JP6669744B2 - ブロモドメインのインヒビターとしての置換ピロロピリジン - Google Patents
ブロモドメインのインヒビターとしての置換ピロロピリジン Download PDFInfo
- Publication number
- JP6669744B2 JP6669744B2 JP2017525075A JP2017525075A JP6669744B2 JP 6669744 B2 JP6669744 B2 JP 6669744B2 JP 2017525075 A JP2017525075 A JP 2017525075A JP 2017525075 A JP2017525075 A JP 2017525075A JP 6669744 B2 JP6669744 B2 JP 6669744B2
- Authority
- JP
- Japan
- Prior art keywords
- pyrrolo
- pyridin
- oxo
- enyl
- alkyl
- 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.)
- Expired - Fee Related
Links
- 0 *[n](cc1)c2c1C(c1cc(C(N3CCOCC3)O)c3[n+]c[n](*)c3c1)=CN(CCC=C)C2=* Chemical compound *[n](cc1)c2c1C(c1cc(C(N3CCOCC3)O)c3[n+]c[n](*)c3c1)=CN(CCC=C)C2=* 0.000 description 3
- PPFUIVDWRYGXAS-SNAWJCMRSA-N C/C=C/CN(C=C(c1c2[nH]c(C)c1)c1cc(C(NCc3cncnc3)=O)ccc1OC)C2=O Chemical compound C/C=C/CN(C=C(c1c2[nH]c(C)c1)c1cc(C(NCc3cncnc3)=O)ccc1OC)C2=O PPFUIVDWRYGXAS-SNAWJCMRSA-N 0.000 description 1
- ZGGQBUJHVGCBAB-ONEGZZNKSA-N C/C=C/CN(C=C(c1c2[nH]c(C)c1)c1ccc(C(N3CCNCC3)=O)c(Cl)c1)C2=O Chemical compound C/C=C/CN(C=C(c1c2[nH]c(C)c1)c1ccc(C(N3CCNCC3)=O)c(Cl)c1)C2=O ZGGQBUJHVGCBAB-ONEGZZNKSA-N 0.000 description 1
- MITBTHHFLRBDQI-UHFFFAOYSA-N CCCCN(C=C(c1c2[nH]c(C)c1)c(cc(c(C(N1CCOCC1)=O)c1)OC)c1OC)C2=O Chemical compound CCCCN(C=C(c1c2[nH]c(C)c1)c(cc(c(C(N1CCOCC1)=O)c1)OC)c1OC)C2=O MITBTHHFLRBDQI-UHFFFAOYSA-N 0.000 description 1
- MROWCPGGIGFQIJ-UHFFFAOYSA-N COC(N=C1)=C2NC=CC2C1Br Chemical compound COC(N=C1)=C2NC=CC2C1Br MROWCPGGIGFQIJ-UHFFFAOYSA-N 0.000 description 1
- ACUFFKOLHJOZSS-UHFFFAOYSA-N COC(c1cc(B(O)O)c2nc[nH]c2c1)=O Chemical compound COC(c1cc(B(O)O)c2nc[nH]c2c1)=O ACUFFKOLHJOZSS-UHFFFAOYSA-N 0.000 description 1
- LMTOCDATIYGDHE-UHFFFAOYSA-N O=C(c1cc(Br)cc2c1nc[nH]2)N1CCOCC1 Chemical compound O=C(c1cc(Br)cc2c1nc[nH]2)N1CCOCC1 LMTOCDATIYGDHE-UHFFFAOYSA-N 0.000 description 1
Classifications
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- 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
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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
-
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P5/00—Drugs for disorders of the endocrine system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
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- A—HUMAN NECESSITIES
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- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Emergency Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Transplantation (AREA)
- Oncology (AREA)
- Vascular Medicine (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462077703P | 2014-11-10 | 2014-11-10 | |
| US62/077,703 | 2014-11-10 | ||
| PCT/US2015/060003 WO2016077378A1 (en) | 2014-11-10 | 2015-11-10 | Substituted pyrrolopyrdines as inhibitors of bromodomain |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017533248A JP2017533248A (ja) | 2017-11-09 |
| JP2017533248A5 JP2017533248A5 (enExample) | 2018-12-20 |
