公开(公告)号：US20230144767A1

公开(公告)日：2023-05-11

申请号：US18093704

申请日：2023-01-05

申请人： University of Pittsburgh - Of the Commonwealth System of Higher Education

发明人： Peter Wipf ,  Marie-Celine Frantz

IPC分类号： C07K5/08 ,  A61K31/454 ,  C07D211/58 ,  C07D401/12 ,  A61K47/64 ,  C07D417/12 ,  C07C237/16 ,  C07D209/46 ,  C07D211/94 ,  C07D221/22 ,  C07D209/44 ,  C07D279/06 ,  C07D471/08

CPC分类号： C07K5/08 ,  A61K31/454 ,  C07D211/58 ,  C07D401/12 ,  A61K47/64 ,  C07D417/12 ,  C07C237/16 ,  C07D209/46 ,  C07D211/94 ,  C07D221/22 ,  C07D209/44 ,  C07D279/06 ,  C07D471/08

摘要： Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.

公开(公告)号：US20170057914A1

公开(公告)日：2017-03-02

申请号：US15349297

申请日：2016-11-11

申请人： BAYER CROPSCIENCE AG ,  BAYER INTELLECTUAL PROPERTY GMBH

发明人： Adeline KOEHLER ,  Bernd ALIG ,  Angela BECKER ,  Arnd VOERSTE ,  Ulrich GOERGENS ,  Reiner FISCHER ,  Wahed Ahmed MORADI ,  Silvia CEREZO-GALVEZ ,  Julia Johanna HAHN ,  Kerstin ILG ,  Hans-Georg SCHWARZ ,  Takuya GOMIBUCHI ,  Masahito ITO ,  Daiei YAMAZAKI ,  Katsuhiko SHIBUYA ,  Eiichi SHIMOJO

IPC分类号： C07C323/41 ,  C07C323/45 ,  C07C317/40 ,  C07C315/02 ,  C07C323/36 ,  C07D333/38 ,  C07D207/34 ,  C07D307/68 ,  C07C319/14 ,  C07D213/78 ,  C07D295/13 ,  C07D241/24 ,  C07D207/22 ,  C07D279/06 ,  C07D263/28 ,  C07D277/16 ,  C07D277/54 ,  C07C335/16 ,  C07D239/28 ,  C07D305/08 ,  C07D211/98 ,  C07D307/24 ,  C07D277/38 ,  C07D331/04 ,  C07D333/48 ,  C07D211/38 ,  C07D401/06 ,  C07D285/08 ,  C07C319/20

CPC分类号： A01N41/10 ,  A01N41/12 ,  A01N43/08 ,  A01N43/10 ,  A01N43/36 ,  A01N43/40 ,  A01N43/60 ,  A01N43/84 ,  A01N43/86 ,  C07C315/02 ,  C07C317/34 ,  C07C317/40 ,  C07C319/14 ,  C07C319/20 ,  C07C323/36 ,  C07C323/41 ,  C07C323/44 ,  C07C323/45 ,  C07C335/16 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D207/22 ,  C07D207/34 ,  C07D211/38 ,  C07D211/72 ,  C07D211/98 ,  C07D213/61 ,  C07D213/78 ,  C07D239/28 ,  C07D241/24 ,  C07D263/28 ,  C07D277/16 ,  C07D277/18 ,  C07D277/38 ,  C07D277/54 ,  C07D279/06 ,  C07D285/08 ,  C07D295/125 ,  C07D295/13 ,  C07D305/08 ,  C07D307/24 ,  C07D307/68 ,  C07D331/04 ,  C07D333/38 ,  C07D333/48 ,  C07D401/06

摘要： The present invention relates to novel N-arylamide-substituted trifluoroethyl sulfide derivatives of the formula (I) in which X1, X2, X3, X4, R1, R2, R3, n have the meanings given in the description—to their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparation

公开(公告)号：US20160326158A1

公开(公告)日：2016-11-10

申请号：US15222567

申请日：2016-07-28

申请人： Shionogi & Co., Ltd.

