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WO/2009/054887A1 |
The present invention relates to a process for preparing inhibitors of cholesterol absorption of Formula II: II and the pharmaceutically acceptable salts and esters thereof, employing a metal-catalyzed dynamic kinetic resolution (DKR) as...
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WO/2009/051244A1 |
Disclosed is a compound represented by the following formula (I). (In the formula, the symbols are as defined in the description.) This compound has an excellent RBP4 lowering effect, and is useful as an agent for prevention or treatment...
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WO/2009/045419A1 |
The invention is directed to novel azetidinones selected from 2-(S)-[4-(((2-(Dimethylamino)ethyl)ethylamino)carbonyl)pheno
xy]-3,3-diethyl-N-[1-(R)-(4-(trifluoromethoxy)phenyl)butyl]-
4-oxo-1-azetidin ecarboxamide, 2-(S)-[4-(((2-(Dimethy...
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WO/2009/043117A1 |
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/2009/038759A2 |
The present invention relates to amides that have activity as SlP receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate SlP receptor activity. The compounds may be used as immunomodulato...
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WO/2009/032326A1 |
In accordance with one embodiment, the present invention provides a compound of general formula (I), stereoisomers thereof and/or its pharmaceutically acceptable salts thereof, which have antibacterial activity; with methods of treating ...
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WO/2009/021758A1 |
The present invention relates to compounds of the general formula (I) in which A, B, D, Y, R1, R2, R3, R4 and R5 are as defined in claim 1, the enantiomers thereof, the diastereomers thereof, the mixtures thereof and the salts thereof, e...
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WO/2009/021945A1 |
The present invention relates to compounds of the general formula (I), wherein A1, A2, B, D, Y, R1, R2, R3, R4 and R5 are defined as mentioned in the description, the enantiomers, diastereomers, mixtures, and salts thereof, particularly ...
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WO/2009/021946A1 |
The present invention relates to compounds of the general formula (I), wherein A, B, D, Y, R1, R2, R3, R4 und R5 are defined as mentioned in claims 1, the enantiomers, diastereomers, mixtures, and salts thereof, particularly physiologica...
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WO/2009/016048A1 |
The present invention relates to compounds of formula (I) wherein R1 is hydrogen, lower alkyl or benzyl which may be optionally substituted by halogen or lower alkoxy; R2 is hydrogen, halogen or OR, wherein R is lower alkyl, aryl or lowe...
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WO/2009/016085A1 |
The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, for treating diseases and conditions of the central nervous system (CNS), in particular sleep disorders.
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WO/2009/015485A1 |
A CPTl inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural ...
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WO/2009/009550A1 |
The present application relates to cannabinoid receptor ligands containing compounds of formula (I) wherein A, R1, R2, and R3 are as defined in the specification. The present application also relates to compositions comprising such compo...
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WO/2009/000397A1 |
The invention relates to an improved process for preparing benzyl pentahydroxyhexylcarbamoylundecanoate. Benzyl pentahydroxyhexylcarbamoyl-undecanoate has the formula (I).
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WO/2008/157565A1 |
The present application describes deuterium-enriched ezetimibe, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
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WO/2008/151324A1 |
Processes for preparing ezetimibe-related compounds with a ketoreductase and for purifying ezetimibe are disclosed.
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WO/2008/139287A1 |
The present invention relates to a class of EP2 antagonist azetidines of general formula (I) wherein the variables and substituents are as defined herein, and especially to EP2 antagonist compounds, to their use in medicine, particularly...
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WO/2008/135819A1 |
This invention relates to the hydrochloride salt of 5-[3-{3-hydroxyphenoxy)azetidin-1-yl]-5- methyl-2,2-diphenylhexanamide or derived form thereof and its use as a medicament.
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WO/2008/133900A1 |
The invention provides compounds of the formula: (I) in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a, Z and Q are as defined in the specification. These compounds are muscarinic receptor antago...
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WO/2008/127070A1 |
The present invention relates to a process for preparing (3R,4S)-3-[[[R]-V-t- butyldimethylsilyloxy] ethyl] -4- [(/?)- l"-carboxyethyl]-2-azetidinone [4-BMA: formula (6)], a key intermediate for the synthesis of carbapenem and penem anti...
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WO/2008/124838A1 |
Methods for treating cancer using compounds that inhibit human DNA ligases. Methods for using compounds that inhibit human DNA ligases to provide insights into the reaction mechanisms of human DNA ligases, for example to identify the hum...
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WO/2008/118091A1 |
The present invention relates to 3-bromo-N-{(2S)-2-(4-fluorophenyl)-4-[3-(4- acetylpiperazin-1-yl)azetidin-1-yl]butyl}-N-methyl-5-(triflu
oromethyl)benzamide fumarate and crystalline forms thereof. The present invention also relates to t...
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WO/2008/118092A1 |
The present invention relates to 3-bromo-N-{(2S)-2-(4-fluorophenyl)-4-[3-(4-acetylpiperazin-1
-yl)azetidin-1-yl]butyl}-N-methyl-5-(trifluoromethyl)benzami
de maleate and crystalline forms thereof. The present invention also relates to th...
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WO/2008/108145A1 |
The invention is directed to a method for producing a beta-lactam compound, wherein a cyclization reaction of a compound having a double bond and a sulfonyl isocyanate is continuously carried out using a tubular reactor. According to the...
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WO/2008/106900A1 |
A method of manufacturing (3R,4S)-l-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3- hydroxypropyl)]-4-(4-hydroxyphenyl)-2-azetidinone (Ezetimibe) of formula I, starting from the optically active (S)-N-acyl-oxazolidide of formula II, which...
