公开(公告)号：US08889670B2

公开(公告)日：2014-11-18

申请号：US13147432

申请日：2010-02-16

Applicant: Alessandra Bartolozzi ,  Angela Berry ,  Pier Francesco Cirillo ,  Eugene Richard Hickey ,  Doris Riether ,  Lifen Wu ,  Renee M. Zindell

Inventor： Alessandra Bartolozzi ,  Angela Berry ,  Pier Francesco Cirillo ,  Eugene Richard Hickey ,  Doris Riether ,  Lifen Wu ,  Renee M. Zindell

IPC: A61K31/4545 ,  C07D211/60 ,  C07D401/12 ,  C07D405/04 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

CPC classification number: C07D413/12 ,  C07D211/60 ,  C07D401/12 ,  C07D405/04 ,  C07D417/12 ,  C07D417/14

Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Abstract translation: 公开了调节CB2受体的化合物。 根据本发明的化合物与CB2受体结合并且是激动剂，并且可用于治疗炎症。 作为激动剂的那些化合物另外可用于治疗疼痛。

公开(公告)号：US08575201B2

公开(公告)日：2013-11-05

申请号：US13237112

申请日：2011-09-20

Applicant: Alessandra Bartolozzi ,  Todd Bosanac ,  Zhidong Chen ,  Stephane De Lombaert ,  Jonathon Alan Dines ,  John D. Huber ,  Weimin W. Liu ,  Pui Leng Loke ,  Tina Marie Morwick ,  Alan Olague ,  Doris Riether ,  Heather Tye ,  Lifen Wu ,  Renee M. Zindell

Inventor： Alessandra Bartolozzi ,  Todd Bosanac ,  Zhidong Chen ,  Stephane De Lombaert ,  Jonathon Alan Dines ,  John D. Huber ,  Weimin W. Liu ,  Pui Leng Loke ,  Tina Marie Morwick ,  Alan Olague ,  Doris Riether ,  Heather Tye ,  Lifen Wu ,  Renee M. Zindell

IPC: A01N43/40 ,  A61K31/44

CPC classification number: C07D413/14

Abstract: The present invention relates to compounds of formula (I) and (IA): and pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Abstract translation: 本发明涉及式（I）和（IA）化合物及其药学上可接受的盐，其中R 1 -R 5如本文所定义。 本发明还涉及包含这些化合物的药物组合物，使用这些化合物治疗各种疾病和病症的方法，制备这些化合物的方法和可用于这些方法的中间体。

公开(公告)号：US08349871B2

公开(公告)日：2013-01-08

申请号：US13238054

申请日：2011-09-21

Applicant: Alessandra Bartolozzi ,  Angela Berry ,  Eugene Richard Hickey ,  Doris Riether ,  Achim Sauer ,  David Smith Thomson ,  Lifen Wu ,  Renee M. Zindell ,  Patricia Amouzegh ,  Nigel James Blumire ,  Stephen Peter East ,  Monika Ermann ,  Someina Khor ,  Innocent Mushi

Inventor： Alessandra Bartolozzi ,  Angela Berry ,  Eugene Richard Hickey ,  Doris Riether ,  Achim Sauer ,  David Smith Thomson ,  Lifen Wu ,  Renee M. Zindell ,  Patricia Amouzegh ,  Nigel James Blumire ,  Stephen Peter East ,  Monika Ermann ,  Someina Khor ,  Innocent Mushi

IPC: A61K31/454 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/42 ,  A61K31/427 ,  C07D401/12 ,  C07D285/135 ,  C07D261/14 ,  C07D249/14 ,  C07D277/46 ,  C07D277/62

CPC classification number: C07D413/12 ,  C07D249/14 ,  C07D261/14 ,  C07D405/12 ,  C07D413/04 ,  C07D413/14

Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Abstract translation: 公开了式（I）的化合物。 根据本发明的化合物结合并且是CB 2受体的激动剂，拮抗剂或反向激动剂，并且可用于治疗炎症。 作为激动剂的那些化合物另外可用于治疗疼痛。

公开(公告)号：US20070027183A1

公开(公告)日：2007-02-01

申请号：US11407500

申请日：2006-04-19

Applicant: Alessandra Bartolozzi ,  Stewart Campbell ,  Hope Foudoulakis ,  Enoch Kim ,  Paul Sweetnam ,  Yingfei Yang

