公开(公告)号：US20120136014A1

公开(公告)日：2012-05-31

申请号：US13151683

申请日：2011-06-02

Applicant: Zhiyong Chen ,  Christopher J. Creghton ,  Mark Cunningham ,  John Finn ,  Mark Hilgers ,  Michael Jung ,  Lucy Aguirre Kohnen ,  Thanh Lam ,  Xiaoming Li ,  Mark Stidham ,  Les Tari ,  Michael Trzoss ,  Junhu Zhang

Inventor： Zhiyong Chen ,  Christopher J. Creghton ,  Mark Cunningham ,  John Finn ,  Mark Hilgers ,  Michael Jung ,  Lucy Aguirre Kohnen ,  Thanh Lam ,  Xiaoming Li ,  Mark Stidham ,  Les Tari ,  Michael Trzoss ,  Junhu Zhang

IPC: A61K31/517 ,  C07D401/14 ,  C07D239/72 ,  A61P31/10 ,  A61P33/00 ,  A61P31/04 ,  A61P29/00 ,  C12N9/99 ,  C07D417/14

CPC classification number: C07D401/14 ,  C07D239/95 ,  C07D417/14

Abstract: The present disclosure provides compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R5, R6 and Z are as described herein. The disclosure also provides pharmaceutical compositions thereof; and methods for inhibiting DHFR activity; and methods for treating cell proliferative diseases, autoimmune disease, inflammatory disease or bacterial, fungal or parasitic infection by administering a compound of Formula I.

Abstract translation: 本公开提供式I化合物或其药学上可接受的盐，其中R 5，R 6和Z如本文所述。 本公开还提供其药物组合物; 和抑制DHFR活性的方法; 以及通过给予式I化合物治疗细胞增殖性疾病，自身免疫疾病，炎性疾病或细菌，真菌或寄生虫感染的方法。

公开(公告)号：US20140343458A1

公开(公告)日：2014-11-20

申请号：US14121045

申请日：2014-07-24

Applicant: Zhiyong Chen ,  Zhilin Liao ,  Frank C. Tortella ,  Xi-Chun May Lu ,  Jitendra R. Dave ,  Jay E. Bartlett ,  Mark F. Arnold ,  Mark P. Easterday ,  Mark W. Brown ,  Larry R. Holmes ,  Zachary J. Larimore ,  Kara E. Schmid ,  Deborah A. Shear ,  Lai Yee Leung ,  Andrea Mountney

Inventor： Zhiyong Chen ,  Zhilin Liao ,  Frank C. Tortella ,  Xi-Chun May Lu ,  Jitendra R. Dave ,  Jay E. Bartlett ,  Mark F. Arnold ,  Mark P. Easterday ,  Mark W. Brown ,  Larry R. Holmes ,  Zachary J. Larimore ,  Kara E. Schmid ,  Deborah A. Shear ,  Lai Yee Leung ,  Andrea Mountney

IPC: A61B5/00 ,  G01L5/00 ,  A01K29/00

CPC classification number: A61B5/4064 ,  A01K29/00 ,  A22B3/02 ,  A61B5/1036 ,  A61B5/6803 ,  A61B2503/40 ,  A61B2562/0247 ,  F41B11/60 ,  G01L5/0052

Abstract: An apparatus and method for inflicting brain injury on a laboratory animal that employs a platform for supporting the laboratory animal. The platform defines an opening for positioning the head of the laboratory animal over the opening. A projectile is launched from a projectile launching device orientated below the opening of the platform. The projectile launching device has a means for propelling the projectile directly at and/or through the opening of said platform, thereby inflicting brain injury on the animal via either a pressure wave or concussive impact of the projectile. Without helmet, direct impact of the projectile results in severe traumatic brain injury. Use of helmet protects animals from skull fracture, subdural hematoma, intracerebral hemorrhage and contusion yet produces mild concussion-like pathology.

