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公开(公告)号：US20220202837A1
公开(公告)日：2022-06-30
申请号：US17672508
申请日：2022-02-15
Applicant: The Regents of the University of California
Inventor： Carolyn Ruth Bertozzi , Nicholas J. Agard , Jennifer A. Prescher , Jeremy Michael Baskin , Ellen May Sletten
IPC: A61K31/655 , C07C45/29 , C07C45/51 , C07C45/63 , C07C49/457 , C07C49/753 , C07C59/72 , C07C63/66 , C07C69/708 , C07C69/76 , C07D207/416 , C07D207/452 , C07D249/16 , C07D495/04 , G01N33/531 , G01N33/68 , C07C63/74 , C07C57/26
Abstract: The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).
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公开(公告)号：US11046666B2
公开(公告)日：2021-06-29
申请号：US16569840
申请日：2019-09-13
Applicant: CORSAIR PHARMA, INC.
Inventor： Cyrus K. Becker , Meenakshi S. Venkatraman , Xiaoming Zhang
IPC: C07D321/00 , C07D453/02 , C07D257/06 , C07C59/72 , C07C235/20 , A61K31/165 , C07C69/734 , A61K31/216 , A61K31/365 , C07D307/20 , A61K31/341 , A61K45/06 , A61K9/00 , C07D317/34 , C07C69/712 , C07D317/40 , C07C219/16 , C07D263/24 , C07D263/26 , C07D265/30 , C07D207/08 , C07D295/088 , C07D211/60 , C07D295/145 , C07C69/74 , C07C69/96 , A61K9/70
Abstract: Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.
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公开(公告)号：US10995051B2
公开(公告)日：2021-05-04
申请号：US16731705
申请日：2019-12-31
Applicant: L'OREAL
Inventor： Maria Dalko , Xavier Marat , Julien Hitce , Chao-Jun Li
IPC: C07C45/69 , C07C59/11 , C07C51/38 , C07C69/675 , C07C45/54 , C07C67/347 , C07C69/757 , C07C69/732 , C07C69/734 , C07D213/30 , A61K8/365 , A61Q17/00 , A61Q19/00 , C07C51/09 , C07C59/54 , C07C59/56 , C07C59/72
Abstract: The present invention relates to compounds of formula (I): in which R1 is a hydrogen atom, a phenyl radical, or a straight or branched, saturated or unsaturated hydrocarbon radical having 1 to 8 carbon atoms.
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公开(公告)号：US10669226B2
公开(公告)日：2020-06-02
申请号：US16321024
申请日：2017-08-02
Applicant: SEED CO., LTD.
Inventor： Yoshiko Yamazaki
IPC: C07C69/54 , C07C229/34 , C07C57/50 , C07C59/72
Abstract: It is an objective of the present invention to provide a novel polymerizable triptycene derivative that has a structure in which three benzene rings arranged at the axis formed by barrelene of the triptycene skeleton can rotate evenly and that has hydrophilicity imparted to it as compared to any of the prior art triptycene derivatives and is thus highly useful in functional materials.The above objective is achieved by the polymerizable triptycene derivative having substituents with an unsaturated bonding functional group at position 9 and/or position 10 of the triptycene skeleton, the polymerizable triptycene derivative having two carboxyl groups and the polymerizable triptycene derivative having one carboxyl group and one amino group.
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公开(公告)号：US20200095184A1
公开(公告)日：2020-03-26
申请号：US16495013
申请日：2018-03-16
Applicant: University of South Alabama
Inventor： Gary Piazza , Xi Chen , Herbert Weissbach , Shailaja Kesraju Allani
Abstract: The disclosure provides chemical compounds possessing therapeutic and/or protective properties against oxidative damage. Methods of making such therapeutic and/or protective compounds and associated compositions are also provided, as are methods for their use, which include protecting cells from oxidative damage and/or inhibiting production of ROS in a cell or subject, as well as preventing or reducing the extent of tissue damage caused by an ischemic event in a subject at elevated risk of such an event.
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公开(公告)号：US10556851B2
公开(公告)日：2020-02-11
申请号：US16071967
申请日：2017-01-25
Applicant: Emcure Pharmaceuticals Limited
IPC: C07C51/08 , C07C37/00 , C07C45/64 , C07C253/00 , C07C253/30 , C07B51/00 , C07C39/17 , C07C47/575 , C07C59/72 , C07C255/13
Abstract: The invention relates to improved method of synthesis for Treprostinil comprising condensation reaction of the carbonyl compound having allyl, alkyl, crotyl or MEM-protected phenolic hydroxyl group, compound (4) with a hydroxyl-protected alkynol (5) to give the condensation product, compound (6). Subjecting compound (6) to oxidation, reduction, hydroxyl protection and carbonylation, cyclization reactions gave the tricyclic derivative (10). Further reactions comprising reduction, hydrogenation and deprotection of the phenolic and side-chain hydroxyl groups, wherein the sequence and choice of reagents was governed by protecting groups, gave the triol intermediate, compound (14). Cyanoalkylation at phenolic hydroxyl functionality and further hydrolysis yielded the prostacyclin compound, Treprostinil (1) and its pharmaceutically acceptable salts, having desired purity.
