JP2013534245A5 - - Google Patents
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- Publication number
- JP2013534245A5 JP2013534245A5 JP2013524874A JP2013524874A JP2013534245A5 JP 2013534245 A5 JP2013534245 A5 JP 2013534245A5 JP 2013524874 A JP2013524874 A JP 2013524874A JP 2013524874 A JP2013524874 A JP 2013524874A JP 2013534245 A5 JP2013534245 A5 JP 2013534245A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- optionally substituted
- independently
- pharmaceutically acceptable
- acceptable salt
- 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 49
- -1 —O-benzyl Chemical group 0.000 claims 24
- 150000001875 compounds Chemical class 0.000 claims 23
- 150000003839 salts Chemical class 0.000 claims 23
- 229910052739 hydrogen Inorganic materials 0.000 claims 20
- 239000001257 hydrogen Substances 0.000 claims 20
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 20
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 17
- 125000003545 alkoxy group Chemical group 0.000 claims 16
- 150000002431 hydrogen Chemical class 0.000 claims 14
- 125000000623 heterocyclic group Chemical group 0.000 claims 13
- 229910052736 halogen Inorganic materials 0.000 claims 12
- 150000002367 halogens Chemical class 0.000 claims 11
- 125000004043 oxo group Chemical group O=* 0.000 claims 11
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 10
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 10
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 9
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 9
- 125000002757 morpholinyl group Chemical group 0.000 claims 8
- 125000004193 piperazinyl group Chemical group 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 125000003386 piperidinyl group Chemical group 0.000 claims 6
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 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
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 6
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 5
- 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 5
- 125000004663 dialkyl amino group Chemical group 0.000 claims 5
- 150000002617 leukotrienes Chemical class 0.000 claims 5
- 230000001404 mediated effect Effects 0.000 claims 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 4
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 125000002883 imidazolyl group Chemical group 0.000 claims 4
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims 4
- 125000003226 pyrazolyl group Chemical group 0.000 claims 4
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 4
- 125000000335 thiazolyl group Chemical group 0.000 claims 4
- 125000003282 alkyl amino group Chemical group 0.000 claims 3
- 125000002393 azetidinyl group Chemical group 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
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 3
- 125000000842 isoxazolyl group Chemical group 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 3
- 125000002971 oxazolyl group Chemical group 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 3
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 2
- 206010038389 Renal cancer Diseases 0.000 claims 2
- 208000026935 allergic disease Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 230000003176 fibrotic effect Effects 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000002541 furyl group Chemical group 0.000 claims 2
- 208000027866 inflammatory disease Diseases 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
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 208000017169 kidney disease Diseases 0.000 claims 2
- 150000002825 nitriles Chemical class 0.000 claims 2
- 125000003566 oxetanyl group Chemical group 0.000 claims 2
- 125000000168 pyrrolyl 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
- 125000006559 (C1-C3) alkylamino group Chemical group 0.000 claims 1
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000019693 Lung disease Diseases 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 125000001246 bromo group Chemical group Br* 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 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
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 239000000203 mixture Substances 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
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 229910052717 sulfur Chemical group 0.000 claims 1
- 239000011593 sulfur Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 0 *C(*)(c1n[o]c(*)n1)c1ccc(*)cc1* Chemical compound *C(*)(c1n[o]c(*)n1)c1ccc(*)cc1* 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US37392510P | 2010-08-16 | 2010-08-16 | |
| US61/373,925 | 2010-08-16 | ||
| US201161492176P | 2011-06-01 | 2011-06-01 | |
| US61/492,176 | 2011-06-01 | ||
| PCT/US2011/047356 WO2012024150A1 (en) | 2010-08-16 | 2011-08-11 | Oxadiazole inhibitors of leukotriene production |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013534245A JP2013534245A (ja) | 2013-09-02 |
| JP2013534245A5 true JP2013534245A5 (enExample) | 2014-01-09 |
| JP5619284B2 JP5619284B2 (ja) | 2014-11-05 |
Family
ID=44511591
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013524874A Active JP5619284B2 (ja) | 2010-08-16 | 2011-08-11 | ロイコトリエン産生のオキサジアゾール阻害薬 |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US8658661B2 (enExample) |
| EP (1) | EP2606045B1 (enExample) |
| JP (1) | JP5619284B2 (enExample) |
| KR (1) | KR20130100105A (enExample) |
| CN (1) | CN103180314A (enExample) |
| AP (1) | AP2013006678A0 (enExample) |
