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1. 发明申请

WO2005016868A3 MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：基质金属蛋白酶抑制剂
公开(公告)号：WO2005016868A3
公开(公告)日：2005-05-19
申请号：PCT/EP2004009087
申请日：2004-08-12
申请人： GLAXO GROUP LTD , HOLMES IAN , WATSON STEPHEN PAUL
发明人： HOLMES IAN , WATSON STEPHEN PAUL
IPC分类号： C07C233/51 , C07C235/34 , C07C235/78 , C07C255/57 , C07D209/08 , C07D333/24 , C07C235/00 , C07C255/00
CPC分类号： C07C235/78 , C07C233/51 , C07C235/34 , C07C255/57 , C07C2601/14 , C07D209/08 , C07D333/24
摘要： Compounds of Formula (I), wherein R represents optionally substituted -C4-12 alkyl, -C2-10alkylcycloalkyl, -C2-6 alkyl heterocycloalkyl, -C2-6alkylaryl, optionally substituted 5- or 6- membered aryl or heteroaryl, except pyridinyl. Z represents a bond, CH2, O, S, SO, SO2, NR , OCR R , CR R O, or Z, R and Q together form an optionally substituted fused tricyclic group; Q represents an optionally substituted 5- or 6- membered aryl or heteroaryl ring; X represents COR ; R represents CONH2, CO2H, CO2R , SO2R or SO2NR R , except that R ; may not represent CO2R when X is CONH2 ; R represents OR , or NR R ; R and R each independently represents H, C1-6 alkyl or C1-4 alkylaryl; R represents H or C1-6 alkyl; R represents C1-6 alkyl; R and R each independently represents H or C1-6 alkyl or R and R together with the nitrogen atom to which they are attached form a 5- or 6- membered ring which may optionally include 1 or more further heteroatoms selected from O, S and N; and physiologically functional derivatives thereof with the exception of [3-(acetylamino)-4-cyclohexylphenyl]-butanedioic acid and 3-(acetylamino)-4-cyclohexylphenyl]-butanedioic acid diethyl ether; butanedioic acid [3-methoxy-4-(phenylmethoxy)phenyl]; butanedioic acid [4-(phenylmethoxy)phenyl]; with the proviso that when R represents C4-12 alkyl, Z is other than a bond, O or CH2; and physiologically functional derivatives thereof , processes for their preparation, pharmaceutical formulations containing them and their use as inhibitors of matrix metallproteinase enzymes (MMPs) are described.
摘要翻译：式（I）化合物，其中R 1表示任选取代的-C 4-12烷基，-C 2-10烷基环烷基，-C 2-6烷基杂环烷基，-C 2-6烷基芳基，任选取代的5-或6-元芳基或杂芳基，除了吡啶基。 Z表示键，CH 2，O，S，SO，SO 2，NR 4，OCR 4 R 5，CR 4 R 5 O或Z，R 1和Q一起形成任选取代的稠合三环基团; Q代表任选取代的5元或6元芳基或杂芳基环; X代表COR 3; R 2代表CONH 2，CO 2 H，CO 2 R 7，SO 2 R 7或SO 2 NR 8 R 9，除了R 2; 当X是CONH 2时可能不代表CO 2 R 7; R 3表示OR 6或NR 8 R 9; R 4和R 5各自独立地表示H，C 1-6烷基或C 1-4烷基芳基; R6代表H或C1-6烷基; R 7表示C 1-6烷基; R 8和R 9各自独立地表示H或C 1-6烷基或者R 8和R 9与它们所连接的氮原子一起形成5-或6-元环，其可任选地包括1个或多个选自O，S和N的其他杂原子; 以及除[3-（乙酰氨基）-4-环己基苯基] - 丁二酸和3-（乙酰氨基）-4-环己基苯基] - 丁二酸二乙酯以外的其生理学功能衍生物; 丁二酸[3-甲氧基-4-（苯基甲氧基）苯基]; 丁二酸[4-（苯基甲氧基）苯基]; 条件是当R 1代表C 4-12烷基时，Z不是键，O或CH 2; 及其生理功能衍生物，其制备方法，含有它们的药物制剂以及它们作为基质金属蛋白酶（MMP）抑制剂的用途。

