JP2006507299A5 - - Google Patents
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- JP2006507299A5 JP2006507299A5 JP2004550130A JP2004550130A JP2006507299A5 JP 2006507299 A5 JP2006507299 A5 JP 2006507299A5 JP 2004550130 A JP2004550130 A JP 2004550130A JP 2004550130 A JP2004550130 A JP 2004550130A JP 2006507299 A5 JP2006507299 A5 JP 2006507299A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- benzyl
- phenylthieno
- pyrazin
- cycloalkyl
- 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
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- 125000000623 heterocyclic group Chemical group 0.000 claims 24
- 150000001875 compounds Chemical class 0.000 claims 22
- 125000003118 aryl group Chemical group 0.000 claims 18
- 125000000217 alkyl group Chemical group 0.000 claims 16
- 239000003814 drug Substances 0.000 claims 12
- 229940079593 drug Drugs 0.000 claims 12
- 239000008194 pharmaceutical composition Substances 0.000 claims 12
- 125000001424 substituent group Chemical group 0.000 claims 10
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 9
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 9
- 125000000304 alkynyl group Chemical group 0.000 claims 8
- 229910052757 nitrogen Inorganic materials 0.000 claims 8
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 7
- 125000003342 alkenyl group Chemical group 0.000 claims 7
- 125000000753 cycloalkyl group Chemical group 0.000 claims 7
- 125000005865 C2-C10alkynyl group Chemical group 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- 239000003112 inhibitor Substances 0.000 claims 6
- 125000002950 monocyclic group Chemical group 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 125000005843 halogen group Chemical group 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- VEEGZPWAAPPXRB-BJMVGYQFSA-N (3e)-3-(1h-imidazol-5-ylmethylidene)-1h-indol-2-one Chemical compound O=C1NC2=CC=CC=C2\C1=C/C1=CN=CN1 VEEGZPWAAPPXRB-BJMVGYQFSA-N 0.000 claims 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 4
- 229940121369 angiogenesis inhibitor Drugs 0.000 claims 4
- 239000004037 angiogenesis inhibitor Substances 0.000 claims 4
- 239000003937 drug carrier Substances 0.000 claims 4
- 239000002834 estrogen receptor modulator Substances 0.000 claims 4
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- UCOJJLRFYUCWKS-UHFFFAOYSA-N 3-[1-[[4-(2-phenylthieno[3,4-b]pyrazin-3-yl)phenyl]methyl]piperidin-4-yl]-1h-benzimidazol-2-one Chemical compound O=C1NC2=CC=CC=C2N1C(CC1)CCN1CC(C=C1)=CC=C1C1=NC2=CSC=C2N=C1C1=CC=CC=C1 UCOJJLRFYUCWKS-UHFFFAOYSA-N 0.000 claims 3
- 229940122440 HIV protease inhibitor Drugs 0.000 claims 3
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 3
- 229940123468 Transferase inhibitor Drugs 0.000 claims 3
- 208000007502 anemia Diseases 0.000 claims 3
- 230000003474 anti-emetic effect Effects 0.000 claims 3
- 230000001028 anti-proliverative effect Effects 0.000 claims 3
