公开(公告)号：US11155528B2

公开(公告)日：2021-10-26

申请号：US16663861

申请日：2019-10-25

申请人： King Abdulaziz University

发明人： Moustafa E. El-Araby ,  Abdelsattar M. Omar ,  Martin K. Safo ,  Radwan S. Elhaggar ,  Tamer M. Abdelghany ,  Mostafa H. Ahmed

IPC分类号： C07D295/108 ,  C07D307/52 ,  C07D209/14 ,  C07D213/75 ,  C07D295/15 ,  C07D207/06 ,  C07D233/40 ,  C07D333/24 ,  C07D241/04 ,  C07D295/13 ,  C07C233/40

摘要： A compound of formula (I), wherein R1 is an optionally substituted aryl or an optionally substituted heteroaryl, R2 is an optionally substituted aryl or an optionally substituted heteroaryl, and R3 is an optionally substituted alkylamino, an optionally substituted cycloalkylamino, an optionally substituted arylamino, an optionally substituted heterocyclylamino, an optionally substituted heterocyclyl, and an optionally substituted dialkylamino. A pharmaceutical composition which includes the compound of formula (I) and a pharmaceutically acceptable carrier and/or excipient. A method of treating colorectal cancer in a subject, whereby a therapeutically effective amount of the compound of formula (I) is administered to the subject.

公开(公告)号：US10889540B2

公开(公告)日：2021-01-12

申请号：US15871856

申请日：2018-01-15

申请人： BEIJING J-TEC TECHNOLOGY CO., LTD.

发明人： Chenghan Tang ,  Yunjian Zhao ,  Anxing Wei ,  Wei Guo

IPC分类号： C07C221/00 ,  C07C231/02 ,  C07D207/06 ,  C07D295/108

摘要： The present application provides a preparation method of a formamide compound, the preparation process includes: uniformly mixing raw material of methanoic acid and an amine compound selected from a primary amine or a secondary amine to prepare a homogeneous reaction system; the above homogeneous reaction system is heated to 160-230° C., allowing carbon monoxide to be decomposed from the homogeneous reaction system and participates in the reaction, and collecting the reaction product to obtain a formamide compound. The present application provides a new technology using a homogeneous method to synthesize a formamide compound, the reaction process needs no use of a catalyst, the operation process is simple and controllable, and the raw material of the amine compound has a high selectivity.

公开(公告)号：US20190194163A1

公开(公告)日：2019-06-27

申请号：US16322278

申请日：2016-08-04

申请人： Sunovion Pharmaceuticals Inc.

发明人： Michele L.R. HEFFERNAN ,  Larry Wendell HARDY ,  Scott P. BROWN ,  Lee W. HERMAN

IPC分类号： C07D401/08 ,  C07D405/06 ,  C07D401/06 ,  C07D401/14 ,  C07D207/12 ,  C07D295/096 ,  C07D295/027 ,  C07D311/22 ,  C07D471/04 ,  C07D235/12 ,  C07D237/14 ,  C07D217/24 ,  C07D295/073 ,  C07D295/108 ,  C07D275/04 ,  C07D311/08 ,  C07D307/83 ,  C07D491/048 ,  C07D277/66 ,  C07D401/12 ,  C07D211/44 ,  C07D211/58 ,  C07D265/30 ,  C07D413/06 ,  C07D241/04 ,  C07D223/08 ,  C07D267/10 ,  C07D243/08 ,  C07D413/08 ,  C07D471/08 ,  C07D487/10 ,  C07D471/10 ,  C07D491/107

