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WO/2011/058427A1 |
Provided are metabolites of palonosetron that can be used in treating animals, particularly humans, of the formula (I): or a pharmaceutically acceptable salt or prodrug thereof; wherein R1 and R4 independently can be H, hydroxyl, or carb...
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WO/2011/053706A1 |
Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, Ra, and Y are defined herein.
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WO/2011/049155A1 |
Disclosed is a process for producing cis-QMF, which has low environmental burden and is industrially advantageous. Specifically disclosed is a process for producing a cis-type 2-alkylspiro(1,3-oxathiolan-5,3')quinuclidine hydrochloric ac...
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WO/2011/048607A1 |
The present invention describes recovery and racemization of (1R)-Phenyl- 1,2,3,4-tetrahydroisoquinoline of compound of formula (III) to obtain racemic 1- phenyl-1, 2,3,4-tetrahydroisoquinoline of compound of formula (I) and its further ...
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WO/2011/043480A1 |
Disclosed is a homocysteine synthase inhibitor which is useful for the prevention or treatment of diseases associated with a homocysteine synthase. Specifically disclosed is a compound represented by general formula (I) [wherein each sym...
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WO/2011/013095A1 |
The present invention relates to novel processes for the preparation of N-[(3S)-1- azabicyclo[2.2.2]oct-3-yl]-5,6,7,8-tetrahydronaphthalene-1-c
arboxamide of Formula I. The present invention further relates to processes for the preparati...
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WO/2011/003624A1 |
The invention relates to a preparation and purification processes of solifenacin salts, particularly to a crystallization process of solifenacin succinate, leading to high purity of the obtained product as well as to the desired average ...
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WO/2010/144043A1 |
The invention provides a 4-methylbenzenesulphonate salt of the muscarinic antagonist (R)- 1-(4-fluorophenethyl)-3-((S)-2-phenyl-2-(piperidin-1 -yl)propanoyloxy)-1- azoniabicyclo[2.2.2]octane and its use in therapy,as well as a process fo...
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WO/2010/131145A1 |
The present invention relates to compounds of the formula (I): to pharmaceutically acceptable salts therefore and to pharmaceutically acceptable solvates of said compounds and salts, wherein the substituents are defined herein; to compos...
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WO/2010/121963A1 |
The present invention relates to substituted resorcinol derivatives which inhibit the activity of Heat Shock Protein HSP90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurode...
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WO/2010/113834A1 |
Disclosed is a novel and excellent method for preventing and/or treating cannabinoid-2 receptor-related diseases, which is based on an agonist action on cannabinoid-2 receptors. Specifically disclosed is a heterocyclic derivative mainly ...
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WO/2010/103529A1 |
A new method for the preparation of solifenacin by reacting quinuclidin-3-ol and bis (aryl) carbonate to form (3R)-l -azabicyclo[2.2.2]oct-3-yl 4-aryl carbonate of formula (IVa); and treating (3R)-I - azabicyclo[2.2.2]oct-3-yl 4-aryl car...
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WO/2010/094210A1 |
The method for preparing the (4S,5R)-half-ester which is the important intermediate of synthesizing the (+)-biotin is provided, which comprises reacting cycloanhydride with alcohol through enantioselective ring opening reaction in the p...
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WO/2010/092153A1 |
The invention relates to substituted tetrahydronapthalenes, to derivatives thereof, to physiologically acceptable salts thereof, to physiologically functional derivatives, to the production thereof, to drugs containing at least one subst...
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WO/2010/091164A1 |
The present invention comprises glucosylceramide synthase (GCS) modulators of following structural formula (I); wherein R1, A, L, R2, R3, and m are defined herein, as well as N-oxides of them and pharmaceutically acceptable salts thereof...
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WO/2010/085724A1 |
The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and t...
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WO/2010/072742A1 |
The present invention relates to the cinchonidine salt useful in the preparation of intermediates for preparing a macrocyclic HCV inhibitor, as well as processes involving this salt.
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WO/2010/072296A1 |
The invention relates to the compounds of the formula I, where Y, R1, R2, R3, and R3' are as defined in claim 1, wherein said compounds are inhibitors of tyrosine kinases, particularly of Met kinase, and can be used for treating tumors, ...
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WO/2010/072338A1 |
The present invention relates to alkaloid aminoester derivatives acting as muscarinic receptor antagonists, to methods of preparing such derivatives, to compositions comprising them and therapeutic use thereof.
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WO/2010/056656A2 |
Processes for the preparation of palonosetron hydrochloride and its crystalline forms.
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WO/2010/053182A1 |
A kynurenine production inhibitor or the like, which contains a nitrogen-containing heterocyclic compound represented by formula (I). (In the formula, R50 and R51 may be the same or different and each represents a hydrogen atom or the l...
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WO/2010/048526A2 |
The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator ("CFTR"), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators...
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WO/2010/043515A1 |
The present invention provides novel methods for preparing 5-(trifluoromethoxy)-lH-3- indazolecarboxylic acid (3), which is a useful precursor for the preparation of bicyclic-5- trifluoromethoxy-lH-indazole-S-carboxylic acid amides of Fo...
