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WO/1999/052908A1 |
An efficient method for the synthesis of a compound of formula (2) is disclosed which comprises reacting a 4-acyl-2-azetidinone with a titanium, zirconium or hafnium enolate of a 1-hydroxy-2-butanone derivative.
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WO/1999/043648A1 |
Cyclic amino compounds represented by general formula (I) or pharmacologically acceptable salts thereof having an excellent antiplatelet aggregation effect, etc. and thus being useful as preventives or remedies for embolism, thrombosis o...
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WO/1999/043647A1 |
The invention relates to a compound having formula (I) wherein A is an optionally unsaturated 5- or 6-membered ring, which may comprise a heteroatom selected from N, O and S and which may be substituted with oxo or (1-6C)alkyl; R?1¿, R?...
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WO/1999/042435A2 |
The invention relates to compounds of general formula (A), where R is COOH, COOR?1¿, CH¿2?-OH, C(=O)NR?2¿R?3¿, CN, CH¿2?NR?2¿R?3¿, C(=O)-Z, CH¿2?-Z, or a substituent in accordance with formula (C), R?4¿ is COOH, COOR?1¿, CH¿2?...
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WO/1999/037613A1 |
A compound of formula (1), wherein R?1¿ is aryl; and R?2¿ is hydrogen or alkyl; pharmaceutically acceptable addition compounds thereof; and their use in therapy, particularly for the treatment and prophylaxis of CNS disorders such as a...
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WO/1999/037614A1 |
A compound of formula (1) wherein R?1¿ is aryl; and R?2¿, R?3¿, R?4¿, R?5¿ and R?6¿ which may be the same or different are selected from H, alkyl and aryl; pharmaceutically acceptable addition compounds thereof; and the use of the ...
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WO/1999/037612A1 |
A compound of formula (1), wherein: R?1¿ is aryl; R?2¿ is H, alkyl or aryl; and R?3¿ is hydrogen or alkyl; pharmaceutically acceptable addition compounds thereof; and the use of the compounds in therapy, particularly for the treatment...
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WO1999019297A9 |
The present invention provides compound having formula (I) useful as building blocks for combinatorial libraries and methods of making such compounds. Also provided are compositions comprising the compounds.
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WO/1999/029667A1 |
Compounds of formula (I) or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH¿...
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WO/1999/018073A1 |
A compound of formula (I) wherein R¿1? is hydrogen, methyl, ethyl, methoxy or methylthio; R¿2? and R¿3? each independently is hydrogen or C¿1-3? alkyl; R¿4? is hydrogen, lower alkyl, methoxy, ethoxy, or benzyloxy; R¿5? is lower alk...
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WO/1999/018074A1 |
The present application describes novel lactams and derivatives thereof of formula (I), or pharmaceutically acceptable salt forms thereof, wherein ring B is a 4-8 membered cyclic amide containing from 0-3 additional heteroatoms selected ...
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WO/1999/018072A1 |
A compound of formula (I) wherein R?1¿ is hydrogen, methyl, ethyl, methoxy or methylthio; R?2¿ and R?3¿ each independently is hydrogen or lower alkyl; R?4¿ is hydrogen, lower alkyl, methoxy, ethoxy or benzyloxy; R?5¿ is lower alkyl,...
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WO/1999/018071A1 |
A compound of formula (1) wherein Y is S or O; R¿1? is C¿1-6? alkyl; (C¿0-6? alkyl)aryl; (C¿0-6? alkyl)Het; or R¿1? is an amino acid analog or dipeptide analog of formula (I) wherein R¿2? is H, C¿1-10? alkyl; or an amide or ester ...
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WO1998050032A9 |
This invention relates to a novel method for treating disease or disorders mediated by the lipid inflammatory mediators, arachidonic acid, its metabolites and/or platelet activating factor (PAF), which method comprising administering to ...
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WO/1999/012931A1 |
According to the invention are provided compounds of formula (I) (relative stereochemistry indicated) wherein R?1¿, R?2¿ and R?3¿ are as defined in the specification. Compounds of formula (I) are useful $i(inter alia) in the treatment...
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WO/1999/010323A1 |
The instant invention relates to a compound of formula (I) wherein R?a¿ and P are: (a) hydrogen, (b) methyl, or (c) a hydroxy protecting group and an efficient process for its synthesis.
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WO/1999/005091A1 |
A novel cystacycline derivative which has an excellent effect of promoting the differentiation of neurons and is useful as a remedy for central nervous system disorders, a remedy for peripheral nerve disorders, etc.
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WO/1999/005093A1 |
The invention relates to compounds with general formula (I) in wchich A is a group having formula (a) or (b), and Z is an O or S atom. The invention also relates to their further processing to form new secondary amidoalkyl carbonic acid ...
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WO/1999/003459A1 |
Anti-pruritic pharmaceutical formulations containing kappa agonist compounds and methods of prevention or treatment of pruritus in a mammal with the anti-pruritic formulations.
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WO/1999/001451A1 |
Compounds of formula (I) and pharmaceutically acceptable salts thereof are useful as tachykinin inhibitors which act at the NK¿1?, NK¿2? and NK¿3? receptors or a combination of two or more thereof. In said formula (I) A is CO, SO¿2? ...
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WO/1999/000356A1 |
This invention relates to compounds of formula (I) which inhibit Factor Xa, to pharmaceutical compositions containing the compounds, and to the use of the compounds for the treatment of patients suffering from conditions which can be ame...
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WO/1998/058934A1 |
The invention concerns novel 2-(iminomethyl)amino-phenyl derivatives, their preparation, their application as medicines and compositions containing them.
