公开(公告)号：US20050176955A1

公开(公告)日：2005-08-11

申请号：US10508094

申请日：2003-03-12

Applicant: Melissa Egbertson ,  H. Marie Langford ,  Jeffrey Melamed ,  John Wai ,  Wei Han ,  Debbie Perlow ,  Linghang Zhuang ,  Mark Embrey ,  Steven Young

Inventor： Melissa Egbertson ,  H. Marie Langford ,  Jeffrey Melamed ,  John Wai ,  Wei Han ,  Debbie Perlow ,  Linghang Zhuang ,  Mark Embrey ,  Steven Young

IPC: A61K31/4375 ,  A61K31/541 ,  A61K31/549 ,  A61K45/00 ,  A61P31/18 ,  A61P43/00 ,  C07D471/02 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: N-(Substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides are inhibitors of HIV integrase and inhibitors of HIV replication. The naphthyridine carboxamides are of Formula (I): wherein R1′, R2′ and R3′ are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are described.

Abstract translation: N-（取代的苄基）-8-羟基-1,6-萘啶-7-甲酰胺是HIV整合酶和HIV复制抑制剂的抑制剂。 萘啶甲酰胺具有式（I）：其中R 1，R 2和R 3'在本文中定义。 这些化合物可用于预防和治疗艾滋病毒感染以及预防，延迟艾滋病的发病和治疗。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。 描述了预防，治疗或延缓AIDS发病的方法以及预防或治疗HIV感染的方法。

公开(公告)号：US07538112B2

公开(公告)日：2009-05-26

申请号：US11579772

申请日：2005-05-03

Applicant: John S. Wai ,  Joseph P. Vacca ,  Linghang Zhuang ,  Boyoung Kim ,  Terry A. Lyle ,  Catherine M. Wiscount ,  Melissa S. Egbertson ,  Lou Anne Neilson ,  Mark Embrey ,  Thorsten E. Fisher ,  Donnette D. Staas

Inventor： John S. Wai ,  Joseph P. Vacca ,  Linghang Zhuang ,  Boyoung Kim ,  Terry A. Lyle ,  Catherine M. Wiscount ,  Melissa S. Egbertson ,  Lou Anne Neilson ,  Mark Embrey ,  Thorsten E. Fisher ,  Donnette D. Staas

IPC: C07D487/14 ,  A61K31/5025 ,  A61K31/4985

CPC classification number: A61K31/5025 ,  C07D487/14 ,  Y02A50/414

Abstract: Hydroxy-substituted pyrazinopyrrolopyridazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I) wherein R1, R2, R3, R4, R5, R6 and R7 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Abstract translation: 羟基取代的吡嗪并吡咯并哒嗪二酮化合物是HIV整合酶和HIV复制抑制剂的抑制剂。 在一个实施方案中，二酮化合物具有式（I），其中R 1，R 2，R 3，R 4，R 5，R 6和R 7在本文中定义。 这些化合物可用于预防和治疗艾滋病毒感染以及预防，延迟艾滋病的发病和治疗。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

公开(公告)号：US07323460B2

公开(公告)日：2008-01-29

申请号：US10508094

申请日：2003-03-12

Applicant: Melissa Egbertson ,  H. Marie Langford ,  Jeffrey Y. Melamed ,  John S. Wai ,  Wei Han ,  Debbie S. Perlow ,  Linghang Zhuang ,  Mark Embrey

Inventor： Melissa Egbertson ,  H. Marie Langford ,  Jeffrey Y. Melamed ,  John S. Wai ,  Wei Han ,  Debbie S. Perlow ,  Linghang Zhuang ,  Mark Embrey

IPC: C07D401/02 ,  A61K31/4375

CPC classification number: C07D471/04

Abstract: N-(Substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides are inhibitors of HIV integrase and inhibitors of HIV replication. The naphthyridine carboxamides are of Formula (I): wherein R1′, R2′ and R3′ are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are described.

Abstract translation: N-（取代的苄基）-8-羟基-1,6-萘啶-7-甲酰胺是HIV整合酶和HIV复制抑制剂的抑制剂。 萘啶甲酰胺具有式（I）：其中R 1，R 2，R 3和R 3'在本文中定义。 这些化合物可用于预防和治疗艾滋病毒感染以及预防，延迟艾滋病的发病和治疗。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。 描述了预防，治疗或延缓AIDS发病的方法以及预防或治疗HIV感染的方法。

