BR112013026137B1 - pirimidinil-pirróis substituídos ativos como inibidores da quinase - Google Patents
pirimidinil-pirróis substituídos ativos como inibidores da quinase Download PDFInfo
- Publication number
- BR112013026137B1 BR112013026137B1 BR112013026137-4A BR112013026137A BR112013026137B1 BR 112013026137 B1 BR112013026137 B1 BR 112013026137B1 BR 112013026137 A BR112013026137 A BR 112013026137A BR 112013026137 B1 BR112013026137 B1 BR 112013026137B1
- Authority
- BR
- Brazil
- Prior art keywords
- compound
- formula
- pyrrole
- aminopyrimidin
- carboxamide
- Prior art date
Links
Classifications
-
- 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
- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- 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
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/025—Boronic and borinic acid compounds
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (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)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11162960.6 | 2011-04-19 | ||
| EP11162960 | 2011-04-19 | ||
| PCT/EP2012/056266 WO2012143248A1 (en) | 2011-04-19 | 2012-04-05 | Substituted pyrimidinyl-pyrroles active as kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| BR112013026137A2 BR112013026137A2 (pt) | 2017-10-24 |
| BR112013026137A8 BR112013026137A8 (pt) | 2018-01-30 |
| BR112013026137B1 true BR112013026137B1 (pt) | 2020-12-01 |
Family
ID=45928917
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112013026137-4A BR112013026137B1 (pt) | 2011-04-19 | 2012-04-05 | pirimidinil-pirróis substituídos ativos como inibidores da quinase |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US9283224B2 (enExample) |
| EP (1) | EP2699564B1 (enExample) |
| JP (1) | JP5970537B2 (enExample) |
| CN (1) | CN103502241B (enExample) |
| BR (1) | BR112013026137B1 (enExample) |
| ES (1) | ES2616458T3 (enExample) |
| RU (1) | RU2621732C2 (enExample) |
| WO (1) | WO2012143248A1 (enExample) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| JP6219922B2 (ja) * | 2012-03-30 | 2017-10-25 | ダウ アグロサイエンシィズ エルエルシー | ３−置換−６−トリフルオロメチルピリジンを調製する方法およびハロゲン化６−トリクロロメチルピリジンを使用する方法 |
| US20160237158A1 (en) * | 2013-09-23 | 2016-08-18 | Institut National De La Santé Et Da La Recherche Médicale (Inserm) | Methods and Compositions for Targeting Tumor Microenvironment and for preventing Metastasis |
| PT3322706T (pt) | 2015-07-16 | 2021-03-08 | Array Biopharma Inc | Compostos de pirazolo[1,5-a]piridina substituídos como inibidores da quinase do ret |
| TN2019000271A1 (en) | 2015-10-26 | 2021-01-07 | Univ Colorado Regents | Point mutations in trk inhibitor-resistant cancer and methods relating to the same |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| IL304018A (en) | 2016-04-04 | 2023-08-01 | Loxo Oncology Inc | Liquid formulations of (S)-N-(5-((R)-2-(5,2-difluorophenyl)-pyrrolidine-1-yl)-pyrazolo[5,1-A]pyrimidin-3-yl)-3 -hydroxypyrrolidine-1-carboxamide |
| TN2019000332A1 (en) | 2016-04-04 | 2021-05-07 | Loxo Oncology Inc | Methods of treating pediatric cancers |
