Abstract: A sulfamato hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a process for preparing the same, intermediate compounds useful in those syntheses, and a treatment process that comprises administering a contemplated sulfamato hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

Abstract: This invention relates to N-aroyl cyclic amine derivatives of formula (I): wherein: Y represents a bond, oxygen, or a group (CH2)n, wherein n represents 1, 2 or 3 m represents 1, 2 or 3; p represents 0 or 1; X is O,SC═O, SO2, or —CH═CH; Ar1 is aryl, or a mono or bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S; any of which may be optionally substituted; Ar2 represents phenyl or a 5- or 5-membered heterocyclyl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heterocyclyl group is substituted by R1 and further optional substituents; or Ar2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 3 heteroatoms selected from N, O and S; R1 represents hydrogen, optionally substituted (C1-4)alkoxy, halo, cyano, optionally substituted (C1-16)alkyl, optionally substituted 5- or 6-membered heterocyclic ring containing up to 4 heteroatoms selected from N, O and S; or a pharmaceutical acc

Abstract: Compounds of formula (I) 1

Abstract: The present invention relates to a compound of the formula (I) or salt thereof in which R1 is identical or different at each occurrence and is H, halogen, CN, nitro, SF5, (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, (C1-C8)alkoxy, [(C1-C8)alkyl]-carbonyl or (C1-C8)alkylsulfonyl, each of the radicals being unsubstituted or substituted,  or is S(O)p—R7, where p=0, 1 or 2 and R7 is (C1-C8)alkyl, (C1-C8)haloalkyl or NR8R9, where  R8 and R9 independently of one another are identical or different and are H, (C1-C8)alkyl, (C2-C8)alkenyl, (C7-C10)arylalkyl, (C7-C10)alkylaryl or (C6-C10)aryl, each of the last-mentioned five radicals being unsubstituted or substituted,  or is a group of the formula where R10 is (C1-C8)alkyl which is unsubstituted or substituted, and W=O or S, A is optionally substituted aryl or an optionally substituted heterocyclic radical, X is O or S, R2,R3,R4, and R5 are identical or different and are H, hal

Abstract: This invention relates to N-aroyl cyclic amine derivatives of formula (1), wherein X represents a bond, oxygen, NR3 or a group (CH2), wherein n represents 1, 2 or 3; Y represents CH2, CO, CH(OH), or CH2CH(OH); Het is an optionally substituted bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S; Ar2 represents an optionally substituted phenyl or a 5- or 6-membered heterocyclyl group containing up to 3 heteroatoms selected from N, O and S and their use as pharmaceuticals, specifically as orexin receptor antagonists.

Abstract: The present invention relates to piperazine and piperidine derivatives, which are especially useful for treating or preventing neuronal damage, particularly damage associated with neurological diseases. These compounds are also useful for stimulating nerve growth. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage or for stimulating nerve growth.

Abstract: Novel fused heteroaromatic compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-&bgr; signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer and fibrotic diseases.

Abstract: A compound of the formula: [wherein R1 is a hydrocarbon group which may be substituted; R2 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; R3 is halogen atoms, a carbamoyl group which may be substituted, a sulfamoyl group which may be substituted, an acyl group derived from sulfonic acid, a C1-4 alkyl group which may be substituted, a C1-4 alkoxy group which may be substituted, an amino group which may be substituted, a nitro group or a cyano group; R4 is hydrogen atoms or a hydroxy group; n is 0 or 1; and p is 0 or 1 to 4]; or a salt thereof, has potent CCR5 antagonistic activity and can be advantageously used as a medicament for inhibition of HIV infection to human peripheral blood mononuclear cells, especially for the treatment or prevention of AIDS.

Abstract: The invention relates to the use of compounds of formula (I) as medicaments, to the novel compounds of formula (I) themselves, and to a method for the production thereof.

Abstract: The present invention relates to the potentiation of glutamate receptor function using certain sulphonamide derivatives. It also relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.

Abstract: Disclosed are novel processes and novel intermediate compounds for preparing aryl- and heteroaryl-substituted urea compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.

Abstract: Compounds of general formula (I), in which Het represents a five or six membered saturated, partially unsaturated or aromatic ring containing between one and six heteroatoms of the group N, O, S, in which the heterocycle is substituted in an adjacent manner with -P-Qi-T-Q2, -GZ and Y, such that the substituant -GZ is adjacent to both, the other substituants being as defined in the description, process for preparing this compound, fungicidal composition comprising this compound, method for treating plants by applying this compound or composition.

Abstract: Substituted 2-pyridine cyclohexane-1,4-diamine compounds, a method for their production, pharmaceutical compositions containing them, and the use of such substituted 2-pyridine cyclohexane-1,4-diamine compounds for treating pain and various other medical conditions.

Abstract: Compound of general formula (I), in which: Y and G together with carbon atoms 3 and 4, form a 5 or 6 member ring chosen from the following structures (A) to (F), the other substituents being as defined in the description. Process for preparing this compound. Fungicidal composition comprising this compound. Method for treating plants by applying this compound or composition.

Abstract: This invention provides compounds of Formula I, their N-oxides and agriculturally suitable salts wherein A and B are independently O or S; J is an optionally substituted 5- or 6-memebered nonaromatic heterocyclic ring; K is taken together with the two contiguous linking carbon atoms to form a phenyl ring or a 5- or 6-membered heteroaromatic ring, each ring optionally substituted; and R1, R2, and R3 are as defined in the disclosure. Also disclosed are methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula I, an N-oxide thereof or a suitable salt of the compound (e.g., as a composition described herein).

