JP2009538309A5 - - Google Patents
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- Publication number
- JP2009538309A5 JP2009538309A5 JP2009512121A JP2009512121A JP2009538309A5 JP 2009538309 A5 JP2009538309 A5 JP 2009538309A5 JP 2009512121 A JP2009512121 A JP 2009512121A JP 2009512121 A JP2009512121 A JP 2009512121A JP 2009538309 A5 JP2009538309 A5 JP 2009538309A5
- Authority
- JP
- Japan
- Prior art keywords
- administration
- compound
- sterile
- injectable
- pharmaceutically acceptable
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 description 12
- 239000000243 solution Substances 0.000 description 7
- 239000000725 suspension Substances 0.000 description 7
- 239000002904 solvent Substances 0.000 description 6
- 239000000203 mixture Substances 0.000 description 5
- 238000002360 preparation method Methods 0.000 description 5
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 4
- 239000002270 dispersing agent Substances 0.000 description 4
- 239000000346 nonvolatile oil Substances 0.000 description 4
- 238000010521 absorption reaction Methods 0.000 description 3
- 239000003085 diluting agent Substances 0.000 description 3
- 238000000034 method Methods 0.000 description 3
- 239000003921 oil Substances 0.000 description 3
- 235000019198 oils Nutrition 0.000 description 3
- 239000003981 vehicle Substances 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 2
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 2
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 description 2
- 239000005642 Oleic acid Substances 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 229920002988 biodegradable polymer Polymers 0.000 description 2
- 239000004621 biodegradable polymer Substances 0.000 description 2
- 235000019437 butane-1,3-diol Nutrition 0.000 description 2
- 238000006880 cross-coupling reaction Methods 0.000 description 2
- 239000013078 crystal Substances 0.000 description 2
- 235000014113 dietary fatty acids Nutrition 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 239000000839 emulsion Substances 0.000 description 2
- 239000000194 fatty acid Substances 0.000 description 2
- 229930195729 fatty acid Natural products 0.000 description 2
- 150000004665 fatty acids Chemical class 0.000 description 2
- 229910052736 halogen Inorganic materials 0.000 description 2
- 125000001475 halogen functional group Chemical group 0.000 description 2
- 150000002367 halogens Chemical class 0.000 description 2
- 238000001802 infusion Methods 0.000 description 2
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 description 2
- 231100000252 nontoxic Toxicity 0.000 description 2
- 230000003000 nontoxic effect Effects 0.000 description 2
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 2
- 210000000056 organ Anatomy 0.000 description 2
- 238000007911 parenteral administration Methods 0.000 description 2
- 229920000642 polymer Polymers 0.000 description 2
- 239000007921 spray Substances 0.000 description 2
- 239000000375 suspending agent Substances 0.000 description 2
- 230000000699 topical effect Effects 0.000 description 2
- 239000000080 wetting agent Substances 0.000 description 2
- RFSKGCVUDQRZSD-UHFFFAOYSA-N 3-methoxythiophene Chemical compound COC=1C=CSC=1 RFSKGCVUDQRZSD-UHFFFAOYSA-N 0.000 description 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Polymers OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 229920002732 Polyanhydride Polymers 0.000 description 1
- 229920000954 Polyglycolide Polymers 0.000 description 1
- 229920001710 Polyorthoester Polymers 0.000 description 1
- 102000001253 Protein Kinase Human genes 0.000 description 1
- 230000010933 acylation Effects 0.000 description 1
- 238000005917 acylation reaction Methods 0.000 description 1
- 239000012472 biological sample Substances 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 1
- 239000004359 castor oil Substances 0.000 description 1
- 235000019438 castor oil Nutrition 0.000 description 1
- 239000013256 coordination polymer Substances 0.000 description 1
- 230000008878 coupling Effects 0.000 description 1
- 238000010168 coupling process Methods 0.000 description 1
- 238000005859 coupling reaction Methods 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 238000010511 deprotection reaction Methods 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 239000003995 emulsifying agent Substances 0.000 description 1
- 125000004185 ester group Chemical group 0.000 description 1
- 208000030533 eye disease Diseases 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 125000000524 functional group Chemical group 0.000 description 1
- 125000005456 glyceride group Chemical group 0.000 description 1
