- A Unified Approach to Decarboxylative Halogenation of (Hetero)aryl Carboxylic Acids
-
Aryl halides are a fundamental motif in synthetic chemistry, playing a critical role in metal-mediated cross-coupling reactions and serving as important scaffolds in drug discovery. Although thermal decarboxylative functionalization of aryl carboxylic acids has been extensively explored, the scope of existing halodecarboxylation methods remains limited, and there currently exists no unified strategy that provides access to any type of aryl halide from an aryl carboxylic acid precursor. Herein, we report a general catalytic method for direct decarboxylative halogenation of (hetero)aryl carboxylic acids via ligand-to-metal charge transfer. This strategy accommodates an exceptionally broad scope of substrates. We leverage an aryl radical intermediate toward divergent functionalization pathways: (1) atom transfer to access bromo- or iodo(hetero)arenes or (2) radical capture by copper and subsequent reductive elimination to generate chloro- or fluoro(hetero)arenes. The proposed ligand-to-metal charge transfer mechanism is supported through an array of spectroscopic studies.
- Blakemore, David C.,Castellano, Felix N.,Chen, Tiffany Q.,Danilov, Evgeny O.,Dechert-Schmitt, Anne-Marie,Dow, Nathan W.,Fayad, Remi,Hauke, Cory E.,Knauber, Thomas,Macmillan, David W. C.,Pedersen, P. Scott,Rosko, Michael C.
-
supporting information
(2022/05/20)
-
- MYST FAMILY HISTONE ACETYLTRANSFERASE INHIBITORS
-
The present disclosure provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
- -
-
Paragraph 0337-0340; 0336
(2019/06/19)
-
- Complexes featuring N-heterocyclic carbenes with bowl-shaped wingtips
-
Three imidazolium salts having their two N-substituents equipped with remote calix[4]arenyl termini have been synthesised and converted into N-heterocyclic carbene (NHC) complexes of the type [PdCl2(NHC)(pyridine)]. An X-ray diffraction study c
- Almallah, Hamzé,Nos, Mélodie,Ayzac, Virgile,Brenner, Eric,Matt, Dominique,Gourlaouen, Christophe,Jahjah, Mohamad,Hijazi, Akram
-
p. 299 - 309
(2019/03/02)
-
- FNEW ACTIVATORS OF SIRT1 ENZYME FOR THE TREATMENT OF CARDIOVASCULAR AND CARDIOMETABOLIC PATHOLOGIES
-
This invention describes a class of compounds able to activate the human SIRT1 enzyme and regulate many metabolic functions. This invention relates to compounds that can be employed in medical applications, specifically for the treatment or prevention of cardiometabolic diseases, such as diabetes, and of cardiovascular disorders, such as coronaropathy, heart failure and atherosclerosis.
- -
-
Page/Page column 13; 17; 29
(2019/09/12)
-
- Investigation of the molecular characteristics of bisindole inhibitors as HIV-1 glycoprotein-41 fusion inhibitors
-
In previous work, we described 6-6‘-bisindole compounds targeting a hydrophobic pocket on the N-heptad repeat region of viral glycoprotein-41 as effective inhibitors of HIV-1 fusion. Two promising compounds with sub-micromolar IC50's contained a benzoic acid group and a benzoic acid ester attached at the two indole nitrogens. Here we have conducted a thorough structure-activity relationship (SAR) study evaluating the contribution of each of the ring systems and various substituents to compound potency. Hydrophobicity, polarity and charge were varied to produce 35 new compounds that were evaluated in binding, cell-cell fusion and viral infectivity assays. We found that (a) activity based solely on increasing hydrophobic content plateaued at ～ 200 nM; (b) the bisindole scaffold surpassed other heterocyclic ring systems in efficacy; (c) a polar interaction possibly involving Gln575 in the pocket could supplant less specific hydrophobic interactions; and (d) the benzoic acid ester moiety did not appear to form specific contacts with the pocket. The importance of this hydrophobic group to compound potency suggests a mechanism whereby it might interact with a tertiary component during fusion, such as membrane. A promising small molecule 10b with sub-μM activity was discovered with molecular weight 500 da and reduced logP compared to earlier compounds. The work provides insight into requirements for small molecule inhibition of HIV-1 fusion.
