Abstract: Disclosed are compounds of Formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, methods for inhibiting tumor necrosis factor-.alpha. and methods for treating septic shock, inflammation, or allergic disease.

Abstract: Derivatives of benzo[5,6]cyclohepta pyridine, and pharmaceutically acceptable salts and solvates thereof are disclosed, which possess anti-allergic and anti-inflammatory activity. Methods for preparing and using the compounds are also described.

Abstract: Bis-benzo or benzopyrido piperidene, piperidylidene and piperazine compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof are disclosed, wherein Z represents --(C(R.sup.a).sub.2).sub.m --Y--(C(R.sup.a).sub.2).sub.n -- or ##STR2## The compounds of Formula I possess anti-allergic and anti-inflammatory activity. Methods for preparing and using the compounds are also described.

Abstract: Novel heterocyclic compound of the general formula: ##STR1## wherein ring A and ring B each means a benzene ring which is substituted or unsubstituted; X means a group of the formula: ##STR2## wherein R.sup.2 is hydrogen an alkyl or an alkoxy; m is 0 or 1, the formula: ##STR3## wherein R.sup.3 is hydrogen or an alkyl, or the formula: --O--CO--; Y means a bond, --NH--, an C.sub.1 or 2 alkylene group or --CH.dbd.CH--; R.sup.1 means a hydrocarbon group which is substituted or unsubstituted; and n means a whole number of 3 through 6, or a salt thereof, having excellent acyl-CoA:cholesterol acyltransferase inhibitory activity, and a method for preparing it and its use.

Abstract: The present invention relates to 8-chloro-11-[1-[(5-methyl-3-pyridyl)methyl]-4-piperidyliden]-6,11-dihydro- 5H-benzo[5,6]cyclohepta[1,2-b]pyridine, to a process for its preparation and to pharmaceutical compositions containing it. This compound is a dual PAF antagonist and antihistamine.

Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; X is alkyl of 3-18 carbon atoms, cycloalkyl of 3-7 carbon atoms or cycloalkylloweralkyl; R is hydrogen, loweralkyl or loweralkylcarbonyl; R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl or oxygen-bridged diarylloweralkyl; stereo isomers thereof and pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory, methods for synthesizing them, and pharmaceutical compositions comprising an effective memory enhancing amount of such a compound.

Abstract: 1-Hetero substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.

Abstract: The present invention encompasses compounds of the formula: ##STR1## and pharmaceutically acceptable non-toxic salts thereof wherein: A represents nitrogen or C--H, andB represents nitrogen or C--H, with the proviso that when A is nitrogen, B is C--H, and when B is nitrogen, A is C--H;n is 0, 1, or 2;Y represents nitrogen or carbon, each of which is substituted with various organic or inorganic substituents;W represents an aromatic group unsubstituted or substituted with various organic or inorganic substituents; andR1 and R2 are the same or different and represent hydrogen or lower alkyl.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.

Abstract: Compounds of formula (1), wherein X is CH or N; Z is CH.dbd.CH or S; A is CH.sub.2 CH.sub.2, CH.dbd.CH, CH(OH)CH.sub.2, or COCH.sub.2 ; B is a direct link or --CH.sub.2 --, --CH(CH.sub.3)-- or --C(CH.sub.3).sub.2 --; or when Z is CH.dbd.CH, B may form a cyclopentane ring fused to the attached benzene ring; Y completes a fused benzo or thienyl ring which is optionally substituted by halo or C.sub.1 -C.sub.4 alkyl; n is 0, 1 or 2; and m is 0 or 1; are antagonists of both PAF and histamine H.sub.1 having utility in the treatment of allergic inflammatory conditions such as allergic rhinitis.

Abstract: Described are a class of chemiluminescent compound characterized by the presence an aryl ester, thioester or amide of a carboxylic acid substituted heterocyclic ring that is susceptible to chemical attack (such as by oxidic attack) to dissociate the heterocyclic ring to a transient compound. The heterocyclic ring is ring carbon-bonded to the carbonyl of the ester, thioester and amide moiety and possesses a heteroatom in an oxidation state that allows chemiluminescence by dissociating a compound ("intermediate") that decays to produce chemiluminescence, at the carbon bonded to the carbonyl. The aryl ring or ring system is ring carbon-bonded to the oxygen, sulfur or nitrogen of the ester, thioester or amide, as the case may be, and contains at least three substituents on a six-member ring. The substitution on the six-member ring comprises three or more groups acting in concert to sterically and electronically hinder hydrolysis of the ester, thioester or amide linkage.

