- HETEROCYCLIC COMPOUNDS AND USE THEREOF
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Heterocyclic compounds of Formula (I) shown herein. Also disclosed is a pharmaceutical composition containing one of the heterocyclic compounds. Further disclosed are methods of using one of the heterocyclic compounds for mobilizing hematopoietic stem cells and endothelial progenitor cells into the peripheral circulation, and for treating tissue injury, cancer, inflammatory disease, and autoimmune disease.
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Page/Page column 19
(2018/08/03)
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- 4,5-DIHYDROISOXAZOLE DERIVATIVES AS NAMPT INHIBITORS
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The present invention provides 4,5-dihydroisoxazole derivatives of formula (I), which may be therapeutically useful, more particularly as NAMPT inhibitors. wherein, ring A, L1, L2, X1, X2, X3, Z, R1, R2, R3, R4, R5, m, n, p and q have the meanings given in the specification and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder, caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPT) in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted 4,5-dihydroisoxazole derivatives of formula (I) or a pharmaceutically acceptable salt thereof or a stereoisomer thereof.
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Page/Page column 26
(2016/02/26)
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- Five-membered azole heterocyclic compound and its preparation method, pharmaceutical composition and use thereof
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The present invention relates to a five-membered azole heterocycle compound represented by the following general formula (I), a preparation method of the five-membered azole heterocycle compound, a drug composition of the five-membered azole heterocycle compound, and a use of the five-membered azole heterocycle compound in preparation of drugs for prevention or treatment of TGR5-mediated diseases. The formula (I) is represented by the instruction.
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Paragraph 0695; 0696
(2017/02/28)
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- Metal-free C-N cross-coupling of electrophilic compounds and N-haloimides
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When DBU is added, the cross-coupling reaction between alkyl halides (halogen = Cl, Br and I) and N-haloimides (halogen = Cl, Br) occurs, resulting in the formation of aminated products. A halogen bond activated nucleophilic substitution mechanism was proposed. The methodology represents an elegant example of applying the halogen bond activation strategy in an organic transformation.
- Zhang, Luyan,Li, Yanru,Jin, Long-Yi,Liang, Fushun
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p. 65600 - 65603
(2015/08/18)
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- 4,5-DIHYDROISOXAZOLE DERIVATIVES AS NAMPT INHIBITORS
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The present invention provides substituted 4,5-dihydroisoxazole derivatives of formula (I), which may be therapeutically useful, more particularly NAMPT inhibitors and in which R1 R2, Y, X, "Het" and "p" have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPT) in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted 4,5-dihydroisoxazole derivatives of formula (I) or a pharmaceutically acceptable salts or stereoisomers or N-oxide thereof.
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Page/Page column 121; 122
(2014/08/06)
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- Synthesis of some analogues of (±)gelliusine F, (±)gelliusine E, and total synthesis of 2,2-di(6′-bromo-3′-indolyl)ethylamine
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Synthesis of some analogues of indole based marine alkaloid (±)gelliusine F, (±)gelliusine E, and total synthesis of 2,2-di(6′-bromo-3′-indolyl)ethylamine are reported.
- Seetham Naidu,Bhuyan, Pulak J.
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experimental part
p. 426 - 428
(2012/03/07)
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- Synthesis of "Trioxaquantel" derivatives as potential new antischistosomal drugs
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Over the past 20 years, praziquantel, a pyrazinoisoquinoline derivative, has become the mainstay for morbidity control of human and animal schistosomiasis. From early in their lives in vertebrate hosts, schistosomes ingest hemoglobin and aggregate the released heme as a dark pigment very similar to the hemozoin produced by Plasmodium in malaria infection. The antimalarial artemisinin derivatives have real, though low, schistosomicide activity. Because of the complementarity of the two drug classes - praziquantel and artemisinin derivatives - we designed new molecules, named trioxaquantels, that combine the 1,2,4-trioxane unit responsible for the activity of artemisinin, and the pyrazinoisoquinoline moiety of praziquantel within a single drug. The synthesis of these new drugs and their preliminary evaluation in mice infected with Schistosoma mansoni is reported here. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
- Laurent, Sophie A.-L.,Boissier, Jerome,Cosledan, Frederic,Gornitzka, Heinz,Robert, Anne,Meunier, Bernard
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experimental part
p. 895 - 913
(2009/04/08)
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- Total synthesis of (-)-praziquantel: An anthelmintic drug
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The optically pure (-)-praziquantel was synthesised using phenylethylamine as starting material in 12% overall yield. The key step was achived by a chiral auxiliary mediated Pictet-Spengler reaction.
- Ma, Chen,Zhang, Qian-Feng,Tan, Ye-Bang,Wang, Long
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p. 186 - 187
(2007/10/03)
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- Synthesis of deoxyvariolin B
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A synthesis of deoxyvariolin B (5) is described. The tricyclic pyridopyrrolopyrimidone (11) was prepared from 7-azaindole via lithiation at C-2, introduction of an aminoethyl side-chain, then closure of the third ring. A heteroaryl palladium(0)-catalysed coupling reaction was used to introduce a pyrimidine substituent at C-5.
- álvarez, Mercedes,Fernández, David,Joule, John A.
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p. 315 - 317
(2007/10/03)
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- Nucleoside analogs. 14. The synthesis and antitumor activity in mice of molecular combinations of 5-fluorouracil and N-(2-chloroethyl)-N-nitrosourea moieties separated by a three-carbon chain
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5-Fluorouracil (5-FU) seco-nucleosides having as the "sugar" moiety a two-carbon (C2) side chain carrying a N-(2-chloroethyl)-N-nitrosourea group were designed as molecular combinations of antimetabolite and alkylating agent, but hydrolytic release of free 5-FU was not fast enough for significant contribution to the high activity they showed against colon and breast tumors in mice. In the present study of the synthesis of the more reactive C3 seco-nucleosides, it emerged that, of various groups attached to the aldehydic center in the precursor phthalimides, only the alkoxy/uracil-1-yl type was conveniently obtained by the standard method. The methylthio/uracil-1-yl analog required relatively large amounts of reagent methanethiol, and exploration of alternatives involving α-chlorination of alkyl methyl sulfide or Pummerer rearrangement of its S-oxide, or successive hydrolysis and methylation of isothiouronium bromide, gave disappointing yields. For successful preparation of the alkoxy/ uracil-3-yl compounds, the route used for C2 homologs required considerable experimental modification. In addition to these O,N- and S,N-acetals, some N,N-acetals bearing two 5-FU residues were prepared. The new drugs have been tested against a panel of experimental tumors in mice. Although it is evident from a parallel study that even these C8 seco-nucleosides release free 5-FU too slowly in vivo, several of them have shown impressive anticancer activity. Reviewing their performance in comparison with earlier molecular combinations, a short list of seven [B.4152 (6), B.4015 (5), B.4030 (10), B.3999 (4), B.3995 (2), B.4083 (3), and B.3996 (the N3-substituted analog of 1)] should be investigated further. This is particularly appropriate in light of the present understanding of the mode of action of chloroethylating agents. Following a prolonged period of clinical impatience with nitrosoureas because of limited selectivity of action, a new era is confidently anticipated as these powerful drugs are increasingly studied in combination with O6-benzylguanine and other more efficient inhibitors of repair enzymes like O6-alkylguanine-DNA-alkyltransferase now being developed.
- McElhinney, R. Stanley,McCormick, Joan E.,Bibby, Mike C.,Double, John A.,Radacic, Marco,Dumont, Patrick
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p. 1408 - 1412
(2007/10/03)
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