公开(公告)号：EP3118204A1

公开(公告)日：2017-01-18

申请号：EP15740755.2

申请日：2015-01-14

申请人： Sun Yat-Sen University

发明人： BU, Xianzhang ,  ZHU, Cuige ,  YUE, Xin ,  ZUO, Yinglin ,  CHEN, Yu ,  WEN, Gesi

IPC分类号： C07F5/02 ,  C07C225/22 ,  C07C221/00 ,  C07C45/45 ,  C07C49/84 ,  C07C49/835 ,  C07F9/12 ,  C07C253/30 ,  A61P35/00

CPC分类号： C07F9/12 ,  C07C45/45 ,  C07C45/63 ,  C07C49/248 ,  C07C49/255 ,  C07C49/835 ,  C07C49/84 ,  C07C51/347 ,  C07C51/373 ,  C07C65/38 ,  C07C221/00 ,  C07C225/22 ,  C07C253/30 ,  C07C255/56 ,  C07C303/22 ,  C07C309/44 ,  C07D207/08 ,  C07D295/112 ,  C07D295/12 ,  C07F5/025 ,  C07C49/813

摘要： Disclosed are an o-phenyl chalcone compounds and preparation methods and uses thereof. The o-phenyl chalcone compounds are capable of inhibiting the aggregation of microtubules in tumor cells and influencing the mitosis of the cells, and has a high antitumor activity. The compounds also have inhibitory activity against proliferation on various tumor cells, such as a human ovary cancer cell A2780, a human colon cancer cell HCT8, a human breast cancer cell MCF7, a human lung cancer cell A549, a human colon cancer cell SW480, a human nasopharyngeal carcinoma cell CNE2, a human liver cancer cell HepG2 and the like at nanomole concentrations.

摘要翻译： 公开了邻苯基查耳酮化合物及其制备方法和用途。 邻苯基查耳酮化合物能够抑制肿瘤细胞中微管的聚集并影响细胞的有丝分裂，并且具有高的抗肿瘤活性。 该化合物还具有抑制各种肿瘤细胞增殖的作用，例如人卵巢癌细胞A2780，人结肠癌细胞HCT8，人乳腺癌细胞MCF7，人肺癌细胞A549，人结肠癌细胞SW480， 人鼻咽癌细胞CNE2，人肝癌细胞HepG2等纳米摩尔浓度。

公开(公告)号：EP2741609A4

公开(公告)日：2015-04-08

申请号：EP12823508

申请日：2012-08-10

申请人： SALK INST FOR BIOLOGICAL STUDI

发明人： SCHUBERT DAVID R ,  MAHER PAMELA A ,  CHIRUTA CHANDRAMOULI

IPC分类号： A01N37/10 ,  C07D215/233

CPC分类号： A61K31/47 ,  A61K31/12 ,  A61K31/352 ,  A61K31/353 ,  A61K31/4025 ,  A61K31/4709 ,  A61K45/06 ,  C07C49/835 ,  C07C49/84 ,  C07D215/233 ,  C07D295/112 ,  C07D311/30 ,  C07D311/60 ,  C07D311/62 ,  C07D311/78

摘要： The present invention provides neuroprotective polyphenol compounds, which can be synthetic analogs of fisetin, baicalein or chlorogenic acid, that maintain neuroprotective, anti-inflammatory, glutathione promoting, and/or antioxidant properties. The neuroprotective polyphenol compounds are useful for promoting, enhancing and/or increasing neuron protection, growth and/or regeneration. The polyphenol compounds further find use for increasing and or maintaining intracellular glutathione (GSH) levels. The polyphenol compounds are also useful for treating, preventing, mitigating and/or delaying neurodegenerative conditions, including diabetes, Parkinson's disease, Huntington's disease, Alzheimer's disease, non-Alzheimer's dementias, multiple sclerosis, traumatic brain injury, spinal cord injury or ALS.

