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| Number | Title | Issue Date |
| 8163736 | Cytotoxic agents comprising new tomaymycin derivatives The present invention is related to new tomaymycin derivatives, their process of preparation and their therapeutic uses. ... | 04/24/2012 |
| 8153626 | Substituted diazepine sulfonamides as bombesin receptor subtype-3 modulators Certain novel substituted diazepine sulfonamides are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases an... | 04/10/2012 |
| 8153627 | Quinazoline linked pyrrolo[2,1-][1, 4]benzodiazepine hybrids as potential anticancer agents and process for the preparation thereof The present invention provides a compound of general formula 5, useful as potential antitumour agents against human cancer cell lines. The present invention further provides a process for the preparation of pyrrolo[2,1-c][1,4]benzodiazepine hybrids of general formul... | 04/10/2012 |
| 8119629 | Carboxamide GABAα2 modulators The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders. ... | 02/21/2012 |
| 8106041 | Combination product comprising an antagonist or inverse agonist of histamine receptor H and an antipsychotic and antidepressant agent, and use thereof for the preparation of a medicament that prevents the adverse effects of psychotropic drugs Medicament comprising, in a pharmaceutically acceptable vehicle, an anti-psychotic or an antidepressant (A), which, on its own, has an undesirable effect of a gain in body weight or sedation, and an antagonist and/or inverse agonist (B) of the histamine H3 | 01/31/2012 |
| 8093240 | Triazole derivatives Novel triazole derivatives are inhibitors of TGF-beta receptor I kinase, and can be employed, inter alia, for the treatment of tumours. ... | 01/10/2012 |
| 8039464 | Muscarinic antagonists with PARP and SIR modulating activity as agents for inflammatory diseases The present invention relates generally to the cytoprotective activity of mixed muscarinic inhibition/PARP modulation and in particular to the use of dual inhibitors of M1 muscarinic receptor and poly(ADP-ribose) polymerase (PARP) as epithelioprotective medicaments,... | 10/18/2011 |
| 8034808 | Therapeutic compositions containing at least one pyrrolobenzodiazepine derivative and fludarabine The invention concerns the use of a therapeutic composition comprising at least one pyrrolobenzodiazepine derivative combined with fludarabine for treating cancer and more particularly hematological diseases. ... | 10/11/2011 |
| 8022065 | Purine derivatives as kinase inhibitors The present invention provides kinase inhibitors of Formula I. ... | 09/20/2011 |
| 7998954 | Pyrimidodiazepinone derivative The invention provides a pyrimidodiazepinone derivative represented by the general formula (I) [wherein n represents 1 or 2, Z represents a hydrogen atom or the like, R1 and R2 may be the same or diffe... | 08/16/2011 |
| 7981884 | Process for the preparation of olanzapine The invention relates to a process for the preparation of 2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno-[2,3-b][1,5]benzodiazepine (olanzapine) of the formula (I) by reacting 4-amino-2-methyl-10H-thieno[2,3-b][1/5]benzodiazepine hydrochloride of the formula (II) wi... | 07/19/2011 |
| 7973034 | Amide, aryl sulfonamide, aryl urea, and α,β-diketone derived carboxylesterase inhibitors, and their methods of use This disclosure relates to amides, aryl sulphonamides, aryl ureas, and α,β-diketones derivatives useful as carboxylesterase esterase inhibitors. The disclosure is also directed to the use of these compounds as selective human intestinal carboxylesterase inhibitors... | 07/05/2011 |
| 7951799 | Lactam compound, a method for producing the same, and a diabetic therapy by administering the same The present invention provides a lactam compound, a sugar transport enhancement agent containing this compound as an active ingredient, an agent for the prevention and/or treatment of diabetes mellitus, diabetic peripheral neuropathy, diabetic nephropathy, diabetic ... | 05/31/2011 |
