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21. 发明专利

CA1051001A 1-(2-('-NAPHTHYLOXY)ETHYL)-3-METHYLPYRAZOLONE-(5) AND PROCESS FOR ITS PREPARATION AND USE 未知
公开(公告)号：CA1051001A
公开(公告)日：1979-03-20
申请号：CA228726
申请日：1975-06-06
申请人： BAYER AG
发明人： MOLLER EIKE , MENG KARL-AUGUST , HORSTMANN HARALD , SEUTER FRIEDEL , WEHINGER EGBERT
IPC分类号： A61K31/415 , A61P7/02 , C07D231/20
摘要： 1-2-(.beta.-Naphthyloxy)ethyl!-3-methylpyrazolone- (5) of the formula: is prepared through the reaction of 2-(.beta.-naphthyloxy)-ethylhydrazine with either an acetoacetate or an ester of tetrolic acid, or through the condensation of 3-methyl-pyrazolinone-(5) with a derivative of 2-(.beta.-naphthyloxy)-ethane, optionally with subsequent salt formation. The compound and its salts are useful in the treatment and prophylaxis of thrombotic conditions.

22. 发明专利

CA1048513A PYRAZOL-5-ONES 未知
公开(公告)号：CA1048513A
公开(公告)日：1979-02-13
申请号：CA197658
申请日：1974-04-17
申请人： BAYER AG
发明人： MOELLER EIKE , MENG KARL , WEHINGER EGBERT , HORSTMANN HARALD
IPC分类号： A61K31/415 , A61P7/02 , A61P7/10 , A61P9/12 , C07D231/20 , C07D231/24 , C07D231/52
摘要： PYRAZOL-5-ONES 1-Substituted pyrazol-5-ones of the formula and pharmaceutically acceptable, nontoxic salts thereof, wherein R is hydrogen or amino; R1 is hydrogen, alkyl, alkenyl, unsubstituted or substituted aryl or unsubstituted or substituted aralkyl; X is a) ethylene, ethylene wherein 1 hydrogen atom on one of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms, ethylene wherein 1 hydrogen atom on each of the two carbon atoms is substituted by alkyl of 1 to 4 carbon atoms or said ethylene which is linked to R2 via an oxygen or sulphur atom;b) propenyl, propenyl wherein 1 hydrogen atom on one, two or three of the carbon atoms is substituted by alkyl of 1 to 4 carbon atoms, said propenyl being linked to the N1 atom of the pyrazol ring via its methylene moiety; orc) methylene; provided that when X is methylene, R1 is not hydrogen if R is amino; R2 is aryl unsubstituted or substituted by:a) 1 or 2 of the same or different substituents selected from the group consisting of halogen, trifluoromethyl, alkyl of 1 to 8 carbon atoms, alkenyl of 2 to 8 carbon atoms and lower alkoxy;b) cycloalkyl of 5, 6 or 7 carbon atoms or cycloalkenyl of 5, 6 or 7 carbon atoms;c) alkylamino, dialkylamino, cyano, trifluoromethoxy, nitro, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, or said carbamoyl wherein the nitrogen atom is a member of a heterocyclic ring, sulphamyl, alkylsulphamyl, dialkylsulphamyl, or said sulphamyl wherein the nitrogen is a member of a heterocyclic ring, or -SOn-alkyl wheeein n is 0, 1 or 2;d) alkylamino, dialkylamino, cyano, trifluoromethoxy, nitro, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, or said carbamoyl wherein the nitrogen atom is a member of a heterocyclic ring, sulphamyl, alkylsulphamyl, dialkylsulphamyl or said sulphamyl wherein the nitrogen is a member of heterocyclic ring, or -SOn-alkyl whereln n is 0, 1 or 2, and 1 or 2 of the same or different substituents selected from the group consisting of alkyl, alkenyl, alkoxy, halogen, and trifluoromethyl; ore) a fused, saturated or unsaturated 5-, 6-, or 7membered ring or said ring containing 1 or 2 oxygen or sulphur atoms; are useful for their diuretic, saluretic, antihypertensive and antithrombotic effects.

