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Class 546/68 - Chalcogen or nitrogen bonded directly to ring carbon of the six-membered hetero ring


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein chalcogen (i.e., oxygen, sulfur, selenium,
No. of patents: 90
Last issue date: 03/28/2006


1      
NumberTitleIssue Date
7019140Process for the synthesis of pergolide
A process for the synthesis of pergolide (Formula (I)) (D-6-n-propyl-8βmethylmercaptomethylergo line) from acid 9,10-dihydrolysergic is herein disclosed. The process can be carried out without isolating most intermediates and is particularly convenient both from th...
03/28/2006
6777406Substituted pyrroloquinolines and pyridoquinolines as serotinin agonists and antagonists
The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein is R1, R6a, R6b, R7
08/17/2004
6476021Compounds having cGMP-PDE inhibitory effect
Novel fused tetracyclic heterocyclic compounds having a potent and highly selective effect of inhibiting cyclic GMP phosphodiesterase (cGMP-PDE) and a high safety; a process for producing the same; drugs characterized by containing at least one of these c...
11/05/2002
6388079Process for preparing pergolide
This invention relates to a process for preparing pergolide, which comprises the steps of reacting 9,10-dihydrolysergol with an acid anhydride at an elevated temperature in the presence of a catalyst to form a triacylated product intermediate; reducing th...
05/14/2002
6087371Heterocyclyl-ergoline derivatives as 5-HT1A receptor ligands
Ergoline derivative having formula (I) wherein R1 is hydrogen atom or C1-4 alkyl group; R2 is hydrogen, chlorine, or bromine atom, methyl or C1-4 alkylthio group; n is 0, 1 or 2; the substituent at position 8 is...
07/11/2000
6060483Antineurodegenerative ergoline derivatives
The present invention provides the new use in the treatment of neurodegenerative diseases with ergoline derivatives of formula (I) ##STR1## wherein R1 represents a hydrogen atom or a linear or branched C1 -C5 alkyl or...
05/09/2000
5495032Process for producing 7-(substituted)-8-(substituted-9-[(substituted glycyl)amido]-6-demethyl-6-deoxytetracyclines
The invention provides a process for the production of compounds of the formula: ##STR1## wherein, R, R3, R4, X and W are defined in the specification in which a compound of the following formula: ##STR2## is reacted w...
02/27/1996
5463060One-pot process
Pergolide is produced from 8,9-dihydroelymoclavine by a one-pot process in which it is reacted successively with 1-iodopropane, with a sulfonyl halide, and with an alkali metal thiomethoxide without isolation of intermediate products....
10/31/1995
5430031Serotoninergic ergoline derivatives
The present invention provides compounds of the formula (I) ##STR1## wherein A, R1, R2 and R3 are defined as in the specification, or a pharmaceutically acceptable salt thereof. A process for their preparation and the...
07/04/1995
54119662, 13-disubstituted ergolines, their production and use in pharmaceutical agents
Compounds of formula I and their acid addition salts ##STR1## in which R2 R6 R13 and X have the meanings defined herein are described as well as a process and intermediates for their production, and pharmaceutical age...
05/02/1995
54017482,14-disubstituted ergolines, their production and use in pharmaceutical compositions
2,14-Disubstituted ergolines of formula I ##STR1## in which R, R2, R6, R14 and X have the meaning named in the application, as well as their production and use in pharmaceutical agents, are described....
03/28/1995
5242678BR*-diagnostics for monoamine receptors
Compounds of general Formula I labeled with 75 Br, 76 Br, 77 Br, 80m Br or 80 Br isotopes ##STR1## wherein R6 is a C1-6 hydrocarbon residue and C2 C3, ...
09/07/1993
52121788଱-acylamino ergolines and use as pharmaceutical agents
8଱-acylamino ergolines are useful dopamine agonists....
05/18/1993
51589572-substituted ergolines
2-Substituted ergolines ##STR1## wherein C2 C3 and C9 C10 represent a single of double bond; X is oxygen or sulfur; R2 is C1-10 alkyl, optionally halogen-substituted C2-10 ...