Inventor： Alessandra Bartolozzi ,  Stewart Campbell ,  Hope Foudoulakis ,  Enoch Kim ,  Paul Sweetnam ,  Yingfei Yang

IPC: A61K31/4709 ,  C07D401/02

CPC classification number: C07D217/06 ,  A61K31/18 ,  A61K31/47 ,  A61K31/472 ,  A61K31/4725 ,  A61K45/06 ,  C07D417/04

Abstract: The present invention relates to compounds which are inhibitors of microsomal triglyceride transfer protein and/or apolipoprotein B (Apo B) secretion. These compounds can be useful for the prevention and treatment of various diseases, particularly atherosclerosis and its clinical sequelae, for lowering serum lipids, and related ailments. The invention further relates to pharmaceutical compositions comprising the compounds and to methods of treating diseases, such as hypertriglyceridemia, hyperchylomicronemia, atherosclerosis, obesity, and related conditions using the compounds. A method for decreasing apolipoprotein B (apo B) secretion is also provided.

Abstract translation: 本发明涉及作为微粒体甘油三酯转运蛋白和/或载脂蛋白B（Apo B）分泌抑制剂的化合物。 这些化合物可用于预防和治疗各种疾病，特别是动脉粥样硬化及其临床后遗症，用于降低血清脂质和相关疾病。 本发明进一步涉及包含该化合物的药物组合物以及使用该化合物治疗诸如高甘油三酯血症，高白蛋白血症，动脉粥样硬化，肥胖症和相关病症等疾病的方法。 还提供了降低载脂蛋白B（apo B）分泌的方法。

公开(公告)号：US20160039765A1

公开(公告)日：2016-02-11

申请号：US14660453

申请日：2015-03-17

Applicant: Alessandra Bartolozzi ,  Stewart Campbell ,  Hope Foudoulakis ,  Enoch Kim ,  Paul Sweetnam ,  Yingfei Yang

Inventor： Alessandra Bartolozzi ,  Stewart Campbell ,  Hope Foudoulakis ,  Enoch Kim ,  Paul Sweetnam ,  Yingfei Yang

IPC: C07D217/06 ,  A61K31/4725 ,  C07D417/04 ,  A61K45/06 ,  A61K31/472

CPC classification number: C07D217/06 ,  A61K31/18 ,  A61K31/47 ,  A61K31/472 ,  A61K31/4725 ,  A61K45/06 ,  C07D417/04

Abstract: The present invention relates to compounds which are inhibitors of microsomal triglyceride transfer protein and/or apolipoprotein B (Apo B) secretion. These compounds can be useful for the prevention and treatment of various diseases, particularly atherosclerosis and its clinical sequelae, for lowering serum lipids, and related ailments. The invention further relates to pharmaceutical compositions comprising the compounds and to methods of treating diseases, such as hypertriglyceridemia, hyperchylomicronemia, atherosclerosis, obesity, and related conditions using the compounds. A method for decreasing apolipoprotein B (apo B) secretion is also provided.

Abstract translation: 本发明涉及作为微粒体甘油三酯转运蛋白和/或载脂蛋白B（Apo B）分泌抑制剂的化合物。 这些化合物可用于预防和治疗各种疾病，特别是动脉粥样硬化及其临床后遗症，用于降低血清脂质和相关疾病。 本发明进一步涉及包含该化合物的药物组合物以及使用该化合物治疗诸如高甘油三酯血症，高白蛋白血症，动脉粥样硬化，肥胖症和相关病症等疾病的方法。 还提供了降低载脂蛋白B（apo B）分泌的方法。

公开(公告)号：US09174980B2

公开(公告)日：2015-11-03

申请号：US13752640

申请日：2013-01-29

Applicant: Alessandra Bartolozzi ,  Zhidong Chen ,  Jonathon Alan Dines ,  Ho Yin Lo ,  Pui Leng Loke ,  Alan Olague ,  Doris Riether ,  Heather Tye ,  Lifen Wu ,  Renee M. Zindell

Inventor： Alessandra Bartolozzi ,  Zhidong Chen ,  Jonathon Alan Dines ,  Ho Yin Lo ,  Pui Leng Loke ,  Alan Olague ,  Doris Riether ,  Heather Tye ,  Lifen Wu ,  Renee M. Zindell

IPC: C07D403/10 ,  A61K31/404 ,  C07D471/04 ,  C07D409/14 ,  C07D413/14 ,  C07D403/14 ,  C07D417/14 ,  C07D413/10 ,  C07D417/10 ,  C07D405/14 ,  C07D401/14 ,  C07D401/12

