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WO2004112793B1 |
A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to subjects. The compounds have the structure IA...
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WO/2005/007634A1 |
The present invention relates to the use of a compound of formula I as a coupling reagent in forming amide or ester bonds from a reaction between a carboxylic acid and an amine or an alcohol, respectively. The compounds of formula I are ...
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WO/2005/003104A2 |
The invention relates to lamotrigine (3,5-diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine) monohydrate (Ia) and anhydrous lamotrigine, and a process for preparing the same. An improved process is provided for manufacturing the lamotrigine ...
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WO/2004/108690A1 |
The invention provides pyrimidine, pyridazine and triazine compounds for use in therapy.
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WO/2004/096129A2 |
The present invention is directed to compounds which contain a heterocyclic triazine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containi...
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WO/2004/092125A2 |
Substituted alkylmetal reagents such as (trimethylsilylmethyl)lithium are reacted with azaaromatic compounds and/or nitrogen heterocycle compounds to produce functionalized azaaromatic compounds and functionalized nitrogen heterocycle co...
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WO/2004/082822A2 |
The invention includes methods for isolating crystalline Form I of 5-azacytidine substantially free of other forms, wherein 5-azacytidine is represented by the formula: The invention also includes pharmaceutical compositions comprising F...
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WO/2004/083191A1 |
The present invention relates to novel crystalline forms of lamotrigine, to processes for their preparation and pharmaceutical compositions containing them.
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WO/2004/074266A1 |
The present invention relates to HIV replication inhibitors of formula (I) as defined in the specification their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.
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WO/2004/072030A2 |
An improved process for the preparation of certain pyrrolotriazine compounds is disclosed. The compounds exhibit utility as kinase inhibitors.
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WO/2004/063166A1 |
The present invention is directed to compounds represented by the following structural formula, Formula I: wherein: (a) X is selected from the group consisting of a single bond, O, S, S(O)2 and N; (b) U is an aliphatic linker; (c) Y is s...
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WO/2004/063165A1 |
The present invention is directed to a compound, &lcub 2-Methyl-4-[3-methyl-1-(4-trifluoromethyl-phenyl)-1H-pyrazol
-4-ylmethylsulfanyl]-phenoxy&rcub -acetic acid and pharmaceutical uses thereof.
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WO/2004/058270A1 |
The present invention provides benzamide inhibitors of the P2X7 receptor of the formula (I), wherein R1 and R2 are as defined in claim 1. R3 is a nitrogen linked (C1-C10) heterocyclyl of formula (II), wherein R4 and R7 are as defined in ...
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WO/2004/050613A2 |
This invention provides 2-substituted-propenamide derivatives and their compositions for the treament of hepatitis B virus and/or hepatitis D virus.
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WO/2004/048348A1 |
The invention relates to substituted 2-aryl-1,2,4-triazine-3,5-di(thi)ones of general formula (I), in which Q1, Q2, R1, R2, R3, R4, R5 and R6 are defined as cited in the description, to a method for their production and to their use as h...
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WO/2004/041210A2 |
Quinoline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans.
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WO/2004/039767A1 |
The invention discloses a method for preparing the intermediate 2-(2,3-dichlorophenyl)-2-(aminoguanidine) acetonitrile of formula (II), which comprises the reaction of 2,3-dichlorobenzoyl cyanide with aminoguanidine bicarbonate in non-aq...
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WO/2004/032879A2 |
1,2,4-Triazin-5-ones useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
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WO/2004/034023A2 |
An improved method of producing 3-amino-1,2,4-benzotriazines using nitrobenzene or a derivative thereof, a guanidine salt and a base as reactants is provided. The method is carried out at a moderate reaction temperature without producing...
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WO/2004/030635A2 |
Compositions and methods and are provided for treating disorders associated with compromised vasculostasis. Invention methods and compositions are useful for treating a variety of disorders including for example, stroke, myocardial infar...
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WO/2004/026846A1 |
The present invention relates to DNA-targeted 1,2,4-benzotriazine- 1,4-dioxides and related analogues, to their preparation, and to their use as hypoxia-selective drugs and radiosensitizers for cancer therapy, both alone or in combinatio...
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WO/2004/026845A1 |
The present invention relates to a new process for the synthesis of high purity 3,5-diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine of formula (I) using 2,3-dichlorobenzoyl cyanide and an aminoguanidine salt as starting materials. 2,3-dich...
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WO/2004/007455A1 |
The invention relates to heterocyclically substituted benzoylureas, in addition to their physiologically compatible salts and physiologically functional derivatives. The invention relates in particular to compounds of formula (I), in whi...
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WO2003090912A9 |
Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.
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WO/2004/000215A2 |
In accordance with the present invention, there are provided novel chemical entities which have multiple utilities, e.g., as prodrugs of NSAIDs; as dual inhibitors of cyclooxygenase (COX) and 5-lipoxygenase (5-LO); as anticancer agents (...
