Abstract: The present invention relates to novel achiral seco-analogues of DNA minor groove and sequence-selective alkylating agents (+)-CC1065 and the duocarmycins, depicted as general class I, II, III, IV and V: wherein X is a good leaving group, such as a chloride, a bromide, an iodide, a mesylate, a tosylate, an acetate, a quaternary ammonium moiety, a mercaptan, an alkylsulfoxyl, or an alkylsulfonyl group, preferably either a chloride, a bromide, or an iodide group. R1 is a suitable minor groove binding agent to enhance the interactions of the achiral seco-cyclopropaneindole (Cl) or an achiral seco-duocarmycin with specific sequences of DNA.

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 is directed to a series of substituted pyridine compounds, a method for selectively controlling neurotransmitter release in mammals using these compounds, and pharmaceutical compositions containing these compounds. Preferred compounds are 3′-(5′- and/or 6′-substituted) pyridyl ethers.

Abstract: Novel calcilytic compounds and methods of using them are provided.

Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: The invention discloses a novel process for the preparation of enantiomerically enriched mixtures of compounds of structural formula I which are useful intermediates in the synthesis of &agr;v&bgr;3 integrin receptor antagonists

Abstract: Disclosed are (i) compounds of a steroid, a &bgr;-agonist, an anticholinergic, a mast cell stabilizer and a phosphodiesterase (PDE) inhibitor directly or indirectly linked to a NO or NO2 group or a group which stimulates endogenous production of NO or EDRF in vivo; (ii) compositions of steroids, &bgr;-agonists, anticholinergics, mast cell stabilizers and PDE inhibitors, which can optionally be substituted with at least one NO or NO2 moiety or a group which stimulates endogenous production of NO or EDRF in vivo, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO•) or that stimulates endogenous production of NO or EDRF in vivo; and (iii) uses for them in preventing and/or treating respiratory disorders.

Abstract: In accordance with the present invention, a novel class of substituted pyridine compounds (optionally containing ether, ester, amide, ketone or thioether substitutions) that promote the release of ligands involved in neurotransmission have been discovered. In a particular aspect compounds of the present invention are capable of modulating acetylcholine receptors. The compounds of the present invention are capable of modulating acetylcholine receptors. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors.

Abstract: Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof aryloxyalkylamines and arylthioalkylamines, including pyridyloxyl-alkylamines, phenoxyalkylamines, pyridylthiolalkylamines and phenylthio-alkylamines. Exemplary compounds include (2-(5-bromo(3-pyridylthio))-ethyl)methylamine, (2-(5-bromo(3-pyridylthio))isopropyl)methylamine, (2-(5-bromo(3-pyridylthio))propyl)methylamine, (3-(5-bromo(3-pyridylthio))-propyl)methylamine, 3-((3S)-3-pyrrolidinyloxy)pyridine, 3-(4-piperidinyloxy)pyridine, 3-(1-methyl-4-piperidinyloxy)pyridine, (3-benzo[3,4-d]1,3-dioxolan-5-yloxypropyl)methylamine, and methyl(3-tricyclo[7.3.1.0<5,13>]tridec-2-yloxypropyl)amine.

Abstract: The invention is directed primarily to compounds of Formula I: wherein: R1 is a polymeric residue; L1 is a bifunctional linking group; Y1 and Y2 are independently O, S or NR7; R2-7 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy; D is a moiety that is a leaving group or a residue of a compound to be delivered into a cell; Z is selected from the group consisting of: a moiety that is actively transported into a target cell, a hydrophobic moiety, and combinations thereof; Ar is a moiety which when included in Formula (I) forms a multi-substituted aromatic hydrocarbon or a multi-substituted heterocyclic group; and (y) is a positive integer greater than or equal to 1. Methods of making and using the same are also disclosed.

Abstract: The present invention provides a short, convergent total synthesis of camptothecin and related compounds which consists of a novel 4+1 radical annulation. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.

