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1. 发明申请

WO2005097100A2 ANTIBACTERIAL AGENTS 审中-公开
标题翻译：抗菌剂
公开(公告)号：WO2005097100A2
公开(公告)日：2005-10-20
申请号：PCT/GB2005/001295
申请日：2005-04-01
申请人： PROLYSIS LTD. , BOYD, Edward, Andrew , HATCHER, Stuart , CZAPLEWSKI, Lloyd , ERRINGTON, Jeffrey , BROWN, David
发明人： BOYD, Edward, Andrew , HATCHER, Stuart , CZAPLEWSKI, Lloyd , ERRINGTON, Jeffrey , BROWN, David
IPC分类号： A61K31/197
CPC分类号： C07D333/32 , A61K31/197 , A61K31/341 , C07C229/14 , C07D257/04 , C07D277/28 , C07D307/52 , C07D317/58 , C07D333/20
摘要： Compounds of formula (I) have antibacterial activity: Formula (I), wherein Z is a carboxyl radical HOC (=O)-, a carboxyl ester radical, or a carboxyl isostere radical; ring A is an optionally substituted monocyclic aryl, heteroaryl or cycloalkyl radical; ring B is a monocyclic aryl, heteroaryl or cycloalkyl radical; X is -O-, -S-, -(CH 2 )-, -(CH=CH)-, -C (=C? 2 )-, -CH (CH 3 )-, -C(=O)-, -C(=S)-, -C(=NR 1 )-, or-NR 1 -wherein R 1 is hydrogen or C 1 -C 6 alkyl; R is (i) an optionally substituted monocyclic aryl, heteroaryl, or cycloalkyl radical, or an optionally substituted cycloalkyl(C 1 -C 6 alkyl)- radical in which the cycloalkyl moiety is monocyclic, or (ii) an optionally substituted C 1 -C 6 alkyl radical which may be interrupted by -O-, -S-, or -NR 2 -wherein R 2 hydrogen or is C 1 -C 6 alkyl.
摘要翻译：式（I）化合物具有抗菌活性：式（I）其中Z为羧基HOC（= O） - ，羧基酯基或羧基等价基; 环A是任选取代的单环芳基，杂芳基或环烷基; 环B是单环芳基，杂芳基或环烷基; X是-O - ， - S - ， - （CH 2） - ， - （CH = CH） - ， - C（= C 2） - ， - CH（CH 3） C（= S） - ， - C（= NR 1） - 或-NR 1 - ，其中R 1是氢或C 1 -C 6烷基; R是（i）任选取代的单环芳基，杂芳基或环烷基，或其中环烷基部分是单环的任选取代的环烷基（C 1 -C 6烷基） - 基团，或（ii）任选取代的C 1 -C 6烷基其可以被-O - ， - S - 或-NR 2 - 中间体，其中R 2氢或是C 1 -C 6烷基。

