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1. 发明申请

WO2020110011A1 CYCLIC PEPTIDES AS PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9) INHIBITORS FOR THE TREATMENT OF METABOLIC DISORDERS 审中-公开
公开(公告)号：WO2020110011A1
公开(公告)日：2020-06-04
申请号：PCT/IB2019/060203
申请日：2019-11-26
申请人： NOVARTIS AG
发明人： FLYER, Alec Nathanson , GOLOSOV, Andrei Alexandrovich , GROSCHE, Philipp , LEWIS, Ian , LIU, Eugene Yuejin , MARZINZIK, Andreas , MONOVICH, Lauren Gilchrist , OTTL, Johannes , PATEL, Tajesh Jayprakash , REID, Patrick Crawford , SEEPERSAUD, Mohindra
IPC分类号： C07K7/08 , A61K38/00
摘要： The disclosure relates to inhibitors of PCSK9 useful in the treatment of lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, or tautomer thereof, wherein R 1 , X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , X 8 , X 9 , X 10 , X 11 , X 12 , and X 13 are described herein.

2. 发明申请

WO2009068682A2 PHENYL-OXETANYL-DERIVATIVES 审中-公开
标题翻译：苯基氧杂环衍生物
公开(公告)号：WO2009068682A2
公开(公告)日：2009-06-04
申请号：PCT/EP2008/066517
申请日：2008-12-01
申请人： NOVARTIS AG , ALBERT, Rainer , COOKE, Nigel Graham , ZECRI, Frédéric , LEWIS, Ian
发明人： ALBERT, Rainer , COOKE, Nigel Graham , ZECRI, Frédéric , LEWIS, Ian
IPC分类号： C07D305/08 , C07D305/10 , C07D413/10 , A61K31/4245 , A61K31/337 , A61P37/02 , A61P37/06
CPC分类号： C07D413/10 , C07D305/08 , C07D305/10
摘要： Novel organic compounds are described and claimed which may in particular be useful in the treatment of diseases being triggered by the (human) autoimmune system.
摘要翻译：描述和要求保护的新型有机化合物，其特别可用于治疗由（人）自身免疫系统触发的疾病。

3. 发明申请

WO2013088404A1 Use of inhibitors of the activity or function of PI3K 审中-公开
标题翻译：使用PI3K活性或功能的抑制剂
公开(公告)号：WO2013088404A1
公开(公告)日：2013-06-20
申请号：PCT/IB2012/057332
申请日：2012-12-14
申请人： NOVARTIS AG
发明人： COOKE, Nigel Graham , FERNANDES GOMES DOS SANTOS, Paulo Antonio , FURET, Pascal , HEBACH, Christina , HÖGENAUER, Klemens , HOLLINGWORTH, Gregory , KALIS, Christoph , LEWIS, Ian , SMITH, Alexander Baxter , SOLDERMANN, Nicolas , STAUFFER, Frédéric , STRANG, Ross , STOWASSER, Frank , TUFILLI, Nicola , VON MATT, Anette , WOLF, Romain , ZECRI, Frédéric
IPC分类号： A61K31/517 , A61K31/519 , A61P33/00
CPC分类号： A61K31/519 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K31/551 , C07D239/74 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/14 , C07D487/08 , Y02A50/409 , Y02A50/411 , Y02A50/414
摘要： The invention relates to new uses of PI3K inhibitors, wherein said inhibitors have an inhibitory action on the PI3K isoform delta for the treatment of immunopathology in a subject suffering from a disease or disorder selected from malaria, leishmaniasis, trypanosomiasis, toxoplasmosis and/or neurocysticercosis, via functional inhibition of TLR9 of the infected subject.
摘要翻译：本发明涉及PI3K抑制剂的新用途，其中所述抑制剂对PI3K同种型δ具有抑制作用，用于治疗患有选自疟疾，利什曼病，锥虫病，弓形体病和/或神经囊尾erc病的疾病或病症的受试者的免疫病理学，通过功能抑制感染受试者的TLR9。

4. 发明申请

WO2002010192A3 SOMATOSTATIN ANALOGUES 审中-公开
公开(公告)号：WO2002010192A3
公开(公告)日：2002-02-07
申请号：PCT/EP2001/008824
申请日：2001-07-30
申请人： NOVARTIS AG , NOVARTIS-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , ALBERT, Rainer , BAUER, Wilfried , BODMER, David , BRUNS, Christian , FELNER, Ivo , HELLSTERN, Heribert , LEWIS, Ian , MEISENBACH, Mark , WECKBECKER, Gisbert , WIETFELD, Bernhard
发明人： ALBERT, Rainer , BAUER, Wilfried , BODMER, David , BRUNS, Christian , FELNER, Ivo , HELLSTERN, Heribert , LEWIS, Ian , MEISENBACH, Mark , WECKBECKER, Gisbert , WIETFELD, Bernhard
IPC分类号： C07K14/655
摘要： The invention provides cyclo[{4-(NH 2 -C 2 H 4 -NH-CO-O-)Pro}-Phg-DTrp-Lys-Tyr(4-Benzyl)-Phe], optionally in protected form, or a pharmaceutically acceptable salt or complex thereof, which has interesting pharmaceutical properties.

5. 发明申请

WO2013093849A1 DIHYDRO-BENZO-OXAZINE AND DIHYDRO-PYRIDO-OXAZINE DERIVATIVES 审中-公开
标题翻译：二氢苯并氧INE嗪和二氢吡啶 - 氧杂衍生物
公开(公告)号：WO2013093849A1
公开(公告)日：2013-06-27
申请号：PCT/IB2012/057554
申请日：2012-12-20
申请人： NOVARTIS AG
发明人： CARAVATTI, Giorgio , CHAMOIN, Sylvie , FURET, Pascal , HÖGENAUER, Klemens , HURTH, Konstanze , KALIS, Christoph , KAMMERTOENS, Karen , LEWIS, Ian , MOEBITZ, Henrik , SMITH, Alexander Baxter , SOLDERMANN, Nicolas , WOLF, Romain , ZECRI, Frédéric
IPC分类号： C07D413/14 , C07D498/04 , A61K31/536 , A61K31/5365 , A61P19/02 , A61P37/08 , A61P35/00 , A61P33/06
CPC分类号： A61K31/5383 , A61K31/538 , C07D413/14 , C07D498/04 , C12N9/12 , C12Q1/25 , C12Q1/686 , Y02A50/409 , Y02A50/411
摘要： The invention relates to dihydro-benzo-oxazine and dihydro-pyrido-oxazine compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein Y, V, W, U, Q, R 1 , R 5 , R 7 and R 30 are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.
摘要翻译：本发明涉及式（I）的二氢 - 苯并恶嗪和二氢 - 吡啶并恶嗪化合物和/或其药学上可接受的盐和/或溶剂合物，其中Y，V，W，U，Q，R 1，R 5，R 7 和R30如说明书中所定义。这些化合物适用于治疗由PI3K酶的活性介导的病症或疾病。

6. 发明申请

WO2008037476A1 OXADIAZOLE DERIVATIVES WITH ANTI-INFLAMMATORY AND IMMUNOSUPPRESSIVE PROPERTIES 审中-公开
标题翻译：具有抗炎和免疫抑制特性的奥多唑衍生物
公开(公告)号：WO2008037476A1
公开(公告)日：2008-04-03
申请号：PCT/EP2007/008431
申请日：2007-09-27
申请人： NOVARTIS AG , ALBERT, Rainer , COOKE, Nigel, Graham , LEWIS, Ian , WEILER, Sven , ZECRI, Frédéric
发明人： ALBERT, Rainer , COOKE, Nigel, Graham , LEWIS, Ian , WEILER, Sven , ZECRI, Frédéric
IPC分类号： C07D271/06 , A61K31/4245 , A61P37/06
CPC分类号： C07D271/06
摘要： Disclosed are polycyclic compounds of the following formula (I) and their use as anti-inflammatory and immunosuppressive agents.
摘要翻译：公开了下式（I）的多环化合物及其作为抗炎和免疫抑制剂的用途。

