JP2021521138A - Bcl−2阻害剤 - Google Patents
Bcl−2阻害剤 Download PDFInfo
- Publication number
- JP2021521138A JP2021521138A JP2020555218A JP2020555218A JP2021521138A JP 2021521138 A JP2021521138 A JP 2021521138A JP 2020555218 A JP2020555218 A JP 2020555218A JP 2020555218 A JP2020555218 A JP 2020555218A JP 2021521138 A JP2021521138 A JP 2021521138A
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- Prior art keywords
- ring
- heterocyclyl
- alkyl
- compound according
- cycloalkyl
- Prior art date
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- 0 CC(C)(C)OC(C(CCCC1)*C1c(cccc1)c1Br)=O Chemical compound CC(C)(C)OC(C(CCCC1)*C1c(cccc1)c1Br)=O 0.000 description 82
- DHXVGJBLRPWPCS-UHFFFAOYSA-N C1CCOCC1 Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 description 1
- GNSVJYWRBFETPY-QMMMGPOBSA-N C1NC(N=CC2=C[C@@H]22)=C2C#C1 Chemical compound C1NC(N=CC2=C[C@@H]22)=C2C#C1 GNSVJYWRBFETPY-QMMMGPOBSA-N 0.000 description 1
- UZDAWRJAKREQHS-UHFFFAOYSA-N CC(C)C1=CC=C[I]=C1 Chemical compound CC(C)C1=CC=C[I]=C1 UZDAWRJAKREQHS-UHFFFAOYSA-N 0.000 description 1
- UQUHQKVINDTPNE-UHFFFAOYSA-N CC(CC1)CCN1N Chemical compound CC(CC1)CCN1N UQUHQKVINDTPNE-UHFFFAOYSA-N 0.000 description 1
- KNTRGPOHMOAXRI-KXGSVCODSA-N CC12C=CNC1[C@@H]2N Chemical compound CC12C=CNC1[C@@H]2N KNTRGPOHMOAXRI-KXGSVCODSA-N 0.000 description 1
- QEICMLKMFUWDPG-UHFFFAOYSA-O CC1=C(C[OH+]C)[Tl](C)CC1=C Chemical compound CC1=C(C[OH+]C)[Tl](C)CC1=C QEICMLKMFUWDPG-UHFFFAOYSA-O 0.000 description 1
- ITFNNPVTNIJTIP-UHFFFAOYSA-N CC1C(C)=CC=C(C)C1 Chemical compound CC1C(C)=CC=C(C)C1 ITFNNPVTNIJTIP-UHFFFAOYSA-N 0.000 description 1
- OVRKATYHWPCGPZ-UHFFFAOYSA-N CC1CCOCC1 Chemical compound CC1CCOCC1 OVRKATYHWPCGPZ-UHFFFAOYSA-N 0.000 description 1
- LTQRSLYAFGWNLJ-UHFFFAOYSA-N CC1N(C)[IH]CC=C1 Chemical compound CC1N(C)[IH]CC=C1 LTQRSLYAFGWNLJ-UHFFFAOYSA-N 0.000 description 1
- JOACFWQRHFKJOZ-UHFFFAOYSA-N CCC(CC)c1c(C2CC2)cccc1 Chemical compound CCC(CC)c1c(C2CC2)cccc1 JOACFWQRHFKJOZ-UHFFFAOYSA-N 0.000 description 1
- ARUPKXQNKYZPSQ-UHFFFAOYSA-N CCC1(CC[U]CC1)F Chemical compound CCC1(CC[U]CC1)F ARUPKXQNKYZPSQ-UHFFFAOYSA-N 0.000 description 1
- XKDAKRNKDAXFSZ-UHFFFAOYSA-N CCCC(CC)N1CCC(C)(C)CC1 Chemical compound CCCC(CC)N1CCC(C)(C)CC1 XKDAKRNKDAXFSZ-UHFFFAOYSA-N 0.000 description 1
- PEZIFOQHEIMSKF-UVTDQMKNSA-N CCCC(CCCC(C)=C)N(C1)C(C(C(C)C2CC2)/C(/C)=[I]/C)C(/C=C\C)=C1C=C Chemical compound CCCC(CCCC(C)=C)N(C1)C(C(C(C)C2CC2)/C(/C)=[I]/C)C(/C=C\C)=C1C=C PEZIFOQHEIMSKF-UVTDQMKNSA-N 0.000 description 1
- XJINZNWPEQMMBV-UHFFFAOYSA-N CCCCCCNC Chemical compound CCCCCCNC XJINZNWPEQMMBV-UHFFFAOYSA-N 0.000 description 1
