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：US20180044307A1

公开(公告)日：2018-02-15

申请号：US15552053

申请日：2016-03-04

申请人： UNICHEM LABORATORIES LIMITED

发明人： Dhananjay G. SATHE ,  Dnyaneshwar V. GAWAS ,  Sanjay Bhaskar KEKAR ,  Jotirling Ramling MALI

IPC分类号： C07D295/15

CPC分类号： C07D295/15

摘要： A process for the preparation of Ranolazine (I) and its acid addition salts and the process for the preparation of compound of formula (7).

公开(公告)号：US20170355678A1

公开(公告)日：2017-12-14

申请号：US15688310

申请日：2017-08-28

申请人： Exelixis, Inc.

发明人： Lynne Canne Bannen ,  Diva Sze-Ming Chan ,  Jeff Chen ,  Lisa Esther Dalrymple ,  Timothy Patrick Forsyth ,  Tai Phat Huynh ,  Vasu Jammalamadaka ,  Richard George Khoury ,  James William Leahy ,  Morrison B. Mac ,  Grace Mann ,  Larry W. Mann ,  John M. Nuss ,  Jason Jevious Parks ,  Craig Stacy Takeuchi ,  Yong Wang ,  Wei Xu

IPC分类号： C07D215/233 ,  C07D239/94 ,  A61K31/4725 ,  C07D239/88 ,  C07D405/14 ,  A61K31/5377 ,  A61K31/505 ,  A61K31/517 ,  C07D295/15 ,  C07D413/12 ,  A61K31/506 ,  C07D401/12 ,  A61K31/501 ,  C07D413/14 ,  C07D215/46 ,  A61K31/47 ,  C12Q1/48 ,  A61K31/4709 ,  C07D403/12 ,  C07D215/22 ,  C07D215/36 ,  C07D417/12 ,  C07D215/38 ,  C07D401/14 ,  A61K31/496

CPC分类号： C07D215/233 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/501 ,  A61K31/505 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  C07D215/22 ,  C07D215/36 ,  C07D215/38 ,  C07D215/46 ,  C07D239/88 ,  C07D239/94 ,  C07D295/15 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C12Q1/485 ,  G01N2500/04 ,  Y02A50/393

摘要： The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

公开(公告)号：US20170313920A1

公开(公告)日：2017-11-02

申请号：US15649869

申请日：2017-07-14

申请人： Thomas P. Daly

发明人： Thomas P. Daly

IPC分类号： C09K3/00 ,  C07C205/15 ,  C07F9/38 ,  C07F9/09 ,  C07D295/15 ,  C07D295/088 ,  C07D213/74 ,  C07C309/14 ,  C07C229/22 ,  C07C229/12 ,  C07C219/22 ,  C07C219/06 ,  C07C217/48 ,  C07C217/28 ,  C07C217/08 ,  C07C215/08 ,  C07C205/40 ,  C07F9/58 ,  C11D1/66

摘要： Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

公开(公告)号：US20170247383A1

公开(公告)日：2017-08-31

申请号：US15320057

申请日：2015-06-25

申请人： THE GENERAL HOSPITAL CORPORATION

发明人： Randall T. PETERSON ,  Andrew J. RENNEKAMP ,  David KOKEL ,  You WANG

IPC分类号： C07D487/10 ,  C07D295/15 ,  C07D295/192 ,  C07D307/81 ,  C07D295/155 ,  A61K49/00 ,  C07D215/12

CPC分类号： C07D487/10 ,  A61K49/0008 ,  C07D215/12 ,  C07D295/15 ,  C07D295/155 ,  C07D295/192 ,  C07D307/81

摘要： The invention described herein relates generally to neuroactive compounds and compositions for the treatment psychotic disorders, methods for treating psychosis using these neuroactive compounds, and methods for screening for novel neuroactive compounds. Certain aspects are directed to a family of compounds called “finazines.” Certain aspects are directed to in vivo screening methods using high-through-put behavioral assays in zebrafish.

