JP2012082234A5 - - Google Patents
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- JP2012082234A5 JP2012082234A5 JP2012015831A JP2012015831A JP2012082234A5 JP 2012082234 A5 JP2012082234 A5 JP 2012082234A5 JP 2012015831 A JP2012015831 A JP 2012015831A JP 2012015831 A JP2012015831 A JP 2012015831A JP 2012082234 A5 JP2012082234 A5 JP 2012082234A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- cancer
- composition
- inhibiting
- disease
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 150000001875 compounds Chemical class 0.000 claims 89
- 239000000203 mixture Substances 0.000 claims 42
- 230000002401 inhibitory effect Effects 0.000 claims 37
- 150000003839 salts Chemical class 0.000 claims 30
- 108091000080 Phosphotransferase Proteins 0.000 claims 29
- 201000010099 disease Diseases 0.000 claims 29
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 29
- 102000020233 phosphotransferase Human genes 0.000 claims 29
- 239000012453 solvate Substances 0.000 claims 28
- 102000001253 Protein Kinase Human genes 0.000 claims 22
- 108060006633 protein kinase Proteins 0.000 claims 22
- 239000003814 drug Substances 0.000 claims 18
- 238000004519 manufacturing process Methods 0.000 claims 17
- 102000003989 Aurora kinases Human genes 0.000 claims 8
- 108090000433 Aurora kinases Proteins 0.000 claims 8
- 206010028980 Neoplasm Diseases 0.000 claims 7
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 6
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 6
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 6
- 239000002246 antineoplastic agent Substances 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- 210000004027 cell Anatomy 0.000 claims 6
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 5
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 5
- 230000000694 effects Effects 0.000 claims 5
- 201000000050 myeloid neoplasm Diseases 0.000 claims 5
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 3
- 208000036762 Acute promyelocytic leukaemia Diseases 0.000 claims 3
- 206010003571 Astrocytoma Diseases 0.000 claims 3
- 208000003950 B-cell lymphoma Diseases 0.000 claims 3
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 3
- 206010005003 Bladder cancer Diseases 0.000 claims 3
- 206010006187 Breast cancer Diseases 0.000 claims 3
- 208000026310 Breast neoplasm Diseases 0.000 claims 3
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 3
- 206010008342 Cervix carcinoma Diseases 0.000 claims 3
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 3
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 3
- 201000008808 Fibrosarcoma Diseases 0.000 claims 3
- 208000004463 Follicular Adenocarcinoma Diseases 0.000 claims 3
- 208000022072 Gallbladder Neoplasms Diseases 0.000 claims 3
- 208000032612 Glial tumor Diseases 0.000 claims 3
- 206010018338 Glioma Diseases 0.000 claims 3
- 208000017604 Hodgkin disease Diseases 0.000 claims 3
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 3
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 3
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 3
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 3
- 206010025323 Lymphomas Diseases 0.000 claims 3
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 3
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 3
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 3
- 206010029260 Neuroblastoma Diseases 0.000 claims 3
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 3
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 3
- 206010033128 Ovarian cancer Diseases 0.000 claims 3
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 3
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 3
- 206010060862 Prostate cancer Diseases 0.000 claims 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 3
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 3
- 206010038389 Renal cancer Diseases 0.000 claims 3
- 201000010208 Seminoma Diseases 0.000 claims 3
- 208000000453 Skin Neoplasms Diseases 0.000 claims 3
- 206010041067 Small cell lung cancer Diseases 0.000 claims 3
