JP6857606B2 - ブロモドメインｂｒｄ９の阻害剤としての新規ピリジノンおよびイソキノリノン - Google Patents
ブロモドメインｂｒｄ９の阻害剤としての新規ピリジノンおよびイソキノリノン Download PDFInfo
- Publication number
- JP6857606B2 JP6857606B2 JP2017546629A JP2017546629A JP6857606B2 JP 6857606 B2 JP6857606 B2 JP 6857606B2 JP 2017546629 A JP2017546629 A JP 2017546629A JP 2017546629 A JP2017546629 A JP 2017546629A JP 6857606 B2 JP6857606 B2 JP 6857606B2
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- mmol
- methyl
- compound
- pyridin
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
- 0 *=C(C=**C1=O)C1=* Chemical compound *=C(C=**C1=O)C1=* 0.000 description 3
- IVBFYFAHHQFQKP-UHFFFAOYSA-N CC1=CC(c2cc(OC)c(CN(C3)CC3Cl)cc2)=CN(C)C1=O Chemical compound CC1=CC(c2cc(OC)c(CN(C3)CC3Cl)cc2)=CN(C)C1=O IVBFYFAHHQFQKP-UHFFFAOYSA-N 0.000 description 2
- YCYRWLPOFCNZPY-UHFFFAOYSA-N CN(C=C(c1ccccc11)Br)C1=O Chemical compound CN(C=C(c1ccccc11)Br)C1=O YCYRWLPOFCNZPY-UHFFFAOYSA-N 0.000 description 2
- JIABXBYOURNKRZ-UHFFFAOYSA-N O=S(c(cc1)ccc1Br)(N1CCNCC1)=O Chemical compound O=S(c(cc1)ccc1Br)(N1CCNCC1)=O JIABXBYOURNKRZ-UHFFFAOYSA-N 0.000 description 2
- ISQRPPLHUONLDQ-UHFFFAOYSA-N CC(C(c1ccc(CN)cc1)=CN1C)=C(C)C1=O Chemical compound CC(C(c1ccc(CN)cc1)=CN1C)=C(C)C1=O ISQRPPLHUONLDQ-UHFFFAOYSA-N 0.000 description 1
- XIEDZIAXYGMWOO-UHFFFAOYSA-N CC(C)(C)OC(N(CC1)CCN1C(c(c(OC)c1)ccc1C(C=C1I)=CN(C)C1=O)=O)=O Chemical compound CC(C)(C)OC(N(CC1)CCN1C(c(c(OC)c1)ccc1C(C=C1I)=CN(C)C1=O)=O)=O XIEDZIAXYGMWOO-UHFFFAOYSA-N 0.000 description 1
- CYFYGUQFVPHZEC-UHFFFAOYSA-N CC(C)(C)OC(N1CCN(Cc(cc2)c(C)cc2C(C=C2C)=CN(C)C2=O)CC1)=O Chemical compound CC(C)(C)OC(N1CCN(Cc(cc2)c(C)cc2C(C=C2C)=CN(C)C2=O)CC1)=O CYFYGUQFVPHZEC-UHFFFAOYSA-N 0.000 description 1
- HZRZWSRYHCOSGO-GJZGRUSLSA-N CC(C)(C)OC(N1[C@@H](C2)CN(Cc(c(OC)c3)ccc3Br)[C@@H]2C1)=O Chemical compound CC(C)(C)OC(N1[C@@H](C2)CN(Cc(c(OC)c3)ccc3Br)[C@@H]2C1)=O HZRZWSRYHCOSGO-GJZGRUSLSA-N 0.000 description 1
- ZMCYAMSUAVCZME-UHFFFAOYSA-N CC(C)(C)OC(NC1CN(Cc(c(OC)cc(C(c2c3cncn2)=CN(C)C3=O)c2)c2OC)C1)=O Chemical compound CC(C)(C)OC(NC1CN(Cc(c(OC)cc(C(c2c3cncn2)=CN(C)C3=O)c2)c2OC)C1)=O ZMCYAMSUAVCZME-UHFFFAOYSA-N 0.000 description 1
- MUUKNVJLQNKIRG-UHFFFAOYSA-N CC1(C)OB(C(C=C2)=C(C)N(C)C2=O)OC1(C)C Chemical compound CC1(C)OB(C(C=C2)=C(C)N(C)C2=O)OC1(C)C MUUKNVJLQNKIRG-UHFFFAOYSA-N 0.000 description 1
- MNGVVKQGTQXIRS-UHFFFAOYSA-N CC1=CC(c2cc(CN(C)C3)c3cc2)=CN(C)C1=O Chemical compound CC1=CC(c2cc(CN(C)C3)c3cc2)=CN(C)C1=O MNGVVKQGTQXIRS-UHFFFAOYSA-N 0.000 description 1
- CUFDWRAKYNAYPD-UHFFFAOYSA-N CC1=CC(c2cc(OC)c(CNC3CN(C)C3)c(OC)c2)=CN(C)C1=O Chemical compound CC1=CC(c2cc(OC)c(CNC3CN(C)C3)c(OC)c2)=CN(C)C1=O CUFDWRAKYNAYPD-UHFFFAOYSA-N 0.000 description 1
- MEGILMBSBHJLCU-UHFFFAOYSA-N CC1=CC(c2ccc(CO)cc2)=CN(C)C1=O Chemical compound CC1=CC(c2ccc(CO)cc2)=CN(C)C1=O MEGILMBSBHJLCU-UHFFFAOYSA-N 0.000 description 1
- VPLQRDBWOZNCIR-UHFFFAOYSA-N CCS(Cc(cc(cc1)C(C=C2C)=CN(C)C2=O)c1C(N1CCNCC1)=O)(=O)=O Chemical compound CCS(Cc(cc(cc1)C(C=C2C)=CN(C)C2=O)c1C(N1CCNCC1)=O)(=O)=O VPLQRDBWOZNCIR-UHFFFAOYSA-N 0.000 description 1