公开(公告)号：EP2766339A1

公开(公告)日：2014-08-20

申请号：EP12783752.4

申请日：2012-10-15

申请人： The United States Of America, As Represented By The Secretary, Department Of Health And Human Services ,  The Cooper Health System

发明人： WAINER, Irving, W. ,  MOADDEL, Ruin ,  BERNIER, Michel ,  ZARATE, Carlos, A. ,  TORJMAN, Marc, C. ,  GOLDBERG, Michael, E. ,  TANGA, Mary, J.

IPC分类号： C07C225/20 ,  C07C237/02 ,  C07D295/155 ,  C07D295/145 ,  A61P25/04 ,  A61P25/28 ,  A61P25/00 ,  A61K31/133 ,  A61K31/122

CPC分类号： A61K31/5375 ,  A61K31/137 ,  A61K31/165 ,  A61K31/222 ,  A61K31/24 ,  A61K31/265 ,  A61K31/4453 ,  C07B2200/07 ,  C07C225/20 ,  C07C229/48 ,  C07C237/04 ,  C07C237/20 ,  C07C2601/14 ,  C07C2601/16 ,  C07D295/108 ,  C07D295/112 ,  C07D295/15 ,  C07D295/155

摘要： The disclosure provides pharmaceutical preparations containing (2R,6R)-hydroxynorketamine, or (R)- or (S)-dehydronorketamine, or other stereoisomeric dehydro or hydroxylated ketamine metabolite. (2R,6R)-hydroxynorketamine The disclosure also provides novel ketamine metabolite prodrugs. The disclosure provides methods of treating, bipolar depression, major depressive disorder, neuropathic and chronic pain, including complex regional pain disorder (CRPS) by administering a purified ketamine metabolite or a ketamine metabolite prodrug directly to patients in need of such treatment.

摘要翻译： 因此，本发明提供了新颖的氯胺酮代谢物的前体药物。 本公开提供治疗双相抑郁症，重度抑郁症，神经性疼痛和慢性疼痛，包括复杂区域疼痛合成疼痛障碍（CRPD）通过给予纯化氯胺酮的代谢产物或代谢氯胺酮前体药物直接有需要的患者寻求治疗的方法。

公开(公告)号：EP1553074B1

公开(公告)日：2014-06-18

申请号：EP03788076.2

申请日：2003-08-11

申请人： Takeda Pharmaceutical Company Limited

发明人： SHIRAISHI, Mitsuru ,  HARA, Takahito ,  KUSAKA, Masami ,  KANZAKI, Naoyuki ,  YAMAMOTO, Satoshi ,  MIYAWAKI, Toshio

IPC分类号： C07C35/52 ,  C07C255/52 ,  C07C255/53 ,  C07C255/56 ,  C07D207/06 ,  C07D207/08 ,  C07D207/10 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D207/22 ,  C07D211/22 ,  C07D211/34 ,  C07D405/04 ,  C07D409/04 ,  A61K31/045 ,  A61K31/402 ,  A61K31/42 ,  A61K31/54 ,  A61P5/26 ,  A61P15/00 ,  A61P35/00

CPC分类号： C07C255/52 ,  C07C35/52 ,  C07C217/04 ,  C07C255/53 ,  C07C255/54 ,  C07C255/56 ,  C07C2601/08 ,  C07C2601/10 ,  C07D207/06 ,  C07D207/08 ,  C07D207/10 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D207/22 ,  C07D207/24 ,  C07D209/46 ,  C07D211/22 ,  C07D211/28 ,  C07D211/34 ,  C07D211/42 ,  C07D211/46 ,  C07D211/60 ,  C07D211/62 ,  C07D211/74 ,  C07D231/08 ,  C07D261/04 ,  C07D265/02 ,  C07D267/10 ,  C07D295/073 ,  C07D295/112 ,  C07D295/155 ,  C07D303/46 ,  C07D307/79 ,  C07D333/54 ,  C07D405/04 ,  C07D409/04 ,  C07D491/10

