公开(公告)号：WO2022129047A2

公开(公告)日：2022-06-23

申请号：PCT/EP2021/085688

申请日：2021-12-14

Applicant: H. LUNDBECK A/S

Inventor： KILBURN, John, Paul ,  ASCIC, Erhad ,  MARIGO, Mauro ,  DAVID, Laurent

IPC: C07D207/10 ,  A61P25/00 ,  A61P25/24 ,  C07C235/00 ,  C07D211/34 ,  C07D213/56 ,  C07D213/61 ,  C07D215/48 ,  C07D217/24 ,  C07D231/12 ,  C07D231/16 ,  C07D233/64 ,  C07D235/06 ,  C07D239/26 ,  C07D241/12 ,  C07D249/06 ,  C07D249/08 ,  C07D261/08 ,  C07D263/32 ,  C07D265/30 ,  C07D275/02 ,  C07D277/30 ,  C07D295/155 ,  C07D305/08 ,  C07D307/16 ,  C07D307/54 ,  C07D333/24 ,  A61K31/415 ,  A61K31/5375 ,  A61K31/425 ,  A61K31/47 ,  A61K31/472 ,  A61K31/4196 ,  A61K31/42 ,  A61K31/421 ,  A61K31/4192 ,  A61K31/40 ,  A61K31/4184 ,  A61K31/44 ,  A61K31/426 ,  A61K31/381 ,  A61K31/4164 ,  A61K31/341 ,  A61K31/337 ,  A61K31/505 ,  A61K31/4965 ,  A61K31/451

Abstract: The present invention is directed to novel modulators of the NMDA receptor. Separate aspects of the inventions are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat neurological disorders or neuropsychiatric disorders such as depression.

公开(公告)号：WO2022053994A1

公开(公告)日：2022-03-17

申请号：PCT/IB2021/058236

申请日：2021-09-10

Applicant: PI INDUSTRIES LIMITED

Inventor： PATRA, Pranab Kumar ,  SYTHANA, Suresh Kumar ,  NAGLE, Pramod ,  SHENDE, Kantilal Balu ,  SINGH, Vipender ,  KLAUSENER, Alexander G.M.

IPC: C07D213/61 ,  C07C253/30 ,  C07C255/10 ,  C07D213/77

Abstract: The present invention discloses a process for the preparation of substituted pyridine compounds of formula (I), comprises a step in which vinylogous nitriles of formula (II), are obtained from substituted α,β-unsaturated nitrile compounds of formula (III), and a further step of converting the vinylogous nitrile compounds of formula (II) into substituted pyridines of formula (I); wherein R1, R2, R3, R4 and LG are as defined in the description.

公开(公告)号：WO2022038365A2

公开(公告)日：2022-02-24

申请号：PCT/GB2021/052158

申请日：2021-08-20

Applicant: SITRYX THERAPEUTICS LIMITED

Inventor： COOKE, Michael Liam ,  FYFE, Matthew Colin Thor ,  TEOBALD, Barry John

IPC: C07C69/60 ,  C07D257/04 ,  A61P29/00 ,  A61P37/00 ,  A61K31/225 ,  A61K31/41 ,  C07D213/30 ,  C07D305/08 ,  C07D331/04 ,  C07D213/61 ,  C07D309/10 ,  C07D333/16 ,  C07D239/26 ,  A61K31/351 ,  A61K31/337 ,  A61K31/38 ,  A61K31/381 ,  A61K31/505 ,  C07C2601/04 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/50 ,  C07C2603/18 ,  C07C69/73

Abstract: The invention relates to compounds of formula (I) and to their use in treating or preventing an inflammatory disease or a disease associated with an undesirable immune response: wherein R, R1, R2 and RB are as defined herein.

公开(公告)号：WO2021234003A1

公开(公告)日：2021-11-25

申请号：PCT/EP2021/063296

申请日：2021-05-19

Applicant: F. HOFFMANN-LA ROCHE AG ,  ROCHE DIAGNOSTICS GMBH ,  ROCHE DIAGNOSTICS OPERATIONS, INC.

