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1. 发明申请

WO2005014517A3 NOVEL DIBENZO[B,F]OXEPINE-10-CARBOXAMIDES AND PHARMACEUTICAL USES THEREOF 审中-公开
标题翻译：新的DIBENZO [B，F] OXEPINE-10-CARBOXAMIDES及其药物用途
公开(公告)号：WO2005014517A3
公开(公告)日：2005-04-28
申请号：PCT/EP2004008283
申请日：2004-07-23
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , AUBERSON YVES , BETSCHART CLAUDIA , FLOHR STEFANIE , GLATTHAR RALF , SIMIC OLIVER , TINTELNOT-BLOMLEY MARINA , TROXLER THOMAS J , VANGREVELINGHE ERIC , VEENSTRA SIEM JACOB
发明人： AUBERSON YVES , BETSCHART CLAUDIA , FLOHR STEFANIE , GLATTHAR RALF , SIMIC OLIVER , TINTELNOT-BLOMLEY MARINA , TROXLER THOMAS J , VANGREVELINGHE ERIC , VEENSTRA SIEM JACOB
IPC分类号： C07C235/82 , C07D313/14 , C07D405/12 , C07D407/12 , C07D413/12 , C07D453/02 , C07D491/04 , C07C235/40 , A61K31/165 , A61K31/335 , A61K31/395 , A61P25/28 , C07D267/20
CPC分类号： C07D405/12 , C07C235/82 , C07C2603/32 , C07D313/14 , C07D407/12 , C07D413/12 , C07D453/02 , C07D491/04
摘要： The present invention pertains to compounds of formula (I) wherein X is O, NH, N(C1-4)alkyl, CO or CHOH, Y is CH or N, A and B are each hydrogen or together form a second bond between the carbon atoms to which they are attached, R1 is hydrogen or (C1-4)alkyl, R2 is optionally substituted (C1-8)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, aryl or heteroaryl, R3 is CH(Re)CONRaRb or (CH2)nNRc,Rd, n is 0, 1 or 2, Ra, Rb, Rc and Rd, independently, are hydrogen or optionally substituted (C1-8)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, (C7-9)bicycloalkyl, 1-aza-(C7-9)bicycloalkyl, aryl, aryl(C1-4)alkyl, heteroaryl, heteroaryl(C1-4)alkyl or heterocyclyl, or Ra, Rb, Rc and Rd, together with the nitrogen to which they are attached, form an optionally substituted pyrrolidinyl, piperidino, morpholino or piperazinyl group, Re is (C1-8)alkyl, (C1-4)alkoxy(C1-4)alkyl, (C3-7)cycloalkyl or (C3-7)cycloalkyl(C1-4)alkyl, and R4, R5, R6, R7, R8 and R9, independently, are hydrogen, (C1-4)alkyl, (C1-4)alkoxy, (C1-4)alkyl-SO2, cyano, nitro or halogen; to a process for the preparation of such compounds of formula (I), their use as a pharmaceuticals, especially in the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation, and to pharmaceutical compositions and combinations comprising such compounds of formula (I).
摘要翻译：本发明涉及式（I）的化合物，其中X是O，NH，N（C 1-4）烷基，CO或CHOH，Y是CH或N，A和B各自是氢或一起在（C 1-4）烷基，R 2是任选取代的（C 1-8）烷基，（C 3-7）环烷基，（C 3-7）环烷基（C 1-4）烷基，芳基或杂芳基，R 3为CH（R e）CONR a R b或（CH 2）n NR c，R d，n为0,1或2，R a，R b，R c和R d独立地为氢或任选取代的（C 1-8）（C 1-7）环烷基，（C 3-7）环烷基（C 1-4）烷基，（C 7-9）双环烷基，1-氮杂 - （C 7-9）双环烷基，芳基，（C 1-4）烷基或杂环基，或者R a，R b，R c和R d与它们所连接的氮一起形成任选取代的吡咯烷基，哌啶子基，吗啉代或哌嗪基，R e是（C 1-8）烷基，（C 1-4）烷基，（C 3-7）环烷基或（C 3-7）环烷基（C 1-4）烷基，且R 4，，（C1-4 ）烷基，（C 1-4）烷氧基，（C 1-4）烷基-SO 2，氰基，硝基或卤素; 涉及制备式（I）化合物的方法，其作为药物的用途，特别是用于治疗与β-淀粉状蛋白产生和/或聚集相关的神经和血管疾病，以及包含这些化合物的药物组合物和组合（I）的结构。

2. 发明专利

AT361300T 未知
公开(公告)号：AT361300T
公开(公告)日：2007-05-15
申请号：AT03790945
申请日：2003-08-29
申请人： NOVARTIS PHARMA GMBH
发明人： ALTMANN EVA , BETSCHART CLAUDIA , HAYAKAWA KENJI , IRIE OSAMU , SAKAKI JUNICHI , IWASAKI GENJI , LATTMANN RENE , MISSBACH MARTIN , TENO NAOKI
IPC分类号： C07D239/42 , C07D239/94 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D413/12 , C07D417/06 , C07D473/34 , C07D473/00
摘要： The invention provides compounds of formula I or a pharmaceutically acceptable salt or ester thereof wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use pharmaceutically for treatment of diseases and medical conditions in which cathepsin K is implicated, e.g. various disorders including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis and tumors.

3. 发明专利

PT1537111E DERIVADOS DE HETEROARIL-NITRILO. 未知
公开(公告)号：PT1537111E
公开(公告)日：2007-08-09
申请号：PT03790945
申请日：2003-08-29
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH
发明人： ALTMANN EVA , BETSCHART CLAUDIA , HAYAKAWA KENJI , IRIE OSAMU , SAKAKI JUNICHI , MISSBACH MARTIN , TENO NAOKI , WASAKI GENJII , LATTMANN RENE
IPC分类号： C07D473/00 , C07D239/42 , C07D239/94 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D413/12 , C07D417/06 , C07D473/34

4. 发明专利

AT326469T 未知
公开(公告)号：AT326469T
公开(公告)日：2006-06-15
申请号：AT02797553
申请日：2002-08-29
申请人： NOVARTIS PHARMA GMBH
发明人： BETSCHART CLAUDIA , HAYAKAWA KENJI , IRIE OSAMU , SAKAKI JUNICHI , IWASAKI GENJI , LATTMANN RENE , MISSBACH MARTIN , TENO NAOKI
IPC分类号： A61K31/519 , A61K31/5377 , A61K31/551 , A61P9/00 , A61P9/10 , A61P11/00 , A61P19/02 , A61P19/10 , A61P29/00 , A61P31/00 , A61P35/00 , A61P35/04 , A61P37/02 , A61P37/06 , A61P43/00 , C07D473/00 , C07D487/04 , C07D519/00 , A61K31/529 , A61K31/52
摘要： The invention provides compounds of Formula I or a pharmaceutically acceptable salt or ester thereof wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use pharmaceutically for treatment of diseases and medical conditions in which cathepsin K is implicated, e.g. various disorders including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis and tumors.

5. 发明专利

AT389642T 未知
公开(公告)号：AT389642T
公开(公告)日：2008-04-15
申请号：AT04740596
申请日：2004-07-02
申请人： NOVARTIS PHARMA GMBH
发明人： BETSCHART CLAUDIA , TINTELNOT-BLOMLEY MARINA
IPC分类号： C07D273/02 , A61K31/33 , A61P25/00 , C07D285/00 , C07D291/08
摘要： The present invention relates to macro-cyclic compounds of formula (I), wherein R 1 , is (C 1-8 )alkyl, (C 1-4 )alkoxy(C 1-4 )alkyl, hydroxy(C 1-6 )alkyl, (C 1-4 )alkylthio(C 1-4 )alkyl, (C 1-6 )alkenyl, (C 3-7 )cycloalkyl, (C 3-7 )cycloalkyl(C 1-4 )alkyl, piperidinyl or pyrrolidinyl, R 2 and R 4 , independently, are hydrogen or optionally substituted (C 1-8 )alkyl, (C 3-7 )cycloalkyl, (C 3-7 )cycloalkyl(C 1-4 )alkyl, aryl, aryl(C 1-4 )alkyl, heteroaryl or heteroaryl(C 1-4 )alkyl, or R 2 and R 4 , together with the nitrogen to which they are attached, form an optionally substituted piperidino, pyrrolidinyl, morpholino or piperazinyl group, R 3 is hydrogen or (C 1-4 )alkyl, X 1 is CH 2 , X 2 is CH 2 , O, S, CO, COO, OCO, NHCO, CONH, or NR, R being hydrogen or (C 1-4 )alkyl, Y is (C 1-8 )alkylen or (C 1-8 )alkylenoxy(C 1-6 )alkylen, (C 1-8 )alkenylen or (C 1-8 )alkenylenoxy(C 1-6 )alkylen, Ar is a phenyl ring optionally mono- di or trisubstituted by, independently, hydroxy or halogen, whereby X 1 , and X 2 are in meta or para position to each other, and either Z is CO, AA is a natural or unnatural alpha-amino-acid, and n is 0 or 1, or Z is S0 2 , AA is an optionally substituted ethylencarbonyl group (derived from a natural or unnatural alpha-amino acid by replacement of the nitrogen by a methylen group), and n is 1; processes for the preparation of these compounds; pharmaceutical compositions and combinations comprising the same; and their use in the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation.