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 3
- 206010042971 T-cell lymphoma Diseases 0.000 claims 3
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 3
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 3
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 3
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 3
- 201000006083 Xeroderma Pigmentosum Diseases 0.000 claims 3
- 230000001154 acute effect Effects 0.000 claims 3
- 201000010881 cervical cancer Diseases 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 201000004101 esophageal cancer Diseases 0.000 claims 3
- 201000010175 gallbladder cancer Diseases 0.000 claims 3
- 206010017758 gastric cancer Diseases 0.000 claims 3
- 201000010536 head and neck cancer Diseases 0.000 claims 3
- 208000014829 head and neck neoplasm Diseases 0.000 claims 3
- 201000010982 kidney cancer Diseases 0.000 claims 3
- 208000032839 leukemia Diseases 0.000 claims 3
- 201000007270 liver cancer Diseases 0.000 claims 3
- 208000014018 liver neoplasm Diseases 0.000 claims 3
- 201000005202 lung cancer Diseases 0.000 claims 3
- 208000020816 lung neoplasm Diseases 0.000 claims 3
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 3
- 201000001441 melanoma Diseases 0.000 claims 3
- 208000007538 neurilemmoma Diseases 0.000 claims 3
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 3
- 201000008968 osteosarcoma Diseases 0.000 claims 3
- 201000002528 pancreatic cancer Diseases 0.000 claims 3
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 3
- 230000002062 proliferating effect Effects 0.000 claims 3
- 206010038038 rectal cancer Diseases 0.000 claims 3
- 201000001275 rectum cancer Diseases 0.000 claims 3
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 3
- 201000000849 skin cancer Diseases 0.000 claims 3
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 3
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 3
- 201000011549 stomach cancer Diseases 0.000 claims 3
- 208000001608 teratocarcinoma Diseases 0.000 claims 3
- 201000002510 thyroid cancer Diseases 0.000 claims 3
- 208000030901 thyroid gland follicular carcinoma Diseases 0.000 claims 3
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 3
- 201000005112 urinary bladder cancer Diseases 0.000 claims 3
- 208000012902 Nervous system disease Diseases 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 201000004384 Alopecia Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 101000777293 Homo sapiens Serine/threonine-protein kinase Chk1 Proteins 0.000 claims 1
- 101000777277 Homo sapiens Serine/threonine-protein kinase Chk2 Proteins 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000031888 Mycoses Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 102100031081 Serine/threonine-protein kinase Chk1 Human genes 0.000 claims 1
- 102100031075 Serine/threonine-protein kinase Chk2 Human genes 0.000 claims 1
- 231100000360 alopecia Toxicity 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 230000001886 ciliary effect Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 210000005036 nerve Anatomy 0.000 claims 1
- 210000000653 nervous system Anatomy 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 239000008177 pharmaceutical agent Substances 0.000 claims 1
- 108010083755 proto-oncogene proteins pim Proteins 0.000 claims 1
- 238000001959 radiotherapy Methods 0.000 claims 1
- 206010039667 schwannoma Diseases 0.000 claims 1
- 210000004291 uterus Anatomy 0.000 claims 1
- 230000003612 virological effect Effects 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US72415805P | 2005-10-06 | 2005-10-06 | |
| US60/724,158 | 2005-10-06 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008534673A Division JP5152922B2 (ja) | 2005-10-06 | 2006-10-04 | プロテインキナーゼを阻害するためのピラゾロ[1,5−a]ピリミジン誘導体の使用およびプロテインキナーゼを阻害する方法 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014002164A Division JP2014062129A (ja) | 2005-10-06 | 2014-01-09 | プロテインキナーゼを阻害するためのピラゾロ[1,5−a]ピリミジン誘導体の使用およびプロテインキナーゼを阻害する方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012082234A JP2012082234A (ja) | 2012-04-26 |