Abstract translation: 在实验室动物身上造成脑损伤的装置和方法，该实验动物采用支撑实验室动物的平台。 平台定义了用于将实验室动物的头部定位在开口上的开口。 弹射器从位于平台开口下方的射弹发射装置发射。 射弹发射装置具有在所述平台的开口处和/或通过所述平台的开口直接推进射弹的手段，从而通过射弹的压力波或震荡冲击对动物造成脑损伤。 没有头盔，射弹的直接影响会导致严重的创伤性脑损伤。 使用头盔保护动物免受颅骨骨折，硬膜下血肿，脑内出血和挫伤，但产生轻度脑震荡样病理。

公开(公告)号：US20120238751A1

公开(公告)日：2012-09-20

申请号：US13496188

申请日：2012-03-14

Applicant: Daniel Bensen ,  Zhiyong Chen ,  John Finn ,  Thanh To Lam ,  Suk Joong Lee ,  Xiaoming Li ,  Douglas W. Phillipson ,  Leslie William Tari ,  Michael Trzoss ,  Junhu Zhang ,  Felice C. Lightstone ,  Toan B. Nguyen ,  Sergio E. Wong ,  Paul Aristoff ,  Michael Jung

Inventor： Daniel Bensen ,  Zhiyong Chen ,  John Finn ,  Thanh To Lam ,  Suk Joong Lee ,  Xiaoming Li ,  Douglas W. Phillipson ,  Leslie William Tari ,  Michael Trzoss ,  Junhu Zhang ,  Felice C. Lightstone ,  Toan B. Nguyen ,  Sergio E. Wong ,  Paul Aristoff ,  Michael Jung

IPC: C07D487/04 ,  C07D471/10 ,  C07D487/08 ,  C07D471/08 ,  C07D487/10 ,  C07D491/048 ,  C07D491/056 ,  C07D487/14 ,  C07D471/14 ,  C07D471/04 ,  C07D498/04

CPC classification number: C07D487/04 ,  C07D487/14

Abstract: Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors.Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.

Abstract translation: 本文公开了具有式I结构的化合物及其药学上合适的盐，酯和前药，其可用作抗菌三环类回旋酶抑制剂。 还考虑了相关的药物组合物，用途和制备化合物的方法。

公开(公告)号：US08835445B2

公开(公告)日：2014-09-16

申请号：US13151683

申请日：2011-06-02

Applicant: Zhiyong Chen ,  Christopher J. Creighton ,  Mark Cunningham ,  John Finn ,  Mark Hilgers ,  Michael Jung ,  Lucy Aguirre Kohnen ,  Thanh Lam ,  Xiaoming Li ,  Mark Stidham ,  Les Tari ,  Michael Trzoss ,  Junhu Zhang

Inventor： Zhiyong Chen ,  Christopher J. Creighton ,  Mark Cunningham ,  John Finn ,  Mark Hilgers ,  Michael Jung ,  Lucy Aguirre Kohnen ,  Thanh Lam ,  Xiaoming Li ,  Mark Stidham ,  Les Tari ,  Michael Trzoss ,  Junhu Zhang

IPC: A01N43/54 ,  A61K31/517 ,  C07D239/72 ,  C07D401/00

CPC classification number: C07D401/14 ,  C07D239/95 ,  C07D417/14

Abstract: The present disclosure provides compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R5, R6 and Z are as described herein. The disclosure also provides pharmaceutical compositions thereof; and methods for inhibiting DHFR activity; and methods for treating cell proliferative diseases, autoimmune disease, inflammatory disease or bacterial, fungal or parasitic infection by administering a compound of Formula I.

Abstract translation: 本公开提供式I化合物或其药学上可接受的盐，其中R 5，R 6和Z如本文所述。 本公开还提供其药物组合物; 和抑制DHFR活性的方法; 以及通过给予式I化合物治疗细胞增殖性疾病，自身免疫疾病，炎性疾病或细菌，真菌或寄生虫感染的方法。