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WO/2002/022623A1 |
Prochiral ketones are enantioselectively reduced to chiral secondary alcohols with a compound having the formula I: where, the two R¿2? groups are identical and are each a substituted or unsubstituted, aryl, alkyl, cycloalkyl or aralkyl...
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WO/2002/022557A2 |
The present invention relates to 2-amino-2-alkyl-4 heptenoic and heptynoic ac derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.
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WO/2002/023784A2 |
The present invention relates to compounds, compositions and methods for treating diseases associated with cysteine protease activity, particularly diseases associated with activity of cathepsins B, K, L or S.The present invention thus p...
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WO/2002/022622A2 |
One aspect of the present invention relates to 2-hydroxymethylglutamic acid and congeners thereof. A second aspect of the invention relates to a method of synthesizing 2-hydroxymethylglutamic acid and congeners thereof.
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WO/2002/020558A2 |
The invention concerns a method for binding, in solution, at least a peptide composition and at least a lipophilic vector bearing an aldehyde function, said coupling comprising a step which consists in producing a hydrazone bond between ...
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WO/2002/020462A1 |
Benzoic acid derivatives represented by the following general formula (I) and nontoxic salts thereof wherein R?1¿ represents COOH, COOR?6¿, etc.; A and B each represents a carbon ring or a heterocycle; R?2¿ represents alkyl, alkenyl, ...
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WO/2002/018331A1 |
The invention relates to benzoyl cyclohexane dione of general formula (I) wherein C?1¿, C?2¿, C?3¿ represent cyclic radicals; X?1¿ represents a heteroatom; X?2¿ represents a chain of carbon atoms; L represents a chain-shaped element...
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WO/2002/018354A1 |
Compounds of forumula (I) or therapeutically acceptable salts or prodrugs thereof, are useful for treating bacterial infections, psoriasis, arthritis, and toxicity due to chemotherapy. Preparation of the compounds, compositions containin...
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WO/2002/018355A1 |
Compounds represented by the following structural formula (I), and pharmaceutically acceptable salts, solvates and hydrates thereof, wherein R1 is an unsubstituted or substituted aryl, heteroaryl, cycloalkyl, aryl-alkyl, heteroaryl-alkyl...
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WO/2002/018353A2 |
Compounds of the formula (I) or therapeutically acceptable salts or prodrugs thereof, are useful for treating bacterial infections, psoriasis, arthritis, and toxicity due to chemotherapy. Preparation of the compounds, compositions contai...
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WO/2002/018391A1 |
A compound and method for producing an enantiomerically enriched epoxide from an olefin using a chiral ketone and an oxidizing agent is disclosed. In particular, the compound is of the formula: I wherein R?1¿, R?2¿, R?3¿ and R?4¿ are...
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WO/2002/016327A1 |
The invention provides novel compounds selected from the group consisting of formula (I) and (II). The compounds of the present invention are useful for the treatment and prevention of a variety of diseases and conditions associated with...
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WO/2002/016331A1 |
Compounds represented by the following structural formula (I), and pharmaceutically acceptable salts, solvates and hydrates thereof, wherein: n is 2, 3, or 4 and W is CH¿2?, CH(OH), C(O) or O; R1 is an unsubstituted or substituted aryl,...
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WO/2002/016332A1 |
Novel compounds that are modulators of PPAR receptors, and pharmaceutically acceptable salts, solvates and hydrates thereof, processes for making the compounds, pharmaceutical compositions containing the compounds, or pharmaceutically ac...
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WO/2002/014291A1 |
Compounds of the general formula (|) or salts thereof; and activators of PPAR$g(d) (peroxisome proliferator activated receptor $g(d)) containing the compounds or the salts as the active ingredient: (I) wherein R?1¿ and R?2¿ are each hy...
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WO/2002/014275A2 |
The present invention provides certain heterocyclic sulfonamide derivatives of formula (I): useful for potentiating glutamate receptor function in a patient and therefore, useful for treating a wide variety of conditions, such as psychia...
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WO/2002/014292A1 |
The invention provides a method of producing 5,5-dimethyloxazolidine-2, 4-dione including reacting $g(a)-hydroxyisobutyramide with di(lower alkyl) carbonate and an alkali metal alcoholate, to thereby produce a 5,5-dimethyloxazolidine-2, ...
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WO2001058869B1 |
Use of a compound for treating a respiratory disease in a mammal wherein the compound is a cannabinoid receptor modulator is disclosed. Compounds useful as cannabinoid receptor modulators for treating respiratory and non-respiratory leuk...
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WO/2002/014294A2 |
The present invention provides certain heterocyclic sulfonamide derivatives of formula (I): useful for potentiating glutamate receptor function in a patient and therefore, useful for treating a wide variety of conditions, such as psychia...
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WO/2002/014290A1 |
The invention provides scintillator molecules, consisting of one or more X moieties, which is a phosphor, covalently attached to one or more R?1¿ moieties which is a lipophilic or amphiphilic group, wherein the scintillator molecule is ...
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WO/2002/012184A1 |
The invention relates to (D)- or (L)-alpha-amino acids and their derivatives comprising phenylalanine or homophenylalanine having formula (I) or (II) and a process for the preparation thereof by stereoselective synthesis from aziridine h...
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WO/2002/012247A1 |
The invention relates to a method for the preparation of compound of formula (1). The invention further relates to the previously unknown compounds of formulas (5 and 6) as intermediates in the production of benzodiazepines of formula (1).
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WO/2002/010096A1 |
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/2002/010162A1 |
The present invention describes compounds of the formula: and enantiomers, diasteromers, solvates, and pharmaceutically acceptable salts thereof. The formula compounds are protein kinase inhibitors and are useful in the treatment of prol...
