JP2006524254A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2006524254A5 JP2006524254A5 JP2006513159A JP2006513159A JP2006524254A5 JP 2006524254 A5 JP2006524254 A5 JP 2006524254A5 JP 2006513159 A JP2006513159 A JP 2006513159A JP 2006513159 A JP2006513159 A JP 2006513159A JP 2006524254 A5 JP2006524254 A5 JP 2006524254A5
- Authority
- JP
- Japan
- Prior art keywords
- phenyl
- methyl
- benzimidazol
- piperidin
- pyridin
- 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.)
- Ceased
Links
- 125000000623 heterocyclic group Chemical group 0.000 claims 21
- 125000003118 aryl group Chemical group 0.000 claims 20
- 125000000217 alkyl group Chemical group 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 14
- 241000124008 Mammalia Species 0.000 claims 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- 238000000034 method Methods 0.000 claims 9
- 125000001424 substituent group Chemical group 0.000 claims 8
- 125000000304 alkynyl group Chemical group 0.000 claims 7
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 6
- -1 4-{[4- (2-methyl-1H-benzimidazol-1-yl) piperidin-1-yl] methyl} phenyl Chemical group 0.000 claims 6
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 6
- 125000003342 alkenyl group Chemical group 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 125000005865 C2-C10alkynyl group Chemical group 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 201000011510 cancer Diseases 0.000 claims 5
- 125000005843 halogen group Chemical group 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 230000033115 angiogenesis Effects 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 230000003211 malignant effect Effects 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- BFQMNZSGJRJNHK-UHFFFAOYSA-N 1-ethyl-3-[1-methyl-6-[4-[[4-(2-oxo-3h-benzimidazol-1-yl)piperidin-1-yl]methyl]phenyl]-5-phenylpyrazolo[3,4-b]pyridin-3-yl]urea Chemical compound C1=C2C(NC(=O)NCC)=NN(C)C2=NC(C=2C=CC(CN3CCC(CC3)N3C(NC4=CC=CC=C43)=O)=CC=2)=C1C1=CC=CC=C1 BFQMNZSGJRJNHK-UHFFFAOYSA-N 0.000 claims 3
- WTOLMDZZQMSFOI-UHFFFAOYSA-N 3-[1-[[4-(3-amino-5-phenyl-2h-pyrazolo[3,4-b]pyridin-6-yl)phenyl]methyl]piperidin-4-yl]-1h-benzimidazol-2-one Chemical compound C1=C2C(N)=NNC2=NC(C=2C=CC(CN3CCC(CC3)N3C(NC4=CC=CC=C43)=O)=CC=2)=C1C1=CC=CC=C1 WTOLMDZZQMSFOI-UHFFFAOYSA-N 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- QEHLNDRCMQCNLS-UHFFFAOYSA-N methyl 3-amino-6-[4-[[4-(6-fluoro-1h-benzimidazol-2-yl)piperidin-1-yl]methyl]phenyl]-5-phenylfuro[2,3-b]pyridine-2-carboxylate Chemical compound C1=C2C(N)=C(C(=O)OC)OC2=NC(C=2C=CC(CN3CCC(CC3)C=3NC4=CC(F)=CC=C4N=3)=CC=2)=C1C1=CC=CC=C1 QEHLNDRCMQCNLS-UHFFFAOYSA-N 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- CFZCFLONWSUZFP-UHFFFAOYSA-N 3-[1-[[4-(3-amino-1-methyl-5-phenylpyrazolo[3,4-b]pyridin-6-yl)phenyl]methyl]piperidin-4-yl]-1h-benzimidazol-2-one Chemical compound C=1C=C(CN2CCC(CC2)N2C(NC3=CC=CC=C32)=O)C=CC=1C=1N=C2N(C)N=C(N)C2=CC=1C1=CC=CC=C1 CFZCFLONWSUZFP-UHFFFAOYSA-N 0.000 claims 2
