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1. 发明申请

WO2006029850A1 HYDRAZONE DERIVATIVES AND THEIR USE AS BETA SECRETASE INHIBITORS 审中-公开
标题翻译：水解衍生物及其作为BETA秘密酶抑制剂的用途
公开(公告)号：WO2006029850A1
公开(公告)日：2006-03-23
申请号：PCT/EP2005/009902
申请日：2005-09-14
申请人： THE GENETICS COMPANY, INC. , SCHINDELHOLZ, Benno , SCHMID, Gerard , BRIGO, Alessandro , MILAS, Dragana , GARCIA, Gabriel
发明人： SCHINDELHOLZ, Benno , SCHMID, Gerard , BRIGO, Alessandro , MILAS, Dragana , GARCIA, Gabriel
IPC分类号： C07D213/00 , C07D233/00 , A61K31/15 , A61P25/00
CPC分类号： C07D213/53 , C07D209/08 , C07D213/65 , C07D213/77 , C07D215/12 , C07D215/26 , C07D233/54 , C07D239/42 , C07D239/48 , C07D285/01 , C07D307/56 , C07D403/04 , C07D409/04 , C07D417/12 , C07D473/34 , C07D495/04 , C07H19/167
摘要： The invention relates to compounds having the general formula (I) wherein R 3 is selected from the group consisting of H, methyl and hydroxyalkyl, and wherein Z 1 and Z 2 are selected independently from one another from the group consisting of substituted or unsubstituted phenyl, naphtyl, pyridinyl, pyrazolyl, pyramidinyl, pyrazidinyl, quinolinyl, iso-quinolinyl, coumarinyl, indolyl, thiazolyl and thiophenyl groups bearing substituents n R 1 and m R 2 , wherein R 1 and R 2 which may be the same or are different from one another are selected from the group consisting of H, alkyl, cycloalkyl, -C0 2 R 4 , -CONHR 4 , -CR 4 O, -SO 2 R 4 , -NR 4 -CO-R 4 , alkoxy, alkylthio, -OH, -O-aryl, -O-cycloalkyl, -S-aryl, -S-cycloalkyl, hydroxyalkyl, halogen, haloalkyl, haloalkoxy, -CN, -NO 2 , hydroxyal kylamine, aminoalkyl, alkylamine, aryl, heteroaryl and sulfonamide, wherein R 4 is selected from the group consisting of H, C 1 to C 6 branched or unbranched alkyl, aryl, cycloalkyl, alkoxy, heterocycloalkyl, -OH, -O-aryl, -O-alkyl, -O-cycloalkyl, aminoalkyl, alkylamine, aryl and heteroaryl, and wherein n and m are the numbers of the substituents R 1 and R 2 in Z 1 and Z 2 , respectively, which are in a range between 0 and 5, with the proviso that if n and m are integers higher than 2, R 1 and/or R 2 may form a fused aromatic or a carbocyclic or heterocyclic ring system, or a salt, or a physiologically functional derivative, or a prodrug thereof.
摘要翻译：本发明涉及具有通式（I）的化合物，其中R 1为低级烷基

