- NAPTHOQUINONES, PRO-DRUGS, AND METHODS OF USE THEREOF
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Provided herein are naphthoquinones compounds such as those with a hydrogen bond donating group of the formula (I): wherein: R1, R2, R3, R4, R5, and n are as defined herein. Also provided herein are pharmaceutical composition of the present compounds and methods of treatment using the compounds including their use in the treatment of cancer.
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Paragraph 00139
(2017/07/06)
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- THERAPEUTIC COMPOUNDS
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The invention provides compounds of formula (I): wherein, A, C, D, X, and Y have any of the values defined in the specification, and salts thereof. The compounds are SIRT2 inhibitors and are useful for treating SIRT2 associated conditions.
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Paragraph 0264; 0265; 0316
(2017/01/23)
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- Tricyclic [1,2,4]triazine 1,4-dioxides as hypoxia selective cytotoxins
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A series of novel tricyclic triazine-di-N-oxides (TTOs) related to tirapazamine have been designed and prepared. A wide range of structural arrangements with cycloalkyl, oxygen-, and nitrogen-containing saturated rings fused to the triazine core, coupled with various side chains linked to either hemisphere, resulted in TTO analogues that displayed hypoxia-selective cytotoxicity in vitro. Optimal rates of hypoxic metabolism and tissue diffusion coefficients were achieved with fused cycloalkyl rings in combination with both the 3-aminoalkyl or 3-alkyl substituents linked to weakly basic soluble amines. The selection was further refined using pharmacokinetic/pharmacodynamic model predictions of the in vivo hypoxic potency (AUCreq) and selectivity (HCD) with 12 TTO analogues predicted to be active in vivo, subject to the achievement of adequate plasma pharmacokinetics.
- Hay, Michael P.,Hicks, Kevin O.,Pchalek, Karin,Lee, Ho H.,Blaser, Adrian,Pruijn, Frederik B.,Anderson, Robert F.,Shinde, Sujata S.,Wilson, William R.,Denny, William A.
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supporting information; experimental part
p. 6853 - 6865
(2009/12/03)
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- TRICYCLIC 1,2,4-TRIAZINE OXIDES AND COMPOSITIONS THEREFROM FOR THERAPEUTIC USE IN CANCER TREATMENTS
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The invention relates to novel tricyclic 1,2,4-triazine-1-oxides and novel tricyclic 1,2,4-triazine-1,4-dioxides of formula: (I); and to related analogues, to their preparation, and to their use as hypoxia-selective drugs and radiosensitizers for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.
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Page/Page column 126
(2008/06/13)
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- Process for the preparation of 5-nitro-3,4-dihydro-1(2H)-naphthalenone, 1,5-naphthalendiamine and 1,5-naphthalendiisocyanate
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A process for the production of 1,5-naphthalene diamine (I) comprises reaction of 4-(2-nitrophenyl)-n-butyronitrile to 4-(2-nitrophenyl)-n-butyric acid. Independent claims are included for: (1) a process for the production of 5-nitro-3,4-dihydro-1(2H)-naphthalinone by reaction of 4-(2-nitrophenyl)-n-butyronitrile to 4-(2-nitrophenyl)-n-butyric acid and; (2) a process for the production of 1,5-naphthalene diisocyanate by phosgenation of 1,5-naphthalene diamine (I).
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- Process for preparation of 1,5-diaminonaphthalenes
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In a process where an ortho-alkylnitrobenzene derivative and a vinyl compound as starting materials are used to prepare a 1,5-diaminonaphthalene derivative via a 4-(2-nitrobenzene)propane derivative and a 5-nitro-1-tetralone derivative, the ortho-alkylnit
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- Process for the production of 1,5-naphthalenediamine
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The invention relates to a process for the production of 1,5-naphthalenediamine and to the intermediates 4-(2-nitrophenyl)butyronitrile, 5-nitro-3,4-dihydro-1(2H)-naphthyl-imine, 5-nitroso-1-naphthylamine, 5-nitro-1-naphthylamine, 4-(2-aminophenyl)-butyronitrile, 5-amino-3,4-dihydro-1(2H)-naphthalene imine, 4-(2-nitrophenyl)ethyl butyrate and 4-(2-nitrophenyl)butyramide obtainable during the process.
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- 4-(5-isothiocyanato-1,2,3,4-tetrahydro-1-naphthyl)-1H-imidazole: An imidazole-type affinity label for the α1-adrenergic receptor
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Based on the conformationally restricted analog 5 of medetomidine (4), a prototypic compound of the novel imidazole class of (α2-adrenergic receptor (AR) agonists, compound 6 was prepared and evaluated at human platelet (α2-AR and ra
- Zheng,Jing,Patil,Lei,Feller,Miller
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p. 318 - 327
(2007/10/03)
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- Chirochromism-photochromism by epimerization: Search for a liquid crystal phototrigger
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A new class of photochromic reactions was investigated as a possible trigger for phase transitions in liquid crystals. Chirochromic compounds have two chiral units. One unit is fixed, and the other can be switched with light. A series of diastereomeric co
- Zhang, Mingbao,Schuster, Gary B.
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p. 4852 - 4857
(2007/10/02)
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- Synthesis and Evaluation of N,N-Di-n-propyltetrahydrobenzindol-7-amine and Related Congeners as Dopaminergic Agonists
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An evaluation of 6-indole (4), its rigid analogue N,N-di-n-propyl-5,6,7,8-tetrahydrobenzindol-7-amine (5), and some related congeners, for ability to suppress serum prolactin in reserpinized rats, revealed modest biological a
- Nichols, David E.,Cassady, John M.,Persons, Paul E.,Yeung, Ming C.,Clemens, James A.,Smalstig, E. Barry
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p. 2128 - 2134
(2007/10/02)
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- Nitrodienamines: An Easy Synthesis and Cycloaddition Reactions with α,β-Unsaturated Carbonyl Compounds and Quinones
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The nitrodienamine 6 was synthesized through the vinamidinium salt 7.The reactivity of 6 was investigated with the α,β-unsaturated carbonyls and styrene 8-14, and the quinones 15, 16, 25, 29, 31, 33, 37, and 41.Keywords: nitrodienamine; synthesis; cycloaddition; α,β-unsaturated carbonyl; quinone; vinamidinium salt
- Takeuchi, Naoki,Ohki, Junji,Tobinaga, Seisho
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p. 481 - 487
(2007/10/02)
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- Monoquaternary neuromuscular blocking agents based on 1 tetralone and 1 indanone
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The preparation of three isomeric 1 tetralone hydrazones and three isomeric 1 indanone hydrazones possessing a single quaternary ammonium center is described. Several of the compounds possessed significant neuromuscular blocking activity, and two approached suxamethonium in potency. 1H NMR evidence obtained from a study of the N,N dimethylhydrazones indicated that the hydrazones adopted an E configuration in solution.
- Biggs,Casy,Chu,Coutts
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p. 472 - 475
(2007/10/06)
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