EA019554B1 - Аминопиразольное соединение - Google Patents
Аминопиразольное соединение Download PDFInfo
- Publication number
- EA019554B1 EA019554B1 EA201170831A EA201170831A EA019554B1 EA 019554 B1 EA019554 B1 EA 019554B1 EA 201170831 A EA201170831 A EA 201170831A EA 201170831 A EA201170831 A EA 201170831A EA 019554 B1 EA019554 B1 EA 019554B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- methyl
- chloro
- cells
- pyridazin
- morpholinomethyl
- Prior art date
Links
- -1 Amino pyrazole compound Chemical class 0.000 title claims description 48
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims abstract description 8
- 208000032839 leukemia Diseases 0.000 claims abstract description 6
- 206010006187 Breast cancer Diseases 0.000 claims abstract description 5
- 208000026310 Breast neoplasm Diseases 0.000 claims abstract description 5
- 208000034578 Multiple myelomas Diseases 0.000 claims abstract description 5
- 206010035226 Plasma cell myeloma Diseases 0.000 claims abstract description 5
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims abstract description 5
- 208000005017 glioblastoma Diseases 0.000 claims abstract description 5
- 206010060862 Prostate cancer Diseases 0.000 claims abstract description 4
- 150000001875 compounds Chemical class 0.000 claims description 66
- 150000003839 salts Chemical class 0.000 claims description 15
- VRHSUUSKSRWSLL-UHFFFAOYSA-N 2-(5-methyl-1H-pyrazol-3-yl)-8-(morpholin-4-ylmethyl)imidazo[1,2-b]pyridazin-6-amine Chemical compound CC1=CC(=NN1)C=1N=C2N(N=C(C=C2CN2CCOCC2)N)C=1 VRHSUUSKSRWSLL-UHFFFAOYSA-N 0.000 claims description 10
- 238000000034 method Methods 0.000 claims description 10
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 6
- 208000008601 Polycythemia Diseases 0.000 claims description 6
- 125000001064 morpholinomethyl group Chemical group [H]C([H])(*)N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H] 0.000 claims description 6
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- 208000003476 primary myelofibrosis Diseases 0.000 claims description 5
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims description 4
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims description 4
- 241000124008 Mammalia Species 0.000 claims description 4
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims description 4
- 208000014767 Myeloproliferative disease Diseases 0.000 claims description 4
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 208000037398 BCR-ABL1 negative atypical chronic myeloid leukemia Diseases 0.000 claims description 3
- 208000037379 Myeloid Chronic Atypical BCR-ABL Negative Leukemia Diseases 0.000 claims description 3
- 201000004892 atypical chronic myeloid leukemia Diseases 0.000 claims description 3
- 239000003085 diluting agent Substances 0.000 claims description 3
- 239000003937 drug carrier Substances 0.000 claims description 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 3
- 208000016595 therapy related acute myeloid leukemia and myelodysplastic syndrome Diseases 0.000 claims description 3
- 230000000694 effects Effects 0.000 claims description 2
- DCLWNTIANRACSB-UHFFFAOYSA-N imidazo[1,2-b]pyridazin-6-amine Chemical compound N1=C(N)C=CC2=NC=CN21 DCLWNTIANRACSB-UHFFFAOYSA-N 0.000 claims description 2
- LETVJWLLIMJADE-UHFFFAOYSA-N pyridazin-3-amine Chemical compound NC1=CC=CN=N1 LETVJWLLIMJADE-UHFFFAOYSA-N 0.000 claims description 2
- 230000008520 organization Effects 0.000 claims 1
- 230000001575 pathological effect Effects 0.000 claims 1
- 201000001514 prostate carcinoma Diseases 0.000 claims 1
- JVVRJMXHNUAPHW-UHFFFAOYSA-N 1h-pyrazol-5-amine Chemical class NC=1C=CNN=1 JVVRJMXHNUAPHW-UHFFFAOYSA-N 0.000 abstract description 2
- 206010028980 Neoplasm Diseases 0.000 abstract description 2
- 210000004027 cell Anatomy 0.000 description 101
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- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 28