发明人： Akihiro HORI ,  Shuji YONEZAWA ,  Chiaki FUJIKOSHI ,  Sae MATSUMOTO ,  Yuuji KOORIYAMA ,  Tatsuhiko UENO ,  Terukazu KATO

IPC分类号： C07D417/12

CPC分类号： C07D417/12 ,  A61K9/0019 ,  A61K9/1623 ,  A61K9/2018 ,  C07D279/06 ,  C07D417/10 ,  C07D417/14 ,  C07D487/04

摘要： The following compound is provided as an agent for treating a disease induced by production, secretion and/or deposition of amyloid β protein, for example., a compound represented by the formula (I): wherein ring A in an optionally substituted carbocyclic group or an optionally substituted heterocyclic group. R1 is optionally substituted lower alkyl or the like, R2a and R2b each independently hydrogen, optionally substituted lower alkyl or the like, R3a and R3c are each independently hydrogen, halogen, hydroxy, optionally substituted lower alkyl or the like, or a pharmaceutical acceptable salt thereof, or a solvate thereof.

公开(公告)号：US09216976B2

公开(公告)日：2015-12-22

申请号：US14088233

申请日：2013-11-22

申请人： Peter Wipf ,  Marie-Celine Frantz

发明人： Peter Wipf ,  Marie-Celine Frantz

IPC分类号： C07D417/12 ,  A61K31/454 ,  A61K47/48 ,  C07D211/58 ,  C07D401/12 ,  C07C237/16 ,  C07D209/46 ,  C07D211/94 ,  C07D221/22

CPC分类号： C07K5/08 ,  A61K31/454 ,  A61K47/64 ,  C07C237/16 ,  C07D209/44 ,  C07D209/46 ,  C07D211/58 ,  C07D211/94 ,  C07D221/22 ,  C07D279/06 ,  C07D401/12 ,  C07D417/12 ,  C07D471/08

摘要： Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.

摘要翻译： 本文提供了可用于自由基清除的组合物和相关方法，对线粒体具有特别的选择性。 化合物包含连接到线粒体靶向基团的含氮氧基的基团。 化合物可以交联成二聚体而不损失活性。 本文还提供了用于防止，减轻和治疗由辐射引起的损伤的方法。 该方法包括以有效预防，减轻或治疗由辐射引起的损伤的量和剂量方案将如本文所述的化合物递送至患者。

公开(公告)号：US20150210680A1

公开(公告)日：2015-07-30

申请号：US14679666

申请日：2015-04-06

申请人： Shionogi & Co., Ltd.

发明人： Naotake KOBAYASHI ,  Kazuo UEDA ,  Naohiro ITOH ,  Shinji SUZUKI ,  Gaku SAKAGUCHI ,  Akira KATO ,  Akira YUKIMASA ,  Akihiro HORI ,  Yuji KORIYAMA ,  Hidekazu HARAGUCHI ,  Ken YASUI ,  Yasuhiko KANDA

IPC分类号： C07D417/14 ,  C07D281/02 ,  C07D265/08 ,  C07D239/14 ,  C07D279/08 ,  C07D417/12 ,  C07D279/12 ,  C07D417/04 ,  C07D405/04 ,  C07D279/06 ,  C07D277/18

CPC分类号： C07D417/14 ,  A61K9/0019 ,  A61K9/1623 ,  A61K9/2018 ,  A61K31/426 ,  A61K31/505 ,  A61K31/506 ,  A61K31/535 ,  A61K31/54 ,  A61K31/541 ,  A61K31/5415 ,  A61K31/55 ,  A61K31/551 ,  A61K31/554 ,  C07D239/14 ,  C07D239/24 ,  C07D239/42 ,  C07D265/08 ,  C07D277/18 ,  C07D279/06 ,  C07D279/08 ,  C07D279/12 ,  C07D281/02 ,  C07D405/04 ,  C07D405/10 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  C07D471/04

摘要： A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a and R4b is each independently a hydrogen atom, halogen, or hydroxy etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 0 to 3; R5 is a hydrogen atom or substituted lower alkyl; its pharmaceutically acceptable salt, or a solvate thereof.

公开(公告)号：US08884062B2

公开(公告)日：2014-11-11

申请号：US13887745

申请日：2013-05-06

申请人： Shionogi & Co., Ltd.