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WO/2010/037129A1 |
Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorder...
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WO/2010/029313A1 |
Described are various compounds and methods for the treatment of infections. In particular, alkaloids and imino sugars with antiviral activity are described, including those with activity against HCV and RSV.
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WO/2010/030592A1 |
The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected w...
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WO/2010/024430A1 |
Disclosed is a compound which is useful as a medicinal agent having a PKCθ inhibition activity, particularly as an active ingredient for a pharmaceutical composition for inhibiting acute rejection occurring in transplantation. Studies h...
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WO/2010/015324A1 |
The invention relates to quinuclidine carbonate derivatives acting as muscarinic receptor antagonists, to methods of preparing such derivatives, to compositions comprising them and therapeutic use thereof.
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WO/2010/012459A2 |
The invention relates to the synthesis of solifenacin, the preparation of its salts and their inclusion into pharmaceutically acceptable dosage forms.
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WO/2009/138707A9 |
The invention provides named compounds of formula (I), wherein R4 is a N- sustituted quinuclidine (I) pharmaceutical compositions containing them and a process for preparing the pharmaceutical compositions. Their use in therapy for' the ...
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WO/2010/008117A1 |
The present invention relates to cinchona-based bifunctional organocatalysts and methods for preparing chiral hemiesters using the same. More specifically, the present invention relates to methods for preparing chiral hemiesters from pro...
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WO/2010/002675A2 |
Disclosed are new quinine sulfate/bisulfate solid complexes, methods of making the solid complexes as well as formulations prepared therefrom and uses thereof.
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WO/2009/153536A1 |
The invention provides named compounds of formula (I), pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions and their use in therapy.
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WO/2009/150141A1 |
This invention relates to novel azabicyclooctyl-quinazolinone derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine ...
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WO/2009/145323A1 |
Disclosed is a novel method for oxidizing an alcohol compound. The method for oxidizing an alcohol compound, which is expressed by scheme (1), is characterized by using oxygen in the presence of a polycyclic compound and a nitrous acid c...
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WO/2009/142522A1 |
A process for the preparation of solifenacin and/or the pharmaceutically acceptable salts thereof of high pharmaceutical purity is characterized in that 3-(R)-quinuclidinoloxy anion generated in situ from 3-(R)-quinuclidinol in a presenc...
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WO/2009/139002A2 |
The present invention relates to an improved process for the preparation of solifenacin compound of formula (1) and its succinate salt compound of formula (1a), comprising the condensation of (R)-3- quinuclidinol with (S)-ethyl- 1 -pheny...
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WO/2009/139710A1 |
The invention provides compounds of formula (I) wherein R1, R2, R3, Het1, n, Y and X are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing pharmaceutica...
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WO/2009/139709A1 |
The invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5, Het1, n, Y and X are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing pharm...
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WO/2009/136405A1 |
The present invention describes the process for the preparation of pure enantiomeric form of palonosetron base of formula (I), and its solid-state characteristics of said compound.
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WO/2009/132832A2 |
The invention relates to a method for producing 1,4-benzothiepin-1,1-dioxide derivatives substituted with benzyl groups.
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WO/2009/131065A1 |
Disclosed is a compound useful as a prophylactic agent or a therapeutic agent for cardiovascular diseases, nervous system diseases, metabolic diseases, genital diseases, gastrointestinal diseases, neoplasm, infectious diseases and others...
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WO/2009/126806A2 |
Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation ...
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WO/2009/122664A1 |
Provided is a photobase generator that can efficiently generate amines (tertiary amine and amidine) having high catalytic activity when exposed to light with wavelengths of 350−500nm (especially 400−500nm). The photobase generator is...
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WO/2009/099086A1 |
Disclosed is a compound which is useful as a prophylactic or therapeutic agent for cardiovascular diseases, nervous system diseases, metabolic diseases, genital diseases and gastrointestinal diseases. Specifically disclosed is a compound...
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WO/2009/098453A1 |
This invention relates to M3 antagonists of formula (I): wherein R2, R4, R5, R6, W, V, A, D, X, t, u and v are as defined herein; pharmaceutical compositions containing them; methods for their preparation; and their use in the treatment ...
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WO/2009/055437A9 |
The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nic...
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WO/2009/090008A1 |
The invention relates to a pharmaceutical formulation in the form of inhalable dry powder comprising particles of a pharmaceutically acceptable salt of 3-[[[(3-fluorophenyl)[(3,4,5-trifluorophenyl)methyl]amino]ca
rbonyl]-oxy]-l-[2-oxo-2-...
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WO/2009/087664A1 |
The present invention provides improved processes for preparing chemically and chirally pure Solifenacin base. The present invention also provides for a composition comprising of a salt of Solifenacin having at least 98 % purity. The pre...
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WO/2009/087643A1 |
The present invention relates to novel crystalline forms, designated as Form (I) and Form (II) of Palonosetron Hydrochloride ((3as)-2[(3s)-1-Azabicyclo[2.2.2]Oct-3-yl]-2,3,3a,4,5,6- hexahydro-1H-benz[de]isoquinoline-1-one mono hydrchlori...
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