23. 发明专利

CH605799A5 未知
公开(公告)号：CH605799A5
公开(公告)日：1978-10-13
申请号：CH156777
申请日：1974-04-16
申请人： BAYER AG
发明人： MOELLER EIKE , MENG KARL AUGUST , WEHINGER EGBERT , HORSTMANN HARALD
IPC分类号： A61K31/415 , A61P7/02 , A61P7/10 , A61P9/12 , C07D231/20 , C07D231/24 , C07D231/52 , C07D231/38
摘要： 1-Substituted pyrazole-5-ones of the formula AND PHARMACEUTICALLY ACCEPTABLE, NONTOXIC SALTS THEREOF, WHEREIN R is hydrogen or amino; R1 is hydrogen, alkyl, alkenyl, unsubstituted or substituted aryl or unsubstituted or substituted aralky; X is A. ETHYLENE, ETHYLENE WHEREIN 1 HYDROGEN ATOM ON ONE OF THE CARBON ATOMS IS SUBSTITUTED BY ALKYL OF 1 TO 4 CARBON ATOMS, ETHYLENE WHEREIN 1 HYDROGEN ATOM ON EACH OF THE TWO CARBON ATOMS IS SUBSTITUTED BY ALKYL OF 1 TO 4 CARBON ATOMS OR SAID ETHYLENE WHICH IS LINKED TO R2 via an oxygen or sulphur atom; B. PROPENYL, PROPENYL WHEREIN 1 HYDROGEN ATOM ON ONE, TWO OR THREE OF THE CARBON ATOMS IS SUBSTITUTED BY ALKYL OF 1 TO 4 CARBON ATOMS, SAID PROPENYL BEING LINKED TO THE N1 atom of the pyrazol ring via its methylene moiety; or C. METHYLENE; PROVIDED THAT WHEN X is methylene, R1 is not hydrogen if R is amino; R2 is aryl unsubstituted or substituted by:

24. 发明专利

CH605797A5 未知
公开(公告)号：CH605797A5
公开(公告)日：1978-10-13
申请号：CH156677
申请日：1974-04-16
申请人： BAYER AG
发明人： MOELLER EIKE , MENG KARL , WEHINGER EGBERT , HORSTMANN HARALD
IPC分类号： C07D231/18 , A61K31/415 , A61P7/02 , A61P7/10 , A61P9/12 , C07D231/20 , C07D231/24 , C07D231/52 , C07D401/06
摘要： 1429141 Pyrazolin-5-ones BAYER AG 16 April 1974 [17 April 1973 19 Dec 1973] 16507/74 Heading C2C The invention comprises compounds of formula (including tautomers thereof, especially when R is amino), wherein R is H, amino, alkyl, alkenyl, CF 3 or Ph; R 1 is H, alkyl, alkenyl or an optionally substituted aryl or aralkyl radical; R 2 is an alkyl group; and R 3 is a pyridyl radical or an aryl radical carrying 1 or 2 identical or different substituents, which are selected from halogen, CF 3 , alkyl, alkenyl, and alkoxy radicals, or carrying one mono- or di-alkylamino, CF 3 O, nitro, nitrile, carbamoyl, alkyl- or dialkylcarbamoyl, sulphamyl, or alkyl- or dialkylsulphamyl radical, or a group -B, -CO.B or -SO 2 .B (in which B is a saturated ring containing a nitrogen atom in the 1-position) or a -SO n alkyl group (in which n=0, 1 or 2), optionally together with 1 or 2 substituents selected from alkyl, alkenyl, alkoxy, halogen and CF 3 , or carrying none or 1 only of these substituents and a fused branched or unbranched, saturated or unsaturated 5-, 6- or 7- membered ring optionally containing 1 or 2 oxygen or sulphur atoms. In examples, these compounds are prepared by (a) reacting R 2 R 3 CHNHNH 2 with an appropriate ring-forming co-reactant, (2) replacing a compound in which R is halogen, by amino, (3) hydrolysing a compound in which R is (e.g.) NHCO 2 Et, or (4) introducing the R 2 R 3 CH group by N 1 -substitution. Therapeutic compositions having diuretic, saluretic, antihypertensive and antithrombotic activity comprise compounds of the above formula, and may be administered orally, parenterally, rectally, topically, or by spray.

