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    • 2. 发明授权
    • Substituted phenoxy thiazolidinediones as estrogen related receptor-á modulators
    • 取代苯氧基噻唑烷二酮作为雌激素相关受体α调节剂
    • US08344009B2
    • 2013-01-01
    • US12899812
    • 2010-10-07
    • Michael GaulAlexander KimLily Lee SearleRaymond PatchDionisois RentzeperisGuozhang XuXizhen Zhu
    • Michael GaulAlexander KimLily Lee SearleRaymond PatchDionisois RentzeperisGuozhang XuXizhen Zhu
    • A61K31/426C07D277/04
    • C07D277/34C07D263/44
    • The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.
    • 本发明涉及式(I)化合物,制备这些化合物的方法,组合物,中间体及其衍生物,用于治疗包括但不限于强直性脊柱炎,动脉粥样硬化,关节炎(如类风湿性关节炎,感染性关节炎,儿童期 关节炎,牛皮癣关节炎,反应性关节炎),骨相关疾病(包括与骨形成相关的疾病),乳腺癌(包括对抗雌激素治疗无反应的那些),心血管疾病,软骨相关疾病(如软骨损伤/损失, 软骨变性和与软骨形成相关的软骨变性,软骨发育不全,软骨肉瘤,慢性背部损伤,慢性支气管炎,慢性炎症性气道疾病,慢性阻塞性肺病,糖尿病,能量稳态障碍,痛风,假性血糖,脂质障碍,代谢综合征,多发性 骨髓瘤,肥胖症,骨关节炎,成骨不全,骨质溶解骨 骨质疏松症,骨质疏松症,佩吉特氏病,牙周病,风湿性多肌痛,莱特综合征,重复性应激损伤,高血糖,升高的血糖水平和胰岛素抵抗。
    • 3. 发明申请
    • Substituted 1,4-benzodiazepines and uses thereof
    • 取代的1,4-苯并二氮杂及其用途
    • US20060148792A1
    • 2006-07-06
    • US11371964
    • 2006-03-09
    • Tianbao LuLouis LaFranceDaniel ParksKaren MilkiewiczRaul CalvoMaxwell CummingsAlexander KimBruce GrasbergerTheodore Carver
    • Tianbao LuLouis LaFranceDaniel ParksKaren MilkiewiczRaul CalvoMaxwell CummingsAlexander KimBruce GrasbergerTheodore Carver
    • A61K31/551C07D243/12C07D243/18
    • C07D401/04C07D243/14C07D403/10C07D405/04C07D409/04
    • The present invention is directed to novel 1,4-benzodiazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein: X and Y are independently —C(O)—, —CH2— or —C(S)—; R1, R2, R3, R4, R7, R8, Rb, Rc, Rd and M arm defined herein; R5 is hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aralkyl, optionally substituted heteroaralkyl, carboxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, aminocarbonyl, aminocarbonylalkyl, alkylaminocarbonyl or alkylaminocarbonylalkyl; R6 is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; R9 is cycloalkyl: aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkyl(alkyl), aralkyl or heteroarylalkyl, each of which is optionally substituted; and R10 is —(CH2)n—CO2Rb, —(CH2)m—CO2M, —(CH2)i—OH or —(CH2)j—CONRcRd n is 0-8, m is 0-8, i is 1-8 and j is 0-8.
    • 本发明涉及新的1,4-苯二氮卓类药物,其药物组合物及其作为HDM2-p53相互作用抑制剂的用途。 化合物具有式I:或其溶剂合物,水合物或其药学上可接受的盐; 其中:X和Y独立地为-C(O) - , - CH 2 - 或-C(S) - ; R 1,R 2,R 3,R 4,R 7, R 8,R b,R c,R d,R d和M臂; R 5是氢,烷基,环烷基,任选取代的芳基,任选取代的杂芳基,任选取代的芳烷基,任选取代的杂芳烷基,羧基烷基,烷氧基羰基,烷氧基羰基烷基,氨基羰基,氨基羰基烷基,烷基氨基羰基或烷基氨基羰基烷基; R 6是环烷基,芳基,杂芳基,环烷基烷基,芳烷基,杂芳基烷基或饱和或部分不饱和的杂环,其各自任选被取代; R 9是环烷基:芳基,杂芳基,饱和或部分不饱和的杂环,环烷基(烷基),芳烷基或杂芳基烷基,其各自任选被取代; 和R 10是 - (CH 2)n - - - - - - (CH 2)n - , - (CH 2)2 - , - M 2 - , - (CH 2) -OH或 - (CH 2 CH 2)n -CONR C n R n为0-8 ,m为0-8,i为1-8,j为0-8。
    • 4. 发明授权
    • Substituted phenoxy aminothiazolones as estrogen related receptor-α modulators
    • 取代的苯氧基氨基噻唑酮作为雌激素相关受体α调节剂
    • US08580832B2
    • 2013-11-12
    • US12043311
    • 2008-03-06
    • Michael GaulAlexander KimLily Lee SearleDionisios RentzeperisGilles C. Bignan
    • Michael GaulAlexander KimLily Lee SearleDionisios RentzeperisGilles C. Bignan
    • A61K31/425C07D277/08C07D277/12
    • C07D277/34C07D417/04
    • The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.
