Patent classifications
A61P7/12
SOLID FORMS OF N-[2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE-3-CARBOXAMIDE
The present invention relates to solid state forms of N-[2,4-bis(1,1-diethylethyl)-5-hydroxyphenyl]-1,4-dihydro-1-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.
Compound with effects of thrombolysis, free radical scavenging and thrombus-targeting
The present invention discloses a novel compound with effects of thrombolysis, free radical scavenging and thrombus-targeting, as well as a preparation method and use thereof. The compound is a ternary conjugate formed by conjugating a thrombolytic peptide, a free radical scavenger and a thrombus-targeting/antithrombotic peptide together via a linking arm. The present invention also discloses a pharmaceutical composition containing the compounds, wherein the compounds form a nanospherical structure.
Methods of treating mixed dyslipidemia
The present disclosure relates to, inter alia, methods of treating cardiovascular-related disease.
Long-acting co-agonists of the glucagon and GLP-1 receptors
Long-acting co-agonists of the glucagon and GLP-1 receptors are described.
Long-acting co-agonists of the glucagon and GLP-1 receptors
Long-acting co-agonists of the glucagon and GLP-1 receptors are described.
Transdermal therapeutic system for the administration of peptides
The invention relates to a transdermal therapeutic system (TTS) which is suited for the administration of a peptide to a patient through skin treated with ablation. The transdermal therapeutic system incorporates a back layer and an active substance-containing layer that includes at least one peptide and a carrier substance.
TRICYCLIC QUINOLINE AND QUINOXALINE DERIVATIVES
The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT.sub.2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT.sub.2C receptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT.sub.2C receptor.
Autotaxin Inhibitory Compunds
The present invention relates to compounds of formula I
##STR00001##
wherein A.sub.1, A.sub.2, A.sub.3, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, L, Ar and Q are each as defined herein. The compounds of the present invention are inhibitors of autotaxin (ATX) enzyme activity. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions (e.g. fibrosis) in which ATX activity is implicated.
HETEROAROMATIC COMPOUNDS AND THEIR USE AS DOPAMINE D1 LIGANDS
The present invention provides, in part, compounds of Formula I:
##STR00001##
and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), Parkinson's disease and chronic apathy.
Hydroxamate triterpenoid derivatives
Triterpenoid derivatives and compositions comprising said triterpenoids derivatives of Formula (I) are described, wherein RC(O)NHOH. Said triterpenoids and compositions show capacity to bind PHD2, stabilize HIF-1 and HIF-2 proteins, activate the HIF pathway in different cell types, induce angiogenesis in human endothelial vascular cell, show neuroprotective activity in vitro and in vivo, antidiabetic activity and reduce the levels of lipids in vivo, and increase the plasma levels of Erythropoietin in vivo. The triterpenoid derivatives described act also in a selective manner and do not induce Nrf2 activation, NF-B inhibition, STAT3 inhibition, and TGR5 activation, which are known activities of the natural triterpenoid precursors. Said triterpenoid derivatives are useful in the treatment of conditions and diseases which are responsive to HIF activation such as stroke, cerebral palsy, traumatic injuries and neurodegenerative diseases; and also IBD, myocardial ischaemia-reperfusion injury, acute lung injury, diabetic and chronic wounds, organ transplantation, acute kidney injury or arterial diseases. ##STR00001##