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41. 发明授权

US06127383A 2-aryl-substituted pyridines 失效
标题翻译： 2-芳基取代的吡啶
公开(公告)号：US06127383A
公开(公告)日：2000-10-03
申请号：US217214
申请日：1998-12-21
申请人： Gunter Schmidt , Rolf Angerbauer , Arndt Brandes , Michael Logers , Matthias Muller-Gliemann , Hilmar Bischoff , Delf Schmidt , Stefan Wohlfeil
发明人： Gunter Schmidt , Rolf Angerbauer , Arndt Brandes , Michael Logers , Matthias Muller-Gliemann , Hilmar Bischoff , Delf Schmidt , Stefan Wohlfeil
IPC分类号： C07D221/18 , A61K31/435 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/455 , A61P3/06 , A61P9/10 , C07D213/26 , C07D213/30 , C07D213/38 , C07D213/50 , C07D213/53 , C07D401/06 , C07D417/06 , A61K31/4709
CPC分类号： C07D213/30 , C07D213/38 , C07D213/50 , C07D401/06 , C07D417/06
摘要： The 2-aryl-substituted pyridines are prepared by reacting pyridylaldehydes with organometallic compounds and then selectively reducing the products. The 2-aryl-substituted pyridines are suitable as active compounds in medicaments, in particular in medicaments for the treatment of arteriosclerosis.
摘要翻译： 2-芳基取代的吡啶通过使吡啶基醛与有机金属化合物反应然后选择性还原产物来制备。 2-芳基取代的吡啶适合作为药物中的活性化合物，特别是用于治疗动脉硬化的药物。

42. 发明授权

US6063788A Bicyclic-fused pyridines 失效
标题翻译：双环稠合吡啶
公开(公告)号：US6063788A
公开(公告)日：2000-05-16
申请号：US883067
申请日：1997-06-27
申请人： Arndt Brandes , Michael Logers , Gunter Schmidt , Rolf Angerbauer , Carsten Schmeck , Klaus-Dieter Bremm , Hilmar Bischoff , Delf Schmidt , Joachim Schuhmacher
发明人： Arndt Brandes , Michael Logers , Gunter Schmidt , Rolf Angerbauer , Carsten Schmeck , Klaus-Dieter Bremm , Hilmar Bischoff , Delf Schmidt , Joachim Schuhmacher
IPC分类号： C07D221/04 , A61K31/435 , A61K31/44 , A61P3/06 , A61P9/00 , A61P9/10 , C07D221/16
CPC分类号： C07D221/16
摘要： Bicyclic-fused pyridines are prepared by introducing the appropriate side chain by reaction of the corresponding aldehydes with the aid of Wittig or Grignard reagents. The bicyclic-fused pyridines are suitable as active compounds in medicaments, in particular in medicaments for the treatment of arteriosclerosi.
摘要翻译：通过使用相应的醛借助Wittig或格氏试剂引入合适的侧链来制备双环稠合的吡啶。双环稠合的吡啶适合作为药物中的活性化合物，特别是用于治疗动脉硬化的药物。

43. 发明授权

US5409910A Substituted pyridines 失效
标题翻译：取代吡啶
公开(公告)号：US5409910A
公开(公告)日：1995-04-25
申请号：US169804
申请日：1993-12-17
申请人： Rolf Angerbauer , Peter Fey , Walter Hubsch , Thomas Philipps , Hilmar Bischoff , Hans-Peter Krause , Jorg P. von Gehr , Delf Schmidt
发明人： Rolf Angerbauer , Peter Fey , Walter Hubsch , Thomas Philipps , Hilmar Bischoff , Hans-Peter Krause , Jorg P. von Gehr , Delf Schmidt
IPC分类号： A61K31/44 , A61K31/4418 , A61K31/443 , A61K31/445 , A61K31/66 , A61P3/06 , A61P9/10 , A61P43/00 , C07D213/30 , C07D213/48 , C07D213/50 , C07D213/74 , C07D405/06 , C07F9/58 , A61K31/675 , C07D401/00
CPC分类号： C07D213/30 , C07D405/06
摘要： New substituted pyridines are prepared by reducing suitably substituted pyridine derivatives. The new substituted pyridines are suitable as active compounds in pharmaceuticals, in particular for the treatment of hyperlipoproteinaemia.
摘要翻译：通过还原适当取代的吡啶衍生物制备新的取代的吡啶。新的取代的吡啶适合作为药物中的活性化合物，特别是用于治疗高脂蛋白血症。

