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    Therapeutic compounds for inhibiting interleukin-12 signaling and methods for using same
    2.
    发明授权
    Therapeutic compounds for inhibiting interleukin-12 signaling and methods for using same 失效
    用于抑制白细胞介素-12信号的治疗化合物及其使用方法

    公开(公告)号：US06774130B2

    公开(公告)日：2004-08-10

    申请号：US09288556

    申请日：1999-04-09

    申请人： J. Peter Klein ,  Stephen J. Klaus ,  Anil M. Kumar ,  Baoqing Gong

    发明人： J. Peter Klein ,  Stephen J. Klaus ,  Anil M. Kumar ,  Baoqing Gong

    IPC分类号： A61K31522

    CPC分类号： C07D473/04 ,  A61K31/00 ,  C07D473/06 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04

    摘要： Novel heterocyclic compounds having a six membered ring structure fused to a five membered ring structure are found to be useful for the treatment and prevention of symptoms or manifestations associated with disorders affected by Interleukin-12 (“IL-12”) intracellular signaling, such as, for example, Th1 cell-mediated disorders. The therapeutic compounds, pharmaceutically acceptable derivatives (e.g., resolved enantiomers, diastereomers, tautomers, salts and solvates thereof) or prodrugs thereof, have the following general formula: Each X, Y and Z are independently selected from a member of the group consisting of C(R3), N, N(R3) and S. Each R1, R2 and R3 is substituted or unsubstituted and is independently selected from a member of the group consisting of hydrogen, halo, oxo, C(1-20)alkyl, C(1-20)hydroxyalkyl, C(1-20)thioalkyl, C(1-20)alkylamino, C(1-20)alkylaminoalkyl, C(1-20)aminoalkyl, C(1-20)aminoalkoxyalkenyl, C(1-20)aminoalkoxyalkynyl, C(1-20)diaminoalkyl, C(1-20)triaminoalkyl, C(1-20)tetraaminoalkyl, C(5-15)aminotrialkoxyamino, C(1-20)alkylamido, C(1-20)alkylamidoalkyl, C(1-20)amidoalkyl, C(1-20)acetamidoalkyl, C(1-20)alkenyl, C(1-20)alkynyl, C(3-8)alkoxyl, C(1-11)alkoxyalkyl, and C(1-20)dialkoxyalkyl.

    摘要翻译： 发现具有与五元环结构稠合的六元环结构的新型杂环化合物可用于治疗和预防与受白细胞介素-12（“IL-12”）影响的紊乱相关的症状或表现， ，例如，Th1细胞介导的疾病。 治疗化合物，药学上可接受的衍生物（例如分解的对映异构体，非对映异构体，互变异构体，其盐和溶剂合物）或其前药具有以下通式：每个X，Y和Z独立地选自C （R 3），N，N（R 3）和S.每个R 1，R 2和R 3是取代或未取代的，并且独立地选自氢，卤素，氧代，C（1-20）烷基，C （1-20）羟基烷基，C（1-20）硫代烷基，C（1-20）烷基氨基，C（1-20）烷基氨基烷基，C（1-20）氨基烷基，C（1-20）氨基烷氧羰基，C（1 （1-20）氨基烷基，C（1-20）四氨基烷基，C（5-15）氨基三烷氧基氨基，C（1-20）烷基酰氨基，C（1-20）烷基氨基烷基，C（1-20） ）烷基酰氨基烷基，C（1-20）酰氨基烷基，C（1-20）乙酰氨基烷基，C（1-20）烯基，C（1-20）炔基，C（3-8）烷氧基，C（1-11）烷氧基烷基 ，和C（1-20）二烷氧基烷基。

    Therapeutic compounds for inhibiting interleukin-12 signals and method for using same
    3.
    发明授权
    Therapeutic compounds for inhibiting interleukin-12 signals and method for using same 失效
    用于抑制白细胞介素-12信号的治疗化合物及其使用方法

    公开(公告)号：US06878715B1

    公开(公告)日：2005-04-12

    申请号：US09544984

    申请日：2000-04-07

    申请人： J. Peter Klein ,  Stephen J. Klaus ,  Anil M. Kumar ,  Baoqing Gong

    发明人： J. Peter Klein ,  Stephen J. Klaus ,  Anil M. Kumar ,  Baoqing Gong

    IPC分类号： A61K31/00 ,  C07D239/54 ,  C07D473/04 ,  C07D473/06 ,  C07D473/10 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04 ,  A61K31/522

    CPC分类号： C07D239/54 ,  A61K31/00 ,  C07D473/04 ,  C07D473/06 ,  C07D473/10 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04

