公开(公告)号：US20160318848A1

公开(公告)日：2016-11-03

申请号：US14702744

申请日：2015-05-03

Applicant: Mark Quang Nguyen

Inventor： Mark Quang Nguyen

IPC: C07C233/05 ,  C07C233/18 ,  A61K31/5375 ,  A61K45/06 ,  A61K31/225 ,  C07D295/185

CPC classification number: C07C233/05 ,  A61K31/225 ,  A61K31/357 ,  A61K31/40 ,  A61K31/41 ,  A61K31/4164 ,  A61K31/4166 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/4453 ,  A61K31/45 ,  A61K31/495 ,  A61K31/513 ,  A61K31/5375 ,  A61K45/06 ,  C07C69/675 ,  C07C233/18 ,  C07C235/06 ,  C07C235/08 ,  C07C235/12 ,  C07C235/14 ,  C07C235/16 ,  C07C2601/14 ,  C07D295/185 ,  A61K2300/00

Abstract: Fumarate compounds, pharmaceutical compositions comprising the fumarate compounds, and methods of using fumarate compounds and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed.

公开(公告)号：US20160289171A1

公开(公告)日：2016-10-06

申请号：US15088211

申请日：2016-04-01

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： James Aaron Balog ,  Emily Charlotte Cherney ,  Weiwei Guo ,  Audris Huang ,  Jay A. Markwalder ,  Steven P. Seitz ,  Weifang Shan ,  David K. Williams ,  Natesan Murugesan ,  Susheel Jethanand Nara ,  Saumya Roy ,  Soodamani Thangavel ,  Ramesh Kumar Sistla ,  Srinivas Cheruku ,  Srinivasan Thangathirupathy ,  Yadagiri Kanyaboina ,  Nagalakshmi Pulicharla

IPC: C07C229/42 ,  A61K31/196 ,  C07D239/47 ,  A61K31/505 ,  C07C255/58 ,  A61K31/277 ,  C07C275/40 ,  A61K31/17 ,  C07D295/155 ,  A61K31/5375 ,  C07D277/64 ,  A61K31/428 ,  C07D335/02 ,  A61K31/382 ,  C07D409/12 ,  A61K31/506 ,  C07D309/04 ,  A61K31/351 ,  C07D405/12 ,  C07D211/14 ,  A61K31/445 ,  C07D401/12 ,  C07D413/12 ,  A61K31/5377 ,  C07D405/14 ,  C07D417/12 ,  C07D487/04 ,  A61K31/519 ,  A61K31/501 ,  C07D471/04 ,  A61K31/437 ,  C07D205/04 ,  A61K31/397 ,  A61K31/538 ,  C07D265/36 ,  A61K39/395

CPC classification number: C07C275/40 ,  A61K31/17 ,  A61K31/196 ,  A61K31/277 ,  A61K31/351 ,  A61K31/382 ,  A61K31/397 ,  A61K31/428 ,  A61K31/437 ,  A61K31/445 ,  A61K31/501 ,  A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/538 ,  A61K39/3955 ,  A61K39/39558 ,  A61K45/06 ,  C07C229/42 ,  C07C233/81 ,  C07C235/38 ,  C07C235/56 ,  C07C255/57 ,  C07C255/58 ,  C07C275/30 ,  C07C275/42 ,  C07D205/04 ,  C07D207/08 ,  C07D207/12 ,  C07D211/08 ,  C07D211/14 ,  C07D239/34 ,  C07D239/47 ,  C07D265/30 ,  C07D265/36 ,  C07D277/64 ,  C07D295/155 ,  C07D307/22 ,  C07D309/04 ,  C07D309/14 ,  C07D317/46 ,  C07D335/02 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/08

Abstract: There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.