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WO/2008/096372A2 |
The present invention relates to an industrially advantageous process for the preparation of ezetimibe of formula (I) in high yields by using novel benzyl ester intermediates. The present invention further provides a process for the puri...
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WO/2008/089984A2 |
The present invention relates to the method of preparing of ezetimibe and in particular to novel intermediates for its synthesis and an improved process for preparing such intermediates. Said intermediates may be obtained in high yields ...
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WO/2008/074723A1 |
The invention belongs to the field of organic chemistry and relates to a novel inclusion complex of ezetimibe with a cyclodextrin. Provided is a process for the preparation of an inclusion complex of ezetimibe and a cyclodextrin and char...
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WO/2008/074703A1 |
Compounds of the formula (I) or pharmaceutically acceptable salts thereof, wherein m, n, Ar, R1, R2, Ra and Rb are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
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WO/2008/076042A1 |
The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising said compounds, and to the use of said compounds in therapy. The present invention further relates to processes for the preparation ...
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WO/2008/075005A1 |
The invention provides compounds of formula (I) wherein R5 is a group of formula (II) or (III) and R1, R2, R3, R4, R6, a, b, Z, Y and X are as defined in the specification, a process for their preparation, pharmaceutical compositions con...
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WO/2008/072032A1 |
The novel positively charged pro-drugs of beta-lactam antibiotics in the general 'Structure 4' were designed. The positively charged amino group of the pro-drug not only makes the drugs soluble in water, but also bonds to the negative ch...
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WO/2008/068475A1 |
There are provided crystalline forms of the compounds Ph(3-Cl)(5-OCHF2)-(R)CH(OH)C(O)-Aze-Pab(OMe) (Compound A) and Ph(3-Cl)(5-OCHF2)-(R)CH(OH)C(O)-Aze-Pab(OH) (Compound B), pharmaceutical compositions containing them, processes for obta...
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WO/2008/061238A2 |
The present invention relates to processes for the production of 4-biphenylylazetidin-2-one derivatives of formula (I).
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WO/2008/059782A1 |
Disclosed is a process for producing a mugineic acid compound, which is shown by the following scheme. STEP 1 STEP 2 STEP 3 STEP 4 wherein R1 and R2 independently represent a hydrogen atom or a hydroxyl group; R3 represents a hydroxyl gr...
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WO/2008/052658A1 |
The invention relates to the compound of the formula (I) and to its physiologically compatible salts. The compound is suitable, for example, as a hypolipidemic agent.
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WO2007030721A9 |
The invention encompasses (3R,4S)-4-((4-benzyloxy)phenyl)-l-(4-fluorophenyl)-3- (3-(4-fluorophenyl)-3-oxopropyl)-2-azetidinone (Compound 2a). The invention further encompasses processes tor preparing Compound 2a from Compound 1. The inve...
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WO/2008/035157A1 |
The invention relates to compounds of formula (I) processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical compositions containing them.
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WO/2008/035153A2 |
Novel process for the preparation of the Faropenem of formula (I) where, R is hydrogen, alkali metal salts such as sodium or potassium, or prodrug residue.
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WO/2008/033278A1 |
The invention relates to heterosubstituted N-thiolated beta-lactams, compositions comprising these compounds, methods for their production, and methods of use as antibiotics to inhibit the growth of bacteria. The antibacterial agents of ...
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WO/2008/032338A2 |
The present invention provides an improved process for the preparation of ezetimibe through novel organic amine salt compounds of general formula (1). The present invention also relates to a highly pure ezetimibe and 3-((3R,4S)-1-(4-fluo...
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WO/2008/027081A1 |
Provided are processes for purifying (3R,4S)-4-(4-hydroxyprotected-phenyl)- l-(4-fluorophenyl)-3-[3-(4-fluorophenyl)-3-oxopropyl]azetidi
n-2-one having the following formula II, wherein X and Y are hydrogen or a substituted or unsubstitu...
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WO/2008/024892A2 |
Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-Beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11...
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WO/2008/022945A1 |
The invention relates to compounds of the general formula (I) in which A, B, D, Y, R1, R2, R3, R4 and R5 are defined as per claim 1, to their enantiomers, their diastereomers, their mixtures and their salts, especially their physiologica...
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WO/2008/020597A1 |
Disclosed is a method for producing a commercially suitable 1-methylcarbapenem production intermediate (II), which does not comprise a complicated step, while using low-cost raw material. Specifically disclosed is a method for producing ...
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WO/2008/016007A1 |
A phthalic acid derivative represented by the general formula (1) has an inhibitory activity on metallo-β-lactamase. Therefore, when used in combination with a β-lactam antibiotic, the derivative can inhibit the deactivation of the β-...
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WO/2008/007836A1 |
The present invention relates to a method for preparing 4-acetoxyazetidinone and derivatives thereof, and in particular to the preparation method comprising the steps of: dissolving a compound which is substituted with a ketone derivativ...
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WO/2008/000131A1 |
The present application discloses a type of α-amino-N-substituted amide compounds, compositions and uses thereof. The present compounds are represented by general formula I. It is easy to prepare these compounds. These compounds have st...
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WO/2007/147771A2 |
Compounds of the formula (I), (II) or (III); or pharmaceutically acceptable salts thereof, wherein m, n, q, Ar, R1, R2, R3, R4 and R5 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods fo...
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WO/2007/147770A2 |
The present invention relates to compounds of the general formula (i), wherein R1 is -OR1 ', heterocycloalkyl, aryl or heteroaryl, which are unsubstituted or substituted by lower alkyl or halogen; R1' is lower alkyl, lower alkyl substitu...
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