| JP2012082234A5 true JP2012082234A5 (enExample) | 2012-08-16 |
| JP5520325B2 JP5520325B2 (ja) | 2014-06-11 |
Family
ID=37943366
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008534673A Active JP5152922B2 (ja) | 2005-10-06 | 2006-10-04 | プロテインキナーゼを阻害するためのピラゾロ[1,5−a]ピリミジン誘導体の使用およびプロテインキナーゼを阻害する方法 |
| JP2012015831A Active JP5520325B2 (ja) | 2005-10-06 | 2012-01-27 | プロテインキナーゼを阻害するためのピラゾロ[1,5−a]ピリミジン誘導体の使用およびプロテインキナーゼを阻害する方法 |
| JP2014002164A Pending JP2014062129A (ja) | 2005-10-06 | 2014-01-09 | プロテインキナーゼを阻害するためのピラゾロ[1,5−a]ピリミジン誘導体の使用およびプロテインキナーゼを阻害する方法 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008534673A Active JP5152922B2 (ja) | 2005-10-06 | 2006-10-04 | プロテインキナーゼを阻害するためのピラゾロ[1,5−a]ピリミジン誘導体の使用およびプロテインキナーゼを阻害する方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014002164A Pending JP2014062129A (ja) | 2005-10-06 | 2014-01-09 | プロテインキナーゼを阻害するためのピラゾロ[1,5−a]ピリミジン誘導体の使用およびプロテインキナーゼを阻害する方法 |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US20070082900A1 (enExample) |
| EP (1) | EP1942900B1 (enExample) |
| JP (3) | JP5152922B2 (enExample) |
| CN (1) | CN101360499B (enExample) |
| BR (1) | BRPI0616985B1 (enExample) |
| CA (1) | CA2627623C (enExample) |
| NO (1) | NO20082093L (enExample) |
| NZ (1) | NZ567151A (enExample) |
| TW (1) | TWI421078B (enExample) |
| WO (1) | WO2007044441A2 (enExample) |
| ZA (1) | ZA200802998B (enExample) |
Families Citing this family (63)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US8580782B2 (en) * | 2002-09-04 | 2013-11-12 | Merck Sharp & Dohme Corp. | Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors |
| US7601724B2 (en) * | 2002-09-04 | 2009-10-13 | Schering Corporation | Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors |
| US7563798B2 (en) * | 2002-09-04 | 2009-07-21 | Schering Corporation | Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors |
| US7605155B2 (en) * | 2002-09-04 | 2009-10-20 | Schering Corporation | Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors |
| US7196092B2 (en) * | 2002-09-04 | 2007-03-27 | Schering Corporation | N-heteroaryl pyrazolopyrimidines as cyclin dependent kinase inhibitors |
| EP1945216A1 (en) * | 2005-11-10 | 2008-07-23 | Schering Corporation | Methods for inhibiting protein kinases |
| BRPI0708693A2 (pt) * | 2006-03-08 | 2011-06-14 | Novartis Ag | uso de derivados de pirazol[1,5,a]pirimidin-7-il amina no tratamento de distérbios neurolàgicos |
| AU2007268083A1 (en) * | 2006-05-22 | 2007-12-06 | Schering Corporation | Pyrazolo [1, 5-A] pyrimidines as CDK inhibitors |
| US20100143332A1 (en) * | 2006-11-17 | 2010-06-10 | Schering Corporation | Combination therapy for proliferative disorders |
| WO2008140724A1 (en) | 2007-05-08 | 2008-11-20 | Schering Corporation | Methods of treatment using intravenous formulations comprising temozolomide |
| WO2008153870A1 (en) * | 2007-06-07 | 2008-12-18 | Schering Corporation | Synthesis of substituted-3-aminopyrazoles |
| JP2011503084A (ja) * | 2007-11-07 | 2011-01-27 | シェーリング コーポレイション | 新規の細胞周期チェックポイント調節剤およびこれらの調節剤とチェックポイント阻害剤との併用 |
| CA2709202C (en) * | 2007-12-19 | 2013-04-23 | Amgen Inc. | Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors |
| WO2009089352A1 (en) | 2008-01-08 | 2009-07-16 | Array Biopharma Inc. | Pyrrolopyridines as kinase inhibitors |
| JP5608098B2 (ja) * | 2008-01-09 | 2014-10-15 | アレイ バイオファーマ、インコーポレイテッド | キナーゼ阻害薬としてのピラゾロピリジン |
| WO2009126584A1 (en) * | 2008-04-07 | 2009-10-15 | Amgen Inc. | Gem-disubstituted and spirocyclic amino pyridines/pyrimidines as cell cycle inhibitors |
| AR071717A1 (es) | 2008-05-13 | 2010-07-07 | Array Biopharma Inc | Pirrolo[2,3-b]piridinas inhibidoras de quinasas chk1 y chk2,composiciones farmaceuticas que las contienen,proceso para prepararlas y uso de las mismas en el tratamiento y prevencion del cancer. |
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| JP5769199B2 (ja) * | 2008-10-31 | 2015-08-26 | ジェネンテック, インコーポレイテッド | ピラゾロピリミジンjak阻害剤化合物と方法 |
