公开(公告)号：WO2019063465A1

公开(公告)日：2019-04-04

申请号：PCT/EP2018/075754

申请日：2018-09-24

Applicant: NESTEC S.A.

Inventor： MAHIEUX, Julien, Philippe, Nicolas ,  PALZER, Stefan ,  NIEDERREITER, Gerhard ,  FORNY, Laurent ,  MORA, Federico ,  CHAVEZ MONTES, Bruno, Edgar ,  POQUET, Laure ,  OERTLING, Heiko

IPC: A23F5/22 ,  C07D473/12

Abstract: The present invention provides a method for producing caffeine, wherein the method comprises: (a) combining a coffee extract comprising caffeine with an aqueous organic acid; (b) crystallizing the coffee extract and the aqueous organic acid so as to form caffeine-organic acid co-crystals in an aqueous phase; (c) separating the caffeine-organic acid co-crystals from the aqueous phase; and (d) extracting caffeine from the co-crystals obtained in step (c), wherein step (d) comprises placing the co-crystals in an aqueous solution so as to form a caffeine precipitate and a solution comprising the organic acid. Also provided is a method for producing a decaffeinated coffee extract comprising chlorogenic acids.

公开(公告)号：WO2013103924A3

公开(公告)日：2015-05-28

申请号：PCT/US2013020428

申请日：2013-01-05

Applicant: GUILFORD FREDERICK TIMOTHY

Inventor： GUILFORD FREDERICK TIMOTHY

IPC: A61K38/06 ,  A61K9/127 ,  A61K31/198 ,  A61K31/355 ,  A61K38/24 ,  A61K47/02 ,  A61K47/06 ,  A61P35/00 ,  C07D473/12

CPC classification number: A61K31/198 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/06 ,  A61K9/107 ,  A61K9/127 ,  A61K31/19 ,  A61K31/522 ,  A61K38/063 ,  A61K2300/00

Abstract: This invention proposes an agent to block the "fuel supply" that energizes cancer cell growth by protecting surrounding cells to the cancer, particularly stromal fibroblast cells. The invention disables the products of surrounding cells useable for energy conversion by the cancer cell thereby crippling the cell and disabling its growth process. This application describes the use of a formulation of liposomally encapsulated glutathione that is preferably used orally to increase the level of glutathione in tissues in order to prevent and reverse the metabolic changes in cells that results in the formation of the metabolic fuel that supports cancer cells and to prevent the oxidative stress that damages normal support cells such as fibroblasts and can prevent and reverse these cells from the steps of autophagy and mitophagy that results in the cells decreasing the normal mitochondrial production of ATP for energy and resorting to the use of aerobic glycolysis for energy production. The use of oral liposomally encapsulated glutathione will maintain the presence and normal function of caveolin in fibroblast and other cells, thus preventing their conversion to autophagic tumor stromal cells. By stopping the formation of autophagic cells, the production of the metabolic fuel needed by cancer cells is stopped, which results in the death of the cancer cells. Compositions using liposomally encapsulated glutathione and other compounds that enhance the favorable effects of liposomal glutathione on cancer disease are referenced.

Abstract translation: 本发明提出了一种阻止通过保护周围细胞对癌症，特别是基质成纤维细胞来激活癌细胞生长的“燃料供应”的药剂。 本发明禁止由癌细胞用于能量转换的周围细胞的产物，从而破坏细胞并使其生长过程失效。 本申请描述了脂质体包封的谷胱甘肽制剂的用途，其优选口服用于增加组织中谷胱甘肽的水平，以便防止和逆转导致形成支持癌细胞的代谢燃料的细胞中的代谢变化，以及 以防止损伤正常支持细胞如成纤维细胞的氧化应激，并且可以预防和逆转这些细胞从自噬和间质细胞的步骤，导致细胞降低ATP的正常线粒体产生能量，并利用有氧糖酵解的用途 能源生产。 口服脂质体包裹的谷胱甘肽的使用将维持成纤维细胞和其他细胞中小窝蛋白的存在和正常功能，从而防止其转化为自噬性肿瘤基质细胞。 通过停止形成自噬细胞，停止癌细胞所需的代谢燃料的产生，这导致癌细胞的死亡。 参考了使用脂质体包封的谷胱甘肽和其它增强脂质体谷胱甘肽对癌症疾病的有益作用的化合物的组合物。

