公开(公告)号：US20210363098A1

公开(公告)日：2021-11-25

申请号：US17325291

申请日：2021-05-20

Applicant: University of Georgia Research Foundation, Inc.

Inventor： David Crich ,  Asiri Hettikankanamalage ,  Jarvis Hill

IPC: C07C239/20 ,  C07B43/04 ,  C07D211/94 ,  C07D215/58 ,  C07D265/30 ,  C07D217/08 ,  C07D209/08 ,  C07D471/08 ,  C07H1/00 ,  C07C247/04 ,  C07D241/04 ,  C07D213/74 ,  C07D207/46 ,  C07H17/02 ,  C07H17/00 ,  C07D275/04

Abstract: In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.

公开(公告)号：US20210292275A1

公开(公告)日：2021-09-23

申请号：US16336844

申请日：2017-11-02

Applicant: VYSOKA SKOLA CHEMICKO-TECHNOLOGICKA V PRAZE ,  VYZKUMNY USTAV VETERINARNIHO LEKARSTVI, V.V.I. ,  APIGENEX S.R.O.

Inventor： Mirolav LEDVINA ,  Roman EFFENBERG ,  Jaroslav TURANEK ,  Elissa BARTHELDYOVA ,  Ladislav DROZ ,  Josef MASEK ,  Frantisek HUBATKA

IPC: C07C239/20 ,  A61K9/127 ,  A61K47/69 ,  A61K47/68 ,  A61K47/54 ,  A61K47/61

Abstract: New aminooxylipids of general formula I, wherein n1=5-30 and X is polymethylene linker of the general formula II where n2=2-10, or X is polyethylene glycol linker of the general formula III, wherein n3=1-14 are provided. A method of preparation of the aminooxylipids of general formula I characterized in that the acylation of N-tert-butoxycarbonyl-polymethylenediamine {(CH3)3C—O—(C═O)—HN—(CH2)n—NH2, n=2-13}, or N-tert-butoxycarbonyl-polyethyleglycoldiamine {(CH3)3C—O—(C═O)—HN—(CH2)2—[O—(CH2)]n—O—(CH2)2NH2, n=1-14} with in position C(2) symmetrically branched fatty acids of general formula IV, wherein n1=5-30, in the presence of condensation reagent, or from acid of general formula IV derived acylchloride of general formula V wherein n1=5-30, produces N-Boc-aminolipids of general formula VI, wherein n1=5-30 a X is polymethylene linker of the general formula II or X is polyethylene glycol linker of the general formula III.

公开(公告)号：US10919863B2

公开(公告)日：2021-02-16

申请号：US16319957

申请日：2017-07-28

Applicant: Vectus Biosystems Limited

Inventor： Karen Annette Duggan

IPC: C07D239/26 ,  A61P11/00 ,  C07C39/15 ,  C07C215/54 ,  C07C233/11 ,  C07D207/408 ,  C07D213/56 ,  C07D237/08 ,  C07D261/14 ,  C07D263/44 ,  C07D277/30 ,  C07D401/10 ,  C07D403/10 ,  C07D333/24 ,  C07C233/07 ,  C07D231/56 ,  C07D235/26 ,  C07D235/06 ,  C07C59/52 ,  C07C275/42 ,  C07D213/73 ,  C07D277/68 ,  A61P11/06 ,  C07D231/12 ,  C07C211/29 ,  C07D207/38 ,  C07C255/00 ,  C07C271/28 ,  C07C217/48 ,  C07C261/04 ,  C07D241/12 ,  C07D309/10 ,  C07D233/78 ,  C07D261/08 ,  C07D209/48 ,  C07C237/20 ,  C07D207/327 ,  C07C237/22 ,  C07D307/54 ,  C07D249/18 ,  C07D209/34 ,  C07D263/38 ,  C07C307/10 ,  C07D207/26 ,  C07D207/444 ,  C07C235/34 ,  C07C311/03 ,  C07C311/08 ,  C07C239/20 ,  C07C235/78 ,  C07D209/18 ,  C07D263/58 ,  C07D215/14 ,  C07D207/40 ,  A61K45/06

Abstract: The present invention relates to compounds and their use in the prophylactic and/or therapeutic treatment of pulmonary fibrosis and/or related conditions.

