KR20060010709A - 사이클린 의존성 키나제 억제제로서의 신규한 이미다조피라진 - Google Patents
사이클린 의존성 키나제 억제제로서의 신규한 이미다조피라진 Download PDFInfo
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- KR20060010709A KR20060010709A KR1020057004674A KR20057004674A KR20060010709A KR 20060010709 A KR20060010709 A KR 20060010709A KR 1020057004674 A KR1020057004674 A KR 1020057004674A KR 20057004674 A KR20057004674 A KR 20057004674A KR 20060010709 A KR20060010709 A KR 20060010709A
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- Prior art keywords
- alkyl
- compound
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- aryl
- heteroaryl
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- 125000003944 tolyl group Chemical group 0.000 description 1
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- 239000003053 toxin Substances 0.000 description 1
- 231100000765 toxin Toxicity 0.000 description 1
- 108700012359 toxins Proteins 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- 230000016596 traversing start control point of mitotic cell cycle Effects 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- 230000005747 tumor angiogenesis Effects 0.000 description 1
- 210000003932 urinary bladder Anatomy 0.000 description 1
- 238000007631 vascular surgery Methods 0.000 description 1
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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
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
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- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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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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- A—HUMAN NECESSITIES
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Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Urology & Nephrology (AREA)
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- Neurology (AREA)
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- Neurosurgery (AREA)
- Oncology (AREA)
- Biomedical Technology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Dermatology (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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| US41290602P | 2002-09-23 | 2002-09-23 | |
| US60/412,906 | 2002-09-23 |
Publications (1)
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| KR20060010709A true KR20060010709A (ko) | 2006-02-02 |
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| CA (1) | CA2499874A1 (enExample) |
| MX (1) | MXPA05003119A (enExample) |
| NZ (1) | NZ538686A (enExample) |
| TW (1) | TW200412967A (enExample) |
| WO (1) | WO2004026310A1 (enExample) |
| ZA (1) | ZA200502380B (enExample) |
Families Citing this family (58)
| Publication number | Priority date | Publication date | Assignee | Title |
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| EP0977563B1 (en) * | 1996-12-03 | 2005-10-12 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto, analogues and uses thereof |
| US20020058286A1 (en) * | 1999-02-24 | 2002-05-16 | Danishefsky Samuel J. | Synthesis of epothilones, intermediates thereto and analogues thereof |
| US6919340B2 (en) | 2002-04-19 | 2005-07-19 | Cellular Genomics, Inc. | Imidazo[1,2-a]pyrazin-8-ylamines, method of making, and method of use thereof |
| US7649006B2 (en) | 2002-08-23 | 2010-01-19 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| WO2004018478A2 (en) * | 2002-08-23 | 2004-03-04 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto, analogues and uses thereof |
| US6921769B2 (en) | 2002-08-23 | 2005-07-26 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| WO2004022562A1 (en) * | 2002-09-09 | 2004-03-18 | Cellular Genomics, Inc. | 6-ARYL-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINES, METHOD OF MAKING, AND METHOD OF USE THEREOF |
| TW200413378A (en) * | 2002-09-23 | 2004-08-01 | Schering Corp | Novel imidazopyrazines as cyclin dependent kinase inhibitors |
| US7576085B2 (en) * | 2002-09-23 | 2009-08-18 | Schering Corporation | Imidazopyrazines as cyclin dependent kinase inhibitors |
| US7189723B2 (en) | 2003-02-10 | 2007-03-13 | Cgi Pharmaceuticals, Inc. | Certain 8-heteroaryl-6-phenyl-imidazo[1,2-a]pyrazines as modulators of kinase activity |
| WO2005014599A1 (en) * | 2003-06-04 | 2005-02-17 | Cellular Genomics, Inc. | Imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of bruton’s tyrosine kinase by such compounds |
