title: Novel tricyclic benzothiazolo[2,3-c]thiadiazine antagonists of the platelet ADP receptor (P2Y(12)).
abstract: Novel non-nucleoside tricyclic platelet ADP receptor (P2Y(12)) antagonists have been discovered that bind reversibly and with high affinity to the platelet receptor. Condensation of various 2-aminobenzothiazoles with chlorosulfonylacetyl chloride affords these novel tricyclic heterocycles, which are novel and unpredicted products of this reaction.
authors.affiliation: COR Therapeutics, Inc., Departments of Medicinal Chemistry and Biology, 94080, South San Francisco, CA, USA. rscarborough@corr.com
authors.forename: R M
authors.initials: RM
authors.lastname: Scarborough
authors.forename: A M
authors.initials: AM
authors.lastname: Laibelman
authors.forename: L A
authors.initials: LA
authors.lastname: Clizbe
authors.forename: L J
authors.initials: LJ
authors.lastname: Fretto
authors.forename: P B
authors.initials: PB
authors.lastname: Conley
authors.forename: E E
authors.initials: EE
authors.lastname: Reynolds
authors.forename: D M
authors.initials: DM
authors.lastname: Sedlock
authors.forename: H
authors.initials: H
authors.lastname: Jantzen
mesh_terms: D000244:Adenosine Diphosphate / Q000378:metabolism; D001665:Binding Sites / Q000187:drug effects / Q000502:physiology; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D008565:Membrane Proteins; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D058919:Purinergic P2 Receptor Antagonists; D011869:Radioligand Assay; D058925:Receptors, Purinergic P2Y12; D013829:Thiadiazines / Q000138:chemical synthesis / Q000494:pharmacology; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: C435072:CT 50547; D006571:Heterocyclic Compounds; D008565:Membrane Proteins; C548576:P2RY12 protein, human; D010975:Platelet Aggregation Inhibitors; D058919:Purinergic P2 Receptor Antagonists; D058925:Receptors, Purinergic P2Y12; D013829:Thiadiazines; D013844:Thiazoles; D000244:Adenosine Diphosphate