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1. 发明授权

US4719231A 3-[N-(mercaptoacyl)]amino-4-arylbutanoic acid derivatives and an analgesic agent comprising the same 失效
标题翻译： 3- [N-（巯基酰基）]氨基-4-芳基丁酸衍生物和包含其的止痛剂
公开(公告)号：US4719231A
公开(公告)日：1988-01-12
申请号：US735643
申请日：1985-05-20
申请人： Hamao Umezawa , Tomio Takeuchi , Takaaki Aoyagi , Mitsugu Hachisu , Masao Hirayama , Shinjiro Murata , Shunzo Fukatsu
发明人： Hamao Umezawa , Tomio Takeuchi , Takaaki Aoyagi , Mitsugu Hachisu , Masao Hirayama , Shinjiro Murata , Shunzo Fukatsu
IPC分类号： A61K31/165 , A61K31/195 , A61K31/215 , A61P25/04 , C07C67/00 , C07C313/00 , C07C323/60 , C07C327/32 , C07C153/017 , C07C149/41 , C07C149/43 , C07C153/023
CPC分类号： C07C323/60
摘要： New 3-[N-(mercaptoacyl)]amino-4-arylbutanoic acid derivatives are now provided, which exhibit analgesic activity and are effective to enhance the analgesia induced by a known analgesic compound, ]D-ala.sup.2,met.sup.5 ]-enkephalin (DAME).
摘要翻译：现在提供新的3- [N-（巯基乙酰基）]氨基-4-芳基丁酸衍生物，其显示镇痛活性并且有效增强已知镇痛化合物[D-ala2，met5] - 脑啡肽（DAME）诱导的镇痛）。

2. 发明授权

US4518613A Thioalkanoyl-carnitines, process for their preparation and mucolytic pharmaceutical compositions containing same 失效
标题翻译：硫酰基肉碱，其制备方法和含有它们的粘液溶解药物组合物
公开(公告)号：US4518613A
公开(公告)日：1985-05-21
申请号：US436190
申请日：1982-10-22
申请人： Claudio Cavazza , Maria O. Tinti
发明人： Claudio Cavazza , Maria O. Tinti
IPC分类号： C07C327/28 , A61K20060101 , A61K31/14 , A61K31/205 , A61K31/255 , A61K31/265 , A61P11/00 , A61P11/14 , C07C20060101 , C07C67/00 , C07C325/00 , C07C327/22 , C07D405/06 , C07C153/017
CPC分类号： C07C327/32 , A61K9/0019 , A61K9/0031 , A61K9/0078 , A61K9/009 , A61K9/0095 , A61K9/02
摘要： Thioalkanoyl-carnitines of general formula (I) ##STR1## wherein R is a straight alkylene radical having from 2 to 6 carbon atoms, or is a branched alkylene radical having from 3-6 carbon atoms, or is a branched alkylene radical having from 3-6 carbon atoms,R.sub.1 is a straight or branched lower alkyl radical having from 1 to 4 carbon atoms, andX.sup.- is a halogen anionare prepared by reacting a thio-acid (II) of general formula R.sub.1 COSH(a) if in (I) the thioalkanoyl radical R.sub.1 COS-- is in terminal position, with a compound of general formula (III) ##STR2## wherein n is an integer comprised between 0 and 4 or(b) if in (I) the thioalkanoyl radical R.sub.1 COS-- is not in terminal position, with a compound of general formula (IV) ##STR3## wherein m and m.sup.1 are integers comprised between 0 and 3, andR.sub.2 is a lower alkyl radical having from 1 to 4 carbon atoms.The pharmaceutical compositions containing the thioalkanoyl-carnitines (I) possess mucolytic and antitussive activity.
摘要翻译：通式（I）的硫代酰基 - 肉碱其中R是具有2至6个碳原子的直链亚烷基，或是具有3-6个碳原子的支链亚烷基，或是具有3个 -6个碳原子，R 1是具有1至4个碳原子的直链或支链低级烷基，X-是卤素阴离子是通过使通式R 1 COSH（a）的硫代酸（II）如果在（ I）硫代烷酰基R1COS-位于末端，与通式（III）的化合物其中n是0至4之间的整数，或（b）如果在（I）中硫代烷酰基R1COS-不是在末端位置与通式（IV）的化合物其中m和m1是0和3之间的整数，R2是具有1至4个碳原子的低级烷基。含有硫代链烷酰基肉碱（I）的药物组合物具有粘液分解和镇咳活性。

