专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

21. 发明专利

DK132075C 未知
公开(公告)号：DK132075C
公开(公告)日：1976-03-15
申请号：DK286671
申请日：1971-06-11
申请人： BAYER AG
发明人： WOLLWEBER H , FLUCKE W
IPC分类号： A61K31/155 , A61K31/135 , A61K31/16 , A61K31/165 , A61K31/18 , A61K31/22 , A61K31/325 , A61K31/34 , A61K31/341 , A61K31/42 , A61P33/00 , A61P33/10 , C07C67/00 , C07C239/00 , C07C257/14 , C07C259/14 , C07C271/26 , C07C301/00 , C07C303/38 , C07C303/40 , C07C311/08 , C07D209/42 , C07D215/54 , C07D231/14 , C07D233/90 , C07D241/24 , C07D261/18 , C07D277/56 , C07D307/12 , C07D307/18 , C07D307/20 , C07D307/54 , C07D307/68 , C07D309/08 , C07D333/16 , C07D333/24 , C07D333/38 , C07C123/00
摘要： N-phenylacetamidines with an acylamino or sulphonylamino group introduced into the phenyl nucleus have high anthelmintic activity and are effective even with a single dose against nematodes and cestodes in an amount between 5 and 4,500 mg. A representative compound is N-(4-carbethoxyaminophenyl)-N',N' -dimethyl-acetamidine.

22. 发明专利

ZA745908B NEW N'- (AMINOACYLAMINOPHENYL) - ACETAMIDINES AND SALTS THEREOF, THEIR PRODUCTION, AND THEIR MEDICAL USE 未知
公开(公告)号：ZA745908B
公开(公告)日：1975-09-24
申请号：ZA745908
申请日：1974-09-17
申请人： BAYER AG
发明人： WOLLWEBER H , THOMAS H , ANDREWS P , NIEMERS E , SCHULZ H
IPC分类号： A61K31/165 , A61K31/155 , A61K31/40 , A61K31/495 , A61K31/535 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C239/00 , C07C257/14 , C07C257/20 , C07D295/15 , C07C , A61K
摘要： A new class of N'-(aminoacylaminophenyl) acetamidines: in which R1 and R2 are the same or different and represent hydrogen, alkyl, aryl or the substituted derivatives thereof or, together with the nitrogen atom to which they are attached, an heterocyclic ring; and R3 is hydrogen, alkyl, aryl, aralkyl, or a heterocyclic moiety including the substituted derivatives thereof. The products have utility as anthelmintics.

23. 发明专利

SE370939B 未知
公开(公告)号：SE370939B
公开(公告)日：1974-11-04
申请号：SE759871
申请日：1971-06-11
申请人： BAYER AG
发明人： WOLLWEBER H , FLUCKE W
IPC分类号： C07D223/12 , A61K31/40 , A61K31/445 , A61P9/12 , A61P33/10 , C07D203/00 , C07D207/08 , C07D207/22 , C07D211/00 , C07D211/72 , C07D225/02 , C07D27/04
摘要： 1325528 Aminophenyl - cycloamidine derivatives BAYER AG 11 June 1971 [13 June 1970] 27494/71 Heading C2C Novel aminophenyl-cycloamidine derivatives (1) wherein R is a hydrogen atom or a straight or branched chain alkyl, alkenyl or alkynyl group, which can be substituted by a halogen atom or an alkoxy or hydroxy group; R 2 is a -COR 4 or -SO 2 R 5 group [in which R 4 is a hydrogen atom; a straight or branched chain alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, alkoxyalkoxy, alkoxyalkyl or alkoxy group, which can be substituted by a chlorine atom or by a hydroxy, cyano or oxo group; a cycloalkyl group or a cycloalkenyl group containing one or two double bonds, which groups can be substituted by one or more alkyl groups; a cycloalkylalkyl, tetrahydrofurfuryl, tetrahydrofuryl or tetrahydropyranyl group which can be substituted by one or more alkyl groups; a trifluoromethyl group; a carbalkoxyalkyl group; a cycloalkylalkoxy, cycloalkoxy, or tetrahydrofurylalkoxy group; a phenalkoxy, phenoxyalkoxy, phenoxy, phenylalkyl, phenyl or naphthyl group, the aromatic ring of which can be substituted by one or more alkyl, alkenyl, alkoxy, nitro, trifluoromethyl, cyano, alkylsulphonyl, acylamino and/or alkylsulphonylamino groups and/or halogen atoms; or a heteroaromatic O- and/or N-containing ring system; R 5 is a straight or branched chain alkyl or alkenyl group; a cycloalkyl group; a phenylalkyl, phenyl or naphthyl group, the aromatic ring of which can be substituted by one or more alkyl, alkenyl, alkoxy, nitro, trifluoromethyl, cyano, acylamino, alkylsulphonyl and/or alkylsulphonylamino groups and/or chlorine, bromine or fluorine atoms]; R 3 , R 7 and R 8 , which can be the same or different, are each a hydrogen or halogen atom or a straight or branchedchain alkyl, alkenyl or alkoxy group or a cyano or trifluoromethyl group; R 6 and R 9 , which can be the same or different, are each a hydrogen atom or an alkyl group; and n is 3, 4 or 5; and salts thereof may be prepared by (a) reacting a compound (3) with a lactam or thiolactam (4) in which W is oxygen or sulphur, or with a salt or a reactive derivative thereof especially a lactam; (b) reacting an imide chloride (6) with an amine RNH 2 ; (c) reacting an arylisocyanate (8) with a lactam (9) (d) reacting a carbamic acid chloride (10) with a lactam (9); (e) alkylating a compound (1) in which R is hydrogen with B-R in which B is a reactive ester group or a halogen, and R is as above except hydrogen; or (f) reacting an aminophenyl-cyclo-amidine (13) with an acylating or sulphonating agent R 2 Y where Y is a reactive ester group. The intermediate 2-(4-aminophenyl-imino)-1- methyl-pyrrolidine may be prepared by catalytic hydrogenation of 2 - (4 - nitrophenylimino)- 1-methyl pyrrolidine. Other listed intermediates may be prepared by known methods. Pharmaceutical compositions of the compounds (1) show parasiticide, especially antihelminthic, activity and some have antihypertensive activity when administered orally or parenterally alone or with the usual excipients.

