公开(公告)号：US20080153809A1

公开(公告)日：2008-06-26

申请号：US12033144

申请日：2008-02-19

Applicant: CHIH-HUNG LEE ,  Erol K. Bayburt ,  Stanley DiDomenico ,  Irene Drizin ,  Arthur R. Gomtsyan ,  John R. Koenig ,  Richard J. Perner ,  Robert G. Schmidt ,  Sean C. Turner ,  Tammie K. White ,  Guo Zhu Zheng

Inventor： CHIH-HUNG LEE ,  Erol K. Bayburt ,  Stanley DiDomenico ,  Irene Drizin ,  Arthur R. Gomtsyan ,  John R. Koenig ,  Richard J. Perner ,  Robert G. Schmidt ,  Sean C. Turner ,  Tammie K. White ,  Guo Zhu Zheng

IPC: A61K31/55 ,  C07D213/02 ,  A61K31/44 ,  C07D221/00 ,  A61K31/4523 ,  A61K31/4375 ,  A61K31/506 ,  A61P43/00 ,  A61K31/439 ,  C07D239/24 ,  C07D221/02 ,  C07D295/00 ,  A61K31/5377 ,  C07D223/02

CPC classification number: C07D451/02 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D417/04 ,  C07D471/08 ,  C07D487/08

Abstract: The present invention relates to compounds of formula (I-VII) or a pharmaceutically acceptable salt or prodrug thereof, in which A, L, R6, R7 and R8 are defined herein. The present invention also relates to methods of treating pain using these compounds and pharmaceutical compositions including these compounds.

Abstract translation: 本发明涉及式（I-VII）化合物或其药学上可接受的盐或前药，其中A，L，R 6，R 7和R 7， 本文定义了SUB 8。 本发明还涉及使用这些化合物治疗疼痛的方法和包括这些化合物的药物组合物。

公开(公告)号：US07074805B2

公开(公告)日：2006-07-11

申请号：US10364210

申请日：2003-02-11

Applicant: Chih-Hung Lee ,  Erol K. Bayburt ,  Stanley DiDomenico, Jr. ,  Irene Drizin ,  Arthur R. Gomtsyan ,  John R. Koenig ,  Richard J. Perner ,  Robert G. Schmidt, Jr. ,  Sean C. Turner ,  Tammie K. White ,  Guo Zhu Zheng

Inventor： Chih-Hung Lee ,  Erol K. Bayburt ,  Stanley DiDomenico, Jr. ,  Irene Drizin ,  Arthur R. Gomtsyan ,  John R. Koenig ,  Richard J. Perner ,  Robert G. Schmidt, Jr. ,  Sean C. Turner ,  Tammie K. White ,  Guo Zhu Zheng

IPC: A61K31/47 ,  C07D217/00

CPC classification number: C07D249/08 ,  C07D209/08 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07D217/26 ,  C07D231/12 ,  C07D231/56 ,  C07D233/56 ,  C07D237/28 ,  C07D401/12 ,  C07D405/12

Abstract: The isoquinoline compounds of formula (I) are VR1 antagonists that are useful in treating pain, inflammation, thermal hyperalgesia, urinary incontinence and bladder over activity. The “R”, “Z” and “L” variables are defined in the disclosure and the “X” variables are defined as follows: X1 is CR1; X2 is selected from the group consisting of N and CR2; X3 is selected from the group consisting of N and CR3; X4 is CR4; and X5 is selected from the group consisting of N and C.

Abstract translation: 式（I）的异喹啉化合物是可用于治疗疼痛，炎症，热痛觉过敏，尿失禁和膀胱过度活动的VR1拮抗剂。 在本公开中定义了“R”，“Z”和“L”变量，“X”变量定义如下：X 1是CR 1 1。 X 2选自N和CR 2; X 3选自N和CR 3; X 4是CR 4; 并且X 5选自N和C。

公开(公告)号：US06693136B1

公开(公告)日：2004-02-17

申请号：US10206265

申请日：2002-07-26

Applicant: Chih-Hung Lee ,  Meiqun Jiang ,  Richard A. Perner ,  Arthur Gomtsyan ,  Erol K. Bayburt ,  Guo Zhu Zheng

Inventor： Chih-Hung Lee ,  Meiqun Jiang ,  Richard A. Perner ,  Arthur Gomtsyan ,  Erol K. Bayburt ,  Guo Zhu Zheng

IPC: A61K3118

CPC classification number: C07C311/21 ,  C07C311/29 ,  C07C2603/18 ,  C07C2603/24

Abstract: Compounds of formula (I) are novel P2X3 and P2X2/P2X3 containing receptor antagonists and are useful in treating pain, urinary incontinence, and bladder overactivity.

