ES2649156T3 - Compuestos bicíclicos de carboxamida aromática útiles como inhibidores de quinasas Pim - Google Patents
Compuestos bicíclicos de carboxamida aromática útiles como inhibidores de quinasas Pim Download PDFInfo
- Publication number
- ES2649156T3 ES2649156T3 ES14702167T ES14702167T ES2649156T3 ES 2649156 T3 ES2649156 T3 ES 2649156T3 ES 14702167 T ES14702167 T ES 14702167T ES 14702167 T ES14702167 T ES 14702167T ES 2649156 T3 ES2649156 T3 ES 2649156T3
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- Spain
- Prior art keywords
- alkyl
- nrc3rd3
- membered
- independently selected
- cycloalkyl
- 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.)
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- -1 Bicyclic aromatic carboxamide compounds Chemical class 0.000 title 1
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 46
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 20
- 125000001424 substituent group Chemical group 0.000 abstract 20
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 19
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 17
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 17
- 229910052736 halogen Inorganic materials 0.000 abstract 15
- 150000002367 halogens Chemical class 0.000 abstract 15
- 125000005843 halogen group Chemical group 0.000 abstract 12
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 12
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 11
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 abstract 7
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 6
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 abstract 6
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 6
- 125000006163 5-membered heteroaryl group Chemical group 0.000 abstract 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 6
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 5
- 101100310926 Caenorhabditis elegans sra-3 gene Proteins 0.000 abstract 4
- 101100310920 Caenorhabditis elegans sra-2 gene Proteins 0.000 abstract 3
- 125000004432 carbon atom Chemical group C* 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- 101100310927 Caenorhabditis elegans sra-4 gene Proteins 0.000 abstract 2
- 101100310928 Caenorhabditis elegans sra-6 gene Proteins 0.000 abstract 2
- 102100038417 Cytoplasmic FMR1-interacting protein 1 Human genes 0.000 abstract 2
- 101710181791 Cytoplasmic FMR1-interacting protein 1 Proteins 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- CZWUESRDTYLNDE-UHFFFAOYSA-N (2z)-2-[(2e,4e,6e)-7-[1-(5-carboxypentyl)-3,3-dimethyl-5-sulfoindol-1-ium-2-yl]hepta-2,4,6-trienylidene]-1-ethyl-3,3-dimethylindole-5-sulfonate Chemical compound CC1(C)C2=CC(S([O-])(=O)=O)=CC=C2N(CC)\C1=C/C=C/C=C/C=C/C1=[N+](CCCCCC(O)=O)C2=CC=C(S(O)(=O)=O)C=C2C1(C)C CZWUESRDTYLNDE-UHFFFAOYSA-N 0.000 abstract 1
- 125000006568 (C4-C7) heterocycloalkyl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- 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
-
- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- 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
- 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
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Dermatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Urology & Nephrology (AREA)
- Neurology (AREA)
- Vascular Medicine (AREA)
- Pain & Pain Management (AREA)
- Transplantation (AREA)
- Obesity (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361752249P | 2013-01-14 | 2013-01-14 | |
| US201361791275P | 2013-03-15 | 2013-03-15 | |
| PCT/US2014/011487 WO2014110574A1 (en) | 2013-01-14 | 2014-01-14 | Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2649156T3 true ES2649156T3 (es) | 2018-01-10 |
Family
ID=50030545
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES14702167T Active ES2649156T3 (es) | 2013-01-14 | 2014-01-14 | Compuestos bicíclicos de carboxamida aromática útiles como inhibidores de quinasas Pim |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US9278950B2 (enExample) |
| EP (1) | EP2943485B1 (enExample) |
| JP (1) | JP6437452B2 (enExample) |
| CA (1) | CA2897200C (enExample) |
| ES (1) | ES2649156T3 (enExample) |
| WO (1) | WO2014110574A1 (enExample) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9453003B2 (en) * | 2011-08-11 | 2016-09-27 | Jikai Biosciences, Inc. | Pyrimidine derivatives as PIM kinase inhibitors and preparation methods and use in medicinal manufacture thereof |
| US9458151B2 (en) * | 2011-08-11 | 2016-10-04 | Jikai Biosciences, Inc. | Isothiazole derivatives as PIM kinase inhibitors and preparation methods and use in medicinal manufacture thereof |
| JP6437452B2 (ja) | 2013-01-14 | 2018-12-12 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｐｉｍキナーゼ阻害剤として有用な二環式芳香族カルボキサミド化合物 |