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 1
- 230000026030 halogenation Effects 0.000 description 1
- 238000005658 halogenation reaction Methods 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 239000007972 injectable composition Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 208000028774 intestinal disease Diseases 0.000 description 1
- 238000007917 intracranial administration Methods 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 238000010255 intramuscular injection Methods 0.000 description 1
- 239000007927 intramuscular injection Substances 0.000 description 1
- 238000007912 intraperitoneal administration Methods 0.000 description 1
- 238000007919 intrasynovial administration Methods 0.000 description 1
- 238000007913 intrathecal administration Methods 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 239000002502 liposome Substances 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000006194 liquid suspension Substances 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 1
- 239000004530 micro-emulsion Substances 0.000 description 1
- 239000007922 nasal spray Substances 0.000 description 1
- 229940097496 nasal spray Drugs 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 239000004006 olive oil Substances 0.000 description 1
- 235000008390 olive oil Nutrition 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 229920000136 polysorbate Polymers 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 108060006633 protein kinase Proteins 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 238000005245 sintering Methods 0.000 description 1
- 208000017520 skin disease Diseases 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 238000010254 subcutaneous injection Methods 0.000 description 1
- 239000007929 subcutaneous injection Substances 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 150000003577 thiophenes Chemical class 0.000 description 1
- 238000011200 topical administration Methods 0.000 description 1
- 239000012049 topical pharmaceutical composition Substances 0.000 description 1
- 238000002054 transplantation Methods 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US80286706P | 2006-05-23 | 2006-05-23 | |
| PCT/US2007/012270 WO2007139816A2 (en) | 2006-05-23 | 2007-05-23 | Thiophene-carboxamides useful as inhibitors of protein kinases |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2009538309A JP2009538309A (ja) | 2009-11-05 |
| JP2009538309A5 true JP2009538309A5 (enExample) | 2010-07-01 |
Family
ID=38606563
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009512121A Pending JP2009538309A (ja) | 2006-05-23 | 2007-05-23 | プロテインキナーゼのインヒビターとして有用なチオフェンカルボキサミド |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US8853244B2 (enExample) |
| EP (2) | EP2439206A1 (enExample) |
| JP (1) | JP2009538309A (enExample) |
| CN (1) | CN101484447A (enExample) |
| AU (1) | AU2007267986A1 (enExample) |
| CA (1) | CA2652816A1 (enExample) |
| WO (1) | WO2007139816A2 (enExample) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1989205B1 (en) | 2006-01-23 | 2012-06-13 | Vertex Pharmceuticals Incorporated | Thiophene-carboxamides useful as inhibitors of protein kinases |
| EP2418210A1 (en) * | 2006-04-13 | 2012-02-15 | Vertex Pharmceuticals Incorporated | Thiophene-carboxamides useful as inhibitors of protein kinases |
| JP2009538305A (ja) | 2006-05-23 | 2009-11-05 | バーテックス ファーマシューティカルズ インコーポレイテッド | プロテインキナーゼのインヒビターとして有用なチオフェンカルボキサミド |
| CN101484447A (zh) | 2006-05-23 | 2009-07-15 | 沃泰克斯药物股份有限公司 | 可用作蛋白激酶抑制剂的噻吩-甲酰胺类 |
| US9029411B2 (en) | 2008-01-25 | 2015-05-12 | Millennium Pharmaceuticals, Inc. | Thiophenes and uses thereof |
| US9090601B2 (en) | 2009-01-30 | 2015-07-28 | Millennium Pharmaceuticals, Inc. | Thiazole derivatives |
| US8796314B2 (en) | 2009-01-30 | 2014-08-05 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| EP2391619A1 (en) | 2009-01-30 | 2011-12-07 | Millennium Pharmaceuticals, Inc. | Heteroaryls and their use as pi3k inhibitors |
| ES2603032T3 (es) | 2010-07-15 | 2017-02-23 | Bayer Intellectual Property Gmbh | Compuestos de 3-piridil-heteroarilcarboxamida como pesticidas |
| US8859768B2 (en) | 2010-08-11 | 2014-10-14 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| SG10201506238SA (en) | 2010-08-11 | 2015-09-29 | Millennium Pharm Inc | Heteroaryls And Uses Thereof |
| US9062038B2 (en) | 2010-08-11 | 2015-06-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| PE20141044A1 (es) | 2010-10-13 | 2014-09-07 | Millennium Pharm Inc | Heteroarilos y sus usos |
| AU2012225805B2 (en) * | 2011-03-04 | 2017-03-02 | Lexicon Pharmaceuticals, Inc. | MST1 kinase inhibitors and methods of their use |
