JPWO2021209425A5 - - Google Patents
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- JPWO2021209425A5 JPWO2021209425A5 JP2022562248A JP2022562248A JPWO2021209425A5 JP WO2021209425 A5 JPWO2021209425 A5 JP WO2021209425A5 JP 2022562248 A JP2022562248 A JP 2022562248A JP 2022562248 A JP2022562248 A JP 2022562248A JP WO2021209425 A5 JPWO2021209425 A5 JP WO2021209425A5
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- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- composition according
- compound
- pharma
- alkyl
- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims description 20
- 239000008194 pharmaceutical composition Substances 0.000 claims description 17
- 125000000217 alkyl group Chemical group 0.000 claims description 9
- 208000015181 infectious disease Diseases 0.000 claims description 9
- 150000003839 salts Chemical class 0.000 claims description 7
- 201000010284 hepatitis E Diseases 0.000 claims description 5
- 206010061598 Immunodeficiency Diseases 0.000 claims description 2
- 230000001684 chronic effect Effects 0.000 claims description 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
Description
本明細書に引用される全ての参照（例えば、文献又は特許若しくは特許出願書）は、各個別の参照（例えば、文献又は特許若しくは特許出願書）があらゆる目的のためにその全体が参照により組み込まれることを具体的かつ個別に示した場合と同程度に、それらの全体が参照することによりあらゆる目的のために本明細書に組み込まれる。他の実施形態は、以下の特許請求の範囲内である。
以下の態様を包含し得る。
［１］ Ｅ型肝炎感染症の治療を必要とする対象においてＥ型肝炎感染症を治療することにおける使用のための化合物であって、前記化合物が、以下の式（Ｉ）の化合物
式中、
塩基が、以下の（ｂ－１）、（ｂ－２）、（ｂ－３）、（ｂ－４）、（ｂ－５）、（ｂ－６）、（ｂ－７）、及び（ｂ－８）からなる群から選択され、
Ｒ
２
が、Ｈ及びＣ（＝Ｏ）Ｃ
１～４
アルキルからなる群から選択され、
Ｒ
３
が、Ｈ及びＦからなる群から選択される、使用のための化合物。
［２］ 塩基が、（ｂ－４）又は（ｂ－８）である、上記［１］に記載の使用のための化合物。
［３］ Ｒ
１
が、Ｈ及びＣ（＝Ｏ）Ｃ
１～４
アルキルからなる群から選択される、上記［１］又は［２］に記載の使用のための化合物。
［４］ Ｒ
１
が、Ｈである、上記［１］～［３］のいずれか一項に記載の使用のための化合物。
［５］ Ｒ
１
が、Ｃ（＝Ｏ）Ｃ
１～４
アルキルである、上記［１］～［３］のいずれか一項に記載の使用のための化合物。
［６］ Ｒ
２
が、Ｃ（＝Ｏ）Ｃ
１～４
アルキルである、上記［１］～［５］のいずれか一項に記載の使用のための化合物。
［７］ Ｒ
３
が、Ｆである、上記［１］～［６］のいずれか一項に記載の使用のための化合物。
［８］ 前記化合物が、
［９］ 前記化合物が、以下である、上記［１］に記載の使用のための化合物。
［１１］ 前記Ｅ型肝炎感染症が、慢性ＨＥＶ感染症である、上記［１］～［９］のいずれか一項に記載の使用のための化合物、又は上記［１０］に記載の使用のための医薬組成物。
［１２］ 前記ＨＥＶ感染症が、遺伝子型１、遺伝子型２、又は遺伝子型３のものである、上記［１］～［９］のいずれか一項に記載の使用のための化合物、又は上記［１０］に記載の使用のための医薬組成物。
［１３］ 前記対象が、妊婦、免疫不全対象、又は免疫欠損対象である、上記［１］～［９］のいずれか一項に記載の使用のための化合物、又は上記［１０］に記載の使用のための医薬組成物。
All references (e.g., literature or patents or patent applications) cited herein are incorporated by reference in their entirety for all purposes to the same extent as if each individual reference (e.g., literature or patent or patent application) was specifically and individually indicated to be incorporated by reference in its entirety for all purposes. Other embodiments are within the scope of the following claims.
The following aspects may be included.
[1] A compound for use in treating a hepatitis E infection in a subject in need thereof, the compound being represented by the following formula (I):
In the formula,
the base is selected from the group consisting of (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), and (b-8);
R 2 is selected from the group consisting of H and C(═O)C 1-4 alkyl;
The compound for use wherein R3 is selected from the group consisting of H and F.
[2] The compound for use according to the above [1], wherein the base is (b-4) or (b-8).
[3] The compound for use according to the above [1] or [2], wherein R 1 is selected from the group consisting of H and C(═O)C 1-4 alkyl.