2. 发明申请

WO2008071397A1 AROMATIC 1,4-DI-CARBOXYLAMIDES AND THEIR USE 审中-公开
标题翻译：芳香1,4-二羧酸酯及其用途
公开(公告)号：WO2008071397A1
公开(公告)日：2008-06-19
申请号：PCT/EP2007/010829
申请日：2007-12-11
申请人： THE GENETICS COMPANY INC. , GARCIA, Gabriel , DARAM, Pierre , FROESCH, Barbara , LEMAILLET, Guy , SCAPOZZA, Leonardo
发明人： GARCIA, Gabriel , DARAM, Pierre , FROESCH, Barbara , LEMAILLET, Guy , SCAPOZZA, Leonardo
IPC分类号： C07D233/96 , C07D401/14 , C07D407/12 , A61K31/444 , A61K31/505 , A61P35/00
CPC分类号： C07D401/14 , C07D233/96 , C07D407/12
摘要： The invention relates to novel compounds of formula (I) wherein X, Y, Z represent independently from one another C or N, n stands for 1, 2, 3, m is 0 or 1, p stands for 0 or an integer from 1 to 6, R 1 , R 2 represent independently from one another hydrogen, a halogen atom, a hydroxyl group, a C 1 -C 3 alkyl group and a C 1 -C 3 alkoxy group, R 3 represents, independently from one another if p is not 0, hydrogen, halogen, a C 1 -C 5 linear or branched alkyl, a carboxylyl, a carbomethoxyl, carboethoxyl, a benzyl, an acyl, a hydroxyl, a C 1 -C 4 linear or branched alkoxyl, a trifluoromethyl, a cyano, a morpholino, a 1,3-dioxolyl, an N-acetylamidyl or an amidoyl group, a saturated 5-8 membered ring, a heterocyclic ring, optionally substituted by a C 1 -C 3 alkyl, a hydroxyl or a benzyl group, a C 1 -C 6 alkylsulfonyl, a mono or disubstituted C 1 -C 5 alkyl group, a branched or a cyclic amine, R 6 is H or part of a alicyclic, heteroalicyclic ring system, if m is 0 then C represents CF 3 or a branched or unbranched C 1 -C 4 alkyl group, if m = 1 then C represents -CH 2 -O-, -CH 2 -, -CH 2 CH 2 -, -CH 2 CH 2 CH 2 -, -CH 2 (CH 2 )CH 2 - or denotes a chemical bond between N-C or C-C, the CONR 6 group may be linked to C either via its carbon or via its nitrogen atom, CYC stands for a by R 3 substituted or unsubstituted phenyl, pyridinyl, naphthyl, quinolinyl, isoquinolinyl, isoxaxolinyl, thiophenyl, 1,3,4-thiadiazazolidinyl, furanyl, tetrahydroquinolinyl, tetrahydroisoquinolinyl, morpholinyl, furanyl, cyclohexenyl, and chromen-2-on-yl and its use as a medicament for the treatment of cancer.
摘要翻译：本发明涉及新的式（I）化合物，其中X，Y，Z彼此独立地表示C或N，n表示1,2,3，m为0或1，p表示0或1的整数至6，R 1，R 2 2彼此独立地表示氢，卤素原子，羟基，C 1 -C 3烷基， C 1 -C 3烷基和C 1 -C 3烷氧基，R 3独立地表示如果p 不为0，氢，卤素，C 1 -C 5直链或支链烷基，羧基，甲酯基，碳乙氧基，苄基，酰基，羟基， C 1 -C 4直链或支链烷氧基，三氟甲基，氰基，吗啉代，1,3-二氧杂环戊烯基，N-乙酰基氨基或酰胺基，饱和的5-8元环，任选被C 1 -C 3烷基取代的杂环，羟基或苄基，C 1 C 1 -C 6烷基磺酰基，单或二取代的C 1 -C 6烷基磺酰基 1-C 5烷基，支链或环状胺，R 6是H或脂环族杂脂环系的一部分，如果m为0 那么C代表CF 3或支链或非支链C 1 -C 4烷基，如果m = 1，则C代表-CH _{2 -O - ， - CH 2 - ， - CH 2 CH 2 - ， - CH 2， CH 2，CH 2，CH 2，CH 2，CH 2，CH 2，CH 2，CH 2，CH 2，或者表示NC或CC之间的化学键，CONR 6个基团可以通过其碳或经由其氮原子与C连接，CYC代表R 3 吡啶基，萘基，喹啉基，异喹啉基，异恶唑啉基，噻吩基，1,3,4-噻二唑烷基，呋喃基，四氢喹啉基，四氢异喹啉基，吗啉基，呋喃基，环己烯基和色烯-2-酮基和其用作治疗癌症的药物。}

