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WO/2010/010435A2 |
The present invention provides fused oxazole and thiazole derivatives as TRPM8 (Transient Receptor Potential subfamily M, member 8) modulators. In particular, compounds described herein are useful for treating diseases, disorders, condit...
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WO/2010/010014A1 |
The invention relates to compounds of formula(I) wherein R1 is hydrogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, halogen, cyano, nitro, hydroxy, C(O)O-lower alkyl, S(O)2-lower a...
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WO/2010/008522A2 |
Iodylbenzene derivatives substituted with electron donating as well as electron withdrawing groups on the aromatic ring are used as precursors in aromatic nucleophilic substitution reactions. The iodyl group (IO2) is regiospecifically su...
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WO/2010/004228A2 |
The invention relates to a novel discriminating molecule family for neutron and gamma radiation and to the preparation method thereof. Said molecules are also useful for detecting radiation (X, gamma, electrons, protons, ions), and thus ...
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WO/2010/002209A2 |
This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The...
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WO/2009/157019A2 |
The present invention provides an efficient and industrially advantageous process for the preparation of ezetimibe of formula (I), using novel intermediates.
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WO/2009/154785A2 |
The invention provides a series of C4-substituted oxazole compounds having an alpha keto side chain at the 2 position, for example, compounds of formula I. The compounds can inhibit fatty acid amide hydrolase and can be useful for treatm...
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WO/2009/153238A1 |
The present invention relates to aminothiazoline compounds of the general formula (I): wherein A is a radical of the formulae A1 or A2: wherein * denotes the binding site and wherein the indices and variables are as defined in the descri...
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WO/2009/149508A1 |
The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the tr...
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WO/2009/101082A9 |
The present invention relates to the use of substituted sulfonic acid amide compounds of formula I, wherein Ra, n, Het, A, Y and D are as defined in the claims and the N-oxides and the salts thereof for combating phytopathogenic harmful ...
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WO/2009/140932A2 |
Method of producing (3R,4S)1 -(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3- hydroxypropyl)]-4-(4-hydroxyphenyl)-2-azetidinone (ezetimibe) of formula 1, in which alcohol-oxazolidide of general formula II, wherein PG is a phenol protectin...
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WO/2009/139373A1 |
Disclosed is a compound useful as an active ingredient of a pharmaceutical composition, such as a pharmaceutical composition for treating chronic renal failure and/or diabetic nephropathy. Extensive studies are made for the purpose of fi...
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WO/2009/137340A1 |
Described herein are compounds that can be useful as bioactive agents. More specifically, the compounds described herein can be useful as both α2B and α2c adrenergic agonists. Methods of synthesis and administration of the compounds ar...
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WO/2009/135526A1 |
Substituted amides of the general formula (I): with the residues A, R1 and R2 as explained in detail in the description are described. The compounds are suitable in particular as neutral endopeptidase inhibitors and are highly potent.
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WO/2009/132740A2 |
The invention relates to reactive ionic liquids comprising organic cations with electrochemically reducible groups or substituents and anions of fluoroalkyl phosphates, fluoroalkyl phosphinates, fluoroalkyl phosphonates, acetates, trifla...
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WO/2009/132119A2 |
The present invention relates to new oxazolidinone modulators of skeletal muscle function and tone, pharmaceutical compositions thereof, and methods of use thereof.
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WO/2009/129953A1 |
The invention relates to 2-(benzylsulfonyl)-oxazole derivatives, chiral 2-(benzylsulfinyl)-oxazole derivatives and 2-(benzylsulfanyl)-oxazole derivatives of general formula (I) and the salts thereof, wherein the individual radicals and i...
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WO/2009/127338A1 |
The present invention relates to novel carboxylic acid derivates of the formula (I), having an oxo-substituted azaheterocyclic partial structure, method for the production thereof, use thereof for treating and/or preventing illnesses and...
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WO/2009/129097A1 |
Provided is a process for the formation of nitrated compounds by the nitration of hydrocarbon compounds with dilute nitric acid. Also provided are processes for preparing industrially useful downstream derivatives of the nitrated compoun...
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WO/2009/129267A2 |
Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.
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WO/2009/123316A1 |
Disclosed is an sGC activator, particularly a compound which is useful for the prevention or treatment of diseases including hypertension, ischemic heart diseases, heart failure, kidney diseases, arteriosclerotic diseases, atrial fibrill...
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WO/2009/123241A1 |
Disclosed is a novel compound having an inhibitory activity on a plasminogen activator inhibitor-1 (PAI-1). Also disclosed is a PAI-1 inhibitor comprising the compound as an active ingredient. Further disclosed is a pharmaceutical compos...
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WO/2009/123164A1 |
Disclosed is a compound useful as an endothelial lipase inhibitor. Specifically disclosed is a compound represented by the formula, a pharmaceutically acceptable salt thereof, or a solvate of the compound or the pharmaceutically acceptab...
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WO/2009/115491A1 |
The present invention relates to azolin-2-ylamino compounds of formulae (I) and (II), wherein n is 0 to 3; Ar is phenyl; A is a radical of formulae A1 or A2, wherein * indicates the point of attachment; X is S, O or N(R10); R7a-d are H, ...
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WO/2009/117109A1 |
This invention relates to novel compounds of the Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation...
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WO/2009/113320A1 |
Provided is a new compound with excellent MMP inhibitory effect and reduced side-effects. The compound is a matrix metalloproteinase inhibitor with, as an active ingredient, the hydroxamic acid derivative represented by general formula (...
