公开(公告)号：US20190127330A1

公开(公告)日：2019-05-02

申请号：US15857701

申请日：2017-12-29

申请人： NATIONAL TAIWAN NORMAL UNIVERSITY

发明人： Ching-Fa YAO

IPC分类号： C07D221/18 ,  C07D491/056 ,  C07D471/04 ,  C07D495/04

CPC分类号： C07D221/18 ,  C07D471/04 ,  C07D491/056 ,  C07D495/04

摘要： A method for preparing indenoisoquinoline derivatives represented by the following formula (I) is disclosed, which comprises the following steps: (A) providing a first reactant represented by the following formula (II) and a second reactant represented by the following formula (III): and(B) reacting the first reactant represented by the formula (II) and the second reactant represented by the formula (III) in a solvent and selectively adding R2NH2 therein, to obtain the indenoisoquinoline derivatives represented by the formula (I), wherein, R1, R2, R3, A, X, Y, Z, m and n are defined in the specification.

公开(公告)号：US20180325898A1

公开(公告)日：2018-11-15

申请号：US16042206

申请日：2018-07-23

申请人： Paul S. Charifson ,  Kevin Michael Cottrell ,  Hongbo Deng ,  John P. Duffy ,  Huai Gao ,  Simon Giroux ,  Jeremy Green ,  Katrina Lee Jackson ,  Joseph M. Kennedy ,  David J. Lauffer ,  Mark Willem Ledeboer ,  Pan Li ,  John Patrick Maxwell ,  Mark A. Morris ,  Albert Charles Pierce ,  Nathan D. Waal ,  Jinwang Xu

发明人： Paul S. Charifson ,  Kevin Michael Cottrell ,  Hongbo Deng ,  John P. Duffy ,  Huai Gao ,  Simon Giroux ,  Jeremy Green ,  Katrina Lee Jackson ,  Joseph M. Kennedy ,  David J. Lauffer ,  Mark Willem Ledeboer ,  Pan Li ,  John Patrick Maxwell ,  Mark A. Morris ,  Albert Charles Pierce ,  Nathan D. Waal ,  Jinwang Xu

IPC分类号： A61K31/506 ,  A61K9/48 ,  C07D417/10 ,  A61K41/00 ,  C07D521/00 ,  C07D495/04 ,  C07D491/056 ,  C07D491/048 ,  C07D471/04 ,  C07D417/14 ,  C07D417/04 ,  C07D413/10 ,  C07D413/04 ,  C07D409/14 ,  C07D409/04 ,  C07D239/42 ,  C07D403/10 ,  C07D403/04 ,  C07D401/04 ,  C07D413/14 ,  C07D405/14 ,  C07D401/14 ,  A61K47/55 ,  A61K31/53 ,  A61K47/54 ,  A61K31/5377 ,  A61K9/20

CPC分类号： C07D401/14 ,  A61K9/20 ,  A61K9/48 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61K41/0038 ,  A61K47/545 ,  A61K47/55 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D491/048 ,  C07D491/056 ,  C07D495/04 ,  C07D521/00

摘要： The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

公开(公告)号：US20180298019A1

公开(公告)日：2018-10-18

申请号：US15769065

申请日：2016-10-18

申请人： SUNSHINE LAKE PHARMA CO., LTD.

发明人： Bing LIU ,  Weihong ZHANG ,  Yingjun ZHANG

IPC分类号： C07D491/056 ,  A61P35/04

CPC分类号： C07D491/056 ,  A61K31/337 ,  A61K31/427 ,  A61K31/436 ,  A61K31/517 ,  A61K31/5355 ,  A61K31/573 ,  A61K31/7072 ,  A61K45/06 ,  A61K2300/00 ,  A61P35/04

摘要： The invention relates to a salt, a hydrate or a crystalline form of an EGFR inhibitor, and use thereof. Specifically it relates to 4-[(3-chloro-4-fluorophenyl) amino]-7-methoxy-6-[3-[(1R,6S)-2,5-dioxa-8-azabicyclo [4.3.0] nonan-8-yl] propoxy]quinazoline dimethanesulfonate, hydrate and a crystalline form thereof; the invention also relates to a preparation method of the crystalline form disclosed herein, a pharmaceutical composition containing the crystalline form, and uses thereof for treating proliferative disorders.

公开(公告)号：US20180228776A1

公开(公告)日：2018-08-16

申请号：US15751273

申请日：2016-08-10

申请人： MOCHIDA PHARMACEUTICAL CO., LTD.