| JP6669744B2 true JP6669744B2 (ja) | 2020-03-18 |
Family
ID=54608969
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017525075A Expired - Fee Related JP6669744B2 (ja) | 2014-11-10 | 2015-11-10 | ブロモドメインのインヒビターとしての置換ピロロピリジン |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US10183009B2 (enExample) |
| EP (1) | EP3218375B1 (enExample) |
| JP (1) | JP6669744B2 (enExample) |
| CN (3) | CN115583947A (enExample) |
| MA (1) | MA40943A (enExample) |
| WO (1) | WO2016077378A1 (enExample) |
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX366703B (es) | 2013-03-15 | 2019-07-22 | Incyte Holdings Corp | Heterociclos tricíclicos como inhibidores de la proteína bet. |
| EP2988752A4 (en) | 2013-04-24 | 2017-01-18 | Salk Institute for Biological Studies | Vitamin d receptor/smad genomic circuit gates fibrotic response |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| SI3674302T1 (sl) | 2014-04-23 | 2023-07-31 | Incyte Holdings Corporation | 1h-pirolo(2,3-c)piridin-7(6h)-oni in pirazolo(3,4-c)piridin-7(6h)-oni kot zaviralci proteinov bet |
| ES2855225T3 (es) | 2014-09-15 | 2021-09-23 | Incyte Corp | Heterociclos tricíclicos para su uso como inhibidores de proteínas BET |
| JP6639497B2 (ja) * | 2014-11-10 | 2020-02-05 | ジェネンテック, インコーポレイテッド | ブロモドメインインヒビターおよびその使用 |
| MA40940A (fr) * | 2014-11-10 | 2017-09-19 | Constellation Pharmaceuticals Inc | Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines |
| CN107531692B (zh) | 2015-01-29 | 2020-12-25 | 基因泰克公司 | 治疗化合物及其用途 |
| EP3265453B1 (en) * | 2015-03-05 | 2022-06-29 | Boehringer Ingelheim International GmbH | New pyridinones and isoquinolinones as inhibitors of the bromodomain brd9 |
| AR104259A1 (es) | 2015-04-15 | 2017-07-05 | Celgene Quanticel Res Inc | Inhibidores de bromodominio |
| US20170121347A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
| CR20190027A (es) | 2016-06-20 | 2019-05-16 | Incyte Corp | Formas sólidas cristalinas de un inhibidor de bet |
| WO2018130174A1 (zh) * | 2017-01-11 | 2018-07-19 | 江苏豪森药业集团有限公司 | 吡咯并[2,3-c]吡啶类衍生物、其制备方法及其在医药上的应用 |
| AU2018209164B2 (en) | 2017-01-17 | 2021-11-04 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| WO2018137655A1 (zh) * | 2017-01-25 | 2018-08-02 | 江苏豪森药业集团有限公司 | 吡咯并吡啶类n-氧化衍生物及其制备方法和应用 |
| EP3609896A4 (en) * | 2017-04-14 | 2020-11-04 | AbbVie Inc. | BROMODOMAIN INHIBITORS |
| 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 |
| CN109970733B (zh) * | 2017-12-28 | 2020-05-08 | 新发药业有限公司 | 一种维罗非尼及其类似物的简便制备方法 |
| US10442799B1 (en) | 2018-04-07 | 2019-10-15 | Fuqiang Ruan | Heterocyclic compounds and uses thereof |
| CN110577526B (zh) * | 2018-06-07 | 2023-10-27 | 上海翰森生物医药科技有限公司 | 溴域结构蛋白抑制剂的盐及其制备方法和应用 |
| CN110372693B (zh) * | 2018-07-04 | 2022-05-03 | 清华大学 | 一种靶向降解bet蛋白的化合物及其应用 |
| 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 |
| CN110818609A (zh) * | 2018-08-11 | 2020-02-21 | 中国药科大学 | 3-乙酰基吲哚类brpf1抑制剂的制备方法及其用途 |
