EA033084B1 - Бигетероарильные соединения и их применения - Google Patents
Бигетероарильные соединения и их примененияInfo
- Publication number
- EA033084B1 EA033084B1 EA201792471A EA201792471A EA033084B1 EA 033084 B1 EA033084 B1 EA 033084B1 EA 201792471 A EA201792471 A EA 201792471A EA 201792471 A EA201792471 A EA 201792471A EA 033084 B1 EA033084 B1 EA 033084B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- compounds
- biheteroaryl compounds
- biheteroaryl
- formula
- diseases
- Prior art date
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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- 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
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- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
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- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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- C07D451/14—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantane; Cyclic acetals thereof
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Abstract
В настоящем изобретении предложены соединения формулы I-I и их воплощения и соли для лечения заболеваний (например, нейродегенеративных заболеваний). Все переменные R, R, R, X, X, A и Cy в формуле I-I имеют значение, определенное в данном документе.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US201361817966P | 2013-05-01 | 2013-05-01 |
Publications (2)
Publication Number | Publication Date |
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EA201792471A1 EA201792471A1 (ru) | 2018-04-30 |
EA033084B1 true EA033084B1 (ru) | 2019-08-30 |
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Family Applications (3)
Application Number | Title | Priority Date | Filing Date |
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EA201991064A EA038235B1 (ru) | 2013-05-01 | 2014-04-30 | Бигетероарильные соединения и их применения |
EA201792471A EA033084B1 (ru) | 2013-05-01 | 2014-04-30 | Бигетероарильные соединения и их применения |
EA201592060A EA029568B8 (ru) | 2013-05-01 | 2014-04-30 | Бигетероарильные соединения и их применения |
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Families Citing this family (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2844652B1 (en) * | 2012-05-03 | 2019-03-13 | Genentech, Inc. | Pyrazole aminopyrimidine derivatives as lrrk2 modulators |
WO2014111496A1 (en) * | 2013-01-18 | 2014-07-24 | F. Hoffmann-La Roche Ag | 3-substituted pyrazoles and use as dlk inhibitors |
MY182082A (en) | 2013-05-01 | 2021-01-18 | Hoffmann La Roche | Biheteroaryl compounds and uses thereof |
CA2907912A1 (en) * | 2013-05-01 | 2014-11-06 | F. Hoffmann-La Roche Ag | C-linked heterocycloalkyl substituted pyrimidines and their uses |
MX2016008110A (es) * | 2013-12-20 | 2016-08-19 | Hoffmann La Roche | Derivados de pirazol como inhibidores de la cinasa de cremallera de leucina dual (dlk) y usos de los mismos. |
CN104926716A (zh) * | 2015-06-10 | 2015-09-23 | 哈尔滨工业大学 | 吡啶衍生物2,6-二[(6-甲氧基吡啶-2-基)甲基]吡啶及其合成方法 |
MX2019002444A (es) * | 2016-08-29 | 2019-09-02 | Univ Texas | Inhibidores de cinasa de cremallera de leucina dual (dlk) para el tratamiento de enfermedades. |
CN110191878B (zh) | 2016-12-08 | 2023-05-26 | 德州大学系统董事会 | 疾病治疗用双亮氨酸拉链(dlk)激酶的二环[1.1.1]戊烷抑制剂 |
CN110914271A (zh) | 2017-07-14 | 2020-03-24 | 豪夫迈·罗氏有限公司 | 二环酮化合物及其使用方法 |
AU2018348930A1 (en) | 2017-10-11 | 2020-03-26 | F. Hoffmann-La Roche Ag | Bicyclic compounds for use as RIP 1 kinase inhibitors |
