CAS: 19156-54-8; 4,5,6,7-Tetrahydrobenzo[b]Thiophene-3-Carboxylic Acid

上下游产品

CAS号14559-12-7 4,5,6,7-四氢苯并[b]... | CAS号4506-71-2 2-氨基-4,5,6,7-四氢...

📜2-氨基-4,5,6,7-四氢苯并噻酚-3-羧酸乙酯置于盐酸,Sodium Hydroxide,Sodium Nitrite体系中,用 1,4-二氧六环,乙醇 用作溶剂,化学反应 1.25H,反应生成4,5,6,7-四氢苯并[b]噻吩-3-羧酸
参考文献:一类新型的,有效的,选择性的和口服活性的前列腺素d2受体拮抗剂的各种衍生物的合成和生物活性.2.6,6-二甲基双环[3.1.1]庚烷衍生物.
标题:一类新型的,有效的,选择性的和口服活性的前列腺素d2受体拮抗剂的各种衍生物的合成和生物活性.2.6,6-二甲基双环[3.1.1]庚烷衍生物.
摘要:在较早的论文中,我们报道了以双环[2.2.1]庚烷环系统为前列腺素骨架的新型前列腺素d(2)(pgd(2))受体拮抗剂是一种有效的新型抗过敏剂,可抑制各种过敏性炎症诸如在结膜炎和哮喘模型中观测到的反应.在本研究中,我们合成了具有6,6-二甲基双环[3.1.1]庚烷环系统的pgd(2)受体拮抗剂.与具有磺酰胺基的双环[2.2.1]庚烷环系统的那些相反,这些衍生物具有酰胺部分.具有6,6-二甲基双环[3.1.1]庚烷环的衍生物在pgd(2)受体结合和camp形成分析中也显示出强大的活性.在诸如过敏性鼻炎,结膜炎和哮喘模型等体内分析中,这些系列的衍生物显示出优异的药理特性.特别地,化合物45在过敏性鼻炎和哮喘模型中也有效抑制了嗜酸性粒细胞的浸润.该化合物(45,S-5751)现在正被开发为一种有前途的抗过敏药物候选物.
Doi:10.1021/jm0205189

专利信息

专利号:US-2007275962-A1
优先权日:2003-09-10
标 题:Heterobicyclic Compounds as Pharmaceutically Active Agents
发明人：KOUL ANIL; KLEBL BERT; MULLER GERHARD; MISSIO ANDREA; SCHWAB WILFRIED; HAFENBRADL DORIS; NEUMANN LARS; SOMMER MARC-NICOLA; MULLER STEFAN; HOPPE EDMUND; FREISLEBEN ACHIM; BACKES ALEXANDER; HARTUNG CHRISTIAN; FELBER BEATRICE; ZECH BIRGIT; ENGKVIST OLA; KERI GYORGY; ORFI LASZLO; BANHEGYI PETER; GREFF ZOLTAN; HORVATH ZOLTAN; VARGA ZOLTAN; MARKO PETER; PATO JANOS; SZABADKAI ISTVAN; SZEKELYHID ZSOLT; WACZEK FRIGYES
权利人:GPC BIOTECH AG
摘要:Described are heterobicyclic compounds such as 4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]thiopyran 3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]pyran-3-carboxylic acid amides, or benzo[b]thiophene-3-carboxylic acid amides and pharmaceutically acceptable salts thereof, the use of these derivatives for the prophylaxis and/or treatment of various diseases such as infectious diseases, including mycobacteriainduced infections and opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, as well as compositions containing at least one heterobicyclic compound and/or pharmaceutically acceptable salts thereof. Furthermore, reaction procedures for the synthesis of the heterobicyclic compound are disclosed.