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1. 发明申请

WO2021087306A1 DIRECT FLUORESCENT GLYCAN LABELING 审中-公开
公开(公告)号：WO2021087306A1
公开(公告)日：2021-05-06
申请号：PCT/US2020/058282
申请日：2020-10-30
申请人： BIO-TECHNE CORPORATION , WU, Zhengliang , WHITTAKER, Mark Russell , PERSON, Anthony D. , KALABOKIS, Vassilios , ERTELT, James Michael
发明人： WU, Zhengliang , WHITTAKER, Mark Russell , PERSON, Anthony D. , KALABOKIS, Vassilios , ERTELT, James Michael
IPC分类号： G01N33/533 , G01N33/58
摘要： This disclosure describes compositions including fluorophore-conj ugated sialic acids and fluorophore-conjugated fucose and methods of making and using those compositions. A fluorophore-conjugated sialic acid may include a cytidine monophosphate activated fluorophore- conjugated sialic acids (CMP-f-SA); a fluorophore-conjugated fucose may include a guanosine 5'-diphosphate activated fluorophore-conjugated fucose (GDP-f-Fuc). Methods of using the compositions include enzymatic incorporation of a fluorophore-conjugated sialic acid or a fluorophore-conjugated fucose or both to label and detect N- and O-glycans on glycoproteins. The compositions and methods may allow for the detection of specific glycans.

2. 发明申请

WO2008142720A4 QUINAZOLIN-OXIME DERIVATIVES AS HSP90 INHIBITORS 审中-公开
标题翻译：喹唑啉 - 肟衍生物作为HSP90抑制剂
公开(公告)号：WO2008142720A4
公开(公告)日：2009-03-05
申请号：PCT/IT2008000326
申请日：2008-05-15
申请人： DAC SRL , COURTNEY STEPHEN MARTIN , WHITTAKER MARK , MATHER OWEN CLIFFORD , YARNOLD CHRISTOPHER JOHN , BARKER OLIVER ROBIN , MONTALBETTI CHRISTIAN ALDO GEO , HESTERKAMP THOMAS , GARDINER MIHALY DANIEL
发明人： COURTNEY STEPHEN MARTIN , WHITTAKER MARK , MATHER OWEN CLIFFORD , YARNOLD CHRISTOPHER JOHN , BARKER OLIVER ROBIN , MONTALBETTI CHRISTIAN ALDO GEO , HESTERKAMP THOMAS , GARDINER MIHALY DANIEL
IPC分类号： C07D239/84 , A61K31/517 , A61P35/00 , C07D401/04 , C07D403/10 , C07D405/04 , C07D409/04
CPC分类号： C07D239/84 , C07D401/04 , C07D403/10 , C07D405/04 , C07D409/04
摘要： Compounds of general formula (I); or a stereoisomers, tautomers, pharmaceutically acceptable salts, or prodrugs thereof, wherein R1, R2, R3, R4, R5, R6, R8 and R9 are as defined herein, are useful for the treatment of diseases and conditions which are mediated by excessive or inappropriate Hsp90 activity such as cancers, viral infection and inflammatory diseases or conditions.
摘要翻译：通式（I）的化合物; 或其立体异构体，互变异构体，药学上可接受的盐或前药，其中R 1，R 2，R 3，R 4，R 5，R 6，R 8和R 9如本文所定义，可用于治疗由过量或不适当的Hsp90活性，例如癌症，病毒感染和炎性疾病或病症。

