JP6832923B2 - ブロモドメイン阻害薬としての2−オキソ−1,2−ジヒドロピリジン−3,5−ジカルボキサミド化合物 - Google Patents
ブロモドメイン阻害薬としての2−オキソ−1,2−ジヒドロピリジン−3,5−ジカルボキサミド化合物 Download PDFInfo
- Publication number
- JP6832923B2 JP6832923B2 JP2018517320A JP2018517320A JP6832923B2 JP 6832923 B2 JP6832923 B2 JP 6832923B2 JP 2018517320 A JP2018517320 A JP 2018517320A JP 2018517320 A JP2018517320 A JP 2018517320A JP 6832923 B2 JP6832923 B2 JP 6832923B2
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- oxo
- dihydropyridine
- dicarboxamide
- benzyl
- 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 COC(C1=CC(Br)=CN(C(*)*)C1=O)OC Chemical compound COC(C1=CC(Br)=CN(C(*)*)C1=O)OC 0.000 description 6
- IQBVYZUOXFKSGT-UHFFFAOYSA-N CCCCOC(C(C=C1C(NC)=O)=CN(Cc2cccc(C)c2F)C1=O)=O Chemical compound CCCCOC(C(C=C1C(NC)=O)=CN(Cc2cccc(C)c2F)C1=O)=O IQBVYZUOXFKSGT-UHFFFAOYSA-N 0.000 description 1
- SDPVKAGJYCRGDD-UHFFFAOYSA-N CNC(C1=CC(Br)=CN(Cc2ccccc2)C1=O)=O Chemical compound CNC(C1=CC(Br)=CN(Cc2ccccc2)C1=O)=O SDPVKAGJYCRGDD-UHFFFAOYSA-N 0.000 description 1
- STZDNDKVRQFUIU-UHFFFAOYSA-N COC(C1=CC=C[U]C1=O)=O Chemical compound COC(C1=CC=C[U]C1=O)=O STZDNDKVRQFUIU-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
- C07D213/82—Amides; Imides in position 3
-
- 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
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
-
- 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
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Transplantation (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (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 |
|---|---|---|---|
| US201562237002P | 2015-10-05 | 2015-10-05 | |
| US62/237,002 | 2015-10-05 | ||
| PCT/EP2016/073532 WO2017060180A1 (en) | 2015-10-05 | 2016-10-03 | 2-oxo-1,2-dihydropyridine-3,5-dicarboxamide compounds as bromodomain inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018529737A JP2018529737A (ja) | 2018-10-11 |
| JP2018529737A5 JP2018529737A5 (enExample) | 2019-11-07 |
| JP6832923B2 true JP6832923B2 (ja) | 2021-02-24 |
Family
ID=57113320
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018517320A Expired - Fee Related JP6832923B2 (ja) | 2015-10-05 | 2016-10-03 | ブロモドメイン阻害薬としての2−オキソ−1,2−ジヒドロピリジン−3,5−ジカルボキサミド化合物 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US10471050B2 (enExample) |
| EP (1) | EP3359531B1 (enExample) |
| JP (1) | JP6832923B2 (enExample) |
| KR (1) | KR20180059551A (enExample) |
| CN (1) | CN108290866B (enExample) |
| AU (1) | AU2016334637A1 (enExample) |
| BR (1) | BR112018006545A2 (enExample) |
| CA (1) | CA2999379A1 (enExample) |
| ES (1) | ES2831322T3 (enExample) |
| RU (1) | RU2018114705A (enExample) |
| WO (1) | WO2017060180A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2016315360B2 (en) | 2015-09-02 | 2019-09-12 | Glaxosmithkline Intellectual Property (No.2) Limited | Pyridinone dicarboxamide for use as bromodomain inhibitors |
| US10370356B2 (en) | 2015-09-22 | 2019-08-06 | Glaxosmithkline Intellectual Property (No. 2) Limited | Pyridinone dicarboxamide for use as bromodomain inhibitors |
| RU2018114705A (ru) | 2015-10-05 | 2019-11-07 | ГлаксоСмитКлайн Интеллекчуал Проперти (N2) Лимитед | Соединения 2-оксо-1,2-дигидропиридин-3,5-дикарбоксамида в качестве ингибиторов бромодомена |
| ES2840848T3 (es) | 2016-04-07 | 2021-07-07 | Glaxosmithkline Ip No 2 Ltd | Derivados de piridilo como inhibidores de bromodominio |
| BR112018073524A2 (pt) * | 2016-05-24 | 2019-05-28 | Glaxosmithkline Ip No 2 Ltd | composto, composição farmacêutica, combinação, uso de um composto ou um sal farmaceuticamente aceitável do mesmo, e, método de tratamento de uma doença ou condição. |
