JPWO2021089419A5 - - Google Patents

Download PDF

Info

Publication number
JPWO2021089419A5
JPWO2021089419A5 JP2022525916A JP2022525916A JPWO2021089419A5 JP WO2021089419 A5 JPWO2021089419 A5 JP WO2021089419A5 JP 2022525916 A JP2022525916 A JP 2022525916A JP 2022525916 A JP2022525916 A JP 2022525916A JP WO2021089419 A5 JPWO2021089419 A5 JP WO2021089419A5
Authority
JP
Japan
Prior art keywords
cell lymphoma
pharmaceutically acceptable
formula
acceptable salt
compound
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
JP2022525916A
Other languages
Japanese (ja)
Other versions
JP2023501317A (en
Publication date
Application filed filed Critical
Priority claimed from PCT/EP2020/080493 external-priority patent/WO2021089419A1/en
Publication of JP2023501317A publication Critical patent/JP2023501317A/en
Publication of JPWO2021089419A5 publication Critical patent/JPWO2021089419A5/ja
Pending legal-status Critical Current

Links

Description

上記で引用された全ての参考文献（特許及び非特許）は、参照により本特許出願に組み込まれる。これらの参考文献の考察は、単にそれらの著者によりなされた主張を要約することを意図している。任意の参考文献（又は任意の参考文献の一部）が関連する先行技術（又はあらゆる先行技術）であることを、何ら承認するものではない。出願人は、引用された参考文献の正確さ及び妥当性に異議を唱える権利を留保する。
本発明には、次の態様が含まれる。
［項１］ Ｂ細胞悪性腫瘍の処置が必要なヒト対象においてそれを処置する方法であって、式Ｉの化合物：
［化１］

