JP2006505509A5 - - Google Patents
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- Publication number
- JP2006505509A5 JP2006505509A5 JP2004521770A JP2004521770A JP2006505509A5 JP 2006505509 A5 JP2006505509 A5 JP 2006505509A5 JP 2004521770 A JP2004521770 A JP 2004521770A JP 2004521770 A JP2004521770 A JP 2004521770A JP 2006505509 A5 JP2006505509 A5 JP 2006505509A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- compound
- substituted lower
- ring system
- cancer
- 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 description 60
- 125000004122 cyclic group Chemical group 0.000 claims description 49
- 125000000217 alkyl group Chemical group 0.000 claims description 43
- 229920006395 saturated elastomer Polymers 0.000 claims description 42
- 125000004429 atom Chemical group 0.000 claims description 28
- 238000004132 cross linking Methods 0.000 claims description 18
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 16
- 229910052760 oxygen Inorganic materials 0.000 claims description 16
- 125000000623 heterocyclic group Chemical group 0.000 claims description 15
- 125000004193 piperazinyl group Chemical group 0.000 claims description 14
- 229910052799 carbon Inorganic materials 0.000 claims description 12
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 10
- 239000001301 oxygen Substances 0.000 claims description 10
- 229910052736 halogen Inorganic materials 0.000 claims description 9
- 150000002367 halogens Chemical class 0.000 claims description 9
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 8
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 8
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 8
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims description 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 7
- 125000005842 heteroatom Chemical group 0.000 claims description 7
- 229910052757 nitrogen Inorganic materials 0.000 claims description 7
- 125000003107 substituted aryl group Chemical group 0.000 claims description 7
- 125000004953 trihalomethyl group Chemical group 0.000 claims description 7
- ZQHJAAMMKABEBS-UHFFFAOYSA-N morpholin-2-one Chemical group O=C1CNCCO1 ZQHJAAMMKABEBS-UHFFFAOYSA-N 0.000 claims description 6
- 229910052698 phosphorus Inorganic materials 0.000 claims description 6
- 229910052717 sulfur Inorganic materials 0.000 claims description 6
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims description 4
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical group C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 4
- 150000001721 carbon Chemical group 0.000 claims description 4
- 125000003386 piperidinyl group Chemical group 0.000 claims description 4
- 229910001873 dinitrogen Inorganic materials 0.000 claims description 2
- 125000001434 methanylylidene group Chemical group [H]C#[*] 0.000 claims description 2
- 238000006467 substitution reaction Methods 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 10
- 150000004677 hydrates Chemical class 0.000 claims 8
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- 229910052801 chlorine Inorganic materials 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 4
- 229910052794 bromium Inorganic materials 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 230000000694 effects Effects 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 208000002699 Digestive System Neoplasms Diseases 0.000 claims 3
- 208000024558 digestive system cancer Diseases 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 201000010231 gastrointestinal system cancer Diseases 0.000 claims 3
- 208000005017 glioblastoma Diseases 0.000 claims 3
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 3
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 3
- 206010005003 Bladder cancer Diseases 0.000 claims 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 2
- 206010029260 Neuroblastoma Diseases 0.000 claims 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 108091000080 Phosphotransferase Proteins 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims 2
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 2
- 125000005018 aryl alkenyl group Chemical group 0.000 claims 2
- 125000005015 aryl alkynyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 201000010881 cervical cancer Diseases 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims 2