2. 发明申请

WO2007017687A2 EP2 RECEPTOR AGONISTS 审中-公开
标题翻译： EP2受体激素
公开(公告)号：WO2007017687A2
公开(公告)日：2007-02-15
申请号：PCT/GB2006/002979
申请日：2006-08-09
申请人： ASTERAND UK LIMITED , OXFORD, Alexander, William , DAVIS, Richard, Jon , COLEMAN, Robert, Alexander , CLARK, Kenneth, Lyle , CLARK, David, Edward , HARRIS, Neil, Victor , FENTON, Garry , HYND, George , STUTTLE, Keith, Alfred, James , SUTTON, Jonathan, Mark , ASHTON, Mark, Richard , BOYD, Edward, Andrew , BRUNTON, Shirley, Ann
发明人： OXFORD, Alexander, William , DAVIS, Richard, Jon , COLEMAN, Robert, Alexander , CLARK, Kenneth, Lyle , CLARK, David, Edward , HARRIS, Neil, Victor , FENTON, Garry , HYND, George , STUTTLE, Keith, Alfred, James , SUTTON, Jonathan, Mark , ASHTON, Mark, Richard , BOYD, Edward, Andrew , BRUNTON, Shirley, Ann
CPC分类号： C07C233/81 , C07C257/18 , C07D213/70 , C07D263/57 , C07D307/42 , C07D307/54 , C07D307/68 , C07D307/91 , C07D405/12
摘要： A compound of formula (III): or a salt, solvate and chemically protected form thereof, wherein: R 5 is an optionally substituted C 5-20 aryl or C 4-20 alkyl group; L' is a single bond, -O- or -C(=O)-; A is selected from the group consisting of: formulae (i) (ii) (iii) wherein X and Y are selected from the group consisiting of: O and CR 3 ; S and CR 3 ; NH and CR 3 ; NH and N; O and N; S and N; N and S; and N and O, and where the dotted lines indicate a double bond in the appropriate location, and where Q is either N or CH; D is selected from: formulae (i) (ii) (iii) (iv) (v) (vi) (vii) (viii) (ix) B is selected from the group consisting of: formulae (A) (B) where R P6 is selected from fluoro and chloro; and R 2 is either: (i) -CO 2 H; (ii) -CONH 2 ; (iii) -CH 2 -OH; or (iv) tetrazol-5-yl.
摘要翻译：式（III）化合物或其盐，溶剂合物和化学保护形式，其中：R 5是任选取代的C 5-20-20芳基或C _{4-20 烷基; L'是单键，-O-或-C（= O） - ; A选自由式（ⅰ）（ⅱ）（ⅲ）组成的组：其中X和Y选自：O和CR 3; S和CR 3; NH和CR 3; NH和N; O和N; S和N; N和S; 和N和O，并且其中虚线表示适当位置的双键，并且其中Q为N或CH; D选自：式（i）（ii）（iii）（iv）（v）（vi）（vii）（viii）（ix）B选自：式（A）（B）其中 R 6 P 6选自氟和氯; 和R 2是：（i）-CO 2 H; （ii）-CONH 2; （iii）-CH 2 -OH; 或（iv）四唑-5-基。}

3. 发明申请

WO2005121141A1 PYRROLOPYRIDINE DERIVATIVES AND USE THEREOF FOR TREATING DISEASES MEDIATED BY PROSTAGLANDIN D2 (PGD2) 审中-公开
标题翻译：吡咯啉衍生物及其用于治疗PROSTAGLANDIN D2（PGD2）介导的疾病的用途
公开(公告)号：WO2005121141A1
公开(公告)日：2005-12-22
申请号：PCT/GB2005/002242
申请日：2005-06-07
申请人： OXAGEN LIMITED , ARMER, Richard, Edward , BOYD, Edward, Andrew , BROOKFIELD, Frederick, Arthur
发明人： ARMER, Richard, Edward , BOYD, Edward, Andrew , BROOKFIELD, Frederick, Arthur
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Compounds of formula (Ia) or (Ib): or pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs thereof are useful in the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
摘要翻译：式（Ia）或（Ib）化合物或其药学上可接受的盐，水合物，溶剂化物，复合物或前药可用于治疗过敏性疾病如哮喘，过敏性鼻炎和特应性皮炎。

4. 发明申请

WO2005063746A1 PYRROLO[2,3-b]PYRIDINE DERIVATIVES ACTIVE AS KINASE INHIBITORS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM 审中-公开
标题翻译：作为激酶抑制剂活性的吡咯并[2,3-b]吡啶衍生物，其制备方法和包含它们的药物组合物
公开(公告)号：WO2005063746A1
公开(公告)日：2005-07-14
申请号：PCT/EP2004/014674
申请日：2004-12-23
申请人： PHARMACIA ITALIA S.p.A. , SALOM, Barbara , D'ANELLO, Matteo , BRASCA, Maria, Gabriella , GIORDANO, Patrizia , MARTINA, Katia , ANGELUCCI, Francesco , BROOKFIELD, Frederick, Arthur , TRIGG, William, John , BOYD, Edward, Andrew , LARARD, Jonathan, Anthony
发明人： SALOM, Barbara , D'ANELLO, Matteo , BRASCA, Maria, Gabriella , GIORDANO, Patrizia , MARTINA, Katia , ANGELUCCI, Francesco , BROOKFIELD, Frederick, Arthur , TRIGG, William, John , BOYD, Edward, Andrew , LARARD, Jonathan, Anthony
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Compounds which are pyrrolo[2,3-b]pyridine derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases and neurodegenerative disorders; also disclosed is a process under SPS conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
摘要翻译：公开了吡咯并[2,3-b]吡啶衍生物或其药学上可接受的盐的化合物，其制备方法和包含它们的药物组合物; 这些化合物可用于治疗由改变的蛋白激酶活性如癌症，细胞增殖性疾病，阿尔茨海默病，病毒感染，自身免疫疾病和神经变性疾病引起的和/或与其相关的疾病。还公开了在SPS条件下制备本发明化合物的方法和包含其中多个化合物的化学文库。

