AR070531A1 - Inhibidores de cinasa pim y metodos para su uso - Google Patents
Inhibidores de cinasa pim y metodos para su usoInfo
- Publication number
- AR070531A1 AR070531A1 ARP090100684A ARP090100684A AR070531A1 AR 070531 A1 AR070531 A1 AR 070531A1 AR P090100684 A ARP090100684 A AR P090100684A AR P090100684 A ARP090100684 A AR P090100684A AR 070531 A1 AR070531 A1 AR 070531A1
- Authority
- AR
- Argentina
- Prior art keywords
- methyl
- compounds
- och3
- pharmaceutically acceptable
- pim kinase
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
- 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
- C07D417/02—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 containing two hetero rings
- C07D417/12—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 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D417/14—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 containing three or more hetero rings
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Virology (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente se refiere a compuestos de Ia formula (1), a sus tautomeros, estereoisomeros y polimorfos, y a las sales farmacéuticamente aceptables, ésteres, metabolitos o pro-fármacos de los mismos, a composiciones de los compuestos junto con vehículos farmacéuticamente aceptables, y al uso de los compuestos, ya sea solos o bien en combinacion con cuando menos un agente terapéutico adicional, en la inhibicion de la actividad de la cinasa Pim y/o en la profilaxis o el tratamiento de cáncer. Reivindicacion 1: Un compuesto de la formula (1), o un estereoisomero, tautomero, o una sal farmacéuticamente aceptable del mismo, en donde: R1 se selecciona a partir de los compuestos del grupo de formulas (2); X representa CH o N; R2a se selecciona a partir de amino, metilo, CH2F, CF3, C2H5, y H; R2b se selecciona a partir de H, y metilo; R3 se selecciona a partir de H, OH, OCH3, CH3, F, y CI; R4a se selecciona a partir de amino, metilo, OH, OCH3, OC2H5, F, CF3, H, y etilo; R4b se selecciona a partir de metilo, H, y F; R21 representa H o F; R22 representa H, CI, o F; R23 representa F, OC2H5, OCH3, CI, H, metilo, OH, u OCH(CH3)2; y R24 representa H u OH.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US3335908P | 2008-03-03 | 2008-03-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR070531A1 true AR070531A1 (es) | 2010-04-14 |
Family
ID=41055566
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090100684A AR070531A1 (es) | 2008-03-03 | 2009-02-27 | Inhibidores de cinasa pim y metodos para su uso |
Country Status (21)
| Country | Link |
|---|---|
| EP (2) | EP2262802B1 (es) |
| JP (1) | JP5412448B2 (es) |
| KR (1) | KR20100120709A (es) |
| CN (2) | CN102015701B (es) |
| AR (1) | AR070531A1 (es) |
| AU (1) | AU2009221134B2 (es) |
| BR (1) | BRPI0909102A2 (es) |
| CA (1) | CA2717388A1 (es) |
| CL (1) | CL2009000483A1 (es) |
| CO (1) | CO6290687A2 (es) |
| EA (1) | EA201001412A1 (es) |
| EC (1) | ECSP10010447A (es) |
| ES (2) | ES2443496T3 (es) |
| IL (1) | IL207865A0 (es) |
| MA (1) | MA32135B1 (es) |
| MX (1) | MX2010009739A (es) |
| PE (1) | PE20091577A1 (es) |
| TW (1) | TW200942536A (es) |
| UY (1) | UY31679A1 (es) |
| WO (1) | WO2009109576A1 (es) |
| ZA (1) | ZA201006128B (es) |