Abstract translation: 式（I）化合物是新型P2X3和P2X2 / P2X3受体拮抗剂，可用于治疗疼痛，尿失禁和膀胱过度活动。

公开(公告)号：US20160263093A1

公开(公告)日：2016-09-15

申请号：US14757822

申请日：2015-12-23

Applicant: Jermaine Thomas ,  Sha Mi ,  Edward Yin-Shiang ,  Guo Zhu Zheng ,  Bin Ma ,  Richard D. Caldwell ,  Kevin Guckian ,  Gnanasambandam Kumaravel

Inventor： Jermaine Thomas ,  Sha Mi ,  Edward Yin-Shiang ,  Guo Zhu Zheng ,  Bin Ma ,  Richard D. Caldwell ,  Kevin Guckian ,  Gnanasambandam Kumaravel

IPC: A61K31/445 ,  A61K39/395 ,  C07K16/28 ,  A61K38/21 ,  A61K31/695 ,  A61K31/55 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/4545 ,  A61K31/225 ,  A61K31/517

CPC classification number: A61K31/445 ,  A61K31/225 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/517 ,  A61K31/55 ,  A61K31/695 ,  A61K38/21 ,  A61K39/3955 ,  C07D211/34 ,  C07D211/60 ,  C07D211/62 ,  C07D215/20 ,  C07D401/06 ,  C07D405/12 ,  C07K16/2842

Abstract: Compounds of formula (I) or (II) can modulate the activity of S1P receptors.

Abstract translation: 式（I）或（II）的化合物可以调节S1P受体的活性。

公开(公告)号：US20140100195A1

公开(公告)日：2014-04-10

申请号：US13646143

申请日：2012-10-05

Applicant: Richard D. Caldwell ,  Kevin M. GUCKIAN ,  Gnanasambandam KUMARA VEL ,  Wen-Cherng LEE ,  Edward Yin-Shiang LIN ,  Xiaogao LlU ,  Bin MA ,  Daniel M. SCOTT ,  Zhan SHl ,  Jermaine THOMAS ,  Arthur G. TAVERAS ,  Guo Zhu ZHENG

Inventor： Richard D. Caldwell ,  Kevin M. GUCKIAN ,  Gnanasambandam KUMARA VEL ,  Wen-Cherng LEE ,  Edward Yin-Shiang LIN ,  Xiaogao LlU ,  Bin MA ,  Daniel M. SCOTT ,  Zhan SHl ,  Jermaine THOMAS ,  Arthur G. TAVERAS ,  Guo Zhu ZHENG

IPC: A61K31/685 ,  A61K31/195 ,  C07C229/36 ,  A61K31/216 ,  C07C217/58 ,  A61K31/137 ,  C07D263/24 ,  A61K31/421 ,  C07D215/20 ,  A61K31/47 ,  C07F9/60 ,  A61K31/675 ,  C07D239/80 ,  A61K31/517 ,  C07D413/04 ,  C07F9/6512 ,  C07D277/64 ,  A61K31/428 ,  A61P37/06 ,  A61P7/00 ,  C07C233/47

CPC classification number: C07F9/6512 ,  C07C217/58 ,  C07C217/74 ,  C07C229/36 ,  C07C233/47 ,  C07C2602/10 ,  C07D215/06 ,  C07D215/20 ,  C07D215/227 ,  C07D233/32 ,  C07D239/74 ,  C07D239/80 ,  C07D263/24 ,  C07D277/64 ,  C07D401/04 ,  C07F9/091 ,  C07F9/60 ,  C07F9/65744

Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Abstract translation: 提供了在一种或多种S1P受体上具有激动剂活性的化合物。 化合物是鞘氨醇类似物，其在磷酸化之后可以作为S1P受体的激动剂。

公开(公告)号：US08592467B2

公开(公告)日：2013-11-26

申请号：US12489269

申请日：2009-06-22

Applicant: Marlon D. Cowart ,  Minghua Sun ,  Chen Zhao ,  Guo Zhu Zheng

Inventor： Marlon D. Cowart ,  Minghua Sun ,  Chen Zhao ,  Guo Zhu Zheng

IPC: A61K31/428 ,  C07D277/62

CPC classification number: C07D277/64 ,  C07D417/04 ,  C07D417/08 ,  C07D417/12 ,  C07D487/04

Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).

公开(公告)号：US20100222358A1

公开(公告)日：2010-09-02

申请号：US12715660

申请日：2010-03-02

Applicant: Marlon D. Cowart ,  Chen Zhao ,  Minghua Sun ,  Lawrence A. Black ,  Guo Zhu Zheng ,  Robert J. Gregg ,  Geoff G.Z. Zhang ,  Ahmad Y. Sheikh ,  Xiaochun Lou ,  Rodger F. Henry ,  David M. Barnes ,  Lawrence Kolaczkowski ,  Anthony R. Haight ,  Sou-Jen Chang ,  Steven J. Wittenberger ,  Michael G. Fickes

Inventor： Marlon D. Cowart ,  Chen Zhao ,  Minghua Sun ,  Lawrence A. Black ,  Guo Zhu Zheng ,  Robert J. Gregg ,  Geoff G.Z. Zhang ,  Ahmad Y. Sheikh ,  Xiaochun Lou ,  Rodger F. Henry ,  David M. Barnes ,  Lawrence Kolaczkowski ,  Anthony R. Haight ,  Sou-Jen Chang ,  Steven J. Wittenberger ,  Michael G. Fickes

IPC: A61K31/501 ,  A61K31/407 ,  C07D487/04 ,  A61K31/47 ,  C07D215/00 ,  A61K31/4439 ,  C07D401/14 ,  A61K31/428 ,  C07D417/14 ,  A61K31/4164 ,  C07D233/00 ,  C07D403/14 ,  A61K31/506 ,  A61K31/497 ,  A61P3/04 ,  A61P5/00 ,  A61P11/06 ,  A61P25/00 ,  A61P29/00 ,  A61P37/08 ,  A61P1/02

CPC classification number: C07D487/04

Abstract: Octahydro-pyrrolo[3,4-b]pyrrole derivatives are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.

