidine or other hydrazine type compound incubated with an Amadori product (1-propylamine-1-deoxy-D-fructose) under physiological conditions proceeds through the reactive intermediate 1-propyl...
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WO/1994/008977A1 |
This invention relates to novel substituted caprolactams of formula (I), including 4-azacaprolactams, and derivatives thereof which inhibit HIV protease and are useful for treatment of HIV disease. Also included in this invention are pha...
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WO/1994/008051A1 |
Encoded combinatorial chemistry is provided, where sequential synthetic schemes are recorded using organic molecules, which define choice of reactant, and stage, as the same or different bit of information. Various products can be produc...
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WO/1994/006291A1 |
Methods, compositions and devices for synthesizing combinatorial libraries of various useful compounds, such as benzodiazepines, prostaglandins, beta-turn mimetics and glycerol derived drugs is described. Methodologies for solid phase sy...
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WO/1994/005671A1 |
The invention concerns an addition compound obtained by reacting C60 or C70 fullerenes with a diamine of formula (I) in which R1 is C2 to C4 alkylene or 1,2- or 1,3-cyclo-(C3 to C7)-alkylene and R2 and R3, which may be the same or differ...
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WO/1994/003437A1 |
Compounds of formula (I), and salts and prodrugs thereof, wherein R1 represents H, optionally substituted C1-6alkyl or C3-7cycloalkyl; R2 is NHR12 or (CH2)sR13 where s is 0, 1 or 2; R3 represents C1-6alkyl, halo or NR6R7; R4 and R5 are H...
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WO/1994/000438A1 |
A novel benzodiazepine derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof. These compounds are useful as medicines, in particular, for treating and preventing diseases in which CCK-B receptor and ...
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WO/1993/020067A1 |
The present invention is directed to novel benzodiazepine derivatives which are synthesized for the covalent attachment to antigens (proteins or polypeptides) for the preparation of antibodies or receptors to the benzodiazepine metabolit...
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WO/1993/019052A1 |
Compounds of formula (I), and salts and prodrugs thereof. In that said formula, R1 represents certain optionally substitued alkyl or C3-7cycloalkyl; R2 represents (II) or (III), where m is 0, 1, 2 or 3, R9 is H or C1-6alkyl, R10 is imida...
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WO/1993/017011A1 |
Compounds of formula (I), and salts and prodrugs thereof wherein: R1 is H, certain optionally substituted C1-6alkyl, or C3-7cycloalkyl; R2 is (CH2)q-tetrazolyl optionally substituted in the tetrazole ring by C1-4alkyl, (CH2)q-imidazolyl ...
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WO/1993/016999A1 |
A benzodiazepine derivative of formula (I), or a pharmaceutically acceptable salt thereof, wherein (a) R?1¿ is -CH¿2?CHOH(CH¿2?)¿a?R?4¿ or a ketone group -CH¿2?CO(CH¿2?)¿a?R?5¿ in which a is 0 or 1 and R?4¿ and R?5¿ are select...
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WO/1993/015090A1 |
Described are racemic optically active phosphorus compounds of formula (I), in which R is a hydroxy or protected hydroxy group, R1 is a hydroxy or protected hydroxy group or a lower alkoxy group and R2 is a lower alkyl, cycloalkyl or ary...
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WO/1993/015091A1 |
Described are racemic optically active phosphorus compounds of the formula (I), in which R is a lower alkyl or lower alkoxy group and R1 is a lower alkyl, cycloalkyl or substituted phenyl group. The compounds of the formula (I) act, in t...
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WO/1993/014772A1 |
The invention relates to a new utilization of niobium derivatives in the 4 or 5 oxidation status as active principle for the production of medicaments useful in the treatment and/or prevention of glucid and/or lipid metabolism troubles. ...
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WO/1993/014075A1 |
Compounds of general formula (I), wherein R1 represents a phenyl, C3-7cycloalkyl, bridged C7-11cycloalkyl or C1-6alkyl group which alkyl group may be substituted by a hydroxy, phenyl, C1-6alkoxycarbonyl, C3-7cycloalkyl or bridged C7-11cy...
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WO/1993/013775A1 |
The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging) which contain diaminopyridines and derivatives thereof. Accordingly, a composition is disclosed which comprises an agent ...
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WO/1993/014074A1 |
Compounds of general formula (I), wherein R1 represents a phenyl, C3-7cycloalkyl, C7-11 bridged cycloalkyl or C1-6alkyl group which alkyl group may be substituted by a hydroxy, phenyl, C1-6alkoxycarbonyl, C3-7cycloalkyl, or C7-11 bridged...