- WOONFMKPGHLZIY-GRGQKVDUSA-N CCC[C@](C)(C1)C[C@@]1(C)N1C(CC(CC(C#CC2)[IH+])[C@H]2C2CC2)CCC1 Chemical compound CCC[C@](C)(C1)C[C@@]1(C)N1C(CC(CC(C#CC2)[IH+])[C@H]2C2CC2)CCC1 WOONFMKPGHLZIY-GRGQKVDUSA-N 0.000 description 1
- DUKQZHHRTGZMRY-UHFFFAOYSA-N CCC[U]CCF Chemical compound CCC[U]CCF DUKQZHHRTGZMRY-UHFFFAOYSA-N 0.000 description 1
- AIHBMMDTRKMDQW-UHFFFAOYSA-N C[C@H](CC1)CC[S@]1(C)OC Chemical compound C[C@H](CC1)CC[S@]1(C)OC AIHBMMDTRKMDQW-UHFFFAOYSA-N 0.000 description 1
- YKIVDJSUUNWXRY-RKDXNWHRSA-N C[C@H]1c2cc(C)cnc2[C@H](C)C1 Chemical compound C[C@H]1c2cc(C)cnc2[C@H](C)C1 YKIVDJSUUNWXRY-RKDXNWHRSA-N 0.000 description 1
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
- C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyrrole Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Priority Applications (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024094048A JP7540113B1 (ja) | 2018-04-29 | 2024-06-11 | Bcl-2阻害剤 |
| JP2024135320A JP7688210B2 (ja) | 2018-04-29 | 2024-08-14 | Bcl-2阻害剤 |
| JP2025085498A JP2025119001A (ja) | 2018-04-29 | 2025-05-22 | Bcl-2阻害剤 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2018085217 | 2018-04-29 | ||
| CNPCT/CN2018/085217 | 2018-04-29 | ||
| CN2018107134 | 2018-09-21 | ||
| CNPCT/CN2018/107134 | 2018-09-21 | ||
| PCT/CN2019/085001 WO2019210828A1 (en) | 2018-04-29 | 2019-04-29 | Bcl-2 INHIBITORS |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024094048A Division JP7540113B1 (ja) | 2018-04-29 | 2024-06-11 | Bcl-2阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021521138A true JP2021521138A (ja) | 2021-08-26 |
| JP2021521138A5 JP2021521138A5 (https=) | 2022-04-22 |
| JPWO2019210828A5 JPWO2019210828A5 (https=) | 2022-04-22 |
Family
ID=68386968
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020555218A Withdrawn JP2021521138A (ja) | 2018-04-29 | 2019-04-29 | Bcl−2阻害剤 |
| JP2024094048A Active JP7540113B1 (ja) | 2018-04-29 | 2024-06-11 | Bcl-2阻害剤 |
| JP2024135320A Active JP7688210B2 (ja) | 2018-04-29 | 2024-08-14 | Bcl-2阻害剤 |
| JP2025085498A Pending JP2025119001A (ja) | 2018-04-29 | 2025-05-22 | Bcl-2阻害剤 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024094048A Active JP7540113B1 (ja) | 2018-04-29 | 2024-06-11 | Bcl-2阻害剤 |
| JP2024135320A Active JP7688210B2 (ja) | 2018-04-29 | 2024-08-14 | Bcl-2阻害剤 |
| JP2025085498A Pending JP2025119001A (ja) | 2018-04-29 | 2025-05-22 | Bcl-2阻害剤 |
Country Status (22)
| Country | Link |
|---|---|
| US (3) | US11420968B2 (https=) |
| EP (2) | EP3788042B1 (https=) |
| JP (4) | JP2021521138A (https=) |
| KR (1) | KR102738032B1 (https=) |
| CN (3) | CN117683029A (https=) |
| AU (1) | AU2019264475C1 (https=) |
| BR (1) | BR112020022092A2 (https=) |
| CA (1) | CA3098348A1 (https=) |
