公开(公告)号：US20060241151A1

公开(公告)日：2006-10-26

申请号：US11415454

申请日：2006-05-02

申请人： Wenge Zhong ,  Mark Norman ,  Matthew Kaller ,  Thomas Nguyen ,  Robert Rzasa ,  Christopher Tegley ,  Hui-Ling Wang

发明人： Wenge Zhong ,  Mark Norman ,  Matthew Kaller ,  Thomas Nguyen ,  Robert Rzasa ,  Christopher Tegley ,  Hui-Ling Wang

IPC分类号： A61K31/4439 ,  C07D417/02

CPC分类号： C07D417/14 ,  C07D417/04 ,  C07D471/04 ,  C07D491/04

摘要： Selected compounds are effective for treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving stroke, cancer and the like. The subject invention also realtes to processes for making such compounds as well as to intermediates useful in such processes.

摘要翻译： 选择的化合物对于治疗疾病如细胞增殖或细胞凋亡介导的疾病是有效的。 本发明包括新型化合物，类似物，前药及其药学上可接受的衍生物，用于预防和治疗疾病和其它疾病或涉及中风，癌症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

公开(公告)号：US20070032518A1

公开(公告)日：2007-02-08

申请号：US10936538

申请日：2004-09-09

申请人： Mark Norman ,  Hui-Ling Wang ,  Robert Rzasa ,  Wenge Zhong ,  Thomas Nguyen ,  Matthew Kaller ,  Hu Liu

发明人： Mark Norman ,  Hui-Ling Wang ,  Robert Rzasa ,  Wenge Zhong ,  Thomas Nguyen ,  Matthew Kaller ,  Hu Liu

IPC分类号： C07D471/02 ,  C07D491/02 ,  C07D498/02

CPC分类号： C07D417/14 ,  C07D471/04 ,  C07D491/04 ,  C07D513/04

摘要： Selected compounds are effective for treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving stroke, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

摘要翻译： 选择的化合物对于治疗疾病如细胞增殖或细胞凋亡介导的疾病是有效的。 本发明包括新型化合物，类似物，前药及其药学上可接受的衍生物，用于预防和治疗疾病和其它疾病或涉及中风，癌症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

公开(公告)号：US07119111B2

公开(公告)日：2006-10-10

申请号：US10446440

申请日：2003-05-27

申请人： Qi Huang ,  Matthew Kaller ,  Thomas Nguyen ,  Mark H. Norman ,  Robert Rzasa ,  Hui-Ling Wang ,  Wenge Zhong

发明人： Qi Huang ,  Matthew Kaller ,  Thomas Nguyen ,  Mark H. Norman ,  Robert Rzasa ,  Hui-Ling Wang ,  Wenge Zhong

IPC分类号： C07D277/60 ,  C07D487/00 ,  A01N43/78

CPC分类号： C07D417/14 ,  C07D403/04 ,  C07D409/14 ,  C07D417/04 ,  C07D471/04 ,  C07D491/04 ,  C07D513/04

摘要： Selected compounds are effective for treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving stroke, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

公开(公告)号：US06822097B1

公开(公告)日：2004-11-23

申请号：US10360226

申请日：2003-02-06

申请人： Mark H. Norman ,  Hui-Ling Wang ,  Robert Rzasa ,  Wenge Zhong ,  Thomas Nguyen ,  Matthew Kaller ,  Hu Liu

发明人： Mark H. Norman ,  Hui-Ling Wang ,  Robert Rzasa ,  Wenge Zhong ,  Thomas Nguyen ,  Matthew Kaller ,  Hu Liu

IPC分类号： C07D21516

CPC分类号： C07D417/14 ,  C07D471/04 ,  C07D491/04 ,  C07D513/04

摘要： Selected compounds are effective for treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving stroke, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

摘要翻译： 选择的化合物对于治疗疾病如细胞增殖或细胞凋亡介导的疾病是有效的。 本发明包括新型化合物，类似物，前药及其药学上可接受的衍生物，用于预防和治疗疾病和其它疾病或涉及中风，癌症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

