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1. 发明申请

WO2010019097A1 PHARMACEUTICAL PRODUCT COMPRISING A MUSCARINIC RECEPTOR ANTAGONIST AND A SECOND ACTIVE INGREDIENT 审中-公开
标题翻译：药物产品，包括一个muscarinic受体拮抗剂和第二个有效成分
公开(公告)号：WO2010019097A1
公开(公告)日：2010-02-18
申请号：PCT/SE2009/050924
申请日：2009-08-11
申请人： ASTRAZENECA AB , ARGENTA DISCOVERY Ltd. , AVITABILE, Barbara Guiseppina , NADIN, Alan John , RAY, Nicholas Charles
发明人： AVITABILE, Barbara Guiseppina , NADIN, Alan John , RAY, Nicholas Charles
IPC分类号： A61K31/439 , A61P11/06 , A61P11/08 , C07D471/08 , A61K31/438 , A61K31/4468 , C07D261/08 , C07D271/06
CPC分类号： A61K45/06 , A61K31/438 , A61K31/439 , A61K31/4468 , A61K2300/00
摘要： The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is a selected muscarinic receptor antagonist, and a second active ingredient which is selected from a phosphodiesterase inhibitor, a modulator of chemokine receptor function, an inhibitor of kinase function, a protease inhibitor, a steroidal glucocorticoid receptor agonist, a non-steroidal glucocorticoid receptor agonist and a purinoceptor antagonist, of use in the treatment of respiratory diseases such as chronic obstructive pulmonary disease and asthma.
摘要翻译：本发明提供了药物产品，药盒或组合物，其包含作为选择的毒蕈碱性受体拮抗剂的第一活性成分和选自磷酸二酯酶抑制剂，趋化因子受体功能调节剂，激酶功能抑制剂，蛋白酶抑制剂，甾体糖皮质激素受体激动剂，非甾体糖皮质激素受体激动剂和嘌呤受体拮抗剂，用于治疗呼吸疾病如慢性阻塞性肺病和哮喘。

2. 发明申请

WO2010018352A1 HETEROCYCLIC COMPOUNDS USED IN THE TREATMENT OF DISEASES WHERE ENHANCED M3 RECEPTOR ACTIVATION IS IMPLICATED 审中-公开
标题翻译：用于治疗M3受体激活的疾病治疗中使用的杂环化合物
公开(公告)号：WO2010018352A1
公开(公告)日：2010-02-18
申请号：PCT/GB2008/002728
申请日：2008-08-12
申请人： ARGENTA DISCOVERY LIMITED , ASTRAZENECA AB , NADIN, Alan, John , OSBOURN, Susan, Elizabeth , TISSELLI, Patrizia , RAY, Nicholas, Charles
发明人： NADIN, Alan, John , OSBOURN, Susan, Elizabeth , TISSELLI, Patrizia , RAY, Nicholas, Charles
IPC分类号： C07D471/08 , A61K31/439 , A61P11/00 , C07D271/06 , C07D271/10
CPC分类号： C07D471/08 , C07D271/06 , C07D271/10
摘要： The invention provides named compounds of formula (I), pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions and their use in in the treatment of diseases where enhanced M3 receptor activation is implicated.
摘要翻译：本发明提供命名的式（I）化合物，含有它们的药物组合物，制备药物组合物的方法及其用于治疗涉及M3受体活化增强的疾病的用途。

3. 发明申请

WO2004101539A1 CYCLIC SULFONAMIDES FOR INHIBITION OF GAMMA-SECRETASE 审中-公开
标题翻译：用于抑制GAMMA-分泌酶的循环磺酰胺
公开(公告)号：WO2004101539A1
公开(公告)日：2004-11-25
申请号：PCT/GB2004/002013
申请日：2004-05-07
申请人： MERCK SHARP & DOHME LIMITED , DINNELL, Kevin , HARRISON, Timothy , NADIN, Alan, John , OWENS, Andrew, Pate , SHAW, Duncan, Edward , WILLIAMS, Brian, John
发明人： DINNELL, Kevin , HARRISON, Timothy , NADIN, Alan, John , OWENS, Andrew, Pate , SHAW, Duncan, Edward , WILLIAMS, Brian, John
IPC分类号： C07D285/16
CPC分类号： C07D279/02
摘要： Compounds of formula (I) inhibit the processing of APP by gamma-secretase, and hence are useful in the treatment or prevention of Alzheimer's disease.
摘要翻译：式（I）化合物通过γ-分泌酶抑制APP的加工，因此可用于治疗或预防阿尔茨海默氏病。

