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1. 发明申请

WO2005051366A2 DIARYL UREA DERIVATIVES IN THE TREATMENT OF PROTEIN KINASE DEPENDENT DISEASES 审中-公开
标题翻译：治疗蛋白激酶依赖性疾病的二尿嘧啶衍生物
公开(公告)号：WO2005051366A2
公开(公告)日：2005-06-09
申请号：PCT/EP2004013459
申请日：2004-11-26
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BOLD GUIDO , CARAVATTI GIORGIO , FLOERSHEIMER ANDREAS , GUAGNANO VITO , IMBACH PATRICIA , MASUYA KEIICHI , ROESEL JOHANNES , VAUPEL ANDREA , GARCIA-ECHEVERRIA CARLOS
发明人： BOLD GUIDO , CARAVATTI GIORGIO , FLOERSHEIMER ANDREAS , GUAGNANO VITO , IMBACH PATRICIA , MASUYA KEIICHI , ROESEL JOHANNES , VAUPEL ANDREA , GARCIA-ECHEVERRIA CARLOS
IPC分类号： C07D239/34 , C07D239/46 , C07D401/12 , C07D403/12 , A61K31/00
CPC分类号： C04B35/632 , C07D239/34 , C07D239/47 , C07D401/12 , C07D403/12
摘要： The invention relates to the use of diaryl urea derivatives for the manufacture of pharmaceutical compositions for the treatment of RET dependent disorders, especially RET dependent tumor diseases. The invention further relates to novel N-[4-(pyrimidin-4-yloxy)-phenyl]-N'-phenyl-urea derivatives and their use in the treatment of the animal or human body, especially in the treatment of a protein kinase dependent disease, to pharmaceutical compositions comprising such novel N-[4-pyrimidin-4-yloxy)-phenyl]-N'-phenyl-urea derivatives and to the use of such novel N-[4-(pyrimidin-4-yloxy)-phenyl]-N'-phenyl-urea derivatives for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as tumour diseases.
摘要翻译：本发明涉及二芳基脲衍生物在制备用于治疗RET依赖性疾病，特别是RET依赖性肿瘤疾病的药物组合物中的用途。本发明还涉及新的N- [4-（嘧啶-4-基氧基） - 苯基] -N'-苯基 - 脲衍生物及其在治疗动物或人体中的用途，特别是在治疗蛋白激酶对于包含这样的新的N- [4-嘧啶-4-基氧基） - 苯基] -N'-苯基 - 脲衍生物的药物组合物和使用这种新的N- [4-（嘧啶-4-基氧基） - 苯基] -N'-苯基 - 脲衍生物，用于制备用于治疗蛋白激酶依赖性疾病，特别是增殖性疾病如肿瘤疾病的药物组合物。

2. 发明申请

WO2006059234A3 BICYCLIC AMIDES AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的双环酰胺
公开(公告)号：WO2006059234A3
公开(公告)日：2006-07-20
申请号：PCT/IB2005004030
申请日：2005-09-14
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BOLD GUIDO , CAPRARO HANS-GEORG , CARAVATTI GIORGIO , FLOERSHEIMER ANDREAS , FURET PASCAL , MANLEY PAUL W , VAUPEL ANDREA , PISSOT SOLDERMANN CAROLE , GESSIER FRANCOIS , SCHNELL CHRISTIAN , LITTLEWOOD-EVANS AMANDA JANE , KAPA PRASAD KOTESWARA , BAJWA JOGINDER S , JIANG XINGLONG
发明人： BOLD GUIDO , CAPRARO HANS-GEORG , CARAVATTI GIORGIO , FLOERSHEIMER ANDREAS , FURET PASCAL , MANLEY PAUL W , VAUPEL ANDREA , PISSOT SOLDERMANN CAROLE , GESSIER FRANCOIS , SCHNELL CHRISTIAN , LITTLEWOOD-EVANS AMANDA JANE , KAPA PRASAD KOTESWARA , BAJWA JOGINDER S , JIANG XINGLONG
IPC分类号： C07D403/12 , A61K31/505 , C07D239/46 , C07D413/12
CPC分类号： C07D239/47 , C07D403/12 , C07D413/12
摘要： The invention relates to compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases.
摘要翻译：本发明涉及式（I）化合物及其在治疗动物或人体中的用途，涉及包含式I化合物的药物组合物，以及涉及式I化合物在制备使用的药物组合物中的用途用于治疗蛋白激酶依赖性疾病，特别是增殖性疾病，例如特别是肿瘤疾病。

