cas 129611-32-1, 2-Bromo-3-hydroxy-6-iodopyridine

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Halogenation of pyridinols using bis(sym-collidine)iodine(I) and bis(sym-collidine)bromine(I) hexafluorophosphate
Iodination and bromination of pyridinols was achieved by action of the title reagents in methylene chloride.
Rousseau, Gerard,Robin, Sylvie
p. 2467 - 2470
(1997)
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NOVEL ISOINDOLINE DERIVATIVE, AND PHARMACEUTICAL COMPOSITION AND APPLICATION THEREOF
Disclosed are a novel isoindoline derivative, a pharmaceutical composition and use thereof. The compound of formula I, or the pharmaceutically acceptable salt, solvate, polymorph, co-crystal, stereoisomer, isotopic compound, metabolite or prodrug thereof disclosed in the invention can regulate the generation and/or activity of PDE4 and/or TNF-α so as to effectively treat cancer and inflammatory diseases.
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Paragraph 0199; 0206-0207

(2020/01/22)

Boron Containing PDE4 Inhibitors
The present invention relates to boron containing compounds of Formula (I) [in-line-formulae]X—Y—Z?? Formula (I)[/in-line-formulae] that inhibit phosphodiesterase 4 (PDE4). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating diseases, conditions, or disorders ameliorated by inhibition of PDE4.
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Paragraph 0731-0732

(2020/04/29)

Condensed tricyclic compound and applications in medicines
The invention relates to a condensed tricyclic compound and applications in medicines, particularly to applications of the condensed tricyclic compound as drugs for treating and/or preventing hepatitis B, specifically to a compound represented by general
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Paragraph 0554; 0556-0559

(2020/04/02)

Fused tricyclic compound and application in medicines
The invention relates to a condensed tricyclic compound and application in medicines, particularly to application of the condensed tricyclic compound as a medicine for treating and/or preventing hepatitis B. Specifically the present invention relates to a
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Paragraph 0451-0456

(2020/06/17)

A 5, 6 - dimethoxy -2 - picolinic acid synthesis method
This invention relates to a 5, 6 - dimethoxy - 2 - pyridine carboxylic acid synthesis method. To solve the synthetic method on the reaction of high temperature, operation of the experiment is difficult, high requirements on equipment, unfavorable to industrialization production and amplification of the technical problem. The invention synthetic method comprises the following steps: 1st step, at room temperature, 2 - bromo - 3 - hydroxy pyridine in the potassium carbonate aqueous solution and hydrazine hydrate in the reaction, to obtain compound 1, product need purification, directly used for the next step reaction; 2nd step, compound 1 in N, N - dimethyl formamide and potassium carbonate in the reaction after adding methyl iodide, stirring overnight, to obtain compound 2; 3rd step, compound 2 and sodium methoxide in N, N - dimethyl formamide in reaction, bromine quilt methoxy selectively substituted, to obtain compound 3; 4th step, at the low temperature compound 3 and butyl lithium in tetrahydrofuran reaction, then added with the solid carbon dioxide, the reaction at room temperature, acidified by hydrochloric acid, to obtain the target compound 4, in petroleum ether and ethyl acetate mixed solvent recrystallization purification get the pure product.
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Paragraph 0007

(2019/02/13)

NOVEL AMINOPYRIDINEMETHANOL COMPOUNDS AND THEIR USE
The present invention is directed to novel compounds of Formula (I): pharmaceutically acceptable salts or solvates thereof, and their use, in particular in the treatment or prevention of malaria.
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Page/Page column 51; 66; 67

(2019/05/22)

Oxadiazolopyridine Derivates for Use as Ghrelin O-Acyl Transferase (GOAT) Inhibitors
The present invention relates to compounds of general formula I, wherein the groups R1, R2 and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to ghrelin O-acyl transferase (GOAT) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular obesity.
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Paragraph 0289-0292

(2018/03/01)

COMPOUNDS AND USES THEREOF
The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.
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Page/Page column 214

