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21. 发明申请

WO2007085806A2 THERAPEUTIC DELIVERY OF CARBON MONOXIDE 审中-公开
标题翻译：治疗性输送一氧化碳
公开(公告)号：WO2007085806A2
公开(公告)日：2007-08-02
申请号：PCT/GB2007/000198
申请日：2007-01-23
申请人： HEMOCORM LIMITED , UNIVERSITY OF SHEFFIELD , MOTTERLINI, Roberto, Angelo , MANN, Brian, Ernest , JOHNSON, Tony, Richard , SCAPENS, David, Alistair , AQIL, Rehan
发明人： MOTTERLINI, Roberto, Angelo , MANN, Brian, Ernest , JOHNSON, Tony, Richard , SCAPENS, David, Alistair , AQIL, Rehan
IPC分类号： A61K31/28 , A61K33/00
CPC分类号： A61K33/00 , A61K31/28
摘要： Compounds, pharmaceutical compositions and methods for the therapeutic delivery of carbon monoxide to humans and other mammals that employ transition metal complexes having at least a substituted cyclopentadienyl, indenyl or fluorenyl ligand and two or more carbonyl ligands.
摘要翻译：用于将一氧化碳治疗性递送给使用具有至少一个取代的环戊二烯基，茚基或芴基配体和两个或多个羰基配体的过渡金属配合物的人和其他哺乳动物的化合物，药物组合物和方法。 / p>

22. 发明申请

WO2007006714A1 CYSTEINE PROTEASE INHIBITORS 审中-公开
标题翻译： CYSTEINE PROTEASE抑制剂
公开(公告)号：WO2007006714A1
公开(公告)日：2007-01-18
申请号：PCT/EP2006/063950
申请日：2006-07-06
申请人： MEDIVIR AB , KANGASMETSA, Jussi , HISCOCK, Stephen , JOHNSON, Tony , SAMUELSSON, Bertil , TOZER, Matt , GRABOWSKA, Urszula
发明人： KANGASMETSA, Jussi , HISCOCK, Stephen , JOHNSON, Tony , SAMUELSSON, Bertil , TOZER, Matt , GRABOWSKA, Urszula
IPC分类号： C07D487/04 , A61K31/407 , A61P19/10
CPC分类号： C07D487/04
摘要： Compounds of the formula II wherein R 1 and R 1, are halo; or one of R 1 and R 1, is halo, and the other is is H; R 2 is R 4 , -C(=O)R 4 ; -OC(=O)R 4 , -S(=O) n R 4 , -S(=O)nNRdRe; R 3 is H, -OR 4 , -SR 4 ; R 3' is H; or R 3 and R 3' together define =O; R 4 is -C 1 C 6 alkyl, -C 0 -C 3 alkylenecarbocyclyl or -C 0 -C 3 alkyleneheterocyclyl, any of which is optionally substituted with up to three substituents selected from R 7 ; R 5 is -C 1 C 5 alkyl, -CH 2 CR 5" C 3 -C 4 -cycloalkyl; R 5' is H; or R 5 and R 5' together with the carbon to which they are attached define C 4 -C 6 -cycloalkyl; R 5" is H, C 1 C 2 alkyl, C 1 C 2 haloalkyl, hydroxyl, OC 1 C 2 alkyl, fluoro; E is -C(=O)-, -S(=O) m -, -NRaS(=O) m -, -NRaC(=O)-, -OC(=O)-, -CRbRc-; R 6 is a stable, optionally substituted, monocyclic or bicyclic carbocycle or heterocycle, wherein the, or each, ring has 4, 5 or 6 ring atoms and 0 to 3 hetero atoms selected from S, O and N; have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepisn K, such as osteoporosis, osteoarthritis, rhuematoid arthritis or bone metastases.
摘要翻译：其中R 1和R 2的式II化合物是卤素; 或R 1和R 2中的一个为卤素，另一个为H; R 2是R 4，-C（= O）R 4; -OC（= O）R 4，-S（= O）n R 4，-S（= O）n NR d Re; R 3是H，-OR 4，-SR 4; R 3'是H; 或R 3和R 3'一起定义= O; R 4是-C 1 -C 6烷基，-C 0 -C 3 -C 3 亚烷基环丙基或-C 0 -C 3亚烷基杂环基，其中任何一个任选被至多三个选自R 7的取代基取代; R 5是-C 1 -C 5烷基，-CH 2 CH 2，5“ > C 3 -C 4 - 环烷基; R 5'是H;或R 5和R SUP > 5'与它们所连接的碳一起定义为C 4 -C 6 - 环烷基; R 5“是 H，C 1 -C 2烷基，C 1 -C 2卤代烷基，羟基，OC 1，氟; C 1 -C 6烷基，氟; E是-C（= O） - ， - S（= O）m - ， - NR a（= O）m - ， - NR a C（= O） - ， -OC（= O） - ， - CR b R c-; R 6是稳定的，任选取代的单环或双环碳环或杂环，其中环或每个环具有4,5或6个环原子和0至3个选自S，O的杂原子和 N; 可用于治疗特征为导管骨K不适当表达或活化的疾病，如骨质疏松症，骨关节炎，类型性关节炎或骨转移。

23. 发明申请

WO2005066180A1 CYSTEINE PROTEASE INHIBITORS 审中-公开
标题翻译： CYSTEINE PROTEASE抑制剂
公开(公告)号：WO2005066180A1
公开(公告)日：2005-07-21
申请号：PCT/GB2005/050003
申请日：2005-01-06
申请人： MEDIVIR AB , NILSSON, Magnus , ZHOU, Xiao-Xiong , ODEN, Lourdes , CLASSON, Bjorn , NOREN, Rolf , GRABOWSKA, Urszula , JACKSON, Philip , FALLON, Philip , CARR, Andrew , LILEY, Mark , TOZER, Matt , JOHNSON, Tony , DIAZ, Victor , CRESPO, Laia , KANGASMETSA, Jussi , BONNAUD, Thierry
发明人： NILSSON, Magnus , ZHOU, Xiao-Xiong , ODEN, Lourdes , CLASSON, Bjorn , NOREN, Rolf , GRABOWSKA, Urszula , JACKSON, Philip , FALLON, Philip , CARR, Andrew , LILEY, Mark , TOZER, Matt , JOHNSON, Tony , DIAZ, Victor , CRESPO, Laia , KANGASMETSA, Jussi , BONNAUD, Thierry
IPC分类号： A61K31/407 , C07D491/04
CPC分类号： C07D491/04 , A61K31/407
摘要： A compound of the formula (II) wherein one of R 1 and R 2 is halo and the other is H or halo; R 3 is C 1 -C 4 straight or branched chain, optionally fluorinated, alkyl; R 4 is H; or R 3 together with R 4 and the adjoining backbone carbon defines: a spiro-C 5 -C 7 cycloalkyl, optionally substituted with 1 to 3 substituents selected from halo, hydroxyl, C 1 -C 4 alkyl or C 1 -C 4 haloalkyl; or optionally bridged with a methylene group; or a C 4 -C 6 saturated heterocycle having a hetero atom selected from O, NRa, S, S(=O) 2 ; where Ra is H, C 1 -C 4 alkyl or CH 3 C(=O); R 5 is independently selected from H or methyl; E is -C(=O)-, -S(=O) m -, -NR 5 S(=O) m -, -NR 5 C(=O)-, -OC(=O)-, R 6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or hetorocycle; m is independently 0,1 or 2; are inhibitors of cathepsin K and useful in the treatment or prophylaxis of osteoporosis.
摘要翻译：其中R 1和R 2之一为卤素且另一个为H或卤素的式（II）化合物; R 3是C 1 -C 4直链或支链，任选氟化的烷基; R 4是H; 或R 3与R 4一起，相邻的主链碳定义：任选被1至3个选自卤素，羟基，C 1 -C 4烷基或C 1 -C 4卤代烷基的取代基取代的螺C5-C7环烷基; 或任选地与亚甲基桥连; 或具有选自O，NR a，S，S（= O）2的杂原子的C 4 -C 6饱和杂环; 其中R a是H，C 1 -C 4烷基或CH 3 C（= O）; R 5独立地选自H或甲基; E是-C（= O） - ， - S（= O）m - ， - NR 5 S（= O）m - ， - NR 5 C（= O） - ， - OC（= O） - ，R 6是稳定的，任选取代的单环或双环碳环或hetorocycle; m独立地为0,1或2; 是组织蛋白酶K的抑制剂，可用于治疗或预防骨质疏松症。