Figure 2021089419000011
又はその薬学的に許容される塩の第１の量、及び式ＩＩの化合物：
［化２］
Figure 2021089419000012
又はその薬学的に許容される塩の第２の量を前記ヒト対象に投与することを含み、前記第１の量及び前記第２の量が、合わせて治療有効量を構成する、方法。
［項２］ 前記Ｂ細胞悪性腫瘍が、非ホジキンリンパ腫である、項１に記載の方法。
［項３］ 前記Ｂ細胞悪性腫瘍が、マントル細胞リンパ腫；濾胞性リンパ腫；初発びまん性大細胞型Ｂ細胞リンパ腫；形質転換びまん性大細胞型Ｂ細胞リンパ腫；Ｔ細胞／組織球豊富型大細胞型Ｂ細胞リンパ腫；原発性皮膚びまん性大細胞型Ｂ細胞リンパ腫；下肢型原発性皮膚びまん性大細胞型Ｂ細胞リンパ腫；エプスタイン・バーウイルス陽性びまん性大細胞型Ｂ細胞リンパ腫；慢性炎症に伴うびまん性大細胞型Ｂ細胞リンパ腫；原発性縦隔大細胞型Ｂ細胞リンパ腫；血管内大細胞型Ｂ細胞リンパ腫；未分化リンパ腫キナーゼ陽性（ＡＬＫ＋）大細胞型Ｂ細胞リンパ腫；並びにＭＹＣ及びＢＣＬ２又はＢＣＬ６及びＭＹＣの再構成を伴う高悪性度Ｂ細胞リンパ腫からなる群から選択される、項１に記載の方法。
［項４］ 前記Ｂ細胞悪性腫瘍が、初発びまん性大細胞型Ｂ細胞リンパ腫；形質転換びまん性大細胞型Ｂ細胞リンパ腫；Ｔ細胞／組織球豊富型大細胞型Ｂ細胞リンパ腫；原発性皮膚びまん性大細胞型Ｂ細胞リンパ腫；下肢型原発性皮膚びまん性大細胞型Ｂ細胞リンパ腫；エプスタイン・バーウイルス陽性びまん性大細胞型Ｂ細胞リンパ腫；慢性炎症に伴うびまん性大細胞型Ｂ細胞リンパ腫；原発性縦隔大細胞型Ｂ細胞リンパ腫；血管内大細胞型Ｂ細胞リンパ腫；未分化リンパ腫キナーゼ陽性（ＡＬＫ＋）大細胞型Ｂ細胞リンパ腫；並びにＭＹＣ及びＢＣＬ２又はＢＣＬ６及びＭＹＣの再構成を伴う高悪性度Ｂ細胞リンパ腫からなる群から選択される、項１に記載の方法。
［項５］ 前記Ｂ細胞悪性腫瘍が、びまん性大細胞型Ｂ細胞リンパ腫である、項１に記載の方法。
［項６］ 前記びまん性大細胞型Ｂ細胞リンパ腫が、初発びまん性大細胞型Ｂ細胞リンパ腫、再発性／難治性びまん性大細胞型Ｂ細胞リンパ腫、及び形質転換びまん性大細胞型Ｂ細胞リンパ腫からなる群から選択される、項５に記載の方法。
［項７］ 前記びまん性大細胞型Ｂ細胞リンパ腫が、胚中心Ｂ細胞びまん性大細胞型Ｂ細胞リンパ腫及び活性化Ｂ細胞びまん性大細胞型Ｂ細胞リンパ腫からなる群から選択される、項５に記載の方法。
［項８］ 前記びまん性大細胞型Ｂ細胞リンパ腫が、活性化Ｂ細胞びまん性大細胞型Ｂ細胞リンパ腫である、項５に記載の方法。
［項９］ 前記ヒト対象が、前記びまん性大細胞型Ｂ細胞リンパ腫に対する少なくとも１種の事前の化学免疫療法を既に受けている、項５～８のいずれか一項に記載の方法。
［項１０］ 前記式Ｉの化合物、又はその薬学的に許容される塩、及び前記式ＩＩの化合物、又はその薬学的に許容される塩を、前記ヒト対象に経口投与することを含む、項１～９のいずれか一項に記載の方法。
［項１１］ 前記式Ｉの化合物、又はその薬学的に許容される塩が、前記式ＩＩの化合物、又はその薬学的に許容される塩と共に前記ヒト対象に経口共投与される、項１１に記載の方法。
［項１２］ 前記式Ｉの化合物、又はその薬学的に許容される塩が、前記式ＩＩの化合物、又はその薬学的に許容される塩の前又は後に、前記ヒト対象に経口投与される、項１１に記載の方法。
［項１３］ 前記ヒト対象に投与される前記式Ｉの化合物、又はその薬学的に許容される塩の前記第１の量が、１日約７５ｍｇ～約２２５ｍｇである、項１～１２のいずれか一項に記載の方法。
［項１４］ 前記ヒト対象に投与される前記式Ｉの化合物、又はその薬学的に許容される塩の前記第１の量が、１日１回、約１００ｍｇである、項１～１２のいずれか一項に記載の方法。
［項１５］ 前記ヒト対象に投与される前記式Ｉの化合物、又はその薬学的に許容される塩の前記第１の量が、１日２回、約１００ｍｇである、項１～１２のいずれか一項に記載の方法。
［項１６］ 前記式Ｉの化合物、又はその薬学的に許容される塩が、連続投与スケジュール下にて前記ヒト対象に経口投与される、項１～１５のいずれか一項に記載の方法。
［項１７］ 前記式ＩＩの化合物、又はその薬学的に許容される塩が、断続的投与スケジュール下にて前記ヒト対象に経口投与される、項１～１５のいずれか一項に記載の方法。
［項１８］ 前記式Ｉの化合物、又はその薬学的に許容される塩が、連続投与スケジュール下にて前記ヒト対象に経口投与され；且つ
前記式ＩＩの化合物、又はその薬学的に許容される塩が、断続的投与スケジュール下にて前記ヒト対象に経口投与される、項１～１５のいずれか一項に記載の方法。
［項１９］ 前記ヒト対象に投与される前記式ＩＩの化合物、又はその薬学的に許容される塩の前記第２の量が、１日２回約５０ｍｇ～１日２回約９００ｍｇである、項１～１８のいずれか一項に記載の方法。
［項２０］ 同時に、別個に、又は逐次的に投与するための組み合わせであって、式Ｉの化合物：
［化３］
Figure 2021089419000013
又はその薬学的に許容される塩と、式ＩＩの化合物：
［化４］
Figure 2021089419000014
又はその薬学的に許容される塩と、を含む、組み合わせ。
［項２１］ Ｂ細胞悪性腫瘍を処置するための、式Ｉの化合物：
［化５］
Figure 2021089419000015
又はその薬学的に許容される塩と、式ＩＩの化合物：
［化６］
Figure 2021089419000016
［項２２］ Ｂ細胞悪性腫瘍を処置するための薬剤を製造する際の、式Ｉの化合物：
［化７］
Figure 2021089419000017
又はその薬学的に許容される塩と、式ＩＩの化合物：
［化８］
Figure 2021089419000018
又はその薬学的に許容される塩と、を含む組み合わせの使用。
［項２３］ 式Ｉの化合物：
［化９］
Figure 2021089419000019
又はその薬学的に許容される塩と；
式ＩＩの化合物：
［化１０］
Figure 2021089419000020
又はその薬学的に許容される塩と；
薬学的に許容される担体と、を含む、医薬組成物。
［項２４］ 式Ｉの化合物：
［化１１］
Figure 2021089419000021
又はその薬学的に許容される塩と、薬学的に許容される担体と、を含む第１の医薬組成物と；
式ＩＩの化合物：
［化１２］
Figure 2021089419000022
又はその薬学的に許容される塩と、
薬学的に許容される担体と、を含む第２の医薬組成物と、を含む、キット。 All references (patent and non-patent) cited above are incorporated by reference into this patent application. The discussion of these references is merely intended to summarize the claims made by their authors. There is no admission that any reference (or part of any reference) is relevant prior art (or any prior art). Applicant reserves the right to challenge the accuracy and validity of cited references.
The present invention includes the following aspects.
[Section 1] A method of treating a B-cell malignancy in a human subject in need thereof, the method comprising: a compound of formula I:
[Chemical formula 1]