- FLNMQGISZVYIIK-UHFFFAOYSA-N CC[n]1nccc1 Chemical compound CC[n]1nccc1 FLNMQGISZVYIIK-UHFFFAOYSA-N 0.000 description 1
- OBGKOEHEKOTUHQ-UHFFFAOYSA-N CCc1c(C(N2CCNCC2)=O)c(OC)cc(C(C=C2C)=CN(C)C2=O)c1 Chemical compound CCc1c(C(N2CCNCC2)=O)c(OC)cc(C(C=C2C)=CN(C)C2=O)c1 OBGKOEHEKOTUHQ-UHFFFAOYSA-N 0.000 description 1
- FCWPHMAVXUGUKP-UHFFFAOYSA-N CCc1c(CN(C)C)c(OC)cc(C(C=C2C)=CN(C)C2=O)c1 Chemical compound CCc1c(CN(C)C)c(OC)cc(C(C=C2C)=CN(C)C2=O)c1 FCWPHMAVXUGUKP-UHFFFAOYSA-N 0.000 description 1
- CCASOLBFEDZOHP-UHFFFAOYSA-N CCc1cc(C(C=C2C)=CN(C)C2=O)cc(OC)c1N=C Chemical compound CCc1cc(C(C=C2C)=CN(C)C2=O)cc(OC)c1N=C CCASOLBFEDZOHP-UHFFFAOYSA-N 0.000 description 1
- MDPXZFFDWKOTNK-UHFFFAOYSA-N CN(C)Cc(ccc(C(c1c2cccc1)=CN(C)C2=O)c1)c1OC Chemical compound CN(C)Cc(ccc(C(c1c2cccc1)=CN(C)C2=O)c1)c1OC MDPXZFFDWKOTNK-UHFFFAOYSA-N 0.000 description 1
- RZGMDOOPSIUYEA-UHFFFAOYSA-N CN(C=C(c(cc1)ccc1C(N1CCNCC1)=O)c1c2cccc1)C2=O Chemical compound CN(C=C(c(cc1)ccc1C(N1CCNCC1)=O)c1c2cccc1)C2=O RZGMDOOPSIUYEA-UHFFFAOYSA-N 0.000 description 1
- PVAKOEDSIZWGQS-HOTGVXAUSA-N CN(C=C(c1c2[nH]cc1)c1cc(OC)c(CN3[C@@H](C4)CN[C@@H]4C3)cc1)C2=O Chemical compound CN(C=C(c1c2[nH]cc1)c1cc(OC)c(CN3[C@@H](C4)CN[C@@H]4C3)cc1)C2=O PVAKOEDSIZWGQS-HOTGVXAUSA-N 0.000 description 1
- HKBIABUNFSSVLK-UHFFFAOYSA-N Cc(c(NS(C)(=O)=O)c1)ccc1C(c1c2cccc1O)=CN(C)C2=O Chemical compound Cc(c(NS(C)(=O)=O)c1)ccc1C(c1c2cccc1O)=CN(C)C2=O HKBIABUNFSSVLK-UHFFFAOYSA-N 0.000 description 1
- DIPUVACKCJZMPW-UHFFFAOYSA-N Cc(ccc(C(C=C1C)=CN(C)C1=O)c1)c1NS(C)(=O)=O Chemical compound Cc(ccc(C(C=C1C)=CN(C)C1=O)c1)c1NS(C)(=O)=O DIPUVACKCJZMPW-UHFFFAOYSA-N 0.000 description 1
- VSJHFWDYFQTNCW-UHFFFAOYSA-N Cc(cccc12)c1C(Br)=CNC2=O Chemical compound Cc(cccc12)c1C(Br)=CNC2=O VSJHFWDYFQTNCW-UHFFFAOYSA-N 0.000 description 1
- RWXZXCZBMQPOBF-UHFFFAOYSA-N Cc1ccc2nc[nH]c2c1 Chemical compound Cc1ccc2nc[nH]c2c1 RWXZXCZBMQPOBF-UHFFFAOYSA-N 0.000 description 1
- JCBIPKKIGJQGCM-UHFFFAOYSA-N O=C(c1cccc(F)c11)NC=C1Br Chemical compound O=C(c1cccc(F)c11)NC=C1Br JCBIPKKIGJQGCM-UHFFFAOYSA-N 0.000 description 1
- WXRLCVUDLFFTFF-UHFFFAOYSA-N [O-][N+](c1cc(Br)cnc1O)=O Chemical compound [O-][N+](c1cc(Br)cnc1O)=O WXRLCVUDLFFTFF-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/62—Oxygen or sulfur atoms
- C07D213/63—One oxygen atom
- C07D213/64—One oxygen atom attached in position 2 or 6
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
- C07D217/24—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
- C07D237/28—Cinnolines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
- C07D237/30—Phthalazines
- C07D237/32—Phthalazines with oxygen atoms directly attached to carbon atoms of the nitrogen-containing ring
-
- 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
- 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
- C07D401/06—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 linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D401/10—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 linked by a carbon chain containing aromatic rings
-