公开(公告)号：WO2010111626A3

公开(公告)日：2010-11-18

申请号：PCT/US2010028878

申请日：2010-03-26

Applicant: TAKEDA PHARMACEUTICAL ,  BROWN JASON W ,  GANGLOFF ANTHONY R ,  JENNINGS ANDREW JOHN ,  VU PHONG H

Inventor： BROWN JASON W ,  GANGLOFF ANTHONY R ,  JENNINGS ANDREW JOHN ,  VU PHONG H

IPC: C07D265/36 ,  A61K31/538 ,  A61P3/00 ,  A61P9/00 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D473/12

CPC classification number: C07D265/36 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D473/12

Abstract: Compounds of the following formula are provided for use in inhibiting Poly (ADP-ribose) Polymerase (PARP): wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds.

Abstract translation: 提供下式的化合物用于抑制聚（ADP-核糖）聚合酶（PARP）：其中变量如本文所定义。 还提供了包含此类化合物的药物组合物，试剂盒和制品，用于制备所述化合物的方法和中间体，以及使用所述化合物的方法。

公开(公告)号：WO2008024277A3

公开(公告)日：2008-12-04

申请号：PCT/US2007018235

申请日：2007-08-17

Applicant: NOVACARDIA INC ,  MUGERDITICHIAN MARK ,  DITTRICH HOWARD ,  FARMER BRIAN ,  MURRAY THOMAS ,  KEANA JOHN

Inventor： MUGERDITICHIAN MARK ,  DITTRICH HOWARD ,  FARMER BRIAN ,  MURRAY THOMAS ,  KEANA JOHN

IPC: C07D473/04 ,  A61K31/52 ,  A61K31/522 ,  A61P7/10 ,  A61P11/08 ,  C07D473/06 ,  C07D473/08 ,  C07D473/10 ,  C07D473/12 ,  C07D473/14 ,  C07D473/20 ,  C07D473/22

CPC classification number: C07D473/04 ,  C07D473/06

Abstract: The present invention relates to certain compounds and to methods for the preparation of certain compounds that can be used in the fields of chemistry and medicine. Specifically, described herein are methods for the preparation of various compounds and intermediates, and the compounds and intermediates themselves. More specifically, described herein are methods for synthesizing KW-3902 derivatives of Formula (I), (II), (HI), (IV), (V), and (VI).

Abstract translation: 本发明涉及某些化合物以及制备可用于化学和医学领域的某些化合物的方法。 具体来说，本文描述了制备各种化合物和中间体以及化合物和中间体本身的方法。 更具体地，本文描述了合成式（I），（II），（III），（IV），（V）和（VI）的KW-3902衍生物的方法。

公开(公告)号：WO2006059713A1

公开(公告)日：2006-06-08

申请号：PCT/JP2005/022170

申请日：2005-12-02

Applicant: 協和▲醗▼酵工業株式会社 ,  加瀬 準也 ,  黒川 昌子 ,  塩崎 静男 ,  妹尾 直樹

Inventor： 加瀬 準也 ,  黒川 昌子 ,  塩崎 静男 ,  妹尾 直樹

IPC: C07D473/12 ,  A61K31/522 ,  A61K45/00 ,  A61P25/30 ,  A61P25/32 ,  A61P25/36 ,  C07D473/06

CPC classification number: A61K31/522 ,  C07D473/06

Abstract: A preventive and/or therapeutic agent for drug dependence which contains as an active ingredient either a compound having antagonistic activity against an adenosine A 2A receptor, such as a xanthine derivative represented by, e.g., the formula (I) (wherein R 1 , R 2 , and R 3 are the same or different and each represents hydrogen, lower alkyl, lower alkenyl, or lower alkynyl; R 4 represents cycloalkyl, -(CH 2 ) n -R 5 , or the formula (II); and X 1 and X 2 are the same or different and each represents oxygen or sulfur) or a pharmacologically acceptable salt of the compound.

