公开(公告)号：US09593108B2

公开(公告)日：2017-03-14

申请号：US13259283

申请日：2010-04-05

Applicant: Malcolm Maccoss ,  F. George Njoroge ,  Amin Nomeir ,  Guangming Chen ,  Gary Mitchell Karp ,  William Jospeh Lennox ,  Chunshi Li ,  Christie Morrill ,  Steven D. Paget ,  Hongyu Ren ,  Nanjing Zhang ,  Xiaoyan Zhang

Inventor： Malcolm Maccoss ,  F. George Njoroge ,  Amin Nomeir ,  Guangming Chen ,  Gary Mitchell Karp ,  William Jospeh Lennox ,  Chunshi Li ,  Christie Morrill ,  Steven D. Paget ,  Hongyu Ren ,  Nanjing Zhang ,  Xiaoyan Zhang

IPC: C07D487/04 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  A61K31/437 ,  A61K31/506 ,  A61P31/14 ,  C07D471/04

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/506 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D487/04

Abstract: The present invention is directed to compounds and forms and pharmaceutical compositions thereof useful for treating a viral infection, or for affecting viral activity by modulating viral replication.

Abstract translation: 本发明涉及用于治疗病毒感染或通过调节病毒复制影响病毒活性的化合物及其形式和药物组合物。

公开(公告)号：US08859776B2

公开(公告)日：2014-10-14

申请号：US13501685

申请日：2010-10-05

Applicant: Stephane L. Bogen ,  Yao Ma ,  Yaolin Wang ,  Brian Robert Lahue ,  Latha G. Nair ,  Manami Shizuka ,  Matthew Ernst Voss ,  Margarita Kirova-Snover ,  Weidong Pan ,  Yuan Tian ,  Bheemashankar A. Kulkarni ,  Craig R. Gibeau ,  Yuan Liu ,  Giovanna Scapin ,  Diane Rindgen ,  Ronald J. Doll ,  Timothy J. Guzi ,  Danny J. Hicklin ,  Amin Nomeir ,  Gerald W. Shipps, Jr. ,  Malcolm MacCoss

Inventor： Stephane L. Bogen ,  Yao Ma ,  Yaolin Wang ,  Brian Robert Lahue ,  Latha G. Nair ,  Manami Shizuka ,  Matthew Ernst Voss ,  Margarita Kirova-Snover ,  Weidong Pan ,  Yuan Tian ,  Bheemashankar A. Kulkarni ,  Craig R. Gibeau ,  Yuan Liu ,  Giovanna Scapin ,  Diane Rindgen ,  Ronald J. Doll ,  Timothy J. Guzi ,  Danny J. Hicklin ,  Amin Nomeir ,  Gerald W. Shipps, Jr. ,  Malcolm MacCoss

IPC: C07D401/00 ,  A01N43/40 ,  C07D401/14 ,  C07D409/14

CPC classification number: C07D401/14 ,  C07D409/14

Abstract: The present invention provides a compound of Formula 1 as described herein or a pharmaceutically acceptable salt, solvate or ester thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.

Abstract translation: 本发明提供本文所述的式1的化合物或其药学上可接受的盐，溶剂合物或酯。 该化合物可用作HDM2蛋白的抑制剂。 还公开了包含上述化合物的药物组合物和使用其治疗癌症的方法。

公开(公告)号：US20140242027A1

公开(公告)日：2014-08-28

申请号：US13579399

申请日：2011-02-18

Applicant: Ashok Arasappan ,  F. George Njoroge ,  Cecil D. Kwong ,  Subramaniam Ananthan ,  Frank Bennett ,  Francisco Velazquez ,  Vinay Girijavallabhan ,  Yuhua Huang ,  Hollis S. Kezer ,  Joseph Maddry ,  Robert C. REynold ,  Abhijit Roychowdhury ,  Anita T. Fowler ,  John A. Secrist, III ,  Ling Tong ,  Seong Heon Kim ,  Malcolm MacCoss ,  Srikanth Venkatraman ,  vishal Verma

Inventor： Ashok Arasappan ,  F. George Njoroge ,  Cecil D. Kwong ,  Subramaniam Ananthan ,  Frank Bennett ,  Francisco Velazquez ,  Vinay Girijavallabhan ,  Yuhua Huang ,  Hollis S. Kezer ,  Joseph Maddry ,  Robert C. REynold ,  Abhijit Roychowdhury ,  Anita T. Fowler ,  John A. Secrist, III ,  Ling Tong ,  Seong Heon Kim ,  Malcolm MacCoss ,  Srikanth Venkatraman ,  vishal Verma

IPC: C07D513/04 ,  C07D417/04 ,  A61K45/06 ,  C07D417/14 ,  C07D491/048 ,  A61K31/506

CPC classification number: A61K31/506 ,  A61K45/06 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07D491/048 ,  C07D513/04

Abstract: The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.

