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公开(公告)号：US20060160796A1
公开(公告)日：2006-07-20
申请号：US11385204
申请日：2006-03-20
申请人： Magnus Pfahl , Catherine Tachdjian , Lyle Spruce , Hussien Al-Shamma , Mohamed Boudjelal , Andrea Fanjul , Torsten Wiemann , David Pleynet
发明人： Magnus Pfahl , Catherine Tachdjian , Lyle Spruce , Hussien Al-Shamma , Mohamed Boudjelal , Andrea Fanjul , Torsten Wiemann , David Pleynet
IPC分类号： A61K31/538 , A61K31/517 , A61K31/498 , A61K31/4709 , A61K31/427 , A61K31/423 , A61K31/422 , C07D413/02 , C07D417/02
CPC分类号： C07D277/20 , C07D417/06 , C07D417/10 , C07D417/14
摘要： The present invention relates to certain compounds of Formula (I) which can be useful in the treatment of diseases, such as, cancer, metabolic disorders, Type 2 Diabetes, dyslipidemia and/or hyperchloesterolemia:
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公开(公告)号：US20050070581A1
公开(公告)日：2005-03-31
申请号：US10894411
申请日：2004-07-19
申请人： Magnus Pfahl , Catherine Tachdjian , Hussien Al-Shamma , Andrea Fanjul , David Pleynet , Lyle Spruce
发明人： Magnus Pfahl , Catherine Tachdjian , Hussien Al-Shamma , Andrea Fanjul , David Pleynet , Lyle Spruce
IPC分类号： C07D233/76 , A61K31/4166 , A61K31/426 , A61K31/4439 , A61K31/4709 , A61K31/498 , A61P1/00 , A61P1/04 , A61P3/06 , A61P3/08 , A61P3/10 , A61P9/10 , A61P11/00 , A61P15/00 , A61P19/02 , A61P29/00 , A61P35/00 , A61P35/02 , C07D233/40 , C07D233/42 , C07D233/86 , C07D233/96 , C07D261/12 , C07D277/20 , C07D277/34 , C07D277/36 , C07D401/06 , C07D401/10 , C07D403/10 , C07D405/10 , C07D417/06 , C07D417/10 , C07D285/14 , C07D263/02 , C07D277/04
CPC分类号： C07D277/20 , C07D233/40 , C07D233/42 , C07D233/72 , C07D233/84 , C07D233/86 , C07D233/96 , C07D261/12 , C07D277/34 , C07D277/36 , C07D401/06 , C07D401/10 , C07D403/10 , C07D405/10 , C07D417/06 , C07D417/10
摘要： The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymphoma, Hodgkin's Disease, leukemia, breast cancer, prostate cancer or cancers in general; and inflammation, such as osteoarthritis, rheumatoid arthritis, Crohn's Disease or Inflammatory Bowel Disease.
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3.发明申请Benzoxazole, benzothiazole, and benzimidazole derivatives for the treatment of cancer and other diseases 审中-公开苯并恶唑，苯并噻唑和苯并咪唑衍生物用于治疗癌症等疾病公开(公告)号：US20050014767A1
公开(公告)日：2005-01-20
申请号：US10769725
申请日：2004-01-29
申请人： Magnus Pfahl , Catherine Tachdjian , Torsten Wiemann , Christopher Cow , Lyle Spruce , Andrea Giachino , Allan Kaspar , James Zapf
发明人： Magnus Pfahl , Catherine Tachdjian , Torsten Wiemann , Christopher Cow , Lyle Spruce , Andrea Giachino , Allan Kaspar , James Zapf
IPC分类号： A61K20060101 , A61K31/4184 , A61K31/423 , A61K31/4439 , A61K31/497 , C07D401/14 , C07D417/14
CPC分类号： C07D417/14
摘要： The invention relates to certain compounds whose structures are shown below, and their pharmaceutically acceptable salts and prodrugs, and pharmaceutical compositions thereof, which are useful for treating treating diseases of uncontrolled cellular proliferation, including cancer. wherein: a) Ar1 has the structure: wherein a) R1 has the structure b) Ar2 has the structure; c) R3 is hydrogen, or an alkyl radical; d) ----- represents a bond present or absent; and e) HAr has the formula
摘要翻译： 本发明涉及其结构如下所示的某些化合物及其药学上可接受的盐和前药及其药物组合物，其可用于治疗治疗包括癌症在内的不受控制的细胞增殖的疾病。 其中：a）Ar1具有以下结构：其中a）R 1具有结构b）Ar 2具有结构; c）R3是氢或烷基; d）-----表示存在或不存在的债券; 和e）HAr具有公式
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4.发明授权Peptoid and nonpeptoid containing alpha-keto oxadiazoles as serine protease inhibitors 失效含有α-酮基恶二唑作为丝氨酸蛋白酶抑制剂的胡椒和非头孢托酸公开(公告)号：US06255453B1
公开(公告)日：2001-07-03
申请号：US09325512
申请日：1999-06-03
IPC分类号： A61K3806
CPC分类号： C07D271/10 , A61K38/00 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/0202 , C07K5/06052 , C07K5/0806 , C07K5/12
摘要： The present invention relates to certain substituted oxadiazole peptoids and nonpeptoids useful as inhibitors of serine proteases, especially human neutophil elastase (HNE). Compounds of the present invention are useful for the treatment or amelioration of symptoms of adult respiratory distress syndrome, septic shock, and multiple organ failure. Processes mediated by HNE are also implicated in conditions such as arthritis, periodontal disease, glomerulonephritis, and cystic fibrosis.
