公开(公告)号：EP2640423A1

公开(公告)日：2013-09-25

申请号：EP11793558.5

申请日：2011-11-10

申请人： Ischemix LLC

发明人： BAGUISI, Alexander, B. ,  BEEUWKES, Reinier ,  CASALE, Ralph ,  KATES, Steven, A. ,  LADER, Alan, S.

IPC分类号： A61K47/48 ,  C07K5/06 ,  C07D339/04

CPC分类号： C07D339/04 ,  A61K47/64 ,  C07F9/655345 ,  C07K5/06026 ,  C07K5/06078 ,  C07K5/06104 ,  C07K5/06113

摘要： The present invention relates, in various embodiments, to a compound represented by Structural Formula (I), pharmaceutically acceptable salts or prodrugs thereof, and compositions comprising said compounds, or pharmaceutically acceptable salts or prodrugs thereof. Methods of using compounds of Structural Formulas (I) and (la) or compositions comprising compounds of Structural Formulas (I) and (la), or pharmaceutically acceptable salts or prodrugs thereof, to treat ischemia or ischemia-reperfusion injury are also disclosed.

摘要翻译： 本发明在各种实施方案中涉及由结构式（I）表示的化合物，其药学上可接受的盐或前药，以及包含所述化合物或其药学上可接受的盐或前药的组合物。 还公开了使用结构式（I）和（Ia）化合物或包含结构式（I）和（Ia）化合物或其药学上可接受的盐或前药的组合物治疗缺血或缺血再灌注损伤的方法。

公开(公告)号：EP2542547A2

公开(公告)日：2013-01-09

申请号：EP11731488.0

申请日：2011-02-26

申请人： Krisani Biosciences (P) Ltd.

发明人： Kandula, Mahesh

IPC分类号： C07D339/04 ,  A61K31/385 ,  A61P1/16 ,  A61P35/00 ,  A61P25/16 ,  A61P25/28 ,  A61P39/04 ,  A61K31/27 ,  C07C323/59

CPC分类号： C07D339/04 ,  C07C323/59 ,  C07D417/12

摘要： A compound, composition, method of synthesizing and using the compound of formula 1 are disclosed. The compound of formula I also comprises of salts, polymorphs, solvates, and hydrates thereof. The compound may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for peroral, topical, transmucosal, inhalation, targeted delivery and sustained release formulations. Such compositions may be used to treat hepatic and genetic disorders related to copper overload. Multiple other compounds may be added with the instant claimed compounds and may be delivered as a pharmaceutical dose suitable for treating Wilson's disease.

摘要翻译： 合成和使用式1的化合物的化合物，组合物，方法是游离缺失光盘。 式I的化合物还包括盐，多晶型物，溶剂化物，和它们的水合物的。 所述化合物可以配制成药物组合物。 所述药物组合物可以配制经口，局部，透粘膜，吸入，靶向递送和持续释放配方蒸发散。 搜索的组合物可用于治疗与铜相关的超载肝脏和遗传性疾病。 多个其它化合物可以与本要求保护的化合物被加入，并且可以被递送作为适合于治疗威尔逊氏病的药物的剂量。

公开(公告)号：EP2364304A1

公开(公告)日：2011-09-14

申请号：EP09763890.2

申请日：2009-11-06

申请人： ISTITUTO BIOCHIMICO NAZIONALE SAVIO s.r.l.

发明人： BRUFANI, Mario ,  MEDICI, Ilaria ,  MARINI BETTOLO, Rinaldo ,  MIGNECO, Luisa Maria ,  MARZELLA, Rolando ,  FIGLIOLA, Rocco ,  LA BELLA, Angela

