CN103687858B - 作为mknk1激酶抑制剂的氨基取代的咪唑并哒嗪 - Google Patents
作为mknk1激酶抑制剂的氨基取代的咪唑并哒嗪 Download PDFInfo
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- CN103687858B CN103687858B CN201280035372.7A CN201280035372A CN103687858B CN 103687858 B CN103687858 B CN 103687858B CN 201280035372 A CN201280035372 A CN 201280035372A CN 103687858 B CN103687858 B CN 103687858B
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- amino
- imidazo
- pyridazin
- benzofuran
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- 0 CCN(C)*CCC*(C)=CC Chemical compound CCN(C)*CCC*(C)=CC 0.000 description 5
- REAUMEFIVWHGEV-QGZVFWFLSA-N COc1nccc2c1cc(-c1cnc(cc3)[n]1nc3NC[C@H](c1ccccc1)O)[o]2 Chemical compound COc1nccc2c1cc(-c1cnc(cc3)[n]1nc3NC[C@H](c1ccccc1)O)[o]2 REAUMEFIVWHGEV-QGZVFWFLSA-N 0.000 description 1
- BZRPUMWQSFSNSM-UHFFFAOYSA-N Cc1cc2ncc(-c3cc(cccc4)c4[o]3)[n]2nc1Cl Chemical compound Cc1cc2ncc(-c3cc(cccc4)c4[o]3)[n]2nc1Cl BZRPUMWQSFSNSM-UHFFFAOYSA-N 0.000 description 1
- LTPYMDGHUGZUBZ-UHFFFAOYSA-N Nc1cc(nccc2)c2[o]1 Chemical compound Nc1cc(nccc2)c2[o]1 LTPYMDGHUGZUBZ-UHFFFAOYSA-N 0.000 description 1
- AEWCZIWKJPNHNP-SFHVURJKSA-N O[C@@H](CNc(cc1)n[n]2c1ncc2-c1cc(cccc2)c2[o]1)c1ccccc1 Chemical compound O[C@@H](CNc(cc1)n[n]2c1ncc2-c1cc(cccc2)c2[o]1)c1ccccc1 AEWCZIWKJPNHNP-SFHVURJKSA-N 0.000 description 1
- RGXKEDZRUAEVNO-KRWDZBQOSA-N O[C@@H](CNc(cc1)n[n]2c1ncc2-c1cc2ccccc2[o]1)c1cnccc1 Chemical compound O[C@@H](CNc(cc1)n[n]2c1ncc2-c1cc2ccccc2[o]1)c1cnccc1 RGXKEDZRUAEVNO-KRWDZBQOSA-N 0.000 description 1
Classifications
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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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
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- A61P13/10—Drugs for disorders of the urinary system of the bladder
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P35/04—Antineoplastic agents specific for metastasis
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- Health & Medical Sciences (AREA)
- Chemical & Material 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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Endocrinology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pulmonology (AREA)
- Neurosurgery (AREA)
- Transplantation (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pain & Pain Management (AREA)
- Biomedical Technology (AREA)
- Reproductive Health (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11166426.4 | 2011-05-17 | ||
| EP11166426 | 2011-05-17 | ||
| PCT/EP2012/058931 WO2012156367A1 (en) | 2011-05-17 | 2012-05-14 | Amino-substituted imidazopyridazines as mknk1 kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103687858A CN103687858A (zh) | 2014-03-26 |
| CN103687858B true CN103687858B (zh) | 2017-11-21 |
Family
ID=46124340
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280035372.7A Expired - Fee Related CN103687858B (zh) | 2011-05-17 | 2012-05-14 | 作为mknk1激酶抑制剂的氨基取代的咪唑并哒嗪 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20140288069A1 (https=) |
| EP (1) | EP2710004A1 (https=) |
| JP (1) | JP6121991B2 (https=) |
| CN (1) | CN103687858B (https=) |
| CA (1) | CA2836203A1 (https=) |
| WO (1) | WO2012156367A1 (https=) |
Families Citing this family (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012163942A1 (en) * | 2011-06-01 | 2012-12-06 | Bayer Intellectual Property Gmbh | Substituted aminoimidazopyridazines |
| UA117092C2 (uk) | 2011-09-06 | 2018-06-25 | Байєр Інтеллектуал Проперті Гмбх | Амінозаміщені імідазопіридазини |
| CA2849345A1 (en) * | 2011-09-23 | 2013-03-28 | Bayer Intellectual Property Gmbh | Substituted imidazopyridazines |
| CN104114559B (zh) * | 2011-12-12 | 2016-08-24 | 拜耳知识产权有限责任公司 | 氨基取代的咪唑并哒嗪 |
