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公开(公告)号:US20140031360A1
公开(公告)日:2014-01-30
申请号:US13991603
申请日:2011-12-07
申请人: Hui-Ling Wang , Kaustav Biswas , Victor J. Cee , Frank Chavez, JR. , Bradley J. Herberich , Claire L.M. Jackson , Brian A. Lanman , Matthew Lee , Thomas Nixey , Liping H. Pettus , Anthony B. Reed , Robert M. Rzasa , Shannon Rumfelt , Andrew Tasker , Bin Wu , Ryan Wurz
发明人: Hui-Ling Wang , Kaustav Biswas , Victor J. Cee , Frank Chavez, JR. , Bradley J. Herberich , Claire L.M. Jackson , Brian A. Lanman , Matthew Lee , Thomas Nixey , Liping H. Pettus , Anthony B. Reed , Robert M. Rzasa , Shannon Rumfelt , Andrew Tasker , Bin Wu , Ryan Wurz
IPC分类号: C07D401/14 , C07D405/14 , C07D403/14 , C07D417/14 , C07D471/04 , C07D405/04
CPC分类号: C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要: The invention relates to bicyclic compounds of formula (1′), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.
摘要翻译: 本发明涉及式(1')的双环化合物及其盐。 在一些实施方案中,本发明涉及Pim-1和/或Pim-2和/或Pim-3蛋白激酶活性或酶功能的抑制剂或调节剂。 在另外的实施方案中,本发明涉及包含本文公开的化合物的药物组合物及其在预防和治疗Pim激酶相关病症和疾病,优选癌症中的用途。
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公开(公告)号:US09090593B2
公开(公告)日:2015-07-28
申请号:US13991603
申请日:2011-12-07
申请人: Hui-Ling Wang , Kaustav Biswas , Victor J. Cee , Frank Chavez, Jr. , Bradley J. Herberich , Claire L. M. Jackson , Brian A. Lanman , Matthew Lee , Thomas Nixey , Liping H. Pettus , Anthony B. Reed , Robert M. Rzasa , Shannon Rumfelt , Andrew Tasker , Bin Wu , Ryan Wurz
发明人: Hui-Ling Wang , Kaustav Biswas , Victor J. Cee , Frank Chavez, Jr. , Bradley J. Herberich , Claire L. M. Jackson , Brian A. Lanman , Matthew Lee , Thomas Nixey , Liping H. Pettus , Anthony B. Reed , Robert M. Rzasa , Shannon Rumfelt , Andrew Tasker , Bin Wu , Ryan Wurz
IPC分类号: C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D405/04
CPC分类号: C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要: The invention relates to bicyclic compounds of formula (1′), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.
摘要翻译: 本发明涉及式(1')的双环化合物及其盐。 在一些实施方案中,本发明涉及Pim-1和/或Pim-2和/或Pim-3蛋白激酶活性或酶功能的抑制剂或调节剂。 在另外的实施方案中,本发明涉及包含本文公开的化合物的药物组合物及其在预防和治疗Pim激酶相关病症和疾病,优选癌症中的用途。
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公开(公告)号:US20140187553A1
公开(公告)日:2014-07-03
申请号:US14006285
申请日:2012-03-21
申请人: Hui-Ling Wang , Victor J. Cee , Bradley J. Herberich , Claire L.M. Jackson , Brian Alan Lanman , Thomas Nixey , Liping H. Pettus , Anthony B. Reed , Bin Wu , Ryan Wurz , Andrew Tasker
发明人: Hui-Ling Wang , Victor J. Cee , Bradley J. Herberich , Claire L.M. Jackson , Brian Alan Lanman , Thomas Nixey , Liping H. Pettus , Anthony B. Reed , Bin Wu , Ryan Wurz , Andrew Tasker
IPC分类号: C07D413/14 , C07D487/04 , C07D417/04 , C07D471/04 , C07D417/14
CPC分类号: C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04
摘要: The invention relates to bicyclic compounds of formulas I and Ia, and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.
