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WO/2006/010511A1 |
The invention relates to a method for producing a compound 3-(4-Piperidinyl)-2,3,4,5-tetrahydro-1,3-benzodiazepin-2(1H)
-on of formula (I), wherein said compound is a structural element of CGRP-antagonists which are particularly suitable...
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WO/2006/006180A1 |
Disclosed is a process for producing pure form of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]
benzodiazepine. The process comprises of reacting 2-(2-aminoanilino)-5-methylthiophene-3-carbonitrile with N-methyl piperaz...
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WO/2006/004200A1 |
A urea derivative having excellent DGAT inhibitory activity or a pharmacologically acceptable salt thereof. The urea derivative is represented by the general formula (I) (II) (III) (XXXIX) (XL) [wherein R1 is, e.g., C6-10 aryl optionally...
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WO/2006/001866A2 |
Disclosed herein are crystalline Forms A, B, C, D, and E of N-desmethylclozapine, methods of preparing the same, pharmaceutical compositions comprising the same, and methods of therapeutic treatment involving N-desmethylclozapine polymor...
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WO2005103041A9 |
The invention is directed to compositions and methods useful for treating Central Nervous System (CNS) disorders. Furthermore, the invention provides compositions and methods of treating sleep disorders. More specifically, the invention ...
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WO/2005/117876A1 |
The present invention provides analogs and derivatives of thalidomide which inhibit cancer and angiogenesis. The present invention further provides compounds which disrupt microtubule polymerization. The present further provides methods ...
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WO/2005/116034A1 |
This invention relates to CCK-A agonists of Formula (I) wherein R1-R4, A, B, X, D, E and G are as defined in the specificiation, as well as, among other things, pharmaceutical compositions containing the compounds and methods of use of t...
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WO/2005/113517A1 |
The invention especially relates to novel type 2,3-benzodiazepine stereospecific derivatives as inhibitors of phosphodiesterase, especially types 2 and 4, and to the applications thereof in the field of therapeutics, especially for the p...
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WO/2005/113542A2 |
The invention provides N-cyclic sulfonamido compounds for use in treating or preventing cognitive disorders, such as Alzheimer’s Disease. Compounds of particular interest are defined by Formula (I), wherein R4, R5, R6, R7 and R8 are as...
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WO/2005/111001A1 |
This invention relates to novel compounds having the Formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of H. pylori infection.
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WO/2005/103037A2 |
The invention relates to CGRP antagonists of general formula (I), wherein A, X, Q, and R1 to R3 are defined as indicated in claim 1, the tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures, and salts thereof, and the hydra...
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WO/2005/091697A2 |
The invention provides N,N'-disubstituted monothiourea or bisthiourea-Pd(0) complexes that are useful as catalysts for palladium-catalyzed Heck reaction of aryl iodides and bromides with olefins, and as catalysts for palladium catalyze...
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WO/2005/090319A1 |
A process for producing a compound which is a benzodiazepine derivative of formula: (I) wherein: represents or R1 represents C1-6 alkyl, aryl or heteroaryl; each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1...
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WO/2005/089770A1 |
Use of a compound which is (a) a benzodiazepine derivative of the formula (I) or an N-oxide thereof or (b) a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in treating or preventing an RSV infection ...
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WO/2005/090322A1 |
The invention relates to a compound having general formula (I), wherein: n = 1 or 2; p represents an integer varying between 1 and 7; A is selected from one or more X, Y and/or Z groups; X = optionally-substituted methylene; Y = C2-alken...
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WO/2005/087236A1 |
Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.
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WO/2005/084668A1 |
A medicine for the prevention and/or treatment of ischemic circulatory diseases which contains as an active ingredient a compound which is an aminobenzenesulfonic acid derivative represented by the general formula (I): (for the symbols i...
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WO/2005/080976A1 |
A method of evaluating memory/learning functions with the use of a model with glutamic acid N-methyl-D-aspartate (NMDA) type receptor dysfunction as an animal model of schizophrenia and with the use of reference memory problems, wherein ...
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WO/2005/077899A2 |
Compounds of formula (I) wherein A and B are amine-substituted sidechains, Y1 and Y2 form various tricyclic cores, Xa and Xb are C, CH, or N, as defined herein, and Rx is an optional substituent. Compounds and compositions of formula (I)...
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WO/2005/070872A1 |
The invention provides novel β2-adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with β2-adrenergic r...
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WO/2005/065779A1 |
The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors ('CGRP-receptor'), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment usin...
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WO/2005/063723A1 |
The invention relates to compounds of formula (I) having PDE2 inhibitory activities, as well as therapeutic methods by administering said compounds, in particular for treating various diseases of the central or peripheral nervous system....
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WO/2005/061467A2 |
Compounds (I) are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical comp...
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WO/2005/058884A2 |
The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane c...
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WO/2005/058863A1 |
Disclosed are reactive cyclic carbonates and ureas of formula (I) or (II), wherein R and X have the meaning indicated in the description. Said carbonates and ureas allow functional groups to be specifically introduced into biomolecules, ...
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WO/2005/058832A1 |
The present invention relates to diacylhydrazine derivatives of formula I, the use of the compounds of formula I as inhibitors of raf-kinase, the use of the compounds of formula I for the manufacture of a pharmaceutical composition and a...
