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US 12,668,589 B2Granted
N-formamidopyrazoline derivative as P2X3 receptor antagonist and use thereof
AssigneeHangzhou Westan Pharmaceutical Technology Co., Ltd
InventorsYunfeng Cheng, Xinqiang Zhu
Life of this patent
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Abstract
An N-formamidopyrazoline derivative is a compound having General Formula (I) or an enantiomer, a diastereomer, an epimer and a racemate thereof, or a pharmaceutically acceptable salt thereof. The compound is an antagonist of a ligand-gated non-selective cation channel receptor subtype P2X3, and can be used for treating or preventing various diseases mediated by the receptor P2X3.
Claims10
An N-formamidopyrazoline compound of General Formula (I), or an enantiomer, a diastereomer, a racemate thereof, or a pharmaceutically acceptable salt thereof:
- wherein
- Ar is selected from 1,3-benzodioxole;
- or Ar is selected from the following substituted phenyls, substitute five-membered or six-membered heteroaromatic ring groups:
- R5 and R6 are independently selected from the group consisting of H, halogen, nitryl, cyano group, methyl, trifluoromethyl, trifluoromethoxy, and C1 to C3 straight or branched chain alkoxy;
- and
- R7 is selected from methyl, ethyl, isopropyl, and cyclopropyl;
- R1 is selected from substituted or unsubstituted phenyl or substituted or unsubstituted pyridyl, wherein R1 is substituted with a group selected from halogen, C1 to C3 straight or branched chain alkyl, C1 to C3 straight or branched chain alkoxy, trifluoromethyl and trifluoromethoxy;
- and R2 is selected from a methyl, an ethyl, an isopropyl and a cyclopropyl;
- and
- wherein the R3 and the R4 are each independently selected from H, methyl, ethyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, isopropoxycarbonyl, tert-butoxycarbonyl, formyl, acetyl, and N,N-dialkylaminoacetyl;
- or the R3 and the R4 together with the N to which they both are connected form substituted or unsubstituted morpholinone, substituted or unsubstituted morpholinyl, substituted or unsubstituted piperidinyl, substituted or unsubstituted piperazinyl, substituted or unsubstituted piperazinone, substituted or unsubstituted pyrrolidone, substituted or unsubstituted oxazolidinone, substituted or unsubstituted imidazolidinone, substituted or unsubstituted imidazolyl, substituted or unsubstituted pyrazolyl, 1,2,3-triazolyl, and 1,2,4-triazolyl;
- and
- wherein substituted groups on morpholinone, morpholinyl, piperidinyl, piperazinyl, piperazinone, pyrrolidone, oxazolidinone, imidazolidinone, imidazolyl and pyrazolyl are selected from C1 to C3 straight or branched chain alkyl, formyl, acetyl, and C1 to C5 straight or branched chain alkoxy.
10 more elements
Dependencies are inferred from the claim text.