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公开(公告)号：WO2008039087A3
公开(公告)日：2008-08-14
申请号：PCT/NZ2007000285
申请日：2007-09-28
申请人： AUCKLAND UNISERVICES LTD , STRIBBLING STEPHEN MARK , MOUNTJOY KATHLEEN GRACE , TERCEL MOANA , WILSON WILLIAM ROBERT , DENNY WILLIAM ALEXANDER , STEVENSON RALPH JAMES , LU GUO-LIANG
发明人： STRIBBLING STEPHEN MARK , MOUNTJOY KATHLEEN GRACE , TERCEL MOANA , WILSON WILLIAM ROBERT , DENNY WILLIAM ALEXANDER , STEVENSON RALPH JAMES , LU GUO-LIANG
IPC分类号： C07D403/12 , A61K31/395 , A61K31/403 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , C07D209/56
CPC分类号： C07D209/60 , C07D403/12
摘要： The present invention relates to compounds which are indoline derivatives of formula (I), wherein Rl, R2, R3, R4 and n are as defined in the specification, intermediates used in their synthesis and pharmaceutical compositions containing these compounds. The invention is also concerned with methods utilising these compounds in prophylactic or therapeutic treatment of obesity, weight gain, metabolic disorders resulting in obesity or weight gain and associated conditions such as high blood glucose and triglycerides, and Type II diabetes.
摘要翻译： 本发明涉及作为式（I）的二氢吲哚衍生物的化合物，其中R1，R2，R3，R4和n如本说明书中所定义，在其合成中使用的中间体和含有这些化合物的药物组合物。 本发明还涉及利用这些化合物在预防或治疗肥胖症，体重增加，导致肥胖或体重增加的代谢紊乱以及相关病症如高血糖和甘油三酸酯以及II型糖尿病中的方法。
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公开(公告)号：WO2018083635A3
公开(公告)日：2018-05-11
申请号：PCT/IB2017/056848
申请日：2017-11-03
申请人： AUCKLAND UNISERVICES LIMITED , MARSHALL, Andrew James , BUCHANAN, Christina Maree , REWCASTLE, Gordon William , LU, Guo-Liang , FLANAGAN, Jack Urquhart , BONNET, Muriel , SHEPHERD, Peter Robin , JAMIESON, Stephen Michael Frazer , GAMAGE, Swarnalatha Akuratiya , DENNY, William Alexander
发明人： MARSHALL, Andrew James , BUCHANAN, Christina Maree , REWCASTLE, Gordon William , LU, Guo-Liang , FLANAGAN, Jack Urquhart , BONNET, Muriel , SHEPHERD, Peter Robin , JAMIESON, Stephen Michael Frazer , GAMAGE, Swarnalatha Akuratiya , DENNY, William Alexander
IPC分类号： C07D219/06 , C07D311/86 , C07D219/14 , C07D335/12 , A61K31/435 , A61K31/35 , A61P35/00 , A61P19/02
摘要： Disclosed are tricyclic heterocyclic compounds having kinase inhibitory activity, pharmaceutical compositions and kits comprising the compounds, and use of the compounds in the treatment of or in medicaments for the treatment of various diseases and conditions. In particular, disclosed are tricyclic heterocyclic compounds of the formula (I) having CSF-1R (c-FMS kinase) inhibitory activity and their use in the treatment of various diseases and conditions, such as those mediated by CSF-1R, including proliferative or neoplastic diseases and conditions, including cancers, and bone, inflammatory, and autoimmune diseases and conditions.
