公开(公告)号：US20180072745A1

公开(公告)日：2018-03-15

申请号：US15823411

申请日：2017-11-27

Applicant: SHANGHAI FOSUN PHARMACEUTICAL NDUSTRIAL DEVELOPMENT CO. LTD.

Inventor： Qingping Zeng ,  Warren S. Wade ,  John Bruce Patterson

IPC: C07D487/08 ,  C07D277/18 ,  C07D307/68 ,  C07D409/12 ,  C07D263/34 ,  C07D277/12 ,  C07D295/32 ,  C07D295/26 ,  C07D401/04 ,  C07D211/58 ,  C07D211/26 ,  C07D213/38 ,  C07D401/12 ,  C07D207/16 ,  C07D249/06 ,  C07D295/108 ,  C07D213/74 ,  C07D207/08 ,  C07D207/14 ,  C07D295/112 ,  C07D333/38

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：US09751847B2

公开(公告)日：2017-09-05

申请号：US13878189

申请日：2011-10-14

Applicant: Eric W. Schmidt ,  Zhenjian Lin ,  Rowena R. Antemano ,  Alan Light ,  Baldomero M. Olivera ,  Gisela P. Concepcion

Inventor： Eric W. Schmidt ,  Zhenjian Lin ,  Rowena R. Antemano ,  Alan Light ,  Baldomero M. Olivera ,  Gisela P. Concepcion

IPC: A61K31/427 ,  A61K31/425 ,  C07D277/10 ,  A61K31/421 ,  A61K31/426 ,  A61K45/06 ,  C07D277/12

CPC classification number: C07D277/10 ,  A61K31/421 ,  A61K31/426 ,  A61K31/427 ,  A61K45/06 ,  C07D277/12 ,  A61K2300/00

Abstract: In one aspect, the invention relates to compounds having a general structure: and methods of using same to modulate calcium release. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

公开(公告)号：US09096553B2

公开(公告)日：2015-08-04

申请号：US14264959

申请日：2014-04-29

Applicant: University of Florida Research Foundation, Inc.

Inventor： Raymond J. Bergeron, Jr.

IPC: C07D277/12 ,  C07D277/10

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

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

Abstract translation: 由结构式（I）表示的结构式表示的化合物或其药学上可接受的盐可用于治疗诸如金属过载，氧化应激和肿瘤和肿瘤前病症的病症。

公开(公告)号：US20140018400A1

公开(公告)日：2014-01-16

申请号：US13878189

申请日：2011-10-14

Applicant: Eric W. Schmidt ,  Zhenjian Lin ,  Rowena R. Antemano ,  Alan Light ,  Baldomero M. Olivera ,  Gisela P. Concepcion

Inventor： Eric W. Schmidt ,  Zhenjian Lin ,  Rowena R. Antemano ,  Alan Light ,  Baldomero M. Olivera ,  Gisela P. Concepcion

IPC: C07D277/10 ,  A61K31/426 ,  C07D277/12 ,  A61K45/06

CPC classification number: C07D277/10 ,  A61K31/421 ,  A61K31/426 ,  A61K31/427 ,  A61K45/06 ,  C07D277/12 ,  A61K2300/00

Abstract: In one aspect, the invention relates to compounds having a general structure: and methods of using same to modulate calcium release. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract translation: 一方面，本发明涉及具有一般结构的化合物及其用于调节钙释放的方法。 该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。

公开(公告)号：US08324397B2

公开(公告)日：2012-12-04

申请号：US12450194

申请日：2008-03-14

Applicant: Raymond J. Bergeron, Jr.

Inventor： Raymond J. Bergeron, Jr.

IPC: A61K31/426 ,  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.

