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1. 发明申请

WO2019186358A1 3-HYDROXY-N-(3-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)PHENYL)PYRROLIDINE-1-CARBOXAMIDE DERIVATIVES 审中-公开
公开(公告)号：WO2019186358A1
公开(公告)日：2019-10-03
申请号：PCT/IB2019/052392
申请日：2019-03-25
申请人： NOVARTIS AG
发明人： ARISTA, Luca , HEBACH, Christina , HOLLINGWORTH, Gregory John , HOLZER, Philipp , IMBACH-WEESE, Patricia , MACHAUER, Rainer , SCHMIEDEBERG, Niko , VULPETTI, Anna , ZOLLER, Thomas
IPC分类号： C07D487/04 , C07D519/00 , A61P35/00 , A61K31/519
摘要： The invention relates to compounds of the formula (I) or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

2. 发明申请

WO2022189859A1 FATTY ACID-BIFUNCTIONAL DEGRADER CONJUGATES AND THEIR METHODS OF USE 审中-公开
公开(公告)号：WO2022189859A1
公开(公告)日：2022-09-15
申请号：PCT/IB2022/000119
申请日：2022-03-10
申请人： NOVARTIS AG
发明人： ADCOCK, Claire , BROENNIMANN, Valerie , CHENG, Jiashun , DUVADIE, Rohit Kumar , FAZAL, Tanzina , GAO, Jinhai , GUO, Fengfeng , GROTZFELD, Robert, Martin , HEBACH, Christina , HOLLINGWORTH, Gregory John , JONES, Darryl, Brynley , KARPOV, Alexei , LI, Jialiang , LORBER, Julien , METCALF III, Chester A. , MICHAEL, Walter , PALERMO, Mark, Gabriel , PLUMMER, Scott, Vaughan , ROACHE, James, Harold , SENDZIK, Martin , THOMAS, Ranny, Mathew , USERA, Aimee, Richardson , VULPETTI, Anna , ZECRI, Frederic , ZHAO, Liang , ZOLLER, Thomas
IPC分类号： A61K47/54 , A61P35/00
摘要： Described herein are fatty acid-bifunctional degrader compounds, their various targets, their preparation, pharmaceutical compositions comprising them, and their use in the treatment of conditions, diseases, and disorders mediated by various target proteins.

3. 发明申请

WO2008065068A3 SUBSTITUTED DIHYDROIMIDAZOLES AND THEIR USE IN THE TREATMENT OF TUMORS 审中-公开
公开(公告)号：WO2008065068A3
公开(公告)日：2008-06-05
申请号：PCT/EP2007/062804
申请日：2007-11-26
申请人： NOVARTIS AG , CHAMOIN, Sylvie , ROTH, Hans-Jörg , ZIMMERMANN, Juerg , ZOLLER, Thomas
发明人： CHAMOIN, Sylvie , ROTH, Hans-Jörg , ZIMMERMANN, Juerg , ZOLLER, Thomas
IPC分类号： C07D233/40 , C07D401/12 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/12 , A61K31/4178 , A61P35/00
摘要： The invention relates to dihydroimidazoles of formula rac-(l), wherein the radicals and symbols are as defined herein; their use as inhibitors of the interaction of the MDM2 protein with a p53-like peptide, new pharmaceutical formulations comprising said compounds, said compounds for use in the therapeutic treatment of warm-blooded animals, especially humans, their use in the treatment of proliferative diseases or for the manufacture of pharmaceutical formulations useful in the treatment of proliferative diseases that respond to modulation of the interaction of the MDM2 protein with a p53-like peptide, a pharmaceutical formulation e.g. useful in the treatment of proliferative diseases that respond to modulation of the interaction of the MDM2 protein with a p53-like peptide comprising said compound, methods of treatment comprising administration of said compounds to a warm-blooded animal, and/or processes for the manufacture of said compounds.

