公开(公告)号：US07008953B2

公开(公告)日：2006-03-07

申请号：US10866059

申请日：2004-06-10

Applicant: Susan Elizabeth Kephart ,  Indrawan James McAlpine ,  Siegfried Heinz Reich

Inventor： Susan Elizabeth Kephart ,  Indrawan James McAlpine ,  Siegfried Heinz Reich

IPC: A61K31/4439 ,  C07D401/14

CPC classification number: C07D401/14

Abstract: 3,5 disubstituted indazole compounds that modulate and/or inhibit cell proliferation, such as the activity of protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating CDK dependent diseases 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.

Abstract translation: 描述了调节和/或抑制细胞增殖的3,5二取代吲唑化合物，例如蛋白激酶的活性。 这些化合物和含有它们的药物组合物能够介导CDK依赖性疾病调节和/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：US06884890B2

公开(公告)日：2005-04-26

申请号：US10326755

申请日：2003-02-13

Applicant: 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

Inventor： 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: C07D209/18 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D401/02

CPC classification number: C07D401/12 ,  C07D209/18 ,  C07D401/14 ,  C07D403/12

Abstract: 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.

Abstract translation: 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：US06693199B2

公开(公告)日：2004-02-17

申请号：US10300638

申请日：2002-11-21

Applicant: Bruce A. Dressman ,  James E. Fritz ,  Marlys Hammond ,  William J. Hornback ,  Stephen W. Kaldor ,  Vincent J. Kalish ,  John E. Munroe ,  Siegfried Heinz Reich ,  John H. Tatlock ,  Timothy A. Shepherd ,  Michael J. Rodriguez

Inventor： Bruce A. Dressman ,  James E. Fritz ,  Marlys Hammond ,  William J. Hornback ,  Stephen W. Kaldor ,  Vincent J. Kalish ,  John E. Munroe ,  Siegfried Heinz Reich ,  John H. Tatlock ,  Timothy A. Shepherd ,  Michael J. Rodriguez

IPC: C07D51502

CPC classification number: C07D401/06 ,  C07C237/42 ,  C07C323/60 ,  C07D207/16 ,  C07D209/08 ,  C07D211/60 ,  C07D213/40 ,  C07D215/48 ,  C07D215/50 ,  C07D217/02 ,  C07D217/06 ,  C07D217/26 ,  C07D401/12 ,  C07D403/14 ,  C07D409/12 ,  C07D417/12 ,  C07D495/04 ,  C07F9/62

Abstract: A method of making HIV protease inhibitors of general formula (1): These HIV compounds inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optically other antiviral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.

Abstract translation: 制备通式（1）的HIV蛋白酶抑制剂的方法：这些HIV化合物抑制或阻断HIV蛋白酶的生物活性，导致HIV病毒的复制终止。 这些化合物以及含有这些化合物和光学其它抗病毒剂作为活性成分的药物组合物适用于治疗已知导致AIDS的HIV病毒感染的患者或宿主。

公开(公告)号：US06534530B1

公开(公告)日：2003-03-18

申请号：US09631708

申请日：2000-08-03

Applicant: Peter Scott Dragovich ,  Ru Zhou ,  Stephen Evan Webber ,  Thomas J. Prins ,  Siegfried Heinz Reich ,  Susan E. Kephart ,  Yuanjin Rui

Inventor： Peter Scott Dragovich ,  Ru Zhou ,  Stephen Evan Webber ,  Thomas J. Prins ,  Siegfried Heinz Reich ,  Susan E. Kephart ,  Yuanjin Rui

IPC: A61K31427

CPC classification number: C07K5/06043 ,  A61K38/00 ,  C07K5/06191 ,  C07K5/0821 ,  C07K5/0827 ,  Y02A50/463 ,  Y02A50/465

Abstract: Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.