Abstract translation: 本发明提供式（I）的化合物：所述化合物的互变异构体，异构体和酯，以及所述化合物的药学上可接受的盐，溶剂合物和前药，其中R，R 1，X，Y，Z，R 2， R3，R4，R5，R6，R7，R8，R9，R18，R19和n独立选择和如本文所定义。 还提供了包含这些化合物的组合物。 本发明的化合物作为HCV的抑制剂是有效的，并且单独和与其它治疗剂一起用于治疗或预防疾病或病症如病毒感染和病毒相关疾病。

公开(公告)号：US20120208844A1

公开(公告)日：2012-08-16

申请号：US13501685

申请日：2010-10-05

Applicant: Stephane L. Bogen ,  Yao Ma ,  Yaolin Wang ,  Brian Robert Lahue ,  Latha G. Nair ,  Manami Shizuka ,  Matthew Ernst Voss ,  Margarita Kirova-Snover ,  Weidong Pan ,  Yuan Tian ,  Bheemashankar A. Kulkarni ,  Craig R. Gibeau ,  Yuan Liu ,  Giovanna Scapin ,  Diane Rindgen ,  Ronald J. Doll ,  Timothy J. Guzi ,  Danny J. Hicklin ,  Amin Nomeir ,  Cynthia Seidel-Dugan ,  Gerald W. Shipps, JR. ,  Malcolm MacCoss

Inventor： Stephane L. Bogen ,  Yao Ma ,  Yaolin Wang ,  Brian Robert Lahue ,  Latha G. Nair ,  Manami Shizuka ,  Matthew Ernst Voss ,  Margarita Kirova-Snover ,  Weidong Pan ,  Yuan Tian ,  Bheemashankar A. Kulkarni ,  Craig R. Gibeau ,  Yuan Liu ,  Giovanna Scapin ,  Diane Rindgen ,  Ronald J. Doll ,  Timothy J. Guzi ,  Danny J. Hicklin ,  Amin Nomeir ,  Cynthia Seidel-Dugan ,  Gerald W. Shipps, JR. ,  Malcolm MacCoss

IPC: A61K31/4545 ,  A61P35/02 ,  A61P35/00 ,  C07D409/14 ,  C07D401/14

CPC classification number: C07D401/14 ,  C07D409/14

Abstract: The present invention provides a compound of Formula (1) as described herein or a pharmaceutically acceptable salt, solvate or ester thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.

Abstract translation: 本发明提供本文所述的式（1）化合物或其药学上可接受的盐，溶剂合物或酯。 该化合物可用作HDM2蛋白的抑制剂。 还公开了包含上述化合物的药物组合物和使用其治疗癌症的方法。

公开(公告)号：US20110306593A1

公开(公告)日：2011-12-15

申请号：US13128316

申请日：2009-11-11

Applicant: Zhaoning Zhu ,  William J. Greenlee ,  Hongmei Li ,  Monica L. Vicarel ,  Jun Qin ,  Pawan Kumar Dhondi ,  Xianhai Huang ,  Anandan Palani ,  Xiaoxiang Liu ,  Zhong-Yue Sun ,  Hubert B. Josien ,  Ruo Xu ,  David James Cole ,  Duane A. Burnett ,  Chad E. Bennett ,  Troy McCracken ,  Malcolm MacCoss

Inventor： Zhaoning Zhu ,  William J. Greenlee ,  Hongmei Li ,  Monica L. Vicarel ,  Jun Qin ,  Pawan Kumar Dhondi ,  Xianhai Huang ,  Anandan Palani ,  Xiaoxiang Liu ,  Zhong-Yue Sun ,  Hubert B. Josien ,  Ruo Xu ,  David James Cole ,  Duane A. Burnett ,  Chad E. Bennett ,  Troy McCracken ,  Malcolm MacCoss

IPC: A61K31/553 ,  C07D498/10 ,  C07D498/04 ,  A61P25/28 ,  C07D413/14 ,  C07D498/14 ,  A61K31/5395 ,  C07D498/20 ,  C07D413/10

CPC classification number: C07D498/04 ,  C07D409/14 ,  C07D413/10 ,  C07D498/14 ,  C07D498/20

Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more disease associated with the central nervous system using such compounds or pharmaceutical compostions.