6. 发明专利

AT479651T 未知
公开(公告)号：AT479651T
公开(公告)日：2010-09-15
申请号：AT98958887
申请日：1998-11-03
申请人： NOVARTIS PHARMA GMBH
发明人： ALTMANN EVA , BETSCHART CLAUDIA , GOHDA KEIGO , HORIUCHI MIYUKI , LATTMANN RENE , MISSBACH MARTIN , SAKAKI JUNICHI , TAKAI MICHIHIRO , TENO NAOKI , COWEN SCOTT , GREENSPAN PAUL , MCQUIRE LESLIE , TOMMASI RUBEN , VAN DUZER JOHN
IPC分类号： C07C255/29 , C07D249/04 , A61K31/275 , A61K31/33 , A61K31/341 , A61K31/343 , A61K31/352 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4155 , A61K31/4164 , A61K31/4192 , A61K31/426 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/443 , A61K31/4433 , A61K31/4453 , A61K31/451 , A61K31/47 , A61K31/495 , A61K31/4965 , A61K31/519 , A61K31/5375 , A61K38/00 , A61P9/10 , A61P19/02 , A61P19/10 , A61P29/00 , A61P35/00 , A61P35/04 , C07C255/44 , C07C271/22 , C07C317/44 , C07C323/52 , C07C323/62 , C07D207/32 , C07D207/327 , C07D207/416 , C07D209/08 , C07D209/18 , C07D209/42 , C07D211/06 , C07D211/14 , C07D213/56 , C07D213/64 , C07D213/81 , C07D213/82 , C07D215/48 , C07D231/14 , C07D233/54 , C07D233/64 , C07D241/44 , C07D249/06 , C07D277/20 , C07D277/56 , C07D295/092 , C07D295/14 , C07D295/15 , C07D295/155 , C07D295/18 , C07D307/54 , C07D307/68 , C07D307/79 , C07D307/84 , C07D307/85 , C07D317/68 , C07D333/24 , C07D333/40 , C07D333/48 , C07D403/12 , C07D405/12 , C07D409/12 , C07D487/04 , C07K5/06 , C07K5/062
摘要： N-terminal substituted dipeptide nitriles as defined are useful as inhibitors of cysteine cathepsins, e.g. cathepsins B, K, L and S, and can be used for the treatment of cysteine cathepsin dependent diseases and conditions, including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis, tumors (especially tumor invasion and tumor metastasis), coronary disease, atherosclerosis (including atherosclerotic plaque rupture and destabilization). Particular dipeptide nitriles are compounds of formula (I), or physiologically-acceptable and -cleavable esters or salts thereof, wherein: the symbols are as defined. In particular it has been found that by appropriate choice of groups R, R2, R3, R4, R5, X1, Y and L, the relative selectivity of the compounds as inhibitors of the various cysteine cathepsin types, e.g. cathepsins B, K, L and S, may be altered, e.g. to obtain inhibitors which selectively inhibit a particular cathepsin type or combination of cathepsin types.

7. 发明专利

AT430126T 未知
公开(公告)号：AT430126T
公开(公告)日：2009-05-15
申请号：AT04763454
申请日：2004-07-23
申请人： NOVARTIS PHARMA GMBH
发明人： AUBERSON YVES , BETSCHART CLAUDIA , FLOHR STEFANIE , GLATTHAR RALF , SIMIC OLIVER , TINTELNOT-BLOMLEY MARINA , TROXLER THOMAS , VANGREVELINGHE ERIC , VEENSTRA SIEM
IPC分类号： C07C235/40 , A61K31/165 , A61K31/335 , A61K31/395 , A61P25/28 , C07C235/82 , C07D267/20 , C07D313/14 , C07D405/12 , C07D407/12 , C07D413/12 , C07D453/02 , C07D491/04
摘要： The present invention pertains to novel dibenzo[b,f]oxepine-10-carboxamides compound to a process for the preparation of such compounds of formula I, their use as a pharmaceuticals, especially in the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation, and to pharmaceutical compositions and combinations comprising such compounds of formula I.

8. 发明专利

SI1423391T1 Pirolo pirimidini kot sredstva, ki inhibirajo cisteinske proteaze 未知
公开(公告)号：SI1423391T1
公开(公告)日：2006-10-31
申请号：SI200230374
申请日：2002-08-29
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH
发明人： BETSCHART CLAUDIA , HAYAKAWA KENJI , IRIE OSAMU , SAKAKI JUNICHI , IWASAKI GENJI , LATTMANN RENU , MISSBACH MARTIN , TENO NAOKI
IPC分类号： C07D487/00 , A61K31/00 , A61P29/00 , A61P35/00 , C07D473/00

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