公开(公告)号：US20240131028A1

公开(公告)日：2024-04-25

申请号：US18263551

申请日：2022-02-02

申请人： Justin A. BODDEY ,  David B. OLSEN ,  Ryan STEEL ,  John A. MCCAULEY ,  Manuel DE LERA RUIZ ,  Merck Sharp & Dohme LLC ,  The Walter and Eliza Hall Institute of Medical Research

发明人： Justin A. Boddey ,  David B. Olsen ,  Ryan Steel ,  John A. McCauley ,  Manuel De Lera Ruiz

IPC分类号： A61K31/513 ,  A61K39/015 ,  A61K45/06 ,  A61P33/06

CPC分类号： A61K31/513 ,  A61K39/015 ,  A61K45/06 ,  A61P33/06 ,  A61K2039/522

摘要： The present invention relates to a method of chemovaccination against Plasmodium infection comprising administering to a patient an effective amount of a selective inhibitor of plasmepsin X, or a pharmaceutically acceptable salt thereof.

公开(公告)号：US09233977B2

公开(公告)日：2016-01-12

申请号：US13880992

申请日：2011-10-25

申请人： John A. McCauley ,  Hemaka A. Rajapakse ,  Thomas J. Greshock ,  John Sanders ,  Boyoung Kim ,  Vanessa L. Rada ,  Jonathan T. Kern ,  Heather H. Stevenson ,  Mark T. Bilodeau

发明人： John A. McCauley ,  Hemaka A. Rajapakse ,  Thomas J. Greshock ,  John Sanders ,  Boyoung Kim ,  Vanessa L. Rada ,  Jonathan T. Kern ,  Heather H. Stevenson ,  Mark T. Bilodeau

IPC分类号： C07D495/04 ,  C07D495/10 ,  A61K31/438 ,  A61K31/4365

CPC分类号： C07D495/04 ,  C07D495/10

摘要： Disclosed are compounds of Formula (I): and the pharmaceutically acceptable salts thereof, wherein “A” is S—; —SO—, —SO2—, —O— or NRac—, wherein Rac is H, or C1-20 alkyl and R1 through R5 are defined herein. Also disclosed are pharmaceutical formulations comprising a compound of Formula I and methods of treating, managing, or ameliorating diseases amenable to treatment, management, or amelioration by inhibition of LRRK2 kinase activity, for example, Parkinson's disease.

摘要翻译： 公开了式（I）的化合物及其药学上可接受的盐，其中“A”为S-; -SO - ， - SO 2 - ， - O-或NRac-，其中Rac是H，或C 1-20烷基和R 1至R 5在本文中定义。 还公开了包含式I化合物的药物制剂以及通过抑制LRRK2激酶活性（例如帕金森病）治疗，治疗或改善易于治疗，治疗或改善的疾病的方法。

公开(公告)号：US20130178413A1

公开(公告)日：2013-07-11

申请号：US13825245

申请日：2011-09-16

申请人： John A. McCauley ,  Nigel J. Liverton ,  Michael T. Rudd ,  Kevin F. Gilbert ,  Marco Ferrara ,  Vincenzo Summa ,  Benedetta Crescenzi

发明人： John A. McCauley ,  Nigel J. Liverton ,  Michael T. Rudd ,  Kevin F. Gilbert ,  Marco Ferrara ,  Vincenzo Summa ,  Benedetta Crescenzi

IPC分类号： A61K38/07 ,  C07K5/103 ,  A61K45/06 ,  C07K5/107

CPC分类号： A61K38/07 ,  A61K45/06 ,  C07D498/18 ,  C07K5/101 ,  C07K5/1016

摘要： The present invention relates to macrocyclic compounds of formula I that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

摘要翻译： 本发明涉及可用作丙型肝炎病毒（HCV）NS3蛋白酶抑制剂及其合成及其用于治疗或预防HCV感染的用途的式I的大环化合物。

公开(公告)号：US20110318266A1

公开(公告)日：2011-12-29

申请号：US12737943

申请日：2009-08-24

申请人： John A. McCauley

发明人： John A. McCauley

IPC分类号： A61K51/00 ,  C07D417/12 ,  G01N33/567 ,  C07F7/02 ,  C07D401/12 ,  A61K49/00

CPC分类号： C07D401/14 ,  C07D401/12 ,  C07D417/12 ,  C07D471/04

摘要： Disclosed are mGluR4 positive allosteric modulator ligands of general formula (I) and radiolabeled derivates, their use as therapeutic agents for the treatment of central nervous system disorders modulated by mGluR4 and as ligands for the labeling and diagnostic imaging of mGluR4 in mammals.

