公开(公告)号：WO2010042867A3

公开(公告)日：2010-04-15

申请号：PCT/US2009/060237

申请日：2009-10-09

Applicant: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES ,  THOMAS, Craig J. ,  AULD, Douglas S. ,  INGLESE, James ,  SKOUMBOURDIS, Amanda P. ,  JIANG, Jian-Kang ,  BOXER, Matthew

Inventor： THOMAS, Craig J. ,  AULD, Douglas S. ,  INGLESE, James ,  SKOUMBOURDIS, Amanda P. ,  JIANG, Jian-Kang ,  BOXER, Matthew

IPC: C07D209/08 ,  C07D211/54 ,  C07D215/36 ,  C07D265/36 ,  C07D277/64 ,  C07D295/26 ,  C07D311/70 ,  C07D317/62 ,  C07D319/18 ,  C07D321/10 ,  C07D401/12 ,  C07D403/12 ,  C07D495/14 ,  A61K31/18 ,  A61P35/00

Abstract: Disclosed are pyruvate kinase M2 activators, which are bis sulfonamide piperazinyl and piperidinyl compounds of Formula (I), 2,4-disubstituted 4 H - thieno[3,2- c ]pyrrole-2-(substituted benzyl)pyridazin-3(2 H )-ones of Formula (II) and 6-(3,4-dimethylphenylaminosulfonyl)-3,4-dihydro-1 H -quinolin-2-one of formula (III), wherein L, R 1 , R 2 , R 11 to R 16 , R 21 and R 22 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia.

公开(公告)号：WO2018031730A3

公开(公告)日：2018-02-15

申请号：PCT/US2017/046228

申请日：2017-08-10

Applicant: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES ,  THE UNIVERSITY OF TOKYO ,  NEW ENGLAND BIOLABS, INC. ,  INGLESE, James ,  DRANCHAK, Patricia ,  MACARTHUR, Ryan ,  SUGA, Hiroaki ,  YU, Hao ,  CARLOW, Clotilde ,  LI, Zhiru

Inventor： INGLESE, James ,  DRANCHAK, Patricia ,  MACARTHUR, Ryan ,  SUGA, Hiroaki ,  YU, Hao ,  CARLOW, Clotilde ,  LI, Zhiru

IPC: C07K7/50

Abstract: Disclosed herein are isolated peptides inhibit activity of a cofactor-independent phosphoglycerate mutase. In some examples, the isolated peptide is 6-20 amino acids long and includes the amino acid sequence of any one of SEQ ID NOs: 1-22 or 54, an analog or derivative thereof, or a pharmaceutically acceptable salt or ester thereof. In some examples, the peptide is a cyclic peptide with an N-terminal ring of 6-15 amino acids (for example, 6-10 amino acids) and a C-terminal linear portion of 1-9 amino acids (for example, 3-8 amino acids. Also disclosed h are methods of treating or inhibiting an infection in a subject, including administering to the subject an effective amount of a composition including one of more of the disclosed peptides, or analogs or derivative thereof, or pharmaceutically acceptable salts or esters thereof.

公开(公告)号：WO2003072041A3

公开(公告)日：2003-09-04

申请号：PCT/US2003/005458

申请日：2003-02-23

Applicant: MERCK & CO., INC. ,  ESPESETH, Amy, S. ,  FERRER, Marc ,  FLORES, Osvaldo, A. ,  HAZUDA, Daria, J. ,  INGLESE, James ,  MILLER, Michael, D. ,  REGISTER, Bruce ,  SHI, Xiao-Ping ,  SIMON, Adam, J. ,  ZUCK, Paul, D.

Inventor： ESPESETH, Amy, S. ,  FERRER, Marc ,  FLORES, Osvaldo, A. ,  HAZUDA, Daria, J. ,  INGLESE, James ,  MILLER, Michael, D. ,  REGISTER, Bruce ,  SHI, Xiao-Ping ,  SIMON, Adam, J. ,  ZUCK, Paul, D.

