公开(公告)号：US11312688B2

公开(公告)日：2022-04-26

申请号：US16903646

申请日：2020-06-17

申请人： Sumitomo Dainippon Pharma Co., Ltd.

发明人： Izumi Sasaki ,  Tomohiro Toyoda ,  Hidefumi Yoshinaga ,  Itaru Natsutani ,  Yoko Takahashi

IPC分类号： C07D231/20 ,  C07D231/18 ,  C07D231/38 ,  C07D405/06 ,  C07D493/08 ,  C07D231/22 ,  C07D231/44

摘要： The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT2C inverse agonistic action comprising Compound (1): or a pharmaceutically acceptable salt thereof wherein R1, R2, R3 and R4 are independently hydrogen or C1-6 alkyl etc.; R5 is C4-7 alkyl or —(CR8R9)r-E; R6, R7, R8 and R9 are independently hydrogen, fluorine or C1-6 alkyl; A is C6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C3-8 cycloalkyl or C6-10 aryl etc.; L is oxygen, sulfur or —NR10—; n is 1, 2 or 3; R10 is hydrogen or C1-6 alkyl etc.; and X is hydrogen or halogen etc.

公开(公告)号：US20210355127A1

公开(公告)日：2021-11-18

申请号：US17237656

申请日：2021-04-22

申请人： ASTRAZENECA AB

发明人： Johan Olof Broddefalk ,  Hans Fredrik Emtenäs ,  Kenneth Lars Granberg ,  Malin Anita Lemurell ,  Daniel Tor Pettersen ,  Alleyn Thomas Plowright ,  Lars Johan Andreas Ulander

IPC分类号： C07D487/04 ,  C07D231/40 ,  C07D231/44 ,  C07D231/50 ,  C07D413/12 ,  C07D417/12 ,  C07D498/04 ,  A61P9/10 ,  A61P9/00 ,  A61K31/4155 ,  A61K31/4985

摘要： The present application relates to novel compounds of formula (I) to their utility in treating and/or preventing clinical conditions including cardiovascular diseases (CVD), to methods for their therapeutic use, to pharmaceutical compositions containing them and to processes for preparing such compounds.

公开(公告)号：US20200339541A1

公开(公告)日：2020-10-29

申请号：US16925738

申请日：2020-07-10

申请人： BEIJING INNOCARE PHARMA TECH CO., LTD.

发明人： Xiangyang Chen ,  Yingxiang Gao ,  Norman Xianglong Kong

IPC分类号： C07D401/14 ,  A61P35/00 ,  C07D403/04 ,  C07D403/06 ,  A61K31/454 ,  A61K31/4155 ,  C07D401/04 ,  A61K31/415 ,  C07D401/06 ,  C07D231/14 ,  C07D231/44 ,  C07D405/14

摘要： The present invention relates to an alkynyl-substituted heterocyclic compound acting as an FGFR inhibitor, a preparation method therefor and a medical use thereof. In particular, the present invention relates to a compound as shown in general formula (I) and a pharmaceutically acceptable salt thereof; a pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof; a method for treating and/or preventing FGFR-associated diseases, particularly tumors, by using the compound or a pharmaceutically acceptable salt thereof; and a preparation method for the compound or a pharmaceutically acceptable salt thereof. The present invention also relates to the use of the compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof in the preparation of a drug for treating and/or preventing FGFR-associated diseases, particularly tumors, wherein the definition of each substituent group in general formula (I) is the same as that in the description.

公开(公告)号：US20190210997A1

公开(公告)日：2019-07-11

申请号：US16353806

申请日：2019-03-14

申请人： BEIJING INNOCARE PHARMA TECH CO., LTD.

