CN101600718B - 咪唑并[1,2-b]哒嗪和吡唑并[1,5-a]嘧啶衍生物及其作为蛋白激酶抑制剂的用途 - Google Patents
咪唑并[1,2-b]哒嗪和吡唑并[1,5-a]嘧啶衍生物及其作为蛋白激酶抑制剂的用途 Download PDFInfo
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- CN101600718B CN101600718B CN2007800412832A CN200780041283A CN101600718B CN 101600718 B CN101600718 B CN 101600718B CN 2007800412832 A CN2007800412832 A CN 2007800412832A CN 200780041283 A CN200780041283 A CN 200780041283A CN 101600718 B CN101600718 B CN 101600718B
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- 0 CCCC1CCC(CC*C)CC1 Chemical compound CCCC1CCC(CC*C)CC1 0.000 description 6
- QUMFENBLHSNPNH-UHFFFAOYSA-N CCC(CNc(cc1)n[n]2c1ncc2-c1cc(OC(F)(F)F)ccc1)N1CCN(C)CC1 Chemical compound CCC(CNc(cc1)n[n]2c1ncc2-c1cc(OC(F)(F)F)ccc1)N1CCN(C)CC1 QUMFENBLHSNPNH-UHFFFAOYSA-N 0.000 description 1
- HZOZGTVOMTVWDK-UHFFFAOYSA-N CCN1CCC(CNC(C=C2)=NN3C2=NCC3(C)c2cc(OC(F)(F)F)ccc2)CC1 Chemical compound CCN1CCC(CNC(C=C2)=NN3C2=NCC3(C)c2cc(OC(F)(F)F)ccc2)CC1 HZOZGTVOMTVWDK-UHFFFAOYSA-N 0.000 description 1
- IKJWCJBQADONGF-UHFFFAOYSA-N CN1CCC(CNc(cc2)n[n]3c2ncc3-c(cc(cc2)OC(F)(F)F)c2O)CC1 Chemical compound CN1CCC(CNc(cc2)n[n]3c2ncc3-c(cc(cc2)OC(F)(F)F)c2O)CC1 IKJWCJBQADONGF-UHFFFAOYSA-N 0.000 description 1
- MHXGEROHKGDZGO-UHFFFAOYSA-N CN1CCC(CNc(cc2)n[n]3c2ncc3-c2cccc(OC(F)(F)F)c2)CC1 Chemical compound CN1CCC(CNc(cc2)n[n]3c2ncc3-c2cccc(OC(F)(F)F)c2)CC1 MHXGEROHKGDZGO-UHFFFAOYSA-N 0.000 description 1
- SQZQTKQCWIKGPB-UHFFFAOYSA-N COc(ccc(C(F)(F)F)c1)c1-c1cnc(cc2)[n]1nc2Cl Chemical compound COc(ccc(C(F)(F)F)c1)c1-c1cnc(cc2)[n]1nc2Cl SQZQTKQCWIKGPB-UHFFFAOYSA-N 0.000 description 1
- UWDLNRUFHRYMSE-UHFFFAOYSA-N Cc1cc(N)nnc1Cl Chemical compound Cc1cc(N)nnc1Cl UWDLNRUFHRYMSE-UHFFFAOYSA-N 0.000 description 1
- VVYQQZDXZWTXIU-UHFFFAOYSA-N Cc1cc2[n]cc(-c3cc(OC(F)(F)F)ccc3)[n]2nc1NCC1CCN(C)CC1 Chemical compound Cc1cc2[n]cc(-c3cc(OC(F)(F)F)ccc3)[n]2nc1NCC1CCN(C)CC1 VVYQQZDXZWTXIU-UHFFFAOYSA-N 0.000 description 1
- VFPVLQQNCLDGTI-UHFFFAOYSA-N Cc1cc2ncc[n]2nc1Cl Chemical compound Cc1cc2ncc[n]2nc1Cl VFPVLQQNCLDGTI-UHFFFAOYSA-N 0.000 description 1
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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
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US86456606P | 2006-11-06 | 2006-11-06 | |
| US60/864,566 | 2006-11-06 | ||
| US89252307P | 2007-03-01 | 2007-03-01 | |
| US60/892,523 | 2007-03-01 | ||
| US95798807P | 2007-08-24 | 2007-08-24 | |
| US60/957,988 | 2007-08-24 | ||
| PCT/US2007/083773 WO2008058126A2 (en) | 2006-11-06 | 2007-11-06 | Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101600718A CN101600718A (zh) | 2009-12-09 |
| CN101600718B true CN101600718B (zh) | 2013-07-03 |
Family
ID=39277096
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2007800412832A Active CN101600718B (zh) | 2006-11-06 | 2007-11-06 | 咪唑并[1,2-b]哒嗪和吡唑并[1,5-a]嘧啶衍生物及其作为蛋白激酶抑制剂的用途 |