摘要翻译： 公开了通式（I）的mGluR4正变构调节剂配体和放射性标记的衍生物，其用作治疗由mGluR4调节的中枢神经系统疾病的治疗剂，以及作为哺乳动物中mGluR4的标记和诊断成像的配体。

公开(公告)号：US07217716B2

公开(公告)日：2007-05-15

申请号：US10470561

申请日：2002-02-20

申请人： Christopher F. Claiborne ,  David A. Claremon ,  Brian E. Libby ,  John W. Butcher ,  John A. McCauley ,  Nigel J. Liverton ,  Peter M. Munson ,  Kevin T. Nguyen ,  Brian Phillips ,  Wayne Thompson

发明人： Christopher F. Claiborne ,  David A. Claremon ,  Brian E. Libby ,  John W. Butcher ,  John A. McCauley ,  Nigel J. Liverton ,  Peter M. Munson ,  Kevin T. Nguyen ,  Brian Phillips ,  Wayne Thompson

IPC分类号： C07D401/12 ,  A61K31/444

CPC分类号： C07D409/14 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D451/02 ,  C07D471/04 ,  C07D473/16 ,  C07D473/34 ,  C07D475/08

摘要： Compounds represented by Formula (I): (I) or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain

摘要翻译： 由式（I）表示的化合物：（I）或其药学上可接受的盐作为可用于缓解疼痛的NMDA NR2B拮抗剂是有效的

公开(公告)号：US06291499B1

公开(公告)日：2001-09-18

申请号：US09696612

申请日：2000-10-25

申请人： Wayne Thompson ,  David A. Claremon ,  Peter M. Munson ,  John A. McCauley

发明人： Wayne Thompson ,  David A. Claremon ,  Peter M. Munson ,  John A. McCauley

IPC分类号： A61K314184

CPC分类号： C07D403/12 ,  C07D235/08 ,  C07D235/10 ,  C07D235/12 ,  C07D235/14 ,  C07D235/16 ,  C07D235/30 ,  C07D405/12 ,  C07D417/12

摘要： Novel 4-substituted cyclohexanes substituted in the 1-position with 2-benzimidazoles, 2-imidazopyridines, or 4-imidazoles either directly or through a C1-C4alkyl, cycloalkyl, hydroxyalkyl, alkoxy or aminoalkyl chain are effective as NMDA NR2B antagonists useful for relieving pain.

摘要翻译： 通过直接或通过C 1 -C 4烷基，环烷基，羟基烷基，烷氧基或氨基烷基链在1-位上与2-苯并咪唑，2-咪唑并吡啶或4-咪唑取代的新的4-取代的环己烷作为可用于缓解的NMDA NR2B拮抗剂是有效的 疼痛。

公开(公告)号：US5621108A

公开(公告)日：1997-04-15

申请号：US349413

申请日：1994-12-05

申请人： Amos B. Smith, III ,  Stephen M. Condon ,  Johnnie L. Leazer, Jr. ,  Robert E. Maleczka ,  John A. McCauley ,  James W. Leahy

发明人： Amos B. Smith, III ,  Stephen M. Condon ,  Johnnie L. Leazer, Jr. ,  Robert E. Maleczka ,  John A. McCauley ,  James W. Leahy

IPC分类号： C07C35/17 ,  C07C49/11 ,  C07C49/175 ,  C07D303/14 ,  C07D405/06 ,  C07F7/18

CPC分类号： C07D405/06 ,  C07C35/17 ,  C07C403/16 ,  C07C49/175 ,  C07D303/14 ,  C07F7/1856 ,  C07C2101/14

摘要： Novel processes for the preparation of lactam- and lactone-containing macrocyles are provided. In preferred embodiments, rapamycin and demethoxyrapamycin are prepared by a convergent synthesis regime. Intermediates useful in the synthetic processes are also provided.

