公开(公告)号：EP4174075A1

公开(公告)日：2023-05-03

申请号：EP21382981.5

申请日：2021-10-29

申请人： Consejo Superior de Investigaciones Científicas (CSIC) ,  Universidad de Sevilla ,  Academia Sinica

发明人： García Fernandez, José Manuel ,  Ortiz Mellet, Carmen ,  González Cuesta, Manuel ,  Sánchez Fernández, Elena Matilde ,  Chang, Ya-Jen ,  Lai, Alan Chuan-Ying

IPC分类号： C07D498/04 ,  A61K31/4355 ,  A61K31/7056 ,  C07H19/044 ,  A61P37/00 ,  A61P37/02 ,  A61P37/04 ,  A61P37/06 ,  A61P37/08 ,  A61P29/00 ,  A61P1/00 ,  A61P1/16 ,  A61P3/00 ,  A61P31/00 ,  A61P11/00 ,  A61P11/06

摘要： The invention relates to a 5-aminohexahydro-6,7,8-trihydroxy-3H-oxazolo[3,4-a]pyridin-3-one (i.e. 2,3,4-trihydroxy-5N,6O-oxomethylidene-nojirimycin-1-amine) glycolipid mimetic derivative of formula I

acting as antagonists or agonist of the TLR4 for the treatment and/or prevention of an immune disease such as e.g. acute inflammation, chronic disease allergy, cancer chemotherapy, infectious disease, the Metabolic Syndrome, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), immune mediated hepatitis, an autoimmune disease, graft rejection pathology, inflammatory bowel disease, atherosclerosis and airway hyperactivity, such as e.g. asthma and allergic rhinitis.
An exemplary compound is e.g. example 1, compound 1:

公开(公告)号：EP3502119A2

公开(公告)日：2019-06-26

申请号：EP18196575.7

申请日：2015-05-08

申请人： Immunexcite, Inc.

发明人： SIEDLECKI, James Michael ,  REZNIK, Gabriel Oscar ,  KANE, John James ,  MIAO, Hua ,  KLUGE, Arthur F. ,  RUBIN-BEJERANO, Ifat

IPC分类号： C07H3/06 ,  C07H5/04 ,  C07H13/04 ,  C07H15/04 ,  C07H15/18 ,  C07H15/203 ,  C07H15/26 ,  C07H19/044 ,  C07H19/048 ,  A61K31/716

摘要： This invention relates to modifications of β-1,6-D-glucans, e.g., structures according to Formula (I), and the ability of these compositions to modulate an immune response.

公开(公告)号：EP2825546B1

公开(公告)日：2017-07-12

申请号：EP12827811.6

申请日：2012-09-04

申请人： Case Western Reserve University

发明人： BERDIS, Anthony, J. ,  LEE, Irene ,  MOTEA, Edward

IPC分类号： C07H19/044 ,  C07H19/14 ,  C07H19/16 ,  G01N33/50 ,  A61K48/00 ,  C12Q1/68 ,  G01N33/574

CPC分类号： C12Q1/6876 ,  C07H19/044 ,  G01N33/57407 ,  G01N2800/52 ,  G01N2800/56

摘要： A theranostic agent for inhibiting translesion DNA replication comprises natural adenine ribose analog having formula I.

摘要翻译： 用于抑制转座病毒DNA复制的抑制剂包含具有式I的天然腺嘌呤核糖类似物。

公开(公告)号：EP2552930A2

公开(公告)日：2013-02-06

申请号：EP11714465.9

申请日：2011-03-31

申请人： Gilead Pharmasset LLC

发明人： ROSS, Bruce, S. ,  SOFIA, Michael, Joseph ,  PAMULAPATI, Ganapati, Reddy ,  RACHAKONDA, Suguna ,  ZHANG, Hai-Ren ,  CHUN, Byoung-Kwon ,  WANG, Peiyuan

IPC分类号： C07H19/06 ,  C07H19/207 ,  A61K31/7072 ,  C07F9/26 ,  A61P31/14 ,  C07F9/24 ,  C07F9/655 ,  C07F9/6558 ,  C07F9/6561 ,  C07H19/04 ,  C07H19/044 ,  C07H19/052 ,  C07H19/10 ,  C07H19/24 ,  A61K31/664 ,  A61K31/7056

CPC分类号： C07H19/10 ,  C07F7/1856 ,  C07F9/242 ,  C07F9/2458 ,  C07F9/65517 ,  C07F9/65586 ,  C07F9/65616 ,  C07H19/04 ,  C07H19/044 ,  C07H19/052 ,  C07H19/06 ,  C07H19/20 ,  C07H19/207 ,  C07H19/24

摘要： Disclosed herein are nucleoside phosphorainidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals.

