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公开(公告)号:CA1124718A
公开(公告)日:1982-06-01
申请号:CA300288
申请日:1978-04-03
Applicant: DEGUSSA
Inventor: KLEEMANN AXEL , JAKOVLEV VLADIMIR , THIEMER KLAUS , ENGEL JURGEN
IPC: C07D295/08 , A61K31/495 , A61K31/496 , A61P25/18 , A61P25/20 , C07D213/74 , C07D213/80 , C07D295/033 , C07D295/088 , C07D295/092 , C07D295/135 , C07D303/24 , C07D307/68 , C07D333/38 , C07D401/00
Abstract: The present invention provides 1-3-(3,4,5-trimethoxy-phenoxy)-2-hydroxypropyl!-4-aryl piperazine derivatives. The derivatives have the formula in which R1 in a hydrogen atom, a C2 to C6-alkanoyl radical, 3,4,5-trimethoxy benzoyl radical, a nicotinoyl radical or a thienyl carbonyl radical and R2 represents a phenyl, naphthyl or pyridyl radical which may be substituted by the radicals R3 and R4, the radicals R3 and R4, which may be the same or different, each representing hydrogen, hydroxyl, fluorine, chlorine, bromine, a nitro group, a trifluoromethyl group, a C1 to C6-alkyl radical, a C1 to C6-alkoxy radical, a C1 to C6alkyl thio radical, a C2 to C6-alkanoyl radical, an amino group, a C2-C6-alkanoyl-amino group, a C2-C6-alkanoyl-oxy group, a benzoyl-oxy group, a cyclohexyl-carbonyl-oxy group or a thienylcarbonyl-oxy group, pharmaceutically acceptable, and to salts of their compounds. The compounds are pharmacodynamically active and show, for example, a pronounced anti-aggressive action together with neuroleptic properties, anti-convulsive and hypnotic effects being in evidence to a very limited extent only, if at all. In addition, the compounds show fever-reducing and oedemainhibiting effects.
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公开(公告)号:AU521928B2
公开(公告)日:1982-05-06
申请号:AU4709479
申请日:1979-05-16
Applicant: DEGUSSA
Inventor: ENGEL JURGEN , KLEEMANN AXEL , POSSELT KLAUS , STROMAN FRITZ , THIEMER KLAUS
IPC: A61K31/135 , A61K20060101 , A61K31/13 , A61K31/137 , A61K31/43 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P29/00 , C07C20060101 , C07C67/00 , C07C213/00 , C07C213/02 , C07C213/08 , C07C215/30 , C07C215/60 , C07C221/00 , C07C225/06 , C07C225/10 , C07C225/14 , C07C97/10
Abstract: There are prepared compounds of the formula: wherein X is the group >C=O or >CH(OH), Y is the group R2 is hydrogen or C1 to C6 alkyl, R3 is hydrogen or a hydroxy group and R1 is the adamantyl group or a saturated or single unsaturated C3 to C16 cycloalkyl group where the C3 to C16 cycloalkyl group can be substituted by a C1-C4 alkyl group or a halogen atom and their salts. The compounds are useful in dilating the peripheral blood vessels and in lowering blood pressure.
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33.
公开(公告)号:IN149393B
公开(公告)日:1981-11-28
申请号:IN849CA1979
申请日:1979-08-16
Applicant: DEGUSSA
Inventor: KIEL REINHOLD , KLEEMANN AXEL , NUBERT INGOMAR
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公开(公告)号:DD148775A5
公开(公告)日:1981-06-10
申请号:DD21847080
申请日:1980-01-15
Applicant: DEGUSSA
Inventor: ENGEL JUERGEN , KLEEMANN AXEL , STROMAN FRITZ , ACHTERRATH-TUCKERMANN UTE , THIEMER KLAUS
IPC: C07D333/00 , C07D409/14
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公开(公告)号:CA1096380A
公开(公告)日:1981-02-24
申请号:CA294846
申请日:1978-01-12
Applicant: DEGUSSA
Inventor: KLEEMANN AXEL , NUBERT INGOMAR , STROMAN FRITZ , THIEMER KLAUS
IPC: C07D333/24 , A61K31/38 , A61K31/381 , A61P9/08 , C07D333/16 , C07D333/20 , C07D409/14
Abstract: The present invention provides compounds of the general formula I wherein has either the structure or the structure , Alk represents a straight or branched C1-C5-alkylene group and Y a C3-C7-cycloalkyl radical, a methylenedioxy-benzyl radical, a benzyl radical which is singly, doubly or triply substituted by C1-C4-alkoxy groups, or it represents a straight or branched C1-C6-alkyl radical substituted by a di-C1-C4-alkyl-amino group, a morpholino group, or it represents the radical wherein R represents a C1-C4-alkyl group and the hydroxyl group can also be acylated by a C2-C6-alkanoyl group or wherein the group -NHY represents the radical and R' represents a phenyl radical, a phenyl radical, which is Aingly or doubly substituted by C1-C4-alkyl groups, C1-C4 alkoxy groups or halogen atoms, a C1-C6-alkyl radical, a C1-C4-oxy-alkyl radical or a phenyl-C1-C4-alkyl radical, which can also be substituted in the phenyl ring by 1 to 3 C1-C4-alkoxy groups or the radical -NH-CH(R)-CH(OH)-C6H5 (wherein R has the meaning defined above) when Alk consists of 2 to 5 carbon atoms or a pharmaceutically acceptable salt thereof. These compounds are pharmaceutically effective, particularly in the case of heart and circulation disorders. In particular, they cause an increase of the peripheral and cerebral blood flow.
