公开(公告)号：EP2635274B1

公开(公告)日：2017-12-06

申请号：EP11838597.0

申请日：2011-10-31

Applicant: The Ohio State University Research Foundation

Inventor： CHEN, Ching-shih ,  CHIU, Hao-Chieh ,  WANG, Dasheng ,  KULP, Samuel, K.

IPC: A61K31/415 ,  A61K31/4155 ,  A61K31/5415 ,  C07D231/12 ,  C07D405/04 ,  C07D471/04 ,  A61P31/04

CPC classification number: C07D471/04 ,  A61K31/415 ,  A61K31/5415 ,  C07D231/12 ,  C07D405/04

Abstract: A method of treating infection by Staphylococcus in a subject by administering a pharmaceutical composition including a celecoxib derivative of formula I or a pharmaceutically acceptable salt thereof is described. The preparation of numerous celecoxib derivatives for testing as potential anti-staphylococcal agents is also described.

公开(公告)号：EP3207929A3

公开(公告)日：2017-10-11

申请号：EP16198280.6

申请日：2004-04-14

Applicant: California Pacific Medical Center ,  Catholic Healthcare West, d.b.a. St. Mary's Medical Center

Inventor： YANG, Li-Xi

IPC: A61K31/4439 ,  A61K31/433 ,  A61K31/403 ,  A61K31/155 ,  A61K31/175 ,  C07C323/41 ,  C07C323/42 ,  C07C323/60 ,  C07H5/06 ,  C07D295/15

CPC classification number: C07C323/41 ,  C07C323/42 ,  C07C323/60 ,  C07C2603/18 ,  C07C2603/24 ,  C07C2603/34 ,  C07D295/15 ,  C07H5/06

Abstract: Certain N-deacetylcolchicine and N-deacetylthiocolchine derivatives are described wherein the 7-N position on the B ring is substituted with the group - C(O)-(CHR 4 ) m -AR, wherein m is an integer of 0-10, A is S, O, N or a covalent bond; R 1 is substituted phenyl or substituted benzoyl; optionally substituted cycloalkyl of 3-7 carbons; optionally substituted naphtyl; an optionally substituted imide ring; an optionally substituted 5 or 6 member heterocycle with at least one N, S, or O in the ring; or an optionally substituted fused heterocyclic or fused carboxyclic ring system; R 2 (at the 2-position of the A ring) is methoxy, hydroxy, or methylenedioxy when taken together with R 3 ; R 3 (at the 3-position of the A ring) is methoxy, hydroxy, a monosaccharide radical, or is methylenedioxy when taken together with R 2 ; and R 4 is H or is H or methyl when m is 1. Also dimers of such compounds are disclosed. When combined with suitable pharmaceutical excipients, these compounds are useful for treating various types of cancer.

公开(公告)号：EP2650283B1

公开(公告)日：2017-06-07

申请号：EP13175481.4

申请日：2007-04-24

Applicant: NIPPON SODA CO., LTD.

Inventor： Shibata, Yasushi ,  Imagawa, Tsutomu

IPC: C07D213/61 ,  C07B43/04 ,  C07D401/06 ,  C07D401/14 ,  C07D257/08 ,  C07D277/20

CPC classification number: C07D213/61 ,  C07B43/04 ,  C07C209/06 ,  C07C211/03 ,  C07C211/48 ,  C07C211/62 ,  C07D251/04 ,  C07D257/08 ,  C07D277/20 ,  C07D401/06 ,  C07D401/14 ,  C08G73/0627 ,  C08G73/0644

Abstract: The present invention provides a process that enables a substituted methylamine compound which is useful as an intermediate for the production of agricultural chemicals and medicines, to be produced easily, with good yield, and at low cost, and also provides a production intermediate thereof. The process comprises a step of reacting a hexamethylenetetraammonium salt compound represented by a formula (I) with a base to obtain an N-methylidene-substituted methylamine oligomer represented by a formula (II) or a mixture of two or more of the oligomers, and a step of hydrolyzing the N-methylidene-substituted methylamine oligomer represented by formula (II) or the mixture of two or more of the oligomers in the presence of an acid. (wherein A represents an organic group that is either a hydrocarbon group or a heterocyclic group, or said organic group that has a substituent, R represents a hydrogen atom, an organic group that is either a hydrocarbon group or a heterocyclic group, or said organic group that has a substituent, L represents a halogen atom and the like, and n represents an integer of 2 to 20)

