公开(公告)号：US09822080B2

公开(公告)日：2017-11-21

申请号：US15220293

申请日：2016-07-26

申请人： Mironova Innovations, LLC ,  Jan Trampota

发明人： Bohumil Zák ,  Marie Záková ,  Jan Trampota ,  John Olszewski ,  Theodore Gribb, III

IPC分类号： C07D233/84 ,  C07C269/00 ,  C07C221/00 ,  C07C225/06 ,  C07C271/12

CPC分类号： C07D233/84 ,  C07C221/00 ,  C07C225/06 ,  C07C269/00 ,  C07C271/12

摘要： Provided herein are Nα,Nα,Nα-trialkyl histidine derivative compounds and methods of their preparation. Also provided are methods of their use for preparing useful compounds such as ergothioneine.

公开(公告)号：US20170247321A1

公开(公告)日：2017-08-31

申请号：US15597478

申请日：2017-05-17

申请人： Roche Palo Alto LLC

发明人： Robert Greenhouse ,  Ralph New Harris, III ,  Saul Jaime-Figueroa ,  James M. Kress ,  David Bruce Repke ,  Russell Stephen Stabler

IPC分类号： C07C317/32 ,  C07D207/325 ,  C07D207/34 ,  C07D207/36 ,  C07D209/30 ,  C07D231/18 ,  C07D233/20 ,  C07D233/34 ,  C07D233/48 ,  C07D233/54 ,  C07D233/64 ,  C07D233/84 ,  C07D233/88 ,  C07D233/90 ,  C07D235/06 ,  C07D239/14 ,  C07D239/42 ,  C07D277/82 ,  C07D233/44 ,  C07D233/58 ,  C07C317/44 ,  C07D207/16

CPC分类号： C07C317/32 ,  C07C317/44 ,  C07C2602/08 ,  C07C2602/10 ,  C07D207/16 ,  C07D207/325 ,  C07D207/34 ,  C07D207/36 ,  C07D209/30 ,  C07D231/18 ,  C07D233/20 ,  C07D233/34 ,  C07D233/44 ,  C07D233/48 ,  C07D233/54 ,  C07D233/58 ,  C07D233/64 ,  C07D233/84 ,  C07D233/88 ,  C07D233/90 ,  C07D235/06 ,  C07D239/14 ,  C07D239/42 ,  C07D277/82

摘要： The application discloses pharmaceutical compounds of formula I useful for treating CNS diseases wherein m, s, R1 R5, R6 and R7 are as defined herein.

公开(公告)号：US09725436B2

公开(公告)日：2017-08-08

申请号：US15021532

申请日：2014-09-15

申请人： CORTENDO AB (PUBL)

发明人： Benjamin Eric Blass ,  Magid A Abou-Gharbia ,  Wayne E. Childers ,  Pravin Iyer ,  Joshodeep Boruwa

IPC分类号： C07D401/10 ,  C07D213/26 ,  A61K31/4418 ,  C07D401/12 ,  C07D213/71 ,  C07D233/60 ,  C07D233/61 ,  C07D233/84 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D213/30 ,  C07D213/38 ,  C07D213/65 ,  C07D213/56

CPC分类号： C07D401/12 ,  A61K31/4418 ,  C07D213/26 ,  C07D213/30 ,  C07D213/38 ,  C07D213/56 ,  C07D213/65 ,  C07D213/71 ,  C07D233/60 ,  C07D233/61 ,  C07D233/84 ,  C07D401/10 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

摘要： Embodiments of the present invention relate to novel cytochrome P450 inhibitors and pharmaceutical compositions thereof having a disease-modifying action in the treatment of diseases associated with the production of cortisol that include metabolic syndrome, obesity, headache, depression, hypertension, diabetes mellitus, Cushing's Syndrome, pseudo-Cushing syndrome, cognitive impairment, dementia, heart failure, renal failure, psoriasis, glaucoma, cardiovascular disease, cancer, stroke or incidentalomas.

