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    Alkoxy-substituted compounds, methods, and compositions for inhibiting PARP activity
    2.
    发明授权
    Alkoxy-substituted compounds, methods, and compositions for inhibiting PARP activity 失效
    用于抑制PARP活性的烷氧基取代的化合物，方法和组合物

    公开(公告)号：US06197785B1

    公开(公告)日：2001-03-06

    申请号：US09145166

    申请日：1998-09-01

    申请人： Paul F. Jackson ,  Keith M. Maclin ,  Jie Zhang

    发明人： Paul F. Jackson ,  Keith M. Maclin ,  Jie Zhang

    IPC分类号： C07D21724

    CPC分类号： C07D471/06 ,  C07D217/22 ,  C07D217/24 ,  C07D221/12 ,  C07D221/18 ,  C07D237/30 ,  C07D237/32 ,  C07D237/34 ,  C07D239/88 ,  C07D239/93 ,  C07D239/94 ,  C07D475/02 ,  C07D491/04 ,  C07F9/6561

    摘要： A compound, compositions, methods of use, and processes of making formula I: or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof, wherein: R1, when present, is hydrogen or lower alkyl; R2 is lower alkyl, aryl, aralkyl, lower alkanoyl, or —(CH2)n—(CHOH)y(CH2)mA, wherein n is 1-4, y is 0 or 1, m is 0-5, and A is cycloalkyl, cycloalkenyl, lower alkanoyl, aryl, aralkyl, —NH2, —NH—(lower alkyl), Y represents the atoms necessary to form a fused 5- to 6-membered ring that is aromatic or nonaromatic and carbocyclic or heterocyclic; Z is (i) —CHR2CHR3— where R2 and R3 are independently hydrogen, alkyl, aryl or aralkyl; (ii) —R6C═CR3— where R6 and R3 are independently hydrogen, lower alkyl, aryl, aralkyl, chlorine, bromine or —NR7R8, where R7 and R8 are independently hydrogen or lower alkyl, or, R6 and R3, taken together, form a fused 5- to 6-membered ring that is aromatic or nonaromatic and carbocyclic or heterocyclic; (iii) —R2C═N—; (iv) —CR2(OH)—NR7—; or (v) —C(O)—NR7—.

    摘要翻译： 化合物，组合物，使用方法和制备式I的方法：或其药学上可接受的盐，水合物，酯，溶剂化物，前药，代谢物，立体异构体或其混合物，其中：R 1当存在时为氢或低级烷基 或 - （CH 2）n - （CHOH）y（CH 2）mA，其中n为1-4，y为0或1，m为0-5，A为 是环烷基，环烯基，低级烷酰基，芳基，芳烷基，-NH 2，-NH-（低级烷基），Y表示形成芳族或非芳族和碳环或杂环的稠合5-至6-元环所必需的原子; Z 是（i）-CHR2CHR3-，其中R2和R3独立地是氢，烷基，芳基或芳烷基;（ii）-R6C = CR3-，其中R6和R3独立地是氢，低级烷基，芳基，芳烷基，氯，溴或-NR7R8 其中R 7和R 8独立地为氢或低级烷基，或者R 6和R 3一起形成芳族或非芳族和碳环或杂环的稠合5-至6-元环;（ⅲ）-R2C = N-; （一世 v）-CR 2（OH）-NR 7 - ; 或（ⅴ）-C（O）-NR7-。

    Alkoxy-substituted compounds, methods, and compositions for inhibiting PARP activity
    4.
    发明授权
    Alkoxy-substituted compounds, methods, and compositions for inhibiting PARP activity 失效
    用于抑制PARP活性的烷氧基取代的化合物，方法和组合物

    公开(公告)号：US06380211B1

    公开(公告)日：2002-04-30

    申请号：US09711953

    申请日：2000-11-15

    申请人： Paul F. Jackson ,  Keith M. Maclin ,  Jie Zhang

    发明人： Paul F. Jackson ,  Keith M. Maclin ,  Jie Zhang

    IPC分类号： A61K3147

    CPC分类号： C07D471/06 ,  C07D217/22 ,  C07D217/24 ,  C07D221/12 ,  C07D221/18 ,  C07D237/30 ,  C07D237/32 ,  C07D237/34 ,  C07D239/88 ,  C07D239/93 ,  C07D239/94 ,  C07D475/02 ,  C07D491/04 ,  C07F9/6561

