CA2756759C - Imidazopyrazines for use as kinase inhibitors - Google Patents
Imidazopyrazines for use as kinase inhibitors Download PDFInfo
- Publication number
- CA2756759C CA2756759C CA2756759A CA2756759A CA2756759C CA 2756759 C CA2756759 C CA 2756759C CA 2756759 A CA2756759 A CA 2756759A CA 2756759 A CA2756759 A CA 2756759A CA 2756759 C CA2756759 C CA 2756759C
- Authority
- CA
- Canada
- Prior art keywords
- morpholin
- imidazo
- pyrazine
- methyl
- pyrazin
- 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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- 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
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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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
- C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
- C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
- C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
- C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
- C07D243/20—Nitrogen atoms
-
- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Oncology (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Obesity (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Molecular Biology (AREA)
- Endocrinology (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Emergency Medicine (AREA)
- Pain & Pain Management (AREA)
- Surgery (AREA)
- AIDS & HIV (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09380079.5 | 2009-04-16 | ||
| EP09380079 | 2009-04-16 | ||
| PCT/GB2010/000773 WO2010119264A1 (en) | 2009-04-16 | 2010-04-16 | Imidazopyrazines for use as kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2756759A1 CA2756759A1 (en) | 2010-10-21 |
| CA2756759C true CA2756759C (en) | 2017-11-07 |
Family
ID=40940522
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2756759A Active CA2756759C (en) | 2009-04-16 | 2010-04-16 | Imidazopyrazines for use as kinase inhibitors |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US8778935B2 (https=) |
| EP (1) | EP2419429B1 (https=) |
| JP (1) | JP5805623B2 (https=) |
| KR (2) | KR101792837B1 (https=) |
| CN (1) | CN102428087B (https=) |
| AU (1) | AU2010238361B2 (https=) |
| BR (1) | BRPI1014572B8 (https=) |
| CA (1) | CA2756759C (https=) |
| DK (1) | DK2419429T3 (https=) |
| EA (1) | EA022629B1 (https=) |
| ES (1) | ES2475091T3 (https=) |
| IL (1) | IL215297A (https=) |
| MX (1) | MX2011010915A (https=) |
| NZ (1) | NZ596185A (https=) |
| SG (1) | SG175195A1 (https=) |
| WO (1) | WO2010119264A1 (https=) |
| ZA (1) | ZA201107717B (https=) |
Families Citing this family (74)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8563573B2 (en) | 2007-11-02 | 2013-10-22 | Vertex Pharmaceuticals Incorporated | Azaindole derivatives as CFTR modulators |
| MX2011009796A (es) | 2009-03-20 | 2011-12-14 | Amgen Inc | Inhibidores de la cinasa pi3. |
| PH12012500778A1 (en) | 2009-10-30 | 2012-11-26 | Janssen Pharmaceutica Nv | IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS |
| EP2526102B1 (en) * | 2010-01-22 | 2017-03-08 | Fundación Centro Nacional de Investigaciones Oncológicas Carlos III | Inhibitors of PI3 kinase |
| AR080754A1 (es) | 2010-03-09 | 2012-05-09 | Janssen Pharmaceutica Nv | Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10 |
