Abstract: A novel process for the manufacture of compounds of the formula wherein R1 and R2 independently represent aroyl. The present invention also concerns novel intermediates used in the novel process for making compounds of formula I.

Abstract: This invention provides novel azepane derivatives or pharmaceutically acceptable salts thereof, according to the general formula (I) wherein the symbols are defined in the specification, as well as processes for their manufacture. The compounds according to this invention possess anti-cell proliferation activity and show an increased plasma-stability.

Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6, R7, R8, R9, X, b, k, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

Abstract: The invention relates to photoisomerizable compounds of formula I wherein A, Z, L, R, R1, k, m and r are defined herein.

Abstract: The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile and a chiral or prochiral cyclic substrate in the presence of a non-racemic, chiral catalyst to produce a stereoisomerically- and/or regioisomerically-enriched product. The present invention also relates to hydrolytic kinetic resolutions of racemic and diastereomeric mixtures of epoxides.

Abstract: The invention concerns amide derivatives of the Formula (I) wherein R3 is (1-6C)alkyl or halogeno; Q is aryl or heteroaryl which optionally bears 1, 2, 3 or 4 substituents such as hydroxy, halogeno, trifluoromethyl, cyano, (1-6C)alkyl, (1-6C)alkoxy, halogeno(1-6C)alkyl, hydroxy-(1-6C)alkyl, di-[(1-6C)alklyl]amino-(1-6C)alkyl, hydroxy-(2-6C)alkoxy, (1-6)alkoxy-(2-6C)alkoxy, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, amino-2(2-6C)alkylamino, N-(1-6C)alkyl-(1-6C)alkylamino-(2-6C)alkylamino, aryl, aryl-(1-6C)alkoxy, heteroaryl, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyl-(1-6C)alkyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; p is 0-2 and R2 is a substituent such as hydroxy and halogeno; q is 0-4; and R4 includes optionally substituted aryl, cycloalkyl, heteroaryl and heterocyclyl; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of disease

Abstract: The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile and a chiral or prochiral cyclic substrate in the presence of a non-racemic, chiral catalyst to produce a stereoisomerically- and/or regioisomerically-enriched product. The present invention also relates to hydrolytic kinetic resolutions of racemic and diastereomeric mixtures of epoxides.

Abstract: Disclosed are compounds having the formula: where R1=H, C1-C6 alkyl, cycloalkyl, R2=H, C1-C6 alkyl, cycloalkyl W=CnH2n-m—NH (n=1-6, m=0, 2, or 4), Z=CONR8(CH2)n, CONR8(CH2)nCO, P(CH3)OCHR8OCOR9, SO2, SO2(CH2)n, SO2(CH2)nCO, SO2NR8(CH2)n, SO2NR8(CH2)nCO, n=1-4 R4=H, (CH2)nOH, (CH2)nOCOR10, (CH2)nNR10R11, (CH2)nCONR10R11, n=0-4 R5=H, (CH2)nNR12R13, n=0-4 R6=H, (CH2)nNR14R15, n=0-4 R7=H, C1-C6 alkyl, cycloalkyl; R8=H, C1-C6 alkyl, cycloalkyl; R9=H, C1-C6 alkyl, cycloalkyl; R10=H, C1-C6 alkyl, cycloalkyl; R11=H, C1-C6 alkyl, cycloalkyl; R12=H, C1-C6 alkyl, cycloalkyl; R13=H, C1-C6 alkyl, cycloalkyl; R14=H, C1-C6 alkyl, cycloalkyl; R15=H, C1-C6 alkyl, cycloalkyl Dashed lines: optional; conformational constraint by (CH2)n, n=1-3, R′=H or O(═) as well as pharmaceuticals c

Abstract: The present invention relates to novel compounds of Formula (I), to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases.

Abstract: The present invention provides certain cycloalkenylsulfonamide derivatives of the formula: 1

Abstract: The present invention relates to novel compounds of formula (I), to a process for their menufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases.

Abstract: The present invention relates to chemical compounds comprising a nitric oxide (NO) donor and a superoxide ion (O2−) scavenger, their preparation and their use in the treatment of conditions associated with oxidative stress or endothelial dysfunction. In particular, the present invention relates to chemical compounds of Formula (I) wherein: R1 may be the same of different and are independently selected from hydrogen, alkoyl, carboxy, hydroxy, amino, amido, cyano, nitro, thio, sulphonyl, sulphoxide alkyl groups comprising an NO-donor, provided that at least one R1 is a group comprising an NO-donor; R2 may be the same or different and are independently selected from alkyl groups; n is an integer 1, 2, or 3; or a salt thereof.

Abstract: The present invention is related to substantially hydrophilic sulfonamide derivatives, or sulfonamide derivatives having a substantially hydrophilic moiety, of formula I notably for use as pharmaceutically active compounds, as well as 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 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation.

