公开(公告)号：US09538753B2

公开(公告)日：2017-01-10

申请号：US14585962

申请日：2014-12-30

Applicant: DOW AGROSCIENCES LLC

Inventor： W. John Owen ,  Chenglin Yao ,  Beth Lorsbach

IPC: A61K31/513 ,  C07D239/47 ,  A01N43/54 ,  A01N37/34 ,  A01N37/50 ,  A01N43/40 ,  A01N43/56 ,  A01N43/88 ,  A01N47/08

CPC classification number: A01N43/54 ,  A01N37/34 ,  A01N37/50 ,  A01N43/40 ,  A01N43/56 ,  A01N43/653 ,  A01N43/88 ,  A01N47/08 ,  A01N45/02 ,  A01N47/14 ,  A01N47/24 ,  A01N47/04

Abstract: A fungicidal composition containing a fungicidally effective amount of the compound of Formula I: 5-fluoro-4-imino-3-methyl-1-tosyl-3,4-dihydropyrimidin-2(1H)-one, and at least one fungicide selected from the group consisting of mancozeb, chlorothalonil, pyraclostrobin, fluoxastrobin, azoxystrobin, trifloxystrobin, picoxystrobin, and kresoxim-methyl provides synergistic control of selected fungi.

Abstract translation: 含有杀真菌有效量的式I化合物：5-氟-4-亚氨基-3-甲基-1-甲苯磺酰基-3,4-二氢嘧啶-2（1H） - 酮的杀真菌组合物和选自至少一种杀真菌剂 来自由代森锰锌，百菌清，嘧菌酯，氟草胺，嘧菌酯，肟菌酯，吡肟菌酯和克雷肟甲酯组成的组提供了所选真菌的协同控制。

公开(公告)号：US20160318879A1

公开(公告)日：2016-11-03

申请号：US15210255

申请日：2016-07-14

Applicant: ACTELION PHARMACEUTICALS LTD.

Inventor： Stefan ABELE ,  Jacques-Alexis FUNEL ,  Ivan SCHINDELHOLZ

IPC: C07D239/47

CPC classification number: C07D239/47

Abstract: The present invention relates to a new synthetic intermediate, namely the compound of formula I-2 or a salt thereof. Said compound of formula I-2 or its salt can be used to prepare the compound of formula I-3 which is an important synthetic intermediate used in the preparation of macitentan.

Abstract translation: 这是一种重要的合成中间体，用于制备麦可坦。

公开(公告)号：US20160304466A1

公开(公告)日：2016-10-20

申请号：US15101738

申请日：2014-12-03

Applicant: THE SCRIPPS RESEARCH INSTITUTE

Inventor： Yangbo Feng ,  Philip Lograsso ,  Ke Zheng ,  Chul Min Park

IPC: C07D231/40 ,  C07D401/14 ,  C07D409/14 ,  C07D403/12 ,  C07D239/47 ,  C07D405/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D401/12 ,  C07D403/14

CPC classification number: C07D231/40 ,  C07D231/54 ,  C07D239/47 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention is directed to modulators, such as inhibitors, of JNK isoform 2 (JNK2) or isoform 3 (JNK3) comprising compounds of formula (I) or formula (II) as described herein. Compounds of the invention can be used for treatment of a medical disorder in a patient wherein modulation of JNK3 is medically indicated, such as when the disorder is Parkinson disease (PD) Alzheimer's disease (AD), Huntington's disease (HD), amyotrophic lateral sclerosis (ALS), multiple sclerosis (MS), myocardial infarction (MI), glaucoma, obesity, diabetes, cancer, rheumatoid arthritis, fibrotic disease, pulmonary fibrosis, kidney disease, liver inflammation, Crohns disease, hearing loss, Prader Willi syndrome, or a condition where modification of feeding behavior is medically indicated.