Abstract: A chemiluminescent label compound and conjugate containing the same, in which the compound involves a fused ring system comprising a(i) hetercyclic ring as a fused member thereof in which the heterocyclic ring contains(a) one or more nitrogen heteroatoms in the ring;(b) at least one saturated or unsaturated ring in fused state with the heterocyclic ring;(c) an available carbon atom in the heterocyclic ring that is adjacent to a carbon forming a fused ring with the heterocyclic ring; and(d) at least one substituent that is peri relative said available carbon of the heterocyclic ring, which substituent serves to enhance the hydrolytic stability of the chemiluminescent label compound; and(ii) a leaving group coupled to the heterocyclic ring through a carbon adjacent to a fused ring carbon such that the leaving group and heterocyclic ring join to form a difunctional carboxy-containing linkage in which the carboxy carbon is directly bonded to the carbon of the heterocyclic ring adjacent to a fused ring carbon,(a)

Abstract: A novel chemiluminescent labeling compositions comprising an ester, thiolester or amide covalently and jointly bonded to (1) a carbon of a heterocyclic ring or ring system that is susceptible to attack by peroxide or molecular oxygen and (2) an aryl ring or ring system wherein the heterocyclic ring or ring system is distinguished by a heteroatom thereof in an oxidation state which causes the attacked carbon atom to form an intermediate that decays and produces chemiluminescence; the aryl ring or ring system contains at least three substituents on a six-member aromatic hydrocarbon that together sterically and electronically hinder hydrolysis of the linkage, which substituents involve ortho substituent groups on the aryl in conjunction with --NO.sub.2 meta or para substituents thereon.

Abstract: A novel chemiluminescent labeling compositions comprising an ester, thioester or amide covalently and jointly bonded to (1) a carbon of a heterocyclic ring or ring system that is susceptible to attack by peroxide or molecular oxygen and (2) an aryl ring or ring system wherein the heterocyclic ring or ring system is distinguished by a heteroatom thereof in an oxidation state which causes the attacked carbon atom to form an intermediate that decays and produces chemiluminescence; the aryl ring or ring system contains at least three substituents on a six-member aromatic hydrocarbon that together sterically and electronically hinder hydrolysis of the linkage, which substituents involve ortho substituent groups on the aryl in conjunction with meta and/or para substituents thereon that possess an electron withdrawing capacity characterized as a .sigma..sub.p value greater than 0 and less than 1.

Abstract: A chemiluminescent labeling composition comprising an ester, thioester or amide covalently and jointly bonded to (1) a carbon of a heterocyclic ring or ring system that is susceptible to attack by peroxide or molecular oxygen and (2) an aryl ring or ring system wherein the heterocyclic ring or ring system is distinquished by a heteroatom thereof in an oxidation state which causes the attacked carbon atom to form an intermediate that decays and produces chemiluminescence; the aryl ring or ring system contains at least three substituents on a six-member aromatic hydrocarbon that together sterically and electronically hinder hydrolysis of the linkage, which substituents involve ortho substituent groups on the aryl in conjunction with meta and/or para --SO.sub.2 -- substituents thereon.

Abstract: A chemiluminescent compound possessing an aryl ester, thioester or amide of a carboxylic acid substituted heterocyclic ring or ring system that is susceptible to chemical attack to dissociate the heterocyclic ring to a transient compound. The heterocyclic ring is ring carbon-bonded to the carbonyl of the ester, thioester or amide moiety and possesses a heteroatom in an oxidation state that allows chemiluminescence by dissociating a compound at the carbon bonded to the carbonyl that decays to produce chemiluminescence. The heterocyclic ring or ring sustem contains bonded to it through an organic moiety, a functional group that is functionally reactive with an active hydrogen containing compound. The aryl ring is a ring or ring system that is ring carbon-bonded to the oxygen, sulfur or nitrogen of the ester, thioester or amide, as the case may be, and contains substituents on a six-member ring that act to sterically and electronically hinder hydrolysis of the ester, thioester or amide linkage.

