公开(公告)号：EP2763677B1

公开(公告)日：2020-02-26

申请号：EP12837804.9

申请日：2012-10-03

Applicant: Janus Biotherapeutics, Inc. ,  Lipford, Grayson, B. ,  Zepp, Charles, M.

Inventor： LIPFORD, Grayson, B. ,  ZEPP, Charles, M.

IPC: A61K31/535 ,  C07D471/00 ,  A01N43/42 ,  A61K31/44

公开(公告)号：EP2763677A4

公开(公告)日：2015-05-20

申请号：EP12837804

申请日：2012-10-03

Applicant: JANUS BIOTHERAPEUTICS INC ,  LIPFORD GRAYSON B ,  ZEPP CHARLES M

Inventor： LIPFORD GRAYSON B ,  ZEPP CHARLES M

IPC: A61K31/535 ,  A01N43/42 ,  A61K31/44 ,  C07D471/00

CPC classification number: C07D471/04

Abstract: The present invention relates to a compound of Formula I: or an enantiomer, diastereomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.

公开(公告)号：EP2763677A2

公开(公告)日：2014-08-13

申请号：EP12837804.9

申请日：2012-10-03

Applicant: Janus Biotherapeutics, Inc. ,  Lipford, Grayson, B. ,  Zepp, Charles, M.

Inventor： LIPFORD, Grayson, B. ,  ZEPP, Charles, M.

IPC: A61K31/535 ,  C07D471/00 ,  A01N43/42 ,  A61K31/44

CPC classification number: C07D471/04

Abstract: The present invention relates to a compound of Formula I: or an enantiomer, diastereomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.

Abstract translation: 本发明涉及式I化合物或其对映异构体，非对映异构体，互变异构体或其药学上可接受的盐或溶剂合物，其中符号如说明书中所定义; 包含其的药物组合物; 以及使用其治疗或预防自身免疫性疾病的方法。

公开(公告)号：WO2012167053A1

公开(公告)日：2012-12-06

申请号：PCT/US2012/040425

申请日：2012-06-01

Applicant: JANUS BIOTHERAPEUTICS, INC. ,  LIPFORD, Grayson, B. ,  ZEPP, Charles, M.

Inventor： LIPFORD, Grayson, B. ,  ZEPP, Charles, M.

IPC: A01N43/90 ,  A61K31/52 ,  C07D473/00

CPC classification number: C07D473/34 ,  C07D473/24 ,  C07D473/30 ,  C07D473/32 ,  C07D473/38 ,  C07D473/40

Abstract: The present invention relates to a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.

Abstract translation: 本发明涉及式I化合物或其药学上可接受的盐，其中符号如说明书中所定义; 包含其的药物组合物; 以及使用其治疗或预防自身免疫性疾病的方法。

公开(公告)号：WO2005007672A3

公开(公告)日：2005-09-15

申请号：PCT/US2004019714

申请日：2004-06-18

Applicant: COLEY PHARM GMBH ,  COLEY PHARM GROUP INC ,  LIPFORD GRAYSON B ,  FORSBACH ALEXANDRA ,  ZEPP CHARLES M

Inventor： LIPFORD GRAYSON B ,  FORSBACH ALEXANDRA ,  ZEPP CHARLES M

IPC: A01N43/54 ,  A61K31/517 ,  C07D239/72 ,  C07D471/00 ,  C07K20060101 ,  A61B31/66

CPC classification number: A61K31/437 ,  A61K31/122 ,  A61K31/382 ,  A61K31/4462 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/517 ,  A61K31/5415 ,  A61K31/55 ,  A61K31/553 ,  C07D221/10 ,  C07D239/94 ,  C07D239/95 ,  C07D405/12

Abstract: The invention provides methods and compositions useful for modulating signaling through Toll-like receptors. The methods involve contacting a TLR-expressing cell with a small molecule having a core structure including at least two rings. Certain of the compounds are 4-primary amino quinolines. Many of the compounds and methods are useful specifically for inhibiting immune stimulation involving at least one of TLR9, TLR8, TLR7, and TLR3. The methods may have use in the treatment of autoimmunity, inflammation, allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer, and immunodeficiency.

