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1. 发明授权

US4125608A Appetite curbing preparation containing an alginate and a diphosphonic acid 失效
标题翻译：含有藻酸盐和二膦酸的食欲遏制制剂
公开(公告)号：US4125608A
公开(公告)日：1978-11-14
申请号：US740531
申请日：1976-11-10
申请人： Helmut Blum , Christian Gloxhuber , Christian Heine , Karl-Heinz Worms
发明人： Helmut Blum , Christian Gloxhuber , Christian Heine , Karl-Heinz Worms
IPC分类号： A23L1/0532 , A23L1/308 , C08L5/04 , A01N9/00 , A01N9/28 , A01N9/36
CPC分类号： A61K31/715 , A23L29/256 , A23L33/21 , C08L5/04
摘要： An appetite curbing preparation comprising an alginate and diphosphonic acid or a nontoxic pharmacologically acceptable water-soluble salt thereof as an inhibitor of the precipitation of calcium salts. This preparation is useful for curbing the appetite of a warm-blooded animal.
摘要翻译：包含藻酸盐和二膦酸的食欲抑制制剂或其无毒的药理学上可接受的水溶性盐作为钙盐沉淀的抑制剂。这种制剂可用于抑制温血动物的食欲。

2. 发明授权

US3962433A Method of treatment of calcium disorders using phosphonoalkane-polycarboxylic acids 失效
标题翻译：使用膦酰基烷烃多元羧酸治疗钙障碍的方法
公开(公告)号：US3962433A
公开(公告)日：1976-06-08
申请号：US529040
申请日：1974-12-03
申请人： Karl-Heinz Worms , Christian Gloxhuber , Manfred Schmidt-Dunker , Helmut Blum
发明人： Karl-Heinz Worms , Christian Gloxhuber , Manfred Schmidt-Dunker , Helmut Blum
IPC分类号： A61K31/66 , C07F9/38
CPC分类号： C07F9/3869 , A61K31/66 , C07F9/3808
摘要： A method for the treatment of diseases relating to the abnormal deposition or dissolution of difficutly soluble calcium salts in the body of warm-blooded animals which consists of administering orally, parenterally or topically to said warm-blooded animals, a safe but effective amount of at least one pharmacologically acceptable phosphonoalkane-polycarboxylic acid and water-soluble salts thereof.
摘要翻译：一种治疗与难以溶解的钙盐异常沉积或溶解在温血动物身体中的疾病的方法，其包括向所述温血动物口服，肠胃外或局部施用，安全但有效量的至少一种药学上可接受的膦酰基烷烃 - 多元羧酸及其水溶性盐。

3. 发明授权

US4069246A Production of 1-hydroxy-alkane-1,1-diphosphonic acids 失效
标题翻译： 1-羟基 - 烷烃-1,1-二膦酸的制备
公开(公告)号：US4069246A
公开(公告)日：1978-01-17
申请号：US692326
申请日：1976-06-03
申请人： Helmut Blum , Karl-Heinz Worms
发明人： Helmut Blum , Karl-Heinz Worms
IPC分类号： C07F9/38
CPC分类号： C07F9/386
摘要： A process for the production of 1-hydroxy-alkane-1,1-diphosphonic acids comprises reacting 1-amino-alkane-1,1-diphosphonic acids with nitrous acid, halides of nitrous acid or a substance forming nitrous acid under the reaction conditions.
摘要翻译： 1-羟基 - 烷烃-1,1-二膦酸的制备方法包括在反应条件下使1-氨基 - 烷烃-1,1-二膦酸与亚硝酸，亚硝酸的卤化物或形成亚硝酸的物质反应。

