公开(公告)号：WO2021067836A1

公开(公告)日：2021-04-08

申请号：PCT/US2020/054107

申请日：2020-10-02

Applicant: STEALTH BIOTHERAPEUTICS CORP ,  KEEFE, Dennis ,  ZHENG, Guozhu ,  ARSENJANS, Pavels

Inventor： KEEFE, Dennis ,  ZHENG, Guozhu ,  ARSENJANS, Pavels

IPC: C07F7/08 ,  C07C50/28 ,  C07D201/00

Abstract: The disclosure provides therapeutic compositions (i.e., therapeutic agents) and methods of preventing or treating Friedreich's ataxia in a mammalian subject, reducing risk factors, signs and/or symptoms associated with Friedreich's ataxia (e.g. Complex I deficiency), and/or reducing the likelihood or severity of Friedreich's ataxia. The disclosure further provides novel intermediates for the production of said therapeutic compositions and related reduced versions of said therapeutic compositions, which reduce forms may also be used as therapeutic agents (or prodrugs of the therapeutic agent(s)).

公开(公告)号：WO2020097363A2

公开(公告)日：2020-05-14

申请号：PCT/US2019/060315

申请日：2019-11-07

Applicant: TRITON ALGAE INNOVATIONS, INC.

Inventor： TRAN, Miller ,  DEATON, John ,  ADAMS, Brock ,  MAYFIELD, Michael ,  LONGO, Amanda ,  GONZALEZ, Oscar ,  HANSEN, Jon ,  WANG, Xun ,  SCHROEDER, David

IPC: A23J3/20 ,  C12N15/11 ,  C07D201/00 ,  C07D207/34 ,  A23J3/22 ,  C07D487/22 ,  C07K14/795 ,  C12N1/12 ,  C12N15/113 ,  A23L27/26

Abstract: Provided herein are compositions and processes for producing compositions from an algae to provide heme and a red or red-like color to edible compositions including ingredients and finished food products. Also provided are methods of growing heme-producing algae, methods of producing algae preparations therefrom and methods of making ingredients and food products with algae preparations. Also provided are compositions, including edible compositions that include heme and other nutrient components produced from algae.

公开(公告)号：WO2019201569A1

公开(公告)日：2019-10-24

申请号：PCT/EP2019/057916

申请日：2019-03-28

Applicant: UNILEVER PLC ,  UNILEVER N.V. ,  CONOPCO, INC., D/B/A UNILEVER

Inventor： BREEDEN, Simon, William ,  CLARK, James, Hanley ,  FARMER, Thomas, James ,  MACQUARRIE, Duncan, James ,  MCELROY, Con, Robert ,  OGUNJOBI, Joseph, Kolawole ,  THORNTHWAITE, David, William

IPC: C07C69/82 ,  C07D307/68 ,  C07C67/347 ,  C07C401/00 ,  C07C27/00 ,  C07D201/00

Abstract: A process for preparing dialkyl terephalate comprising the following steps:- i) providing furan-2,5-dicarboxylate; ii) esterifying the furan-2,5-dicarboxylate with alcohol to form furan-2,5-carboxylic acid dialkyl ester; iii) reacting the furan-2,5-carboxylic acid dialkyl ester with ethylene under Diels Alder conditions, elevated temperature and pressure and in the presence of a catalyst such that dialkyl terephthalate is produced; wherein the Diels-Alder reaction is free from solvent; wherein the catalyst comprises a clay comprising metal ions and having Lewis acidity.

公开(公告)号：WO2019081517A3

公开(公告)日：2019-05-02

申请号：PCT/EP2018/079049

申请日：2018-10-23

Applicant: ASSOCIATION POUR LA RECHERCHE À L`IGBMC (ARI)

Inventor： CHAMBON, Pierre ,  HUA, Guoqiang

IPC: A61K31/137 ,  A61K31/343 ,  A61K31/381 ,  C07D201/00 ,  C07D307/88 ,  A61P1/00 ,  A61P17/06 ,  A61P29/00 ,  A61P17/00 ,  A61P11/06

Abstract: The present invention relates to the two enantiomers of a SElective Glucocorticoid Receptor Agonistic Modulator (SEGRAM) of Formula 1 or a derivative thereof; to a deuterated form of a SEGRAM of Formula 1 or a derivative thereof; and to the two deuterated enantiomers of a SEGRAM of (Formula 1) or a derivative thereof: or a pharmaceutically acceptable salt, solvate and/or prodrug thereof. The present invention also relates to a SEGRAM of Formula 1 or a derivative thereof, or a pharmaceutically acceptable enantiomer, deuterated form, salt, solvate and/or prodrug thereof, for use in the prevention or treatment of an inflammatory disorder in a subject in need thereof.