发明人： Yuusuke Tamura ,  Shinji Suzuki ,  Yukio Tada ,  Shuji Yonezawa ,  Chiaki Fujikoshi ,  Sae Matsumoto ,  Yuuji Kooriyama ,  Tatsuhiko Ueno

IPC分类号： C07C215/20

CPC分类号： C07C215/20 ,  A61K9/0019 ,  A61K9/1623 ,  A61K9/2018 ,  C07D279/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04

摘要： This invention provides a compound of the formula (I): wherein the ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl; R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or optionally substituted acyl; R3a, R3b, R3c and R3d are each independently hydrogen, halogen, hydroxy or optionally substituted lower alkyl etc.; a pharmaceutically acceptable salt or solvate thereof, which is useful for treating diseases induced by production, secretion and/or deposition of amyloid β protein.

摘要翻译： 本发明提供式（I）的化合物：其中环A为任选取代的碳环基或任选取代的杂环基; R1是任选取代的低级烷基，任选取代的低级烯基，任选取代的低级炔基; R2a和R2b各自独立地为氢，任选取代的低级烷基或任选取代的酰基; R3a，R3b，R3c和R3d各自独立地为氢，卤素，羟基或任选取代的低级烷基等; 其药学上可接受的盐或溶剂合物，其可用于治疗由淀粉样蛋白的生产，分泌和/或沉积诱导的疾病; 蛋白。

公开(公告)号：US20140058097A1

公开(公告)日：2014-02-27

申请号：US14070202

申请日：2013-11-01

申请人： Shionogi & Co., Ltd.

发明人： Naotake Kobayashi ,  Kazuo Ueda ,  Naohiro Itoh ,  Shinji Suzuki ,  Gaku Sakaguchi ,  Akira Kato ,  Akira Yukimasa ,  Akihiro Hori ,  Yuuji Kooriyama ,  Hidekazu Haraguchi ,  Ken Yasui ,  Yasuhiko Kanda

IPC分类号： C07D471/04 ,  C07D295/192 ,  C07D279/06 ,  C07D285/36 ,  C07D277/18 ,  C07D405/04 ,  C07D295/155 ,  C07D265/08 ,  C07D417/12 ,  C07D417/04

CPC分类号： C07D471/04 ,  A61K9/0019 ,  A61K9/1623 ,  A61K9/2018 ,  A61K31/426 ,  A61K31/506 ,  A61K31/535 ,  A61K31/54 ,  A61K31/541 ,  A61K31/554 ,  C07D239/14 ,  C07D265/08 ,  C07D277/18 ,  C07D279/06 ,  C07D281/02 ,  C07D285/36 ,  C07D295/155 ,  C07D295/192 ,  C07D405/04 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  A61K2300/00

摘要： A pharmaceutical composition for treating Alzheimer's disease containing a compound represented by the general formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene, etc.; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2, R2b, R3a, R3b, R4a and R4b are each independently a hydrogen atom, halogen, hydroxy, etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 1 to 3; and R5 is a hydrogen atom, optionally substituted lower alkyl, etc.; its pharmaceutically acceptable salt, or a solvate thereof as an active ingredient.

摘要翻译： 一种用于治疗含有由通式（I）表示的化合物的阿尔茨海默病的药物组合物：其中环A是任选取代的碳环基团或任选取代的杂环基团; E为低级亚烷基等; X是S，O或NR1; R1是氢原子或低级烷基; R2，R2b，R3a，R3b，R4a和R4b各自独立地为氢原子，卤素，羟基等; n和m各自独立地为0〜3的整数， n + m为1〜3的整数， R5为氢原子，任意取代的低级烷基等; 其药学上可接受的盐或其溶剂合物作为活性成分。

公开(公告)号：US20130303755A1

公开(公告)日：2013-11-14

申请号：US13941082

申请日：2013-07-12

申请人： Shionogi & Co., Ltd.

发明人： Naotake KOBAYASHI ,  Kazuo UEDA ,  Naohiro ITOH ,  Shinji SUZUKI ,  Gaku SAKAGUCHI ,  Akira KATO ,  Akira YUKIMASA ,  Akihiro HORI ,  Yuji KORIYAMA ,  Hidekazu HARAGUCHI ,  Ken YASUI ,  Yasuhiko KANDA

