Abstract:
The invention relates to thiazole compounds of Formula I and Formula II and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.
Abstract:
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 1 , A 2 , B, R 2 and R 3 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).
Abstract:
The invention relates to thiazole compounds of Formula (I) and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.
Abstract:
The present invention relates to pyridines, pyrimidines and derivatives thereof, (I) or a pharmaceutically acceptable salts thereof, wherein X 1 is N or CR 3 ; X 2 is N or CR 4 ; or -X 1 =X 2 - is -C(=O)-N(R a )- or -N(R a )-C(=O)-; X 3 is N or CR 4 ; X 4 is N or CR 4 ; X 5 is N or CR 6 ; X 6 is N or CR 6 ; wherein only 1, 2 or 3 of X 1 , X 2 , X 3 and X 4 are N; R 1 is a saturated partially 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 is substituted by 0, 1, 2 or 3 substituents. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic ß 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.
Abstract translation:本发明涉及吡啶,嘧啶及其衍生物,(I)或其药学上可接受的盐,其中X 1是N或CR 3; X 2是N或CR 4; 或-X 1 = X 2 - 是-C(= O)-N(R a) - 或-N(R 0) >一 SUP>) - C(= O) - ; X 3是N或CR 4; X 4是N或CR 4; X 5是N或CR 6; X 6是N或CR 6; 其中X 1,X 2,X 3和X 4中仅有1,2或3是N; R 1是饱和的部分饱和或不饱和的含有0,1,2或3个选自N,O和S的原子的5-,6-或7-元环,其中环被 0,1,2或3个取代基。 还包括治疗炎症,类风湿性关节炎,佩吉特病,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。
Abstract:
The present invention relates to pyrimidinones and pyridones 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 ß 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.
Abstract:
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.
Abstract:
The invention relates to thiazole compounds of Formula (I) and Formula (II) and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.
Abstract:
The present invention relates to nitrogen-containing compounds according to formula (I) 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 ß 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.
Abstract:
The invention encompasses compounds represented by the following general structures: formula (I) and formula (II), wherein X; R 1 -R 3 ; R11; R12; and R14 are as defined in the claims and pharmaceutically acceptable salts thereof, pharmaceutical compositions, uses and methods for prophylaxis and treatment of cancer.
Abstract:
The present invention relates to benzothiophene sulfonamides and other compounds that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.