Abstract: A novel chemiluminescent labeling compositions comprising an ester or thiolester covalently and jointly bonded to (1) a carbon of a heterocyclic ring or ring system that is susceptible to attack by peroxide or molecular oxygen and (2) an aryl ring or ring system wherein the heterocyclic ring or ring system is distinquished by a heteroatom thereof in an oxidation state which causes the attacked carbon atom to form an intermediate that decays and produces chemiluminescence; the aryl ring or ring system contains at least three substituents on a six-member aromatic hydrocarbon that together sterically and electronically hinder hydrolysis of the linkage, which substituents involve ortho substituent groups on the aryl in conjunction with quaternary ammonium meta or para substituents thereon.

Abstract: This invention relates to compounds useful in treating HT.sub.4 and/or HT.sub.3 mediated conditions of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, alkoxy, halogen, amino, monoalkylamino, dialkylamino, acylamino and alkylsulfonylamino; R.sub.3 is selected from the group consisting of H, alkyl and cycloalkyl; X is NH or O; Z is selected from the group consisting of ##STR2## n and r are independently 1 or 2; p is 0 or 1; pharmaceutical compositions containing the compounds and a method for treating serotonin mediated condition with the compositions which act as 5-HT.sub.4 agonists or antagonists and/or 5-HT.sub.3 antagonists.

Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

Abstract: Novel heterocyclic compound of the general formula: ##STR1## wherein ring A and ring B each means a benzene ring which is substituted or unsubstituted; X means a group of the formula: ##STR2## wherein R.sup.2 is hydrogen, an alkyl or an alkoxy; m is 0 or 1, the formula: ##STR3## wherein R.sup.3 is hydrogen or an alkyl, or the formula: --O--CO--; Y means a bond, --NH--, an C.sub.1 or 2 alkylene group or --CH.dbd.CH--; R.sup.1 means a hydrocarbon group which is substituted or unsubstituted; and n means a whole number of 3 through 6, or a salt thereof, having excellent acyl-CoA:cholesterol acyltransferase inhibitory activity, and a method for preparing it and its use.

Abstract: A class of 2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-c]pyridine and 2,3,4,4a,5,6,7,11b-octahydro-1H-benzo[3,4]cyclohepta[1,2-c]pyridine derivatives are selective ligands at sigma recognition sites and are therefore useful in the treatment and/or prevention of psychiatric and/or gastrointestinal disorders.

Abstract: A piperidine compound of the formula (I): ##STR1## wherein A is a fused aromatic ring; R is hydrogen, chloro or methoxy; X is (CH.sub.2).sub.n, which may be substituted, in which n is 0 or an integer of 1 to 10, --CH.dbd.CH--, --C.dbd.C--, --O--, --S--, --NH--, --N(COCH.sub.3)--, --N(COOC.sub.2 H.sub.5)--, --N(CHO)--, --N(CH.sub.3)--, --CO--, --SO--, or --SO.sub.2 --; Y is --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, --CH.sub.2 CO--, --O--, --S--, --NH--, --OCH.sub.2 --, --SCH.sub.2 --, --NHCH.sub.2 --, --CH(OH)CH.sub.2 -- or --CH(OH)CH(OH)--; and Q is substituted or unsubstituted n-hexyl, carboxypropyl, ethoxycarbonylpropyl, cyanopropyl, cyclohexyl, phenyl, indanyl, naphthyl, tetrahydronaphthyl, benzocycloheptyl, piperidinyl, tetrahydroisoquinolinyl, indolyl, pyrolyl, furyl, thienyl, thiazolyl, oxazolyl or N-methylpyrolyl, wherein any one or more of the --(CH.sub.2)-groups of the hexyl, carboxypropyl, ethoxycarbonylpropyl and cyanopropyl groups may be replaced by --CH.dbd.CH--, --C.dbd.

Abstract: The synthesis of enamines in aqueous media and a process for the preparation of memory enhancing 9-amino-1,2,3,4-tetrahydracridines are described.

Abstract: Quinoline derivatives of the formula, ##STR1## wherein >A represents a group >N--(CH.sub.2).sub.n --, >C.dbd., >C.dbd.CH(CH.sub.2).sub.n --, or >CH(CH.sub.2).sub.n --, wherein n is an integer of 0-7; Y represents a group >C.dbd.O or >CHOH, R.sup.1 is a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, or an alkylthio group, R.sup.2 is a hydrogen atom, a halogen atom, an alkyl group, a hydroxy group, an alkoxy group, a phenyl group which may have a substituent, a phenoxy group, an alkanoyloxy group, or an amino group which may have a substituent, R.sup.3 is a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group, and m is an integer of 1-3. The compounds and their salts exhibit a superior anti-acetylcholinesterase activity with no side effects and are effective for the prevention or cure of senile dementia or memory disturbance.