| DK (1) | DK3788042T3 (https=) |
| ES (1) | ES3018793T3 (https=) |
| FI (1) | FI3788042T3 (https=) |
| HR (1) | HRP20250392T1 (https=) |
| HU (1) | HUE071493T2 (https=) |
| IL (1) | IL278366B2 (https=) |
| LT (1) | LT3788042T (https=) |
| MX (2) | MX2020011495A (https=) |
| PL (1) | PL3788042T3 (https=) |
| PT (1) | PT3788042T (https=) |
| SG (1) | SG11202009933WA (https=) |
| SI (1) | SI3788042T1 (https=) |
| TW (1) | TWI855062B (https=) |
| WO (1) | WO2019210828A1 (https=) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2024119916A (ja) * | 2018-04-29 | 2024-09-03 | ベイジーン リミテッド | Bcl-2阻害剤 |
| JP2024540534A (ja) * | 2021-12-06 | 2024-10-31 | 杭州和正医薬有限公司 | 抗アポトーシスタンパク質bcl-2阻害剤、医薬組成物及びその使用 |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3565815B1 (en) | 2017-01-07 | 2024-03-13 | Fochon Pharmaceuticals, Ltd. | Compounds as bcl-2-selective apoptosis-inducing agents |
| HUE060310T2 (hu) | 2017-04-18 | 2023-02-28 | Shanghai Fochon Pharmaceutical Co Ltd | Apoptosis-indukáló szerek |
| EP3737681A4 (en) | 2018-01-10 | 2022-01-12 | Recurium IP Holdings, LLC | BENZAMIDE COMPOUNDS |
| WO2020140005A2 (en) | 2018-12-29 | 2020-07-02 | Newave Pharmaceutical Inc. | Bcl-2 inhibitors |
| WO2021083135A1 (en) * | 2019-10-28 | 2021-05-06 | Beigene, Ltd. | Bcl-2 INHIBITORS |
| WO2021110102A1 (en) * | 2019-12-02 | 2021-06-10 | Beigene, Ltd. | Methods of cancer treatment using bcl-2 inhibitor |
| KR20220100992A (ko) | 2019-12-06 | 2022-07-18 | 록쏘 온콜로지, 인코포레이티드 | 브루톤 티로신 키나제 억제제의 투여 |
| WO2021133817A1 (en) | 2019-12-27 | 2021-07-01 | Guangzhou Lupeng Pharmaceutical Company Ltd. | 1h-pyrrolo[2,3-b]pyridine derivatives as bcl-2 inhibitors for the treatment of neoplastic and autoimmune diseases |
| JP7839962B2 (ja) * | 2020-04-15 | 2026-04-03 | ビーワン メディシンズ ワン ゲーエムベーハー | Bcl-2阻害剤 |
| EP4146649A4 (en) * | 2020-05-08 | 2024-09-11 | Fochon Biosciences, Ltd. | COMPOUNDS AS BCL-2 INHIBITORS |
| CN114478520B (zh) * | 2020-10-28 | 2025-01-10 | 杭州和正医药有限公司 | Bcl-2蛋白凋亡诱导剂及应用 |
| CN117642157A (zh) * | 2021-03-19 | 2024-03-01 | 伊尔治疗学股份有限公司 | 具有((3-硝基苯基)磺酰基)乙酰胺作为bcl-2抑制剂的化合物 |
| CN117616023A (zh) * | 2021-04-13 | 2024-02-27 | 爱新医药科技(香港)有限公司 | Bcl-2或bcl-2/bcl-xl调节剂及其用途 |
| EP4351542A4 (en) * | 2021-06-02 | 2025-04-09 | BeiGene Switzerland GmbH | Method for treating B-cell malignancy with BCL-2 inhibitor |
| CN115490708B (zh) * | 2021-06-18 | 2025-01-24 | 苏州亚盛药业有限公司 | 磺酰胺类大环衍生物及其制备方法和用途 |
| CA3230314A1 (en) * | 2021-08-31 | 2023-03-09 | Beigene Switzerland Gmbh | Solid forms of bcl-2 inhibitors, method of preparation, and use thereof |
| WO2023078398A1 (en) * | 2021-11-05 | 2023-05-11 | Fochon Pharmaceuticals, Ltd. | Compounds as bcl-2 inhibitors |