发明人： Fumihiko SAITOH ,  Tomoyuki KAMINO ,  Motoi NAKAHARA

IPC分类号： A61K31/427

CPC分类号： A61K31/427 ,  A61K31/395 ,  A61K31/4162 ,  A61K31/428 ,  A61K31/4355 ,  A61K31/436 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/55 ,  A61K31/553 ,  A61K31/695 ,  C07C53/00 ,  C07C53/10 ,  C07C53/18 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D491/056 ,  C07D491/107 ,  C07D498/04 ,  C07D498/14 ,  C07D519/00

摘要： The present invention provides a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof or a solvate of these. A compound having Nrf2 activation ability is provided by the present invention.

公开(公告)号：US10035808B1

公开(公告)日：2018-07-31

申请号：US15957872

申请日：2018-04-19

申请人： Chengyuan Liang ,  Danni Tian ,  Minyi Jia

发明人： Chengyuan Liang ,  Danni Tian ,  Minyi Jia

IPC分类号： C07D491/056

CPC分类号： C07D491/056

摘要： An isatin peroxo compound has the following formula (I): R1 is H, halogen, or C1-3 alkyl, and R2, is H, C1-3 alkyl, or phenyl.

公开(公告)号：US09987284B2

公开(公告)日：2018-06-05

申请号：US15133378

申请日：2016-04-20

申请人： Vertex Pharmaceuticals Incorporated

发明人： John Patrick Maxwell ,  Paul S. Charifson ,  Qing Tang ,  Steven M. Ronkin ,  Katrina Lee Jackson ,  Albert Charles Pierce ,  David J. Lauffer ,  Pan Li ,  Simon Giroux ,  Jinwang Xu ,  Kevin Michael Cottrell ,  Mark A. Morris ,  Nathan D. Waal ,  John J. Court ,  Wenxin Gu ,  Hongbo Deng

IPC分类号： A61K31/4245 ,  C07D271/12 ,  A61K31/5377 ,  C07D513/04 ,  A61K31/506 ,  A61K31/5386 ,  C07D241/40 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D473/40 ,  C07D475/00 ,  C07D487/04 ,  C07D491/048 ,  C07D498/08 ,  C07D241/42 ,  C07D413/04 ,  C07D241/44 ,  C07D491/052 ,  C07D401/12 ,  C07D413/14 ,  C07D491/056 ,  C07D491/08

CPC分类号： A61K31/5377 ,  A61K31/506 ,  A61K31/5386 ,  C07D241/40 ,  C07D241/42 ,  C07D241/44 ,  C07D271/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D473/40 ,  C07D475/00 ,  C07D487/04 ,  C07D491/048 ,  C07D491/052 ,  C07D491/056 ,  C07D491/08 ,  C07D498/08 ,  C07D513/04

摘要： Provided are compounds of Formula (I): wherein R1, R2, X, Ring A, Ring B, and Ring C are as defined herein. Compounds of Formula (I) are useful as inhibitors of DNA-PK. Also provided are pharmaceutical compositions comprising said compounds and methods of using the compounds and compositions in the treatment of various diseases, conditions, and disorders.

公开(公告)号：US09932317B2

公开(公告)日：2018-04-03

申请号：US14385268

申请日：2013-03-19

申请人： Imperial Innovations Limited ,  Emory University

发明人： Robert Brown ,  Matthew John Fuchter ,  Nadine Chapman-Rothe ,  Nitipol Srimongkolpithak ,  Joachim Caron ,  James Snyder ,  Thota Ganesh ,  Jin Liu ,  Aiming Sun

IPC分类号： C07D401/12 ,  C07D401/14 ,  A61K31/517 ,  C07D239/95 ,  C07D405/14 ,  C07D491/056 ,  C07D403/12 ,  C07D401/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/551

CPC分类号： C07D239/95 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/551 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D491/056

摘要： This invention relates to quinazoline compounds of Formula (I) which are inhibitors of the histone lysine methyltransferase (HKMTase) EZH2, and to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of EZH2 provides a therapeutic or prophylactic effect.

