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WO/2003/064432A1 |
Intermediates for the total synthesis of ecteinascidins which are represented by the general formula (2) and bear the skeletal pentacyclic structure of ecteinascidins, characterized in that the 4-position OH group and trichloroethoxycarb...
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WO/2003/062192A1 |
Cycloalkyl ketoamide derivatives, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such cycloalkyl ketoamide derivatives as well as methods of using the same in the ...
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WO/2003/059864A2 |
Formula (I) compounds are described: Where the groups are as defined here below, and their use as medinies, particularly as serum glucose and serum lipid lowering agents. Said medicines are useful for the prophylaxis and treatment of dia...
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WO/2003/059339A1 |
Novel tricyclic−bis−enone derivatives (TBEs) as well as the process for the preparation of such TBEs are provided. Also provided are methods for prevention and&sol or treatment of cancer, Alzheimer's disease, Parkinson's disease, mul...
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WO/2003/059873A1 |
This invention relates to novel compounds characterized by the general Formula (I) any of its enantiomers or any mixture of its enantiomers, or a pharmaceutically acceptable salt thereof, or an N-oxide thereof, useful as potassium channe...
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WO/2003/059898A2 |
The present invention provides compounds having formula (I) : wherein R1-R6, A, J, D, E, G, Q, w, x, y, and z are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof,...
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WO/2003/060026A1 |
The invention provides water-soluble, β-hydroxy carbamate-functional materials and coating compositions, especially waterborne coating compositions, containing the carbamate-functional materials. The invention further provide a coating ...
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WO/2003/057169A2 |
The present invention pertains, at least in part, to novel substituted 4-dedimethylamino tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infect...
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WO/2003/053919A1 |
The present invention relates to compounds of formula (I) wherein A?1¿, A?2¿, A?3¿, A?4¿, A?5¿, A?6¿, A?7¿, A?8¿, A?9¿, A?10¿, U, V, W, m, n and p are as defined in the description and claims, and pharmaceutically acceptable sa...
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WO/2003/053885A1 |
The invention concerns a method for generating a carbon-carbon or carbon-heteroatom linkage by reacting an unsaturated compound bearing a leaving group and a nucleophilic compound. The invention also concerns generating a carbon-nitrogen...
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WO/2003/053916A1 |
The invention concerns a new process for preparing (S)-(+)-2-(substituted phenyl)-2-hydroxy-ethyl carbamates and to novel intermediates used in this process. It further relates to polymorphic forms of said carbamates and to processes for...
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WO/2003/051841A2 |
Carbamates and related compounds of formula R1 R2NCO-Y or R1 R2NCS-Y wherein R1 and R2 are hydrogen, alkyl, aryl, heteroaryl or may together form a piperidine, piperazine, morpholine or other heterocyclic ring, are inhibitors of hormone ...
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WO/2003/051842A2 |
Carbamates and related compounds of formula R1R2NCO-Y or R1R2NCS-Y wherein R1 and R2 may form a ring, are inhibitors of hormone sensitive lipase and are useful for the treatment of any disorder where it is desirable to modulate the plasm...
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WO/2003/050073A1 |
Disclosed are compounds of the formula (I) and the pharmaceutically acceptable salts thereof wherein the variables G, L, A, W, E, R2, R3, R4, R5, RN, and RC are defined herein. These compounds interact with and inhibit the activity of th...
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WO/2003/048101A1 |
The present invention provides compounds that are inducers or inhibitors of apoptosis or apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals wi...
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WO/2003/047740A2 |
Nonmetallic organic catalysts are provided that facilitate the enantioselective reaction of &agr ,β−unsaturated ketones. The catalysts are chiral imidazolidinone compounds having the structure of formula (IIA): or (IIB): or are acid a...
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WO/2003/048108A2 |
Novel acyl urea, thiourea, carbamate, thiocarbamate and related compounds are provided which are effective in inhibiting the cytokine−mediated inflammatory response in cultured cells, in ameliorating bone destruction, in an animal mode...
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WO/2003/047581A1 |
The invention provides compounds of formula (I) wherein m, n, A, R, R', R', R¿o?, X and Y are as defined in the description, and their preparation. The compounds of formula (I) are useful as pharmaceuticals in the treatment of e.g. nerv...
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WO/2003/045921A1 |
The present invention relates to a compound of the formula (I) wherein R?1¿ is optionally substituted aryl; R?2¿ is optionally substituted aryl, optionally substituted heteroaryl, optionally substituted lower cycloalkyl, optionally sub...
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WO/2003/045898A1 |
This invention relates to synthetic excitatory amino acid prodrugs of formula (I) wherein the residues R11, R12 and R13 are as defined in claim 1. The invention further relates to processes for the preparation of the compounds of formula...
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WO/2003/043974A2 |
Compounds of formula (I), wherein E, G, T, R¿d?, R¿e?, and R¿f? are as defined in claims, release levodopa and a COMT inhibitor so that they can be used for the treatment of diseases or conditions, wherein levodopa and inhibition of C...
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WO/2003/042150A1 |
Because of having an anti−arthritic effect, inhibiting bone fracture induced by arthritis and having a high safety, benzophenone derivatives represented by the following general formula or salts thereof are useful as remedies for arthr...
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WO/2003/040096A2 |
Disclosed are compounds of the formula (I), wherein the variables RN, RC, R1, R25, R2, and R3 are as defined herein. These compounds have activity as inhibitors of betasecretase and are therefore useful in treating a variety of discorder...
