JP2009521399A5 - - Google Patents
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- Publication number
- JP2009521399A5 JP2009521399A5 JP2008535605A JP2008535605A JP2009521399A5 JP 2009521399 A5 JP2009521399 A5 JP 2009521399A5 JP 2008535605 A JP2008535605 A JP 2008535605A JP 2008535605 A JP2008535605 A JP 2008535605A JP 2009521399 A5 JP2009521399 A5 JP 2009521399A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- leukotriene
- nhc
- alkyl
- 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.)
- Granted
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- 150000002617 leukotrienes Chemical class 0.000 claims 14
- 125000000217 alkyl group Chemical group 0.000 claims 11
- 125000001072 heteroaryl group Chemical group 0.000 claims 11
- 125000003118 aryl group Chemical group 0.000 claims 10
- 150000001875 compounds Chemical class 0.000 claims 10
- 239000003112 inhibitor Substances 0.000 claims 9
- 208000024891 symptom Diseases 0.000 claims 8
- 125000003342 alkenyl group Chemical group 0.000 claims 7
- 230000001419 dependent effect Effects 0.000 claims 7
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 125000005330 8 membered heterocyclic group Chemical group 0.000 claims 3
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- -1 or arthrotech Chemical compound 0.000 claims 3
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 claims 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 239000000090 biomarker Substances 0.000 claims 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 2
- 229960005293 etodolac Drugs 0.000 claims 2
- XFBVBWWRPKNWHW-UHFFFAOYSA-N etodolac Chemical compound C1COC(CC)(CC(O)=O)C2=N[C]3C(CC)=CC=CC3=C21 XFBVBWWRPKNWHW-UHFFFAOYSA-N 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000004404 heteroalkyl group Chemical group 0.000 claims 2
- CGIGDMFJXJATDK-UHFFFAOYSA-N indomethacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 239000003550 marker Substances 0.000 claims 2
- KBOPZPXVLCULAV-UHFFFAOYSA-N mesalamine Chemical compound NC1=CC=C(O)C(C(O)=O)=C1 KBOPZPXVLCULAV-UHFFFAOYSA-N 0.000 claims 2
- 239000003607 modifier Substances 0.000 claims 2
- 108090000623 proteins and genes Proteins 0.000 claims 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims 2
- WONYMNWUJVKVII-UHFFFAOYSA-N 3,5-diiodothyropropionic acid Chemical compound IC1=CC(CCC(=O)O)=CC(I)=C1OC1=CC=C(O)C=C1 WONYMNWUJVKVII-UHFFFAOYSA-N 0.000 claims 1
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 1
- 102000004023 5-Lipoxygenase-Activating Proteins Human genes 0.000 claims 1
- 108090000411 5-Lipoxygenase-Activating Proteins Proteins 0.000 claims 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 1
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 1
- 206010002329 Aneurysm Diseases 0.000 claims 1
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- UCHDWCPVSPXUMX-TZIWLTJVSA-N Montelukast Chemical compound CC(C)(O)C1=CC=CC=C1CC[C@H](C=1C=C(\C=C\C=2N=C3C=C(Cl)C=CC3=CC=2)C=CC=1)SCC1(CC(O)=O)CC1 UCHDWCPVSPXUMX-TZIWLTJVSA-N 0.000 claims 1
- BLXXJMDCKKHMKV-UHFFFAOYSA-N Nabumetone Chemical compound C1=C(CCC(C)=O)C=CC2=CC(OC)=CC=C21 BLXXJMDCKKHMKV-UHFFFAOYSA-N 0.000 claims 1
- CMWTZPSULFXXJA-UHFFFAOYSA-N Naproxen Natural products C1=C(C(C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- YEEZWCHGZNKEEK-UHFFFAOYSA-N Zafirlukast Chemical compound COC1=CC(C(=O)NS(=O)(=O)C=2C(=CC=CC=2)C)=CC=C1CC(C1=C2)=CN(C)C1=CC=C2NC(=O)OC1CCCC1 YEEZWCHGZNKEEK-UHFFFAOYSA-N 0.000 claims 1
- 229960001138 acetylsalicylic acid Drugs 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940072224 asacol Drugs 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 125000006580 bicyclic heterocycloalkyl group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229960000590 celecoxib Drugs 0.000 claims 1
- RZEKVGVHFLEQIL-UHFFFAOYSA-N celecoxib Chemical compound C1=CC(C)=CC=C1C1=CC(C(F)(F)F)=NN1C1=CC=C(S(N)(=O)=O)C=C1 RZEKVGVHFLEQIL-UHFFFAOYSA-N 0.000 claims 1
- 229960001259 diclofenac Drugs 0.000 claims 1