- 229940125683 antiemetic agent Drugs 0.000 claims 3
- 239000002111 antiemetic agent Substances 0.000 claims 3
- 231100000433 cytotoxic Toxicity 0.000 claims 3
- 230000001472 cytotoxic effect Effects 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 239000004030 hiv protease inhibitor Substances 0.000 claims 3
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 3
- 230000000091 immunopotentiator Effects 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 230000036457 multidrug resistance Effects 0.000 claims 3
- 208000004235 neutropenia Diseases 0.000 claims 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 3
- 125000001844 prenyl group Chemical group [H]C([*])([H])C([H])=C(C([H])([H])[H])C([H])([H])[H] 0.000 claims 3
- 102000004169 proteins and genes Human genes 0.000 claims 3
- 108090000623 proteins and genes Proteins 0.000 claims 3
- 229940075993 receptor modulator Drugs 0.000 claims 3
- 102000027483 retinoid hormone receptors Human genes 0.000 claims 3
- 108091008679 retinoid hormone receptors Proteins 0.000 claims 3
- 239000003419 rna directed dna polymerase inhibitor Substances 0.000 claims 3
- 239000000849 selective androgen receptor modulator Substances 0.000 claims 3
- 239000003558 transferase inhibitor Substances 0.000 claims 3
- MJBOFBIPDKCUNO-OAQYLSRUSA-N 1-ethyl-3-[(3r)-1-[[4-(2-phenylthieno[3,4-b]pyrazin-3-yl)phenyl]methyl]pyrrolidin-3-yl]urea Chemical compound C1[C@H](NC(=O)NCC)CCN1CC1=CC=C(C=2C(=NC3=CSC=C3N=2)C=2C=CC=CC=2)C=C1 MJBOFBIPDKCUNO-OAQYLSRUSA-N 0.000 claims 2
- RENKTCQFQAOCAX-UHFFFAOYSA-N 2-phenyl-3-[4-[(4-purin-9-ylpiperidin-1-yl)methyl]phenyl]thieno[3,4-b]pyrazine Chemical compound C1CC(N2C3=NC=NC=C3N=C2)CCN1CC(C=C1)=CC=C1C1=NC2=CSC=C2N=C1C1=CC=CC=C1 RENKTCQFQAOCAX-UHFFFAOYSA-N 0.000 claims 2
- QBIKMVGWIQYZFN-UHFFFAOYSA-N 3-[1-[[4-(2-phenylthieno[3,4-b]pyrazin-3-yl)phenyl]methyl]-3,6-dihydro-2h-pyridin-4-yl]-1h-benzimidazol-2-one Chemical compound O=C1NC2=CC=CC=C2N1C(CC1)=CCN1CC(C=C1)=CC=C1C1=NC2=CSC=C2N=C1C1=CC=CC=C1 QBIKMVGWIQYZFN-UHFFFAOYSA-N 0.000 claims 2
- GCFRORJRTAXRIQ-UHFFFAOYSA-N 3-[4-[(2-methylbenzimidazol-1-yl)methyl]phenyl]-2-phenylthieno[3,4-b]pyrazine Chemical compound CC1=NC2=CC=CC=C2N1CC(C=C1)=CC=C1C1=NC2=CSC=C2N=C1C1=CC=CC=C1 GCFRORJRTAXRIQ-UHFFFAOYSA-N 0.000 claims 2
- RDWKSMJKIZSTIX-UHFFFAOYSA-N 3-[4-[(4-imidazo[4,5-b]pyridin-3-ylpiperidin-1-yl)methyl]phenyl]-2-phenylthieno[3,4-b]pyrazine Chemical compound C1CC(N2C3=NC=CC=C3N=C2)CCN1CC(C=C1)=CC=C1C1=NC2=CSC=C2N=C1C1=CC=CC=C1 RDWKSMJKIZSTIX-UHFFFAOYSA-N 0.000 claims 2
- WPUBAPJNLXUPGY-UHFFFAOYSA-N 6-[4-[[4-(2-oxo-3h-benzimidazol-1-yl)piperidin-1-yl]methyl]phenyl]-5-phenyl-1,2-dihydropyrazolo[3,4-b]pyrazin-3-one Chemical compound N=1C2=C(O)NN=C2N=C(C=2C=CC(CN3CCC(CC3)N3C(NC4=CC=CC=C43)=O)=CC=2)C=1C1=CC=CC=C1 WPUBAPJNLXUPGY-UHFFFAOYSA-N 0.000 claims 2
