86823-81-6Relevant articles and documents
DISUBSTITUTED 3,4-DIAMINO-3-CYCLOBUTENE-1,2-DIONE COMPOUNDS FOR USE IN THE TREATMENT OF CHEMOKINE-MEDIATED PATHOLOGIES
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Paragraph 0179; 0180, (2014/10/29)
Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds are disclosed that are represented by general formula (I). Also disclosed, are pharmaceutical compositions including these compounds and methods of using these compounds and compositions for the
Synthesis of benzothiophenones and naphthothiophenone as anticholinesterases
Jung
, p. 5325 - 5327 (2013/07/26)
Since AChE and BuChE belong to the same serine hydrolazes, we designed and synthesized compounds 1-6 as anticholinesterases and measured their inhibition poteucies on ChEs. 7-Methoxy-3H-benzo[c]thiophen-1-one 4, 4,6-dibromo-5,7- methoxy-3H-benzo[c]thiophe
Method of inhibiting protein tyrosine phosphatase 1B and/or T-cell protein tyrosine phosphatase 4 and/or other PTPases with an Asp residue at position 48
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Page/Page column 134-135, (2010/11/23)
The present invention provides a method of inhibiting a member of a family of Protein Tyrosine Phosphatases (PTPases, PTPs) such as PTP1B, TC-PTP, CD45, SHP-1, SHP-2, PTPα, PTPε, PTPμ, PTPδ, PTPσ, PTPζ, PTPβ, PTPD1, PTPD2, PTPH1, PTP-MEG1, PTP-LAR, and HePTP by exposing said Ptpase member by administration to a host or otherwise to at least one compound with certain structural, physical and spatial characteristics that allow for the interaction of said compound with specific residues of the active site of PTP1B and/or TC-PTP. These compounds are indicated in the management or treatment of a broad range of diseases such as autoimmune diseases, acute and chronic inflammation, osteoporosis, various forms of cancer and malignant diseases, and type I diabetes and type II diabetes, as well as in the isolation of PTPases and in elucidation or further elucidation of their biological function.
The total synthesis of coleophomones B, C, and D
Nicolaou,Montagnon, Tamsyn,Vassilikogiannakis, Georgios,Mathison, Casey J. N.
, p. 8872 - 8888 (2007/10/03)
Members of the coleophomone family of natural products all possess several intriguing and challenging architectural features, as well as exhibit unusual biological activity. They, therefore, constitute attractive targets for synthesis. In this Article, we describe the total synthesis of coleophomones B (2), C (3), and D (4). The highly strained and congested 11-membered macrocycle of coleophomones B (2) and C (3) was constructed using an impressive olefin metathesis reaction. Furthermore, both of the requisite geometric isomers of the Δ within the macrocycle could be accessed from a common precursor, facilitating a divergence that lent the coleophomone B (2)/C (3) synthesis an unusually high degree of efficiency. The synthesis of coleophomone D (4) confirmed that it exists as a dynamic mixture of isomeric forms with a different aromatic substitution pattern from the other family members.
Protoberberines from Reissert-Compounds VIII [1]. Oxazoloisoquinolines, New and Efficient Educts for the Synthesis of 8-Oxoprotoberberines
Reimann, Eberhard,Grasberger, Fritz,Polborn, Kurt
, p. 991 - 1014 (2007/10/03)
Certain benzylated oxazoloisoquinolinones readily available from Reissert compounds provided an efficient access to 8-oxoprotoberberines in three steps. A series of these new precursors as well as several oxoprotoberberines were prepared and the scope and limitation of this procedure were investigated.
Modulators of protein tyrosine phosphateses (PTPases)
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, (2008/06/13)
Disclosed are novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds of Formula 1 are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) including PTP1B, T cell PTP, wherein n, m, X, R1, R2, R3, R4, R5, R6, and R7are defined more fully in the description. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, and other diseases.
Synthesis of Dibenzoquinolizines - A New Entry to Protoberberines
Reimann, Eberhard,Benend, Helmut
, p. 939 - 948 (2007/10/02)
A novel synthesis to prepare dibenzo-8-quinolizinones 8 is reported using the intramolecular cyclisation of the benzylated Reissert compounds 6 for the key step.Methylation of 8 by methyllithium gives partial deoxygenated coralynes 10 which in turn can be reduced by NaBH4 yielding the 8-methyltetrahydro-protoberberines 11.The structures are assigned by NMR-spectroscopy. Keywords.Reissert compounds; Intramolecular cyclisation; Dibenzo-8-quinolizinones; Deoxygenated coralynes; 8-Methyltetrahydro-protoberberines.
Efficient total synthesis of AI-77-B, a gastroprotective substance from Bacillus pumilus AI-77
Hamada,Hara,Kawai,Kohno,Shioiri
, p. 8635 - 8652 (2007/10/02)
First total synthesis of AI-77-B (1), a gastroprotective substance from Bacillus pumilus AI-77, was achieved in a stereoselective and convergent manner. In this synthesis, the dihydroisocoumarin part 2 was constructed in one step through 1,2-addition of the benzylic anion 17b to Boc-L-leucinal 7b. The hydroxy amino acid 4 was elaborated from (R)-glutamic acid in a highly stereoselective manner. Condensation of 2·HCl and 4, intramolecular Pinner reaction, followed by mild hydrolysis afforded AI-77-B (1).
