cas 17694-68-7, 3-(2-Bromoacetyl)pyridine hydrobromide

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Synthesis, structures, and biological activities of new 1H-1,2,4-triazole derivatives containing pyridine unit
Fourteen new 1H-1,2,4-triazole derivatives containing pyridine moiety were synthesized by condensation of 1-(pyridine-3-yl)-2-(1H-1,2,4-triazol1-yl) ethanone with aryl aldehydes, and their reaction conditions were studied. The title compounds were screened for their antibacterial and plant growth regulatory activities. The screening data revealed that most of the compounds showed some antifungal and plant growth regulatory activities.
Liu, Jian-Bing,Tao, Wei-Feng,Dai, Hong,Jin, Zhong,Fang, Jian-Xin
p. 376 - 380
(2007)
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HETEROCYCLIC COMPOUNDS FOR MODULATING NR2F6
The present disclosure relates to compounds capable of modulating the activity of NR2F6. The compounds of the disclosure may be used in methods for the prevention and/or the treatment of diseases and disorders associated with modulating NR2F6 activity.
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Paragraph 00468-00469

(2021/09/04)

Thiazole analogues of the marine alkaloid nortopsentin as inhibitors of bacterial biofilm formation
Anti-virulence strategy is currently considered a promising approach to overcome the global threat of the antibiotic resistance. Among different bacterial virulence factors, the biofilm formation is recognized as one of the most relevant. Considering the high and growing percentage of multi-drug resistant infections that are biofilm-mediated, new therapeutic agents capable of counteracting the formation of biofilms are urgently required. In this scenario, a new series of 18 thiazole derivatives was efficiently synthesized and evaluated for its ability to inhibit biofilm formation against the Gram-positive bacterial reference strains Staphylococcus aureus ATCC 25923 and S. aureus ATCC 6538 and the Gram-negative strain Pseudomonas aeruginosa ATCC 15442. Most of the new compounds showed a marked selectivity against the Gram-positive strains. Remarkably, five compounds exhibited BIC50 values against S. aureus ATCC 25923 ranging from 1.0 to 9.1 μM. The new compounds, affecting the biofilm formation without any interference on microbial growth, can be considered promising lead compounds for the development of a new class of anti-virulence agents.
Carbone, Anna,Cascioferro, Stella,Parrino, Barbara,Carbone, Daniela,Pecoraro, Camilla,Schillaci, Domenico,Cusimano, Maria Grazia,Cirrincione, Girolamo,Diana, Patrizia
(2021/02/02)

4-PHENYL-N-(PHENYL)THIAZOL-2-AMINE DERIVATIVES AND RELATED COMPOUNDS AS ARYL HYDROCARBON RECEPTOR (AHR) AGONISTS FOR THE TREATMENT OF E.G. ANGIOGENESIS IMPLICATED OR INFLAMMATORY DISORDERS
4-phenyl-N-(phenyl)thiazol-2-amine and 4-(pyridin-3-yl)-N-( phenyl) thiazol-2-amine derivatives and the corresponding thiadiazole, thiophene, oxazole, oxadiazole, imidazole and triazole derivatives and related compounds as aryl hydrocarbon receptor (AHR) agonists for the treatment of angiogenesis implicated disorders, such as e.g. retinopathy, psoriasis, rheumatoid arthritis, obesity and cancer, or inflammatory disorders.
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Paragraph 00221; 00360

(2021/06/26)

Synthesis, antioxidant and antimicrobial properties of novel pyridyl-carbonyl thiazoles as dendrodoine analogs
Marine compound dendrodoine was first obtained from tunicate species (Dendrodo grossularia). It has a five-membered ring, namely, it is a heterocycle thiadiazole, which is found rarely in natural sources. Following its biological activities, novel analogs have been investigated recently. Synthesis of the analogs for this study is realized with uncommon thiazole closure, including methylene-carbonyl condensation. Structures are elucidated by NMR (1H, 13C) and HRMS spectrums. As an alkaloid derivative, antioxidant properties were evaluated with DPPH and FRAP assays and antimicrobial effect with microdilution method. Among the series, 3bc-3cf showed higher antioxidant activity than those having 3 or 4-pyridyl substituents. There is lesser activity for 2-pyridyl activity for 2-pyridyl containing group, which may be a result of intramolecular interactions. No activity was observed against gram-negative bacteria at 250 μg/mL. 3ae and 3ce showed activity at 64 μg/mL against S. aureus and 3ae showed activity at 16 μg/mL against S. epidermidis gram-positive bacteria. Chloramphenicol showed activity against all microorganisms at 8-16 μg/mL. Sixteen original dendrodoine analogs have been defined by close/higher activity compared to dendrodoine analogs and Trolox.
?ahin, Zafer,Biltekin, Sevde Nur,Yurtta?, Leyla,Demirayak, ?eref
p. 1733 - 1741
(2021/01/04)