Abstract: Novel substituted 2-azabicyclo[2.2.2]octane derivatives, pharmaceutical compositions containing them, methods for treating central nervous system disorders utilizing them, and processes for synthesizing them.

Abstract: Benzo[5,6]cyclohepta[1,2-b]pyridine derivatives of the following formula: ##STR1## wherein R.sup.1 represents a cyano, carbamoyl, alkylsulfoxy, alkylsulfonyl, tetrazolyl or sulfonic acid group, and R.sup.2 represents a hydrogen atom, a cyano, phenyl, aralkyl, alkoxycarbonylalkyl, aminoalkylcarbamoylalkyl or lower alkyl group, or a group ##STR2## or --X--R.sub.4, X being an oxygen or sulfur atom, R.sup.3 standing for a hydrogen atom or a substituted or unsubstituted lower alkyl, phenyl or aralkyl group, and R.sup.4 being a substituted or unsubstituted lower alkyl, phenyl or aralkyl group or an aminoalkyl group, and salts thereof. Antiallergic and antihistamic agents containing one of the above derivatives or salts as an active ingredient are also described.

Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; R is hydrogen, loweralkyl or loweralkylcarbonyl; R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl, or oxygen-bridged diaryllowerallyl; A is a direct bond or (CHR.sub.3).sub.m, m being 1-3; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.4 or --NR.sub.5 R.sub.6, R.sub.4 being hydrogen or loweralkyl, and R.sub.5 and R.sub.6 being independently hydrogen, loweralkyl or cycloalkyl; Y is O, S or NR.sub.7 ; and each R.sub.2, each R.sub.3 and R.sub.

Abstract: Compounds selected from the group consisting of 9-amino-4-oxa-1,2,3,4-tetrahydro-acridine, 9-amino-2-oxa-1,2,3,4-tetrahydro-acridine, 9-amino-8-fluoro-4-oxa-1,2,3,4-tetrahydro-acridine, 9-amino-4-oxa-1,2,3,4,5,6,7,8-octahydro-acridine or a pharmaceutical acceptable salt thereof are useful treating Alzheimer's disease.

Abstract: A novel heterocyclic amine derivative of the general formula: ##STR1## wherein a ring A and a ring B stand independently for an optionally substituted benzene ring, Z.degree. stands for O or S or ##STR2## stands for --CH.sub.2 --, X stands for O, S or NR.sup.1 wherein R.sup.1 stands for hydrogen atom or an alkyl group, Y stands for NH, O or (CH.sub.2).sub.n wherein n denotes 0 to 2, and R.sup.2 stands for an optionally substituted hydrocarbon group, or their salts.

Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

Abstract: The invention relates to new di- and tetrahydroisoquinoline derivatives having interesting cytostatic properties, to the preparation of the said new compounds, and to compositions comprising such a compound as a cytostatically active substance.

Abstract: Heterocyclic N-oxide derivatives of substituted benzo[5,6]cycloheptapyridines, and pharmaceutically acceptable salts and solvates thereof are disclosed, which possess anti-allergic and anti-inflammatory activity. Methods for preparing and using the compounds are also described.

Abstract: 5-Hydroxy-benzo-(1',2')-cyclodeca-2,7-diyne-1-one and derivatives thereof and related fused ring diyneone macrocyclic compounds are disclosed. The compounds possess DNA-cleaving, antibiotic and tumor growth-inhibiting properties. Methods of making and using the same are also disclosed.