[4] The compound for use according to any one of the above [1] to [3], wherein R 1 is H.
[5] The compound for use according to any one of the above [1] to [3], wherein R 1 is C(═O)C 1-4 alkyl.
[6] The compound for use according to any one of the above [1] to [5], wherein R 2 is C(═O)C 1-4 alkyl.
[7] The compound for use according to any one of the above [1] to [6], wherein R 3 is F.
[8] The compound,
[9] The compound for use according to the above-mentioned [1], wherein the compound is:
[11] The compound for use according to any one of the above-mentioned [1] to [9], or the pharmaceutical composition for use according to the above-mentioned [10], wherein the hepatitis E infection is a chronic HEV infection.
[12] The compound for use according to any one of the above-mentioned [1] to [9], or the pharmaceutical composition for use according to the above-mentioned [10], wherein the HEV infection is of genotype 1, genotype 2, or genotype 3.
[13] The compound for use according to any one of the above-mentioned [1] to [9], or the pharmaceutical composition for use according to the above-mentioned [10], wherein the subject is a pregnant woman, an immunocompromised subject, or an immunodeficient subject.
Claims (13)
以下の式（Ｉ）の化合物
式中、
塩基が、以下の（ｂ－１）、（ｂ－２）、（ｂ－３）、（ｂ－４）、（ｂ－５）、（ｂ－６）、（ｂ－７）、及び（ｂ－８）からなる群から選択され、
Ｒ２が、Ｈ及びＣ（＝Ｏ）Ｃ１～４アルキルからなる群から選択され、
Ｒ３が、Ｈ及びＦからなる群から選択される、
医薬組成物。 1. A pharmaceutical composition for use in treating a Hepatitis E (HEV) infection in a subject in need thereof, comprising:
A compound of formula (I)
In the formula,
the base is selected from the group consisting of (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), and (b-8);
R 2 is selected from the group consisting of H and C(═O)C 1-4 alkyl;
R3 is selected from the group consisting of H and F;
Pharmaceutical compositions .
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP20169486 | 2020-04-14 | ||
| EP20169486.6 | 2020-04-14 | ||
| PCT/EP2021/059510 WO2021209425A1 (en) | 2020-04-14 | 2021-04-13 | Alkynyl nucleoside analogs for treatment of hepatitis e |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2023521425A JP2023521425A (en) | 2023-05-24 |
| JPWO2021209425A5 true JPWO2021209425A5 (en) | 2024-04-19 |
Family
ID=70289603
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022562248A Pending JP2023521425A (en) | 2020-04-14 | 2021-04-13 | Alkynyl nucleoside analogues for the treatment of hepatitis E |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20230201239A1 (en) |
| EP (1) | EP4138850A1 (en) |
| JP (1) | JP2023521425A (en) |
| CN (1) | CN115916217A (en) |
| AU (1) | AU2021256669A1 (en) |
| BR (1) | BR112022020820A2 (en) |
| CA (1) | CA3174637A1 (en) |
| MX (1) | MX2022012901A (en) |
| WO (1) | WO2021209425A1 (en) |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR072906A1 (en) | 2008-08-06 | 2010-09-29 | Novartis Ag | MODIFIED NUCLEOSIDS USEFUL AS ANTIVIRAL |
| CA2966033A1 (en) * | 2014-10-31 | 2016-05-06 | Cocrystal Pharma, Inc. | 2',2'-dihalo nucleoside analogs for treatment of the flaviviridae family of viruses and cancer |
| EP3288957A4 (en) * | 2015-05-01 | 2019-01-23 | Cocrystal Pharma, Inc. | Nucleoside analogs for treatment of the flaviviridae family of viruses and cancer |
| CN109689063A (en) * | 2016-04-28 | 2019-04-26 | 埃默里大学 | Nucleotide containing alkynes and nucleosides therapeutic combination and its associated uses |
-
2021
- 2021-04-13 US US17/995,945 patent/US20230201239A1/en active Pending
- 2021-04-13 WO PCT/EP2021/059510 patent/WO2021209425A1/en unknown
- 2021-04-13 MX MX2022012901A patent/MX2022012901A/en unknown
- 2021-04-13 EP EP21716788.1A patent/EP4138850A1/en active Pending
- 2021-04-13 JP JP2022562248A patent/JP2023521425A/en active Pending
- 2021-04-13 AU AU2021256669A patent/AU2021256669A1/en active Pending
- 2021-04-13 CN CN202180027994.4A patent/CN115916217A/en active Pending
- 2021-04-13 BR BR112022020820A patent/BR112022020820A2/en unknown
- 2021-04-13 CA CA3174637A patent/CA3174637A1/en active Pending
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