C07B2200/07

Substituted indoline derivatives as dengue viral replication inhibitors

The present invention concerns substituted indoline derivatives, methods to prevent or treat dengue viral infections by using said compounds and also relates to said compounds for use as a medicine, more preferably for use as a medicine to treat or prevent dengue viral infections. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of dengue viral infections. The invention also relates to processes for preparation of the compounds. ##STR00001##

Methods for producing D-α-methyldopa

The present invention provides methods of synthesizing D-α-methyldopa and L-α-methyldopa.

PROCESSES RELATED TO FORMATION OF ARYLCYCLOPROPYL CARBOXYLIC ACIDS

This disclosure relates to processes to form arylcyclopropyl carboxylic acids useful in forming molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda.

Pyridine acetamide derivative serving as CDK inhibitor, and preparation method therefor and use thereof
20230219961 · 2023-07-13 ·

The present disclosure relates to the technical field of pyridine acetamide derivatives, and specifically relates to a pyridine acetamide derivative as a CDK inhibitor, a preparation method therefor and a use thereof. The pyridine acetamide derivative exhibits excellent CDK9/CDK7 kinase inhibitory activity, and can be used for preparing medications for treating cancers; and the cancers are particularly blood cancers, including acute myeloid leukemia, multiple myeloma, chronic lymphocytic leukemia, follicular lymphoma and the like, and solid tumors, including breast cancer, prostate cancer, ovarian cancer, hepatocellular carcinoma, pancreatic cancer, kidney cancer, stomach cancer, colorectal cancer, lung cancer and the like.

VINYLETHER COMPOUNDS AND PROCESSES FOR PREPARING ALDEHYDE COMPOUNDS AND A CARBOXYLATE COMPOUND THEREFROM
20230014797 · 2023-01-19 ·

The present invention provides a vinylether compound of the following general formula (1), wherein R.sup.1 represents a monovalent hydrocarbon group having 1 to 15 carbon atoms, and the wavy line represents the E-form, the Z-form, or a mixture thereof. The present invention further provides a process for preparing 2,3,4,4-tetramethyl-1-cyclopentenecarbaldehyde of the following formula of the following formula (2), the process comprising subjecting the vinylether compound (1) to a hydrolysis reaction to form 2,3,4,4-tetramethyl-1-cyclopentenecarbaldehyde (2).

##STR##

##STR##

BIVALENT COMPOUNDS, CONJUGATES AND USES THEREOF

There are provided bivalent compounds and conjugates thereof, the conjugates comprising a bivalent compound, a targeting moiety, and a bioactive agent, as well as pharmaceutical compositions and methods of use of the conjugate for the treatment, inhibition, or prevention of diseases and disorders which are therapeutic targets of the bioactive agent.

##STR00001##

Dithioamine reducing agents

Dithioamine reducing agents useful for the reduction of disulfide bonds. The reducing agents of this invention are useful, for example, to reduce disulfide bonds, particularly in proteins, or to prevent the formation of disulfide bonds, particularly in proteins and other biological molecules. Reducing agents of this invention can be employed to regulate protein function in proteins in which a sulfhydryl group is associated with biological activity. Reducing agents of this invention can prevent inactivation of a given protein or enhance activation of a given protein or other biological molecule in vitro and/or in vivo. Reducing agents of this invention can prevent or reduce oxidation of cysteine residues in proteins and prevent the formation of reduced activity protein dimers (or other oligomers). Reducing agents of this invention are useful and suitable for application in a variety of biological applications, particularly as research and synthetic reagents. The invention provides S-acylated dithioamines which can be selectively activated reducing agents by removal of the S-acyl groups enzymatically or chemically. The invention further provides dithiane precursors of thioamino reducing agents. The invention provides dithioamine reducing agents, S-acylated dithioamines and dithianes which are immobilized on surfaces, including among others, glass, quartz, microparticles, nanoparticles and resins.

DEUTERATED TRYPTAMINE DERIVATIVES AND METHODS OF USE
20230219889 · 2023-07-13 · ·

The present disclosure is directed to chemical compounds and to the use of such compounds in the treatment of diseases associated with a serotonin 5-HT.sub.2 receptor.

##STR00001##

Compositions and methods for the treatment of neurological diseases
11555007 · 2023-01-17 · ·

The invention relates to the compounds or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II and formula III and the methods for the treatment of neurological diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, lozenge, spray, intravenous, oral solution, nasal spray, oral solution, suspension, oral spray, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of neurological diseases.

DEUBIQUITINASE INHIBITORS AND METHODS OF USE THEREOF

The inventive compounds are small molecule therapeutics that are potent inhibitors of USP7 activity. The invention also provides pharmaceutical compositions comprising the compounds, and methods for using the compounds for treating or preventing a disease, disorder, or condition associated with USP7 activity.