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JP5200288B2 |
The subject invention provides stereoisomeric compounds of formula (x): wherein the variables are as defined herein, and compositions for the safe and effective treatment of various gastrointestinal disorders including, but not limited t...
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JP2013515724A |
The present invention discloses and claims a series of substituted tropinone benzylamines of formula (I): The compounds of this invention are inhibitors of β-tryptase and are, therefore, useful as pharmaceutical agents. Additionally, th...
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JP2013515036A |
The present invention provides novel radio iodinated tropanes incorporating triazole or isoxazole rings. Also provided are methods of preparation of said tropanes from functionalised tropane precursors, using click cycloaddition chemistr...
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JP2013075830A |
To provide a therapeutic or a prophylactic agent which shows good pharmacokinetics in diseases, including depression, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington chorea, eating disorders, hyperte...
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JP5191155B2 |
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JP2013513664A |
The present invention is directed to synthetic bridged bicyclic compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmac...
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JP5179533B2 |
Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A...
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JP5173421B2 |
The invention relates to a new process for preparing tiotropium salts of general formula 1 wherein X− may have the meanings given in the claims and in the specification.
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JP5165244B2 |
Preparation of new tiotropilium salts (1) by subjecting a different tiotropilium salt (2) to anion exchange with an ion source in a solvent. Preparation of new tiotropilium salts of formula (1) by subjecting a different tiotropilium salt...
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JP5165245B2 |
Tiotropium salts, their solvates and hydrates are new. Tiotropium salts of formula (I), their solvates, hydrates are new. [Image] X -> : anion. Independent claims are included for the following: (1) a pharmaceutical composition (C1) comp...
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JP2013047188A |
To provide a new therapeutic agent of diabetes mellitus relating to a GPR119 agonist.In the GPR119 agonist, the following compounds or salt thereof are illustrated as concrete examples: t-butyl 3-[2-(4-methanesulfonylphenoxymethyl)pyridi...
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JP5155472B2 |
This invention relates to solvates of tiotropium bromide having a purity of at least 99%, process for preparing such pure solvates, and their use in pharmaceutical formulations. This invention also provides tiotropium bromide solvates co...
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JP5159317B2 |
The invention provides novel indazole-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT...
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JP5140226B2 |
The invention relates to benzofuran or benzothiophene derivatives of general formula: These compounds are of use as medicinal products, in particular in the treatment of pathological syndromes of the cardiovascular system.
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JP5134756B2 |
Preparation of quaternized scopine 2,2-di-(hetero)arylalkanoic acid esters (I) involves single-stage reaction of a quaternized scopine compound (II) with a di-(hetero)aryl-alkanoic acid (or activated ester) derivative (III). Preparation ...
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JP5126856B2 |
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JP5121717B2 |
The N-pyridylpiperidine compound of the invention is represented by Formula (1) wherein R 1 is a halogen atom, a C 1-4 haloalkyl group, a cyano group, a nitro group, or C 1-4 alkoxycarbonyl group; R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 ...
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JP5119157B2 |
A compound according to Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R6, R7 and Z are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.
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JP5114208B2 |
The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disea...
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JP2012532833A |
The present invention provides novel and advantageous processes for preparing and purifying pharmaceuticals The processes comprise a nucleophilic reaction wherein a modified leaving group LM, which has increased lipophilicity, of a vecto...
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JP5104893B2 |
A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided. A pyrimidine derivative or a salt...
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JP5094453B2 |
Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the t...
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JP5086091B2 |
The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5...
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JP5086267B2 |
This invention relates to a novel crystalline form of tiotropium bromide, processes for preparing it, and its use in pharmaceutical formulations.
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JP5086248B2 |
The invention provides novel benzoimidazolone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated w...
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JP5086280B2 |
The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I):wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, that are antagonists at the mu opioi...
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JP5081363B2 |
The invention relates to benzofuran or benzothiophene derivatives, to processes for preparing them, to pharmaceutical compositions comprising them, and to the method of use thereof in the treatment of pathological syndromes of the cardio...
