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公开(公告)号:US20090163489A1
公开(公告)日:2009-06-25
申请号:US12317166
申请日:2008-12-18
申请人: Shon Booker , Tae-Seong Kim , Hongyu Liao , Longbin Liu , Mark H. Norman , Emily Anne Peterson , Markian Stec , Nuria A. Tamayo
发明人: Shon Booker , Tae-Seong Kim , Hongyu Liao , Longbin Liu , Mark H. Norman , Emily Anne Peterson , Markian Stec , Nuria A. Tamayo
IPC分类号: A61K31/5025 , C07D487/04 , A61K31/5377 , A61P35/02 , A61P35/00 , C07D413/14
CPC分类号: C07D471/04 , C07D487/04
摘要: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof, that inhibit phosphoinositide 3-kinase; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds.
摘要翻译: 本发明涉及抑制磷酸肌醇3-激酶的式I化合物或其药学上可接受的盐; 使用该化合物治疗疾病或病症如癌症的方法; 和含有这些化合物的药物组合物。
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公开(公告)号:US07820665B2
公开(公告)日:2010-10-26
申请号:US12317166
申请日:2008-12-18
申请人: Shon Booker , Tae-Seong Kim , Hongyu Liao , Longbin Liu , Mark H. Norman , Emily Anne Peterson , Markian Stec , Nuria A. Tamayo
发明人: Shon Booker , Tae-Seong Kim , Hongyu Liao , Longbin Liu , Mark H. Norman , Emily Anne Peterson , Markian Stec , Nuria A. Tamayo
IPC分类号: A61K31/4188 , A61K31/5025 , C07D487/04
CPC分类号: C07D471/04 , C07D487/04
摘要: The present invention relates to imidazopyridazine compounds of Formula I, such as representative structure A, or a pharmaceutically acceptable salt thereof, that inhibit phosphoinositide 3-kinase; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds.
摘要翻译: 本发明涉及式I的咪唑并哒嗪化合物,例如抑制磷酸肌醇3-激酶的代表性结构A或其药学上可接受的盐; 使用该化合物治疗疾病或病症如癌症的方法; 和含有这些化合物的药物组合物。
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公开(公告)号:US20100273764A1
公开(公告)日:2010-10-28
申请号:US12768602
申请日:2010-04-27
申请人: Kristin Andrews , Yunxin Y. Bo , Shon Booker , Victor J. Cee , Noel D'Angelo , Bradley J. Herberich , Fang-Tsao Hong , Claire L.M. Jackson , Brian A. Lanman , Hongyu Liao , Longbin Liu , Nobuko Nishimura , Mark H. Norman , Liping H. Pettus , Anthony B. Reed , Adrian L. Smith , Seifu Tadesse , Nuria A. Tamayo , Bin Wu , Ryan Wurz , Kevin Yang
发明人: Kristin Andrews , Yunxin Y. Bo , Shon Booker , Victor J. Cee , Noel D'Angelo , Bradley J. Herberich , Fang-Tsao Hong , Claire L.M. Jackson , Brian A. Lanman , Hongyu Liao , Longbin Liu , Nobuko Nishimura , Mark H. Norman , Liping H. Pettus , Anthony B. Reed , Adrian L. Smith , Seifu Tadesse , Nuria A. Tamayo , Bin Wu , Ryan Wurz , Kevin Yang
IPC分类号: A61K31/53 , C07D473/00 , A61K31/52 , C07D401/14 , A61K31/506 , C07D413/14 , A61K31/5377 , C07D401/04 , C07D417/14 , C07D405/14 , A61K31/541 , C07D471/04 , C07D401/12 , C07D513/04 , A61P35/00 , A61P35/02
CPC分类号: C07D473/00 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.
摘要翻译: 本发明涉及式I化合物或其药学上可接受的盐; 使用该化合物治疗疾病或病症如癌症的方法; 和含有这些化合物的药物组合物,其中变量如本文所定义。
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公开(公告)号:US07301022B2
公开(公告)日:2007-11-27
申请号:US11354650
申请日:2006-02-15
申请人: Yunxin Y. Bo , Partha P. Chakrabarti , Ning Chen , Hongyu Liao , Mark H. Norman , Markian Stec , Nuria Tamayo , Xianghong Wang
发明人: Yunxin Y. Bo , Partha P. Chakrabarti , Ning Chen , Hongyu Liao , Mark H. Norman , Markian Stec , Nuria Tamayo , Xianghong Wang
IPC分类号: C07D239/34 , C07D239/38 , C07D237/14 , C07D237/18 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , A61K31/505 , A61K31/506 , A61K31/4427 , A61P19/02 , A61P35/00
CPC分类号: C07D403/14 , C07D401/14 , C07D417/12 , C07D417/14
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.
