cas 4649-09-6, 7-AZAINDOLE-3-CARBOXALDEHYDE

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Synthesis of 7-azaindole based carbohydrazides and 1,3,4-oxadiazoles; Antioxidant activity, α-glucosidase inhibition properties and docking study
In this current work, 7-azaindole based 1,3,4-oxadiazoles have been successfully prepared by treatment of 3-(hydrazonomethyl)-7-azaindole with the different acyl chlorides or acetic anhydrides to give the corresponding carbohydrazides, followed by iodine mediated synthetic protocol in order to afford the corresponding 2,5-disubstituted 1,3,4-oxadiazoles. The full characterization data of the novel compounds were obtained by utilizing 1H NMR, 13C NMR, FT-IR, high-resolution mass spectrometry and single crystal X-ray diffraction techniques. The antioxidant activity and α-glucosidase inhibition potential of the prepared compounds are examined by in vitro assays. The targeted hydrazide linked 7-azaindoles and their corresponding cyclized form 1,3,4-oxadiazoles exhibited inhibitory potential with IC50 values ranges between 0.46 and 24.92 mM. Plausible binding mode and interaction of ligands with α-glucosidase enzyme have been studied by molecular docking, supporting the experimental results.
?ahin, Engin,Cebeci, Fatma,Izgi, Samet,Kandemir, Hakan,Koca, Mehmet Serdar,Sengul, Ibrahim F.
(2022)
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Azaindole-BODIPYs: Synthesis, fluorescent recognition of hydrogen sulfate anion and biological evaluation
The synthesized and sensing capability of two novel azaindole substituted mono and distyryl BODIPY dyes against bisulfate anion were reported. Structural characterizations of the targeted compounds were conducted by using matrix-assisted laser desorption/
Ke?an, Gürkan,Topalo?lu, Burcu,?zcan, Emrah,Kazan, Hasan Hüseyin,E?ik, Esra Tanr?verdi,?enkuytu, Elif,Sengul, Ibrahim F.,Kandemir, Hakan,?o?ut, Bünyemin
p. 73 - 82
(2019)
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Synthesis and biological evaluation of pyrrolo[2,3-b]pyridine analogues as antiproliferative agents and their interaction with calf thymus DNA
A series of thirty two novel pyrrolo[2,3-b]pyridine analogues synthesized, characterized (1H NMR, 13C NMR and MS) and cytotoxic evaluation of these molecules carried out over a panel of three human cancer cell lines including A549 (l
Narva, Suresh,Chitti, Surendar,Bala, Bhaskara Rao,Alvala, Mallika,Jain, Nishant,Kondapalli, Venkata Gowri Chandra Sekhar
p. 220 - 231
(2016)
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Synthesis and evaluation of 7-azaindole derivatives bearing benzocycloalkanone motifs as protein kinase inhibitors
Protein kinases are important drug targets, especially in the area of oncology. This paper reports the synthesis and biological evaluation of new 7-azaindole derivatives bearing benzocycloalkanone motifs as potential protein kinase inhibitors. Four compounds 8g, 8h, 8i, and 8l were discovered to inhibit cyclin-dependent kinase 9 (CDK9/CyclinT) and/or Haspin kinase in the micromolar to nanomolar range. 8l was identified as the most potent Haspin inhibitor (IC50 = 14 nM), while 8g and 8h acted as dual inhibitors of CDK9/CyclinT and Haspin. These novel compounds constitute a promising starting point for the discovery of dual protein kinase inhibitors that have potential to be developed as anticancer agents, since both CDK9/CyclinT and Haspin are considered to be drug targets in oncology.
Bach, Stéphane,Beteck, Richard M.,Josselin, Béatrice,Legoabe, Lesetja J.,Petzer, Jacobus P.,Qhobosheane, Malikotsi A.,Ruchaud, Sandrine
(2020)
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Radiosynthesis and evaluation of 18F-labeled dopamine D4-receptor ligands
Introduction: The dopamine D4 receptor (D4R) has attracted considerable attention as potential target for the treatment of a broad range of central nervous system disorders. Although many efforts have been made to improve the performance of putative radioligand candidates, there is still a lack of D4R selective tracers suitable for in vivo PET imaging. Thus, the objective of this work was to develop a D4-selective PET ligand for clinical applications. Methods: Four compounds based on previous and new lead structures were prepared and characterized with regard to their D4R subtype selectivity and predicted lipophilicity. From these, 3-((4-(2-fluorophenyl)piperazin-1-yl)methyl)-1H-pyrrolo[2,3-b]pyridine I and (S)-4-(3-fluoro-4-methoxybenzyl)-2-(phenoxymethyl)morpholine II were selected for labeling with fluorine-18 and subsequent evaluation by in vitro autoradiography to assess their suitability as D4 radioligand candidates for in vivo imaging. Results: The radiosynthesis of [18F]I and [18F]II was successfully achieved by copper-mediated radiofluorination with radiochemical yields of 7% and 66%, respectively. The radioligand [18F]II showed specific binding in areas where D4 expression is expected, whereas [18F]I did not show any uptake in distinct brain regions and exhibited an unacceptable degree of non-specific binding. Conclusions: The compounds studied exhibited high D4R subtype selectivity and logP values compatible with high brain uptake, but only ligand [18F]II showed low non-specific binding and is therefore a good candidate for further evaluation. Advances in knowledge: The discovery of new lead structures for high-affinity D4 ligands opens up new possibilities for the development of suitable PET-radioligands. Implications for patient: PET-imaging of dopamine D4-receptors could facilitate understanding, diagnosis and treatment of neuropsychiatric and neurodegenerative diseases.
Willmann, Michael,Ermert, Johannes,Prante, Olaf,Hübner, Harald,Gmeiner, Peter,Neumaier, Bernd
p. 43 - 52
(2020/08/03)