3. 发明申请

WO2004056832A3 EPOTHILONE DERIVATIVES 审中-公开
标题翻译：埃坡美龙衍生物
公开(公告)号：WO2004056832A3
公开(公告)日：2004-09-10
申请号：PCT/EP0314747
申请日：2003-12-22
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , DENNI-DISCHERT DONATIENNE , FLOERSHEIMER ANDREAS , KUESTERS ERNST , OBERER LUKAS , SEDELMEIER GOTTFRIED
发明人： DENNI-DISCHERT DONATIENNE , FLOERSHEIMER ANDREAS , KUESTERS ERNST , OBERER LUKAS , SEDELMEIER GOTTFRIED
IPC分类号： A61P35/00 , C07C59/215 , C07D417/06 , C07D493/04 , A61K31/427 , C07C59/90
CPC分类号： C07D417/06 , C07C59/215 , C07D493/04
摘要： The present invention relates to C4-demethyl-epothilones or C4-bisnor-epothilones of Formula (I), their pharmaceutical use, pharmaceutical composition containing the same and methods for their preparation.
摘要翻译：本发明涉及式（I）的C4-去甲基 - 埃坡霉素或C4-二去甲 - 埃坡霉素，它们的药物用途，含有其的药物组合物及其制备方法。

4. 发明申请

WO9727179A3 ANTIRETROVIRAL BASES 审中-公开
标题翻译：抗病毒基地
公开(公告)号：WO9727179A3
公开(公告)日：1997-12-31
申请号：PCT/EP9700139
申请日：1997-01-14
申请人： CIBA GEIGY AG , FREI JOERG , FAESSLER ALEXANDER , FLOERSHEIMER ANDREAS , HAMY FRANCOIS , KLIMKAIT THOMAS
发明人： FREI JOERG , FAESSLER ALEXANDER , FLOERSHEIMER ANDREAS , HAMY FRANCOIS , KLIMKAIT THOMAS
IPC分类号： A61K31/473 , C07D219/04 , C07D219/12 , C07D221/14 , C07D271/12 , C07D473/40 , A61K31/435
CPC分类号： C07D221/14 , A61K31/473 , C07D219/04 , C07D219/12 , C07D271/12 , C07D473/40
摘要： The invention relates to the use of a compound of formula (I), wherein R1 and R2 are independently amino, N-alkylamino, N,N-dialkylamino, cycloalkylamino, amidino, N-lower alkylamidino, N,N-di-lower alkylamidino, guanidino, N-lower alkylguanidino, N,N-di-lower alkylguanidino or (a); X and Y are independently selected from the group consisting of -(CH2)b-, (b), (c) and -(CH2)g-Cycloalkylen-(CH2)h-; Z is, independently of X and Y, -(CH2)b-, (d) or (e), wherein R is hydrogen or lower alkyl; Q is aryl, arylcarbonyl, arylaminocarbonyl, heterocyclyl, heterocyclylcarbonyl or heterocyclylaminocarbonyl, aryl or heterocyclyl whenever mentioned containing 2 or more annelated rings, a is 2 to 4, b is 2-7, c, d, e and f is 1 to 3, respectively, g and h is 0 to 3, respectively, i is 2 to 7 and k is 1 to 3, with the proviso that Q is arylcarbonyl, arylaminocarbonyl, heterocyclylcarbonyl or heterocyclylaminocarbonyl only if Z is a bivalent radical of formula (f) or (g); a tautomer thereof, or a salt thereof, as antiretroviral therapeutic (also for prophylaxis) inhibiting the interaction of transcriptional regulators with retroviral response elements.
摘要翻译：本发明涉及式（I）化合物的用途，其中R1和R2独立地为氨基，N-烷基氨基，N，N-二烷基氨基，环烷基氨基，脒基，N-低级烷基脒基，N，N-二低级烷基脒基，胍基，N-低级烷基胍基，N，N-二低级烷基胍基或（a）。 X和Y独立地选自 - （CH 2）b - ，（b），（c）和 - （CH 2）g - 亚环烷基 - （CH 2）h - Z独立于X和Y， - （CH2）b-，（d）或（e），其中R是氢或低级烷基; Q为芳基，芳基羰基，芳基氨基羰基，杂环基，杂环基羰基或杂环基氨基羰基，芳基或杂环基，每当含有2个或多个稠环时，a为2至4，b为2至7，c，d，e和f为1至3，只要Z是式（f）的二价基团，则g和h分别为0至3，i为2至7且k为1至3，条件是Q为芳基羰基，芳基氨基羰基，杂环基羰基或杂环基氨基羰基。（G）; 其互变异构体或其盐作为抗逆转录病毒治疗剂（也用于预防）抑制转录调节剂与逆转录病毒应答元件的相互作用。

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