公开(公告)号：US20170121279A1

公开(公告)日：2017-05-04

申请号：US15265064

申请日：2016-09-14

申请人： The Board of Regents of the University of Texas System

发明人： Daniel J. SIEGWART ,  Kejin ZHOU

IPC分类号： C07C321/14 ,  A61K31/7125 ,  A61K47/20 ,  C07D295/15 ,  A61K47/22

CPC分类号： C07C321/14 ,  A61K9/5146 ,  A61K31/7125 ,  A61K47/20 ,  A61K47/22 ,  A61K47/59 ,  C07C323/52 ,  C07D295/15

摘要： Modular dendrimers with cationic groups and lipophilic groups are provided herein. In some aspects, the dendrimers provided herein may be formulated in compositions which contain a nucleic acid and one or more helper excipients. In some aspects, these compositions may also be used to treat diseases or disorders with a therapeutic nucleic acid.

公开(公告)号：US09624166B2

公开(公告)日：2017-04-18

申请号：US13391407

申请日：2010-08-27

申请人： Yonghong Deng ,  Louis Plamondon ,  Cuixiang Sun ,  Xiao-Yi Xiao ,  Jingye Zhou ,  Joyce A. Sutcliffe ,  Magnus P. Ronn

发明人： Yonghong Deng ,  Louis Plamondon ,  Cuixiang Sun ,  Xiao-Yi Xiao ,  Jingye Zhou ,  Joyce A. Sutcliffe ,  Magnus P. Ronn

IPC分类号： A61K31/65 ,  A61P31/04 ,  C07C237/26 ,  C07C311/08 ,  C07C307/10 ,  C07C311/09 ,  C07C311/13 ,  C07C311/21 ,  C07C311/29 ,  C07C311/44 ,  C07D205/04 ,  C07D207/12 ,  C07D207/16 ,  C07D209/44 ,  C07D209/52 ,  C07D211/54 ,  C07D211/60 ,  C07D213/70 ,  C07D213/74 ,  C07D213/82 ,  C07D223/06 ,  C07D231/18 ,  C07D233/60 ,  C07D233/84 ,  C07D295/15 ,  C07D307/64

CPC分类号： C07C311/08 ,  C07C237/26 ,  C07C307/10 ,  C07C311/09 ,  C07C311/13 ,  C07C311/21 ,  C07C311/29 ,  C07C311/44 ,  C07C2101/02 ,  C07C2101/04 ,  C07C2101/08 ,  C07C2101/14 ,  C07C2103/40 ,  C07C2103/44 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2603/40 ,  C07C2603/44 ,  C07C2603/46 ,  C07D205/04 ,  C07D207/12 ,  C07D207/16 ,  C07D209/44 ,  C07D209/52 ,  C07D211/54 ,  C07D211/60 ,  C07D213/70 ,  C07D213/74 ,  C07D213/82 ,  C07D223/06 ,  C07D231/18 ,  C07D233/60 ,  C07D233/84 ,  C07D295/15 ,  C07D307/64

摘要： The present invention is directed to a compound represented by Structural Formula (1): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I) and its therapeutic use.

公开(公告)号：US20160368885A1

公开(公告)日：2016-12-22

申请号：US15114494

申请日：2015-02-03

申请人： GIFU UNIVERSITY

发明人： Kazuo Kuwata

IPC分类号： C07D295/15 ,  C07C57/145

CPC分类号： C07D295/15 ,  C07C57/145

摘要： An object of the present invention is to provide an anti-prion compound that has high crystallinity and is highly stable in the crystalline form and to provide a medicament for preventing, ameliorating or treating a prion disease. The present invention provides a maleic acid salt of a compound represented by formula (1):

摘要翻译： 本发明的目的是提供具有高结晶度并且在结晶形式中高度稳定并提供用于预防，改善或治疗朊病毒疾病的药物的抗朊病毒化合物。 本发明提供式（1）表示的化合物的马来酸盐：