公开(公告)号：WO2013043085A1

公开(公告)日：2013-03-28

申请号：PCT/RU2012/000773

申请日：2012-09-20

Applicant: АХАПКИНА, Валентина Ивановна ,  АХАПКИН, Роман Витальевич

Inventor： АХАПКИНА, Валентина Ивановна ,  АХАПКИН, Роман Витальевич

IPC: A61K31/4015 ,  C07D201/00 ,  C07D201/16 ,  C07D201/18 ,  A61P25/00 ,  A61P9/00 ,  A61P39/06 ,  A61P3/04 ,  A61P7/10 ,  A61P37/02 ,  A61P43/00

CPC classification number: G01N31/16 ,  A61K31/4015 ,  C07D201/16 ,  C07D201/18 ,  C07D207/27 ,  Y10T436/145555

Abstract: Изобретение относится к различным областям медицины, фармации и фармакологии, химико-фармацевтической, фармацевтической и парафармацевтической промышленности, конкретно касается нового класса средств, обладающих модуляторной активностью с соразмерным влиянием. Изобретение заключается в том, что предлагаемый продукт (RS)-2-(2-оксо-4-фенилпирролидин-1-ил)ацетамид не содержит в своем составе биологически инертных веществ, оказывающих негативное влияние на его впервые выявленные и существенно улучшенные известные свойства и характеристики, открывая при этом ранее не известные основополагающие и наиважнейшие представления о составе, расширяя области его применения с повышением эффективности и безопасности применения, увеличением терапевтической широты, обеспечивает получение продукта и его продукции с выявленными свойствами и характеристиками.

Abstract translation: 本发明涉及药物，药物和药理学以及化学制药，制药和制药行业的各个领域，特别涉及具有相似作用的显示调节活性的新一类试剂。 本发明的实质是所提出的（RS）-2-（2-氧代-4-苯基吡咯烷-1-基）乙酰胺产物不含有对其新发现的或显着改善的已知性质产生负面影响的生物惰性物质 特征，引起迄今为止关于该化合物的迄今未知的基本和非常重要的观点，扩大使用范围，增加使用的有效性和安全性，提高治疗指数，并且可以生产该产品和 相关产品具有新发现的特性和特点。

公开(公告)号：WO2004092122A3

公开(公告)日：2005-12-29

申请号：PCT/US2004010745

申请日：2004-04-08

Applicant: ALGORX PHARMACEUTICALS INC ,  MCILVAIN SHARON ,  CHEN WEI ,  RAMIYA PREMCHANDRAN H ,  BURCH RONALD ,  CARTER RICHARD B ,  ANDERSON TIMOTHY A ,  ZHANG HEPING

Inventor： MCILVAIN SHARON ,  CHEN WEI ,  RAMIYA PREMCHANDRAN H ,  BURCH RONALD ,  CARTER RICHARD B ,  ANDERSON TIMOTHY A ,  ZHANG HEPING

IPC: A61K31/05 ,  A61K31/16 ,  A61K31/165 ,  A61K31/5415 ,  A61K31/551 ,  A61K45/06 ,  C07C51/36 ,  C07C231/02 ,  C07C233/20 ,  C07D201/00

CPC classification number: C07C231/02 ,  A61K31/05 ,  A61K31/16 ,  A61K31/165 ,  A61K31/5415 ,  A61K31/551 ,  A61K45/06 ,  C07C51/36 ,  A61K2300/00 ,  C07C57/03 ,  C07C233/20

Abstract: The present invention provides methods for synthesizing the trans isomer of capsaicin and/or capsaicin-like compounds by utilizing a process wherein the trans geometry is set from the beginning of the synthesis reaction and carried through the entire synthesis process.

Abstract translation: 本发明提供了通过利用反应几何形式从合成反应开始设定并通过整个合成过程进行的方法来合成辣椒素和/或辣椒素样化合物的反式异构体的方法。

公开(公告)号：WO2004009541A3

公开(公告)日：2004-05-21

申请号：PCT/US0322410

申请日：2003-07-18

Applicant: PHARMACIA CORP ,  BHAT B GANESH

Inventor： BHAT B GANESH

IPC: C12N15/09 ,  A01N43/04 ,  A61K31/7088 ,  A61K31/7115 ,  A61K31/712 ,  A61K31/7125 ,  A61K48/00 ,  A61P3/00 ,  A61P3/06 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00 ,  C07D20060101 ,  C07D201/00 ,  C07H21/04 ,  C12N5/00 ,  C12N15/113

CPC classification number: C12N15/1137 ,  C12N2310/11 ,  C12N2310/315 ,  C12N2310/321 ,  C12N2310/3341 ,  C12N2310/341 ,  C12N2310/346 ,  C12Y301/01003 ,  Y02P20/582 ,  C12N2310/3525

Abstract: Antisense compounds, compositions and methods are provided for modulating the expression of Endothelial Lipase (EL). The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding EL. Methods of using these compounds for modulation of EL expression and for treatment of diseases associated with expression of EL are provided.