Figure 2021089419000011
or a first amount of a pharmaceutically acceptable salt thereof, and a compound of Formula II:
[Chemical 2]
Figure 2021089419000012
or a pharmaceutically acceptable salt thereof, to said human subject, said first amount and said second amount together comprising a therapeutically effective amount.
[Item 2] The method according to Item 1, wherein the B cell malignant tumor is non-Hodgkin's lymphoma.
[Section 3] The B-cell malignant tumor is mantle cell lymphoma; follicular lymphoma; newly diagnosed diffuse large B-cell lymphoma; transformed diffuse large B-cell lymphoma; T cell/histiocyte-rich large cell lymphoma B-cell lymphoma; primary cutaneous diffuse large B-cell lymphoma; primary cutaneous diffuse large B-cell lymphoma of the lower limb type; Epstein-Barr virus-positive diffuse large B-cell lymphoma; diffuse associated with chronic inflammation Large B-cell lymphoma; primary mediastinal large B-cell lymphoma; intravascular large B-cell lymphoma; anaplastic lymphoma kinase-positive (ALK+) large B-cell lymphoma; and MYC and BCL2 or BCL6 and MYC The method according to item 1, wherein the method is selected from the group consisting of high-grade B-cell lymphoma with rearrangement.
[Section 4] The B-cell malignant tumor is primary diffuse large B-cell lymphoma; transformed diffuse large B-cell lymphoma; T-cell/histiocyte-rich large B-cell lymphoma; primary cutaneous diffuse Large B-cell lymphoma; primary cutaneous diffuse large B-cell lymphoma of the lower limb type; Epstein-Barr virus-positive diffuse large B-cell lymphoma; diffuse large B-cell lymphoma associated with chronic inflammation; primary mediastinal large B-cell lymphoma; intravascular large B-cell lymphoma; anaplastic lymphoma kinase-positive (ALK+) large B-cell lymphoma; and high-grade with MYC and BCL2 or BCL6 and MYC rearrangements. The method according to item 1, wherein the patient is selected from the group consisting of B cell lymphoma.
[Item 5] The method according to Item 1, wherein the B cell malignant tumor is diffuse large B cell lymphoma.
[Section 6] The diffuse large B-cell lymphoma is newly diagnosed diffuse large B-cell lymphoma, relapsed/refractory diffuse large B-cell lymphoma, and transformed diffuse large B-cell lymphoma. The method according to item 5, wherein the method is selected from the group consisting of.
[Item 7] Item 5, wherein the diffuse large B-cell lymphoma is selected from the group consisting of germinal center B-cell diffuse large B-cell lymphoma and activated B-cell diffuse large B-cell lymphoma. The method described in.
[Item 8] The method according to Item 5, wherein the diffuse large B-cell lymphoma is activated B-cell diffuse large B-cell lymphoma.
[Item 9] The method according to any one of Items 5 to 8, wherein the human subject has already received at least one prior chemoimmunotherapy against the diffuse large B-cell lymphoma.
[Item 10] A clause comprising orally administering the compound of Formula I, or a pharmaceutically acceptable salt thereof, and the compound of Formula II, or a pharmaceutically acceptable salt thereof to the human subject. 10. The method according to any one of 1 to 9.
[Item 11] The compound of Formula I, or a pharmaceutically acceptable salt thereof, is orally co-administered to the human subject with the compound of Formula II, or a pharmaceutically acceptable salt thereof. Method described.
