公开(公告)号：US20050038098A1

公开(公告)日：2005-02-17

申请号：US10827111

申请日：2004-04-19

申请人： Catherine Tachdjian ,  Jianhua Guo ,  Mohamed Boudjelal ,  Hussien Al-Shamma ,  Andrea Giachino ,  Karine Jakubowicz-Jaillardon ,  Qing Chen ,  James Zapf ,  Magnus Pfahl

发明人： Catherine Tachdjian ,  Jianhua Guo ,  Mohamed Boudjelal ,  Hussien Al-Shamma ,  Andrea Giachino ,  Karine Jakubowicz-Jaillardon ,  Qing Chen ,  James Zapf ,  Magnus Pfahl

IPC分类号： A61K20060101 ,  A61K31/353 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/416 ,  A61K31/42 ,  C07D277/04 ,  C07D49/02 ,  C07D45/02

CPC分类号： C07D417/10 ,  C07D277/34

摘要： The invention relates to novel heterocyclic compounds having the structure illustrated by Formula (I) wherein the Ar1 radicals are substituted dihydronapthalene or isochroman radicals, the Ar2 radicals are aryl or heteroaryl radicals; and HAr is a 2,4-thiazolidinedione, 2-thioxo-thiazolidine-4-one, 2,4-imidazolidinedione or 2-thioxo-imidazolidine-4-one radical. The compounds of Formula (I) can have biological activity for advantageously regulating carbohydrate metabolism, including serum glucose level, and lipid metabolism, and can be useful for the treatment of hyperlipidemia and/or hypercholesterolemia, and Type II diabetes. The compounds of Formula (I) can also have utility in the treatment of diseases of uncontrolled proliferation, including cancer.

摘要翻译： 本发明涉及具有式（I）所示结构的新型杂环化合物，其中Ar 1基团是取代的二氢萘或异苯并二氢吡喃基，Ar 2基团是芳基或杂芳基; 并且HAr是2,4-噻唑烷二酮，2-硫代 - 噻唑烷-4-酮，2,4-咪唑烷二酮或2-硫代 - 咪唑烷-4-酮基。 式（I）的化合物可以具有有利地调节碳水化合物代谢（包括血清葡萄糖水平和脂质代谢）的生物学活性，并且可用于治疗高脂血症和/或高胆固醇血症和II型糖尿病。 式（I）化合物还可用于治疗不受控制的增殖疾病，包括癌症。

公开(公告)号：US20060241138A1

公开(公告)日：2006-10-26

申请号：US11476330

申请日：2006-06-28

申请人： Magnus Pfahl ,  Catherine Tachdjian ,  Hussien Al-Shamma ,  Andrea Giachino ,  Karine Jakubowicz-Jaillardon ,  Jianhua Guo ,  Mohamed Boudjelal ,  James Zapf

发明人： Magnus Pfahl ,  Catherine Tachdjian ,  Hussien Al-Shamma ,  Andrea Giachino ,  Karine Jakubowicz-Jaillardon ,  Jianhua Guo ,  Mohamed Boudjelal ,  James Zapf

IPC分类号： A61K31/4709 ,  A61K31/427 ,  A61K31/4178

CPC分类号： C07D277/20 ,  C07D417/06 ,  C07D417/10

摘要： The present invention relates to methods of treating breast cancer, diabetes, and/or related metabolic disorders with certain substituted heterocycles of Formula (200), wherein B, H, I, J and K together with the Ar5 form a ring containing at least one amide residue, and W, X, Y and Z together form a 2,4-thiazolidinedione, 2-thioxo-thiazolidine-4-one, 2,4-imidazolidinedione or 2-thioxo-imidazolidine-4-one residue; or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明涉及用某些取代的式（200）杂环治疗乳腺癌，糖尿病和/或相关的代谢紊乱的方法，其中B，H，I，J和K与Ar 5 >形成含有至少一个酰胺残基的环，W，X，Y和Z一起形成2,4-噻唑烷二酮，2-硫代 - 噻唑烷-4-酮，2,4-咪唑烷二酮或2-硫代 - 咪唑烷 - 4-一个残基; 或其药学上可接受的盐。

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。

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:

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.

公开(公告)号：US20070072804A1

公开(公告)日：2007-03-29

申请号：US11603417

申请日：2006-11-22

申请人： Zhi-Liang Chu ,  James Leonard ,  Hussien Al-Shamma ,  Robert Jones

发明人： Zhi-Liang Chu ,  James Leonard ,  Hussien Al-Shamma ,  Robert Jones

IPC分类号： A61K38/17

CPC分类号： G01N33/76 ,  A61K31/00 ,  A61K31/401 ,  A61K31/415 ,  A61K31/4196 ,  A61K45/06 ,  G01N33/74 ,  G01N2333/726 ,  G01N2800/042 ,  G01N2800/2814 ,  G01N2800/2835 ,  G01N2800/2857 ,  G01N2800/2871 ,  A61K2300/00

摘要： The present invention concerns combination of an amount of a GPR119 agonist with an amount of a dipeptidyl peptidase IV (DPP-IV) inhibitor such that the combination provides an effect in lowering a blood glucose level or in increasing a blood GLP-1 level in a subject over that provided by the amount of the GPR119 agonist or the amount of the DPP-IV inhibitor alone and the use of such a combination for treating or preventing diabetes and conditions related thereto or conditions ameliorated by increasing a blood GLP-1 level. The present invention also relates to the use of a G protein-coupled receptor to screen for GLP-1 secretagogues.

公开(公告)号：US20060154866A1

公开(公告)日：2006-07-13

申请号：US11328405

申请日：2006-01-09

申请人： Zhi-Liang Chu ,  James Leonard ,  Hussien Al-Shamma ,  Robert Jones

发明人： Zhi-Liang Chu ,  James Leonard ,  Hussien Al-Shamma ,  Robert Jones

IPC分类号： A61K38/26 ,  A61K38/04 ,  C12Q1/68 ,  G01N33/53

CPC分类号： G01N33/76 ,  A61K31/00 ,  A61K31/401 ,  A61K31/415 ,  A61K31/4196 ,  A61K45/06 ,  G01N33/74 ,  G01N2333/726 ,  G01N2800/042 ,  G01N2800/2814 ,  G01N2800/2835 ,  G01N2800/2857 ,  G01N2800/2871 ,  A61K2300/00

摘要： The present invention concerns combination of an amount of a GPR119 agonist with an amount of a dipeptidyl peptidase IV (DPP-IV) inhibitor such that the combination provides an effect in lowering a blood glucose level or in increasing a blood GLP-1 level in a subject over that provided by the amount of the GPR119 agonist or the amount of the DPP-IV inhibitor alone and the use of such a combination for treating or preventing diabetes and conditions related thereto or conditions ameliorated by increasing a blood GLP-1 level. The present invention also relates to the use of a G protein-coupled receptor to screen for GLP-1 secretagogues.

摘要翻译： 本发明涉及一定量的GPR119激动剂与二肽基肽酶IV（DPP-IV）抑制剂的量的组合，使得该组合提供降低血糖水平或增加血液GLP-1水平的效果 受限于GPR119激动剂的量或单独的DPP-IV抑制剂的量以及这样的组合用于治疗或预防糖尿病和与之相关的病症或通过增加血液GLP-1水平而改善的病症。 本发明还涉及G蛋白偶联受体筛选GLP-1促分泌素的用途。

公开(公告)号：US20070072803A1

公开(公告)日：2007-03-29

申请号：US11603410

申请日：2006-11-22

申请人： Zhi-Liang Chu ,  James Leonard ,  Hussien Al-Shamma ,  Robert Jones

发明人： Zhi-Liang Chu ,  James Leonard ,  Hussien Al-Shamma ,  Robert Jones

IPC分类号： A61K38/17

CPC分类号： G01N33/76 ,  A61K31/00 ,  A61K31/401 ,  A61K31/415 ,  A61K31/4196 ,  A61K45/06 ,  G01N33/74 ,  G01N2333/726 ,  G01N2800/042 ,  G01N2800/2814 ,  G01N2800/2835 ,  G01N2800/2857 ,  G01N2800/2871 ,  A61K2300/00

摘要： The present invention concerns combination of an amount of a GPR119 agonist with an amount of a dipeptidyl peptidase IV (DPP-IV) inhibitor such that the combination provides an effect in lowering a blood glucose level or in increasing a blood GLP-1 level in a subject over that provided by the amount of the GPR119 agonist or the amount of the DPP-IV inhibitor alone and the use of such a combination for treating or preventing diabetes and conditions related thereto or conditions ameliorated by increasing a blood GLP-1 level. The present invention also relates to the use of a G protein-coupled receptor to screen for GLP-1 secretagogues.

摘要翻译： 本发明涉及一定量的GPR119激动剂与二肽基肽酶IV（DPP-IV）抑制剂的量的组合，使得该组合提供降低血糖水平或增加血液GLP-1水平的效果 受限于GPR119激动剂的量或单独的DPP-IV抑制剂的量以及这样的组合用于治疗或预防糖尿病和与之相关的病症或通过增加血液GLP-1水平而改善的病症。 本发明还涉及G蛋白偶联受体筛选GLP-1促分泌素的用途。