44. 发明授权

US5137881A Substituted pyrido-oxazine inhibitors of HMG-COA reductase 失效
标题翻译： HMG-COA还原剂的替代吡咯烷氧化酶抑制剂
公开(公告)号：US5137881A
公开(公告)日：1992-08-11
申请号：US730404
申请日：1991-07-16
申请人： Walter Hubsch , Rolf Angerbauer , Peter Fey , Hilmar Bischoff , Joachim Bender , Delf Schmidt
发明人： Walter Hubsch , Rolf Angerbauer , Peter Fey , Hilmar Bischoff , Joachim Bender , Delf Schmidt
IPC分类号： A61K31/535 , A61K31/66 , A61K31/675 , A61P3/06 , A61P9/10 , A61P43/00 , C07D498/04 , C07F9/6561 , C12N9/99
CPC分类号： C07D498/04 , C07F9/6561
摘要： Substituted pyrido-oxazines can be prepared by reduction of the corresponding ketones. They are useful active compounds in medicaments, in particular for the treatment of hyperlipoproteinaemia, lipoproteinaemia and arteriosclerosis.
摘要翻译：取代的吡啶并恶嗪可以通过还原相应的酮来制备。它们是药物中有用的活性化合物，特别是用于治疗高脂蛋白血症，脂蛋白血症和动脉硬化。

45. 发明授权

US5120782A Substituted pyrrolo-pyridines pharmaceuticals 失效
标题翻译：取代吡咯并吡啶药物
公开(公告)号：US5120782A
公开(公告)日：1992-06-09
申请号：US724414
申请日：1991-06-28
申请人： Walter Hubsch , Rolf Angerbauer , Peter Fey , Hilmar Bischoff , Joachim Bender , Delf Schmidt
发明人： Walter Hubsch , Rolf Angerbauer , Peter Fey , Hilmar Bischoff , Joachim Bender , Delf Schmidt
IPC分类号： A61K31/435 , A61K31/675 , A61P3/06 , A61P9/10 , C07D471/04 , C07F9/6561
CPC分类号： C07D471/04 , C07F9/6561
摘要： Substituted pyrrolo-pyridines can be prepared by reduction of the corresponding ketones. They are useful active compounds for medicaments and can be employed, for example, for the treatment of hyperlipoproteinaemia, lipoproteinaemia and arteriosclerosis.
摘要翻译：取代的吡咯并 - 吡啶可以通过还原相应的酮来制备。它们是用于药物的有用的活性化合物，并且可以用于例如治疗高脂蛋白血症，脂蛋白血症和动脉硬化。

46. 发明授权

US5006530A Certain 7-[2,6-diisopropyl-4-phenyl-5-lower alkoxymethyl-pyrid-3-yl]-3,5-dihydroxy-6-enoates and derivatives useful for treating circulatory diseases 失效
标题翻译：某些7- [2,6-二异丙基-4-苯基-5-低级烷氧基甲基 - 吡啶-3-基] -3,5-二羟基-6-烯酸酯和可用于治疗循环系统疾病的衍生物
公开(公告)号：US5006530A
公开(公告)日：1991-04-09
申请号：US298549
申请日：1989-01-17
申请人： Rolf Angerbauer , Peter Fey , Walter Hubsch , Thomas Philipps , Hilmar Bischoff , Dieter Petzinna , Delf Schmidt , Gunter Thomas
发明人： Rolf Angerbauer , Peter Fey , Walter Hubsch , Thomas Philipps , Hilmar Bischoff , Dieter Petzinna , Delf Schmidt , Gunter Thomas
IPC分类号： C07D333/24 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61P3/06 , A61P9/10 , C07D211/90 , C07D213/30 , C07D213/42 , C07D213/48 , C07D213/55 , C07D213/80 , C07D213/82 , C07D213/84 , C07D213/85 , C07D213/89 , C07D307/54 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07F7/08 , C07F7/18
CPC分类号： C07D213/80 , C07D213/55 , C07D213/82 , C07D213/85 , C07D213/89 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07F7/0812 , C07F7/0818 , C07F7/1856
摘要： Novel compounds for treating hyperproteinaemia, lipoproteinaemia or arteriosclerosis of the formula ##STR1## in which A, B, D and E can have varied meanings,X is --CH.sub.2 --CH.sub.2 or --CH.dbd.CH--, andR is ##STR2## wherein R.sup.21 denotes hydrogen or alkyl andR.sup.22denotes hydrogen,denotes alkyl, aryl or aralkyl, ordenotes a cation,and their oxidation products.
摘要翻译：用于治疗高蛋白血症，脂蛋白血症或动脉硬化的新型化合物，其中A，B，D和E可以具有不同含义，X是-CH 2 -CH 2或-CH = CH-，R是

