公开(公告)号：US11739110B2

公开(公告)日：2023-08-29

申请号：US16675195

申请日：2019-11-05

Applicant: Feng-Wen Yen ,  Tsun-Yuan Huang

Inventor： Feng-Wen Yen ,  Tsun-Yuan Huang

IPC: C07D209/88 ,  C07F15/00 ,  C07C257/18 ,  C07D217/26 ,  C07D213/78 ,  H10K85/30 ,  H10K85/60 ,  H10K50/81 ,  H10K50/82

CPC classification number: C07F15/0033 ,  C07C257/18 ,  C07D209/88 ,  C07D213/78 ,  C07D217/26 ,  H10K85/342 ,  H10K85/615 ,  H10K85/654 ,  H10K85/6572 ,  H10K50/81 ,  H10K50/82

Abstract: A compound having a first ligand of the following




is described. Ring A represents a monocyclic aromatic group or a polycyclic aromatic group. Ring B represents a polycyclic aromatic group. Z is a carbon. Z and the right N are coordinated to a metal to form a five-membered chelate ring. R1 and R2 independently represent mono to a maximum possible number of substitutions, or no substitution.

公开(公告)号：US20200068886A1

公开(公告)日：2020-03-05

申请号：US16675336

申请日：2019-11-06

Applicant: Bayer CropScience Aktiengesellschaft

Inventor： Stefan HILLEBRAND ,  Mazen ES-SAYED ,  Ulrike WACHENDORFF-NEUMANN ,  Stephane BRUNET

IPC: A01N37/52 ,  C07C257/18 ,  C07C205/38 ,  C07C217/90 ,  C07C257/12

Abstract: The present invention relates to halogen-substituted phenoxyphenylamidines of the general formula (I), to a process for their preparation, to the use of the amidines according to the invention for controlling unwanted microorganisms and also to an agrochemical formulation for this purpose, comprising the halogen-substituted phenoxyphenylamidines according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms by applying the compounds according to the invention to the microorganisms and/or their habitat.

公开(公告)号：US20180036296A1

公开(公告)日：2018-02-08

申请号：US15466530

申请日：2017-03-22

Applicant: Millennium Pharmaceuticals, Inc.

Inventor： Bing-Yan Zhu ,  Penglie Zhang ,  Lingyan Wang ,  Wenrong Huang ,  Erick A. Goldman ,  Wenhao Li ,  Jingmei Zuckett ,  Yonghong Song ,  Robert M. Scarborough

IPC: A61K31/44 ,  A61K9/20 ,  A61K9/48 ,  A61K31/616 ,  A61K45/06 ,  C07C237/42 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C317/44 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D217/22 ,  C07D231/12 ,  C07D249/08 ,  C07C255/60 ,  C07C257/18 ,  C07C259/18 ,  C07D233/56 ,  C07D233/64 ,  C07D295/125 ,  C07D333/38 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14

CPC classification number: A61K31/44 ,  A61K9/20 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/48 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/616 ,  A61K45/06 ,  A61K2201/094 ,  C07C237/42 ,  C07C255/60 ,  C07C257/18 ,  C07C259/18 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C317/44 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D217/22 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D249/08 ,  C07D295/125 ,  C07D333/38 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14

Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.

公开(公告)号：US20170349538A1

公开(公告)日：2017-12-07

申请号：US15683739

申请日：2017-08-22

Applicant: Human BioMolecular Research Foundation

Inventor： John R. Cashman ,  Jaroslaw Kalisiak

IPC: C07C251/40 ,  C07D239/06 ,  C07C279/12 ,  C07C257/12 ,  C07C257/18 ,  C07C257/14 ,  C07D249/04 ,  C07D233/24

CPC classification number: C07C251/40 ,  C07C257/12 ,  C07C257/14 ,  C07C257/18 ,  C07C279/12 ,  C07D233/24 ,  C07D239/06 ,  C07D249/04

Abstract: The invention describes pharmaceutical agents capable of crossing the blood brain barrier to protect against organophosphate pesticides and nerve agents or other electrophiles by reactivating inhibited cholinesterase (i.e., acetylcholinesterase and butyrylcholinesterase) and other proteins in the peripheral and central nervous system.