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WO/2005/054211A1 |
A new method of purification of Lorazepam is disclosed that consists in removing products of synthesis, decomposition products, water or other solvent that forms a solvate with Lorazepam, by crystallization or stirring in an organic solv...
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WO/2005/040144A1 |
The present invention relates to novel diazepanyl derivatives of formula (I) having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiat...
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WO/2005/040126A1 |
The present invention relates to compounds of the general formula (I) Wherein R1 is -(CHR’)q-aryl or -(CHR')q-heteroaryl, which are unsubstituted or mono, di- or tri-substituted by lower alkyl, lower alkoxy, CF3 or halogen, or is lower...
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WO/2005/037207A2 |
The present invention is directed to alkanoyl and cycloalkanoyl-amine derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake inclu...
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WO/2005/037810A2 |
The invention relates to a compound of formula (I), wherein n ranges from 1 to 6, A is aryl such as phenyl or naphtyle, or monocyclic heteroaryl such as thienyl, furyl or pyrrolyl; aryl or heteroaryl being substituted, if necessary; B is...
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WO/2005/037809A1 |
The present invention is directed to substituted aryl cycloalkanoyl derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake includi...
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WO/2005/023772A1 |
The invention relates to malonamide derivatives of formula (I), wherein: R1 is one of the following groups (Formulae a), b), c), d)); R2 is lower alkyl, lower alkinyl, -(CH2)n-O-lower alkyl, -(CH2)n-S-lower alkyl, -(CH2)n-CN, -(CR'R')n-C...
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WO/2005/021005A2 |
The field of the invention relates to a process for the preparation of 1,4-benzodiazepine derivatives. It also relates to pharmaceutical compositions that include the 1,4- benzodiazepine derivatives.
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WO/2005/016876A2 |
Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R is-C(O)-N(R27 )(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical composi...
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WO/2005/011581A2 |
The present invention is directed to hexahydrodiazepinone compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme ('DPP-IV inhibitors') and which are useful in the treatment or prevention of diseases in which the dipeptidyl ...
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WO/2005/012266A1 |
The present invention relates to new D3 and D2 dopamine receptor subtype preferring ligands of formula (I): wherein R1 and R2 represent independently a substituent selected from hydrogen, alkyl, aryl, cycloalkyl, aroyl, or R1 and R2 may ...
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WO/2005/012265A1 |
The invention relates to new 8-chloro-2,3-benzodiazepine derivatives of the general formula (I),wherein R stands for a lower alkyl group or a group of the general formula -NH-R', wherein R' stands for a lower alkyl or a lower cycloalkyl ...
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WO/2005/005394A2 |
Methods for treatment of IP antagonist mediated diseases or conditions by administration to a subject in need thereof a compound of formula (I) wherein R1, R 2 , A and X are as defined herein. Also disclosed are compounds and related com...
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WO/2004/106310A1 |
The present invention relates to compounds of formula (I). The invention also relates to methods for preparing the compounds and their uses as CCK receptor ligands and CCK antagonists.
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WO/2004/099124A2 |
The invention relates to novel bioisosteres of the antibiotic actinonin of general formula (I). Said novel compounds are of particular interest when used as inhibitors of metalloproteinases.
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WO/2004/096134A2 |
The present invention is directed to novel 1,4-diazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I as defined herein, with R 1 to R 8 and X as defined here...
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WO/2004/096818A2 |
The invention relates to methods and compositions for identifying compounds having therapeutic activity against human immunodeficiency virus (HIV).
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WO/2004/092124A2 |
Cyclopentyl compounds linked to a benzoxazinyl group through an amido moiety utilizing the ring nitrogen of the benzoxazine, and further substituted with a heterocyclic moiety, such compounds represented by formula (I): which are used to...
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WO/2004/089916A1 |
The present invention relates to novel benzodiazepine compounds exhibiting RXR-antagonist efficacy, for delaying progression of, preventing or treating a condition or disease being associated with RXR-antagonism, in particular selected f...
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WO/2004/089313A2 |
The invention provides novel soluble olanzapine forms. These forms include salts, co-crystals, and solvates of olanzapine. The invention also provides novel pharmaceutical compositions comprising these novel soluble forms and related met...
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WO1995018619A9 |
Certain compounds within formula (I) are inhibitors of platelet aggregation wherein A<1> is NH or CH<2>; R is H, C1-6alkyl, benzyl or a carboxy protecting group; R<3> is C1-6alkyl, Ar- C0-6alkyl, C1-6cycloalkyl C0-6alkyl, or Het C0-6alky...
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WO/2004/087711A1 |
The present invention relates to pyrrolo [2,1-c][1,4]benzodiazepine hybrids useful as potential antitumour agents. This invention also relates to a process for the preparation of new pyrrolo[2,1-c][1,4]benzodiazepine hybrids as potential...
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WO/2004/084898A1 |
The present invention relates to a benzenesulfonamide derivative of formula (I), which is useful as an active ingredient of pharmaceutical preparations. The benzenesulfonamide derivatives of the present invention have CCR3 (CC type chemo...
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WO/2004/085410A1 |
The present invention relates to an adenosine deaminase inhibitor and a novel Bacillus sp. strain which produces it. Particularly, the present 5 invention relates to the adenosine deaminase inhibitor, and the novel Bacillus sp. IADA-7 pr...
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