CPC classification number: C07D471/04 ,  A61K31/404 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14

Abstract: The present invention relates to compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R7, A and HET are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐，其中R 1 -R 7，A和HET如本文所定义。 本发明还涉及包含这些化合物的药物组合物，使用这些化合物治疗各种疾病和病症的方法，制备这些化合物的方法和可用于这些方法的中间体。

公开(公告)号：US08383651B2

公开(公告)日：2013-02-26

申请号：US12882328

申请日：2010-09-15

Applicant: Alessandra Bartolozzi ,  Doris Riether ,  Renee M. Zindell ,  Patricia Amouzegh ,  Nigel James Blumire ,  Monika Ermann ,  Innocent Mushi ,  Robert John Scott

Inventor： Alessandra Bartolozzi ,  Doris Riether ,  Renee M. Zindell ,  Patricia Amouzegh ,  Nigel James Blumire ,  Monika Ermann ,  Innocent Mushi ,  Robert John Scott

IPC: A61K31/351 ,  A61K31/4525 ,  A61K31/4196 ,  C07D401/12 ,  C07D249/08 ,  C07D413/12 ,  C07D407/12

CPC classification number: C07D413/14 ,  C07D413/04 ,  C07D413/06 ,  C07D417/04 ,  C07D417/14

Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Abstract translation: 公开了式（I）的化合物。 根据本发明的化合物结合并且是CB 2受体的激动剂，拮抗剂或反向激动剂，并且可用于治疗炎症。 作为激动剂的那些化合物另外可用于治疗疼痛。

公开(公告)号：US08372874B2

公开(公告)日：2013-02-12

申请号：US12564133

申请日：2009-09-22

Applicant: Alessandra Bartolozzi ,  Eugene Richard Hickey ,  Doris Riether ,  Lifen Wu ,  Renee M. Zindell ,  Monika Ermann

Inventor： Alessandra Bartolozzi ,  Eugene Richard Hickey ,  Doris Riether ,  Lifen Wu ,  Renee M. Zindell ,  Monika Ermann

IPC: A61K31/4196 ,  A61K31/42 ,  A61K31/422 ,  C07D261/14 ,  C07D249/14

CPC classification number: C07D413/12 ,  C07D249/14 ,  C07D261/14 ,  C07D405/12 ,  C07D413/04 ,  C07D413/14

Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

公开(公告)号：US08357693B2

公开(公告)日：2013-01-22

申请号：US11887218

申请日：2006-03-27

Applicant: Alessandra Bartolozzi ,  Stewart Campbell ,  Hope Foudoulakis ,  Brian Kirk ,  Siya Ram ,  Paul Sweetnam

Inventor： Alessandra Bartolozzi ,  Stewart Campbell ,  Hope Foudoulakis ,  Brian Kirk ,  Siya Ram ,  Paul Sweetnam

IPC: A01N43/54 ,  A61K31/517

CPC classification number: C07D413/14 ,  B82Y30/00 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14

Abstract: The present invention relates to inhibitors of ROCK1 and ROCK2 and methods of modulating the pharmacokinetic and/or pharmacodynamic properties of such compounds. Also provided are methods of inhibiting ROCK1 and or ROCK2 that are useful for the treatment of disease.

Abstract translation: 本发明涉及ROCK1和ROCK2的抑制剂和调节这些化合物的药代动力学和/或药效学性质的方法。 还提供抑制可用于治疗疾病的ROCK1和/或ROCK2的方法。

公开(公告)号：US08299103B2

公开(公告)日：2012-10-30

申请号：US12791213

申请日：2010-06-01

Applicant: Alessandra Bartolozzi ,  Eugene Richard Hickey ,  Doris Riether

Inventor： Alessandra Bartolozzi ,  Eugene Richard Hickey ,  Doris Riether

IPC: A61K31/42 ,  A61K31/41 ,  C07D285/08 ,  C07D277/28 ,  C07D261/04 ,  C07D257/00

CPC classification number: C07D413/12 ,  C07D261/14 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Abstract translation: 公开了式（I）的化合物。 根据本发明的化合物结合并且是CB 2受体的激动剂，拮抗剂或反向激动剂，并且可用于治疗炎症。 作为激动剂的那些化合物另外可用于治疗疼痛。