Patent classifications
C07D211/34
Biguanide compound and use thereof
The present invention relates to a guanidine compound and a use thereof, and more specifically, to a guanidine derivative showing excellent effects of inhibiting cancer cell proliferation, cancer metastasis, and cancer recurrence; a preparation method thereof; and a pharmaceutical composition containing the same as an active ingredient. Compared to existing drugs, the guanidine derivative according to the present invention shows excellent effects of inhibiting cancer cell proliferation, cancer metastasis, and cancer recurrence even with small doses, and may thus be effectively used in preventing or treating various cancers such as uterine cancer, breast cancer, stomach cancer, brain cancer, rectal cancer, colorectal cancer, lung cancer, skin cancer, blood cancer, liver cancer, etc., inhibiting cancer cell proliferation and cancer metastasis.
AMINO ACID HAVING FUNCTIONAL GROUP CAPABLE OF INTERMOLECULAR HYDROGEN BONDING, PEPTIDE COMPOUND CONTAINING SAME AND METHOD FOR PRODUCTION THEREOF
It has been found that the membrane permeability of peptide compounds can be improved by making at least one of amino acids constituting the peptide compound be an amino acid having a side chain capable of forming an intramolecular hydrogen bond.
AMINO ACID HAVING FUNCTIONAL GROUP CAPABLE OF INTERMOLECULAR HYDROGEN BONDING, PEPTIDE COMPOUND CONTAINING SAME AND METHOD FOR PRODUCTION THEREOF
It has been found that the membrane permeability of peptide compounds can be improved by making at least one of amino acids constituting the peptide compound be an amino acid having a side chain capable of forming an intramolecular hydrogen bond.
5-HT2A agonists for use in treatment of depression
The present invention relates to agonists of the 5-HT.sub.2A serotonin receptors and their medical uses. In one aspect the invention relates to 5-HT.sub.2A agonists of formula (I). In second aspect, the invention relates to selective 5-HT.sub.2A agonists of formula (II). In another aspect, the invention relates to mixed 5-HT.sub.2A/5-HT.sub.2C agonists of formula (III). In yet another aspect, the invention relates to 5-HT.sub.2A agonists for use in the treatment of a depressive disorder, more particular a 5-HT.sub.2A agonist for the use in the treatment of treatment-resistant depression.
5-HT2A agonists for use in treatment of depression
The present invention relates to agonists of the 5-HT.sub.2A serotonin receptors and their medical uses. In one aspect the invention relates to 5-HT.sub.2A agonists of formula (I). In second aspect, the invention relates to selective 5-HT.sub.2A agonists of formula (II). In another aspect, the invention relates to mixed 5-HT.sub.2A/5-HT.sub.2C agonists of formula (III). In yet another aspect, the invention relates to 5-HT.sub.2A agonists for use in the treatment of a depressive disorder, more particular a 5-HT.sub.2A agonist for the use in the treatment of treatment-resistant depression.
RORgT INHIBITOR, PREPARATION METHOD THEREOF AND USE THEREOF
A RORγt inhibitor as well as a preparation method thereof and uses thereof, and a pharmaceutical composition including the compound, a method for preparing the pharmaceutical composition, and use of the compound or the pharmaceutical composition in the treatment or prevention of RORγt-mediated cancer, inflammation, or autoimmune diseases in mammals, especially humans.
RORgT INHIBITOR, PREPARATION METHOD THEREOF AND USE THEREOF
A RORγt inhibitor as well as a preparation method thereof and uses thereof, and a pharmaceutical composition including the compound, a method for preparing the pharmaceutical composition, and use of the compound or the pharmaceutical composition in the treatment or prevention of RORγt-mediated cancer, inflammation, or autoimmune diseases in mammals, especially humans.
Small molecule inhibitors of Ebola and Lassa fever viruses and methods of use
Disclosed herein are compounds having a structure of formula (I), compositions and methods useful for the treatment of a disease or infection, such as a viral infection (e.g., Ebola), cancer and obesity: ##STR00001##
wherein A is N or CR.sup.8; Z is ##STR00002## E is selected from optionally substituted alkyl, cycloalkyl, arylalkyl, cycloalkylalkyl, amino, alkoxy, cycloalkyloxy, and cycloalkylamino; R.sup.1 is selected from optionally substituted aryl and heteroaryl, R.sup.2 and R.sup.3 are independently selected from H, deutero, optionally substituted alkyl, haloalkyl, or R.sup.2 and R.sup.3, together with the carbon to which they are bound, combine to form a carbonyl; and R.sup.8 is selected from H, deutero, halo, hydroxyl, cyano, amino, alkyl, alkoxy, carboxy, alkoxycarbonyl, and aminocarbonyl,
provided that E is not ##STR00003##
FERROPTOSIS INHIBITORS - DIARYLAMINE PARA-ACETAMIDES
Provided are compounds that inhibit ferroptosis activity, or modulate or inhibit a disease associated with ferroptosis dysregulation, such as neuropathy, ischemia reperfusion injury, acute kidney failure and cancer, including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
FERROPTOSIS INHIBITORS - DIARYLAMINE PARA-ACETAMIDES
Provided are compounds that inhibit ferroptosis activity, or modulate or inhibit a disease associated with ferroptosis dysregulation, such as neuropathy, ischemia reperfusion injury, acute kidney failure and cancer, including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.