Patent classifications
C07K5/06026
ENZYME INHIBITORS
- Rebecca Louise Davie ,
- Hannah Joy Edwards ,
- David Michael Evans ,
- Simon Teanby Hodgson ,
- Sally Louise MARSH ,
- Alessandro MAZZACANI ,
- David Philip Rooker ,
- Michael John Stocks ,
- Andrew Peter CRIDLAND ,
- Emanuela GANCIA ,
- Julie Nicole HAMBLIN ,
- Paul Stuart HINCHLIFFE ,
- Stefano LEVANTO ,
- Terence Aaron PANCHAL ,
- Iain Robert MILLER
The present invention provides compounds of formula (I): Formula (I) compositions comprising such compounds; the use of such compounds in therapy; and methods of treating patients with such compounds; wherein A, Y, n, R1, R2.sup.A, R2.sup.B, R3 and *1 are as defined herein.
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PEPTIDOMIMETICS FOR THE TREATMENT OF CORONAVIRUS AND PICORNAVIRUS INFECTIONS
Compounds, compositions and methods for preventing, treating or curing a coronavirus, picornavirus, and/or hepeviridae virus infection in human subjects or other animal hosts. Specific viruses that can be treated include enteroviruses. In one embodiment, the compounds can be used to treat an infection with a severe acute respiratory syndrome virus, such as human coronavirus 229E, SARS, MERS, SARS-CoV-1 (OC43), and SARS-CoV-2. In another embodiment, the methods are used to treat a patient co-infected with two or more of these viruses, or a combination of one or more of these viruses and norovirus.
CYCLIC COMPOUNDS AND METHODS OF MAKING AND USING
Disclosed are compounds and methods for highly effective chemoselective peptide cyclization and bicyclization directly on unprotected peptides and other compounds as well as the compounds produced by the methods, which have a novel structural motif. The fast reaction rate and operational simplicity render this method to be highly effective to synthesize cyclic structures, i.e. cyclic peptides. The cyclic compounds allow for various functionalities useful in chemical biology study and drug discovery.
CANNABINOID PRODRUG COMPOUNDS
A prodrug compound of cannabidiol (CBD), pharmaceutical composition thereof and methods of use thereof in patients in need.
CAMPTOTHECINE ANTIBODY-DRUG CONJUGATES AND METHODS OF USE THEREOF
The present disclosure provides antibody-drug conjugate (ADC) structures, which include a camptothecine or a camptothecine derivative linked to a polypeptide (e.g., an antibody) through a linker. The disclosure also encompasses compounds and methods for production of such conjugates, as well as methods of using the conjugates.
METHOD FOR PHOTOCLEAVAGE OF AMIDE BONDS
The present disclosure provides a method for photocleavage of an amide bond, the method has mild reaction conditions and can realize the cleavage of amide bonds by using light. The method comprises the following steps: subjecting 2,4-dinitrofluorobenzene to a reaction with an amino group of a substance represented by structural formula I with an α-amino acid at the end to produce a compound 1 represented by structural formula II; then under light irradiation, subjecting the compound 1 to a cleavage reaction of amide bond;
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Wherein, R1 is the side chain group of α-amino acid; R2 is: aryl, aliphatic hydrocarbon, —CH(R)—COOH or polypeptide.
PSMA-TARGETED NIR DYES AND THEIR USES
The present disclosure relates to prostate specific membrane antigen (PSMA) targeted compounds conjugated to near-infra red (NIR) dyes and methods for their therapeutic and diagnostic use. More specifically, this disclosure provides compounds and methods for diagnosing and treating diseases associated with cells and/or vasculature expressing prostate specific membrane antigen (PSMA), such as prostate cancer and related diseases. The disclosure further describes methods and compositions for making and using the compounds, methods incorporating the compounds, and kits incorporating the compounds.
MYC-MAX INHIBITOR COMPOUND THERAPEUTICS FOR CANCER TREATMENT, METHODS AND USES ASSOCIATED THEREWITH
Provided herein are Myc-Max inhibitory compounds having the structure of Formula (I) and compositions thereof for use in the treatment of cancer. In particular, the Myc-Max inhibitory compounds may be useful for the treatment of cancers selected from one or more of: prostate cancer, breast cancer, colon cancer, cervical cancer, small-cell lung carcinomas, neuroblastomas, osteosarcomas, glioblastomas, melanoma and myeloid leukaemia.
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AMINOCARBAMOYL COMPOUNDS FOR THE TREATMENT OF VIRAL INFECTIONS
The present invention relates to compounds of formula (I),
##STR00001##
wherein R.sup.1-R.sup.5 and L are as described herein, and their pharmaceutically acceptable salt thereof, and compositions including the compounds and methods of using the compounds.
LINKER COMPOUNDS COMPRISING AMIDE BONDS
Various embodiments provide a homo-bivalent linker compound comprising identical functional groups at either end, methods of making such linker compounds, and methods of using the linker compounds.