- Immunomodulator
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The invention discloses an immunomodulator, and particularly relates to compounds for inhibiting IL-17A and application of the compounds serving as the immunomodulator in preparation of drugs. The invention discloses an application of a compound shown as a formula I or a stereoisomer thereof in preparing medicines for inhibiting IL-17A, and provides a new choice for clinically screening and/or preparing medicines for treating diseases related to IL-17A activity.
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Paragraph 0240-0241; 0245-0247
(2021/02/10)
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- Immunomodulator
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The invention discloses an immunomodulator, and particularly relates to compounds for inhibiting IL17A and application of the compounds serving as the immunomodulator in preparation of drugs. The invention discloses an application of a compound shown as a formula I or a stereoisomer thereof in preparing medicines for inhibiting IL-17A, and provides a new choice for clinically screening and/or preparing medicines for treating diseases related to IL-17A activity.
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Paragraph 0180-0181; 0191-0193
(2021/02/10)
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- Discovery of BAY-985, a Highly Selective TBK1/IKK? Inhibitor
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The serine/threonine kinase TBK1 (TANK-binding kinase 1) and its homologue IKK? are noncanonical members of the inhibitor of the nuclear factor κB (IκB) kinase family. These kinases play important roles in multiple cellular pathways and, in particular, in inflammation. Herein, we describe our investigations on a family of benzimidazoles and the identification of the potent and highly selective TBK1/IKK? inhibitor BAY-985. BAY-985 inhibits the cellular phosphorylation of interferon regulatory factor 3 and displays antiproliferative efficacy in the melanoma cell line SK-MEL-2 but showed only weak antitumor activity in the SK-MEL-2 human melanoma xenograft model.
- Lefranc, Julien,Schulze, Volker Klaus,Hillig, Roman Christian,Briem, Hans,Prinz, Florian,Mengel, Anne,Heinrich, Tobias,Balint, Jozsef,Rengachari, Srinivasan,Irlbacher, Horst,St?ckigt, Detlef,B?mer, Ulf,Bader, Benjamin,Gradl, Stefan Nikolaus,Nising, Carl Friedrich,Von Nussbaum, Franz,Mumberg, Dominik,Panne, Daniel,Wengner, Antje Margret
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supporting information
p. 601 - 612
(2020/02/04)
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- HETEROARYLBENZIMIDAZOLE COMPOUNDS
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The present invention covers heteroarylbenzimidazole compounds of general formula (I) in which R1, R2, R3, R4 and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative and/or inflammatory disorders, as a sole agent or in combination with other active ingredients.
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Page/Page column 318
(2017/07/06)
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- An organic electroluminescent compounds (by machine translation)
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The present invention discloses an organic electroluminescent compounds, such as the formula (I) with or (II) the structure of the shown: Wherein A and Z is independently N or CH; R1 And R2 Are each independently selected from: H, alkyl, cycloalkyl, alkoxy, aromatic, heterocyclic aromatic; R3 - R6 Are each independently selected from: H, cyano, alkyl, cycloalkyl, alkoxy, aromatic, heterocyclic aromatic; R7 And R8 And they are connected together constitute N carbazolyl or C1 - C8 alkyl substituted carbazole-based. The design of the invention a series of boron organic molecule can be used as a light-emitting material used for making the OLED device, which exhibit relatively low driving voltage, high luminous efficiency, high color purity and long service life, has applied to the prospects of AMOLED. (by machine translation)
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Paragraph 0059; 0060; 0061
(2018/03/24)
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- METALLO-BETA-LACTAMASE INHIBITORS
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The present invention relates to compounds of formula I that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
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- METALLO-BETA-LACTAMASE INHIBITORS
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The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
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- IMIDAZOPYRAZINES AND PYRAZOLOPYRIMIDINES AND THEIR USE AS AMPA RECEPTOR MODULATORS
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Provided herein are compounds of Formula (I), and pharmaceutically acceptable salts, N-oxides, or solvates thereof, [Formula should be inserted here] Also provided herein are pharmaceutical compositions, comprising compounds of Formula (I), and methods of
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Page/Page column 97
(2016/12/26)
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- PHOSPHOINOSITIDE 3-KINASE INHIBITORS WITH ZINC BINDING MOIETY
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PROBLEM TO BE SOLVED: To provide phosphoinositide 3-kinase inhibitors with a zinc binding moiety. SOLUTION: There is provided a compound represented by formula (I) in the figure. (X is S, O or the like; Y is CH, N or the like; G1 is optionally substituted N or the like; R1 and R2 are each independently H or the like; C is a substituted heterocycle or the like; B is a linear alkyl or the like; Ra and Rb together with the nitrogen atom coupled to them are morpholino or the like; G2 is an indazole ring or the like; q, r and s are independently from 0 to 1, provided that at least one of them is 1; t is from 0 to 1; n is from 0 to 4; and p is from 0 to 2.) COPYRIGHT: (C)2016,JPOandINPIT
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Paragraph 0296; 0472
(2016/10/07)
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- NOVEL 3-INDOL SUBSTITUTED DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USE
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The present invention relates to compound of Formula (I) or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or HIV, depression, and obesity. The invention also relates to a process for manufacturing compounds of Formula (I).
