公开(公告)号：US11814372B2

公开(公告)日：2023-11-14

申请号：US16026421

申请日：2018-07-03

申请人： CASE WESTERN RESERVE UNIVERSITY

发明人： Bingcheng Wang

IPC分类号： C07D403/04 ,  A61P35/00 ,  C07D405/14 ,  C07D273/04

CPC分类号： C07D405/14 ,  A61P35/00 ,  C07D273/04

摘要： A method of treating cancer in a subject includes administering to the subject a therapeutically effective amount of a small molecule agonist of EphA2 receptor protein, the small molecule having a general formula: A-L-X-Z (I).

公开(公告)号：US10961206B2

公开(公告)日：2021-03-30

申请号：US16496961

申请日：2018-03-27

申请人： Adama Makhteshim Ltd.

发明人： Rajuri Venkataramana ,  Jayapal Reddy Bicidi ,  Bijukumar Gopinathan Pillai ,  Sreedevi Mannam

IPC分类号： C07D273/04

摘要： It is an object of the present invention to provide a novel and advantageous process for commercially preparing of indoxacarb which is racemic or enantiomerically enriched at chiral center from its amide precursor using a new catalytic system.
More particularly, it relates to an efficient method of preparation of indoxacarb which is racemic or enantiomerically enriched at chiral center from methyl-7-chloro-2,5-dihydro-2-[[[(4-tritluoromethoxy)phenyl]amino]carbonyl]-indeno[1,2-e][1,3,4]oxadiazine-4a(3H) carboxylate represented as formula (I) using methoxycarbonylation agent and metal salt of methylsulfinylmethylide in hydrocarbon solvent in the presence of organic base and phase transfer catalyst.

公开(公告)号：US20190002446A1

公开(公告)日：2019-01-03

申请号：US16026421

申请日：2018-07-03

申请人： CASE WESTERN RESERVE UNIVERSITY

发明人： Bingcheng Wang

IPC分类号： C07D405/14 ,  A61P35/00 ,  C07D273/04

摘要： A method of treating cancer in a subject includes administering to the subject a therapeutically effective amount of a small molecule agonist of EphA2 receptor protein, the small molecule having a general formula: A-L-X-Z (I).

公开(公告)号：US20170342039A1

公开(公告)日：2017-11-30

申请号：US15481568

申请日：2017-04-07

申请人： Farmington Pharma Development

发明人： William F. Brubaker

IPC分类号： C07D273/06 ,  C07C279/14 ,  C07C279/24 ,  C07D273/04 ,  C07D271/07

CPC分类号： C07D273/06 ,  C07B2200/05 ,  C07C279/14 ,  C07C279/24 ,  C07D271/07 ,  C07D273/04

摘要： The invention describes membrane permeable creatine prodrugs, pharmaceutical compositions comprising membrane permeable creatine prodrugs, and methods of treating diseases such as ischemia, heart failure, neurodegenerative disorders and genetic disorders affecting the creatine kinase system comprising administering creatine prodrugs or pharmaceutical compositions thereof. The invention also describes treating a genetic disease affecting the creatine kinase system, such as, for example, a creatine transporter disorder or a creatine synthesis disorder comprising administering creatine prodrugs or pharmaceutical compositions thereof.

公开(公告)号：US09790194B2

公开(公告)日：2017-10-17

申请号：US14360727

申请日：2012-11-29

申请人： Covestro Deutschland AG

发明人： Frank Richter ,  Martin Anstock ,  Philip Bahke ,  Andreas Gosch ,  Reinhard Halpaap ,  Andreas Hecking ,  Sigurd Buchholz ,  Ursula Tracht ,  Adrian Cosmin Dobre

IPC分类号： C07D273/04 ,  C08G18/78 ,  C08G18/79 ,  C08G18/09 ,  C08G18/02

CPC分类号： C07D273/04 ,  C08G18/022 ,  C08G18/025 ,  C08G18/092 ,  C08G18/7831 ,  C08G18/791

摘要： A process for continuous preparation of oligomeric or polymeric isocyanates by catalytic modification of monomeric di- and/or triisocyanates, characterized in that at least one isocyanate component A and at least one catalyst component B are combined continuously in a reaction apparatus and conducted through the reaction apparatus as a reaction mixture, the residence time distribution being characterized according to the dispersion model by Bo (Bodenstein number) above 40, preferably above 60 and most preferably above 80.

公开(公告)号：US20140275525A1

公开(公告)日：2014-09-18

申请号：US14359125

申请日：2012-11-27

申请人： Bayer Intellectual Property GmbH

发明人： Frank Richter ,  Martin Brahm

IPC分类号： C07D273/04

CPC分类号： C07D273/04 ,  C08G18/022 ,  C08G18/025 ,  C08G18/092 ,  C08G18/095 ,  C08G18/168 ,  C08G18/7887 ,  C08G18/792

摘要： The invention relates to a method for modifying isocyanates using catalysts having a water content not exceeding 1,000 ppm.