Abstract translation: 本发明提供了一种方法，该方法能够容易地以良好的收率和低成本生产用作农药和药品生产中间体的取代甲胺化合物，并且还提供了其生产中间体。 该方法包括使由式（I）表示的六亚甲基四铵盐化合物与碱反应以获得由式（II）表示的N-亚甲基取代的甲胺低聚物或两种或更多种低聚物的混合物的步骤，以及 在酸的存在下水解由式（II）表示的N-亚甲基取代的甲胺低聚物或两种或更多种低聚物的混合物的步骤。 （式中，A表示烃基或杂环基的有机基团，或者所述具有取代基的有机基团，R表示氢原子，烃基或杂环基的有机基团，或者所述有机基团 具有取代基的基团，L表示卤素原子等，n表示2〜20的整数）

公开(公告)号：EP2623113B1

公开(公告)日：2017-05-31

申请号：EP13157801.5

申请日：2006-11-09

Applicant: Onyx Therapeutics, Inc.

Inventor： Zhou, Han-Jie ,  Sun, Congcong M. ,  Shenk, Kevin D. ,  Laidig, Guy J.

IPC: C07K5/062 ,  A61K38/55 ,  C07K5/08 ,  C07K5/10 ,  C07K5/065 ,  C07K5/078 ,  C07K5/083 ,  C07K5/087 ,  C07K5/097 ,  C07K5/117

CPC classification number: C07K5/08 ,  A61K31/69 ,  A61K38/00 ,  A61K38/06 ,  A61K38/55 ,  A61K45/06 ,  C07K5/06026 ,  C07K5/06034 ,  C07K5/0606 ,  C07K5/06078 ,  C07K5/06139 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/081 ,  C07K5/0812 ,  C07K5/0821 ,  C07K5/1024 ,  A61K2300/00

公开(公告)号：EP2054367B1

公开(公告)日：2017-03-22

申请号：EP07841187.3

申请日：2007-08-22

Applicant: SI Group, Inc.

Inventor： PHAN, Hao, V.

IPC: C07C51/41 ,  C07C51/44 ,  C07C51/46 ,  C07C51/47 ,  C07C57/30

CPC classification number: C07C51/44 ,  C07C51/412 ,  C07C51/47 ,  Y10T428/2982 ,  C07C57/30

Abstract: A free-flowing hydrated sodium salt of ibuprofen of controlled median particle size and water content is provided. It can be produced by adding aqueous NaOH to a non-boiling solution or slurry of ibuprofen in an organic solvent that can be distilled along with water at a temperature in the range of 50 to 120° C. The rate of NaOH addition is at a rate that does not cause the resultant reaction mixture to boil before the addition has been completed. After completing the addition, the water is removed with some of the organic solvent by distillation. After cooling, the hydrated sodium salt of ibuprofen is recovered from the resultant slurry. The process enables the median particle size of the sodium salt of ibuprofen formed to be controlled by selection and use of a predetermined effective concentration of NaOH in the aqueous NaOH solution used.

Abstract translation: 提供了控制中值粒径和含水量的自由流动的布洛芬水合钠盐。 可以通过向非沸腾溶液或布洛芬的浆液中加入NaOH水溶液来制备，所述有机溶剂可以在50至120℃的温度范围内与水一起蒸馏。加入NaOH的速率为 在添加完成之前不会使所得反应混合物沸腾的速率。 加完后，用一些有机溶剂通过蒸馏除去水分。 冷却后，从所得浆料中回收布洛芬的水合钠盐。 该方法可以通过在所用NaOH水溶液中选择和使用预定有效浓度的NaOH来控制形成的布洛芬钠盐的中值粒度。

公开(公告)号：EP3121169A1

公开(公告)日：2017-01-25

申请号：EP16173815.8

申请日：2007-07-10

Applicant: WisTa Laboratories Ltd.