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公开(公告)号:CA1093086A
公开(公告)日:1981-01-06
申请号:CA293092
申请日:1977-12-14
Applicant: DEGUSSA
Inventor: KLEEMANN AXEL , KIEL REINHOLD , NUBERT INGOMAR
IPC: C07D333/14 , A61K31/382 , C07D333/16 , C07D333/20 , C07D409/06
Abstract: The present invention provides a process for the production of 1,1-dithien-(3)-yl-1-hydroxy-(3)-propyl!-1-phenyl-1-hydroxy-(2)-propyl !-amine, which comprises condensing thien-(3)-yl lithium with a .beta.-halogen propionic acid alkyl ester corresponding to the formula II in which R is a lower saturated aliphatic alkyl group and Hal is chlorine, bromine or iodine, in an inert medium at a temperature below -50.degree.C, after which the resulting compound corresponding to the formula III in which Hal is chlorine, bromine or iodine, is reacted with 2-amino-1-hydroxy-1-phenylpropane in an inert medium in the presence of a basic compound.
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公开(公告)号:NO792874L
公开(公告)日:1980-03-07
申请号:NO792874
申请日:1979-09-05
Applicant: DEGUSSA
Inventor: KLINGLER KARL-HEINZ , KLEEMANN AXEL , STROMAN FRITZ , THIEMER KLAUS
IPC: A61K31/403 , A61K31/155 , A61K31/405 , A61P25/02 , A61P27/02 , C07C67/00 , C07C239/00 , C07C279/04 , C07C279/12 , C07D209/08 , C07D209/43 , C07D209/86 , C07D209/88 , C07C
Abstract: Compounds corresponding to the formula I are disclosed, wherein Alk represents a C2-C5-alkylene groups optionally substituted by a hydroxy group and Ar represent an optionally substituted phenyl, naphthyl, tetrahydronaphthyl, indanyl or indenyl radical or a monocyclic or condensed bicyclic or tricyclic heterocyclic radical which is optionally substituted, the heterocyclic radical consisting of individual rings having 5 or 6 members and optionally containing from 1 to 4 hetero atoms, and the acid addition salts thereof. A process for producing these compounds is also disclosed. These substituted aminoalkyl guanidines block the beta -receptors of the adrenergic nerve system, and also reduce blood pressure.
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公开(公告)号:CA1061355A
公开(公告)日:1979-08-28
申请号:CA226929
申请日:1975-05-14
Applicant: DEGUSSA
Inventor: KLEEMANN AXEL , KOLB HEINZ , SCHREYER GERD
IPC: C07D301/00 , B01J23/00 , B01J31/00 , C07B61/00 , C07D303/04 , C07D303/16 , C07D303/44
Abstract: The present invention provides a process for producing glycidyl methacrylate which comprises the transesterification of methyl methacrylate with glycide in the presence of a catalyst selected from an alkali metal or an alkali metal compound. The methanol being formed during the reaction being immediately distilled off.
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公开(公告)号:AU3239278A
公开(公告)日:1979-07-19
申请号:AU3239278
申请日:1978-01-12
Applicant: DEGUSSA
Inventor: KLEEMANN AXEL , NUBERT INGOMAR , STROMAN FRITZ , THIEMER KLAUS
IPC: C07D333/24 , A61K31/38 , A61K31/381 , A61P9/08 , C07D333/16 , C07D333/20 , C07D409/12 , C07D413/12 , A61K31/495 , A61K31/535
Abstract: There are prepared compounds of the formula (I) where >A-B- has either the structure >C(OH)-CH2- or the structure >C=CH, Alk is a straight or branched chain C1-C5-alkylene group and Y is where R is hydrogen or a C1-C4-alkyl group and T is hydrogen or a C2-C6-alkanoyl group where R' is hydrogen, phenyl, phenyl substituted once or twice. The compounds are effective in improving peripheral and cerebral circulation. There are also produced intermediate compounds of formula (II) where NHY is replaced by chlorine, bromine or iodine.
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公开(公告)号:AU3239178A
公开(公告)日:1979-07-19
申请号:AU3239178
申请日:1978-01-12
Applicant: DEGUSSA
Inventor: KLEEMANN AXEL , KIEL REINHOLD , NUBERT INGOMAR
IPC: C07D333/14 , A61K31/382 , C07D333/16 , C07D333/20
Abstract: [1,1-dithien-(3)-yl-1-hydroxy-(3)-propyl]-[1-phenyl-1-hydroxy-(2)-prop yl]-amine is prepared by condensing thien-(3)-yl lithium with a beta -halogen propionic acid alkyl ester of the formula (II) where R is a lower alkyl group and Hal is chlorine, bromine or iodine, in an inert medium at a temperature below -50 DEG C. to form a compound of the formula (III) which is then reacted with 2-amino-1-hydroxy-1-phenylpropane in an inert medium in the presence of a basic compound. The product cn be converted to [1,1-dithien-(3)-yl-(1)-propen-(3)-yl]-[1-phenyl-(2)-propyl]-amine by dehydration.
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