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101. 发明专利

FI761004A 未知
公开(公告)号：FI761004A
公开(公告)日：1976-10-19
申请号：FI761004
申请日：1976-04-13
申请人： BOEHRINGER MANNHEIM GMBH
发明人： STACH KURT , BOSIES ELMAR , HEERDI RUTH , KUEHNLE HANS-FRIEDER , SCHMIDT FELIX HELMUT
IPC分类号： C07D209/42 , A61K31/165 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/51 , C07C233/54 , C07C233/55 , C07C233/81 , C07C233/87 , C07C235/20 , C07C235/24 , C07C235/34 , C07C235/36 , C07C235/38 , C07C235/52 , C07C235/56 , C07C237/20 , C07C237/36 , C07C237/40 , C07C313/00 , C07C319/20 , C07C323/60 , C07D213/82 , C07D215/48 , C07D241/24 , C07D261/18 , C07D263/58 , C07D307/79 , C07D311/66 , C07D333/38 , C07C
摘要： Procedure for the preparation of derivatives of phenylalkanocarboxylic acids of the general formula I ** (See formula) ** wherein A is an aryl, aralkoxy or aryl vinyl radical optionally substituted by hydroxy, halogen, with trifluoromethyl, alcoholic, alcoholic mercapto, alkoxy, alkenyloxy, alkoxyalkoxy, amino substituted by alcohol, aryloxy or aryloxy substituted by alkoxy, aryloxyalkoyl or aryl radicalcoyl radicals., or a heterocyclic ring system optionally substituted with halogen, or with alcohol or alkoxy groups; Y means a valence line or a lower alcohol group with 1 to 3 carbon atoms, possibly branched; X signifies a saturated or unsaturated, straight-chain or branched alcoholic chain with 2 to 8 carbon atoms, at least 2 carbon atoms must be between the benzene ring and the carboxyl group; and R represents hydrogen or lower alcohol; as well as its physiologically safe salts, esters and amides, characterized in that a) an amine of the general formula II is reacted ** (See formula) ** wherein Y, X and R have the above specified meanings, or their acid derivatives, with an acid reactive acid derivative of A-COOH, where A has one of the above indicated meanings; or b) a compound of the general formula III is oxidized ** (See formula) ** wherein A, Y, R and X have the meanings indicated above and B represents a radical capable of being transformed into the carboxyl group; or c) a compound of the general formula IV is reduced ** (See formula) ** where A, R and Y have the meanings specified above, Z means an alcohol chain with 1 to 7 -carbon- atoms, saturated or unsaturated, straight or branched chain, Z'is equal to Z or a valence line, R'signifies hydrogen or an alcoholic group and G signifies the group (see formula) or the group (see formula) -CH-, where L represents the hydroxy or halogen group; or d) a compound of the general formula V is reacted ** (See formula) ** where A, R and Y have the meanings indicated above, M stands for hydrogen or lower alcohol with 1 to 6 carbon atoms, and K represents a valence line or an alcohol chain with 1 to 6 carbon atoms, saturated or unsaturated, straight-chain or branched, with a reactive methylene component of the general formula VI ** (See formula) ** where P represents hydrogen, an alkali metal, lower alcohol or acyl group and Q represents hydrogen, the nitrile group, lower alcohol with 1 to 6 carbon atoms, or the radical -COOP, where P has the meanings above indicated, then saponifying, decarboxylating or hydrogenating, if appropriate, the obtained unsaturated compound; or e) in the event that X in the general formula I represents a saturated straight or branched chain 2 to 4 carbon alcohol chain, a compound of the general formula VII is reacted ** (See formula) ** wherein A, R and Y have the meanings set forth above, and M1 signifies hydrogen or lower alcohol with 1 to 2 carbon atoms, with a compound of the general formula VIII H2c = CHal2 where Hal means halogen; or of) in the event that X in the general formula I represents a saturated, straight-chain alcoholic chain with 2 to 4 carbon atoms, it is reacted under the conditions of the "Willqerodt-Kindler synthesis", a ketone of the general formula IX ** (See formula) ** where A, R and Y have the meanings indicated above and U represents an alcoholic group with 2 to 4 carbon atoms; or g) a halogenated compound of the general formula X is reacted ** (See formula) ** in which A, R, Y, K and Hal have the meanings indicated above and T can be hydrogen or lower alcohol with 1 to 6 carbon atoms, with a reactive methylene component of the general formula XI ** (See formula) ** wherein R2 represents lower alcohol, R1 represents hydrogen or lower alcohol with 1 to 6 carbon atoms, Me represents alkali or alkaline earth metals and W represents OR2 radical or methyl group, is saponified and eventually decarboxylated, and then, optionally, the acid derivatives of the general formula I obtained are transformed into the free acid or, if desired, the free acid obtained from the general formula I is esterified, transformed into an amide or physiologically compatible acid addition salts. (Machine-translation by Google Translate, not legally binding)

