JOP20180120A1 - مشتقات بيريدين مستبدلة كمثبطات انتقائية لـ dnmt1 - Google Patents
مشتقات بيريدين مستبدلة كمثبطات انتقائية لـ dnmt1Info
- Publication number
- JOP20180120A1 JOP20180120A1 JOP/2018/0120A JOP20180120A JOP20180120A1 JO P20180120 A1 JOP20180120 A1 JO P20180120A1 JO P20180120 A JOP20180120 A JO P20180120A JO P20180120 A1 JOP20180120 A1 JO P20180120A1
- Authority
- JO
- Jordan
- Prior art keywords
- dnmt1
- compound
- directed
- iar
- treatment
- Prior art date
Links
- 150000003222 pyridines Chemical class 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 5
- 108010009540 DNA (Cytosine-5-)-Methyltransferase 1 Proteins 0.000 abstract 3
- 102100036279 DNA (cytosine-5)-methyltransferase 1 Human genes 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 208000035475 disorder Diseases 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 208000007056 sickle cell anemia Diseases 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 229940124639 Selective inhibitor Drugs 0.000 abstract 1
- 208000018020 Sickle cell-beta-thalassemia disease syndrome Diseases 0.000 abstract 1
- 206010043391 Thalassaemia beta Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 208000034737 hemoglobinopathy Diseases 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 208000011580 syndromic disease Diseases 0.000 abstract 1
Classifications
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic 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
- A61K31/435—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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
-
- 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
-
- 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
- C07D213/72—Nitrogen atoms
- C07D213/73—Unsubstituted amino or imino radicals
-
- 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
- C07D213/72—Nitrogen atoms
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
-
- 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
- C07D401/12—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
- 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- C07D417/02—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 two hetero rings
- C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662349227P | 2016-06-13 | 2016-06-13 | |
| US201662393256P | 2016-09-12 | 2016-09-12 | |
| US201662412343P | 2016-10-25 | 2016-10-25 | |
| PCT/IB2017/053511 WO2017216727A1 (en) | 2016-06-13 | 2017-06-13 | Substituted pyridines as inhibitors of dnmt1 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JOP20180120A1 true JOP20180120A1 (ar) | 2019-01-30 |
Family
ID=59239935
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JOP/2018/0120A JOP20180120A1 (ar) | 2016-06-13 | 2018-12-10 | مشتقات بيريدين مستبدلة كمثبطات انتقائية لـ dnmt1 |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US10975056B2 (enExample) |
| EP (1) | EP3468953B1 (enExample) |
| JP (1) | JP7051829B2 (enExample) |
| KR (1) | KR20190017030A (enExample) |
| CN (1) | CN109563043B (enExample) |
| AU (1) | AU2017283790B2 (enExample) |
| CA (2) | CA3026211A1 (enExample) |
| CL (1) | CL2018003577A1 (enExample) |
| CO (1) | CO2018013717A2 (enExample) |
| CR (1) | CR20180580A (enExample) |
| DO (1) | DOP2018000273A (enExample) |
| ES (1) | ES2993451T3 (enExample) |
| IL (1) | IL263163B (enExample) |
| JO (1) | JOP20180120A1 (enExample) |
| MA (1) | MA45244A (enExample) |
| MX (1) | MX391600B (enExample) |
| PE (1) | PE20190971A1 (enExample) |
| PH (1) | PH12018502633B1 (enExample) |
| SG (1) | SG11201809559UA (enExample) |
| WO (2) | WO2017216727A1 (enExample) |
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| US11453697B1 (en) | 2015-08-13 | 2022-09-27 | Merck Sharp & Dohme Llc | Cyclic di-nucleotide compounds as sting agonists |
| MA42608A (fr) | 2015-08-13 | 2018-06-20 | Merck Sharp & Dohme | Composés de di-nucléotide cyclique en tant qu'agonistes sting (stimulateur de gène interféron) |
| ES2921432T3 (es) | 2016-06-13 | 2022-08-25 | Gilead Sciences Inc | Derivados de azetidina como moduladores de FXR (NR1H4) |
| CA2968836C (en) | 2016-06-13 | 2025-09-02 | Gilead Sciences, Inc. | FXR MODULATING COMPOUNDS (NR1H4) |