Abstract translation: 本发明涉及如本文所述的包含式（I）或式（II）化合物的JNK同种型2（JNK2）或同种型3（JNK3）的调节剂，例如抑制剂。 本发明的化合物可用于治疗其中医学上指示调节JNK3的患者的医学病症，例如当该疾病是帕金森病（PD）阿尔茨海默病（AD），亨廷顿舞蹈病（HD），肌萎缩性侧索硬化 （ALS），多发性硬化症（MS），心肌梗塞（MI），青光眼，肥胖症，糖尿病，癌症，类风湿性关节炎，纤维化疾病，肺纤维化，肾脏疾病，肝脏炎症，克罗恩病，听力丧失，Prader Willi综合征或 在医学上指示进食行为改变的条件。

公开(公告)号：US09463192B2

公开(公告)日：2016-10-11

申请号：US14768727

申请日：2014-02-18

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Jun Takeuchi ,  Satoshi Itadani ,  Kazuya Hashimura ,  Masahiro Ikura ,  Masato Higashino ,  Tetsuya Yasuhiro ,  Takeshi Nagaura

IPC: A61K31/506 ,  A61K31/136 ,  A61K31/444 ,  A61K31/519 ,  A61K31/663 ,  A61K31/5377 ,  C07D401/14 ,  C07D401/12 ,  C07D213/75 ,  C07D239/47 ,  C07D471/04 ,  C07D487/04 ,  A61K45/06 ,  C07D405/14 ,  C07D409/14

CPC classification number: A61K31/506 ,  A61K31/136 ,  A61K31/444 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/663 ,  A61K45/06 ,  C07D213/75 ,  C07D239/47 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  C07D487/04 ,  Y02A50/414

Abstract: The present invention provides a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy for Trk-related diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I), wherein all symbols represent the same meanings as described in the specification, a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.

公开(公告)号：US20160280662A1

公开(公告)日：2016-09-29

申请号：US15173493

申请日：2016-06-03

Applicant: Adama Makhteshim Ltd.

Inventor： Nakyen Choy ,  Ronald Ross, JR.

IPC: C07D239/47

CPC classification number: C07D239/47 ,  A01N43/54

Abstract: Provided herein are 5-fluoro-4-imino-3-(alkyl/substituted alkyl)-1-(arylsulfonyl)-3,4-dihydropyrimidin-2(1H)-one and processes for their preparation which may include the use of an alkali carbonate and an alkylating agent

公开(公告)号：US20160272618A1

公开(公告)日：2016-09-22

申请号：US15031628

申请日：2014-10-24

Applicant: CHILDREN'S MEDICAL CENTER CORPORATION ,  PRESIDENT AND FELLOWS OF HARVARD COLLEGE

Inventor： Thomas L. Schwarz ,  Matthew R. Banghart ,  Amos Gutnick

IPC: C07D401/12 ,  C07D401/14 ,  A61K41/00 ,  C07D473/18 ,  C07D239/49 ,  C07D239/47 ,  C07D405/14 ,  C07F15/00

CPC classification number: C07D401/12 ,  A61K41/0042 ,  C07D239/47 ,  C07D239/49 ,  C07D401/14 ,  C07D405/14 ,  C07D473/18 ,  C07F15/0053

Abstract: The instant invention provides photolysable compounds, and their use in reversible chemical induced dimerization and light-induced regulation of proteins.

Abstract translation: 本发明提供可光化的化合物，以及它们在可逆化学诱导的二聚化和光诱导的蛋白质调节中的用途。

公开(公告)号：US20160264531A1

公开(公告)日：2016-09-15

申请号：US15160885

申请日：2016-05-20

Applicant: Chimerix Inc.

Inventor： Roy Wendell Ware, JR. ,  Aaron Leigh Downey

IPC: C07D239/47

CPC classification number: C07D239/47 ,  C07F9/53 ,  C07F9/6512

Abstract: The disclosure describes methods of synthesis of phosphonate ester compounds. The methods according to the disclosure allow for large-scale preparation of phosphonate ester compounds having high purity and stability. Also disclosed are morphic forms of phosphonate ester compounds.

公开(公告)号：US09409887B2

公开(公告)日：2016-08-09

申请号：US14448578

申请日：2014-07-31

Applicant: Celgene Avilomics Research, Inc.