Abstract translation: 下式的化合物：其中式变量如本公开所定义，有利地抑制或阻断小核糖核蛋白病毒3C蛋白酶的生物学活性。 这些化合物以及含有这些化合物的药物组合物可用于治疗感染一种或多种微小核糖核酸病毒如RVP的患者或宿主。 还描述了制备这些化合物的中间体和合成方法。

公开(公告)号：US5952343A

公开(公告)日：1999-09-14

申请号：US481831

申请日：1995-06-07

Applicant: Bruce A. Dressman ,  James E. Fritz ,  William J. Hornback ,  Stephen W. Kaldor ,  Vincent J. Kalish ,  John E. Munroe ,  Siegfried Heinz Reich ,  John H. Tatlock ,  Timothy A. Shepherd ,  Michael J. Rodriguez

Inventor： Bruce A. Dressman ,  James E. Fritz ,  William J. Hornback ,  Stephen W. Kaldor ,  Vincent J. Kalish ,  John E. Munroe ,  Siegfried Heinz Reich ,  John H. Tatlock ,  Timothy A. Shepherd ,  Michael J. Rodriguez

IPC: C07D295/20 ,  A61K31/00 ,  A61K31/165 ,  A61K31/33 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/435 ,  A61K31/4353 ,  A61K31/4365 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/47 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/4738 ,  A61K31/4743 ,  A61K31/495 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/675 ,  A61P29/00 ,  A61P31/00 ,  A61P31/12 ,  A61P31/18 ,  A61P43/00 ,  C07C237/42 ,  C07C323/42 ,  C07C323/60 ,  C07D207/16 ,  C07D209/08 ,  C07D211/60 ,  C07D211/62 ,  C07D213/40 ,  C07D213/56 ,  C07D213/81 ,  C07D215/48 ,  C07D215/50 ,  C07D217/02 ,  C07D217/06 ,  C07D217/26 ,  C07D233/66 ,  C07D233/90 ,  C07D295/205 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D417/12 ,  C07D471/04 ,  C07D495/04 ,  C07F9/12 ,  C07F9/62 ,  C07K5/00 ,  C07D217/12 ,  C07D471/02

CPC classification number: C07D401/06 ,  C07C237/42 ,  C07C323/60 ,  C07D207/16 ,  C07D209/08 ,  C07D211/60 ,  C07D213/40 ,  C07D215/48 ,  C07D215/50 ,  C07D217/02 ,  C07D217/06 ,  C07D217/26 ,  C07D401/12 ,  C07D403/14 ,  C07D409/12 ,  C07D417/12 ,  C07D495/04 ,  C07F9/62

Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.

公开(公告)号：US5846993A

公开(公告)日：1998-12-08

申请号：US481833

申请日：1995-06-07

Applicant: Bruce A. Dressman ,  James E. Fritz ,  Stephen W. Kaldor ,  Vincent J. Kalish ,  Siegfried Heinz Reich ,  John H. Tatlock ,  Michael J. Rodriguez

Inventor： Bruce A. Dressman ,  James E. Fritz ,  Stephen W. Kaldor ,  Vincent J. Kalish ,  Siegfried Heinz Reich ,  John H. Tatlock ,  Michael J. Rodriguez

IPC: C07C237/42 ,  C07C323/60 ,  C07D207/16 ,  C07D209/08 ,  C07D211/60 ,  C07D213/40 ,  C07D215/48 ,  C07D215/50 ,  C07D217/02 ,  C07D217/06 ,  C07D217/26 ,  C07D233/66 ,  C07D233/90 ,  C07D401/06 ,  C07D401/12 ,  C07D403/14 ,  C07D409/12 ,  C07D417/12 ,  C07D495/04 ,  C07F9/62 ,  A61K31/40

CPC classification number: C07D213/40 ,  C07C237/42 ,  C07C323/60 ,  C07D207/16 ,  C07D209/08 ,  C07D211/60 ,  C07D215/48 ,  C07D215/50 ,  C07D217/02 ,  C07D217/06 ,  C07D217/26 ,  C07D401/06 ,  C07D401/12 ,  C07D403/14 ,  C07D409/12 ,  C07D417/12 ,  C07D495/04 ,  C07F9/62

Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.

公开(公告)号：US06891044B2

公开(公告)日：2005-05-10

申请号：US10326037

申请日：2003-02-15

Applicant: 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

Inventor： 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: C07D209/18 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D401/02

CPC classification number: C07D401/12 ,  C07D209/18 ,  C07D401/14 ,  C07D403/12

Abstract: 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.