4. 发明申请

WO2019186343A1 N-(3-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)PHENYL)BENZAMIDE DERIVATIVES 审中-公开
公开(公告)号：WO2019186343A1
公开(公告)日：2019-10-03
申请号：PCT/IB2019/052346
申请日：2019-03-22
申请人： NOVARTIS AG
发明人： ARISTA, Luca , HEBACH, Christina , HOLLINGWORTH, Gregory John , HOLZER, Philipp , IMBACH-WEESE, Patricia , LORBER, Julien , MACHAUER, Rainer , SCHMIEDEBERG, Niko , VULPETTI, Anna , ZOLLER, Thomas
IPC分类号： C07D471/10 , C07D487/04 , C07D498/10 , C07D519/00 , A61K31/519
摘要： The invention relates to compounds of the formula (I) (I) or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

5. 发明申请

WO2008037459A1 PYRAZOLO [1, 5-A] PYRIMIDINE DERIVATIVES AND THEIR THERAPEUTIC USE 审中-公开
标题翻译：吡咯并[1,5-A]吡嗪衍生物及其治疗用途
公开(公告)号：WO2008037459A1
公开(公告)日：2008-04-03
申请号：PCT/EP2007/008390
申请日：2007-09-26
申请人： NOVARTIS AG , BUEHLMAYER, Peter , BREITENSTEIN, Werner , FURET, Pascal , PIRARD, Bernard , VON MATT, Anette , ZOLLER, Thomas
发明人： BUEHLMAYER, Peter , BREITENSTEIN, Werner , FURET, Pascal , PIRARD, Bernard , VON MATT, Anette , ZOLLER, Thomas
IPC分类号： C07D487/04 , A61K31/495 , A61P9/00 , A61P25/00 , A61P19/00 , A61P35/00
CPC分类号： C07D487/04
摘要： Disclosed are pyrazolo-pyrimidine derivatives which have interesting pharmaceutical properties.
摘要翻译：公开了具有有趣的药物性质的吡唑并嘧啶衍生物。

6. 发明申请

WO2015181747A1 NOVEL PYRAZOLO PYRIMIDINE DERIVATIVES AND THEIR USE AS MALT1 INHIBITORS 审中-公开
标题翻译：新型吡咯并吡啶衍生物及其作为MALT1抑制剂的用途
公开(公告)号：WO2015181747A1
公开(公告)日：2015-12-03
申请号：PCT/IB2015/053975
申请日：2015-05-27
申请人： NOVARTIS AG , PISSOT SOLDERMANN, Carole , QUANCARD, Jean , SCHLAPBACH, Achim , SIMIC, Oliver , TINTELNOT-BLOMLEY, Marina , ZOLLER, Thomas
发明人： PISSOT SOLDERMANN, Carole , QUANCARD, Jean , SCHLAPBACH, Achim , SIMIC, Oliver , TINTELNOT-BLOMLEY, Marina , ZOLLER, Thomas
IPC分类号： C07D487/04 , A61K31/519 , A61P29/00 , A61P35/00 , A61P37/00
CPC分类号： C07D487/04 , A61K31/519 , A61K31/5377
摘要： The present invention describes new pyrazolo-pyrimidine derivatives of formula (I) or a pharmaceutically acceptable salt thereof; (I) wherein, R1 is halogen, cyano, or C 1 -C 3 alkyl optionally substituted by halogen; R2 is C 1 -C 6 alkyl optionally substituted one or more times by C 1 -C 6 alkyl, C 2 -C 6 alkenyl, hydroxyl, N,N-di-C 1 -C 6 alkyl amino, N-mono-C 1 -C 6 alkyl amino, O-Rg, Rg, phenyl, or by C 1 -C 6 alkoxy wherein said alkoxy again may optionally be substituted by C 1 -C 6 alkoxy, N,N-di-C 1 -C 6 alkyl amino, Rg or phenyl; C 3 -C 6 cycloalkyl optionally substituted by C 1 -C 6 alkyl, N,N-di-C 1 -C 6 alkyl amino or C 1 -C 6 alkoxy-C 1 -C 6 alkyl, and/or two of said optional substituents together with the atoms to which they are bound may form an annulated or spirocyclic 4 - 6 membered saturated heterocyclic ring comprising 1 - 2 O atoms; phenyl optionally substituted by C 1 -C 6 alkoxy; a 5 - 6 membered heteroaryl ring having 1 to 3 heteroatoms selected from N and O said ring being optionally substituted by C 1 -C 6 alkyl which may be optionally substituted by amino or hydroxy; Rg; or N,N-di-C 1 -C 6 alkyl amino carbonyl; and R is phenyl independently substituted two or more times by Ra, 2-pyridyl independently substituted one or more times by Rb, 3-pyridyl independently substituted one or more times by Rc, or 4-pyridyl independently substituted one or more times by Rd; which are generally interacting with MALT1 proteolytic and/or autoproteolytic activity, and in particular which may inhibit said activity. The present invention further describes the synthesis of said new pyrazolo-pyrimidine derivatives, their use as a medicament, especially by interacting with MALT1 proteolytic and/or autoproteolytic activity.
摘要翻译：本发明描述了式（I）的新的吡唑并嘧啶衍生物或其药学上可接受的盐; （I）其中，R 1为卤素，氰基或任选被卤素取代的C 1 -C 3烷基; R2是任选被C 1 -C 6烷基，C 2 -C 6烯基，羟基，N，N-二-C 1 -C 6烷基氨基，N-单-C 1 -C 6烷基氨基，O-R g，R g，苯基，或C 1 -C 6烷氧基，其中所述烷氧基再次可任选被C 1 -C 6烷氧基，N，N-二-C 1烷基氨基，R g或苯基取代; 任选地被C 1 -C 6烷基，N，N-二-C 1 -C 6烷基氨基或C 1 -C 6烷氧基-C 1 -C 6烷基取代的C 3 -C 6环烷基和/或所述任选取代基中的两个与它们所键合的原子一起形成环状或包含1〜2个O原子的螺环4-6元饱和杂环; 任选被C 1 -C 6烷氧基取代的苯基; 具有1至3个选自N和O的杂原子的5-6元杂芳基环，所述环任选被可被氨基或羟基任选取代的C 1 -C 6烷基取代; RG; 或N，N-二-C 1 -C 6烷基氨基羰基; R为独立地被R a取代两次或更多次的苯基，R 2独立地取代一次或多次的2-吡啶基，R c独立地取代一次或多次的3-吡啶基，或被Rd独立地取代一次或多次的4-吡啶基; 其通常与MALT1蛋白水解和/或自发蛋白水解活性相互作用，特别是可能抑制所述活性。本发明还描述了所述新的吡唑并嘧啶衍生物的合成，它们作为药物的用途，特别是通过与MALT1蛋白水解和/或自身蛋白水解活性的相互作用。

