Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.

Abstract: The invention provides a process for preparing a compound of formula (I) and pharmaceutically acceptable derivatives thereof wherein: R0 and R1 are independently selected from H, halogen, C1-6alkyl, C1-6alkoxy, or C1-6alkoxy substituted by one or more fluorine atoms; R2 is H, C1-6alkyl, C1-6alkyl substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulfonyl, C1-6alkoxy substituted by one or more fluorine atoms, halogen, CN, CONR4R5, CO2H, CO2C1-6alkyl, or NHSO2R4; R3 is H or phenyl substituted by SO2C1-6alkyl or SO2NH2; R4 and R5 are independently selected from H, C1-6alkyl, phenyl, phenyl substituted by one or more atoms or groups R6, or together with the nitrogen atom to which they are attached form a saturated 4 to 8 membered ring R6 is halogen, C1-6alkyl, C1-6alkoxy or C1-6alkoxy substituted by one or more fluorine atoms; which comprises rearrangement of an azirine of formula (II)  wherein R0 to R

Abstract: Disclosed is a compound represented by Structural Formula (I): R1 is a substituted or unsubstituted 2-imidazolyl group which is optionally fused to a substituted or unsubstituted aryl group. Z1 is ═O, ═S, ═NOR11, or ═NR11. R is represented by a Structural Formula selected from (II)-(VII): The variables in Structural Formulas (II)-(VII) are described below.

Abstract: The present application describes novel cyclic hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NR1, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-&agr; converting enzyme (TACE), aggrecanase or a combination thereof, pharmaceutical compositions containing the same, and methods of using the same.

Abstract: A process for preparing a compound of formula (II) 1

Abstract: The invention concerns novel oxidative composition for dyeing keratinous fibres comprising at least a 3-amino-pyrazolo-[1,5-a]-pyridine of Formula (I), the dyeing method using said composition, novel 3-amino pyrazolo-[1,5-a]-pyridines, and the method for preparing them.

Abstract: Described herein are compounds useful in the treatment of migraine, which have the general formula: wherein: W is a CH group or a N atom; Z is N or C—R4; B and D are selected independently from CH and N, with the proviso that at least one of B and D is CH and with the further proviso that one of B and D can represent N only when W and Z are both other than N; A is a group of Formula II, III or IV, such that group A contains at least 1 N atom; NR7 is either —NH— or —N═; is a single or double bond; X is a N atom, a CH group or a C(OH) group when is a single bond; or, when is a double bond, a C atom; Y is an NH, N-alkyl, N-benzyl or CH2 group; U and V each represent a N atom or a CH group, with the proviso that both cannot be N; a and b are, independently, 0 or 1; c is an integer from 0 to 3; d is an integer from 1 to 3; e is an integer from 1 to 2; f is an integer from 0 to 3; g is an integer from 3 to 6 and h is an integer from 2 to 3; such that the sum of c a

Abstract: The use of substituted imidazoazines of the formula I, 1

Abstract: A Tert.-butyl-(7-methyl-imidazo[1,2-a]pyridin-3-yl)-amine derivatives of Formula I: wherein the pharmaceutically acceptable salts, methods of making and method of use, in particular for the treatment of migraine.

Abstract: Certain compounds which contain a piperidine moiety flanked by aryl groups are inhibitors of p38-&agr; kinase and thus useful in the treatment of a variety of conditions characterized by inappropriate p38-&agr; kinase activity.

Abstract: A compound of formula (I): wherein: R1 represents hydrogen, or linear or branched (C1-C6)alkyl optionally substituted by one or more identical or different groups selected from aryl, heteroaryl, cycloalkyl and heterocycloalkyl, represents a saturated ring having from 4 to 7 ring members that may contain, in addition to nitrogen, one or two hetero atoms selected from O, S and —NR3 groups, wherein R3 represents hydrogen or linear or branched (C1-C6)alkyl, n represents an integer such that 1≦n≦6, R2 represents any one of the groups described in the description, their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as inhibitor of trypsin-related serine proteases and thrombin.

Abstract: The present invention relates to novel compounds having a phosphatidylinositol 3 kinase (PI3K) inhibiting activity which are useful as medicaments, more particularly as antitumor agent. Novel 3-(imidazo[1,2-a]pyridin-3-yl) derivatives or salts thereof exhibit an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity, and are thus useful as medicaments, especially as PI3K inhibitors and antitumor agents.

Abstract: Compounds of formula (I), in which the substituents have the meanings mentioned in the description, are valuable intermediates for preparing active compounds for the prevention and treatment of gastrointestinal diseases.

