公开(公告)号：US06358971B1

公开(公告)日：2002-03-19

申请号：US09674037

申请日：2000-12-04

Applicant: Jesus Ezquerra-Carrera ,  Joseph Michael Gruber ,  Chafiq Hamdouchi Hamdouchi ,  Richard Elmer Holmes ,  Wayne Alfred Spitzer

Inventor： Jesus Ezquerra-Carrera ,  Joseph Michael Gruber ,  Chafiq Hamdouchi Hamdouchi ,  Richard Elmer Holmes ,  Wayne Alfred Spitzer

IPC: A61K31437

CPC classification number: C07D471/04

Abstract: The present invention relates to compounds of Formula (I) below, which inhibit the growth of picornaviruses, Hepatitus viruses, enteroviruses, cardioviruses, polioviruses, coxsackieviruses of the A and B groups, echo virus and Mengo virus. wherein: A is phenyl, pyridyl, substituted phenyl, substituted pyridyl, or benzyl; R is hydrogen, COR4, or COCF3; X is N—OH, O, or CHR1; R1 is hydrogen, halo, CN, C1-C4 alkyl, —C≡CH, CO(C1-C4 alkyl), CO2(C1-C4 alkyl), or CONR2R3; R2 and R3 are independently hydrogen or C1-C4 alkyl; A′ is hydrogen, halo, C1-C6 alkyl, benzyl, naphthyl, thienyl, furyl, pyridyl, pyrollyl, COR4, S(O)nR4, or a group of the formula R4 is C1-C6 alkyl, phenyl, or substituted phenyl; n is 0, 1, or 2; R5 is independently at each occurrence hydrogen or halo; m is 1, 2, 3, or 4; and R6 is hydrogen, halo, CF3, OH, CO2H, NH2, NO2, CONHOCH3, C1-C4 alkyl, or CO2(C1-C4 alkyl), C1-C4 alkoxy; or a pharmaceutically acceptable salt thereof.

Abstract translation: 本发明涉及抑制小核糖核酸病毒，肝病毒，肠病毒，心脏病毒，脊髓灰质炎病毒，A组和B组柯萨克病毒，回波病毒和孟戈病毒的生长的下列式（I）的化合物。其中A是苯基，吡啶基 取代的苯基，取代的吡啶基或苄基; R是氢，COR4或COCF3; X是N-OH，O或CHR1; R1是氢，卤素，CN，C1-C4烷基，-C = CH， C1-C4烷基），CO2（C1-C4烷基）或CONR2R3; R2和R3独立地是氢或C1-C4烷基; A'是氢，卤素，C1-C6烷基，苄基，萘基，噻吩基，呋喃基，吡啶基 ，吡咯烷基，COR4，S（O）nR4或式R4的基团是C1-C6烷基，苯基或取代的苯基; n是0,1或2; R5各自独立地为氢或卤素; m为 1，2，3或4; 或者其药学上可接受的盐，R 6是氢，卤素，CF 3，OH，CO 2 H，NH 2，NO 2，CONHOCH 3，C 1 -C 4烷基或CO 2（C 1 -C 4烷基），C 1 -C 4烷氧基。

公开(公告)号：US06221876B1

公开(公告)日：2001-04-24

申请号：US09646063

申请日：2000-09-13

Applicant: Joseph Michael Gruber ,  Sean P Hollinshead ,  Bryan H Norman ,  Joseph W Wilson

Inventor： Joseph Michael Gruber ,  Sean P Hollinshead ,  Bryan H Norman ,  Joseph W Wilson

IPC: A61K3147

CPC classification number: C07D498/04

Abstract: The present invention relates to a compound of formula (I) which is useful for inhibiting neoplasms where the resistance is conferred in part or in total by MRP1.

Abstract translation: 本发明涉及可用于抑制由MRP1部分或全部赋予抗性的肿瘤的式（I）化合物。

公开(公告)号：US06743794B2

公开(公告)日：2004-06-01

申请号：US10130800

申请日：2002-05-21

Applicant: Rosanne Bonjouklian ,  Jeffrey Daniel Cohen ,  Joseph Michael Gruber ,  Douglas Webb Johnson ,  Louis Nickolaus Jungheim ,  Julian Stanley Kroin ,  Peter Ambrose Lander ,  Ho-Shen Lin ,  Mark Christopher Lohman ,  Brian Stephen Muehl ,  Bryan Hurst Norman ,  Vinod Francis Patel ,  Michael Enrico Richett ,  Kenneth Jeff Thrasher ,  Sreenivasarao Vepachedu ,  Wesley Todd White ,  Yongping Xie ,  Jeremy Schulenburg York ,  Brandon Lee Parkhurst ,  Qiupang Wang

Inventor： Rosanne Bonjouklian ,  Jeffrey Daniel Cohen ,  Joseph Michael Gruber ,  Douglas Webb Johnson ,  Louis Nickolaus Jungheim ,  Julian Stanley Kroin ,  Peter Ambrose Lander ,  Ho-Shen Lin ,  Mark Christopher Lohman ,  Brian Stephen Muehl ,  Bryan Hurst Norman ,  Vinod Francis Patel ,  Michael Enrico Richett ,  Kenneth Jeff Thrasher ,  Sreenivasarao Vepachedu ,  Wesley Todd White ,  Yongping Xie ,  Jeremy Schulenburg York ,  Brandon Lee Parkhurst ,  Qiupang Wang

IPC: A61K31496

CPC classification number: C07D471/04

Abstract: The present invention further relates to a method of inhibiting MRP1 in a mammal which comprises administering to a mammal in need thereof an effective amount of a compound of formula (I).