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WO/1993/012791A1 |
Pharmaceutical compositions and methods of using CCK-ligands as antipsychotic, antianxiety, and agents useful in treatment or prevention of withdrawal symptoms caused by withdrawal of chronic or long-term use of diazepam, alcohol, cocain...
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WO/1993/011761A1 |
Aryltriflates and related compounds having general formula (1) wherein Ar is an aromatic or heteroaromatic system of a compound which has a therapeutic, biological activity when it, in the same position, carries a hydroxy, alkyloxy, halo...
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WO/1993/011771A1 |
It is a purpose of this invention to provide a means of treating various central nervous system (CNS) injuries to prevent or minimize damage to the CNS. A novel use has been found for some previously known compounds which are inhibitory ...
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WO/1993/011117A1 |
Novel N-[2-(cyclic alkyl)phenyl]pyrazole-4-carboxamides useful as fungicides, methods of using said compounds, and fungicidal compositions containing them.
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WO/1993/008176A1 |
Compounds of formula (I), and salts and prodrugs thereof, wherein X is O, S, NR?4¿ or CH¿2?; R?1¿ represents H, certain optionally substituted C¿1-6? alkyl, or C¿3-7? cycloalkyl; R?2¿ represents phenyl having certain optional subst...
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WO/1993/008175A1 |
Compounds of general formula (I), wherein R?1¿ represents a group selected from CH¿2?CONR?4¿R?5¿, XYR?6¿, phenyl, C¿3-7?-cycloalkyl or C¿1-6?alkyl, optionally substituted by a hydroxy, phenyl, C¿1-6?alkoxycarbonyl, C¿3-7?cycloal...
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WO/1993/008174A1 |
A benzodiazepinedione derivative which acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII¿b?III¿a? receptor and is provided in therapeutic compositions for ...
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WO/1993/007128A1 |
This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral...
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WO/1993/007429A1 |
An air treatment plant, e.g. a freezing plant, for foodstuffs, comprises a housing (1), an elongate trough (11) provided therein for receiving the foodstuff to be treated, a heat exchanger (12) and a fan assembly (13) for producing an ai...
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WO/1993/007143A1 |
Methylpiperazinoazepine derivatives of general formula (I), wherein X, R1, R2, N1 and N2 have various meanings, pharmaceutically acceptable salts thereof, and their preparation and use, are described.
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WO/1993/007130A1 |
Compounds having formula (I), wherein R1 is a hydrogen or halogen atom or an alkyl, alcoxy, alkylthio, nitro, hydroxy or cyano radical; R2 is an alkyl radical or a chain -CH(R5)-CO-R6; R3 is (a) a phenyl radical substituted by one or a p...
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WO/1993/007132A1 |
The present invention provides substituted dibenzoxazepine compounds of formula (I), which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound ...
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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/1993/003011A1 |
A novel urea derivative represented by general formula (I) or a salt thereof, having a $g(k)-receptor activator activity and being useful as a centrally acting analgesic.
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WO/1993/001815A1 |
A drug selectively inhibiting the production of an IgE antibody and useful for preventing and/or treating various allergic diseases, which contains as the active ingredient a lowly toxic 1-phenyl-5H-2,3-benzodiasepine derivative, represe...
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WO/1993/000095A2 |
This invention relates to compounds of formula (I), wherein A1 to A5 form an accessible substituted seven-membered ring, which may be saturated or unsaturated, optionally containing up to two heteroatoms chosen from the group of O, S and...
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WO/1992/020749A1 |
A water-based recording ink comprising water, pigment, a water-soluble homopolymer, and a copolymer having both hydrophobic and hydrophilic parts. This ink can give printed characters excellent in density, lightfasteness and water resist...
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WO/1992/014704A1 |
The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging) which contain novel 2-substituted-2-imidazolines. Accordingly, a composition is disclosed which comprises an agent capabl...
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WO/1992/013860A1 |
The invention concerns compounds of the formula (I), in which R�1?, R�2?, R�3? and R�4? represent groups defined in the claims. The invention also concerns a method of preparing these compounds, drugs containing them for the trea...
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WO/1992/011246A1 |
A novel benzodiazepine derivative represented by general formula (I), a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof, and a process for producing the same. In formula (I), R?1¿ represents optionally sub...
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WO/1992/009297A1 |
Peptide mimics, having a constrained peptide backbone conformation, are HIV protease inhibitors. A compound of this invention is, for example, 3-Benzyl-5(alaninyl-1-aminoethyl)-2,3,6,7-tetrahydro-N-azepi
nyl-2-propionyl-valinyl-valinyl m...
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