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公开(公告)号：US09187415B2
公开(公告)日：2015-11-17
申请号：US13882329
申请日：2011-10-27
IPC分类号： C07C311/41 , C07C311/42 , C07D231/12 , C07D261/08 , C07D277/64 , C07D239/26 , C07D417/12 , C07D417/14 , A61K31/428 , A61K31/42 , A61K31/415 , A61K31/4439 , A61K31/4412 , A61K31/506 , A61K31/18 , C07C311/18 , C07C311/29 , C07C317/40 , C07C323/49 , C07D213/75 , A61K31/63 , A61K31/635 , A61K45/06 , C07D277/62
CPC分类号： C07C311/18 , A61K31/428 , A61K31/4439 , A61K31/506 , A61K31/63 , A61K31/635 , A61K45/06 , C07C311/29 , C07C311/41 , C07C317/40 , C07C323/49 , C07C2601/02 , C07D213/75 , C07D231/12 , C07D239/26 , C07D261/08 , C07D277/62 , C07D277/64 , C07D417/12 , C07D417/14
摘要： Compounds of Formula I are disclosed: wherein L, A, R1, R2, R3A, R3B, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译： 公开了式I的化合物：其中L，A，R1，R2，R3A，R3B，R4A，R4B，R5，R6和R7如本文所定义。 式I所包括的化合物包括可以在体内代谢为HIV蛋白酶抑制剂的HIV蛋白酶抑制剂和其它化合物的化合物。 化合物及其药学上可接受的盐可用于预防或治疗HIV感染以及预防，治疗或延迟艾滋病的发病。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。
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公开(公告)号：US20140018326A1
公开(公告)日：2014-01-16
申请号：US13882329
申请日：2011-10-27
IPC分类号： C07C311/18 , A61K45/06 , C07D261/08 , A61K31/635 , C07D239/26 , C07D213/75 , C07D277/62 , A61K31/428 , C07D417/12 , C07D417/14 , A61K31/4439 , A61K31/506 , A61K31/63 , C07D231/12
CPC分类号： C07C311/18 , A61K31/428 , A61K31/4439 , A61K31/506 , A61K31/63 , A61K31/635 , A61K45/06 , C07C311/29 , C07C311/41 , C07C317/40 , C07C323/49 , C07C2601/02 , C07D213/75 , C07D231/12 , C07D239/26 , C07D261/08 , C07D277/62 , C07D277/64 , C07D417/12 , C07D417/14
摘要： Compounds of Formula I are disclosed: wherein L, A, R1, R2, R3A, R3B, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译： 公开了式I的化合物：其中L，A，R1，R2，R3A，R3B，R4A，R4B，R5，R6和R7如本文所定义。 式I所包括的化合物包括可以在体内代谢为HIV蛋白酶抑制剂的HIV蛋白酶抑制剂和其它化合物的化合物。 化合物及其药学上可接受的盐可用于预防或治疗HIV感染以及预防，治疗或延迟艾滋病的发病。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。
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3.发明申请公开(公告)号：US20160060255A1
公开(公告)日：2016-03-03
申请号：US14786464
申请日：2014-04-22
申请人： Neville J. ANTHONY , Brain M. ANDERSEN , Alan B. NORTHRUP , Kaleen K. CHILDERS , Anthony FRIO , Thomas A. MILLER , Yuan LIU , Michelle R. MACHACEK , Hyun Chong WOO , Kerrie B. SPENCER , John Michael ELLIS , Micheal D. ALTMAN , Eric T. ROMEO , Daniel GUAY , Jonathan GRIMM , Marie-Eve LEBRUN , Joel S. ROBICHAUD , Liping WANG , Byron DUBOIS , Qiaolin DENG , MERICK SHARP & DOHNE CORP. , MERCK CANADA INC.
发明人： Neville J. Anthony , Brian M. Andresen , Alan B. Northrup , Kaleen K. Childers , Anthony Donofrio , Thomas A. Miller , Yuan Liu , Michelle R. Machacek , Hyun Chong Woo , Kerrie B. Spencer , John Michael Ellis , Michael D. Altman , Eric T. Romeo , Daniel Guay , Jonathan Grimm , Marie-Eve Lebrun , Joel S. Robichaud , Liping Wang , Byron DuBois , Qiaolin Deng
IPC分类号： C07D417/14 , A61K31/53 , A61K31/4439 , A61K31/501 , A61K31/506 , A61K31/497
CPC分类号： C07D417/14 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/53 , C07D417/12
摘要： The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, and R4 are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
摘要翻译： 本发明提供式（I）的某些噻唑取代的氨基杂芳基化合物或其药学上可接受的盐，其中X 1，X 2，X 3，X 4，Y 1，Y 2，Y 3，Y 4和R 4如本文所定义。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗由脾脏酪氨酸激酶（Syk）介导的疾病或病症的方法。
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4.发明申请NOVEL SUBSTITUTED HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE 审中-公开新型替代异构化合物作为硬脂酸苄酯DE DELTA-9去饱和酶的抑制剂公开(公告)号：US20110021532A1
公开(公告)日：2011-01-27
申请号：US12934100
申请日：2009-04-21
IPC分类号： A61K31/501 , C07D235/18 , A61K31/4184 , C07D401/02 , A61K31/4439 , C07D403/04 , A61K31/506 , C07D471/02 , A61K31/437 , A61P3/10 , A61P3/00 , A61P3/04 , A61P1/16 , A61P9/00 , A61P9/10
CPC分类号： C12N9/0083 , C07D235/18 , C07D401/04 , C07D401/10 , C07D403/04 , C07D405/10 , C07D409/10 , C07D471/04
摘要： Substituted heteroaromatic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; Type 2 diabetes; insulin resistance; hyperglycemia; Metabolic Syndrome; neurological disease; cancer; and liver steatosis. Formula (I).
摘要翻译： 结构式I的取代的杂芳族化合物是硬脂酰辅酶A delta-9去饱和酶的抑制剂。 本发明的化合物可用于预防和治疗与脂质合成和代谢异常有关的病症，包括心血管疾病，如动脉粥样硬化; 肥胖; 2型糖尿病; 胰岛素抵抗; 高血糖症 代谢综合征; 神经系统疾病; 癌症; 和肝脂肪变性。 式（I）。
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