cas 36052-26-3, 6-AMINOPICOLINIC ACID METHYL ESTER

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POLY HETEROCYCLIC CONJUGATES AND THEIR PHARMACEUTICAL USES
Compounds of Formula (I) shown below and a pharmaceutical composition containing one of the compounds: Each of the variables is defined herein. Also disclosed is a method of treating a condition associated with uncontrolled cell growth with a compound of Formula (I).
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Paragraph 0039-0041

(2022/01/04)

FUSED PYRIMIDINE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF FIBROTIC DISEASES
The present invention discloses compounds according to Formula I: Wherein A, B, R1, R2, and Cy are as defined herein. The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of fibrotic diseases, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, pain, and/or abnormal angiogenesis associated diseases by administering the compounds of the invention.
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Paragraph 0328-0329

(2021/02/25)

Discovery of highly reactive peptide tag by ELISA-type screening for specific cysteine conjugation
We report the discovery of a highly reactive peptide tag for the specific cysteine conjugation of proteins. Screening of cysteine-containing peptides using ELISA-type screening yielded a 19-amino acid tag (DCPPPDDAADDAADDAADD), named DCP3 tag, which enabl
Kurashige, Nobutaka,Fuchida, Hirokazu,Tabata, Shigekazu,Uchinomiya, Shohei,Ojida, Akio
supporting information
p. 3486 - 3489
(2017/07/07)

NOVEL COMPOUND, ORGANIC CATION TRANSPORTER 3 DETECTION AGENT, AND ORGANIC CATION TRANSPORTER 3 ACTIVITY INHIBITOR
[Problem] The present invention addresses the problem of providing a novel compound. The present invention also addresses the problem of providing an OCT3 detection agent or an OCT3 activity inhibitor, which comprises the novel compound. [Solution] A compound represented by formula (A), a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof. ????????R1-R2-R3-R4?????(A)
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Paragraph 0543-0544; 0547-0548

(2016/08/17)

Cation-halide transport through peptide pores containing aminopicolinic acid
Synthetic pores that selectively transport ions of biological significance through membranes could be potentially used in medical diagnostics or therapeutics. Herein, we report cation-selective octapeptide pores derived from alanine and aminopicolinic acid. The ion transport mechanism through the pores has been established to be a cation-chloride symport. The cation-chloride co-transport is biologically essential for the efficient functioning of the central nervous system and has been implicated in diseases such as epilepsy. The pores formed in synthetic lipid bilayers do not exhibit any closing events. The ease of synthesis as well as infinite lifetimes of these pores provides scope for modifying their transport behaviour to develop sensors.
Basak, Debajyoti,Sridhar, Sucheta,Bera, Amal K.,Madhavan, Nandita
supporting information
p. 4712 - 4717
(2016/06/09)

TRISUBSTITUTED HETEROCYCLIC DERIVATIVES AS ROR GAMMA MODULATORS
The present invention provides trisubstituted heterocyclic derivatives of formula (I), which may be therapeutically useful, more particularly as RORγ modulators; (I) in which R1, R2, R3, Ra, X, L, m and ring A have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder where there is an advantage in modulating RORγ receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the trisubstituted heterocyclic derivatives of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
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Page/Page column 59

(2014/09/03)

Synthesis, structural investigation and computational modelling of water-binding aquafoldamers
Detailed studies on water-binding aquafoldamers are presented that illustrate the potential use of the elongated larger aquafoldamers for recognizing larger water clusters of diverse topologies. A novel self-trapping dimerization mode involving two tetramer molecules is proposed, which is consistent with the obtained varying experimental evidences. The Royal Society of Chemistry 2012.
Zhao, Huaiqing,Ong, Wei Qiang,Fang, Xiao,Zhou, Feng,Hii, Meng Ni,Li, Sam Fong Yau,Su, Haibin,Zeng, Huaqiang
p. 1172 - 1180
(2012/03/07)

Convenient synthesis of aminopyridinecarboxylic acids
6-(Alkylamino)pyridine-2-carboxylic acids and 5-(alkylamino)pyridine-3- carboxylic acids were conveniently synthesized from dibromopyridine in satisfactory yields.
Okamoto, Iwao,Terashima, Masayuki,Yoshioka, Rempei,Muramatsu, Tomonori,Kojima, Satomi,Inoue, Haruka,Takahashi, Mio,Morita, Nobuyoshi,Tamura, Osamu
p. 2343 - 2352
(2011/11/06)

Computational prediction and experimental verification of pyridine-based helical oligoamides containing four repeating units per helical turn
Aided by high level ab initio computational modeling, we successfully designed and experimentally proved a new set of backbone-rigidified pyridine-based folding oligoamides that require approximately four repeating units to form a helical turn.
Ong, Wei Qiang,Zhao, Huaiqing,Du, Zhiyun,Yeh, Jared Ze Yang,Ren, Changliang,Tan, Leon Zhen Wei,Zhang, Kun,Zeng, Huaqiang
p. 6416 - 6418
(2011/07/09)

