公开(公告)号：US20090170828A1

公开(公告)日：2009-07-02

申请号：US12227544

申请日：2007-06-08

Applicant: Elise Isabel ,  Renata Oballa ,  David Powell ,  Joel Robichaud

Inventor： Elise Isabel ,  Renata Oballa ,  David Powell ,  Joel Robichaud

IPC: A61K31/397 ,  C07D277/20 ,  C07D403/02 ,  C07D401/02 ,  A61P3/04 ,  A61P3/10 ,  A61P9/10

CPC classification number: C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D413/14 ,  C07D417/04

Abstract: Azetidine derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. 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; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; liver steatosis; and non-alcoholic steatohepatitis. (I)

Abstract translation: 结构式I的氮杂环丁烷衍生物是相对于其它已知的硬脂酰辅酶A去饱和酶的硬脂酰辅酶A delta-9去饱和酶（SCD1）的选择性抑制剂。 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; 动脉粥样硬化 肥胖; 糖尿病; 神经系统疾病; 代谢综合征; 胰岛素抵抗; 肝脂肪变性 和非酒精性脂肪性肝炎。 （一世）

公开(公告)号：US07405229B2

公开(公告)日：2008-07-29

申请号：US10560672

申请日：2004-06-28

Applicant: Christopher Bayly ,  Cameron Black ,  Sheldon Crane ,  Daniel J. McKay ,  Renata Oballa ,  Joel Robichaud

Inventor： Christopher Bayly ,  Cameron Black ,  Sheldon Crane ,  Daniel J. McKay ,  Renata Oballa ,  Joel Robichaud

IPC: A61K31/44 ,  A61K31/445 ,  A61K31/417 ,  A61K31/4184 ,  C07D211/80 ,  C07D233/54 ,  C07D235/04

CPC classification number: C07D213/83 ,  C07C255/29 ,  C07C311/06 ,  C07C323/25 ,  C07C323/49 ,  C07C323/60 ,  C07C323/61 ,  C07C323/62 ,  C07C2601/02 ,  C07C2601/14 ,  C07D211/20 ,  C07D213/32 ,  C07D231/12 ,  C07D233/64 ,  C07D235/06 ,  C07D257/04

Abstract: This invention relates to a class of compounds having the general formula (I) which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

Abstract translation: 本发明涉及一类具有通式（I）的化合物，它是半胱氨酸蛋白酶抑制剂，包括但不限于组织蛋白酶K，L，S和B的抑制剂。这些化合物可用于治疗其中抑制骨的疾病 表示吸收，如骨质疏松症。

公开(公告)号：US07928091B2

公开(公告)日：2011-04-19

申请号：US11988346

申请日：2006-07-05

Applicant: Cameron Black ,  Sheldon Crane ,  Renata Oballa ,  Joel Robichaud

Inventor： Cameron Black ,  Sheldon Crane ,  Renata Oballa ,  Joel Robichaud

IPC: A61K31/663 ,  C07D231/12

CPC classification number: C07D231/12

Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

公开(公告)号：US20070167635A1

公开(公告)日：2007-07-19

申请号：US10560672

申请日：2004-06-28

Applicant: Christopher Bayly ,  Cameron Black ,  Sheldon Crane ,  Daniel McKay ,  Renata Oballa ,  Joel Robichaud

Inventor： Christopher Bayly ,  Cameron Black ,  Sheldon Crane ,  Daniel McKay ,  Renata Oballa ,  Joel Robichaud

IPC: G01N33/48 ,  C07D233/14 ,  C07D233/22

CPC classification number: C07D213/83 ,  C07C255/29 ,  C07C311/06 ,  C07C323/25 ,  C07C323/49 ,  C07C323/60 ,  C07C323/61 ,  C07C323/62 ,  C07C2601/02 ,  C07C2601/14 ,  C07D211/20 ,  C07D213/32 ,  C07D231/12 ,  C07D233/64 ,  C07D235/06 ,  C07D257/04

Abstract: This invention relates to a class of compounds having the general formula (I) which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

Abstract translation: 本发明涉及一类具有通式（I）的化合物，它是半胱氨酸蛋白酶抑制剂，包括但不限于组织蛋白酶K，L，S和B的抑制剂。这些化合物可用于治疗其中抑制骨的疾病 表示吸收，如骨质疏松症。

公开(公告)号：US20130244929A1

公开(公告)日：2013-09-19

申请号：US13583462

申请日：2011-03-04

Applicant: Michel Gallant ,  Karine Villeneuve ,  Patrick Beaulieu ,  Joel Robichaud ,  Helene Juteau ,  Yves Gareau ,  Sherman T. Waddell ,  Nancy Kevin ,  Xin Gu ,  Joann Huber ,  Michael J. Salvatore, JR. ,  Kenneth Wilson ,  Scott K. Smith ,  Deborah Zink

