cas 178876-82-9, Methyl 6-amino-5-bromopyridine-2-carboxylate

Articles about 178876-82-9Total 19 be found

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IMIDAZOPYRIDINE DERIVATIVES AS ALPHA4BETA7 INTEGRIN INHIBITORS
The present disclosure provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing co
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Paragraph 0290

(2020/05/28)

Novel urate anion transporter 1 (URAT1) inhibitors and application thereof in medicines
The invention discloses novel urate anion transporter 1 (URAT1) inhibitors and application thereof in medicines. The novel URAT1 inhibitors are compounds shown in a formula (I) and pharmacologically acceptable salts of the compounds, wherein Y or Z is respectively and independently selected from N or CH; R1 or R2 is respectively and independently selected from H, D, halogen, cyano, hydroxyl, carboxyl, C1-4 alkyl, substituted C1-4 alkyl, C3-4 cycloalkyl, C1-4 alkoxy, substituted C1-4 alkoxy, phenyl, substituted phenyl, heterocyclic aryl or substituted heterocyclic aryl; R3 or R4 is respectively and independently selected from H or C1-3 alkyl, or R3 and R4 form 3-6-membered cycloalkyl together; R5 is H, C1-4 alkyl or substituted C1-4 alkyl. The compounds provided by the invention can be applied to preparation of uric acid excretion promoting medicines, and are especially used for medicines for treating or preventing hyperuricemia or gout. The formula (I) is described in the description.
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Paragraph 0081-0083

(2017/11/04)

Discovery and Optimization of Selective Nav1.8 Modulator Series That Demonstrate Efficacy in Preclinical Models of Pain
Voltage-gated sodium channels, in particular Nav1.8, can be targeted for the treatment of neuropathic and inflammatory pain. Herein, we described the optimization of Nav1.8 modulator series to deliver subtype selective, state, and use-dependent chemical matter that is efficacious in preclinical models of neuropathic and inflammatory pain. (Chemical Presented).
Bagal, Sharan K.,Bungay, Peter J.,Denton, Stephen M.,Gibson, Karl R.,Glossop, Melanie S.,Hay, Tanya L.,Kemp, Mark I.,Lane, Charlotte A. L.,Lewis, Mark L.,Maw, Graham N.,Million, William A.,Payne, C. Elizabeth,Poinsard, Cedric,Rawson, David J.,Stammen, Blanda L.,Stevens, Edward B.,Thompson, Lisa R.
p. 650 - 654
(2015/06/30)

HETEROARYL SUBSTITUTED PIPERIDINES
The invention relates to compounds of formula where hetaryl I, hetaryl II, R1,R2,R3, R4, m, n, and o are as defined in the specification or to pharmaceutically active acid addition salts thereof. The compounds of formula I are modulators for amyloid beta and thus may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
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(2011/09/14)

PIPERIDINE DERIVATIVES
The invention relates to compounds of formula (I). Hetaryl I is a five or six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N; hetaryl II is a five or six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N, or is a two membered ring system containing 1 to 4 heteroatoms selected from S, O or N, wherein at least one ring is aromatic in nature; R1 is lower alkyl, lower alkoxy, lower alkyl substituted by halogen, or halogen; R2 is halogen, lower alkyl, lower alkoxy, hydroxy, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy or benzo[1,3]dioxolyl, or is -(CHR)p-phenyl, optionally substituted by halogen, lower alkyl, lower alkoxy, S(O)2 -1ower alkyl, cyano, nitro, lower alkoxy substituted by halogen, dimethylamino, -(CH2)P-NHC(O)O-Iower alkyl, or lower alkyl substituted by halogen, and R is hydrogen, halogen, hydroxy or lower alkoxy, or is cycloalkenyl or cycloalkyl, optionally substituted by hydroxy or lower alkyl substituted by halogen, or is a five or six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N, which is optionally substituted by halogen, lower alkyl, lower alkoxy or dimethylamino, or is O-phenyl, optionally substituted by halogen, or is heterocycloalkyl, optionally substituted by halogen, hydroxy, lower alkyl substituted by halogen or C(O)O-lower alkyl; R3 is hydrogen, lower alkyl, cyano or phenyl; R4 is lower alkoxy, lower alkyl or halogen; p is 0 or 1; n is 0, 1 or 2; if n is 2 then R4 may be the same or different; m is 0, 1 or 2; if m is 2 then R1 may be the same or different; o is 0, 1, 2 or 3, if o is 2 or 3 then R2 may be the same or different; or to pharmaceutically active acid addition salts thereof. The compounds of formula (I) are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of beta- amyloid in the brain, in particular Alzheimer?s disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome
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(2011/09/19)

