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    • 4. 发明申请
    • FORMULATIONS CONTAINING PYRIDAZINE COMPOUNDS FOR TREATING NEUROINFLAMMATORY DISEASES
    • 含有吡咯烷酮化合物治疗神经炎症性疾病的配方
    • WO2007127375A3
    • 2008-02-07
    • PCT/US2007010248
    • 2007-04-27
    • UNIV NORTHWESTERNWATTERSON MARTINVAN ELDIK LINDAHU WENHUI
    • WATTERSON MARTINVAN ELDIK LINDAHU WENHUI
    • A61K31/501A61K31/506A61P25/28C07D403/04
    • A61K31/506A61K31/501C07D237/20C07D401/12C07D401/14C07D403/12C07D403/14
    • The invention relates to chemical compounds, compositions and methods of making and using the same. In particular, the invention provides selected pyridazine compounds of the formula (I) are independently hydrogen, hydroxyl, alkyl, alkenyl, alkynyl, alkylene, alkenylene, alkoxy, alkenyloxy, cycloalkyl, cycloalkenyl, cycloalkynyl, cycloalkoxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, sulfate, sulfenyl, sulfinyl, sulfonyl, sulfonate, sulfoxide, silyl, silyloxy, silylalkyl, silylthio, =0, =S, phosphonate, ureido, carboxyl, carbonyl, carbamoyl, or carboxamide; and X is optionally substituted pyrimidinyl or pyridazinyl, an isomer, a pharmaceutically acceptable salt, or derivative thereof. The invention additional relates to compositions comprising the compounds, and methods of using the compounds and compositions for modulation of cellular pathways, for treatment or prevention of inflammatory diseases, for research, drug screening, and therapeutic applications.
    • 本发明涉及化合物,组合物和制备和使用它们的方法。 特别地,本发明提供所选择的式(I)哒嗪化合物独立地是氢,羟基,烷基,烯基,炔基,亚烷基,亚烯基,烷氧基,烯氧基,环烷基,环烯基,环炔基,环烷氧基,芳基,芳氧基,芳基烷氧基,芳酰基 杂芳基,杂环基,酰基,酰氧基,氨基,亚氨基,叠氮基,硫醇,硫代烷基,硫代烷氧基,硫代芳基,硝基,氰基,卤素,硫酸酯,亚磺酰基,磺酰基,磺酸酯,亚砜,甲硅烷基,甲硅烷氧基,甲硅烷基烷基,甲硅烷硫基, 0,= S,膦酸酯,脲基,羧基,羰基,氨基甲酰基或甲酰胺; X是任选取代的嘧啶基或哒嗪基,异构体,药用盐或其衍生物。 本发明另外涉及包含该化合物的组合物,以及使用该化合物和组合物调节细胞途径,用于治疗或预防炎性疾病,用于研究,药物筛选和治疗应用的方法。
    • 6. 发明申请
    • FORMULATIONS CONTAINING PYRID AZINE COMPOUND FIELD OF INVENTION
    • 含有吡嗪化合物的制剂技术领域
    • WO2007127375A2
    • 2007-11-08
    • PCT/US2007/010248
    • 2007-04-27
    • NEUROMEDIX, INC.WATTERSON, MartinVAN ELDIK, LindaHU, Wenhui, Ph.D.
    • WATTERSON, MartinVAN ELDIK, LindaHU, Wenhui, Ph.D.
    • A61K31/506A61K31/501C07D237/20C07D401/12C07D401/14C07D403/12C07D403/14
    • The invention relates to chemical compounds, compositions and methods of making and using the same. In particular, the invention provides selected pyridazine compounds of the formula I wherein R1, R4, R5, R6, R7, R8, R9, R12, R13 ET R14 are independently hydrogen, hydroxyl, alkyl, alkenyl, alkynyl, alkylene, alkenylene, alkoxy, alkenyloxy, cycloalkyl, cycloalkenyl, cycloalkynyl, cycloalkoxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, sulfate, sulfenyl, sulfinyl, sulfonyl, sulfonate, sulfoxide, silyl, silyloxy, silylalkyl, silylthio, =0, =S, phosphonate, ureido, carboxyl, carbonyl, carbamoyl, or carboxamide; and X is optionally substituted pyrimidinyl or pyridazinyl, an isomer, a pharmaceutically acceptable salt, or derivative thereof. The invention additional relates to compositions comprising the compounds, and methods of using the compounds and compositions for modulation of cellular pathways, for treatment or prevention of inflammatory diseases, for research, drug screening, and therapeutic applications.