(2018/05/17)

Synthesis of [11C]MK-1064 as a new PET radioligand for imaging of orexin-2 receptor
The reference standard MK-1064 {5″-chloro-N-((5,6-dimethoxypyridin-2-yl)methyl)-[2,2′:5′,3″-terpyridine]-3′-carboxamide} was synthesized from methyl 2-chloro-5-iodonicotinate and 5-(chloropyridin-3-yl)boronic acid in 4 steps with 33% overall chemical yield. The precursor desmethyl-MK-1064 {5″-chloro-N-((5-hydroxy-6-methoxypyridin-2-yl)methyl)-[2,2′:5′,3″-terpyridine]-3′-carboxamide} for radiolabeling was synthesized from 2-bromopyridin-3-ol and 5″-chloro-[2,2′:5′,3″-terpyridine]-3′-carboxylic acid in 6 steps with 17% overall chemical yield. The target tracer [11C]MK-1064 {5″-chloro-N-((5-[11C]methoxy-6-methoxypyridin-2-yl)methyl)-[2,2′:5′,3″-terpyridine]-3′-carboxamide} was prepared by O-[11C]methylation of its corresponding precursor desmethyl-MK-1064 with [11C]CH3OTf under basic condition and isolated by a simplified solid-phase extraction (SPE) method in 50–60% decay corrected radiochemical yields based on [11C]CO2at end of bombardment (EOB). The overall synthesis time from EOB was 23?min, the radiochemical purity was >99%, and the specific activity at end of synthesis (EOS) was 185–555?GBq/μmol.
Gao, Mingzhang,Wang, Min,Zheng, Qi-Huang
p. 3694 - 3699
(2016/07/21)

THERAPEUTIC HYDROXYPYRIDINONES, HYDROXYPYRIMIDINONES AND HYDROXYPYRIDAZINONES
The invention provides compounds of formula (I): and salts and prodrugs thereof wherein R4, X1 and X2 have any of the meanings defined in the specification, as well as pharmaceutical compositions comprising the compounds or salts and methods for their use in therapy. The compounds have useful antiviral properties.
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Page/Page column 37

(2014/04/03)

Aryl Derivatives And Uses Thereof
The present invention relates to antimalarial compounds and their use against protozoa of the genus Plasmodium, including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.
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Paragraph 0374

(2014/05/20)

CYCLOALKENYL ARYL DERIVATIVES FOR CETP INHIBITOR
The present invention relates to cycloalkenyl aryl derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof; a method for preparing the derivatives; and pharmaceutical compositions containing the same.
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Paragraph 0043; 0591; 0592

(2014/02/16)

Phenyl substituted 3-hydroxypyridin-2(1H)-ones: Inhibitors of influenza A endonuclease
Inhibition of the endonuclease activity of influenza RNA-dependent RNA polymerase is recognized as an attractive target for the development of new agents for the treatment of influenza infection. Our earlier study employing small molecule fragment screening using a high-resolution crystal form of pandemic 2009 H1N1 influenza A endonuclease domain (PAN) resulted in the identification of 5-chloro-3-hydroxypyridin-2(1H)-one as a bimetal chelating ligand at the active site of the enzyme. In the present study, several phenyl substituted 3-hydroxypyridin-2(1H)-one compounds were synthesized and evaluated for their ability to inhibit the endonuclease activity as measured by a high-throughput fluorescence assay. Two of the more potent compounds in this series, 16 and 18, had IC50 values of 11 and 23 nM in the enzymatic assay, respectively. Crystal structures revealed that these compounds had distinct binding modes that chelate the two active site metal ions (M1 and M2) using only two chelating groups. The SAR and the binding mode of these 3-hydroxypyridin-2-ones provide a basis for developing a new class of anti-influenza drugs.
Parhi, Ajit K.,Xiang, Amy,Bauman, Joseph D.,Patel, Disha,Vijayan,Das, Kalyan,Arnold, Eddy,Lavoie, Edmond J.
p. 6435 - 6446
(2013/10/22)

