公开(公告)号：US09809595B2

公开(公告)日：2017-11-07

申请号：US14770708

申请日：2014-02-27

Applicant: OKINAWA INSTITUTE OF SCIENCE AND TECHNOLOGY SCHOOL CORPORATION

Inventor： Fadel Alexis Samatey ,  Vladimir A Meshcheryakov ,  Hideyuki Matsunami ,  Akio Kitao

IPC: C07D473/08 ,  A61K31/505 ,  A61K31/522 ,  C12Q1/02 ,  C12Q1/18 ,  C07D239/49

CPC classification number: C07D473/08 ,  A61K31/505 ,  A61K31/522 ,  C07D239/49 ,  C12Q1/025 ,  C12Q1/18 ,  G01N2333/255 ,  G01N2500/04 ,  Y02A50/406 ,  Y02A50/473 ,  Y02A50/475

Abstract: The present invention relates to a method for screening a compound that inhibits secretion of toxins into host-cell cytoplasm by virulent bacteria using a needle type III secretion system. The compound of the invention is selected by screening for a compound which interacts with a loop region of the cytoplasmic domain of the membrane protein FlhB from Salmonella typhimurium or a paralog thereof. Compositions including the compound of the invention, use of the compound, and methods of treating disorders caused by virulent bacteria are also provided.

公开(公告)号：US20170050966A1

公开(公告)日：2017-02-23

申请号：US15305892

申请日：2015-04-23

Applicant: HYDRA BIOSCIENCES, INC.

Inventor： Blaise S. Lippa ,  Xinyuan Wu ,  Qingyi Li ,  Iwona Wrona ,  Andrew J. Jackson ,  Bertrand L. Chenard ,  Christopher Matthew Liu ,  Guohua Liang ,  Matthew F. Baevsky ,  Richard Alan Earl ,  Lisa Mcqueen ,  Jared Smit ,  Brett A. Cowans

IPC: C07D473/08

CPC classification number: C07D473/08 ,  C07B2200/13

Abstract: The present invention relates to compounds of the Formula (I), or a pharmaceutically acceptable salt, pharmaceutical preparation, or pharmaceutical composition thereof, and their use for the treatment of pain, inflammatory disease, neuropathy, dermatological disorders, pulmonary conditions, and cough, as well as inhibiting the Transient Receptor Potential A1 ion channel (TRPA1).

Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐，药物制剂或其药物组合物及其用于治疗疼痛，炎性疾病，神经病，皮肤病，肺病和咳嗽的用途， 以及抑制瞬态受体电位A1离子通道（TRPA1）。

公开(公告)号：US09556175B2

公开(公告)日：2017-01-31

申请号：US15070263

申请日：2016-03-15

Applicant: Boehringer Ingelheim International GmbH

Inventor： Frank Himmelsbach ,  Elke Langkopf ,  Matthias Eckhardt ,  Michael Mark ,  Roland Maier ,  Ralf Lotz ,  Mohammad Tadayyon

IPC: C07D473/04 ,  C07D473/06 ,  C07D473/08 ,  C07D519/00

CPC classification number: C07D473/04 ,  C07D473/06 ,  C07D473/08 ,  C07D519/00

Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are as defined herein, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

Abstract translation: 本发明涉及通式为其中R1至R3如本文所定义的取代黄嘌呤，其互变异构体，立体异构体，混合物，其前药及其盐具有有价值的药理学性质，特别是对 酶二肽肽酶-IV（DPP-IV）。

公开(公告)号：US20160229823A1

公开(公告)日：2016-08-11

申请号：US14230833

申请日：2014-03-31

Applicant: PharmatrophiX, Inc.

Inventor： Damodara GOPAL

IPC: C07D295/135 ,  C07D233/72 ,  C07D233/61 ,  C07D295/13 ,  C07D473/08 ,  C07D241/08 ,  C07K5/062

CPC classification number: C07D295/135 ,  A61K38/00 ,  C07B2200/05 ,  C07D233/61 ,  C07D233/72 ,  C07D241/08 ,  C07D295/13 ,  C07D473/08 ,  C07K5/06034

Abstract: The present application is related to deuterated compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders involving degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such deuterated compounds.