7. 发明申请

WO2012017020A1 N-((6-AMINO-PYRIDIN-3-YL)METHYL)-HETEROARYL-CARBOXAMIDES AS INHIBITORS OF PLASMA KALLIKREIN 审中-公开
标题翻译： N - （（6-氨基 - 吡啶-3-基）甲基） - 乙酰胆碱酰胺作为血浆KALLIKREIN的抑制剂
公开(公告)号：WO2012017020A1
公开(公告)日：2012-02-09
申请号：PCT/EP2011/063389
申请日：2011-08-03
申请人： NOVARTIS AG , BRANDL, Trixi , FLOHR, Stefanie , KOPEC, Sebastian , LACHAL, Julie , MARKERT, Christian , NAMOTO, Kenji , NGANGA, Perle , PIRARD, Bernard , RENATUS, Martin , SEDRANI, Richard , ZOLLER, Thomas
发明人： BRANDL, Trixi , FLOHR, Stefanie , KOPEC, Sebastian , LACHAL, Julie , MARKERT, Christian , NAMOTO, Kenji , NGANGA, Perle , PIRARD, Bernard , RENATUS, Martin , SEDRANI, Richard , ZOLLER, Thomas
IPC分类号： C07D405/14 , C07D403/12 , C07D413/12 , C07D403/14 , C07D417/14 , C07D409/14 , A61K31/4439 , A61P7/02
CPC分类号： C07D409/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/12 , C07D417/14
摘要： The invention relates to compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
摘要翻译：本发明涉及式（I）化合物，其中取代基如说明书中所定义; 以游离形式或盐形式; 作为其制备，用作药物和包含它的药物。