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公开(公告)号：US20190248725A1
公开(公告)日：2019-08-15
申请号：US16397139
申请日：2019-04-29
Inventor： Imre JUHÁSZ , Irén HORTOBÁGYI , Tamás ALTSACH , István LÁSZLÓFI , Ágnes NAGYNÉ BORKÓ , Imre ROZSUMBERSZKI , Gábor HAVASI , Zsuzsanna KARDOS , Péter BUZDER-LANTOS
IPC: C07C51/347 , C07C59/72 , C07C67/14 , C07C13/547 , C07C35/37 , C07C51/41 , C07C51/09 , C07C45/65 , C07C45/30 , C07C41/26 , C07C43/315 , C07C41/48 , C07C41/30 , C07C69/76 , C07C67/293 , C07C67/29
CPC classification number: C07C51/347 , C07C13/547 , C07C35/37 , C07C41/26 , C07C41/30 , C07C41/48 , C07C43/315 , C07C45/30 , C07C45/305 , C07C45/65 , C07C51/09 , C07C51/412 , C07C59/72 , C07C67/14 , C07C67/29 , C07C67/293 , C07C69/76 , C07C2603/14 , C07C49/84 , C07C49/755 , C07C59/70
Abstract: Treprostinil is a synthetic prostacyclin derivative with thrombocyte aggregation inhibitory and vasodilatory activity. Treprostinil can be administered in subcutaneous, intravenous, inhalable, or oral forms. Disclosed is a method for the preparation of treprostinil of formula I and its amorphous form, anhydrate form, monohydrate form, and polyhydrate form salts with bases. In the disclosed method, the chiral center in the 3-hydroxyoctyl substituent is formed at the end of the synthesis, so that the method is robust and well scalable. Also disclosed are treprostinil intermediates and the preparation of the intermediates.
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公开(公告)号：US10329232B2
公开(公告)日：2019-06-25
申请号：US14391651
申请日：2013-03-28
Applicant: UNIVERSITE LIBRE DE BRUXELLES (ULB) , CENTER NATIONAL DE LA RECHERCHE SCIENTIFIQUE—CNRS , UNIVERSITE DE RENNES 1 , UNIVERSITE PARIS DESCARTES
Inventor： Ivan Jabin , Alice Mattiuzzi , Corlnne Lagrost , Philippe Hapiot , Olivia Reinaud
IPC: C08J7/04 , C07C43/21 , C07C59/72 , C07C205/37 , C07C217/94 , C07C245/20 , C07C43/225 , C07C69/736 , C07D333/50
Abstract: A calixarene directly grafted onto the surface of a material, a related grafting process, and certain calixarene intermediates useful for carrying out the grafting process.
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公开(公告)号：US10087156B2
公开(公告)日：2018-10-02
申请号：US15435125
申请日：2017-02-16
Inventor： Xiao-kun Zhang , Ying Su , Hu Zhou , Wen Liu , Pei-Qiang Huang
IPC: C07D295/112 , A61K38/19 , C07C57/62 , C07C59/72 , C07C255/57 , C07D213/55 , G01N33/50
Abstract: Provided herein are methods and compositions related to a retinoid receptor-selective pathway. As described herein, this pathway can be targeted to manipulate a tumor microenviroment. For example, the methods and compositions described herein can be used to induce apoptosis in a cancer cell. Further, the compositions described herein, including Sulindac and analogs thereof, can be used to target this pathway for the treatment or prevention of cancer in human patients.
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公开(公告)号：US10023519B2
公开(公告)日：2018-07-17
申请号：US15509225
申请日：2015-09-08
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Yan Shi , Ying Wang , Peter T. W. Cheng , Shung C. Wu
IPC: C07C59/72 , C07C59/90 , C07D309/12 , C07D237/14 , C07D213/68 , C07D307/79 , C07D213/65 , C07D271/06 , C07D213/70 , C07D213/64 , C07D277/24 , A61K45/06 , A61K31/192 , A61K31/4418 , A61K31/4245 , A61K31/426 , A61K31/343 , A61K31/50 , A61K31/351
Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.
