Abstract: Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty liver, circulatory system diseases, for example, stenocardia, acute/congestive cardiac insufficiency, cardiac infarction, coronary arteriosclerosis, hypertension, nephropathy, sleep disorder and various diseases accompanied by sleep disorder such as idiopathic hypersomnnia, repetitive hypersomnnia, true hypersomnnia, narcolepsy, sleep periodic acromotion disorder, sleep apnea syndrome, circadian rhythm disorder, chronic fatigue syndrome, REM sleep disorder, senile insomnia, night worker sleep insanitation, idiopathic insomnia, repetitive insomnia, true insomnia, electrolyte metabolism disorder, and central and peripheral nervous system diseases such as bulimia, emotional disorder, melancholia, anxiety, epilepsy, delirium, dementia, shinzophrenia, attention deficit/hyperactivity disorder, memory disorder, Alzheimer's dis

Abstract: A subject of the present application is new derivatives of 4-aminopiperidines of formula in which R1, R2 and R3 represent various radical, and their preparation processes by synthetic methods in parallel in liquid and solid phase. These products having a good affinity with certain sub-types of somatostatin receptors, they are particularly useful for treating the pathological states or diseases in which one (or more) somatostatin receptors are involved.

Abstract: The invention describes novel compound of the formula I, wherein the general symbols are as defined in claim 1, as stabilizers for protecting organic materials, in particular synthetic polymers, against oxidative, thermal, dynamic, light-induced and/or ozone-induced degradation.

Abstract: Disclosed is a substance having an antagonistic effect on the binding of histamine to a histamine H3 receptor or an inhibitory effect on the activity which a histamine H3 receptor constantly exhibits. A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof; (I) wherein R1 represents a phenyl group which may be substituted or the like and R2 represents a cyano group which may be substituted or the like, or R1 and R2 together form an aliphatic heterocylic ring which may be substituted; R3 represents a group represented by the formula (II-1) below; and all of X1 to X4 represent a carbon atom or the like: (II-1) where R4 and R5 represent a lower alkyl group or the like; and m1 represents an integer of 2 to 4.

Abstract: The present invention provides a compound of formula (I), wherein: Z is (A) OR (B) and wherein the remaining variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of achemokine (such as CCR3) or H1 mediated disease state.

Abstract: The invention describes novel compound of the formula (I), wherein the general symbols are as defined in claim 1, as stabilizers for protecting organic materials, in particular synthetic polymers, against oxidative, thermal, dynamic, light-induced and/or ozone-induced degradation.

Abstract: Substituted phenylalkynes of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.

Abstract: Diaminoalkanes of Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.

Abstract: Disclosed are compounds of formula I: wherein R1, R2, R3 and X are as defined herein, in free or salt form, which are useful as CCR5 inhibitors, e.g. in the prevention or treatment of disorders mediated by interactions between chemokine receptors and their ligands.

Abstract: A subject of the present application is new derivatives of 4-aminopiperidines of formula in which R1, R2 and R3 represent various radical, and their preparation processes by synthetic methods in parallel in liquid and solid phase. These products having a good affinity with certain sub-types of somatostatin receptors, they are particularly useful for treating the pathological states or diseases in which one (or more) somatostatin receptors are involved.

Abstract: The present invention discloses and claims a compound of general formula (I) wherein A, X and R2 are as described herein. Also disclosed and claimed is application of this compound in a variety of therapeutic applications.

Abstract: The present invention discloses compounds which, are novel receptor antagonists for NPY Y5 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y5 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

Abstract: Compounds of formula (I) in which R, R1, R2, n and X1 have the meanings given in the specification are Factor Xa inhibitors useful in the treatment of thrombotic disorders.

Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, r, R1, R2, R3, R4, R5, R6, R7, and W are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, to the preparation of such compounds and pharmaceutical compositions containing them. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.