ANTI PARASITIC DIHYDROAZOLE COMPOUNDS AND COMPOSITIONS COMPRISING SAME
The present invention relates to novel dihydroazole of formula (I) and salts thereof: Wherein R1, A1, A2, G, X and Y are as defined in the description, compositions thereof, processes for their preparation and their uses t
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Page/Page column 95

(2011/07/07)

ANTIPARISITIC DIHYDROAZOLE COMPOUNDS AND COMPOSITIONS COMPRISING SAME
The present invention relates to novel dihydroazole of formula (I) and salts thereof: Wherein R1, A1, A2, G, X and Y are as defined in the description, compositions thereof, processes for their preparation and their uses t
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Page/Page column 40

(2011/07/06)

GAMMA SECRETASE MODULATORS
The invention relates to compounds of formula wherein R1, R1′, R2, R3, n, A, and hetaryl are defined herein or to pharmaceutically active acid addition salts thereof. The present compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
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(2011/08/08)

GAMMA SECRETASE MODULATERS
The invention relates to compounds of formula ( I ) wherein R1/R1' are independently from each other hydrogen, halogen, lower alkoxy or cyano; R2 is lower alkyl, halogen, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, lower alkyl substituted by OR, =0, -C(O)O-lower alkyl, -C(O)NH-lower alkyl, cyano, CH2-O-lower alkyl, cycloalkyl, NRR'or is -O-(CH2)o-phenyl optionally substituted by halogen, or is -(CH2)o-phenyl optionally substituted by one, two or three substituents, selected from halogen, -(CH2)o-cyano, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, C(O)H, -CH2-NH2-, -CH2-NH-C(O)O-lower alkyl, -CH2-NH-C(O)-lower alkyl, -CH2-NH-lower alkyl, -CH2-NH-S(O)2-lower alkyl, lower alkoxy or by lower alkoxy substituted by halogen, or is -(CH2)o-cycloalkyl, or is -(CH2)o-heterocycloalkyl which is optionally substituted by halogen, CF3, lower alkyl, -CH2CN, -C(O)-lower alkyl, -C(O)O-lower alkyl or S(O)2-lower alkyl, or is heteroaryl selected from the group consisting of furanyl, pyrazinyl, pyridinyl, benzooxazolyl or benzoimidazolyl which are optionally substituted by lower alkyl, or is 4-methyl-3,4-dihydro-2H-benzo[l,4]oxazine R and R' are independently from each other hydrogen or lower alkyl, and o is 0 or 1; R3 may occur once or twice and is lower alkyl; A is Formula a), b), c), d), e), f), h), i), j) and Formula k); R2' is hydrogen, lower alkyl, lower alkyl substituted by halogen, C(O)-lower alkyl, S(O)2-lower alkyl or phenyl optionally substituted by halogen; hetaryl is a 5 or 6 membered N, S or O-containing heteroaryl group; n is O, 1, 2 or 3; if n is 2 or 3, R2 may be the same or not; or to pharmaceutically active acid addition salts thereof. The present compounds of formula ( I ) are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi- infarct dementia, dementia pugilistica and Down syndrome.
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(2011/08/21)

5-Quinoline derivatives having an anti-bacterial activity
The present invention describes novel anti-bacterial compounds of the formula (I). These compounds are, amongst others, of interest as inhibitors of DNA gyrase and topoisomerases, for example of topoisomerase II and IV.
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Page/Page column 10

(2010/12/31)

