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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:US07115607B2
公开(公告)日:2006-10-03
申请号:US10202823
申请日:2002-07-24
申请人: Christopher H. Fotsch , Premilla Arasasingham , Yunxin Bo , Ning Chen , Martin H. Goldberg , Nianhe Han , Feng-Yin Hsieh , Michael G. Kelly , Qingyian Liu , Mark H. Norman , Duncan M. Smith , Markian Stec , Nuria Tamayo , Ning Xi , Shimin Xu
发明人: Christopher H. Fotsch , Premilla Arasasingham , Yunxin Bo , Ning Chen , Martin H. Goldberg , Nianhe Han , Feng-Yin Hsieh , Michael G. Kelly , Qingyian Liu , Mark H. Norman , Duncan M. Smith , Markian Stec , Nuria Tamayo , Ning Xi , Shimin Xu
IPC分类号: A61K31/496 , C07D401/12 , C07D403/12
CPC分类号: C07D207/08 , A61K38/00 , C07D205/04 , C07D207/09 , C07D209/14 , C07D209/42 , C07D211/26 , C07D211/60 , C07D211/62 , C07D213/38 , C07D213/81 , C07D213/82 , C07D215/48 , C07D217/06 , C07D217/14 , C07D217/26 , C07D233/64 , C07D295/185 , C07D317/60 , C07D317/68 , C07D319/18 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D451/02 , C07K5/06026 , C07K5/06139 , C07K5/06147 , C07K5/06191
摘要: Selected substituted piperazine compounds of Formula I are effective for prophylaxis and treatment of diseases, such as obesity and the like. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving activation of the melanocortin receptor. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译: 式I的选择性取代哌嗪化合物对预防和治疗诸如肥胖症等疾病是有效的。 本发明包括新颖的化合物,类似物,前药和药学上可接受的盐,用于预防和治疗涉及黑皮质素受体活化的疾病和其它疾病或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。
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