2. 发明专利

GB2408538B Ground recycled tyre block for use in crash barriers and land erosion control 未知
公开(公告)号：GB2408538B
公开(公告)日：2006-07-05
申请号：GB0406573
申请日：2004-03-24
申请人： HOLMES IAN
发明人： HOLMES IAN
IPC分类号： E02B3/06 , E01F15/04 , E01F15/14 , E02B3/12 , E02B3/14

3. 发明专利

IL275360D0 Optimised compounds 未知
公开(公告)号：IL275360D0
公开(公告)日：2020-07-30
申请号：IL27536020
申请日：2020-06-14
申请人： ENA THERAPEUTICS PTY LTD , JACKSON DAVID , HOLMES IAN , ZENG WEIGUANG , DEMAISON CHRISTOPHE
发明人： JACKSON DAVID , HOLMES IAN , ZENG WEIGUANG , DEMAISON CHRISTOPHE
IPC分类号： A61K47/54 , A61K47/60 , A61P31/00 , A61P31/16 , C07K5/062
摘要： The present invention relates to TLR2 agonist compounds and their compositions, and the use of such compounds and compositions in the prevention and/or treatment of respiratory infections, or diseases or conditions associated with viral or bacterial infections.

4. 发明专利

GB2515565A Improvements to submarine guidance system 未知
公开(公告)号：GB2515565A
公开(公告)日：2014-12-31
申请号：GB201311657
申请日：2013-06-28
申请人： HOLMES IAN
发明人： HOLMES IAN
IPC分类号： B63G8/42 , F42B19/00 , F42B22/00
摘要： A series of undersea vessels may be connected via resilient articulated couplings allowing movement between the vessels. Each of the vessels may be equipped with an explosive charge and may be deployed as array of mines. The vessels may be ship or submarine launched via a tube. The vessels may separate when deployed as a mine array and may have monitoring, listening equipment fitted to detect other vessels. The vessels may have anchors, chains and a buoyancy device to allow them to float above the sea bed. The deployed vessels may be subsequently gathered back together and moved to a second location. The lead vehicle may be fitted with a propulsion means. In a second embodiment the vessels may be equipped for mineral extraction, such as methane hydrates; and transport of said minerals to the surface.

5. 发明专利

GB2408538A Ground recycled tyre block for use in crash barriers and land erosion control 未知
公开(公告)号：GB2408538A
公开(公告)日：2005-06-01
申请号：GB0406573
申请日：2004-03-24
申请人： HOLMES IAN
发明人： HOLMES IAN
IPC分类号： E01F15/14 , E02B3/14 , E02B3/06 , E01F15/04
摘要： A block for use in crash barriers, land erosion control and sea platforms is formed from chips of ground down tyres glued together. The blocks are formed with structure support, holes so that they can be assembled into a structure. The structure may be formed from blocks of the same material but containing rubber that has been ground down differently.

6. 发明专利

AT362910T 未知
公开(公告)号：AT362910T
公开(公告)日：2007-06-15
申请号：AT04739544
申请日：2004-06-01
申请人： GLAXO GROUP LTD
发明人： GAINES SIMON , HOLMES IAN , WATSON STEPHEN
IPC分类号： C07C59/48 , C07C17/16 , C07C59/52 , C07C59/54 , C07C59/56 , C07C59/58 , C07C59/68 , C07C59/86 , C07C59/90 , C07C205/56 , C07C233/33 , C07C233/54 , C07C255/57 , C07C323/62 , C07D277/04 , C07D307/91
摘要： Compounds of formula (I): wherein: Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents O, S, NR 5 or CR 6 R 7 ; Y represents CHOH, CHSH, NOR 8 , CNR 8 or CNOR 8 ; Z represents a bond, CR 10 R 11 , O, S, SO, SO 2 , NR 10 , OCR 10 R 11 , CR 10 R 11 O or Z, R 4 and Q together form an optionally substituted fused tricyclic group; R 1 , R 1' , R 3 and R 3' each independently represents H, C 1-6 alkyl or C 1-4 alkylaryl; R 2 represents CO 2 R 8 , CONR 5 OR 9 or NR 5 COR 9 ; R 4 represents optionally substituted 5- or 6-membered aryl or heteroaryl; R 5 represents H or C 1-3 alkyl; R 6 and R 7 each independently represents H, C 1-3 alkyl or halo; R 8 represents H or C 1-2 alkyl; R 9 represents H or C 1-3 alkyl; R 10 and R 11 each independently represents H, C 1-6 alkyl or C 1-4 alkylaryl; and physiologically functional derivatives thereof, processes for their preparation, pharmaceutical formulations containing them and their use as inhibitors of matrix metalloproteinase enzymes (MMPs) are described.