[Section 12] The compound of Formula I, or a pharmaceutically acceptable salt thereof, is orally administered to the human subject before or after the compound of Formula II, or a pharmaceutically acceptable salt thereof. The method according to item 11.
[Item 13] Any of Items 1 to 12, wherein the first amount of the compound of Formula I, or a pharmaceutically acceptable salt thereof, administered to the human subject is about 75 mg to about 225 mg per day. The method described in paragraph (1).
[Item 14] Any of Items 1 to 12, wherein the first amount of the compound of Formula I, or a pharmaceutically acceptable salt thereof, administered to the human subject is about 100 mg once a day. The method described in paragraph (1).
[Item 15] Any of Items 1 to 12, wherein the first amount of the compound of Formula I, or a pharmaceutically acceptable salt thereof, administered to the human subject is about 100 mg twice a day. The method described in paragraph (1).
[Item 16] The method according to any one of Items 1 to 15, wherein the compound of Formula I, or a pharmaceutically acceptable salt thereof, is orally administered to the human subject under a continuous administration schedule.
[Item 17] The method according to any one of Items 1 to 15, wherein the compound of Formula II, or a pharmaceutically acceptable salt thereof, is orally administered to the human subject under an intermittent dosing schedule. .
[Section 18] The compound of Formula I, or a pharmaceutically acceptable salt thereof, is orally administered to the human subject on a continuous administration schedule; and
16. The method of any one of paragraphs 1-15, wherein said compound of Formula II, or a pharmaceutically acceptable salt thereof, is orally administered to said human subject under an intermittent dosing schedule.
[Item 19] The second amount of the compound of Formula II, or a pharmaceutically acceptable salt thereof, administered to the human subject is from about 50 mg twice a day to about 900 mg twice a day. The method according to any one of items 1 to 18.
[Section 20] A combination for simultaneous, separate or sequential administration of a compound of formula I:
[Chemical 3]
Figure 2021089419000013
or a pharmaceutically acceptable salt thereof and a compound of formula II:
[C4]
Figure 2021089419000014
or a pharmaceutically acceptable salt thereof.
[Section 21] Compounds of formula I for treating B cell malignancies:
[C5]
Figure 2021089419000015
or a pharmaceutically acceptable salt thereof and a compound of formula II:
[Case 6]
Figure 2021089419000016
[Section 22] Compounds of formula I in the manufacture of medicaments for treating B cell malignancies:
[C7]
Figure 2021089419000017
or a pharmaceutically acceptable salt thereof and a compound of formula II:
[Chem.8]
Figure 2021089419000018
or a pharmaceutically acceptable salt thereof.
[Section 23] Compound of formula I:
[Chem.9]
Figure 2021089419000019
or a pharmaceutically acceptable salt thereof;
Compound of formula II:
[Chemical formula 10]
Figure 2021089419000020
or a pharmaceutically acceptable salt thereof;
A pharmaceutical composition comprising: a pharmaceutically acceptable carrier.
[Section 24] Compound of formula I:
[Chemical formula 11]
Figure 2021089419000021
or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier;
Compound of formula II:
[Chemical formula 12]
Figure 2021089419000022
or a pharmaceutically acceptable salt thereof;
a second pharmaceutical composition comprising: a pharmaceutically acceptable carrier;

