- PYRAZOLE DERIVATIVES AS MALT1 INHIBITORS
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Disclosed are compounds, compositions and methods for treating of diseases, syndromes, conditions, and disorders that are affected by the modulation of MALT1. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, R4, R5, R6, R5, G1, and G2 are defined herein.
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Paragraph 1840; 1841
(2018/07/05)
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- A method for synthesizing milrinone
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The invention discloses a new method for synthesizing milrinone. The method is characterized in that a compound of formula 3 and 4-pyridineboronic acid undergo a Suzuki coupling reaction to synthesize milrinone. The method has the advantages of easily available raw materials, high yield and simple post-treatment.
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Paragraph 0051; 0052
(2018/03/13)
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- THIENOPYRIDINE CARBOXAMIDES AS UBIQUITIN-SPECIFIC PROTEASE INHIBITORS
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The disclosure relates to inhibitors of USP28 and/or USP25 useful in the treatment of cancers, inflammation, autoimmune diseases, and infectious diseases, having the Formula (I), where R1, R2, R3, R4, R5, R5', R6, R7, X, m, and n are described herein.
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Paragraph 00323
(2017/09/05)
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- Preparation method of olprinone and 9-azaindole-5-boric acid
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The invention relates to a preparation method of olprinone and 9-azaindole-5-boric acid, in particular to a method for preparing olprinone via Suzuki coupling. In the preparation method of olprinone and 9-azaindole-5-boric acid, a converging synthetic route is innovatively designed, has high atom utilization rate as compared with existing three series synthetic processes and is better than existing synthetic routes in overall reaction yield; the preparation method has mild synthetic reaction conditions, is simple to perform and is easy to industrialize; the prepared olprinone may be further olprinone hydrochloride via salifying, and the prepared olprinone hydrochloride has the advantages such as low impurity content, high purity, high yield and good mildness of reaction conditions.
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Paragraph 0023; 0025
(2017/07/15)
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- CONDENSED TRICLYCLIC COMPOUNDS AS INHIBITORS OF HIV REPLICATION
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Compounds of formula (I) and pharmaceutical compositions thereof: wherein A1 A2 and A3 are each independently selected from the group consisting of N and CR3, wherein R1 is an optionally substituted heterocyclyl or an optionally substituted -(C1-6)alkyl-heterocyclyl, R2 is an optionally substituted aryl or an optionally subsisted heteroaryl, R4 is an optionally substituted aryl, an optionally substituted heterocyclyl or an optionally substituted heteroaryl, useful as an inbitor of HIV replication.
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Page/Page column 40-41
(2013/07/05)
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- Synthesis of amido-N-imidazolium salts and their applications as ligands in suzuki-miyaura reactions: Coupling of hetero- aromatic halides and the synthesis of milrinone and irbesartan
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A new catalytic system based on palladium-amido-N-heterocyclic carbenes for Suzuki-Miyaura coupling reactions of heteroaryl bromides is described. A variety of sterically bulky, amido-N-imidazolium salts were synthesized in high yields from the corresponding anilines. This catalytic system effectively promoted Suzuki-Miyaura couplings of heteroaryl bromides and chlorides with a range of boronic acids to give the corresponding aryl compounds in high yield. The yield was increased with increasing steric bulkiness of the substituted group. Especially, 1-(2,6-diisopropylphenyl)-3-N-(2,4,6-tri-tert- butylphenylacetamido)imidazolium bromide (4bc) exhibited 850,000 TON in the coupling reaction of 2-bromopyridine and phenylboronic acid. In addition, pharmaceutical compounds such as milrinone and irbesartan were synthesized via Suzuki-Miyaura coupling using sterically bulky, amido-N-imidazolium salt (4bc) as a ligand. Copyright
- Kumar, Manian Rajesh,Park, Kyungho,Lee, Sunwoo
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experimental part
p. 3255 - 3266
(2011/02/23)
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- Discovery of potent imidazole and cyanophenyl containing farnesyltransferase inhibitors with improved oral bioavailability
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A pyridyl moiety was introduced into a previously developed series of farnesyltransferase inhibitors containing imidazole and cyanophenyl (such as 4), resulting in potent inhibitors with improved pharmacokinetics.
- Tong, Yunsong,Lin, Nan-Horng,Wang, Le,Hasvold, Lisa,Wang, Weibo,Leonard, Nicholas,Li, Tongmei,Li, Qun,Cohen, Jerry,Gu, Wen-Zhen,Zhang, Haiying,Stoll, Vincent,Bauch, Joy,Marsh, Kennan,Rosenberg, Saul H.,Sham, Hing L.
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p. 1571 - 1574
(2007/10/03)
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- Pyridone-containing farnesyltransferase inhibitors: Synthesis and biological evaluation
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Farnesyltransferase inhibitors (FTIs) have been developed as potential anti-cancer agents due to their efficacy in blocking malignant growth in a variety of murine models of human tumors. To that end, we have developed a series of pyridone farnesyltransferase inhibitors with potent in vitro and cellular activity. The synthesis, SAR and biological properties of these compounds will be discussed.
- Hasvold, Lisa A.,Wang, Weibo,Gwaltney II, Stephen L.,Rockway, Todd W.,Nelson, Lissa T. J.,Mantei, Robert A.,Fakhoury, Stephen A.,Sullivan, Gerard M.,Li, Qun,Lin, Nan-Horng,Wang, Le,Zhang, Haiying,Cohen, Jerome,Gu, Wen-Zhen,Marsh, Kennan,Bauch, Joy,Rosenberg, Saul,Sham, Hing L.
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p. 4001 - 4005
(2007/10/03)
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- Farnesyltransferase inhibitors
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Substituted imidazoles and thiazoles having the formula are useful for inhibiting farnesyltransferase. Also disclosed are farnesyltransferase-inhibiting compositions and methods of inhibiting farnesyltransferase in a patient.
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- Farnesyltransferase inhibitors
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Substituted imidazoles and thiazoles having the formula are useful for inhibiting farnesyltransferase. Also disclosed are farnesyltransferase-inhibiting compositions and methods of inhibiting farnesyltransferase in a patient.
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