3. 发明申请

WO2004101506A1 GLYOXALASE INHIBITORS 审中-公开
标题翻译： GLYOXALASE抑制剂
公开(公告)号：WO2004101506A1
公开(公告)日：2004-11-25
申请号：PCT/GB2004/002101
申请日：2004-05-14
申请人： CHROMA THERAPEUTICS LIMITED , ASHTON, Mark , DAVIDSON, Alan , THOMAS, Russell , WHITTAKER, Mark
发明人： ASHTON, Mark , DAVIDSON, Alan , THOMAS, Russell , WHITTAKER, Mark
IPC分类号： C07C323/62
CPC分类号： C07D405/04 , A61K31/10 , A61K31/381 , A61K31/44 , A61K31/4436 , C07C323/62 , C07D213/85 , C07D217/26 , C07D409/04 , C07D409/14
摘要： This invention relates to compounds of formula (I) which are glyoxalase I inhibitors, pharmaceutical salts or compositions comprising such compounds, and the use of such compositions and compounds to treat various conditions alleviated by the inhibition of glyoxalase I. Wherein X is N or CH. R 2 is H, CF 3 ; or optionally substituted C 5-6 aryl, C 3-7 cycloalkyl, C 5-7 heterocyclyl. R 3 is H; or optionally substituted C 5-6 aryl, C 3-7 cycloalkyl, C 5-7 heterocyclyl. Alternatively R 2 and R 3 together form an optionally substituted C 3-4 alkylene group wherein L 3 and L 4 are single bonds thus forming a C 5-6 ring fused with the aromatic ring to which L 3 and L 4 are attached. L 3 and L 4 are independently selected from a single bond, optionally substituted C 1-4 alkylene, -L 9 YN(OH)C(=O)L 10 - and -L 9 C(=O)N(OH)YL 10 -, wherein L 9 and L 10 are independently selected from optionally substituted C 1-4 alkylene, C 5-6 arylene, C 1-4 alkylene-C 5-6 arylene and a single bond, wherein Y is NH or a single bond.
摘要翻译：本发明涉及作为乙二醛酶I抑制剂的式（I）化合物，包含这些化合物的药物盐或组合物，以及这些组合物和化合物用于治疗通过抑制乙二醛酶I减轻的各种病症的用途。其中X是N或CH 。 R 2是H，CF 3; 或任选取代的C 5-6芳基，C 3-7环烷基，C 5-7杂环基。 R 3为H; 或任选取代的C 5-6芳基，C 3-7环烷基，C 5-7杂环基。或者，R 2和R 3一起形成任选取代的C 3-4亚烷基，其中L 3和L 4是单键，从而形成与芳环稠合的C5-6环，其中L 3 >和L 4连接。 L 3和L 4独立地选自单键，任选取代的C 1-4亚烷基，-L 9 YN（OH）C（= O）L 10 - 和-L 9 C （= O）N（OH）YL 10 - ，其中L 9和L 10独立地选自任选取代的C 1-4亚烷基，C 5-6亚芳基，C 1-4亚烷基-C 5-6亚芳基和单键，其中Y是NH或单键。

4. 发明申请

WO1996026918A1 SYNTHESIS OF CARBOXYLIC AND HYDROXAMIC ACID DERIVATIVES 审中-公开
标题翻译：羧酸和羟基酸衍生物的合成
公开(公告)号：WO1996026918A1
公开(公告)日：1996-09-06
申请号：PCT/GB1996000467
申请日：1996-03-01
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , FLOYD, Christopher, David , WHITTAKER, Mark
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： C07C259/06
CPC分类号： C07C259/06 , C07C231/00 , Y02P20/55
摘要： A method for the preparation of carboxylic and hydroxamic acid derivatives by cocondensation in a liquid organic medium of three reaction components, namely a carboxylic acid reaction component of formula (II), an imine reaction component of formula (III), and an isonitrile reaction component of formula (IV), wherein X is hydrogen or an amino protecting group, or the residue of a solid phase reaction substrate; Y is (i) a group -CO2R5 wherein R5 is a carboxyl protecting group or the residue of a solid phase reaction substrate or (ii) a group -CONR6OR7 wherein R6 is an amino protecting group or the residue of a solid phase reaction substrate and R7 is a hydroxyl protecting group or the residue of a solid phase reaction substrate; [S1], [S2], [S3] and [S4] each represent covalently bound moieties which are substantially non reactive with the reaction components (II), (III), or (IV) defined above; provided that only one of X, R5, R6 and R7 is the residue of a solid phase reaction substrate.
摘要翻译：在三种反应组分的液体有机介质中，即式（II）的羧酸反应组分，式（III）的亚胺反应组分和异氰酸酯反应组分的缩合反应制备羧酸和异羟肟酸衍生物的方法式（Ⅳ）的化合物，其中X为氢或氨基保护基，或固相反应底物的残基; Y是（i）-CO 2 R 5基团，其中R 5是羧基保护基或固相反应底物的残基或（ii）基团-CONR 6OR 7，其中R 6是氨基保护基或固相反应底物的残基， R7是羟基保护基或固相反应底物的残基; [S1]，[S2]，[S3]和[S4]各自表示与上述定义的反应组分（II），（III）或（IV）基本上不反应的共价结合部分; 条件是X，R5，R6和R7中只有一个是固相反应底物的残基。