Abstract translation: 作为药物依赖性的预防和/或治疗剂，其含有对腺苷A 2A受体具有拮抗作用的活性成分，例如由式（I）表示的黄嘌呤衍生物 ）（其中R 1，R 2，R 3和R 3相同或不同，各自表示氢，低级烷基，低级链烯基或 低级炔基; R 4表示环烷基， - （CH 2）n - R 5，或式（ II）; X 1和X 2相同或不同，各自表示氧或硫）或化合物的药理学上可接受的盐。

公开(公告)号：WO2005021044A2

公开(公告)日：2005-03-10

申请号：PCT/US2004027806

申请日：2004-08-25

Applicant: NASTECH PHARM CO ,  QUAY STEVEN C ,  CUI KUNYUAN ,  DATTILO JAMES W

Inventor： QUAY STEVEN C ,  CUI KUNYUAN ,  DATTILO JAMES W

IPC: A61K47/48 ,  C07D473/12 ,  C07H21/04 ,  C12N15/113 ,  C12Q1/68

CPC classification number: C12N15/87 ,  A61K47/645 ,  A61K47/6931 ,  A61K48/00 ,  A61K48/0041 ,  B82Y5/00 ,  C12N15/113

Abstract: Nanoparticles of double-stranded nucleic acid complexed about a complexing agent such as the melamine derivatives of formulae I and II, preferably forming a trimeric nucleic acid complex. In alternative embodiments, polyarginine or a polymer of Gln and Asn further complexed with the double-stranded nucleic acid complex. In a preferred embodiment, the ds nucleic acid is a double stranded RNA having 15 to 30 base pairs suitable for RNA interference. In another aspect of the invention, a ds RNA is produced in which all of the uridines are changed to 5-methyluridine. Preferably, the resultant ds RNAs have 15 to about 30 base pairs and are suitable for RNA interference.

Abstract translation: 双链核酸的纳米颗粒与络合剂例如式I和II的三聚氰胺衍生物络合，优选形成三聚体核酸复合物。 在替代实施方案中，聚精氨酸或Gln和Asn的聚合物与双链核酸复合物进一步复合。 在优选的实施方案中，ds核酸是具有适合于RNA干扰的15至30个碱基对的双链RNA。 在本发明的另一方面，产生ds RNA，其中所有的尿苷都被改变成5-甲基尿苷。 优选地，所得ds RNA具有15至约30个碱基对并且适合于RNA干扰。

公开(公告)号：WO02045707A2

公开(公告)日：2002-06-13

申请号：PCT/US2001/046913

申请日：2001-12-06

IPC: C07D473/06 ,  A61K31/337 ,  A61K31/409 ,  A61K31/505 ,  A61K31/52 ,  A61K31/522 ,  A61K31/704 ,  A61K47/22 ,  A61K47/46 ,  A61K47/48 ,  A61P35/00 ,  C07D473/08 ,  C07D473/10 ,  C07D473/12 ,  C07D473/14 ,  C07H21/04 ,  A61K31/00

CPC classification number: C07H21/04 ,  A61K31/522

Abstract: A method of using modified xanthine molecules as a binding agent is disclosed. Xanthine molecules with at least one substitution of a methyl group at the N1, N3, N7, or N9 position bind to intercalating molecules efficiently. This method can be applied to inhibiting intercalating molecules from binding to nucleic acids, as well as removing intercalating molecules that have been bound to nucleic acids. This method can also be applied to synthesize an efficient drug delivery system for compounds that have low solubility in aqueous media, including anti-neoplastic agents. The method can also be applied to flurosecently labeling nucleic acids.

