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1. 发明授权

US10053433B2 Androgen receptor antagonists 有权
公开(公告)号：US10053433B2
公开(公告)日：2018-08-21
申请号：US15382942
申请日：2016-12-19
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
发明人： Pamela M. England , Robert J. Fletterick , Kristopher Kuchenbecker , Felipe de Jesus Cortez
IPC分类号： C07D213/74 , C07D239/42 , C07D241/26 , A61K31/44 , A61K31/495 , C07D257/08 , C07K14/72 , C07D213/84 , C07D237/24 , C07D253/07
CPC分类号： C07D257/08 , C07D213/74 , C07D213/84 , C07D213/85 , C07D237/24 , C07D239/28 , C07D239/42 , C07D241/26 , C07D253/07 , C07K14/721
摘要： Disclosed herein are compositions and methods for modulating the androgen receptor.

2. 发明授权

US09862691B2 Cyclic triazo and diazo sodium channel blockers 有权
公开(公告)号：US09862691B2
公开(公告)日：2018-01-09
申请号：US15201885
申请日：2016-07-05
申请人： University of Greenwich
发明人： Michael Leach , Laurence Harbige , Dieter Riddall , Karl Franzmann
IPC分类号： A61K31/53 , C07D253/075 , C07D405/04 , C07D253/06 , C07D253/08 , C07D253/07 , C07D253/10 , C07D401/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12
CPC分类号： C07D253/075 , C07D253/06 , C07D253/07 , C07D253/10 , C07D401/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12
摘要： A method of treating a disorder. The method includes administering to a subject in need thereof a compound of general formula (I): Each of A, N*, X, Y, R1, and R2 is defined herein. Also disclosed are compounds of the formula and a pharmaceutical composition containing such a compound.

4. 发明授权

US09708309B2 Arylcyclopropylamine based demethylase inhibitors of LSD1 and their medical use 有权
公开(公告)号：US09708309B2
公开(公告)日：2017-07-18
申请号：US14848649
申请日：2015-09-09
申请人： Oryzon Genomics S.A.
发明人： Alberto Ortega Muñoz , Matthew Colin Thor Fyfe , Marc Martinell Pedemonte , Iñigo Tirapu Fernandez De La Cuesta , Maria de los Ángeles Estiarte-Martinez
IPC分类号： C07D239/02 , C07D413/00 , C07D417/00 , A61K31/505 , A61K31/44 , C07D417/12 , A61K31/433 , A61K31/4245 , A61K31/422 , C07D213/73 , C07D237/20 , C07D239/42 , C07D241/20 , C07D253/07 , C07D261/14 , C07D263/48 , C07D271/07 , C07D271/113 , C07D277/40 , C07D285/12 , C07D401/12 , C07D413/12 , C07D285/135 , C07D285/08
CPC分类号： C07D417/12 , A61K31/422 , A61K31/4245 , A61K31/433 , C07D213/73 , C07D237/20 , C07D239/42 , C07D241/20 , C07D253/07 , C07D261/14 , C07D263/48 , C07D271/07 , C07D271/113 , C07D277/40 , C07D285/08 , C07D285/12 , C07D285/135 , C07D401/12 , C07D413/12
摘要： The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).

5. 发明申请

US20170101384A1 ANDROGEN RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：US20170101384A1
公开(公告)日：2017-04-13
申请号：US15382942
申请日：2016-12-19
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
发明人： Pamela M. ENGLAND , Robert J. Fletterick , Kristopher Kuchenbecker , Felipe de Jesus Cortez
IPC分类号： C07D257/08 , C07D213/84 , C07D253/07 , C07D213/74 , C07D241/26 , C07D237/24 , C07K14/72 , C07D239/42
CPC分类号： C07D257/08 , C07D213/74 , C07D213/84 , C07D213/85 , C07D237/24 , C07D239/28 , C07D239/42 , C07D241/26 , C07D253/07 , C07K14/721
摘要： Disclosed herein are compositions and methods for modulating the androgen receptor.