24. 发明专利

SE347967B 未知
公开(公告)号：SE347967B
公开(公告)日：1972-08-21
申请号：SE337868
申请日：1968-02-14
申请人： BAYER AG
发明人： MENG K , HORSTMANN H , WOLLWEBER H
IPC分类号： C07D307/14 , C07D309/04 , C07D309/20 , C07D7/14
摘要： The invention comprises sulphonamides of the formula and salts thereof, wherein R is hydrogen or C1- 4 alkyl, X is a linear or branched alkylene radical of 1-4 carbon atoms and Y is a saturated or mono- or poly-unsaturated furan or pyran radical which may be substituted by C1- 4 alkyl or C1- 6 alkoxyalkyl radicals, including optically active isomers thereof, and processes for their preparation by (a) condensing 3-sulphamoyl-4-chlorobenzene-sulphonyl chloride with an amine R.HN.X.Y in the presence of an acid-binding agent or (b) for the preparation of compounds wherein Y is a saturated pyran or furan ring, by hydrogenating the corresponding mono- or poly-unsaturated furan or pyran compound. Amines of the formula R.HN.X.Y used as starting materials are made by catalytically hydrogenating corresponding aldehydes or ketones in the presence of ammonia or an amine RNH2, followed if required by hydrogenation of the furan or pyran ring. Alternatively a furan carboxylic amide may be reduced to an amine with lithium aluminium hydride or a cyano-furan, e.g. a -methyl-a -cyanofuran, may be hydrogenated and the resulting amine alkylated, giving, for example, a -methyl-a -tetrahydrofurfuryl-methylamine. 2 - Sulphamoyl - 4 - [N - methyl - N - (cyclopentylmethyl)-sulphamoyl]-chlorobenzene is made by reacting cyclopentylmethylamine with formic acid ester to give N-formyl-cyclopentylmethylamine, reacting with lithium aluminium hydride to give N-methyl-cyclopentylmethylamine and reacting with 4-chloro-3-sulphamoylbenzenesulphonyl chloride.

25. 发明专利

NO124431B 未知
公开(公告)号：NO124431B
公开(公告)日：1972-04-17
申请号：NO377068
申请日：1968-09-24
申请人： BAYER AG
发明人： HOFFMEISTER F , KRONEBERG H , HILTMANN R , WOLLWEBER H
IPC分类号： A61K20060101 , C07D213/75 , C07D401/12 , C07D31/42

26. 发明专利

ZA713765B NEW AMINOPHENYLAMIDINES,THEIR PRODUCTION AND THEIR MEDICINAL USE 未知
公开(公告)号：ZA713765B
公开(公告)日：1972-01-26
申请号：ZA713765
申请日：1971-06-10
申请人： BAYER AG
发明人： WOLLWEBER H , FLUCKE W
IPC分类号： C07D223/12 , A61K31/155 , A61K31/275 , A61K31/395 , A61K31/40 , A61P31/04 , A61P33/00 , A61P33/10 , C07C67/00 , C07C239/00 , C07C257/14 , C07C259/14 , C07D207/22 , C07D211/72 , C07D295/195 , C07D295/215 , A61K
摘要： 4-Amino substituted phenylamidine are anthelmintics. The compounds, of which N-(4-aminophenyl)-N',N'-dimethylacetamidine is a representative embodiment, can be prepared through treatment of a 4-amino aniline with a carboxylic acidamide or thioamide, reduction of an appropriately substituted 4-aminophenylamidine, optionally followed by alkylation of the resultant 4-aminophenylamidine, formation of a Schiff base followed by quarternization and hydrolysis, or hydrolysis of a 4-acylaminophenylamidine.

