KR20160012195A - Bet 억제제로서의 피라졸로-피롤리딘-4-온 유도체 및 질환의 치료에서의 그의 용도 - Google Patents
Bet 억제제로서의 피라졸로-피롤리딘-4-온 유도체 및 질환의 치료에서의 그의 용도 Download PDFInfo
- Publication number
- KR20160012195A KR20160012195A KR1020157036224A KR20157036224A KR20160012195A KR 20160012195 A KR20160012195 A KR 20160012195A KR 1020157036224 A KR1020157036224 A KR 1020157036224A KR 20157036224 A KR20157036224 A KR 20157036224A KR 20160012195 A KR20160012195 A KR 20160012195A
- Authority
- KR
- South Korea
- Prior art keywords
- methyl
- chlorophenyl
- cyclopropyl
- triazolo
- dihydropyrrolo
- 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.)
- Withdrawn
Links
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Classifications
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- 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
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4192—1,2,3-Triazoles
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/16—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
- C07D249/18—Benzotriazoles
-
- 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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13169441 | 2013-05-28 | ||
| EP13169441.6 | 2013-05-28 | ||
| PCT/IB2014/061736 WO2014191906A1 (en) | 2013-05-28 | 2014-05-27 | Pyrazolo-pyrrolidin-4-one derivatives as bet inhibitors and their use in the treatment of disease |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20160012195A true KR20160012195A (ko) | 2016-02-02 |
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| MX366703B (es) | 2013-03-15 | 2019-07-22 | Incyte Holdings Corp | Heterociclos tricíclicos como inhibidores de la proteína bet. |
| MX2015016421A (es) | 2013-05-28 | 2016-03-03 | Novartis Ag | Derivados de pirazolo-pirrolidin-4-ona como inhibidores de bet y su uso en el tratamiento de enfermedades. |
| EP3019502B1 (en) | 2013-07-08 | 2017-05-17 | Incyte Holdings Corporation | Tricyclic heterocycles as bet protein inhibitors |
| 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 |
| WO2015081189A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| WO2015095492A1 (en) | 2013-12-19 | 2015-06-25 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| KR102702503B1 (ko) | 2014-04-23 | 2024-09-05 | 인사이트 홀딩스 코포레이션 | BET 단백질의 저해제로서의 1H-피롤로[2,3-c]피리딘-7(6H)-온 및 피라졸로[3,4-c]피리딘-7(6H)-온 |
| WO2016044130A1 (en) | 2014-09-15 | 2016-03-24 | Incyte Corporation | Tricyclic heterocycles for use as bet protein inhibitors |
| GB201504694D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Covalent conjugates |
| US20170121347A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
| CN109153647A (zh) | 2016-02-15 | 2019-01-04 | 分子医学研究中心责任有限公司 | 用于治疗癌症的taf1抑制剂 |
| PH12021551886A1 (en) | 2016-06-20 | 2023-07-17 | Incyte Corp | Crystalline solid forms of a bet inhibitor |
| CN110225755A (zh) | 2016-11-14 | 2019-09-10 | 分子医学研究中心责任有限公司 | Brd4抑制剂和抗叶酸剂的组合用于治疗癌症 |
| MX2020006612A (es) | 2017-12-20 | 2020-11-09 | Betta Pharmaceuticals Co Ltd | Compuesto que funciona como inhibidor de proteína de bromodominio y composición. |
| KR20210031852A (ko) * | 2018-03-05 | 2021-03-23 | 클리니쿰 레히츠 데어 이자르 데어 테크니쉔 우니베르지테트 뮌헨 | 종양 세포 붕괴성 아데노바이러스와 cdk4/6 억제제의 조합물에 의한 종양의 치료 |
| CN114466849B (zh) * | 2019-07-12 | 2024-07-12 | 欣尼克免疫有限公司 | 作为isoqc和/或qc酶的抑制剂的n-取代的-3,4-(稠合5-环)-5-苯基-吡咯烷-2-酮化合物 |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
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2014
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- 2014-05-27 EP EP14728350.1A patent/EP3004108B1/en not_active Not-in-force
- 2014-05-27 US US14/892,623 patent/US9624247B2/en not_active Expired - Fee Related
- 2014-05-27 ES ES14728350.1T patent/ES2656471T3/es active Active
- 2014-05-27 WO PCT/IB2014/061736 patent/WO2014191906A1/en not_active Ceased
- 2014-05-27 BR BR112015029401A patent/BR112015029401A8/pt not_active Application Discontinuation
- 2014-05-27 CN CN201480030590.0A patent/CN105263934B/zh not_active Expired - Fee Related
- 2014-05-27 PT PT147283501T patent/PT3004108T/pt unknown
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- 2014-05-27 PL PL14728350T patent/PL3004108T3/pl unknown
- 2014-05-27 AU AU2014272695A patent/AU2014272695B2/en not_active Ceased
- 2014-05-27 KR KR1020157036224A patent/KR20160012195A/ko not_active Withdrawn
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Also Published As
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| EA028175B1 (ru) | 2017-10-31 |
| US20160102107A1 (en) | 2016-04-14 |
| PT3004108T (pt) | 2018-01-24 |
| US9624247B2 (en) | 2017-04-18 |
| BR112015029401A8 (pt) | 2020-03-17 |
| CN105263934A (zh) | 2016-01-20 |
| EP3004108B1 (en) | 2017-10-18 |
| ES2656471T3 (es) | 2018-02-27 |
| EA201592255A1 (ru) | 2016-04-29 |
| WO2014191906A1 (en) | 2014-12-04 |
| PL3004108T3 (pl) | 2018-03-30 |
| JP2016520118A (ja) | 2016-07-11 |
| MX2015016421A (es) | 2016-03-03 |
| CA2912986A1 (en) | 2014-12-04 |
| AU2014272695B2 (en) | 2016-10-20 |
| AU2014272695A1 (en) | 2015-11-26 |
| CN105263934B (zh) | 2017-09-08 |
| BR112015029401A2 (pt) | 2017-07-25 |
| EP3004108A1 (en) | 2016-04-13 |
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