公开(公告)号：EP2606021A4

公开(公告)日：2014-05-07

申请号：EP11818654

申请日：2011-08-16

申请人： UNIV TOKYO ,  ANDROSCIENCE CORP

发明人： SHIH CHARLES C-Y ,  KITUMURA TOSHIO ,  SHI QIAN ,  KAWASHIMA TOSHIYUKI ,  WANG HUI-KANG

IPC分类号： C07C49/248 ,  A61K31/121 ,  A61P35/00 ,  C07C309/67 ,  C07D211/06

CPC分类号： C07C49/248 ,  C07C49/235 ,  C07C49/255 ,  C07C69/16 ,  C07C217/22 ,  C07C217/60 ,  C07C235/82 ,  C07C307/02 ,  C07C309/65 ,  C07C309/66 ,  C07C309/73 ,  C07C317/24 ,  C07C2601/14 ,  C07C2601/16 ,  C07D213/68 ,  C07D295/112 ,  C07D295/13 ,  C07F9/06 ,  C07F9/09 ,  C07F9/12 ,  C07F9/32 ,  C07F9/3282

摘要： This invention relates to compounds of Formula (I), (II), or (III) as shown in the specification, which contain a 1,5-diphenylpenta-1,4-dien-3-one backbone. These compounds can be used to treat cancer, inflammatory disease, or autoimmune disease.

公开(公告)号：EP1979311A2

公开(公告)日：2008-10-15

申请号：EP06830789.1

申请日：2006-12-21

申请人： TRANSTECH PHARMA

发明人： SAUERBERG, Per ,  PIHERA, Pavel ,  POLIVKA,Zdenék ,  HAVRANEK, Miroslav ,  PETTERSSON, Ingrid ,  MOGENSEN, John, Patrick

IPC分类号： C07C323/16 ,  A61K31/44 ,  A61P3/10 ,  C07D213/30 ,  C07D211/46 ,  C07D333/54 ,  C07D333/16 ,  C07D231/12 ,  C07D307/79 ,  C07C59/68 ,  C07D295/08

CPC分类号： A61K31/5377 ,  A61K31/192 ,  A61K31/195 ,  A61K31/343 ,  A61K31/381 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/415 ,  A61K31/4402 ,  A61K31/445 ,  A61K31/495 ,  A61K31/5375 ,  C07C59/70 ,  C07C217/48 ,  C07C323/16 ,  C07C323/32 ,  C07C2601/02 ,  C07D211/46 ,  C07D213/30 ,  C07D213/36 ,  C07D231/12 ,  C07D265/30 ,  C07D295/096 ,  C07D295/112 ,  C07D307/79 ,  C07D307/81 ,  C07D333/16 ,  C07D333/20 ,  C07D333/54

摘要： Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPAR´ and should be useful for treating conditions mediated by the same.

公开(公告)号：EP1870405A1

公开(公告)日：2007-12-26

申请号：EP06291027.8

申请日：2006-06-22

申请人： BIOPROJET

发明人： Capet, Marc ,  Danvy, Denis ,  Levoin, Nicolas ,  Berrebi-Bertrand, Isabelle ,  Calmels, Thierry ,  Robert, Philippe ,  Lecomte, Jeanne-Marie ,  Schwartz, Jean-Charles ,  Ligneau, Xavier

IPC分类号： C07D295/12 ,  A61K31/495 ,  A61P25/00 ,  C07D211/26 ,  C07D295/14 ,  C07D295/10 ,  C07D307/24 ,  C07D211/70 ,  C07D211/60 ,  C07D213/74 ,  C07D217/02 ,  C07D239/42 ,  C07D215/40

CPC分类号： C07D213/74 ,  C07D211/26 ,  C07D211/60 ,  C07D211/70 ,  C07D215/40 ,  C07D217/02 ,  C07D239/42 ,  C07D295/10 ,  C07D295/112 ,  C07D295/135 ,  C07D295/14 ,  C07D295/155 ,  C07D307/24

摘要： The invention relates to compounds of the general formula (I):

to the process for preparing them, and to the use thereof as a therapeutic agent.

摘要翻译： 本发明涉及通式（I）的化合物：其制备方法及其作为治疗剂的用途。

公开(公告)号：EP1814850A1

公开(公告)日：2007-08-08

申请号：EP05797249.9

申请日：2005-09-30

申请人： DAC S.R.L.

