公开(公告)号：US20070185133A1

公开(公告)日：2007-08-09

申请号：US11304901

申请日：2005-12-16

申请人： Adrian Smith ,  Paul Brennan ,  Frenel DeMorin ,  Gang Liu ,  Nick Paras ,  Daniel Retz ,  Elizabeth Rainbeau

发明人： Adrian Smith ,  Paul Brennan ,  Frenel DeMorin ,  Gang Liu ,  Nick Paras ,  Daniel Retz ,  Elizabeth Rainbeau

IPC分类号： A61K31/513 ,  A61K31/506 ,  C07D417/14

CPC分类号： C07D417/14 ,  C07D409/14

摘要： The invention relates to aminopyrimidine compounds useful for treating diseases mediated by polo-like kinase 1 (Plk1). The invention also relates to the therapeutic use of such aminopyrimidine compounds and compositions thereof in treating disease states associated with abnormal cell growth and unwanted cell proliferation.

摘要翻译： 本发明涉及可用于治疗由polo样激酶1（Plk1）介导的疾病的氨基嘧啶化合物。 本发明还涉及这种氨基嘧啶化合物及其组合物在治疗与异常细胞生长和不想要的细胞增殖相关的疾病状态中的治疗用途。

公开(公告)号：US20070185324A1

公开(公告)日：2007-08-09

申请号：US11643261

申请日：2006-12-20

申请人： Frenel De Morin ,  Jian Chen ,  Elizabeth Doherty ,  Stephen Hitchcock ,  Qi Huang ,  Joseph Kim ,  Gang Liu ,  Thomas Nixey ,  Nick Paras ,  Jeffrey Petkus ,  Daniel Retz ,  Adrian Smith ,  Andrew Tasker ,  Jiawang Zhu

发明人： Frenel De Morin ,  Jian Chen ,  Elizabeth Doherty ,  Stephen Hitchcock ,  Qi Huang ,  Joseph Kim ,  Gang Liu ,  Thomas Nixey ,  Nick Paras ,  Jeffrey Petkus ,  Daniel Retz ,  Adrian Smith ,  Andrew Tasker ,  Jiawang Zhu

IPC分类号： A61K31/541 ,  A61K31/5377 ,  C07D417/02 ,  C07D403/02

CPC分类号： C07D401/14 ,  C07D239/84 ,  C07D239/95 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

摘要： The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula I wherein R1 is and A1, A2, A3, A4, X, Z, Z′, R1, R2, R3, R4, R5 and R6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.

摘要翻译： 本发明包括能够调节Raf激酶的新一类化合物，因此可用于治疗Raf激酶介导的疾病，包括黑素瘤，肿瘤和其它癌症相关病症。 这些化合物具有通式I，其中R 1是和A 1，A 2，A 3，A 3， X，Z，Z'，R 1，R 2，R 3，R 3， 本文定义了R 5，R 5和R 6。 本发明还包括药物组合物，用于治疗Raf激酶介导的疾病的方法，以及可用于制备本发明化合物的中间体和方法。

公开(公告)号：US20060235036A1

公开(公告)日：2006-10-19

申请号：US11406437

申请日：2006-04-17

申请人： Elizabeth Doherty ,  Hongyu Liao ,  Mark Norman ,  Daniel Retz

发明人： Elizabeth Doherty ,  Hongyu Liao ,  Mark Norman ,  Daniel Retz

IPC分类号： A61K31/506 ,  A61K31/501 ,  C07D403/14

CPC分类号： C07D417/14 ,  C07D401/14 ,  C07D403/12

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.

公开(公告)号：US20060241296A1

公开(公告)日：2006-10-26

申请号：US11411366

申请日：2006-04-25

申请人： Elizabeth Doherty ,  Jodie Katon ,  Mark Norman ,  Daniel Retz ,  Xianghong Wang ,  Yunxin Bo ,  Nuria Tamayo ,  Nobuko Nishimura ,  Hongyu Liao

发明人： Elizabeth Doherty ,  Jodie Katon ,  Mark Norman ,  Daniel Retz ,  Xianghong Wang ,  Yunxin Bo ,  Nuria Tamayo ,  Nobuko Nishimura ,  Hongyu Liao

IPC分类号： A61K31/506 ,  C07D403/02

CPC分类号： C07D413/04 ,  C07D213/74 ,  C07D239/42 ,  C07D239/48 ,  C07D401/04 ,  C07D403/12 ,  C07D405/14

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.

公开(公告)号：US20060069110A1

公开(公告)日：2006-03-30

申请号：US11237513

申请日：2005-09-27

申请人： Denise Andersen ,  Catherine Chang ,  James Falsey ,  Michael Frohn ,  Fang-Tsao Hong ,  Hongyu Liao ,  Longbin Liu ,  Patricia Lopez ,  Daniel Retz ,  Gilbert Rishton ,  Robert Rzasa ,  Aaron Siegmund ,  Seifu Tadesse ,  Nuria Tamayo ,  Christopher Tegley

发明人： Denise Andersen ,  Catherine Chang ,  James Falsey ,  Michael Frohn ,  Fang-Tsao Hong ,  Hongyu Liao ,  Longbin Liu ,  Patricia Lopez ,  Daniel Retz ,  Gilbert Rishton ,  Robert Rzasa ,  Aaron Siegmund ,  Seifu Tadesse ,  Nuria Tamayo ,  Christopher Tegley

IPC分类号： A61K31/506 ,  C07D403/14 ,  C07D403/04

CPC分类号： C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14

摘要： The present invention relates to pyridines, pyrimidines and derivatives thereof, and pharmaceutically acceptable salts thereof. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic β cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer's disease, stroke, myocardial infarction, ischemia reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, myalgias due to HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses or herpes zoster infection in a mammal comprising administering an effective amount a compound as described above.

摘要翻译： 本发明涉及吡啶，嘧啶及其衍生物及其药学上可接受的盐。 还包括治疗炎症，类风湿性关节炎，斑节病，骨质疏松症，多发性骨髓瘤，葡萄膜炎，急性或慢性骨髓性白血病，胰腺β细胞破坏，骨关节炎，类风湿性脊椎炎，痛风性关节炎，炎性肠病，成人呼吸窘迫综合征 （ARDS），牛皮癣，克罗恩病，过敏性鼻炎，溃疡性结肠炎，过敏反应，接触性皮炎，哮喘，肌肉变性，恶病质，赖特综合征，I型糖尿病，II型糖尿病，骨吸收疾病，移植物抗宿主反应，阿尔茨海默病 ，中风，心肌梗塞，缺血再灌注损伤，动脉粥样硬化，脑外伤，多发性硬化，脑疟疾，败血症，败血性休克，中毒性休克综合征，发热，HIV-1，HIV-2，HIV-3，巨细胞病毒 ），流感病毒，腺病毒，哺乳动物中的疱疹病毒或带状疱疹感染，包括给予有效量的如上所述的化合物。