    摘要： A compound, compositions, methods of use, and processes of making formula I: or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof, wherein: R1, when present, is hydrogen or lower alkyl; R2 is lower alkyl, aryl, aralkyl, lower alkanoyl, or —(CH2)n—(CHOH)y(CH2)mA, wherein n is 1-4, y is 0 or 1, m is 0-5, and A is cycloalkyl, cycloalkenyl, lower alkanoyl, aryl, aralkyl, —NH2, —NH—(lower alkyl), Y represents the atoms necessary to form a fused 5- to 6-membered ring that is aromatic or nonaromatic and carbocyclic or heterocyclic; Z is (i) —CHR2CHR3— where R2 and R3 are independently hydrogen, alkyl, aryl or aralkyl; (ii) —R6C═CR3— where R6 and R3 are independently hydrogen, lower alkyl, aryl, aralkyl, chlorine, bromine or —NR7R8, where R7 and R8 are independently hydrogen or lower alkyl, or, R6 and R3, taken together, form a fused 5- to 6-membered ring that is aromatic or nonaromatic and carbocyclic or heterocyclic; (iii) —R2C═N—; (iv) —CR2(OH)—NR7—; or (v) —C(O)—NR7—.

    摘要翻译： 化合物，组合物，使用方法和制备式I的方法：或其药学上可接受的盐，水合物，酯，溶剂化物，前药，代谢物，立体异构体或其混合物，其中：R 1当存在时为氢或低级烷基 或 - （CH 2）n - （CHOH）y（CH 2）mA，其中n为1-4，y为0或1，m为0-5，A为 是环烷基，环烯基，低级烷酰基，芳基，芳烷基，-NH 2，-NH-（低级烷基），Y表示形成芳族或非芳族和碳环或杂环的稠合5-至6-元环所必需的原子; Z 是（i）-CHR2CHR3-，其中R2和R3独立地是氢，烷基，芳基或芳烷基;（ii）-R6C = CR3-，其中R6和R3独立地是氢，低级烷基，芳基，芳烷基，氯，溴或-NR7R8 其中R 7和R 8独立地为氢或低级烷基，或者R 6和R 3一起形成芳族或非芳族和碳环或杂环的稠合5-至6-元环;（ⅲ）-R2C = N-; （iv ）-CR2（OH）-NR7-; 或（ⅴ）-C（O）-NR7-。

    PARP inhibitors, pharmaceutical compositions comprising same, and methods of using same
    6.
    发明授权
    PARP inhibitors, pharmaceutical compositions comprising same, and methods of using same 失效
    PARP抑制剂，包含其的药物组合物及其使用方法

    公开(公告)号：US06635642B1

    公开(公告)日：2003-10-21

    申请号：US09145176

    申请日：1998-09-01

    申请人： Paul F. Jackson ,  Jia-He Li ,  Keith M. Maclin ,  Jie Zhang

    发明人： Paul F. Jackson ,  Jia-He Li ,  Keith M. Maclin ,  Jie Zhang

    IPC分类号： A61K3150

    CPC分类号： A61K31/4725 ,  C07C233/65 ,  C07D209/56 ,  C07D217/24 ,  C07D217/26 ,  C07D221/12 ,  C07D221/14 ,  C07D221/18 ,  C07D237/26 ,  C07D237/32 ,  C07D243/14 ,  C07D267/14 ,  C07D491/06 ,  C07D495/04 ,  C07D495/06

    摘要： The present invention relates to PARP inhibitors, pharmaceutical compositions comprising the same, and methods of using the same to treat tissue damage resulting from cell damage or death due to necrosis or apoptosis, effect neuronal activities not mediated by NMDA toxicity; to treat neural tissue damage resulting from ischemia and reperfusion injury, neurological disorders and neurodegenerative diseases; to prevent or treat vascular stroke; to treat or prevent cardiovascular disorders; to treat other conditions and/or disorders such as age-related macular degeneration, AIDS and other immune senescence diseases, arthritis, atherosclerosis, cachexia, cancer, degenerative diseases of skeletal muscle involving replicative senescence, diabetes, head trauma, immune senescence, inflammatory bowel disorders (such as colitis and Crohn's disease), muscular dystrophy, osteoarthritis, osteoporosis, chronic and/or acute pain (such as neuropathic pain), renal failure, retinal ischemia, septic shock (such as endotoxic shock), organ damage due to transplantation, and skin aging; to extend the lifespan and proliferative capacity of cells; to alter gene expression of senescent cells; or to radiosensitize hypoxic tumor cells.