    • 本发明涉及式(I)化合物,制备这些化合物的方法,组合物,中间体及其衍生物,用于治疗包括但不限于强直性脊柱炎,动脉粥样硬化,关节炎(如类风湿性关节炎,感染性关节炎,儿童期 关节炎,牛皮癣关节炎,反应性关节炎),骨相关疾病(包括与骨形成相关的疾病),乳腺癌(包括对抗雌激素治疗无反应的那些),心血管疾病,软骨相关疾病(如软骨损伤/损失, 软骨变性和与软骨形成相关的软骨变性,软骨发育不全,软骨肉瘤,慢性背部损伤,慢性支气管炎,慢性炎症性气道疾病,慢性阻塞性肺病,糖尿病,能量稳态障碍,痛风,假性血糖,脂质障碍,代谢综合征,多发性 骨髓瘤,肥胖症,骨关节炎,成骨不全,骨质溶解骨 骨质疏松症,骨质疏松症,佩吉特氏病,牙周病,风湿性多肌痛,莱特综合征,重复性应激损伤,高血糖症,升高的血糖水平和胰岛素抵抗。
    • 5. 发明申请
    • SUBSTITUTED PHENOXY AMINOTHIAZOLONES as estrogen related receptor-alpha modulators
    • 作为雌激素相关受体α调节剂的替代苯氧基丙酮酸
    • US20080221179A1
    • 2008-09-11
    • US12043311
    • 2008-03-06
    • Michael GaulAlexander KimLily Lee SearleDionisios RentzeperisGilles C. Bignan
    • Michael GaulAlexander KimLily Lee SearleDionisios RentzeperisGilles C. Bignan
    • A61K31/426C07D277/56A61P19/00A61P11/00A61P35/04A61P3/00
    • C07D277/34C07D417/04
    • The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.
    • 本发明涉及式(I)化合物,制备这些化合物的方法,组合物,中间体及其衍生物,用于治疗包括但不限于强直性脊柱炎,动脉粥样硬化,关节炎(如类风湿性关节炎,感染性关节炎,儿童期 关节炎,牛皮癣关节炎,反应性关节炎),骨相关疾病(包括与骨形成相关的疾病),乳腺癌(包括对抗雌激素治疗无反应的那些),心血管疾病,软骨相关疾病(如软骨损伤/损失, 软骨变性和与软骨形成相关的软骨变性,软骨发育不全,软骨肉瘤,慢性背部损伤,慢性支气管炎,慢性炎症性气道疾病,慢性阻塞性肺病,糖尿病,能量稳态障碍,痛风,假性血糖,脂质障碍,代谢综合征,多发性 骨髓瘤,肥胖症,骨关节炎,成骨不全,骨质溶解骨 骨质疏松症,骨质疏松症,佩吉特氏病,牙周病,风湿性多肌痛,莱特综合征,重复性应激损伤,高血糖症,升高的血糖水平和胰岛素抵抗。
    • 8. 发明申请
    • SUBSTITUTED PHENOXY THIAZOLIDINEDIONES AS ESTROGEN RELATED RECEPTOR-á MODULATORS
    • 作为雌激素相关受体 - 阿尔法调节剂的取代的苯氧基噻唑烷二酮
    • US20110237625A1
    • 2011-09-29
    • US12899812
    • 2010-10-07
    • Michael GaulAlexander KimLily Lee SearleRaymond J. PatchDionisios RentzeperisGuozhang XuXizhen Zhu
    • Michael GaulAlexander KimLily Lee SearleRaymond J. PatchDionisios RentzeperisGuozhang XuXizhen Zhu
    • A61K31/454C07D277/34A61K31/426C07D263/44A61K31/421A61P19/00A61P11/00A61P35/00A61P3/00A61P9/12
    • C07D277/34C07D263/44
    • The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.