摘要翻译： 本发明涉及使用含水量不超过1000ppm的催化剂改性异氰酸酯的方法。

公开(公告)号：US20120108808A1

公开(公告)日：2012-05-03

申请号：US13382265

申请日：2010-07-07

申请人： Young Lag Cho ,  Jong Un Cho ,  Sung Yoon Baek ,  Ho Young Song ,  Tae Kyo Park ,  Sung Ho Woo ,  Yong Zu Kim

发明人： Young Lag Cho ,  Jong Un Cho ,  Sung Yoon Baek ,  Ho Young Song ,  Tae Kyo Park ,  Sung Ho Woo ,  Yong Zu Kim

IPC分类号： C07D273/04

CPC分类号： C07D413/14 ,  C07D413/12

摘要： Provided is a method for preparing (S)-5-chloro-N-((3-(4-(5,6-dihydro-4H-1,2,4-oxadiazin-3-yl)phenyl)-2-oxooxazolidin-5-yl)methyl)thiophene-2-carboxamide derivatives of Formula (I) which are useful as blood coagulation factor Xa inhibitors, and said method using 1-fluoro-4-nitrobenzen as a starting material. According to the method of the present invention, (S)-5-chloro-N-((3-(4-(5,6-dihydro-4H-1,2,4-oxadiazin-3-yl)phenyl)-2-oxooxazolidin-5-yl)methyl)thiophene-2-carboxamide derivatives of Formula (I) which are useful as blood coagulation factor Xa inhibitors can be prepared in a high purity and a high yield.

摘要翻译： 提供制备（S）-5-氯-N - （（3-（4-（5,6-二氢-4H-1,2,4-恶二嗪-3-基）苯基）-2-氧代恶唑烷 -5-基）甲基）噻吩-2-甲酰胺衍生物，所述方法使用1-氟-4-硝基苯作为原料，所述方法可用作凝血因子Xa抑制剂。 根据本发明的方法，（S）-5-氯-N - （（3-（4-（5,6-二氢-4H-1,2,4-恶二嗪-3-基）苯基） - 可用作凝血因子Xa抑制剂的式（I）的噻吩-2-甲酰胺衍生物可以以高纯度和高收率制备。

公开(公告)号：US20110218194A1

公开(公告)日：2011-09-08

申请号：US13108454

申请日：2011-05-16

申请人： Zhaoning Zhu ,  Brian A. Mckittrick ,  Zhong-Yue Sun ,  Yuanzan C. Ye ,  Johannes H. Voight ,  Corey Strickland ,  Elizabeth M. Smith ,  Andrew Stamford ,  William J. Greenlee ,  Robert Mazzola ,  John Caldwell ,  Jared N. Cumming ,  Lingyan Wang ,  Yusheng Wu ,  Ulrich Iserloh ,  Tao Guo ,  Thuy X. H. Le ,  Kurt W. Saionz ,  Suresh D. Babu ,  Rachel C. Hunter ,  Michelle L. Morris ,  Huizhong Gu ,  Gang Qian ,  Dawit Tadesse

发明人： Zhaoning Zhu ,  Brian A. Mckittrick ,  Zhong-Yue Sun ,  Yuanzan C. Ye ,  Johannes H. Voight ,  Corey Strickland ,  Elizabeth M. Smith ,  Andrew Stamford ,  William J. Greenlee ,  Robert Mazzola ,  John Caldwell ,  Jared N. Cumming ,  Lingyan Wang ,  Yusheng Wu ,  Ulrich Iserloh ,  Tao Guo ,  Thuy X. H. Le ,  Kurt W. Saionz ,  Suresh D. Babu ,  Rachel C. Hunter ,  Michelle L. Morris ,  Huizhong Gu ,  Gang Qian ,  Dawit Tadesse

IPC分类号： A61K31/5395 ,  C07D273/04 ,  C07D413/10 ,  A61P9/00 ,  A61P33/02 ,  A61P31/10 ,  A61P25/28 ,  A61P25/00

CPC分类号： C07D233/46 ,  C07D233/70 ,  C07D233/88 ,  C07D239/22 ,  C07D239/70 ,  C07D271/07 ,  C07D273/00 ,  C07D401/04 ,  C07D401/08 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/08 ,  C07D403/10 ,  C07D403/12 ,  C07D405/10 ,  C07D409/04 ,  C07D409/10 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D417/06

摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(═S)—, —S(O)—, —S(O)2—, —C(═O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(═N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(═O)— or —C(═NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(═NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes.Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

