ES2553345T3 - Nuevos derivados de tiofeno como agonistas del receptor S1P1/EDG1 - Google Patents
Nuevos derivados de tiofeno como agonistas del receptor S1P1/EDG1 Download PDFInfo
- Publication number
- ES2553345T3 ES2553345T3 ES07700562T ES07700562T ES2553345T3 ES 2553345 T3 ES2553345 T3 ES 2553345T3 ES 07700562 T ES07700562 T ES 07700562T ES 07700562 T ES07700562 T ES 07700562T ES 2553345 T3 ES2553345 T3 ES 2553345T3
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- Spain
- Prior art keywords
- hydroxy
- 4alkyl
- ethyl
- represents hydrogen
- och2
- 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.)
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- 150000003577 thiophenes Chemical class 0.000 title abstract 2
- 102100025750 Sphingosine 1-phosphate receptor 1 Human genes 0.000 title 2
- 101001021281 Homo sapiens Protein HEXIM1 Proteins 0.000 title 1
- 101000693265 Homo sapiens Sphingosine 1-phosphate receptor 1 Proteins 0.000 title 1
- 101710155454 Sphingosine 1-phosphate receptor 1 Proteins 0.000 title 1
- 239000000018 receptor agonist Substances 0.000 title 1
- 229940044601 receptor agonist Drugs 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 9
- 239000001257 hydrogen Substances 0.000 abstract 9
- 150000002431 hydrogen Chemical group 0.000 abstract 7
- -1 2,3-dihydroxypropyl Chemical group 0.000 abstract 6
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- 229910052736 halogen Chemical group 0.000 abstract 3
- 150000002367 halogens Chemical group 0.000 abstract 3
- 125000000022 2-aminoethyl group Chemical group [H]C([*])([H])C([H])([H])N([H])[H] 0.000 abstract 2
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 abstract 2
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- 125000000143 2-carboxyethyl group Chemical group [H]OC(=O)C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 abstract 1
- QOXOZONBQWIKDA-UHFFFAOYSA-N 3-hydroxypropyl Chemical group [CH2]CCO QOXOZONBQWIKDA-UHFFFAOYSA-N 0.000 abstract 1
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical group C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000006231 alkoxy propyl group Chemical group 0.000 abstract 1
- 125000004848 alkoxyethyl group Chemical group 0.000 abstract 1
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 abstract 1
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 abstract 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 abstract 1
- 125000006222 dimethylaminomethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])* 0.000 abstract 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 abstract 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 125000006533 methyl amino methyl group Chemical group [H]N(C([H])([H])[H])C([H])([H])* 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
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Applications Claiming Priority (3)
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| WOPCT/IB2006/050103 | 2006-01-11 | ||
| IB2006050103 | 2006-01-11 | ||
| PCT/IB2007/050070 WO2007080542A1 (en) | 2006-01-11 | 2007-01-10 | Novel thiophene derivatives as s1p1/edg1 receptor agonists |
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| ES2553345T3 true ES2553345T3 (es) | 2015-12-07 |
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| AU (1) | AU2007204121B2 (enExample) |
| BR (1) | BRPI0706476A2 (enExample) |
| CA (1) | CA2635047C (enExample) |
| ES (1) | ES2553345T3 (enExample) |
| IL (1) | IL192657A (enExample) |
| MY (1) | MY154909A (enExample) |
| NO (1) | NO20083462L (enExample) |
| NZ (1) | NZ570258A (enExample) |
| RU (1) | RU2437877C2 (enExample) |
| TW (1) | TWI404706B (enExample) |
| WO (1) | WO2007080542A1 (enExample) |
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| AU2007292992B2 (en) * | 2006-09-08 | 2013-01-10 | Actelion Pharmaceuticals Ltd | Pyridin-3-yl derivatives as immunomodulating agents |
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| EP2217594B1 (en) * | 2007-11-01 | 2014-01-08 | Actelion Pharmaceuticals Ltd. | Novel pyrimidine derivatives |
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| CA2714665A1 (en) * | 2008-03-06 | 2009-09-11 | Actelion Pharmaceuticals Ltd | Pyridine compounds |
