cas 81245-24-1, METHYL 2-METHOXY-4-METHYLBENZOATE

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Compounds with neuroprotective effect, and preparation method and application thereof
The invention relates to compounds with a neuroprotective effect, and a preparation method and application thereof. Specifically, the compounds disclosed by the invention have a structure as shown in a formula I, and the definitions of all groups and subs
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Paragraph 0424-0428

(2021/06/13)

Synthesis, in-vitro, in-vivo anti-inflammatory activities and molecular docking studies of acyl and salicylic acid hydrazide derivatives
Over the course of time several drugs have been synthesized and are available in market for the treatment of inflammation. However, they were unable to cure effectively and associated with side effects. To effectively deal with such diseases, heterocycles and their derivatives have gained their special position. For this reason 1,3,4-oxadiazole (15–16), 1,2,4-triazole (17–18), Schiff base (19–24) and 3,5-disubstituted pyrazole (25) derivatives were synthesized starting from salicylic acid and acyl acid hydrazides (12–14) as COX-1 and COX-2 inhibitors. In vivo anti-inflammatory activities were also tested by carrageenan-induced mice paw edema against albino mice of any sex. Structures of all the synthesized compounds were confirmed by FT-IR and 1H NMR analysis. Schiff base derivative of 4-amiontirazole (24) with IC50 value of 1.76 ± 0.05 (COX-2) and 117.8 ± 2.59 emerged as potent COX-2 inhibitor. Furthermore, we also performed in-vivo anti-inflammatory investigations by using carrageenan induced paw edema test. From in-vivo anti-inflammatory activities, it was found that after 1 h the maximum percentage inhibition 15.8% was observed by compound 14 which is comparable with that of the standard drug followed by the compound 18 with percentage inhibition of 10.5%. After 3 h, the maximum percentage inhibition was observed by compound 18 with 22.2% and compound 14 with 16.7%. After 5 h the maximum percentage inhibition was observed by compound 18 with 29.4% followed by compound 16 with 23.5%. We further explore the mechanism of the inhibition by using docking simulations. Docking studies revealed that the selective COX-2 inhibitors established interactions with additional COX-2 enzyme pocket residues.
Ali, Gowhar,Ashraf, Zaman,Hussain, Izhar,Khushal, Adil,Mumtaz, Amara,Munir, Abida,Rashid, Umer,Sadiq, Abdul,Saeed Jan, Muhammad,Saeed, Kiran,Ullah Mughal, Ehsan,Ullah, Rahim
(2020/09/18)

Preparation method and application of 4-hydroxyemodin
The invention belongs to the technical field of medicines, and relates to a preparation method and application of 4-hydroxyemodin, in particular to a preparation method of 4-hydroxyemodin and application of 4-hydroxyemodin, optical isomers, pharmaceutical
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Paragraph 0048; 0050-0051

(2020/04/29)

ACTIVATORS OF THE RETINOIC ACID INDUCIBLE GENE "RIG-1" PATHWAY AND METHODS OF USE THEREOF
The present invention is directed to compounds of Formula (I), which are activators of the RIG-I pathway.
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Paragraph 0237

(2020/03/02)

ACTIVATORS OF THE RETINOIC ACID INDUCIBLE GENE "RIG-I' PATHWAY AND METHODS OF USE THEREOF
The present invention is directed to compounds of Formula (I), which are activators of the RIG-I pathway.
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Page/Page column 93

(2020/03/05)

ACTIVATORS OF THE RETINOIC ACID INDUCIBLE GENE "RIG-I" PATHWAY AND METHODS OF USE THEREOF
The present invention is directed to compounds of Formula (I), which are activators of the RIG-I pathway.
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Paragraph 0565

(2020/03/01)

As neuroprotective agents of pharmaceutical compounds
The invention discloses a medicinal compound as a neuroprotective agent. The medicinal compound is a neuronal nitric oxide synthase-postsynaptic density protein 95 (nNOS-PSD95) decoupling agent. The medicinal compound is a benzene ring derivative shown in the general formula (I) or its pharmaceutically acceptable salt. The invention further discloses a preparation method of the medicinal compound and a use of the medicinal compound in prevention and treatment on neuronal damage influence-caused diseases.
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Paragraph 0665; 0666; 0667; 0668

(2019/06/26)

