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1. 发明授权

US4062950A Amino sugar derivatives 失效
标题翻译：氨基糖衍生物
公开(公告)号：US4062950A
公开(公告)日：1977-12-13
申请号：US654627
申请日：1976-02-02
申请人： Werner Frommer , Bodo Junge , Uwe Keup , Lutz Muller , Walter Puls , Delf Schmidt
发明人： Werner Frommer , Bodo Junge , Uwe Keup , Lutz Muller , Walter Puls , Delf Schmidt
IPC分类号： C07H15/207 , C12P19/26 , C12P19/28 , A61K31/71 , C07H15/20
CPC分类号： C07H15/207 , C12P19/26 , C12P19/28 , Y10S435/827
摘要： New amino sugars which are glucopyranosyl and oligoglucosidyl derivatives of 4,6-bisdesoxy-4-(4,5,6-trihydroxy-3-hydroxymethylcyclohex-2-en-1-ylamino)-.alpha.-D-glucopyranose inhibit glycoside hydrolases of the digestive tract. The compounds, of which O-{4,6-bisdesoxy-4-[1S-(1,4,6/5)-4,5,6-trihydroxy-3-hydroxymethylcyclohex-2-en-1-ylamino]-.alpha.-D-glucopyranosyl}-(1.fwdarw.4)-O-.alpha.-D-glucopyranosyl-(1.fwdarw.4)-D-glucopyranose is a representative embodiment, demonstrate both saccharase and amylase inhibiting properties.
摘要翻译：作为4,6-双脱氧-4-（4,5,6-三羟基-3-羟甲基环己-2-烯-1-基） - 吡喃葡萄糖苷的吡喃葡萄糖基和低聚葡糖苷基衍生物的新型氨基糖抑制糖苷水解酶消化道。其中O- {4,6-双脱氧-4- [1S-（1,4,6 / 5）-4,5,6-三羟基-3-羟甲基环己-2-烯-1-基氨基] - α-D-吡喃葡萄糖基} - （1-> 4）-O-D-吡喃葡萄糖基 - （1-> 4）-D-吡喃葡萄糖是代表性的实施方案，证明了糖酶和淀粉酶抑制性质。

2. 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。

3. 发明授权

US4465684A 3,4,5-Trihydroxypiperidine compounds and their use as medicaments and in animal nutrition 失效
标题翻译： 3,4,5-三羟基哌啶化合物及其用作药物和动物营养
公开(公告)号：US4465684A
公开(公告)日：1984-08-14
申请号：US323153
申请日：1981-11-20
申请人： Horst Boshagen , Bodo Junge , Jurgen Stoltefuss , Delf Schmidt , Hans P. Krause , Walter Puls
发明人： Horst Boshagen , Bodo Junge , Jurgen Stoltefuss , Delf Schmidt , Hans P. Krause , Walter Puls
IPC分类号： C07D211/36 , A61K31/445 , A61K31/4545 , A61P1/00 , A61P3/06 , A61P3/08 , A61P3/10 , A61P9/12 , A61P43/00 , C07D211/40 , C07D211/46 , C07D401/12 , C07D401/14
CPC分类号： C07D211/46 , Y10S514/866 , Y10S514/909
摘要： The invention relates, inter alia, to 3,4,5-trihydroxypiperidine compounds of Formula (I), infra, to methods for the manufacture of said compounds, to pharmaceutical compositions containing said compounds and to methods for the use of said compounds and compositions. Also included in the invention are concentrates, premixes and feedstuffs containing said compounds.
摘要翻译：本发明特别涉及式（I）的3,4,5-三羟基哌啶化合物，涉及制备所述化合物的方法，含有所述化合物的药物组合物和使用所述化合物和组合物的方法。本发明还包括含有所述化合物的浓缩物，预混物和饲料。

4. 发明授权

US3934006A Pharmaceutical compositions comprising saccharase inhibitors 失效
标题翻译：包含糖酶抑制剂的药物组合物
公开(公告)号：US3934006A
公开(公告)日：1976-01-20
申请号：US482661
申请日：1974-06-24
申请人： Werner Frommer , Walter Puls , Delf Schmidt
发明人： Werner Frommer , Walter Puls , Delf Schmidt
IPC分类号： C12P19/04 , C12P19/22 , A61K27/00
CPC分类号： C12P19/22 , C12P19/04
摘要： This invention relates to the production of saccharase inhibitors in which a polysaccharidic or oligosaccharidic amylase inhibitor is hydrolytically degraded either enzymatically or by acid hydrolysis. The invention also relates to the use of said saccharase inhibitors in pharmaceutically acceptable therapeutic compositions in the treatment of conditions indicating adiposity, hyperlipaemia (atherosclerosis), diabetes, pre-diabetes, caries and the like.
摘要翻译：本发明涉及糖酶抑制剂的生产，其中多糖或寡糖淀粉酶抑制剂通过酶促或通过酸水解进行水解降解。本发明还涉及所述糖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，高脂血症（动脉粥样硬化），糖尿病，前期糖尿病，龋齿等的病症的用途。

