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1. 发明申请

WO2006005486A1 SULFONAMIDE DERIVATIVES 审中-公开
标题翻译：磺酰胺衍生物
公开(公告)号：WO2006005486A1
公开(公告)日：2006-01-19
申请号：PCT/EP2005/007268
申请日：2005-07-06
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , KITAS, Eric, Argirios , JAKOB-ROETNE, Roland
发明人： GALLEY, Guido , KITAS, Eric, Argirios , JAKOB-ROETNE, Roland
IPC分类号： C07D223/08
CPC分类号： C07D223/12 , C07D403/12
摘要： The invention relates to compounds of the general formula (I), wherein R 1 -R 5 and R 2’ -R 4’ are as described in the claims and to pharmaceutically suitable acid additon salts, optical pure enantiomers, racemates or diastereomeric mixtures thereof for the treatment of Alzheimer’s disease or common cancers.
摘要翻译：本发明涉及通式（I）的化合物，其中R

2. 发明申请

WO2005040126A1 SUBSTITUTED DIBENZO-AZEPINE AND BENZO-DIAZEPINE DERIVATIVES USEFUL AS GAMMA-SECRETASE INHIBITORS 审中-公开
标题翻译：用作GAMMA-分泌酶抑制剂的替代二苯并嗪和苯并二氮吡啶衍生物
公开(公告)号：WO2005040126A1
公开(公告)日：2005-05-06
申请号：PCT/EP2004/010821
申请日：2004-09-27
申请人： F. HOFFMAN-LA ROCHE AG , FLOHR, Alexander , GALLEY, Guido , JAKOB-ROETNE, Roland , KITAS, Eric, Argirios , PETERS, Jens-Uwe , WOSTL, Wolfgang
发明人： FLOHR, Alexander , GALLEY, Guido , JAKOB-ROETNE, Roland , KITAS, Eric, Argirios , PETERS, Jens-Uwe , WOSTL, Wolfgang
IPC分类号： C07D223/18
CPC分类号： C07D409/12 , C07D223/16 , C07D223/18 , C07D243/12 , C07D243/24
摘要： The present invention relates to compounds of the general formula (I) Wherein R 1 is -(CHR’) q -aryl or -(CHR') q -heteroaryl, which are unsubstituted or mono, di- or tri-substituted by lower alkyl, lower alkoxy, CF 3 or halogen, or is lower alkyl, lower alkenyl, -(CH 2 ) n -Si(CH 3 ) 3 , -(CH 2 ) n -O-lower alkyl, -(CH 2 )n-S-lower alkyl, -(CH 2 ) q -cycloalkyl, -(CH 2 ) n -[CH(OH)] m -(CF 2 )p-CH q F( 3-q) , or