Patent classifications
C07D209/34
Salts of Nintedanib and Crystalline Forms Thereof
Provided are novel salts of nintedanib and crystalline forms thereof. Specific salts of nintedanib provided by the present invention include glutarate, hippurate, levulinate, acesulfamate, diacesulfamate, and saccharinate. Also provided are pharmaceutical compositions including the nintedanib salts and crystalline forms thereof, and the use of these salts in the treatment or prevention of fibrotic diseases selected from the group including idiopathic pulmonary fibrosis, chronic fibrosing interstitial lung disease with a progressive phenotype, and systemic sclerosis-associated interstitial lung disease.
[1.1.1] bicyclo compounds as indoleamine 2,3-dioxygenase inhibitors
Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder. ##STR00001##
[1.1.1] bicyclo compounds as indoleamine 2,3-dioxygenase inhibitors
Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder. ##STR00001##
DEGRADATION OF PROTEIN KINASES BY CONJUGATION OF PROTEIN KINASE INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE
The present application provides bifunctional compounds of Formula (X):
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or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for protein kinases. The present application also relates to methods for the targeted degradation of one or more protein kinases through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to one or more protein kinases which can be utilized in the treatment of disorders modulated by protein kinases.
DEGRADATION OF PROTEIN KINASES BY CONJUGATION OF PROTEIN KINASE INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE
The present application provides bifunctional compounds of Formula (X):
##STR00001##
or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for protein kinases. The present application also relates to methods for the targeted degradation of one or more protein kinases through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to one or more protein kinases which can be utilized in the treatment of disorders modulated by protein kinases.
Opioid receptor modulators
Provided herein are opioid receptor modulators and pharmaceutical compositions comprising said compounds.
2-OXINDOLE COMPOUNDS
Oxindole compounds useful for the treatment of CCR(9) mediated conditions or diseases are provided.
2-OXINDOLE COMPOUNDS
Oxindole compounds useful for the treatment of CCR(9) mediated conditions or diseases are provided.
COMPOSITION FOR FORMING ORGANIC FILM, PATTERNING PROCESS, AND COMPOUND AND POLYMER FOR FORMING ORGANIC FILM
An organic film forming composition, containing: a material shown by formula (I) and/or (II); and an organic solvent, where R.sub.1 and R.sub.4 each represent a hydrogen atom, an allyl or propargyl group, R.sub.2 and R.sub.5 each represent a substituent, R.sub.3 and R.sub.6 represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an alkynyl group having 2 to 4 carbon atoms, or an alkenyl group having 2 to 4 carbon atoms. “m” and “i” represent 0 or 1, “k” and “q” represent an integer of 0 to 2, “n” represent 1 or 2, “h”, and “j” represent an integer of 0 to 2 and satisfy the relationship 1≤h+j≤4, and “1” and “r” represent 0 or 1. W represents a single bond or divalent group shown by formulae (3). Each V independently represents a hydrogen atom or linking moiety.
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COMPOSITION FOR FORMING ORGANIC FILM, PATTERNING PROCESS, AND COMPOUND AND POLYMER FOR FORMING ORGANIC FILM
An organic film forming composition, containing: a material shown by formula (I) and/or (II); and an organic solvent, where R.sub.1 and R.sub.4 each represent a hydrogen atom, an allyl or propargyl group, R.sub.2 and R.sub.5 each represent a substituent, R.sub.3 and R.sub.6 represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an alkynyl group having 2 to 4 carbon atoms, or an alkenyl group having 2 to 4 carbon atoms. “m” and “i” represent 0 or 1, “k” and “q” represent an integer of 0 to 2, “n” represent 1 or 2, “h”, and “j” represent an integer of 0 to 2 and satisfy the relationship 1≤h+j≤4, and “1” and “r” represent 0 or 1. W represents a single bond or divalent group shown by formulae (3). Each V independently represents a hydrogen atom or linking moiety.
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