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1.发明授权Compounds and methods to increase plasma HDL cholesterol levels and improve HDL functionality 失效提高血浆HDL胆固醇水平和提高HDL功能的化合物和方法公开(公告)号：US06881860B2
公开(公告)日：2005-04-19
申请号：US09833407
申请日：2001-04-11
IPC分类号： A61K31/7034 , A61K31/10 , A61K31/192 , A61K31/198 , A61K31/255 , A61P3/06 , C07C323/20 , G01N33/92 , C07C321/00
CPC分类号： G01N33/92 , C07C323/20 , G01N2500/00 , G01N2500/10 , G01N2800/044
摘要： It has been discovered that certain selected ethers of probucol, and their pharmaceutically acceptable salts or prodrugs, are useful for increasing circulating HDL cholesterol. These compounds may also improve HDL functionality by (a) increasing clearance of cholesteryl esters, (b) increasing HDL-particle affinity for hepatic cell surface receptors or (c) increasing the half life of apoAI-HDL.
摘要翻译： 已经发现，普罗布考的某些选择的醚及其药学上可接受的盐或前药可用于增加循环HDL胆固醇。 这些化合物还可以通过（a）增加胆固醇酯的清除率，（b）增加对肝细胞表面受体的HDL-粒子亲和力或（c）增加apoAI-HDL的半衰期来改善HDL功能。
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2.发明授权Compounds and methods to increase plasma HDL cholesterol levels and improve HDL functionality 失效提高血浆HDL胆固醇水平和提高HDL功能的化合物和方法公开(公告)号：US07183317B2
公开(公告)日：2007-02-27
申请号：US10886927
申请日：2004-07-08
IPC分类号： A61K31/255 , C07C323/00 , C07C229/00
CPC分类号： G01N33/92 , C07C323/20 , G01N2500/00 , G01N2500/10 , G01N2800/044
摘要： It has been discovered that certain selected ethers of probucol, and their pharmaceutically acceptable salts or prodrugs, are useful for increasing circulating HDL cholesterol. These compounds may also improve HDL functionality by (a) increasing clearance of cholesteryl esters, (b) increasing HDL-particle affinity for hepatic cell surface receptors or (c) increasing the half life of apoAI-HDL.
摘要翻译： 已经发现，普罗布考的某些选择的醚及其药学上可接受的盐或前药可用于增加循环HDL胆固醇。 这些化合物还可以通过（a）增加胆固醇酯的清除率，（b）增加对肝细胞表面受体的HDL-粒子亲和力或（c）增加apoAI-HDL的半衰期来改善HDL功能。
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3.发明授权公开(公告)号：US07897776B2
公开(公告)日：2011-03-01
申请号：US12148966
申请日：2008-04-23
IPC分类号： C07D421/00 , C07D207/00
CPC分类号： C07D401/12 , C07D207/48 , C07D405/12 , C07D417/12
摘要： Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of an inflammatory condition, in particular asthma. The compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof: wherein: X and Y are independently selected from —CH2— or —CH2—CH2—; Z is selected from S(O)m or Se(O)m and m is 0, 1 or 2; R1 is optionally substituted heteroaryl or heterocyclic; R2 is selected from the group consisting of hydrogen, C1-C6 straight alkyl, and C1-C6 branched alkyl, wherein all may be optionally substituted; and R3 and R4 are alkyl.
摘要翻译： 提供化合物，药物组合物和治疗或预防炎性病症，特别是哮喘的方法。 所述化合物具有通式I或其药学上可接受的盐，酯，前药或衍生物：其中：X和Y独立地选自-CH 2 - 或-CH 2 -CH 2 - ; Z选自S（O）m或Se（O）m，m为0,1或2; R1是任选取代的杂芳基或杂环; R 2选自氢，C 1 -C 6直链烷基和C 1 -C 6支链烷基，其中全部可以被任选取代; R3和R4是烷基。
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4.发明授权Sulfonamide-substituted chalcone derivatives and their use to treat diseases 失效磺酰胺取代的查耳酮衍生物及其用于治疗疾病的用途公开(公告)号：US07173129B2
公开(公告)日：2007-02-06
申请号：US10863115
申请日：2004-06-07
申请人： Kimberly J. Worsencroft , Liming Ni , Zhihong Ye , Charles Q. Meng , M. David Weingarten , Jacob E. Simpson , James A. Sikorski
发明人： Kimberly J. Worsencroft , Liming Ni , Zhihong Ye , Charles Q. Meng , M. David Weingarten , Jacob E. Simpson , James A. Sikorski
IPC分类号： C07D413/00 , C07D419/00 , C07D239/02 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00
CPC分类号： A61K31/55 , A61K31/18 , A61K31/397 , A61K31/4015 , A61K31/445
摘要： The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.