Synthesis and antibacterial activity of emodin and its derivatives against methicillin-resistant Staphylococcus aureus
Synthesis of the antibacterial emodin was improved using Friedel-Crafts acylation as a key step leading to 37% overall yield. In addition, 21 analogues were synthesized by structural modification of the hydroxyl and methyl groups, as well as the aromatic ring of emodin. Antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) and cytotoxicity against noncancerous Vero cells were evaluated. A structure-activity relationship (SAR) study indicated that the hydroxyl groups and the methyl group in the emodin skeleton were crucial for anti-MRSA activity. Furthermore, the presence of an iodine atom or ethylamino group on the aromatic ring enhanced the anti-MRSA activity with higher selectivity indices, while derivatives containing bromine, chlorine atoms or quaternary ammonium salt were as active as emodin. The quaternary ammonium group on the aromatic ring also led to non-cytotoxicity against Vero cells.
Chalothorn, Thidarat,Rukachaisirikul, Vatcharin,Phongpaichit, Souwalak,Pannara, Sakawrat,Tansakul, Chittreeya
supporting information

(2019/08/08)

Design, synthesis, and preliminary biological evaluation of 3′,4′,5′-trimethoxy flavonoid salicylate derivatives as potential anti-tumor agents
According to the pharmacophore combination principle, a set of new 3′,4′,5′-trimethoxy flavonoid salicylate derivatives were designed, synthesized, and evaluated for biological activity. The cytotoxicity evaluation revealed that compound 10v exhibited higher potency than 5-Fu against HCT-116 cells. Preliminary biological activity studies showed that compound 10v could inhibit the colony formation and migration of HCT-116 cells. Besides, the Hoechst 33258 staining assay and flow cytometry revealed that treatment with compound 10v induced the apoptosis of HCT-116 cells in a concentration-dependent manner, while it had no effect on their cell cycle. The WB analysis suggested that HIF-1α, tubulin, HK-2, and PFK might be the potential pharmacophore targets of compound 10v. Tubulin was a potential drug target for compound 10v, which was explained by analyzing the crystal structure of compound 10v complexed with tubulin. These results indicated that compound 10v might be a promising anti-tumor agent candidate, deserving further optimization and evaluation.
Deng, Xiangping,Liu, Renbo,Li, Junjian,Li, Zhongli,Liu, Juan,Xiong, Runde,Lei, Xiaoyong,Zheng, Xing,Xie, Zhizhong,Tang, Guotao
p. 1874 - 1884
(2019/01/28)

Novel compounds that are inhibitors of YAP/TAZ-TEAD interaction and their use in the treatment of malignant mesothelioma
These compounds are useful as inhibitors of the YAP/TAZ-TEAD interaction.
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Paragraph 0459-0461

(2020/02/01)

PYRIMIDINONE DERIVATIVES AND USES THEREOF TO NEUTRALIZE THE BIOLOGICAL ACTIVITY OF CHEMOKINES
A subject of the present invention is a compound having the general formula (I) a pharmaceutically acceptable salt thereof or a tautomeric form thereof, wherein A, B3, B4, B5, Y, X, B1 and B2 are as defined in any one of claims 1 to 10. Another subject of the invention is the compound as defined above for use as a medicament, in particular for preventing and/or treating inflammation and inflammatory diseases, immune and auto-immune diseases, pain related diseases, genetic diseases and/or cancer.
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Page/Page column 52

(2018/02/28)

Structure-Guided Design of Novel, Potent, and Selective Macrocyclic Plasma Kallikrein Inhibitors
A series of macrocyclic analogues were designed and synthesized based on the cocrystal structure of small molecule plasma kallikrein (pKal) inhibitor, 2, with the pKal protease domain. This led to the discovery of a potent macrocyclic pKal inhibitor 29, w
Li, Zhe,Partridge, James,Silva-Garcia, Abel,Rademacher, Peter,Betz, Andreas,Xu, Qing,Sham, Hing,Hu, Yunjin,Shan, Yuqing,Liu, Bin,Zhang, Ying,Shi, Haijuan,Xu, Qiong,Ma, Xubo,Zhang, Li
supporting information
p. 185 - 190
(2017/03/08)

Copper-mediated etherification of arenes with alkoxysilanes directed by an (2-aminophenyl)pyrazole group
An efficient copper-mediated etherification of inert C-H bonds of (hetero)arenes with reagent-amounts of alkoxysilanes and alkanols has been developed using (2-aminophenyl)pyrazole (2-APP) as a removable directing group. The reaction is scalable, rapidly proceeds under an open atmosphere, and tolerates diverse functional groups to provide alkyl aryl ethers in high yields (up to 87%). As an application, the formal synthesis of anti-emetic drug metoclopramide is accomplished.
Selvakumar, Jayaraman,Grandhi, Gowri Sankar,Sahoo, Harekrishna,Baidya, Mahiuddin
p. 79361 - 79365
(2016/09/09)

