JP2012255002A5 - - Google Patents
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- Publication number
- JP2012255002A5 JP2012255002A5 JP2012171081A JP2012171081A JP2012255002A5 JP 2012255002 A5 JP2012255002 A5 JP 2012255002A5 JP 2012171081 A JP2012171081 A JP 2012171081A JP 2012171081 A JP2012171081 A JP 2012171081A JP 2012255002 A5 JP2012255002 A5 JP 2012255002A5
- Authority
- JP
- Japan
- Prior art keywords
- disease
- methyl
- use according
- ethyl
- compound
- 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
- 230000001363 autoimmune Effects 0.000 claims description 6
- 208000027866 inflammatory disease Diseases 0.000 claims description 5
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 24
- 201000010099 disease Diseases 0.000 claims 22
- 239000003814 drug Substances 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 12
- 125000006002 1,1-difluoroethyl group Chemical group 0.000 claims 10
- 230000001404 mediated effect Effects 0.000 claims 6
- GEAPKHXZFUKEDK-UHFFFAOYSA-N 2-methyl-5-phenyl-1,3-oxazole-4-carboxylic acid Chemical compound O1C(C)=NC(C(O)=O)=C1C1=CC=CC=C1 GEAPKHXZFUKEDK-UHFFFAOYSA-N 0.000 claims 4
- 208000024827 Alzheimer disease Diseases 0.000 claims 4
- 201000003883 Cystic fibrosis Diseases 0.000 claims 4
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 4
- 206010069351 acute lung injury Diseases 0.000 claims 4
- 208000006673 asthma Diseases 0.000 claims 4
- OMCWOZYMSYZUTD-UHFFFAOYSA-N 2-methyl-5-(3-methylphenyl)-1,3-oxazole-4-carboxylic acid Chemical compound O1C(C)=NC(C(O)=O)=C1C1=CC=CC(C)=C1 OMCWOZYMSYZUTD-UHFFFAOYSA-N 0.000 claims 2
- NDFZHVTZGZRQMP-UHFFFAOYSA-N 2-methyl-5-[3-(trifluoromethyl)phenyl]-1,3-oxazole-4-carboxylic acid Chemical compound O1C(C)=NC(C(O)=O)=C1C1=CC=CC(C(F)(F)F)=C1 NDFZHVTZGZRQMP-UHFFFAOYSA-N 0.000 claims 2
- MOFHRDAQQJGDIT-UHFFFAOYSA-N 5-(3-chlorophenyl)-2-methyl-1,3-oxazole-4-carboxylic acid Chemical compound O1C(C)=NC(C(O)=O)=C1C1=CC=CC(Cl)=C1 MOFHRDAQQJGDIT-UHFFFAOYSA-N 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 206010020751 Hypersensitivity Diseases 0.000 claims 2
- 208000036110 Neuroinflammatory disease Diseases 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- 102000029797 Prion Human genes 0.000 claims 2
- 108091000054 Prion Proteins 0.000 claims 2
- 206010038997 Retroviral infections Diseases 0.000 claims 2
- 208000026935 allergic disease Diseases 0.000 claims 2
- 230000007815 allergy Effects 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 230000028993 immune response Effects 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 230000003959 neuroinflammation Effects 0.000 claims 2
- 201000001119 neuropathy Diseases 0.000 claims 2
- 230000007823 neuropathy Effects 0.000 claims 2
- 230000000414 obstructive effect Effects 0.000 claims 2
- 230000036407 pain Effects 0.000 claims 2
- 208000033808 peripheral neuropathy Diseases 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 208000023504 respiratory system disease Diseases 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 230000001105 regulatory effect Effects 0.000 claims 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 208000001204 Hashimoto Disease Diseases 0.000 description 1
- 208000030836 Hashimoto thyroiditis Diseases 0.000 description 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 description 1
- 230000006472 autoimmune response Effects 0.000 description 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IB2009052445 | 2009-06-09 | ||
| IBPCT/IB2009/052445 | 2009-06-09 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012514570A Division JP5095035B2 (ja) | 2009-06-09 | 2010-06-07 | フッ素化アミノトリアゾール誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012255002A JP2012255002A (ja) | 2012-12-27 |
| JP2012255002A5 true JP2012255002A5 (enExample) | 2013-07-18 |
