Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.

Abstract: The invention is directed to compounds of Formula (I) described herein useful as CETP inhibitors, compositions containing them, and methods of using them.

Abstract: The present invention provides compounds, for example, of formula (I): wherein R1, R2, and R3 have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods, and processes and intermediates useful for preparing compounds of formula I.

Abstract: The present invention is directed to novel compositions and their application as pharmaceuticals for the treatment of disease. Methods of upregulation of GLUT4 via activation of peroxisome proliferator activated receptor delta activity in the adipose tissue of a human or animal subject are also provided, for the treatment of conditions such as diabetes, obesity, insulin resistance, metabolic syndrome, and others in which a reduction in insulin resistance, an increase in glucose utilization, a reduction in visceral fat, a reduction in triglyceride (TG) levels, or an increase in levels of high-density lipoprotein (HDL), is beneficial.

Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals.

Abstract: Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.

Abstract: ?- and ?-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: Compounds of formula (I), wherein one of R1 and R2 is selected from a group (IA), ring A is substituted pyridin-z-yl of thiazol-z-yl, the other substituents are as described in the description and their use in the treatment or prevention of a disease or medical conditions mediated through glucokinase

Abstract: Oral pharmaceutical formulation which improves the bioavailability of pharmaceuticals which are substantially water and oil insoluble is disclosed. In addition to the pharmaceutical, the formulation includes an emulsifier, an oil and an solubilizer. Alternatively, the formulation includes an aqueous solution of solubilizer.

Abstract: Certain Alpha- and Beta-amino acid hydroxyethylamino sulfamic acid derivatives represented by the following formula are useful as retroviral protease inhibitors:

Abstract: A compound of the formula (I): wherein Z4, Z5 and Z9 each is independently carbon atom or nitrogen atom; Y is hydroxy, mercapto or amino; RA is a group of the formula: (wherein C ring is nitrogen-containing heteroaryl) has an inhibitory activity against integrase.

Abstract: In one embodiment, the present application discloses a process for making the compound of the formula:

Abstract: A class of benzopyran, derivatives is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I? wherein X, A1, A2, A3, A4, R, R?, R1 and R2 are as described in the specification.

Abstract: The invention relates to derivatives corresponding to formula I: in which X is an alkyl-(CH2)n— chain with n=0, 1 or 2, or O or N, Z is an aromatic which may contain heteroatoms chosen from O, N or S, as substitutions for the carbon atoms constituting said aromatic ring, this ring being substituted or otherwise with Rb, Rb represents 1 to 3 substituents chosen from —OH, —OR, —COOH, —COOR, —COH, —COR, —NH2, —NH(R), —NH(R,R?), —SH, —SR and CN, Ra is H or —(CH2)n?—Y, with n?=0, 1, 2 or 3 and Y and —CH3, —COOH, —COOR, —CN, —OH, —OR, SR, or an aryl group optionally substituted with Rb, R and R? represent a linear or branched alkyl chain of 1 to 4 C, and their pharmaceutically acceptable salts. Application as active ingredient of medicaments inhibiting retrovirus integrases.

Abstract: This invention provides caspase inhibitors having the formula: wherein Ring A is an optionally substituted piperidine, tetrahydroquinoline or tetrahydroisoquinoline ring; R1 is hydrogen, CHN2, R, or —CH2Y; R is an optionally substituted group selected from an aliphatic group, an aryl group, an aralkyl group, a heterocyclic group, or an heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; Ar is an optionally substituted aryl group; and R3 is hydrogen, an optionally substituted C1-6 alkyl, F2, CN, aryl or R3 is attached to Ar to form an unsaturated or partially saturated five or six membered fused ring having 0–2 heteroatoms. The compounds are useful for treating caspase-mediated diseases in mammals.

Abstract: This invention comprises the novel compounds of formula (I) wherein r, s, t, Y1—Y2, R1, R2, R3, R4, R5 and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

Abstract: The present invention provides compounds, and pharmaceutical compositions containing those compounds, that are active at metabotropic glutamate receptors. The compounds are useful for treating neurological diseases and disorders. Methods of preparing the compounds also are disclosed.