A pharmaceutical composition containing 2-hydroxy-7-methyl octahydrophenanthrene derivative as an estrogen receptor ligand or a pharmaceutically acceptable salt thereof as an effective component
Provided are a compound represented by chemical formulas I and II, or a pharmaceutically acceptable ester, amide, or carbamate salt thereof; and a solvent compound comprising a solvent compound of the ester, amide, or carbamate salt thereof. In addition, provided are use of the compound in treating or preventing diseases or disorders related to activation of an estrogen receptor, and a pharmaceutical composition comprising the compound. In chemical formulas I and II, definitions of R_1, R_2, R_3, and R_4 are the same as those in the specification.COPYRIGHT KIPO 2016
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Paragraph 0053; 0112; 0113

(2017/01/02)

TETRAHYDROISOQUINOLINE DERIVED PRMT5-INHIBITORS
A compound of formula I wherein: n is 1 or 2: p is 0 or 1; R1 is optionally one or more halo or methyl groups; 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; 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 (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted C5-12 heteroaryl.
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Page/Page column 116

(2016/03/19)

PHARMACEUTICAL COMPOUNDS
This invention relates to compounds that inhibit or modulate the activity of Chk-1 kinase. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds.
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Page/Page column 92; 138

(2015/09/23)

Design, synthesis, and structure-activity relationship of a novel series of GluN2C-selective potentiators
NMDA receptors are tetrameric complexes composed of GluN1 and GluN2A-D subunits that mediate a slow Ca2+-permeable component of excitatory synaptic transmission. NMDA receptors have been implicated in a wide range of neurological diseases and thus represent an important therapeutic target. We herein describe a novel series of pyrrolidinones that selectively potentiate only NMDA receptors that contain the GluN2C subunit. The most active analogues tested were over 100-fold selective for recombinant GluN2C-containing receptors over GluN2A/B/D-containing NMDA receptors as well as AMPA and kainate receptors. This series represents the first class of allosteric potentiators that are selective for diheteromeric GluN2C-containing NMDA receptors.
Zimmerman, Sommer S.,Khatri, Alpa,Garnier-Amblard, Ethel C.,Mullasseril, Praseeda,Kurtkaya, Natalie L.,Gyoneva, Stefka,Hansen, Kasper B.,Traynelis, Stephen F.,Liotta, Dennis C.
supporting information
p. 2334 - 2356
(2014/04/17)

TRIAZOLONE COMPOUNDS AS mPGES-1 INHIBITORS
The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
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Page/Page column 107

(2014/01/08)

2 - (BENZYLOXY) BENZAMIDES AS LRRK2 KINASE INHIBITORS
The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by LRRK2 kinase activity, for example Parkinson's disease or Alzheimer's disease.
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Page/Page column 39

(2012/03/26)

Comestible compositions comprising high potency savory flavorants, and processes for producing them
The present invention relates to the use of certain high potency savory (“umami”) taste modifiers, as savory flavoring agents and/or enhancers of monosodium glutamate, for the preparation of foods, beverages, and other comestible compositions, and to processes for preparing food flavorant compositions for use in the preparation of comestible food and drink.
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Page/Page column 72

(2012/04/10)

One-pot transition-metal-free synthesis of dibenzo[b,f]oxepins from 2-halobenzaldehydes
A one-pot transition-metal-free, base-mediated synthesis of dibenzo[b,f]oxepins was developed. The reaction of 2-halobenzaldehydes with (2-hydroxyphenyl)acetonitriles proceeds via a sequential aldol condensation and intramolecular ether formation reaction in the presence of Cs2CO 3 and molecular sieves in toluene.
Choi, Young Lok,Lim, Hye Sun,Lim, Hwan Jung,Heo, Jung-Nyoung
supporting information
p. 5102 - 5105,4
(2012/12/12)

