JPWO2020113216A5 - - Google Patents
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- JPWO2020113216A5 JPWO2020113216A5 JP2021530883A JP2021530883A JPWO2020113216A5 JP WO2020113216 A5 JPWO2020113216 A5 JP WO2020113216A5 JP 2021530883 A JP2021530883 A JP 2021530883A JP 2021530883 A JP2021530883 A JP 2021530883A JP WO2020113216 A5 JPWO2020113216 A5 JP WO2020113216A5
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- Prior art keywords
- leukemia
- composition
- acute
- cancer
- combination according
- Prior art date
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- 239000000203 mixture Substances 0.000 claims description 52
- LQBVNQSMGBZMKD-UHFFFAOYSA-N 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-N-[3-nitro-4-(oxan-4-ylmethylamino)phenyl]sulfonyl-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical compound C=1C=C(Cl)C=CC=1C=1CC(C)(C)CCC=1CN(CC1)CCN1C(C=C1OC=2C=C3C=CNC3=NC=2)=CC=C1C(=O)NS(=O)(=O)C(C=C1[N+]([O-])=O)=CC=C1NCC1CCOCC1 LQBVNQSMGBZMKD-UHFFFAOYSA-N 0.000 claims description 18
- 150000001875 compounds Chemical class 0.000 claims description 18
- 229960001183 venetoclax Drugs 0.000 claims description 18
- 208000000429 Leukemia, Lymphocytic, Chronic, B-Cell Diseases 0.000 claims description 15
- 201000011510 cancer Diseases 0.000 claims description 14
- 239000008194 pharmaceutical composition Substances 0.000 claims description 12
- 206010000880 Acute myeloid leukaemia Diseases 0.000 claims description 11
- 206010024324 Leukaemias Diseases 0.000 claims description 11
- 208000007046 Leukemia, Myeloid, Acute Diseases 0.000 claims description 11
- 210000003719 B-Lymphocytes Anatomy 0.000 claims description 9
- 206010008958 Chronic lymphocytic leukaemia Diseases 0.000 claims description 9
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims description 9
- 206010026798 Mantle cell lymphomas Diseases 0.000 claims description 9
- 201000005787 hematologic cancer Diseases 0.000 claims description 9
- 201000003793 myelodysplastic syndrome Diseases 0.000 claims description 9
- 239000002246 antineoplastic agent Substances 0.000 claims description 8
- 206010012818 Diffuse large B-cell lymphoma Diseases 0.000 claims description 6
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims description 6
- 201000005510 acute lymphocytic leukemia Diseases 0.000 claims description 6
- 230000036210 malignancy Effects 0.000 claims description 6
- 201000007224 myeloproliferative neoplasm Diseases 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 5
- 239000011780 sodium chloride Substances 0.000 claims description 5
- 239000012453 solvate Substances 0.000 claims description 5