Abstract: a prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein L1 and L2 are R1—Y— wherein each (R1—Y)— substituent is defined independently of the other; Y is C1-4alkanediyl, C2-4alkenediyl, C2-4alkynediyl, C(?O), or a direct bond; R1 is hydrogen, cyano, aryl or a substituted or unsubstituted C1-14heterocycle; ?Z1—Z2?Z3— represents a radical of formula ?N—N?CH— (a-1), ?N—CH?N— (a-2), ?CH—N?N— (a-3); X is SO2, (CH2)n wherein n is 1 to 4, C(?O), C(?S), or a direct bond, R2 is aryl, C3-7cycloalkyl, C3-7cycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio, C1-12alkyl or C1-12alkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalky

Abstract: Disclosed are compounds of the formula: or pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof, wherein R1, R2, R3, X, Q1 and Q2 are defined herein, which compounds are ligands for neurokinin receptors, in particular NK-3 receptors, and are therefor useful in the treatment of a wide range of diseases or disorders including, but not limited to depression, anxiety, psychosis, obesity, pain, Parkinson's disease, Alzheimer's disease, neurodegenerative diseases, movement disorders, respiratory diseases, inflammatory diseases, neuropathy, immune disorders, migraine, biliary disfunction, and dermatitis.

Abstract: Pharmaceutical compositions incorporate compounds that are capable of affecting nicotinic cholinergic receptors. A wide variety of conditions and disorders, and particularly conditions and disorders associated with dysfunction of the central and autonomic nervous systems can be treated using pharmaceutical compositions incorporating compounds in which an aromatic ring is bridged with an ethylenic or acetylenic unit to an azabicyclic moiety.

Abstract: Novel PDF inhibitors and novel methods for their use are provided.

Abstract: Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picomaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.

Abstract: A process for making an aromatic aldehyde in which a sulfoxide is reacted with a dihalogenated aromatic compound in the absence of an effective amount of an activating reagent. The aldehyde may then be used to make other compounds, such as a compound that acts as a cPLA inhibitor.

Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.

Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds having Formula I: or pharmaceutically acceptable salts thereof; wherein Q is phenyl, benzyl, pyridyl, thienyl, indolyl, quinolinyl, benzothienyl, biphenylyl, or imidazolyl; any of which can include one or more optional substituents independently selected from halo, trifluoromethyl, hydroxy, amino, nitro, cyano, C1 alkoxy, C1-3 alkyl, methylenedioxy, carboxamido, acetamido, or amidino; X is methylene, carbonyl, or sulfonyl; Z is methylene, ethylene, or propylene; M is methylene or ethylene; and R1 R2 and R3 are independently hydrogen or C1-3 alkyl.

Abstract: Compounds of the general formula (I): or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R1 is a 5- to 6-membered aromatic ring which bears a substituent represented by the general formula: R-Z1-X-Z2- (wherein R1 is hydrogen or optionally substituted hydrocarbyl; X is optionally substituted alkylene; and Z1 and Z2 are each a heteroatom) and may be further substituted, with R being optionally bonded to the aromatic ring to form another ring; Y is optionally substituted imino; and R2 and R3 are each optionally substituted aliphatic hydrocarbyl or an optionally Substituted hetero-alicyclic group.

Abstract: A melanin-concentrating hormone antagonist comprising a compound of the formula (I): wherein Ar1 is a cyclic group which may be substituted; X and Y are the same or different and are a spacer having a main chain of 1 to 6 atoms; Ar is a condensed polycyclic aromatic ring which may be substituted; R1 and R2 are the same or different and are hydrogen atom or a hydrocarbon group which may be substituted; or R1 and R2, together with the adjacent nitrogen atom, may form a nitrogen-containing heterocyclic ring which may be substituted; or R2, together with the adjacent nitrogen atom and Y, may form a nitrogen-containing heterocyclic ring which may be substituted; or R2, together with the adjacent nitrogen atom, Y and Ar, may form a condensed ring; or a salt thereof is useful as an agent for preventing or treating obesity, etc.

Abstract: Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

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

Abstract: Compound of formula (I): wherein: V represents a single bond or an alkylene chain, M represents a single bond or an alkylene chain, A and E each represents nitrogen or CH, but at least one of the two groups A or E represents nitrogen, W represents a group of formula (i), (ii) or (iii): wherein: X represents carbonyl, sulphonyl or sulphoxide, G1, G2 and G3 are as defined in the description, T represents a fused phenyl group or a fused pyridyl group, R1 represents hydrogen, linear or branched (C1-C6)alkyl, aryl or aryl-(C1-C6)alkyl in which the alkyl moiety is linear or branched, R2a and R2b, which are the same or different, are as defined in the description, R3 represents aryl or heteroaryl-A as defined in the description, each of which groups may optionally be substituted, Y represents aryloxy, heteroaryloxy or heteroaryl-B as defined in the description, each of which groups may optionally be substituted, its isomers, its hydrates, its solvates and addition salts thereof with a pharmaceutically a

Abstract: Selected bis-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 invention relates to derivatives corresponding to formula I: 1

Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.

