As per patent office journal dated 15/10/2021, patent number 378938 has been granted to SIMMONS William H. that is titled 4 FLUORO THIO CONTAINING INHIBITORS OF APP2 COMPOSITIONS THEREOF AND METHOD OF USE.
The primary independent claim of this patent states a compound according to a formula II wherein R1 is H or R3—(CO)- ; wherein R2 is H; alkyl or substituted alkyl, having from 1 to 6 carbon atoms; or cycloalkyl-(CH2)a–, aryl-(CH2)a–, substituted aryl-(CH2)a–, or heteroaryl-(CH2)a–, having from 4 to 12 carbon atoms wherein R3 is alkyl or substituted alkyl, having 1 to 6 carbon atoms; or cycloalkyl-(CH2)a– , aryl-(CH2)a–, substituted aryl-(CH2)a–, or heteroaryl-(CH2)a–, having from 4 to 12 carbon atoms; a is zero or an integer from 1 to 6; or a pharmaceutically acceptable salt thereof.
During the patent prosecution, the patent examiner objected to this patent under section 3(d) of the Indian Patents Act. The patent applicant responded to this objection by stating that the claimed compound does not pertain to mere forms/derivatives of known compounds. The applicant further submits that the compound of Formula II show the enhanced efficacy consists of the active agent, i.e., the novel and non-obvious 4-fluoro triproline peptide analog of Formula III, and its readily hydrolysable ester and diester prodrug forms of the active agent, which in turn are hydrolyzed in vivo to release the active agent, i.e., the compound of Formula III. Therefore, the present invention does not fall under section 3(d) of the Patents Act.
This patent falls under the category of Chemical. Overall, this patent covers a fluoro-thiol-containing compound that is capable of specifically inhibiting the enzyme, membrane-bound aminopeptidase P2 5 (APP2), whose natural substrate is bradykinin. The compound is useful as a pharmaceutical agent because by inhibiting bradykinin degradation, the compound allows endogenous bradykinin to exert its beneficial effects in the body including dilating coronary arteries, providing protective effects in the heart during myocardial ischemia/reperfusion injury, stimulating formation of new blood vessels, improving organ 10 function in chronic heart and renal disease, and improving glucose tolerance and insulin sensitivity. Further, the invention is also directed to a pharmaceutical composition comprising the APP2 inhibitor and to a method of inhibiting bradykinin degradation in a mammalian patient, particularly a human patient.
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