| RS62410B1 (sr) | 2016-10-04 | 2021-10-29 | Merck Sharp & Dohme | Benzo[b]tiofenska jedinjenja kao agonisti sting |
| EP4424364B1 (en) | 2017-03-28 | 2026-01-21 | Gilead Sciences, Inc. | Combinations for use in the treatment of cirrhosis and liver fibrosis |
| US11466047B2 (en) | 2017-05-12 | 2022-10-11 | Merck Sharp & Dohme Llc | Cyclic di-nucleotide compounds as sting agonists |
| WO2019027857A1 (en) | 2017-08-04 | 2019-02-07 | Merck Sharp & Dohme Corp. | COMBINATIONS OF PD-1 ANTAGONISTS AND STING BENZO [B] THIOPHENIC AGONISTS FOR THE TREATMENT OF CANCER |
| JP2020530838A (ja) | 2017-08-04 | 2020-10-29 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | がん治療のためのベンゾ［ｂ］チオフェンＳＴＩＮＧアゴニスト |
| CN109651358B (zh) * | 2017-10-11 | 2023-04-07 | 上海迪诺医药科技有限公司 | 4-氨基吡啶衍生物、其药物组合物、制备方法及应用 |
| WO2019125974A1 (en) | 2017-12-20 | 2019-06-27 | Merck Sharp & Dohme Corp. | Cyclic di-nucleotide compounds as sting agonists |
| WO2019195124A1 (en) | 2018-04-03 | 2019-10-10 | Merck Sharp & Dohme Corp. | Benzothiophenes and related compounds as sting agonists |
| WO2019195063A1 (en) | 2018-04-03 | 2019-10-10 | Merck Sharp & Dohme Corp. | Aza-benzothiophene compounds as sting agonists |
| PE20211907A1 (es) | 2019-01-15 | 2021-09-28 | Gilead Sciences Inc | Compuestos moduladores de fxr (nr1h4) |
| KR102725082B1 (ko) | 2019-02-19 | 2024-11-04 | 길리애드 사이언시즈, 인코포레이티드 | Fxr 효능제의 고체 형태 |
| CN111662283B (zh) * | 2019-03-07 | 2021-11-16 | 湖南化工研究院有限公司 | 咪唑并吡啶类化合物及其中间体、制备方法与应用 |
| WO2022076563A1 (en) * | 2020-10-07 | 2022-04-14 | University Of Florida Research Foundation, Incorporated | Macrocyclic compounds and methods of treatment |
| CN116917273A (zh) * | 2021-03-02 | 2023-10-20 | 葛兰素史克知识产权发展有限公司 | 作为dnmt1抑制剂的经取代的吡啶 |
| CN113502265B (zh) * | 2021-05-25 | 2024-05-28 | 昭泰英基生物医药（香港）有限公司 | 将t细胞重编程为类nk细胞的诱导剂及其应用 |
| CN113278021B (zh) * | 2021-05-29 | 2022-09-23 | 天津全和诚科技有限责任公司 | 1,7-二氮杂螺[3.5]壬烷-7-甲酸叔丁酯及其草酸盐的制备方法 |
| JP2024539267A (ja) | 2021-10-19 | 2024-10-28 | アキラバイオ， インコーポレイテッド | ２’－デオキシシチジンアナログを含む組成物、ならびに鎌状赤血球症、サラセミアおよびがんを処置するためのその使用 |
| CN114230459A (zh) * | 2021-12-10 | 2022-03-25 | 武汉九州钰民医药科技有限公司 | 一种化合物的制备方法及分析检测方法 |
| WO2023192629A1 (en) * | 2022-04-01 | 2023-10-05 | Herophilus, Inc. | Induction of mecp2 expression by dna methyl transferase inhibitors |
| WO2024156288A1 (en) * | 2023-01-29 | 2024-08-02 | Shanghai Kygent Pharmaceutical Co., Ltd | Dnmt1 inhibitors, pharmaceutical compositions, and therapeutic applications |
| CN121368481A (zh) * | 2023-06-29 | 2026-01-20 | 丹娜-法伯癌症研究院 | 用于降解dna甲基转移酶1 (dnmt1)的蛋白水解靶向嵌合体(protacs)的合成和体外表征 |
| WO2025085756A1 (en) * | 2023-10-18 | 2025-04-24 | University Of Florida Research Foundation, Incorporated | Macrocyclic compounds and methods of treatment |
| WO2025190285A1 (en) * | 2024-03-12 | 2025-09-18 | Shanghai Kygent Pharmaceutical Co., Ltd | Pyridine compounds, pharmaceutical compositions, and applications |
| CN119306700A (zh) * | 2024-08-28 | 2025-01-14 | 山东大学 | Dnmt1-hdac双靶点抑制剂及其制备方法和应用 |
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|---|---|
| PE20190971A1 (es) | 2019-07-09 |
| CN109563043B (zh) | 2022-05-31 |
| JP2019517596A (ja) | 2019-06-24 |
| CO2018013717A2 (es) | 2019-01-18 |
| EP3468953C0 (en) | 2024-05-22 |
| IL263163A (en) | 2018-12-31 |
| WO2017216726A1 (en) | 2017-12-21 |
| PH12018502633A1 (en) | 2019-09-30 |
| CL2018003577A1 (es) | 2019-04-05 |
| JP7051829B2 (ja) | 2022-04-11 |
| US20190194166A1 (en) | 2019-06-27 |
| KR20190017030A (ko) | 2019-02-19 |
| DOP2018000273A (es) | 2019-03-31 |
| CA3026211A1 (en) | 2017-12-21 |
| CA3026226A1 (en) | 2017-12-21 |
| AU2017283790B2 (en) | 2019-08-29 |
| MA45244A (fr) | 2019-04-17 |
| CN109563043A (zh) | 2019-04-02 |
| ES2993451T3 (en) | 2024-12-30 |
| PH12018502633B1 (en) | 2023-02-01 |
| MX391600B (es) | 2025-03-21 |
| EP3468953A1 (en) | 2019-04-17 |
| EP3468953B1 (en) | 2024-05-22 |
| AU2017283790A1 (en) | 2018-11-22 |
| IL263163B (en) | 2021-10-31 |
| US10975056B2 (en) | 2021-04-13 |
| SG11201809559UA (en) | 2018-12-28 |
| CR20180580A (es) | 2019-07-02 |
| WO2017216727A1 (en) | 2017-12-21 |
| MX2018015483A (es) | 2019-03-18 |
| BR112018075992A2 (pt) | 2019-04-02 |
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