公开(公告)号：US11505572B2

公开(公告)日：2022-11-22

申请号：US17077859

申请日：2020-10-22

Applicant: Mayo Foundation for Medical Education and Research ,  Regents of the University of Minnesota

Inventor： Michael P. Fautsch ,  Peter Dosa ,  Michael A. Walters ,  Gunda I. Georg

IPC: A61K31/353 ,  C07K5/062 ,  C07D405/04 ,  C07D405/12 ,  C07D285/24 ,  A61K31/549 ,  A61K31/454 ,  A61K31/4025 ,  A61K9/00 ,  A61K31/675 ,  A61K31/4439 ,  C07D201/00 ,  C07D311/20 ,  C07D311/70 ,  C07D405/14 ,  C07F9/6547 ,  C07F9/6558

Abstract: The present invention provides benzothiadiazine and chroman derivatives and particularly diazoxide and cromakalim derivatives for use in treating glaucoma, retinopathy, treating age related macular degeneration, treating, stabilizing and/or inhibiting blood and lymph vascularization, and reducing intraocular pressure by administering a pharmaceutically effective amount of a prodrug disposed in an ophthalmically acceptable carrier to the eye, wherein the prodrug specifically modulates a KATP channel to reduce an intraocular pressure.

公开(公告)号：US11149001B2

公开(公告)日：2021-10-19

申请号：US16466230

申请日：2017-12-05

Applicant: TORAY INDUSTRIES, INC.

Inventor： Daijiro Tsukamoto ,  Masateru Ito ,  Katsushige Yamada ,  Masato Akahira ,  Daisuke Yamamoto ,  Koji Yamauchi

IPC: C07D201/00 ,  C07D223/00 ,  C07C255/00 ,  C07D201/08 ,  C07D223/10

Abstract: A method produces ε-caprolactam through adipamide as an intermediate, and characteristically includes a lactamization step of reacting adipamide, formed from a material compound, with hydrogen and ammonia in the presence of a catalyst containing: a metal oxide mainly containing an oxide(s) of one or more metallic elements selected from the group consisting of metallic elements of group 5 and groups 7 to 14 in the 4th to 6th periods of the periodic table; and a metal and/or a metal compound having a hydrogenation ability.

公开(公告)号：US11110114B2

公开(公告)日：2021-09-07

申请号：US16037157

申请日：2018-07-17

Applicant: OXFORD UNIVERSITY INNOVATION LIMITED

Inventor： Tom Brown ,  Afaf Helmy El-Sagheer ,  Pawan Kumar

IPC: A61K31/7084 ,  A61P31/00 ,  A61P35/00 ,  C07D201/00 ,  C07H19/16 ,  C07H19/00 ,  C07H19/06

Abstract: The present disclosure relates to novel dinucleotides comprising at least two locked nucleosides, one of which is directly attached to the 3′ end of the triazole linker moiety and the other of which is directly linked to the 5′ end of the triazole linker moiety and that are useful for the preparation of oligonucleotides. The disclosed dinucleotides may be used in gene therapy.

公开(公告)号：US10689416B2

公开(公告)日：2020-06-23

申请号：US16393651

申请日：2019-04-24

Applicant: UNITY BIOTECHNOLOGY, INC.

Inventor： Ryan Hudson ,  Anne-Marie Beausoleil ,  F. Anthony Romero ,  Remi-Martin Laberge

IPC: C07K7/06 ,  A61K38/06 ,  A61P27/02 ,  A61P9/10 ,  A61P19/02 ,  A61P35/00 ,  A61K31/496 ,  A61K31/519 ,  A61K38/05 ,  A61K38/07 ,  C07D201/00 ,  C07D303/32 ,  C07K5/06 ,  C07K5/08 ,  C07K5/083 ,  C07K5/10 ,  C07K5/107 ,  A61K38/00

Abstract: The proteasome inhibitors of this invention include peptide-based compounds with a short linear sequence of amino acids. An oxo or thio group is attached to the N-terminal amino acid. A protein-reactive electrophilic group such as an epoxyketone, an aziridinylketone, or a beta-lactone is attached to the C-terminal amino acid. Upon contact with a proteasome complex in a target cell, the electrophilic group reacts with a functional group in or near a binding pocket or active site of the proteasome, forming a covalent bond and thereby inactivating the proteasome. These and other proteasome inhibitors can be screened for binding affinity and an ability to selectively eliminate senescent cells or cancer cells. Compounds that selectively remove senescent cells can be developed for the treatment of conditions such as osteoarthritis, ophthalmic disease, pulmonary disease, and atherosclerosis.