- LOKCTEFSRHRXRJ-UHFFFAOYSA-I dipotassium trisodium dihydrogen phosphate hydrogen phosphate dichloride Chemical compound P(=O)(O)(O)[O-].[K+].P(=O)(O)([O-])[O-].[Na+].[Na+].[Cl-].[K+].[Cl-].[Na+] LOKCTEFSRHRXRJ-UHFFFAOYSA-I 0.000 description 27
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Classifications
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Biomedical Technology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US12285408P | 2008-12-16 | 2008-12-16 | |
| PCT/US2009/067056 WO2010074947A1 (en) | 2008-12-16 | 2009-12-08 | Amino pyrazole compound |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201170831A1 EA201170831A1 (ru) | 2011-12-30 |
| EA019554B1 true EA019554B1 (ru) | 2014-04-30 |
Family
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201170831A EA019554B1 (ru) | 2008-12-16 | 2009-12-08 | Аминопиразольное соединение |
Country Status (38)
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8105633B2 (en) * | 2006-03-01 | 2012-01-31 | Spintec Engineering Gmbh | Method and apparatus for extraction of arthropod gland |
| GB2435646A (en) * | 2006-03-01 | 2007-09-05 | Spin Tec Engineering Gmbh | Apparatus and method of extraction of an arthropod gland |
| US20110121485A1 (en) * | 2006-10-30 | 2011-05-26 | Spintec Engineering Gmbh | Method and apparatus for the manufacture of a fiber |
| JP2014511391A (ja) * | 2011-03-07 | 2014-05-15 | フォンダッツィオーネ・テレソン | Ｔｆｅｂリン酸化阻害剤およびその使用 |
| BR112013032360A2 (pt) * | 2011-06-15 | 2017-06-13 | Life And Brain Gmbh | compostos inibidores de glioblastoma e seu uso |
| JP6280546B2 (ja) | 2012-06-26 | 2018-02-14 | デル マー ファーマシューティカルズ | ジアンヒドロガラクチトール、ジアセチルジアンヒドロガラクチトール、ジブロモズルシトール、又はこれらの類似体若しくは誘導体を用いた、遺伝子多型又はａｈｉ１の調節不全若しくは変異を有する患者におけるチロシンキナーゼインヒビター抵抗性悪性腫瘍を処置するための方法 |
| PL400213A1 (pl) | 2012-08-01 | 2014-02-03 | Celon Pharma Spólka Z Ograniczona Odpowiedzialnoscia | Pochodne imidazo[1,2-b]pirydazyno-6-aminy jako inhibitory kinazy JAK-2 |
| MA40596B1 (fr) | 2014-08-11 | 2021-12-31 | Acerta Pharma Bv | Combinaisons thérapeutiques d'un inhibiteur de btk et d'un inhibiteur de bcl-2 |
| US20170239351A1 (en) | 2014-08-11 | 2017-08-24 | Acerta Pharma B.V. | Therapeutic Combinations of a BTK Inhibitor, a PI3K Inhibitor, a JAK-2 Inhibitor, a PD-1 Inhibitor, and/or a PD-L1 Inhibitor |
| TW201618773A (zh) | 2014-08-11 | 2016-06-01 | 艾森塔製藥公司 | Ｂｔｋ抑制劑、ｐｉ３ｋ抑制劑、ｊａｋ－２抑制劑、及／或ｃｄｋ４／６抑制劑的治療組合物 |
| EP3541817B1 (en) * | 2016-11-17 | 2020-12-23 | Bristol-Myers Squibb Company | Imidazopyridazine modulators of il-12, il-23 and/or ifn-alpha |
| WO2018167283A1 (en) | 2017-03-17 | 2018-09-20 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma associated neural remodeling |
| WO2018189335A1 (en) | 2017-04-13 | 2018-10-18 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma |
| KR102328682B1 (ko) | 2018-08-27 | 2021-11-18 | 주식회사 대웅제약 | 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물 |
| WO2020092015A1 (en) | 2018-11-02 | 2020-05-07 | University Of Rochester | Therapeutic mitigation of epithelial infection |
| CN110305140B (zh) | 2019-07-30 | 2020-08-04 | 上海勋和医药科技有限公司 | 二氢吡咯并嘧啶类选择性jak2抑制剂 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007009773A1 (en) * | 2005-07-21 | 2007-01-25 | Novartis Ag | Pyrazolo[1.5-a]pyrimidin-7-yl amine derivatives as protein kinase inhibitors |
| US20070083044A1 (en) * | 2005-10-06 | 2007-04-12 | Schering Corporation | Pyrazolopyrimidines as protein kinase inhibitors |
| WO2007044426A2 (en) * | 2005-10-06 | 2007-04-19 | Schering Corporation | Pyrazolopyrimidines as protein kinase inhibitors |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| NZ526472A (en) | 2000-12-21 | 2004-04-30 | Vertex Pharma | Pyrazole compounds useful as protein kinase inhibitors |
| JP2003137785A (ja) * | 2001-08-23 | 2003-05-14 | Takeda Chem Ind Ltd | Ｊｎｋ活性化阻害剤 |
| CA2467718C (en) | 2001-12-21 | 2011-04-26 | Anormed Inc. | Chemokine receptor binding heterocyclic compounds with enhanced efficacy |
| CA2598076A1 (en) | 2005-02-16 | 2006-08-24 | Astrazeneca Ab | Chemical compounds |
| PT1853588E (pt) | 2005-02-16 | 2008-08-25 | Astrazeneca Ab | Compostos químicos |
