CN102596963A - 二环杂芳基的醚衍生物 - Google Patents
二环杂芳基的醚衍生物 Download PDFInfo
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- CN102596963A CN102596963A CN2010800506564A CN201080050656A CN102596963A CN 102596963 A CN102596963 A CN 102596963A CN 2010800506564 A CN2010800506564 A CN 2010800506564A CN 201080050656 A CN201080050656 A CN 201080050656A CN 102596963 A CN102596963 A CN 102596963A
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- Prior art keywords
- alkyl
- amino
- compound
- pyrrolo
- hydroxyl
- Prior art date
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- 125000001072 heteroaryl group Chemical group 0.000 title description 2
- 150000002170 ethers Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract description 578
- 238000000034 method Methods 0.000 claims abstract description 337
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 52
- 201000010099 disease Diseases 0.000 claims abstract description 51
- 239000003814 drug Substances 0.000 claims abstract description 40
- 238000011282 treatment Methods 0.000 claims abstract description 35
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 22
- -1 heterocyclic radical Chemical class 0.000 claims description 408
- 150000001412 amines Chemical class 0.000 claims description 130
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 69
- XLJMAIOERFSOGZ-UHFFFAOYSA-N cyanic acid Chemical compound OC#N XLJMAIOERFSOGZ-UHFFFAOYSA-N 0.000 claims description 68
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims description 63
- 150000003839 salts Chemical class 0.000 claims description 58
- 229910052739 hydrogen Inorganic materials 0.000 claims description 50
- 239000001257 hydrogen Substances 0.000 claims description 49
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 49
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 48
- 206010028980 Neoplasm Diseases 0.000 claims description 46
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 45
- 125000004429 atom Chemical group 0.000 claims description 44
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 39
- 229910052736 halogen Inorganic materials 0.000 claims description 38
- 150000002367 halogens Chemical class 0.000 claims description 38
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- 125000000623 heterocyclic group Chemical group 0.000 claims description 20
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- 125000004568 thiomorpholinyl group Chemical group 0.000 claims description 7
- YPWFNLSXQIGJCK-UHFFFAOYSA-N 7-oxabicyclo[2.2.1]heptane Chemical compound C1CC2CCC1O2 YPWFNLSXQIGJCK-UHFFFAOYSA-N 0.000 claims description 5
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- 125000004076 pyridyl group Chemical group 0.000 claims description 5
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- ZSIQJIWKELUFRJ-UHFFFAOYSA-N azepane Chemical compound C1CCCNCC1 ZSIQJIWKELUFRJ-UHFFFAOYSA-N 0.000 claims description 4
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 4
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- YDTFRJLNMPSCFM-YDALLXLXSA-M levothyroxine sodium anhydrous Chemical compound [Na+].IC1=CC(C[C@H](N)C([O-])=O)=CC(I)=C1OC1=CC(I)=C(O)C(I)=C1 YDTFRJLNMPSCFM-YDALLXLXSA-M 0.000 claims description 4
- 125000002757 morpholinyl group Chemical group 0.000 claims description 4
- 125000001400 nonyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 4
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- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims description 4
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- 125000006563 (C1-3) alkylaminocarbonyl group Chemical group 0.000 claims description 3
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- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims description 2
- 125000004432 carbon atom Chemical group C* 0.000 claims description 2
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims description 2
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- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 56
- 239000011734 sodium Substances 0.000 description 53
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- 238000001704 evaporation Methods 0.000 description 42
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- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 31