Abstract: The present invention is related to benzsulfonamide derivatives of formula I notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzsulfonamide derivatives. Said benzsulfonamide derivatives are ef-ficient modulators of the JNK pathway, they are in particular efficient and selective in-hibitors of JNK 2 and 3. The present invention is furthermore related to novel benzsul-fonamide derivatives as well as to methods of their preparation (I). The compounds of formula I according to the present invention being suitable pharma-ceutical agents are those wherein Ar1 is a substituted or unsubstituted aryl or heteroaryl group. X is O or S, preferably O.R1 is hydrogen or a C1-C6-alkyl group, preferably H.R2 is hydrogen, —COOR3, —CONR3R3′, OH, a C1-C4 alkyl substituted with an OH group, a hydrazido carbonyl group, a sulfate, a sulfonate, an amine or an ammonium salt; n is either 0 or 1, preferably 1.

Abstract: The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.

Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6, R7, R8, R9, X, b, k, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

Abstract: The present invention provides C3-C6 1-amino-1-acyl cycloalkane-substituted 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.

Abstract: Selected novel carboxylic acid substituted heterocycle compounds are effective for prophylaxis and treatment of inflammation, tissue degradation, cancer, fibrosis and related diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of inflamation, tissue degradation and related diseases. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: A process for preparing N-alkenyl-amides by reacting the corresponding NH-amides with acetylenes in the liquid phase in the presence of basic alkali metal compounds and of a cocatalyst comprises using as the cocatalyst diols of the general formula (I) where X is branched or unbranched alkylene selected from the group consisting of where R1 to R6 are independently hydrogen or C1- to C4-alkyl; or branched or unbranched cyclic alkylene of 3 to 14 carbon atoms including 3 to 12 ring carbon atoms, their monoalkenyl ethers, their dialkenyl ethers or mixtures thereof.

Abstract: The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.

Abstract: A one-pot process for the preparation of functional alkoxyamines of the general formula (I), 1

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

Abstract: The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.

Abstract: This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: Compounds of formula (I): wherein R1 is bicyclyl or heterobicyclyl, R2 and R3 are each independently hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocyclyl, (C1-6)alkylthio, (C2-6)alkenylthio, (C2-6)alkynylthio, aryloxy, arylthio, heterocyclyloxy, heterocyclythio, (C1-6)alkoxy, (C1-6)alkenyloxy, aryl(C1-6)alkoxy, aryl(C1-6)alkylthio, amino, mono- or di-(C1-6)alkylamino, acylamino, sulfonylamino, cycloalkyl, cycloalkenyl, carboxylic acid (C1-6) ester, hydroxy, halogen, carboxamide: CONR8R9 where R8 and R9 are independently selected from the group consisting of hydrogen, alkyl, aryl, arylalkyl and heterocyclyl and includes R8 and R9 as part of a heterocyclyl group, or R2 and R3 together form a cyclic alkyl or alkenyl; R4 and R5 are each independently aryl, heteroaryl, heterocyclyl, alkoxy, alkyl, hydroxy or optionally substituted amino; R6 and R7 are each hydrogen or together form a fused aryl ring; and m and n are each independently from 0 to 2; with the proviso that when n=1 neither R4 nor R

Abstract: A process for preparing N-alkenyl-amides by reacting the corresponding NH-amides with acetylenes in the liquid phase in the presence of basic alkali metal compounds and of a cocatalyst comprises using as the cocatalyst compounds of the general formulae (Ia) and/or (Ib) R1O—(CH2CH2CH2CH2O)n—H  (Ia): R1O—(CH2CH2CH2CH2O)n—R2,  (Ib): where n is 1, 2 or 3 and R1 and R2 are independently C1- to C6-alkyl or C2- to C6-alkenyl, or together a butenyl unit.

Abstract: Sulfonic acid ester derivatives represented by the general formula (4) or (5) are produced by reacting an amino alcohol derivative represented by the general formula (1) or (2) with an organic sulfonyl halide represented by the general formula (3), in a mixed solvent composed of an aprotic organic solvent and water in the presence of a non-water-prohibiting inorganic base. This procedure can be carried out in a simple, easy, safe and economical manner while reducing the load on the environment.

Abstract: Sulfonic acid ester derivatives represented by the general formula (4) or (5) are produced by reacting an amino alcohol derivative represented by the general formula (1) or (2) with an organic sulfonyl halide represented by the general formula (3), in a mixed solvent composed of an aprotic organic solvent and water in the presence of a non-water-prohibiting inorganic base. This procedure can be carried out in a simple, easy, safe and economical manner while reducing the load on the environment.

Abstract: Sulfonic acid ester derivatives represented by the general formula (4) or (5) are produced by reacting an amino alcohol derivative represented by the general formula (1) or (2) with an organic sulfonyl halide represented by the general formula (3), in a mixed solvent composed of an aprotic organic solvent and water in the presence of a non-water-prohibiting inorganic base. This procedure can be carried out in a simple, easy, safe and economical manner while reducing the load on the environment.

