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：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：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：US06469021B1

公开(公告)日：2002-10-22

申请号：US09831572

申请日：2001-10-26

申请人： Larry Kenneth Truesdale ,  Richard A. Bychowski ,  Javier Gonzalez ,  Atsuo Kuki ,  Ranjan Jagath Rajapakse ,  Min Teng ,  Dan Kiel ,  Daljit S. Dhanoa ,  Yufeng Hong ,  Tso-sheng Chou ,  Anthony L. Ling ,  Michael David Johnson ,  Vlad Edward Gregor

发明人： Larry Kenneth Truesdale ,  Richard A. Bychowski ,  Javier Gonzalez ,  Atsuo Kuki ,  Ranjan Jagath Rajapakse ,  Min Teng ,  Dan Kiel ,  Daljit S. Dhanoa ,  Yufeng Hong ,  Tso-sheng Chou ,  Anthony L. Ling ,  Michael David Johnson ,  Vlad Edward Gregor

IPC分类号： A61K31437

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D471/04 ,  C07D471/14 ,  C07D491/04 ,  C07D491/14

摘要： Non-peptide compounds that act as antagonists of the intestinal hormone glucagons-like peptide 1 (GLP-1) have a 9H-b-carboline central motif. The compounds exhibit advantageous physical, chemical and biological properties and inhibit GLP-1 peptide binding to the GLP-1 receptor and/or prevent activation of the receptor by bound GLP-1. The invention further relates to a method of inhibiting the binding of GLP-1 to the GLP-1 receptor and a method of inhibiting the activation of the GLP-1 receptor. Intermediate compounds useful for making non-peptide GLP-1 receptor antagonists are also described.

摘要翻译： 作为肠激素胰高血糖素样肽1（GLP-1）的拮抗剂的非肽化合物具有9H-b-咔啉中心基序。 该化合物表现出有利的物理，化学和生物学特性，并且抑制GLP-1肽与GLP-1受体的结合和/或通过结合的GLP-1阻止受体活化。 本发明还涉及抑制GLP-1与GLP-1受体结合的方法以及抑制GLP-1受体活化的方法。 还描述了可用于制备非肽GLP-1受体拮抗剂的中间体化合物。

公开(公告)号：US06613942B1

公开(公告)日：2003-09-02

申请号：US09220003

申请日：1998-12-23

申请人： Anthony Ling ,  Vlad Gregor ,  Javier Gonzalez ,  Yufeng Hong ,  Dan Kiel ,  Atsuo Kuki ,  Shenghua Shi ,  Lars Naerum ,  Peter Madsen ,  Christian Sams ,  Jesper Lau ,  Michael Bruno Plewe ,  Jun Feng ,  Min Teng ,  Michael David Johnson ,  Kimberly Ann Teston ,  Ulla Grove Sidelmann ,  Lotte Bjerre Knudsen

发明人： Anthony Ling ,  Vlad Gregor ,  Javier Gonzalez ,  Yufeng Hong ,  Dan Kiel ,  Atsuo Kuki ,  Shenghua Shi ,  Lars Naerum ,  Peter Madsen ,  Christian Sams ,  Jesper Lau ,  Michael Bruno Plewe ,  Jun Feng ,  Min Teng ,  Michael David Johnson ,  Kimberly Ann Teston ,  Ulla Grove Sidelmann ,  Lotte Bjerre Knudsen

IPC分类号： C07C23300

CPC分类号： C07D295/192 ,  C07C251/86 ,  C07C255/29 ,  C07C271/12 ,  C07C271/22 ,  C07C271/24 ,  C07C271/28 ,  C07C309/65 ,  C07C311/16 ,  C07C311/20 ,  C07C311/49 ,  C07C317/28 ,  C07C323/45 ,  C07C323/60 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07D209/08 ,  C07D209/48 ,  C07D209/86 ,  C07D213/30 ,  C07D213/80 ,  C07D215/12 ,  C07D215/26 ,  C07D231/12 ,  C07D295/135 ,  C07D295/185 ,  C07D295/26 ,  C07D307/12 ,  C07D307/52 ,  C07D307/84 ,  C07D309/06 ,  C07D317/58 ,  C07D333/24 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06

摘要： Non-peptide compounds comprising a central hydrazide motif and methods for the synthesis thereof are disclosed. The compounds act to antagonize the action of the glucagon peptide hormone.

摘要翻译： 公开了包含中心酰肼基序的非肽化合物及其合成方法。 该化合物起拮抗胰高血糖素肽激素的作用。

公开(公告)号：US06927214B1

公开(公告)日：2005-08-09

申请号：US09483504

申请日：2000-01-14

申请人： Min Teng ,  Larry Kenneth Truesdale ,  Dilip Bhumralkar ,  Dan Kiel ,  Michael D. Johnson ,  Christine Thomas ,  Anker Steen Jorgensen ,  Peter Madsen ,  Preben Houlberg Olesen ,  Liselotte Bjerre Knudsen ,  Ingrid Vivika Petterson ,  Johannes Cornelis de Jong ,  Carsten Behrens ,  Janos Tibor Kodra ,  Jesper Lau

发明人： Min Teng ,  Larry Kenneth Truesdale ,  Dilip Bhumralkar ,  Dan Kiel ,  Michael D. Johnson ,  Christine Thomas ,  Anker Steen Jorgensen ,  Peter Madsen ,  Preben Houlberg Olesen ,  Liselotte Bjerre Knudsen ,  Ingrid Vivika Petterson ,  Johannes Cornelis de Jong ,  Carsten Behrens ,  Janos Tibor Kodra ,  Jesper Lau

IPC分类号： C07D215/20 ,  C07D215/36 ,  C07D241/44 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D417/12 ,  C07D491/10 ,  C07D495/04 ,  A61K31/33 ,  A61K31/495 ,  C07D239/00 ,  C07D241/36

CPC分类号： C07D491/10 ,  C07D215/20 ,  C07D215/36 ,  C07D241/44 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D417/12 ,  C07D495/04

摘要： Novel non-peptide GLP-1 agonists, pharmaceutical compositions comprising them, use of the non-peptide GLP-1 agonists for the preparation of pharmaceutical compositions and methods for the treatment and/or prevention of disorders and diseases wherein an activation of the human GLP-1 receptor is beneficial, especially metabolic disorders such as IGT, Type 1 diabetes, Type 2 diabetes and obesity.

