HRP20161478T1 - Inhibitori protein kinaze (varijante), njihova upotreba za liječenje neuroloških bolesti, kao i farmaceutski pripravak koji se na njima temelji - Google Patents
Inhibitori protein kinaze (varijante), njihova upotreba za liječenje neuroloških bolesti, kao i farmaceutski pripravak koji se na njima temelji Download PDFInfo
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- HRP20161478T1 HRP20161478T1 HRP20161478TT HRP20161478T HRP20161478T1 HR P20161478 T1 HRP20161478 T1 HR P20161478T1 HR P20161478T T HRP20161478T T HR P20161478TT HR P20161478 T HRP20161478 T HR P20161478T HR P20161478 T1 HRP20161478 T1 HR P20161478T1
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- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- compound
- solvate
- ring
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- 201000010099 disease Diseases 0.000 title claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims 3
- 239000003909 protein kinase inhibitor Substances 0.000 title claims 2
- 229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 title 1
- 230000000771 oncological effect Effects 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims 24
- 150000001875 compounds Chemical class 0.000 claims 21
- 239000012453 solvate Substances 0.000 claims 18
- 239000000203 mixture Substances 0.000 claims 16
- 125000005843 halogen group Chemical group 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 239000000825 pharmaceutical preparation Substances 0.000 claims 6
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 4
- 229910020008 S(O) Inorganic materials 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 208000032839 leukemia Diseases 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 101150097247 CRT1 gene Proteins 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 206010051066 Gastrointestinal stromal tumour Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 102000001253 Protein Kinase Human genes 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 229940043355 kinase inhibitor Drugs 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 108060006633 protein kinase Proteins 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- -1 -OH Chemical group 0.000 claims 1
- 108020004021 3-ketosteroid receptors Proteins 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 239000005517 L01XE01 - Imatinib Substances 0.000 claims 1
- 108020000002 NR3 subfamily Proteins 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 238000002648 combination therapy Methods 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 239000000945 filler Substances 0.000 claims 1
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- KTUFNOKKBVMGRW-UHFFFAOYSA-N imatinib Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 KTUFNOKKBVMGRW-UHFFFAOYSA-N 0.000 claims 1
- 229960002411 imatinib Drugs 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 239000008177 pharmaceutical agent Substances 0.000 claims 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
-
- 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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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (17)
1. Inhibitor protein kinaze s Formulom I
[image]
ili tautomer, stereoizomer ili smjesa stereoizomera, ili njegova farmaceutski prihvatljiva sol, solvat ili hidrat, naznačen time da:
X1 je N ili CRt1;
X2 je N ili CRt2;
X3 je N ili CRt3;
X4 je N ili CH;
pri čemu X1, X2, X3, i X4 su odabrani neovisno;
Rt1 je odabran od -H, halo, -COOH, -CN, -CH2OH, C1-C4-alkil, -O(C1-C3-alkil);
Rt2 je odabran od -H, halo, -CH3, -CH2CH3, -OH, -OCH3, i -NH2;
Rt3 je odabran od -H, halo, -S(O)rR4, -CN, i C(O)YR4;
prsten A je aril ili 5- ili 6-člani heteroaril prsten, pri čemu heteroaril koji tvori prsten A sadrži 1-2 heteroatoma koji se biraju od N, S, i O, te pri čemu je prsten A proizvoljno supstituiran s 1-4 skupine Ra;
prsten B je fenil ili 5- ili 6-člani heteroaril prsten, pri čemu heteroaril koji tvori prsten B sadrži 1-2 prstenskih heteroatoma koji se biraju od N ili S i pri čemu je prsten B proizvoljno supstituiran s 1-5 skupina Rb;
Ra i Rb su svaki neovisno odabrani od -H, halo, -CN, -R6, -OR4, -NR4R5, -C(O)YR4, -S(O)rR4, -SO2NR4R5, -NR4SO2NR4R5;
alternativno, jedan Rb supstituent u prstenu B može biti prsten C, pri čemu prsten C je 5- ili 6-člani heteroaril ili heterociklil prsten koji sadrži ugljikove atome i 1-3 heteroatoma koji su neovisno odabrani od O, N i S(O)r, te pri čemu je prsten C proizvoljno supstituiran s 1 do 5 supstituenata Rc;
svaki Rc je neovisno odabran od -H, halo, i -R6;
alternativno jedan od Rb supstituenata može imati strukturu -L2-D, pri čemu D je prsten,
L2 je (CH2)z, i z je 1, 2, 3 ili 4; ili L2 je (OCH2)x, pri čemu x je 0, 1, 2 ili 3, te pri čemu
prsten D je 5- ili 6-člani heteroaril ili heterociklil prsten koji sadrži ugljikove atome i 1-3 heteroatoma neovisno odabrana od O, N i S(O)r, i pri čemu prsten D je proizvoljno supstituiran s 1 do 5 supstituenata Rd;
svaki Rd je neovisno odabran od -H, halo, R6, -OR4 ili -NR4R5;
L1 predstavlja NR3C(O) ili C(O)NR3;
svaki Y je neovisno odabran od kemijske veze, -O-, -S-, i -NR5;
svaki R3, svaki R4 i svaki R5 je neovisno odabran od H i C1-C6-alkil, pri čemu
alternativno skupina NR4R5 može predstavljati 5- ili 6-člani zasićeni, ili
nezasićeni prsten;
svaki R6 je neovisno odabran od C1-C6-alkil ili C2-C6-alkenil; i
r je 0, 1, ili 2.