摘要翻译： 本发明涉及使用通式化合物或其药学上可接受的盐或酯的化合物，药物组合物和方法，其中取代基在本申请中定义。
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公开(公告)号：US07094801B2
公开(公告)日：2006-08-22
申请号：US10324987
申请日：2002-12-19
申请人： James A. Sikorski , Charles Q. Meng , M. David Weingarten , Kimberly J. Worsencroft , Liming Ni
发明人： James A. Sikorski , Charles Q. Meng , M. David Weingarten , Kimberly J. Worsencroft , Liming Ni
IPC分类号： A61K31/38 , A61K31/40 , A61K31/535 , C07D333/56 , C07D409/00
CPC分类号： C07D207/333 , C07C45/63 , C07C47/575 , C07D209/12 , C07D213/50 , C07D231/12 , C07D233/64 , C07D235/18 , C07D239/26 , C07D239/52 , C07D241/12 , C07D249/08 , C07D257/04 , C07D261/08 , C07D277/24 , C07D307/28 , C07D307/46 , C07D307/80 , C07D333/22 , C07D333/38 , C07D333/56 , C07D409/10 , C07D409/12 , C07D413/12 , C07D471/04 , C07H15/203
摘要： The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.
摘要翻译： 本发明涉及使用通式化合物或其药学上可接受的盐或酯的化合物，药物组合物和方法，其中取代基在本申请中定义。
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6.发明申请公开(公告)号：US20090270454A1
公开(公告)日：2009-10-29
申请号：US12148966
申请日：2008-04-23
IPC分类号： A61K31/454 , C07D401/12 , C07D417/12 , A61K31/4025 , C07D403/12 , A61P11/06
CPC分类号： C07D401/12 , C07D207/48 , C07D405/12 , C07D417/12
摘要： Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of an inflammatory condition, in particular asthma. The compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof: wherein:X and Y are independently selected from —CH2— or —CH2—CH2—; Z is selected from S(O)m or Se(O)m and m is 0, 1 or 2; R1 is optionally substituted heteroaryl or heterocyclic; R2 is selected from the group consisting of hydrogen, C1-C6 straight alkyl, and C1-C6 branched alkyl, wherein all may be optionally substituted; and R3 and R4 are alkyl.
摘要翻译： 提供化合物，药物组合物和治疗或预防炎性病症，特别是哮喘的方法。 所述化合物具有通式I或其药学上可接受的盐，酯，前药或衍生物：其中：X和Y独立地选自-CH 2 - 或-CH 2 -CH 2 - ; Z选自S（O）m或Se（O）m，m为0,1或2; R1是任选取代的杂芳基或杂环; R 2选自氢，C 1 -C 6直链烷基和C 1 -C 6支链烷基，其中全部可以被任选取代; 并且R 3和R 4是烷基。
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7.发明授权1,3-bis-(substituted-phenyl)-2-propyn-1-ones and their use to treat disorders 失效1,3-二 - （取代苯基）-2-丙炔-1-酮及其用于治疗疾病的用途公开(公告)号：US07202247B2
公开(公告)日：2007-04-10
申请号：US10325087
申请日：2002-12-19
IPC分类号： C07C49/213 , C07D213/06 , C07D231/02 , A61K31/12
CPC分类号： C07D333/38 , C07D333/22
摘要： The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.
