NO327345B1 - 2,4,5-trisubstituerte tiazolylderivater og deres antiinflammatoriske aktivitet - Google Patents
2,4,5-trisubstituerte tiazolylderivater og deres antiinflammatoriske aktivitet Download PDFInfo
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- NO327345B1 NO327345B1 NO20040631A NO20040631A NO327345B1 NO 327345 B1 NO327345 B1 NO 327345B1 NO 20040631 A NO20040631 A NO 20040631A NO 20040631 A NO20040631 A NO 20040631A NO 327345 B1 NO327345 B1 NO 327345B1
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- -1 2,4,5-trisubstituted thiazolyl Chemical class 0.000 title claims abstract description 108
- 230000003110 anti-inflammatory effect Effects 0.000 title claims description 7
- 150000001875 compounds Chemical class 0.000 claims abstract description 164
- 150000003839 salts Chemical class 0.000 claims abstract description 40
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 31
- 108060008682 Tumor Necrosis Factor Proteins 0.000 claims abstract description 29
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 claims abstract description 29
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims abstract description 25
- 108010065805 Interleukin-12 Proteins 0.000 claims abstract description 23
- 102000013462 Interleukin-12 Human genes 0.000 claims abstract description 23
- 201000010099 disease Diseases 0.000 claims abstract description 22
- 238000011282 treatment Methods 0.000 claims abstract description 20
- 239000003814 drug Substances 0.000 claims abstract description 17
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract description 14
- 230000001404 mediated effect Effects 0.000 claims abstract description 13
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims abstract description 10
- 229920006395 saturated elastomer Polymers 0.000 claims abstract description 10
- 125000003118 aryl group Chemical group 0.000 claims abstract description 9
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract description 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims abstract description 7
- 230000002265 prevention Effects 0.000 claims abstract description 5
- 125000001475 halogen functional group Chemical group 0.000 claims abstract 7
- 125000003277 amino group Chemical group 0.000 claims abstract 3
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- 125000000217 alkyl group Chemical group 0.000 claims description 35
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- 238000000034 method Methods 0.000 claims description 27
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- 125000004122 cyclic group Chemical group 0.000 claims description 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 12
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- 125000003226 pyrazolyl group Chemical group 0.000 claims description 8
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- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 7
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- 230000002757 inflammatory effect Effects 0.000 claims description 6
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- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 5
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- 208000027866 inflammatory disease Diseases 0.000 claims description 5
- 125000004076 pyridyl group Chemical group 0.000 claims description 5
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 5
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- 230000000947 anti-immunosuppressive effect Effects 0.000 claims description 3
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- 238000000844 transformation Methods 0.000 claims 1
