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.

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。

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。

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.

公开(公告)号：US06531491B1

公开(公告)日：2003-03-11

申请号：US09983786

申请日：2001-10-25

申请人： Robert Steven Kania ,  Steven Lee Bender ,  Allen J. Borchardt ,  Stephan James Cripps ,  Cynthia Louise Palmer ,  Anna Maria Tempczyk-Russell ,  Michael David Varney ,  Michael Raymond Collins

发明人： Robert Steven Kania ,  Steven Lee Bender ,  Allen J. Borchardt ,  Stephan James Cripps ,  Cynthia Louise Palmer ,  Anna Maria Tempczyk-Russell ,  Michael David Varney ,  Michael Raymond Collins

IPC分类号： C07D4002

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。

公开(公告)号：US07772246B2

公开(公告)日：2010-08-10

申请号：US12182977

申请日：2008-07-30

申请人： Jingrong Jean Cui ,  Judith Gail Deal ,  Danlin Gu ,  Chuangxing Guo ,  Mary Catherine Johnson ,  Robert Steven Kania ,  Susan Elizabeth Kephart ,  Maria Angelica Linton ,  Indrawan James McAlpine ,  Mason Alan Pairish ,  Cynthia Louise Palmer

发明人： Jingrong Jean Cui ,  Judith Gail Deal ,  Danlin Gu ,  Chuangxing Guo ,  Mary Catherine Johnson ,  Robert Steven Kania ,  Susan Elizabeth Kephart ,  Maria Angelica Linton ,  Indrawan James McAlpine ,  Mason Alan Pairish ,  Cynthia Louise Palmer

IPC分类号： A61K31/505

CPC分类号： C07D471/04 ,  C07D401/14 ,  C07D403/14 ,  C07D487/04

摘要： The present invention is directed to compounds of Formula (I), and to pharmaceutically acceptable salts thereof, their synthesis, and their use as Raf inhibitors.

摘要翻译： 本发明涉及式（I）化合物及其药学上可接受的盐，其合成及其作为Raf抑制剂的用途。

公开(公告)号：US20090221608A1

公开(公告)日：2009-09-03

申请号：US12182977

申请日：2008-07-30

申请人： Jingrong Jean Cui ,  Judith Gail Deal ,  Danlin Gu ,  Chuangxing Guo ,  Mary Catherine Johnson ,  Robert Steven Kania ,  Susan Elizabeth Kephart ,  Maria Angelica Linton ,  Indrawan James McAlpine ,  Mason Alan Pairish ,  Cynthia Louise Palmer

发明人： Jingrong Jean Cui ,  Judith Gail Deal ,  Danlin Gu ,  Chuangxing Guo ,  Mary Catherine Johnson ,  Robert Steven Kania ,  Susan Elizabeth Kephart ,  Maria Angelica Linton ,  Indrawan James McAlpine ,  Mason Alan Pairish ,  Cynthia Louise Palmer

IPC分类号： A61K31/506 ,  C07D401/14 ,  A61K31/496 ,  A61P35/00

CPC分类号： C07D471/04 ,  C07D401/14 ,  C07D403/14 ,  C07D487/04

摘要： The present invention is directed to compounds of Formula (I), and to pharmaceutically acceptable salts thereof, their synthesis, and their use as Raf inhibitors.

摘要翻译： 本发明涉及式（I）化合物及其药学上可接受的盐，其合成及其作为Raf抑制剂的用途。

公开(公告)号：US06869962B2

公开(公告)日：2005-03-22

申请号：US10460010

申请日：2003-06-11

申请人： Michael Collins ,  Stephan Cripps ,  Judith Deal ,  Robert Steven Kania ,  Jihong Lou ,  Mingying He ,  Cynthia Louise Palmer ,  William Henry Romines, III ,  Ru Zhou

发明人： Michael Collins ,  Stephan Cripps ,  Judith Deal ,  Robert Steven Kania ,  Jihong Lou ,  Mingying He ,  Cynthia Louise Palmer ,  William Henry Romines, III ,  Ru Zhou

IPC分类号： A61K31/4365 ,  A61K31/444 ,  A61K31/506 ,  A61K31/5377 ,  A61P1/18 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P13/08 ,  A61P15/08 ,  A61P17/00 ,  A61P17/06 ,  A61P17/12 ,  A61P25/00 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D495/04 ,  C07D409/14

CPC分类号： A61K31/4743 ,  C07D495/04

摘要： The invention relates to compounds represented by the formula I and to prodrugs or metabolites thereof, or pharmaceutically acceptable salts or solvates of said compounds, said prodrugs, and said metabolites, wherein Z, Y, R11 and R14, R15, R16, and R17 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula I and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula I.

摘要翻译： 本发明涉及由式I表示的化合物及其前体药物或代谢物，或所述化合物，所述前药和所述代谢产物的药学上可接受的盐或溶剂合物，其中Z，Y，R 11和R 14， R 16，R 17和R 17如本文所定义。 本发明还涉及含有式I化合物的药物组合物和通过施用式I化合物来治疗哺乳动物中过度增殖性疾病的方法。

公开(公告)号：US07045528B2

公开(公告)日：2006-05-16

申请号：US10796226

申请日：2004-03-09

申请人： Michael Collins ,  Stephan Cripps ,  Judith Deal ,  Robert Steven Kania ,  Jihong Lou ,  Mingying He ,  Cynthia Louise Palmer ,  William Henry Romines, III ,  Ru Zhou

发明人： Michael Collins ,  Stephan Cripps ,  Judith Deal ,  Robert Steven Kania ,  Jihong Lou ,  Mingying He ,  Cynthia Louise Palmer ,  William Henry Romines, III ,  Ru Zhou

IPC分类号： A61K31/4365 ,  C07D495/04

CPC分类号： A61K31/4743 ,  C07D495/04

摘要： The invention relates to compounds represented by the formula I and to prodrugs or metabolites thereof, or pharmaceutically acceptable salts or solvates of said compounds, said prodrugs, and said metabolites, wherein Z, Y, R11 and R14, R15, R16, and R17 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula I and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula I.

公开(公告)号：US07053107B2

公开(公告)日：2006-05-30

申请号：US10737655

申请日：2003-12-15

申请人： Allen J. Borchardt ,  Robert Steven Kania ,  Cynthia L. Palmer

发明人： Allen J. Borchardt ,  Robert Steven Kania ,  Cynthia L. Palmer

IPC分类号： A61K31/4439 ,  A61K31/416 ,  C07D213/06 ,  C07D237/26

CPC分类号： A61K31/416 ,  C07D231/56 ,  C07D401/06 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14

摘要： Indazole compounds that modulate and/or inhibit the ophthalmic diseases and 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 ophthalmic diseases and 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/或抑制眼科疾病和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，以及治疗眼科疾病和癌症以及与不想要的血管生成和/或细胞增殖相关的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 关节炎和牛皮癣，通过施用有效量的这些化合物。