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WO/2009/106021A1 |
A method for the preparation of (S)-alcohol oxazolidides of general formula II, in which PG represents hydrogen or a hydroxyl protecting group, such as trimethylsilyl, tert-butyldimethylsilyl, benzyloxycarbonyl, tert-butoxycarbonyl, benz...
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WO/2009/105214A2 |
This invention provides compounds of formulas H, Ia, H, and or salts thereof, pharmaceutical compositions comprising a compound of formulas H, Ia, H and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor...
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WO/2009/103626A1 |
The present invention relates to a compounds of formula I or a pharmaceutically active acid addition salts thereof. It has been found that the present compounds have Asp2 (β-sccretasc, BACE 1 or Mcmapsin-2) inhibitory activity and that ...
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WO/2009/098455A1 |
The present invention relates to M3 antagonists of formula (I):wherein R1, R2, R3, R4, R5, R6, R8 and A are as defined herein; pharmaceutical compositions containing them; methods for their preparation; and their use in the treatment of ...
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WO/2009/092324A1 |
The present invention provides therapeutically active oxazolidine derivatives and compositions as NMDA antagonists, which are useful in preventing and treating central nervous system disorders by inhibiting over-activation of NMDA recept...
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WO/2009/090177A1 |
The present invention relates to bifeprunox derivatives of the formula (I) wherein R1 is one substituent selected from 3-OH, 4-OH, 3-OSO3H and 4-OSO3H; R2 is H; or an N-oxide or a pharmaceutically acceptable salt, a solvate or hydrate th...
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WO/2009/085637A1 |
The present invention provides various amorphous forms of the compound metaxalone (I), such as solid amorphous metaxalone and amorphous dispersions comprising metaxalone. The present invention further provides pharmaceutical compositions...
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WO/2009/080446A1 |
The object of the invention is a chemical compound of the general formula (I) or (II), where X = O or NR and R = H, an optionally branched C1-C6-alkyl, C3-C6-cycloalkyl, aryl, in particular phenyl, or aralkyl, in particular benzyl, and w...
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WO/2009/080788A2 |
The application concerns compounds for use as antibacterial agents, processes for their preparation, and compositions comprising said agents, wherein said compounds have formula (VI) and r, p, R1, R2, R3 and R4 have defined meanings.
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WO/2009/078694A1 |
The invention relates to formulations comprising an asphaltene-dispersing/-inhibiting additive based on oxazolidines derived from polyalkyl or polyalkenyl N-hydroxyalkyl succinimides. Said formulations can contain: inert organic solvents...
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WO/2009/079593A1 |
The present invention is directed to piperidinyl and piperazinyl derivatives of formula (I) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compoun...
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WO/2009/078813A1 |
A process is provided for the synthesis of 4,5-diamino cyclohexene carboxylate ester (1): or a pharmaceutically acceptable salt thereof. R1 - R3 are a silyl-, an aliphatic, alicyclic, aromatic, arylaliphatic, or an arylalicyclic group. R...
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WO/2009/079597A1 |
The present invention is directed to piperidinyl and piperazinyl derivatives of formula (II) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compou...
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WO/2009/075080A1 |
Disclosed is a fluoroalkylsulfide derivative having excellent pest control activity or a salt thereof. Also disclosed is a pest control agent characterized by containing such a fluoroalkylsulfide derivative or a salt thereof as an active...
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WO/2009/073713A1 |
The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: ( i ) which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A prote...
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WO/2009/066060A2 |
The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain 4-substituted-6-isopropyl-benzene 1,3-diol compounds (referred to herein as IBD compounds), which, inter alia, inhibit heat ...
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WO/2009/067663A1 |
1,3-Dipole-functional compounds (e.g., azide functional compounds) can be reacted with certain alkynes in a cyclization reaction to form heterocyclic compounds. Useful alkynes (e.g., strained, cyclic alkynes) and methods of making such a...
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WO/2009/067618A1 |
The invention relates to substituted benzothiazoles, benzoxazoles - and their counterparts having pyridine and pyrimidine rings replacing the benzene ring - that are PDE4 inhibitors useful for treating stroke, myocardial infarct, and car...
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WO/2009/067604A1 |
The invention relates to substituted benzothiazoles, benzoxazoles - and their counterparts having pyridine and pyrimidine rings replacing the benzene ring - that are are PDE4 inhibitors useful for treating stroke, myocardial infarct, and...
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WO/2009/063505A2 |
The present invention provides novel process for preparation of (S)-N-[[3-[3-Fluoro-4-(4- morpholinyl)phenyl]-2-oxo-5-oxazolidinyl] methyl] -acetamide which comprises combining (R)-N-[3-[3-fluoro-4-morpholinyl phenyl]-2-oxo-5-oxazolidiny...
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WO/2009/064250A1 |
The invention provides compounds of formula wherein R1, R2 , R3, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for...
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WO/2009/064251A1 |
The invention provides compounds of formula wherein R1, R3, L1, L2, G1, G2, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with pr...
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WO/2009/062371A1 |
Carbamate derivatives of 5- or 6-membered ring represented by the general formula (I), a process for preparing them, pharmaceutical compositions comprising them, intermediates for preparing the general formula (I), and a process for prep...
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WO/2009/061233A1 |
The invention relates to electroluminescent material containing an organic luminescent substance. The novel electroluminescent material consists of an electron injecting layer, an active luminescent layer based on a metal chelate complex...
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