公开(公告)号：US20170210737A1

公开(公告)日：2017-07-27

申请号：US15326821

申请日：2015-05-06

申请人： Ohio University

发明人： Douglas Goetz ,  Stephen C. Bergmeier ,  Mark C. McMills ,  Crina M. Orac

IPC分类号： C07D417/14 ,  C07D413/04 ,  C07D405/04 ,  C07D417/04 ,  C07D417/06 ,  C07D277/36 ,  C07D277/84 ,  C07D233/84 ,  C07D277/16

CPC分类号： C07D417/14 ,  A61K31/155 ,  A61K31/4166 ,  A61K31/427 ,  A61K31/428 ,  A61K31/4439 ,  A61K45/06 ,  C07D233/84 ,  C07D277/16 ,  C07D277/36 ,  C07D277/84 ,  C07D405/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/06 ,  Y02A50/411

摘要： Compounds having General Formula (I) or General Formula (II): in which R1 is chosen from C1 to C10 aliphatic or heteroaliphatic groups, optionally substituted with one or more aryl groups, substituted aryl groups, heteroaryl groups, substituted heteroaryl groups, or combination thereof; R2 is chosen from aromatic moieties, substituted aromatic moieties, heteroaromatic moieties substituted heteroaromatic moieties, and coumarin; R3 is chosen from —H, C1 to C10 aliphatic or heteroaliphatic groups, phenyl, or substituted phenyl, wherein the aliphatic or heteroaliphatic groups are optionally substituted with one or more phenyl groups, aryl groups, heteroaryl groups, substituted heteroaryl groups, or combination thereof, and wherein the aliphatic or heteroaliphatic groups are optionally bonded to R2 to form a ring; X is S or O; and Y is S or NH, may be used in pharmaceutical compositions that modify of biological signaling processes or as reagents for biological assays.

公开(公告)号：US09708272B2

公开(公告)日：2017-07-18

申请号：US14839209

申请日：2015-08-28

申请人： TES Pharma S.r.l.

发明人： Roberto Pellicciari ,  Johan Auwerx ,  Nadia Raffaelli

IPC分类号： C07D239/38 ,  C07D403/12 ,  C07D233/68 ,  C07D233/84 ,  C07D233/96 ,  C07D407/12 ,  C07D409/12 ,  A61K31/505 ,  A61K31/513 ,  C07D239/56 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04

CPC分类号： C07D239/38 ,  A61K31/505 ,  A61K31/513 ,  C07D233/68 ,  C07D233/84 ,  C07D233/96 ,  C07D239/56 ,  C07D401/04 ,  C07D403/12 ,  C07D405/04 ,  C07D407/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04

摘要： The present disclosure discloses compounds capable of modulating the activity of α-amino-β-carboxymuconic acid semialdehyde decarboxylase (ACMSD), which are useful for the prevention and/or the treatment of diseases and disorders associated with defects in NAD+ biosynthesis, e.g., metabolic disorders, neurodegenerative diseases, chronic inflammatory diseases, kidney diseases, and diseases associated with ageing. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament.

公开(公告)号：US09656953B2

公开(公告)日：2017-05-23

申请号：US14171273

申请日：2014-02-03

申请人： University of South Florida

发明人： Said M. Sebti ,  Srikumar Chellappan ,  Nicholas James Lawrence

IPC分类号： C07C279/06 ,  C07C335/32 ,  C07C323/45 ,  C07D233/30 ,  C07D233/84 ,  C07D235/08 ,  C07D249/14 ,  C07D249/12 ,  C07D277/42 ,  C07D277/40 ,  C07D317/56 ,  C07D215/12 ,  C07D213/53 ,  C07D235/28 ,  C07D317/58

CPC分类号： C07C323/45 ,  C07C279/06 ,  C07C335/32 ,  C07D213/53 ,  C07D215/12 ,  C07D233/30 ,  C07D233/84 ,  C07D235/28 ,  C07D249/12 ,  C07D249/14 ,  C07D277/40 ,  C07D277/42 ,  C07D317/56 ,  C07D317/58

摘要： The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non-small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.