Abstract translation: 公开了调节或抑制吲哚胺2,3-双加氧酶（IDO）的酶活性的化合物，含有所述化合物的药物组合物和治疗增殖性疾病如癌症，病毒感染和/或炎症性疾病的方法，其利用 发明。

公开(公告)号：US20160279136A1

公开(公告)日：2016-09-29

申请号：US15172955

申请日：2016-06-03

Applicant: Supernus Pharmaceuticals, Inc.

Inventor： Michael L. VIEIRA ,  Austin B. HUANG ,  Padmanabh P. BHATT

IPC: A61K31/5375 ,  A61K9/14 ,  A61K9/48 ,  A61K9/20

CPC classification number: A61K31/5375 ,  A61K9/00 ,  A61K9/146 ,  A61K9/2054 ,  A61K9/485 ,  A61K9/4866 ,  A61K9/50

Abstract: Modified release formulations of viloxazine and methods of administering the same are disclosed. High-drug load formulations of viloxazine are further disclosed.

公开(公告)号：US09446047B2

公开(公告)日：2016-09-20

申请号：US15087807

申请日：2016-03-31

Applicant: Arrien Pharmaceuticals LLC

Inventor： Hariprasad Vankayalapati ,  Venkatakrishnareddy Yerramreddy

IPC: A61K31/5377 ,  A61K31/5375 ,  A61K31/496 ,  A61K31/495 ,  A61K31/451 ,  A61K31/4545

CPC classification number: A61K31/5375 ,  A61K31/122 ,  A61K31/255 ,  A61K31/44 ,  A61K31/445 ,  A61K31/451 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5377 ,  C07C323/22 ,  C07C2602/08 ,  C07D211/14 ,  C07D211/38 ,  C07D211/58 ,  C07D213/50 ,  C07D231/12 ,  C07D241/04 ,  C07D277/42 ,  C07D295/116 ,  C07D295/135 ,  C07D401/10 ,  C07D413/10 ,  C07D413/12

Abstract: The present invention is directed to compounds, their synthesis, and their use as antagonists, inverse agonists, modulators and or inhibitors of the Retinoic acid-related orphan nuclear receptor γt (RORγt)/RORγ. The compounds of the present invention are useful for modulating RORγt)/RORγ activity and for treating diseases or conditions mediated by RORγt)/RORγ such as for example, disease states associated with immunopathology of human autoimmune diseases such as Multiple Sclerosis (MS), Rheumatoid Arthritis (RA), Inflammatory Colitis, Psoriasis, COPD, Pain, Obesity, Diabetes, Dyslipidemia, Osteoporosis, Asthma, Neurodegenerative diseases and Cancer.

公开(公告)号：US09409896B2

公开(公告)日：2016-08-09

申请号：US13882698

申请日：2011-11-01

Applicant: Eric S. Burak ,  Danping Li ,  David S. Dresback

Inventor： Eric S. Burak ,  Danping Li ,  David S. Dresback

IPC: A61K9/20 ,  C07D413/12 ,  A61K9/48 ,  A61K31/4192 ,  A61K31/421 ,  A61K31/5375 ,  A61K47/14 ,  A61K47/22 ,  C07D263/22 ,  C07D413/14

CPC classification number: C07D413/12 ,  A61K9/2018 ,  A61K9/205 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/4192 ,  A61K31/421 ,  A61K31/5375 ,  A61K47/14 ,  A61K47/22 ,  C07D263/22 ,  C07D413/14

Abstract: The present invention relates to carrier systems useful for pharmaceutical compositions. These carriers comprise an emulsifier, and also in further embodiments a polymeric dissolution aid. These carriers are useful for delivering pharmaceutical actives such as antimicrobial agents.

