JP2013537908A5 - - Google Patents
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- Publication number
- JP2013537908A5 JP2013537908A5 JP2013530220A JP2013530220A JP2013537908A5 JP 2013537908 A5 JP2013537908 A5 JP 2013537908A5 JP 2013530220 A JP2013530220 A JP 2013530220A JP 2013530220 A JP2013530220 A JP 2013530220A JP 2013537908 A5 JP2013537908 A5 JP 2013537908A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- independently
- optionally substituted
- alkoxy
- substituted
- 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
Links
- 125000000217 alkyl group Chemical group 0.000 claims 53
- -1 hydroxy, amino Chemical group 0.000 claims 20
- 125000003545 alkoxy group Chemical group 0.000 claims 17
- 229910052739 hydrogen Inorganic materials 0.000 claims 17
- 229910052736 halogen Inorganic materials 0.000 claims 16
- 150000002367 halogens Chemical class 0.000 claims 16
- 239000001257 hydrogen Substances 0.000 claims 16
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 15
- 125000004043 oxo group Chemical group O=* 0.000 claims 14
- 125000000623 heterocyclic group Chemical group 0.000 claims 11
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 9
- 125000002757 morpholinyl group Chemical group 0.000 claims 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 8
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 8
- 125000004193 piperazinyl group Chemical group 0.000 claims 8
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 7
- 125000003386 piperidinyl group Chemical group 0.000 claims 6
- 125000003373 pyrazinyl group Chemical group 0.000 claims 6
- 125000002098 pyridazinyl group Chemical group 0.000 claims 6
- 125000004076 pyridyl group Chemical group 0.000 claims 6
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 6
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 5
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 4
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 4
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 125000002883 imidazolyl group Chemical group 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 4
- 125000003226 pyrazolyl group Chemical group 0.000 claims 4
- 125000006559 (C1-C3) alkylamino group Chemical group 0.000 claims 3
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 3
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 3
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 3
- 150000002617 leukotrienes Chemical class 0.000 claims 3
- 230000001404 mediated effect Effects 0.000 claims 3
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 3
- 125000000335 thiazolyl group Chemical group 0.000 claims 3
- PAPNRQCYSFBWDI-UHFFFAOYSA-N 2,5-Dimethyl-1H-pyrrole Chemical compound CC1=CC=C(C)N1 PAPNRQCYSFBWDI-UHFFFAOYSA-N 0.000 claims 2
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 2
- 125000005189 alkyl hydroxy group Chemical group 0.000 claims 2
- 125000004663 dialkyl amino group Chemical group 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000002541 furyl group Chemical group 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
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 125000003566 oxetanyl group Chemical group 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 claims 1
- OUYLXVQKVBXUGW-UHFFFAOYSA-N 2,3-dimethyl-1h-pyrrole Chemical compound CC=1C=CNC=1C OUYLXVQKVBXUGW-UHFFFAOYSA-N 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000000640 cyclooctyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 230000002526 effect on cardiovascular system Effects 0.000 claims 1
- 230000003176 fibrotic effect Effects 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 150000002825 nitriles Chemical class 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000001301 oxygen Chemical group 0.000 claims 1
- 230000002685 pulmonary effect Effects 0.000 claims 1
- 229910052717 sulfur Chemical group 0.000 claims 1
- 239000011593 sulfur Chemical group 0.000 claims 1
- 125000005958 tetrahydrothienyl group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 0 C*C(*)c1cnc(N)nc1 Chemical compound C*C(*)c1cnc(N)nc1 0.000 description 6
- MKEUSJZGHJDRHG-UHFFFAOYSA-N CC(C)(C)c1ccc(N)nc1 Chemical compound CC(C)(C)c1ccc(N)nc1 MKEUSJZGHJDRHG-UHFFFAOYSA-N 0.000 description 1
- LFGKMIQEQHDOSL-UHFFFAOYSA-N CC(C)c1cnc(NC)nc1 Chemical compound CC(C)c1cnc(NC)nc1 LFGKMIQEQHDOSL-UHFFFAOYSA-N 0.000 description 1
- NCIQRMGNIIQTRF-UHFFFAOYSA-N CCC(C)c1ncc(N)nc1 Chemical compound CCC(C)c1ncc(N)nc1 NCIQRMGNIIQTRF-UHFFFAOYSA-N 0.000 description 1
- LURGZVKKNLPCSQ-UHFFFAOYSA-N Cc1nc(C#N)c(N)nc1 Chemical compound Cc1nc(C#N)c(N)nc1 LURGZVKKNLPCSQ-UHFFFAOYSA-N 0.000 description 1
- UPDBFKHEEKEBOM-UHFFFAOYSA-N Cc1nc(N)cnc1CC=C Chemical compound Cc1nc(N)cnc1CC=C UPDBFKHEEKEBOM-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38573010P | 2010-09-23 | 2010-09-23 | |
| US61/385,730 | 2010-09-23 | ||
| US201161533846P | 2011-09-13 | 2011-09-13 | |
| US61/533,846 | 2011-09-13 | ||
