- L-selectride as a convenient reagent for the selective cleavage of carbamates
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L-Selectride(R) was shown to selectively cleave methyl carbamates in the presence of more sterically demanding carbamates, including the selective cleavage of a methyl carbamate in the presence of an N-Boc group.
- Coop, Andrew,Rice, Kenner C.
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Read Online
- Synthesis, mechanistic studies, and anti-proliferative activity of glutathione/glutathione S-transferase-activated nitric oxide prodrugs
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Nitric oxide (NO) prodrugs such as O2-(2,4-dinitrophenyl) 1-[(4-ethoxycarbonyl)piperazin-1-yl]diazen-1-ium-1,2-diolate (JS-K) are a growing class of promising NO-based therapeutics. Nitric oxide release from the anti-cancer lead compound, JS-K, is proposed to occur through a nucleophilic aromatic substitution by glutathione (GSH) catalyzed by glutathione S-transferase (GST) to form a diazeniumdiolate anion that spontaneously releases NO. In this study, a number of structural analogues of JS-K were synthesized and their chemical and biological properties were compared with those of JS-K. The homopiperazine analogue of JS-K showed anti-cancer activity that is comparable with that of JS-K but with a diminished reactivity towards both GSH and GSH/GST; both the aforementioned compounds displayed no cytotoxic activity towards normal renal epithelial cell line at concentrations where they significantly diminished the proliferation of a panel of renal cancer cell lines. These properties may prove advantageous in the further development of this class of nitric oxide prodrugs as cancer therapeutic agents.
- Chakrapani, Harinath,Kalathur, Ravi C.,Maciag, Anna E.,Citro, Michael L.,Ji, Xinhua,Keefer, Larry K.,Saavedra, Joseph E.
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Read Online
- Heteroaryl substituted dihydro pyrimidine compounds and their use in medicine
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The invention relates to heteroaryl-substituted dihydropyrimidine compounds and application thereof in medicines, particularly application in medicines for treating and preventing hepatitis B. Particularly, the invention relates to compounds disclosed as general formula (I) or (Ia), or enantiomers, diastereoisomers, hydrates, solvates or pharmaceutically acceptable salts thereof, wherein the variables are defined in the specification. The invention also relates to application of the compounds disclosed as general formula (I) or (Ia), or enantiomers, diastereoisomers, hydrates, solvates or pharmaceutically acceptable salts thereof, especially application in medicines for treating and preventing hepatitis B.
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Paragraph 0458; 0461; 0462
(2018/02/23)
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- A carbonyl group-containing modified multi-amine and its preparation method and its in the polyfunctional acrylate in the application of the
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The invention relates to carbonyl-containing modified heterocyclic amine, a preparation method and application in multifunctional acrylic ester thereof. The carbonyl-containing modified heterocyclic amine is heterocyclic amine containing at least two ring structures, and is formed through carrying out ammonolysis reaction on carbonic ester and cycloaliphatic diamine, wherein the cycloaliphatic diamine is one or more selected from piperazine, isophorone diamine, 1, 4-hexamethylenediamine, 1-methyl-2, 4-diaminocyclohexane, N, N'-dimethyl-1 and 2-diaminocyclohexane. According to the application, when the carbonyl-containing modified heterocyclic amine is applied to multifunctional acrylic ester, the curing velocity of multifunctional acrylic ester is remarkably increased, the cure shrinkage rate of multifunctional acrylic ester is decreased, and the hardness and high temperature resistance of multifunctional acrylic ester are remarkably improved; and besides, the generated carbonyl-containing modified heterocyclic amine multifunctional acrylic ester has the characteristics of being light in smell, and small in amine mobility and less prone to yellowing.
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Paragraph 0071-0074
(2017/10/22)
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- Heteroaryl substituted dihydro pyrimidine compounds and their use in medicine
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The invention relates to heteroaryl-substituted dihydropyrimidine compounds and application thereof in medicines, particularly application in medicines for treating and preventing hepatitis B. Particularly, the invention relates to compounds disclosed as general formula (I) or (Ia), or enantiomers, diastereoisomers, hydrates, solvates or pharmaceutically acceptable salts thereof, wherein the variables are defined in the specification. The invention also relates to application of the compounds disclosed as general formula (I) or (Ia), or enantiomers, diastereoisomers, hydrates, solvates or pharmaceutically acceptable salts thereof, especially application in medicines for treating and preventing hepatitis B.
