TWI484960B - 嘧啶衍生物 - Google Patents
嘧啶衍生物 Download PDFInfo
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- TWI484960B TWI484960B TW097113595A TW97113595A TWI484960B TW I484960 B TWI484960 B TW I484960B TW 097113595 A TW097113595 A TW 097113595A TW 97113595 A TW97113595 A TW 97113595A TW I484960 B TWI484960 B TW I484960B
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- Prior art keywords
- group
- alkyl
- aryl
- compound
- heteroaryl
- Prior art date
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- 150000003230 pyrimidines Chemical class 0.000 title description 11
- 150000001875 compounds Chemical class 0.000 claims description 49
- 125000003118 aryl group Chemical group 0.000 claims description 27
- -1 cyano, hydroxy Chemical group 0.000 claims description 25
- 125000000217 alkyl group Chemical group 0.000 claims description 24
- 125000001072 heteroaryl group Chemical group 0.000 claims description 23
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 21
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 19
- 125000003545 alkoxy group Chemical group 0.000 claims description 17
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- 125000000304 alkynyl group Chemical group 0.000 claims description 14
- 230000033115 angiogenesis Effects 0.000 claims description 14
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims description 11
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 11
- 125000005843 halogen group Chemical group 0.000 claims description 11
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
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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
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- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- 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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
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| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| TWI491605B (zh) | 2008-11-24 | 2015-07-11 | Boehringer Ingelheim Int | 新穎化合物 |
| TW201024281A (en) | 2008-11-24 | 2010-07-01 | Boehringer Ingelheim Int | New compounds |
| JP2012197231A (ja) * | 2009-08-06 | 2012-10-18 | Oncotherapy Science Ltd | Ｔｔｋ阻害作用を有するピリジンおよびピリミジン誘導体 |
| US8466155B2 (en) | 2009-10-02 | 2013-06-18 | Boehringer Ingelheim International Gmbh | Pyrimidines |
| CN102070618B (zh) * | 2009-11-23 | 2013-08-21 | 和记黄埔医药（上海）有限公司 | 一种化合物及其晶体 |
| BR112012029647A2 (pt) | 2010-05-21 | 2016-08-02 | Chemilia Ab | novos derivados de pirimidinas |
| EP2395001A1 (en) | 2010-05-21 | 2011-12-14 | Chemilia AB | Novel pyrimidine derivatives |
| EP2433636A1 (en) * | 2010-09-27 | 2012-03-28 | Medizinische Universität Wien | Treatment of Malignant Diseases |
| EP2621276B1 (en) * | 2010-09-30 | 2017-12-27 | Merck Sharp & Dohme Corp. | 2-alkoxy pyrimidine pde10 inhibitors |
| EP2502924A1 (en) | 2011-03-24 | 2012-09-26 | Chemilia AB | Novel pyrimidine derivatives |
| DK2688883T3 (en) | 2011-03-24 | 2016-09-05 | Noviga Res Ab | pyrimidine |
| WO2013054351A1 (en) * | 2011-08-08 | 2013-04-18 | Cadila Healthcare Limited | Heterocyclic compounds |
| EP2711364A1 (en) | 2012-09-21 | 2014-03-26 | Chemilia AB | 4-(Indolyl or benzimidazolyl)amino-2-(2-(indol-3-yl)ethyl)aminopyrimidines useful for the treatment of cancer |