- DCOPUUMXTXDBNB-UHFFFAOYSA-N diclofenac Chemical compound OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl DCOPUUMXTXDBNB-UHFFFAOYSA-N 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 230000002526 effect on cardiovascular system Effects 0.000 claims 1
- 102000054766 genetic haplotypes Human genes 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 229960000905 indomethacin Drugs 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- DKYWVDODHFEZIM-UHFFFAOYSA-N ketoprofen Chemical compound OC(=O)C(C)C1=CC=CC(C(=O)C=2C=CC=CC=2)=C1 DKYWVDODHFEZIM-UHFFFAOYSA-N 0.000 claims 1
- 229960000991 ketoprofen Drugs 0.000 claims 1
- 239000003199 leukotriene receptor blocking agent Substances 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- HYYBABOKPJLUIN-UHFFFAOYSA-N mefenamic acid Chemical compound CC1=CC=CC(NC=2C(=CC=CC=2)C(O)=O)=C1C HYYBABOKPJLUIN-UHFFFAOYSA-N 0.000 claims 1
- 239000002207 metabolite Substances 0.000 claims 1
- 238000012544 monitoring process Methods 0.000 claims 1
- 125000006578 monocyclic heterocycloalkyl group Chemical group 0.000 claims 1
- 229960005127 montelukast Drugs 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 229960004270 nabumetone Drugs 0.000 claims 1
- 229960002009 naproxen Drugs 0.000 claims 1
- CMWTZPSULFXXJA-VIFPVBQESA-N naproxen Chemical compound C1=C([C@H](C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-VIFPVBQESA-N 0.000 claims 1
- 239000002674 ointment Substances 0.000 claims 1
- 239000006195 ophthalmic dosage form Substances 0.000 claims 1
- 239000006186 oral dosage form Substances 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 230000037361 pathway Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 229960002702 piroxicam Drugs 0.000 claims 1
- QYSPLQLAKJAUJT-UHFFFAOYSA-N piroxicam Chemical compound OC=1C2=CC=CC=C2S(=O)(=O)N(C)C=1C(=O)NC1=CC=CC=N1 QYSPLQLAKJAUJT-UHFFFAOYSA-N 0.000 claims 1
- 229960004583 pranlukast Drugs 0.000 claims 1
- UAJUXJSXCLUTNU-UHFFFAOYSA-N pranlukast Chemical compound C=1C=C(OCCCCC=2C=CC=CC=2)C=CC=1C(=O)NC(C=1)=CC=C(C(C=2)=O)C=1OC=2C=1N=NNN=1 UAJUXJSXCLUTNU-UHFFFAOYSA-N 0.000 claims 1
- XOFYZVNMUHMLCC-ZPOLXVRWSA-N prednisone Chemical compound O=C1C=C[C@]2(C)[C@H]3C(=O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 XOFYZVNMUHMLCC-ZPOLXVRWSA-N 0.000 claims 1
- 229960004618 prednisone Drugs 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 208000002815 pulmonary hypertension Diseases 0.000 claims 1
- 230000000241 respiratory effect Effects 0.000 claims 1
- 206010039083 rhinitis Diseases 0.000 claims 1
- 125000006413 ring segment Chemical group 0.000 claims 1
- 229960000371 rofecoxib Drugs 0.000 claims 1
- RZJQGNCSTQAWON-UHFFFAOYSA-N rofecoxib Chemical compound C1=CC(S(=O)(=O)C)=CC=C1C1=C(C=2C=CC=CC=2)C(=O)OC1 RZJQGNCSTQAWON-UHFFFAOYSA-N 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 238000012216 screening Methods 0.000 claims 1
- 239000000243 solution Substances 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 239000000829 suppository Substances 0.000 claims 1
- 239000000725 suspension Substances 0.000 claims 1
- LNPDTQAFDNKSHK-UHFFFAOYSA-N valdecoxib Chemical compound CC=1ON=C(C=2C=CC=CC=2)C=1C1=CC=C(S(N)(=O)=O)C=C1 LNPDTQAFDNKSHK-UHFFFAOYSA-N 0.000 claims 1
- 229960002004 valdecoxib Drugs 0.000 claims 1
- 229960004764 zafirlukast Drugs 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US72557305P | 2005-10-11 | 2005-10-11 | |
| US60/725,573 | 2005-10-11 | ||
| US11/538,762 | 2006-10-04 | ||
| US11/538,762 US7405302B2 (en) | 2005-10-11 | 2006-10-04 | 5-lipoxygenase-activating protein (FLAP) inhibitors |
| PCT/US2006/039421 WO2007047207A2 (en) | 2005-10-11 | 2006-10-05 | 5-lipoxygenase-activating protein (flap) inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009521399A JP2009521399A (ja) | 2009-06-04 |
| JP2009521399A5 true JP2009521399A5 (enExample) | 2009-11-12 |
| JP5327518B2 JP5327518B2 (ja) | 2013-10-30 |
Family
ID=37963034
