cas 161796-10-7, 5-TERT-BUTYL METHYLISOPHTHALATE

Articles about 161796-10-7Total 27 be found

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Photo-induced deep aerobic oxidation of alkyl aromatics
Oxidation is a major chemical process to produce oxygenated chemicals in both nature and the chemical industry. Presently, the industrial manufacture of benzoic acids and benzene polycarboxylic acids (BPCAs) is mainly based on the deep oxidation of polyalkyl benzene, which is somewhat suffering from environmental and economical disadvantage due to the formation of ozone-depleting MeBr and corrosion hazards of production equipment. In this report, photo-induced deep aerobic oxidation of (poly)alkyl benzene to benzene (poly)carboxylic acids was developed. CeCl3 was proved to be an efficient HAT (hydrogen atom transfer) catalyst in the presence of alcohol as both hydrogen and electron shuttle. Dioxygen (O2) was found as a sole terminal oxidant. In most cases, pure products were easily isolated by simple filtration, implying large-scale implementation advantages. The reaction provides an ideal protocol to produce valuable fine chemicals from naturally abundant petroleum feedstocks. [Figure not available: see fulltext.].
Wang, Chang-Cheng,Zhang, Guo-Xiang,Zuo, Zhi-Wei,Zeng, Rong,Zhai, Dan-Dan,Liu, Feng,Shi, Zhang-Jie
p. 1487 - 1492
(2021/07/10)

Exploration of Alternative Scaffolds for P2Y14Receptor Antagonists Containing a Biaryl Core
Various heteroaryl and bicyclo-aliphatic analogues of zwitterionic biaryl P2Y14 receptor (P2Y14R) antagonists were synthesized, and affinity was measured in P2Y14R-expressing Chinese hamster ovary cells by flow cytometry. Given this series' low water solubility, various polyethylene glycol derivatives of the distally binding piperidin-4-yl moiety of moderate affinity were synthesized. Rotation of previously identified 1,2,3-triazole attached to the central m-benzoic acid core (25) provided moderate affinity but not indole and benzimidazole substitution of the aryl-triazole. The corresponding P2Y14R region is predicted by homology modeling as a deep, sterically limited hydrophobic pocket, with the outward pointing piperidine moiety being the most flexible. Bicyclic-substituted piperidine ring derivatives of naphthalene antagonist 1, e.g., quinuclidine 17 (MRS4608, IC50 ≈ 20 nM at hP2Y14R/mP2Y14R), or of triazole 2, preserved affinity. Potent antagonists 1, 7a, 17, and 23 (10 mg/kg) protected in an ovalbumin/Aspergillus mouse asthma model, and PEG conjugate 12 reduced chronic pain. Thus, we expanded P2Y14R antagonist structure-activity relationship, introducing diverse physical-chemical properties.
Jung, Young-Hwan,Yu, Jinha,Wen, Zhiwei,Salmaso, Veronica,Karcz, Tadeusz P.,Phung, Ngan B.,Chen, Zhoumou,Duca, Sierra,Bennett, John M.,Dudas, Steven,Salvemini, Daniela,Gao, Zhan-Guo,Cook, Donald N.,Jacobson, Kenneth A.
p. 9563 - 9589
(2020/09/02)

HETEROCYCLIC P2Y14 RECEPTOR ANTAGONISTS
Disclosed are compounds of formulas (I)-(IX) for treating or preventing a disease or disorder responsive to antagonism of a P2Y14R receptor agonist in a mammal in need thereof, wherein R1-R8, X, Y, Z, X', Y', Z', and A are
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(2019/08/29)

Peptidomimetic plasmepsin inhibitors with potent anti-malarial activity and selectivity against cathepsin D
Following up the open initiative of anti-malarial drug discovery, a GlaxoSmithKline (GSK) phenotypic screening hit was developed to generate hydroxyethylamine based plasmepsin (Plm) inhibitors exhibiting growth inhibition of the malaria parasite Plasmodium falciparum at nanomolar concentrations. Lead optimization studies were performed with the aim of improving Plm inhibition selectivity versus the related human aspartic protease cathepsin D (Cat D). Optimization studies were performed using Plm IV as a readily accessible model protein, the inhibition of which correlates with anti-malarial activity. Guided by sequence alignment of Plms and Cat D, selectivity-inducing structural motifs were modified in the S3 and S4 sub-pocket occupying substituents of the hydroxyethylamine inhibitors. This resulted in potent anti-malarials with an up to 50-fold Plm IV/Cat D selectivity factor. More detailed investigation of the mechanism of action of the selected compounds revealed that they inhibit maturation of the P. falciparum subtilisin-like protease SUB1, and also inhibit parasite egress from erythrocytes. Our results indicate that the anti-malarial activity of the compounds is linked to inhibition of the SUB1 maturase plasmepsin subtype Plm X.
Zogota, Rimants,Kinena, Linda,Withers-Martinez, Chrislaine,Blackman, Michael J.,Bobrovs, Raitis,Pantelejevs, Teodors,Kanepe-Lapsa, Iveta,Ozola, Vita,Jaudzems, Kristaps,Suna, Edgars,Jirgensons, Aigars
supporting information
p. 344 - 352
(2018/12/11)

