公开(公告)号：WO2011151285A1

公开(公告)日：2011-12-08

申请号：PCT/EP2011/058827

申请日：2011-05-30

申请人： Universitaetsklinikum Muenster ,  PREHM, Peter ,  STRACKE, Dennis

发明人： PREHM, Peter ,  STRACKE, Dennis

IPC分类号： A61K31/353 ,  A61P19/02

CPC分类号： C07D311/32 ,  A23L2/52 ,  A23L33/105 ,  A23V2002/00 ,  A61K31/353 ,  C07C49/84 ,  C07D311/60 ,  C07D311/74

摘要： The present invention relates to new compounds which are inter alia derivable from hops for use in the treatment of (for treating)/prevention or healing of a disease which is associated with an excess transport of hyaluronan across a lipid bilayer, in particular a disease which is associated with or characterized by degeneration and/or a destruction of cartilage (and/or for the prevention of aggrecan loss). Food products comprising these compounds for use in the treatment (for treating) a disease which is associated with an excess transport of hyaluronan across a lipid bilayer, in particular a disease which is associated with or characterized by degeneration and/or a destruction of cartilage, are also envisaged.

摘要翻译： 本发明涉及新化合物，其特别是衍生自啤酒花，用于治疗（用于治疗）/预防或愈合与透明质酸通过脂质双层的过度运输相关的疾病，特别是其中 与软骨变性和/或破坏有关（或/或用于预防聚集蛋白聚糖损失）。 包含这些化合物的食品，用于治疗（用于治疗）透明质酸过量运输通过脂质双层的疾病，特别是与软骨变性和/或破坏有关或特征在于的疾病， 也是设想的。

公开(公告)号：WO2010066909A3

公开(公告)日：2010-08-05

申请号：PCT/EP2009067113

申请日：2009-12-14

申请人： UNIVERSITAETSKLINIKUM MUENSTER ,  PREHM PETER

发明人： PREHM PETER

IPC分类号： C07C233/75 ,  A61K31/10 ,  A61K31/16 ,  A61K31/167 ,  A61K31/351 ,  A61P11/00 ,  C07C259/10 ,  C07C309/39 ,  C07D309/10 ,  C07H15/203

CPC分类号： C07C233/25 ,  C07C259/10 ,  C07C309/42 ,  C07D309/10

摘要： The present invention relates in general to a compound which is characterized by a formula selected from the following formulas A, B, C, D, E or F; or a pharmaceutically acceptable salt thereof. The present invention further relates to pharmaceutical composition comprising the inhibitor(s) of the invention and to their use in the treatment of (for treating) a disease which is associated with an excess transport of hyaluronan across a lipid bilayer. The present invention furthermore relates to the use of at least one inhibitor of the invention for the preparation of a pharmaceutical composition for the treatment of (for treating) a disease which is associated with an excess transport of hyaluronan across a lipid bilayer. The present invention also relates to a method for manufacturing a pharmaceutical composition comprising the steps of formulating the inhibitor defined herein in a pharmaceutically acceptable form.

摘要翻译： 本发明一般涉及以下式A，B，C，D，E或F所示的化合物为特征的化合物， 或其药学上可接受的盐。 本发明还涉及包含本发明抑制剂的药物组合物及其在治疗（用于治疗）与透明质酸过量运输通过脂质双层相关的疾病的用途。 本发明还涉及本发明的至少一种抑制剂用于制备用于治疗（用于治疗）与通过脂质双层的透明质酸的过量转运相关的疾病的药物组合物的用途。 本发明还涉及制备药物组合物的方法，其包括以药学上可接受的形式配制本文定义的抑制剂的步骤。

公开(公告)号：WO2005013947A3

公开(公告)日：2005-04-07

申请号：PCT/EP2004008547

申请日：2004-07-29

申请人： UNIVERSITAETSKLINIKUM MUENSTER ,  PREHM PETER

发明人： PREHM PETER

IPC分类号： A61K31/00 ,  A61K31/185 ,  A61K31/277 ,  A61K31/343 ,  A61K31/4422 ,  A61K31/47 ,  A61K31/64 ,  A61P19/02 ,  G01N33/68 ,  A61K38/13 ,  G01N33/50

