86 results about "Thienopyridines" patented technology

The present invention relates to novel compounds, in particular novel thieno-pyridine and thieno-pyrimidine derivatives according to Formula (I), wherein all radicals are defined in the application. The compounds according to the invention are positive allosteric modulators of metabotropic receptors-subtype 2 ("mGluR2") which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

The present invention relates generally to thienopyrimidine and thienopyridine class compounds and methods of use thereof. In particular embodiments, the present invention provides compositions comprising thienopyrimidine class compounds and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins (e.g., for the treatment of leukemia, solid cancers and other diseases dependent on activity of MLL1 and MLL2 or menin).

This invention relates to processes and intermediates for manufacturing fused heterocyclic-type kinase inhibitor compounds, such as thienopyridine-based compounds, and to processes and intermediates for preparing intermediates that are useful in the manufacture of fused heterocyclic-type kinase inhibitor compounds, such as thienopyridine-based compounds, particularly at an industrial level.

A solid dispersion comprises, in essentially non-crystalline form, a kinase inhibitory compound, e.g., N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N′-(3-fluorophenyl)urea, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a cancer.

The invention pertains to the technical field of medicaments for preventing platelet aggregation and provides an oxime derivative which contains thienopyridine and has a structure as shown in the general formula (I), and pharmaceutically acceptable salt thereof, wherein, m equals to 1 and 2 and n equals to 0 and 1; R <1 >, R <2> and R <3> collectively or individually refer to hydrogen, C1-C6 straight-chain or branched-chain alkyl, C3-C6 naphthenic base, halogen, hydroxyl, carboxyl, amino, amido, cyano, nitryl, C1-C4 alkoxy, substituted phenyl and substituted heterocyclic radical; and R<4> refers to hydrogen, C1-C4 straight-chain or branched-chain alkyl as defined in the Instruction in details. In addition, the invention also relates to a preparation method of the compounds and discloses medicament combinations of which the compound or the pharmaceutically acceptable salt of the compound is taken as active ingredient and the application of such medicament combinations as drugs for preventing platelet aggregation.

The invention, belonging to the field of pharmaceutical chemicals, relates to a Thienopyridine alpha-amino benzylphosphonate, a preparation method and an application thereof. concretely, the invention relates to a compound of formula I, its medicinal salt, racemate, stereoisomer, or solvate, wherein each substituent is defined in the specification. The invention further relates to a pharmaceutical composition of the compound. The compound of the invention can effectively resist platelet aggregation and / or protect vascular endothelial cells.

Thienopyridinone compounds of Formula (I) and pharmaceutically acceptable salts thereof are described. In these compounds, one of X1; X2, and X3 is S and the other two are each independently CR, wherein R and all other variables are as defined herein. The compounds are shown to inhibit HPK1 kinase activity and to have in vivo antitumor activity. The compounds can be effectively combined with pharmaceutically acceptable carriers and also with other immunomodulatory approaches, such as checkpoint inhibition or inhibitors of tryptophan oxidation.

The invention belongs to the technical field of drugs for resisting malignant tumor and provides nitrogen-containing heterocyclic thienopyridine compounds with the structure shown as a general formula I and salts thereof, wherein R1 is hydrogen, and C1-C4 are alkanoyloxy substituted by alkyl; and R2 is nitrogen-containing six-membered heterocycle, i.e. benzoazo six-membered heterocycle. The invention further relates to a method for preparing the compounds, and also discloses drug compositions taking the compounds or the salts thereof as the active effective components and application thereof as drugs for resisting malignant tumor.

The invention discloses a novel hydrochloride acetic acid solvate which is 2-acetoxyl-5-(alpha-cyclopropyl carbonyl-2-luorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine shown as formula (I) or a crystal of the solvate and a preparation method of the solvate or the crystal thereof. Compared with prasugrel hydrochloride, the hydrochloride acetic acid solvate or the crystal thereof has higher stability and solubility and better contributes to the application to the preparation of a pharmaceutical preparation.

This application relates to novel fused tricyclic thienopyridines of Formulas I and II, which useful for treating Hepatitis B infection and other diseases. This application also relates to pharmaceutical compositions comprising thienopyridines and to the use of such compositions to treat Hepatitis B and other diseases.

A process for the resolution of each of the enantiomers of methyl-α-5-[4,5,6,7-tetrahydro[3,2-c]thienopyridyl]-(2-chlorophenyl)acetate and salts thereof by diastereomeric crystallization comprising the use of a single optically active resolving agent and at least one solvent.

The invention discloses a method for preparing prasugrel (I). The method comprises the following steps: performing addition reaction of a Grignard reagent prepared from fluorobenzyl bromide and cyclopropanecarbonitrile to obtain cyclopropyl-2-fluorobenzyl ketone; performing chlorination to obtain a main intermediate, namely alpha-cyclopropyl carbonyl-2-fluorobenzyl chloride (II); performing condensation reaction of (II) and 2-oxo-2,4,5,6,7,7alpha-hexahydrothieno[3,2-c]pyridine 4-methylbenzenesulfonate to obtain an intermediate, namely 5-(alpha-cyclopropyl carbonyl-2-fluorobenzyl)-2-oxo-2,4,5,6,7,7alpha-hexahydrothieno[3,2-c]pyridine (IV); and performing acetic anhydride esterification on the (IV) to obtain the prasugrel (I).

