公开(公告)号：EP2137170B1

公开(公告)日：2016-03-09

申请号：EP08742093.1

申请日：2008-03-14

Applicant: University of Florida Research Foundation, Inc.

Inventor： BERGERON, Raymond, J.

IPC: C07D277/12

CPC classification number: A61K31/426 ,  C07D277/12

Abstract: A relatively non-toxic desazadesferrithiocin analog having the formula (I): wherein: R1, R2, R4 and R5 may be the same or different and may be H, straight or branched chain alkyl having up to 14 carbon atoms, e.g., methyl, ethyl, propyl and butyl, or arylalkyl wherein the aryl portion is hydrocarbyl and the alkyl portion is straight or branched chain, the arylalkyl group having up to 14 carbon atoms, R2 optionally being alkoxy having up to 14 carbon atoms; R3 is [(CH2)n—O]x—[(CH2)n—O]y-alkyl; n is, independently, an integer from 1 to 8; x is an integer from 1 to 8; y is an integer from O to 8, and R3O may occupy any position on the phenyl ring except the 4-position, or a salt, hydrate or solvate thereof; and methods and compositions for treating the effects of trivalent metal, i.e., iron, overload.

公开(公告)号：EP2612861A4

公开(公告)日：2014-01-22

申请号：EP11821153

申请日：2011-08-29

Applicant: UNIV BARCELONA ,  FUNDACIO PRIVADA INST D INVESTIGACIO BIOMEDICA ,  FUNDACIO PRIVADA INST DE RECERCA BIOMEDICA ,  FUNDACIO PRIVADA PARC CIENTIFIC DE BARCELONA

Inventor： GIL SANTANO JOAN ,  LAVILLA GRIFOLS RODOLFO ,  ALBERICIO PALOMERA FERNANDO ,  PEREZ PERARNAU ALBA ,  PRECIADO GALLEGO SARA ,  GONZALEZ GIRONES DIANA MA ,  IGLESIAS SERRET DANIEL ,  RAMON ALBALATE ROSARIO

IPC: C07D417/04 ,  A61K31/426 ,  C07D277/32

CPC classification number: C07D277/30 ,  C07D277/12 ,  C07D277/22 ,  C07D277/24 ,  C07D277/32 ,  C07D277/56 ,  C07D417/04

公开(公告)号：EP2496230A1

公开(公告)日：2012-09-12

申请号：EP10828948.9

申请日：2010-11-01

Applicant: MannKind Corporation

Inventor： ZENG, Qingping ,  WADE, Warren S. ,  PATTERSON, John Bruce

IPC: A61K31/185 ,  A61K31/27

CPC classification number: C07D487/08 ,  C07C59/74 ,  C07C65/30 ,  C07C69/738 ,  C07C235/78 ,  C07C235/84 ,  C07D207/08 ,  C07D207/14 ,  C07D207/16 ,  C07D211/26 ,  C07D211/58 ,  C07D211/62 ,  C07D211/66 ,  C07D211/98 ,  C07D213/36 ,  C07D213/38 ,  C07D213/74 ,  C07D213/81 ,  C07D213/82 ,  C07D239/26 ,  C07D239/38 ,  C07D249/06 ,  C07D263/34 ,  C07D277/12 ,  C07D277/18 ,  C07D277/42 ,  C07D277/56 ,  C07D295/108 ,  C07D295/112 ,  C07D295/185 ,  C07D295/192 ,  C07D295/26 ,  C07D295/32 ,  C07D307/68 ,  C07D333/38 ,  C07D333/40 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D413/06 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12

Abstract: The invention provides compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.

公开(公告)号：EP2303853A2

公开(公告)日：2011-04-06

申请号：EP09798650.9

申请日：2009-07-14

Applicant: Ferrokin Biosciences, Inc.

Inventor： TAPPER, Amy, E. ,  RIENHOFF, Hugh, Y. ,  PARENT, Stephan, D. ,  ANDRES, Patricia

IPC: C07D277/22 ,  C07D277/20 ,  A61K31/426 ,  A61P9/10 ,  A61P25/08 ,  A61P9/02

CPC classification number: C07D277/12 ,  C07D277/10

Abstract: Disclosed herein are new salts and polymorphs of desazadesferrithiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.

