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1. 发明申请

WO2003062461A1 FMDV LEADER PEPTIDASE ASSAY 审中-公开
标题翻译： FMDV领导者肽分析
公开(公告)号：WO2003062461A1
公开(公告)日：2003-07-31
申请号：PCT/GB2003/000164
申请日：2003-01-16
申请人： AMURA THERPEUTICS LIMITED , RAMJEE, Manoj, Kumar
发明人： RAMJEE, Manoj, Kumar
IPC分类号： C12Q1/37
CPC分类号： G01N33/6893 , C12Q1/37
摘要： Foot-and-mouth disease virus (FMDV) leader peptidase activity is assayed in the presence of a protective surfactant. Such surfactants significantly enhance peptidase activity. This increase in activity results in increased sensitivity and means that less enzyme is used per assay. This increase in sensitivity also makes the assay amenable to adaptation for generic instrumentation ( e.g. microtitre plates and readers). Suitable protective surfactants include (thio)alkyl glycosides, bile acids, glucamide polyoxyethylenes, n -dodecyl-N,N-dimethylglycine, zwitterionic detergents, dimethyl(C 5 -C 15 )alkylphosphine oxides, sodium n -dodecyl sulphate, alkyl glucosides, 3-([4- tert -octyl]phenoxy)-1-propane sulphonic acid sodium salt and non-detergent sulphobetaines.
摘要翻译：在保护性表面活性剂存在下测定口蹄疫病毒（FMDV）前导肽酶活性。这些表面活性剂显着增强肽酶活性。活性的增加导致敏感性增加，并且意味着每次测定使用较少的酶。灵敏度的这种增加也使得测定法适合于通用仪器（例如微量滴定板和读数器）的适应。合适的保护性表面活性剂包括（硫代）烷基糖苷，胆汁酸，葡糖酰胺聚氧乙烯，正十二烷基-N，N-二甲基甘氨酸，两性离子洗涤剂，二甲基（C 5 -C 15 - 烷基氧化膦，十二烷基硫酸钠，烷基葡糖苷，3 - （[4-叔辛基]苯氧基）-1-丙烷磺酸钠盐和非洗涤剂磺基甜菜碱。

2. 发明申请

WO2003062267A3 ENZYME SUBSTRATES FOR THE DETERMINATION OF ACTIVITY OF STAPHYLOCOCCUS SP. EXTRACELLULAR PROTEASE 审中-公开
公开(公告)号：WO2003062267A3
公开(公告)日：2003-07-31
申请号：PCT/GB2003/000120
申请日：2003-01-16
申请人： AMURA THERAPEUTICS LIMITED , RAMJEE, Manoj, Kumar
发明人： RAMJEE, Manoj, Kumar
IPC分类号： C07K7/06
摘要： Compounds of general formula (I): A) A compound of general formula (I) Y-AA1-AA2-AA3-AA4-R-Glu-NH 2 , Y-A 1 -A 2 -A 3 -A 4 -R-Glu-NH 2 wherein Y and R are reporter groups; A 1 is either the D-isomer or the L-isomer form of isoleucine; each of A 2 and A 3 is independently Ala or 2-aminobutyric acid (Abu); A 4 is Pro, L-3-hydroxyproline (Pro(3-OH)), L-4-hydroxyproline (Pro (4-OH)), L-tetrahydroisoquinoline-1-carboxylic acid (THIQ), L-tetrahydroisoquinoline-3-carboxylic acid (Tic), L-pipecolic acid (Pip), 1-amino-1-cyclopentane carboxylic acid (1-ACP) or D-Pro; and any one of A 1 , A 2 , A 3 and A 4 can be replaced by any other amino acid group (Xaa); and the other protein based substrates are cleavable by Staphyococcus sp. extracellular cysteine protease and are therefore likely to be of use in monitoring enzyme activity for purposes such as investigating candidate enzyme modulators and screening for therapeutic agents.

