A61K31/4353

Chemical synthesis of clopidogrel active metabolites and disulfide conjugate prodrugs

A method of synthesizing a clopidogrel metabolite is provided. A piperidone intermediate is formed from a mandelate. An asymmetric ketone reduction of the piperidone intermediate is performed. A mercapto installation is performed on the piperidone intermediate to form a clopidogrel metabolite that includes a 4-carbon chiral center having an (R) configuration.

ELONGATION FACTOR 1-ALPHA INHIBITORS AND USES THEREOF

Disclosed herein, inter alia, are compounds for inhibiting Elongation Factor 1-alpha and uses thereof.

ELONGATION FACTOR 1-ALPHA INHIBITORS AND USES THEREOF

Disclosed herein, inter alia, are compounds for inhibiting Elongation Factor 1-alpha and uses thereof.

CHEMICAL SYNTHESIS OF CLOPIDOGREL ACTIVE METABOLITES AND DISULFIDE CONJUGATE PRODRUGS
20230201182 · 2023-06-29 ·

A method of synthesizing a clopidogrel metabolite is provided. A piperidone intermediate is formed from a mandelate. An asymmetric ketone reduction of the piperidone intermediate is performed. A mercapto installation is performed on the piperidone intermediate to form a clopidogrel metabolite that includes a 4-carbon chiral center having an (R) configuration.

Cross-linked fatty acid-based biomaterials

Fatty acid-based, pre-cure-derived biomaterials, methods of making the biomaterials, and methods of using them as drug delivery carriers are described. The fatty acid-derived biomaterials can be utilized alone or in combination with a medical device for the release and local delivery of one or more therapeutic agents. Methods of forming and tailoring the properties of said biomaterials and methods of using said biomaterials for treating injury in a mammal are also provided.

Cross-linked fatty acid-based biomaterials

Fatty acid-based, pre-cure-derived biomaterials, methods of making the biomaterials, and methods of using them as drug delivery carriers are described. The fatty acid-derived biomaterials can be utilized alone or in combination with a medical device for the release and local delivery of one or more therapeutic agents. Methods of forming and tailoring the properties of said biomaterials and methods of using said biomaterials for treating injury in a mammal are also provided.

Tricyclic heterocycles as anticancer agents

Tricyclic chemical modulators of FOXO transcription factor proteins are disclosed. The compounds are useful to treat cancer, age-onset proteotoxicity, stress-induced depression, inflammation, and acne. The compounds are of the following and similar genera: ##STR00001##
in which Het is an aromatic heterocyclic ring and Y is a point of attachment of various side chains and rings. An example of such a compound is 4-chloro-N-(3-(10,11-dihydro-5H-benzo[b]pyrido[2,3-f]azepin-5-yl)propyl)benzenesulfonamide: ##STR00002##

Pyrrolo [2,3-B] pyridine CDK9 kinase inhibitors

Disclosed are compounds of Formula (IIa), ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3A, R.sup.3B, R.sup.3C, R.sup.3D, R.sup.3E, and R.sup.4 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions comprising one or more compounds of Formula (IIa).

Hybrid cyclic libraries and screens thereof

Provided are novel types of hybrid cyclic libraries that contain a known protein binding domain of a natural product. Also provided are synthetic methods to make such libraries and methods for the deconvolution of hits using partially split-pooled library compounds. Such methods are applicable for use with the entire human proteome to screen such libraries that bind and for the identification of hits.

Hybrid cyclic libraries and screens thereof

Provided are novel types of hybrid cyclic libraries that contain a known protein binding domain of a natural product. Also provided are synthetic methods to make such libraries and methods for the deconvolution of hits using partially split-pooled library compounds. Such methods are applicable for use with the entire human proteome to screen such libraries that bind and for the identification of hits.