7126-57-0Relevant articles and documents
CRYSTAL FORM OF TRICYCLIC COMPOUNDS AND APPLICATION THEREOF
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Paragraph 0039-0043, (2020/09/18)
本發明公開了式(I)所示化合物的A晶型及B晶型，及其在製備治療HBV相關疾病藥物中的應用。 The invention discloses “A”crystal form and“B”crystal form of a compound represented by formula (I) and an application thereof in a preparation of a medicament for treating HBV-related diseases.
Regioselective Formylation of Pyrrole-2-Carboxylate: Crystalline Vilsmeier Reagent vs Dichloromethyl Alkyl Ether
Warashina, Takuya,Matsuura, Daisuke,Sengoku, Tetsuya,Takahashi, Masaki,Yoda, Hidemi,Kimura, Yoshikazu
, p. 614 - 618 (2018/10/25)
New preparations of crystalline Vilsmeier reagent (VR) and dichloromethyl propyl or butyl ether were developed. The methods are environmentally benign and applicable to large-scale synthesis. Formylations of 1H-pyrrole-2-carboxylates were achieved with th
Identification of azepinone fused tetracyclic heterocycles as new chemotypes with protein kinase inhibitory activities
Psarra, Vassiliki,Fousteris, Manolis A.,Hennig, Lothar,Bantzi, Marina,Giannis, Athanassios,Nikolaropoulos, Sotiris S.
supporting information, p. 2376 - 2385 (2016/04/26)
The design and synthesis of small tetracyclic heterocycles which bear two new regioisomeric 2-carboxyethyl-1H-pyrrole-annulated indoloazepinone scaffolds is described. An azepinone motif, which is inherent in the structures of many well studied protein kinase inhibitors, serves as prominent structural feature of the new compounds. Concise access to the new regioisomeric tetracyclic derivatives was accomplished through amide coupling of appropriate pyrrole and indole precursors followed by an intramolecular Heck coupling reaction of the intermediate amide conjugates. Preliminary evaluation of newly synthesized tetracyclic molecules against a panel of protein kinases indicated their inhibitory activities and revealed promising selectivity profiles. The new compounds displayed no significant antiproliferative activity against MCF-7 cancer cells. Interestingly, derivative 19a exhibited selective TAK1 kinase inhibitory activity and figures as a promising chemotype for the discovery of new TAK1 inhibitors.
Synthesis of new tetracyclic paullone derivatives as potential CDK inhibitors
Koutsandrea, Efthimia G.,Fousteris, Manolis A.,Nikolaropoulos, Sotiris S.
, p. 169 - 179 (2013/01/16)
Synthetic efforts towards new tetracyclic heterocycles bearing the pyrrolo[2',3':5,6]azepino[4,3- b ] indol-4(11 H )-one core are described. Synthesized tetracyclic compounds are the first analogs, structurally related to protein kinase inhibitors paullones which incorporate an azepinone, an indole and a pyrrole ring. The synthetic approach involves palladium mediated intramolecular Heck coupling as a key step.
PHARMACEUTICAL COMPOSITION CONTAINING FUSED HETERO-RING DERIVATIVE
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Page/Page column 99, (2012/06/18)
The present invention provides a compound which indicates a histamine H4 receptor modulating activity.A compound represented by a formula (I): wherein A ring is a ring represented by the following formula: wherein R1 is substituted or unsubstituted alkyl, etc., W is -O-, etc., n is an integer of 0 to 6; X is N(R7)- or -O-; R7 is hydrogen, substituted or unsubstituted alkyl, etc.; Y is-C(R8)= or -N=; R8 is hydrogen, substituted or unsubstituted alkyl, etc.; Z is =O, =S, etc.; B ring is a ring represented by the following formula wherein R10 is each independently substituted or unsubstituted alkyl, halogen, hydroxy, substituted or unsubstituted alkyloxy, substituted or unsubstituted amino; R11, R12a and R12b are each independently hydrogen or substituted or unsubstituted alkyl, etc.; p is an integer of 0 to 4, or its pharmaceutically acceptable salt, or a solvate thereof.The present invention provides a compound which indicates a histamine H4 receptor modulating activity. A compound represented by a formula (I): wherein A ring is a ring represented by the following formula: wherein R 1 is substituted or unsubstituted alkyl, etc., W is -O-, etc., n is an integer of 0 to 6; X is N(R 7 )- or -O-; R 7 is hydrogen, substituted or unsubstituted alkyl, etc.; Y is-C(R 8 )= or -N=; R 8 is hydrogen, substituted or unsubstituted alkyl, etc.; Z is =O, =S, etc.; B ring is a ring represented by the following formula wherein R 10 is each independently substituted or unsubstituted alkyl, halogen, hydroxy, substituted or unsubstituted alkyloxy, substituted or unsubstituted amino; R 11 , R 12a and R 12b are each independently hydrogen or substituted or unsubstituted alkyl, etc.; p is an integer of 0 to 4, or its pharmaceutically acceptable salt, or a solvate thereof.
