公开(公告)号：US20240115221A1

公开(公告)日：2024-04-11

申请号：US18511588

申请日：2023-11-16

Applicant: The Research Foundation for the State University of New York

Inventor： Peter Tonge ,  Zhuo ZHANG ,  Peter Smith-Jones ,  Li LIU ,  Hui WANG

IPC: A61B6/03 ,  A61K51/04 ,  A61P31/04 ,  C07B59/00 ,  C07C227/12 ,  C07C229/60

CPC classification number: A61B6/037 ,  A61K51/0402 ,  A61P31/04 ,  C07B59/001 ,  C07C227/12 ,  C07C229/60

Abstract: The present invention provides a composition comprising the compound having the structure:




or a salt of the compound; 4-amino-2-[19F]-fluorobenzoic acid or a salt of 4-amino-2-[19F]-fluorobenzoic acid; and at least one acceptable carrier.

公开(公告)号：US11857352B2

公开(公告)日：2024-01-02

申请号：US16330679

申请日：2017-09-06

Applicant: The Research Foundation for the State University of New York

Inventor： Peter Tonge ,  Zhuo Zhang ,  Peter Smith-Jones ,  Li Liu ,  Hui Wang

IPC: C07C229/60 ,  C07C227/12 ,  A61B6/03 ,  C07B59/00 ,  A61K51/04 ,  A61P31/04

CPC classification number: A61B6/037 ,  A61K51/0402 ,  A61P31/04 ,  C07B59/001 ,  C07C227/12 ,  C07C229/60

Abstract: The present invention provides a composition comprising the compound having the structure:




or a salt of the compound; 4-amino-2-[19F]-fluorobenzoic acid or a salt of 4-amino-2-[19F]-fluorobenzoic acid; and at least one acceptable carrier.

公开(公告)号：US20190084942A1

公开(公告)日：2019-03-21

申请号：US16085829

申请日：2017-03-17

Applicant: Purdue Pharma L.P.

Inventor： Laykea Tafesse

IPC: C07D241/04 ,  C07D413/04 ,  C07C227/18 ,  C07C229/60

CPC classification number: C07D241/04 ,  A61K31/495 ,  C07C227/18 ,  C07C229/60 ,  C07C2603/24 ,  C07D261/20 ,  C07D295/135 ,  C07D413/04 ,  Y02A50/414

Abstract: The disclosure provides processes of preparing compounds of Formula (I) and Formula (IV), their salts, and intermediates thereof, wherein R1′ R2′ R3, and R7 are defined as set forth in the specification.

公开(公告)号：US10017459B2

公开(公告)日：2018-07-10

申请号：US15693905

申请日：2017-09-01

Applicant: Quadriga Biosciences, Inc.

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

IPC: A61K31/662 ,  C07C229/42 ,  A61K45/06 ,  A61K31/519 ,  A61K31/365 ,  A61K31/42 ,  A61K31/196 ,  C07F9/48 ,  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

CPC classification number: 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

Abstract: 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：US09896419B2

公开(公告)日：2018-02-20

申请号：US15488205

申请日：2017-04-14

Applicant: Aldeyra Therapeutics, Inc.

Inventor： Thomas A. Jordan ,  John E. Dowling ,  John Clifford Chabala

IPC: A61K31/47 ,  C07D215/38 ,  C07D277/56 ,  C07D277/40 ,  C07C229/60 ,  C07C229/56 ,  A61K31/44 ,  A61K31/4706 ,  A61K31/435 ,  A61K31/426 ,  A61K31/423 ,  A61K31/41 ,  A61K31/4418 ,  C07C215/68

CPC classification number: C07D215/38 ,  A61K31/41 ,  A61K31/423 ,  A61K31/426 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/47 ,  A61K31/4706 ,  C07C215/68 ,  C07C229/56 ,  C07C229/60 ,  C07D277/40 ,  C07D277/56

Abstract: Compositions and methods for treating macular degeneration and other forms of retinal disease whose etiology involves the accumulation of A2E and/or lipofuscin, and, more specifically, for preventing the formation and/or accumulation of A2E are disclosed.