- Zhou, Guangyan,Chu, Shidong,Nemati, Ariana,Huang, Chunsheng,Snyder, Beth A.,Ptak, Roger G.,Gochin, Miriam
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supporting information
p. 533 - 542
(2018/11/06)
-
- Selective Oxidative Coupling Reaction of Isocyanides Using Peroxide as Switchable Alkylating and Alkoxylating Reagent
-
A switchable oxidative coupling reaction of isocyanide and peroxide has been disclosed. In the presence of iron catalyst, the coupling reaction affords N-arylacetamides in good yields. By simply replacing the iron with copper catalyst, another different coupling reaction takes place in which peroxide can serve as alkoxylating source. This protocol represents a new fundamental coupling of two basic chemicals involving C?C and C?O bond-forming process. The unusual reactivity of an isocyano group in a radical reaction acting formally as an amidoyl synthon has also been well established. The experiment outcome reveals that aromatic isocyanides are particularly compatible reaction partners in present coupling reaction, whereas no desired products are observed when aliphatic isocyanides are used. (Figure presented.).
- Zhang, Xinglu,Liu, Zhiqiang,Gao, Yu,Li, Feng,Tian, Yaming,Li, Chunju,Jia, Xueshun,Li, Jian
-
supporting information
p. 272 - 277
(2017/11/13)
-
- A relay FRET event in a designed trichromophoric pentapeptide containing an: O -, m -aromatic-amino acid scaffold
-
The concept of a relay FRET event is established in a designed trichromophoric pentapeptide containing an o-,m-aromatic amino acid scaffold in the backbone as a novel β-turn mimetic β-sheet folding nucleator. This system would find application in studying fundamental processes involving interbiomolecular interactions in chemical biology.
- Bag, Subhendu Sekhar,Yashmeen, Afsana
-
supporting information
p. 9765 - 9768
(2018/09/10)
-
- Reevaluating the Substrate Specificity of the L-Type Amino Acid Transporter (LAT1)
-
The L-type amino acid transporter 1 (LAT1, SLC7A5) transports essential amino acids across the blood-brain barrier (BBB) and into cancer cells. To utilize LAT1 for drug delivery, potent amino acid promoieties are desired, as prodrugs must compete with millimolar concentrations of endogenous amino acids. To better understand ligand-transporter interactions that could improve potency, we developed structural LAT1 models to guide the design of substituted analogues of phenylalanine and histidine. Furthermore, we evaluated the structure-activity relationship (SAR) for both enantiomers of naturally occurring LAT1 substrates. Analogues were tested in cis-inhibition and trans-stimulation cell assays to determine potency and uptake rate. Surprisingly, LAT1 can transport amino acid-like substrates with wide-ranging polarities including those containing ionizable substituents. Additionally, the rate of LAT1 transport was generally nonstereoselective even though enantiomers likely exhibit different binding modes. Our findings have broad implications to the development of new treatments for brain disorders and cancer.
- Chien, Huan-Chieh,Colas, Claire,Finke, Karissa,Springer, Seth,Stoner, Laura,Zur, Arik A.,Venteicher, Brooklynn,Campbell, Jerome,Hall, Colton,Flint, Andrew,Augustyn, Evan,Hernandez, Christopher,Heeren, Nathan,Hansen, Logan,Anthony, Abby,Bauer, Justine,Fotiadis, Dimitrios,Schlessinger, Avner,Giacomini, Kathleen M.,Thomas, Allen A.
