Patent classifications
C07D211/28
PROCESS AND INTERMEDIATES FOR MAKING TUBULYSIN ANALOGS
An improved process for making a compound B of the structure
##STR00001##
wherein n, R.sup.1, R.sup.2, and R.sup.3 are as defined in the specification. Compound B can be used to make tubulysin analogs that are, in turn, useful as anti-cancer agents, particularly when deployed in an antibody-drug conjugate.
AMINE-CONTAINING TRANSFECTION REAGENTS AND METHODS FOR MAKING AND USING SAME
There are provided for herein novel amine-containing transfection compounds and methods for making and using same. The compounds are generally obtained by reacting a primary amine with an unsaturated compound. Transfection complexes made using the amine-containing transfection compounds in combination with additional compounds to encapsulate biologically active agents such as nucleic acids are also provided for herein. Methods of using the transfection complexes for the in vivo or in vitro delivery of biologically active agents are also described. The transfection complexes of the present invention are highly potent, thereby allowing effective modulation of a biological activity at relatively low doses compared to analogous transfection compounds known in the art.
AMINE-CONTAINING TRANSFECTION REAGENTS AND METHODS FOR MAKING AND USING SAME
There are provided for herein novel amine-containing transfection compounds and methods for making and using same. The compounds are generally obtained by reacting a primary amine with an unsaturated compound. Transfection complexes made using the amine-containing transfection compounds in combination with additional compounds to encapsulate biologically active agents such as nucleic acids are also provided for herein. Methods of using the transfection complexes for the in vivo or in vitro delivery of biologically active agents are also described. The transfection complexes of the present invention are highly potent, thereby allowing effective modulation of a biological activity at relatively low doses compared to analogous transfection compounds known in the art.
ECTONUCLEOTIDE PYROPHOSPHATASE-PHOSPHODIESTERASE 1 (ENPP-1) INHIBITORS AND USES THEREOF
Disclosed herein are methods and compounds of augmenting and enhancing the production of type I IFNs in vivo. In some embodiments, the compounds disclosed herein are ENPP-1 inhibitors, pharmaceutical compositions, and methods for the treatment of cancer or a viral infection.
ECTONUCLEOTIDE PYROPHOSPHATASE-PHOSPHODIESTERASE 1 (ENPP-1) INHIBITORS AND USES THEREOF
Disclosed herein are methods and compounds of augmenting and enhancing the production of type I IFNs in vivo. In some embodiments, the compounds disclosed herein are ENPP-1 inhibitors, pharmaceutical compositions, and methods for the treatment of cancer or a viral infection.
Necrosis Inhibitors
The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
SMALL MOLECULES FOR CANCER THERAPY THAT REDUCE THE EXPRESSION OF TRANSCRIPTION FACTORS KLF5 AND EGR-1
The present disclosure provides compounds of formula (I), as described herein, their pharmaceutically acceptable salts, and their pharmaceutical compositions, which are effective in reducing the expression level of KLF5 or EGR1 in a living cell, and for the treatment of tumors and colorectal cancer in a human patient.
SMALL MOLECULES FOR CANCER THERAPY THAT REDUCE THE EXPRESSION OF TRANSCRIPTION FACTORS KLF5 AND EGR-1
The present disclosure provides compounds of formula (I), as described herein, their pharmaceutically acceptable salts, and their pharmaceutical compositions, which are effective in reducing the expression level of KLF5 or EGR1 in a living cell, and for the treatment of tumors and colorectal cancer in a human patient.
N-((1-BENZYLPIPERIDIN-3-YL)METHYL)-N-(2-METHOXYETHYL)NAPHTHALENE-2-SULFONAMIDE FOR THE TREATMENT OF CANINE COGNITIVE DYSFUNCTION AND OTHER FORMS OF DEMENTIA IN DOGS
The present invention relates to the fields of medicinal chemistry and veterinary medicine, and in particular to N-((1-benzylpiperidin-3-yl)methyl)-N-(2-methoxyethyl)naphthalene-2-sulfonamide as a pharmaceutically active compound. The compound of the present invention has been proven for the first time to be particularly useful for the treatment of canine cognitive dysfunction and other forms of dementia in dogs which may be therapeutically modified by altering the activity of butyrylcholinesterase.
N-((1-BENZYLPIPERIDIN-3-YL)METHYL)-N-(2-METHOXYETHYL)NAPHTHALENE-2-SULFONAMIDE FOR THE TREATMENT OF CANINE COGNITIVE DYSFUNCTION AND OTHER FORMS OF DEMENTIA IN DOGS
The present invention relates to the fields of medicinal chemistry and veterinary medicine, and in particular to N-((1-benzylpiperidin-3-yl)methyl)-N-(2-methoxyethyl)naphthalene-2-sulfonamide as a pharmaceutically active compound. The compound of the present invention has been proven for the first time to be particularly useful for the treatment of canine cognitive dysfunction and other forms of dementia in dogs which may be therapeutically modified by altering the activity of butyrylcholinesterase.