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1. 发明授权

US3770748A Substituted phenylalkanol derivatives 失效
标题翻译：取代的苯甲醇衍生物
公开(公告)号：US3770748A
公开(公告)日：1973-11-06
申请号：US3770748D
申请日：1972-03-24
申请人： MERCK PATENT GMBH
发明人： BORCK J , DAHM J , WILD A , HOVY J , KRAMER J
IPC分类号： C07D207/12 , C07D211/02 , C07D211/42 , C07D491/10 , C07D29/24
CPC分类号： C07D491/10 , C07D207/12 , C07D211/02 , C07D211/42 , Y10S514/916 , Y10S514/96 , Y10S514/962
摘要： PHENYLALKANOL DERIVATIVES OF THE FORMULA

1-((-(CH2)N-CH(-O-R2)-CH2-)>N-),2-R4,4-(R1-CH2-CH(-R3)-)

BENZENE

WHEREIN R1 IS OH, ALKOXY OF UP TO 6 CARBON ATOMS, CYCLOALKOXY OF UP TO 6 CARBON ATOMS, ARYLOXY OF 6-12 CARBON ATOMS, ARALKOXY OF 7-12 CARBON ATOMS, OR ACYLOXY OF UP TO 18, PREFERABLY UP TO 6, CARBON ATOMS; R2 IS H, ALKYL OF UP TO 6 CARBON ATOMS, CYCLOALKY OF UP TO 6 CARBON ATOMS, ARYL OF 6-12 CARBON ATOMS, ARALKYL OF 7-12 CARBON ATOMS, OR ACYL OF UP TO 18, PREFERABLY UP TO 6, CARBON ATOMS; R3 IS H OR CH3; R4 IS C1, BR OR CH3; AND N IS 2 OR 3; AND THE PHYSIOLOGICALLY ACCEPTABLE ACID ADDITION SALTS AND QUATERNARY AMMONIUM SALTS THEREOF; POSSESS USEFUL PHARMACOLOGICAL ACTIVITY, INCLUDING ANTIPHLOGISTIC. ANALGESIC AND ANTIPYRETIC EFFECTS.

2. 发明专利

SE404022B 未知
公开(公告)号：SE404022B
公开(公告)日：1978-09-18
申请号：SE7409871
申请日：1974-07-31
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.

3. 发明专利

DK137273C 未知
公开(公告)号：DK137273C
公开(公告)日：1978-07-17
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.

4. 发明专利

ZA773484B ALKYNOLS AND PREPARATION THEREOF 未知
公开(公告)号：ZA773484B
公开(公告)日：1978-04-26
申请号：ZA773484
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

5. 发明专利

SE399557B 未知
公开(公告)号：SE399557B
公开(公告)日：1978-02-20
申请号：SE7312484
申请日：1973-09-13
申请人： MERCK PATENT GMBH
发明人： GANTE J , MEHRHOF W , WILD A
IPC分类号： B01J23/00 , B01J31/00 , C07B61/00 , C07D327/08 , C07D335/12 , C07D339/08
摘要： Compounds of the formula WHEREIN R1 is COOH, COO-alkyl, CH2OH or CH2-alkanoyl; R2 is CH3 or C2H5; R3 is H, F, Cl or Br; and Y is CH2, O or S, at least one Y being S, and the physiologically acceptable salts thereof, possesses antiphlogistic activity.

6. 发明专利

DK136065C 未知
公开(公告)号：DK136065C
公开(公告)日：1978-01-09
申请号：DK499975
申请日：1975-11-06
申请人： MERCK PATENT GMBH
发明人： GANTE J , KURMEIER H-A , SCHACHT E , MEHRHOF W , WILD A
IPC分类号： C07D231/08
摘要： Pyrazolidinones of the formula WHEREIN R is a phenyl, phenoxy or a corresponding group monosubstituted or polysubstituted by one or more of F, Cl and Br possess anti-inflammatory activity.

7. 发明专利

SE7706724A 未知
公开(公告)号：SE7706724A
公开(公告)日：1977-12-11
申请号：SE7706724
申请日：1977-06-09
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 , C07C43/27
CPC分类号： C07D309/12

8. 发明专利

DK135684C 未知
公开(公告)号：DK135684C
公开(公告)日：1977-11-14
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

10. 发明专利

ZA7603626B ALKINE DERIVATIVES AND A PROCESS FOR THEIR PREPARATION 未知
公开(公告)号：ZA7603626B
公开(公告)日：1977-05-25
申请号：ZA7603626
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
CPC分类号： C07C29/42 , C07C69/157 , C07C69/63 , C07F1/005 , C07C33/28

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