公开(公告)号：US09533947B2

公开(公告)日：2017-01-03

申请号：US14292087

申请日：2014-05-30

Applicant: Northwestern University ,  The General Hospital Corporation

Inventor： Richard B. Silverman ,  Hua Wang ,  Mohammad Khanfar ,  Aleksey G. Kazantsev

IPC: C07C311/16 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D213/85 ,  C07D207/04 ,  C07D317/48 ,  C07D237/20 ,  C07D271/113 ,  C07C255/60 ,  C07C257/18 ,  C07C323/49 ,  C07D217/04 ,  C07D207/16 ,  C07D295/26 ,  C07D305/06 ,  C07C311/21 ,  C07C311/29 ,  C07C317/44 ,  C07C317/48 ,  C07D213/76 ,  C07D213/80 ,  C07D223/04 ,  C07D239/42 ,  C07D261/14 ,  C07D277/46 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C323/62 ,  C07C311/47 ,  C07C317/22 ,  C07C317/34 ,  C07C323/20 ,  C07C323/42 ,  C07C235/60

CPC classification number: C07C311/21 ,  C07B2200/07 ,  C07C235/60 ,  C07C255/60 ,  C07C257/18 ,  C07C311/16 ,  C07C311/29 ,  C07C311/46 ,  C07C311/47 ,  C07C317/22 ,  C07C317/34 ,  C07C317/40 ,  C07C317/44 ,  C07C317/48 ,  C07C323/20 ,  C07C323/42 ,  C07C323/49 ,  C07C323/62 ,  C07C2601/02 ,  C07D207/16 ,  C07D213/75 ,  C07D213/76 ,  C07D213/80 ,  C07D213/81 ,  C07D213/82 ,  C07D213/85 ,  C07D217/04 ,  C07D223/04 ,  C07D237/20 ,  C07D239/42 ,  C07D261/14 ,  C07D271/113 ,  C07D277/46 ,  C07D295/26 ,  C07D305/06 ,  C07D311/16 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

Abstract: Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease.

Abstract translation: 苯甲酰胺化合物及其衍生物，可用于选择性抑制SIRT2酶和/或用于治疗亨廷顿病的治疗用途。

公开(公告)号：US09108922B2

公开(公告)日：2015-08-18

申请号：US14175087

申请日：2014-02-07

Applicant: Millennium Pharmaceuticals, Inc.

Inventor： Bing-Yan Zhu ,  Wenrong Huang

IPC: C07D213/75 ,  A61K31/44 ,  C07C237/42 ,  C07C255/60 ,  C07C257/18 ,  C07C259/18 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C317/44 ,  C07D213/81 ,  C07D213/82 ,  C07D217/22 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D249/08 ,  C07D295/125 ,  C07D333/38 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14 ,  A61K31/616 ,  A61K45/06

CPC classification number: A61K31/44 ,  A61K9/20 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/48 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/616 ,  A61K45/06 ,  A61K2201/094 ,  C07C237/42 ,  C07C255/60 ,  C07C257/18 ,  C07C259/18 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C317/44 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D217/22 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D249/08 ,  C07D295/125 ,  C07D333/38 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14

Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.

公开(公告)号：US20120197016A1

公开(公告)日：2012-08-02

申请号：US13278465

申请日：2011-10-21

Applicant: Leo Timothy Laughlin, II ,  Tomohiro Hakozaki ,  Wenzhu Zhao ,  Jiazhen Wang ,  John Crist Bierman

Inventor： Leo Timothy Laughlin, II ,  Tomohiro Hakozaki ,  Wenzhu Zhao ,  Jiazhen Wang ,  John Crist Bierman

IPC: C12Q1/02 ,  C07C257/18 ,  C07C233/51 ,  C07D471/10 ,  C07D405/14 ,  C07D209/88 ,  C07D459/00 ,  G01N21/64 ,  C07C229/52

CPC classification number: G01N33/566 ,  G01N2500/10

Abstract: Embodiments of screening methods for determining test agents effective for modifying the appearance of pigmented skin are provided. The screening method may comprise the steps of contacting a cell, a cell culture, or bulk cells with the test agent, wherein the cell, the cell culture, or the bulk cells comprise ADRβ1 receptors, and determining based on the binding interaction of the test agent with the ADRβ1 receptors whether the test agent is an effective ADRβ1 receptor antagonist suitable for modifying the appearance of pigmented skin, wherein a test agent is considered to be an effective ADRβ1 receptor antagonist when it defines a half maximal inhibitory concentration of less than about 1000 ppm.