102. 发明专利

FI760579A 未知
公开(公告)号：FI760579A
公开(公告)日：1976-09-13
申请号：FI760579
申请日：1976-03-05
申请人： BOEHRINGER MANNHEIM GMBH
发明人： BRAUN FRANZ , STACH KURT , THIEL MAX , SPONER GISBERT , DIETMANN KARL
IPC分类号： D07B3/00 , H01B13/02 , C07C

103. 发明专利

FI51354B 未知
公开(公告)号：FI51354B
公开(公告)日：1976-08-31
申请号：FI193067
申请日：1967-07-12
申请人： BOEHRINGER MANNHEIM GMBH
发明人： WINTER WERNER , THIEL MAX , STACH KURT , SCHAUMANN WOLFGANG , DIETMANN KARL
IPC分类号： C07D313/12 , C07D337/12
摘要： 1,134,589. Aminoalkyl derivatives of 6,11- dihydro - dibenzo - [b,e] - oxepine and -thiepine. C. F. BOEHRINGER & SOEHNE G.m.b.H. 13 July, 1967 [14 July, 1966], No. 32335/67. Heading C2C. Novel compounds (and salts thereof) possessing cardiac and circulatory actions of the general formula wherein X represents oxaethylene or thiaethylene, R 1 is a hydrogen or halogen atom or an alkyl, alkoxy, or -CF 3 radical, R 2 is a hydrogen atom or a hydroxyl group, R 3 is a hydrogen atom or, together with R 2 , represents a further valency bond, R 4 and R 5 which may be the same or different, are hydrogen atoms or C 1-3 alkyl radicals, A is an alkylene chain, which may be substituted by alkyl or aryl radicals and which, when Y represents a valency bond, can also carry a hydroxyl group or an acylated hydroxyl group, Y represents a valency bond or an oxygen or sulphur atom or an imino group, which may be alkylated, and Z is an aryl, aralkyl or cycloalkyl radical which may be substituted by halogen atoms, hydroxyl groups or alkoxy, alkyl or -CF 3 radicals, are prepared: (a) by condensing compounds of general formulµ (a reactive derivative of the acid is used) with a compound of general formula R 5 .NHAYZ; or (b) by condensing an amine of general formula with a carbonyl compound, H-A 1 YZ, in which A 1 is the same alkylene chain as A except that it contains a carbonyl group in place of a methylene group (includes aldehydes, ketones and reactive carboxylic acid derivatives related to said aldehydes), followed both in case (a) and (b) by reduction of the intermediate azomethine or acid amide and thereafter by optional N-alkylation. 11 - Hydroxy - 6,11 - dihydro - dibenzo - [b,e]- oxepin - 11 - yl - acetic acid tert. - butyl ester (obtained by condensing 6,11-dihydro-dibenzo- [b,e] - oxepin - 11 - one with tert. - butyl acetate) treated with glacial acetic acid and 48% hydrobromic acid yields 6,11-dihydrodibenzo - [b,e] - oxepin - 11 - ylidene - acetic acid whereas treatment with alcoholic hydrochloric acid yields 6,11-dihydro - dibenzo - [b,e]- oxepin - 11 - ylidene - acetic acid tert. - butyl ester, reduction of which affords 6,11-dihydrodibenzo - [b,e] - oxepin - 11 - yl - acetic acid tert. - butyl ester from which may be obtained the corresponding free acid.

104. 发明专利

AU7826975A NEW AMINE DERIVATIVES OF AZIDOPHENOLS 未知
公开(公告)号：AU7826975A
公开(公告)日：1976-08-19
申请号：AU7826975
申请日：1975-02-17
申请人： BOEHRINGER MANNHEIM GMBH
发明人： KAMPE WOLFGANG , STACH KURT , THIEL MAX , BARTSCH WOLFGANG , DIETMANN KARL
IPC分类号： C07C247/16 , A61K20060101 , A61K31/13 , A61K31/135 , A61K31/655 , A61P9/00 , C07C20060101 , C07C67/00 , C07C217/32 , C07C241/00 , C07D303/22 , A61K27/00 , C07C93/06

105. 发明专利

AU7826875A 1-%3-%NAPHTH-1-YLOXY<-2-HYDROXYPROPYL-<-PIPERAZINE DERIVATIVES 未知
公开(公告)号：AU7826875A
公开(公告)日：1976-08-19
申请号：AU7826875
申请日：1975-02-17
申请人： BOEHRINGER MANNHEIM GMBH
发明人： WITTE ERNST-CHRISTIAN , STACH KURT , THIEL MAX , SPONER GISBERT , ROESCH EGON
IPC分类号： C07D295/08 , A61K31/495 , A61P9/12 , C07D295/088 , C07D295/092 , C07D295/096 , A61K27/00 , C07D51/70
摘要： New 1-[3-(naphth-1-yloxy)-2-hydroxypropyl]-piperazine compounds of the formula: (I) and the pharmacologically compatible salts thereof are outstandingly effective in lowering blood pressure and are thus useful as anti-hypertensive agents.