- YRJDTLJIZXAPEA-UHFFFAOYSA-N 3-[1-[[4-[3-amino-1-(2-hydroxyethyl)-5-phenylpyrazolo[3,4-b]pyridin-6-yl]phenyl]methyl]piperidin-4-yl]-1h-benzimidazol-2-one Chemical compound C1=C2C(N)=NN(CCO)C2=NC(C=2C=CC(CN3CCC(CC3)N3C(NC4=CC=CC=C43)=O)=CC=2)=C1C1=CC=CC=C1 YRJDTLJIZXAPEA-UHFFFAOYSA-N 0.000 claims 2
- MHSHJMBJLQWRBY-UHFFFAOYSA-N 3-[1-[[4-[3-amino-1-(2-morpholin-4-ylethyl)-5-phenylpyrazolo[3,4-b]pyridin-6-yl]phenyl]methyl]piperidin-4-yl]-1h-benzimidazol-2-one Chemical compound C12=NC(C=3C=CC(CN4CCC(CC4)N4C(NC5=CC=CC=C54)=O)=CC=3)=C(C=3C=CC=CC=3)C=C2C(N)=NN1CCN1CCOCC1 MHSHJMBJLQWRBY-UHFFFAOYSA-N 0.000 claims 2
- YNXIBVROBVAXTR-UHFFFAOYSA-N 3-[1-[[4-[3-amino-1-[2-(1h-imidazol-5-yl)ethyl]-5-phenylpyrazolo[3,4-b]pyridin-6-yl]phenyl]methyl]piperidin-4-yl]-1h-benzimidazol-2-one Chemical compound C12=NC(C=3C=CC(CN4CCC(CC4)N4C(NC5=CC=CC=C54)=O)=CC=3)=C(C=3C=CC=CC=3)C=C2C(N)=NN1CCC1=CNC=N1 YNXIBVROBVAXTR-UHFFFAOYSA-N 0.000 claims 2
- GEAIYSCJTKMVMR-UHFFFAOYSA-N 5-[4-[[4-(2-methylbenzimidazol-1-yl)piperidin-1-yl]methyl]phenyl]-6-phenyl-1h-imidazo[4,5-b]pyridine Chemical compound CC1=NC2=CC=CC=C2N1C(CC1)CCN1CC(C=C1)=CC=C1C1=NC=2N=CNC=2C=C1C1=CC=CC=C1 GEAIYSCJTKMVMR-UHFFFAOYSA-N 0.000 claims 2
- ULXDTDVFKRMXTL-UHFFFAOYSA-N 5-[4-[[4-(2-methylbenzimidazol-1-yl)piperidin-1-yl]methyl]phenyl]-6-phenyl-2h-triazolo[4,5-b]pyridine Chemical compound CC1=NC2=CC=CC=C2N1C(CC1)CCN1CC(C=C1)=CC=C1C1=NC=2N=NNC=2C=C1C1=CC=CC=C1 ULXDTDVFKRMXTL-UHFFFAOYSA-N 0.000 claims 2
- KHHTVAGKADOYOC-UHFFFAOYSA-N 9-[1-[[4-(3-amino-1-methyl-5-phenylpyrazolo[3,4-b]pyridin-6-yl)phenyl]methyl]piperidin-4-yl]purin-6-amine Chemical compound C=1C=C(CN2CCC(CC2)N2C3=NC=NC(N)=C3N=C2)C=CC=1C=1N=C2N(C)N=C(N)C2=CC=1C1=CC=CC=C1 KHHTVAGKADOYOC-UHFFFAOYSA-N 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 206010020751 Hypersensitivity Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 102000001708 Protein Isoforms Human genes 0.000 claims 2
- 108010029485 Protein Isoforms Proteins 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 208000026935 allergic disease Diseases 0.000 claims 2
- 230000007815 allergy Effects 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 201000008980 hyperinsulinism Diseases 0.000 claims 2
- 230000003463 hyperproliferative effect Effects 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- VKJKNSCQTXORQP-UHFFFAOYSA-N n-[1-methyl-6-[4-[[4-(2-oxo-3h-benzimidazol-1-yl)piperidin-1-yl]methyl]phenyl]-5-phenylpyrazolo[3,4-b]pyridin-3-yl]acetamide Chemical compound C1=C2C(NC(=O)C)=NN(C)C2=NC(C=2C=CC(CN3CCC(CC3)N3C(NC4=CC=CC=C43)=O)=CC=2)=C1C1=CC=CC=C1 VKJKNSCQTXORQP-UHFFFAOYSA-N 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- UBQKCCHYAOITMY-UHFFFAOYSA-N pyridin-2-ol Chemical compound OC1=CC=CC=N1 UBQKCCHYAOITMY-UHFFFAOYSA-N 0.000 claims 2
- 208000037803 restenosis Diseases 0.000 claims 2
- 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 1