摘要翻译: 本发明涉及式I和Ia的双环化合物及其盐。 在一些实施方案中,本发明涉及Pim-1和/或Pim-2和/或Pim-3蛋白激酶活性或酶功能的抑制剂或调节剂。 在另外的实施方案中,本发明涉及包含本文公开的化合物的药物组合物及其在预防和治疗Pim激酶相关病症和疾病,优选癌症中的用途。
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公开(公告)号:US09321756B2
公开(公告)日:2016-04-26
申请号:US14006285
申请日:2012-03-21
申请人: Hui-Ling Wang , Victor J. Cee , Bradley J. Herberich , Claire L. M. Jackson , Brian Alan Lanman , Thomas Nixey , Liping H. Pettus , Anthony B. Reed , Bin Wu , Ryan Wurz , Andrew Tasker
发明人: Hui-Ling Wang , Victor J. Cee , Bradley J. Herberich , Claire L. M. Jackson , Brian Alan Lanman , Thomas Nixey , Liping H. Pettus , Anthony B. Reed , Bin Wu , Ryan Wurz , Andrew Tasker
IPC分类号: C07D413/14 , C07D487/04 , C07D417/04 , C07D471/04 , C07D417/14 , A61P35/00 , A61P35/02 , A61P35/04
CPC分类号: C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04
摘要: The invention relates to bicyclic compounds of formulas I and Ia, and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.
摘要翻译: 本发明涉及式I和Ia的双环化合物及其盐。 在一些实施方案中,本发明涉及Pim-1和/或Pim-2和/或Pim-3蛋白激酶活性或酶功能的抑制剂或调节剂。 在另外的实施方案中,本发明涉及包含本文公开的化合物的药物组合物及其在预防和治疗Pim激酶相关病症和疾病,优选癌症中的用途。
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公开(公告)号:US20140221344A1
公开(公告)日:2014-08-07
申请号:US14114481
申请日:2012-04-19
申请人: Derin C. D'amico , Bradley J. Herberich , Claire L.M. Jackson , Liping H. Pettus , Andrew Tasker , Hui-Ling Wang , Bin Wu , Ryan Wurz
发明人: Derin C. D'amico , Bradley J. Herberich , Claire L.M. Jackson , Liping H. Pettus , Andrew Tasker , Hui-Ling Wang , Bin Wu , Ryan Wurz
IPC分类号: C07D487/04
CPC分类号: C07D487/04
摘要: The invention relates to bicyclic compounds of formulas I and I′, and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.
摘要翻译: 本发明涉及式I和I'的双环化合物及其盐。 在一些实施方案中,本发明涉及Pim-1和/或Pim-2和/或Pim-3蛋白激酶活性或酶功能的抑制剂或调节剂。 在另外的实施方案中,本发明涉及包含本文公开的化合物的药物组合物及其在预防和治疗Pim激酶相关病症和疾病,优选癌症中的用途。
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公开(公告)号:US09187486B2
公开(公告)日:2015-11-17
申请号:US14114481
申请日:2012-04-19
申请人: Derin C. D'amico , Bradley J. Herberich , Claire L. M. Jackson , Liping H. Pettus , Andrew Tasker , Hui-Ling Wang , Bin Wu , Ryan Wurz
发明人: Derin C. D'amico , Bradley J. Herberich , Claire L. M. Jackson , Liping H. Pettus , Andrew Tasker , Hui-Ling Wang , Bin Wu , Ryan Wurz
IPC分类号: C07D487/04
CPC分类号: C07D487/04
摘要: The invention relates to bicyclic compounds of formulas I and I′, and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.
摘要翻译: 本发明涉及式I和I'的双环化合物及其盐。 在一些实施方案中,本发明涉及Pim-1和/或Pim-2和/或Pim-3蛋白激酶活性或酶功能的抑制剂或调节剂。 在另外的实施方案中,本发明涉及包含本文公开的化合物的药物组合物及其在预防和治疗Pim激酶相关病症和疾病,优选癌症中的用途。
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公开(公告)号:US08455495B2
公开(公告)日:2013-06-04
申请号:US13060663
申请日:2009-08-26
申请人: Liping H. Pettus , Andrew Tasker , Hui-Ling Wang , Bin Wu , Ryan Wurz
发明人: Liping H. Pettus , Andrew Tasker , Hui-Ling Wang , Bin Wu , Ryan Wurz
IPC分类号: A01N43/58 , A61K31/50 , C07D237/26
CPC分类号: C07D471/04
摘要: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A, R1, R2, R3, R4, R5, R6, X and n are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of p38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.