5. 发明申请

WO2005044260A1 USE OF CRTH2 ANTAGONIST COMPOUNDS IN THERAPY 审中-公开
标题翻译： CRTH2拮抗剂化合物在治疗中的应用
公开(公告)号：WO2005044260A1
公开(公告)日：2005-05-19
申请号：PCT/GB2004/004417
申请日：2004-10-19
申请人： OXAGEN LIMITED , MIDDLEMISS, David , ASHTON, Mark, Richard , BOYD, Edward, Andrew , BROOKFIELD, Frederick, Arthur
发明人： MIDDLEMISS, David , ASHTON, Mark, Richard , BOYD, Edward, Andrew , BROOKFIELD, Frederick, Arthur
IPC分类号： A61K31/404
CPC分类号： C07D209/12 , A61K31/404 , A61K31/426 , A61K31/428 , A61K31/4709 , A61K31/498 , C07D209/08 , C07D209/10 , C07D401/06 , C07D403/06 , C07D417/06
摘要： Compounds of general formula (I) wherein R 1 , R 2 , R 3 and R 4 are independently hydrogen, halo,C 1 -C 6 alkyl, -O(C 1 -C 6 alkyl), -CON(R 11 ) 2 , -SO 11 , -SO 2 R 11 , -SO 2 N(R 11 ) 2 , -N(R 11 ) 2 , -NR 11 COR 11 , -CO 2 R 11 , -COR 11 , -SR 11 , -OH, -NO 2 or -CN; each R 11 is independently hydrogen or C 1 -C 6 alkyl; R 5 and R 6 are each independently hydrogen, or C 1 -C 6 alkyl or together with the carbon atom to which they are attached forrn a C 3 -C 7 cycloalkyl group; R 7 is hydrogen or C 1 -C 6 alkyl; R 8 is an aromatic moiety optionally substituted with one or more substituents selected from halo, C 1 -C 6 alkyl, -O(C 1 -C 6 )alkyl, -CON(R 11 ) 2 , -SOR 11 , -SO 2 R 11 , -SO 2 N(R 11 ) 2 , -N(R 11 ) 2 , -NR 11 COR 11 , -CO 2 R 11 , -COR 11 , -SR 11 , -OH, -NO 2 or -CN; wherein R 11 is as defined above; R 9 is hydrogen, or C 1 -C 6 alkyl; provided that: R 8 is not phenyl substituted with -COOH; when any two of R 1 , R 2 , R 3 and R 4 are hydrogen, neither of the other two of R 1 , R 2 , R 3 and R 4 is C 3 -C 6 alkyl; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in the preparation of pharmaceuticals for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
摘要翻译：其中R 1，R 2，R 3和R 4的通式（I）的化合物独立地是氢，卤素，C 1 -C 6烷基，-O（C 1 -C 6烷基），-CON（ R 11）2，-SO 11，-SO 2 R 11，-SO 2 N（R 11）2，-N（R 11）2，-NR 11 COR 11， CO 2 R 11，-COR 11，-SR 11，-OH，-NO 2或-CN; 每个R 11独立地是氢或C 1 -C 6烷基; R 5和R 6各自独立地为氢或C 1 -C 6烷基或与它们连接的碳原子一起形成C 3 -C 7环烷基; R 7是氢或C 1 -C 6烷基; R 8是任选被一个或多个选自卤素，C 1 -C 6烷基，-O（C 1 -C 6）烷基，-CON（R 11）2，-SOR 11 - ， - SO 2 R 11，-SO 2 N（R 11）2，-N（R 11）2，-NR 11 COR 11，-CO 2 R 11，-COR 11， 11，-OH，-NO 2或-CN; 其中R 11如上所定义; R 9是氢或C 1 -C 6烷基; 条件是：R 8不是被-COOH取代的苯基; 当R 1，R 2，R 3和R 4中的任何两个为氢时，R 1，R 2，R 3和R 4中的另外两个 >是C 3 -C 6烷基; 其药学上可接受的盐，水合物，溶剂合物，复合物或前药可用于制备用于治疗过敏性疾病如哮喘，过敏性鼻炎和特应性皮炎的药物。