| 7951798 | Polymorphs of olanzapine hydrochloride The present invention relates to new crystalline forms I, II and III of 2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3-b][1,5]-benzodiazepine hydrochloride, a process for the preparation thereof and pharmaceutical compositions containing the same. Said new polym... | 05/31/2011 |
| 7947678 | Heterocyclic benzodiazepine CGRP receptor antagonists Compounds of formula I: (where variables R2, R7, D, W, X, Y and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in whi... | 05/24/2011 |
| 7943608 | Diazepinoes The invention relates to compounds of the formula (I), to the preparation and use thereof for the preparation of a medicament for the treatment of diseases, in particular tumours and/or diseases in the development or course of which kinases are involved. | 05/17/2011 |
| 7932249 | Olanzapine pamoate dihydrate The present invention relates olanzapine pamoate dihydrate, pharmaceutical compositions thereof and use in treating certain mental disorders, such as schizophrenia. ... | 04/26/2011 |
| 7928101 | Fused polycyclic compounds having a heterocyclic ring(s) and pharmaceutical use thereof The present invention provides a fused polycyclic compound of the following formula, analogues thereof and pharmaceutically acceptable salts thereof; and agents for increasing the sugar-transporting capacity, hypoglycemic agents and pharmaceutical compositions conta... | 04/19/2011 |
| 7910577 | Injectable nanoparticulate olanzapine formulations Described are injectable formulations of nanoparticulate olanzapine that produce a prolonged duration of action upon administration, and methods of making and using such formulations. The injectable formulations comprise nanoparticulate olanzapine. ... | 03/22/2011 |
| 7902185 | Treatment of neurodegenerative diseases using proteasome modulators Methods for modulating proteasome activity in a subject is provided. Proteasome activity is modulated by administering a therapeutically effective amount of proteasome modulating pharmacological agent to a subject. In a preferred embodiment, the proteasome modulatin... | 03/08/2011 |
| 7893053 | Treating psychological conditions using muscarinic receptor Mantagonists Provided are methods of treating psychological diseases and conditions by administration of a preferential muscarinic acetylcholine receptor M1 antagonist, optionally with at least one antidepressant other than a selective muscarinic acetylcholine recepto... | 02/22/2011 |
| 7863267 | Use of selective chloride channel modulators to treat methamphetamine abuse The invention relates to methods of and treatments for using pharmaceutical compositions from a class of compounds that directly or indirectly selectively modulates GABAA chloride channel activity to treat alcohol and/or stimulant substance abuse. The pre... | 01/04/2011 |
| 7834005 | Pyrrolobenzodiazepine derivatives, compositions comprising the same and methods related thereto Disclosed are compounds of Formula I wherein X, Y, R1-R7, T1, T2, Z, and p are as described herein; a pharmaceutical composition comprising a compound of Formula I and a carrier; ... | 11/16/2010 |
| 7820650 | Antifungal 4-substituted 5,6-dihydro-4H-pyrrolo [1,2-a][1,4]benzodiazepines The present invention concerns compounds for use as a medicine having the formula the N-oxide forms, the salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R1 represent... | 10/26/2010 |
| 7790712 | Substituted [1,4]diazepino[1,2-A]indoles and azepino[1,2-A]indoles as anti-cytokine inhibitors The application relates to compounds of formula Ia and analogues thereof wherein R1 to R13 and X are as defined herein. The invention also relates to the use of the compounds of formula Ia as inhibitor... | 09/07/2010 |
| 7786109 | Tricyclic amide derivatives as modulators of H3 receptors The present invention relates to compounds of formula I wherein A, G, r and R1 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are usefu... | 08/31/2010 |
| 7776852 | Process for producing highly pure midazolam and salts thereof Provided is a process for producing highly pure midazolam and salts thereof, and a pharmaceutical composition containing the highly pure midazolam and/or a salt thereof. ... | 08/17/2010 |