Abstract: The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system.

Abstract: The present invention relates to novel prodrugs of pharmaceutical compounds containing one or more N—H bonds. More specifically, the present embodiment of the invention relates to prodrugs wherein sulfur-containing promoieties are attached to pharmaceutical compounds which contain one or more N—H bonds to produce prodrugs containing at least one N—S bond. These N—S bond-containing prodrugs could have optimized stability, solubility, cell membrane permeability, pharmacokinetic properties and other pharmaceutical properties over the pharmaceutical compounds from which they are formed, depending upon the nature of the promoiety. Reversion of the prodrug to the parent pharmaceutical compound occurs by the reaction of the prodrugs with thiol molecules such as cysteine, glutathione or any other thiol containing molecule.

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 invention relates to compounds of the general formula (I): 1

Abstract: This invention relates to novel compounds of Formula (I) to (VII), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: Alkylsulfonamido heterocyclic thrombin inhibitors are provided which have the structure wherein G is  wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; R is hydrogen, hydroxyalkyl, aminoalkyl, alkyl, cycloalkyl, amidoalkyl, arylalkyl, alkenyl, aryl, alkynyl, arylalkoxyalkyl, or an amino acid side chain; R1 and R2 are independently hydrogen, lower alkyl, cycloalkyl, aryl, hydroxy, alkoxy, oxo, thioketal, thioalkyl, thioaryl, amino or alkylamino; or R1 and R2 can be taken together with the carbons to which they are attached to form a cycloalkyl, aryl or heteroaryl ring.

Abstract: This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: Homoiminopiperidinyl Hexanoic Acid derivatives and pharmaceutically acceptable salts thereof useful in the inhibition of the inducible isoform of nitric oxide synthase are disclosed.

Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation.

Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states.

Abstract: Hydroxyazepanes display inhibitory activity with respect to glycosidase, with Ki values from-moderate to low micromolar range. Benzyl and 3,6-dibenzyl derivatives of hydroxyazepanes display inhibitory activity with respect to HIV protease. These compounds are synthesized either by chemoenzymatic or chemical methodologies.

Abstract: Compound of formula (I): wherein: n represents 0 or 1, R1 represents hydrogen, arylalkyl, alkyl, acyl, alkoxycarbonyl, arylalkoxycarbonyl or trifluoroacetyl, R2 represents alkyl, X represents oxygen, chlorine, OR3, SR4 or NOR5, R3 represents hydrogen , alkyl, acyl, alkoxycarbonyl or arylalkoxycarbonyl, R4 represents hydrogen, alkyl or aryl, R5 represents hydrogen or optionally substituted alkyl, represents a single or double bond, Ar represents aryl or heteroaryl, its isomers and addition salts thereof with a pharmaceutically acceptable acid, and medicinal products containing the same which are useful as facilitators of memory and cognition and antalgic agents.

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

Abstract: Sulfamide compounds having formula (I) are described as well as their use in the treatment of diseases dependent on the signaling pathways associated with &bgr;-adrenergic receptors, such as obesity, diabetes, hypertension, gastrointestinal hypo- or hyper-motility and cardiovascular diseases.

Abstract: The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile and a chiral or prochiral cyclic substrate in the presence of a non-racemic, chiral catalyst to produce a stereoisomerically- and/or regioisomerically-enriched product. The present invention also relates to hydrolytic kinetic resolutions of racemic and diastereomeric mixtures of epoxides.

Abstract: The present invention relates to chemical compounds comprising a nitric oxide (NO) donor and a superoxide ion (O2−) scavenger, their preparation and their use in the treatment of conditions associated with oxidative stress or endothelial dysfunction. For example, the present invention relates to chemical compounds of the formula: wherein R1 may be the same or different and are independently selected from hydrogen, alkoyl, alkoxy, carboxy, hydroxy, amino, amido, cyano, nitro, thio, sulphonyl, sulphoxide alkyl groups and groups comprising an NO-donor, provided that at least one R1 is a group comprising an NO-donor; R2 may the same or different and are independently selected from alkyl groups; n is an integer 1, 2 or 3; or a salt thereof.

Abstract: A nitrogen-containing heterocyclic compound represented by the following formula (I) or (II): wherein X1 and X2 are the same or different, each representing a hydrogen atom, an alkyl group, or an electron attractive group and at least one of which being an electron attractive group; R1 and R2 are the same or different, each representing a hydrogen atom, an alkyl group, an aryl group, an aralkyl group, or an alkoxy group, and the ring Z represents a hydrocarbon ring which may have a substituent or a heterocycle which may have a substituent. The compound of the present invention is capable of emitting light or changing its color upon irradiation of light or under the action of an electric field.

Abstract: A new process is described for the preparation of a compound of the formula I 1

Abstract: The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I).

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 invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I).