7. 发明申请

WO2013057711A1 QUINAZOLINE DERIVATIVES AS PI3K MODULATORS 审中-公开
标题翻译：喹诺酮衍生物作为PI3K调节剂
公开(公告)号：WO2013057711A1
公开(公告)日：2013-04-25
申请号：PCT/IB2012/055745
申请日：2012-10-19
申请人： NOVARTIS AG
发明人： FURET, Pascal , HEBACH, Christina , HÖGENAUER, Klemens , HOLLINGWORTH, Gregory , LEWIS, Ian , SMITH, Alexander, Baxter , SOLDERMANN, Nicolas , STAUFFER, Frédéric , WOLF, Romain , ZECRI, Frédéric
IPC分类号： C07D239/74 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/14 , C07D487/08 , A61K31/517 , A61P37/00 , A61P29/00 , A61P11/00 , A61P35/00
CPC分类号： C07D401/04 , C07D239/74 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/14 , C07D487/08
摘要： The invention relates to substituted quinazoline derivative of the formula (I), wherein A, X 1 , X 2 , X 3 , X 4 and R 5 are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.
摘要翻译：本发明涉及式（I）的取代喹唑啉衍生物，其中A，X 1，X 2，X 3，X 4和R 5如说明书中所定义。这些化合物适用于治疗由PI3K酶的活性介导的病症或疾病。

8. 发明申请

WO2006128658A1 ERGOLINE DERIVATIVES AND THEIR USE AS CHEMOKINE RECEPTOR LIGANDS 审中-公开
标题翻译： ERGOLINE衍生物及其作为化合物受体配体使用
公开(公告)号：WO2006128658A1
公开(公告)日：2006-12-07
申请号：PCT/EP2006/005106
申请日：2006-05-29
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BAENTELI, Rolf , GLICKMAN, Fraser , KOVARIK, Jiri , LEWIS, Ian , STREIFF, Markus , THOMA, Gebhard , ZERWES, Hans-Günter
发明人： BAENTELI, Rolf , GLICKMAN, Fraser , KOVARIK, Jiri , LEWIS, Ian , STREIFF, Markus , THOMA, Gebhard , ZERWES, Hans-Günter
IPC分类号： C07D457/06 , C07D457/08 , A61K31/48
CPC分类号： C07D457/06 , C07D457/08
摘要： Disclosed are ergoline derivatives, Formula (I), wherein either each of R 1 and R 2 , independently, is H; optionally R 10 and/or R 11 -substituted-phenyl or - phenyl-C 1-4 alkyl; optionally R 10 and/or R 11 -substituted-heteroaryl or -heteroaryl-C 1-4 alkyl; optionally R 10 and/or R 11 -substituted heteroaryl N-oxide; optionally R 10 -substituted C 1 -C 8 alkyl; optionally R 10 -substituted C 2 -C 8 alkenyl, optionally R 10 -substituted C 2 -C 8 alkynyl; optionally R 10 -substituted C 3 -C 8 cycloalkyl, or optionally R 10 -substituted C 4 -C 8 cycloalkenyl; or R 1 and R 2 form together with the nitrogen atom to which they are attached an optionally R 10 -substituted 3-8 membered ring containing in addition to the nitrogen atom up to 2 heteroatoms selected independently from N, O and S; R 3 is H; OR 1 ; CH 2 R 1 R 2 ; (CH 2 ) 1-2 NR 1 R 2 ; CH 2 -CH 2 -OR 1 ; CH 2 -CO-NR 1 R 2 ; or CO-CH 2 R 1 R 2 ; R 4 is F; CI; Br; I; OR 1 ; NR 1 R 2 or has one of the significances given for R 1 ; and R 5 has one of the significances given for R 1 , in free form or in salt form for preventing or treating disorders or diseases mediated by interactions between chemokine receptors and their ligands.
摘要翻译：公开了麦角灵衍生物，式（I），其中R 1和R 2中的每一个独立地是H; 任选的R 10和/或R 11取代的苯基或 - 苯基-C 1-4烷基; 任选的R 10和/或R 11 - 取代的 - 杂芳基或 - 杂芳基-C 1-4 - 烷基; 任选的R 10和/或R 11 - 取代的杂芳基N-氧化物; 任选的R 10取代的C 1 -C 8烷基; 任选的R 10取代的C 2 -C 8链烯基，任选地R 10取代的C 2 C 8 -C 15炔基; 任选的R 10取代的C 3 -C 8环烷基，或任选地R 10取代的C 1 -C 10 - 4 -C 8环烯基; 或R 1和R 2 2与它们所连接的氮原子一起形成任选的R 10取代的3-8元环，其含有除了氮原子多达2个独立于N，O和S选择的杂原子; R 3是H; OR _{1 ; CH _{2 - [R _{1 - [R _{2 ; （CH _{2 ）_{1-2 NR _{1 - [R _{2 ; CH _{2 -CH _{2 -OR _{1 ; CH _{2 -CO-NR _{1 - [R _{2 ; 或CO-CH 2 R 1 R 2 R 2; R 4是F; CI; BR; 一世; OR _{1 ; NR 1 R 2 R 2或具有对R 1 1给出的含义之一; 和R 5具有游离形式或盐形式的R 1 1给出的意义之一，用于预防或治疗由趋化因子受体及其配体之间的相互作用介导的疾病或疾病。}}}}}}}}}}}}}}}