COMPOUNDS AND METHODS OF USE
This present disclosure relates to compounds with ferroptosis inducing activity, a method of treating a subject with cancer with the compounds, and combination treatments with a second therapeutic agent.
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Page/Page column 76; 77

(2021/03/05)

A 7 - azaindole -3 - formaldehyde synthetic method
The invention discloses a 7 - azaindole - 3 - formaldehyde synthetic method, comprises the following steps: the 7 - aza indole dissolved in the ethanol solution of propionic acid, heating, adding hexamethylenetetramine, under the conditions of the catalysis of the catalyst obtained by the reaction of 7 - azaindole - 3 - formaldehyde. The application of the synthesis method adopts the one-pot synthesis, without intermediate purification step, the reaction conversion is high, a high degree of selectivity. And the mild reaction conditions, low cost, and is suitable for large-scale industrial production.
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Paragraph 0021-0026; 0033-0054

(2019/03/28)

Discovery of Potent, Selective, and Brain-Penetrant 1 H-Pyrazol-5-yl-1 H-pyrrolo[2,3- b]pyridines as Anaplastic Lymphoma Kinase (ALK) Inhibitors
Anaplastic lymphoma kinase (ALK), a member of the receptor tyrosine kinase family, is predominantly expressed in the brain and implicated in neuronal development and cognition. However, the detailed function of ALK in the central nervous system (CNS) is s
Fushimi, Makoto,Fujimori, Ikuo,Wakabayashi, Takeshi,Hasui, Tomoaki,Kawakita, Youichi,Imamura, Keisuke,Kato, Tomoko,Murakami, Morio,Ishii, Tsuyoshi,Kikko, Yorifumi,Kasahara, Maki,Nakatani, Atsushi,Hiura, Yuto,Miyamoto, Maki,Saikatendu, Kumar,Zou, Hua,Lane, Scott Weston,Lawson, J. David,Imoto, Hiroshi
p. 4915 - 4935
(2019/05/22)

Synthesis of 3-Formylindoles via Electrochemical Decarboxylation of Glyoxylic Acid with an Amine as a Dual Function Organocatalyst
A new method for 3-formalytion of indoles has been developed through electrochemical decarboxylation of glyoxylic acid with the amine as a dual function organocatalyst. The amine facilitated both the electrochemical decarboxylation and the nucleophilic reaction efficiently, whose loading can be as low as 1 mol %. This protocol has a broad range of functional group tolerance under ambient conditions. The gram-scale experiment has shown great potential in the synthetic application of this strategy.
Lin, Dian-Zhao,Huang, Jing-Mei
supporting information
p. 5862 - 5866
(2019/08/26)

