C07D403/02

Trypanosomes inhibitors

The invention relates to a compound of formula (I) ##STR00001##
wherein R.sup.1 and R.sup.2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

Methods of synthesizing thyroid hormone analogs and polymorphs thereof

The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TR? mutation.

Methods of synthesizing thyroid hormone analogs and polymorphs thereof

The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TR? mutation.

PYRIMIDINE COMPOUNDS AND PYRIMIDO INDOLE COMPOUNDS AND METHODS OF USE
20190233432 · 2019-08-01 ·

The present invention discloses a compound comprising the formula:

##STR00001##

wherein R is hydrogen or an alkyl group having from one to ten carbon atoms, or a compound of the formula wherein the S is replaced by CH.sub.2 or O, and optionally comprising a pharmaceutically acceptable salt or hydrate thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt or hydrate thereof.

PYRIMIDINE COMPOUNDS AND PYRIMIDO INDOLE COMPOUNDS AND METHODS OF USE
20190233432 · 2019-08-01 ·

The present invention discloses a compound comprising the formula:

##STR00001##

wherein R is hydrogen or an alkyl group having from one to ten carbon atoms, or a compound of the formula wherein the S is replaced by CH.sub.2 or O, and optionally comprising a pharmaceutically acceptable salt or hydrate thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt or hydrate thereof.

Bicyclic urea, thiourea, guanidine and cyanoguanidine compounds useful for the treatment of pain

Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome. ##STR00001##

Bicyclic urea, thiourea, guanidine and cyanoguanidine compounds useful for the treatment of pain

Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome. ##STR00001##

Pharmaceutically Acceptable Salt of EGFR Inhibitor, Crystal Form Thereof, Preparation Method Therefor and Application Thereof
20190194199 · 2019-06-27 ·

Provided in the present disclosure are a pharmaceutically acceptable salt of an epidermal growth factor receptor (EGFR) inhibitor, a crystal form thereof, a preparation method therefor and an application thereof. The structural formula of the EGFR inhibitor is as shown in formula I, and the pharmaceutically acceptable salt is a mesylate, p-toluenesulfonate, phosphate, hydrochloride or citrate salt of the EGFR inhibitor. The pharmaceutically acceptable salt of EGFR inhibitor of the present disclosure has a specific crystal form, has a higher solubility and stability than a corresponding free base, is more suitable for preparing drugs for use in treating cancer (especially non-small cell lung cancer), and satisfies the requirements for bioavailability and drug efficacy.

##STR00001##

N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(3-methyl-2-OXO-2,3-dihydro-1h-benzo[d]imidazol-1-yl)pyrimidin-2-yl)amino)phenyl)acrylamide hydrochloride as an inhibitor of epidermal growth factor receptor activity

The present disclosure relates to aniline pyrimidine derivatives or pharmaceutically acceptable salts thereof as EGFR inhibitors, specifically relates to compounds represented by formula (I) or pharmaceutically acceptable salts, pharmaceutical compositions, the method and uses thereof for treating EGFR mediated diseases. ##STR00001##

Polymer for carbon dioxide capture and separation

One or more embodiments relate to providing substrate for separating a first gas component from a gaseous mixture, said substrate comprising a benzimidazole-linked polymer. Also provided is a method for synthesizing a substrate for separating a first gas component from a gaseous mixture, the method comprising performing a free condensation reaction between an aryl-o-diamine and an aryl-aldehyde to yield a benzimidazole-linked polymer. Other embodiments related to providing a CO.sub.2 separation membrane comprising benzimidazole-linked polymer residing within a matrix.