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公开(公告)号：WO2018083635A2
公开(公告)日：2018-05-11
申请号：PCT/IB2017/056848
申请日：2017-11-03
申请人： AUCKLAND UNISERVICES LIMITED , MARSHALL, Andrew James , BUCHANAN, Christina Maree , REWCASTLE, Gordon William , LU, Guo-Liang , FLANAGAN, Jack Urquhart , BONNET, Muriel , SHEPHERD, Peter Robin , JAMIESON, Stephen Michael Frazer , GAMAGE, Swarnalatha Akuratiya , DENNY, William Alexander
发明人： MARSHALL, Andrew James , BUCHANAN, Christina Maree , REWCASTLE, Gordon William , LU, Guo-Liang , FLANAGAN, Jack Urquhart , BONNET, Muriel , SHEPHERD, Peter Robin , JAMIESON, Stephen Michael Frazer , GAMAGE, Swarnalatha Akuratiya , DENNY, William Alexander
摘要： Disclosed are tricyclic heterocyclic compounds having kinase inhibitory activity, pharmaceutical compositions and kits comprising the compounds, and use of the compounds in the treatment of or in medicaments for the treatment of various diseases and conditions. In particular, disclosed are tricyclic heterocyclic compounds of the formula (I) having CSF-1R (c-FMS kinase) inhibitory activity and their use in the treatment of various diseases and conditions, such as those mediated by CSF-1R, including proliferative or neoplastic diseases and conditions, including cancers, and bone, inflammatory, and autoimmune diseases and conditions.
摘要翻译： 公开了具有激酶抑制活性的三环杂环化合物，包含所述化合物的药物组合物和试剂盒，以及所述化合物在治疗或治疗各种疾病和病症的药物中的用途。 具体而言，公开了具有CSF-1R（c-FMS激酶）抑制活性的式（I）三环杂环化合物及其在治疗各种疾病和病症（例如由CSF-1R介导的那些）中的用途，包括增殖性或 肿瘤疾病和病症，包括癌症，以及骨骼，炎症和自身免疫疾病和病症。
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公开(公告)号：WO2008039087A2
公开(公告)日：2008-04-03
申请号：PCT/NZ2007/000285
申请日：2007-09-28
申请人： AUCKLAND UNISERVICES LIMITED , STRIBBLING, Stephen Mark , MOUNTJOY, Kathleen Grace , TERCEL, Moana , WILSON, William, Robert , DENNY, William, Alexander , STEVENSON, Ralph, James , LU, Guo-Liang
发明人： STRIBBLING, Stephen Mark , MOUNTJOY, Kathleen Grace , TERCEL, Moana , WILSON, William, Robert , DENNY, William, Alexander , STEVENSON, Ralph, James , LU, Guo-Liang
CPC分类号： C07D209/60 , C07D403/12
摘要： The present invention relates to compounds which are indoline derivatives, with intermediates used in their synthesis and with pharmaceutical compositions containing these compounds. The invention is also concerned with methods utilising these compounds in prophylactic or therapeutic treatment of obesity, weight gain, metabolic disorders resulting in obesity or weight gain and associated conditions such as high blood glucose and triglycerides, and Type II diabetes.