| PL1899329T3 (pl) * | 2005-07-01 | 2012-03-30 | Irm Llc | Pirymidyno-podstawione pochodne benzimidazolu jako inhibitory kinaz białkowych |
| KR20080080584A (ko) * | 2005-11-30 | 2008-09-04 | 버텍스 파마슈티칼스 인코포레이티드 | ｃ-Ｍｅｔ의 억제제 및 이의 용도 |
| US7989459B2 (en) | 2006-02-17 | 2011-08-02 | Pharmacopeia, Llc | Purinones and 1H-imidazopyridinones as PKC-theta inhibitors |
| CA2663091A1 (en) | 2006-09-07 | 2008-03-13 | Biogen Idec Ma Inc. | Modulators of interleukin-1 receptor-associated kinase |
| CN101522682A (zh) * | 2006-10-30 | 2009-09-02 | 诺瓦提斯公司 | 作为抗炎剂的杂环化合物 |
| WO2008129255A1 (en) * | 2007-04-18 | 2008-10-30 | Astrazeneca Ab | 5-aminopyrazol-3-yl-3h-imidazo [4,5-b] pyridine derivatives and their use for the treatment of cancer |
| CA2686485A1 (en) | 2007-05-23 | 2008-11-27 | Pharmacopeia, Llc | Purinones and 1h-imidazopyridinones as pkc-theta inhibitors |
| WO2009062059A2 (en) | 2007-11-08 | 2009-05-14 | Pharmacopeia, Inc. | Isomeric purinones and 1h-imidazopyridinones as pkc-theta inhibitors |
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2009
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- 2009-12-01 AR ARP090104627A patent/AR074240A1/es unknown
- 2009-12-01 JO JO2009459A patent/JO2833B1/en active
- 2009-12-04 TW TW098141606A patent/TWI440640B/zh not_active IP Right Cessation
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- 2009-12-08 HR HRP20120918AT patent/HRP20120918T1/hr unknown
- 2009-12-08 US US12/632,879 patent/US7897600B2/en not_active Expired - Fee Related
- 2009-12-08 EA EA201170831A patent/EA019554B1/ru not_active IP Right Cessation
- 2009-12-08 PE PE2011001082A patent/PE20110549A1/es not_active Application Discontinuation
- 2009-12-08 CN CN2009801481167A patent/CN102232075B/zh not_active Expired - Fee Related
- 2009-12-08 ES ES09795842T patent/ES2396617T3/es active Active
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- 2009-12-08 MX MX2011006441A patent/MX2011006441A/es active IP Right Grant
- 2009-12-08 UA UAA201107565A patent/UA104743C2/ru unknown
- 2009-12-08 KR KR1020117013705A patent/KR101300458B1/ko not_active Expired - Fee Related
- 2009-12-08 BR BRPI0923048A patent/BRPI0923048A2/pt not_active IP Right Cessation
- 2009-12-08 MY MYPI2011002704A patent/MY158691A/en unknown
- 2009-12-08 CA CA2744714A patent/CA2744714C/en not_active Expired - Fee Related
- 2009-12-08 DK DK09795842.5T patent/DK2379557T3/da active
- 2009-12-08 WO PCT/US2009/067056 patent/WO2010074947A1/en not_active Ceased
- 2009-12-08 SG SG2011044161A patent/SG172202A1/en unknown
- 2009-12-08 JP JP2011540809A patent/JP5509217B2/ja not_active Expired - Fee Related
- 2009-12-08 SI SI200930448T patent/SI2379557T1/sl unknown
- 2009-12-08 US US12/742,302 patent/US20100286139A1/en not_active Abandoned
- 2009-12-08 PT PT97958425T patent/PT2379557E/pt unknown
- 2009-12-08 EP EP09795842A patent/EP2379557B1/en not_active Not-in-force
- 2009-12-08 PL PL09795842T patent/PL2379557T3/pl unknown
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2011
- 2011-05-23 IL IL213065A patent/IL213065A0/en unknown
- 2011-05-27 ZA ZA2011/03942A patent/ZA201103942B/en unknown
- 2011-06-09 TN TN2011000292A patent/TN2011000292A1/fr unknown
- 2011-06-14 MA MA33943A patent/MA32900B1/fr unknown
- 2011-06-15 EC EC2011011132A patent/ECSP11011132A/es unknown
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- 2011-06-17 CR CR20110341A patent/CR20110341A/es not_active Application Discontinuation
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2012
- 2012-11-27 CY CY20121101146T patent/CY1113637T1/el unknown
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007009773A1 (en) * | 2005-07-21 | 2007-01-25 | Novartis Ag | Pyrazolo[1.5-a]pyrimidin-7-yl amine derivatives as protein kinase inhibitors |
| US20070083044A1 (en) * | 2005-10-06 | 2007-04-12 | Schering Corporation | Pyrazolopyrimidines as protein kinase inhibitors |
| WO2007044426A2 (en) * | 2005-10-06 | 2007-04-19 | Schering Corporation | Pyrazolopyrimidines as protein kinase inhibitors |
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