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WO/1996/030371A1 |
A process for the preparation of esters of anhydroecgonine having formula (I), any of its enantiomers or any mixture thereof, or a salt thereof, wherein R is alkyl, or optionally substituted aryl, or arylalkyl; comprising the step of rea...
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WO/1996/022290A1 |
A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1A receptor. The compounds are particularly useful for alleviating ...
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WO/1996/021644A1 |
A compound of formula (I) or a salt thereof, or a solvate thereof, wherein either: (i) Ra represents a group R5 which is hydrogen, alkyl or optionally substituted aryl and Rb represents a moiety of formula (a); wherein X represents a hyd...
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WO/1996/020940A1 |
The invention relates to a novel chemical compound having structural formula (I). The compound (I) is useful in the diagnosis of dopaminergic diseases like Parkinson's disease and schizophrenia. The invention also relates to mixtures of ...
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WO/1996/019493A1 |
The present invention discloses peptide aldehydes which are potent inhibitors of factor Xa, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for di...
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WO/1996/014316A1 |
A method of treating urinary bladder dysfunctions in a subject in need thereof comprising administering to said subject an effective amount of a compound of formula (I) wherein X is oxygen or sulphur; and G is selected from one of the fo...
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WO/1996/012711A1 |
The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases i...
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WO/1996/011928A1 |
A process of enantioselective synthesis of seven-membered carbocycles in the presence of di-rhodium(II) tetracarboxylate catalysts.
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WO/1996/011192A1 |
The present invention provides compounds of the formula Ar1-Q-Ar2-Y-R-Z and pharmaceutically acceptable salts thereof wherein Ar1 and Ar2 are optionally substituted aryl moieties, Z is an optionally substituted nitrogen-containing moiety...
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WO/1996/009302A1 |
Bicyclic carboxamides of formula (I) and the pharmaceutically acceptable acid addition salts are 5-HT1A binding agents, particularly 5-HT1A antagonists, and may be used, for example, as anxiolytics. In the formula, X represents -CR2 = CR...
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WO/1996/008480A1 |
The invention concerns novel compounds of general formula (I) and pharmacologically acceptable salts thereof, A, B, Z, R1, R2, R3 and m having the definitions given in the description; methods of producing said compounds; and pharmaceuti...
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WO/1996/006082A1 |
A compound of formula (I) and its pharmaceutically acceptable salts, wherein A1 and A2 are each halo; X is direct bond, CH2, CO, O, S, S(O) or S(O)2; R1 is selected from a variety of groups such as hydrogen; substituted or unsubstituted ...
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WO/1996/006081A1 |
This invention relates to compounds of formula (I), or pharmaceutically acceptable acid addition salts thereof, wherein: (a) R2 and R5 are taken separately and R1, R2, R3 and R4 are each independently hydrogen, (C1-C6) alkyl, halo, CF3, ...
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WO/1996/006083A1 |
A compound of formula (I) and its pharmaceutically acceptable salts, wherein A1 and A2 are each halo; X is a direct bond, CH2, CO, O, S, S(O) or S(O)2; R1 is selected from a variety of groups such as hydrogen; substituted or unsubstitute...
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WO/1996/005193A1 |
The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein R is C3-C7 cycloalkyl, aryl or C1-C6 alkyl, said C1-C6 alkyl being optionally substituted by fluoro, -COOH, -COO(C1-C4 alk...
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WO/1996/003123A1 |
Invented is a method of treating opportunistic infections in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a substituted azaspirane.
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WO/1996/003401A2 |
A process for preparing a compound of formula (I), wherein n is 2 or 3; which process comprises reducing a compound of formula (II), wherein R1 is hydrogen or C1-4 alkyl and n is 2 or 3; by catalytic hydrogenation in the presence of a rh...
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WO/1995/034561A1 |
The present invention relates to a novel class of covalently coupled benzoylecgonine, ecgonine and ecgonidine derivatives that are useful for alleviating the symptoms of immunoregulatory disorders, neuromuscular disorders, joint disorder...