Encapsulation of conventional and unconventional water dimers by water-binding foldamers
Water-binding foldamers have been rarely studied. By orienting both H-bond donors and acceptors toward their interior, two pyridine-derived crescent-shaped folding oligoamides were found to be capable of trapping both conventional and unconventional water dimer clusters in their cavity (～2.5 A radius). In the unconventional water dimer cluster, the two water molecules stay in contact via an unusual H-H interaction (2.25 A) rather than the typical H-bond.
Ong, Wei Qiang,Zhao, Huaiqing,Fang, Xiao,Woen, Susanto,Zhou, Feng,Yap, Weiliang,Su, Haibin,Li, Sam F. Y.,Zeng, Huaqiang
p. 3194 - 3197
(2011/08/06)

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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Page/Page column 61

(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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Page/Page column 129

(2011/08/21)

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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Page/Page column 45

(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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Page/Page column 91-92

(2011/09/19)

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.
body text
p. 263 - 271
(2010/04/28)

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)

TRICYCLIC COMPOUND AND PHARMACEUTICAL USE THEREOF
The present invention provides a compound represented by the formula wherein R1 is a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or a heterocyclic group opt
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Page/Page column 48

(2009/09/26)

TRICYCLIC DERIVATIVES AS INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP)
The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion
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Page/Page column 52

(2009/10/22)

A general and efficient 2-amination of pyridines and quinolines
(Chemical Equation Presented) Pyridine N-oxides were converted to 2-aminopyridines in a one-pot fashion using Ts2O-t-BuNH2 followed by in situ deprotection with TFA. The amination proceeded in high yields, excellent 2-/4-selectivity, and with good functional group compatibility. 2-Amino (iso)quinolines were also obtained in the same manner. Combined with the simple oxidation of pyridines to pyridine N-oxides, this method provides a general and efficient way for amination of 2-unsubstituted pyridines.
Yin, Jingjun,Xiang, Bangping,Huffman, Mark A.,Raab, Conrad E.,Davies, Ian W.
p. 4554 - 4557
(2008/02/04)

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 52-53

(2010/10/20)

AZOLECARBOXAMIDE HERBICIDES
Compounds of Formula (I), and their N-oxides and agriculturally suitable salts, are disclosed which are useful for controlling undesired vegetation, wherein J is (J-1), (J-2,(J-3), (J-4), (J-5), (J-6), (J-7), (J-8) and R1a, R1b, R1c, R2a, R2b, R3, R4, R05, T, U, W, Y and Z are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (I) and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula (I). Also disclosed are mixtures and compositions comprising a herbicidally effective amount of a compound of Formula (Iz) wherein J, R1a, R1b, R1c, R2a, R2b, R3, R4, R05, T, U, W, Y and Z are as defined in the disclosure; and an effective amount of another herbicide or herbicide safener. Also disclosed is a method for selectively controlling undesired vegetation in a crop that involves contacting the locus of a crop with an effective amount of a compound of Formula (Iz) and a effective amount of a safener.
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Page 37

(2010/02/06)

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)

peri-Substituted Imidazopyridines. A New Reductive Elimination Reaction
A new reductive elimination reaction of 3,5-disubstituted imidazopyridines (3) with hydrazine is reported.Thus on treatment of the 3,5-dibromo (7a), 5-bromo-3-nitro (7b), and 3,5-dinitro (4) derivatives with hydrazine hydrate in hot ethanol, the bromine and nitro groups are replaced by hydrogen.A mechanism based on the conjugated relationship of these peri-substituents is proposed and used to explain the reported conversion of 1,3,5-trichloro-2,4,6-trinitrobenzene (9) into 1,3-dichloro-4,6-dinitrobenzene (10).A variety of other 3-nitro-5-substituted imidazopyridines (15)-(18) is described, but these could not be cyclised to 1,2,4-triazacyclopentindenes.The 3-amino-5-methoxycarbonyl derivative (19a) cyclises to the triazacyclopentindenone (20) with sodium methoxide.
Rees, Charles W.,Smith, David I.
p. 1159 - 1164
(2007/10/02)

Certain insecticidal cyclopropane carboxylic acid derivatives
Novel esters in all possible isomeric forms or a mixture thereof having the formula STR1 wherein Y is selected from the group consisting of hydrogen, halogen, --OAlK and STR2 AlK is alkyl of 1 to 6 carbon atoms, n is 0, 1 or 2, Z is selected from the grou
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(2008/06/13)