公开(公告)号：EP3081553B1

公开(公告)日：2018-12-12

申请号：EP14869823.6

申请日：2014-12-12

Applicant: University of Tsukuba

Inventor： NAGASE, Hiroshi ,  NAGAHARA, Takashi

IPC: C07C311/29 ,  A61K31/18 ,  A61K31/341 ,  A61K31/381 ,  A61K31/397 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/4453 ,  A61K31/4545 ,  A61P25/20 ,  A61P43/00 ,  C07D213/34 ,  C07D213/61 ,  C07D213/64 ,  C07D213/81 ,  C07D213/82

CPC classification number: C07D213/81 ,  C07C311/21 ,  C07C311/29 ,  C07C311/44 ,  C07D205/04 ,  C07D207/04 ,  C07D211/16 ,  C07D213/34 ,  C07D213/61 ,  C07D213/64 ,  C07D213/82 ,  C07D231/14 ,  C07D233/90 ,  C07D295/192 ,  C07D307/68 ,  C07D333/38 ,  C07D401/12 ,  C07D409/12

Abstract: The present invention aims to provide a novel low-molecular-weight compound having an orexin agonist activity, which is expected to be useful as a superior agent for the treatment or prophylaxis of narcolepsy. The present invention provides a compound showing superior orexin agonist activity which is represented by the formula (I) wherein each symbol is as defined in the DESCRIPTION, and a pharmaceutically acceptable acid addition salt thereof, as well as an orexin agonist containing the compound or a pharmaceutically acceptable acid addition salt thereof.

公开(公告)号：EP3081553A4

公开(公告)日：2017-09-13

申请号：EP14869823

申请日：2014-12-12

Applicant: UNIV TSUKUBA

Inventor： NAGASE HIROSHI ,  NAGAHARA TAKASHI

IPC: C07C311/29 ,  A61K31/18 ,  A61K31/341 ,  A61K31/381 ,  A61K31/397 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/4453 ,  A61K31/4545 ,  A61P25/20 ,  A61P43/00 ,  C07D213/34 ,  C07D213/61 ,  C07D213/64 ,  C07D213/81 ,  C07D213/82

CPC classification number: C07D213/81 ,  C07C311/21 ,  C07C311/29 ,  C07C311/44 ,  C07D205/04 ,  C07D207/04 ,  C07D211/16 ,  C07D213/34 ,  C07D213/61 ,  C07D213/64 ,  C07D213/82 ,  C07D231/14 ,  C07D233/90 ,  C07D295/192 ,  C07D307/68 ,  C07D333/38 ,  C07D401/12 ,  C07D409/12

Abstract: The present invention aims to provide a novel low-molecular-weight compound having an orexin agonist activity, which is expected to be useful as a superior agent for the treatment or prophylaxis of narcolepsy. The present invention provides a compound showing superior orexin agonist activity which is represented by the formula (I) wherein each symbol is as defined in the DESCRIPTION, and a pharmaceutically acceptable acid addition salt thereof, as well as an orexin agonist containing the compound or a pharmaceutically acceptable acid addition salt thereof.

Abstract translation: 本发明的目的在于提供一种具有食欲肽激动剂活性的新型低分子量化合物，预计其可用作治疗或预防发作性睡病的上级药剂。 本发明提供了由式（I）表示的优势的食欲肽激动剂活性的化合物及其药学上可接受的酸加成盐以及含有该化合物或其盐的食欲肽激动剂，其中每个符号如说明书中所定义。 其药学上可接受的酸加成盐。

公开(公告)号：EP3126329A1

公开(公告)日：2017-02-08

申请号：EP15702082.7

申请日：2015-01-16

Applicant: Cardioxyl Pharmaceuticals Inc.

Inventor： KALISH, Vincent Jacob ,  BROOKFIELD, Frederick Arthur ,  COURTNEY, Stephen Martin ,  FROST, Lisa Marie

IPC: C07C311/48 ,  C07D261/20 ,  C07D307/78 ,  C07D307/79 ,  A61K31/18 ,  A61K31/423 ,  A61K31/343 ,  A61P9/04

CPC classification number: C07C311/48 ,  A61K9/0019 ,  A61K9/0053 ,  A61K31/185 ,  A61K31/277 ,  A61K31/337 ,  A61K31/343 ,  A61K31/381 ,  A61K31/423 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/505 ,  A61K31/724 ,  C07C2601/02 ,  C07D213/34 ,  C07D239/26 ,  C07D261/20 ,  C07D305/08 ,  C07D307/38 ,  C07D307/79 ,  C07D307/81 ,  C07D333/18

Abstract: The disclosed subject matter provides N-hydroxymethanesulfonamide compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating heart failure.