IPC: C07H21/02 ,  C12P21/06 ,  C12N1/20 ,  C12N15/00

Abstract: The present invention provides DNA constructs, genetically engineered host cells, and methods for identifying inhibitors of amyloid precursor protein (APP) processing. The methods provide for the convenient identification, in a single assay, of inhibitors of β-secretase and γ-secretase as well as other forms of APP processing. The methods rely on fusion proteins of APP and transcription factors in which APP processing releases the transcription factors, allowing the transcription factors to activate transcription of a reporter gene. Inhibitors are identified as substances that block or diminish transcription factor release from the fusion protein, thereby causing a diminution of reporter gene readout.

公开(公告)号：WO2010047674A1

公开(公告)日：2010-04-29

申请号：PCT/US2008/011958

申请日：2008-10-20

Applicant: THE GOVERNMENT OF THE UNITED STATES OF AMERICA as represented by the SECRETARY OF THE DEPARTMENT OF HEALTH AND HUMAN SERVICES ,  GERSHENGORN, Marvin, C. ,  NEUMANN, Susanne ,  RAAKA, Bruce, M. ,  THOMAS, Craig, J. ,  INGLESE, James ,  SOUTHALL, Noel, T. ,  TITUS, Steven ,  ZHENG, Wei ,  HUANG, Wenwei ,  KRAUSE, Gerd ,  KLEINAU, Gunnar

Inventor： GERSHENGORN, Marvin, C. ,  NEUMANN, Susanne ,  RAAKA, Bruce, M. ,  THOMAS, Craig, J. ,  INGLESE, James ,  SOUTHALL, Noel, T. ,  TITUS, Steven ,  ZHENG, Wei ,  HUANG, Wenwei ,  KRAUSE, Gerd ,  KLEINAU, Gunnar

IPC: C07D235/18 ,  A61K31/4184

CPC classification number: C07D405/06 ,  A61K31/517 ,  A61K49/0004 ,  A61K51/00 ,  C07D239/91 ,  C07D401/06 ,  C07D405/14 ,  C07D487/04

Abstract: Disclosed are oxo-hydroquinazolines of formula I that are useful as selective TSHR agonists. The compounds may be used for detecting or treating thyroid cancer, or treating a bone degenerative disorder.

Abstract translation: 公开了可用作选择性TSHR激动剂的式I的氧代 - 氢喹唑啉。 该化合物可用于检测或治疗甲状腺癌或治疗骨退行性疾病。

公开(公告)号：WO2019090039A1

公开(公告)日：2019-05-09

申请号：PCT/US2018/058887

申请日：2018-11-02

Applicant: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES ,  HOON, Mark A. ,  SOLINSKI, Hans Juergen ,  INGLESE, James ,  DRANCHAK, Patricia

Inventor： HOON, Mark A. ,  SOLINSKI, Hans Juergen ,  INGLESE, James ,  DRANCHAK, Patricia

IPC: A61K31/422 ,  A61K31/4184 ,  A61K31/015 ,  A61K31/42 ,  A61K31/437 ,  A61K31/439 ,  A61K31/4545 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/519 ,  A61K31/55 ,  A61K31/5513 ,  A61K31/5517 ,  A61P17/04 ,  A61P43/00

CPC classification number: C07D471/04 ,  A61K31/015 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/422 ,  A61K31/437 ,  A61K31/439 ,  A61K31/4545 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/519 ,  A61K31/55 ,  A61K31/5513 ,  A61K31/5517 ,  A61P17/04 ,  A61P43/00 ,  C07D413/12 ,  C07D487/04

Abstract: Pharmaceutical compositions comprising a molecular inhibitor of Npr1 are disclosed. Also disclosed are methods of treating, reducing, or preventing acute and/or chronic pruritus in a mammal comprising administering a pharmaceutical composition comprising a molecular inhibitor of Npr1.