CPC分类号： A61K31/64 ,  A61K31/00 ,  A61K31/185 ,  A61K31/277 ,  A61K31/343 ,  A61K31/4422 ,  A61K31/47 ,  G01N33/6872 ,  G01N2333/705 ,  G01N2500/10

摘要： The present invention relates to the use of at least one inhibitor of at least one ABC-­transporter capable of transporting hyaluronan across a lipid bilayer, such as verapamil or valspodar, for the preparation of a pharmaceutical composition for the treatment of a disease which is associated with an excess transport of hyaluronan across a lipid bilayer, e.g. arthritis. Furthermore, the present invention relates to a method for screening a compound which is suitable for the treatment of a disease which is associated with an excess transport of hyaluronan across a lipid bilayer, e.g. arthritis. The present invention also relates to a method for screening a compound which reduces the transport of hyaluronan mediated by (an) ABC-transporter(s). Furthermore, the present invention relates to a method for identifying a subject at risk for a disease which is associated with an excess transport of hyaluronan across a lipid bilayer, e.g. arthritis as well as to a method of screening for a compound which is suitable for the treatment of a disease which is associated with an excess transport of hyaluronan across a lipid bilayer, e.g. arthritis in a subject. In addition, the present invention relates to a method of preventing, ameliorating and/or treating the symptoms of a disease which is associated with an excess transport of hyaluronan across a lipid bilayer, e.g. arthritis in a subject.

摘要翻译： 本发明涉及至少一种能够运输透明质酸穿过脂质双层（如维拉帕米或valspodar）运输透明质酸的至少一种ABC转运蛋白的抑制剂在制备用于治疗相关疾病的药物组合物中的用途 透明质酸穿过脂质双层的过量运输，例如 关节炎。 此外，本发明涉及一种筛选适合于治疗与透明质酸穿过脂质双层的过量转运有关的疾病的化合物的方法，例如， 关节炎。 本发明还涉及一种用于筛选减少由（a）ABC-转运蛋白介导的透明质酸的转运的化合物的方法。 此外，本发明涉及用于鉴定与透明质酸穿过脂质双层的过量运输相关的疾病的风险的受试者的方法，例如， 关节炎以及筛选适合于治疗与透明质酸通过脂质双层的过量转运相关的疾病的化合物的方法，例如， 关节炎在一个科目。 此外，本发明涉及一种预防，改善和/或治疗与透明质酸穿过脂质双层的过量转运相关的疾病症状的方法，例如， 关节炎在一个科目。

公开(公告)号：WO2010066912A4

公开(公告)日：2010-10-14

申请号：PCT/EP2009067124

申请日：2009-12-14

申请人： UNIVERSITAETSKLINIKUM MUENSTER ,  PREHM PETER

发明人： PREHM PETER

IPC分类号： C07C233/75 ,  A61K31/167 ,  A61P11/00

CPC分类号： C07C233/81 ,  C07C233/25 ,  C07H15/203

摘要： The present invention relates to a compound which is characterized by the formula (I) or a pharmaceutically acceptable salt, solvate, hydrate thereof, wherein the ring systems A and B are independently selected from a monosaccharide, aryl (preferably phenyl), a heteroaryl or cycloalkyl (preferably cyclohexan), preferably with all substituents in equatorial configurations; R1 is independently selected from alkyl (preferably C1 to C6), a substituted or unsubstituted phenyl, preferably CH3; R2 is H, alkyl (preferably C1 to C6), a carbohydrate in a glycosidic ß-linkage, preferably H; R3, R4, R5, and R6 are independently selected from H, (OH) hydroxy, alkyl preferably C1 to C6, alkoxy (preferably C1 to C6), amino, alkylamino (preferably C1 to C6), halogen, benzylamino, or benzoylamino; X is O, NH, alkylamino (NR), CO, S; and Y is O, NH, alkylamino (NR), CO, S. The present invention also relates to the compound of the invention and, optionally, a pharmaceutically acceptable carrier, for use in the treatment of (for treating) and/or preventing a disease or medical condition which is associated with mutant CFTR.