| 7763604 | Methods for administration of a farnesyl dibenzodiazepinone This invention relates to methods of inhibiting growth and/or proliferation of a neoplastic cell, and methods of treating neoplasms by administration of the farnesylated dibenzodiazepinone compound of Formula I via continuous intravenous infusion. The invention incl... | 07/27/2010 |
| 7745430 | Transnasal anticonvulsive pharmaceutical composition Disclosed herein is a transnasal anticonvulsive pharmaceutical composition comprising diazepam as an active ingredient, water, a fatty acid ester, diethylene glycol monoethyl ether, ethanol and sodium glycocholate, wherein the weight of the fatty acid ester is at le... | 06/29/2010 |
| 7745429 | Crystal forms of olanzapine and processes for their preparation The invention relates to a process for the preparation of form I of olanzapine, crystallized from a solvent mixture which comprises 2-propanol, some pseudopolymorphic forms, namely solvates of olanzapine, a new polymorphic form A of olanzapine, and processes for the... | 06/29/2010 |
| 7741319 | 11-hydroxy-5h-pyrrolo[2,1-c][1,4] benzodiazepin-5-one derivatives as key intermediates for the preparation of c2 substituted pyrrolobenzodiazepines The present inventors have developed a key intermediate for the production of C2 substituted PBDs, which has a leaving group at the C2 position, a carbamate protecting group at the N10 position and a protected hydroxy group at the C11 position. In a first aspect, th... | 06/22/2010 |
| 7709471 | Compounds There is provided a compound of formula (I): processes for the manufacture thereof, pharmaceutical compositions thereof and uses in therapy. ... | 05/04/2010 |
| 7691848 | Pyrrolobenzodiazepine arylcarboxamides and derivatives thereof as follicle-stimulating hormone receptor antagonists This invention provides pyrrolobenzodiazepine arylcarboxamides selected from those of Formula (1), which act as follicle stimulating hormone receptor antagonists, as well as pharmaceutical compositions and methods of treatment utilizing these compounds. | 04/06/2010 |
| 7678787 | Pyrrolobenzodiazepine pyridine carboxamides and derivatives as follicle-stimulating hormone receptor antagonists This invention provides pyrrolobenzodiazepine pyridine carboxamides selected from those of Formula (1), which act as follicle stimulating hormone receptor antagonists. The invention also provides pharmaceutical compositions and methods of treatment utilizing the com... | 03/16/2010 |
| 7655646 | Dibenzodiazepinone analogues, processes for their production and their use as pharmaceuticals The invention relates to biologically active dibenzodiazepinone analogs represented by Formula I, to methods of producing them, to pharmaceutical compositions comprising them and to methods of treating neoplastic conditions. ... | 02/02/2010 |
| 7632830 | Lactam compounds and pharmaceutical use thereof An agent for increasing the sugar-transporting capacity and an agent for preventing and/or treating diabetes, diabetic peripheral neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic macroangiopathy, impaired glucose tolerance or adiposis, which contains... | 12/15/2009 |
| 7622463 | Dihydrodiazepines useful as inhibitors of protein kinases The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, o... | 11/24/2009 |
| 7618958 | Stereospecific anxiolytic and anticonvulsant agents with reduced muscle-relaxant, sedative-hypnotic and ataxic effects The present invention provides compositions and methods of using stereospecific benzodiazepine derivatives, their salts and prodrugs for the treatment of anxiolytic or convulsant disorders having the side effects of reduced alcohol craving in human alcoholics and a ... | 11/17/2009 |
| 7612062 | Pyrrolobenzodiazepines Compounds of the formula: (I) or solvate thereof, wherein: R2 is an optionally substituted C5-20 aryl group; R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR′, nitro, Me3 | 11/03/2009 |
| 7608615 | Pyrrolo[2,1-][1,4]benzodiazepine hybrids and a process for the preparation thereof The present invention provides quinazolinone linked pyrrolo[2,1-c][1,4]benzodiazepine hybrid of general formula 5, wherein, R is alkyl or halo group selected from H, Cl, F or CH3 and n=1 to 3 useful for antitumou... | 10/27/2009 |