10/27/1992
5097031Steroselective hydrogenation process
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 o...
03/17/1992
5079364t-alkyl ergoline derivatives
t-alkyl eroline derivatives of formula I are produced ##STR1## wherein (R1 =H, OCH3 and R2 H) or (R1 +R2 =a ring bond and R3 =H, optionally substituted nicotinynoyl or 1-oxo-2-cyclopen...
01/07/1992
5077298Novel 8଱-acylaminoergolines
Compounds of formula I ##STR1## wherein R1 is hydrogen or C1-4 alkyl, R2 is hydrogen, chlorine, bromine or methyl, R3 is C1-5 alkyl or C3-5 alkenyl and R4 is C3-7...
12/31/1991
50753188଱-acylaminoergoline, its preparation and pharmaceutical compositions containing it
8଱-Acylaminoergoline useful in the treatment of psychotic disorders and Parkinson's disease....
12/24/1991
50378322-substituted ergolines
2-Substituted ergolines ##STR1## wherein C2 C3 and C9 C10 represent a single or double bond; X is oxygen or sulfur; R2 is C1-10 alkyl, optionally halogen-substituted C2-10 ...
08/06/1991
4970314Process for the preparation of 2-bromo-8-ergolinyl compounds
2-bromo-8-ergolinyl compounds of the formula ##STR1## wherein R8 is NH2, NH--CONEt2, CONH2, ##STR2## and ##STR3## wherein R1 =C1-4 -alkyl and R2 =C1-4 ...
11/13/1990
4968801Process for the production ergoline derivatives
Ergoline derivatives of general Formula I ##STR1## wherein C8 C9 and C9 C10 are both CC-single bonds or one is a C.dbd.C-double bond, R6 is C1-4 alkyl, R8 is methyl, hydroxym...
11/06/1990
49506722-substituted-8଱-branched chain acylaminoergolines
Compounds of the formula I ##STR1## wherein R1 is hydrogen or C1-4 alkyl, R2 is hydrogen, chlorine, bromine or methyl, R3 is C1-5 alkyl or C3-5 alkenyl and R4 is C3-7
08/21/1990
4939258Cycloalkanol esters of dihydrolysergic acid
Cycloalkyl or ketocycloalkyl esters of 1-substituted-6-C1-4 straight chain alkyl (or allyl)-ergoline-8ଲ-carboxylic acids, useful as 5HT receptor antagonists....
07/03/1990
4927926Derivatives of 7-(1-azetidinyl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids, their preparation and application as medicines
The present invention relates to new heterocyclic compounds, derivatives of 7-(1-azetidinyl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids, characterized in that they correspond to formula (I) ##STR1## The invention also relates to the preparation of...
05/22/1990
4910302Psychotropic polycyclic imides
Compounds of the formula: ##STR1## in which Z is ##STR2## wherein X is alkylene, ethanylene or alkylidene; Q is alkylene, alkylidene, ##STR3## or Q, taken together with the carbon atoms to which it is attached forms a benzene ring...
03/20/1990
4908449Process for preparing N-methyl derivatives of lysergol and 10଱-methoxylumilysergol
A process for preparing 1-methyllysergol or 10଱-methoxy-1-methyllumilysergol, which comprises adding a base, which is an alkali metal hydride or alcoholate, to a solution of lyergol or 10଱-methoxylumilysergol in a polar aprotic solvent in such...
03/13/1990
48747681,2-disubstituted ergolines useful for producing central antidopanminergic or 댒-receptor-blocking activity
The disclosure relates to 1,2-substituted ergoline derivatives of general Formula I ##STR1## wherein X is an oxygen or sulfur atom, R1 is a lower alkyl group, R2 is halogen, acyl, a saturated or unsaturated lower alkyl group whi...
10/17/1989
486392912- and 13-substituted ergoline derivatives having alpha2 -receptor-blocking effect
Novel 12- and 13-substituted ergoline derivatives are suitable, e.g., as psychopharmaceuticals and for hypertension therapy....
