cas 55676-22-7, 2-Chloro-5-acetylpyridine | Articles data

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Photoinduced Acetylation of Anilines under Aqueous and Catalyst-Free Conditions
A green and efficient visible-light induced functionalization of anilines under mild conditions has been reported. Utilizing nontoxic, cost-effective, and water-soluble diacetyl as photosensitizer and acetylating reagent, and water as the solvent, a variety of anilines were converted into the corresponding aryl ketones, iodides, and bromides. With advantages of environmentally friendly conditions, simple operation, broad substrate scope, and functional group tolerance, this reaction represents a valuable method in organic synthesis.
Yang, Yu-Ming,Yan, Wei,Hu, Han-Wei,Luo, Yimin,Tang, Zhen-Yu,Luo, Zhuangzhu
p. 12344 - 12353
(2021/09/02)

Method for removing acyl group in diazo of aryl diazonium salt
The invention provides a method for removing an acyl group in diazo of an aryl diazonium salt. The method is characterized in that the aryl diazonium salt and its derivative and an ortho-dicarbonyl compound undergo an illumination reaction to obtain a corresponding arylacyl product. The method has the advantages of high yield of the product, no metal involvement, and simple process.
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Paragraph 0052; 0080-0084; 0088

(2019/02/13)

INHIBITORS OF MUTANT ISOCITRATE DEHYDROGENASES AND COMPOSITIONS AND METHODS THEREOF
The invention provides novel chemical compounds useful for treating cancer, or a related disease or disorder thereof, and pharmaceutical composition and methods of preparation and use thereof.
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Paragraph 00157

(2018/07/29)

pyrrole logical sequence handkerchief nai intermediate preparation method (by machine translation)
The invention relates to a simple operation, raw materials are easy, and the production cost is low, the quality of the product is good and is suitable for the industrial production of the intermediate pyrrole logical sequence handkerchief nai 5 - (pyridine - 2 - yl) - 2 (1H) - pyridone of the preparation method. (by machine translation)
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(2017/07/06)

High-activity iminophenylacetate compound, preparation method and applications thereof
The present invention belongs to the field of pesticides, and particularly relates to a high-activity iminophenylacetate compound, a preparation method and applications thereof. According to the present invention, the research of novel methoxy acrylate compounds is performed, a pyridine aryl ether structure is introduced into the structure of the novel methoxy acrylate compound, the research of the new compound structures is expanded, and the high-activity iminophenylacetate compound is found; and the compound has the bioactivity equal to azoxystrobin and trifloxystrobin, provides good effects on most pathogenic bacteria, especially provides significant prevention and treatment effects on Sclerotinia sclerotiorum bacterial, and is effective at a low doses.
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Paragraph 0053

(2017/08/30)

New Positive allosteric modulators of nicotinic acetylcholine receptor
The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor.
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Paragraph 0187

(2013/03/26)

PRODUCTION PROCESS OF 2,3'-BIPYRIDYL-6'-ONE
A production process where 2,3′-bipyridyl-6′-one can be produced in high purity at low cost on an industrial scale without using an expensive catalyst or special equipment is provided. A process for producing 2,3′-bipyridyl-6′-one comprises reacting an acetylpyridine derivative with at least one of compounds represented by formulae (II) to (V) to synthesize a bipyridine derivative and hydrolyzing the bipyridine derivative by one-pot preparation. In formulae (II) to (V), each of R2 to R8, X and Y represents a given group.
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Page/Page column 9

(2010/02/17)

PROCESS FOR PRODUCTION OF 2,3'-BIPYRIDYL-6'-ONE
A production process where 2,3'-bipyridyl-6'-one can be produced in high purity at low cost on an industrial scale without using an expensive catalyst or special equipment is provided. A process for producing 2,3'-bipyridyl-6'-one comprises reacting an acetylpyridine derivative with at least one of compounds represented by formulae (II) to (V) to synthesize a bipyridine derivative and hydrolyzing the bipyridine derivative by one-pot preparation. In formulae (II) to (V), each of R2 to R8, X and Y represents a given group.
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Page/Page column 13

