公开(公告)号：US20230303498A1

公开(公告)日：2023-09-28

申请号：US17999249

申请日：2021-05-14

申请人： SYNGENTA CROP PROTECTION AG

发明人： Suzanna Jane DALE ,  Zoe Jane ANDERSON ,  Louisa WHALLEY ,  Gordon Richard MUNNS ,  James Alan MORRIS ,  Paul Matthew BURTON

IPC分类号： C07D237/28 ,  A01N43/58 ,  A01N25/32 ,  A01P13/00 ,  C07D413/04 ,  A01N43/76 ,  A01N43/80 ,  C07D403/04 ,  A01N43/647 ,  A01N43/84 ,  C07D405/04

CPC分类号： C07D237/28 ,  A01N43/58 ,  A01N25/32 ,  A01P13/00 ,  C07D413/04 ,  A01N43/76 ,  A01N43/80 ,  C07D403/04 ,  A01N43/647 ,  A01N43/84 ,  C07D405/04

摘要： Compounds of the Formula (I) wherein the substituents are as defined in claim 1. The invention further relates to herbicidal compositions which comprise a compound of Formula (I) and to the use of compounds of Formula (I) for controlling weeds, in particular in crops of useful plants.

公开(公告)号：US20220098160A1

公开(公告)日：2022-03-31

申请号：US17052078

申请日：2019-02-28

申请人： BIOCAD

发明人： Aleksei Leonidovich MINDICH ,  Svetlana Leonidovna GORBUNOVA ,  Aleksandra Vladimirovna POPKOVA ,  Artsiom Evgenievich SHEKHAUTSOU ,  Andrei Ivanovich ALAFINOV ,  Mariia Andreevna KASATKINA ,  Natalia Vladimirovna KOZHEMYAKINA ,  Anna Sergeevna KUSHAKOVA ,  Elena Aleksandrovna MAKSIMENKO ,  Leonid Evgen`evich MIKHAYLOV ,  Mariia Sergeevna MISHINA ,  Anna Jur'evna CHESTNOVA ,  Dmitry Valentinovich MOROZOV

IPC分类号： C07D239/80 ,  A61P35/00 ,  C07D239/95 ,  C07D237/28 ,  C07D215/48 ,  C07D471/04

摘要： The present invention relates to novel compounds of formula (1), which have the properties of a CDK8/19 inhibitor, and to a pharmaceutical composition containing said compounds, and to the use of said compounds and composition as pharmaceutical preparations for treating diseases or disorders.

公开(公告)号：US10934276B2

公开(公告)日：2021-03-02

申请号：US16469972

申请日：2017-12-15

申请人： Vanderbilt University

发明人： Craig W. Lindsley ,  P. Jeffrey Conn ,  Darren W. Engers ,  Julie L. Engers ,  Madeline F. Long

IPC分类号： C07D401/14 ,  A61P25/28 ,  C07D237/28 ,  C07D403/12 ,  C07D403/14

摘要： Disclosed herein are 2,4-dimethylquinoline-6-carboxamide compounds and 3,4-dimethylcinnoline-6-carboxamide compounds, which may be useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4(mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.

公开(公告)号：US20200079756A1

公开(公告)日：2020-03-12

申请号：US16469972

申请日：2017-12-15

申请人： Vanderbilt University

发明人： Craig W. Lindsley ,  P. Jeffrey Conn ,  Darren W. Engers ,  Julie L. Engers ,  Madeline F. Long

IPC分类号： C07D401/14 ,  C07D237/28 ,  C07D403/14 ,  C07D403/12 ,  A61P25/28

摘要： Disclosed herein are 2,4-dimethylquinoline-6-carboxamide compounds and 3,4-dimethylcinnoline-6-carboxamide compounds, which may be useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4(mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.

公开(公告)号：US09732061B2

公开(公告)日：2017-08-15

申请号：US14992464

申请日：2016-01-11

申请人： Janssen Pharmaceutica NV

发明人： Mark Joseph Macielag ,  Yue-Mei Zhang ,  Bart L. DeCorte ,  Michael N. Greco ,  Donald W. Ludovici ,  Michael H. Parker

IPC分类号： C07D401/12 ,  C07D409/14 ,  C07D405/14 ,  C07D417/14 ,  C07D401/04 ,  C07D403/12 ,  C07D237/28

CPC分类号： C07D401/12 ,  C07D237/28 ,  C07D401/04 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

摘要： The present invention is directed to cinnoline derivatives pharmaceutical compositions containing them and their use in the treatment of disorders and conditions mediated by the CB-1 receptor; more particularly, use in the treatment of disorders and conditions responsive to inverse agonism of the CB-1 receptor. More particularly, the compounds of the present invention are useful in the treatment of metabolic disorders.