IPC分类号： C07D339/04 ,  A61K31/385 ,  A61K31/5377 ,  A61P3/00 ,  A61K31/4535 ,  A61K31/496 ,  A61P35/00

CPC分类号： C07D339/04 ,  A61K31/385 ,  A61K31/4535 ,  A61K31/496 ,  A61K31/5377

摘要： The present invention concerns an enantiomer R of a compound of Formula (I), wherein X is -NH-R
1 or of Formula (V) or (VI), R
1 is -(CH
2 )
n -R
2 , R
2 is a linear, branched or cyclic C
1 C
6 aliphatic group, -O-(CH
2 )
n -CH
3, -NH-CO- (CH
2 )
n -CH
3, a 5- or 6-membered aliphatic or aromatic ring optionally comprising a heteroatom, a 5- or 6-membered aromatic ring substituted by one or two substituents, said substituents being selected from the group consisting of -OH, - O(alkyl C
1 C
3 ) and -OCO(alkyl C
1 C
3 ), or of Formula (V), R
3 is H or a C
1 -C
3 aliphatic group and R
4 is a linear C
1 -C
3 or a branched C
3 -C
12 aliphatic group, or R
3 is a C
1 -C
3 aliphatic group and R
4 is a linear C
1 -C
12 aliphatic group, Y is O, CH-(CH
2 )
n -CH
3 or N(CO)(CH
2 )
n -CH
3, and n is an integer from O to 6. It has been found that the enantiomers of the invention are able to release (R)- alpha-lipoic acid, ensuring a longer permanence in the body for the pharmacologically active principle than that obtainable by its direct administration, or to simulate the pharmacological action of alpha-lipoic acid itself, while exhibiting a much more intense and lasting activity.

公开(公告)号：EP1423685B1

公开(公告)日：2011-08-24

申请号：EP02741130.5

申请日：2002-06-20

申请人： M.S. Tech Ltd.

发明人： DAYAN, Lev ,  DAYAGI, Yohai Y. ,  SHALOM, Moshe

IPC分类号： G01N27/00 ,  C07D339/04 ,  C07F5/02

CPC分类号： C07C323/60 ,  B82Y30/00 ,  B82Y35/00 ,  B82Y40/00 ,  C07D339/04 ,  C07F5/02 ,  G01G3/13 ,  G01N29/036 ,  G01N33/0057 ,  G01N2291/0256 ,  G01N2291/0257

摘要： A piezoelectric crystal element and a sensor utilizing the same are presented for use in a sensor device for identifying at least one foreign material from environment. The crystal element comprises at least one crystal resonator in the form of an inverted mesa structure, which has a membrane-like region and has a certain resonance frequency value. A surface region of the crystal resonator is modified by reactive molecules of a kind capable of interacting with the foreign material to yield a reaction product that effects a change in the resonance frequency of the crystal resonator from said certain resonance frequency value. This change is indicative of the identity and quantity of the foreign material.

公开(公告)号：EP1883645B1

公开(公告)日：2011-06-29

申请号：EP06721742.2

申请日：2006-03-31

申请人： Antibe Therapeutics Inc.

发明人： WALLACE, John L. ,  SPARATORE, Anna ,  CIRINO, Giuseppe ,  CALIENDO, Giuseppe ,  SANTAGADA, Vincenzo ,  FIORUCCI, Stefano

IPC分类号： C07F9/6578 ,  C07D339/04 ,  A61K31/16 ,  A61K31/27 ,  A61K31/255 ,  C07C333/02 ,  C07C327/40 ,  C07C321/14 ,  A61K31/325 ,  A61P1/00

CPC分类号： C07C327/42 ,  C07C323/12 ,  C07C323/59 ,  C07C323/60 ,  C07C327/48 ,  C07D339/04 ,  C07F9/6578 ,  C07F9/6587

摘要： The present invention provides new derivatives of 4-or 5-aminosalicylic acid, and a pharmaceutical composition containing these derivatives of 4-or 5-aminosalicylic acid as active ingredients, useful for the treatment of intestinal diseases such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS) and for the prevention/treatment of colon cancer. More particularly, these derivatives comprise a hydrogen sulfide releasing moiety linked via an azo, an ester, an anhydride, a thioester or an amide linkage to a molecule of 4-or 5-aminosalicylic acid. Furthermore, the present invention provides a process for preparing these compounds and their use for treating IBD and IBS and the prevention/treatment of colon cancer.

公开(公告)号：EP1731517B1

公开(公告)日：2010-11-17

申请号：EP05709791.7

申请日：2005-02-04

申请人： Japan Science and Technology Agency ,  National University Corporation Kagoshima University

发明人： SUDA, Yasuo ,  ARANO, Akio ,  KUSUMOTO, Shoichi ,  SOBEL, Michael ,  WAKAO, Masahiro

IPC分类号： C07D339/04 ,  C07H15/04 ,  G01N33/543

CPC分类号： C07H15/04 ,  C07D339/04 ,  G01N33/54353

摘要： A novel linker compound that minimizes any nonspecific hydrophobic interactions and is capable of easily regulating the length to disulfide group subjected to metal bond to thereby enable efficient formation of metal-sulfur bond; a novel ligand complex or ligand carrying substance; and a process for producing them. There is provided a linker compound comprising the structure of the general formula: (1) (wherein each of a, b, d and e independently is an integer of 0 to 6). The above X at a molecular end has an aromatic amino group and at its main chain has a structure of multi-branched structural site composed of 3 or more hydrocarbon-derived chains optionally having carbon-nitrogen bonds. The ligand complex consists of the above linker compound having a sugar molecule introduced therein.