Country Status (14)
| Country | Link |
|---|---|
| US (3) | US7750007B2 (enExample) |
| EP (1) | EP2086979B1 (enExample) |
| JP (1) | JP5357763B2 (enExample) |
| KR (1) | KR101546493B1 (enExample) |
| CN (1) | CN101600718B (enExample) |
| AU (1) | AU2007316417B2 (enExample) |
| BR (1) | BRPI0718029A2 (enExample) |
| CA (1) | CA2667487C (enExample) |
| MX (1) | MX2009004700A (enExample) |
| MY (1) | MY146474A (enExample) |
| NZ (1) | NZ576234A (enExample) |
| RU (1) | RU2487875C2 (enExample) |
| SG (1) | SG176461A1 (enExample) |
| WO (1) | WO2008058126A2 (enExample) |
Families Citing this family (118)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060063766A1 (en) | 2004-07-15 | 2006-03-23 | Molino Bruce F | Use of aryl- and heteroaryl-substituted tetrahydroisoquinolines to block reuptake of norepinephrine, dopamine, and serotonin |
| NZ594628A (en) * | 2005-10-07 | 2013-04-26 | Exelixis Inc | PYRIDOPYRIMIDINONE INHIBITORS OF PI3Ka |
| DK3184526T3 (en) | 2005-12-13 | 2019-01-14 | Incyte Holdings Corp | PYRROLO [2,3-D] PYRIMIDINE DERIVATIVES AS A JANUS-KINASE INHIBITOR |
| WO2008021781A1 (en) | 2006-08-07 | 2008-02-21 | Incyte Corporation | Triazolotriazines as kinase inhibitors |
| JP2010502716A (ja) * | 2006-09-07 | 2010-01-28 | バイオジェン・アイデック・エムエイ・インコーポレイテッド | インターロイキン1受容体関連キナーゼの調節物質 |
| JP2010506948A (ja) * | 2006-10-20 | 2010-03-04 | アイアールエム・リミテッド・ライアビリティ・カンパニー | C−kitおよびpdgfr受容体を調節するための組成物および方法 |
| CA2669991C (en) | 2006-11-22 | 2016-01-26 | Incyte Corporation | Imidazotriazines and imidazopyrimidines as kinase inhibitors |
| AR067326A1 (es) * | 2007-05-11 | 2009-10-07 | Novartis Ag | Imidazopiridinas y pirrolo -pirimidinas sustituidas como inhibidores de cinasa de lipido |
| EP2740731B1 (en) | 2007-06-13 | 2016-03-23 | Incyte Holdings Corporation | Crystalline salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
| FR2918061B1 (fr) | 2007-06-28 | 2010-10-22 | Sanofi Aventis | Derives de 6-cycloamino-3-(pyridin-4-yl)imidazo°1,2-b!- pyridazine,leur preparation et leur application en therapeutique. |
| CA2724842A1 (en) * | 2008-05-19 | 2009-11-26 | Sunovion Pharmaceuticals Inc. | Imidazo[1,2-a]pyridine compounds |
| CA2724742C (en) | 2008-05-21 | 2016-07-19 | Incyte Corporation | Salts of 2-fluoro-n-methyl-4-[7-(quinolin-6-yl-methyl)- imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide and processes related to preparing the same |
| AR071997A1 (es) * | 2008-06-04 | 2010-07-28 | Bristol Myers Squibb Co | Forma cristalina de 6-((4s)-2-metil-4-(2-naftil)-1,2,3,4-tetrahidroisoquinolin-7-il)piridazin-3-amina |
| US9156812B2 (en) | 2008-06-04 | 2015-10-13 | Bristol-Myers Squibb Company | Crystalline form of 6-[(4S)-2-methyl-4-(2-naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine |
| US8987251B2 (en) | 2008-08-19 | 2015-03-24 | Array Biopharma Inc. | Triazolopyridine compounds as PIM kinase inhibitors |
| TWI496779B (zh) * | 2008-08-19 | 2015-08-21 | Array Biopharma Inc | 作為pim激酶抑制劑之三唑吡啶化合物 |
| US8895550B2 (en) | 2008-08-19 | 2014-11-25 | Array Biopharma Inc. | Triazolopyridine compounds as PIM kinase inhibitors |
| US8557809B2 (en) * | 2008-08-19 | 2013-10-15 | Array Biopharma Inc. | Triazolopyridine compounds as PIM kinase inhibitors |
| ES2464461T3 (es) | 2008-09-22 | 2014-06-02 | Array Biopharma, Inc. | Compuestos de imidazo[1,2B]piridazina sustituidos como inhibidores de la TRK cinasa |
| CL2009001884A1 (es) * | 2008-10-02 | 2010-05-14 | Incyte Holdings Corp | Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco. |
| SG196855A1 (en) | 2008-10-22 | 2014-02-13 | Array Biopharma Inc | Substituted pyrazolo[1,5-a]pyrimidine compounds as trk kinase inhibitors |
| JP2012526823A (ja) | 2009-05-12 | 2012-11-01 | アルバニー モレキュラー リサーチ, インコーポレイテッド | アリール、ヘテロアリール、および複素環置換テトラヒドロイソキノリンならびにそれらの使用 |
| WO2010135581A1 (en) * | 2009-05-20 | 2010-11-25 | Cylene Pharmaceuticals, Inc. | Pyrazolopyrimidines and related heterocycles as kinase inhibitors |
| ES2487542T3 (es) * | 2009-05-22 | 2014-08-21 | Incyte Corporation | Derivados de N-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d]pirimidinas y pirrol-3-il-pirrolo[2,3-d]pirimidinas como inhibidores de cinasas Janus |
| WO2010135621A1 (en) * | 2009-05-22 | 2010-11-25 | Incyte Corporation | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| WO2011028685A1 (en) * | 2009-09-01 | 2011-03-10 | Incyte Corporation | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| WO2011090935A1 (en) * | 2010-01-19 | 2011-07-28 | Merck Sharp & Dohme Corp. | PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS mTOR INHIBITORS |
| ES2608329T3 (es) | 2010-02-03 | 2017-04-07 | Incyte Holdings Corporation | Imidazo[1,2-b][1,2,4]triazinas como inhibidores de c-Met |
| AR080151A1 (es) | 2010-02-09 | 2012-03-14 | Exelixis Inc | Metodos para tratar cancer usando inhibidores de piridopirimidinona de pi 3k y mtor en combinacion con inhibidores de autofagia |
| SMT201800137T1 (it) | 2010-03-10 | 2018-07-17 | Incyte Holdings Corp | Derivati di piperidin-4-il azetidina come inibitori di jak1 |
| CN102971326A (zh) * | 2010-04-28 | 2013-03-13 | 百时美施贵宝公司 | 咪唑并哒嗪化合物及其在癌症中的用途 |
| JP5656233B2 (ja) * | 2010-04-30 | 2015-01-21 | 国立大学法人 東京大学 | 抗がん剤 |
| AU2011256380C1 (en) | 2010-05-20 | 2016-09-08 | Array Biopharma Inc. | Macrocyclic compounds as Trk kinase inhibitors |
| PH12012502296B1 (en) | 2010-05-21 | 2017-10-06 | Incyte Holdings Corp | Topical formulation for a jak inhibitor |
| ES2536415T3 (es) | 2010-11-19 | 2015-05-25 | Incyte Corporation | Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK |
| SG190839A1 (en) | 2010-11-19 | 2013-07-31 | Incyte Corp | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| AU2012254082B2 (en) | 2011-02-25 | 2016-12-08 | Array Biopharma Inc. | Triazolopyridine compounds as PIM kinase inhibitors |
| CA2836203A1 (en) | 2011-05-17 | 2012-11-22 | Bayer Intellectual Property Gmbh | Amino-substituted imidazopyridazines as mknk1 kinase inhibitors |
| US9730929B2 (en) | 2011-06-01 | 2017-08-15 | Bayer Intellectual Property Gmbh | Substituted aminoimidazopyridazines |
| WO2012177606A1 (en) | 2011-06-20 | 2012-12-27 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
| HK1197063A1 (en) | 2011-06-22 | 2015-01-02 | 拜耳知识产权有限责任公司 | Heterocyclyl aminoimidazopyridazines |
| WO2013005041A1 (en) * | 2011-07-07 | 2013-01-10 | Centro Nacional De Investigaciones Oncológicas (Cnio) | Tricyclic heterocyclic compounds as kinase inhibitors |
| ES2834093T3 (es) | 2011-07-21 | 2021-06-16 | Sumitomo Dainippon Pharma Oncology Inc | Inhibidores de proteína quinasa heterocíclicos |
| WO2013024002A1 (en) * | 2011-08-12 | 2013-02-21 | F. Hoffmann-La Roche Ag | PYRAZOLO[3,4-c]PYRIDINE COMPOUNDS AND METHODS OF USE |
| 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 |
| UA117092C2 (uk) | 2011-09-06 | 2018-06-25 | Байєр Інтеллектуал Проперті Гмбх | Амінозаміщені імідазопіридазини |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| JP6174586B2 (ja) | 2011-09-23 | 2017-08-02 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH | 置換イミダゾピリダジン |
| KR20140078710A (ko) * | 2011-09-30 | 2014-06-25 | 온코디자인 에스.에이. | 거대고리 flt3 키나제 억제제 |
| ES2583477T3 (es) * | 2011-09-30 | 2016-09-21 | Ipsen Pharma S.A.S. | Inhibidores macrocíclicos de cinasa de LRRK2 |
| WO2013051672A1 (ja) * | 2011-10-04 | 2013-04-11 | 株式会社ヤクルト本社 | チアゾリジン誘導体又はその塩を有効成分とする医薬品 |
| ES2650915T3 (es) * | 2011-12-12 | 2018-01-23 | Bayer Intellectual Property Gmbh | Imidazopiridazinas amino-sustituidas |
| JP6173426B2 (ja) | 2012-03-29 | 2017-08-02 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH | アミノ置換イミダゾピリダジン |
| US10280168B2 (en) * | 2012-03-30 | 2019-05-07 | Agency For Science, Technology And Research | Bicyclic heteroaryl derivatives as MNK1 and MNK2 modulators and uses thereof |
| GB201205669D0 (en) * | 2012-03-30 | 2012-05-16 | Agency Science Tech & Res | Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof |
| CN104321326B (zh) * | 2012-04-04 | 2017-05-31 | 拜耳医药股份有限公司 | 氨基取代的咪唑并哒嗪 |
| WO2013173720A1 (en) | 2012-05-18 | 2013-11-21 | Incyte Corporation | Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| TWI585088B (zh) * | 2012-06-04 | 2017-06-01 | 第一三共股份有限公司 | 作爲激酶抑制劑之咪唑并[1,2-b]嗒衍生物 |
| SG11201408679XA (en) | 2012-06-26 | 2015-01-29 | Del Mar Pharmaceuticals | Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalactitol, dibromodulcitol, or analogs or derivatives thereof |
| PE20151157A1 (es) | 2012-11-15 | 2015-08-19 | Incyte Corp | Formas de dosificacion de ruxolitinib de liberacion sostenida |