| TW201200518A (en) * | 2010-03-10 | 2012-01-01 | Kalypsys Inc | Heterocyclic inhibitors of histamine receptors for the treatment of disease |
| US8802868B2 (en) | 2010-03-25 | 2014-08-12 | Vertex Pharmaceuticals Incorporated | Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide |
| MX353408B (es) | 2010-04-22 | 2018-01-11 | Vertex Pharma | Proceso para producir compuestos de cicloalquilcarboxamido-indol. |
| US20130131057A1 (en) | 2010-05-13 | 2013-05-23 | Centro Nacional De Investigaciones Oncologicas (Cnio | New bicyclic compounds as pi3-k and mtor inhibitors |
| EP2444084A1 (en) | 2010-10-21 | 2012-04-25 | Centro Nacional de Investigaciones Oncológicas (CNIO) | Use of PI3K inibitors for the treatment of obesity |
| WO2012052745A1 (en) | 2010-10-21 | 2012-04-26 | Centro Nacional De Investigaciones Oncológicas (Cnio) | Combinations of pi3k inhibitors with a second anti -tumor agent |
| TWI617559B (zh) | 2010-12-22 | 2018-03-11 | 江蘇恆瑞醫藥股份有限公司 | 2-芳基咪唑并[1,2-b]嗒.2-苯基咪唑并[1,2-a]吡啶,和2-苯基咪唑并[1,2-a]吡衍生物 |
| EP2524918A1 (en) | 2011-05-19 | 2012-11-21 | Centro Nacional de Investigaciones Oncológicas (CNIO) | Imidazopyrazines derivates as kinase inhibitors |
| BR112013033375B1 (pt) | 2011-06-27 | 2022-05-10 | Janssen Pharmaceutica N.V | Derivados de 1-aril-4-metil-[1,2,4]triazolo[4,3-a]quinoxa-lina, seu uso, composição farmacêutica que os compreende, processo de preparação dos mesmos, solução estéril e composto intermediário |
| DK2841075T3 (da) | 2012-04-26 | 2020-06-22 | Massachusetts Gen Hospital | Midler og fremgangsmåder til behandling og forebyggelse af seboroisk keratose |
| CN103450204B (zh) * | 2012-05-31 | 2016-08-17 | 中国科学院上海药物研究所 | 吡咯[2,1-f][1,2,4]并三嗪类化合物,其制备方法及用途 |
| CN102675323B (zh) * | 2012-06-01 | 2014-04-09 | 南京药石药物研发有限公司 | 吡咯并[2,1-f][1,2,4]三嗪衍生物及其抗肿瘤用途 |
| HK1206250A1 (en) | 2012-06-26 | 2016-01-08 | Janssen Pharmaceutica Nv | Combinations comprising pde 2 inhibitors such as 1-aryl-4-methyl-[1,2,4] triazolo [4,3-a] quinoxaline compounds and ped 10 inhibitors for use in the treatment of neurological or metabolic disorders |
| WO2014009305A1 (en) | 2012-07-09 | 2014-01-16 | Janssen Pharmaceutica Nv | Inhibitors of phosphodiesterase 10 enzyme |
| US9145411B2 (en) | 2012-08-02 | 2015-09-29 | Asana Biosciences, Llc | Substituted amino-pyrimidine derivatives |
| WO2014186663A2 (en) * | 2013-05-17 | 2014-11-20 | The General Hospital Corporation | Methods for detecting and treating variants of seborrheic keratoses |
| MX373103B (es) | 2014-02-13 | 2020-04-17 | Incyte Holdings Corp | Ciclopropilaminas como inhibidores de desmetilasa específica de lisina 1 (lsd1). |
| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| EP3105219B9 (en) | 2014-02-13 | 2018-10-03 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| SI3105218T1 (sl) | 2014-02-13 | 2019-11-29 | Incyte Corp | Ciklopropilamini kot inhibitorji LSD1 |
| RU2744460C2 (ru) | 2014-04-15 | 2021-03-09 | Вертекс Фармасьютикалз Инкорпорейтед | Фармацевтические композиции для лечения заболеваний, опосредованных муковисцидозным трансмембранным регулятором проводимости |
| WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| TW201613925A (en) | 2014-07-10 | 2016-04-16 | Incyte Corp | Imidazopyrazines as LSD1 inhibitors |
