公开(公告)号：US20240300901A1

公开(公告)日：2024-09-12

申请号：US18274354

申请日：2022-01-26

Applicant: FMC Corporation ,  FMC AGRO SINGAPORE PTE. LTD.

Inventor： Yanchun CAO ,  Zhijian XU ,  Xin LIU

IPC: C07D231/16 ,  C07D401/04

CPC classification number: C07D231/16 ,  C07D401/04

Abstract: Described herein are novel methods of synthesizing 5-Bromo-2-(3-chloro-pyridin-2-yl)-2H-pyrazole-3-carboxylic acid from pyrazole or pyrazole derivatives.

公开(公告)号：US20230277505A1

公开(公告)日：2023-09-07

申请号：US18079941

申请日：2022-12-13

Applicant: Arena Pharmaceuticals, Inc.

Inventor： Bradley Teegarden ,  Honnappa Jayakumar ,  Hongmei Li ,  Sonja Strah-Pleynet ,  Peter I. Dosa

IPC: A61K31/415 ,  C07D231/12 ,  C07D231/16 ,  C07D405/12 ,  C07D401/12 ,  A61K31/4155 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377

CPC classification number: A61K31/415 ,  C07D231/12 ,  C07D231/16 ,  C07D405/12 ,  C07D401/12 ,  A61K31/4155 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377

Abstract: The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor.




Compounds and pharmaceutical compositions thereof are directed to methods useful in the prophylaxis or treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders and the like.
The present invention also relates to the method of prophylaxis or treatment of 5-HT2A serotonin receptor mediated disorders in combination with a dopamine D2 receptor antagonist such as haloperidol, administered separately or together.

公开(公告)号：US20230271934A1

公开(公告)日：2023-08-31

申请号：US18020317

申请日：2021-08-24

Applicant: Jie LI ,  Avihai YACOVAN ,  Bob CHEN ,  Adama Makhteshim Ltd.

Inventor： Jie Li ,  Avihai Yacovan ,  Bob Chen

IPC: C07D401/04 ,  C07D231/16

CPC classification number: C07D401/04 ,  C07D231/16

Abstract: The present invention relates to the processes for the preparation of substituted pyrazole derivatives of formula (I), (II), (III), (IV), (IV-a) (V), (VII), which are useful as intermediates in anthranilamide insecticides production. In addition, the present invention is directed to a method for the preparation of anthranilamides of formula (VIII) using substituted pyrazole derivatives of formula (I), (III), (IV), (V), (VII). Furthermore, the present invention is directed to substituted halo-pyrazole compounds of formula (III), (IV) and (V), wherein X is halogen and R7 is hydrogen, C1-C4 alkyl.

公开(公告)号：US20190099402A1

公开(公告)日：2019-04-04

申请号：US16144330

申请日：2018-09-27

Applicant: ARENA PHARMACEUTICALS, INC.

Inventor： Lee Alani SELVEY ,  Marlon CARLOS ,  Paul MAFFUID ,  Yun SHAN ,  William L. BETTS, III ,  Deam Windate GIVEN, III ,  Ryan M. HART ,  Zezhi Jesse SHAO

IPC: A61K31/415 ,  A61K9/20 ,  C07D231/16 ,  A61K9/16

CPC classification number: A61K31/415 ,  A61K9/1635 ,  A61K9/2027 ,  A61K9/2054 ,  C07D231/16

Abstract: The present invention relates to certain compositions of a 5-HT2A serotonin receptor modulator and methods for their preparation. The compositions disclosed herein are useful for increasing slow wave sleep, improving sleep consolidation, improving sleep maintenance and improving sleep quality, and for treating insomnia and related sleep disorders, dyssomnias, parasomnias and nonrestorative sleep and the like. The compositions disclosed herein are further useful for treating platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, thrombosis, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders and progressive multifocal leukoencephalopathy and the like.

公开(公告)号：US09957256B2

公开(公告)日：2018-05-01

申请号：US15313343

申请日：2015-05-26

Applicant: BAYER CROPSCIENCE AKTIENGESELLSCHAFT

Inventor： Sergii Pazenok ,  Norbert Lui ,  Christian Funke

IPC: C07D403/04 ,  C07D231/16 ,  C07D231/14 ,  C07C21/18 ,  C07D401/14 ,  C07D231/38

CPC classification number: C07D403/04 ,  C07C21/18 ,  C07D231/14 ,  C07D231/16 ,  C07D231/38 ,  C07D401/14

Abstract: A new process for the preparation of 5-fluoro-1H-pyrazoles of the general formula (I) as described herein and further reactions with this compound.