Claims (24)

Ｂ細胞悪性腫瘍の処置が必要なヒト対象においてそれを処置するための医薬であって、式Ｉの化合物：
Figure 2021089419000001
 又はその薬学的に許容される塩の第１の量と、式ＩＩの化合物：
Figure 2021089419000002
 又はその薬学的に許容される塩の第２の量を含み、
前記式Ｉの化合物又はその薬学的に許容される塩と、前記式ＩＩの化合物又はその薬学的に許容される塩が、前記ヒト対象に同時に、別個に、又は逐次的に投与され、
前記第１の量及び前記第２の量が、合わせて治療有効量を構成する、医薬。 A medicament for the treatment of a B-cell malignancy in a human subject in need thereof, comprising a compound of formula I:
Figure 2021089419000001
 or a first amount of a pharmaceutically acceptable salt thereof , and a compound of formula II:
Figure 2021089419000002
 or a second amount of a pharmaceutically acceptable salt thereof ;
said compound of formula I or a pharmaceutically acceptable salt thereof and said compound of formula II or a pharmaceutically acceptable salt thereof are administered to said human subject simultaneously, separately, or sequentially ;
A medicament , wherein said first amount and said second amount together constitute a therapeutically effective amount. 前記Ｂ細胞悪性腫瘍が、非ホジキンリンパ腫である、請求項１に記載の医薬。 The medicament according to claim 1, wherein the B cell malignant tumor is non-Hodgkin's lymphoma. 前記Ｂ細胞悪性腫瘍が、マントル細胞リンパ腫；濾胞性リンパ腫；初発びまん性大細胞型Ｂ細胞リンパ腫；形質転換びまん性大細胞型Ｂ細胞リンパ腫；Ｔ細胞／組織球豊富型大細胞型Ｂ細胞リンパ腫；原発性皮膚びまん性大細胞型Ｂ細胞リンパ腫；下肢型原発性皮膚びまん性大細胞型Ｂ細胞リンパ腫；エプスタイン・バーウイルス陽性びまん性大細胞型Ｂ細胞リンパ腫；慢性炎症に伴うびまん性大細胞型Ｂ細胞リンパ腫；原発性縦隔大細胞型Ｂ細胞リンパ腫；血管内大細胞型Ｂ細胞リンパ腫；未分化リンパ腫キナーゼ陽性（ＡＬＫ＋）大細胞型Ｂ細胞リンパ腫；並びにＭＹＣ及びＢＣＬ２又はＢＣＬ６及びＭＹＣの再構成を伴う高悪性度Ｂ細胞リンパ腫からなる群から選択される、請求項１に記載の医薬。 The B-cell malignant tumor is mantle cell lymphoma; follicular lymphoma; newly diagnosed diffuse large B-cell lymphoma; transformed diffuse large B-cell lymphoma; T-cell/histiocyte-rich large B-cell lymphoma; Primary cutaneous diffuse large B-cell lymphoma; Primary cutaneous diffuse large B-cell lymphoma of the lower limb type; Epstein-Barr virus-positive diffuse large B-cell lymphoma; Diffuse large B-cell lymphoma associated with chronic inflammation cellular lymphoma; primary mediastinal large B-cell lymphoma; intravascular large B-cell lymphoma; anaplastic lymphoma kinase-positive (ALK+) large B-cell lymphoma; and MYC and BCL2 or BCL6 and MYC rearrangements. The medicament according to claim 1, wherein the medicament is selected from the group consisting of high-grade B-cell lymphoma associated with high-grade B-cell lymphoma. 前記Ｂ細胞悪性腫瘍が、初発びまん性大細胞型Ｂ細胞リンパ腫；形質転換びまん性大細胞型Ｂ細胞リンパ腫；Ｔ細胞／組織球豊富型大細胞型Ｂ細胞リンパ腫；原発性皮膚びまん性大細胞型Ｂ細胞リンパ腫；下肢型原発性皮膚びまん性大細胞型Ｂ細胞リンパ腫；エプスタイン・バーウイルス陽性びまん性大細胞型Ｂ細胞リンパ腫；慢性炎症に伴うびまん性大細胞型Ｂ細胞リンパ腫；原発性縦隔大細胞型Ｂ細胞リンパ腫；血管内大細胞型Ｂ細胞リンパ腫；未分化リンパ腫キナーゼ陽性（ＡＬＫ＋）大細胞型Ｂ細胞リンパ腫；並びにＭＹＣ及びＢＣＬ２又はＢＣＬ６及びＭＹＣの再構成を伴う高悪性度Ｂ細胞リンパ腫からなる群から選択される、請求項１に記載の医薬。 The B-cell malignant tumor is primary diffuse large B-cell lymphoma; transformed diffuse large B-cell lymphoma; T-cell/histiocyte-rich large B-cell lymphoma; primary cutaneous diffuse large cell lymphoma. B-cell lymphoma; primary cutaneous diffuse large B-cell lymphoma of the lower extremity; Epstein-Barr virus-positive diffuse large B-cell lymphoma; diffuse large B-cell lymphoma associated with chronic inflammation; primary large mediastinum From cell-type B-cell lymphoma; intravascular large B-cell lymphoma; anaplastic lymphoma kinase-positive (ALK+) large B-cell lymphoma; and high-grade B-cell lymphoma with MYC and BCL2 or BCL6 and MYC rearrangements. The medicament according to claim 1, which is selected from the group consisting of: 前記Ｂ細胞悪性腫瘍が、びまん性大細胞型Ｂ細胞リンパ腫である、請求項１に記載の医薬。 The medicament according to claim 1, wherein the B cell malignant tumor is diffuse large B cell lymphoma. 前記びまん性大細胞型Ｂ細胞リンパ腫が、初発びまん性大細胞型Ｂ細胞リンパ腫、再発性／難治性びまん性大細胞型Ｂ細胞リンパ腫、及び形質転換びまん性大細胞型Ｂ細胞リンパ腫からなる群から選択される、請求項５に記載の医薬。 The diffuse large B-cell lymphoma is from the group consisting of newly diagnosed diffuse large B-cell lymphoma, relapsed/refractory diffuse large B-cell lymphoma, and transformed diffuse large B-cell lymphoma. The medicament according to claim 5, which is selected. 前記びまん性大細胞型Ｂ細胞リンパ腫が、胚中心Ｂ細胞びまん性大細胞型Ｂ細胞リンパ腫及び活性化Ｂ細胞びまん性大細胞型Ｂ細胞リンパ腫からなる群から選択される、請求項５に記載の医薬。 6. The diffuse large B-cell lymphoma of claim 5, wherein the diffuse large B-cell lymphoma is selected from the group consisting of germinal center B-cell diffuse large B-cell lymphoma and activated B-cell diffuse large B-cell lymphoma. Medicine . 前記びまん性大細胞型Ｂ細胞リンパ腫が、活性化Ｂ細胞びまん性大細胞型Ｂ細胞リンパ腫である、請求項５に記載の医薬。 The medicament according to claim 5, wherein the diffuse large B-cell lymphoma is an activated B-cell diffuse large B-cell lymphoma. 前記ヒト対象が、前記びまん性大細胞型Ｂ細胞リンパ腫に対する少なくとも１種の事前の化学免疫療法を既に受けている、請求項５～８のいずれか一項に記載の医薬。 Medicament according to any one of claims 5 to 8, wherein the human subject has already received at least one prior chemoimmunotherapy against the diffuse large B-cell lymphoma. 前記式Ｉの化合物又はその薬学的に許容される塩と、前記式ＩＩの化合物又はその薬学的に許容される塩が、前記ヒト対象に経口投与される、請求項１～９のいずれか一項に記載の医薬。 Claims 1-9, wherein the compound of Formula I or a pharmaceutically acceptable salt thereof and the compound of Formula II or a pharmaceutically acceptable salt thereof are orally administered to the human subject. The medicament according to any one of . 前記式Ｉの化合物又はその薬学的に許容される塩が、前記式ＩＩの化合物又はその薬学的に許容される塩と共に前記ヒト対象に経口共投与される、請求項１０に記載の医薬。 11. The compound of Formula I or a pharmaceutically acceptable salt thereof is orally co-administered to the human subject with the compound of Formula II or a pharmaceutically acceptable salt thereof. medicine . 前記式Ｉの化合物又はその薬学的に許容される塩が、前記式ＩＩの化合物又はその薬学的に許容される塩の前又は後に、前記ヒト対象に経口投与される、請求項１１に記載の医薬。 12. The compound of Formula I or a pharmaceutically acceptable salt thereof is orally administered to the human subject before or after the compound of Formula II or a pharmaceutically acceptable salt thereof. 12. The medicament according to 11. 前記ヒト対象に投与される前記式Ｉの化合物又はその薬学的に許容される塩の前記第１の量が、１日約７５ｍｇ～約２２５ｍｇである、請求項１～１２のいずれか一項に記載の医薬。 Any one of claims 1-12, wherein the first amount of the compound of Formula I or a pharmaceutically acceptable salt thereof administered to the human subject is about 75 mg to about 225 mg per day. Medicines listed in section. 前記ヒト対象に投与される前記式Ｉの化合物又はその薬学的に許容される塩の前記第１の量が、１日１回、約１００ｍｇである、請求項１～１２のいずれか一項に記載の医薬。 13. Any one of claims 1-12, wherein the first amount of the compound of formula I or a pharmaceutically acceptable salt thereof administered to the human subject is about 100 mg once a day. Medicines listed in section. 前記ヒト対象に投与される前記式Ｉの化合物又はその薬学的に許容される塩の前記第１の量が、１日２回、約１００ｍｇである、請求項１～１２のいずれか一項に記載の医薬。 13. Any one of claims 1 to 12, wherein the first amount of the compound of formula I or a pharmaceutically acceptable salt thereof administered to the human subject is about 100 mg twice a day. Medicines listed in section. 前記式Ｉの化合物又はその薬学的に許容される塩が、連続投与スケジュール下にて前記ヒト対象に経口投与される、請求項１～１５のいずれか一項に記載の医薬。 A medicament according to any one of claims 1 to 15, wherein the compound of formula I or a pharmaceutically acceptable salt thereof is orally administered to the human subject under a continuous administration schedule. 前記式ＩＩの化合物又はその薬学的に許容される塩が、断続的投与スケジュール下にて前記ヒト対象に経口投与される、請求項１～１５のいずれか一項に記載の医薬。 A medicament according to any one of claims 1 to 15, wherein the compound of formula II or a pharmaceutically acceptable salt thereof is orally administered to the human subject under an intermittent dosing schedule. 前記式Ｉの化合物又はその薬学的に許容される塩が、連続投与スケジュール下にて前記ヒト対象に経口投与され；且つ
前記式ＩＩの化合物又はその薬学的に許容される塩が、断続的投与スケジュール下にて前記ヒト対象に経口投与される、請求項１～１５のいずれか一項に記載の医薬。 said compound of formula I or a pharmaceutically acceptable salt thereof is orally administered to said human subject under a continuous dosing schedule; and said compound of formula II or a pharmaceutically acceptable salt thereof is 16. A medicament according to any one of claims 1 to 15, which is orally administered to said human subject under an intermittent administration schedule. 前記ヒト対象に投与される前記式ＩＩの化合物又はその薬学的に許容される塩の前記第２の量が、１日２回約５０ｍｇ～１日２回約９００ｍｇである、請求項１～１８のいずれか一項に記載の医薬。 Claim 1, wherein the second amount of the compound of Formula II, or a pharmaceutically acceptable salt thereof, administered to the human subject is from about 50 mg twice a day to about 900 mg twice a day. 19. The medicament according to any one of 18 to 18. 同時に、別個に、又は逐次的に投与するための組み合わせ医薬であって、式Ｉの化合物：
Figure 2021089419000003
 又はその薬学的に許容される塩と、式ＩＩの化合物：
Figure 2021089419000004
 又はその薬学的に許容される塩と、を含む、組み合わせ医薬。 A combination medicament for simultaneous, separate or sequential administration of a compound of formula I:
Figure 2021089419000003
 or a pharmaceutically acceptable salt thereof and a compound of formula II:
Figure 2021089419000004
 or a pharmaceutically acceptable salt thereof. Ｂ細胞悪性腫瘍を処置するための請求項２０に記載の組み合わせ医薬。 Combination medicament according to claim 20 for treating B cell malignancies. Ｂ細胞悪性腫瘍を処置するための薬剤を製造する際の、式Ｉの化合物：
Figure 2021089419000005
 又はその薬学的に許容される塩と、式ＩＩの化合物：
Figure 2021089419000006
 又はその薬学的に許容される塩と、を含む組み合わせの使用。 Compounds of formula I in the manufacture of medicaments for treating B-cell malignancies:
Figure 2021089419000005
 or a pharmaceutically acceptable salt thereof and a compound of formula II:
Figure 2021089419000006
 or a pharmaceutically acceptable salt thereof. 式Ｉの化合物：
Figure 2021089419000007
 又はその薬学的に許容される塩と；
式ＩＩの化合物：
Figure 2021089419000008
 又はその薬学的に許容される塩と；
薬学的に許容される担体と、を含む、医薬組成物。 Compounds of formula I:
Figure 2021089419000007
 or a pharmaceutically acceptable salt thereof;
Compound of formula II:
Figure 2021089419000008
 or a pharmaceutically acceptable salt thereof;
A pharmaceutical composition comprising: a pharmaceutically acceptable carrier. 式Ｉの化合物：
Figure 2021089419000009
 又はその薬学的に許容される塩と、薬学的に許容される担体と、を含む第１の医薬組成物と；
式ＩＩの化合物：
Figure 2021089419000010
 又はその薬学的に許容される塩と、
薬学的に許容される担体と、を含む第２の医薬組成物と、を含む、キット。 Compounds of formula I:
Figure 2021089419000009
 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier;
Compound of formula II:
Figure 2021089419000010
 or a pharmaceutically acceptable salt thereof;
a second pharmaceutical composition comprising: a pharmaceutically acceptable carrier;
JP2022525916A 2019-11-04 2020-10-30 Therapeutic combination of acalabrutinib and capivasertib for treating B-cell malignancies Pending JP2023501317A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962930208P 2019-11-04 2019-11-04
US62/930,208 2019-11-04
PCT/EP2020/080493 WO2021089419A1 (en) 2019-11-04 2020-10-30 Therapeutic combinations of acalabrutinib and capivasertib to treat b-cell malignancies

Publications (2)

Publication Number Publication Date
JP2023501317A JP2023501317A (en) 2023-01-18
JPWO2021089419A5 true JPWO2021089419A5 (en) 2023-10-13

Family

ID=73043259

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2022525916A Pending JP2023501317A (en) 2019-11-04 2020-10-30 Therapeutic combination of acalabrutinib and capivasertib for treating B-cell malignancies

Country Status (9)

Country Link
US (1) US20220401442A1 (en)
EP (1) EP4054582A1 (en)
JP (1) JP2023501317A (en)
KR (1) KR20220098175A (en)
CN (1) CN114728003A (en)
AU (1) AU2020381240C1 (en)
CA (1) CA3158321A1 (en)
MX (1) MX2022005250A (en)
WO (1) WO2021089419A1 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023230286A2 (en) * 2022-05-25 2023-11-30 Onconova Therapeutics, Inc. Methods and compositions for treating cancer
WO2024104561A1 (en) * 2022-11-15 2024-05-23 Astrazeneca Ab Therapeutic combinations of capivasertib and venetoclax

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UY31384A1 (en) 2007-10-11 2009-05-29 NEW HETEROCICLIC COMPOUNDS FOR THE INHIBITION OF PROTEIN KINASE B
HRP20212021T1 (en) 2011-07-19 2022-04-01 Merck Sharp & Dohme B.V. 4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides as btk-inhibitors
US20170071962A1 (en) * 2015-09-11 2017-03-16 Acerta Pharma B.V. Therapeutic Combinations of a Proteasome Inhibitor and a BTK Inhibitor
CN108430993A (en) * 2015-12-17 2018-08-21 吉利德科学公司 TANK- combination kinase inhibitor compounds
CN107344940B (en) * 2016-05-06 2020-04-21 广东东阳光药业有限公司 BTK inhibitors and uses thereof
TW202014184A (en) * 2018-04-30 2020-04-16 瑞典商阿斯特捷利康公司 Combinations for treating cancer

Similar Documents

Publication Publication Date Title
RU2757373C2 (en) Combination therapy with antitumor alkaloid
JP2012500180A5 (en)
RU2010133489A (en) USE OF GAMMA SECRETASE INHIBITORS FOR TREATMENT OF CANCER
JP2012515184A (en) How to treat colorectal cancer
US20110053991A1 (en) Treatment of Histone Deacetylase Mediated Disorders
TWI441639B (en) Combination comprising paclitaxel for treating ovarian cancer
CA2712747A1 (en) Combinatory cancer treatment
JP2002507571A (en) Antitumor composition containing a synergistic combination of anthracycline derivative and camptothecin derivative
JP2009536956A (en) Anticancer therapy
TW200306185A (en) Combinations comprising EPOTHILONES and anti-metabolites
JPWO2021089419A5 (en)
US20110182909A1 (en) Glufosfamide combination therapy
CN113573702A (en) Adansstat combinations for cancer treatment
CN100553634C (en) The epothilone derivate that is used for the treatment of multiple myeloma
JPWO2019211721A5 (en)
TW202333675A (en) Use of combination therapy for treating cancer
WO2024104561A1 (en) Therapeutic combinations of capivasertib and venetoclax
JPWO2020112765A5 (en)
TW201313225A (en) Antitumour combination comprising ombrabulin and cisplatin, associated with radiotherapy
TW201315461A (en) Antitumour combination comprising ombrabulin and cetuximab, associated with radiotherapy