Abstract: The invention provides a compound of formula (I): and its pharmaceutically acceptable salts, wherein R is halo C2-C8 alkenyl or halo C2-C8 alkynyl; R1 is hydrogen, halo or C1-C6 alkoxy; or R and R1, together with the two carbon atoms to which they are attached, form a C4-C6 cycloalkyl or a C4-C6 oxacycloalkyl ring wherein said ring may be optionally substituted by one or more substituents selected from the group consisting of halo, C1-C6 alkyl and halo C1-C6 alkyl; X is C1-C6 alkoxy, halo C1-C6 alkoxy, phenoxy or halo; and Ar is phenyl optionally substituted by halo. These compounds are useful in the treatment of a gastrointestinal disorder; a central nervous system (CNS) disorder; an inflammatory disease; emesis; urinary incontinence; pain; migraine; sunburn; diseases, disorders and adverse conditions caused by Heliobacter pylori; or angiogenesis especially CNS disorders in a mammalian subject, especially humans.

Abstract: The present invention relates to a novel process for the preparation of a diastereomeric mixture of piperidinylaminomethyl trifluoromethyl cyclic ether compounds of formulae Ia and Ib: and pharmaceutically acceptable salts thereof, wherein R1 is C1-C6 alkyl; R2 is C1-C6 alkyl, halo C1-C6 alkyl or phenyl or substituted phenyl; R3 is hydrogen or halo; m is zero, one or two, and wherein said mixture is highly enriched in the compound of formula Ia, and to novel processes for the preparation and purification of intermediate compounds useful in the preparation of compounds of formulae Ia and Ib.

Abstract: The present invention relates to compounds of the formula wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.

Abstract: This invention relates to the use of a compound of the formula wherein m, R1, R2, R3, R4, R5 and X are as defined in the disclosure, for treating or preventing migraine, depression and other disorders for which a 5-HT1 agonist or antagonist is indicated.

Abstract: The present invention relates to compounds of the formula I wherein R1, R2, R3, X, Y and the dashed line are as defined in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use as psychotherapeutic agents.

Abstract: A compound of the formula: or the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined above are useful as ORL1-receptor agonists, and useful as analgesics or the like in mammalian subjects.

Abstract: Compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are defined as in the specification, intermediates in the synthesis of such compounds. pharmaceutical compositions containing such compounds and methods of using such compounds, in the treatment of neurological and psychological disorders.

Abstract: The present invention relates to compounds of the formula wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.

Abstract: This invention relates to novel processes for preparing the pharmaceutically active compound 5-(3-[(2S)-exo-bicyclo[2.2.1]hept-2-yloxy]-4-methoxyphenyl)-3,4,5,6-tetrahydropyrimidin-2(1H)-one and its corresponding 2R enantiomer and for preparing certain intermediates used in the synthesis of these compounds. It also relates to novel intermediates used in the synthesis of such pharmaceutically active compounds and to other novel compounds that are related to such intermediates.

Abstract: The present invention provides intermediates for the preparation of compounds of the formula wherein R, R1, W, X, Y, Ar and ZA are defined herein.

Abstract: The present invention relates to compounds of the formula wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.

Abstract: The present invention relates to 2-aminopyridine derivatives of the formula I: or pharmaceutically acceptable salts thereof, wherein A and B are each independently H, or together, A and B form a ring fused to the phenyl ring, said ring being saturated or unsaturated and containing from 5 to 7 ring member atoms, where said ring member atoms may optionally comprise from 1 to 2 heteroatoms selected independently from the group consisting of N, O or S, provided that no two adjacent ring members are heteroatoms; X is oxygen or a single bond; Y is (C1-C6)alkyl; R1 is hydrogen, (C1-C6)alkyl or a (C1-C6 alkyl) group substituted with —NR2R3 wherein R2 and R3 are either selected independently from the group consisting of H, alkyl, aryl, aralkyl or tetrahydronaphthalene, wherein said aryl group or said aryl moiety of said aralkyl group is phenyl or naphthyl, said alkyl group or said alkyl moiety of said aralkyl group contains from one to six carbon atoms and is straight-chained or branched,

Abstract: The present invention is concerned with a crystalline, polymorphic form of a compound of formula (I) characterized by a powder X-ray diffraction pattern obtained using copper K-alpha1 radiation (&lgr;=0.15046 nm) which shows main peaks at 9.28, 10.38, 11.37, 12.40, 16.84, 17.46, 17.53, 17.78, 17.98, 19.48, 20.70, 21.29, 21.45, 22.21, 22.64, 23.08, 25.20 and 25.79. The invention also relates to processes for the preparation of said form, to pharmaceutical compositions containing same and to its use in medicine, particularly the treatment of conditions for which an agonist of 5-HT1 receptors is indicated, for example, migraine.

Abstract: The invention provides a substituted benzylaminopiperidine compounds that are useful in the treatment of gastrointestinal disorders; central nervous system (CNS) disorders; inflammatory disease; emesis; urinary incontinence; pain; migraine; sunburn; diseases, disorders and adverse conditions caused by Heliobacter pylori; or angiogenesis, especially CNS disorders in a mammalian subject, especially in humans.

Abstract: Compounds of the formula wherein R1 R2, R7, R8, X, Y, M and L are defined as below. The compounds of formula I are cholinesterase inhibitors and are useful in enhancing memory in patients suffering from dementia and Alzheimer's disease.

Abstract: A compound of the formula wherein m, R1, R2, R3, R4, R5 and X are as defined, useful in treating or preventing migraine, depression and other disorders for which a 5-HT1 agonist or antagonist is indicated.

Abstract: This invention relates to compounds of the formula and to pharmaceutically acceptable salts thereof. The compounds of formula 1 are potent antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1.

Abstract: Compounds of formula I are antagonists of Substance P and have activity against CNS and gastrointestinal disorders.

Abstract: The invention provides a process for the production of a compound of formula I, which comprises reacting a compound of formula II with a compound of formula III, in the presence of a strong base and a palladium(0) catalyst, at an elevated temperature, in a solvent which does not adversely affect the reaction. Compounds of formula I may be further processed to compounds of formula V, which are useful in the treatment of inter alia migraine.

Abstract: A compound of the formula or the pharmaceutically acceptable salt thereof, wherein Z is oxygen, S(O)m wherein m is 0, 1 or 2; or NQ wherein Q is hydrogen, (C1-C6)alkyl or phenyl; X is hydrogen, chloro, fluoro, bromo, iodo, hydroxy, nitro, cyano, (C1-C6)alkyl, trifluoromethyl, (C1-C6)alkoxy, (C1-C6)alkyl S(O)a wherein a is 0, 1 or 2; or phenyl wherein the phenyl group is optionally substituted; Y is wherein M is oxygen or sulfur; X2 is hydrogen, fluoro, chloro, trifluoromethyl, (C1-C6)alkyl, (C1-C6)alkoxy or (C1-C6)alkyl S(O)c wherein c is 0, 1 or 2; R1 is selected from wherein R6 is selected from the group consisting of hydrogen, optionally substituted (C1-C6)alkyl; and wherein R6 in G5 together with R7 form a 2 carbon chain; and R9 and R10 are independently hydrogen or (C1-C6)alkyl; R2 is hydrogen, (C1-C4)alkyl, phenyl or naphthyl, wherein said phenyl or naphthyl may optionally substituted; and R3 is —(CH2)tB, wherein t is 0-3 and B is hydrog