-
supporting information
p. 7358 - 7373
(2018/08/06)
-
- Effective approach to ureas through organocatalyzed one-pot process
-
An efficient approach to N, N′-unsymmetrically substituted ureas 9 has been developed through the ammonolysis process of N-Boc protected anilines 7 with amines prompted by 1,5,7-triazabicyclo[4.4.0]dec-5-ene (TBD). Moreover, a convenient protocol for the
- Wang, Mingliang,Han, Jilai,Si, Xiaojia,Hu, Yimin,Zhu, Jidong,Sun, Xun
-
supporting information
p. 1614 - 1618
(2018/03/28)
-
- Teaching Old Compounds New Tricks: DDQ-Photocatalyzed C?H Amination of Arenes with Carbamates, Urea, and N-Heterocycles
-
The C?H amination of benzene derivatives was achieved using DDQ as photocatalyst and BocNH2 as the amine source under aerobic conditions and visible light irradiation. Electron-deficient and electron-rich benzenes react as substrates with moderate to good product yields. The amine scope of the reaction comprises Boc-amine, carbamates, pyrazoles, sulfonimides and urea. Preliminary mechanistic investigations indicate arene oxidation by the triplet of DDQ to radical cations with different electrophilicity and a charge transfer complex between the amine and DDQ as intermediate of the reaction.
- Das, Somnath,Natarajan, Palani,K?nig, Burkhard
-
supporting information
p. 18161 - 18165
(2017/12/28)
-
- HETEROARYL COMPOUNDS AND PHARMACEUTICAL APPLICATIONS THEREOF
-
The present invention provides herein is a heteroaryl compound or a stereoisomer, a geometric isomer, a tautomer, a racemate, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, as well as a pharmaceutical composition containing the compound disclosed herein. The present invention also provides herein is use of the compound or the pharmaceutical composition thereof disclosed herein in the manufacture of a medicine for treating autoimmune diseases or proliferative diseases.
- -
-
Paragraph 00528
(2016/01/25)
-
- Highly ortho-Selective Chlorination of Anilines Using a Secondary Ammonium Salt Organocatalyst
-
An organocatalytic, highly facile, efficient, and regioselective ortho-chlorination of anilines is described. A secondary ammonium chloride salt has been employed as the catalyst and the reaction can be conducted at room temperature without protection from air and moisture. In addition, the reaction is readily scalable and the catalyst can be recycled and reused. This catalytic protocol has been applied to the efficient synthesis of a highly potent c-Met kinase inhibitor. Mechanistic studies revealed that unique structural features of the secondary ammonium chloride salt are important for both the catalysis and regioselectivity of the electrophilic ortho-chlorination.
- Xiong, Xiaodong,Yeung, Ying-Yeung
-
supporting information
p. 16101 - 16105
(2016/12/26)
-
- Betti reaction enables efficient synthesis of 8-hydroxyquinoline inhibitors of 2-oxoglutarate oxygenases
-
There is interest in developing potent, selective, and cell-permeable inhibitors of human ferrous iron and 2-oxoglutarate (2OG) oxygenases for use in functional and target validation studies. The 3-component Betti reaction enables efficient one-step C-7 functionalisation of modified 8-hydroxyquinolines (8HQs) to produce cell-active inhibitors of KDM4 histone demethylases and other 2OG oxygenases; the work exemplifies how a template-based metallo-enzyme inhibitor approach can be used to give biologically active compounds.
- Thinnes,Tumber,Yapp,Scozzafava,Yeh,Chan,Tran,Hsu,Tarhonskaya,Walport,Wilkins,Martinez,Müller,Pugh,Ratcliffe,Brennan,Kawamura,Schofield
-
supporting information
p. 15458 - 15461
(2015/10/20)
-
- Triazolo-β-aza-ε-amino acid and its aromatic analogue as novel scaffolds for β-turn peptidomimetics
-
Triazolo-β-aza-ε-amino acid and its aromatic analogue (AlTAA/ArTAA) in the peptide backbone mark a novel class of conformationally constrained molecular scaffolds to induce β-turn conformations. This was demonstrated forAlTAA in a Leu-enkephalin analogue and in a designed pentapeptide wherein the FRET process was established. Restricted rotation induced chirality and turn conformation into the achiral aromatic amino acid scaffold,ArTAA, which in a short tripeptide backbone acted as a β-turn mimic as a β-sheet folding nucleator. This journal is
- Bag, Subhendu Sekhar,Jana, Subhashis,Yashmeen, Afsana,De, Suranjan
-
supporting information
p. 5242 - 5245
(2015/03/30)
-
- INHIBITORS OF THE MITF MOLECULAR PATHWAY
-
Provided herein are compounds of the formula (IV) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful as MITF inhibitors, MITF pathway inhibitors and for the treatment of cancer.
