Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma, processes for preparing and intermediates thereof.

Abstract: A novel 4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivative or a pharmaceutically acceptable salt thereof, which is useful as an agent for treating or preventing nocturia and/or diabetes insipidus, is provided.

Abstract: The present invention provides for new crystal forms of oxcarbazepine, more particularly oxcarbazepine Forms B, C, D and E. The present invention further provides processes for preparation of these forms. Form B is prepared by evaporating the solvents from a solution of oxcarbazepine in toluene and dichloromethane. Form B is also obtained by immediately cooling the solution of oxcarbazepine and toluene. Cooling the same solution at a slower rate, but still fairly rapidly, results in oxcarbazepine Form C. Cooling the same solution at even a slower rate results in another Form, oxcarbazepine Form D. Oxcarbazepine Form E, a solvate of chloroform, is obtained by precipitating a solution of oxcarbazepine and chloroform. The present invention also provides processes for converting one of the newly discovered crystal forms of oxcarbazepine into another crystal form, including Form A, which is in the prior art.

Abstract: Heterocyclic compounds that bind chemokine receptors and inhibit the binding of their natural ligands are disclosed. The invention compounds are protective against infection by HIV and exert effects characteristic of antagonists to the CXCR4 receptor.

Abstract: Piperidine-2,6-diones heterocyclically substituted in the 3-position corresponding to formula I Also the production and use of such compounds in pharmaceutical formulations and related methods of treatment.

Abstract: The present invention relates to 2-imino-1,3-thiazine derivatives, in specific, 2-imino-1,3-thiazine derivatives having a selective antagonistic activity or agonistic activity to a cannabinoid type 2 receptor and their pharmaceutical use.

Abstract: The present invention provides a compound represented by the formula (I) wherein R1 is a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, an optionally substituted hydroxy group, an optionally substituted thiol group or an optionally substituted amino group, A is an optionally substituted cyclic amino group or —NR2—W—D wherein R2 is a hydrogen atom or an alkyl group, W is a bond or a divalent acyclic hydrocarbon group, and D is an optionally substituted cyclic group, an optionally substituted amino group or an optionally substituted acyl group, B is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, X is an oxygen atom, a sulfur atom or an optionally substituted nitrogen atom, and Y is a bond or a divalent acyclic hydrocarbon group, or a salt thereof, which is useful for the prophylaxis or treatment of diabetic neuropathy and the like.

Abstract: Novel compounds of the formula I in which D, W, X, Y, T and R1 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.

Abstract: Disclosed are novel compounds useful for the control of harmful organisms, harmful organism control agents using the same, and processes for producing the novel compounds. The useful novel compounds according to the present invention include compounds represented by formula (1).

Abstract: The invention relates to new basic amino acid derivatives of general formulae I, II and III, and the preparation and use thereof in treatment of pain. The compounds have histogranin-like antinociceptive, morphine potentiating and COX-2 induction modulating activities.

Abstract: The present invention relates to bicyclic imidazole compounds of general formula wherein R1 to R3 and A are defined as in claims 1 to 8, the tautomers, the enantiomers, the stereoisomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

Abstract: Disclosed are sulfonylquinoxalone derivatives of the general formula: These compounds are useful as bradykinin antagonists.

Abstract: The present invention is directed to compounds useful for treating addictive behavior and sleep disorders represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The compounds used in the method of treatment of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including addictive behavior and sleep disorders.

Abstract: The invention relates to new piperidinyl-alkylamino-pyridazinone derivatives of the general Formula (I) (wherein R is hydrogen or C1-4-alkyl; one of X and Y stands for hydrogen and the other represents a group of the general Formula (II) Hal stands for halogen; and n is 1 or 2) and pharmaceutically acceptable acid addition salts thereof a process for the preparation thereof and pharmaceutical compositions comprising said compounds.

Abstract: This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with new aminium salts of 1,2,3-triazoles which can be used as prodrugs to improve the solubility or pharmaceutical properties of 1,2,3-triazole containing compounds. More particularly, the present disclosure relates to compounds containing N-aminium-1,2,3-triazoles that are useful as antiviral agents and specifically for the treatment of HIV and AIDS.

