公开(公告)号：US10214515B2

公开(公告)日：2019-02-26

申请号：US15741639

申请日：2016-08-19

申请人： Zhejiang Hisun Pharmaceutical Co., Ltd.

发明人： Lei Chen ,  Dongliang Guan ,  Hua Bai ,  Xing Yan ,  Shuai Miao ,  Songsong Zhu

IPC分类号： A61K31/4155 ,  C07D231/38 ,  C07D403/14 ,  A61K31/4184 ,  A61P35/00 ,  C07D233/06 ,  C07D233/28 ,  C07D233/46 ,  C07D233/48 ,  C07D401/14

摘要： An indole derivative as expressed by Formula (I), a preparation method thereof, a pharmaceutical salt, and use thereof as a therapeutic agent, especially as a FGFR inhibitor. Each substituent in Formula (I) has identical definition as specified in the specification.

公开(公告)号：US10214494B2

公开(公告)日：2019-02-26

申请号：US15725848

申请日：2017-10-05

申请人： The United States of America as Represented by the Secretary of the Air Force

发明人： Rusty L. Blanski ,  Robert H. Grubbs

IPC分类号： C07D233/28 ,  C07F15/00

摘要： Backfunctionalized imidazolinium salts and methods of synthesizing the same and NHC carbene-metal complexes therefrom. For backfunctionalized imidazolinium salts of the formula: Wherein R1 is selected from the group consisting of an ester group, an amide group, and an aromatic group; R2 is selected from the group consisting of hydrogen, an ester group, an amide group, and an aromatic group; R3 and R4 are each an aliphatic group; and X is an anion; the method comprises cyclization of a halogenated acrylate with Hünig's base in a solvent.

公开(公告)号：US20180072681A1

公开(公告)日：2018-03-15

申请号：US15725848

申请日：2017-10-05

申请人： Government of the United States as Represented by the Secretary of the Air Force

发明人： Rusty L. Blanski ,  Robert H. Grubbs

IPC分类号： C07D233/28 ,  C07F15/00

CPC分类号： C07D233/28 ,  C07F15/0033 ,  C07F15/0046

摘要： Backfunctionalized imidazolinium salts and methods of synthesizing the same and NHC carbene-metal complexes therefrom. For backfunctionalized imidazolinium salts of the formula: Wherein R1 is selected from the group consisting of an ester group, an amide group, and an aromatic group; R2 is selected from the group consisting of hydrogen, an ester group, an amide group, and an aromatic group; R3 and R4 are each an aliphatic group; and X is an anion; the method comprises cyclization of a halogenated acrylate with Hünig's base in a solvent.

公开(公告)号：US09716241B2

公开(公告)日：2017-07-25

申请号：US14965128

申请日：2015-12-10

申请人： BASF SE

发明人： Hans Juerg Kirner ,  Natalia Chebotareva ,  Olivier Frederic Aebischer

IPC分类号： C08G75/00 ,  H01L51/00 ,  C07D233/28 ,  C08G61/12 ,  C07D495/04 ,  C07D513/14 ,  C07F7/08 ,  C08F128/06 ,  C08G75/06 ,  C08G75/32 ,  H01L51/05

CPC分类号： H01L51/0094 ,  C07D233/28 ,  C07D495/04 ,  C07D513/14 ,  C07F7/0814 ,  C08F128/06 ,  C08G61/122 ,  C08G61/123 ,  C08G61/126 ,  C08G75/06 ,  C08G75/32 ,  C08G2261/3241 ,  C08G2261/3243 ,  C08G2261/3247 ,  C08G2261/414 ,  C08G2261/92 ,  C09B57/00 ,  H01L51/0003 ,  H01L51/0036 ,  H01L51/0043 ,  H01L51/0071 ,  H01L51/0074 ,  H01L51/0545 ,  H01L51/0558 ,  Y02E10/549

摘要： The present invention relates to novel compounds, corresponding oligomers and (co)polymers. The compounds according to the invention are useful as semiconductors and have excellent solubility in organic solvents and excellent film-forming properties. In addition, high efficiency of energy conversion, excellent field-effect mobility, good on/off current ratios and/or excellent stability can be observed, when the polymers according to the invention are used in organic field effect transistors, organic photovoltaics (solar cells) and photodiodes.