4. 发明授权

US4054598A 1-Hydroxy-3-amino-alkane-1,1-diphosphonic acids and salts 失效
标题翻译： 1-羟基-3-氨基 - 烷烃-1,1-二膦酸及其盐
公开(公告)号：US4054598A
公开(公告)日：1977-10-18
申请号：US705792
申请日：1976-07-16
申请人： Helmut Blum , Karl-Heinz Worms
发明人： Helmut Blum , Karl-Heinz Worms
IPC分类号： C09K3/00 , A61K8/55 , A61K51/00 , A61P3/00 , A61P3/14 , A61Q11/00 , C02F5/14 , C07F9/38 , C07F9/40 , C11D3/36 , C23F11/167
CPC分类号： A61K8/55 , A61Q11/00 , C02F5/14 , C07F9/3873 , C11D3/364 , C23F11/1676
摘要： 1-Hydroxy-3-amino-alkane-1,1-diphosphonic acids having the formula ##STR1## wherein X is a member selected from the group consisting of ##STR2## and ##STR3## wherein R.sub.1 is a member selected from the group consisting of hydrogen and alkyl having 1 to 3 carbon atoms and R.sub.2 is alkyl having 1 to 3 carbon atoms; as well as their water-soluble salts. The 1-hydroxy-3-amino-alkane-1,1-diphosphonic acids are excellent sequestering agents especially for alkaline earth metal ions. The compounds are useful in pharmaceutical preparations for treatment of disturbances of calcium or phosphate metabolism or cosmetic preparations such as toothpastes or mouthwashes for the prevention of tartar and plaque depositions.
摘要翻译：具有式“IMAGE”的1-羟基-3-氨基 - 烷烃-1,1-二膦酸，其中X是选自下组的成员：其中R1是选自下组的成员：的氢和具有1至3个碳原子的烷基，R 2是具有1至3个碳原子的烷基; 以及它们的水溶性盐。 1-羟基-3-氨基 - 烷烃-1,1-二膦酸是特别用于碱土金属离子的优异的螯合剂。该化合物可用于治疗钙或磷酸盐代谢紊乱的药物制剂或用于预防牙垢和斑块沉积的牙膏或漱口剂的化妆品制剂。

5. 发明授权

US4077997A Diphosphonoalkane carboxylic acids, process of preparation and methods of use 失效
标题翻译：二膦酰基烷烃羧酸，其制备方法和使用方法
公开(公告)号：US4077997A
公开(公告)日：1978-03-07
申请号：US761271
申请日：1977-01-21
申请人： Helmut Blum , Karl-Heinz Worms
发明人： Helmut Blum , Karl-Heinz Worms
IPC分类号： C09K3/00 , A61K8/00 , A61K8/55 , A61K8/58 , A61K31/66 , A61P3/00 , A61Q11/00 , C07F9/38 , C07F9/40 , C11D3/36 , C23G1/00 , C23G3/00 , A61K7/16 , A61K31/185
CPC分类号： A61K31/66 , A61K8/55 , A61Q11/00 , C07F9/3839 , C11D3/365 , Y10S514/825 , Y10S71/02
摘要： Diphosphonoalkane carboxylic acids having the formula ##STR1## wherein R is H or --CH.sub.2 --CH.sub.2 --COOH; as well as their water-soluble salts. The compounds are excellent sequestering agents, especially for alkaline earth and earth metal ions. They are stabilizers for percompounds and are useful in the delaying of the setting times for gypsum. In addition, the compounds are useful in cosmetic preparations, such as toothpastes and mouthwashes where they prevent formation of tartar and plaque and are useful in therapy in the treatment of diseases related to the abnormal deposition or dissolution of difficultly soluble calcium salts in the animal body.
摘要翻译：具有式“IMAGE”的二膦酰基烷烃羧酸，其中R是H或-CH 2 -CH 2 -COOH; 以及它们的水溶性盐。这些化合物是优异的螯合剂，特别是对于碱土金属和地球金属离子。它们是化合物的稳定剂，对于延迟石膏凝固时间是有用的。此外，这些化合物可用于化妆品制剂，例如牙膏和漱口剂，其中它们防止形成牙垢和斑块，并且可用于治疗与难溶性钙盐在动物体内的异常沉积或溶解有关的疾病的治疗。

6. 发明授权

US4120890A Diphosphonoalkane carboxylic acids, process of preparation and methods of use 失效
公开(公告)号：US4120890A
公开(公告)日：1978-10-17
申请号：US833143
申请日：1977-09-14
申请人： Helmut Blum , Karl-Heinz Worms
发明人： Helmut Blum , Karl-Heinz Worms
IPC分类号： A61K8/55 , A61K31/66 , A61Q11/00 , C07F9/38 , C11D3/36 , A61K7/16
CPC分类号： A61K31/66 , A61K8/55 , A61Q11/00 , C07F9/3839 , C11D3/365
摘要： Diphosphonoalkane carboxylic acids having the formula ##STR1## wherein R is H or --CH.sub.2 --CH.sub.2 --COOH; as well as their water-soluble salts. The compounds are excellent sequestering agents, especially for alkaline earth and earth metal ions. They are stabilizers for percompounds and are useful in the delaying of the setting times for gypsum. In addition, the compounds are useful in cosmetic preparations, such as toothpastes and mouthwashes where they prevent formation of tartar and plaque and are useful in therapy in the treatment of diseases related to the abnormal deposition or dissolution of difficultly soluble calcium salts in the animal body.