公开(公告)号：US09708286B2

公开(公告)日：2017-07-18

申请号：US14748925

申请日：2015-06-24

申请人： LEO Laboratories Limited

发明人： Gunnar Grue-Sørensen ,  Xifu Liang ,  Thomas Högberg ,  Kristoffer Månsson ,  Per Vedsø ,  Thomas Vifian

IPC分类号： C07C271/34 ,  C07D333/38 ,  C07C271/36 ,  C07C271/38 ,  C07D249/06 ,  C07D261/18 ,  C07D277/32 ,  C07D295/21 ,  C07D309/08 ,  C07D401/04 ,  C07D471/04 ,  C07D495/04 ,  C07D265/36 ,  C07D271/08 ,  C07D277/587 ,  C07D295/205 ,  C07D307/00 ,  C07D307/94 ,  C07D405/06 ,  C07D513/04 ,  A61K31/365 ,  A61K31/381 ,  A61K31/404 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/472 ,  A61K31/502 ,  A61K31/5375 ,  A61K31/538 ,  C07D209/42 ,  C07D217/26 ,  C07D231/14 ,  C07D231/56 ,  C07D237/28 ,  C07D249/04

CPC分类号： C07D261/18 ,  A61K31/365 ,  A61K31/381 ,  A61K31/404 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/472 ,  A61K31/502 ,  A61K31/5375 ,  A61K31/538 ,  C07C271/34 ,  C07C271/36 ,  C07C271/38 ,  C07C2603/86 ,  C07D209/08 ,  C07D209/42 ,  C07D213/79 ,  C07D215/50 ,  C07D217/26 ,  C07D231/14 ,  C07D231/56 ,  C07D233/90 ,  C07D237/28 ,  C07D239/28 ,  C07D249/04 ,  C07D249/06 ,  C07D261/20 ,  C07D263/34 ,  C07D265/36 ,  C07D271/08 ,  C07D277/32 ,  C07D277/56 ,  C07D277/587 ,  C07D295/182 ,  C07D295/205 ,  C07D295/21 ,  C07D307/00 ,  C07D307/68 ,  C07D307/94 ,  C07D309/08 ,  C07D333/38 ,  C07D333/40 ,  C07D401/04 ,  C07D405/06 ,  C07D471/04 ,  C07D493/08 ,  C07D495/04 ,  C07D513/04

摘要： The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.

公开(公告)号：US20160257674A1

公开(公告)日：2016-09-08

申请号：US14392304

申请日：2014-09-23

申请人： CHDI FOUNDATION, INC.

发明人： Celia Dominguez ,  Leticia M. Toledo-Sherman ,  Michael Prime ,  William Mitchell ,  Naomi Went

IPC分类号： C07D413/12 ,  C07D277/64 ,  C07D217/02 ,  C07D239/74 ,  C07D237/28 ,  C07D241/42 ,  C07D263/56 ,  C07D235/08 ,  C07D209/08 ,  C07D231/56 ,  C07D261/20 ,  C07D407/12 ,  C07D333/28 ,  C07D333/10 ,  C07D277/24 ,  C07D307/79

CPC分类号： C07D413/12 ,  C07D209/08 ,  C07D213/46 ,  C07D215/18 ,  C07D217/02 ,  C07D231/56 ,  C07D235/08 ,  C07D237/28 ,  C07D239/74 ,  C07D241/42 ,  C07D261/20 ,  C07D263/56 ,  C07D277/24 ,  C07D277/64 ,  C07D307/79 ,  C07D319/18 ,  C07D333/06 ,  C07D333/10 ,  C07D333/28 ,  C07D407/12

摘要： Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

公开(公告)号：US09403802B2

公开(公告)日：2016-08-02

申请号：US14382390

申请日：2013-02-28

申请人： Takeda Pharmaceutical Company Limited

发明人： Hiroki Sakamoto ,  Takahiro Sugimoto

IPC分类号： C07D401/14 ,  C07D209/12 ,  C07D401/04 ,  C07D405/12 ,  C07D215/56 ,  C07D401/10 ,  C07D401/12 ,  C07D237/28 ,  C07D401/06 ,  C07D403/10