公开(公告)号：US20050277631A1

公开(公告)日：2005-12-15

申请号：US11195134

申请日：2005-08-01

申请人： Elizabeth Doherty ,  Jiawang Zhu ,  Markian Stec ,  Mark Norman ,  Hui-Ling Wang ,  Christopher Fotsch ,  Ning Chen ,  Partha Chakrabarti ,  Celia Dominguez ,  James Falsey ,  Christopher Hulme ,  Jodie Katon ,  Thomas Nixey ,  Vassil Ognyanov ,  Liping Pettus ,  Robert Rzasa

发明人： Elizabeth Doherty ,  Jiawang Zhu ,  Markian Stec ,  Mark Norman ,  Hui-Ling Wang ,  Christopher Fotsch ,  Ning Chen ,  Partha Chakrabarti ,  Celia Dominguez ,  James Falsey ,  Christopher Hulme ,  Jodie Katon ,  Thomas Nixey ,  Vassil Ognyanov ,  Liping Pettus ,  Robert Rzasa

IPC分类号： A61P29/00 ,  C07D209/08 ,  C07D209/12 ,  C07D209/42 ,  C07D209/48 ,  C07D213/26 ,  C07D213/64 ,  C07D213/643 ,  C07D213/74 ,  C07D213/75 ,  C07D215/22 ,  C07D215/227 ,  C07D215/38 ,  C07D217/04 ,  C07D231/40 ,  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 ,  A61K31/549 ,  A61K31/501 ,  C07D417/02 ,  C07D43/02

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.

公开(公告)号：US20050272777A1

公开(公告)日：2005-12-08

申请号：US11195159

申请日：2005-08-01

申请人： Elizabeth Doherty ,  Jiawang Zhu ,  Markian Stec ,  Mark Norman ,  Hui-Ling Wang ,  Christopher Fotsch ,  Ning Chen ,  Partha Chakrabarti ,  Celia Dominguez ,  James Falsey ,  Christopher Hulme ,  Jodie Katon ,  Thomas Nixey ,  Vassil Ognyanov ,  Liping Pettus ,  Robert Rzasa

发明人： Elizabeth Doherty ,  Jiawang Zhu ,  Markian Stec ,  Mark Norman ,  Hui-Ling Wang ,  Christopher Fotsch ,  Ning Chen ,  Partha Chakrabarti ,  Celia Dominguez ,  James Falsey ,  Christopher Hulme ,  Jodie Katon ,  Thomas Nixey ,  Vassil Ognyanov ,  Liping Pettus ,  Robert Rzasa

IPC分类号： A61P29/00 ,  C07D209/08 ,  C07D209/12 ,  C07D209/42 ,  C07D209/48 ,  C07D213/26 ,  C07D213/64 ,  C07D213/643 ,  C07D213/74 ,  C07D213/75 ,  C07D215/22 ,  C07D215/227 ,  C07D215/38 ,  C07D217/04 ,  C07D231/40 ,  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 ,  A61K31/4439 ,  C07D417/02

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.

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。

公开(公告)号：US20060089360A1

公开(公告)日：2006-04-27

申请号：US11256427

申请日：2005-10-21

申请人： Mark Norman ,  Vassil Ognyanov ,  Robert Rzasa

发明人： Mark Norman ,  Vassil Ognyanov ,  Robert Rzasa

IPC分类号： A61K31/506 ,  C07D403/02 ,  C07D405/02

CPC分类号： C07D401/04 ,  C07D403/04 ,  C07D405/04

摘要： Substituted nitrogen-containing heterocycles 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.

摘要翻译： 取代的含氮杂环和含有它们的组合物，用于治疗急性，炎性和神经性疼痛，牙痛，一般头痛，偏头痛，丛集性头痛，混合血管和非血管性综合征，紧张性头痛，一般炎症，关节炎，风湿 疾病，骨关节炎，炎症性肠病，炎症性眼病，炎症性或不稳定性膀胱病，银屑病，皮肤炎症成分炎症，慢性炎性病症，炎性疼痛及相关的痛觉过敏和异常性疼痛，神经性疼痛及相关的痛觉过敏和异常性疼痛，糖尿病性神经病疼痛， 咳嗽痛，交感神经痛，交感综合征，哮喘，上皮组织损伤或功能障碍，单纯疱疹，呼吸道内脏运动紊乱，泌尿生殖道，胃肠道或血管区，伤口，烧伤，过敏性皮肤反应，瘙痒，白癜风，一般胃肠道紊乱 胃溃疡，十二指肠溃疡，腹泻，坏死因子诱导的胃损伤，毛发生长，血管舒缩或过敏性鼻炎，支气管疾病或膀胱疾病。

