- ESTROGEN RECEPTOR ANTAGONIST
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Provided is an indole compound. In particular, disclosed are a compound represented by formula (II) or an isomer or pharmaceutically acceptable salt thereof and a use of the same as an estrogen receptor antagonist in preparing a drug for treating estrogen receptor-positive breast cancer.
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Paragraph 0226
(2021/10/07)
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- Triazole glycoside derivative of 3-nitro-1-benzenesulfonyl-7-azaindole and preparation method and application thereof
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The invention belongs to the technical field of medicines, and particularly relates to a triazole glycoside derivative of 3-nitro-1-benzenesulfonyl-7-azaindole and a preparation method and applicationthereof. The triazole glycoside derivative of 3-nitro-1
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Paragraph 0031
(2020/08/07)
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- Design and synthesis of azaindole heterocycle decorated new scaffold in fluorometric sensing of F? and H2PO4?
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7-Azaindole has been used in designing new molecular structure 1 on enediyne spacer for its application in anion sensing. New structure 1 has been established as efficient fluorescent sensor of H2PO4? and F? ion
- Ghosh, Kumaresh,Ali, Sk. Sarfaraj,Joardar, Soumen
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p. 3558 - 3565
(2020/08/06)
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- Peptidylarginine deiminase inhibitor and application thereof
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The invention belongs to the technical field of medicine, and particularly relates to a peptidylarginine deiminase PAD4 inhibitor compound shown in a formula (I) or pharmaceutically acceptable salts,stereoisomers and tautomers thereof, as well as pharmaceutical compositions, pharmaceutical preparations and application thereof. X, Y, R1, R2, R3, R4, R5, R7, R8, R9, ring B and m are as defined in the specification. The compound has inhibitory effect on peptidylarginine deiminase PAD4, and can be used for treating various diseases, such as rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, multiple sclerosis, cystic fibrosis, cancer, cutaneous lupus erythematosus, asthma and psoriasis.
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Paragraph 0048; 0049; 0050; 0051; 0052
(2019/09/10)
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- Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors
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From four molecules, inspired by the structural features of fascaplysin, with an interesting potential to inhibit cyclin-dependent kinases (CDKs), we designed a new series of tri-heterocyclic derivatives based on 1H-pyrrolo[2,3-b]pyridine (7-azaindole) an
- Baltus, Christine B.,Jorda, Radek,Marot, Christophe,Berka, Karel,Bazgier, Václav,Kry?tof, Vladimír,Prié, Gildas,Viaud-Massuard, Marie-Claude
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p. 701 - 719
(2016/01/09)
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- MAP4K4 (HGK) Inhibitors
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The invention provides mitogen-activated protein kinase kinase kinase kinase 4 (MAP4K4) inhibitors, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant diminution of tumor cell growth, cancer or metastasis.
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Paragraph 0290
(2016/08/10)
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- Palladium-Catalyzed Amination of N-Free 2-Chloro-7-azaindole
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A simple and efficient procedure for the Pd-catalyzed amination of N-free 2-chloro-7-azaindole is described, using either primary or secondary amines. An optimized combination of Brettphos, a Brettphos precatalyst, and LiHMDS in THF led us to a novel methodology, applied to various functionalized amines to study the scope of the reaction. This is the first report of cross-coupling amination on N-free 2-chloro-7-azaindole.
- Plas, Aurélie,Martin, Camille,Joubert, Nicolas,Viaud-Massuard, Marie-Claude
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supporting information
p. 4710 - 4713
(2015/10/12)
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- ISOTOPICALLY ENRICHED AZAINDOLES
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The present invention relates to a deuterated pyrrolo[2,3-b]pyridinyl compound that is useful for inhibiting Janus kinases. The invention also relates to processes and intermediates useful for preparing such a compound.