摘要翻译： 提供了用于制备含内酰胺和内酯的大环的新方法。 在优选的实施方案中，雷帕霉素和去甲氧西拉霉素通过收敛合成方案制备。 还提供了在合成方法中有用的中间体。

公开(公告)号：US20230139282A1

公开(公告)日：2023-05-04

申请号：US17795349

申请日：2021-02-02

申请人： Manuel DE LERA RUIZ ,  Paola FAVUZZA ,  Zhuyan GUO ,  Bin HU ,  Michael J. KELLY, III ,  Zhiyu LEI ,  John A. MCCAULEY ,  David B. OLSEN ,  Brad SLEEBS ,  Tony TRIGLIA ,  Dongmei ZHAN ,  Lianyun ZHAO ,  Merck Sharp & Dohme LLC ,  The Walter and Eliza Hall Institute of Medical Research ,  MSD R&D (China) Co., Ltd.

发明人： Manuel de Lera Ruiz ,  Paola Favuzza ,  Zhuyan Guo ,  Bin Hu ,  Michael J. Kelly, III ,  Zhiyu Lei ,  John A. McCauley ,  David B. Olsen ,  Brad Sleebs ,  Tony Triglia ,  Dongmei Zhan ,  Lianyun Zhao

IPC分类号： A61K31/513 ,  A61K45/06 ,  C07D405/12 ,  C07D233/88 ,  C07D405/14 ,  C07D417/14 ,  C07D491/18 ,  A61P33/06 ,  A61K31/529 ,  A61K31/5377 ,  C07D401/06

摘要： Provided are methods of treating malaria comprising administration of compounds of Formula (I) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables are as defined herein. Also provided are uses of the compounds of Formula (I), as defined herein, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.

公开(公告)号：US20210309671A1

公开(公告)日：2021-10-07

申请号：US17057875

申请日：2019-05-31

申请人： Tao Yu ,  Alan Whitehead ,  Yili Chen ,  Chunrui Sun ,  Zhiy-ong Hu ,  Kake Zhao ,  Ronald M. Kim ,  John A. McCauley ,  MERCK SHARP & DOHME CORP.

发明人： Tao YU ,  Alan WHITEHEAD ,  Yili CHEN ,  Chunrui SUN ,  Zhiyong HU ,  Kake ZHAO ,  Ronald M. KIM ,  John A. McCAULEY

IPC分类号： C07D498/22 ,  C07D471/16 ,  C07D491/22 ,  A61K45/06 ,  A61P31/18

摘要： The present invention relates to Tricyclic Heterocycle Compounds of Formula (I): (I) and pharmaceutically acceptable salts or prodrug thereof, where-in R1, R2, R3, R4, R5, R6 and n are as defined herein. The present invention also relates to compositions comprising at least one Tricyclic Heterocycle Compound, and methods of using the Tricyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.

公开(公告)号：US20170217986A1

公开(公告)日：2017-08-03

申请号：US15123111

申请日：2015-03-02

申请人： John A. MCCAULEY ,  David Johathan BENNETT ,  Christopher J. BUNGARD ,  Thomas J. GRESHOCK ,  M. Katharine HOLLOWAY ,  Peter D. WILLIAMS ,  Christian BEAULIEU ,  Sheldon CRANE ,  Stephanie LESSARD ,  Daniel MCKAY ,  Carmela MOLINARO ,  Oscar Miguel MORADEI ,  Vijayasaradhi SIVALENKA ,  Vouy Linh TRUONG ,  Satyanarayana TUMMANAPALLI ,  Merck Canada Inc.

发明人： John A. McCauley ,  David Jonathan Bennett ,  Christopher J. Bungard ,  Thomas J. Greshock ,  M. Katharine Holloway ,  Peter D. Williams ,  Christian Beaulieu ,  Sheldon Crane ,  Stephanie Lessard ,  Daniel Mckay ,  Carmela Molinaro ,  Oscar Miguel Moradei ,  Vijayasaradhi Sivalenka ,  Vouy Linh Truong ,  Satyanarayana Tummanapalli

IPC分类号： C07D498/10 ,  A61K31/5375 ,  C07D413/12 ,  A61K31/5377 ,  C07D417/14 ,  A61K45/06 ,  C07D487/04 ,  C07D471/04 ,  C07D413/06 ,  C07D265/36 ,  A61K31/5386 ,  C07D265/30 ,  C07D413/14

CPC分类号： C07D498/10 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/5386 ,  A61K45/06 ,  C07D265/30 ,  C07D265/36 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

摘要： The present invention is directed to 2,6-morpholine derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein Z1, Z2, V1, V2, V3, R6, R6A, and X are defined herein. The invention also relates to methods of using the 2,6-morpholine derivatives of the invention for the inhibition of HV protease, the inhibition of HV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.