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: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

Abstract: Patients susceptible to or suffering from central nervous system disorders are treated by administering effective amounts of aryl substituted aliphatic amine compounds, aryl substituted olefinic amine compounds or aryl substituted acetylenic amine compounds. A representative compound is (E)-N-methyl-5-(3-pyridinyl)-4-penten-2-amine.

Abstract: A light emitting device material comprising a compound represented by the following formula (I): 1

Abstract: The present invention relates to novel oxime O-ether compounds represented by a general formula [I]; wherein R1 represents C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkoxy, etc., m represents an integer of 1 to 4, R2 represents hydrogen atom, C1-6 alkyl, etc., R3 and R4 each independently represents hydrogen atom or C1-6 alkyl, etc., R5 represents hydrogen atom, C1-6 alkyl, etc., R6 represents C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, Halogen atom, etc. and n represents an integer of 1 to 4, and a fungicide for agricultural and horticultural use comprising the compound as the active ingredient.

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.

Abstract: The present invention relates to a novel blocked phenylenediamine developer useful, in reactive association, for enabling, on development, a non-magenta color, for example a cyan color, from a dye-forming coupler. In one embodiment, the developer has the property that the dye color formed with the coupler is distinctly different from the color formed by the same coupler with an oxidized form of the conventional developer 4-(N-ethyl-N-2-hydroxyethyl)-2-methylphenylenediamine. The invention is also directed to a light-sensitive silver-halide color photographic element comprising the blocked developing agent according to the present invention.

Abstract: Hydroxamic and carboxylic acid derivatives having MMP and TNF inhibitory activity.

Abstract: Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: wherein X is O or NR9 and Het, R1, R7, R8, R12-R15, Ra, Rb, Rc, Z, and n are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier.

Abstract: The present invention provides a compound of the formula (I):   wherein A ring, B ring and C ring are each independently optionally substituted aromatic carbocycle or optionally substituted 5- or 6-membered heterocycle which may fuse with benzene ring, W1, W2 and/or W3 represents a bond when A ring, B ring and/or C ring is optionally substituted 5-membered heterocycle, X is —O—, —NR1— wherein R1 is hydrogen, lower alkyl etc. or the like, Y is hydrogen, lower alkyl, lower alkenyl or the like, one of V1 and V2 is a bond, and the other is a bond, —O— or the like, and a pharmaceutical composition comprising the same.

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.

Abstract: A compound of the formula (I) wherein X1 ? is bond or —O(CH2)m— (in which m is an integral number of 1, 2 or 3); X2 is bond, —(CH2)n—, etc. (in which n is an integral number of 1, 2 or 3); R1 is hydrogen or amino protective group; R2 is hydroxy(lower)alkyl or (lower)alkoxy(lower)alkyl; A is phenyl, pyridyl, indolyl or carbazolyl, each of which may be substituted with one or two substituent(s) selected from the group consisting of halogen, hydroxy, lower alkyl, etc.; and B is phenyl or pyridyl, each of which may be substituted with one or two substituent(s) selected from the group consisting of halogen, hydroxy, nitro, etc.; and a pharmaceutically acceptable salt thereof which is useful as a medicament.

Abstract: The invention provides pyridoxal and pyridoxine analogues, pharmaceutical compositions containing pyridoxine and pyridoxal analogues, and methods of administering pharmaceutical compositions containing a therapeutically effective amount of at least one of these analogues. In accordance with the present invention, the pyridoxal and pyridoxine analogues can be used in the treatment of undesired platelet aggregation, and in the treatment of symptoms thereof.