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：US20160264530A1

公开(公告)日：2016-09-15

申请号：US15067687

申请日：2016-03-11

申请人： Jan Trampota ,  Mironova Innovations LLC

发明人： Bohumil Zák ,  Marie Záková ,  Jan Trampota ,  John Olszewski ,  Theodore Gribb, III

IPC分类号： C07D233/84 ,  C07C229/26 ,  C07C269/00

CPC分类号： C07D233/84 ,  C07C221/00 ,  C07C225/06 ,  C07C269/00 ,  C07C271/12

摘要： Provided herein are Nα,Nα,Nα-trialkyl histidine derivative compounds and methods of their preparation. Also provided are methods of their use for preparing useful compounds such as ergothioneine.

摘要翻译： 本文提供了Nα，Nα，Nα-三烷基组氨酸衍生物化合物及其制备方法。 还提供了它们用于制备有用化合物如麦角硫杆菌素的方法。

公开(公告)号：US20160256439A1

公开(公告)日：2016-09-08

申请号：US15032508

申请日：2014-10-31

申请人： OHIO UNIVERSITY

发明人： Kelly D. McCall ,  Frank L. Schwartz ,  Douglas J. Goetz ,  Ramiro Malgor

IPC分类号： A61K31/4184 ,  A61K45/06 ,  A61K31/4164

CPC分类号： A61K31/4184 ,  A61K31/4164 ,  A61K45/06 ,  C07D233/84

摘要： Methods for preventing, treating, and/or reducing the risk of developing non-alcoholic fatty liver disease in a subject in need thereof and pharmaceutical compositions for the prevention or treatment of non-alcoholic fatty liver disease. The methods include administering a therapeutically effective amount of phenylmethimazole, methimazole derivatives, and/or tautomeric cyclic thiones to the subject. The pharmaceutical composition includes phenylmethimazole, methimazole derivatives, and/or tautomeric cyclic thiones formulated for administration to a subject for the prevention or treatment of non-alcoholic fatty liver disease.

摘要翻译： 用于预防，治疗和/或降低在有需要的受试者中发展非酒精性脂肪肝疾病的风险的方法和用于预防或治疗非酒精性脂肪性肝病的药物组合物。 所述方法包括向受试者施用治疗有效量的苯基甲基咪唑，甲巯咪唑衍生物和/或互变异构环状硫堇。 药物组合物包括配制用于给予受试者预防或治疗非酒精性脂肪性肝病的苯甲基咪唑，甲巯咪唑衍生物和/或互变异构环状硫堇。

公开(公告)号：US20160221990A1

公开(公告)日：2016-08-04

申请号：US15021532

申请日：2014-09-15

申请人： CORTENDO AB (PUBL)

发明人： Benjamin Eric Blass ,  Magid A Abou-Gharbia ,  Wayne E. Childers ,  Pravin Iyer ,  Joshodeep Boruwa

IPC分类号： C07D401/12 ,  C07D233/61 ,  C07D213/26 ,  C07D233/84 ,  C07D213/56 ,  C07D233/60 ,  C07D401/10

CPC分类号： C07D401/12 ,  A61K31/4418 ,  C07D213/26 ,  C07D213/30 ,  C07D213/38 ,  C07D213/56 ,  C07D213/65 ,  C07D213/71 ,  C07D233/60 ,  C07D233/61 ,  C07D233/84 ,  C07D401/10 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

摘要： Embodiments of the present invention relate to novel cytochrome P450 inhibitors and pharmaceutical compositions thereof having a disease-modifying action in the treatment of diseases associated with the production of cortisol that include metabolic syndrome, obesity, headache, depression, hypertension, diabetes mellitus, Cushing's Syndrome, pseudo-Cushing syndrome, cognitive impairment, dementia, heart failure, renal failure, psoriasis, glaucoma, cardiovascular disease, cancer, stroke or incidentalomas.

摘要翻译： 本发明的实施方案涉及新型细胞色素P450抑制剂及其药物组合物，其在治疗与皮质醇生成相关的疾病中具有疾病修饰作用，其包括代谢综合征，肥胖症，头痛，抑郁症，高血压，糖尿病，库兴综合征 ，假库兴综合征，认知障碍，痴呆，心力衰竭，肾衰竭，牛皮癣，青光眼，心血管疾病，癌症，中风或间质瘤。