| EP2711365A1 (en) | 2012-09-21 | 2014-03-26 | Chemilia AB | 4-Indazolylamino-2-(2-(indol-3-yl)ethyl)aminopyrimidines useful for the treatment of cancer |
| RU2674249C2 (ru) * | 2012-11-05 | 2018-12-06 | НэнтБайо, Инк. | Замещенные производные индол-5-ола и их терапевтическое применение |
| CA2906185A1 (en) | 2013-03-15 | 2014-09-18 | Nantbioscience, Inc. | Substituted indol-5-ol derivatives and their therapeutic applications |
| CN105601573B (zh) * | 2014-11-24 | 2021-07-02 | 中国科学院上海药物研究所 | 2-氨基嘧啶类化合物及其药物组合物和应用 |
| BR112017018183A2 (pt) * | 2015-02-27 | 2018-07-24 | Nantbioscience Inc | derivados de pirimidina como inibidores de quinase e suas aplicações terapêuticas. |
| WO2017190050A1 (en) | 2016-04-28 | 2017-11-02 | Cornell University | Inhibitors of soluble adenylyl cyclase |
| TW202115042A (zh) * | 2019-06-21 | 2021-04-16 | 大陸商江蘇豪森藥業集團有限公司 | 芳基磷氧化物類衍生物抑制劑、其製備方法和應用 |
| CN111004221B (zh) * | 2019-12-13 | 2021-02-02 | 长治学院 | 一种嘧啶/苯并咪唑杂合物、制备方法及医药用途 |
| EP4251613A4 (en) * | 2020-11-27 | 2024-11-20 | Allorion Therapeutics Inc. | AMINOHETEROARYL KINASE INHIBITORS |
Citations (1)
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| US20040180914A1 (en) * | 1999-06-18 | 2004-09-16 | Celltech R&D Limtied | 5-Cyano-2-aminopyrimidine derivatives |
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| AU661533B2 (en) * | 1992-01-20 | 1995-07-27 | Astrazeneca Ab | Quinazoline derivatives |
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- 2008-04-15 BR BRPI0809715-1A patent/BRPI0809715A2/pt not_active Application Discontinuation
- 2008-04-15 PT PT87458816T patent/PT2154967E/pt unknown
- 2008-04-15 CA CA2684470A patent/CA2684470C/en active Active
- 2008-04-15 EP EP08745881.6A patent/EP2154967B9/en active Active
- 2008-04-15 SI SI200831203T patent/SI2154967T1/sl unknown
- 2008-04-15 RU RU2009141982/04A patent/RU2455994C2/ru active
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- 2008-04-15 KR KR1020097023882A patent/KR101424847B1/ko not_active Expired - Fee Related
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| NZ580671A (en) | 2012-03-30 |
| RU2009141982A (ru) | 2011-05-27 |
| EP2154967B9 (en) | 2014-07-23 |
| JP2010524952A (ja) | 2010-07-22 |
| PT2154967E (pt) | 2014-06-05 |
| PL2154967T3 (pl) | 2014-08-29 |
| AU2008240084A1 (en) | 2008-10-23 |
| WO2008128231A1 (en) | 2008-10-23 |
| DK2154967T3 (da) | 2014-04-07 |
| ES2465673T9 (es) | 2014-11-14 |
| MX2009011199A (es) | 2010-03-17 |
| EP2154967B1 (en) | 2014-03-05 |
| JP5635398B2 (ja) | 2014-12-03 |
| KR20100016592A (ko) | 2010-02-12 |
| US8349859B2 (en) | 2013-01-08 |
| EP2154967A1 (en) | 2010-02-24 |
| RU2455994C2 (ru) | 2012-07-20 |
| TW200848049A (en) | 2008-12-16 |
| HRP20140377T2 (hr) | 2015-01-16 |
| US20080255172A1 (en) | 2008-10-16 |
| KR101424847B1 (ko) | 2016-07-08 |
| HRP20140377T1 (en) | 2014-05-23 |
| BRPI0809715A2 (pt) | 2019-11-05 |
| CA2684470C (en) | 2016-02-09 |
| EP2154967A4 (en) | 2010-05-19 |
| CA2684470A1 (en) | 2008-10-23 |
| US8901143B2 (en) | 2014-12-02 |
| DK2154967T5 (en) | 2014-11-17 |
| SI2154967T1 (sl) | 2014-06-30 |
| US20130065890A1 (en) | 2013-03-14 |
| ES2465673T3 (es) | 2014-06-06 |
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