3. 发明申请

WO2002057248A3 INHIBITORS OF CRUZIPAIN AND OTHER CYSTEINE PROTEASES 审中-公开
公开(公告)号：WO2002057248A3
公开(公告)日：2002-07-25
申请号：PCT/GB2002/000188
申请日：2002-01-17
申请人： INCENTA LIMITED , QUIBELL, Martin
发明人： QUIBELL, Martin
IPC分类号： C07D307/32
摘要： Compounds of general formula (I): wherein R 1 , R 2 , Y,(X) o , (W) n , (V) m , Z and U are as defined in the specification, are inhibitors of cruzipain and other cysteine protease inhibitors and are useful as therapeutic agents, for example in Chagas' disease, or for validating therapeutic target compounds.

4. 发明申请

WO2000015839A9 METHOD FOR DETERMINING SUSCEPTIBILITY TO BONE DAMAGE BY SCREENING POLYMORPHISMS IN THE VITAMIN D RECEPTOR GENE 审中-公开
公开(公告)号：WO2000015839A9
公开(公告)日：2000-03-23
申请号：PCT/EP1999/007719
申请日：1999-09-10
申请人： ERASMUS UNIVERSITEIT ROTTERDAM , UITTERLINDEN, Andreas, Gerardus , VAN LEEUWEN, Johannes, Petrus, Thomas, Maria , POLS, Huibert, Adriaan, Pieter
发明人： UITTERLINDEN, Andreas, Gerardus , VAN LEEUWEN, Johannes, Petrus, Thomas, Maria , POLS, Huibert, Adriaan, Pieter
IPC分类号： C12Q1/68
摘要： The present invention relates to a prognostic method and means for determining susceptibility to bone damage in a subject, by screening for polymorphisms in the Vitamin D receptor or collagen Iα1 genes. In particular, the method for determining susceptibility to bone damage comprises analysing the genetic material of a subject to determine which of the B/b, A/a or T/t alleles of the restriction enzyme sites Bsm I, Apa I and Taq I respectively are present. The method may further comprise determining which allele is present at the Sp 1 restriction site of the collagen Iα1 gene. Specific combinations of the above alleles represent a haplotype which is associated with susceptibility to bone damage.

5. 发明申请

WO2004007501A1 BIOLOGICALLY ACTIVE COMPOUNDS 审中-公开
标题翻译：生物活性化合物
公开(公告)号：WO2004007501A1
公开(公告)日：2004-01-22
申请号：PCT/GB2003/002957
申请日：2003-07-15
申请人： AMURA THERAPEUTICS LIMITED , QUIBELL, Martin , RAY, Peter, Christopher , WATTS, John Paul
发明人： QUIBELL, Martin , RAY, Peter, Christopher , WATTS, John Paul
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Compounds of general formula (I) wherein: Z = CR 3 R 4 , where R 3 and R 4 are independently chosen from C O-7 -alkyl P 1 = CR 5 R 6 , P 2 = O, CR 7 R 8 or NR 9 , Y = CR 10 R 11 -C(O) or CR 10 R 11 -C(S) or CR 10 R 11 -S(O) or CR 10 R 11 -SO 2 (X) o =.CR 16 R 17 (W) n = 0, S, C(O), S(O) or S(O) 2 -or NR 18 (V) m = C(O), C(S), S(O), S(O) 2 , S(O) 2 NH, OC(O), NHC(O), NHS(O), NHS(O) 2 , OC(O)NH, C(O)NH or CR 19 R 20 , C=N-C(O)-OR 19 or C=N-C(O)-NHR 19 , U = a stable. 5- to 7-membered monocyclic or a stable 8- to 11-membered bicyclic ring which is either saturated or unsaturated, and which includes zero to four heteroatoms and their salts, hydrates, solvates, complexes and prodrugs are inhibitors of cathepsin K and other cysteine protease inhibitors and are useful as therapeutic agents, .for example in osteoporosis, Paget's disease gingival diseases such as gingivitis and periodontitis, hypercalaemia of malignancy, metabolic bone disease, diseases involving matrix or cartilage degradation, in particular osteoarthritis and rheumatoid arthritis and neoplastic diseases. The compounds are also useful for validating therapeutic target compounds.
摘要翻译：通式（I）的化合物，其中：Z = CR 3 R 4，其中R 3和R 4独立地选自CO-7-烷基P1 = CR 5 R 6， R 2 = O，CR 7 R 8或NR 9，Y = CR 10 R 11 -C（O）或CR 10 R 11 -C（S）（O）或CR 10 R 11 -SO 2（X）o = CR 16 R 17（W）n = 0，S，C（O） S（O）或S（O）2 - 或NR 18（V）m = C（O），C（S），S（O），S（O）2，S（O）2 NH，OC O），NHC（O），NHS（O），NHS（O）2，OC（O）NH，C（O）NH或CR 19 R 20，C = NC（O） >或C = NC（O）-NHR 19，U =稳定的。 5-至7-元单环或饱和或不饱和的稳定的8至11元双环，并且其包括0至4个杂原子及其盐，水合物，溶剂化物，复合物和前药是组织蛋白酶K等的抑制剂半胱氨酸蛋白酶抑制剂，并且可用作治疗剂，例如骨质疏松症，佩吉特氏病牙龈疾病如牙龈炎和牙周炎，恶性高钙血症，代谢性骨病，涉及基质或软骨降解的疾病，特别是骨关节炎和类风湿性关节炎和肿瘤性疾病。所述化合物也可用于验证治疗性目标化合物。