| AR (1) | AR082696A1 (enExample) |
| AU (1) | AU2011292285A1 (enExample) |
| BR (1) | BR112013003439A2 (enExample) |
| CA (1) | CA2807364A1 (enExample) |
| CL (1) | CL2013000455A1 (enExample) |
| CO (1) | CO6680645A2 (enExample) |
| EA (1) | EA201300250A1 (enExample) |
| EC (1) | ECSP13012494A (enExample) |
| MX (1) | MX2013001872A (enExample) |
| NZ (1) | NZ605690A (enExample) |
| PE (1) | PE20130751A1 (enExample) |
| PH (1) | PH12013500301A1 (enExample) |
| SG (1) | SG187549A1 (enExample) |
| TW (1) | TW201238947A (enExample) |
| UY (1) | UY33557A (enExample) |
| WO (1) | WO2012024150A1 (enExample) |
| ZA (1) | ZA201300238B (enExample) |
Families Citing this family (19)
| 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 |
| EP2651930B1 (en) * | 2010-12-16 | 2015-10-28 | Boehringer Ingelheim International GmbH | Biarylamide inhibitors of leukotriene production |
| US9199904B2 (en) * | 2011-03-18 | 2015-12-01 | Boehringer Ingelheim International Gmbh | Process for preparing carboxylic acids |
| WO2013116182A1 (en) * | 2012-01-31 | 2013-08-08 | Boehringer Ingelheim International Gmbh | Heterocyclic compounds as inhibitors of leukotriene production |
| 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 |
| US9029592B2 (en) * | 2012-02-09 | 2015-05-12 | Boehringer Ingelheim International Gmbh | Process for preparing carboxamidine compounds |
| WO2014095249A1 (en) | 2012-12-19 | 2014-06-26 | Basf Se | Fungicidal imidazolyl and triazolyl compounds |
| WO2014095381A1 (en) | 2012-12-19 | 2014-06-26 | Basf Se | Fungicidal imidazolyl and triazolyl compounds |
| EP2746256A1 (en) | 2012-12-19 | 2014-06-25 | Basf Se | Fungicidal imidazolyl and triazolyl compounds |
| EP2746279A1 (en) | 2012-12-19 | 2014-06-25 | Basf Se | Fungicidal imidazolyl and triazolyl compounds |
| EP2746277A1 (en) | 2012-12-19 | 2014-06-25 | Basf Se | Fungicidal imidazolyl and triazolyl compounds |
| CN103724279B (zh) * | 2014-01-20 | 2016-04-06 | 新发药业有限公司 | 一步成环制备2-甲基-4-氨基-5-氨基甲基嘧啶的便捷合成方法 |
| EP3119774A1 (en) * | 2014-03-17 | 2017-01-25 | reMynd NV | Oxadiazole compounds |
| IL291418B2 (en) | 2022-03-16 | 2024-05-01 | Anima Biotech Inc | Substances that function as modulators of cMYC-mRNA translation and their uses for cancer treatment |
| JP7805983B2 (ja) | 2022-03-22 | 2026-01-26 | アッヴィ・インコーポレイテッド | ブルトン型チロシンキナーゼを分解するためのピリミジン |
| CN119330887B (zh) * | 2024-10-18 | 2026-04-28 | 上海锐谱医药科技有限公司 | 一种一锅法制备药物砌块5-溴-4-氟嘧啶-2-胺的方法 |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3141019A (en) * | 1964-07-14 | Chaohj | ||
| NL302339A (enExample) * | 1963-03-22 | |||
| JP2719742B2 (ja) * | 1991-04-30 | 1998-02-25 | 株式会社大塚製薬工場 | フェニルチアゾール誘導体 |
| IL133916A0 (en) * | 1997-07-10 | 2001-04-30 | Janssen Pharmaceutica Nv | Il-5 inhibiting 6-azauracil derivatives |
| EP0987265A1 (en) * | 1998-09-18 | 2000-03-22 | Janssen Pharmaceutica N.V. | Interleukin-5 inhibiting 6-azauracil derivatives |
| 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 |
| GB0516464D0 (en) * | 2005-08-10 | 2005-09-14 | Smithkline Beecham Corp | Novel compounds |
| 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 |
| GB2431927B (en) * | 2005-11-04 | 2010-03-17 | 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 |
| EP2013174B1 (en) | 2006-04-11 | 2013-05-08 | Merck Sharp & Dohme Corp. | Diaryl substituted alkanes |
| WO2007130499A2 (en) * | 2006-05-01 | 2007-11-15 | Virobay, Inc. | Antiviral agents |
| 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 |
| FR2906866A1 (fr) * | 2006-10-10 | 2008-04-11 | Felix Ifrah | Luminaire comprenant au moins un moyen d'eclairage dont l'activation s'effectue par l'emission d'un rayonnement lumineux |
| 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 |
| 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 |
-
2011
- 2011-08-11 AU AU2011292285A patent/AU2011292285A1/en not_active Abandoned
- 2011-08-11 EP EP11748842.9A patent/EP2606045B1/en active Active
- 2011-08-11 CN CN2011800500399A patent/CN103180314A/zh active Pending
- 2011-08-11 WO PCT/US2011/047356 patent/WO2012024150A1/en not_active Ceased
- 2011-08-11 EA EA201300250A patent/EA201300250A1/ru unknown
- 2011-08-11 AP AP2013006678A patent/AP2013006678A0/xx unknown
- 2011-08-11 PE PE2013000279A patent/PE20130751A1/es not_active Application Discontinuation
- 2011-08-11 BR BR112013003439A patent/BR112013003439A2/pt not_active IP Right Cessation
- 2011-08-11 KR KR1020137003938A patent/KR20130100105A/ko not_active Withdrawn
- 2011-08-11 NZ NZ605690A patent/NZ605690A/en not_active IP Right Cessation
- 2011-08-11 PH PH1/2013/500301A patent/PH12013500301A1/en unknown
- 2011-08-11 SG SG2013003694A patent/SG187549A1/en unknown
- 2011-08-11 CA CA2807364A patent/CA2807364A1/en not_active Abandoned
- 2011-08-11 JP JP2013524874A patent/JP5619284B2/ja active Active
- 2011-08-11 MX MX2013001872A patent/MX2013001872A/es not_active Application Discontinuation
- 2011-08-12 US US13/208,582 patent/US8658661B2/en active Active
- 2011-08-15 TW TW100129127A patent/TW201238947A/zh unknown
- 2011-08-15 AR ARP110102966A patent/AR082696A1/es unknown
- 2011-08-15 UY UY0001033557A patent/UY33557A/es not_active Application Discontinuation
-
2013
- 2013-01-10 ZA ZA2013/00238A patent/ZA201300238B/en unknown
- 2013-02-14 CL CL2013000455A patent/CL2013000455A1/es unknown
- 2013-02-15 CO CO13031460A patent/CO6680645A2/es not_active Application Discontinuation
- 2013-03-15 EC ECSP13012494 patent/ECSP13012494A/es unknown
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