Abstract: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.

Abstract: A compound selected from those of general formula (I): ##STR1## wherein A represents a bivalent radical ##STR2## and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and Z are as defined in the description,the isomers and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful in the treatment of depression and anxiety.

Abstract: Methods for purifying 20(S)-camptothecin are described. The 20(S)-camptothecin in purified form is useful in the treatment of cancer.

Abstract: A compound selected from those of general formula (I): ##STR1## wherein A represents a bivalent radical selected from ##STR2## and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and Z are as defined in the description,the isomers and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful in the treatment of depression and anxiety.

Abstract: A tetracyclic compound of the formula: ##STR1## wherein A and the atoms to which it is attached and the optional double bond represent a mono- or di-heterocyclic ring selected from: ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X are specifically defined, which compounds are useful in the treatment of dopamine-related neurological, psychological and cardiovascular disorders as well as in the treatment of substance abuse and other addictive behavior disorders, cognitive impairment and attention deficit disorder.

Abstract: Anticancer compounds of formula I: ##STR1## and pharmaceutically acceptable salts thereof, wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.9 and R.sup.10 are independently selected from the group H, C.sub.1 -C.sub.4 alkyl, OR.sup.4, N(R.sup.4).sub.2, NO.sub.2, CN, F, Cl, Br, I, Ph, and CF.sub.3, and NHC(O)R.sup.4 ;R.sup.4 is independently selected from the group H, C.sub.1 -C.sub.4 alkyl, Ph, and CH.sub.2 Ph;X.sup.1 and Y.sup.1, and X.sup.2 and Y.sup.2 when present, join together to form:a benzene ring substituted with 1-4 R.sup.3 ;a five membered heterocycle having 1-2N, NH, O or S atoms and substituted with 1-2 R.sup.3 ;a six membered heterocycle having 1-2N and substituted with 1-2 R.sup.3 ; orthe group: ##STR2## wherein one of W or Z is C.dbd.O and the other is C.dbd.O, NH, S or O; or when X.sup.2 and Y.sup.2 are present and not joined together and when R.sup.2 is in the 4-position, then X.sup.2 and R.sup.2 may join together to form an ethylene bridge;are addressed.

Abstract: An ellipticine derivative of the formula [I]: ##STR1## wherein R is a substituted lower alkyl group, a substituted or unsubstituted lower alkoxy group or a heteromonocyclic group,or a pharmaceutically acceptable salt thereof, which show excellent antitumor activity, less side effects, less toxicity and/or high solubility in water and are useful as antitumor agent, and a process for preparing the same.

Abstract: The present patent application discloses compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.3, R.sup.4, R.sup.6 and R.sup.7 each have the meanings set forth in the specification.The compounds are useful for the treatment of various central nervous system disorders such as epilepsy and other convulsive disorders, anxiety, sleep disorders and memory disorders.

Abstract: The present invention provides novel tetrahydro-beta-carboline compounds and intermediates having useful central nervous system activity.

Abstract: Methods for purifying 20(S)-camptothecin are described. The 20(S)-camptothecin in purified form is useful in the treatment of cancer.

Abstract: The present invention relates to novel alkaloids from Mappia foetida, foetidine 1 and 2, having anticancer and antiviral properties. These alkaloids, soluble in water, are present in all the parts of the plant, and are the precursors of camptothecin and of 9-methoxy-camptothecin, which are alkaloids known to have pharmacodynamic properties but also to be insoluble in water. The particular water solubility of the novel compounds make them particularly suitable for the treatment of the patients by the parenteral route, avoiding the use of toxic excipients or of unsuitable chemical derivatizations.

Abstract: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided 3-ethanamine and 3-ethanamine related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds.

Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined in the description, and medicaments containing the same.

Abstract: Certain new 1,2-dihydroellipticine compounds having activity against CNS specific cancer cell lines because of their ease of passage across the blood-brain barrier are disclosed along with formulations and methods for treating CNS cancers employing these compounds.

Abstract: Novel polycyclic quinoline, naphthyridine and pyrazinopyridine derivatives are disclosed which are useful for treating allergic reactions, inflammation, peptic ulcers, hypertension, and hyperproliferative skin diseases and for suppressing the immune response in mammals. Methods for preparing said compounds are also disclosed.

Abstract: Anticancer compounds of formula I: ##STR1## and pharmaceutically acceptable salts thereof, wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected H, CH.sub.3, NH.sub.2, NO.sub.2, and CN;R.sup.9 and R.sup.10 are H or alkyl or halo, X.sup.1 and Y.sup.1 or X.sup.2 and Y.sup.2, when present, join together to form, independently, a six membered 1N heterocycle substituted with 1-2 R.sup.3 ; or the group: ##STR2## wherein one of W or Z is C.dbd.O and the other is C.dbd.O, NH, S or O; or when X.sup.2 and Y.sup.2 are not joined together and when R.sup.2 is in the 4-position, then X.sup.2 and R.sup.2 may join together to form an ethylene bridge; are disclosed.

Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined in the specification, and medicaments.

Abstract: A process for the production of ergoline derivatives of general formula I is described ##STR1## in which the bonds represent two single-bonds or a double bond and a single bond.R.sub.1 means a hydrogen atom or an alkyl group with 1-6 carbon atomsR.sub.2 symbolizes a hydrogen atom or an alkyl group with 1-6 carbon atoms,R.sub.3 represents a carboxyl group or a grouping of formula--CONR.sub.4 R.sub.5 or --NHCQNR.sub.6 R.sub.7with R.sub.4 and R.sub.5 meaning hydrogen or an alkyl radical with 1-6 carbons atoms optionally substituted by a hydroxy group and R.sub.6 and R.sub.7 meaning an alkyl group containing 1-4 carbon atoms and Q meaning an oxygen or sulfur atom.

Abstract: The invention relates to a novel process for the preparation of (-) -1.beta.-ethyl-1.alpha.-(hydroxymethyl) - 1,2,3,4,6,7,12,12b.alpha.-octahydro-indolo[2,3-a]quinolizine of the formula (I) ##STR1## and to novel intermediates obtained in this process. The compound of the formula (I) prepared by the process of the invention possesses a peripheral vasodilator effect.

Abstract: Methods for purifying camptothecin compounds are described. The camptothecin compounds in purified form are useful in the treatment of cancer.

Abstract: Compounds of the formula I ##STR1## in which X is O, S, SO, SO.sub.2 or NR.sub.13, R.sub.13 is, for example, methyl, and R.sub.1 to R.sub.12, independently of one another, are, for example, H, C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 Alkoxy, halogen or --CN. The compounds are photosensitive and photochromic and are suitable as photosensitizers and simultaneously as color indicators, and as photoswitchable color filters.

Abstract: Novel 4-[(alkyl or dialkyl)amino]quinolines are disclosed that are prepared by condensinBACKGROUND OF THE INVENTIONThe United States government has rights in this invention as a result of a grant from the NIAID of the National Institute of Health, Bethesda, Md.

Abstract: The present invention provides a new Pictet-Spengler process useful for preparing tetrahydro-beta-carboline compounds.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X, m, n, p, and q are as set forth in the specification, as well as pharmaceutically acceptable salts of acidic compounds of formula I with bases and of basic compounds of formula I with acids, which are useful in the control or prevention of inflammatory, immunological, oncological, bronchopulmonary, dermatological or cardiovascular disorders or for the treatment of asthma, AIDS or diabetic complications or for the stimulation of hair growth are described.

Abstract: Certain new 1,2-dihydroellipticine compounds having activity against CNS specific cancer cell lines because of their ease of passage across the blood-brain barrier are disclosed along with formulations and methods for treating CNS cancers employing these compounds.

Abstract: 5,6,7,8,9,10-Hexahydro-7,10-iminocyclohept[b]indole, 6,7,8,9,10,11-hexahydro-7,11-imino-5H-cyclooct[b]indole and substituted derivatives are effective in the treatment of psychoses with limited liability to produce concomitant adverse extrapyramidal symptoms. These compounds are also useful for treating other central nervous system and cardiovascular disorders.

Abstract: This invention is directed to a indole derivative represented by the general formula (1) ##STR1## wherein R.sub.1 stands for alkyl of 1 to 5 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms, cycloalkenylalkyl of 5 to 7 carbon atoms, aralkyl of 7 to 14 carbon atoms, trans-alkenyl of 4 to 5 carbon atoms, allyl, furanyl-2-ylalkyl of 1 to 5 carbon atoms, thienyl-2-ylalkyl of 1 to 5 carbon atoms, vinyloxycarbonyl, trichloroethoxycarbonyl, benzyloxycarbonyl, alkanoyl of 1 to 5 carbon atoms, aralkylcarbonyl of 7 to 14 carbon atoms, 2-furoyl, thiophene-2-carbonyl, cycloalkylcarbonyl of 4 to 7 carbon atoms, alkenylcarbonyl of 3 to 8 carbon atoms, or anisoyl, R.sub.2 for a hydrogen atoms, alkyl of 1 to 3 carbon atoms, benzyl, or alkanoyl of 1 to 5 carbon atoms, R.sub.3 for a hydrogen atoms, a fluorine atom, a chlorine atom, a bromine atom, nitro, or alkyl of 1 to 5 carbon atoms, R.sub.4 for a hydrogen atom, alkyl of 1 to 5 carbon atoms, benzyl, or phenyl, and R.sub.

