公开(公告)号：EP1414835B1

公开(公告)日：2005-05-04

申请号：EP02700494.4

申请日：2002-02-27

申请人： PLIVA-ISTRAZIVACKI INSTITUT d.o.o.

发明人： KUJUNDZIC, Nedjeljko ,  BUKVIC KRAJACIC, Mirjana ,  DUMIC, Miljenko ,  HASENOHRL, Andrea

IPC分类号： C07H17/00 ,  A61K31/70 ,  A61P31/04

CPC分类号： C07H17/00

摘要： The invention relates to 9a-N[N'-(phenylsulfonyl)carbamoyl] derivatives of 9-deoxo-9-dihydro-9a-aza-homoerythromycin A and 5-O-desosaminyl-9-deoxo-9-dihydro-9a-aza-9a-homoerythronolide A, novel semisynthetic macrolide antibiotics from the class of azalides, of the general formula 1 wherein R denotes H, C1-C4alkyl or halogen and R denotes H or cladinosyl radical, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to intermediates and methods for their preparation, to a process for the preparation of pharmaceutical compositions as well as to the use of pharmaceutical compositions in the treatment of bacterial infections.

公开(公告)号：EP1524554A2

公开(公告)日：2005-04-20

申请号：EP04022238.2

申请日：2004-09-17

申请人： Shin-Etsu Chemical Co., Ltd.

发明人： Goto, Tomoyuki, c/o Sil. Denshi Zairyo Gijutsu ,  Tabei, Eiichi, c/o Sil. Denshi Zairyo Gijutsu ,  Yamamoto, Akira,c/o Sil. Denshi Zairyo Gijutsu

IPC分类号： G03F7/075

CPC分类号： G03F7/0757 ,  C08G77/12 ,  C08G77/16 ,  C08G77/18 ,  C08G77/20 ,  C08G77/70 ,  C08K5/54 ,  C08K5/5403 ,  C08K2201/014 ,  C08L83/04 ,  C08L83/00

摘要： A curable silicone resin composition is provided. It includes (A) an aromatic ring-containing hydrocarbon compound containing at least 2 silicon-bonded hydrogen atoms, in which the silicon atoms are bonded to the hydrocarbon skeleton; (B) an organopolysiloxane with a branched or three dimensional network structure, and with a viscosity at 25°C of at least 1,000 mPa·s, having an average composition formula (1):

        R 1 x SiO {(4-x)/2}      (I)

wherein, R 1 independently represent a substituted or unsubstituted monovalent hydrocarbon group, a substituted or unsubstituted hydrocarbyloxy group, or a hydroxyl group, provided from 0.1 to 80 mol% of all the R 1 groups are alkenyl groups, and x represents a positive number that satisfies 1 ≤ x

摘要翻译： 提供可固化的有机硅树脂组合物。 它包括（A）含有至少2个与硅键合的氢原子的含芳环的烃化合物，其中硅原子键合到烃骨架上; （B）具有支链或三维网状结构的有机聚硅氧烷，在25℃下的粘度为至少1000mPa·s，具有平均组成式（1）：€ƒ€ƒ€ƒ€ ƒ€ƒ€ƒR 1 x SiO {（4-x）/ 2}€ƒ€ƒ€ƒ（I）其中，R 1独立地表示取代或未取代的单价烃基，取代或未取代的烃氧基 基团或羟基，所有R 1基团为0.1〜80摩尔％为链烯基，x表示满足1‰×2的正数; 和（C）氢化硅烷化反应催化剂。 该组合物产生透明的固化产物并显示出优异的硬度和弯曲强度。

公开(公告)号：EP1514878A1

公开(公告)日：2005-03-16

申请号：EP04021021.3

申请日：2004-09-03

申请人： Shin-Etsu Chemical Co., Ltd.

发明人： Watanabe, Mikio,c/o Enbi-Kobunshi Zairyo Kenkyusho ,  Amano, Tadashi, c/o Enbi-Kobunshi Zairyo Kenkyusho

IPC分类号： C08F2/00

CPC分类号： C08F2/004 ,  C08F2/00 ,  C08F2/005

摘要： A polymer scale preventive agent for use in the polymerization of a monomer containing an ethylenic double bond is provided. The agent includes (A) a condensation reaction product obtained by reacting an aldehyde compound and a hydroxynaphthalene-based compound in the presence of a reducing agent, and (B) a polymer compound containing a nitrogen atom. This agent is capable of forming a coating with satisfactory scale prevention properties on inner wall surfaces of a polymerization vessel with a single-stage application, enabling the production process time to be shortened and the productivity and quality of polymeric products improved.

