Abstract: The present invention provides (8.beta.)-N-substituted cyclo or bicycloalkyl-6-(substituted)-ergoline-8-carboxamides useful for occupying 5HT.sub.2 or 5HT.sub.1c receptors in mammals. The invention also provides methods for treating a variety of disorders and conditions related to or affecting these receptors as well as pharmaceutical formulations of the compounds of the invention.

Abstract: The present invention provides compounds of the formula (I) ##STR1## wherein A, R.sub.1, R.sub.2 and R.sub.3 are defined as in the specification, or a pharmaceutically acceptable salt thereof. A process for their preparation and the pharmacetical compositions comprising them are also provided.

Abstract: The invention provides a process for the preparation of ergoline derivatives of the formula I ##STR1## the process comprising reacting an ergoline amide of the formula II with an isocyanate of formula III ##STR2## in presence of a metal catalyst and of a phosphorus compound. The compounds of the formula I are useful antiprolactinic and antiparkinson agents.

Abstract: There are disclosed novel ergoline derivatives of 2-propinylamine of the general formula I ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 independently represent a hydrogen atom or a straight-chain or branched-chain C.sub.1 -C.sub.6 alkyl group,X represents a hydrogen or a halogen atom,Z represents a carbonyl or methylene group andC.sub.9 C.sub.10 represents a single or a double bond, diastereomeric forms, racemates and acid addition salts thereof.There are also described a process for the manufacture of the compounds of the general formula I and a pharmaceutical composition containing the same.The compounds of the general formula I can be used in the pharmaceutical industry as active substances for the manufacture of medicaments used in the treatment of hypertension, migraine, anxiety states, depressions, obesity etc.

Abstract: The present invention relates to compounds of the general formula I ##STR1## wherein A.sup..sym. and B.sup..sym. independently of one another denote a proton, with the limitation that they do not both simultaneously denote protons, the equivalent part of the barium ion, an ion of the general formula II ##STR2## or an ion of the general formula III ##STR3## and wherein R.sup.1 to R.sup.8, R.sup.11 to R.sup.16, X and m and n are as defined in the description, processes for their preparation and their use as charge control agents in toners and developers and as charge improving agents in powders and varnishes.

Abstract: Compounds of formula I ##STR1## in which R.sup.2 means optionally substituted C.sub.1-7 alkyl, C.sub.2-7 alkenyl, CH.sub.2 --O--C.sub.1-4 alkyl or CH.sub.2 --S--C.sub.1-4 alkylR.sup.6 means C.sub.2-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-5 -cycloalkyl-C.sub.1-2 alkyl andR.sup.8 means CH.sub.2 --X, ##STR2## in which X stands for CN, OCH.sub.3, SCH.sub.3 or CONH.sub.2 and R.sup.1 stands for hydrogen, halogen, methyl or methoxy, and R.sup.3 and R.sup.4 each mean C.sub.1-4 alkyl or (CH.sub.2).sub.n --N(CH.sub.3).sub.2, in which n=1-4, and their acid addition salts, the process for their production, their use as pharmaceutical agents as well as intermediate compounds are described.

Abstract: This invention provides N-(2-hydroxycyclopentyl)-1-isopropyl-6-methylergoline-8-carboxamides useful for blocking 5HT.sub.2 receptors in mammals having an excess of serotonin centrally or peripherally. The invention also provides methods for treating sexual dysfunction, hypertension, migraine, vasospasm, thrombosis, ischemia, depression, anxiety, sleep disorders and appetite disorders with a compound of the invention.

Abstract: The invention relates to a novel stereoselective process for the preparation of dihdyrolysergol from lysergol by hydrogenation in the presence of solvent and palladium catalyst applied on a carrier, which comprises hydrogenating lysergol in the presence of one or more aprotic solvent(s) containing tertiary nitrogen atom(s) and a palladium catalyst applied on activated carbon, and recovering the product obtained from the reaction mixture in a known manner.

Abstract: This invention provides N-(2-hydroxycyclopentyl)-1-isopropyl-6-methylergoline-8-carboxamides useful for blocking 5HT.sub.2 receptors in mammals having an excess of serotonin centrally or peripherally. The invention also provides methods for treating sexual dysfunction, hypertension, migraine, vasospasm, thrombosis, ischemia, depression, anxiety, sleep disorders and appetite disorders with a compound of the invention.