| ES2952056T3 (es) | 2016-05-18 | 2023-10-26 | Loxo Oncology Inc | Preparación de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| JP6888101B2 (ja) | 2017-01-18 | 2021-06-16 | アレイ バイオファーマ インコーポレイテッド | ＲＥＴキナーゼ阻害剤としての置換ピラゾロ［１，５−ａ］ピラジン化合物 |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| GB201706806D0 (en) | 2017-04-28 | 2017-06-14 | Sentinel Oncology Ltd | Pharmaceutical compounds |
| TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
| TWI876442B (zh) | 2017-10-10 | 2025-03-11 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
| CN107970438B (zh) * | 2017-11-28 | 2021-08-13 | 镇江市中西医结合医院（镇江市第二人民医院） | 一种神经再生凝胶及其制备方法和应用 |
| WO2019143977A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| WO2019143991A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | SUBSTITUTED PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS AS RET KINASE INHIBITORS |
| JP6997876B2 (ja) | 2018-01-18 | 2022-02-04 | アレイ バイオファーマ インコーポレイテッド | Ｒｅｔキナーゼ阻害剤としての置換ピラゾリル［４，３－ｃ］ピリジン化合物 |
| JP7286755B2 (ja) | 2018-07-31 | 2023-06-05 | ロクソ オンコロジー， インコーポレイテッド | （ｓ）－５－アミノ－３－（４－（（５－フルオロ－２－メトキシベンズアミド）メチル）フェニル）－１－（１，１，１－トリフルオロプロパン－２－イル）－１ｈ－ピラゾール－４－カルボキサミドの噴霧乾燥分散体および製剤 |
| CA3111984A1 (en) | 2018-09-10 | 2020-03-19 | Array Biopharma Inc. | Fused heterocyclic compounds as ret kinase inhibitors |
| JP2022515198A (ja) | 2018-12-19 | 2022-02-17 | アレイ バイオファーマ インコーポレイテッド | ＦＧＦＲチロシンキナーゼの阻害剤としての置換ピラゾロ［１，５－ａ］ピリジン化合物 |
| CN113474337A (zh) | 2018-12-19 | 2021-10-01 | 奥瑞生物药品公司 | 作为fgfr抑制剂用于治疗癌症的7-((3，5-二甲氧基苯基)氨基)喹喔啉衍生物 |
| US20220372135A1 (en) | 2019-09-27 | 2022-11-24 | Disc Medicine, Inc. | Methods for treating myelofibrosis and related conditions |
| WO2021113492A1 (en) | 2019-12-06 | 2021-06-10 | Schrödinger, Inc. | Cyclic compounds and methods of using same |
| MX2022007171A (es) | 2019-12-27 | 2022-08-22 | Schroedinger Inc | Compuestos cíclicos y métodos de uso de estos. |
| CA3177830A1 (en) | 2020-05-13 | 2021-11-18 | Maria BECONI | Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis |
| CN116490507A (zh) | 2020-09-10 | 2023-07-25 | 薛定谔公司 | 用于治疗癌症的杂环包缩合cdc7激酶抑制剂 |
| CN116323595B (zh) * | 2020-09-23 | 2025-08-19 | 内尔维亚诺医疗科学公司 | 作为激酶抑制剂的吡唑基-嘧啶衍生物 |
| US20240148732A1 (en) | 2021-01-26 | 2024-05-09 | Schrödinger, Inc. | Tricyclic compounds useful in the treatment of cancer, autoimmune and inflammatory disorders |
| TW202300150A (zh) | 2021-03-18 | 2023-01-01 | 美商薛定諤公司 | 環狀化合物及其使用方法 |
| WO2025059027A1 (en) | 2023-09-11 | 2025-03-20 | Schrödinger, Inc. | Cyclopenta[e]pyrazolo[1,5-a]pyrimidine derivatives as malt1 inhibitors |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7419984B2 (en) * | 2002-10-17 | 2008-09-02 | Cell Therapeutics, Inc. | Pyrimidines and uses thereof |
| TW200526626A (en) * | 2003-09-13 | 2005-08-16 | Astrazeneca Ab | Chemical compounds |
| CN101421250A (zh) * | 2006-01-30 | 2009-04-29 | 埃克塞里艾克西斯公司 | 作为jak-2调节剂的4-芳基-2-氨基-嘧啶或4-芳基-2-氨基烷基-嘧啶及包含它们的药物组合物 |
| KR20090008286A (ko) * | 2006-03-27 | 2009-01-21 | 네르비아노 메디칼 사이언시스 에스.알.엘. | 키나제 억제제로서의 피리딜- 및 피리미디닐-치환된 피롤-,티오펜- 및 푸란- 유도체 |
| WO2009046416A1 (en) * | 2007-10-05 | 2009-04-09 | Targegen Inc. | Anilinopyrimidines as jak kinase inhibitors |
| TWI426074B (zh) * | 2008-04-30 | 2014-02-11 | Nerviano Medical Sciences Srl | ５－（２－胺基－嘧啶－４－基）－２－芳基－１ｈ－吡咯－３－羧醯胺之製造方法 |
| EP2417125B1 (en) * | 2009-03-27 | 2015-09-09 | Nerviano Medical Sciences S.r.l. | N-aryl-2-(2-arylaminopyrimidin-4-yl)pyrrol-4-carboxamide derivatives as mps1 kinase inhibitors |
| CA2779785C (en) * | 2009-11-04 | 2017-09-12 | Nerviano Medical Sciences S.R.L. | Process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1h-pyrrole-3-carboxamides |
| CN102666528B (zh) * | 2009-11-11 | 2014-04-16 | 内尔维阿诺医学科学有限公司 | 晶体cdc7 抑制剂盐 |
| EP2736514B1 (en) * | 2011-07-28 | 2017-10-18 | Nerviano Medical Sciences S.r.l. | Alkynyl substituted pyrimidinyl-pyrroles active as kinases inhibitors |
-
2012
- 2012-04-05 RU RU2013151174A patent/RU2621732C2/ru active
- 2012-04-05 BR BR112013026137-4A patent/BR112013026137B1/pt not_active IP Right Cessation
- 2012-04-05 CN CN201280018834.4A patent/CN103502241B/zh not_active Expired - Fee Related
- 2012-04-05 EP EP12711904.8A patent/EP2699564B1/en active Active
- 2012-04-05 US US14/112,559 patent/US9283224B2/en active Active
- 2012-04-05 JP JP2014505570A patent/JP5970537B2/ja not_active Expired - Fee Related
- 2012-04-05 ES ES12711904.8T patent/ES2616458T3/es active Active
- 2012-04-05 WO PCT/EP2012/056266 patent/WO2012143248A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| HK1187905A1 (zh) | 2014-04-17 |
| RU2013151174A (ru) | 2015-05-27 |
| CN103502241B (zh) | 2016-03-23 |
| CN103502241A (zh) | 2014-01-08 |
| EP2699564B1 (en) | 2016-12-14 |
| BR112013026137A8 (pt) | 2018-01-30 |
| US9283224B2 (en) | 2016-03-15 |
| RU2621732C2 (ru) | 2017-06-07 |
| EP2699564A1 (en) | 2014-02-26 |
| JP5970537B2 (ja) | 2016-08-17 |
| ES2616458T3 (es) | 2017-06-13 |
| WO2012143248A1 (en) | 2012-10-26 |
| JP2014516360A (ja) | 2014-07-10 |
| BR112013026137A2 (pt) | 2017-10-24 |
| US20140155421A1 (en) | 2014-06-05 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] | ||
| B06F | Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette] | ||
| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] | ||
| B06U | Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette] | ||
| B06A | Patent application procedure suspended [chapter 6.1 patent gazette] | ||
| B09A | Decision: intention to grant [chapter 9.1 patent gazette] | ||
| B16A | Patent or certificate of addition of invention granted [chapter 16.1 patent gazette] |
Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 05/04/2012, OBSERVADAS AS CONDICOES LEGAIS. |
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| B21F | Lapse acc. art. 78, item iv - on non-payment of the annual fees in time |
Free format text: REFERENTE A 13A ANUIDADE. |
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| B24J | Lapse because of non-payment of annual fees (definitively: art 78 iv lpi, resolution 113/2013 art. 12) |
Free format text: EM VIRTUDE DA EXTINCAO PUBLICADA NA RPI 2822 DE 04-02-2025 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDA A EXTINCAO DA PATENTE E SEUS CERTIFICADOS, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013. |