| US9573954B2 (en) | 2012-11-16 | 2017-02-21 | University Health Network | Pyrazolopyrimidine compounds |
| US8871754B2 (en) | 2012-11-19 | 2014-10-28 | Irm Llc | Compounds and compositions for the treatment of parasitic diseases |
| US9783543B2 (en) | 2012-11-19 | 2017-10-10 | Bayer Pharma Aktiengesellschaft | Aminoimidazopyridazines |
| PT2925757T (pt) | 2012-11-19 | 2018-01-09 | Novartis Ag | Compostos e composições para o tratamento de doenças parasitárias |
| EP2943485B1 (en) | 2013-01-14 | 2017-09-20 | Incyte Holdings Corporation | Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors |
| HUE050215T2 (hu) | 2013-01-15 | 2020-11-30 | Incyte Holdings Corp | Pim kináz inhibitorokként hasznos tiazolkarboxamid és piridinkarboxamid vegyületek |
| EP2951181A1 (en) | 2013-01-30 | 2015-12-09 | Bayer Pharma Aktiengesellschaft | Amidoimidazopyridazines as mknk-1 kinase inhibitors |
| JP2016509036A (ja) | 2013-02-20 | 2016-03-24 | バイエル・ファルマ・アクティエンゲゼルシャフト | Mknk1阻害剤としての置換イミダゾ[1,2−b]ピリダジン |
| LT3489239T (lt) | 2013-03-06 | 2022-03-10 | Incyte Holdings Corporation | Jak inhibitoriaus gamybos būdai ir tarpiniai junginiai |
| EP2964230A4 (en) * | 2013-03-07 | 2016-10-26 | Califia Bio Inc | KINASEHEMMER WITH MIXED ABSTRACT AND TREATMENT PROCESS THEREWITH |
| CN105209040A (zh) * | 2013-03-15 | 2015-12-30 | 昂科迪塞恩股份有限公司 | 大环的盐可诱导的激酶抑制剂 |
| JP6023630B2 (ja) * | 2013-04-03 | 2016-11-09 | 株式会社ヤクルト本社 | チアゾロン誘導体 |
| US11491154B2 (en) | 2013-04-08 | 2022-11-08 | Dennis M. Brown | Therapeutic benefit of suboptimally administered chemical compounds |
| MX372671B (es) * | 2013-07-19 | 2020-04-23 | Onyx Therapeutics Inc | Inhibidores de proteasoma de epoxicetona peptídica en combinacion con inhibidores de cinasa pim para el tratamiento de canceres. |
| UA120499C2 (uk) | 2013-08-07 | 2019-12-26 | Інсайт Корпорейшн | Лікування захворювань із застосуванням лікарських форм з уповільненим вивільненням для інгібітора jak1 |
| TW201605866A (zh) | 2013-08-23 | 2016-02-16 | 英塞特公司 | 可用作pim激酶抑制劑之呋喃并-及噻吩并-吡啶甲醯胺化合物 |
| AR097543A1 (es) * | 2013-09-06 | 2016-03-23 | Lexicon Pharmaceuticals Inc | COMPUESTOS BASADOS EN IMIDAZO[1,2-b]PIRIDAZINA, COMPOSICIONES QUE LOS COMPRENDEN Y SUS MÉTODOS DE USO |
| EP3092242A1 (en) | 2014-01-09 | 2016-11-16 | Bayer Pharma Aktiengesellschaft | Amido-substituted imidazopyridazines useful in the treatment of hyper-proliferative and/or angiogenesis disorders |
| CN103864800A (zh) * | 2014-04-03 | 2014-06-18 | 定陶县友帮化工有限公司 | 6-氯咪唑并[1,2-b]哒嗪的合成方法 |
| 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 |
| GB201410817D0 (en) * | 2014-06-17 | 2014-07-30 | Ucb Biopharma Sprl And Katholieke Universiteit Leuven K U Leuven R & D | Therapeutic agents |
