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1. 发明申请

WO2009137717A1 NOVEL NITROSO COMPOUNDS AS NITROXYL DONORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：新型硝基化合物作为硝基衍生物及其使用方法
公开(公告)号：WO2009137717A1
公开(公告)日：2009-11-12
申请号：PCT/US2009/043203
申请日：2009-05-07
申请人： CARDIOXYL PHARMACEUTICALS INC. , FROST, Lisa, Marie , COURTNEY, Stephen, Martin , BROOKFIELD, Frederick, Arthur , KALISH, Vincent, J.
发明人： FROST, Lisa, Marie , COURTNEY, Stephen, Martin , BROOKFIELD, Frederick, Arthur , KALISH, Vincent, J.
IPC分类号： A61K31/535
CPC分类号： C07C207/00 , C07C207/04 , C07C255/19 , C07D211/44 , C07D211/58 , C07D309/10 , C07D309/14 , C07D333/42 , C07D405/12 , C07D405/14 , C07D407/12 , C07D451/10 , C07F9/117 , C07F9/585 , C07F9/595
摘要： The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.
摘要翻译：本发明涉及在生理条件下给予硝酰基（HNO）的羟基亚硝基化合物的羧酸和磷酸酯的亚硝基衍生物。本发明的化合物和组合物可用于治疗和/或预防对硝酰病毒治疗（包括心力衰竭，局部缺血/再灌注损伤和癌症）有反应的疾病或病症的发作和/或发展。

2. 发明申请

WO2009042970A1 N-HYDROXYLSULFONAMIDE DERIVATIVES AS NEW PHYSIOLOGICALLY USEFUL NITROXYL DONORS 审中-公开
标题翻译： N-羟基磺酰胺衍生物作为新生物学上有用的硝基衍生物
公开(公告)号：WO2009042970A1
公开(公告)日：2009-04-02
申请号：PCT/US2008/078024
申请日：2008-09-26
申请人： JOHNS HOPKINS UNIVERSITY , CARDIOXYL PHARMACEUTICALS, INC. , TOSCANO, John, P. , BROOKFIELD, Frederick, Arthur , COHEN, Andrew, D. , COURTNEY, Stephen, Martin , FROST, Lisa, Marie , KALISH, Vincent, Jacob
发明人： TOSCANO, John, P. , BROOKFIELD, Frederick, Arthur , COHEN, Andrew, D. , COURTNEY, Stephen, Martin , FROST, Lisa, Marie , KALISH, Vincent, Jacob
IPC分类号： C07C311/48 , C07D333/34 , C07D295/192 , A61K31/18 , A61K31/192 , A61K31/235 , A61K31/5377 , A61P9/04 , A61P9/10 , C07D333/38
CPC分类号： C07C317/48 , C07C311/48 , C07D295/155 , C07D295/16 , C07D295/192 , C07D295/26 , C07D333/26 , C07D333/36 , C07D333/38
摘要： The invention relates to N -hydroxylsulfonamide derivatives for formula (I), (II) or (III), in which the variables are as defined in the claims, that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. N -hydroxylsulfonamide derivatives release HNO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of the functional groups on the N -hydroxylsulfonamide derivatives.
摘要翻译：本发明涉及式（I），（II）或（III）的N-羟基磺酰胺衍生物，其中变量如权利要求中所定义，在生理条件下提供硝酰基（HNO），并且可用于治疗和/或防止对硝酰病治疗有反应的疾病或病症的发生和/或发展，包括心力衰竭和缺血/再灌注损伤。 N-羟基磺酰胺衍生物在生理条件下以控制速率释放HNO，并且通过改变N-羟基磺酰胺衍生物上的官能团的性质和位置来调节HNO释放速率。

3. 发明申请

WO2007109175A1 N-HYDROXYLSULFONAMIDE DERIVATIVES AS NEW PHYSIOLOGICALLY USEFUL NITROXYL DONORS 审中-公开
标题翻译： N-羟基磺酰胺衍生物作为新生物学上有用的硝基衍生物
公开(公告)号：WO2007109175A1
公开(公告)日：2007-09-27
申请号：PCT/US2007/006710
申请日：2007-03-16
申请人： JOHN HOPKINS UNIVERSITY SCHOOL OF MEDICINE , TOSCANO, John, P. , BROOKFIELD, Frederick, Arthur , COHEN, Andrew, D. , COURTNEY, Stephen, Martin , FROST, Lisa, Marie , KALISH, Vincent, Jacob
发明人： TOSCANO, John, P. , BROOKFIELD, Frederick, Arthur , COHEN, Andrew, D. , COURTNEY, Stephen, Martin , FROST, Lisa, Marie , KALISH, Vincent, Jacob
IPC分类号： A61K31/18 , A61P9/04 , C07C311/48 , C07C317/14 , C07C323/67 , C07D207/36 , C07D213/71 , C07D213/74 , C07D215/28 , C07D215/36 , C07D231/18 , C07D233/84 , C07D239/38 , C07D241/18 , C07D249/12
CPC分类号： C07C311/48 , C07C317/14 , C07C323/67 , C07D213/74 , C07D231/18 , C07D261/10 , C07D263/58 , C07D285/125 , C07D295/096 , C07D307/82 , C07D309/12 , C07D317/14 , C07D333/34 , C07D333/62
摘要： The invention relates to N -hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N -hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N -hydroxysulfonamide derivatives.
摘要翻译：本发明涉及在生理条件下给予硝酰基（HNO）的N-羟基磺酰胺衍生物，并且可用于治疗和/或预防对硝酰病治疗有反应的疾病或病症的发作和/或发展，包括心力衰竭和缺血/再灌注伤害。新的N-羟基磺酰胺衍生物在生理条件下以受控的速率释放NHO，并且通过改变N-羟基磺酰胺衍生物上官能团的性质和位置来调节HNO释放速率。

