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公开(公告)号：US3914232A
公开(公告)日：1975-10-21
申请号：US44608374
申请日：1974-02-26
Applicant: HOFFMANN LA ROCHE
Inventor： MOHACSI ERNEST , LEIMGRUBER WILLY
IPC: C07D221/26 , C07D221/28 , A61K31/485
CPC classification number: C07D221/26 , C07D221/28
Abstract: Novel 2- and 4-acyloxy morphinan derivatives, which may bear a variety of N-substituents, are disclosed. These morphinans are useful as analgesic agents and are also useful as antagonists of certain strong analgesics such as morphine.
Abstract translation: 公开了可能具有各种N-取代基的新的2-和4-酰氧基吗啡喃衍生物。 这些吗啡可用作止痛剂，也可用作某些强镇痛药如吗啡的拮抗剂。
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公开(公告)号：US3904632A
公开(公告)日：1975-09-09
申请号：US50813074
申请日：1974-09-23
Applicant: HOFFMANN LA ROCHE
Inventor： HOLLANDER CHARLES WILLIAM DEN , LEIMGRUBER WILLY , MOHACSI ERNEST
IPC: C07H7/027 , C07D221/28 , C07D407/04
CPC classification number: C07H7/027
Abstract: Racemic modifications of optically active amines are treated with (-)-di-O-isopropylidene-2-keto-L-gulonic acid to form diastereomeric salts. The so-formed diastereomeric salts are separated and chemically decomposed to give the desired enantiomers of the amine. The resolving agent, (-)-di-Oisopropylidene-2-keto-L-gulonic acid, is recovered by precipitation from aqueous solution.
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3.发明授权Esterification of carboxylic acids by reaction with o-lower alkyl imino ethers 失效通过与邻 - 低级烷基亚氨基醚反应酯化羧酸
公开(公告)号：US3875209A
公开(公告)日：1975-04-01
申请号：US35686873
申请日：1973-05-03
Applicant: HOFFMANN LA ROCHE
Inventor： MOHACSI ERNEST , LEIMGRUBER WILLY
IPC: C07C69/003 , C07D207/24 , C07D211/76 , C07C69/78
CPC classification number: C07D207/24 , C07D211/76
Abstract: Process for preparing an ester by reacting a carboxylic acid with an O-lower alkyl imino ether.
Abstract translation: 通过使羧酸与O-低级烷基亚氨基醚反应来制备酯的方法。
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公开(公告)号：US3681331A
公开(公告)日：1972-08-01
申请号：US3681331D
申请日：1970-04-02
Applicant: HOFFMANN LA ROCHE
Inventor： LEIMGRUBER WILLY , WEIGELE MANFRED
IPC: C07D241/52 , C07D87/40
CPC classification number: C07D241/52
Abstract: 6-Substituted derivatives of 1-phenazinol 5,10-dioxide which possess broad spectrum anti-microbial activity are disclosed.
Abstract translation: 公开了6-取代的具有广谱抗微生物活性的1-苯并菲醇5,10-二氧化物的衍生物。
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公开(公告)号：US3914234A
公开(公告)日：1975-10-21
申请号：US44608974
申请日：1974-02-26
Applicant: HOFFMANN LA ROCHE
Inventor： MOHACSI ERNEST , LEIMGRUBER WILLY
IPC: C07D221/26 , C07D221/28 , A61K31/485
CPC classification number: C07D221/26 , C07D221/28
Abstract: Novel 2-lower alhoxy morphinan derivatives which may bear a variety of N-substituents, are disclosed. These morphinans are useful as analgesic agents and are also useful as antagonists of certain strong analgesics such as morphine.