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Paragraph 0283; 0284
(2015/03/13)
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- 2-(AZAINDOL-2-YL)BENZIMIDAZOLES AS PAD4 INHIBITORS
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Compounds of formula (I): wherein; R1 is hydrogen or C1-6alkyl;R2 is hydrogen, C1-6alkyl, perhalomethylC0-5alkyl-O—, or C1-6alkoxy;R3 is hydrogen, C1-6alkyl, or C1-6alkoxyC1-6alkyl;R4 is hydrogen, C1-6alkyl, perhalomethylC1-6alkyl; or unsubstituted C3-6cycloalkylC1-6 alkyl;A is C—R5 or N;B is C—R6 or N;D is C—R7 or N;with the proviso that at least one of A, B, and D, is N;R5 is hydrogen or C1-6alkyl;R6 is hydrogen or C1-6alkyl;R7 is hydrogen, C1-6alkyl, C1-6alkoxy, or hydroxy;R8 is hydrogen or C1-6alkyl, with the proviso that one of R4 and R8 is hydrogen;R9 is hydrogen or hydroxy;R10 is hydrogen or C1-6alkyl; and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.
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Paragraph 0338; 0339; 0340
(2015/07/02)
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- Photochromism of new unsymmetrical diarylethenes based on the hybrid of azaindole and thiophene moieties
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A new class of photochromic diarylethenes with both azaindole and thiophene moieties were synthesized to investigate the effects of the substituents on their photochromic behaviors, and their structures were determined by single crystal X-ray diffraction
- Sun, Zhiyuan,Li, Hui,Liu, Gang,Fan, Congbin,Pu, Shouzhi
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- Synthesis and photochromism of novel unsymmetrical diarylethenes with an azaindole unit
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A new class of unsymmetrical photochromic diarylethenes with an azaindole moiety has been firstly synthesized. Their properties, including photochromism, crystal structure, as well as fluorescence, were investigated systematically. The azaindole was conne
- Sun, Zhiyuan,Li, Hui,Pu, Shouzhi,Liu, Gang,Chen, Bing
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supporting information
p. 2471 - 2475
(2014/05/06)
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- 2 - (AZAINDOL- 2 -YL) BENZ IMIDAZOLES AS PAD4 INHIBITORS
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Compounds of formula (I) wherein; R1 is hydrogen or C1-6alkyl; R2 is hydrogen, C1-6alkyl, perhalomethylC0-5alkyl-O-, or C1-6alkoxy; R3 is hydrogen, C1-6alkyl, or C1-6alkoxyC1-6alkyl; R4 is hydrogen, C1-6alkyl, perhalomethylC1-6alkyl; or unsubstituted C3-6cycloalkylC1-6alkyl; A is C-R5 or N; B is C-R6 or N; D is C-R7 or N; with the proviso that at least one of A, B, and D, is N; R5 is hydrogen or C1-6alkyl; R6 is hydrogen or C1-6alkyl; R7 is hydrogen, C1-6alkyl, C1-6alkoxy, or hydroxy; R8 is hydrogen or C1-6alkyl, with the proviso that one of R4 and R8 is hydrogen; R9 is hydrogen or hydroxy; R10 is hydrogen or C1-6alkyl; and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.
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Page/Page column 45
(2014/02/16)
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- Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases
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Optimization of a 7-azaindole-3-acetic acid CRTh2 receptor antagonist chemotype derived from high throughput screening furnished a highly selective compound NVP-QAV680 with low nM functional potency for inhibition of CRTh2 driven human eosinophil and Th2 lymphocyte activation in vitro. The molecule exhibited good oral bioavailability in the rat, combined with efficacy in rodent CRTh2-dependent mechanistic and allergic disease models and was suitable for clinical development.
- Sandham, David A.,Arnold, Nicola,Aschauer, Heinrich,Bala, Kamlesh,Barker, Lucy,Brown, Lyndon,Brown, Zarin,Budd, David,Cox, Brian,Docx, Cerys,Dubois, Gerald,Duggan, Nicholas,England, Karen,Everatt, Brian,Furegati, Marcus,Hall, Edward,Kalthoff, Frank,King, Anna,Leblanc, Catherine J.,Manini, Jodie,Meingassner, Josef,Profit, Rachael,Schmidt, Alfred,Simmons, Jennifer,Sohal, Bindi,Stringer, Rowan,Thomas, Matthew,Turner, Katharine L.,Walker, Christoph,Watson, Simon J.,Westwick, John,Willis, Jennifer,Williams, Gareth,Wilson, Caroline
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supporting information
p. 6582 - 6591
(2013/10/22)
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- Azaindole-1,2,3-triazole conjugate as selective fluorometric sensor for dihydrogenphosphate
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A new receptor 1 has been designed and synthesized. The open cavity of 1 selectively recognizes H2PO4- over a series of other anions in CH3CN containing 0.01% DMSO by exhibiting a ratiometric change in emission.
