EA201891988A1 - Ингибиторы mcl-1 на основе замещенных индолов - Google Patents
Ингибиторы mcl-1 на основе замещенных индоловInfo
- Publication number
- EA201891988A1 EA201891988A1 EA201891988A EA201891988A EA201891988A1 EA 201891988 A1 EA201891988 A1 EA 201891988A1 EA 201891988 A EA201891988 A EA 201891988A EA 201891988 A EA201891988 A EA 201891988A EA 201891988 A1 EA201891988 A1 EA 201891988A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- mcl
- inhibitors based
- indols
- substituted
- present
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D403/14—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 three or more hetero rings
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Abstract
В настоящем изобретении предусмотрены соединения, которые подавляют активность антиапоптотического белка 1, ассоциированного с миелоидным лейкозом (Mcl-1), представителя семейства Bcl-2. В настоящем изобретении также предусмотрены фармацевтические композиции, а также способы применения соединений для лечения заболеваний и состояний (например, рака), характеризующихся сверхэкспрессией или дисрегуляцией белка Mcl-1.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201662304124P | 2016-03-04 | 2016-03-04 | |
US201662402903P | 2016-09-30 | 2016-09-30 | |
PCT/US2017/020699 WO2017152076A1 (en) | 2016-03-04 | 2017-03-03 | Substituted indole mcl-1 inhibitors |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201891988A1 true EA201891988A1 (ru) | 2019-02-28 |
EA038143B1 EA038143B1 (ru) | 2021-07-13 |
Family
ID=59744491
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201891988A EA038143B1 (ru) | 2016-03-04 | 2017-03-03 | ИНГИБИТОРЫ Mcl-1 НА ОСНОВЕ ЗАМЕЩЕННЫХ ИНДОЛОВ |
Country Status (14)
Country | Link |
---|---|
US (2) | US11596639B2 (ru) |
EP (2) | EP3423435B1 (ru) |
JP (1) | JP7086395B2 (ru) |
KR (1) | KR102396177B1 (ru) |
CN (1) | CN109153643B (ru) |
AU (1) | AU2017228385B2 (ru) |
BR (1) | BR112018067775B1 (ru) |
CA (1) | CA3016182C (ru) |
CL (1) | CL2018002516A1 (ru) |
EA (1) | EA038143B1 (ru) |
IL (1) | IL261231B (ru) |
MX (1) | MX2018010678A (ru) |
PH (1) | PH12018501877A1 (ru) |
WO (1) | WO2017152076A1 (ru) |
Families Citing this family (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP3572416B1 (en) | 2014-01-24 | 2022-09-21 | Turning Point Therapeutics, Inc. | Diaryl macrocycles as modulators of protein kinases |
EP3122353B1 (en) | 2014-03-27 | 2020-10-28 | Vanderbilt University | Substituted indole mcl-1 inhibitors |
RU2732405C2 (ru) | 2015-07-02 | 2020-09-16 | Тёрнинг Поинт Терапьютикс, Инк. | Хиральные диарильные макроциклы в качестве модуляторов протеинкиназ |
EP3214092A1 (en) | 2016-03-04 | 2017-09-06 | Bayer Pharma Aktiengesellschaft | Prodrugs of the selective progesterone receptor modulator (sprm) (11.beta.,17.beta.)-17-hydroxy-11-[4-(methylsulphonyl)phenyl]-17-(pentafluoroethyl)estra-4,9-dien-3-one |
CN109715632B (zh) | 2016-05-19 | 2021-10-26 | 拜尔公开股份有限公司 | 大环吲哚衍生物 |
CN111757884B (zh) | 2017-11-17 | 2023-12-19 | 拜耳股份公司 | 取代的大环吲哚衍生物 |
EP3710449B1 (en) | 2017-11-17 | 2022-07-06 | The Broad Institute, Inc. | Macrocyclic fluorine substituted indole derivatives as mcl-1 inhibitors, for use in the treatment of cancer |
US11447504B2 (en) | 2017-11-17 | 2022-09-20 | Bayer Aktiengesellschaft | Macrocyclic chlorine substituted indole derivatives |
US11478451B1 (en) | 2017-11-17 | 2022-10-25 | Bayer Aktiengesellschaft | Macrocyclic chlorine substituted indole derivatives |
EP3710456B1 (en) * | 2017-11-17 | 2022-09-21 | The Broad Institute, Inc. | Macrocyclic indole derivatives |
US11760701B2 (en) | 2018-02-27 | 2023-09-19 | The Research Foundation For The State University Of New Yrok | Difluoromethoxylation and trifluoromethoxylation compositions and methods for synthesizing same |
WO2020048548A1 (zh) * | 2018-09-07 | 2020-03-12 | 正大天晴药业集团股份有限公司 | 一种作用于crbn蛋白的三并环类化合物 |
CN111904958B (zh) * | 2019-05-09 | 2022-09-13 | 浙江大学 | Umi-77作为线粒体自噬诱导剂在制备治疗炎症及神经退行性疾病药物中的应用 |
JP7209897B2 (ja) * | 2019-09-12 | 2023-01-20 | メッドシャイン ディスカバリー インコーポレイテッド | Crbnタンパク質モジュレーターとしての二環式化合物 |
