- Synthesis, biological evaluation and SAR of naftopidil-based arylpiperazine derivatives
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For the development of potential anti-prostate cancer agents, 24 kinds of novel naftopidil-based arylpiperazine derivatives have been synthesized and characterized by spectroscopic methods. Their antitumor activities were evaluated against several classic
- Chen, Hong,Wang, Cai-Lu,Sun, Tao,Zhou, Zhan,Niu, Jiang-Xiu,Tian, Xiu-Mei,Yuan, Mu
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- Design, synthesis and biological evaluation of novel arylpiperazine derivatives on human prostate cancer cell lines
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A series of novel arylpiperazine derivatives was synthesized. The in vitro cytotoxic activities of all synthesized compounds against three human prostate cancer cell lines (PC-3, LNCaP, and DU145) were evaluated by a CCK-8 assay. Compounds 8, 10, 13, 17 a
- Chen, Hong,Xu, Fang,Xu, Bing-Bing,Xu, Jing-Yi,Shao, Bin-Hao,Huang, Bi-Yun,Yuan, Mu
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- Synthesis, structure-activity relationship and biological evaluation of novel arylpiperzines as α1A/1D-AR subselective antagonists for BPH
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A series of novel arylpiperazine derivatives as α1A/1D-adrenergic receptors (AR) subtype selective antagonists were designed, synthesized and evaluated for their antagonistic activities towards α1-ARs (α1A, α1B,
- Xu, Fang,Chen, Hong,Xu, Jingyi,Liang, Xue,He, Xuelan,Shao, Binhao,Sun, Xianqiang,Li, Bing,Deng, Xiaoliang,Yuan, Mu
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- Design, synthesis and biological evaluation of novel arylpiperazine derivatives on human prostate cancer cell lines
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A series of novel arylpiperazine derivatives was synthesized. The in vitro cytotoxic activities of all synthesized compounds against three human prostate cancer cell lines (PC-3, LNCaP, and DU145) were evaluated by a CCK-8 assay. Compounds 10, 24 and 29 e
- Chen, Hong,Xu, Fang,Liang, Xue,Xu, Bing-Bing,Yang, Zong-Lin,He, Xue-Lan,Huang, Bi-Yun,Yuan, Mu
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- Synthesis and biological evaluation of arylpiperazine derivatives as potential anti-prostate cancer agents
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A novel scaffold of arylpiperazine derivatives was discovered as potent androgen receptor (AR) antagonist through rational drug designation based on our pre-work, leading to the discovery of a series of new antiproliferative compounds. Compounds 10, 16, 2
- Chen, Hong,Yu, Yu-Zhong,Tian, Xiu-Mei,Wang, Cai-Lu,Qian, Yu-Na,Deng, Zai-An,Zhang, Jing-Xiao,Lv, Dao-Jun,Zhang, Hai-Bo,Shen, Jian-Liang,Yuan, Mu,Zhao, Shan-Chao
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Read Online
- Synthesis and cytotoxic activity evaluation of novel arylpiperazine derivatives on human prostate cancer cell lines
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A series of novel arylpiperazine derivatives was synthesized. The in vitro cytotoxic activities of all synthesized compounds against three human prostate cancer cell lines (PC-3, LNCaP, and DU145) were evaluated by a CCK-8 assay. Compounds 9 and 15 exhibi
- Chen, Hong,Liang, Xue,Xu, Fang,Xu, Bingbing,He, Xuelan,Huang, Biyun,Yuan, Mu
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- FENTANYL HAPTENS FOR THE PREPARATION OF A FENTANYL VACCINE
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Described is the preparation of novel fentanyl haptens of Formula (1) through (6) and their use in the preparation of effective fentanyl vaccines.
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Paragraph 0199
(2021/07/24)
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- PYRIDINE COMPOUND SUBSTITUTED WITH AZOLE
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The present invention provides a compound represented by formula [I] shown below or a pharmaceutically acceptable salt thereof that has an inhibitory effect on 20-HETE producing enzyme. (in formula [I] above, the structure represented by formula [II] below: represents any of the structures represented by formula group [III] below: R1, R2, R3, and R4 independently represent a hydrogen atom, a fluorine atom, methyl, or the like, R5 represents any of the structures represented by formula group [IV]:
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Paragraph 0917; 1077
(2020/07/07)
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- Compounds and Their Use in Treating Cancer
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The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts and prodrugs thereof, where R1, R4, R5, R6, R7, Linker, X, Y, A, G, D and E have any of the meanings defined herein. This specification also relates to the use of such compounds and pharmaceutically acceptable salts and prodrugs thereof in methods of treatment of the human or animal body, for example in prevention or treatment of cancer. This specification also relates to processes and intermediate compounds involved in the preparation of such compounds and to pharmaceutical compositions containing them.