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| EP2417138B1 (en) | 2009-04-09 | 2019-11-27 | Merck Sharp & Dohme Corp. | Pyrazolo[1, 5-a]pyrimidine derivatives as mtor inhibitors |
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| PL3808749T3 (pl) | 2012-12-07 | 2023-07-10 | Vertex Pharmaceuticals Incorporated | Pirazolo[1,5-a]pirymidyny użyteczne jako inhibitory kinazy atr do leczenia chorób nowotworowych |
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| PL3077397T3 (pl) | 2013-12-06 | 2020-04-30 | Vertex Pharmaceuticals Inc. | Związek 2-amino-6-fluoro-n-[5-fluoro-pirydyn-3-ylo]pyrazolo [1,5-a]pirymidino-3-karboksamidu przydatny jako inhibitor kinazy atr, jego wytwarzanie, różne postacie stałe i ich radioznakowane pochodne |
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| PT3157566T (pt) | 2014-06-17 | 2019-07-11 | Vertex Pharma | Método para tratamento de cancro utilizando uma combinação de inibidores chk1 e atr |
| 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 |
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| US20210395256A1 (en) * | 2018-12-07 | 2021-12-23 | Betta Pharmaceuticals Co., Ltd. | Tyrosine kinase inhibitors, compositions and methods there of |
| SG11202110523XA (en) | 2019-03-26 | 2021-10-28 | Ventyx Biosciences Inc | Tyk2 pseudokinase ligands |
| TWI882032B (zh) | 2019-11-08 | 2025-05-01 | 美商凡帝克斯生物科學公司 | Tyk2假激酶配位體 |
| JOP20220125A1 (ar) | 2019-11-25 | 2023-01-30 | Amgen Inc | مركبات حلقية غير متجانسة على هيئة مثبطات دلتا-5 ديساتوراز وطرق لاستخدامها |
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| US7196078B2 (en) * | 2002-09-04 | 2007-03-27 | Schering Corpoartion | Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors |
| US7119200B2 (en) * | 2002-09-04 | 2006-10-10 | Schering Corporation | Pyrazolopyrimidines as cyclin dependent kinase inhibitors |
| BRPI0407834A (pt) * | 2003-02-28 | 2006-02-14 | Teijin Pharma Ltd | composto, processo para a manufatura do mesmo, composição, processo para a manufatura da mesma, método de tratamento ou prevenção de um distúrbio mediado por proteìna quinase em um indivìduo, uso de um composto, ensaio para determinar a atividade dos compostos, e, método de inibição da atividade ou função de uma proteìna quinase |
| WO2004087707A1 (en) * | 2003-03-31 | 2004-10-14 | Vernalis (Cambridge) Limited | Pyrazolopyrimidine compounds and their use in medicine |
| JP3940700B2 (ja) * | 2003-05-22 | 2007-07-04 | 茂 相馬 | 楽器用ケース |
| AR049769A1 (es) * | 2004-01-22 | 2006-09-06 | Novartis Ag | Derivados de pirazolo(1,5-a)pirimidin 7-il-amina para utilizarse en el tratamiento de enfermedades dependientes de la quinasa de proteina |
| JP3104094U (ja) * | 2004-03-18 | 2004-09-02 | チャン ホアン−リン | 両用スーツケース |
| TWI333953B (en) * | 2005-10-06 | 2010-12-01 | Schering Corp | Pyrazolopyrimidines as protein kinase inhibitors |
| US7776865B2 (en) * | 2005-10-06 | 2010-08-17 | Schering Corporation | Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors |
| JP3174645U (ja) * | 2012-01-19 | 2012-03-29 | 株式会社セイバン | ランドセル |
-
2006
- 2006-10-04 BR BRPI0616985-6A patent/BRPI0616985B1/pt active IP Right Grant
- 2006-10-04 NZ NZ567151A patent/NZ567151A/en not_active IP Right Cessation
- 2006-10-04 CN CN200680045935.5A patent/CN101360499B/zh active Active
- 2006-10-04 WO PCT/US2006/038917 patent/WO2007044441A2/en not_active Ceased
- 2006-10-04 CA CA2627623A patent/CA2627623C/en active Active
- 2006-10-04 EP EP06836185.6A patent/EP1942900B1/en active Active
- 2006-10-04 TW TW095136818A patent/TWI421078B/zh not_active IP Right Cessation
- 2006-10-04 US US11/542,801 patent/US20070082900A1/en not_active Abandoned
- 2006-10-04 JP JP2008534673A patent/JP5152922B2/ja active Active
-
2008
- 2008-04-04 ZA ZA200802998A patent/ZA200802998B/xx unknown
- 2008-05-05 NO NO20082093A patent/NO20082093L/no not_active Application Discontinuation
-
2010
- 2010-01-15 US US12/688,664 patent/US8211854B2/en active Active
-
2012
- 2012-01-27 JP JP2012015831A patent/JP5520325B2/ja active Active
-
2014
- 2014-01-09 JP JP2014002164A patent/JP2014062129A/ja active Pending
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