公开(公告)号：US20110319378A1

公开(公告)日：2011-12-29

申请号：US13153345

申请日：2011-06-03

Applicant: Michael David BARTBERGER ,  Ana GONZALEZ BUENROSTRO ,  Hilary Plake BECK ,  Xiaoqi CHEN ,  Richard Victor CONNORS ,  Jeffrey DEIGNAN ,  Jason DUQUETTE ,  John EKSTEROWICZ ,  Benjamin FISHER ,  Brian Matthew FOX ,  Jiasheng FU ,  Zice FU ,  Felix GONZALEZ LOPEZ DE TURISO ,  Michael GRIBBLE, JR. ,  Darin James GUSTIN ,  Julie Anne HEATH ,  Xin HUANG ,  Xianyun JIAO ,  Michael G. JOHNSON ,  Frank KAYSER ,  David John KOPECKY ,  Sujen LAI ,  Yihong LI ,  Zhihong LI ,  Jiwen LIU ,  Jonathan Dante LOW ,  Brian Stuart LUCAS ,  Zhihua MA ,  Lawrence McGEE ,  Joel McINTOSH ,  Dustin McMINN ,  Julio Cesar MEDINA ,  Jeffrey Thomas MIHALIC ,  Steven Howard Olson ,  Yosup REW ,  Philip Marley ROVETO ,  Daqing SUN ,  Xiaodong WANG ,  Yingcai WANG ,  Xuelei YAN ,  Ming YU ,  Jiang ZHU

Inventor： Michael David BARTBERGER ,  Ana GONZALEZ BUENROSTRO ,  Hilary Plake BECK ,  Xiaoqi CHEN ,  Richard Victor CONNORS ,  Jeffrey DEIGNAN ,  Jason DUQUETTE ,  John EKSTEROWICZ ,  Benjamin FISHER ,  Brian Matthew FOX ,  Jiasheng FU ,  Zice FU ,  Felix GONZALEZ LOPEZ DE TURISO ,  Michael GRIBBLE, JR. ,  Darin James GUSTIN ,  Julie Anne HEATH ,  Xin HUANG ,  Xianyun JIAO ,  Michael G. JOHNSON ,  Frank KAYSER ,  David John KOPECKY ,  Sujen LAI ,  Yihong LI ,  Zhihong LI ,  Jiwen LIU ,  Jonathan Dante LOW ,  Brian Stuart LUCAS ,  Zhihua MA ,  Lawrence McGEE ,  Joel McINTOSH ,  Dustin McMINN ,  Julio Cesar MEDINA ,  Jeffrey Thomas MIHALIC ,  Steven Howard Olson ,  Yosup REW ,  Philip Marley ROVETO ,  Daqing SUN ,  Xiaodong WANG ,  Yingcai WANG ,  Xuelei YAN ,  Ming YU ,  Jiang ZHU

IPC: A61K31/451 ,  C07D413/06 ,  A61K31/5377 ,  C07D401/06 ,  A61K31/454 ,  C07D417/06 ,  A61K31/541 ,  A61K31/4545 ,  C07D413/12 ,  C07D471/10 ,  A61K31/438 ,  C07D409/04 ,  A61K31/4535 ,  A61K31/496 ,  C07D279/02 ,  C07D498/08 ,  A61K31/5386 ,  A61K31/549 ,  C07D498/16 ,  A61K31/437 ,  A61P35/00 ,  C07D211/40

CPC classification number: C07D211/76 ,  C07D221/20 ,  C07D279/02 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D407/04 ,  C07D407/06 ,  C07D409/04 ,  C07D409/12 ,  C07D413/06 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D491/08 ,  C07D491/153 ,  C07D498/08 ,  C07D498/14 ,  C07D498/20

Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.

