Patent classifications
C07C2601/02
KDM1A inhibitors for the treatment of disease
Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDMIA, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.
Methods and compositions for selective and targeted cancer therapy
Provided herein are methods and compositions for selective and targeted cancer therapy, in particular certain benzothiophenes, benzothiazoles, oxalamides, N-acyl ureas and chromones, and their use in selectively treating certain adenocarcinomas. In some embodiments, the selective toxicity of the compounds may be mediated through SCD1 and/or CYP450 such as CYP4F11.
Necrosis Inhibitors
The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
Thyromimetics
Compounds are provided having the structure of Formula (I): ##STR00001##
or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein A, X.sup.1, X.sup.2, Q, R.sup.1, R.sup.2 and n are as defined herein. Such compounds function as thyromimetics and have utility for treating diseases such as neurodegenerative disorders and fibrotic diseases. Pharmaceutical compositions containing such compounds are also provided, as are methods of their use and preparation.
Process for preparing the anti-tumor agent 6-(7-((1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide and its crystalline
The present invention relates a new process to synthesize 6-(7-((1-aminocyclo-propyl)-methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide (AL3810) by deprotection of substituted benzyl 1-((6-methoxy-4-(5-(methylcarbamoyl)naphthalen-2-yloxy)quinolin-7-yloxy)-methyl)cyc-lopropylcarbamate (Formula I) under a diluted or weak acidic condition. A stable crystalline form of 6-(7-((1-aminocyclo-propyl)-methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide has also been prepared. ##STR00001##
3′-substituted-abscisic acid derivatives
The invention relates to a novel class of (S)-3′-substituted-abscisic acid derivatives and (±)-3′-substituted-abscisic acid derivatives, and methods of synthesizing the derivatives.
Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto
- Ronald J. Heemstra ,
- Ronald Ross, Jr. ,
- Kyle DeKorver ,
- Kaitlyn Gray ,
- Daniel I. Knueppel ,
- Peter Vednor ,
- Timothy P. Martin ,
- Joseph D. Eckelbarger ,
- John F. Daeuble, SR. ,
- Ricky Hunter ,
- David A. Demeter ,
- Tony K. Trullinger ,
- Erich Baum ,
- Zoltan L. Benko ,
- Nakyen Choy ,
- Gary Crouse ,
- Fangzheng Li ,
- Jeff Nissen ,
- Monica B. Olson ,
- Michelle Riener ,
- Thomas C. Sparks ,
- Frank J. Wessels ,
- Maurice C. Yap
This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”). ##STR00001##
Treprostinil derivative compounds and methods of using same
Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.
CYCLOPROPANE DERIVATIVES IN FLAVOR AND FRAGRANCE COMPOSITIONS
The present invention relates to novel cyclopropane derivatives represented by Formula I:
##STR00001##
wherein R represents a hydrocarbon group containing 1-20 carbon atoms or an ester containing 1-20 carbon atoms;
wherein R′ represents a C.sub.1-C.sub.6 acyclic carboxylic acid ester, a C.sub.4-C.sub.6 cyclic carboxylic acid ester or —OR″, and R″ is selected from the group consisting of H, a C.sub.1-C.sub.6 acyclic hydrocarbon group, a C.sub.3-C.sub.6 carbocyclic ring and a C.sub.4-C.sub.5 heterocyclic ring; and
wherein the composition is selected from the group consisting of a flavor composition and a fragrance composition.
Benzenesulfonyl-Asymmetric Ureas and Medical Uses Thereof
Benzenesulfonyl-asymmetric ureas are provided for the treatment of conditions modulated by the ghrelin receptor.