6. 发明申请

WO2003027234A2 SMALL ORGANIC MOLECULE REGULATORS OF CELL PROLIFERATION 审中-公开
标题翻译：细胞增殖的小有机分子调节剂
公开(公告)号：WO2003027234A2
公开(公告)日：2003-04-03
申请号：PCT/US2002/029522
申请日：2002-09-18
申请人： CURIS, INC. , BAXTER, Anthony, David , BOYD, Edward, Andrew , GUICHERIT, Oivin , PORTER, Jeffery , PRICE, Stephen , RUBIN, Lee, L. , STIBBARD, John, Harry, Alexander
发明人： BAXTER, Anthony, David , BOYD, Edward, Andrew , GUICHERIT, Oivin , PORTER, Jeffery , PRICE, Stephen , RUBIN, Lee, L. , STIBBARD, John, Harry, Alexander
IPC分类号： C12N
CPC分类号： A61K31/422 , A61K31/381 , A61K31/44 , A61K31/4436 , A61K31/50 , A61K31/517 , C07D333/70 , C07D409/12 , C07D409/14
摘要： The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a hedgehog agonist, such as the compounds depicted in Figures 32 and 33. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal ptc pathway or agonizing smoothened or hedgehog activity.
摘要翻译：本发明提供用于调节细胞或组织中增殖或分化的可用方法和试剂，包括使细胞与刺猬激动剂例如图32和33所示的化合物接触。在某些实施方案中，可以使用所述方法和试剂纠正或抑制异常或不想要的生长状态，例如通过拮抗正常的ptc途径或激动平滑或刺猬活动。

7. 发明申请

WO2006095183A1 1-ACETIC ACID-INDOLE DERIVATIVES WITH PGD2 ANTAGONIST ACTIVITY 审中-公开
标题翻译：具有PGD2拮抗剂活性的1-乙酸内酯衍生物
公开(公告)号：WO2006095183A1
公开(公告)日：2006-09-14
申请号：PCT/GB2006/000851
申请日：2006-03-10
申请人： OXAGEN LIMITED , ARMER, Richard, Edward , BOYD, Edward, Andrew , HAY, Philip, Andrew
发明人： ARMER, Richard, Edward , BOYD, Edward, Andrew , HAY, Philip, Andrew
IPC分类号： C07D209/30 , C07D209/42 , A61K31/405 , A61P11/00 , A61P37/00
CPC分类号： C07D403/06
摘要： Compounds of general formula: (I) wherein R 1 is halo or cyano; R 2 is C 1 -C 4 alkyl; and R 3 is phenyl substituted with one or more substituents chosen from C 1 -C 6 alkyl, halo or -SO 2 (C 1 -C 6 alkyl); or a pharmaceutically acceptable salt, hydrate, solvate, complex or prodrug thereof; are useful in the treatment of diseases and conditions mediated by the action of PGD 2 at the CRTH2 receptor.
摘要翻译：通式（I）的化合物，其中R 1是卤素或氰基; R 2是C 1 -C 4烷基; R 2是C 1 -C 4烷基; R 3是被一个或多个选自C 1 -C 6烷基，卤素或-SO 2的取代基取代的苯基，（C 1 -C 6烷基）; 或其药学上可接受的盐，水合物，溶剂化物，复合物或前药; 可用于治疗由CRD2受体上的PGD 2 N 2的作用介导的疾病和病症。

