JP2010510216A5 - - Google Patents
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- JP2010510216A5 JP2010510216A5 JP2009537209A JP2009537209A JP2010510216A5 JP 2010510216 A5 JP2010510216 A5 JP 2010510216A5 JP 2009537209 A JP2009537209 A JP 2009537209A JP 2009537209 A JP2009537209 A JP 2009537209A JP 2010510216 A5 JP2010510216 A5 JP 2010510216A5
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- JP
- Japan
- Prior art keywords
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- groups
- composition
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- 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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- 150000001875 compounds Chemical class 0.000 claims description 74
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 32
- 229910052757 nitrogen Inorganic materials 0.000 claims description 28
- 125000001931 aliphatic group Chemical group 0.000 claims description 26
- 125000005842 heteroatom Chemical group 0.000 claims description 26
- 229910052760 oxygen Inorganic materials 0.000 claims description 26
- 239000000203 mixture Substances 0.000 claims description 24
- 229910052717 sulfur Inorganic materials 0.000 claims description 22
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 18
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 18
- 229910052799 carbon Inorganic materials 0.000 claims description 18
- 239000001301 oxygen Substances 0.000 claims description 18
- 239000011593 sulfur Substances 0.000 claims description 18
- 125000000217 alkyl group Chemical group 0.000 claims description 16
- 125000005843 halogen group Chemical group 0.000 claims description 16
- 125000003118 aryl group Chemical group 0.000 claims description 14
- 229920006395 saturated elastomer Polymers 0.000 claims description 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 13
- 238000000034 method Methods 0.000 claims description 12
- 206010028980 Neoplasm Diseases 0.000 claims description 10
- 201000011510 cancer Diseases 0.000 claims description 10
- 239000003795 chemical substances by application Substances 0.000 claims description 10
- 208000035475 disorder Diseases 0.000 claims description 9
- 102000001253 Protein Kinase Human genes 0.000 claims description 8
- 125000004432 carbon atom Chemical group C* 0.000 claims description 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 8
- 125000001072 heteroaryl group Chemical group 0.000 claims description 8
- 125000000623 heterocyclic group Chemical group 0.000 claims description 8
- 229910052739 hydrogen Inorganic materials 0.000 claims description 8
- 108060006633 protein kinase Proteins 0.000 claims description 8
- 239000013256 coordination polymer Substances 0.000 claims description 6
- 230000000694 effects Effects 0.000 claims description 6
- 230000001404 mediated effect Effects 0.000 claims description 6
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 6
- 208000023275 Autoimmune disease Diseases 0.000 claims description 5
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 5
- 230000002062 proliferating effect Effects 0.000 claims description 5
- 210000003169 central nervous system Anatomy 0.000 claims description 4
- 239000007819 coupling partner Substances 0.000 claims description 4
- 239000002552 dosage form Substances 0.000 claims description 4
- 230000002401 inhibitory effect Effects 0.000 claims description 4
- 125000002950 monocyclic group Chemical group 0.000 claims description 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- 229940124597 therapeutic agent Drugs 0.000 claims description 4
- 239000012472 biological sample Substances 0.000 claims description 3
- 208000027866 inflammatory disease Diseases 0.000 claims description 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 2
- BGDOLELXXPTPFX-UHFFFAOYSA-N 3,4-dihydro-2h-1,2-benzoxazine Chemical group C1=CC=C2ONCCC2=C1 BGDOLELXXPTPFX-UHFFFAOYSA-N 0.000 claims description 2
- 206010005003 Bladder cancer Diseases 0.000 claims description 2
- 208000019838 Blood disease Diseases 0.000 claims description 2