摘要翻译： 本发明涉及二氢吲哚衍生物，其合成中使用的中间体和含有这些化合物的药物组合物。 本发明还涉及利用这些化合物在预防或治疗肥胖症，体重增加，导致肥胖或体重增加的代谢紊乱以及相关病症如高血糖和甘油三酸酯以及II型糖尿病中的方法。
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公开(公告)号：WO2010104406A8
公开(公告)日：2010-09-16
申请号：PCT/NZ2010/000040
申请日：2010-03-11
申请人： AUCKLAND UNISERVICES LIMITED , SMAILL, Jeffrey, Bruce , PATTERSON, Adam Vorn , HAY, Michael Patrick , DENNY, William, Alexander , WILSON, William Robert , LU, Guo-Liang , ANDERSON, Robert, Forbes , LEE, Ho Huat , ASHOORZADEH, Amir
发明人： SMAILL, Jeffrey, Bruce , PATTERSON, Adam Vorn , HAY, Michael Patrick , DENNY, William, Alexander , WILSON, William Robert , LU, Guo-Liang , ANDERSON, Robert, Forbes , LEE, Ho Huat , ASHOORZADEH, Amir
IPC分类号： C07D471/04 , A61K31/519 , C07D403/14 , A61K31/4178 , A61P35/00 , C07D405/14 , A61K31/4709 , C07D239/94 , A61K31/517 , C07D403/12
摘要： The invention provides novel prodrug compounds comprising a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger, where the compound carries a positive charge. In preferred embodiments, the compounds are of Formula I: where: X is any negatively charged counterion; R 1 is a group of the formula —(CH 2 ) n Tr, where Tr is an aromatic nitroheterocycle or aromatic nitrocarbocycle and —(CH 2 ) n Tr acts as a reductively-activated fragmenting trigger; and n is an integer from 0 to 6; R 2 , R 3 and R 4 may each independently be selected from aliphatic or aromatic groups of a tertiary amine kinase inhibitor (R 2 )(R 3 )(R 4 )N, or two of R 2 , R 3 , and R 4 may form an aliphatic or aromatic heterocyclic amine ring of a kinase inhibitor, or one of R 2 , R 3 and R 4 may be absent and two of R 2 , R 3 and R 4 form an aromatic heterocyclic amine ring of a kinase inhibitor. The compounds of the invention are useful in treating proliferative diseases such as cancer.
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公开(公告)号：WO2011028135A1
公开(公告)日：2011-03-10
申请号：PCT/NZ2010/000174
申请日：2010-09-02
申请人： AUCKLAND UNISERVICES LIMITED , SMAILL, Jeffrey Bruce , PATTERSON, Adam Vorn , LU, Guo-Liang , LEE, Ho Huat , ASHOORZADEH, Amir , ANDERSON, Robert Forbes , WILSON, William Robert , DENNY, William Alexander , HSU, Huai-Ling (Annie) , MAROZ, Andrej , JAMIESON, Stephen Michael Frazer , MOWDAY, Alexandra Marie , CARLIN, Kendall Marie
发明人： SMAILL, Jeffrey Bruce , PATTERSON, Adam Vorn , LU, Guo-Liang , LEE, Ho Huat , ASHOORZADEH, Amir , ANDERSON, Robert Forbes , WILSON, William Robert , DENNY, William Alexander , HSU, Huai-Ling (Annie) , MAROZ, Andrej , JAMIESON, Stephen Michael Frazer , MOWDAY, Alexandra Marie , CARLIN, Kendall Marie
IPC分类号： C07D471/04 , C07D403/12 , C07D403/14 , A61K31/519 , A61P35/00
CPC分类号： C07D471/04 , A61K31/519
摘要： The present invention relates to pyrido[3,4-d]pyrimidine compounds of formula (I) suitable as kinase inhibitors, kinase inhibitors in prodrug form, their use in compositions and medicaments which are suitable for the treatment of diseases related to kinase activity such as cancers.