| US20060183746A1 (en) * | 2003-06-04 | 2006-08-17 | Currie Kevin S | Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds |
| WO2005005429A1 (en) * | 2003-06-30 | 2005-01-20 | Cellular Genomics, Inc. | Certain heterocyclic substituted imidazo[1,2-a]pyrazin-8-ylamines and methods of inhibition of bruton’s tyrosine kinase by such compounds |
| US7259164B2 (en) | 2003-08-11 | 2007-08-21 | Cgi Pharmaceuticals, Inc. | Certain substituted imidazo[1,2-a]pyrazines, as modulators of kinase activity |
| WO2005085252A1 (en) * | 2004-03-04 | 2005-09-15 | Biofocus Discovery Limited | Imidazo ‘1,2-a’ pyrazine compounds which interact with protein kinases |
| NZ556433A (en) * | 2005-01-14 | 2010-10-29 | Cgi Pharmaceuticals Inc | 1, 3-diaryl substituted ureas as modulators of kinase activity |
| WO2007024294A2 (en) * | 2005-05-03 | 2007-03-01 | Cgi Pharmaceuticals, Inc. | Certain substituted ureas, as modulators of kinase activity |
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| JP2009508868A (ja) * | 2005-09-16 | 2009-03-05 | シェーリング コーポレイション | テモゾロミドおよびプロテインキナーゼインヒビターを用いる薬学的組成物および方法 |
| EP1945216A1 (en) | 2005-11-10 | 2008-07-23 | Schering Corporation | Methods for inhibiting protein kinases |
| BRPI0618520A2 (pt) * | 2005-11-10 | 2011-09-06 | Schering Corp | imidazopirazinas como inibidores de proteìna cinase |
| US20090018142A9 (en) * | 2006-05-02 | 2009-01-15 | Zhengping Zhuang | Use of phosphatases to treat tumors overexpressing N-CoR |
| US20090175852A1 (en) | 2006-06-06 | 2009-07-09 | Schering Corporation | Imidazopyrazines as protein kinase inhibitors |
| AU2008214299B2 (en) * | 2007-02-06 | 2014-01-09 | Lixte Biotechnology, Inc. | Oxabicycloheptanes and oxabicycloheptenes, their preparation and use |
| US20090035292A1 (en) * | 2007-08-03 | 2009-02-05 | Kovach John S | Use of phosphatases to treat neuroblastomas and medulloblastomas |
| MX2010003417A (es) * | 2007-10-01 | 2010-09-10 | Lixte Biotechnology Inc | Inhibidores de histona desacetilasa. |
| AU2009215191A1 (en) | 2008-02-13 | 2009-08-20 | Gilead Connecticut, Inc. | 6-aryl-imidaz0[l, 2-a] pyrazine derivatives, method of making, and method of use thereof |
| EP2318005B1 (en) | 2008-08-01 | 2017-11-01 | Lixte Biotechnology, Inc. | Neuroprotective agents for the prevention and treatment of neurodegenerative diseases |
| WO2010147612A1 (en) | 2009-06-18 | 2010-12-23 | Lixte Biotechnology, Inc. | Methods of modulating cell regulation by inhibiting p53 |
| US8227473B2 (en) | 2008-08-01 | 2012-07-24 | Lixte Biotechnology, Inc. | Oxabicycloheptanes and oxabicycloheptenes, their preparation and use |
| WO2010014141A1 (en) * | 2008-08-01 | 2010-02-04 | Lixte Biotechnology, Inc. | Methods for regulating cell mitosis by inhibiting serine/threonine phosphatase |
| BRPI0922225B1 (pt) | 2008-12-08 | 2022-01-11 | Gilead Connecticut, Inc. | Inibidores de syk imidazopirazina, composição farmacêutica, e uso do composto |
| US8450321B2 (en) | 2008-12-08 | 2013-05-28 | Gilead Connecticut, Inc. | 6-(1H-indazol-6-yl)-N-[4-(morpholin-4-yl)phenyl]imidazo-[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a SYK inhibitor |
| PE20120121A1 (es) | 2008-12-08 | 2012-02-20 | Gilead Connecticut Inc | Derivados de imidazopirazina como inhibidores de syk |
| US8993535B2 (en) | 2009-09-04 | 2015-03-31 | Merck Sharp & Dohme Corp. | Modulators of cell cycle checkpoints and their use in combination with checkpoint kinase inhibitors |
| NZ599597A (en) | 2009-10-30 | 2013-05-31 | Janssen Pharmaceutica Nv | IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS |
| AR080754A1 (es) | 2010-03-09 | 2012-05-09 | Janssen Pharmaceutica Nv | Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10 |
| KR101717809B1 (ko) | 2010-03-11 | 2017-03-17 | 질레드 코네티컷 인코포레이티드 | 이미다조피리딘 ｓｙｋ 억제제 |
| EP2651945A1 (en) * | 2010-12-17 | 2013-10-23 | Bayer Intellectual Property GmbH | 6-substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders |
| CA2821817A1 (en) * | 2010-12-17 | 2012-06-21 | Bayer Intellectual Property Gmbh | Substituted 6-imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders |
| WO2013000924A1 (en) | 2011-06-27 | 2013-01-03 | Janssen Pharmaceutica Nv | 1-ARYL-4-METHYL-[1,2,4]TRIAZOLO[4,3-a]QUINOXALINE DERIVATIVES |
| WO2014001314A1 (en) | 2012-06-26 | 2014-01-03 | Janssen Pharmaceutica Nv | Combinations comprising pde 2 inhibitors such as 1-aryl-4-methyl- [1,2,4] triazolo [4,3-a] quinoxaline compounds and pde 10 inhibitors for use in the treatment of neurological or metabolic disorders |
