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31. 发明专利

ZA8000922B PYRAZOLE DERIVATIVES PHARMACEUTICAL FORMULATIONS CONTAINING THESE DERIVATIVES AND PROCESSES FOR THEIR PREPARATION 未知
公开(公告)号：ZA8000922B
公开(公告)日：1981-02-25
申请号：ZA8000922
申请日：1980-02-18
申请人： MERCK PATENT GMBH
发明人： KLOCKOW , RADUNZ H , GANTE J , MINCK K , ORTH D , WILD A
IPC分类号： A61K31/42 , A61K31/425 , A61K31/435 , A61P7/02 , A61P25/04 , A61P29/00 , C07D231/12 , C07D403/06 , C07D413/06 , C07D417/06 , C07D
CPC分类号： C07D231/12

32. 发明专利

AU510322B2 ALKYNOLS 未知
公开(公告)号：AU510322B2
公开(公告)日：1980-06-19
申请号：AU2549977
申请日：1977-05-25
申请人： MERCK PATENT GMBH
发明人： KURMEIER H-A , SCHACHT E , GANTE J , ORTH D , SIMANE Z , WILD A
IPC分类号： C07C43/295 , A61K31/055 , A61K31/085 , A61K31/35 , A61K31/351 , A61P3/06 , A61P7/02 , A61P25/04 , A61P29/00 , C07C27/00 , C07C33/48 , C07C41/00 , C07C67/00 , C07D309/12 , C07C33/10 , A61K31/065

33. 发明专利

AU499362B2 ARYL AND ARYLOXY PHENYL ALKANOLS 未知
公开(公告)号：AU499362B2
公开(公告)日：1979-04-12
申请号：AU1350876
申请日：1976-04-30
申请人： MERCK PATENT GMBH
发明人： GANTE J , KURMEIER H A , ORTH D , SCHACHT E , WILD A
IPC分类号： A61K31/06 , A61K31/085 , C07C27/00 , C07C33/46 , C07C41/00 , C07C43/295 , C07C67/00 , C07C253/00 , C07C255/36 , C07C255/37 , C07C31/34 , C07C43/28 , C07C121/75 , A61K31/065 , A61K31/275
摘要： Phenylalkanols of the formula wherein Ar is phenyl or phenyl monosubstituted or disubstituted by F, Cl, Br and/or CH3; X is F, Cl, Br or CN; m is 0 or 1; and n 2 or 3; possess antiinflammatory activity and can be produced by treating a compound of formula wherein Q is a functionally modified hydroxy group and Ar, X, m and n have the values given above, with a solvolyzing agent.

34. 发明专利

ZA7703484B ALKYNOLS AND PREPARATION THEREOF 未知
公开(公告)号：ZA7703484B
公开(公告)日：1978-04-26
申请号：ZA7703484
申请日：1977-06-09
申请人： MERCK PATENT GMBH
发明人： SIMANE Z , ORTH D , KURMEIER H , WILD A , GANTE J , SCHACHT E
IPC分类号： C07C43/295 , A61K31/055 , A61K31/085 , A61K31/35 , A61K31/351 , A61P3/06 , A61P7/02 , A61P25/04 , A61P29/00 , C07C27/00 , C07C33/48 , C07C41/00 , C07C67/00 , C07D309/12 , C07C , A61K , C07D
CPC分类号： C07D309/12

