72 results about "Tetrahydro-beta-carboline" patented technology

A composition includes a substituted dihydro- or tetrahydro-beta-carboline of formula (II) or (III), wherein the aromatic ring of the carboline may include one or more substituents selected from the group consisting of hydroxy, C1-6 alkoxy, benzyloxy, C1-6 acyloxy, amino, C1-6 alkyl, C1-6 dialkylamino, halogen, and carboxy, and the C-1 position of the carboline may include a substitutent selected from the group consisting of a carbocyclic group and a heterocyclic group. The composition may include a salt or a prodrug of the substituted dihydro- or tetrahydro-beta-carboline. The composition may further includes a pharmaceutically acceptable carrier, diluent, or excipient.

The invention discloses an acyl-tetrahydro-beta-carboline micro-molecular organic compound shown as a structural formula (I) or a hydrate thereof or pharmaceutically acceptable salts, application of a compound containing the acyl-tetrahydro-beta-carboline micro-molecular organic compound provided by the invention or a medical composition thereof to the preparation of medicaments for treating various diseases such as cancer, tumor metastasis and the like, and a preparation method of the acyl-tetrahydro-beta-carboline micro-molecular organic compound provided by the invention and derivatives thereof.

The invention discloses a (3S) -1, 1-Dihydroxymethyl-Tetrahydro-Beta-Carboline-3-Formyl-Gly-Arg-Gly-Asp-Val, discloses a preparation method thereof, discloses the anti-arterial thrombosis activity, discloses the anti-venous thrombosis activity, discloses the activity of inhibiting the GPIIb/IIIa expression, and discloses the activity of inhibiting the P-selectin expressionin vivo. Therefore, the invention discloses the application in preparing anti-arterial thrombosis medicine, the application in preparing the anti-venous thrombosis medicine, the application in preparing the GPIIb/IIIa antagonist and the application in preparing P-selectin antagonist. The formulas are shown in the decription.

The invention discloses a compound with general formula (I) of anti-thrombus activity. The invention also discloses a preparation method of the compound and the application as the anti-thrombus agent. The invention introduces the amino acid residues into the second N of (3S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid to prepare the compound with general formula (I) of the invention. The compound of the invention not only has the good anti-thrombus activity, but also has the simpler structure and the lower preparation cost by comparing with the anti-thrombus agent prepared by the L-amino acid modification of (3S)-1,2,3,4-tetrahydro-Beta-carboline-3-carboxylic acid. Moreover, whether in the polar solvent or the non-polar solvent, the compound with the general formula (I) of the invention has the good solubility and high bioavailability.

The present invention belongs to the field of medicine synthesis technology, and is especially 1- (3-indolyl)-1, 2, 3, 4-tetrahydro-beta-carboline compounds and analogs in the general expression as shown and with substituted hydroxyl radical or acyl radical in the 2nd position, and their preparation process and medical application. Initial pharmacodynamic research of extracorporeal rice blast mold resisting experiment and extracorporeal antitumor experiment shows that these compounds has excellent antifungal activity and antitumor activity, so that they may be developed into antifungal medicine and antitumor medicine.

The invention discloses a (3S) -1, 1-Dihydroxymethyl-Tetrahydro-Beta-Carboline-3-Formyl-Gly-Arg-Gly-Asp-Ser, discloses a preparation method thereof, discloses the anti-arterial thrombosis activity, discloses the anti-venous thrombosis activity, discloses the activity of inhibiting the GPIIb/IIIa expression, and discloses the activity of inhibiting the P- selectin expression in vivo. Therefore, theinvention discloses the application in preparing anti-arterial thrombosis medicine, the application in preparing the anti-venous thrombosis medicine, the application in preparing the GPIIb/IIIa antagonist and the application in preparing P- selectin antagonist. The formulas are shown in the decription.

