EA201290324A1 - Киназные ингибиторы - Google Patents
Киназные ингибиторыInfo
- Publication number
- EA201290324A1 EA201290324A1 EA201290324A EA201290324A EA201290324A1 EA 201290324 A1 EA201290324 A1 EA 201290324A1 EA 201290324 A EA201290324 A EA 201290324A EA 201290324 A EA201290324 A EA 201290324A EA 201290324 A1 EA201290324 A1 EA 201290324A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- protein kinase
- provides
- diseases
- pyropyrimidine
- pyrazolopyrimidine
- Prior art date
Links
Classifications
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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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- 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
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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
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- C07D403/14—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 three or more hetero rings
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- 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
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- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
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- 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
- C07D487/08—Bridged systems
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- Health & Medical Sciences (AREA)
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- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
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Abstract
В изобретении заявлена новая группа протеинкиназных ингибиторов, производных пирропиримидина и пиразолопиримидина, и их фармацевтически приемлемые соли и пролекарства, которые применяют для лечения пролиферативных заболеваний и расстройств клеток, таких как рак, аутоиммунные заболевания, инфекции, сердечно-сосудистые заболевания и нейродегенеративные заболевания и расстройства. В данном изобретении представлены способы синтеза и введения соединений протеинкиназных ингибиторов. В изобретении также представлены фармацевтические композиции, содержащие по меньшей мере одно соединение протеинкиназного ингибитора вместе с фармацевтически приемлемым носителем, разбавителем или наполнителем. В изобретении также представлены промежуточные соединения, полученные во время синтеза производных пирропиримидина и пиразолопиримидина.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US26110009P | 2009-11-13 | 2009-11-13 | |
PCT/US2010/056583 WO2011060295A1 (en) | 2009-11-13 | 2010-11-12 | Kinase inhibitors |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201290324A1 true EA201290324A1 (ru) | 2012-12-28 |
EA024729B1 EA024729B1 (ru) | 2016-10-31 |
Family
ID=43992073
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201290324A EA024729B1 (ru) | 2009-11-13 | 2010-11-12 | Киназные ингибиторы |
Country Status (17)
Country | Link |
---|---|
US (1) | US8629132B2 (ru) |
EP (1) | EP2498607B1 (ru) |
JP (1) | JP5740409B2 (ru) |
KR (1) | KR101663637B1 (ru) |
CN (1) | CN102811619B (ru) |
BR (1) | BR112012011287B1 (ru) |
CA (1) | CA2780892C (ru) |
CL (1) | CL2012001221A1 (ru) |
EA (1) | EA024729B1 (ru) |
HK (1) | HK1179477A1 (ru) |
IL (1) | IL219726A (ru) |
MX (1) | MX2012005332A (ru) |
MY (1) | MY160820A (ru) |
NZ (1) | NZ599041A (ru) |
SG (1) | SG10201407453TA (ru) |
WO (1) | WO2011060295A1 (ru) |
ZA (1) | ZA201204246B (ru) |
Families Citing this family (99)