SUBSTITUTED PYRAZOLO[4,3-b]PYRIDINES AND THEIR USE AS GLUN2B RECEPTOR MODULATORS
Substituted pyrazolo[4,3-b]pyridines as GluN2B receptor ligands. Such compounds may be used in GluN2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by GluN2B receptor activity.
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Paragraph 0275; 0276

(2020/12/25)

Synthesis of enantiopure 1,2-azido and 1,2-amino alcohols via regio- and stereoselective ring-opening of enantiopure epoxides by sodium azide in hot water
A practical and convenient method for the efficient and regio- and stereoselective ring-opening of enantiopure monosubstituted epoxides by sodium azide under hydrolytic conditions is reported. The ring-opening of enantiopure styryl and pyridyl (S)-epoxides by N3- in hot water takes place preferentially at the internal position with complete inversion of configuration to produce (R)-2-azido ethanols with up to 99% enantio- and regioselectivity, while the (S)-adamantyl oxirane provides mainly the (S)-1-adamantyl-2-azido ethanol in excellent yield. In general, 1,2-amino ethanols were obtained in high yield and excellent enantiopurity by the reduction of the chiral 1,2-azido ethanols with PPh3 in water/THF, and then converted into the Boc or acetamide derivatives.
Wang, Hai-Yang,Huang, Kun,De Jesús, Melvin,Espinosa, Sandraliz,Pi?ero-Santiago, Luis E.,Barnes, Charles L.,Ortiz-Marciales, Margarita
p. 91 - 100
(2016/02/09)

BACE INHIBITORS
The present invention provides compounds of Formula I useful as BACE inhibitors in the treatment of e.g. Alzheimer's disease : wherein A is selected from the group consisting of; of; R1 is H or F; R2 is H, -OCH3, C1-C3 alkyl,; R3 is H, -CH3, or -OCH3; and R4 is H or F; or a pharmaceutically acceptable salt thereof.
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Page/Page column 22

(2014/05/24)

BENZIMIDAZOLE DERIVATIVES AS SELECTIVE PROTEINE KINASE INHIBITORS
The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof. Wherein n, R1, R2, R3, R4, R5, A, Q and X are as defined in the description. These compounds selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant proteine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective native and/or mutant c-kit inhibitors.
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Page/Page column 44

(2015/01/07)

4-Pyridylanilinothiazoles that selectively target von Hippel - Lindau deficient renal cell carcinoma cells by inducing autophagic cell death
Renal cell carcinomas (RCC) are refractory to standard therapy with advanced RCC having a poor prognosis; consequently treatment of advanced RCC represents an unmet clinical need. The von Hippel-Lindau (VHL) tumor suppressor gene is mutated or inactivated in a majority of RCCs. We recently identified a 4-pyridyl-2-anilinothiazole (PAT) with selective cytotoxicity against VHL-deficient renal cells mediated by induction of autophagy and increased acidification of autolysosomes. We report exploration of structure-activity relationships (SAR) around this PAT lead. Analogues with substituents on each of the three rings, and various linkers between rings, were synthesized and tested in vitro using paired RCC4 cell lines. A contour map describing the relative spatial contributions of different chemical features to potency illustrates a region, adjacent to the pyridyl ring, with potential for further development. Examples probing this domain validated this approach and may provide the opportunity to develop this novel chemotype as a targeted approach to the treatment of RCC. 2009 American Chemical Society.
Hay, Michael P.,Turcotte, Sandra,Flanagan, Jack U.,Bonnet, Muriel,Chan, Denise A.,Sutphin, Patrick D.,Nguyen, Phuong,Giaccia, Amato J.,Denny, William A.
supporting information; experimental part
p. 787 - 797
(2010/07/05)

CYCLOALKYLIDENE AND HETEROCYCLOALKYLIDENE INHIBITOR COMPOUNDS
The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.
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Page/Page column 83-84

(2010/02/17)

