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 |
| NZ586735A (en) | 2007-12-18 | 2012-06-29 | Actelion Pharmaceuticals Ltd | Aminotriazole derivatives as alx agonists |
| SG176137A1 (en) | 2009-05-18 | 2011-12-29 | Actelion Pharmaceuticals Ltd | Bridged spiro [2.4] heptane derivatives as alx receptor and/or fprl2 agonists |
| US8674111B2 (en) | 2009-06-12 | 2014-03-18 | Actelion Pharmaceuticals Ltd. | Oxazole and thiazole derivatives as ALX receptor agonists |
| CN103221392B (zh) | 2010-11-17 | 2015-06-03 | 埃科特莱茵药品有限公司 | 桥联螺[2.4]庚酯衍生物 |
| CN103249413B (zh) * | 2010-12-07 | 2015-11-25 | 埃科特莱茵药品有限公司 | 作为脂氧素(alx)受体激动剂的羟基化氨基三唑衍生物 |
| CN103261194B (zh) | 2010-12-07 | 2016-02-24 | 埃科特莱茵药品有限公司 | 作为alx受体激动剂的噁唑基-甲醚衍生物 |
| WO2013171687A1 (en) | 2012-05-16 | 2013-11-21 | Actelion Pharmaceuticals Ltd | 1-(p-tolyl)cyclopropyl substituted bridged spiro[2.4]heptane derivatives as alx receptor agonists |
| 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 |
| JP6244365B2 (ja) | 2012-10-10 | 2017-12-06 | アクテリオン ファーマシューティカルズ リミテッドＡｃｔｅｌｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｌｔｄ | ［オルトビ−（ヘテロ−）アリール］−［２−（メタビ−（ヘテロ−）アリール）−ピロリジン−１−イル］−メタノン誘導体であるオレキシン受容体アンタゴニスト |
| EP2970241A1 (en) | 2013-03-12 | 2016-01-20 | Actelion Pharmaceuticals Ltd. | Azetidine amide derivatives as orexin receptor antagonists |
| US10370451B2 (en) | 2013-04-22 | 2019-08-06 | The University Of Tokyo | Preventive or therapeutic agent for inflammatory disease |
| 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 |
| KR20160033747A (ko) | 2013-07-18 | 2016-03-28 | 액테리온 파마슈티칼 리미티드 | Ａｌｘ 수용체 아고니스트로서의 피페라진 치환된 브릿지연결 스피로［２．４］헵탄 유도체 |
| AR097279A1 (es) | 2013-08-09 | 2016-03-02 | Actelion Pharmaceuticals Ltd | Derivados de benzimidazolil-metil urea como agonistas del receptor de alx |
| LT3077391T (lt) | 2013-12-04 | 2018-10-25 | Idorsia Pharmaceuticals Ltd | Benzimidazolo prolino darinių panaudojimas |
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 |
| AU2003214249A1 (en) | 2002-04-03 | 2003-10-13 | Bayer Aktiengesellschaft | Diagnostics and therapeutics for diseases associated with n-formyl peptide receptor like 1 (fprl1) |
| CL2003002353A1 (es) * | 2002-11-15 | 2005-02-04 | Vertex Pharma | Compuestos derivados de diaminotriazoles, inhibidores d ela proteina quinasa; composicion farmaceutica; procedimiento de preparacion; y su uso del compuesto en el tratamiento de enfermedades de desordenes alergicos, proliferacion, autoinmunes, condic |
| BRPI0416272A (pt) | 2003-11-07 | 2007-01-09 | Acadia Pharm Inc | usos do receptor fprl1, e de compostos, uso profilático de compostos, métodos de triagem para um composto capaz de afetar uma ou mais atividades de um receptor fprl1, de tratamento ou prevenção de inflamação, de identificação de um composto de indução de vasodilatação, para antagonismo de uma resposta vasoconstrutiva a um sulfidopeptìdeo leucotrieno em um indivìduo, e para estimulação de proliferação celular em um indivìduo, e, composto |
| AU2005247473A1 (en) * | 2004-05-25 | 2005-12-08 | Metabolex, Inc. | Substituted triazoles as modulators of PPAR and methods of their preparation |
| PT1791830E (pt) * | 2004-09-17 | 2011-04-04 | Vertex Pharma | Compostos de diaminotriazole úteis como inibidores de proteína-quinase |
| US20060293288A1 (en) | 2005-01-07 | 2006-12-28 | Serhan Charles N | Use of resolvins to treat gastrointestinal diseases |
| AU2006312083A1 (en) * | 2005-11-03 | 2007-05-18 | Merck Sharp & Dohme Corp. | Histone deacetylase inhibitors with aryl-pyrazolyl motifs |
| ES2545121T3 (es) | 2007-08-21 | 2015-09-08 | Senomyx, Inc. | Compuestos que inhiben (bloquean) el sabor amargo en composiciones, y uso de los mismos |
| AR069650A1 (es) | 2007-12-14 | 2010-02-10 | Actelion Pharmaceuticals Ltd | Derivados de aminopirazol como agonistas no peptidicos del receptor alx humano |
| NZ586735A (en) | 2007-12-18 | 2012-06-29 | Actelion Pharmaceuticals Ltd | Aminotriazole derivatives as alx agonists |
| SG176137A1 (en) | 2009-05-18 | 2011-12-29 | Actelion Pharmaceuticals Ltd | Bridged spiro [2.4] heptane derivatives as alx receptor and/or fprl2 agonists |
| US8674111B2 (en) | 2009-06-12 | 2014-03-18 | Actelion Pharmaceuticals Ltd. | Oxazole and thiazole derivatives as ALX receptor agonists |
-
2010
- 2010-06-07 RU RU2011153772/04A patent/RU2544862C2/ru not_active IP Right Cessation
- 2010-06-07 WO PCT/IB2010/052509 patent/WO2010143116A1/en not_active Ceased
- 2010-06-07 MX MX2011012739A patent/MX342440B/es active IP Right Grant
- 2010-06-07 MY MYPI2011005927A patent/MY161243A/en unknown
- 2010-06-07 JP JP2012514570A patent/JP5095035B2/ja 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 KR KR1020127000486A patent/KR101444559B1/ko not_active Expired - Fee Related
- 2010-06-07 CA CA2760588A patent/CA2760588C/en not_active Expired - Fee Related
- 2010-06-07 PL PL10725500.2T patent/PL2440555T3/pl unknown
- 2010-06-07 CN CN201080018293.6A patent/CN102414207B/zh not_active Expired - Fee Related
- 2010-06-07 EP EP10725500.2A patent/EP2440555B1/en not_active Not-in-force
- 2010-06-07 BR BRPI1010738A patent/BRPI1010738A8/pt not_active Application Discontinuation
- 2010-06-07 US US13/376,966 patent/US8580831B2/en not_active Expired - Fee Related
- 2010-06-07 ES ES10725500.2T patent/ES2587139T3/es active Active
- 2010-06-07 AU AU2010258334A patent/AU2010258334B2/en not_active Ceased
- 2010-06-07 NZ NZ597453A patent/NZ597453A/xx not_active IP Right Cessation
- 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