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71. 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。

72. 发明授权

US07063952B2 Masking background flourescence and luminescence in optical analysis of biomedical assays 有权
公开(公告)号：US07063952B2
公开(公告)日：2006-06-20
申请号：US09966137
申请日：2001-09-28
申请人： Thoams Krahn , Wolfgang Paffhausen , Andreas Schade , Martin Bechem , Delf Schmidt
发明人： Thoams Krahn , Wolfgang Paffhausen , Andreas Schade , Martin Bechem , Delf Schmidt
IPC分类号： G01N33/567
CPC分类号： G01N33/542 , G01N33/5005 , G01N33/5306 , G01N33/54393 , Y10S436/80 , Y10S436/805 , Y10S436/823 , Y10T436/13
摘要： In a process for the quantitative optical analysis of fluorescently labelled biological cells 5, a cell layer on a transparent support at the bottom 2 of a reaction vessel 1 is in contact with a solution 3 containing the fluorescent dye 4. The sensitivity of analytical detection can be considerably improved if to the fluorescent dye 4 already present in addition a masking dye 9, which absorbs the excitation light 6 for the fluorescent dye 4 and/or its emission light 7, is added to the solution 3 and/or if a separating layer 10 permeable to the solution and absorbing and/or reflecting the excitation light 6 or the emission light 7 is applied to the cell layer at the bottom 2. This process can also be used for improving the sensitivity in the quantitative optical analysis of a luminescent biological cell layer. The separating layer 10 must in this case be composed such that it has a high power of reflection for the luminescent light 11. Analogously, these process principles can also be used in receptor studies for the masking of the interfering background radiation in the quantitative optical analysis of fluorescently or luminescently labelled reaction components. In this case, a receptor layer 12 at the bottom 2 of a reaction vessel 1 is in contact with a solution (supernatant 3) in which a fluorescent or luminescent ligand 13 is dissolved. The sensitivity and accuracy of the analytical detection can be considerably improved here if a masking dye 9 which absorbs the excitation light 6 for the fluorescent dye and/or its emission light or (in the case of luminescent ligands) the luminescent light is added to the supernatant 3. Instead of the masking dye in the solution 3 or optionally as an additional measure, a separating layer 10 permeable to the solution 3 and absorbing and/or reflecting the excitation light 6 and/or the emission light or the luminescent light can be applied to the cell or receptor layer 12 at the bottom 2.

73. 发明申请

US20060004015A1 Substituted 2-phenyl-3(2h)-pyridazinones 失效
标题翻译：取代的2-苯基-3（2h） - 哒嗪酮
公开(公告)号：US20060004015A1
公开(公告)日：2006-01-05
申请号：US10511225
申请日：2003-04-08
申请人： Rudolf Schohe-Loop , Elmar Burchardt , Christiane Faeste , Claudia Hirth-Dietrich , Jorg Keldenich , Andreas Knorr , Thomas Lampe , Paul Naab , Delf Schmidt
发明人： Rudolf Schohe-Loop , Elmar Burchardt , Christiane Faeste , Claudia Hirth-Dietrich , Jorg Keldenich , Andreas Knorr , Thomas Lampe , Paul Naab , Delf Schmidt
IPC分类号： A61K31/501 , C07D43/02
CPC分类号： C07D231/12 , C07D233/56 , C07D237/22 , C07D249/08 , C07D401/04 , C07D401/12
摘要： The invention relates to substituted 2-phenyl-3(2h)-pyridazinones, to a method for the production thereof, and to their use as medicaments used in the prophylaxis and/or treatment of diseases in humans and/or animals.
摘要翻译：本发明涉及取代的2-苯基-3（2h） - 哒嗪酮，其制备方法及其用作预防和/或治疗人和/或动物疾病的药物。

74. 发明授权

US06589972B2 &bgr;-phenylalanine derivatives as integrin antagonists 失效
标题翻译： β-苯丙氨酸衍生物作为整联蛋白拮抗剂
公开(公告)号：US06589972B2
公开(公告)日：2003-07-08
申请号：US09867835
申请日：2001-05-30
申请人： Andreas Schoop , Gerhard Mueller , Ulf Brueggemeier , Delf Schmidt , Beatrix Stelte-Ludwig , Joerg Keldenich
发明人： Andreas Schoop , Gerhard Mueller , Ulf Brueggemeier , Delf Schmidt , Beatrix Stelte-Ludwig , Joerg Keldenich
IPC分类号： A01N4350
CPC分类号： C07C311/19 , C07C311/47
摘要： The present invention relates to compounds of the general formula (1) wherein R4 is —SO2R4′, —COOR4″, —COR4′, —CONR4′2 or —CSNR4′2; R4′ is hydrogen, a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; R4″ is a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; L is a sulphonamide, amide, ether, ester, keto, urea, thioether, sulphoxide or sulphone unit optionally extended by one or two methylene groups; and X is N, O or S; and their physiologically acceptable salts and stereoisomers. The present invention furthermore relates to a process for the preparation of the compounds of the formula (1), a pharmaceutical composition containing at least one of these compounds, and the use of compounds of the formula (1) for the production of a pharmaceutical composition having integrin-antagonistic action and in particular for the therapy and prophylaxis of cancer, osteolytic diseases such as osteoporosis, arteriosclerosis, restenosis and ophthalmic disorders.
摘要翻译：本发明涉及通式（1）的化合物，其中R 4是-SO 2 R 4'，-COOR 4“，-COR 4'， - CONR 4'2或-CSNR 4'2; R 4'是氢，取代或未取代的烷基或环烷基残基，取代或未取代的芳基残基或饱和或不饱和的任选取代的杂环残基; R 4“是取代或未取代的烷基或环烷基残基，取代或未取代的芳基残基或饱和或不饱和的任选取代的杂环残基; L是任选被一个或两个亚甲基延伸的磺酰胺，酰胺，醚，酯，酮，脲，硫醚，亚砜或砜单元; X为N，O或S; 及其生理上可接受的盐和立体异构体。本发明还涉及制备式（1）化合物的方法，含有这些化合物中的至少一种的药物组合物，以及式（1）化合物在制备药物组合物中的用途具有整合素拮抗作用，特别是用于治疗和预防癌症，溶骨性疾病如骨质疏松症，动脉硬化，再狭窄和眼科疾病。

75. 发明授权

US06339083B1 Multiheterocyclic pharmAceuticals 失效
标题翻译：多杂环药物治疗
公开(公告)号：US06339083B1
公开(公告)日：2002-01-15
申请号：US09211274
申请日：1998-12-14
申请人： Klaus Urbahns , Delf Schmidt , Ulf Brueggemeier , Christoph Gerdes , Beatrix Stelte-Ludwig , Jörg Keldenich , Elke Stahl
发明人： Klaus Urbahns , Delf Schmidt , Ulf Brueggemeier , Christoph Gerdes , Beatrix Stelte-Ludwig , Jörg Keldenich , Elke Stahl
IPC分类号： A61K315513
CPC分类号： C07D413/14 , C07D417/14
摘要： The present invention relates to compounds of the general formula (I): and their preparation and use for the production of pharmaceuticals, and pharmaceuticals comprising these compounds.
摘要翻译：本发明涉及通式（I）的化合物及其药物制备和用途以及包含这些化合物的药物。

76. 发明授权

US06291503B1 &bgr;-phenylalanine derivatives as integrin antagonists 失效
标题翻译： β-苯丙氨酸衍生物作为整联蛋白拮抗剂
公开(公告)号：US06291503B1
公开(公告)日：2001-09-18
申请号：US09232738
申请日：1999-01-15
申请人： Andreas Schoop , Gerhard Mueller , Ulf Brueggemeier , Delf Schmidt , Beatrix Stelte-Ludwig , Joerg Keldenich
发明人： Andreas Schoop , Gerhard Mueller , Ulf Brueggemeier , Delf Schmidt , Beatrix Stelte-Ludwig , Joerg Keldenich
IPC分类号： A01N4356
CPC分类号： C07C311/19 , C07C311/47
摘要： The present invention relates to compounds of the general formula (1) wherein R4 is —SO2R4, —COOR4′, —COR4′, —CONR4′2 or —CSNR4′2; R4′ is hydrogen, a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; R4″ is a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; L is a sulphonamide, amide, ether, ester, keto, urea, thioether, sulphoxide or sulphone unit optionally extended by one or two methylene groups; and X is N, O or S; and their physiologically acceptable salts and stereoisomers. The present invention furthermore relates to a process for the preparation of the compounds of the formula (1), a pharmaceutical composition containing at least one of these compounds, and the use of compounds of the formula (1) for the production of a pharmaceutical composition having integrin-antagonistic action and in particular for the therapy and prophylaxis of cancer, osteolytic diseases such as osteoporosis, arteriosclerosis, restenosis and ophthalmic disorders.
摘要翻译：本发明涉及通式（1）的化合物，其中R4是-SO2R4，-COOR4'，-COR4'，-CONR4'2或-CSNR4'2; R 4'是氢，取代或未取代的烷基或环烷基残基，取代或未取代的芳基残基或饱和或不饱和的任选取代的杂环残基; R 4“是取代或未取代的烷基或环烷基残基，取代或未取代的芳基残基或饱和或不饱和的任选取代的杂环残基; L是任选被一个或两个亚甲基延伸的磺酰胺，酰胺，醚，酯，酮，脲，硫醚，亚砜或砜单元; X为N，O或S; 及其生理上可接受的盐和立体异构体。本发明还涉及制备式（1）化合物的方法，含有这些化合物中的至少一种的药物组合物，以及式（1）化合物在制备药物组合物中的用途具有整合素拮抗作用，特别是用于治疗和预防癌症，溶骨性疾病如骨质疏松症，动脉硬化，再狭窄和眼科疾病。

