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1. 发明申请

US20050090543A1 Method for the preparation of tetrahydrobenzothiepines 审中-公开
标题翻译：四氢苯并噻吩的制备方法
公开(公告)号：US20050090543A1
公开(公告)日：2005-04-28
申请号：US10848566
申请日：2004-05-19
申请人： Kevin Babiak , Andrew Carpenter , Shine Chou , Pierre-Jean Colson , Farid Payman , Robert Hett , Christian Huber , Kevin Koeller , Jon Lawson , James Li , Eduardo Mar , Lawrence Miller , Vladislav Orlovski , James Peterson , Mark Pozzo , Claire Przybyla , Samuel Tremont , Jay Trivedi , Grace Wagner , Gerald Weisenburger , Benxin Zhi
发明人： Kevin Babiak , Andrew Carpenter , Shine Chou , Pierre-Jean Colson , Farid Payman , Robert Hett , Christian Huber , Kevin Koeller , Jon Lawson , James Li , Eduardo Mar , Lawrence Miller , Vladislav Orlovski , James Peterson , Mark Pozzo , Claire Przybyla , Samuel Tremont , Jay Trivedi , Grace Wagner , Gerald Weisenburger , Benxin Zhi
IPC分类号： C07D317/18 , A61K31/235 , A61K31/38 , A61K31/495 , A61K31/4995 , A61P3/06 , A61P43/00 , C07B53/00 , C07B55/00 , C07B57/00 , C07B61/00 , C07C201/12 , C07C205/35 , C07C315/02 , C07C315/04 , C07C317/24 , C07C317/36 , C07C319/14 , C07C321/28 , C07D337/08 , C07D409/12 , C07D487/08 , C07D337/16
CPC分类号： C07D409/12 , A61K31/235 , A61K31/38 , A61K31/495 , C07D337/08 , C07D487/08 , A61K2300/00
摘要： Among its several embodiments, the present invention provides an improved process for the preparation of tetrahydrobenzothiepine-1,1-dioxide compounds; the provision of a process for preparing a diastereomeric mixture of tetrahydrobenzothiepine-1,1-dioxide compounds from a single diastereomer of such compounds; the provision of a process for the preparation of 3-bromo-2-substituted propionaldehyde compounds; and the provision of a process for the preparation of 3-thio-2-substituted propionaldehyde compounds.
摘要翻译：在其几个实施方案中，本发明提供了一种制备四氢苯并噻吩一-1,1-二氧化物化合物的改进方法; 提供了由这种化合物的单一非对映异构体制备四氢苯并噻吩一-1,1-二氧化物化合物的非对映体混合物的方法; 提供了制备3-溴-2-取代的丙醛化合物的方法; 并提供了制备3-硫代-2-取代的丙醛化合物的方法。

