公开(公告)号：EP1143951A2

公开(公告)日：2001-10-17

申请号：EP99951524.0

申请日：1999-09-21

Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC. ,  The Trustees of Columbia University in the City of New York

Inventor： BERGERON, Raymond, J. ,  BRITTENHAM, Gary, M.

IPC: A61K31/00

CPC classification number: C07D417/04 ,  A61K31/4164 ,  A61K31/426 ,  A61K31/4436 ,  A61K31/4439 ,  C07D207/22 ,  C07D233/28 ,  C07D277/10 ,  C07D277/12 ,  Y02A50/411

Abstract: Composition, article of manufacture for and method of treating malaria in a human having an infestation of Plasmodium protozoans are described. The method comprises administering a therapeutically-effective amount of a compound of formula (I) or (IV), i.e. sufficient quantity to reduce the population of Plasmodium. The composition of the invention is a compound of formula (I) or (IV) with a pharmaceutical excipient. The article of manufacture is the composition in combination with labeling for treating malaria. The substituents are detailed in the specification.

公开(公告)号：EP0976741A4

公开(公告)日：2000-12-20

申请号：EP97901828

申请日：1997-02-04

Applicant: SHIONOGI & CO

Inventor： HAYASE YOSHIO ,  KOBAYASHI SHINOBU ,  UEDA KAZUO ,  HIDAKA SHIGETADA

IPC: C07D277/10 ,  C07D277/12 ,  C07K5/078 ,  C12P17/16 ,  A61K31/425 ,  A61K38/05

CPC classification number: C07K5/06139 ,  C07D277/10 ,  C07D277/12 ,  C12P17/167

Abstract: Novel compounds having various biological activities useful as drugs and animal drugs. Compounds represented by general formula (I) and salts or metal complexes thereof, wherein R1 represents COOR?4, CONR5R6, CO-R7¿-OR or CH¿2?OR?8; R2¿ represents hydrogen, alkyl, aralkyl, heteroaryl, heteroaryl-alkyl, COR?13, COOR14¿ or CONR?15R16; R3¿ represents oxygen or OR3'; and the broken line (- - -) represents the presence of a double bond when R3 is oxygen, or the absence of a double bond when R?3 is OR3'¿.

公开(公告)号：EP3190106A1

公开(公告)日：2017-07-12

申请号：EP16196408.5

申请日：2006-03-22

Applicant: University of Florida Research Foundation, Inc.

Inventor： Bergeron,, Raymond J

IPC: C07D277/10 ,  A61K31/426 ,  A61P39/04

CPC classification number: C07D277/12 ,  A61K31/426 ,  C07B2200/07 ,  C07D277/10

Abstract: Compounds represented by structural formulas described herein, such as Structural Formula (I): are useful in treating conditions such as metal overload, oxidative stress, and neoplastic and preneoplastic conditions.

Abstract translation: 由本文所述的结构式如结构式（I）代表的化合物：可用于治疗诸如金属超负荷，氧化应激以及肿瘤和肿瘤前病症的病症。

公开(公告)号：EP1866296B1

公开(公告)日：2016-11-02

申请号：EP06739627.5

申请日：2006-03-22

Applicant: University of Florida Research Foundation, Inc.

Inventor： BERGERON, Raymond J.

IPC: C07D277/10 ,  A61K31/426 ,  A61P39/04

CPC classification number: C07D277/12 ,  A61K31/426 ,  C07B2200/07 ,  C07D277/10

Abstract: Compounds represented by structural formulas described herein, such as Structural Formula (I): are useful in treating conditions such as metal overload, oxidative stress, and neoplastic and preneoplastic conditions.

公开(公告)号：EP3071201A1

公开(公告)日：2016-09-28

申请号：EP14864521.1

申请日：2014-11-21

Applicant: University of Florida Research Foundation, Inc.

Inventor： BERGERON, Raymond, J., Jr.

IPC: A61K31/426

CPC classification number: A61K31/426 ,  A61K31/4439 ,  C07D277/12 ,  C07D417/04 ,  C07H15/26

Abstract: Iron overload is associated with pathological conditions such as oxidative stress, transfusional iron overload, thalassemia, primary hemochromatosis, secondary hemochromatosis, diabetes, liver disease, heart disease, cancer, radiation injury, neurological or neurodegenerative disorder, Friedreich's ataxia (FRDA), macular degeneration, closed head injury, irritable bowel disease, and reperfusion injury. The present invention provides methods and pharmaceutical compositions using desferrithiocin analogs of Formulae (A) and (J) for treating and/or preventing these pathological conditions, metal (e.g., iron, aluminum, a lanthanide, or an actinide (e.g., uranium)) overload conditions, and infectious diseases (e.g., malaria).

Abstract translation: 铁超载与氧化应激，输血铁超载，地中海贫血，原发性血色素沉着症，继发性血色素沉着症，糖尿病，肝病，心脏病，癌症，放射性损伤，神经或神经变性疾病，弗里德里希共济失调（FRDA），黄斑变性 闭合性头部损伤，肠易激综合征和再灌注损伤。 本发明提供了使用式（A）和（J）的脱铁硫代类似物用于治疗和/或预防这些病理状况的方法和药物组合物，金属（例如铁，铝，镧系元素或锕系元素（例如铀）） 过载条件和传染病（如疟疾）。

公开(公告)号：EP2787994A1

公开(公告)日：2014-10-15

申请号：EP12856135.4

申请日：2012-12-07

Applicant: Ferrokin Biosciences, Inc.

Inventor： RIENHOFF, Hugh, Y., Jr.

IPC: A61K31/426 ,  C07D277/00

CPC classification number: C07D277/12 ,  A61K9/4866 ,  A61K31/426

Abstract: The present invention provides, among other things, effective oral formulations based on desazadesferrithiocin polyether (DADFT-PE) analogues, salts and polymorphs thereof, as well as their application for treatment of metal overload, in particular, iron overload, and associated diseases, disorders and conditions.

公开(公告)号：EP2754657A1

公开(公告)日：2014-07-16

申请号：EP12825868.8

申请日：2012-08-22

Applicant: The University of Electro-Communications

Inventor： NISHIYAMA Shigeru ,  SAITO Tsuyoshi ,  MAKI Shojiro ,  NIWA Haruki

IPC: C07D277/12 ,  C07D277/66 ,  C12Q1/66 ,  G01N21/76

CPC classification number: C12Q1/66 ,  A61K49/003 ,  C07D277/12 ,  C07D277/66 ,  C07D417/04 ,  C07D417/06

Abstract: [Problem] It is an object of the present invention to provide a firefly luciferin and firefly luciferin analog that are modified to maintain luminescent activity by luciferase in a firefly bioluminescent system. In particular, it is an object of the present invention to provide a new luminescent substrate for which the emission wavelength in a firefly bioluminescent system is shifted to a longer wavelength than that of a conventional luminescent substrate.
[Solution] The present invention provides a luciferin in which the benzothiazole ring moiety has been modified at the 7-position, a luciferin analog in which the benzene ring moiety has been modified at the 6-position, and a luciferin analog in which the 6-(dialkylamino)-2-naphthalenyl moiety has been modified at the 5-position.

Abstract translation: 本发明的目的是提供萤火虫荧光素和萤火虫萤光素类似物，其被修饰以通过荧光素酶在萤火虫生物发光系统中维持发光活性。 特别地，本发明的目的是提供一种荧光生物发光系统中的发射波长比常规发光基片的波长更长的新的发光基片。 [解决方案]本发明提供了其中苯并噻唑环部分已在7位修饰的荧光素，其中苯环部分已经在6位被修饰的萤光素类似物和荧光素类似物，其中6位 - （二烷基氨基）-2-萘基部分已在5位修饰。

公开(公告)号：EP2096112A3

公开(公告)日：2009-09-09

申请号：EP09160649.1

申请日：1997-03-31

Applicant: University of Florida Research Foundation, Inc.

Inventor： Bergeron, Raymond J Jr

IPC: C07D277/10 ,  C07D277/12 ,  C07D417/04 ,  A61K31/425

CPC classification number: C07D417/04 ,  C07D277/10 ,  C07D277/12

Abstract: Derivatives of 2-(2-Hydroxy aryl)-thiazoline-4-carboxylic acids are useful as chelators of trivalent metals in therapeutic applications.

公开(公告)号：EP0937708B1

公开(公告)日：2002-12-18

申请号：EP99301296.2

申请日：1999-02-23

Applicant: ELI LILLY AND COMPANY

Inventor： Escribano, Ana Maria ,  Ornstein, Paul Leslie ,  Arnold, Macklin Brian ,  Zimmerman, Dennis Michael

IPC: C07C311/03 ,  C07C311/04 ,  C07C311/05 ,  C07C311/06 ,  C07D207/325 ,  C07D213/42 ,  C07D277/10 ,  C07D277/28 ,  C07D307/52 ,  C07D307/88 ,  C07D333/20 ,  C07D401/04 ,  A61K31/18

CPC classification number: C07D213/40 ,  C07C311/03 ,  C07C311/04 ,  C07C311/05 ,  C07C311/06 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07D277/12 ,  C07D277/28 ,  C07D333/20 ,  C07D409/04

公开(公告)号：EP1214292A1

公开(公告)日：2002-06-19

申请号：EP00965417.9

申请日：2000-09-25

Applicant: Genentech, Inc.

Inventor： JACKSON, David, Y. ,  SAILES, Frederick, C. ,  SUTHERLIN, Daniel, P.

IPC: C07C271/44

CPC classification number: C07D213/75 ,  C07C233/87 ,  C07C271/22 ,  C07C271/44 ,  C07C271/48 ,  C07C271/54 ,  C07C271/56 ,  C07C271/58 ,  C07C311/06 ,  C07C311/09 ,  C07C311/58 ,  C07C323/43 ,  C07C323/59 ,  C07D207/16 ,  C07D207/22 ,  C07D207/28 ,  C07D211/46 ,  C07D211/60 ,  C07D211/62 ,  C07D215/36 ,  C07D217/06 ,  C07D217/14 ,  C07D217/22 ,  C07D231/16 ,  C07D235/06 ,  C07D235/26 ,  C07D249/18 ,  C07D277/12 ,  C07D277/56 ,  C07D295/205 ,  C07D317/58 ,  C07D333/20 ,  C07D333/34 ,  C07D333/38 ,  C07D333/62 ,  C07D333/72 ,  C07D471/10

Abstract: The compounds of the invention are inhibitors of alpha4 containing integrin-mediated binding to ligands such as VCAM-1 and MAdCAM.