The invention discloses heterocyclic carboxylic acid-modified anti-tumor oligopeptides. The heterocyclic carboxylic acid-modified anti-tumor oligopeptides have a general formula I. In the general formula I, RCO represents 1,2,3,4-tetrahydro-beta-carboline-3-formyl, beta-carboline-3-formyl, 1,2,3,4-tetrahydroisoquinol-3-formyl, isoquinol-3-formyl, or 1-methyl-1,2,3,4-tetrahydro-beta-carboline-3-formyl. The invention also discloses a preparation method of the heterocyclic carboxylic acid-modified anti-tumor oligopeptides, and in-vitro tumor cell proliferation-resistant activity of the heterocyclic carboxylic acid-modified anti-tumor oligopeptides. The invention further discloses heterocyclic carboxylic acid-modified anti-tumor oligopeptide activity of inhibiting weight gain of a tumor in a S180 tumor-loading mice, and application of the heterocyclic carboxylic acid-modified anti-tumor oligopeptides in preparation of anti-tumor drugs. The general formula I is RCO-Leu-Pro-Asn-Ile-Ser-Lys-Pro.

The invention relates to a tetrahydro-beta-carboline derivative, a preparation method thereof and a use thereof. The invention discloses the tetrahydro-beta-carboline derivative described as a general formula (I), wherein R1 is H, benzyl, benzoyl or C1-6 acyl, R2 is H, C1-6 alkyl, C1-6 alkoxyl, COOH, COOR3, AA or AA-R4, R3 is C1-6 alkyl, R4 is COOH or COOR3 and AA is amino acid group. The invention further discloses the preparation method of a compound described as the general formula (I), a pharmaceutical composition containing the compound described as the general formula (I) and the use ofthe compound in the preparation of anti-inflammatory medicaments.

The invention discloses a compound with a general formula II and thrombolytic activity and a preparation method thereof, and application of the compound serving as a thrombolytic. The thrombolytic activity of the compound with the general formula II is evaluated by using a rat cervical artery and vein bypass cannula thrombosis model. The result of an animal test shows that the compound with the general formula II has excellent thrombolytic activity and can clinically serve as the thrombolytic.

The invention relates to a 4-methoxyphenyl substituted tetrahydro-beta-carboline piperazine dione derivative and uses thereof, and specifically discloses a compound represented by a formula I, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, wherein each group is defined in the specification. According to the present invention, the compound has dual inhibitory activity onacetylcholinesterase and phosphodiesterase 5, and has good blood-brain barrier permeability, such that the compound can be used for preparing drugs for treatment and/or prevention of Alzheimer's diseases. The formula I is defined in the specification.

The invention discloses a green synthetic method of a beta-carboline compound. The green synthetic method of the beta-carboline compound is technically characterized by comprising the following steps: carrying out Pictet-Spengler reaction on L-tryptophan to prepare tetrahydro-beta-carboline-3-carboxylic acid; and decarboxylating and oxidizing the tetrahydro-beta-carboline-3-carboxylic acid under the effect of an oxidizing decarboxylating agent hydrogen peroxide to prepare the beta-carboline compound. The invention discloses specific synthetic steps and main reaction equations in the preparation process. The method disclosed by the invention has the advantages of simple preparation and safety and environmental-friendliness, and the yield of the beta-carboline compound is high, so that the demand on green chemistry is satisfied.

The invention relates to an improvement on a synthesis method of a tetrahydro-beta-carboline compound (II). The method comprises reacting D-tryptophan methyl ester hydrochloride and piperonal at 50 DEG C-150 DEG C in a certain solvent to obtain hydrochloride of a structural formula (II) compound, wherein the solvent can be nitroethane, dioxane, methylbenzene, dimethylbenzene, benzene or nitrobenzene. The yield and purity of products prepared by the method are greatly improved, and the method is especially suitable for industrial production.

The invention discloses (3S)-1,1-dimethylol-tetrahydro-beta-carboline-3-formyl-Gly-Leu-Asp-Val, a preparation method, anti-arterial-thrombus activity, anti-venous-thrombosis activity, GPIIb/IIIa expression inhibiting activity and P-selectin expression inhibition activity thereof, such that the prevent invention discloses applications of the (3S)-1,1-dimethylol-tetrahydro-beta-carboline-3-formyl-Gly-Leu-Asp-Val in preparation of anti-arterial-thrombus drugs, anti-venous-thrombosis drugs, GPIIb/IIIa antagonists and P-selectin antagonists. The structure formula is defined in the specification.