摘要翻译： 本发明涉及可用作丝氨酸蛋白酶，特别是人neutophil弹性蛋白酶（HNE）的抑制剂的某些取代的恶二唑拟肽和非幌子。 本发明的化合物可用于治疗或改善成人呼吸窘迫综合征，败血性休克和多器官功能衰竭的症状。 由HNE介导的过程也涉及诸如关节炎，牙周病，肾小球性肾炎和囊性纤维化的病症。
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公开(公告)号：US20050209286A1
公开(公告)日：2005-09-22
申请号：US11069930
申请日：2005-03-01
申请人： Magnus Pfahl , Catherine Tachdjian , Hussien Al-Shamma , Andrea Fanjul , David Pleynet , Lyle Spruce , Richard Fine , James Zapf , Jianhua Guo , Karine Jakubowicz-Jaillardon
发明人： Magnus Pfahl , Catherine Tachdjian , Hussien Al-Shamma , Andrea Fanjul , David Pleynet , Lyle Spruce , Richard Fine , James Zapf , Jianhua Guo , Karine Jakubowicz-Jaillardon
IPC分类号： A61K31/4245 , A61K31/426 , A61K31/454 , A61K45/00 , A61P1/00 , A61P3/06 , A61P3/10 , A61P7/12 , A61P9/10 , A61P11/00 , A61P19/02 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/02 , C07D271/06 , C07D271/07 , C07D277/20 , C07D277/34 , C07D277/36 , C07D417/10 , A61K31/4439 , C07D285/14 , G01N33/48 , G01N33/50 , G06F19/00
CPC分类号： C07D271/07 , C07D277/20 , C07D417/10
摘要： Disclosed are molecules that activate an RXR receptor, wherein the molecule comprises an RXR binding portion which binds the RXR receptor and comprises a side pocket contacting residue which contacts a side-pocket 1 of an RXR receptor.
摘要翻译： 公开了激活RXR受体的分子，其中分子包含结合RXR受体的RXR结合部分，并且包含与RXR受体的侧囊1接触的侧袋接触残基。
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公开(公告)号：US06548638B2
公开(公告)日：2003-04-15
申请号：US09842543
申请日：2001-04-26
IPC分类号： A61K3805
CPC分类号： C07D271/10 , A61K38/00 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/0202 , C07K5/06052 , C07K5/0806 , C07K5/12
摘要： The present invention relates to certain substituted oxadiazole peptoids and nonpeptoids useful as inhibitors of serine proteases, especially human neutophil elastase (HNE). Compounds of the present invention are useful for the treatment or amelioration of symptoms of adult respiratory distress syndrome, septic shock, and multiple organ failure. Processes mediated by HNE are also implicated in conditions such as arthritis, periodontal disease, glomerulonephritis, and cystic fibrosis.
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7.发明申请公开(公告)号：US20060004059A1
公开(公告)日：2006-01-05
申请号：US11210403
申请日：2005-08-24
申请人： Magnus Pfahl , Catherine Tachdjian , Hussein Al-Shamma , Andrea Fanjul , David Pleynet , Lyle Spruce
发明人： Magnus Pfahl , Catherine Tachdjian , Hussein Al-Shamma , Andrea Fanjul , David Pleynet , Lyle Spruce
IPC分类号： A61K31/4439 , A61K31/426
CPC分类号： C07D277/20 , C07D233/40 , C07D233/42 , C07D233/72 , C07D233/84 , C07D233/86 , C07D233/96 , C07D261/12 , C07D277/34 , C07D277/36 , C07D401/06 , C07D401/10 , C07D403/10 , C07D405/10 , C07D417/06 , C07D417/10
摘要： The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymphoma, Hodgkin's Disease, leukemia, breast cancer, prostate cancer or cancers in general; and inflammation, such as osteoarthritis, rheumatoid arthritis, Crohn's Disease or Inflammatory Bowel Disease.
摘要翻译： 本发明涉及某些可用于治疗与脂质和碳水化合物代谢有关的疾病的取代的式（I）的杂环，例如2型糖尿病，脂肪细胞分化，不受控制的增殖，例如淋巴瘤，霍奇金病，白血病，乳腺癌 一般癌症，前列腺癌或癌症; 和炎症，例如骨关节炎，类风湿性关节炎，克罗恩病或炎症性肠病。
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