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 1
- 125000006664 (C1-C3) perfluoroalkyl group Chemical group 0.000 claims 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 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
- 229940122440 HIV protease inhibitor Drugs 0.000 claims 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 1
- 229940122054 Peroxisome proliferator-activated receptor delta agonist Drugs 0.000 claims 1
- 229940080774 Peroxisome proliferator-activated receptor gamma agonist Drugs 0.000 claims 1
- 229940123468 Transferase inhibitor Drugs 0.000 claims 1
- 125000005275 alkylenearyl group Chemical group 0.000 claims 1
- 239000004037 angiogenesis inhibitor Substances 0.000 claims 1
- 229940121369 angiogenesis inhibitor Drugs 0.000 claims 1
- 230000001028 anti-proliverative effect Effects 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
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 230000012820 cell cycle checkpoint Effects 0.000 claims 1
- 230000004663 cell proliferation Effects 0.000 claims 1
- 230000001672 cytoproliferative effect Effects 0.000 claims 1
- 239000002254 cytotoxic agent Substances 0.000 claims 1
- 229940127089 cytotoxic agent Drugs 0.000 claims 1
- 231100000599 cytotoxic agent Toxicity 0.000 claims 1
- 239000002834 estrogen receptor modulator Substances 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 239000004030 hiv protease inhibitor Substances 0.000 claims 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 125000005010 perfluoroalkyl group Chemical group 0.000 claims 1
- 125000001844 prenyl group Chemical group [H]C([*])([H])C([H])=C(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 238000001959 radiotherapy Methods 0.000 claims 1
- 229940075993 receptor modulator Drugs 0.000 claims 1
- 102000027483 retinoid hormone receptors Human genes 0.000 claims 1
- 108091008679 retinoid hormone receptors Proteins 0.000 claims 1
- 239000003419 rna directed dna polymerase inhibitor Substances 0.000 claims 1
- 239000000849 selective androgen receptor modulator Substances 0.000 claims 1
- 230000007755 survival signaling Effects 0.000 claims 1
- 239000003558 transferase inhibitor Substances 0.000 claims 1
- 0 CC(*1)*(*)c2c1nc(-c1ccc(CN3CCC(*)CC3)cc1)c(-c1ccccc1)c2 Chemical compound CC(*1)*(*)c2c1nc(-c1ccc(CN3CCC(*)CC3)cc1)c(-c1ccccc1)c2 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US46512303P | 2003-04-24 | 2003-04-24 | |
| PCT/US2004/012187 WO2004096130A2 (en) | 2003-04-24 | 2004-04-20 | Inhibitors of akt activity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2006524254A JP2006524254A (ja) | 2006-10-26 |
| JP2006524254A5 true JP2006524254A5 (enExample) | 2007-04-05 |
Family
ID=33418186
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006513159A Ceased JP2006524254A (ja) | 2003-04-24 | 2004-04-20 | Ａｋｔ活性の阻害剤 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US7638530B2 (enExample) |
| EP (1) | EP1620095A4 (enExample) |