摘要翻译： 本发明涉及以式（I）表示的化合物或其药学上可接受的盐，溶剂合物，水合物，其中环系统A和B独立地选自单糖，芳基（优选苯基），杂芳基或 环烷基（优选环己烷），优选具有赤道结构中的全部取代基; R 1独立地选自烷基（优选C 1至C 6），取代或未取代的苯基，优选CH 3; R2是H，烷基（优选C1至C6），糖苷键中的碳水化合物，优选H; R3，R4，R5和R6独立地选自H，（OH）羟基，优选C1至C6烷基，烷氧基（优选C1至C6），氨基，烷基氨基（优选C1至C6），卤素，苄基氨基或苯甲酰氨基; X是O，NH，烷基氨基（NR），CO，S; 并且Y是O，NH，烷基氨基（NR），CO，S。本发明还涉及本发明的化合物和任选的药学上可接受的载体，用于治疗（和/或预防） 与突变CFTR相关的疾病或医学病症。

公开(公告)号：WO2010040862A3

公开(公告)日：2010-08-05

申请号：PCT/EP2009067119

申请日：2009-12-14

申请人： UNIVERSITAETSKLINIKUM MUENSTER ,  PREHM PETER

发明人： PREHM PETER

IPC分类号： C07C233/75 ,  A61K31/167 ,  A61P11/00

CPC分类号： C07C233/81 ,  C07C233/25 ,  C07H15/203

摘要： The present invention relates in general to a compound (activator) which is characterized by a formula selected from the following formulas A, B and/or C or a pharmaceutically acceptable salt thereof. The present invention further relates to pharmaceutical composition comprising the activator(s) of the invention and to their use in the treatment of (for treating) and/or preventing diseases or medical conditions which benefit from an increased transport of hyaluronan across a lipid bilayer. The present invention also relates to a method for manufacturing a pharmaceutical composition comprising the steps of formulating the activator defined herein in a pharmaceutically acceptable form.

摘要翻译： 本发明通常涉及特征在于选自下式A，B和/或C的式的化合物（活化剂）或其药学上可接受的盐。 本发明进一步涉及包含本发明活化剂的药物组合物以及它们在治疗（用于治疗）和/或预防受益于乙酰透明质酸跨脂质双层转运增加的疾病或医学病症中的用途。 本发明还涉及制备药物组合物的方法，其包括以药学上可接受的形式配制本文定义的活化剂的步骤。

公开(公告)号：WO2010040862A2

公开(公告)日：2010-04-15

申请号：PCT/EP2009/067119

申请日：2009-12-14

申请人： UNIVERSITÄTSKLINIKUM MÜNSTER ,  PREHM, Peter

发明人： PREHM, Peter

CPC分类号： C07C233/81 ,  C07C233/25 ,  C07H15/203

摘要： The present invention relates in general to a compound (activator) which is characterized by a formula selected from the following formulas A, B and/or C or a pharmaceutically acceptable salt thereof. The present invention further relates to pharmaceutical composition comprising the activator(s) of the invention and to their use in the treatment of (for treating) and/or preventing diseases or medical conditions which benefit from an increased transport of hyaluronan across a lipid bilayer. The present invention also relates to a method for manufacturing a pharmaceutical composition comprising the steps of formulating the activator defined herein in a pharmaceutically acceptable form.

摘要翻译： 本发明一般涉及一种化合物（活化剂），其特征在于选自下式A，B和/或C的化学式或其药学上可接受的盐。 本发明进一步涉及包含本发明的活化剂的药物组合物及其用于治疗（治疗）和/或预防受益于透明质酸穿过脂质双层的运输增加的疾病或医学病症的用途。 本发明还涉及制备药物组合物的方法，其包括以药学上可接受的形式配制本文定义的活化剂的步骤。