Abstract: The present invention provides compositions of matter, kits and methods for their use in the treatment of MAP kinase-related conditions and/or HMG-CoA reductase-related conditions. In particular, the invention provides compositions for treating inflammatory and/or cardiovascular conditions in an animal subject by inhibiting p38? MAP kinase and/or HMG-CoA reductase, as well as providing formulations and modes of administering such compositions. The invention further provides methods for the rational design of inhibitors of MAP kinase, HMG-CoA reductase, or both for use in the practice of the present invention.

Abstract: The present invention relates to novel compounds and methods that are useful in treating members of the Flaviviridae family of viruses. Compounds of the present invention will have a structure according to Formulas (I)–(VI) as recited throughout the application.

Abstract: Disclosed are compounds Formula I and pharmaceutically acceptable salts thereof, wherein R1, R2, R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.

Abstract: This invention concerns a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents a 6-membered heterocycle; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyloxyC1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is O or S; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R3 is hydrogen; hydroxy; halo; optionally substituted C1-6alkyl or C2-6alkenyl or C2-6alkynyl; C1-6alkyloxy; C1-6alkylthio; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R21; R21—C1-6alkyl; R21—O—; R21—S—; R21—C(?O)—; R21—S(?O)p—; R7—S(?O)p—; R7—S(?O)p—NH—; R21—S(?O)p—NH—; R7—C(?O)—; —NHC(?O)H; —C(?O)NHNH2; R7—C(?O)—NH—;

Abstract: The present invention relates to medical uses of 39-desmethoxyrapamycin.

Abstract: The present invention relates to novel compounds, their use for inhibiting post prolin/analine-cleaving proteases, such as serine proteases, such as dipeptidyl peptidases, such as dipeptidyl peptidase IV (DPP-IV), and to methods for their production and their therapeutic utility.

Abstract: The present invention a novel use of primaquine derivative N1-(3-ethylidinotetrahydrofuran-2-one)-N4-(6-methoxy-8-quinolinyl)-1,4-pentanediamine in the treatment and controlling the spread of malaria. In particular, the present invention discloses a method of treatment of malaria by the use of primaquine derivative N1-(3-ethylidinotetrahydrofuran-2-one)-N4-(6-methoxy-8-quinolinyl)-1,4-pentanediamine as a gametocytocidal agent.

Abstract: This invention is directed to compounds of formula I: wherein R1–R5 and a-e are as defined in the specification; or pharmaceutically-acceptable salt or solvate or stereoisomer thereof. The invention also directed to pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors using such compounds.

Abstract: This application is directed to compounds of the formula wherein j is 1; k is 0 or 1; m is 1, 2 or 3; n is 1 or 2; W1 and W2 are independently —O— or —S(?O)t—, where t is 0, 1, or 2; Y is ?C(R1a)—, where R1a is a member selected from the group consisting of H; F; Cl; CN; NO2; —(C1–C4)alkyl; —(C2–C4)alkynyl; fluorinated-(C1–C3)alkyl; fluorinated-(C1–C3)alkoxy; —OR16; and —C(?O)NR22aR22b; R22a and R22b are defined as set forth in the specification; —RA and RB are each a member independently selected from the group consisting of H; F; CF3; —(C1–C4)alkyl; —(C3–C7)cycloalkyl; phenyl; and benzyl; wherein said cycloalkyl, phenyl, and benzyl moieties are each independently substituted with 0 to 3 substituents R10, which is defined as set forth in the specification; R16 and R17 are defined as set forth in the specification; —RC and RD have the same meaning as defined above for RA and RB except that one of them must be —H, and they are selected independently of each other and of RA and RB; R1 and R2 are each a memb

Abstract: The invention relates to indole derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The indole derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.

