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公开(公告)号：US5972719A
公开(公告)日：1999-10-26
申请号：US743960
申请日：1996-11-05
申请人： Roland Ellwood Dolle, III , Tao Guo , Theodore Otto Johnson, Jr. , Hitesh K. Patel , Shiwei Tao , Zhen Min He
发明人： Roland Ellwood Dolle, III , Tao Guo , Theodore Otto Johnson, Jr. , Hitesh K. Patel , Shiwei Tao , Zhen Min He
IPC分类号： C07D207/14 , C07D207/16 , C07D241/04 , G01N33/53 , C07C23/00 , G01N33/543 , G01N33/551
CPC分类号： C07D207/14 , C07D207/16 , C07D241/04
摘要： Combinatorial chemical libraries of Formula I ##STR1## and methods for their preparation are disclosed. The libraries allow one to screen large numbers of compounds for a desired biological activity with relative ease. The libraries may be tagged or untagged. In preferred libraries, Y is the residue of an N-acylated amino acid, a substituted 4-aminoproline or a substituted piperazinealkanoic acid. The use of the libraries to discover biologically active compounds is also disclosed.
摘要翻译： 公开了式I的组合化学文库及其制备方法。 这些文库允许相对容易地筛选大量化合物以获得所需的生物活性。 库可能被标记或未标记。 在优选的文库中，Y是N-酰化氨基酸，取代的4-氨基脯氨酸或取代的哌嗪烷酸的残基。 还公开了使用这些文库发现生物活性化合物。
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公开(公告)号：US09040547B2
公开(公告)日：2015-05-26
申请号：US13617035
申请日：2012-09-14
申请人： Hengmiao Cheng , Theodore Otto Johnson, Jr. , John Charles Kath , Kevin Kun-Chin Liu , Elizabeth Ann Lunney , Asako Nagata , Sajiv Krishnan Nair , Simon Paul Planken , Scott Channing Sutton
发明人： Hengmiao Cheng , Theodore Otto Johnson, Jr. , John Charles Kath , Kevin Kun-Chin Liu , Elizabeth Ann Lunney , Asako Nagata , Sajiv Krishnan Nair , Simon Paul Planken , Scott Channing Sutton
IPC分类号： A61K31/519 , A61K31/5377 , A61K31/52 , C07D473/16 , C07D487/04
CPC分类号： C07D487/04 , C07D473/18 , C07D519/00
摘要： The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, T, V, W, X, Y, Z, ring A, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and m are defined herein. There novel pyrrolopyrimidine and purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.
摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，其中Q，T，V，W，X，Y，Z，环A，R1，R2，R3，R4，R5，R5a，R6，R7 ，R 8，R 9，R 10，R 11，R 12，R 13，R 14，R 15，R 16，R 17和m如本文所定义。 有新的吡咯并嘧啶和嘌呤衍生物可用于哺乳动物治疗异常细胞生长，如癌症。 另外的实施方案涉及含有化合物的药物组合物和使用化合物和组合物治疗哺乳动物异常细胞生长的方法。
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公开(公告)号：US20130079324A1
公开(公告)日：2013-03-28
申请号：US13617035
申请日：2012-09-14
申请人： Hengmiao Cheng , Theodore Otto Johnson, JR. , John Charles Kath , Kevin Kun-Chin Liu , Elizabeth Ann Lunney , Asako Nagata , Sajiv Krishnan Nair , Simon Paul Planken , Scott Channing Sutton
发明人： Hengmiao Cheng , Theodore Otto Johnson, JR. , John Charles Kath , Kevin Kun-Chin Liu , Elizabeth Ann Lunney , Asako Nagata , Sajiv Krishnan Nair , Simon Paul Planken , Scott Channing Sutton
IPC分类号： A61K31/519 , C07D473/18 , A61P35/00 , A61K31/5377 , C07D498/10 , A61K31/5386 , C07D487/04 , A61K31/52
CPC分类号： C07D487/04 , C07D473/18 , C07D519/00
摘要： The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, T, V, W, X, Y, Z, ring A, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and m are defined herein. There novel pyrrolopyrimidine and purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.