Abstract: Compounds of formula I wherein A represents: and R, R1, R2, R3 and R4 are as defined in the specification, pharmaceutically-cceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially in the treatment or prophylaxis of psychotic disorders and intellectual impairment disorders.

Abstract: Substituted bicyclic imidazo-3-yl-amines and medicaments comprising these compounds, useful, inter alia, as analgesics.

Abstract: Azaindolizinon derivatives or pharmaceutically acceptable salts thereof represented by the formula I: wherein R1 represents hydrogen atom, halogen atom or C1-C6 alkyl, R2 represents hydrogen atom, C1-C6 alkyl, C1-C6alkoxy, hydroxy, halogen atom, amino, acetylamino, benzylamino, trifluoromethyl or —O—(CH2)n—R5 (R5 represents vinyl, C3-C8 cycloalkyl or phenyl, n being 0 or 1), R3 and R4 respectively represent C1-C6 alkyl or —CH(R7)—R6 (wherein R6 represents vinyl, ethynyl, phenyl (which may be substituted with C1-C6 alkyl, C1-C6 alkoxy, hydroxy, one or two halogen atoms, di C1-C6 alkylamino, cyano, nitro, carboxy or phenyl), phenethyl, pyridyl, thienyl or furyl and R7 represents hydrogen atom or C1-C6 alkyl) or R3 is coupled with R4 to form indan or dihydrophenalene.

Abstract: This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof wherein R1 is hydrogen, halo or alkyl; R2 and R3 are independently hydrogen, alkyl, alkenyl, alkynyl, aminoalkyl or hydroxyalkyl; or R2 and R3 taken together with the nitrogen atom to which they are attached may form hetrocyclic; R4 is hydrogen, halo, acyl, amino, amido, aryl, arylalkyl, or heteroaryl; R5 is hydrogen, halo, alkyl alkenyl, alkynyl, acyl, amino, amido, aryl, arylalkyl, or heteroaryl; R6 is hydrogen, alkyl or alkoxyalkyl; X is NR9 wherein R9 is hydrogen or alkyl; and Y is (CR7R8)n wherein n is an integer from 0 to 5. These compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, Functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

Abstract: A sulfamoyl compound of the general formulae (1): wherein R1 and R2 are each independently C1-4 alkyl, or R1 and R2 together are C4-6 alkylene or C4-6 alkyleneoxy, Y is H, halogen, C1-8 alkyl, C1-8 alkoxy, C1-8 alkylthio, C1-8 haloalkyl, C1-8 haloalkoxy or C1-8 haloalkylthio, A is a predetermined heterocyclic group, B is a predetermined heterocyclic group which is identical with or different from A, W is a chemical bond or O, V is O or S, D, E, F and G are each independently N, CR7, CR8, CR9 or CR10, and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are each independently predetermined group such as H, or an unsubstituted or substituted aliphatic, aromatic or heterocyclic group. The sulfamoyl compound is useful as an agricultural and horticultural fungicide.

Abstract: The present invention relates to novel compounds, and therapeutically acceptable salts thereof of the formula (I), which inhibit exogenously or endogenously stimulated gastric acid secretion and thus can be used in the prevention and treatment of gastrointestinal inflammatory diseases.

Abstract: Nucleoside analogues or base analogues having structure (I), where X=O or NH or S, Y=N or CHR6 or CR6, W=N or NR6 or CHR6 or CR6 or S, n=1 or 2; each R6 is independently H or O or alkyl or alkenyl or alkoxy or aryl or a reporter moiety; where necessary (i.e. when Y and/or W is N or CR6 where R6 is not O) a double bond is present between Y and W or W and W, and Q is H or a sugar or a sugar analogue or a nucleic acid backbone or backbone analogue.

Abstract: The present invention relates to a process for preparing 3-acylamino imidazo[1,2-a]pyridines having the formula: 1

Abstract: The present invention is a series of novel compounds of formula I and a method of treatment or prevention of a mGluR5 receptor mediated disease by administering an therapeutically effective amount of a compound formula wherein R1 and R2 are selected from hydrogen, (C1-6)-alkyl, halogen, hydroxy, (C1-6)-alkoxy and A is defined the description, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.

Abstract: The invention relates to a process for preparing a compound of formula (I) wherein a compound of formula (II),  wherein R1 denotes chlorine, bromine, iodine, —O—COCH3, tosylate or mesylate, is reacted with a compound of formula (III),  optionally in a suitable diluent and/or in the presence of a suitable added reagent or catalyst, the reaction being carried out in a temperature range from 20 to 80° C.

Abstract: The present invention relates to novel compounds, and therapeutically acceptable salts thereof of the formula (I), which inhibit exogenously or endogenously stimulated gastric acid secretion and thus can be used in the prevention and treatment of gastrointestinal inflammatory diseases.

