C07D239/86

Quinazoline derivatives substituted by aniline, preparation method and use thereof
09730934 · 2017-08-15 · ·

The invention relates to quinazoline derivatives substituted by aniline which are represented by the below formula (I), pharmaceutical acceptable salts and stereoisomer thereof, wherein these groups of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, L and n have the meanings given in the specification. The invention also relates to preparation methods, pharmaceutical compositions, pharmaceutical preparation and the use for preparation of medicine of treating excessive hyperplasia and chronic obstructive pulmonary disease and uses for treating excessive hyperplasia and chronic obstructive pulmonary disease thereof. ##STR00001##

Activators of autophagic flux and phospholipase D and clearance of protein aggregates including tau and treatment of proteinopathies

The present application discloses compounds which are activators of autophagic flux and pharmaceutical compositions comprising said activators. It further discloses use of said compounds and pharmaceutical compositions in the treatment of neurodegenerative diseases, particularly proteinopathies and tauopathies such as Alzheimer's disease. It further discloses methods of enhancing autophagic flux.

Activators of autophagic flux and phospholipase D and clearance of protein aggregates including tau and treatment of proteinopathies

The present application discloses compounds which are activators of autophagic flux and pharmaceutical compositions comprising said activators. It further discloses use of said compounds and pharmaceutical compositions in the treatment of neurodegenerative diseases, particularly proteinopathies and tauopathies such as Alzheimer's disease. It further discloses methods of enhancing autophagic flux.

ANTI-WOLBACHIA PYRIDO[2,3-d]PYRIMIDINECOMPOUNDS

The present invention relates to compounds of Formulae I and II as defined herein, and salts and solvates thereof.

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The present invention also relates to pharmaceutical compositions comprising compounds of Formulae I and II, and to the use of compounds of Formulae I and II in the treatment or prevention of filarial worm infection, as well as other diseases or conditions in which filarial worm infection is implicated.

ANTI-WOLBACHIA PYRIDO[2,3-d]PYRIMIDINECOMPOUNDS

The present invention relates to compounds of Formulae I and II as defined herein, and salts and solvates thereof.

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The present invention also relates to pharmaceutical compositions comprising compounds of Formulae I and II, and to the use of compounds of Formulae I and II in the treatment or prevention of filarial worm infection, as well as other diseases or conditions in which filarial worm infection is implicated.

Bicyclic-Fused Heteroaryl or Aryl Compounds

Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia,

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as defined in the specification. In an embodiment, a pharmaceutical composition can be in a liquid dosage form and can comprise a therapeutically effective amount of the compound or a pharmaceutically acceptable salt thereof as an adjuvant and a therapeutic agent. In another embodiment, a method of adjuvant treating a disorder or condition can comprising administering the pharmaceutical composition to a patient.

Bicyclic-Fused Heteroaryl or Aryl Compounds

Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia,

##STR00001##

as defined in the specification. In an embodiment, a pharmaceutical composition can be in a liquid dosage form and can comprise a therapeutically effective amount of the compound or a pharmaceutically acceptable salt thereof as an adjuvant and a therapeutic agent. In another embodiment, a method of adjuvant treating a disorder or condition can comprising administering the pharmaceutical composition to a patient.

NOVEL CDK 8/19 INHIBITORS

The present invention relates to novel compounds of formula (1), which have the properties of a CDK8/19 inhibitor, and to a pharmaceutical composition containing said compounds, and to the use of said compounds and composition as pharmaceutical preparations for treating diseases or disorders.

4,6-DI- AND 2,4,6-TRISUBSTITUTED QUINAZOLINE DERIVATIVES USEFUL FOR TREATING VIRAL INFECTIONS

This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R.sub.2 is hydrogen, NR′R″, C.sub.1-7alkyl, arylC.sub.1-7 alkyl or C.sub.3-10 cycloalkyl; R.sub.4 is amino, C.sub.1-7alkyl, C.sub.2-7 alkenyl, C.sub.3-10 cycloalkyl, C.sub.3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C.sub.1-7alkyl or C.sub.3-10 cycloalkyl-C.sub.1-7 alkyl; R.sub.5 is hydrogen or C.sub.1-7 alkyl, or R.sub.5 and R.sub.4 together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, C.sub.1-7alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene; R.sub.6 is halogen, heteroaryl or aryl; R′ and R″ are each independently hydrogen, C.sub.1-7 alkyl-carbonyl or C.sub.1-7 alkyl; provided that R.sub.4 is not phenyl substituted with morpholino when R.sub.2 is H and R.sub.5 is H, and provided that when NR.sub.4R.sub.5 is piperazinyl, said NR.sub.4R.sub.5 is either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.

4,6-DI- AND 2,4,6-TRISUBSTITUTED QUINAZOLINE DERIVATIVES USEFUL FOR TREATING VIRAL INFECTIONS

This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R.sub.2 is hydrogen, NR′R″, C.sub.1-7alkyl, arylC.sub.1-7 alkyl or C.sub.3-10 cycloalkyl; R.sub.4 is amino, C.sub.1-7alkyl, C.sub.2-7 alkenyl, C.sub.3-10 cycloalkyl, C.sub.3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C.sub.1-7alkyl or C.sub.3-10 cycloalkyl-C.sub.1-7 alkyl; R.sub.5 is hydrogen or C.sub.1-7 alkyl, or R.sub.5 and R.sub.4 together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, C.sub.1-7alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene; R.sub.6 is halogen, heteroaryl or aryl; R′ and R″ are each independently hydrogen, C.sub.1-7 alkyl-carbonyl or C.sub.1-7 alkyl; provided that R.sub.4 is not phenyl substituted with morpholino when R.sub.2 is H and R.sub.5 is H, and provided that when NR.sub.4R.sub.5 is piperazinyl, said NR.sub.4R.sub.5 is either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.