KR102194611B1 - 티로신 수용체 키나아제 btk 억제제로서 치환된 n-(3-(피리미딘-4-일)페닐)아크릴아미드 유사체 - Google Patents
티로신 수용체 키나아제 btk 억제제로서 치환된 n-(3-(피리미딘-4-일)페닐)아크릴아미드 유사체 Download PDFInfo
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- KR102194611B1 KR102194611B1 KR1020157011753A KR20157011753A KR102194611B1 KR 102194611 B1 KR102194611 B1 KR 102194611B1 KR 1020157011753 A KR1020157011753 A KR 1020157011753A KR 20157011753 A KR20157011753 A KR 20157011753A KR 102194611 B1 KR102194611 B1 KR 102194611B1
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- alkyl
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- 0 S=*Cc1ccccc1 Chemical compound S=*Cc1ccccc1 0.000 description 7
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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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
- A61K31/495—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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- 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
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen 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
- C07D401/12—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
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- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Engineering & Computer Science (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Oncology (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Physical Education & Sports Medicine (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Epidemiology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261709519P | 2012-10-04 | 2012-10-04 | |
| US61/709,519 | 2012-10-04 | ||
| PCT/US2013/063549 WO2014055928A2 (en) | 2012-10-04 | 2013-10-04 | Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20150067759A KR20150067759A (ko) | 2015-06-18 |
| KR102194611B1 true KR102194611B1 (ko) | 2020-12-23 |
Family
ID=50435582
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020157011753A Expired - Fee Related KR102194611B1 (ko) | 2012-10-04 | 2013-10-04 | 티로신 수용체 키나아제 btk 억제제로서 치환된 n-(3-(피리미딘-4-일)페닐)아크릴아미드 유사체 |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US9828376B2 (enExample) |
| EP (2) | EP2903972B1 (enExample) |
| JP (1) | JP6401169B2 (enExample) |
| KR (1) | KR102194611B1 (enExample) |
| CN (1) | CN104822664B (enExample) |
| CA (1) | CA2887435A1 (enExample) |
| WO (1) | WO2014055928A2 (enExample) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012135801A1 (en) | 2011-04-01 | 2012-10-04 | University Of Utah Research Foundation | Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors |
| WO2014055934A2 (en) | 2012-10-04 | 2014-04-10 | University Of Utah Research Foundation | Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors |
| KR102194611B1 (ko) * | 2012-10-04 | 2020-12-23 | 유니버시티 오브 유타 리서치 파운데이션 | 티로신 수용체 키나아제 btk 억제제로서 치환된 n-(3-(피리미딘-4-일)페닐)아크릴아미드 유사체 |
| US9512084B2 (en) | 2013-11-29 | 2016-12-06 | Novartis Ag | Amino pyrimidine derivatives |
| CN105712998B (zh) * | 2014-12-05 | 2019-12-13 | 上海润诺生物科技有限公司 | 氮杂吲哚类衍生物、其制备方法及其在医药上的应用 |
| CN117281803A (zh) | 2018-07-31 | 2023-12-26 | 罗索肿瘤学公司 | 喷雾干燥的分散体和制剂 |
| US12157730B2 (en) | 2019-03-19 | 2024-12-03 | Voronoi Inc. | Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component |
| MA55380A (fr) | 2019-03-19 | 2022-01-26 | B2Sbio Inc | Dérivé hétéroaryle, son procédé de production et composition pharmaceutique le comprenant en tant que constituant efficace |
| JP2022526713A (ja) | 2019-03-21 | 2022-05-26 | オンクセオ | がんの処置のための、キナーゼ阻害剤と組み合わせたDbait分子 |
| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| EP4135700A4 (en) * | 2020-04-15 | 2024-04-17 | Pyramid Biosciences, Inc. | PROCESSES FOR PREPARING RECEPTOR TYROSINE KINASE INHIBITORS |
| WO2022236255A2 (en) * | 2021-05-03 | 2022-11-10 | Nuvation Bio Inc. | Heterocyclic compounds as kinase inhibitors |
| WO2023168298A2 (en) * | 2022-03-02 | 2023-09-07 | Denali Therapeutics Inc. | Compounds, compositions, and methods |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9523675D0 (en) | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| GB9924862D0 (en) | 1999-10-20 | 1999-12-22 | Celltech Therapeutics Ltd | Chemical compounds |
| JP2007500179A (ja) | 2003-07-30 | 2007-01-11 | サイクラセル・リミテッド | キナーゼ阻害剤としての2−アミノフェニル−4−フェニルピリミジン |
| ATE499364T1 (de) | 2004-04-09 | 2011-03-15 | Merck Sharp & Dohme | Hemmer der akt aktivität |
| MX362412B (es) | 2005-11-01 | 2019-01-15 | Targegen Inc | Inhibidores de biaril meta-pirimidina de cinasas. |
| US8133900B2 (en) | 2005-11-01 | 2012-03-13 | Targegen, Inc. | Use of bi-aryl meta-pyrimidine inhibitors of kinases |
| EA200870217A1 (ru) * | 2006-01-30 | 2009-02-27 | Экселиксис, Инк. | 4-арил-2-аминопиримидины или 4-арил-2-аминоалкилпиримидины в качестве модуляторов jak-2 и содержащие их фармацевтические композиции |
| BRPI0811617A2 (pt) | 2007-05-04 | 2017-06-06 | Irm Llc | derivados de primidina e composições como inibidores de c-kit e pdgfr quinase. |
| CA2698511C (en) * | 2007-09-04 | 2016-10-11 | The Scripps Research Institute | Substituted pyrimidinyl-amines as protein kinase inhibitors |
| US8450335B2 (en) * | 2008-06-27 | 2013-05-28 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| US8426428B2 (en) | 2008-12-05 | 2013-04-23 | Principia Biopharma, Inc. | EGFR kinase knockdown via electrophilically enhanced inhibitors |
| CN102356075B (zh) | 2009-01-23 | 2015-06-10 | 里格尔药品股份有限公司 | 抑制jak途径的组合物和方法 |
| CN102307875A (zh) | 2009-02-09 | 2012-01-04 | 苏伯俭股份有限公司 | 吡咯并嘧啶基axl激酶抑制剂 |
| JP5918693B2 (ja) * | 2009-05-05 | 2016-05-18 | ダナ ファーバー キャンサー インスティテュート インコーポレイテッド | Egfr阻害剤及び疾患の治療方法 |
| US7718662B1 (en) | 2009-10-12 | 2010-05-18 | Pharmacyclics, Inc. | Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase |
| EP2693881B1 (en) | 2011-04-01 | 2019-09-04 | University of Utah Research Foundation | Substituted n-phenylpyrimidin-2-amine analogs as inhibitors of the axl kinase |
| WO2012135801A1 (en) * | 2011-04-01 | 2012-10-04 | University Of Utah Research Foundation | Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors |
| US8993756B2 (en) | 2011-12-06 | 2015-03-31 | Merck Sharp & Dohme Corp. | Pyrrolopyrimidines as janus kinase inhibitors |
| WO2014055934A2 (en) | 2012-10-04 | 2014-04-10 | University Of Utah Research Foundation | Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors |
| KR102194611B1 (ko) | 2012-10-04 | 2020-12-23 | 유니버시티 오브 유타 리서치 파운데이션 | 티로신 수용체 키나아제 btk 억제제로서 치환된 n-(3-(피리미딘-4-일)페닐)아크릴아미드 유사체 |
-
2013
- 2013-10-04 KR KR1020157011753A patent/KR102194611B1/ko not_active Expired - Fee Related
- 2013-10-04 CN CN201380063038.7A patent/CN104822664B/zh not_active Expired - Fee Related
- 2013-10-04 CA CA 2887435 patent/CA2887435A1/en not_active Abandoned
- 2013-10-04 JP JP2015535838A patent/JP6401169B2/ja not_active Expired - Fee Related
- 2013-10-04 EP EP13844466.6A patent/EP2903972B1/en active Active
- 2013-10-04 EP EP19213349.4A patent/EP3680238A1/en not_active Withdrawn
- 2013-10-04 WO PCT/US2013/063549 patent/WO2014055928A2/en not_active Ceased
- 2013-10-04 US US14/433,579 patent/US9828376B2/en not_active Expired - Fee Related
-
2017
- 2017-11-01 US US15/801,123 patent/US20180134719A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| HK1213243A1 (en) | 2016-06-30 |
| KR20150067759A (ko) | 2015-06-18 |
| EP2903972A2 (en) | 2015-08-12 |
| US20180134719A1 (en) | 2018-05-17 |
| JP2015532304A (ja) | 2015-11-09 |
| US20150252048A1 (en) | 2015-09-10 |
| EP2903972A4 (en) | 2016-04-06 |
| WO2014055928A3 (en) | 2014-06-26 |
| CN104822664A (zh) | 2015-08-05 |
| WO2014055928A2 (en) | 2014-04-10 |
| US9828376B2 (en) | 2017-11-28 |
| EP2903972B1 (en) | 2019-12-04 |
| CN104822664B (zh) | 2017-01-18 |
| EP3680238A1 (en) | 2020-07-15 |
| CA2887435A1 (en) | 2014-04-10 |
| JP6401169B2 (ja) | 2018-10-03 |
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