is -(CH 2 )n-CR 2 -CF 3 , wherein the two R radicals form together with the carbon atom a cycloalkyl ring; R' is hydrogen or lower alkyl; n is 1, 2 or 3; in is 0 or 1; p is 0, 1, 2, 3, 4, 5 or 6; q is 0, 1, 2 or 3; R 2 is hydrogen or lower alkyl; R 3 is hydrogen, lower alkyl, -CH 2 CF 2 CF 3 , CH 2 CF 3 , (CH 2 ) 2 CF 3 , CF 3 , CHF 2 , CF 3 , CHF 2 , CH 2 F, or is aryl, optionally mono, di or tri-substituted by halogen, or is (CH 2 ) n NR 5 R 6 , wherein R 5 and R 6 are independently from each other hydrogen or lower alkyl; R 4 is one of the following groups wherein R 7 is hydrogen, lower akl, -(CH 2 ) n -CF 3 or -(CH 2 ) n -cycloalkyl; R 8 is hydrogen, lower alkyl, -C(O)-phenyl, -C(O)-lower alkyl, -C(O)O-(CH 2 ) n - cycloalkyl, -C(O)O-(CH 2 ) n -lower alkyl, -C(O)NH-(CH 2 ) n -lower alkyl or -C(O)NH(CH 2 ).-CyClOalkYl; R 9 is hydrogen, lower alkyl, -(CH 2 ) n -cycloalkyl or -(CH 2 ) n -CF 3 ; and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racernates or diastereomeric mixtures thereof for the treatment of Alzheimer's disease..
摘要翻译：本发明涉及通式（I）的化合物，其中R 1是 - （CHR'）q-芳基或 - （CHR'）q-杂芳基，它们是未被取代的或被一个或二个或三个被低级烷基，低级烷氧基，CF 3或卤素，或低级烷基，低级烯基， - （CH 2）n -Si（CH 3）3 - ，（CH 2）n O-低级烷基， - （CH 2） CH 2）q - 环烷基， - （CH 2）n - [CH（OH）] m - （CF 2）p-CHFF（3-q）或 - 是（CH 2）n CR 2 CF 3，与碳原子一起为环烷基环; R'是氢或低级烷基; n为1,2或3; in是0或1; p是0，1，2，3，4，5或6; q为0,1,2或3; R 2是氢或低级烷基; R 3是氢，低级烷基，-CH 2 CF 2 CF 3，CH 2 CF 3，（CH 2）2 CF 3，CF 3，CHF 2，CF 3，CHF 2，CH 2 F，或者是芳基，任选地单，二或被卤素三取代，或是（CH 2）n NR 5 R 6，其中R 5和R 6彼此独立地是氢或低级烷基; R 4是下列基团之一，其中R 7是氢，低级ak， - （CH 2）n -CF 3或 - （CH 2）n - 环烷基; R8是氢，低级烷基，-C（O） - 苯基，-C（O） - 低级烷基，-C（O）O-（CH2）n-环烷基，-C（O）O-（CH2）低级烷基，-C（O）NH-（CH 2）n - 低级烷基或-C（O）NH（CH 2） R 9是氢，低级烷基， - （CH 2）n - 环烷基或 - （CH 2）n -CF 3; 以及用于治疗阿尔茨海默氏病的药学上合适的酸加成盐，光学纯对映异构体，ernernate或非对映体混合物。