Dual selectivity: Electrophile and nucleophile selective cross-coupling reactions on a single aromatic substrate
The development of a high yielding, both nucleophile and electrophile selective cross-coupling reaction with aromatic rings is presented. The reaction is general with respect to functional groups. Furthermore, the products still contain a boronic ester and a bromide. These two functional groups allow them to be easy-to-prepare, highly complex starting materials for further reactions, avoiding protecting group transformations.
Heinrich, Annika C. J.,Thiedemann, Birk,Gates, Paul J.,Staubitz, Anne
supporting information
p. 4666 - 4669
(2013/10/08)

CYCLOALKENYL ARYL DERIVATIVES FOR CETP INHIBITOR
The present invention relates to cycloalkenyl aryl derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof; a method for preparing the derivatives; and pharmaceutical compositions containing the same. The compounds of the present invention show the effect of CETP activity inhibition. It means that the compounds can increase HDL-cholesterol and decrease LDL-cholesterol.
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Page/Page column 41-42; 145-146

(2012/11/06)

INHIBITORS OF CATECHOL O-METHYL TRANSFERASE AND THEIR USE IN THE TREATMENT OF PSYCHOTIC DISORDERS
The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. Th
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Page/Page column 54

(2011/10/03)

COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS
This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
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Page/Page column 141-142

(2010/06/11)

Synthesis of the phenylpyridal scaffold as a helical peptide mimetic
Phenylpyridal- and phenyldipyridal-based scaffolds have been designed and synthesized as novel helical peptide mimetics. The synthesis required optimisation and selective alkylation in producing 2,6-functionalized 3-hydroxypyridine derivatives for a convergent scheme. The pyridine analogues were coupled by a series of Suzuki/Stille types cross-coupling reactions. A series of biaryl and ter-aryl substituted heterocycles were produced. The synthetic approach was concise and high yielding allowing large variability at the wanted sidechain attachment points. A number of compounds were synthesised to show the versatility of the strategy.
Bourne, Gregory T.,Kuster, Daniel J.,Marshall, Garland R.
supporting information; experimental part
p. 8439 - 8445
(2010/09/08)

TRIPYRIDYL CARBOXAMIDE OREXIN RECEPTOR ANTAGONISTS
The present invention is directed to tripyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
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Page/Page column 17-18

(2010/03/02)

ISONICOTINAMIDE OREXIN RECEPTOR ANTAGONISTS
The present invention is directed to isonicotinamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. Th
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Page/Page column 47; 54-55

(2010/05/14)

PYRIDAZINE CARBOXAMIDE OREXIN RECEPTOR ANTAGONISTS
The present invention is directed to pyridazine carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
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Page/Page column 45

(2010/05/14)

PYRAZINE CARBOXAMIDE OREXIN RECEPTOR ANTAGONISTS
The present invention is directed to pyrazine carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involve
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Page/Page column 41

(2010/12/29)

Design of potent IGF1-R inhibitors related to bis-azaindoles
From an azaindole lead, identified in high throughput screen, a series of potent bis-azaindole inhibitors of IGF1-R have been synthesized using rational drug design and SAR based on a in silico binding mode hypothesis. Although the resulting compounds produced the expected improved potency, the model was not validated by the co-crystallization experiments with IGF1-R.
Nemecek, Conception,Metz, William A.,Wentzler, Sylvie,Ding, Fa-Xiang,Venot, Corinne,Souaille, Catherine,Dagallier, Anne,Maignan, Sebastien,Guilloteau, Jean-Pierre,Bernard, Francois,Henry, Alain,Grapinet, Sandrine,Lesuisse, Dominique
scheme or table
p. 100 - 106
(2011/03/19)

PYRIDINE CARBOXAMIDE OREXIN RECEPTOR ANTAGONISTS
The present invention is directed to pyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved
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Page/Page column 70