Abstract translation: 具有式（I）的相对无毒的脱氮代铁硫代类似物：其中：R 1，R 2，R 4和R 5可以相同或不同，可以是H，具有至多14个碳原子的直链或支链烷基，例如甲基， 乙基，丙基和丁基，或芳基烷基，其中芳基部分为烃基，烷基部分为直链或支链，芳基烷基具有至多14个碳原子，R2任选为具有至多14个碳原子的烷氧基; R3是[（CH2）n-O] x - [（CH2）n-O] y-烷基; n独立地为1至8的整数; x是1至8的整数; y为0至8的整数，R3O可占据除4-位之外的苯环上的任何位置，或其盐，水合物或溶剂合物; 以及用于处理三价金属（即铁）过载的作用的方法和组合物。

公开(公告)号：US07153815B2

公开(公告)日：2006-12-26

申请号：US10500925

申请日：2003-01-10

Applicant: Shinji Kawata ,  Shuko Okui ,  Shigeru Suzuki ,  Toshiki Fukuchi ,  Akiyuki Suwa

Inventor： Shinji Kawata ,  Shuko Okui ,  Shigeru Suzuki ,  Toshiki Fukuchi ,  Akiyuki Suwa

IPC: A01N35/08 ,  A01N43/54 ,  A01N43/58 ,  A01N43/40 ,  A01N43/08 ,  A01N43/10 ,  A01N37/18 ,  A01N37/20 ,  C07C239/22 ,  C07C239/20 ,  C07D333/28 ,  C07D277/10 ,  C07D277/12 ,  C07D213/81 ,  C07D213/82 ,  C07D413/12 ,  C07D239/24

CPC classification number: C07D213/40 ,  A01N37/50 ,  A01N43/08 ,  A01N43/10 ,  A01N43/40 ,  A01N43/54 ,  A01N43/58 ,  A01N43/60 ,  A01N43/78 ,  A01N43/80 ,  C07C251/76 ,  C07D213/61 ,  C07D213/68 ,  C07D213/74 ,  C07D213/75 ,  C07D213/77

Abstract: A insecticide characterized by containing as active ingredient a hydrazone derivative of formula (I) wherein A and Q are an aryl or a heterocyclic group, W is oxygen atom, an aminylene, an alkylene group, an oxyalkylene group or an alkyleneoxy, X1 and X2 are hydrogen atom, an alkyl, an alkenyl, an alkynyl, an aryl, a heterocyclic group, formyl, an acyl, an alkoxycarbonyl, an aryloxycarbonyl, a heterocyclic oxycarbonyl, an alkylsulfinyl, an arylsulfinyl, a heterocyclic sulfinyl, an alkylsulfonyl, an arylsulfonyl or a heterocyclic sulfonyl, Y is oxygen atom or sulfur atom, Z is hydrogen atom, a halogen atom, cyano, an alkyl, an alkenyl, an alkynyl, an amino, an alkoxy or an alkylthio, the substituents may be substituted; and novel hydrazon derivatives.

Abstract translation: 一种杀虫剂，其特征在于含有作为活性成分的式（I）腙衍生物，其中A和Q为芳基或杂环基，W为氧原子，亚氨基，亚烷基，氧化烯基或亚烷基氧基，X ^{1和X 2是氢原子，烷基，烯基，炔基，芳基，杂环基，甲酰基，酰基，烷氧基羰基，芳氧基羰基，杂环氧基羰基 ，烷基亚磺酰基，芳基亚磺酰基，杂环亚磺酰基，烷基磺酰基，芳基磺酰基或杂环磺酰基，Y是氧原子或硫原子，Z是氢原子，卤素原子，氰基，烷基，烯基，炔基， 氨基，烷氧基或烷硫基，取代基可以被取代; 和腙衍生物。}

公开(公告)号：US20050245579A1

公开(公告)日：2005-11-03

申请号：US10993417

申请日：2004-11-19

Applicant: Raymond Bergeron

Inventor： Raymond Bergeron

IPC: A61K31/4164 ,  A61K31/426 ,  A61K31/4436 ,  A61K31/4439 ,  C07D207/22 ,  C07D233/28 ,  C07D277/10 ,  C07D277/12 ,  C07D417/04 ,  C07D513/18

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.

