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1. 发明授权

EP2598482B1 ARYLCYCLOPROPYLAMINE BASED DEMETHYLASE INHIBITORS OF LSD1 AND THEIR MEDICAL USE 有权转让
标题翻译：芳基丙氨酰胺类LSD1二甲基酶抑制剂及其医疗用途
公开(公告)号：EP2598482B1
公开(公告)日：2018-04-04
申请号：EP11749119.1
申请日：2011-07-27
申请人： Oryzon Genomics, S.A.
发明人： ORTEGA MUÑOZ, Alberto , FYFE, Matthew, Colin, Thor , MARTINELL PEDEMONTE, Marc , TIRAPU FERNANDEZ DE LA CUESTA, Iñigo , ESTIARTE-MARTÍNEZ, Maria de los Ángeles
IPC分类号： A61K31/422 , A61K31/4245 , A61K31/433 , C07D285/08 , C07D285/135 , C07D213/73 , C07D237/20 , C07D239/42 , C07D241/20 , C07D263/48 , C07D277/40 , C07D401/12 , C07D417/12 , C07D271/07 , C07D271/113 , C07D253/07 , C07D261/14 , C07D285/12 , C07D413/12
CPC分类号： C07D417/12 , A61K31/422 , A61K31/4245 , A61K31/433 , A61K31/4439 , A61K31/506 , 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.

2. 发明授权

EP2300455B1 SALTS OF 2-FLUORO-N-METHYL-4-[7-(QUINOLIN-6-YL-METHYL)- IMIDAZO[1,2-B][1,2,4]TRIAZIN-2-YL]BENZAMIDE AND PROCESSES RELATED TO PREPARING THE SAME 有权转让
公开(公告)号：EP2300455B1
公开(公告)日：2017-07-19
申请号：EP09751439.2
申请日：2009-05-20
申请人： Incyte Holdings Corporation
发明人： WENG, Lingkai , QIAO, Lei , ZHOU, Jiacheng , LIU, Pingli , PAN, Yongchun
IPC分类号： C07D401/10 , C07D487/04 , C07D253/07 , A61K31/53 , A61P35/00
CPC分类号： A61K31/53 , C07D253/07 , C07D401/10 , C07D487/04
摘要： The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof.

3. 发明公开

EP3116861A1 SMALL MOLECULES FOR INHIBITING MALE FERTILITY 有权
标题翻译： KLEINMOLEKÜLEZUR HEMMUNG DERMÄNNLICHENFRUCHTBARKEIT
公开(公告)号：EP3116861A1
公开(公告)日：2017-01-18
申请号：EP15761799.4
申请日：2015-03-13
申请人： The University of North Carolina at Chapel Hill
发明人： O'RAND, Michael
IPC分类号： C07D251/52 , C07D253/07 , C07D253/075 , C07D487/04 , C07D498/04 , A61K31/53 , A61P15/16
CPC分类号： C07D251/52 , A61K31/53 , C07D253/07 , C07D253/075 , C07D487/04 , C07D498/04
摘要： Compounds suitable for use in providing male contraception, an assay method for identifying such compounds, and methods of providing contraception using the compounds, are provided. In one embodiment, the compounds described herein mimic the binding of anti-EPPIN antibodies to EPPIN, and thus inhibit the forward motility of sperm in humans and other primates. In another embodiment, the compounds described herein inhibit or enhance EPPIN-semenogelin binding, and inhibit forward motility of sperm. The assays described herein identify compounds which inhibit sperm motility, and can be carried out in a high throughput manner, using labeled recombinant EPPIN and semenogelin. The compounds can be used in oral or transdermal compositions to temporarily and reversibly inhibit male fertility. They can also be used in addition to, or in place of, spermicides in spermicidal compositions, such as those used in conjunction with condoms, diaphragms, and spermicidal jellies.
摘要翻译：提供了适用于提供男性避孕的化合物，用于鉴定这些化合物的测定方法以及使用该化合物提供避孕方法。在一个实施方案中，本文所述的化合物模拟抗EPPIN抗体与EPPIN的结合，并因此抑制精子在人和其他灵长类动物中的向前运动。在另一个实施方案中，本文所述的化合物抑制或增强EPPIN-精液素结合，并抑制精子的向前运动。本文描述的测定法使用标记的重组EPPIN和精液蛋白来鉴定抑制精子活力的化合物，并且可以以高通量的方式进行。这些化合物可用于口服或透皮组合物中以暂时和可逆地抑制雄性生育力。除了杀精组合物中的杀精剂外，还可以使用它们，例如与避孕套，隔膜和杀精胶冻结合使用的杀精剂。