公开(公告)号：EP1625138A4

公开(公告)日：2010-06-23

申请号：EP04759940

申请日：2004-04-16

申请人： ALNYLAM PHARMACEUTICALS INC

发明人： MANOHARAN MUTHIAH

IPC分类号： C12N15/11 ,  C07C20060101 ,  C07C233/00 ,  C07D207/00 ,  C07H7/04 ,  C07H7/06 ,  C07H19/00 ,  C07H19/02 ,  C07H19/04 ,  C07H19/044 ,  C07H19/052 ,  C07H19/056 ,  C07H19/067 ,  C07H19/14 ,  C07H19/167 ,  C07H19/22 ,  C07H19/23 ,  C07H19/24 ,  C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  C07H23/00 ,  C12N15/00

CPC分类号： C07H23/00 ,  A61K31/00 ,  C07H7/04 ,  C07H7/06 ,  C07H19/02 ,  C07H19/04 ,  C07H19/044 ,  C07H19/052 ,  C07H19/056 ,  C07H19/067 ,  C07H19/14 ,  C07H19/167 ,  C07H19/22 ,  C07H19/23 ,  C07H19/24 ,  C07H21/02

公开(公告)号：EP1780214A3

公开(公告)日：2008-06-18

申请号：EP07003419.4

申请日：2001-06-13

申请人： INSTITUT PASTEUR ,  CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)

发明人： Marliere, Philippe ,  Pochet, Sylvie

IPC分类号： C07H19/044 ,  C07H19/052 ,  C07H19/056 ,  C07H19/06 ,  C07H19/16 ,  C07H21/00 ,  C12Q1/68 ,  G01N33/53 ,  A61K31/7052 ,  A61P31/12 ,  A61P35/00

CPC分类号： C07H19/06 ,  A61K31/7052 ,  C07H19/044 ,  C07H19/052 ,  C07H19/056 ,  C07H19/16 ,  C07H21/00 ,  C12N15/102 ,  C40B40/00 ,  Y02P20/55

摘要： La présente invention concerne l'utilisation d'analogues de nucléotides comportant une fonction réactive hydrazide de formule I, notamment le composé de formule suivante :

pour induire des mutations ou inhiber une ADN polymérase ou une kinase.

公开(公告)号：EP1167972A3

公开(公告)日：2006-05-24

申请号：EP01120242.1

申请日：1999-01-22

申请人： Celmed Oncology (USA), Inc.

发明人： Shepard, Michael H. ,  Groziak, Michael P.

IPC分类号： G01N33/50 ,  C12Q1/00 ,  C07H19/04 ,  C07H19/06 ,  C07H19/044 ,  A61K51/00

CPC分类号： C07H19/20 ,  A61K47/54 ,  A61K47/555 ,  A61K47/556 ,  A61K47/67 ,  B82Y5/00 ,  C07F9/65122 ,  C07H19/06 ,  C07H19/10

摘要： This invention provides a method for identifying potential therapeutic agents by contacting a target cell with a candidate therapeutic agent which is a selective substrate for an endogenous, intracellular enzyme in the cell which is enhanced in its expression as a result of selection by biologic or chemotherapy. This invention also provides methods and examples of molecules for selectively killing a pathological cell by contacting the cell with a prodrug that is a selective substrate for an endogenous, intracellular enzyme. The prodrug is subsequently converted to a cellular toxin. Further provided by this invention is a method for treating a pathology characterized by pathological, hyperproliferative cells in a subject by administering to the subject a prodrug that is a selective substrate for an endogenous, overexpressed, intracellular enzyme, and converted by the enzyme to a cellular toxin in the hyperproliferative cell.