公开(公告)号：WO2018031730A2

公开(公告)日：2018-02-15

申请号：PCT/US2017/046228

申请日：2017-08-10

Applicant: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES ,  THE UNIVERSITY OF TOKYO ,  NEW ENGLAND BIOLABS, INC. ,  INGLESE, James ,  DRANCHAK, Patricia ,  MACARTHUR, Ryan ,  SUGA, Hiroaki ,  YU, Hao ,  CARLOW, Clotilde ,  LI, Zhiru

Inventor： INGLESE, James ,  DRANCHAK, Patricia ,  MACARTHUR, Ryan ,  SUGA, Hiroaki ,  YU, Hao ,  CARLOW, Clotilde ,  LI, Zhiru

IPC: C07K7/50

Abstract: Disclosed herein are isolated peptides inhibit activity of a cofactor-independent phosphoglycerate mutase. In some examples, the isolated peptide is 6-20 amino acids long and includes the amino acid sequence of any one of SEQ ID NOs: 1-22 or 54, an analog or derivative thereof, or a pharmaceutically acceptable salt or ester thereof. In some examples, the peptide is a cyclic peptide with an N-terminal ring of 6-15 amino acids (for example, 6-10 amino acids) and a C-terminal linear portion of 1-9 amino acids (for example, 3-8 amino acids. Also disclosed h are methods of treating or inhibiting an infection in a subject, including administering to the subject an effective amount of a composition including one of more of the disclosed peptides, or analogs or derivative thereof, or pharmaceutically acceptable salts or esters thereof.

Abstract translation: 本文公开的是分离的肽抑制辅因子非依赖性磷酸甘油酸变位酶的活性。 在一些实例中，分离的肽长6-20个氨基酸并且包括SEQ ID NO：1-22或54中任一个的氨基酸序列，其类似物或衍生物或其药学上可接受的盐或酯。 在一些实例中，肽是具有6-15个氨基酸（例如6-10个氨基酸）的N端环和1-9个氨基酸的C端线性部分的环状肽（例如3个 还公开了治疗或抑制受试者感染的方法，包括向受试者施用有效量的组合物，所述组合物包括一种或多种所公开的肽或其类似物或衍生物，或其药学上可接受的盐 或其酯。

公开(公告)号：WO2012112674A3

公开(公告)日：2012-08-23

申请号：PCT/US2012/025228

申请日：2012-02-15

Applicant: THE JOHNS HOPKINS UNIVERSITY ,  ZACK, Donald J. ,  BERLINICKE, Cynthia ,  HACKLER, Laszlo ,  YANG, Zhiyong ,  STEINER, Joseph P. ,  VOJKOVSKY, Tomas ,  FERRARIS, Dana ,  SLUSHER, Barbara S. ,  INGLESE, James

Inventor： ZACK, Donald J. ,  BERLINICKE, Cynthia ,  HACKLER, Laszlo ,  YANG, Zhiyong ,  STEINER, Joseph P. ,  VOJKOVSKY, Tomas ,  FERRARIS, Dana ,  SLUSHER, Barbara S. ,  INGLESE, James

IPC: C07D403/12 ,  C07D403/14 ,  A61K31/506 ,  A61P25/00

Abstract: Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.

公开(公告)号：WO2012112674A2

公开(公告)日：2012-08-23

申请号：PCT/US2012025228

申请日：2012-02-15

Applicant: UNIV JOHNS HOPKINS ,  ZACK DONALD J ,  BERLINICKE CYNTHIA ,  HACKLER LASZLO ,  YANG ZHIYONG ,  STEINER JOSEPH P ,  VOJKOVSKY TOMAS ,  FERRARIS DANA ,  SLUSHER BARBARA S ,  INGLESE JAMES

Inventor： ZACK DONALD J ,  BERLINICKE CYNTHIA ,  HACKLER LASZLO ,  YANG ZHIYONG ,  STEINER JOSEPH P ,  VOJKOVSKY TOMAS ,  FERRARIS DANA ,  SLUSHER BARBARA S ,  INGLESE JAMES

CPC classification number: C07D403/12 ,  C07D401/14 ,  C07D403/14 ,  C07D453/02

Abstract: Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.

