- New 1-hydroxy-1,1-bisphosphonates derived from 1H-Pyrazolo[3,4-b]pyridine: Synthesis and characterization
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A number of 1H-pyrazolo[3,4-b]pyridine derivatives, starting from 2-chloro-3-formyl pyridine, was synthesized to obtain new 1- hydroxybisphosphonates, a class of compounds with potential biological interest. Spectroscopic data were used to characterize all compounds and to identify N-1 and N-2 regioisomers, and mono- and bisphosphonates derivatives. X-ray diffractometry studies of compound 7a confirmed the proposed structure.
- Teixeira, Fa?tima C.,Lucas, Carla,Curto, M. Joa?o M.,Neves,Duarte, M. Teresa,Andre?, Va?nia,Teixeira, Anto?nio P. S.
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- Novel Bisphosphonates Derived from 1H-Indazole, 1H-Pyrazolo[3,4-b]Pyridine, and 1H-Pyrazolo[3,4-b]Quinoline
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Novel tetraethyl ethylene-1,1-bisphosphonate esters derived from 1H-indazole, 1H-pyrazolo[3,4-b]pyridine, and 1H-pyrazolo[3,4-b]quinoline were synthesized by a Michael addition reaction of tetraethyl ethylidene-1,1-bisphosphonate with the corresponding heterocycle, using conventional heating and microwave-assisted methods. The microwave-assisted method provides shorter reaction times and better yields. The hydrolysis of bisphosphonates afforded the corresponding bisphosphonic acids or salt, using concentrated hydrochloric acid or TMSBr/collidine, respectively. All new compounds were fully characterized, and their structures were assigned using 1H, 31P, and 13C NMR and IR spectroscopies and mass spectrometry. The molecular structure of compound 6 was confirmed by X-ray diffraction studies.
- Teixeira, Ftima C.,Lucas, Carla,Curto, M. Joo M.,Teixeira, Antnio P. S.,Duarte, M. Teresa,Andr, Vnia
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Read Online
- A novel copper-catalyzed, hydrazine-free synthesis of N-1 unsubstituted 1H-indazoles using stable guanylhydrazone salts as substrates
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A CuI-catalyzed, hydrazine-free transformation of 2-(2-bromoarylidene)guanylhydrazone hydrochlorides using Cs2CO3 as a base and DMEDA as a ligand at 120 °C for 5 h delivers substituted 1H-indazoles with yields up to 75%. The C,N double bond configuration of the substrates was determined by NMR experiments and quantum chemical calculations. The reaction mechanism was studied using quantum chemical calculations.
- Rekowski, Szymon P.,Kroener, Bettina K.,Kathuria, Deepika,Wani, Aabid A.,Chourasiya, Sumit S.,Conrad, Jürgen,Bharatam, Prasad V.,Frey, Wolfgang,Beifuss, Uwe
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- INHIBITORS OF CYCLIN DEPENDNT KINASE 7 (CDK7)
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The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
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Paragraph 505
(2018/02/28)
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- "On Water" Direct C-3 Arylation of 2H-Pyrazolo[3,4-b]pyridines
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An "on water" palladium-catalyzed direct (hetero)arylation of 2H-pyrazolo[3,4-b]pyridines has been developed. The reactions proceeds smoothly with at low catalytic loading at low temperature providing the C3 (hetero)arylated products in good to excellent isolated yields. Free NH 3-arylated 7-azaindazoles were also prepared by simple cleavage of the N-protected groups.
- Faarasse, Soukaina,El Kazzouli, Sa?d,Naas, Mohammed,Jouha, Jabrane,Suzenet, Franck,Guillaumet, Gérald
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p. 12300 - 12306
(2017/12/08)
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- PYRIMIDINE AND TRIAZINE DERIVATIVES AND THEIR USE AS AXL INHIBITORS
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Compounds of the general formula(I): (I) processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
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- Design, synthesis and evaluation of 7-azaindazolyl-indolyl-maleimides as glycogen synthase kinase-3β (GSK-3β) inhibitors
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A series of 7-azaindazolyl-indolyl-maleimides were designed, synthesized and evaluated for their GSK-3β inhibitory activity. Most compounds exhibited potent activity against GSK-3β. Among them, compounds 17a, 17b, 17g, 17i, 29a and 30 significantly reduced Aβ-induced Tau hyperphosphorylation, showin;g the inhibition of GSK-3β at the cell level. Preliminary structure-activity relationships were discussed based on the experimental data obtained.
- Ye, Qing,Shen, Yanhong,Zhou, Yubo,Lv, Dan,Gao, Jianrong,Li, Jia,Hu, Yongzhou
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p. 361 - 371
(2013/10/01)
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- INHIBITORS OF INFLUENZA VIRUSES REPLICATION
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Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
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Page/Page column 126
(2012/06/30)
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- Synthesis and biological evaluation of imidazo[4,5-b]pyridine and 4-heteroaryl-pyrimidine derivatives as anti-cancer agents
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A series of N-phenyl-imidazo[4,5-b]pyridin-2-amines, 4-indazolyl-N- phenylpyrimidin-2-amines and N-phenyl-4-pyrazolo[3,4-b]pyridin-pyrimidin-2- amines have been synthesized. Their anti-proliferative activities were tested in HCT-116 human colon carcinoma and MCF-7 breast carcinoma cell lines. Many exhibited potent anti-proliferative and CDK9 inhibitory activities. A lead compound 18b demonstrated the ability to reduce the level of Mcl-1 anti-apoptotic protein, to activate caspase 3/7 and induce cancer cell apoptosis.
