ES2405054T3 - Derivados de pirazol-1,2,4-oxadiazol como agonistas de esfingosina-1-fosfato - Google Patents
Derivados de pirazol-1,2,4-oxadiazol como agonistas de esfingosina-1-fosfato Download PDFInfo
- Publication number
- ES2405054T3 ES2405054T3 ES10701183T ES10701183T ES2405054T3 ES 2405054 T3 ES2405054 T3 ES 2405054T3 ES 10701183 T ES10701183 T ES 10701183T ES 10701183 T ES10701183 T ES 10701183T ES 2405054 T3 ES2405054 T3 ES 2405054T3
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- Prior art keywords
- benzyl
- alkyl
- azetidine
- pyrazol
- phenyl
- Prior art date
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- AZPBLVQAOKGVEO-UHFFFAOYSA-N 1,2,4-oxadiazole;1h-pyrazole Chemical class C=1C=NNC=1.C=1N=CON=1 AZPBLVQAOKGVEO-UHFFFAOYSA-N 0.000 title description 2
- 229940124751 sphingosine-1-phosphate agonist Drugs 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims abstract description 215
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- 150000002367 halogens Chemical class 0.000 claims abstract description 50
- 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 abstract description 45
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract description 43
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract description 42
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims abstract description 41
- 125000001424 substituent group Chemical group 0.000 claims abstract description 39
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- 125000000623 heterocyclic group Chemical group 0.000 claims abstract description 34
- 125000003118 aryl group Chemical group 0.000 claims abstract description 26
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- 239000001257 hydrogen Substances 0.000 claims abstract description 19
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| PCT/US2010/021696 WO2010085584A1 (en) | 2009-01-23 | 2010-01-22 | Pyrazole-i, 2, 4 -oxad iazole derivatives as s.phing0sine-1-ph0sphate agonists |
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| WO (1) | WO2010085584A1 (enExample) |
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| EP2389377B1 (en) | 2009-01-23 | 2014-07-16 | Bristol-Myers Squibb Company | Substituted oxadiazole derivatives as s1p agonists in the treatment of autoimmune and inflammatory diseases |
| JP2012515787A (ja) | 2009-01-23 | 2012-07-12 | ブリストル−マイヤーズ スクイブ カンパニー | 自己免疫疾患および炎症性疾患の処置におけるｓ１ｐアゴニストとしての置換オキサジアゾール誘導体 |
| AR076984A1 (es) * | 2009-06-08 | 2011-07-20 | Merck Serono Sa | Derivados de pirazol oxadiazol |
| US8399451B2 (en) | 2009-08-07 | 2013-03-19 | Bristol-Myers Squibb Company | Heterocyclic compounds |
| BR112012028651A2 (pt) | 2010-05-08 | 2016-08-09 | Bayer Ip Gmbh | heterociclilbenzilpirazóis substituídos e uso do mesmo |
| WO2011141325A1 (de) | 2010-05-08 | 2011-11-17 | Bayer Pharma Aktiengesellschaft | Hydroxyalkylbenzyl- pyrazole und ihre verwendung zur behandlung von hyperproliferativen und angiogenen erkrankungen |
| ES2539256T3 (es) | 2010-07-20 | 2015-06-29 | Bristol-Myers Squibb Company | Compuestos de 3-fenil-1,2,4-oxadiazol sustituidos |
| JP5869579B2 (ja) | 2010-09-24 | 2016-02-24 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | 置換オキサジアゾール化合物およびそれらのｓ１ｐ１アゴニストとしての使用 |
| WO2012061459A1 (en) * | 2010-11-03 | 2012-05-10 | Bristol-Myers Squibb Company | Heterocyclic compounds as s1p1 agonists for the treatment of autoimmune and vascular diseases |
| RU2013130019A (ru) | 2010-12-03 | 2015-01-10 | Аллерган, Инк. | Новые производные азетидина в качестве модуляторов рецептора сфингозин 1-фосфата (s1p) |
| EP2738170B1 (en) | 2011-07-29 | 2017-08-30 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| US8987467B2 (en) | 2013-02-14 | 2015-03-24 | Allergan, Inc. | Substituted pyrazole azetidines as sphingosine receptor modulators |
| WO2014127149A1 (en) * | 2013-02-15 | 2014-08-21 | Allergan, Inc. | Substituted 4,5-dihydropyrazole-1,2,4-oxadiazole derivatives as sphingosine receptor modulators |
| WO2014127141A1 (en) * | 2013-02-15 | 2014-08-21 | Allergan, Inc. | Substituted 1h-pyrazol-1,2,4-oxadiazole derivatives as sphingosine receptor modulators |
| TWI613182B (zh) | 2013-02-21 | 2018-02-01 | 必治妥美雅史谷比公司 | 雙環化合物 |
| TWI689487B (zh) | 2014-08-20 | 2020-04-01 | 美商必治妥美雅史谷比公司 | 經取代雙環化合物 |
| WO2021233882A1 (en) * | 2020-05-22 | 2021-11-25 | Boehringer Ingelheim International Gmbh | Process for manufacturing alkyl 7-amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridine-carboxylate |