公开(公告)号：US08912192B2

公开(公告)日：2014-12-16

申请号：US13578323

申请日：2011-02-10

Applicant: Noriyuki Hirasawa ,  Nobuyoshi Kamikido ,  Akihiko Tasaki ,  Shusei Ito

Inventor： Noriyuki Hirasawa ,  Nobuyoshi Kamikido ,  Akihiko Tasaki ,  Shusei Ito

IPC: C07D201/00 ,  A61K31/501 ,  A61K9/20

CPC classification number: A61K31/501 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2095

Abstract: Disclosed is a sustained release preparation which releases a poorly soluble medicinal agent in a pH-independent manner. Also disclosed is a sustained release preparation which is capable of controlling the Cmax of a medicinal agent to an adequate amount and is thus capable of maintaining the level of the medicinal agent in the blood to a level at which medicinal effects can be expected for a long period of time. Specifically disclosed is a sustained release preparation which is characterized by containing a pharmaceutically acceptable salt of 4-bromo-6-[3-(4-chlorophenyl)propoxy]-5-(3-pyridylmethylamino)-3(2H)-pyridazinone, and hypromellose. An organic acid is blended in the sustained release preparation in an amount of less than 1% by mass.

Abstract translation: 公开了一种以pH不依赖的方式释放难溶性药物的缓释制剂。 还公开了一种能够将药剂的Cmax控制在足够量的缓释制剂，因此能够将血液中的药剂的水平维持在长期以来可以期待药效的水平 一段的时间。 具体公开的是持续释放制剂，其特征在于含有4-溴-6- [3-（4-氯苯基）丙氧基] -5-（3-吡啶基甲基氨基）-3（2H） - 哒嗪酮的药用盐， 羟丙甲纤维素 持续释放制剂中的有机酸以小于1质量％的量共混。

公开(公告)号：US08188269B1

公开(公告)日：2012-05-29

申请号：US12119203

申请日：2008-05-12

Applicant: Ananda G. Lugade ,  Kurt D. Hoffacker ,  Adam J. Jenkins ,  Karri L. Michael-Ballard ,  Leonid Patsenker ,  Ewald Terpetschnig ,  Veronica D. Thomason ,  Ralph McDade

Inventor： Ananda G. Lugade ,  Kurt D. Hoffacker ,  Adam J. Jenkins ,  Karri L. Michael-Ballard ,  Leonid Patsenker ,  Ewald Terpetschnig ,  Veronica D. Thomason ,  Ralph McDade

IPC: C07D201/00

CPC classification number: B82Y30/00 ,  C07B2200/11 ,  C07C243/28 ,  C07C303/22 ,  C07C303/32 ,  C07C315/04 ,  C07C319/18 ,  C07C319/22 ,  C07C381/02 ,  C07C2601/04 ,  C07D239/48 ,  C07K1/042 ,  C07K17/00 ,  G01N33/54353 ,  Y10S977/902 ,  C07C309/47 ,  C07C309/88 ,  C07C309/46 ,  C07C317/18 ,  C07C323/65 ,  C07C323/42 ,  C07C309/42

Abstract: The present invention relates to improved covalent coupling of two or more entities such as biomolecules, polymer compositions, organic/inorganic molecules/materials, and the like, including their combinations, through one or more novel reactive groups attached to linker groups of 2-1000 atoms length. The present invention also contemplates the use of bifunctional bridge molecules to link two or more entities, wherein the functional groups of the bridge molecules are the novel reactive groups of the present invention.