公开(公告)号：WO2010066912A3

公开(公告)日：2010-08-19

申请号：PCT/EP2009067124

申请日：2009-12-14

申请人： UNIVERSITAETSKLINIKUM MUENSTER ,  PREHM PETER

发明人： PREHM PETER

IPC分类号： C07C233/75 ,  A61K31/167 ,  A61P11/00

CPC分类号： C07C233/81 ,  C07C233/25 ,  C07H15/203

摘要： The present invention relates to a compound which is characterized by the formula (I) or a pharmaceutically acceptable salt, solvate, hydrate thereof, wherein the ring systems A and B are independently selected from a monosaccharide, aryl (preferably phenyl), a heteroaryl or cycloalkyl (preferably cyclohexan), preferably with all substituents in equatorial configurations; R1 is independently selected from alkyl (preferably C1 to C6), a substituted or unsubstituted phenyl, preferably CH3; R2 is H, alkyl (preferably C1 to C6), a carbohydrate in a glycosidic ß-linkage, preferably H; R3, R4, R5, and R6 are independently selected from H, (OH) hydroxy, alkyl preferably C1 to C6, alkoxy (preferably C1 to C6), amino, alkylamino (preferably C1 to C6), halogen, benzylamino, or benzoylamino; X is O, NH, alkylamino (NR), CO, S; and Y is O, NH, alkylamino (NR), CO, S. The present invention also relates to the compound of the invention and, optionally, a pharmaceutically acceptable carrier, for use in the treatment of (for treating) and/or preventing a disease or medical condition which is associated with mutant CFTR.

摘要翻译： （I）的化合物或其药学上可接受的盐，溶剂化物，水合物，其中环体系A和B独立地选自单糖，芳基（优选苯基），杂芳基或 环烷基（优选环己烷），优选具有赤道构型的所有取代基; R1独立地选自烷基（优选C1-C6），取代或未取代的苯基，优选CH3; R2是H，烷基（优选C1-C6），糖苷β-连接中的碳水化合物，优选H; （OH）羟基，烷基优选C1-C6，烷氧基（优选C1-C6），氨基，烷基氨基（优选C1-C6），卤素，苄基氨基或苯甲酰氨基; R3，R4，R5和R6独立地选自H， X是O，NH，烷基氨基（NR），CO，S; 和Y是O，NH，烷基氨基（NR），CO，S。本发明还涉及本发明化合物和任选的药学上可接受的载体，用于治疗（用于治疗）和/或预防 与突变CFTR相关的疾病或医学病症。

公开(公告)号：WO2010066912A2

公开(公告)日：2010-06-17

申请号：PCT/EP2009/067124

申请日：2009-12-14

申请人： UNIVERSITÄTSKLINIKUM MÜNSTER ,  PREHM, Peter

发明人： PREHM, Peter

IPC分类号： C07C233/75 ,  A61K31/167 ,  A61P11/00

CPC分类号： C07C233/81 ,  C07C233/25 ,  C07H15/203

摘要： The present invention relates to a compound which is characterized by the formula (I) or a pharmaceutically acceptable salt, solvate, hydrate thereof, wherein the ring systems A and B are independently selected from a monosaccharide, aryl (preferably phenyl), a heteroaryl or cycloalkyl (preferably cyclohexan), preferably with all substituents in equatorial configurations; R1 is independently selected from alkyl (preferably C1 to C6), a substituted or unsubstituted phenyl, preferably CH3; R2 is H, alkyl (preferably C1 to C6), a carbohydrate in a glycosidic β-linkage, preferably H; R3, R4, R5, and R6 are independently selected from H, (OH) hydroxy, alkyl preferably C1 to C6, alkoxy (preferably C1 to C6), amino, alkylamino (preferably C1 to C6), halogen, benzylamino, or benzoylamino; X is O, NH, alkylamino (NR), CO, S; and Y is O, NH, alkylamino (NR), CO, S. The present invention also relates to the compound of the invention and, optionally, a pharmaceutically acceptable carrier, for use in the treatment of (for treating) and/or preventing a disease or medical condition which is associated with mutant CFTR.