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WO/1995/032209A1 |
Novel 5-HT3 receptor antagonist compounds having general formula (I) wherein each of R, R1 and R2, which may be the same or different, is hydrogen, halogen, hydroxy, cyano, C1-C6 alkyl, CF3, C1-C6 alkoxy, C1-C6 alkylthio, formyl, C2-C6 a...
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WO/1995/031455A1 |
A quinolinecarboxylic acid represented by general formula (C) or a medicinally acceptable salt thereof, each having a serotonergic receptor-stimulating effect on sertonin 4 receptors. In said formula, C represents hydroxymethyl, methoxy,...
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WO/1995/030640A1 |
Compounds having formula (I) are useful as inhibitors of protein kinase C. Also disclosed are pharmaceutical compositions including such compounds.
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WO/1995/028401A1 |
The present invention discloses compounds of formula (I), (II), (III) or (IV) any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or 2-hydroxyeth...
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WO/1995/023799A1 |
A process for preparing granisetron (1) or a pharmaceutically acceptable salt thereof, which process comprises deprotecting a compound of Structure (2), wherein R is a nitrogen-protecting group which does not significantly reduce the nuc...
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WO/1995/023147A1 |
Endo-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl) 1-isopropyl-2(1H)-quinolone-3-carboxylate represented by formula (1) or an acid-addition salt thereof, acting on serotonin 4 receptors to exhibit a serotonin-like receptor-stimulating effects. ...
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WO/1995/021820A1 |
A carbamate derivative represented by general formula (I), a salt thereof, a hydrate thereof, or a solvate thereof, said derivative having a muscarine M3 receptor antagonism and being useful as a preventive or remedy for digestive, respi...
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WO/1995/011901A1 |
Disclosed are certain cocaine analogs useful for imaging of cocaine receptors and dopamine receptors. Also disclosed are analogs useful for imaging diagnostics for Parkinson's disease.
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WO/1995/006635A1 |
A carbamate derivative represented by general formula (I), a salt thereof, a hydrate thereof, or a solvate thereof. It has a muscarine M3 receptor antagonism and is useful for preventing or treating digestive, respiratory or urologic dis...
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WO/1995/005379A1 |
The method of this invention comprises administering to a patient suffering from or susceptible to schizophrenia or schizophreniform conditions an effective amount of a compound of formula (I), wherein X is oxygen or sulphur; G is select...
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WO/1995/005364A2 |
The present invention provides a compound having structure (I), (II) or (III). The present invention also provides a pharmaceutical composition comprising the compound above and a pharmaceutically acceptable carrier. The present inventio...
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WO/1995/003301A1 |
A compound of formula (I) or a salt thereof, or a solvate thereof, wherein B represents a C1-4 n-alkylene group wherein each carbon is optionally substituted by a C1-6 alkyl group; Z represents a bond, CH2, (CH2)2 or X-CH2-CH2 wherein X ...
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WO/1995/001184A1 |
An iodinated neuroprobe is provided for mapping monoamine reuptake sites. The iodinated neuroprobe is of formula (I), wherein: R = a monofluoroalkyl group including nF where n=18 or 19; R' = a CnH2n+1 group where n=0-6; X = an isotope of...
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WO/1994/029306A1 |
Methylecgonidine (MEG; anhydroecgonine methylester) is produced when cocaine base ("crack") is heated. MEG alone and in combination with cocaine was tested for action on isolated tracheal rings stimulated to contact with acetylcholine. A...
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WO/1994/026274A1 |
Selective blockade of DA and 5-HT uptake sites with 3-aryltropane derivatives.
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WO/1994/020464A1 |
The instant invention is a method of coupling compounds comprising the septs of: a) forming a maleimide derivative by reacting a maleimide containing compound having formula (I) with an amine functional compound capable of displacing the...
