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    • 21. 发明申请
    • CHEMICAL COMPOUNDS
    • 化学化合物
    • WO2006051314A2
    • 2006-05-18
    • PCT/GB2005004361
    • 2005-11-11
    • UCL BIOMEDICA PLCVALLANCE PATRICK JOHN THOMPSONLEIPER JAMES MITCHELLSELWOOD DAVID LAWRENCEROSSITER SHARONHARTZOULAKIS BASIL
    • VALLANCE PATRICK JOHN THOMPSONLEIPER JAMES MITCHELLSELWOOD DAVID LAWRENCEROSSITER SHARONHARTZOULAKIS BASIL
    • C07C279/14A61K31/16A61K31/198A61K31/223A61K31/40A61K31/445A61K31/5375A61P9/10A61P11/06A61P19/02C07C279/16C07C279/18C07C323/52C07D295/215
    • C07C279/14A61K31/16A61K31/198A61K31/223A61K31/40A61K31/445A61K31/4453A61K31/5375C07C279/16C07C279/18C07C323/44C07C2601/02C07D295/215C07D295/32
    • Compounds of formula (I) have been found to be useful as inhibitors of DDAH use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in the treatment of a disease whose pathology is affected by DDAH formula (I) wherein: either - (a) R 1 is C 3 -C 12 alkyl, C 3 -C 12 alkenyl, C 3 -C 12 alkynyl, C 6 -C 10 aryl, C 3 -C 8 carbocyclyl, 5- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, -L-A, -L-Het-L', -L-Y-L', -L-Het-A or -L-Y-A, wherein: L is C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl; L' is C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl; A is C 6 -C 10 aryl, C 3 -C 8 carbocyclyl, 5- to 10-membered heterocyclyl or 5- to 10-membered heteroaryl; Het is -O-, -S- or -NR'-, wherein R' is hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl; and Y is -CO-, -SO-, -SO 2 -, -CO-O-, -CO-NR'-, -O-CO- or -NR'-CO-, wherein R' is as defined above; - R 2 is hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl; and - R 3 is hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl, - or (b) R 1 and R 2 form, together with the nitrogen to which they are attached, a 5- to 10-membered heterocyclic or heteroaryl ring, and R 3 is as defined above, - or (c) R 1 and R 3 form, together with the -N-C=N- moiety to which they are attached, a 5- to 10-membered heterocyclic or heteroaryl ring, and R 2 is as defined above; - R 4 is hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl; B is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, -O-L-, -S-L- or-L-Het-L'-, wherein L, L' and Het are as defined above; - X is -O-, -S- or -NR'-, wherein R' is as defined above; -R 5 is hydrogen, C 1 -C 6 alkyl, C 2 - 6 alkenyl, C 2 -C 6 alkynyl, aryl, C 3 -C 8 carbocyclyl, 5- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, -L-A, -L-Het-L', -L-Y-L', -L-Het-A, -L-Y-A, -L-A-Het-A, -L-A-L'-A or -L-A-Het-L'-A, wherein L, L', Het and Y are as defined above and wherein each A is the same or different and is as defined above; -R 6 is hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl; - R 7 is hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl, or R 7 is a bond, a C 1 -C 4 alkyl or C 2 -C 4 alkenyl moiety which is joined to one of the carbon atoms of B to form, together with the -N-C- moiety to which R 7 and B are attached, a 5- to 10-membered heterocyclic ring; and - R 8 is hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl.
    • 已经发现式(I)化合物可用作DDAH抑制剂用于式(I)化合物或其药学上可接受的盐在制备用于治疗病症为 受DDAH式(I)影响,其中: - (a)R 1是C 3 -C 12烷基,C 3 C 12 - 12链烯基,C 3 -C 12炔基,C 6-C≡N C 10 -C 10芳基,C 3 -C 8碳环基,5至10元杂环基,5至10元杂芳基,-LA,-L -Het-L',-LY-L',-L-Het-A或-LYA,其中:L为C 1 -C 6烷基,C 如上所定义; R 4是氢,C 1 -C 6烷基,C 2 -C 6烷基,C 1 -C 6烷基, 烯基或C 2 -C 6 - 炔基; B是C 1 -C 6烷基,C 2 -C 6链烯基,-OL-,-SL - 或-L-Het-L'-,其中L,L'和Het如上所定义; -X是-O - , - S-或-NR'-,其中R'如上定义; R 5是氢,C 1 -C 6烷基,C 2 -C 6 - 亚烷基,C 2 -C 6炔基,芳基,C 3 -C 8碳环基,5- 至10元杂环基,5至10元杂芳基,-LA,-L-Het-L',-LY-L',-L-Het-A,-LYA,-LA-Het-A,-LA -L'-A或-LA-Het-L'-A,其中L,L',Het和Y如上所定义,并且其中每个A相同或不同,如上所定义; R 6是氢,C 1 -C 6烷基,C 2 -C 6烷基,C 1 -C 6烷基,C 1 -C 6烷基, 烯基或C 2 -C 6 - 炔基; R 7是氢,C 1 -C 6烷基,C 2 -C 6烷基,C 1 -C 6烷基,C 1 -C 6烷基, C 1 -C 12烷基或C 2 -C 6 - 炔基,或R 7是键,C 1〜 -C 4烷基或C 2 -C 4亚烷基部分,其与B的一个碳原子连接形成,与 R 7和B连接的-NC-部分,5至10元杂环; 和 - R 8是氢,C 1 -C 6烷基,C 2 -C 6烷基,C 1 -C 6烷基,C 1 -C 6烷基, 烯基或C 2 -C 6炔基。
    • 30. 发明申请
    • MATTRESS PROTECTION
    • MATTRESS保护
    • WO2005051134A1
    • 2005-06-09
    • PCT/GB2004/004942
    • 2004-11-22
    • UCL BIOMEDICA PLCBAIN, DuncanPELL, Martin, FergusonNICHOLSON, Graham
    • BAIN, DuncanPELL, Martin, FergusonNICHOLSON, Graham
    • A47C21/06
    • A61F5/48A47C27/006
    • The present invention seeks to address the chronic and worsening problem of mattress management in hospitals by providing a mattress protector to shield a mattress or mattress core from body fluids, the protector not only comprising a shielding cover for the mattress (1) or mattress core but also a detector in an inter­ or under-layer (2) of the cover to detect body fluid that has passed into or through the cover. The detector may be chemical, with the cover being a transparent cover (3) and the under-layer being absorbent and having a dye that is activated by a body fluid to provide a visual indication of presence of the body fluid. In an alternative embodiment the detector may be an apparatus monitoring electrical conductivity. This suitably uses threads of electrically conductive yarn forming either the warp or weft of a thin flexible under layer of the protective cover (5) and which are linked to a small processor (7) which monitors the electrical conductivity between neighbouring conductive threads in the sensing layer.
    • 本发明旨在通过提供床垫保护器来将床垫或床垫芯与体液屏蔽,来解决医院床垫管理的长期和恶化问题,保护器不仅包括用于床垫(1)或床垫芯的屏蔽罩,而且 也是盖子的中间层或下层(2)中的检测器,以检测已经通过或穿过盖的体液。 检测器可以是化学的,其中盖是透明盖(3),底层是吸收性的,并且具有被体液激活的染料以提供体液存在的视觉指示。 在替代实施例中,检测器可以是监测导电性的装置。 这适当地使用形成保护盖(5)的薄柔性底层的经线或纬线的导电纱线,并且连接到小型处理器(7),该小处理器(7)监测感测中相邻导电丝之间的导电性 层。