67 results about "Benzodiazepine Compounds" patented technology

Benzodiazepinc compounds, and methods for using those compounds are provided. Some of the benzodiazepine compounds include 1,4-benzodiazepine-2-one and 1,4-benzodiazepine-2,5-dione compounds of structures (I) or (II): wherein R₁, R₂, R₃ and R₄ are as defined. The invention also includes enantiomers, pharmaceutically acceptable salts, prodrugs or derivatives of the benzodiazepine compounds. Any one or more of these benzodiazepine compounds can be used to treat a variety of dysregulatory disorders related to cellular death. Such disorders include autoimmune disorders, inflammatory conditions, hyperproliferative conditions, viral infections, and atherosclerosis. In addition, the above compounds can be used to prepare medicaments to treat the above-described dysregulatory disorders. The benzodiazepines can also be used in drugs screening assays and other diagnostic methods.

The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VII). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

The invention discloses a method for quickly detecting the doping of a benzodiazepine compound in a food, a medicine or a health-care product. The method comprises the following steps: firstly, preprocessing a sample to be measured, extracting the benzodiazepine compound which is added in an enriched transgression way and then combining with a colloidal gold immunological chromatographic method, thereby realizing the quick detection of the benzodiazepine compound added into the food, the medicine or the health-care product.The invention features wide coverage range of measured targets, simple operation, high detection speed and easy observation of a detection result, can realize the quick screening of a large number of samples, picks out the samples added with the benzodiazepine compound in a transgression way from a large number of samples, lowers the cost greatly and reduces the workload.The preprocessing method can effectively enrich the concentration of a substance to be measured, so the detection result is more sensitive and accurate.The invention is suitable for various common medicament forms in the food, the medicine or the health-care product, can fill up a system screening method which is absent in the industry, executes the supervision and control over the food and medicine market effectively and guarantees the safety of the diet and medicine of people.

The invention relates to a method for preparing benzodiazepine compounds, and discloses a method for preparing 8-R2-6-(2-R1-phenyl)-1-methyl-3a,4-dihydro-3H-imidazo[1,5-a][1,4] benzodiazepine (midbody II) and 8-R2-6-(2-R1-phenyl)-1-methyl-4H-imidazo[1,5-a][1,4] benzodiazepine (product III), wherein R is hydrogen, fluorine, chlorine, bromine or iodine; R2 is fluorine, chlorine, bromine or iodine. The midbody II is prepared from 7-R2-5-(2-R1-phenyl)-2-aminomethyl-2,3-dihydro-1H-[1,4] benzodiazepine and triethyl orthoacetate as raw materials through ultrasonic reaction; the product III is prepared by performing enzyme dehydrogenation on the midbody II. By adopting the technical scheme of the invention, the dehydrogenation reaction selectivity is improved, and the reaction yield is improved.

The invention discloses 1,3-benzodiazepine compounds with anticancer activity and a synthesis method thereof, and belongs to the technical field of drug development. The structural general formula ofthe 1,3-benzodiazepine compounds is shown in the specification; and the synthesis method comprises the following steps: mixing N-aryl amidine 1, propargyl alcohol ester compounds 2, a rhodium or ruthenium catalyst, an additive and an organic solvent, and performing heating and reacting to obtain the 1, 3-benzodiazepine compounds 3. The synthesis method disclosed by the invention has the advantagesof simple and easily available raw materials, simplicity and convenience in operation, mild conditions, wide substrate application range and the like, and the compounds have remarkable inhibitory activity on cancer cells such as HeLa or Ramos and are potential candidate drug molecular structures.

The present invention relates to benzodiazepine derivative compounds of formula (I), or pharmaceutically acceptable salts thereof. The present benzodiazepine compounds are useful Clostridium difficile inhibitors in the treatment of Clostridium difficile infection in humans. The present invention provides a pharmaceutical composition containing benzodiazepine compounds of formula (I) and a method of making as well as a method of using the same in treating patients infected with Clostridium difficile infection by administering the same. The compounds of the present invention may be used in combination with additional antibiotics or anti-toxin antibody drugs.

The present invention relates to novel pyrrolo[2,1-c][1,4]benzodiazepines compounds of general formula V as shown below, which are useful as potential antitumour agents and a process of preparing these compounds; particularly the present invention provides a process for the preparation of 7-methoxy-8-{n-[7-methoxy-(11aS)-1,2,3,10,11,11a-hexahydro-5H-pyrrolo[2,1-c][1,4]ben-zodiazepine-5-one-8-yloxy]alkyloxy}-(11aS)-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one, with varying aliphatic chain length and its 2-hydroxy derivatives.

The invention relates to a preparation method of a benzodiazepine compound, which comprises the following steps: reacting amino functionalized ionic liquid, phenylpropyl aldehyde, Boc-anthranilic acid and cyclohexyl isonitrile to obtain an ionic-liquid-loaded Ugi product; reacting the ionic-liquid-loaded Ugi product under the catalytic action of hydrogen chloride gas to obtain a benzodiazepine compound of which the side chain is modified by Ugi reaction; and carrying out rotary evaporation on the reaction liquid, and washing out residues with anhydrous aether to obtain the required benzodiazepine compound. Compared with the existing preparation method, the preparation method provided by the invention shortens the reaction procedures and enhances the reaction efficiency; and the synthesis method is simple and efficient, and has wide application prospects.

The invention is directed to novel [1,4]benzodiazepine compounds useful as vasopressin receptor antagonists for treating conditions involving increased vascular resistance and cardiac insufficiency. Pharmaceutical compositions comprising [1,4]benzodiazepine compounds of the present invention and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure, cerebral edema and ischemia, stroke, thrombosis, or water retention are also disclosed.

The invention relates to benzodiazepine compounds shown in a formula (I) as well as a preparation method and an application thereof. The compounds can be used for preparing a sterilizing agent.