Abstract translation: 本发明提供了用于调节通过Toll样受体的信号传导的方法和组合物。 该方法涉及使表达TLR的细胞与具有包含至少两个环的核心结构的小分子接触。 某些化合物是4-伯氨基喹啉。 许多化合物和方法特别有用于抑制涉及TLR9，TLR8，TLR7和TLR3中的至少一种的免疫刺激。 该方法可用于治疗自身免疫，炎症，变态反应，哮喘，移植排斥，移植物抗宿主疾病，感染，败血症，癌症和免疫缺陷。

公开(公告)号：WO1996020592A1

公开(公告)日：1996-07-11

申请号：PCT/US1996000271

申请日：1996-01-02

Applicant: HEMASURE INC. ,  ZEPP, Charles, M. ,  HEEFNER, Donald, L.

Inventor： HEMASURE INC.

IPC: A01N01/02

CPC classification number: C12N7/00 ,  A61L2/0011 ,  A61L2/0088 ,  A61L2/08 ,  A61L2/18 ,  C12N7/04 ,  C12N7/06 ,  C12N2710/10363 ,  C12N2750/14363 ,  C12N2770/32463 ,  C12N2770/32663

Abstract: Method for inactivating non-enveloped viruses using a viricide-potentiating agent. In a preferred embodiment, the method may be used to inactivate non-enveloped viruses present within a sample of whole blood or a blood product and comprises (a) adding to the blood sample a photoactivatable viricide, such as a psoralen, hypericin, methylene blue, toluidine blue or the like, which, when activated, is effective in inactivating enveloped viruses; (b) adding to the blood sample a viricide-potentiating chemical agent that increases the sensitivity of non-enveloped viruses to the activated viricide; and (c) activating the photoactivatable viricide. Preferably, the viricide-potentiating chemical agent includes a first moiety which possesses an affinity for a component of the non-enveloped virus and a second moiety which includes a lipid tail, the first and second moieties being structurally interrelated so that, when the first moiety becomes associated with a component of the non-enveloped virus, the second moiety penetrates or at least partially surrounds the viral capsid of the non-enveloped virus. Examples of the chemical agent include cationic lipopolyamines, such as dioctadecylamidoglycylspermine.

Abstract translation: 使用杀病毒剂增效剂灭活非包膜病毒的方法。 在优选的实施方案中，该方法可用于灭活全血或血液制品样品中存在的非包膜病毒，并且包括（a）向血液样品中加入可光活化的杀戮剂，例如补骨脂素，金丝桃素，亚甲基蓝 甲苯胺蓝等，其在活化时有效灭活包膜病毒; （b）向血液样品中加入增加非包膜病毒对活化杀戮剂的敏感性的杀病剂增效化学试剂; 和（c）活化可光活化杀戮剂。 优选地，杀病毒剂增强化学试剂包括对非包膜病毒的组分具有亲和力的第一部分和包含脂质尾部的第二部分，第一和第二部分在结构上相互关联，使得当第一部分 变得与非包膜病毒的组分相关联，第二部分渗透或至少部分地包围非包膜病毒的病毒衣壳。 化学试剂的实例包括阳离子脂多胺，如双十八烷基酰氨基甘氨酰精胺。

公开(公告)号：WO2013052550A3

公开(公告)日：2014-05-15

申请号：PCT/US2012058566

申请日：2012-10-03

Applicant: JANUS BIOTHERAPEUTICS INC ,  LIPFORD GRAYSON B ,  ZEPP CHARLES M

Inventor： LIPFORD GRAYSON B ,  ZEPP CHARLES M

IPC: A61K31/535 ,  A01N43/42 ,  A61K31/44 ,  C07D471/00

CPC classification number: C07D471/04

Abstract: The present invention relates to a compound of Formula (I): or an enantiomer, diastereomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.

