- Discovery of GCC5694A: A potent and selective sodium glucose co-transporter 2 inhibitor for the treatment of type 2 diabetes
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Sodium-dependent glucose co-transporter 2 (SGLT2) has emerged as a promising drug target for the treatment of type 2 diabetes, and recently, several SGLT2 inhibitors have been approved for clinical use. A series of molecules with a C-aryl glucoside scaffo
- Kong, Young Kyu,Song, Kwang-Seop,Jung, Myung Eun,Kang, Misuk,Kim, Hyeon Jung,Kim, Min Ju
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supporting information
(2021/12/02)
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- Efficient synthesis of NIR emitting bis[2-(2′-hydroxylphenyl)benzoxazole] derivative and its potential for imaging applications
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Unassymetric bis[2-(2′-hydroxyphenylbenzoxole)] bis(HBO) derivatives with a DPA functionality for zinc binding have been developed with an efficient synthetic route, using the retrosynthetic analysis. Comparison of bis(HBO) derivatives with different substitution patterns allows us to verify and optimize their unique fluorescence properties. Upon binding zinc cation, bis(HBO) derivatives give a large fluorescence turn-on in both visible (λem ≈ 536 nm) and near-infrared (NIR) window (λem ≈ 746 nm). The probes are readily excitable by a 488 nm laser, making this series of compounds a suitable imaging tool for in vitro and in vivo study on a confocal microscope. The application of zinc binding-induced fluorescence turn-on is successfully demonstrated in cellular environments and thrombus imaging.
- Wang, Junfeng,Baumann, Hannah,Bi, Xiaoman,Shriver, Leah P.,Zhang, Zhaoda,Pang, Yi
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- METHOD FOR PRODUCING DIPHENYLMETHANE DERIVATIVE
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The present invention relates to an improved method for producing a diphenylmethane derivative which is effective as a sodium-dependent glucose cotransporter (SGLT) inhibitor, the method being carried out by means of a convergent synthesis method in which
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Paragraph 0259; 0260
(2019/06/14)
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- As a new polyphenylenepolymethylenepolyisocyanate deriv. SGLT2 inhibitor
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A compound with a diphenylmethane moiety having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney is disclosed. A pharmaceutical composition including the compound as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes is disclosed. A method for preparing the compound, and a method for preventing or treating metabolic disorders, particularly diabetes, by using the compound is provided.
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Paragraph 0235-0236
(2016/10/09)
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- CLASS OF NEAR INFRARED MOLECULAR PROBES FOR BIOLOGICAL APPLICATIONS
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Methods for preparing 2,5-Bis(benzoxazol-2′-yl)benzene-1,4-diol derivatives (Zinhbo derivatives) are provided. Zinhbo derivatives are used to detect zinc ions and have particular application in vivo and in vitro. Zinhbo derivatives upon excitation give a florescence response emission that can be used to determine the presence of zinc cation in solution. Zinhbo derivatives complexed with zinc cations upon excitation can produce a florescence response emission in the visible and near infrared range. Zinhbo derivatives complexed with zinc cations exhibit a large stoke shift between the excitation and emission wavelengths.
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Paragraph 0092
(2014/10/16)
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- QUINAZOLINES AND AZAQUINAZOLINES AS DUAL INHIBITORS OF RAS/RAF/MEK/ERK AND PI3K/AKT/PTEN/MTOR PATHWAYS
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The present application provides novel quinazolines and azaquinazolines and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in for co-regulating RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR pathways by administering a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, T and R4, and R6 to R8' are defined herein, to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR pathways. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment/ the disease is cancer.
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- A versatile synthesis of bis[2-(2'-hydroxylphenyl)benzoxazole] derivatives as zinc sensors
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A versatile synthetic route has been developed to prepare 2, 5-bis(benzoxazole-2-yl)benzene-1,4-diol derivatives 2. Although one of the derivatives (2b) has recently been shown to exhibit an excellent response to Zn2+ cations, the low yielding synthetic route will likely prevent its wide application. This report describes an improved synthetic procedure to obtain 2, thereby making this class of compounds available for biologically relevant studies. An effective synthesis has been developed for 2-aminophenol derivative 6, which bears a carboxylate group in the desired position. The strategy allows construction of bis(benzoxazole) compound 5, where the built-in ester group can be easily converted to either a hydroxymethyl or a bromomethyl group to introduce the zinc-chelating ligand. The Royal Society of Chemistry 2013.
- Wang, Junfeng,Pang, Yi
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p. 10208 - 10212
(2013/09/02)
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- Efficient synthesis and 5-LOX/COX-inhibitory activity of some 3-hydroxybenzo[b]thiophene-2-carboxylic acid derivatives
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A series of 3-hydroxybenzo[b]thiophene-2-carboxylic acid derivatives has been prepared and subsequently evaluated with regards to the inhibition of 5-LOX/COX. Structure optimization furnished derivatives with promising in vitro activity as dual 5-LOX/COX inhibitors with submicromolar IC50 values for inhibition of 5-LOX and COX-1, respectively.
- Hansen, Finn K.,Khankischpur, Mehdi,Tolaymat, Ibrahim,Mesaros, Renata,Dannhardt, Gerd,Geffken, Detlef
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scheme or table
p. 5031 - 5034
(2012/08/28)
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- NOVEL 4-OXOQUINOLINE COMPOUND AND USE THEREOF AS HIV INTEGRASE INHIBITOR
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Provision of a compound having an anti-HIV activity, particularly an integrase inhibitory activity.A 4-oxoquinoline compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof: wherein each symbol is as defined in the specification.The present invention also relates to a pharmaceutical composition containing the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier; an integrase inhibitor, an antiviral agent, anti-HIV agent and the like, which contains the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof as an active ingredient; an anti-HIV composition containing the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof, and one or more other kinds of anti-HIV activity substances as active ingredients; an anti-HIV agent containing the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof as an active ingredient, which is used for a multiple drug therapy with other anti-HIV agent(s), and the like.
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Page/Page column 121
(2008/06/13)
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- 4-OXOQUINOLINE COMPOUNDS AND UTILIZATION THEREOF AS HIV INTEGRASE INHIBITORS
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An anti-HIV agent containing, as an active ingredient, a 4-oxoquinoline compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. The compound of the present invention has HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compound can become a more effective anti-HIV agent. Since the compound has high inhibitory activity specific for integrases, it can provide a safe pharmaceutical agent with a fewer side effects for human.
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Page/Page column 64
(2008/06/13)
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