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WO/2004/001058A2 |
Methods for identifying compound useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. In one embodiment, the method comprises contacting a microbial cell comprising: 1) a selectable marker un...
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WO/2003/104206A2 |
Compounds of formula (I), wherein Q is a group, (II), (III), (IV), (V), (VI) or (VII); Z is =N-, (VIII) or =C(R1)-; n is 0, 1, 2, 3 or 4; R1 and R2 are as defined in claim 1; R3 and R4 are each independently of the other hydrogen, haloge...
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WO/2003/101442A1 |
Novel PDF inhibitors and novel methods for their use are provided.
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WO/2003/101444A1 |
Disclosed are novel inhibitors of Chk-1 and methods of using the same for therapy.
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WO/2003/099818A1 |
A variety of low molecular weight, guanidino-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure of Formulas (IA), (IB), or...
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WO/2003/097645A1 |
The invention relates to novel 5-ethyl-imidazotriazinones, processes for their preparation and their use in medicaments, esp. for the treatment and/or prophylaxis of inflammatory processes and/or immune diseases.
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WO/2003/093270A1 |
The invention relates to novel 5-ethyl-imidazotriazinones, processes for their preparation and their use in medicaments, esp. for the treatment and/or prophylaxis of inflammatory processes and/or immune diseases.
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WO/2003/093268A1 |
The invention relates to novel 7-amino-imidazotriazinones, processes for their preparation and their use in medicaments, esp. for the treatment and/or prophylaxis of inflammatory processes and/or immune diseases.
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WO/2003/093242A2 |
The present invention relates to substituted 5-membered polycyclic compounds and prodrugs thereof, compositions and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and ...
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WO/2003/091229A1 |
Compounds having the formula (I), [chemical structure] and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are surprisingly advantageous as p38 kinase inhibitors, wherein R3 is hydrogen, methyl, perfluoromethyl, methox...
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WO/2003/087067A1 |
Compounds of formula (I) wherein Q is a group formula (II), (III); Z is=N-, formula (IV) or =C(R2)-; n is 0, 1, 2 or 3; R3 or R4 are each independently of the other hydrogen, alogen, -CN, C1-C4alkyl or C1-C4alkoxyl; or R3 and R4 together...
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WO/2003/084927A1 |
Haloalkenes represented by the general formula (I) which are useful as pest controllers: (I) wherein X1 and X2 are each halogeno; Y is hydrogen or halogeno; n is 0 to 5; and Q is (1) a heterocyclic group selected from among thienyl, fury...
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WO/2003/082861A2 |
Compounds of formula (I) wherein: R1 represents substituted or unsubstituted heteroaryl; Y represents -(CRnaRnb)n-; Rna and Rnb are each independently hydrogen or C1-6alkyl; n is an integer from 0 to 5;R2 represents unsubstituted or subs...
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WO/2003/077828A2 |
The present invention relates to novel florfenicol compounds having the chemical structure (I) wherein the compounds are useful for the treatment and/or prevention of bacterial infections in a broad range of patients such as, without lim...
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WO/2003/078376A1 |
A NK1 antagonist having the formula (I), with the variables defined herein, which is useful for treating a number of disorders, including emesis, depression, anxiety and cough.
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WO/2003/078407A1 |
A process for the manufacture of 3,5-diamino-kgg6-substituted-1,2,4-triazines is disclosed which comprises the steps of: (a) reacting a compound of formula (II): with aminoguanidine salts, (b) dehydrating the compound obtained to form a ...
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WO/2003/070709A1 |
The following phenylalanine derivative having an &agr 4 integrin inhibitory effect, its analogs and remedies for various diseases in which &agr 4 integrin participates.
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WO/2003/064369A1 |
It is intended to provide compounds represented by the following general formula (I) which have a high affinity for human thyroid hormone receptors, in particular, human thyroid hormone receptor β, medicinal compositions containing the ...
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WO/2003/062228A1 |
The present invention discloses novel compounds of Formula I which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprisi...
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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/2003/042191A1 |
The present invention relates to novel to P2X7 inhibitors of formula (I) and to processes for their preparation, intermediates useful in their preparation, pharmaceutical compositions containing them, and their use in therapy. The active...
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WO/2003/042192A1 |
Industrially applicable process for preparing 3-amino-1,2,4-benzotriazine 1,4-dioxide.
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WO/2003/042190A1 |
The present invention relates to novel to N-alkyl adamantyl triazinyl benzylamide derivatives of formula (I) and to process for their preparation, intermediates useful in their preparation, pharmaceutical compositions containing them, an...
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WO/2003/033476A1 |
A compound of formula (Ia) comprising a pharmaceutically acceptable salt or solvate thereof, formulations, processes of preparing, and methods of administering to mammals are provided
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