The invention discloses a tetrahydro carboline derivative modified with two amino acids and a preparation method and an application thereof. According to the invention, L-tryptophan methyl ester is allowed to react with 1,1,3,3-tetramethoxy propane by a microwave reaction; the obtained product is modified by amino acids to obtain a series of (1R, 3S)-1-[1-(1R, 3S)-tetrahydro beta-carboline-3-formyl amino acid-1-yl-methyl]-tetrahydro beta-carboline-3-formyl amino acid derivatives and intermediates thereof; and the derivatives are evaluated for in vitro antiplatelet aggregation activity and in vitro antithrombotic activity. The method of the invention is simple; the used raw materials are easily available, safe and cheap; the obtained product has antiplatelet aggregation activity and antithrombotic activity, which indicates the clinical application prospects of (1R, 3S)-1-[1-(1R, 3S)-tetrahydro beta-carboline-3-formyl amino acid-1-yl-methyl]-tetrahydro beta-carboline-3-formyl amino acidas an antithrombotic agent.

The present invention discloses an aromatic alkanoyl tetrahydro-beta-carboline compound represented by a structural formula (I), and related analogs thereof or hydrates or pharmaceutically acceptable salts thereof, and the application of the compound or pharmaceutical compositions containing the compound in the preparation of drugs for treatment of various cancers and tumor metastasis.

The invention provides nauclea officinalis pierre ex pitard total alkaloid extract, which comprises 3-R-3,4-dihydroangustoline, naucleofficine D, 1,2,3,4-tetrahydro-beta-carboline, 3-S-3,4-dihydroangustoline, latifoliamide D, latifoliamide B, angustoline, 3,14-dihydroangustine, 3,14,18,19-tetrahydroangustine, 6'-acetyl strictosamide, vincoside lactam and strictosamide. The content of total alkaloids in the nauclea officinalis pierre ex pitard total alkaloid extract obtained by such a preparation method is more than 50 weight percent. The nauclea officinalis pierre ex pitard total alkaloid extract obtained by the preparation method and a medicinal composition prepared from the nauclea officinalis pierre ex pitard total alkaloid extract have better anti-inflammatory effects.

The present invention relates to a 3,4-methylenedioxyphenyl substituted tetrahydro-beta-carboline piperazine dione derivative and uses thereof, and specifically discloses a compound represented by a formula I, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, wherein each group is defined in the specification. According to the present invention, the compound has dual inhibitory activity on acetylcholinesterase and phosphodiesterase 5, and has good blood-brain barrier permeability, such that the compound can be used for preparing drugs for treatment and/or prevention ofAlzheimer's diseases. The formula I is defined in the specification.

The invention relates to a bactericidal composition containing an alternaria tenuissima activator protein. The alternaria tenuissima activator protein and a compound A serve as active ingredients, andthe compound A is a tetrahydro-beta-carboline compound containing an acylhydrazone structure. The composition can be used for controlling viral diseases of fruit trees, vegetables and field crops andcan achieve the effects of effectively improving stress resistance of the crops, regulating growth of the crops, promoting flowering, improving yield, improving the fruit quality and the like.

The invention discloses a (3S) -1, 1-Dihydroxymethyl-Tetrahydro-Beta-Carboline-3-Formyl-Gly-Arg-Gly-Asp-Phe, discloses a preparation method thereof, discloses the anti-arterial thrombosis activity, discloses the anti-venous thrombosis activity, discloses the activity of inhibiting the GPIIb/IIIa expression, and discloses the activity of inhibiting the P-selectin expression in vivo. Therefore, theinvention discloses the application in preparing anti-arterial thrombosis medicine, the application in preparing the anti-venous thrombosis medicine, the application in preparing the GPIIb/IIIa antagonist and the application in preparing P- selectin antagonist. The formulas are shown in the decription.