Abstract translation: 本文公开了desazadesferrithiocin聚醚（DADFT-PE）类似物的新盐和多晶型物，以及包含它们的药物组合物以及它们作为用于治疗疾病的金属螯合剂的应用。 还提供了人或动物受试者中铁和其他金属螯合的方法用于治疗金属超载和毒性。

公开(公告)号：EP2096112A2

公开(公告)日：2009-09-02

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 ,  C07D417/04 ,  A61K31/426 ,  A61K31/4709 ,  A61P7/00

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：EP1963262A2

公开(公告)日：2008-09-03

申请号：EP06821047.5

申请日：2006-12-04

Applicant: Vicuron Pharmaceuticals, Inc.

Inventor： JAIN, Rakesh, Kumar ,  GORDEEV, Mikhail, Fedorovich ,  LEWIS, Jason, Gustaf ,  FRANCAVILLA, Charles

IPC: C07D207/16 ,  C07D231/12 ,  C07D277/12 ,  C07D277/56 ,  C07D307/68 ,  C07C259/06 ,  C07C317/50 ,  C07C323/60

CPC classification number: C07D207/16 ,  C07C259/06 ,  C07C317/50 ,  C07C323/60 ,  C07D231/12 ,  C07D277/06 ,  C07D277/12 ,  C07D277/56 ,  C07D307/68 ,  C07D333/24

Abstract: Described herein are N-hydroxyamlde antibacterial compounds, methods for making the compounds, pharmaceutical compositions containing the compounds and methods of treating bacterial infections utilizing the compounds and pharmaceutical compositions. compound of Formula (I): or a salt, solvate ti hydrate thereof, wherein A is (a) each ~~~ indicates a point of attachment.

公开(公告)号：EP1656360B1

公开(公告)日：2007-08-15

申请号：EP04755044.7

申请日：2004-06-12

Applicant: JANSSEN PHARMACEUTICA N.V.

Inventor： NG, Raymond A., c/o Johnson & Johnson Pharmaceut. ,  SUI, Zhihua, c/o Johnson & Johnson Pharmaceutical

IPC: C07D277/12 ,  A61K31/426 ,  A61P5/26

CPC classification number: C07D277/12

Abstract: The present invention is directed to novel thiazoline derivatives of the general fomula (I); wherein all variables are as herein defined, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.

公开(公告)号：EP1214292B1

公开(公告)日：2007-06-13

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.

公开(公告)号：EP1548013A1

公开(公告)日：2005-06-29

申请号：EP03748633.9

申请日：2003-10-01

Applicant: KANEKA CORPORATION

Inventor： MARUOKA, Keiji, Kyoto University ,  OOI, Takashi, Kyoto University ,  INOUE, Kenji, Kaneka Corp. Takasago Plant

IPC: C07D277/12 ,  B01J31/02 ,  B01J38/00 ,  C07C321/04 ,  C07C321/08

CPC classification number: B01J31/0239 ,  B01J31/40 ,  C07B2200/07 ,  C07C319/02 ,  C07D277/12 ,  Y02P20/584 ,  C07C323/58

Abstract: The present invention provides a simple, practical, and industrially advantageous process for producing an optically active α-substituted cysteine or a salt thereof from inexpensive and readily available materials.
The present invention provides a process for producing an optically active α-substituted cysteine or a salt thereof by converting a cysteine derivative into a thiazoline compound and subjecting the resulting thiazoline compound to a stereoselective substituent-introducing reaction catalyzed by an optically active quaternary ammonium salt, in particular, an axially asymmetric quaternary ammonium salt to produce an optically active thiazoline compound and then hydrolyzing the resulting thiazoline compound.

Abstract translation: 本发明提供在光学活性的α-取代的半胱氨酸或从廉价且容易获得的材料或其盐生产一种简单，实用，和工业上有利的方法。 本发明提供了一种通过半胱氨酸衍生物将所得的噻唑啉化合物转化成噻唑啉化合物和经受通过在光学活性催化立体选择性取代基的引入反应在光学活性的α-取代的半胱氨酸或其盐的制造它们的 季铵盐，具体地讲，轴不对称季铵盐的以噻唑啉化合物产生光学活性，然后水解所得的噻唑啉化合物。

公开(公告)号：EP1380577A1

公开(公告)日：2004-01-14

申请号：EP03021526.3

申请日：1997-03-31

Applicant: UNIVERSITY OF FLORIDA

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.

Abstract translation: 2-（2-羟基芳基） - 噻唑啉-4-羧酸的衍生物可用作治疗应用中的三价金属的螯合剂。