公开(公告)号：US20080032988A1

公开(公告)日：2008-02-07

申请号：US11789189

申请日：2007-04-23

申请人： Fang-Tsao Hong ,  James Falsey ,  Robert Rzasa ,  Seifu Tadesse ,  Andrew Tasker

发明人： Fang-Tsao Hong ,  James Falsey ,  Robert Rzasa ,  Seifu Tadesse ,  Andrew Tasker

IPC分类号： A61K31/50 ,  A61P19/02 ,  C07D237/00

CPC分类号： C07D495/04

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 A1, A2, B, R2 and R3 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 kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation 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 1，A 2，B，R 2和R 3是 本文定义。 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激酶介导的疾病包括类风湿性关节炎，牛皮癣和其它炎症疾病的用途，以及可用于制备 一级方程式

公开(公告)号：US20070054916A1

公开(公告)日：2007-03-08

申请号：US11240590

申请日：2005-09-30

申请人： Vinod Patel ,  Joseph Kim ,  Stephanie Geuns-Meyer ,  Stuart Chaffee ,  Victor Cee ,  Brian Hodous ,  Steven Bellon ,  Jean-Christophe Harmange ,  Philip Olivieri ,  Maya Thaman ,  Erin DiMauro ,  John Buchanan ,  David McGowan ,  Brian Albrecht ,  Holly Deak ,  Jean Bemis ,  Ryan White ,  Matthew Martin ,  Gregory Habgood ,  Paul Tempest ,  Craig Masse ,  William Buckner ,  Bradley Herberich ,  Russell Graceffa ,  Dawei Zhang ,  Shimin Xu ,  Kelvin Sham ,  Robert Rzasa ,  James Falsey ,  Partha Chakrabarti ,  Guo-Qiang Cao ,  Susan Tomlinson ,  Liping Pettus ,  Adrian Smith ,  Nick Paras ,  Gang Liu ,  Frenel DeMorin ,  Andrew Tasker ,  Anthony Reed

发明人： Vinod Patel ,  Joseph Kim ,  Stephanie Geuns-Meyer ,  Stuart Chaffee ,  Victor Cee ,  Brian Hodous ,  Steven Bellon ,  Jean-Christophe Harmange ,  Philip Olivieri ,  Maya Thaman ,  Erin DiMauro ,  John Buchanan ,  David McGowan ,  Brian Albrecht ,  Holly Deak ,  Jean Bemis ,  Ryan White ,  Matthew Martin ,  Gregory Habgood ,  Paul Tempest ,  Craig Masse ,  William Buckner ,  Bradley Herberich ,  Russell Graceffa ,  Dawei Zhang ,  Shimin Xu ,  Kelvin Sham ,  Robert Rzasa ,  James Falsey ,  Partha Chakrabarti ,  Guo-Qiang Cao ,  Susan Tomlinson ,  Liping Pettus ,  Adrian Smith ,  Nick Paras ,  Gang Liu ,  Frenel DeMorin ,  Andrew Tasker ,  Anthony Reed

IPC分类号： A61K31/525 ,  A61K31/519 ,  A61K31/517

CPC分类号： C07D215/38 ,  C07C205/37 ,  C07D215/12 ,  C07D217/12 ,  C07D217/22 ,  C07D217/26 ,  C07D239/26 ,  C07D239/84 ,  C07D239/94 ,  C07D239/95 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

摘要： The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I wherein A1, A2, A3, B, R1, R2, R3 and R4 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.

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，癌症和相关病症的化合物。 化合物具有通式I，其中A 1，A 2，A 3，B，R 1， R 2，R 3和R 4在本文中定义。 因此，本发明还包括含有本发明化合物的药物组合物，使用本发明化合物和组合物预防和治疗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。