Abstract: A method for treating Tourette's syndrome, obsessive compulsive disorder, chronic motor or vocal tic disorder in a mammal, including a human, comprising administering to said mammal an effective amount of a compound of the formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein n, X, Y and Ar are as defined above.

Abstract: The present invention relates to diazabicyclic compounds and, specifically, to compounds of the formula ##STR1## wherein A, G, R.sup.1, R.sup.2, R.sup.3, R.sup.4.sub.1 R.sup.5, R.sup.6, and R.sup.7 are as defined in the specification. The compounds of formula I are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.

Abstract: The present invention relates to processes for the preparation of 3-(1-piperazinyl)-1,2-benzoisothiazole or its pharmaceutically acceptable salt and to novel intermediates used in the process.

Abstract: The invention provides compounds of formula (I), ##STR1## wherein R.sup.1 represents C.sub.1-4 alkoxy optionally substituted by one or more fluorine atoms; R.sup.2 represents H or C.sub.1-6 alkoxy optionally substituted by one or more fluorine atoms; R.sup.3 represents one or more groups independently selected from H, halogen, C.sub.1-4 alkoxy and CF.sub.3 ; in addition, R.sup.2 and one R.sup.3 group may together represent --OCH.sub.2 --, the methylene group being attached to the ortho-position of the pendant phenyl ring; R.sup.4 represents a 4-, 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent or represents a cyclic group or an open chain group; and pharmaceutically acceptable salts thereof.

Abstract: The compounds of the formula wherein A, R.sub.1, R.sub.3, X.sub.1, Y and Z are as defined herein, have corticotropin-releasing factor (CRF) antagonist activity. They are useful in the treatment of illnesses induced by CRF, such as stress and anxiety related disorders.

Abstract: The compounds of the formula wherein A, R.sub.1, R.sub.3, X.sub.1, Y and Z are as defined herein, have corticotropin-releasing factor (CRF) antagonist activity. They are useful in the treatment of illnesses induced by CRF, such as stress and anxiety related disorders.

Abstract: The present invention relates to a pro-drug of ziprasidone or pharmaceutically acceptable salts thereof, processes for its preparation, and pharmaceutical compositions and methods of treatment comprising said pro-drug.

Abstract: This invention relates to compounds of formula (IA), (IB), (IC) or (ID), wherein m, X, Z, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.14 and the dotted lines are as defined below, their pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of using them to treat Alzheimer's disease, age-associated memory impairment, Parkinson's disease and other central nervous system disorders. The claimed compounds have the ability to enhance the release of neurotransmitters such as acetylcholine, dopamine and serotonin.

Abstract: The present invention relates to diazabicyclic compounds and, specifically, to compounds of the formula ##STR1## wherein A, G, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are as defined in the specification. The compounds of formula I are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.

Abstract: The present invention is directed to compounds of formula (I), and the pharmaceutically acceptable acid addition salts thereof, wherein R is selected from the group consisting of F,--CF.sub.3, --OCH.sub.3, --O(C.sub.1)alkyl substituted with 1 to 3 fluoro atoms. --O(C.sub.2) substituted with 1 to 5 fluoro atoms, and --O(C.sub.3)alkyl substituted with 1 to 7 fluoro atoms. The compounds of formula (I) are useful in the treatment of stroke, traumatic brain injury and central nervous system degenerative diseases.

Abstract: Compounds of the formula: ##STR1## wherein: X is O, NH or NR.sup.1 ; R.sup.1 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.4)alkyl, aryl or aryl (C.sub.1 -C.sub.4)alkyl; wherein the C.sub.1 -C.sub.6 alkyl group is optionally substituted by fluorine and the C.sub.3 -C.sub.7 cycloalkyl or C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.4 )alkyl group is optionally substituted in the cycloalkyl ring by up to two substituents each independently selected from halo, C.sub.1 -C.sub.4 alkoxy or halo(C.sub.1 -C.sub.4)alkoxy; R.sup.2 is phenyl optionally substituted with one or two halo substituents, indolyl or thienyl; R.sup.3 is NH.sub.2, --NR.sup.4 SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --NR.sup.4 SO.sub.2 aryl, --NR.sup.4 CO(C.sub.1 -C.sub.6 alkyl), --NR.sup.4 CO aryl or a 5 to 7-membered N-linked cyclic group incorporating W in the ring wherein W is O, NR.sup.5, CH(OH), CHCO.sub.2 H, CHN(R.sup.4).sub.2, CHF, CF.sub.2, C.dbd.O or CH.sub.2 ; R.sup.4 is H or C.sub.1 -C.sub.