Inventor： WISCHIK, Claude Michel ,  STOREY, John Mervyn David ,  MARSHALL, Colin ,  SINCLAIR, James Peter ,  BADDELEY, Thomas Craven

IPC: C07D279/18

CPC classification number: A61K31/5415 ,  C07D279/18 ,  C07D279/20

Abstract: This invention pertains generally to the field of chemical synthesis and purification, and more specifically to methods of synthesis and/or purification of certain 3,7-diamino-phenothiazin-5-ium compounds (referred to herein as "diaminophenothiazinium compounds") including Methylthioninium Chloride (MTC) (also known as Methylene Blue). The present invention also pertains to the resulting (high purity) compounds, compositions comprising them (e.g., tablets, capsules), and their use in methods of inactivating pathogens, and methods of medical treatment, prophylaxis, and diagnosis, etc., for example, a tauopathy; a disease of tau protein aggregation; Alzheimer's disease (AD); Pick's disease; Progressive Supranuclear Palsy (PSP); fronto-temporal dementia (FTD); FTD and parkinsonism linked to chromosome 17 (FTDP-17); disinhibition-dementia-parkinsonism-amyotrophy complex (DDPAC); pallido-ponto-nigral degeneration (PPND); Guam-ALS syndrome; pallido-nigro-luysian degeneration (PNLD); cortico-basal degeneration (CBD); mild cognitive impairment (MCI); skin cancer; melanoma; methemoglobinemia; a viral infection; a bacterial infection; a protozoal infection; a parasitic infection; malaria; visceral leishmaniasis; African sleeping sickness; toxoplasmosis; giardiasis; Chagas' disease; Hepatitis C virus (HCV) infection; human immunodeficiency virus (HIV) infection; West Nile virus (WNV) infection; a synucleinopathy; Parkinson's disease (PD); dementia with Lewy bodies (DLB); multiple system atrophy (MSA); drug-induced parkinsonism; and pure autonomic failure (PAF).

Abstract translation: 本发明一般涉及化学合成和纯化领域，更具体地涉及某些3,7-二氨基 - 吩噻嗪-5-鎓化合物（本文称为“二氨基吩噻嗪鎓化合物”）的合成和/或纯化方法，包括甲基锍 氯化物（MTC）（也被称为亚甲蓝）。 本发明还涉及所得（高纯度）化合物，包含它们的组合物（例如片剂，胶囊），以及它们在灭活病原体的方法中的用途，以及医学治疗，预防和诊断等的方法 ，一种tau蛋白病; τ蛋白质聚集的疾病; 阿尔茨海默病（AD）; 皮克氏病; 进行性核上性麻痹（PSP）; 额颞叶痴呆（FTD）; 与17号染色​​体相关的FTD和帕金森综合征（FTDP-17）; 去抑制 - 痴呆 - 帕金森病 - 肌萎缩综合征（DDPAC）; 苍白球 - 黑质变性（PPND）; 关岛 - ALS综合征; pallido-nigro-luysian degeneration（PNLD）; 皮质基底变性（CBD）; 轻度认知障碍（MCI）; 皮肤癌; 黑色素瘤; 高铁血红蛋白血症; 病毒感染; 细菌感染; 原虫感染; 寄生虫感染; 疟疾; 内脏利什曼病; 非洲昏睡病; 弓形虫病; 贾第虫病; 南美锥虫病; 丙型肝炎病毒（HCV）感染; 人类免疫缺陷病毒（HIV）感染; 西尼罗河病毒（WNV）感染; 突触核蛋白病; 帕金森病（PD）; 路易体痴呆（DLB）; 多系统萎缩（MSA）; 药物性帕金森综合征; 和纯自主神经衰竭（PAF）。

公开(公告)号：EP2207791B1

公开(公告)日：2016-04-13

申请号：EP08834964.2

申请日：2008-10-03

Applicant: Onyx Therapeutics, Inc.

Inventor： PHIASIVONGSA, Pasit ,  SEHL, Louis, C. ,  FULLER, William, Dean ,  LAIDIG, Guy, J.