- -
-
Paragraph 00187
(2015/01/09)
-
- CaMKII INHIBITORS AND USES THEREOF
-
The present invention provides compounds useful as inhibitors of Ca2+/calmodulindependent protein kinase (CaMKII), compositions thereof, and methods of using the same. Cardiovascular disease remains the number one cause of death in developed countries. Furthermore, incidence of cardiovascular disease has increased dramatically in developing countries. Although cardiovascular disease usually affects older adults, the antecedents of cardiovascular disease, notably atherosclerosis, begin in early life, making primary prevention efforts necessary from childhood.
- -
-
Paragraph 00191-00192
(2014/09/29)
-
- A 2,6-bis(phenylamino)pyridinato titanium catalyst for the highly regioselective hydroaminoalkylation of styrenes and 1,3-butadienes
-
The C-C bond forming catalytic hydroaminoalkylation of terminal alkenes, 1,3-dienes, or styrenes allows a direct and highly atom efficient (100 %) synthesis of amines which can result in the formation of two regioisomers, the linear and the branched product. We present a new titanium catalyst with 2,6-bis(phenylamino)pyridinato ligands for intermolecular hydroaminoalkylation reactions of styrenes and 1-phenyl-1,3-butadienes that delivers the corresponding linear hydroaminoalkylation products with excellent regioselectivities. Linear progress: A new Ti complex with 2,6-bis(phenylamino) pyridinato ligands catalyzes highly regioselective hydroaminoalkylation reactions of styrenes. The process that directly gives access to the corresponding linear hydroaminoalkylation products offers a new and flexible synthetic approach towards pharmaceutically important 3-arylpropylamines. It is also possible to convert (E)-1-phenyl-1,3-butadienes into the corresponding linear products.
- Doerfler, Jaika,Preuss, Till,Schischko, Alexandra,Schmidtmann, Marc,Doye, Sven
-
supporting information
p. 7918 - 7922
(2014/08/05)
-
- Nano-ferrous ferric oxide (nano-Fe3O4): Powerful, reusable, and stable catalyst for N-Boc protection of amines
-
Nano-ferrous ferric oxide (nano-Fe3O4) efficiently catalyzed N-boc protection of amines in high yields and acceptable reaction times. Nano-Fe3O4 was applied as an efficient, green, heterogeneous and reusable magnetite catalyst. Clean reaction, simple purification, short reaction time and high yield were some other advantages of this compound.
- Zolfigol, Mohammad Ali,Moosavi-Zare, Ahmad Reza,Moosavi, Parvin,Khakyzadeh, Vahid,Zare, Abdolkarim
-
p. 962 - 966
(2013/11/06)
-
- Magnetic nanoparticles catalyzed N-tert-butoxycarbonylation of Amines and amine derivatives
-
A simple and efficient protocol for the chemoselective mono-N-Boc protection of various structurally diverse amines with di-tert-butyl dicarbonate using magnetically recoverable γ-Fe2O3@SiO 2 nanoparticles is reported. The catalyst can be easily recovered and recycled without a significant loss in the catalytic activity. No competitive side reactions, such as formation of isocyanate, urea, oxazolidinone, and N,N-di-Boc derivatives were obsereved.
- Akbari, Jafar,Sajirani, Soghra B.,Nezhad, Jafar M.,Heydari, Akbar
-
experimental part
p. 165 - 168
(2012/07/14)
-
- Simple and efficient method for n-boc protection of amines using PEG-400 as a reaction medium under mild conditions
-
Simple and efficient method for N-Boc protection of amines using PEG-400 as an ecofriendly reaction medium at room temperature is described. Various aromatic, heteroaromatic, and aliphatic amines were converted to the corresponding N-tert-butyl-carbamates in good to excellent yields in short times.
