Patent classifications
C07D295/00
Substituted 4-phenylpiperidines, their preparation and use
The present invention provides a compound having the structure: ##STR00001## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are each independently H, halogen, CF.sub.3 or C.sub.1-C.sub.4 alkyl, wherein two or more of R.sub.1, R.sub.2, R.sub.3, R.sub.4, or R.sub.5 are other than H; R.sub.6 is H, OH, or halogen; and B is a substituted or unsubstituted heterobicycle, wherein when R.sub.1 is CF.sub.3, R.sub.2 is H, R.sub.3 is F, R.sub.4 is H, and R.sub.5 is H, or R.sub.1 is H, R.sub.2 is CF.sub.3, R.sub.3 is H, R.sub.4 is CF.sub.3, and R.sub.5 is H, or R.sub.1 is Cl, R.sub.2 is H, R.sub.3 is H, R.sub.4 is F, and R.sub.5 is H, or R.sub.1 is CF.sub.3, R.sub.2 is H, R.sub.3 is F, R.sub.4 is H, and R.sub.5 is H, or R.sub.1 is CF.sub.3, R.sub.2 is F, R.sub.3 is H, R.sub.4 is H, and R.sub.5 is H, or R.sub.1 is Cl, R.sub.2 is F, R.sub.3 is H, R.sub.4 is H, and R.sub.5 is H, then B is other than ##STR00002##
or a pharmaceutically acceptable salt thereof.
Substituted piperazines as selective HDAC1,2 inhibitors
Provided herein are compounds of Formula II, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity ##STR00001##
Method for the synthesis of rapamycin derivatives
The present invention relates to a method for the production of a rapamycin derivative of formula (I), the method comprising the preparation of a 2-(tri-substituted silyl)oxyethyl triflate by reacting ethylene oxide and a tri-substituted silyl triflate, reaction of the resulting 2-(tri-substituted silyl)oxyethyl triflate with rapamycin in the presence of a molar excess of organic base, and deprotection to obtain the rapamycin derivative of compound (I).
Bicyclic aza compounds as muscarinic M1 receptor antagonists
This invention relates to compounds (Formula (1)) that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where R.sub.1-R.sub.5, X.sub.1, X.sub.2 and p are as defined herein. ##STR00001##
Compounds useful for treating a Mannheimia haemolytica or Histophilus somni infection
The present invention discloses compounds that are useful in the treatment of respiratory diseases of animals, especially Bovine or Swine Respiratory disease (BRD and SRD).
OXALIC ACID MONOAMIDE LIGAND, AND USES THEREOF IN COUPLING REACTION OF COPPER-CATALYZED ARYL HALOGEN SUBSTITUTE
The present invention provides oxalic amide ligands and uses thereof in copper-catalyzed coupling reaction of aryl halides. Specifically, the present invention provides a use of a compound represented by formula I, wherein definitions of each group are described in the specification. The compound represented by formula I can be used as a ligand in copper-catalyzed coupling reaction of aryl halides for the formation of CN, CO and CS bonds.
##STR00001##
OXALIC ACID MONOAMIDE LIGAND, AND USES THEREOF IN COUPLING REACTION OF COPPER-CATALYZED ARYL HALOGEN SUBSTITUTE
The present invention provides oxalic amide ligands and uses thereof in copper-catalyzed coupling reaction of aryl halides. Specifically, the present invention provides a use of a compound represented by formula I, wherein definitions of each group are described in the specification. The compound represented by formula I can be used as a ligand in copper-catalyzed coupling reaction of aryl halides for the formation of CN, CO and CS bonds.
##STR00001##
Beta-lactamase inhibitor and process for preparing the same
A process for preparing a diazabicyclooctane compound represented by the following formula (I): ##STR00001##
wherein A represents RcO; B represents NH or NC.sub.1-6 alkyl; C represents a benzyl group; Rc represents a C.sub.1-6 alkyl group; A is substituted with one substituent Fn1, wherein Fn1 represents an azetidine group; the process including: (a) silylating the compound represented by the following formula (IV-c): ##STR00002##
wherein in the formula (IV-c), OBn represents benzyloxy, and (b) carrying out an intramolecular urea formation reaction.
ANTI-VIRAL COMPOUNDS
This invention relates to compounds that can be used to treat viral infections. The compounds are papain-like protease (PLpro) inhibitors.
COMPOSITIONS AND METHODS FOR DELIVERING MOLECULES
Compositions comprising mRNA, self-amplifying mRNA (sa-mRNA), modified mRNA, or circular RNA constructs comprising a gene-of-interest, and lipids and LNPs for use in therapy are disclosed. A method of delivering a payload to immune cells ex vivo by contacting immune cells with a lipid nanoparticle (LNP) encapsulating a payload encoding at least one polypeptide of interest, wherein the polypeptide of interest is an antigen receptor or an antibody.