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Paragraph 0465-0469
(2017/08/14)
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- BENZOPIPERIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER AND HEMOGLOBINOPATHIES
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A compound of formula I: (I) wherein: n is 1 or 2; p is 0 or 1; R1a, R1b, R1c and R1d are independently selected from H, halo, C1-4 alkyl, C1-4 fluoroalkyl, C3-4 cycloalkyl, C1-4 alkyloxy, NH-C1-4 alkyl and cyano; R2a and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2e is H or Me; R3a and R3b are independently selected from H and Me; R4 is either H or Me; R5 is either H or Me; R6a and R6b are independently selected from H and Me; A is either (IIa), where R7a is selected from N-linked N-containing C5-7 heterocycyl and (A); or (ii) (IIb), where X is selected from CH2, N H and O, one of R8a and R8b is selected from CI and ethoxy and the other of R8a and R8b is H.
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Page/Page column 52
(2017/09/27)
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- Protein-protein communication and enzyme activation mediated by a synthetic chemical transducer
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The design and function of a synthetic chemical transducer that can generate an unnatural communication channel between two proteins is described. Specifically, we show how this transducer enables platelet-derived growth factor to trigger (in vitro) the catalytic activity of glutathione-s-transferase (GST), which is not its natural enzyme partner. GST activity can be further controlled by adding specific oligonucleotides that switch the enzymatic reaction on and off. We also demonstrate that a molecular machine, which can regulate the function of an enzyme, could be used to change the way a prodrug is activated in a programmable manner.
- Peri-Naor, Ronny,Ilani, Tal,Motiei, Leila,Margulies, David
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supporting information
p. 9507 - 9510
(2015/08/18)
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- CARBODITHIOATES WITH SPERMICIDAL ACTIVITY AND PROCESS FOR PREPARATION THEREOF
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The present invention relates to the synthesis and biological evaluation of compound of formula I as spermicidal agents, and its pharmaceutically acceptable acid salt thereof. The invention provides bis(4- substituted-1-piperazinylthiocarbonyl) disulfide (when n = 0) and alkane-1,n-diylbis(4-substituted piperazine-1-carbodithioate) (when n = 0, 1, 2 or 3) as shown in figure 1 of the accompanying drawing. These compounds are found to be useful for spermicidal activity.
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Page/Page column 41
(2014/08/20)
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- Substituted phenoxypropyl-(R)-2-methylpyrrolidine aminomethyl ketones as histamine-3 receptor inverse agonists
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Optimization of a series of aminomethyl ketone diamine H3R antagonists to reduce the brain exposure by lowering the pKa, led to molecules with improved pharmacokinetic properties. Compounds 9, 19, and 25 had high affinity for human H3R and demonstrated in vivo H3R functional activity in the rat dipsogenia model. Compound 9 displayed modest wake-promoting activity in the rat EEG/EMG model.
- Zulli, Allison L.,Aimone, Lisa D.,Mathiasen, Joanne R.,Gruner, John A.,Raddatz, Rita,Bacon, Edward R.,Hudkins, Robert L.
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scheme or table
p. 2807 - 2810
(2012/05/20)
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- Unsymmetrical tetrasubstituted ureas from tertiary carbamoylimidazole: Activation by AlMe3
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An efficient and general method for the synthesis of unsymmetrical tetrasubstituted ureas from carbamoylimidazole is described. The conversion is achieved by the concurrent quarternization of the imidazole nitrogen and activation of amines with AlMe3. The Royal Society of Chemistry 2012.
- Velavan,Sumathi,Balasubramanian
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supporting information; experimental part
p. 6420 - 6431
(2012/09/05)
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- CDI-mediated monoacylation of symmetrical diamines and selective acylation of primary amines of unsymmetrical diamines
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A highly efficient and green protocol for monoacylation of symmetrical diamines and chemoselective acylation of primary amines of unsymmetrical diamines has been developed.
