公开(公告)号：US20190247513A1

公开(公告)日：2019-08-15

申请号：US16312569

申请日：2017-06-27

申请人： Tagworks Pharmaceuticals B.V.

发明人： Marc Stefan ROBILLARD ,  Wolter TEN HOEVE ,  Freek Johannes Maria HOEBEN ,  Ronny Mathieu VERSTEEGEN ,  Hendricus Marie JANSSEN ,  Arthur Henry Antoon Marie VAN ONZEN ,  Raffaella ROSSIN

IPC分类号： A61K47/68 ,  C07D257/08 ,  A61K47/60 ,  A61K47/64

CPC分类号： A61K47/6889 ,  A61K47/555 ,  A61K47/60 ,  A61K47/6415 ,  A61K47/66 ,  A61K47/6817 ,  A61K47/6897 ,  A61K2039/505 ,  C07D257/08 ,  C07K16/30 ,  C07K16/3046 ,  C07K2317/626 ,  C07K2317/94

摘要： Disclosed is an advancement in provoked chemical cleavage. Thereby the invention provides the use of a diene as a chemically cleavable group attached to a Construct, and the use of a dienophile to provoke the release of the Construct by allowing the diene to react with a dienophile capable of undergoing an inverse electron demand Diels Alder reaction with the diene. The invention includes a kit for releasing a Construct CA bound to a Trigger TR, the kit comprising a tetrazine and a dienophile, wherein the Trigger is the tetrazine. The invention also includes the use of the formation of a pyridazine by reacting a tetrazine comprising a Construct CA bound thereto and a dienophile, as a chemical tool for the release, in a chemical, biological or physiological environment, of said Construct.

公开(公告)号：US20190127394A1

公开(公告)日：2019-05-02

申请号：US16017638

申请日：2018-06-25

申请人： The General Hospital Corporation

发明人： Ralph Mazitschek ,  Alexandra M. Courtis ,  James Adam Hendricks

IPC分类号： C07F5/02 ,  C07D257/08 ,  A61K51/04 ,  G01N33/534

CPC分类号： C07F5/02 ,  A61K51/0446 ,  C07D257/08 ,  C07F5/025 ,  G01N33/534

摘要： This invention relates to water-soluble mono-alkoxy and mono-alkyne BODIPY derivatives, including methods for making the same. For examples, provided herein are compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: is a BODIPY ligand system; X is a halogen; L is absent or a linker; and Z is selected from the group consisting of: a group reactive with a biologically active molecule and a detectable agent.

公开(公告)号：US20180258256A1

公开(公告)日：2018-09-13

申请号：US15917236

申请日：2018-03-09

申请人： ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA

发明人： Douglas A. Loy ,  Robb E. Bagge ,  Wenmo Sun

IPC分类号： C08K5/3477 ,  C07D257/08 ,  C08K5/00 ,  C07D231/10 ,  C08L25/06 ,  C08L23/06 ,  C08L23/12 ,  C08L57/00

CPC分类号： C08K5/3477 ,  C07C7/00 ,  C07D231/10 ,  C07D257/08 ,  C08J2300/22 ,  C08J2300/24 ,  C08J2300/26 ,  C08K5/005 ,  C08L23/06 ,  C08L23/12 ,  C08L25/06 ,  C08L57/00 ,  C08L2201/08 ,  C09D5/086 ,  C09D7/48 ,  C07C15/44

摘要： Hydrotetrazine compounds having antioxidant properties and uses thereof are described herein. These compounds may be dihydrotetrazines, tetrahydrotetrazines, or hexahydrotetrazines that can be utilized as antioxidants for use in thermoplastics, thermosets and elastomers; free radical inhibitors to stabilize reactive chemicals, such as monomers against free radical polymerizations; and as anticorrosion agents in coatings to protect against metal oxidation. The hydrogenated tetrazines can donate hydrogen atom equivalents to terminate radical chain reactions. These compounds can change colors to signal when oxidation has occurred, and can be further recycled by reduction reactions.

公开(公告)号：US09902705B2

公开(公告)日：2018-02-27

申请号：US14437905

申请日：2013-03-14

申请人： The General Hospital Corporation

发明人： Scott A. Hilderbrand ,  Neal K. Devaraj ,  Ralph Weissleder ,  Mark R. Karver

IPC分类号： C07D257/08 ,  C07D403/12 ,  C07D401/04 ,  A61K31/4015

CPC分类号： C07D257/08 ,  C07D401/04 ,  C07D403/12

摘要： The present application relates to functionalized 1,2,4,5-tetrazine compounds. The compounds are useful in compositions and methods using bioorthogonal inverse electron demand Diels-Alder cycloaddition reactions for the rapid and specific covalent delivery of a “payload” to a ligand bound to a biological target.