公开(公告)号：US20050176718A1

公开(公告)日：2005-08-11

申请号：US11056412

申请日：2005-02-11

Applicant: Neville Anthony ,  Robert Gomez ,  Steven Young ,  Melissa Egbertson ,  John Wai ,  Linghang Zhuang ,  Mark Embrey ,  Lekhanh Tran ,  Jeffrey Melamed ,  H. Langford ,  James Guare ,  Thorsten Fisher ,  Samson Jolly ,  Michelle Kuo ,  Debra Perlow ,  Jennifer Bennett ,  Timothy Funk

Inventor： Neville Anthony ,  Robert Gomez ,  Steven Young ,  Melissa Egbertson ,  John Wai ,  Linghang Zhuang ,  Mark Embrey ,  Lekhanh Tran ,  Jeffrey Melamed ,  H. Langford ,  James Guare ,  Thorsten Fisher ,  Samson Jolly ,  Michelle Kuo ,  Debra Perlow ,  Jennifer Bennett ,  Timothy Funk

IPC: A61K31/4375 ,  A61K31/47 ,  A61K31/4985 ,  A61K31/541 ,  A61K31/554 ,  A61P31/12 ,  A61P31/18 ,  C07D20060101 ,  C07D215/48 ,  C07D221/00 ,  C07D241/00 ,  C07D471/00 ,  C07D471/04 ,  C07D471/16 ,  C07D487/00 ,  C07D519/00 ,  A61K31/498 ,  A61K31/4745 ,  C07D471/02 ,  C07D487/02

CPC classification number: C07D471/04

Abstract: Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

公开(公告)号：US06921759B2

公开(公告)日：2005-07-26

申请号：US09973853

申请日：2001-10-10

Applicant: Neville J. Anthony ,  Robert P. Gomez ,  Steven D. Young ,  Melissa Egbertson ,  John S. Wai ,  Linghang Zhuang ,  Mark Embrey ,  Jeffrey Y. Melamed ,  H. Marie Langford ,  James P. Guare ,  Thorsten E. Fisher ,  Samson M. Jolly ,  Michelle S. Kuo ,  Debra S. Perlow ,  Jennifer J. Bennett ,  Timothy W. Funk

Inventor： Neville J. Anthony ,  Robert P. Gomez ,  Steven D. Young ,  Melissa Egbertson ,  John S. Wai ,  Linghang Zhuang ,  Mark Embrey ,  Jeffrey Y. Melamed ,  H. Marie Langford ,  James P. Guare ,  Thorsten E. Fisher ,  Samson M. Jolly ,  Michelle S. Kuo ,  Debra S. Perlow ,  Jennifer J. Bennett ,  Timothy W. Funk

IPC: A61K31/4375 ,  A61K31/47 ,  A61K31/4985 ,  A61K31/541 ,  A61K31/554 ,  A61P31/12 ,  A61P31/18 ,  C07D20060101 ,  C07D215/48 ,  C07D221/00 ,  C07D241/00 ,  C07D471/00 ,  C07D471/04 ,  C07D471/16 ,  C07D487/00 ,  C07D519/00 ,  A61P31/00 ,  C07D471/02

CPC classification number: C07D471/04

Abstract: Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

Abstract translation: 描述了包括某些喹啉羧酰胺和萘啶甲酰胺衍生物的氮杂和多氮萘基甲酰胺衍生物。 这些化合物是HIV整合酶和HIV复制抑制剂的抑制剂，并且可用于预防或治疗HIV感染和治疗AIDS，作为化合物或药学上可接受的盐，或作为药物组合物中的成分，任选地与其它组合 抗病毒药，免疫调节剂，抗生素或疫苗。 还描述了预防，治疗或延缓AIDS发病的方法以及预防或治疗HIV感染的方法。

公开(公告)号：US20080009490A1

公开(公告)日：2008-01-10

申请号：US10592222

申请日：2005-03-04

Applicant: Peter Williams ,  John Wai ,  Mark Embrey ,  Donnette Staas ,  Linghang Zhuang ,  H. Langford

Inventor： Peter Williams ,  John Wai ,  Mark Embrey ,  Donnette Staas ,  Linghang Zhuang ,  H. Langford

IPC: A61K31/5377 ,  A61K31/522 ,  A61P31/18 ,  C07D413/08 ,  C07D471/04

CPC classification number: C07D487/04 ,  A61K31/495 ,  A61K31/50 ,  A61K31/535 ,  A61K31/54 ,  A61K45/06 ,  A61K2300/00

Abstract: Bicyclic uracils and related compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the compounds are of Formula I: wherein a, b, Y, R1, R2, R3 and R4 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Abstract translation: 双环尿嘧啶和相关化合物是HIV整合酶和HIV复制抑制剂的抑制剂。 在一个实施方案中，化合物具有式I：其中a，b，Y，R 1，R 2，R 3和R 3， SUP> 4 在本文中定义。 这些化合物可用于预防和治疗艾滋病毒感染以及预防，延迟艾滋病的发病和治疗。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