| JP (1) | JP2006524254A (enExample) |
| CN (1) | CN1809351A (enExample) |
| AU (1) | AU2004233827B2 (enExample) |
| CA (1) | CA2522430A1 (enExample) |
| WO (1) | WO2004096130A2 (enExample) |
Families Citing this family (81)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA81453C2 (en) | 2003-02-27 | 2008-01-10 | Pyrazolopyridine derivates | |
| EA200600372A1 (ru) * | 2003-09-05 | 2006-08-25 | Ньюроджин Корпорейшн | Конденсированные с гетероарилом пиридины, пиразины и пиримидины в качестве лигандов рецептора кортикотропин-рилизинг-фактора (crf 1) |
| US7572914B2 (en) | 2003-12-19 | 2009-08-11 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| CA2561311A1 (en) * | 2004-04-09 | 2005-10-27 | Merck & Co., Inc. | Inhibitors of akt activity |
| CN1942470A (zh) * | 2004-04-09 | 2007-04-04 | 默克公司 | Akt活性抑制剂 |
| AR050188A1 (es) * | 2004-08-03 | 2006-10-04 | Uriach Y Compania S A J | Compuestos heterociclicos condensados utiles en terapia como inhibidores de quinasas p38 y composiciones farmaceuticas que los contienen |
| WO2006023931A2 (en) | 2004-08-18 | 2006-03-02 | Takeda San Diego, Inc. | Kinase inhibitors |
| US7544677B2 (en) | 2004-08-23 | 2009-06-09 | Merck & Co., Inc. | Inhibitors of Akt activity |
| EP1812439B2 (en) | 2004-10-15 | 2017-12-06 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| AR051596A1 (es) * | 2004-10-26 | 2007-01-24 | Irm Llc | Compuestos heterociclicos condensados nitrogenados como inhibidores de la actividad del receptor canabinoide 1; composiciones farmaceuticas que los contienen y su empleo en la preparacion de medicamentos para el tratamiento de trastornos alimentarios |
| PE20061119A1 (es) | 2005-01-19 | 2006-11-27 | Aventis Pharma Sa | PIRAZOLO PIRIDINAS SUSTITUIDAS COMO INHIBIDORES DE CINASAS FAK, KDR Y Tie |
| AU2006216998B2 (en) * | 2005-02-14 | 2010-12-23 | Merck Sharp & Dohme Corp. | Inhibitors of Akt activity |
| ATE550019T1 (de) | 2005-05-17 | 2012-04-15 | Merck Sharp & Dohme | Cis-4-ä(4-chlorophenyl)sulfonylü-4-(2,5- difluorophenyl)cyclohexanepropansäure zur behandlug von krebs |
| WO2006135627A2 (en) * | 2005-06-10 | 2006-12-21 | Merck & Co., Inc. | Inhibitors of akt activity |
| FR2889526B1 (fr) | 2005-08-04 | 2012-02-17 | Aventis Pharma Sa | 7-aza-indazoles substitues, compositions les contenant, procede de fabrication et utilisation |
| US8119655B2 (en) | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| AU2006315436A1 (en) | 2005-11-15 | 2007-05-24 | Vertex Pharmaceuticals Incorporated | Azaindazoles useful as inhibitors of kinases |
| WO2007087246A2 (en) | 2006-01-24 | 2007-08-02 | Merck & Co., Inc. | Jak2 tyrosine kinase inhibition |
| RU2481336C2 (ru) | 2006-07-06 | 2013-05-10 | Эррэй Биофарма Инк. | Циклопента(d)пиримидины в качестве ингибиторов протеинкиназ акт |
| DE602007011628D1 (de) | 2006-07-06 | 2011-02-10 | Array Biopharma Inc | Dihydrofuropyrimidine als akt-proteinkinaseinhibitoren |