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Paragraph 0964; 0965
(2019/07/10)
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- ESTROGEN RECEPTOR-MODULATING COMPOUNDS
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Described herein are compounds that are estrogen receptor modulators of formula I' Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
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Paragraph 000243; 000274
(2019/08/08)
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- Aryl piperazine derivatives I and its salt, preparation method and use thereof
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The invention relates to the fields of pharmaceutical chemistry and lead compounds in drug discovery, and specifically relates to aryl piperazine derivatives (I). In the formula (I), the definitions of R1 to R5 have been represented in the description. Th
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Paragraph 0043-0045
(2018/04/20)
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- INHIBITORS OF THE MENIN-MLL INTERACTION
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The present invention is directed to inhibitors of the interaction of menin with MLL and MLL fusion proteins, pharmaceutical compositions containing the same, and their use in the treatment of cancer and other diseases mediated by the menin-MLL interaction.
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Page/Page column 125; 126
(2018/04/14)
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- Aryl piperazine derivatives II and its salt, preparation method and use thereof (by machine translation)
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The invention relates to the chemical, of pharmaceutical lead compound discovery field, and in particular relates to aryl piperazine derivatives (1) or (2). The invention also discloses the preparation of these aryl piperazine derivatives and the use of t
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Paragraph 0037; 0038; 0039
(2018/11/22)
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- Hydroxyzine derivative, and preparation method, application and preparation thereof
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The invention discloses a novel hydroxyzine derivative having the structure of the formula (I), a preparation method thereof, an application thereof in antitumor medicines, and a preparation. Compared with an antitumor medicine Naftopidil which is known i
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Paragraph 0081; 0082; 0083
(2017/08/10)
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- Ether aryl piperazine derivatives and salts thereof, preparation method and use thereof
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The invention discloses ether aryl piperazine derivatives and salt thereof as well as a preparation method and application of the ether aryl piperazine derivatives and in particular relates to an ether aryl piperazine derivative (I), wherein, the definiti
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Paragraph 0064; 0065; 0066
(2017/08/25)
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- COMPOSITE PREPARATION, CONTAINING NOVEL 3-(4-(BENZYLOXY)PHENYL)HEX-4-INOIC ACID DERIVATIVE AND ANOTHER ACTIVE INGREDIENT, FOR PREVENTING OR TREATING METABOLIC DISEASES
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The present invention relates to a pharmaceutical composition for preventing or treating metabolic diseases, in which a novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative and at least another active ingredient, which is selected from the group consisting of dipeptidyl peptidase-4 (DPPIV) inhibitor-based, sulfonylurea-based, thiazolidinedione (TZD)-based, biguanide-based, and sodium/glucose cotransporter 2 (SGLT2) inhibitor-based drugs, may be administered in combination or in the form of a composite preparation. The use of the composition of the present invention can provide a remarkably excellent blood sugar reducing effect in various animal diabetic disease models, and the composition of the present invention can be favorably used as a pharmaceutical composition for preventing or treating metabolic diseases, such as obesity, diabetes type I, diabetes type II, glucose intolerance symptoms, insulin resistance symptoms, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia, and syndrome X.
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Paragraph 0219-0221
(2017/09/04)
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- Ethers aryl-piperzine derivatives and salt, and preparation method and applications thereof in preparation of drug for treating anti-tumor drug
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The invention relates to ethers aryl-piperzine derivatives and salt, and a preparation method and applications thereof. The ethers aryl-piperzine derivatives have a structure shown in the formula I, and the salt of the ethers aryl-piperzine derivatives ha
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Paragraph 0054-0059
(2017/08/31)
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- NOVEL 3-(4(BENZYLOXY)PHENYL)HEX-4-INOIC ACID DERIVATIVE, METHOD OF PREPARING SAME AND PHARMACEUTICAL COMPOSITION FOR PREVENTING AND TREATING METABOLIC DISEASE INCLUDING SAME AS EFFECTIVE INGREDIENT
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The present invention relates to a novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, a preparation method thereof, and a pharmaceutical composition comprising the same as an active ingredient for the prevention and treatment of metabolic disease. The novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention has excellent activities of activating GPR40 protein and promoting insulin secretion accordingly but has no toxicity when co-administered with other drugs. That is, the novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention can be co-administered with other drugs and can promote the activation of GPR40 protein significantly, so that the composition comprising the same as an active ingredient can be efficiently used as a pharmaceutical composition for the prevention and treatment of metabolic disease such as obesity, type I diabetes, type II diabetes, incompatible glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia, and syndrome X, etc.