Abstract: Certain novel substituted quinuclidine compounds having the ability to antagonize substance P and having the following formula: ##STR1## wherein Ar.sup.1 and Ar.sup.2 are each, independently, thienyl, phenyl, fluorophenyl, chlorophenyl or bromophenyl;X is --CONR.sup.3 R.sup.4, --CO.sub.2 R.sup.3, --CH.sub.2 OR.sup.3, --CH.sub.2 NR.sup.3 R.sup.4 or --CONR.sup.3 OR.sup.4 ;R.sup.1, R.sup.3 and R.sup.4 are each, independently, hydrogen or alkyl having 1 to 4 carbon atoms;R.sup.

Abstract: This invention provides a compound of the formula: ##STR1## and its pharmaceutically acceptable salts, wherein R.sup.1 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, halo C.sub.1 -C.sub.6 alkyl or terahydropyranyl, having one or more substituents selected from cyano, 1,3-thiazolanyl, COOR.sup.2, COR.sup.2, OCOR.sup.2, CONR.sup.3 R.sup.4, NR.sup.3 R.sup.4, NR.sup.5 COR.sup.3 and C.ident.CR.sup.6, wherein R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sup.3 and R.sup.4 are independently hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.3 -C.sub.6 cycloalkyl, R.sup.5 is C.sub.1 -C.sub.4 alkyl or C.sub.3 -C.sub.6 cycloalkyl and R.sup.6 is hydrogen, halo, cyano, C.sub.1 -C.sub.6 alkyl, COOH, COO(C.sub.1 -C.sub.4 alkyl) or phenyl; X is C.sub.1 -C.sub.6 alkoxy or halo C.sub.1 -C.sub.6 alkoxy; and Ar is phenyl optionally substituted with halo.

Abstract: The present invention relates to a method treating or preventing disorders caused by a spiral urease-positive gram-negative bacterium such as Helicobacter pylori in mammals, including humans, using compounds that are substance P receptor antagonists and, specifically, using certain quinuclidine derivatives, piperidine derivatives, pyrrolidine derivatives, azanorbornane derivatives, ethylene diamine derivatives and related compounds.

Abstract: Compounds useful in the treatment of inflammatory disorders, central nervous system disorders and other disorders of the formula I and the pharmaceutically-acceptable salts thereof; ##STR1## wherein R is C.sub.1 -C.sub.6 alkyl; X is C.sub.1 -C.sub.6 alkyl having one or more substituents which include at least one heteroatom; Ar.sup.1 and Ar.sup.2 are each, independently, aryl optionally substituted by one C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, halogen, cyano, nitro, phenoxy, mono C.sub.1 -C.sub.6 alkylamino, di C.sub.1 -C.sub.6 alkylamino, halosubstituted C.sub.1 -C.sub.6 alkyl, or halosubstituted C.sub.1 -C.sub.6 alkoxy; Y is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, Z--(CH.sub.2).sub.p --, or W--(CH.sub.2).sub.m --CHR.sup.2 --(CH.sub.2).sub.n --NR.sup.1 CO-- wherein Y is at the 4-, 5- or 6-position on the quinuclidine ring; R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, benzyl or --(CH.sub.2).sub.r --W; R.sup.

Abstract: The present invention relates to novel substituted benzylamino nitrogen containing non-aromatic heterocycles and, specifically, to compounds of the formula ##STR1## wherein W, R.sup.1, R.sup.2, R.sup.3 and A are as defined in the specification, and to intermediates used in the synthesis of such compounds. The novel compounds of formula I are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.

Abstract: The compounds of the formula ##STR1## wherein A, R.sub.1, R.sub.3, Z and Y are as defined herein, have corticotropin-releasing factor (CRF) antagonist activity. They are useful in the treatment of illnesses induced by CRF, such as stress and anxiety related disorders.

Abstract: The present invention relates to the derivatives of the compound of formula (I), which are useful in the treatment of inflammatory and central nervous system disorders, as well as other diorders ##STR1##

Abstract: The present invention relates to compounds of the formula ##STR1## The present invention also relates to intermediates for the preparation of compounds of the formula I, pharmaceutical compositions and method of use.

Abstract: The present invention provides a novel culture which belongs to Actinoplanes (Actinoplanes sp. FERM BP-3832). This culture is capable of producing rapamycin more than ten times efficiently than the cultures which have been reported (e.g., Streptomyces hygroscopicus ATCC 29253). The present invention provides a process for the production of rapamycin which comprises cultivating Actinoplanes sp. FERM BP-3832 and thereafter isolating rapamycin from the fermentation mixture.