Abstract: This invention is directed to physiologically active compounds of formula (I) wherein represents a bicyclic ring system, of about 10 to about 13 ring members, in which the ring is an azaheterocycle, and the ring represents an azaheteroaryl ring, or an optionally halo substituted benzene ring; R1 represents hydrogen or a straight- or branched-chain alkyl group of 1 to about 4 carbon atoms, optionally substituted by hydroxy or one or more halogen atoms, or when Z1 represents a direct bond R1 may also represent a lower alkenyl or lower alkynyl group, or a formyl group; R2 represents hydrogen, alkenyl, alkoxy, alkyl, alkylsulphinyl, alkylsulphonyl, alkylthio, aryl, arylalkyloxy, arylalkylsulphinyl, arylalkylsulphonyl, arylalkylthio, aryloxy, arylsulphinyl, arylsulphonyl, arylthio, cyano, cycloalkenyl, cycloalkenyloxy, cycloalkyl, cycloalkyloxy, heteroaryl, heteroarylalkyloxy, heteroaryloxy, hydroxy, —SO2NR4R5, —NR4SO2R5, —

Abstract: Compounds of formula (I): wherein: V represents a single bond or a linear or branched (C1-C6)alkylene chain, M represents a single bond or a linear or branched (C1-C6)alkylene chain, A and E each represents nitrogen or CH, but at least one of the two groups A or E represents nitrogen, W represents a group of formula (i): X represents carbonyl, G1 represents a linear C3 alkylene chain optionally containing a double bond and/or being optionally substituted by a hydroxyl group, their isomers, their hydrates, their solvates, and additional salts thereof with a pharmaceutically acceptable acid, and medicinal products containing the same which are useful in the treatment of diseases or pathological conditions in which endothelial dysfunction is known.

Abstract: A compound, or a solvate or a salt thereof, of formula (I): wherein, Ar is an optionally substituted aryl or a C5-7 cycloalkdienyl group, or an optionally substituted C5-7 cycloalkyl group, or an optionally substituted single or fused ring aromatic heterocyclic group; R is hydrogen, linear or branched C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl; R1 represents hydrogen or up to three optional substituents selected from the list consisting of: C1-6 alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, amino or mono- and di-C1-6 alkylamino, R2 represents a moiety —(CH2)n—NYY2 wherein n is an integer in the range of from 1 to 9, Y1 and Y2 are independently selected from C1-6-alkyl; C1-6 alkyl substituted with hydroxy, alkoxy, C1-6 alkylamino or bis (C1-6 alkyl) amino; C3-6 cycloalkyl; C4-6 azacycloalkyl; C1-6-alkenyl; aryl or aryl-C1-6-alkyl or Y1 and Y2 together with the nit

Abstract: Tetrahydroquinoline compounds of general formula (I) or pharmacologically acceptable salts thereof, which have a specific and strong binding affinity for AR, exhibit AR agonism or antagonism, have therapeutic effects on AR-mediated diseases, particularly by not acting excessively on the prostate as AR agonists, but by showing potent action on skeletal muscle tissue and bone tissue; and pharmaceutical compositions comprising the compounds or the salts as active ingredients:

Abstract: The present invention concerns a process for oxidising an aromatic aldehyde to the corresponding carboxylic acid. The process of the invention for preparing an aromatic acid by oxidising an aromatic aldehyde consists of carrying out the oxidation of the aromatic aldehyde in a basic medium using molecular oxygen or a gas containing molecular oxygen in the presence of a catalyst, and is characterized in that oxidation is carried out in the presence of an effective quantity of a palladium and/or platinum based catalyst under conditions such that oxidation is carried out in a diffusion regime.

Abstract: A compound of formula (I) as detailed in the specification or a pharmaceutically acceptable salt or solvate thereof, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds in medicine.

Abstract: A compound of formula (I) as detailed in the specification or a pharmaceutically acceptable salt or solvate thereof, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds in medicine. Figure (I) wherein: R1 is H or alkyl; R2 is aryl or cycloalkyl or heteroaryl; R3 is H or alkyl, wherein the group may be optionally substituted by one or more fluorine atoms; R4 is NR8R9; R8 is H, lakyl or R11R12 and R9 is H, alkyl or R13R14; or R8 and R9 together with the N atom to wich they are attached form a heterocyclic ring comprising 4-8 ring members, said ring members optionally including in addition to said N atom one or more further heteroatoms selected from N, O or S; and further detailed in the specification.