CPC分类号： C07D401/08 ,  A61P25/18 ,  A61P25/28 ,  C07D207/12 ,  C07D207/36 ,  C07D211/42 ,  C07D211/44 ,  C07D211/58 ,  C07D213/81 ,  C07D217/24 ,  C07D221/20 ,  C07D223/08 ,  C07D235/12 ,  C07D237/14 ,  C07D241/04 ,  C07D243/08 ,  C07D249/12 ,  C07D265/30 ,  C07D267/10 ,  C07D275/04 ,  C07D277/66 ,  C07D295/027 ,  C07D295/073 ,  C07D295/088 ,  C07D295/096 ,  C07D295/104 ,  C07D295/108 ,  C07D307/83 ,  C07D311/08 ,  C07D311/22 ,  C07D311/58 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06 ,  C07D413/08 ,  C07D417/04 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/10 ,  C07D491/048 ,  C07D491/107 ,  C07D491/20 ,  C07D513/04

摘要： Compounds of formula I: are disclosed, as are pharmaceutical compositions containing such compounds. Methods of treating neurological or psychiatric disorders in a patient in need are also disclosed. Such disorders include depression, bipolar disorder, pain, schizophrenia, obsessive compulsive disorder, addiction, social disorder, attention deficit hyperactivity disorder, an anxiety disorder, autism, a cognitive impairment, or a neuropsychiatric symptom such as apathy, depression, anxiety, psychosis, aggression, agitation, impulse control disorders, and sleep disorders in neurological disorders such as Alzheimer's and Parkinson's diseases.

公开(公告)号：US20190071391A1

公开(公告)日：2019-03-07

申请号：US15871856

申请日：2018-01-15

申请人： BEIJING J-TEC TECHNOLOGY CO., LTD.

发明人： CHENGHAN TANG ,  YUNJIAN ZHAO ,  ANXING WEI ,  WEI GUO

IPC分类号： C07C221/00 ,  C07D295/108 ,  C07C231/02 ,  C07D207/06

摘要： The present application provides a preparation method of a formamide compound, the preparation process includes: uniformly mixing raw material of methanoic acid and an amine compound selected from a primary amine or a secondary amine to prepare a homogeneous reaction system; the above homogeneous reaction system is heated to 160-230° C., allowing carbon monoxide to be decomposed from the homogeneous reaction system and participates in the reaction, and collecting the reaction product to obtain a formamide compound. The present application provides a new technology using a homogeneous method to synthesize a formamide compound, the reaction process needs no use of a catalyst, the operation process is simple and controllable, and the raw material of the amine compound has a high selectivity.

公开(公告)号：US10202602B2

公开(公告)日：2019-02-12

申请号：US15247584

申请日：2016-08-25

申请人： Sarepta Therapeutics, Inc.

发明人： Gunnar J. Hanson ,  Alexander Charles Rudolph ,  Bao Zhong Cai ,  Ming Zhou ,  Dwight D. Weller

IPC分类号： C12N15/113 ,  C07F9/59 ,  C07F9/572 ,  C07F9/6558 ,  C07F9/6561 ,  C07F9/6584 ,  C07H21/00 ,  A61K31/496 ,  A61K31/5377 ,  C07D265/30 ,  C07D295/108 ,  C07F9/22 ,  C07F9/26 ,  C07F9/6544

摘要： Oligonucleotide analogs comprising modified intersubunit linkages and/or modified 3′ and/or 5′-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.

公开(公告)号：US20180098993A1

公开(公告)日：2018-04-12

申请号：US15836396

申请日：2017-12-08

申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH & HUMAN SERVIC ,  COOPER HEALTH SYSTEM ,  SRI International

发明人： IRVING W. WAINER ,  RUIN MOADDEL ,  MICHEL BERNIER ,  CARLOS A. ZARATE ,  MARC C. TORJMAN ,  MICHAEL E. GOLDBERG ,  MARY J. TANGA

IPC分类号： A61K31/5375 ,  C07C225/20 ,  C07C237/04 ,  A61K31/24 ,  A61K31/222 ,  C07D295/108 ,  C07D295/15 ,  A61K31/137 ,  C07D295/112 ,  C07D295/155 ,  C07C237/20 ,  C07C229/48 ,  A61K31/265 ,  A61K31/4453 ,  A61K31/165

