Patent classifications
C07C271/14
Photobase generators and photoresist compositions comprising same
New photobase generators suitable for use in photoresists are provided that correspond to Formula (I):
X.sub.1R.sub.1OC(O)N(R.sub.2)R.sub.3(I)
wherein X.sub.1 is an optionally substituted aromatic group; R.sub.1 is a linker; and R.sub.2 and R.sub.3 are the same or different optionally substituted linear, branched or cyclic aliphatic group or an optionally substituted aromatic group, wherein at least one of R.sub.2 and R.sub.3 is an optionally substituted branched alkyl group having 4 or more carbon atoms.
Photobase generators and photoresist compositions comprising same
New photobase generators suitable for use in photoresists are provided that correspond to Formula (I):
X.sub.1R.sub.1OC(O)N(R.sub.2)R.sub.3(I)
wherein X.sub.1 is an optionally substituted aromatic group; R.sub.1 is a linker; and R.sub.2 and R.sub.3 are the same or different optionally substituted linear, branched or cyclic aliphatic group or an optionally substituted aromatic group, wherein at least one of R.sub.2 and R.sub.3 is an optionally substituted branched alkyl group having 4 or more carbon atoms.
Organocatalytic asymmetric synthesis of antidepressants
The present invention relates to a short enantioselective synthesis of 1-amino aryl tetraline compounds of Formula 1 via nucleophilic enamine catalysis using organocatalyst such as proline. ##STR00001## wherein R.sub.1 and R.sub.2 represent independent of each other hydrogen, (un)substituted or substituted amine; R.sub.3 and R.sub.4 represent independent of each other hydrogen or halogen.
Organocatalytic asymmetric synthesis of antidepressants
The present invention relates to a short enantioselective synthesis of 1-amino aryl tetraline compounds of Formula 1 via nucleophilic enamine catalysis using organocatalyst such as proline. ##STR00001## wherein R.sub.1 and R.sub.2 represent independent of each other hydrogen, (un)substituted or substituted amine; R.sub.3 and R.sub.4 represent independent of each other hydrogen or halogen.
BETA-SUBSTITUTED BETA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS AND USES THEREOF
-Substituted -amino acids, -substituted -amino acid derivatives, and -substituted -amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the -substituted -amino acid derivatives and -substituted -amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.
BETA-SUBSTITUTED BETA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS AND USES THEREOF
-Substituted -amino acids, -substituted -amino acid derivatives, and -substituted -amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the -substituted -amino acid derivatives and -substituted -amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.
PROCESS FOR PREPARATION OF NITROGEN MUSTARD DERIVATIVES
The present invention provides a process for the production of compound (III) or a deprotected product thereof: comprising reacting compound (II) with chloroacetic acid, in the presence of a reducing agent; wherein PG is a protecting group and R is OH in a suitably protected form or (A). The invention further provides intermediate compounds formed in the process of the invention, and processes for the production of intermediate compounds.
##STR00001##
PROCESS FOR PREPARATION OF NITROGEN MUSTARD DERIVATIVES
The present invention provides a process for the production of compound (III) or a deprotected product thereof: comprising reacting compound (II) with chloroacetic acid, in the presence of a reducing agent; wherein PG is a protecting group and R is OH in a suitably protected form or (A). The invention further provides intermediate compounds formed in the process of the invention, and processes for the production of intermediate compounds.
##STR00001##
Compositions, methods and kits for treating a contact lens
Provided herein are fluorinated compounds having chemical structures: (I) where n is 0 or greater, or (II) where m and n are 0 or greater, or an amino acid, a soluble polymer, an oligo(ethylene glycol), a poly(ethylene glycol), or a carbohydrate each fluorinated with perfluorocarbons having the chemical structure (III) where n is 0 or greater. These fluorinated compounds are utilized in contact lenses to impart lipid-resistant, protein-resistant and biofouling-resistant properties, thus reducing discomfort and infection caused by contact lens wear without changing its transmission characteristics. Also provided is an ophthalmic drug delivery system comprising at least one of the compounds described above embedded in the contact lens and a kit to incorporate the ophthalmic into a contact lens. Methods for incorporating these compounds onto a contact lens without affecting transparency and for use in treating an ophthalmologic-associated condition are provided.
Compositions, methods and kits for treating a contact lens
Provided herein are fluorinated compounds having chemical structures: (I) where n is 0 or greater, or (II) where m and n are 0 or greater, or an amino acid, a soluble polymer, an oligo(ethylene glycol), a poly(ethylene glycol), or a carbohydrate each fluorinated with perfluorocarbons having the chemical structure (III) where n is 0 or greater. These fluorinated compounds are utilized in contact lenses to impart lipid-resistant, protein-resistant and biofouling-resistant properties, thus reducing discomfort and infection caused by contact lens wear without changing its transmission characteristics. Also provided is an ophthalmic drug delivery system comprising at least one of the compounds described above embedded in the contact lens and a kit to incorporate the ophthalmic into a contact lens. Methods for incorporating these compounds onto a contact lens without affecting transparency and for use in treating an ophthalmologic-associated condition are provided.