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1. 发明授权

US5703059A Disaccharide ligands for selectins 失效
标题翻译：选择素的二糖配体
公开(公告)号：US5703059A
公开(公告)日：1997-12-30
申请号：US492002
申请日：1996-03-12
申请人： Nigel Mark Allanson , Alan Hornsby Davidson
发明人： Nigel Mark Allanson , Alan Hornsby Davidson
IPC分类号： C07H15/04 , C07H15/10 , A61K31/715 , C07H15/00
CPC分类号： C07H15/10 , C07H15/04 , Y02P20/55
摘要： Compounds of formula (I), or a salt, solvate or hydrate thereof, wherein Z represents a divalent group selected from those of formulae I(a) to I(g) defined in the specification; Y represents a single bond or a divalent group selected from those of formulae I(h) to I(j) defined in the specification; each Z independently represents hydrogen or a hydroxyl protecting group; R.sup.1 represents hydrogen or a group --CH(OZ)CH.sub.2 (OZ) wherein Z has the meaning defined above; R.sup.2 represents hydrogen, a pharmaceutically acceptable cation, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, or (optionally substituted)phenyl-(C.sub.1-4) alkyl; and R.sup.3 represents hydrogen, C.sub.1-6 alkyl, (C.sub.1-4) alkyl-substituted phenyl or benzoate; and n is 1, 2 or 3. The compounds are ligands of E-, P-, and L-selectins and are useful as anti-inflammatory agents and as agents for the control of tumour metastasis.
摘要翻译： PCT No.PCT / GB94 / 00088 Sec。 371日期：1996年4月12日 102（e）日期1996年4月12日PCT 1994年1月19日PCT PCT。公开号WO94 / 17084 日期：1994年8月4日图像化合物（I）或其盐，溶剂合物或水合物，其中Z表示选自式I（a）至I（g ）; Y表示选自本说明书中定义的式I（h）至I（j）的单键或二价基团; 每个Z独立地表示氢或羟基保护基; R 1表示氢或基团-CH（OZ）CH 2（OZ），其中Z具有上述定义; R 2表示氢，药学上可接受的阳离子，C 1-6烷基，C 2-6烯基或（任选取代的）苯基 - （C 1-4）烷基; 并且R 3表示氢，C 1-6烷基，（C 1-4）烷基取代的苯基或苯甲酸酯; 并且n是1,2或3.化合物是E-，P-和L-选择蛋白的配体，并且可用作抗炎剂和用作控制肿瘤转移的试剂。

2. 发明授权

US06274716B1 Combinatorial library of moenomycin analogs and methods of producing same 失效
公开(公告)号：US06274716B1
公开(公告)日：2001-08-14
申请号：US09394044
申请日：1999-09-13
申请人： Nigel Mark Allanson , Tin Yau Chan , Nicole T. Hatzenbuhler , Rakesh K. Jain , Ramesh Kakarla , Rui Liang , Dashan Liu , Domingos J. Silva , Michael J. Sofia
发明人： Nigel Mark Allanson , Tin Yau Chan , Nicole T. Hatzenbuhler , Rakesh K. Jain , Ramesh Kakarla , Rui Liang , Dashan Liu , Domingos J. Silva , Michael J. Sofia
IPC分类号： C07H500
CPC分类号： C07H15/04 , C07H15/203 , C40B40/00
摘要： A combinatorial chemical library of compounds structurally related to the moenomycin class of antibiotics has the formula wherein D is a donor mono- or disaccharide, A is an acceptor monosaccharide, and P-R is a lipophosphoglycerate mimetic group. Members of the library have a glycosidic linkage between the anomeric carbon of D and the C2 carbon of A, and the D-A moiety is in turn covalently linked through the anomeric carbon of A to the P-R group. Members of the library exhibit their greatest structural diversity in terms of substitutions occurring at the C3 position of the A residue, substitutions at the C2 position of the D residue, and different P-R groups used in assembling the compounds. Members of the library are preferably synthesized by solid phase techniques involving stepwise coupling of the respective units to a support, functionalizing the A and/or D saccharides either before or after immobilizing them on the support, and cleaving the assembled compounds from the support. Preferred functionalities attached to the sugar residues are amides, carbamates, ureas, sulfonamides, substituted amines, esters, carbonates, and sulfates. Exemplary P-R groups are derivatives of homoserine, glyceric acid, salicylates and mandelic acid. Members of the library can be screened for anti-microbial activity by contacting them with a culture of microbes and monitoring the growth rate of the microbes.