公开(公告)号：US20160362595A1

公开(公告)日：2016-12-15

申请号：US15111443

申请日：2013-12-20

申请人： NALCO COMPANY

发明人： Erick J. Acosta ,  Tran-Bich Cao

IPC分类号： C09K8/52 ,  C08G65/00 ,  C07D295/15

CPC分类号： C09K8/52 ,  C07D295/088 ,  C07D295/15 ,  C08G65/00 ,  C09K2208/22 ,  C10L1/232 ,  C10L1/233 ,  C10L1/2387 ,  C10L1/2462 ,  C10L1/2475 ,  C10L3/107 ,  C10L2230/14

摘要： Disclosed herein are beta-amino ester surfactant compounds and compositions useful in applications relating to inhibition of gas hydrate agglomerates in the production, transportation, storage, and separation of crude oil and natural gas. Also disclosed herein are methods of using the compounds and compositions as gas hydrate inhibitors, particularly in applications relating to the production, transportation, storage, and separation of crude oil and natural gas.

摘要翻译： 本文公开了β-氨基酯表面活性剂化合物和组合物，其用于涉及在原油和天然气的生产，运输，储存和分离中气体水合物附聚物的抑制。 本文还公开了将化合物和组合物用作气体水合物抑制剂的方法，特别是在与原油和天然气的生产，运输，储存和分离有关的应用中。

公开(公告)号：US09464032B2

公开(公告)日：2016-10-11

申请号：US14001203

申请日：2012-02-23

申请人： Jean-Michel Bolla ,  Jean Michel Brunel ,  Joseph Pierre Félix Casanova ,  Vannina Lorenzi ,  Liliane Berti

发明人： Jean-Michel Bolla ,  Jean Michel Brunel ,  Joseph Pierre Félix Casanova ,  Vannina Lorenzi ,  Liliane Berti

IPC分类号： A61K31/32 ,  C07C211/22 ,  A61K31/132 ,  A61K31/16 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/4375 ,  A61K31/495 ,  A61K31/5375 ,  A61K45/06 ,  C07C211/21 ,  C07C233/38 ,  C07D207/27 ,  C07D295/13 ,  A01N33/02 ,  A01N37/18 ,  A01N43/36 ,  A01N43/60 ,  A01N43/84 ,  A23L3/3526 ,  A61K8/41 ,  A61K8/42 ,  A61K8/49 ,  A61K31/131 ,  A61K31/165 ,  A61K31/431 ,  A61K31/546 ,  A61K31/65 ,  A61K31/7048 ,  C07D295/15

CPC分类号： C07C211/22 ,  A01N33/02 ,  A01N37/18 ,  A01N43/36 ,  A01N43/60 ,  A01N43/84 ,  A23L3/3526 ,  A61K8/41 ,  A61K8/42 ,  A61K8/49 ,  A61K8/4913 ,  A61K8/494 ,  A61K31/131 ,  A61K31/132 ,  A61K31/16 ,  A61K31/165 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/431 ,  A61K31/4375 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/546 ,  A61K31/65 ,  A61K31/7048 ,  A61K45/06 ,  C07C211/21 ,  C07C233/38 ,  C07D207/27 ,  C07D295/13 ,  C07D295/15 ,  Y02A50/473 ,  Y02A50/481 ,  A61K2300/00

摘要： The present invention relates to the use of polyaminoisoprenyl derivatives in antibiotic or antiseptic treatment of bacteria including those presenting multiple drug resistance (MDR), in particular as efflux pump inhibitors. It also relates to novel polyaminoisoprenyl derivatives, compositions comprising the same, process for preparing the same, and use thereof in antibiotic or antiseptic treatment.

摘要翻译： 本发明涉及聚氨基异戊二烯基衍生物在抗菌素或抗菌处理细菌中的用途，包括具有多重耐药性（MDR）的细菌，特别是作为外排泵抑制剂。 它还涉及新的聚氨基异戊二烯基衍生物，包含其的组合物，其制备方法及其在抗生素或防腐处理中的用途。