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Paragraph 0325-0327
(2016/02/18)
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- Imide type of phenyl piperazine derivatives and salts thereof, preparation method and use
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The invention discloses imide phenylpiperazine derivatives as well as salts, a preparation method and an application of the imide phenylpiperazine derivatives. The imide phenylpiperazine derivatives are as shown in the specification (I), wherein m, n, o,
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Paragraph 0139; 0140; 0141
(2016/10/09)
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- Clay-Supported Cu(II) Catalyst: An Efficient, Heterogeneous, and Recyclable Catalyst for Synthesis of 1,4-Disubstituted 1,2,3-Triazoles from Alloxan-Derived Terminal Alkyne and Substituted Azides Using Click Chemistry
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A novel series of alloxan-derived 1,4-disubstituted 1,2,3-triazoles was synthesized in excellent yields under catalytic conditions using a click reaction strategy through 1,3-dipolar cycloaddition. Their structures have been ascertained on the basis of spectroanalytical and elemental analysis data. Synthesis of hybrid compounds with varying substitutions in the triazole ring was achieved by reaction between alloxan-derived terminal alkyne and a pertinent azide derivative in the presence of clay-Cu(II) as the catalyst in methanolic medium. Also, comparative evaluation of various catalytic systems [viz., CuI, CuSO4, CuI-zeolite, K10Ti, and clay-Cu(II)] was investigated. Of these catalytic systems, clay-Cu(II) was observed to be the best. The catalyst was recyclable for several runs without showing significant loss in its activity. The good selectivity, cost-efficiency, short reaction time, milder reaction conditions, and simple workup procedure are the added salient features of this synthetic protocol.
- Dubey, Nitin,Sharma, Pratibha,Kumar, Ashok
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p. 2608 - 2626
(2015/11/28)
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- Structure-Based Design and Optimization of Multitarget-Directed 2 H -Chromen-2-one Derivatives as Potent Inhibitors of Monoamine Oxidase B and Cholinesterases
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The multifactorial nature of Alzheimer's disease calls for the development of multitarget agents addressing key pathogenic processes. To this end, by following a docking-assisted hybridization strategy, a number of aminocoumarins were designed, prepared, and tested as monoamine oxidases (MAOs) and acetyl- and butyryl-cholinesterase (AChE and BChE) inhibitors. Highly flexible N-benzyl-N-alkyloxy coumarins 2-12 showed good inhibitory activities at MAO-B, AChE, and BChE but low selectivity. More rigid inhibitors, bearing meta- and para-xylyl linkers, displayed good inhibitory activities and high MAO-B selectivity. Compounds 21, 24, 37, and 39, the last two featuring an improved hydrophilic/lipophilic balance, exhibited excellent activity profiles with nanomolar inhibitory potency toward hMAO-B, high hMAO-B over hMAO-A selectivity and submicromolar potency at hAChE. Cell-based assays of BBB permeation, neurotoxicity, and neuroprotection supported the potential of compound 37 as a BBB-permeant neuroprotective agent against H2O2-induced oxidative stress with poor interaction as P-gp substrate and very low cytotoxicity.
- Farina, Roberta,Pisani, Leonardo,Catto, Marco,Nicolotti, Orazio,Gadaleta, Domenico,Denora, Nunzio,Soto-Otero, Ramon,Mendez-Alvarez, Estefania,Passos, Carolina S.,Muncipinto, Giovanni,Altomare, Cosimo D.,Nurisso, Alessandra,Carrupt, Pierre-Alain,Carotti, Angelo
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p. 5561 - 5578
(2015/08/03)
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- BENZAMIDE DERIVATIVES AND THEIR USE AS HSP90 INHIBTORS
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The invention provides a compound which is (a) a phenylamide derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate, prodrug or solvate thereof: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.
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Page/Page column 98
(2012/01/05)
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- Reduction of pentafluorophenyl esters to the corresponding primary alcohols using sodium borohydride
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Primary alcohols and chiral N-protected 2-amino alcohols can be obtained in high yields from the reaction of pentafluorophenyl esters of the corresponding carboxylic acids with sodium borohydride in THF under mild conditions. This reductive method is rapid and compatible with various functional groups as well as with the most common N-protective groups Z, Boc and Fmoc.