Abstract translation: 所公开的主题提供了N-羟基甲磺酰胺化合物，包含这些化合物的药物组合物和试剂盒，以及使用这些化合物或药物组合物的方法。 具体而言，所公开的主题提供了使用这种化合物或药物组合物治疗心力衰竭的方法。

公开(公告)号：EP3120701A1

公开(公告)日：2017-01-25

申请号：EP16181237.5

申请日：2009-12-22

Applicant: Dow AgroSciences LLC

Inventor： QIN, Kuide ,  BOUCHER, Raymond, E., Jr.

IPC: A01N25/22 ,  A01N47/40 ,  A01N51/00 ,  A01P7/04 ,  C07D213/26 ,  C07D213/34 ,  C07D409/04

CPC classification number: A01N25/22 ,  C07D213/26 ,  C07D213/34 ,  C07D213/52 ,  C07D213/57 ,  C07D213/61 ,  C07D409/04 ,  A01N47/40 ,  A01N51/00

Abstract: Insect controlling compositions including an N-substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximine compound and one of: (i) an organic acid other than benthiavalicarb; (ii) a dicarboxylic acid or a salt thereof; and (iii) a tricarboxylic acid or a salt thereof, exhibit increased stability.

Abstract translation: 包括N-取代的（6-卤代烷基吡啶-3-基）烷基亚磺酰亚胺化合物的昆虫控制组合物和（i）除苦草酸之外的有机酸; （ii）二羧酸或其盐; 和（iii）三羧酸或其盐表现出增加的稳定性。

公开(公告)号：EP2344449B1

公开(公告)日：2015-05-13

申请号：EP09785121.6

申请日：2009-09-18

Applicant: Pimco 2664 Limited

Inventor： GREIG, Iain Robert ,  SHERIDAN, Rose Mary ,  FISHER, Raymond ,  TOZER, Matthew, John ,  CLASE, Juha, Andrew ,  SMITH, Andrew ,  TUFFNELL, Andrew, Robert ,  VAN 'T HOF, Robert, Jurgen

IPC: C07C311/20 ,  C07C311/28 ,  C07D213/52 ,  C07D213/61 ,  C07D239/26 ,  C07D239/30 ,  C07D295/135 ,  A61K31/18 ,  A61P29/00

CPC classification number: A61K31/18 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/505 ,  C07C311/20 ,  C07C311/28 ,  C07C311/29 ,  C07D207/04 ,  C07D213/34 ,  C07D213/52 ,  C07D213/61 ,  C07D239/26 ,  C07D239/30 ,  C07D295/135

公开(公告)号：EP2814812A1

公开(公告)日：2014-12-24

申请号：EP13748778.1

申请日：2013-02-15

Applicant: Dow AgroSciences LLC

Inventor： ADAWAY, Timothy J.

IPC: C07D213/34 ,  C07D277/26 ,  C07D285/02 ,  A01N43/10

CPC classification number: C07D213/57 ,  C07D213/34

Abstract: Methods of producing a sulfilimine compound, such as
N -cyano-
S -methyl-
S -[1-(6-trifluoromethyl-3-pyridinyl)ethyl]sulfilimine or other substituted sulfilimine compound. The method includes combining a sulfide compound, cyanamide, a hypochlorite compound, and a base, and oxidizing the sulfide compound to form the sulfilimine compound. The sulfide compound may include a 2-trifluoromethyl-5-(1-substituted)alkyl-thiopyridine compound. The base may include sodium hydroxide. A buffer, such as a phosphate buffer, may, optionally, be used in the reaction.

Abstract translation: 生产硫氰胺化合物如N-氰基-3-甲基-S- [1-（6-三氟甲基-3-吡啶基）乙基]硫亚胺或其它取代的硫亚胺化合物的方法。 该方法包括将硫化物，氰胺，次氯酸盐化合物和碱结合，并氧化硫化物形成硫亚胺化合物。 硫化物可以包括2-三氟甲基-5-（1-取代）烷基 - 硫代吡啶化合物。 碱可以包括氢氧化钠。 可任选地在反应中使用缓冲液，例如磷酸盐缓冲液。

公开(公告)号：EP2717875A2

公开(公告)日：2014-04-16

申请号：EP12731173.6

申请日：2012-06-06

Applicant: Université de Strasbourg ,  Centre National de la Recherche Scientifique (CNRS)