6. 发明申请

US20160302418A1 Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto 有权
标题翻译：具有杀虫效用的分子，以及与之相关的中间体，组合物和方法
公开(公告)号：US20160302418A1
公开(公告)日：2016-10-20
申请号：US15092646
申请日：2016-04-07
申请人： Dow AgroSciences LLC
发明人： Timothy P. Martin , Joseph D. Eckelbarger , Ronald Ross, JR. , Kyle DeKorver , Ronald J. Heemstra , Daniel I. Knueppel , Peter Vednor , Ricky Hunter , David A. Demeter , Tony K. Trullinger , Erich Baum , Zoltan Benko , Nakyen Choy , Gary Crouse , John F. Daeuble, SR. , Fangzheng Li , Jeff Nissen , Michelle Riener , Tom Sparks , Frank Wessels , Maurice Yap
IPC分类号： A01N53/00 , C07C237/22 , C07D213/56 , C07C259/10 , C07C255/29 , C07C317/28 , C07C323/42 , C07D207/10 , C07D307/52 , C07D249/08 , C07D277/30 , C07D231/12 , C07C311/46 , C07D333/60 , C07D233/36 , C07C237/42
CPC分类号： A01N53/00 , A01N37/22 , A01N37/34 , A01N41/10 , A01N43/40 , A01N43/60 , A01N43/653 , A01N43/707 , A01N43/82 , A01N43/90 , C07C233/63 , C07C233/65 , C07C237/22 , C07C237/42 , C07C255/29 , C07C255/46 , C07C255/57 , C07C255/60 , C07C259/10 , C07C271/28 , C07C271/66 , C07C311/08 , C07C311/46 , C07C317/14 , C07C317/28 , C07C317/40 , C07C317/50 , C07C323/41 , C07C323/42 , C07C323/59 , C07C331/12 , C07C381/10 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D205/04 , C07D207/10 , C07D207/273 , C07D207/452 , C07D209/49 , C07D213/56 , C07D213/75 , C07D213/81 , C07D213/84 , C07D213/89 , C07D215/227 , C07D215/38 , C07D231/12 , C07D231/56 , C07D233/36 , C07D233/80 , C07D235/30 , C07D241/20 , C07D249/08 , C07D253/07 , C07D261/12 , C07D263/26 , C07D277/30 , C07D277/36 , C07D285/06 , C07D295/32 , C07D305/08 , C07D307/33 , C07D307/52 , C07D309/14 , C07D331/04 , C07D333/36 , C07D333/48 , C07D333/60 , C07D487/04
摘要： This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).
摘要翻译：本公开涉及具有杀虫效果的分子领域，其中包括节肢动物，软体动物和线虫中的害虫，产生这种分子的方法，用于此类方法的中间体，含有这种分子的杀虫组合物，以及使用这种杀虫剂组合物抗这种害虫的方法。这些杀虫剂组合物可以用作例如杀螨剂，杀虫剂，杀螨剂，杀软体动物剂和杀线虫剂。该文献公开了具有下式（“一级方程式”）的分子。

7. 发明申请

US20150376177A1 ARYLCYCLOPROPYLAMINE BASED DEMETHYLASE INHIBITORS OF LSD1 AND THEIR MEDICAL USE 有权
标题翻译：基于ARYLCYCLOPROPYLAMINE的LSD1的DEMETHYLASE抑制剂及其医疗用途
公开(公告)号：US20150376177A1
公开(公告)日：2015-12-31
申请号：US14848649
申请日：2015-09-09
申请人： Oryzon Genomics S.A.
发明人： Alberto ORTEGA MUÑOZ , Matthew Colin Thor FYFE , Marc MARTINELL PEDEMONTE , Iñigo TIRAPU FERNANDEZ DE LA CUESTA , Maria de los Ángeles ESTIARTE-MARTINEZ
IPC分类号： C07D417/12 , C07D277/40 , C07D401/12 , C07D271/07 , C07D271/113 , C07D413/12 , C07D285/135 , C07D263/48 , C07D261/14 , C07D285/08 , C07D213/73 , C07D237/20 , C07D241/20 , C07D253/07 , C07D239/42
CPC分类号： C07D417/12 , A61K31/422 , A61K31/4245 , A61K31/433 , C07D213/73 , C07D237/20 , C07D239/42 , C07D241/20 , C07D253/07 , C07D261/14 , C07D263/48 , C07D271/07 , C07D271/113 , C07D277/40 , C07D285/08 , C07D285/12 , C07D285/135 , C07D401/12 , C07D413/12
摘要： The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).
摘要翻译：本发明涉及（异）芳基环丙胺化合物，特别包括本文所述和定义的式（I）化合物及其在治疗中的用途，包括例如治疗或预防癌症，神经疾病或病症，或病毒感染。因此，在一个具体方面，本发明涉及式（II），（III），（IV），（V），（VI），（VII），（VIII），（IX）。