25. 发明专利

NO741364L Analogifremgangsmåte til fremstilling av terapeutisk aktive pyrazolon-(5)-forbindelser. 未知
公开(公告)号：NO741364L
公开(公告)日：1974-10-18
申请号：NO741364
申请日：1974-04-16
申请人： BAYER AG
发明人： WEHINGER EGBERT , MÖLLER EIKE , HORSTMANN HARALD , MENG KARL
IPC分类号： C07D231/20 , A61K31/415 , A61P7/02 , A61P7/10 , A61P9/12 , C07D231/24 , C07D231/52

26. 发明专利

GB1137446A Novel disulphonamides and their production 未知
公开(公告)号：GB1137446A
公开(公告)日：1968-12-18
申请号：GB2770867
申请日：1967-06-15
申请人： BAYER AG
发明人： HORSTMANN HARALD , WOLLWEBER HARTMUND , MENG KARL
IPC分类号： C07D307/33
摘要： 1,137,446. Disulphonamides. FARBENFABRIKEN BAYER A.G. 15 June, 1967 [16 June, 1966], No. 27708/67. Heading C2C. Novel disulphonamides (and salts thereof) of the general formula and the corresponding compounds arising from opening of the lactone ring, i.e. of the formula wherein R is hydrogen or methyl, R 1 and R 11 are hydrogen or C 1-4 alkyl and n is 0 or 1, are prepared (a) by reacting 4-chloro-3-sulphonamido - benzene sulphochloride either with the appropriate aminoalkyl - lactone (or salt thereof) or with an aminoalkyl-hydroxy-carboxylic acid (or ester or salt thereof) and in the latter case cyclizing the resulting open-ring compound (corresponding to the compound illustrated above) to the lactone by heating and/or acidifying; or (b) by treating the corresponding tetrahydrofuran or tetrahydropyran with oxidizing agents. Dextro - rotatory 2 - methyl - 2 - methylaminomethyl - tetrahydrofuran is obtained from the racemic mixture by resolution using (d)( - )- tartaric acid (the hydrochloride of the dextro form is also described). α - Aminomethyl - α - methyl - butyrolactone acetate is obtained by catalytic hydrogenation of the corresponding nitrile in glacial acetic acid. γ - Hydroxy - γ - aminomethyl - valeric acid ethyl ester acetate (formed by hydrogenation of the corresponding cyano compound) treated with benzaldehyde and dimethyl sulphate followed by hydrochloric acid yields α-methyl-α- methylaminomethyl - butyrolactone (isolated as the hydrochloride). Chloro - 2 - sulphamoyl - 4 - [N - methyl - N - (2- methyl - tetrahydrofurfuryl)]- sulphamoyl - benzene is prepared by the interaction of 4-chloro-3- sulphonamido - benzene sulphochloride and 2 - methyl - 2 - methylaminomethyl - tetrahydrofuran. Pharmaceutical preparations effective against edema and hypertension contain as active ingredient the above novel compounds and administration is parenterally.

27. 发明专利

DK109265C 未知
公开(公告)号：DK109265C
公开(公告)日：1968-04-08
申请号：DK136066
申请日：1964-11-27
申请人： BAYER AG
发明人： HORSTMANN HARALD , MENG KARL , WOLLWEBER HARTMUND
IPC分类号： C07D307/14 , C07D309/04 , C07D309/20 , C07D5/00 , C07D7/00
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.

28. 发明专利

FR1450363A 未知
公开(公告)号：FR1450363A
公开(公告)日：1966-06-24
申请号：FR867149
申请日：1961-07-06
申请人： BAYER AG
发明人： WORFFEL UDO , HORSTMANN HARALD , WIRTZ SOPHIE
IPC分类号： C07D239/69

29. 发明专利

GB1031916A Sulphonamides 未知
公开(公告)号：GB1031916A
公开(公告)日：1966-06-02
申请号：GB4855664
申请日：1964-11-30
申请人： BAYER AG
发明人： HORSTMANN HARALD , WOLLWEBER HARTMUND , MENG KARL
IPC分类号： C07D307/14 , C07D309/04 , C07D309/20
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.

30. 发明专利

DK157013C 未知
公开(公告)号：DK157013C
公开(公告)日：1990-03-26
申请号：DK399079
申请日：1979-09-24
申请人： BAYER AG
发明人： HORSTMANN HARALD , BOSSERT FRIEDRICH , HEISE AREND , KAZDA STANISLAV
IPC分类号： A61K31/44 , A61K31/445 , A61K31/451 , A61K31/455 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/08 , C07D211/90 , C07D401/04 , C07D405/04 , C07D409/04

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