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EP2918588B1 (en) | 2010-05-20 | 2017-05-03 | Array Biopharma, Inc. | Macrocyclic compounds as TRK kinase inhibitors |
SI2576541T1 (sl) | 2010-06-04 | 2016-07-29 | F. Hoffmann-La Roche Ag | Aminopirimidinski derivati kot modulatorji lrrk2 |
KR101566091B1 (ko) | 2010-11-10 | 2015-11-04 | 에프. 호프만-라 로슈 아게 | Lrrk2 조절제로서 피라졸 아미노피리미딘 유도체 |
US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
WO2013054351A1 (en) * | 2011-08-08 | 2013-04-18 | Cadila Healthcare Limited | Heterocyclic compounds |
CN104024248A (zh) * | 2011-08-25 | 2014-09-03 | 霍夫曼-拉罗奇有限公司 | 丝氨酸/苏氨酸pak1抑制剂 |
US8815877B2 (en) | 2011-12-22 | 2014-08-26 | Genentech, Inc. | Serine/threonine kinase inhibitors |
EP2804861B1 (en) * | 2012-01-20 | 2018-02-28 | Genosco | Substituted pyrimidine compounds and their use as syk inhibitors |
US9096579B2 (en) * | 2012-04-20 | 2015-08-04 | Boehringer Ingelheim International Gmbh | Amino-indolyl-substituted imidazolyl-pyrimidines and their use as medicaments |
ES2646777T3 (es) * | 2012-05-15 | 2017-12-15 | Novartis Ag | Derivados de pirimidina, piridina y pirazina amida sustituidos con tiazol o imidazol y compuestos relacionados como inhibidores de ABL1, ABL2 y BCR-ABL1 para el tratamiento del cáncer, infecciones víricas específicas y trastornos específicos del CNS |
CN104379574B (zh) | 2012-05-15 | 2017-03-01 | 诺华股份有限公司 | 用于抑制abl1、abl2和bcr‑abl1的活性的苯甲酰胺衍生物 |
PT2861579T (pt) | 2012-05-15 | 2018-04-27 | Novartis Ag | Derivados de benzamida para inibir a atividade de abl1, abl2 e bcr-abl |
EP2861576B1 (en) | 2012-05-15 | 2018-01-10 | Novartis AG | Benzamide derivatives for inhibiting the activity of abl1, abl2 and bcr-abl1 |
ME03300B (me) | 2012-06-13 | 2019-07-20 | Incyte Holdings Corp | Supsтituisana triciklična jedinjenja као inhibiтori fgfr |
CN105732639A (zh) | 2012-06-29 | 2016-07-06 | 辉瑞大药厂 | 作为LRRK2抑制剂的4-(取代的氨基)-7H-吡咯并〔2,3-d〕嘧啶类 |
US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
WO2014110574A1 (en) | 2013-01-14 | 2014-07-17 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors |
ME03780B (me) | 2013-01-15 | 2021-04-20 | Incyte Holdings Corp | Jedinjenja tiazolkarboksamida i piridinkarboksamida korisna kao inhibitori pim kinaze |
WO2014134772A1 (en) * | 2013-03-04 | 2014-09-12 | Merck Sharp & Dohme Corp. | Compounds inhibiting leucine-rich repeat kinase enzyme activity |
ES2657451T3 (es) | 2013-04-19 | 2018-03-05 | Incyte Holdings Corporation | Heterocíclicos bicíclicos como inhibidores del FGFR |
CN103232394B (zh) * | 2013-05-14 | 2014-09-24 | 浙江医药高等专科学校 | 含吡唑类化合物、其制备方法和用途 |
CN103396400B (zh) * | 2013-07-16 | 2014-12-17 | 浙江医药高等专科学校 | 含吡唑酰胺类化合物、其制备方法和用途 |
CN103387568B (zh) * | 2013-07-16 | 2014-11-05 | 浙江医药高等专科学校 | 一类化合物、其制备方法和用途 |
CN103382198B (zh) * | 2013-07-16 | 2014-11-19 | 浙江医药高等专科学校 | 吡唑酰胺类化合物、其制备方法和用途 |
CN103382202B (zh) * | 2013-07-16 | 2014-11-26 | 浙江医药高等专科学校 | 含呋喃取代的化合物、其制备方法和用途 |
CN103420993B (zh) * | 2013-07-16 | 2014-12-17 | 浙江医药高等专科学校 | 含噻吩取代的化合物、其制备方法和用途 |
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CN102811619B (zh) | 2015-04-22 |
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JP2013510876A (ja) | 2013-03-28 |
SG10201407453TA (en) | 2014-12-30 |
CL2012001221A1 (es) | 2013-06-07 |
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AU2010319382A1 (en) | 2012-04-19 |
CA2780892A1 (en) | 2011-05-19 |
BR112012011287B1 (pt) | 2022-02-08 |
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MY160820A (en) | 2017-03-31 |
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