Abstract translation: 提供反义化合物，组合物和方法用于调节内皮脂肪酶（EL）的表达。 该组合物包含靶向编码EL的核酸的反义化合物，特别是反义寡核苷酸。 提供了使用这些化合物调节EL表达和治疗与EL表达相关的疾病的方法。

公开(公告)号：WO0191715A2

公开(公告)日：2001-12-06

申请号：PCT/EP0106281

申请日：2001-06-01

Applicant: PENTAPHARM LTD ,  EZAKI GLICO CO ,  KURIKI TAKASHI ,  NAKAE TAKASHI ,  NISHIMURA TAKAHISA ,  NAKAYAMA HIROKI

Inventor： KURIKI TAKASHI ,  NAKAE TAKASHI ,  NISHIMURA TAKAHISA ,  NAKAYAMA HIROKI

IPC: A61K8/00 ,  A61K8/19 ,  A61K8/23 ,  A61K8/30 ,  A61K8/33 ,  A61K8/34 ,  A61K8/35 ,  A61K8/36 ,  A61K8/362 ,  A61K8/365 ,  A61K8/368 ,  A61K8/40 ,  A61K8/41 ,  A61K8/42 ,  A61K8/44 ,  A61K8/46 ,  A61K8/49 ,  A61K8/60 ,  A61K8/64 ,  A61K8/67 ,  A61K8/68 ,  A61K8/72 ,  A61K8/73 ,  A61K8/86 ,  A61K8/96 ,  A61K8/97 ,  A61K8/98 ,  A61K31/198 ,  A61K31/355 ,  A61K31/375 ,  A61K31/70 ,  A61K31/7048 ,  A61K31/715 ,  A61K36/06 ,  A61Q5/00 ,  A61Q19/00 ,  A61Q19/02 ,  C07D201/00 ,  A61K7/48

CPC classification number: A61Q19/02 ,  A61K8/0208 ,  A61K8/19 ,  A61K8/347 ,  A61K8/35 ,  A61K8/362 ,  A61K8/365 ,  A61K8/368 ,  A61K8/41 ,  A61K8/44 ,  A61K8/466 ,  A61K8/4926 ,  A61K8/494 ,  A61K8/4946 ,  A61K8/498 ,  A61K8/4986 ,  A61K8/60 ,  A61K8/602 ,  A61K8/64 ,  A61K8/671 ,  A61K8/673 ,  A61K8/676 ,  A61K8/678 ,  A61K8/68 ,  A61K8/735 ,  A61K8/736 ,  A61K8/86 ,  A61K8/97 ,  A61K8/9706 ,  A61K8/982 ,  A61K36/06 ,  A61K36/23 ,  A61K36/258 ,  A61K36/484 ,  A61K36/515 ,  A61Q19/00 ,  A61K2300/00

Abstract: The objective of the present invention was to enhance the skin whitening effects and blackening prevention effects and supply safe and stable topical agents for dermatological use. For that purpose 4-Hydroxyphenyl- alpha -D-glucopyranoside was combined with auxiliary agents such as ascorbic acid and its derivatives, crude drugs and its extracts, hydroxycarboxylic acid and its salts, oil soluble glycyrrhiza extract, gentian extract, phenol derivatives and their salts, placenta extract, kojic acid and its derivatives, glucosamine and its derivatives, azelaic acid and its derivatives, retinol and its derivatives, pyridoxin and its derivatives, tocopherol and its derivatives, chitosan and its decomposition products, caffeic acid derivatives, hydroxycinnamate and its derivatives, Umbelliferae plant extracts, mycelial cultures and their extracts, plant leaves and their extracts.