5. 发明申请

WO1996016931A1 METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：金属蛋白酶抑制剂
公开(公告)号：WO1996016931A1
公开(公告)日：1996-06-06
申请号：PCT/GB1995002770
申请日：1995-11-27
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , BECKETT, Raymond, Paul , WHITTAKER, Mark , MILLER, Andrew , MARTIN, Fionna, Mitchell
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： C07C235/70
CPC分类号： C07C237/22 , C07C259/06 , C07D333/34
摘要： Compounds of general formula (I), principally characterized in that R4 is a polyether group, are water soluble matrix metalloproteinase inhibitors.
摘要翻译：通式（I）的化合物，其主要特征在于R4是聚醚基，是水溶性基质金属蛋白酶抑制剂。

6. 发明申请

WO1996006074A1 METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：金属蛋白酶抑制剂
公开(公告)号：WO1996006074A1
公开(公告)日：1996-02-29
申请号：PCT/GB1995001971
申请日：1995-08-18
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , BECKETT, Raymond, Paul , MILLER, Andrew , WHITTAKER, Mark
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： C07C259/06
CPC分类号： C07D209/48 , C07C259/06 , C07C323/60 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D333/34
摘要： Compounds of formula (I) principally characterised in that R4 is an optionally substituted C3-C8 cycloalkyl group or optionally substituted C4-C8 cycloalkenyl group are inhibitors of matrix metalloproteinases.
摘要翻译：式（I）化合物主要特征在于R4是任选取代的C 3 -C 8环烷基或任选取代的C 4 -C 8环烯基是基质金属蛋白酶的抑制剂。

7. 发明申请

WO1993014072A1 AMINO ACID DERIVATIVES AS PAF-RECEPTOR ANTAGONISTS 审中-公开
标题翻译：氨基酸衍生物作为PAF-受体拮抗剂
公开(公告)号：WO1993014072A1
公开(公告)日：1993-07-22
申请号：PCT/GB1993000009
申请日：1993-01-06
申请人： BRITISH BIO-TECHNOLOGY LIMITED , BOWLES, Stephen, Arthur , MILLER, Andrew , WHITTAKER, Mark
发明人： BRITISH BIO-TECHNOLOGY LIMITED
IPC分类号： C07D235/08
CPC分类号： C07D471/04 , C07D213/56 , C07D213/57 , C07D235/08
摘要： Compounds of general formula (I), wherein W represents pyrid-3-yl, benzimidazol-1-yl, imidazo(4,5-c)pyridin-1-yl, imidazo(4,5-c)pyridin-3-yl and imidazo(4,5-c)pyridin-5-yl optionally substituted by alkyl; Z represents: a) a divalent alkanediyl, alkenediyl or alkynediyl group, b) a -(CH2)qU(CH2)r- group, optionally substituted, q is an integer from 0-3, r is an integer from 0-3 and U is -O-, -S- or a furandiyl, tetrahydrofurandiyl, thiophenediyl, tetrahydrothiophenediyl, thiazolediyl, tetrahydrothiazolediyl, piperazinediyl, piperidinediyl, cyclopentanediyl, cyclohexanediyl, cycloheptenediyl or benzenediyl group; or c) a ( alpha ) group wherein m is an integer from 0-3, X is -O-, -S- or -CH2- and each of R and R is independently hydrogen or alkyl; Q represents a carbonyl, thiocarbonyl or sulphonyl group or a bond; B represents: a) a -VR group wherein V is -C(=O)-, -C(=O)O-, -CH2O-, -CH2OC(=O)-, -C(=S)-, -CH2OC(=O)NH-, -C(=S)O-, -CH2S-, -C(=O)NHSO2- or -SO2NHC(=O)-; b) a -CH2NR R group or a -CONR R group; c) a group Y where Y is a 5- or 6-membered heterocyclic ring; d) a group -CH2-Y or C(=O)NHY; are antagonists of platelet activating factor (PAF).
摘要翻译：通式（I）的化合物，其中W表示吡啶-3-基，苯并咪唑-1-基，咪唑并（4,5-c）吡啶-1-基，咪唑并（4,5-c）吡啶-3-基和任选被烷基取代的咪唑并（4,5-c）吡啶-5-基; Z表示：a）二价烷二基，亚烯基或炔二基，b）α-（CH 2）q U（CH 2）r - 基，任选取代，q是0-3的整数，r是0-3的整数， U是-O-，-S-或呋喃基，四氢呋喃二基，噻吩二基，四氢噻吩二基，噻唑二基，四氢噻唑二基，哌嗪二基，哌啶二基，环戊二基，环己二基，环庚二烯基或苯二基。或c）（α）基团，其中m是0-3的整数，X是-O - ， - S-或-CH 2 - ，R 4和R 5各自独立地是氢或烷基; Q表示羰基，硫代羰基或磺酰基或键; B表示：a）-VR 8基团，其中V是-C（= O） - ， - C（= O）O-，-CH 2 O - ， - CH 2 OC（= O） - ， - C（= S） - ， - CH 2 OC（= O）NH - ， - C（= S）O-，-CH 2 S-，-C（= O）NHSO 2 - 或-SO 2 NHC（= O） - ; b）-CH 2 NR 9 R 10基团或-CONR 9 R 10基团; c）Y为5或6元杂环的Y基团; d）基团-CH 2 -Y或C（= O）NHY; 是血小板激活因子（PAF）的拮抗剂。

