- Conversion of Aldehydes to Branched or Linear Ketones via Regiodivergent Rhodium-Catalyzed Vinyl Bromide Reductive Coupling-Redox Isomerization Mediated by Formate
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A regiodivergent catalytic method for direct conversion of aldehydes to branched or linear alkyl ketones is described. Rhodium complexes modified by PtBu2Me catalyze formate-mediated aldehyde-vinyl bromide reductive coupling-redox isomerization to form branched ketones. Use of the less strongly coordinating ligand, PPh3, promotes vinyl-to allylrhodium isomerization en route to linear ketones. This method bypasses the 3-step sequence often used to convert aldehydes to ketones involving the addition of pre-metalated reagents to Weinreb or morpholine amides.
- Swyka, Robert A.,Shuler, William G.,Spinello, Brian J.,Zhang, Wandi,Lan, Chunling,Krische, Michael J.
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supporting information
p. 6864 - 6868
(2019/05/10)
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- Amide derivatives, and preparation method and application thereof to medicines
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The invention relates to amide derivatives, and a preparation method and application thereof to medicines. Specifically, the invention relates to amide derivatives shown as a general formula (I), a preparation method thereof, pharmaceutical salts thereof and application of the amide derivatives and pharmaceutical salts thereof as therapeutic agents, especially as pancreatic hyperglycemia receptor antagonists. The substituted groups in the general formula (I) are defined as in the description.
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Paragraph 0138; 0143; 0144; 0145; 0146
(2017/10/22)
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- COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES
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The invention relates to certain compounds or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders
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Paragraph 00109
(2013/05/21)
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- QUINOLINYL GLUCAGON RECEPTOR MODULATORS
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The present invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, A2, A3, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
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- GLUCAGON RECEPTOR MODULATORS
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The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
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Page/Page column 20
(2012/08/27)
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- AMINOPHENYLPROPANOIC ACID DERIVATIVE
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A compound represented by the formula (1): wherein each symbol is as defined in the specification, and a salt thereof and a prodrug thereof unexpectedly have superior GPR40 receptor agonist activity, superior in the properties as a pharmaceutical product such as stability and the like, and can be a safe and useful pharmaceutical agent as a drug for the prophylaxis or treatment of GPR40 receptor related pathology or diseases such as diabetes and the like.
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- PHENYLPROPANOIC ACID DERIVATIVES
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The present invention provides a novel compound having a GPR40 receptor function modulating action, which is useful as an insulin secretagogue, a drug for the prophylaxis or treatment of diabetes and the like. A compound represented by the formula (I) wherein each symbol is as defined in the specification, a salt thereof and a prodrug thereof have unexpectedly superior GPR40 receptor agonist activity and also show superior properties as a pharmaceutical product, such as stability and the like. Thus, they can be safe and useful drugs for the prophylaxis or treatment of GPR40 receptor related conditions or diseases in mammals.
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Page/Page column 48-49
(2008/06/13)
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- GLUCAGON RECEPTOR ANTAGONISTS, PREPARATION AND THERAPEUTIC USES
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The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.
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