利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

23 条记录 (耗时 0.035 秒)

    Amine substituted xanthinyl compounds
    13.
    发明授权
    Amine substituted xanthinyl compounds 失效
    胺取代的黄原胶化合物

    公开(公告)号：US5807861A

    公开(公告)日：1998-09-15

    申请号：US476911

    申请日：1995-06-07

    申请人： J. Peter Klein ,  Gail E. Underiner ,  Anil M. Kumar ,  Lance H. Ridgers ,  Glenn C. Rice ,  David W. Leung

    发明人： J. Peter Klein ,  Gail E. Underiner ,  Anil M. Kumar ,  Lance H. Ridgers ,  Glenn C. Rice ,  David W. Leung

    IPC分类号： C07D239/54 ,  C07D473/04 ,  C07D473/06 ,  C07D487/04 ,  C07D513/04 ,  A61K31/52

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

    摘要： A method for treating a disease caused by an undesirable cell response mediated by a proliferative intracellular signaling pathway is provided wherein an effective amount of a compound is administered. The compound, resolved enantiomers, diastereomers, hydrates, salts, solvates and mixtures thereof, has the formula CORE MOIETY--(R).sub.j wherein j is an integer from one to three; the core moiety is xanthinyl; and R is independently selected from the group consisting of amine, hydrogen, halogen, hydroxyl, C.sub.(1-10) alkyl, C.sub.(2-10) alkenyl, 2-bromopropyl, 4-chloropentyl, cyclohexyl, cyclopentyl, 3-dimethylaminobutyl, 2-hydroxyethyl, 5-hydroxyhexyl, 3-hydroxy-n-butyl, 3-hydroxypropyl, 2-methoxyethyl, 4-methoxy-n-butyl, phenyl, and formula I, at least one R comprising formula I ##STR1## wherein (CH.sub.2).sub.n is optionally substituted; n is an integer from five to twenty; each R.sub.1 or R.sub.2 is independently hydrogen or an optionally substituted group that is herein defined; and wherein, when the (CH.sub.2).sub.n, R.sub.1 or R.sub.2 is substituted, a substituent is selected from the group consisting of carbamoyl, primary, secondary and tertiary amino, C.sub.(2-8) alkenyl, C.sub.(1-8) alkyl, C.sub.(1-8) alkoxyl, C.sub.(1-8) hydroxyalkyl, azido, carbonato, carbonyl, carboxyl, cyano, C.sub.(1-8) haloalkyl, isocyano, isomercaptocyano, phospho, phosphonato, sulfonato, alkylsulfonyl, alkylsulfoxidyl, mercaptocarbonyl, mercaptocarbonato, thioureido and ureido.

    摘要翻译： 提供了治疗由增殖性细胞内信号传导途径介导的不良细胞应答引起的疾病的方法，其中施用有效量的化合物。 化合物，拆分的对映体，非对映异构体，水合物，盐，溶剂合物及其混合物具有式CORE MOIETY-（R）j，其中j是1至3的整数; 核心部分是xanthinyl; 并且R独立地选自胺，氢，卤素，羟基，C（1-10）烷基，C（2-10）烯基，2-溴丙基，4-氯戊基，环己基，环戊基，3-二甲基氨基丁基， 2-羟基乙基，5-羟基己基，3-羟基 - 正丁基，3-羟基丙基，2-甲氧基乙基，4-甲氧基 - 正丁基，苯基和式I，至少一个R包括式I其中 （CH 2）n任选被取代; n是从5到20的整数; 每个R 1或R 2独立地为氢或本文定义的任选取代的基团; 并且其中当（CH 2）n，R 1或R 2被取代时，取代基选自氨基甲酰基，伯，仲和叔氨基，C（2-8）烯基，C（1-8）烷基， C（1-8）烷氧基，C（1-8）羟基烷基，叠氮基，碳酸根，羰基，羧基，氰基，C（1-8）卤代烷基，异氰基，异构体巯基，磷酸根，膦酸根，磺酸根，烷基磺酰基，烷基亚砜基，巯基羰基， 巯基羰基，硫脲基和脲基。

    Amine substituted compounds
    14.
    发明授权
    Amine substituted compounds 失效
    胺取代的化合物

    公开(公告)号：US5801182A

    公开(公告)日：1998-09-01

    申请号：US485777

    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 ,  A61K31/505 ,  C07D239/02

    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.j In 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化合物。至少一种具有式 I： I在式I中，n是4至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。

    Therapeutic compounds for inhibiting interleukin-12 signals and method for using same
    19.
    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
    20.
    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。