Optimization of a small tropomyosin-related kinase B (TrkB) agonist 7,8-dihydroxyflavone active in mouse models of depression
Structure-activity relationship study shows that the catechol group in 7,8-dihdyroxyflavone, a selective small TrkB receptor agonist, is critical for agonistic activity. To improve the poor pharmacokinetic profiles intrinsic to catechol-containing molecules and to elevate the agonistic effect of the lead compound, we initiated the lead optimization campaign by synthesizing various bioisosteric derivatives. Here we show that the optimized 2-methyl-8-(4′- (pyrrolidin-1-yl)phenyl)chromeno[7,8-d]imidazol-6(1H)-one derivative possesses enhanced TrkB stimulatory activity. Chronic oral administration of this compound significantly reduces the immobility in forced swim test and tail suspension test, two classical antidepressant behavioral animal models, which is accompanied by robust TrkB activation in hippocampus of mouse brain. Further, in vitro ADMET studies demonstrate that this compound possesses the improved features compared to the previous lead compound. Hence, this optimized compound may act as a promising lead candidate for in-depth drug development for treating various neurological disorders including depression.
Liu, Xia,Chan, Chi-Bun,Qi, Qi,Ye, Keqiang,Xiao, Ge,Luo, Hongbo R.,He, Xiaolin
p. 8524 - 8537,14
(2020/09/15)

Design, synthesis and biological evaluation of nuclear receptor-degradation inducers
Compounds that regulate the function(s) of nuclear receptors (NRs) are useful for biological studies and as candidate therapeutic agents. Most such compounds are agonists or antagonists. On the other hand, we have developed specific protein degradation in
Itoh, Yukihiro,Kitaguchi, Risa,Ishikawa, Minoru,Naito, Mikihiko,Hashimoto, Yuichi
experimental part
p. 6768 - 6778
(2012/01/13)

NOVEL FIVE-MEMBERED RING COMPOUND
Disclosed is a five-membered ring compound represented by formula (1) or a pharmaceutically acceptable salt thereof. The compound inhibits infiltration of leukocytes including eosinophils and lymphocytes, and is effective as a drug for treating various inflammations. The compound is highly safe and can be administered for a long period. A pharmaceutical product containing the five-membered ring compound or a pharmaceutically acceptable salt thereof is also disclosed. (In the formula, R1 represents a halogen atom or a phenyl group which may be substituted by a C1-C3 alkyl group or a C1-C3 alkoxy group; R2 represents a C1-C3 alkylene group which may be substituted by a C1-C3 alkyl group or a carbonyl group; R3 represents a C1-C3 alkyl group; R4 and R5 independently represent a hydrogen atom or a C1-C3 alkyl group, or -N(R4)R5 may represent a morpholino group which may be substituted by a C1-C3 alkyl group; Y2 represents a C2-C4 alkylene group; and R6 represents a hydrogen atom, a halogen atom, a C1-C3 alkyl group or a C1-C3 alkoxy group.)
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Page/Page column 19

(2011/02/17)

Modulation on C- and N-terminal moieties of a series of potent and selective linear tachykinin NK2 receptor antagonists
Herein we describe the synthesis of a series of new potent tachykinin NK2 receptor antagonists by the modulation of the Cand N-terminal moieties of ibodutant (MEN 15596, 1). The Nterminal benzo[b]thiophene ring was replaced by different substituted naphthalenes and benzofurans, while further modifications were evaluated at the C-terminal tetrahydropyran moiety. Most compounds demonstrated a high affinity for the human NK2 receptor and high in vitro antagonist potency, indicating that a wide range of substituents at both termini can be incorporated in the molecule without detrimental effects on the interactions with the NK2 receptor. Selected compounds were tested in vivo confirming their activity as NK2 antagonists. In particular, after both iv and id administration to guinea pig, compound 61b was able to antagonize NK2-induced colonic contractions with a potency and duration-of-action fully comparable to the reference compound 1 (MEN 15596, ibodutant).
Gensini, Martina,Altamura, Maria,Dimoulas, Tula,Fedi, Valentina,Giannotti, Danilo,Giuliani, Sandro,Guidi, Antonio,Harmat, Nicholas J. S.,Meini, Stefania,Nannicini, Rossano,Pasqui, Franco,Tramontana, Manuela,Triolo, Antonio,Maggi, Carlo Alberto
experimental part
p. 65 - 78
(2010/11/16)

THIENO [2, 3-B] PYRIDINE DERIVATIVES AS VIRAL REPLICATION INHIBITORS
The present invention relates to a series of compounds of formula (A) having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having anti-viral activity.
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Page/Page column 133

(2010/12/17)

COMESTIBLE COMPOSITIONS COMPRISING HIGH POTENCY SAVORY FLAVORANTS, AND PROCESSES FOR PRODUCING THEM
The present invention relates to the use of certain high potency savory (“umami”) taste modifiers, as savory flavoring agents and/or enhancers of monosodium glutamate, for the preparation of foods, beverages, and other comestible compositions, and to processes for preparing food flavorant compositions for use in the preparation of comestible food and drink.
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(2009/12/04)