Abstract: This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —XC(O)Y, alkylene-XC(O)Y, cycloalkylene-X—C(O)—Y, —CH—X—C(O)—NR3—Y or —CH—X—C(O)—Y, wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.

Abstract: Substituted non-imidazole aryloxypiperidine compounds, compositions containing them, and methods of making and using them to treat or prevent histamine-mediated conditions.

Abstract: This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —X(CO)Y, or alkylene-X(CO)Y wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.

Abstract: This invention discloses and claims a compound of general formula (I) in which R1 represents either a hydrogen atom, or an optionally substituted alkyl group, or a cycloalkylalkyl group, or an optionally substituted phenylalkyl group, or an alkenyl group, X represents a hydrogen atom or one or more substituents chosen from halogen atoms and trifluoromethyl, alkyl and alkoxy groups, R2 represents one or more substituents chosen from halogen atoms, optionally substituted alkoxy and optionally substituted amino. The compounds of this invention exhibit therapeutic utility.

Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.

Abstract: Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having the general structure: wherein Q is selected from the group consisting of N, O and S; L is any bivalent organic radical capable of linking each Q, such as C, CH, (CH2)1, or {(CH2)i—Y—(CH2)j}k, wherein Y is selected from the group consisting of CH2, an ether, a polyether, an amide, a polyamide, an ester, a sulfide, a urea, a thiourea, a guanidyl, a carbamoyl, a carbonate, a phosphate, a sulfate, a sulfoxide, an imine, a carbonyl, and a secondary amino group and wherein Y is optionally substituted by —X1—L?—X2—Z or —Z; R1–R6, independently of one another, are selected from the group consisting of H, —CH2)p—D—Z, an alkyl, an alkenyl, an aryl, and an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkylthio, a urea, a thiourea, a guanidyl, or a carbamoyl group, and

Abstract: The invention relates to benzofuran or benzothiophene derivatives of general formula: These compounds are of use as medicinal products, in particular in the treatment of pathological syndromes of the cardiovascular system.

Abstract: Compounds of formula (I) in which R1, R2, n and X1 have the meanings given in the specification are Factor Xa inhibitors useful in the treatment of thrombotic disorders.

Abstract: Compounds of formula (I) in which R, R1, R2, n and X1 have the meanings given in the specification are Factor Xa inhibitors useful in the treatment of thrombotic disorders.

Abstract: A water soluble derivative of buckministerfullerene (C50) having antiviral and virucidal properties is used to inhibit human retroviral replication and infections. The derivatized fullerene is symmetrically substituted with polar organic moieties containing 1 to 20 carbon atoms and optionally further containing oxygen or nitrogen.

Abstract: Liquid crystal mixture comprising compounds of formula (I) wherein R1: is H or a linear or branched alkyl group or branched alkenyl group R2: stands for a) H or F b) a linear or branched alkyl group or a linear or branched alkenyl group c) a radical wherein R3, R4, R5, R6: are an alkyl group M1, M2: represent independently from another a single bond, —OC(?O), —C(?O)O—, —OCH2—, —NH— A: is a) a linear or branched alkan-?,?-diylgroup or alkene-?,?-diyl group b) the group —C(?Y)— wherein Y is CH-Z with Z being phenylen-1,4-diyl, optionally substituted by one to three halogenatoms, alkyl or alkyloxy groups, c) the group —CHY wherein Y is CH2-Z with Z being phenylen-1,4-diyl, optionally substituted by one to three halogenatoms, alkyl or alkyloxy groups d) a group wherein p, q are 0, 1 or 2; M3 is a single bond or —OC(?O)—, —C(?O)O—, —OCH2—, —CH2O—, —C?C—, —CH2CH2—, —CH2CH2CH2CH2— the radicals are phenylen-1,4-diyl, X is H, OH, a linear or branched alkyl or alkyloxy group, m: is 0 or 1 X and M1-(A

Abstract: Methods and compositions are provided for the direct catalytic asymmetric aldol reaction of aldehydes with donor molecules selected from ketones and nitroalkyl compounds. The reactions employ as catalyst a Group 2A or Group 2B metal complex of a ligand of formula I, as defined further herein.

Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; —G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems recit

Abstract: The invention concerns compounds inhibiting LTA4 hydrolase of formula (I). The invention also concerns their therapeutic, in particular anti-inflammatory, applications.

Abstract: Couplers for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): wherein X is selected from halogen and R5SO4 where the halogen is preferably Cl, Br or I; R, R1 and R2 are each individually selected from C1 to C22 alkyl and C1 to C22 mono or dihydroxyalkyl, or two of R, R1 and R2 together with the nitrogen atom to which they are attached form a C3 to C6 saturated or unsaturated ring optionally containing in the ring one or more additional hetero atoms selected from O, S and N atoms; R3 and R4 are each individually selected from C1 to C6 alkyl, C1 to C6 hydroxyalkyl, C1 to C6 alkoxy, C1 to C6 aminoalkyl or R3 and R4 together form a C1 to C5 alkylene group; and R5 is selected from C1 to C22 alkyl and C1 to C22 mono or dihydroxyalkyl.

Abstract: The present invention relates to the synthesis of a new class of indeno [1,2-c]pyrazol-4-ones of formula (I): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.

Abstract: Compounds of formula (I): wherein L is CH or N; M is CH or N; provided that L and M are not both CH; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).

Abstract: The present invention discloses compounds, which are novel muscarinic receptor antagonists, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such muscarinic receptor antagonists as well as methods for using them to treat cognitive disorders such as Alzheimer's disease.

Abstract: In one embodiment, the present invention describes the synthesis of 4-[(Z)-(4-bromophenyl)(ethoxyimino)methyl]-1′-[(2,4-dimethyl-1-oxido-3-pyridinyl)carbonyl]-4′-methyl-1,4′-bipiperidine, and intermediates therefor from easily available starting materials by a simple route.

Abstract: The present invention relates to selected 4-imino-N-alkoxy-polyalkyl-peperidine compounds preparation, a polymerizable composition comprising a) at least one ethylenically unsaturated monomer and b) a 4-imino-N-alkoxy-polyalkyl-piperidine compound. Further aspects of the present invention are a process for polymerizing ethylenically unsaturated monomers, and the use of 4-imino-N-alkoxy-polyalkyl-piperidine compounds for controlled polymerization. The intermediate N-oxyl derivatives, a composition of the N-oxyl derivatives with ethylenically unsaturated monomers and a free radical initiator, as well as a process for polymerization are also subjects of the present invention.

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: This invention discloses novel gamma secretase inhibitors of the formula: 1

Abstract: Compounds of formula (I) are useful as inhibitors of trypsin like serine protease enzymes such as thrombin, factor VIIa, factor Xa, TF/FVIIa, and trypsin. These compounds could be useful to treat and/or prevent clotting disorders, and as anticoagulating agents.

Abstract: Compounds of the formula 1

Abstract: Piperidine derivatives of formula (I) as disclosed in the specification have interesting pharmaceutical properties e.g. as CCR5 inhibitors.

Abstract: A novel means for DNA compaction is provided. The object is accomplished by providing a fullerene derivative having 1 to 4 nitrogen-containing hydrophilic side chain(s) or its salt for DNA compaction. DNA compaction can be achieved effectively, and application to gene therapy is also expected.

Abstract: Couplers for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): wherein X is selected from halogen and R5SO4 where the halogen is preferably Cl, Br or I; R, R1 and R2 are each individually selected from C1 to C22 alkyl and C1 to C22 mono or dihydroxyalkyl, or two of R, R1 and R2 together with the nitrogen atom to which they are attached form a C3 to C6 saturated or unsaturated ring optionally containing in the ring one or more additional hetero atoms selected from O, S and N atoms; R3 and R 4 are each individually selected from C1 to C6 alkyl, C1 to C6 hydroxyalkyl, C1 to C6 alkoxy, C1 to C6 aminoalkyl or R3 and R4 together form a C1 to C5 alkylene group; and R5 is selected from C1 to C22 alkyl and C1 to C22 mono or dihydroxyalkyl.