公开(公告)号：US09764038B2

公开(公告)日：2017-09-19

申请号：US14367840

申请日：2012-12-21

申请人： Innate Pharma ,  Paul Scherrer Institut

发明人： Patrick Dennler ,  Delphine Bregeon ,  Laurent Gauthier ,  François Romagné ,  Christian Belmant ,  Eliane Fischer ,  Roger Schibli

IPC分类号： A61K47/48 ,  C07K16/18 ,  C07K16/22 ,  C07K16/28 ,  C07K16/30 ,  C07K16/00 ,  C07K19/00 ,  C07C217/08 ,  C07C223/02 ,  C07C229/26 ,  C07C233/62 ,  C07C247/04 ,  C07C323/12 ,  C07C323/60 ,  C07D225/08 ,  C07D257/08 ,  C07D277/06 ,  C07F9/50 ,  C12N9/10 ,  C12P21/00 ,  G01N33/68

CPC分类号： A61K47/6803 ,  A61K47/60 ,  A61K47/68 ,  A61K47/6807 ,  A61K47/6813 ,  A61K47/6817 ,  A61K47/6865 ,  A61K47/6871 ,  C07C217/08 ,  C07C223/02 ,  C07C229/26 ,  C07C233/62 ,  C07C247/04 ,  C07C323/12 ,  C07C323/60 ,  C07D225/08 ,  C07D257/08 ,  C07D277/06 ,  C07F9/5022 ,  C07K16/00 ,  C07K19/00 ,  C07K2317/40 ,  C12N9/1044 ,  C12P21/005 ,  G01N33/6854

摘要： The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs. Also disclosed herein are linking reagents, functionalized antibodies, pharmaceutical compositions, and method of treating disease and/or conditions.

公开(公告)号：US09359400B2

公开(公告)日：2016-06-07

申请号：US14329758

申请日：2014-07-11

申请人： Aimee Usera ,  Zachary Robinson ,  Jennifer Cobb

发明人： Aimee Usera ,  Zachary Robinson ,  Jennifer Cobb

IPC分类号： C07K5/103 ,  A61K49/00 ,  A61K47/48 ,  C07K5/083 ,  C07K5/062 ,  C07K1/13 ,  C07D209/42 ,  C07K7/02 ,  C07K5/072 ,  C07C271/22 ,  C07C317/28 ,  A61K38/06 ,  A61K38/05 ,  A61K38/07

CPC分类号： C07K5/101 ,  A61K38/00 ,  A61K38/05 ,  A61K38/06 ,  A61K38/07 ,  A61K47/6415 ,  A61K49/0002 ,  C07C271/22 ,  C07C317/28 ,  C07C2602/24 ,  C07D209/42 ,  C07D229/02 ,  C07D257/08 ,  C07K1/13 ,  C07K5/06043 ,  C07K5/06104 ,  C07K5/0808 ,  C07K7/02

摘要： The present invention relates to methods and reagents for use in site-selective modification of proteins having lysine residues with functionalized peptides using a chemoenzymatic microbial transglutaminase-mediated reaction. The functionalized proteins may be used for study or therapeutic uses.

摘要翻译： 本发明涉及用于使用化学酶微生物转谷氨酰胺酶介导的反应对具有赖氨酸残基的蛋白质进行位点选择性修饰的功能化肽的方法和试剂。 功能化蛋白质可用于研究或治疗用途。

公开(公告)号：US20140121345A1

公开(公告)日：2014-05-01

申请号：US14123435

申请日：2012-05-31

申请人： Martin Schadt ,  Sayaka Nose ,  Masayuki Iwakubo ,  Masanao Hayashi ,  Yutaka Nagashima ,  Isa Nishiyama ,  Haruyoshi Takatsu

发明人： Martin Schadt ,  Sayaka Nose ,  Masayuki Iwakubo ,  Masanao Hayashi ,  Yutaka Nagashima ,  Isa Nishiyama ,  Haruyoshi Takatsu

IPC分类号： G02B1/04

CPC分类号： G02B1/04 ,  C07C69/732 ,  C07C69/92 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D207/452 ,  C07D257/08 ,  C08F20/40 ,  C08F22/40 ,  C09K19/56 ,  C09K2019/0448 ,  G02F1/133711 ,  G02F1/133788

摘要： Provided is a liquid crystal alignment layer of which a constituent member is a compound represented by the general formula (I).