Acid addition salts of 2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine with sulfuric acid or sulfonic acids, pharmaceutical compositions comprising the same and processes for the production thereof. The acid addition salts have a low toxicity.

The invention belongs to the technical field of malignant tumor resistant medicaments and provides 2-(substituted phenyl)-2-(4,5,6,7-thiophane[3,2-c] pyridine-5(4H)-group)-N-substitute-acetamide with a structure of a general formula I and a pharmaceutically acceptable salt thereof, wherein R is hydrogen, a C1-C3 straight chain or a branched alkyl group; and R1 and R2 are hydrogen, C1-C3 straight chains or branched alkyl groups, halogens, halogenated methyl groups and C1-C3 alkoxyl groups. The invention also relates to a preparation method of the compound and also discloses a medical composition using the compound or the pharmaceutically acceptable salt thereof as an active and effective constituent and application thereof as malignant tumor resistant medicaments.

Novel bicyclic heteroaromatic compounds are provided that are inhibitors of bacterial methionyl tRNA synthetase (MetRS). Compounds of the invention generally have a left hand side phenylether constituent and a right hand side thienopyridone constituent. Also disclosed are methods for their preparation and their use in therapy as antibacterial agents, particularly as anti-Clostridium difficile agents.

Salts of N-(4- {4-amino-7-[ 1 -(2-hydroxyethyl)- 1 H-pyrazol-4-yl]thieno[3,2-c]pyridin- 3-yl}phenyl)-N'-(3-fluorophenyl)urea and crystalline forms thereof are suitable pharmaceutical ingredients for pharmaceutical compositions useful in the treatment of disease, for example, cancer.

The invention relates to novel 5-cyano-thienopyridines of the formula (I) where R1, R2, and R3 have the meanings designated in Claim 1. Said 5-cyano-thienopyridines are inhibitors of TGF-beta receptor kinase and may be used, among other things, for the treatment of tumors.

Use of thienopyridone derivatives of formula (I), in which B, R, R6, Y and Z are as defined in the description, and their pharmaceutically acceptable salts, for the preparation of a pharmaceutical composition useful for the treatment of diabetes, metabolic syndrome, related disorders and obesity.

The invention relates to a preparation method for 2-oxygen-2, 4, 5, 6, 7, 7alpha-hexahydro thiophene and (3, 2-c) pyridine, which includes the following steps: a compound of the following formula or the corresponding salt under the acidic condition is hydrolyzed and a target product is obtained by post-processing; wherein, R stands for alkyl. The method adopts the existing ordinary compound materials, and obtains 2-oxygen-2, 4, 5, 6, 7, 7alpha-hexahydro thiophene and (3, 2-c) pyridine by one step of hydrolysis reaction. Meanwhile, the method has the advantages of the high yield, the mild reaction condition, and is very suitable for the industrial mass production.

The invention relates to a new method for synthesizing a prasugrel intermediate 2,4,5,6,7,7alpha-hexahydro thieno[3,2-c]pyridine-2-ketone and an application of the method in synthesizing prasugrel. The preparation method of the prasugrel intermediate comprises the following steps: 2,4,5,6,7,7alpha-hexahydro thieno[3,2-c]pyridine-2-ketone is obtained through protecting 4,5,6,7-tetrahydro thieno[3,2-c]pyridine hydrochloride, carrying out catalytic oxidation by a metal salt in high pressure oxygen atmosphere and carrying out protective group removal; and an equation is shown in the specification. The method of the present invention which has the characteristics of safety and high yield is suitable for large-scale industrial production, and the method for preparing prasugrel with the intermediate of the present invention has a higher total yield than present preparation methods.

The invention belongs to the technical field of antineoplastic medicines and provides thieno pyridinone derivative with the structure of the general formula I and salt thereof which are acceptable in pharmacy, wherein n, R1 and R2 are defined in the specification. The invention also relates to a preparation method of the compound, and discloses pharmaceutical composites using the compound or the salt thereof which are acceptable in pharmacy as active ingredient and the applications of the pharmaceutical composites used as the antineoplastic medicines.

The compound of the present invention possesses excellent gonadotropin-releasing hormone antagonizing activity, and is useful for preventing or treating sex hormone-dependent diseases, e.g., sex hormone-dependent cancers (e.g., prostatic cancer, uterine cancer, breast cancer, pituitary tumor), prostatic hypertrophy, hysteromyoma, endometriosis, precocious puberty, amenorrhea syndrome, multilocular ovary syndrome, pimples etc. or as a pregnancy regulator (e.g., contraceptive), infertility remedy or menstruation regulator.