RU2621732C2 - Замещенные пиримидинилпирролы, активные в качестве ингибиторов киназы - Google Patents
Замещенные пиримидинилпирролы, активные в качестве ингибиторов киназы Download PDFInfo
- Publication number
- RU2621732C2 RU2621732C2 RU2013151174A RU2013151174A RU2621732C2 RU 2621732 C2 RU2621732 C2 RU 2621732C2 RU 2013151174 A RU2013151174 A RU 2013151174A RU 2013151174 A RU2013151174 A RU 2013151174A RU 2621732 C2 RU2621732 C2 RU 2621732C2
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- formula
- compound
- pyrrole
- carboxamide
- aminopyrimidin
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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
- C07D403/04—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
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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
-
- 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
- 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
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- 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 (2)
| Publication Number | Publication Date |
|---|---|
| RU2013151174A RU2013151174A (ru) | 2015-05-27 |
| RU2621732C2 true RU2621732C2 (ru) | 2017-06-07 |
Family
ID=45928917
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2013151174A RU2621732C2 (ru) | 2011-04-19 | 2012-04-05 | Замещенные пиримидинилпирролы, активные в качестве ингибиторов киназы |
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 |
| BR112014024064B8 (pt) | 2012-03-30 | 2022-10-11 | Dow Agrosciences Llc | Métodos para preparação de 3-substituída-6-triflúormetil piridinas e para formação de 3-halo-6-triflúormetil piridina |
| WO2015040243A2 (en) * | 2013-09-23 | 2015-03-26 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and compositions for targeting tumor microenvironment and for preventing metastasis |
| JP6816100B2 (ja) | 2015-07-16 | 2021-01-20 | アレイ バイオファーマ、インコーポレイテッド | RETキナーゼ阻害物質としての置換ピラゾロ[1,5−a]ピリジン化合物 |
| US10724102B2 (en) | 2015-10-26 | 2020-07-28 | Loxo Oncology, Inc. | Point mutations in TRK inhibitor-resistant cancer and methods relating to the same |
| SG11201808559PA (en) | 2016-04-04 | 2018-10-30 | Loxo Oncology Inc | Liquid formulations of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| PL3439663T3 (pl) | 2016-04-04 | 2024-11-18 | Loxo Oncology, Inc. | Sposoby leczenia nowotworów wieku dziecięcego |
| FI3800189T3 (fi) | 2016-05-18 | 2023-07-31 | Loxo Oncology Inc | (s)-n-(5-((r)-2-(2,5-difluorifenyyli)pyrrolidin-1-yyli)pyratsolo[1,5-a]pyrimidin-3-yyli)-3-hydroksipyrrolidiini-1-karboksamidin valmistaminen |
| 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 |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| ES2948194T3 (es) | 2017-01-18 | 2023-09-01 | Array Biopharma Inc | Compuestos de pirazolo[1,5-a]pirazina sustituida como inhibidores de la cinasa RET |
| 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 |
| TWI812649B (zh) | 2017-10-10 | 2023-08-21 | 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 |
| 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 |
| 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 |
| TW201938169A (zh) | 2018-01-18 | 2019-10-01 | 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[3,4-d]嘧啶化合物 |
| US11603374B2 (en) | 2018-01-18 | 2023-03-14 | Array Biopharma Inc. | Substituted pyrrolo[2,3-d]pyrimidines 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 |
| CA3224985A1 (en) | 2018-07-31 | 2020-02-06 | Loxo Oncology, Inc. | Spray-dried dispersions, formulations, and polymorphs of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1h-pyrazole-4-carboxamide |
| CA3111984A1 (en) | 2018-09-10 | 2020-03-19 | Array Biopharma Inc. | Fused heterocyclic compounds as ret kinase inhibitors |
| CN113490666A (zh) | 2018-12-19 | 2021-10-08 | 奥瑞生物药品公司 | 作为fgfr酪氨酸激酶的抑制剂的取代的吡唑并[1,5-a]吡啶化合物 |
| EP3898615A1 (en) | 2018-12-19 | 2021-10-27 | Array Biopharma, Inc. | 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer |
| US20220372135A1 (en) | 2019-09-27 | 2022-11-24 | Disc Medicine, Inc. | Methods for treating myelofibrosis and related conditions |
| EP4069369A4 (en) | 2019-12-06 | 2024-02-14 | Schrödinger, Inc. | CYCLIC COMPOUNDS AND METHODS OF USE THEREOF |