Preparation method of 7-azaindole-3-formaldehyde
The invention discloses a preparation method of 7-azaindole-3-formaldehyde. The method comprises the following steps: dissolving 7-azaindole in an organic solvent, adding lithium formic anhydride salt, and under the catalysis of a catalyst, performing a reaction to prepare 7-azaindole-3-formaldehyde. The method adopts a one-step reaction and a binary catalyst system, and is high in reaction conversion rate and selectivity. The preparation method is mild in reaction conditions and low in reaction cost and has bright industrial production prospects.
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Paragraph 0021; 0023; 0024; 0025; 0027; 0029; 0031

(2017/08/25)

Discovery of (S)-1-(1-(Imidazo[1,2- a ]pyridin-6-yl)ethyl)-6-(1-methyl-1 H -pyrazol-4-yl)-1 H -[1,2,3]triazolo[4,5- b ]pyrazine (Volitinib) as a Highly Potent and Selective Mesenchymal-Epithelial Transition Factor (c-Met) Inhibitor in Clinical Development for Treatment of Cancer
HGF/c-Met signaling has been implicated in human cancers. Herein we describe the invention of a series of novel triazolopyrazine c-Met inhibitors. The structure-activity relationship of these compounds was investigated, leading to the identification of compound 28, which demonstrated favorable pharmacokinetic properties in mice and good antitumor activities in the human glioma xenograft model in athymic nude mice.
Jia, Hong,Dai, Guangxiu,Weng, Jianyang,Zhang, Zhulin,Wang, Qing,Zhou, Feng,Jiao, Longxian,Cui, Yumin,Ren, Yongxin,Fan, Shiming,Zhou, Jinghong,Qing, Weiguo,Gu, Yi,Wang, Jian,Sai, Yang,Su, Weiguo
supporting information
p. 7577 - 7589
(2014/12/11)

Tryptophan-based fluorophores for studying protein conformational changes
With the continuing interest in deciphering the interplay between protein function and conformational changes, small fluorescence probes will be especially useful for tracking changes in the crowded protein interior space. Presently, we describe the poten
Talukder, Poulami,Chen, Shengxi,Liu, C. Tony,Baldwin, Edwin A.,Benkovic, Stephen J.,Hecht, Sidney M.
p. 5924 - 5934
(2015/01/09)

7,7′-Diazaindirubin - A small molecule inhibitor of casein kinase 2 in vitro and in cells
Aza- and diaza-bisindoles were synthesized by coupling of 7-azaisatin, 7-azaoxindol, 7-azaindoxyl acetate, and their non-aza counterparts, respectively. Whereas 7,7′-diazaindigo (10) and 7,7′-diazaisoindigo (11) did not show antiproliferative activity in several human tumor cell lines up to 100 μM, 7-azaindirubin (12) and 7′-azaindirubin (13) were more active than the parent molecule, indirubin, in LXFL529L cells (human large cell lung tumor xenograft), and 7,7′-diazaindirubin (14) was exhibiting substantially enhanced growth inhibitory activity in these cells. In the NCI 60 cell line panel, 14 displayed antiproliferative activity preferentially in certain melanoma and non-small cell lung cancer cells. In contrast to the potent serine/threonine/tyrosine kinase inhibition observed for indirubins, kinase inhibition profiling of 14 in 220 kinases revealed largely a loss of kinase inhibitory activity towards most kinases, with retained inhibitory activity for just a few kinases. At 1 μM concentration, especially casein kinases CK1γ3, CK2α, CK2α2, and SIK were inhibited by more than 50%. In cell-based assays, 14 markedly affected CK2-mediated signaling in various human tumor cells. In MCF7 cells, 14 induced cell cycle arrest at G1 and G2/M and apoptosis, whereas CK2-deficient MCF7 cells were resistant. These findings reveal a novel key mechanism of action for 14, suggesting primarily CK2 inhibition to be causally related to growth inhibition of human tumor cells.
Cheng, Xinlai,Merz, Karl-Heinz,Vatter, Sandra,Christ, Jochen,W?lfl, Stefan,Eisenbrand, Gerhard
p. 247 - 255
(2014/01/17)

CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR
Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
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Page/Page column 12

(2012/10/08)

AZAINDOLE DERIVATIVE
The present invention provides a (di)azaindole derivative represented by the formula (I). A compound of the present invention inhibits a Cdc7 protein kinase activity and suppresses cell proliferation.
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Page/Page column 36-37

(2012/01/14)

Deformylation of indole and azaindole-3-carboxaldehydes using anthranilamide and solid acid heterogeneous catalyst via quinazolinone intermediate
The deformylation of indole and azaindole-3-carboxaldehydes was achieved in the presence of anthranilamide and a solid acid heterogeneous catalyst under reflux conditions in 25-90% yield. The reaction proceeds via quinazolinone intermediate, which undergoes acid catalyzed cleavage to form deformylated product.
Yadav, Rammohan R.,Battini, Narsaiah,Mudududdla, Ramesh,Bharate, Jaideep B.,Muparappu, Nagaraju,Bharate, Sandip B.,Vishwakarma, Ram A.
scheme or table
p. 2222 - 2225
(2012/05/20)

CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR
Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
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Page/Page column 23

(2011/07/30)

5,6-BICYCLIC HETEROARYL-CONTAINING UREA COMPOUNDS AS KINASE INHIBITORS
The present invention provides 5,6-bicyclic heteroaryl-containing urea compounds of Formula I or II and use of the same for treating conditions mediated by protein kinase such as VEGFR2, c-Met, PDGFRβ c-Kit, CSFlR, or EphA2.
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Page/Page column 54-55

(2011/04/14)

Synthesis and CDK2 kinase inhibitory activity of 7/7′-azaindirubin derivatives
A series of novel 7′-azaindirubin (1a-g) and 7-azaindirubin (2a, 2c, 2e and 2f) derivatives were designed and synthesized. Their structures were characterized by 1H NMR and MS spectroscopy as well as by elemental analysis. Their inhibitory properties against CDK2/cylinA were evaluated in vitro. In contrast to indirubin, some of the described azaindirubins emerged as potent inhibitors of CDK2/cylinA and compound 2b had more potent activity. Biological tests also showed that nitrogen atom at 7-position of azaindirubin was more beneficial to enhance the kinase inhibitory activity.
Wang, Zhao Hui,Dong, Ying,Wang, Tao,Shang, Ming Hong,Hua, Wei Yi,Yao, Qi Zheng
scheme or table
p. 297 - 300
(2010/12/19)

7-azaindirubins, 7'-azaindirubins, 7-7'-diazaindirubin and the corresponding 3'-oxime ether derivates: production thereof, their production and use as a medicament
The present invention relates to 7-azaindirubins (1), 7'-azaindirubins (2), and 7,7'-diaza-indirubins (3), wherein E, R1 and R2 have the meanings detailed in the description, their production and use as a medicament for treating cancer, neurodegenerative diseases, bipolar disorders, inflammatory and infectious diseases, including viral diseases. Depending on structure, these indirubins act as inhibitors of various kinases involved in tumor cell growth, and, most notably, as inhibitors of human tumor cell proliferation. As compared to indirubins bearing identical substituents but no hetero atoms in position 7 and 7', the activity of the compounds according to the present invention is increased and the propensity to get metabolized by CYP450s is reduced, resulting in improved metabolic stability.
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Page/Page column 9

(2010/07/06)

A facile chemoenzymatic approach: One-step syntheses of monoterpenoid indole alkaloids
Facile chemoenzymatic syntheses of cytotoxic monoterpenoid indole alkaloids with novel skeletons and multiple chiral centers are described. Synthesis of these alkaloids was achieved by a simple one-step reaction using strictosidine and 12-aza-strictosidine as the key intermediates. Strictosidines were prepared by coupling of secologanin with tryptamine and 7-aza-tryptamine, respectively, using the immobilized recombinant Rauvolfia strictosidine synthase. A detailed stereochemical analysis is presented herein. The results provide an opportunity for a chemoenzymatic approach that leads to an increased diversification of complex alkaloids with improved structures and activities.
Zou, Hong-Bin,Zhu, Hua-Jian,Zhang, Liang,Yang, Liu-Qing,Yu, Yong-Ping,Stoeckigt, Joachim
supporting information; experimental part
p. 2400 - 2404
(2011/08/04)

A rapid method toward the synthesis of new substituted tetrahydro α-carbolines and α-carbolines
A rapid and efficient method for stereoselective synthesis of new substituted tetrahydro-α-carbolines using Diels-Alder reaction under microwave irradiation has been developed. Further, dehydrogenation of these adducts resulted in synthesis of new substit
Chavan, Neelam L.,Nayak, Sandip K.,Kusurkar, Radhika S.
scheme or table
p. 1827 - 1831
(2010/04/06)

