JP2006524710A5 - - Google Patents
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- JP2006524710A5 JP2006524710A5 JP2006513386A JP2006513386A JP2006524710A5 JP 2006524710 A5 JP2006524710 A5 JP 2006524710A5 JP 2006513386 A JP2006513386 A JP 2006513386A JP 2006513386 A JP2006513386 A JP 2006513386A JP 2006524710 A5 JP2006524710 A5 JP 2006524710A5
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- JP
- Japan
- Prior art keywords
- conjugate
- kinase
- independently
- formula
- conjugate according
- 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 22
- 229910052760 oxygen Inorganic materials 0.000 claims 21
- 229910052757 nitrogen Inorganic materials 0.000 claims 19
- 239000000203 mixture Substances 0.000 claims 14
- 125000004432 carbon atom Chemical group C* 0.000 claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 108091000080 Phosphotransferase Proteins 0.000 claims 6
- 102000020233 phosphotransferase Human genes 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 229940043355 kinase inhibitor Drugs 0.000 claims 4
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 4
- 125000006239 protecting group Chemical group 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000012453 solvate Substances 0.000 claims 4
- 102000001301 EGF receptor Human genes 0.000 claims 3
- 108060006698 EGF receptor Proteins 0.000 claims 3
- 101001059454 Homo sapiens Serine/threonine-protein kinase MARK2 Proteins 0.000 claims 3
- 101000934996 Homo sapiens Tyrosine-protein kinase JAK3 Proteins 0.000 claims 3
- 108090000744 Mitogen-Activated Protein Kinase Kinases Proteins 0.000 claims 3
- 102000004232 Mitogen-Activated Protein Kinase Kinases Human genes 0.000 claims 3
- 108010055723 PDGF receptor tyrosine kinase Proteins 0.000 claims 3
- 102000003923 Protein Kinase C Human genes 0.000 claims 3
- 108090000315 Protein Kinase C Proteins 0.000 claims 3
- 102100028904 Serine/threonine-protein kinase MARK2 Human genes 0.000 claims 3
- 102100025387 Tyrosine-protein kinase JAK3 Human genes 0.000 claims 3
- 108010056708 bcr-abl Fusion Proteins Proteins 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 229940079593 drug Drugs 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 230000002401 inhibitory effect Effects 0.000 claims 3
- 108010042209 insulin receptor tyrosine kinase Proteins 0.000 claims 3
- 229960004441 tyrosine Drugs 0.000 claims 3
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims 2
- 239000005517 L01XE01 - Imatinib Substances 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000002837 carbocyclic group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 150000002430 hydrocarbons Chemical group 0.000 claims 2
- KTUFNOKKBVMGRW-UHFFFAOYSA-N imatinib Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 KTUFNOKKBVMGRW-UHFFFAOYSA-N 0.000 claims 2
- 238000001727 in vivo Methods 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 125000005647 linker group Chemical group 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- ALBODLTZUXKBGZ-JUUVMNCLSA-N (2s)-2-amino-3-phenylpropanoic acid;(2s)-2,6-diaminohexanoic acid Chemical compound NCCCC[C@H](N)C(O)=O.OC(=O)[C@@H](N)CC1=CC=CC=C1 ALBODLTZUXKBGZ-JUUVMNCLSA-N 0.000 claims 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000005862 (C1-C6)alkanoyl group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- GFMMXOIFOQCCGU-UHFFFAOYSA-N 2-(2-chloro-4-iodoanilino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide Chemical compound C=1C=C(I)C=C(Cl)C=1NC1=C(F)C(F)=CC=C1C(=O)NOCC1CC1 GFMMXOIFOQCCGU-UHFFFAOYSA-N 0.000 claims 1