- Ghosh, Kumaresh,Kar, Debasis,Joardar, Soumen,Sahu, Debashis,Ganguly, Bishwajit
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p. 16144 - 16151
(2013/09/12)
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- Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H- pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4- (phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones
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Several members of the quinazoline class of known tyrosine kinase inhibitors are approved anticancer agents, often showing selectivity for receptors of the HER/ErbB-family. Combining structural elements of this class with the bisindolylmethanone-structure
- Beckers, Thomas,Sellmer, Andreas,Eichhorn, Emerich,Pongratz, Herwig,Sch?chtele, Christoph,Totzke, Frank,Kelter, Gerhard,Krumbach, Rebekka,Fiebig, Heinz-Herbert,B?hmer, Frank-D.,Mahboobi, Siavosh
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experimental part
p. 125 - 136
(2012/02/16)
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- Design, synthesis and biological evaluation of new thalidomide analogues as TNF-α and IL-6 production inhibitors
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Several thalidomide analogues were synthesized and compared to thalidomide and its more active analogue, lenalidomide, for their ability to inhibit the production of the pro-inflammatory cytokine tumour necrosis factor (TNF)-α and interleukin (IL)-6 by LPS-activated peripheral blood mononuclear cells (PBMCs). Among these compounds, two analogues containing sulfonyl group displayed interesting downregulation of TNF-α and IL-6 production.
- Chaulet, Charlotte,Croix, Cécile,Alagille, David,Normand, Sylvain,Delwail, Adriana,Favot, Laure,Lecron, Jean-Claude,Viaud-Massuard, Marie-Claude
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scheme or table
p. 1019 - 1022
(2011/03/21)
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- 7-Azaindole-3-acetic acid derivatives: Potent and selective CRTh2 receptor antagonists
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High throughput screening identified a 7-azaindole-3-acetic acid scaffold as a novel CRTh2 receptor antagonist chemotype, which could be optimised to furnish a highly selective compound with good functional potency for inhibition of human eosinophil shape change in whole blood and oral bioavailability in the rat.
- Sandham, David A.,Adcock, Claire,Bala, Kamlesh,Barker, Lucy,Brown, Zarin,Dubois, Gerald,Budd, David,Cox, Brian,Fairhurst, Robin A.,Furegati, Markus,Leblanc, Catherine,Manini, Jodie,Profit, Rachael,Reilly, John,Stringer, Rowan,Schmidt, Alfred,Turner, Katharine L.,Watson, Simon J.,Willis, Jennifer,Williams, Gareth,Wilson, Caroline
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scheme or table
p. 4794 - 4798
(2010/05/18)
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- PYRIDINONYL PDK1 INHIBITORS
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The present invention provides pyridinonyl PDKl inhibitors and methods of treating cancer using the same.
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Page/Page column 102
(2008/06/13)
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- Azaindolylidene derivatives as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
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The present invention is directed to compounds of the formula or pharmaceutically acceptable salts, prodrug, solvate or optical isomer thereof, pharmaceutical compositions containing same and use thereof for treating diseases linked to disregulated cell p
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Page/Page column 36
(2010/11/27)
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- PYRIMIDINYL SUBSTITUTED FUSED-PYRROLYL COMPOUNDS USEFUL IN TREATING KINASE DISORDERS
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The present invention provides pyrimidinyl substituted fused-pyrrolyl compounds of Formula (I) and pharmaceutical compositions comprising the compounds and methods of synthesis and use thereof. The compounds are kinase inhibitors useful in treating or ameliorating a kinase mediated, angiogenesis-mediated or hyperproliferative disorder. The invention thus also provides a therapeutic or prophylactic method of use for the compounds and/or pharmaceutical compositions to treat such disorders.
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Page/Page column 61
(2010/11/30)
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- Synthesis of 2-amino-4-(7-azaindol-3-yl)pyrimidines as cyclin dependent kinase 1 (CDK1) inhibitors
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A novel series of 2-amino-4-(7-azaindol-3-yl)pyrimidines was discovered as cyclin dependent kinase 1 (CDK1) inhibitors. The core structure was synthesized via Pd(II) catalyzed coupling reaction. A number of analogues showed good potency for CDK1 and exhib
- Huang, Shenlin,Li, Ronghua,Connolly, Peter J.,Emanuel, Stuart,Middleton, Steven A.