3. 发明授权

US4028408A Novel preparation of trifluoromethylthioacetic acid 失效
标题翻译：三氟代硫代乙酸的新型制备
公开(公告)号：US4028408A
公开(公告)日：1977-06-07
申请号：US677190
申请日：1976-04-15
申请人： Sidney Harry Levinson , Wilford Lee Mendelson
发明人： Sidney Harry Levinson , Wilford Lee Mendelson
IPC分类号： C07B61/00 , B01J27/00 , B01J27/06 , C07C67/00 , C07C313/00 , C07C319/14 , C07C323/12 , C07D501/02 , C07C149/16 , C07C148/00 , C07C153/017
CPC分类号： C07C323/00
摘要： Methods and intermediates are disclosed for the preparation of trifluoromethylthioacetic acid using the reaction of trifluoromethylsulfenyl halides with certain orthoesters.
摘要翻译：公开了使用三氟甲基硫基卤化物与某些原酸酯反应制备三氟甲硫基乙酸的方法和中间体。

4. 发明授权

US4647562A Anti-spasmodic agents having three branch chains 失效
标题翻译：具有三条支链的抗痉挛剂
公开(公告)号：US4647562A
公开(公告)日：1987-03-03
申请号：US703263
申请日：1985-02-20
申请人： William M. Davis
发明人： William M. Davis
IPC分类号： C07D295/088 , A61K31/54 , A61K31/265 , C07C153/017 , C07D279/12
CPC分类号： C07D295/088
摘要： A new class of anti-spasmodic compounds having three branch chains is provided. These compounds have the general formula: ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are saturated straight chain or branched alkyl groups contained from 1 to 8 carbon atoms, and are separated or linked to one another to form an aliphatic ring system. k is an integer from 0 to 5, and the total number of carbon atoms in R.sub.1 plus R.sub.2 plus R.sub.3 plus k are equal to or less than 12. Furthermore, l is an integer from 1 to 3, m is an integer from 1 to 3, n is an integer from 1 to 3, and X may be nonexistent or may be O, S, NH or CH.sub.2 or salts thereof. However, when X is nonexistent the terminal group in both the m chain and the n chain is a methyl group.
摘要翻译：提供了一类新的具有三条支链的抗痉挛化合物。这些化合物具有以下通式：其中R 1，R 2和R 3是含有1至8个碳原子的饱和直链或支链烷基，并且彼此分离或连接以形成脂族环系。 k为0〜5的整数，R1 + R2 + R3 + k中的碳原子总数等于或小于12.此外，l为1〜3的整数，m为1〜 3，n为1〜3的整数，X可以不存在，也可以为O，S，NH或CH 2或其盐。然而，当X不存在时，m链和n链中的末端基团是甲基。

5. 发明授权

US4564478A Fluorinated thiocarbonic acid ester-fluorides 失效
标题翻译：氟化硫代碳酸酯 - 氟化物
公开(公告)号：US4564478A
公开(公告)日：1986-01-14
申请号：US670693
申请日：1984-11-13
申请人： Erich Klauke , Engelbert Kuhle
发明人： Erich Klauke , Engelbert Kuhle
IPC分类号： C07C323/52 , A01N37/02 , C07C67/00 , C07C313/00 , C07C325/00 , C07C327/00 , C07C329/00 , C07C329/02 , C07C333/02 , C07C153/017 , C07C148/00 , C07C153/023
CPC分类号： C07C329/00 , C07C323/00
摘要： Novel fluorinated thiocarbonic acid ester-fluorides of the formula ##STR1## in which R.sup.1 represents alkyl, cycloalkyl or optionally substituted aryl andR.sup.2 and R.sup.3 independently of one another represent hydrogen or alkyl, orR.sup.1 and R.sup.2 together represent an alkylene chain,a new process for the preparation of the new compounds and their use as intermediates for the preparation of compounds having herbicidal properties.Novel intermediates of the formulae ##STR2## in which R.sup.2 and R.sup.3 have the above-mentioned meaning,R.sup.4 is optionally substituted aryl,R.sup.5 is alkyl or cycloalkyl, andX is fluorine or chlorine, at least one X representing chlorine.
摘要翻译：式（I）的新型氟代硫代碳酸酯 - 氟化物，其中R 1表示烷基，环烷基或任选取代的芳基，R 2和R 3彼此独立地表示氢或烷基，或者R 1和R 2一起表示亚烷基链，用于制备新化合物的新方法及其作为制备具有除草性的化合物的中间体的用途。其中R 2和R 3具有上述含义的式“IMAGE”的新型中间体，R 4是任选取代的芳基，R 5是烷基或环烷基，X是氟或氯，至少一个X代表氯。