| JP5775496B2 JP5775496B2 (ja) | 2015-09-09 |
Family
ID=42371383
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012514570A Expired - Fee Related JP5095035B2 (ja) | 2009-06-09 | 2010-06-07 | フッ素化アミノトリアゾール誘導体 |
| JP2012171081A Expired - Fee Related JP5775496B2 (ja) | 2009-06-09 | 2012-08-01 | フッ素化アミノトリアゾール誘導体 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012514570A Expired - Fee Related JP5095035B2 (ja) | 2009-06-09 | 2010-06-07 | フッ素化アミノトリアゾール誘導体 |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US8580831B2 (enExample) |
| EP (1) | EP2440555B1 (enExample) |
| JP (2) | JP5095035B2 (enExample) |
| KR (1) | KR101444559B1 (enExample) |
| CN (1) | CN102414207B (enExample) |
| AR (1) | AR077032A1 (enExample) |
| AU (1) | AU2010258334B2 (enExample) |
| BR (1) | BRPI1010738A8 (enExample) |
| CA (1) | CA2760588C (enExample) |
| CL (1) | CL2011003097A1 (enExample) |
| ES (1) | ES2587139T3 (enExample) |
| IL (1) | IL216792A (enExample) |
| MA (1) | MA33420B1 (enExample) |
| MX (1) | MX342440B (enExample) |
| MY (1) | MY161243A (enExample) |
| NZ (1) | NZ597453A (enExample) |
| PL (1) | PL2440555T3 (enExample) |
| RU (1) | RU2544862C2 (enExample) |
| SG (1) | SG175363A1 (enExample) |
| TW (1) | TWI404717B (enExample) |
| WO (1) | WO2010143116A1 (enExample) |
| ZA (1) | ZA201200127B (enExample) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR069650A1 (es) | 2007-12-14 | 2010-02-10 | Actelion Pharmaceuticals Ltd | Derivados de aminopirazol como agonistas no peptidicos del receptor alx humano |
| SI2225231T1 (sl) | 2007-12-18 | 2011-12-30 | Actelion Pharmaceuticals Ltd | Derivati aminotriazola kot alx agonisti |
| JP5510945B2 (ja) | 2009-05-18 | 2014-06-04 | アクテリオン ファーマシューティカルズ リミテッド | Ａｌｘ受容体及び／又はｆｐｒｌ２アゴニストとしての架橋スピロ［２．４］ヘプタン誘導体 |
| WO2010143158A1 (en) | 2009-06-12 | 2010-12-16 | Actelion Pharmaceuticals Ltd | Oxazole and thiazole derivatives as alx receptor agonists |
| ES2553635T3 (es) | 2010-11-17 | 2015-12-10 | Actelion Pharmaceuticals Ltd. | Derivados de éster spiro[2.4]heptano puenteados |
| BR112013014035A2 (pt) * | 2010-12-07 | 2016-09-13 | Actelion Pharmaceuticals Ltd | derivados de aminotriazol hidroxilado como agonistas dos receptores de alx |
| PL2649068T3 (pl) * | 2010-12-07 | 2015-03-31 | Idorsia Pharmaceuticals Ltd | Pochodne eteru oksazolilowo-metylowego jako agoniści receptora ALX |
| ES2596521T3 (es) | 2012-05-16 | 2017-01-10 | Actelion Pharmaceuticals Ltd. | Derivados de espiro[2.4]heptano sustituidos con puente 1-(p-tolil)ciclopropilo como agonistas de receptor de ALX |
| MA37618B1 (fr) | 2012-05-16 | 2017-08-31 | Actelion Pharmaceuticals Ltd | Dérivés pontés fluorés de spiro[2.4]heptane en tant qu'agonistes de récepteur alx |
| PL2855453T3 (pl) | 2012-06-04 | 2017-05-31 | Actelion Pharmaceuticals Ltd. | Pochodne benzimidazoloproliny |
| CN104703980B (zh) | 2012-10-10 | 2017-09-22 | 埃科特莱茵药品有限公司 | 属于[邻双(杂)芳基]‑[2‑(间双(杂)芳基)吡咯烷‑1‑基]甲酮衍生物的食欲素受体拮抗剂 |
| WO2014141065A1 (en) | 2013-03-12 | 2014-09-18 | Actelion Pharmaceuticals Ltd | Azetidine amide derivatives as orexin receptor antagonists |
| JP6366195B2 (ja) | 2013-04-22 | 2018-08-01 | 国立大学法人 東京大学 | 炎症性疾患の予防又は治療剤 |
| AR096686A1 (es) | 2013-06-25 | 2016-01-27 | Actelion Pharmaceuticals Ltd | Derivados de espiro[2.4]heptano puenteados sustituidos con difluoroetil-oxazol como agonistas del receptor de alx |
| CN105377824B (zh) | 2013-07-18 | 2017-08-04 | 埃科特莱茵药品有限公司 | 作为alx受体激动剂的经哌嗪取代桥联螺[2,4]庚烷衍生物 |
| AR097279A1 (es) | 2013-08-09 | 2016-03-02 | Actelion Pharmaceuticals Ltd | Derivados de benzimidazolil-metil urea como agonistas del receptor de alx |
| EP3077391B1 (en) | 2013-12-04 | 2018-08-15 | Idorsia Pharmaceuticals Ltd | Use of benzimidazole-proline derivatives |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS62234018A (ja) | 1986-04-02 | 1987-10-14 | Rooto Seiyaku Kk | 糖尿病併発症治療剤 |