- 102000012803 ephrin Human genes 0.000 claims 2
- 108060002566 ephrin Proteins 0.000 claims 2
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 2
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 2
- 201000004101 esophageal cancer Diseases 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000004449 heterocyclylalkenyl group Chemical group 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims 2
- 201000011682 nervous system cancer Diseases 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 102000020233 phosphotransferase Human genes 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- 125000000547 substituted alkyl group Chemical group 0.000 claims 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims 2
- 101100381481 Caenorhabditis elegans baz-2 gene Proteins 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 101100372762 Rattus norvegicus Flt1 gene Proteins 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 206010046431 Urethral cancer Diseases 0.000 claims 1
- 206010046458 Urethral neoplasms Diseases 0.000 claims 1
- 108010053099 Vascular Endothelial Growth Factor Receptor-2 Proteins 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 208000003362 bronchogenic carcinoma Diseases 0.000 claims 1
- 230000001413 cellular effect Effects 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 208000029078 coronary artery disease Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 125000005415 substituted alkoxy group Chemical group 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US39626902P | 2002-07-15 | 2002-07-15 | |
| US60/396,269 | 2002-07-15 | ||
| US44721203P | 2003-02-13 | 2003-02-13 | |
| US60/447,212 | 2003-02-13 | ||
| PCT/US2003/021923 WO2004006846A2 (en) | 2002-07-15 | 2003-07-14 | Receptor-type kinase modulators and methods of use |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010259281A Division JP2011079844A (ja) | 2002-07-15 | 2010-11-19 | 受容体型キナーゼモジュレーターおよびその使用方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2006505509A JP2006505509A (ja) | 2006-02-16 |
| JP2006505509A5 true JP2006505509A5 (https=) | 2010-07-29 |
| JP4703183B2 JP4703183B2 (ja) | 2011-06-15 |
Family
ID=30118575
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004521770A Expired - Fee Related JP4703183B2 (ja) | 2002-07-15 | 2003-07-14 | 受容体型キナーゼモジュレーターおよびその使用方法 |
| JP2010259281A Pending JP2011079844A (ja) | 2002-07-15 | 2010-11-19 | 受容体型キナーゼモジュレーターおよびその使用方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010259281A Pending JP2011079844A (ja) | 2002-07-15 | 2010-11-19 | 受容体型キナーゼモジュレーターおよびその使用方法 |
Country Status (7)
| Country | Link |
|---|---|
| US (5) | US7576074B2 (https=) |
| EP (3) | EP2280003B1 (https=) |
| JP (2) | JP4703183B2 (https=) |
| AU (2) | AU2003249212C1 (https=) |
| CA (1) | CA2491191C (https=) |
| ES (1) | ES2400339T3 (https=) |
| WO (1) | WO2004006846A2 (https=) |
Families Citing this family (72)
| Publication number | Priority date | Publication date | Assignee | Title |
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| EP2280003B1 (en) | 2002-07-15 | 2014-04-02 | Symphony Evolution, Inc. | Process for preparing receptor-type kinase modulators |
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| AU2004272346A1 (en) * | 2003-09-16 | 2005-03-24 | Astrazeneca Ab | Quinazoline derivatives |
| ES2305844T3 (es) | 2003-09-16 | 2008-11-01 | Astrazeneca Ab | Derivados de quinazolina como inhibidores de tirosina cinasa. |
| WO2005028469A1 (en) | 2003-09-19 | 2005-03-31 | Astrazeneca Ab | Quinazoline derivatives |
| GB0322409D0 (en) * | 2003-09-25 | 2003-10-29 | Astrazeneca Ab | Quinazoline derivatives |
| PT2213661E (pt) | 2003-09-26 | 2011-12-15 | Exelixis Inc | Moduladores de c-met e métodos de uso |
| US20050192314A1 (en) | 2003-11-13 | 2005-09-01 | Ambit Biosciences Corporation | Urea derivatives as C-kit modulators |
| GB0326459D0 (en) | 2003-11-13 | 2003-12-17 | Astrazeneca Ab | Quinazoline derivatives |
| MX2007007645A (es) * | 2004-12-22 | 2007-08-06 | Bayer Schering Pharma Ag | Derivado de quinolina, su uso, preparacion y medicamento que lo contiene. |
| FR2889200B1 (fr) | 2005-07-27 | 2008-01-04 | Inst Vaisseaux Et Du Sang Ass | Systeme marqueur cellulaire/ligand, ou le marqueur est du type eph, materiau cellulaire comprenant ce systeme, procede de preparation et utilisation proangiogenique |
