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111. 发明公开

EP1788876A1 METHOD FOR MANUFACTURING IMIDAZOLE COMPOUNDS AND SALTS AND PSEUDOPOLYMORPHS THEREOF 有权转让
标题翻译：用于生产咪唑盐和假多
公开(公告)号：EP1788876A1
公开(公告)日：2007-05-30
申请号：EP05786030.6
申请日：2005-09-13
申请人： FERRER INTERNACIONAL, S.A.
发明人： PETSCHEN, Inés , CAMPS, Xavier , SALLARES, Juan
IPC分类号： A01N43/50 , A61K31/38 , A61K31/415 , C07D233/00 , C07D333/00
CPC分类号： A01N43/50 , C07D409/12
摘要： The invention relates to a method for manufacturinc sertaconazole mononitrate. The invention also relates tcsertaconazole mononitrate that is characterized by it: particle size and to sertaconazole mononitrate monohydrate.

112. 发明公开

EP1758655A2 TETRAHYDROPYRIDOTHIOPHENES FOR TREATING HYPERPROLIFERATIVE DISORDERS 审中-公开
标题翻译：四氢吡啶治疗疾病过度增生
公开(公告)号：EP1758655A2
公开(公告)日：2007-03-07
申请号：EP05752591.7
申请日：2005-06-10
申请人： Altana Pharma AG
发明人： PEKARI, Klaus , BAER, Thomas , SCHMIDT, Mathias , BECKERS, Thomas
IPC分类号： A61P35/00 , C07D495/04 , A61K31/4365 , C07D333/00 , C07D221/00
CPC分类号： C07D495/04 , A61K31/4365
摘要： The use of tetrahydropyridothiophenes of a certain formula (I), in which Ra and Rb have the meanings indicated in the description, is novel for treating hyperproliferative diseases and/or disorders responsive to the induction of apoptosis.

113. 发明授权

EP1603914B1 COMPOUNDS HAVING ACTIVITY AT 5HT2C RECEPTOR AND USES THEREOF 有权
标题翻译：用5-HT 2C受体的影响和使用链接
公开(公告)号：EP1603914B1
公开(公告)日：2007-01-17
申请号：EP04713892.0
申请日：2004-02-24
申请人： GLAXO GROUP LIMITED
发明人： HAMPRECHT, Dieter, GlaxoSmithKline , MICHELI, Fabrizio, GlaxoSmithKline
IPC分类号： C07D487/04 , C07D495/04 , A61K31/407 , A61P25/00 , C07D209/00 , C07D333/00
CPC分类号： C07D487/04 , C07D495/04
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein Q is phenyl or a 6-membered heteroaromatic group containing at least one nitrogen atom; A is -(CH2-CH2)-, -(CH=CH)-, -(CH2)3-, -C(CH3)2-, -(CH=CH-CH2)-, or a group -(CHR3)- wherein R3 is hydrogen, halogen, hydroxy, cyano, nitro, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy or C1-6alkylthio; B is O, S or NR11, wherein R11 is hydrogen, C1-6alkyl optionally substituted by C1-6alkoxy, or is C1-6alkanoyl optionally substituted by C1-6alkoxy; R1 is halogen, cyano, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, C1-6alkoxy, C1-6alkylthio, hydroxy, amino, mono- or di-C1- 6alkylamino, an N-linked 4 to 7 membered heterocyclic group, nitro, haloC1-6alkyl, haloC1-6alkoxy, aryl, arylC1-6alkyl, arylC1-6alkyloxy, arylC1-6alkylthio, COR4 (wherein R4 is amino, mono- or di-C1-6alkylamino or an N-linked 4 to 7 membered heterocyclic group), COOR5 or COR6 (wherein R5 and R6 are independently hydrogen or C1-6alkyl); p is 0, 1 or 2 or 3; R2 is hydrogen, halogen, hydroxy, cyano, nitro, C1-6alkyl, C1-6alkanoyl, C3-7cycloalkyl, C3-7cycloalkyloxy, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, C1-6alkylthio, amino, mono- or di-C1-6alkylamino or an N-linked 4 to 7 membered heterocyclic group; X is oxygen, sulfur, -CH2- or NR8 wherein R8 is hydrogen or C1-6alkyl; Y is a single bond, -CH2-, -(CH2)2- or -CH=CH-; and Z is an optionally substituted N-linked heterocyclic group or a C-linked 4 to 7 membered heterocyclic group containing at least one nitrogen, or Z is -NR9R10 where R9 and R10 are independently hydrogen or C1-6alkyl. Method of preparation and uses thereof in therapy, such as for example in treatment of depression and anxiety, are also disclosed.