摘要翻译： 本发明涉及适合作为激酶抑制剂的式（I）的吡啶并[3,4-d]嘧啶化合物，其为前体药物形式的激酶抑制剂，其在组合物和药物中的用途，其适用于治疗与激酶活性相关的疾病 作为癌症。
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公开(公告)号：WO2010104406A1
公开(公告)日：2010-09-16
申请号：PCT/NZ2010000040
申请日：2010-03-11
申请人： AUCKLAND UNISERVICES LTD , SMAILL JEFFREY BRUCE , PATTERSON ADAM VORN , DENNY WILLIAM ALEXANDER , WILSON WILLIAM ROBERT , LU GUO-LIANG , ANDERSON ROBERT FORBES , LEE HO HUAT , ASHOORZADEN AMIR
发明人： SMAILL JEFFREY BRUCE , PATTERSON ADAM VORN , DENNY WILLIAM ALEXANDER , WILSON WILLIAM ROBERT , LU GUO-LIANG , ANDERSON ROBERT FORBES , LEE HO HUAT , ASHOORZADEN AMIR
IPC分类号： C07D471/04 , A61K31/4178 , A61K31/4709 , A61K31/517 , A61K31/519 , A61P35/00 , C07D239/94 , C07D403/12 , C07D403/14 , C07D405/14
CPC分类号： C07D471/04 , A61K31/4178 , A61K31/4709 , A61K31/517 , A61K31/519 , C07D239/94 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14
摘要： The invention provides novel prodrug compounds comprising a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger, where the compound carries a positive charge. In preferred embodiments, the compounds are of Formula I: where: X is any negatively charged counterion; R1 is a group of the formula -(CH2)nTr, where Tr is an aromatic nitroheterocycle or aromatic nitrocarbocycle and -(CH2)nTr acts as a reductively-activated fragmenting trigger; and n is an integer from 0 to 6; R2, R3 and R4 may each independently be selected from aliphatic or aromatic groups of a tertiary amine kinase inhibitor (R2)(R3)(R4)N, or two of R2, R3, and R4 may form an aliphatic or aromatic heterocyclic amine ring of a kinase inhibitor, or one of R2, R3 and R4 may be absent and two of R2, R3 and R4 form an aromatic heterocyclic amine ring of a kinase inhibitor. The compounds of the invention are useful in treating proliferative diseases such as cancer.
摘要翻译： 本发明提供包含激酶抑制剂和还原活化的片段化芳族硝基杂环或芳族硝基碳环触发剂的新型前药化合物，其中化合物携带正电荷。 在优选的实施方案中，化合物具有式I：其中：X是任何带负电的抗衡离子; R1是式 - （CH2）nTr的基团，其中Tr是芳族硝基杂环或芳族硝基碳环，和 - （CH2）nTr作为还原活化的片段触发剂; n为0〜6的整数。 R2，R3和R4可以各自独立地选自叔胺激酶抑制剂（R2）（R3）（R4）N的脂族或芳族基团，或者R2，R3和R4中的两个可以形成脂族或芳族杂环胺环 的激酶抑制剂，或R 2，R 3和R 4中的一个可以不存在，R2，R3和R4中的两个形成激酶抑制剂的芳族杂环胺环。 本发明的化合物可用于治疗增殖性疾病如癌症。
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公开(公告)号：WO2008039087A8
公开(公告)日：2009-07-09
申请号：PCT/NZ2007000285
申请日：2007-09-28
申请人： AUCKLAND UNISERVICES LTD , STRIBBLING STEPHEN MARK , MOUNTJOY KATHLEEN GRACE , TERCEL MOANA , WILSON WILLIAM ROBERT , DENNY WILLIAM ALEXANDER , STEVENSON RALPH JAMES , LU GUO-LIANG
发明人： STRIBBLING STEPHEN MARK , MOUNTJOY KATHLEEN GRACE , TERCEL MOANA , WILSON WILLIAM ROBERT , DENNY WILLIAM ALEXANDER , STEVENSON RALPH JAMES , LU GUO-LIANG
IPC分类号： C07D403/12 , A61K31/395 , A61K31/403 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , C07D209/56
CPC分类号： C07D209/60 , C07D403/12
摘要： The present invention relates to compounds which are indoline derivatives of formula (I), wherein Rl, R2, R3, R4 and n are as defined in the specification, intermediates used in their synthesis and pharmaceutical compositions containing these compounds. The invention is also concerned with methods utilising these compounds in prophylactic or therapeutic treatment of obesity, weight gain, metabolic disorders resulting in obesity or weight gain and associated conditions such as high blood glucose and triglycerides, and Type II diabetes.
摘要翻译： 本发明涉及作为式（I）的二氢吲哚衍生物的化合物，其中R1，R2，R3，R4和n如说明书中所定义，用于其合成的中间体和含有这些化合物的药物组合物。 本发明还涉及利用这些化合物在预防或治疗肥胖症，体重增加，导致肥胖或体重增加的代谢紊乱以及相关病症如高血糖和甘油三酸酯以及II型糖尿病中的方法。
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