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Page/Page column 102; 103
(2016/01/12)
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- PDE 10a Inhibitors for the Treatment of Type II Diabetes
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Disclosed are compounds, compositions and methods for treating Type II diabetes. Such compounds are represented by Formula (I) as follows: wherein R1, R2, L, and Q are defined herein.
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Paragraph 0482-0484
(2015/01/06)
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- TREATMENT OF CANCERS HAVING K-RAS MUTATIONS
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The present invention provides a method of treating a cancer associated with a K-ras mutation in a subject in need thereof. The method comprises the steps of: (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) administering to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.
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Paragraph 0554; 0555
(2013/05/08)
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- Nanoscale Fe2O3-based catalysts for selective hydrogenation of nitroarenes to anilines
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Production of anilines - key intermediates for the fine chemical, agrochemical, and pharmaceutical industries - relies on precious metal catalysts that selectively hydrogenate aryl nitro groups in the presence of other easily reducible functionalities. Herein, we report convenient and stable iron oxide (Fe2O3) - based catalysts as a more earth-abundant alternative for this transformation. Pyrolysis of iron-phenanthroline complexes on carbon furnishes a unique structure in which the active Fe2O 3 particles are surrounded by a nitrogen-doped carbon layer. Highly selective hydrogenation of numerous structurally diverse nitroarenes (more than 80 examples) proceeded in good to excellent yield under industrially viable conditions.
- Jagadeesh, Rajenahally V.,Surkus, Annette-Enrica,Junge, Henrik,Pohl, Marga-Martina,Radnik, Joerg,Rabeah, Jabor,Huan, Heming,Schunemann, Volker,Brueckner, Angelika,Beller, Matthias
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p. 1073 - 1076
(2014/01/06)
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- TREATMENT OF CANCERS HAVING K-RAS MUTATIONS
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The present invention provides a method of treating a cancer associated with a K- ras mutation in a subject in need thereof. The method comprises the steps of (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) adminsiterign to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.
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Page/Page column 222
(2011/11/01)
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- PYRIMIDINE INHIBITORS OF KINASE ACTIVITY
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Described herein are compounds of formula (I) or pharmaceutical acceptable salts or solvates thereof, wherein G1, L1, R2, R3, n, p, Ar1, and Ar2 are defined in the description. Methods of making said compounds, and compositions comprising said compounds which are useful for inhibiting kinases such as IGF-IR are also disclosed.
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Page/Page column 58-59
(2010/12/26)
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- PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES
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Compounds of the following formula (I) are inhibitors of microtubule affinity regulating kinase, and hence find use in the treatment of neurodegenerative diseases associated with hyperphosphorylation of tau.
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Page/Page column 43; 23
(2009/03/07)
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- Development of multitargeted inhibitors of both the insulin-like growth factor receptor (IGF-IR) and members of the epidermal growth factor family of receptor tyrosine kinases
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Emerging clinical and pre-clinical data indicate that both insulin-like growth factor receptor (IGF-IR) and members of the epidermal growth factor (EGF) family of receptor tyrosine kinases (RTKs) exhibit significant cross-talk in human cancers. Therefore, a small molecule that successfully inhibits the signaling of both classes of oncogenic kinases might provide an attractive agent for chemotherapeutic use. Herein, we disclose the structure activity relationships that led to the synthesis and biological characterization of 14, a novel small molecule inhibitor of both IGF-IR and members of the epidermal growth factor family of RTKs.
