Patent classifications
C07D265/32
AMINO ACID-, PEPTIDE- AND POLYPEPTIDE-LIPIDS, ISOMERS, COMPOSITIONS, AND USES THEREOF
Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein:
##STR00001##
wherein m, n, p, R′, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.8, Z, W, Y, and Z are as defined herein.
AMINO ACID-, PEPTIDE- AND POLYPEPTIDE-LIPIDS, ISOMERS, COMPOSITIONS, AND USES THEREOF
Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein:
##STR00001##
wherein m, n, p, R′, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.8, Z, W, Y, and Z are as defined herein.
NURR1 RECEPTOR MODULATORS
Described herein, inter alia, are Nurr1 receptor modulators and uses thereof. In an aspect is provided a method for treating a disease associated with dysregulation and/or degeneration of dopaminergic neurons in the central nervous system of a subject in need thereof, the method including administering to the subject in need thereof a therapeutically effective amount of a compound described herein.
NURR1 RECEPTOR MODULATORS
Described herein, inter alia, are Nurr1 receptor modulators and uses thereof. In an aspect is provided a method for treating a disease associated with dysregulation and/or degeneration of dopaminergic neurons in the central nervous system of a subject in need thereof, the method including administering to the subject in need thereof a therapeutically effective amount of a compound described herein.
SUBSTITUTED NAPHTHYL P38ALPHA MITOGEN-ACTIVATED PROTEIN KINASE INHIBITORS
Substituted naphthyl p38α mitogen-activated protein kinase inhibitors, pharmaceutical compositions thereof, and the use of the substituted naphthyl p38α mitogen-activated protein kinase inhibitors and pharmaceutical compositions thereof for treating diseases are disclosed.
SUBSTITUTED NAPHTHYL P38ALPHA MITOGEN-ACTIVATED PROTEIN KINASE INHIBITORS
Substituted naphthyl p38α mitogen-activated protein kinase inhibitors, pharmaceutical compositions thereof, and the use of the substituted naphthyl p38α mitogen-activated protein kinase inhibitors and pharmaceutical compositions thereof for treating diseases are disclosed.
Method of improving cognition and social behavior in humans having deficits therein due to neurodegenerative disorders and compounds and compositions therefor
A β.sub.1-ADR agonist prodrug compound, which is hydrolysable in vivo to release a β1-ADR agonist compound, and which prodrug compound contains a group which imparts greater lipophilicity and CNS bioavailability to the prodrug compound relative to the β1-ADR agonist compound.
PRODRUGS OF ALPHA-KETOGLUTARATE, ALPHA-KETOBUTYRATE, ALPHA-KETOISOVALERATE, AND ALPHA-KETOISOHEXANOATE, AND USES THEREOF
The present disclosure provides compounds and compositions capable of extending lifespan, and methods of use thereof.
PROCESS FOR PREPARING A POLYMORPH OF RIVAROXABAN
This invention describes a process for the preparation of rivaroxaban modification I comprising: (i) dissolving rivaroxaban in a mixture of a solvent (e.g. THF) and an antisolvent (e.g. water and/or toluene), wherein the antisolvent has a higher boiling point than the solvent; (ii) removing the solvent by distillation; and (iii) collecting the resultant rivaroxaban modification I.
PROCESS FOR PREPARING A POLYMORPH OF RIVAROXABAN
This invention describes a process for the preparation of rivaroxaban modification I comprising: (i) dissolving rivaroxaban in a mixture of a solvent (e.g. THF) and an antisolvent (e.g. water and/or toluene), wherein the antisolvent has a higher boiling point than the solvent; (ii) removing the solvent by distillation; and (iii) collecting the resultant rivaroxaban modification I.