- MLDQJTXFUGDVEO-UHFFFAOYSA-N BAY-43-9006 Chemical compound C1=NC(C(=O)NC)=CC(OC=2C=CC(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 MLDQJTXFUGDVEO-UHFFFAOYSA-N 0.000 claims 1
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- CKLJMWTZIZZHCS-UWTATZPHSA-N D-aspartic acid Chemical compound OC(=O)[C@H](N)CC(O)=O CKLJMWTZIZZHCS-UWTATZPHSA-N 0.000 claims 1
- -1 Drampimod Chemical compound 0.000 claims 1
- 101710200424 Inosine-5'-monophosphate dehydrogenase Proteins 0.000 claims 1
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 claims 1
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 claims 1
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims 1
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims 1
- UIARLYUEJFELEN-LROUJFHJSA-N LSM-1231 Chemical compound C12=C3N4C5=CC=CC=C5C3=C3C(=O)NCC3=C2C2=CC=CC=C2N1[C@]1(C)[C@](CO)(O)C[C@H]4O1 UIARLYUEJFELEN-LROUJFHJSA-N 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 241001465754 Metazoa Species 0.000 claims 1
- ABLZXFCXXLZCGV-UHFFFAOYSA-N Phosphorous acid Chemical group OP(O)=O ABLZXFCXXLZCGV-UHFFFAOYSA-N 0.000 claims 1
- 239000004473 Threonine Substances 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000004423 acyloxy group Chemical group 0.000 claims 1
- 125000004450 alkenylene group Chemical group 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 125000004419 alkynylene group Chemical group 0.000 claims 1
- IYABWNGZIDDRAK-UHFFFAOYSA-N allene Chemical group C=C=C IYABWNGZIDDRAK-UHFFFAOYSA-N 0.000 claims 1
- 229940024606 amino acid Drugs 0.000 claims 1
- 150000001413 amino acids Chemical class 0.000 claims 1
- 230000002924 anti-infective effect Effects 0.000 claims 1
- 230000003110 anti-inflammatory effect Effects 0.000 claims 1
- 230000000340 anti-metabolite Effects 0.000 claims 1
- 229940100197 antimetabolite Drugs 0.000 claims 1
- 239000002256 antimetabolite Substances 0.000 claims 1
- 239000003443 antiviral agent Substances 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 229960005261 aspartic acid Drugs 0.000 claims 1
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 125000002993 cycloalkylene group Chemical group 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229960001433 erlotinib Drugs 0.000 claims 1
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical group C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 claims 1
- 229960002584 gefitinib Drugs 0.000 claims 1
- 229940080856 gleevec Drugs 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 1
- 229960002885 histidine Drugs 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 229960002411 imatinib Drugs 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 238000013160 medical therapy Methods 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- BMGQWWVMWDBQGC-IIFHNQTCSA-N midostaurin Chemical compound CN([C@H]1[C@H]([C@]2(C)O[C@@H](N3C4=CC=CC=C4C4=C5C(=O)NCC5=C5C6=CC=CC=C6N2C5=C43)C1)OC)C(=O)C1=CC=CC=C1 BMGQWWVMWDBQGC-IIFHNQTCSA-N 0.000 claims 1
- 229950010895 midostaurin Drugs 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 239000002777 nucleoside Substances 0.000 claims 1
- 150000003833 nucleoside derivatives Chemical class 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000004437 phosphorous atom Chemical group 0.000 claims 1
- 229920000729 poly(L-lysine) polymer Polymers 0.000 claims 1
- 229920002643 polyglutamic acid Polymers 0.000 claims 1
- 108010055896 polyornithine Proteins 0.000 claims 1
- 108010000222 polyserine Proteins 0.000 claims 1
- 108090000765 processed proteins & peptides Proteins 0.000 claims 1