6. 发明授权

US4549992A Antihypertensive amides 失效
标题翻译：抗高血压药物
公开(公告)号：US4549992A
公开(公告)日：1985-10-29
申请号：US355830
申请日：1982-03-08
申请人： John T. Suh , Jerry W. Skiles , Bruce E. Williams , Alfred Schwab
发明人： John T. Suh , Jerry W. Skiles , Bruce E. Williams , Alfred Schwab
IPC分类号： C07C327/20 , C07D207/08 , C07D211/26 , C07D213/40 , C07D213/75 , C07D217/22 , C07D219/14 , C07D235/30 , C07D239/42 , C07D277/46 , C07D307/52 , C07D307/66 , C07D307/82 , C07D309/14 , C07D317/66 , C07D319/18 , C07D333/20 , C07D333/36 , C07D333/48 , C07C153/017
CPC分类号： C07D213/40 , C07C327/00 , C07D207/08 , C07D211/26 , C07D213/75 , C07D217/22 , C07D219/14 , C07D235/30 , C07D239/42 , C07D277/46 , C07D307/52 , C07D307/66 , C07D307/82 , C07D309/14 , C07D317/66 , C07D319/18 , C07D333/20 , C07D333/36 , C07D333/48
摘要： Compounds of the structure: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are independently hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, or cycloalkyl,n is an integer from 0 to 4 inclusive,M is alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, polycycloalkyl, polycyclo-alkyl-alkyl, aryl, aryalkyl, heteroaryl, heteroaryl-alkyl, hetero-cycloalkyl, hetero-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, dialkylaminoalkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused hetero-aryl-cycloalkyl, or fused heteroaryl-cycloalkyl-alkyl,Y is hydroxy, alkoxy, amino, or substituted amino, amino-alkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy, andR.sub.7 is a group of the formula ##STR2## wherein X is a branched alkane or cycloalkyl; and where Y is hydroxy their non-toxic, pharmaceutically acceptable alkali metal, alkaline earth metal, and amine salts.The compounds of this invention and their salts possess antihypertensive and angiotensin converting enzyme inhibitory activity.
摘要翻译：结构化合物：其中R 1，R 2，R 3，R 4，R 5和R 6独立地为氢，烷基，烯基，炔基，苯基 - 烷基或环烷基，n为0-4的整数，M为烯基，炔基，环烷基，环烷基 - 烷基，多环烷基，多环烷基 - 烷基，芳基，芳烷基，杂芳基，杂芳基 - 烷基，杂环烷基，杂环烷基 - 烷基，烷氧基烷基，烷硫基烷基，烷基氨基 - 烷基，二烷基氨基烷基，稠合芳基稠合芳基 - 环烷基 - 烷基，稠合杂芳基 - 环烷基或稠合杂芳基 - 环烷基 - 烷基，Y是羟基，烷氧基，氨基或取代的氨基，氨基 - 烷酰基，芳氧基，氨基烷氧基或羟基烷氧基，R7 是下式的基团：其中X是支链烷烃或环烷基; 并且其中Y是羟基，它们是无毒的药学上可接受的碱金属，碱土金属和胺盐。本发明化合物及其盐具有抗高血压和血管紧张素转化酶的抑制活性。

7. 发明授权

US4759881A Process for the preparation of trifluorodichloroethyl-substituted acids and zinc compounds 失效
标题翻译：制备三氟氯乙基取代的酸和锌化合物的方法
公开(公告)号：US4759881A
公开(公告)日：1988-07-26
申请号：US835481
申请日：1986-03-03
申请人： Robert W. Lang , Bernd Klingert
发明人： Robert W. Lang , Bernd Klingert
IPC分类号： C07C53/21 , C07C51/00 , C07C51/10 , C07C51/15 , C07C67/00 , C07C313/00 , C07C313/04 , C07C325/00 , C07C327/06 , C07F3/06 , C07C153/017 , C07C145/00
CPC分类号： C07C313/04 , C07C327/00 , C07C51/15 , C07F3/06
摘要： Zinc compounds of formula IICF.sub.3 CCl.sub.2 ZnCl.yL (II)wherein y is 1 or 2 and L is a solvent ligand selected from the group of the N-disubstituted acid amides, N-substituted lactams and the organic sulfoxides, are suitable for reaction with CO.sub.2, COS or SO.sub.2 to give, after working up, the acids of formula ICF.sub.3 CCl.sub.2 --X (I)wherein X is --CO.sub.2 H, --CSOH or --SO.sub.2 H, in good yield.
摘要翻译：式II的锌化合物CF3CCl2ZnCl.yL（Ⅱ）其中y是1或2，L是选自N-二取代的酰胺，N-取代的内酰胺和有机亚砜的溶剂配体，适于与CO 2反应，COS或SO 2，在加工后，以良好的收率得到其中X是-CO 2 H，-CSOOH或-SO 2 H的式I的CF 3 CCl 2 -X（I）的酸。