摘要翻译： 本发明涉及特征在于式（I）的化合物或其药学上可接受的盐，溶剂化物，水合物，其中环体系A和B独立地选自单糖，芳基 （优选苯基），杂芳基或环烷基（优选环己烷），优选具有赤道构型的所有取代基; R1独立地选自烷基（优选C1-C6），取代或未取代的苯基，优选CH3; R2是H，烷基（优选C1-C6），糖苷β-连接中的碳水化合物，优选H; （OH）羟基，烷基优选C1-C6，烷氧基（优选C1-C6），氨基，烷基氨基（优选C1-C6），卤素，苄基氨基或苯甲酰氨基; R3，R4，R5和R6独立地选自H， X是O，NH，烷基氨基（NR），CO，S; 和Y是O，NH，烷基氨基（NR），CO，S。本发明还涉及本发明化合物和任选的药学上可接受的载体，用于治疗（用于治疗）和/或预防 与突变CFTR相关的疾病或医疗状况。

公开(公告)号：WO2010066909A2

公开(公告)日：2010-06-17

申请号：PCT/EP2009/067113

申请日：2009-12-14

申请人： UNIVERSITÄTSKLINIKUM MÜNSTER ,  PREHM, Peter

发明人： PREHM, Peter

IPC分类号： C07C233/75 ,  C07C259/10 ,  C07C309/39 ,  C07D309/10 ,  A61K31/167 ,  A61K31/16 ,  A61K31/10 ,  A61K31/351 ,  A61P11/00 ,  C07H15/203

CPC分类号： C07C233/25 ,  C07C259/10 ,  C07C309/42 ,  C07D309/10

摘要： The present invention relates in general to a compound which is characterized by a formula selected from the following formulas A, B, C, D, E or F; or a pharmaceutically acceptable salt thereof. The present invention further relates to pharmaceutical composition comprising the inhibitor(s) of the invention and to their use in the treatment of (for treating) a disease which is associated with an excess transport of hyaluronan across a lipid bilayer. The present invention furthermore relates to the use of at least one inhibitor of the invention for the preparation of a pharmaceutical composition for the treatment of (for treating) a disease which is associated with an excess transport of hyaluronan across a lipid bilayer. The present invention also relates to a method for manufacturing a pharmaceutical composition comprising the steps of formulating the inhibitor defined herein in a pharmaceutically acceptable form.

摘要翻译： 本发明一般涉及由选自下式A，B，C，D，E或F的式表征的化合物; 或其药学上可接受的盐。 本发明进一步涉及包含本发明抑制剂的药物组合物，并涉及它们在治疗（用于治疗）与透明质酸过量转运穿过脂质双层相关的疾病中的用途。 本发明还涉及本发明的至少一种抑制剂在制备用于治疗（用于治疗）与透明质酸过量转运穿过脂质双层相关的疾病的药物组合物中的用途。 本发明还涉及用于制造药物组合物的方法，其包括以药学上可接受的形式配制本文定义的抑制剂的步骤。

公开(公告)号：WO9524497A3

公开(公告)日：1995-11-16

申请号：PCT/EP9500935

申请日：1995-03-10

申请人： FIDIA ADVANCED BIOPOLYMERS SRL ,  LANSING MANFRED ,  PREHM PETER ,  REGAN MICHAEL O ,  MARTINI IRENE

发明人： LANSING MANFRED ,  PREHM PETER ,  O'REGAN MICHAEL ,  MARTINI IRENE

IPC分类号： A61K31/728 ,  A61L15/28 ,  A61L27/20 ,  A61L31/04 ,  C12N11/10 ,  C12P19/26 ,  A61K31/715 ,  A61K31/735 ,  A61L27/00 ,  A61L29/00 ,  A61L31/00 ,  C08L1/02 ,  C08L5/00 ,  C08L5/04 ,  C08L5/08 ,  C12N11/04 ,  C12N11/12 ,  C12P19/04 ,  C12P19/18

CPC分类号： A61L27/20 ,  A61K31/728 ,  A61L15/28 ,  A61L31/042 ,  C12N11/10 ,  C12P19/26 ,  C08L5/08 ,  C08L5/04 ,  C08L1/02

摘要： Provided are in vitro processes for the production of polysaccharides such as hyaluronic acid, cellulose, polymannuronan, chitin, etc. These processes are carried out under reaction conditions that permit the recycling of nucleotide-phosphates required for the formation of sugar nucleotide precursors employed in the synthesis of these polysaccharides. Also provided are polysaccharides produced via these processes, and pharmaceutical and cosmetic compositions containing these polysaccharides.