3. 发明申请

WO2005023772A1 MALONAMIDE DERIVATIVES BLOCKING THE ACTIVITY OF GAMA-SECRETASE 审中-公开
标题翻译：马洛酮衍生物阻断游离氨基酸酶的活性
公开(公告)号：WO2005023772A1
公开(公告)日：2005-03-17
申请号：PCT/EP2004/009700
申请日：2004-08-31
申请人： F. HOFFMANN-LA ROCHE AG , FLOHR, Alexander , GALLEY, Guido , JAKOB-ROETNE, Roland , KITAS, Eric, Argirios , PETERS, Jens-Uwe , WOSTL, Wolfgang
发明人： FLOHR, Alexander , GALLEY, Guido , JAKOB-ROETNE, Roland , KITAS, Eric, Argirios , PETERS, Jens-Uwe , WOSTL, Wolfgang
IPC分类号： C07D223/18
CPC分类号： C07D223/16 , A61K31/335 , A61K31/55 , A61K31/5513 , C07D223/20 , C07D243/24 , C07D273/00 , C07D313/14
摘要： The invention relates to malonamide derivatives of formula (I), wherein: R 1 is one of the following groups (Formulae a), b), c), d)); R 2 is lower alkyl, lower alkinyl, -(CH 2 ) n -O-lower alkyl, -(CH 2 ) n -S-lower alkyl, -(CH 2 ) n -CN, -(CR'R") n -CF 3 , -(CR'R") n -CHF 2 , -(CR'R") n -CH 2 F, -(CH 2 ) n -C(O)O-lower alkyl, -(CH 2 ) n -halogen, or is -(CH 2 ) n -cycloalkyl, optionally substituted by one or more substituents, selected from the group consisting of phenyl, halogen or CF 3 ; R',R" are independently from n and from each other hydrogen, lower alkyl, lower alkoxy, halogen or hydroxy; R 3 , R 4 are independently from each other hydrogen, lower alkyl, lower alkoxy, phenyl or halogen; R 5 is hydrogen, lower alkyl, -(CH 2 ) n -CF 3 or -(CH 2 ) n -cycloalkyl; R 6 is hydrogen or halogen; R 7 is hydrogen or lower alkyl; R 8 is hydrogen, lower alkyl, lower alkinyl, -(CH 2 ) n -CF 3 ,-(CH 2 ) n -cycloalkyl or -(CH 2 ) n -phenyl, optionally substituted by halogen; R 9 is hydrogen, lower alkyl, -C(O)H, -C(O)-lower alkyl, -C(O)-CF 3 ,-C(O)-CH 2 F,-C(O)-CHF 2 ,-C(O)-cycloalkyl,-C(O)-(CH 2 ) n -O-lower alkyl,-C(O)O-(CH 2 ) n -cycloalkyl, -C(O)-phenyl, optionally substituted by one or more substituents selected from the group consisting of halogen or -C(O)O-lower alkyl, or is -S(O) 2 -lower alkyl, -S(O) 2 -CF 3 ,-(CH 2 ) n -cycloalkyl or is -(CH 2 ) n -phenyl, optionally substituted by halogen; n is 0, 1, 2, 3 or 4; and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixture thereof. These compounds may be used for the treatment of Alzheimer’s disease.
摘要翻译：本发明涉及式（I）的丙二酰胺衍生物，其中：R 1是以下基团之一（式a），b），c），d））; R 2是低级烷基，低级炔基， - （CH 2）n O-低级烷基， - （CH 2）n S-低级烷基， - （CH 2）n -CN， - （CR'R“ CR'R“）n-CHF 2， - （CR'R”）n -CH 2 F， - （CH 2）n C（O）O-低级烷基， - （CH 2）n-卤素，或是 - （CH 2）任选被一个或多个选自苯基，卤素或CF 3的取代基取代; R'，R“独立地为n和彼此独立地为氢，低级烷基，低级烷氧基，卤素或羟基; R 3，R 4彼此独立地为氢，低级烷基，低级烷氧基，苯基或卤素; R 5是氢，低级烷基， - （CH 2）n -CF 3或 - （CH 2）n - 环烷基; R 6是氢或卤素; R 7是氢或低级烷基; R 8是任选被卤素取代的氢，低级烷基，低级炔基， - （CH 2）n -CF 3， - （CH 2）n - 环烷基或 - （CH 2） R 9是氢，低级烷基，-C（O）H，-C（O） - 低级烷基，-C（O）-CF 3，-C（O）-CH 2 F，-C（O） -C（O） - 环烷基，-C（O） - （CH 2）n O-低级烷基，-C（O）O-（CH 2）n - 环烷基，-C（O） - 苯基，任选被一个或多个或选自卤素或-C（O）O-低级烷基，或者是-S（O）2 - 低级烷基，-S（O）2-CF 3， - （CH 2）n - （CH 2）n - 苯基，任选被卤素取代; n为0,1,2,3或4; 和药学上合适的酸加成盐，旋光纯对映异构体，外消旋体或非对映体混合物。这些化合物可用于治疗阿尔茨海默病。