27. 发明专利

ZA713764B NEW AMINOPHENYL-CYCLOAMIDINES,THEIR PRODUCTION AND THEIR MEDICINAL USE 未知
公开(公告)号：ZA713764B
公开(公告)日：1972-01-26
申请号：ZA713764
申请日：1971-06-10
申请人： BAYER AG
发明人： WOLLWEBER H , FLUCKE W
IPC分类号： C07D223/12 , A61K31/40 , A61K31/445 , A61P9/12 , A61P33/10 , C07D203/00 , C07D207/08 , C07D207/22 , C07D211/00 , C07D211/72 , C07D225/02 , A61K
摘要： 1325528 Aminophenyl - cycloamidine derivatives BAYER AG 11 June 1971 [13 June 1970] 27494/71 Heading C2C Novel aminophenyl-cycloamidine derivatives (1) wherein R is a hydrogen atom or a straight or branched chain alkyl, alkenyl or alkynyl group, which can be substituted by a halogen atom or an alkoxy or hydroxy group; R 2 is a -COR 4 or -SO 2 R 5 group [in which R 4 is a hydrogen atom; a straight or branched chain alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, alkoxyalkoxy, alkoxyalkyl or alkoxy group, which can be substituted by a chlorine atom or by a hydroxy, cyano or oxo group; a cycloalkyl group or a cycloalkenyl group containing one or two double bonds, which groups can be substituted by one or more alkyl groups; a cycloalkylalkyl, tetrahydrofurfuryl, tetrahydrofuryl or tetrahydropyranyl group which can be substituted by one or more alkyl groups; a trifluoromethyl group; a carbalkoxyalkyl group; a cycloalkylalkoxy, cycloalkoxy, or tetrahydrofurylalkoxy group; a phenalkoxy, phenoxyalkoxy, phenoxy, phenylalkyl, phenyl or naphthyl group, the aromatic ring of which can be substituted by one or more alkyl, alkenyl, alkoxy, nitro, trifluoromethyl, cyano, alkylsulphonyl, acylamino and/or alkylsulphonylamino groups and/or halogen atoms; or a heteroaromatic O- and/or N-containing ring system; R 5 is a straight or branched chain alkyl or alkenyl group; a cycloalkyl group; a phenylalkyl, phenyl or naphthyl group, the aromatic ring of which can be substituted by one or more alkyl, alkenyl, alkoxy, nitro, trifluoromethyl, cyano, acylamino, alkylsulphonyl and/or alkylsulphonylamino groups and/or chlorine, bromine or fluorine atoms]; R 3 , R 7 and R 8 , which can be the same or different, are each a hydrogen or halogen atom or a straight or branchedchain alkyl, alkenyl or alkoxy group or a cyano or trifluoromethyl group; R 6 and R 9 , which can be the same or different, are each a hydrogen atom or an alkyl group; and n is 3, 4 or 5; and salts thereof may be prepared by (a) reacting a compound (3) with a lactam or thiolactam (4) in which W is oxygen or sulphur, or with a salt or a reactive derivative thereof especially a lactam; (b) reacting an imide chloride (6) with an amine RNH 2 ; (c) reacting an arylisocyanate (8) with a lactam (9) (d) reacting a carbamic acid chloride (10) with a lactam (9); (e) alkylating a compound (1) in which R is hydrogen with B-R in which B is a reactive ester group or a halogen, and R is as above except hydrogen; or (f) reacting an aminophenyl-cyclo-amidine (13) with an acylating or sulphonating agent R 2 Y where Y is a reactive ester group. The intermediate 2-(4-aminophenyl-imino)-1- methyl-pyrrolidine may be prepared by catalytic hydrogenation of 2 - (4 - nitrophenylimino)- 1-methyl pyrrolidine. Other listed intermediates may be prepared by known methods. Pharmaceutical compositions of the compounds (1) show parasiticide, especially antihelminthic, activity and some have antihypertensive activity when administered orally or parenterally alone or with the usual excipients.