Abstract translation: 本发明涉及式（I）的化合物或其对映异构体，非对映异构体，互变异构体或其药学上可接受的盐或溶剂化物，其中符号如说明书中所定义; 包含其的药物组合物; 以及使用其治疗或预防自身免疫性疾病的方法。

公开(公告)号：WO2004033478A3

公开(公告)日：2004-09-30

申请号：PCT/US0331923

申请日：2003-10-08

Applicant: SEPRACOR INC ,  CURRIE MARK G ,  JONES STEVEN ,  ZEPP CHARLES M

Inventor： CURRIE MARK G ,  JONES STEVEN ,  ZEPP CHARLES M

IPC: A61K31/56 ,  C07J5/00 ,  C07J71/00 ,  A61K31/573

CPC classification number: C07J5/00 ,  C07J5/0076 ,  C07J5/0092 ,  C07J71/0031 ,  Y10S514/826 ,  Y10S514/886

Abstract: A genus of 11,21-dihydroxypregna-1,4-diene-3,20-diones is disclosed, in which the 21-hydroxy is esterified with C8 to C24 hydrocarbon or the residue of misoprostol. The compounds are useful for treating rhinitis and asthma, particularly by inhalation, and for treating inflammation, particularly by local or topical administration.

Abstract translation: 公开了11,21-二羟基孕酮-1,4-二烯-3,20-二酮的一种，其中21-羟基被C 8〜C 24烃或米索前列醇的残基酯化。 该化合物可用于治疗鼻炎和哮喘，特别是通过吸入治疗和治疗炎症，特别是通过局部或局部给药治疗炎症。

公开(公告)号：WO2003039540A2

公开(公告)日：2003-05-15

申请号：PCT/US2002/036051

申请日：2002-11-12

Applicant: SEPRACOR INC. ,  HEEFNER, Donald, L. ,  CURRIE, Mark, G. ,  ROSSI, JR., Richard, Filip ,  ZEPP, Charles, M.

Inventor： HEEFNER, Donald, L. ,  CURRIE, Mark, G. ,  ROSSI, JR., Richard, Filip ,  ZEPP, Charles, M.

IPC: A61K31/405

CPC classification number: A61K31/34 ,  A61K31/401 ,  A61K31/404 ,  A61K31/405 ,  A61K31/473

Abstract: Methods and pharmaceutical compositions which inhibit the activity of D-amino acid oxidase (DAO) are disclosed. Inhibition of DAO improves memory, learning and cognition in individuals suffering from neurodegenerative diseases such as Alzheimer's, Huntington's or Parkinson's diseases; the methods and pharmaceutical compositions which inhibit the activity of DAO also improve cognitive dysfunctions associated with aging and improve catatonic schizophrenia. Several genera of heterocycle-2-carboxylic acids are disclosed as DAO inhibitors.

Abstract translation: 公开了抑制D-氨基酸氧化酶（DAO）活性的方法和药物组合物。 DAO的抑制改善了患有神经退行性疾病如阿尔茨海默病，亨廷顿舞蹈病或帕金森病的个体的记忆，学习和认知; 抑制DAO活性的方法和药物组合物也改善与衰老相关的认知功能障碍并改善紧张性精神分裂症。 作为DAO抑制剂公开了几个杂环-2-羧酸的属。

公开(公告)号：WO2004043447A2

公开(公告)日：2004-05-27

申请号：PCT/US2003/036269

申请日：2003-11-13

Applicant: SEPRACOR, INC. ,  CURRIE, Mark, G. ,  HEEFNER, Donald, L. ,  RUBIN, Paul ,  ZEPP, Charles, M.

Inventor： CURRIE, Mark, G. ,  HEEFNER, Donald, L. ,  RUBIN, Paul ,  ZEPP, Charles, M.

IPC: A61K31/17

CPC classification number: A61K31/17 ,  A61K31/495

Abstract: Ototoxic side-effects have either limited the application of an important group of antibiotics, aminoglycoside antibiotics, or have added further burden to those who have to resort to platinum-containing antineoplastic agents to treat life-threatening tumors. The present invention discloses pharmaceutical compositions that prevent or treat the ototoxic side-effects of aminoglycoside antibiotics and platinum-containing antineoplastic agents. The otoprotective compositions disclosed herein can also be used to treat noise induced hearing loss.

Abstract translation: 耳毒性副作用限制了一组重要的抗生素，氨基糖苷类抗生素的应用，或者为那些不得不使用含铂抗肿瘤剂治疗危及生命的肿瘤的人增加了进一步的负担。 本发明公开了预防或治疗氨基糖苷类抗生素和含铂抗肿瘤剂的耳毒性副作用的药物组合物。 本文公开的保护性组合物也可用于治疗噪声引起的听力损失。