摘要翻译： 提供用于聚合含有烯属双键的单体的聚合物垢预防剂。 该试剂包括（A）在还原剂存在下使醛化合物与羟基萘系化合物反应而得到的缩合反应产物，和（B）含有氮原子的高分子化合物。 该试剂能够在单级施用的聚合反应器的内壁表面上形成具有令人满意的结垢防止性能的涂层，使生产过程时间缩短，聚合物产品的生产率和质量提高。

公开(公告)号：EP1509532A1

公开(公告)日：2005-03-02

申请号：EP03755235.3

申请日：2003-05-20

申请人： Pliva - Istrazivacki Institutd.o.o.

发明人： MERCEP, MLADEN ,  MESIC, Milan ,  MODRIC, Marina ,  PESIC, Dijana ,  KIDEMET, Davor

IPC分类号： C07D513/04 ,  A61K31/55 ,  A61P35/00

CPC分类号： C07D513/04

摘要： The present invention relates to derivatives of 1-thia-3-aza-dibenzoazulene class, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the inhibition of tumour necrosis factor-a (TNF-(x) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

公开(公告)号：EP1036083B9

公开(公告)日：2005-01-12

申请号：EP98946627.1

申请日：1998-10-13

申请人： Pliva - Istrazivacki Institut d.o.o.

发明人： KOBREHEL, Gabrijela ,  LAZAREVSKI, Gorjana ,  VINKOVIC, Mladen

IPC分类号： C07H17/08 ,  A61K31/70

CPC分类号： C07H17/08 ,  C07H17/00

公开(公告)号：EP1492797A1

公开(公告)日：2005-01-05

申请号：EP03745848.6

申请日：2003-04-09

申请人： PLIVA-ISTRAZIVACKI INSTITUT d.o.o.

发明人： MERCEP, Mladen ,  MESIC, Milan ,  PESIC, Dijana ,  BENKO, Iva

IPC分类号： C07D498/04 ,  A61K31/42

CPC分类号： C07D263/52 ,  Y02P20/55

摘要： The present invention relates to derivatives of 1-oxa-3-aza-dibenzoazulene class, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory actions, especially to the inhibition of tumour necrosis factor-α (TNF-α) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

公开(公告)号：EP1117643B1

公开(公告)日：2004-12-29

申请号：EP99949272.1

申请日：1999-10-01

申请人： Pliva, Farmaceutska, Industrija, Dionicko Drustvo

发明人： FILIC, Darko ,  DUMIC, Miljenko ,  DANILOVSKI, Aleksandar ,  KLEPIC, Bozena ,  FISTRIC, Ines ,  ORESIC, Marina ,  HORVAT MIKULCIC, Jasna

IPC分类号： C07D213/74

CPC分类号： A61K31/44 ,  C07D213/53 ,  C07D213/71 ,  C07D213/74

摘要： The present invention relates to the characterization of a new crystal modification III of torasemide, to a process for the preparation thereof by the use of controlled acidifying of alkaline solutions of torasemide with inorganic or organic acids with or without addition of a crystal seed, to its use as a raw material for the preparation of the crystal modification I of torasemide and of pharmaceutically acceptable salts of torasemide as well as to pharmaceutical forms containing this new crystal modification III of torasemide.

