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WO/2009/093009A1 |
A series of fused tricyclic thiophene derivatives, which are substituted in the 2-position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in t...
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WO/2009/069147A2 |
An improved process for preparation of triazol-benzodiazepine derivatives, such as alprazolam, triazolam, brotizolam and etizolam, is presented. The process comprises a cyclization reaction of compound Formula (B) in toluene with catalyt...
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WO/2009/052288A1 |
The present invention relates to compounds of Formula (I), below, (wherein X, R1, R2, R3, p, E, ring A, and ring B are as defined herein). The present invention also relates to compositions (including pharmaceutically acceptable composit...
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WO/2009/010785A1 |
A class of macrocyclic compounds of formula (I), wherein R7,A,Ar, B,D, F, M, Q1, Q2, W, X, Y and Z are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided....
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WO/2009/010783A1 |
A class of macrocyclic compounds of formula (I), wherein R7, R9, B, F, M, Q, W, Y and Z are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also provi...
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WO/2008/140420A2 |
The present invention relates to pyrimidine compounds that are useful as agents for the treatment of kinase related disorders such as proliferative disorders. More particularly, the present invention relates to substituted pyrimidine com...
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WO/2008/115381A1 |
In its many embodiments, the present invention provides -substituted pyridazinone compounds as glucan synthase inhibitors, methods of preparing such compounds, pharmaceutical including one or more of such compounds, methods of preparing ...
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WO/2008/105526A1 |
Disclosed is a new class of compound which has HSP90 inhibitory activity and is useful as an antitumor agent or the like. Also disclosed is a compound which is useful as a synthesis intermediate for the compound having HSP90 inhibitory a...
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WO/2008/101665A1 |
The present application describes macrocyclic compounds of formula (I) with NS3 protease inhibitory activity for treating hepatitis C virus infection.
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WO/2008/075103A1 |
Compounds of the formula (I) wherein A, B, D, M, Ar, W, X, Y, Z and R1 are as defined herein, are useful in the prevention and treatment of hepatitis C infections. The compounds, their preparation, pharmaceutical compositions containing ...
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WO/2008/007661A1 |
Disclosed is a tricyclic heterocyclic compound having a serotonin 5-HT2C receptor activating effect and the like. Specifically disclosed is a serotonin 5-HT2C receptor activator containing a compound represented by the formula (I) below,...
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WO/2007/136746A2 |
Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where, p, q, K, L, W, V, R2, R3, R...
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WO/2007/095389A2 |
The invention relates to N-oxides of camptothecin analogs having activity for treating hyperproliferative disorders. Pharmaceutical compositions comprising therapeutically effective amount of camptothecin analog N-oxides and bis N-oxides...
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WO/2007/092641A2 |
Methods for preparing compounds of the Formulas IV and I are disclosed. The methods include combining a compound of the Formula II: with a benzylamine of the Formula III: in the presence of an acid to provide a 1H-imidazo[4,5-c]pyridine ...
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WO/2007/075194A1 |
The present invention provides, among other things, new benzylamine compounds, compositions comprising benzylamine compounds, methods of making benzylamine compounds, and methods of using benzylamine compounds for treating or preventing ...
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WO/2007/007399A1 |
Compounds having an anti-MRSA activity and having a skeleton and action mechanism different from those of existing drugs, which are useful as a novel antimicrobial agent. Conventionally, vancomycin is used as a drug for MRSA. However, re...
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WO/2006/130673A1 |
The present invention is directed to novel 3-benzoimidazolyl-pyrazolopyridine compounds of formula (I): and pharmaceutically acceptable forms thereof and their synthesis and use as inhibitors of serine-threonine protein kinases and tyros...
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WO/2006/103088A1 |
The present invention relates to novel hydroxyethylamine and ketone compounds having Asp2 (β-secretase, BACE1 or Memapsin-2) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the t...
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WO/2006/088191A1 |
An eudistomin derivative represented by the general formula (I) or a salt thereof or a hydrate or solvate thereof which has anti-viral effect against viruses including hepatisis C virus: (I) wherein R represents an alkyl group which may ...
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WO/2006/050435A1 |
NLO chromophores of the form of Formula (I) and the acceptable salts, solvates and hydrates thereof, wherein Z, X1-4, &pgr 1-2, D and A have the definitions provided herein.
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WO/2005/090357A1 |
This invention relates to benzopyran derivatives of formula (I) or (II), or pharmaceutically acceptable salts thereof wherein R1 and R2 are independently of each other hydrogen atom, C1-6alkyl group or C6-14aryl group, R3 is hydrogen ato...
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WO/2005/058231A2 |
The present invention features rifamycin analogs that can be used as therapeutics for treatics or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form,...
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WO/2005/049735A2 |
The present invention is directed to an aqueous process for reducing particle size of organic pigments by milling the crude pigment in the presence of a water soluble styrene copolymer dispersants, optionally a defoamer, optionally an ad...
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WO/2004/108090A2 |
Oxycodone is manufactured in high yields and with a high purity using 5 codeine or a salt of codeine as the starting material. The manufacturing process involves the following steps: (a) codeine or a codeine salt (e.g., codeine phosphate...
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WO/2004/094371A2 |
The present invention is directed to compounds of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X, n and the broken lines are as defined herein which are useful as modulators of chemokine receptor activity. In particular, thes...