| ATE483972T1 (de) * | 2006-02-16 | 2010-10-15 | Ventana Med Syst Inc | Reagenzien und verfahren für krebsprognose und pathologische einstufung |
| WO2008020302A2 (en) * | 2006-08-17 | 2008-02-21 | Pfizer Products Inc. | Heteroaromatic quinoline-based compounds as phosphodiesterase (pde) inhibitors |
| WO2008076415A1 (en) | 2006-12-14 | 2008-06-26 | Exelixis, Inc. | Methods of using mek inhibitors |
| US7638541B2 (en) | 2006-12-28 | 2009-12-29 | Metabolex Inc. | 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine |
| JP2010523670A (ja) * | 2007-04-10 | 2010-07-15 | エクセリクシス， インク． | Ｐｉ３ｋアルファのピリドピリミジノン阻害剤を使用した治療方法 |
| DE102007024470A1 (de) | 2007-05-24 | 2008-11-27 | Bayer Schering Pharma Aktiengesellschaft | Neue Sulfoximin-substituierte Chinolin- bzw. Chinazolinderivate als Kinase-Inhibitoren |
| AU2008279447A1 (en) | 2007-07-19 | 2009-01-29 | Metabolex, Inc. | N-azacyclic substituted pyrrole, pyrazole, imidazole, triazole and tetrazole derivatives as agonists of the RUP3 or GPR119 receptor for the treatment of diabetes and metabolic disorders |
| EP2072502A1 (de) | 2007-12-20 | 2009-06-24 | Bayer Schering Pharma Aktiengesellschaft | Sulfoximid-substituierte Chinolin- und Chinazolinderivate als Kinase-Inhibitoren |
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| UA108618C2 (uk) | 2009-08-07 | 2015-05-25 | Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку | |
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| CA2784119A1 (en) * | 2009-12-15 | 2011-06-23 | Neurop, Inc. | Compounds for the treatment of neurologic disorders |
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| CN103313713B (zh) | 2010-08-26 | 2014-12-31 | 和谐进化股份有限公司 | 受体型激酶调节剂和多囊性肾病的治疗方法 |
| CN102382065B (zh) * | 2010-08-30 | 2014-05-28 | 山东轩竹医药科技有限公司 | 苯胺取代的喹唑啉衍生物 |
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| CN103804308A (zh) * | 2012-11-06 | 2014-05-21 | 天津药物研究院 | 7-取代环己基喹唑啉衍生物及其制备方法和用途 |
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| HRP20190101T1 (hr) | 2013-04-05 | 2019-03-08 | Boehringer Ingelheim International Gmbh | Terapeutske uporabe empagliflozina |
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| KR20250097990A (ko) | 2016-11-10 | 2025-06-30 | 베링거 인겔하임 인터내셔날 게엠베하 | 약제학적 조성물, 치료 방법 및 이의 용도 |
| EP3548007A4 (en) | 2016-12-01 | 2020-08-12 | Ignyta, Inc. | METHOD OF TREATMENT OF CANCER |
| US12600726B2 (en) | 2017-07-12 | 2026-04-14 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor M4 |
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| CN111788182B (zh) | 2018-02-02 | 2023-09-26 | 范德堡大学 | 毒蕈碱性乙酰胆碱受体m4的拮抗剂 |
| CN110229172B (zh) * | 2018-03-06 | 2020-12-25 | 北京赛特明强医药科技有限公司 | 一种酰基取代的噁嗪并喹唑啉类化合物、制备方法及其应用 |
| GB201909468D0 (en) | 2019-07-01 | 2019-08-14 | Karus Therapeutics Ltd | Compounds for treating cancer |
| CN112442045B (zh) * | 2019-09-03 | 2022-02-18 | 北京赛特明强医药科技有限公司 | 一种酰基取代的噁嗪并喹唑啉类化合物、制备方法及其应用 |
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-
2003
- 2003-07-14 EP EP10184164.1A patent/EP2280003B1/en not_active Expired - Lifetime
- 2003-07-14 CA CA2491191A patent/CA2491191C/en not_active Expired - Lifetime
- 2003-07-14 EP EP10183590A patent/EP2277867B1/en not_active Expired - Lifetime
- 2003-07-14 AU AU2003249212A patent/AU2003249212C1/en not_active Expired
- 2003-07-14 ES ES10183590T patent/ES2400339T3/es not_active Expired - Lifetime
- 2003-07-14 WO PCT/US2003/021923 patent/WO2004006846A2/en not_active Ceased
- 2003-07-14 JP JP2004521770A patent/JP4703183B2/ja not_active Expired - Fee Related
- 2003-07-14 US US10/522,004 patent/US7576074B2/en active Active
- 2003-07-14 EP EP03764599.1A patent/EP1521747B1/en not_active Expired - Lifetime
-
2009
- 2009-06-08 US US12/455,867 patent/US8658654B2/en not_active Expired - Fee Related
-
2010
- 2010-10-01 AU AU2010226916A patent/AU2010226916B2/en not_active Expired
- 2010-11-19 JP JP2010259281A patent/JP2011079844A/ja active Pending
-
2013
- 2013-10-22 US US14/060,123 patent/US9359332B2/en not_active Expired - Fee Related
-
2015
- 2015-09-04 US US14/845,763 patent/US9796704B2/en not_active Expired - Fee Related
-
2017
- 2017-08-31 US US15/692,445 patent/US10266518B2/en not_active Expired - Lifetime
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