EA019951B1 - Ингибиторы киназы pim и способы их применения - Google Patents
Ингибиторы киназы pim и способы их применения Download PDFInfo
- Publication number
- EA019951B1 EA019951B1 EA200901144A EA200901144A EA019951B1 EA 019951 B1 EA019951 B1 EA 019951B1 EA 200901144 A EA200901144 A EA 200901144A EA 200901144 A EA200901144 A EA 200901144A EA 019951 B1 EA019951 B1 EA 019951B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- amino
- butyl
- tert
- group
- piperidin
- Prior art date
Links
- 238000000034 method Methods 0.000 title claims abstract description 362
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- LFPQJVGUJOEHTQ-UHFFFAOYSA-N tert-butyl n-[4-[tert-butyl(dimethyl)silyl]oxy-1-(3-nitropyridin-4-yl)piperidin-3-yl]carbamate Chemical compound C1CC(O[Si](C)(C)C(C)(C)C)C(NC(=O)OC(C)(C)C)CN1C1=CC=NC=C1[N+]([O-])=O LFPQJVGUJOEHTQ-UHFFFAOYSA-N 0.000 description 1
- YGBJSOUMTFURQY-UHFFFAOYSA-N tert-butyl n-[6-(3-aminopyridin-4-yl)-2-(trifluoromethyl)pyrimidin-4-yl]carbamate Chemical compound FC(F)(F)C1=NC(NC(=O)OC(C)(C)C)=CC(C=2C(=CN=CC=2)N)=N1 YGBJSOUMTFURQY-UHFFFAOYSA-N 0.000 description 1
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- POLUQQOEPPLKHA-UHFFFAOYSA-N tert-butyl n-[[1-(6-amino-2-oxo-1h-pyrimidin-5-yl)piperidin-3-yl]methyl]carbamate Chemical compound C1C(CNC(=O)OC(C)(C)C)CCCN1C1=C(N)NC(=O)N=C1 POLUQQOEPPLKHA-UHFFFAOYSA-N 0.000 description 1
- CBXCPBUEXACCNR-UHFFFAOYSA-N tetraethylammonium Chemical compound CC[N+](CC)(CC)CC CBXCPBUEXACCNR-UHFFFAOYSA-N 0.000 description 1
- WHRNULOCNSKMGB-UHFFFAOYSA-N tetrahydrofuran thf Chemical compound C1CCOC1.C1CCOC1 WHRNULOCNSKMGB-UHFFFAOYSA-N 0.000 description 1
- QEMXHQIAXOOASZ-UHFFFAOYSA-N tetramethylammonium Chemical compound C[N+](C)(C)C QEMXHQIAXOOASZ-UHFFFAOYSA-N 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 229950006410 tezacitabine Drugs 0.000 description 1
- GFFXZLZWLOBBLO-ASKVSEFXSA-N tezacitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(=C/F)/[C@H](O)[C@@H](CO)O1 GFFXZLZWLOBBLO-ASKVSEFXSA-N 0.000 description 1
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- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- 238000011200 topical administration Methods 0.000 description 1
- XFCLJVABOIYOMF-QPLCGJKRSA-N toremifene Chemical compound C1=CC(OCCN(C)C)=CC=C1C(\C=1C=CC=CC=1)=C(\CCCl)C1=CC=CC=C1 XFCLJVABOIYOMF-QPLCGJKRSA-N 0.000 description 1
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- 238000013519 translation Methods 0.000 description 1
- 230000005945 translocation Effects 0.000 description 1
- 229960005526 triapine Drugs 0.000 description 1
- YOWGRWHKDCHINP-UHFFFAOYSA-N tributyl(1,3-oxazol-2-yl)stannane Chemical compound CCCC[Sn](CCCC)(CCCC)C1=NC=CO1 YOWGRWHKDCHINP-UHFFFAOYSA-N 0.000 description 1
- YYQKQPYPLADFMK-UHFFFAOYSA-N tributyl(1,3-thiazol-4-yl)stannane Chemical compound CCCC[Sn](CCCC)(CCCC)C1=CSC=N1 YYQKQPYPLADFMK-UHFFFAOYSA-N 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
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- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 description 1
- MWKJTNBSKNUMFN-UHFFFAOYSA-N trifluoromethyltrimethylsilane Chemical compound C[Si](C)(C)C(F)(F)F MWKJTNBSKNUMFN-UHFFFAOYSA-N 0.000 description 1
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- 230000004614 tumor growth Effects 0.000 description 1
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- 150000004917 tyrosine kinase inhibitor derivatives Chemical class 0.000 description 1
- ZDPHROOEEOARMN-UHFFFAOYSA-N undecanoic acid Chemical compound CCCCCCCCCCC(O)=O ZDPHROOEEOARMN-UHFFFAOYSA-N 0.000 description 1
- 125000002948 undecyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