| WO2016010897A1 (en) | 2014-07-14 | 2016-01-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| WO2016042087A1 (en) * | 2014-09-17 | 2016-03-24 | Oncodesign S.A. | Macrocyclic rip2 kinase inhibitors |
| EP3699181B1 (en) | 2014-11-16 | 2023-03-01 | Array Biopharma, Inc. | Crystalline form of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate |
| US9540347B2 (en) | 2015-05-29 | 2017-01-10 | Incyte Corporation | Pyridineamine compounds useful as Pim kinase inhibitors |
| TWI734699B (zh) | 2015-09-09 | 2021-08-01 | 美商英塞特公司 | Pim激酶抑制劑之鹽 |
| WO2017059251A1 (en) | 2015-10-02 | 2017-04-06 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| US10724102B2 (en) | 2015-10-26 | 2020-07-28 | Loxo Oncology, Inc. | Point mutations in TRK inhibitor-resistant cancer and methods relating to the same |
| CA3017641C (en) | 2016-03-25 | 2023-12-12 | Charles J. Bieberich | Pim kinase inhibitors in combination with rna splicing modulators/inhibitors for treatment of cancers |
| SG11201808559PA (en) | 2016-04-04 | 2018-10-30 | Loxo Oncology Inc | Liquid formulations of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| PL3439663T3 (pl) | 2016-04-04 | 2024-11-18 | Loxo Oncology, Inc. | Sposoby leczenia nowotworów wieku dziecięcego |
| FI3800189T3 (fi) | 2016-05-18 | 2023-07-31 | Loxo Oncology Inc | (s)-n-(5-((r)-2-(2,5-difluorifenyyli)pyrrolidin-1-yyli)pyratsolo[1,5-a]pyrimidin-3-yyli)-3-hydroksipyrrolidiini-1-karboksamidin valmistaminen |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| SG11201909710XA (en) | 2017-04-21 | 2019-11-28 | Kyn Therapeutics | Indole ahr inhibitors and uses thereof |
| FI3661935T3 (fi) * | 2017-08-11 | 2023-01-13 | Kinaasin estäjinä käyttökelpoiset pyratsolipyrimidiinit | |
| CA3073051A1 (en) | 2017-08-17 | 2019-02-21 | Ikena Oncology, Inc. | Ahr inhibitors and uses thereof |
| US11319320B2 (en) | 2017-11-06 | 2022-05-03 | Snap Bio, Inc. | PIM kinase inhibitor compositions, methods, and uses thereof |
| WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| IL276302B2 (en) | 2018-01-30 | 2023-11-01 | Incyte Corp | Procedures for preparing [1-(3-fluoro-2-(trifluoromethyl(isonicotinyl}piperidine-4-one) |
| SMT202400306T1 (it) | 2018-03-30 | 2024-09-16 | Incyte Corp | Trattamento dell'idrosadenite suppurativa utilizzando inibitori di jak. |
| CA3095580A1 (en) | 2018-04-13 | 2019-10-17 | Sumitomo Dainippon Pharma Oncology, Inc. | Pim kinase inhibitors for treatment of myeloproliferative neoplasms and fibrosis associated with cancer |
| HUE072069T2 (hu) | 2019-02-12 | 2025-10-28 | Sumitomo Pharma America Inc | 2-((1R,4R)-4-((3-(3-(trifluormetil)fenil)imidazo[1,2- b]piridazin-6-il)amino)ciklohexil)propán-2-ol sósavas sójának kristályos formája |
| CR20220280A (es) | 2019-11-22 | 2022-09-02 | Incyte Corp | Terapia de combinación que comprende un inhibidor de alk2 y un inhibidor de jak2 |