| PCT/US2011/052252 WO2012040137A1 (en) | 2010-09-23 | 2011-09-20 | Oxadiazole inhibitors of leukotriene production |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013537908A JP2013537908A (ja) | 2013-10-07 |
| JP2013537908A5 true JP2013537908A5 (enExample) | 2014-11-13 |
| JP5828188B2 JP5828188B2 (ja) | 2015-12-02 |
Family
ID=44720162
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013530220A Active JP5828188B2 (ja) | 2010-09-23 | 2011-09-20 | ロイコトリエン産生のオキサジアゾール阻害剤 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US8580825B2 (enExample) |
| EP (1) | EP2619196B1 (enExample) |
| JP (1) | JP5828188B2 (enExample) |
| WO (1) | WO2012040137A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2011292285A1 (en) | 2010-08-16 | 2013-01-31 | Boehringer Ingelheim International Gmbh | Oxadiazole inhibitors of leukotriene production |
| EP2609092B1 (en) * | 2010-08-26 | 2015-04-01 | Boehringer Ingelheim International GmbH | Oxadiazole inhibitors of leukotriene production |
| US8580825B2 (en) | 2010-09-23 | 2013-11-12 | Boehringer Ingelheim International Gmbh | Oxadiazole inhibitors of leukotriene production |
| BR112013008638A2 (pt) * | 2010-09-23 | 2016-06-21 | Boehringer Ingelheim Int | inibidores de oxadiazol de produção de leucotrieno |
| AR089853A1 (es) | 2012-02-01 | 2014-09-24 | Boehringer Ingelheim Int | Inhibidores de oxadiazol de la produccion de leucotrienos para terapia de combinacion, composicion farmaceutica, uso |
| CN107098884A (zh) | 2016-02-19 | 2017-08-29 | 中国科学院上海药物研究所 | 一类取代的氨基吡啶类化合物及其制备和用途 |
| CN114957234A (zh) * | 2022-05-31 | 2022-08-30 | 浙江工业大学 | 一种含三唑的苯基连噁二唑类衍生物及其制备方法和应用 |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5102897A (en) * | 1990-03-27 | 1992-04-07 | Warner-Lambert Company | 3,5-ditertiarybutyl-4-hydroxyphenyl, 1,3,4-thiadiazoles and oxadiazoles linked by carbon, oxygen, and sulfur residues |
| TR200200310T2 (tr) * | 1999-08-06 | 2002-08-21 | Janssen Pharmaceutica N.V. | Interlökin-5 inhibe eden 6-azaurasil türevleri. |
| US7319108B2 (en) | 2004-01-25 | 2008-01-15 | Sanofi-Aventis Deutschland Gmbh | Aryl-substituted heterocycles, process for their preparation and their use as medicaments |
| WO2006044602A2 (en) | 2004-10-18 | 2006-04-27 | Merck & Co., Inc. | Diphenyl substituted alkanes as flap inhiibitors |
| JP5112316B2 (ja) * | 2005-08-10 | 2013-01-09 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | 選択的ｈｍ７４ａアゴニストとしてのキサンチン誘導体 |
| 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 |
| US8399666B2 (en) | 2005-11-04 | 2013-03-19 | Panmira Pharmaceuticals, Llc | 5-lipoxygenase-activating protein (FLAP) inhibitors |
| EP2013174B1 (en) | 2006-04-11 | 2013-05-08 | Merck Sharp & Dohme Corp. | Diaryl substituted alkanes |
| ATE540681T1 (de) | 2006-06-26 | 2012-01-15 | Amgen Inc | Verfahren zur behandlung von atherosklerose |
| JP2010502615A (ja) * | 2006-09-01 | 2010-01-28 | メルク エンド カムパニー インコーポレーテッド | ５−リポキシゲナーゼ活性化タンパク質（ｆｌａｐ）の阻害剤 |
| WO2008050200A1 (en) * | 2006-10-24 | 2008-05-02 | Pfizer Products Inc. | Oxadiazole compounds as calcium channel antagonists |
| CA2683948A1 (en) | 2007-04-20 | 2008-10-30 | Merck Frosst Canada Ltd. | Novel heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase |
| AU2008266960A1 (en) | 2007-06-20 | 2008-12-24 | Merck Sharp & Dohme Corp. | Diphenyl substituted alkanes |
| EP2209761A4 (en) | 2007-10-10 | 2012-01-04 | Merck Sharp & Dohme | DIPHENYL-SUBSTITUTED CYCLOAL CANS |
| US8598209B2 (en) * | 2008-10-31 | 2013-12-03 | Merck Sharp & Dohme Corp. | P2X3, receptor antagonists for treatment of pain |
| WO2010057118A2 (en) * | 2008-11-17 | 2010-05-20 | Amira Pharmaceuticals, Inc. | Heterocyclic antagonists of prostaglandin d2 receptors |
| EP2393811A1 (en) | 2009-02-04 | 2011-12-14 | Pfizer Inc. | 4-amino-7,8-dihydropyrido[4,3-d]pyrimidin-5(6h)-one derivatives |
| RU2012154447A (ru) | 2010-05-12 | 2014-06-20 | Вандербилт Юниверсити | Гетероциклические сульфоновые аллостерические потенциаторы mglur4, композиции и способы лечения неврологических дисфункций |
| AU2011292285A1 (en) * | 2010-08-16 | 2013-01-31 | Boehringer Ingelheim International Gmbh | Oxadiazole inhibitors of leukotriene production |
| EP2609092B1 (en) * | 2010-08-26 | 2015-04-01 | Boehringer Ingelheim International GmbH | Oxadiazole inhibitors of leukotriene production |
| US8580825B2 (en) | 2010-09-23 | 2013-11-12 | Boehringer Ingelheim International Gmbh | Oxadiazole inhibitors of leukotriene production |
| BR112013008638A2 (pt) * | 2010-09-23 | 2016-06-21 | Boehringer Ingelheim Int | inibidores de oxadiazol de produção de leucotrieno |
-
2011
- 2011-09-20 US US13/237,106 patent/US8580825B2/en active Active
- 2011-09-20 EP EP11761774.6A patent/EP2619196B1/en active Active
- 2011-09-20 WO PCT/US2011/052252 patent/WO2012040137A1/en not_active Ceased
- 2011-09-20 JP JP2013530220A patent/JP5828188B2/ja active Active
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