Abstract: A compound represented by the following formula (1): (wherein each of R1 and R2, which may be identical to or different from each other, represents a hydrogen atom, a methyl group, or an ethyl group; each of R3a, R3b, R4a, and R4b, which may be identical to or different from each other, represents a hydrogen atom, a halogen atom, a nitro group, a hydroxyl group, a C1-4 alkyl group, a trifluoromethyl group, a C1-4 alkoxy group, a C1-4 alkylcarbonyloxy group, a di-C1-4 alkylamino group, a C1-4 alkylsulfonyloxy group, a C1-4 alkylsulfonyl group, a C1-4 alkylsulfinyl group, or a C1-4 alkylthio group, or R3a and R3b, or R4a and R4b may be linked together to form an alkylenedioxy group; X represents an oxygen atom, a sulfur atom, or N—R5 (R5 represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkylsulfonyl group, or a C1-4 alkyloxycarbonyl group); Y represents an oxygen atom, S(O)l (l is a number of 0 to 2), a carbonyl group, a carbonylamino group, an aminocarbonyl group, a sulfonylamino group, or an aminosu

Abstract: The present invention comprises novel and known pyrazole derivatives having anti-HIV activity, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds of formula I are inhibitors of the human immunodeficiency virus reverse transcriptase enzyme which is involved in viral replication. Consequently the compounds of this invention may be advantageously used as therapeutic agents for HIV infection.

Abstract: Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.

Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: (I) A is an aryl group; Q1 is a covalent bond or an aryl leader group; J is a sulfonamide linkage selected from: —S(?O)2NR1— and —NR1S(?O)2—; R1 is a sulfonamido substituent; and, Q2 is an acid leader group; with the proviso that if J is —S(?O)2NR1—, then Q1 is an aryl leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.

Abstract: The present invention provides a tetrazoyloxime derivative which is less likely to cause chemical injury to useful plants and is also superior in chemical efficacy to a conventional hetero ring-substituted oxime derivative. A tetrazoyloxime derivative represented by the general formula (1): X represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, a cyano group, a methanesulfonyl group, a nitro group, a trifluoromethyl group, or an aryl group; A represents a 1-alkyltetrazoyl-5-yl group or a 5-alkyltetrazoyl-1-yl group; and Het represents a pyridyl group having a substituent or a thiazoyl group having a substituent, and a plant disease controlling agent containing the same as an active ingredient are disclosed.

Abstract: Substituted aryl aminomethyl thiazole ureas and analogues thereof that act as inhibitors of viral capsid formation, including HIV capsid formation, are provided here. Generally the virus capsid formation inhibitors described herein are compounds of Formula I wherein the variables A, R1, R2, R3, R4, X, Y, Z, A5, A6, A7, R8, R9, R12, and R13 are defined herein. Pharmaceutical compositions comprising such compounds and methods of treating animals infected with a virus having a capsid protein are provided herein. Methods of using such compounds to treat human patients infected with an HIV virus and reducing the mortality of AIDS are also provided herein.

Abstract: The present invention relates to novel oxazolidinone compounds of the general formula (I). where R1, R2, R3, Y1, Y2, Y3, and Z are as defined in the description; their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them.

Abstract: Compounds having the structure of formula I are described wherein R, R?, R1, R2, and R3 are as defined in the specification. The compounds can inhibit hepatitis C virus (HCV) replication, and in particular the function of the HCV NS5A protein.

Abstract: Compounds of formula I: inhibit gamma-secretase and hence find use in treatment of Alzheimer's disease.

Abstract: Compounds of the formula provide pharmacological agents which are potent agonists of Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases, ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X.

Abstract: The present invention provides a process for the preparation of imidazoles by reacting a cyano compound with a silylalkylisocyanide compound. Such imidazoles are useful pharmacologically-active compounds and/or intermediates for the preparation of pharmacologically-active compounds.

Abstract: A compound of the formula (I): wherein R1 is hydrogen or lower alkyl; R2 is lower alkyl, etc.; R3 is lower alkoxy, etc.; R4 is hydroxy, etc.; X is O, S, etc.; Y is CH or N; Z is lower alkylene or lower alkenylene; and m is 0 or 1; or salts thereof, which are useful as a medicament.

Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein B, R1, n, R3, Q and R4 are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.