5. 发明授权

US4019960A Process for the production of a saccharase inhibitor 失效
标题翻译：生产糖酶抑制剂的方法
公开(公告)号：US4019960A
公开(公告)日：1977-04-26
申请号：US336741
申请日：1973-02-28
申请人： Werner Frommer , Walter Puls , Delf Schmidt
发明人： Werner Frommer , Walter Puls , Delf Schmidt
IPC分类号： C12N9/99 , A61K38/55 , C12P1/06 , C12R1/045 , C12D13/02
CPC分类号： C12P1/06 , Y10S435/803 , Y10S435/822
摘要： The invention relates to a saccharase inhibitor derived from Actinoplanaceae Strain CBS 961.70, including mutants and variants thereof, means for the production of said saccharase inhibitors comprising cultivation of Actinoplanaceae Strain CBS 961.70, including mutants and variants thereof, in appropriate nutrient solutions which are characterized by being starch free under conditions most favorable to growth and production of said saccharase inhibitor and recovering a saccharase inhibitor from culture broths of said nutrient solutions, as well as the use of said inhibitor in pharmaceutically acceptable therapeutic compositions suitable for use in the treatment and relief of conditions indicative of adiposity, diabetes, pre-diabetes, hyperlipaemia (atherosclerosis), caries and the like.
摘要翻译：本发明涉及衍生自Actinoplanaceae菌株CBS 961.70的糖酶抑制剂，包括突变体及其变体，用于产生所述糖酶抑制剂的方法，该方法包括在合适的营养液中培养Actinoplanaceae菌株CBS 961.70（包括其突变体和变体），其特征在于在最有利于生长和产生所述糖酶抑制剂的条件下淀粉，并从所述营养液的培养液中回收糖酶抑制剂，以及所述抑制剂在适用于治疗和缓解的药学上可接受的治疗组合物中的用途指示肥胖，糖尿病，前期糖尿病，高脂血症（动脉粥样硬化），龋齿等的状况。

6. 发明授权

US3995026A Amylase inhibitor 失效
标题翻译：淀粉酶抑制剂
公开(公告)号：US3995026A
公开(公告)日：1976-11-30
申请号：US482660
申请日：1974-06-24
申请人： Werner Frommer , Walter Puls , Delf Schmidt
发明人： Werner Frommer , Walter Puls , Delf Schmidt
IPC分类号： C12N9/99 , A61K38/55 , C12N9/26 , C12P1/06 , C12R1/045 , A61K35/00
CPC分类号： C12P1/06 , Y10S435/826 , Y10S435/827
摘要： The invention relates to an amylase inhibitor for glycoside-hydrolases derived from a new strain of microorganism, mutants and variants thereof, of the order Actinomycetales, means for their production comprising cultivation of the new strain of the order Actinomycetales, mutants and variants thereof, in appropriate nutrient solutions under conditions most favorable to growth and production of said amylase inhibitor and recovering an amylase inhibitor from culture broths of said nutrient solutions and said new strain of microorganism, mutants and variants thereof, of the order Actinomycetales as well as the use of said enzyme inhibitor in pharmaceutically acceptable therapeutic compositions suitable for use in the treatment and relief of conditions indicative of obesity, diabetes, pre-diabetes, gastritis, gastric and duodenal ulcers, hyperlippidemia (atheriosclerosis) 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 enzyme in the presence of a glycoside-hydrolase enzyme derived from a new strain, mutants and variants thereof, of the order Actinomycetales. The invention further contemplates the provision of method for the treatment of indications of the group consisting of obesity, adipose, hyperlippidemia (atheriosclerosis), diabetes, pre-diabetes, gastritis, gastric ulcer, duodenal ulcer and dental caries induced by the action of glycoside-hydrolase enzymes and carbohydrates which comprises employing an enzyme inhibitor for glycoside-hydrolase enzymes produced by a new strain of microorganism of the order Actinomycetales of the family Actinoplanaceae.
摘要翻译：本发明涉及一种用于衍生自放线菌纲的微生物，突变体和变体的新菌株的糖苷 - 水解酶的淀粉酶抑制剂，其生产方法包括培养放线菌纲的新菌株，其突变体和变体，在最有利于所述淀粉酶抑制剂的生长和产生的条件下，在所述营养液和所述新型放线菌纲的微生物，突变体和变体菌株的培养液中回收淀粉酶抑制剂以及使用所述淀粉酶抑制剂适合用于治疗和缓解指示肥胖症，糖尿病，前期糖尿病，胃炎，胃和十二指肠溃疡，高脂血症（动脉硬化）等）的药物学上可接受的治疗组合物中的酶抑制剂。本发明还考虑提供通过在存在下进行所述碳水化合物和糖苷 - 水解酶的所述反应来抑制碳水化合物和糖苷 - 水解酶的反应的方法，特别是消除道的碳水化合物 - 裂解糖苷 - 水解酶的衍生自放线菌纲的新菌株，其突变体和变体的糖苷 - 水解酶。本发明进一步考虑了提供治疗由糖苷类药物诱导的肥胖，脂肪，高脂血症（动脉粥样硬化），糖尿病，糖尿病前期，胃炎，胃溃疡，十二指肠溃疡和龋齿组成的组的适应症的方法，水解酶和碳水化合物，其包括使用酶抑制剂用于通过科诺诺科科放线菌放线菌的新菌株产生的糖苷 - 水解酶。

