98952-77-3

Upstream product

• 873-74-5 4-Aminobenzonitrile 
• 107-07-3 2-chloro-ethanol 
• 1194-02-1 4-fluorobenzonitrile 
• 141-43-5 ethanolamine 
• 75-21-8 oxirane 
• 78604-19-0 1-(p-cyanophenyl)-3-(2-chloroethyl)triazene 

Downstream Products

• 1021112-16-2 C₉H₁₂N₂O₂ 
• 635751-18-7 2-[[4-(aminocarbonyl)phenyl]amino]ethyl acetate 
• 1610612-45-7 4-(2-(tert-butyldimethylsilyloxy)ethylamino)benzonitrile 
• 635751-84-7 2-[[4-(aminocarbonyl)phenyl] [[(R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]-1H-benzimidazol-1-yl]carbonyl]amino]ethyl acetate 
• 1448673-47-9 4-({2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)oxy]ethyl}amino)benzonitrile 
• 1448673-50-4 4-{[2-(aminooxy)ethyl]amino}benzenecarboximidamide 
• 1448673-48-0 4-{[2-(aminooxy)ethyl]amino}benzonitrile 

Relevant academic research and scientific papers

ANTIBACTERIAL COMPOUNDS

The present invention relates to the following compounds wherein the integers are as defined in the description, and where the compounds may be useful as medicaments, for instance for use in the treatment of tuberculosis.

CONTROLLED RELEASE PREPARATION

A controlled release preparation wherein the release of active ingredient is controlled, which releases an active ingredient for an extended period of time by staying or slowly migrating in the gastrointestinal tract, is provided by means such as capsulating a tablet, granule or fine granule wherein the release of active ingredient is controlled and a gel-forming polymer. Said tablet, granule or fine granule has a release-controlled coating-layer formed on a core particle containing an active ingredient.

COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES

The present invention provides compounds of formula I: [INSERT FORMULA HERE] or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a Plasmodium parasite, such as malaria.

AMIDINE SUBSTITUTED BETA - LACTAM COMPOUNDS, THEIR PREPARATION AND USE AS ANTIBACTERIAL AGENTS

The present invention relates to novel β-lactam compounds of formula (I), their preparation and use. In particular, this invention relates to novel β-lactam compounds which are amidine substituted monobactam derivatives useful as antimicrobial agents and their preparation.

Syntheses of novel 1,3-diazaazulene derivatives and their nonlinear optical characterization

We have synthesized three new 1,3-diazaazulene derivatives, namely, 2-(4′-N,N-dimethylaminophenyl)-6-nitro-1,3-diazaazulene (18, DMAPNA), 2-(4′-aminophenyl)-6-nitro-1,3-diazaazulene (19, APNA) and 2-[4′-N-(2-hydroxyethyl)aminophenyl]-6-nitro-1,3-diazaazulene (20, HEAPNA), each of them contains an amino substitute as the electron donor (D), 2-phenyl-1,3-diazaazulene as the π-conjugated bridge and a nitro as the electron acceptor (A). Our theoretical results have predicted that these D-π-A type chromophores possess low ground-state dipole moment (μg) and large first-order hyperpolarizability (β), which may facilitate a low degree of aggregation for the chromophores dispersed in a polymeric matrix as well as a large nonlinear optical (NLO) response. The expected NLO performance has been confirmed by the experimental β and μg values, e.g., for 18, 407.8 × 10-30 esu and 4.7 D, respectively. The origins of large β and low μg are explained in terms of a two-state quantum model. The DMAPNA (18)-doped and poled polymethylmethacrylate film exhibits a large second harmonic generation (SHG) coefficient of d33 = 10.9 pm V-1 with excellent thermal stability (above 70% of the maximal SHG coefficient remains at ～100 °C). The Royal Society of Chemistry.

DRUG COMPOSITION HAVING ACTIVE INGREDIENT ADHERED AT HIGH CONCENTRATION TO SPHERICAL CORE

Granule, fine particle or tablet of excellent leaching property, comprising a drug active ingredient in high content realized by forming a layer containing drug active ingredient on core particles through a combination of a method of dispersing and adhering an active ingredient while spraying or adding a binder with a method of spraying or adding a solution or suspension wherein an active ingredient and a binder are contained so as to effect adhesion. Further, there are provided a drug composition containing such a granule, fine particle or tablet and a process for producing the same.

CONTROLLED RELEASE COMPOSITION

The present invention provides a controlled release composition showing release of an active ingredient (proton pump inhibitor) controlled in two or more steps at different release rates, which contains1) a release-controlled part A capable of controlling release of the active ingredient to occur at a predetermined rate,2) a release-controlled part B capable of controlling release of the active ingredient to occur at a predetermined rate lower than the release rate of the release-controlled part A, and where necessary, 3) a release-controlled part C capable of controlling release of the active ingredient to occur at a predetermined rate faster than the release rate of the release-controlled part B, wherein the release of the active ingredient from the release-controlled part B precedes the release of the active ingredient from the release-controlled part A (when release-controlled part C is contained, the release of the active ingredient from the release-controlled part C precedes the release of the active ingredient from the release-controlled part B).

PRODRUGS OF IMIDAZOLE DERIVATIVES, FOR USE AS PROTON PUMP INHIBITORS IN THE TREATMENT OF E.G. PEPTIC ULCERS

An imidazole compound represented by the formula (I), a salt thereof and a compound of the formula (V), which is one of the intermediates thereof. wherein each symbol is as defined in the present specification. The compound of the present invention shows a superior anti-ulcer activity, a gastric acid secretion inhibitory action, a mucosa-protecting action, an anti-Helicobacter pylori action and the like. Since it shows low toxicity, the compound is useful as a pharmaceutical product.

Imidazoquinazoline derivatives

PCT No. PCT/JP97/03023 Sec. 371 Date Apr. 27, 1998 Sec. 102(e) Date Apr. 27, 1998 PCT Filed Aug. 29, 1997 PCT Pub. No. WO98/08848 PCT Pub. Date Mar. 5, 1998Imidazoquinoline derivatives of the formula (wherein X may be O or S) provide selective cyclic guanosine 3',5' monophosphate (cGMP)-specific phosphodiesterase (PDE) inhibitory activity. The compounds are useful for treating or ameliorating cardiovascular disease such as thrombosis, angina pectoris, hypertension, heart failure and arterial sclerosis, as well as asthma, impotence and the like.