8. 发明申请

WO2010043584A1 SALICYLIC ACID DERIVATIVES BEING FARNESYL PYROPHOSPHATE SYNTHASE ACTIVITY INHIBITORS 审中-公开
标题翻译：磷酸酯合成酶活性抑制剂的脂肪酸衍生物
公开(公告)号：WO2010043584A1
公开(公告)日：2010-04-22
申请号：PCT/EP2009/063257
申请日：2009-10-12
申请人： NOVARTIS AG , COTESTA, Simona , GLICKMAN, Joseph Fraser , JAHNKE, Wolfgang , MARZINZIK, Andreas , OFNER, Silvio , RONDEAU, Jean-Michel , ZOLLER, Thomas
发明人： COTESTA, Simona , GLICKMAN, Joseph Fraser , JAHNKE, Wolfgang , MARZINZIK, Andreas , OFNER, Silvio , RONDEAU, Jean-Michel , ZOLLER, Thomas
IPC分类号： C07C65/21 , C07C229/64 , C07D207/06 , C07D207/08 , C07D209/08 , C07D211/22 , C07D213/74 , C07D231/38 , C07D295/10 , C07D307/14 , C07D319/08 , C07D333/20 , A61P43/00 , A61K31/192
CPC分类号： C07D207/26 , C07C65/24 , C07C229/64 , C07C233/54 , C07C255/58 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2601/18 , C07D207/09 , C07D207/327 , C07D209/18 , C07D211/22 , C07D211/58 , C07D213/36 , C07D213/64 , C07D213/74 , C07D231/38 , C07D243/08 , C07D295/155 , C07D295/185 , C07D307/14 , C07D307/54 , C07D307/79 , C07D317/60 , C07D319/18 , C07D333/20 , C07D333/60
摘要： The invention relates to the use of and mainly novel compounds of the formula (I) wherein the moieties are as defined in the description, which are useful as farnesyl pyrophosphate synthase modulators and e.g. in the treatment of proliferative diseases.
摘要翻译：本发明涉及式（I）的新型化合物和主要新颖化合物，其中部分如说明书中所定义，其可用作法呢基焦磷酸合酶调节剂，在治疗增殖性疾病。

9. 发明申请

WO2021055295A1 BRD9 BIFUNCTIONAL DEGRADERS AND THEIR METHODS OF USE 审中-公开
公开(公告)号：WO2021055295A1
公开(公告)日：2021-03-25
申请号：PCT/US2020/050768
申请日：2020-09-14
申请人： NOVARTIS AG , LORBER, Julien , SENDZIK, Martin
发明人： CHEN, Xin , GOUDE, Marie-line , HARRINGTON, Edmund, Martin , HOLLINGWORTH, Gregory, John , VULPETTI, Anna , ZOLLER, Thomas
IPC分类号： C07D401/14 , C07D471/04 , A61P35/00 , A61K31/513
摘要： The disclosure provides BRD9 bifunctional compounds of Formula (A) or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, to their preparation, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases and disorders mediated by a bromodomain-containing protein, such as bromodoma in-containing protein 9 (BRD9)

10. 发明申请

WO2021053495A1 BIFUNCTIONAL DEGRADERS AND THEIR METHODS OF USE 审中-公开
公开(公告)号：WO2021053495A1
公开(公告)日：2021-03-25
申请号：PCT/IB2020/058535
申请日：2020-09-14
申请人： NOVARTIS AG
发明人： ARISTA, Luca , BROENNIMANN, Valerie , D’ALESSANDRO, Pier Luca , DOUMAMPOUOM-METOUL, Lionel , GOUDE, Marie-Line , HEBACH, Christina , HOLLINGWORTH, Gregory John , JEULIN, Ingrid Karen Jennifer , KIRMAN, Louise Clare , LORBER, Julien , MA, Fupeng , VULPETTI, Anna , YAMADA, Ken , ZOLLER, Thomas
IPC分类号： A61P35/00 , C07D239/22 , C07D401/06 , C07D401/12 , C07D401/14 , C07D471/10 , C07D471/14 , C07D487/14 , A61K31/513
摘要： Described herein are bifunctional degrader compounds, their various targets, their preparation, pharmaceutical compositions comprising them, and their use in the treatment of conditions, diseases, and disorders mediated by various target proteins.

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