Abstract translation: 描述了具有侵染疟原虫原虫的人的组合物，制品和治疗疟疾的方法。 该方法包括施用治疗有效量的式（I）或（IV）的化合物，即足够的量以减少疟原虫的种群。 本发明的组合物是具有药物赋形剂的式（I）或（IV）的化合物。 该制品是与治疗疟疾标签相结合的组合物。 取代基在说明书中详细描述。

公开(公告)号：US20040162433A1

公开(公告)日：2004-08-19

申请号：US10782024

申请日：2004-02-18

Applicant: Schering Aktiengesellschaft

Inventor： John G. Bauman ,  William J. Guilford ,  John F. Parkinson ,  Werner Skuballa ,  Babu Subramanyam

IPC: C11D001/28 ,  C07D327/04 ,  C07D277/12

CPC classification number: C07D317/72 ,  A61K31/202 ,  A61K31/216 ,  C07C59/68 ,  C07C59/70 ,  C07C69/708 ,  C07C69/736 ,  C07C209/68 ,  C07C217/46 ,  C07C229/12 ,  C07C235/06 ,  C07C323/52 ,  C07D317/22

Abstract: This invention is directed to lipoxin A4 analogs of the following formula (I) and (II): 1 wherein R1, R2, R3, R4 and R5 are described herein. These analogs are useful in treating inflammatory and autoimmune disorders in humans. These analogs are also useful in treating pulmonary or respiratory tract inflammation in humans.

Abstract translation: 本发明涉及下述式（I）和（II）的脂氧素A4类似物：其中R 1，R 2，R 3，R 4和R 5如本文所述。 这些类似物可用于治疗人类的炎性和自身免疫性疾病。 这些类似物也可用于治疗人类的肺或呼吸道炎症。

公开(公告)号：US20030100755A1

公开(公告)日：2003-05-29

申请号：US10280652

申请日：2002-10-25

Inventor： Hing Leung Sham ,  Daniel W. Norbeck ,  Xiaoqi Chen ,  David A. Betebenner ,  Dale J. Kempf ,  Thomas R. Herrin ,  Gondi N. Kumar ,  Stephen L. Condon ,  Arthur J. Cooper ,  Daniel A. Dickman ,  Steven M. Hannick ,  Lawrence Kolaczkowski ,  Patricia A. Oliver ,  Daniel J. Plata ,  Peter J. Stengel ,  Eric J. Stoner ,  Jieh-Heh J. Tien ,  Jih-Hua Liu ,  Ketan M. Patel

IPC: C07D279/06 ,  C07D277/12 ,  C07D277/34

CPC classification number: C07D207/27 ,  C07D207/404 ,  C07D207/408 ,  C07D223/10 ,  C07D233/32 ,  C07D233/42 ,  C07D239/10 ,  C07D239/22 ,  C07D241/08 ,  C07D241/18 ,  C07D253/06 ,  C07D263/22 ,  C07D307/20 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12

Abstract: A compound of the formula: 1 is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

公开(公告)号：US20010008902A1

公开(公告)日：2001-07-19

申请号：US09783494

申请日：2001-02-14

Inventor： Hans-Frieder Kuhnle ,  Ernst-Christian Witte ,  Hans-Peter Wolff

IPC: C07D277/04 ,  C07D277/12 ,  C07D277/14 ,  C07D277/16 ,  C07D277/32 ,  C07D277/34 ,  C07D277/36

CPC classification number: C07D417/12 ,  C07D417/14

Abstract: Improved process of compounds of formula III 1 in which A denotes CHnullCH or S W denotes O X denotes S, O or NR2 in which the residue R2 is hydrogen or C1-C6 alkyl, Y denotes CH or N R denotes naphthyl, thienyl or phenyl which is optionally monosubstituted or disubstituted with C1-C3 alkyl, CF3, C1-C3 alkoxy, F, Cl or bromine, R1 denotes hydrogen or C1-C6 alkyl and n denotes 1-3 by reducing a compound of the general formula IV, 2 ,2 in which A, W, X, Y, R, R1 and n have the meanings stated above with activated aluminium in a protic solvent, as well as new compounds of formula III and pharmaceutical preparations containing these compounds.

Abstract translation: 其中A表示CH = CH或SW的式III化合物的改进方法表示OX表示其中残基R2为氢或C1-C6烷基，Y表示CH或NR的S，O或NR2表示萘基，噻吩基或苯基， 任选被C 1 -C 3烷基，CF 3，C 1 -C 3烷氧基，F，Cl或溴单取代或二取代，R 1表示氢或C 1 -C 6烷基，n表示1-3，通过将通式IV， 其中A，W，X，Y，R，R 1和n在质子溶剂中具有上述含活性铝的含义，以及新的式III化合物和含有这些化合物的药物制剂。