公开(公告)号：EP3835287B1

公开(公告)日：2024-10-02

申请号：EP19847498.3

申请日：2019-08-08

IPC: C07C229/12 ,  C07C271/20 ,  C12N15/113 ,  C07C219/06 ,  C07C229/06

CPC classification number: C07C229/12 ,  C12N2320/3220130101 ,  C12N2310/1420130101 ,  C12N15/111 ,  C07C229/06 ,  C07C219/06 ,  C07C271/20 ,  C12N2310/32120130101 ,  C12N2310/32220130101 ,  C12N2310/31520130101 ,  C12N2310/34520130101 ,  C12N2310/34620130101 ,  C12N2310/34420130101

公开(公告)号：EP3279185B1

公开(公告)日：2018-11-14

申请号：EP16182859.5

申请日：2016-08-04

Applicant: Taminco bvba

Inventor： VAN WAES, Frederik ,  MOONEN, Kristof ,  ULRICHTS, Dieter

IPC: C07C269/04 ,  C07C271/20

CPC classification number: C07C269/04 ,  C07C271/20

Abstract: A process for the preparation of N-(dialkylaminoalkyl)-carbamic acid esters, in particular (propyl N-[3-(dimethylamino)propyl] carbamate) comprising an oxidative carbonylation reaction of a compound of general structure (II) wherein each of R 1 and R 2 , equal to or different from each other, are independently selected from an alkyl group having 1 to 10 carbon atoms, which is optionally substituted by at least one halogen atom, an aryl group or an aralkyl group; R 3 is selected from an alkyl group having 1 to 36 carbon atoms, which is optionally substituted by at least one halogen atom, an aryl group or an aralkyl group; each of R', R" and R 4 , equal to or different from each other, are independently selected from H, an alkyl group having 1 to 10 carbon atoms, which is optionally substituted by at least one halogen atom, an aryl group or an aralkyl group; and n is an integer in the range from 1 to 8, with a hydroxyl compound of general formula (III), R 3 -OH (III) and in the presence of a catalyst system.

公开(公告)号：EP3365324A1

公开(公告)日：2018-08-29

申请号：EP16791733.5

申请日：2016-10-21

Applicant: The Procter & Gamble Company

Inventor： YELM, Kenneth, Edward ,  WOS, John, August ,  BUNKE, Gregory, Mark ,  FREDERICK, Heath ,  HAUGHT, John, Christian ,  HOKE, Steven, Hamiliton ,  SREEKRISHNA, Koti, Tatachar ,  LIN, Yakang

IPC: C07C269/06 ,  C07C231/02

CPC classification number: C07C237/10 ,  A61K8/41 ,  A61K2800/244 ,  A61Q11/00 ,  C07B2200/07 ,  C07C231/02 ,  C07C269/06 ,  C07C319/20 ,  C07C2601/14 ,  C07D213/81 ,  C07C233/62 ,  C07C271/20 ,  C07C271/22 ,  C07C237/22 ,  C07C233/78 ,  C07C321/14

Abstract: Synthesis methods to produce a series of carboxamides built off of an (S)-2-amino acid backbone or an (R)-2-amino acid backbone, depending upon the desired diastereomer of the end product.

公开(公告)号：EP3350165A1

公开(公告)日：2018-07-25

申请号：EP16847452.6

申请日：2016-09-16

Applicant: Metacrine, Inc.

Inventor： SMITH, Nicholas D. ,  GOVEK, Steven P. ,  NAGASAWA, Johnny Y.

IPC: C07D213/63 ,  C07D207/12 ,  A61K31/4418 ,  A61K31/4412 ,  A61K31/16

CPC classification number: C07C233/80 ,  A61K31/167 ,  A61K31/216 ,  A61K31/381 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/421 ,  A61K31/425 ,  A61K31/426 ,  A61K31/4418 ,  A61K31/445 ,  A61K31/4965 ,  A61K31/505 ,  A61K45/06 ,  C07C233/59 ,  C07C233/62 ,  C07C233/63 ,  C07C237/22 ,  C07C237/42 ,  C07C271/20 ,  C07C2601/04 ,  C07C2601/14 ,  C07D205/04 ,  C07D207/08 ,  C07D207/12 ,  C07D207/24 ,  C07D207/27 ,  C07D211/42 ,  C07D211/46 ,  C07D211/94 ,  C07D213/40 ,  C07D213/64 ,  C07D213/65 ,  C07D213/68 ,  C07D213/75 ,  C07D213/80 ,  C07D239/34 ,  C07D241/18 ,  C07D263/32 ,  C07D275/03 ,  C07D277/34 ,  C07D333/32

Abstract: Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.

公开(公告)号：EP2881392B1

公开(公告)日：2018-06-06

申请号：EP14191380.6

申请日：2011-11-16

Applicant: Texas Heart Institute

Inventor： Biediger, Ronald, J. ,  Gundlach, IV, William, C. ,  Market, Robert, V. ,  Savage, Michael, M. ,  Vanderslice, Peter

IPC: C07D409/12 ,  A61K31/381 ,  A61P9/00

CPC classification number: C07D333/20 ,  A61K35/12 ,  A61K35/17 ,  A61K35/51 ,  C07C229/34 ,  C07C271/20 ,  C07C271/22 ,  C07C311/08 ,  C07D213/64 ,  C07D275/02 ,  C07D317/60 ,  C07D333/10 ,  C07D333/24 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14

Abstract: A method of enhancing binding of cells to an integrin-binding ligand comprises treating integrin-expressing cells in vitro with an agonist of integrin, wherein the integrin is selected from the group consisting of ±4²1, ±4²1, ±4²7, ±4²3 and ±L²2, and contacting the treated cells with an integrin-binding ligand; integrin agonist compounds having the general formula I; methods of treating integrin-expressing cells with such agonists to enhance binding; and therapeutic methods comprising administering agonist-treated cells or agonist compounds to a mammal.

公开(公告)号：EP3278787A1

公开(公告)日：2018-02-07

申请号：EP16773099.3

申请日：2016-03-31

Applicant: Mitsui Chemicals, Inc. ,  SUN MEDICAL CO., LTD.

Inventor： YOSHINAGA, Kazuhiko ,  TANABE, Yoshimitsu ,  KINOSHITA, Shinsuke ,  MITAMURA, Takenori ,  MURAI, Hiroki ,  YOKOYAMA, Takeshi ,  KAMIMOTO, Yoshihisa ,  ORI, Tatsuya ,  SHIMIZU, Hirohisa ,  ARATA, Masami ,  TSUCHIKAWA, Masuji ,  MIYAMORI, Sayaka ,  KATSURA, Yoshiaki

IPC: A61K6/083 ,  A61K6/00

CPC classification number: A61K6/0023 ,  A61K6/00 ,  A61K6/0052 ,  A61K6/083 ,  C07C271/20 ,  C07C2602/42

Abstract: The present invention provides polymerizable monomers represented by the following general formula (1) that are useful as dental materials.

In the general formula (1), R a is a divalent C 6-9 aromatic hydrocarbon group or a divalent C 6-9 optionally bridged cyclic hydrocarbon group, R 1 and R 2 are each a hydrogen atom or a C 1-3 alkyl group, R 3 , R 4 , R 5 and R 6 are each a hydrogen atom or a hydrocarbon group, R 7 and R 8 are each a hydrogen atom or a methyl group, m and n are each independently 0 to 4, and R b and R c are each independently a C 2-6 linear alkylene or C 2-6 linear oxyalkylene group optionally substituted with a C 1-3 alkyl group or a (meth)acryloyloxymethylene group in place of a hydrogen atom.

Abstract translation: 本发明提供可用作牙科材料的由以下通式（1）表示的可聚合单体。 在通式（1）中，Ra为二价C6-9芳族烃基或二价C6-9任选桥接的环状烃基，R1和R2各自为氢原子或C1-3烷基，R3，R4， R5和R6各自为氢原子或烃基，R7和R8各自为氢原子或甲基，m和n各自独立地为0至4，并且Rb和Rc各自独立地为C2-6直链亚烷基或 任选被C1-3烷基或（甲基）丙烯酰氧基亚甲基取代的氢原子取代的C2-6直链氧化烯基。

公开(公告)号：EP3010896B1

公开(公告)日：2017-11-01

申请号：EP14731625.1

申请日：2014-06-18

Applicant: CYGNET BIOSCIENCES B.V.

Inventor： SANFILIPPO, Stefania ,  POSTERARO, Brunella ,  SANGUINETTI, Maurizio ,  BOTTA, Maurizio ,  MACCARI, Giorgio ,  DE LUCA, Filomena ,  DOCQUIER, Jean-Denis ,  DEODATO, Davide

IPC: C07D273/00 ,  C07D413/04 ,  A61K31/395 ,  A61P31/10 ,  A61P11/06 ,  C07C271/20 ,  C07C279/24

CPC classification number: C07D273/00 ,  A61K31/395 ,  A61K31/4192 ,  A61K45/06 ,  C07C271/20 ,  C07C279/24 ,  C07D413/04

公开(公告)号：EP3037410A4

公开(公告)日：2017-05-03

申请号：EP14838284

申请日：2014-08-11

Applicant: MITSUI CHEMICALS INC

Inventor： KOJIMA KOUYA ,  TSUKADA HIDETAKA ,  TAKASHINA MAMORU ,  SHIMAKAWA CHITOSHI ,  KAKINUMA NAOYUKI

IPC: C07C263/04 ,  C07C209/48 ,  C07C253/28 ,  C07C265/14 ,  C07C269/00 ,  C07C269/06 ,  C07C271/14 ,  C07C271/20 ,  C07C273/18 ,  C07C275/24

CPC classification number: C07C263/06 ,  C07C209/48 ,  C07C253/28 ,  C07C263/04 ,  C07C269/00 ,  C07C269/06 ,  C07C271/20 ,  C07C273/1809 ,  C07C273/1854 ,  C07C265/14 ,  C07C271/14 ,  C07C275/24