Abstract translation: 本发明涉及可用于药物组合物的载体系统。 这些载体包含乳化剂，并且在其它实施方案中也包括聚合物溶解助剂。 这些载体可用于递送药物活性物质如抗微生物剂。

公开(公告)号：US09409895B2

公开(公告)日：2016-08-09

申请号：US13833460

申请日：2013-03-15

Applicant: Darren Mark Legrand ,  Vikki Furminger ,  Christopher Thomson ,  Owen Rhys Hughes ,  Emily Stanley

Inventor： Darren Mark Legrand ,  Vikki Furminger ,  Christopher Thomson ,  Owen Rhys Hughes ,  Emily Stanley

IPC: C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  A61K31/4192 ,  A61K31/454 ,  A61K31/55 ,  C07D211/34 ,  C07D295/185 ,  A61K31/337 ,  A61K31/4174 ,  A61K31/4245 ,  A61K31/426

CPC classification number: A61K31/5377 ,  A61K31/337 ,  A61K31/4174 ,  A61K31/4192 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/439 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5375 ,  A61K31/55 ,  C07D211/34 ,  C07D249/08 ,  C07D295/185 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  A61K2300/00

Abstract: The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in diseases and disorders mediated by autotaxin.

Abstract translation: 本发明涉及自体吸收素抑制剂的新型化合物，其制备方法，药物组合物和含有它们的药物及其在自体吸收素介导的疾病和病症中的用途。

公开(公告)号：US09402819B2

公开(公告)日：2016-08-02

申请号：US14647159

申请日：2013-12-13

Applicant: Sichuan University

Inventor： Rui Li ,  Yuquan Wei

IPC: A61K31/10 ,  A61K31/167 ,  A61K31/18 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/683 ,  A61K31/255 ,  C07C323/62 ,  C07C317/48 ,  C07C317/50 ,  C07C323/63 ,  C07C237/44 ,  C07F9/40

CPC classification number: A61K31/167 ,  A61K31/18 ,  A61K31/255 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/683 ,  C07C237/44 ,  C07C317/48 ,  C07C317/50 ,  C07C323/62 ,  C07C323/63 ,  C07F9/4056

Abstract: The present invention relates to the technical field of chemically synthesized drugs, in particular to an anti-HIV drug or prodrug and preparation method and uses thereof. The compound or prodrug compound of the present invention has a structural formula as represented by formula I. The compounds have anti-HIV-1 and anti-HIV-2 virus activity, and have a C8166 therapeutic index as high as 2081.59 and an H9 therapeutic index as high as 303.03. Furthermore, the compounds have high solubility up to 1290-2845.5 μg/ml in an aqueous solution, and can be formulated into an oral formulation.

Abstract translation: 本发明涉及化学合成药物的技术领域，特别涉及抗HIV药物或前药及其制备方法和用途。 本发明的化合物或前药化合物具有由式I表示的结构式。该化合物具有抗HIV-1和抗HIV-2病毒活性，并具有高达2081.59的C8166治疗指数和H9治疗 指数高达303.03。 此外，化合物在水溶液中具有高达1290-2845.5μg/ ml的高溶解度，并且可以配制成口服制剂。

公开(公告)号：US20160193215A1

公开(公告)日：2016-07-07

申请号：US15067057

申请日：2016-03-10

Applicant: DONGGUK UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION ,  KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY

Inventor： Kyeong LEE ,  Mi-Sun WON ,  Hwan-Mook KIM ,  Song-Kyu PARK ,  Ki-Ho LEE ,  Chang-Woo LEE ,  Bo-Kyung KIM ,  Hyun-Seung BAN ,  Kyung-Sook CHUNG ,  Naik RAVI

IPC: A61K31/5375 ,  A61K31/4985 ,  A61K31/495

CPC classification number: A61K31/5375 ,  A61K31/495 ,  A61K31/4985 ,  C07C231/02 ,  C07C235/20 ,  C07C235/22 ,  C07D241/04 ,  C07D279/12 ,  C07D295/073 ,  C07D295/104 ,  C07D295/108 ,  C07D295/182 ,  C07D295/185 ,  C07D307/46 ,  C07D487/04

Abstract: The present invention relates to novel compounds as HIF-1α inhibitors, manufacturing process thereof, and a pharmaceutical compositions. The compounds according to the present invention having inhibition activity against HIF-1α, can be used as a therapeutic prevention and/or treatment for various solid cancers such as colon cancer, liver cancer, stomach cancer and breast cancer. Also, the compounds according to the present invention are useful in the treatment of diabetic retinopathy and rheumatoid arthritis, which are aggravated by HIF-1α-mediated VEGFA expression.

