Patent classifications
C07D309/06
SSAO INHIBITORS AND USE THEREOF
The application relates to a compound of Formula (I′) or (I):
##STR00001##
or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of SSAO, a pharmaceutical composition comprising a compound of Formula (I′) or (I), and a method of treating or preventing a disease in which SSAO plays a role.
SSAO INHIBITORS AND USE THEREOF
The application relates to a compound of Formula (I′) or (I):
##STR00001##
or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of SSAO, a pharmaceutical composition comprising a compound of Formula (I′) or (I), and a method of treating or preventing a disease in which SSAO plays a role.
Methods for the treatment of diabetic retinopathy and other ophthalmic diseases
Methods are provided herein for the treatment of ophthalmic diseases or conditions such as an ophthalmic disease or disorder associated with diabetes in a patient. Also provided herein are methods of treating retinopathy of prematurity in a patient. Further, provided herein are methods for treating wet age-related macular degeneration in a patient. The methods comprise administration of compounds disclosed herein to a patient in need thereof that inhibit or slow one or more signs or symptoms of such conditions.
Methods for the treatment of diabetic retinopathy and other ophthalmic diseases
Methods are provided herein for the treatment of ophthalmic diseases or conditions such as an ophthalmic disease or disorder associated with diabetes in a patient. Also provided herein are methods of treating retinopathy of prematurity in a patient. Further, provided herein are methods for treating wet age-related macular degeneration in a patient. The methods comprise administration of compounds disclosed herein to a patient in need thereof that inhibit or slow one or more signs or symptoms of such conditions.
KETONE SYNTHESIS AND APPLICATIONS
Provided are new nickel./zirconium-mediated coupling reactions useful in the synthesis of ketone-containing compounds, e.g., halichondrin natural products and related molecules. A feature of the present disclosure is the use of a nickel(I) catalyst in tandem with a nickel (II) catalyst in the Ni/Zr-mediated coupling reactions. Without wishing to be bound by any particular theory, the nickel (I) catalyst selectively activates the electrophilic coupling partner (i.e., the compound of Formula (A)), and the nickel(ll) catalyst selectively activates the nucleophilic coupling partner (i.e., a thioester of Formula (B)). This dual catalyst system leads to improved coupling efficiency and eliminates the need for a large excess of one of the coupling partners (i.e., a compound of Formula (A) or (B)).
Processes for preparing a 3-isopropenyl-6-heptenal compound and a 6- isopropenyl-3-methyl-3,9-decadienyl carboxylate compound, and an intermediate therefor
The present invention relates to a process for preparing a 3-isopropenyl-6-heptenal compound of the following formula (2): wherein R.sup.1 represents a hydrogen atom or a methyl group, the process comprising: subjecting a 3-isopropenyl-6-heptenoate ester compound of the following formula (1): wherein R.sup.1 is as defined above, and R.sup.2 represents a monovalent hydrocarbon group having 1 to 10 carbon atoms, to a reduction reaction with a reducing agent to form the 3-isopropenyl-6-heptenal compound (2). ##STR00001##
COMPOUNDS FOR INCREASING THE NICOTINAMIDE ADENINE DINUCLEOTIDE IN A SUBJECT AND METHODS OF USE THEREOF
In accordance with the purpose(s) of the present disclosure, as embodied and broadly described herein, the disclosure, in one aspect, relates to compounds that increase the amount of nicotinamide adenine dinucleotide (NAD.sup.+) in a subject. By raising the amount of nicotinamide adenine dinucleotide in a subject, diseases associated with reduced levels of nicotinamide adenine dinucleotide can be treated or prevented. In one aspect, raising the amount of NAD.sup.+ in a subject can reduce or ameliorate one or more symptoms of Parkinson’s disease, Alzheimer’s disease, Huntington’s disease, multiple sclerosis, amylotrophic lateral sclerosis, AIDS-induced dementia, or epilepsy.
COMPOUNDS FOR INCREASING THE NICOTINAMIDE ADENINE DINUCLEOTIDE IN A SUBJECT AND METHODS OF USE THEREOF
In accordance with the purpose(s) of the present disclosure, as embodied and broadly described herein, the disclosure, in one aspect, relates to compounds that increase the amount of nicotinamide adenine dinucleotide (NAD.sup.+) in a subject. By raising the amount of nicotinamide adenine dinucleotide in a subject, diseases associated with reduced levels of nicotinamide adenine dinucleotide can be treated or prevented. In one aspect, raising the amount of NAD.sup.+ in a subject can reduce or ameliorate one or more symptoms of Parkinson’s disease, Alzheimer’s disease, Huntington’s disease, multiple sclerosis, amylotrophic lateral sclerosis, AIDS-induced dementia, or epilepsy.
CXCR6 SULFONAMIDE COMPOUNDS
Provided are sulfonamide compounds having formula (I):
##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and the subscripts n and m have the meanings provided in the specification. The compounds are useful for treating diseases and conditions associated with CXCR6 activity.
CXCR6 SULFONAMIDE COMPOUNDS
Provided are sulfonamide compounds having formula (I):
##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and the subscripts n and m have the meanings provided in the specification. The compounds are useful for treating diseases and conditions associated with CXCR6 activity.