| JO3407B1 (ar) | 2012-05-31 | 2019-10-20 | Eisai R&D Man Co Ltd | مركبات رباعي هيدرو بيرازولو بيريميدين |
| WO2016161145A1 (en) * | 2015-03-31 | 2016-10-06 | Dana-Farber Cancer Institute, Inc. | Stk4 inhibitors for treatment of hematologic malignancies |
| CN116057045A (zh) | 2020-06-05 | 2023-05-02 | 金耐特生物制药公司 | 成纤维细胞生长因子受体激酶抑制剂 |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1255802B (it) | 1992-08-07 | 1995-11-16 | Luso Farmaco Inst | Derivati imidazolici ad attivita' a ii antagonista |
| CA2230896A1 (en) | 1995-09-01 | 1997-03-13 | Signal Pharmaceuticals, Inc. | Pyrimidine carboxylates and related compounds and methods for treating inflammatory conditions |
| WO1998047894A1 (en) | 1997-04-24 | 1998-10-29 | Dow Agrosciences Llc | Pesticidal 3-(substituted phenyl)-5-(thienyl or furyl)-1,2,4-triazoles |
| DE19744026A1 (de) | 1997-10-06 | 1999-04-08 | Hoechst Marion Roussel De Gmbh | Pyrazol-Derivate, ihre Herstellung und ihre Verwendung in Arzneimitteln |
| EP0957099B1 (en) * | 1998-04-15 | 2002-11-20 | Pfizer Products Inc. | Heterocyclic carboxamides |
| CN1136218C (zh) | 1998-10-23 | 2004-01-28 | 道农业科学公司 | 制备3-(取代的苯基)-5-(噻吩基或呋喃基)-1,2,4-三唑的方法以及在其中使用的新中间体 |
| WO2001064646A2 (en) | 2000-03-01 | 2001-09-07 | Tularik Inc. | Hydrazones and analogs as cholesterol lowering agents |
| US7273868B2 (en) | 2000-04-28 | 2007-09-25 | Tanabe Seiyaku Co., Ltd. | Pyrazine derivatives |
| CN1638776A (zh) | 2001-06-08 | 2005-07-13 | 西托维亚公司 | 取代的3－芳基－5－芳基－[1,2,4]－噁二唑和类似物 |
| MXPA04004064A (es) * | 2001-10-30 | 2004-09-06 | Pharmacia Corp | Derivados heteroaromaticos de carboxamida para el tratramiento de la inflamacion. |
| US7064204B2 (en) | 2002-05-30 | 2006-06-20 | King Pharmacueticals Reserch And Development, Inc. | Pharmaceutically active compounds having a tricyclic pyrazolotriazolopyrimidine ring structure and methods of use |
| CA2493908A1 (en) * | 2002-08-08 | 2004-02-19 | Smithkline Beecham Corporation | Thiophene compounds |
| WO2004058253A1 (en) | 2002-12-18 | 2004-07-15 | Cytovia, Inc. | 3,5-disubstituted-[1,2,4]-oxadiazoles and analogs as activators of caspases and inducers of apoptosis and the use thereof |
| ES2326808T3 (es) | 2003-04-01 | 2009-10-20 | Smithkline Beecham Corporation | Compuestos de imidazotriazina para el tratamiento de enfermedades cancerosas. |
| US20050090529A1 (en) | 2003-07-31 | 2005-04-28 | Pfizer Inc | 3,5 Disubstituted indazole compounds with nitrogen-bearing 5-membered heterocycles, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation |
| US7465807B2 (en) | 2003-10-16 | 2008-12-16 | Smithkline Beecham Corporation | Process for preparing benzimidazole thiophenes |
| JP2007519753A (ja) | 2004-01-30 | 2007-07-19 | スミスクライン ビーチャム コーポレーション | 化合物 |
| GB0402809D0 (en) | 2004-02-09 | 2004-03-10 | Glaxo Group Ltd | Chemical compounds |
| CN1989131A (zh) * | 2004-03-30 | 2007-06-27 | 希龙公司 | 取代的噻吩衍生物用作抗癌药 |
| EP1756108A2 (en) | 2004-04-02 | 2007-02-28 | Vertex Pharmaceuticals Incorporated | Azaindoles useful as inhibitors of rock and other protein kinases |
| CN101098870B (zh) | 2004-11-08 | 2010-11-03 | 万有制药株式会社 | 新型稠环咪唑衍生物 |
| MX2007007032A (es) | 2004-12-17 | 2007-07-04 | Amgen Inc | Compuestos de aminopirimidina y metodos de uso. |
| ES2338590T3 (es) | 2005-09-06 | 2010-05-10 | Glaxosmithkline Llc | Procedimiento regioselectivo de preparacion de benzoimidazoltiofenos. |
| EP1989205B1 (en) | 2006-01-23 | 2012-06-13 | Vertex Pharmceuticals Incorporated | Thiophene-carboxamides useful as inhibitors of protein kinases |
| EP2418210A1 (en) * | 2006-04-13 | 2012-02-15 | Vertex Pharmceuticals Incorporated | Thiophene-carboxamides useful as inhibitors of protein kinases |
| CN101484447A (zh) | 2006-05-23 | 2009-07-15 | 沃泰克斯药物股份有限公司 | 可用作蛋白激酶抑制剂的噻吩-甲酰胺类 |
| JP2009538305A (ja) | 2006-05-23 | 2009-11-05 | バーテックス ファーマシューティカルズ インコーポレイテッド | プロテインキナーゼのインヒビターとして有用なチオフェンカルボキサミド |
-
2007
- 2007-05-23 CN CNA2007800257358A patent/CN101484447A/zh active Pending
- 2007-05-23 WO PCT/US2007/012270 patent/WO2007139816A2/en not_active Ceased
- 2007-05-23 CA CA002652816A patent/CA2652816A1/en not_active Abandoned
- 2007-05-23 US US11/805,418 patent/US8853244B2/en not_active Expired - Fee Related
- 2007-05-23 EP EP11184587A patent/EP2439206A1/en not_active Withdrawn
- 2007-05-23 AU AU2007267986A patent/AU2007267986A1/en not_active Abandoned
- 2007-05-23 EP EP07795219A patent/EP2027116A2/en not_active Withdrawn
- 2007-05-23 JP JP2009512121A patent/JP2009538309A/ja active Pending
-
2014
- 2014-09-02 US US14/474,887 patent/US20150038535A1/en not_active Abandoned
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