Patent classifications
A61K31/396
Substituted Phenyl Aziridine Precursor Analogs for Inhibiting Androgen-Independent Prostate Cancer Cell Growth
Disclosed are methods and pharmaceutical compositions for modulating one or more steroidal receptor activities. The methods typically utilize and the pharmaceutical compositions typically include one or more substituted phenyl aziridine precursors, their respective aziridines, analogs thereof, derivatives thereof, or pharmaceutically acceptable salts thereof such as CpdA. The methods and compositions may be used for treating diseases, disorders, and conditions associated with glucocorticoid receptor activity, androgen receptor activity, or both, such as cancers, acne vulgaris, and alopecia.
Pharmaceutical composition for treating fibrosis
To provide a novel therapeutic agent for fibrosis that induces selective cell death of lung fibroblasts and suppresses lung fibrosis without injuring alvocar epithelial cells. A pharmaceutical composition for treating fibrosis, the pharmaceutical composition comprising a compound of formula (I) or formula (II): ##STR00001## wherein in formula (I), R.sup.1 represents a C.sub.1-4 alkyl group optionally substituted with a halogen atom, and l represents an integer of 3 to 6; and in formula (II), n represents an integer of 8 to 12,
or a pharmaceutically acceptable salt thereof or a solvate of the compound or the salt thereof.
ANTI-FUNGALS COMPOUNDS TARGETING THE SYNTHESIS OF FUNGAL SPHINGOLIPIDS
The present invention provides a compound having the structure:
##STR00001## wherein R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 are each independently, H, halogen, CN, CF.sub.3, OCF.sub.3, NO.sub.2, alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocycle, OH, OAc, OR.sub.13, COR.sub.13, CH.sub.2OR.sub.13, SH, SR.sub.13, SO.sub.2R.sub.13, NH.sub.2, NHR.sub.13, NR.sub.14R.sub.15, NHCOR.sub.12, or CONR.sub.14R.sub.15; R.sub.9, R.sub.10, R.sub.11, and R.sub.12 are each independently, H, CN, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, OAc, COR.sub.13, SH, SR.sub.13, SO.sub.2R.sub.13, NH.sub.2, NHR.sub.13, NR.sub.14R.sub.15, NHCOR.sub.12, or CONR.sub.14R.sub.15; wherein each occurrence of R.sub.13 is independently alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R.sub.14 is independently H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R.sub.15 is independently H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein when R.sub.14 is methyl, R.sub.15 is not methyl; wherein at least one of R.sub.9, R.sub.10, R.sub.11, and R.sub.12 is not H; wherein at least one of R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 is not H.
ANTI-FUNGALS COMPOUNDS TARGETING THE SYNTHESIS OF FUNGAL SPHINGOLIPIDS
The present invention provides a compound having the structure:
##STR00001## wherein R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 are each independently, H, halogen, CN, CF.sub.3, OCF.sub.3, NO.sub.2, alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocycle, OH, OAc, OR.sub.13, COR.sub.13, CH.sub.2OR.sub.13, SH, SR.sub.13, SO.sub.2R.sub.13, NH.sub.2, NHR.sub.13, NR.sub.14R.sub.15, NHCOR.sub.12, or CONR.sub.14R.sub.15; R.sub.9, R.sub.10, R.sub.11, and R.sub.12 are each independently, H, CN, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, OAc, COR.sub.13, SH, SR.sub.13, SO.sub.2R.sub.13, NH.sub.2, NHR.sub.13, NR.sub.14R.sub.15, NHCOR.sub.12, or CONR.sub.14R.sub.15; wherein each occurrence of R.sub.13 is independently alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R.sub.14 is independently H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R.sub.15 is independently H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein when R.sub.14 is methyl, R.sub.15 is not methyl; wherein at least one of R.sub.9, R.sub.10, R.sub.11, and R.sub.12 is not H; wherein at least one of R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 is not H.
NOVEL ANTI-FIBROTIC DRUGS
The present invention relates to new cinnamic add amides which may be used for treatment of fibrosis and neoplasia and to cinnamic acid amides for use in the treatment of fibrosis, neoplasia, arthrolithiasis, familiar mediterranean fever and pericarditis. Further, the invention relates to a pharmaceutical composition comprising said cinnamic acid amides and to a screening essay for identifying compounds suitable for the treatment of fibrosis.
NOVEL ANTI-FIBROTIC DRUGS
The present invention relates to new cinnamic add amides which may be used for treatment of fibrosis and neoplasia and to cinnamic acid amides for use in the treatment of fibrosis, neoplasia, arthrolithiasis, familiar mediterranean fever and pericarditis. Further, the invention relates to a pharmaceutical composition comprising said cinnamic acid amides and to a screening essay for identifying compounds suitable for the treatment of fibrosis.
PHOTOCROSSLINKING REAGENTS AND METHODS OF USE THEREOF
Provided herein are photocrosslinking reagents, crosslinkable proteins displaying photocrosslinking groups, crosslinked protein-protein complexes, and methods of use thereof.
AZIRIDINE CONTAINING DNA ALKYLATING AGENTS
Provided herein are compounds of formula (I)-(VI), wherein the variables are defined herein, processes of making them, and methods of treating cancer comprising administering such compounds.
AZIRIDINE CONTAINING DNA ALKYLATING AGENTS
Provided herein are compounds of formula (I)-(VI), wherein the variables are defined herein, processes of making them, and methods of treating cancer comprising administering such compounds.
BICYCLIC AMIDE COMPOUNDS AND METHODS OF USE THEREOF
The invention provides novel compounds having the general formula I:
##STR00001##
wherein R.sup.1, R.sup.2, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds and methods of using the compounds.