Abstract translation: 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：US06632825B2

公开(公告)日：2003-10-14

申请号：US09882345

申请日：2001-06-13

Applicant: Theodore O. Johnson, Jr. ,  Shao Song Chu ,  Brian Walter Eastman ,  Ye Hua ,  Hiep The Luu ,  Siegfried Heinz Reich ,  Donald James Skalitzky ,  Yi Yang ,  Thomas F. Hendrickson ,  Fora P. Chan

Inventor： Theodore O. Johnson, Jr. ,  Shao Song Chu ,  Brian Walter Eastman ,  Ye Hua ,  Hiep The Luu ,  Siegfried Heinz Reich ,  Donald James Skalitzky ,  Yi Yang ,  Thomas F. Hendrickson ,  Fora P. Chan

IPC: A61K3144

CPC classification number: C07D207/26 ,  C07C237/22 ,  C07C275/16 ,  C07D209/42 ,  C07D215/48 ,  C07D231/14 ,  C07D241/44 ,  C07D249/06 ,  C07D333/70 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12

Abstract: Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.

Abstract translation: 下式的化合物：其中式变量如本公开所定义，有利地抑制或阻断小核糖核蛋白病毒3C蛋白酶的生物学活性。 这些化合物以及含有这些化合物的药物组合物可用于治疗感染一种或多种微小核糖核酸病毒如RVP的患者或宿主。 还描述了制备这些化合物的中间体和合成方法

公开(公告)号：US5834467A

公开(公告)日：1998-11-10

申请号：US482504

申请日：1995-06-07

Applicant: Vincent J. Kalish ,  Bruce A. Dressman ,  James E. Fritz ,  Marlys Hammond ,  William J. Hornback ,  Stephen W. Kaldor ,  John E. Munroe ,  Siegfried Heinz Reich ,  John H. Tatlock ,  Timothy A. Shepherd ,  Michael J. Rodriquez

Inventor： Vincent J. Kalish ,  Bruce A. Dressman ,  James E. Fritz ,  Marlys Hammond ,  William J. Hornback ,  Stephen W. Kaldor ,  John E. Munroe ,  Siegfried Heinz Reich ,  John H. Tatlock ,  Timothy A. Shepherd ,  Michael J. Rodriquez

IPC: C07D295/20 ,  A61K31/00 ,  A61K31/165 ,  A61K31/33 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/435 ,  A61K31/4353 ,  A61K31/4365 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/47 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/4738 ,  A61K31/4743 ,  A61K31/495 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/675 ,  A61P29/00 ,  A61P31/00 ,  A61P31/12 ,  A61P31/18 ,  A61P43/00 ,  C07C237/42 ,  C07C323/42 ,  C07C323/60 ,  C07D207/16 ,  C07D209/08 ,  C07D211/60 ,  C07D211/62 ,  C07D213/40 ,  C07D213/56 ,  C07D213/81 ,  C07D215/48 ,  C07D215/50 ,  C07D217/02 ,  C07D217/06 ,  C07D217/26 ,  C07D233/66 ,  C07D233/90 ,  C07D295/205 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D417/12 ,  C07D471/04 ,  C07D495/04 ,  C07F9/12 ,  C07F9/62 ,  C07K5/00 ,  A61K31/50

CPC classification number: C07D401/06 ,  C07C237/42 ,  C07C323/60 ,  C07D207/16 ,  C07D209/08 ,  C07D211/60 ,  C07D213/40 ,  C07D215/48 ,  C07D215/50 ,  C07D217/02 ,  C07D217/06 ,  C07D217/26 ,  C07D401/12 ,  C07D403/14 ,  C07D409/12 ,  C07D417/12 ,  C07D495/04 ,  C07F9/62

Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.

公开(公告)号：US07232912B2

公开(公告)日：2007-06-19

申请号：US11112423

申请日：2005-04-22

Applicant: Siegfried Heinz Reich ,  Ted Michael Bleckman ,  Susan Elizabeth Kephart ,  William Henry Romines, III ,  Michael Brennan Wallace

Inventor： Siegfried Heinz Reich ,  Ted Michael Bleckman ,  Susan Elizabeth Kephart ,  William Henry Romines, III ,  Michael Brennan Wallace

IPC: C07D235/04

CPC classification number: C07D249/08 ,  B22D41/56 ,  C07D231/12 ,  C07D231/56 ,  C07D233/56 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D471/04 ,  C07F7/1804

Abstract: Indazole compounds that modulate and/or inhibit cell proliferation, such as the activity of protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating, e.g., kinases-dependent diseases 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.

Abstract translation: 描述了调节和/或抑制细胞增殖的吲唑化合物，例如蛋白激酶的活性。 这些化合物和含有它们的药物组合物能够介导例如激酶依赖性疾病以调节和/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。