Patent classifications
C07D207/273
Urea derivative or pharmacologically acceptable salt thereof
Provided is a compound having a formyl peptide receptor like 1 (FPRL1) agonist effect. The present invention relates to a compound represented by the general formula (I) or a pharmacologically acceptable salt thereof. The present invention also relates to a pharmaceutical composition containing the compound represented by the general formula (I) or a pharmacologically acceptable salt thereof. ##STR00001##
Urea derivative or pharmacologically acceptable salt thereof
Provided is a compound having a formyl peptide receptor like 1 (FPRL1) agonist effect. The present invention relates to a compound represented by the general formula (I) or a pharmacologically acceptable salt thereof. The present invention also relates to a pharmaceutical composition containing the compound represented by the general formula (I) or a pharmacologically acceptable salt thereof. ##STR00001##
Process for the preparation of N-((1R,2S,5R)-5-(<i>tert</i>-butylamino)-2-((S)-3-(7-<i>tert</i>-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrroldin-1-yl)cyclohexyl)acetamide
- Burcu Selin Aytar ,
- Alina Borovika ,
- Collin Chan ,
- Joerg Deerberg ,
- Nathan R. Domagalski ,
- Martin D. Eastgate ,
- Yu Fan ,
- Michael David Bengt Fenster ,
- Robert V. Forest ,
- Francisco Gonzalez-Bobes ,
- Rebecca A. Green ,
- Matthew R. Hickey ,
- Nathaniel David Kopp ,
- Thomas E. La Cruz ,
- Kathleen Lauser ,
- Hong Geun Lee ,
- David K. Leahy ,
- Helen Y. Luo ,
- Thomas M. Razler ,
- Scott A. Savage ,
- Chris Sfouggatakis ,
- Maxime C. D. Soumeillant ,
- Serge Zaretsky ,
- Bin Zheng ,
- Ye Zhu
The invention generally relates to an improved process for the preparation of N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide, ##STR00001## as well as novel intermediates employed in the process, which may be useful for the treatment of cancer.
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##
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##
Ethynylbenzene derivatives
Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R.sub.1, R.sub.2, R.sub.3, R.sub.101, L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections. ##STR00001##
Ethynylbenzene derivatives
Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R.sub.1, R.sub.2, R.sub.3, R.sub.101, L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections. ##STR00001##
PROCESS FOR PREPARING SPIRO DERIVATIVES
The invention relates to a novel process for preparing spiro derivatives, in particular 7-methyl-2-[4-methyl-6-[4-(trifluoromethyl)-phenyl]pyrimidin-2-yl]-1,7-diazaspiro[4.4]nonan-6-one, and to novel intermediates for use in said process along with processes for preparing said intermediates.
Compounds for Treating Cannabinoid Toxicity and Acute Cannabinoid Overdose
The present invention relates to novel compounds that can act as antidotes for treating “Acute Cannabinoid Overdose” produced by classical cannabinoids such as Δ.sup.9-tetrahydrocannabinol (THC) and several synthetic psychoactive cannabinoids (SPCs). The cannabis constituent THC exerts its psychotropic effects via CB1 receptor activation and SPCs mimic the effects of THC with higher potency and severe neurotoxicity. Compounds disclosed in this invention, their enantiomers, diastereomers, geometric isomers, racemates, tautomers, rotamers, atropisomers, metabolites, N-oxides, salts, solvates, hydrates, isotopic variations and their polymorphic forms can be therapeutically useful in an emergency setting for counteracting the intoxicating effects of acute THC ingestion and SPC overdose. Also, aspects of the invention are concerned with pyrazoles, imidazoles, triazoles, thiazoles, oxazoles, dihydropyrazoles, pyrrolidinones, azetidines, oxyazetidines and azaspiro[3.3]heptanes with unique pharmacokinetic and pharmacodynamic properties for treating “Acute Cannabinoid Overdose”.
Compounds for Treating Cannabinoid Toxicity and Acute Cannabinoid Overdose
The present invention relates to novel compounds that can act as antidotes for treating “Acute Cannabinoid Overdose” produced by classical cannabinoids such as Δ.sup.9-tetrahydrocannabinol (THC) and several synthetic psychoactive cannabinoids (SPCs). The cannabis constituent THC exerts its psychotropic effects via CB1 receptor activation and SPCs mimic the effects of THC with higher potency and severe neurotoxicity. Compounds disclosed in this invention, their enantiomers, diastereomers, geometric isomers, racemates, tautomers, rotamers, atropisomers, metabolites, N-oxides, salts, solvates, hydrates, isotopic variations and their polymorphic forms can be therapeutically useful in an emergency setting for counteracting the intoxicating effects of acute THC ingestion and SPC overdose. Also, aspects of the invention are concerned with pyrazoles, imidazoles, triazoles, thiazoles, oxazoles, dihydropyrazoles, pyrrolidinones, azetidines, oxyazetidines and azaspiro[3.3]heptanes with unique pharmacokinetic and pharmacodynamic properties for treating “Acute Cannabinoid Overdose”.