公开(公告)号：US20210347715A1

公开(公告)日：2021-11-11

申请号：US17190694

申请日：2021-03-03

申请人： Countertrace, LLC

发明人： Robert E. Hanes, Jr. ,  Richard L. Pettys ,  David M. Headley ,  Paul T. Hoopingarner

IPC分类号： C07C22/04 ,  C07D303/36 ,  C07C235/60 ,  C07C247/10 ,  C07D249/06 ,  C07D405/14

摘要： Phenyl rings provide a robust scaffold for molecular design, given the limited number of ring carbon atoms and the fixed geometry in between. However, it can be difficult to form highly substituted phenyl rings suitable for covalent attachment of multiple moieties thereto. Moreover, binding phenyl rings to a surface in a fixed geometry may be difficult. Hexasubstituted benzenes having certain structural features may alleviate the foregoing difficulties by providing versatile groups for further functionalization and surface attachment. Such hexasubstituted benzenes may have a structure of in which each X is independently Cl, Br or N3, and each Z is independently —CH(Br)CH3, —CH(N3)CH3, —CH═CH2, —CH2CH3, —CH2CH2SiR′3 (R′=hydrocarbyl), or Alternating groups in the hexasubstituted benzenes may be directed toward opposite faces of the phenyl ring, such that orthogonal reactive groups are directed toward the opposite faces. Certain groups may facilitate surface attachment of the hexasubstituted benzenes.

公开(公告)号：US20190284231A1

公开(公告)日：2019-09-19

申请号：US16433862

申请日：2019-06-06

申请人： LAURUS LABS LIMITED

发明人： Sanjay Kumar Dehury ,  Nagaraju Mekala ,  Jahangeer Baba Shaik ,  Srinivasa Rao Buddepu ,  Lakshmi Kanth Kola ,  Venkata Sunil Kumar Indukuri ,  Seeta Rama Anjaneyulu Gorantla ,  Satyanarayana Chava

IPC分类号： C07K5/103 ,  C07D303/36 ,  A61K9/00 ,  C07C271/18 ,  C07C271/22 ,  C07C271/16

摘要： The present invention relates to an improved process for the preparation of carfilzomib or a pharmaceutically acceptable salt thereof. The present invention also relates to a process for the preparation of amorphous form of carfilzomib.

公开(公告)号：US10364269B2

公开(公告)日：2019-07-30

申请号：US15573912

申请日：2016-05-21

申请人： LAURUS LABS PRIVATE LIMITED

发明人： Sanjay Kumar Dehury ,  Nagaraju Mekala ,  Jahangeer Baba Shaik ,  Srinivasa Rao Buddepu ,  Lakshmi Kanth Kola ,  Venkata Sunil Kumar Indukuri ,  Seeta Rama Anjaneyulu Gorantla ,  Satyanarayana Chava

IPC分类号： C07K5/103 ,  A61K47/42 ,  C07C271/22 ,  C07D303/36 ,  C07C271/16 ,  C07C271/18 ,  A61K9/00 ,  A61K38/07

摘要： The present invention relates to an improved process for the preparation of carfilzomib or a pharmaceutically acceptable salt thereof. The present invention also relates to a process for the preparation of amorphous form of carfilzomib.

公开(公告)号：US20190185413A1

公开(公告)日：2019-06-20

申请号：US16280996

申请日：2019-02-20

申请人： Quadriga Biosciences, Inc.

发明人： Bernd Jandeleit ,  Wolf-Nicolas Fischer ,  Kerry J. Koller ,  Gordon Ringold

IPC分类号： C07C229/42 ,  C07C233/54 ,  C07C271/22 ,  C07C237/30 ,  C07C239/20 ,  C07C271/14 ,  C07C271/46 ,  C07C229/22 ,  C07C309/69 ,  C07F9/48 ,  A61K45/06 ,  C07D303/32 ,  A61K31/137 ,  A61K31/336 ,  A61K31/245 ,  A61K31/27 ,  A61K31/197 ,  A61K31/255 ,  A61K31/662 ,  A61K31/196 ,  A61K31/42 ,  A61K31/365 ,  A61K31/519 ,  C07C229/60 ,  C07D303/36 ,  C07C237/04 ,  C07C229/34 ,  C07C215/68 ,  C07C291/04