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- MZOFCQQQCNRIBI-VMXHOPILSA-N (3s)-4-[[(2s)-1-[[(2s)-1-[[(1s)-1-carboxy-2-hydroxyethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-[[2-[[(2s)-2,6-diaminohexanoyl]amino]acetyl]amino]-4-oxobutanoic acid Chemical compound OC[C@@H](C(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@@H](N)CCCCN MZOFCQQQCNRIBI-VMXHOPILSA-N 0.000 abstract description 20
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- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
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- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
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- C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- Health & Medical Sciences (AREA)
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Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
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| EP01203088 | 2001-08-13 | ||
| PCT/EP2002/008956 WO2003015776A1 (fr) | 2001-08-13 | 2002-08-09 | Derives de thiazolyl 2,4,5-trisubstitue et activite anti-inflammatoire associee |
Publications (2)
| Publication Number | Publication Date |
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| NO20040631L NO20040631L (no) | 2004-03-12 |
| NO327345B1 true NO327345B1 (no) | 2009-06-15 |
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Family Applications (1)
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Country Status (26)
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| EP (1) | EP1418911B1 (fr) |
| JP (1) | JP4491231B2 (fr) |
| KR (1) | KR100922538B1 (fr) |
| CN (1) | CN100502863C (fr) |
| AR (1) | AR037232A1 (fr) |
| AT (1) | ATE325608T1 (fr) |
| AU (1) | AU2002331227B2 (fr) |
| BR (1) | BR0211910A (fr) |
| CA (1) | CA2451981C (fr) |
| DE (1) | DE60211348T2 (fr) |
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| HK (1) | HK1077507A1 (fr) |
| HR (1) | HRP20040098B1 (fr) |
| HU (1) | HUP0401160A3 (fr) |
| IL (2) | IL160327A0 (fr) |
| MX (1) | MXPA04001400A (fr) |
| MY (1) | MY130780A (fr) |
| NO (1) | NO327345B1 (fr) |
| NZ (1) | NZ530772A (fr) |
| PL (1) | PL210475B1 (fr) |
| TW (1) | TWI268152B (fr) |
| UA (1) | UA79756C2 (fr) |
| WO (1) | WO2003015776A1 (fr) |
| ZA (1) | ZA200401164B (fr) |
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| AU2003247959B2 (en) * | 2002-07-09 | 2010-07-29 | Vertex Pharmaceuticals Incorporated | Imidazoles, oxazoles and thiazoles with protein kinase inhibiting activities |
| PA8578101A1 (es) * | 2002-08-13 | 2004-05-07 | Warner Lambert Co | Derivados de heterobiarilo como inhibidores de metaloproteinasa de la matriz |
| GB0308466D0 (en) | 2003-04-11 | 2003-05-21 | Novartis Ag | Organic compounds |
| US7560568B2 (en) | 2004-01-28 | 2009-07-14 | Smithkline Beecham Corporation | Thiazole compounds |
| WO2006038734A1 (fr) * | 2004-10-08 | 2006-04-13 | Astellas Pharma Inc. | Dérivés de la pyridazinone inhibiteurs de cytokines |
| EP1802588A4 (fr) * | 2004-10-15 | 2010-02-17 | Astrazeneca Ab | Amino-pyrimidones substitues et utilisation de ceux-ci |
| JP2008516945A (ja) * | 2004-10-15 | 2008-05-22 | アストラゼネカ・アクチエボラーグ | 置換されたアミノ化合物およびそれらの使用 |
| JP2008531537A (ja) * | 2005-02-25 | 2008-08-14 | クドス ファーマシューティカルズ リミテッド | 化合物 |
| EP1932840B1 (fr) * | 2005-10-03 | 2014-04-09 | Ono Pharmaceutical Co., Ltd. | Composé hétérocyclique azoté et application pharmaceutique de celui-ci |
| KR20100092473A (ko) * | 2007-11-01 | 2010-08-20 | 액테리온 파마슈티칼 리미티드 | 신규한 피리미딘 유도체 |
| JP5581219B2 (ja) | 2008-01-25 | 2014-08-27 | ミレニアム ファーマシューティカルズ， インコーポレイテッド | チオフェンおよびホスファチジルイノシトール３−キナーゼ（ｐｉ３ｋ）阻害薬としてのその使用 |
