公开(公告)号：EP4293035A1

公开(公告)日：2023-12-20

申请号：EP22752816.3

申请日：2022-02-10

申请人： AJINOMOTO CO., INC.

发明人： HAYAKAWA, Nobuhiko ,  ICHIMARU, Taisuke ,  INOUE, Satoshi ,  TAKAHASHI, Daisuke

IPC分类号： C07H21/04 ,  C07D213/71 ,  C07D235/28 ,  C07D249/04 ,  C07D257/04 ,  C07D263/58 ,  C07D277/78 ,  C07D513/04 ,  C12N15/11

摘要： The present invention provides a method for producing an oligonucleotide having a phosphate ester bond by oxidizing an oligonucleotide precursor having a phosphite ester bond or a phosphonate ester bond with an oxidant, wherein the oxidant is a compound represented by the formula (I) excluding 2,2-dipyridyl disulfide:

wherein the symbols are as defined in the specification.

公开(公告)号：EP4223746A1

公开(公告)日：2023-08-09

申请号：EP23177983.6

申请日：2012-04-27

申请人： Zeon Corporation

发明人： Sakamoto, Kei ,  Okuyama, Kumi

IPC分类号： C07D277/82 ,  C07C251/86 ,  C07C249/16 ,  C07D215/38 ,  C07D263/58 ,  C08F20/36 ,  C08F20/38 ,  G02B5/30 ,  G02F1/13363

摘要： The present invention relates to the use of certain hydrazine compounds, such as the one represented by formula (H), as a raw material for producing a polymerizable liquid crystal compound showing reverse wavelength dispersion.

公开(公告)号：EP4074707A1

公开(公告)日：2022-10-19

申请号：EP20899991.2

申请日：2020-12-10

申请人： Shanghai Zhimeng Biopharma, Inc.

发明人： LIANG, Bo ,  CHEN, Huanming ,  LIU, Gang ,  ZHANG, Zhijun ,  XIA, Tian ,  HUA, Bo ,  JIN, Qiu

IPC分类号： C07D413/04 ,  C07D413/14 ,  C07D498/10 ,  C07H13/10 ,  C07D413/12 ,  C07D263/58 ,  C07D265/18 ,  C07H1/00 ,  A61K31/536 ,  A61K31/537 ,  A61K31/423 ,  A61K31/424 ,  A61K31/706 ,  A61K31/675 ,  C07F9/6584 ,  A61P25/04 ,  A61P25/06 ,  A61P9/10 ,  A61P25/24 ,  A61P25/28 ,  A61P25/08

摘要： Disclosed are a compound having a neuroprotective effect, a preparation method therefor and a use thereof. Specifically, the compound has the structure shown by formula I, the definition of each group and substituent being as described in the description. Further disclosed are a preparation method for the compound and a use thereof for neuroprotection.

公开(公告)号：EP3483141A3

公开(公告)日：2019-07-10

申请号：EP18210839.9

申请日：2012-04-27

申请人： Zeon Corporation

发明人： Sakamoto, Kei ,  Okuyama, Kumi

IPC分类号： C07C251/86 ,  C07C249/16 ,  C07D215/38 ,  C07D263/58 ,  C07D277/82 ,  C08F20/36 ,  C08F20/38 ,  G02B5/30 ,  G02F1/13363

摘要： The present invention relates to: a hydrazine compound represented by formula (3), wherein A x and A y have the meanings indicated in claims 1 to 5; a method for producing an optically anisotropic article by (i) obtaining a polymerizable compound by reacting the hydrazine compound with a carbonyl compound, (ii) forming an alignment film on a substrate, and (iii) forming a liquid crystal layer on the alignment film using the polymer obtained by polymerizing the polymerizable compound or a polymerizable composition including the polymerizable compound and an initiator; and a method for producing a polymerizable compound represented by formula (I), by reacting the hydrazine compound with a carbonyl compound represented by formula (4). The film thus obtained has a low melting point, excellent solubility, is capable of being manufactured at low cost, and capable of uniform polarized light conversion across a broad wavelength region.

