公开(公告)号：US20180140600A1

公开(公告)日：2018-05-24

申请号：US15579429

申请日：2016-05-27

Applicant: MARINE BIOMEDICAL RESEARCH INSTITUTE OF QINGDAO CO., LTD.

Inventor： Wenbao LI ,  Tianwen SUN ,  Shixiao WANG ,  Jianchun ZHAO ,  Bing CAI ,  Huashi GUAN

IPC: A61K31/496 ,  C07B59/00 ,  C07D233/64 ,  C07D403/06 ,  A61P35/00

CPC classification number: A61K31/496 ,  A61P35/00 ,  C07B59/00 ,  C07B59/002 ,  C07D233/64 ,  C07D403/06

Abstract: Provided are a deuterium-substituted dehydrophenylahistin-like compound, preparation method thereof and use in a preparation of antitumor drugs. The deuterium-substituted dehydrophenylahistin-like compound has a structure of general formula (I), and a synthesis method thereof comprises: firstly conducting a condensation reaction of diacetyldiketopiperazine and an aldehyde intermediate a or a deuterated aldehyde compound b to form a heterocyclic compound c or a deuterium-containing heterocyclic compound d, which is then subjected to a condensation reaction with benzaldehyde and a deuterium-substituted benzaldehyde-like compound to form the deuterium-substituted dehydrophenylahistin-like compound. Also provided are a highly effective deuterated aldehyde intermediate with a high deuterium substitution rate and a deuterium-containing heterocycle intermediate, and a synthesis method thereof. An experiment shows that the deuterium-substituted dehyd-rophenylahistin-like compound provided by the present invention has an effect on tubulin depolymerization and can treat a refractory solid tumor or lymphoma. The present invention provides a method for researching and developing antitumor drugs of the related compound.

公开(公告)号：US20180134691A1

公开(公告)日：2018-05-17

申请号：US15843192

申请日：2017-12-15

Applicant: NUHOPE, LLC

Inventor： James R. Connor ,  Sang Yong Lee ,  Thomas James Brown ,  Phillip Martin Cowley

IPC: C07D405/06 ,  C07D403/06 ,  A61K31/513 ,  C07D239/60 ,  C07D401/06

CPC classification number: C07D405/06 ,  A61K31/513 ,  C07D239/60 ,  C07D401/06 ,  C07D403/06

Abstract: Provided are methods and compositions for use in therapy, and in particular for treating cancer, preferably drug-resistant cancer, and/or radiation resistant cancer. The compounds may be used for reducing tumor size in a mammalian subject and for inducing apoptosis in a tumor cell. The methods are effective on tumor cells that are resistant to drugs such as temozolomide, doxorubicin, and geldanamycin, as well as non-resistant tumor cells. Further provided are barbiturate and thiobarbiturates diene compounds for use in treating cancer, and uses, methods and compositions relating to these compounds.

公开(公告)号：US09956302B2

公开(公告)日：2018-05-01

申请号：US15782755

申请日：2017-10-12

Applicant: Graybug Vision, Inc.

Inventor： Jeffrey L. Cleland ,  Ming Yang ,  John G. Bauman ,  Nu Hoang ,  Emmett Cunningham

IPC: C07D403/06 ,  A61K47/54 ,  A61K47/59 ,  A61K47/55 ,  A61K47/60 ,  C07D513/04 ,  C07D495/04 ,  C07C69/73

CPC classification number: A61K47/54 ,  A61K47/542 ,  A61K47/543 ,  A61K47/55 ,  A61K47/59 ,  A61K47/593 ,  A61K47/60 ,  C07C69/73 ,  C07C2601/08 ,  C07D403/06 ,  C07D495/04 ,  C07D513/04

Abstract: The disclosure describes prodrugs and derivatives of prostaglandins, carbonic anhydrase inhibitors, kinase inhibitors, beta-adrenergic receptor antagonists and other drugs, as well as controlled delivery formulations containing such prodrugs and derivatives, for the treatment of ocular disorders.

