- Facile synthesis of functionalized 4-aminopyridines
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The title compounds are readily available by ring transformation of nitropyrimidinone with active methylene compounds in the presence of ammonium acetate.
- Nishiwaki, Nagatoshi,Azuma, Mayumi,Tamura, Mina,Hori, Kazushige,Tohda, Yasuo,Ariga, Masahiro
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Read Online
- High-yield synthesis method of methyl 4-aminonicotinate
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The invention discloses a high-yield synthesis method of methyl 4-aminonicotinate, which comprises the following steps: by taking 3, 4-dipicolinic acid as a raw material, carrying out intramolecular dehydration substitution, ammonia ammonification, improved NBS Hofmann rearrangement and hydrolysis to obtain the methyl 4-aminonicotinate. The synthesis method disclosed by the invention is simpler to operate, mild in reaction condition and higher in total yield, and has an extremely high application value.
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Paragraph 0024; 0030-0033; 0039-0042; 0048-0050
(2021/09/08)
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- PYRIDOPYRIMIDINES AND METHODS OF THEIR USE
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Disclosed are compounds useful in the treatment of neurological disorders. The compounds described herein, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological diseases.
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Page/Page column 83
(2021/12/28)
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- POLY-ADP RIBOSE POLYMERASE (PARP) INHIBITORS
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The present invention is related to a pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and a compound represented by the following structural formula: The present invention is also related a method of treating a subject with a disease which can be ameliorated by inhibition of poly(ADP-ribose)polymerase (PARP). The definitions of the variables are provided herein.
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Page/Page column 98; 99
(2018/07/29)
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- Novel Aryl-Modified Benzoylamino-N-(5,6-dimethoxy-1H-benzoimidazol-2-yl)-heteroamides as Potent Inhibitors of Vascular Endothelial Growth Factor Receptors 1 and 2
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Tumor angiogenesis has become an important target for antitumor therapy, with most current therapies aimed at blocking the vascular endothelial growth factor (VEGF) pathway. The VEGF and its receptors have been implicated as key factors in tumor angiogenesis and are major targets in cancer therapy. A series of aryl-modified benzoylamino-N-(5,6-dimethoxy-1H-benzoimidazol-2-yl)-heteroamides were synthesized from 2-amino-5,6-dimethoxy benzimidazole and aryl-substituted benzoylamino hetero acids. The new compounds were tested for inhibition of VEGF receptors I and II (VEGFR-1 and VEGFR-2). Compound 6e displayed VEGFR-2 inhibitory activity with a 50% inhibition concentration value as low as 0.020 μM in a homogeneous time-resolved fluorescence enzymatic assay. VEGFR-2 active compounds display good activity against VEGFR-1 as well.
- Ashok, Abhishek,Thanukrishnan, Kannan,Bhojya Naik, Halehatty S.,Maridu, Rajendraswami
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p. 1949 - 1956
(2017/05/29)
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- Azaindole synthesis through dual activation catalysis with N-heterocyclic carbenes
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A convergent, transition-metal-free synthesis of 2-aryl-azaindoles has been developed. The interception of a reactive aza-ortho-azaquinone methide intermediate by an acyl anion equivalent generated through carbene catalysis provides high yields, a wide substrate scope, and the synthesis of previously inaccessible azaindoles.
- Sharma, Hayden A.,Todd Hovey,Scheidt, Karl A.
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supporting information
p. 9283 - 9286
(2016/07/25)
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- COMPOUNDS AND METHODS OF USE
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This disclosure provides compounds and compositions and methods of using those compounds and compositions to treat diseases and disorders associated with excessive transforming growth factor-beta (TGFβ) activity. This disclosure also provides methods of using the compounds in combination with one or more cancer immunotherapies.
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Paragraph 0183
(2015/07/16)
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- PYRROL-1 -YL BENZOIC ACID DERIVATES USEFUL AS MYC INHIBITORS
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The present invention provides compounds of Formula (I-A), (I-B), and (I-C), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting Myc (e.g., c-Myc) activity. The p
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Paragraph 00323
(2014/05/24)
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- Iminooxazolidine Derivatives and Their Use
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The present application relates to novel iminooxazolidine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular thromboembolic disorders.
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Page/Page column 17
(2010/02/16)
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- Nicotinic acid adenine dinucleotide phosphate analogues containing substituted nicotinic acid: Effect of modification on Ca2+ release
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Analogues of nicotinic acid adenine dinucleotide phosphate (NAADP) with substitution at either the 4- or the 5-position position of the nicotinic acid moiety have been synthesized from NADP enzymatically using Aplysia californica ADP-ribosyl cyclase or mammalian NAD glycohydrolase. Substitution at the 4-position of the nicotinic acid resulted in the loss of agonist potency for release of Ca2+-ions from sea urchin egg homogenates and in potency for competition ligand binding assays using [32P]NAADP. In contrast, several 5-substituted NAADP derivatives showed high potency for binding and full agonist activity for Ca2+ release. 5-Azido-NAADP was shown to release calcium from sea urchin egg homogenates at low concentration and to compete with [32P]NAADP in a competition ligand binding assay with an IC50 of 18 nM, indicating that this compound might be a potential photoprobe useful for specific labeling and identification of the NAADP receptor.
- Jain, Pooja,Slama, James T.,Perez-Haddock, Leroy A.,Walseth, Timothy F.
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experimental part
p. 7599 - 7612
(2011/02/22)
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- ANTITHROMBOTIC AROMATIC ETHERS
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This application relates to a compound of formula (I) (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor.
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Page/Page column 107
(2008/06/13)
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- COMPOUNDS, COMPOSITIONS, AND METHODS
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Compounds, compositions and methods useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
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- HETEROAROMATIC AMIDES AS INHIBITOR OF FACTOR XA
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This application relates to heteroaromatic amides (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
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- Syntheses of ortho-hydroxymethylpyridinols and dioxaphosphorino[m,n-x]pyridines
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Dioxaphosphorino[m,n-x]pyridines compounds have been prepared by condensation of methyl dichlorophosphate with new ortho-hydroxymethylpyridinols.
- Leroy,Despres,Bigan,Blondeau
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p. 2257 - 2272
(2007/10/03)
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- STUDY OF AMINO-IMINO TAUTOMERISM IN DERIVATIVES OF 2-, 4- AND 6-AMINONICOTINIC ACID
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13C NMR spectra of p-nitrobenzoyl 2-, 4-, and 6-aminopyridine-3-carboxylates, their hydrochlorides, trifluoroacetates and 1-benzyl derivatives were studied.As found from the chemical shifts of pyridine carbon atoms C-2, C-4 and C-6, the free bases exist i
- Snrckova, Stavata,Juricova, Kristina,Prutianov, Viktor
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p. 2057 - 2068
(2007/10/02)
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