Abstract: The invention relates to compounds of formula (I): wherein R1 and R2 together form the following carbon-containing chain: wherein: R3 represents a hydrogen atom or an alkyl group, R4 represents a hydrogen atom or an alkyl, aryl, heteroaryl, 3,4-dioxocyclobutenyl, alkylcarbonyl, cycloalkylcarbonyl, heterocycloalkylcarbonyl, benzoyl, arylsulphonyl or heteroarylsulphonyl group, each of those groups optionally being substituted, or R3 and R4 together with the nitrogen atom carrying them form a 5- to 8-membered ring, the ring thereby formed optionally being substituted. Medicinal products containing the same which are useful in treating conditions requiring a D3 receptor antagonist.

Abstract: The present invention relates to compounds of the Formula (I) which are useful for treating conditions associated with mGluR3 receptors, such as depression, schizophrenia and migraine, pharmaceutical compositions thereof, and methods of using the same.

Abstract: The present invention provides a compound having an excellent inhibitory action on melanin production and being useful as a whitening agent, and a skin external preparation containing the compound. The whitening agent of the present invention comprises, as an active ingredient, a compound represented by formula (1) or a pharmacologically acceptable salt thereof: wherein X1, X2, and X3 are each CR2 or N; R1, R2, and R3 are each H, C1-6 alkyl, C1-6 alkoxy, SH, OH, or NRbRc, wherein Rb and Rc are each H, C1-6 alkyl, or hydroxy-C1-6 alkyl, or NRbRc forms a saturated or unsaturated 5- or 6-membered hetero ring; and B is a substituted or unsubstituted pyrazole, imidazole, pyridine, or piperidine; with the proviso that at least one of R1, R3, R4, and R6 is a group other than C1-3 alkyl in the case where X1?X2?Y1?N and X3?CR2.

Abstract: An improved process for manufacture of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid calcium salt, which is useful for the production of a pharmaceutical useful in the treatment of, inter alia, hypercholesterolemia, hyperlipoproteinemia and atherosclerosis, is described.

Abstract: The present invention provides novel substituted pyrimidinyl-amines that are useful as inhibitors of protein kinases, especially c-Jun N-terminal kinases (JNK) and pharmaceutical compositions thereof and methods of using the same for treating conditions responsive to the inhibition of the JNK pathway.

Abstract: Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty liver, circulatory system diseases, for example, stenocardia, acute/congestive cardiac insufficiency, cardiac infarction, coronary arteriosclerosis, hypertension, nephropathy, sleep disorder and various diseases accompanied by sleep disorder such as idiopathic hypersomnia, repetitive hypersomnia, true hypersomnia, narcolepsy, sleep periodic acromotion disorder, sleep apnea syndrome, circadian rhythm disorder, chronic fatigue syndrome, REM sleep disorder, senile insomnia, night worker sleep insanitation, idiopathic insomnia, repetitive insomnia, true insomnia, electrolyte metabolism disorder; and central and peripheral nervous system diseases such as bulimia, emotional disorder, melancholia, anxiety, epilepsy, delirium, dementia, shinzophrenia, attention deficit/hyperactivity disorder, memory disorder, Alzheimer's diseas

Abstract: The present invention is directed to a compounds, methods and compositions for making the compounds and methods of treating a variety of diseases and disease states including atherosclerosis, arthritis, restenosis, diabetic nephropathy, or dyslipidemia, or disease states mediated by the low expression of Perlecan, comprising the administration of new heterocyclic compounds, particularly substituted pyrimidines.

Abstract: A 2-(N-methyl-N-methanesulfonylamino)pyrimidine compound of the formula (3): [R is a hydrocarbyl group], is prepared by the steps of: (I) reacting an isobutyrylacetate ester with 4-fluorobenzaldehyde and urea in the presence of a protonic compound and a metal salt; (II) oxidizing the reaction product of the step (I); (III) reacting the oxidation product of the step (II) with an organic sulfonyl halide or an organic sulfonyl anhydride; and (IV) reacting the reaction product of the step (III) with N-methyl-N-methanesulfonamide.

Abstract: The present invention relates to substituted pyrimidine compounds of formula I useful as orexin receptor antagonists. The invention also relates to pharmaceutical compositions containing said compounds.

Abstract: The present application relates to compounds of formula wherein the definitions are as described herein. The present compounds are high potential NK-3 receptor antagonists that are useful for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.

Abstract: The present invention relates to compounds of formula I: wherein R1, R2, R3, R4, R5, and R6 are defined herein.

Abstract: A series of N-substituted oxindole derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.

