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JP4545152B2 |
The invention relates to a process for preparing N-substituted 3beta-aminonortropanes of formula I wherein R1 has the meaning given in the claims, from the corresponding 3-oxonortropane or the corresponding 3 alpha-aminonortropane, in wh...
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JP2010529993A |
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or dysregulated B cell activi...
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JP4529685B2 |
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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JP2010527953A |
A method for the production of quaternised scopine esters of optionally substituted diphenylacetic acids, involves the one-step reaction of quat. salts of scopine with the corresponding acids or their derivatives such as esters. A method...
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JP4527406B2 |
The invention relates to bicyclic heterocycles of general formula (I), in which R, R, R, A, B, C, D, E and X are defined as in Claim 1, to tautomers, stereoisomers, mixtures and salts thereof, particularly their physiologically compatibl...
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JP2010527357A |
The invention provides methods of bowel preparation before a diagnostic, surgical or therapeutic procedure, in particular, bowel preparation before a colonoscopy procedure, using a 5-HT4 receptor agonist as a prokinetic agent.
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JP4522651B2 |
Disclosed are novel compounds of the formula Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, alle...
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JP2010526763A |
The present invention relates to novel pharmaceutical compositions based on a new anticholinergic and a new long-acting beta2~agonist, processes for the preparation thereof and the use thereof in the treatment of respiratory complaints.
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JP2010526777A |
The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydro-genase type 1 (11βHSD1) and the use of these compounds as pharmaceutical composi-tions, are described. Also a novel class of substituted amides, th...
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JP2010526122A |
This invention relates to novel chromen-2-one derivatives useful as starting material for synthesis of pharmaceuticals. On other aspects the invention relates to a method of preparing the chromen-2-one derivatives of the invention.
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JP2010525020A |
The present invention relates to heterocyclic compounds of the formula (I) wherein - the heterocycle comprises two double bonds which may be present at several positions, represented by the dashed lines ( -- ); - the heterocycle contains...
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JP4509565B2 |
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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JP4505135B2 |
Compounds of general formula (I)in which U represents a group of general formula (A) or (B)in which formulae V represents a hydrogen or halogen atom, a (C1-C3)alkyl group or one or two (C1-C3)alkoxy groups, W and X each represent, respec...
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JP4502804B2 |
Heterocyclic amides useful as inhibitors of dipeptylpeptidase-IV (DPP-IV) enzyme, process for the preparation thereof and intermediates therefore.
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JP4500689B2 |
The present invention provides a compound represented by the following formula (I); [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like; formula (I-1) represents a single bond or a double...
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JP2010522766A |
A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the a...
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JP4496377B2 |
The present invention relates to a method of preparing BCH-189 and various analogues of BCH-189 from inexpensive precursors with the option of introducing functionality as needed. This synthetic route allows the stereoselective preparati...
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JP4497814B2 |
The invention relates to heterocyclic substituted urea derivatives of the formula (I) that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disor...
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JP4497815B2 |
The invention relates to heterocyclic substituted amide derivatives of formula (I) that display selective binding to dopamine D 3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorde...
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JP4490421B2 |
The present invention provides a method for the treatment of schizophrenia which comprises administering a compound of formula wherein the substituents are as described herein or a pharmaceutically active acid-addition salt thereof. In p...
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JP4485192B2 |
Preparation of tropenol (I) involves: (a) reducing a scopine ester (II) using zinc in presence of an activating metal salt; and (b) saponifying the product using base. Preparation of tropenol of formula (I) (or its acid addition salt) in...
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JP4484521B2 |
The invention relates to novel anticholinergic agents of general formula (1), in which X - and the groups A, B, R, R1, R2, R3, R3', R4, R4', Rx and Rx' can be defined as per the claims and the description. The invention also relates to a...
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JP4484522B2 |
Esters (I) of fluorene-9-carboxylic acid with a bicyclic nitrogen heterocycle are new. Esters, of formula (I), of fluorene-9-carboxylic acid with a bicyclic nitrogen heterocycle are new. [Image] A : -CH 2CH 2-, -CH=CH- or oxiranyl; X ->m...
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JP2010520172A |
The invention relates to a hydrochloride salt of (1R,2R,3S,5S)-3-(3,4-dichlorophenyl)-2-[(methyloxy)methyl]-8
-azabicyclo[3.2.1]octane, uses of the salt as a medicament in the treatment inter alia of disorders of the central nervous syst...
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JP2010519216A |
The present invention relates to a CCR5 antagonist compound for elevating high density lipoprotein (HDL) particles in a patient, improving plasma lipid profile in a patient or reducing triglycerides in a patient. The invention also relat...
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JP2010518043A |
The present invention relates to compounds of formula I wherein A and R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of d...