CPC分类号： C07D405/12 ,  C07D215/56 ,  C07D237/28 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10

摘要： The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity, and useful as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, a sleep disorder and the like. The present invention relates to a compound represented by the formula (I): wherein R1 is an optionally substituted amino group or an optionally substituted cyclic amino group, R2 and R3 are each independently a hydrogen atom or a substituent, X is —CH═ or —N═, and ring A is an optionally substituted 5- to 10-membered ring, or a salt thereof.

摘要翻译： 本发明提供具有胆碱能毒蕈碱M1受体阳性变构调节剂活性的化合物，可用作阿尔茨海默病，精神分裂症，疼痛，睡眠障碍等的预防或治疗药物。 本发明涉及由式（I）表示的化合物：其中R 1为任选取代的氨基或任选取代的环状氨基，R 2和R 3各自独立地为氢原子或取代基，X为-CH =或 -N =，环A为任选取代的5至10元环或其盐。

公开(公告)号：US09090561B2

公开(公告)日：2015-07-28

申请号：US13614838

申请日：2012-09-13

申请人： Yihan Wang ,  Xiaotian Zhu ,  Rajeswari Sundaramoorthi ,  Wei-Sheng Huang ,  Dong Zou ,  R. Mathew Thomas ,  Jiwei Qi ,  Jan Antoinette C. Romero ,  David C. Dalgarno ,  William C. Shakespeare ,  Tomi K. Sawyer ,  Chester A. Metcalf, III

发明人： Yihan Wang ,  Xiaotian Zhu ,  Rajeswari Sundaramoorthi ,  Wei-Sheng Huang ,  Dong Zou ,  R. Mathew Thomas ,  Jiwei Qi ,  Jan Antoinette C. Romero ,  David C. Dalgarno ,  William C. Shakespeare ,  Tomi K. Sawyer ,  Chester A. Metcalf, III

IPC分类号： C07D471/04 ,  A61K31/4375 ,  C07D213/56 ,  C07D213/73 ,  C07D213/75 ,  C07D213/78 ,  C07D217/14 ,  C07D217/22 ,  C07D237/20 ,  C07D237/28 ,  C07D239/26 ,  C07D241/12 ,  C07D241/20 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/06 ,  C07D413/12 ,  C07D417/12

CPC分类号： C07D213/56 ,  C07D213/73 ,  C07D213/75 ,  C07D213/78 ,  C07D217/14 ,  C07D217/22 ,  C07D237/20 ,  C07D237/28 ,  C07D239/26 ,  C07D241/12 ,  C07D241/20 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/06 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04

摘要： This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.

摘要翻译： 本发明涉及以下通式的化合物：其中可变基团如本文所定义，及其制备和用途。

公开(公告)号：US08865709B2

公开(公告)日：2014-10-21

申请号：US14034718

申请日：2013-09-24

申请人： Neosome Life Sciences, LLC

发明人： Laxman S. Desai ,  Srinivas Chittaboina

IPC分类号： A61K31/421 ,  A61K31/4725 ,  A61K31/426 ,  A61K31/506 ,  A61P35/00 ,  A61P1/16 ,  A61P9/10 ,  A61P37/06 ,  A61P3/00 ,  A61P17/06 ,  A61P3/10 ,  A61P17/02 ,  A61P29/00 ,  A61P25/28 ,  C07D263/48 ,  C07D413/10 ,  C07D277/42 ,  C07D417/14 ,  C07D417/02 ,  C07D237/28 ,  C07D237/30 ,  C07D241/38 ,  C07D239/74 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07D487/04 ,  C07D413/04 ,  C07D295/135 ,  C07D401/04

CPC分类号： C07D487/04 ,  C07D263/48 ,  C07D277/42 ,  C07D295/135 ,  C07D401/04 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04

摘要： Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.

摘要翻译： 描述恶唑衍生物。 本发明化合物可用作激酶抑制剂，可用于治疗癌症，例如前列腺癌，肺癌，乳腺癌，结肠癌，白血病，CNS癌，黑素瘤，卵巢癌和肾癌。