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| CA2715317A1 (en) * | 2008-03-07 | 2009-09-11 | Actelion Pharmaceuticals Ltd | Novel aminomethyl benzene derivatives |
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| US8580841B2 (en) | 2008-07-23 | 2013-11-12 | Arena Pharmaceuticals, Inc. | Substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives useful in the treatment of autoimmune and inflammatory disorders |
| EP2342205B1 (en) | 2008-08-27 | 2016-04-20 | Arena Pharmaceuticals, Inc. | Substituted tricyclic acid derivatives as s1p1 receptor agonists useful in the treatment of autoimmune and inflammatory disorders |
| WO2011007324A1 (en) * | 2009-07-16 | 2011-01-20 | Actelion Pharmaceuticals Ltd | Pyridin-4-yl derivatives |
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| EP4148045A1 (en) | 2010-01-27 | 2023-03-15 | Arena Pharmaceuticals, Inc. | Intermediate compounds for the preparation of (r)-2-(7-(4-cyclopentyl-3- (trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b] indol-3-yl)acetic acid and salts thereof |
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| WO2011133734A1 (en) | 2010-04-23 | 2011-10-27 | Bristol-Myers Squibb Company | 4 - (5 - isoxazolyl or 5 - pyrrazolyl -1,2,4- oxadiazol - 3 - yl) -mandelic acid amides as sphingosin- 1 - phosphate 1 rreceptor agonists |
| TW201206429A (en) * | 2010-07-08 | 2012-02-16 | Merck Serono Sa | Substituted oxadiazole derivatives |
| US9187437B2 (en) | 2010-09-24 | 2015-11-17 | Bristol-Myers Squibb Company | Substituted oxadiazole compounds |
| UA109804C2 (xx) | 2011-01-19 | 2015-10-12 | 2-метоксипіридин-4-ільні похідні | |
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| US10111841B2 (en) | 2015-06-19 | 2018-10-30 | University Of South Florida | Stabilization of alcohol intoxication-induced cardiovascular instability |
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| WO2018151834A1 (en) | 2017-02-16 | 2018-08-23 | Arena Pharmaceuticals, Inc. | Compounds and methods for treatment of inflammatory bowel disease with extra-intestinal manifestations |
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| CN119751336A (zh) | 2018-09-06 | 2025-04-04 | 艾尼纳制药公司 | 可用于治疗自身免疫性病症和炎性病症的化合物 |
| US11014897B1 (en) | 2018-10-16 | 2021-05-25 | Celgene Corporation | Solid forms comprising a thiazolidinone compound, compositions and methods of use thereof |
| US11013723B1 (en) | 2018-10-16 | 2021-05-25 | Celgene Corporation | Solid forms of a thiazolidinone compound, compositions and methods of use thereof |
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| WO1991015583A1 (en) | 1990-04-05 | 1991-10-17 | The American National Red Cross | A protein family related to immediate-early protein expressed by human endothelial cells during differentiation |
| DE19643037A1 (de) * | 1996-10-18 | 1998-04-23 | Boehringer Ingelheim Kg | Neue Oxadiazole, Verfahren zu ihrer Herstellung sowie deren Verwendung als Arzneimittel |
| WO1999046277A1 (en) | 1998-03-09 | 1999-09-16 | Smithkline Beecham Corporation | HUMAN EDG-1c POLYNUCLEOTIDES AND POLYPEPTIDES AND METHODS OF USE |
| RU2233839C1 (ru) * | 2000-07-13 | 2004-08-10 | Санкио Компани, Лимитед | Производные аминоспиртов, фармацевтическая композиция, способ профилактики или лечения, промежуточные соединения и способ получения промежуточных соединений |
| ATE448193T1 (de) * | 2002-01-18 | 2009-11-15 | Merck & Co Inc | ßN-(BENZYL)AMINOALKYL CARBOXYLATE, PHOSPHINATE, PHOSPHONATE UND TETRAZOLE ALS EDG REZEPTORAGONISTENß |
| CA2472680A1 (en) * | 2002-01-18 | 2003-07-31 | Merck & Co., Inc. | Selective s1p1/edg1 receptor agonists |
| ATE441654T1 (de) | 2002-01-18 | 2009-09-15 | Merck & Co Inc | Edg-rezeptoragonisten |
| CA2488117A1 (en) | 2002-06-17 | 2003-12-24 | Merck & Co., Inc. | 1-((5-aryl-1,2,4-oxadiazol-3-yl)benzyl)azetidine-3-carboxylates and 1-((5-aryl-1,2,4-oxadiazol-3-yl)benzyl)pyrrolidine-3-carboxylates as edg receptor agonists |
| WO2004035538A1 (en) | 2002-10-15 | 2004-04-29 | Merck & Co., Inc. | Process for making azetidine-3-carboxylic acid |