Abstract translation: 八氢吡咯并[3,4-b]吡咯衍生物可用于治疗组胺-3受体配体预防或改善的病症或病症。 八氢吡咯并[3,4-b]吡咯化合物，使用这些化合物的方法，制备它们的组合物和制备这些化合物的方法在本文中公开。

公开(公告)号：US06831193B2

公开(公告)日：2004-12-14

申请号：US10141989

申请日：2002-05-10

Applicant: Chih-Hung Lee ,  Richard J. Perner ,  Daniel P. Larson ,  John R. Koenig ,  Arthur R. Gomtsyan ,  Guo Zhu Zheng ,  Stanley DiDomenico ,  Andrew O. Stewart ,  Erol K. Bayburt

Inventor： Chih-Hung Lee ,  Richard J. Perner ,  Daniel P. Larson ,  John R. Koenig ,  Arthur R. Gomtsyan ,  Guo Zhu Zheng ,  Stanley DiDomenico ,  Andrew O. Stewart ,  Erol K. Bayburt

IPC: C07C22900

CPC classification number: C07D213/40 ,  C07D213/68 ,  C07D213/71 ,  C07D239/34 ,  C07D309/12 ,  C07D317/72 ,  C07D333/20 ,  C07D333/34 ,  C07D333/72

Abstract: Compounds of formula (I) are novel P2X3 and P2X2/P2X3 antagonists which are useful in treating pain, urinary incontinence and bladder overactivity.

Abstract translation: 式（I）化合物是可用于治疗疼痛，尿失禁和膀胱过度活动的新型P2X3和P2X2 / P2X3拮抗剂。

公开(公告)号：US20140371209A1

公开(公告)日：2014-12-18

申请号：US13983489

申请日：2012-02-03

Applicant: Jermaine Thomas ,  Sha Mi ,  Edward Yin-Shiang Lin ,  Guo Zhu Zheng ,  Bin Ma ,  Kevin Guckian ,  Gnanasambandam Kumaravel

Inventor： Jermaine Thomas ,  Sha Mi ,  Edward Yin-Shiang Lin ,  Guo Zhu Zheng ,  Bin Ma ,  Richard D. Caldwell ,  Kevin Guckian ,  Gnanasambandam Kumaravel

IPC: C07D401/06 ,  C07D211/62 ,  C07D215/20

CPC classification number: A61K31/445 ,  A61K31/225 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/517 ,  A61K31/55 ,  A61K31/695 ,  A61K38/21 ,  A61K39/3955 ,  C07D211/34 ,  C07D211/60 ,  C07D211/62 ,  C07D215/20 ,  C07D401/06 ,  C07D405/12 ,  C07K16/2842

Abstract: Compounds of formula (I) or (II) can modulate the activity of SIP receptors.

Abstract translation: 式（I）或（II）的化合物可以调节SIP受体的活性。

公开(公告)号：US08399468B2

公开(公告)日：2013-03-19

申请号：US12715660

申请日：2010-03-02

Applicant: Marlon D. Cowart ,  Chen Zhao ,  Minghua Sun ,  Lawrence A. Black ,  Guo Zhu Zheng ,  Robert J. Gregg ,  Geoff G. Z. Zhang ,  Ahmad Y. Sheikh ,  Xiaochun Lou ,  Rodger F. Henry ,  David M. Barnes ,  Lawrence Kolaczkowski ,  Anthony R. Haight ,  Sou-Jen Chang ,  Steven J. Wittenberger ,  Michael G. Fickes

Inventor： Marlon D. Cowart ,  Chen Zhao ,  Minghua Sun ,  Lawrence A. Black ,  Guo Zhu Zheng ,  Robert J. Gregg ,  Geoff G. Z. Zhang ,  Ahmad Y. Sheikh ,  Xiaochun Lou ,  Rodger F. Henry ,  David M. Barnes ,  Lawrence Kolaczkowski ,  Anthony R. Haight ,  Sou-Jen Chang ,  Steven J. Wittenberger ,  Michael G. Fickes

IPC: A61K31/501 ,  C07D403/10

CPC classification number: C07D487/04

Abstract: Octahydro-pyrrolo[3,4-b]pyrrole derivatives are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.

Abstract translation: 八氢吡咯并[3,4-b]吡咯衍生物可用于治疗组胺-3受体配体预防或改善的病症或病症。 八氢吡咯并[3,4-b]吡咯化合物，使用这些化合物的方法，制备它们的组合物和制备这些化合物的方法在本文中公开。