Abstract: This invention discloses novel imidazo[2,1-a]pyrrolo[2,1-c][1,4]benzodiazepine derivatives, processes for their preparation, pharmaceutical compositions thereof and methods for using the compounds. The compounds of this invention are useful as antiobesity agents to reduce food intake in a mammal.

Abstract: 7,8,9,10-Tetrahydrobenzo[h]quinolin-9-amine derivatives of the formula ##STR1## in which R.sup.1 and R.sup.2 each independently is hydrogen or lower alkyl, or R.sup.1 and R.sup.2 together form a chain of the formula --(CH.sub.2).sub.n -- where n is the integer 4, 5 or 6, are useful for treating depression.

Abstract: The N-substituted dimeric cyclopeptide derivatives of formula ##STR1## in which A is a peptide residue having one to four amino acid residues; R.sup.1 is lower alkyl, phenyl or phenyl(lower)alkylene; R.sup.2 is lower alkyl, cyclo(lower)alkyl or lower alkoxycarbonyl(lower)alkylene; and R.sup.3 is a neutral amino acid side chain and a method for the preparation of the compounds of formula I are disclosed. The compounds of formula I are useful for treating microbial infections. Pharmaceutical compositions also are disclosed.

Abstract: 1,4,5,6-Tetrahydropyrimidine derivatives characterized by having a phenyl or substituted phenyl at positions 1 and 6 in addition being further substituted at position 2. The foregoing compounds are useful as diuretic agents in a mammal. Methods for the preparation and use of the compounds are disclosed.

Abstract: Herein is disclosed compounds of the formula ##STR1## in which R.sup.1,R.sup.2,R.sup.3,R.sup.4 and R.sup.5 each is hydrogen or lower alkyl, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the compounds and pharmaceutical compositions. The compounds exhibit dopamine-receptor stimulating activity in a mammal and are useful for treating hyperprolactinemia, galactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders.

Abstract: 13-Chloro-octahydrobanzo[6,7]cyclohepta[1,2,3-de]pyrido[2,1-a]isoquinolin-5 -ols, substituted on the piperidine ring with lower alkyl or a cycloalkyl are disclosed. The compounds are useful CNS depressants. Methods for their preparation and use also are disclosed.

Abstract: Compounds of formula I ##STR1## in which R.sup.1 is hydrogen, halogen, nitro, trifluoromethyl, lower alkyl or lower alkoxy; R.sup.2 is hydrogen or lower alkyl; R.sup.3 is hydroxy, 1H-tetrazol-5-yl or COOR.sup.4 wherein R.sup.4 is hydrogen or lower alkyl, and X is O, S, SO or SO.sub.2, are disclosed. The compounds of formula I are useful for treating allergic conditions. Methods for the preparation and use of the compounds are disclosed.

Abstract: Compounds of formula I ##STR1## in which R.sup.1 is hydrogen, halogen, nitro, trifluoromethyl, lower alkyl or lower alkoxy; R.sup.2 is hydrogen or lower alkyl; R.sup.3 is hydroxy, 1H-tetrazol-5-yl or COOR.sup.4 wherein R.sup.4 is hydrogen or lower alkyl, and X is O, S, SO or SO.sub.2, are disclosed. The compounds of formula I are useful for treating allergic conditions. Methods for the preparation and use of the compounds are disclosed.

Abstract: [2]Benzopyrano[3,4-c]pyridine derivatives characterized by having a 2,3,4,4a,6,10b-hexahydro-1H-[2]benzopyrano[3,4-c]pyridine nucleus bearing a substituent at position 6 are disclosed. The nucleus can be optionally further substituted at positions 2,3,4,6 and on the aromatic ring. The derivatives are useful diuretic, anorexic, antidepressant, anticonvulsant and antihypertensive agents. Methods for their preparation and use also are disclosed.

Abstract: [2]Benzopyrano[4,3-c]pyridine derivatives characterized by having a 2,3,4,4a,6,10b-hexahydro-1H-[2]benzopyrano[4,3-c]pyridine nucleus are disclosed. The nucleus can be optionally further substituted at positions 2,6 and on the aromatic ring. The derivatives are useful diuretic, anorexic, antidepressant, anticonvulstant and antihypertensive agents. Methods for the preparation and use of these derivatives also are disclosed.

Abstract: Disclosed herein are compounds of the formula ##STR1## in which Ar is phenyl or 1-naphthyl; R.sup.1 is hydrogen or lower alkyl; and R.sup.2 and R.sup.3 are either the same or different selected from the group consisting of hydrogen or lower alkyl; with the proviso that when R.sup.1 is lower alkyl then R.sup.2 is the same lower alkyl. The compounds are antidepressant agents and methods for their preparation and use also are disclosed.

Abstract: Tricyclic alkylamines, and their acid addition salts with pharmaceutically acceptable acids, are disclosed. The tricyclic ring system for these compounds is selected from the group consisting of 1,2,3,4-tetrahydrocyclopent[b]indole, 1,2,3,4-tetrahydrocarbazole and 5,6,7,8,9,10-hexahydrocyclohept[b]indole. The compounds are characterized further in that the ring system carbon atom bearing the alkylamine residue is carbon atom 3, 1 and 6 in the respective ring systems and in each case the said carbon atom also is substituted with a lower alkyl. The tricyclic alkylamines are useful antidepressant agents. Methods for their preparation and use are disclosed.

