- RESORCINOL DERIVATIVE AS HSP90 INHIBITOR
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The present invention relates to a compound represented by formula (I) of a resorcinol derivative as an HSP90 inhibitor or pharmaceutically accepted salts thereof. The compound in the present invention has the activity of inhibiting heat shock protein HSP90. Therefore, the compound in the present invention is used to treat proliferative diseases such as cancer and neurodegenerative diseases. The present invention further provides the compounds and preparation methods for pharmaceutical compositions comprising the compounds, a method for treating diseases, and pharmaceutical compositions comprising the compounds.
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- Silver(I)-catalyzed iodination of arenes: Tuning the lewis acidity of N-iodosuccinimide activation
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A mild and rapid method for the iodination of arenes that utilizes silver(I) triflimide as a catalyst for activation of N-iodosuccinimide has been developed. The transformation was found to be general for a wide range of anisole, aniline, acetanilide, and phenol derivatives and allowed the late-stage iodination of biologically active compounds such as PIMBA, a SPECT imaging agent of breast cancer, and (a?)-IBZM, a dopamine D2 receptor antagonist. The method was also modified for the radioiodination of arenes using a one-pot procedure involving the in situ generation of [125I]-N-iodosuccinimide followed by the silver(I)-catalyzed iodination.
- Racys, Daugirdas T.,Sharif, Salaheddin A. I.,Pimlott, Sally L.,Sutherland, Andrew
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p. 772 - 780
(2016/02/18)
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- Highly Regioselective Iodination of Arenes via Iron(III)-Catalyzed Activation of N-Iodosuccinimide
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An iron(III)-catalyzed method for the rapid and highly regioselective iodination of arenes has been developed. Use of the powerful Lewis acid, iron(III) triflimide, generated in situ from iron(III) chloride and a readily available triflimide-based ionic liquid allowed activation of N-iodosuccinimide (NIS) and efficient iodination under mild conditions of a wide range of substrates including biologically active compounds and molecular imaging agents.
- Racys, Daugirdas T.,Warrilow, Catherine E.,Pimlott, Sally L.,Sutherland, Andrew
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supporting information
p. 4782 - 4785
(2015/10/12)
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- Mild arming and derivatization of natural products via an In(OTf) 3-catalyzed arene iodination
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Figure presented Iodination of arene-containing natural products employing N-iodosuccinimide catalyzed by In(OTf)3 at ambient temperature is reported as a versatile and mild method for natural product derivatization amenable to small scale. This process facilitates natural product derivatization of arene moieties for SAR studies, homo- and heterodimerization of natural products, and also conjugation with reporters such as biotin via subsequent metal-mediated coupling reactions.
- Zhou, Cong-Ying,Li, Jing,Peddibhotla, Satyamaheshwar,Romo, Daniel
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supporting information; experimental part
p. 2104 - 2107
(2010/09/15)
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- BICYCLO-SUBSTITUTED PYRAZOLON AZO DERIVATIVES, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF
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The bicyclo-substituted pyrazolon-azo derivatives of formula (I) or pharmaceutical acceptable salts, hydrates or solvates thereof, methods for their preparation, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics and their use as agonists of thrombopoietin receptor are disclosed. The definition of substituents in formula (I) are the same as defined in the description.
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Page/Page column 81
(2010/10/19)
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- Amino-5-(5-membered)hetero-arylimidazolone compounds and the use thereof for beta-secretase modulation
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The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles
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Page/Page column 42-43
(2008/06/13)
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- The regioselective synthesis of aryl pyrroles
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Pyrrole is a unique aromatic molecule as it can readily undergo substitution at all five positions but obtaining the desired regioisomer can prove difficult to control. We now report our results on the regioselective arylation of pyrrole, utilizing select
- Smith, Jason A.,Ng, Sarah,White, Jonathon
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p. 2477 - 2482
(2008/03/11)
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- PYRROLE COMPOUNDS AS INHIBITORS OF ERK PROTEIN KINASE, SYNTHESIS THEREOF AND INTERMEDIATES THERETO
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The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
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Paragraph 0089
(2010/02/14)
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- Polyaromatic propynyl compounds and pharmaceutical/cosmetic compositions comprised thereof
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Novel pharmaceutically/cosmetically-active polyaromatic propynyl compounds have the structural formula (1): STR1 in which X is one of the radicals: STR2 and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
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- Polycyclic aromatic compounds and pharmaceutical/cosmetic compositions comprised thereof
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Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds have the structural formula (I): STR1 wherein Ar is a radical having one of the formulae (a)-(i): STR2 and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
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- A bridged porphyrinato(thiolato)iron(III) complex as a model of the active center of the cytochrome P-450 isozyme
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Protection by shielding-the porphyrinophane complex 1, a functionally active model compound of the cytochrome P-450 isozyme, was prepared in an 18-step convergent synthesis. Porphyrin complex 1 catalyzes the epoxidation of cis-stilbene with iodosylbenzene
- Volz,Holzbecher
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p. 1442 - 1445
(2007/10/03)
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