4. 发明公开

EP2903976A1 1,2,4-TRIAZINE DERIVATIVES FOR THE TREATMENT OF VIRAL INFECTIONS. 有权
标题翻译：用于治疗病毒感染的1,2,4-三嗪衍生物
公开(公告)号：EP2903976A1
公开(公告)日：2015-08-12
申请号：EP13773690.6
申请日：2013-10-01
申请人： Centre National de la Recherche Scientifique (CNRS) , Universite de Rouen , Institut National Des Sciences Appliquees De Rouen
发明人： GEMBUS, Vincent , JUBAULT, Philippe , HOARAU, Christophe , LEVACHER, Vincent , BONFANTI, Jean-François , MC GOWAN, David, Graig , GUILLEMONT, Jérôme, Emile, Georges
IPC分类号： C07D401/12 , C07D253/07 , A61K31/53 , A61P31/12
CPC分类号： C07D253/075 , C07D253/07 , C07D401/12
摘要： This invention relates to 1,2,4-triazine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.

5. 发明授权

EP2697302B1 COMPOSITION DE CAOUTCHOUC COMPRENANT UN DÉRIVÉ DE LA 1,2,4-TRIAZINE 有权
标题翻译： WITH A 1,2,4-三嗪衍生物的橡胶组合物
公开(公告)号：EP2697302B1
公开(公告)日：2015-06-03
申请号：EP12715955.6
申请日：2012-04-16
申请人： Compagnie Générale des Etablissements Michelin , MICHELIN Recherche et Technique S.A.
发明人： VEYLAND, Anne , SEEBOTH, Nicolas
IPC分类号： C08K5/00 , C08K5/3492 , C07D253/07 , C08L21/00
CPC分类号： C08L9/06 , C07D253/07 , C07D487/04 , C07F9/65212 , C08K5/0025 , C08K5/34928 , C08K5/378 , C08K5/5373 , C08L21/00

6. 发明授权

EP2325186B1 Fused Bicyclic mTor Inhibitors 有权
标题翻译：稠合双环mTOR抑制剂
公开(公告)号：EP2325186B1
公开(公告)日：2014-10-08
申请号：EP11155268.3
申请日：2006-11-15
申请人： OSI Pharmaceuticals, LLC
发明人： Chen, Xin , Coate, Heather , Crew, Andrew-Philip , Dong, Han-Qing , Honda, Ayako , Mulvihill, Mark Joseph , Tavares, Paula, A.R. , Wang, Jing , Werner, Douglas S. , Mulvihill, Kristen Michelle , Siu, Kam W. , Panicker, Bijoy , Bharadwaj, Apoorba , Arnoldd, Lee D. , Jin, Meizhong , Volk, Brian , Weng, Qinghua , Beard, James David
IPC分类号： C07D487/04 , C07D519/00 , A61K31/4985 , A61P35/00
CPC分类号： C07D487/04 , A61K31/5025 , C07D253/07 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14

7. 发明公开

EP2633088A1 NON METAL TANNING 有权转让
标题翻译： METALLFREIE GERBUNG
公开(公告)号：EP2633088A1
公开(公告)日：2013-09-04
申请号：EP11771023.6
申请日：2011-10-05
申请人： Clariant Finance (BVI) Limited
发明人： REINEKING, Claus , GAMARINO, Roberta , TRIMARCO, Licia , QUAGLIERINI, Maurizio , GISLER, Markus , NUSSER, Rainer
IPC分类号： C14C3/26 , C14C3/28 , C07D251/44
CPC分类号： C14C3/00 , C07D251/44 , C07D253/00 , C07D253/065 , C07D253/07 , C07D253/075 , C14C3/02 , C14C3/04 , C14C3/08 , C14C3/26 , C14C3/28
摘要： Tanned leather, skin or pelt is produced by non-metal tanning, comprising the step of tanning a bated hide, skin or pelt with a tanning agent (A), the tanning agent (A) being at least one compound of a formula (I), wherein X signifies fluorine or chlorine, and/or (+NR3)0-1, wherein R is a substituted or unsubstituted C1 to C6 alkyl group, a substituted or unsubstituted C6 to C10 aryl or a C5 to C6heteroaryl group, R1 signifies hydrogen, C1-8-alkyl or an alkyleneoxy radical of a formula (Ia), -(—C2-3 alkylene-O—)q—H (Ia), R2 signifies hydrogen or hydroxyl, m, signifies 1, 2 or 3, q is of from 1 to 10, M signifies hydrogen or an alkali metal cation or an ammonium cation, being a protonated tertiary amine or a quaternary ammonium cation, in a tanning bath having a pH of from 6 to 10 at the beginning of tanning step.