(2009/12/07)

Synthesis of a neonicotinoide pesticide derivative via chemoenzymatic dynamic kinetic resolution
(Chemical Equation Presented) Chemoenzymatic dynamic kinetic resolution (DKR) via combined ruthenium and enzyme catalysis was used in the key step of a synthesis of a neonicotinoid pesticide derivative (S)-3. The DKR was carried out under mild conditions
Krumlinde, Patrik,Bogar, Krisztian,Baeckvall, Jan-E.
scheme or table
p. 7407 - 7410
(2010/01/06)

Identification of KD5170: A novel mercaptoketone-based histone deacetylase inhibitor
We report the identification of KD5170, a potent mercaptoketone-based Class I and II-histone deacetylase inhibitor that demonstrates broad spectrum cytotoxic activity against a range of human tumor-derived cell lines. KD5170 exhibits robust and sustained histone H3 hyperacetylation in HCT-116 xenograft tumors following single oral or iv dose and inhibition of tumor growth following chronic dosing.
Payne, Joseph E.,Bonnefous, Celine,Hassig, Christian A.,Symons, Kent T.,Guo, Xin,Nguyen, Phan-Manh,Annable, Tami,Wash, Paul L.,Hoffman, Timothy Z.,Rao, Tadimeti S.,Shiau, Andrew K.,Malecha, James W.,Noble, Stewart A.,Hager, Jeffrey H.,Smith, Nicholas D.
scheme or table
p. 6093 - 6096
(2009/07/18)

α-Mercaptoketone based histone deacetylase inhibitors
In an effort to discover novel non-hydroxamic acid histone deacetylase (HDAC) inhibitors, a novel α-mercaptoketone was identified in a high-throughput screen. Lead optimization of the screening hit, led to a number of potent HDAC inhibitors. In particular, α-mercaptoketone 19y (KD5150) exhibited nanomolar in vitro activity and inhibition of tumor growth in vivo.
Wash, Paul L.,Hoffman, Timothy Z.,Wiley, Brandon M.,Bonnefous, Celine,Smith, Nicholas D.,Sertic, Michael S.,Lawrence, Charles M.,Symons, Kent T.,Nguyen, Phan-Manh,Lustig, Kevin D.,Guo, Xin,Annable, Tami,Noble, Stewart A.,Hager, Jeffrey H.,Hassig, Christian A.,Malecha, James W.
scheme or table
p. 6482 - 6485
(2009/10/01)

NOVEL SULFONAMIDE SUBSTITUTED CHROMAN DERIVATIVES USEFUL AS BETA-3 ADRENORECEPTOR AGONISTS
This invention relates to novel sulfonamide substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.
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Page/Page column 25

(2008/12/07)

Multicyclic sulfonamide compounds as inhibitors of histone deacetylase for the treatment of disease
Disclosed herein are sulfonamide compounds of Formula VII as described herein. Methods and compositions are disclosed for treating disease states including, but not limited to cancers, autoimmune diseases, tissue damage, central nervous system disorders, neurodegenerative disorders, fibrosis, bone disorders, polyglutamine-repeat disorders, anemias, thalassemias, inflammatory conditions, cardiovascular conditions, and disorders in which angiogenesis play a role in pathogenesis, using the compounds of the invention. In addition, methods of modulating the activity of histone deacetylase (HDAC) are also disclosed.
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Page/Page column 17; 19

(2010/11/25)