- Verma, Sanjeev K.,Ghorpade, Ramarao,Pratap, Ajay,Kaushik
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experimental part
p. 326 - 329
(2012/04/10)
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- Dendritic polymers with enhanced amplification and interior functionality
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Poly(ester-acrylate) and poly(ester/epoxide) dendrimers. These materials can be synthesized by utilizing the so-called “sterically induced stoichiometric” principles. The preparation of the dendrimers is carried out by reacting precursor amino/polyamino-functional core materials with various branch cell reagents. The branch cell reagents are dimensionally large, relative to the amino/polyamino-initiator core and when reacted, produce generation=1 dendrimers directly in one step. There is also a method by which the dendrimers can be stabilized and that method is the reaction of the dendrimers with surface reactive molecules to pacify the reactive groups on the dendrimers.
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- Tetracyclic benzimidazole derivatives and combinatorial libraries thereof
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The present invention relates to novel tetracyclic benzimidazole derivative compounds of the following formula: wherein R1to R10have the meanings described in here. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing tetracyclic benzimidazole derivative compounds.
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- 14-substituted marcfortines and derivatives useful as antiparasitic agents
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There are disclosed 14α-hydroxymarcfortine derivatives of the natural products marcfortine A, B, C, and D useful in the treatment and prevention of helminth and arthropod infections of animals and plants. The synthetic derivatives are of Formula (I). STR1
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- Marcfortine/paraherquamide derivatives useful as antiparasitic agents
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There are disclosed 18-thiomarcfortine derivatives of the natural products marcfortine A, B and C, C-18 thioparaherquamide and derivatives thereof, novel N-1 marcfortines A, B, and C and derivatives thereof, novel N-1 paraherquamide and derivatives thereof usefull in the treatment and prevention of helninth and arthropod infections of animals and plants. Any inquiry concerning this communication or earlier communications from the examiner should be directed to Examiner Robert T. Bond whose telephone number is (703)308-4711. The examiner can normally be reached on Monday through Friday from 8:00 AM to 4:30 PM.
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- Scavenger assisted combinatorial process for preparing libraries of amides, carbamates and sulfonamides
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This invention relates to a novel solution phase process for the preparation of amide, carbamate, and sulfonamide combinatorial libraries. These libraries have utility for drug discovery and are used to form wellplate components of novel assay kits.
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- Antiatherosclerotic and antithrombotic 1-benzopyran-4-ones and 2-amino-1,3-benzoxazine-4-ones
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This invention relates to compounds of Formula I STR1 which are useful in association with a pharmaceutical carrier as antiatherosclerotic agents. In addition, various compounds of Formula I are useful inhibitors of cell proliferation.
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- Antiatherosclerotic and antithrombotic 2-amino-6-phenyl-4H-pyran-4-ones
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This invention relates to compounds of Formula I STR1 which are useful as antiatherosclerotic agents and inhibitors of cell proliferation for the treatment of proliferative diseases. In addition, various compounds of Formula I are useful inhibitors of platelet aggregation.
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- Pharmaceutical compositions of N-heterocyclic benzenesulfonamides and their use
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The invention relates to new N-cyclic benzenesulfonamides, their process of preparation and their use as active substance of pharmaceutical compositions. The new benzenesulfonamides according to the invention correspond to the following general formula (I): STR1 in which: V represents, for example, hydrogen, W represents, for example CF3, X represents, for example, hydrogen, Y represents, for example, hydrogen, n is 2 or 3, Z represents, for example, the group NR4, in which R4 represents, for example, hydrogen. These compounds are useful in pharmaceutical compositions for the treatment of nervous disorders with anxiety.
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- Studies in Potential Filaricides: Part XV - Synthesis of 1-Acyl/Aryl-4-substituted-piperazines as Diethylcarbamazine Analogs
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1-Acyl-4-substituted-piperazines (4-29) have been prepared starting from 1-benzylpiperazine while 1-aryl-4-aroylpiperazines (30-44) have been obtained from the corresponding 1-arylpiperazines.None of the compounds shows any significant filaricidal activity against Litomosoides carinii in cotton rats and cestodicial activity against Hymenolepis nana in mice.
- Agrawal, V. K.,Sharma, Satyavan
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p. 650 - 654
(2007/10/02)
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