24. 发明申请

WO1997042216A1 AUTO-DECONVOLUTING COMBINATORIAL LIBRARIES 审中-公开
标题翻译：自动解除组合图书馆
公开(公告)号：WO1997042216A1
公开(公告)日：1997-11-13
申请号：PCT/GB1997001158
申请日：1997-04-24
申请人： PEPTIDE THERAPEUTICS LIMITED , QUIBELL, Martin , JOHNSON, Tony , HART, Terance
发明人： PEPTIDE THERAPEUTICS LIMITED
IPC分类号： C07K01/04
CPC分类号： C07K7/06 , B01J19/0046 , B01J2219/00315 , B01J2219/00504 , B01J2219/0072 , C07K1/047 , C07K5/06043 , C07K5/06191 , C07K7/02 , C40B60/14 , G01N33/68
摘要： The present invention relates to the field of apparatus and methods which provide the rapid generation of structure/activity relationships using auto-deconvoluting combinatorial libraries, which facilitate the invention of novel active compounds. The invention provides apparatus and methods which can be used for the rapid generation of structure/activity relationship (SAR) data, and, therefore, the characterisation of the active motif of any group of compounds. The invention provides libraries of compounds which interact with an active moiety, and apparatus and methods to identify such compounds. The active moieties may be (but are not limited to) enzymes, receptors, antibodies, etc. The interaction of the active moiety with the compounds of the library may be (but is not limited to) the interaction of a substrate or inhibitor with an enzyme, the interaction of a ligand with a receptor, the interaction of an antigen or antigenic epitope with an antibody, etc.
摘要翻译：本发明涉及使用自动去卷积组合库快速产生结构/活性关系的装置和方法领域，其促进了新型活性化合物的发明。本发明提供了可用于快速产生结构/活性关系（SAR）数据的装置和方法，并因此用于表征任何一组化合物的活性基序。本发明提供了与活性部分相互作用的化合物文库，以及鉴定这些化合物的装置和方法。活性部分可以是（但不限于）酶，受体，抗体等。活性部分与文库化合物的相互作用可以是（但不限于）底物或抑制剂与酶，配体与受体的相互作用，抗原或抗原表位与抗体的相互作用等

25. 发明申请

WO1995008561A1 SYNTHESES OF AZAPEPTIDES BY THE FMOC/TERT-BUTYL/POLYAMIDE TECHNIQUE 审中-公开
标题翻译：通过FMOC /叔丁基/多胺技术合成腈肟酸
公开(公告)号：WO1995008561A1
公开(公告)日：1995-03-30
申请号：PCT/GB1994002103
申请日：1994-09-26
申请人： MEDICAL RESEARCH COUNCIL , JOHNSON, Tony , QUIBELL, Martin
发明人： MEDICAL RESEARCH COUNCIL
IPC分类号： C07K01/04
CPC分类号： C07K1/04 , C07C271/12
摘要： Disclosed is a method of synthesising a peptide comprising at least one aza-amino acid residue, the method comprising: coupling one or more amino acids to a solid phase support so as to form a supported moiety; activating the supported moiety; reacting the activated supported moiety with one or more aza-amino acid precursors having a fluorenylmethoxycarbonyl (Fmoc)-protected free amino function, so as to form a supported azapeptide; releasing the azapeptide from the solid phase support and deprotecting (if necessary) the side chains of the one or more amino acid and one or more aza-amino acid residues, together with certain novel compounds of use in the method and more generally.
摘要翻译：公开了一种合成包含至少一个氮杂 - 氨基酸残基的肽的方法，所述方法包括：将一个或多个氨基酸偶联到固相载体上以形成负载部分; 活化支持的部分; 使活化的支持部分与一种或多种具有芴基甲氧基羰基（Fmoc）保护的游离氨基官能团的氮杂 - 氨基酸前体反应，以形成负载的氮杂肽; 从固相载体中释放azapeptide，并将一个或多个氨基酸和一个或多个氮杂氨基酸残基的侧链（如果需要）脱保护（连同某些在该方法中使用的新化合物）。

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