Patent classifications
C07D309/30
HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES
The present invention relates to novel hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, pancreatitius, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES
The present invention relates to novel hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, pancreatitius, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
CHIRAL-SUBSTITUTED POLY-N-VINYLPYRROLIDINONES AND COMPLEXES WITH BIMETALLIC NANOCLUSTERS AND USES THEREOF IN ASYMMETRIC OXIDATION REACTIONS
Chiral polyvinylpyrrolidinone (CSPVP), complexes of CSPVP with a core species, such as a bimetallic nanocluster catalyst, and enantioselective oxidation reactions utilizing such complexes are disclosed. The catalytic complexes have exhibited the ability to achieve reaction products have a very high degree of optical purifies. These reaction products can be used as reagents in the synthesis of complex organic molecules, such as bioactive products, and C—H bond oxidation of complex molecules including various drugs and natural products.
CHIRAL-SUBSTITUTED POLY-N-VINYLPYRROLIDINONES AND COMPLEXES WITH BIMETALLIC NANOCLUSTERS AND USES THEREOF IN ASYMMETRIC OXIDATION REACTIONS
Chiral polyvinylpyrrolidinone (CSPVP), complexes of CSPVP with a core species, such as a bimetallic nanocluster catalyst, and enantioselective oxidation reactions utilizing such complexes are disclosed. The catalytic complexes have exhibited the ability to achieve reaction products have a very high degree of optical purifies. These reaction products can be used as reagents in the synthesis of complex organic molecules, such as bioactive products, and C—H bond oxidation of complex molecules including various drugs and natural products.
RESIST COMPOSITION, METHOD OF FORMING RESIST PATTERN, COMPOUND, AND RESIN
A resist composition containing a polymeric compound having a constitutional unit (a01) derived from a compound represented by General Formula (a0-1). In the formula, represents a polymerizable group-containing group, Ra.sup.01 represents a linear or branched hydrocarbon group, and Ra.sup.02 and Ra.sup.03 each independently represents a hydrocarbon group which may have a substituent
##STR00001##
ANTIBODY DRUG CONJUGATES
Drug conjugates of formula [D-(X).sub.b-(AA).sub.w-(L)-].sub.n-Ab wherein: D is a drug moiety having the following formula (I) or a pharmaceutically acceptable salt, ester, solvate, tautomer or stereoisomer thereof, wherein:
##STR00001## A is selected from
##STR00002## R.sub.1, R.sub.2 and R.sub.3 is H, OR.sub.a, OCOR.sub.a, OCOOR.sub.a, alkyl, alkenyl, alkynyl, etc; R.sub.3′ is, COR.sub.a, COOR.sub.a, CONR.sub.aR.sub.b, etc; each of R.sub.4to R.sub.10 and R.sub.12 is alkyl, alkenyl or alkynyl; R.sub.11 is H, COR.sub.a, COOR.sub.a, alkyl, alkenyl or alkynyl, or R.sub.11 and R.sub.12+N+C atoms to which they are attached may form a heterocyclic group; each of R.sub.13 and R.sub.14 is H, COR.sub.a, COOR.sub.a, alkyl, alkenyl or alkynyl; each R.sub.a and R.sub.b is H, alkyl, alkenyl, alkynyl, etc.; each dotted line represents an optional additional bond; X is an extending group; AA is an amino acid unit; L is a linker group; w is 0 to 12; b is 0 or 1; Ab is a moiety comprising at least one antigen binding site, and n is the ratio of the group [D-(X).sub.b-(AA).sub.w-(L)-] to the moiety comprising at least one antigen binding site and is in the range from 1 to 20, are useful in the treatment of cancer.
ANTIBODY DRUG CONJUGATES
Drug conjugates of formula [D-(X).sub.b-(AA).sub.w-(L)-].sub.n-Ab wherein: D is a drug moiety having the following formula (I) or a pharmaceutically acceptable salt, ester, solvate, tautomer or stereoisomer thereof, wherein:
##STR00001## A is selected from
##STR00002## R.sub.1, R.sub.2 and R.sub.3 is H, OR.sub.a, OCOR.sub.a, OCOOR.sub.a, alkyl, alkenyl, alkynyl, etc; R.sub.3′ is, COR.sub.a, COOR.sub.a, CONR.sub.aR.sub.b, etc; each of R.sub.4to R.sub.10 and R.sub.12 is alkyl, alkenyl or alkynyl; R.sub.11 is H, COR.sub.a, COOR.sub.a, alkyl, alkenyl or alkynyl, or R.sub.11 and R.sub.12+N+C atoms to which they are attached may form a heterocyclic group; each of R.sub.13 and R.sub.14 is H, COR.sub.a, COOR.sub.a, alkyl, alkenyl or alkynyl; each R.sub.a and R.sub.b is H, alkyl, alkenyl, alkynyl, etc.; each dotted line represents an optional additional bond; X is an extending group; AA is an amino acid unit; L is a linker group; w is 0 to 12; b is 0 or 1; Ab is a moiety comprising at least one antigen binding site, and n is the ratio of the group [D-(X).sub.b-(AA).sub.w-(L)-] to the moiety comprising at least one antigen binding site and is in the range from 1 to 20, are useful in the treatment of cancer.
Spontaneous alignment assistant for liquid crystal compositions
The spontaneous orientation aid for a liquid crystal composition provides storage stability and allows liquid crystal molecules to be vertically aligned without a PI layer when added to a liquid crystal composition. When used in a liquid crystal composition, the spontaneous orientation aid can adsorb to substrates sandwiching a liquid crystal composition (liquid crystal layer) and keep the liquid crystal molecules aligned in a vertical direction. The spontaneous orientation aid makes it possible to align liquid crystal molecules without a PI layer (to induce vertical alignment of liquid crystal molecules under no applied voltage and to achieve horizontal alignment of the liquid crystal molecules under an applied voltage).
Spontaneous alignment assistant for liquid crystal compositions
The spontaneous orientation aid for a liquid crystal composition provides storage stability and allows liquid crystal molecules to be vertically aligned without a PI layer when added to a liquid crystal composition. When used in a liquid crystal composition, the spontaneous orientation aid can adsorb to substrates sandwiching a liquid crystal composition (liquid crystal layer) and keep the liquid crystal molecules aligned in a vertical direction. The spontaneous orientation aid makes it possible to align liquid crystal molecules without a PI layer (to induce vertical alignment of liquid crystal molecules under no applied voltage and to achieve horizontal alignment of the liquid crystal molecules under an applied voltage).
Derivatives of korormicin useful as antibiotics
Described herein is a process for antibiotic development comprising: (a) generating a compound of formula (III): ##STR00001##
or a salt or stereoisomer or prodrug thereof; wherein R.sup.1-R.sup.3 and R.sup.5-R.sup.10 are independently selected from H, alkyl group, substituted alkyl group, halogen, OH, NH.sub.2, or SH; R.sup.4 is H, alkyl group or substituted alkyl group; X.sup.1-X.sup.2 are independently selected from ═O, ═S, ═NH, H, alkyl, halogen, OH, SH, or NH.sub.2; W is a saturated acyclic hydrocarbon chain of 1 to 15 carbon atoms; and Z is a neutral or positively charged organic group comprising a nitrogen or phosphorus atom; and; and (b) determining efficacy of the compound to inhibit growth of a bacteria. Systems of drug development of these antibiotic compounds are also described.