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- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 30
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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
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
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- A—HUMAN NECESSITIES
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
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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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biophysics (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Inorganic Chemistry (AREA)
- Gastroenterology & Hepatology (AREA)
- Pulmonology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24118209P | 2009-09-10 | 2009-09-10 | |
| US61/241,182 | 2009-09-10 | ||
| PCT/EP2010/063334 WO2011029915A1 (en) | 2009-09-10 | 2010-09-10 | Ether derivatives of bicyclic heteroaryls |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102596963A true CN102596963A (zh) | 2012-07-18 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN2010800506564A Pending CN102596963A (zh) | 2009-09-10 | 2010-09-10 | 二环杂芳基的醚衍生物 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20120165310A1 (OSRAM) |
| EP (1) | EP2475668A1 (OSRAM) |
| JP (1) | JP2013504543A (OSRAM) |
| KR (1) | KR20120093867A (OSRAM) |
| CN (1) | CN102596963A (OSRAM) |
| AU (1) | AU2010294209A1 (OSRAM) |
| BR (1) | BR112012005400A2 (OSRAM) |
| CA (1) | CA2773661A1 (OSRAM) |
| EA (1) | EA201200471A1 (OSRAM) |
| IN (1) | IN2012DN02139A (OSRAM) |
| MX (1) | MX2012002997A (OSRAM) |
| WO (1) | WO2011029915A1 (OSRAM) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107098909A (zh) * | 2017-05-19 | 2017-08-29 | 四川大学华西医院 | 烷氧端基寡peg修饰的氨基嘧啶衍生物及抗肿瘤应用 |
| WO2018000550A1 (zh) * | 2016-06-29 | 2018-01-04 | 四川大学华西医院 | 吡唑并[3,4-d]嘧啶衍生物 |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2571361A4 (en) | 2010-05-19 | 2013-11-13 | Univ North Carolina | PYRAZOLOPYRIMIDINE COMPOUNDS FOR CANCER TREATMENT |
| US9273056B2 (en) * | 2011-10-03 | 2016-03-01 | The University Of North Carolina At Chapel Hill | Pyrrolopyrimidine compounds for the treatment of cancer |
| CN104080789B (zh) * | 2012-01-31 | 2016-05-11 | 南京奥昭生物科技有限公司 | 作为布鲁顿酪氨酸激酶抑制剂的环状分子 |
| TW201348231A (zh) * | 2012-02-29 | 2013-12-01 | Amgen Inc | 雜雙環化合物 |
| US9567326B2 (en) | 2012-05-22 | 2017-02-14 | The University Of North Carolina At Chapel Hill | Pyrimidine compounds for the treatment of cancer |
| WO2014062774A1 (en) | 2012-10-17 | 2014-04-24 | The University Of North Carolina At Chapel Hill | Pyrazolopyrimidine compounds for the treatment of cancer |
| BR112015010221B1 (pt) | 2012-11-06 | 2022-09-13 | Shanghai Fochon Pharmaceutical Co., Ltd. | Inibidores de quinase alk, seus usos, composição farmacêutica, e método para fabricação de medicamento |
| WO2014085225A1 (en) | 2012-11-27 | 2014-06-05 | The University Of North Carolina At Chapel Hill | Pyrimidine compounds for the treatment of cancer |
| WO2015157127A1 (en) | 2014-04-11 | 2015-10-15 | The University Of North Carolina At Chapel Hill | Therapuetic uses of selected pyrimidine compounds with anti-mer tyrosine kinase activity |
| US10112924B2 (en) | 2015-12-02 | 2018-10-30 | Astraea Therapeutics, Inc. | Piperdinyl nociceptin receptor compounds |
| CN108883103A (zh) * | 2015-12-02 | 2018-11-23 | 阿斯特来亚治疗有限责任公司 | 哌啶基痛敏肽受体化合物 |
| US10709708B2 (en) | 2016-03-17 | 2020-07-14 | The University Of North Carolina At Chapel Hill | Method of treating cancer with a combination of MER tyrosine kinase inhibitor and an epidermal growth factor receptor (EGFR) inhibitor |
| CA3169649A1 (en) | 2020-01-30 | 2021-08-05 | The Regents Of The University Of California | Strad-binding agents and uses thereof |
| US12084453B2 (en) | 2021-12-10 | 2024-09-10 | Incyte Corporation | Bicyclic amines as CDK12 inhibitors |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001072751A1 (en) * | 2000-03-29 | 2001-10-04 | Knoll Gesellschaft Mit Beschraenkter Haftung | Pyrrolopyrimidines as tyrosine kinase inhibitors |
| CN1531538A (zh) * | 2001-05-14 | 2004-09-22 | ��˹��ŵ�� | 4-氨基-5-苯基-7-环丁基-吡咯并[2,3-d]嘧啶衍生物 |
| CN1898240A (zh) * | 2003-10-15 | 2007-01-17 | Osi制药公司 | 咪唑并吡嗪类酪氨酸激酶抑制剂 |