Abstract: The present invention relates to 4-formylamino-N-methylpiperidine derivatives of the formula (I) where the variables are as defined in the Description, to a process for preparing these piperidine derivatives, to the use of these piperidine derivatives of the invention, or prepared according to the invention, for stabilizing organic material, in particular for stabilizing plastics or coating materials, and also to the use of these piperidine derivatives of the invention, or prepared according to the invention, as light stabilizers or stabilizers for wood surfaces. The present invention further relates to stabilized organic material which comprises these piperidine derivatives of the invention or prepared according to the invention.

Abstract: The present invention is directed to a series of novel substituted aminoalkylamide derivatives, pharmaceutical compositions containing them and their use in the treatment of reproductive disorders and affective conditions. Further, the compounds of the invention are antagonists of follicle stimulating hormone, a hormone associated with the human reproductive system.

Abstract: Substituted propane-1,3-diamine derivatives, methods for producing such derivatives, and medicaments and pharmaceutical compositions containing such derivatives useful for the treatment or prophylaxis of pain, urinary incontinence, itching, tinitus aurium, or diarrhea are provided.

Abstract: This invention discloses novel gamma secretase inhibitors of the formula: 1

Abstract: Oligomeric compounds and methods of making the compound having the formula: T—&Parenopenst;E—F&Parenclosest;i—&Parenopenst;E—F′&Parenclosest;j—&Parenopenst;E′—F&Parenclosest;k—&Parenopenst;E′—F′&Parenclosest;l—S  (II) wherein i, j, k, and l are integers from about 0 to 300 and the sum of i, j, k, and l is greater than 2, wherein the units F, F′ and T are derived from one or more multi-functional carbonyl compounds of general structure DO—CO—CRaRb—(—CRcRd—)n—NH—(Y)m—CO—OD  (IV) wherein n is an integer from 1 to 15, m is either 0 or 1; Ra, Rb, Rc, and Rd, are each a hydrogen or a hydrocarbyl group; Y is CO—(CReRf)p, wherein Re and Rf are each a hydrogen or hydrocarbyl group and p is zero or an integer from 1 to 20 or CO—C6H4—, wherein the substitution pattern on the phenylene group is an ortho, meta, or para substitution pattern, and

Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as aromatic sulfone hydroxamic acids) and salts thereof that, inter alia, tend to inhibit matrix metalloproteinase (also known as matrix metalloprotease or MMP) activity and/or aggrecanase activity. This invention also is directed to a treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP activity and/or aggrecanase activity.

Abstract: The present invention relates to 1-alkoxy-polyalkyl-piperidine derivatives containing a structural element of formula (I) wherein G1, G2, G3, G4 are independently C1-C6alkyl with the proviso that at least one is not methyl or G1 and G2 or G3 and G4, or G1 and G2 and G3 and G4 together form a C5-C12cycloalkyl group; G5, G6 independently are H, C1-C18alkyl, phenyl, naphthyl or a group COOC1-C18alkyl and X represents a group such that the free radical X. derived from X is capable of initiating polymerization of ethylenically unsaturated monomers, with the proviso that compounds A1 and A2 are excluded Further subjects of the invention are a polymerizable composition comprising a) at least one ethylenically unsaturated monomer and b) a 1-alkoxy-polyalkyl-piperidine derivative, a process for polymerizing ethylenically unsaturated monomers, and the use of 1-alkoxy-polyalkyl-piperidine derivatives for controlled polymerization.

Abstract: The present invention provides a compound of a formula (I): 1