3. 发明申请

WO2008071398A1 SULFONAMIDES AND THEIR USE AS A MEDICAMENT 审中-公开
标题翻译：磺酰胺及其作为药物使用
公开(公告)号：WO2008071398A1
公开(公告)日：2008-06-19
申请号：PCT/EP2007/010830
申请日：2007-12-11
申请人： THE GENETICS COMPANY, INC. , GARCIA, Gabriel , DARAM, Pierre , FROESCH, Barbara , FRANK, Jaschinski , LEMAILLET, Guy , MARTY-ERNST, Cornelia , MARZI, Elena , SCAPOZZA, Leonardo
发明人： GARCIA, Gabriel , DARAM, Pierre , FROESCH, Barbara , FRANK, Jaschinski , LEMAILLET, Guy , MARTY-ERNST, Cornelia , MARZI, Elena , SCAPOZZA, Leonardo
IPC分类号： C07C311/37 , C07D211/26 , C07D231/12 , C07D295/08 , A61K31/18 , A61K31/415 , A61K31/435 , A61K31/535 , A61P35/00
CPC分类号： C07C311/38 , C07C311/21 , C07D207/335 , C07D209/40 , C07D213/24 , C07D213/53 , C07D215/12 , C07D217/12 , C07D231/12 , C07D233/64 , C07D271/12 , C07D295/096 , C07D295/135 , C07D295/155 , C07D333/58
摘要： The present invention relates to the use of a sulfonamide compound of formula (I): wherein R 1 is selected from the group consisting of H, CN, halogen, trifluoromethyl, methyl, ethyl, hydroxy, methoxy, ethoxy, morpholino, R 2 is selected from H, phenyl, substituted phenyl, CN, -SO 2 R, wherein R is phenyl or morpholino, -NC(O)Me, -NC(O)Et, - CH 2 C(O)OMe, CH 2 C(O)OEt, R 3 is selected from the group consisting of H, NO 2 , NH 2 , halogen, -COOMe, -COOEt, RC(O)N-, morpholino, R 4 is selected from the group consisting of H, a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, methoxy, ethoxy, propoxy, butoxy, a substituted or unsubstituted phenyl, alkinyl, Me 2 SO 2 -, COOR, wherein R is a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, - MeOC(O)-, a substituted or unsubstituted five or sixmembered aromatic or non-aromatic heterocyclic system with one, two or three heteroatoms, a hetaryl system, a condensed benzoheterocyclic system, X is a linker comprising 2 or 3 atoms, selected from the group consisting of -NH-NH-, -NH-NH-CH2-, ethinyl, -NH-C(O)-CH 2 -, - NH-NH-SO 2 -, -C(O)-NH-CH 2 -, -NH-N=CH-, -NH-N=C(Me)-, a -NH-N=CH- motif being part of a heterocyclic system, preferably a substituted or unsubstituted pyrazole or pyridazine system, and pharmaceutically active salts thereof. Further, the invention relates to the use of these compounds as a medicament, especially for the treatment of cancer.
摘要翻译：本发明涉及式（I）的磺酰胺化合物的用途：其中R 1选自H，CN，卤素，三氟甲基，甲基，乙基，羟基，甲氧基，乙氧基，吗啉代，R 2选自H，苯基，取代的苯基，CN，-SO 2 R，其中R是苯基或吗啉代，-NC（O）Me ，-NC（O）Et，-CH 2 C（O）OMe，CH 2 C（O）OEt，R 3选择由H，NO 2，NH 2，卤素，-COOMe，-COOEt，RC（O）N-，吗啉代，R 4，乙基，丙基，丁基，戊基，甲氧基，乙氧基，丙氧基，丁氧基，取代或未取代的苯基，炔基，Me 2 其中R是支链或非支链的甲基，乙基，丙基，丁基，戊基， - MeOC（O） - ，取代或未取代的五或六元芳香或非芳香族杂环系统与一，二或三 e杂原子，杂芳基系统，缩合苯并杂环系统，X是包含2或3个原子的连接体，其选自-NH-NH-，-NH-NH-CH 2 - ，乙炔基，-NH-C（O ）-CH 2 - ， - NH-NH-SO 2 - ， - C（O）-NH-CH 2 - ， - NH -N = CH-，-NH-N = C（Me） - ，作为杂环体系的一部分的-NH-N = CH-基序，优选取代或未取代的吡唑或哒嗪系统及其药学活性盐。此外，本发明涉及这些化合物作为药物，特别是用于治疗癌症的用途。

