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1. 发明授权

US6124493A Process for the preparation of o-chloromethyl-phenylglyoxylic acid derivatives 有权
标题翻译：制备邻氯甲基 - 苯基乙醛酸衍生物的方法
公开(公告)号：US6124493A
公开(公告)日：2000-09-26
申请号：US174966
申请日：1998-10-19
申请人： Jean-Marie Assercq , Hans-Dieter Schneider , Albert Pfiffner , Werner Pfaff
发明人： Jean-Marie Assercq , Hans-Dieter Schneider , Albert Pfiffner , Werner Pfaff
IPC分类号： C07C229/40 , C07C69/716 , C07C69/738 , C07C69/76 , C07C229/34 , C07C229/36 , C07C249/08 , C07C251/48 , C07C251/52 , C07C251/58 , C07C251/60 , C07D295/155 , C07C229/00
CPC分类号： C07D295/155 , C07C229/34 , C07C249/08 , C07C251/48 , C07C251/60 , C07C69/738 , C07C69/76 , C07C2101/02
摘要： There is described a process for the preparation of a compound of formula I ##STR1## in which process: a) a compound of formula II ##STR2## is reacted with an organolithium compound of formula IIILi--R.sub.7 (III)b) the resulting lithium complex is reacted with a compound of formula IVY.sub.1 --CO--CO--Y.sub.1 IVto form a compound of formula V ##STR3## c) that compound is, in either order, c1) oximated with O-methylhydroxylamine; or oximated with hydroxylamine and then methylated or fluoromethylated or difluoromethylated;c2) reacted with a chloroformic acid ester.X, m, Y, R.sub.1 to R.sub.3 and R.sub.7 are as defined in the description.
摘要翻译：描述了制备式I化合物的方法，其中方法：a）使式II化合物与式IIIL-R7（III）的有机锂化合物反应b）将所得锂络合物与化合物式IVY1-CO-CO-Y1IV形成式V化合物c）该化合物以任何顺序c1）用O-甲基羟胺进行氧化; 或用羟胺肟化，然后甲基化或氟甲基化或二氟甲基化; c2）与氯甲酸酯反应。 X，m，Y，R 1至R 3和R 7如说明书中所定义。

2. 发明授权

US5756811A Process for the preparation of o-chloromethyl-phenylglyoxylic acid derivatives 失效
标题翻译：制备邻氯甲基 - 苯基乙醛酸衍生物的方法
公开(公告)号：US5756811A
公开(公告)日：1998-05-26
申请号：US774470
申请日：1996-12-30
申请人： Jean-Marie Assercq , Hans-Dieter Schneider , Albert Pfiffner , Werner Pfaff
发明人： Jean-Marie Assercq , Hans-Dieter Schneider , Albert Pfiffner , Werner Pfaff
IPC分类号： C07C229/40 , C07C69/716 , C07C69/738 , C07C69/76 , C07C229/34 , C07C229/36 , C07C249/08 , C07C251/48 , C07C251/52 , C07C251/58 , C07C251/60 , C07D295/155 , C07C229/30
CPC分类号： C07D295/155 , C07C229/34 , C07C249/08 , C07C251/48 , C07C251/60 , C07C69/738 , C07C69/76 , C07C2101/02
摘要： There is described a process for the preparation of a compound of formula I ##STR1## in which process: a) a compound of formula II ##STR2## is reacted with an organolithium compound of formula III Li--R.sub.7 (III) b) the resulting lithium complex is reacted with a compound of formula IV Y.sub.1 --CO--CO--Y.sub.1 IV to form a compound of formula V ##STR3## c) that compound is, in either order, c1) oximated with O-methylhydroxylamine; or oximated with hydroxylamine and then methylated or fluoromethylated or difluoromethylated; c2) reacted with a chloroformic acid ester. X, m, Y, R.sub.1 to R.sub.3 and R.sub.7 are as defined in the description.
摘要翻译：描述了制备式I化合物I的方法，其中方法：a）式II的化合物II与式IIIL-R7（III）的有机锂化合物反应b）将式使所得的锂络合物与式IVY1-CO-CO-Y1IV的化合物反应以形成式V的化合物c）该化合物以O-甲基羟胺为原料，以任意顺序c1）化合物; 或用羟胺肟化，然后甲基化或氟甲基化或二氟甲基化; c2）与氯甲酸酯反应。 X，m，Y，R 1至R 3和R 7如说明书中所定义。