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公开(公告)号：US06534524B1
公开(公告)日：2003-03-18
申请号：US09983783
申请日：2001-10-25
申请人： Robert Steven Kania , Steven Lee Bender , Allen J. Borchardt , Stephan James Cripps , Ye Hua , Michael David Johnson , Theodore Otto Johnson, Jr. , Hiep The Luu , Cynthia Louise Palmer , Siegfried Heinz Reich , Anna Marie Tempczyk-Russell , Min Teng , Christine Thomas , Michael David Varney , Michael Brennan Wallace , Michael Raymond Collins
发明人： Robert Steven Kania , Steven Lee Bender , Allen J. Borchardt , Stephan James Cripps , Ye Hua , Michael David Johnson , Theodore Otto Johnson, Jr. , Hiep The Luu , Cynthia Louise Palmer , Siegfried Heinz Reich , Anna Marie Tempczyk-Russell , Min Teng , Christine Thomas , Michael David Varney , Michael Brennan Wallace , Michael Raymond Collins
IPC分类号： C07D40302
CPC分类号： C07D401/12 , C07D209/18 , C07D401/14 , C07D403/12
摘要： Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
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公开(公告)号：US07141587B2
公开(公告)日：2006-11-28
申请号：US10992146
申请日：2004-11-18
申请人： Robert Steven Kania , Steven Lee Bender , Allen J. Borchardt , Stephan James Cripps , Ye Hua , Michael David Johnson , Theodore Otto Johnson, Jr. , Hiep The Luu , Cynthia Louise Palmer , Siegfried Heinz Reich , Anna Maria Tempczyk-Russell , Min Teng , Christine Thomas , Michael David Varney , Michael Brennan Wallace , Michael Raymond Collins
发明人： Robert Steven Kania , Steven Lee Bender , Allen J. Borchardt , Stephan James Cripps , Ye Hua , Michael David Johnson , Theodore Otto Johnson, Jr. , Hiep The Luu , Cynthia Louise Palmer , Siegfried Heinz Reich , Anna Maria Tempczyk-Russell , Min Teng , Christine Thomas , Michael David Varney , Michael Brennan Wallace , Michael Raymond Collins
IPC分类号： C07D401/02 , A61K31/44
CPC分类号： C07D401/12 , C07D209/18 , C07D401/14 , C07D403/12
摘要： Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
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公开(公告)号：US06369226B1
公开(公告)日：2002-04-09
申请号：US09597148
申请日：2000-06-20
申请人： Siegfried Heinz Reich , Susan Elizabeth Kephart , Michael Brennan Wallace , Theodore Otto Johnson, Jr.
发明人： Siegfried Heinz Reich , Susan Elizabeth Kephart , Michael Brennan Wallace , Theodore Otto Johnson, Jr.
IPC分类号： C07D21174
CPC分类号： C07D295/205 , C07C235/84 , C07C237/30 , C07D295/155 , C07D413/04
摘要： Nonpeptide benzamide-containing inhibitors of human rhinovirus (HRV) 3C protease are described.
