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    Hydroxyl-containing compounds
    1.
    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。

    Xanthine modulators of metabolism of cellular P-450
    2.
    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。

    Amine substituted compounds
    4.
    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。

    Therapeutic compounds containing xanthinyl
    5.
    发明授权
    Therapeutic compounds containing xanthinyl 失效
    含有黄原素的治疗化合物

    公开(公告)号：US6100271A

    公开(公告)日：2000-08-08

    申请号：US483871

    申请日：1995-06-07

    申请人： J. Peter Klein ,  Alistair J. Leigh ,  Gail E. Underiner ,  Anil M. Kumar

    发明人： J. Peter Klein ,  Alistair J. Leigh ,  Gail E. Underiner ,  Anil M. Kumar

    IPC分类号： C07D239/54 ,  A61K31/42 ,  A61K31/421 ,  A61K31/496 ,  A61K31/505 ,  A61K31/52 ,  A61K31/522 ,  A61P9/10 ,  A61P9/14 ,  A61P11/16 ,  A61P13/02 ,  A61P15/00 ,  A61P25/28 ,  A61P29/00 ,  A61P31/12 ,  A61P31/18 ,  A61P35/00 ,  A61P37/04 ,  A61P37/08 ,  A61P43/00 ,  C07C47/198 ,  C07C47/277 ,  C07C49/175 ,  C07C49/255 ,  C07C57/46 ,  C07C59/64 ,  C07C65/21 ,  C07C69/06 ,  C07C69/14 ,  C07C69/24 ,  C07C69/608 ,  C07C69/612 ,  C07C225/06 ,  C07C233/01 ,  C07D239/56 ,  C07D241/18 ,  C07D263/30 ,  C07D473/04 ,  C07D473/06 ,  C07D473/10 ,  C07D487/04 ,  C07D513/04 ,  C07D521/00

    CPC分类号： C07D487/04 ,  C07D473/04 ,  C07D473/06 ,  C07D473/10 ,  C07D513/04

    摘要： Therapeutic compounds with at least one carboxylic acid, ester or amide-substituted side chain have the formula:CORE MOIETY --(R).sub.jwherein j is an integer from one to three. The core moiety is non-cyclic or cyclic (carbocyclic or heterocyclic). R may be selected from among hydrogen, halogen, hydroxyl, amino, substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(2-10) alkenyl, carbocyclic or heterocyclic groups and at least one R has the formula I: ##STR1## wherein: one or two p are the integer one, otherwise p is two; and n is an integer from three to twenty; R.sub.1 is selected from the group consisting of substituted and unsubstituted CH.sub.2 ; NR.sub.3, R.sub.3 being hydrogen, substituted or unsubstituted C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl or C.sub.(1-20) hydroxyalkyl, or carbocyclic or heterocyclic group; O; --CHR.sub.4 O--, R.sub.4 being substituted or unsubstituted C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl, C.sub.(1-20) hydroxyalkyl, or R.sub.2 and R.sub.4 join to form a substituted or unsubstituted heterocycle having four to seven ring atoms, the ether group --O-- of --CHR.sub.4 O-- being a member of the heterocycle. R.sub.2 is selected from the group consisting of hydrogen; halogen; substituted or unsubstituted C.sub.(1-10) alkyl; C.sub.(1-10) alkoxyl; C.sub.(2-10) alkenyl; C.sub.(1-10) hydroxyallyl; --A(R.sub.5).sub.m, A being N or O, m being one or two and R.sub.5 being hydrogen, a substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(1-10) alkoxyl, C.sub.(2-10) alkenyl or C.sub.(1-10) hydroxyalkyl), or carbocyclic or heterocyclic group. At least one of R.sub.1 is NR.sub.3, O or --CHR.sub.4 O--, or R.sub.2 is --A(R.sub.5).sub.m. The compounds and pharmaceutical compositions thereof are useful as therapies for diseases advanced via intracellular signaling through specific intracellular signaling pathways by mediating a signaling response to an external stimuli.

    摘要翻译： 具有至少一个羧酸，酯或酰胺取代的侧链的治疗化合物具有下式：CORE MOIETY - （R）j，其中j是1至3的整数。 核心部分是非环状或环状的（碳环或杂环）。 R可以选自氢，卤素，羟基，氨基，取代或未取代的C（1-10）烷基，C（2-10）烯基，碳环或杂环基，并且至少一个R具有式I：其中： 或两个p为整数，否则p为2; n为3〜20的整数。 R1选自取代和未取代的CH 2; NR 1，R 3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C（1-20）羟基烷基或碳环或杂环基; O; -CHR4O-，R4是取代或未取代的C（1-20）烷基，C（1-20）烷氧基，C（2-20）烯基，C（1-20）羟基烷基或R2和R4连接形成取代的 或具有4-7个环原子的未取代的杂环，-CHR4O-的醚基-O-是杂环的成员。 R2选自氢; 卤素; 取代或未取代的C（1-10）烷基; C（1-10）烷氧基; C（2-10）烯基; C（1-10）羟基烯基; -A（R5）m，A是N或O，m是一个或两个，R5是氢，取代或未取代的C（1-10）烷基，C（1-10）烷氧基，C（2-10）烯基 或C（1-10）羟烷基）或碳环或杂环基。 R 1中的至少一个为NR 3，O或-CHR 4 O-，或R 2为-A（R 5）m。 这些化合物及其药物组合物可用作通过介导对外部刺激的信号反应的特异性细胞内信号通路的细胞内信号传导的疾病的治疗。

    Amine substituted xanthinyl compounds
    6.
    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
    7.
    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。