    • 本发明涉及式(I)化合物,制备这些化合物的方法,组合物,中间体及其衍生物,用于治疗包括但不限于强直性脊柱炎,动脉粥样硬化,关节炎(如类风湿性关节炎,感染性关节炎,儿童期 关节炎,牛皮癣关节炎,反应性关节炎),骨相关疾病(包括与骨形成相关的疾病),乳腺癌(包括对抗雌激素治疗无反应的那些),心血管疾病,软骨相关疾病(如软骨损伤/损失, 软骨变性和与软骨形成相关的软骨变性,软骨发育不全,软骨肉瘤,慢性背部损伤,慢性支气管炎,慢性炎症性气道疾病,慢性阻塞性肺病,糖尿病,能量稳态障碍,痛风,假性血糖,脂质障碍,代谢综合征,多发性 骨髓瘤,肥胖症,骨关节炎,成骨不全,骨质溶解骨 骨质疏松症,骨质疏松症,佩吉特氏病,牙周病,风湿性多肌痛,莱特综合征,重复性应激损伤,高血糖症,升高的血糖水平和胰岛素抵抗。
    • 9. 发明授权
    • Substituted phenoxy thiazolidinediones as estrogen related receptor-α modulators
    • 取代苯氧基噻唑烷二酮类作为雌激素相关受体α调节剂
    • US07846953B2
    • 2010-12-07
    • US12043269
    • 2008-03-06
    • Michael GaulAlexander KimLily Lee SearleRaymond PatchDionisois RentzeperisGuozhang XuXizhen Zhu
    • Michael GaulAlexander KimLily Lee SearleRaymond PatchDionisois RentzeperisGuozhang XuXizhen Zhu
    • A61K31/426C07D277/04
    • C07D277/34C07D263/44
    • The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.
    • 本发明涉及式(I)化合物,制备这些化合物的方法,组合物,中间体及其衍生物,用于治疗包括但不限于强直性脊柱炎,动脉粥样硬化,关节炎(如类风湿性关节炎,感染性关节炎,儿童期 关节炎,牛皮癣关节炎,反应性关节炎),骨相关疾病(包括与骨形成相关的疾病),乳腺癌(包括对抗雌激素治疗无反应的那些),心血管疾病,软骨相关疾病(如软骨损伤/损失, 软骨变性和与软骨形成相关的软骨变性,软骨发育不全,软骨肉瘤,慢性背部损伤,慢性支气管炎,慢性炎症性气道疾病,慢性阻塞性肺病,糖尿病,能量稳态障碍,痛风,假性血糖,脂质障碍,代谢综合征,多发性 骨髓瘤,肥胖症,骨关节炎,成骨不全,骨质溶解骨 骨质疏松症,骨质疏松症,佩吉特氏病,牙周病,风湿性多肌痛,莱特综合征,重复性应激损伤,高血糖症,升高的血糖水平和胰岛素抵抗。
    • 10. 发明申请
    • SUBSTITUTED PHENOXY THIAZOLIDINEDIONES AS ESTROGEN RELATED RECEPTOR-alpha MODULATORS
    • 作为雌激素相关受体-α调节剂的取代的苯氧基噻唑烷
    • US20090111855A1
    • 2009-04-30
    • US12043269
    • 2008-03-06
    • Michael GaulAlexander KimLily Lee SearleRaymond J. PatchDionisios RentzeperisGuozhang XuXizhen Zhu
    • Michael GaulAlexander KimLily Lee SearleRaymond J. PatchDionisios RentzeperisGuozhang XuXizhen Zhu
    • A61K31/454C07D277/34A61K31/426A61K31/421C07D263/44A61P3/04
    • C07D277/34C07D263/44
    • The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.
    • 本发明涉及式(I)化合物,制备这些化合物的方法,组合物,中间体及其衍生物,用于治疗包括但不限于强直性脊柱炎,动脉粥样硬化,关节炎(如类风湿性关节炎,感染性关节炎,儿童期 关节炎,牛皮癣关节炎,反应性关节炎),骨相关疾病(包括与骨形成相关的疾病),乳腺癌(包括对抗雌激素治疗无反应的那些),心血管疾病,软骨相关疾病(如软骨损伤/损失, 软骨变性和与软骨形成相关的软骨变性,软骨发育不全,软骨肉瘤,慢性背部损伤,慢性支气管炎,慢性炎症性气道疾病,慢性阻塞性肺病,糖尿病,能量稳态障碍,痛风,假性血糖,脂质障碍,代谢综合征,多发性 骨髓瘤,肥胖症,骨关节炎,成骨不全,骨质溶解骨 骨质疏松症,骨质疏松症,佩吉特氏病,牙周病,风湿性多肌痛,莱特综合征,重复性应激损伤,高血糖,升高的血糖水平和胰岛素抵抗。