摘要:
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.
摘要:
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.
摘要:
β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-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 β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-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 β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.
摘要:
Disclosed herein are convenient, industrially advantageous and environmentally friendly processes for the preparation of cinacalcet hydrochloride. Disclosed also herein are novel hydrochloride, oxalate and di-p-toluoyl-L-(+)-tartrate salts of (R)-α-methyl-N-[3-[3-(trifluoromethyl)phenyl]propylene]-1-naphthalenemethaneamine (unsaturated cinacalcet), solid state forms of the salts, and a process for their preparation thereof.
摘要:
The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.
摘要:
Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
摘要:
Provided is a compound having one or more structures of the formula: 1 wherein X is a primary carbamate group, Y is a hydroxy or halide group, n is an integer of 2 or more, nnull is an integer of 1 or more, and R0, R1, R2, R3, R4 and R5 may be H or a group selected from alkyl groups, aliphatic groups, cycloaliphatic groups, aromatic groups and mixtures thereof, with the provisos that at least one R1 or R2 group is selected from the group consisting of aliphatic groups, cycloaliphatic groups, and aromatic groups, and in substantially all structures primary carbamate group X is attached to a carbon atom having a lower degree of substitution than a carbon atom to which functional group Y is attached. The invention provides a method of making the claimed compound.
摘要:
Per(poly)fluorinated polyoxyethylated carbamates of general formula (I) in which R.sub.F represents a perfluorinated group containing between 1 and 18 carbon atoms, W represents an oxo group or nothing, n is an integer from 1 to 10, m is from values 2 to 6, 80 or not defined, R is an alkyl group, R.sub.F W(CH.sub.2).sub.n+1 NHC(O)-- in which R.sub.F and W are as defined above, --(CHCH.sub.3 CH.sub.2 O).sub.30 (CH.sub.2 CH.sub.2).sub.80 C(O)NH(CH.sub.2).sub.n+1 R.sub.F in which R.sub.F is a perfluorinated group containing from 1 to 18 carbon atoms, R' is a hydrogen atom, an alkyl group containing between 1 and 18 carbon atoms which is optionally substituted, an optionally substituted aryl or aralkyl group, an allyl, methallyl or propargyl group or a perfluorinated chain having between 1 and 18 carbon atoms. These compounds can be used as anti-thrombosis agents or as surfactants or cosurfactants for phospholipids intended for the preparation or stabilization of fluorocarbon emulsions, notably emulsions for biomedical applications.
摘要:
Novel monoamine oxidase B inhibitors of formula (I), wherein R.sub.1 .dbd.H, an optionally substituted benzyloxy or phenylethoxy group; p=0-3; R.sub.3 .dbd.H, a CN, OH, CCH group, a C.sub.1 -C.sub.3 alkoxy-carbonyl group, or a C.sub.1 -C.sub.3 alkylated cyanomethyl group; R.sub.2 .dbd.H or a C.sub.1 -C.sub.3 alkyl group; n=0 or 1; if n=0, R.sub.4 is a C.sub.1 -C.sub.3 alkyl group or a C.sub.1 -C.sub.3 alkoxy group, while if n=1, y=1 and R.sub.4 is a C.sub.1 -C.sub.3 alkyl group, a C.sub.1 -C.sub.3 alkoxy group or a phenyl group. The invention also concerns processes for the preparation of said novel inhibitors and the therapeutic use thereof. ##STR1##
摘要:
Aromatic amides of poly(oxyalkylene) carbamates having the formula: ##STR1## or a fuel-soluble salt thereof; wherein A, R.sub.1 -R.sub.10, x, y, and z are as defined herein.