76283-09-5Relevant articles and documents
tBuOK-Promoted Cyclization of Imines with Aryl Halides
Li, Ya-Wei,Zheng, Hong-Xing,Yang, Bo,Shan, Xiang-Huan,Qu, Jian-Ping,Kang, Yan-Biao
supporting information, p. 4553 - 4556 (2020/06/08)
A transition-metal-free indole synthesis using radical coupling of 2-halotoluenes and imines via the later-stage C-N bond construction was reported for the first time. It includes an aminyl radical generation by C-H cleaving addition of 2-halotoluenes to imines via the carbanion radical relay and an intramolecular coupling of aryl halides with aminyl radicals. One standard condition can be used for all halides including F, Cl, Br, and I. No extra oxidant or transition metal is required.
METHOD FOR PRODUCING 4-BORONO-L-PHENYLALANINE HAVING 18F ATOM INTRODUCED THEREINTO, AND PRECURSOR OF 4-BORONO-L-PHENYLALANINE HAVING 18F ATOM INTRODUCED THEREINTO
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Paragraph 0144; 0145; 0146, (2017/02/02)
18F-labeled 4-boronophenylalanine (BPA) can be produced by preparing and further processing a precursor of 18F-labeled BPA represented by the following formula: in which R1 represents a bromo group, an iodo group, a fluoro group, a diazaborinane derivative, BX3? or BX3?M+ (wherein X represents a halogen atom; and M+ represents a monovalent monoatomic cation, a polyatomic cation or a complex cation).
Novel Triazolopyrazine Derivatives and Use Thereof
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Paragraph 0268, (2017/07/31)
The present invention relates to novel triazolopyrazine derivatives or a pharmaceutically acceptable salt, and a pharmaceutical composition for inhibiting c-Met tyrosine kinase activity and a pharmaceutical composition for preventing or treating hyperproliferative disorders, containing the same as active ingredients. The present invention effectively inhibits c-Met tyrosine kinase activity, thereby being able to be useful as a drug for various hyperproliferative disorders such as cancers, psoriasis, rheumatoid arthritis, diabetic retinitis, etc. related to excessive cell proliferation and growth by abnormal kinase activation.
NOVEL TRIAZOLOPYRAZINE DERIVATIVE AND USE THEREOF
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Paragraph 0169; 1070, (2015/10/06)
The present invention relates to a novel triazolopyrazine derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same as an active ingredient for preventing or treating hyper proliferative disorder. The present invention can be useful as a therapeutic agent for various hyper proliferative disorders associated with excessive cell proliferation and growth caused by abnormal kinase activity, such as cancer, psoriasis, rheumatoid arthritis, and diabetic retinopathy, by efficiently inhibiting c-Met tyrosine kinase activity.
INHIBITORS OF BRUTON'S TYROSINE KINASE
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Page/Page column 66, (2014/06/11)
This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
8-ETHYL-6-(ARYL)PYRIDO [2,3-D]PYRIMIDIN-7(8H) -ONES FOR THE TREATMENT OF NERVOUS SYSTEM DISORDERS AND CANCER
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Paragraph 00602; 00649, (2013/04/10)
Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders or neurofibromatosis. Also described herein are methods of utilizing PAK inhibitors for the treatment of cancer.
Synthesis of novel phenylacetic acid derivatives with halogenated benzyl subunit and evaluation as aldose reductase inhibitors
Rakowitz, Dietmar,Gmeiner, Andreas,Schroeder, Nicole,Matuszczak, Barbara
, p. 188 - 193 (2007/10/03)
In the course of our ongoing studies several substituted benzyloxyphenylacetic acids were prepared. Comparison of their aldose reductase inhibition with the biological activity obtained for recently evaluated benzoic acid analogues revealed the critical role of a methylene spacer between the aromatic core and the acidic function. Starting from the most potent derivative (i.e. 5d, IC50 = 20.9 μM) further structural modifications were performed and their influence on the inhibitory effect was established.
Synthesis and evaluation of 2′-substituted 4-(4′-carboxy- or 4′-carboxymethylbenzylidene)-N-acylpiperidines: Highly potent and in vivo active steroid 5α-reductase type 2 inhibitors
Picard, Franck,Barassin, Stephan,Mokhtarian, Armand,Hartmann, Rolf W.
, p. 3406 - 3417 (2007/10/03)
Sixteen compounds derived from N-acyl-4-benzylidenepiperidine-4′-carboxylic acids were synthesized and evaluated for inhibition of rat and human steroid 5α-reductase isozymes types 1 and 2. In the dicyclohexylacetyl series, fluorination in the 2-position of the benzene nucleus (15), exchange of the carboxy group by a carboxymethyl moiety (20), and combination of both structural modifications (25) led to highly active inhibitors of the human type 2 isozyme (IC50 values: 15, 11 nM; 20, 6 nM; 25, 7 nM; finasteride, 5 nM). In vivo all compounds tested markedly reduced the prostate weights in castrated testosterone-treated rats. Oral activity was shown for compound 7. From the finding that compound 15 is active in the rat, although it is a rather poor inhibitor of the rat enzyme and is a strong inhibitor of the human enzyme, it is concluded that it should be highly potent in men.
Balanced AT1/AT2 receptor antagonists. 4. XR510 and related 5-(3- amidopropanoyl)imidazoles possessing equal affinity for the AT1 and AT2 receptors
Quan,Chin,Ellis,Wong,Wexler,Timmermans
, p. 2938 - 2945 (2007/10/02)
The identification of the AT1 and AT2 receptor subtypes has stimulated interest in developing balanced angiotensin II receptor antagonists. A series of 5-(3-amidopropanoyl)imidazoles has been prepared which possess balanced affinity for the AT1 and AT2 receptors. XR510 (1), 1-[[2'- [[(isopentoxycarbonyl)amino]sulfonyl]-3-fluoro(1,1'-biphenyl)-4-yl]methyl]- 5-[3-(N-pyridin-3-ylbutanamido)propanoyl]-4-ethyl-2-propyl-1H-imidazole, potassium salt, exhibits subnanomolar affinity for both receptor sites. XR510 is very active in lowering blood pressure in renal hypertensive rats and furosemide-treated dogs following oral administration.