Abstract translation: 本发明提供了式I的MDM2抑制剂化合物，其中变量如上所定义，哪些化合物可用作治疗剂，特别是用于治疗癌症。 本发明还涉及含有MDM2抑制剂的药物组合物。

公开(公告)号：US07511043B2

公开(公告)日：2009-03-31

申请号：US10794228

申请日：2004-03-04

Applicant: Jonathan Houze ,  Sharon McKendry ,  Joshua Gergely ,  Yi Xia ,  Bei Shan ,  Frank Kayser

Inventor： Jonathan Houze ,  Sharon McKendry ,  Joshua Gergely ,  Yi Xia ,  Bei Shan ,  Frank Kayser

IPC: A61K31/497 ,  C07D241/36

CPC classification number: C07D209/48 ,  C07C233/75 ,  C07C237/22 ,  C07C311/19 ,  C07C311/29 ,  C07C2601/14 ,  C07D241/44 ,  C07D279/02

Abstract: The present invention provides compounds, pharmaceutical compositions and methods that are useful in modulating the farnesoid X receptor (FXR). As FXR is involved in negatively controlling the expression level of cholesterol 7α-hydroxylase (cyp7a), the rate-limiting enzyme involved in the oxidative metabolism of cholesterol into bile acids, the compounds described herein find utility in treating diseases associated with abnormally high or low cholesterol levels. In certain aspects, the FXR modulators (e.g., antagonists) described herein block the negative feed-back downregulation of cyp7a expression produced by certain cholic acids, the endogenous ligands for FXR. Moreover, as FXR forms heterodimers with the retinoid X receptor (RXR) in some cell types, modulation of the level of FXR activity in cells has a wide range of effects on a variety of biological processes which are mediated by RXR or other RXR-interacting proteins such as PPARγ and PPARα. Thus, compounds described herein are useful in treating other biological activities such as obesity, diabetes, lipid associated disorders, cancer, inflammatory disorders, disorders involving a disrupted or dysfunctional epidermal barrier, and various other metabolic disorders.

公开(公告)号：US07473703B2

公开(公告)日：2009-01-06

申请号：US11501594

申请日：2006-08-08

Applicant: Xian Yun Jiao ,  Frank Kayser ,  David J. Kopecky ,  Sharon McKendry ,  Derek E. Piper ,  Andrew K. Shiau

Inventor： Xian Yun Jiao ,  Frank Kayser ,  David J. Kopecky ,  Sharon McKendry ,  Derek E. Piper ,  Andrew K. Shiau

IPC: A61K31/40 ,  C07D207/325

CPC classification number: C07D207/333 ,  C07D207/335

Abstract: Heterocyclic arylsulfonamidobenzylic compounds are provided which are useful in treating lipid disorders, metabolic disorders and cell-proliferative diseases.

Abstract translation: 提供了可用于治疗脂质疾病，代谢紊乱和细胞增殖性疾病的杂环芳基磺酰氨基苄基化合物。

公开(公告)号：US07300932B2

公开(公告)日：2007-11-27

申请号：US10913307

申请日：2004-08-06

Applicant: Brian M. Fox ,  Kiyosei Iio ,  Takashi Inaba ,  Frank Kayser ,  Kexue Li ,  Shoichi Sagawa ,  Masahiro Tanaka ,  Atsuhito Yoshida

Inventor： Brian M. Fox ,  Kiyosei Iio ,  Takashi Inaba ,  Frank Kayser ,  Kexue Li ,  Shoichi Sagawa ,  Masahiro Tanaka ,  Atsuhito Yoshida

IPC: C07D487/04 ,  A61K31/5025

CPC classification number: C07D487/04

Abstract: Compounds, pharmaceutical compositions and methods that are useful in the treatment or prevention of metabolic and cell proliferative diseases or conditions are provided herein. In particular, the invention provides compounds which modulate the activity of proteins involved in lipid metabolism and cell proliferation.

