JP2011500621A5 - - Google Patents
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- Publication number
- JP2011500621A5 JP2011500621A5 JP2010529353A JP2010529353A JP2011500621A5 JP 2011500621 A5 JP2011500621 A5 JP 2011500621A5 JP 2010529353 A JP2010529353 A JP 2010529353A JP 2010529353 A JP2010529353 A JP 2010529353A JP 2011500621 A5 JP2011500621 A5 JP 2011500621A5
- Authority
- JP
- Japan
- Prior art keywords
- alkylene
- phenyl
- het
- aryl
- 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
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 64
- 229910052731 fluorine Inorganic materials 0.000 claims 40
- 125000001072 heteroaryl group Chemical group 0.000 claims 33
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 29
- 125000004043 oxo group Chemical group O=* 0.000 claims 27
- 150000001875 compounds Chemical class 0.000 claims 25
- 229910052736 halogen Inorganic materials 0.000 claims 25
- 150000002367 halogens Chemical class 0.000 claims 25
- 229910052799 carbon Inorganic materials 0.000 claims 22
- 229910052801 chlorine Inorganic materials 0.000 claims 22
- 239000000460 chlorine Substances 0.000 claims 22
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 20
- 229910052794 bromium Inorganic materials 0.000 claims 19
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 19
- 125000002950 monocyclic group Chemical group 0.000 claims 18
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 18
- -1 C 1-6 -alkanol Chemical group 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 16
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 14
- 229920006395 saturated elastomer Polymers 0.000 claims 11
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 9
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 9
- 239000011737 fluorine Substances 0.000 claims 9
- 125000005842 heteroatom Chemical group 0.000 claims 9
- 229910052760 oxygen Inorganic materials 0.000 claims 9
- 229910052717 sulfur Inorganic materials 0.000 claims 9
- 125000000623 heterocyclic group Chemical group 0.000 claims 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 7
- 125000000217 alkyl group Chemical group 0.000 claims 7
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 6
- 125000002619 bicyclic group Chemical group 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 5
- 230000001154 acute effect Effects 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 2
- 208000020925 Bipolar disease Diseases 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- 208000028683 bipolar I disease Diseases 0.000 claims 2
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 210000003169 central nervous system Anatomy 0.000 claims 2
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 230000000414 obstructive effect Effects 0.000 claims 2
- 230000002093 peripheral effect Effects 0.000 claims 2
- 210000001428 peripheral nervous system Anatomy 0.000 claims 2
- 125000001639 phenylmethylene group Chemical group [H]C(=*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- 230000000241 respiratory effect Effects 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 102100024167 C-C chemokine receptor type 3 Human genes 0.000 claims 1
- 101710149862 C-C chemokine receptor type 3 Proteins 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 206010009137 Chronic sinusitis Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010019196 Head injury Diseases 0.000 claims 1
- 206010021143 Hypoxia Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000019693 Lung disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 102100029438 Nitric oxide synthase, inducible Human genes 0.000 claims 1
- 101710089543 Nitric oxide synthase, inducible Proteins 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 claims 1
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 208000005298 acute pain Diseases 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 125000000958 aryl methylene group Chemical group 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 102000012740 beta Adrenergic Receptors Human genes 0.000 claims 1
- 108010079452 beta Adrenergic Receptors Proteins 0.000 claims 1
- 208000025307 bipolar depression Diseases 0.000 claims 1
- 230000006931 brain damage Effects 0.000 claims 1
- 231100000874 brain damage Toxicity 0.000 claims 1
- 208000029028 brain injury Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000027157 chronic rhinosinusitis Diseases 0.000 claims 1
- 239000003246 corticosteroid Substances 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 230000001079 digestive effect Effects 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 229940121647 egfr inhibitor Drugs 0.000 claims 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 1