5-(3-Bromophenyl)-7-(6-morpholin-4-ylpyridin-3-yl)pyrido[2,3-d] pyrimidin-4-ylamine: Structure-activity relationships of 7-substituted heteroaryl analogs as non-nucleoside adenosine kinase inhibitors
4-Amino-5,7-disubstituted pyridopyrimidines are potent, non-nucleoside inhibitors of adenosine kinase (AK). We recently identified a potent, orally efficacious analog, 4 containing a 7-pyridylmorpholine substituted ring system as the key structural element of this template. In this report, we disclose the pharmacologic effects of five- and six-membered heterocyclic ring replacements for the pyridine ring in 4. These replacements were found to have interesting effects on in vivo efficacy and genotoxicity as well as in vitro potency. We discovered that the nitrogen in the heterocyclic ring at C(7) is important for the modulation of mutagenic side effects (Ames assay).
Matulenko, Mark A.,Lee, Chih-Hung,Jiang, Meiqun,Frey, Robin R.,Cowart, Marlon D.,Bayburt, Erol K.,DiDomenico Jr., Stanley,Gfesser, Gregory A.,Gomtsyan, Arthur,Guo, Zhu Zheng,McKie, Jeffery A.,Stewart, Andrew O.,Yu, Haixia,Kohlhaas, Kathy L.,Alexander, Karen M.,McGaraughty, Steve,Wismer, Carol T.,Mikusa, Joseph,Marsh, Kennan C.,Snyder, Ronald D.,Diehl, Marilyn S.,Kowaluk, Elizabeth A.,Jarvis, Michael F.,Bhagwat, Shripad S.
p. 3705 - 3720
(2007/10/03)

AMIDE DERIVATIVE
The present invention provides an amide derivative represented by the following general formula (1): wherein R1 represents a saturated cyclic amino group, R2 represents alkyl, halogen or haloalkyl, R3 represents hydrogen or halogen, Het 2 represents pyridyl or pyrimidinyl, and Het 1 represents a group of the formula [6], or a salt thereof, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention is useful as a BCR-ABL tyrosine kinase inhibitor.
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Page/Page column 16

(2008/06/13)

INHIBITORS OF HISTONE DEACETYLASE
The invention relates to a series of compounds useful for inhibiting histone deacetylase (HDAC) enzymatic activity. The invention also provides a method for inhibiting histone descetylase in a cell using said compounds as well as a method for treating cell proliferative diseases and conditions using said HDAC inhibitors. Further, the invention provides pharmaceutical compositions comprising the HDAC inhibiting compounds and a pharmaceutically acceptable carrier.
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Page/Page column 71

(2010/02/14)

2-PROPENE-1-ONES AS HSP 70 INDUCERS
The present invention relates to novel compounds of 2-propene-1-one series, of general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them, wherein R5, R6, Q and Y are as defined in the specification. The present invention also relates to a process for preparing such compounds, compositions containing such compounds, and use of such compound and composition in medicine. The compounds of the general formula (I) induce HSP-70 and are useful for the treatment of diseases accompanying pathological stress in a living mammalian organism, including a human being, such as stroke, myocardial infarction, inflammatory disorder, hepatotoxicity, sepsis, diseases of viral origin, allograft rejection, tumourous diseases, gastric mucosal damage, brain haemorrhage, endothelial dysfunctions, diabetic complications, neuro-degenerative diseases, post-traumatic neuronal damage, acute renal failure, glaucoma and aging related skin degeneration.
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Page/Page column 116-117

(2010/02/14)

Synthesis and biological evaluation of pteridine and pyrazolopyrimidine based adenosine kinase inhibitors
Three new approaches have been tested to modify existing pyridopyrimidine and alkynylpyrimidine classes of nonnucleoside adenosine kinase inhibitors 2 and 3. 4-Amino-substituted pteridines 8a-e were generally less active than corresponding 5- and 6-substituted pyridopyrimidines 2. Pyrazolopyrimidine 13c with IC50=7.5nM was superior to its open chain alkynylpyrimidine analog 13g (IC50=22nM) while pyrrolopyrimidines such as 17a were inactive.
Gomtsyan, Arthur,Didomenico, Stanley,Lee, Chih-Hung,Stewart, Andrew O.,Bhagwat, Shripad S.,Kowaluk, Elizabeth A.,Jarvis, Michael F.
p. 4165 - 4168
(2007/10/03)