2. Spoj, tautomer, stereoizomer, smjesa stereoizomera, ili farmaceutski prihvatljiva sol, solvat ili hidrat prema zahtjevu 1, naznačen time da X1 je CRt1, X2 je CRt2, X3 je CRt3, i X4 je CH.
3. Spoj, tautomer, stereoizomer, smjesa stereoizomera, ili farmaceutski prihvatljiva sol, solvat ili hidrat prema zahtjevu 1, ili njihova farmaceutski prihvatljiva sol, naznačen time da Rt1 je -H ili -Cl.
4. Spoj, tautomer, stereoizomer, smjesa stereoizomera, ili farmaceutski prihvatljiva sol, solvat ili hidrat prema zahtjevu 1, ili njihova farmaceutski prihvatljiva sol, naznačen time da Rt2 je -H.
5. Spoj, tautomer, stereoizomer, smjesa stereoizomera, ili farmaceutski prihvatljiva sol, solvat ili hidrat prema zahtjevu 1, ili njihova farmaceutski prihvatljiva sol, naznačen time da Rt3 je -H ili halo.
6. Spoj, tautomer, stereoizomer, smjesa stereoizomera, ili farmaceutski prihvatljiva sol, solvat ili hidrat prema zahtjevu 1, ili njihova farmaceutski prihvatljiva sol, naznačen time da prsten A je fenil.
7. Spoj, tautomer, stereoizomer, smjesa stereoizomera, ili farmaceutski prihvatljiva sol, solvat ili hidrat prema zahtjevu 1, naznačen time da svaki R6 je neovisno odabran iz skupa koji čine fluorometil, difluorometil i trifluorometil.
8. Spoj, tautomer, stereoizomer, smjesa stereoizomera, ili farmaceutski prihvatljiva sol, solvat ili hidrat prema zahtjevu 1, ili njihova farmaceutski prihvatljiva sol, naznačen time da skupina
[image]
ima jednu od slijedećih struktura:
[image]
ili
[image]
9. Spoj, tautomer, stereoizomer, smjesa stereoizomera, ili farmaceutski prihvatljiva sol, solvat ili hidrat prema zahtjevu 1, naznačen time da spoj ima jednu od slijedećih struktura:
[image]
[image]
[image]
ili
[image]
10. Spoj, tautomer, stereoizomer, smjesa stereoizomera, ili farmaceutski prihvatljiva sol, solvat ili hidrat prema zahtjevu 1, ili njihova farmaceutski prihvatljiva sol, naznačen time da spoj ima slijedeću strukturu:
[image]
11. Farmaceutski pripravak naznačen time da sadrži spoj, tautomer, stereoizomer, smjesu stereoizomera, ili farmaceutski prihvatljivu sol, solvat ili hidrat prema bilo kojem od patentnih zahtjeva 1 do 10 i farmaceutski prihvatljiv nosač, otapalo ili punilo.