公开(公告)号：US20160102061A1

公开(公告)日：2016-04-14

申请号：US14880147

申请日：2015-10-09

申请人： Government of the United States as Represented by the Secretary of the Air Force

发明人： Rusty L. Blanski ,  Robert H. Grubbs

IPC分类号： C07D233/28 ,  C07F15/00

CPC分类号： C07D233/28 ,  C07F15/0033 ,  C07F15/0046

摘要： Backfunctionalized imidazolinium salts and methods of synthesizing the same and NHC carbene-metal complexes therefrom. For backfunctionalized imidazolinium salts of the formula: Wherein R1 is selected from the group consisting of an ester group, an amide group, and an aromatic group; R2 is selected from the group consisting of hydrogen, an ester group, an amide group, and an aromatic group; R3 and R4 are each an aliphatic group; and X is an anion; the method comprises cyclization of a halogenated acrylate with Hünig's base in a solvent.

摘要翻译： 回归功能化的咪唑啉鎓盐及其合成方法和由其制备的NHC卡宾 - 金属络合物。 对于下式的后官能化咪唑啉鎓盐：其中R1选自酯基，酰胺基和芳族基团; R2选自氢，酯基，酰胺基和芳族基; R3和R4各自为脂族基团; X为阴离子; 该方法包括在溶剂中将Hünig碱卤化丙烯酸酯环化。

公开(公告)号：US08946276B2

公开(公告)日：2015-02-03

申请号：US13536960

申请日：2012-06-28

申请人： Michael T. Nordsiek ,  Kodumudi S. Balaji

发明人： Michael T. Nordsiek ,  Kodumudi S. Balaji

IPC分类号： A01N43/50 ,  A61K31/415 ,  C07D233/28 ,  C07D233/91 ,  A61K9/00 ,  A61K31/4164 ,  A61K47/10 ,  A61K47/14 ,  A61K9/06 ,  A61K47/32

CPC分类号： A61K31/4168 ,  A61K9/0034 ,  A61K9/06 ,  A61K31/4164 ,  A61K47/10 ,  A61K47/14 ,  A61K47/32

摘要： The present disclosure provides mucoadhesive aqueous-based gel formulations of metronidazole useful for a variety of purposes, including intravaginal application as a therapeutic approach towards the treatment of individuals suffering from and/or diagnosed with bacterial vaginosis.

摘要翻译： 本公开提供了用于各种目的的甲硝唑的粘膜粘附性水基凝胶制剂，包括阴道内施用作为治疗患有和/或诊断为细菌性阴道炎的个体的治疗方法。

公开(公告)号：US08258166B2

公开(公告)日：2012-09-04

申请号：US13365723

申请日：2012-02-03

申请人： Yasushi Murakami ,  Naoko Kobayashi ,  Azuma Nishio ,  Nobuo Kubota

发明人： Yasushi Murakami ,  Naoko Kobayashi ,  Azuma Nishio ,  Nobuo Kubota

IPC分类号： A01N43/52 ,  A61K31/415 ,  C07D233/28 ,  C07D233/91

CPC分类号： A61K9/08 ,  A61K9/0019 ,  A61K31/4168 ,  A61K41/0038 ,  C07D233/91

摘要： A Cancer radiotherapeutic method using 1-(1-hydroxymethyl-2,3-dihydroxypropyl)oxymethyl-2-nitroimidazole (compound (i), and creatinine in an amount of 0.001 to part by mass with respect to 1 part by mass of compound (1); and irradiation.

摘要翻译： 相对于1质量份化合物，使用1-（1-羟甲基-2,3-二羟丙基）氧甲基-2-硝基咪唑（化合物（i））和肌酸酐0.001〜质量份的癌症放射治疗法 1）和照射。

公开(公告)号：US08030338B2

公开(公告)日：2011-10-04

申请号：US12522926

申请日：2008-01-17

申请人： Azuma Nishio

发明人： Azuma Nishio

IPC分类号： A61K31/4168 ,  C07D233/28

CPC分类号： C07D233/91 ,  A61K51/0453

摘要： It is an object to provide a method for producing a 2-nitroimidazole derivative having an acyclic sugar chain in a side chain, which is suitable for production of a derivative having a radioisotope.A method for producing 1-(1-benzoyloxymethyl-2-hydroxyethyl)oxymethyl-2-nitroimidazole, characterized by reacting glycerin with a benzoylating agent to obtain 1-O-benzoylglycerin, reacting 1-O-benzoylglycerin with dimethoxymethane in the presence of a dehydrating agent to obtain 4-benzoyloxymethyl-1,3-dioxolane, and then reacting this product with 2-nitroimidazole or 2-nitro-1-trialkylsilylimidazole in the presence of a Lewis acid.

