Patent classifications
C07C2601/02
METHODS FOR INHIBITING CONVERSION OF CHOLINE TO TRIMETHYLAMINE (TMA)
A method of inhibiting the conversion of choline to trimethylamine (TMA) and lowering TMAO by providing a composition comprising a compound set forth in Formula (I):
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PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO
This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the following formula (“Formula One”).
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THERAPEUTIC COMPOUNDS AND USES THEREOF
Provided herein are compounds of formula I:
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and salts thereof and compositions and uses thereof. The compounds are useful as inhibitors of LSD1. Also included are pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various LSD1-mediated disorders.
Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto
- Timothy P. Martin ,
- Joseph D. Eckelbarger ,
- Ronald Ross, Jr. ,
- Kyle A. DeKorver ,
- Ronald J. Heemstra ,
- Daniel I. Knueppel ,
- Peter Vednor ,
- Ricky Hunter ,
- David A. Demeter ,
- Tony K. Trullinger ,
- Erich W. Baum ,
- Zoltan L. Benko ,
- Nakyen Choy ,
- Gary D. Crouse ,
- John F. Daeuble, SR. ,
- Fangzheng Li ,
- Jeffrey Nissen ,
- 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”).
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IMMUNOMODULATOR COMPOUNDS
Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (II):
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including stereoisomers and pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
CYSTINE DIAMIDE ANALOGS FOR THE PREVENTION OF CYSTINE STONE FORMATION IN CYSTINURIA
Cystine analogs that improve the solubility of L-cystine in urine for treatment of cystinuria and which have the structure:
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and pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein each R and R′ pair are independently selected from (i) or (ii); (i) R and R′ are independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alcohol, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclic, and substituted or unsubstituted heteroaryl, or (ii) R and R′ together form a substituted or unsubstituted heterocyclic ring structure, or a substituted or unsubstituted heteroaryl ring structure; X is hydrogen, or an alkyl; and Y is O or S.
Organic Compound of Formula (I) for Use in Organic Electronic Devices, a Composition Comprising a Compound of Formula (IV) and at Least One Compound of Formula (IVa) to (IVd), an Organic Semiconductor Layer Comprising the Compound or Composition, an Organic Electronic Device Comprising the Organic Semiconductor Layer, and a Display Device Comprising the Organic Electronic Device
The present invention relates to a compound of formula (I) for use in organic electronic devices, a composition comprising a compound of formula (IV) and at least one compound of formula (IVa) to (IVd), an organic semiconductor layer comprising the compound or composition, an organic electronic device comprising the organic semiconductor layer, and a display device comprising the organic electronic device.
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ERAP1 MODULATORS
The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, A compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, (I) wherein: Z is a group of formula: (II) wherein P and Q are each independently CR.sub.12R.sub.13; or one of P and Q is NR.sub.14 and the other is CR.sub.12R.sub.13; the group X—Y is —NHSO.sub.2— or —SO2NH—; R.sub.1 is H, CN or alkyl; R.sub.2 is selected from COOH and a tetrazolyl group; R.sub.3 is selected from H, Cl and alkyl; R.sub.4 is selected from H and halo; R.sub.5 is selected from H, alkyl, haloalkyl, SO.sub.2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R.sub.6 is H; R.sub.7 is selected from H, CN, haloalkyl, halo, SO.sub.2-alkyl, heteroaryl, SO.sub.2NR.sub.16R.sub.17, CONR.sub.10R.sub.11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.8 is selected from H, alkyl, haloalkyl and halo; R.sub.9 is H or halo; and R.sub.10, R.sub.11, R.sub.12, R.sub.13, R.sub.14, R.sub.16 and R.sub.17 are each independently H or alkyl; R.sub.15 is selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; and m and n are each independently 0, 1, 2 or 3. Further aspects of the invention relate to such compounds for use in the field of immune-oncology and related applications.
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LIPID COMPOUNDS AND LIPID NANOPARTICLE COMPOSITIONS
Provided herein are lipid compounds that can be used in combination with other lipid components, such as neutral lipids, cholesterol and polymer conjugated lipids, to form lipid nanoparticles for delivery of therapeutic agents (e.g., nucleic acid molecules) for therapeutic or prophylactic purposes, including vaccination. Also provided herein are lipid nanoparticle compositions comprising said lipid compounds.
ARYLAMIDE DERIVATIVE HAVING ANTITUMOR ACTIVITY
The present disclosure provides, for example, a compound represented by general formula (6) below or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of the compound or salt:
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wherein X.sub.1, X.sub.2, X.sub.3 and X.sub.4 are each independently —CR.sub.2═ or —N═, R.sub.2 is, for example, a halogen atom, R.sub.1 is, for example, —S(═O).sub.2—NH—R.sub.8, R.sub.8 is, for example, a C1-6 alkyl group, R.sub.3 is, for example, a hydrogen atom, R.sub.5 is, for example, a halogen atom, R.sub.6 is, for example, a hydrogen atom, and R.sub.4 is, for example, a cyclopropyl group. The compounds, salts or solvates provided by the present disclosure exhibit high RAF/MEK complex-stabilizing activity and can be used for the treatment or prevention of cell proliferative disorders, particularly cancers.