35. 发明专利

DK137273B 未知
公开(公告)号：DK137273B
公开(公告)日：1978-02-13
申请号：DK145572
申请日：1972-03-24
申请人： MERCK PATENT GMBH
发明人： BORCK J , DAHM J , HOVY J W , KRAEMER J , WILD A
IPC分类号： C07D207/12 , C07D211/02 , C07D211/42 , C07D491/10
摘要： 1359600 4 - (3 - Hydroxy - pyrrolidino or -piperidino)-phenylalkanol derivatives MERCK PATENT GmbH 10 March 1972 [25 March 1971] 11292/72 Heading C2C Novel 4 - (3 - hydroxy - pyrrolidino or -piperidino)-phenylalkanol derivatives of the general formula wherein R 1 is a hydroxyl, C 1-6 alkoxy, C 3-6 cycloalkoxy, C 6-12 aryloxy, C 7-12 aralkoxy or C 1-18 acyloxy group, or a heterocycloalkoxy group with up to 6 carbon atoms which may optionally be substituted with an alkoxy group, R 2 is a hydrogen atom or a C 1-6 alkyl, C 3-6 cycloalkyl, C 6-12 aryl, C 7-12 aralkyl or C 1-18 acyl group, R 3 is a hydrogen atom or methyl group, R 4 is a chlorine or bromine atom or a methyl group and n is 2 or 3, and acid addition and quaternary ammonium salts thereof are prepared, e.g. (a) when R 1 is a hydroxyl group, R 2 is a hydrogen atom and R 3 is a methyl group, by catalytic hydrogenation of the corresponding 2-phenyl-allyl alcohol; (b) when R 1 is a C 1-6 alkoxy group and R 2 is a C 1-6 alkyl group, by reaction of the corresponding compound in which R 1 is a hydroxyl group and R 2 is a hydrogen atom with a C 1-6 alkyl iodide or bromide or a di-C 1-6 alkyl sulphate, (c) when R 1 is a C 1-18 acyloxy group and R 2 is a C 1-18 acyl group, by acylation of the corresponding compound in which R 1 is a hydroxyl group and R 2 is a hydrogen atom; (d) when R 1 is a hydroxyl group and R 2 is a hydrogen atom, by reduction of an appropriate phenylalkanal, phenylalkanoic acid or ester thereof or 4-(3-oxo-pyrrolidino or -piperidino)-phenylalkanol with lithium aluminium hydride; (e) when R 1 is a hydroxyl group and R 2 is a hydrogen atom, by alkaline hydrolysis of the corresponding compound in which R 1 is a bromine atom; (f) when R 1 is a hydroxyl group and R 2 is a hydrogen atom, by reaction of an appropriate 4-hydroxy-alkylaniline with an #,# 1 -dibromoalkanol; (g) when R 1 is a hydroxyl group, R 2 is a hydrogen atom and R 4 is a chlorine atom, by diazotization of the corresponding compound in which R 4 is an amino group, followed by treatment with cuprous chloride in hydrochloric acid; (h) when R 1 is a hydroxyl group and R 2 is a hydrogen atom, by alkaline hydrolysis of the corresponding 4-(3-bromo-pyrrolidino or -piperidino)-phenylalkanol; and (i) when R 1 is a C 1-18 acyloxy group and R 2 is a C 1-18 acyl group, by catalytic hydrogenation of the corresponding compound in which the heterooyclic ring contains a C-C double bond; followed optionally by salification or desalification of the product or separation of a resulting racemate into its optical antipodes. Pharmaceutical compositions having antiinflammatory activity comprise, as active ingredient, a 4-(3-hydroxy-pyrrolidino or -piperidino)-phenylalkanol derivative of the general formula above or an acid addition or quaternary ammonium salt thereof, together with an inert, physiologically acceptable carrier therefor, and may be administered parenterally, enterally or locally.

36. 发明专利

DK135684B 未知
公开(公告)号：DK135684B
公开(公告)日：1977-06-06
申请号：DK262473
申请日：1973-05-11
申请人： MERCK PATENT GMBH
发明人： GANTE J , MEHRHOF W , WILD A
IPC分类号： C07D307/91 , C07D333/76