HYDROXY FORMAMIDE DERIVATIVES AND THEIR USE
Disclosed are compounds having the formula: (I) wherein R1, R2 and R3 are as defined herein, and methods of making and using the same, including use as inhibitors of BMP1, TLL1 and/or TLL2 and in treatment of diseases associated with BMP1, TLL1 and/or TLL2 activity.
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Page/Page column 216

(2017/01/26)

Biphenyl Pyridazinone Derivatives as Inhaled PDE4 Inhibitors: Structural Biology and Structure-Activity Relationships
Cyclic nucleotide cAMP is a ubiquitous secondary messenger involved in a plethora of cellular responses to biological agents involving activation of adenylyl cyclase. Its intracellular levels are tightly controlled by a family of cyclic nucleotide degrading enzymes, the PDEs. In recent years, cyclic nucleotide phosphodiesterase type 4 (PDE4) has aroused scientific attention as a suitable target for anti-inflammatory therapy in respiratory diseases, particularly in the management of asthma and COPD. Here we describe our efforts to discover novel, highly potent inhaled inhibitors of PDE4. Through structure based design, with the inclusion of a variety of functional groups and physicochemical profiles in order to occupy the solvent-filled pocket of the PDE4 enzyme, we modified the structure of our oral PDE4 inhibitors to reach compounds down to picomolar enzymatic potencies while at the same time tackling successfully an uncovered selectivity issue with the adenosine receptors. In vitro potencies were demonstrated in a rat lung neutrophilia model by administration of a suspension with a Penn-Century MicroSprayer Aerosolizer.
Gràcia, Jordi,Buil, Maria Antonia,Castro, Jordi,Eichhorn, Peter,Ferrer, Manel,Gavaldà, Amadeu,Hernández, Bego?a,Segarra, Victor,Lehner, Martin D.,Moreno, Imma,Pagès, Lluís,Roberts, Richard S.,Serrat, Jordi,Sevilla, Sara,Taltavull, Joan,Andrés, Miriam,Cabedo, Judit,Vilella, Dolors,Calama, Elena,Carcasona, Carla,Miralpeix, Montserrat
p. 10479 - 10497
(2016/12/16)

COMPOUNDS AND METHODS for the inhibition of HDAC
Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, R3, R4, Y, A, Z, L and n are as defined herein, and methods of making and using the same.
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Paragraph 0343-0344

(2015/11/24)

ANILINE DERIVATIVES,THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
The present invention relates to aniline derivatives, to their preparation and to their therapeutic application.
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(2013/03/28)

3-(5-Amino-6-oxo-1,6-dihydropyridazin-3-yl)-biphenyl derivatives as PDE4 inhibitors
New pyridazin-3(2H)-one derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of the phosphodiesterase IV (PDE4).
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Page/Page column 34

(2012/01/03)

ASPARTYL PROTEASE INHIBITORS
A compound of formula (I): N-oxides, addition salts, quaternary amines metal complexes stereochemically isomeric forms and metabolites thereof, wherein A is CR1 or N; D is H, C1-C6alkyl, C2-C6alkenyl,
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Page/Page column 66

(2010/04/28)

(3-oxo)pyridazin-4-ylurea derivatives as PDE4 inhibitors
New (3-oxo)pyridazin-4-ylurea derivatives having the chemcial structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of the phosphodiesterase IV (PDE4).
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Page/Page column 45; 46

(2010/07/03)

Molecular modeling, synthesis, and activity studies of novel biaryl and fused-ring BACE1 inhibitors
A series of transition state analogues of beta-secretases 1 and 2 (BACE1, 2) inhibitors containing fused-ring or biaryl moieties were designed computationally to probe the S2 pocket, synthesized, and tested for BACE1 and BACE2 inhibitory activity. It has
Chirapu, Srinivas Reddy,Pachaiyappan, Boobalan,Nural, Hikmet F.,Cheng, Xin,Yuan, Hongbin,Lankin, David C.,Abdul-Hay, Samer O.,Thatcher, Gregory R.J.,Shen, Yong,Kozikowski, Alan P.,Petukhov, Pavel A.
scheme or table
p. 264 - 274
(2009/05/26)

P2X3 RECEPTOR ANTAGONISTS FOR TREATMENT OF PAIN
The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor s
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Page/Page column 61-62

(2009/06/27)

AMIDE COMPOUNDS, COMPOSITIONS AND USES THEREOF
Compounds are provided according to formula (1 ) : where A, B, W, X', L, R1, R3, R4b, and m' are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.
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Page/Page column 81

(2009/10/22)

PIPERIDINE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
The present application describes modulators of MIP-1 of formula (I) : or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as set forth above. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators are disclosed.
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Page/Page column 87-88

(2009/03/07)