| GB201703282D0 (en) * | 2017-03-01 | 2017-04-12 | Glaxosmithkline Intellectual Property (No 2) Ltd | Compounds |
| JOP20190192A1 (ar) | 2017-03-01 | 2019-08-08 | Glaxosmithkline Ip No 2 Ltd | مشتقات بيرازول بوصفها مثبطات برومودومين |
| GB201814167D0 (en) | 2018-08-31 | 2018-10-17 | Glaxosmithkline Ip No 2 Ltd | Compounds |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR0116539A (pt) | 2000-12-28 | 2003-09-23 | Shionogi & Co | Derivados de piridona tendo uma atividade de ligação para o receptor 2 do tipo canabinóide |
| US20050101590A1 (en) * | 2002-02-19 | 2005-05-12 | Kiyoshi Yasui | Antipruritics |
| WO2004033446A1 (en) | 2002-10-09 | 2004-04-22 | Danter Wayne R | Protein tyrosine kinase inhibitors |
| EP1433788A1 (en) | 2002-12-23 | 2004-06-30 | Aventis Pharma Deutschland GmbH | Pyrazole-derivatives as factor Xa inhibitors |
| GB0919434D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| PE20150953A1 (es) | 2012-11-08 | 2015-06-20 | Bristol Myers Squibb Co | Compuestos de piridilo sustituidos con heteroarilo utiles como moduladores de cinasa |
| CA2895905A1 (en) | 2012-12-21 | 2014-06-26 | Zenith Epigenetics Corp. | Novel heterocyclic compounds as bromodomain inhibitors |
| EP3027604B1 (en) | 2013-07-31 | 2019-02-20 | Zenith Epigenetics Ltd. | Novel quinazolinones as bromodomain inhibitors |
| AU2016315360B2 (en) | 2015-09-02 | 2019-09-12 | Glaxosmithkline Intellectual Property (No.2) Limited | Pyridinone dicarboxamide for use as bromodomain inhibitors |
| RU2018114705A (ru) | 2015-10-05 | 2019-11-07 | ГлаксоСмитКлайн Интеллекчуал Проперти (N2) Лимитед | Соединения 2-оксо-1,2-дигидропиридин-3,5-дикарбоксамида в качестве ингибиторов бромодомена |
| ES2840848T3 (es) | 2016-04-07 | 2021-07-07 | Glaxosmithkline Ip No 2 Ltd | Derivados de piridilo como inhibidores de bromodominio |
| BR112018073524A2 (pt) | 2016-05-24 | 2019-05-28 | Glaxosmithkline Ip No 2 Ltd | composto, composição farmacêutica, combinação, uso de um composto ou um sal farmaceuticamente aceitável do mesmo, e, método de tratamento de uma doença ou condição. |
-
2016
- 2016-10-03 RU RU2018114705A patent/RU2018114705A/ru not_active Application Discontinuation
- 2016-10-03 KR KR1020187012923A patent/KR20180059551A/ko not_active Withdrawn
- 2016-10-03 JP JP2018517320A patent/JP6832923B2/ja not_active Expired - Fee Related
- 2016-10-03 CA CA2999379A patent/CA2999379A1/en not_active Abandoned
- 2016-10-03 AU AU2016334637A patent/AU2016334637A1/en not_active Abandoned
- 2016-10-03 BR BR112018006545A patent/BR112018006545A2/pt active Search and Examination
- 2016-10-03 US US15/766,222 patent/US10471050B2/en not_active Expired - Fee Related
- 2016-10-03 WO PCT/EP2016/073532 patent/WO2017060180A1/en not_active Ceased
- 2016-10-03 CN CN201680071214.5A patent/CN108290866B/zh not_active Expired - Fee Related
- 2016-10-03 EP EP16778310.9A patent/EP3359531B1/en active Active
- 2016-10-03 ES ES16778310T patent/ES2831322T3/es active Active
Also Published As
| Publication number | Publication date |
|---|---|
| KR20180059551A (ko) | 2018-06-04 |
| ES2831322T3 (es) | 2021-06-08 |
| AU2016334637A1 (en) | 2018-04-12 |
| JP2018529737A (ja) | 2018-10-11 |
| US20180280368A1 (en) | 2018-10-04 |
| US10471050B2 (en) | 2019-11-12 |
| CA2999379A1 (en) | 2017-04-13 |
| CN108290866A (zh) | 2018-07-17 |
| BR112018006545A2 (pt) | 2018-10-16 |
| EP3359531A1 (en) | 2018-08-15 |
| WO2017060180A1 (en) | 2017-04-13 |
| EP3359531B1 (en) | 2020-08-19 |
| CN108290866B (zh) | 2020-12-18 |
| RU2018114705A (ru) | 2019-11-07 |
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Legal Events
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