Optimisation of permanganate oxidation and suzuki-miyaura coupling steps in the synthesis of a Nav1.8 Sodium channel modulator
The development is described of a viable kilo-scale synthesis of the Nav1.8 sodium channel modulator, N-methyl-6-amino- 5-(2,3,5-trichlorophenyl)pyridine-2-carboxamide(PF-1247324) in five steps, starting from 6-amino-5-bromo-2-picoline, in 33% overall yield. Two key steps required significant optimisation to improve yield and reproducibility. Oxidation of 6-acetamido-5-bromo-2-methylpyridine by permanganate to give the corresponding carboxylic acid derivative was improved by adding potassium dihydrogen phosphate, which moderated the reaction mixture pH and doubled the yield. The potassium fluoride-promoted Suzuki-Miyaura coupling between 2,4,5-trichlorophenylboronic acid and methyl 6-amino-5-bromopyridine-2- carboxylate, catalysed by tri(tert-butyl)phosphinepalladium (0), proceeded reliably to completion at room temperature in high yield when water was added. Anhydrous reaction mixtures reacted much more slowly, and 'wet' mixtures led to significant proto- deboronation in the absence of sufficient active catalyst. In the final step, amidation of the ester with methylamine gave PF-1247324.
Fray, M. Jonathan,Gillmore, Adam T.,Glossop, Melanie S.,McManus, David J.,Moses, Ian B.,Praquin, Celine F.B.,Reeves, Keith A.,Thompson, Lisa R.
experimental part
p. 263 - 271
(2010/04/28)

The design of efficient and selective routes to pyridyl analogues of 3-oxo-3,4-dihydro-2H-1,4-(benzothiazine or benzoxazine)-6-carbaldehydes
This Letter describes the synthesis of challenging pyridyl analogues of 3-oxo-3,4-dihydro-2H-1,4-(benzothiazine or benzoxazine)-6-carbaldehydes. The six different routes described are high yielding, contain no major purification issues and have been used to give gram quantities of each aldehyde.
Brooks, Gerald,Dabbs, Steven,Davies, David T.,Hennessy, Alan J.,Jones, Graham E.,Markwell, Roger E.,Miles, Timothy J.,Owston, Nathan A.,Pearson, Neil D.,Peng, Tony W.
scheme or table
p. 5035 - 5037
(2011/01/04)

IMIDAZOPYRIDINE COMPOUNDS USEFUL AS MMP-13 INHIBITORS
Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I.
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Page/Page column 42

(2009/12/23)

PYRIDINE DERIVATIVES AS SODIUM CHANNEL MODULATORS
The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds for the treatment of pain.
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Page/Page column 35-36

(2010/11/28)

Identification of thieno[3,2-b]pyrroles as allosteric inhibitors of hepatitis C virus NS5B polymerase
Thieno[3,2-b]pyrroles are a novel class of allosteric inhibitors of HCV NS5B RNA-dependent RNA polymerase which show potent affinity for the NS5B enzyme. Introduction of a polar substituent in the position N1 led to a compound that efficiently blocks subg
Ontoria, Jesus M.,Martin Hernando, Jose I.,Malancona, Savina,Attenni, Barbara,Stansfield, Ian,Conte, Immacolata,Ercolani, Caterina,Habermann, Joerg,Ponzi, Simona,Di Filippo, Marcello,Koch, Uwe,Rowley, Michael,Narjes, Frank
p. 4026 - 4030
(2007/10/03)

NOVEL COMPOUNDS HAVING AN ANTI-BACTERIAL ACTIVITY
The present invention describes novel anti-bacterial compounds of formula (I). These compounds are, amongst others, of interest as inhibitors of DNA gyrase.
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Page/Page column 53

(2010/10/20)

PYRIDINE DERIVATIVES
The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds for the treatment of pain.
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Page/Page column 46-47

(2008/06/13)

NITROGEN-CONTAINING BICYCLIC HETEROCYCLES FOR USE AS ANTIBACTERIALS
Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives hereof useful in methods of treatment of bacterial infections in mammals, particularly man.
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Page/Page column 94

(2010/02/07)

Total synthesis of dimethyl sulfomycinamate
Dimethyl sulfomycinamate (1), a methanolysis product from the natural antibiotic sulfomycin I, is synthesized in 11 steps. The chemistry of various pyridine, thiazole, and oxazole heterocycles and their coupling reactions under palladium catalysis are examined. The key transformations in the synthesis are the selective palladium-catalyzed coupling reactions on doubly activated pyridine 62 and the condensation reaction between bromo ketone 69 and amide 28 to form the oxazole moiety 76. The first preparation of oxazole triflates is described, as are some of their chemical properties.
Kelly, T. Ross,Lang, Fengrui
p. 4623 - 4633
(2007/10/03)