JP2006507299A5 - - Google Patents
Download PDFInfo
- Publication number
- 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
Links
- 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 (enExample) | 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 (enExample) |
| EP (1) | EP1558586B1 (enExample) |
| JP (1) | JP2006507299A (enExample) |
| AT (1) | ATE503483T1 (enExample) |
| AU (1) | AU2003284981B2 (enExample) |
| CA (1) | CA2501365C (enExample) |
| DE (1) | DE60336576D1 (enExample) |
| WO (1) | WO2004041162A2 (enExample) |
Families Citing this family (66)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2004233826B2 (en) * | 2003-04-24 | 2009-08-13 | Merck Sharp & Dohme Corp. | Inhibitors of Akt activity |
| EP1631548B1 (en) * | 2003-04-24 | 2009-10-28 | Merck & Co., Inc. | Inhibitors of akt activity |
| ATE512957T1 (de) | 2003-04-24 | 2011-07-15 | Merck Sharp & Dohme | Hemmer der akt aktivität |
| JP2006524254A (ja) * | 2003-04-24 | 2006-10-26 | 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 |
| CN1942470A (zh) * | 2004-04-09 | 2007-04-04 | 默克公司 | Akt活性抑制剂 |
| ATE499364T1 (de) * | 2004-04-09 | 2011-03-15 | Merck Sharp & Dohme | Hemmer der akt aktivität |
| CA2576172A1 (en) * | 2004-08-23 | 2006-04-06 | Merck & Co., Inc. | Inhibitors of akt activity |
| CN101098872B (zh) | 2004-11-22 | 2012-09-05 | 沃泰克斯药物股份有限公司 | 可用作蛋白激酶抑制剂的吡咯并吡嗪和吡唑并吡嗪 |
| US8362075B2 (en) | 2005-05-17 | 2013-01-29 | Merck Sharp & Dohme Corp. | Cyclohexyl sulphones for treatment of cancer |
| AU2006258124B8 (en) | 2005-06-10 | 2010-01-07 | Merck Sharp & Dohme Corp. | Inhibitors of Akt activity |
| US20090062302A1 (en) | 2006-01-24 | 2009-03-05 | Buser-Doepner Carolyn A | Jak2 Tyrosine Kinase Inhibition |
| US8063050B2 (en) | 2006-07-06 | 2011-11-22 | Array Biopharma Inc. | Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| ATE493418T1 (de) * | 2006-07-06 | 2011-01-15 | Array Biopharma Inc | Dihydrofuropyrimidine als akt- proteinkinaseinhibitoren |
| ES2372955T3 (es) | 2006-07-06 | 2012-01-30 | Array Biopharma, Inc. | Ciclopenta[d]pirimidinas como inhibidores de la proteína cinasa akt. |
| JP5231411B2 (ja) * | 2006-07-06 | 2013-07-10 | アレイ バイオファーマ、インコーポレイテッド | Ａｋｔプロテインキナーゼ阻害剤としてのジヒドロチエノピリミジン |
| 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 |
| AR064010A1 (es) * | 2006-12-06 | 2009-03-04 | Merck & Co Inc | Inhibidores de la actividad de la akt |
| 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 |
| NZ582692A (en) | 2007-07-05 | 2012-05-25 | 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 |
| US8377937B2 (en) | 2007-07-05 | 2013-02-19 | Array Biopharma Inc. | Pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| WO2009089459A1 (en) | 2008-01-09 | 2009-07-16 | Array Biopharma Inc. | Hydroxylated pyrimidyl cyclopentanes as akt protein kinase inhibitors |
| CA2711692A1 (en) | 2008-01-09 | 2009-07-16 | Array Biopharma Inc. | Hydroxylated pyrimidyl cyclopentane as akt protein kinase inhibitor |
| US20100048912A1 (en) | 2008-03-14 | 2010-02-25 | Angela Brodie | Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens, In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity |
| CA2726317A1 (en) * | 2008-06-03 | 2009-12-10 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| AU2009255329A1 (en) * | 2008-06-03 | 2009-12-10 | Msd K.K. | Inhibitors of Akt activity |