Synthesis and SAR of hydroxyethylamine based phenylcarboxyamides as inhibitors of BACE
A series of N-((2S,3R)-1-(3,5-difluorophenyl)-3-hydroxy-4-(3-methoxybenzylamino)-butan-2-yl)benzamides has been synthesized as BACE inhibitors. A variety of P2 and P3 substituents has been explored, and these efforts have culminated in the identification
Wu, Yong-Jin,Zhang, Yunhui,Good, Andrew C.,Burton, Catherine R.,Toyn, Jeremy H.,Albright, Charles F.,Macor, John E.,Thompson, Lorin A.
scheme or table
p. 2654 - 2660
(2010/01/16)

Alpha-helical mimetics
Benzoyl urea derivatives that are alpha helical peptides mimetics that mimic BH3-only proteins, compositions containing them, their conjugation to cell-targeting-moieties, and their use in the regulation of cell death are disclosed. The benzoyl urea derivatives are capable of binding to and neutralizing pro-survival Bcl-2 proteins. Use of benzoyl urea derivatives in the treatment and/or prophylaxis of diseases or conditions associated with deregulation of cell death are also described.
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Page/Page column 87

(2011/05/18)

AMIDE DERIVATIVES AS INHIBITORS OF ASPARTYL PROTEASES
The invention provides compounds of the formula (I). N-oxides, addition salts, quaternary amines, metal complexes, stereochemically isomeric forms and metabolites thereof, wherein W is H,C 1-C 6 alkyl, C 3-C 6 cycloalkyl, aryl or heterocyclyl; Q is aryl or heterocyclyl; A is a five or six membered saturated, partially unsaturated or aromatic ring; D is (II) or (III) the other variables are as defined in the specification. The compounds of the invention are inhibitors of BACE and are among other things useful for the treatment and/or prevention of conditions associated with BACE activity such as Alzheimer's disease.
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Page/Page column 92

(2008/12/04)

Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors
This Letter describes the design and synthesis of tertiary carbinamine macrocyclic inhibitors of the β-secretase (BACE-1) enzyme. These macrocyclic inhibitors, some of which incorporate novel P2 substituents, display a 2- to 100-fold increase in potency r
Lindsley, Stacey R.,Moore, Keith P.,Rajapakse, Hemaka A.,Selnick, Harold G.,Young, Mary Beth,Zhu, Hong,Munshi, Sanjeev,Kuo, Lawrence,McGaughey, Georgia B.,Colussi, Dennis,Crouthamel, Ming-Chih,Lai, Ming-Tain,Pietrak, Beth,Price, Eric A.,Sankaranarayanan, Sethu,Simon, Adam J.,Seabrook, Guy R.,Hazuda, Daria J.,Pudvah, Nicole T.,Hochman, Jerome H.,Graham, Samuel L.,Vacca, Joseph P.,Nantermet, Philippe G.
p. 4057 - 4061
(2008/02/10)

Novel phenylcarboxyamides as beta-secretase inhibitors
There is provided a series of novel phenylcarboxyamides of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and Y as defined herein, their pharmaceutical compositions and
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Page/Page column 8-9

(2008/06/13)

QUINAZOLINONE DERIVATIVES AND THEIR USE AS B-RAF INHIBITORS
The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.
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Page/Page column 66; 68

(2008/06/13)

QUINOXALINES AS B RAF INHIBITORS
The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.
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Page/Page column 73-74

(2010/11/08)

ALPHA-HELICAL MIMETICS
Benzoyl urea derivatives that are alpha helical peptide mimetics that mimic BH3-only proteins, compositions containing them, their conjugation to cell-targeting moieties, and their use in the regulation of cell death are disclosed. The benzoyl urea derivatives are capable of binding to and neutralising pro-survival Bcl-2 proteins. Use of the benzoyl urea derivatives in the treatment and/or prophylaxis of diseases or conditions associated with deregulation of cell death are also disclosed.
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Page/Page column 176

(2010/02/15)

NOVEL ISOPHTHALATES AS BETA-SECRETASE INHIBITORS
There is provided a series of substituted isophthalates of formula (I) or a stereoisomer thereof; or a pharmaceutically acceptable salt thereof, wherein W, R3, R5 and R6 as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
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Page/Page column 41

(2010/11/23)

Substituted 1,2-ethylenediamines, Methods for Preparing Them and Uses Thereof
The present invention relates to substituted 1,2-ethylenediamines of general formula (I) wherein the groups R1 to R15, A, B, L, i as well as X1-X4 are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.
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Page/Page column 193

(2010/11/24)

1,3,5-SUBSTITUTED PHENYL DERIVATIVE COMPOUNDS USEFUL AS BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
The present invention is directed to 1,3,5-phenyl substituted derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
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Page/Page column 83

(2010/02/14)

Rigid macrocyclic triamides as anion receptors: Anion-dependent binding stoichiometries and 1H chemical shift changes
The cyclic triamide of 3′-amino-3-biphenylcarboxlic acid is readily synthesized in a stepwise manner and represents a novel class of anion receptors with a large central cavity. This macrocycle binds more strongly to tetrahedral anions than spherical or p
Choi, Kihang,Hamilton, Andrew D.
p. 10241 - 10249
(2007/10/03)