- 239000012268 protein inhibitor Substances 0.000 claims description 4
- 229940121649 protein inhibitors Drugs 0.000 claims description 4
- 206010001019 Acute promyelocytic leukaemia Diseases 0.000 claims description 3
- 206010073479 Acute undifferentiated leukaemia Diseases 0.000 claims description 3
- 206010073478 Anaplastic large-cell lymphoma Diseases 0.000 claims description 3
- 208000009899 Burkitt Lymphoma Diseases 0.000 claims description 3
- 206010014958 Eosinophilic leukaemia Diseases 0.000 claims description 3
- 208000008456 Leukemia, Myelogenous, Chronic, BCR-ABL Positive Diseases 0.000 claims description 3
- 208000002490 Leukemia, Myelomonocytic, Juvenile Diseases 0.000 claims description 3
- 208000000015 Leukemia, Neutrophilic, Chronic Diseases 0.000 claims description 3
- 208000005749 Leukemia, Promyelocytic, Acute Diseases 0.000 claims description 3
- 208000003747 Lymphoid Leukemia Diseases 0.000 claims description 3
- 208000008968 Lymphoma, Large-Cell, Anaplastic Diseases 0.000 claims description 3
- 102000008037 Myeloid-Lymphoid Leukemia Protein Human genes 0.000 claims description 3
- 108010075393 Myeloid-Lymphoid Leukemia Protein Proteins 0.000 claims description 3
- 201000011186 acute T cell leukemia Diseases 0.000 claims description 3
- 230000001058 adult Effects 0.000 claims description 3
- 201000006934 chronic myeloid leukemia Diseases 0.000 claims description 3
- 201000010903 chronic neutrophilic leukemia Diseases 0.000 claims description 3
- 201000005992 juvenile myelomonocytic leukemia Diseases 0.000 claims description 3
- 201000006439 lymphocytic leukemia Diseases 0.000 claims description 3
- HPLNQCPCUACXLM-PGUFJCEWSA-N 4-[4-[[2-(4-chlorophenyl)phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonylbenzamide Chemical compound C([C@@H](CCN(C)C)NC=1C(=CC(=CC=1)S(=O)(=O)NC(=O)C=1C=CC(=CC=1)N1CCN(CC=2C(=CC=CC=2)C=2C=CC(Cl)=CC=2)CC1)[N+]([O-])=O)SC1=CC=CC=C1 HPLNQCPCUACXLM-PGUFJCEWSA-N 0.000 claims description 2
- 208000003950 B-Cell Lymphoma Diseases 0.000 claims description 2
- JLYAXFNOILIKPP-KXQOOQHDSA-N Navitoclax Chemical compound C([C@@H](NC1=CC=C(C=C1S(=O)(=O)C(F)(F)F)S(=O)(=O)NC(=O)C1=CC=C(C=C1)N1CCN(CC1)CC1=C(CCC(C1)(C)C)C=1C=CC(Cl)=CC=1)CSC=1C=CC=CC=1)CN1CCOCC1 JLYAXFNOILIKPP-KXQOOQHDSA-N 0.000 claims description 2
- 229950004847 Navitoclax Drugs 0.000 claims description 2
- 239000006186 oral dosage form Substances 0.000 claims description 2
- 230000035772 mutation Effects 0.000 claims 5
- 102100004121 IDH1 Human genes 0.000 claims 4
- 101700024037 IDH1 Proteins 0.000 claims 4
- 101700066748 IDH3B Proteins 0.000 claims 4