摘要翻译： 本发明的目的是提供一种用于制备侧链中具有无环糖链的2-硝基咪唑衍生物的方法，其适用于制备具有放射性同位素的衍生物。 1-（1-苯甲酰氧基甲基-2-羟乙基）氧基甲基-2-硝基咪唑的制备方法，其特征在于使甘油与苯甲酰化试剂反应，得到1-O-苯甲酰甘油，使1-O-苯甲酰甘油与二甲氧基甲烷在 脱水剂，得到4-苯甲酰氧基甲基-1,3-二氧戊环，然后在路易斯酸存在下使该产物与2-硝基咪唑或2-硝基-1-三烷基甲硅烷基咪唑反应。

公开(公告)号：US07847092B2

公开(公告)日：2010-12-07

申请号：US11720393

申请日：2005-12-09

申请人： Dae Hyuk Moon ,  Dae Yoon Chi ,  Dong Wook Kim ,  Seung Jun Oh ,  Jin-sook Ryu

发明人： Dae Hyuk Moon ,  Dae Yoon Chi ,  Dong Wook Kim ,  Seung Jun Oh ,  Jin-sook Ryu

IPC分类号： C07H19/073 ,  C07H5/02 ,  C07D451/02 ,  C07D233/28 ,  C07J75/00 ,  C07C255/09 ,  C07C19/08

CPC分类号： C07C209/02 ,  A61K51/1282 ,  B65B3/003 ,  C07B39/00 ,  C07B59/00 ,  C07B59/002 ,  C07B2200/05 ,  C07C213/08 ,  C07C253/30 ,  C07C303/30 ,  C07D213/64 ,  C07D233/91 ,  C07D451/02 ,  C07H5/02 ,  C07H19/06 ,  C07J1/0051 ,  C07C309/73 ,  C07C255/42 ,  C07C211/63 ,  C07C215/40 ,  C07C217/80

摘要： The present invention relates to a method for preparation of organofluoro compounds containing radioactive isotope fluorine-18. More particularly, the present invention relates to a method for preparation of primary or secondary organofluoro compound by reacting fluorine salt containing radioactive isotope fluorine-18 with primary or secondary alkyl halide or primary or secondary alkyl sulfonate in the presence of alcohol of Chemical Formula 1 as a solvent to obtain high yield of organofluoro compound. Synthesis reaction according to the present invention may be carried out under mild condition to give high yield of the organofluoro compounds and the reaction time is decreased, and thereby is suitable for the mass production of the organofluoro compounds.

摘要翻译： 本发明涉及含有放射性同位素氟-18的有机氟化合物的制备方法。 更具体地说，本发明涉及在化学式1的醇存在下，通过使含有放射性同位素氟-18的氟盐与伯或仲烷基卤或伯或仲烷基磺酸盐反应来制备伯或仲有机氟化合物的方法， 得到高收率的有机氟化合物的溶剂。 根据本发明的合成反应可以在温和条件下进行，得到有机氟化合物的高产率，反应时间降低，从而适合大量生产有机氟化合物。

公开(公告)号：US20070197619A1

公开(公告)日：2007-08-23

申请号：US10592283

申请日：2005-03-07

申请人： Robert Zelle ,  Paul Will

发明人： Robert Zelle ,  Paul Will

IPC分类号： A61K31/4178 ,  A61K31/4172 ,  C07D403/02 ,  C07D233/28

CPC分类号： C07D233/64 ,  C07D233/90 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/14 ,  C07D417/04

摘要： The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particularly those mediated by certain calcium channel subtype targets.

摘要翻译： 本发明涉及化合物，包含该化合物的组合物，以及使用该化合物和化合物组合物的方法。 本文所述的化合物，组合物和方法可用于治疗性调节离子通道功能，以及治疗疾病和疾病症状，特别是由某些钙通道亚型靶标介导的那些症状。