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JP5086513B2 |
N-Benzoyl arylsulfonamides having the formula (I) are BCL-Xl inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-Xl inhibiting compositions and methods of promoting apoptosis in a mammal.
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JP2012229163A |
To provide a novel compound which is useful as an oxidation catalyst for alcohol compounds.This invention relates to a 2-aza-adamantane compound represented by formula (1) and a method for producing the same. In formula (1), N-A represen...
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JP5073746B2 |
The present invention relates to compounds of general formula I wherein the groups and radicals B, k, L, U,V, W, X, Y, Z, R 1 , R 2 , have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions conta...
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JP2012528165A |
The invention is directed to Compounds of Formula (I): the invention provides compounds that inhibit, regulate, and/or modulate P13K and/or mTOR that are useful in the treatment of hyperproliferative diseases, such as cancer, in mammals....
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JP2012527474A |
The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
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JP2012211193A |
To provide 8-azabicyclo[3.2.1]octane compounds as μ opioid receptor antagonist.The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, A, and G are defined in the specification, or a pharmace...
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JP2012526744A |
The present applications discloses novel 8-aza-bicyclo[3.2.1]oct-3-yloxy)-chromen-2-one derivatives and their use as monoamine neurotransmitter re-uptake inhibitors. In other aspects the applications discloses the use of these compounds ...
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JPWO2010122968A1 |
To provide a compound useful as an anti-obesity drug. The present inventors have investigated a compound having a DGAT1 inhibitory action, which is promising as an active ingredient of a pharmaceutical composition for treating obesity, t...
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JP2012525325A |
The present invention relates to a compound represented by a formula (I): wherein X is a group represented by or the like; Y is a group represented by or the like; and Ar1 is a group represented by or a pharmaceutically acceptable salt t...
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JP5048408B2 |
This invention relates to solvates of tiotropium bromide having a purity of at least 99%, process for preparing such pure solvates, and their use in pharmaceutical formulations. This invention also provides tiotropium bromide solvates co...
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JPWO2010113834A1 |
To provide a novel and excellent method for preventing and / or treating a disease related to a cannabinoid type 2 receptor based on an agonistic action on the cannabinoid type 2 receptor. A hetero ring derivative having mainly two subst...
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JP5042028B2 |
The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5...
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JP5042043B2 |
The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5...
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JP2012176975A |
To provide a novel crystalline form of tiotropium bromide.The crystalline tiotropium bromide is characterized by the X-ray powder diffraction pattern having peaks at approximately 8.7, 15.3, 15.5, and 25.3±0.2° 2θ.
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JP5022494B2 |
The present invention relates to compounds and formulations capable of affecting nicotinic acetylcholine receptors (nAChRs), for example, as modulators of specific nicotinic receptor subtypes (specifically, the alpha7 nAChR subtype). The...
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JP2012520884A |
Clemizole and clemizole analog compounds, and pharmaceutical compositions of the same, are useful in methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of inhibiting HCV replication in a hos...
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JP5008812B2 |
Antitumor compounds have the five membered fused ring ecteinascidin structure of the formula (XIV). The present compounds lack a 1,4-bridging group as found in the ecteinascidins. They have at the C-1 position a substituent selected from...
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JP2012153725A |
To provide crystalline salt forms of a quinolinone-carboxamide compound which are useful as 5-HT4 receptor agonists.There are provided a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5...
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JP5001480B2 |
Radiopharmaceutical compounds are disclosed. A tropane compound is linked through the N atom at the 8-position to a chelating ligand capable of complexing technetium or rhenium to produce a neutral labeled complex that selectively binds ...
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JP5001156B2 |
This invention relates to novel chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compo...
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JP2012517447A |
Provided herein is a method for chemically programmed vaccination. Methods include inducing a covalent-binding polyclonal antibody response in a subject and programming the polyclonal response with a targeting compound.
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JP4981683B2 |
The present invention relates to a method for preparation of organofluoro compounds containing radioactive isotope fluorine-18. More particularly, the present invention relates to a method for preparation of primary or secondary organofl...
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JP4986369B2 |
The invention relates to a new process for producing powdered preparations for inhalation.
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