| ES2663609T3 (es) | 2012-03-29 | 2018-04-16 | Bayer Intellectual Property Gmbh | Imidazopiridazinas amino-sustituidas |
| EP2834245B1 (en) * | 2012-04-04 | 2017-12-13 | Bayer Pharma Aktiengesellschaft | Amino-substituted imidazopyridazines |
| RS58514B1 (sr) | 2012-06-13 | 2019-04-30 | Incyte Holdings Corp | Supstituisana triciklična jedinjenja kao inhibitori fgfr |
| ES2646916T3 (es) | 2012-11-19 | 2017-12-18 | Bayer Pharma Aktiengesellschaft | Aminoimidazopiridazinas como inhibidores de MKNK1 cinasa |
| JP6510419B2 (ja) * | 2012-12-17 | 2019-05-08 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung | 液晶ディスプレイ、およびホメオトロピック配列を有する液晶媒体 |
| ES2649156T3 (es) | 2013-01-14 | 2018-01-10 | Incyte Holdings Corporation | Compuestos bicíclicos de carboxamida aromática útiles como inhibidores de quinasas Pim |
| PE20191245A1 (es) | 2013-01-15 | 2019-09-18 | Incyte Holdings Corp | Compuestos de tiazolcarboxamidas y piridinacarboxamida utiles como inhibidores de quinasa pim |
| WO2014118135A1 (en) * | 2013-01-30 | 2014-08-07 | Bayer Pharma Aktiengesellschaft | Amidoimidazopyridazines as mknk-1 kinase inhibitors |
| CA2899662A1 (en) | 2013-02-01 | 2014-08-07 | Bayer Pharma Aktiengesellschaft | Substituted pyrazolopyrimidinylamino-indazoles |
| HK1212699A1 (zh) * | 2013-02-20 | 2016-06-17 | 拜耳医药股份公司 | 作为mknk1抑制剂的取代的咪唑并[1,2-b]哒嗪类化合物 |
| PH12015502383B1 (en) | 2013-04-19 | 2023-02-03 | Incyte Holdings Corp | Bicyclic heterocycles as fgfr inhibitors |
| EA201690458A1 (ru) | 2013-08-23 | 2016-07-29 | Инсайт Корпорейшн | Фуро- и тиенопиридинкарбоксамиды, используемые в качестве ингибиторов pim-киназы |
| CN105899512A (zh) | 2014-01-09 | 2016-08-24 | 拜耳医药股份公司 | 可用于治疗过度增殖性和/或血管生成疾病的酰胺基团取代的咪唑并哒嗪 |
| US9822124B2 (en) | 2014-07-14 | 2017-11-21 | 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 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| TWI712601B (zh) | 2015-02-20 | 2020-12-11 | 美商英塞特公司 | 作為fgfr抑制劑之雙環雜環 |
| EP3285809B1 (en) | 2015-04-20 | 2019-09-11 | eFFECTOR Therapeutics, Inc. | Inhibitors of immune checkpoint modulators for use in treating cancer and infections |
| WO2016196244A1 (en) | 2015-05-29 | 2016-12-08 | 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 |
| US9920032B2 (en) | 2015-10-02 | 2018-03-20 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| WO2017117052A1 (en) | 2015-12-31 | 2017-07-06 | Effector Therapeutics, Inc. | Mnk biomarkers and uses thereof |
| WO2017157418A1 (en) | 2016-03-15 | 2017-09-21 | Bayer Pharma Aktiengesellschaft | Combination of mknk1-inhibitors |
| US20180072741A1 (en) | 2016-09-09 | 2018-03-15 | Incyte Corporation | Pyrazolopyrimidine compounds and uses thereof |
| WO2018049214A1 (en) | 2016-09-09 | 2018-03-15 | Incyte Corporation | Pyrazolopyridine derivatives as hpk1 modulators and uses thereof for the treatment of cancer |
| CN115819417A (zh) | 2016-09-09 | 2023-03-21 | 因赛特公司 | 作为hpk1调节剂的吡唑并吡啶衍生物及其用于治疗癌症的用途 |
| WO2018152220A1 (en) | 2017-02-15 | 2018-08-23 | Incyte Corporation | Pyrazolopyridine compounds and uses thereof |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| US10722495B2 (en) | 2017-09-08 | 2020-07-28 | Incyte Corporation | Cyanoindazole compounds and uses thereof |
| WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| US10745388B2 (en) | 2018-02-20 | 2020-08-18 | Incyte Corporation | Indazole compounds and uses thereof |
| US10752635B2 (en) | 2018-02-20 | 2020-08-25 | Incyte Corporation | Indazole compounds and uses thereof |
| EP3755703B1 (en) | 2018-02-20 | 2022-05-04 | Incyte Corporation | N-(phenyl)-2-(phenyl)pyrimidine-4-carboxamide derivatives and related compounds as hpk1 inhibitors for treating cancer |
| US11299473B2 (en) | 2018-04-13 | 2022-04-12 | Incyte Corporation | Benzimidazole and indole compounds and uses thereof |