发明人： MINUCCI, Saverio ,  PELICCI, Pier Giuseppe ,  MAI, Antonello ,  BALLARINI, Marco ,  GARGIULO, Gaetano ,  MASSA, Silvio

IPC分类号： C07D207/32 ,  C07D307/46 ,  C07D333/22 ,  C07D409/06 ,  C07C259/06 ,  C07D333/56 ,  C07D213/46 ,  C07D307/80 ,  A61K31/165 ,  A61K31/435 ,  A61K31/4436 ,  A61P35/00

CPC分类号： C07C259/06 ,  C07D207/333 ,  C07D213/46 ,  C07D213/54 ,  C07D295/112 ,  C07D307/46 ,  C07D307/80 ,  C07D333/22 ,  C07D333/56 ,  C07D409/06

摘要： New inhibitors of histone deacetylases having antitumor activity, and the process of preparation thereof are herein described. These compounds belong to the structural formula (I) where R1 is a linear or branched chain containing at least two conjugated double bonds, A is an optionally substituted phenyl or pyridyl ring, Ar is an aryl or heteroaryl group, and R3 is hydrogen or alkoxyalkyl. The application also describes the use of said compounds in the treatment of diseases associated to the deregulation of histone deacetylases activity, such as tumors, as well as the relevant pharmaceutical compositions for administration to patients requiring said treatment.

公开(公告)号：EP1682486A1

公开(公告)日：2006-07-26

申请号：EP04790064.2

申请日：2004-10-28

申请人： Lica Pharmaceuticals A/S

发明人： NIELSEN, Simon, Feldb k

IPC分类号： C07C225/22 ,  C07C225/16 ,  C07C217/22 ,  C07D295/10 ,  A61K31/14 ,  A61K31/4965 ,  A61P31/04

CPC分类号： C07D295/112 ,  C07C217/22 ,  C07C225/16 ,  C07C225/22

摘要： The present invention provides novel quaternary amino-functional chalcone derivatives and analogues exhibiting interesting antibacterial activity. The compounds have the general formula (Y1)m-Ar1(X1)-C(=O)Var2(X2)-(Y2)p (I), wherein V designates -CH2-CH2-, -CH=CH-or -C=C; Ar1 and Ar2 independently are aryl and heteroary.; m=0, 2, p=0, 1, 2, m+p>0; each Y1 and Y2 independently is -Z-N+(R1)(R2)R4 Q-(A); -NR3-Z-N+(R1)(R2)R4 Q- (B), or O-Z-N+(R1)(R2)R4 Q- (C), R1, R2, R3, R4, X1, X2 are substituents, and Q- is an anion. The present invention also relates to the compounds for sue as pharmaceutically active agents, in particular against bacterial infections (such as Gram-negative and Gram-positive bacteria, including antibiotic-sensitive or resistant strains), and in the medical treatment of bacterial infections in mammals.

公开(公告)号：EP1451167B1

公开(公告)日：2006-03-08

申请号：EP02792315.0

申请日：2002-12-02

申请人： Ortho-McNeil Pharmaceutical, Inc.

发明人： APODACA, Richard ,  XIAO, Wei ,  JABLONOSKI, Jill, A.

IPC分类号： C07D295/02 ,  C07D211/14 ,  C07D211/46 ,  C07D215/06 ,  A61K31/44 ,  A61P25/00

CPC分类号： C07D239/42 ,  A61K31/444 ,  A61K31/4453 ,  A61K31/4709 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/541 ,  C07D203/12 ,  C07D209/16 ,  C07D211/14 ,  C07D211/22 ,  C07D211/44 ,  C07D211/46 ,  C07D211/60 ,  C07D211/62 ,  C07D213/38 ,  C07D215/06 ,  C07D273/00 ,  C07D277/04 ,  C07D295/02 ,  C07D295/03 ,  C07D295/073 ,  C07D295/096 ,  C07D295/112 ,  C07D295/135 ,  C07D295/205 ,  C07D401/04 ,  C07D401/12 ,  C07D471/10 ,  C07D491/10

摘要： Substituted phenylalkynes of formula (l), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.