Abstract translation: 在其许多实施方案中，本发明提供了一类新颖的下式杂环化合物：作为γ-分泌酶的调节剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备包含一种或多种这样的化合物的药物制剂的方法 化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与中枢神经系统相关的一种或多种疾病的方法。

公开(公告)号：US07632821B2

公开(公告)日：2009-12-15

申请号：US11990051

申请日：2006-08-04

Applicant: Gabor Butora ,  Kenneth Alan Koeplinger ,  Malcolm MacCoss ,  Daniel R. McMasters ,  David B. Olsen ,  Lihu Yang

Inventor： Gabor Butora ,  Kenneth Alan Koeplinger ,  Malcolm MacCoss ,  Daniel R. McMasters ,  David B. Olsen ,  Lihu Yang

IPC: A01N43/04 ,  A61K31/70

CPC classification number: C07H19/06 ,  C07H19/16

Abstract: The present invention provides ribonucleoside 2′,3′-cyclic acetals of structural formula I which are precursors or prodrugs of inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors of inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors or prodrugs of inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors or prodrugs of inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such ribonucleoside 2′,3′-cyclic acetals alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the ribonucleoside 2′,3′-cyclic acetals of the present invention.

Abstract translation: 本发明提供结构式I的核糖核苷2'，3'-环状缩醛，其为RNA依赖性RNA病毒聚合酶抑制剂的前体或前药。 这些化合物是RNA依赖性RNA病毒复制的抑制剂的前体，可用于治疗RNA依赖性RNA病毒感染。 它们特别可用作丙型肝炎病毒（HCV）NS5B聚合酶抑制剂的前体或前药，作为HCV复制抑制剂的前体或前药，和/或用于治疗丙型肝炎感染。 本发明还描述了含有这种核糖核苷2'，3'-环状缩醛单独或与其它对RNA依赖性RNA病毒感染，特别是HCV感染有活性的试剂组合的药物组合物。 还公开了本发明的核糖核苷2'，3'-环状缩醛的抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。

公开(公告)号：US20090099126A1

公开(公告)日：2009-04-16

申请号：US11990051

申请日：2006-08-04

Applicant: Gabor Butora ,  Kenneth Alan Koeplinger ,  Malcolm MacCoss ,  Daniel R. McMasters ,  David B. Olsen ,  Lihu Yang

Inventor： Gabor Butora ,  Kenneth Alan Koeplinger ,  Malcolm MacCoss ,  Daniel R. McMasters ,  David B. Olsen ,  Lihu Yang

IPC: A61K31/7076 ,  C07H19/16 ,  A61K31/7064 ,  A61P31/12 ,  C07H19/06

CPC classification number: C07H19/06 ,  C07H19/16

Abstract: The present invention provides ribonucleoside 2′,3′-cyclic acetals of structural formula I which are precursors or prodrugs of inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors of inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as pre-cursors or prodrugs of inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors or prodrugs of inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such ribonucleoside 2′,3′-cyclic acetals alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the ribonucleoside 2′,3′-cyclic acetals of the present invention.