7. 发明授权

US3951745A Glycoside-hydrolase enzyme inhibitors 失效
标题翻译：糖苷 - 水解酶抑制剂
公开(公告)号：US3951745A
公开(公告)日：1976-04-20
申请号：US493464
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
摘要： This invention relates to inhibitors for glycoside-hydrolases 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：本发明涉及来源于放线菌纲的细菌的糖苷 - 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，在合适的营养溶液中培养放线菌纲的微生物，来自培养物的新产品，糖苷 - 水解酶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）等等。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。

8. 发明授权

US3937817A Pharmaceutical compositions containing a saccharase inhibitor 失效
标题翻译：含有SACCHARASE抑制剂的药物组合物
公开(公告)号：US3937817A
公开(公告)日：1976-02-10
申请号：US481224
申请日：1974-06-20
申请人： Werner Frommer , Walter Puls , Delf Schmidt
发明人： Werner Frommer , Walter Puls , Delf Schmidt
IPC分类号： A61K38/00 , C07K14/365 , C12P1/06 , A61K35/00
CPC分类号： C12P1/06 , A61K38/005 , C07K14/365 , Y10S435/827
摘要： The invention relates to a saccharase inhibitor derived from Actinoplanaceae Strain CBS 961.70, including mutants and variants thereof, means for the production of said saccharase inhibitors comprising cultivation of Actinoplanaceae Strain CBS 961.70, including mutants and variants thereof, in appropriate nutrient solutions which are characterized by being starch free under conditions most favorable to growth and production of said saccharase inhibitor and recovering a saccharase inhibitor from culture broths of said nutrient solutions, as well as the use of said inhibitor in pharmaceutically acceptable therapeutic compositions suitable for use in the treatment and relief of conditions indicative of adiposity, diabetes, pre-diabetes, hyperlipaemia (atherosclerosis), caries and the like.

9. 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。

10. 发明授权

US3950319A Amylase inhibitor from wheat gluten using alcohol 失效
标题翻译：使用酒精的燕麦淀粉酶抑制剂
公开(公告)号：US3950319A
公开(公告)日：1976-04-13
申请号：US435648
申请日：1974-01-23
申请人： Delf Schmidt , Walter Puls
发明人： Delf Schmidt , Walter Puls
IPC分类号： A61K38/00 , C07K14/415 , C07G7/00
CPC分类号： C07K14/415 , A61K38/00
摘要： An inhibitor for .alpha.-amylases, particularly pancreas amylase, is extracted from wheat, as for example, wheat flour or wheat gluten, by means of aqueous alcoholic solutions of lower alcohols of 1 to 3 carbon atoms, or dilute aqueous acid solutions having a pH of from 1 to 5, or of mixtures of the aqueous alcoholic solutions with dilute acids, and separating the desired amylase inhibitor contained in the aqueous phase from the extraction mixture by known methods. The amylase inhibitor thus obtained is particularly effective against pancreas amylase and is indicated as a therapeutic agent for the treatment of conditions resulting from alimentary hyperglycemia, such as adiposity, arteriosclerosis, diabetes and prediabetes.

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