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| GB1524747A (en) | 1976-05-11 | 1978-09-13 | Ici Ltd | Polypeptide |
| LU88769I2 (fr) | 1982-07-23 | 1996-11-05 | Zeneca Ltd | Bicalutamide et ses sels et esters pharmaceutiquement acceptables (Casodex (R)) |
| GB8327256D0 (en) | 1983-10-12 | 1983-11-16 | Ici Plc | Steroid derivatives |
| US5010099A (en) | 1989-08-11 | 1991-04-23 | Harbor Branch Oceanographic Institution, Inc. | Discodermolide compounds, compositions containing same and method of preparation and use |
| NZ243082A (en) | 1991-06-28 | 1995-02-24 | Ici Plc | 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof |
| GB9300059D0 (en) | 1992-01-20 | 1993-03-03 | Zeneca Ltd | Quinazoline derivatives |
| TW225528B (OSRAM) | 1992-04-03 | 1994-06-21 | Ciba Geigy Ag | |
| ATE215565T1 (de) | 1992-10-28 | 2002-04-15 | Genentech Inc | Verwendung von anti-vegf antikörpern zur behandlung von krebs |
| DE69520282T2 (de) | 1994-09-29 | 2001-08-09 | Novartis Ag, Basel | Pyrrolo[2,3-d]pyrimidinderivate und ihre verwendung |
| GB9508538D0 (en) | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quinazoline derivatives |
| US5880141A (en) | 1995-06-07 | 1999-03-09 | Sugen, Inc. | Benzylidene-Z-indoline compounds for the treatment of disease |
| US5843901A (en) | 1995-06-07 | 1998-12-01 | Advanced Research & Technology Institute | LHRH antagonist peptides |
| SI9620103A (sl) | 1995-07-06 | 1998-10-31 | Novartis Ag | Pirolopirimidini in postopki za njihovo pripravo |
| GB9516842D0 (en) | 1995-08-17 | 1995-10-18 | Ciba Geigy Ag | Various acylated oligopeptides |
| GB9517060D0 (en) | 1995-08-17 | 1995-10-25 | Ciba Geigy Ag | Acylated oligopeptide derivatives |
| CH690773A5 (de) | 1996-02-01 | 2001-01-15 | Novartis Ag | Pyrrolo(2,3-d)pyrimide und ihre Verwendung. |
| US5760041A (en) | 1996-02-05 | 1998-06-02 | American Cyanamid Company | 4-aminoquinazoline EGFR Inhibitors |
| GB9603095D0 (en) | 1996-02-14 | 1996-04-10 | Zeneca Ltd | Quinazoline derivatives |
| AU1794697A (en) | 1996-03-06 | 1997-09-22 | Novartis Ag | 7-alkyl-pyrrolo{2,3-d}pyrimidines |
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- 2010-09-10 CN CN2010800506564A patent/CN102596963A/zh active Pending
- 2010-09-10 EA EA201200471A patent/EA201200471A1/ru unknown
- 2010-09-10 KR KR1020127009095A patent/KR20120093867A/ko not_active Withdrawn
- 2010-09-10 IN IN2139DEN2012 patent/IN2012DN02139A/en unknown
- 2010-09-10 MX MX2012002997A patent/MX2012002997A/es not_active Application Discontinuation
- 2010-09-10 EP EP10763143A patent/EP2475668A1/en not_active Withdrawn
- 2010-09-10 CA CA2773661A patent/CA2773661A1/en not_active Abandoned
- 2010-09-10 AU AU2010294209A patent/AU2010294209A1/en not_active Abandoned
- 2010-09-10 WO PCT/EP2010/063334 patent/WO2011029915A1/en active Application Filing
- 2010-09-10 JP JP2012528376A patent/JP2013504543A/ja active Pending
- 2010-09-10 BR BR112012005400A patent/BR112012005400A2/pt not_active Application Discontinuation
- 2010-09-10 US US13/394,534 patent/US20120165310A1/en not_active Abandoned
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| WO2001072751A1 (en) * | 2000-03-29 | 2001-10-04 | Knoll Gesellschaft Mit Beschraenkter Haftung | Pyrrolopyrimidines as tyrosine kinase inhibitors |
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| CN1898240A (zh) * | 2003-10-15 | 2007-01-17 | Osi制药公司 | 咪唑并吡嗪类酪氨酸激酶抑制剂 |
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| WO2018000550A1 (zh) * | 2016-06-29 | 2018-01-04 | 四川大学华西医院 | 吡唑并[3,4-d]嘧啶衍生物 |
| US10611771B2 (en) | 2016-06-29 | 2020-04-07 | West China Hospital, Sichuan University | Pyrazolo [3,4-d] pyrimidine derivative |
| CN107098909A (zh) * | 2017-05-19 | 2017-08-29 | 四川大学华西医院 | 烷氧端基寡peg修饰的氨基嘧啶衍生物及抗肿瘤应用 |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2010294209A1 (en) | 2012-03-29 |
| JP2013504543A (ja) | 2013-02-07 |
| BR112012005400A2 (pt) | 2016-04-05 |
| WO2011029915A1 (en) | 2011-03-17 |
| EP2475668A1 (en) | 2012-07-18 |
| KR20120093867A (ko) | 2012-08-23 |
| US20120165310A1 (en) | 2012-06-28 |
| EA201200471A1 (ru) | 2012-10-30 |
| CA2773661A1 (en) | 2011-03-17 |
| MX2012002997A (es) | 2012-08-01 |
| IN2012DN02139A (OSRAM) | 2015-08-07 |
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