3. 发明授权

US06114309A Combinatorial library of moenomycin analogs and methods of producing same 失效
标题翻译：霉酚霉素类似物组合库及其生产方法
公开(公告)号：US06114309A
公开(公告)日：2000-09-05
申请号：US975229
申请日：1997-11-21
申请人： Nigel Mark Allanson , Tin Yau Chan , Nicole T. Hatzenbuhler , Rakesh K. Jain , Ramesh Kakarla , Rui Liang , Dashan Liu , Domingos J. Silva , Michael J. Sofia
发明人： Nigel Mark Allanson , Tin Yau Chan , Nicole T. Hatzenbuhler , Rakesh K. Jain , Ramesh Kakarla , Rui Liang , Dashan Liu , Domingos J. Silva , Michael J. Sofia
IPC分类号： C12Q1/02 , A61K31/7016 , A61K31/702 , A61P31/04 , C07B61/00 , C07H1/02 , C07H5/08 , C07H11/04 , C07H15/04 , C07H15/203 , A61K31/70 , C07H13/00
CPC分类号： C07H15/04 , C07H15/203 , C40B40/00
摘要： A combinatorial chemical library of compounds structurally related to the moenomycin class of antibiotics has the formula ##STR1## wherein D is a donor mono- or disaccharide, A is an acceptor monosaccharide, and P-R is a lipophosphoglycerate mimetic group. Members of the library have a glycosidic linkage between the anomeric carbon of D and the C2 carbon of A, and the D-A moiety is in turn covalently linked through the anomeric carbon of A to the P-R group. Members of the library exhibit their greatest structural diversity in terms of substitutions occurring at the C3 position of the A residue, substitutions at the C2 position of the D residue, and different P-R groups used in assembling the compounds. Members of the library are preferably synthesized by solid phase techniques involving stepwise coupling of the respective units to a support, functionalizing the A and/or D saccharides either before or after immobilizing them on the support, and cleaving the assembled compounds from the support. Preferred functionalities attached to the sugar residues are amides, carbamates, ureas, sulfonamides, substituted amines, esters, carbonates, and sulfates. Exemplary P-R groups are derivatives of homoserine, glyceric acid, salicylates and mandelic acid. Members of the library can be screened for anti-microbial activity by contacting them with a culture of microbes and monitoring the growth rate of the microbes.
摘要翻译：结构上与新霉素类抗生素相关的化合物的组合化学文库具有下式：其中D是供体单糖或二糖，A是受体单糖，P-R是脂磷酸甘油酸酯模拟组。文库成员在D的异头碳和A的C2碳之间具有糖苷键，D-A部分又通过A的端基异碳共价连接到P-R基团。关于在A残基的C3位置发生的取代，在D残基的C2位置的取代以及用于组装化合物的不同的P-R基团，图书馆的成员表现出最大的结构多样性。文库的成员优选通过固相技术合成，其包括将各单元逐步偶联到载体上，在将它们固定在载体上之前或之后将A和/或D糖功能化，并将载体化合物从载体上分离。附着于糖残基的优选功能是酰胺，氨基甲酸酯，脲，磺酰胺，取代的胺，酯，碳酸酯和硫酸酯。示例性的P-R基团是高丝氨酸，甘油酸，水杨酸盐和扁桃酸的衍生物。通过与微生物培养物接触并监测微生物的生长速率，可以筛选图书馆成员的抗菌活性。