MACROCYCLIC COMPOUND
The present invention provides a novel class of compounds that have the activity of inhibiting HSP90 enzyme and are useful as anti-cancer agents or such, and compounds that are useful as synthetic intermediates thereof. Specifically, the present invention provides compounds represented by the following formula (1), and pharmaceutically acceptable salts thereof: wherein X, R1, R2, R3, R4, R5, R6, R7, L1, L2, and L3 are as defined in the specification.
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Page/Page column 33-34

(2009/12/05)

NOVEL ADENINE COMPOUND
A novel adenine compound represented by the formula (1): wherein A represents an (un)substituted aromatic carbocycle or (un)substituted aromatic heterocycle; L1 and L2 each independently represents straighted or branched alkylene, et
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Page/Page column 54-55

(2009/12/27)

Improved replicon cellular activity of non-nucleoside allosteric inhibitors of HCV NS5B polymerase: From benzimidazole to indole scaffolds
Benzimidazole-based allosteric inhibitors of the hepatitis C virus (HCV) NS5B polymerase were diversified to a variety of topologically related scaffolds. Replacement of the polar benzimidazole core by lipophilic indoles led to inhibitors with improved potency in the cell-based subgenomic HCV replicon system. Transposing the indole scaffold into a previously described series of benzimidazole-tryptophan amides generated the most potent inhibitors of HCV RNA replication in cell culture reported to date in this series (EC50 ～ 50 nM).
Beaulieu, Pierre L.,Gillard, James,Bykowski, Darren,Brochu, Christian,Dansereau, Nathalie,Duceppe, Jean-Simon,Hache, Bruno,Jakalian, Araz,Lagace, Lisette,LaPlante, Steven,McKercher, Ginette,Moreau, Elaine,Perreault, Stephane,Stammers, Timothy,Thauvette, Louise,Warrington, Jeff,Kukolj, George
p. 4987 - 4993
(2007/10/03)

INHIBITORS OF PAPILLOMA VIRUS
The use of a compound of formula (II): or its enantiomers or diastereoisomers thereof, or salts or pharmaceutically-acceptable esters thereof, in the treatment or prevention of a papilloma virus infection, particularly human papilloma virus in a mammal, wherein R11; X4; X5; X6; R13; R14; W; Z; Y; T; and R18 are defined herein. The present invention also provides novel compounds, pharmaceutical compositions and methods for using these compounds and compositions in the treatment or prevention of papilloma virus infection. More particularly, the present invention provides compounds, compositions and methods for inhibiting papilloma virus DNA replication by interfering with the E1-E2 protein-protein interaction essential for viral DNA replication.
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Page 45-46

(2008/06/13)

VIRAL POLYMERASE INHIBITORS
An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula (I): wherein wherein A, B, R2, R3, L, M1, M2, M3, M4, Y1, Y0, Z and Sp are as defined in claim 1, or a salt thereof, as an inhibitor of HCV NS5B polymerase.
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Page 152 - 153; 157

(2010/02/07)

NOVEL BENSOPHENONE DERIVATIVES OR SALTS THEREOF
A benzophenone derivative represented by the following formula: whereinR1 represents, for example, an optionally substituted heterocyclic group, or a substituted phenyl group; Z represents, for example, an alkylene group; R2 represents, for example, a carboxyl group optionally protected with alkyl;R3 represents, for example, an optionally protected hydroxyl group; R4 represents, for example, an optionally substituted cycloalkyloxy group; and R5 represents, for example, a hydrogen atom, ???or a salt thereof has anti-arthritic activity, inhibits bone destruction caused by arthritis, and provides high safety and excellent pharmacokinetics and thus is useful as therapeutic agent for arthritis. These compounds have inhibitory effect on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression of AP-1 is involved.
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Page 123-124

(2010/02/07)

ANTITHROMBOTIC ETHERS
This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor (I).
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Page 198-199

(2008/06/13)

Superoxide dismutase mimetics: synthesis and structure-activity relationship study of MnTBAP analogues.
Carboxylic ester and amide-substituted analogues of [5,10,15,20-tetrakis(4-carboxyphenyl)-porphyrinato]manganese(III) chloride (MnTBAP) were synthesized and assayed as potential superoxide dismutase (SOD) mimetics. The tetraester analogues 4a and 4b were
Gauuan, Polivina Jolicia F,Trova, Michael P,Gregor-Boros, Livia,Bocckino, Stephen B,Crapo, James D,Day, Brian J
p. 3013 - 3021
(2007/10/03)