- Lukasik, Pawel M.,Elabar, Sherifa,Lam, Frankie,Shao, Hao,Liu, Xiangrui,Abbas, Abdullah Y.,Wang, Shudong
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p. 311 - 322
(2013/01/15)
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- INDAZOLEPROPIONIC ACID AMIDE COMPOUND
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Disclosed is a compound which is useful in preventing and treating cardiac arrhythmia such as atrial fibrillation. A compound represented by formula (1) or a pharmaceutically acceptable salt of the same. In formula (1), ring X represents benzene or pyridine; R1 represents an optionally substituted alkyl group; R2 represents an optionally substituted aryl group, an optionally substituted heterocyclic group, an optionally substituted arylalkyl group or an optionally substituted heterocyclic group-substituted alkyl group; R3, R4, R5, R6, R7, R8 and R9 represent each hydrogen or an alkyl group, provided that R3 and R5 may be bonded to each other to form, together with the carbon atom adjacent thereto, a cycloalkyl group; and m represents 0 or 1.
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Page/Page column 28
(2012/02/01)
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- SOLUBLE GUANYLATE CYCLASE ACTIVATORS
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A compound of Formula (I): or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate ("cGMP") and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I , or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the above mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of Formula (I) or a pharmaceutically acceptable salt thereof
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Page/Page column 98
(2011/12/14)
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- Synthesis and evaluation of novel 7-azaindazolyl-indolyl-maleimide derivatives as antitumor agents and protein kinase C inhibitors
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A series of novel 7-azaindazolyl-indolyl-maleimides were synthesized and evaluated for their antiproliferative activity in vitro against various human cancer cell lines and protein kinase C inhibitory activity. Compounds 8a-c, 8e and 14a were the most pro
- Ye, Qing,Cao, Ji,Zhou, Xinglu,Lv, Dan,He, Qiaojun,Yang, Bo,Hu, Yongzhou
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scheme or table
p. 4763 - 4772
(2009/11/30)
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- MULTIKINASE INHIBITOR
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It is intended to provide a compound represented by the formula (1): [wherein Ar is an arylene group to be attached selected from the following formula (2): (wherein * represents a binding site to a nitrogen atom and ** represents a binding site to T); T represents -(O)n-R; R represents a C1-C6 alkyl group or the like; n represents 0 or 1; X represents O or the like; R2, R3 and R4 are independently selected from a hydrogen atom or C1-C3 alkyl; or R2 and R3 may join together with an urea structure containing the nitrogen atoms to which they bind to form a 5- or 6-membered heterocycle; Y represents CH or N], or a pharmaceutically acceptable salt thereof or a prodrug thereof and a pharmaceutical composition containing the same.
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Page/Page column 32
(2008/12/05)
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- HIV reverse transcriptase inhibitors
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Compounds having the structure: are HIV reverse transcriptase inhibitors, wherein A, X, Y, Z, R1 and R2 are defined herein. The compounds and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
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Page/Page column 56
(2010/11/25)
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- The Semmler-Wolff Aromatization and Schmidt Reaction Applied to Some Pyridopyrazolobenzotriazines
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Pyridopyrazolobenzotriazin-4(1H)ones were transformed via their oximes in a Semmler-Wolff aromatization process in the tetracyclic heteroaromatic amines 4 or by Schmidt reaction into a mixture of the same amine 4 and a ring enlarg
- Kocevar, Marijan,Stanovnik, Branko,Tisler, Miha
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p. 597 - 604
(2007/10/02)
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- Pyrazolopyridines. The Preparation of 1-Protected-1H-pyrazolopyridines and Attempts to Remove the 1-Substituent. Some Reactions of 1-Benzyl-1H-pyrazolopyridine and its 7-Oxide
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1-Protected-1H-pyrazolopyridines and -1H-pyrazolopyridin-6(7H)-ones have been obtained from 1-substituted-5-aminopyrazoles , and the removal of the protecting groups has been investigated.Cyclisation of 1-substituted-5-aminopyrazoles with ethyl acetoacetate under acidic conditions or of the β-aminopropionic acid derivative (19) under the same conditions gave only the 1H-pyrazolopyridin-6(7H)-one isomer .N-Oxidation of 1-benzyl-1H-pyrazolopyridine (4) gave the 7-oxide (21) which yielded (20) and the less usual β-substitution product (22) with acetic anhydride.Nitration of either (4) or (21) gave only substitution at the para-position of the 1-benzyl substituent, but bromination or chlorination gave substitution at the 3-position of the heterocycle.
- Dorgan, Roderick J.J.,Parrick, John,Hardy, Christopher R.
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p. 938 - 942
(2007/10/02)
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