公开(公告)号：US20180051033A1

公开(公告)日：2018-02-22

申请号：US15713956

申请日：2017-09-25

申请人： TRUSTEES OF BOSTON UNIVERSITY

发明人： Ulla Hansen ,  Scott Schaus ,  Trevor Grant ,  Joshua Bishop ,  John Kavouris ,  Lisa M. Christadore

IPC分类号： C07D491/056 ,  C07D215/227

CPC分类号： C07D491/056 ,  C07D215/20 ,  C07D215/227

摘要： The present invention is directed to methods, compositions and kits for treatment of cancer, e.g. heptacellular carcinoma. In some embodiments, the present invention discloses the use of a small-molecule compound of formula (I)-(XXVI) and (III′) as disclosed herein to inhibit transcription factor Late SV40 Factor (LSF) for treatment of cancer, e.g., HCC.

公开(公告)号：US20180043009A1

公开(公告)日：2018-02-15

申请号：US15603069

申请日：2017-05-23

申请人： Arbutus Biopharma Corporation

发明人： Muthiah Manoharan ,  Kallanthottathil G. Rajeev ,  Muthusamy Jayaraman ,  David Butler ,  Jayaprakash K. Nair ,  Martin Maier ,  Laxman Eltepu

IPC分类号： A61K39/39 ,  A61K31/713 ,  A61K39/00 ,  A61K47/10 ,  A61K47/18 ,  A61K47/20 ,  A61K47/28 ,  C07C229/08 ,  C07C229/30 ,  C07C237/16 ,  C07C251/38 ,  C07C251/78 ,  C07C271/12 ,  C07C271/20 ,  C07C323/25 ,  C07D203/10 ,  C07D317/28 ,  C07D319/06 ,  C12N15/11 ,  C12N15/113 ,  A61K9/127

CPC分类号： A61K47/44 ,  A61K9/1272 ,  A61K31/7088 ,  A61K31/713 ,  A61K39/00 ,  A61K39/39 ,  A61K47/10 ,  A61K47/18 ,  A61K47/20 ,  A61K47/28 ,  A61K2039/55555 ,  A61K2039/55561 ,  C07C229/08 ,  C07C229/30 ,  C07C237/16 ,  C07C251/38 ,  C07C251/78 ,  C07C271/12 ,  C07C271/20 ,  C07C323/25 ,  C07D203/10 ,  C07D317/28 ,  C07D317/44 ,  C07D317/46 ,  C07D317/72 ,  C07D319/06 ,  C07D405/12 ,  C07D491/056 ,  C07D491/113 ,  C12N15/111 ,  C12N15/113 ,  C12N2310/14 ,  C12N2310/3515 ,  C12N2320/32 ,  Y02A50/464

摘要： The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure wherein R1 and R2 are each independently for each occurrence optionally substituted C10-C30alkyl, optionally substituted C10-C30alkenyl, optionally substituted C10-C30alkynyl, optionally substituted C10-C30acyl, or -linker-ligand; R3 is H, optionally substituted C1-C10alkyl, optionally substituted C2-C10alkenyl, optionally substituted C2-C10alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, ω-aminoalkyls, ω-(substituted)aminoalkyls, ω-phosphoalkyls, ω-thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; E is O, S, N(Q), C(O), N(Q)C(O), C(O)N(Q), (Q)N(CO)O, O(CO)N(Q), S(O), NS(O)2N(Q), S(O)2, N(Q)S(O)2, SS, O═N, aryl, heteroaryl, cyclic or heterocycle; and, Q is H, alkyl, ω-aminoalkyl, ω-(substituted)aminoalky, ω-phosphoalkyl or ω-thiophosphoalkyl.

公开(公告)号：US09889122B2

公开(公告)日：2018-02-13

申请号：US15370958

申请日：2016-12-06

申请人： H. Lundbeck A/S

发明人： Jorgen Eskildsen ,  Anette Graven Sams ,  Ask Puschl

IPC分类号： C07D213/84 ,  C07D405/12 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/44 ,  C07D213/71 ,  C07D213/74 ,  C07D213/85 ,  C07D239/34 ,  C07D491/056 ,  C07D213/40 ,  C07D213/61 ,  C07D213/647 ,  C07D213/65 ,  A61K45/06 ,  A61K31/4427 ,  A61K31/4355 ,  A61K31/436 ,  A61K31/505

CPC分类号： A61K31/44 ,  A61K31/4355 ,  A61K31/436 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/505 ,  A61K45/06 ,  C07D213/40 ,  C07D213/61 ,  C07D213/647 ,  C07D213/65 ,  C07D213/71 ,  C07D213/74 ,  C07D213/84 ,  C07D213/85 ,  C07D239/34 ,  C07D405/12 ,  C07D491/056

摘要： The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor.