RU2021102253A - Деструкторы белка mdm2 - Google Patents
Деструкторы белка mdm2 Download PDFInfo
- Publication number
- RU2021102253A RU2021102253A RU2021102253A RU2021102253A RU2021102253A RU 2021102253 A RU2021102253 A RU 2021102253A RU 2021102253 A RU2021102253 A RU 2021102253A RU 2021102253 A RU2021102253 A RU 2021102253A RU 2021102253 A RU2021102253 A RU 2021102253A
- Authority
- RU
- Russia
- Prior art keywords
- solvate
- pharmaceutically acceptable
- acceptable salt
- group
- compound according
- Prior art date
Links
- 102000012199 E3 ubiquitin-protein ligase Mdm2 Human genes 0.000 title 1
- 108050002772 E3 ubiquitin-protein ligase Mdm2 Proteins 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims 104
- 239000012453 solvate Substances 0.000 claims 104
- 150000001875 compounds Chemical class 0.000 claims 76
- 229910052739 hydrogen Inorganic materials 0.000 claims 35
- 239000001257 hydrogen Substances 0.000 claims 35
- 206010028980 Neoplasm Diseases 0.000 claims 25
- 125000000217 alkyl group Chemical group 0.000 claims 21
- 201000011510 cancer Diseases 0.000 claims 20
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 18
- 229910052736 halogen Inorganic materials 0.000 claims 18
- 150000002367 halogens Chemical class 0.000 claims 18
- 150000002431 hydrogen Chemical class 0.000 claims 17
- 206010041067 Small cell lung cancer Diseases 0.000 claims 10
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 10
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 125000004438 haloalkoxy group Chemical group 0.000 claims 9
- 125000001188 haloalkyl group Chemical group 0.000 claims 9
- 229910052799 carbon Inorganic materials 0.000 claims 7
- 150000001721 carbon Chemical group 0.000 claims 7
- 125000005466 alkylenyl group Chemical group 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 6
- 206010000871 Acute monocytic leukaemia Diseases 0.000 claims 5
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 5
- 208000023275 Autoimmune disease Diseases 0.000 claims 5
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 5
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 5
- 206010006187 Breast cancer Diseases 0.000 claims 5
- 208000026310 Breast neoplasm Diseases 0.000 claims 5
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 5
- 206010008342 Cervix carcinoma Diseases 0.000 claims 5
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 5
- 206010009944 Colon cancer Diseases 0.000 claims 5
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 5
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 5
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 5
- 208000035489 Monocytic Acute Leukemia Diseases 0.000 claims 5
- 208000034578 Multiple myelomas Diseases 0.000 claims 5
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 5
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 5
- 206010029260 Neuroblastoma Diseases 0.000 claims 5
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 5
- 206010033128 Ovarian cancer Diseases 0.000 claims 5
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 5
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 5
- 206010060862 Prostate cancer Diseases 0.000 claims 5
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 5
- 206010040047 Sepsis Diseases 0.000 claims 5
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 5
- 208000036142 Viral infection Diseases 0.000 claims 5
- 201000010881 cervical cancer Diseases 0.000 claims 5
- 230000001684 chronic effect Effects 0.000 claims 5
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 5
- 208000035475 disorder Diseases 0.000 claims 5
- 201000004101 esophageal cancer Diseases 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 230000004968 inflammatory condition Effects 0.000 claims 5
- 208000032839 leukemia Diseases 0.000 claims 5
- 238000000034 method Methods 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 230000002062 proliferating effect Effects 0.000 claims 5
- 125000003107 substituted aryl group Chemical group 0.000 claims 5
- 230000009385 viral infection Effects 0.000 claims 5
- 201000009030 Carcinoma Diseases 0.000 claims 4
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 229910052731 fluorine Inorganic materials 0.000 claims 3
- 239000011737 fluorine Substances 0.000 claims 3
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 2
- 150000003857 carboxamides Chemical class 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- 201000004253 NUT midline carcinoma Diseases 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000004404 heteroalkyl group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
Classifications
-
- 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
-
- 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
- A61K31/407—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 other heterocyclic ring systems, e.g. ketorolac, physostigmine
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- 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
- C07D487/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Communicable Diseases (AREA)
- Immunology (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Virology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662318974P | 2016-04-06 | 2016-04-06 | |
| US62/318,974 | 2016-04-06 | ||
| US201662393874P | 2016-09-13 | 2016-09-13 | |
| US62/393,874 | 2016-09-13 | ||
| US201662409571P | 2016-10-18 | 2016-10-18 | |
| US62/409,571 | 2016-10-18 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2018138735A Division RU2743432C2 (ru) | 2016-04-06 | 2017-04-06 | Деструкторы белка mdm2 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2021102253A true RU2021102253A (ru) | 2021-03-03 |
Family
ID=58549316
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2018138735A RU2743432C2 (ru) | 2016-04-06 | 2017-04-06 | Деструкторы белка mdm2 |
| RU2021102253A RU2021102253A (ru) | 2016-04-06 | 2017-04-06 | Деструкторы белка mdm2 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2018138735A RU2743432C2 (ru) | 2016-04-06 | 2017-04-06 | Деструкторы белка mdm2 |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US11192898B2 (enExample) |
| EP (1) | EP3440066B1 (enExample) |
| JP (2) | JP7037500B2 (enExample) |
| KR (1) | KR102387316B1 (enExample) |
| CN (2) | CN109415336B (enExample) |
| AU (1) | AU2017246452C1 (enExample) |
| CA (1) | CA3020275A1 (enExample) |
| IL (1) | IL262103B (enExample) |
| MX (1) | MX2018012174A (enExample) |
| RU (2) | RU2743432C2 (enExample) |
| SG (1) | SG11201808728QA (enExample) |
| UA (1) | UA123786C2 (enExample) |
| WO (1) | WO2017176957A1 (enExample) |
| ZA (1) | ZA201806968B (enExample) |
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|---|---|---|---|---|
| SG11201808728QA (en) * | 2016-04-06 | 2018-11-29 | Univ Michigan Regents | Mdm2 protein degraders |
| CA3021358A1 (en) | 2016-04-22 | 2017-10-26 | Dana-Farber Cancer Institute, Inc. | Bifunctional molecules for degradation of egfr and methods of use |
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| WO2017197055A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| EP3454862B1 (en) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
| CN109641874A (zh) | 2016-05-10 | 2019-04-16 | C4医药公司 | 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体 |
| RS64976B1 (sr) | 2016-12-01 | 2024-01-31 | Arvinas Operations Inc | Derivati tetrahidronaftalena i tetrahidroizohinolina kao degradatori estrogenih receptora |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
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| KR102548191B1 (ko) | 2018-04-09 | 2023-06-28 | 상하이테크 유니버시티 | 표적 단백질 분해 화합물, 이의 항종양 응용, 이의 중간체 및 중간체의 응용 |
| EP3781156A4 (en) | 2018-04-16 | 2022-05-18 | C4 Therapeutics, Inc. | SPIROCYCLIC COMPOUNDS |
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| JP7629459B2 (ja) | 2019-11-19 | 2025-02-13 | ブリストル－マイヤーズ スクイブ カンパニー | Ｈｅｌｉｏｓタンパク質の阻害剤として有用な化合物 |
| KR20220145325A (ko) | 2019-12-17 | 2022-10-28 | 카이메라 쎄라퓨틱스 인코포레이티드 | Irak 분해제 및 이의 용도 |
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| IL262103A (en) | 2018-11-29 |
| AU2017246452C1 (en) | 2021-06-03 |
| NZ747251A (en) | 2024-05-31 |
| JP7037500B2 (ja) | 2022-03-16 |
| UA123786C2 (uk) | 2021-06-02 |
| US11192898B2 (en) | 2021-12-07 |
| KR20180132125A (ko) | 2018-12-11 |
| SG11201808728QA (en) | 2018-11-29 |
| AU2017246452B2 (en) | 2021-02-25 |
| JP2019510798A (ja) | 2019-04-18 |
| EP3440066B1 (en) | 2022-11-30 |
| AU2017246452A1 (en) | 2018-11-08 |
| MX2018012174A (es) | 2019-07-08 |
| BR112018070549A2 (pt) | 2019-02-12 |
| IL262103B (en) | 2021-05-31 |
| EP3440066A1 (en) | 2019-02-13 |
| WO2017176957A1 (en) | 2017-10-12 |
| US20220411432A1 (en) | 2022-12-29 |
| WO2017176957A8 (en) | 2018-11-08 |
| ZA201806968B (en) | 2020-02-26 |
| KR102387316B1 (ko) | 2022-04-15 |
| CN113788818A (zh) | 2021-12-14 |
| JP2022078201A (ja) | 2022-05-24 |
| RU2743432C2 (ru) | 2021-02-18 |
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