Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-9963455-B2
Publication Date
2018-05-08
Expiration Date
Abstract
A compound of formula (I) or a pharmaceutically acceptable salt thereof, useful in therapy, in particular in the treatment of a viral infection.
Core Innovation
The invention relates to substituted pyrazolo[1,5-a]pyrimidin-7-amine scaffold compounds, pharmaceutical compositions, and methods of treatment using compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds are defined by formula (I) and related formulae, including (Id) and (Ih), with a fused N-containing bicyclic core, ring A as phenyl or 5- or 6-membered heteroaryl, and ring B as a 5- or 6-membered heteroaryl, phenyl, or 5- or 6-membered saturated or unsaturated carbocyclyl ring system.
The substituent framework includes W, p, Z, R1, R2, R3, m, and R4, together with broader substituent classes for R5 to R23. The descriptions include C1-C6 alkyl, halogen, oxygen-containing and sulfur-containing groups, optional fluorinated alkyl, methylenedioxy or ethylenedioxy biradicals, and ring-formation options when adjacent substituents on ring B combine to form a 5- or 6-membered heterocyclic or carbocyclic ring or a benzene ring.
The disclosed embodiments also include explicit exclusions of specified substituted pyrazolo[1,5-a]pyrimidin-7-amine derivatives and structural restrictions such as the phenyl ring not being substituted in ortho position, and, for formula (Ih), no R2 attached in ortho position on the phenyl ring. The document ties the chemical series to pharmaceutical compositions and methods of treatment for viral infections in a mammal, including RNA viral infection.
Claims Coverage
The independent claims cover four inventive features: a pharmaceutical composition, compounds of formula (Id) and (Ih), and a method of treatment of viral infection. Across these claims, the main inventive features are the formula-defined substituted pyrazolo[1,5-a]pyrimidin-7-amine scaffold, constrained ring A and ring B definitions, selected substituent sets for W, p, Z, R1 to R4 and R5 to R23, explicit exclusion lists, and therapeutic administration for viral infection.
Pharmaceutical composition with formula (I) scaffold and constrained substituents
A pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, with ring A as phenyl or 5- or 6-membered heteroaryl, ring B as a 5- or 6-membered saturated or unsaturated carbocyclyl, 5- or 6-membered heteroaryl or phenyl, W, p, and the multiple substituent variables R1, R2, R3, R4, and R5 to R23 defined by the stated options and constraints, including optional fluorinated alkyl, methylenedioxy or ethylenedioxy biradicals, ring-formation rules, and excluded named compounds.
Compound of formula (Id) with defined substituent and ring constraints
A compound of formula (Id) or a pharmaceutically acceptable salt thereof, with ring B as phenyl or 5- or 6-membered heteroaryl, W and the multiple substituent variables R1 to R23 defined by the stated options and constraints, including optional fluorinated alkyl, methylenedioxy or ethylenedioxy biradicals, ring-formation rules, and explicit exclusion of specified compounds.
Compound of formula (Ih) with Z selection and ortho attachment restriction
A compound of formula (Ih) or a pharmaceutically acceptable salt thereof, with p as 1 to 3, Z as N or CR2, ring B as a 5- or 6-membered heteroaryl or phenyl, R1 to R23 defined by the stated options and constraints, and the restriction that no R2 is attached in ortho position on the phenyl ring, together with explicit exclusion of specified compounds.
Treatment of viral infection using formula (I) compound
A method of treatment of a viral infection by administration of a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof, with the same scaffold and substituent definitions and ring constraints, and with explicit exclusions of specified compounds; dependent claim text narrows the infection to RNA viral infection.
The claim set centers on substituted pyrazolo[1,5-a]pyrimidin-7-amine compounds defined by formula (I), (Id), and (Ih), with pharmaceutical composition and treatment coverage built around tightly constrained ring and substituent definitions. The claims also include explicit exclusions of specified compounds and, for the method claim, therapeutic administration for viral infection.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Treatment of viral infection.
Treatment of RNA viral infection.
Administration to a mammal in need thereof.
Pharmaceutical compositions comprising the defined compounds or pharmaceutically acceptable salts.
Interested in licensing this patent?