Abstract: Processes for the preparation of esters of N.sub.1 -methyl-10.alpha.-methoxylumilysergol are described, in which lysergol esters are subjected to N-methylation and subsequently to photochemical reaction with methanol/H.sub.2 SO.sub.4. The esters of N.sub.1 -methyl-10-methoxylumilysergol obtained in this way can then be saponified or converted directly into other esters.

Abstract: 2-bromo-8-ergolinyl compounds of the formula ##STR1## wherein R.sup.8 is NH.sub.2, NH--CONEt.sub.2, CONH.sub.2, ##STR2## and ##STR3## wherein R.sup.1 =C.sub.1-4 -alkyl andR.sup.2 =C.sub.1-4 -alkyl and benzyl,R.sup.9 and R.sup.10 each mean hydrogen or, together, a bond, and the substituent R.sup.8 can be in the .alpha.- or .beta.- position, and their acid addition salts,can be prepared from corresponding 8-ergolinyl compounds and their acid addition salts by bromination with elemental bromine in the presence of hydrogen bromide in a halogenated hydrocarbon.

Abstract: Ergoline derivatives of general Formula I ##STR1## wherein C.sub.8 C.sub.9 and C.sub.9 C.sub.10 are both CC-single bonds or one is a C.dbd.C-double bond,R.sup.6 is C.sub.1-4 alkyl,R.sup.8 is methyl, hydroxymethyl, carbonylmethoxy, ureido or N,N-diethylureido, each in the .alpha.- or .beta.-position, andR is hydrogen or nitro,are prepared by dehydrogenation of corresponding 2,3-dihydroergoline derivatives using an electrophilic reagent in an apolar solvent and a base.

Abstract: Alkoxycycloalkyl esters of 1-substituted-6-C.sub.1-4 straight chain alkyl (or allyl)ergoline-8.beta.-carboxylic acids, useful as 5HT receptor antagonists.

Abstract: Cycloalkyl or ketocycloalkyl esters of 1-substituted-6-C.sub.1-4 straight chain alkyl (or allyl)-ergoline-8.beta.-carboxylic acids, useful as 5HT receptor antagonists.

Abstract: This invention provides (8.beta.)-N-cycloalkyl-1-alkyl-6-(substituted) ergoline-8-carboxamides useful for blocking 5HT.sub.2 receptors in mammals having an excess of serotonin centrally or peripherally. The invention also provides methods for treating hypertension, migraine, vasospasm, thrombosis, ischemia, depression, anxiety, sleep disorders and appetite disorders with a compound of the invention.

Abstract: Alkoxycycloalkyl esters of 1-substituted-6-C.sub.1-4 straight chain alkyl (or allyl)ergoline-8.beta.-carboxylic acids, useful as 5HT receptor antagonists.

Abstract: A process for preparing 1-methyllysergol or 10.alpha.-methoxy-1-methyllumilysergol, which comprises adding a base, which is an alkali metal hydride or alcoholate, to a solution of lyergol or 10.alpha.-methoxylumilysergol in a polar aprotic solvent in such a way that the molecular ratio between the base and the lysergol or 10.alpha.-methoxylumilysergol remains less than 0.5:1, and then adding a methylating agent which is methyl iodide, methyl sulphate or trimethylsulphonium iodide.1-methyllysergol and 10.alpha.-methoxy-1-methyllysergol are useful intermediates in the synthesis of pharmacological compounds.

Abstract: Cycloalkyl or ketocycloalkyl esters of 1-substituted-6-C.sub.1-4 straight chain alkyl (or allyl)-ergoline-8.beta.-carboxylic acids, useful as 5HT receptor antagonists.

Abstract: This invention provides (8.beta.)-N-heteroalkyl-1-alkyl-6-(substituted)ergoline-8-carboxamides useful for blocking 5HT.sub.2 receptors in mammals having an excess of serotonin centrally or peripherally. The invention also provides methods for treating sexual dysfunction, hypertension, migraine, vasospasm, thrombosis, ischemia, depression, anxiety, sleep disorders and appetite disorders with a compound of the invention.

Abstract: Organic amide compounds of the formula ##STR1## wherein R.sub.1 --CO is a residue of a carboxylic acid with the proviso that the carboxylic acid is not a natural fatty acid normally bound to nitrogen of nitrogenous lipids, R.sub.2 is a hydrogen atom, a C.sub.1-7 alkyl group, or a C.sub.4-7 cycloalkyl group, and R.sub.3-N is a residue of a nitrogenous lipid. The compounds are useful in increasing or stimulating the in vivo biological activity of in vitro biologically active carboxylic acids.