发明人： Xiangyang Chen ,  Yingxiang Gao ,  Norman Xianglong Kong

IPC分类号： C07D401/14 ,  C07D231/44 ,  C07D405/14 ,  A61P35/00

摘要： The present invention relates to an alkynyl-substituted heterocyclic compound acting as an FGFR inhibitor, a preparation method therefor and a medical use thereof. In particular, the present invention relates to a compound as shown in general formula (I) and a pharmaceutically acceptable salt thereof; a pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof; a method for treating and/or preventing FGFR-associated diseases, particularly tumors, by using the compound or a pharmaceutically acceptable salt thereof; and a preparation method for the compound or a pharmaceutically acceptable salt thereof. The present invention also relates to the use of the compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof in the preparation of a drug for treating and/or preventing FGFR-associated diseases, particularly tumors, wherein the definition of each substituent group in general formula (I) is the same as that in the description.

公开(公告)号：US20190152921A1

公开(公告)日：2019-05-23

申请号：US16257452

申请日：2019-01-25

申请人： Anat Levin ,  Michael Grabarnick

发明人： Anat Levin ,  Michael Grabarnick

IPC分类号： C07D231/44

摘要： An improved oxidation process for preparing 5-amino-3-cyano-1-(2,6-dichloro-4-trifluoromethylphenyl)-4-trifluoromethylsulphinyl-pyrazole, of formula (I) is described. The process includes admixing 5-amino-3-cyano-1-(2, 6-dichloro-4-trifluoromethylphenyl)-4-trifluoromethylthiopyrazole of formula (II) with dichloroacetic acid and hydrogen peroxide in the presence of a strong acid.

公开(公告)号：US09913473B2

公开(公告)日：2018-03-13

申请号：US13459890

申请日：2012-04-30

申请人： Heidi Emilia Saxell ,  Peter Erk ,  Claude Taranta ,  Thomas Kröhl ,  Gerhard Cox ,  Martin Sukopp ,  Gautam R. Desiraju ,  Rahul Banerjee ,  Prashant M. Bhatt

发明人： Heidi Emilia Saxell ,  Peter Erk ,  Claude Taranta ,  Thomas Kröhl ,  Gerhard Cox ,  Martin Sukopp ,  Gautam R. Desiraju ,  Rahul Banerjee ,  Prashant M. Bhatt

IPC分类号： A01N47/02 ,  A01N43/56 ,  A01P7/04 ,  A01P7/00 ,  A01C1/06 ,  A61P33/00 ,  A61K31/415 ,  C07D231/44

CPC分类号： A01N47/02 ,  A01N2300/00

摘要： The present invention relates to a novel crystalline modification of fipronil, to a process for the preparation of the same, to pesticidal and parasiticidal mixtures and compositions comprising said crystalline modification and to their use for combating pests and parasites.

公开(公告)号：US20170121290A1

公开(公告)日：2017-05-04

申请号：US15408124

申请日：2017-01-17

申请人： Anat Levin ,  Michael Grabarnick

发明人： Anat Levin ,  Michael Grabarnick

IPC分类号： C07D231/44

CPC分类号： C07D231/44

摘要： An improved oxidation process for preparing 5-amino-3-cyano-1-(2,6-dichloro-4-trifluoromethylphenyl)-4-trifluoromethylsulphinyl-pyrazole, of formula (I) is described. The process includes admixing 5-amino-3-cyano-1-(2, 6-dichloro-4-trifluoromethylphenyl)-4-trifluoromethylthiopyrazole of formula (II) with dichloroacetic acid and hydrogen peroxide in the presence of a strong acid.

公开(公告)号：US20170120231A1

公开(公告)日：2017-05-04

申请号：US15317725

申请日：2015-03-20

申请人： JOHNSON MATTHEY PUBLIC LIMITED COMPANY

发明人： Thomas COLACOT ,  Andrew JON DEANGELIS

IPC分类号： B01J31/24 ,  C07C213/02 ,  C07C67/343 ,  C07C231/08 ,  C07D317/66 ,  C07D213/74 ,  C07D401/12 ,  C07D471/04 ,  C07D409/12 ,  C07B43/04 ,  C07B37/02 ,  C07B47/00 ,  C07D231/44 ,  C07D215/38 ,  C07D417/12 ,  C07D405/12 ,  C07D207/27 ,  C07D263/22 ,  C07D263/24 ,  C07D277/42 ,  C07D241/20 ,  C07D217/02 ,  C07D213/76 ,  C07D209/08 ,  C07D401/04 ,  C07F15/00