- Zeng, Hongyao,Li, Yongjia,Shao, Huawu
-
experimental part
p. 25 - 32
(2011/10/19)
-
- Chemical synthesis, biological evaluation and structure-activity relationship analysis of azaisoindolinones, a novel class of direct enoyl-ACP reductase inhibitors as potential antimycobacterial agents
-
The synthesis and biological evaluation of azaisoindolinone compounds embedding a lipophilic chain on the framework were performed. These compounds were designed as InhA inhibitors and as anti-Mycobacterium tuberculosis agents. Structure-activity relation
- Deraeve, Céline,Dorobantu, Ioana Miruna,Rebbah, Farah,Le Quéméner, Frédéric,Constant, Patricia,Quémard, Anna?k,Bernardes-Génisson, Vania,Bernadou, Jean,Pratviel, Geneviève
-
supporting information; experimental part
p. 6225 - 6232
(2011/12/14)
-
- Synthesis and crystal structure determination of [H2-cryptand 222](Br3)2: A unique tribromide catalyst for the catalytic chemoselective N-boc protection of amines
-
The organic tribromide, [H2-cryptand 222](Br3) 2 was synthesized and characterized by X-ray crystallography, and was utilized as an active catalyst for the N-boc protection of amines. The method is general for the preparation of N-boc derivatives of aliphatic (acyclic and cyclic), aromatic, primary and secondary amines. We also applied our new reaction protocols for the N-boc protection of some new amines and spectral and physical data for the obtained products are reported.
- Chehardoli, Gholamabbas,Zolfigol, Mohammad Ali,Khakyzadeh, Vahid,Golbedaghi, Reza,Hall, Nikita A.,Blackman, Allan G.
-
experimental part
p. 538 - 543
(2012/01/03)
-
- Thioglycoluril as a highly efficient, recyclable and novel organocatalyst for N-Boc protection of amines
-
A simple and efficient protocol for the chemoselective mono-N-Boc protection of various structurally diverse amines with di-tert-butyl dicarbonate using thioglycoluril as the catalyst is described. The catalyst can be readily separated from the reaction products by simple filtration and recovered for reuse. No competitive side reactions, such as formation of isocyanate, urea, oxazolidinone, and N,N-di-Boc derivatives were observed.
- Khaksar, Samad,Vahdat, Seyed Mohammad,Tajbakhsh, Mahmood,Jahani, Fatemeh,Heydari, Akbar
-
experimental part
p. 6388 - 6391
(2011/01/03)
-
- Saccharin sulfonic acid catalyzed N-Boc protection of amines and formation of tertbutyl ethers from alcohols
-
Saccharin sulfonic acid (SaSA), as a stable reagent is easily prepared by the reaction of saccharin with neat chlorosulfonic acid at room temperature. This compound is able to catalyze conversion of amines to their corresponding N-Boc protected amines with (Boc)2O. Alcohols were also converted to their corresponding tert-butyl ethers. All reactions took place under mild conditions giving the desired products in good to high yields.
- Shirini,Zolfigol,AbediniM.
-
experimental part
p. 603 - 607
(2010/10/21)
-
- NOVEL BIAROMATIC COMPOUNDS THAT MODULATE PPAR-RECEPTORS
-
Novel biaromatic compounds that modulate peroxisome proliferator-activator receptors, known as PPAR, having the formula (I): are formulated into pharmaceutical compositions useful in human or veterinary medicine, or alternatively, in cosmetic compositions.
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-
Page/Page column 11-12
(2009/01/23)
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- Efficient, solventless N-Boc protection of amines carried out at room temperature using sulfamic acid as recyclable catalyst
-
A simple, rapid, and efficient protocol for the chemoselective N-Boc protection of amines using sulfamic acid as catalyst is described. N-Boc protection of various structurally diverse aliphatic, aromatic, alicyclic, and heterocyclic amines (1°, 2°, 3°) was carried out with (Boc)2O using sulfamic acid as catalyst (5 mol %) at room temperature under solventless conditions. The advantages of this method are simplicity, shorter reaction times (1-15 min), a cost-effective catalyst, and excellent isolated yields (90-100%); it is also environmentally benign. Moreover, the combined use of ultrasound and sulfamic acid achieves a synergic effect that is especially marked in the N-Boc protection of deactivated (sterically hindered and electron-deficient) amines. The catalyst possesses distinct advantages: ease of handling, cleaner reactions, high activity, and excellent chemoselectivity.
- Upadhyaya, Dharita J.,Barge, Alessandro,Stefania, Rachele,Cravotto, Giancarlo
-
p. 8318 - 8322
(2008/04/13)
-
- NOVEL BIAROMATIC COMPOUNDS THAT ACTIVATE PPAR TYPE RECEPTORS, AND USE THEREOF IN COSMETIC OR PHARMACEUTICAL COMPOSITIONS
-
The invention relates to novel biaromatic compounds that correspond to the general formula (I) and also to the method for preparing them, and to their use in pharmaceutical compositions for use in human or veterinary medicine (in dermatology, and also in the field of cardiovascular diseases, immune diseases and/or lipid metabolism-related diseases), or alternatively in cosmetic compositions.
- -
-
Page/Page column 16; 17
(2010/10/20)
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- NOVEL COMPOUNDS THAT MODULATE PPARγ TYPE RECEPTORS, AND USE THEREOF IN COSMETIC OR PHARMACEUTICAL COMPOSITIONS
-
The invention relates to novel compounds corresponding to the general formula (I) below: and also to the method for preparing them, and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (in dermatology, and also
- -
-
Page/Page column 43
(2010/11/08)
-
- Synthesis of analogs of the phenylamino-pyrimidine type protein kinase C inhibitor CGP 60474 utilizing a Negishi cross-coupling strategy
-
Analogs of 3-{4-[2-(3-chlorophenylamino)-pyrimidin-4-yl]-pyridin-2-yl- amino}-propanol (CGP 60474) were synthesized as useful models for the evaluation of structure-activity relationships of phenylamino-pyrimidine-type protein kinase C inhibitors. The app
- Stanetty, Peter,R?hrling, Jürgen,Schnürch, Michael,Mihovilovic, Marko D.
-
p. 2380 - 2387
(2007/10/03)
-
- NOVEL BIAROMATIC COMPOUNDS WHICH ACTIVATE PPARγ-TYPE RECEPTORS, THEIR PROCESS OF PREPARATION AND THEIR USE IN COSMETIC OR PHARMACEUTICAL COMPOSITIONS
-
The invention relates to novel biaromatic compounds which correspond to the following general formula (I) and to their method of preparation and to their use in pharmaceutical compositions intended for use in human or veterinary medicine, in particular in
- -
-
Page/Page column 25-26
(2008/06/13)
-
- SUBSTITUTED TRIAZOLES AS SODIUM CHANNEL BLOCKERS
-
Substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other the
- -
-
Page/Page column 42-43
(2008/06/13)
-
- Pyrazolopyrimidines as therapeutic agents
-
The present invention is directed to pyrazolopyrimidine derivatives of formula (I) wherein the substituents are defined herein, which are useful as kinase inhibitors and as such are useful for affecting angiogenesis and diseases and conditions associated with angiogenesis.
- -
-
-
- NOVEL COMPOUNDS THAT MODULATE PPARγ TYPE RECEPTORS, AND USE THEREOF IN COSMETIC OR PHARMACEUTICAL COMPOSITIONS
-
The invention relates to novel compounds corresponding to the general formula (I) below: (I) and also to the method for preparing them, and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism),-or alternatively in cosmetic compositions.