IPC: A61P19/08 ,  A61P25/28 ,  A61P31/00 ,  A61P33/00 ,  A61P35/00 ,  A61P37/00 ,  A61P37/06 ,  C07D303/36 ,  C07D301/00 ,  C07K5/087 ,  C07D301/03 ,  A61K38/06

CPC classification number: C07K5/1016 ,  A61K38/00 ,  C07C51/412 ,  C07C53/18 ,  C07D301/00 ,  C07D301/03 ,  C07D303/36 ,  C07K1/1075 ,  C07K1/306 ,  C07K5/0812 ,  C07K5/1008

公开(公告)号：EP2309988B1

公开(公告)日：2015-11-25

申请号：EP09790340.5

申请日：2009-07-13

Applicant: SI Group, Inc.

Inventor： HU, Patrick, C.

IPC: A61K9/16 ,  A61K9/20 ,  A61K31/192

CPC classification number: A61K31/192 ,  A61K9/1611 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/1694 ,  A61K9/2009 ,  A61K9/2027 ,  A61K9/2054

Abstract: Granules of racemic sodium ibuprofen dihydrate formed from components specified herein have very desirable properties and can be effectively used in conventional rotary press tableting equipment without operational difficulties often encountered in actual practice. Their preparation by a wet granulation process, the wet granule compositions, formulations adapted for preparation of solid dosage forms utilizing a rotary press, solid dosage forms, and methods of preparing solid dosage forms in a rotary press are also described.

公开(公告)号：EP2888254A1

公开(公告)日：2015-07-01

申请号：EP13759274.7

申请日：2013-08-22

Applicant: The Institute of Cancer Research : The Royal Cancer Hospital

Inventor： JONES, Keith ,  CHEESEMAN, Matthew David ,  LINARDOPOULOS, Spyridon ,  FAISAL, Amir ,  BARBEAU, Olivier Remi ,  KALUSA, Andrew

IPC: C07D413/10 ,  C07D417/10 ,  C07D417/14 ,  A61K31/427 ,  A61K31/4439 ,  A61P35/00

CPC classification number: C07D417/14 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D417/10

Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts, hydrates and solvates thereof for use in the treatment of cancer:

公开(公告)号：EP2874606A1

公开(公告)日：2015-05-27

申请号：EP13820351.8

申请日：2013-07-17

Applicant: Onyx Therapeutics, Inc.

Inventor： CHU, Katherine, A. ,  CHAN, Elena, T. ,  FANG, Ying ,  JUMAA, Mouhannad ,  KIRK, Christopher, Justin ,  MUCHAMUEL, Tony, Marcel ,  WANG, Zhengping ,  JIANG, Jing ,  JONES, Jeffrey, Joseph

IPC: A61K9/127

CPC classification number: A61K9/127 ,  A61K9/1271 ,  A61K9/1277 ,  A61K38/07 ,  A61K45/06 ,  A61K47/22 ,  A61K47/6951

Abstract: Liposomal compositions comprising peptide epoxyketone compounds are described, as well as methods of making and using such liposomal compositions. These liposomal compositions enhance the therapeutic window of peptide epoxyketone compounds by improving in vivo half-life relative to non-liposomal compositions comprising peptide epoxyketone compounds, providing desirable pharmacodynamic profiles, and providing anti-tumor activity in a human tumor xenograft model, greater than or equal to non-liposomal compositions comprising peptide epoxyketone compounds. Further, experiments performed in support of the present invention demonstrated improved tolerability of liposomal compositions comprising peptide epoxyketone compounds.

Abstract translation: 描述了包含肽环氧酮化合物的脂质体组合物，以及制备和使用这种脂质体组合物的方法。 这些脂质体组合物通过相对于包含肽环氧酮化合物的非脂质体组合物改善体内半衰期而提高了肽环氧酮化合物的治疗窗口，提供了期望的药效学概况并提供了在人类肿瘤异种移植模型中的抗肿瘤活性， 等于包含肽环氧酮化合物的非脂质体组合物。 此外，支持本发明进行的实验表明包含肽环氧酮化合物的脂质体组合物的耐受性提高。