CPC分类号： A61K31/5375 ,  A61K31/137 ,  A61K31/165 ,  A61K31/222 ,  A61K31/24 ,  A61K31/265 ,  A61K31/4453 ,  C07B2200/07 ,  C07C225/20 ,  C07C229/48 ,  C07C237/04 ,  C07C237/20 ,  C07C2601/14 ,  C07C2601/16 ,  C07D295/108 ,  C07D295/112 ,  C07D295/15 ,  C07D295/155

摘要： The disclosure provides pharmaceutical preparations containing (2R,6R)-hydroxynorketamine, or (R)- or (S)-dehydronorketamine, or other stereoisomeric dehydro or hydroxylated ketamine metabolite. The disclosure also provides novel ketamine metabolite prodrugs. The disclosure provides methods of treating, bipolar depression, major depressive disorder, neuropathic and chronic pain, including complex regional pain synthetic pain disorder (CRPD) by administering a purified ketamine metabolite or a ketamine metabolite prodrug directly to patients in need of such treatment.

公开(公告)号：US09720137B2

公开(公告)日：2017-08-01

申请号：US15024052

申请日：2014-09-25

申请人： MITSUI CHEMICALS, INC.

发明人： Satoshi Yamasaki ,  Goro Kuwamura ,  Daisuke Nishiguchi ,  Daisuke Hasegawa ,  Toshihiko Nakagawa ,  Hirokazu Morita ,  Hidetaka Tsukada ,  Kenichi Goto ,  Shinsuke Ito ,  Naoyuki Kakinuma ,  Tetsuya Hamada ,  Shinji Kiyono ,  Takeshi Fukuda ,  Kazuhiro Kosumi

IPC分类号： G02C7/02 ,  G02B1/04 ,  C08J5/18 ,  D04H3/009 ,  G02C5/00 ,  C08G18/79 ,  C08K5/3412 ,  C07C265/04 ,  C07C265/14 ,  C07D295/08 ,  C07D295/067 ,  C07D295/10 ,  C07D295/104 ,  C07D295/108 ,  C07D295/16 ,  C07D295/185 ,  C08G18/78 ,  C08G18/48 ,  C08G18/73 ,  C08G18/75 ,  C08G18/28 ,  C08G18/32 ,  C08G18/38 ,  C08G18/40 ,  C08G18/42 ,  C08G18/44 ,  C07C263/20 ,  C08G18/10 ,  C08L75/08 ,  C09D175/04 ,  A47D1/00 ,  C08G18/62 ,  C08G18/66 ,  C08G18/72 ,  C08G18/76 ,  C08G101/00 ,  D01F6/70

CPC分类号： G02B1/041 ,  A47D1/00 ,  C07C263/20 ,  C07C265/04 ,  C07C265/14 ,  C07D295/06 ,  C07D295/067 ,  C07D295/08 ,  C07D295/10 ,  C07D295/104 ,  C07D295/108 ,  C07D295/16 ,  C07D295/185 ,  C08G18/10 ,  C08G18/283 ,  C08G18/3206 ,  C08G18/3275 ,  C08G18/3855 ,  C08G18/3878 ,  C08G18/4018 ,  C08G18/4063 ,  C08G18/4202 ,  C08G18/4277 ,  C08G18/44 ,  C08G18/4808 ,  C08G18/4825 ,  C08G18/4854 ,  C08G18/6229 ,  C08G18/6677 ,  C08G18/722 ,  C08G18/73 ,  C08G18/757 ,  C08G18/758 ,  C08G18/7642 ,  C08G18/7818 ,  C08G18/7831 ,  C08G18/7837 ,  C08G18/7843 ,  C08G18/792 ,  C08G2101/00 ,  C08G2170/20 ,  C08G2190/00 ,  C08J5/18 ,  C08J2375/04 ,  C08K5/3412 ,  C08L75/08 ,  C09D175/04 ,  D01F6/70 ,  D04H3/009 ,  G02B1/04 ,  G02C5/00 ,  G02C5/008 ,  Y10T428/249921 ,  Y10T442/60 ,  C08L75/04 ,  C08G18/12 ,  C08G18/3228