Inventor： FEVE, Marie ,  ZENIOU-MEYER, Maria ,  HAIECH, Jacques ,  CHNEIWEISS, Hervé ,  KILHOFFER, Marie-Claude ,  MAMERI, Samir ,  HIBERT, Marcel

IPC: A61K31/4402 ,  A61K31/4425 ,  A61P35/00 ,  A61K31/05 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4409

CPC classification number: C07D213/16 ,  A61K31/05 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4425 ,  C07D213/26 ,  C07D213/30 ,  C07D213/34 ,  C07F7/1804 ,  G01N33/5011

Abstract: The present invention provides compounds having the formula A: (A) or pharmaceutically acceptable salt thereof, wherein W, R1, R2 and R5 are as defined in classes and subclasses herein, and pharmaceutical compositions thereof, as described generally and in subclasses herein, which compounds are useful as cytotoxic agents towards proliferating and/or quiescent cancer stem cells, and thus are useful, for example, for the treatment of cancer.

公开(公告)号：EP2342193B1

公开(公告)日：2013-06-05

申请号：EP09815778.7

申请日：2009-09-29

Applicant: Matrix Laboratories Limited

Inventor： LAHIRI, Saswata ,  VADALI, Lakshmana, Rao ,  SAIDUGARI, Swamy ,  BANDLAMUDI, Veera, Narayana ,  MAKAM, Parameshwar ,  MANUKONDA, Seshadri, Rao ,  DATTA, Debashish

IPC: C07D401/12 ,  C07D213/34

CPC classification number: C07D401/12 ,  C07D213/34 ,  C07D213/71 ,  C07D213/89

公开(公告)号：EP2501686A1

公开(公告)日：2012-09-26

申请号：EP10775828.6

申请日：2010-11-11

Applicant: Merial Limited

Inventor： SÖRGEL, Sebastian ,  PAULINI, Ralph ,  GROSS, Steffen ,  BEYER, Carsten ,  POHLMAN, Matthias ,  BASTIAANS, Henricus Maria Martinus ,  RACK, Michael ,  CULBERTSON, Deborah, L. ,  ANSPAUGH, Douglas, D. ,  THOMPSON, Sarah ,  SALGADO, Vincent

IPC: C07D285/12 ,  A01N43/824 ,  A61K31/433 ,  A61P33/00

CPC classification number: C07D285/12 ,  A01N43/08 ,  A01N43/10 ,  A01N43/22 ,  A01N43/40 ,  A01N43/46 ,  A01N43/50 ,  A01N43/54 ,  A01N43/56 ,  A01N43/58 ,  A01N43/60 ,  A01N43/62 ,  A01N43/647 ,  A01N43/66 ,  A01N43/713 ,  A01N43/72 ,  A01N43/78 ,  A01N43/80 ,  A01N43/82 ,  C07D207/325 ,  C07D209/10 ,  C07D209/12 ,  C07D213/32 ,  C07D213/34 ,  C07D233/66 ,  C07D235/12 ,  C07D237/08 ,  C07D239/20 ,  C07D249/08 ,  C07D251/16 ,  C07D257/04 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/26 ,  C07D307/38 ,  C07D307/40 ,  C07D307/79 ,  C07D307/80 ,  C07D333/18 ,  C07D333/54 ,  C07D333/56

Abstract: The invention relates to alkylsulfide derivatives compounds of formula I as hererunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.

公开(公告)号：EP2321266A2

公开(公告)日：2011-05-18

申请号：EP09781509.6

申请日：2009-08-05

Applicant: F. Hoffmann-La Roche AG

Inventor： Firooznia, Fariborz ,  Gillespie, Paul ,  Goodnow Jr., Robert Alan ,  Lin, Tai-An ,  Sidduri, Achyutharao ,  So, Sung-Sau ,  tan, Jenny

IPC: C07C311/20 ,  C07C311/29 ,  C07D213/34 ,  A61P11/00 ,  A61K31/18 ,  A61K31/395

CPC classification number: C07C311/29 ,  C07C311/20 ,  C07C317/14 ,  C07C2602/10 ,  C07D213/34

Abstract: The invention is concerned with the compounds of formula (I), and pharmaceutically acceptable salts and esters thereof, wherein R
1 -R
4 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.

Abstract translation: 本发明涉及式I化合物及其药学上可接受的盐和酯，其中R 1 -R 4在详细描述和权利要求书中定义。 此外，本发明涉及制备和使用式I化合物的方法以及含有这些化合物的药物组合物。 式I化合物是CRTH2受体的拮抗剂，可用于治疗与该受体相关的疾病和病症如哮喘。