4. 发明申请

WO2007020190A1 FLUORO SUBSTITUTED 2-OXO AZEPAN DERIVATIVES 审中-公开
标题翻译：氟替代2-OXO AZEPAN衍生物
公开(公告)号：WO2007020190A1
公开(公告)日：2007-02-22
申请号：PCT/EP2006/064935
申请日：2006-08-02
申请人： F. HOFFMANN-LA ROCHE AG , FLOHR, Alexander , GALLEY, Guido , JAKOB-ROETNE, Roland , KITAS, Eric Argirios , WOSTL, Wolfgang
发明人： FLOHR, Alexander , GALLEY, Guido , JAKOB-ROETNE, Roland , KITAS, Eric Argirios , WOSTL, Wolfgang
IPC分类号： C07D223/12 , C07D413/12 , C07D401/12 , C07D403/12 , C07D409/14 , A61K31/55 , A61P25/28 , A61P35/00
CPC分类号： C07D409/14 , C07D223/12 , C07D401/12 , C07D403/12 , C07D413/12
摘要： The invention relates to compounds of general formula (I), wherein R 1 is lower alkyl substituted by halogen, or is aryl or heteroaryl, unsubstituted or substituted by halogen; R 2 is heterocycloalkyl, aryl or heteroaryl, which are unsubstituted or substituted by one or more substituents, selected from the group consisting of halogen, lower alkyloxy, lower alkyl substituted by halogen, O-lower alkyl substituted by halogen or are substituted by C(O)-NR" 2 , (CR 2 )m-C(O)-R’ heteroaryl or S(O) 2 -lower alkyl; R 3 /R 3’ , R 4 /R 4’ and R 5 /R5’ are independently from each other hydrogen or fluoro, wherein at least one of R4/R4’ or R 5 /R 5’ is always fluoro; R' is aryl or hydroxy; R" is hydrogen, cycloalkyl or is heterocycloalkyl; R is hydrogen or lower alkyl; m is 0, 1, 2 or 3; and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. It has been found that the compounds of general formula (I) are γ-secretase inhibitors and the related compounds may be useful in the treatment of Alzheimer's disease or common cancers including but not limited to cervical carcinomas and breast carcinomas and malignancies of the hematopoietic system.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1为被卤素取代的低级烷基，或未取代或被卤素取代的芳基或杂芳基; R 2是未取代的或被一个或多个选自以下的取代基取代的杂环烷基，芳基或杂芳基：卤素，低级烷氧基，被卤素取代的低级烷基，被卤素或被C（O）-NR“2取代，（CR 2）m C（O）-R'杂芳基或S（O） /低级烷基; R 3，R 3，R 3，R 4，R 4，R 4， R 5 / R 5'或R 5'或R 5'中的至少一个独立地为氢或氟，其中R 4 / R 4'或R 5' 总是氟; R'是芳基或羟基; R“是氢，环烷基或杂环烷基; R是氢或低级烷基; m为0,1,2或3; 以及药学上合适的酸加成盐，旋光纯对映异构体，外消旋体或非对映体混合物。已经发现通式（I）的化合物是γ-分泌酶抑制剂，相关化合物可用于治疗阿尔茨海默病或常见癌症，包括但不限于宫颈癌和乳腺癌以及造血系统的恶性肿瘤。

5. 发明申请

WO9951629A2 NEW COMPOUNDS FOR DNA-TRANSFECTION 审中-公开
标题翻译：用于DNA转染的新化合物
公开(公告)号：WO9951629A2
公开(公告)日：1999-10-14
申请号：PCT/EP9902361
申请日：1999-04-07
申请人： ROCHE DIAGNOSTICS GMBH , KITAS ERIC ARGIRIOS , SCHLAEGER ERNST JUERGEN
发明人： KITAS ERIC ARGIRIOS , SCHLAEGER ERNST-JUERGEN
IPC分类号： A61K9/127 , A61K47/48 , A61K48/00 , C07K14/00 , C07K14/435 , C12N15/09 , C12N15/88
CPC分类号： C12N15/88
摘要： The invention relates to conjugates of lipids and basic, modified membrane disturbing peptides, characterized in that the peptides comprises a reversed amide backbone, particularly compounds of formula (I), wherein R and R are a hydrocarbyl moiety of a straight-chain or branched-chain, saturated or unsaturated aliphatic carboxylic acid or a phospholipid moiety, R is a basic, modified membrane disturbing peptide with a reversed amide backbone, Y is C2-10 alkylene, X is -C(O)-NH- or -S-S-, and salts thereof.
摘要翻译：本发明涉及脂质和碱性修饰的膜扰动肽的缀合物，其特征在于所述肽包含反向酰胺骨架，特别是式（I）的化合物，其中R 1和R 2是烃基的烃基部分直链或支链，饱和或不饱和的脂族羧酸或磷脂部分，R 3是具有相反酰胺骨架的碱性修饰的膜修饰肽，Y是C 2-10亚烷基，X是-C（O ）-NH-或-SS-及其盐。

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