7. 发明授权

US3965024A Washing agent compositions and washing assistant composition containing phosphonopolycarboxylate sequestering agents 失效
标题翻译：洗涤剂组合物和含有膦多羧酸盐螯合剂的洗涤助剂组合物
公开(公告)号：US3965024A
公开(公告)日：1976-06-22
申请号：US417891
申请日：1973-11-21
申请人： Edmund Schmadel , Gunter Jakobi , Karl-Heinz Worms , Helmut Blum
发明人： Edmund Schmadel , Gunter Jakobi , Karl-Heinz Worms , Helmut Blum
IPC分类号： C07F9/38 , C07F9/40 , C11D3/00 , C11D3/36 , C11D3/395
CPC分类号： C11D3/365
摘要： Washing agent compositions and washing assistant compositions containing from 0.5% to 70% by weight of a phosphonopolycarboxylate having the formula ##EQU1## WHEREIN Me is H, alkali metal, or H.NR.sub.3, R.sub.1 is H or CH.sub.3, R.sub.2 is H, alkyl having 1 to 4 carbon atoms or --CH.sub.2 --CHR--COOMe, R.sub.3 is H, alkyl or alkylol having 1 to 6 carbon atoms, and X is a direct bond or the groups ##EQU2## from 0 to 96.5% of other sequestering and non-sequestering, preferably phosphorus-free builders, and from 3% to 45% by weight of at least one surface-active compound of an anionic or non-ionic nature, whereby a 1% aqueous solution thereof has a pH of between 6 and 11.5. Preferably said phosphonopolycarboxylate sequestering agents are present as water-soluble salts capable of complex formation with alkaline earth metal ions. The invention also resides in the process of sequestering alkaline earth metal ions using aqueous solutions of the washing agent composition.
摘要翻译：洗涤剂组合物和洗涤助剂组合物，其含有0.5重量％至70重量％的具有式COOMeCOOMe O || PARALLEL CH --- C-X-P-OMe || R1R2OMe的膦酸多羧酸酯，其中Me为H，碱金属或H.NR 3，R 1为H或CH 3，R 2为H，具有1至4个碳原子的烷基或-CH 2 -CHR-COOMe，R 3为H，具有1至6个碳原子的烷基或烷醇，X为直接键或基团COOMe COOMe OMe | | | -C-CH2-，-C-或O = P-OMe，| | | H R1 -C- | R1从0到96.5％的其他螯合和非螯合，优选无磷助洗剂，和3重量％至45重量％的至少一种阴离子或非离子性表面活性化合物，其中1％的水溶液的pH为6至11.5。优选地，所述膦酸多羧酸盐螯合剂作为能够与碱土金属离子复合形成的水溶性盐存在。本发明还在于使用洗涤剂组合物的水溶液螯合碱土金属离子的过程。

8. 发明授权

US4407761A Process for the production of .omega.-amino-1-hydroxyalkylidene-1,1-bisphosphonic acid 失效
标题翻译：生产ω-氨基-1-羟基亚烷基-1,1-二膦酸的方法
公开(公告)号：US4407761A
公开(公告)日：1983-10-04
申请号：US254918
申请日：1981-04-16
申请人： Helmut Blum , Karl-Heinz Worms
发明人： Helmut Blum , Karl-Heinz Worms
IPC分类号： C02F1/68 , C02F5/14 , C07F9/38 , C07F9/40
CPC分类号： C07F9/3873 , C02F1/683 , C02F5/14
摘要： A process for the preparation of a .omega.-amino-1-hydroxyalkylidine-1,1-biphosphonic acid of the formula ##STR1## wherein n is an integer from 3 to 5, consisting essentially of the steps ofreacting an aminocarboxylic acid of the formulaNH.sub.2 --CH.sub.2 --(CH.sub.2).sub.m --COOHwherein m is an integer from 2 to 4, with a phosphonating reactant selected from the group consisting of(a) a mixture of phosphorous acid and PCl.sub.3,(b) a mixture of phosphorous acid and PCl.sub.5, and(c) a mixture of phosphorous acid and POCl.sub.3,hydrolyzing the reaction mixture with a strong acid which does not oxidize aminophosphonic acids, and recovering said .omega.-amino-1-hydroxyalkylidene-1,1-bisphosphonic acid.
摘要翻译：一种制备式IMAGE的ω-氨基-1-羟基烷基-1,1-二膦酸的方法，其中n为3至5的整数，其基本上由以下步骤组成：使下式的氨基羧酸 NH 2 -CH 2 - （CH 2）m -COOH，其中m是2至4的整数，膦酸化反应物选自（a）亚磷酸和PCl 3的混合物，（b）亚磷酸和 PCl5和（c）亚磷酸和POCl 3的混合物，用不氧化氨基膦酸的强酸水解反应混合物，并回收所述ω-氨基-1-羟基亚烷基-1,1-二膦酸。

