C07B2200/07

SUBSTITUTED THIOPHENE CARBOXAMIDES, THIOPHENE CARBOXYLIC ACIDS AND DERIVATIVES THEREOF

The present disclosure relates to substituted thiophene carboxamides derivatives of formula (I) and (II), their use for controlling phytopathogenic microorganisms and compositions comprising thereof.

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PROCESS FOR THE PREPARATION OF (9S)-2-BROMO-9-(2,3,4-TRIFLUOROPHENYL)-6,7,8,9-TETRAHYDRO-5H-[1,2,4]TRIAZOLO[1,5-A]AZEPINE

The present invention relates to a process for synthesizing large scale a compound of formula (I), or pharmacuetically acceptable salt thereof, which is useful as the key intermediate for the synthesis of compounds for prophylaxis and treatment of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.

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FLUORINE-CONTAINING HETEROCYCLIC DERIVATIVES WITH MACROCYCLIC STRUCTURE AND USE THEREOF

Disclosed are a macrocyclic fluorine-containing heterocyclic derivative of formula (I), a preparation method thereof, and a use thereof in treatment of TRK kinase-mediated diseases.

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PREPARATION METHOD FOR OPTICALLY ACTIVE CITRONELLAL
20230043867 · 2023-02-09 ·

A preparation method for optically active citronellal, which can obviously enhance the catalytic stability of an optically active transition metal catalyst for asymmetric hydrogenation of homogeneous catalysis and thereby achieve higher turnover numbers. In the preparation method for optically active citronellal, a substrate is subjected to an asymmetric hydrogenation reaction in the presence of the transition metal catalyst to generate the optically active citronellal, wherein the transition metal catalyst is obtained by reacting a transition metal compound with an optically active ligand containing two phosphorus atoms, and the raw material of the substrate is one of neral and geranial or a combination thereof to control the hydroxyl value to be less than or equal to 6 mgKOH/g and/or the iron content to be less than or equal to 50 ppm in the raw material of the substrate for the asymmetric hydrogenation reaction.

MODULATORS OF INTEGRATED STRESS RESPONSE PATHWAY

The present disclosure relates generally to therapeutic agents that may be useful as modulators of Integrated Stress Response (ISR) pathway.

HPK1 antagonists and uses thereof

The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of HPK1, and the treatment of HPK1-mediated disorders.

Polycyclics as sigma receptor modulators
11548879 · 2023-01-10 · ·

The present invention discloses a number of polycyclic amines that are useful as opioid receptor modulators. The compounds of the invention are useful in both therapeutic and diagnostic methods, including for treating pain, neurological disorders, cardiac disorders, bowel disorders, drug and alcohol addiction, drug overdose, urinary disorders, respiratory disorders, sexual dysfunction, psoriasis, graft rejection or cancer.

Processes for the production of isomerically pure or enriched cis-clomiphene
11572333 · 2023-02-07 · ·

The present disclosure relates to methods for the production of the isomerically pure or isomerically enriched cis-clomiphene and salts thereof.

Affinity illudofulvene conjugates
11591295 · 2023-02-28 · ·

In an embodiment of the invention, a composition for treating a cell population comprises a medicant. The medicant moiety can be an illudofulvene analog. In an embodiment of the invention, a composition for treating a cell population comprises an Affinity Medicant Conjugate (AMC). The affinity moiety can be an antibody, an antibody fragment, a receptor protein, a peptidic growth factor, an anti-angiogenic protein, a specific binding peptide, protease cleavable peptide, a glycopeptide, a peptide, a peptidic toxin, a protein toxin and an oligonucleotide. The affinity moiety can be covalently bound to the medicant via a linker.

SHORT-ACTING BENZODIAZEPINE SALTS AND THEIR POLYMORPHIC FORMS
20180002338 · 2018-01-04 · ·

The invention relates to besylate salts of the compound of formula (I):

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Methods of preparing the salts, and their use as medicaments, in particular for sedative or hypnotic, anxiolytic, muscle relaxant, or anticonvulsant purposes is also described.