- Papavassilopoulou, Eleni,Christofis, Petros,Terzoglou, Despina,Moutevelis-Minakakis, Panagiota
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p. 8323 - 8325
(2008/04/13)
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- AZOLE AND THIAZOLE DERIVATIVES AND THEIR USE
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Compounds of formula (I) are useful in the treatment of diseases where enhanced M3 receptor activation is implicated, such as respiritory tract diseases: wherein (i) R1 is C1-C6-alkyl or hydrogen; and R2 is hydrogen or a group -R7, -Z-Y-R7, -Z-NR9R10; -Z-CO-NR9R10, -Z-NR9-[AE11]C(O)O-R7, or -Z-C(O)-R7; and R3 is a lone pair, or C1C6-alkyl; or (ii) R1 and R3 together with the nitrogen to which they are attached form a heterocycloalkyl ring, and R2 is a lone pair or a group -R7, -Z-Y-R7, -Z-NR9R10, -Z-CO-NR9R10, -Z-NR9-[AE12]C(O)O-R7; or; -Z-C(O)-R7; or (iii) R1 and R2 together with the nitrogen to which they are attached form a heterocycloalkyl ring, said ring being substituted by a group -Y-R7, -Z-Y-R7, -Z-NR9R10; -Z-CO-NR9R10; -Z-NR9-[AE13]C(O)O-R7; or; -Z-C(O)-R7; and R3 is a lone pair, or C1-C6-aIkyl; R4 and R5 are independently selected from the group consisting of aryl, arytfused-heterocycloalkyl, heteroaryl, C1-C6-alkyl, cycloalkyl; R6 is -OH, C1-C6-alkyl, C1-C6-alkoxy, hydroxy-C1-C6-alkyl, nitrile, a group CONR82 or a hydrogen atom; A is an oxygen or a sulfur atom; X is an alkylene, alkenylene or alkynylene group; R7 is an C1-C6-alkyl, aryl, aryl-fused-cycloalkyl, aryl-ffused-heterocycloalkyl, heteroaryl, aryl(C1-C8-alkyl)-, heteroaryl(C1-C8-alkyl)-, cycloalkyl or heterocycloalkyl group; R8 is C1-C6-alkyl or a hydrogen atom; Z is a C1-C16-alkylene, C2-C16-alkenylene or C2-C16-alkynylene group; Y is a bond or oxygen atom; R9 and R10 are independently a hydrogen atom, C1-C6-alkyl, aryl, aryl-fused-heterocycloalkyl, aryl-fused-cycloalkyl, heteroaryl, aryl(C1-C6-alkyl)-, or heteroaryl(C1-C6-alkyl)- group; or R9 and R10 together with the nitrogen atom to which they are attached form a heterocyclic ring of 48 atoms, optionally containing a further nitrogen or oxygen atom.
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Page/Page column 49
(2010/11/25)
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- Solid-supported synthesis of highly functionalized tripodal peptides with flexible but preorganized geometry: Towards potential serine protease mimics
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Tripodal scaffold 1 has been used in the synthesis of a representative member of a library of serine protease mimics, possessing three independent functionalized peptide chains on a central core. Each peptide chain contains one residue of the classical ca
- Gea, An,Farcy, Nadia,Roque I Rossell, Nuria,Martins, Jose C.,De Clercq, Pierre J.,Madder, Annemieke
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p. 4135 - 4146
(2007/10/03)
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- A pentaerythritol-based molecular scaffold for solid-phase combinatorial chemistry
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(Matrix Presented) A convergent synthesis has been developed for the preparation of solid-phase bound construct 1, consisting of an orthogonally protected trifunctional core structure that is attached to TentaGel via a photocleavable linker.
- Farcy, Nadia,De Muynck, Hilde De,Madder, Annemieke,Hosten, Noel,De Clercq, Pierre J.
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p. 4299 - 4301
(2007/10/03)
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- Substituted sulfonamides, process of preparation and medicines containing same
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The present invention concerns new substituted sulfonamides, and the physiologically acceptable salts possibly in the form of complexes, esters and amides thereof, represented by the formula: STR1
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- Carbacyclin analogs
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Carbacyclin analogs that exhibit platelet aggregation inhibition activity and other biological activites common to structurally related prostacyclins are provided.
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- A NEW PREPARATION OF 4-(BOC-AMINOACYLOXYMETHYL)PHENYLACETIC ACIDS FOR SOLID-PHASE PEPTIDE SYNTHESIS
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A new preparation of 4-(BOC-aminoacyloxymethyl)phenylacetic acids 1, constisting of an esterification of the corresponding BOC-amino acids 2 with 4-(bromomethyl)phenethyl alcohol 3, followed by a Collins oxidation and an oxidation with sodium chlorite is
- Plaue, Serge,Heissler, Denis
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p. 1401 - 1404
(2007/10/02)
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