Abstract translation: 本文提供了可用于治疗或预防代谢和细胞增殖性疾病或病症的化合物，药物组合物和方法。 特别地，本发明提供调节参与脂质代谢和细胞增殖的蛋白质的活性的化合物。

公开(公告)号：US20070244096A1

公开(公告)日：2007-10-18

申请号：US11743376

申请日：2007-05-02

Applicant: Brian Fox ,  Noboru Furukawa ,  Xiaolin Hao ,  Kiyosei Iio ,  Takashi Inaba ,  Simon Jackson ,  Frank Kayser ,  Marc Labelle ,  Kexue Li ,  Takuya Matsui ,  Dustin McMinn ,  Nobuya Ogawa ,  Steven Rubenstein ,  Shoichi Sagawa ,  Kazuyuki Sugimoto ,  Masahiro Suzuki ,  Masahiro Tanaka ,  Guosen Ye ,  Atsuhito Yoshida ,  Jian Zhang

Inventor： Brian Fox ,  Noboru Furukawa ,  Xiaolin Hao ,  Kiyosei Iio ,  Takashi Inaba ,  Simon Jackson ,  Frank Kayser ,  Marc Labelle ,  Kexue Li ,  Takuya Matsui ,  Dustin McMinn ,  Nobuya Ogawa ,  Steven Rubenstein ,  Shoichi Sagawa ,  Kazuyuki Sugimoto ,  Masahiro Suzuki ,  Masahiro Tanaka ,  Guosen Ye ,  Atsuhito Yoshida ,  Jian Zhang

IPC: A61K31/55 ,  A61K31/542 ,  A61K31/5383 ,  C07D497/02 ,  C07D498/02 ,  C07D491/02

CPC classification number: C07D491/04

Abstract: Compounds, pharmaceutical compositions and methods that are useful in the treatment or prevention of metabolic and cell proliferative diseases or conditions are provided herein. In particular, the invention provides compounds which modulate the activity of proteins involved in lipid metabolism and cell proliferation.

Abstract translation: 本文提供了可用于治疗或预防代谢和细胞增殖性疾病或病症的化合物，药物组合物和方法。 特别地，本发明提供调节参与脂质代谢和细胞增殖的蛋白质的活性的化合物。

公开(公告)号：US20060270718A1

公开(公告)日：2006-11-30

申请号：US11501594

申请日：2006-08-08

Applicant: Xian Jiao ,  Frank Kayser ,  David Kopecky ,  Sharon McKendry ,  Derek Piper ,  Andrew Shiau

Inventor： Xian Jiao ,  Frank Kayser ,  David Kopecky ,  Sharon McKendry ,  Derek Piper ,  Andrew Shiau

IPC: A61K31/44 ,  A61K31/426 ,  A61K31/421 ,  A61K31/4196 ,  A61K31/4192 ,  A61K31/4172

CPC classification number: C07D207/333 ,  C07D207/335

Abstract: Heterocyclic arylsulfonamidobenzylic compounds are provided which are useful in treating lipid disorders, metabolic disorders and cell-proliferative diseases.

公开(公告)号：US20060040965A1

公开(公告)日：2006-02-23

申请号：US11169313

申请日：2005-06-29

Applicant: Christopher Farthing ,  Paul Faulder ,  Alexander Frenkel ,  Martin Harrison ,  Xianyun Jiao ,  Frank Kayser ,  David Kopecky ,  Jinqian Liu ,  Sarah Lively ,  Rajiv Sharma ,  Stephen Shuttleworth

Inventor： Christopher Farthing ,  Paul Faulder ,  Alexander Frenkel ,  Martin Harrison ,  Xianyun Jiao ,  Frank Kayser ,  David Kopecky ,  Jinqian Liu ,  Sarah Lively ,  Rajiv Sharma ,  Stephen Shuttleworth

IPC: A61K31/519 ,  C07D487/02

CPC classification number: C07D487/04

Abstract: Compounds that modulate the action of ACK1 and LCK, and related compositions methods for treating ACK1- and LCK-mediated diseases are described. In one aspect, the compounds have the general structure: where the values of the substituents are provided herein.

