SG11201808729WA - Bet protein degraders - Google Patents
Bet protein degradersInfo
- Publication number
- SG11201808729WA SG11201808729WA SG11201808729WA SG11201808729WA SG11201808729WA SG 11201808729W A SG11201808729W A SG 11201808729WA SG 11201808729W A SG11201808729W A SG 11201808729WA SG 11201808729W A SG11201808729W A SG 11201808729WA SG 11201808729W A SG11201808729W A SG 11201808729WA
- Authority
- SG
- Singapore
- Prior art keywords
- international
- ann arbor
- pct
- english
- april
- 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
-
- 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
- A61P35/00—Antineoplastic agents
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
- C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
- Peptides Or Proteins (AREA)
Abstract
INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization 1111111101111011101010111110101111101110111111011101111101011111111101111011111 International Bureau ... .... ..Yjd (10) International Publication Number ..... ...,/ (43) International Publication Date WO 2017/180417 Al 19 October 2017(19.10.2017) WIPO I PCT (51) International Patent Classification: (74) Agent: NAPOLI, James, J.; Marshall, Gerstein & Borun C07D 487/04 (2006.01) A61P 35/00 (2006.01) LLP, 233 S. Wacker Drive, 6300 Willis Tower, Chicago, A61K 31/4745 (2006.01) IL 60606-6357 (US). (21) International Application Number: (81) Designated States (unless otherwise indicated, for every PCT/US2017/026278 kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, (22) International Filing Date: BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, 6 April 2017 (06.04.2017) DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (25) Filing Language: English HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, (26) Publication Language: English MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, (30) Priority Data: NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, 62/321,499 12 April 2016 (12.04.2016) US RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, 62/393,888 13 September 2016 (13.09.2016) US TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (71) Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN [US/US]; Office of Technology Transfer, (84) Designated States (unless otherwise indicated, for every 1600 Huron Parkway, 2nd Floor, Ann Arbor, MI 48109- kind of regional protection available): ARIPO (BW, GH, 2590 (US). GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, _ (72) Inventors: WANG, Shaomeng; 3336 Stirling Ct., Superi- TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, or Township, MI 49198 (US). ZHOU, Bing; 555 Zu DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, — _ Chong Zhi Road, Shanghai Institute Of Materia Medica, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, Room 3508, Shanghai 20123 (CN). XU, Fuming; 3111 In- SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, ternationa Dr., Apt. 2203A, Ypsilanti, MI 48197 (US). GW, KM, ML, MR, NE, SN, TD, TG). HU, Jiantao; 3005 Whisperwood Dr., Apartmetn 280, Ann Arbor, MI 48105 (US). BAI, Longchuan; 1530 Wood- Published: creek Blvd., Ann Arbor, MI 48104 (US). YANG, Chao- — with international search report (Art. 21(3)) - - . Yie; 4826 Hillway Court, Ann Arbor, MI 48105 (US). = = = = = = = = = Title: BET PROTEIN DEGRADERS — (54) = 0 R1 ,-1 . 4 1 4101 IN N- Q 1 11 0 0 0 0 N Q2 -1 ,.. x .L... y -B H I 1-1 IN 1-1 (57) : The present disclosure provides compounds represented by Formula I: and the pharmaceutically acceptable salts, hy - 0 drates, and solvates thereof, wherein B, R I , R 5 , Q I , Q\", L, X, Y, and Z are as defined as set forth in the specification. The present dis - \" closure also provids compounds of Formula I for use to treat a condition or disorder responsive to degradation of BET bromodo - 0 mains such as cancer.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662321499P | 2016-04-12 | 2016-04-12 | |
| US201662393888P | 2016-09-13 | 2016-09-13 | |
| PCT/US2017/026278 WO2017180417A1 (en) | 2016-04-12 | 2017-04-06 | Bet protein degraders |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201808729WA true SG11201808729WA (en) | 2018-11-29 |
Family
ID=58548921
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201808729WA SG11201808729WA (en) | 2016-04-12 | 2017-04-06 | Bet protein degraders |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US10633386B2 (en) |
| EP (1) | EP3442976B1 (en) |
| JP (1) | JP7072519B2 (en) |
| KR (1) | KR20180132861A (en) |
| CN (1) | CN109311890B (en) |
| AU (1) | AU2017250076B2 (en) |
| BR (1) | BR112018070859A2 (en) |
| CA (1) | CA3020541A1 (en) |
| IL (1) | IL262139B (en) |
| MX (1) | MX2018012379A (en) |
| RU (1) | RU2752677C2 (en) |
| SG (1) | SG11201808729WA (en) |