8. 发明申请

WO1993001191A1 CYCLIC ETHER ACETAL PAF ANTAGONISTS 审中-公开
标题翻译：周期性乙醚PAF拮抗剂
公开(公告)号：WO1993001191A1
公开(公告)日：1993-01-21
申请号：PCT/GB1992001189
申请日：1992-07-01
申请人： BRITISH BIO-TECHNOLOGY LIMITED , WHITTAKER, Mark , MILLER, Andrew , BOWLES, Stephen, Arthur
发明人： BRITISH BIO-TECHNOLOGY LIMITED
IPC分类号： C07D471/04
CPC分类号： C07D403/12 , C07D405/12 , C07D417/12 , C07D471/04
摘要： Compounds of general formula (I), wherein W represents a 5- or 6-membered aromatic heterocyclic ring containing one or more non-quaternised sp2 nitrogen atoms in its ring, which heterocyclic ring may be optionally fused to a benzene ring or to a further 5- or 6-membered aromatic heterocyclic ring containing one or more nitrogen atoms, wherein at least one of the said heterocyclic rings may also contain an oxygen or sulphur atom, and wherein any of the rings may be optionally substituted with one or more substituents selected from -C1-C6 alkyl, -OC1-C6 alkyl, halo, -CF3 and -CN; Z represents a) a divalent alkanediyl group from 1 to 8 carbon atoms which may be a straight or branched-chain, wherein the said group is either unsubstituted or substituted by one or more substituents selected from hydroxy, -OC1-C6 alkyl, -SC1-C6 alkyl and halo; or b) a divalent alkenediyl or alkynediyl group from 2 to 8 carbon atoms which may be a straight or branched-chain, wherein the said group is either unsubstituted or subtituted by one or more substituents selected from hydroxy, -OC1-C6 alkyl, -SC1-C6 alkyl and halo; R , R , R , R , R , and R each represents a hydrogen atom, a -C1-C18 alkyl or a -C2-C18 alkenyl group; or R and R together with the carbon atoms to which they are attached can form a five to ten membered monocycloalkyl or bicycloalkyl ring which may be optionally substituted with one or more substituents selected from -C1-C6 alkyl, -OC1-C6 alkyl, halo, -CF3 and -CN; or R , R and R , R and the carbon atoms to which they are attached form a phenyl ring which may be optionally substituted with one or more substituents selected from -C1-C6 alkyl, -OC1-C6 alkyl, halo, -CF3 and -CN; X represents a bond, an oxygen atom, a sulphur atom, a -NH- group, a -N(C1-C6alkyl)- group, a -(CH2)n- group or a -CR R - group; n represents an integer of 1, 2 or 3; R and R each represents a -C1-C18 alkyl or a -C2-C18 alkenyl group; or R and R together with the carbon atoms to which they are attached can form a five to ten membered monocycloalkyl or bicycloalkyl ring which may be optionally substituted with one or more substituents selected from -C1-C6 alkyl, -OC1-C6 alkyl, halo, -CF3 and -CN; or R , R and R , R and the carbon atoms to which they are attached form a phenyl ring which may be optionally substituted with one or more substituents selected from -C1-C6 alkyl, -OC1-C6 alkyl, halo, -CF3 and -CN; and their pharmaceutically and veterinarily acceptable acid addition salts and hydrates are antagonists of platelet activating factor (PAF) and as such are useful in the treatment or amelioration of various diseases or conditions mediated by PAF.
摘要翻译：通式（I）的化合物，其中W表示在其环中含有一个或多个非季铵化的sp2氮原子的5-或6-元芳族杂环，该杂环可以任选地稠合至苯环或另一个含有一个或多个氮原子的5-或6-元芳族杂环，其中所述杂环中的至少一个也可以含有氧或硫原子，并且其中任何环可任选地被一个或多个选自下列的取代基取代： -C 1 -C 6烷基，-OC 1 -C 6烷基，卤素，-CF 3和-CN; Z表示a）可以是直链或支链的1至8个碳原子的二价烷二基，其中所述基团是未取代的或被一个或多个选自羟基，-OC 1 -C 6烷基，-SC 1 -C 1-6烷基和卤素; 或b）可以是直链或支链的2至8个碳原子的二价亚烯二基或炔二基，其中所述基团是未取代的或被一个或多个选自羟基，-OC 1 -C 6烷基， SC1-C6烷基和卤素; R 1，R 2，R 3，R 4，R 5和R 6各自表示氢原子，-C 1 -C 18烷基或-C 2 -C 18烯基 ; 或R 3和R 5与它们所连接的碳原子一起可以形成5至10元单环烷基或双环烷基环，其可任选被一个或多个选自以下的取代基取代：-C 1 -C 6烷基， OC 1 -C 6烷基，卤素，-CF 3和-CN; 或R 3，R 4和R 5，R 6和它们所连接的碳原子形成苯环，所述苯环可任选被一个或多个选自以下的取代基取代：-C 1 -C 6烷基，-OC 1 -C 6烷基，卤素，-CF 3和-CN; X表示键，氧原子，硫原子，-NH-基，-N（C1-C6烷基） - 基， - （CH2）n-基或-CR7R8 - 组; n表示1,2或3的整数; R 7和R 8各自表示-C 1 -C 18烷基或-C 2 -C 18烯基; 或R 3和R 7与它们所连接的碳原子一起可以形成5至10元单环烷基或双环烷基环，其可任选被一个或多个选自以下的取代基取代：-C 1 -C 6烷基， OC 1 -C 6烷基，卤素，-CF 3和-CN; 或R 3，R 4和R 7，R 8和它们所连接的碳原子形成苯环，该苯环可任选地被一个或多个选自以下的取代基取代：-C 1 -C 6烷基，-OC 1 -C 6烷基，卤素，-CF 3和-CN; 其药物和兽医学上可接受的酸加成盐和水合物是血小板活化因子（PAF）的拮抗剂，因此可用于治疗或改善PAF介导的各种疾病或病症。