28. 发明专利

SE317075B 未知
公开(公告)号：SE317075B
公开(公告)日：1969-11-10
申请号：SE664467
申请日：1967-05-11
申请人： BAYER AG
发明人： WOLLWEBER H , HORSTMANN H , MENG K
IPC分类号： C07D207/26 , C07D211/02 , C07D211/76 , C07D211/78 , C07D27/02
摘要： 1,140,008. Disulphonamides. FARBENFABRIKEN BAYER A.G. 8 May, 1967 [12 May, 1966], No. 21283/67. Heading C2C. Novel disulphonamides (and salts thereof) of the general formula (and also the corresponding compounds wherein the heterocyclic ring is broken between the members N and X and accordingly the resulting nitrogen bond is satisfied by a hydrogen atom and X is a carboxy (-COOH) group) wherein R is H or Me, R 1 is H or C 1-4 alkyl, R 11 is H, C 1-4 alkyl, alkoxyalkyl, aryl or aralkyl, X is carbonyl or methylene and n is 0 or 1 are prepared by the interaction of 4-chloro-3-sulphonamido-benzenesulphochloride and the appropriate aminomethyl- or methylamino -compound. Pharmaceutical compositions having diuretic and saluretic activity, and suitable for the treatment of hypertension, contain as the active ingredient the above novel compounds and are preferably administered parenterally in the form of capsules, tablets, pills, powder, granulates or suppositories and ampoules or drops. N - # - Methoxyethyl -, N - benzyl - and N - #- phenethyl - 5 - methyl - 5 - cyano - pyrrolidone- (2) are prepared by the interaction of laevulinic acid ethyl ester cyanohydrin and #-methoxyethylamine, benzylamine or #-phenethylamine respectively. Reduction of the cyano groups therein yields the respective N-substituted-5- methyl - 5 - aminomethyl - pyrrolidone - (2); N- methyl - and N - ethyl - 5 - methyl - 5 - aminomethyl-pyrrolidone-(2) are also described. Treatment of the 5-methyl-5-aminomethyl-pyrrolidones, wherein the N-substituent is a methyl, ethyl, benzyl or #-methoxyethyl group or attached to nitrogen is a hydrogen atom, with benzaldehyde and dimethyl sulphate yields the corresponding 5-methyl-5-methylaminomethylpyrrolidone. Reduction of 6-cyano-6,N-dimethyl-piperidone- (2), which is prepared by the interaction of 4- acetyl butyric acid ethyl ester cyanohydrin (from the ester and hydrocyanic acid) and methylamine, yields 6,N - dimethyl - 6 - aminomethylpiperidone-(2). N, 2 - Dimethyl - 2 - methylaminomethylpyrrolidine is obtained by reducing 5-formylaminomethyl - N,5 - dimethyl - pyrrolidone - (2) which in turn is prepared by the reaction of ethyl formate with 5-methylaminomethyl-N,5- dimetbyl-pyrrolidone-(2). N - Methyl - 2 - methylaminomethyl - pyrrolidine is obtained by the reaction of N-methyl- 3-chloropiperidine with methylamine.

29. 发明专利

SE311645B 未知
公开(公告)号：SE311645B
公开(公告)日：1969-06-23
申请号：SE922964
申请日：1964-07-29
申请人： BAYER AG
发明人： HOFFMEISTER F , WIRTH W , HILTMANN R , WOLLWEBER H
IPC分类号： C07C69/66 , C07D261/02 , C07D265/02 , C07C103/30

30. 发明专利

SE310878B 未知
公开(公告)号：SE310878B
公开(公告)日：1969-05-19
申请号：SE46365
申请日：1962-12-20
申请人： BAYER AG
发明人： HILTMANN R , WOLLWEBER H , HOFFMEISTER F , WIRTH W
IPC分类号： C07C233/00 , C07D295/192 , C07C103/30
摘要： The invention comprises compounds of the formula: (wherein R is alkyl or alkenyl of at most 4 carbon atoms, R1 is methyl or ethyl, R11 is hydrogen, methyl or ethyl, R111 is hydrogen or alkyl of at most 4 carbon atoms and R1111 is alkyl or alkoxy of at most 4 carbon atoms, or R111 and R1111 together with the nitrogen atom can form a saturated hererocyclic radical which may contain a further hetero atom) and their preparation by (1) reacting a compound of the formula: (wherein X is a reactive group such as a halogen atom or an alkyl- or aryl-sulphonyl group) with the appropriate 3-alkoxy-4-hydroxy-benzoic acid ester; or (2) reacting a 3-alkoxy-4-(a -carboxyalkoxy)-benzoic acid ester or a reactive functional derivative thereof with the appropriate amine NHR111R1111 or a reactive derivative thereof; or (3) reacting an acid of the formula: or a reactive derivative thereof with the appropriate alcohol ROH or a reactive ester thereof such as a halide. Examples are given. Chloroacetic acid-N-ethoxy-N-ethylamide is prepared from a -chloroacetyl chloride and N,O-diethyl-hydroxylamine. 3-Methoxy-4-carbomethoxy-benzoic acid n-propyl ester is prepared from vanillic acid n-propyl ester and sodium chloroacetate. 3-Methoxy-4-(N,N-diethylcarbamidomethoxy)-benzoic acid is prepared by saponification of the methyl ester.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式