公开(公告)号：EP1258490B1

公开(公告)日：2003-11-26

申请号：EP01906200.9

申请日：2001-02-22

申请人： BANYU PHARMACEUTICAL CO., LTD.

发明人： HIRAGA, Shouichi, c/o Banyu Pharmaceut. Co., Ltd ,  KAWASAKI, Masashi, c/o Banyu Pharmaceut. Co., Ltd ,  AKAO, Atsushi, c/o Banyu Pharmaceutical Co., Ltd ,  KAMATANI, Asayuki, c/o Banyu Pharmaceut. Co., Ltd ,  HAGIWARA, Masayuki, c/o Banyu Pharmaceut. Co., Ltd ,  NAKANO, Fumio, c/o Banyu Pharmaceutical Co., Ltd ,  MASE, Toshiaki, c/o Banyu Pharmaceutical Co., Ltd

IPC分类号： C07H19/044

CPC分类号： C07H15/252 ,  A61K31/7052 ,  C07H19/044 ,  C07H19/23 ,  Y02P20/55

摘要： A process for preparing indolopyrrolocarbazole derivatives [I] by treating a compound [V] with a base in an inert solvent to prepare a compound [IV], reacting the compound [IV] with a compound [III] to prepare a compound [II], and deblocking the compound [II]; intermediates [II], [III] and [IV]; and a process for preparing compounds [III]:[wherein Y is hydrogen, C1-4 alkyl, phenyl, benzyloxymethyl, or aralkyl; R , R , R , R , R and R are each independently a hydroxyl-protecting group; R and R are each independently hydrogen or a hydroxyl-protecting group; and X is an acid molecule]. The above process is a safe and easy industrial process for preparing indolopyrrolocarbazole derivatives [1] useful as antitumor agents.

摘要翻译： 通过在惰性溶剂中用碱处理化合物[V]制备化合物[IV]，使化合物[IV]与化合物[III]反应制备化合物[II]，制备吲哚并吡咯并咔唑衍生物[ ，并将化合物[II]解封闭; 中间体[II]，[III]和[IV]; 和制备化合物[III]的方法：[其中Y 1是氢，C 1-4烷基，苯基，苄氧基甲基或芳烷基; R 1，R 2，R 3，R 4，R 5和R 6各自独立地为羟基保护基; R 7和R 8各自独立地为氢或羟基保护基; 并且X是酸分子]。 上述过程是用于制备可用作抗肿瘤剂的吲哚并吡咯并咔唑衍生物[1]的安全且容易的工业方法。

公开(公告)号：EP1302474A1

公开(公告)日：2003-04-16

申请号：EP02021991.1

申请日：1997-10-15

申请人： Ribapharm, Inc.

发明人： Ramasamy, Kandasamy ,  Tam, Robert ,  Averett, Devron

IPC分类号： C07H15/20 ,  C07H19/00 ,  C07H19/02 ,  C07H19/04 ,  C07H19/044 ,  C07H19/048 ,  C07H19/052 ,  C07H19/056 ,  C07H19/06 ,  C07H19/12

CPC分类号： C07H19/056

摘要： Novel monocyclic L-nucleoside compounds have the general formula (I). Embodiments of these compounds are contemplated to be useful in treating a wide variety of diseases including infections, infestations, neoplasms, and autoimmune diseases. Viewed in terms of mechanism, embodiments of the novel compounds show immunomodulatory activity, and are expected to be useful in modulating the cytokine pattern, including modulation of Th1 and Th2 response.

公开(公告)号：EP1246832A1

公开(公告)日：2002-10-09

申请号：EP00986610.4

申请日：2000-12-15

申请人： ICN Pharmaceuticals, Inc.

发明人： TAM, Robert

IPC分类号： C07H19/044 ,  C07H19/056 ,  A01N43/04 ,  A61K31/70

CPC分类号： A61K31/7056 ,  C07H19/044 ,  C07H19/056

摘要： A 1-(β-L-ribofuranosyl)-1,2,4-triazole-3-carboxamide is administered in a method of treatment of a viral infection in a patient, including HIV infection, HCV infection, or BHV infection.