公开(公告)号：EP2552888B1

公开(公告)日：2018-09-26

申请号：EP10799032.7

申请日：2010-12-22

申请人： Serentrix, LLC

发明人： NAPOLETANO, Mauro ,  TREVISANI, Marcello ,  PAVANI, Maria Giovanna ,  FRUTTAROLO, Francesca

IPC分类号： C07D209/32 ,  C07D235/26 ,  C07D263/58 ,  C07D265/36 ,  C07D401/12 ,  C07D403/12 ,  C07D407/12 ,  A61K31/404 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/538 ,  A61P29/00 ,  A61P11/00 ,  A61P13/00 ,  A61P17/00

CPC分类号： C07D413/14 ,  C07D209/34 ,  C07D235/26 ,  C07D263/58 ,  C07D265/36 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12

摘要： The invention discloses compounds of formula I wherein Y s selected from a group of formula and W, Q, n, R1, R2, R3, U1-U5 have the meanings given in the description. The compounds of formula I are TRPV1 antagonists and are useful as active ingredients of pharmaceutical compositions for the treatment of pain and other conditions ameliorated by the inhibition of the vanilloid receptor TRPV1. 1.

公开(公告)号：EP3098217B1

公开(公告)日：2018-04-25

申请号：EP15743807.8

申请日：2015-02-02

申请人： Tokyo University of Science Foundation

发明人： SHIINA, Isamu

IPC分类号： C07D207/327 ,  C07B53/00 ,  C07B55/00 ,  C07D207/27 ,  C07D207/333 ,  C07D207/416 ,  C07D209/08 ,  C07D209/12 ,  C07D209/34 ,  C07D209/38 ,  C07D209/48 ,  C07D209/86 ,  C07D235/06 ,  C07D263/58 ,  C07D403/06 ,  C07B61/00 ,  C07C269/06 ,  C07C271/22 ,  C07D471/04 ,  C07D513/04

CPC分类号： C07B53/00 ,  C07B55/00 ,  C07B2200/07 ,  C07C269/06 ,  C07D207/27 ,  C07D207/327 ,  C07D207/333 ,  C07D207/34 ,  C07D207/416 ,  C07D209/08 ,  C07D209/12 ,  C07D209/34 ,  C07D209/38 ,  C07D209/48 ,  C07D209/86 ,  C07D235/06 ,  C07D263/58 ,  C07D403/06 ,  C07D471/04 ,  C07D513/04 ,  C07C271/22

摘要： Provided is a method for producing an optically active carboxylic acid ester at a high yield and with high enantioselectivity using dynamic kinetic resolution, said optically active carboxylic acid ester having an ±-nitrogen substituent. This method for producing an optically active carboxylic acid ester includes a step in which racemic carboxylic acid represented by formula (a) and a specific alcohol or phenol derivative are reacted in a polar solvent having a dipole moment of at least 3.5 in the presence of an acid anhydride and an asymmetric catalyst, one enantiomer of the racemic carboxylic acid is selectively esterified, and the other enantiomer is racemized. In formula (a), Ra1 represents a nitrogen-containing heteroaromatic ring group bonded to an assymetric carbon via a nitrogen atom constituting a ring, and Ra2 is an organic group.

公开(公告)号：EP2934498B1

公开(公告)日：2017-11-15

申请号：EP13814926.5

申请日：2013-12-20

申请人： Janssen Sciences Ireland UC

发明人： GUILLEMONT, Jerôme Emile Georges ,  MOTTE, Magali Madeleine Simone ,  KOUL, Anil ,  LOUNIS, Nacer

IPC分类号： A61K31/00 ,  A61K31/423 ,  A61K31/428 ,  A61P31/04 ,  A61P31/06 ,  A61K45/06 ,  C07D277/62 ,  C07D277/82 ,  C07D263/58

CPC分类号： C07D277/82 ,  A61K31/423 ,  A61K31/428 ,  A61K45/06 ,  C07D263/58 ,  C07D277/62 ,  A61K2300/00

摘要： The present invention relates to the following compounds for use in the treatment of a bacterial infection wherein the integers are as defined in the description. The invention also relates to compounds for use as medicaments, pharmaceutical compositions and some novel compounds.

公开(公告)号：EP3054936A4

公开(公告)日：2017-03-29

申请号：EP14852765

申请日：2014-10-10

申请人： EASTERN VIRGINIA MEDICAL SCHOOL ,  THE REGENTS OF THE UNIV OF CALIFORNIA SANTA CRUZ ,  THE UNITED STATES OF AMERICA DEPT OF HEALTH AND HUMAN SERVICES ,  UNIV JEFFERSON

发明人： MALONEY DAVID J ,  LUCI DIANE K ,  JADHAV AJIT ,  HOLMAN THEODORE ,  NADLER JERRY L ,  HOLINSTAT MICHAEL ,  TAYLOR-FISHWICK DAVID ,  SIMEONOV ANTON ,  YASGAR ADAM ,  MCKENZIE STEVEN E