    摘要翻译： 本发明涉及PARP抑制剂，包含其的药物组合物及其用途，用于治疗由于坏死或凋亡引起的细胞损伤或死亡引起的组织损伤，影响不被NMDA毒性介导的神经元活性; 治疗由缺血和再灌注损伤，神经系统疾病和神经退行性疾病引起的神经组织损伤; 预防或治疗血管中风; 治疗或预防心血管疾病; 治疗年龄相关性黄斑变性，艾滋病和其他免疫衰老疾病，关节炎，动脉粥样硬化，恶病质，癌症，涉及复制衰老的骨骼肌退行性疾病，糖尿病，头部创伤，免疫衰老，炎性肠等其他病症和/或病症 疾病（如结肠炎和克罗恩病），肌营养不良症，骨关节炎，骨质疏松症，慢性和/或急性疼痛（如神经性疼痛），肾衰竭，视网膜缺血，败血性休克（如内毒素性休克），移植器官损伤 ，皮肤老化; 延长细胞的寿命和增殖能力; 改变衰老细胞的基因表达; 或放射性敏感的缺氧性肿瘤细胞。

    Alkoxy-substituted compounds, methods and compositions for inhibiting parp activity
    7.
    发明授权
    Alkoxy-substituted compounds, methods and compositions for inhibiting parp activity 失效
    烷氧基取代的化合物，用于抑制parp活性的方法和组合物

    公开(公告)号：US06426415B1

    公开(公告)日：2002-07-30

    申请号：US09079508

    申请日：1998-05-15

    申请人： Paul F. Jackson ,  Keith M. Maclin ,  Jie Zhang

    发明人： Paul F. Jackson ,  Keith M. Maclin ,  Jie Zhang

    IPC分类号： C07D23730

    CPC分类号： C07D471/06 ,  C07D217/22 ,  C07D217/24 ,  C07D221/12 ,  C07D221/18 ,  C07D237/30 ,  C07D237/32 ,  C07D237/34 ,  C07D239/88 ,  C07D239/93 ,  C07D239/94 ,  C07D475/02 ,  C07D491/04 ,  C07F9/6561

    摘要： A compound of formula I: or a pharmaceutically acceptable salt, prodrug, metabolite, optical isomer or stereoisomer thereof, wherein: R1, when present, is hydrogen or lower alkyl; R2 is lower alkyl, aryl, aralkyl, lower alkanoyl, or —(CH2)n—(CHOH)y(CH2)mA, wherein n is 1-4, y is 0 or 1, m is 0-5, and A is cycloalkyl, cycloalkenyl, lower alkanoyl, aryl, aralkyl, —NH2, —NH-(lower alkyl), Y represents the atoms necessary to form a fused 5- to 6-membered ring that is aromatic or nonaromatic and carbocyclic or heterocyclic; Z is (i) —CHR2CHR3— where R2 and R3 are independently hydrogen, alkyl, aryl or aralkyl; (ii) —R6C═CR3— where R6 and R3 are independently hydrogen, lower alkyl, aryl, aralkyl, chlorine, bromine or —NR7R8, where R7 and R8 are independently hydrogen or lower alkyl, or, R6 and R3, taken together, form a fused 5- to 6-membered ring that is aromatic or nonaromatic and carbocyclic or heterocyclic; (iii) —R2C═N—; (iv) —CR2(OH)—NR7—; or (v) —C(O)—NR7—.

    摘要翻译： 式I的化合物或其药学上可接受的盐，前药，代谢物，旋光异构体或立体异构体，其中：当存在时，R 1为氢或低级烷基; R 2为低级烷基，芳基，芳烷基，低级烷酰基或 - （ CH2）n-（CHOH）y（CH2）mA，其中n为1-4，y为0或1，m为0-5，A为环烷基，环烯基，低级烷酰基，芳基，芳烷基，-NH2， NH-（低级烷基），Y表示形成芳族或非芳族和碳环或杂环的稠合5-至6-元环所必需的原子; Z为（i）-CHR2CHR3-，其中R2和R3独立地为氢，烷基 ，芳基或芳烷基;（ii）-R6C = CR3-，其中R6和R3独立地为氢，低级烷基，芳基，芳烷基，氯，溴或-NR7R8，其中R7和R8独立地为氢或低级烷基，或R6和 R 3一起形成芳族或非芳族和碳环或杂环的稠合的5-至6-元环;（iii）-R2C = N - ;（iv）-CR2（OH）-NR7-; 或（ⅴ）-C（O）-NR7-。

    Compounds, methods and pharmaceutical compositions for treating neural or cardiovascular tissue damage
    8.
    发明授权
    Compounds, methods and pharmaceutical compositions for treating neural or cardiovascular tissue damage 失效
    用于治疗神经或心血管组织损伤的化合物，方法和药物组合物