Abstract translation: 公开了用于治疗与神经变性或眼部疾病相关的病症的化合物，组合物，试剂盒和方法。

公开(公告)号：WO2004062609A3

公开(公告)日：2004-11-25

申请号：PCT/US2004000584

申请日：2004-01-09

Applicant: PHARMACOPEIA INC ,  ERICKSON SHAWN DAVID ,  BALDWIN JOHN J ,  DOLLE RONALD E III ,  INGLESE JAMES ,  OHLMEYER MICHAEL H J ,  HO KOC-KAN ,  BOHNSTEDT ADOLPH C ,  KULTGEN STEVEN G ,  WEBB MARIA L ,  AULD DOUGLAS S ,  ROUGHTON ANDREW LAIRD ,  CONTI PAOLO GIOVANNI MARTINO C ,  LEYSEN DIRK ,  VAN DER LOUW JAAP ,  AKZO NOBEL NV

Inventor： ERICKSON SHAWN DAVID ,  BALDWIN JOHN J ,  DOLLE RONALD E III ,  INGLESE JAMES ,  OHLMEYER MICHAEL H J ,  HO KOC-KAN ,  BOHNSTEDT ADOLPH C ,  KULTGEN STEVEN G ,  WEBB MARIA L ,  AULD DOUGLAS S ,  ROUGHTON ANDREW LAIRD ,  CONTI PAOLO GIOVANNI MARTINO C ,  LEYSEN DIRK ,  VAN DER LOUW JAAP

IPC: A61P35/00 ,  C07D239/42 ,  C07D239/46 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D405/12 ,  C07D521/00 ,  A61K31/505 ,  A61K31/506 ,  C07D239/47 ,  C07D405/14

CPC classification number: C07D239/42 ,  C07D231/12 ,  C07D233/56 ,  C07D239/47 ,  C07D249/08 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D405/12

Abstract: Compounds containing the pyrimidine nucleus and their use to treat diseases and conditions related to inappropriate Interleukin-8 receptor activity are disclosed. The compounds are of the formula (I). In these compounds, Q is preferably unsubstituted and substituted heterocyclyl; U is usually hydrogen or fluorine; and V is preferably hydrogen, halogen, alkyl, -O-alkyl or -S-alkyl. A representative example is formula (X).

Abstract translation: 公开了含有嘧啶核的化合物及其用于治疗与不适当的白细胞介素-8受体活性有关的疾病和病症的用途。 该化合物具有式（I）。 在这些化合物中，Q优选为未取代的和取代的杂环基; U通常是氢或氟; 且V优选为氢，卤素，烷基，-O-烷基或-S-烷基。 一个代表性的例子是公式（X）。

公开(公告)号：WO2010042867A2

公开(公告)日：2010-04-15

申请号：PCT/US2009060237

申请日：2009-10-09

Applicant: US HEALTH ,  THOMAS CRAIG J ,  AULD DOUGLAS S ,  INGLESE JAMES ,  SKOUMBOURDIS AMANDA P ,  JIANG JIAN-KANG ,  BOXER MATTHEW

Inventor： THOMAS CRAIG J ,  AULD DOUGLAS S ,  INGLESE JAMES ,  SKOUMBOURDIS AMANDA P ,  JIANG JIAN-KANG ,  BOXER MATTHEW

IPC: C07D209/08 ,  A61K31/18 ,  A61P35/00 ,  C07D211/54 ,  C07D215/36 ,  C07D265/36 ,  C07D277/64 ,  C07D295/26 ,  C07D311/70 ,  C07D317/62 ,  C07D319/18 ,  C07D321/10 ,  C07D401/12 ,  C07D403/12 ,  C07D495/14

CPC classification number: A61K31/496 ,  A61K31/445 ,  A61K31/495 ,  A61K31/5025 ,  C07D295/26 ,  C07D319/18 ,  C07D495/14

Abstract: Disclosed are pyruvate kinase M2 activators, which are, bis sulfonamide piperazinyl compounds of Formula (I) and 2,4-disubstituted 4H-thieno[3,2-b]pyrrole-2-(substituted benzyl)pyridazin-3(2H)ones of Formula (II), wherein L and R1 to R16 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia, Formulas (I); (II).

Abstract translation: 公开了丙酮酸激酶M2活化剂，其为式（I）的双磺酰胺哌嗪基化合物和2,4-二取代的4H-噻吩并[3,2-b]吡咯-2-（取代的苄基）哒嗪-3（2H） 式（II）的化合物，其中L和R 1至R 16如本文所定义，其可用于治疗可通过PKM2的活化治疗的许多疾病，例如癌症和贫血，式（I）; （II）。