4. 发明申请

WO2004101538A1 CYCLOHEXYL SULPHONES AS GAMMA-SECRETASE INHIBITORS 审中-公开
标题翻译： CYCLOHEXYL SULPHONES作为GAMMA-SECRETASE抑制剂
公开(公告)号：WO2004101538A1
公开(公告)日：2004-11-25
申请号：PCT/GB2004/001973
申请日：2004-05-07
申请人： MERCK SHARP & DOHME LIMITED , DINNELL, Kevin , HARRISON, Timothy , GIBSON, Karl, Richard , JELLEY, Richard, Alexander , NADIN, Alan, John , OAKLEY, Paul Joseph , OWENS, Andrew, Pate , SHAW, Duncan, Edward , WILLIAMS, Brian, John
发明人： DINNELL, Kevin , HARRISON, Timothy , GIBSON, Karl, Richard , JELLEY, Richard, Alexander , NADIN, Alan, John , OAKLEY, Paul Joseph , OWENS, Andrew, Pate , SHAW, Duncan, Edward , WILLIAMS, Brian, John
IPC分类号： C07D285/16
CPC分类号： C07D279/02
摘要： Compounds of formula (I): inhibit gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.
摘要翻译：式（I）化合物：抑制γ-分泌酶，因此可用于治疗或预防阿尔茨海默氏病。

5. 发明申请

WO2004031139A1 CYCLOHEXYL SULPHONES AS GAMMA-SECRETASE INHIBITORS 审中-公开
标题翻译： CYCLOHEXYL SULPHONES作为GAMMA-SECRETASE抑制剂
公开(公告)号：WO2004031139A1
公开(公告)日：2004-04-15
申请号：PCT/GB2003/004196
申请日：2003-09-25
申请人： MERCK SHARP & DOHME LIMITED , CHURCHER, Ian , HARRISON, Timothy , KERRAD, Sonia , NADIN, Alan, John , OWENS, Andrew, Pate , SHAW, Duncan, Edward , THOMSON, Joanne , WILLIAMS, Susannah
发明人： CHURCHER, Ian , HARRISON, Timothy , KERRAD, Sonia , NADIN, Alan, John , OWENS, Andrew, Pate , SHAW, Duncan, Edward , THOMSON, Joanne , WILLIAMS, Susannah
IPC分类号： C07C317/30
CPC分类号： C07D213/70 , A61K31/10 , C07C317/30 , C07C2601/14 , C07D213/74 , C07D231/18 , C07D233/42 , C07D249/12 , C07D257/04 , C07D261/10 , C07D275/03 , C07D277/36 , C07D295/088 , C07D307/64 , C07D333/34
摘要： Compounds of formula (I) inhibit the processing of APP by gamma-secretase, and hence are useful in treating or preventing Alzheimer's disease.
摘要翻译：式（I）化合物通过γ-分泌酶抑制APP的加工，因此可用于治疗或预防阿尔茨海默氏病。

6. 发明申请

WO2009053715A8 THIENOPYRIMIDIENE DERIVATIVES AS PI3K INHIBITORS 审中-公开
标题翻译：作为PI3K抑制剂的三烯衍生物衍生物
公开(公告)号：WO2009053715A8
公开(公告)日：2010-06-03
申请号：PCT/GB2008003621
申请日：2008-10-27
申请人： HOFFMANN LA ROCHE , HANCOX TIMOTHY COLIN , PEGG NEIL ANTHONY , NADIN ALAN JOHN , PRICE STEPHEN
发明人： HANCOX TIMOTHY COLIN , PEGG NEIL ANTHONY , NADIN ALAN JOHN , PRICE STEPHEN
IPC分类号： C07D495/04 , A61K31/519 , A61P35/00 , C07D519/00
CPC分类号： C07D495/04 , C07D519/00
摘要： Thienopyrimidines of formula (I) wherein W and R1 to R4 are as defined in the claims, and the pharmaceutically acceptable salts thereof are inhibitors of PI3K and are selective for the p110d isoform, which is a class Ia PI3 kinase, over both other class Ia and class Ib kinases. The compounds may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
摘要翻译：其中W和R 1至R 4如权利要求中所定义的式（I）的噻吩并嘧啶及其药学上可接受的盐是PI3K的抑制剂，并且对于作为Ia类PI3激酶的p110d同种型，对于其它Ia类和1b类激酶。该化合物可用于治疗与PI3激酶例如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌功能障碍和神经障碍相关的异常细胞生长，功能或行为引起的疾病和障碍。