Abstract: A method for producing meta-xylylenediisocyanates includes a reaction step in which monohalogenated benzenes, formaldehydes, and an amide compound represented by general formula (1) below are allowed to react in the presence of an acidic liquid to produce a bisamide compound; a dehalogenation step in which in the bisamide compound, the halogen atom derived from the monohalogenated benzenes is replaced with a hydrogen atom; and a thermal decomposition step in which the bisamide compound from which the halogen atom is eliminated is subjected to thermal decomposition. In the reaction step, the acidic liquid contains inorganic acid, the equivalent ratio of the hydrogen atom of the inorganic acid relative to the monohalogenated benzenes is more than 14, the acidic liquid has an acid concentration of more than 90 mass%, and the reaction temperature is more than 10°C. General formula (1): (in general formula (1), R 1 represents an alkoxy group or an amino group).

Abstract translation: 作为间苯二甲基二异氰酸酯的制造方法，可以列举在酸性液体的存在下使单卤代苯，甲醛类和下述通式（1）所示的酰胺化合物反应而生成双酰胺化合物的反应工序， 脱卤化步骤，其中在双酰胺化合物中，源自单卤代苯的卤素原子被氢原子置换; 以及热分解步骤，其中消除卤素原子的双酰胺化合物经受热分解。 在反应步骤中，酸性液体含有无机酸，无机酸的氢原子相对于单卤代苯的当量比大于14，酸性液体的酸浓度大于90质量％，并且反应 温度超过10°C。 通式（1）:(通式（1）中，R 1表示烷氧基或氨基。

公开(公告)号：EP3037410A1

公开(公告)日：2016-06-29

申请号：EP14838284.9

申请日：2014-08-11

Applicant: Mitsui Chemicals, Inc.

Inventor： KOJIMA, Kouya ,  TSUKADA, Hidetaka ,  TAKASHINA, Mamoru ,  SHIMAKAWA, Chitoshi ,  KAKINUMA, Naoyuki

IPC: C07C263/04 ,  C07C265/14 ,  C07C269/00 ,  C07C271/14

CPC classification number: C07C263/06 ,  C07C209/48 ,  C07C253/28 ,  C07C263/04 ,  C07C269/00 ,  C07C269/06 ,  C07C271/20 ,  C07C273/1809 ,  C07C273/1854 ,  C07C265/14 ,  C07C271/14 ,  C07C275/24

Abstract: A method for producing meta-xylylenediisocyanates includes a reaction step in which monohalogenated benzenes, formaldehydes, and an amide compound represented by general formula (1) below are allowed to react in the presence of an acidic liquid to produce a bisamide compound; a dehalogenation step in which in the bisamide compound, the halogen atom derived from the monohalogenated benzenes is replaced with a hydrogen atom; and a thermal decomposition step in which the bisamide compound from which the halogen atom is eliminated is subjected to thermal decomposition. In the reaction step, the acidic liquid contains inorganic acid, the equivalent ratio of the hydrogen atom of the inorganic acid relative to the monohalogenated benzenes is more than 14, the acidic liquid has an acid concentration of more than 90 mass%, and the reaction temperature is more than 10°C. General formula (1):

(in general formula (1), R 1 represents an alkoxy group or an amino group).

公开(公告)号：EP2947066A4

公开(公告)日：2016-06-22

申请号：EP14740691

申请日：2014-01-21

Applicant: UNIV OSAKA ,  KNC LAB CO LTD

Inventor： KANAI YOSHIKATSU ,  NAGAMORI SHUSHI ,  KITAURA YOSHIHIKO ,  NEYA MASAHIRO ,  MATSUSHITA NAOHIRO

IPC: C07C211/09 ,  A61K31/138 ,  A61K31/341 ,  A61K31/381 ,  A61K31/40 ,  A61K31/421 ,  A61K31/426 ,  A61K31/4409 ,  A61K31/4453 ,  A61K31/47 ,  A61K31/4704 ,  A61P35/00 ,  A61P43/00 ,  C07C217/04 ,  C07C217/72 ,  C07C255/37 ,  C07C255/54 ,  C07C271/16 ,  C07C271/20 ,  C07C317/22

CPC classification number: C07C217/48 ,  C07C211/09 ,  C07C217/04 ,  C07C217/72 ,  C07C255/37 ,  C07C255/54 ,  C07C271/16 ,  C07C271/20 ,  C07C317/22 ,  C07C317/28 ,  C07C323/20 ,  C07C323/25 ,  C07D209/48 ,  C07D213/68 ,  C07D215/22 ,  C07D215/233 ,  C07D215/26 ,  C07D263/32 ,  C07D277/28 ,  C07D295/08 ,  C07D307/52 ,  C07D333/20 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D409/06 ,  C07D413/04 ,  C07D413/06 ,  C07D417/04 ,  C07D417/06

Abstract: The present invention provides a compound having a selective inhibitory activity against highly-expressed LAT-1 in tumor cell. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, and a LAT-1 inhibitor comprising the same.