公开(公告)号：EP2168567A1

公开(公告)日：2010-03-31

申请号：EP09164395.7

申请日：2009-07-02

申请人： L'Oréal

发明人： Marat, Xavier ,  Lucet-Levannier, Karine

IPC分类号： A61K8/49 ,  A61Q17/04 ,  C07D339/04 ,  A61Q19/08

CPC分类号： C07D339/04 ,  A61K8/4986 ,  A61K2800/522 ,  A61Q17/04 ,  A61Q19/08

摘要： La présente invention concerne l'utilisation cosmétique d'au moins un composé dithiolane choisi parmi ceux répondant à la formule (I), suivante

dans une composition comprenant un milieu physiologiquement acceptable, dans le but de renforcer et/ou de préserver la protection antioxydante naturelle de la peau face au stress oxydatif notamment causé par les radiations UV.

摘要翻译： 化妆品使用至少一种二硫化合物（I）或其盐，螯合物，溶剂化物或旋光异构体，在组合物中包含的介质，以加强和/或维护针对优选通过UV辐射引起的氧化应激面部皮肤的天然抗氧化防护的 ，声称。 美容用途式（I）或其盐，螯合物，中的至少一个二硫化合物的溶剂化物或光学异构体，在包括介质的组合物，以加强和/或保存的脸部皮肤的天然抗氧化保护，防止优选通过引起氧化应激 紫外线辐射，其特征在于。 Y 1> O，NR 1>或S; 或者，R 1> H，或饱和的直链或支链的1-2℃3-20C 2-20C烷基或不饱和烃基，或苯基被一个或多个OH任选取代和/或一个或多个1-8C烷氧基; 和R：H，或饱和的直链或支链的1-2℃3-20C 2-20C烷基或不饱和烃基，苯基，或1（由一个或多个OH和/或一个或多个烷氧基1-8C任选取代的）饱和的 -8C具有苯基取代基任选地被一个或多个OH和/或一个或多个烷氧基1-8C，其中R是任选被一个或多个取代基，其包含或2'，SR 2'，NR 2>，R 3> substituiertem取代 或COOR 2>; 或RR 1>（当Y 1>是NR 1>）：吡咯烷，吡咯啉，哌啶，哌嗪，（硫代）吗啉或氮杂; R 2> H，或饱和的直链或支链1-5C 3-5C或2-5C不饱和烃基，或苯基; ，R 3> R 2>或乙酰基; 且m，n：0-2。 独立权利要求中包括了：（1）二硫化合物，其中（I）不包括：4-甲基-1,2-二硫戊环-4-羧酸，4-甲基-1,2-二硫戊环-4-甲酰胺，4-甲基 -1,2-二硫戊环-4-羧酸甲酯，4-甲基-1,2-二硫戊环-4-羧酸乙酯，4-甲基-1,2-二硫戊环-4-羧酸正丙酯，4-甲基-1,2- 二硫戊环-4-羧酸苄基，N-甲基-4-甲基-1,2-二硫戊环-4-羧酸甲酯，和{[（4-甲基-1,2-二硫戊环-4-基）羰基]氨基}乙酸; 和（2）在培养基中，其包含（I）的组合物。 [图像] ACTIVITY：皮肤病。 作用机理：没有给出。

公开(公告)号：EP2046773A1

公开(公告)日：2009-04-15

申请号：EP07796141.5

申请日：2007-06-14

申请人： Indigene Pharmaceuticals Inc.

发明人： MYLARI, Banavara, L. ,  VAMAN RAO, Mary, E.

IPC分类号： C07D339/04 ,  A61K31/385

CPC分类号： C07D339/04

摘要： Described herein is a compound of Formula (I), which is the metformin salt of the naturally occurring endogenous biological compound, (R)-(+) α lipoic acid, pharmaceutical compositions containing the compound of Formula (I), and methods of treatment of diabetes or diabetic complications with the compound of Formula (I).

公开(公告)号：EP2024323A1

公开(公告)日：2009-02-18

申请号：EP07719924.8

申请日：2007-06-06

申请人： Antibe Therapeutics Inc.