The effect of an alkoxy group on the kinetic and thermodynamic acidity of benzene and toluene
2-, 3- and 4-Methoxytoluene can be selectively metalated at an O-adjacent ortho position when butyllithium or tert-butyllithium in the presence of sodium (potassium) tert-butoxide or N,N,N',N'',N''-pentamethyldiethylenetriamine are employed as reagents. In contrast, lithium diisopropylamide or lithium 2,2,6,6-tetramethylpiperidide deprotonate the benzylic α-position of 2- and 3-methoxytoaluene exclusively and of 4-methoxytoluene preferentially. These relative reactivities can be rationalized by an interplay of transition state stabilizing and destabilizing forces (dipole matching and metal coordination vs. lone pair repulsion).
Schlosser, Manfred,Maccaroni, Paola,Marzi, Elena
p. 2763 - 2770
(2007/10/03)

Synthesis of Saturated Anacardic Acids, and Alkenyl and Alkynyl Analogues
The C-alkylation of esters of 2-methoxy-6-methylbenzoic acid and of the 4-methyl isomers affords a route to homologous compounds including in the former case members of the natural anacardic acids from Anacardium occidentale and ω-alkynyl compounds suitable for synthesising other natural phenolic lipids or for structure/activity studies.
Tyman, John H. P.,Visani, Naina
p. 228 - 240
(2007/10/03)

5-SUBSTITUTED IMIDAZO[4,5-C]PYRIDINES
The present invention relates to a class of compounds represented by the formula STR1 or a pharmaceutically acceptable salt thereof useful in the treatment of diseases or disorders mediated by platelet activating factor (PAF).
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(2008/06/13)

Binding of Phenylalkylamine Derivatives at 5-HT1C and 5-HT2 Serotonin Receptors: Evidence for a Lack of Selectivity
Certain phenyalkylamine derivatives have been considered to bind selectively at 5-HT2 serotonin receptors.It is now recognized that the most widely used derivatives, i.e., 1-(2,5-dimethoxy-4-X-phenyl)-2-aminopropanes where X = Me (DOM), Br (DOB), and I (DOI) (1-3, respectively) also bind at the more recently identified population of serotonin 5-HT1C receptors.The purpose of the present investigation was to determine whether simple phenylalkylamines bind selectively at one population of receptors over the other.An examination of 34 derivatives reveals (i) similar structure-affinity relationships and (ii) a significant correlation (r = >0.9, n = 25) between 5-HT1C and 5-HT2 affinity.None of the compounds included in the present study displayed more than a 10-fold selectivity for one population of these receptors over the other; the results suggest that these compounds (including the widely used 5-HT2 agonists DOB and DOI) are 5-HT1C/5-HT2 agents.
Glennon, Richard A.,Raghupathi, Reva,Bartyzel, Piotr,Teitler, Milt,Leonhardt, Sigrun
p. 734 - 740
(2007/10/02)

SYNTHESIS OF SUBSTITUTED BENZENOIDS AND BIPHENYLS VIA DIELS-ALDER CYCLOADDITION OF 6-METHOXY-2-PYRONES
A convenient synthesis of substituted 6-methoxy-2-pyrones from alkyl and aryl esters is described.These pyrones undergo Diels-Alder reactions with acetylenic dienophiles to provide an efficient route to polysubstituted benzoates, phthalates and biphenyls.
Ahmed, Salman A.,Bardshiri, Esfandiar,Simpson, Thomas J.
p. 1595 - 1596
(2007/10/02)

REGIOSELECTIVE METALLATIONS OF (METHOXYMETHOXY)ARENES
The methoxymethoxy substituent when attached to an aromatic ring functions as a moderately strong ortho-directing group in hydrogen-metal exchenge reactions.In many cases the propensity of the methoxymethoxylated arene toward ring metallations is greatly enhanced with concomitant suppression of undesirable side reactions such as nucleophilic attack and addition of metallating species.Unlike many other ortho-directing groups, the regio-direction of the methoxymethoxy substituent when in conjunction with other weaker directing groups is dependent upon the metallating medium.Thus, by changing the electron donating capacity of the metallating medium it is possible to selectively direct metallation to either of the positions ortho to the methoxymethoxy substituent.
Ronald, Robert C.,Winkle, Mark R.
p. 2031 - 2042
(2007/10/02)