| TWI403506B (zh) * | 2008-06-16 | 2013-08-01 | Faes Farma Sa | 用於治療急性和慢性發炎疾病之５－（４－甲磺醯基－苯基）－噻唑衍生物類 |
| JP5681105B2 (ja) | 2008-07-17 | 2015-03-04 | バイエル・クロップサイエンス・アーゲーＢａｙｅｒ Ｃｒｏｐｓｃｉｅｎｃｅ Ａｇ | 殺害虫剤として使用されるヘテロ環式化合物 |
| NZ592297A (en) * | 2008-09-22 | 2012-11-30 | Cayman Chemical Co Inc | 2-Aryl-5-heteroaryl pyridine and pyrimidine derivatives as pharmaceutical active agents |
| US8314130B2 (en) | 2008-10-01 | 2012-11-20 | Synta Pharmaceuticals Corp. | Compounds inclunding substituted pyridines for inflammation and immune-related uses |
| CN101391984B (zh) * | 2008-11-07 | 2010-12-08 | 东华大学 | 碳酸二甲酯对含巯基的嘧啶杂环化合物进行甲基化的方法 |
| US8796314B2 (en) | 2009-01-30 | 2014-08-05 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| US9139589B2 (en) | 2009-01-30 | 2015-09-22 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| US9090601B2 (en) * | 2009-01-30 | 2015-07-28 | Millennium Pharmaceuticals, Inc. | Thiazole derivatives |
| BR112012028280A2 (pt) | 2010-05-05 | 2015-09-15 | Bayer Ip Gmbh | derivados de tiazole como pesticidas |
| WO2012021611A1 (fr) | 2010-08-11 | 2012-02-16 | Millennium Pharmaceuticals, Inc. | Hétéroaryles et utilisations de ceux-ci |
| WO2012021696A1 (fr) | 2010-08-11 | 2012-02-16 | Millennium Pharmaceuticals, Inc. | Hétéroaryles et leurs utilisations |
| US8859768B2 (en) | 2010-08-11 | 2014-10-14 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| CN103237450A (zh) | 2010-10-13 | 2013-08-07 | 米伦纽姆医药公司 | 杂芳基化合物和其用途 |
| US20120129843A1 (en) * | 2010-11-18 | 2012-05-24 | Yan Zhang | Pyridyl-thiazolyl inhibitors of pro-matrix metalloproteinase activation |
| WO2012109573A1 (fr) * | 2011-02-11 | 2012-08-16 | Purdue Research Foundation | Thiazoles substitués utilisés en tant qu'agents antiviraux |
| GEP201706748B (en) | 2012-08-10 | 2017-10-10 | Boehringer Ingelheim Int | Heteroaromatic compounds as bruton's tyrosine kinase (btk) inhibitors |
| US20150284380A1 (en) * | 2012-10-31 | 2015-10-08 | Bayer Cropscience Ag | Novel heterocyclic compounds as pest control agents |
| BR112015011497B1 (pt) | 2012-11-27 | 2023-01-10 | Thomas Helledays Stiftelse För Medicinsk Forskning | Composto, e, formulação farmacêutica |
| JP6486954B2 (ja) | 2014-01-29 | 2019-03-20 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｂｔｋ阻害剤としてのピラゾール化合物 |
| CA2948601A1 (fr) | 2014-06-04 | 2015-12-10 | Thomas Helledays Stiftelse For Medicinsk Forskning | Inhibiteurs de mth1 destines au traitement des etats inflammatoires et auto-immuns |
| WO2015187088A1 (fr) | 2014-06-04 | 2015-12-10 | Thomas Helledays Stiftelse För Medicinsk Forskning | Inhibiteurs mth1 pour le traitement du cancer |
| JOP20200117A1 (ar) | 2014-10-30 | 2017-06-16 | Janssen Pharmaceutica Nv | كحولات ثلاثي فلوروميثيل كمُعدلات للمستقبل النووي جاما تي المرتبط بحمض الريتيونَويك ROR?t |
| HUE046888T2 (hu) * | 2014-10-30 | 2020-03-30 | Janssen Pharmaceutica Nv | Amid-szubsztituált tiazolok mint ROR-gamma-t modulátorok |
| ES2708025T3 (es) * | 2014-10-30 | 2019-04-08 | Janssen Pharmaceutica Nv | Tiazoles como moduladores de RORyt |
| SI3390390T1 (sl) | 2015-12-16 | 2021-12-31 | Boehringer Ingelheim International Gmbh | Bipirazolilni derivati, uporabni za zdravljenje avtoimunskih bolezni |
| WO2017123695A1 (fr) | 2016-01-13 | 2017-07-20 | Boehringer Ingelheim International Gmbh | Utilisation d'isoquinolones comme inhibiteurs de btk |
| TW201803869A (zh) | 2016-04-27 | 2018-02-01 | 健生藥品公司 | 作為ＲＯＲγＴ調節劑之６－胺基吡啶－３－基噻唑 |
| US10414759B2 (en) * | 2017-05-08 | 2019-09-17 | Purdue Research Foundation | Phenylthiazoles and uses thereof |