| CN113332435B (zh) * | 2021-06-18 | 2022-10-18 | 广州中医药大学(广州中医药研究院) | 鞘氨醇-1-磷酸4受体激动剂及其与真武汤联合在制备治疗慢性肾小球肾炎药物中的应用 |
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| US4200750A (en) | 1977-01-07 | 1980-04-29 | Westwood Pharmaceuticals Inc. | 4-Substituted imidazo [1,2-a]quinoxalines |
| WO2003061567A2 (en) | 2002-01-18 | 2003-07-31 | Merck & Co., Inc. | Selective s1p1/edg1 receptor agonists |
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| AU2003296760B2 (en) | 2002-11-15 | 2009-11-19 | Tibotec Pharmaceuticals Ltd. | Substituted indolepyridinium as anti-infective compounds |
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| EP1625123A4 (en) * | 2003-05-15 | 2007-08-29 | Merck & Co Inc | 3- (2-AMINO-1-AZACYCLYL) -5-ARYL-1,2,4-OXADIAZOLE AS S1P RECEPTOR AGONISTS |
| EP2644195A1 (en) | 2003-05-19 | 2013-10-02 | Irm Llc | Immunosuppressant Compounds and Compositions |
| JP4773972B2 (ja) | 2003-12-17 | 2011-09-14 | メルク・シャープ・エンド・ドーム・コーポレイション | Ｓ１Ｐ（Ｅｄｇ）受容体作働薬としての（３，４−ジ置換）プロパンカルボン酸 |
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| WO2006047195A2 (en) | 2004-10-22 | 2006-05-04 | Merck & Co., Inc. | 2-(aryl)azacyclylmethyl carboxylates, sulfonates, phosphonates, phosphinates and heterocycles as s1p receptor agonists |
| BRPI0607435A2 (pt) | 2005-02-14 | 2010-04-06 | Univ Virginia | composto ou um sal ou éster farmaceuticamente aceitável do mesmo, e, uso de um composto |
| BRPI0609515A8 (pt) | 2005-03-23 | 2017-12-26 | Actelion Pharmaceuticals Ltd | Composto, composição farmacêutica, e, uso de um composto |
| NZ562561A (en) | 2005-03-23 | 2010-11-26 | Actelion Pharmaceuticals Ltd | Novel thiophene derivatives as sphingosine-1-phosphate-1 receptor agonists |
| TW200642683A (en) | 2005-04-22 | 2006-12-16 | Sankyo Co | Heterocyclic compound |
| JP2008545767A (ja) | 2005-06-08 | 2008-12-18 | ノバルティス アクチエンゲゼルシャフト | 多環式オキサジアゾールまたはイソキサゾールおよびｓｉｐ受容体リガンドとしてのそれらの使用 |
| US20090221547A1 (en) | 2005-08-23 | 2009-09-03 | Irm Llc | Immunosuppressant Compounds and Compositions |
| AU2006317689B2 (en) | 2005-11-23 | 2013-07-25 | Epix Delaware, Inc. | S1P receptor modulating compounds and use thereof |
| GB0601744D0 (en) | 2006-01-27 | 2006-03-08 | Novartis Ag | Organic compounds |
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| JP2009269819A (ja) | 2006-08-25 | 2009-11-19 | Asahi Kasei Pharma Kk | アミン化合物 |
| AR061841A1 (es) | 2006-09-07 | 2008-09-24 | Actelion Pharmaceuticals Ltd | Derivados de tiofen-oxadiazoles, agonistas del receptor s1p1/edg1, composiciones farmaceuticas que los contienen y usos como agentes inmunomoduladores. |
| KR101470659B1 (ko) | 2006-09-07 | 2014-12-08 | 액테리온 파마슈티칼 리미티드 | 면역조절제로서 피리딘-4-일 유도체 |
| EP2069318B1 (en) | 2006-09-21 | 2012-09-12 | Actelion Pharmaceuticals Ltd. | Phenyl derivatives and their use as immunomodulators |
| NZ577111A (en) | 2006-12-15 | 2012-05-25 | Abbott Lab | Novel oxadiazole compounds |
| EP2120575A4 (en) | 2006-12-21 | 2011-04-27 | Abbott Lab | AGONISTS AND ANTAGONISTS OF SPHINGOSINE-1-PHOSPHATE RECEPTORS |
| GB0625648D0 (en) | 2006-12-21 | 2007-01-31 | Glaxo Group Ltd | Compounds |
| KR20100016617A (ko) * | 2007-05-18 | 2010-02-12 | 바이엘 쉐링 파마 악티엔게젤샤프트 | 과증식성 장애 및 혈관형성 관련 질환의 치료에 유용한 저산소증 유도성 인자 （ｈｉｆ）의 억제제 |
| US20090069288A1 (en) | 2007-07-16 | 2009-03-12 | Breinlinger Eric C | Novel therapeutic compounds |
| CA2696863C (en) | 2007-10-04 | 2016-10-18 | Anna Quattropani | Oxadiazole derivatives |
| MX2010003614A (es) | 2007-10-04 | 2010-04-21 | Merck Serono Sa | Compuestos de diarilo oxadiazol. |
| BRPI0818804A2 (pt) | 2007-11-01 | 2015-04-22 | Actelion Pharmaceuticals Ltd | Composto derivado de pirimidina, composição farmacêutica que o compreende e uso desse composto. |
| MX2010007026A (es) * | 2007-12-21 | 2010-10-05 | Merck Serono Sa | Derivados de triazoloxadiazoles. |
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| EP2913326B1 (en) | 2008-05-14 | 2020-07-15 | The Scripps Research Institute | Novel modulators of sphingosine phosphate receptors |
| CA2739303A1 (en) | 2008-10-01 | 2010-04-08 | Synta Pharmaceuticals Corp. | Compounds for inflammation and immune-related uses |
| AU2009300317A1 (en) | 2008-10-01 | 2010-04-08 | Synta Pharmaceuticals Corp. | Compounds for inflammation and immune-related uses |
| WO2010065760A1 (en) | 2008-12-04 | 2010-06-10 | Exelixis, Inc. | Imidazo [1,2a] pyridine derivatives, their use as s1p1 agonists and methods for their production |
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| EP2382211A1 (en) | 2011-11-02 |
| US8389509B2 (en) | 2013-03-05 |
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