| US20220079951A1 (en) * | 2018-12-20 | 2022-03-17 | Saint Louis University | Bet inhibitors for modulating dux4 expression in fshd |
| AU2020214802A1 (en) | 2019-01-29 | 2021-08-12 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| GB201905721D0 (en) | 2019-04-24 | 2019-06-05 | Univ Dundee | Compounds |
| 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 |
| WO2021233371A1 (zh) * | 2020-05-21 | 2021-11-25 | 贝达药业股份有限公司 | 作为溴结构域蛋白质抑制剂的化合物和组合物 |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| US11787800B2 (en) | 2020-07-29 | 2023-10-17 | Foghorn Therapeutics Inc. | BRD9 degraders and uses thereof |
| 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 |
| WO2023283263A1 (en) | 2021-07-06 | 2023-01-12 | Foghorn Therapeutics Inc. | Citrate salt, pharmaceutical compositions, and methods of making and using the same |
| 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 |
| WO2024193527A1 (zh) * | 2023-03-20 | 2024-09-26 | 山东新时代药业有限公司 | 作为溴结构域抑制剂的吡咯并[2,3-c]吡啶类化合物 |
| WO2025117674A1 (en) * | 2023-11-28 | 2025-06-05 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Compounds for targeted degradation of taf1 |
| 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 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CU22545A1 (es) | 1994-11-18 | 1999-03-31 | Centro Inmunologia Molecular | Obtención de un anticuerpo quimérico y humanizado contra el receptor del factor de crecimiento epidérmico para uso diagnóstico y terapéutico |
| US4943533A (en) | 1984-03-01 | 1990-07-24 | The Regents Of The University Of California | Hybrid cell lines that produce monoclonal antibodies to epidermal growth factor receptor |
| DE69025946T2 (de) | 1989-09-08 | 1996-10-17 | Univ Duke | Modifikationen der struktur des egf-rezeptor-gens in menschlichen glioma |
| AU661533B2 (en) | 1992-01-20 | 1995-07-27 | Astrazeneca Ab | Quinazoline derivatives |
| GB9314893D0 (en) | 1993-07-19 | 1993-09-01 | Zeneca Ltd | Quinazoline derivatives |
| ATE207366T1 (de) | 1993-12-24 | 2001-11-15 | Merck Patent Gmbh | Immunokonjugate |
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2015
- 2015-11-09 MA MA040943A patent/MA40943A/fr unknown
- 2015-11-10 WO PCT/US2015/060003 patent/WO2016077378A1/en not_active Ceased
- 2015-11-10 CN CN202211065963.0A patent/CN115583947A/zh active Pending
- 2015-11-10 JP JP2017525075A patent/JP6669744B2/ja not_active Expired - Fee Related
- 2015-11-10 EP EP15797766.1A patent/EP3218375B1/en active Active
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| Publication number | Publication date |
|---|---|
| CN107207493B (zh) | 2023-01-20 |
| US20170340605A1 (en) | 2017-11-30 |
| CN116003409A (zh) | 2023-04-25 |
| JP2017533248A (ja) | 2017-11-09 |
| EP3218375A1 (en) | 2017-09-20 |
| CN107207493A (zh) | 2017-09-26 |
| MA40943A (fr) | 2017-09-19 |
| WO2016077378A1 (en) | 2016-05-19 |
| US10183009B2 (en) | 2019-01-22 |
| CN115583947A (zh) | 2023-01-10 |
| EP3218375B1 (en) | 2022-04-27 |
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