Abstract: A process for the synthesis of perindopril of formula (I): and its pharmaceutically acceptable salts.

Abstract: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment or prevention of disorders and diseases mediated by agonists and antagonists of the progesterone receptor. The clinical uses of these compounds are related to contraception, the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, or minication of side effects of cyclid menstrual bleeding. Additional uses of the invention include stimulation of food intake.

Abstract: A compound comprising or a pharmaceutically acceptable salt or a prodrug thereof, having the groups described in detail herein is disclosed. Also disclosed herein are compounds comprising or derivatives thereof, or pharmaceutically acceptable salts, tetrazoles, or prodrugs of compounds of the structure or derivatives thereof, said derivatives being described in detail herein. Also disclosed herein are methods of treating diseases or conditions, including glaucoma and elevated intraocular pressure. Compositions and methods of manufacturing medicaments related thereto are also disclosed.

Abstract: The present invention provides novel compounds and methods for using them to treat diseases with aminothiophene inhibitors of IKK-? phosphorylation of I?B. In yso doing these aminothiophene inhibitors block pathological activation of transcription factor NF-?B in which diseases excessive activation of NF-?B is implicated.

Abstract: Texanes having a heterosubstituted acetate substituent at C(7), a hydroxy substitutent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.

Abstract: Novel tricyclic cannabinoid compounds are presented. Some of these compounds exhibit fluorescence properties. The fluorescent cannabinoid compounds are typically endogenously fluorescent. Some of these compounds, when administered in a therapeutically effective amount to an individual or animal, result in a sufficiently high level of that compound in the individual or animal to cause a physiological response. The physiological response useful to treat a number of physiological conditions.

Abstract: A method for preventing or for treating anxiety in a patient in need thereof comprising administering wogonin to the patient in an effective dose that does not cause sedative or myorelaxant side effects. Methods for extracting wogonin from the roots of Scutelleria baicalensis Georgi are also described.

Abstract: The described invention relates to the new compound “sucrose-octasulphate salified with silver” usefully applicable in the prevention and cure of infections by micro-organisms of bacterial, fungal, viral and/or yeast origins and in the promotion of tissue repair. The silver salts of sucrose octasulphate, subject of the invention have in fact been shown to possess antimicrobial activities even higher than that of known silver compounds. These properties therefore make them particularly suitable for use in different pathological or paraphysiological conditions of the skin, of the epithelia and of the mucosa both intact and lesioned.

Abstract: Human papillomavirus (HPV) protein expression is downregulated in patients infected with HPV by administration of PPAR? ligand, selective inhibitor of cyclooxygenase-2 (COX-2), diaryl heterocycle, inhibitor of HPV protein from a natural source and/or certain non-steroidal anti-inflammatory drugs.

Abstract: It has been discovered that certain selected ethers of probucol, and their pharmaceutically acceptable salts or prodrugs, are useful for increasing circulating HDL cholesterol. These compounds may also improve HDL functionality by (a) increasing clearance of cholesteryl esters, (b) increasing HDL-particle affinity for hepatic cell surface receptors or (c) increasing the half life of apoAI-HDL.

Abstract: The invention concerns compounds of formula (1): R-A-R? wherein: A is as defined in the description; R represent a group (V), (VI), (VII), or (VIII), where E, Q, R1, R2, R3, v and R4 are as defined in the description; R? represents a —(CH2)t—R5 group wherein t and R5 are as defined in the description, and medicaments containing the same

Abstract: Novel mono- and dihydroxy phenylethylamine derivatives useful in treating melanoma are provided having the formulae (Ia, Ib or Ic). In the above formulae, Ra is hydrogen or —COORb, Rb is hydrogen or C1-6 alkyl; Re and Re independently represent hydrogen and hydroxy, Rf is hydrogen, C1–4? alkyl or halogen, X is —CHOH—, —CH2-oxygen or sulphur, m is zero or 1, W is oxygen or sulphur, and —ODrug, —NHDrug and —N(Drug)2 each represent a residue of a therapeutically active agent. The above compounds are prodrugs which are inactive until metabolised by enzymes expressed by host melanoma cells.