Families Citing this family (51)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| LT2474545T (lt) | 2005-12-13 | 2017-02-27 | Incyte Holdings Corporation | Heteroarilu pakeisti pirolo[2,3-b]piridinai ir pirolo[2,3-b]pirimidinai kaip janus kinazės inhibitoriai |
| LT3070090T (lt) | 2007-06-13 | 2019-06-25 | Incyte Holdings Corporation | Janus kinazės inhibitoriaus (r)-3-(4-(7h-pirol[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropannitrilo druskų panaudojimas |
| GEP20135849B (en) * | 2008-09-02 | 2013-06-10 | Novartis Ag | Picolinamide derivatives as kinase inhibitors |
| JP5775070B2 (ja) | 2009-05-22 | 2015-09-09 | インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ | ヤヌスキナーゼ阻害剤としてのピラゾール−４−イル−ピロロ［２，３−ｄ］ピリミジンおよびピロール−３−イル−ピロロ［２，３−ｄ］ピリミジンのＮ−（ヘテロ）アリール−ピロリジン誘導体 |
| MY161416A (en) | 2009-05-22 | 2017-04-14 | Incyte Holdings Corp | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4yl)-1h-pyrazol-1-yl]octane-or heptane-nitrile as jak inhibitors |
| US9249145B2 (en) | 2009-09-01 | 2016-02-02 | Incyte Holdings Corporation | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| US8435976B2 (en) | 2009-09-08 | 2013-05-07 | F. Hoffmann-La Roche | 4-substituted pyridin-3-yl-carboxamide compounds and methods of use |
| CN102625807B (zh) * | 2009-09-08 | 2016-03-09 | 霍夫曼-拉罗奇有限公司 | 4-取代的吡啶-3-基-甲酰胺化合物和使用方法 |
| AR081315A1 (es) | 2010-03-10 | 2012-08-08 | Incyte Corp | Derivados heterociclicos de piperidin y pirimidin -4-il-azetidina, una forma cristalina de la sal del acido acetonitriladipico de un derivado pirimidinico, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de enfermedades relacionadas con la inhibicion de jak-1, t |
| AU2011237936A1 (en) * | 2010-04-07 | 2012-10-11 | F. Hoffmann-La Roche Ag | Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use |
| WO2011136319A1 (ja) * | 2010-04-30 | 2011-11-03 | 国立大学法人 東京大学 | 抗がん剤 |
| ME02445B (me) | 2010-05-21 | 2016-09-20 | Incyte Holdings Corp | Topikalna formulacija za inhibiciju jak-a |
| WO2012004217A1 (en) * | 2010-07-06 | 2012-01-12 | Novartis Ag | Cyclic ether compounds useful as kinase inhibitors |
| AR083933A1 (es) | 2010-11-19 | 2013-04-10 | Incyte Corp | Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak |
| US9034884B2 (en) | 2010-11-19 | 2015-05-19 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors |
| JP2014506915A (ja) * | 2011-03-04 | 2014-03-20 | ノバルティス アーゲー | キナーゼ阻害剤としての四置換シクロヘキシル化合物 |
| UY33930A (es) * | 2011-03-04 | 2012-10-31 | Novartis Ag | Inhibidores novedosos de quinasas |
| WO2012148775A1 (en) | 2011-04-29 | 2012-11-01 | Amgen Inc. | Bicyclic pyridazine compounds as pim inhibitors |
| PE20140832A1 (es) | 2011-06-20 | 2014-07-14 | Incyte Corp | Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak |
| US9416132B2 (en) | 2011-07-21 | 2016-08-16 | Tolero Pharmaceuticals, Inc. | Substituted imidazo[1,2-b]pyridazines as protein kinase inhibitors |
| CN102924445B (zh) * | 2011-08-11 | 2015-07-08 | 上海吉铠医药科技有限公司 | Pim激酶抑制剂及其制备方法与在制药中的应用 |
| TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物 |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| JP6120861B2 (ja) | 2011-09-27 | 2017-04-26 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | ピラゾール−４−イル−ヘテロシクリル−カルボキサミド化合物と使用方法 |
| US9193733B2 (en) | 2012-05-18 | 2015-11-24 | Incyte Holdings Corporation | Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors |
| KR20150013548A (ko) * | 2012-05-21 | 2015-02-05 | 노파르티스 아게 | 키나제 억제제로서의 신규 고리-치환된 n-피리디닐 아미드 |