4. 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。

5. 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。

6. 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。

7. 发明申请

WO2005040112A1 COMPOUNDS WITH PGD2 ANTAGONIST ACTIVITY 审中-公开
标题翻译：具有PGD2拮抗剂活性的化合物
公开(公告)号：WO2005040112A1
公开(公告)日：2005-05-06
申请号：PCT/GB2004/004337
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： C07D209/18
CPC分类号： C07D403/12 , C07D209/18
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), -C 1 -C 6 alkyl(C 3 -C 7 cycloalkyl), -CON(R 9 ) 2 , -SOR 9 , -S0 2 R 9 . -S0 2 N(R 9 ) 2 , -N(R 9 ) 2 , -NR 9 OR 9 , -C0 2 R 9 , COR 9 , -SR 9 , -OH, -N0 2 or -CN; each R 9 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 form a C 3 -C 7 cycloalkyl. group; R 7 is hydrogen or C 1 -C 6 alkyl; R 8 is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl or an aromatic moiety, any of which may optionally be substituted with one or more substituents selected from halo, -SOR 13 -S0 2 R 13 , -R 14 , -OR 14 , -CON(R 14 )2 -SOR 14 , -S0 2 R 14 , -S0 2 N(R 14 ) -SO 2 N(R 14 ) 2 , -N(R 14 )2, NR 14 COR 14 , -CO 2 R 14 , COR 14 , -SR 14 , -N0 2 or -CN; wherein R 13 is a 5 to 7 membered heterocyclic ring; and each R 14 is independently hydrogen, alkyl or aryl, the aryl being optionally substituted by -R 9 , -OR 9 , -CON(R 9 ) 2 , -SOR 9 -S0 2 R 9 , -S0 2 N(R 9 ) 2 , -N(R 9 ) 2 , NR9COR 9 , -C0 2 R 9 , -COR 9 , -SR 9 , halo, -N0 2 or -CN; wherein R 9 is as defined above; provided that when R 1 , R 3 and R 4 are hydrogen and R 2 is hydrogen, halogen or -O(C 1 -C 6 )alkyl, R 8 is not unsubstituted phenyl or phenyl substituted by halo, C 1 -C 6 alkyl, -O(C 1 -C 6 )alkyl, -S(C 1 -C 6 )alkyl or -CO(C 1 -C 6 )alkyl; or pharmaceutically acceptable salts, hydrates, solvates, compexes or prodrugs therof are useful in the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
摘要翻译：通式（I）的化合物; 其中R 1，R 2，R 3和R 4独立地是氢，卤素，-C 1 -C 6烷基，-O（C 1 -C 6烷基），-C 1 -C 6烷基（C 3 -C 7 环烷基），-CON（R 9）2，-SOR 9，-SO 2 R 9。 -SO 2 N（R 9）2，-N（R 9）2，-NR 9 OR 9，-CO 2 R 9，COR 9，-SR 9，-OH， -NO 2或-CN; 每个R 9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，或与它们所连接的碳原子一起形成C 3 -C 7环烷基。组; R 7是氢或C 1 -C 6烷基; R 8是C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基或芳族部分，其中任何一个可任选地被一个或多个选自卤素，-SOR 13 -SO 2 R 13，，-R 14，-OR 14，-CON（R 14）2 -SOR 14，-SO 2 R 14，-SO 2 N（R 14）-SO 2 N（R 14）2，-N（R COR 14，-C 14 R 14，COR 14，-SR 14，-NO 2或-CN; 其中R 13为5至7元杂环; 并且每个R 14独立地为氢，烷基或芳基，芳基任选被-R 9，-OR 9，-CON（R 9）2，-SOR 9 - （R 9）2，-N（R 9）2，NR 9 COR 9，-CO 2 R 9，-COR 9，-SR 9，卤素，-NO 2 或-CN; 其中R 9如上所定义; 条件是当R 1，R 3和R 4为氢且R 2为氢，卤素或-O（C 1 -C 6）烷基时，R 8为未取代的苯基或被卤素，C 1 -C 6烷基，-O（C 1 -C 6）烷基，-S（C 1 -C 6）烷基或-CO（C 1 -C 6）烷基; 或其药学上可接受的盐，水合物，溶剂合物，混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。

8. 发明申请

WO2011048111A1 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2011048111A1
公开(公告)日：2011-04-28
申请号：PCT/EP2010/065746
申请日：2010-10-19
申请人： RESPIVERT LIMITED , KING-UNDERWOOD, John , ITO, Kazuhiro , MURRAY, Peter, John , HARDY, George , BROOKFIELD, Frederick, Arthur , BROWN, Christopher, John
发明人： KING-UNDERWOOD, John , ITO, Kazuhiro , MURRAY, Peter, John , HARDY, George , BROOKFIELD, Frederick, Arthur , BROWN, Christopher, John
IPC分类号： C07D487/04 , A61K31/519 , A61P11/00 , A61P11/06 , A61P17/00 , A61P19/02 , A61P35/00
CPC分类号： C07D487/04 , A61K31/4965
摘要： The present invention relates to compounds of formula (I) and to compositions comprising the same and to the use of the compounds and their 10 compositions in treatment, for example in the treatment of inflammatory diseases, in particular respiratory inflammatory disease. The invention also extends to methods of making said compounds.
摘要翻译：本发明涉及式（I）化合物和包含其的组合物，以及该化合物及其10种组合物在治疗中的用途，例如治疗炎性疾病，特别是呼吸道炎性疾病。本发明还涉及制备所述化合物的方法。

9. 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。

10. 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。

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