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- C07D471/08—Bridged systems
-
- 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
- C07D487/08—Bridged 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
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15157879 | 2015-03-05 | ||
| EP15157879.6 | 2015-03-05 | ||
| EP15199403 | 2015-12-10 | ||
| EP15199403.5 | 2015-12-10 | ||
| PCT/EP2016/054713 WO2016139361A1 (en) | 2015-03-05 | 2016-03-04 | New pyridinones and isoquinolinones as inhibitors of the bromodomain brd9 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018507238A JP2018507238A (ja) | 2018-03-15 |
| JP2018507238A5 JP2018507238A5 (enExample) | 2020-08-06 |
| JP6857606B2 true JP6857606B2 (ja) | 2021-04-14 |
Family
ID=55521687
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017546629A Active JP6857606B2 (ja) | 2015-03-05 | 2016-03-04 | ブロモドメインｂｒｄ９の阻害剤としての新規ピリジノンおよびイソキノリノン |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US11319318B2 (enExample) |
| EP (1) | EP3265453B1 (enExample) |
| JP (1) | JP6857606B2 (enExample) |
| WO (1) | WO2016139361A1 (enExample) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2988752A4 (en) | 2013-04-24 | 2017-01-18 | Salk Institute for Biological Studies | Vitamin d receptor/smad genomic circuit gates fibrotic response |
| AR104259A1 (es) | 2015-04-15 | 2017-07-05 | Celgene Quanticel Res Inc | Inhibidores de bromodominio |
| WO2019023149A1 (en) | 2017-07-24 | 2019-01-31 | Salk Institute For Biological Studies | USE OF BROMODOMAIN-CONTAINING PROTEIN-9 ANTAGONISTS IN ASSOCIATION WITH VITAMIN D RECEPTOR AGONISTS IN THE TREATMENT OF DIABETES |
| US11466034B2 (en) * | 2017-12-20 | 2022-10-11 | Betta Pharmaceuticals Co., Ltd. | Compound functioning as bromodomain protein inhibitor, and composition |
| JP2021512167A (ja) | 2018-01-30 | 2021-05-13 | フォグホーン セラピューティクス インコーポレイテッドＦｏｇｈｏｒｎ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｉｎｃ． | 障害を治療するための方法及び化合物 |
| CN111936498B (zh) | 2018-03-26 | 2024-04-16 | 诺华股份有限公司 | N-(3-(7H-吡咯并[2,3-d]嘧啶-4-基)苯基)苯甲酰胺衍生物 |
| US10442799B1 (en) | 2018-04-07 | 2019-10-15 | Fuqiang Ruan | Heterocyclic compounds and uses thereof |
| CN110776508B (zh) * | 2018-07-27 | 2021-07-16 | 海创药业股份有限公司 | 一种brd4抑制剂及其制备方法和用途 |
| WO2020160193A2 (en) * | 2019-01-29 | 2020-08-06 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| AU2020214802A1 (en) * | 2019-01-29 | 2021-08-12 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| US12384776B2 (en) | 2019-01-29 | 2025-08-12 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| WO2020160198A1 (en) * | 2019-01-29 | 2020-08-06 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| GB201905721D0 (en) * | 2019-04-24 | 2019-06-05 | Univ Dundee | Compounds |
| CN110003204B (zh) * | 2019-04-30 | 2020-08-11 | 上海勋和医药科技有限公司 | 一种bet蛋白抑制剂、其制备方法及用途 |
| WO2020242245A1 (ko) * | 2019-05-29 | 2020-12-03 | 에스티팜 주식회사 | 프탈라진온 화합물 및 이들의 용도 |
| US20220289711A1 (en) * | 2019-07-31 | 2022-09-15 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| UY38880A (es) * | 2019-09-16 | 2021-04-30 | Novartis Ag | Degradadores bifuncionales de brd9 y sus métodos de uso |