Inventor： Michel Gallant ,  Karine Villeneuve ,  Patrick Beaulieu ,  Joel Robichaud ,  Helene Juteau ,  Yves Gareau ,  Sherman T. Waddell ,  Nancy Kevin ,  Xin Gu ,  Joann Huber ,  Michael J. Salvatore, JR. ,  Kenneth Wilson ,  Scott K. Smith ,  Deborah Zink

IPC: A61K38/08 ,  A61K31/407 ,  C07K7/02

CPC classification number: A61K38/08 ,  A61K31/407 ,  A61K38/00 ,  C07K5/0202 ,  C07K7/02

Abstract: The present invention provides novel lipoglycopeptide compounds which are Type 1 signal peptidase inhibitors (SpsB). Compounds of the present invention are useful for the treatment of various bacterial related infectious diseases, particularly when used as a potentiator of a β-lactam antibiotic such as imipenem and ertapenem. Accordingly, the present invention provides a method for the treatment of bacterial related infections using the compounds described herein, either alone or in combination with a β-lactam antibiotic.

Abstract translation: 本发明提供了作为1型信号肽酶抑制剂（SpsB）的新型脂多糖化合物。 本发明的化合物可用于治疗各种细菌相关感染性疾病，特别是用作β-内酰胺抗生素如亚胺培南和厄他替班的增效剂时。 因此，本发明提供了使用本文所述的化合物单独或与β-内酰胺抗生素组合治疗细菌相关感染的方法。

公开(公告)号：US20100298347A1

公开(公告)日：2010-11-25

申请号：US12743610

申请日：2008-12-01

Applicant: Michel Belley ,  Denis Deschenes ,  Rejean Fortin ,  Jean-Francois Fournier ,  Sebastien Gagne ,  Yves Gareau ,  Jacques Yves Gauthier ,  Lianhai Li ,  Joel Robichaud ,  Michel Therien ,  Geoffrey K. Tranmer ,  Zhaoyin Wang

Inventor： Michel Belley ,  Denis Deschenes ,  Rejean Fortin ,  Jean-Francois Fournier ,  Sebastien Gagne ,  Yves Gareau ,  Jacques Yves Gauthier ,  Lianhai Li ,  Joel Robichaud ,  Michel Therien ,  Geoffrey K. Tranmer ,  Zhaoyin Wang

IPC: A61K31/519 ,  C07C63/72 ,  C07D333/34 ,  C07D333/22 ,  C07C63/42 ,  C07D317/54 ,  C07D409/12 ,  C07D487/04 ,  C07D249/08 ,  C07D211/94 ,  C07D211/32 ,  A61K31/192 ,  A61K31/381 ,  A61K31/194 ,  A61K31/36 ,  A61K31/4436 ,  A61K31/4196 ,  A61K31/451 ,  A61P3/10 ,  A61P5/50 ,  A61P3/04 ,  A61P3/00

CPC classification number: C07D211/34 ,  C07C65/24 ,  C07C65/30 ,  C07C65/40 ,  C07C69/76 ,  C07C69/94 ,  C07C317/44 ,  C07C317/46 ,  C07C323/62 ,  C07D211/52 ,  C07D249/08 ,  C07D317/60 ,  C07D333/16 ,  C07D333/24 ,  C07D333/34 ,  C07D487/04

Abstract: Substituted 2-naphthoic acids of structural formula are effective as antagonists of the biological activity of GPR105 protein. They are useful for the treatment, control or prevention of disorders responsive to antagonism of this receptor, such as diabetes, particularly, Type 2 diabetes, insulin resistance, hyperglycemia, lipid disorders, obesity, atherosclerosis, and conditions associated with the Metabolic Syndrome.

Abstract translation: 结构式的取代的2-萘甲酸作为GPR105蛋白的生物活性的拮抗剂是有效的。 它们可用于治疗，控制或预防对该受体的拮抗作用有响应的病症，例如糖尿病，特别是2型糖尿病，胰岛素抵抗，高血糖症，脂质障碍，肥胖症，动脉粥样硬化和与代谢综合征有关的病症。

公开(公告)号：US20090093444A1

公开(公告)日：2009-04-09

申请号：US11988346

申请日：2006-07-05

Applicant: Cameron Black ,  Sheldon Crane ,  Renata Oballa ,  Joel Robichaud

Inventor： Cameron Black ,  Sheldon Crane ,  Renata Oballa ,  Joel Robichaud

IPC: A61K31/663 ,  C07D231/12 ,  A61K31/59 ,  A61P19/00 ,  A61P35/00 ,  A61P11/00 ,  A61P3/00 ,  A61P19/10 ,  A61K31/415

CPC classification number: C07D231/12

Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

Abstract translation: 本发明涉及一类新的化合物，它们是半胱氨酸蛋白酶抑制剂，包括但不限于组织蛋白酶K，L，S和B的抑制剂。这些化合物可用于治疗其中指示抑制骨吸收的疾病，例如 骨质疏松症