| US8063050B2 (en) | 2006-07-06 | 2011-11-22 | Array Biopharma Inc. | Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| WO2008006039A1 (en) | 2006-07-06 | 2008-01-10 | Array Biopharma Inc. | Dihydrothieno pyrimidines as akt protein kinase inhibitors |
| JP2010505962A (ja) | 2006-10-09 | 2010-02-25 | 武田薬品工業株式会社 | キナーゼ阻害剤 |
| 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 |
| EP1958947A1 (en) | 2007-02-15 | 2008-08-20 | Ranbaxy Laboratories Limited | Inhibitors of phosphodiesterase type 4 |
| US8642067B2 (en) | 2007-04-02 | 2014-02-04 | Allergen, Inc. | Methods and compositions for intraocular administration to treat ocular conditions |
| US9409886B2 (en) | 2007-07-05 | 2016-08-09 | Array Biopharma Inc. | Pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| CA2692502C (en) | 2007-07-05 | 2016-03-01 | Array Biopharma Inc. | Pyrimidyl cyclopentanes as akt protein kinase inhibitors |
| US8846683B2 (en) | 2007-07-05 | 2014-09-30 | Array Biopharma, Inc. | Pyrimidyl cyclopentanes as Akt protein kinase inhibitors |
| MX2009014013A (es) | 2007-07-05 | 2010-01-28 | Array Biopharma Inc | Pirimidil ciclopentanos como inhibidores de la proteina cinasa akt. |
| US8314131B2 (en) | 2007-09-21 | 2012-11-20 | Amgen Inc. | Triazole fused heteroaryl compounds and methods of use thereof |
| US8835434B2 (en) | 2008-01-09 | 2014-09-16 | Array Biopharma, Inc. | Hydroxylated pyrimidyl cyclopentanes as akt protein kinase inhibitors |
| US8853216B2 (en) | 2008-01-09 | 2014-10-07 | Array Biopharma, Inc. | Hydroxylated pyrimidyl cyclopentane as AKT protein kinase inhibitor |
| US20100048524A1 (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 |
| JP2011522047A (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 |
| US8207169B2 (en) * | 2008-06-03 | 2012-06-26 | Msd K.K. | Substituted [1,2,4]triazolo[4′,3′:1,6]pyrido[2,3-b]pyrazines of the formula D |
| NZ590784A (en) * | 2008-07-23 | 2012-12-21 | Vertex Pharma | Pyrazolopyridine kinase inhibitors |
| EP2393827B1 (en) | 2009-02-05 | 2015-10-07 | Tokai Pharmaceuticals, Inc. | Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens |
| US8957064B2 (en) * | 2009-02-13 | 2015-02-17 | Bayer Intellectual Property Gmbh | Fused pyrimidines |
| WO2010104705A1 (en) | 2009-03-12 | 2010-09-16 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| EP2413932A4 (en) | 2009-04-01 | 2012-09-19 | Merck Sharp & Dohme | HAMMER OF ACT ACTIVITY |
| WO2011019780A1 (en) | 2009-08-11 | 2011-02-17 | Bristol-Myers Squibb Company | Azaindazoles as btk kinase modulators and use thereof |
| CA2777043C (en) | 2009-10-14 | 2015-12-15 | Schering Corporation | Substituted piperidines that increase p53 activity and the uses thereof |
| GB0919380D0 (en) * | 2009-11-04 | 2009-12-23 | Almac Discovery Ltd | Pharmaceutical compouds |
| EP2584903B1 (en) | 2010-06-24 | 2018-10-24 | Merck Sharp & Dohme Corp. | Novel heterocyclic compounds as erk inhibitors |
| CN103068980B (zh) | 2010-08-02 | 2017-04-05 | 瑟纳治疗公司 | 使用短干扰核酸（siNA）的RNA干扰介导的联蛋白（钙粘蛋白关联蛋白质），β1（CTNNB1）基因表达的抑制 |
