Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: The present invention is directed to certain hydropyranopyrrolidine compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

Abstract: This invention relates to novel potassium channel modulating agents, and their use in the preparation of pharmaceutical compositions.

Abstract: The present invention is related to benzazole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzazole derivatives. Said benzazole derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and/or 3. The present invention is furthermore related to novel benzazole derivatives as well as to methods of their preparation. X is O, S or NR0, with R0 being H or an unsubstantiated or substituted C1-C6 alkyl; G is an unsubstantiated or substituted pyrimidinyl group.

Abstract: A liquid crystal compound represented by the following formula is provided to enhance the contrast of a liquid crystal device using ferroeloctric liquid crystal: R1 is an alkyl group having 4 to 6 carbon atoms. R2 is an alkyl group having 6 to 18 carbon atoms or an alkoxy group having 6 to 18 carbon atoms. X1 and X2 are each independently hydrogen ox fluorine.

Abstract: GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein A, Q, R1, R2, R3a, R3b, R4, R5, R6 and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

Abstract: HIF-1 inhibitors and methods of use thereof are provided.

Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oglimers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R?; J is sulfur or oxygen; R?, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.

Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia.

Abstract: This invention relates to a group of novel chelating agents, novel chelates, biomolecules labeled with said chelates or chelating agents as well as solid supports conjugated with said chelates, chelating agents or labeled biomolecules. Especially the invention relates to novel chelating agents useful in solid phase synthesis of oligonucleotides or oligopeptides and the oligonucleotides and oligopeptides so obtained.

Abstract: Compounds of the formula I in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors.

Abstract: Disclosed are therapeutic tetrahydroisoquinoline compositions for the treatment of cancer, these compositions having selectivity for cancer cells while demonstrating few, if any, deleterious side effects on normal cells.

Abstract: A glucokinase activator is provided; and a treatment and/or a preventive for diabetes, or a treatment and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a treatment and/or a preventive for obesity are provided. The invention relates to a compound of a formula (I): [wherein R1 and R2 represent a hydrogen, etc.; R3 represents a hydrogen atom, a halogen atom, etc.; R4 each independently represents a hydrogen atom, a lower alkyl group, etc.; Q represents a carbon atom, a nitrogen atom or a sulfur atom (the sulfur atom may be mono- or di-substituted with an oxo group); R5 and R6 each represent a hydrogen atom, a lower alkyl group, etc.

Abstract: The present invention is directed in part towards methods of modulating the function of calcium channels with pyrimidine-based compounds. In addition, the invention describes methods of preventing and treating calcium channel-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to pyrimidine-based compounds and pharmaceutical compositions comprising these compounds.

Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R?; J is sulfur or oxygen; R?, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrite, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.

Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R?; J is sulfur or oxygen; R?, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.

Abstract: A compound of formula (1), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.

Abstract: Selective antagonists of A2B adenosine receptors like those of formula I are provide. The compounds and compositions are useful as pharmaceutical agents.

Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.

Abstract: This invention is concerned with compounds of the formula wherein A, R1 to R5 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.

Abstract: The present invention is related to benzazole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzazole derivatives. Said benzazole derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and/or 3. The present invention is furthermore related to novel benzazole derivatives as well as to methods of their preparation. X is O, S or NR0, with R0 being H or an unsubstituted or substituted C1-C6 alkyl; G is an unsubstituted or substituted pyrimidinyl group.

Abstract: The present invention provides a process for producing the pyridine compound [d]: [wherein R3 and R4 are as defined below], which has an excellent herbicidal activity, by making a pyridine compound [a]: [wherein R1 represents a C1–C6 alkoxy group, R3 represents a halogen atom, cyano group or nitro group, and R4 ?????????? ? ???????? ???? ?? ??????? ????] ????? ???? ?? ?-diazoester compound [f]: N2CHCOR1[f] [wherein R1 is defined above] in the presence of an acid.

Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is sulfur or oxygen; J is nitrogen or C—R?; R1, R? is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy or a functional group having one of following general formulae: wherein A1, A2, A3, A4, A5, is independently selected from H, halogen such as F, Cl, Br or I, CF3, alkyl, preferably C1–C4 alkyl, nitro, nitrile, alkoxy, preferably C1–C4 alkoxy, halogenated (such as F, Cl, Br and I) alkyl, preferably halogenated C1–C4 alkyl, halogenated (such as F, Cl, Br and I) alkoxy, preferably halogenated C1–C4 alkoxy, phenyl, and halogenated (such as F, Cl, Br and I phenyl; R2 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nuc

Abstract: The present invention provides a genus of pyrimidine amides that are useful as openers of potassium ion channels. The compounds of the invention are of use in both therapeutic and diagnostic methods.