摘要： The eyewear material is an eyewear material containing thermoplastic polyurethane. The eyewear material has a tan δ peak at both less than 0° C. and 0° C. or more and 70° C. or less observed in dynamic viscoelasticity measurement in tensile mode under the measurement conditions of a temperature increase speed of 5° C./min and a measurement frequency of 10 Hz.

公开(公告)号：US20160060235A1

公开(公告)日：2016-03-03

申请号：US14780052

申请日：2014-03-28

申请人： NATIONAL UNIVERSITY CORPORATION KUMAMOTO UNIVERSITY ,  KUMAMOTO HEALTH SCIENCE UNIVERSITY

发明人： Kazuhito Tomizawa ,  Fanyan Wei ,  Kengo Inoue ,  Tadashi Okawara

IPC分类号： C07D295/108 ,  C07D211/58

CPC分类号： C07D295/108 ,  A61K31/192 ,  A61K31/197 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  A61K45/06 ,  C07D211/58 ,  C07D215/48 ,  C07D295/15 ,  C07D295/185 ,  C07D333/20 ,  Y02A50/473 ,  A61K2300/00

摘要： An object of the present invention is to provide a novel therapeutic agent for a patient with type 2 diabetes, a cause of which is the abnormal synthesis of insulin attributed to the abnormal modification of tRNALys (UUU) in pancreatic β cells having Cdkal1 gene mutation. The present inventors have used (1) a screening system using E. coli in which correct translation into luciferase requires frameshift resulting from mistranslation during protein translation, (2) a screening system using the pancreatic islet of Langerhans isolated from a pancreatic β cell-specific Cdkal1-deficient mouse, and (3) a screening system using a pancreatic β cell-specific Cdkal1-deficient mouse, and found that a compound represented by any of the following formulas (I) to (III) can serve as a therapeutic agent for a patient with type 2 diabetes with Cdkal1 gene mutation resulting in the reduced ability to secrete insulin.

摘要翻译： 本发明的目的是提供一种用于2型糖尿病患者的新型治疗剂，其原因是由于胰腺中tRNALys（UUU）的异常修饰引起的胰岛异常合成; 细胞具有Cdkal1基因突变。 本发明人已经使用（1）使用大肠杆菌的筛选系统，其中正确翻译成荧光素酶需要在蛋白质翻译过程中由于错译造成的移码，（2）使用从胰腺分离的朗格汉斯胰岛的筛选系统; 细胞特异性Cdkal1缺陷小鼠，和（3）使用胰腺的筛选系统; 细胞特异性Cdkal1缺陷小鼠，发现由下式（I）至（III）中任一项表示的化合物可用作具有Cdkal1基因突变的2型糖尿病患者的治疗剂，导致其降低的能力 分泌胰岛素

公开(公告)号：US09006457B2

公开(公告)日：2015-04-14

申请号：US12990029

申请日：2009-03-31

申请人： Michael Schmidt ,  Nikolai (Mykola) Ignatyev ,  William-Robert Pitner

发明人： Michael Schmidt ,  Nikolai (Mykola) Ignatyev ,  William-Robert Pitner

IPC分类号： C07D207/06 ,  C07D295/037 ,  C07C211/63 ,  C07C219/04 ,  C07C225/06 ,  C07C229/08 ,  C07C255/25 ,  C07C309/06 ,  C07C309/65 ,  C07C311/48 ,  C07C317/04 ,  C07D263/04 ,  C07D295/088 ,  C07D295/108 ,  C07D295/145 ,  C07F9/54 ,  C07F9/6568 ,  H01B1/12 ,  H01M10/052 ,  H01M10/0569 ,  H01G11/06 ,  H01G11/58 ,  H01M10/0525

