An anti-influenza virus derivative and uses thereof
AssigneesShijiazhuang Discovery Medicine Technology Co., Ltd, Taiji Group Chongqing Fuling Pharmaceutical Company Limited
InventorsZhefeng Zhang, Haide Li, Wen Hou, Haijian Fu, Long Jiang, Wei Pan
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Abstract
The present application discloses a highly effective antiviral derivative and its use; the derivative is a compound as shown in the following formula (I-0) or hydrate, solvate, optical isomer, polymorph, isotopic derivative, pharmaceutically acceptable salt thereof, and a preparation method of the derivative is also disclosed. The compound of the present application can be used for the preparation of drugs for preventing/treating influenza virus.
Claims23
A compound as shown in the following formula (I-0), or its hydrate, solvate, optical isomer, polymorph, isotopic derivative, or pharmaceutically acceptable salt thereof, wherein:
- in the formula (I-0), Ra is selected from the group consisting of hydrogen, deuterium, methyl and deuterated methyl;
- X is S or Se, and when X is S, at least one deuterium atom is contained in the formula (I-0);
- Rb and Rc are each independently hydrogen, deuterium, C1-C3 alkyl, deuterated C1-C3 alkyl, or Rb, Rc, and the carbon atom to which they are attached together comprise cyclopropyl or deuterated cyclopropyl;
- R is hydrogen,
- wherein
- X1 is an oxygen atom or a sulfur atom;
- n1 is 0, 1 or 2;
- each R1 or R2 is independently selected from the group consisting of hydrogen, deuterium, methyl and deuterated methyl;
- R3 is selected from the group consisting of C1-C8 alkyl, C1-C8 alkoxy, C1-C8 alkylthio and C1-C8 alkylamino, one or more hydrogen atoms of each of the said groups being substituted or unsubstituted by deuterium;
- R4 and R5 are each independently hydroxy;
- or are each independently selected from the group consisting of C1-C8 alkoxy, C1-C8 alkylthio, C1-C8 alkylamino, C6-C20 aralkyloxy, one or more hydrogen atoms of each of the said groups being substituted or unsubstituted by deuterium;
- and R4 and R5 together with the phosphorus atom to which they are attached form a 5-7 membered ring of
- wherein, R6, R7, R8, R9, R10, R11, R12, R13 and R14 are each independently hydrogen or C1-C3 alkyl, or R6 and R7, R8 and R9, R11 and R12, R12 and R13 each together with the carbon atom to which they are attached form an aromatic ring, wherein one or more of the hydrogen atoms in the substituent of the 5-7 membered ring formed by R4 and R5 together with the phosphorus atom to which they are attached can be substituted or unsubstituted by deuterium.
A compound as represented by Formula (I), or its hydrate, solvate, optical isomer, polymorph, isotopic derivative, or pharmaceutically acceptable salt thereof, wherein:
- in Formula (I), Ra is selected from the group consisting of hydrogen, deuterium, methyl and deuterated methyl;
- Rb and Rc are each independently hydrogen, deuterium, C1-C3 alkyl, deuterated C1-C3 alkyl, or Rb, Rc, and the carbon atom to which they are attached together comprise cyclopropyl or deuterated cyclopropyl;
- R is hydrogen,
- wherein
- X1 is an oxygen atom or a sulfur atom;
- n1 is 0, 1 or 2;
- each R1 or R2 is independently selected from the group consisting of hydrogen, deuterium, methyl and deuterated methyl;
- R3 is selected from the group consisting of C1-C8 alkyl, C1-C8 alkoxy, C1-C8 alkylthio and C1-C8 alkylamino, wherein one or more hydrogen atoms of the said groups are substituted or unsubstituted with deuterium;
- R4 and R5 are each independently hydroxy;
- or are each independently selected from the group consisting of C1-C8 alkoxy, C1-C8 alkylthio, C1-C8 alkylamino, C6-C20 aralkyloxy, one or more hydrogen atoms of each of the said groups being substituted or unsubstituted by deuterium;
- and R4 and R5 together with the phosphorus atom to which they are attached form a 5-7 membered ring of
- wherein R6, R7, R8, R9, R10, R11, R12, R13, and R14 are each independently hydrogen or C1-C3 alkyl, or R6 and R7, R8 and R9, R11 and R12, R12 and R13 each together with the carbon atoms to which they are attached form an aromatic ring, wherein one or more of the hydrogen atoms in the substituent of the 5-7 membered ring formed by R4 and R5 together with the phosphorus atom to which they are attached can be substituted or unsubstituted by deuterium.
(canceled)
Dependencies are inferred from the claim text.