114. 发明公开

EP1690854A1 Heterocyclic urea and related compounds useful as anti-inflammatory agents 审中-公开
标题翻译： Heterozyklischer Harnstoff und verwandte Verbindungen alsentzündungshemmendeMittel
公开(公告)号：EP1690854A1
公开(公告)日：2006-08-16
申请号：EP06114944.9
申请日：2000-02-16
申请人： Boehringer Ingelheim Pharmaceuticals, Inc.
发明人： Betageri, Rajashekhar , Breitfelder, Steffen , Cirillo, Pier Francesco , Gilmore, Thomas A. , Hickey, Eugene Richard , Kirrane, Thomas , Moriak, Monica Helen , Moss, Neil , Patel, Usha R. , Proudfoot, John R. , Regan, John Robinson , Sharma, Rajiv , Sun, Sanxing , Swinamer, Alan D. , Takahashi, Hidenori
IPC分类号： C07D231/38 , C07D213/38 , C07D213/74 , A61K31/44 , A61K31/50 , A61K31/415 , A61K31/505 , C07D401/14 , C07D405/12 , C07D401/12 , C07D213/76 , C07D409/12 , C07D493/08 , C07D495/08 , A61P29/00 , C07D307/00 , C07D209/00 , C07D333/00
CPC分类号： C07D231/40 , C07D213/38 , C07D213/64 , C07D213/74 , C07D213/75 , C07D231/12 , C07D307/12 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12
摘要： Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.
摘要翻译：公开了可用于治疗涉及炎症的疾病或病理状态的新型芳族化合物，例如慢性炎性疾病。还公开了含有制备这些化合物的药物组合物和方法。

115. 发明授权

EP1445259B1 Use of crystal forms of 2-methyl-thieno-benzodiazepine 失效
标题翻译：使用2-甲基 - 噻吩并苯并二氮杂的晶体形式
公开(公告)号：EP1445259B1
公开(公告)日：2006-06-28
申请号：EP03077455.8
申请日：1996-03-22
申请人： ELI LILLY AND COMPANY , ELI LILLY AND COMPANY LIMITED
发明人： Bunnell, Charles Arthur , Hendriksen, Barry Arnold , Larsen, Samuel Dean
IPC分类号： C07D495/04 , C07B63/00 , A61K31/55 , C07D333/00 , C07D243/00
CPC分类号： C07D495/04