Abstract: The invention provides a process for preparing single enantiomers of compounds represented by the formula: ##STR1## and chiral acid addition salts thereof; wherein: X and Y are independently hydrogen; lower alkyl; lower alkoxy; or halo; or X and Y taken together is methylenedioxy or ethylene-1,2-dioxy;which includes reduction of a compound represented by the formula: ##STR2## to give a mixture of stereoisomers represented by the formula: ##STR3## wherein each wavy line independently represents a bond in either the .alpha. or .beta. position;followed by dissolving the mixture of stereoisomers and a chiral resolving acid in a suitable solvent and allowing the solution to crystallize, giving a salt of the desired enantiomer.

Abstract: Compounds of the formula ##STR1## wherein: m is an integer of 1-6;n is an integer of 1 or 2;X and Y are independently hydrogen; hydroxy; lower alkyl; lower alkoxy; or halo; or X and Y when adjacent and taken together are methylenedioxy or ethylene-1,2-dioxy;R is ##STR2## wherein: R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl, or when taken together with the carbon to which they are attached are cycloalkyl;R.sup.3 is hydrogen, lower alkyl, lower alkoxy, hydroxy, trifluoromethyl or halo; and ##STR3## and pharmaceutically acceptable acid addition salts thereof. The compounds and salts exhibit useful pharmacological properties, including selective .alpha..sub.2 -adrenoceptor antagonist properties and 5-HT.sub.1A receptor partial agonist properties, and are particularly useful for the treatment of sexual dysfunction, depression and anxiety.

Abstract: The invention relates to a group of new annelated indolo [3,2-c] lactam derivatives of the formula ##STR1## having an antagonistic activity on 5-HT receptors. The compounds can be used for the treatment of symptoms which are caused by excessive stimulation of said receptors in the gastrointestinal system, the central nervous system, the cardiovascular system, the respiratory system, and for alleviating or preventing withdrawal symptoms which are induced by abuse of drugs.

Abstract: The present invention relates to racemic or optically active cis octahydro-indolo [2,3-a] quinolizine diester derivatives.

Abstract: The present invention provides condensed quinoline compounds represented by the following general formula (I): ##STR1## in which Z is NH, X is hydrogen, L is lower alkoxy, M is NHQ, Q is --SO.sub.2 CH.sub.3, Y is --NHR, and R is: ##STR2## These compounds are effective for inhibiting KB-cell growth and prolongation of the life span of mice implanted with tumor P-388.

Abstract: A method for permanently coloring fruits (cherries) and vegetables using carmine and other anthraquinones, using mixtures of multivalent metal ions and acid. The cherries are infused with a mixture of calcium ions, other multivalent metal ions, and carmine dye, at a pH at which the carmine is in soluble form. The cherries are then infused with an acidification solution which results in the preciptation of an insoluble carmine-metal ion complex within the cherries. Unused dye is treated and recycled.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 to R.sub.8, which may be identical to or different from each other, have diverse meanings, and the dotted line between the carbon atoms in the 4- and 4a- position or the 4a- and 5-position or the 42- and 12a position may be a single or double bond, or pharmaceutically acceptable salts thereof, as well as a process for the preparation of these compounds, and pharmaceutical compositions containing these compounds. The compounds and their salts are useful for the treatment of heart-circulation disorders.

Abstract: A method for making 8-methyl-7-(1-oxopropyl)indolizino[1,2-b]quinolin-9(11H)-ones from 4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-3,14(4H,12 H)-diones, said method being graphically illustrated as follows: ##STR1##

Abstract: Novel indoloquinoline compounds of formula (I), benzo(b)acridines of formula (II) and benzo(c)acridines of formula (III) have carcinostatic activities. The compounds, processes for preparing the compounds via nucleophilic aromatic substitution, and carcinostatic compositions containing the same are disclosed.

Abstract: New intermediate compounds are disclosed of the formula I, ##STR1## wherein R.sub.1 and R.sub.2 are independently alkyl having 1 to 4 carbon atoms,or acid-addition salts thereof of formula Ib, ##STR2## wherein X represents an acid residue, and a process for the preparation of the intermediate compounds.

Abstract: New pyridobenzoindole derivatives of general formula (I), in which R is H or alkyl (1 or 2 C), alk is straight or branched alkylene (2 to 4 C), R.sub.1 denotes a hydrogen atom or an alkyl radical (1 or 2 C), R.sub.2 denotes a hydroxy or methoxy radical, and R.sub.3 is methyl or ethyl and their addition salts with acids, useful as antitumor agents.

Abstract: The subject of the present invention is a process for the preparation of isoquinoline derivatives in four steps wherein use is made as synthetic intermediates of organo-lithium compounds or related compounds.

Abstract: A compound for formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, and Z are described in claim 1.

Abstract: Substituted 1,8-naphthalenedicarboximides of the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Y, and Z have the meanings recited in the disclosure are disclosed as new compounds suitable for use as antidotes in herbicidal compositions.