| TWI687419B (zh) | 2014-07-10 | 2020-03-11 | 美商英塞特公司 | 作為lsd1抑制劑之咪唑并吡啶及咪唑并吡嗪 |
| WO2016007727A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| PL236355B1 (pl) * | 2015-04-02 | 2021-01-11 | Celon Pharma Spolka Akcyjna | Pochodne 7-(morfolin-4-ylo)pirazolo[1,5-α]pirymidyny jako inhibitory kinazy PI3 |
| EP3277689B1 (en) | 2015-04-03 | 2019-09-04 | Incyte Corporation | Heterocyclic compounds as lsd1 inhibitors |
| LT3334709T (lt) | 2015-08-12 | 2025-03-10 | Incyte Holdings Corporation | Lsd1 inhibitoriaus druskos |
| EP3365340B1 (en) | 2015-10-19 | 2022-08-10 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| US20170145025A1 (en) | 2015-11-19 | 2017-05-25 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| ES2916874T3 (es) | 2015-12-17 | 2022-07-06 | Incyte Corp | Derivados de N-fenil-piridina-2-carboxamida y su uso como moduladores de la interacción proteína/proteína PD-1/PD-L1 |
| AU2016379372A1 (en) | 2015-12-22 | 2018-08-02 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| CN105622526A (zh) * | 2016-02-24 | 2016-06-01 | 湖北工业大学 | 一种2-氨基吡嗪衍生物的制备方法 |
| SG11201808907PA (en) * | 2016-04-15 | 2018-11-29 | Blueprint Medicines Corp | Inhibitors of activin receptor-like kinase |
| JP6999574B2 (ja) | 2016-04-22 | 2022-01-18 | インサイト・コーポレイション | Lsd1阻害剤の製剤 |
| ES2906460T3 (es) | 2016-05-06 | 2022-04-18 | Incyte Corp | Compuestos heterocíclicos como inmunomoduladores |
| ES2905980T3 (es) | 2016-05-26 | 2022-04-12 | Incyte Corp | Compuestos heterocíclicos como inmunomoduladores |
| BR112018076534A2 (pt) | 2016-06-20 | 2019-04-02 | Incyte Corporation | compostos heterocíclicos como imunomoduladores |
| MA45669A (fr) | 2016-07-14 | 2019-05-22 | Incyte Corp | Composés hétérocycliques utilisés comme immunomodulateurs |
| ES2941716T3 (es) | 2016-08-29 | 2023-05-25 | Incyte Corp | Compuestos heterocíclicos como inmunomoduladores |
| TW202233190A (zh) * | 2016-12-07 | 2022-09-01 | 英屬開曼群島商百濟神州有限公司 | 作為PI3Kδ抑制劑的咪唑並[1,5-A]吡衍生物 |
| ES2856248T3 (es) * | 2016-12-21 | 2021-09-27 | Acerta Pharma Bv | Inhibidores de imidazopirazina de la tirosina quinasa de Bruton |
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| EP2419429A1 (en) | 2012-02-22 |
| BRPI1014572B1 (pt) | 2021-07-13 |
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| CA2756759A1 (en) | 2010-10-21 |
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| SG175195A1 (en) | 2011-11-28 |
| KR101792837B1 (ko) | 2017-11-02 |
| ES2475091T3 (es) | 2014-07-10 |
| US20120083492A1 (en) | 2012-04-05 |
| IL215297A (en) | 2016-08-31 |
| HK1167142A1 (en) | 2012-11-23 |
| JP2012524053A (ja) | 2012-10-11 |
| KR20120034613A (ko) | 2012-04-12 |
| CN102428087B (zh) | 2015-06-17 |
| WO2010119264A1 (en) | 2010-10-21 |
| NZ596185A (en) | 2013-01-25 |
| EA022629B1 (ru) | 2016-02-29 |
| AU2010238361B2 (en) | 2015-08-06 |
| AU2010238361A1 (en) | 2011-11-10 |
| BRPI1014572A2 (pt) | 2016-04-26 |
| KR20170116250A (ko) | 2017-10-18 |
| IL215297A0 (en) | 2011-12-29 |
| DK2419429T3 (da) | 2014-06-23 |
| BRPI1014572B8 (pt) | 2022-07-19 |
| EA201101497A1 (ru) | 2012-04-30 |
| JP5805623B2 (ja) | 2015-11-04 |
| US8778935B2 (en) | 2014-07-15 |
| ZA201107717B (en) | 2015-08-26 |
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