- Hubbard, Robert D.,Bamaung, Nwe Y.,Fidanze, Steve D.,Erickson, Scott A.,Palazzo, Fabio,Wilsbacher, Julie L.,Zhang, Qian,Tucker, Lora A.,Hu, Xiaoming,Kovar, Peter,Osterling, Donald J.,Johnson, Eric F.,Bouska, Jennifer,Wang, Jieyi,Davidsen, Steven K.,Bell, Randy L.,Sheppard, George S.
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scheme or table
p. 1718 - 1721
(2009/11/30)
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- Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): Optimization of the 6-aryl substituent
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Design and synthesis of a series of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d] pyrimidines as potent and selective inhibitors of the mammalian target of rapamycin (mTOR) are described. Optimization of the 6-aryl substituent led to the discovery of inhibitors carrying 6-ureidophenyl groups, the first reported active site inhibitors of mTOR with subnanomolar inhibitory concentrations. The data presented in this paper show that 6-arylureidophenyl substituents led to potent mixed inhibitors of mTOR and phosphatidylinositol 3-kinase α (PI3K-α), whereas 6-alkylureidophenyl appendages gave highly selective mTOR inhibitors. Combination of 6-alkylureidophenyl groups with 1-carbamoylpiperidine substitution resulted in compounds with subnanomolar IC50 against mTOR and greater than 1000-fold selectivity over PI3K-α. In addition, structure based drug design resulted in the preparation of several 6-arylureidophenyl-1H-pyrazolo[3,4-d]pyrimidines, substituted in the 4-position of the arylureido moiety with water solubilizing groups. These compounds combined potent mTOR inhibition (IC50501 nM). 2009 American Chemical Society.
- Verheijen, Jeroen C.,Richard, David J.,Curran, Kevin,Kaplan, Joshua,Lefever, Mark,Nowak, Pawel,Malwitz, David J.,Brooijmans, Natasja,Toral-Barza, Lourdes,Zhang, Wei-Guo,Lucas, Judy,Hollander, Irwin,Ayral-Kaloustian, Semiramis,Mansour, Tarek S.,Yu, Ker,Zask, Arie
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supporting information; experimental part
p. 8010 - 8024
(2010/07/04)
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- Benzoxazoles and oxazolopyridines being useful as Janus kinases inhibitors
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The invention relates to 2,7-disubstituted benzoxazole and 2,4-disubstituted oxazolo[5,4-c]pyridine compounds of the formula I given below, as well as salts thereof, processes for the preparation thereof, the application thereof in a process for the treat
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Page/Page column 24
(2008/06/13)
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- Pharmaceutical compounds
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Compounds of Formulae Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia and Ib for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
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Page/Page column 102
(2008/06/13)
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- PYRIMIDINONES AS CASEIN KINASE II (CK2) MODULATORS
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A compound having Formula I :or a pharmaceutically acceptable salt thereof, wherein X, R, R and R are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof. The compounds of Fomula I are inhibitors of Casein kina
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Page/Page column 72
(2009/01/20)
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- PROTEIN KINASE INHIBITORS
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Compounds that inhibit protein kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.
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Page/Page column 84
(2010/11/28)
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- Hangman salophens
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We report here a modular approach for the construction of a new class of compounds, the Hangman salophens. In the Hangman motif, an acid-base functionality "hangs" over the face of a redox cofactor. In contrast to more synthetically intractable porphyrin-based Hangman systems, Hangman salophens permit the facile control of their proton and redox properties for the study of the proton-coupled electron transfer (PCET) activation of small molecules. By investigating the catalase-like disproportionation of H2O2, we show that the presence (1) of a strong proton-donating hanging group (i.e., carboxylic acid) and (2) of electron-donating groups on the redox-active salen imparts significant catalytic activity for the O-O bond activation of small molecule substrates. The contribution of the new ligand framework to furthering our understanding of how PCET can be implemented in the design of active/selective catalysts will be discussed. Copyright
- Liu, Shih-Yuan,Nocera, Daniel G.
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p. 5278 - 5279
(2007/10/03)
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