Muscarinic receptor 1 agonist activity of novel N-aryl carboxamide substituted 3-morpholino arecoline derivatives in Alzheimer's presenile dementia models
Earlier we have reported the effect of arecoline thiazolidinone and morpholino arecoline derivatives as muscarinic receptor 1 agonists in Alzheimer's presenile dementia models. To elucidate further our Structure-Activity Relationship (SAR) studies on the chemistry and muscarinic receptor 1 binding efficacy, a series of novel carboxamide derivatives of 2-(1-methyl-1,2,5,6-tetrahydropyridin-3-yl)morpholine molecule have been designed and synthesized as a new class of M1 receptor agonists with a low toxicity effect profile that enhances memory function in animal models of Alzheimer's presenile dementia and also modulates the APP secretion from rat brain cerebrocortical slices by activating M1 receptor in vitro. Results suggest that compound 9b having methyl group at the para position of the aryl group attached to the carboxamide of morpholino arecoline could emerge as a potent molecule having antidementia activity.
Malviya, Manish,Sunil Kumar,Mythri,Venkateshappa,Subhash,Rangappa
experimental part
p. 5526 - 5534
(2009/12/06)

HETEROARYL COMPOUNDS, COMPOSITIONS, AND METHODS OF USE IN CANCER TREATMENT
Provided herein are novel heteroaryl compounds, compositions comprising the compounds, and methods of treatment or prevention comprising administration of the compounds. The compounds are effective in the targeting of cells defective in the von Hippel-Lindau gene and in inducing autophagic cell death. The methods are directed to treating or preventing diseases such as cancer, and in particular cancers resulting from von Hippel-Lindau disease. The compounds of the invention may be administered in combination with another therapeutic agent.
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Page/Page column 110

(2009/10/22)

Substituted Aminothiazole Prodrugs of Compounds with Anti-HCV Activity
The invention provides amino-substituted aminothiazole compounds of Formula I and Formula II where A is a group of the formula: and the variables X, Y, R, and R1 to R7 are described herein. These compounds are prodrugs of compounds useful as inhibitors of viral replication. Compositions containing such compounds, and methods of treating viral infections with these compounds, as well as to processes and intermediates useful for preparing such compounds are also provided by the invention.
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(2009/12/24)

HETEROARYL SUBSTITUTED THIAZOLES
The invention provides heteroaryl substituted thiazolo compounds of Formula I and II and pharmaceutically acceptable salts thereof. The variables A and R3 to R7 are defined herein. The invention also includes methods for preparing compounds and salts of Formula I and II. The present invention also includes pharmaceutical compositions containing heteroaryl substituted thiazolo compounds and methods for using heteroaryl substituted thiazolo compounds, including methods for using the compounds in the treatment of hepatitis C virus.
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Page/Page column 44; 48

(2009/01/20)

Novel synthetic approach to N-aryl-4-(3-pyridyl)thiazol-2-amine and analogues using HMCM-41 as catalyst, and their biological evaluation as human platelet aggregation inhibitors
A novel synthetic approach to N-aryl-4-(3-pyridyl)thiazol-2-amine and analogues using HMCM-41, a mesoporous aluminosilicate catalyst and their in vitro ADP-induced platelet aggregation inhibitory activity on human blood platelets is described. Among the test compounds N-(2′-flourophenyl)-4-(3-pyridyl)thiazol-2-amine (9e) was found to be the most potent, IC50 = 4.84 × 10-7 M.
Bhoga, Umadevi
p. 1144 - 1150
(2008/03/12)

HETEROCYCLIC COMPOUNDS
The invention is related to novel substituted diazaheterocycles useful as effective antihypercholesterolemic agents, methods of their preparation, and pharmaceutical compositions containing them.
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Page/Page column 14

(2008/06/13)

