Patent classifications
C07C323/32
SPHINGOSINE KINASE TYPE 1 INHIBITORS AND USES THEREOF
Provided are inhibitors of sphingosine kinase Type I that are useful in a number of applications, indications and diseases, as well as for monitoring pharmacokinetics and patient management. These compounds are applicable to treating tumors of the central nervous system, such as glioblastoma multiforme (GBM).
SPHINGOSINE KINASE TYPE 1 INHIBITORS AND USES THEREOF
Provided are inhibitors of sphingosine kinase Type I that are useful in a number of applications, indications and diseases, as well as for monitoring pharmacokinetics and patient management. These compounds are applicable to treating tumors of the central nervous system, such as glioblastoma multiforme (GBM).
NON-HALLUCINOGENIC ARIADNE ANALOGS FOR TREATMENT OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS
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.
NON-HALLUCINOGENIC ARIADNE ANALOGS FOR TREATMENT OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS
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.
Phenoxy acetic acids and phenyl propionic acids as PPAR delta agonists
Phenoxy acetic acids and phenyl propionic acids and their use in improving mitochondrial energy output in a subject are provided herein. The present compounds are activators of PPAR and may be useful for treating conditions mediated by the same.
Phenoxy acetic acids and phenyl propionic acids as PPAR delta agonists
Phenoxy acetic acids and phenyl propionic acids and their use in improving mitochondrial energy output in a subject are provided herein. The present compounds are activators of PPAR and may be useful for treating conditions mediated by the same.
Sphingosine kinase type 1 inhibitors and uses thereof
Provided are inhibitors of sphingosine kinase Type I and their use in the treatment of asthma, among other indications and diseases.
Sphingosine kinase type 1 inhibitors and uses thereof
Provided are inhibitors of sphingosine kinase Type I and their use in the treatment of asthma, among other indications and diseases.
PHENALKYLAMINES AND METHODS OF MAKING AND USING THE SAME
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.
PHENALKYLAMINES AND METHODS OF MAKING AND USING THE SAME
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.