CPC分类号： C07F15/006 ,  B01J31/2291 ,  B01J31/24 ,  B01J31/2404 ,  B01J31/2419 ,  B01J2231/4205 ,  B01J2231/4283 ,  B01J2231/44 ,  B01J2531/824 ,  C07B37/02 ,  C07B43/04 ,  C07B47/00 ,  C07C67/343 ,  C07C213/02 ,  C07C231/08 ,  C07D207/27 ,  C07D209/08 ,  C07D213/74 ,  C07D213/76 ,  C07D215/38 ,  C07D217/02 ,  C07D231/44 ,  C07D241/20 ,  C07D263/22 ,  C07D263/24 ,  C07D277/42 ,  C07D317/66 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D471/04

摘要： A palladium(II) complex of formula (1) or a palladium(II) complex of formula (3). Also, processes for the preparation of the complexes, and their use in carbon-carbon and carbon-heteroatom coupling reactions.

公开(公告)号：US09580389B2

公开(公告)日：2017-02-28

申请号：US14940201

申请日：2015-11-13

申请人： Adama Makhteshim Ltd.

发明人： Sharona Zamir

IPC分类号： A61K31/415 ,  C07D231/44 ,  A01N47/02 ,  C07C15/06 ,  C07C49/203 ,  A01N43/56

CPC分类号： C07D231/44 ,  A01N43/56 ,  A01N47/02 ,  C07B2200/13 ,  C07C15/06 ,  C07C49/203

摘要： The present invention relates to novel crystalline polymorphs, solvate pseudomorphs and amorphous form of 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4-[(trifluoro ethyl)sulfinyl]-1H-pyrazole-3-carbonitrile (fipronil). The present invention also provides methods for preparing the novel polymorphs, pseudomorphs and amorphous form, as well as insecticidal or pesticidal compositions comprising same, and methods of use thereof as pesticidal agents.

摘要翻译： 本发明涉及5-氨基-1- [2,6-二氯-4-（三氟甲基）苯基] -4 - [（三氟乙基）亚磺酰基] -1H-吡唑-4-基）苯胺的新结晶多晶型物，溶剂化物假晶体和无定形形式， （氟虫腈）。 本发明还提供了制备新型多晶型物，假晶体和无定形形式的方法，以及包含其的杀虫剂或杀虫剂组合物的方法及其作为杀虫剂的使用方法。

公开(公告)号：US20160304467A1

公开(公告)日：2016-10-20

申请号：US15196633

申请日：2016-06-29

申请人： Anat Levin ,  Michael Grabarnick

发明人： Anat Levin ,  Michael Grabarnick

IPC分类号： C07D231/44

CPC分类号： C07D231/44

摘要： An improved oxidation process for preparing 5-amino-3-cyano-1-(2,6-dichloro-4-trifluoromethylphenyl)-4-trifluoromethylsulphinyl-pyrazole, of formula (I) is described. The process includes admixing 5-amino-3-cyano-1-(2, 6-dichloro-4-trifluoromethylphenyl)-4-trifluoromethylthiopyrazole of formula (II) with dichloroacetic acid and hydrogen peroxide in the presence of a strong acid.

摘要翻译： 描述了用于制备式（I）的5-氨基-3-氰基-1-（2,6-二氯-4-三氟甲基苯基）-4-三氟甲基亚磺酰基 - 吡唑的改进的氧化方法。 该方法包括在强酸存在下将式（II）的5-氨基-3-氰基-1-（2,6-二氯-4-三氟甲基苯基）-4-三氟甲硫基吡唑与二氯乙酸和过氧化氢混合。