7-AZAINDOLE DERIVATIVES AS SELECTIVE 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITORS
The present invention relates to 7-azaindole derivatives of formula (I) as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11 β-HSD-1 ) and the use of such compounds for the treatment and prevention of metabolic syndrome, d
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Page/Page column 50-51

(2009/06/27)

COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
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Page/Page column 35

(2008/12/06)

COMPOUNDS MODULATING C-FMS AND/OR C-KIT ACTIVITY AND USES THEREFOR
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Page/Page column 58

(2008/12/05)

1H-PYRROLO[2,3-B]PYRIDINE DERIVATIVES USEFUL AS HSP90 INHIBITORS
Compounds of formula (I) have HSP90 inhibitory activity: ring A is an aryl or heteroaryl ring or ring system; R1 is hydrogen, fluoro, chloro, bromo, or a radical of formula (1A): -X-Alk1-(Z)m-(Alk2)n-Q (IA) wherein X is a bond, -O-, -S-, -S(O)-, -SO2-, or -NH-, Z is -O-, -S-, -(C=O)-, -(C=S)-, -S(O)-, -SO2-, -NRA-, or, in either orientation -C(=O)O-, -C(=O)NRA-, -C(=S)NRA-, -SO2NRA-, -NRAC(=O)-, or -NRASO2- wherein RA is hydrogen or C1-C6 alkyl in which one or more hydrogens is optionally substituted by fluorine;Alk1 and AIk2 are optionally substituted divalent C1-C3 alkylene:or C2-C3 alkenylene radicals, m and n are independently 0 or 1, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R2 is cyano (-CN), fluoro, chloro, bromo, methyl, ethyl, -OH, -CH2OH, -C(=O)NH2,-C(=O)H, -C(=O)CH3, or -NH2; R3 and R4 are independently selected from hydrogen, fluoro, chloro, bromo, cyano (-CN), C1-C3alkyl optionally substituted with one or more fluorine substituents, C1-C3alkoxy optionally substituted with one or more fluorine substituents, -CH=CH2, -C≡CH, cyclopropyl and -NH2, or R3 and R4 together represent methylenedioxy (-OCH2O-) or ethylenedioxy (-OCH2CH2O-) in either of which one or more hydrogens are optionally replaced by fluorine; S1 is as defined in the description.
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Page/Page column 33-34

(2008/06/13)

Substituted Tetrahydroisoquinolines as Beta-secretase Inhibitors
There is provided a series of tetrahydroisoquinoline diaminopropane compounds of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R, R8 and R9 are as defined herein, their pharmaceutical compositi
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Page/Page column 24

(2008/12/06)

Synthesis and antidiabetic activity of 2,5-disubstituted-3-imidazol-2-yl-pyrrolo[2,3-b]pyridines and thieno[2,3-b]pyridines
In the present investigation, two series of 2,5-disubstituted-3-imidazol-2-yl-pyrrolo[2,3-b]pyridines (2a-l) and thieno[2,3-b]pyridines (3a-l) were designed as analogs of BL 11282 (1). The in vitro glucose dependent insulinotropic activity of all the test compounds was evaluated using RIN5F cell based assay and all the test compounds showed glucose and concentration dependent insulin secretion. The in vivo antidiabetic activities of most potent compounds from each series (2c and 3c) were assessed in C57BL/6J mice. Compounds 2c and 3c showed dose dependent insulin secretion and significant glucose reduction in vivo. In general, compounds 2c and 3c were found to be equipotent at all the three different doses selected and with respect to BL 11282, both the test compounds were found to be more potent, at all the time points.
Bahekar, Rajesh H.,Jain, Mukul R.,Jadav, Pradip A.,Prajapati, Vijay M.,Patel, Dipam N.,Gupta, Arun A.,Sharma, Ajay,Tom, Robby,Bandyopadhya, Debdutta,Modi, Honey,Patel, Pankaj R.
p. 6782 - 6795
(2008/03/28)

PYRROLO[2,3-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
Compounds of formula III which are active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
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Page/Page column 113

(2010/11/25)

COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY
The present disclosure provides compounds having affinity for the 5HT6 receptor which are of the formula (I), wherein R1-R3 A, B, D, E, G, Q, and x are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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Page/Page column 116

(2010/11/28)

COMPOUNDS AND METHODS OF USE
Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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Page/Page column 112