Abstract translation: 提供了用于确定有效改善着色皮肤外观的试验剂的筛选方法的实施方案。 筛选方法可以包括使细胞，细胞培养物或体细胞与测试试剂接触的步骤，其中细胞，细胞培养物或体细胞包含ADR和bgr1受体，并且基于 具有ADR＆bgr.1受体的测试剂是否是测试剂是适合于改变着色皮肤外观的有效ADR＆bgr1受体拮抗剂，其中测试剂被认为是有效ADR＆bgr1受体拮抗剂，当它定义一半 最大抑制浓度小于约1000ppm。

公开(公告)号：US20110301109A1

公开(公告)日：2011-12-08

申请号：US13139156

申请日：2009-12-10

Applicant: Zheng Liu ,  Jianfeng Li ,  Xiaojun Yang ,  Zhen Wang ,  Jinfeng Zhang ,  Yi Zhu ,  Guanghui Tian ,  Qing Jin ,  Jingkang Shen ,  Weiliang Zhu ,  Hualiang Jiang ,  Jingshan Shen

Inventor： Zheng Liu ,  Jianfeng Li ,  Xiaojun Yang ,  Zhen Wang ,  Jinfeng Zhang ,  Yi Zhu ,  Guanghui Tian ,  Qing Jin ,  Jingkang Shen ,  Weiliang Zhu ,  Hualiang Jiang ,  Jingshan Shen

IPC: A61K31/7068 ,  C07H7/06 ,  C07D239/36 ,  A61K31/513 ,  C07H15/26 ,  C07D401/12 ,  C07D413/12 ,  A61K31/5377 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  A61K31/55 ,  C07D413/10 ,  C07C257/18 ,  A61P11/06 ,  A61P15/00 ,  A61P13/08 ,  A61P15/10 ,  A61P9/12 ,  A61P9/00 ,  A61P29/00 ,  C07D403/12

CPC classification number: A61K31/505 ,  C07D239/36 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07H15/26

Abstract: The present invention relates to a class of phenylpyrimidone compounds, the pharmaceutical composition, the preparation method and the use thereof. More specifically, the present invention relates to a type of phenylpyrimidone compounds of the following formula I, the pharmaceutically acceptable salts or solvates thereof and to the pharmaceutical composition as well as the preparation method of the compounds. The compounds of formula I according to the present invention can effectively inhibit type V phosphodiesterase (PDE5), and thus can be used for the treatment of various vascular disorders, such as male erectile dysfunction, pulmonary hypertension and the like.

Abstract translation: 本发明涉及一类苯基嘧啶酮化合物，药物组合物，其制备方法及用途。 更具体地，本发明涉及一种下式I的苯基嘧啶酮化合物，其药学上可接受的盐或溶剂化物以及该药物组合物以及该化合物的制备方法。 根据本发明的式I化合物可以有效抑制V型磷酸二酯酶（PDE5），从而可用于治疗各种血管疾病，如男性勃起功能障碍，肺动脉高压等。

公开(公告)号：US20100092402A1

公开(公告)日：2010-04-15

申请号：US12524506

申请日：2008-01-25

Applicant: Roderick Lindsay Hall ,  Peter John Cole

Inventor： Roderick Lindsay Hall ,  Peter John Cole

IPC: A61K31/24 ,  A61K39/00 ,  A61P11/00 ,  A61K9/12 ,  C07C257/18

CPC classification number: A61K31/245 ,  A61K31/216 ,  A61K31/24

Abstract: The invention relates to the use of amidino compounds in the manufacture and formulation of medicaments for the treatment of respiratory diseases.

Abstract translation: 本发明涉及脒基化合物在制备和制备用于治疗呼吸系统疾病的药物中的用途。

公开(公告)号：US07667077B2

公开(公告)日：2010-02-23

申请号：US11853951

申请日：2007-09-12

Applicant: H. V. Rasika Dias ,  Lorraine G. Van Waasbergen ,  Jaime A. Flores

Inventor： H. V. Rasika Dias ,  Lorraine G. Van Waasbergen ,  Jaime A. Flores

IPC: C07C251/00 ,  C07C257/14 ,  C07C257/18 ,  A61K31/155 ,  A61K31/13

CPC classification number: C07C257/14 ,  A01N35/10 ,  A01N55/02 ,  A01N59/16 ,  A01N59/20 ,  A01N2300/00

Abstract: A new class of fluorinated or polyhalogenated triazapentadienes are disclosed. The synthesized triazapentadienes are thermally stable, soluble in typical solvents and have several metal binding sites for complexation with metal ions. The compounds are prepared as colorless crystalline solids. Synthesis takes advantage of a reaction with triethylamine. Synthesized triazapentadienes (with and without complexed metals) inhibit bacterial growth of both Gram positive and Gram-negative bacteria.

Abstract translation: 公开了一类新的氟化或多卤代三氮代二烯。 合成的三氮杂二烯是热稳定的，可溶于典型的溶剂，并具有几个与金属离子络合的金属结合位点。 化合物制备为无色结晶固体。 合成利用与三乙胺的反应。 合成的三氮代二烯（有和没有复合金属）抑制革兰氏阳性和革兰氏阴性细菌的细菌生长。