- 101700030371 IDH2 Proteins 0.000 claims 2
- 102100002772 IDH2 Human genes 0.000 claims 2
- 102200002933 HSP90AA1 G97D Human genes 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000004301 light adaptation Effects 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000006011 modification reaction Methods 0.000 description 1
Description
本発明を、その提唱された特定の実施形態と共に説明してきたが、さらなる変更が可能であること、また本出願が、概して、本発明の原理に従って、ならびに本発明が関係する技術分野内での既知または通例の実施内に収まる、及び上記で示される本質的な特徴に適用され得る、及び添付の請求項の範囲内に従う本開示からの逸脱を含めて、本発明の任意の変形形態、用途、または適応を網羅するように意図されていることが理解されよう。
本発明は、例えば、以下の項目を提供する。
（項目１）
治療有効量の
またはその医薬的に許容される塩もしくは溶媒和物と、少なくとも１つのさらなる抗がん剤とを含む、医薬的組合せ。
（項目２）
前記抗がん剤がＢＣＬ－２（Ｂ細胞リンパ腫２）タンパク質阻害剤である、項目１に記載の医薬的組合せ。
（項目３）
前記ＢＣＬ－２タンパク質阻害剤が、ベネトクラクス、ナビトクラクス、及びＡＢＴ－７３７からなる群のうちの１つ以上から選択される、項目２に記載の医薬的組合せ。
（項目４）
前記組合せが化合物７及びベネトクラクスである、項目３に記載の医薬的組合せ。
（項目５）
前記化合物７及びベネトクラクスがいずれも経口用剤形である、項目４に記載の医薬的組合せ。
（項目６）
前記組合せが、化合物７及びベネトクラクスの両方を含む単一の医薬組成物である、項目４に記載の医薬的組合せ。
（項目７）
前記医薬組成物が経口投薬用組成物である、項目６に記載の医薬組成物。
（項目８）
前記経口投薬用組成物が錠剤である、項目７に記載の医薬組成物。
（項目９）
化合物７及びベネトクラクスが対象に同時投与される、項目４に記載の医薬組成物。
（項目１０）
化合物７及びベネトクラクスが同日内に対象に同時投与される、項目９に記載の医薬組成物。
（項目１１）
ベネトクラクスの投薬量が約１ｍｇ～約１５０ｍｇの範囲である、項目４に記載の医薬組成物。
（項目１２）
化合物７の投薬量が約１ｍｇ～約３００ｍｇの範囲である、項目４に記載の医薬組成物。
（項目１３）
ベネトクラクスの投薬量が約１ｍｇ～約１５０ｍｇの範囲である、項目７に記載の医薬組成物。
（項目１４）
化合物７の投薬量が約１ｍｇ～約３００ｍｇの範囲である、項目１３に記載の医薬組成物。
（項目１５）
対象におけるがんを治療する方法であって、その必要のある前記対象に、治療有効量の化合物７：
またはその医薬的に許容される塩もしくは溶媒和物と、少なくとも１つのさらなる抗がん剤とを投与することを含む、前記方法。
（項目１６）
前記さらなる抗がん剤がベネトクラクスである、項目１５に記載の方法。
（項目１７）
前記がんが血液悪性腫瘍またはＢ細胞悪性腫瘍である、項目１６に記載の方法。
（項目１８）
治療される前記Ｂ細胞悪性腫瘍が、マントル細胞リンパ腫（ＭＣＬ）、Ｂ細胞急性リンパ芽球性白血病（Ｂ－ＡＬＬ）、バーキットリンパ腫、慢性リンパ性白血病（ＣＬＬ）、小リンパ球性リンパ腫（ＳＬＬ）、及びびまん性大細胞型Ｂ細胞リンパ腫（ＤＬＢＣＬ）からなる群のうちの１つ以上から選択される、項目１７に記載の方法。
（項目１９）
前記がんが血液悪性腫瘍である、項目１６に記載の方法。
（項目２０）
前記血液悪性腫瘍が白血病である、項目１９に記載の方法。
（項目２１）
前記白血病が、急性リンパ性白血病、急性骨髄性白血病、急性前骨髄球性白血病、慢性リンパ性白血病、慢性骨髄性白血病、慢性好中球性白血病、急性未分化白血病、未分化大細胞リンパ腫、前リンパ球性白血病、若年性骨髄単球性白血病、成人Ｔ細胞急性リンパ性白血病、３系統骨髄異形成を伴う急性骨髄性白血病、混合系統白血病、好酸球性白血病、及び／またはマントル細胞リンパ腫である、項目２０に記載の方法。
（項目２２）
前記白血病が急性骨髄性白血病である、項目２１に記載の方法。
（項目２３）
前記がんが骨髄異形成症候群（ＭＤＳ）または骨髄増殖性腫瘍（ＭＰＮ）である、項目１６に記載の方法。
While the invention has been described with specific proposed embodiments thereof, it is recognized that further modifications are possible and that the application is generally understood in accordance with the principles of the invention and within the technical field to which the invention pertains. Any variation, use, of the invention, including departing from the present disclosure that falls within known or customary practice and may be applied to the essential features set forth above, and that falls within the scope of the appended claims , or adaptations.
The present invention provides, for example, the following items.
