742058-39-5Relevant articles and documents
Anti-tumor activity with acetylene derivatives
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Paragraph 0211-0214, (2016/10/08)
The present invention relates to an aromatic ring disubstituted acetylene derivative of formula I, a pharmaceutical composition comprising the compound, and a use of the compound and of the pharmaceutical composition in the treatment and/or prevention of tumors, where A, B, T, M, Ra, Rb, Rt, m, n, and p are as defined in the present document.
Synthesis and cytotoxic evaluation for some new 2,5-disubstituted pyrimidine derivatives for anticancer activity
Reddy, Onteddu Surendranatha,Suryanarayana, Ch. Venkata,Narayana,Anuradha,Babu, B. Hari
, p. 1777 - 1788 (2015/05/27)
Abstract An efficient synthetic approach for 2,5-disubstituted pyrimidines has been reported. The desired 2,5-substituted pyrimidines were obtained by Suzuki coupling of 2-substituted benzyloxy-5-bromopyrimidines with various aryl boronic acids in the presence catalytic amount of PdCl2(PPh3)2 with 0.5 M aqueous Na2CO3 in water at 80 °C. 2-Benzyloxy-5-bromopyrimidines were synthesized, in turn by the reaction of 2-chloro-5-bromopyrimidine with substituted benzyl alcohols in the presence of Cs2CO3 in CH3CN:DMF (1:1). Some of the 2,5-disubstituted pyrimidines have shown moderate in vitro cytotoxic activity against HeLa cell line.
A PROCESS FOR PREPARING TETRAHYDROQUINOLINE DERIVATIVES
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Page/Page column 51-52, (2008/06/13)
The present invention is to provide a process for preparing optically active tetrahydroquinoline derivatives which can be used for the treatment and/or prevention of diseases such as arteriosclerotic diseases, dyslipidemia and the like, and a process for preparing synthetic intermediates thereof. Specifically, (2R,4S)-2-ethyl-6-trifluoromethyl-1,2,3,4-tetrahydroquinolin-4-ylamine or a salt thereof is prepared with fewer steps without using an optical resolution, and the optically active tetrahydroquinoline derivatives are obtained from the amine compound.
BIS(HETERO)ARYL CARBOXAMIDE DERIVATIVES FOR USE AS PGI2 ANTAGONISTS
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Page 52, (2010/02/08)
The present invention relates to aryl or heteroaryl amido alkane derivatives of formula (I) wherein R6 represents carboxy or tetrazolyl, which are useful as an active ingredient of pharmaceutical preparations. The aryl or heteroaryl amido alkanes of the present invention have PGI2 antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with PGI2 activity.Such diseases include urological diseases or disorder as follows: bladder outlet obstruction, overactive bladder, urinary incontinence, detrusor hyper-reflexia, detrusor instability, reduced bladder capacity, frequency of micturition, urge incontinence, stress incontinence, bladder hyperreactivity, benighn prostatic hypertrophy (BPH), prostatitis, urinary frequency, nocturia, urinary urgency, pelvic hypersensitivity, urethritis, pelvic pain syndrome, prostatodynia, cystitis, or idiophatic bladder hypersensitivity.The compounds of the present invention are also useful for treatment of pain including, but not limited to inflammatory pain, neuropathic pain, acute pain, chronic pain, dental pain, premenstrual pain, visceral pain, headaches, and the like; hypotension;hemophilia and hemorrhage; and inflammation, since the diseases also relate to PGI2.