Inventor： HAHN, Robert ,  HEINDL, Dieter ,  HOFFMANN, Thomas ,  JOSEL, Hans-Peter ,  KOBOLD, Uwe ,  KUCHELMEISTER, Hannes ,  LOIBL, Simon Ferdinand ,  MAZZIER, Daniela ,  MILIC, Jelena ,  PRENCIPE, Giuseppe ,  REMPT, Martin ,  SEIDEL, Christoph

IPC: C07D213/46 ,  C07D213/55 ,  C07D213/61 ,  C07D213/86 ,  C07D401/04

Abstract: The present invention relates to compounds which are suitable to be used in mass spectrometry as well as methods of mass spectrometric determination of analyte molecules using said compounds.

公开(公告)号：WO2021188728A1

公开(公告)日：2021-09-23

申请号：PCT/US2021/022839

申请日：2021-03-17

Applicant: THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM ,  HERIOT-WATT UNIVERSITY

Inventor： ZHOU, Jia ,  YARWOOD, Stephen ,  WANG, Pingyuan ,  LUCHOWSKA-STANSKA, Urszula ,  VAN BASTEN, Boy

IPC: C07C311/16 ,  C07C311/17 ,  C07C311/20 ,  C07C311/53 ,  C07D209/08 ,  C07D213/61 ,  C07D213/74 ,  C07D215/20 ,  C07D215/227 ,  C07D217/04 ,  C07D231/12 ,  C07D231/56 ,  C07D239/95 ,  C07D307/38 ,  C07D487/04

Abstract: The invention relates generally to novel EPAC1 activators, such as Formula (I) and (II) and the preparation thereof as well as the use of EPAC1 activators disclosed herein as to selectively activate EPAC1 in cells.

公开(公告)号：WO2021185391A1

公开(公告)日：2021-09-23

申请号：PCT/CZ2020/050038

申请日：2020-06-02

Applicant: UNIVERZITA PALACKEHO V OLOMOUCI

Inventor： NISLER, Jaroslav ,  KOPECNY, David ,  SPICHAL, Lukas ,  STRNAD, Miroslav

IPC: C07D213/61 ,  A01N47/30 ,  A01N47/36 ,  C07C275/32 ,  C07C275/34 ,  C07D213/63 ,  A61P21/00

Abstract: The present invention relates to substituted 1-[2-(hydroxyalkyl)phenyl]-3-yl-urea derivatives of the general formula (I), which inhibit one of the key plant enzymes cytokinin oxidase/dehydrogenase (CKX); wherein R1 is hydrogen, halogen, methoxy group, trifluoromethoxy group, methylsulphanyl group or trifluoromethylsulphanyl group; R2 is hydrogen, halogen, amino group, (C1-C5) alkyl, (C2-C5) alkenyl, (C2-C5) alkynyl, or (C1-C5) alkylamino group, wherein (C1-C5) alkyl, (C2-C5) alkenyl, (C2-C5) alkynyl and (C-C5) alkylamino group is optionally substituted with hydroxy and/or amino group; and R3 and R4 are independently hydrogen or halogen, and wherein when X is nitrogen, then R2 is hydrogen or halogen. The invention further relates to the use of these substances in agriculture as stimulators of plant growth and development and as anti-stress factors and to the preparations containing these derivatives.

公开(公告)号：WO2021117846A1

公开(公告)日：2021-06-17

申请号：PCT/JP2020/046201

申请日：2020-12-11

Applicant: 日本新薬株式会社

Inventor： 浅田　純司 ,  春田　剛位 ,  藥師寺　宏幸 ,  田中　徹 ,  倉本　和也 ,  古杉　圭司 ,  渕上　千晶

IPC: A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P9/14 ,  A61P11/00 ,  A61P11/06 ,  A61P11/08 ,  A61P27/02 ,  A61P35/00 ,  A61P35/02 ,  A61P43/00 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  C07D471/04 ,  C07D495/04 ,  C07D513/04 ,  A61P17/00 ,  C07D213/54 ,  C07D213/61 ,  C07D213/73 ,  C07D213/81 ,  C07D215/12 ,  C07D263/34 ,  C07D487/04 ,  C07D498/04 ,  C07D239/14 ,  C07D239/74 ,  C07D277/56 ,  C07D241/12 ,  C07D241/20 ,  A61K31/421 ,  A61K31/426 ,  A61K31/429 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/4965 ,  A61K31/5025 ,  A61K31/505 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5383

