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 (https=) | 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 (https=) |
| EP (1) | EP2214673B1 (https=) |
| JP (1) | JP2011500621A (https=) |
| CA (1) | CA2702447A1 (https=) |
| WO (1) | WO2009053268A1 (https=) |
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 |
| EP2205609B1 (de) | 2007-10-19 | 2017-03-29 | Boehringer Ingelheim International GmbH | Heterocyclus-substituierte piperazino-dihydrothienopyrimidine |
| MX2010004026A (es) * | 2007-10-19 | 2010-04-30 | Boehringer Ingelheim Int | Piperidino-dihidrotienopirimidinas sustituidas. |
| ATE537175T1 (de) | 2007-10-19 | 2011-12-15 | Boehringer Ingelheim Int | Neue piperazino-dihydrothienopyrimidin-derivate |
| CA2753597A1 (en) * | 2009-02-27 | 2010-09-02 | Boehringer Ingelheim International Gmbh | Drug combinations containing pde4-inhibitors and nsaids |
| US9802954B2 (en) | 2011-08-24 | 2017-10-31 | Boehringer Ingelheim International Gmbh | Piperidino-dihydrothienopyrimidine sulfoxides and their use for treating COPD and asthma |
| US20130059866A1 (en) | 2011-08-24 | 2013-03-07 | Boehringer Ingelheim International Gmbh | Novel piperidino-dihydrothienopyrimidine sulfoxides and their use for treating copd and asthma |
| WO2019057806A1 (en) | 2017-09-20 | 2019-03-28 | Leo Pharma A/S | SUBSTITUTED DIHYDROTHIENOPYRIMIDINES AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS |
| JP7198820B2 (ja) * | 2017-12-15 | 2023-01-04 | ユニオン・セラピューティクス・アクティエセルスカブ | 置換アゼチジンジヒドロチエノピリミジンおよびホスホジエステラーゼ阻害剤としてのそれらの使用 |
| ES2935615T3 (es) | 2017-12-15 | 2023-03-08 | Union Therapeutics As | Azetidina dihidrotienopiridinas sustituidas y su uso como inhibidores de la fosfodiesterasa |
| CN111712503B (zh) | 2017-12-15 | 2024-04-09 | 联合疗法公司 | 取代的四氢吡喃二氢噻吩并嘧啶类化合物及其作为磷酸二酯酶抑制剂的用途 |
| EP4570804A1 (en) * | 2022-08-09 | 2025-06-18 | Xizang Haisco Pharmaceutical Co., Ltd. | Pde4b inhibitor and use thereof |
| WO2024067660A1 (zh) | 2022-09-29 | 2024-04-04 | 苏州爱科百发生物医药技术有限公司 | 氮杂稠环类化合物、其制备方法及其在医药上的应用 |
| TW202535412A (zh) * | 2024-02-04 | 2025-09-16 | 大陸商西藏海思科製藥有限公司 | Pde4b抑制劑的晶型及其在醫藥上的用途 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA03009925A (es) * | 2001-04-30 | 2004-06-30 | Bayer Pharmaceuticals Corp | Nuevas tiofeno [2,3-d]pirimidinas 4-amino-5,6-sustituidas. |
| RS51163B (sr) * | 2006-04-19 | 2010-10-31 | Boehringer Ingelheim International Gmbh. | Dihidrotienopirimidin za lečenje zapaljenskih bolesti |
| EP1847543A1 (de) * | 2006-04-19 | 2007-10-24 | Boehringer Ingelheim Pharma GmbH & Co. KG | Dihydrothienopyrimidine zur Behandlung von entzündlichen Erkrankungen |
-
2008
- 2008-10-13 JP JP2010529353A patent/JP2011500621A/ja active Pending
- 2008-10-13 EP EP08841954A patent/EP2214673B1/de active Active
- 2008-10-13 CA CA2702447A patent/CA2702447A1/en not_active Abandoned
- 2008-10-13 WO PCT/EP2008/063747 patent/WO2009053268A1/de not_active Ceased
- 2008-10-13 US US12/738,412 patent/US20110028441A1/en not_active Abandoned
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