106. 发明专利

AU7591574A QUINOLONE DERIVATIVES 未知
公开(公告)号：AU7591574A
公开(公告)日：1976-06-03
申请号：AU7591574
申请日：1974-11-29
申请人： BOEHRINGER MANNHEIM GMBH
发明人： RHOMBERG ALFRED , MERDES HARTMUT , STACH KURT , VOMEL WOLFGANG
IPC分类号： C07D221/10 , C07D221/16 , C07D39/00 , A61K27/00

107. 发明专利

AU7557574A NEW INDOLE DERIVATIVES 未知
公开(公告)号：AU7557574A
公开(公告)日：1976-05-20
申请号：AU7557574
申请日：1974-11-20
申请人： BOEHRINGER MANNHEIM GMBH
发明人： HEERDT RUTH , HUBNER MANFRED , SCHMIDT FELIX HELMUT , STACH KURT
IPC分类号： C07D209/12 , C07D209/60 , C07D27/56 , A61K27/00 , C07D27/70

108. 发明专利

FI751528A 未知
公开(公告)号：FI751528A
公开(公告)日：1975-12-02
申请号：FI751528
申请日：1975-05-26
申请人： BOEHRINGER MANNHEIM GMBH
发明人： BOSIES ELMAR , STACH KURT , SCHMIDT FELIX HELMUT , HEERDT RUTH , WEBER HELMUT
IPC分类号： C07C279/26 , A61K20060101 , A61K31/155 , C07C20060101 , C07C67/00 , C07C239/00 , C07C

109. 发明专利

FI751093A 未知
公开(公告)号：FI751093A
公开(公告)日：1975-10-18
申请号：FI751093
申请日：1975-04-11
申请人： BOEHRINGER MANNHEIM GMBH
发明人： BERGER HERBERT , GALL RUDI , STACH KURT , VOEMEL WOLFGANG , HOFFMANN RITA
IPC分类号： C07D403/14 , A61K31/5025 , C07D487/04 , C07D
摘要： New nitroimidazolyl-triazolo-pyridazines of the formula:

110. 发明专利

FR2137731B1 未知
公开(公告)号：FR2137731B1
公开(公告)日：1975-10-17
申请号：FR7216718
申请日：1972-05-10
申请人： BOEHRINGER MANNHEIM GMBH
发明人： WITTE ERNST-CHRISTIAN , STACH KURT , THIEL MAX , ROESCH ANDRONIKI , ROESCH EGON
IPC分类号： C07D309/16 , A61K31/35 , A61K31/351 , A61K31/352 , A61K31/495 , A61P3/00 , A61P29/00 , A61P37/08 , C07D309/32 , C07D311/16 , A61K27/00 , C07D99/00
摘要： 1335946 Coumarin-7-yloxyalkyl-piperazine derivatives BOEHRINGER MANNHEIM GmbH 11 May 1972 [14 May 1971] 22070/72 Heading C2C Novel compounds of the Formula (I) wherein R 1 is a hydrogen atom or a C 1-5 alkyl radical, R 2 is a C 1-5 alkyl radical, R 3 is an unsubstituted or substituted phenyl or benzyl radical, the substituents, when present, being halogen atoms or C 1-5 alkyl or C 1-5 alkoxy radicals, and n is 1, 2 or 3; and the pharmacologically compatible salts thereof, may be obtained by (a) condensing a compound of the Formula (II) in which X is a halogen atom, with a 7-hydroxy- 3 - R 1 - 4 - R 2 - substituted - coumarin, (b) condensation of a compound of the Formula (IV) with an R 3 -substituted-piperazine, (c) condensation of a compound of Formula (I), in which R 3 is H, with a compound of the formula X.R 3 , in which R 3 is an unsubstituted or substituted benzyl radical; or (d) condensation of a compound of the Formula (VII) with an amine of formula H 2 N-R 3 , and thereafter, if desired, converting the products into their physiologically compatible salts. Pharmaceutical compositions having antiinflammatory and anti-allergic action comprise at least one compound of the Formula (I) in admixture with a solid or liquid pharmaceutical diluent or carrier, for example in the form of tablets or dragees or suspended or dissolved in water or an oil.

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