MUSCARINIC ANTAGONISTS
Heterocyclic derivatives of di-N-substituted piperazine or 1,4 di-substituted piperidine compounds in accordance with formula (I) (including all isomers, salts and solvates), wherein one of Y and Z is -N- and the other is -N- or -CH-; X is -O-, -S-, -SO-, -SO2- or -CH2-; Q is (1), (2), (3); R is alkyl, cycloalkyl, optionally substituted aryl or heteroaryl; R, R and R are H or alkyl; R is alkyl, cyclolalkyl or (4); R is H, alkyl, -C(O)alkyl, arylcarbonyl, -SO2alkyl, aryl-sulfonyl-C(O)Oalkyl, aryloxycarbonyl, -C(O)NH-alkyl or aryl-aminocarbonyl, wherein the aryl portion is optionally substituted; R is H or alkyl; and R is H, alkyl, hydroxyalkyl or alkoxyalkyl; are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of treatment are also disclosed.
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Page 7; 24

(2010/02/07)

2-AMINOPYRIMIDINE DERIVATIVES AS RAF KINASE INHIBITORS
This application discloses compounds that inhibit Raf kinase having the formula (I), wherein R1 is a phenyl radical or a heteroaryl radical; and R2 is a phenyl radical; or an N-oxide or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of proliferative diseases, such as cancer.
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Page/Page column 24

(2010/02/09)

Adenosine kinase inhibitors: Polar 7-substitutent of pyridopyrimidine derivatives improving their locomotor selectivity
We have discovered that polar 7-substituents of pyridopyrimidine derivatives affect not only whole cell AK inhibitory potency, but also selectivity in causing locomotor side effects in vivo animal models. We have identified compound, 1o, which has potent whole cell AK inhibitory potency, analgesic activity and minimal reduction of locomotor activity.
Zheng, Guo Zhu,Mao, Yue,Lee, Chih-Hung,Pratt, John K.,Koenig, John R.,Perner, Richard J.,Cowart, Marlon D.,Gfesser, Gregory A.,McGaraughty, Steve,Chu, Katharine L.,Zhu, Chang,Yu, Haixia,Kohlhaas, Kathy,Alexander, Karen M.,Wismer, Carol T.,Mikusa, Joseph,Jarvis, Michael F.,Kowaluk, Elizabeth A.,Stewart, Andrew O.
p. 3041 - 3044
(2007/10/03)

Asymmetric chloronicotinyl insecticide, 1-[1-(6-chloro-3-pyridyl)ethyl]-2-nitroiminoimidazolidine: preparation, resolution and biological activities toward insects and their nerve preparations.
The asymmetric chloronicotinyl insecticide, 1-[1-(6-chloro-3-pyridyl)ethyl]-2-nitroiminoimidazolidine, was prepared, and the absolute configurations of the enantiomers were determined by an X-ray analysis. The insecticidal activity against the housefly measured with metabolic inhibitors showed the (S) enantiomer to be slightly more active than the (R) isomer. Electrophysiological measurements on the American cockroach central nerve cord showed the compounds to elicite the impulses and subsequently blocked them. The neuroblocking potency of the (S) isomer was 5.9 microM, while that of the (R) isomer was as high as 73 microM. The molar concentrations required for 50% inhibition of the specific binding of [3H]imidacloprid to the housefly head membrane preparation were respectively 0.19 microM and 0.95 microM for the (S) and (R) isomers. This enatioselectivity ratio was smaller than 35 for nicotine isomers but greater than 2 for epibatidine isomers.
Kagabu, Shinzo,Kiriyama, Kazuhisa,Nishiwaki, Hisashi,Kumamoto, Yuko,Tada, Toshiji,Nishimura, Keiichiro
p. 980 - 988
(2007/10/03)