Abstract translation: 本发明的目的是增强皮肤美白效果和防止黑化作用，并提供用于皮肤病学用途的安全和稳定的外用剂。 为此，将4-羟基苯基-α-D-吡喃葡萄糖苷与助剂如抗坏血酸及其衍生物，生药及其提取物，羟基羧酸及其盐，油溶性甘草提取物，龙胆提取物，苯酚衍生物及其盐 ，胎盘提取物，曲酸及其衍生物，葡糖胺及其衍生物，壬二酸及其衍生物，视黄醇及其衍生物，吡哆酮及其衍生物，生育酚及其衍生物，壳聚糖及其分解产物，咖啡酸衍生物，羟基肉桂酸酯及其衍生物 ，伞形植物提取物，菌丝体培养物及其提取物，植物叶及其提取物。

公开(公告)号：WO99040068A3

公开(公告)日：1999-11-25

申请号：PCT/EP1999/000855

申请日：1999-02-05

IPC: A61K31/4709 ,  A61K31/496 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D201/00 ,  C07D215/38 ,  C07D401/12 ,  C07D405/12 ,  A61K31/47 ,  A61K31/495 ,  C07D405/14

CPC classification number: C07D215/38 ,  C07D401/12 ,  C07D405/12

Abstract: The present invention relates to a group of novel 2-aminoquinoline derivatives which are potent and selective agonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R1)n represents 1 or 2 substituents, which can be the same or different, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, and mono- or dialkyl (C1-2)-amino, or two groups R1 at adjacent carbon atoms together with the benzene ring may form the benzdioxane group or benzofuran group, X represents nitrogen or carbon, and the dotted line may represent a double bond, (R2)p represents 0, 1 or 2 substituents, which can be the same or different, from the group methyl and ethyl, or (R2)p is a methylene bridge or ethylene bridge, R3 is hydrogen or methyl, and (R)m represents 0, 1, or 2 substituents, which can be the same or different and can be located at all available positions of the quinolyl group, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, and mono- or dialkyl (C1-2)-amino, on the understanding that R1 cannot represent o-OCH3 when X is nitrogen, (R2)p and R3 are hydrogen, m is 0 and n is 1.

Abstract translation: 本发明涉及一组新的2-氨基喹啉衍生物，它们是有效的和选择性的多巴胺D4受体拮抗剂。 这些化合物具有通式（I），其中（R 1）n表示0,1或2个可以相同或不同的选自C 1-3烷基或烷氧基，卤素，三氟甲基，硝基，氨基和单 或二烷基（C1-2） - 氨基，或在与苯环连接的相邻碳原子上的两个R1基团可形成苯并二恶烷基团或苯并呋喃基团; X代表氮和碳，并且虚线可以代表双键; （R2）p代表0,1或2个取代基，它们可以相同或不同，选自甲基和乙基，或（R2）p是亚甲基桥或亚乙基桥; R 3表示氢或甲基，和（R2）m表示0，1或2个取代基，其可以相同或不同，并且可以位于所述喹啉基的所有可用的位置，选自C 1-3烷基或烷氧基，卤素 ，三氟甲基，硝基，氨基和单或二烷基（C1-2） - 氨基，应当理解，当X代表氮时，R1不能代表o-OCH3，（R2）p和R3代表氢，并且m是0和 n 1。

公开(公告)号：WO2023073634A1

公开(公告)日：2023-05-04

申请号：PCT/IB2022/060389

申请日：2022-10-28

Applicant: UNIVERSITA' DEGLI STUDI DI FIRENZE ,  UNIVERSITA' DEGLI STUDI DI PARMA

Inventor： CARTA, Fabrizio ,  ANGELI, Andrea ,  SELLERI, Silvia ,  SUPURAN, Claudiu T. ,  CABASSI, Clotilde Silvia ,  SPADINI, Costanza

IPC: C07C391/00 ,  C07C391/02 ,  C07D201/00 ,  C07D277/52 ,  A61P31/00 ,  A61P33/00 ,  A61K31/00

Abstract: Compounds containing the carbamoselenoyl and/or sulfamoyl function, usable as selective antifungal agents against Malassezia pachydermatis strains for topical veterinary and human use, having the following general structures: Formula I; Formula II; Formula III where X= C,N,O,S,Se or a Metal (M) R= H, SO2NHR, Alkyl, Alkylaryl, Halogen, Alkoxy, NO2, NNPR, Piperonyl, Naphthyl R2 = H, alkyl, aryl, heteroaryl. and designed to act through a dual action: a) the inhibition of the metal enzyme Carbonic Anhydrase (AC; EC 4.2.1.1 ) specifically expressed by Malassezia pachydermatis; b) the function as a carrier of the element selenium in organic form which is known to very effectively interfere with the metabolism and biosynthesis of lipid components of the target fungal organisms.