7. 发明申请

WO2010019099A1 2-HYDROXY-ETHANESULFONATE SALT 审中-公开
标题翻译： 2-羟基 - 乙磺酸盐
公开(公告)号：WO2010019099A1
公开(公告)日：2010-02-18
申请号：PCT/SE2009/050926
申请日：2009-08-11
申请人： ASTRAZENECA AB , ARGENTA DISCOVERY Ltd. , NADIN, Alan John
发明人： NADIN, Alan John
IPC分类号： A61K31/439 , A61P11/00 , A61K31/42
CPC分类号： C07D453/02
摘要： The invention provides (R) -1- [3- (R) -cyclohexyl-hydroxy-phenyl- methyl) -isoxazol-5-ylmethyl] -3- (3-f luoro-phenoxy) -1-azonia- bicyclo[2.2.2]octane 2-hydroxy ethanesulf onate, pharmaceutical compositions containing the compound and its use as a muscarinic antagonists, for the treatment of chronic obstructive pulmonary disease.
摘要翻译：本发明提供（R）-1- [3-（R） - 环己基 - 羟基 - 苯基 - 甲基） - 异恶唑-5-基甲基] -3-（3-氟 - 苯氧基）-1-氮鎓 - 二环[2.2 .2]辛烷-2-羟基乙磺酸盐，含有该化合物的药物组合物及其作为毒蕈碱性拮抗剂的用途，用于治疗慢性阻塞性肺疾病。

8. 发明申请

WO2008152394A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2008152394A1
公开(公告)日：2008-12-18
申请号：PCT/GB2008/002023
申请日：2008-06-12
申请人： F.HOFFMANN-LA ROCHE AG , HANCOX, Timothy, Colin , PEGG, Neil, Anthony , NADIN, Alan, John , PRICE, Stephen
发明人： HANCOX, Timothy, Colin , PEGG, Neil, Anthony , NADIN, Alan, John , PRICE, Stephen
IPC分类号： C07D491/048 , C07D519/00 , A61K31/33 , A61P35/00
CPC分类号： C07D519/00 , C07D491/048
摘要： Furanopyrimidines of formula (I): wherein W represents a furan ring; R 1 and R 2 form, together with the N atom to which they are attached, a group of the following formula (IIa): in which A is selected from: (a) a 4- to 7-membered saturated N-containing heterocyclic ring which includes 0 or 1 additional heteroatoms selected from N, S and O, the ring being fused to a second ring selected from a 4- to 7-membered saturated N-containing heterocyclic ring as defined above, a 5- to 12-membered unsaturated heterocyclic ring, a 5- to 7-membered saturated O-containing heterocyclic ring, a 3- to 12- membered saturated carbocyclic ring and an unsaturated 5- to 12- membered carbocyclic ring to form a heteropolycyclic ring system, the heteropolycyclic ring system being unsubstituted or substituted; (b) a 4- to 7-membered saturated N-containing heterocyclic ring which includes 0 or 1 additional heteroatoms selected from N, S and O and which further comprises, linking two constituent atoms of the ring, a bridgehead group selected from -(CR' 2 ) n - and -(CR' 2 ) r -O-(CR' 2 ) s - wherein each R' is independently H or C 1 - C 6 alkyl, n is 1, 2 or 3, r is 0 or 1 and s is 0 or 1, the remaining ring positions being unsubstituted or substituted; and (c) a group of formula (IIb): wherein ring B is a 4- to 7-membered saturated N-containing heterocyclic ring which includes 0 or 1 additional heteroatoms selected from N, S and O and ring B' is a 3- to 12- membered saturated carbocyclic ring, a 5- to 7- membered saturated O-containing heterocyclic ring or a 4- to 7-membered saturated N-containing heterocyclic ring as defined above, each of B and B' being unsubstituted or substituted; m is 0, 1 or 2; R 3 is H or C 1 -C 6 alkyl; R 4 is an indole group which is unsubstituted or substituted; and R a is selected from R, halo, CN, C(O)NR 2 , halo(C1-C 6 )alkyl, SO 2 R, SO 2 NR 2 , NRSO 2 R, NRC(O)R, NRC(O)OR and NRC(O)NR 2 wherein each R is independently H or C 1 -C 6 alkyl; and the pharmaceutically acceptable salts thereof are inhibitors of PI3K and are selective for the p110δ isoform, which is a class Ia PI3 kinase, over both other class Ia and class Ib kinases. The compounds may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
摘要翻译：式（I）的呋喃并嘧啶：其中W表示呋喃环; R1和R2与它们所连接的N原子一起形成下式（IIa）的基团：其中A选自：（a）4至7元饱和的含N的杂环，其中包括选自N，S和O的0或1个另外的杂原子，该环与第二个环稠合，所述第二个环选自如上定义的4-7元饱和的含氮杂环，5-至12元不饱和杂环环，5至7元饱和的含O的杂环，3至12元饱和碳环和不饱和的5至12元碳环以形成杂多环环系，杂多环系为未取代的或取代; （b）含有0或1个选自N，S和O的杂原子的4至7元饱和的含N杂环，并且还包含连接环的两个组成原子的桥头基，所述桥头基选自 - （ CR'2）n - 和 - （CR'2）rO-（CR'2）s-，其中每个R'独立地为H或C 1 -C 6烷基，n为1,2或3，r为0或1，s 为0或1，其余环位未取代或取代; 和（c）式（IIb）的基团：其中环B是包含0或1个选自N，S和O的另外的杂原子的4至7元饱和的含N杂环，并且环B'是3 至12元饱和碳环，5-至7-元饱和含O杂环或如上定义的4-至7-元饱和含氮杂环，B和B'各自为未取代或取代的 ; m为0,1或2; R3是H或C1-C6烷基; R4是未取代或取代的吲哚基; 并且R a选自R，卤素，CN，C（O）NR 2，卤代（C 1 -C 6）烷基，SO 2 R，SO 2 NR 2，NRSO 2 R，NRC（O）R，NRC（O）OR和NRC（O） R独立地为H或C 1 -C 6烷基; 其药学上可接受的盐是PI3K的抑制剂，并且对于其它Ia类和1b类激酶对p110d亚型是Ia类PI3激酶具有选择性。该化合物可用于治疗与PI3激酶例如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌功能障碍和神经障碍相关的异常细胞生长，功能或行为引起的疾病和障碍。