Abstract translation: 本申请涉及新型神经营养因子模拟物的氘代化合物。 本申请还公开了通过施用有效量的这种氘代化合物来治疗涉及哺乳动物表达p75的细胞降解或功能障碍的疾病。

公开(公告)号：US09382250B2

公开(公告)日：2016-07-05

申请号：US14113239

申请日：2012-04-20

Applicant: Akinori Goto ,  Mamoru Fukuda

Inventor： Akinori Goto ,  Mamoru Fukuda

IPC: C07B63/00 ,  C07D223/26 ,  C07D473/08 ,  C07D487/04

CPC classification number: C07D473/08 ,  C07B63/00 ,  C07D223/26 ,  C07D487/04

Abstract: The present invention relates to a method for producing a complex crystal composed of two or more different compounds, comprising crystallizing the two or more different compounds under a condition at which menthol is heat melted, and a method for screening a complex crystal. In accordance with the method for producing a complex crystal of the present invention, a complex crystal capable of being used as a drug material can be produced rapidly, simply and efficiently. In addition, in accordance with the method for screening a complex crystal of the present invention, a stable complex crystal can be searched, which is industrially useful.

Abstract translation: 本发明涉及一种由两种或更多种不同化合物组成的复合晶体的制造方法，包括在薄荷醇被热熔融的条件下使两种或更多种不同的化合物结晶，以及筛选复合结晶的方法。 根据本发明的复合结晶的制造方法，可以快速，简单，有效地制造能够作为药物材料使用的复合结晶。 此外，根据本发明的复合晶体的筛选方法，可以搜索在工业上有用的稳定的复合晶体。

公开(公告)号：US09278951B2

公开(公告)日：2016-03-08

申请号：US14114324

申请日：2012-04-30

Applicant: Wiley Youngs ,  Matthew Panzner ,  Claire Tessier ,  Michael Deblock ,  Brian Wright ,  Patrick Wagers ,  Nikki Robishaw

Inventor： Wiley Youngs ,  Matthew Panzner ,  Claire Tessier ,  Michael Deblock ,  Brian Wright ,  Patrick Wagers ,  Nikki Robishaw

IPC: C07D235/02 ,  C07D235/04 ,  C07D233/58 ,  C07D233/60 ,  C07D233/68 ,  C07D401/14 ,  C07D403/12 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D405/06 ,  C07D487/04 ,  C07D403/14 ,  C07D473/08

CPC classification number: C07D401/14 ,  C07D233/58 ,  C07D233/60 ,  C07D233/68 ,  C07D235/02 ,  C07D235/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D473/08 ,  C07D487/04

Abstract: Singly and multiply charged imidazolium cations (ICs) have been identified as a class of chemical compositions that possess potent antineoplastic, antibacterial and antimicrobial properties. The imidazolium cations disclosed demonstrate greater or equivalent potency towards cancerous cells as the current clinical standard, cisplatin. These imidazolium cations, however, achieve this efficacy without any of the known toxic side effects caused by heavy metal-based antineoplastic drugs such as cisplatin.

Abstract translation: 已经将单加和多倍荷电咪唑阳离子（IC）鉴定为具有有效的抗肿瘤，抗细菌和抗微生物特性的一类化学组合物。 所公开的咪唑阳离子表现出对目前临床标准顺铂的癌细胞更大或等效的效力。 然而，这些咪唑阳离子实现了这种功效，而没有由重金属基抗肿瘤药物如顺铂引起的任何已知的毒副作用。

公开(公告)号：US20150307503A1

公开(公告)日：2015-10-29

申请号：US14646092

申请日：2013-11-20

Applicant: DISCOVERYBIOMED, INC.

Inventor： Erik Schwiebert ,  John Streiff ,  John Dixon ,  Hongwu Gao

IPC: C07D487/14 ,  C07D473/08 ,  C07D498/14

CPC classification number: C07D487/14 ,  C07D473/08 ,  C07D498/14

Abstract: Novel CFTR corrector compounds that are effective in rescuing halide efflux, delF508-CFTR protein processing, and apical functional chloride ion transport in a cell are provided. Also provided are methods for treating protein folding disorders (e.g., cystic fibrosis). The methods include administering a CFTR corrector compound or pharmaceutically acceptable salt or prodrug thereof. Methods of rescuing halide efflux in a cell, correcting a processing defect of a delF508-CFTR protein in a cell, and correcting functional delF508-CFTR chloride channels in a cell are also provided.