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- CZPRKINNVBONSF-UHFFFAOYSA-M zinc;dioxido(oxo)phosphanium Chemical compound [Zn+2].[O-][P+]([O-])=O CZPRKINNVBONSF-UHFFFAOYSA-M 0.000 description 1
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Classifications
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- 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
- C07D401/02—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 two hetero rings
- C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/435—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
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| US89244407P | 2007-03-01 | 2007-03-01 | |
| US2377708P | 2008-01-25 | 2008-01-25 | |
| PCT/US2008/055724 WO2008106692A1 (en) | 2007-03-01 | 2008-03-03 | Pim kinase inhibitors and methods of their use |
Publications (2)
| Publication Number | Publication Date |
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| EA200901144A1 EA200901144A1 (ru) | 2010-04-30 |
| EA019951B1 true EA019951B1 (ru) | 2014-07-30 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200901144A EA019951B1 (ru) | 2007-03-01 | 2008-03-03 | Ингибиторы киназы pim и способы их применения |
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| Country | Link |
|---|---|
| US (1) | US8822497B2 (enExample) |
| EP (1) | EP2132177B1 (enExample) |
| JP (1) | JP5330274B2 (enExample) |
| KR (1) | KR101514853B1 (enExample) |
| CN (1) | CN101679266B (enExample) |
| AU (1) | AU2008221263B2 (enExample) |
| BR (1) | BRPI0808523A2 (enExample) |
| CA (1) | CA2679659C (enExample) |
| EA (1) | EA019951B1 (enExample) |
| ES (1) | ES2431163T3 (enExample) |
| MX (1) | MX2009009304A (enExample) |
| WO (1) | WO2008106692A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2605400C1 (ru) * | 2015-11-13 | 2016-12-20 | ЗАО "Р-Фарм" | ПРОИЗВОДНЫЕ 1-(3-АМИНОФЕНИЛ)-6,8-ДИМЕТИЛ-5-(4-ИОД-2-ФТОР-ФЕНИЛАМИНО)-3-ЦИКЛОПРОПИЛ-1H,6H-ПИРИДО[4,3-d]ПИРИМИДИН-2,4,7-ТРИОНА В КАЧЕСТВЕ ИНГИБИТОРОВ МЕК1/2 |
Families Citing this family (155)
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| US8093401B2 (en) | 2005-08-04 | 2012-01-10 | Sirtris Pharmaceuticals, Inc. | Sirtuin modulating compounds |
| US7855289B2 (en) | 2005-08-04 | 2010-12-21 | Sirtris Pharmaceuticals, Inc. | Sirtuin modulating compounds |
| US8088928B2 (en) | 2005-08-04 | 2012-01-03 | Sirtris Pharmaceuticals, Inc. | Sirtuin modulating compounds |
| EP2388263A1 (en) | 2005-08-04 | 2011-11-23 | Sirtris Pharmaceuticals, Inc. | Imidazo[2,1-b]thiazole derivatives as sirtuin modulators |
| PT1966202E (pt) | 2005-12-13 | 2012-01-03 | Incyte Corp | Pirrolo[2,3-b] pirimidinas e pirrolo[2,3-b]piridinas substituídas com heteroarilo como inibidores de janus quinase |
| PE20080928A1 (es) | 2006-10-31 | 2008-08-15 | Schering Corp | Derivados de anilinopiperazina como inhibidores de proteina quinasa |
| EP2078003B1 (en) | 2006-10-31 | 2017-03-08 | Merck Sharp & Dohme Corp. | Anilinopiperazine derivatives and methods of use thereof |
| US20140249135A1 (en) * | 2007-03-01 | 2014-09-04 | Novartis Ag | Pim kinase inhibitors and methods of their use |
| AU2008247102B2 (en) | 2007-05-03 | 2011-11-24 | Pfizer Limited | 2 -pyridine carboxamide derivatives as sodium channel modulators |
| RS53245B2 (sr) | 2007-06-13 | 2022-10-31 | Incyte Holdings Corp | Soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo(2,3-d) pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropan-nitrila |
| CL2008001821A1 (es) | 2007-06-20 | 2009-03-13 | Sirtris Pharmaceuticals Inc | Compuestos derivados de imidazo[2,1-b]-tiazol; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento de diabetes, sindrome metabolico, resistencia a la insulina, entre otras. |