公开(公告)号：US20180297935A1

公开(公告)日：2018-10-18

申请号：US15986059

申请日：2018-05-22

Applicant: Quadriga Biosciences, Inc.

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

IPC: C07C229/42 ,  A61K31/196 ,  A61K31/197 ,  A61K31/245 ,  A61K31/255 ,  A61K31/27 ,  A61K31/336 ,  A61K31/365 ,  A61K31/42 ,  A61K31/519 ,  A61K31/662 ,  A61K45/06 ,  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 ,  A61K31/137 ,  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：US20180230080A1

公开(公告)日：2018-08-16

申请号：US15920654

申请日：2018-03-14

Applicant: Purdue Research Foundation

Inventor： Mingji Dai ,  Val J. Watts ,  Zhishi Ye

IPC: C07C211/28 ,  C07D209/14 ,  C07C229/34 ,  C07C229/38 ,  C07C211/30 ,  C07C217/62 ,  C07C211/45 ,  C07D295/03 ,  C07C211/27 ,  C07C215/34 ,  C07D471/04 ,  C07C239/20 ,  C07C211/55 ,  C07C311/16 ,  C07D223/16 ,  C07C229/14 ,  C07C233/05

CPC classification number: C07C211/28 ,  C07C211/27 ,  C07C211/30 ,  C07C211/45 ,  C07C211/55 ,  C07C215/34 ,  C07C217/62 ,  C07C229/14 ,  C07C229/34 ,  C07C229/38 ,  C07C233/05 ,  C07C239/20 ,  C07C311/16 ,  C07D209/14 ,  C07D223/16 ,  C07D295/03 ,  C07D471/04

Abstract: The invention generally relates to adenylyl cyclase inhibitor compounds and methods for treating neuropathic or inflammatory pain by using those compounds.

公开(公告)号：US09227974B2

公开(公告)日：2016-01-05

申请号：US14399181

申请日：2013-05-14

Applicant: Mahesh Kandula

Inventor： Mahesh Kandula

IPC: C07D473/04 ,  C07C229/40 ,  C07C237/40 ,  C07D339/04 ,  C07D213/66 ,  C07C237/20 ,  A61K47/48 ,  C07C275/40 ,  C07C239/20

CPC classification number: C07D473/04 ,  A61K47/48038 ,  A61K47/481 ,  A61K47/48107 ,  A61K47/542 ,  A61K47/55 ,  A61K47/551 ,  C07C229/40 ,  C07C237/20 ,  C07C237/40 ,  C07C239/20 ,  C07C275/40 ,  C07C2601/14 ,  C07D213/66 ,  C07D339/04

Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of respiratory disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of viscid or excessive mucus, cough, inflammation, redness in sore throat, infection in the throat, sore throat, abnormal mucus secretion, impaired mucus transport, allergic rhinitis, asthma, COPD, respiratory muscular disorders and pain in acute sore throat.

Abstract translation: 本发明涉及式I化合物或其药学上可接受的盐，以及其多晶型物，溶剂合物，对映体，立体异构体和水合物。 包含有效量的式I化合物和用于治疗呼吸系统疾病的方法的药物组合物可以配制用于口服，口腔，直肠，局部，透皮，经粘膜，静脉内，肠胃外给药，糖浆或注射。 这些组合物可用于治疗粘稠或过度粘液，咳嗽，炎症，喉咙发红，咽喉感染，喉咙痛，粘液分泌异常，粘液运输受损，过敏性鼻炎，哮喘，COPD，呼吸肌肉疾病和疼痛 在喉咙痛。

公开(公告)号：US20120172407A1

公开(公告)日：2012-07-05

申请号：US13392306

申请日：2010-08-23

Applicant: Harald Walter ,  Ramya Rajan ,  Daniel Stierli

Inventor： Harald Walter ,  Ramya Rajan ,  Daniel Stierli

IPC: A01N43/56 ,  C07C239/20 ,  A01P3/00 ,  C07D231/14

CPC classification number: C07D231/14 ,  A01N43/56 ,  C07C239/10 ,  C07C239/20 ,  C07D231/16

Abstract: Compounds of formula (I) in which the substituents are as defined in claim 1, are suitable for use as microbiocides.