Abstract: Provided are alkyl ammonium crystalline salts of rosuvastatin that provide for purification of rosuvastatin and its pharmaceutically acceptable salts.

Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the pyrimidine to which it is fused, R4, R5, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.

Abstract: Compounds having formula I are provided where the variables have the values described herein. Pharmaceutical formulations include the compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier and combinations with other agents. A method of treating a patient comprises administering a pharmaceutical formulation according to the invention to a patient in need thereof.

Abstract: An amine, which is substituted by phenyl-substituted pyrimidin; and phenyl; and a third substituent and its use as an immunoglobulin E (IgE) inhibitor.

Abstract: The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor.

Abstract: A pharmaceutical composition for treating Alzheimer's disease containing a compound represented by the general formula (I); wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene, etc.; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a and R4b are each independently a hydrogen atom, halogen, hydroxy, etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 1 to 3; and R5 is a hydrogen atom, optionally substituted lower alkyl, etc.; its pharmaceutically acceptable salt, or a solvate thereof as an active ingredient.

Abstract: The present invention relates in general to anti-cancer drug design. More specifically, the invention provides methods of mapping and screening for anti-cancer agents using pharmacophore models. The invention demonstrates that, conformational sampling of a small lead molecule, followed by representative pharmacophore model development, is an efficient approach for rational design of novel anticancer agents with similar or better potency than the original lead but with different physicochemical properties.

Abstract: The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula I wherein Q, X, Y, Z, R1, R2, R4, m and n are as defined herein.

Abstract: A heterocyclic inhibitor having the formula I, with the variables defined herein, which is useful for treating inflammatory and other physiological disorders in which PKC-theta isoform plays a role:

Abstract: Disclosed is a compound represented by the general formula shown below, which can bind to a retinoid X receptor (RXR), which is one of nuclear receptors, and exhibit an agonistic or antagonistic action. [Wherein, R1 is selected from the group consisting of an alkyl group, an alkenyl group, an alkynyl group and an aryl group. R2 is selected from the group consisting of an alkoxy group, an alkyl group, an alkenyl group, an alkynyl group and an aryl group. W is NR3 or CR3; and R3 is selected from a hydrogen, an alkyl group, an alkenyl group, an alkynyl group and an aryl group. X1 and Y1 are selected from CH or N. X2 and Y2 are selected from CH, CR4 or N. R4 is selected from an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, a halogen, a nitro group and an amino group. Z is selected from a carboxylic acid, a carboxylate ester or a hydroxamic acid, which is bound directly or via an alkyl group, an alkenyl group or an alkynyl group.

Abstract: 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 aryl or heteroaryl group, possibly substituted by the substituents listed in the description.

Abstract: This invention relates to a compound of formula I, wherein R1, R2, R3, m, n, W, X and Y are as defined herein, or a physiologically tolerated salt thereof, its pharmaceutical composition and use for lowering blood glucose, treating diabetes, or increasing insulin release.

Abstract: The invention relates to compounds of formula (I) prodrugs thereof, and the pharmaceutically acceptable salts of the compounds and prodrugs, wherein Ra, Rb, R1 and R2 are as defined herein; pharmaceutical compositions thereof; and uses thereof.

Abstract: 5-Phenylpyrimidines of the formula I, in which the substituents have the following meanings: R1 is a five- to ten-membered saturated, partially unsaturated or aromatic mono- or bicyclic heterocycle comprising one to four hetero atoms selected from the group consisting of O, N or S, which heterocycle can be substituted as defined in the description, R2 is hydrogen, halogen, cyano, alkyl, haloalkyl or alkoxy; R3, R4 are hydrogen, alkyl, haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, haloalkenyl, cycloalkenyl, alkynyl, haloalkynyl or cycloalkynyl, R3 and R4 together with the nitrogen atom to which they are bonded may also form a five- or six-membered ring which can be interrupted by a hetero atom and have attached to it one or more substituents; R5, R6 are hydrogen, halogen, alkyl, haloalkyl or alkoxy; R7, R8 are hydrogen, halogen, alkyl or haloalkyl; R9 is hydrogen, halogen, alkyl, alkoxy, cycloalkoxy, haloalkoxy or alkoxycarbonyl, Processes and intermediates for the preparation of these compounds, and t

Abstract: Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are provided, said processes comprise: a) reacting 4-(2-cyanoethenyl)-2,6-dimethylbenzenamine with an intermediate of formula (III) in the presence of a suitable solvent; b) reacting an intermediate of formula (IV) with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent; c) dehydrating the corresponding amide of the compound of formula (I).