Abstract: A 1-aryl-1,8-naphthylidin-4-one derivative having the formula (I): wherein R1 indicates a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaryl group, R2, R3, and R4 independently indicate a hydrogen atom, a substituted or unsubstituted lower alkyl group, or a halogen atom, X indicates a group NR5R6 or a group OR7, wherein R5 and R6 independently indicate a hydrogen a atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted cycloalkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted heteroaryl group, and R7 indicates a hydrogen atom, a substituted or unsubstituted lower alkyl group, or a substituted or unsubstituted cycloalkyl group or a salt or solvate thereof and a type IV phosphodiesterase inhibitor containing the same as an effective component.

Abstract: A method of making a compound of Formula VI: wherein Tr is a triphenyl group; R1, R2 and R3 are each independently selected from the group consisting of H, C1-C4 alkyl, C1-C4 alkoxy, aryl, heteroaryl, and arylalkyl; R4 is C2-C6 alkyl, and R5 and R6 are each independently H or C1-C4 alkyl, involves the step of reacting a compound of Formula V: with Tr-OH to produce a compound of Formula VI. The compounds of Formula VI are useful as intermediates in the manufacture of antibiotic agents. Methods of making compounds of Formula V, and intermediates made or used in the foregoing methods, are also described.

Abstract: Patients susceptible to or suffering from central nervous system disorders (e.g., Alzheimer's disease, Parkinson's disease, Tourette's syndrome, attention deficit disorder or schizophrenia) are treated by administering an effective amount of an aryl substituted olefinic amine compound. Exemplary compounds include (E)-N-methyl-4-[3-(5-benzyloxypyridin)yl]-3-buten-1-amine, (E)-N-methyl-4-[3-(5-phenoxypyridin)yl]-3-buten-1-amine, (E)-N-methyl-4-[3-(5-isopropoxypyridin)yl]-3-buten-1-amine, (E)-N-methyl-4-[3-(5-methoxymethylpyridin)yl]-3-buten-1-amine, and (E)-N-methyl-4-[3-(5-phenylpyridin)yl]-3-buten-1-amine.

Abstract: The invention discloses a novel process for the preparation of enantiomerically enriched mixtures of compounds of structural formula I which are useful intermediates in the synthesis of &agr;v&bgr;3 integrin receptor antagonists.

Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract: The present invention features calcilytic compounds. “Calcilytic compounds” refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.

Abstract: Disclosed are pyroglutamic acid derivatives and related compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: This invention relates to a series of substituted aromatic ethers of the formula I 1

Abstract: An aryloxyaniline derivative represented by the formula: wherein Ar1 and Ar2 are the same or different, and are each a substituted or unsubstituted phenyl group, a substituted or unsubstituted pyridyl group or a naphthyl group, provided that Ar1 and Ar2 are not both phenyl or both naphthyl and are not phenyl and naphthyl, R1 is a hydrogen atom, a substituted or unsubstituted alkyl group having 1 to 10 carbon atoms, an alkoxy group having 1 to 10 carbon atoms, a substituted or unsubstituted phenyl group or a group of the formula: —NR2(R3) (wherein R2 and R3 are the same or different, and are each a hydrogen atom or an alkyl group having 1 to 10 carbon atoms, X1 is a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, a phenoxy group, a halogen atom, a trifluoromethyl group, a carbamoyl group or an aminosulfonyl group, Y1 is a branched or unbranched alkylene group having 1 to 6 carbon atoms or a single bond; and pharmaceutically acceptabl

Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted cycloalkyl aminoalcohols.

Abstract: The present invention relates to pyridone derivatives and herbicidal compositions containing the pyridone derivatives as active ingredients.

Abstract: Novel biphenyl sulfonamide compounds which are combined angiotensin and endothelin receptor antagonists are claimed along with methods of using such compounds in the treatment of conditions such as hypertension and other diseases, as well as pharmaceutical compositions containing such compounds.

Abstract: The present invention is concerned with 3-(amino- or aminoalkyl)pyridinone derivatives which inhibit the reverse transcriptase of the Human Immunodeficiency Virus (HIV). It relates moreover to the use of such compounds for treating HIV-related diseases. Furthermore it relates to a process for the preparation of these compounds.

