78 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).

The present invention relates to selective allosteric potentiators of the Formula (I):

or pharmaceutically acceptable salts thereof, for the treatment of disorders associated with M₄ muscarinic receptors.

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.

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 present disclosure provides compounds and methods for inhibiting the interaction of menin with its upstream or downstream signaling molecules including but not limited to MLL1, MLL2 and MLL-fusion oncoproteins. Compounds of the disclosure may be used in methods for the treatment of a wide variety of cancers and other diseases associated with one or more of MLL1, MLL2, MLL fusion proteins, and menin.

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.

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.

The invention discloses a method for synthesizing 2-carbonyl thienopyridine compound. According to the method provided by the invention, 2-halo-3-alkynol pyridine as shown in formula (I) and sulfur sources are mixed; and with the aid of a catalyst, after reacting in a solvent for a while, 2-carbonyl thienopyridine compound as shown in formula (II) is prepared after purification treatment. The sulfur sources are selected from one or more of elemental sulphur, ammonium sulfide, thiourea, sodium sulfide, and ethyl potassium xanthate, and the catalyst is selected from one of copper acetate, cuprous iodide, cuprous bromide, cuprous chloride, copper chloride, cupric acetylacetonate, palladium chloride, and copper trifluoromethanesulfonate. The technical scheme of the invention has the advantagesof less reaction steps, simple operation method, wide source of reaction substrate, low costs and easy availability of the catalyst, high product yield and the like, and the technical scheme is verysuitable for industrial mass production. The formulas are shown in the description.

The thieno[2,3-b]pyridines of general formula (I),

wherein

R¹ is Me, C₆H₅, 3,4,5-(OMe)₃C₆H₂, NH₂;

R² is H, CN, COMe, COOC_1-4alkyl, COOC₂H₄OMe, COOC₂H₄OPr(n);

R³ is C₆H₄R⁶, 3,4-OCH₂O—C₆H₃; 2-furanyl;

• • R⁶ is 4-Cl, 4-NO₂, 4-N(C_1-4alkyl)₂, 3-(C_1-4alkyloxy), 4-(C_1-4alkyloxy), 3,4-(C_1-4alkyloxy)₂, 3,4,5-(C_1-4alkyloxy)₃;

R⁴ is NH₂, NHCOMe;

R⁵ is CN, COMe, COC₆H₄R⁷; CO-(2-naphthyl);

R⁷ is H, 4-F, 4-Cl, 3-OMe, 4-OMe, 2,4-(OMe)₂, 3,4,5-(OMe)₃

as multidrug resistance modulators to increase the effectiveness of chemotherapy in cancer treatment.