| UA (1) | UA123168C2 (en) |
| WO (1) | WO2017180417A1 (en) |
| ZA (1) | ZA201806969B (en) |
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| AU2017281903B2 (en) * | 2016-06-23 | 2020-12-24 | Dana-Farber Cancer Institute, Inc. | Degradation of bromodomain-containing protein 9 (BRD9) by conjugation of BRD9 inhibitors with E3 ligase ligand and methods of use |
| CN110769822A (en) | 2017-06-20 | 2020-02-07 | C4医药公司 | N/O-linked degron and degron bodies for protein degradation |
| CN109422751B (en) * | 2017-09-03 | 2022-04-22 | 上海美志医药科技有限公司 | Compound with activity of degrading tyrosine protein kinase JAK3 |
| CN111315735B (en) | 2017-09-04 | 2024-03-08 | C4医药公司 | Dihydrobenzimidazolone |
| EP3679026A1 (en) | 2017-09-04 | 2020-07-15 | C4 Therapeutics, Inc. | Glutarimide |
| WO2019043208A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | Dihydroquinolinones |
| WO2019094772A1 (en) * | 2017-11-10 | 2019-05-16 | The Regents Of The University Of Michigan | Ash1l degraders and methods of treatment therewith |
| WO2019099868A2 (en) | 2017-11-16 | 2019-05-23 | C4 Therapeutics, Inc. | Degraders and degrons for targeted protein degradation |
| JP2021519337A (en) | 2018-03-26 | 2021-08-10 | シー４ セラピューティクス， インコーポレイテッド | Cereblon binder for the degradation of Ikaras |
| CN112312904A (en) | 2018-04-16 | 2021-02-02 | C4医药公司 | Spiro compounds |
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| WO2020076996A1 (en) * | 2018-10-09 | 2020-04-16 | The Regents Of The University Of California | Covalent targeting of e3 ligases |
| CN113453679A (en) | 2018-12-20 | 2021-09-28 | C4医药公司 | Targeted protein degradation |
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| EP4039333A4 (en) * | 2019-09-30 | 2024-02-14 | Kyowa Kirin Co Ltd | Bet degrader |
| TW202146412A (en) | 2020-03-05 | 2021-12-16 | 美商Ｃ４醫藥公司 | Compounds for targeted degradation of brd9 |
| CN113387932B (en) * | 2020-03-14 | 2023-05-09 | 成都先导药物开发股份有限公司 | Bifunctional compound for inducing BRD4 protein degradation |
| CN112920176B (en) * | 2020-05-25 | 2022-11-04 | 四川大学华西医院 | Bifunctional compound capable of inducing PRC2 protein complex core subunit degradation, pharmaceutical composition and application |
| WO2022051616A1 (en) * | 2020-09-03 | 2022-03-10 | Board Of Regents Of The University Of Nebraska | Cdk targeted heterobifunctional small molecule proteolysis targeting chimeras |
| CN117580592A (en) | 2021-05-05 | 2024-02-20 | 渤健马萨诸塞州股份有限公司 | Compounds for targeting bruton's tyrosine kinase degradation |
| CN113336801B (en) * | 2021-06-08 | 2023-08-22 | 中国人民解放军空军军医大学 | Tetravalent platinum complexes containing BET inhibitors and use thereof |
| EP4366834A1 (en) | 2021-07-07 | 2024-05-15 | Biogen MA Inc. | Compounds for targeting degradation of irak4 proteins |
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-
2017
- 2017-04-06 MX MX2018012379A patent/MX2018012379A/en unknown
- 2017-04-06 JP JP2018553365A patent/JP7072519B2/en active Active
- 2017-04-06 US US16/093,160 patent/US10633386B2/en active Active
- 2017-04-06 CA CA3020541A patent/CA3020541A1/en active Pending
- 2017-04-06 SG SG11201808729WA patent/SG11201808729WA/en unknown
- 2017-04-06 WO PCT/US2017/026278 patent/WO2017180417A1/en active Application Filing
- 2017-04-06 UA UAA201811059A patent/UA123168C2/en unknown
- 2017-04-06 KR KR1020187032621A patent/KR20180132861A/en active IP Right Grant
- 2017-04-06 EP EP17717993.4A patent/EP3442976B1/en active Active
- 2017-04-06 AU AU2017250076A patent/AU2017250076B2/en not_active Ceased
- 2017-04-06 CN CN201780036434.9A patent/CN109311890B/en not_active Expired - Fee Related
- 2017-04-06 RU RU2018139537A patent/RU2752677C2/en active
- 2017-04-06 BR BR112018070859A patent/BR112018070859A2/en not_active IP Right Cessation
-
2018
- 2018-10-04 IL IL262139A patent/IL262139B/en active IP Right Grant
- 2018-10-18 ZA ZA2018/06969A patent/ZA201806969B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| RU2752677C2 (en) | 2021-07-29 |
| BR112018070859A2 (en) | 2019-02-05 |
| ZA201806969B (en) | 2019-12-18 |
| AU2017250076A1 (en) | 2018-11-08 |
| AU2017250076B2 (en) | 2021-07-22 |
| JP2019511528A (en) | 2019-04-25 |
| US10633386B2 (en) | 2020-04-28 |
| EP3442976A1 (en) | 2019-02-20 |
| MX2018012379A (en) | 2019-07-04 |
| US20190169195A1 (en) | 2019-06-06 |
| CN109311890A (en) | 2019-02-05 |
| CN109311890B (en) | 2021-08-31 |
| RU2018139537A3 (en) | 2020-08-11 |
| JP7072519B2 (en) | 2022-05-20 |
| WO2017180417A1 (en) | 2017-10-19 |
| CA3020541A1 (en) | 2017-10-19 |
| KR20180132861A (en) | 2018-12-12 |
| UA123168C2 (en) | 2021-02-24 |
| RU2018139537A (en) | 2020-05-14 |
| EP3442976B1 (en) | 2022-07-20 |
| IL262139B (en) | 2021-05-31 |
| IL262139A (en) | 2018-11-29 |
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