12. Spoj, tautomer, stereoizomer, smjesa stereoizomera, ili farmaceutski prihvatljiva sol, solvat ili hidrat prema bilo kojem od patentnih zahtjeva 1 do 10 ili farmaceutski pripravak prema zahtjevu 11 naznačen time da je za uporabu u medicini.
13. Spoj, tautomer, stereoizomer, smjesa stereoizomera, ili farmaceutski prihvatljiva sol, solvat ili hidrat prema bilo kojem od patentnih zahtjeva 1 do 10 ili farmaceutski pripravak prema zahtjevu 11 naznačen time da je za uporabu za liječenje bolesti povezane s netipičnom aktivnošću protein kinaze.
14. Spoj, tautomer, stereoizomer, smjesa stereoizomera, ili farmaceutski prihvatljiva sol, solvat ili hidrat, ili farmaceutski pripravak za uporabu prema zahtjevu 13, naznačen time da bolest povezana s netipičnom aktivnošću protein kinaze je leukemija, kronična mijelogena leukemija, hepatocelulani karcinom, karcinom pluća ne-malih stanica ili gastrointestinalni stromalni tumor.
15. Spoj, tautomer, stereoizomer, smjesa stereoizomera, ili farmaceutski prihvatljiva sol, solvat ili hidrat, ili farmaceutski pripravak za uporabu prema zahtjevu 14, naznačen time da je leukemija rezistentna na liječenje s imatinibom, ili drugim inhibitorom kinaze.
16. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, solvat ili hidrat, naznačen time da spoj ima slijedeću strukturu:
[image]
naznačen time da je za uporabu za liječenje leukemije, kronične mijelogene leukemije, hepatocelulanog karcinoma, karcinoma pluća ne-malih stanica ili gastrointestinalnog stromalnog tumora
17. Spoj, tautomer, stereoizomer, smjesa stereoizomera, ili farmaceutski prihvatljiva sol, solvat ili hidrat, ili farmaceutski pripravak za uporabu prema zahtjevu 13, 14, ili 15, ili spoj, farmaceutski prihvatljiva sol, solvat ili hidrat za uporabu prema zahtjevu 16, naznačen time da se spoj primjenjuje u kombiniranoj terapiji s drugim farmaceutskim sredstvom.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| RU2011124304/04A RU2477723C2 (ru) | 2011-06-16 | 2011-06-16 | Ингибиторы протеинкиназ (варианты), их применение для лечения онкологических заболеваний и фармацевтическая композиция на их основе |
| EP12801171.5A EP2743266B8 (en) | 2011-06-16 | 2012-05-29 | Protein kinase inhibitors (variants), use thereof in treating oncological diseases and a pharmaceutical composition based thereon |
| PCT/RU2012/000423 WO2012173521A2 (ru) | 2011-06-16 | 2012-05-29 | Ингибиторы протеинкиназ (варианты), их применение для лечения онкологических заболеваний и фармацевтическая композиция на их основе |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20161478T1 true HRP20161478T1 (hr) | 2016-12-16 |
Family
ID=47357651
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20161478TT HRP20161478T1 (hr) | 2011-06-16 | 2016-11-08 | Inhibitori protein kinaze (varijante), njihova upotreba za liječenje neuroloških bolesti, kao i farmaceutski pripravak koji se na njima temelji |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US9522910B2 (hr) |
| EP (1) | EP2743266B8 (hr) |
| AU (1) | AU2012269818B2 (hr) |
| CA (1) | CA2850137C (hr) |
| CY (1) | CY1118513T1 (hr) |
| DK (1) | DK2743266T3 (hr) |
| EA (1) | EA026704B1 (hr) |
| ES (1) | ES2602797T3 (hr) |
| HK (1) | HK1195771A1 (hr) |
| HR (1) | HRP20161478T1 (hr) |
| HU (1) | HUE031837T2 (hr) |
| IL (1) | IL232357A (hr) |
| IN (1) | IN2014MN00635A (hr) |
| LT (1) | LT2743266T (hr) |
| PL (1) | PL2743266T3 (hr) |
| PT (1) | PT2743266T (hr) |
| RS (1) | RS55380B1 (hr) |
| RU (1) | RU2477723C2 (hr) |
| SI (1) | SI2743266T1 (hr) |
| SM (1) | SMT201600398B (hr) |
| UA (1) | UA115228C2 (hr) |
| WO (1) | WO2012173521A2 (hr) |
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| US8859553B2 (en) * | 2012-07-30 | 2014-10-14 | Astar Biotech Llc | Protein kinase inhibitors |
| CN103664787B (zh) * | 2012-09-17 | 2015-09-09 | 南京圣和药业股份有限公司 | 炔杂芳环化合物及其应用 |
| CN104341416B (zh) * | 2013-07-31 | 2017-03-29 | 南京圣和药业股份有限公司 | 蛋白酪氨酸激酶抑制剂及其应用 |
| US10172839B2 (en) | 2014-03-06 | 2019-01-08 | University Of Southern California | Use of short term starvation regimen in combination with kinase inhibitors to enhance traditional chemo-drug efficacy and feasibility and reverse side effects of kinases in normal cells and tissues |
| ES2846153T3 (es) * | 2014-03-06 | 2021-07-28 | Univ Southern California | Uso de régimen de inanición a corto plazo en combinación con inhibidores de cinasa para potenciar la eficacia y viabilidad de fármacos quimioterápicos tradicionales y revertir efectos secundarios de cinasas en células y tejidos normales |
| CN106146391A (zh) | 2015-04-15 | 2016-11-23 | 中国科学院上海药物研究所 | 5-芳香炔基取代的苯甲酰胺类化合物及其制备方法、药物组合物和用途 |
| AR104259A1 (es) * | 2015-04-15 | 2017-07-05 | Celgene Quanticel Res Inc | Inhibidores de bromodominio |
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| RU2652992C2 (ru) * | 2016-04-18 | 2018-05-04 | Общество С Ограниченной Ответственностью "Фьюжн Фарма" | Новая кристаллическая солевая форма 3-(1,2,4-триазоло[4,3-а]пиридин-3-илэтинил)-4-метил-n-(4-((4-метилпиперазин-1-ил)метил)-3-трифторметилфенил)бензамида для медицинского применения |
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| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| CN110267960B (zh) | 2017-01-18 | 2022-04-26 | 阿雷生物药品公司 | 作为RET激酶抑制剂的取代的吡唑并[1,5-a]吡嗪化合物 |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
| TWI812649B (zh) | 2017-10-10 | 2023-08-21 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
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| CA3111984A1 (en) | 2018-09-10 | 2020-03-19 | Array Biopharma Inc. | Fused heterocyclic compounds as ret kinase inhibitors |
| BR112021008524A8 (pt) * | 2018-11-02 | 2023-02-07 | Merck Sharp & Dohme | 2-amino-n-heteroaril-nicotinamidas como inibidores de nav 1.8 |
| WO2022015051A1 (ko) * | 2020-07-14 | 2022-01-20 | 주식회사 보로노이바이오 | 아릴 또는 헤테로아릴 유도체, 및 이를 유효성분으로 포함하는 키나아제 관련 질환 예방 또는 치료용 약학적 조성물 |
| GB202209210D0 (en) * | 2022-06-23 | 2022-08-10 | Univ Strathclyde | Cycloaddition reactions |
| CN116217571A (zh) * | 2023-03-28 | 2023-06-06 | 上海锐谱医药科技有限公司 | 一种制备药物砌块1,2,4-三唑并[4,3-a]吡啶-3-胺的方法 |
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| HUP0302173A2 (hu) | 2000-09-15 | 2003-09-29 | Vertex Pharmaceuticals Incorporated | Protein kináz inhibitorokként alkalmazható pirazolvegyületek |
| RU2340611C2 (ru) * | 2000-09-15 | 2008-12-10 | Вертекс Фармасьютикалз Инкорпорейтед | Производные пиразола, используемые в качестве ингибиторов протеинкиназы |
| US7709520B2 (en) | 2000-10-06 | 2010-05-04 | The Texas A&M University System | Diindolylmethane and C-substituted diindolylmethane compositions and methods for the treatment of multiple cancers |