| PH12022551523A1 (en) | 2019-12-27 | 2024-01-29 | SchraDinger Inc | Cyclic compounds and methods of using same |
| IL297437A (en) | 2020-05-13 | 2022-12-01 | Disc Medicine Inc | 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 |
| US20240285621A1 (en) * | 2020-09-23 | 2024-08-29 | Nerviano Medical Sciences S.R.L. | Pyrazolyl-pyrimidine derivatives as kinase inhibitors |
| JP2024505890A (ja) | 2021-01-26 | 2024-02-08 | シュレーディンガー, インコーポレイテッド | がん、自己免疫及び炎症性障害の治療に有用な三環式化合物 |
| 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 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040204386A1 (en) * | 2002-10-17 | 2004-10-14 | Cell Therapeutics, Inc. | Pyrimidines and uses thereof |
| WO2007110344A1 (en) * | 2006-03-27 | 2007-10-04 | Nerviano Medical Sciences S.R.L. | Pyridyl- and pyrimidinyl-substituted pyrrole-, thiophene- and furane-derivatives as kinase inhibitors |
| RU2006112046A (ru) * | 2003-09-13 | 2007-11-10 | Астразенека Аб (Se) | Производные пиррола с антибактериальным действием |
| WO2009133170A1 (en) * | 2008-04-30 | 2009-11-05 | Nerviano Medical Sciences S.R.L. | Process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1h-pyrrole-3-carboxamides |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| WO2009046416A1 (en) * | 2007-10-05 | 2009-04-09 | Targegen Inc. | Anilinopyrimidines as jak kinase inhibitors |
| WO2010108921A1 (en) * | 2009-03-27 | 2010-09-30 | Nerviano Medical Sciences S.R.L. | N-aryl-2-(2-arylaminopyrimidin-4-yl)pyrrol-4-carboxamide derivatives as mps1 kinase inhibitors |
| JP5715146B2 (ja) * | 2009-11-04 | 2015-05-07 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | 5−(2−アミノ−ピリミジン−4−イル)−2−アリール−1h−ピロール−3−カルボキサミドの調製方法 |
| EP2499128B1 (en) * | 2009-11-11 | 2015-06-03 | Nerviano Medical Sciences S.r.l. | Crystalline cdc7 inhibitor salts |
| JP6016915B2 (ja) * | 2011-07-28 | 2016-10-26 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | キナーゼ阻害剤として活性なアルキニル置換ピリミジニルピロール |
-
2012
- 2012-04-05 EP EP12711904.8A patent/EP2699564B1/en active Active
- 2012-04-05 RU RU2013151174A patent/RU2621732C2/ru 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 WO PCT/EP2012/056266 patent/WO2012143248A1/en not_active Ceased
- 2012-04-05 ES ES12711904.8T patent/ES2616458T3/es active 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
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040204386A1 (en) * | 2002-10-17 | 2004-10-14 | Cell Therapeutics, Inc. | Pyrimidines and uses thereof |
| RU2006112046A (ru) * | 2003-09-13 | 2007-11-10 | Астразенека Аб (Se) | Производные пиррола с антибактериальным действием |
| WO2007110344A1 (en) * | 2006-03-27 | 2007-10-04 | Nerviano Medical Sciences S.R.L. | Pyridyl- and pyrimidinyl-substituted pyrrole-, thiophene- and furane-derivatives as kinase inhibitors |
| EA015126B1 (ru) * | 2006-03-27 | 2011-06-30 | НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. | Пиридил- и пиримидинилзамещённые производные пиррола, тиофена и фурана в качестве ингибиторов киназ |
| WO2009133170A1 (en) * | 2008-04-30 | 2009-11-05 | Nerviano Medical Sciences S.R.L. | Process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1h-pyrrole-3-carboxamides |
| EA019036B1 (ru) * | 2008-04-30 | 2013-12-30 | НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. | Способ получения 5-(2-аминопиримидин-4-ил)-2-арил-1н-пиррол-3-карбоксамидов |
Non-Patent Citations (1)
| Title |
|---|
| DATABASE REGISTRY, CHEMICAL ABSTRACTS SERVICE, COLUMBIO OHIO, US: abstracts REGISTRY: (Entered STN: 04 Nov 2004, RN 774608-41-2 CA)- STN: 13 Jul 2009, RN 1162257-08-0 CA); (Entered STN: 12 Nov 2012, RN 1403679-84-4 (CA INDEX NAME). * |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2012143248A1 (en) | 2012-10-26 |
| US9283224B2 (en) | 2016-03-15 |
| BR112013026137B1 (pt) | 2020-12-01 |
| CN103502241B (zh) | 2016-03-23 |
| RU2013151174A (ru) | 2015-05-27 |
| CN103502241A (zh) | 2014-01-08 |
| BR112013026137A8 (pt) | 2018-01-30 |
| ES2616458T3 (es) | 2017-06-13 |
| US20140155421A1 (en) | 2014-06-05 |
| JP2014516360A (ja) | 2014-07-10 |
| EP2699564B1 (en) | 2016-12-14 |
| EP2699564A1 (en) | 2014-02-26 |
| HK1187905A1 (zh) | 2014-04-17 |
| JP5970537B2 (ja) | 2016-08-17 |
| BR112013026137A2 (pt) | 2017-10-24 |
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