77. 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。

78. 发明授权

US4273571A Organic chemical compound, microbiological process for its preparation, and its use as a herbicide 失效
标题翻译：有机化合物，其制备的微生物过程及其作为除草剂的用途
公开(公告)号：US4273571A
公开(公告)日：1981-06-16
申请号：US967930
申请日：1978-12-08
申请人： Dieter Berg , Werner Frommer , Delf Schmidt , Robert R. Schmidt , Dietmar Schafer
发明人： Dieter Berg , Werner Frommer , Delf Schmidt , Robert R. Schmidt , Dietmar Schafer
IPC分类号： C12P13/00 , A01N63/02 , C12P1/00 , C12P1/06 , A01N63/04
CPC分类号： C12P1/00 , A01N63/02 , C12P1/06 , Y10S435/822 , Y10S435/827
摘要： A herbicidally active compound of the empirical formula C.sub.10 H.sub.14 N.sub.6 O.sub.3, exhibiting substantially the IR KBr-absorption spectrum shown in FIG. 2, is produced by aerobic culturing of a micro-organism of the family of the Actinoplanaceae under aerobic conditions in a nutrient medium which contains an assimilable carbon source, at least one assimilable nitrogen source and mineral salts, at a pH of 6 to 8 and a temperature of 20.degree. to 40.degree. C.
摘要翻译：经验式C10H14N6O3的除草活性化合物，基本上表现出图1所示的IR KBr吸收光谱。 2是通过在有氧条件下在含有可同化碳源的营养培养基，至少一种可同化的氮源和矿物盐，pH6至8的有氧培养下，通过需氧培养Actinoplanaceae的微生物，温度为20°C至40°C

79. 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.

80. 发明授权

US07094911B2 Biphenyl and biphenyl-analogous compounds as integrin antagonists 失效
标题翻译：联苯和联苯类似物作为整联蛋白拮抗剂
公开(公告)号：US07094911B2
公开(公告)日：2006-08-22
申请号：US10285073
申请日：2002-10-31
申请人： Markus Albers , Klaus Urbahns , Andrea Vaupel , Michael Härter , Delf Schmidt , Beatrix Stelte-Ludwig , Christoph Gerdes , Elke Stahl , Jörg Keldenich , Ulf Brueggemeier , Klemens Lustig
发明人： Markus Albers , Klaus Urbahns , Andrea Vaupel , Michael Härter , Delf Schmidt , Beatrix Stelte-Ludwig , Christoph Gerdes , Elke Stahl , Jörg Keldenich , Ulf Brueggemeier , Klemens Lustig
IPC分类号： C07D333/24 , C07D333/36 , C07D409/06 , A61K31/38 , A61P19/10
CPC分类号： C07D213/40 , C07C237/36 , C07C271/22 , C07C275/42 , C07C311/06 , C07C311/09 , C07C311/10 , C07C311/11 , C07C311/13 , C07C311/19 , C07C311/29 , C07C311/43 , C07C311/47 , C07C317/14 , C07C323/44 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/42 , C07D207/34 , C07D213/38 , C07D213/55 , C07D213/74 , C07D213/75 , C07D213/82 , C07D231/18 , C07D233/64 , C07D233/84 , C07D233/88 , C07D233/90 , C07D235/30 , C07D235/32 , C07D261/10 , C07D263/58 , C07D277/42 , C07D277/54 , C07D277/82 , C07D285/10 , C07D285/135 , C07D285/14 , C07D295/096 , C07D295/13 , C07D295/15 , C07D295/215 , C07D307/52 , C07D333/34 , C07D333/48 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases. The compounds according to the invention have the formula (1) wherein R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.
摘要翻译：本发明涉及联苯和联苯类似物，其作为药物组合物的制备和用途，作为整联蛋白拮抗剂，特别涉及用于治疗和预防癌症，动脉硬化，再狭窄，溶骨性疾病如骨质疏松和眼科疾病根据本发明的化合物具有式（1）其中R 1，R 2，U，V，A，B，W，R 3， SUP，C和R 4具有如权利要求中所定义的含义。

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