Abstract: Novel 9-amino-1,2,3,4-tetrahydroacridines and related compounds of the formula ##STR1## wherein R.sup.1 is H, loweralkyl, or benzyl; R.sup.3 is H, loweralkyl, a group of the formula CH.sub.2 CHR.sup.2 Hal wherein R.sup.2 is hydrogen, loweralkyl, or phenyl and Hal is chloro, bromo, or iodo, or a group of the formula CHR.sup.2 CO.sub.2 R.sup.5 wherein R.sup.2 is as above and R.sup.5 is H or loweralkyl; Z is O or S; X is H, halogen, loweralkoxy, loweralkyl, or trifluoromethyl; n is 1, 2, or 3; the group ZR.sup.3 is bound to either the A- or B-position of the heteroaromatic nucleus; the pharmaceutically acceptable salts thereof; and the optical isomers thereof, useful as intermediates for the preparation of memory dysfunction relieving hexahydro-1H-quino[4,3,2-ef][1,4]benzoxazepines are related compounds and for relieving memory dysfunction are disclosed.

Abstract: The present invention relates to a method for the synthesis of certain bridged fused ring pyridines. Such bridged fused ring pyridines can be converted to huperzine A and analogs of huperzine A. The present invention also covers such bridged fused ring pyridines, compounds utilized for the preparation of the bridged fused ring pyridines and analogs of huperzine A.

Abstract: Novel benzopyrido piperidiene, piperidylidene and piperazine compounds of the generalized formula ##STR1## are disclosed as useful for the treatment of asthma, allergy and inflammation. Novel pharmaceutical compositions containing such compounds and processes for producing the compounds are also disclosed.

Abstract: Derivatives of benzo[5,6]cyclohepta pyridine, and pharmaceutically acceptable salts and solvates thereof are disclosed, which possess anti-allergic and anti-inflammatory activity. Methods for preparing and using the compounds are also described.

Abstract: This invention is directed to certain dibenzofurancarboxamides and dibenzofurancarboxamide acids and their use as 5HT.sub.3 antagonists having unique CNS, anti-emetic and gastric prokinetic activity void of any significant D.sub.2 receptor binding properties. Further, this invention relates to a process for the synthesis of stereoisomeric compounds having such CNS, anti-emetic and gastric prokinetic activity.

Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

Abstract: A method of reducing a carbonyl containing acridine of the formula ##STR1## where n is 1, 2 or 3; X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, trifluoromethyl, or NR.sub.3 R.sub.4 where R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R is hydrogen or loweralkyl and R.sub.1 is hydrogen, loweralkyl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, furylloweralkyl, thienylloweralkyl, oxygen-bridged arylloweralkyl, oxygen-bridged diarylloweralkyl, oxygen-bridged furylloweralkyl or oxygen-bridged thienylloweralkyl, is disclosed.

Abstract: Substituted 8-alkoxy-1,2,3,3a,8,8a-hexahydroindeno-[1,2-c]pyrroles; 5-alkoxy-2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-c]pyridines; and 9-alkoxy-2,3,3a,4,5,9a-hexahydro-1H-benz[e]isoindoles are selective 5-HT receptor agents and are thus useful in the treatment of anxiety, depression, and hypertension.

Abstract: There are disclosed novel compounds having the formula, ##STR1## wherein, m is an integer of 0-3;n is an integer of 1-4;R.sub.1 is hydrogen, alkyl, cycloalkyl, arylloweralkyl, aryl, naphthyl, furyl, thienyl, pyridinyl or pyrrolyl; each R.sub.2 and R.sub.3 are independently hydrogen, loweralkyl or arylloweralkyl, or alternatively R.sub.2 and R.sub.3 taken together form a methylene or ethylene bridge;X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkoxycarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.4 or --NR.sub.5 R.sub.6, R.sub.4 being hydrogen or loweralkyl, and R.sub.5 and R.sub.6 being independently hydrogen, loweralkyl or cycloalkyl;Y is CH.sub.2, CH.dbd.CH, O, S or NR.sub.7, R.sub.7 being hydrogen, loweralkyl or arylloweralkyl; with the proviso that the number of said methylene or ethylene bridge shall not exceed 1 and that when Y is CH.sub.2, one and only one combination of R.sub.2 and R.sub.

Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; R.sub.1 is hydrogen, alkyl, aryl, arylloweralkyl, naphthyl, furyl, thienyl, pyridinyl or pyrrolyl; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.2 or --NR.sub.3 R.sub.4 where R.sub.2 is hydrogen or loweralkyl, and R.sub.3 and R.sub.4 are independently hydrogen, loweralkyl or cycloalkyl; stereo, optical and geometrical isomers thereof, and pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory and pharmaceutical compositions comprising an effective memory enhancing amount of such a compound.

