The present invention relates to new benzoquinolone inhibitors of VMAT2, pharmaceutical compositions thereof, and methods of use thereof.

##STR00001##

Provided herein are compounds of Formula (I), or pharmaceutically acceptable salt thereof, wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and n are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof, and methods of using a compound of Formula (I) or pharmaceutically acceptable salt thereof, e.g., in the treatment of a mental health disease or disorder. ##STR00001##

The present invention provides a compound having the structure:

##STR00001## wherein R.sub.1 is (C.sub.2-C.sub.12 alkyl), -(alkenyl), -(alkynyl), -(cycloalkyl); R.sub.2 is H, halogen, NO.sub.2, CN, CF.sub.3, CF.sub.2H, CH.sub.2OCH.sub.3, CF.sub.2CH.sub.3, CF.sub.2OCH.sub.3, -(alkyl), -(alkenyl), -(alkynyl), -(cycloalkyl), -(cycloalkylalkyl), -(heteroalkyl), -(heterocycle), -(heterocycloalkyl), -(aryl), -(heteroaryl), -(hydroxyalkyl), -(haloalkyl), -(alkylaryl), OH, O-(alkyl), O-(alkenyl), O-(alkynyl), O-(haloalkyl), O-(aryl), O-(heteroaryl), OCF.sub.3, SH, S-(alkyl), S-(alkenyl), S-(alkynyl), S-(aryl), S-(heteroaryl), NH.sub.2, NH-(alkyl), NH-(alkenyl), NH-(alkynyl), N-(alkyl).sub.2, NH-(aryl), NH-(heteroaryl), CO.sub.2H, CO.sub.2-(alkyl), C(O)NH.sub.2, C(O)NH-(alkyl), C(O)NH-(aryl), SO.sub.2CH.sub.3 or Si(CH.sub.3) .sub.3; R.sub.3 is OCH.sub.3, OCH.sub.2CH.sub.3, F or Cl; and R.sub.4 is OCH.sub.3, OCH.sub.2CH.sub.3 or SCH.sub.3; wherein when R.sub.1 is CH.sub.2CH.sub.3, R.sub.3 is OCH.sub.3, and R.sub.4 is OCH.sub.3, then R.sub.2 is other than H, CH.sub.3, CH.sub.2CH.sub.3, CH.sub.2CH.sub.2CH.sub.3, CH(CH.sub.3).sub.2, CH.sub.2CH.sub.2CH.sub.2CH.sub.3, CH.sub.2OH, CH(OH) CH.sub.3, OH, OCH.sub.2CH.sub.3, OCH.sub.2CH.sub.2CH.sub.3, OCH(CH.sub.3).sub.2, SCH.sub.3, SCH.sub.2CH.sub.3, SCH.sub.2CH.sub.2CH.sub.3, NO.sub.2, NH.sub.2, F, Cl, Br or I,
or a pharmaceutically acceptable salt thereof.

The present invention provides a compound having the structure:

##STR00001## wherein R.sub.1 is (C.sub.2-C.sub.12 alkyl), -(alkenyl), -(alkynyl), -(cycloalkyl); R.sub.2 is H, halogen, NO.sub.2, CN, CF.sub.3, CF.sub.2H, CH.sub.2OCH.sub.3, CF.sub.2CH.sub.3, CF.sub.2OCH.sub.3, -(alkyl), -(alkenyl), -(alkynyl), -(cycloalkyl), -(cycloalkylalkyl), -(heteroalkyl), -(heterocycle), -(heterocycloalkyl), -(aryl), -(heteroaryl), -(hydroxyalkyl), -(haloalkyl), -(alkylaryl), OH, O-(alkyl), O-(alkenyl), O-(alkynyl), O-(haloalkyl), O-(aryl), O-(heteroaryl), OCF.sub.3, SH, S-(alkyl), S-(alkenyl), S-(alkynyl), S-(aryl), S-(heteroaryl), NH.sub.2, NH-(alkyl), NH-(alkenyl), NH-(alkynyl), N-(alkyl).sub.2, NH-(aryl), NH-(heteroaryl), CO.sub.2H, CO.sub.2-(alkyl), C(O)NH.sub.2, C(O)NH-(alkyl), C(O)NH-(aryl), SO.sub.2CH.sub.3 or Si(CH.sub.3) .sub.3; R.sub.3 is OCH.sub.3, OCH.sub.2CH.sub.3, F or Cl; and R.sub.4 is OCH.sub.3, OCH.sub.2CH.sub.3 or SCH.sub.3; wherein when R.sub.1 is CH.sub.2CH.sub.3, R.sub.3 is OCH.sub.3, and R.sub.4 is OCH.sub.3, then R.sub.2 is other than H, CH.sub.3, CH.sub.2CH.sub.3, CH.sub.2CH.sub.2CH.sub.3, CH(CH.sub.3).sub.2, CH.sub.2CH.sub.2CH.sub.2CH.sub.3, CH.sub.2OH, CH(OH) CH.sub.3, OH, OCH.sub.2CH.sub.3, OCH.sub.2CH.sub.2CH.sub.3, OCH(CH.sub.3).sub.2, SCH.sub.3, SCH.sub.2CH.sub.3, SCH.sub.2CH.sub.2CH.sub.3, NO.sub.2, NH.sub.2, F, Cl, Br or I,
or a pharmaceutically acceptable salt thereof.

The present invention comprises novel aromatic molecules, which can be used in the treatment of pathological conditions, such as cancer, skin diseases, muscle disorders, and immune system-related disorders such as disorders of the haematopoietic system including the haematologic system in human and veterinary medicine.

##STR00001##

The present invention comprises novel aromatic molecules, which can be used in the treatment of pathological conditions, such as cancer, skin diseases, muscle disorders, and immune system-related disorders such as disorders of the haematopoietic system including the haematologic system in human and veterinary medicine.

##STR00001##

This present disclosure is directed to compounds of formula (I): ##STR00001## where r, q, R.sup.1a, R.sup.1b, R.sup.1c, R.sup.1d, R.sup.1e, R.sup.2, R.sup.3, R.sup.4a, R.sup.5a, R.sup.5b, R.sup.6a, R.sup.6b, R.sup.8, and R.sup.9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A.sub.4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions including the compounds described herein and methods of preparing the compounds described herein are also provided.

This present disclosure is directed to compounds of formula (I): ##STR00001## where r, q, R.sup.1a, R.sup.1b, R.sup.1c, R.sup.1d, R.sup.1e, R.sup.2, R.sup.3, R.sup.4a, R.sup.5a, R.sup.5b, R.sup.6a, R.sup.6b, R.sup.8, and R.sup.9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A.sub.4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions including the compounds described herein and methods of preparing the compounds described herein are also provided.

The present disclosure provides phenalkylamine compounds and their use in treating medical disorders, such as psychiatric diseases and disorders. Pharmaceutical compositions and methods of making various phenalkylamine compounds are provided.

The present disclosure provides phenalkylamine compounds and their use in treating medical disorders, such as psychiatric diseases and disorders. Pharmaceutical compositions and methods of making various phenalkylamine compounds are provided.