Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl]piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.

Abstract: There are described compounds having the general formula (I) below and their pharmaceutically acceptable salts thereof, wherein E, X, m, q, R1, R2, n and ZBG have the meanings reported in the description useful, in therapy, as inhibitors of zinc metalloproteinases.

Abstract: The present invention relates to a chemical genus of biaryl substituted nitrogen-attached heterocycles that are inhibitors of LTA4H (leukotriene A4 hydrolase). The compounds have the general formula: They are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.

Abstract: Compounds having the formula are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

Abstract: N-substituted azacycle derivative compounds represented by formula (I): wherein m, q, r, t and u are independently selected from 0 or 1; and p is 0, 1, 2, or 3; and A, B, D, X, Y, R, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are fully described herein. The compounds being particularly useful in compositions comprising an insecticidally effective amount of at least one compound of formula I, and an insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.

Abstract: The present invention relates to a chemical genus of biaryl substituted nitrogen-attached heterocycles that are inhibitors of LTA4H (leukotriene A4 hydrolase). The compounds have the general formula: They are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.

Abstract: The present invention relates to a method for preparing a syn-form piperidine compound represented by general formula [I]: wherein, bold lines represent bonds in which substituents at positions 2 and 4 of a piperidine ring are in the syn configuration, and the other symbols have the same meaning as defined below, or a salt thereof, comprising: reducing a compound represented by general formula [II]: wherein, ring A represents an optionally substituted benzene ring, R2 represents a hydrogen atom, an optionally substituted hydroxyl group, an optionally substituted amino group, an optionally substituted alkyl group, a substituted carbonyl group or a halogen atom, and M represents an alkaline metal or hydrogen atom.

Abstract: This invention provides compounds of formula I: wherein a, b, c, m, p, r, R1, R2, R3, R4, R5, R6, W and X1 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 discloses processes for preparing piperidine derivative compounds of the formula: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.

Abstract: This invention provides compounds of formula I: wherein a, b, c, m, p, r, R1, R2, R3, R4, R5, R6, W and X1 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: A compound represented by the following general formula (1) or (100), a salt thereof or a hydrate of the foregoing has excellent cell adhesion inhibitory action and cell infiltration inhibitory action. wherein R10 represents 5- to 10-membered cycloalkyl etc. optionally substituted with hydroxyl etc., R30, R31 and R32 may be the same or different and each represents hydrogen etc., R40 represents C1-10 alkyl etc. optionally substituted with hydroxyl etc., n represents an integer of 0, 1 or 2, X1 represents CH or nitrogen, and R20, R21, R22 and R23 may be the same or different and each represents hydrogen etc.

Abstract: This invention relates to novel alkyl substituted piperidine derivatives useful as monoamine neurotransmitter re-up-take inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

Abstract: Processes are disclosed for preparing piperidine derivative compounds of the formulae I, II or III:

Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

Abstract: This invention relates to compounds of formula I: wherein R1 and R2 are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions and combinations comprising such compounds, processes and intermediates for preparing such compounds, and methods of using such compound to, for example, treat pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.

Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.

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

Abstract: The invention provides compounds of formula I: wherein a, b, c, d, f, W, Q, Y, R1, R2, and R3 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: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof are disclosed herein. Details are provided herein. Compositions, methods, and medicaments related thereto are also disclosed.

Abstract: Novel substituted piperidines of the general formulae (I) and (II) with the substituent definitions as explained in detail in the description are described. The compounds are suitable in particular as renin inhibitors and are highly potent.

Abstract: The present invention relates to new D3 dopamine receptor subtype selectice ligands of formula (I) to pharmacological compositions containing the same and to their use in therapy and/or prevention of psychoses (e.g. schizophrenia, schizo-affective disorders, etc), drug (e.g. alcohol, cocaine and nicotine, opioids etc.) abuse, cognitive impairment accompanying schizophrenia, mild-to-moderate cognitive deficits, amnesia, eating disorders (e.g. bulimia nervosa, etc.), attention deficit disorders, hyperactivity disorders in children, psychotic depression, mania, paranoid and delusional disorders, dyskinetic disorders (e.g. Parkinson's diseases, neuroleptic induced Parkinson's dissases, tardive dyskinesias) anxiety, sexual dysfunction, sleep disorders, emesis, aggression, autism, pain ophthalmological diseases (e.g. glaucoma etc.).

Abstract: Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration.