Chain mechanism in the photocleavage of phenacyl and pyridacyl esters in the presence of hydrogen donors
Excited phenacyl and 3-pyridacyl esters of benzoic acid react with an excess of aliphatic alcohols in a chain reaction process involving hydrogen transfer from the ketyl radical intermediates, leading to benzoic acid in addition to acetophenone and 3-acetylpyridine, respectively, as the byproducts. While the maximum quantum yields reached 4 in both cases, the 2- or 4-pyridacyl ester photoreduction proceeded with the efficiency below 100% under the same conditions. The investigation indicates that a radical coupling between ketyl radicals, both formed from the excited ester by hydrogen abstraction from an alcohol, is accompanied by the elimination of benzoic acid from the ester ketyl radical itself. A partitioning between two reactions was found to be remarkably sensitive to the chromophore nature, such as a position of the nitrogen atom in the pyridacyl moiety, The magnitude of a radical chain process is dependent on the efficiency of consecutive steps that produce free radicals capable of a subsequent ester reduction. The driving force of a possible electron transfer from the ketyl radicals to the ester has been excluded on the basis of cyclic voltametry measurements. The observed quantum yields of photoreduction were found to be diminished by formation of relatively long-lived light absorbing transients, coproducts obtained apparently by secondary photochemical reactions. Additionally, it is shown that basic additives such as pyridine can further increase the efficiency of the photoreduction by a factor of 4. A radical nature of the reduction mechanism was supported by finding a large kinetic chain length of an analogous reaction initiated by free radicals generated thermally yet again when phenacyl or 3-pyridacyl benzoate was used. Both phenacyl and pyridacyl chromophores are pronounced to be valuable as the photoremovable protecting groups when high quantum and chemical yields of carboxylic acid elimination are important, but higher concentrations of the hydrogen atom donors are not destructive for a reaction system or are experimentally impractical.
Literak, Jaromir,Dostalova, Anna,Klan, Petr
p. 713 - 723
(2007/10/03)

THIAZOLE COMPOUNDS AND METHODS OF USE
The present invention provides compounds, salts and hydrates of Formula I, wherein the variables Ar1R2, R3, R4, r, q, and t are defined herein. Certain compounds of Formula I described herein possess potent antiviral activity. The invention also provides compounds of Formula I that are potent and/ or selective inhibitors of Hepatitis C virus replication. Certain compounds described herein inhibit assembly of the HCV replication complex. The invention also provides pharmaceutical compositions containing one or more compounds of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease. These infectious diseases include viral infections, particularly HCV infections. The invention is particularly includes methods of treating human patients suffering from an infectious disease, but also encompasses methods of treating other animals, including livestock and domesticated companion animals, suffering from an infectious disease. Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with on or more other therapeutic agent.
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Page/Page column 40

(2010/11/24)

USE OF C-KIT INHIBITORS FOR TREATING TYPE II DIABETES
The present invention relates to a method for treating type II diabetes, comprising administering a compound capable of depleting mast cells to a human in need of such treatment. Such compounds can be chosen from non-toxic, selective and potent c-kit inhibitors.
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Page/Page column 82

(2008/06/13)

2-AMINOARYLOXAZOLE COMPOUNDS FOR THE TREATMENT OF DISEASES
The present invention relates to novel compounds selected from 2-aminoaryloxazoles that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective c-kit, bcr-abl, FGFR3 and/or Flt-3 inhibitors.
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Page/Page column 36

(2008/06/13)

2-(3-AMINOARYL) AMINO-4-ARYL-THIAZOLES AND THEIR USE AS C-KIT INHIBITORS
The present invention relates to the use of masitinib or a pharmaceutically acceptable salt thereof, and in particular of masitinib mesylate, for the preparation of a medicament for the treatment of GIST, to the use of this therapy for the treatment of GIST, and a method of treating mammals, including humans, suffering from GIST by administering to said mammal in need of such treatment an effective dose of masitinib, and in particular masitinib mesylate
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Page 78-79

(2010/11/30)

NOVEL DERIVATIVES OF PYRIDYLETHANOL (PHENYLETHYL) AMINES AS INHIBITORS OF CHOLESTEROL BIOSYNTHESIS, PROCESSES FOR THEIR PREPARATION, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
The novel derivatives of pyridylethanol (phenylethyl) amines of formula I are described wherein n is an integer from 1 to 4, R1 is a hydrogen atom, hydroxyl group or lower C1-6 alkoxy group R2 is a hydrogen atom or a straight or branched lower C1-6 alkyl group X, is hydrogen, fluorine, chlorine, bromine, hydroxyl group, trifluoromethyl group, 3,4-di-CI,2,4-di-CI or lower C1-6 alkoxy group, the enantiomers, diastereoisomers or racemates thereof or the physiologically acceptable acid addition salts thereof which are ligands of sigma receptors for inhibiting cholesterol biosynthesis and are thus appropriate for the treatment of hypercholesterolemia and hyperlipemia in humans. The greatest lowering of cholesterol was observed by 1-(d-pyridyl)-2-(N-(2-(3,4-dicholorophenyl)ethyl-N-propylamino)ethanol in the form of dihydrobromide salt (signature BK-35. 2HBr).
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Page 15

(2008/06/13)