| AU2020394424A1 (en) | 2019-11-26 | 2022-06-16 | Ikena Oncology, Inc. | Polymorphic carbazole derivatives and uses thereof |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| WO2022053838A1 (en) * | 2020-09-14 | 2022-03-17 | The University Of Sussex | Small molecule inhibitors of lemur tyrosine kinase 3 |
| WO2022140769A1 (en) * | 2020-12-22 | 2022-06-30 | Enliven Therapeutics, Inc. | Lactam (hetero)arylfusedpyrimidine derivatives as inhibitors of erbb2 |
| CN115991706A (zh) * | 2021-02-08 | 2023-04-21 | 杭州邦顺制药有限公司 | Pim激酶抑制剂 |
| US20250002491A1 (en) * | 2021-10-04 | 2025-01-02 | Forx Therapeutics Ag | N,n-dimethyl-4-(7-(n-(1-methylcyclopropyl)sulfamoyl)-imidazo[1,5-a]pyridin-5-yl)piperazine-1-carboxamide derivatives and the corresponding pyrazolo[1,5-a]pyridine derivatives as parg inhibitors for the treatment of cancer |
| CN116262753A (zh) * | 2021-12-13 | 2023-06-16 | 杭州邦顺制药有限公司 | 一种新颖的pim激酶抑制剂 |
| AU2023372386A1 (en) | 2022-10-31 | 2025-05-08 | Sumitomo Pharma America, Inc. | Pim1 inhibitor for treating myeloproliferative neoplasms |
| EP4434972A1 (en) * | 2023-03-22 | 2024-09-25 | Eberhard-Karls-Universität Tübingen | Atm kinase inhibitors |
| WO2025231117A1 (en) * | 2024-05-01 | 2025-11-06 | Nimbus Salacia, Inc. | Sik2 modulators and uses thereof |
| WO2025231112A1 (en) * | 2024-05-01 | 2025-11-06 | Nimbus Salacia, Inc. | Sik2 modulators and uses thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1798747A (zh) * | 2000-08-22 | 2006-07-05 | 葛兰素集团有限公司 | 为蛋白激酶抑制剂的稠合的吡唑衍生物 |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8719368D0 (en) * | 1987-08-15 | 1987-09-23 | Wellcome Found | Heterocyclic compounds |
| IL112248A0 (en) | 1994-01-25 | 1995-03-30 | Warner Lambert Co | Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them |
| SK133297A3 (en) | 1995-04-04 | 1998-07-08 | Glaxo Group Ltd | Imidazo[1,2-a]pyridine derivatives, pharmaceutical composition containing same and their use |
| US5747498A (en) | 1996-05-28 | 1998-05-05 | Pfizer Inc. | Alkynyl and azido-substituted 4-anilinoquinazolines |
| AR007857A1 (es) | 1996-07-13 | 1999-11-24 | Glaxo Group Ltd | Compuestos heterociclicos fusionados como inhibidores de proteina tirosina quinasa, sus metodos de preparacion, intermediarios uso en medicina ycomposiciones farmaceuticas que los contienen. |
| ID18494A (id) | 1996-10-02 | 1998-04-16 | Novartis Ag | Turunan pirazola leburan dan proses pembuatannya |
| EP0984692A4 (en) * | 1997-05-30 | 2001-02-21 | Merck & Co Inc | ANGIOGENESIS INHIBITORS |
| WO1999024440A1 (en) | 1997-11-11 | 1999-05-20 | Pfizer Products Inc. | Thienopyrimidine and thienopyridine derivatives useful as anticancer agents |
| BRPI0117360B8 (pt) | 2000-02-15 | 2021-07-06 | Upjohn Co | inibidores de proteína de quinase de 2-indolinona de pirrol substituído, seus sais e composições farmacêuticas compreendendo os mesmos |