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公开(公告)号:US20120190666A1
公开(公告)日:2012-07-26
申请号:US13319683
申请日:2010-05-12
申请人: Christiane Bode , Alessandro Boezio , Alan C. Cheng , Deborah Choquette , James Robert Coats , Katrina Woodin Copeland , Hongbing Huang , Daniel La , Richard Thomas Lewis , Hongyu Liao , Michele Potashman , John Stellwagen , Shuyan Yi , Mark H. Norman , Markian M. Stec , Emily Anne Peterson , Russell Graceffa
发明人: Christiane Bode , Alessandro Boezio , Alan C. Cheng , Deborah Choquette , James Robert Coats , Katrina Woodin Copeland , Hongbing Huang , Daniel La , Richard Thomas Lewis , Hongyu Liao , Michele Potashman , John Stellwagen , Shuyan Yi , Mark H. Norman , Markian M. Stec , Emily Anne Peterson , Russell Graceffa
IPC分类号: A61K31/52 , C07D401/14 , A61K31/506 , A61P35/02 , A61K31/53 , C07D487/04 , A61K31/5377 , A61P35/00 , C07D473/40 , C07D471/04
CPC分类号: C07D401/14 , C07D403/04 , C07D403/14 , C07D471/04 , C07D487/04 , C07D519/00
摘要: The present invention provides compounds that are PIKK inhibitors, more specifically, mTOR and/or PI3Kα kinase inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of kinases, specifically PI3 kinases, more specifically, mTOR and/or PI3Kα, such as cancer. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
摘要翻译: 本发明提供了PIKK抑制剂,更具体地,mTOR和/或PI3Kα激酶抑制剂的化合物,因此可用于治疗通过抑制激酶可治疗的疾病,特别是PI3激酶,更具体地,mTOR和/或PI3Kα,例如 癌症。 还提供含有这些化合物的药物组合物和制备这些化合物的方法。
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公开(公告)号:US07026326B2
公开(公告)日:2006-04-11
申请号:US10438553
申请日:2003-05-13
申请人: Guo-Qiang Cao , Celia Dominguez , Martin H. Goldberg , Fang-Tsao Hong , Kelvin K. C. Sham , Seifu Tadesse , Nuria A. Tamayo , Kurt E. Weiler , Dawei Zhang , Hongyu Liao
发明人: Guo-Qiang Cao , Celia Dominguez , Martin H. Goldberg , Fang-Tsao Hong , Kelvin K. C. Sham , Seifu Tadesse , Nuria A. Tamayo , Kurt E. Weiler , Dawei Zhang , Hongyu Liao
IPC分类号: A61K31/505
CPC分类号: C07D401/04
摘要: The present invention relates to compounds having the general formula or a pharmaceutically acceptable salt thereof, wherein R1 is a saturated or unsaturated 5-, 6- or 7-membered, ring containing 0, 1, 2 or 3 atoms selected from N, O and S, wherein the ring may be fused with a benzo group, and is substituted by 0, 1 or 2 oxo groups, and wherein R1 is additionally substituted; and R2 is a substituted C1-6alkyl. Also included is a method of prophylaxis or 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: 本发明涉及具有通式的化合物或其药学上可接受的盐,其中R 1是饱和或不饱和的5-,6-或7-元环,其含有0,1,2或 3个选自N,O和S的原子,其中环可以与苯并稠合,并被0,1或2个氧代基取代,并且其中R 1是另外被取代的; R 2是取代的C 1-6烷基。 还包括预防或治疗炎症,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,肌肉退化,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,心肌梗死,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,巨细胞病毒引起的肌痛 (CMV),流感,腺病毒,哺乳动物中的疱疹病毒或带状疱疹感染,包括给予有效量的化合物d 以上所述。
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公开(公告)号:US20060183745A1
公开(公告)日:2006-08-17
申请号:US11354650
申请日:2006-02-15
申请人: Yunxin Bo , Partha Chakrabarti , Ning Chen , Hongyu Liao , Mark Norman , Markian Stec , Nuria Tamayo , Xianghong Wang
发明人: Yunxin Bo , Partha Chakrabarti , Ning Chen , Hongyu Liao , Mark Norman , Markian Stec , Nuria Tamayo , Xianghong Wang
IPC分类号: A61K31/513 , A61K31/501 , C07D403/02
CPC分类号: C07D403/14 , C07D401/14 , C07D417/12 , C07D417/14
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.
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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。
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公开(公告)号:US07480416B2
公开(公告)日:2009-01-20
申请号:US10435499
申请日:2003-05-09
申请人: Hongyu Liao , Mrinal K. Mandal , Bruce F. Cockburn
发明人: Hongyu Liao , Mrinal K. Mandal , Bruce F. Cockburn
CPC分类号: G06F17/148
摘要: Compact and efficient hardware architectures for implementing lifting-based DWTs, including 1-D and 2-D versions of recursive and dual scan architectures. The 1-D recursive architecture exploits interdependencies among the wavelet coefficients by interleaving, on alternate clock cycles using the same datapath hardware, the calculation of higher order coefficients along with that of the first-stage coefficients. The resulting hardware utilization exceeds 90% in the typical case of a 5-stage 1-D DWT operating on 1024 samples. The 1-D dual scan architecture achieves 100% datapath hardware utilization by processing two independent data streams together using shared functional blocks. The 2-D recursive architecture is roughly 25% faster than conventional implementations, and it requires a buffer that stores only a few rows of the data array instead of a fixed fraction (typically 25% or more) of the entire array. The 2-D dual scan architecture processes the column and row transforms simultaneously, and the memory buffer size is comparable to existing architectures. The recursive and dual scan architectures can be readily extended to the N-D case.
摘要翻译: 紧凑且高效的硬件架构,用于实现基于升级的DWT,包括递归和双扫描架构的1-D和2-D版本。 1-D递归架构通过交织利用相互依赖关系,在使用相同数据路径硬件的交替时钟周期上,计算较高阶系数以及第一阶段系数。 在典型情况下,在1024个样本上运行的5级1-DWT DWT,所得到的硬件利用率将超过90%。 1-D双扫描架构通过使用共享功能块处理两个独立数据流来实现100%的数据路径硬件利用率。 2-D递归架构比传统实现快25%,它需要一个只存储几行数据的缓冲区,而不是整个阵列的固定分数(通常为25%或更多)。 2-D双扫描架构同时处理列和行变换,并且内存缓冲区大小与现有架构相当。 递归和双重扫描架构可以容易地扩展到N-D情况。
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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.
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