| KR20220133259A (ko) * | 2020-01-29 | 2022-10-04 | 포그혼 쎄라퓨틱스 인크. | 화합물 및 이의 용도 |
| CA3165309A1 (en) | 2020-03-05 | 2021-09-10 | Christopher G. Nasveschuk | Compounds for targeted degradation of brd9 |
| JP2023536139A (ja) * | 2020-07-29 | 2023-08-23 | フォグホーン セラピューティクス インコーポレイテッド | 化合物及びその使用 |
| US11787800B2 (en) | 2020-07-29 | 2023-10-17 | Foghorn Therapeutics Inc. | BRD9 degraders and uses thereof |
| US20240150755A1 (en) * | 2021-02-26 | 2024-05-09 | Salk Institute For Biological Studies | Modulating regulatory t cell function in autoimmune disease and cancer |
| WO2023283263A1 (en) | 2021-07-06 | 2023-01-12 | Foghorn Therapeutics Inc. | Citrate salt, pharmaceutical compositions, and methods of making and using the same |
| WO2023010354A1 (zh) * | 2021-08-04 | 2023-02-09 | 四川大学华西医院 | 一种具有egfr抑制活性的小分子化合物及其制备方法与应用 |
| EP4540226A1 (en) | 2022-06-16 | 2025-04-23 | Amphista Therapeutics Ltd | Bifunctional molecules for targeted protein degradation |
| WO2024057021A1 (en) | 2022-09-13 | 2024-03-21 | Amphista Therapeutics Limited | Compounds for targeted protein degradation |
| WO2024163641A2 (en) * | 2023-02-01 | 2024-08-08 | Foghorn Therapeutics Inc. | Formulations for treating cancer |
| WO2024238871A1 (en) * | 2023-05-18 | 2024-11-21 | Rectify Pharmaceuticals, Inc. | Aryl sulfonamide compounds and their use in treating medical conditions |
| CN117229202B (zh) * | 2023-11-15 | 2024-01-26 | 苏州美诺医药科技有限公司 | 一种brd9靶向降解化合物的中间体的制备方法 |
| GB202319256D0 (en) | 2023-12-15 | 2024-01-31 | Amphista Therapeutics Ltd | Novel compounds for targeted protein degradation |
| WO2025191109A1 (en) | 2024-03-13 | 2025-09-18 | Amphista Therapeutics Limited | Combinations comprising brd9 bifunctional compounds and their use in the treatment of cancer |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5716954A (en) * | 1991-10-09 | 1998-02-10 | Syntex U.S.A. Inc. | Benzopyridazinone and pyridopyridazinone compounds |
| IL103388A (en) * | 1991-10-09 | 1997-09-30 | Syntex Inc | PYRIDO £2,3-d| PYRIDAZINONES AND PYRIDAZINETHIONES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM |
| US5466697A (en) * | 1994-07-13 | 1995-11-14 | Syntex (U.S.A.) Inc. | 8-phenyl-1,6-naphthyridin-5-ones |
| ES2232306B1 (es) * | 2003-11-10 | 2006-08-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de piridazin-3(2h)-ona. |
| AR063706A1 (es) * | 2006-09-11 | 2009-02-11 | Cgi Pharmaceuticals Inc | Determinadas amidas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden. |
| CL2008002793A1 (es) * | 2007-09-20 | 2009-09-04 | Cgi Pharmaceuticals Inc | Compuestos derivados de amidas sustituidas, inhibidores de la actividad de btk; composicion farmaceutica que los comprende; utiles en el tratamiento del cancer, trastornos oseos, enfermedades autoinmunes, entre otras |
| EP2196465A1 (en) | 2008-12-15 | 2010-06-16 | Almirall, S.A. | (3-oxo)pyridazin-4-ylurea derivatives as PDE4 inhibitors |