Abstract translation: 本发明涉及作为HIF-1α抑制剂的新化合物，其制备方法和药物组合物。 具有抑制HIF-1α活性的本发明化合物可用作结肠癌，肝癌，胃癌和乳腺癌等各种固体癌症的治疗性预防和/或治疗。 此外，本发明的化合物可用于治疗由HIF-1α介导的VEGFA表达加重的糖尿病性视网膜病变和类风湿性关节炎。

公开(公告)号：US09375421B2

公开(公告)日：2016-06-28

申请号：US14970134

申请日：2015-12-15

Applicant: Gilrose Pharmaceuticals, LLC

Inventor： Bruce Roseman ,  Gilla Kaplan

IPC: A61K31/435 ,  A61K31/4458

CPC classification number: A61K31/4458 ,  A61K31/135 ,  A61K31/137 ,  A61K31/138 ,  A61K31/165 ,  A61K31/421 ,  A61K31/522 ,  A61K31/5375

Abstract: A pharmaceutical intervention and therapeutic method for treating an apraxia of speech in children. The child can also be diagnosed with gait abnormalities or impairment autism, mental retardation and dyslexia. If the child demonstrates at least an 18 to 24 month development stage of either verbal development or non-verbal development, a therapeutic dose of a dopamine agonistic, particularly a nonlinear lower alkyl phenidate or dextro-threo-methylphenidate is administered to the child.

Abstract translation: 用于治疗儿童言语障碍的药物干预和治疗方法。 孩子也可以被诊断为步态异常或减退自闭症，精神发育迟滞和诵读困难。 如果孩子表现出至少18到24个月的语言发展或非语言发展的发展阶段，则向儿童施用治疗剂量的多巴胺激动剂，特别是非线性低级烷基苯酞酸酯或右旋 - 苏氨哌甲酯。

公开(公告)号：US20160175275A1

公开(公告)日：2016-06-23

申请号：US15056202

申请日：2016-02-29

Applicant: ADT PHARMACEUTICALS, INC.

Inventor： Gary A. Piazza ,  Xi Chen ,  Adam B. Keeton ,  Michael R. Boyd

IPC: A61K31/341 ,  A61K31/4406 ,  G01N33/574 ,  A61K31/165 ,  A61K31/167 ,  A61K45/06 ,  A61K31/40

CPC classification number: C07D317/64 ,  A61K31/165 ,  A61K31/167 ,  A61K31/216 ,  A61K31/341 ,  A61K31/36 ,  A61K31/40 ,  A61K31/401 ,  A61K31/421 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/445 ,  A61K31/496 ,  A61K31/5375 ,  A61K31/5377 ,  A61K45/06 ,  A61K2300/00 ,  C07C233/58 ,  C07C235/32 ,  C07C235/34 ,  C07C237/20 ,  C07C311/29 ,  C07C2601/02 ,  C07C2602/08 ,  C07D207/14 ,  C07D207/335 ,  C07D207/337 ,  C07D211/56 ,  C07D213/24 ,  C07D213/40 ,  C07D213/75 ,  C07D235/30 ,  C07D307/38 ,  C07D307/52 ,  C07D307/54 ,  C07D405/12 ,  G01N33/5748 ,  A61K2800/00

Abstract: Disclosed are compounds, for example, a compound of formula I, wherein R, R0, R1-R8, n, X, Y, Y′, and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition for example, cancer, mediated by the ras gene.

Abstract translation: 公开了化合物，例如式I化合物，其中R，R 0，R 1 -R 8，n，X，Y，Y'和E如本文所述，含有这些化合物的药物组合物，以及治疗或预防的方法 由ras基因介导的疾病或病症，例如癌症。