摘要翻译： 本发明涉及使用通式化合物的化合物，药物组合物和方法
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8.发明授权公开(公告)号：US07078431B2
公开(公告)日：2006-07-18
申请号：US10443470
申请日：2003-05-21
申请人： Charles Q. Meng , Liming Ni , James A. Sikorski , Lee K. Hoong
发明人： Charles Q. Meng , Liming Ni , James A. Sikorski , Lee K. Hoong
IPC分类号： A61K31/38 , A61K31/36 , A61K31/435 , C07D409/00 , C07C49/213
CPC分类号： A61K31/381 , A61K9/0031 , A61K9/0034 , A61K9/1271 , A61K31/44 , A61K31/505 , A61K31/513 , A61K45/06 , C07D333/16 , C07D333/56 , C07D409/10 , C07D493/04 , A61K2300/00
摘要： It has been discovered certain 1,3-bis-(substituted-phenyl)-2-propen-1-ones, including compounds of formula (I) inhibit the expression of VCAM-1, and thus can be used to treat a patient with a disorder mediated by VCAM-1. Examples of inflammatory disorders that are mediated by VCAM-1 include, but are not limited to arthritis, asthma, dermatitis, cystic fibrosis, post transplantation late and chronic solid organ rejection, multiple sclerosis, systemic lupus erythematosis, inflammatory bowel diseases, autoimmune diabetes, diabetic retinopathy, rhinitis, ischemia-reperfusion injury, post-angioplasty restenosis, chronic obstructive pulmonary disease (COPD), glomerulonephritis, Graves disease, gastrointestinal allergies, conjunctivitis, atherosclerosis, coronary artery disease, angina and small artery disease.
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9.发明授权1, 3-bis-(substituted-phenyl)-2-propen-1-ones and their use to treat VCAM-1 mediated disorders 失效1,3-双 - （取代苯基）-2-丙烯-1-酮及其用于治疗VCAM-1介导的病症公开(公告)号：US06608101B1
公开(公告)日：2003-08-19
申请号：US09886348
申请日：2001-06-20
申请人： Liming Ni , Lee K. Hoong , James A. Sikorski , Charles Q. Meng
发明人： Liming Ni , Lee K. Hoong , James A. Sikorski , Charles Q. Meng
IPC分类号： A61K3138
CPC分类号： C07D409/10 , A61K9/0031 , A61K9/0034 , A61K31/381 , A61K31/44 , A61K31/505 , A61K31/513 , A61K45/06 , C07C49/796 , C07C49/813 , C07C49/835 , C07C49/84 , C07C49/86 , C07C205/45 , C07D309/06 , C07D317/44 , C07D333/16 , C07D333/56 , C07D413/10 , C07D417/10 , C07D493/04 , A61K2300/00
摘要： It has been discovered certain 1,3-bis-(substituted-phenyl)-2-propen-1-ones, including compounds of formula (I) inhibit the expression of VCAM-1, and thus can be used to treat a patient with a disorder mediated by VCAM-1. Examples of inflammatory disorders that are mediated by VCAM-1 include, but are not limited to arthritis, asthma, dermatitis, cystic fibrosis, post transplantation late and chronic solid organ rejection, multiple sclerosis, systemic lupus erythematosis, inflammatory bowel diseases, autoimmune diabetes, diabetic retinopathy, rhinitis, ischemia-reperfusion injury, post-angioplasty restenosis, chronic obstructive pulmonary disease (COPD), glomerulonephritis, Graves disease, gastrointestinal allergies, conjunctivitis, atherosclerosis, coronary artery disease, angina and small artery disease.
摘要翻译： 已经发现某些1,3-双（取代苯基）-2-丙烯-1-酮，包括式（I）化合物抑制VCAM-1的表达，因此可用于治疗患有 由VCAM-1介导的病症。 由VCAM-1介导的炎性病症的实例包括但不限于关节炎，哮喘，皮炎，囊性纤维化，移植后晚期和慢性固体器官排斥，多发性硬化，系统性红斑狼疮，炎性肠病，自身免疫性糖尿病， 糖尿病性视网膜病变，鼻炎，缺血再灌注损伤，血管成形术后再狭窄，慢性阻塞性肺疾病（COPD），肾小球性肾炎，格雷夫斯病，胃肠道过敏，结膜炎，动脉粥样硬化，冠状动脉疾病，心绞痛和小动脉疾病。
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公开(公告)号：US20080176842A1
公开(公告)日：2008-07-24
申请号：US11940035
申请日：2007-11-14
IPC分类号： A61K31/18 , A61K31/495 , A61K31/445 , A61K31/496 , A61K31/5377 , C07D413/02 , C07D401/02 , C07D403/02 , C07D295/14 , C07C311/00 , A61P31/18
CPC分类号： C07C311/29 , C07D235/26 , C07D235/32 , C07D277/82 , C07D295/26 , C07D307/79 , C07D317/62 , C07D319/18 , C07D405/12
摘要： Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.
摘要翻译： 双亚磺酰氨基羟乙基氨基化合物作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶的抑制剂。 本发明涉及下式的逆转录病毒蛋白酶抑制化合物：或其药学上可接受的盐，前药或酯，其中变量如本文所定义。
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