IPC分类号： A61K31/045 ,  A61K31/10 ,  A61K31/18 ,  A61P3/00 ,  A61P7/00 ,  A61P35/00 ,  C07C311/44 ,  C07D211/28 ,  C07D213/76 ,  C07D217/02 ,  C07D217/22 ,  C07D235/30 ,  C07D239/69 ,  C07D261/16 ,  C07D263/58 ,  C07D277/52 ,  C07D277/82 ,  C07D295/135 ,  C07D333/36 ,  C07D417/12 ,  C12Q1/26

CPC分类号： C07C311/44 ,  C07D211/28 ,  C07D213/76 ,  C07D217/02 ,  C07D217/22 ,  C07D235/30 ,  C07D239/69 ,  C07D261/16 ,  C07D263/58 ,  C07D277/52 ,  C07D277/82 ,  C07D295/135 ,  C07D333/36 ,  C07D417/12

摘要： Human lipoxygenases (LOXs) are a family of iron-containing enzymes involved in catalyzing the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation, and cell proliferation. Platelet-type 12-(S)-LOX (12-LOX) is of particular interest because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Disclosed herein is the identification and medicinal chemistry optimization of a 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide-based scaffold. The compounds display nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases. In addition to possessing favorable ADME properties, the compounds also inhibit PAR-4 induced aggregation and calcium mobilization in human platelets, and reduce 12-HETE in mouse/human beta cells. The compounds can also be used in methods for treating or preventing a 12-lipoxygenase mediated disease or disorder.

公开(公告)号：EP3098217A1

公开(公告)日：2016-11-30

申请号：EP15743807.8

申请日：2015-02-02

申请人： Tokyo University of Science Foundation

发明人： SHIINA, Isamu

IPC分类号： C07D207/327 ,  C07B53/00 ,  C07B55/00 ,  C07D207/27 ,  C07D207/333 ,  C07D207/416 ,  C07D209/08 ,  C07D209/12 ,  C07D209/34 ,  C07D209/38 ,  C07D209/48 ,  C07D209/86 ,  C07D235/06 ,  C07D263/58 ,  C07D403/06 ,  C07B61/00 ,  C07C269/06 ,  C07C271/22 ,  C07D471/04 ,  C07D513/04

CPC分类号： C07B53/00 ,  C07B55/00 ,  C07B2200/07 ,  C07C269/06 ,  C07D207/27 ,  C07D207/327 ,  C07D207/333 ,  C07D207/34 ,  C07D207/416 ,  C07D209/08 ,  C07D209/12 ,  C07D209/34 ,  C07D209/38 ,  C07D209/48 ,  C07D209/86 ,  C07D235/06 ,  C07D263/58 ,  C07D403/06 ,  C07D471/04 ,  C07D513/04 ,  C07C271/22

摘要： Provided is a method for producing an optically active carboxylic acid ester at a high yield and with high enantioselectivity using dynamic kinetic resolution, said optically active carboxylic acid ester having an α-nitrogen substituent. This method for producing an optically active carboxylic acid ester includes a step in which racemic carboxylic acid represented by formula (a) and a specific alcohol or phenol derivative are reacted in a polar solvent having a dipole moment of at least 3.5 in the presence of an acid anhydride and an asymmetric catalyst, one enantiomer of the racemic carboxylic acid is selectively esterified, and the other enantiomer is racemized. In formula (a), Ra1 represents a nitrogen-containing heteroaromatic ring group bonded to an assymetric carbon via a nitrogen atom constituting a ring, and Ra2 is an organic group.

摘要翻译： 提供了使用动态动力学拆分以高产率和高对映选择性制备光学活性羧酸酯的方法，所述光学活性羧酸酯具有± - 氮取代基。 该光学活性羧酸酯的制造方法包括使式（a）表示的外消旋羧酸和特定的醇或苯酚衍生物在偶极矩为3.5以下的极性溶剂中，在 酸酐和不对称催化剂，外消旋羧酸的一种对映异构体被选择性酯化，另一种对映体被外消旋化。 在式（a）中，Ra1表示通过构成环的氮原子键合到不对称碳上的含氮杂芳环，Ra2是有机基。

公开(公告)号：EP2488504B1

公开(公告)日：2016-07-06

申请号：EP10754433.0

申请日：2010-09-14

申请人： Merck Patent GmbH

发明人： SCHIEMANN, Kai ,  SCHULTZ, Melanie ,  STAEHLE, Wolfgang

IPC分类号： C07D249/18 ,  C07D263/58 ,  A61K31/4192 ,  A61K31/423 ,  A61P35/00

CPC分类号： C07D249/18 ,  C07D263/58