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JP2010516616A |
Preparing ammonium hexafluorophosphate compound (I) comprises: reacting quaternary ammonium compound (a) with a phosphate salt compound (b) in the presence of solvent to give (I), which is not a tiotropium hexafluorophosphate compound (I...
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JP4460292B2 |
5-Substituted 2,4-diamino-pyrimidine derivatives (I) are new. Pyrimidines of formula (I) (including tautomers, racemates, enantiomers, diastereomers and their mixtures) and their acid addition salts are new. [Image] R aH or T; T : 1-4C a...
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JP2010514693A |
The invention provides novel compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.
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JP2010513458A |
The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are as defined herein, compositions containing such compounds and the uses of such compounds f...
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JP2010513392A |
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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JP2010513456A |
This invention provides compounds of the formula: useful in the inhibition or modulation of serine palmitoyl transferase and their use in methods of treatment or amelioration of type 2 diabetes, type 1 diabetes, insulin resistance, the e...
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JP2010513391A |
This invention relates to novel chromen-2-one derivatives of Formula (I) 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 pharm...
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JP2010510987A |
Heteroaryl amide derivatives suitable as P2X7 receptor antagonists of the following Formula are provided. The compounds can be applied in the treatment of pain, inflammation, a neurological or neurodegenerative disorder, a centrally-medi...
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JP4447663B2 |
The invention disclosed herein relates to novel a 8-azabicyclo[3.2.1]oct-2-ene compound of Formula II, wherein R is hydrogen, methyl, ethyl or benzyl; and R1 is 3-thienyl, 2-thienyl, 2-(3-methoxymethyl), 3-quinolinyl, 3-benzofuryl, 2-ben...
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JP2010510186A |
The invention relates to a new crystalline form of tiotropium bromide, processes for preparing it and its use for preparing a pharmaceutical composition for the treatment of respiratory complaints, particularly for the treatment of COPD ...
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JP2010510224A |
The present invention is directed to novel aminopyrrolidines of formula I pharmaceutically acceptable salts thereof, metabolites thereof, isomers thereof, stereoisomers thereof or pro-drugs thereof, wherein the variables are as defined h...
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JP4435687B2 |
CGRP antagonists of the formula of which the following are exemplary: (1) 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidi
ne-1-carboxylic acid-{(R)-1-(3,4-diethyl-benzyl)-2-[4-(1-methyl-piperidin-4-
yl)-piperazin-1-yl]-2-oxo...
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JP2010043116A |
To provide a new method for industrially producing tropenol, optionally in the form of an acid addition salt thereof, which is usable as a starting material for preparing a pharmacologically effective compound.The production method for t...
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JP2010037341A |
To provide new compounds having tolerability higher than morphine and effective on treating pain etc.The compounds are nonane and decane diazabicyclic derivatives having homopiperazine as a main ring, affinity for the opioidergic and/or ...
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JP2010024239A |
To provide an inhibitor to enterokinesis aggravative action caused by nonsteroidal anti-inflammatory drugs, and to provide an antiinflammatory composition decreased in enterokinesis aggravating action.The inhibitor to enterokinesis aggra...
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JP2010501540A |
The invention pertains to pyrimidone compounds that serve as effective GSK-3 inhibitors. The invention further relates to pharmaceutical compositions and methods comprising such pyrimidone compounds; and the use of such compounds for tre...
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JP4401296B2 |
The invention relates to CGRP antagonists of general formula (I), in which A, U, V, W, X and R<1> to R <3> are as defined in claim 1, the tautomers, diastereomers, enantiomers, hydrates, mixtures, salts, hydrates of the salts, in particu...
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JP4390559B2 |
A compound of formula wherein the substituents are as defined in the specification and their use as pharmaceutical, particularly for treatment of disorders mediated by the action of steroid sulfatase.
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JP2009543812A |
A compound of Formula I: and a method for treating a 5-HT2C receptor-mediated disorder in a mammal using the same.
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JP2009542670A |
The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.
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JP2009541464A |
The present invention is related to a compound of formula (I) wherein R1a, R1b, R1c, R1d, R2a, R2b, R3, R4, p, r and are as defined herein, its preparation, pharmaceutical composition and use as a modulator of the activity of the 11β-hy...
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JP2009540013A |
The present invention relates to 2-arylamino-4-(heterocyclic)aminopyrimidines inhibitors which are inhibitors and therefore inhibit Protein Kinase C-alpha (PKC-α). The PKC-α inhibitors of the present invention are important for improvi...
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JP2009539833A |
Compounds of Formula IA, or pharmaceutically acceptable salts thereof: IA wherein G1, G2, G3, G4, R1, R2, X, Y, Z and n are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prep...
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JP4366532B2 |
The present invention relates to a compound represented by Formula ÄIÜ Äwherein represents an aromatic carbo- or heterocyclic ring which may have a substituent; Cy represents a mono-, bi- or tricyclic aliphatic carbocyclic group havin...
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