2. 发明授权

US6096692A Synthetic lubricating oil 失效
标题翻译：合成润滑油
公开(公告)号：US6096692A
公开(公告)日：2000-08-01
申请号：US776751
申请日：1997-02-13
申请人： Toshiya Hagihara , Shoji Nakagawa , Yuichiro Kobayashi , Hiroyasu Togashi , Koji Taira , Akimitsu Sakai
发明人： Toshiya Hagihara , Shoji Nakagawa , Yuichiro Kobayashi , Hiroyasu Togashi , Koji Taira , Akimitsu Sakai
IPC分类号： C07D317/12 , C07D317/22 , C07D493/04 , C10M105/18 , C10M171/00 , C07D317/18
CPC分类号： C07D493/04 , C07D317/12 , C07D317/22 , C10M105/18 , C10M171/008 , C10M2207/044 , C10M2211/022 , C10M2211/06 , C10N2240/00 , C10N2240/02 , C10N2240/22 , C10N2240/30 , C10N2240/50 , C10N2240/52 , C10N2240/54 , C10N2240/56 , C10N2240/58 , C10N2240/60 , C10N2240/66
摘要： The present invention relates to a synthetic lubricating oil comprising cyclic ketals or cyclic acetals obtained by a reaction between one or more polyhydric alcohols having an even number of hydroxyl groups of not less than 4 and not more than 10 and one or more specific carbonyl compounds, or one or more ketals or acetals which are reactive derivatives of said carbonyl compounds; a working fluid composition for a refrigerating machine comprising a hydrofluorocarbon and a refrigeration oil containing the cyclic ketals or cyclic acetals; and novel compounds of the above cyclic acetals and a production method thereof. The present invention provides a synthetic lubricating oil which shows a good thermal stability, a good oxidation resistance, no carboxylic acid formation due to hydrolysis and a low hygroscopicity and is inexpensive as well. Also, a working fluid composition for a refrigerating machine which shows a good insulating property, favorable hygroscopicity, and no carboxylic acid formation due to hydrolysis as well as being inexpensive can be provided.
摘要翻译： PCT No.PCT / JP95 / 00304 Sec。 371日期1996年2月13日 102（e）日期1996年2月13日PCT提交1995年2月27日PCT公布。公开号WO96 / 06839 日期：1996年3月7日本发明涉及一种合成润滑油，其包含通过一种或多种具有偶数个羟基的多元醇的反应而获得的环状缩酮或环状缩醛，所述羟基数为4以上且10以下，更特异的羰基化合物或作为所述羰基化合物的反应性衍生物的一种或多种缩酮或缩醛; 一种用于制冷机的工作流体组合物，包括氢氟烃和含有环状缩酮或环状缩醛的冷冻机油; 和上述环状缩醛的新化合物及其制备方法。本发明提供合成润滑油，它具有良好的热稳定性，良好的抗氧化性，由于水解而不形成羧酸，吸湿性低，并且也便宜。另外，也可以提供一种冷冻机的工作流体组合物，其具有良好的绝缘性，良好的吸湿性，并且由于水解而不形成羧酸，而且价格便宜。

3. 发明授权

US5981585A Phenyl acetic acid derivatives as pesticides 失效
标题翻译：苯乙酸衍生物作为农药
公开(公告)号：US5981585A
公开(公告)日：1999-11-09
申请号：US968143
申请日：1997-11-12
申请人： Hugo Ziegler , Stephan Trah , Saleem Farooq , Rene Zurfluh
发明人： Hugo Ziegler , Stephan Trah , Saleem Farooq , Rene Zurfluh
IPC分类号： A01N37/34 , A01N37/36 , A01N37/44 , A01N37/50 , A01N43/28 , A01N43/30 , A01N43/36 , A01N43/40 , A01N43/46 , A01N43/653 , A01N43/84 , A01N55/00 , C07C229/00 , C07C251/60 , C07C251/76 , C07C251/80 , C07C255/00 , C07C255/54 , C07C255/61 , C07D213/77 , C07D295/088 , C07D295/30 , C07D317/18 , C07D317/58 , C07D333/22 , C07D521/00 , A61K31/24 , A01N37/12
CPC分类号： C07D213/77 , A01N37/36 , A01N37/50 , A01N43/28 , A01N43/30 , A01N43/36 , A01N43/40 , A01N43/46 , A01N43/653 , A01N43/84 , A01N55/00 , C07C251/60 , C07C251/76 , C07C251/80 , C07C255/54 , C07C255/61 , C07D231/12 , C07D233/56 , C07D249/08 , C07D295/088 , C07D295/30 , C07D317/18 , C07D317/58 , C07D333/22 , C07C2101/02
摘要： Compounds of the formula I ##STR1## and the isomers thereof, in which either a) X is an N atom and Y is OR.sub.11 or N(R.sub.12)R.sub.13, orb) X is CH and Y is OR.sub.11,and in which furthermore:R.sub.11 is C.sub.1 -C.sub.4 alkyl;R.sub.12 and R.sub.13, independently, are hydrogen or C.sub.1 -C.sub.4 alkyl;A is an O atom or the group NR.sub.4 ; and whereinR.sub.1, R.sub.2 and R.sub.3 are as defined herein, are pesticidal active ingredients. They can be used for pest control, in particular as microbicides, insecticides and acaricides in agriculture, horticulture and in the hygiene sector.
摘要翻译：式Ⅰ化合物及其异构体，其中a）X为N原子，Y为OR 11或N（R 12）R 13，或b）X为CH，Y为OR 11，此外，R 11为Cl -C 1-4烷基; R 12和R 13独立地是氢或C 1 -C 4烷基; A是O原子或NR4基团; 并且其中R1，R2和R3如本文所定义，是农药活性成分。它们可以用于害虫控制，特别是作为农业，园艺和卫生领域的杀菌剂，杀虫剂和杀螨剂。

4. 发明授权

US5869702A Polyol ether derivatives and production methods therefor 失效
标题翻译：多元醇醚衍生物及其制备方法
公开(公告)号：US5869702A
公开(公告)日：1999-02-09
申请号：US869141
申请日：1997-06-04
申请人： Shoji Nakagawa , Hiroki Sawada , Hiroyasu Togashi , Toshiya Hagihara
发明人： Shoji Nakagawa , Hiroki Sawada , Hiroyasu Togashi , Toshiya Hagihara
IPC分类号： C07C43/10 , C07C43/13 , C07C43/184 , C07D317/22 , C07D319/06 , C07D493/04 , C10M105/18 , C10M107/30 , C10M169/04 , C10M171/00 , C07D317/18 , C07D319/08 , C07D407/04 , C07C41/00
CPC分类号： C07D493/04 , C07C43/10 , C07C43/13 , C07C43/135 , C07C43/184 , C07D317/22 , C07D319/06 , C10M105/18 , C10M107/30 , C10M169/04 , C10M171/008 , C10M2201/041 , C10M2201/042 , C10M2201/066 , C10M2207/023 , C10M2207/024 , C10M2207/025 , C10M2207/026 , C10M2207/027 , C10M2207/04 , C10M2207/0406 , C10M2207/042 , C10M2207/044 , C10M2207/046 , C10M2207/08 , C10M2207/24 , C10M2207/28 , C10M2207/283 , C10M2207/289 , C10M2211/022 , C10M2211/06 , C10M2213/00 , C10M2213/02 , C10M2213/04 , C10M2213/06 , C10M2213/062 , C10M2215/064 , C10M2215/065 , C10M2215/14 , C10M2215/22 , C10M2215/221 , C10M2215/225 , C10M2215/226 , C10M2215/30 , C10M2219/068 , C10M2219/082 , C10M2219/083 , C10M2219/085 , C10M2219/10 , C10M2219/102 , C10M2219/104 , C10M2219/106 , C10M2219/108 , C10M2223/04 , C10M2223/041 , C10M2223/042 , C10M2223/045 , C10M2227/02 , C10M2229/041 , C10M2229/045 , C10M2229/046 , C10M2229/047 , C10M2229/048 , C10M2229/05 , C10N2210/02 , C10N2210/06 , C10N2240/00 , C10N2240/22 , C10N2240/30 , C10N2240/50 , C10N2240/52 , C10N2240/54 , C10N2240/56 , C10N2240/58 , C10N2240/60 , C10N2240/66
摘要： Polyol ether derivatives, a method for producing the polyol ether derivatives, and a working fluid composition for a refrigerating machine containing a hydrofluorocarbon and a refrigeration oil containing the polyol ether derivatives as a base oil.
摘要翻译：多元醇醚衍生物，多元醇醚衍生物的制造方法以及含有氢氟烃和含有多元醇醚衍生物作为基础油的冷冻机的制冷机的工作流体组合物。

5. 发明授权

US5712418A Synthesis and use of amino acid fluorides as peptide coupling reagents 失效
公开(公告)号：US5712418A
公开(公告)日：1998-01-27
申请号：US284964
申请日：1994-08-02
申请人： Louis A. Carpino , Ayman Ahmed El-Faham
发明人： Louis A. Carpino , Ayman Ahmed El-Faham
IPC分类号： C07C237/22 , C07C255/14 , C07C271/10 , C07C271/34 , C07C275/40 , C07C275/70 , C07C317/04 , C07C317/10 , C07C317/14 , C07C317/18 , C07C321/14 , C07C321/20 , C07C323/14 , C07D207/16 , C07D209/20 , C07D233/64 , C07D233/68 , C07D295/215 , C07D317/18 , C07K1/06 , C07K1/08 , C07K1/10 , C07K1/113 , C07D233/02 , C07C257/14 , C07C257/18 , C07D207/02
CPC分类号： C07D295/215 , C07C271/10 , C07C271/34 , C07C275/40 , C07C275/70 , C07C317/04 , C07C317/10 , C07C317/14 , C07C317/18 , C07C321/14 , C07C321/20 , C07C323/14 , C07D207/16 , C07D209/20 , C07D233/68 , C07K1/088 , C07K1/10 , C07C2103/18 , Y02P20/55
摘要： The present invention is directed to the process of preparing a peptide comprising reacting a first amino acid or peptide with an amino acid fluoride of the formula: ##STR1## or the acid fluoride salts thereof wherein BLK is an N-amino protecting group AA is an amino acid residue and X is H or a protecting group useful, and the first amino and peptide have a free amino group and a blocked carboxy end.

6. 发明授权

US4708966B1 失效
公开(公告)号：US4708966B1
公开(公告)日：1991-03-12
申请号：US87986386
申请日：1986-06-27
申请人： PROCTER & GAMBLE
发明人： MAURICE E LOOMANS , RANDALL S MATTHEWS , JOSEPH A MILLER
IPC分类号： C07C17/00 , A61K31/01 , A61K31/015 , A61K31/047 , A61K31/05 , A61K31/12 , A61K31/13 , A61K31/135 , A61K31/165 , A61K31/19 , A61K31/22 , A61K31/335 , A61K31/357 , A61K31/385 , A61K31/695 , A61P3/06 , A61P9/00 , A61P9/10 , A61P25/04 , A61P29/00 , A61P37/00 , A61P43/00 , C07C1/00 , C07C15/48 , C07C22/04 , C07C22/08 , C07C27/00 , C07C33/18 , C07C39/18 , C07C39/24 , C07C39/373 , C07C41/00 , C07C43/166 , C07C43/315 , C07C45/00 , C07C45/29 , C07C45/45 , C07C45/67 , C07C45/68 , C07C45/71 , C07C47/52 , C07C49/248 , C07C49/255 , C07C49/76 , C07C49/794 , C07C49/80 , C07C49/835 , C07C49/84 , C07C65/00 , C07C67/00 , C07C69/017 , C07C69/533 , C07C209/00 , C07C211/27 , C07C211/29 , C07C213/00 , C07C215/48 , C07C217/48 , C07C219/28 , C07C229/34 , C07C381/12 , C07D317/18 , C07D317/26 , C07D319/06 , C07D339/00 , C07F7/08 , C07F7/18
CPC分类号： C07F7/0818 , C07C39/18 , C07C43/315 , C07C45/004 , C07C45/292 , C07C45/45 , C07C45/67 , C07C45/673 , C07C45/68 , C07C45/71 , C07C49/248 , C07C49/255 , C07C49/794 , C07C49/80 , C07C49/835 , C07C49/84
摘要： The present invention relates to novel specifically-substituted phenyl compounds, especially substituted di-tert-butyl phenol derivatives, which are effective as anti-inflammatory, analgesic and/or antipyretic agents. These phenyl compounds are substituted with a low molecular weight alkyl chain which terminates in a specific unsaturated functional group. These unsaturated functionalities are -C=CH, C=CH2, C=C=CH2, and aldehydes in the form of their acetals. The present invention further relates to pharmaceutical compositions which contain an anti-inflammatory agent of the present invention and a pharmaceutically-acceptable carrier. Finally, the present invention relates to methods for treating diseases characterized by inflammation, such as rheumatoid arthritis and osteoarthritis, in humans or lower animals. Such methods comprise administering to a human or lower animal in need of such treatment a safe and effective amount of an anti-inflammatory agent or composition of the present invention.

7. 发明授权

US4918173A 2',6'-Dideoxy derivatives of anthracycline glycosides 失效
标题翻译： 2'，6'-二脱氧衍生物的蒽环类苷
公开(公告)号：US4918173A
公开(公告)日：1990-04-17
申请号：US880075
申请日：1986-06-30
申请人： Claude Monneret , Jean-Claude Florent , Agnes Genot
发明人： Claude Monneret , Jean-Claude Florent , Agnes Genot
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , A61P35/02 , C07D317/18 , C07D317/22 , C07D317/24 , C07D317/26 , C07D317/72 , C07D407/06 , C07F7/18 , C07H15/252
CPC分类号： C07D317/72 , C07D317/22 , C07D317/24 , C07D317/26 , C07F7/1856 , C07H15/252 , Y02P20/55
摘要： The present invention relates to new tetralins and their use for the preparation of anthracyclinones and anthracyclins. These tetralins contain at least one chiral carbon atom and correspond to the formula (V) below: ##STR1## in which: R.sub.1 and R.sub.2 denote a hydrogen atom, or a halogen atom or the group OCH.sub.3, provided that one of the two substituents (R.sub.1 or R.sub.2) must denote OCH.sub.3, andR.sub.3 denotes a hydrogen atom or the OR' group, R' being hydrogen or a hydroxyl-protecting group. Application: synthesis of glycosides of great therapeutic value.
摘要翻译：本发明涉及新的四氢化萘及其用于制备蒽环霉素和蒽环霉素的用途。这些四氢化萘含有至少一个手性碳原子，对应于下式（V）：其中：R 1和R 2表示氢原子，或卤素原子或基团OCH 3，条件是两个取代基（R1或R2）必须表示OCH3，R3表示氢原子或OR'基团，R'为氢或羟基保护基团。应用：合成糖苷具有很大的治疗价值。

8. 发明授权

US4748253A Process for preparing esters of alkanoic acids via rearrangement of alpha-haloketals 失效
标题翻译：通过α-卤代酮重排制备链烷酸酯的方法
公开(公告)号：US4748253A
公开(公告)日：1988-05-31
申请号：US329333
申请日：1981-12-10
申请人： Claudio Giordano , Aldo Belli , Fulvio Uggeri , Giovanni Villa
发明人： Claudio Giordano , Aldo Belli , Fulvio Uggeri , Giovanni Villa
IPC分类号： C07C43/174 , C07C43/225 , C07C43/30 , C07C43/303 , C07C43/315 , C07C45/63 , C07C51/00 , C07C59/64 , C07C67/475 , C07C69/734 , C07D209/48 , C07D317/16 , C07D317/18 , C07D317/22 , C07D317/28 , C07D319/06 , C07D333/16 , C07D333/22 , C07D333/24 , C07C69/76
CPC分类号： C07D209/48 , C07C43/303 , C07C43/315 , C07C45/63 , C07C51/00 , C07C59/64 , C07D317/16 , C07D317/22 , C07D317/28 , C07D319/06 , C07D333/22
摘要： Process for preparing esters of alkanoic acids via rearrangement of alpha-haloketals in the presence of a Lewis acid.The rection is preferably carried out in the presence of catalytic amounts of a Lewis acid and of a diluent at a temperature in the range from about 0.degree. to the reflux temperature of diluent.The esters thus obtained are useful as intermediate products for preparing drugs.The process involves the preparation of new alpha-haloketals.

9. 发明授权

US4707182A Phenoxine-ketal ethers, compositions containing them and the use thereof 失效
标题翻译：苯氧基 - 缩酮醚，含有它们的组合物及其用途
公开(公告)号：US4707182A
公开(公告)日：1987-11-17
申请号：US733353
申请日：1985-05-13
申请人： Henry Martin , Urs Fricker
发明人： Henry Martin , Urs Fricker
IPC分类号： A01N25/32 , A01N33/24 , A01N35/10 , A01N43/20 , A01N43/32 , A01P13/00 , C07C67/00 , C07C239/00 , C07C251/50 , C07C251/54 , C07C313/00 , C07C315/04 , C07C317/32 , C07C319/20 , C07C323/47 , C07D307/12 , C07D309/06 , C07D309/12 , C07D317/18 , C07D317/22 , C07D319/06 , C07D321/02 , C07D321/06 , C07D339/06 , C07D339/08 , A01N43/40 , A01N43/08 , C07D317/16
CPC分类号： C07D319/06 , A01N25/32 , C07D307/12 , C07D309/06 , C07D317/22 , C07D321/06 , C07D339/06 , C07D339/08
摘要： The oxime ethers of the formula I below are able to act as antidotes or safeners to protect cultivated plants from the phytotoxic effects of herbicides. Such cultivated plants are preferably sorghum, cereals, maize and rice, and herbicides are principally chloroacetanilides and thiocarbamates. The oxime ethers have the formula I ##STR1## wherein n is 1 or 2, each of R.sub.1 and R.sub.2 is hydrogen or C.sub.1 -C.sub.4 alkyl each of R.sub.3 and R.sub.4 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 haloalkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.1 -C.sub.4 haloalkylsulfinyl, C.sub.1 -C.sub.4 haloalkylsulfonyl or nitro; each of R.sub.5 and R.sub.6 independently of the other is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.2 -C.sub.8 alkoxyalkyl, C.sub.3 -C.sub.4 alkenyl, C.sub.3 -C.sub.4 alkynyl, or together form a 2- to 6-membered alkylene or alkenylene bridge which may be substituted by 1 to 4 C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.2 -C.sub.4 alkenyloxy, C.sub.2 -C.sub.8 alkoxyalkyl or C.sub.3 -C.sub.8 alkenyloxyalkyl groups; each of A and B independently of the other is oxygen or sulfur, or one of A and B is the methine group, X is a fluorinated C.sub.1 -C.sub.3 alkyl radical which may also additionally contain chlorine, and Y is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy or phenyl.
摘要翻译：以下式I的肟醚能够用作解毒剂或安全剂，以保护栽培植物免受除草剂的植物毒性作用。这样的栽培植物优选是高粱，谷物，玉米和水稻，除草剂主要是氯乙酰苯胺和硫代氨基甲酸盐。肟醚具有式I（I）其中n为1或2，R 1和R 2各自为氢或R 3和R 4各自为C 1 -C 4烷基，卤素，C 1 -C 4烷基，C 1 -C 4 卤代烷基，C1-C4烷氧基，C1-C4卤代烷氧基，C1-C4烷硫基，C1-C4卤代烷硫基，C1-C4烷基亚磺酰基，C1-C4烷基磺酰基，C1-C4卤代烷基亚磺酰基，C1-C4卤代烷基磺酰基或硝基; R 5和R 6各自独立地是C 1 -C 4烷基，C 1 -C 4卤代烷基，C 2 -C 8烷氧基烷基，C 3 -C 4烯基，C 3 -C 4炔基，或一起形成2-至6-元亚烷基或亚烯基桥，其中可以被1至4个C 1 -C 4烷基，C 1 -C 4卤代烷基，C 1 -C 4烷氧基，C 2 -C 4烯氧基，C 2 -C 8烷氧基烷基或C 3 -C 8链烷氧基烷基取代; A和B各自独立地是氧或硫，或者A和B中的一个是次甲基，X是还可以另外含有氯的氟化的C 1 -C 3烷基，Y是氢，C 1 -C 4烷基，C 1 -C 4卤代烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷氧基或苯基。