| US20250122191A1 (en) * | 2021-11-20 | 2025-04-17 | Fochon Biosciences, Ltd | Compounds as bcl-2 inhibitors |
| TW202400163A (zh) | 2022-05-12 | 2024-01-01 | 英屬開曼群島商百濟神州有限公司 | 使用bcl-2抑制劑治療髓性惡性腫瘤之方法 |
| CN119365456A (zh) * | 2022-06-01 | 2025-01-24 | 重庆复创医药研究有限公司 | 作为bcl-2抑制剂的化合物 |
| CN119584963A (zh) * | 2022-07-21 | 2025-03-07 | 百济神州(苏州)生物科技有限公司 | 使用bcl-2抑制剂治疗多发性骨髓瘤的方法 |
| WO2024140690A1 (en) * | 2022-12-27 | 2024-07-04 | Beigene (Suzhou) Co., Ltd. | Intermediates of sonrotoclax and the method of preparing the same |
| AU2023416871A1 (en) * | 2022-12-27 | 2025-08-14 | Beone Medicines I Gmbh | Salts and solid forms of sonrotoclax intermediate |
| WO2024140678A1 (en) * | 2022-12-27 | 2024-07-04 | Beigene (Suzhou) Co., Ltd. | A ketal protected intermediate for sonrotoclax and preparation method thereof |
| WO2026002056A1 (en) | 2024-06-26 | 2026-01-02 | Beone Pharmaceutical (Suzhou) Co., Ltd. | A pharmaceutical formulation comprising solid dispersion of sonrotoclax and a process of preparation thereof |
| WO2026019442A1 (en) * | 2024-07-14 | 2026-01-22 | Eil Therapeutics, Inc. | Compounds having (3-nitrophenyl)acetamide as bcl-2 inhibitors |
Citations (3)
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| JP2012528178A (ja) * | 2009-05-26 | 2012-11-12 | アボット・ラボラトリーズ | 癌ならびに免疫疾患および自己免疫疾患の治療用のアポトーシス誘発剤 |
| JP2013527202A (ja) * | 2010-05-26 | 2013-06-27 | アッヴィ・インコーポレイテッド | 癌ならびに免疫疾患および自己免疫疾患の治療用のアポトーシス誘発剤 |
| CN106749233A (zh) * | 2016-11-24 | 2017-05-31 | 中山大学 | 一类磺酰胺衍生物及其应用 |
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| CA2577752A1 (en) | 2004-08-20 | 2006-03-02 | The Regents Of The University Of Michigan | Small molecule inhibitors of anti-apoptotic bcl-2 family members and the uses thereof |
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| HUE029289T2 (en) | 2008-12-05 | 2017-02-28 | Abbvie Inc | Sulfonamide derivatives as Bcl-2 selective apoptosis inducers for the treatment of cancer and immune diseases |
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| AU2009326259A1 (en) | 2008-12-08 | 2011-07-28 | Boehringer Ingelheim International Gmbh | Compounds for treating cancer |
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| WO2011029842A1 (en) | 2009-09-10 | 2011-03-17 | Novartis Ag | Sulfonamides as inhibitors of bcl-2 family proteins for the treatment of cancer |
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| JP2024540534A (ja) * | 2021-12-06 | 2024-10-31 | 杭州和正医薬有限公司 | 抗アポトーシスタンパク質bcl-2阻害剤、医薬組成物及びその使用 |
| JP7765790B2 (ja) | 2021-12-06 | 2025-11-07 | 杭州和正医薬有限公司 | 抗アポトーシスタンパク質bcl-2阻害剤、医薬組成物及びその使用 |
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