Carboxyl substituted chroman derivatives useful as beta 3 adrenoreceptor agonists
This invention is related to novel carboxyl substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.
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(2011/11/14)

CARBOXYL SUBSTITUTED CHROMAN DERIVATIVES USEFUL AS BETA 3 ADRENORECEPTOR AGONISTS
This invention is related to novel carboxyl substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.
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(2011/11/14)

Oxime compounds, their use, and intermediates for their production
Oxime compounds of formula (1) wherein R1, R2, and R3 are independently halogen, C1-C3 alkyl, C1-C3 halolalkyl, C1-C3 alkoxy, C1-C3 haloalkoxy, nitro, or cyano; R4 is 3,3-dihalogeno-2-propenyl; a is an integer of 0 to 2; Y is oxygen, sulfur, or NH; Z is oxygen, sulfur, or NR5wherein R5 is hydrogen, acetyl, or C1-C3 alkyl; and X is of formula (2) insecticidal/acaricidal agents containing them as active ingredients; and intermediates for their production.
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(2008/06/13)

Pyridopyrimidine analogues as novel adenosine kinase inhibitors
A novel series of pyridopyrimidine analogues 9 was identified as potent adenosine kinase inhibitors based on the SAR and computational studies. Substitution of the C7 position of the pyridopyrimidino core with C2′ substituted pyridino moiety increased the in vivo potency and enhanced oral bioavailability of these adenosine kinase inhibitors.
Zheng, Guo Zhu,Lee, Chih-Hung,Pratt, John K.,Perner, Richard J.,Jiang, Mei Qun,Gomtsyan, Arthur,Matulenko, Mark A.,Mao, Yui,Koenig, John R.,Kim, Ki H.,Muchmore, Steve,Yu, Haixia,Kohlhaas, Kathy,Alexander, Karen M.,McGaraughty, Steve,Chu, Katharine L.,Wismer, Carol T.,Mikusa, Joseph,Jarvis, Michael F.,Marsh, Kennan,Kowaluk, Elizabeth A.,Bhagwat, Shripad S.,Stewart, Andrew O.
p. 2071 - 2074
(2007/10/03)

Discovery of 4-amino-5-(3-bromophenyl)-7-(6-morpholino-pyridin-3-yl)pyrido [2,3-d]pyrimidine, an orally active, non-nucleoside adenosine kinase inhibitor
Adenosine (ADO) is an endogenous homeostatic inhibitory neuromodulator that reduces cellular excitability at sites of tissue injury and inflammation. Inhibition of adenosine kinase (AK), the primary metabolic enzyme for ADO, selectively increases ADO concentrations at sites of tissue trauma and enhances the analgesic and antiinflammatory actions of ADO. Optimization of the high-throughput screening lead, 4-amino-7-aryl-substituted pteridine (5) (AK IC50 = 440 nM), led to the identification of compound 21 (4-amino-5-(3-bromophenyl)-7-(6-morpholino-pyridin-3-yl)pyrido [2,3-d]pyrimidine, ABT-702), a novel, potent (AK IC50 = 1.7 nM) nonnucleoside AK inhibitor with oral activity in animal models of pain and inflammation.
Lee,Jiang,Cowart,Gfesser,Perner,Ki Hwan Kim,Yu Gui Gu,Williams,Jarvis,Kowaluk,Stewart,Bhagwat
p. 2133 - 2138
(2007/10/03)

Tertiary amines
Tertiary amines of the formula STR1 wherein A1, A2, A3, A4, L, M, p, T, and Q are as defined herein, have antimycotic and cholesterol-lowering activity.
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(2008/06/13)