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WO/1994/020496A1 |
The present invention relates to therapeutically active azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful as stimulants of the cognitive func...
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WO/1994/015935A1 |
A compound of formula (I), formula (II) or formula (III), wherein R1 is selected from the group consisting of H; branched or unbranched alkyl, alkenyl and alkynyl, said alkyl, alkenyl and alkynyl being optionally substituted with OH, SH,...
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WO/1994/012497A1 |
Endo-N-(8-Methyl-8-azabicyclo[3.2.1]oct-3-yl)-1-isopropyl-2(
1H)-quinolone-3-carboxamide represented by formula (I) or an acid addition salt thereof has a strong stimulating effect on serotonin 4 receptors and is useful for treating dise...
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WO/1994/004151A1 |
Invented is a method of treatment of psoriasis in a mammal in need thereof which comprises administering to such mammal an effective amount of a substituted azaspirane.
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WO/1994/004495A1 |
Compounds characterized generally as piperidinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of formula (I), wh...
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WO/1994/004146A1 |
Disclosed are benztropine and CFT analogs useful for imaging of cocaine receptors and treatment of cocaine abuse. Also disclosed are analogs useful for imaging and treatment of Parkinson\'s disease.
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WO/1994/003426A1 |
Compounds of formula (I), wherein R1 represents C1-4alkyl; and R2, R3, R4 and R5 each independently represent hydrogen, halogen, C1-4alkyl, C1-4alkoxy, C1-4alkoxyC1-4alkyl, C1-4alkylsulphonyl, trifluoromethylsulphonyl; optionally substit...
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WO/1994/001435A1 |
Compounds of general formula (I), where Ar = phenyl or beta-naphtyl, R1 = one or more substituents of the phenyl or beta-naphtyl nucleus, preferably in para position, and selected out of the group consisting of H, CH3, C(CH3)3, CH2-CH-(C...
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WO/1994/000448A1 |
Pharmacologically active azacyclic and azabicyclic alkyliden hydroxylamines as cholinergic agents, useful in the treatment of neurological and mental diseases of formula (I), wherein A, n, R1 and R2 have the meanings specified in the des...
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WO/1993/021236A1 |
Photopolymerizable compositions containing photoinitiator systems that absorb in the visible are disclosed.
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WO/1993/020076A1 |
This invention provides compounds which are analogs to the hydrolysis transition-state of a cocaine benzoyl ester group. This invention also provides such analogs linked to carrier proteins, and antibodies thereto. This invention further...
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WO/1993/018033A1 |
Preparation of biologically active tropane derivatives of formula (1) and structural isomers thereof wherein R equals C1 to C8 alkyl and Ar is an aromatic ring moiety. The compounds are prepared by decomposing vinyl-diazomethanes in the ...
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WO/1993/015735A1 |
Invented is a method of preventing or delaying the occurrence of aquired immunodeficiency syndrome (AIDS) in human immunodeficiency virus (HIV) seropositive humans which comprises administering to such human an effective therefor amount ...
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WO/1993/015052A1 |
Compounds of formula (I) in which W is -CH2-, a bond, O or S; k is 0, or when W represents -CH2- k may also be 2, in which case the dotted lines represent single bonds; R is C1-8alkyl(phenyl)p, C2-8alkenyl(phenyl)p, C2-8alkynyl(phenyl)p,...
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WO/1993/012111A1 |
Compounds are provided for the preparation of reagents, including labels which can be used in immunoassays of cocaine and cocaine metabolites. The compounds are derivatives of cocaine which are conjugated to antigenic proteins or polypep...
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WO/1993/009814A1 |
Novel compounds show high affinity for specific cocaine receptors in the brain, particularly dopamine transporter sites, and have formula (I), wherein Y = CH2R3, CO2R2 or (II), R1 = hydrogen, C1-5 alkyl, R2 = hydrogen, C1-6 alkyl, C3-8 c...
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