Abstract: Compounds of formula 1 ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different selected from the group consisting of hydrogen, halogen, nitro, trifluoromethyl, lower alkyl and lower alkoxy, or R.sup.1 and R.sup.2, R.sup.2 and R.sup.3, or R.sup.3 and R.sup.4 together form a CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 chain and R.sup.3 and R.sup.4, R.sup.1 and R.sup.4 and R.sup.1 and R.sup.2, respectively, are as defined above, R.sup.5 is hydrogen, lower alkyl or a radical of formula --Alk--OR.sup.6 wherein Alk is an alkylene selected from the group consisting of CR.sup.7 R.sup.8, CR.sup.7 R.sup.8 CR.sup.9 R.sup.10, CR.sup.7 R.sup.8 CR.sup.9 R.sup.10 CR.sup.11 R.sup.12 and CR.sup.7 R.sup.8 CR.sup.9 R.sup.10 CR.sup.11 R.sup.12 CR.sup.13 R.sup.14 wherein each of R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 is hydrogen or lower alkyl and R.sup.6 is hydrogen or lower alkyl; R.sup.15 is hydrogen or lower alkyl; X is O, S, SO or SO.sub.2 ; Y is O or NR.sup.

Abstract: The dipeptide derivatives of formula Ih--l--pro--N(R.sup.1)CH(R.sup.2)CO--NHR.sup.3 (I)in which R.sup.1, R.sup.2 and R.sup.3 each independently is lower alkyl and a method for their preparation are disclosed. The dipeptide derivatives of formula I possess central nervous system activity and methods for their use are given.

Abstract: A process for preparing 11-deoxyprostaglandin E.sub.1, E.sub.2 and E.sub.3 and analogs thereof is realized by treating an appropriate di(lower)alkyl 3-(optionally substituted)-2-formylcyclopropane-1,1-dicarboxylate with an ylid prepared from a Witting reagent of formula (AlkO).sub.2 POCH.sub.2 CO-(c)-CH.sub.3 in which Alk is an alkyl containing one to three carbon atoms and (c) is either (CH.sub.2).sub.q wherein q is an integer from 1 to 6 or cis CH.sub.2 CH.dbd.CH(CH.sub.2).sub.r wherein r is an integer from 0 to 3 to obtain the corresponding compound of formula: ##STR1## in which R.sup.2 is hydrogen, lower alkyl or CH.sub.2 OR.sup.3 wherein R.sup.3 is lower alkanoyl, R.sup.4 is lower alkyl and (c) is as defined herein. The latter compound is reduced with an alkali metal borohydride to yield the corresponding alcohol derivative. Condensation of this alcohol derivative or preferably its corresponding tetrahydropyran-2-yl ether derivative with a triester of formula CH(COOR.sup.6).sub.2 -(a)-(CH.sub.

Abstract: Disclosed herein are compounds of the formula ##STR1## in which Ar is phenyl or 1-naphthyl; R.sup.1 is hydrogen or lower alkyl; and R.sup.2 and R.sup.3 are either the same or different selected from the group consisting of hydrogen or lower alkyl; with the proviso that when R.sup.1 is lower alkyl then R.sup.2 is the same lower alkyl. The compounds are antidepressant agents and methods for their preparation and use also are disclosed.

Abstract: 2-(1-Hydroxy-2-octynyl)- and 2-(3-hydroxy-1-octynyl)-5-oxocyclopentaneheptanoic acids, their salts and their corresponding lower alkyl esters are disclosed. The compounds inhibit the actions of prostaglandins. Methods for their preparation and use are given.

Abstract: Tropone derivatives substituted with an amino-derivative of oxalic acid or acetic acid are disclosed. In addition, the tropone nucleus can be optionally further substituted. The foregoing compounds are useful for preventing or treating allergic conditions in a mammal. Methods for the preparation and use of the compounds are disclosed.

Abstract: Thiazinoindole derivatives characterized by having an amino(lower)alkyl radical attached to the 1 position of a 1H-1,4-thiazino[4,3-a]indole nucleus are disclosed. The amino portion of the amino(lower)alkyl radical may be further substituted with one or two lower alkyl groups or incorporated in a heterocyclic amine radical. The derivatives are substituted further at positions 1 and 10 and may be optionally substituted at positions 3, 4, 6, 7, 8 and 9. The thiazinoindole derivatives of this invention are useful antidepressant and antiulcer agents. Methods for the use of these derivatives and compositions containing them are also disclosed.

Abstract: The tripeptide derivatives of formulaH--L--Pro--N(R.sup.1)CH(R.sup.2)CO--Y--R.sup.3 (1)in which R.sup.1 is hydrogen, lower alkyl or NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 each are lower alkyl, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is amino, lower alkylamino, di(lower)alkylamino or amino(lower)alkylamino and Y is one of the amino acid residues Gly or D-Ala with the proviso that when R' is NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are as defined herein and R.sup.2 and Y are as defined herein, R.sup.3 is lower alkylamino, di(lower)alkylamino or amino(lower)alkylamino, .Iadd.and with the further proviso that when R.sup.1 is hydrogen, R.sup.2 is hydrogen or lower alkyl and Y is Gly then R.sup.3 is amino(lower)alkylamino, .Iaddend.and a method for their preparation are disclosed. The tripeptide derivatives of formula 1 possess central nervous system activity and methods for their use are given.