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WO/1998/057932A1 |
There is provided compounds of formula (I), wherein R?1�, R�x?, Y, R?y�, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in th...
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WO/1998/057639A1 |
This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha la adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia...
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WO/1998/051298A1 |
This invention relates to a series of arylsubstituted piperazines, of Formula (I), pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the...
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WO/1998/050031A1 |
Compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R�1? is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L�2?-, and (i) heterocyclic -L�2?-;...
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WO/1998/050029A1 |
Compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R�1? is (a) hydrogen, (b) lower alkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl -L�2?-, and (i) heterocyclic -L�2?...
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WO/1998/049897A1 |
This invention relates to a method of treating or reducing cell proliferation in a mammal in need thereof, which comprises administering to said mammal an effective CoA-independent transacylase (CoA-IT) inhibiting amount of a compound of...
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WO/1998/050030A1 |
Compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R�1? is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L�2?-, and (i) heterocyclic-L�2?-; ...
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WO/1998/047867A1 |
Efficient and economical processes for producing azetidine-2-carboxylic acid and intermediates thereof on an industrial scale. Azetidine-2-carboxylic acid of structural formula (5) is produced by reducing a 4-oxo-2-azetidinecarboxylic ac...
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WO/1998/045260A1 |
The present invention relates to a process for stereoselective preparation of (3S,4S)-3- [(1R)-hydroxyethyl]-4-acyl-1-p-methoxyphenyl-2-azetidinone which is a useful intermediate for preparing carbapenem and penem type antibiotics.
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WO/1998/033768A1 |
A compound of formula (I) wherein R?1�, R?2� and Q are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, macular degeneration, restenosis, periodontal...
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WO/1998/031666A1 |
A process of synthesizing a compound of formula (1) is described, wherein P and P' independently represent H or a protecting group, R?1¿ represents H or C¿1-4? alkyl, and Hal represents a halogen selected from C1, Br and I.
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WO/1998/030540A1 |
An efficient method for the quantitative preparation and isolation of a compound of formula (I) or its enantiomer, a chiral mediator used in enantioselective synthesis.
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WO/1998/025895A1 |
This invention is directed to novel azetidinone compounds, to certain intermediates and processes for preparing these azetidinone compounds, and to formulations containing the same. The present invention also relates to the use of these ...
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WO/1998/025920A1 |
The present invention relates to a method of controlling pain in mammals, including humans, comprising administering to a mammal or patient in need of treatment thereof selected compounds of formula (I) or a pharmaceutically acceptable s...
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WO/1998/024784A1 |
The compounds of formula (I) exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, the...
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WO/1998/022432A1 |
Acylamino-substituted acylanilide derivatives represented by general formula (I) or salts thereof, and a pharmaceutical composition comprising the same. They have an antiandrogenic activity and are useful as a prophylactic or therapeutic...
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WO/1998/012176A1 |
The present invention is based on the discovery that certain 3,4-disubstituted-azetidin-2-one derivatives exhibit excellent cysteine proteinase inhibitory activity which can be used for treatment of different diseases such as muscular dy...
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WO/1998/008811A1 |
Cyclic amine derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, excellent in the effect of inhibiting platelet aggregation and useful as a preventive or remedy for embolism, thrombosis or arteri...
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WO/1998/007690A1 |
The present invention relates to a process for stereoselective preparation of (3R,4R)-4-acetoxy-3-{[(1'R)-1'-t-butyldimethylsilyloxy]ethyl
}-2-azetidinone (I) which is a useful intermediate for preparing carbapenem and penem type $g(b)-l...
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WO/1998/007691A1 |
The present invention relates to a process for stereoselective preparation of (3S,4S)-3-[(1'R)-1'-hydroxyethyl]-4-alkoxycarbonyl-2-azetidi
none (I) which is a useful intermediate for preparing carbaphenem and phenem type $g(b)-lactam ant...
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WO/1998/007420A1 |
There are disclosed novel neuropeptide Y ligands having general formula (I) wherein the symbols W, A, D, R?1�, R?2�, R?3�, R?4� are further defined in the description. Compounds of formula (I) are agonists and antagonists of neur...
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WO/1998/002568A1 |
There is provided a process for obtaining an enantiomerically enriched $i(N)-acylazetidine-2-carboxylic acid, which process compri ses the biotransformation of a racemic $i(N)-acylazetidine-2-carb oxylic acid ester with an enzyme that di...
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WO/1998/002417A1 |
There is provided a process for obtaining an enantiomerically enriched $i(N)-acylazetidine-2-carboxylic acid, which comprises the selective crystallisation of a diastereoisomeric salt formed between the required enantiomer of the $i(N)-a...
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WO/1997/049404A1 |
This invention relates to a compound of formula (I) X-C(O)-Y-G-R (wherein X, Y, G and R have the values defined in the description), or a pharmaceutically acceptable salt thereof, processes and intermediates for the preparation of such a...
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WO/1997/047621A1 |
The invention provides a process for the preparation of compounds of formula (I) wherein R1, R2, R3 R4 and R5 are as defined in the specification; and wherein any functional groups are optionally protected; and salts thereof; which proce...
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WO/1997/047194A1 |
Compounds represented by formula (I), and pharmaceutically acceptacle salts thereof; and their method of preparation are provided. Compounds of the above formula are influenza virus neuraminidase inhibitors and can be used in treating pa...
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WO/1997/046577A1 |
There is provided compounds of formula (I), wherein R1, R2, R3, Rx, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatm...
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WO/1997/045406A1 |
The invention relates to a process for producing a compound of formula (I) wherein R1, R2 and R3 are as defined in the specification, which comprises reacting a lactone with an imine to obtain a chiral diol of formula (IV) oxidizing the ...
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