    • 本发明涉及化合物,组合物和制备和使用它们的方法。 特别地,本发明提供了选择的式I的哒嗪化合物,其中R 1,R 4,R 5,R 6,R 7,R 8,R 9,R 12,R 13,ET R 14独立地为氢,羟基,烷基,烯基,炔基,亚烷基,亚烯基, ,烯氧基,环烷基,环烯基,环炔基,环烷氧基,芳基,芳氧基,芳基烷氧基,芳酰基,芳基,杂环,酰基,酰氧基,氨基,亚氨基,叠氮基,硫醇,硫代烷基,硫代烷氧基,硫代芳基,硝基,氰基, 磺酰基,磺酰基,亚砜,甲硅烷基,甲硅烷氧基,甲硅烷基烷基,甲硅烷硫基,= O,= S,膦酸酯,脲基,羧基,羰基,氨基甲酰基或甲酰胺; X是任选取代的嘧啶基或哒嗪基,异构体,药用盐或其衍生物。 本发明另外涉及包含该化合物的组合物,以及使用该化合物和组合物调节细胞途径,用于治疗或预防炎性疾病,用于研究,药物筛选和治疗应用的方法。
    • 7. 发明申请
    • SALTS OF PYRIDAZINE COMPOUNDS
    • 吡啶化合物的盐
    • WO2007127448A3
    • 2008-01-31
    • PCT/US2007010368
    • 2007-04-27
    • UNIV NORTHWESTERNWATTERSON MARTINVAN ELDIK LINDAHU WENHUI
    • WATTERSON MARTINVAN ELDIK LINDAHU WENHUI
    • A61K31/506A61P25/00A61P25/28C07D403/12
    • A61K31/506C07D403/12
    • The invention relates to stable and substantially purified synthetic pharmaceutically acceptable acid addition salts of pyridazine compounds of the formula I wherein R10 is hydrogen, hydroxyl, alkyl, alkoxy, alkenyl, alkynyl, alkylene, aryl, heteroaryl, sulfonyl, sulfinyl, sulfenyl, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, =0, =S, carboxyl, carbonyl, carbamoyl, carboxamide, or phosphonate, and R11 is alkyl, alkoxy, alkenyl, alkynyl, alkylene, alkenylene, alkenyloxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, sulfonyl, sulfinyl, sulfenyl, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, =0, =S, phosphonate, carboxyl, carbonyl, carbamoyl, carboxamide, or ureido. The invention also relates to formulations, dosage forms and compositions comprising the salts, and methods of using the salts, formulations, dosage forms and compositions.
    • 本发明涉及式I的哒嗪化合物的稳定且基本纯化的合成药学上可接受的酸加成盐,其中R 10是氢,羟基,烷基,烷氧基,烯基,炔基,亚烷基,芳基,杂芳基,磺酰基,亚磺酰基,亚硫酰基,氨基, 亚氨基,叠氮基,硫醇,硫代烷基,硫代烷氧基,硫代芳基,硝基,氰基,卤素,= S,羧基,羰基,氨基甲酰基,羧酰胺或膦酸酯,R11是烷基,烷氧基,烯基,炔基,亚烷基,亚烯基, 链烯氧基,芳基,芳氧基,芳基烷氧基,芳酰基,杂芳基,杂环基,酰基,酰氧基,磺酰基,亚磺酰基,亚磺酰基,氨基,亚氨基,叠氮基,硫醇,硫代烷基,硫代烷氧基,硫代芳基,硝基,氰基,卤素, 膦酸酯,羧基,羰基,氨基甲酰基,羧酰胺或脲基。 本发明还涉及制剂,剂型和包含盐的组合物,以及使用盐,制剂,剂型和组合物的方法。
    • 10. 发明申请
    • SALTS OF PYRIDAZINE COMPOUNDS
    • 吡啶化合物的盐
    • WO2007127448A2
    • 2007-11-08
    • PCT/US2007/010368
    • 2007-04-27
    • NEUROMEDIX, INC.WATTERSON, MartinVAN ELDIK, LindaHU, Wenhui
    • WATTERSON, MartinVAN ELDIK, LindaHU, Wenhui
    • C07D403/12
    • A61K31/506C07D403/12
    • The invention relates to stable and substantially purified synthetic pharmaceutically acceptable acid addition salts of pyridazine compounds of the formula I wherein R10 is hydrogen, hydroxyl, alkyl, alkoxy, alkenyl, alkynyl, alkylene, aryl, heteroaryl, sulfonyl, sulfinyl, sulfenyl, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, =0, =S, carboxyl, carbonyl, carbamoyl, carboxamide, or phosphonate, and R11 is alkyl, alkoxy, alkenyl, alkynyl, alkylene, alkenylene, alkenyloxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, sulfonyl, sulfinyl, sulfenyl, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, =0, =S, phosphonate, carboxyl, carbonyl, carbamoyl, carboxamide, or ureido. The invention also relates to formulations, dosage forms and compositions comprising the salts, and methods of using the salts, formulations, dosage forms and compositions.
    • 本发明涉及式I的哒嗪化合物的稳定且基本纯化的合成药学上可接受的酸加成盐,其中R 10是氢,羟基,烷基,烷氧基,烯基,炔基,亚烷基,芳基,杂芳基,磺酰基,亚磺酰基,亚硫酰基,氨基, 亚氨基,叠氮基,硫醇,硫代烷基,硫代烷氧基,硫代芳基,硝基,氰基,卤素,= S,羧基,羰基,氨基甲酰基,羧酰胺或膦酸酯,R11是烷基,烷氧基,烯基,炔基,亚烷基,亚烯基, 链烯氧基,芳基,芳氧基,芳基烷氧基,芳酰基,杂芳基,杂环基,酰基,酰氧基,磺酰基,亚磺酰基,亚磺酰基,氨基,亚氨基,叠氮基,硫醇,硫代烷基,硫代烷氧基,硫代芳基,硝基,氰基,卤素, 膦酸酯,羧基,羰基,氨基甲酰基,羧酰胺或脲基。 本发明还涉及制剂,剂型和包含盐的组合物,以及使用盐,制剂,剂型和组合物的方法。