发明人： WALLACE, John, L. ,  CIRINO, Giuseppe ,  SANTAGADA, Vincenzo ,  CALIENDO, Giuseppe

IPC分类号： C07C219/14 ,  A61K31/24 ,  A61P29/00 ,  C07C213/08 ,  C07C327/48 ,  C07D339/04

CPC分类号： C07C279/32 ,  C07C219/22 ,  C07C323/60 ,  C07C327/48 ,  C07D339/04

摘要： Unique salts of trimebutine and N-monodesmethyl trimebutine, and their corresponding stereoisomers, having improved analgesic properties useful in the treatment of visceral pain are provided. The salts of the present invention are particularly useful in the treatment of conditions characterized by abdominal pain, such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS), diabetic gastroparesis, and dyspepsia.

公开(公告)号：EP1968993A1

公开(公告)日：2008-09-17

申请号：EP06841375.6

申请日：2006-12-14

申请人： Pierre Fabre Dermo-Cosmétique

发明人： BORDAT, Pascal ,  TARROUX, Roger ,  SAURAT, Jean-Hilaire ,  SORG, Olivier ,  BRAYER, Jean-Louis ,  FRISON, Natacha

IPC分类号： C07H15/203 ,  C07H15/207 ,  C07D339/04 ,  C07C403/14 ,  C07C403/20 ,  A61K8/67 ,  A61Q19/02 ,  C07D311/72

CPC分类号： C07D339/04 ,  A61K8/33 ,  A61K8/37 ,  A61K8/4986 ,  A61K8/585 ,  A61K8/602 ,  A61Q19/02 ,  C07B2200/09 ,  C07C403/08 ,  C07C403/10 ,  C07C403/14 ,  C07C403/20 ,  C07C2601/16 ,  C07F7/0812 ,  C07F7/0818 ,  C07H15/203

摘要： The invention concerns novel polyunsaturated compounds of formula (I) wherein: R1 represents a R'1, -A-R'1 group, R'1 being selected from - COOH, -COOR3, -CONH2, -CONHR3, -CONR3 R4, -CHO, -CH2OH, -CH2OR5, and A represents a C2-C16 alkylene, alkenylene or alkynylene; R2 represents: an optionally substituted aryl group or an optionally substituted heteroaryl group; a sugar residue or, a fatty acid residue optionally branched and/or substituted preferably at the chain terminus and particularly by hydroxy, acetoxy radical or by an optionally protected amino radical; a -OC -(CH2)n CO-tocopheryl (alpha, beta or gamma or delta) group, with 2 ≤ n ≤ 10; a -R'2-O-R6 group, wherein R'2 is an optionally substituted arylene group or an optionally substituted heteroarylene group, and R6 represents a hydrogen atom, a straight or branched optionally substituted C1-C16 alkyl, a straight or branched optionally substituted C2-C16 alkenyl, or a straight or branched C2-C16 alkynyl group, an optionally substituted tocopheryl radical or the like, an amino acid residue, or a sugar residue. The invention also concerns the compositions, in particular cosmetic and/or dermatological compositions containing at least one compound of formula (I) as well as their use as whitening and/or depigmenting agent, and the cosmetic method using said compositions.

摘要翻译： 本发明涉及（I）worin式的新多不饱和化合物：R1 darstellt一个R'1，-AR'1基，R“1选自-COOH被选择，-COOR 3，-CONH 2，-CONHR 3，-CONR3 R4，-CHO ，-CH2OH，-CH2OR5，和A代表C2-C16亚烷基，亚烯基或亚炔基; R2 darstellt：在在OPTIONALLY substituiertem任选取代的芳基或杂芳基; 糖残基，或脂肪酸残基任选支化和/或substituiertem优选在链末端和特别被羟基，乙酰氧基或由可被保护的氨基烷基; 一个-OC - （CH 2）N CO生育酚（α，β或γ或δ）基团，其中2 $ M（F）N $ M（F）10; 一个-R'2-O-R 6基团，R'2 worin是亚芳基或在OPTIONALLY substituiertem任选取代的亚杂芳基，和R6表示氢原子，直链或支链的任选取代的C 1-C 16烷基，直 或支链的C2-C16链烯基substituiertem任选地，或直链或支链的C2-C16炔基，在OPTIONALLY substituiertem生育酚自由基等，在氨基酸残基，或糖残基。 因此本发明涉及所述组合物，特别是美容和/或含有式（I）的至少一种化合物皮肤病学组合物以及它们作为美白和/或脱色剂，以及使用所说的组合物化妆品方法中使用。