Abstract: The present invention is to provide a novel heterocyclic compound of the formula [I]: wherein R1 is a halogen, nitro, an alkyl, etc.; R2 is hydrogen, an alkyl, etc.; Ring A is 2-oxo-4-imidazolin-3,4-diyl, etc.; Ring B is a cycloalkyl, monocyclic saturated heterocyclic group; X is CH, N; Y is a single bond, CO, SO2; Z is O, NH, etc.; and Ring C is an aryl, a heterocyclic group, or a pharmaceutically acceptable salt thereof, which is useful as a p38 MAP kinase inhibitor.

Abstract: Compounds of the class 3,9-diaza-bicyclo [3.3.1]nonane derivatives. The compounds correspond to structural Formula (I): wherein Ra is hydrogen or optionally substituted alkyl and Rb is a monocyclic heteroaryl group. The compounds are useful in the treatment, prevention, or alleviation of diseases or disorders or conditions that are responsive to modulation of nicotinic acetylcholine receptors, including cognitive disorders, Alzheimer's disease, attention deficit hyperactivity disorder (ADHD), Tourette's syndrome, Bipolar Disorder, obsessive compulsive disorders (OCD), narcolepsy, senile dementia, autism, Parkinson'disease, Amyotrophic Lateral Sclerosis, epilepsy, and diabetic neuropathy.

Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders/diseases mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease, in particular pain such as inflammatory pain, neuropathic pain or visceral pain.

Abstract: The present invention provides (I) These compounds are useful in prevention and treatment of neurodegenerative disorders, such as Alzheimer's, Parkinson's and Huntington's as well as type II diabetes.

Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.

Abstract: This relates to novel pyrimidine derivatives, pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decrease in activity of the cannabinoid receptor.

Abstract: Substituted biaryl piperazinyl-pyridine analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptors activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Abstract: A compound represented by the following general formula (I), wherein R1, R2, R3, R4 and R5 represent hydrogen atom, a halo(lower alkyl) group, cyano group and the like, R6 represents an alkyl group, a cycloalkyl group and the like, R7, R8, R9 and R10 represent hydrogen atom, a halogen atom, a lower alkyl group, a halo(lower alkyl) group and the like, R11 and R12 represent hydrogen atom, a lower alkyl group, a (lower cycloalkyl) (lower alkyl) group and the like, and R13 represents hydrogen atom, a halogen atom, a lower alkoxy group and the like, which has potent inhibitory activity on cholesterol ester transfer protein (CETP).

Abstract: The present invention relates to new, potent DPP-IV enzyme inhibitors of the general formula (I), which contain fluorine atoms.

Abstract: The present invention relates to the novel compounds of the general formula (I) possessing dipeptidyl peptidase IV enzyme inhibitory activity, pharmaceutical compositions thereof, methods of using said compounds, processes for their preparation and intermediates of the general formulae (II), (IV), (V), (VII), (VIII) and (IX).

Abstract: The present invention is directed to processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine H4 receptor modulators, and to intermediates in H4 modulator synthesis.

Abstract: Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.

Abstract: The present invention relates to novel pyrimidine derivatives, pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decrease in activity of the cannabinoid receptor.

Abstract: In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted or unsubstituted six membered heterocyclic ring that includes at least two nitrogen atoms. The ring additionally includes four carbon atoms. The heterocyclic ring has at least one substituent located at a ring position adjacent to a ring nitrogen atom. This mandatory substituent of the ring includes a moiety (B), linked to the heterocyclic ring via a carbon-carbon triple bond. The mandatory substituent is positioned adjacent to the ring nitrogen atom. Invention compounds are capable of a wide variety of uses. For example heterocyclic compounds can act to modulate physiological processes by functioning as agonists and antagonists of receptors in the nervous system. Invention compounds may also act as insecticides, and as fungicides. Pharmaceutical compositions containing invention compounds also have wide utility.

Abstract: Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.

Abstract: Novel compounds having the general formula (I) below: are useful in a wide variety of applications in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively are formulated into cosmetic compositions.

Abstract: Multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use are described.

Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein R1, X, Z, R2, X1, Ar, n, R3 and R4 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR8 and accordingly are useful for the treatment of a variety of inflammatory and allergic disorders.

Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.

Abstract: Compounds represented by formula (1) shown below, pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising such compounds are provided.

Abstract: This invention comprises the novel compounds of formula (I) wherein t, R1, R2, L, Q, X, Y, Z and (a) have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.

Abstract: Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.