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WO2002048097A9 |
Compounds and pharmaceutical compositions useful as anti-parasitic agents, particularly in the treatment, prevention or amelioration of one or more symptoms of malaria or Chagas' disease, are provided. In particular, methods of modulatin...
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WO/2003/034989A2 |
Acylated $g(a)-hydroxyarylbutanamines and related sulfonamides, ureas and carbamates that inhibit aspartyl protease are disclosed, as are methods of treating diseases, particularly HIV, using these compounds. The compounds have the formu...
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WO/2003/032970A1 |
Compounds of formula (I) or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
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WO/2003/031393A2 |
The invention relates to compounds of the general formula (I), wherein Ar¿1?, Ar¿2?, R¿4?, R¿5?, R¿6?, R¿7?, R¿8?, W, X, a and b have the significances given in claim 1, and optionally the enantiomers thereof. The active ingredien...
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WO/2003/029190A1 |
Processes for the efficient production of chiral amino nitriles are disclosed. Generally, the processes include the esterification of the alcohol of an amino protected alcohol followed by nucleophilic substitution of the ester with a cya...
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WO/2003/029200A2 |
Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R¿1?, R¿2?, R¿3?, R¿4?, R¿5?, R¿6?, R¿8?, R¿9? and X aredefined herein. The compoundsare useful for treating autoi...
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WO/2003/027058A1 |
The invention relates to compounds of the general formula (I), as defined, and to pharmaceutical compositions containing them. The compounds of formula (I) are inhibitors of various lipid-related enzymes. They can be used in reducing acc...
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WO/2003/024402A2 |
The present invention relates to compounds according to formula (I) as disclosed herein as well as pharmaceutical compositions which include those compounds. Also disclosed are methods of using such compounds, which have activity as agon...
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WO/2003/024401A2 |
The present application describes modulators of CCR3 of formula (I) or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
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WO/2003/024439A1 |
The present invention relates to novel compounds of formula (I), to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of...
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WO/2003/024591A1 |
The invention relates to a process for the preparation of an active alumina catalyst impregnated with a base, which is chosen from alkali or alkaline earth metals and its synthetic applications. The catalyst has been used for the protect...
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WO/2003/022797A1 |
Carba−sugar amine derivatives represented by the general formula (1) or (2) are useful as active ingredients of β−galactosidase inhibitors or treating agents for disorder of glycolipid metabolism: (1) (2) wherein R1 and R2 are each ...
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WO/2003/020685A1 |
A fluorine compound represented by the general formula (1). It is effective in incorporating fluorine atoms into a compound having an active group such as an oxygenic functional group and is usable in applications such as surface treatme...
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WO/2003/020688A1 |
Compounds of formula (I) or therapeutically acceptable salts thereof, are selective protein tyrosine kinase-B (PTP1B) inhibitors. Preparation of the compounds, compositions containing the compounds, and treatment of disorders using the c...
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WO/2003/020684A1 |
The present invention describes immobilized haloenamine reagents, immobilized tertiary amides, methods for their preparation, and methods of use.
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WO/2003/018542A1 |
A norstatin derivative represented by the following general formula (I) or a salt thereof, which are useful as an intermediate for medicines, e.g., HIV protease inhibitors, bestatin and taxol as carcinostatic agents, and renin inhibitors...
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WO/2003/018535A2 |
The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compo...
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WO/2003/018538A1 |
A compound represented by the following general formula (1), etc. and analogues thereof, which selectively inhibit N−type calcium channels&semi and a remedy for pains, etc. which contains any of the compound and analogues. (1) [In the ...
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WO/2003/018552A2 |
The present invention is directed to protected amino acid halide monomers and oligomers, and to their use in the efficient sythesis of polyamides. The present invention is further directed to the use of -haloenamine reagents, which may o...
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WO/2003/014069A1 |
The present invention provides compounds of formula (1) R¿1?-HN-CH¿2?-CF¿2?-(CH¿2?)¿l?-CR¿3?R¿4?-CO-R¿2?, wherein: l is 0, 1 or 2; R¿1? is a labile amino protecting group, R¿2? is hydroxy group or the residue of an activated es...
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WO/2003/014076A2 |
Synthesis routes that can be adapted to large scale synthesis of oligoguanidine compounds such as oligoarginine compounds are described which use a perguanidinylation step to convert a group of $g(v)-amino groups to the corresponding gua...
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WO/2003/013502A1 |
Compounds which mimic the chemical and/or biological activity of discodermolide are provided.
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WO/2003/011799A1 |
One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing cataly...
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WO/2003/010134A1 |
Disclosed is a method for the production of 1,2,4-triaminobenzolecarbamic acid esters, characterized by the use of pyro- or polypyrocarbonate. The use of pyro- or polypyrocarbonate results in increased yields and increased purity of said...
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WO/2003/010089A1 |
The invention relates to a method for obtaining an ammonium carbamate solution from a gas mixture that contains more than 40 wt.% NH3, less than 50 wt.% CO2 and less than 40 wt.% H2O and has a pressure between 0.1 MPa and 4 MPa, comprisi...
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WO/2003/010148A1 |
The invention relates to novel pyrazoline derivatives of formula (I), in which R?1¿, R?2¿, R?3¿ and R?4¿ have the meanings as cited in the description, to a number of methods for producing these substances, to their use for controlli...
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WO/2003/010130A1 |
The present invention provides certain alpha-amino acids and derivatives thereof, such as, but not limited to, esters, amides and salts. The present invention also provides a novel method for the synthesis of alpha-amino acids and deriva...
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