| RU2745848C2 (ru) | 2010-08-17 | 2021-04-01 | Сирна Терапьютикс, Инк. | ОПОСРЕДУЕМОЕ РНК-ИНТЕРФЕРЕНЦИЕЙ ИНГИБИРОВАНИЕ ЭКСПРЕССИИ ГЕНОВ ВИРУСА ГЕПАТИТА B (HBV) С ПРИМЕНЕНИЕМ МАЛОЙ ИНТЕРФЕРИРУЮЩЕЙ НУКЛЕИНОВОЙ КИСЛОТЫ (миНК) |
| EP2613782B1 (en) | 2010-09-01 | 2016-11-02 | Merck Sharp & Dohme Corp. | Indazole derivatives useful as erk inhibitors |
| WO2012058210A1 (en) | 2010-10-29 | 2012-05-03 | Merck Sharp & Dohme Corp. | RNA INTERFERENCE MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACIDS (siNA) |
| WO2012087772A1 (en) | 2010-12-21 | 2012-06-28 | Schering Corporation | Indazole derivatives useful as erk inhibitors |
| FI2694072T4 (fi) | 2011-04-01 | 2024-09-30 | Genentech Inc | Akt-inhibiittoriyhdisteen ja abirateronin yhdistelmä käytettäväksi terapeuttisissa hoidoissa |
| TR201815685T4 (tr) | 2011-04-01 | 2018-11-21 | Genentech Inc | Kanser tedavisi için akt ve mek inhibe edici bileşiklerin kombinasyonları. |
| 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 |
| EP3919620A1 (en) | 2012-05-02 | 2021-12-08 | Sirna Therapeutics, Inc. | Short interfering nucleic acid (sina) compositions |
| CA2882950A1 (en) | 2012-09-28 | 2014-04-03 | Merck Sharp & Dohme Corp. | Novel compounds that are erk inhibitors |
| SMT201700595T1 (it) | 2012-11-28 | 2018-03-08 | Merck Sharp & Dohme | Composizioni e metodi per trattare il cancro |
| WO2014100065A1 (en) | 2012-12-20 | 2014-06-26 | Merck Sharp & Dohme Corp. | Substituted imidazopyridines as hdm2 inhibitors |
| WO2014120748A1 (en) | 2013-01-30 | 2014-08-07 | Merck Sharp & Dohme Corp. | 2,6,7,8 substituted purines as hdm2 inhibitors |
| CA2904170A1 (en) | 2013-03-14 | 2014-09-25 | University Of Maryland, Baltimore | Androgen receptor down-regulating agents and uses thereof |
| 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 |
| CN106061969B (zh) * | 2014-01-06 | 2019-10-29 | 阿尔戈么迪克斯有限公司 | Trpa1调节剂 |
| CA3029901A1 (en) * | 2016-07-06 | 2018-01-11 | Algomedix, Inc. | Trpa1 antagonists for treatment of dry eye, ocular pain and inflammation |
| JOP20190055A1 (ar) | 2016-09-26 | 2019-03-24 | Merck Sharp & Dohme | أجسام مضادة ضد cd27 |
| US10975084B2 (en) | 2016-10-12 | 2021-04-13 | Merck Sharp & Dohme Corp. | KDM5 inhibitors |
| JP7160833B2 (ja) | 2017-04-13 | 2022-10-25 | サイロパ ビー．ブイ． | 抗ｓｉｒｐアルファ抗体 |
| EP3706742B1 (en) | 2017-11-08 | 2023-03-15 | Merck Sharp & Dohme LLC | Prmt5 inhibitors |
| WO2019094312A1 (en) | 2017-11-08 | 2019-05-16 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| WO2019148412A1 (en) | 2018-02-01 | 2019-08-08 | Merck Sharp & Dohme Corp. | Anti-pd-1/lag3 bispecific antibodies |
| WO2020033282A1 (en) | 2018-08-07 | 2020-02-13 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| EP3833667B1 (en) | 2018-08-07 | 2024-03-13 | Merck Sharp & Dohme LLC | Prmt5 inhibitors |
