AR058956A1 - Derivados de tiofeno agonistas de receptores s1p1/edg1, composiciones farmaceuticas que los contienen y usos como agentes inmunomoduladores. - Google Patents
Derivados de tiofeno agonistas de receptores s1p1/edg1, composiciones farmaceuticas que los contienen y usos como agentes inmunomoduladores.Info
- Publication number
- AR058956A1 AR058956A1 ARP070100083A ARP070100083A AR058956A1 AR 058956 A1 AR058956 A1 AR 058956A1 AR P070100083 A ARP070100083 A AR P070100083A AR P070100083 A ARP070100083 A AR P070100083A AR 058956 A1 AR058956 A1 AR 058956A1
- Authority
- AR
- Argentina
- Prior art keywords
- hydroxy
- ethyl
- alkyl
- represents hydrogen
- och2
- Prior art date
Links
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical class C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 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
- 239000000556 agonist Substances 0.000 title 1
- 239000002955 immunomodulating agent Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 9
- 239000001257 hydrogen Substances 0.000 abstract 9
- -1 2,3-dihydroxypropyl Chemical group 0.000 abstract 7
- 150000002431 hydrogen Chemical group 0.000 abstract 7
- 125000004178 (C1-C4) alkyl group 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
- 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
- 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
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000005157 alkyl carboxy group Chemical group 0.000 abstract 1
- 125000000217 alkyl 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
- 125000005113 hydroxyalkoxy group Chemical group 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
- 150000003577 thiophenes Chemical class 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- 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
- C07D333/22—Radicals substituted by doubly bound hetero atoms, or by two hetero atoms other than halogen singly bound to the same carbon atom
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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| AU2007292992B2 (en) * | 2006-09-08 | 2013-01-10 | Actelion Pharmaceuticals Ltd | Pyridin-3-yl derivatives as immunomodulating agents |
| MX2009006304A (es) | 2006-12-15 | 2009-06-23 | Abbott Lab | Nuevos compuestos de oxadiazol. |
| SI2125797T1 (sl) * | 2007-03-16 | 2014-03-31 | Actelion Pharmaceuticals Ltd. | Derivati amino-piridina kot agonisti receptorja s1p1/edg1 |
| PE20090305A1 (es) * | 2007-05-22 | 2009-03-15 | Wyeth Corp | Proceso mejorado para la elaboracion de hidrazidas |
| ES2361463T3 (es) * | 2007-08-17 | 2011-06-17 | Actelion Pharmaceuticals Ltd. | Derivados de piridina como moduladores del receptor s1p1/edg1. |
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| EP2217594B1 (en) * | 2007-11-01 | 2014-01-08 | Actelion Pharmaceuticals Ltd. | Novel pyrimidine derivatives |
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| CA2715317A1 (en) * | 2008-03-07 | 2009-09-11 | Actelion Pharmaceuticals Ltd | Novel aminomethyl benzene derivatives |
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| WO2011007324A1 (en) * | 2009-07-16 | 2011-01-20 | Actelion Pharmaceuticals Ltd | Pyridin-4-yl derivatives |
| US8399451B2 (en) | 2009-08-07 | 2013-03-19 | Bristol-Myers Squibb Company | Heterocyclic compounds |
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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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| US10111841B2 (en) | 2015-06-19 | 2018-10-30 | University Of South Florida | Stabilization of alcohol intoxication-induced cardiovascular instability |
| CA3002551A1 (en) | 2015-06-22 | 2016-12-29 | Arena Pharmaceuticals, Inc. | Crystalline l-arginine salt of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid(com pound 1)for use in s1p1 receptor-associated disorders |
| 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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| CA3102136A1 (en) | 2018-06-06 | 2019-12-12 | Arena Pharmaceuticals, Inc. | Methods of treating conditions related to the s1p1 receptor |
| 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 |
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| 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 |
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| 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 |
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| 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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- 2007-01-10 ES ES07700562T patent/ES2553345T3/es active Active
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- 2007-01-10 BR BRPI0706476-4A patent/BRPI0706476A2/pt not_active IP Right Cessation
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Also Published As
| Publication number | Publication date |
|---|---|
| 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 |
| ES2553345T3 (es) | 2015-12-07 |
| US20100240717A1 (en) | 2010-09-23 |
| TW200804298A (en) | 2008-01-16 |
| JP5114430B2 (ja) | 2013-01-09 |
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