Abstract: This invention provides compounds of formula I: wherein a, b, c, m, p, s, t, W, Ar1, X1, R1, R2, R3, R4, R6, and R7 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: This invention provides cyclicamino-phenyl sulfamate derivatives represented by a formula wherein each of R1 and R2 stands for hydrogen or lower alkyl; each of R3 and R4 stands for hydrogen, halogen, cyano or the like; A stands for nitrogen or CH; B stands for CH2, SO2, CO, optionally substituted phenyl or the like; and R5 stands for alkyl, phenyl, amino or the like, or salts thereof which exhibit excellent steroid sulfatase inhibitory activity and are useful for prevention or treatment of diseases associated with steroids such as estrogen, androgen and the like.

Abstract: Compounds of Formula I wherein R1, D, R2, A and R3 are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.

Abstract: The invention relates to a compound of formula (I): Wherein m, n, X, Y, R1, R2, R3 and R4 are as defined herein. The invention also relates to the use of same in therapeutics.

Abstract: The present invention relates to compounds of formula (I) wherein R1 is as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP-IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.

Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl] piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.

Abstract: An amine ether of formula A wherein a is 1 or 2; and when a is 1, E is E?; when a is 2, E is L; E? is C1-C36 alkyl; C3-C18 alkenyl; C2-C18 alkinyl; C5-C18 cycloalkyl; C5-C18 cycloalkenyl; a radical of a saturated or unsaturated aliphatic bicyclic or tricyclic hydrocarbon of 7 to 12 carbon atoms; C2-C7alkyl or C3-C7alkenyl substituted by halogen; C7-C15 aralkyl or C7-C15 aralkyl substituted by C1-C4 alkyl or phenyl; or E? is a radical of formula (VII) as explained in claim 1; T? is tertiary C4-C18alkyl or phenyl, each of which are unsubstituted or substituted by halogen, OH, COOR21 or C(O)—R22; or T? is C5-C12cycloalkyl; C5-C12cycloalkyl which is interrupted by at least one O or —NR18—; a polycyclic alkyl radical having 7-18 carbon atoms, or the same radical which is interrupted by at least one O or —NR18—; or T? is —C(G1)(G2)-T?; or C1-C18alkyl or C5-C12cycloalkyl substituted by T? is hydrogen, halogen, NO2, cyano, or is a monovalent organic radical comprising 1-50 carbon atoms; or T? and T?

Abstract: The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis.

Abstract: The present invention relates to stable S-nitrosothiols derivatives of formula (I) having vasodilating effect and which inhibit the aggregation of the platelets and which therefore are useful for the preparation of medicaments for treatment of NO related diseases. The invention also relates to a process for the synthesis of the compounds of formula (I).

Abstract: Sterically hindered N-hydrocarbyloxyamines are prepared from hindered amine N-oxyl compounds by a process which uses hydrogen peroxide or a hydrogen peroxide equivalent, a catalytic amount of a peroxide decomposing transition metal salt, metal oxide, or metal-ligand complex, a hydrocarbon solvent containing no activated hydrogen atoms, and a relatively inert cosolvent. These compounds are useful as thermal and light stabilizers for a variety of organic substrates.

Abstract: The present invention is directed to certain piperidine compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

Abstract: The object of the present invention is to provide a compound useful for the prevention and treatment of viral infectious diseases, and particularly liver diseases caused by HCV infection due to its having a high degree of replication inhibitory activity against HCV, its production method, an intermediate compound useful for its production and a pharmaceutical composition containing these compounds, and the present invention relates to a compound represented by the formula (I): (wherein A represents —(CH2)n—, etc.; B represents —(C?O)—, etc.; D represents —(CH2)m—R?, etc.; E represents a hydrogen atom, etc.; G represents —(CH2)p-J, etc.; bond Q represents a single bond or double bond; and R1, R2 and R3 may be the same or different and each represent a hydrogen atom, etc.), a prodrug thereof or a pharmaceutically acceptable salt thereof.

Abstract: The present invention is directed to 2,6-disubstituted piperidine and piperazine analogs having the following general formula: which are used to treat diseases of the central nervous system, drug abuse, and withdrawal therefrom as well as treating eating disorders.

Abstract: The present invention provides a method of treating inflammatory bowel disease which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a piperidinyl prostaglandin E analog.

Abstract: Cosmetic or dermatological compositions which comprise at least one piperidinium salt, preferably a 4-[(2-cyclopentyl-2-hydroxyphenylacetyl)oxy]-1,1-dimethyl-piperidinium salt, and the use thereof, particularly as antiperspirants. This Abstract is neither intended to define the invention disclosed in this specification nor intended to limit the scope of the invention in any way.