TWI797176B (zh) * | 2017-10-17 | 2023-04-01 | 西班牙商帕羅製藥有限公司 | 4-胺基嘧啶化合物之合成 |
EP3704097B1 (en) | 2017-10-31 | 2023-10-25 | F. Hoffmann-La Roche AG | Bicyclic sulfones and sulfoxides and methods of use thereof |
CN112074519A (zh) | 2018-04-20 | 2020-12-11 | 豪夫迈·罗氏有限公司 | 作为rip1激酶抑制剂用于治疗e.g.肠易激综合征(ibs)的n-[4-氧代-2,3-二氢-1,5-苯并氧氮杂-3-基]-5,6-二氢-4h-吡咯并[1,2-b]吡唑-2-甲酰胺衍生物和有关化合物 |
EP3908586B1 (en) | 2019-01-11 | 2022-12-21 | F. Hoffmann-La Roche AG | Bicyclic pyrrolotriazolr ketone compounds and methods of use thereof |
CA3128416A1 (en) * | 2019-01-31 | 2020-08-06 | The National Institutes of Pharmaceutical R&D Co., Ltd. | Aromatic ring or heteroaromatic ring compounds, preparation method therefor and medical use thereof |
US11560366B2 (en) | 2019-10-21 | 2023-01-24 | Board Of Regents, The University Of Texas System | Bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (DLK) kinase for the treatment of disease |
MX2023003759A (es) * | 2020-10-02 | 2023-04-24 | Genentech Inc | Proceso para la preparacion de compuestos de biheteroarilo y formas cristalinas de estos. |
CA3229861A1 (en) * | 2021-09-01 | 2023-03-09 | John F. BROGNARD | Mixed lineage kinase inhibitors and methods of use |
WO2023067550A1 (en) * | 2021-10-20 | 2023-04-27 | Yousef Najajreh | Allosteric inhibitor compounds for overcoming cancer resistance |
Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2007084786A1 (en) * | 2006-01-20 | 2007-07-26 | Novartis Ag | Pyrimidine derivatives used as pi-3 kinase inhibitors |
WO2008098058A1 (en) * | 2007-02-06 | 2008-08-14 | Novartis Ag | Pi 3-kinase inhibitors and methods of their use |
WO2009066084A1 (en) * | 2007-11-21 | 2009-05-28 | F. Hoffmann-La Roche Ag | 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors |
WO2010049481A1 (en) * | 2008-10-31 | 2010-05-06 | Novartis Ag | Combination of a phosphatidylinositol-3-kinase (pi3k) inhibitor and a mtor inhibitor |
WO2011114275A1 (en) * | 2010-03-15 | 2011-09-22 | University Of Basel | Spirocyclic compounds and their use as therapeutic agents and diagnostic probes |
WO2012122383A2 (en) * | 2011-03-09 | 2012-09-13 | Avila Therapeutics, Inc. | Pi3 kinase inhibitors and uses thereof |
Family Cites Families (29)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3773919A (en) | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
US4485045A (en) | 1981-07-06 | 1984-11-27 | Research Corporation | Synthetic phosphatidyl cholines useful in forming liposomes |
EP0102324A3 (de) | 1982-07-29 | 1984-11-07 | Ciba-Geigy Ag | Lipide und Tenside in wässriger Phase |
US4544545A (en) | 1983-06-20 | 1985-10-01 | Trustees University Of Massachusetts | Liposomes containing modified cholesterol for organ targeting |
HUT35524A (en) | 1983-08-02 | 1985-07-29 | Hoechst Ag | Process for preparing pharmaceutical compositions containing regulatory /regulative/ peptides providing for the retarded release of the active substance |
US5004697A (en) | 1987-08-17 | 1991-04-02 | Univ. Of Ca | Cationized antibodies for delivery through the blood-brain barrier |
US5112596A (en) | 1990-04-23 | 1992-05-12 | Alkermes, Inc. | Method for increasing blood-brain barrier permeability by administering a bradykinin agonist of blood-brain barrier permeability |
US5268164A (en) | 1990-04-23 | 1993-12-07 | Alkermes, Inc. | Increasing blood-brain barrier permeability with permeabilizer peptides |
WO1994002178A1 (en) | 1992-07-27 | 1994-02-03 | The Government Of The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services | Targeting of liposomes to the blood-brain barrier |