- MYRRAMLWCGCWAT-UHFFFAOYSA-N 9-[1-[[4-(2-phenylthieno[3,4-b]pyrazin-3-yl)phenyl]methyl]piperidin-4-yl]purin-6-amine Chemical compound C1=NC=2C(N)=NC=NC=2N1C(CC1)CCN1CC(C=C1)=CC=C1C1=NC2=CSC=C2N=C1C1=CC=CC=C1 MYRRAMLWCGCWAT-UHFFFAOYSA-N 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 102000001708 Protein Isoforms Human genes 0.000 claims 2
- 108010029485 Protein Isoforms Proteins 0.000 claims 2
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 claims 2
- JVKQDSZPQIIGDO-UHFFFAOYSA-N [1-[[4-(2-phenylthieno[3,4-b]pyrazin-3-yl)phenyl]methyl]benzimidazol-2-yl]methanol Chemical compound OCC1=NC2=CC=CC=C2N1CC(C=C1)=CC=C1C1=NC2=CSC=C2N=C1C1=CC=CC=C1 JVKQDSZPQIIGDO-UHFFFAOYSA-N 0.000 claims 2
- -1 benzimidazolonyl Chemical group 0.000 claims 2
- 239000003102 growth factor Substances 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- SZGLCYVOKGFRIE-OAQYLSRUSA-N n-[(3r)-1-[[4-(2-phenylthieno[3,4-b]pyrazin-3-yl)phenyl]methyl]pyrrolidin-3-yl]-1,3-thiazole-5-carboxamide Chemical compound C([C@H](C1)NC(=O)C=2SC=NC=2)CN1CC(C=C1)=CC=C1C1=NC2=CSC=C2N=C1C1=CC=CC=C1 SZGLCYVOKGFRIE-OAQYLSRUSA-N 0.000 claims 2
- SZUGMRINYQBJPH-LJQANCHMSA-N n-[(3r)-1-[[4-(3-oxo-5-phenyl-1,2-dihydropyrazolo[3,4-b]pyrazin-6-yl)phenyl]methyl]pyrrolidin-3-yl]-1,3-thiazole-5-carboxamide Chemical compound N([C@@H]1CCN(C1)CC1=CC=C(C=C1)C1=NC2=NNC(=C2N=C1C=1C=CC=CC=1)O)C(=O)C1=CN=CS1 SZUGMRINYQBJPH-LJQANCHMSA-N 0.000 claims 2
- 238000001959 radiotherapy Methods 0.000 claims 2
- 125000006664 (C1-C3) perfluoroalkyl group Chemical group 0.000 claims 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- 125000006663 (C1-C6) perfluoroalkyl group Chemical group 0.000 claims 1
- UEJJHQNACJXSKW-UHFFFAOYSA-N 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione Chemical compound O=C1C2=CC=CC=C2C(=O)N1C1CCC(=O)NC1=O UEJJHQNACJXSKW-UHFFFAOYSA-N 0.000 claims 1
- 125000004777 2-fluoroethyl group Chemical group [H]C([H])(F)C([H])([H])* 0.000 claims 1
- 102000012936 Angiostatins Human genes 0.000 claims 1
- 108010079709 Angiostatins Proteins 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- 229940122204 Cyclooxygenase inhibitor Drugs 0.000 claims 1
- 102000006992 Interferon-alpha Human genes 0.000 claims 1
- 108010047761 Interferon-alpha Proteins 0.000 claims 1
- 102000013462 Interleukin-12 Human genes 0.000 claims 1
- 108010065805 Interleukin-12 Proteins 0.000 claims 1
- 229940124761 MMP inhibitor Drugs 0.000 claims 1
- 229930012538 Paclitaxel Natural products 0.000 claims 1
- 102000010780 Platelet-Derived Growth Factor Human genes 0.000 claims 1
- 108010038512 Platelet-Derived Growth Factor Proteins 0.000 claims 1
- UIRKNQLZZXALBI-MSVGPLKSSA-N Squalamine Chemical compound C([C@@H]1C[C@H]2O)[C@@H](NCCCNCCCCN)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@H](C)CC[C@H](C(C)C)OS(O)(=O)=O)[C@@]2(C)CC1 UIRKNQLZZXALBI-MSVGPLKSSA-N 0.000 claims 1