4. 发明授权

US06207820B1 Combinatorial library of moenomycin analogs and methods of producing same 失效
标题翻译：霉酚霉素类似物组合库及其生产方法
公开(公告)号：US06207820B1
公开(公告)日：2001-03-27
申请号：US09394045
申请日：1999-09-13
申请人： Nigel Mark Allanson , Tin Yau Chan , Nicole T. Hatzenbuhler , Rakesh K. Jain , Ramesh Kakarla , Rui Liang , Dashan Liu , Domingos J. Silva , Michael J. Sofia
发明人： Nigel Mark Allanson , Tin Yau Chan , Nicole T. Hatzenbuhler , Rakesh K. Jain , Ramesh Kakarla , Rui Liang , Dashan Liu , Domingos J. Silva , Michael J. Sofia
IPC分类号： C07H100
CPC分类号： C07H15/04 , C07H15/203 , C40B40/00
摘要： A combinatorial chemical library of compounds structurally related to the moenomycin class of antibiotics has the formula wherein D is a donor mono- or disaccharide, A is an acceptor monosaccharide, and P—R is a lipophosphoglycerate mimetic group. Members of the library have a glycosidic linkage between the anomeric carbon of D and the C2 carbon of A, and the D—A moiety is in turn covalently linked through the anomeric carbon of A to the P—R group. Members of the library exhibit their greatest structural diversity in terms of substitutions occurring at the C3 position of the A residue, substitutions at the C2 position of the D residue, and different P—R groups used in assembling the compounds. Members of the library are preferably synthesized by solid phase techniques involving stepwise coupling of the respective units to a support, functionalizing the A and/or D saccharides either before or after immobilizing them on the support, and cleaving the assembled compounds from the support. Preferred functionalities attached to the sugar residues are amides, carbamates, ureas, sulfonamides, substituted amines, esters, carbonates, and sulfates. Exemplary P—R groups are derivatives of homoserine, glyceric acid, salicylates and mandelic acid. Members of the library can be screened for anti-microbial activity by contacting them with a culture of microbes and monitoring the growth rate of the microbes.
摘要翻译：结构上与霉酚霉素类抗生素有关的化合物的组合化学文库，其中D是供体单糖或二糖，A是受体单糖，P-R是脂磷酸甘油酸酯模拟组。文库成员在D的异头碳和A的C2碳之间具有糖苷键，D-A部分又通过A的端基异碳共价连接到P-R基团。关于在A残基的C3位置发生的取代，在D残基的C2位置的取代以及用于组装化合物的不同的P-R基团，图书馆的成员表现出最大的结构多样性。文库的成员优选通过固相技术合成，其包括将各单元逐步偶联到载体上，在将它们固定在载体上之前或之后将A和/或D糖功能化，并将载体化合物从载体上分离。附着于糖残基的优选功能是酰胺，氨基甲酸酯，脲，磺酰胺，取代的胺，酯，碳酸酯和硫酸酯。示例性的P-R基团是高丝氨酸，甘油酸，水杨酸盐和扁桃酸的衍生物。通过与微生物培养物接触并监测微生物的生长速率，可以筛选图书馆成员的抗菌活性。

5. 发明授权

US08486962B2 Antifungal agents 有权
标题翻译：抗真菌剂
公开(公告)号：US08486962B2
公开(公告)日：2013-07-16
申请号：US11914516
申请日：2006-05-18
申请人： Samantha Patricia Thomson , Rhian Teresa Davies , Nigel Mark Allanson , Alexandre Kuvshinov , Gareth Morse Davies , Philip Neil Edwards
发明人： Samantha Patricia Thomson , Rhian Teresa Davies , Nigel Mark Allanson , Alexandre Kuvshinov , Gareth Morse Davies , Philip Neil Edwards
IPC分类号： A61K31/437 , A01P3/00 , A01N43/52
CPC分类号： A61K31/437
摘要： Compounds of formula (I), and pharmaceutically acceptable salts thereof, may be used in therapy, for example as antifungal agents: (I) wherein: R1, R2, R3, R4, R5, R6, R7, X and X1 are as defined herein. Certain compounds of formula (I) are also provided. Compounds of formula (T), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
摘要翻译：式（I）化合物及其药学上可接受的盐可用于治疗，例如抗真菌剂：（I）其中：R1，R2，R3，R4，R5，R6，R7，X和X1定义如下：这里。还提供某些式（I）化合物。式（T）化合物及其农业上可接受的盐也可用作农业杀真菌剂。

6. 发明申请

US20080161302A1 Antifungal Agents 有权
标题翻译：抗真菌剂
公开(公告)号：US20080161302A1
公开(公告)日：2008-07-03
申请号：US11914516
申请日：2006-05-18
申请人： Samantha Patricia Thomson , Rhian Teresa Davies , Nigel Mark Allanson , Alexandre Kuvshinov , Gareth Morse Davies , Philip Neil Edwards
发明人： Samantha Patricia Thomson , Rhian Teresa Davies , Nigel Mark Allanson , Alexandre Kuvshinov , Gareth Morse Davies , Philip Neil Edwards
IPC分类号： A61K31/437 , C07D471/04 , A61K31/5377 , A61K31/496 , A61P31/10
CPC分类号： A61K31/437
摘要： Compounds of formula (I), and pharmaceutically acceptable salts thereof, may be used in therapy, for example as antifungal agents: (I) wherein: R1, R2, R3, R4, R5, R6, R7, X and X1 are as defined herein. Certain compounds of formula (I) are also provided. Compounds of formula (T), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
摘要翻译：式（I）化合物及其药学上可接受的盐可用于治疗，例如抗真菌剂：（I）其中：R1，R2，R3，R4，R5，R6，R7，X和X 1 如本文所定义。还提供某些式（I）化合物。式（T）化合物及其农业上可接受的盐也可用作农业杀真菌剂。

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