(Item 1)
a therapeutically effective amount of
or a pharmaceutical combination comprising a pharmaceutically acceptable salt or solvate thereof and at least one additional anticancer agent.
(Item 2)
A pharmaceutical combination according to item 1, wherein said anticancer agent is a BCL-2 (B cell lymphoma 2) protein inhibitor.
(Item 3)
3. The pharmaceutical combination of item 2, wherein said BCL-2 protein inhibitor is selected from one or more of the group consisting of venetoclax, navitoclax, and ABT-737.
(Item 4)
4. A pharmaceutical combination according to item 3, wherein said combination is compound 7 and venetoclax.
(Item 5)
5. A pharmaceutical combination according to item 4, wherein both compound 7 and venetoclax are in oral dosage form.
(Item 6)
5. Pharmaceutical combination according to item 4, wherein said combination is a single pharmaceutical composition comprising both compound 7 and venetoclax.
(Item 7)
7. A pharmaceutical composition according to item 6, wherein said pharmaceutical composition is an oral dosage composition.
(Item 8)
8. Pharmaceutical composition according to item 7, wherein said oral dosage composition is a tablet.
(Item 9)
5. The pharmaceutical composition of item 4, wherein Compound 7 and venetoclax are co-administered to the subject.
(Item 10)
10. The pharmaceutical composition of item 9, wherein Compound 7 and venetoclax are co-administered to the subject within the same day.
(Item 11)
5. The pharmaceutical composition of item 4, wherein the dosage of venetoclax ranges from about 1 mg to about 150 mg.
(Item 12)
5. The pharmaceutical composition of item 4, wherein the dosage of compound 7 ranges from about 1 mg to about 300 mg.
(Item 13)
8. The pharmaceutical composition of item 7, wherein the dosage of venetoclax ranges from about 1 mg to about 150 mg.
(Item 14)
14. The pharmaceutical composition of item 13, wherein the dosage of compound 7 ranges from about 1 mg to about 300 mg.
(Item 15)
A method of treating cancer in a subject comprising administering to said subject in need thereof a therapeutically effective amount of Compound 7:
or a pharmaceutically acceptable salt or solvate thereof and at least one additional anticancer agent.
(Item 16)
16. The method of item 15, wherein said additional anti-cancer agent is venetoclax.
(Item 17)
17. The method of item 16, wherein said cancer is a hematologic malignancy or a B-cell malignancy.
(Item 18)
The B-cell malignancies to be treated are mantle cell lymphoma (MCL), B-cell acute lymphoblastic leukemia (B-ALL), Burkitt's lymphoma, chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma (SLL) ), and diffuse large B-cell lymphoma (DLBCL).
(Item 19)
17. The method of item 16, wherein said cancer is a hematologic malignancy.
(Item 20)
20. The method of item 19, wherein said hematologic malignancy is leukemia.
(Item 21)
The leukemia is acute lymphocytic leukemia, acute myeloid leukemia, acute promyelocytic leukemia, chronic lymphocytic leukemia, chronic myeloid leukemia, chronic neutrophilic leukemia, acute undifferentiated leukemia, anaplastic large cell lymphoma, promyelocytic leukemia, Lymphocytic leukemia, juvenile myelomonocytic leukemia, adult T-cell acute lymphoblastic leukemia, acute myelogenous leukemia with trilineage myelodysplasia, mixed lineage leukemia, eosinophilic leukemia, and/or mantle cell lymphoma 21. The method of item 20.
(Item 22)
22. The method of item 21, wherein said leukemia is acute myeloid leukemia.
(Item 23)
17. The method of item 16, wherein said cancer is myelodysplastic syndrome (MDS) or myeloproliferative neoplasm (MPN).
Claims (40)
またはその医薬的に許容される塩もしくは溶媒和物と、少なくとも１つのさらなる抗がん剤とを含む、医薬的組合せ。 a therapeutically effective amount of
or a pharmaceutical combination comprising a pharmaceutically acceptable salt or solvate thereof and at least one additional anticancer agent.
