Abstract: The invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, n and m are as defined herein. The compounds of formula I are useful in the treatment of hyperproliferative diseases, such as cancer. The invention further relates to processes of making the compounds of formula I and to methods of using such compounds in the treatment of hyperproliferative diseases.

Abstract: 3R*4S*3-?4-(4-fluorophenyl)-4-hydroxy-piperidin-1-yl!-chroman-4,7-diol, its enantiomers and pharmaceutically acceptable salts are effective oral agents for treating diseases and conditions susceptible to treatment by NMDA blocking drugs.

Abstract: The instant invention is directed to compounds, compositions and antipsychotic methods of use wherein the compounds are of formula I: ##STR1## wherein Y is an imide or benzoyl alkyl group and X is a cycloalkyl, phenyl or dibenzoazepinyl group.

Abstract: Optically pure intermediates of formula (1) wherein the substituent B is either cis or trans to the C.sub.9a -C.sub.1 bond and is selected from the group consisting of --CH.sub.2 OH, --CHO, --CH.sub.2 OSO.sub.2 R, --CH.sub.2 CN, --CH(OH)CH.sub.2 NO.sub.2, --CH.dbd.CH--NO.sub.2, (2) and (3), C is selected from the group consisting of --H, (4), (5), and a nitrogen protecting group which is removable by hydrogenation or acid treatment; and wherein R is (C.sub.1 -C.sub.8) alkyl, phenyl or alkyl substituted phenyl; X is N or CH; Y is O or S and Z is H or Cl; for the synthesis of octahydro-1H-pyrido(1,2-a)pyrazinyl ethyl carboxamide anxiolytic agents.

Abstract: A method of treating tinnitus in a mammal in need of such treatment, in which the method comprises administering a therapeutically effective amount of a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 -R.sup.6 are as defined herein.

Abstract: The invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts thereof, wherein A, W, P, R.sup.3, Q and R.sup.1 are as defined herein. The compounds of formula I, and pharmaceutically acceptable salts thereof, are substance P antagonists and as such are useful in the treament of various inflammatory and central nervous system disorders.

Abstract: The invention relates to compounds of the formula I ##STR1## and to pharmaceutically acceptable salts thereof, wherein Z, A, Y, X.sub.1, R.sub.1, R.sub.2, and R.sub.3 are as defined herein. The invention further relates to pharmaceutical compositions containing, and to methods of using, the compounds of formula I in the treatment of those disorders that can be treated with compounds having corticotropin-releasing factor antagonistic activity. Such disorders include various stress-related conditions, such as anxiety.

Abstract: Certain novel heteroaryl cycloalkenyl hydroxyurea compounds having the ability to inhibit the 5-lipoxygenase enzyme and having formula (I) and the pharmaceutically acceptable salts thereof, wherein each R.sup.1, independently, is hydrogen, hydroxy, chloro, fluoro, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkyl or C.sub.1 -C.sub.4 haloalkoxy; R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.3 is hydrogen, chloro, fluoro or C.sub.1 -C.sub.4 alkyl; X is O, S, SO or SO.sub.2 ; Z is methylene or ethylene; A is divalent radical derived from furan, thiophene, pyridine, benzofuran, benzothiophene or quinoline, or one of these groups having one substituent selected from chloro, fluoro, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkyl and C.sub.1 -C.sub.4 haloalkoxy; n is 1, 2 or 3; and M is hydrogen or a pharmaceutically acceptable cation.

Abstract: Compounds of the formula ##STR1## wherein B, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined herein with reference to formula IX have corticotropin-releasing factor antagonist activity and as such are of use in the treatment of panics, phobias and other stress-related disorders.

Abstract: Racemic or optically active pyrido[1,2-a]pyrazine derivatives of the formula ##STR1## wherein X is N or CH and Y represents one of certain pyrazolo, triazolo, tetrazolo or cyclic imido radicals are useful in the treatment of abuse of and/or addiction to such substances as narcotics, alcohol and nicotine.

Abstract: The invention provides antifungal compounds of the formula: ##STR1## and pharmaceutical salts thereof, whereinR is phenyl substituted by 1 to 3 substituents each independently selected from halo, --CF.sub.3 and --OCF.sub.3 ;R.sup.1 is C.sub.1 -C.sub.4 alkyl;R.sup.2 is H or C.sub.1 -C.sub.4 alkyl;X is CH or N; andY is F or Cl.