9. 发明公开

EP2794600A1 DIHYDRO-BENZO-OXAZINE AND DIHYDRO-PYRIDO-OXAZINE DERIVATIVES 有权
标题翻译： 2,3-二氢苯并[1,4]氧杂 - 衍生物磷酸三磷酸激酶3（PI3K）抑制剂ZUR BEHANDLUNG VON RHEUMATOIDER ARTHRITIS
公开(公告)号：EP2794600A1
公开(公告)日：2014-10-29
申请号：EP12823036.4
申请日：2012-12-20
申请人： Novartis AG
发明人： CARAVATTI, Giorgio , CHAMOIN, Sylvie , FURET, Pascal , HÖGENAUER, Klemens , HURTH, Konstanze , KALIS, Christoph , KAMMERTOENS, Karen , LEWIS, Ian , MOEBITZ, Henrik , SMITH, Alexander Baxter , SOLDERMANN, Nicolas , WOLF, Romain , ZECRI, Frédéric
IPC分类号： C07D413/14 , C07D498/04 , A61K31/536 , A61K31/5365 , A61P19/02 , A61P37/08 , A61P35/00 , A61P33/06
CPC分类号： A61K31/5383 , A61K31/538 , C07D413/14 , C07D498/04 , C12N9/12 , C12Q1/25 , C12Q1/686 , Y02A50/409 , Y02A50/411
摘要： The invention relates to dihydro-benzo-oxazine and dihydro-pyrido-oxazine compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein Y, V, W, U, Q, R1, R5, R7 and R30 are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.
摘要翻译：本发明涉及式（I）的二氢 - 苯并恶嗪和二氢 - 吡啶并 - 恶嗪化合物和/或其药学上可接受的盐和/或溶剂合物，其中Y，V，W，U，Q，R 1，R 5，R 7 和R30如说明书中所定义。此类化合物适用于治疗由PI3K酶的活性介导的疾病或疾病。

10. 发明公开

EP1893611A1 ERGOLINE DERIVATIVES AND THEIR USE AS CHEMOKINE RECEPTOR LIGANDS 审中-公开
标题翻译：麦角灵衍生物和它们作为趋化因子受体配体的用途
公开(公告)号：EP1893611A1
公开(公告)日：2008-03-05
申请号：EP06753946.0
申请日：2006-05-29
申请人： Novartis AG
发明人： BAENTELI, Rolf , GLICKMAN, Fraser , KOVARIK, Jiri , LEWIS, Ian , STREIFF, Markus , THOMA, Gebhard , ZERWES, Hans-Günter
IPC分类号： C07D457/06 , C07D457/08 , A61K31/48
CPC分类号： C07D457/06 , C07D457/08
摘要： Disclosed are ergoline derivatives, Formula (I), wherein either each of R1 and R2, independently, is H; optionally R10 and/or R11-substituted-phenyl or - phenyl-C1-4alkyl; optionally R10 and/or R11-substituted-heteroaryl or -heteroaryl-C1-4alkyl; optionally R10 and/or R11-substituted heteroaryl N-oxide; optionally R10-substituted C1-C8 alkyl; optionally R10-substituted C2-C8 alkenyl, optionally R10-substituted C2-C8 alkynyl; optionally R10-substituted C3-C8 cycloalkyl, or optionally R10-substituted C4-C8 cycloalkenyl; or R1 and R2 form together with the nitrogen atom to which they are attached an optionally R10-substituted 3-8 membered ring containing in addition to the nitrogen atom up to 2 heteroatoms selected independently from N, O and S; R3 is H; OR1; CH2R1R2; (CH2)1-2NR1R2; CH2-CH2-OR1; CH2-CO-NR1R2; or CO-CH2R1R2; R4 is F; CI; Br; I; OR1; NR1R2 or has one of the significances given for R1; and R5 has one of the significances given for R1, in free form or in salt form for preventing or treating disorders or diseases mediated by interactions between chemokine receptors and their ligands.

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