- -
-
-
- BIARYL SUBSTITUTED TRIAZOLES AS SODIUM CHANNEL BLOCKERS
-
Biaryl substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof, and a process for making such compounds and salts thereof. Pharmaceutical compositions comprise an effective amount of the instant com
- -
-
-
- PIPERIDINYL COMPOUNDS THAT SELECTIVELY BIND INTEGRINS
-
The invention is directed to piperidinyl compounds of formula (I) and (II) that selectively bind integrin receptors and methods for treating an integrin mediated disorder, wherein W, R2, Z and q are described in the application.
- -
-
-
- Biaromatic ligand activators of PPARgamma receptors
-
Novel pharmaceutical/cosmetic compositions contain at least one biaromatic ligand activator of a PPARγ receptor, such biaromatic ligand having the structural formula (I): and are well suited, inter alia, for regulating and/or restoring skin lipid metabolism, for treating a wide variety of dermatological afflictions, and for preventing and/or treating the signs of aging and/or dry skin.
- -
-
-
- Polymers based on N-carbamyl-N'-dimethysilyl methyl-piperazine traceless linkers for the solid phase synthesis of phenyl based libraries
-
The present invention relates to polymers characterized by novel silicon linkers based on the carbamyl piperazine moiety, methods of preparing these polymers and their use in the solid phase synthesis of compounds or libraries of compounds embracing a phenyl ring in their structure.
- -
-
-
- Sulfonamide inhibitors of aspartyl protease
-
The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical
- -
-
-
- Pyrazolopyrimidines as therapeutic agents
-
The present invention provides compounds of Formula I, including pharmaceutically acceptable salts and/or prodrugs thereof, where G, R2, and R3 are defined as described herein.
- -
-
-
- Compounds having a plurality of nitrogenous substitutents
-
Novel compounds having the formula: STR1wherein the constituent variables are defined herein. The compounds are constructed to include a central aromatic, aliphatic, or heterocyclic ring system. Attached to the central ring system are two linear groups having nitrogenous moieties that are derivatized with chemical functional groups. The ring system can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring, that may also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the these compounds. In accordance with certain embodiments of the invention, libraries of such compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the libraries.
- -
-
-
- Inhibitors of aspartyl protease
-
The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
- -
-
-
- Pyran-4-ylmethyl substituted arylalkylaryl-, arylalkenylylaryl-, and arylalkynylarylurea inhibitors of 5-lipoxygenase
-
Compounds of structure STR1 where W is selected from STR2 where Q is oxygen or sulfur, R5 and R6 are independently selected from hydrogen and alkyl, or R5 and R6, together with the nitrogen atoms to which they a
- -
-
-
- TRANS-1,4-DIALKOXYCYCLOHEXYL SUBSTITUTED ARYLALKYLARYL- ARYLALKENYLARYL-, AND ARYLALKYNYLARYLUREA INHIBITORS OF 5-LIPOXYGENASE
-
Compounds of stracture where W is selected from the group consisting of where Q is oxygen or sulfur, R7 and R8 are independently selected from hydrogen and alkyl, or R7 and R8, together with the nitrogen atoms to which they are attached, define a radical
- -
-
-
- (4-alkoxypyran-4-yl) substituted arylalkylaryl-, aryalkenylaryl-, and aryalkynylarylurea inhibitors of 5-lipoxygenase
-
Compounds of the structure STR1 wherein W is selected from STR2 where Q is oxygen or sulfur, R6 and R7 are hydrogen or alkyl, or R6 and R7, together with the nitrogen atoms to which they are attached, define a r
- -
-
-
- (4-ALKOXYPYRAN-4-YL) SUBSTITUTED ARYLALKYLARYL-, ARYLALKENYLARYL-, AND ARYLALKYNYLARYLUREA INHIBITORS OF 5-LIPOXYGENASE
-
Compounds of the structure wherein W is selected from where Q is oxygen or sulfur, R6 and R7 are hydrogen or alkyl, or R6 and R7, together with the nitrogen atoms to which they are attached, define a radical of formulaR8 is selected from hydrogen, alkyl,
- -
-
-