Abstract: Certain novel isoxazoline compounds having the ability to inhibit the 5-lipoxygenase enzyme and having formula (I), ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.4 alkyl or --NR.sub.3 R.sub.4 ; R.sub.3 and R.sub.4 are each independently H or C.sub.1 -C.sub.4 alkyl; M is H or a pharmaceutically acceptable cation; A is C.sub.1 -C.sub.6 alkylene, C.sub.2 -C.sub.6 alkenylene or C.sub.2 -C.sub.6 alkynylene; Ar is phenylene or mono-, di- or tri-substituted phenylene wherein the substituents are each independently selected from halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy; n is an integer of 0 or 1; Y is H or C.sub.1 -C.sub.4 alkyl; R.sub.2 is C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.4 arylalkyl or C.sub.2 -C.sub.4 arylalkenyl; and said aryl and each aryl moiety in said arylalkyl and arylalkenyl may be substituted by from one to three substituents independently selected from halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halosubstituted C.sub.1 -C.sub.4 alkyl, halosubstituted C.sub.1 -C.sub.

Abstract: The invention provides antifungal compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein R is phenyl substituted by up to 3 substituents each independently selected from halo and trifluoromethyl;R.sup.1 is C.sub.1 -C.sub.4 alkyl;R.sup.2 is ##STR2## R.sup.3 is --S(O).sub.m R.sup.4 ; R.sup.4 is C.sub.1 -C.sub.4 alkyl; andm is 0, 1 or 2, together with pharmaceutical compositions containing, and processes and intermediates for preparing, said compounds.

Abstract: 1S,4S and 1R,4R-2-Alkyl-2,5-diazabicyclo[2.2.1]-heptanes useful as intermediates in the synthesis of certain antibacterial quinolones, are prepared respectively, from trans-4-hydroxy-L-proline and trans-4-hydroxy-D-proline via multistep procedures.

Abstract: Compounds of the formula ##STR1## wherein A is C1 to C3 alkylene, Ar is phenyl or styryl, R is halosubstituted C1 to C3 alkyl, NHR' or ##STR2## R' is hydrogen or C2 to C8 alkytthioalkyl, n is an integer of from 1 to 4 and p is an integer of from 2 to 5, with the proviso that when R' is hydrogen then Ar is styryl, and the pharmaceutically acceptable salts thereof, inhibit the enzyme lipoxygenase and are useful in treating allergy and inflammatory and cardiovascular conditions for which the action of lipoxygenase has been implicated. These compounds form the active ingredient in pharmaceutical compositions for treating such conditions.

Abstract: Compounds of the formula ##STR1## wherein n is 1 to 5 and R is hydrogen, C.sub.1 to C.sub.4 alkyl, arylalkyl having from one to four carbon atoms in the alkyl moiety or arylalkyl substituted with one or more substituents selected independently from the group consisting of halogen, nitro, cyano, C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy, C.sub.1 to C.sub.6 halosubstituted alkyl, C.sub.1 to C.sub.6 hydroxysubstituted alkyl, C.sub.2 to C.sub.7 alkoxycarbonyl and aminocarbonyl, and the pharmaceutically acceptable salts thereof, inhibit the enzyme lipoxygenase and are useful in treating allergy and inflammatory and cardiovascular conditions for which the action of lipoxygenase has been implicated. These compounds form the active ingredient in pharmaceutical compositions for treating such conditions.

Abstract: 1S,4S and 1R,4R-2-Alkyl-2,5-diazabicyclo[2.2.1]heptanes useful as intermediates in the synthesis of certain antibacterial quinolones, are prepared respectively, from trans-4-hydroxy-L-proline and trans-4-hydroxy-D-proline via multistep procedures.

Abstract: (C.sub.1 -C.sub.3)Alkyl-4,6,7,8,9,9a-hexahydro-2H,3H-pyrido[1,2-a]pyrazin-1-one-7-c arboxylate esters, important precursors to certain bis-aza-bicyclic anxiolytics, can be prepared from di(C.sub.1 -C.sub.3)alkyl cis-piperidine-2,5-dicarboxylate starting material by a new process via a new class of intermediates, di(C.sub.1 -C.sub.3)alkyl cis-N-(2-(phthalimido)ethyl)piperidine-2,5-dicarboxylates. In the process, the starting material is reacted with either 2-(phthalimido)ethyl triflate or 2-(phthalimido)acetaldehyde to form the new intermediate, which can then be cyclized to the aforementioned precursor.