Abstract: Compounds of the formula I, 1

Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension.

Abstract: The present invention discloses compounds, which are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided.

Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension.

Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension.

Abstract: Disclosed are novel compounds represented by Structural Formula II, IX or XXVIII: R1, R2, and R22 are independently an aliphatic group, a substituted aliphatic group, an aromatic group or a substituted aromatic group. R2 is —NR4R5 or —N+≡C−. Alternatively, R1, and R2, taken together with the methine group to which they are bonded, are a moiety represented by the following structural formula: R3 is —NH2, —OH, —OC(O)H or —OR9. R5, R6 and R7 are independently —H or an amine protecting group. R8 is —H, —OH or —OR8. R9 is an alcohol protecting group. Also disclosed are methods of preparing these compounds.

Abstract: The invention provides compounds that are useful for the treatment of bacterial infections in mammals.

Abstract: The invention provides compounds of Formula (I): 1

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

Abstract: Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.

Abstract: The present invention relates to compounds of formula (I): 1

Abstract: Compounds of peptide mimetic nature having the general formula I wherein a and b are independently 1 or 2, R1 and R2 are independently H or C1-6alkyl, G and J are independently, inter alia, aromats, and D and E are independently several different groups are growth hormone secretagogous with improved bioavailability.

Abstract: The present invention provides amino ceramide-like compounds which inhibit glucosyl ceramide (GlyCer) formation by inhibiting the enzyme GlyCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.

Abstract: The invention is directed to physiologically active compounds of formula (I): wherein one of A1, A2 and A3 represents NR2 and the others represent C(R3)(R4); R1 represents R5Z1—Het— or R6N(R7)—C(═O)—NH—Ar2—; Ar1 represents aryldiyl or heteroaryldiyl; L1 represents a —R12-R13— linkage (where R12 is a direct bond or an alkylene chain, an alkenylene chain or an alkynylene chain and R13 is a direct bond, cycloalkylene, heterocycloalkylene, aryldiyl, heteroaryldiyl, —C(═Z3)—NR11—, —NR11—C(═Z3)—, —Z3—, —C(═O)—, —C(═NOR11)—, —NR11—, —NR11—C(═Z3)—NR11—, —SO2—NR11—, —NR —SO2—, —O—C(═O)—, —C(═O)—O—, —NR11—C(═O)—O— or —O—C(═O)—NR11—); and their prodrugs, and pharmaceutically accepta

Abstract: The present invention provides certain alpha-amino acids and derivatives thereof, such as, but not limited to, esters, amides and salts. The present invention also provides a novel method for the synthesis of alpha-amino acids and derivatives thereof.

Abstract: Non-peptide acetamide derivatives of Formula I are specific NK1 antagonists, 1

Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below.

Abstract: The present application describes modulators of MCP-1 of formula (I): 1

Abstract: N-Substituted-N′-substituted urea derivatives represented by the following formula, analogs thereof or pharmaceutically acceptable salts thereof are herein provided. These compounds show a TNF-&agr; production inhibitory activity.

Abstract: This invention encompasses the novel compounds of Formula I, which are useful in the treatment of caspase-3 mediated diseases.

Abstract: The present application describes modulators of CCR3 of formula (I): 1

Abstract: A compound represented by the following formula: 1

Abstract: The present application describes modulators of CCR3 of formula (I): 1

Abstract: N-heterocyclic moiety containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: Compounds of Formula I are disclosed which are useful as fungicides wherein R1 is hydrogen; halogen; C1-C2 alkoxy; C1-C2 haloalkoxy; cyano; or C1-C2 alkyl optionally substituted with halogen, C1-C2 alkoxy or cyano; R2 is hydrogen; halogen; or C1-C4 alkyl optionally substituted with halogen, C1-C2 alkoxy or cyano; R3 is hydrogen; halogen; C1-C4 alkoxy; C1-C4 haloalkoxy; or C1-C4 alkyl optionally substituted with halogen, C1-C2 alkoxy or cyano; or R2 and R3 can be taken together as —CH2CH2—; R4 is C1-C2 alkyl; R5 is R6, CH(R8)OR6, CH(R8)CH(R7)R6 or C(R8)═C(R7)R6; and R6, R7 and R8 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula I and a method for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound of Formula I.

Abstract: Substituted benzene acetamide compounds and pharmaceutically acceptable salts thereof are useful as glucokinase activators.

Abstract: This invention relates to certain 2,4-substituted pyrrolidine derivatives that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.

Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH-mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.

Abstract: Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin di

Abstract: The present application relates to carboxylic acid amides of general formula wherein A, B and R1 to R3 are defined as in claim 1, processes for preparing them, pharmaceutical compositions containing these compounds and the use thereof and their preparation.