摘要翻译： 新型非肽GLP-1激动剂，包含它们的药物组合物，使用非肽GLP-1激动剂来制备用于治疗和/或预防疾病和疾病的药物组合物和方法，其中人GLP -1受体是有益的，特别是代谢疾病如IGT，1型糖尿病，2型糖尿病和肥胖。

公开(公告)号：US08999981B2

公开(公告)日：2015-04-07

申请号：US13345528

申请日：2012-01-06

申请人： Iriny Botrous ,  Yufeng Hong ,  Hui Li ,  Kevin Kun-Chin Liu ,  Seiji Nukui ,  Min Teng ,  Eileen Valenzuela Tompkins ,  Chunfeng Yin

发明人： Iriny Botrous ,  Yufeng Hong ,  Hui Li ,  Kevin Kun-Chin Liu ,  Seiji Nukui ,  Min Teng ,  Eileen Valenzuela Tompkins ,  Chunfeng Yin

IPC分类号： A61K31/5377 ,  A61K31/495 ,  A61K31/499 ,  A61K31/497 ,  C07D413/14 ,  C07D237/02 ,  C07D239/02 ,  C07D241/02 ,  C07D241/36 ,  C07D239/70 ,  C07D403/14 ,  C07D401/14 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.

摘要翻译： 本发明涉及式（I）的化合物和药学上可接受的盐：其中X，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8如上所定义。 本发明还涉及包含该化合物和药学上可接受的盐的药物组合物以及治疗糖尿病及其并发症（特别是糖尿病性视网膜病变，肾病或神经病变），癌症，缺血，炎症，中枢神经系统疾病，心血管疾病， 阿尔茨海默病和皮肤病疾病，病毒性疾病，炎症性疾病或肝脏是靶器官的疾病。

公开(公告)号：US20100249128A1

公开(公告)日：2010-09-30

申请号：US12532051

申请日：2008-04-10

申请人： Iriny Botrous ,  Yufeng Hong ,  Hui Li ,  Kevin Kun-Chin Liu ,  Seiji Nukui ,  Min Teng ,  Eileen Valenzuela Tompkins ,  Chunfeng Yin

发明人： Iriny Botrous ,  Yufeng Hong ,  Hui Li ,  Kevin Kun-Chin Liu ,  Seiji Nukui ,  Min Teng ,  Eileen Valenzuela Tompkins ,  Chunfeng Yin

IPC分类号： A61K31/4985 ,  C07D487/04 ,  A61K31/499 ,  A61K31/496 ,  C07D471/04 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61P3/10 ,  A61P9/10 ,  A61P9/00 ,  A61P17/00 ,  A61P25/28 ,  A61P35/00 ,  A61P29/00 ,  A61P31/12 ,  A61P1/16 ,  A61P25/00

CPC分类号： C07D487/04

摘要： The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.

摘要翻译： 本发明涉及式（I）的化合物和药学上可接受的盐：其中X，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8如上所定义。 本发明还涉及包含该化合物和药学上可接受的盐的药物组合物以及治疗糖尿病及其并发症（特别是糖尿病性视网膜病变，肾病或神经病变），癌症，缺血，炎症，中枢神经系统疾病，心血管疾病， 阿尔茨海默病和皮肤病疾病，病毒性疾病，炎症性疾病或肝脏是靶器官的疾病。

公开(公告)号：US20050043381A1

公开(公告)日：2005-02-24

申请号：US10897849

申请日：2004-07-22

申请人： Michael Johnson ,  Min Teng ,  Jinjiang Zhu

发明人： Michael Johnson ,  Min Teng ,  Jinjiang Zhu

IPC分类号： A61P35/00 ,  C07D231/38 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  A61K31/425 ,  C07D275/02

CPC分类号： C04B35/632 ,  C07D231/38 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12

摘要： Described herein are aminopyrazole compounds of formula I: wherein R1, R2, L and Ar are as defined in the specification. Such compounds are capable of modulating the activity of a checkpoint kinase and methods for utilizing such modulation to treat cell proliferative disorders. Also described are pharmaceutical compositions containing such compounds. Also described are the therapeutic or prophylactic use of such compounds and compositions, and methods of treating cancer as well as other diseases associated with unwanted cellular proliferation, by administering effective amounts of such compounds in combination with anti-neoplastic agents.

摘要翻译： 本文描述的是式I的氨基吡唑化合物：其中R 1，R 2，L和Ar如说明书中所定义。 这些化合物能够调节检查点激酶的活性和利用这种调节来治疗细胞增殖性疾病的方法。 还描述了含有这些化合物的药物组合物。 还描述了这样的化合物和组合物的治疗或预防用途，以及通过与抗肿瘤剂组合施用有效量的这种化合物来治疗癌症以及与不想要的细胞增殖相关的其它疾病的方法。