6. 发明申请

WO2003087824A3 CHARGE-BALANCED CHEMOSELECTIVE LINKERS 审中-公开
公开(公告)号：WO2003087824A3
公开(公告)日：2003-10-23
申请号：PCT/GB2003/001505
申请日：2003-04-07
申请人： AMURA THERAPEUTICS LIMITED , FLINN, Nicholas, Sean , QUIBELL, Martin , TURNELL, William, Gordon , RAMJEE, Manoj, Kumar
发明人： FLINN, Nicholas, Sean , QUIBELL, Martin , TURNELL, William, Gordon , RAMJEE, Manoj, Kumar
IPC分类号： G01N33/543
摘要： Compounds according to general formulae (Ia to Ie) wherein: X = O or S; Y is O, S or CH 2 , CHR, CRR, where R is C 1-7 alkyl; Z is O or S; R 1 is H or C 1-7 alkyl; R 2 is H or C 1-7 alkyl; R 4 is H or C 1-7 alkyl at any vacant position on the aromatic ring; R 3 is C 1-7 alkyl-L 1 -R 5 -L 2 - R 6 -COOH, C 3-10 cycloalkyl-L 1 -R 5 -L 2 - R 6 -COOH or Ar-C 0-7 alkyl-L 1 -R 5 -L 2 - R 6 -COOH; each of L 1 and L 2 is absent or a suitable linker such as an amide CONH; or an ether -O-, or a thioether -S- or a sulphone -S0 2 -; R 5 is C 1-7 alkyl, C 3-1O cycloalkyl or Ar-C 0-7 alkyl each of which is substituted with either NR 8 R 9 , where the nitrogen atom is capable of being protonated in solution to give N + HR 8 R 9 ; or a quaternary nitrogen atom N + R 8 R 9 R 10 , such that R 5 contains a positive charge; each of R 8 , R 9 and R 10 is independently C 1-7 alkyl, C 3-10 cycloalkyl or Ar-C 0-7 alkyl, or any two or more of R 8 , R 9 and R 10 together form an alicyclic or arylalicyclic ring system; R 6 is C 1-7 alkyl, C 3-10 cycloalkyl or Ar-C 0-7 alkyl; and their salts, hydrates, solvates, complexes or prodrugs are of use as linkers for conjugating an epitope to a carrier protein.