Abstract: The invention provides compounds of formula (I): as modulators of chemokine and H1 receptor activity. The compounds are especially useful in the treatment of asthma and rhinitis.

Abstract: A compound of Formula I are provided: wherein R is: R1 is a substituted or unsubstituted alkyl group; W1-4 are independently selected from hydrogen, substituted or unsubstituted alkyl groups, substituted or unsubstituted haloalkyl groups, substituted or unsubstituted alkanoyl groups, substituted or unsubstituted aroyl groups, or substituted or unsubstituted haloalkanoyl groups; X1-5 are independently selected from H, NO2, N3, and NH2;Y is absent or is a substituted or unsubstituted C1-alkyl group, other than carbonyl; Z is selected from a bond or NH, provided that when Z is a bond, Y is absent, and provided that when Z is NH, Y is a substituted or unsubstituted C1-alkyl group, other than carbonyl. Also provided are D-arabinitol compounds, methods for preparing such compounds and compositions of such compounds, and methods of using such compounds.

Abstract: One aspect of the present invention relates to a method of treating of drug addiction or drug dependence in a mammal, comprising the step of administering to a mammal in need thereof a therapuetically effective amount of a heterocyclic compound, e.g., a 3-substituted piperidine. In a preferred embodiment, the method of the present invention treats cocaine addiction or methamphetamine addiction.

Abstract: This invention relates to compounds of formula I: wherein R1 and R2 are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions and combinations comprising such compounds, processes and intermediates for preparing such compounds, and methods of using such compound to, for example, treat pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.

Abstract: The invention provides compounds of the Formula: wherein m, n, A, X, Y, Z, R1, R2, R4, R6, R7, R8, R9 and R10 are as defined herein, and pharmaceutically acceptable salts, solvates, prodrugs, single isomers or racemic or non-racemic mixture of isomers thereof. The invention also provides methods for preparing, compositions comprising, and methods for using compounds of formula I.

Abstract: The invention provides compounds of formula (I) wherein: T is C(O) or S(O)2; W is C(O) or S(O)2; X is CH2, O or NH; Y is CR11 or N; n is 0, 1 or 2; m is 1 or, when Y is CR11 m is 0; R1 is optionally substituted aryl or optionally substituted heterocyclyl; R2, R3, R,4, R5, R6, R7 and R8 are, independently, hydrogen or C?1-6#191 alkyl; R9 is hydrogen or C1-C6 alkyl; R10 is alkyl, optionally substituted aryl, optionally substituted aralkyl or optionally substituted heterocyclyl; and R11 is hydrogen or C1-C6 allkyl; that are modulators of chemokine (especially CCR3) activity and are especially useful for treating asthma and/or rhinitis.

Abstract: The present invention relates to a chemical genus of biaryl substituted nitrogen-attached heterocycles that are inhibitors of LTA4H (leukotriene A4 hydrolase). The compounds have the general formula: They are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.

Abstract: Compounds of Formula 1 [Region ?]?[Region ?]?[Region ?]?[Region ?] ??(I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds.

Abstract: A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof [wherein R1 represents a substituted morpholino group, a substituted piperidino group, a piperazin-1-yl group, a substituted piperazin-1-yl group, a thiomorpholin-1-yl group, a perhydroazepin-1-yl group, a perhydroazocin-1-yl group, a tetrahydropyridin-1-yl group, a pyrrolin-1-yl group, etc.; X represents a nitrogen atom or a group represented by CR5; and R2 to R5 are the same or different and each represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, a trifluoromethyl group or a halogen atom.] There is provided a drug which inhibits an enzyme producing 20-HETE participating in a contracting or dilating action for microvessels and an inducing action for cell proliferation in main organs such as kidney and cerebrovascular vessels.

Abstract: Disclosed are N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. In Formula (I), R1, R2, R3, R4, R3?, R10 and R11 are as described herein. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders using compounds of Formula (I).

Abstract: A compound of the formula wherein R1, R2 and R3 are as defined above, useful as inhibitors of protein kinases, such as the enzyme Janus Kinase 3.

Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein X, Y, Z, D and R3 are as defined in the specification. Also disclosed are compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof; wherein A, X, J, and R3 are as defined in the specification. Also disclosed are compounds having an ? and an ? chain comprising or derivatives thereof, as defined in the specification or pharmaceutically acceptable salts or prodrugs thereof.

Abstract: The present invention relates to alanine 2,6-dialkoxyphenyl ester derivatives having the general formula I The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these alanine 2,6-dialkoxyphenyl ester derivatives as hypnotics for the induction and maintenance of general anaesthesia.