47 results about "Thienopyridine" patented technology

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 and thienopyridine 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, MLL2, MLL fusion proteins, and / or menin).

A formulation of a compound of formula (I) process of manufacture and methods of using it are disclosed.

A method of treating or preventing a disease or condition in a subject that was previously treated with at least one thienopyridine is described. The method includes administering to the subject an effective amount of at least one reversible, short-acting P2Yi2 inhibitor. The described method can be used for subjects diagnosed with symptoms such as stable or unstable angina, vascular ischemic events, atherosclerosis, acute coronary syndrome, as well as STEMi or N-STEMI. The described method can also be used for patients having previously received a stent, such as a bare metal stent or a drug-eluting stent, and the treatment or prevention of stent thrombosis. The method can be used prior to, during, or after an invasive procedure such as coronary artery bypass grafting, percutaneous coronary intervention, or other general surgical procedure.

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 belongs to the medical technology field of anti-platelet aggregation effect, and provides a thienopyridine ester derivative containing nitrile group and its pharmaceutically acceptable salt possessing a structure shown in a general formula I, wherein R is a nitrile group. The invention also relates to a preparation method of the above compound, simultaneously, the present invention also discloses the medical composition using the compound or its pharmaceutically acceptable salt as an effective activity ingredient, and the applications as medicines for anti-platelet aggregation.

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 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 relates to tetrahydrothieno-[2,3-c]pyridine deuterated derivatives and a preparation method and medicament applications thereof, belonging to the field of medicinal chemistry. The derivatives contain salt of a compound in the formula I, and enantiomer and racemate of the compound in the formula I. The in-vitro whole-blood hydrolysis experiment results show that the stability of the compound in the formula I on esterase is good, and the hydrolysis rate of methyl carboxylate is obviously slower than that of non-deuterated methyl ester. The compound in the formula I can be effectively converted into pharmacological active metabolite in a human body to achieve the effect of inhibiting the platelet aggregation, and the concentration of the active metabolite is obviously higher than that of a non-deuterated compound of clopidogrel or a corresponding structure. The pharmacodynamic experiment results show that the compound in the formula I has the effect of obviously inhibiting the platelet aggregation, and the effect of inhibiting the platelet aggregation is obviously better than that of the non-deuterated compound of clopidogrel and the corresponding structure. Therefore, the compound in the formula I can be used for preparing medicaments for preventing or treating related thrombus and embolism diseases.

The compounds of the present invention possess 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 present invention relates to compounds of formula (I) wherein R1, R2 and B1, B2 are as defined in claim 1, including pharmaceutical compositions thereof and for their use in the treatment and / or prevention of diseases and disorders modulated by AMP agonists. The invention is also directed to intermediates and to a method of preparation of compounds of formula (I).

The present invention relates to a method for inhibiting the activity or expression of FLT3 tyrosine kinase in a cell or a subject, or reducing the activity or expression of FLT3 kinase, comprising administering a farnesyl transferase inhibitor and a compound selected from formula I' and formula II' FLT3 kinase inhibitors of thienopyrimidines and thienopyridines: where R 1 , R 3 , B, Z, Q, p, q and X are as defined herein. The invention includes prophylactic and therapeutic methods for treating subjects at risk of (or susceptible to) developing a cell proliferative disorder or a FLT3-related disorder.

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.

The present invention relates to novel NADPH oxidase II inhibitors and their use in the treatment of diseases mediated by the NADPH oxidase II enzyme.