26893-72-1Relevant academic research and scientific papers
Cation-halide transport through peptide pores containing aminopicolinic acid
Basak, Debajyoti,Sridhar, Sucheta,Bera, Amal K.,Madhavan, Nandita
, p. 4712 - 4717 (2016)
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.
NOVEL COMPOUND, ORGANIC CATION TRANSPORTER 3 DETECTION AGENT, AND ORGANIC CATION TRANSPORTER 3 ACTIVITY INHIBITOR
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Paragraph 0543-0544; 0546, (2016/08/17)
[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)
GAMMA SECRETASE MODULATORS
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Page/Page column 61, (2011/08/08)
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.
GAMMA SECRETASE MODULATERS
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Page/Page column 129, (2011/08/21)
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.
HETEROARYL SUBSTITUTED PIPERIDINES
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Page/Page column 45, (2011/09/14)
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.
PIPERIDINE DERIVATIVES
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Page/Page column 91, (2011/09/19)
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
Metallo-controlled dynamic molecular tweezers: Design, synthesis, and self-assembly by metal-ion coordination
Ulrich, Sebastien,Petitjean, Anne,Lehn, Jean-Marie
scheme or table, p. 1913 - 1928 (2011/01/10)
The introduction of controllable dynamic features into synthetic receptors represents a step towards "smart" adaptive nanodevices. We report herein our studies on the construction of dynamic molecular tweezers in which the binding of a substrate is allost
Synthesis and crystallographic analysis of short pyridine-based oligoamides as DNA-targeting supramolecular binders
Frimannsson, Daniel O.,McCabe, Thomas,Schmitt, Wolfgang,Lawler, Mark,Gunnlaugsson, Thorfinnur
scheme or table, p. 483 - 490 (2010/11/18)
In this study, the synthesis of the pyridine peptides 1-4, formed from amino-picolinic acid, and pyridine peptide 5, made from coupling of a mono-protected pyridine diamine to a mono-protected pyridine dicarboxylic acid and the X-ray crystallographic structures of 1 and 5 are discussed, along with their supramolecular interactions in the solid state. The structure of these compounds showed that they possess concave appearance which can be employed to bind to nucleic acids through multiple hydrogen bonding, which would facilitate the formation of helical-based pyridine oligoamides as novel DNA-binding molecules. This was proven by carrying out DNA denaturation studies and ethidium displacement assay on 5, but, by using MTT assays, 5 was shown to be cytotoxic against drug-resistant chronic myeloid leukaemia K562 cell-line.
5-Quinoline derivatives having an anti-bacterial activity
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Page/Page column 10, (2010/12/31)
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.
BENZISOXAZOLE COMPOUND
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Page/Page column 153; 154, (2009/02/10)
Disclosed is a compound represented by the general formula (I) or a salt thereof: wherein any one of R1, R2 and R3 represents a group represented by the formula: -(CH2)m-NR11R12 (wherein m is 1 or 2; and R11 and R12 independently represent a hydrogen atom or a C1-6 alkyl group or may, together with a nitrogen atom to which R11 and R12 are bound, form a 4- or 5-membered cyclic group); the remaining two or R1, R2 and R3 independently represent a group represented by the formula: -(O)n-R21 (wherein n is 0 or 1; and R21 represents a hydrogen atom, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, or the like); and R4 represents a C1-6 alkyl group which may have a substituent or the like.