| WO2013142390A1 (en) * | 2012-03-21 | 2013-09-26 | Gtx, Inc. | Aldo-keto reductase subfamily 1c3 (akr1c3) inhibitors |
| US9212182B2 (en) * | 2013-06-12 | 2015-12-15 | Amgen Inc. | Bicyclic sulfonamide compounds as sodium channel inhibitors |
| WO2015004534A2 (en) * | 2013-06-21 | 2015-01-15 | Zenith Epigenetics Corp. | Novel substituted bicyclic compounds as bromodomain inhibitors |
| CN103396774B (zh) | 2013-08-09 | 2017-09-19 | 西南石油大学 | 堵漏剂及其制备方法 |
| EA035727B1 (ru) * | 2013-10-18 | 2020-07-31 | Селджен Квонтисел Рисёрч, Инк. | Ингибиторы бромодомена |
| US9399640B2 (en) | 2013-11-26 | 2016-07-26 | Incyte Corporation | Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors |
| WO2015081246A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| MA40943A (fr) * | 2014-11-10 | 2017-09-19 | Constellation Pharmaceuticals Inc | Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines |
| MA40940A (fr) * | 2014-11-10 | 2017-09-19 | Constellation Pharmaceuticals Inc | Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines |
-
2016
- 2016-03-04 EP EP16708994.5A patent/EP3265453B1/en active Active
- 2016-03-04 US US15/554,440 patent/US11319318B2/en active Active
- 2016-03-04 WO PCT/EP2016/054713 patent/WO2016139361A1/en not_active Ceased
- 2016-03-04 JP JP2017546629A patent/JP6857606B2/ja active Active
Also Published As
| Publication number | Publication date |
|---|---|
| JP2018507238A (ja) | 2018-03-15 |
| EP3265453B1 (en) | 2022-06-29 |
| US20180044335A1 (en) | 2018-02-15 |
| WO2016139361A1 (en) | 2016-09-09 |
| US11319318B2 (en) | 2022-05-03 |
| EP3265453A1 (en) | 2018-01-10 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP6857606B2 (ja) | ブロモドメインｂｒｄ９の阻害剤としての新規ピリジノンおよびイソキノリノン | |
| US9296748B2 (en) | Pyridinones | |
| CN104870448B (zh) | 三唑并吡嗪 | |
| US9199988B2 (en) | Dihydroquinazolinone analogues | |
| TWI586649B (zh) | ６－乙炔基吡啶及其用途 | |
| US8575203B2 (en) | Chemical compounds | |
| JP6424224B2 (ja) | 新規ビスアミドピリジン | |
| JP6338665B2 (ja) | 新規６−アルキニルピリジン | |
| EP2978757A1 (en) | Indolinone analogues as brd4 inhibitors | |
| JP6250226B2 (ja) | Ｓｍａｃ模倣薬としての６−アルキニル−ピリジン誘導体 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20190304 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20190304 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20191216 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20191212 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20200313 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20200616 |
|
| A524 | Written submission of copy of amendment under article 19 pct |
Free format text: JAPANESE INTERMEDIATE CODE: A524 Effective date: 20200616 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20200928 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20201228 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20210118 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20210218 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20210322 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 6857606 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |