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：US08039596B2

公开(公告)日：2011-10-18

申请号：US12365638

申请日：2009-02-04

申请人： Steven Lee Bender ,  Gerald Fries Casperson ,  Dana Dan Hu-Lowe ,  Xin Jiang ,  Gang Li ,  Michael Aidan North ,  Jianying Wang ,  Grant Wickman ,  Peter Brams ,  Haichun Huang ,  Brigitte Devaux ,  Haibin Chen ,  Dawn M. Tanamachi ,  Kristopher Toy ,  Lan Yang ,  Tim W. Sproul ,  Mark Yamanaka

发明人： Steven Lee Bender ,  Gerald Fries Casperson ,  Dana Dan Hu-Lowe ,  Xin Jiang ,  Gang Li ,  Michael Aidan North ,  Jianying Wang ,  Grant Wickman ,  Peter Brams ,  Haichun Huang ,  Brigitte Devaux ,  Haibin Chen ,  Dawn M. Tanamachi ,  Kristopher Toy ,  Lan Yang ,  Tim W. Sproul ,  Mark Yamanaka

IPC分类号： C07K16/00 ,  C12P21/08 ,  A61K39/395 ,  A61K39/00

CPC分类号： C07K16/2842 ,  A61K2039/505 ,  C07K2317/21 ,  C07K2317/33 ,  C07K2317/52 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/567 ,  C07K2317/72 ,  C07K2317/73 ,  C07K2317/732 ,  C07K2317/76 ,  C07K2317/92 ,  C07K2319/30

摘要： The present disclosure provides isolated monoclonal antibodies, particularly human monoclonal antibodies, or antigen binding portions thereof, that specifically bind to integrin α5β1 with high affinity. Nucleic acid molecules encoding the antibodies of the disclosure, expression vectors, host cells and methods for expressing the antibodies of the disclosure are also provided. Immunoconjugates, bispecific molecules and pharmaceutical compositions comprising the antibodies or antigen binding portions thereof are also provided. The disclosure also provides methods for treating various cancers using the anti-α5β1 antibodies or antigen binding portions thereof described herein.

摘要翻译： 本公开提供以高亲和力特异性结合整联蛋白α5和bgr1的分离的单克隆抗体，特别是人单克隆抗体或其抗原结合部分。 还提供了编码本公开的抗体的核酸分子，表达载体，宿主细胞和用于表达本公开的抗体的方法。 还提供了免疫偶联物，双特异性分子和包含抗体或其抗原结合部分的药物组合物。 本公开还提供了使用本文所述的抗α5和bgr1抗体或其抗原结合部分治疗各种癌症的方法。

公开(公告)号：US06774243B2

公开(公告)日：2004-08-10

申请号：US09984555

申请日：2001-10-30

申请人： Qingping Tian ,  Naresh K. Nayyar ,  Srinivasan Babu ,  Junhua Tao ,  Terence Jarold Moran ,  Raymond Dagnino, Jr. ,  Lennert J. Mitchell, Jr. ,  Travis Paul Remarchuk ,  Michael Joseph Melnick ,  Steven Lee Bender

发明人： Qingping Tian ,  Naresh K. Nayyar ,  Srinivasan Babu ,  Junhua Tao ,  Terence Jarold Moran ,  Raymond Dagnino, Jr. ,  Lennert J. Mitchell, Jr. ,  Travis Paul Remarchuk ,  Michael Joseph Melnick ,  Steven Lee Bender

IPC分类号： C07D20726

CPC分类号： B01J19/2435 ,  B01J19/2475 ,  B01J2219/00033 ,  B01J2219/00099 ,  B01J2219/00103 ,  B01J2219/00159 ,  B01J2219/00162 ,  B01J2219/00177 ,  C07B2200/07 ,  C07C69/732 ,  C07C229/34 ,  C07C271/22 ,  C07C303/28 ,  C07D207/26 ,  C07D261/18 ,  C07D413/12 ,  C07C309/65

摘要： Efficient synthetic routes for the preparation of rhinovirus protease inhibitors of formula I, as well as key intermediates useful in those synthetic routes. These compounds of formula I, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.

摘要翻译： 用于制备式I的鼻病毒蛋白酶抑制剂的高效合成路线，以及在那些合成路线中有用的关键中间体。 这些式I化合物以及含有这些化合物的药物组合物适用于治疗患有一种或多种微小核糖核酸病毒感染的患者或宿主。

公开(公告)号：US06620828B2

公开(公告)日：2003-09-16

申请号：US09783584

申请日：2001-02-15

申请人： Shao Song Chu ,  Larry Andrew Alegria ,  Steven Lee Bender ,  Suzanne Pritchett Benedict ,  Allen J. Borchardt ,  Robert Steve Kania ,  Mitchell David Nambu ,  Anna Maria Tempczyk-Russell ,  Sepehr Sarshar ,  Dilip Bhumralkar ,  Zhengwei Peng ,  Michelle Yang

发明人： Shao Song Chu ,  Larry Andrew Alegria ,  Steven Lee Bender ,  Suzanne Pritchett Benedict ,  Allen J. Borchardt ,  Robert Steve Kania ,  Mitchell David Nambu ,  Anna Maria Tempczyk-Russell ,  Sepehr Sarshar ,  Dilip Bhumralkar ,  Zhengwei Peng ,  Michelle Yang

IPC分类号： C07D41704

CPC分类号： C07D417/04 ,  C07D277/38 ,  C07D277/62 ,  C07D417/14 ,  C07F9/6539 ,  C07F9/65583

摘要： Diaminothiazole 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 in order to 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 as well as 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：US06355807B1

公开(公告)日：2002-03-12

申请号：US09643864

申请日：2000-08-23

申请人： Qingping Tian ,  Naresh K. Nayyar ,  Srinivasan Babu ,  Junhua Tao ,  Terence Jarold Moran ,  Raymond Dagnino, Jr. ,  Lennert J. Mitchell, Jr. ,  Travis Paul Remarchuk ,  Michael Joseph Melnick ,  Steven Lee Bender

发明人： Qingping Tian ,  Naresh K. Nayyar ,  Srinivasan Babu ,  Junhua Tao ,  Terence Jarold Moran ,  Raymond Dagnino, Jr. ,  Lennert J. Mitchell, Jr. ,  Travis Paul Remarchuk ,  Michael Joseph Melnick ,  Steven Lee Bender

IPC分类号： C07D20726

CPC分类号： C07D207/26 ,  B01J19/2435 ,  B01J19/2475 ,  B01J2219/00033 ,  B01J2219/00099 ,  B01J2219/00103 ,  B01J2219/00159 ,  B01J2219/00162 ,  B01J2219/00177 ,  C07B2200/07 ,  C07C69/732 ,  C07C229/34 ,  C07C271/22 ,  C07C303/28 ,  C07D261/18 ,  C07D413/12 ,  C07C309/65

摘要： Efficient synthetic routes for the preparation of rhinovirus protease inhibitors of formula I, as well as key intermediates useful in those synthetic routes. These compounds of formula I, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses

摘要翻译： 用于制备式I的鼻病毒蛋白酶抑制剂的高效合成途径，以及在那些合成路线中有用的关键中间体。 这些式I化合物以及含有这些化合物的药物组合物适用于治疗感染了一种或多种微小核糖核酸病毒的患者或宿主

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：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：US06635641B2

公开(公告)日：2003-10-21

申请号：US09764306

申请日：2001-01-19

申请人： Steven Lee Bender ,  Dilip Bhumralkar ,  Michael Raymond Collins ,  Stephen James Cripps ,  Judith Gail Deal ,  Lei Jia ,  Mitchell David Nambu ,  Cynthia Louise Palmer ,  Zhengwei Peng ,  Michael David Varney

发明人： Steven Lee Bender ,  Dilip Bhumralkar ,  Michael Raymond Collins ,  Stephen James Cripps ,  Judith Gail Deal ,  Lei Jia ,  Mitchell David Nambu ,  Cynthia Louise Palmer ,  Zhengwei Peng ,  Michael David Varney

IPC分类号： C07D24118

CPC分类号： C07D213/30 ,  C07D213/56 ,  C07D217/14 ,  C07D217/16 ,  C07D217/22 ,  C07D231/12 ,  C07D231/38 ,  C07D233/56 ,  C07D237/28 ,  C07D241/12 ,  C07D241/18 ,  C07D249/08 ,  C07D249/14 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/12 ,  C07D471/04 ,  C07D487/04

摘要： Amide compounds represented by the formula: wherein: R1 is a moiety represented by the formula  where X is selected from the group consisting of CH2, O, S, and NH; and Y is selected from the group consisting of CH2, O, and S, provided that at least one of X and Y is CH2, or X and Y together with the bond there-between form a cyclopropyl; are described. These compounds and pharmaceutical compositions containing them modulate and/or inhibit the activity of certain protein kinases and are capable of mediating tyrosine kinase signal transduction in order to 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 as well as 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： 由下式表示的酰胺化合物：其中：R 1是由式R表示的部分，X选自CH 2，O，S和NH; 并且Y选自CH 2，O和S，条件是X和Y中的至少一个是CH 2，或者X和Y以及它们之间的键，形成环丙基; 被描述。 这些化合物和含有它们的药物组合物调节和/或抑制某些蛋白激酶的活性，并且能够介导酪氨酸激酶信号转导以调节和/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，以及治疗癌症以及与不想要的血管发生和/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，类风湿性关节炎 和牛皮癣，通过施用有效量的这种化合物。

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：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。