| WO2020033285A1 (en) | 2018-08-07 | 2020-02-13 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| CA3108388A1 (en) | 2018-08-07 | 2020-02-13 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| CN114981298B (zh) | 2019-12-12 | 2024-08-20 | 听治疗有限责任公司 | 用于预防和治疗听力损失的组合物和方法 |
| ES3022307T3 (en) | 2019-12-17 | 2025-05-28 | Merck Sharp & Dohme Llc | Prmt5 inhibitors |
| ES3074517T3 (en) | 2019-12-17 | 2026-07-21 | Merck Sharp & Dohme Llc | 4-(3,4-dihydroisoquinolin-2(1h)-yl)-3-hydroxypiperidine derivatives as prmt5 inhibitors for the treatment of cancer and sickle cell disease |
| EP4076460B1 (en) | 2019-12-17 | 2026-01-21 | Merck Sharp & Dohme LLC | 1,4-dihydro-2h-spiro[isoquinoline-3,4'-piperidine derivatives as prmt5 inhibitors for the treatment of cancer |
| EP4076459B1 (en) | 2019-12-17 | 2026-04-29 | Merck Sharp & Dohme LLC | Prmt5 inhibitors |
| DE212025000115U1 (de) | 2024-07-30 | 2026-06-18 | Sairopa B.V. | Anti-SIRP Alpha-Antikörperformulierungen und ihre Verwendung |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW251284B (enExample) | 1992-11-02 | 1995-07-11 | Pfizer | |
| GB9420521D0 (en) | 1994-10-12 | 1994-11-30 | Smithkline Beecham Plc | Novel compounds |
| 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 |
| GB9517559D0 (en) | 1995-08-26 | 1995-10-25 | Smithkline Beecham Plc | Novel compounds |
| US20020127214A1 (en) * | 1995-11-16 | 2002-09-12 | Hemmings Brian Arthur | RAC-protein kinase as therapeutic agent or in diagnostics |
| JP2000502097A (ja) | 1995-12-20 | 2000-02-22 | メディカル、リサーチ、カウンシル | タンパク質合成の制御、および作用薬のスクリーニング法 |
| JP3404749B2 (ja) | 1996-06-27 | 2003-05-12 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | Ｎ―［４―（ヘテロアリールメチル）フェニル］―ヘテロアリールアミン |
| US6060491A (en) * | 1997-06-19 | 2000-05-09 | Dupont Pharmaceuticals | 6-membered aromatics as factor Xa inhibitors |
| HRP20000209A2 (en) * | 1997-10-20 | 2001-04-30 | Hoffmann La Roche | Bicyclic kinase inhibitors |
| 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 |
| AU2001290912A1 (en) * | 2000-09-15 | 2002-03-26 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| 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 |
| US6960584B2 (en) * | 2001-04-10 | 2005-11-01 | Merck & Co., Inc. | Inhibitors of Akt activity |
| WO2002083140A1 (en) * | 2001-04-10 | 2002-10-24 | Merck & Co., Inc. | Inhibitors of akt activity |
| US20040116433A1 (en) * | 2002-04-08 | 2004-06-17 | Owens Andrew Pate | Inhibitors of akt activity |
| JP4361276B2 (ja) | 2001-04-10 | 2009-11-11 | メルク エンド カムパニー インコーポレーテッド | Ａｋｔ活性の阻害物質 |
| WO2003086404A1 (en) * | 2002-04-08 | 2003-10-23 | Merck & Co., Inc. | Fused quinoxaline derivatives as inhibitors of akt activity |
| AU2003226301A1 (en) | 2002-04-08 | 2003-10-20 | Merck And Co., Inc. | Method of treating cancer |
| 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 |
| CA2480800C (en) | 2002-04-08 | 2008-09-23 | Mark T. Bilodeau | Inhibitors of akt activity |
| WO2003086279A2 (en) * | 2002-04-08 | 2003-10-23 | Merck & Co., Inc. | Inhibitors of akt activity |