116. 发明公开

EP1443041A4 5-AMIDINO-2-HYDROXYBENZENESULFONAMIDE DERIVATIVES, MEDICINAL COMPOSITIONS CONTAINING THE SAME, MEDICINAL USE THEREOF AND INTERMEDIATES IN THE PRODUCTION THEREOF 审中-公开
标题翻译： 5-脒基-2-羟基苯磺酰胺，MEDICAL COMPOSITIONS CONTAINING，医疗用途以及它们的生产的中间产品
公开(公告)号：EP1443041A4
公开(公告)日：2006-06-07
申请号：EP02777984
申请日：2002-10-29
申请人： KISSEI PHARMACEUTICAL
发明人： UCHIDA MASAHIKO , KOBAYASHI HIROAKI , KAI YUICHIRO , YOKOYAMA KENJI , TERAO YOSHIHIRO , MURANAKA HIDEYUKI
IPC分类号： A61K31/18 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/00 , A61P13/12 , A61P25/28 , A61P31/16 , C07C311/29 , C07D207/00 , C07D207/16 , C07D207/26 , C07D207/273 , C07D211/42 , C07D211/60 , C07D213/42 , C07D213/82 , C07D231/12 , C07D233/02 , C07D261/08 , C07D263/38 , C07D271/10 , C07D271/113 , C07D277/28 , C07D277/44 , C07D277/46 , C07D295/088 , C07D295/13 , C07D295/185 , C07D295/192 , C07D317/62 , C07D333/20 , C07C311/37 , A61K31/00 , C07D211/62 , C07D213/00 , C07D233/36 , C07D241/04 , C07D263/20 , C07D271/00 , C07D295/00 , C07D333/00
CPC分类号： C07D207/273 , A61K31/18 , C07C311/29 , C07D207/00 , C07D207/16 , C07D211/42 , C07D211/60 , C07D213/42 , C07D213/82 , C07D231/12 , C07D233/02 , C07D261/08 , C07D263/38 , C07D271/113 , C07D277/28 , C07D277/46 , C07D295/088 , C07D295/13 , C07D295/185 , C07D295/192 , C07D317/62 , C07D333/20
摘要： 5-Amidino-2-hydroxybenzenesulfonamide derivatives represented by the following general formula [I] exhibiting a potent and selective inhibitory activity on activated blood coagulation factor X and thus being useful as preventives or remedies for diseases in the onset of which activated blood coagulation factor X participates: [I] wherein R1 represents optionally substituted lower alkyl, optionally substituted lower alkoxy, optionally substituted alkenyl, cycloalkyl, lower acyl, etc.; Q represents hydrogen or optionally substituted lower alkyl; and Z represents hydrogen, hydroxy, etc.; pharmacologically acceptable salts thereof, medicinal compositions containing the same and intermediates in the production thereof. These compounds are useful as preventives or remedies for various diseases such as brain infarction, cerebral thrombosis, cerebral embolism, TIA, cerebral vascular jerk, Alzheimer’s diseases, myocardial infarction, heart attack, heart failure, thrombosis, pulmonary infarction and pulmonary embolism.

117. 发明公开

EP1622867A1 N-(2-PHENYLETHYL)SULFAMIDE DERIVATIVES AS INTEGRIN ALPHA4 ANTAGONISTS 有权
标题翻译： N-（2-苯基乙基）磺酰胺衍生物作为整联的α4拮抗剂
公开(公告)号：EP1622867A1
公开(公告)日：2006-02-08
申请号：EP04730833.3
申请日：2004-05-03
申请人： Almirall Prodesfarma, S.A.
发明人： JIMENEZ MAYORGA, Juan, Miguel , VIDAL GISPERT, Laura , WARRELLOW, Graham
IPC分类号： C07C307/06 , C07D213/81 , C07D295/26 , C07D333/20 , C07D409/12 , C07D471/04 , A61K31/16 , A61P37/00 , A61P29/00 , C07D333/00 , C07D221/00
CPC分类号： C07D213/81 , C07C307/06 , C07D295/26 , C07D333/20 , C07D409/12 , C07D471/04
摘要： Compounds of formula (I): wherein the various symbols are as defined and salts thereof are described as integrin α4-antagonists.

118. 发明公开

EP1575932A2 OKTUPOLARE MOLEKÜLE ALS ORGANISCHE HALBLEITER 审中-公开
标题翻译：八极分子有机半导体
公开(公告)号：EP1575932A2
公开(公告)日：2005-09-21
申请号：EP03766287.1
申请日：2003-07-24
申请人： Infineon Technologies AG
发明人： HALIK, Marcus , KLAUK, Hagen , SCHMID, Günter
IPC分类号： C07D333/00
CPC分类号： H01L51/0068 , C07D333/18 , C07D409/14 , H01L51/0067 , H01L51/0512 , H01L51/0541 , H01L51/0545
摘要： The invention relates to novel octupolar compounds and the production and use thereof as organic semi-condutors, particularly for organic field effect transistors.