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p. 4818 - 4821
(2007/10/03)
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- Design, synthesis, and biological activity of novel factor Xa inhibitors: Improving metabolic stability by S1 and S4 ligand modification
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Serine protease factor xa (fXa) inhibitor 1 showed good ex vivo anti-fXa activity upon oral administration in rats. However, it has been revealed that 1 had low metabolic stability against human liver microsomes. To improve the metabolic stability, we att
- Komoriya, Satoshi,Kobayashi, Shozo,Osanai, Ken,Yoshino, Toshiharu,Nagata, Tsutomu,Haginoya, Noriyasu,Nakamoto, Yumi,Mochizuki, Akiyoshi,Nagahara, Takayasu,Suzuki, Makoto,Shimada, Takashi,Watanabe, Kengo,Isobe, Yumiko,Furugoori, Taketoshi
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p. 1309 - 1330
(2007/10/03)
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- Reaction of bromomethylazoles and tosylmethyl isocyanide. A novel heterocyclization method for the synthesis of the core of marine alkaloids variolins and related azolopyrimidines
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A novel and efficient synthesis of the pyrido[3′,2′:4,5] pyrrolo[1,2-c]pyrimidine system, the heterocyclic core of the variolin family of marine alkaloids, is described. The route involves the reaction of 3-bromo-2-(bromomethyl)pyrrolo[2,3-b]pyridine and tosylmethyl isocyanide (TosMIC) under phase-transfer conditions. This unprecedented reaction was also used to synthesize a series of new methoxycarbonyl azolopyrimidines by reaction of TosMIC with bromomethylindoles, bromomethylbenzimidazole, and bromomethylpyrazole. Hydrolysis and decarboxylation of 5-bromo-7- methoxycarbonylpyrido[3′,2′:4,5]pyrrolo[1,2-c]pyrimidine obtained by this heterocyclization process and installation of the pyrimidine moiety in the C5 position open an alternative approach to complete a total synthesis of variolin B.
- Mendiola, Javier,Baeza, Alejandro,Alvarez-Builla, Julio,Vaquero, Juan J.
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p. 4974 - 4983
(2007/10/03)
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- Syntheses, structures, and electroluminescence of new blue/green luminescent chelate compounds: Zn(2-py-in)2(THF), BPh2(2-py-in), Be(2-py- in)2, and BPh2(2-py-aza) [2-py-in = 2-(2-pyridyl)indole; 2-py-aza = 2-(2
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Four novel blue/green luminescent compounds, Zn(2-py-in)2(THF) (1), BPh2(2-py-in) (2), Be(2-py-in)2 (3), and BPh2(2-py-aza) (4), where 2-py-in = 2-(2-pyridyl)indole and 2-py-aza = 2-(2-pyridyl)-7-azaindole, have
- Liu, Shi-Feng,Wu, Qingguo,Schmider, Hartmut L.,Aziz, Hany,Hu, Nan-Xing,Popovic, Zoran,Wang, Suning
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p. 3671 - 3678
(2007/10/03)
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- Synthesis of 2-substituted-1H-pyrrolo[2,3-b]pyridines: Preparation of 7-azaolivacine analogue and 7-azaindolopyridopyrimidine derivatives
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2-Substituted-1H-pyrrolo(2,3-b]pyridines have been prepared from 7-azaindole by lithiation followed by addition of various electrophiles. A 7-azaolivacine analogue and pyrido[3'2':4,5]pyrrolo[1,2-c]pyrido[3,2-d]pyrimidine have also been prepared.
- Desarbre, Eric,Coudret, Sandrine,Meheust, Cecile,Merour, Jean-Yves
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p. 3637 - 3648
(2007/10/03)
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- SUBSTITUTED PYROLLO-FUSED 6 MEMBERED HETROCYCLES AS ANGIOTENSIN II ANTAGONISTS
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Substituted pyrrolo-fused 6-membered heterocycles of structural formula: STR1 wherein A, B, C, and D are independently carbon atoms or nitrogen atoms are angiotensin II antagonists useful in the treatment of hypertension and congestive heart failure.
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