    摘要： Novel heterocyclic compounds having a six membered ring structure fused to a five membered ring structure are found to be useful for the treatment and prevention of symptoms or manifestations associated with disorders affected by Interleukin-12 (“IL-12”) intracellular signaling, such as, for example, Th1 cell-mediated disorders. The therapeutic compounds, pharmaceutically acceptable derivatives (e.g., resolved enantiomers, diastereomers, tautomers, salts and solvates thereof) or prodrugs thereof, have the following general formula: Each X, Y and Z are independently selected from a member of the group consisting of C(R3), N, N(R3) and S. Each R1, R2 and R3 is substituted or unsubstituted and is independently selected from a member of the group consisting of hydrogen, halo, oxo, C(1-20)alkyl, C(1-20)hydroxyalkyl, C(1-20)thioalkyl, C(1-20)alkylamino, C(1-20)alkylaminoalkyl, C(1-20)aminoalkyl, C(1-20)aminoalkoxyalkenyl, C(1-20)aminoalkoxyalkynyl, C(1-20)diaminoalkyl, C(1-20)triaminoalkyl, C(1-20)tetraaminoalkyl, C(5-15)aminotrialkoxyamino, C(1-20)alkylamido, C(1-20)alkylamidoalkyl, C(1-20)amidoalkyl, C(1-20)acetamidoalkyl, C(1-20)alkenyl, C(1-20)alkynyl, C(3-8)alkoxyl, C(1-11)alkoxyalkyl, and C(1-20)dialkoxyalkyl.

    摘要翻译： 发现具有与五元环结构稠合的六元环结构的新型杂环化合物可用于治疗和预防与受白细胞介素-12（“IL-12”）影响的紊乱相关的症状或表现， ，例如，Th1细胞介导的疾病。 治疗化合物，药学上可接受的衍生物（例如分解的对映异构体，非对映异构体，互变异构体，其盐和溶剂合物）或其前药具有以下通式：每个X，Y和Z独立地选自C （R 3），N，N（R 3）和S.每个R 1，R 2和R 3是取代或未取代的，并且独立地选自氢，卤素，氧代，C（1-20）烷基，C （1-20）羟基烷基，C（1-20）硫代烷基，C（1-20）烷基氨基，C（1-20）烷基氨基烷基，C（1-20）氨基烷基，C（1-20）氨基烷氧羰基，C（1 （1-20）氨基烷基，C（1-20）四氨基烷基，C（5-15）氨基三烷氧基氨基，C（1-20）烷基酰氨基，C（1-20）烷基氨基烷基，C（1-20） ）烷基酰氨基烷基，C（1-20）酰氨基烷基，C（1-20）乙酰氨基烷基，C（1-20）烯基，C（1-20）炔基，C（3-8）烷氧基，C（1-11）烷氧基烷基 ，和C（1-20）二烷氧基烷基。

    Hydroxyl-containing compounds
    5.
    发明授权
    Hydroxyl-containing compounds 失效
    含羟基的化合物

    公开(公告)号：US06693105B1

    公开(公告)日：2004-02-17

    申请号：US09361145

    申请日：1999-07-27

    申请人： Gail E. Underiner ,  David Porubek ,  J. Peter Klein ,  Paul Woodson ,  Stephen J. Klaus ,  Anil M. Kumar ,  John Tulinsky

    发明人： Gail E. Underiner ,  David Porubek ,  J. Peter Klein ,  Paul Woodson ,  Stephen J. Klaus ,  Anil M. Kumar ,  John Tulinsky

    IPC分类号： A61K31522

    CPC分类号： C07D209/48 ,  A61K31/00 ,  A61K31/519 ,  A61K31/522 ,  C07C233/91 ,  C07C317/18 ,  C07D211/76 ,  C07D211/88 ,  C07D215/22 ,  C07D239/54 ,  C07D239/88 ,  C07D239/96 ,  C07D295/088 ,  C07D473/04 ,  C07D473/06 ,  C07D473/08 ,  C07D473/10 ,  C07D475/02 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04 ,  Y10T436/147777

    摘要： Disclosed are therapeutic compounds having the formula: (R)j—(CORE MOIETY), including resolved enantiomers, diastereomers, hydrates, salts, solvates or mixtures thereof where j is an integer from one to three. The core moiety is a bicyclic ring structure having at least one heterocyclic ring that contains five to six ring atoms and up to two nitrogen heteroatoms. R is selected from the group consisting of hydrogen, halogen, hydroxyl, amino, substituted or unsubstituted benzyl, C1-6 alkyl or C1-6 alkenyl, and at least one R has the formula I: n is an integer from 1 to 20, at least one of X or Y is —OH. Another of X or Y, which is not —OH, is hydrogen, CH3—, CH3—CH2—, CH3—(CH2)2—or (CH3)2—CH2—, and each W1, W2, and W3 is independently hydrogen, CH3—, CH3—CH2—, CH3—(CH2)2— or (CH3)2—CH2—. The X, Y, W1, W2, or W3 alkyl groups may be unsubstituted or substituted by an hydroxyl, halo or dimethylamino group. The disclosed compounds and therapeutic compositions thereof are useful in treating individuals having a disease or treatment-induced toxicity, mediated by second messenger activity.