Abstract translation: 描述了调节ACK1和LCK的作用的化合物以及用于治疗ACK1和LCK介导的疾病的相关组合物方法。 在一个方面，化合物具有一般结构：其中本文提供取代基的值。

公开(公告)号：US06455548B2

公开(公告)日：2002-09-24

申请号：US09795030

申请日：2001-02-27

Applicant: Jennifer Chee ,  Jill N. Johanson ,  Frank Kayser ,  William H. Parsons ,  Kathleen M. Rupprecht

Inventor： Jennifer Chee ,  Jill N. Johanson ,  Frank Kayser ,  William H. Parsons ,  Kathleen M. Rupprecht

IPC: A61K31454

CPC classification number: C07D409/04 ,  A61K31/445 ,  A61K31/4535 ,  A61K31/454 ,  C07D409/14 ,  C07D413/06 ,  C07D413/14

Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.

Abstract translation: 本发明涉及可用作趋化因子受体活性调节剂的式I的吡咯烷化合物（其中R1，R2，R3，R4c，R4d和R4f如本文所定义）。 特别地，这些化合物可用作趋化因子受体CCR-3和/或CCR-5的调节剂。

公开(公告)号：US06303637B1

公开(公告)日：2001-10-16

申请号：US09422500

申请日：1999-10-21

Applicant: Jianming Bao ,  Andrew Kotliar ,  Frank Kayser ,  William H. Parsons ,  Kathleen M. Rupprecht ,  Christopher F. Claiborne ,  David A. Claremon ,  Nigel Liverton ,  Wayne J. Thompson

Inventor： Jianming Bao ,  Andrew Kotliar ,  Frank Kayser ,  William H. Parsons ,  Kathleen M. Rupprecht ,  Christopher F. Claiborne ,  David A. Claremon ,  Nigel Liverton ,  Wayne J. Thompson

IPC: A61K31445

CPC classification number: C07D211/96 ,  A61K31/445 ,  A61K31/47 ,  A61K31/52 ,  A61K31/535 ,  A61K31/70 ,  A61K38/13 ,  A61K45/06 ,  C07D211/26 ,  A61K31/365 ,  A61K31/16 ,  A61K2300/00

Abstract: The present invention relates to a class of heterocyclic compounds of Formula I that are useful as potassium channel inhibitors to treat autoimmune disorders, cardiac arrhythmias, and the like.

Abstract translation: 本发明涉及可用作治疗自身免疫性疾病，心律失常等的钾通道抑制剂的一类式I的杂环化合物。

公开(公告)号：US06194458B1

公开(公告)日：2001-02-27

申请号：US09422499

申请日：1999-10-21

Applicant: Robert K. Baker ,  Jianming Bao ,  Frank Kayser ,  Andrew Kotliar ,  William H. Parsons ,  Kathleen M. Rupprecht ,  Christopher F. Claiborne ,  David A. Claremon ,  Nigel Liverton ,  Wayne J. Thompson

Inventor： Robert K. Baker ,  Jianming Bao ,  Frank Kayser ,  Andrew Kotliar ,  William H. Parsons ,  Kathleen M. Rupprecht ,  Christopher F. Claiborne ,  David A. Claremon ,  Nigel Liverton ,  Wayne J. Thompson

IPC: A61K3122

CPC classification number: C07D307/79 ,  A61K45/06 ,  C07C235/60 ,  C07C271/20

Abstract: This invention relates to benzamide potassium channel inhibitors of general structural Formula I. The compounds of this invention are useful in the treatment of autoimmune diseases, the prevention of rejection of foreign organ transplants and related afflictions, diseases and illnesses, and cardiac arrhythmias. Also within the scope of this invention are pharmaceutical formulations comprising a compound of Formula I and a pharmaceutical carrier, as well as pharmaceutical formulations comprising a compound of Formula I, one or more immunosuppressive compounds and a pharmaceutical carrier.

Abstract translation: 本发明涉及一般结构式I的苯甲酰胺钾通道抑制剂。本发明的化合物可用于治疗自身免疫性疾病，预防外来器官移植排斥和相关疾病，疾病和疾病以及心律失常。 也包括本发明范围的药物制剂，其包含式I化合物和药物载体，以及包含式I化合物，一种或多种免疫抑制化合物和药物载体的药物制剂。