EA201101497A1 - Имидазопираны для применения в качестве ингибиторов киназ - Google Patents
Имидазопираны для применения в качестве ингибиторов киназInfo
- Publication number
- EA201101497A1 EA201101497A1 EA201101497A EA201101497A EA201101497A1 EA 201101497 A1 EA201101497 A1 EA 201101497A1 EA 201101497 A EA201101497 A EA 201101497A EA 201101497 A EA201101497 A EA 201101497A EA 201101497 A1 EA201101497 A1 EA 201101497A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- imidazopirana
- treatment
- kinaz
- inhibitors
- kinaz inhibitors
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 abstract 1
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 abstract 1
- 150000001408 amides Chemical class 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 150000002632 lipids Chemical class 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
- 102000004169 proteins and genes Human genes 0.000 abstract 1
- 108090000623 proteins and genes Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
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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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- 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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- 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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- A—HUMAN NECESSITIES
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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)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
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- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
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- Engineering & Computer Science (AREA)
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- Urology & Nephrology (AREA)
- Obesity (AREA)
- Molecular Biology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
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- Epidemiology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Hospice & Palliative Care (AREA)
- Transplantation (AREA)
- Emergency Medicine (AREA)
- Pain & Pain Management (AREA)
Abstract
Описываются соединения формулы Iгде R, R, R, Rи Rимеют значения, указанные в описании, и их фармацевтически приемлемые сложные эфиры, амиды, сольваты или соли, применимые при лечении заболеваний, при которых желательно или требуется ингибирование протеин- или липидкиназы (например, PI3-K и/или mTOR), в частности, при лечении рака или пролиферативного заболевания.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
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 |
---|---|
EA201101497A1 true EA201101497A1 (ru) | 2012-04-30 |
EA022629B1 EA022629B1 (ru) | 2016-02-29 |
Family
ID=40940522
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201101497A EA022629B1 (ru) | 2009-04-16 | 2010-04-16 | Имидазопираны для применения в качестве ингибиторов киназ |
Country Status (17)
Country | Link |
---|---|
US (1) | US8778935B2 (ru) |
EP (1) | EP2419429B1 (ru) |
JP (1) | JP5805623B2 (ru) |
KR (2) | KR101792837B1 (ru) |
CN (1) | CN102428087B (ru) |
AU (1) | AU2010238361B2 (ru) |
BR (1) | BRPI1014572B8 (ru) |
CA (1) | CA2756759C (ru) |
DK (1) | DK2419429T3 (ru) |
EA (1) | EA022629B1 (ru) |
ES (1) | ES2475091T3 (ru) |
IL (1) | IL215297A (ru) |
MX (1) | MX2011010915A (ru) |
NZ (1) | NZ596185A (ru) |
SG (1) | SG175195A1 (ru) |
WO (1) | WO2010119264A1 (ru) |
ZA (1) | ZA201107717B (ru) |
Families Citing this family (71)
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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. |
AU2010311511B2 (en) | 2009-10-30 | 2014-07-17 | Janssen Pharmaceutica Nv | Imidazo[1,2-b]pyridazine derivatives and their use as PDE10 inhibitors |
CA2787714C (en) | 2010-01-22 | 2019-04-09 | Joaquin Pastor Fernandez | 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 |
SG184987A1 (en) | 2010-04-22 | 2012-11-29 | Vertex Pharma | Process of producing cycloalkylcarboxamido-indole compounds |
WO2011141713A1 (en) | 2010-05-13 | 2011-11-17 | 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 |
CN103619846B (zh) | 2011-06-27 | 2016-08-17 | 詹森药业有限公司 | 1-芳基-4-甲基-[1,2,4]三唑[4,3-a]喹喔啉衍生物 |
PT2841075T (pt) | 2012-04-26 | 2020-06-25 | Massachusetts Gen Hospital | Agentes e métodos para tratamento e prevenção de queratose seborreica |
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 |
RU2657540C2 (ru) | 2012-06-26 | 2018-06-14 | Янссен Фармацевтика Нв | Комбинации, содержащие ингибиторы pde 2, такие как 1-арил-4-метил-[1,2,4]триазоло[4,3-а]хиноксалиновые соединения, и ингибиторы pde 10, для применения в лечении неврологических или метаболических расстройств |
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 |
EP3105219B9 (en) | 2014-02-13 | 2018-10-03 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
WO2015123437A1 (en) | 2014-02-13 | 2015-08-20 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
WO2015123465A1 (en) | 2014-02-13 | 2015-08-20 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
SMT201900620T1 (it) | 2014-02-13 | 2020-01-14 | Incyte Corp | Ciclopropilammine come inibitori di lsd1 |
PL3131582T3 (pl) | 2014-04-15 | 2018-10-31 | Vertex Pharmaceuticals Incorporated | Kompozycje farmaceutyczne do leczenia chorób, w których pośredniczy mukowiscydozowy przezbłonowy regulator przewodnictwa |
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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 |
US9758523B2 (en) | 2014-07-10 | 2017-09-12 | Incyte Corporation | Triazolopyridines and triazolopyrazines as LSD1 inhibitors |
US9695167B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines 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 |
UA122688C2 (uk) | 2015-04-03 | 2020-12-28 | Інсайт Корпорейшн | Гетероциклічні сполуки як інгібітори lsd1 |
PH12018500317B1 (en) | 2015-08-12 | 2023-01-11 | Incyte Holdings Corp | Salts of an lsd1 inhibitor |
US20170107216A1 (en) | 2015-10-19 | 2017-04-20 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
DK3377488T3 (da) | 2015-11-19 | 2022-10-03 | Incyte Corp | Heterocykliske forbindelser som immunomodulatorer |
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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 |
PL3442977T3 (pl) * | 2016-04-15 | 2024-03-04 | Blueprint Medicines Corporation | Inhibitory kinazy podobnej do receptora aktywiny |
TWI833686B (zh) | 2016-04-22 | 2024-03-01 | 美商英塞特公司 | Lsd1 抑制劑之調配物 |
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BRPI1014572A2 (pt) | 2016-04-26 |
EA022629B1 (ru) | 2016-02-29 |
CA2756759A1 (en) | 2010-10-21 |
CN102428087B (zh) | 2015-06-17 |
EP2419429A1 (en) | 2012-02-22 |
BRPI1014572B1 (pt) | 2021-07-13 |
JP5805623B2 (ja) | 2015-11-04 |
CN102428087A (zh) | 2012-04-25 |
MX2011010915A (es) | 2012-01-27 |
KR20170116250A (ko) | 2017-10-18 |
EP2419429B1 (en) | 2014-03-26 |
JP2012524053A (ja) | 2012-10-11 |
KR20120034613A (ko) | 2012-04-12 |
BRPI1014572B8 (pt) | 2022-07-19 |
WO2010119264A1 (en) | 2010-10-21 |
IL215297A (en) | 2016-08-31 |
ZA201107717B (en) | 2015-08-26 |
KR101792837B1 (ko) | 2017-11-02 |
HK1167142A1 (en) | 2012-11-23 |
CA2756759C (en) | 2017-11-07 |
IL215297A0 (en) | 2011-12-29 |
AU2010238361B2 (en) | 2015-08-06 |
SG175195A1 (en) | 2011-11-28 |
US8778935B2 (en) | 2014-07-15 |
NZ596185A (en) | 2013-01-25 |
AU2010238361A1 (en) | 2011-11-10 |
ES2475091T3 (es) | 2014-07-10 |
DK2419429T3 (da) | 2014-06-23 |
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