| AU2019262579B2 (en) | 2018-05-04 | 2024-09-12 | Incyte Corporation | Salts of an FGFR inhibitor |
| HRP20241288T1 (hr) | 2018-05-04 | 2024-12-06 | Incyte Corporation | Čvrsti oblici fgfr inhibitora i postupci za njihovu proizvodnju |
| US10899755B2 (en) | 2018-08-08 | 2021-01-26 | Incyte Corporation | Benzothiazole compounds and uses thereof |
| WO2020068729A1 (en) | 2018-09-25 | 2020-04-02 | Incyte Corporation | Pyrazolo[4,3-d]pyrimidine compounds as alk2 abd/or fgfr modulators |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| BR112022002059A2 (pt) | 2019-08-06 | 2022-06-07 | Incyte Corp | Formas sólidas de um inibidor de hpk1 |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| CA3157361A1 (en) | 2019-10-14 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| JP7832891B2 (ja) | 2019-12-04 | 2026-03-18 | インサイト・コーポレイション | Fgfr阻害剤の誘導体 |
| CA3163875A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2022221170A1 (en) | 2021-04-12 | 2022-10-20 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| US11939331B2 (en) | 2021-06-09 | 2024-03-26 | Incyte Corporation | Tricyclic heterocycles as FGFR inhibitors |
| CA3220155A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
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| US20070093490A1 (en) * | 2005-09-02 | 2007-04-26 | Olaf Prien | Substituted imidazo[1,2b]pyridazines as kinase inhibitors, their preparation and use as medicaments |
| WO2007147646A1 (de) * | 2006-06-21 | 2007-12-27 | Bayer Schering Pharma Aktiengesellschaft | OXO-SUBSTITUIERTE IMIDAZO[1,2b]PYRIDAZINE, DEREN HERSTELLUNG UND VERWENDUNG ALS ARZNEIMITTEL |
| WO2008030579A2 (en) * | 2006-09-07 | 2008-03-13 | Biogen Idec Ma Inc. | Irak modulators for treating an inflammatory condition, cell proliferative disorder, immune disorder |
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| AR064420A1 (es) | 2006-12-21 | 2009-04-01 | Alcon Mfg Ltd | Composiciones farmaceuticas oftalmicas que comprenden una cantidad efectiva de analogos de 6-aminoimidazo[1,2b]piridazinas, utiles para el tratamiento del glaucoma y/o controlar la presion intraocular normal o elevada(iop). |
| EP2217601A1 (en) | 2007-11-08 | 2010-08-18 | Centro Nacional de Investigaciones Oncológicas (CNIO) | Imidazopyridazines for use as protein kinase inhibitors |
-
2012
- 2012-05-14 US US14/118,519 patent/US20140288069A1/en not_active Abandoned
- 2012-05-14 CN CN201280035372.7A patent/CN103687858B/zh not_active Expired - Fee Related
- 2012-05-14 EP EP12721826.1A patent/EP2710004A1/en not_active Withdrawn
- 2012-05-14 CA CA2836203A patent/CA2836203A1/en not_active Abandoned
- 2012-05-14 WO PCT/EP2012/058931 patent/WO2012156367A1/en not_active Ceased
- 2012-05-14 JP JP2014510768A patent/JP6121991B2/ja active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070093490A1 (en) * | 2005-09-02 | 2007-04-26 | Olaf Prien | Substituted imidazo[1,2b]pyridazines as kinase inhibitors, their preparation and use as medicaments |
| WO2007147646A1 (de) * | 2006-06-21 | 2007-12-27 | Bayer Schering Pharma Aktiengesellschaft | OXO-SUBSTITUIERTE IMIDAZO[1,2b]PYRIDAZINE, DEREN HERSTELLUNG UND VERWENDUNG ALS ARZNEIMITTEL |
| WO2008030579A2 (en) * | 2006-09-07 | 2008-03-13 | Biogen Idec Ma Inc. | Irak modulators for treating an inflammatory condition, cell proliferative disorder, immune disorder |
Also Published As
| Publication number | Publication date |
|---|---|
| JP6121991B2 (ja) | 2017-04-26 |
| JP2014513704A (ja) | 2014-06-05 |
| CN103687858A (zh) | 2014-03-26 |
| WO2012156367A1 (en) | 2012-11-22 |
| EP2710004A1 (en) | 2014-03-26 |
| US20140288069A1 (en) | 2014-09-25 |
| CA2836203A1 (en) | 2012-11-22 |
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