Design of adenosine kinase inhibitors from the NMR-based screening of fragments
A strategy is described for designing high-affinity ligands using information derived from the NMR-based screening of fragments. The method involves the fragmentation of an existing lead molecule, identification of suitable replacements for the fragments, and incorporation of the newly identified fragments into the original scaffold. Using this technique, novel substituents were rapidly identified and incorporated into lead inhibitors of adenosine kinase that exhibited potent in vitro and in vivo activities. This approach is a valuable strategy for modifying existing leads to improve their potency, bioavailability, or toxicity profile and thus represents a useful technique for lead optimization.
Hajduk,Gomtsyan,Didomenico,Cowart,Bayburt,Solomon,Severin,Smith,Walter,Holzman,Stewart,McGaraughty,Jarvis,Kowaluk,Fesik
p. 4781 - 4786
(2007/10/03)

SULFONAMIDE SUBSTITUTED CHROMAN DERIVATIVES USEFUL AS BETA 3 ADRENORECEPTOR AGONISTS
This invention related to novel sulfonamide substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.
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(2011/11/14)

2-Pyrimidineamine derivatives and processes for their preparation
Compounds of general formula (1) are described wherein: Ar is an optionally substituted aromatic group; R2 is a hydrogen or halogen atom or a group -X1-R2a where X1 is a direct bond or a linker atom or group, and R2a is an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R3 is an optionally substituted heterocycloalkyl group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective protein tyrosine kinase inhibitors, particularly the kinases ZAP-70 and syk and are of use in the prophylaxis and treatment of immune or allergic diseases and diseases involving inappropriate platelet activation.
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(2008/06/13)

A concise route to novel 1-aryl and 1-pyridyl-2-azabicyclo[2.1.1]hexanes
A number of novel 1-aryl and 1-pyridyl-2-azabicyclo[2.1.1]hexane derivatives were prepared by an intramolecular [2+2] photocycloaddition in the presence of acetophenone as the sensitizer. Substitution of the azabicyclo[2.1.1]hexane ring was accomplished by appropriate choice of the heteroaryl ketone and allylamine starting materials. Several aryl 9a-e, g and pyridyl analogs 9h-l were prepared by this method. The structures of 9a and 9i were verified by X-ray crystallography. Several of the photoproducts 9 were converted into the corresponding N-Me and N-H 2,4-methanonicotine analogs 4 by reduction or hydrolysis of the N-carboethoxy group.
Piotrowski, David W.
p. 1091 - 1093
(2007/10/03)

3-pyridylethanolamines: Potent and selective human β3 adrenergic receptor agonists
The 3-pyridylethanolamine L-757,793 is a potent β3 AR agonist (EC50 6.3 nM, 70% activation) with 1,300- and 500-fold selectivity over binding to the β1 and β2 ARs, respectively. L-757,793 stimulated lipolysis in rhesus monkeys (ED50 0.2 mg/kg) with a maximum response equivalent to that elicited by isoproterenol.
Naylor, Elizabeth M.,Colandrea, Vincent J.,Candelore, Mari R.,Cascieri, Margaret A.,Colwell Jr., Lawrence F.,Deng, Liping,Feeney, William P.,Forrest, Michael J.,Hom, Gary J.,MacIntyre, D. Euan,Strader, Catherine D.,Tota, Laurie,Wang, Pei-Ran,Wyvratt, Matthew J.,Fisher, Michael H.,Weber, Ann E.
p. 3087 - 3092
(2007/10/03)

Pyrimidineamine derivatives and processes for the preparation thereof
N-phenyl-2-pyrimidineamine derivatives of formula (I) wherein the substituents are as defined in claim 1 are described. Those compounds can be used for example, in the treatment of tumour diseases. STR1
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(2008/06/13)

Magnesium chloride catalysed acylation reaction
An efficient and practical preparation of methyl ketones, via a magnesium chloride catalysed acylation reaction of dimethyl malonate with acid chlorides in the presence of tertiary base and followed by a decarbmethoxylation reaction, is described.
Kuo
p. 9233 - 9236
(2007/10/02)