- UIRKNQLZZXALBI-UHFFFAOYSA-N Squalamine Natural products OC1CC2CC(NCCCNCCCCN)CCC2(C)C2C1C1CCC(C(C)CCC(C(C)C)OS(O)(=O)=O)C1(C)CC2 UIRKNQLZZXALBI-UHFFFAOYSA-N 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000005275 alkylenearyl group Chemical group 0.000 claims 1
- FZCSTZYAHCUGEM-UHFFFAOYSA-N aspergillomarasmine B Natural products OC(=O)CNC(C(O)=O)CNC(C(O)=O)CC(O)=O FZCSTZYAHCUGEM-UHFFFAOYSA-N 0.000 claims 1
- DXZDEAJXVCLRLE-UHFFFAOYSA-N azepin-2-one Chemical compound O=C1C=CC=CC=N1 DXZDEAJXVCLRLE-UHFFFAOYSA-N 0.000 claims 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 210000001339 epidermal cell Anatomy 0.000 claims 1
- 210000002950 fibroblast Anatomy 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- YAMHXTCMCPHKLN-UHFFFAOYSA-N imidazolidin-2-one Chemical compound O=C1NCCN1 YAMHXTCMCPHKLN-UHFFFAOYSA-N 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 102000006495 integrins Human genes 0.000 claims 1
- 108010044426 integrins Proteins 0.000 claims 1
- 229940117681 interleukin-12 Drugs 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 229960001592 paclitaxel Drugs 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- XUWHAWMETYGRKB-UHFFFAOYSA-N piperidin-2-one Chemical compound O=C1CCCCN1 XUWHAWMETYGRKB-UHFFFAOYSA-N 0.000 claims 1
- 125000005936 piperidyl group Chemical group 0.000 claims 1
- 239000002599 prostaglandin synthase inhibitor Substances 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- VTGOHKSTWXHQJK-UHFFFAOYSA-N pyrimidin-2-ol Chemical compound OC1=NC=CC=N1 VTGOHKSTWXHQJK-UHFFFAOYSA-N 0.000 claims 1
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 229960004622 raloxifene Drugs 0.000 claims 1
- GZUITABIAKMVPG-UHFFFAOYSA-N raloxifene Chemical compound C1=CC(O)=CC=C1C1=C(C(=O)C=2C=CC(OCCN3CCCCC3)=CC=2)C2=CC=C(O)C=C2S1 GZUITABIAKMVPG-UHFFFAOYSA-N 0.000 claims 1
- 229950001248 squalamine Drugs 0.000 claims 1
- 229960001603 tamoxifen Drugs 0.000 claims 1
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 claims 1
- 229960003433 thalidomide Drugs 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 229960000575 trastuzumab Drugs 0.000 claims 1
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 claims 1
- 239000005483 tyrosine kinase inhibitor Substances 0.000 claims 1
- 150000004917 tyrosine kinase inhibitor derivatives Chemical class 0.000 claims 1
- 0 C*1CCCN(Cc(cc2)ccc2-c2nc(**C(C)(C)*3)c3nc2C2C=CC=CC2)CCCCCC1 Chemical compound C*1CCCN(Cc(cc2)ccc2-c2nc(**C(C)(C)*3)c3nc2C2C=CC=CC2)CCCCCC1 0.000 description 4
- GTDRXSGQFSLDHR-UHFFFAOYSA-N CC(C)N1c(cccc2)c2NC1 Chemical compound CC(C)N1c(cccc2)c2NC1 GTDRXSGQFSLDHR-UHFFFAOYSA-N 0.000 description 1
- UMJVKPYTXOUBSB-UHFFFAOYSA-N CC(C)[n]1c2ccccc2nc1 Chemical compound CC(C)[n]1c2ccccc2nc1 UMJVKPYTXOUBSB-UHFFFAOYSA-N 0.000 description 1
- VATSEXCEOAFVSO-UHFFFAOYSA-N CNC(c1cnc[s]1)=O Chemical compound CNC(c1cnc[s]1)=O VATSEXCEOAFVSO-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US42230702P | 2002-10-30 | 2002-10-30 | |
| PCT/US2003/034007 WO2004041162A2 (en) | 2002-10-30 | 2003-10-24 | Inhibitors of akt activity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2006507299A JP2006507299A (ja) | 2006-03-02 |
| JP2006507299A5 true JP2006507299A5 (https=) | 2006-09-14 |
Family
ID=32312489
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004550130A Pending JP2006507299A (ja) | 2002-10-30 | 2003-10-24 | Ａｋｔ活性の阻害薬 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US7399764B2 (https=) |
| EP (1) | EP1558586B1 (https=) |
| JP (1) | JP2006507299A (https=) |
| AT (1) | ATE503483T1 (https=) |
| AU (1) | AU2003284981B2 (https=) |
| CA (1) | CA2501365C (https=) |
| DE (1) | DE60336576D1 (https=) |
| WO (1) | WO2004041162A2 (https=) |
Families Citing this family (69)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE461179T1 (de) * | 2003-04-24 | 2010-04-15 | Merck Sharp & Dohme | Hemmer der akt aktivität |
| CN1809354A (zh) | 2003-04-24 | 2006-07-26 | 麦克公司 | Akt活性抑制剂 |
| US7414055B2 (en) * | 2003-04-24 | 2008-08-19 | Merck & Co., Inc. | Inhibitors of Akt activity |
| EP1620095A4 (en) * | 2003-04-24 | 2009-04-01 | Merck & Co Inc | HEMMER OF ACT ACTIVITY |
| CA2561311A1 (en) * | 2004-04-09 | 2005-10-27 | Merck & Co., Inc. | Inhibitors of akt activity |
| EP1737861A4 (en) * | 2004-04-09 | 2010-04-28 | Merck Sharp & Dohme | HEMMER OF ACT ACTIVITY |
| EP1784175A4 (en) * | 2004-08-23 | 2009-07-22 | Merck & Co Inc | INHIBITORS OF ACT ACTIVITY |
| WO2006058120A1 (en) * | 2004-11-22 | 2006-06-01 | Vertex Pharmaceuticals Incorporated | Bicyclic inhibitors or rho kinase |
| ES2382814T3 (es) | 2005-05-17 | 2012-06-13 | Merck Sharp & Dohme Ltd. | Ácido cis-4-[(4-clorofenil)sulfonil]-4-(2,5-difluorofenil)ciclohexanopropanoico para el tratamiento del cáncer |
| EP1898903B8 (en) | 2005-06-10 | 2013-05-15 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| EP1978964A4 (en) | 2006-01-24 | 2009-12-09 | Merck & Co Inc | JAK2 tyrosine kinase Inhibition |
| ATE523499T1 (de) | 2006-07-06 | 2011-09-15 | Array Biopharma Inc | Cyclopenta [d]-pyrimidine als akt-proteinkinasehemmer |
| ATE532789T1 (de) * | 2006-07-06 | 2011-11-15 | Array Biopharma Inc | Dihydrothienopyrimidine als akt-proteinkinase- inhibitoren |
| CA2656566C (en) * | 2006-07-06 | 2014-06-17 | Array Biopharma Inc. | Dihydrofuro pyrimidines as akt protein kinase inhibitors |
| US8063050B2 (en) | 2006-07-06 | 2011-11-22 | Array Biopharma Inc. | Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| AR064010A1 (es) * | 2006-12-06 | 2009-03-04 | Merck & Co Inc | Inhibidores de la actividad de la akt |
| JP2010512312A (ja) * | 2006-12-06 | 2010-04-22 | メルク エンド カムパニー インコーポレーテッド | Ａｋｔ活性の阻害剤 |
| WO2008070823A2 (en) * | 2006-12-07 | 2008-06-12 | University Of South Florida | Substrate-mimetic akt inhibitor |
| US8846683B2 (en) | 2007-07-05 | 2014-09-30 | Array Biopharma, Inc. | Pyrimidyl cyclopentanes as Akt protein kinase inhibitors |
| US9409886B2 (en) | 2007-07-05 | 2016-08-09 | Array Biopharma Inc. | Pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| WO2009006567A2 (en) | 2007-07-05 | 2009-01-08 | Array Biopharma Inc. | Pyrimidyl cyclopentanes as akt protein kinase inhibitors |
| CN101918373B (zh) | 2007-07-05 | 2013-06-05 | 阵列生物制药公司 | 作为akt蛋白激酶抑制剂的嘧啶基环戊烷 |
| EP2240455B1 (en) | 2008-01-09 | 2012-12-26 | Array Biopharma, Inc. | Hydroxylated pyrimidyl cyclopentane as akt protein kinase inhibitor |
| ES2422733T3 (es) | 2008-01-09 | 2013-09-13 | Array Biopharma Inc | Pirimidilciclopentanos hidroxilados como inhibidores de proteínas cinasas AKT |
| US20100048913A1 (en) | 2008-03-14 | 2010-02-25 | Angela Brodie | Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens;Synthesis In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity |
| US8536193B2 (en) * | 2008-06-03 | 2013-09-17 | Merck Sharp & Dohme Corp. | Inhibitors of AKT activity |
| JP2011522048A (ja) * | 2008-06-03 | 2011-07-28 | メルク・シャープ・エンド・ドーム・コーポレイション | Ａｋｔ活性の阻害剤 |
| CN102686600A (zh) | 2009-02-05 | 2012-09-19 | 托凯药业股份有限公司 | 甾体cyp17抑制剂/抗雄激素物质的新型药物前体 |
| EA201101186A1 (ru) * | 2009-02-13 | 2012-04-30 | Байер Фарма Акциенгезельшафт | Конденсированные пиримидины |
| US8168652B2 (en) | 2009-03-12 | 2012-05-01 | Merck Sharp & Dohme Corp. | Inhibitors of AKT activity |
| WO2010114780A1 (en) * | 2009-04-01 | 2010-10-07 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| PE20121172A1 (es) | 2009-10-14 | 2012-09-05 | Merck Sharp & Dohme | Piperidinas sustituidas con actividad en la hdm2 |
| CA2787079A1 (en) * | 2010-01-27 | 2011-08-04 | Vertex Pharmaceuticals Incorporated | Pyrazolopyrazine kinase inhibitors |
| WO2011163330A1 (en) | 2010-06-24 | 2011-12-29 | Merck Sharp & Dohme Corp. | Novel heterocyclic compounds as erk inhibitors |
| CA2806655A1 (en) * | 2010-07-28 | 2012-02-02 | Bayer Intellectual Property Gmbh | Substituted imidazo[1,2-b]pyridazines |
| EP3330377A1 (en) | 2010-08-02 | 2018-06-06 | Sirna Therapeutics, Inc. | Rna interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (ctnnb1) gene expression using short interfering nucleic acid (sina) |
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- 2003-10-24 JP JP2004550130A patent/JP2006507299A/ja active Pending
- 2003-10-24 EP EP03779301A patent/EP1558586B1/en not_active Expired - Lifetime
- 2003-10-24 DE DE60336576T patent/DE60336576D1/de not_active Expired - Lifetime
- 2003-10-24 CA CA2501365A patent/CA2501365C/en not_active Expired - Fee Related
- 2003-10-24 WO PCT/US2003/034007 patent/WO2004041162A2/en not_active Ceased
- 2003-10-24 AT AT03779301T patent/ATE503483T1/de not_active IP Right Cessation
- 2003-10-24 AU AU2003284981A patent/AU2003284981B2/en not_active Ceased
- 2003-10-24 US US10/530,252 patent/US7399764B2/en not_active Expired - Fee Related
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