| GB0119249D0 (en) * | 2001-08-07 | 2001-10-03 | Novartis Ag | Organic compounds |
| AU2003272548A1 (en) | 2002-09-16 | 2004-04-30 | Plexxikon, Inc. | Crystal structure of pim-1 kinase |
| NZ541151A (en) * | 2002-12-18 | 2008-09-26 | Vertex Pharma | Triazolopyridazines as protein kinase inhibitors |
| WO2007013673A1 (en) * | 2005-07-29 | 2007-02-01 | Astellas Pharma Inc. | Fused heterocycles as lck inhibitors |
| WO2007025090A2 (en) * | 2005-08-25 | 2007-03-01 | Kalypsys, Inc. | Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase |
| US7750000B2 (en) * | 2005-09-02 | 2010-07-06 | Bayer Schering Pharma Ag | Substituted imidazo[1,2b]pyridazines as kinase inhibitors, their preparation and use as medicaments |
| DE102005042742A1 (de) | 2005-09-02 | 2007-03-08 | Schering Ag | Substituierte Imidazo[1,2b]pyridazine als Kinase-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel |
| US20070132596A1 (en) * | 2005-10-05 | 2007-06-14 | Lg Home Products, Llc | Sound Privacy Machine and Methods of Use Thereof |
| US7776865B2 (en) * | 2005-10-06 | 2010-08-17 | Schering Corporation | Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors |
| EP1873157A1 (en) | 2006-06-21 | 2008-01-02 | Bayer Schering Pharma Aktiengesellschaft | Pyrazolopyrimidines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same |
| DE102006029447A1 (de) * | 2006-06-21 | 2007-12-27 | Bayer Schering Pharma Ag | Oxo-substituierte Imidazo[1,2b]pyridazine, deren Herstellung und Verwendung als Arzneimittel |
| EP1900739A1 (en) * | 2006-08-30 | 2008-03-19 | Cellzome Ag | Diazolodiazine derivatives as kinase inhibitors |
| JP2010502716A (ja) * | 2006-09-07 | 2010-01-28 | バイオジェン・アイデック・エムエイ・インコーポレイテッド | インターロイキン1受容体関連キナーゼの調節物質 |
| KR20090073121A (ko) | 2006-09-29 | 2009-07-02 | 노파르티스 아게 | Pi3k 지질 키나제 억제제로서의 피라졸로피리미딘 |
| CA2667962A1 (en) * | 2006-10-30 | 2008-05-08 | Novartis Ag | Heterocyclic compounds as antiinflammatory agents |
| US20120058997A1 (en) * | 2006-11-06 | 2012-03-08 | Supergen, Inc. | Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors |
| EP2217601A1 (en) * | 2007-11-08 | 2010-08-18 | Centro Nacional de Investigaciones Oncológicas (CNIO) | Imidazopyridazines for use as protein kinase inhibitors |
| ES2464461T3 (es) * | 2008-09-22 | 2014-06-02 | Array Biopharma, Inc. | Compuestos de imidazo[1,2B]piridazina sustituidos como inhibidores de la TRK cinasa |
-
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- 2007-11-06 US US11/935,959 patent/US7750007B2/en active Active
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1798747A (zh) * | 2000-08-22 | 2006-07-05 | 葛兰素集团有限公司 | 为蛋白激酶抑制剂的稠合的吡唑衍生物 |
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| CA2667487C (en) | 2017-04-04 |
| KR101546493B1 (ko) | 2015-08-21 |
| RU2487875C2 (ru) | 2013-07-20 |
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