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11. 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。

12. 发明申请

WO2011071951A3 N-ACYLOXYSULFONAMIDE AND N-HYDROXY-N-ACYLSULFONAMIDE DERIVATIVES 审中-公开
标题翻译： N-羟基甲酰胺和N-羟基-N-亚磺酰胺衍生物
公开(公告)号：WO2011071951A3
公开(公告)日：2012-03-29
申请号：PCT/US2010059335
申请日：2010-12-07
申请人： UNIV JOHNS HOPKINS , CARDIOXYL PHARMACEUTICALS INC , TOSCANO JOHN P , SUTTON ART , KALISH VINCENT J , BROOKFIELD FREDERICK ARTHUR , COURTNEY STEPHEN MARTIN , FROST LISA MARIE
发明人： TOSCANO JOHN P , SUTTON ART , KALISH VINCENT J , BROOKFIELD FREDERICK ARTHUR , COURTNEY STEPHEN MARTIN , FROST LISA MARIE
IPC分类号： C07C311/48 , A61K31/18 , A61P9/04 , C07C317/14 , C07D265/00
CPC分类号： C07C311/48 , C07C311/51 , C07C317/14 , C07C317/32 , C07C2601/14 , C07D207/06 , C07D207/16 , C07D209/48 , C07D211/46 , C07D211/58 , C07D211/62 , C07D213/40 , C07D213/46 , C07D213/59 , C07D213/71 , C07D213/74 , C07D233/38 , C07D241/04 , C07D241/08 , C07D295/192 , C07D295/195 , C07D295/205 , C07D307/82 , C07D309/12 , C07D317/30 , C07D333/34 , C07D401/04 , C07D413/04
摘要： The invention provides certain N-acyloxysulfonamide and N-hydroxy-N-acylsulfonamide derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
摘要翻译：本发明提供某些N-酰氧基亚磺酰胺和N-羟基-N-酰基磺酰胺衍生物化合物，包含这些化合物的药物组合物和试剂盒，以及使用这些化合物或药物组合物的方法。特别地，本发明提供了使用这些化合物或药物组合物治疗，预防或延缓疾病或病症发作和/或发展的方法。在一些实施方案中，疾病或病症选自心血管疾病，缺血，再灌注损伤，癌性疾病，肺动脉高压和对硝酰基治疗有反应的病症。

13. 发明申请

WO2011071947A3 BIS-ACYLATED HYDROXYLAMINE DERIVATIVES 审中-公开
标题翻译：二异氰酸酯衍生物
公开(公告)号：WO2011071947A3
公开(公告)日：2012-03-29
申请号：PCT/US2010059331
申请日：2010-12-07
申请人： UNIV JOHNS HOPKINS , CARDIOXYL PHARMACEUTICALS INC , TOSCANO JOHN P , SUTTON ART , KALISH VINCENT J , BROOKFIELD FREDERICK ARTHUR , COURTNEY STEPHEN MARTIN , FROST LISA MARIE
发明人： TOSCANO JOHN P , SUTTON ART , KALISH VINCENT J , BROOKFIELD FREDERICK ARTHUR , COURTNEY STEPHEN MARTIN , FROST LISA MARIE
IPC分类号： C07C311/48 , A61K31/18 , A61K31/67 , A61P9/04 , C07C233/66 , C07C233/92
CPC分类号： C07D333/34 , C07C233/01 , C07C233/64 , C07C259/06 , C07C259/10 , C07C271/08 , C07C311/51 , C07C311/53 , C07C317/14 , C07C317/28 , C07C317/32 , C07C2601/08 , C07C2601/14 , C07D207/16 , C07D213/40 , C07D213/71 , C07D295/205 , C07D295/215 , C07D307/82 , C07D309/12
摘要： The invention provides certain bis-acylated hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
摘要翻译：本发明提供某些双酰化羟胺衍生物化合物，包含这些化合物的药物组合物和试剂盒，以及使用这些化合物或药物组合物的方法。特别地，本发明提供了使用这些化合物或药物组合物治疗，预防或延缓疾病或病症发作和/或发展的方法。在一些实施方案中，疾病或病症选自心血管疾病，缺血，再灌注损伤，癌性疾病，肺动脉高压和对硝酰基治疗有反应的病症。

14. 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。

15. 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。

16. 发明申请

WO2005063747A1 PYRROLO[2,3-b] PYRIDINE DERIVATIVES ACTIVE AS KINASE INHIBITORS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITION 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：WO2005063747A1
公开(公告)日：2005-07-14
申请号：PCT/EP2004/014676
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 , BROOKFIELD, Frederick, Arthur , TRIGG, William, John , BOYD, Edward, Andrew , LARARD, Jonathan, Anthony , TESEI, Dania
发明人： SALOM, Barbara , D'ANELLO, Matteo , BRASCA, Maria, Gabriella , GIORDANO, Patrizia , MARTINA, Katia , BROOKFIELD, Frederick, Arthur , TRIGG, William, John , BOYD, Edward, Andrew , LARARD, Jonathan, Anthony , TESEI, Dania
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 neurodegenrative 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引起的和/或与其相关的疾病，例如癌症，细胞增殖性疾病，阿尔茨海默病，病毒感染，自身免疫性疾病和神经发生性疾病; 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。

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