公开(公告)号：US20180111894A1

公开(公告)日：2018-04-26

申请号：US15846198

申请日：2017-12-18

Applicant: Mark G. DeGiacomo

Inventor： Hassan Pajouhesh ,  Richard Holland ,  Lingyun Zhang ,  Hossein Pajouhesh ,  Jason Lamontagne ,  Brendan Whelan

IPC: C07C237/06 ,  C07C237/22 ,  C07D265/30 ,  C07D231/14 ,  C07C237/04 ,  C07D241/08 ,  C07D413/06 ,  C07D401/12 ,  C07D205/04 ,  C07D413/04 ,  C07D403/06 ,  C07D403/04 ,  C07D401/04 ,  C07D235/14 ,  C07D211/60 ,  C07D207/16 ,  C07C237/24

CPC classification number: C07C237/06 ,  A61K31/401 ,  A61K31/454 ,  A61K31/5377 ,  C07C237/04 ,  C07C237/22 ,  C07C237/24 ,  C07C2601/02 ,  C07C2601/14 ,  C07D205/04 ,  C07D207/16 ,  C07D211/60 ,  C07D231/14 ,  C07D235/14 ,  C07D241/08 ,  C07D265/30 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D413/04 ,  C07D413/06

Abstract: The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns compounds (e.g., compounds according to any of Formulas (I)-(XIII) and in particular Formula (X), and Compounds (1)-(236) of Table 1) that are useful in treatment of a variety of diseases and conditions.

公开(公告)号：US20180105509A1

公开(公告)日：2018-04-19

申请号：US15567668

申请日：2016-04-20

Applicant: ALMIRALL, S.A.

Inventor： James DUFFY ,  Mark Stuart CHAMBERS ,  Alastair RAE ,  James OSBORNE ,  Isabelle Anne LEMASSON ,  Michael Daniel GOLDSMITH ,  Andrew SHARPE ,  Silvia FONQUERNA POU

IPC: C07D401/12 ,  C07D231/38 ,  C07D249/06 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  A61P25/02

CPC classification number: C07D401/12 ,  A61P25/02 ,  C07D231/38 ,  C07D249/06 ,  C07D249/14 ,  C07D401/04 ,  C07D401/14 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14

Abstract: The present invention relates to novel aminoindazolyl derivative compounds of Formula (I), the use of said compounds in treating diseases mediated by modulation of voltage-gated sodium channels in particular Nav1.7 AND to compositions containing said derivatives.

公开(公告)号：US09944627B2

公开(公告)日：2018-04-17

申请号：US15590394

申请日：2017-05-09

Applicant: National Taiwan University

Inventor： Ken-Tsung Wong ,  Chung-Chih Wu ,  Tanmay Chatterjee ,  Ting-An Lin ,  Wei-Lung Tsai ,  Meng-Jung Wu

IPC: C07D403/02 ,  C09K11/07 ,  C07D487/10 ,  C07D255/02 ,  C07D221/06 ,  C07D221/22 ,  C07D253/065 ,  H01L51/00 ,  C07D403/12 ,  C07D403/06 ,  C07D403/08 ,  C07D403/10

CPC classification number: C07D403/02 ,  C07D221/06 ,  C07D221/22 ,  C07D253/065 ,  C07D255/02 ,  C07D403/06 ,  C07D403/08 ,  C07D403/10 ,  C07D403/12 ,  C07D487/10 ,  C09K11/07 ,  H01L51/0052 ,  H01L51/0059 ,  H01L51/0062 ,  H01L51/0067 ,  H01L51/0072 ,  H01L51/5012 ,  H01L51/5016 ,  H01L51/5028

Abstract: The present invention relates to compounds of the formula (1), to the use thereof in electroluminescent devices, and particularly organic electroluminescence devices, comprising said compounds according to the invention.