またはその医薬的に許容される塩もしくは溶媒和物と、少なくとも１つのさらなる抗がん剤とを含む、組合せ。 Compound 7 for treating cancer in a subject:
or a combination comprising a pharmaceutically acceptable salt or solvate thereof and at least one additional anticancer agent.
またはその医薬的に許容される塩もしくは溶媒和物を含む組成物であって、前記対象が、ＩＤＨ１及び／またはＩＤＨ２の変異形態を有する、組成物。or a pharmaceutically acceptable salt or solvate thereof, wherein said subject has a mutant form of IDH1 and/or IDH2.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862773686P | 2018-11-30 | 2018-11-30 | |
| US62/773,686 | 2018-11-30 | ||
| PCT/US2019/063993 WO2020113216A1 (en) | 2018-11-30 | 2019-12-02 | Combination therapy with 2,3-dihydro-isoindole-1-one compounds and methods for treating patients with various mutations |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2022509257A JP2022509257A (en) | 2022-01-20 |
| JPWO2020113216A5 true JPWO2020113216A5 (en) | 2022-12-14 |
Family
ID=70849819
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021530883A Pending JP2022509257A (en) | 2018-11-30 | 2019-12-02 | Combination therapy with 2,3-dihydro-isoindole-1-one compounds and methods for treating patients with various mutations |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20200171001A1 (en) |
| EP (1) | EP3886840A4 (en) |
| JP (1) | JP2022509257A (en) |
| KR (1) | KR20210150353A (en) |
| CN (1) | CN113365622A (en) |
| AU (1) | AU2019387508A1 (en) |
| CA (1) | CA3133376A1 (en) |
| WO (1) | WO2020113216A1 (en) |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012047017A2 (en) * | 2010-10-05 | 2012-04-12 | 크리스탈지노믹스(주) | 2,3-dihydro-isoindol-1-one derivative and a composition comprising the same |
| EP2940014B1 (en) * | 2012-12-28 | 2018-09-26 | Crystalgenomics, Inc. | 2,3-dihydro-isoindole-1-on derivative as btk kinase suppressant, and pharmaceutical composition including same |
| CN105263496A (en) * | 2013-04-08 | 2016-01-20 | 药品循环有限责任公司 | Ibrutinib combination therapy |
| CA2994265A1 (en) * | 2015-08-03 | 2017-02-09 | Gilead Sciences, Inc. | Combination therapies for treating cancers |
| ES2905915T3 (en) * | 2015-12-04 | 2022-04-12 | Servier Lab | Treatment procedures for malignant neoplasms |
| EP3490553A4 (en) * | 2016-07-29 | 2020-03-25 | Oncternal Therapeutics, Inc. | Uses of indolinone compounds |
| US20200054639A1 (en) * | 2016-10-31 | 2020-02-20 | Oregon Health & Science University | Combinations of agents to treat hematological malignancies |
| TWI821174B (en) * | 2017-02-21 | 2023-11-11 | 加拿大商艾普托斯生物科學公司 | Methods for treating patients with hematolgic malignancies |
-
2019
- 2019-12-02 KR KR1020217019708A patent/KR20210150353A/en unknown
- 2019-12-02 AU AU2019387508A patent/AU2019387508A1/en active Pending
- 2019-12-02 WO PCT/US2019/063993 patent/WO2020113216A1/en unknown
- 2019-12-02 JP JP2021530883A patent/JP2022509257A/en active Pending
- 2019-12-02 EP EP19888779.6A patent/EP3886840A4/en active Pending
- 2019-12-02 US US16/700,426 patent/US20200171001A1/en active Pending
- 2019-12-02 CA CA3133376A patent/CA3133376A1/en active Pending
- 2019-12-02 CN CN201980090539.1A patent/CN113365622A/en active Pending
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