9. 发明申请

WO2008152387A1 QUINAZOLINE DERIVATIVES AS PI3 KINASE INHIBITORS 审中-公开
标题翻译：喹诺酮衍生物作为PI3激酶抑制剂
公开(公告)号：WO2008152387A1
公开(公告)日：2008-12-18
申请号：PCT/GB2008/002009
申请日：2008-06-12
申请人： F.HOFFMANN-LA ROCHE AG , BAKER, Stewart, J. , HANCOX, Timothy, Colin , PEGG, Neil, Anthony , NADIN, Alan, John , PRICE, Stephen
发明人： BAKER, Stewart, J. , HANCOX, Timothy, Colin , PEGG, Neil, Anthony , NADIN, Alan, John , PRICE, Stephen
IPC分类号： C07D413/14 , A61K31/5377 , A61P35/00 , A61P9/00 , A61P31/12
CPC分类号： C07D413/14
摘要： The invention provides a compound which is a quinazoline of formula (I): and the pharmaceutically acceptable salts thereof are inhibitors of PI3K and are selective for the p110δ isoform, which is a class Ia PI3 kinase, over other class Ia PI3 kinases and over class Ib kinases. The compounds may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
摘要翻译：本发明提供了一种化合物，其是式（I）的喹唑啉：其药学上可接受的盐是PI3K的抑制剂，并且对于与其它Ia类PI3激酶相似的p110d同种型（其为Ia类PI3激酶）而言是选择性的 Ib激酶。该化合物可用于治疗与PI3激酶例如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌功能障碍和神经障碍相关的异常细胞生长，功能或行为引起的疾病和障碍。

10. 发明申请

WO2008023157A1 NITROGEN CONTAINING HETEROCYCLIC COMPOUNDS USEFUL AS M3-RECEPTOR MODULATORS 审中-公开
标题翻译：含有杂环化合物的含氮作为M3受体调节剂有用
公开(公告)号：WO2008023157A1
公开(公告)日：2008-02-28
申请号：PCT/GB2007/003170
申请日：2007-08-20
申请人： ARGENTA DISCOVERY LIMITED , ASTRAZENECA AB , BULL, Richard, James , VAN DEN HEUVEL, Marco , METE, Antonio , NADIN, Alan, John , RAY, Nicholas, Charles
发明人： BULL, Richard, James , VAN DEN HEUVEL, Marco , METE, Antonio , NADIN, Alan, John , RAY, Nicholas, Charles
IPC分类号： C07D231/12 , C07D233/61 , C07D249/08 , C07D261/08 , C07D263/32 , C07D271/06 , C07D271/10 , C07D277/28 , C07D285/08 , C07D285/12 , C07D413/14 , A61K31/41 , A61P11/00 , A61P1/00 , A61P9/00
CPC分类号： C07D271/10 , C07D231/12 , C07D233/61 , C07D249/08 , C07D261/08 , C07D263/32 , C07D271/06 , C07D277/28 , C07D285/08 , C07D285/12 , C07D413/04 , C07D413/14
摘要： A compound of formula (I): Formula (I) having M3 receptor- antagonist activity or having both muscarinic receptor antagonist and β2-agonist activity; a composition comprising such a compound; the use of such a compound in therapy (such as asthma or COPD); and a method of treating a patient with such a compound.
摘要翻译：式（I）的化合物：具有M3受体拮抗剂活性或具有毒蕈碱受体拮抗剂和β2激动剂活性的式（I）包含这种化合物的组合物; 在治疗（如哮喘或COPD）中使用这种化合物; 以及用这种化合物治疗患者的方法。

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