公开(公告)号：US20180085351A1

公开(公告)日：2018-03-29

申请号：US15718886

申请日：2017-09-28

Applicant: ARENA PHARMACEUTICALS, INC

Inventor： Lee Alani SELVEY ,  Marlon CARLOS ,  Paul MAFFUID ,  Yun SHAN ,  William L. BETTS, III ,  Deam Windate GIVEN, III ,  Ryan M. HART ,  Zezhi Jesse SHAO

IPC: A61K31/415 ,  A61K9/20 ,  A61K9/16 ,  C07D231/16

CPC classification number: A61K31/415 ,  A61K9/1635 ,  A61K9/2027 ,  A61K9/2054 ,  C07D231/16

Abstract: The present invention relates to certain compositions of a 5-HT2A serotonin receptor modulator and methods for their preparation. The compositions disclosed herein are useful for increasing slow wave sleep, improving sleep consolidation, improving sleep maintenance and improving sleep quality, and for treating insomnia and related sleep disorders, dyssomnias, parasomnias and nonrestorative sleep and the like. The compositions disclosed herein are further useful for treating platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, thrombosis, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders and progressive multifocal leukoencephalopathy and the like.

公开(公告)号：US20180072680A1

公开(公告)日：2018-03-15

申请号：US15681766

申请日：2017-08-21

Applicant: Arena Pharmaceuticals, Inc.

Inventor： Marlon CARLOS ,  Weitong DONG ,  Mark MACIAS ,  Suzanne Michiko SATO ,  Lee Alani SELVEY

IPC: C07D231/12 ,  C07D231/16

CPC classification number: A61K31/415 ,  C07D231/12 ,  C07D231/16

Abstract: The present invention is directed to processes and intermediates useful for the preparation of 1-[3-(4-bromo-2-N methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea (Compound I), crystalline forms and solvate forms thereof; and compositions comprising 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea, crystalline forms and solvate forms thereof prepared by processes as described herein.

公开(公告)号：US20180029991A1

公开(公告)日：2018-02-01

申请号：US15551401

申请日：2016-05-04

Applicant: SHENYANG SINOCHEM AGROCHEMICALS R&D CO., LTD

Inventor： Liang LV ,  Gang WANG ,  Zhonggang SHAN ,  Jiyong LIU ,  Qin SUN ,  Junfeng WANG ,  Bin LI

IPC: C07D231/16 ,  C07D277/56 ,  A01N43/78 ,  A01N43/56

CPC classification number: C07D231/16 ,  A01N43/56 ,  A01N43/78 ,  C07D231/14 ,  C07D277/56

Abstract: The present invention belongs to the field of fungicides, and relates to an amide compound and the preparation method and use thereof. The amide compound is as shown in general formula I: Each substituent in Formula I is defined in the description. The compound of general formula I of the present invention has an outstanding fungicidal activity, and can be used for controlling fungal diseases.

公开(公告)号：US09878985B2

公开(公告)日：2018-01-30

申请号：US15031456

申请日：2014-10-28

Applicant: BAYER CROPSCIENCE AKTIENGESELLSCHAFT

Inventor： Christophe Dubost ,  Ulrike Wachendorff-Neumann ,  Philipp Winter ,  Stephane Brunet ,  Jean-Pierre Vors ,  Cyril Montagne

IPC: C07D231/16 ,  A01N43/40 ,  A01N43/56 ,  A01N45/00 ,  C07C211/60 ,  C07D213/82 ,  C07C211/61 ,  C07C25/22 ,  C07C17/23 ,  C07C17/275 ,  C07C209/62 ,  C07D231/14

CPC classification number: C07D231/16 ,  A01N43/40 ,  A01N43/56 ,  A01N45/00 ,  C07C17/23 ,  C07C17/275 ,  C07C25/22 ,  C07C209/62 ,  C07C211/60 ,  C07C211/61 ,  C07C2602/06 ,  C07C2603/94 ,  C07D213/82 ,  C07D231/14

Abstract: The present invention relates to novel benzocyclobutane(thio) carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.

公开(公告)号：US20170367341A1

公开(公告)日：2017-12-28

申请号：US15540291

申请日：2016-01-22

Applicant: KYOYU AGRI CO., LTD.

Inventor： Ken MATSUBARA ,  Makoto NIINO

IPC: A01N43/90 ,  A01N43/56 ,  C07D231/54 ,  C07D231/16

CPC classification number: A01N43/90 ,  A01N43/56 ,  C07D231/16 ,  C07D231/54 ,  C07D471/04

Abstract: Provided is a compound capable of effectively control worst weeds of higher leaf stages that present practical problems. A specific pyrazolylpyrazole derivative of formula (I) is disclosed that is able to solve the above-mentioned problems.