- Synthesis of new 6-substituted purinyl-5′-nor-1′- homocarbanucleosides based on indanol
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A series of new 6-substituted purinyl-5′-nor-1′- homocarbanucleosides based on indanol were synthesized from (±)-cis-3- hydroxymethyl-1-indanol, an appropriately functionalized derivative of which was reacted with 6-chloropurine in the presence of NaH and
- Fernández, Franco,García-Mera, Xerardo,Morales, Melvin,Vilari?o, Leonardo,Caama?o, Olga,De Clercq, Eric
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Read Online
- Preparation method and application of tetrahydroisoquinoline derivative
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The invention discloses a preparation method of a tetrahydroisoquinoline derivative. The tetrahydroisoquinoline derivative is prepared by subjecting 1-(tetrapyrrolidin-1-yl)-1,2,3,4-tetrahydroisoquinoline and 2,3-dihydro-indene-3-one-1-carboxylic acid to condensation. Process conditions are optimized so that preparation steps are simplified. Agents used in the preparation are pollution free. The prepared tetrahydroisoquinoline derivative 1-(tetrapyrrolidin-1-methyl)-2-(2,3-dihydro-indene-3-one-1-carbonyl)-1,2,3,4-tetrahydroisoquinoline can provide good calming effect against neuropathic pain.The tetrahydroisoquinoline derivative has high medical value in drug compositions for pain treatment and in replacing dependent analgesics, such as morphine.
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Paragraph 0035; 0039
(2019/03/08)
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- Compound as potassium channel modulator
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The invention relates to a compound as a potassium channel modulator, which is a compound of a formula (I) or a pharmaceutically acceptable salt thereof. The compound or the pharmaceutically acceptable salt thereof is effective for curing and preventing diseases and symptoms influenced by the activity of potassium ion channels.
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Paragraph 0195; 0197; 0198; 0199
(2018/07/30)
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- SPIROCYCLIC HAT INHIBITORS AND METHODS FOR THEIR USE
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Compounds having a structure of Formula (IX) or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b, R3a, R3b, R4a, R4b, Q1----Q2, R6, R7, A, B, W, x, and y are as defined herein and are provided. Pharmaceutical compositions comprising such compounds and methods for treating various HAT-related conditions or diseases, including cancer, by administration of such compounds are also provided.
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Page/Page column 661
(2016/04/10)
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- Rhodium-catalyzed C-H activation of phenacyl ammonium salts assisted by an oxidizing C-N bond: A combination of experimental and theoretical studies
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Rh(III)-catalyzed C-H activation assisted by an oxidizing directing group has evolved to a mild and redox-economic strategy for the construction of heterocycles. Despite the success, these coupling systems are currently limited to cleavage of an oxidizing
- Yu, Songjie,Liu, Song,Lan, Yu,Wan, Boshun,Li, Xingwei
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p. 1623 - 1631
(2015/02/19)
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- Discovery, stereospecific characterization and peripheral modification of 1-(pyrrolidin-1-ylmethyl)-2-[(6-chloro-3-oxo-indan)-formyl]-1,2,3,4-tetrahydroisoquinolines as novel selective κ opioid receptor agonists
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A novel series of 1-(pyrrolidin-1-ylmethyl)-2-[(3-oxo-indan)-formyl]-1,2,3,4-tetrahydroisoquinoline derivatives maj-3a-maj-3u were synthesized and evaluated in vitro for their binding affinity at κ-opioid receptors. Maj-3c displayed the highest affinity for κ-opioid receptors (Ki = 0.033 nM) among all the compounds evaluated. Furthermore, all four stereoisomers of compound 3c were prepared, and (1S,18S)-3c was identified as the most potent (Ki = 0.0059 nM) κ-opioid receptor agonist among the four stereoisomers. Maj-3c produced significant antinociception (ED50 = 0.000406 mg kg-1) compared to U-50,488H and original BRL 52580 in the acetic acid writhing assay, but its strong sedative effect (ED50 = 0.000568 mg kg-1) observed in the mouse rotation test reduced its druggability. To minimize the central nervous system side effects, a series of hydroxyl-containing analogs of maj-3c were synthesized, and maj-11a was found to be a potent κ-opioid receptor agonist (Ki = 35.13 nM). More importantly, the dose for the sedative effect (ED50 = 9.29 mg kg-1) of maj-11a was significantly higher than its analgesic dose (ED50 = 0.392 mg kg-1), which made it a promising peripheral analgesic candidate compound with weak sedative side effects.