公开(公告)号：US20070093496A1

公开(公告)日：2007-04-26

申请号：US10576328

申请日：2004-10-18

Applicant: John Wai ,  Thorsten Fisher ,  Linghang Zhuang ,  Donnette Staas ,  Terry Lyle ,  Boyoung Kim ,  Mark Embrey ,  Catherine Wiscount ,  Lekhanh Tran ,  Melissa Egbertson ,  Kelly Savage

Inventor： John Wai ,  Thorsten Fisher ,  Linghang Zhuang ,  Donnette Staas ,  Terry Lyle ,  Boyoung Kim ,  Mark Embrey ,  Catherine Wiscount ,  Lekhanh Tran ,  Melissa Egbertson ,  Kelly Savage

IPC: A61K31/498 ,  C07D487/14

CPC classification number: C07D471/14

Abstract: Hydroxy-substituted pyridopyrrolopyrazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I): (I) wherein a, b, A, B, R1, R2, R3, R4, R5, R6, R7 and R8 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Abstract translation: 羟基取代的吡啶并吡咯并吡嗪二酮化合物是HIV整合酶和HIV复制抑制剂的抑制剂。 在一个实施方案中，二酮化合物具有式（I）：（I）其中a，b，A，B，R 1，R 2， R 4，R 4，R 5，R 6，R 7和R 9， 这里定义了8。 这些化合物可用于预防和治疗艾滋病毒感染以及预防，延迟艾滋病的发病和治疗。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

公开(公告)号：US20050010048A1

公开(公告)日：2005-01-13

申请号：US10398929

申请日：2001-10-09

Applicant: Linghang Zhuang ,  John Wai ,  Linda Payne ,  Steven Young ,  Thorsten Fisher ,  Mark Embrey ,  James Guare

Inventor： Linghang Zhuang ,  John Wai ,  Linda Payne ,  Steven Young ,  Thorsten Fisher ,  Mark Embrey ,  James Guare

IPC: C07D215/26 ,  A61K31/4375 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/513 ,  A61K31/5377 ,  A61P31/18 ,  A61P43/00 ,  C07D215/04 ,  C07D401/06 ,  C07D401/10 ,  C07D471/04 ,  C07D521/00 ,  C07D471/02 ,  C07D487/02

CPC classification number: C07D215/04 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D471/04

Abstract: Certain aza- and polyaza-naphthalenyl ketones including certain quinolinyl and naphthyridinyl ketones are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment or the delay in the onset of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

Abstract translation: 包括某些喹啉基和萘啶基酮的某些氮杂和多氮萘基酮被描述为HIV整合酶的抑制剂和HIV复制抑制剂。 这些化合物可用于预防或治疗艾滋病毒感染以及作为化合物或药学上可接受的盐或作为药物组合物中的成分治疗或延迟发作的AIDS，任选地与其它抗病毒剂，免疫调节剂，抗生素或其它抗生素组合 疫苗。 还描述了治疗或延缓AIDS发病的方法以及预防或治疗HIV感染的方法。

公开(公告)号：US20080287394A1

公开(公告)日：2008-11-20

申请号：US11579772

申请日：2005-05-03

Applicant: John S. Wai ,  Joseph P. Vacca ,  Linghang Zhuang ,  Boyoung Kim ,  Terry A. Lyle ,  Catherine M. Wiscount ,  Melissa S. Egbertson ,  Lou Anne Neilson ,  Mark Embrey ,  Thorsten E. Fisher ,  Donnette D. Staas

Inventor： John S. Wai ,  Joseph P. Vacca ,  Linghang Zhuang ,  Boyoung Kim ,  Terry A. Lyle ,  Catherine M. Wiscount ,  Melissa S. Egbertson ,  Lou Anne Neilson ,  Mark Embrey ,  Thorsten E. Fisher ,  Donnette D. Staas

IPC: A61K31/69 ,  C07D487/14 ,  C07F5/02 ,  A61K31/541 ,  A61P31/18 ,  C07D417/14 ,  A61K31/5025

CPC classification number: A61K31/5025 ,  C07D487/14 ,  Y02A50/414

Abstract: Hydroxy-substituted pyrazinopyrrolopyridazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I) wherein R1, R2, R3, R4, R5, R6 and R7 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Abstract translation: 羟基取代的吡嗪并吡咯并哒嗪二酮化合物是HIV整合酶和HIV复制抑制剂的抑制剂。 在一个实施方案中，二酮化合物具有式（I），其中R 1，R 2，R 3，R 4， / SUP，R 5，R 6和R 7在本文中定义。 这些化合物可用于预防和治疗艾滋病毒感染以及预防，延迟艾滋病的发病和治疗。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。