- Synthesis and antiproliferatory activity of ruthenium complexes containing N-heterocyclic carboxylates
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Solvates of the complexes Ru2Cl(pic)4(EtOH) (2), Ru(Im-CO2)3 (3), and Ru(Im-CO2)(Im-CO2H)Cl2 (4), were synthesized from reaction of RuCl3·3H2O or K3[RuCl6] with the N-heterocyclic carboxylic acids pyridine-2-carboxylic acid (picolinic acid, Hpic), and imidazole-4-carboxylic acid (Im-CO2H). Crystals of 2–4 could not be grown and hence characterization was done by elemental analysis, NMR, IR, and conductivity data; 2 and 4 were tested for antiproliferatory activity in vitro against a human breast cancer cell line, but were less active than, for example, Ru complexes containing bis-imidazole or 4,4′-biimidazole that we studied previously [see Can. J. Chem. 89 (2011) 948]. Preliminary work with a third potential ligand, 3-nitro-1,2,4-triazole-5-carboxylic acid (abbreviated HCANT), and other nitro heterocyclic compounds is also presented.
- Kennedy, David C.,James, Brian R.
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Read Online
- IRAK DEGRADERS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same.
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Paragraph 2699; 2700
(2019/07/10)
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- Tripterine imidazole derivative as well as preparation method and application thereof
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The invention discloses a novel tripterine imidazole derivative as well as a preparation method and application thereof, and belongs to the field of biomedicine. The tripterine imidazole derivative has a structure shown as a formula I as shown in the specification, wherein R1, R2 and R3 are respectively selected from H, alkyl, hetero-atomic alkyl, halogen or nitryl; and X is selected from a saturated or unsaturated linear aliphatic hydrocarbon fragment containing 3-6 carbon atoms. The novel tripterine imidazole derivative as well as the preparation method and the application thereof disclosedby the invention have the benefits that the preparation method of the compound is mild in reaction conditions; a used reagent is low in toxicity, raw materials are easy to obtain, the post-treatment is convenient, and the yield is relatively high. Pharmacological experiment studies shows that the compound has excellent anti-tumor activity and can be applied to the preparation of an anti-tumor drug.
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Paragraph 0291; 0292; 0293; 0294
(2019/02/27)
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- Intermediate for preparing medetomidine and its preparation method and use
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The invention provides an intermediate for preparing medetomidine. The intermediate is a compound shown in the formula (I). The invention also provides a preparation method of the intermediate, and ause of the intermediate in the preparation of medetomidine. The compound shown in the formula (I) is used for preparation of medetomidine so that the raw material is cheap and easy to obtain, synthesis processes are simple, the reaction cycle is short, the environmental pollution is avoided, operation is simple, the harsh reaction conditions are avoided, the operation and post-treatment are simple, the yield and the product purity are high, the intermediate in each step is a solid and is easy to purify, a production cost is low, and the intermediate is suitable for industrial large-scale production and conforms to the principle of green chemistry.
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Paragraph 0086-0088
(2018/08/03)
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- PDE9 INHIBITORS FOR TREATMENT OF PERIPHERAL DISEASES
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The present invention relates to PDE9 inhibitors, their synthesis, and their use for treatment of benign prostate hyperplasia, beta thalassemia, and sickle cell disease.
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Paragraph 00195; 00248-00249
(2018/09/25)
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- PDE9 INHIBITORS WITH IMIDAZO TRIAZINONE BACKBONE AND IMIDAZO PYRAZINONE BACKBONE FOR TREATMENT OF PERIPHERAL DISEASES
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The present invention relates to PDE9 inhibitors and their use for treatment of benign prostate hyperplasia and sickle cell disease.
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Page/Page column 40
(2017/02/09)
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- An efficient one-pot oxidative esterification of aldehydes to carboxylic esters using B(C6F5)3-TBHP
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A simple and efficient protocol for oxidative esterification of diverse aldehydes with alcohols was accomplished with tert-butyl hydroperoxide and 1 mol % of tris(pentafluorophenyl)borane [B(C6F5)3] to generate the corresponding esters in good to excellent yields. The present protocol represents compatibility with wide range of functional groups as well as exceptional tolerance toward acid labile protecting groups such as TBDPS, TBDMS, acetonide, and Boc.
- Guggilapu, Sravanthi Devi,Prajapti, Santosh Kumar,Babu, Bathini Nagendra
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supporting information
p. 889 - 892
(2015/02/05)
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- ANDROGEN RECEPTOR MODULATING CARBOXAMIDES
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Compounds of formula (I) or (II) wherein Rx, Rz, R9, R10, R14, R14′, R15, R15′, A and B are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds possess utility as tissue-selective androgen receptor modulators (SARM) and are useful as medicaments in the treatment of prostate cancer and other AR dependent conditions and diseases where AR antagonism is desired.
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Page/Page column
(2015/05/06)
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- ANDROGEN RECEPTOR MODULATING CARBOXAMIDES
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Compounds of formula (I) wherein Rx, Rz, R9, R10, R14, R14', R15, R15', A and B are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds possess utility as tissue-selective androgen receptor modulators (SARM) and are particularly useful as medicaments in the treatment of prostate cancer and other AR dependent conditions and diseases where AR antagonism is desired.