- 208000020084 Bone disease Diseases 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 229940126062 Compound A Drugs 0.000 claims description 2
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims description 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 206010025323 Lymphomas Diseases 0.000 claims description 2
- 108010025020 Nerve Growth Factor Proteins 0.000 claims description 2
- 102000007072 Nerve Growth Factors Human genes 0.000 claims description 2
- 206010029260 Neuroblastoma Diseases 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 206010038389 Renal cancer Diseases 0.000 claims description 2
- 102100031463 Serine/threonine-protein kinase PLK1 Human genes 0.000 claims description 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 239000002260 anti-inflammatory agent Substances 0.000 claims description 2
- 229940121363 anti-inflammatory agent Drugs 0.000 claims description 2
- 230000001028 anti-proliverative effect Effects 0.000 claims description 2
- 239000003443 antiviral agent Substances 0.000 claims description 2
- 208000037979 autoimmune inflammatory disease Diseases 0.000 claims description 2
- 201000010881 cervical cancer Diseases 0.000 claims description 2
- 238000002512 chemotherapy Methods 0.000 claims description 2
- 208000029742 colonic neoplasm Diseases 0.000 claims description 2
- 230000008878 coupling Effects 0.000 claims description 2
- 238000010168 coupling process Methods 0.000 claims description 2
- 238000005859 coupling reaction Methods 0.000 claims description 2
- 230000001066 destructive effect Effects 0.000 claims description 2
- 206010012601 diabetes mellitus Diseases 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 206010017758 gastric cancer Diseases 0.000 claims description 2
- 208000014951 hematologic disease Diseases 0.000 claims description 2
- 208000018706 hematopoietic system disease Diseases 0.000 claims description 2
- 239000002955 immunomodulating agent Substances 0.000 claims description 2
- 229940121354 immunomodulator Drugs 0.000 claims description 2
- 230000002584 immunomodulator Effects 0.000 claims description 2
- 229960003444 immunosuppressant agent Drugs 0.000 claims description 2
- 230000001861 immunosuppressant effect Effects 0.000 claims description 2
- 239000003018 immunosuppressive agent Substances 0.000 claims description 2
- 208000033065 inborn errors of immunity Diseases 0.000 claims description 2
- 230000005764 inhibitory process Effects 0.000 claims description 2
- 201000010982 kidney cancer Diseases 0.000 claims description 2
- 208000032839 leukemia Diseases 0.000 claims description 2
- 208000019423 liver disease Diseases 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 201000001441 melanoma Diseases 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 201000000050 myeloid neoplasm Diseases 0.000 claims description 2
- 239000003900 neurotrophic factor Substances 0.000 claims description 2
- 201000002528 pancreatic cancer Diseases 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 108010056274 polo-like kinase 1 Proteins 0.000 claims description 2
- 208000028529 primary immunodeficiency disease Diseases 0.000 claims description 2
- RDRCCJPEJDWSRJ-UHFFFAOYSA-N pyridine;1h-pyrrole Chemical group C=1C=CNC=1.C1=CC=NC=C1 RDRCCJPEJDWSRJ-UHFFFAOYSA-N 0.000 claims description 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 2
- 201000011549 stomach cancer Diseases 0.000 claims description 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 2
- 239000003981 vehicle Substances 0.000 claims description 2
- 229940079593 drug Drugs 0.000 claims 4
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 2
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
- 0 C*C=C(CC1CC(C)(C)C(C(C)C)C(CC(C)=C)C1)*C Chemical compound C*C=C(CC1CC(C)(C)C(C(C)C)C(CC(C)=C)C1)*C 0.000 description 7
- 201000010099 disease Diseases 0.000 description 4
- 108091000080 Phosphotransferase Proteins 0.000 description 3
- 102000020233 phosphotransferase Human genes 0.000 description 3
- 238000010835 comparative analysis Methods 0.000 description 1