4. 发明申请

WO2004113302A1 N-SUBSTITUTED 6,8-DIALKOXY-1,2,3,4-TETRAHYDRO-1H-ISOQUINOLINE AS POTASSIUM CHANNELS MODULATORS 审中-公开
标题翻译： N-取代的6,8-二烷氧基-1,2,3,4-四氢-1H-异喹啉作为钾通道调节剂
公开(公告)号：WO2004113302A1
公开(公告)日：2004-12-29
申请号：PCT/EP2004/006552
申请日：2004-06-17
申请人： 4SC AG , GARCIA, Gabriel , SAEB, Wael , KRAMER, Bernd
发明人： GARCIA, Gabriel , SAEB, Wael , KRAMER, Bernd
IPC分类号： C07D217/06
CPC分类号： C07D217/06
摘要： The invention relates to compounds having the Formula (I) or a salt, or a physiologically functional derivative, or a prodrug thereof, (I) wherein Z is carbonyl or sulfonyl; R 1 is alkyl, alkenyl, alkynyl, aryl, H, halogen, haloalkyl, haloalkoxy, hydroxyalkyl, cycloalkyl or heteroaryl; R 2 is H, OH, -CH 2 -SO 2 -alkyl, -CH 2 -SO 2 -cycloalkyl, -CH 2 -SO 2 -aryl, -CH 2 -SO 2 -heteroaryl, alkylamine, alkenylamine, alkynylamine, cycloalkylamine, arylamine, heteroarylamine, aryl, haloalkyl, haloalkoxy, hydroxyalkyl, cycloalkyl, heteroaryl or a linear or branched alkyl, alkenyl, alkynyl, which can optionally be substituted by one or more substituentes R 3 ; R 3 is H, alkyl, alkenyl, alkynyl, cycloalkyl, -CO 2 R 4 , -CONHR 4 , -CONR 4 R 4 , - CR 4 O, SO 2 R 4 , -NR 4 -CO-R 4 , alkoxy, alkylthio, -OH, -SH, -O-aryl, -O-cycloalkyl, -S-aryl, -S-cycloalkyl, hydroxyalkyl, halogen, haloalkyl, haloalkoxy, CN, NO 2 , hydroxyalkylamine, aminoalkyl, alkylamine, aryl or heteroaryl; R 4 is H, halogen, alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, alkylthio, -O-aryl, - O-cycloalkyl, OH, SH, -S-aryl, -S-cycloalkyl, hydroxyalkyl, haloalkyl, haloalkoxy, hydroxyalkyl-amine, aminoalkyl, alkylamine, aryl or heteroaryl; R 5 is alkyl, alkenyl or alkynyl.
摘要翻译：本发明涉及具有式（I）的化合物或其盐或其生理功能衍生物或其前药，其中Z为羰基或磺酰基; R 1是烷基，烯基，炔基，芳基，H，卤素，卤代烷基，卤代烷氧基，羟基烷基，环烷基或杂芳基; R 2是H，OH，-CH 2 -SO 2 - 烷基，-CH 2 -SO 2 - 环烷基，-CH 2 -SO 2 - 芳基，-CH 2 -SO 2 - 杂芳基，烷基胺，链烯基胺，炔基胺，环烷基胺，芳基胺，杂芳基胺，芳基卤代烷基，卤代烷氧基，羟基烷基，环烷基，杂芳基或直链或支链烷基，烯基，炔基，其可任选被一个或多个取代基R 3取代; R 3是H，烷基，烯基，炔基，环烷基，-CO 2 R 4，-CONHR 4，-CONR 4 R 4，-CR 4，SO 2 R 4， NR 4 -CO-R 4，烷氧基，烷硫基，-OH，-SH，-O-芳基，-O-环烷基，-S-芳基，-S-环烷基，羟烷基，卤素，卤代烷基，卤代烷氧基， CN，NO 2，羟烷基胺，氨基烷基，烷基胺，芳基或杂芳基; R 4是H，卤素，烷基，烯基，炔基，环烷基，烷氧基，烷硫基，-O-芳基，-O-环烷基，OH，SH，-S-芳基，-S-环烷基，羟基烷基，卤代烷基，卤代烷氧基，羟基烷基 - 胺，氨基烷基，烷基胺，芳基或杂芳基; R 5是烷基，烯基或炔基。

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