Abstract translation: 公开了使用改性黄嘌呤分子作为结合剂的方法。 在N1，N3，N7或N9位具有至少一个甲基取代基的黄嘌呤分子有效地结合嵌入分子。 该方法可用于抑制嵌入分子与核酸的结合，以及去除已经与核酸结合的嵌入分子。 该方法还可以用于合成在含水介质中包括抗肿瘤剂的溶解度低的化合物的有效药物递送系统。 该方法也可以用于灵敏地标记核酸。

公开(公告)号：WO0055624A3

公开(公告)日：2001-02-01

申请号：PCT/CA0000246

申请日：2000-03-09

Applicant: LEYLAND JONES BRIAN ,  WONG PIERRE

Inventor： LEYLAND-JONES BRIAN ,  WONG PIERRE

IPC: G01N33/53 ,  G01N33/543 ,  G01N33/94 ,  C07D473/08 ,  C07D473/10 ,  C07D473/12

CPC classification number: G01N33/94 ,  G01N2800/52

Abstract: The invention relates to an enzyme linked immunosorbent assay (ELISA) kit for the rapid determination of metabolic phenotypes including but not limited to CYP 1A2, N-acetyltamferase-1 (NAT-1), CYP 2P6, CYP 2E1 and CYP 3A4, which can be used on a routine basis in a clinical laboratory. The ELISA kit allows physicians to a) individualize therapy of drugs such as theophylline, tamoxifen, and clozapine and b) to predict susceptibility to carcinogen induced diseases such as colon rectal cancers. To reduce the number of patients undergoing clinical testing by selecting for patients with the appropriate phenotype most likely to respond.

Abstract translation: 本发明涉及用于快速测定代谢表型的酶联免疫吸附测定（ELISA）试剂盒，其包括但不限于CYP 1A2，N-乙酰基转移酶-1（NAT-1），CYP2P6，CYP2E1和CYP3A4，其可以 在临床实验室中常规使用。 ELISA试剂盒允许医师a）个体化药物如茶碱，他莫昔芬和氯氮平的治疗，以及b）预测致癌物诱导的疾病如结肠直肠癌的易感性。 通过选择最有可能应答的适当表型的患者，减少接受临床检测的患者人数。

公开(公告)号：WO00008025A1

公开(公告)日：2000-02-17

申请号：PCT/SE1999/001339

申请日：1999-08-05

IPC: C07D473/18 ,  A61K31/522 ,  C07B53/00 ,  C07B61/00 ,  C07C303/30 ,  C07C309/45 ,  C07C309/73 ,  C07D473/00 ,  C07D473/12 ,  C07D473/32 ,  C07D473/40

CPC classification number: C07D473/00 ,  C07C309/73 ,  C07D473/18 ,  Y02P20/55

Abstract: Novel intermediates and improvements in the synthesis of acyclic guanine nucleoside prodrugs of the formula (R)-9-[(2-alkanoylmethyl)-4-(aminoacyloxy)butyl]guanine (for example valtamociclovir stearate), including purine salts amenable to one pot alkylation with the acyclic side chain, acyclic 2-amino-6-halo-purine and protected guanine precursors, one pot manipulations thereof and last step work up procedures.

Abstract translation: 新型中间体和改进的式（R）-9 - [（2-烷酰基甲基）-4-（氨基酰氧基）丁基]鸟嘌呤（例如硬脂酸戊戊昔昔维酸）的无环鸟嘌呤核苷前体药物的合成，包括适用于一锅的嘌呤盐 用无环侧链烷基化，无环2-氨基-6-卤素嘌呤和受保护的鸟嘌呤前体，其一锅操作和最后一步处理程序。

公开(公告)号：WO2023023867A1

公开(公告)日：2023-03-02

申请号：PCT/CA2022/051295

申请日：2022-08-26

Applicant: MCMASTER UNIVERSITY

Inventor： MAGOLAN, Jakob ,  AUSTIN, Richard ,  LEBEAU, Paul ,  BYUN, Jae Hyun ,  SALIBA, Paul ,  SGUAZZIN, Matthew

IPC: C07D473/08 ,  A61K31/522 ,  A61P3/06 ,  C07D473/12

Abstract: This application relates to compounds such as compounds of Formula (I) that block SREBP2-induced hepatic PCSK9 expression, compositions comprising these compounds and methods of use thereof; for example, for treating diseases, disorders or conditions treatable by blocking SREBP2 activation and/or PCSK9 gene expression. (I)