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WO/2002/009704A2 |
The invention concerns a pharmaceutical composition for transdermal delivery of befloxatone, capable of being in the form of gel, ointment or transdermal patch or a sprayed film. The invention is characterised in that it comprises at lea...
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WO/2002/009759A2 |
Combinations of aldosterone blockers an Cyclooxygenase-2 inhibitors useful in the treatment of inflammation are disclosed.
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WO/2002/010163A1 |
The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R, R?1¿, R?2¿, R?3...
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WO/2002/008197A1 |
The invention relates to novel biphenyl carboxamides of formula (I), wherein A, R, Z, X, Y, m and n have the meanings given in the description, to multiple methods for producing these substances, to their use for combating unwanted micro...
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WO/2002/006278A1 |
The present invention relates to certain substituted phenyl oxazolidinones and to processes for the synthesis of the same. This invention also relates to pharma-ceutical compositions containing the compounds of the present invention as a...
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WO/2002/006257A1 |
The invention relates to novel heterocyclic fluoroalkenyl thioethers of formula (I) wherein X represents hydrogen, halogen or alkyl; m represents whole numbers from 3 to 10; n represents 0, 1 or 2; Y represents sulphur or oxygen; R?1¿ r...
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WO/2002/006259A1 |
The invention relates to novel heterocyclic fluoralkenyl thioethers of formula (I) wherein m represents whole numbers from 3 to 10, n represents 0, 1 or 2, and Het represents the following respectively and optionally substituted grouping...
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WO/2002/006267A2 |
The present invention provides an efficient synthetic strategy for the preparation of analogs that incorporate important structural elements of the marine natural product curacin A, the compositions and various uses of the compositions. ...
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WO/2002/006276A1 |
The present invention relates to a $g(b)¿3? adrenergic receptor agonist of formula (I) or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Typ...
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WO/2002/006269A1 |
Novel compounds of formula (I), wherein R?1¿, R?2¿, R?2'¿, R?2''¿, R?3¿, R?4¿, R?5¿, R?5'¿, R?5''¿, R?5'''¿, R?5''''¿, X, Y, U, V and W have the meanings given in claim no.1, are inhibitors of the coagulation factors Xa and VI...
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WO/2002/006304A1 |
A process is described for the preparation of dipeptide derivatves having formula (I) characterized by reaction scheme (II).
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WO/2002/004409A2 |
This invention relates generally to tetrahydrobenzothiazole analogues and tetrahydrobenzooxyzole analogues, to pharmaceutical compositions which include these compounds and a pharmaceutically acceptable carrier, and to methods of treatme...
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WO/2002/002538A1 |
Amino acid-N-carboxy anhydrides having an N-acyl substituent at nitrogen which are represented by the following general formula (1); and a process for producing the same. These compounds easily react with free amino acids, alcohols or nu...
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WO/2002/002539A1 |
The present invention relates to novel heterocyclyl-containing diaryl sulfide compounds that are useful for treating inflammatory and immune diseases, to pharmaceutical compositions comprising these compounds, and to methods of inhibitin...
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WO/2002/002540A1 |
A benzoxazole compound represented by the following formula (I) wherein R1 to R4 may be the same or different and each represents hydrogen, C¿1-6? alkyl, C¿1-4? alkoxy, etc.; A represents single bond, CHR5-Y, CR5=CR6, CR5R7-CHR6, or CH...
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WO/2002/000612A1 |
A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or preventio...
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WO/2002/000601A1 |
An economically advantageous and industrially appropriate process for producing 3-amino-2-hydroxypropionic acid derivatives (1) without resort to any dangerous reagents characterized by comprising treating an N-protected-3-amino-2-hdyrox...
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WO/2002/000590A1 |
The invention is directed to the cross-metathesis and ring-closing metathesis reactions between geminal disubstituted olefins and terminal olefins, wherein the reaction employs a Ruthenium or Osmium metal carbene complex. Specifically, t...
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WO/2002/000200A1 |
The present invention relates to a novel process for preparing crystalline particles of a salt of a substance, particularly particles of therapeutically useful or carrier substances of a size suitable for inhalation therapy.
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WO/2001/097810A2 |
The invention relates to the use of therapeutic benzamide compounds of formula (I). As microsomal triglyceride transfer protein (MTP) inhibitors for treating obesity and post-prandial hyperlipemia.
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WO/2001/098297A2 |
The present invention provides a thiazine oxazolidinone useful as antimicrobial.
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WO/2001/096333A1 |
The invention relates to novel compounds of formula (I) in which A, B, W, G and Het have the same designation cited in the description. The invention also relates to several methods for the production of said new compounds and the use th...
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WO2001077107B1 |
A compound represented by formula (1) wherein m is 1 or 2, R<1> is a halogen or an optionally halogenated C1-2 alkyl; one of R<2> and R<3> is a hydrogen atom and the other is a group represented by formula (2) or (3) wherein n is 3 or 4;...
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WO/2001/096305A1 |
Compounds of formula (I) where R¿5?, R¿6a?, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.
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WO/2001/093840A2 |
The invention relates to the use of cyclic compounds as ligands of integrin receptors, in particular as ligands of the $g(a)¿v?ß¿3? integrin receptor. The invention also relates to the novel compounds, to the use thereof and to pharma...
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WO/2001/094321A1 |
Described are heterocycle-substituted cyclohexylamines of formula (I), and their pharmaceutically acceptable salts thereof. The compounds of formula (I) are antagonists of NMDA receptor channel complexes useful for treating cerebral vasc...
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