| TW200916472A (en) | 2007-06-20 | 2009-04-16 | Sirtris Pharmaceuticals Inc | Sirtuin modulating compounds |
| CL2008001943A1 (es) | 2007-07-02 | 2009-09-11 | Boehringer Ingelheim Int | Compuestos derivados de fenil-triazol, inhibidores de enzimas de señales especificas que participan del control de la proliferacion celular; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar cancer, infecciones, enfermedades inflamatorias y autoinmunes. |
| RU2474580C2 (ru) * | 2007-07-19 | 2013-02-10 | Шеринг Корпорейшн | Гетероциклические амидные соединения как ингибиторы протеинкиназ |
| WO2009020198A1 (ja) * | 2007-08-03 | 2009-02-12 | Kinopharma, Inc. | 抗dnaウイルス作用を有するアニリン誘導体 |
| EP2215066A1 (en) * | 2007-11-01 | 2010-08-11 | Sirtris Pharmaceuticals, Inc. | Amide derivatives as sirtuin modulators |
| PE20091577A1 (es) * | 2008-03-03 | 2009-11-05 | Novartis Ag | Inhibidores de cinasa pim y metodos para su uso |
| CL2009001152A1 (es) | 2008-05-13 | 2009-10-16 | Array Biopharma Inc | Compuestos derivados de n-(4-(cicloalquilo nitrogenado-1-il)-1h-pirrolo[2,3-b]piridin-3-il)amida, inhibidores de cinasa; proceso de preparacion; composicion farmaceutica; y su uso para el tratamiento de una enfermedad proliferativa. |
| AU2011265439B2 (en) * | 2008-09-02 | 2012-09-20 | Novartis Ag | Picolinamide derivatives as kinase inhibitors |
| PE20110298A1 (es) * | 2008-09-02 | 2011-05-21 | Novartis Ag | Derivados de picolinamida como inhibidores de cinasa |
| US8778929B2 (en) * | 2008-09-29 | 2014-07-15 | Boehringer Ingelheim International Gmbh | Substituted heteroaryl inhibitors of B-RAF |
| US8110578B2 (en) | 2008-10-27 | 2012-02-07 | Signal Pharmaceuticals, Llc | Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway |
| KR101712576B1 (ko) | 2008-11-10 | 2017-03-06 | 버텍스 파마슈티칼스 인코포레이티드 | Atr 키나제의 억제제로서 유용한 화합물 |
| CA2747715A1 (en) | 2008-12-19 | 2010-06-24 | Sirtris Pharmaceuticals, Inc. | Thiazolopyridine sirtuin modulating compounds |
| PL2376485T3 (pl) | 2008-12-19 | 2018-05-30 | Vertex Pharmaceuticals Incorporated | Pochodne pirazyny użyteczne jako inhibitory kinazy ATR |
| PL2432472T3 (pl) | 2009-05-22 | 2020-03-31 | Incyte Holdings Corporation | 3-[4-(7H-Pirolo[2,3-d]pirymidyn-4-ylo)-1H-pirazol-1-ilo]oktano- lub heptano-nitryle jako inhibitory JAK |
| TW201100429A (en) | 2009-05-22 | 2011-01-01 | Incyte Corp | N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| AR077328A1 (es) | 2009-07-24 | 2011-08-17 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos |
| US8415381B2 (en) * | 2009-07-30 | 2013-04-09 | Novartis Ag | Heteroaryl compounds and their uses |
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| RU2605400C1 (ru) * | 2015-11-13 | 2016-12-20 | ЗАО "Р-Фарм" | ПРОИЗВОДНЫЕ 1-(3-АМИНОФЕНИЛ)-6,8-ДИМЕТИЛ-5-(4-ИОД-2-ФТОР-ФЕНИЛАМИНО)-3-ЦИКЛОПРОПИЛ-1H,6H-ПИРИДО[4,3-d]ПИРИМИДИН-2,4,7-ТРИОНА В КАЧЕСТВЕ ИНГИБИТОРОВ МЕК1/2 |
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| AU2008221263A1 (en) | 2008-09-04 |
| JP2010520228A (ja) | 2010-06-10 |
| EP2132177B1 (en) | 2013-07-17 |
| KR101514853B1 (ko) | 2015-04-24 |
| AU2008221263B2 (en) | 2012-02-23 |
| US20120208815A1 (en) | 2012-08-16 |
| KR20100015331A (ko) | 2010-02-12 |
| WO2008106692A1 (en) | 2008-09-04 |
| CA2679659C (en) | 2016-01-19 |
| ES2431163T3 (es) | 2013-11-25 |
| US8822497B2 (en) | 2014-09-02 |
| WO2008106692B1 (en) | 2008-10-30 |
| CN101679266B (zh) | 2015-05-06 |
| CA2679659A1 (en) | 2008-09-04 |
| JP5330274B2 (ja) | 2013-10-30 |
| MX2009009304A (es) | 2009-11-18 |
| BRPI0808523A2 (pt) | 2014-08-19 |
| CN101679266A (zh) | 2010-03-24 |
| EP2132177A1 (en) | 2009-12-16 |
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