(2010/11/27)

Design, synthesis, and evaluation of potential inhibitors of brassinin glucosyltransferase, a phytoalexin detoxifying enzyme from Sclerotinia sclerotiorum
Sclerotinia sclerotiorum is a fungal pathogen, which causes stem rot in crucifer crops and in several other plant families resulting in enormous yield losses all over the world. Brassinin is a phytoalexin produced by crucifer plants as part of a general d
Pedras, M. Soledade C.,Hossain, Mohammad
p. 5981 - 5996
(2008/03/27)

Azaindole thiazolinones
Azaindole thiazolinone derivatives which demonstrate CDK1 and CDK2 antiproliferative activities and are useful as anti-cancer agents.
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Page/Page column 7

(2010/10/20)

(2-carboxamido)(3-amino) thiophene compounds
Amidoaryl/amidoheteroaryl substituted thiophenes, further substituted with a heteroarylmethylamino group, are useful in the treatment of cancer.
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(2008/06/13)

Substituted indoles as alpha-1 agonists
This invention relates to compounds which are alpha-1 receptor agonists, preferably alpha-1A/L receptor agonists, and which are represented by Formula I: wherein m, A, X, Y, R1, R2, R3, R4 and R5 are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.
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Page 32

(2010/02/09)

Antifungal and/or antiparasitic pharmaceutical composition and novel indole derivatives as active principle of such a composition
The present invention relates to novel indole derivatives, their method of preparation and their pharmacological activity as antimycotic and/or antiparasitic compounds.
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Page/Page column 29

(2010/02/06)

Synthesis and evaluation of fluorine-substituted 1H-pyrrolo[2,3-b]pyridine derivatives for dopamine D4 receptor imaging
Seven fluorine-substituted 1H-pyrrolo[2,3-b]pyridine derivatives were synthesized based on a lead ligand, 3-[[4-(4-iodophenyl)piperazin-1-yl]-methyl]- 1H-pyrrolo[2,3-b]pyridine (L-750,667) and evaluated as potential dopamine D 4 receptor imagin
Oh, Seung-Jun,Lee, Kyo Chul,Lee, Sang-Yoon,Ryu, Eun Kyoung,Saji, Hideo,Choe, Yearn Seong,Chi, Dae Yoon,Kim, Sang Eun,Lee, Jeewoo,Kim, Byung-Tae
p. 5505 - 5513
(2007/10/03)

(2-carboxamido)(3-amino)thiophene compounds
Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein R1 is R2 is and R3 is C0-4alkyl, are useful in the treatment of cancer.
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Page/Page column 13

(2008/06/13)

BIOREDUCTIVE CONJUGATES FOR DRUG TARGETING
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(2008/06/13)

SUBSTITUTED AZAINDOLYLIDENE COMPOUNDS AND PROCESS FOR THEIR PREPARATION
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(2008/06/13)

Potential Dopamine D4 Receptor Imaging Agents: Fluoromethylated 1-Phenyl-3-(aminomethyl)pyrroles and 7-Azaindole Analog
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Oh, S. J.,Choe, Y. S.,Kim, S. E.,Choi, Y.,Lee, K. H.,et al.
p. 26 - 28
(2007/10/03)

Substituted indole derivatives
Compounds of the Formula (I), (II), or (III): STR1 wherein the variables are as defined in the specification and the pharmaceutically acceptable salts thereof, exhibit useful pharmacological properties, and are particularly useful as angiotensin II antago
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(2008/06/13)

Syntheses of a potential fluorescence probe, (-)-(R)-7-azatryptophan, via alkylation of the (1R,4R)-camphor imine of tert-butylglycinate
The synthesis of (-)-(R)-7-azatryptophan (2) from commercially available 7-azaindole (4) is described.The key step involved the diastereoselective alkylation of tert-butyl acetate (3) with 1-(tert-butyloxycarbonyl-3-(iodomethyl)-7-azaindole (14).The alkylation, conducted at -100 deg C in a THF/HMPA solvent using potassium hexamethyldisilazide as the base, afforded 7 in a greater than 98 percent diastereomeric excess.Hydrolysis and deprotecting gave (-)-(R)-7-azatryptophan.
Sanchez-Obregon, Ruben,Fallis, Alex G.,Szabo, Arthur G.
p. 1531 - 1536
(2007/10/02)