7. 发明专利

AT413384T 未知
公开(公告)号：AT413384T
公开(公告)日：2008-11-15
申请号：AT04765231
申请日：2004-09-10
申请人： GLAXO GROUP LTD
发明人： GAINES SIMON , HOLMES IAN , MARTIN STEPHEN , WATSON STEPHEN
IPC分类号： C07D209/48 , A61K31/4035 , A61K31/505 , A61K31/506 , A61P29/00 , C07D239/54 , C07D403/10 , C07D405/10
摘要： Compounds of Formula (I): Wherein: A represents bond, C 1-6 alkyl or CH=CH-C 1-4 alkyl; B represents bond, O, S, SO, SO 2 , CO, CR 7 R 8 , CO 2 R 14 , CONR 14 R 15 , N(COR 14 )(COR 15 ), N(SO 2 R 14 )(COR 15 ) or NR 14 R 15 ; D represents bond, or C 1-6 alkyl; E represents substituted aryl or substituted or unsubstituted heteroaryl; Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents O, S, SO, SO 2 , CO, CNR 5 , CNOR 5 , CNNR 5 R 6 , NR 11 or CR 7 R 8 ; Y represents CR 5 OR 11 , CR 5 SR 11 , NOR 5 , CR 5 NR 6 R 11 , SO, SO 2 , CO, CNR 5 , CNOR 5 or CS; R 1 and R 1' each independently represents H, C 1-6 alkyl or C 1-4 alkylaryl; R 2 represents CO 2 R 12 , CH 2 OR 12 or CONR 12 R 13 , CONR 12 OR 13 , NR 12 COR 13 , SR 12 , PO(OH) 2 , PONHR 12 or SONHR 12 ; R 3 represents H, C 1-6 alkyl or C 1-4 alkylaryl; R 4 represents optionally substituted aryl or heteroaryl; Z represents a bond, CH 2 , O, S, SO, SO 2 , NR 5 , OCR 5 R 6 , CR 9 R 10 O or Z, R 4 and Q together form an optionally substituted fused tricyclic group; R 5 and R 6 each independently represent H, C 1-6 alkyl or C 1-4 alkylaryl; R 7 and R 8 each independently represent H, halo, C 1-6 alkyl or C 1-4 alkylaryl; R 9 and R 10 each independently represents H, C 1-6 alkyl optionally substituted by halo, cyano, OR 11 or NR 6 R 11 , C 1-4 alkylaryl optionally substituted by halo, cyano, OR11 or NR 6 R 11 , OR 11 or, together with the N to which they are attached, R 9 and R 10 form a heterocyclic group: R 11 represents H, C 1-6 alkyl, C 1-4 alkylaryl or COR 5 ; R 12 and R 13 each independently represent H, C 1-3 alkyl, C 1-3 alkylaryl or C 1-3 alkylheteroaryl or, together with the functionality to which they are attached, R 12 and R 13 form a heterocyclic group: R 14 and R 15 each independently represent H, C 1-6 alkyl, C 1-4 alkylaryl or C 1-4 alkylheteroaryl or together with the functionality to which they are attached R 14 and R 15 form a heterocyclic or fused heterocyclic group: and physiologically functional derivatives thereof, processes for their preparation, pharmaceutical formulations containing them and their use as inhibitors of matrix metallproteinase enzymes (MMPs) are described.

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