Abstract: Stable Crystalline chloride or bromide salts of swainsonine are prepared.

Abstract: Disclosed is a compound represented by Structural Formula (I): 1

Abstract: The invention relates to a process for preparing a compound of formula (I) wherein a compound of formula (II),  wherein R1 denotes chlorine, bromine, iodine, —O—COCH3, tosylate or mesylate, is reacted with a compound of formula (III),  optionally in a suitable diluent and/or in the presence of a suitable added reagent or catalyst, the reaction being carried out in a temperature range from 20 to 80° C.

Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X, A, B, C, D and W are defined herein, which compounds bind with high selectivity and high affinity to the benzodiazepine site of the GABAA receptors and are therefore useful in the treatment of certain central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples.

Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.

Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1&bgr; converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-&ggr; inducing factor-(IGIF), or interferon-&ggr;-(“IFN-&ggr;”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases.

Abstract: The invention provides the compounds of formula (I) wherein: R0 and R1 are independently selected from H, halogen, C1-6alkyl, C1-6alkoxy, or C1-6alkoxy substituted by one or more fluorine atoms; R2 is halogen, CN, CONR4R5, CO2H, CO2C1-6alkyl, or NHSO2R4; R3 is C1-6alkyl or NH2; and R4 and R5 are independently selected from H, C1-6alkyl, phenyl, phenyl substituted by one or more atoms or groups (selected from halogen, C1-6alkyl, C1-6alkoxy, or C1-6alkoxy substituted by one or more fluorine atoms), or together with the nitrogen atom to which they are attached form a saturated 4 to 8 membered ring; and pharmaceutically acceptable derivatives thereof. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.

Abstract: A class of 3-phenylimidazo[1,2-a]pyridine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.

Abstract: The present invention is a series of novel compounds of formula I and a method of treatment or prevention of a mGluR5 receptor mediated disease by administering an therapeutically effective amount of a compound formula 1

Abstract: New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.

Abstract: The present invention relates to compounds of the formula (I): wherein: Het represents a heterocyclic residue selected from: where the dotted line in (b) represents an optional double bond; A completes a fused pyridine ring; and B completes a fused benzene or pyridine ring. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.

Abstract: Methods of making substituted pyrazolopyrimidines generally and, more particularly, N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-&agr;]pyrimidin-7-yl}phenyl)acetamide. Such compounds have utility over a wide range of indications, including treatment of insomnia. In the practice of the present invention, improved techniques which do not require use and/or isolation of the pyrazole intermediate are disclosed, as well as improved techniques for making the reaction intermediates themselves. Such techniques offer significant advantages, including enhanced efficiency, particularly in the context of large scale manufacture.

Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein A, B, C, D, Y, R1, R3, R4, R5, and R6 are variables defined herein, which compounds are modulators of Bradykinin B2 receptors. These compounds are useful in the diagnosis and treatment of renal diseases, heart failure, hypertension, Meniere's disease, vaginal inflammation and pain, peripheral circulatory disorders, climacteric disturbance, retinochoroidal circulatory disorders, myocardial ischemia, myocardial infarction, postmyocardial infarction syndrome, angina pectoris, restenosis after percutaneous transluminal coronary angioplasty, hepatitis, liver cirrhosis, pancreatitis, ileus, diabetes, diabetic complications, male infertility, glaucoma, pain, asthma, and rhinitis and for the increase of permeability of the blood-brain barrier or the blood-brain-tumor barrier.

Abstract: Mercaptoalkanoylamino lactam acids are recrystallized by treatment with an agent that minimizes the formation of disulfides. Suitable agents are bismercaptans, phosphine or phosphite reducing agents, zinc metal powder, and sodium hydrosulfite.

Abstract: The present invention provides for novel polymorphs of zolpidem hemitartrate and the preparation of the polymorphs.

Abstract: It comprises reducing the hydroxy ester of formula (X) by reacting it in DMF and then with an iminium salt of formula (XIII) formed in situ with thionyl chloride and dimethylformamide, and subsequent reduction with an appropriate reducing agent to form the ester of formula (XII), which is then reacted with dimethylamine in a polyhydroxylated solvent medium at an appropriate

Abstract: The present invention relates to novel compounds having a phosphatidylinositol 3 kinase (PI3K) inhibiting activity which are useful as medicaments, more particularly as antitumor agent. Novel 3-(imidazo[1,2-a]pyridin-3-yl) derivatives or salts thereof exhibit an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity, and are thus useful as medicaments, especially as PI3K inhibitors and antitumor agents.