Abstract translation: 公开了可能具有多种N-取代基的新的2-低级甲氧基吗啡喃衍生物。 这些吗啡可用作止痛剂，也可用作某些强镇痛药如吗啡的拮抗剂。
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Patent Agency Ranking
公开(公告)号：US3912761A
公开(公告)日：1975-10-14
申请号：US50812874
申请日：1974-09-23
Applicant: HOFFMANN LA ROCHE
Inventor： DEN HOLLANDER CHARLES WILLIAM , LEIMGRUBER WILLY , MOHACSI ERNEST
IPC: C07H7/027 , C07D317/26
CPC classification number: C07H7/027
Abstract: Racemic modifications of optically active amines are treated with (-)-di-O-isopropylidene-2-keto-L-gulonic acid to form diastereomeric salts. The so-formed diastereomeric salts are separated and chemically decomposed to give the desired enantiomers of the amine. The resolving agent, (-)-di-0isopropylidene-2-keto-L-gulonic acid, is recovered by precipitation from aqueous solution.
Abstract translation: 用（ - ） - 二-O-异亚丙基-2-酮-L-古洛糖酸处理光学活性胺的外消旋体，形成非对映异构体盐。 将如此形成的非对映异构体盐分离并化学分解，得到所需胺的对映异构体。 通过从水溶液中沉淀来回收拆分剂（ - ） - 二-O-异亚丙基-2-酮-L-古洛糖酸。
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7.发明授权Organometallic derivatives of 6-lower alkoxy 1-phenazinol 5,10-dioxide 失效6位低碱性1-PHENAZINOL 5,10-二氧化物的有机衍生物
公开(公告)号：US3586674A
公开(公告)日：1971-06-22
申请号：US3586674D
申请日：1969-04-08
Applicant: HOFFMANN LA ROCHE
Inventor： LEIMGRUBER WILLY , MAESTRONE GIAN PAOLO , MITROVIC MILAN , WEIGELE MANFRED
IPC: C07D241/52 , C07D51/80
CPC classification number: C07D241/52 , Y10S514/924
Abstract: COPPER DERIVATIVES OF 6-LOWER ALKOXY-1-PHENAZINOL 5,10DIOXIDE PREPARED BY TREATING A 6-LOWER ALKOXY-1-PHENAZINOL 5,10-DIOXIDE WITH A COPPER SALT POSSESS BROAD SPECTRUM ANTI-MICROBIAL ACTIVITY.
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公开(公告)号：US3575983A
公开(公告)日：1971-04-20
申请号：US3575983D
申请日：1967-08-30
Applicant: HOFFMANN LA ROCHE
Inventor： LEIMGRUBER WILLY , SCHENKER FAUSTO EUGENIO
IPC: C07D217/02 , C07D217/04 , C07D217/10 , C07D35/28
CPC classification number: C07D217/04 , C07D217/02 , C07D217/10
Abstract: NOVEL PHARMACOLOGICALLY ACTIVE 1,2,3,4-TETRAHYDRO-8ISOQUINOLINOL, 1- AND/OR 2-(LOWER ALKYL)-1,2,3,4-TETRAHYDRO-8-ISOQUINOLINOLS AND INTERMEDIATES THEREFOR, ARE PREPARED UTILIZING, FOR EXAMPLE, 8-ISOQUINOLINOL AS A STARTING MATERIAL. THE PHARMACOLOGICALLY ACTIVE COMPOUNDS OF THE INVENTION ARE USEFUL AS HYPOTENSIVE AGENTS.
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公开(公告)号：US3542848A
公开(公告)日：1970-11-24
申请号：US3542848D
申请日：1968-04-09
Applicant: HOFFMANN LA ROCHE
Inventor： LEIMGRUBER WILLY , WEIGELE MANFRED
IPC: C07C255/30 , C07C121/42
CPC classification number: C07C255/00
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公开(公告)号：US3530130A
公开(公告)日：1970-09-22
申请号：US3530130D
申请日：1967-09-14
Applicant: HOFFMANN LA ROCHE
Inventor： LEIMGRUBER WILLY , WEIGELE MANFRED
IPC: C07D241/52 , C07D51/80
CPC classification number: C07D241/52
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