09/05/1989
4859678N-oxide ergolines as antihypertensive agents
An ergoline derivative of the formula I: ##STR1## wherein R1 represents hydrogen or a methyl group; R2 represents hydrogen or a halogen atom, a methyl, cyano or phenyl group or an alkylthio group having from 1 to about 4 carbon ...
08/22/1989
4857298I*-diagnostics for monoamine receptors using ergolines
Compounds of general Formula I labeled with 121 I, 122 I, 123 I, 124 I, 125 I, 131 I and 132 I isotopes ##STR1## wherein R6 is a C1-6 aliphatic hydrocarbon ...
08/15/1989
4853390(2-Haloergolinyl)-N'-N'-diethylurea compounds useful as medicinal agents E.G., as neuroleptics
(2-Haloergolinyl)-N',N'-diethylurea derivatives of Formula I ##STR1## and the salts thereof, wherein R is hydrogen, alkyl of up to 6 carbon atoms, or alkenyl of up to 3 carbon atoms, X is halogen, ##STR2## is a CC single or CC double bond, and ...
08/01/1989
48472622-substituted ergolines having neuroleptic and antidepressant activities
Novel ergoline derivatives, substituted in the 2-position, of the formula ##STR1## wherein C8 ---C9 and C9 ---C10 each independently is a CC-single or a C.dbd.C-double bond, but not together a cumulated double ...
07/11/1989
4841056Substituted hexahydro-4H-indolo[6,5,4-cd]indoles
There are disclosed intermediates to pharmaceutical compounds of the formula ##STR1## in which R1 is an aliphatic or aromatic function, and R2 and R3 are each hydrogen, C1-4 alkyl or a protecting group; and...
06/20/1989
48268512-substituted ergoline urea and thio-urea derivatives having neurolyptic/dopaminergic activity
Novel 2-substituted ergolinyl urea and thioruea derivatives are disclosed, as well as their use as pharmaceuticals, specifically as neuroleptics. The compounds, which possess central dopaminergic activity, have the formula ##STR1## wherein X is an ox...
05/02/1989
4826852Novel ergolinyl compounds nitrogen-substituted in the 8-position, useful for treating dopamine deficiency
Ergolinyl compounds which are nitrogen-substituted in the 8-position and have Formula (I) ##STR1## and physiologically compatible salts thereof, wherein (a) R1 is hydrogen, the 8-substituent can be in the ଱- or ଲ-position and ...
05/02/1989
4816587Process for the preparation of 2-halogenated ergoline derivatives
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...
03/28/1989
4801714Process for the preparation of ergolinylthioureas
Ergolinylthioureas derivatives of the general Formula I ##STR1## wherein R1 is hydrogen, lower alkyl or acyl, R2 is hydrogen, halogen or a lower alkylthio group R3 is lower alkyl, R4, R5 and R6,...
01/31/1989
47911152,6-dimethyl-8଱-pivaloylamino-9,10-didehydro-ergoline
Compounds of formula I ##STR1## wherein R1 is hydrogen or C1-4 alkyl, R2 is hydrogen, chlorine, bromine or methyl, R3 is C1-5 alkyl or C3-5 alkenyl and R4 is C1-7...
12/13/1988
4791116N,N-diethyl-N'-[(8଱)-1-ethyl-6-methyl-ergolin-8-yl]-sulfamide useful as prolactin secretion inhibitor, anti-parkinson agents and anti-depressant agents
The present invention provides N,N-Diethyl-N'-[(8଱)-1-ethyl-6-methyl-ergolin-8-yl]-sulfamide, and N,N-Diethyl-N'-[(8଱)-1-isopropyl-6-methyl-ergolin-8-yl)-sulfamide useful as prolactin secretion inhibiton, anti-parkinson agents and anti-de...
12/13/1988
47726101-alkyl ergolinylthiourea derivatives and their use as antidepressant agents
Novel 1-alkyl ergolinylthiourea derivatives of the general formula ##STR1## wherein R1 is C1-6 alkyl, R2 and R3 are C1-4 alkyl, R4 is hydrogen or C1-4 alkyl and C9---- C
09/20/1988
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