公开(公告)号：US20170362166A1

公开(公告)日：2017-12-21

申请号：US15693905

申请日：2017-09-01

Applicant: Quadriga Biosciences, Inc.

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

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

CPC classification number: 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

Abstract: 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：US09822066B2

公开(公告)日：2017-11-21

申请号：US15336154

申请日：2016-10-27

Applicant: NUFORMIX LIMITED

Inventor： Joanne Holland ,  Christopher Frampton

IPC: C07C233/55 ,  C07D275/06 ,  C07C65/03 ,  C07C275/02 ,  C07C229/56

CPC classification number: C07C233/55 ,  C07B2200/13 ,  C07C65/03 ,  C07C65/05 ,  C07C65/10 ,  C07C229/56 ,  C07C229/60 ,  C07C235/38 ,  C07C275/02 ,  C07D213/82 ,  C07D275/06

Abstract: New tranilast complexes and new tranilast cocrystals are disclosed. These include a 1:1 tranilast nicotinamide complex, a 1:1 tranilast nicotinamide cocrystal, a 1:1 tranilast saccharin complex, a 1:1 tranilast saccharin cocrystal, a 1:1 tranilast gentisic acid complex, a 1:1 tranilast gentisic acid cocrystal, a 1:1 tranilast salicylic acid complex, a 1:1 tranilast salicylic acid cocrystal, a 1:1 tranilast urea complex, a 1:1 tranilast urea cocrystal, a 1:1 tranilast 4-aminobenzoic acid complex, a 1:1 tranilast 4-aminobenzoic acid cocrystal, a 1:1 tranilast 2,4-dihydroxybenzoic acid complex and a 1:1 tranilast 2,4-dihydroxybenzoic acid cocrystal. Also disclosed are pharmaceutical compositions containing a tranilast complex or cocrystal of the invention and a pharmaceutically acceptable carrier. Methods of treatment using the tranilast complexes and cocrystals as well as the pharmaceutical compositions are disclosed.

公开(公告)号：US09751844B2

公开(公告)日：2017-09-05

申请号：US13994339

申请日：2011-12-13

Applicant: Dae-Yoon Chi ,  Byoung-Se Lee ,  Jae-Hak Lee ,  So-Young Chu ,  Woon-Jung Jung ,  Hye-Rim Kwon

Inventor： Dae-Yoon Chi ,  Byoung-Se Lee ,  Jae-Hak Lee ,  So-Young Chu ,  Woon-Jung Jung ,  Hye-Rim Kwon

IPC: A61K9/00 ,  C07D249/04 ,  A61K51/04 ,  C07B59/00 ,  C07C229/60 ,  C07D403/12 ,  C07D417/14 ,  C07D487/04 ,  C07H19/06 ,  C08F212/08 ,  C08F212/14 ,  C08F8/02 ,  C08F8/30 ,  C08F8/34 ,  C08F8/44 ,  C08F12/26 ,  C08F12/30 ,  C08F212/32

CPC classification number: C07D249/04 ,  A61K51/04 ,  A61K51/0406 ,  A61K51/0453 ,  A61K51/0455 ,  A61K51/0465 ,  A61K51/047 ,  A61K51/0491 ,  C07B59/00 ,  C07C229/60 ,  C07D403/12 ,  C07D417/14 ,  C07D487/04 ,  C07H19/06 ,  C08F8/02 ,  C08F8/30 ,  C08F8/34 ,  C08F8/44 ,  C08F12/26 ,  C08F12/30 ,  C08F212/08 ,  C08F212/14 ,  C08F212/32 ,  C08F12/18 ,  C08F12/22 ,  C08F212/36

Abstract: The present invention relates to a solid precursor in the form of an organic salt, the solid precursor having a solid support, a method for manufacturing same, and an application thereof. The solid precursor of the present invention enables omission of the [18F]fluoride refining process using additional cartridge, and the use of excessive phase-transfer catalyst, and can easily remove remaining substance after reaction through the solid support inside the precursor. The solid precursor of the present invention is very appropriate for an automated synthesis device as an all-in-one system that can carry out overall process of [18F]fluorosis reaction, when used by charging in a cartridge.