(2009/07/03)

Novel Bis-Azaindole Derivatives, Preparation And Pharmaceutical Use Thereof As Kinase Inhibitors
Disclosed are compounds of formula (I): wherein R1, R2, R3, R4, and R5 have the meanings given in the description, and to salts thereof, pharmaceutical compositions comprising said compounds and the use thereof as protein kinase inhibitors.
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Page/Page column 25; 22

(2010/11/30)

TRISUBSTITUTED AMINE COMPOUND
The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted heterocyclic group, and the like; R1 is an optionally substituted alkyl group, wherein the alkyl group further may optionally be substituted by an optionally substituted homocyclic group, and the like; and R2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.
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Page/Page column 165-166

(2008/06/13)

PHOSPHODIESTERASE 4 INHIBITORS
PDE4 inhibition is achieved by novel compounds,' e.g., N-substituted diarylamine analogs. The compounds of the present invention are of Formulas I-III; (I), (II) and (III) wherein A, B, D, E, G, J, K, R1, R2, R3, R4/
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Page/Page column 71

(2008/06/13)

PHOSPHODIESTERASE 4 INHIBITORS, INCLUDING N-SUBSTITUTED DIARYLAMINE ANALOGS
PDE4 inhibition is achieved by novel compounds, e.g., N-substituted diarylamine analogs. The compounds of the present invention are of Formula (I), wherein A, B, D, R1, R2, R3 and R4 are as defined herein.
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Page/Page column 68; 80-81

(2010/02/12)

Quinuclidine compounds and drugs containing the same as the active ingredient
The present invention provides an excellent squalene synthesizing enzyme inhibitor. Specifically, it provides a compound (I) represented by the following formula, a salt thereof or a hydrate of them. In which R1 represents (1) hydrogen atom or (2) hydroxyl group; HAr represents an aromatic heterocycle which may be substituted with 1 to 3 groups; Ar represents an optionally substituted aromatic ring; W represents a chain represented by (1) —CH2—CH2— which may be substituted, (2) —CH=CH— which may be substituted, (3) —C≡C—, (4) —NH—CO—, (5) —CO—NH—, (6) —NH—CH2—, (7) —CH2—NH—, (8) —CH2—CO—, (9) —CO—CH2—, (10) —NH—S(O)l—, (11) —S(O)l—NH—, (12) —CH2—S(O)— or (13) —S(O)l—CH2— (l denotes 0, 1 or 2); and X represents a chain represented by (1) a single bond, (2) an optionally substituted C1-6 alkylene chain, (3) an optionally substituted C2-6 alkenylene chain, (4) an optionally substituted C2-6 alkynylene chain, (5) a formula —Q— (wherein Q represents oxygen atom, sulfur atom, CO or N(R2) (wherein R2 represents a C1-6 alkyl group or a C1-6 alkoxy group)), (6) —NH—CO—, (7) —CO—NH—, (8) —NH—CH2—, (9) —CH2—NH—, (10) —CH2—CO—, (11) —CO—CH2—, (12) —NH—S(O)m—, (13) —S(O)m—NH—, (14) —CH2—S(O)m—, (15) —S(O)m—CH2— (wherein m denotes 0, 1 or 2) or (16) —(CH2)n—O— (wherein n denotes an integer from 1 to 6).
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(2008/06/13)

Total synthesis of (±)-cytisine
(equation presented) The nicotine partial agonist cytisine was prepared in five steps featuring an "in situ" Stille or Suzuki biaryl pyridine coupling. Differentiation of the pyridyl rings was accomplished via selective benzylation and then reduction of a pyridinium ring. The penultimate diazabicyclo[3.3.1]-nonane intermediate was obtained with high diastereoselectivity. A similar sequence has been employed for the synthesis of novel derivative 9-methoxycytisine.
O'Neill, Brian T.,Yohannes, Daniel,Bundesmann, Mark W.,Arnold, Eric P.
p. 4201 - 4204
(2007/10/03)