Abstract: 本発明の目的は、ＰＤＧＦ受容体キナーゼ阻害活性を有する化合物を提供することである。　本発明として、例えば次の式［１］で表される化合物もしくはその医薬上許容される塩、またはその溶媒和物を挙げることができる。本発明化合物は、ＰＤＧＦ受容体キナーゼ阻害活性を有している。また、本発明化合物はＰＤＧＦ受容体キナーゼ阻害活性を有することから、呼吸器疾患、がん、平滑筋増殖性疾患、血管増殖性疾患、自己免疫性/炎症性疾患、代謝性疾患、血管閉塞性疾患等等の治療剤として有用である。

公开(公告)号：WO2021018833A1

公开(公告)日：2021-02-04

申请号：PCT/EP2020/071130

申请日：2020-07-27

Applicant: SYNGENTA CROP PROTECTION AG

Inventor： HENNESSY, Alan, Joseph ,  JONES, Elizabeth, Pearl ,  DALE, Suzanna, Jane ,  GREGORY, Alexander, William ,  HOULSBY, Ian, Thomas, Tinmouth ,  BHONOAH, Yunas ,  COMAS-BARCELO, Julia ,  ELVES, Philip, Michael

IPC: C07D205/04 ,  C07C1/00 ,  C07D211/30 ,  C07D213/40 ,  C07D213/61 ,  C07D213/75 ,  C07D213/81 ,  C07D213/84 ,  C07D239/30 ,  C07D239/42 ,  C07D261/02 ,  C07D263/04 ,  C07D295/185 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  A01N43/34

Abstract: The present invention relates to compounds of Formula (I), wherein R 1 , R 2 , R 3 , R 4x , R 4y , k and G are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I), to their use for controlling weeds, in particular in crops of useful plants.

公开(公告)号：WO2020252414A1

公开(公告)日：2020-12-17

申请号：PCT/US2020/037639

申请日：2020-06-13

Applicant: PTC THERAPEUTICS, INC. ,  UTEULIYEV, Maulen M. ,  SHU, Lianhe

Inventor： UTEULIYEV, Maulen M. ,  SHU, Lianhe ,  RICHARDS, Steven J. ,  WARKENTIN, Alexander A. ,  DAVIS, Dana

IPC: C07D213/50 ,  C07D213/61 ,  C07D213/65 ,  C07D213/79 ,  C07D213/82 ,  C07D213/84 ,  C07D237/08 ,  C07D237/14 ,  C07D237/24 ,  C07D239/26 ,  C07D405/10 ,  A61K31/44 ,  A61P25/28 ,  A61P25/16

Abstract: Disclosed herein are naphthoquinone derivative compounds of the formula shown below, compositions thereof, and methods of using such compounds and compositions for treating or suppressing oxidative stress disorders and/or neurodegenerative disorders and/or for inhibiting ferroptosis.

公开(公告)号：WO2020161275A1

公开(公告)日：2020-08-13

申请号：PCT/EP2020/053069

申请日：2020-02-07

Applicant: MEDIBIOFARMA, S.L.

Inventor： PALOMINO LARIA, Julio Castro ,  CAMACHO GÓMEZ, Juan ,  RODRÍGUEZ IGLESIAS, Rodolfo ,  VELILLA MARTÍNEZ, Irene

IPC: C07D231/12 ,  C07D333/24 ,  C07C233/53 ,  C07D213/56 ,  C07D213/61 ,  A61P35/00 ,  A61K31/166 ,  A61K31/4409

Abstract: The present invention relates to novel, optionally substituted, N-benzyl-2- phenoxybenzamide derivatives of formula (I), as modulators of EP4 and/or EP2 receptors of prostaglandin E2 (PGE2), to processes for their preparation, to pharmaceutical compositions comprising said compounds and to said compound for use in the treatment of pathological conditions, disorders or diseases that can improve by modulation of EP4 and/or EP2 receptors of prostaglandin E2 (PGE2) such as cancer disease, pain, inflammation, neurodegenerative diseases and kidney diseases.