| ME03780B (me) | 2013-01-15 | 2021-04-20 | Incyte Holdings Corp | Jedinjenja tiazolkarboksamida i piridinkarboksamida korisna kao inhibitori pim kinaze |
| EA201690458A1 (ru) | 2013-08-23 | 2016-07-29 | Инсайт Корпорейшн | Фуро- и тиенопиридинкарбоксамиды, используемые в качестве ингибиторов pim-киназы |
| US9822124B2 (en) | 2014-07-14 | 2017-11-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| WO2016161248A1 (en) * | 2015-04-02 | 2016-10-06 | Tolero Pharmaceuticals, Inc. | Targeting pim kinases in combination with btk inhibition |
| WO2016196244A1 (en) | 2015-05-29 | 2016-12-08 | Incyte Corporation | Pyridineamine compounds useful as pim kinase inhibitors |
| AR105967A1 (es) | 2015-09-09 | 2017-11-29 | Incyte Corp | Sales de un inhibidor de pim quinasa |
| WO2017059251A1 (en) * | 2015-10-02 | 2017-04-06 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| MX376974B (es) * | 2016-02-19 | 2025-03-07 | Phoenix Molecular Designs | Derivados de carboxamida útiles como inhibidores de rsk. |
| CN106336371A (zh) * | 2016-08-16 | 2017-01-18 | 成都百事兴科技实业有限公司 | 叔丁氧羰基‑l‑焦谷氨酸甲酯的合成方法 |
| WO2018083085A1 (en) * | 2016-11-02 | 2018-05-11 | F. Hoffmann-La Roche Ag | PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS |
| WO2019090205A1 (en) | 2017-11-06 | 2019-05-09 | Snap Bio, Inc. | Pim kinase inhibitor compositions, methods, and uses thereof |
| WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| CU24621B1 (es) | 2017-12-13 | 2022-09-08 | Lupin Ltd | Componentes heterocíclicos bicíclicos sustituidos como inhibidores de prmt5 |
| TW202448431A (zh) * | 2023-04-27 | 2024-12-16 | 南韓商大熊製藥股份有限公司 | 作為DNA聚合酶θ抑制劑以治療及預防癌症的新穎雜環化合物及包含其之醫藥組成物 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4188078B2 (ja) | 2000-06-28 | 2008-11-26 | スミスクライン ビーチャム ピー エル シー | 湿式粉砕法 |
| AU2002246864A1 (en) | 2000-12-27 | 2002-07-24 | The Trustees Of Columbia University In The City Of New York | Pim kinase-related methods |
| DE10123055A1 (de) | 2001-05-11 | 2003-03-20 | Gruenenthal Gmbh | Screeningverfahren mit PIM1-Kinase oder PIM3-Kinase |
| DE10226702A1 (de) | 2002-06-14 | 2004-09-09 | Grünenthal GmbH | Antisense Oligonukleotide gegen PIM1 |
| WO2006078228A1 (en) | 2002-09-16 | 2006-07-27 | Plexxikon, Inc. | Methods for the design of molecular scaffolds and ligands |
| AU2003272548A1 (en) | 2002-09-16 | 2004-04-30 | Plexxikon, Inc. | Crystal structure of pim-1 kinase |
| WO2004090106A2 (en) | 2003-04-04 | 2004-10-21 | Vertex Pharmaceuticals Incorporated | Crystal structures of human pim-1 kinase protein complexes and binding pockets thereof, and uses thereof in drug design |
| WO2005028624A2 (en) | 2003-09-15 | 2005-03-31 | Plexxikon, Inc. | Molecular scaffolds for kinase ligand development |
| WO2005033310A1 (de) | 2003-10-01 | 2005-04-14 | Grünenthal GmbH | Pim-1-spezifische dsrna-verbindungen |
| WO2006006569A1 (ja) | 2004-07-12 | 2006-01-19 | Nihon Nohyaku Co., Ltd. | フェニルピリジン類又はその塩類、これらを有効成分とする除草剤及びその使用方法 |
| BRPI0519424B8 (pt) | 2004-12-28 | 2021-05-25 | Athenex Inc | compostos, composição e uso dos ditos compostos para a preparação de um medicamento para prevenção ou tratamento de um distúrbio de proliferação celular ou infecção microbiana |
| UA95244C2 (ru) | 2005-06-22 | 2011-07-25 | Плексикон, Инк. | Соединения и способ модулирования активности киназ, и показания для их применения |
| WO2007011760A2 (en) | 2005-07-15 | 2007-01-25 | Kalypsys, Inc. | Inhibitors of mitotic kinesin |
| US7776865B2 (en) | 2005-10-06 | 2010-08-17 | Schering Corporation | Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors |
| JP5238506B2 (ja) | 2005-10-06 | 2013-07-17 | エグゼリクシス， インコーポレイテッド | Ｐｉｍ−１および／またはｐｉｍ−３のピリドピリミジノンインヒビター |
| JP5376950B2 (ja) | 2005-10-21 | 2013-12-25 | エクセリクシス， インク． | カゼインキナーゼｉｉ（ｃｋ２）モジュレーターとしてのピリミジオン類 |
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-
2014
- 2014-01-14 JP JP2015552897A patent/JP6437452B2/ja active Active
- 2014-01-14 WO PCT/US2014/011487 patent/WO2014110574A1/en not_active Ceased
- 2014-01-14 EP EP14702167.9A patent/EP2943485B1/en active Active
- 2014-01-14 ES ES14702167T patent/ES2649156T3/es active Active
- 2014-01-14 CA CA2897200A patent/CA2897200C/en active Active
- 2014-01-14 US US14/155,134 patent/US9278950B2/en active Active
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2016
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| US9278950B2 (en) | 2016-03-08 |
| EP2943485B1 (en) | 2017-09-20 |
| WO2014110574A1 (en) | 2014-07-17 |
| JP6437452B2 (ja) | 2018-12-12 |
| US20140200216A1 (en) | 2014-07-17 |
| JP2016505021A (ja) | 2016-02-18 |
| HK1216316A1 (en) | 2016-11-11 |
| EP2943485A1 (en) | 2015-11-18 |
| US20160137626A1 (en) | 2016-05-19 |
| US9676750B2 (en) | 2017-06-13 |
| CA2897200A1 (en) | 2014-07-17 |
| CA2897200C (en) | 2021-07-06 |
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