| CN1933839A (zh) | 2004-01-23 | 2007-03-21 | 安进公司 | 化合物和使用方法 |
| US7745437B2 (en) | 2004-06-10 | 2010-06-29 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| US8158825B2 (en) | 2005-06-24 | 2012-04-17 | Merck Sharp & Dohme Corp. | Modified malonate derivatives |
| JP5200939B2 (ja) * | 2005-12-23 | 2013-06-05 | アリアド・ファーマシューティカルズ・インコーポレイテッド | 二環式ヘテロアリール化合物 |
| EP1989203A2 (en) | 2006-02-16 | 2008-11-12 | Millennium Pharmaceuticals, Inc. | Alpha carbolines and uses thereof |
| JP5273037B2 (ja) * | 2006-05-08 | 2013-08-28 | アリアド・ファーマシューティカルズ・インコーポレイテッド | アセチレン性ヘテロアリール化合物 |
| WO2007145840A2 (en) | 2006-06-13 | 2007-12-21 | Oncomed Pharmaceuticals, Inc. | Compositions and methods for diagnosing and treating cancer |
| US7612085B2 (en) | 2006-07-11 | 2009-11-03 | Washington University | Sigma 2 receptor ligands and therapeutic uses therefor |
| WO2008077138A1 (en) | 2006-12-19 | 2008-06-26 | The Board Of Trustees Of The University Of Illinois | 3-benzofuranyl-4-indolyl maleimides as potent gsk3 inhibitors for neurogenerative disorders |
| JP2010531304A (ja) | 2007-06-18 | 2010-09-24 | ユニバーシティ オブ ルイビル リサーチ ファウンデーション、インコーポレイテッド | 抗悪性腫瘍活性を有するｐｆｋｆｂ３阻害物質ファミリー |
| US8124768B2 (en) | 2008-01-23 | 2012-02-28 | Bristol-Myers Squibb Company | 4-pyridinone compounds and their use for cancer |
| US8211911B2 (en) | 2008-08-19 | 2012-07-03 | Guoqing Paul Chen | Compounds as kinase inhibitors |
| US8188109B2 (en) | 2009-07-20 | 2012-05-29 | Naxospharma S.R.L. | Benzoquinolizinium salt derivatives as anticancer agents |
| US8242282B2 (en) | 2010-05-18 | 2012-08-14 | Taipei Medical University | Histone deacetylase inhibitors |
| RU2011113236A (ru) | 2011-04-07 | 2012-10-20 | Общество с ограниченной ответственностью "Фьюжн Фарма" (RU) | Новые химические соединения для лечения онкологических заболеваний |
| WO2013170770A1 (zh) * | 2012-05-16 | 2013-11-21 | 上海医药集团股份有限公司 | 具有抗肿瘤活性的乙炔衍生物 |
| US8859553B2 (en) | 2012-07-30 | 2014-10-14 | Astar Biotech Llc | Protein kinase inhibitors |
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| CA2850137C (en) | 2016-10-25 |
| EA201491356A1 (ru) | 2015-01-30 |
| EP2743266A2 (en) | 2014-06-18 |
| RS55380B1 (sr) | 2017-03-31 |
| ES2602797T3 (es) | 2017-02-22 |
| EP2743266B1 (en) | 2016-08-17 |
| PT2743266T (pt) | 2016-10-14 |
| US20140213592A1 (en) | 2014-07-31 |
| CY1118513T1 (el) | 2017-07-12 |
| SI2743266T1 (en) | 2017-02-28 |
| RU2011124304A (ru) | 2012-12-27 |
| EA026704B1 (ru) | 2017-05-31 |
| WO2012173521A2 (ru) | 2012-12-20 |
| SMT201600398B (it) | 2017-01-10 |
| IN2014MN00635A (hr) | 2015-07-03 |
| LT2743266T (lt) | 2016-12-12 |
| HK1195771A1 (zh) | 2014-11-21 |
| DK2743266T3 (en) | 2016-12-05 |
| AU2012269818B2 (en) | 2016-05-19 |
| IL232357A0 (en) | 2014-07-01 |
| UA115228C2 (uk) | 2017-10-10 |
| WO2012173521A3 (ru) | 2013-03-28 |
| CA2850137A1 (en) | 2012-12-20 |
| AU2012269818A1 (en) | 2014-06-26 |
| RU2477723C2 (ru) | 2013-03-20 |
| EP2743266B8 (en) | 2016-09-28 |
| US9522910B2 (en) | 2016-12-20 |
| PL2743266T3 (pl) | 2017-02-28 |
| HUE031837T2 (en) | 2017-08-28 |
| EP2743266A4 (en) | 2015-03-11 |
| IL232357A (en) | 2017-05-29 |
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