Abstract translation: 本发明涉及两个或多个实体如生物分子，聚合物组合物，有机/无机分子/材料等的改进的共价偶联，包括其组合，通过连接到2-1000的连接基团上的一个或多个新的反应性基团 原子长度。 本发明还考虑使用双官能桥分子连接两个或多个实体，其中桥分子的官能团是本发明的新的反应性基团。

公开(公告)号：US07385053B2

公开(公告)日：2008-06-10

申请号：US11621209

申请日：2007-01-09

Applicant: Ananda G. Lugade ,  Kurt D. Hoffacker ,  Adam J. Jenkins ,  Karri L. Michael-Ballard ,  Leonid Patsenker ,  Ewald Terpetschnig ,  Veronica D. Thomason ,  Ralph McDade

Inventor： Ananda G. Lugade ,  Kurt D. Hoffacker ,  Adam J. Jenkins ,  Karri L. Michael-Ballard ,  Leonid Patsenker ,  Ewald Terpetschnig ,  Veronica D. Thomason ,  Ralph McDade

IPC: C07D345/00 ,  C07D201/00 ,  C07D255/00 ,  C07H21/00 ,  C12Q1/68

CPC classification number: B82Y30/00 ,  C07B2200/11 ,  C07C243/28 ,  C07C303/22 ,  C07C303/32 ,  C07C315/04 ,  C07C319/18 ,  C07C319/22 ,  C07C381/02 ,  C07C2601/04 ,  C07D239/48 ,  C07K1/042 ,  C07K17/00 ,  G01N33/54353 ,  Y10S977/902 ,  C07C309/47 ,  C07C309/88 ,  C07C309/46 ,  C07C317/18 ,  C07C323/65 ,  C07C323/42 ,  C07C309/42

Abstract: The present invention relates to improved covalent coupling of two or more entities such as biomolecules, polymer compositions, organic/inorganic molecules/materials, and the like, including their combinations, through one or more novel reactive groups attached to linker groups of 2-1000 atoms length. The present invention also contemplates the use of bifunctional bridge molecules to link two or more entities, wherein the functional groups of the bridge molecules are the novel reactive groups of the present invention.

Abstract translation: 本发明涉及两个或多个实体如生物分子，聚合物组合物，有机/无机分子/材料等的改进的共价偶联，包括其组合，通过连接到2-1000的连接基团上的一个或多个新的反应性基团 原子长度。 本发明还考虑使用双官能桥分子连接两个或多个实体，其中桥分子的官能团是本发明的新的反应性基团。

公开(公告)号：US07241883B2

公开(公告)日：2007-07-10

申请号：US10293260

申请日：2002-11-14

Applicant: Ananda G. Lugade ,  Kurt D. Hoffacker ,  Adam J. Jenkins ,  Karri L. Michael-Ballard ,  Leonid Patsenker ,  Ewald Terpetschnig ,  Veronica D. Thomason ,  Ralph McDade

Inventor： Ananda G. Lugade ,  Kurt D. Hoffacker ,  Adam J. Jenkins ,  Karri L. Michael-Ballard ,  Leonid Patsenker ,  Ewald Terpetschnig ,  Veronica D. Thomason ,  Ralph McDade

IPC: C07D345/00 ,  C07D201/00 ,  C07C255/00 ,  C07H21/00 ,  C12Q1/68

CPC classification number: B82Y30/00 ,  C07B2200/11 ,  C07C243/28 ,  C07C303/22 ,  C07C303/32 ,  C07C315/04 ,  C07C319/18 ,  C07C319/22 ,  C07C381/02 ,  C07C2601/04 ,  C07D239/48 ,  C07K1/042 ,  C07K17/00 ,  G01N33/54353 ,  Y10S977/902 ,  C07C309/47 ,  C07C309/88 ,  C07C309/46 ,  C07C317/18 ,  C07C323/65 ,  C07C323/42 ,  C07C309/42

Abstract: The present invention relates to improved covalent coupling of two or more entities such as biomolecules, polymer compositions, organic/inorganic molecules/materials, and the like, including their combinations, through one or more novel reactive groups attached to linker groups of 2–1000 atoms length. The present invention also contemplates the use of bifunctional bridge molecules to link two or more entities, wherein the functional groups of the bridge molecules are the novel reactive groups of the present invention.