Abstract: The invention relates to new heterocyclylbenzonitriles of the general formula (I) in which R1, R2, R3 and Het have the meanings given in the description, new processes and new intermediate products for their preparation and their use as herbicides.

Abstract: The present invention relates to compounds selected from the group consisting of: (i) the compounds of the formula  in which X is a halogen atom, A is a group —NH—(CH2)n—NH—CO—, —NH—CH2— or Q is a group R1 is hydrogen, halogen, C1-C3 alkyl or C1-C5 1-oxoalkyl, R2 is H or OH and n is 2, 3 or 4; and (ii) their addition salts. It further relates to the process for their preparation and to their use in therapeutics, especially for combating pathological conditions involving bradykinin.

Abstract: A process for the preparation of 2-phenyl-imidazo[1,2-a]pyridine-3-acetamides comprises the reaction of a 2-phenyl-imidazo[1,2-a]pyridine with an oxalic ester reactive derivative, followed by reduction of the carbonyl group and reaction with an amine.

Abstract: The invention provides imidazo [1,2-a] pyridines of formula (1), wherein Y is selected from F, Cl, Br, I, OH, SH, NH2, CN and COOH; Z is selected from N(R3)C(O)R4 and C(O)NR3R4; R1, R2, R3, R4 can represent various radicals; m and n are independently 0, 1 or 2; and p is an integer from 1 to 4; radiolabelled derivatives and pharmaceutical compositions thereof. The compounds of the invention are useful for the diagnosis and treatment, including radiotherapy, of disorders that are characterized by an abnormal density of peripheral benzodiazepine receptors.

Abstract: The invention concerns compounds of formula (I), wherein: A is a 5 membered heteroaryl ring, a bicyclic benzo system containing such a 5 membered heteroaryl ring or a bicyclic or tricyclic heteroaryl ring system with at least one bridgehead nitrogen and optionally a further 1-3 heteroatoms chosen from oxygen, sulfur and nitrogen; R1 is, for example, hydroxy, halo, amino, nitro, cyano, carboxy, thiol, C1-4alkanoyloxy, C1-4alkoxycarbonyl, dimethylaminomethyleneaminocarbonyl, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, optionally substituted phenyl, an optionally substituted 5- or 6-membered heteroaryl ring or hydroxyC1-4alkyl; n is 0-6; R2 and R3 are independently hydrogen or fluoro; R4 is, for example, C1-4alkyl; pharmaceutically acceptable salts and in vivo hydrolysable ester thereof; processes for their preparation; pharmaceutical compositions containing them and their use as antibacterial agents.

Abstract: The present invention relates to compounds of Formula (I) below, which inhibit the growth of picornaviruses, Hepatitus viruses, enteroviruses, cardioviruses, polioviruses, coxsackieviruses of the A and B groups, echo virus and Mengo virus. wherein: A is phenyl, pyridyl, substituted phenyl, substituted pyridyl, or benzyl; R is hydrogen, COR4, or COCF3; X is N—OH, O, or CHR1; R1 is hydrogen, halo, CN, C1-C4 alkyl, —C≡CH, CO(C1-C4 alkyl), CO2(C1-C4 alkyl), or CONR2R3; R2 and R3 are independently hydrogen or C1-C4 alkyl; A′ is hydrogen, halo, C1-C6 alkyl, benzyl, naphthyl, thienyl, furyl, pyridyl, pyrollyl, COR4, S(O)nR4, or a group of the formula R4 is C1-C6 alkyl, phenyl, or substituted phenyl; n is 0, 1, or 2; R5 is independently at each occurrence hydrogen or halo; m is 1, 2, 3, or 4; and R6 is hydrogen, halo, CF3, OH, CO2H, NH2, NO2, CONHOCH3, C1-C4 alkyl, or CO2(C1-C4 alkyl), C1-C4 alkoxy; or a pharmaceutically acceptable salt thereof.

Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R3, R4, R5, R6, R7, R8, X, n, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.

Abstract: A sulfamoyl compound of the general formulae (1): wherein R1 and R2 are each independently C1-4 alkyl, or R1 and R2 together are C4-6 alkylene or C4-6 alkyleneoxy, Y is H, halogen, C1-8 alkyl, C1-8 alkoxy, C1-8 alkylthio, C1-8 haloalkyl, C1-8 haloalkoxy or C1-8 haloalkylthio, A is a predetermined heterocyclic group, B is a predetermined heterocyclic group which is identical with or different from A, W is a chemical bond or O, V is O or S, D, E, F and G are each independently N, CR7, CR8, CR9 or CR10, and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are each independently predetermined group such as H, or an unsubstituted or substituted aliphatic, aromatic or heterocyclic group. The sulfamoyl compound is useful as an agricultural and horticultural fungicide.