- 230000003463 hyperproliferative effect Effects 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000031146 intracellular signal transduction Effects 0.000 description 1
- 230000004770 neurodegeneration Effects 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US85911306P | 2006-11-15 | 2006-11-15 | |
| US98414907P | 2007-10-31 | 2007-10-31 | |
| PCT/US2007/023999 WO2008060597A2 (en) | 2006-11-15 | 2007-11-15 | Compounds useful as protein kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010510216A JP2010510216A (ja) | 2010-04-02 |
| JP2010510216A5 true JP2010510216A5 (enExample) | 2011-12-15 |
Family
ID=39402262
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009537209A Pending JP2010510216A (ja) | 2006-11-15 | 2007-11-15 | プロテインキナーゼのインヒビターとして有用な化合物 |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US7838517B2 (enExample) |
| EP (1) | EP2094712B1 (enExample) |
| JP (1) | JP2010510216A (enExample) |
| AT (1) | ATE528309T1 (enExample) |
| AU (1) | AU2007319786A1 (enExample) |
| CA (1) | CA2669886A1 (enExample) |
| ES (1) | ES2372320T3 (enExample) |
| MX (1) | MX2009005231A (enExample) |
| NZ (1) | NZ576950A (enExample) |
| WO (1) | WO2008060597A2 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0620059D0 (en) * | 2006-10-10 | 2006-11-22 | Ucb Sa | Therapeutic agents |
| WO2008060597A2 (en) | 2006-11-15 | 2008-05-22 | Vertex Pharmaceuticals Incorporated | Compounds useful as protein kinase inhibitors |
| SG181715A1 (en) | 2009-12-18 | 2012-07-30 | Janssen Pharmaceutica Nv | Bicyclic thiazoles as allosteric modulators of mglur5 receptors |
| SG181716A1 (en) * | 2009-12-18 | 2012-07-30 | Janssen Pharmaceutica Nv | Bicyclic thiazoles as allosteric modulators of mglur5 receptors |
| CA2803446C (en) | 2010-07-02 | 2019-06-04 | University Health Network | Use of plk4 antagonists for treating pten mutant diseases |
| JP7008073B2 (ja) * | 2016-12-12 | 2022-01-25 | ユニオン・セラピューティクス・アクティエセルスカブ | 置換ピラゾロアゼピン－４－オンおよびそれらのホスホジエステラーゼ阻害剤としての使用 |
| US10793580B2 (en) | 2016-12-12 | 2020-10-06 | Leo Pharma A/S | Substituted pyrazoloazepin-8-ones and their use as phosphodiesterase inhibitors |
| US10906915B2 (en) | 2016-12-12 | 2021-02-02 | Leo Pharma A/S | Substituted pyrazoloazepin-4-ones and their use as phosphodiesterase inhibitors |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CH632755A5 (de) * | 1976-04-10 | 1982-10-29 | Basf Ag | Verfahren zur herstellung von thiophenverbindungen. |
| US5206240A (en) * | 1989-12-08 | 1993-04-27 | Merck & Co., Inc. | Nitrogen-containing spirocycles |
| CA2104371A1 (en) | 1991-12-26 | 1993-06-27 | Tohru Nakao | Condensed thiophene compound and pharmaceutical use thereof |
| BR0317430A (pt) * | 2002-12-20 | 2005-10-25 | Pharmacia Corp | Compostos inibidores de quinase-2 de proteìna ativada por quinase de proteìna ativada por mitógeno |
| US20060019952A1 (en) * | 2004-01-29 | 2006-01-26 | Elixir Pharmaceuticals, Inc. | Anti-viral therapeutics |
| GB0508471D0 (en) * | 2005-04-26 | 2005-06-01 | Celltech R&D Ltd | Therapeutic agents |
| WO2008060597A2 (en) | 2006-11-15 | 2008-05-22 | Vertex Pharmaceuticals Incorporated | Compounds useful as protein kinase inhibitors |
-
2007
- 2007-11-15 WO PCT/US2007/023999 patent/WO2008060597A2/en not_active Ceased
- 2007-11-15 CA CA002669886A patent/CA2669886A1/en not_active Abandoned
- 2007-11-15 ES ES07867462T patent/ES2372320T3/es active Active
- 2007-11-15 EP EP07867462A patent/EP2094712B1/en not_active Not-in-force
- 2007-11-15 NZ NZ576950A patent/NZ576950A/en not_active IP Right Cessation
- 2007-11-15 AT AT07867462T patent/ATE528309T1/de not_active IP Right Cessation
- 2007-11-15 JP JP2009537209A patent/JP2010510216A/ja active Pending
- 2007-11-15 AU AU2007319786A patent/AU2007319786A1/en not_active Abandoned
- 2007-11-15 MX MX2009005231A patent/MX2009005231A/es active IP Right Grant
-
2009
- 2009-05-15 US US12/466,420 patent/US7838517B2/en not_active Expired - Fee Related
-
2010
- 2010-10-13 US US12/903,390 patent/US8399458B2/en not_active Expired - Fee Related
-
2013
- 2013-02-13 US US13/765,864 patent/US20130267498A1/en not_active Abandoned
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