CPC分类号： C07C229/42 ,  A61K31/137 ,  A61K31/196 ,  A61K31/197 ,  A61K31/245 ,  A61K31/255 ,  A61K31/27 ,  A61K31/336 ,  A61K31/365 ,  A61K31/42 ,  A61K31/519 ,  A61K31/662 ,  A61K45/06 ,  C07B2200/07 ,  C07C215/68 ,  C07C229/22 ,  C07C229/34 ,  C07C229/60 ,  C07C233/54 ,  C07C237/04 ,  C07C237/30 ,  C07C239/20 ,  C07C271/14 ,  C07C271/22 ,  C07C271/46 ,  C07C291/04 ,  C07C309/69 ,  C07D303/32 ,  C07D303/36 ,  C07F9/4808

摘要： β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

公开(公告)号：US10280148B2

公开(公告)日：2019-05-07

申请号：US15328262

申请日：2015-09-04

申请人： CANON KABUSHIKI KAISHA

发明人： Satoru Nishioka ,  Satoru Yamada ,  Kazuhiro Yamauchi ,  Yuichi Kikuchi

IPC分类号： G03G15/02 ,  C07D303/36 ,  C08K5/17 ,  C08K5/19 ,  C08L63/00 ,  C08L101/00 ,  G03G15/08 ,  G03G15/16 ,  G03G21/00 ,  C07D471/08 ,  C08G59/24 ,  C08G59/32 ,  C08G59/28 ,  C07D487/08

摘要： Provided is an electroconductive member for electrophotography in which movement of a quaternary ammonium salt toward the surface of a binder resin is suppressed and which exhibits a less reduction in electroconductivity through electrification. The electroconductive member for electrophotography comprises an electroconductive shaft core and a resin layer, and the resin layer comprises a binder resin and at least one selected from quaternary ammonium salts having structures represented by the formulae (1) to (8).

公开(公告)号：US10246406B2

公开(公告)日：2019-04-02

申请号：US15986059

申请日：2018-05-22

申请人： Quadriga Biosciences, Inc.

发明人： Bernd Jandeleit ,  Wolf-Nicolas Fischer ,  Kerry J. Koller ,  Gordon Ringold

IPC分类号： C07C229/42 ,  A61K45/06 ,  A61K31/519 ,  A61K31/365 ,  A61K31/42 ,  A61K31/196 ,  C07F9/48 ,  A61K31/662 ,  C07C309/69 ,  A61K31/255 ,  A61K31/197 ,  C07C229/22 ,  C07C271/46 ,  A61K31/27 ,  C07C271/14 ,  C07C239/20 ,  C07C237/30 ,  C07C229/60 ,  A61K31/245 ,  C07C233/54 ,  C07D303/32 ,  A61K31/336 ,  A61K31/137 ,  C07C271/22 ,  C07C291/04 ,  C07C215/68 ,  C07C229/34 ,  C07C237/04 ,  C07D303/36

摘要： β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

公开(公告)号：US09777135B2

公开(公告)日：2017-10-03

申请号：US15191041

申请日：2016-06-23

申请人： DAICEL CORPORATION

发明人： Masanori Sakane

IPC分类号： B32B27/04 ,  B32B27/18 ,  D06M15/61 ,  C08L79/02 ,  C08G59/00 ,  C08K5/17 ,  C08G59/18 ,  C08G59/24 ,  C07D303/36 ,  C08J5/06 ,  C08J5/24 ,  C07C215/44 ,  C08G59/14

CPC分类号： C08K5/17 ,  C07C215/44 ,  C07C2601/14 ,  C07D303/36 ,  C08G59/1477 ,  C08G59/184 ,  C08G59/24 ,  C08J5/06 ,  C08J5/24 ,  C08J2363/02 ,  Y10T428/2918

摘要： Provided is an epoxy-amine adduct that offers high reactivity, contributes to better adhesion between a resin and a reinforcing fiber in a fiber-reinforced composite material, and can be easily blended with another component such as a resin. The epoxy-amine adduct has two or more amino groups per molecule and is obtained by a reaction of an epoxy compound (A) having two or more alicyclic epoxy groups per molecule with an amine compound (B) having two or more amino groups per molecule. The epoxy compound (A) is preferably a compound represented by Formula (a):

公开(公告)号：US20170144954A1

公开(公告)日：2017-05-25

申请号：US15309758

申请日：2015-05-08

申请人： Mitsubishi Gas Chemical Company, Inc.