Dihydroindolone compounds, a process for their preparation and pharmaceutical compositions containing them
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Page/Page column 6, (2011/02/26)
Compounds of formula (I): wherein: m and n represent 1 or 2,A represents a pyrrolyl group,X represents a C(O), S(O) or SO2 group,R1 and R2 represent an alkyl group or, together with the nitrogen atom carrying them, form a heterocyclic group,R3 and R4, together with the atoms carrying them, form a heterocyclic group,R5 represents a hydrogen atom or an alkyl group,R6 represents a hydrogen atom or a halogen atom. Medicinal products containing the same which are useful in treating cancer.
Synthesis, biological evaluation and molecular modelling of N-heterocyclic dipeptide aldehydes as selective calpain inhibitors
Jones, Matthew A.,Morton, James D.,Coxon, James M.,McNabb, Stephen B.,Lee, Hannah Y.-Y.,Aitken, Steven G.,Mehrtens, Janna M.,Robertson, Lucinda J.G.,Neffe, Axel T.,Miyamoto, Shigeru,Bickerstaffe, Roy,Gately, Karl,Wood, Jacqueline M.,Abell, Andrew D.
, p. 6911 - 6923 (2008/12/22)
A series of N-heterocyclic dipeptide aldehydes 4-13 have been synthesised and evaluated as inhibitors of ovine calpain 1 (o-CAPN1) and ovine calpain 2 (o-CAPN2). 5-Formyl-pyrrole 9 (IC50 values of 290 and 25 nM against o-CAPN1 and o-CAPN2, respectively) was the most potent and selective o-CAPN2 inhibitor, displaying >11-fold selectivity. The amino acid sequences of o-CAPN1 and o-CAPN2 have been determined. Because of the lack of available structural information on the ovine calpains, in silico homology models of the active site cleft of o-CAPN1 and o-CAPN2 were developed based on human calpain 1 (h-CAPN1) X-ray crystal structure (PDB code 1ZCM). These models were used to rationalise the observed SAR for compounds 4-13 and the selectivity observed for 9. The o-CAPN2 selective inhibitor 9 (CAT0059) was assayed in an in vitro ovine lens culture system and shown to successfully protect the lens from calcium-induced opacification.
The intramolecular photometathesis of pyrroles
Elliott, Luke D.,Berry, Malcolm,Orr-Ewing, Andrew J.,Booker-Milburn, Kevin I.
, p. 3078 - 3079 (2007/10/03)
UV irradiation of various electron deficient pyrrole derivatives induces a novel methathesis sequence resulting in selective cleavage of the 2,3-pyrrole bond. The overall sequence has been shown to proceed by two discrete wavelength-dependent steps involving sequential [2+2] cyclobutane formation followed by photochemically mediated retro-[2+2] to the products. Copyright
5-sulfonamido-substituted indolinone compounds as protein kinase inhibitors
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Page/Page column 16, (2010/02/08)
The present invention relates to 5-sulfonamido substituted indolinones that modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
Sulfonamide substituted indolinones as inhibitors of DNA dependent protein kinase (DNA-PK)
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Page 12, (2010/02/10)
The present invention relates generally to the field of radiosensitizing agents which are capable of enhancing radiotherapy by inhibiting DNA-PK (DNA-protein kinase). In particular, it relates to sulfonamide substituted indolinones which inhibit DNA-PK.