37. 发明专利

ZA763845B ARALIPHATIC DIHALOGEN COMPOUNDS WITH PROCESSES FOR THEIR PREPARATION 未知
公开(公告)号：ZA763845B
公开(公告)日：1977-05-25
申请号：ZA763845
申请日：1976-06-28
申请人： MERCK PATENT GMBH
发明人： GANTE J , KURMEIER H , WILD A , ORTH D , SCHACHT E
IPC分类号： C07C69/73 , A61K31/045 , A61K31/085 , A61K31/19 , A61K31/215 , A61K31/22 , A61P3/06 , A61P7/04 , A61P25/04 , A61P29/00 , C07C27/00 , C07C29/14 , C07C29/141 , C07C29/147 , C07C29/60 , C07C33/46 , C07C41/00 , C07C43/295 , C07C51/00 , C07C57/58 , C07C57/60 , C07C57/76 , C07C59/56 , C07C59/68 , C07C67/00 , C07C69/025 , C07C69/65 , C07F1/00 , C07F9/40 , C07C , A61K

38. 发明专利

ZA763626B ALKINE DERIVATIVES AND A PROCESS FOR THEIR PREPARATION 未知
公开(公告)号：ZA763626B
公开(公告)日：1977-05-25
申请号：ZA763626
申请日：1976-06-18
申请人： MERCK PATENT GMBH
发明人： ORTH D , SCHACHT E , GANTE J , KURMEIER H , WILD A
IPC分类号： C07C69/007 , A61K31/065 , A61K31/085 , A61K31/215 , A61K31/22 , A61P3/06 , A61P7/02 , A61P25/04 , A61P29/00 , C07C27/00 , C07C29/42 , C07C33/28 , C07C33/48 , C07C41/00 , C07C43/295 , C07C67/00 , C07C69/145 , C07F1/00 , C07C
摘要： Alkyne compounds of the formula wherein R1 is H, alkyl of up to 4 carbon atoms or phenyl; R2 is H, aliphatic acyl of up to 6 carbon atoms or aroyl of up to 11 carbon atoms; R3 and R4 are H, F, Cl or Br and n is 0 or 1, and physiologicaly acceptable metals salts thereof, have antiinflammatory activity. These compounds can be made from compounds of the formula wherein Q is a functionally-modified hydroxy and R1, R3, R4 and n are as above by treatment with a solvolyzing agent.

39. 发明专利

DK134645C 未知
公开(公告)号：DK134645C
公开(公告)日：1977-05-16
申请号：DK415274
申请日：1974-08-02
申请人： MERCK PATENT GMBH
发明人： GANTE J , KURMEIER H A , MEHRHOF W , WILD A
IPC分类号： C07D327/08 , C07D335/12 , C07D335/16 , C07D339/08
摘要： Sulfoxides and sulfones of the formula WHEREIN R1 is COOH, COOR4, CH2OH, or CH2OR5; R2 is CH3 or C2H5; R3 is H, F, Cl, or Br; R4 is alkyl of 1-8 carbon atoms; R5 is alkanoyl of 2-4 carbon atoms; one of the Y groups is SO or SO2 and the other Y group is CH2, O, S, SO, or SO2; and the physiologically acceptable salts thereof, which compounds possess anti-inflammatory activity, can be produced by converting in a compound of the formula WHEREIN X is a group convertible into the group -CHR1R2 wherein R1, R2, R3, and Y have the values given above, the group X into the group -CHR1R3.

40. 发明专利

ZA762605B PHENYLALKANOLS AND THEIR PREPARATION 未知
公开(公告)号：ZA762605B
公开(公告)日：1977-04-27
申请号：ZA762605
申请日：1976-04-30
申请人： MERCK PATENT GMBH , SCHACHT E
发明人： ORTH D , GANTE J , KURMEIER H , WILD A
IPC分类号： A61K31/06 , A61K31/085 , C07C27/00 , C07C33/46 , C07C41/00 , C07C43/295 , C07C67/00 , C07C253/00 , C07C255/36 , C07C255/37 , C07C
摘要： Phenylalkanols of the formula wherein Ar is phenyl or phenyl monosubstituted or disubstituted by F, Cl, Br and/or CH3; X is F, Cl, Br or CN; m is 0 or 1; and n 2 or 3; possess antiinflammatory activity and can be produced by treating a compound of formula wherein Q is a functionally modified hydroxy group and Ar, X, m and n have the values given above, with a solvolyzing agent.

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