CPC分类号： C07C229/12 ,  C07C211/63 ,  C07C219/04 ,  C07C225/06 ,  C07C229/08 ,  C07C255/25 ,  C07C309/06 ,  C07C309/65 ,  C07C311/48 ,  C07C317/04 ,  C07D207/08 ,  C07D211/14 ,  C07D263/04 ,  C07D295/037 ,  C07D295/088 ,  C07D295/108 ,  C07D295/145 ,  C07F9/28 ,  C07F9/301 ,  C07F9/5428 ,  C07F9/65688 ,  H01B1/122 ,  H01G11/06 ,  H01G11/58 ,  H01G11/60 ,  H01G11/62 ,  H01G11/64 ,  H01M10/052 ,  H01M10/0525 ,  H01M10/0567 ,  H01M10/0568 ,  H01M10/0569 ,  Y02E60/122 ,  Y02E60/13

摘要： The invention relates to reactive ionic liquids containing organic cations with groups or substituents which are susceptible to electrochemical reduction and anions obtained from fluoroalkyl phosphates, fluoroalkyl phosphinates, fluoroalkyl phosphonates, acetates, triflates, imides, methides, borates, phosphates and/or aluminates, for use in electrochemical cells, such as lithium ion batteries and double-layer capacitors.

摘要翻译： 本发明涉及含有有机阳离子的反应性离子液体，其具有易于电化学还原的有机阳离子和从氟烷基磷酸盐，氟代烷基次膦酸盐，氟代烷基膦酸盐，乙酸盐，三氟甲磺酸盐，酰亚胺，甲基化物，硼酸盐，磷酸盐和/或铝酸盐获得的阴离子， 用于电化学电池，如锂离子电池和双层电容器。

公开(公告)号：US20140228357A1

公开(公告)日：2014-08-14

申请号：US14347556

申请日：2012-09-27

申请人： KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY ,  DONGGUK UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION

发明人： Kyeong Lee ,  Mi-Sun Won ,  Hwan-Mook Kim ,  Song-Kyu Park ,  Ki-Ho Lee ,  Chang-Woo Lee ,  Bo-Kyung Kim ,  Hyun-Seung Ban ,  Kyung-Sook Chung ,  Naik Ravi

IPC分类号： C07D487/04 ,  C07C231/02 ,  C07D295/182 ,  C07C235/20 ,  C07D295/108

CPC分类号： A61K31/5375 ,  A61K31/495 ,  A61K31/4985 ,  C07C231/02 ,  C07C235/20 ,  C07C235/22 ,  C07D241/04 ,  C07D279/12 ,  C07D295/073 ,  C07D295/104 ,  C07D295/108 ,  C07D295/182 ,  C07D295/185 ,  C07D307/46 ,  C07D487/04

摘要： The present invention relates to novel compounds as HIF-1α inhibitors, manufacturing process thereof, and a pharmaceutical compositions. The compounds according to the present invention having inhibition activity against HIF-1α, can be used as a therapeutic prevention and/or treatment for various solid cancers such as colon cancer, liver cancer, stomach cancer and breast cancer. Also, the compounds according to the present invention are useful in the treatment of diabetic retinopathy and rheumatoid arthritis, which are aggravated by HIF-1α-mediated VEGFA expression.

摘要翻译： 本发明涉及作为HIF-1α抑制剂的新化合物，其制备方法和药物组合物。 具有抑制HIF-1α活性的本发明化合物可用作结肠癌，肝癌，胃癌和乳腺癌等各种固体癌症的治疗性预防和/或治疗。 此外，本发明的化合物可用于治疗由HIF-1α介导的VEGFA表达加重的糖尿病性视网膜病变和类风湿性关节炎。