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JP5389917B2 |
The invention is concerned with novel heterocyclyl compounds of formula (I): wherein A, X, R3, R4, R5, R6, R7, R8, R9, R10, m, n and p are as defined in the description and in the claims, as well as physiologically acceptable salts there...
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JP5383513B2 |
The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine compounds, and structurally and functionally related compound...
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JP5368556B2 |
The invention is concerned with novel heterocyclyl compounds of formula (I) wherein A, X, Y1, Y2, Y3, R3, R4, R5, R6, R7, R8, R9, R10, m, n and p are as defined in the description and in the claims, as well as physiologically acceptable ...
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JP5364871B2 |
There is described a combination of ritonavir or a pharmaceutically acceptable salt thereof in combination with another HIV protease inhibitor, formulated as a single or separate composition, for use in the inhibition or treatment of an ...
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JP5355582B2 |
The present invention provides a novel benzodiazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The benzodiazepine compound of the invention is represented by General...
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JP5340177B2 |
Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions compris...
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JP5298103B2 |
Benzodiazepine derivative of formula (I), and pharmaceutically acceptable salts thereof, are found to be active against RSV Formula (I) Wherein: —R1 represents C1-6 alkyl, aryl or heteroaryl; —R2 represents hydrogen or C1-6 alkyl; -e...
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JP5274470B2 |
The present invention relates to new phenylsulfamoyl benzamide derivatives of formula (I) wherein R1-R5 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which ar...
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JP5264716B2 |
The present invention relates to benzodiazepine compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferati...
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JP5264160B2 |
A compound comprising a substituent of the formula (II) is disclosed as an HIV protease inhibitor. Intermediates for making such compounds and processes for making such intermediates are also disclosed.
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JP5250627B2 |
Novel compounds of which the following is exemplary:
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JP5246865B2 |
Provided are compositions and methods useful for modulation signaling through the Toll-like receptor TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versu...
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JP5220611B2 |
A 1,4-benzodiazepine derivative having an [(R)-1-(2-chloro-4-alkoxybenzoyl)-3-methyl-1,2,3,5- tetrahydrobenzo[e]-1,4-diazepine-4-carbonyl]amine skeleton, such as methyl=(S)-2-[[(R)-1-(2-chloro-4-ethoxybenzoyl)-3- methyl-1,2,3,5-tetrahydr...
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JP2013121919A |
To provide a pharmaceutical product, particularly a pharmaceutical composition having a plasma kallikrein inhibition activity, useful as a prophylactic or therapeutic agent for edemas (particularly hereditary vascular edema), and useful ...
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JP5215975B2 |
The present invention relates to acylated indanyl amines according to the general formula (I) wherein R1-R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1-C3-alkyl), B is CH2 or CH—(C1-C3-alkyl), and R5 is an ar...
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JP5208510B2 |
The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
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JP5208412B2 |
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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JP2013521250A |
The instant invention relates to derivatives of formula (I) and their application in therapeutics.
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JP5204231B2 |
Amide compounds (I) and their enantiomers, diastereomers, mixtures and salts, preferably with organic or inorganic acids or bases, are new. Amide compounds of formula (R 5>-A-R 4>-B1-R 3>-A-D1-Y1-N(R 2>)-SO 2-R 1>) (I) and their enantiom...
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JP5205266B2 |
The described invention relates to compounds (I) which modulate cell migration, and find use in, for example, wound healing, cancer progression and angiogenesis. All definitions as in claim 1.
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JP5203363B2 |
The invention relates to a compound (I) wherein R is a heterocyclyl radical; R 1 and R 2 are independently H or alkyl; R 3 is H, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, aryl, arylalkyl, heterocyclyl or heterocyclylalkyl; R 4 and R 5...
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JP2013519693A |
Compounds of formula (I) wherein m, R1, R2, R3, X and Y are defined herein, are useful as inhibitors of HIV replication.
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JP2013082729A |
To provide substituted phenoxyacetic acids useful as pharmaceutical compounds for treating a respiratory disorder, a pharmaceutical composition containing them, and a method of manufacturing them.The compounds of formula (I) or pharmaceu...
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JP2013075910A |
To provide a novel improved salt of a known compound of formula I.The invention relates to salts of 1-(2-fluoro-phenyl)-3-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e
][1,4]diazepin-3-yl)-urea and crystalline forms thereof, their production an...
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JP5186219B2 |
The invention relates to 5-HT6 receptor antagonists. Novel arylamine compounds and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated ...