| FR2763337B1 (fr) * | 1997-05-13 | 1999-08-20 | Sanofi Sa | Nouveaux derives du triazole, un procede pour leur preparation et compositions pharmaceutiques les contenant |
| KR20030030029A (ko) | 2000-09-22 | 2003-04-16 | 니혼노야쿠가부시키가이샤 | Ｎ-(4-피라졸릴)아미드 유도체 및 농원예용 약제 그리고그 사용방법 |
| US20050164305A1 (en) | 2002-04-03 | 2005-07-28 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with n-formyl peptide receptor like 1 (fprl1) |
| TWI335913B (en) * | 2002-11-15 | 2011-01-11 | Vertex Pharma | Diaminotriazoles useful as inhibitors of protein kinases |
| CA2544983A1 (en) | 2003-11-07 | 2005-05-26 | Acadia Pharmaceuticals Inc. | Use of the lipoxin receptor, fprl1, as a tool for identifying compounds effective in the treatment of pain and inflammation |
| AU2005247473A1 (en) * | 2004-05-25 | 2005-12-08 | Metabolex, Inc. | Substituted triazoles as modulators of PPAR and methods of their preparation |
| DE602005025655D1 (de) * | 2004-09-17 | 2011-02-10 | Vertex Pharma | Als proteinkinaseinhibitoren geeignete diaminotriazolverbindungen |
| US20060293288A1 (en) | 2005-01-07 | 2006-12-28 | Serhan Charles N | Use of resolvins to treat gastrointestinal diseases |
| WO2007055941A2 (en) * | 2005-11-03 | 2007-05-18 | Merck & Co., Inc. | Histone deacetylase inhibitors with aryl-pyrazolyl motifs |
| US7939671B2 (en) | 2007-08-21 | 2011-05-10 | Senomyx, Inc. | Compounds that inhibit (block) bitter taste in composition and use thereof |
| AR069650A1 (es) | 2007-12-14 | 2010-02-10 | Actelion Pharmaceuticals Ltd | Derivados de aminopirazol como agonistas no peptidicos del receptor alx humano |
| SI2225231T1 (sl) * | 2007-12-18 | 2011-12-30 | Actelion Pharmaceuticals Ltd | Derivati aminotriazola kot alx agonisti |
| JP5510945B2 (ja) | 2009-05-18 | 2014-06-04 | アクテリオン ファーマシューティカルズ リミテッド | Ａｌｘ受容体及び／又はｆｐｒｌ２アゴニストとしての架橋スピロ［２．４］ヘプタン誘導体 |
| WO2010143158A1 (en) | 2009-06-12 | 2010-12-16 | Actelion Pharmaceuticals Ltd | Oxazole and thiazole derivatives as alx receptor agonists |
-
2010
- 2010-06-07 MY MYPI2011005927A patent/MY161243A/en unknown
- 2010-06-07 BR BRPI1010738A patent/BRPI1010738A8/pt not_active Application Discontinuation
- 2010-06-07 MX MX2011012739A patent/MX342440B/es active IP Right Grant
- 2010-06-07 CN CN201080018293.6A patent/CN102414207B/zh not_active Expired - Fee Related
- 2010-06-07 KR KR1020127000486A patent/KR101444559B1/ko not_active Expired - Fee Related
- 2010-06-07 MA MA34521A patent/MA33420B1/fr unknown
- 2010-06-07 SG SG2011078706A patent/SG175363A1/en unknown
- 2010-06-07 RU RU2011153772/04A patent/RU2544862C2/ru not_active IP Right Cessation
- 2010-06-07 PL PL10725500.2T patent/PL2440555T3/pl unknown
- 2010-06-07 WO PCT/IB2010/052509 patent/WO2010143116A1/en not_active Ceased
- 2010-06-07 CA CA2760588A patent/CA2760588C/en not_active Expired - Fee Related
- 2010-06-07 JP JP2012514570A patent/JP5095035B2/ja not_active Expired - Fee Related
- 2010-06-07 ES ES10725500.2T patent/ES2587139T3/es active Active
- 2010-06-07 NZ NZ597453A patent/NZ597453A/xx not_active IP Right Cessation
- 2010-06-07 AU AU2010258334A patent/AU2010258334B2/en not_active Ceased
- 2010-06-07 US US13/376,966 patent/US8580831B2/en not_active Expired - Fee Related
- 2010-06-07 EP EP10725500.2A patent/EP2440555B1/en not_active Not-in-force
- 2010-06-08 TW TW099118594A patent/TWI404717B/zh not_active IP Right Cessation
- 2010-06-09 AR ARP100102022A patent/AR077032A1/es unknown
-
2011
- 2011-12-06 IL IL216792A patent/IL216792A/en not_active IP Right Cessation
- 2011-12-07 CL CL2011003097A patent/CL2011003097A1/es unknown
-
2012
- 2012-01-06 ZA ZA2012/00127A patent/ZA201200127B/en unknown
- 2012-08-01 JP JP2012171081A patent/JP5775496B2/ja not_active Expired - Fee Related