| AU2013289284B2 (en) | 2012-07-09 | 2017-03-30 | Janssen Pharmaceutica Nv | Inhibitors of phosphodiesterase 10 enzyme |
| EP2983661B1 (en) | 2013-04-09 | 2024-05-29 | Lixte Biotechnology, Inc. | Formulations of oxabicycloheptanes and oxabicycloheptenes |
| AU2014296308C1 (en) | 2013-07-30 | 2018-09-13 | Kronos Bio, Inc. | Polymorph of Syk inhibitors |
| UA115815C2 (uk) | 2013-07-30 | 2017-12-26 | Гіліад Коннектікут, Інк. | Склад на основі інгібіторів syk |
| CA2932726C (en) | 2013-12-04 | 2019-06-04 | Gilead Sciences, Inc. | Methods for treating cancers with entospletinib |
| US9290505B2 (en) | 2013-12-23 | 2016-03-22 | Gilead Sciences, Inc. | Substituted imidazo[1,2-a]pyrazines as Syk inhibitors |
| TWI662037B (zh) | 2013-12-23 | 2019-06-11 | 美商基利科學股份有限公司 | 脾酪胺酸激酶抑制劑 |
| EP3169366A1 (en) | 2014-07-14 | 2017-05-24 | Gilead Sciences, Inc. | Combinations for treating cancers |
| JP6895963B2 (ja) | 2015-11-18 | 2021-06-30 | ジェンザイム・コーポレーション | 多発性嚢胞腎のバイオマーカーおよびその使用 |
| WO2018107004A1 (en) | 2016-12-08 | 2018-06-14 | Lixte Biotechnology, Inc. | Oxabicycloheptanes for modulation of immune response |
| CN115028640A (zh) | 2017-08-25 | 2022-09-09 | 吉利德科学公司 | Syk抑制剂的多晶型物 |
| CN113950479A (zh) | 2019-02-22 | 2022-01-18 | 克洛诺斯生物股份有限公司 | 作为syk抑制剂的缩合吡嗪的固体形式 |
| US20230348475A1 (en) * | 2020-09-17 | 2023-11-02 | The Translational Genomics Research Institute | Imidazopyridazine and imidazopyrazine compounds as inhibitors of cdk7 |
| CN114042065B (zh) * | 2021-11-26 | 2024-03-15 | 长沙拜特生物科技研究所有限公司 | 一种复方甲苯咪唑透皮溶液剂及其制备方法 |
| WO2025199359A1 (en) * | 2024-03-21 | 2025-09-25 | The Translational Genomics Research Institute | Methods of modulating cdk7 and flt3 using fused bicyclic compounds |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4797764A (en) * | 1986-01-27 | 1989-01-10 | Minnesota Mining And Manufacturing Company | Recording disk with low total indicated runout |
| FR2607813B1 (fr) | 1986-12-05 | 1989-03-31 | Montpellier I Universite | Alkylamino-8 imidazo (1,2-a) pyrazines et derives, leur preparation et leur application en therapeutique |
| EP0778277B1 (en) | 1995-12-08 | 2003-06-25 | Pfizer Inc. | Substituted heterocyclic derivatives as CRF antagonists |
| EP1301511A2 (en) | 2000-07-14 | 2003-04-16 | Bristol-Myers Squibb Pharma Company | IMIDAZO 1,2-a]PYRAZINES FOR THE TREATMENT OF NEUROLOGICAL DISORDERS |
| AU2001259704A1 (en) | 2000-07-26 | 2002-02-13 | Bristol-Myers Squibb Company | N-(5-(((5-alkyl-2-oxazolyl)methyl)thio)-2-thiazolyl) carboxamide inhibitors of cyclin dependent kinases |
| WO2002060492A1 (en) | 2001-01-30 | 2002-08-08 | Cytopia Pty Ltd | Methods of inhibiting kinases |
| US6919340B2 (en) | 2002-04-19 | 2005-07-19 | Cellular Genomics, Inc. | Imidazo[1,2-a]pyrazin-8-ylamines, method of making, and method of use thereof |
| TW200413378A (en) * | 2002-09-23 | 2004-08-01 | Schering Corp | Novel imidazopyrazines as cyclin dependent kinase inhibitors |
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2003
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- 2003-09-19 US US10/666,424 patent/US7186740B2/en not_active Expired - Fee Related
- 2003-09-19 NZ NZ538686A patent/NZ538686A/en unknown
- 2003-09-19 CA CA002499874A patent/CA2499874A1/en not_active Abandoned
- 2003-09-19 CN CNA038251027A patent/CN1694706A/zh active Pending
- 2003-09-19 TW TW092125931A patent/TW200412967A/zh unknown
- 2003-09-19 WO PCT/US2003/029456 patent/WO2004026310A1/en not_active Ceased
- 2003-09-19 MX MXPA05003119A patent/MXPA05003119A/es active IP Right Grant
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2007
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Also Published As
| Publication number | Publication date |
|---|---|
| CA2499874A1 (en) | 2004-04-01 |
| US20040072835A1 (en) | 2004-04-15 |
| US7186740B2 (en) | 2007-03-06 |
| TW200412967A (en) | 2004-08-01 |
| CN1694706A (zh) | 2005-11-09 |
| AU2003275031A1 (en) | 2004-04-08 |
| ZA200502380B (en) | 2005-09-27 |
| US20070155751A1 (en) | 2007-07-05 |
| WO2004026310A8 (en) | 2005-06-30 |
| EP1542693A1 (en) | 2005-06-22 |
| AR041346A1 (es) | 2005-05-11 |
| NZ538686A (en) | 2008-01-31 |
| WO2004026310A1 (en) | 2004-04-01 |
| AU2003275031B2 (en) | 2006-08-17 |
| MXPA05003119A (es) | 2005-06-22 |
| JP2006503838A (ja) | 2006-02-02 |
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