| WO2014033631A1 (en) * | 2012-08-31 | 2014-03-06 | Novartis Ag | N-(3-pyridyl) biarylamides as kinase inhibitors |
| WO2014033630A1 (en) * | 2012-08-31 | 2014-03-06 | Novartis Ag | Novel aminothiazole carboxamides as kinase inhibitors |
| RS60202B1 (sr) * | 2012-09-26 | 2020-06-30 | Hoffmann La Roche | Jedinjenja cikličnog etra pirazol-4-il-heterociklil-karboksamida i postupci primene |
| CA3178452A1 (en) | 2012-11-15 | 2014-05-22 | Incyte Holdings Corporation | Sustained-release dosage forms of ruxolitinib |
| 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 |
| LT3489239T (lt) | 2013-03-06 | 2022-03-10 | Incyte Holdings Corporation | Jak inhibitoriaus gamybos būdai ir tarpiniai junginiai |
| MY195091A (en) | 2013-08-07 | 2023-01-10 | Incyte Corp | Sustained Release Dosage Forms for a JAK1 Inhibitor |
| CN105658653A (zh) * | 2013-08-23 | 2016-06-08 | 因赛特公司 | 可用作pim激酶抑制剂的呋喃并-和噻吩并-吡啶甲酰胺化合物 |
| WO2015184305A1 (en) | 2014-05-30 | 2015-12-03 | Incyte Corporation | TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1 |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| US9822124B2 (en) | 2014-07-14 | 2017-11-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors |
| US9540347B2 (en) | 2015-05-29 | 2017-01-10 | Incyte Corporation | Pyridineamine compounds useful as Pim kinase inhibitors |
| AR105967A1 (es) | 2015-09-09 | 2017-11-29 | Incyte Corp | Sales de un inhibidor de pim quinasa |
| WO2017059251A1 (en) | 2015-10-02 | 2017-04-06 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| CA3075985A1 (en) * | 2017-09-20 | 2019-03-28 | Lead Discovery Center Gmbh | Coumarin derivatives, processes for their preparation and uses thereof for the treatment of cancer |
| US10596161B2 (en) | 2017-12-08 | 2020-03-24 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| WO2019111218A1 (en) | 2017-12-08 | 2019-06-13 | Cadila Healthcare Limited | Novel heterocyclic compounds as irak4 inhibitors |
| WO2019152374A1 (en) | 2018-01-30 | 2019-08-08 | Incyte Corporation | Processes for preparing (1 -(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one) |
| MX2020010322A (es) | 2018-03-30 | 2022-11-30 | Incyte Corp | Tratamiento de la hidradenitis supurativa mediante el uso de inhibidores de actividad de la cinasa janus (jak). |
| CN112236139A (zh) | 2018-04-13 | 2021-01-15 | 大日本住友制药肿瘤公司 | 用于治疗骨髓增殖性肿瘤和与癌症相关的纤维化的pim激酶抑制剂 |
| WO2020167990A1 (en) | 2019-02-12 | 2020-08-20 | Tolero Pharmaceuticals, Inc. | Formulations comprising heterocyclic protein kinase inhibitors |
| CN110452164B (zh) * | 2019-09-10 | 2022-07-22 | 上海皓鸿生物医药科技有限公司 | Pim447关键中间体的制备方法 |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| WO2024097653A1 (en) | 2022-10-31 | 2024-05-10 | Sumitomo Pharma America, Inc. | Pim1 inhibitor for treating myeloproliferative neoplasms |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7223759B2 (en) | 2003-09-15 | 2007-05-29 | Anadys Pharmaceuticals, Inc. | Antibacterial 3,5-diaminopiperidine-substituted aromatic and heteroaromatic compounds |
| TW200523252A (en) * | 2003-10-31 | 2005-07-16 | Takeda Pharmaceutical | Pyridine compounds |
| CA2613162A1 (en) * | 2005-06-28 | 2007-01-04 | Takeda Cambridge Limited | Heterocyclic non-peptide gnrh antagonists |
| RU2008122967A (ru) * | 2005-11-10 | 2009-12-20 | Шеринг Корпорейшн (US) | Имидазопиразины в качестве ингибиторов протеинкиназ |
| JP5182088B2 (ja) * | 2006-04-19 | 2013-04-10 | アステラス製薬株式会社 | アゾールカルボキサミド誘導体 |
| WO2008054701A1 (en) * | 2006-10-31 | 2008-05-08 | Schering Corporation | 2-aminothiazole-4-carboxylic amides as protein kinase inhibitors |
| AU2007314342B2 (en) * | 2006-10-31 | 2013-02-21 | Merck Sharp & Dohme Corp. | Anilinopiperazine Derivatives and methods of use thereof |
| EP2078004B1 (en) * | 2006-10-31 | 2015-02-25 | Merck Sharp & Dohme Corp. | 2-aminothiazole-4-carboxylic amides as protein kinase inhibitors |
| MX2009009304A (es) * | 2007-03-01 | 2009-11-18 | Novartis Ag | Inhibidores de cinasa pim y metodos para su uso. |
-
2009
- 2009-02-27 AR ARP090100684A patent/AR070531A1/es not_active Application Discontinuation
- 2009-02-27 PE PE2009000308A patent/PE20091577A1/es not_active Application Discontinuation
- 2009-02-27 UY UY031679A patent/UY31679A1/es not_active Application Discontinuation
- 2009-03-02 TW TW098106739A patent/TW200942536A/zh unknown
- 2009-03-02 CL CL2009000483A patent/CL2009000483A1/es unknown
- 2009-03-03 ES ES09717066.6T patent/ES2443496T3/es active Active
- 2009-03-03 EP EP09717066.6A patent/EP2262802B1/en active Active
- 2009-03-03 AU AU2009221134A patent/AU2009221134B2/en not_active Expired - Fee Related
- 2009-03-03 BR BRPI0909102A patent/BRPI0909102A2/pt not_active IP Right Cessation
- 2009-03-03 CA CA2717388A patent/CA2717388A1/en not_active Abandoned
- 2009-03-03 CN CN200980115821.7A patent/CN102015701B/zh active Active
- 2009-03-03 EP EP13154157.5A patent/EP2596790B1/en active Active
- 2009-03-03 ES ES13154157.5T patent/ES2562306T3/es active Active
- 2009-03-03 JP JP2010549127A patent/JP5412448B2/ja active Active
- 2009-03-03 KR KR1020107022008A patent/KR20100120709A/ko not_active Application Discontinuation
- 2009-03-03 CN CN201410286911.5A patent/CN104098559A/zh active Pending
- 2009-03-03 WO PCT/EP2009/052506 patent/WO2009109576A1/en active Application Filing
- 2009-03-03 EA EA201001412A patent/EA201001412A1/ru unknown
- 2009-03-03 MX MX2010009739A patent/MX2010009739A/es not_active Application Discontinuation
-
2010
- 2010-08-27 ZA ZA2010/06128A patent/ZA201006128B/en unknown
- 2010-08-30 IL IL207865A patent/IL207865A0/en unknown
- 2010-09-02 MA MA33140A patent/MA32135B1/fr unknown
- 2010-09-03 EC EC2010010447A patent/ECSP10010447A/es unknown
- 2010-09-07 CO CO10110544A patent/CO6290687A2/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| KR20100120709A (ko) | 2010-11-16 |
| ZA201006128B (en) | 2011-10-26 |
| AU2009221134B2 (en) | 2012-02-23 |
| EA201001412A1 (ru) | 2011-06-30 |
| PE20091577A1 (es) | 2009-11-05 |
| CN102015701B (zh) | 2014-07-23 |
| AU2009221134A1 (en) | 2009-09-11 |
| CO6290687A2 (es) | 2011-06-20 |
| JP5412448B2 (ja) | 2014-02-12 |
| MX2010009739A (es) | 2010-09-28 |
| TW200942536A (en) | 2009-10-16 |
| CA2717388A1 (en) | 2009-09-11 |
| CN102015701A (zh) | 2011-04-13 |
| BRPI0909102A2 (pt) | 2019-01-15 |
| ECSP10010447A (es) | 2010-10-30 |
| CL2009000483A1 (es) | 2010-02-19 |
| UY31679A1 (es) | 2009-09-30 |
| EP2596790B1 (en) | 2015-12-09 |
| MA32135B1 (fr) | 2011-03-01 |
| IL207865A0 (en) | 2010-12-30 |
| JP2011513363A (ja) | 2011-04-28 |
| ES2443496T3 (es) | 2014-02-19 |
| ES2562306T3 (es) | 2016-03-03 |
| EP2262802A1 (en) | 2010-12-22 |
| EP2596790A1 (en) | 2013-05-29 |
| WO2009109576A1 (en) | 2009-09-11 |
| CN104098559A (zh) | 2014-10-15 |
| EP2262802B1 (en) | 2013-10-23 |
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