8. 发明授权

US09139560B2 Substituted pyrazines as tubulin inhibitors 有权
标题翻译：取代的吡嗪作为微管蛋白抑制剂
公开(公告)号：US09139560B2
公开(公告)日：2015-09-22
申请号：US14194543
申请日：2014-02-28
申请人： YM Biosciences Australia Pty Ltd
发明人： Christopher John Burns , Andrew Frederick Wilks , Michael Francis Harte , Harrison Sikanyika , Emmanuelle Fantino
IPC分类号： A61K31/4965 , C07D241/20 , C07D401/12 , C07D213/74 , C07D239/42 , C07D253/07 , C07D401/14 , C07D403/12
CPC分类号： C07D253/07 , C07D213/74 , C07D239/42 , C07D241/20 , C07D401/12 , C07D401/14 , C07D403/12
摘要： Compounds of general formula (I), (II), (III) and (V) are described for use in modulating microtubule polymerization and in the treatment of associated disease states. Use of compounds (I), (III) and (V) in the treatment of kinase-associated disease states is also described. Further described are novel compounds of formula (II), (III) and (V).
摘要翻译：描述了通式（I），（II），（III）和（V）的化合物用于调节微管聚合和治疗相关疾病状态。还描述了化合物（I），（III）和（V）在激酶相关疾病状态的治疗中的用途。进一步描述的是式（II），（III）和（V）的新化合物。

9. 发明申请

US20150191454A1 MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
标题翻译：用于治疗相关疾病的前列腺素（PGI2）受体的调节剂
公开(公告)号：US20150191454A1
公开(公告)日：2015-07-09
申请号：US14566019
申请日：2014-12-10
申请人： Thuy-Anh Tran , Rena Hayashi , Jason B. Ibarra , Brett Ullman , Ning Zou
发明人： Thuy-Anh Tran , Rena Hayashi , Jason B. Ibarra , Brett Ullman , Ning Zou
IPC分类号： C07D409/04 , C07D403/04 , C07D253/07 , C07D237/14 , C07D401/04
CPC分类号： C07D237/14 , C07D253/07 , C07D401/04 , C07D403/04 , C07D409/04
摘要： Cyclohexane derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH) and related disorders; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD).
摘要翻译：式Ia的环己烷衍生物及其药物组合物，其调节PGI 2受体的活性。本发明的化合物及其药物组合物涉及可用于治疗肺动脉高压（PAH）和相关疾病的方法; 血小板聚集; 冠状动脉疾病; 心肌梗死; 短暂性脑缺血发作; 心绞痛行程; 缺血再灌注损伤; 再狭窄; 房颤; 在血管成形术或冠状动脉旁路手术个体或患有心房颤动的个体中血凝块形成; 动脉粥样硬化动脉粥样硬化血栓形成哮喘或其症状; 糖尿病性相关疾病如糖尿病性周围神经病变，糖尿病性肾病或糖尿病性视网膜病变; 青光眼或其他眼睛异常眼内疾病; 高血压; 炎; 银屑病; 牛皮癣关节炎类风湿关节炎; 克罗恩病; 移植排斥反应多发性硬化症系统性红斑狼疮（SLE）; 溃疡性结肠炎缺血再灌注损伤; 再狭窄; 动脉粥样硬化粉刺; 1型糖尿病; 2型糖尿病; 败血症和慢性阻塞性肺疾病（COPD）。

10. 发明申请

US20140100323A1 RUBBER COMPOSITION INCLUDING A 1,2,4-TRIAZINE DERIVATIVE 有权
标题翻译：橡胶组合物，包括1,2,4-三唑衍生物
公开(公告)号：US20140100323A1
公开(公告)日：2014-04-10
申请号：US14111600
申请日：2012-04-16
申请人： Anne Veyland , Nicolas Seeboth
发明人： Anne Veyland , Nicolas Seeboth
IPC分类号： C08K5/378 , C08K5/5373 , C08L9/06
CPC分类号： C08L9/06 , C07D253/07 , C07D487/04 , C07F9/6521 , C08K5/0025 , C08K5/34928 , C08K5/378 , C08K5/5373 , C08L21/00
摘要： A rubber composition for manufacturing tyres is based on one or more diene elastomers, one or more reinforcing fillers, and a vulcanization system. The vulcanization system includes one or more 1,2,4-triazine compounds chosen from compounds of formula I and compounds of formula II: Certain specific 1,2,4-triazine derivatives are described.
摘要翻译：用于制造轮胎的橡胶组合物基于一种或多种二烯弹性体，一种或多种增强填料和硫化体系。硫化体系包括一种或多种选自式I化合物和式II化合物的1,2,4-三嗪化合物：描述了某些具体的1,2,4-三嗪衍生物。

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