IPC分类号： C07D281/02

CPC分类号： C07D417/14 ,  A61K9/0019 ,  A61K9/1623 ,  A61K9/2018 ,  A61K31/426 ,  A61K31/505 ,  A61K31/506 ,  A61K31/535 ,  A61K31/54 ,  A61K31/541 ,  A61K31/5415 ,  A61K31/55 ,  A61K31/551 ,  A61K31/554 ,  C07D239/14 ,  C07D239/24 ,  C07D239/42 ,  C07D265/08 ,  C07D277/18 ,  C07D279/06 ,  C07D279/08 ,  C07D279/12 ,  C07D281/02 ,  C07D405/04 ,  C07D405/10 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  C07D471/04

摘要： A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a and R4b is each independently a hydrogen atom, halogen, or hydroxy etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 0 to 3; R5 is a hydrogen atom or substituted lower alkyl; its pharmaceutically acceptable salt, or a solvate thereof.

公开(公告)号：US08546380B2

公开(公告)日：2013-10-01

申请号：US13243971

申请日：2011-09-23

申请人： Naotake Kobayashi ,  Kazuo Ueda ,  Naohiro Itoh ,  Shinji Suzuki ,  Gaku Sakaguchi ,  Akira Kato ,  Akira Yukimasa ,  Akihiro Hori ,  Yuji Koriyama ,  Hidekazu Haraguchi ,  Ken Yasui ,  Yasuhiko Kanda

发明人： Naotake Kobayashi ,  Kazuo Ueda ,  Naohiro Itoh ,  Shinji Suzuki ,  Gaku Sakaguchi ,  Akira Kato ,  Akira Yukimasa ,  Akihiro Hori ,  Yuji Koriyama ,  Hidekazu Haraguchi ,  Ken Yasui ,  Yasuhiko Kanda

IPC分类号： C07D279/00 ,  C07D265/00 ,  A61K31/535 ,  A61K31/541

CPC分类号： C07D417/14 ,  A61K9/0019 ,  A61K9/1623 ,  A61K9/2018 ,  A61K31/426 ,  A61K31/505 ,  A61K31/506 ,  A61K31/535 ,  A61K31/54 ,  A61K31/541 ,  A61K31/5415 ,  A61K31/55 ,  A61K31/551 ,  A61K31/554 ,  C07D239/14 ,  C07D239/24 ,  C07D239/42 ,  C07D265/08 ,  C07D277/18 ,  C07D279/06 ,  C07D279/08 ,  C07D279/12 ,  C07D281/02 ,  C07D405/04 ,  C07D405/10 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  C07D471/04

摘要： A composition having BACE 1 inhibitory activity containing a compound represented by the formula (I): wherein ring A is an optionally substituted heterocyclic group; E is lower alkylene; X is S; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a and R4b is each independently a hydrogen atom, halogen, or hydroxy etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 0 to 3; R5 is a hydrogen atom or substituted lower alkyl; or its pharmaceutically acceptable salt thereof.

摘要翻译： 一种具有BACE1抑制活性的组合物，其含有式（I）表示的化合物：其中环A为任选取代的杂环基; E为低级亚烷基; X是S; R1是氢原子或低级烷基; R2a，R2b，R3a，R3b，R4a和R4b各自独立地为氢原子，卤素或羟基等; n和m各自独立地为0〜3的整数， n + m为0〜3的整数， R5是氢原子或取代的低级烷基; 或其药学上可接受的盐。

公开(公告)号：US20130096107A1

公开(公告)日：2013-04-18

申请号：US13706394

申请日：2012-12-06

申请人： Hoffmann-La Roche Inc.

发明人： Jeremy Beauchamp ,  Agnes Benardeau ,  Hans Hilpert ,  Cristiano Migliorini ,  William Riboulet ,  Haiyan Wang

IPC分类号： C07D495/04 ,  C07D279/06 ,  C07D417/12

CPC分类号： C07D495/04 ,  A61K31/54 ,  A61K31/541 ,  C07D279/06 ,  C07D417/12

摘要： This invention relates to compounds of formula I, wherein R1 to R3 are as defined herein, as well as pharmaceutically acceptable salts thereof, pharmaceutical compositions containing such compounds and methods for using such compounds for the treatment or prevention of diabetes, particularly type 2 diabetes.

摘要翻译： 本发明涉及式I化合物，其中R 1至R 3如本文所定义，以及其药学上可接受的盐，含有这些化合物的药物组合物和使用该化合物治疗或预防糖尿病，特别是2型糖尿病的方法。