Abstract: This invention provides compounds of Formula I having the structure wherein: B, C, D, and R1 are as defined hereinbefore in the specification, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 1-benzyl-naphthyls which are &agr;-substituted with ether, thioether, amino, hydrazino, cyano or halo that are useful for the treatment of the various medical indications associated with post-menopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus and cervix. The present invention further relates to intermediate compounds and processes useful for preparing the pharmaceutically active compounds of the present invention, and pharmaceutical compositions.

Abstract: There is disclosed substituted thiocarboxamides compounds of the formula (I): wherein R1, R2, R3 and Z are as defined in the specification. The compounds are useful as herbicides.

Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: 1

Abstract: Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof aryloxyalkylamines, including pyridyloxylalkylamines and phenoxyalkylamines.

Abstract: Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof aryloxyalkylamines, including pyridyloxylalkylamines and phenoxyalkylamines, such as (3-(3-pyridyloxy)propyl)methylamine and (3-(5-bromo(3-pyridyloxy))propyl)methylamine.

Abstract: This invention relates to a compound of formula I: or a pharmaceutically acceptable salt thereof; in which preferably R3, R4 and R6 are each hydrogen; X is C═O or CH2; and R7 and R8 are each independently selected from the group consisting of hydrogen, (C1-C12)alkyl, (C3-C8)cycloalkyl and (C1-C12)alkyl(C6-C14)aryl; or R7 and R8 when taken together form a (C2-C7)alkylene group; or —NR7R8 together forms a (C2-C14)heterocyclic or substituted (C2-C14)heterocyclic. Such compounds modulate the activity of serine hydrolases and can be used in pharmaceutical compositions for the treatment of Alzheimer's disease.

Abstract: The invention provides pyridoxal and pyridoxine analogues, pharmaceutical compositions containing pyridoxine and pyridoxal analogues, and methods of administering pharmaceutical compositions containing a therapeutically effective amount of at least one of these analogues. In accordance with the present invention, the pyridoxal and pyridoxine analogues can be used in the treatment of cardiovascular or related diseases and in the treatment of symptoms thereof.

Abstract: A novel process is provided for the preparation of imidazolidinone &agr;v&bgr;3/&agr;v&bgr;5 integrin antagonists, and the useful intermediates obtained therein. These compounds are antagonists of &agr;v&bgr;3/&agr;v&bgr;5 integrin receptors and thus useful for inhibiting bone resorption and treating and preventing osteoporosis. Also disclosed is 3-{2-oxo-3-[3-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-propyl]imidazolidin-1-yl}-3(S)-(6-methoxy-pyridin-3-yl)-propionic acid in the form of a hemihydrate.

Abstract: The invention relates to a method for producing optically pure compounds of 3(R)- and 3(S)-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine or its carboxylic acid esters by reacting the enantiomer mixtures stereoselectively, using an enzyme.

Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.

Abstract: The present invention provides a compound of formula I wherein R1 is H, OH, halo, OCO(C1-C6 alkyl), OCO(aryl), OSO2(C4-C6 alkyl), OCOO(C1-C6 alkyl), OCOO(aryl), OCONH(C1-C6 alkyl), or OCON(C1-C6 alkyl)2; R2 is aryl, C1-C6 alkyl, C3-C6 cycloalkyl, or 4-cyclohexanol; R3 is O(CH2)2 or O(CH2)3; R4 and R5 are optionally CO(CH2)2CH3, CO(CH2)3CH3, C1-C6 alkyl, or R4 and R5 combine to form, with the nitrogen to which they are attached, piperidine, morpholine, pyrrolidine, 3-methylpyrrolidine, 3,3-dimethylpyrrolidine, 3,4-dimethylpyrrolidine, azepine, or pipecoline; and pharmaceutically acceptable salts thereof. The invention further provides pharmaceutical compositions containing compounds of formula I and methods of use for the compounds of formula I.