7. 发明申请

WO2003062460A1 ASSAY FOR STAPHYLOCOCCUS SP. EXTRACELLULAR CYSTEINE PEPTIDASE ACTIVITY 审中-公开
标题翻译：测定STAPHYLOCOCCUS SP。细胞外蛋白肽活性
公开(公告)号：WO2003062460A1
公开(公告)日：2003-07-31
申请号：PCT/GB2003/000139
申请日：2003-01-16
申请人： AMURA THERAPEUTICS LIMITED , RAMJEE, Manoj, Kumar
发明人： RAMJEE, Manoj, Kumar
IPC分类号： C12Q1/37
CPC分类号： C12Q1/37
摘要： Staphylococcus sp. extracellullar cysteine peptidase activity is assayed in the presence of a protective surfactant. Such surfactants significantly enhance peptidase activity. This increase in activity results in increased sensitivity and means that less enzyme is used per assay. This increased in sensitivity also makes the assay amenable to adaptation for generic instrumentation ( e.g. microtitre plates and readers). Sutable protective surfacants includes polyoxyethylenes and (C 5 -C 15 )alkyl sulphates.
摘要翻译：葡萄球菌 sp。在保护性表面活性剂存在下测定细胞外半胱氨酸肽酶活性。这些表面活性剂显着增强肽酶活性。活性的增加导致敏感性增加，并且意味着每次测定使用较少的酶。灵敏度的增加也使得测定法适合于通用仪器（例如微量滴定板和读数器）的适应。可食用保护性表面活性剂包括聚氧乙烯和（C5-C15）烷基硫酸盐。

8. 发明公开

EP1358176A2 INHIBITORS OF CRUZIPAIN AND OTHER CYSTEINE PROTEASES 审中-公开
标题翻译：抑制剂和其他cruzipain半胱氨酸蛋白酶
公开(公告)号：EP1358176A2
公开(公告)日：2003-11-05
申请号：EP02715508.4
申请日：2002-01-17
申请人： Amura Therapeutics Limited
发明人： QUIBELL, Martin,c/o Incenta House , RAMJEE, Manoj, Kumar,c/o Incenta House
IPC分类号： C07D307/93 , C07D409/12 , A61K31/381 , A61K31/5377 , A61K31/343 , A61P33/02
CPC分类号： C07D307/935 , C07D409/12
摘要： Compounds of general formula (I): wherein R1, Y, (X)¿0?, (W)n, (V)m, Z and U are as defined in the specification, are inhibitors of cruzipain and other cysteine protease inhibitors and are useful as therpeutic agents, for example in Chagas' disease, or for validating therapeutic target compounds.

9. 发明授权

EP0470127B1 PCP RECEPTOR LIGANDS AND THE USE THEREOF 失效
标题翻译： PCP受体配体及其用途
公开(公告)号：EP0470127B1
公开(公告)日：2003-02-26
申请号：EP90906688.8
申请日：1990-04-13
申请人： STATE OF OREGON BY AND THROUGH OREGON STATE BOARD OF HIGHER EDUCATION ON BEHALF OREGON HEALTH SC. UNIV. AND OREGON STATE UNIV.
发明人： WEBER, Eckard , KEANA, John , BARMETTLER, Peter
IPC分类号： C07D471/08 , A61K31/55
CPC分类号： A61K31/55

10. 发明授权

EP0920330B1 hCG AND DERIVATIVES AS MATRIX METALLOPROTEASES INHIBITORS 失效
标题翻译： HCG和衍生物作为抑制剂基质金属蛋白酶
公开(公告)号：EP0920330B1
公开(公告)日：2002-11-27
申请号：EP97934545.1
申请日：1997-07-25
申请人： Applied Research Systems ARS Holding N.V.
发明人： ALBINI, Adriana , ORENGO, Giorgia
IPC分类号： A61K38/24 , A61P29/00 , A61P25/28
CPC分类号： A61K38/24
摘要： The use of hCG, hCG beta -subunit, as well as fragments and active derivatives thereof, or hCG beta -core in the preparation of a medicament for the prophylaxis and/or the treatment of pathologies requiring inhibition of the matrix metalloprotease (MMP) enzymatic activity.

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