10. 发明授权

US4690931A Therapeutically useful 1-phenyl-2-piperidinoalkanol derivatives 失效
标题翻译：治疗上有用的1-苯基-2-哌啶子基链烷醇衍生物
公开(公告)号：US4690931A
公开(公告)日：1987-09-01
申请号：US773926
申请日：1985-09-09
申请人： Alexander Wick , Jonathan Frost , Bernard Gaudilliere , Jean Bertin , Regis Dupont , Jean Rousseau
发明人： Alexander Wick , Jonathan Frost , Bernard Gaudilliere , Jean Bertin , Regis Dupont , Jean Rousseau
IPC分类号： C07D211/12 , A61K31/445 , A61K31/451 , A61P9/08 , A61P25/24 , A61P25/26 , A61P25/28 , C07C45/00 , C07C45/45 , C07C45/54 , C07C45/63 , C07C45/71 , C07C49/76 , C07C49/80 , C07C49/825 , C07C49/84 , C07C63/70 , C07C67/00 , C07C69/76 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/26 , C07D211/28 , C07D211/30 , C07D211/32 , C07D211/62 , C07D213/50 , C07D213/78 , C07D317/18 , C07D317/30
CPC分类号： C07D211/22 , C07C45/004 , C07C45/45 , C07C45/54 , C07C45/63 , C07C45/71 , C07C49/80 , C07C49/825 , C07C49/84 , C07D211/14 , C07D211/18
摘要： Compounds of the formula: ##STR1## wherein R.sub.1 is hydrogen, halogen, trifluoromethyl, alkyl, hydroxyl, alkyoxy, benzyloxy, alkanoyloxy, or benzoyloxy, or when R.sub.2 is hydroxyl or methoxy in the 4-position and R.sub.3 is hydrogen, R.sub.1 may also represent hydroxymethyl carbamoyl or alkoxycarbonyl,R.sub.2 is hydrogen, halogen, alkyl, hydroxyl, or alkoxy,R.sub.3 is hydrogen or alkyl,R.sub.4 is alkyl (in which case the compounds are (.+-.)-erythro) or when R.sub.3 represents hydrogen, R.sub.4 may also be hydrogen, and R.sub.5 is hydrogen, halogen, alkyl, alkoxy, or three methoxy groups in the 3-, 4- and 5-positions and pharmaceutically acceptable acid addition salts thereof, with the exclusion of compounds wherein:(a) one of R.sub.1 and R.sub.2 is in the 4-position and is hydroxyl, alkoxy or benzyloxy, the other is in the 3-position and is hydrogen, hydroxyl, alkoxy or benzyloxy, and R.sub.3 and R.sub.5 are hydrogen and wherein:(b) R.sub.1 is in the 4-position and is halogen, R.sub.4 is methyl and R.sub.2, R.sub.3 and R.sub.5 are hydrogen, are useful as medicaments.
摘要翻译：下式的化合物：其中R 1为氢，卤素，三氟甲基，烷基，羟基，烷氧基，苄氧基，烷酰氧基或苯甲酰氧基，或当R 4为4-位的羟基或甲氧基且R 3为氢时， R1还可以表示羟甲基氨基甲酰基或烷氧基羰基，R2是氢，卤素，烷基，羟基或烷氧基，R3是氢或烷基，R4是烷基（在这种情况下，化合物是（+/-） - 赤式）氢，R 4也可以是氢，R 5是氢，卤素，烷基，烷氧基或三个甲氧基的3-，4-和5-位及其药学上可接受的酸加成盐，其中：（ a）R1和R2中的一个是4-位，羟基，烷氧基或苄氧基，另一个是3-位，是氢，羟基，烷氧基或苄氧基，R3和R5是氢，其中：（b ）R1为4-位且为卤素，R4为甲基，R2，R3和R5为氢，可用作药物。

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