- QQONPFPTGQHPMA-UHFFFAOYSA-N propylene Natural products CC=C QQONPFPTGQHPMA-UHFFFAOYSA-N 0.000 claims 1
- 125000004805 propylene group Chemical group [H]C([H])([H])C([H])([*:1])C([H])([H])[*:2] 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 229930195734 saturated hydrocarbon Natural products 0.000 claims 1
- 229960003787 sorafenib Drugs 0.000 claims 1
- UXXQOJXBIDBUAC-UHFFFAOYSA-N tandutinib Chemical compound COC1=CC2=C(N3CCN(CC3)C(=O)NC=3C=CC(OC(C)C)=CC=3)N=CN=C2C=C1OCCCN1CCCCC1 UXXQOJXBIDBUAC-UHFFFAOYSA-N 0.000 claims 1
- 229960002898 threonine Drugs 0.000 claims 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 claims 1
- 229930195735 unsaturated hydrocarbon Natural products 0.000 claims 1
- 0 CCCC(C)(C*(CC)[N+](C(*)(*)*)[O-])OC1(C)C=CC(CC)=CC=C1 Chemical compound CCCC(C)(C*(CC)[N+](C(*)(*)*)[O-])OC1(C)C=CC(CC)=CC=C1 0.000 description 2
Applications Claiming Priority (19)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US46556903P | 2003-04-25 | 2003-04-25 | |
| US46546503P | 2003-04-25 | 2003-04-25 | |
| US46559403P | 2003-04-25 | 2003-04-25 | |
| US46558803P | 2003-04-25 | 2003-04-25 | |
| US49568503P | 2003-08-15 | 2003-08-15 | |
| US49568603P | 2003-08-15 | 2003-08-15 | |
| US49552703P | 2003-08-15 | 2003-08-15 | |
| US49538203P | 2003-08-15 | 2003-08-15 | |
| US51392503P | 2003-10-24 | 2003-10-24 | |
| US51436803P | 2003-10-24 | 2003-10-24 | |
| US51411503P | 2003-10-24 | 2003-10-24 | |
| US51432403P | 2003-10-24 | 2003-10-24 | |
| US51420703P | 2003-10-24 | 2003-10-24 | |
| US51395603P | 2003-10-24 | 2003-10-24 | |
| US51433003P | 2003-10-24 | 2003-10-24 | |
| US51397403P | 2003-10-24 | 2003-10-24 | |
| US53193203P | 2003-12-22 | 2003-12-22 | |
| US53605404P | 2004-01-12 | 2004-01-12 | |
| PCT/US2004/013062 WO2004096234A2 (en) | 2003-04-25 | 2004-04-26 | Kinase inhibitor phosphonate conjugates |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007114889A Division JP2007291111A (ja) | 2003-04-25 | 2007-04-24 | キナーゼインヒビターホスホネート抱合体 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2006524710A JP2006524710A (ja) | 2006-11-02 |
| JP2006524710A5 true JP2006524710A5 (https=) | 2007-07-19 |
Family
ID=33425953
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006513386A Withdrawn JP2006524710A (ja) | 2003-04-25 | 2004-04-26 | キナーゼインヒビターホスホネート抱合体 |
| JP2007114889A Withdrawn JP2007291111A (ja) | 2003-04-25 | 2007-04-24 | キナーゼインヒビターホスホネート抱合体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007114889A Withdrawn JP2007291111A (ja) | 2003-04-25 | 2007-04-24 | キナーゼインヒビターホスホネート抱合体 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US7417055B2 (https=) |
| EP (1) | EP1620109A2 (https=) |
| JP (2) | JP2006524710A (https=) |
| KR (1) | KR20060022647A (https=) |
| AU (1) | AU2004233897A1 (https=) |
| CA (1) | CA2522845A1 (https=) |
| EA (1) | EA200501676A1 (https=) |
| MX (1) | MXPA05011296A (https=) |
| NO (1) | NO20055590L (https=) |
| WO (1) | WO2004096234A2 (https=) |
Families Citing this family (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2003231765B9 (en) | 2002-04-26 | 2010-01-28 | Gilead Sciences, Inc. | Cellular accumulation of phosphonate analogs of HIV protease inhibitor compounds and the compounds as such |
| US7141035B2 (en) * | 2003-03-28 | 2006-11-28 | Sherwood Services Ag | Catheter with occlusion resistant tip |
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| US7407965B2 (en) | 2003-04-25 | 2008-08-05 | Gilead Sciences, Inc. | Phosphonate analogs for treating metabolic diseases |
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| WO2005002626A2 (en) | 2003-04-25 | 2005-01-13 | Gilead Sciences, Inc. | Therapeutic phosphonate compounds |