摘要翻译： 提供一种液晶取向层，其构成成分是由通式（I）表示的化合物。

公开(公告)号：US20100121054A1

公开(公告)日：2010-05-13

申请号：US12596950

申请日：2007-04-24

申请人： Yasushi Shibata ,  Tsutomu Imagawa

发明人： Yasushi Shibata ,  Tsutomu Imagawa

IPC分类号： C07D401/14 ,  C07D213/38

CPC分类号： C07D213/61 ,  C07B43/04 ,  C07C209/06 ,  C07C211/03 ,  C07C211/48 ,  C07C211/62 ,  C07D251/04 ,  C07D257/08 ,  C07D277/20 ,  C07D401/06 ,  C07D401/14 ,  C08G73/0627 ,  C08G73/0644

摘要： The present invention provides a process that enables a substituted methylamine compound which is useful as an intermediate for the production of agricultural chemicals and medicines, to be produced easily, with good yield, and at low cost, and also provides a production intermediate thereof. The process comprises a step of reacting a hexamethylenetetraammonium salt compound represented by a formula (I) with a base to obtain an N-methylidene-substituted methylamine oligomer represented by a formula (II) or a mixture of two or more of the oligomers, and a step of hydrolyzing the N-methylidene-substituted methylamine oligomer represented by formula (II) or the mixture of two or more of the oligomers in the presence of an acid. (wherein A represents an organic group that is either a hydrocarbon group or a heterocyclic group, or said organic group that has a substituent, R represents a hydrogen atom, an organic group that is either a hydrocarbon group or a heterocyclic group, or said organic group that has a substituent, L represents a halogen atom and the like, and n represents an integer of 2 to 20)

摘要翻译： 本发明提供了能够容易地以良好的产率，低成本地制造可用作农药和药品的中间体的取代甲胺化合物的方法，并且还提供其制备中间体。 该方法包括使由式（I）表示的六亚甲基四铵盐化合物与碱反应以获得由式（II）表示的N-亚甲基取代的甲基胺低聚物或两种或更多种低聚物的混合物的步骤，以及 在酸存在下水解由式（II）表示的N-亚甲基取代的甲胺低聚物或两种或更多种低聚物的混合物的步骤。 （其中A表示烃基或杂环基的有机基团或具有取代基的有机基团，R表示氢原子，作为烃基或杂环基的有机基团或所述有机基团 具有取代基的基团，L表示卤素原子等，n表示2〜20的整数）

公开(公告)号：US20090298835A1

公开(公告)日：2009-12-03

申请号：US12503589

申请日：2009-07-15

申请人： Julius Rebek, JR. ,  Shen Gu ,  Shannon Biros

发明人： Julius Rebek, JR. ,  Shen Gu ,  Shannon Biros

IPC分类号： A61K31/501 ,  A61K31/50 ,  C07K1/107 ,  C07D237/06 ,  C07D403/14

CPC分类号： C07D237/24 ,  C07D237/08 ,  C07D257/08 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D413/04

摘要： Functionalized pyridazine derivatives having a low molecular weight and pharmaceutical compositions thereof are useful as alpha-helix mimetics and for treating conditions and/or disorders mediated by alpha-helix-binding receptors and proteins.

摘要翻译： 具有低分子量的官能化哒嗪衍生物及其药物组合物可用作α-螺旋模拟物和用于治疗由α-螺旋结合受体和蛋白质介导的病症和/或病症。

公开(公告)号：US5034388A

公开(公告)日：1991-07-23

申请号：US489521

申请日：1990-03-07

申请人： John M. Clough ,  Christopher R. A. Godfrey

发明人： John M. Clough ,  Christopher R. A. Godfrey

IPC分类号： A01N43/58 ,  A01N43/60 ,  A01N43/66 ,  A01N43/707 ,  A01N43/713 ,  C07D237/14 ,  C07D237/18 ,  C07D237/28 ,  C07D241/18 ,  C07D241/44 ,  C07D251/20 ,  C07D251/22 ,  C07D251/26 ,  C07D251/30 ,  C07D251/38 ,  C07D253/02 ,  C07D253/04 ,  C07D253/06 ,  C07D253/07 ,  C07D253/08 ,  C07D253/10 ,  C07D257/08

CPC分类号： C07D257/08 ,  A01N43/58 ,  A01N43/60 ,  A01N43/66 ,  A01N43/707 ,  A01N43/713 ,  C07D237/14 ,  C07D237/18 ,  C07D237/28 ,  C07D241/18 ,  C07D241/44 ,  C07D251/20 ,  C07D251/22 ,  C07D251/26 ,  C07D253/02 ,  C07D253/07 ,  C07D253/10

摘要： This invention relates to derivatives of acrylic acid of the formula: ##STR1## useful as fungicides, to processes for preparing them, to fungicidal compositions containing them, and to methods of using them to combat fungi, especially fungal infections in plants. The values of the variables are provided herein.