    摘要翻译： 公开了具有下式的治疗化合物：包括拆分的对映异构体，非对映异构体，水合物，盐，溶剂合物或其混合物，其中j是1至3的整数。 核心部分是具有至少一个含有5至6个环原子和至多2个氮杂原子的杂环的双环结构。 R选自氢，卤素，羟基，氨基，取代或未取代的苄基，C 1-6烷基或C 1-6烯基，至少一个R具有式I：n为1至20的整数， X或Y中的至少一个是-OH。 不是-OH的X或Y中的另一个是氢，CH 3 - ，CH 3 -CH 2 - ，CH 3 - （CH 2）2 - 或（CH 3）2 -CH 2 - ，并且每个W 1，W 2和W 3独立地是氢 ，CH 3 - ，CH 3 -CH 2 - ，CH 3 - （CH 2）2 - 或（CH 3）2 -CH 2 - 。 X，Y，W1，W2或W3烷基可以是未取代的或被羟基，卤素或二甲基氨基取代。 所公开的化合物及其治疗组合物可用于治疗由第二信使活性介导的患有疾病或治疗诱导的毒性的个体。

    Amine substituted compounds
    7.
    发明授权
    Amine substituted compounds 失效
    胺取代的化合物

    公开(公告)号：US6103730A

    公开(公告)日：2000-08-15

    申请号：US486264

    申请日：1995-06-07

    申请人： J. Peter Klein ,  Gail E. Underiner ,  Anil M. Kumar ,  Lance H. Ridgers

    发明人： J. Peter Klein ,  Gail E. Underiner ,  Anil M. Kumar ,  Lance H. Ridgers

    IPC分类号： C07D239/54 ,  C07D473/04 ,  C07D473/06 ,  C07D487/04 ,  C07D513/04 ,  A61K31/522 ,  C07D473/10

    CPC分类号： C07D239/54 ,  C07D473/04 ,  C07D473/06 ,  C07D487/04 ,  C07D513/04

    摘要： Compounds and pharmaceutical compositions, including resolved enantiomers and/or diastereomers, hydrates, salts, solvates and mixtures thereof, have the formula:CORE MOIETY--(R).sub.jIn these compounds, j is an integer from one to three; the core moiety is a cyclic core, the cyclic core being non-cyclic or at least one five- to seven-member non-heterocyclic ring or heterocycle; and R is selected from the group consisting of amine, hydrogen, halogen, hydroxyl, substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(2-10) alkenyl, cyclic or heterocyclic group or formula I. At least one R having formula I: ##STR1## In formula I, n is an integer from four to twenty; and each R.sub.1 or R.sub.2 is independently hydrogen, substituted or unsubstituted C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl or cyclic or heterocyclic group. The compounds are useful in treating or preventing, for example, sepsis syndrome, hematopoietic or organ toxicity, cancer, viral activity, AIDS and AIDS-related indications, allopecia caused by cytotoxic therapies, and progression of an inflammatory or autoimmune disease.

    摘要翻译： 化合物和药物组合物，包括拆分的对映异构体和/或非对映异构体，水合物，盐，溶剂合物及其混合物，具有下式：CORE MOIETY-（R）j在这些化合物中，j是1至3的整数; 核心部分是环核心，环核心是非环状的或至少一个五至七元的非杂环环或杂环; 并且R选自胺，氢，卤素，羟基，取代或未取代的C（1-10）烷基，C（2-10）烯基，环状或杂环基或式I。至少一个具有式 I：式I中，n为4〜20的整数。 并且每个R 1或R 2独立地为氢，取代或未取代的C 1-20烷基，C（1-20）烷氧基，C（2-20）烯基或环状或杂环基。 该化合物可用于治疗或预防例如败血症综合征，造血或器官毒性，癌症，病毒活性，AIDS和AIDS相关适应症，​​由细胞毒性疗法引起的脱发，以及炎性或自身免疫性疾病的进展。

    Xanthine modulators of metabolism of cellular P-450
    8.
    发明授权
    Xanthine modulators of metabolism of cellular P-450 失效
    细胞P-450代谢的黄嘌呤调节剂

    公开(公告)号：US6075029A

    公开(公告)日：2000-06-13

    申请号：US2345

    申请日：1998-01-02

    申请人： J. Peter Klein ,  Anil M. Kumar ,  Paul Woodson

    发明人： J. Peter Klein ,  Anil M. Kumar ,  Paul Woodson

    IPC分类号： C07D473/04 ,  A61K31/52 ,  C07D473/06 ,  C07D473/10

    CPC分类号： C07D473/04

    摘要： A new class of xanthine compounds, variously substituted at the 1, 3, 7 and 8 positions, is characterized by an ability to modulate the activity of key enzymes involved in drug metabolism. These compounds generally are useful in affecting drug metabolism and, particularly, in extending the circulating half-life of compounds that are metabolized via P-450-mediated pathways.

    摘要翻译： 在1,3,7和8位各种替代的新一类黄嘌呤化合物的特征在于调节参与药物代谢的关键酶的活性的能力。 这些化合物通常可用于影响药物代谢，特别是延长通过P-450介导途径代谢的化合物的循环半衰期。