| ES2929140T3 (es) | 2018-06-18 | 2022-11-25 | Janssen Pharmaceutica Nv | Imidazoles sustituidos con fenilo y piridinilo como moduladores de RORgammat |
| CN112566901A (zh) | 2018-06-18 | 2021-03-26 | 詹森药业有限公司 | 作为RORγt的调节剂的苯基取代的吡唑类 |
| WO2019244001A1 (fr) | 2018-06-18 | 2019-12-26 | Janssen Pharmaceutica Nv | 6-aminopyridin-3-yl pyrazoles en tant que modulateurs de roryt |
| EP3807261B1 (fr) | 2018-06-18 | 2022-07-13 | Janssen Pharmaceutica NV | Pyridinyl-pyrazoles utilisés utilisés comme modulateurs de roryt |
| CN110746325A (zh) * | 2018-07-24 | 2020-02-04 | 上海和辉光电有限公司 | 一种基于胍骨架的n型掺杂化合物及其应用 |
| CN110452224B (zh) * | 2019-08-30 | 2022-06-03 | 西南大学 | 嘧啶唑醇类化合物及其制备方法和应用 |
| WO2022155941A1 (fr) * | 2021-01-25 | 2022-07-28 | Qilu Regor Therapeutics Inc. | Inhibiteurs de cdk2 |
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| DE258165C (fr) | ||||
| US3499762A (en) | 1966-11-03 | 1970-03-10 | Eastman Kodak Co | Photographic elements comprising novel u.v.-absorbing optical brightening agents |
| DE1959307A1 (de) | 1969-11-26 | 1971-06-03 | Basf Ag | Optische Aufheller |
| BE795907A (fr) * | 1972-02-25 | 1973-06-18 | Luso Farmaco Inst | 2-amino-4-arylthiazoles 5-substitues et leur preparation |
| US4649146A (en) | 1983-01-31 | 1987-03-10 | Fujisawa Pharmaceutical Co., Ltd. | Thiazole derivatives and pharmaceutical composition comprising the same |
| JPH03144612A (ja) | 1989-10-31 | 1991-06-20 | Nec Corp | 接続方法 |
| JPH04368375A (ja) * | 1991-06-17 | 1992-12-21 | Otsuka Pharmaceut Factory Inc | イソオキサゾール誘導体 |
| US5240929A (en) * | 1992-08-03 | 1993-08-31 | Warner-Lambert Company | 2-heterocyclic-5-hydroxy-1,3-pyrimidines useful as antiinflammatory agents |
| JPH10504542A (ja) * | 1994-07-27 | 1998-05-06 | ジー．ディー．サール アンド カンパニー | 炎症処置用の置換チアゾール化合物 |
| JPH10507205A (ja) | 1995-08-02 | 1998-07-14 | ホータ．ウリアッヒ イ シイア．エセ．アー． | 抗真菌活性を有する新規カルボンアミド |
| AR008395A1 (es) * | 1996-07-09 | 2000-01-19 | Astra Pharma Prod | Compuesto derivado de pirimidina, composicion farmaceutica que lo comprende, procedimiento para prepararlo, y compuesto intermediario util parallevar a cabo dicho procedimiento. |
| EP0920426B9 (fr) | 1996-08-26 | 2005-04-06 | ALTANA Pharma AG | Nouveaux derives de thiazol a effet inhibant la phosphodiesterase |
| AU4015497A (en) | 1996-08-26 | 1998-03-19 | Byk Gulden Lomberg Chemische Fabrik Gmbh | Thiazole derivatives useful as selective inhibitors of pde-iv |
| WO2000035911A1 (fr) * | 1998-12-16 | 2000-06-22 | Aventis Pharma Limited | Acetals heteroaryl-cycliques |
| DE10001644A1 (de) * | 1999-01-19 | 2000-07-20 | Clariant Gmbh | Fluorierte Azole und ihre Verwendung in flüssigkristallinen Mischungen |
| DE60024480T2 (de) | 1999-10-27 | 2006-07-27 | Novartis Ag | Thiazol und imidazo[4,5-b]pyridin verbindungen und ihre verwendung als pharmazeutika |
| CN1230166C (zh) * | 2000-01-18 | 2005-12-07 | 沃泰克斯药物股份有限公司 | 回旋酶抑制剂及其用途 |
| AU3740101A (en) | 2000-03-01 | 2001-09-12 | Janssen Pharmaceutica Nv | 2,4-disubstituted thiazolyl derivatives |
| HUP0300382A3 (en) * | 2000-03-29 | 2006-11-28 | Cyclacel Ltd | 2-substituted 4-heteroaryl-pyrimidines and their use in the treatmetn of proliferative disorders and pharmaceutical compositions containing the compounds |
| JP2004517100A (ja) * | 2000-12-20 | 2004-06-10 | グラクソ グループ リミテッド | ｈＰＰＡＲアルファアゴニストとしての置換オキサゾールおよびチアゾール |
| GB0031103D0 (en) * | 2000-12-20 | 2001-01-31 | Glaxo Group Ltd | Chemical compounds |
| GB0031109D0 (en) * | 2000-12-20 | 2001-01-31 | Glaxo Group Ltd | Chemical compounds |
| GB0031107D0 (en) * | 2000-12-20 | 2001-01-31 | Glaxo Group Ltd | Chemical compounds |
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