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WO/2004/089936A1 |
A novel heteroarylsulfonanilide derivative represented by the general formula [I]. It has potent ß3 receptor-stimulating activity, shows excellent selectivity, and is useful as a ß3 adrenergic receptor agonist having excellent pharmaco...
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WO/2004/069843A1 |
The invention relates to compounds of formula (I), where (a) is a benzyl or pyridyl group, optionally fused at position ( 2-3, 3-4, or 4-5), and optionally substituted, (W) is a X-Y or Y-X group, where (X) is a group (b) and (Y) is an ox...
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WO/2004/069844A1 |
The invention relates to compounds of formula (I) wherein (A) and (B) each represent an optionally-substituted benzyl or pyridyl group, W is (b1) or (b2), Y is (CH2)n or an alkenyl or alkynyl group, n is zero or a whole number such that ...
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WO/2004/054504A2 |
Aminocyanopyridine compounds are described which are capable of inhibiting mitogen activated protein kinase-activated protein kinase-2. Pharmaceutical compositions and kits are also described, which include an anminocyanopyridine MK-2 in...
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WO/2004/039809A1 |
Quinoxaline derivatives represented by the general formula (I) or pharmaceutically acceptable salts or esters thereof: (I) wherein X is NH, S, or the like; Y is O or the like; the group represented by the general formula (II): (II) is, e...
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WO/2004/028454A2 |
The present invention provides compounds and methods for treatment of viral diseases and cancer.
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WO/2004/020443A1 |
A method for manufacturing hydrogen sulphate (alpha S) of the alpha-(2-chlorophenyl)-6,7dihydro-thieno[3,2-c]pyridine-5(
4H)-acetic acid methyl ester (clopidogrel hydrogen sulphate) of formula I, in crystalline Form I, wherein the comp...
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WO/2003/066638A2 |
Ecteinascidin compounds with a quinone ring for ring E are active as anti−cancer agents. Related processes and compounds are provided.
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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/2003/051362A2 |
Provided are new crystalline Forms III, IV, V and VI of clopidogrel hydrogensulfate and the amorphous form of clopidogrel hydrogensulfate, as well as their pharmaceutical compositions, and method of treatments with such compositions. Als...
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WO/2003/039571A1 |
Improved dosing schedules for ecteinascidin 743 are given for treatment of cancer.
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WO/2003/032999A1 |
A compound of Formula (I) or a pharmaceutical acceptable salt thereof, or a tautomer thereof, wherein G¿1?, G¿2?, and B are as defined in the application, are selective inhibitors of MMP-13. The compounds are useful for treating diseas...
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WO/2003/025017A1 |
A crystalline composition comprising a crystal of the IL-6 receptor I chain is provided. Also provided are methods of using the crystal and related structural information to screen for and design compounds that interact with IL-6R, or va...
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WO/2003/020731A1 |
The invention relates to novel substituted, annelated indole and heteroindole derivatives of general formula (I), to tautomers, stereoisomers, mixtures and pharmaceutically acceptable salts thereof and to the production and use thereof a...
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WO/2003/014127A1 |
Derivatives of ecteinascidin 736 of general formula (I) wherein the groups R¿1?, R¿2?, R¿3?, R¿4? and R¿5? are each independently selected from the group consisting of H, OH, OR', SH, SR', SOR', SO¿2?R', C(=O)R', C(=O)OR', NO¿2?, ...
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WO/2003/008423A1 |
Derivatives of Et-743 or Et-770 or Et-729 are provided. The derivatives are of the general formula (Ia) wherein the substituent groups take various permitted meanings.
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WO/2002/100865A1 |
The present invention relates to benzoxazepine derivative having the general formula I, wherein X represents CO or SO¿2?; R?1¿, R?2¿, R?3¿ and R?4¿ are independently selected from H, (C¿1-4?)alkyl, (C¿1-4?)alkyloxy, (C¿1-4?)alkyl...
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WO/2002/064843A1 |
The present invention provides a bacterial symbiont of Ecteinascidia turbinata, and methods for the synthesis of an ecteinascidin.
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WO/2002/046197A1 |
This invention is directed to macroheterocyclic compounds useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.
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WO/2002/028865A2 |
Compounds of general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents._In particular, the invention relates to compounds that are potent and selective inhibitors of cyclic guanosine 3'...
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WO/2002/020015A1 |
The present invention is directed to piperidine- and pyrrolidine-containing macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherape...
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WO/2001/087894A1 |
Antitumour compounds have the five membered fused ring ecteinascidin structure of the formula (XIV). The present compounds lack a 1,4-bridging group as found in the ecteinascidins. They have at the C-1 position a substituent selected fro...
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WO/2001/087895A1 |
Processes are provided for preparing compounds with a fused ring structure of formula (XIV). Such products include ecteinascidins and have a spiroamine-1,4-bridge. The process involving forming a 1,4 bridge using a l-labile, 10-hydroxy, ...
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WO/2001/077114A1 |
The present invention is directed to peptidomimetic macrocyclic compounds that inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions contain...
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WO/2001/077115A1 |
Compounds having a fused ecteinascidin five ring system with a 1,4 bridge having the structure of formula (VIa or VIb) and compounds in which the -NH¿2? or -OH of the 1,4 bridge is derivatised are disclosed. Such compounds are useful in...
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