公开(公告)号：EP1437359A2

公开(公告)日：2004-07-14

申请号：EP04004844.9

申请日：1998-10-13

申请人： Pliva, Farmaceutska, Industrija, Dionicko Drustvo

发明人： Kobrehel, Gabrijela ,  Lazarevski, Gorjana ,  Vinkovic, Mladen

IPC分类号： C07H17/00 ,  A61K31/70 ,  A61P31/04

CPC分类号： C07H17/08 ,  C07H17/00

摘要： The invention relates to compounds of general formula (I) characterized in that R 1 individually stands for hydroxyl, L-cladinosyl group of formula (II) wherein R 2 individually stands for hydrogen or a silyl group; R 3 individually stands for hydrogen or together with R 6 stands for an ether group; R 4 individually stands for hydrogen, (C 1 -C 4 )acyl group or -COO-(CH 2 ) n -Ar group, wherein n is 1-7 and Ar individually stands for unsubstituted or substituted aryl group with up to 18 carbon atoms; R 5 individually stands for hydrogen, methyl group or -COO-(CH 2 ) n -Ar group, wherein n is 1-7 and Ar individually stands for unsubstituted or substituted aryl group with up to 18 carbon atoms; R 6 individually stands for a hydroxyl group or together with R 3 stands for an ether group; R 7 individually stands for hydrogen, (C 1 -C 12 )alkyl group, silyl group or together with R g and C-11/C-12 carbon atoms stands for a cyclic carbonate, R 8 individually stands for hydrogen, (C 1 -C 12 )alkyl group, silyl group or together with R 7 and C-11/C-12 carbon atoms stands for a cyclic carbonate; and its pharmaceutically acceptable additions salts with inorganic or organic acids, to a process for the preparation thereof and to the use thereof as antibiotics or as intermediates for the synthesis of other macrolide antibiotics.

摘要翻译： 新型大环内酯抗生素（I）包含9a-氮杂多苷的3,6-半缩酮。 式（I）的大环内酯类及其与无机或有机酸的加成盐是新的。 式（a）的R 1 OH或L-克立豆糖基; R2H或甲硅烷基; R3H; R 6 OH; 或R3 + R6醚基团; R4H，1-4C酰基或COO（CH2）nAr; n：1-7; Ar：任选取代至18 C芳基; R5H，Me或COO（CH2）nAr; R7，R8H，I2-C12烷基或甲硅烷基; 或R7 + R8环碳酸酯。 [图]还包括从阿奇霉素制备（I）的独立权利要求。 活性：抗菌。 12-O-甲基 - 阿奇霉素（Ia）对金黄色葡萄球菌ATCC 6538P，黄曲霉ATCC 12228，粪肠球菌ATCC 8043，枯草芽孢杆菌ATCC显示出0.25,0.12,0.25,1和0.5的MIC值（μg/ ml） 11778和大肠杆菌ATCC 10536。 阿奇霉素的相应值分别为（μg/ ml）：1,0.25,0.5,0.5和1。 行动机制：无给予。

公开(公告)号：EP1414835A2

公开(公告)日：2004-05-06

申请号：EP02700494.4

申请日：2002-02-27

申请人： PLIVA D.D.

发明人： KUJUNDZIC, Nedjeljko ,  BUKVIC KRAJACIC, Mirjana ,  DUMIC, Miljenko ,  HASENOHRL, Andrea

IPC分类号： C07H17/00 ,  A61K31/70 ,  A61P31/04

CPC分类号： C07H17/00

摘要： The invention relates to 9a-N[N'-(phenylsulfonyl)carbamoyl] derivatives of 9-deoxo-9-dihydro-9a-aza-homoerythromycin A and 5-O-desosaminyl-9-deoxo-9-dihydro-9a-aza-9a-homoerythronolide A, novel semisynthetic macrolide antibiotics from the class of azalides, of the general formula (I) wherein R1 denotes H, C1-C4alkyl or halogen and R denotes H or cladinosyl radical, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to intermediates and methods for their preparation, to a process for the preparation of pharmaceutical compositions as well as to the use of pharmaceutical compositions in the treatment of bacterial infections.

公开(公告)号：EP1404268A1

公开(公告)日：2004-04-07

申请号：EP02736866.1

申请日：2002-05-16

申请人： Regenerx Biopharmaceuticals, Inc.

发明人： GOLDSTEIN, Allan, L. ,  FINKELSTEIN, Jack, Jr.

IPC分类号： A61F13/00

CPC分类号： A61K38/2292 ,  A61K38/08 ,  A61K2039/505

摘要： Blister, sores or skin degradation associated with Epidermolysis Bullosa is treated or prevented by administration of a actin-sequestering peptide such as Thymosin β4, an isoform of Thymosin β4 or oxidized Thymosin β4.