Abstract translation: 本发明提供结构式I的核糖核苷2'，3'-环状缩醛，其为RNA依赖性RNA病毒聚合酶抑制剂的前体或前药。 这些化合物是RNA依赖性RNA病毒复制的抑制剂的前体，可用于治疗RNA依赖性RNA病毒感染。 它们特别可用作丙型肝炎病毒（HCV）NS5B聚合酶的抑制剂的前体或前药，作为HCV复制抑制剂的前体或前药，和/或用于治疗丙型肝炎感染。 本发明还描述了含有这种核糖核苷2'，3'-环状缩醛单独或与其它对RNA依赖性RNA病毒感染，特别是HCV感染有活性的试剂组合的药物组合物。 还公开了本发明的核糖核苷2'，3'-环状缩醛的抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。

公开(公告)号：US20080200376A1

公开(公告)日：2008-08-21

申请号：US11665127

申请日：2005-10-25

Applicant: Malcolm MacCoss ,  Duncan E. MacIntyre ,  Alison M. Strack

Inventor： Malcolm MacCoss ,  Duncan E. MacIntyre ,  Alison M. Strack

IPC: A61K38/22 ,  A61K31/155 ,  A61K31/485 ,  A61K31/357 ,  A61K31/42 ,  A61K31/473 ,  A61K31/519 ,  A61P3/00 ,  A61P35/00 ,  A61P9/00 ,  A61P15/00

CPC classification number: A61K31/519 ,  A61K45/06 ,  A61K2300/00

Abstract: The present invention relates to methods of treating and preventing obesity and obesity-related disorders in a subject comprising administering a neurokinin-1 antagonist and an anti-obesity agent, such as a melanocortin 4 receptor agonist, to said subject. The present invention further related to methods of treating or preventing sexual dysfunction, including male erectile dysfunction, in a subject comprising administering a neurokinin-1 antagonist and a sexual dysfunction therapeutic agent, such as a melanocortin 4 receptor agonist, to said subject. The present invention further provides for pharmaceutical compositions and medicaments useful in carrying out these methods.

Abstract translation: 本发明涉及治疗和预防受试者中肥胖和肥胖相关疾病的方法，包括向所述受试者施用神经激肽-1拮抗剂和抗肥胖剂如黑皮质素4受体激动剂。 本发明还涉及治疗或预防包括男性勃起功能障碍在内的性功能障碍的方法，所述方法包括向所述受试者施用神经激肽-1拮抗剂和性功能障碍治疗剂如黑皮质素4受体激动剂。 本发明进一步提供可用于实施这些方法的药物组合物和药物。

公开(公告)号：US07125887B2

公开(公告)日：2006-10-24

申请号：US10399084

申请日：2001-10-09

Applicant: Jeffrey J. Hale ,  Charles G. Caldwell ,  Dooseop Kim ,  Dong-Ming Shen ,  Sander G. Mills ,  Kevin T. Chapman ,  Liya Chen ,  Malcolm MacCoss ,  Amy Gentry ,  Christopher L. Lynch ,  Yuan Cheng, legal representative

Inventor： Christopher A. Willoughby, deceased

IPC: A61K31/44 ,  C07D221/02

CPC classification number: C07D401/14 ,  C07D405/14 ,  C07D471/04 ,  C07D495/04

Abstract: Pyrrolidine compounds of Formula (I), (wherein R1, R2, R3, R4, R5, R6a, R6b, R7 and R8 are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor activity. The compounds are useful, for example, 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 treating AIDS and methods of preventing or treating infection by HIV are also described

Abstract translation: 式（I）的吡咯烷化合物（其中R 1，R 2，R 3，R 3，R 4， R 5，R 6a，R 6b，R 7和R 8都是 描述于此。 这些化合物是CCR5趋化因子受体活性的调节剂。 所述化合物可用于例如预防或治疗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，任选地与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合。 还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法

公开(公告)号：US06699871B2

公开(公告)日：2004-03-02

申请号：US10189603

申请日：2002-07-05

Applicant: Scott D. Edmondson ,  Michael H. Fisher ,  Dooseop Kim ,  Malcolm Maccoss ,  Emma R. Parmee ,  Ann E. Weber ,  Jinyou Xu

Inventor： Scott D. Edmondson ,  Michael H. Fisher ,  Dooseop Kim ,  Malcolm Maccoss ,  Emma R. Parmee ,  Ann E. Weber ,  Jinyou Xu

IPC: C07D48704

CPC classification number: A61K31/4985 ,  A61K31/498 ,  A61K38/28 ,  A61K45/06 ,  C07D487/04 ,  Y10S514/866 ,  A61K2300/00

Abstract: The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

Abstract translation: 本发明涉及作为二肽基肽酶-IV酶（“DP-IV抑制剂”）抑制剂的化合物，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病 特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。