HETEROARYL-ETHANOLAMINE DERIVATIVES AS ANTIVIRAL AGENTS
The present invention provides a compound of formula (I), which are useful as antiviral agents, in particular, as agents against viruses of the herpes family.
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Page 38

(2010/02/06)

SUBSTITUTED THIAZOLE DERIVATIVES BEARING 3-PYRIDYL GROUPS, PROCESS FOR PREPARING THE SAME AND USE THEREOF
The present invention provides a pharmaceutical composition having a steroid C17,20-lyase inhibitory activity, which is useful as a prophylactic or therapeutic agent of prostatism, tumor such as breast cancer and the like, more particularly, a steroid C17,20-lyase inhibitor containing a compound represented by the formula: wherein A1 is an aromatic hydrocarbon group optionally having substituents or a heterocyclic group optionally having substituents, one of A2 and A3 is a hydrogen atom, a halogen atom, a C1-4 aliphatic hydrocarbon group optionally having substituents or an optionally esterified carboxyl group, the other of A2 and A3 is an aromatic hydrocarbon group optionally having substituents or a heterocyclic group optionally having substituents, and at least one of A1, A2 and A3 is a 3-pyridyl group optionally having substituents, or a salt thereof or a prodrug thereof.
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Page/Page column 37

(2008/06/13)

Identification of novel inhibitors of the transforming growth factor β1 (TGF-β1) type 1 receptor (ALK5)
Screening of our internal compound collection for inhibitors of the transforming growth factor β1 (TGF-β1) type I receptor (ALK5) identified several hits. Optimization of the dihydropyrroloimidazole hit 2 by introduction of a 2-pyridine and 3,4-methylenedioxyphenyl group gave 7, a selective ALK5 inhibitor. With this information, optimization of the triarylimidazole hit 8 gave the selective inhibitor 14, which inhibits TGF-β1-induced fibronectin mRNA formation while displaying no measurable cytotoxicity in the 48 h XTT assay.
Callahan, James F.,Burgess, Joelle L.,Fornwald, James A.,Gaster, Laramie M.,Harling, John D.,Harrington, Frank P.,Heer, Jag,Kwon, Chet,Lehr, Ruth,Mathur,Olson, Barbara A.,Weinstock, Joseph,Laping, Nicholas J.
p. 999 - 1001
(2007/10/03)

Imidazopyridazines. VI. Syntheses and Central Nervous System Activities of Some 6-(Alkoxy- and methylthio-phenoxy and methoxybenzylthio)-3-methoxy-2-phenyl(substituted phenyl and pyridinyl)imidazopyridazines
Series of 6-(alkoxy- and methylthio-phenoxy)-2-phenyl(substituted phenyl and pyridinyl)imidazopyridazines and 3-methoxy-6-(methoxybenzylthio)-2-phenyl(substituted phenyl and pyridinyl)imidazopyridazines have been prepared and subsesquently tested for their ability to inhibit GABA-stimulated 3H-diazepam binding to rat brain plasma membranes.The 6-(alkoxy- and methylthio-phenoxy) and 6-(methoxybenzylthio) compounds were much more effective in the displacement studies than the parent 6-phenoxy or 6-benzylthio compounds respectively.3-Methoxy-6-(2'-methoxyphenoxy)-2-phenylimidazopyridazine (GBLD-167, IC50 70 nM) was 16 times more effective than its 3-methoxy-6-phenoxy analogue (GBLD-214, IC50 1120 nM) and the 3-methoxy-6-(2'-methoxybenzylthio)-2-phenyl compound (GBLD-163, IC50 9 nM) was two and a half times more active than its 6-benzylthio-3-methoxy analogue (GBLD-137, IC50 22nM).The most active member of the 6-phenoxy series was the 2-(4'-fluorophenyl)-3-methoxy-6-(2''-methoxyphenoxy) compound (GBLD-255, IC50 30nM) and, within the 6-benzylthio series, the 2-(4'-fluorophenyl, 3'-aminophenyl, and pyridin-3'-yl)-3-methoxy-6-(3''-methoxybenzylthio) compounds (GBLD-233, 301 and 296) all gave IC50 5nM.A Hansch-type analysis of the results for these two closely related series of compounds indicates that electron-donating substituents in 2-(para substituted phenyl) derivatives favour binding, but bulky substituents hinder this effect.
Barlin, Gordon B.,Davies, Les P.,Ireland, Stephen J.,Ngu, Maria M.L.
p. 1735 - 1748
(2007/10/02)