摘要翻译: 本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病,包括炎症和相关病症的化合物。 化合物具有通式I,其中A,R 1,R 2,R 3,R 4,R 5,R 6,X和n如本文所定义。 本发明还包括药物组合物,其包含一种或多种式I化合物,这些化合物和组合物用于治疗p38地图激酶介导的疾病包括类风湿性关节炎,银屑病,慢性阻塞性肺病,疼痛和其它炎性疾病以及中间体 和可用于制备式I化合物的方法。
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公开(公告)号:US20110275629A1
公开(公告)日:2011-11-10
申请号:US13060663
申请日:2009-08-26
申请人: Liping H. Pettus , Andrew Tasker , Hui-Ling Wang , Bin Wu , Ryan Wurz
发明人: Liping H. Pettus , Andrew Tasker , Hui-Ling Wang , Bin Wu , Ryan Wurz
IPC分类号: A61K31/5025 , C07D413/14 , A61K31/5377 , A61P19/08 , A61P19/10 , A61P35/00 , A61P27/02 , A61P35/02 , A61P5/48 , A61P19/02 , A61P29/00 , A61P19/06 , A61P11/00 , A61P1/00 , A61P37/08 , A61P25/00 , A61P17/00 , A61P11/06 , A61P21/00 , A61P3/10 , A61P37/06 , A61P25/28 , A61P9/10 , A61P31/00 , A61P31/18 , A61P31/16 , A61P31/14 , A61P31/22 , C07D471/04
CPC分类号: C07D471/04
摘要: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A, R1, R2, R3, R4, R5, R6, X and n are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of p38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.
摘要翻译: 本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病,包括炎症和相关病症的化合物。 化合物具有通式I,其中A,R 1,R 2,R 3,R 4,R 5,R 6,X和n如本文所定义。 本发明还包括药物组合物,其包含一种或多种式I化合物,这些化合物和组合物用于治疗p38地图激酶介导的疾病包括类风湿性关节炎,银屑病,慢性阻塞性肺病,疼痛和其它炎性疾病以及中间体 和可用于制备式I化合物的方法。
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公开(公告)号:US07332511B2
公开(公告)日:2008-02-19
申请号:US11195159
申请日:2005-08-01
申请人: Elizabeth M. Doherty , Jiawang Zhu , Markian Stec , Mark H. Norman , Hui-Ling Wang , Christopher H. Fotsch , Ning Chen , Partha P. Chakrabarti , Celia Dominguez , James Richard Falsey , Christopher Hulme , Jodie Katon , Thomas Nixey , Vassil I. Ognyanov , Liping H. Pettus , Robert Michael Rzasa
发明人: Elizabeth M. Doherty , Jiawang Zhu , Markian Stec , Mark H. Norman , Hui-Ling Wang , Christopher H. Fotsch , Ning Chen , Partha P. Chakrabarti , Celia Dominguez , James Richard Falsey , Christopher Hulme , Jodie Katon , Thomas Nixey , Vassil I. Ognyanov , Liping H. Pettus , Robert Michael Rzasa
IPC分类号: C07D213/30 , C07D213/32 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , A61K31/4427 , A61P19/02 , A61P35/00
CPC分类号: C07D231/40 , C07D209/08 , C07D209/12 , C07D209/42 , C07D209/48 , C07D213/26 , C07D213/643 , C07D213/74 , C07D213/75 , C07D215/227 , C07D215/38 , C07D217/04 , C07D231/56 , C07D233/38 , C07D239/42 , C07D239/90 , C07D241/42 , C07D263/56 , C07D265/36 , C07D277/62 , C07D277/82 , C07D307/79 , C07D319/20 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/14 , C07D413/12 , C07D417/12
摘要: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.
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公开(公告)号:US07144888B2
公开(公告)日:2006-12-05
申请号:US10638009
申请日:2003-08-08
申请人: Elizabeth M. Doherty , Jiawang Zhu , Markian Stec , Mark H. Norman , Hui-Ling Wang , Christopher H. Fotsch , Ning Chen , Partha P. Chakrabarti , Celia Dominguez , James Richard Falsey , Christopher Hulme , Jodie Katon , Thomas Nixey , Vassil I. Ognyanov , Liping H. Pettus , Robert Michael Rzasa
发明人: Elizabeth M. Doherty , Jiawang Zhu , Markian Stec , Mark H. Norman , Hui-Ling Wang , Christopher H. Fotsch , Ning Chen , Partha P. Chakrabarti , Celia Dominguez , James Richard Falsey , Christopher Hulme , Jodie Katon , Thomas Nixey , Vassil I. Ognyanov , Liping H. Pettus , Robert Michael Rzasa
IPC分类号: C07D239/34 , C07D239/38 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , A61K31/505 , A61K31/506 , A61K31/4427 , A61P19/02 , A61P25/06
CPC分类号: C07D231/40 , C07D209/08 , C07D209/12 , C07D209/42 , C07D209/48 , C07D213/26 , C07D213/643 , C07D213/74 , C07D213/75 , C07D215/227 , C07D215/38 , C07D217/04 , C07D231/56 , C07D233/38 , C07D239/42 , C07D239/90 , C07D241/42 , C07D263/56 , C07D265/36 , C07D277/62 , C07D277/82 , C07D307/79 , C07D319/20 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/14 , C07D413/12 , C07D417/12
摘要: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.
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