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| US7452901B2 (en) | 2003-04-25 | 2008-11-18 | Gilead Sciences, Inc. | Anti-cancer phosphonate analogs |
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| US7273716B2 (en) | 2003-04-25 | 2007-09-25 | Gilead Sciences, Inc. | Methods and compositions for identifying therapeutic compounds with GS-7340 ester hydrolase |
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| EP2345657A1 (en) | 2003-05-30 | 2011-07-20 | Pharmasset, Inc. | Modified fluorinated nucleoside analogues |
| US7427624B2 (en) | 2003-10-24 | 2008-09-23 | Gilead Sciences, Inc. | Purine nucleoside phosphorylase inhibitory phosphonate compounds |
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| NO20035682D0 (no) * | 2003-12-18 | 2003-12-18 | Amersham Health As | Optisk avbildning av ösofagkreft og Barretts ösofag |
| NO20035681D0 (no) * | 2003-12-18 | 2003-12-18 | Amersham Health As | Optisk avbildning av lungekreft |
| CA2548951A1 (en) * | 2003-12-22 | 2005-07-14 | Gilead Sciences, Inc. | Kinase inhibitor phosphonate conjugates |
| WO2005063751A1 (en) | 2003-12-22 | 2005-07-14 | Gilead Sciences, Inc. | 4’-substituted carbovir-and abacavir-derivatives as well as related compounds with hiv and hcv antiviral activity |
| CN101023094B (zh) | 2004-07-21 | 2011-05-18 | 法莫赛特股份有限公司 | 烷基取代的2-脱氧-2-氟代-d-呋喃核糖基嘧啶和嘌呤及其衍生物的制备 |
| ME03423B (me) | 2004-07-27 | 2020-01-20 | Gilead Sciences Inc | Fosfonatni analozi jedinjenja hiv inhibitora |
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| JP2014503499A (ja) | 2010-11-18 | 2014-02-13 | シンタ ファーマスーティカルズ コーポレーション | 低酸素状態に基づく治療に適した被験体の事前選択 |
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| US8889159B2 (en) | 2011-11-29 | 2014-11-18 | Gilead Pharmasset Llc | Compositions and methods for treating hepatitis C virus |
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| ES2739749T3 (es) * | 2015-05-18 | 2020-02-03 | Tolero Pharmaceuticals Inc | Profármacos de alvocidib que tienen biodisponibilidad aumentada |
| MX2018001289A (es) | 2015-08-03 | 2018-04-30 | Tolero Pharmaceuticals Inc | Terapias de combinacion para el tratamiento del cancer. |
| AU2017231824B2 (en) | 2016-03-09 | 2021-07-01 | Alios Biopharma, Inc. | Acyclic antivirals |
| WO2018094275A1 (en) | 2016-11-18 | 2018-05-24 | Tolero Pharmaceuticals, Inc. | Alvocidib prodrugs and their use as protein kinase inhibitors |
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2004
- 2004-04-26 MX MXPA05011296A patent/MXPA05011296A/es not_active Application Discontinuation
- 2004-04-26 US US10/832,811 patent/US7417055B2/en not_active Expired - Fee Related
- 2004-04-26 JP JP2006513386A patent/JP2006524710A/ja not_active Withdrawn
- 2004-04-26 KR KR1020057020117A patent/KR20060022647A/ko not_active Withdrawn
- 2004-04-26 CA CA002522845A patent/CA2522845A1/en not_active Abandoned
- 2004-04-26 WO PCT/US2004/013062 patent/WO2004096234A2/en not_active Ceased
- 2004-04-26 EA EA200501676A patent/EA200501676A1/ru unknown
- 2004-04-26 EP EP04750806A patent/EP1620109A2/en not_active Withdrawn
- 2004-04-26 AU AU2004233897A patent/AU2004233897A1/en not_active Abandoned
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2005
- 2005-11-25 NO NO20055590A patent/NO20055590L/no not_active Application Discontinuation
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2007
- 2007-04-24 JP JP2007114889A patent/JP2007291111A/ja not_active Withdrawn
-
2008
- 2008-07-02 US US12/167,038 patent/US20090181930A1/en not_active Abandoned
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