公开(公告)号：US07060817B2

公开(公告)日：2006-06-13

申请号：US10910943

申请日：2004-08-04

申请人： Jürgen Köcher ,  Reinhard Halpaap

发明人： Jürgen Köcher ,  Reinhard Halpaap

IPC分类号： C07D229/00 ,  C07D251/34 ,  C07D273/04

CPC分类号： C07D295/30 ,  C07D241/20 ,  C07D261/14 ,  C07D277/52 ,  C08G18/022 ,  C08G18/027 ,  C08G18/1883

摘要： The present invention relates to the use of sulphonamide salts as catalysts for oligomerizing isocyanates and also to a process for NCO oligomerization using the catalysts of the invention.

摘要翻译： 本发明涉及磺酰胺盐作为用于低聚异氰酸酯的催化剂的用途，以及使用本发明的催化剂的NCO低聚方法。

公开(公告)号：US20050143418A1

公开(公告)日：2005-06-30

申请号：US10512377

申请日：2003-04-28

申请人： John Dixson ,  Zeinab Elshenawy ,  Harvey Wendt ,  Saroj Sehgel ,  Robert Henrie II ,  David Roush ,  Ping Ding ,  John Lyga ,  Stephen Donovan

发明人： John Dixson ,  Zeinab Elshenawy ,  Harvey Wendt ,  Saroj Sehgel ,  Robert Henrie II ,  David Roush ,  Ping Ding ,  John Lyga ,  Stephen Donovan

IPC分类号： C07D233/06 ,  A01N33/02 ,  A01N37/52 ,  A01N43/06 ,  A01N43/08 ,  A01N43/18 ,  A01N43/40 ,  A01N43/50 ,  A01N43/54 ,  A01N43/56 ,  A01N43/76 ,  A01N43/78 ,  A01N43/88 ,  A61K31/4164 ,  A61K31/4178 ,  C07D207/333 ,  C07D233/10 ,  C07D233/20 ,  C07D233/22 ,  C07D233/24 ,  C07D233/26 ,  C07D233/54 ,  C07D233/64 ,  C07D239/06 ,  C07D263/12 ,  C07D263/14 ,  C07D273/04 ,  C07D277/10 ,  C07D401/04 ,  C07D401/06 ,  C07D405/04 ,  C07D405/06 ,  C07D407/04 ,  C07D409/04 ,  C07D409/06 ,  C07D413/04 ,  C07D417/04 ,  C07D491/052 ,  C07D495/04 ,  C07F9/6506 ,  C07F9/6533 ,  C07F9/6558

CPC分类号： A01N43/88 ,  A01N43/50 ,  A01N43/54 ,  A01N43/56 ,  A01N43/76 ,  A01N43/78 ,  C07D211/70 ,  C07D211/74 ,  C07D233/10 ,  C07D233/20 ,  C07D233/22 ,  C07D233/24 ,  C07D233/26 ,  C07D233/64 ,  C07D263/14 ,  C07D273/04 ,  C07D277/14 ,  C07D307/06 ,  C07D307/12 ,  C07D307/20 ,  C07D309/18 ,  C07D309/20 ,  C07D309/22 ,  C07D309/30 ,  C07D333/08 ,  C07D333/16 ,  C07D333/32 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07F9/6506 ,  C07F9/6533 ,  C07F9/65586

摘要： It has now been found that certain novel heterocyclic derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): R Preferred are those compounds of formula (I) where R2 and R3 taken together is ═NCH(R6)CH(R7)N(R8)—, ═NC(R6)═C(R7)N(R8)—, or ═CHN═C(R7)N(R8)—, and tautomers thereof, and where R4 and R5 taken together is —C(R11)═C(R12)C(R13)═C(R14) 1 12, —, where R,R,R 6, R 7, R8, R I1, R R 13, R 14, and X are described. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.

摘要翻译： 现在已经发现某些新的杂环衍生物已经提供了意想不到的杀虫活性。 这些化合物由式（I）表示：R优选的是式（I）的那些化合物，其中R 2和R 3一起是-NCH（R 6）CH（ N（R 8） - （R 8）N（R 8） - 或-CHN-C（R' 7）N（R 8） - 及其互变异构体，其中R 4和R 5一起是-C （R 11）-C（R 12）C（R 13）-C（R 14）12， - ，其中R，R，R 6，R 7，R 8，R 11，R R 13，R 14和X。 此外，还公开了包含杀虫有效量的至少一种式（I）化合物和任选的有效量的至少一种第二化合物与至少一种与杀虫相容的载体的组合物; 以及控制昆虫的方法，包括将所述组合物施用于存在昆虫或预期存在的场所。