119. 发明授权

EP1252133B1 PHARMACEUTICAL COMPOUNDS 有权
标题翻译：药物化合物
公开(公告)号：EP1252133B1
公开(公告)日：2005-06-08
申请号：EP00953102.1
申请日：2000-07-27
申请人： NicOx S.A.
发明人： DEL SOLDATO, Piero
IPC分类号： C07C219/14 , C07C219/30 , C07C229/42 , C07C233/25 , C07D219/10 , C07D295/08 , C07D309/30 , C07D401/12 , C07D471/04 , C07D495/04 , C07D499/68 , C07H15/252 , A61K31/21 , C07D495/00 , C07D333/00 , C07D213/00
CPC分类号： C07D295/088 , C07C203/04 , C07C219/22 , C07C219/24 , C07C229/42 , C07C233/25 , C07C317/44 , C07C2602/08 , C07D219/10 , C07D309/30 , C07D401/12 , C07D499/00 , C07F9/3873 , C07H15/252

120. 发明公开

EP0986384A4 INHIBITORS OF PROTEIN ISOPRENYL TRANSFERASES 失效
标题翻译： ISOPRENTRANSFERASE蛋白抑制剂
公开(公告)号：EP0986384A4
公开(公告)日：2004-09-15
申请号：EP98922122
申请日：1998-05-07
申请人： UNIV PITTSBURGH
发明人： SEBTI SAID M , HAMILTON ANDREW D , AUGERI DAVID J , BARR KENNETH J , DONNER BERNARD G , FAKHOURY STEPHEN A , JANOWICK DAVID A , KALVIN DOUGLAS M , LARSEN JOHN J , LIU GANG , O'CONNOR STEPHEN J , ROSENBERG SAUL H , SHEN WANG , SWENSON ROLF E , SORENSEN BRYAN K , SULLIVAN GERARD M , SZCZEPANKIEWICZ BRUCE G , TASKER ANDREW S , WASICK JAMES I
IPC分类号： C07D295/12 , A61K31/198 , A61K31/223 , A61K31/341 , A61K31/343 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/404 , A61K31/415 , A61K31/4152 , A61K31/4184 , A61K31/42 , A61K31/423 , A61K31/426 , A61K31/4402 , A61K31/4406 , A61K31/445 , A61K31/4453 , A61K31/4458 , A61K31/472 , A61K31/4965 , A61K31/4985 , A61K31/505 , A61K31/5375 , A61K31/7028 , A61P9/10 , A61P35/00 , A61P43/00 , C07C237/36 , C07C239/20 , C07C271/22 , C07C317/50 , C07C323/16 , C07C323/59 , C07C323/60 , C07C327/42 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/10 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/26 , C07D207/267 , C07D209/14 , C07D209/40 , C07D209/48 , C07D211/14 , C07D211/22 , C07D211/42 , C07D211/52 , C07D211/58 , C07D211/60 , C07D211/90 , C07D213/30 , C07D213/32 , C07D213/36 , C07D213/38 , C07D213/56 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/70 , C07D213/71 , C07D213/74 , C07D213/75 , C07D213/76 , C07D217/26 , C07D231/38 , C07D231/48 , C07D233/54 , C07D233/64 , C07D235/06 , C07D235/08 , C07D237/14 , C07D237/20 , C07D239/26 , C07D239/42 , C07D241/04 , C07D241/12 , C07D241/18 , C07D241/20 , C07D241/24 , C07D253/06 , C07D257/04 , C07D261/02 , C07D261/14 , C07D263/22 , C07D263/24 , C07D263/32 , C07D265/30 , C07D275/02 , C07D277/04 , C07D277/06 , C07D277/20 , C07D277/22 , C07D277/26 , C07D277/28 , C07D277/30 , C07D277/34 , C07D277/36 , C07D277/42 , C07D277/46 , C07D277/48 , C07D277/50 , C07D277/66 , C07D279/12 , C07D285/12 , C07D285/135 , C07D295/084 , C07D295/13 , C07D295/155 , C07D295/185 , C07D307/52 , C07D307/54 , C07D307/66 , C07D307/81 , C07D309/04 , C07D309/14 , C07D317/30 , C07D317/58 , C07D317/60 , C07D317/66 , C07D319/06 , C07D319/08 , C07D319/18 , C07D333/18 , C07D333/20 , C07D333/24 , C07D335/04 , C07D471/04 , C07D487/08 , C07F9/53 , C07H15/18 , A61K31/38 , A61K31/095 , A61K31/18 , A61K31/39 , A61K31/425 , A61K31/44 , A61K31/495 , C07C303/00 , C07C307/00 , C07C309/00 , C07C311/00 , C07D209/10 , C07D239/24 , C07D263/02 , C07D307/00 , C07D333/00
CPC分类号： C07D207/08 , C07B2200/07 , C07C237/36 , C07C239/20 , C07C271/22 , C07C317/50 , C07C323/59 , C07C323/60 , C07C327/42 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2602/08 , C07C2603/18 , C07C2603/24 , C07C2603/74 , C07D205/04 , C07D207/09 , C07D207/10 , C07D207/12 , C07D207/26 , C07D207/267 , C07D209/48 , C07D211/14 , C07D211/42 , C07D211/52 , C07D211/58 , C07D213/30 , C07D213/32 , C07D213/38 , C07D213/56 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/70 , C07D213/71 , C07D213/74 , C07D213/75 , C07D213/76 , C07D233/64 , C07D235/06 , C07D237/14 , C07D239/26 , C07D239/42 , C07D241/04 , C07D241/12 , C07D241/18 , C07D253/06 , C07D257/04 , C07D261/02 , C07D263/22 , C07D263/32 , C07D265/30 , C07D277/30 , C07D277/36 , C07D277/48 , C07D277/50 , C07D277/587 , C07D279/12 , C07D295/084 , C07D295/13 , C07D295/155 , C07D295/185 , C07D307/54 , C07D307/81 , C07D317/30 , C07D317/60 , C07D333/18 , C07D333/20 , C07D333/24 , C07D487/08 , C07F9/5333
摘要： Compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) lower alkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl -L2-, and (i) heterocyclic -L2-; R2 is selected from (a) formula (1), (b) -C(O)NH-CH(R14)-C(O)OR15, (c) formula (2), (d) -C(O)NH-CH(R14)-C(O)NHSO2R16, (e) -C(O)NH-CH(R14)-tetrazolyl, (f) -C(O)NH-heterocyclic, and (g) -C(O)NH-CH(R14)-C(O)NR17R18; R3 is substituted or unsubstituted heterocyclic or aryl, substituted or unsubstituted cycloalkyl or cycloalkenyl, formula (3), and -P(W)R?R3RR3'; R¿4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylalkyl, heterocyclic, or (heterocyclic)alkyl; L1 is absent or is selected from (a) -L4-N(R5)-L5-, (b) -L4-O-L5-, (c) -L4-S(O)n-L5-, (d) -L4-L6-C(W)-N(R5)-L5-, (e) -L4-L6-S(O)m-N(R5)-L5-, (f) -L4-N(R5)-C(W)-L7-L5-, (g) -L4-N(R5)-S(O)p-L7-L5-, (h) optionally substituted alkylene, (i) optionally substituted alkenylene, (j) optionally substituted alkynylene, (k) a covalent bond, (1) formula (4), and (m) formula (5) are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases.

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