Patent classifications
C07D417/00
COMPOUNDS, COMPOSITIONS AND METHODS
Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
COMPOUNDS, COMPOSITIONS AND METHODS
Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
Arylcyclopropylamine based demethylase inhibitors of LSD1 and their medical use
The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX). ##STR00001## ##STR00002##
Salt polymorph of thioxanthene-9-ylidene-1-methyl piperidine acid addition salts as antimigraine compounds
The present invention relates to novel crystal forms of 4-(6-ethoxy-1-methoxy-thioxanthene-9-ylidene)-1-methyl piperidine salts and 4-(6-ethoxy-1-hydroxy-thioxanthene-9-ylidene)-1-methyl piperidine salts; especially to novel crystal forms of 4-(6-ethoxy-1-methoxy-thioxanthene-9-ylidene)-1-methyl piperidine hydrochloride and 4-(6-ethoxy-1-hydroxy-thioxanthene-9-ylidene)-1-methyl piperidine hydrochloride as well as to the use of these salts for preventing or treating migraine or pulmonary hypertension.
Urethanes, ureas, amidines and related inhibitors of factor Xa
The invention relates to a new class of compounds, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions that are effective as selective inhibitors of factor Xa, both in the isolated state and in a complex with other proteins. The compounds of the invention can be used for treating and preventing diseases, such as acute coronary syndrome, myocardial infarction, unstable angina, refractory angina, thromboses caused by post-thrombolytic therapy or coronary angioplasty, acute ischemia mediated cerebrovascular syndrome, embolic stroke, thrombotic stroke, and other diseases in humans and other mammals associated with blood coagulation problems.
Organic thin film transistor, organic semiconductor thin film, and organic semiconductor material
An organic thin film transistor containing a compound represented by one of the following formulae in a semiconductor active layer has a high carrier mobility and a small change in the threshold voltage after repeated driving. X represents S or O, and at least one of R.sup.1 to R.sup.6 represents -L-R wherein L represents alkylene, etc., and R represents alkyl, etc. ##STR00001##
Trisubstituted bicyclic heterocyclic compounds with kinase activities and uses thereof
Trisubstituted bicyclic heterocyclic compounds (e.g., chromenones and quinolines) and pharmaceutical compositions,that modulate kinase activity, including PI3 kinase activity, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
METHODS FOR PREPARATION OF QUINAZOLINE DERIVATIVES
Methods for preparing compounds having the following structure (I):
##STR00001##
or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, wherein R.sup.1, R.sup.2a, R.sup.2b, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b and R.sup.4c, are as defined herein are provided. Related compounds and methods for making the same are also provided.
Small molecule modifiers of the Hec1-Nek2 interaction in G2/M
Certain embodiments of the present invention provide selected compounds having a molecular structure according to Formula 1: ##STR00001## In Formula 1, Z is CO, SO, or SO.sub.2; Ar is phenyl, heteroaryl, or heterocycloalkyl; Het is heteroaryl; R is R, X, or NR.sub.1R.sub.2; R is R.sub.3, or OR.sub.3; R is R.sub.4, or OR.sub.4; R.sub.1 and R.sub.2 are each independently H, alkyl, or acyl; R.sub.3 is H, heteroaryl, or alkyl; R.sub.4 is H, heteroaryl, or C.sub.nH.sub.2n+1 (n>2); and X is F, Br, I, CN, or NO.sub.2. In some embodiments, compounds having a molecular structure according to Formula 1 have the property of inhibiting a growth of a cell line selected from HeLa and MB468 with a sub-micromolar IC.sub.50.
Compounds, compositions and methods
Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.