Abstract: Compounds of Formula I have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4 and are useful for treating disease whose symptoms and or damage are related to the binding of VCAM-1 to cells expressing VLA-4.

Abstract: A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof.

Abstract: Compounds of formula I: 1

Abstract: Compounds of formula (I) 1

Abstract: Novel isothiazole and isoxazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-&bgr; signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer, and fibrotic diseases.

Abstract: Novel pyrazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-&bgr; signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer, and fibrotic diseases.

Abstract: The invention relates to compounds of formula (I), a method for the production thereof and the use of the same as pharmaceuticals.

Abstract: The present invention is directed to selective LXR modulators, small molecule compounds corresponding to Formula I and is further directed to a process of treating a condition in a mammal that is modulated by LXR using a therapeutically effective dose of a compound of Formula I.

Abstract: Compounds of the invention are amine oxide prodrugs showing activity on the NK1 receptor.

Abstract: Novel imidazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-&bgr; signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer and fibrotic diseases.

Abstract: Disclosed are novel aromatic compounds of the formula(I) described herein, wherein G, E, W, Ar, X, Y and Z are disclosed herein. The compounds are useful for treating cytokine mediated diseases or conditions such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.

Abstract: The present invention provides certain amide, carbamate and urea derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.

Abstract: Benzanilides are provided which are voltage-dependent potassium channel openers. Methods of using the benzanilides of the invention are also provided.

Abstract: Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially ER-&bgr;. Methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natureal hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.

Abstract: Provided are MC4-R binding compounds of the formula XVII: 1

Abstract: An amide of the formula I 1

Abstract: The invention provides compounds of formula VI 1

Abstract: The present invention is related to sulfonamide derivatives having a lipophilic moiety and which are substantially soluble. Said compounds are notably for use as pharmaceutically active compounds. The present invention also related to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation.

Abstract: Invented are non-peptide TPO mimetics. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative.

Abstract: Disclosed are compounds of formula (I): 1

Abstract: Tri-heterocyclic compound of formula (I) 1

Abstract: The present invention relates to compounds of the formula I, 1

Abstract: The present invention relates to a class of compounds represented by the Formula I.

Abstract: The present invention provides compounds of the formula: wherein R1-R8, X, Y, Z, n and m are defined in the application. The compounds of the invention have affinity for the 5-HT1A receptor.

Abstract: The invention relates to new pyridyl alkane acid amides according to general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppression.

Abstract: What is described are amides of the formula (I) and salts thereof, 1

Abstract: Pharmaceutical agents for inhibiting the production of 20-HETE which participates in constriction or dilation of microvessels in major organs such as the kidneys and the cerebral blood vessels, or participates in causing cell proliferation are provided.

Abstract: 1,3-Oxazoline and 1,3-thiazoline derivatives, their preparation, and their use as pesticides 1,3-Oxazoline and 1,3-thiazoline derivatives of the formula (I) where the symbols have the following meanings: A is phenyl, pyridyl, pyrimidinyl, pyrazinyl, pyrazolyl or thienyl, E is a single bond, (C1-C4)alkylene, —O—CH2— or —CH2—O—; G is a radical selected from the group consisting of Z is oxygen or sulfur. Compounds of the formula (I) have, in particular, a very good acaricidal and insecticidal action with regard to the spectrum of action and the potency.

Abstract: The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R17, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.

Abstract: The present invention provides novel compounds of Formula (I), its prodrug forms, or pharmaceutically acceptable salts thereof. The compounds of this invention are inhibitors of serine proteases, Urokinase (uPA), Factor Xa (FXa), and/or Factor VIIa (FVIIa), and have utility as anti cancer agents and/or as anticoagulants for the treatment or prevention of thromboembolic disorders in mammals. The present invention also provides a process for the selective acylation of an amino group.

Abstract: The present invention relates to novel antidiabetic, hypolipidemic, antiobesity and hypocholesterolemic compounds of formula (I), 1

Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are and pharmaceutical compositions containing, intermediate compounds and processes of making such compounds.

Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes.

Abstract: The present invention relates compounds of the formula (I): wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of: (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), (l) and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R?17, R18, R19, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.

Abstract: The present invention concerns pyridine derivatives having the formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein L is hydrogen; C1-6alkyl; C1-6alkyl carbonyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl; C3-6alkenyl; substituted C3-6alkenyl; piperidyl; substituted piperidyl; C1-6alkylsulfonyl or arylsulfonyl; —A—B— is —CR8═CR5— or—CHR4—CHR5—; D is O or NR6; R1 is a hydrogen or C1-4alkyl; R2 is hydrogen; halo; C1-6alkyl; trifluoromethyl; C3-6cycloalkyl; carboxyl; C1-4alkyl oxycarbonyl; C3-6cycloalkylaminocarbonyl; aryl; Het1; or substituted C1-6alkyl; or R2 is —O—R9 or —NH—R10; R3 is hydrogen, halo, hydroxy, C1-6alkyl or C1-6alkyloxy; or R2 and R1, or R2 and R3 taken together may form a bivalent radical; Q is disubstituted pyridine; R7 and R8 each independently are hydrogen; C1-6alkyl; difluoromethyl; trifluoromethyl; C3-6cyclo alkyl; a