47. 发明授权

US4937255A Disubstituted pyrroles 失效
标题翻译：二取代的吡咯
公开(公告)号：US4937255A
公开(公告)日：1990-06-26
申请号：US325273
申请日：1989-03-16
申请人： Walter Hubsch , Rolf Angerbauer , Peter Fey , Hilmar Bischoff , Dieter Petzinna , Delf Schmidt , Gunter Thomas
发明人： Walter Hubsch , Rolf Angerbauer , Peter Fey , Hilmar Bischoff , Dieter Petzinna , Delf Schmidt , Gunter Thomas
IPC分类号： C07D207/33 , A61K31/40 , A61K31/4025 , A61P3/00 , A61P9/10 , A61P43/00 , C07D207/32 , C07D207/333 , C07D207/337 , C07D207/34 , C07D405/06 , C07D405/14
CPC分类号： C07D207/333 , C07D207/337 , C07D405/06
摘要： For inhibiting 3-hydroxy-3-methylglutaryl coenzyme A and cholesterol biosynthesis, the novel disubstituted pyrroles of the formula ##STR1## in which R.sup.1 is aryl or heteroaryl,R.sup.2 is cycloalkyl or optionally substituted alkyl,R.sup.3 is hydrogen or cycloalkyl, or optionally substituted alkyl, aryl or heteroaryl,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.6 is hydrogen or alkyl, and R.sup.7 is hydrogen, a cation or alkyl, aryl or aralkyl.
摘要翻译：为了抑制3-羟基-3-甲基戊二酰辅酶A和胆固醇生物合成，其中R 1为芳基或杂芳基，R 2为环烷基或任选取代的烷基，R 3为氢或环烷基的式（I）的新二取代吡咯，或任选取代的烷基，芳基或杂芳基，X为-CH 2 -CH 2 - 或-CH = CH-，A为R 6为氢或烷基，R 7为氢，阳离子或烷基，芳基或芳烷基。

48. 发明授权

US4307194A Inhibitors, obtained from bacilli, for glycoside hydrolases 失效
标题翻译：抑制剂，从杆菌获得，用于糖苷水解酶
公开(公告)号：US4307194A
公开(公告)日：1981-12-22
申请号：US858036
申请日：1977-12-06
申请人： Werner Frommer , Lutz Muller , Delf Schmidt , Walter Puls , Hans-Peter Krause , Ulrich Heber
发明人： Werner Frommer , Lutz Muller , Delf Schmidt , Walter Puls , Hans-Peter Krause , Ulrich Heber
IPC分类号： C12P17/12 , A23K1/17 , A23K1/18 , A61K31/445 , A61K35/74 , C07D211/46 , C12N1/20 , C12N9/99 , C12P1/04 , C12P19/26 , C12R1/07 , C12R1/12 , C12R1/125
CPC分类号： C12R1/07 , A23K20/195 , A23K50/30 , A61K31/445 , C12N1/20 , C12P1/04 , Y10S435/832 , Y10S435/839
摘要： According to the present invention inhibitors for glycoside hydrolases, and in particular glucosidase inhibitors especially saccharase inhibitors, which are active in the digestive tract are formed by culturing organisms of the family Bacillaceae, particularly by strains of the genus Bacillus.It has also been found that certain strains of organisms of the family Bacillaceae, especially strains DSM 7, DSM 704 and DSM 675 produce the antibiotic known as 1-desoxynojirimycin. The invention therefore provides a method of producing 1-desoxynojirimycin which comprises culturing a 1-desoxynojirimycin producing organism of the genus Bacillus. Inhibitors for glycoside hydrolases and the invention includes methods for producing such inhibitors, pharmaceutical compositions containing the inhibitors and methods of treatment involving the use of the inhibitors.
摘要翻译：根据本发明，通过培养家蚕科的生物体，特别是通过芽孢杆菌属的菌株形成糖苷水解酶抑制剂，特别是在消化道中有活性的葡糖苷酶抑制剂，特别是糖酶抑制剂。还已经发现，芽孢杆菌科的特定菌株DSM 7，DSM 704和DSM 675的生物体产生称为1-脱氧野尻霉素的抗生素。因此，本发明提供了一种生产1-脱氧野尻霉素的方法，该方法包括培养产生芽孢杆菌属的1-脱氧诺伊霉素生物的生物。糖苷水解酶和本发明的抑制剂包括制备这种抑制剂的方法，含有抑制剂的药物组合物和涉及使用抑制剂的治疗方法。

49. 发明授权

US4013510A Glycoside-hydrolase enzyme inhibitors 失效
标题翻译：糖苷 - 水解酶抑制剂
公开(公告)号：US4013510A
公开(公告)日：1977-03-22
申请号：US493463
申请日：1974-07-31
申请人： Werner Frommer , Walter Puls , Dietmar Schafer , Delf Schmidt
发明人： Werner Frommer , Walter Puls , Dietmar Schafer , Delf Schmidt
IPC分类号： C12P1/04 , C12P1/06 , C12D13/00
CPC分类号： A61K31/70 , C12P1/04 , C12P1/06 , Y10S435/803 , Y10S435/822 , Y10S435/827 , Y10S435/886 , Y10S435/889 , Y10S435/896 , Y10S435/907 , Y10S435/911
摘要： This invention relates to inhibitors for glycosidehydrolases derived from bacteria of the order Actinomycetales, means for their production comprising cultivation of a microorganism of the order Actinomycetales in appropriate nutrient solutions under conditions most favorable to growth and production of the enzyme inhibitor and recovering, as a new product, glycoside-hydrolase enzyme inhibitors, from the culture as well as the use of said enzyme inhibitors in pharmaceutically acceptable therapeutic compositions in the treatment of conditions indicating obesity, diabetes, pre-diabetes, gastritis, gastric ulcer, hyperlipidemia (arteriosclerosis) and the like. The invention also contemplates the provision of methods of inhibiting the reaction of carbohydrates and glycoside-hydrolase enzymes and particularly carbohydrate-splitting glycoside-hydrolase enzymes of the digestive tract by means of conducting said reaction of said carbohydrates and glycoside-hydrolase enzymes in the presence of a glycoside-hydrolase enzyme inhibitor for said glycoside-hydrolase enzyme derived from a strain of microorganism of the order Actinomycetales. The invention further contemplates the provision of methods for the treatment of indications of the group consisting of obesity, adipose, hyperlipidemia (arteriosclerosis), diabetes, pre-diabetes, gastritis, gastric ulcer, duodenal ulcer, and caries induced by the action of glycoside-hydrolase enzymes and carbohydrates, the improvement which comprises employing an enzyme inhibitor for glycoside-hydrolase enzymes produced by a strain of microorganism of the order Actinomycetales.
摘要翻译：本发明涉及来自放线菌纲序列的细菌的糖苷水解酶的抑制剂，其生产方法包括在最有利于生长和产生酶抑制剂的条件下，在适当的营养液中培养放线菌纲的微生物，并作为新的产品，糖苷 - 水解酶抑制剂，以及所述酶抑制剂在药学上可接受的治疗组合物中用于治疗指示肥胖，糖尿病，前期糖尿病，胃炎，胃溃疡，高脂血症（动脉硬化）和喜欢。本发明还考虑提供通过在所述碳水化合物和糖苷 - 水解酶的存在下进行所述碳水化合物和糖苷 - 水解酶的反应来抑制碳水化合物和糖苷 - 水解酶，特别是消化道的碳水化合物 - 裂解糖苷 - 水解酶的反应的方法一种衍生自放线菌纲的微生物菌株的糖苷 - 水解酶的糖苷 - 水解酶抑制剂。本发明进一步考虑了提供治疗由肥胖，脂肪，高脂血症（动脉硬化），糖尿病，前期糖尿病，胃炎，胃溃疡，十二指肠溃疡以及由糖苷 - 水解酶和碳水化合物，其改进包括使用由抑制放线菌的微生物菌株产生的糖苷 - 水解酶的酶抑制剂。

50. 发明授权

US07192971B2 4-Heteroaryl-tetrahydroquinolines and their use as inhibitors of the cholesterin-ester transfer protein 失效
标题翻译： 4-杂芳基四氢喹啉及其作为胆固醇酯转移蛋白的抑制剂的用途
公开(公告)号：US07192971B2
公开(公告)日：2007-03-20
申请号：US11257931
申请日：2005-10-25
申请人： Jürgen Stoltefuss , Michael Lörges , Gunter Schmidt , Arndt Brandes , Carsten Schmeck , Klaus-Dieter Bremm , Hilmar Bischoff , Delf Schmidt
发明人： Jürgen Stoltefuss , Michael Lörges , Gunter Schmidt , Arndt Brandes , Carsten Schmeck , Klaus-Dieter Bremm , Hilmar Bischoff , Delf Schmidt
IPC分类号： A61K31/4709 , C07D401/04
CPC分类号： C07D401/04 , C07D215/20 , C07D409/04
摘要： Hetero-tetrahydroquinolines can be prepared either by condensing correspondingly substituted hetero-tetrahydroquinoline aldehydes with the desired substituent or by reducing the corresponding keto-substituted hetero-tetrahydroquinolines, followed by introduction of the desired substituent by customary methods. The hetero-tetrahydroquinolines are suitable for use as active compounds in medicaments, in particular in medicaments for treating artheriosclerosis and dyslipidaemias.
摘要翻译：异四氢喹啉可以通过将相应取代的杂四氢喹啉醛与所需的取代基缩合或通过还原相应的酮取代的杂四氢喹啉来制备，然后通过常规方法引入所需的取代基。杂四氢喹啉适合用作药物中的活性化合物，特别是用于治疗动物硬化和血脂异常的药物。

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