Photocleavable and acid cleavable linkers for combinatorial chemistry
    1.
    发明授权
    Photocleavable and acid cleavable linkers for combinatorial chemistry 失效
    用于组合化学的可透光和可酸切割接头

    公开(公告)号:US06642417B2

    公开(公告)日:2003-11-04

    申请号:US09766987

    申请日:2001-01-22

    Abstract: A substrate for solid phase synthesis comprising a solid phase-linker combination of the formula I is disclosed. Also disclosed are processes for preparing the substrate and chemical intermediates useful therein. Among the novel intermediates are compounds of the formula II wherein R1 is —NO2 or —CHO; R2 is —OCH3, —CHO or —H; R3 is chosen from the group consisting of hydroxyl, the residue of a solid support having a plurality of amino groups, and the residue of an ester, and n=1 or 3-12. A substrate of solid phase synthesis of the formula III is also disclosed.

    Abstract translation: 公开了一种用于固相合成的底物,其包含式I的固相 - 连接体组合。 还公开了制备基材和其中有用的化学中间体的方法。 其中新的中间体是式II化合物,其中R 1是-NO 2或-CHO; R 2是-OCH 3,-CHO或-H; R 3选自羟基,具有多个氨基的固体支持物的残基和酯的残基,n = 1或3-12。A的固相合成底物 还公开了式III。

    Photocleavable and acid cleavable linkers for combinatorial chemistry
    2.
    发明授权
    Photocleavable and acid cleavable linkers for combinatorial chemistry 失效
    用于组合化学的可透光和可酸切割接头

    公开(公告)号:US06310244B1

    公开(公告)日:2001-10-30

    申请号:US09121262

    申请日:1998-07-23

    Abstract: A substrate for solid phase synthesis comprising a solid phase-linker combination of the formula I is disclosed. Also disclosed are processes for preparing the substrate and chemical intermediates useful therein. Among the novel intermediates are compounds of the formula II wherein R1 is —NO2 or —CHO; R2 is —OCH3, —CHO or —H; R3 is chosen from the group consisting of hydroxyl, the residue of a solid support having a plurality of amino groups, and the residue of an ester, and n=1 or 3. A substrate of solid phase synthesis of the formula III is also disclosed.

    Abstract translation: 公开了一种用于固相合成的底物,其包含式I的固相 - 连接体组合。 还公开了制备基材和其中有用的化学中间体的方法。 其中新型中间体为式II化合物,其中R 1为-NO 2或-CHO; R2是-OCH3,-CHO或-H; R3选自羟基,具有多个氨基的固体支持物的残基和酯的残基,n = 1或3.还公开了式III的固相合成底物 。

    Vanilloid receptor ligands and their use in treatments
    4.
    发明授权
    Vanilloid receptor ligands and their use in treatments 失效
    香草素受体配体及其在治疗中的应用

    公开(公告)号:US08026241B2

    公开(公告)日:2011-09-27

    申请号:US12367352

    申请日:2009-02-06

    Abstract: Therapeutic benzimidazoles and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotizing agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

    Abstract translation: 治疗性苯并咪唑和含有它们的组合物,用于治疗急性,炎性和神经性疼痛,牙痛,一般头痛,偏头痛,丛集性头痛,混合血管和非血管综合征,紧张性头痛,一般炎症,关节炎,风湿性疾病,骨关节炎 ,炎症性肠病,炎症性眼病,炎症性或不稳定性膀胱病,银屑病,皮肤炎症成分炎症,慢性炎性病症,炎性疼痛及相关的痛觉过敏和异常性疼痛,神经性疼痛及相关的痛觉过敏和异常性疼痛,糖尿病性神经病疼痛,灼痛,交感神经痛 维持疼痛,输血综合征,哮喘,上皮组织损伤或功能障碍,单纯疱疹,呼吸道,泌尿生殖道,胃肠道或血管区内脏运动紊乱,伤口,烧伤,过敏性皮肤反应,瘙痒,白癜风,一般胃肠道疾病,胃溃疡 十二指肠溃疡,腹泻,坏死因子诱发的胃损伤,毛发生长,血管舒缩或过敏性鼻炎,支气管疾病或膀胱疾病。

    VANILLOID RECEPTOR LIGANDS AND THEIR USE IN TREATMENTS
    8.
    发明申请
    VANILLOID RECEPTOR LIGANDS AND THEIR USE IN TREATMENTS 失效
    VANILLOID受体配体及其在治疗中的应用

    公开(公告)号:US20090143575A1

    公开(公告)日:2009-06-04

    申请号:US12367352

    申请日:2009-02-06

    Abstract: Therapeutic benzimidazoles and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotizing agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

    Abstract translation: 治疗性苯并咪唑和含有它们的组合物,用于治疗急性,炎性和神经性疼痛,牙痛,一般头痛,偏头痛,丛集性头痛,混合血管和非血管综合征,紧张性头痛,一般炎症,关节炎,风湿性疾病,骨关节炎 ,炎症性肠病,炎症性眼病,炎症性或不稳定性膀胱病,银屑病,皮肤炎症成分炎症,慢性炎性病症,炎性疼痛及相关的痛觉过敏和异常性疼痛,神经性疼痛及相关的痛觉过敏和异常性疼痛,糖尿病性神经病疼痛,灼痛,交感神经痛 维持疼痛,输血综合征,哮喘,上皮组织损伤或功能障碍,单纯疱疹,呼吸道,泌尿生殖道,胃肠道或血管区内脏运动紊乱,伤口,烧伤,过敏性皮肤反应,瘙痒,白癜风,一般胃肠道疾病,胃溃疡 十二指肠溃疡,腹泻,坏死因子诱发的胃损伤,毛发生长,血管舒缩或过敏性鼻炎,支气管疾病或膀胱疾病。

    TRP-M8 receptor ligands and their use in treatments
    10.
    发明授权
    TRP-M8 receptor ligands and their use in treatments 有权
    TRP-M8受体配体及其在治疗中的应用

    公开(公告)号:US08476297B2

    公开(公告)日:2013-07-02

    申请号:US12746292

    申请日:2008-12-04

    Abstract: Tetrahydroisoquinoline compounds of formula (I), and compositions containing them, for the treatment of acute, inflammatory and neurophatic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neurophatic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

    Abstract translation: 式(I)的四氢异喹啉化合物和含有它们的组合物,用于治疗急性,炎性和神经性疼痛,牙痛,一般头痛,偏头痛,丛集性头痛,混合血管和非血管综合征,紧张性头痛,一般炎症, 关节炎,风湿性疾病,骨关节炎,炎症性肠病,炎症性眼病,炎性或不稳定性膀胱病,牛皮癣,皮肤炎症成分投诉,慢性炎性病症,炎性疼痛及相关的痛觉过敏和异常性疼痛,神经性疼痛及相关的痛觉过敏和异常性疼痛,糖尿病 神经病痛,咳嗽痛,交感神经保持疼痛,交感综合征,哮喘,上皮组织损伤或功能障碍,单纯疱疹,呼吸道内脏运动紊乱,泌尿生殖道,胃肠道或血管区,伤口,烧伤,过敏性皮肤反应,瘙痒,白癜风,一般 胃肠道 胃溃疡,十二指肠溃疡,腹泻,坏死因子诱导的胃损伤,毛发生长,血管舒缩或过敏性鼻炎,支气管疾病或膀胱疾病。

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