US20220402893A1 (en) | 2019-11-25 | 2022-12-22 | Unimatec Co., Ltd. | Fluorine-containing pyrimidine compound and method for producing same |
CN116710430A (zh) * | 2020-05-12 | 2023-09-05 | 皮姆维制药公司 | 用于恢复突变p53功能的方法和化合物 |
CN113512025B (zh) * | 2020-07-31 | 2023-01-06 | 四川大学 | 一种吲唑酯类化合物及其制药用途 |
CN115785014A (zh) * | 2022-12-27 | 2023-03-14 | 瑞石生物医药有限公司 | 四唑衍生物及其用途 |
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DE4128015A1 (de) | 1991-08-23 | 1993-02-25 | Kali Chemie Pharma Gmbh | 1,7-anellierte 2-(piperazinoalkyl)indol-derivate sowie verfahren und zwischenprodukte zu ihrer herstellung und diese verbindugnen enthaltende arzneimittel |
EP0639573A1 (de) | 1993-08-03 | 1995-02-22 | Hoechst Aktiengesellschaft | Benzokondensierte 5-Ringheterocyclen, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament, ihre Verwendung als Diagnostikum, sowie sie enthaltendes Medikament |
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JP3739432B2 (ja) | 1994-02-25 | 2006-01-25 | ダイセル化学工業株式会社 | オゾン開裂反応 |
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PL366068A1 (en) | 2000-10-10 | 2005-01-24 | Smithkline Beecham Corporation | Substituted indoles, pharmaceutical compositions containing such indoles and their use as ppar-gamma binding agents |
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CA2810499A1 (en) | 2010-09-08 | 2012-03-15 | University Of Pittsburgh - Of The Commonwealth System Of Higher Educatio N | P53-mdm2 antagonists |
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WO2014047427A2 (en) | 2012-09-21 | 2014-03-27 | Vanderbilt University | Substituted benzofuran, benzothiophene and indole mcl-1 inhibitors |
US10005728B2 (en) * | 2013-08-28 | 2018-06-26 | Vanderbilt University | Substituted indole Mcl-1 inhibitors |
EP3122353B1 (en) | 2014-03-27 | 2020-10-28 | Vanderbilt University | Substituted indole mcl-1 inhibitors |
-
2017
- 2017-03-03 CN CN201780027686.5A patent/CN109153643B/zh active Active
- 2017-03-03 US US16/081,709 patent/US11596639B2/en active Active
- 2017-03-03 CA CA3016182A patent/CA3016182C/en active Active
- 2017-03-03 EA EA201891988A patent/EA038143B1/ru unknown
- 2017-03-03 WO PCT/US2017/020699 patent/WO2017152076A1/en active Application Filing
- 2017-03-03 EP EP17760914.6A patent/EP3423435B1/en active Active
- 2017-03-03 BR BR112018067775-2A patent/BR112018067775B1/pt active IP Right Grant
- 2017-03-03 EP EP23188050.1A patent/EP4292662A3/en active Pending
- 2017-03-03 AU AU2017228385A patent/AU2017228385B2/en active Active
- 2017-03-03 MX MX2018010678A patent/MX2018010678A/es unknown
- 2017-03-03 JP JP2018546464A patent/JP7086395B2/ja active Active
- 2017-03-03 KR KR1020187028435A patent/KR102396177B1/ko active IP Right Grant
-
2018
- 2018-08-19 IL IL261231A patent/IL261231B/en unknown
- 2018-09-03 CL CL2018002516A patent/CL2018002516A1/es unknown
- 2018-09-03 PH PH12018501877A patent/PH12018501877A1/en unknown
-
2022
- 2022-12-09 US US18/064,206 patent/US20230330099A1/en active Pending
Also Published As
Publication number | Publication date |
---|---|
KR102396177B1 (ko) | 2022-05-09 |
CL2018002516A1 (es) | 2019-02-01 |
IL261231A (en) | 2018-10-31 |
EA038143B1 (ru) | 2021-07-13 |
JP2019513697A (ja) | 2019-05-30 |
JP7086395B2 (ja) | 2022-06-20 |
EP3423435A4 (en) | 2019-08-14 |
EP4292662A2 (en) | 2023-12-20 |
CN109153643A (zh) | 2019-01-04 |
US11596639B2 (en) | 2023-03-07 |
CN109153643B (zh) | 2022-06-21 |
BR112018067775B1 (pt) | 2024-02-15 |
EP3423435A1 (en) | 2019-01-09 |
PH12018501877A1 (en) | 2019-02-04 |
EP3423435B1 (en) | 2023-08-23 |
CA3016182C (en) | 2024-02-27 |
WO2017152076A1 (en) | 2017-09-08 |
AU2017228385A1 (en) | 2018-09-06 |
KR20180118199A (ko) | 2018-10-30 |
BR112018067775A2 (pt) | 2019-04-09 |
EP4292662A3 (en) | 2024-02-21 |
IL261231B (en) | 2021-10-31 |
US20210283138A1 (en) | 2021-09-16 |
MX2018010678A (es) | 2019-01-17 |
AU2017228385B2 (en) | 2021-11-04 |
CA3016182A1 (en) | 2017-09-08 |
US20230330099A1 (en) | 2023-10-19 |
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