Patent classifications
C07D295/084
HETEROCYCLIC COMPOUNDS FOR CANCER IMAGING AND TREATMENT AND METHODS FOR THEIR USE
Compounds having a structure of Formula I:
##STR00001##
or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.11a, R.sup.11b, R.sup.11c, R.sup.11d, X, n.sup.1, n.sup.2, and n.sup.3 are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.
Heterocyclic compounds for cancer imaging and treatment and methods for their use
Compounds having a structure of Formula I: ##STR00001##
or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.11a, R.sup.11b, R.sup.11c, R.sup.11d, X, n.sup.1, n.sup.2, and n.sup.3 are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.
Heterocyclic compounds for cancer imaging and treatment and methods for their use
Compounds having a structure of Formula I: ##STR00001##
or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.11a, R.sup.11b, R.sup.11c, R.sup.11d, X, n.sup.1, n.sup.2, and n.sup.3 are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.
TOTAL SYNTHESES OF SPECIALIZED PRO-RESOLVING MEDIATORS (SPMS), STRUCTURAL ISOMERS AND STRUCTURAL ANALOGS
A method for the synthesis of specialized pro-resolving mediators, structural isomers thereof and analogs thereof is disclosed herein. The method comprises reacting a compound of the formula (I):
##STR00001## wherein R.sub.1 is alkyl.sub.(C≤12), cycloalkyl.sub.(C≤12), alkenyl.sub.(C≤12), alkylidene.sub.(C≤12), alkynyl.sub.(C≤12), aryl, aralkyl, heteroaryl or heteroaralkyl; and X.sub.1, X.sub.2 and X.sub.3 are each independently hydroxy or OP, wherein P is a hydroxy protecting or hydroxy activating group; with a reducing agent under conditions sufficient to produce a compound of the formula (II):
##STR00002## wherein: R.sub.1, X.sub.1, X.sub.2 and X.sub.3 are as defined above.
Novel protectins, more specifically novel structural isomers and analogs of PD1 and PDX are also disclosed.
TOTAL SYNTHESES OF SPECIALIZED PRO-RESOLVING MEDIATORS (SPMS), STRUCTURAL ISOMERS AND STRUCTURAL ANALOGS
A method for the synthesis of specialized pro-resolving mediators, structural isomers thereof and analogs thereof is disclosed herein. The method comprises reacting a compound of the formula (I):
##STR00001## wherein R.sub.1 is alkyl.sub.(C≤12), cycloalkyl.sub.(C≤12), alkenyl.sub.(C≤12), alkylidene.sub.(C≤12), alkynyl.sub.(C≤12), aryl, aralkyl, heteroaryl or heteroaralkyl; and X.sub.1, X.sub.2 and X.sub.3 are each independently hydroxy or OP, wherein P is a hydroxy protecting or hydroxy activating group; with a reducing agent under conditions sufficient to produce a compound of the formula (II):
##STR00002## wherein: R.sub.1, X.sub.1, X.sub.2 and X.sub.3 are as defined above.
Novel protectins, more specifically novel structural isomers and analogs of PD1 and PDX are also disclosed.
SUBSTITUTED HALOALKYL SULFONANILIDE HERBICIDES
Disclosed are compounds of Formula 1, all stereoisomers, N-oxides, and salts thereof,
##STR00001##
wherein G is CONR.sup.5R.sup.6 or selected from
##STR00002## and R.sup.1 through R.sup.18, R.sup.f and G are as defined in the Disclosure.
Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.
Aziridinyl and amino dimeric naphthoquinone compounds and use for acute myeloid leukemia
The invention relates to new amino dimeric naphthoquinone compounds with antileukemic activity. Compounds of the invention demonstrated increased aqueous solubility compared to previously available dimeric naphthoquinones and potent nanomolar inhibition of cell survival in AML cells. Preferred compounds contained an aziridine or a secondary amino alcohol pharmacophore.
BUMETANIDE ANALOGS, COMPOSITIONS AND METHODS OF USE
The present invention provides bumetanide analogs and compositions comprising such analogs. The present invention also provides pharmaceutical compositions containing these bumetanide analogs and methods for their use. These analogs are believed useful for the treatment and/or prophylaxis of conditions that involve the Na.sup.+K.sup.+Cl.sup.− co-transporter or GABA.sub.A receptor.
BUMETANIDE ANALOGS, COMPOSITIONS AND METHODS OF USE
The present invention provides bumetanide analogs and compositions comprising such analogs. The present invention also provides pharmaceutical compositions containing these bumetanide analogs and methods for their use. These analogs are believed useful for the treatment and/or prophylaxis of conditions that involve the Na.sup.+K.sup.+Cl.sup.− co-transporter or GABA.sub.A receptor.
CONJUGATED LIPOMERS AND USES THEREOF
The present invention provides inventive conjugated polyethyleneimine (PEI) polymers and conjugated aza-macrocycles (collectively referred to herein as “conjugated lipomers” or “lipomers”) containing one or more groups of the formula (iii):
##STR00001##
wherein R.sup.3 and R.sup.4 are as defined herein. Also provided are compositions comprising the inventive conjugated lipomers, and methods of preparation and use.