发明人： Takashi MAKINOSHIMA ,  Masatoshi ECHIGO

IPC分类号： C07C39/12 ,  C09D161/06 ,  C07C25/22 ,  C07C205/06 ,  C07C211/61 ,  C07D303/36 ,  C07D303/18 ,  C07C69/52 ,  C07C69/533 ,  C07C321/26 ,  C07C43/285 ,  G03F7/004 ,  G03F7/16 ,  G03F7/11 ,  G03F7/039 ,  G03F7/20 ,  G03F7/38 ,  G03F7/32 ,  H01L21/308 ,  H01L21/306 ,  C08G8/08

CPC分类号： C07C39/12 ,  C07C25/22 ,  C07C43/285 ,  C07C69/52 ,  C07C69/533 ,  C07C205/06 ,  C07C211/61 ,  C07C321/26 ,  C07C2603/54 ,  C07D303/18 ,  C07D303/36 ,  C08G8/08 ,  C09D161/06 ,  G03F7/0045 ,  G03F7/039 ,  G03F7/11 ,  G03F7/162 ,  G03F7/168 ,  G03F7/2037 ,  G03F7/26 ,  G03F7/322 ,  G03F7/38 ,  H01L21/027 ,  H01L21/30604 ,  H01L21/3081 ,  H01L21/3086

摘要： The material for forming a film for lithography according to the present invention contains a compound represented by the following formula (1): wherein, each R0 independently represents a monovalent group having an oxygen atom, a monovalent group having a sulfur atom, a monovalent group having a nitrogen atom, a hydrocarbon group or a halogen atom, and each p is independently an integer of 0 to 4.

公开(公告)号：US09359398B2

公开(公告)日：2016-06-07

申请号：US13580112

申请日：2011-03-01

申请人： Kevin D. Shenk ,  Francesco Parlati ,  Mark K. Bennett

发明人： Kevin D. Shenk ,  Francesco Parlati ,  Mark K. Bennett

IPC分类号： A01N37/18 ,  A61K38/00 ,  A61P31/00 ,  A61P29/00 ,  A61P3/04 ,  A61P25/00 ,  A61P35/00 ,  A61K38/06 ,  A61K38/07 ,  C07K5/00 ,  C07K7/00 ,  C07K16/00 ,  C07K17/00 ,  C07K5/08 ,  C07D209/20 ,  C07D241/24 ,  C07D295/104 ,  C07D303/36 ,  C07D405/12

CPC分类号： C07K5/0827 ,  C07D209/20 ,  C07D241/24 ,  C07D295/104 ,  C07D303/36 ,  C07D405/12

摘要： One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.

摘要翻译： 本发明的一个方面涉及优先抑制免疫蛋白酶体活性超过组成型蛋白酶体活性的抑制剂。 在某些实施方案中，本发明涉及治疗免疫相关疾病，包括施用本发明的化合物。 在某些实施方案中，本发明涉及治疗癌症，包括施用本发明的化合物。

公开(公告)号：US20150126755A1

公开(公告)日：2015-05-07

申请号：US14391033

申请日：2013-06-27

申请人： NISSAN CHEMICAL INDUSTRIES, LTD.

发明人： Yukihiro Nishino ,  Kazuya Wakui ,  Shota Murase ,  Yoshifumi Sakai

IPC分类号： C07D301/00 ,  C07D303/36 ,  C07C213/00

CPC分类号： C07D301/00 ,  C07C213/00 ,  C07C269/06 ,  C07D301/19 ,  C07D303/36 ,  Y02P20/55 ,  C07C271/16

摘要： A novel method for producing a stereoselective epoxyketone compound is provided. A method for producing an epoxyketone compound represented by the formula (1), as represented by the following scheme, whereby it is possible to obtain an epoxyketone derivative in good yield and at high selectivity and to provide an industrially useful production method and an intermediate thereof. wherein R1 is a hydrogen atom, a linear, branched or cyclic alkyl group, an aromatic group which may have a substituent, or a heterocyclic group which may have a substituent, and R2 is a protective group for an amino group. R is a hydrogen atom or a C1-10 alkyl group, and R's may be the same or different, provided that at least one R is a C1-10 alkyl group.

摘要翻译： 提供了一种制备立体选择性环氧酮化合物的新方法。 由下式表示的由式（1）表示的环氧酮化合物的制造方法，可以以良好的收率和高选择性得到环氧酮衍生物，提供工业上有用的制造方法及其中间体 。 其中，R 1为氢原子，直链状，支链状或环状的烷基，可具有取代基的芳香族基，或可具有取代基的杂环基，R2为氨基的保护基。 R是氢原子或C 1-10烷基，R可以相同或不同，条件是至少一个R是C1-10烷基。