Abstract translation: 本发明涉及两个或多个实体如生物分子，聚合物组合物，有机/无机分子/材料等的改进的共价偶联，包括其组合，通过连接到2-1000的连接基团上的一个或多个新的反应性基团 原子长度。 本发明还考虑使用双官能桥分子连接两个或多个实体，其中桥分子的官能团是本发明的新的反应性基团。

公开(公告)号：US20050090539A1

公开(公告)日：2005-04-28

申请号：US10716012

申请日：2003-11-18

Applicant: Truc Vu ,  David Brzozowski ,  Rita Fox ,  Jollie Godfrey ,  Ronald Hanson ,  Sergei Kolotuchin ,  John Mazzullo ,  Ramesh Patel ,  Jianji Wang ,  Kwok Wong ,  Jurong Yu ,  Jason Zhu ,  David Magnin ,  David Augeri ,  Lawrence Hamann

Inventor： Truc Vu ,  David Brzozowski ,  Rita Fox ,  Jollie Godfrey ,  Ronald Hanson ,  Sergei Kolotuchin ,  John Mazzullo ,  Ramesh Patel ,  Jianji Wang ,  Kwok Wong ,  Jurong Yu ,  Jason Zhu ,  David Magnin ,  David Augeri ,  Lawrence Hamann

IPC: A61K31/403 ,  A61K31/435 ,  C07C62/06 ,  C07C69/00 ,  C07C69/716 ,  C07C229/28 ,  C07C271/22 ,  C07D20060101 ,  C07D201/00 ,  C07D207/22 ,  C07D207/277 ,  C07D209/02 ,  C07D209/52 ,  C07D221/02

CPC classification number: C07C69/757 ,  C07C62/06 ,  C07C69/635 ,  C07C69/675 ,  C07C229/28 ,  C07C271/22 ,  C07C2603/74 ,  C07D207/22 ,  C07D209/52

Abstract: Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.

Abstract translation: 提供了用于制备二肽基肽酶IV的环丙基稠合吡咯烷基抑制剂的方法和化合物。

公开(公告)号：US20050075465A1

公开(公告)日：2005-04-07

申请号：US10497297

申请日：2002-11-21

Applicant: Thomas Bolle ,  Andreas Valet ,  David Leppard ,  Stephen Andrews ,  Ramanathan Ravichandran ,  Markus Grob ,  Dirk Simon

Inventor： Thomas Bolle ,  Andreas Valet ,  David Leppard ,  Stephen Andrews ,  Ramanathan Ravichandran ,  Markus Grob ,  Dirk Simon

IPC: C07D251/24 ,  C08F8/30 ,  C08F291/00 ,  C08K5/3492 ,  C08L101/00 ,  C07D201/00 ,  C08F20/00 ,  C09K3/00

CPC classification number: C08F8/30 ,  C07D251/24 ,  C08F291/00 ,  C08K5/3492 ,  C08F222/1006

Abstract: Compounds of the general formula I′ in which R1 is H, C1-C12alkyl; C5-C12cycloalkyl; C2-C18alkyl which is interrupted by one or more O; SR4; OR5; or is a group of formula II or III R2, R21 and R3 independently of one another, are H or —Y-T as defined in claim 1, where T is a reactive group selected from OH, acryl- and methacryloxy and arylcarbonate groups, and further symbols are as defined in claim 1, are effective as crosslinking agents for polymeric networks, especially as in flexographic printing plates, coatings, and plastic containers or films. Further provided is a method of protecting the content of a clear or lightly colored plastic container or film against the deleterious effects of ultraviolet radiation, which method comprises permanently and covalently bonding one or more UV absorbing moieties of a durable s-triazine UV absorber via condensation to a suitable polymer component.

Abstract translation: 通式I'的化合物，其中R 1是H，C 1 -C 12烷基; C5-C12环烷基; 被一个或多个O中断的C 2 -C 18烷基; SR4; OR5; 或者是式II或III中的R 2，R 21和R 3彼此独立的基团是如权利要求1所定义的H或-YT，其中T是选自OH，丙烯酰基和甲基丙烯酰氧基和芳基碳酸酯基的反应性基团， 符号如权利要求1中所定义，可用作聚合物网络的交联剂，特别是在柔性版印刷版，涂料和塑料容器或薄膜中。 进一步提供了一种保护透明或浅色塑料容器或薄膜的含量以抵抗紫外线辐射的有害影响的方法，该方法包括通过冷凝物永久地和共价键合耐久的三嗪UV吸收剂的一个或多个UV吸收部分 到合适的聚合物组分。