    公开(公告)号：US06514983B1

    公开(公告)日：2003-02-04

    申请号：US09145181

    申请日：1998-09-01

    申请人： Jia-He Li ,  Jie Zhang ,  Paul F. Jackson ,  Keith M. Maclin

    发明人： Jia-He Li ,  Jie Zhang ,  Paul F. Jackson ,  Keith M. Maclin

    IPC分类号： A61K3147

    CPC分类号： C07D249/08 ,  A61K31/4741 ,  A61K31/502 ,  A61K31/5025 ,  C07D231/12 ,  C07D233/56 ,  C07D237/32 ,  C07D491/06 ,  C07D495/06

    摘要： This invention relates to compounds, pharmaceutical compositions, and methods of using compounds of the formula: or a pharmaceutically acceptable salt, hydrate, prodrug, or mixtures thereof, wherein Y is alkylhalo, alkyl-CO—G, COG, a direct bond, C═O, O, NR11, or CR8; G is NR11R16, OR9, SR9, or R10; Z is O, S, or NR11; X is NR16, O, S, CR12R13, C═O, a bond, —CR12═CR13—, —C(R12R13)C(R14R15)—, or; Rhd 1, R2, R3, R4, R5, R6, R7, R8, R10, R12, R13, R14, or R15 are independently: hydrogen, halo, alkylhalo, hydroxy, C1-C9 straight or branched chain alkyl, C2-C9 straight or branched chain alkenyl group, C3-C8 cycloalkyl, C5-C7 cycloalkenyl, aryl, amino, alkylamino, nitro, nitroso, carboxy, or aralkyl; R9 is hydrogen, hydroxy, C1-C9 straight or branched chain alkyl, C2-C9 straight or branched chain alkenyl group, C3-C8 cycloalkyl, C5-C7 cycloalkenyl, aryl, amino, alkylamino, carboxy, or aralkyl; R11 or R16 are independently: hydrogen, halo, alkylhalo, hydroxy, C1-C9 straight or branched chain alkyl, C2-C9 straight or branched chain alkenyl group, C3-C8 cycloalkyl, C5-C7 cycloalkenyl, aryl, amino, alkylamino, carboxy, or aralkyl.

    摘要翻译： 本发明涉及化合物，药物组合物和使用下式的化合物或其药学上可接受的盐，水合物，前药或其混合物的方法，其中Y是烷基卤素，烷基-CO-G，COG，直接键，C = O，O，NR11或CR8; G是NR11R16，OR9，SR9或R10; Z是O，S或NR11; X是NR16，O，S，CR12R13，C = O，键，-CR12 = CR13 - ， - C（R 12 R 13）C（R 14 R 15） - 或者; R 1d，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 10，R 12，R 13，R 14或R 15独立地为氢，卤素，烷基卤素 ，羟基，C1-C9直链或支链烷基，C2-C9直链或支链烯基，C3-C8环烷基，C5-C7环烯基，芳基，氨基，烷基氨基，硝基，亚硝基，羧基或芳烷基; R9是氢 ，羟基，C 1 -C 9直链或支链烷基，C 2 -C 9直链或支链烯基，C 3 -C 8环烷基，C 5 -C 7环烯基，芳基，氨基，烷基氨基，羧基或芳烷基; R 11或R 16独立地为氢 卤素，烷基卤素，羟基，C 1 -C 9直链或支链烷基，C C 2 -C 9直链或支链烯基，C 3 -C 8环烷基，C 5 -C 7环烯基，芳基，氨基，烷基氨基，羧基或芳烷基。

    Thio-substituted pentanedioic acid derivatives
    9.
    发明授权
    Thio-substituted pentanedioic acid derivatives 失效
    硫代取代戊二酸衍生物

    公开(公告)号：US06265609B1

    公开(公告)日：2001-07-24

    申请号：US09228391

    申请日：1999-01-12

    申请人： Paul F. Jackson ,  Keith M. Maclin ,  Eric Wang ,  Barbara S. Slusher ,  Rena Lapidus

    发明人： Paul F. Jackson ,  Keith M. Maclin ,  Eric Wang ,  Barbara S. Slusher ,  Rena Lapidus

    IPC分类号： C07C5502

    CPC分类号： C07C323/56 ,  C07C323/52

    摘要： The present invention relate to thio-substituted pentanedioic acid derivatives that inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising the same, and methods of using the same to inhibit NAALADase enzyme activity, to effect neuronal activities, to inhibit angiogenesis, and to treat glutamate abnormalities, compulsive disorders and prostate diseases.

    摘要翻译： 本发明涉及抑制N-乙酰化α链接酸性二肽酶（NAALADase）酶活性的硫代取代戊二酸衍生物，包含其的药物组合物及其用于抑制NAALADase酶活性，影响神经元活性的方法， 抑制血管发生，并治疗谷氨酸异常，强迫症和前列腺疾病。