8. 发明授权

EP2486088B1 COMPOSITION DE CAOUTCHOUC COMPRENANT UNE 1, 2, 4 - TRIAZINE 有权
标题翻译：包含1,2,4 - 三嗪的橡胶组合物
公开(公告)号：EP2486088B1
公开(公告)日：2013-09-04
申请号：EP10768440.9
申请日：2010-10-08
申请人： COMPAGNIE GENERALE DES ETABLISSEMENTS MICHELIN , MICHELIN Recherche et Technique S.A.
发明人： VEYLAND, Anne , SEEBOTH, Nicolas , ARAUJO DA SILVA, José Carlos
IPC分类号： C08K5/00 , C08K5/3492 , B60C1/00 , C07D253/02 , C08K5/43
CPC分类号： C07D253/07 , B60C1/00 , B60C1/0016 , C08K5/0025 , C08K5/3492 , C08K5/43 , C08L21/00

9. 发明公开

EP2611771A1 NEW COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF 有权
标题翻译：替代代谢产物阿维菌素衍生物ALS ACC HEMMER ZUR BEHANDLUNG代谢物KRANKHEITEN
公开(公告)号：EP2611771A1
公开(公告)日：2013-07-10
申请号：EP11752529.5
申请日：2011-09-01
申请人： Boehringer Ingelheim International GmbH
发明人： ROTH, Gerald Juergen , FLECK, Martin , HEINE, Niklas , KLEY, Joerg , LEHMANN-LINTZ, Thorsten , NEUBAUER, Heike , NOSSE, Bernd
IPC分类号： C07C233/16 , C07C233/57 , C07C233/64 , C07C255/50 , C07C271/16 , C07C275/24 , C07D209/10 , C07D213/08 , C07D213/24 , C07D213/60 , C07D231/12 , C07D233/54 , C07D239/26 , C07D239/42 , C07D241/12
CPC分类号： C07C233/18 , C07B2200/07 , C07C233/05 , C07C233/13 , C07C233/20 , C07C233/31 , C07C233/36 , C07C233/47 , C07C233/58 , C07C233/60 , C07C235/08 , C07C235/40 , C07C237/08 , C07C237/22 , C07C237/42 , C07C255/19 , C07C255/46 , C07C255/60 , C07C271/16 , C07C275/24 , C07C275/40 , C07C311/04 , C07C311/10 , C07C311/14 , C07C317/44 , C07C323/41 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2602/08 , C07D205/04 , C07D205/08 , C07D207/10 , C07D207/12 , C07D207/325 , C07D209/08 , C07D209/44 , C07D211/16 , C07D211/76 , C07D213/30 , C07D213/40 , C07D213/64 , C07D213/643 , C07D213/65 , C07D213/74 , C07D213/75 , C07D213/79 , C07D213/82 , C07D215/12 , C07D217/06 , C07D231/12 , C07D231/14 , C07D233/64 , C07D233/90 , C07D237/08 , C07D237/14 , C07D239/26 , C07D239/28 , C07D239/34 , C07D239/38 , C07D239/42 , C07D239/52 , C07D249/10 , C07D253/07 , C07D261/08 , C07D261/14 , C07D261/18 , C07D263/32 , C07D263/34 , C07D263/58 , C07D271/08 , C07D277/24 , C07D277/28 , C07D277/56 , C07D295/088 , C07D295/192 , C07D305/06 , C07D305/08 , C07D307/14 , C07D307/24 , C07D307/68 , C07D307/79 , C07D309/12 , C07D317/62 , C07D319/08 , C07D321/10 , C07D401/04 , C07D401/08 , C07D401/12 , C07D403/04 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The invention relates to new compounds of the formula (I) to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
摘要翻译：本发明涉及其用作药物的式I的新化合物，其治疗用途的方法和含有它们的药物组合物。

10. 发明公开

EP2370413A1 MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 有权转让
标题翻译：前列腺素（PGI2）受体的调节剂可用于治疗与其有关的疾病
公开(公告)号：EP2370413A1
公开(公告)日：2011-10-05
申请号：EP09775380.0
申请日：2009-12-07
申请人： Arena Pharmaceuticals, Inc.
发明人： TRAN, Thuy-Anh , HAYASHI, Rena , IBARRA, Jason B. , ULLMAN, Brett , ZOU, Ning
IPC分类号： C07D237/14 , C07D401/04 , C07D403/04 , C07D409/04 , C07D253/07 , A61K31/50 , A61K31/501 , A61K31/53 , A61P11/08
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调节PGI 2受体活性的药物组合物。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）和相关病症的方法; 血小板聚集; 冠状动脉疾病; 心肌梗塞; 短暂性脑缺血发作; 心绞痛; 行程; 缺血再灌注损伤; 再狭窄; 心房颤动; 血管成形术或冠状动脉旁路手术中的血块形成个体或患有心房纤颤的个体; 动脉粥样硬化; 动脉粥样硬化; 哮喘或其症状; 糖尿病相关病症如糖尿病周围神经病变，糖尿病肾病或糖尿病视网膜病变; 青光眼或眼内压异常的其他疾病; 高血压; 炎; 银屑病; 银屑病关节炎; 类风湿关节炎; 克罗恩病; 移植排斥; 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; 和慢性阻塞性肺病（COPD）。

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