Abstract: There are disclosed a 9-acylamino-tetrahydroacridine derivative represented by the following formula (I): ##STR1## wherein R ##STR2## are as defined in the specification, its optical antipode or pharmaceutically acceptable acid addition salt thereof and a memory enhancing agent containing the same as an active ingredient.

Abstract: A pyridine derivative represented by formula (I): ##STR1## wherein the symbols are as defined in the specification, which exhibits selective, potential, and long-lasting inhibitory activity on biosynthesis of thromboxane A.sub.2 and is useful in the treatment and prevention of a broad range of diseases.

Abstract: A compound, or a solvate or salt thereof, of formula (I): ##STR1## in which: RCO is an acyl group in which the group R contains a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic ring and R.sub.1 R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4 -12 cycloalkylalkyl groups or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, or phenyl, or R.sub.3 together with R.sub.1 forms a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, group; R.sub.4 and R.sub.5, which may be the same or different and may be attached to the same or different carbon atoms of the isoquinoline nucleus, are each hydrogen, halogen, hydroxy, C.sub.1-6 alkyl, aryl, or R.sub.4 together with R.sub.5 form a --(CH.sub.2).sub.p -- group, where p is an integer of from 1 to 5 and one or more of the --(CH.sub.2)-- moieties is optionally substituted by a C.

Abstract: The present invention relates to a method for the synthesis of certain bridged fused ring pyridines. Such bridged fused ring pyridines can be converted to huperzine A and analogs of huperzine A. The present invention also covers such bridged fused ring pyridines, compounds utilized for the preparation of the bridged fused ring pyridines and analogs of huperzine A.

Abstract: The invention provides a compound of formula III ##STR1## or an acid addition salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are the same or different and represent hydrogen or lower alkyl, cycloalkyl, lower aralkyl or phenyl radicals any of which radicals may be substituted by lower alkyl, lower alkoxy or trifluoromethyl or R.sup.2 and R.sup.3 taken together, form a 5, 6 or 7 membered saturated ring, R.sup.4 and R.sup.5 may also represent lower alkoxy or cycloalkoxy, n is 1, 2 or 3 and, if more than one R.sup.4 radical is present the R.sup.4 radicals may be the same or different and esters of carboxylic acids with the hydroxy group shown, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and n are as defined above, with the provisos that (1) R.sup.6 and R.sup.7 are other than hydrogen when R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are all hydrogen and (2) R.sup.6 and R.sup.7 are not both methyl when R.sup.4 is methyl.

Abstract: Fluorinated aniline derivatives of the general formula I are described ##STR1## in which R.sup.1 represents H or (CH.sub.2).sub.n -X, n is a whole number from 1 to 3, X is H, OH, NH.sub.2, CH.sub.3 CONH, CH.sub.3 SO.sub.2 NH, SO.sub.3 H or ArSO.sub.3 H, Ar is optionally substituted arylene radical, R.sup.1 is alternatively also a --(CH.sub.2).sub.3 -- group, which is bonded to the free o-position next to the N-atom, Y is H, --O--, --NH--, --S-- or a C--C single bond, R.sup.2, in the event that Y=H, is the same as or different from R.sup.1 and means one of the radicals shown for R.sup.1, and in the event that Y is a C--C single bond or --O--, --NH-- or --S--, is an alkylene group having 1 to 3 carbon atoms linked with Y, and R.sup.3 =H, alkyl having 1 to 3 carbon atoms, OCH.sub.3, CH.sub.3 CONH, CO.sub.2 H or SO.sub.3 H.

Abstract: There are disclosed compounds having the formula ##STR1## where n is 1, 2 or 3;X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro or trifluoromethylR.sub.1 and R.sub.2 are each independently hydrogen, lower alkyl or arylloweralkyl, but both may not be arylloweralkyl simultaneously;R.sub.3 and R.sub.4 are each independently hydrogen, lower alkyl, arylloweralkyl, formyl or lower alkylcarbonyl, or alternatively the group --NR.sub.3 R.sub.4 taken as a whole constitutes ##STR2## stereo isomers thereof and pharmaceutically acceptable acid addition salts thereof, which are useful for the treatment of various memory dysfunctions characterized by decreased cholinergic function, such as Alzheimer's disease.

Abstract: Certain benzocycloheptapyridine compounds with fluorine substitution across the exocyclic double bond are prepared and they are useful as antihistaminic agents.