US6514221B2 (en) | 2000-07-27 | 2003-02-04 | Brigham And Women's Hospital, Inc. | Blood-brain barrier opening |
AU2001286930A1 (en) | 2000-08-30 | 2002-03-13 | The Board Of Trustees Of The Leland Stanford Junior University | Glucocorticoid blocking agents for increasing blood-brain barrier permeability |
US7034036B2 (en) | 2000-10-30 | 2006-04-25 | Pain Therapeutics, Inc. | Inhibitors of ABC drug transporters at the blood-brain barrier |
DE10121982B4 (de) | 2001-05-05 | 2008-01-24 | Lts Lohmann Therapie-Systeme Ag | Nanopartikel aus Protein mit gekoppeltem Apolipoprotein E zur Überwindung der Blut-Hirn-Schranke und Verfahren zu ihrer Herstellung |
CA2450073C (en) | 2001-07-25 | 2017-08-29 | Biomarin Pharmaceutical Inc. | Compositions and methods for modulating blood-brain barrier transport |
US20030162695A1 (en) | 2002-02-27 | 2003-08-28 | Schatzberg Alan F. | Glucocorticoid blocking agents for increasing blood-brain barrier permeability |
JP4790266B2 (ja) | 2002-09-30 | 2011-10-12 | バイエル・シエリング・フアーマ・アクチエンゲゼルシヤフト | 縮合アゾールピリミジン誘導体 |
KR101111477B1 (ko) | 2002-12-03 | 2012-02-23 | 블랜체트 록펠러 뉴로사이언시즈 인스티튜트 | 치료제와 연결된 콜레스테롤을 포함하는 접합체 |
WO2005025511A2 (en) | 2003-09-10 | 2005-03-24 | Cedars-Sinai Medical Center | Potassium channel mediated delivery of agents through the blood-brain barrier |
GB0508471D0 (en) | 2005-04-26 | 2005-06-01 | Celltech R&D Ltd | Therapeutic agents |
WO2008064244A2 (en) | 2006-11-20 | 2008-05-29 | The Trustees Of Columbia University In The City Of New York | Phosphoinositide modulation for the treatment of neurodegenerative diseases |
AR067585A1 (es) | 2007-07-19 | 2009-10-14 | Schering Corp | Compuestos heterociclicos de amidas como inhibidores de la proteincinasa |
US20100056609A1 (en) | 2008-08-26 | 2010-03-04 | Washington University | Methods and compositions for inhibition of axonal degeneration by modulation of the dlk/jnk pathway |
GB2465405A (en) * | 2008-11-10 | 2010-05-19 | Univ Basel | Triazine, pyrimidine and pyridine analogues and their use in therapy |
MX339584B (es) | 2009-09-09 | 2016-06-01 | Avila Therapeutics Inc | Inhibidores de pi3 cinasa y usos de los mismos. |
US20120328609A1 (en) | 2009-10-22 | 2012-12-27 | Genentech, Inc. | Modulation of Axon Degeneration |
CN103153994B (zh) | 2010-05-24 | 2016-02-10 | 罗切斯特大学 | 双环杂芳基激酶抑制剂及使用方法 |
MY182082A (en) * | 2013-05-01 | 2021-01-18 | Hoffmann La Roche | Biheteroaryl compounds and uses thereof |
CN103483345B (zh) | 2013-09-25 | 2016-07-06 | 中山大学 | Pi3k激酶抑制剂、包含其的药物组合物及其应用 |
JP5920747B1 (ja) | 2015-04-07 | 2016-05-18 | エイピーエス.エスエイ | アプリケーションプログラムおよびカード |
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Patent Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2007084786A1 (en) * | 2006-01-20 | 2007-07-26 | Novartis Ag | Pyrimidine derivatives used as pi-3 kinase inhibitors |
WO2008098058A1 (en) * | 2007-02-06 | 2008-08-14 | Novartis Ag | Pi 3-kinase inhibitors and methods of their use |
WO2009066084A1 (en) * | 2007-11-21 | 2009-05-28 | F. Hoffmann-La Roche Ag | 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors |
WO2010049481A1 (en) * | 2008-10-31 | 2010-05-06 | Novartis Ag | Combination of a phosphatidylinositol-3-kinase (pi3k) inhibitor and a mtor inhibitor |
WO2011114275A1 (en) * | 2010-03-15 | 2011-09-22 | University Of Basel | Spirocyclic compounds and their use as therapeutic agents and diagnostic probes |
WO2012122383A2 (en) * | 2011-03-09 | 2012-09-13 | Avila Therapeutics, Inc. | Pi3 kinase inhibitors and uses thereof |
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