9. 发明授权

US4327039A Process for the production of 3-amino-1-hydroxypropane-1,1-diphosphonic acid 失效
标题翻译： 3-氨基-1-羟基丙烷-1,1-二膦酸的制备方法
公开(公告)号：US4327039A
公开(公告)日：1982-04-27
申请号：US192733
申请日：1980-10-01
申请人： Helmut Blum , Karl-Heinz Worms
发明人： Helmut Blum , Karl-Heinz Worms
IPC分类号： C07F9/38 , C07F9/40
CPC分类号： C07F9/3873
摘要： A process for the preparation of 3-amino-1-hydroxypropane-1,1-diphosphonic acid having the formula: ##STR1## wherein R.sub.1 and R.sub.2 are selected from the group consisting of hydrogen and lower alkyl, consisting essentially of the steps of reacting a .beta.-alanine compound selected from the group consisting of .beta.-alanine and lower alkylated .beta.-alanine with a phosphonating reactant selected from the group consisting of:(1) a mixture of phosphorous acid and PCl.sub.5, and(2) a mixture of phosphorous acid, PCl.sub.3 and Cl.sub.2,hydrolyzing the reaction mixture, and recovering said 3-amino-1-hydroxypropane-1,1-diphosphonic acid.
摘要翻译：制备具有下式的3-氨基-1-羟基丙烷-1,1-二膦酸的方法：其中R 1和R 2选自氢和低级烷基，其基本上由以下步骤组成：使选自β-丙氨酸和低级烷基化β-丙氨酸的β-丙氨酸化合物，其中膦酸化反应物选自：（1）亚磷酸和PCl5的混合物，和（2）磷的混合物酸，PCl 3和Cl 2，水解反应混合物，并回收所述3-氨基-1-羟基丙烷-1,1-二膦酸。

10. 发明授权

US4267108A Hydroxyalkane diphosphonic acids 失效
标题翻译：羟基烷基二膦酸
公开(公告)号：US4267108A
公开(公告)日：1981-05-12
申请号：US944603
申请日：1978-09-21
申请人： Helmut Blum , Hans-Ulrich Hempel , Karl-Heinz Worms
发明人： Helmut Blum , Hans-Ulrich Hempel , Karl-Heinz Worms
IPC分类号： A61K8/55 , A61K31/66 , A61K31/675 , A61K51/00 , A61P3/00 , A61P9/10 , A61Q11/00 , C02F5/00 , C02F5/08 , C02F5/10 , C02F5/12 , C02F5/14 , C07F9/38 , C07F9/40 , C07F9/572 , C11D3/36 , C07D207/12 , C07F9/02
CPC分类号： A61K8/55 , A61Q11/00 , C02F5/14 , C07F9/3873 , C07F9/5722 , C11D3/361 , A61K2800/51
摘要： Hydroxyalkane diphosphonic acids having the formula ##STR1## wherein X is a member selected from the group consisting of ##STR2## and their water-soluble salts; as well as the process of preparing the same.The compounds are excellent sequestering agents, especially for alkaline earth and earth metal ions. They are stabilizers for percompounds and are useful in the delaying of the setting times for gypsum. In addition, the compounds are useful in cosmetic preparations, such as toothpastes and mouthwashes where they prevent formation of tartar and plaque and are useful in therapy in the treatment of diseases related to the abnormal deposition or dissolution of difficultly soluble calcium salts in the animal body.
摘要翻译：具有式“IMAGE”的羟基烷基二膦酸，其中X是选自由它们的水溶性盐组成的组的成员; 以及准备相同的过程。这些化合物是优异的螯合剂，特别是对于碱土金属和地球金属离子。它们是化合物的稳定剂，对于延迟石膏凝固时间是有用的。此外，这些化合物可用于化妆品制剂，例如牙膏和漱口剂，其中它们防止形成牙垢和斑块，并且可用于治疗与难溶性钙盐在动物体内的异常沉积或溶解相关的疾病的治疗。

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