Inventor： Kwangho Lee ,  Deqiang Niu ,  Matthew F. Baevsky

IPC: C07D403/12 ,  C07D239/48 ,  C12N9/12 ,  A61K31/155 ,  A61K45/06 ,  C07D239/42 ,  C07D239/47

CPC classification number: C07D403/12 ,  A61K31/155 ,  A61K31/505 ,  A61K31/506 ,  A61K45/06 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C12N9/12 ,  C12Y207/10 ,  A61K2300/00

Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

Abstract translation: 本发明提供化合物，其药学上可接受的组合物及其使用方法。

公开(公告)号：US20160221965A1

公开(公告)日：2016-08-04

申请号：US15021372

申请日：2014-09-12

Applicant: BAYER PHARMA AKTIENGESELLSCHAFT

Inventor： Alexander STRAUB ,  Marie-Pierre COLLIN ,  Michael KOCH ,  Jutta MEYER ,  Karl-Heinz SCHLEMMER ,  Carl Friedrich NISING ,  Nicole BIBER ,  Sonja ANLAUF ,  Matthias Beat WITTWER

IPC: C07D239/47 ,  A61K45/06 ,  C07D401/12 ,  C07D239/56 ,  C07D239/36 ,  C07D401/06 ,  A61K31/513 ,  C07D239/52

CPC classification number: C07D239/47 ,  A61K31/513 ,  A61K45/06 ,  C07D239/36 ,  C07D239/52 ,  C07D239/54 ,  C07D239/545 ,  C07D239/56 ,  C07D401/06 ,  C07D401/12

Abstract: The present application relates to novel 2,5-disubstituted 6-(trifluoromethyl)pyrimidin-4(3H)-one derivatives, to processes for their preparation, to their use alone or in combinations for the treatment and/or prevention of diseases, and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for treatment and/or prevention of cardiovascular, renal, inflammatory and fibrotic diseases.

Abstract translation: 本申请涉及新的2,5-二取代的6-（三氟甲基）嘧啶-4（3H） - 酮衍生物，其制备方法单独使用或组合用于治疗和/或预防疾病，以及 用于制备用于治疗和/或预防疾病的药物，特别是用于治疗和/或预防心血管，肾，炎症和纤维化疾病。

公开(公告)号：US20160198711A1

公开(公告)日：2016-07-14

申请号：US15072035

申请日：2016-03-16

Applicant: DOW AGROSCIENCES LLC

Inventor： Beth Lorsbach ,  W. John Owen ,  Lindsay Stelzer ,  Chenglin Yao

IPC: A01N43/54 ,  A01N47/30 ,  C07D409/12 ,  C07D239/47

CPC classification number: C07D239/47 ,  A01N43/54 ,  A01N47/30 ,  A01N47/38 ,  C07D409/12 ,  A01N25/00

Abstract: This present disclosure is related to the field of to N-(substituted)-5-fluoro-4-imino-3-methyl-2-oxo-3,4-di-hydropyrimidme-1(2H)-carboxamide compounds and their derivatives and to the use of these compounds as fungicides. This application claims the benefit of U.S. Provisional Patent Application Ser. No. 61/1746,837 filed Dec. 28, 2012, which is expressly incorporated by reference herein. Background and Summary of the Invention Fungicides are compounds, of natural or synthetic origin, which act to protect and/or cure plants against damage caused by agriculturally relevant fungi. Generally, no single fungicide is useful in all situations. Consequently, research is ongoing to produce fungicides that may have better performance, are easier to use, and cost less.

Abstract translation: 本发明涉及N-（取代的）-5-氟-4-亚氨基-3-甲基-2-氧代-3,4-二氢嘧啶-2（2H） - 甲酰胺化合物及其衍生物的领域 以及这些化合物作为杀真菌剂的使用。 本申请要求美国临时专利申请 2012年12月28日提交的No.61 / 1746,837，其明确地通过引用并入本文。 背景技术杀真菌剂是天然或合成来源的化合物，其用于保护和/或治愈植物免受农业相关真菌引起的损害。 通常，在所有情况下，没有一种杀真菌剂是有用的。 因此，正在进行研究，以生产可能具有更好性能，更易于使用和更低成本的杀真菌剂。