- Gan, Zong-Jie,Wang, Yu-Hua,Xu, Yun-Gen,Guo, Ting,Wang, Jun,Song, Qiao,Xu, Xue-Jun,Hu, Shi-Yuan,Wang, Yu-Jun,Wang, De-Chuan,Sun, De-Zhu,Zhang, Di,Xi, Tao,Li, Hao-Dong,Zhang, Hai-Bo,Hang, Tai-Jun,Lu, Hong-Guo,Liu, Jing-Gen
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p. 5656 - 5673
(2015/05/27)
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- TETRAHYDRO ISOQUINOLINE DERIVATIVES, PREPARATION METHODS AND MEDICINAL USES THEREOF
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A kind of tetrahydro isoquinoline derivatives (I), their preparation methods, medicine compositions and medicinal uses thereof, especially their uses as κ-opioid receptor excitant in pain relieving, which belongs to the medicine chemistry. The substituents R1, R2, R3, R4 of general formula (I) are defined as the description.
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Page/Page column 8
(2009/04/23)
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- Tetrahydro isoquinoline derivatives, preparation methods and medicinal uses thereof
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A kind of tetrahydro isoquinoline derivatives (I), their preparation methods, medicine compositions and medicinal uses thereof, especially their uses as kappa-opioid receptor excitant in pain relieving, which belongs to the medicine chemistry. The substituents R1, R2, R3, R4 of general formula (I) are defined as the description.
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Page/Page column 6
(2009/12/02)
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- Aminoindanes
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The present invention relates to therapeutically active novel aminoindanes of formula (I). Also provided is a method of preparing compounds of formula (I), and pharmaceutical compositions comprising the compounds. The novel compounds act as modulators of
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Page/Page column 25-26; 29-31
(2010/02/05)
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- Structure-based design of peptidomimetic antagonists of p56lck SH2 domain
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Starting from the tetrapeptide Ac-pYEEI-NHMe and using a structure-based approach, we have designed and synthesised a peptidomimetic ligand for p56lck SH2 domain containing a conformationally restricted replacement for the two glutamate residue
- Hobbs, Christopher J.,Bit, Rino A.,Cansfield, Andrew D.,Harris, Bill,Hill, Christopher H.,Hilyard, Katherine L.,Kilford, Ian R.,Kitas, Eric,Kroehn, Antonin,Lovell, Peter,Pole, David,Rugman, Paul,Sherborne, Brad S.,Smith, Ian E.D.,Vesey, David R.,Walmsley, D. Lee,Whittaker, David,Williams, Glyn,Wilson, Fiona,Banner, David,Surgenor, Allan,Borkakoti, Neera
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p. 1365 - 1369
(2007/10/03)
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- A short, efficient synthesis of substituted uracil: An indane carbocyclic nucleoside
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(±)-cis-1-(3-Hydroxymethyl-1-indanyl)-1,2,3,4-tetrahy-dropyrimidine-2, 4-dione (1) was synthesised in two steps and with an overall yield of 51percent from (±)-cis-3-amino-1-indanylmethanol (4) and 3-ethoxy-2-propenoyl isocyanate (3). The isocyanate 3 was prepared in 76percent overall yield by reacting silver cyanate with 3-ethoxy-2-propenoyl chloride (2), which was obtained in one pot from ethyl vinyl ether and oxalyl chloride. The aminoalcohol (4) was prepared from phenylsuccinic anhydride in four steps.
- Ferna?ndez,Garci?a-Mera,Morales,Rodri?guez-Borges
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p. 239 - 242
(2007/10/03)
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- Conformational and steric aspects of the inhibition of phenylethanolamine N-methyltransferase by benzylamines
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Compounds of the benzylamine (BA) class are potent inhibitors of phenylethanolamine N-methyltransferase (PNMT, EC 2.1.1.28). Restriction of the aminomethyl side chain through its incorporation into a cyclic framework as in 1,2,3,4-tetrahydroisoquinoline (
- Grunewald,Sall,Monn
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p. 433 - 444
(2007/10/02)
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- SYNTHESE DU METHOXYCARBONYL-3 INDENE ET DE METHOXYCARBONYL-4 DIHYDRO-1,2 NAPHTALENES. OBTENTION DES β-TETRALONES A PARTIR DES α-TETRALONES CORRESPONDANTES
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The synthesis of variously substituted 3-methoxycarbonylindene and 4-methoxycarbonyl-1,2-dihydronaphthalenes is described.A simple and efficient method for the transformation of 1-tetralone into 2-tetralone is reported.
- Vebrel, Joel,Carrie, Robert
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p. 161 - 166
(2007/10/02)
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