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008535605A Expired - Fee Related JP5327518B2 (ja) | 2005-10-11 | 2006-10-05 | ５−リポキシゲナーゼ−活性化タンパク質（ｆｌａｐ）阻害剤 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US7405302B2 (enExample) |
| EP (1) | EP1933842B1 (enExample) |
| JP (1) | JP5327518B2 (enExample) |
| ES (1) | ES2399702T3 (enExample) |
| WO (1) | WO2007047207A2 (enExample) |
Families Citing this family (82)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8399666B2 (en) * | 2005-11-04 | 2013-03-19 | Panmira Pharmaceuticals, Llc | 5-lipoxygenase-activating protein (FLAP) inhibitors |
| GB2431927B (en) * | 2005-11-04 | 2010-03-17 | Amira Pharmaceuticals Inc | 5-Lipoxygenase-activating protein (FLAP) inhibitors |
| US7977359B2 (en) | 2005-11-04 | 2011-07-12 | Amira Pharmaceuticals, Inc. | 5-lipdxygenase-activating protein (FLAP) inhibitors |
| US20070225285A1 (en) * | 2005-11-04 | 2007-09-27 | Amira Pharmaceuticals, Inc. | 5-lipoxygenase-activating protein (flap) inhibitors |
| US20070219206A1 (en) * | 2005-11-04 | 2007-09-20 | Amira Pharmaceuticals, Inc. | 5-lipoxygenase-activating protein (flap) inhibitors |
| US20070244128A1 (en) * | 2005-11-04 | 2007-10-18 | Amira Pharmaceuticals, Inc. | 5-lipoxygenase-activating protein (flap) inhibitors |
| WO2008067566A1 (en) | 2006-11-30 | 2008-06-05 | Amira Pharmaceuticals, Inc. | Compositions and treatments comprising 5-lipoxygenase-activating protein inhibitors and nitric oxide modulators |
| JP5220025B2 (ja) | 2006-12-04 | 2013-06-26 | プロメディオール， インコーポレイテッド | 線維症疾患を処置するための併用療法 |
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| TW200920369A (en) * | 2007-10-26 | 2009-05-16 | Amira Pharmaceuticals Inc | 5-lipoxygenase activating protein (flap) inhibitor |
| JP5791500B2 (ja) * | 2008-05-23 | 2015-10-07 | パンミラ ファーマシューティカルズ，エルエルシー． | ５−リポキシゲナーゼ活性化タンパク質阻害剤 |
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| US5081138A (en) | 1986-12-17 | 1992-01-14 | Merck Frosst Canada, Inc. | 3-hetero-substituted-n-benzyl-indoles and prevention of leucotriene synthesis therewith |
| NZ234883A (en) * | 1989-08-22 | 1995-01-27 | Merck Frosst Canada Inc | Quinolin-2-ylmethoxy indole derivatives, preparation and pharmaceutical compositions thereof |
| US5252585A (en) * | 1992-02-03 | 1993-10-12 | Merck Frosst Canada, Inc. | Fluorinated quinoline indoles as inhibitors of the biosynthesis of leukotrienes |
| US5308850A (en) * | 1991-09-30 | 1994-05-03 | Merck Frosst Canada, Inc. | (Bicyclic-hetero-arylmethoxy)indoles as inhibitors of leukotriene biosynthesis |
| US5389650A (en) * | 1991-09-30 | 1995-02-14 | Merck Frosst Canada, Inc. | (Azaarylmethoxy)indoles as inhibitors of leukotriene biosynthesis |
| CA2079374C (en) * | 1991-09-30 | 2003-08-05 | Merck Frosst Canada Incorporated | (bicyclic-azaarylmethoxy)indoles as inhibitors of leukotriene biosynthesis |
| DE19948417A1 (de) * | 1999-10-07 | 2001-04-19 | Morphochem Ag | Imidazol-Derivate und ihre Verwendung als Arzneimittel |
| DE10007203A1 (de) * | 2000-02-17 | 2001-08-23 | Asta Medica Ag | Neue Kombination nichtsedierender Antihistaminika mit Substanzen, die die Leukotrienwirkung beeinflussen, zur Behandlung der Rhinitis/Konjunktivitis |
| MXPA02010763A (es) * | 2000-06-14 | 2003-03-10 | Warner Lambert Co | Heterociclicos biciclos-6,5 fusionados. |
| AU2003211384B2 (en) * | 2002-02-21 | 2008-12-11 | Asahi Kasei Pharma Corporation | Substituted phenylalkanoic acid derivative and use thereof |
| US20040198800A1 (en) | 2002-12-19 | 2004-10-07 | Geoffrey Allan | Lipoxygenase inhibitors as hypolipidemic and anti-hypertensive agents |
| 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) |
| EP1911759A4 (en) * | 2005-07-22 | 2010-07-21 | Shionogi & Co | AZAINDOL DERIVATIVE ANTAGONISTIC EFFECT ON PGD2 RECEPTOR |
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- 2006-10-05 WO PCT/US2006/039421 patent/WO2007047207A2/en not_active Ceased
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