摘要翻译： 描述了人类鼻病毒（HRV）3C蛋白酶的含有多肽苯甲酰胺的抑制剂
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7.发明授权Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use 有权吲唑化合物和抑制蛋白激酶的药物组合物及其使用方法公开(公告)号：US06884890B2
公开(公告)日：2005-04-26
申请号：US10326755
申请日：2003-02-13
申请人： Robert Steven Kania , Steven Lee Bender , Allen J. Borchardt , Stephan James Cripps , Ye Hua , Michael David Johnson , Theodore Otto Johnson, Jr. , Hiep The Luu , Cynthia Louise Palmer , Siegfried Heinz Reich , Anna Marie Tempczyk-Russell , Min Teng , Christine Thomas , Michael David Varney , Michael Brennan Wallace , Michael Raymond Collins
发明人： Robert Steven Kania , Steven Lee Bender , Allen J. Borchardt , Stephan James Cripps , Ye Hua , Michael David Johnson , Theodore Otto Johnson, Jr. , Hiep The Luu , Cynthia Louise Palmer , Siegfried Heinz Reich , Anna Marie Tempczyk-Russell , Min Teng , Christine Thomas , Michael David Varney , Michael Brennan Wallace , Michael Raymond Collins
IPC分类号： C07D209/18 , C07D401/12 , C07D401/14 , C07D403/12 , C07D401/02
CPC分类号： C07D401/12 , C07D209/18 , C07D401/14 , C07D403/12
摘要： Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
摘要翻译： 描述了调节和/或抑制某些蛋白激酶活性的吲唑化合物。 这些化合物和含有它们的药物组合物能够介导酪氨酸激酶信号转导，从而调节和/或抑制不期望的细胞增殖。 本发明还涉及含有这些化合物的药物组合物的治疗或预防用途，以及治疗与不需要的血管生成和/或细胞增殖相关的癌症和其它疾病状态的方法，例如糖尿病性视网膜病变，新生血管性青光眼，类风湿性关节炎和 银屑病，通过施用有效量的这种化合物。
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公开(公告)号：US06218551B1
公开(公告)日：2001-04-17
申请号：US09337618
申请日：1999-06-21
申请人： Roland Ellwood Dolle, III , Tao Guo , Theodore Otto Johnson, Jr. , Hitesh K. Patel , Shiwei Tao , Zhen Min He
发明人： Roland Ellwood Dolle, III , Tao Guo , Theodore Otto Johnson, Jr. , Hitesh K. Patel , Shiwei Tao , Zhen Min He
IPC分类号： C07D20716
CPC分类号： C07D207/14 , C07D207/16 , C07D241/04
摘要： Combination chemical libraries of Formula I and methods for preparation are disclosed. The libraries allow one to screen large numbers of compounds for a desired biological activity with relative ease. The libraries may be tagged or untagged. In preferred libraries, Y is the residue of an N-acylated amino acid, a substituted 4-aminoproline or substituted piperazinealkanoic acid. The use of the libraries to discover biologically active compounds is also disclosed.
摘要翻译： 公开了式I的组合化学文库和制备方法。 这些文库允许相对容易地筛选大量化合物以获得所需的生物活性。 库可能被标记或未标记。 在优选的文库中，Y是N-酰化氨基酸，取代的4-氨基脯氨酸或取代的哌嗪烷酸的残基。 还公开了使用这些文库发现生物活性化合物。
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9.发明授权Indazole compounds and pharmaceutical compositions for Inhibiting protein kinases, and methods for their use 有权用于抑制蛋白激酶的吲唑化合物和药物组合物及其使用方法公开(公告)号：US06891044B2
公开(公告)日：2005-05-10
申请号：US10326037
申请日：2003-02-15
申请人： Robert Steven Kania , Steven Lee Bender , Allen J. Borchardt , Stephan James Cripps , Ye Hua , Michael David Johnson , Theodore Otto Johnson, Jr. , Hiep The Luu , Cynthia Louise Palmer , Siegfried Heinz Reich , Anna Maria Tempczyk-Russell , Min Teng , Christine Thomas , Michael David Varney , Michael Brennan Wallace , Michael Raymond Collins
发明人： Robert Steven Kania , Steven Lee Bender , Allen J. Borchardt , Stephan James Cripps , Ye Hua , Michael David Johnson , Theodore Otto Johnson, Jr. , Hiep The Luu , Cynthia Louise Palmer , Siegfried Heinz Reich , Anna Maria Tempczyk-Russell , Min Teng , Christine Thomas , Michael David Varney , Michael Brennan Wallace , Michael Raymond Collins
IPC分类号： C07D209/18 , C07D401/12 , C07D401/14 , C07D403/12 , C07D401/02
CPC分类号： C07D401/12 , C07D209/18 , C07D401/14 , C07D403/12
摘要： Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
摘要翻译： 描述了调节和/或抑制某些蛋白激酶活性的吲唑化合物。 这些化合物和含有它们的药物组合物能够介导酪氨酸激酶信号转导，从而调节和/或抑制不期望的细胞增殖。 本发明还涉及含有这些化合物的药物组合物的治疗或预防用途，以及治疗与不需要的血管生成和/或细胞增殖相关的癌症和其它疾病状态的方法，例如糖尿病性视网膜病变，新生血管性青光眼，类风湿性关节炎和 银屑病，通过施用有效量的这种化合物。
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