公开(公告)号：US20170247342A1

公开(公告)日：2017-08-31

申请号：US15593531

申请日：2017-05-12

Applicant: SANTEN PHARMACEUTICAL CO., LTD.

Inventor： Kazuhiro KUDOU ,  Masato NAGATSUKA

IPC: C07D241/44 ,  C07C229/60 ,  C07C227/18

CPC classification number: C07D241/44 ,  C07C227/18 ,  C07C229/60 ,  Y02P20/55

Abstract: An object is to provide a novel production method suitable for industrial production of a 3,3-dimethyl-3,4-dihydro-1H-quinoxalin-2-one derivative and a synthetic intermediate for the method. Provided is a method for producing a compound represented by formula (1): wherein R1 represents a hydrogen atom, an optionally substituted alkyl group, an optionally substituted cycloalkyl group, or an optionally substituted aryl group, R2 represents a hydrogen atom, an optionally substituted alkyl group, a hydroxy group, or a nitrogen atom-protecting group, R3 represents a hydrogen atom, an optionally substituted alkyl group, a hydroxy group, or a nitrogen atom-protecting group, and X represents a hydroxy group or a leaving group, or a salt thereof, the method comprising the steps of: reacting a compound represented by formula (2): wherein R1, R2, and X are the same as defined in formula (1), R4 represents an optionally substituted alkyl group, an optionally substituted cycloalkyl group, or an optionally substituted aryl group, or a salt thereof with a nitrating agent to obtain a compound represented by formula (3): wherein R1, R2, R4, and X are the same as defined in formulae (1) and (2), or a salt thereof, and reducing the compound represented by formula (3) or the salt thereof to obtain the compound represented by formula (1) or the salt thereof.

公开(公告)号：US20170173569A1

公开(公告)日：2017-06-22

申请号：US15379986

申请日：2016-12-15

Applicant: Bruce H. Lipshutz ,  Sachin Handa

Inventor： Bruce H. Lipshutz ,  Sachin Handa

IPC: B01J23/89 ,  C07B31/00 ,  B01J37/00 ,  B01J23/745 ,  B01J35/00

CPC classification number: B01J23/8906 ,  B01J23/72 ,  B01J23/745 ,  B01J23/755 ,  B01J31/0202 ,  B01J31/0209 ,  B01J31/0225 ,  B01J31/04 ,  B01J31/068 ,  B01J31/2404 ,  B01J35/0013 ,  B01J37/009 ,  B01J37/16 ,  B01J2231/327 ,  B01J2231/4211 ,  B01J2231/4266 ,  B01J2231/64 ,  B01J2531/824 ,  B01J2531/842 ,  B01J2531/96 ,  C07B31/00 ,  C07B37/04 ,  C07C209/325 ,  C07C213/02 ,  C07C221/00 ,  C07C227/04 ,  C07C231/12 ,  C07C253/30 ,  C07C319/20 ,  C07C2601/14 ,  C07D209/12 ,  C07D211/90 ,  C07D213/30 ,  C07D213/61 ,  C07D215/40 ,  C07D235/18 ,  C07D249/04 ,  C07D249/06 ,  C07D277/48 ,  C07D295/192 ,  C07D401/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/12 ,  C07D471/04 ,  C07J41/0055 ,  C07C211/52 ,  C07C229/60 ,  C07C233/55 ,  C07C217/84 ,  C07C211/58 ,  C07C217/86 ,  C07C215/76 ,  C07C211/45 ,  C07C237/30 ,  C07C237/36 ,  C07C215/70 ,  C07C217/60 ,  C07C229/42 ,  C07C229/08 ,  C07C255/58 ,  C07C255/59 ,  C07C223/06 ,  C07C225/22 ,  C07C323/36

Abstract: In one embodiment, the application discloses a composition for the reduction of an organic compound comprising a nitro group to form an organic compound comprising an amine group, the composition comprising: a) a transition metal salt; b) an iron salt; and c) a reducing agent; and methods for the use of such compositions, including Click chemistry and cross coupling reactions.