Abstract translation: 提供了有效拯救细胞中卤化物外排，delF508-CFTR蛋白加工和顶端功能氯离子转运的新型CFTR校正剂化合物。 还提供了治疗蛋白质折叠障碍（例如囊性纤维化）的方法。 所述方法包括施用CFTR校正化合物或其药学上可接受的盐或前药。 还提供了在细胞中拯救卤素流出的方法，校正细胞中delF508-CFTR蛋白的加工缺陷以及校正细胞中的功能性delF508-CFTR氯化物通道。

公开(公告)号：US09108964B2

公开(公告)日：2015-08-18

申请号：US14154885

申请日：2014-01-14

Applicant: Boehringer Ingelheim International GmbH

Inventor： Frank Himmelsbach ,  Elke Langkopf ,  Matthias Eckhardt ,  Roland Maier

IPC: C07D473/04 ,  C07D473/06 ,  C07D473/08

CPC classification number: C07D473/04 ,  C07D473/06 ,  C07D473/08 ,  C07D519/00

Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are as defined herein, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

Abstract translation: 本发明涉及通式为其中R1至R3如本文所定义的取代黄嘌呤，其互变异构体，立体异构体，混合物，其前药及其盐具有有价值的药理学性质，特别是对 酶二肽肽酶-IV（DPP-IV）。

公开(公告)号：US09102619B2

公开(公告)日：2015-08-11

申请号：US14496136

申请日：2014-09-25

Applicant: Chiesi Farmaceutici S.p.A.

Inventor： Maurizio Delcanale ,  Elisabetta Armani ,  Gabriele Amari

IPC: A61K31/44 ,  C07D213/61 ,  C07D213/30 ,  C07D213/89 ,  C07D401/12 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/522 ,  A61K31/5377 ,  A61K31/538 ,  A61K45/06 ,  C07D213/79 ,  C07D405/12 ,  C07D417/12 ,  C07D473/04 ,  A61K31/455 ,  C07D213/38 ,  C07D213/80 ,  C07D473/08

CPC classification number: C07D213/30 ,  A61K31/44 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/455 ,  A61K31/4709 ,  A61K31/522 ,  A61K31/5377 ,  A61K31/538 ,  A61K45/06 ,  C07D213/38 ,  C07D213/61 ,  C07D213/79 ,  C07D213/80 ,  C07D213/89 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12 ,  C07D473/04 ,  C07D473/08

Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.

公开(公告)号：US20150183788A1

公开(公告)日：2015-07-02

申请号：US14409952

申请日：2013-05-15

Applicant: Chengdu Easton Pharmaceutical Co., Ltd.

Inventor： Ying Wang ,  Yongzhe Xiang ,  Guodong Cen ,  Long Huang ,  Jian Liu ,  Ning Zhou ,  Jibing Zhang

IPC: C07D473/08

CPC classification number: C07D473/08 ,  A61K31/437 ,  A61K31/522 ,  C07D473/06

Abstract: The present invention discloses a xanthine derivative having the structure of the following general formula (I) or a pharmaceutically acceptable salt thereof; further discloses a preparation method for the xanthine derivative or a pharmaceutically acceptable salt thereof; and further discloses the use of the xanthine derivative or a pharmaceutically acceptable salt thereof. Through experiments of DPP-IV activity inhibition experiments in vitro, impact on glucose tolerance in normal mice and impact on blood glucose in spontaneous diabetic mice, it proves that the compounds and pharmaceutically acceptable salts thereof show good DPP-IV inhibition activity, can be applied to prepare medicines for treating dipeptidyl peptidase IV-related diseases, and more particularly, can be applied to the use of medicines for treating type II diabetes or diseases of abnormal glucose tolerance.

Abstract translation: 本发明公开了具有以下通式（I）的结构的黄嘌呤衍生物或其药学上可接受的盐; 进一步公开了黄嘌呤衍生物或其药学上可接受的盐的制备方法; 并进一步公开了黄嘌呤衍生物或其药学上可接受的盐的用途。 通过体外DPP-IV活性抑制实验实验，正常小鼠对葡萄糖耐量的影响和对自发性糖尿病小鼠血糖的影响，证明其化合物及其药学上可接受的盐显示出良好的DPP-IV抑制活性，可以应用 制备用于治疗二肽基肽酶IV相关疾病的药物，更具体地，可以应用于用于治疗II型糖尿病或异常葡萄糖耐量异常的药物。