Abstract: Alkoxycycloalkyl esters of 1-substituted-6-C.sub.1-4 straight chain alkyl (or allyl)ergoline-8.beta.-carboxylic acids, useful as 5HT receptor antagonists.

Abstract: Cycloalkyl or ketocycloalkyl esters of 1-substituted-6-C.sub.1-4 straight chain alkyl (or allyl)-ergoline-8.beta.-carboxylic acids, useful as 5HT receptor antagonists.

Abstract: The present invention provides novel bicyclic ergoline esters useful as serotonin antagonists.

Abstract: Ketoalkyl esters of 1-substituted-6-C.sub.1-4 straight chain alkyl (or allyl)ergoline-8.beta.-carboxylic acid, useful as 5HT receptor antagonists.

Abstract: The invention relates to a novel process for the halogenation in 2-position of ergot alkaloids. The process is characterized by that as a halogenating agent a system consisting of dimethylsulfoxide, a trialkylhalosilane or triarylhalosilane and optionally a hydrogen halide is used.

Abstract: Method of blocking 5HT without effect on alpha receptors with 1-loweralkyl-6-straight chain alkyl-8.beta.-hydroxycycloalkyloxycarbonylergolines.

Abstract: A therapeutic method employing 2,3-dihydroergolines is disclosed. Said method enhances serotonergic function in the nervous system of a mammal in need thereof, thereby finding application in serotonin-mediated physiological manifestations including memory, depression, anxiety, pain and appetite. Also disclosed are pharmaceutical compositions containing said 2,3-dihydroergolines in admixture with pharmaceutically acceptable diluents and carriers.

Abstract: The present invention provides novel bicyclic ergoline esters useful as serotonin antagonists.

Abstract: Ketoalkyl esters of 1-substituted-6-C.sub.1-4 straight chain alkyl (or allyl)ergoline-8.beta.-carboxylic acid, useful and 5HT receptor antagonists.

Abstract: Organic amide compounds of the formula ##STR1## wherein R.sub.1 --CO is a residue of a carboxylic acid with the proviso that the carboxylic acid is not a natural fatty acid normally bound to nitrogen of nitrogenous lipids, R.sub.2 is a hydrogen atom, a C.sub.1-7 alkyl group, or a C.sub.4-7 cycloalkyl group, and R.sub.3-N is a residue of a nitrogenous lipid. The compounds are useful in increasing or stimulating the in vivo biological activity of in vitro biologically active carboxylic acids.

Abstract: A process for preparing an N-methyl derivative of ergoline of formula: ##STR1## in which R.sub.1 denotes a carboxy or alkoxycarbonyl group in which the alkyl portion contains 1 to 4 carbon atoms, R.sub.2 denotes a hydrogen atom or a methoxy group and R.sub.3 denotes a hydrogen atom or R.sub.2 and R.sub.3 together form a direct bond, or in which R.sub.1 denotes a hydroxymethyl group, R.sub.2 denotes a hydrogen atom or a methoxy group and R.sub.3 denotes a hydrogen atom, which comprises methylating an ergoline derivative of formula: ##STR2## in which R.sub.1, R.sub.2 and R.sub.3 are defined as above, with methyl carbonate in the presence of a basic agent, in an apolar aprotic solvent in the present of a phase transfer catalyst.

Abstract: A process for preparing an ergoline of the formula ##STR1## wherein C.sub.9 ----C.sub.10 is a CC single or double bond,R.sup.1 is hydrogen or CONR.sub.2, R being hydrogen, methyl, or ethyl, and wherein NR' is in the .alpha.- or .beta.- position,R.sup.2 is lower alkyl of up to 3 carbon atoms, and the salts thereof,comprises treating the corresponding ergolinyl carboxylic acid amide with lead(IV) acetate in an aprotic polar solvent; reacting the intermediarily formed corresponding isocyanate with water or with a reactive amine of up to 4 carbon atoms, (e.g. a mono- or dialkylamine of up to 4-C atoms); and, optionally, treating the resultant product with an acid to form the corresponding salt.

Abstract: A process for preparing an N-methyl derivative of methyl dihydrolysergate and methyl methoxylumilysergate, of formula: ##STR1## in which R.sub.1 denotes a hydrogen atom or a methoxy group, which comprises reacting a methylating agent with a compound of formula: ##STR2## in which R.sub.1 is defined as above, in the presence of a quaternary salt, in the presence of a solid metal alcoholate of formula CH.sub.3 --OM in which M denotes an alkali metal atom, or an alkali metal hydride, and in the presence of a dehydrating agent of formula R.sub.2 --COO--CH.sub.3 in which R.sub.2 denotes a hydrogen atom or an alkyl, alkyloxy, alkyloxycarbonyl or aryl group or of formula R.sub.3 --C(OCH.sub.3).sub.3 in which R.sub.3 denotes a hydrogen atom, an alkyl group or an aryl group.

Abstract: The present invention provides a process for N-alkylating dihydrolysergic acid with a substituted benzenesulfonate derivative.

Abstract: Novel ergoline derivatives, substituted in the 2-position, of the formula ##STR1## wherein C.sub.8 -C.sub.9 and C.sub.9 -C.sub.10 each independently is a CC-single or a C.dbd.C-double bond, but not together a cumulated double bond, and the substituent in the 8-position is in the .alpha.- or .beta.-configuration where C.sub.8 -C.sub.9 is a CC-single bond,R.sup.2 isCN, SR, SOR, ##STR2## wherein n is 2 or 3, ##STR3## and --CH(OH)R, wherein R has the meaning of H or C.sub.1-4 -alkyl, the grouping COR' and CSR' wherein R'.dbd.OH, OC.sub.1-4 -alkyl, benzyl, NH.sub.2 or NHR",the grouping CH.dbd.CH--CO.sub.2 R" and CH.sub.2 --CH.sub.2 --CO.sub.2 R" wherein R".dbd.C.sub.1-4 -alkyl,the grouping C.vertline.C-R'" and HC.dbd.CH--R'" wherein R'".dbd. hydrogen, C.sub.1-4 -alkyl, phenyl, CH.sub.2 OH, CR".sub.2 OH, ##STR4## CO.sub.2 R", CH.sub.2 NR".sub.2 or SiMe.sub.2 R"; C.sub.1-3 -alkyl, or C.sub.1-3 -alkyl substituted by OH or phenyl; or ##STR5## wherein R" is C.sub.1-4 alkyl, R.sup.6 is C.sub.1-4 -alkyl andR.sup.

Abstract: Alkoxycycloalkyl esters of 1-substituted-6-C.sub.1-4 straight chain alkyl (or allyl)ergoline-8.beta.-carboxylic acids, useful as 5HT receptor antagonists.

Abstract: Alkoxy or dialkoxyalkyl esters of 1-substituted-6-C.sub.1-4 straight chain alkyl (or allyl)ergoline-8.beta.-carboxylic acid, useful as 5HT receptor antagonists.

Abstract: Method of blocking 5HT without effect on alpha receptors with 1-loweralkyl-6-straight chain alkyl-8.beta.-hydroxycycloalkyloxycarbonylergolines.

Abstract: Cyclic ether esters of 1-substituted-6-C.sub.1-4 straight chain alkyl (or allyl)ergoline-8.beta.-carboxylic acid, useful as 5HT receptor antagonists.

Abstract: Phenacyl or substituted phenacyl esters of 1-substituted-6-C.sub.1-4 straight chain alkyl (or allyl)ergoline-8.beta.-carboxylic acid, useful as 5HT receptor antagonists.

Abstract: The invention relates to a novel process for the preparation of 2-bromo-.alpha.-ergocryptine and its acid addition salt by brominating .alpha.-ergocryptine in such a way that the bromination is carried out at room temperature by using a dimethylsulphoxide-hydrogen bromide mixture containing no more 0.02% of water and, if desired, converting the thus-obtained 2-bromo-.alpha.-ergocryptine to an acid addition salt in a known manner.

Abstract: 2-bromoergolines can be reduced in good yields, without dimerization as determined by NMR product analysis, to the corresponding 2,3-dihydroergolines under otherwise conventional reducing conditions by introducing 2-bromoergolines, together with sodium borohydride, into trifluoroacetic acid under cooling to prevent the reaction mixture from rising above ambient temperature.

Abstract: Compounds of formula I: ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group; R.sub.2 represents a hydrogen or halogen atom or a methyl, cyano, C.sub.1 -C.sub.4 alkylthio or phenylthio group; R.sub.7 and R.sub.8 represent hydrogen atoms and R.sub.3 represents a hydrogen atom or a methoxy group, or R.sub.7 represents a hydrogen atom and R.sub.3 and R.sub.8 taken together represent a bond, or R.sub.3 represents a hydrogen atom or a methoxy group and R.sub.7 and R.sub.8 taken together represent a bond; R.sub.4 represents a hydrocarbon group having from 1 to 4 carbon atoms; R.sub.5 represents a hydrogen atom or a hydrocarbon group having from 1 to 4 carbon atoms or a phenyl group; X represents an oxygen or sulphur atom or an imino group, R.sub.9 represents a hydrogen atom and B represents a cyano, a C.sub.2 -C.sub.5 alkoxycarbonyl or carbamoyl group, or R.sub.

Abstract: A biologically active compound can be solubilized by reaction in different sequences to form a derivative carrying the active moiety, a linking group such as an optionally substituted diisocyanate radical, a polyether moiety such as a polyoxyethylene radical, and a terminal group such as a butyl radical, e.g. ##STR1## n=1 to 400. The active materials can be agricultural chemicals, pharmaceuticals, and the like.

Abstract: Mono, difluoro or trifluoroalkyl esters of 1-substituted-6-C.sub.1-4 straight chain alkyl (or allyl)-ergoline-8.beta.-carboxylic acid, useful as 5HT.sub.2 receptor antagonists.

Abstract: Cycloalkyl or ketocycloalkyl esters of 1-substituted-6-C.sub.1-4 straight chain alkyl (or allyl)-ergoline-8.beta.-carboxylic acids, useful as 5HT.sub.2 receptor antagonists.

Abstract: 9-thia ergot cyclic peptide alkaloids produced by fermentation or synthetic methods have interesting anti-parkinson and other pharmacological activities.

Abstract: Ergoline derivatives of formula: ##STR1## wherein n=0,1,2; R.sub.1 =H, CH.sub.3 ; R.sub.2 =H, CH.sub.3, halogen; R.sub.3 =H, OCH.sub.3 ; R.sub.4 =hydrocarbon group and R.sub.5 is a residue of general formula II, III, IV, V, VI, VII: ##STR2## wherein R.sub.6 =H, Cl, OCH.sub.3, NR.sub.11 R.sub.12, wherein R.sub.11 and R.sub.12 =H, lower alkyl; phenyl or are bonded together to form a heterocyclic ring, R.sub.7, R.sub.8 and R.sub.9 and R.sub.10 =H or C.sub.1 -C.sub.3 alkyl, with the proviso that if R.sub.5 is of formula II and R.sub.2 =R.sub.7 =R.sub.8 =H, then R.sub.4 is not methyl or n is not 0.Pharmaceutically acceptable acid addition salts are also provided. A method for their preparation is also provided.The compounds have anti-depressive, anti-hypertensive and antiprolactin activity.

Abstract: There are provided ergoline derivatives of the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group, R.sub.2 represents a hydrogen or halogen atom or a methyl group, R.sub.3 represents a hydrogen atom or a methoxy group, R.sub.4 represents a hydrocarbon group having from 1 to 4 carbon atoms; each of X and W independently represents a hydrogen atom, a methyl group, a chlorine atom or a methoxy group, and n is 0, 1 or 2. A method for their preparation is also provided. The compounds have strong antiprolactin activity.

Abstract: The present invention provides an improved process for the production of a compound of formula I ##STR1## wherein R.sub.1 is carboxyl, alkoxy(C.sub.1-5)carbonyl, amido, alkyl(C.sub.1-5)amido, di(alkyl(C.sub.1-5)amido or an amido radical of formula II ##STR2## wherein R.sub.a is alkyl(C.sub.1-4),R.sub.b is alkyl(C.sub.1-4) or benzyl, andR.sub.2 is hydrogen or alkyl(C.sub.1-4), andeitherR.sub.3 is hydrogen and R.sub.4 is hydrogen or alkoxy(C.sub.1-4)orR.sub.3 and R.sub.4 together are a single bond,characterized in that a compound of formula III ##STR3## wherein R.sub.1 to R.sub.4 are as defined above,is brominated with a bromine complex of 3-bromo-6-chloro-2-methyl-imidazo[1,2-b]pyridazine.