Abstract: GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein A, Q, R1, R2, R3a, R3b, R4, R5, R6 and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

Abstract: This invention provides compounds defined by Formula I or a pharmaceutically acceptable salt thereof, wherein R1, Q, R2, R3, and R4 are as defined in the specification. The invention also provides related pharmaceutical compositions, methods of use, and combinations.

Abstract: The present invention relates to a compound of formula (I) (wherein R1 and R2 represent an aryl group, a heterocyclic group, an alkyl group, an alkenyl group and the like which are optionally substituted, R3 represents a hydrogen atom or a hydroxyl group, and X1 and X2 represent an oxygen atom or a sulfur atom, or a nitrogen atom which may be substituted), a pharmaceutically acceptable derivative thereof or a salt thereof. The present invention also relates to a pharmaceutical composition comprising a compound described above as an active ingredient for the prevention or treatment of bacterial infections. The present invention includes the use of a compound described above in order to prepare a medicament effective in the prevention or treatment of bacterial infections.

Abstract: The present invention provides a process for producing the pyridine compound [d]: [wherein R3 and R4 are as defined below], which has an excellent herbicidal activity, by making a pyridine compound [a]: [wherein R1 represents a C1–C6 alkoxy group, R3 represents a halogen atom, cyano group or nitro group, and R4 represents a hydrogen atom or halogen atom] react with an ?-diazoester compound [f]: N2CHCOR1[f] [wherein R1 is defined above] in the presence of an acid.

Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.

Abstract: The present invention is a sulfonamide substituted xanthine derivative of formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is lower alkyl, lower alkyl substituted by phenyl, or lower alkyl substituted by halogen substituted phenyl; R2 is lower alkyl or lower alkyl substituted by lower cycloalkyl; and R3 is: Compounds of formula I and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.

Abstract: The present invention is a 1,3,8 substituted xanthine derivative of formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are as defined in the specification. Compounds of formula I and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.

Abstract: Disclosed are processes for the synthesis of novel compounds that are A2B adenosine receptor antagonists, having the structure of Formula I or Formula II: by cyclizing a compound of the formula (3):

Abstract: The present invention relates to novel LXR ligands of Formula I and the pharmaceutically acceptable salts, esters and tautomers thereof, which are useful in the treatment of dyslipidemic conditions, particularly depressed levels of HDL cholesterol.

Abstract: Pyrimidinone compounds of formula (10 are inhibitors of the enzyme Lp-PLA2 and of use in therapy, in particular for treating atherosclerosis.

Abstract: Pyrimidinedione derivatives of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them are useful for the treatment of inflammation and immunological diseases

Abstract: The present invention relates to a novel process for preparing known 1-amino-3-phenyluracil derivatives, to novel 1-amino-6-hydroxy-3-phenyldihydro-2,4(1H,3H)pyrimidinedione derivatives of the formula (II) in which R1 is hydrogen, cyano, nitro or halogen, R2 is cyano, nitro, halogen or optionally substituted alkyl or alkoxy, R3 is hydrogen, hydroxyl, mercapto, amino, hydroxyamino, hydrazino, halogen, or one of the radicals —R6, -Q-R6, —NH—R6, —NH—O—R6, —NH—SO2—R6, —N(SO2—R6)2, —CQ1-R6, —CQ1-Q2-R6, —CQ1-NH—R6, -Q2-CQ1-R6, —NH—CQ1-R6, —N(SO2—R6)(CQ1-R6), -Q2-CQ1-Q2-R6, —NH—CQ1-Q2-R6 or -Q2-CQ1-NH—R6, where Q is O, S, SO or SO2, Q1 and Q2 are each independently oxygen or sulphur and R6 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heterocyclyl or heterocyclylalkyl, R4 is hydrogen, halogen or optionally substituted alkyl, and R5 is fluorine- and/or chlorine-substituted alkyl, as intermediates for the 1-amino-3-phenyluracil derivatives, and to a process f

Abstract: This invention concerns new biocidal compounds of formula (I) wherein R is H or CH3. Of particular interest are two isomers that are named malayamycin A and desmethylmalayamycin A. These isomers, which may be prepared by growing under controlled conditions a previously unknown strain of micro-organism from the species Streptomyces malaysiensis, are characterised by nmr and mass spectroscopic data. They have biocidal activity, including anti-fungal, anti-viral and anti-cancer activity, and are of special interest for use in agriculture, horticulture, animal and human health.

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl uracil compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.