| EP2393827B1 (en) | 2009-02-05 | 2015-10-07 | Tokai Pharmaceuticals, Inc. | Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens |
| KR20110114663A (ko) * | 2009-02-13 | 2011-10-19 | 바이엘 파마 악티엔게젤샤프트 | 융합된 피리미딘 |
| 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 |
| JP5099731B1 (ja) | 2009-10-14 | 2012-12-19 | メルク・シャープ・アンド・ドーム・コーポレーション | ｐ５３活性を増大する置換ピペリジン及びその使用 |
| EP2550272A1 (en) * | 2010-01-27 | 2013-01-30 | Vertex Pharmaceuticals Incorporated | Pyrazolopyrazine kinase inhibitors |
| EP2584903B1 (en) | 2010-06-24 | 2018-10-24 | Merck Sharp & Dohme Corp. | Novel heterocyclic compounds as erk inhibitors |
| CN103384670B (zh) * | 2010-07-28 | 2016-05-25 | 拜耳知识产权有限责任公司 | 取代的咪唑并[1,2-b]哒嗪 |
| CN107090456B (zh) | 2010-08-02 | 2022-01-18 | 瑟纳治疗公司 | 使用短干扰核酸的RNA干扰介导的联蛋白（钙粘蛋白关联蛋白质），β1基因表达的抑制 |
| LT2606134T (lt) | 2010-08-17 | 2019-07-25 | Sirna Therapeutics, Inc. | Hepatito b viruso (hbv) geno raiškos slopinimas, tarpininkaujant rnr interferencijai naudojant mažą interferuojančią nukleorūgštį (sina) |
| WO2012030685A2 (en) | 2010-09-01 | 2012-03-08 | Schering Corporation | Indazole derivatives useful as erk inhibitors |
| ES2663009T3 (es) | 2010-10-29 | 2018-04-10 | Sirna Therapeutics, Inc. | Inhibición de la expresión génica mediada por interferencia por ARN utilizando ácidos nucleicos de interferencia cortos (ANic) |
| US9351965B2 (en) | 2010-12-21 | 2016-05-31 | Merck Sharp & Dohme Corp. | Indazole derivatives useful as ERK inhibitors |
| CA2831932A1 (en) | 2011-04-01 | 2012-10-04 | Genentech, Inc. | Combinations of akt and mek inhibitor compounds, and methods of use |
| RS56759B2 (sr) | 2011-04-01 | 2024-10-31 | Genentech Inc | Kombinacija akt inhibitor jedinjenja i abiraterona za upotrebu pri terapeutskim tretiranjima |
| EP2770987B1 (en) | 2011-10-27 | 2018-04-04 | Merck Sharp & Dohme Corp. | Novel compounds that are erk inhibitors |
| US9408885B2 (en) | 2011-12-01 | 2016-08-09 | Vib Vzw | Combinations of therapeutic agents for treating melanoma |
| EP3358013B1 (en) | 2012-05-02 | 2020-06-24 | Sirna Therapeutics, Inc. | Short interfering nucleic acid (sina) compositions |
| US9233979B2 (en) | 2012-09-28 | 2016-01-12 | Merck Sharp & Dohme Corp. | Compounds that are ERK inhibitors |
| RU2660349C2 (ru) | 2012-11-28 | 2018-07-05 | Мерк Шарп И Доум Корп. | Композиции и способы для лечения злокачественной опухоли |
| BR112015013611A2 (pt) | 2012-12-20 | 2017-11-14 | Merck Sharp & Dohme | composto, e, composição farmacêutica |
| KR101470115B1 (ko) * | 2013-01-09 | 2014-12-05 | 동국대학교 산학협력단 | 2-(페닐에티닐)티에노[3,4-b]피라진 유도체 및 이를 포함하는 암의 예방 또는 치료용 약학적 조성물 |
| WO2014120748A1 (en) | 2013-01-30 | 2014-08-07 | Merck Sharp & Dohme Corp. | 2,6,7,8 substituted purines as hdm2 inhibitors |
| RU2015137617A (ru) | 2013-03-14 | 2017-04-18 | Юниверсити Оф Мэриленд, Балтимор Офис Оф Текнолоджи Трансфер | Агенты, подавляющие андрогенные рецепторы, и их применение |
| KR20160058774A (ko) | 2013-08-12 | 2016-05-25 | 토카이 파마슈티컬, 아이엔씨. | 안드로겐-표적 치료제를 이용하는 종양 질환 치료를 위한 바이오마커 |
| WO2015034925A1 (en) | 2013-09-03 | 2015-03-12 | Moderna Therapeutics, Inc. | Circular polynucleotides |
| JOP20190055A1 (ar) | 2016-09-26 | 2019-03-24 | Merck Sharp & Dohme | أجسام مضادة ضد cd27 |
| WO2018071283A1 (en) | 2016-10-12 | 2018-04-19 | Merck Sharp & Dohme Corp. | Kdm5 inhibitors |
| CN118267470A (zh) | 2017-04-13 | 2024-07-02 | 赛罗帕私人有限公司 | 抗SIRPα抗体 |
| WO2019094312A1 (en) | 2017-11-08 | 2019-05-16 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| US10947234B2 (en) | 2017-11-08 | 2021-03-16 | Merck Sharp & Dohme Corp. | PRMT5 inhibitors |
| WO2019148412A1 (en) | 2018-02-01 | 2019-08-08 | Merck Sharp & Dohme Corp. | Anti-pd-1/lag3 bispecific antibodies |
| EP3833668B1 (en) | 2018-08-07 | 2025-03-19 | Merck Sharp & Dohme LLC | Prmt5 inhibitors |
| MA53287A (fr) | 2018-08-07 | 2022-05-11 | Merck Sharp & Dohme | Inhibiteurs de prmt5 |
| WO2020033284A1 (en) | 2018-08-07 | 2020-02-13 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| WO2021118924A2 (en) | 2019-12-12 | 2021-06-17 | Ting Therapeutics Llc | Compositions and methods for the prevention and treatment of hearing loss |
| US12441730B2 (en) | 2019-12-17 | 2025-10-14 | Merck Sharp & Dohme Llc | PRMT5 inhibitors |
| WO2021126731A1 (en) | 2019-12-17 | 2021-06-24 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| US20230108114A1 (en) | 2019-12-17 | 2023-04-06 | Merck Sharp & Dohme Llc | Prmt5 inhibitors |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3431262A (en) * | 1968-03-26 | 1969-03-04 | American Home Prod | Pyrazolo quinoxalines |
| JPS5416497A (en) * | 1977-07-08 | 1979-02-07 | Nippon Soda Co Ltd | Aminooxopyrrolopyrazine compounds and their preparation |
| TW251284B (enExample) | 1992-11-02 | 1995-07-11 | Pfizer | |
| US5474995A (en) | 1993-06-24 | 1995-12-12 | Merck Frosst Canada, Inc. | Phenyl heterocycles as cox-2 inhibitors |
| WO1996023769A2 (en) | 1995-02-02 | 1996-08-08 | Smithkline Beecham Plc | Heterocyclic compounds possessing 5ht2c receptor antagonist activity |
| NZ301265A (en) | 1995-02-02 | 1998-12-23 | Smithkline Beecham Plc | Indole derivatives as 5ht receptor antagonists, preparation and pharmaceutical compositions thereof |
| US20020132326A1 (en) | 1995-12-15 | 2002-09-19 | Hemmings Brian A. | Process for activating a kinase |
| US20020127214A1 (en) | 1995-11-16 | 2002-09-12 | Hemmings Brian Arthur | RAC-protein kinase as therapeutic agent or in diagnostics |
| PT862622E (pt) | 1995-11-16 | 2005-01-31 | Novartis Ag | Metodo de rastreio para compostos que interagem com proteina cinase rac |
| GB9525702D0 (en) | 1995-12-15 | 1996-02-14 | Ciba Geigy Ag | Process for activating a kinase |
| EP0868195A2 (en) | 1995-12-20 | 1998-10-07 | Medical Research Council | Control of protein synthesis, and screening method for agents |
| DE69717627T2 (de) | 1996-06-27 | 2003-09-18 | Janssen Pharmaceutica N.V., Beerse | N-4-(heteroarylmethyl)phenyl-heteroarylaminderivate |
| US6060491A (en) | 1997-06-19 | 2000-05-09 | Dupont Pharmaceuticals | 6-membered aromatics as factor Xa inhibitors |
| AU8689298A (en) | 1997-08-05 | 1999-03-01 | Sugen, Inc. | Tricyclic quinoxaline derivatives as protein tyrosine kinase inhibitors |
| AU1918299A (en) | 1998-02-23 | 1999-09-06 | Warner-Lambert Company | Substituted quinoxaline derivatives as interleukin-8 receptor antagonists |
| GB0005642D0 (en) | 2000-03-10 | 2000-05-03 | Astrazeneca Uk Ltd | Chemical compounds |
| IL136458A0 (en) | 2000-05-30 | 2001-06-14 | Peptor Ltd | Protein kinase inhibitors |
| DE10058663A1 (de) * | 2000-11-25 | 2002-05-29 | Merck Patent Gmbh | Verwendung von Thienopyrimidinen |
| JP2002284684A (ja) * | 2001-01-16 | 2002-10-03 | Japan Science & Technology Corp | チエノイソキノロン含有抗菌抗ウィルス剤および抗腫瘍剤 |
| JP2002220338A (ja) * | 2001-01-26 | 2002-08-09 | Banyu Pharmaceut Co Ltd | ビアリールウレア化合物又はその塩を有効成分として含有するＣｄｋ４及び／又はＣｄｋ６阻害剤 |
| AU2002251266A1 (en) | 2001-04-10 | 2002-10-28 | Merck Sharp And Dohme Limited | Inhibitors of akt activity |
| EP1379251B1 (en) * | 2001-04-10 | 2008-07-09 | Merck & Co., Inc. | Inhibitors of akt activity |
| US6958334B2 (en) | 2001-04-10 | 2005-10-25 | Merck & Co., Inc. | Inhibitors of Akt activity |
| JP2004527531A (ja) | 2001-04-10 | 2004-09-09 | メルク エンド カムパニー インコーポレーテッド | 癌を治療する方法 |
| US20040116433A1 (en) | 2002-04-08 | 2004-06-17 | Owens Andrew Pate | Inhibitors of akt activity |
| JP4451136B2 (ja) | 2002-04-08 | 2010-04-14 | メルク エンド カムパニー インコーポレーテッド | Ａｋｔ活性阻害薬 |
| AU2003223467B2 (en) | 2002-04-08 | 2007-10-04 | Merck Sharp & Dohme Corp. | Inhibitors of Akt activity |
| US20060142178A1 (en) | 2002-04-08 | 2006-06-29 | Barnett Stanley F | Method of treating cancer |
| CA2481241C (en) | 2002-04-08 | 2010-07-27 | Merck & Co., Inc. | Fused quinoxaline derivatives as inhibitors of akt activity |
| CA2481229C (en) | 2002-04-08 | 2010-09-21 | Merck & Co., Inc. | Substituted pyrazine inhibitors of akt |
| US20040102360A1 (en) | 2002-10-30 | 2004-05-27 | Barnett Stanley F. | Combination therapy |
-
2003
- 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 US US10/530,252 patent/US7399764B2/en not_active Expired - Fee Related
- 2003-10-24 AU AU2003284981A patent/AU2003284981B2/en not_active Ceased
- 2003-10-24 JP JP2004550130A patent/JP2006507299A/ja active Pending
- 2003-10-24 AT AT03779301T patent/ATE503483T1/de not_active IP Right Cessation
- 2003-10-24 WO PCT/US2003/034007 patent/WO2004041162A2/en not_active Ceased
- 2003-10-24 EP EP03779301A patent/EP1558586B1/en not_active Expired - Lifetime
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2006507299A5 (enExample) | ||
| CA2501365A1 (en) | Inhibitors of akt activity | |
| CA2481241A1 (en) | Fused quinoxaline derivatives as inhibitors of akt activity | |
| JP2006524254A5 (enExample) | ||
| EP1404672B1 (en) | Tyrosine kinase inhibitors | |
| US6586424B2 (en) | Tyrosine kinase inhibitors | |
| US6306874B1 (en) | Tyrosine kinase inhibitors | |
| JP5210866B2 (ja) | キナーゼ阻害剤としての置換ベンゾイミダゾール | |
| US6794393B1 (en) | Tyrosine kinase inhibitors | |
| RU2437882C2 (ru) | Производные имидазолидинона | |
| US20040192725A1 (en) | Tyrosine kinase inhibitors | |
| AU2002346053A1 (en) | Tyrosine kinase inhibitors | |
| CA2481229A1 (en) | Substituted pyrazine inhibitors of akt | |
| JP2005504100A5 (enExample) | ||
| JP2006206609A5 (enExample) | ||
| RU2006100190A (ru) | Производные хинолиламида в качестве антагонистов ccr-5 | |
| WO2003015778A1 (en) | Tyrosine kinase inhibitors | |
| RU2003115612A (ru) | Производные амидоалкилпиперидинов и амидоалкилпиперазинов, пригодные для лечения нарушений нервной системы | |
| JP2008517042A5 (enExample) | ||
| US7186723B2 (en) | Tyrosine kinase inhibitors | |
| JP2014521620A5 (enExample) | ||
| JP2007532523A5 (enExample) | ||
| RU2002110111A (ru) | Замещенные пирролы в качестве антипролиферативных средств для лечения рака | |
| JPWO2023091746A5 (enExample) | ||
| RU2021113492A (ru) | Новые аминопиримидонилпиперидинильные производные, способ их получения и содержащие их фармацевтические композиции |