- COVALENT TARGETING OF E3 LIGASES
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Disclosed herein, inter alia, are compositions and methods for targeting E3 ligases. In an aspect is a targeted protein degrader including 1) a targeted protein binder and 2) an E3 Ubiquitin ligase binder, wherein the E3 Ubiquitin ligase is human RNF4 or human RNF114. In an aspect is provided a pharmaceutical composition including a compound as described herein, including embodiments, and a pharmaceutically acceptable excipient.
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Paragraph 0591; 0600; 0700; 0720; 0816; 0837
(2020/05/19)
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- SPIROCYCLIC HAT INHIBITORS AND METHODS FOR THEIR USE
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Compounds having a structure of Formula (IX) or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b, R3a, R3b, R4a, R4b, Q1----Q2, R6, R7, A, B, W, x, and y are as defined herein and are provided. Pharmaceutical compositions comprising such compounds and methods for treating various HAT-related conditions or diseases, including cancer, by administration of such compounds are also provided.
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- Uracil derivatives, its preparation method and application thereof
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The invention relates to a uracil derivative shown as a general formula I, salt thereof acceptable in pharmacy, a solvate thereof and a solvate of the salt thereof acceptable in pharmacy. The invention also relates to a preparation method of the uracil derivative and an application thereof as a therapeutic agent, particularly a dipeptidyl peptidase-IV (DDP-IV) inhibitor.
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- Xanthine derivatives, their preparation and use
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The present invention relates to a xanthine derivative, a pharmaceutically acceptable salt thereof, a solvate of the derivative, a solvate of the pharmaceutically acceptable salt, a chemically protected form or prodrug thereof and a preparation method and a use thereof; and also relates to an intermediate compound used for preparing the xanthine derivative and a preparation method of the intermediate compound. The xanthine derivative and a pharmaceutical composition thereof effectively inhibit the activity of DPP-IV, and can be used for preparing a drug for diseases associated with dipeptidyl peptidase (DPP-IV).
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- Rapid photoassisted access to N,O,S-polyheterocycles with benzoazocine and hydroquinoline cores: Intramolecular cycloadditions of photogenerated azaxylylenes
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Ring the changes: A new photoassisted approach to give conformationally constrained N,O,S-polyheterocyclic scaffolds of unprecedented topologies was achieved by intramolecular [4+4] and [4+2] cycloadditions of photogenerated o-azaxylylenes (23 examples; see scheme). The precursors can be readily assembled by simple and high-yielding reactions, thus making this a powerful synthetic method amenable to high-throughput diversity-oriented synthesis.
- Mukhina, Olga A.,Bhuvan Kumar,Arisco, Teresa M.,Valiulin, Roman A.,Metzel, Greg A.,Kutateladze, Andrei G.
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p. 9423 - 9428
(2011/11/06)
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- 2,4-DI(AMINOPHENYL) PYRIMIDINES AS PLK INHIBITORS
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The invention relates to compounds of general formula (1), wherein A, W, X, Y, Z, Ra, Rb, Rc, R1, and R3 are defined as indicated in claim 1. Said compounds are used for the treatment of diseases characterized by excessive or anomalous cell proliferation. Also disclosed is the use of the inventive compounds for producing a medicament having said properties.
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Page/Page column 36-37
(2008/06/13)
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- A Convenient Synthesis of 7-Halo-1-indanones and 8-Halo-1-tetralones
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A regioselective oxidation of N-indan-4-yl-acetamide or N-(5,6,7,8-tetrahydronaphthalen-1-yl)acetamide with potassium permanganate followed by acidic hydrolysis gave 7-aminoindan-1-one or 8-aminotetral-1-one in good yield. The amino ketones were converted to the corresponding 7-haloindanone or the 8-halotetralone. Another method to prepare 7-haloindan-1-ones was completed by a cyclization of 3-chloro-1-(2-halophenyl)propan-1-one under Friedel-Crafts conditions to produce the product in gram quantity.
- Nguyen, Phong,Corpuz, Evelyn,Heidelbaugh, Todd M.,Chow, Ken,Garst, Michael E.
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p. 10195 - 10198
(2007/10/03)
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- 4-SUBSTITUTED IMIDAZOLE-2-THIONES AND IMIDAZOL- 2-ONES AS AGONISTS OF THE ALPHA- 2B AND ALPHA-2C ADRENERGIC RECEPTORS
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Compounds of Formula (I): where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardivascular and/or sedatory activity. These compounds of Formula (I) are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula (I) where X is O also have the advantageous property that they have no or only minimal cardivascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and/or sedatory activity.
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