Abstract: A method of preparing certain substituted alkali metal 4-carboxy-piperidine salts (I) by alkaline hydrolysis of certain novel substituted 1,3,8-triazaspiro[4.5]decane-2, 4-diones (IV) which in turn are obtained from certain novel substituted chlorosulphonylamido piperidines (III).

Abstract: The invention provides lactam derivatives of the general formula (I) ##STR1## wherein n represents 2 or 3; Im represents an imidazolyl group of the formula: ##STR2## wherein one of the groups represented by R.sup.1, R.sup.2 and R.sup.3 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl- group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; Y represents a group --(CH.sub.2).sub.m --, wherein m represents 2, 3 or 4; or Y represents a group --X(CH.sub.2).sub.p --, wherein p represents 2 or 3, X represents an oxygen or a sulphur atom or a group NR.sup.4, where R.sup.4 is a C.sub.1-6 alkyl group, and X is attached to the benzene ring moiety of the molecule; and physiologically acceptable salts and solvates thereof.The compounds of formula (I) are potent and selective antagonists of 5-hydroxytryptamine at 5-HT.sub.

Abstract: Disclosed are the compounds of formula I ##STR1## wherein R.sub.1 -R.sub.3 represent hy drogen or lower alkyl; m represents the integer 2 or 3; n represents the integer 1 or 2; Het represents a pyrrole or imidazole ring bonded at any two adjacent positions and optionally substituted by one or two of lower alkyl; and pharmaceutically acceptable salts of compounds of formula I wherein Het represents optionally substituted imidazole; their methods of preparation; pharmaceutical compositions thereof, and their use for treating cognitive disorders in mammals.

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: Tetracyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, X, Y, Z and n are as hereinafter described, and salts thereof, prepared starting from corresponding tricyclic compounds, are described. The compounds I and some of the said tricyclic compounds have antibacterial activity, and are therefore useful as antibacterial agents.

Abstract: To prepare the compound (I), a lithiation of the compound (II) is performed, an aldehyde (IV) is reacted with the compound (III) formed, leading to the secondary alcohol (V) which is subjected to a reduction leading to the compound (VI), which is then subjected to a hydrolysis (of the dioxolane group)/cyclization/dehydration reaction. The procedure may be followed by a nucleophilic substitution reaction of the chlorine. The compounds (a) below exhibit antitumor activity. ##STR1## R=C.sub.1 -C.sub.3 alkyl; Ar=aromatic or polycyclic aromatic group; R.sub.1 and r.sub.2 =H or C.sub.1 -C.sub.3 alkyl; and n=2 to 4. No drawing.

Abstract: The invention provides a process for preparing compounds, as a single enantiomer or mixture of enantiomers, represented by the formula: ##STR1## in which: X and Y are independently hydrogen, hydroxy, lower alkyl, lower alkoxy or halo, or X and Y taken together is methylenedioxy or ethylene-1,2-dioxy, andZ is --SO.sub.2 R or --C(O)NR.sup.3 R.sup.4, in which;R is lower alkyl, optionally substituted phenyl, --(CH.sub.2).sub.m OR.sup.1 or --NR.sup.1 R.sup.2 wherein m is an integer of 1 to 6 and R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl; andR.sup.3 and R.sup.4 are independently hydrogen, alkyl, optionally substituted phenyl or phenyl lower alkyl; orR.sup.1 and R.sup.2 taken together with the nitrogen to which they are attached or R.sup.3 and R.sup.4 taken together with the nitrogen to which they are attached represent a heterocycle of the formula: ##STR2## wherein A is --CH.sub.2 --, --NR.sup.1 -- or oxygen; and novel intermediates.

Abstract: Compounds of formulas (1) and (2): ##STR1## in which: X and Y are independently hydrogen, hydroxy, lower alkyl, lower alkoxy or halo, or X and Y taken together is methylenedioxy or ethylene-1,2-dioxy;W is oxygen or sulfur; andZ is --R.sup.1, --OR.sup.2 or --NR.sup.3 R.sup.4, whereinR.sup.1 is lower alkyl, lower haloalkyl, cycloalkyl, optionally substituted phenyl or phenyl lower alkyl, or heteroaryl;R.sup.2 is lower alkyl, optionally substituted phenyl or phenyl lower alkyl;R.sup.3 and R.sup.4 are independently hydrogen, alkyl, optionally substituted phenyl or phenyl lower alkyl; orR.sup.3 and R.sup.4 taken together with the nitrogen to which they are attached represent a heterocycle of the formula: ##STR2## wherein A is --(CH.sub.2).sub.m, --N(R.sup.5)-- or oxygen, in which m is an integer of 0-2 and R.sup.5 is hydrogen or lower alkyl;or a pharmaceutically acceptable salt thereof, are useful as .alpha..sub.2 -blockers.