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JP2013512272A |
Compounds of the formula I: wherein m, n, X1, X2, Y1, Y2, R1 and R2 are as defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
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JP5179486B2 |
The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT1 such as cognitive disorders as...
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JP2013505914A |
The invention relates to a novel class of [1,4]-benzodiazepine derivatives, processes for their preparation, intermediates usable in these processes, and pharmaceutical compositions containing the compounds. Other aspects of the inventio...
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JP5148646B2 |
Novel cycloalkyl compounds useful as inhibitors of potassium channel function (especially inhibitors of the K v l subfamily of voltage gated K + channels, especially inhibitors K v 1.5 which has been linked to the ultra-rapidly activatin...
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JP2013505258A |
The invention provides 1,4-benzodiazepinone compounds, pharmaceutical compositions, and methods of treating autoimmune disorders, chronic inflammatory disorders, and hyperproliferative disorders. For example, the 1,4-benzodiazepinone com...
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JP2013503829A |
The invention relates to compounds of the general formula (1) or the acid addition salts thereof with organic and/or inorganic acids; as well as to the use of the compounds of the general formula (1) in medicine.
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JP2013014628A |
To provide heterocyclic aspartyl protease inhibitors, pharmaceutical compositions comprising the compounds, their use in the treatment of cardiovascular diseases, cognitive and neurodegenerative diseases, and their use as inhibitors of t...
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JP5127096B2 |
Benzodiazepine compounds, and methods for using those compounds are provided. Some of the benzodiazepine compounds include 1,4-benzodiazepine-2-one and 1.4-benzodiazepine-2,5-dione compounds of structures (I) or (II): wherein R 1 , R 2 ,...
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JP5117382B2 |
A 7-membered heterocyclic compound having the formula (I), or its salt, or a solvate thereof with a chymase inhibitory action and useful for the prevention or treatment of various diseases, in which chymase is involved: a method for prod...
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JP5114202B2 |
The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergi...
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JP5106107B2 |
The present invention relates to a novel class of paramagnetic ion-based contrast agents of formula (I), wherein a chelating backbone moiety is highly functionalized by the presence of one or more polyhydroxylated chain, that show a phar...
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JP2012229185A |
To provide a novel aniline derivative having pharmaceutical actions such as excellent neuroprotective action, neurogenesis (neurorestorative) promoting action and cognitive function improving action.The aniline derivative is a compound r...
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JP5073149B2 |
The present invention relates to acylated indanyl amines according to the general formula (I) wherein R1-R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1-C3-alkyl), B is CH2 or CH—(C1-C3-alkyl), and R5 is an ar...
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JP5054877B2 |
Preparation of cyclic urea compounds (I) from activated carbamic acid derivative(s) (II) is new. Preparation of cyclic urea compounds (I) from activated carbamic acid derivative(s) (II) containing a non-protected primary or secondary ami...
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JP2012525442A |
Compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) acting to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating...
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JP2012525356A |
The present invention relates to novel benzenesulfonanilide compounds of the formulae I and I′ and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are pa...
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JP2012525355A |
The present invention relates to novel benzenesulfonanilide compounds of the formulae I and I′ and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are pa...
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JP2012524789A |
Provided herein are 2,5-disubstituted arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or ...
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JP2012197305A |
To provide novel compounds and methods to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, and hyperproliferation, and the like.Benzodiazepine deriv...
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JP5047777B2 |
The invention provides N,N'-disubstituted monothiourea or bis-thiourea-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 catalyzed...
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JPWO2010113458A1 |
Provided is an industrially advantageous method for producing a 1,5-benzodiazepine compound. Compound (5) is obtained by the following reaction formula, and this is used as an intermediate.
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JP5042987B2 |
Compounds of the formula (I), in which the radicals R1 to R3 and AR are as defined in the description, processes for the preparation thereof, the use thereof in the treatment of cardiovascular diseases, and pharmaceutical compositions co...
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JP5041814B2 |
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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JP2012184225A |
To provide a medicine having atrial-selective K+ channel blocking action.The medicine is a diazepine compound represented by general formula (1), wherein R1 to R4 are each independently H, lower alkyl or the like, R2 and R3 may form lowe...
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JP5033301B2 |
The polyarylcarboxamide compound (+)-phenyl-(4-{4-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-a
mino]-phenyl}-piperidin-1-yl)-acetic acid methyl ester is useful as a lipid lowering agent.
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