Abstract translation: 其中取代基如权利要求1中所定义的式（I）化合物适合用作杀微生物剂。

公开(公告)号：US06974853B2

公开(公告)日：2005-12-13

申请号：US10343181

申请日：2001-07-27

Applicant: Marc Husemann ,  Stephan Zöllner

Inventor： Marc Husemann ,  Stephan Zöllner

IPC: C07C239/20 ,  C07C291/02 ,  C08F4/00 ,  C08F20/00 ,  C09J11/06 ,  C09J133/06 ,  C08F2/00

CPC classification number: C08F4/00

Abstract: An initiator system for radical polymerization, which comprises a combination of compounds of the formulae:

Abstract translation: 用于自由基聚合的引发剂体系，其包含下式的化合物的组合：

公开(公告)号：US06951958B1

公开(公告)日：2005-10-04

申请号：US10049669

申请日：2000-08-03

Applicant: Carl-Magnus A. Andersson ,  Magnus Gustafsson ,  Kent R. I. Olsson

Inventor： Carl-Magnus A. Andersson ,  Magnus Gustafsson ,  Kent R. I. Olsson

IPC: C07C209/40 ,  C07C211/00 ,  C07C211/17 ,  C07C211/27 ,  C07C239/20 ,  C07C249/08

CPC classification number: C07C239/20 ,  C07C209/40 ,  C07C211/17 ,  C07C211/27 ,  C07C249/08 ,  C07C2601/14

Abstract: Described is method for preparing tertiary amines comprising sequential, exhaustive alkylation of a hydroxylamine derivative and cleavage of the O—N bond using the following steps: a) reacting the hydroxylamine derivative with an alkylating agent or with a carbonyl compound to form an oxime intermediate. b) reacting the oxime intermediate with a reducing agent to produce an alkylated derivative c) reacting the alkylated derivative with an alkylating agent or a carbonyl compound in the presence of a reducing agent to produce a dialkylated derivative d) reacting the dialkylated derivative with an alkylating agent to produce a quaternized derivative e) reacting the quaternized derivative with a reagent causing cleavage of the O—N bond to produce a tertiary amine.

Abstract translation: 描述了制备叔胺的方法，其包括羟胺衍生物的连续彻底烷基化和O-N键的切割，使用以下步骤：a）使羟胺衍生物与烷基化剂或羰基化合物反应形成肟中间体。 b）使肟中间体与还原剂反应以产生烷基化衍生物c）在还原剂存在下使烷基化衍生物与烷基化剂或羰基化合物反应以产生二烷基化衍生物d）使二烷基化衍生物与烷基化反应 试剂以产生季铵化衍生物e）使季铵化衍生物与导致ON键断裂以产生叔胺的试剂反应。

公开(公告)号：US20050070707A1

公开(公告)日：2005-03-31

申请号：US10497479

申请日：2002-11-27

Applicant: Reiner Fischer ,  Thomas Schenke ,  Angelika Lubos-Erdelen

Inventor： Reiner Fischer ,  Thomas Schenke ,  Angelika Lubos-Erdelen

IPC: A01N43/72 ,  C07C239/20 ,  C07D209/48 ,  C07D265/02

CPC classification number: C07D265/02

Abstract: The present invention relates to novel [1,2]-oxazine-3,5-dione derivatives of the formula (I) in which W, X, Y, Z, G, D, A and B are as defined in the disclosure, to a plurality of processes for their preparation, and to their use as microbicides, pesticides and herbicides.

Abstract translation: 本发明涉及式（I）的新的[1,2] - 恶嗪-3,5-二酮衍生物，其中W，X，Y，Z，G，D，A和B如本公开所定义， 涉及多种制备方法，以及它们作为杀微生物剂，杀虫剂和除草剂的用途。