3. 发明授权

US4282318A .alpha.-Amylase inhibitor from a streptomycete and process for its preparation 失效
标题翻译：来自链霉菌的α-淀粉酶抑制剂及其制备方法
公开(公告)号：US4282318A
公开(公告)日：1981-08-04
申请号：US109170
申请日：1980-01-02
申请人： Volker Oeding , Werner Pfaff , Laszlo Vertesy , Hans-Ludwig Weidenmuller
发明人： Volker Oeding , Werner Pfaff , Laszlo Vertesy , Hans-Ludwig Weidenmuller
IPC分类号： A61K35/74 , A61K38/55 , A61P3/06 , A61P3/08 , C07G99/00 , C07K14/005 , C07K14/195 , C07K14/36 , C07K14/41 , C12N9/99 , C12P21/00 , C12R1/465
CPC分类号： C07K14/36 , C12N9/99 , Y10S435/886 , Y10S530/82 , Y10S530/823 , Y10S530/825
摘要： Inhibitor for the glycoside hydrolases of the digestive tract, more particularly of the pancreatic .alpha.-amylase produced by fermentation of the specific microorganism Streptomyces tendae, strain 4158, as well as the variants and mutants thereof, the microbe strain per se and processes for the isolation of the inhibitor and for its purification.
摘要翻译：消化道的糖苷水解酶的抑制剂，更特别是通过特异性微生物链霉菌发酵产生的胰腺α-淀粉酶，菌株4158，以及其变体和突变体，微生物菌株本身以及分离过程的抑制剂和其纯化。

4. 发明授权

US4221815A Benzoic acids, their derivatives and process for preparing them 失效
标题翻译：苯甲酸及其衍生物及其制备方法
公开(公告)号：US4221815A
公开(公告)日：1980-09-09
申请号：US646378
申请日：1976-01-02
申请人： Rudi Weyer , Volker Hitzel , Karl Geisen , Werner Pfaff
发明人： Rudi Weyer , Volker Hitzel , Karl Geisen , Werner Pfaff
IPC分类号： C07C67/00 , C07C231/00 , C07C231/02 , C07C231/10 , C07C231/12 , C07C233/81 , C07C235/52 , C07C237/36 , C07D213/82 , C07D215/44 , C07D215/48 , C07D307/79 , C07D311/58 , C07D333/38 , A61K31/195 , C07C101/72
CPC分类号： C07D213/82 , C07D215/48 , C07D307/79 , C07D311/58 , C07D333/38 , Y10S514/866
摘要： Acyl-aminoalkyl-benzoic acid and derivates thereof show a blood sugar lowering effect upon oral administration and can be used as orally applicable hypoglycemiants.
摘要翻译：酰基 - 氨基烷基 - 苯甲酸及其衍生物在口服给药时显示降血糖作用，可用作口服降血糖药。

5. 发明授权

US3998968A Benzenesulfonyl ureas and process for their manufacture 失效
标题翻译：苯磺酰脲及其制备方法
公开(公告)号：US3998968A
公开(公告)日：1976-12-21
申请号：US559712
申请日：1975-03-19
申请人： Volker Hitzel , Werner Pfaff , Rudi Weyer , Helmut Weber
发明人： Volker Hitzel , Werner Pfaff , Rudi Weyer , Helmut Weber
IPC分类号： C07C311/58 , A61K20060101 , A61K31/00 , A61K31/17 , A61K31/18 , A61K31/64 , C07C20060101 , C07C67/00 , C07C301/00 , C07C303/36 , C07C303/38 , C07C303/40 , C07C127/00
CPC分类号： C07C311/58 , Y10S514/866
摘要： N-acylaminoalkyl-benzenesulfonyl-N'-methyl ureas, especially those of the general formula ##STR1## in which R is C.sub.1-- C.sub.4 --alkyl or a phenyl radical substituted in 2-position by alkoxy of 1 to 4 carbon atoms, phenoxy or dimethylamino and in 5-position by H, CH.sub.3, Cl or Br, their manufacture and their use as oral antidiabetics.
摘要翻译： N-酰基氨基烷基 - 苯磺酰基-N'-甲基脲，特别是其中R为C 1 -C 4 - 烷基或2-位被1-4个碳原子的烷氧基取代的苯基的通式为“IMAGE”的那些，苯氧基或二甲基氨基，在H，CH3，Cl或Br的5-位，它们的制备及其作为口服抗糖尿病药的用途。

6. 发明申请

US20120095265A1 CHEMICAL PROCESS FOR THE PRODUCTION OF HALOALKENONE ETHERS 有权
标题翻译：化学工艺生产哈洛酮类化合物
公开(公告)号：US20120095265A1
公开(公告)日：2012-04-19
申请号：US13254795
申请日：2010-03-02
申请人： David Anthony Jackson , Florian Schleth , Devender Singh Negi , Werner Pfaff
发明人： David Anthony Jackson , Florian Schleth , Devender Singh Negi , Werner Pfaff
IPC分类号： C07C45/00
CPC分类号： C07C45/65 , C07C45/41 , C07C45/455 , C07C49/255 , C07C49/175
摘要： The present invention relates to a continuous process for producing a haloalkenone ether of the Formula (I) wherein R1 is C1-C6 haloalkyl, R2 is a C1-C6 alkyl or phenyl, the process comprising:—(i) reacting, in a first continuous stirred tank reactor comprising a solvent, a halide of Formula (II) wherein R1 is as previously defined and R3 is halogen, with a vinyl ether of Formula (III) wherein R2 is as previously defined, to form an intermediate compound of Formula (IV), wherein the concentration of the vinyl ether of Formula (III) in the reaction mass is 15% or less w/w; and (ii) transferring the reaction mass from the first continuous stirred tank reactor into a subsequent continuous stirred tank reactor, wherein the conditions within the subsequent reactor permit the elimination of hydrogen halide (HR3) from the intermediate compound of Formula (IV) to provide the haloalkenone ether of Formula (I).
摘要翻译：本发明涉及制备式（I）的卤代烯酮醚的连续方法，其中R 1是C 1 -C 6卤代烷基，R 2是C 1 -C 6烷基或苯基，该方法包括：（ⅰ）连续搅拌釜反应器，其包含溶剂，式（II）的卤化物，其中R 1如前所定义且R 3是卤素，与式（III）的乙烯基醚（其中R 2如前所定义）形成中间体式 IV），其中反应物质中式（III）的乙烯基醚的浓度为w / w为15％以下; 和（ii）将反应物质从第一连续搅拌釜反应器转移到随后的连续搅拌釜反应器中，其中随后反应器中的条件允许从式（IV）的中间体化合物除去卤化氢（HR 3），以提供式（I）的卤代烯酮醚。

7. 发明授权

US4339436A .alpha.-Amylase inhibitor from a streptomycete and process for its preparation 失效
标题翻译：来自链霉菌的α-淀粉酶抑制剂及其制备方法
公开(公告)号：US4339436A
公开(公告)日：1982-07-13
申请号：US237097
申请日：1981-02-23
申请人： Volker Oeding , Werner Pfaff , Laszlo Vertesy , Hans-Ludwig Weidenmuller
发明人： Volker Oeding , Werner Pfaff , Laszlo Vertesy , Hans-Ludwig Weidenmuller
IPC分类号： A61K35/74 , A61K38/55 , A61P3/06 , A61P3/08 , C07G99/00 , C07K14/005 , C07K14/195 , C07K14/36 , C07K14/41 , C12N9/99 , C12P21/00 , C12R1/465 , A61K35/00 , A61K37/00
CPC分类号： C07K14/36 , C12N9/99 , Y10S435/886 , Y10S530/82 , Y10S530/823 , Y10S530/825
摘要： Inhibitor for the glycoside hydrolases of the digestive tract, more particularly of the pancreatic .alpha.-amylase produced by fermentation of the specific microorganism Streptomyces tendae, strain 4158, as well as the variants and mutants thereof, the microbe strain per se and processes for the isolation of the inhibitor and for its purification.
摘要翻译：消化道的糖苷水解酶的抑制剂，更特别是通过特异性微生物链霉菌发酵产生的胰腺α-淀粉酶，菌株4158，以及其变体和突变体，微生物菌株本身以及分离过程的抑制剂和其纯化。

8. 发明授权

US4157395A Benzenesulfonyl ureas 失效
标题翻译：苯磺酰脲
公开(公告)号：US4157395A
公开(公告)日：1979-06-05
申请号：US903548
申请日：1978-05-08
申请人： Volker Hitzel , Rudi Weyer , Werner Pfaff , Karl Geisen
发明人： Volker Hitzel , Rudi Weyer , Werner Pfaff , Karl Geisen
IPC分类号： C07D213/81 , A61K31/63 , A61P3/08 , A61P3/10 , C07D213/82 , C07D213/56 , A61K31/44
CPC分类号： C07D213/82 , Y10S514/866
摘要： Benzenesulfonyl ureas of the formula ##STR1## in which R, R.sup.1, X, X.sup.1 and Y have the defined meanings, and the salts thereof, process for preparing these compounds, pharmaceutical preparations containing them and their use for lowering the blood sugar level.
摘要翻译：其中R，R1，X，X1和Y具有定义的式“IMAGE”的苯磺酰脲及其盐，制备这些化合物的方法，含有它们的药物制剂及其降低血糖水平的用途。

9. 发明授权

US4226764A .alpha.-Amylase inhibitor from a streptomycete and process for its preparation 失效
标题翻译：来自链霉菌的α-淀粉酶抑制剂及其制备方法
公开(公告)号：US4226764A
公开(公告)日：1980-10-07
申请号：US870247
申请日：1978-01-17
申请人： Volker Oeding , Werner Pfaff , Laszlo Vertesy , Hans-Ludwig Weidenmuller
发明人： Volker Oeding , Werner Pfaff , Laszlo Vertesy , Hans-Ludwig Weidenmuller
IPC分类号： A61K35/74 , A61K38/55 , A61P3/06 , A61P3/08 , C07G99/00 , C07K14/005 , C07K14/195 , C07K14/36 , C07K14/41 , C12N9/99 , C12P21/00 , C12R1/465 , C07G7/028
CPC分类号： C07K14/36 , C12N9/99 , Y10S435/886 , Y10S530/82 , Y10S530/823 , Y10S530/825
摘要： Inhibitor for the glycoside hydrolases of the digestive tract, more particularly of the pancreatic .alpha.-amylase produced by fermentation of the specific microorganism Streptomyces tendae, strain 4158, as well as the variants and mutants thereof, the microbe strain per se and processes for the isolation of the inhibitor and for its purification.
摘要翻译：消化道的糖苷水解酶的抑制剂，更特别是通过特异性微生物链霉菌发酵产生的胰腺α-淀粉酶，菌株4158，以及其变体和突变体，微生物菌株本身以及分离过程的抑制剂和其纯化。

10. 发明授权

US4132795A Benzenesulfonyl ureas and their use for the treatment of diabetes mellitus 失效
标题翻译：苯磺酰脲及其用于治疗糖尿病的用途
公开(公告)号：US4132795A
公开(公告)日：1979-01-02
申请号：US797132
申请日：1977-05-16
申请人： Volker Hitzel , Rudi Weyer , Werner Pfaff , Karl Geisen
发明人： Volker Hitzel , Rudi Weyer , Werner Pfaff , Karl Geisen
IPC分类号： A61K31/44 , A61K31/4412 , A61K31/4418 , A61K31/4425 , A61K31/47 , A61P25/04 , C07D213/82 , C07D215/54 , C07D213/56 , A61K31/455
CPC分类号： C07D213/82 , C07D215/54 , Y10S514/866
摘要： Benzenesulfonyl ureas of the formula ##STR1## in which R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and Y have the defined meanings, and the salts thereof, process for preparing them, pharmaceutical preparations containing them and their use for lowering the blood sugar level.
摘要翻译：其中R，R 1，R 2，R 3，R 4和Y具有确定含义的式“IMAGE”的苯磺酰脲及其盐，其制备方法，含有它们的药物制剂及其降低血糖水平的用途。

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