9. 发明申请

WO1992003423A1 BENZIMIDAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND APPLICATION 审中-公开
标题翻译：苯并咪唑衍生物，其制备和应用的方法
公开(公告)号：WO1992003423A1
公开(公告)日：1992-03-05
申请号：PCT/GB1991001392
申请日：1991-08-15
申请人： BRITISH BIO-TECHNOLOGY LIMITED , WHITTAKER, Mark , MILLER, Andrew , BOWLES, Stephen, Arthur
发明人： BRITISH BIO-TECHNOLOGY LIMITED
IPC分类号： C07D235/08
CPC分类号： C07D401/12 , A61K31/415 , C07D235/08 , C07D403/12 , C07D471/04 , C07F7/1804
摘要： Compounds of general formula I; I wherein: A1 is =N-, =CH- or =CR1-; A2 is =N-, =CH- or =CR2-; provided that, when one of A1 and A2 is a nitrogen atom, the other of A1 and A2 is other than a nitrogen atom; wherein the other variables are as defined in the specification and their pharmaceutically and veterinarily acceptable acid addition salts and hydrates are antagonists of platelet activating factor (PAF) and as such are useful in the treatment or amelioration of various diseases or disorders mediated by PAF.

10. 发明申请

WO1992003422A1 BENZIMIDAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR APPLICATION 审中-公开
标题翻译：苯并咪唑衍生物，其制备方法及其应用
公开(公告)号：WO1992003422A1
公开(公告)日：1992-03-05
申请号：PCT/GB1991001391
申请日：1991-08-15
申请人： BRITISH BIO-TECHNOLOGY LIMITED , WHITTAKER, Mark , MILLER, Andrew
发明人： BRITISH BIO-TECHNOLOGY LIMITED
IPC分类号： C07D235/08
CPC分类号： C07D401/12 , A61K31/415 , C07D235/08 , C07D403/12 , C07D471/04 , C07F7/1804
摘要： Compounds of general formula I; I wherein: A1 is =N-, =CH- or =CR1-; A2 is -N=, -CH= or -CR2=; provided that, when one of A1 and A2 is a nitrogen atom, the other of A1 and A2 is other than a nitrogen atom; the rest of the variables are described in the specification; and their pharmaceutically and veterinarily acceptable acid addition salts and hydrates are antagonists of platelet activating factor (PAF) and as such are useful in the treatment or amelioration of various diseases or disorders mediated by PAF.

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