8. 发明申请

WO2006092579A1 MICROCRYSTALLINE ( 5-FLUORO-2-METHYL-3-QUINOLIN-2-YLMETHYL-INDOL-1-YL) ACETIC ACID 审中-公开
标题翻译：微晶（5-氟-2-甲基-3-喹啉-2-基甲基）吲哚-1-基）乙酸
公开(公告)号：WO2006092579A1
公开(公告)日：2006-09-08
申请号：PCT/GB2006/000704
申请日：2006-03-01
申请人： OXAGEN LIMITED , BOYD, Edward, Andrew , BROOKFIELD, Frederick, Arthur , BRENNAN, Christopher, James , PALMER, Christopher, Francis , PEARCEY, Leigh, Andre , LOVELL, James, Matthew
发明人： BOYD, Edward, Andrew , BROOKFIELD, Frederick, Arthur , BRENNAN, Christopher, James , PALMER, Christopher, Francis , PEARCEY, Leigh, Andre , LOVELL, James, Matthew
IPC分类号： C07D401/06 , A61K31/4709 , A61P11/06
CPC分类号： C07D401/06
摘要： The invention relates to a microcrystalline form of a compound which is an inhibitor of PGD 2 at the CRTH2 receptor. The microcrystalline form is obtained from a simple chemical reaction without the need for a milling process.
摘要翻译：本发明涉及一种化合物的微晶形式，其是在CRTH2受体上的PGD 2 N 2抑制剂。微晶形式由简单的化学反应获得，而不需要研磨过程。

9. 发明申请

WO2005040114A1 COMPOUNDS HAVING CRTH2 ANTAGONIST ACTIVITY 审中-公开
标题翻译：具有CRTH2拮抗剂活性的化合物
公开(公告)号：WO2005040114A1
公开(公告)日：2005-05-06
申请号：PCT/GB2004/004336
申请日：2004-10-13
申请人： OXAGEN LIMITED , MIDDLEMISS, David , ASHTON, Mark, Richard , BOYD, Edward, Andrew , BROOKFIELD, Frederick, Arthur , ARMER, Richard, Edward
发明人： MIDDLEMISS, David , ASHTON, Mark, Richard , BOYD, Edward, Andrew , BROOKFIELD, Frederick, Arthur , ARMER, Richard, Edward
IPC分类号： C07D209/30
CPC分类号： C04B35/632 , C07D209/30 , C07D401/12 , C07D403/12 , C07D417/12
摘要： Compounds of general formula (I) and their pharmaceutically acceptable salts, hydrates, solvates, complexes and prodrugs are useful in the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
摘要翻译：通式（I）化合物及其药学上可接受的盐，水合物，溶剂合物，复合物和前药可用于治疗过敏性疾病如哮喘，过敏性鼻炎和特应性皮炎。

10. 发明申请

WO2006050506A1 MEDIATORS OF HEDGEHOG SIGNALING PATHWAYS, COMPOSITIONS AND USES RELATED THERETO 审中-公开
标题翻译： HEDGEHOG信号通道的路由器，组成和使用相关的介质
公开(公告)号：WO2006050506A1
公开(公告)日：2006-05-11
申请号：PCT/US2005/040054
申请日：2005-11-03
申请人： CURIS, INC. , GUICHERIT, Oivin, M. , BOYD, Edward, Andrew , BRUNTON, Shirley, Ann , PRICE, Stephen , STIBBARD, John, Harry, Alexander , MACKINNON, Colin, H.
发明人： GUICHERIT, Oivin, M. , BOYD, Edward, Andrew , BRUNTON, Shirley, Ann , PRICE, Stephen , STIBBARD, John, Harry, Alexander , MACKINNON, Colin, H.
IPC分类号： A61K31/4184 , C07D401/10 , C07D401/14 , C07D413/10 , C07D417/10 , C07D417/14 , A61P35/00
CPC分类号： A61K31/4427 , C07D401/10 , C07D401/12 , C07D401/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/04
摘要： The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist of formula (I) in a sufficient amount to aberrant growth state, e.g ., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.
摘要翻译：本发明提供用于抑制由刺猬获得功能，功能丧失功能或平滑增益功能引起的异常生长状态的可用方法和试剂，包括使细胞与式（I）的刺猬蛋白拮抗剂在足够量的异常生长状态，例如，激发正常的ptc途径或拮抗平滑或刺猬活性。

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