Abstract: The invention relates to novel substituted phenyl uracils of the formula (I) in which R1 represents hydrogen, amino or in each case optionally substituted alkyl, alkenyl or alkynyl, R2 represents cyano, carboxy, carbamoyl, thiocarbamoyl or optionally substituted alkyl or alkoxycarbonyl, R3 represents hydrogen, halogen or optionally substituted alkyl, R4 represents hydrogen, nitro, cyano, alkoxy or halogen, R5 represents cyano, thiocarbamoyl, halogen or optionally substituted alkyl or alkoxy and R6 represents an optionally substituted nitrogen-containing heterocyclic group which is attached to R6 via N, to processes for their preparation, to their use as crop treatment agents, and to intermediates and processes for their preparation.

Abstract: The present invention relates to pyrimidinedione derivatives of following formula (I) which are useful as antiviral agents, especially as agents for treatment of AIDS, pharmaceutically acceptable salts thereof, process for the preparation thereof and pharmaceutical compositions containing the same, wherein R represents cyclopropyl; cyclobutyl; cyclohexyl; unsubstituted or mono-, di- or trisubstituted phenyl with a group selected from hydroxy, C1–C4 alkyl, C1–C4 alkoxy, halogen, trifluoromethyl, cyano and amino; 1- or 2-naphthyl; 9-anthracenyl; 2-anthraquinonyl; unsubstituted or substituted pyridyl with a group selected from C1–C4 alkyl, C1–C4 alkoxy, cyano and halogen; 2-, 3- or 4-quinolinyl; oxiranyl; 1-benzotriazolyl; 2-benzoxazolyl; furanyl substituted with C1–C4 alkoxycarbonyl; C1–C4 alkylcarbonyl; or benzoyl, R1 represents halogen or C1–C4 alkyl, R2 and R3 represent independently hydrogen or C1–C4 alkyl, X represents oxygen atom, and Y represents oxygen atom, sulfur atom or carbonyl.

Abstract: The invention relates to novel aryl-ethene-sulfonamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as endothelin receptor antagonists.

Abstract: Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

Abstract: Bradykinin B1-receptor antagonists of formula are disclosed. The compounds are useful for treating diseases associated with inappropriate bradykinin receptor activity, such as diabetic vasculopathy, inflammation, pain, hyperalgesia, asthma, rhinitis, septic shock, atherosclerosis and multiple sclerosis. Pyrimidines, triazines, and anilines in which Q is imidazolyl or pyrrolyl are particularly preferred.

Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein A, Q, R1, R2, R3a, R3b, R4, R5, R6 and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

Abstract: The invention relates to novel substituted benzoylisoxazoles of the general formula (I), in which n represents the number 0, 1, 2 or 3, A represents a single bond or represents alkanediyl (alkylene), R1 represents hydrogen or represents in each case optionally substituted alkyl, alkenyl or cycloalkyl, R2 represents hydrogen, cyano, carbamoyl, halogen, or represents in each case optionally substituted alkyl, alkylcarbonyl, alkoxy, alkoxycarbonyl or alkylthio, alkylsulphinyl or alkylsulphonyl, R3 represents hydrogen, nitro, cyano, carboxyl, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylamino, dialkylamino or dialkylaminosulphonyl, R4 represents nitro, cyano, carboxyl, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylamino, dialkylamino or dialkylaminosulphonyl, and Z represents an optionally substituted 4-

Abstract: Substituted aryl ether derived compounds represented by general structure (I) are described. X and Y are independent of each other and are represented by hydrogen, halogen, cyano, nitro, (C1-4)alkyl, (C1-4)haloalkyl, or (C1-4)haloalkoxy; Z is oxygen or sulfur, Q is selected form Q1 to Q6; A is oxygen, sulfur, or imino; R1 is hydrogen, (C1-4)alkyl, (C1-4)haloalkyl, or amino and can be independent of each other in a single molecule; R2 and R3 are independent of each other and may be selected from the group consisting of hydrogen, halogen, cyano nitro, (C1-4)alkyl, (C1-4)haloalkyl, (C2-4)alkenyl, (C2-6)haloalkenyl and amino which may be optionally substituted with (C1-4)alkyl or (C1-4)haloalkyl; Ar is substituted or unsubstituted carbocyclic or heterocyclic aromatic ring being at least a five or six membered ring. This ring can be fused with another substituted or unsubstituted five or six membered carbocyclic or heterocyclic ring. When Q is Q5, unsubstituted or substituted phenyl is excluded.

Abstract: The present invention relates to novel pyrimidones of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention more particularly novel pyrimidones of the general formula (I).

Abstract: Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R3, R4, R5, R6, R16 and R17 are as defined in the application, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment disorders including CNS and stress-related disorders.

Abstract: The present invention provides a process for producing the pyridine compound [d]: 1

Abstract: Disclosed are compounds of the formula