| JP2006528980A (ja) | 2003-05-15 | 2006-12-28 | メルク エンド カムパニー インコーポレーテッド | S1p受容体作働薬としての3−(2−アミノ−1−アザシクロ)−5−アリール−1,2,4−オキサジアゾール類 |
| WO2005014525A2 (en) * | 2003-08-12 | 2005-02-17 | Mitsubishi Pharma Corporation | Bi-aryl compound having immunosuppressive activity |
| AU2004277947A1 (en) | 2003-10-01 | 2005-04-14 | Merck & Co., Inc. | 3,5-aryl, heteroaryl or cycloalkyl substituted-1,2,4-oxadiazoles as S1P receptor agonists |
| AU2004299456B2 (en) | 2003-12-17 | 2010-10-07 | Merck Sharp & Dohme Corp. | (3,4-disubstituted)propanoic carboxylates as S1P (Edg) receptor agonists |
| US8039674B2 (en) * | 2004-06-23 | 2011-10-18 | Ono Pharmaceutical Co., Ltd. | Compound having S1P receptor binding potency and use thereof |
| WO2006010379A1 (en) * | 2004-07-29 | 2006-02-02 | Actelion Pharmaceuticals Ltd. | Novel thiophene derivatives as immunosuppressive agents |
| ATE413874T1 (de) * | 2005-03-23 | 2008-11-15 | Actelion Pharmaceuticals Ltd | Neue thiophen-derivate als sphingosin-1-phosphat- 1-rezeptorantagonisten |
| US7846964B2 (en) * | 2005-03-23 | 2010-12-07 | Actelion Pharmaceuticals Ltd. | Thiophene derivatives as spingosine-1-phosphate-1 receptor agonists |
| WO2006100631A1 (en) * | 2005-03-23 | 2006-09-28 | Actelion Pharmaceuticals Ltd | Hydrogenated benzo (c) thiophene derivatives as immunomodulators |
| WO2006131336A1 (en) | 2005-06-08 | 2006-12-14 | Novartis Ag | POLYCYCLIC OXADIAZOLES OR I SOXAZOLES AND THEIR USE AS SlP RECEPTOR LIGANDS |
| BRPI0611631A2 (pt) * | 2005-06-24 | 2010-09-21 | Actelion Pharmaceuticals Ltd | composto, composição farmacêutica, e, uso de um composto |
| GB0601744D0 (en) | 2006-01-27 | 2006-03-08 | Novartis Ag | Organic compounds |
| MX2009006304A (es) | 2006-12-15 | 2009-06-23 | Abbott Lab | Nuevos compuestos de oxadiazol. |
| WO2008091967A1 (en) | 2007-01-26 | 2008-07-31 | Smithkline Beecham Corporation | Chemical compounds |
| MX2010005889A (es) * | 2007-12-10 | 2010-06-22 | Actelion Pharmaceuticals Ltd | Derivados de tiofeno como agonistas de s1p1/edg1. |
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2007
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- 2007-01-09 AR ARP070100083A patent/AR058956A1/es unknown
- 2007-01-10 MY MYPI20082557A patent/MY154909A/en unknown
- 2007-01-10 ES ES07700562T patent/ES2553345T3/es active Active
- 2007-01-10 US US12/160,520 patent/US8003800B2/en not_active Expired - Fee Related
- 2007-01-10 AU AU2007204121A patent/AU2007204121B2/en not_active Ceased
- 2007-01-10 BR BRPI0706476-4A patent/BRPI0706476A2/pt not_active IP Right Cessation
- 2007-01-10 WO PCT/IB2007/050070 patent/WO2007080542A1/en not_active Ceased
- 2007-01-10 KR KR1020087018081A patent/KR101382710B1/ko not_active Expired - Fee Related
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- 2007-01-10 JP JP2008549960A patent/JP5114430B2/ja not_active Expired - Fee Related
- 2007-01-10 NZ NZ570258A patent/NZ570258A/en not_active IP Right Cessation
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- 2007-01-10 CN CN2007800022066A patent/CN101370496B/zh not_active Expired - Fee Related
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Also Published As
| Publication number | Publication date |
|---|---|
| AR058956A1 (es) | 2008-03-05 |
| CA2635047A1 (en) | 2007-07-19 |
| KR101382710B1 (ko) | 2014-04-08 |
| CA2635047C (en) | 2014-07-29 |
| NO20083462L (no) | 2008-10-09 |
| CN101370496A (zh) | 2009-02-18 |
| RU2437877C2 (ru) | 2011-12-27 |
| EP1976512B1 (en) | 2015-09-30 |
| NZ570258A (en) | 2011-07-29 |
| MY154909A (en) | 2015-08-28 |
| JP2009523165A (ja) | 2009-06-18 |
| TWI404706B (zh) | 2013-08-11 |
| RU2008132802A (ru) | 2010-02-20 |
| AU2007204121B2 (en) | 2012-06-07 |
| WO2007080542A1 (en) | 2007-07-19 |
| CN101370496B (zh) | 2012-07-04 |
| BRPI0706476A2 (pt) | 2011-04-05 |
| US8003800B2 (en) | 2011-08-23 |
| IL192657A (en) | 2015-09-24 |
| EP1976512A1 (en) | 2008-10-08 |
| KR20080083010A (ko) | 2008-09-12 |
| AU2007204121A1 (en) | 2007-07-19 |
| IL192657A0 (en) | 2009-02-11 |
| US20100240717A1 (en) | 2010-09-23 |
| TW200804298A (en) | 2008-01-16 |
| JP5114430B2 (ja) | 2013-01-09 |
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