公开(公告)号：US20180086746A1

公开(公告)日：2018-03-29

申请号：US15719165

申请日：2017-09-28

Applicant: University of Southern California

Inventor： Robert D. Ladner ,  Bruno Giethlen

IPC: C07D413/06 ,  C07D403/06 ,  C12Q1/68 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/513

CPC classification number: C07D413/06 ,  A61K31/496 ,  A61K31/513 ,  A61K31/5377 ,  C07D403/06 ,  C12Q1/6876 ,  C12Q2600/158

Abstract: Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions in a method of treating cancer. The dUTPase inhibitors disclosed contain a uracil isostere in the molecule represented by a 2,6-diketopiperazine moiety. Thioanalogs of the uracil isostere where a thione replaces each of the ketone are also disclosed.

公开(公告)号：US09926303B2

公开(公告)日：2018-03-27

申请号：US14293642

申请日：2014-06-02

Applicant: Medivation Technologies LLC

Inventor： Bing Wang ,  Daniel Chu ,  Yongbo Liu ,  Quan Jiang ,  Lei Lu

IPC: C07D405/06 ,  C07D249/08 ,  C07D401/04 ,  C07D403/06 ,  C07D471/06

CPC classification number: C07D405/06 ,  C07D249/08 ,  C07D401/04 ,  C07D403/06 ,  C07D471/06

Abstract: Provided herein are processes for synthesizing dihydropyridophthalazinone derivatives, such as for example, 5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one and its stereoisomers, which are potent poly(ADP-ribose)polymerase (PARP) inhibitors as well as novel synthetic intermediate compounds.

公开(公告)号：US09890126B2

公开(公告)日：2018-02-13

申请号：US15065571

申请日：2016-03-09

Applicant: BOARD OF TRUSTEES OF NORTHERN ILLINOIS UNIVERSITY ,  BERYLLIUM DISCOVERY CORP.

Inventor： Timothy J. Hagen ,  Zheng Zhang ,  Zachary Lazowski ,  Michael Clare ,  Darren W. Begley

IPC: C07D233/64 ,  C07D403/12 ,  C07F9/6571 ,  C07D239/47 ,  C07D417/12 ,  A61K45/06 ,  A61K31/4164 ,  A61K31/506 ,  C07D401/12 ,  C07D403/06 ,  C07D405/06 ,  C07D405/12 ,  A61K31/4174 ,  A61K31/4178 ,  C07D413/12

CPC classification number: C07D233/64 ,  A61K31/4164 ,  A61K31/4174 ,  A61K31/4178 ,  A61K31/506 ,  A61K45/06 ,  C07D239/47 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07F9/657136 ,  Y02A50/411 ,  A61K2300/00

Abstract: Antibacterial and antimalarial IspF inhibitor compounds and compositions are described. Methods include administering described compounds and compositions to treat bacterial or parasitic infections and to inhibit parasite or bacterial growth.

公开(公告)号：US20180037590A1

公开(公告)日：2018-02-08

申请号：US15787880

申请日：2017-10-19

Applicant: SUNOVION PHARMACEUTICALS INC.

Inventor： John Emmerson Campbell ,  Michael Charles Hewitt ,  Philip Xinhe Jones ,  Linghong Xie

IPC: C07D498/06 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5383 ,  C07D233/58 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/4985 ,  C07D498/04 ,  C07D409/14 ,  C07D413/06 ,  C07D417/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/06 ,  C07D519/00 ,  C07D498/14 ,  C07D491/056 ,  C07D487/04 ,  C07D471/14 ,  C07D471/04 ,  C07D403/06 ,  C07D471/06 ,  C07D401/06

CPC classification number: C07D498/06 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5383 ,  C07D233/58 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D417/06 ,  C07D471/04 ,  C07D471/06 ,  C07D471/14 ,  C07D487/04 ,  C07D491/056 ,  C07D498/04 ,  C07D498/14 ,  C07D519/00

Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.