| BR0314392A (pt) | 2002-09-16 | 2005-07-12 | Glaxo Group Ltd | Composto ou um sal do mesmo, composição farmacêutica, uso de um composto, método de tratamento e/ou profilaxia de uma doença inflamatória e/ou alérgica ou deficiência cognitiva em um mamìfero, e, combinação |
| US20040102360A1 (en) * | 2002-10-30 | 2004-05-27 | Barnett Stanley F. | Combination therapy |
| AU2003284981B2 (en) * | 2002-10-30 | 2009-05-28 | Merck Sharp & Dohme Corp. | Inhibitors of Akt activity |
-
2004
- 2004-04-20 AU AU2004233827A patent/AU2004233827B2/en not_active Ceased
- 2004-04-20 CA CA002522430A patent/CA2522430A1/en not_active Abandoned
- 2004-04-20 US US10/554,185 patent/US7638530B2/en not_active Expired - Fee Related
- 2004-04-20 WO PCT/US2004/012187 patent/WO2004096130A2/en not_active Ceased
- 2004-04-20 CN CNA2004800171014A patent/CN1809351A/zh active Pending
- 2004-04-20 JP JP2006513159A patent/JP2006524254A/ja not_active Ceased
- 2004-04-20 EP EP04760293A patent/EP1620095A4/en not_active Withdrawn
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| TWI248932B (en) | Respiratory syncytial virus replication inhibitors | |
| AU2013361127B2 (en) | Compounds and methods for kinase modulation, and indications therefor | |
| AU2017395023B2 (en) | Compounds and methods for CDK8 modulation and indications therefor | |
| CA2787823C (en) | Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same | |
| US10227357B2 (en) | Compounds and methods for kinase modulation, and indications therefor | |
| KR102066297B1 (ko) | 헤테로사이클릭 화합물 및 이의 유형 3 수용체 티로신 키나아제의 조절인자로서의 용도 | |
| RU2011108453A (ru) | Производные имидазопиридин-2-она | |
| US10406162B2 (en) | Substituted 2,3-dihydroimidazo[1,2-C]quinazoline-containing combinations | |
| JP2019512505A5 (enExample) | ||
| CA2481241A1 (en) | Fused quinoxaline derivatives as inhibitors of akt activity | |
| JP2012525335A5 (enExample) | ||
| IL187690A (en) | Derivatives 1, 2, 4 - Triazolo - 1, 6 - Naphthiridines as inhibitors of AKT activity for use in the preparation of drugs for the treatment of cancer | |
| RU2003106193A (ru) | Способ лечения аллергий с использованием замещенных пиразолов | |
| JP2006507299A5 (enExample) | ||
| CA2670362A1 (en) | Compounds modulating c-fms and/or c-kit activity and uses therefor | |
| CA2501365A1 (en) | Inhibitors of akt activity | |
| JP2013507425A5 (enExample) | ||
| SK287900B6 (sk) | Substituted azaindolexoacetic piperazine derivatives and pharmaceutical composition containing thereof | |
| RU2011114487A (ru) | Гетероциклические соединения как ингибиторы протеинкиназы | |
| JP7597709B2 (ja) | 置換インドールおよびインダゾール化合物 | |
| JP2008507539A5 (enExample) | ||
| RU2005138546A (ru) | 2-имидазобензотиазолы, как лиганды аденозинового рецептора | |
| JP2005508942A5 (enExample) | ||
| US11185549B2 (en) | Combination of a PI3K-inhibitor with an androgen receptor antagonist | |
| RU2007105558A (ru) | Новые производные 2, 6-диаминопиридин-3-она |