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Page/Page column 79
(2012/11/07)
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- Imidazole Derivative
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To provide a novel compound or an isotope thereof or a pharmaceutically acceptable salt thereof having S1P lyase inhibitory capacity and inducing the decrease in number of lymphocytes, and a pharmaceutical composition containing these as active ingredients. A compound represented by the general formula (I): or the general formula (II): or an isotope thereof or a pharmaceutically acceptable salt thereof.
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Page/Page column 41
(2013/02/27)
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- Synthesis, in silico docking experiments of new 2-pyrrolidinone derivatives and study of their anti-inflammatory activity
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A new class of 2-pyrrolidinone derivatives was designed, synthesized, and tested for their antioxidant and anti-inflammatory activities. The compounds were evaluated for their inhibitory activity against LOX. The most potent among them, 14d [IC50 0.08 (±0.005) mM], and 14e [IC50 0.0705 (±0.003) mM], were also tested in vivo. The compound 14d induced equipotent inhibition against rat paw edema, which is very close to the effect produced by the commonly used standard, namely indomethacin (47%). The LOX inhibitory activity of the compound 14e proceeds in parallel to the % inhibitory value of lipid peroxidation meaning that this LOX inhibitory activity is supported by the lipid peroxidation inhibition. The molecular features that govern their bioactivity were explored through in silico docking experiments. The results showed that acidic moieties must be placed in certain distance and orientation in the active site of LOX enzyme in order to productively exhibit inhibitory activity. In addition, the 2-pyrrolidinone template significantly contributes in the inhibitory properties of the new compounds.
- Moutevelis-Minakakis, Panagiota,Papavassilopoulou, Eleni,Michas, George,Georgikopoulou, Kalliopi,Ragoussi, Maria-Eleni,Neophytou, Niki,Zoumpoulakis, Panagiotis,Mavromoustakos, Thomas,Hadjipavlou-Litina, Dimitra
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experimental part
p. 2888 - 2902
(2011/06/17)
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- NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-COA DESATURASE
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The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
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Page/Page column 23-24
(2010/07/04)
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- Indole- and benzimidazole-substituted imidazole and benzimidazole derivatives
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Novel compounds are disclosed having the formula STR1 wherein X, R1, R2, R3, R4, and R5 are substituents. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
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- HISTAMINE DERIVATIVE, PROCESS FOR PREPARING IT AND ITS THERAPEUTIC USE
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The present invention relates to α,β-dimethylhistamine, of the rmula: STR1 in racemic form, or an optical isomer form or mixture of diastereoisomers and its acid addition salts. It may be prepared from an alkyl 2-amino 3-(1H-imidazol-4-yl)-carboxylate.
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- Two-step Synthesis of Imidazoles from Activated Alkynes
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Conjugate addition of 2-(tri-n-butylstannyl)tetrazoles (1) to activated alkynes gives 1-alkenyltetrazoles (4) and (5) predominantly.Use of the N-tributylstannyl derivatives, rather than the parent tetrazole, gives a high ratio of 1- to 2-alkenyl isomers and avoids the complication of further addition of the tetrazole or the alkyne to the initial adduct.Irradiation of the (Z)- and (E)-1-alkenyltetrazoles (4) and (5) at 254 nm then gives the expected imidazoles in moderate yield.However, 5-phenyl-2-(tri-n-butylstannyl)tetrazole (1a) reacted only slowly with ethyl phenylpropiolate to give ethyl 3,5-diphenylpyrazole-4-carboxylate (8), presumably via the 2-alkenyltetrazole (9) formed in preference to the 1-isomer for steric reasons.
- Casey, Michael,Moody, Christopher J.,Rees, Charles W.,Young, Richard G.
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p. 741 - 746
(2007/10/02)
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- Chemistry of Pyrimidine. 2. Synthesis of Pyrimidine N-Oxides and 4-Pyrimidinones by Reaction of 5-Substituted Pyrimidines with Peracids. Evidence for Covalent Hydrates as Reaction Intermediates
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The reaction of 5-substituted pyrimidines with peracids has been found to take divergent pathways depending on the presence or absence of a strong acid.Reaction of 5-bromo- (1) or 5-methoxypyrimidine (6) with m-chloroperbenzoic acid afforded the corresponding N-oxides in 29percent and 70percent yields, respectively.The formation of an N-oxide was not observed when either 1 or 6 was treated with 40percent peracetic acid in the presence of 1 equiv of sulfuric acid.In the case of 1, the product was 5-bromo-5(3H)-pyrimidinone (3), formed in 70percent yield.From 6, two products, 5-methoxy-4-(3H)-pyrimidinone (8) and 4(5)-carbomethoxyimidazole (9), were formed in a combined yield of 70percent (3:2 ratio of 8 to 9).The N-oxides were demonstrated to be stable to the above reaction conditions and are therefore not intermediates in the formation of 3, 8, or 9.Evidence for the existence of covalent hydrates makes it reasonable to suggest their formation as reaction intermediates.
- Kress, Thomas J.
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p. 3073 - 3076
(2007/10/02)
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