Abstract: A compound, or a solvate or a salt thereof, of formula (I): wherein, Ar is an optionally substituted aryl or a C5-7 cycloalkdienyl group, or a C5-7 cycloalkyl group or an optionally substituted single or fused ring aromatic heterocyclic group; R is C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, optionally substituted phenyl or phenyl C1-6 alkyl, an optionally substituted five-membered heteroaromatic ring comprising up to four heteroatoms selected from O and N, hydroxy C1-6 alkyl, amino C1-6 alkyl, C1-6 alkylaminoalkyl, di C1-6 alkylaminoalkyl, C1-6 acylaminoalkyl, C1-6 alkoxyalkyl, C1-6 alkylcarbonyl, carboxy, C1-6 alkoxycarbonyl, C1-6 alkoxycarbonyl C1-6 alkyl, aminocarbonyl, C1-6 alkylaminocarbonyl, di C1-6 alkylaminocarbonyl, halogeno C1-6 alkyl; or R is a group —(CH2)p— wherein p is 2 or 3 which group forms a ring with a carbon atom of Ar, R1 represents hydrogen or up to four optional substituents selected from the list consisting of: C1-6 alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, h

Abstract: Heterocyclic dicarboxylic acid diamide derivative represented by the general formula (I): wherein R1, R2 and R3 represent each H, optionally halogenated C3-6 cycloalkyl, etc.; Het represents a 5- or 6-membered heterocycle; X and Y represent each halocyano, nitro, optionally halogenated C3-6, cycloalkyl, optionally substituted phenyl, an optionally substituted heterocycle, etc; n is from 0 to 3; m is from 1 to 5; Z1 and Z2 represent each O or S; and B1 to B4 represent each C or N. Agricultural/horticultural insecticides having an excellent controlling effect on pest insects such as diamond-back moth (Pluntella xylostella) and tobacco cutworm (Spodoptera litura).

Abstract: The present invention provides to an isoxazoline derivative of formula (I), the pharmaceutically acceptable salts, esters and stereochemically isomeric forms thereof, and the use of the derivative in inhibiting the activity of caspases. The present invention also provides a pharmaceutical composition for preventing inflammation and apoptosis which comprise the isoxazoline derivative, pharmaceutically acceptable salts, esters and stereochemically isomeric forms thereof and the process for preparing the same. The derivative according to the present invention can be effectively used in treating diseases due to caspases, such as, for example the disease in which cells are abnormally died, dementia, cerebral stroke, AIDS, diabetes, gastric ulcer, hepatic injury by hepatitis, sepsis, organ transplantation rejection reaction and anti-inflammation.

Abstract: The present invention relates to compound of formula (I) wherein R1, R2, R3, R4, R5 and n are as defined in the description and claims and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment of diseases which are associated with cysteine proteases such as osteoporosis, osteoarthritis, rheumatoid arthritis, tumor metastasis, glomerulonephritis, atherosclerosis, myocardial infarction, angina pectoris, instable angina pectoris, stroke, plaque rupture, transient ischemic attacks, amaurosis fugax, peripheral arterial occlusive disease, restenosis after angioplasty and stent placement, abdominal aortic aneurysm formation, inflammation, autoimmune disease, malaria, ocular fundus tissue cytopathy and respiratory disease.

Abstract: Certain compounds of formula (I) below or a pharmaceutically acceptable salt or hydrate thereof:

Abstract: Quinolylpropylpiperidine derivatives of general formula (I) in which R1 is hydrogen or fluorine, R2 is carboxyl, carboxymethyl or hydroxymethyl, R3 is alkyl substituted either with phenylthio optionally substituted with halogen, hydroxyl, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkyloxycarbonyl, cyano or amino, or with cycloalkylthio (3 to 7 members) optionally substituted with halogen or trifluoromethyl, or with heteroarylthio (5 to 6 members and 1 to 4 heteroatoms chosen from N, O and S), optionally substituted with halogen, hydroxyl, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkyloxycarbonyl, cyano or amino or R3 is propargyl substituted by phenyl or heteroaryl as defined above and R4 is alkyl, alkenyl-CH2— or alkynyl-CH2—, cycloalkyl or cycloalkylalkyl, in their various isomeric forms, separate or as mixtures, and also their salts, their preparation process and intermediates and the compositions containing them.

Abstract: A process for making an aromatic aldehyde in which a sulfoxide is reacted with a dihalogenated aromatic compound in the absence of an effective amount of an activating reagent. The aldehyde may then be used to make other compounds, such as a compound that acts as a cPLA inhibitor.

Abstract: 2-Cyclopropyl-4-(4′-fluorophenyl)quinoline-3-carboxyaldehyde useful as a material for pharmaceutical products, can be obtained by reacting 3-cyclopropyl-3-oxopropanenitrile with 2-amino-4′-fluorobenzophenone to obtain 2-cyclopropyl-4-(4′-fluorophenyl)quinoline-3-carbonitrile, and reducing it.

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.