Abstract: Compounds represented by structural formula I 1

Abstract: The invention concerns amide derivatives of Formula (I) wherein: R1 and R2 include hydroxy, C1-6alkoxy, mercapto, C1-6akylthio, amino and heterocyclyl; m and p are independently 0-3; R3 is halo, cyano or C1-6alkoxy; q is 0-4; and R4 is aryl or cycloalkyl wherein R4 is optionally substituted with up to 3 substituents having any value defined for each R1 group; or a pharmaceutically-acceptable salt or in-vivo-cleavable ester thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.

Abstract: Described are compounds of formula (I), wherein W is O or S; X is NR8; Y is CR9R10—(CH2)n wherein R9 and R10 are independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is S02; R1 is aryl; R2 is a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms with the exception that R2 cannot represent 2-phthalimidyl, and in case of Y=SO2 cannot represent 2,1,3-benzothiadiazol-4-yl; any of R3, R4, R5 and R6, independently of the other, is H or a substituent other than hydrogen; and R7 and R8, independently of each other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g.

Abstract: Benzamides of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: R1—C1-C6-alkyl, branched or unbranched, where one of the C atoms in this chain may be substituted by a phenyl ring, cyclohexyl ring, indolyl ring and an SCH3 group, and the phenyl ring in turn is substituted by by [sic] a maximum of two R4 radicals, where R4 [lacuna] hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, NHCO—C1-C4-alkyl, and R2 can be NR5CO—R6 and NHR5SO2—R6, and R3 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl, CN, COOH, CONH2, COO—C1-C4-alkyl, SO2—C1-C4-alkyl, —SO2Ph, SO2NH—C1-C4-alkyl, iodine, SO2NH2 and NH2, and A can be arom

Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Abstract: The present invention provides novel indane-like compounds which can be useful for treating psychosis and other conditions associated with the modulation of a muscarinic receptor. The invention provides formulations and methods for using the novel compounds.

Abstract: A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

Abstract: Compounds of the formula: 1

Abstract: The compound is a neuropeptide Y antagonist and is effective in treating feeding disorders, cardiovascular diseases and other physiological disorders.

Abstract: Substituted cinnamic acid guanidides, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them. Compounds of the formula I which may be obtained by reaction of a compound II with guanidine.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof, where G is a methylene or ethylene linkage; R1 is hydrogen, C1-6alkylO—; R2 is hydrogen, halogen, CN, N3, trifluoromethyldiazirinyl, CF3, CF3O—, CF3S—, CF3CO—, C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl-, C1-6alkylO—, C1-6alkylCO—, C3-6cycloalkylCO—, C3-6cycloalkyl-C1-4-alkylCO—, phenyl, phenoxy, benzyloxy, benzoyl and substituted benzoyl, phenyl-C1-4alkyl-, C1-6alkylSO2—, (C1-4alkyl)2NSO2— or (C1-4alkyl)NHSO2—; R3 is hydrogen, halogen, CN, N3, trifluoromethyldiazirinyl, C1-6alkylO—, C1-6alkylS—, C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl-, C1-6alkenyl, C1-6alkynyl, CF3CO—, C1-6alkylCO—, C3-6cycloalkylCO—, C3-6cycloalkyl-C1-4alkylCO—, phenyl, phenoxy, benzyloxy, benzoyl, phenyl-C1-4alkyl-, or —NR5R6 where R5 is hydrogen or C1-4alkyl; and R6 is hydrogen, C1-4alkyl, —CHO, —CO2C1-4alkyl or —COC1-4alk

Abstract: The present invention provides a compound that includes an active therapeutic agent attached to a blocking moiety that is sensitive to the catalytic action of molecules having retro-aldol and retro-Michael catalytic activity, methods for making such compounds and methods of converting such compounds to active therapeutic agents using molecules having aldolase activity.

Abstract: Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin di

Abstract: The invention relates to a new process for concentrating epothilones in culture media, a new process for the production of epothilones, a new process for separating epothilones A and B and a new strain obtained by mutagenesis for the production of epothilones, as well as aspects related thereto. New crystal forms of epothilone B are also described.

Abstract: Trisubstituted N-protected guanidines and methods for use as guanidinylating reagents to yield N-protected guanidine derivatives.

Abstract: A compound of the formula (I): or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.

Abstract: The invention pertains to novel peptide analogs suitable for inhibiting protein:prenyl transferases. As such they are therapeutically useful in e.g. inhibiting oncogenesis and other unwanted cell proliferation, and in supressing aberrant high signal transduction. The analogs comply with the following formula: in which: R1 is hydrogen or a thiol-protecting group; R2 and R3 are independently hydrogen or C1-C4 alkyl; R4 is hydrogen, C1-C4 alkyl, C1-C4 acyl or peptidyl; R5 is hydrogen or C1-C4 alkyl; R6 is hydrogen or optionally substituted C1-C6 alkyl; A is a direct bond or an optionally substituted C1-C4 alkylene chain; Y represents an oxo group or two hydrogen atoms; Z is oxygen, sulphur, imino or C1-C5 alkyl-, aryl- or acylimino; M is 0, 1 or 2; N is 0 or 1.

Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.

Abstract: An aromatic sulfonyl alpha-hydroxy hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.