- 230000007954 hypoxia Effects 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- YEESKJGWJFYOOK-IJHYULJSSA-N leukotriene D4 Chemical compound CCCCC\C=C/C\C=C/C=C/C=C/[C@H]([C@@H](O)CCCC(O)=O)SC[C@H](N)C(=O)NCC(O)=O YEESKJGWJFYOOK-IJHYULJSSA-N 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 230000003843 mucus production Effects 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 claims 1
- 125000003367 polycyclic group Chemical group 0.000 claims 1
- 239000000018 receptor agonist Substances 0.000 claims 1
- 229940044601 receptor agonist Drugs 0.000 claims 1
- 208000023504 respiratory system disease Diseases 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 125000003003 spiro group Chemical group 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07118897 | 2007-10-19 | ||
| PCT/EP2008/063747 WO2009053268A1 (de) | 2007-10-19 | 2008-10-13 | Neue phenyl-substituierte piperazino-dihydrothienopyrimidine |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011500621A JP2011500621A (ja) | 2011-01-06 |
| JP2011500621A5 true JP2011500621A5 (enExample) | 2011-12-01 |
Family
ID=39349696
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010529353A Pending JP2011500621A (ja) | 2007-10-19 | 2008-10-13 | 新規フェニル置換ピペラジノ−ジヒドロチエノピリミジン |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20110028441A1 (enExample) |
| EP (1) | EP2214673B1 (enExample) |
| JP (1) | JP2011500621A (enExample) |
| CA (1) | CA2702447A1 (enExample) |
| WO (1) | WO2009053268A1 (enExample) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1847543A1 (de) | 2006-04-19 | 2007-10-24 | Boehringer Ingelheim Pharma GmbH & Co. KG | Dihydrothienopyrimidine zur Behandlung von entzündlichen Erkrankungen |
| RU2500681C2 (ru) | 2007-10-19 | 2013-12-10 | Берингер Ингельхайм Интернациональ Гмбх | Замещенные гетероциклом пиперазинодигидротиенопиримидины |
| SI2610258T1 (sl) | 2007-10-19 | 2014-12-31 | Boehringer Ingelheim International Gmbh | Substituirani piperidino-dihidrotienopirimidini |
| EP2215093B1 (de) | 2007-10-19 | 2011-12-14 | Boehringer Ingelheim International GmbH | Neue piperazino-dihydrothienopyrimidin-derivate |
| WO2010097332A1 (de) * | 2009-02-27 | 2010-09-02 | Boehringer Ingelheim International Gmbh | Arzneimittelkombinationen enthaltend pde4-inhibitoren und nsaids |
| US20130059866A1 (en) | 2011-08-24 | 2013-03-07 | Boehringer Ingelheim International Gmbh | Novel piperidino-dihydrothienopyrimidine sulfoxides and their use for treating copd and asthma |
| US9802954B2 (en) | 2011-08-24 | 2017-10-31 | Boehringer Ingelheim International Gmbh | Piperidino-dihydrothienopyrimidine sulfoxides and their use for treating COPD and asthma |
| US11365204B2 (en) | 2017-09-20 | 2022-06-21 | UNION therapeutics A/S | Substituted dihydrothienopyrimidines and their use as phosphodiesterase inhibitors |
| WO2019115775A1 (en) | 2017-12-15 | 2019-06-20 | Leo Pharma A/S | Substituted tetrahydropyran dihydrothienopyrimidines and their use as phosphodiesterase inhibitors |
| WO2019115776A1 (en) | 2017-12-15 | 2019-06-20 | Leo Pharma A/S | Substituted azetidine dihydrothienopyridines and their use as phosphodiesterase inhibitors |
| WO2019115774A1 (en) | 2017-12-15 | 2019-06-20 | Leo Pharma A/S | Substituted azetidine dihydrothienopyrimidines and their use as phosphodiesterase inhibitors |
| JP2025528779A (ja) * | 2022-08-09 | 2025-09-02 | シーザン ハイスーク ファーマシューティカル カンパニー リミテッド | Ｐｄｅ４ｂ阻害剤及びその用途 |
| EP4596554A4 (en) | 2022-09-29 | 2025-12-10 | Suzhou Arkbiopharmaceutical Co Ltd | Fused AZA Cyclic Compound, its Preparation Process and its Use in Medicine |
| WO2025162289A2 (zh) * | 2024-02-04 | 2025-08-07 | 西藏海思科制药有限公司 | 一种pde4b抑制剂的晶型及其在医药上的用途 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101100472A (zh) * | 2001-04-30 | 2008-01-09 | 美国拜尔公司 | 4-氨基-5,6-取代的噻吩并[2,3-d]嘧啶化合物及其应用 |
| EP1847543A1 (de) * | 2006-04-19 | 2007-10-24 | Boehringer Ingelheim Pharma GmbH & Co. KG | Dihydrothienopyrimidine zur Behandlung von entzündlichen Erkrankungen |
| HRP20090395T1 (hr) * | 2006-04-19 | 2009-08-31 | Boehringer Ingelheim International Gmbh | Dihidrotienpirimidini za liječenje upalnih bolesti |
-
2008
- 2008-10-13 CA CA2702447A patent/CA2702447A1/en not_active Abandoned
- 2008-10-13 US US12/738,412 patent/US20110028441A1/en not_active Abandoned
- 2008-10-13 EP EP08841954A patent/EP2214673B1/de active Active
- 2008-10-13 JP JP2010529353A patent/JP2011500621A/ja active Pending
- 2008-10-13 WO PCT/EP2008/063747 patent/WO2009053268A1/de not_active Ceased