8. 发明授权

US4466914A Process for the conversion of primary and secondary alcohols to their corresponding thiols and thiol esters 失效
标题翻译：将伯和仲醇转化成其相应的硫醇和硫醇酯的方法
公开(公告)号：US4466914A
公开(公告)日：1984-08-21
申请号：US270321
申请日：1981-06-04
申请人： George G. Hazen , Ralph P. Volante
发明人： George G. Hazen , Ralph P. Volante
IPC分类号： C07B45/06 , C07C327/20 , C07C405/00 , C07D205/08 , C07D477/02 , C07J31/00 , C07C149/18 , C07C153/01 , C07C153/017 , C07C153/023
CPC分类号： C07J31/006 , C07B45/06 , C07C319/02 , C07C327/22 , C07C405/00 , C07C405/0033 , C07D205/08 , C07D477/02 , C07B2200/07 , C07C2101/10
摘要： Disclosed is a mild, efficient, stereo-selective process for a one step conversion of primary and secondary alcohols to their corresponding thiol ester and thiol derivatives with inversion of configuration. The process comprises the reaction of the alcohol in question (4), the thiolacid of choice (5) in the presence of adduct 3; the resulting thiol ester 6 may be converted to the free thiol 7 by hydrolysis or reductive methods: ##STR1##
摘要翻译：公开了一种温和的，有效的立体选择性方法，用于将伯醇和仲醇转化成其相应的硫醇酯和硫醇衍生物并进行反相配置。该方法包括所讨论的醇（4），选择的硫醇（5）在加合物3的存在下的反应; 所得到的硫羟酸酯6可以通过水解或还原方法转化成游离硫醇7：

9. 发明授权

US4297282A Resolution of mercaptopropionic acids 失效
标题翻译：巯基丙酸的分辨率
公开(公告)号：US4297282A
公开(公告)日：1981-10-27
申请号：US90857
申请日：1979-11-02
申请人： Naohito Ohashi , Shoji Nagata , Junki Katsube
发明人： Naohito Ohashi , Shoji Nagata , Junki Katsube
IPC分类号： C07C327/00 , C07D207/16 , C07C153/017
CPC分类号： C07C327/00 , C07D207/16
摘要： This invention relates to a process for the optical resolution of DL-.alpha.-methyl-.beta.-acylthiopropionic acids of the formula [I], ##STR1## wherein R is a lower alkyl group having 1-4 carbon atoms, phenyl or substituted phenyl bearing methyl or chloro radical; a method for the racemization of an optically active .alpha.-methyl-.beta.-acylthiopropionic acid of the formula [Ia], ##STR2## wherein R is as defined above; and a process for the synthesis of captopril of the formula [II], ##STR3## using the D-acid [Ia] as an intermediate. The optically active .alpha.-methyl-.beta.-acylthiopropionic acids are useful as intermediates for the production of medicines, for example, captopril or its congeners.
摘要翻译：本发明涉及一种用于光学拆分式[I]，其中R是具有1-4个碳原子的低级烷基的式[I]，其中R 1是苯基或取代的含甲基或氯基的苯基; 式[Ia]的光学活性α-甲基-β-酰基硫代丙酸外消旋化的方法，其中R如上定义; 以及使用D-酸[Ia]作为中间体合成式[II]，IMAGE [II]的卡托普利的方法。光学活性α-甲基-β-酰基硫代丙酸可用作生产药物的中间体，例如卡托普利或其同系物。

10. 发明授权

US4705880A Carbonylation of mercaptans 失效
标题翻译：硫醇的羰基化
公开(公告)号：US4705880A
公开(公告)日：1987-11-10
申请号：US870187
申请日：1986-06-03
申请人： Howard Alper , David J. H. Smith
发明人： Howard Alper , David J. H. Smith
IPC分类号： C07B61/00 , B01J31/00 , B01J31/02 , C07C20060101 , C07C67/00 , C07C325/00 , C07C327/02 , C07C327/06 , C07C327/20 , C07C327/26 , C07C153/017 , C07C153/023
CPC分类号： C07C327/00
摘要： Thioesters of the formula RCOSR are produced from a mercaptan of the formula RSH wherein R is a benzylic, aromatic or aliphatic moiety by reacting the mercaptan with carbon monoxide in the presence of a polyunsaturated olefinic hydrocarbon and as catalyst a metal component selected from iron, cobalt, nickel, molybdenum, ruthenium, rhodium and iridium, the metal component being in free or combined form.
摘要翻译：式RCOSR的硫代酯由式RSH的硫醇制备，其中R是苄基，芳族或脂族部分，通过在多不饱和烯烃存在下使硫醇与一氧化碳反应，并作为催化剂选择铁，钴，镍，钼，钌，铑和铱，金属组分为游离或组合形式。

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