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    Olefin-substituted long chain xanthine compounds
    11.
    发明授权
    Olefin-substituted long chain xanthine compounds 失效
    烯烃取代的长链黄嘌呤化合物

    公开(公告)号：US5354756A

    公开(公告)日：1994-10-11

    申请号：US3372

    申请日：1993-01-12

    申请人： Gail Underiner ,  David Porubek ,  J. Peter Klein

    发明人： Gail Underiner ,  David Porubek ,  J. Peter Klein

    IPC分类号： C07D473/06 ,  A61K31/52 ,  C07D473/02

    CPC分类号： C07D473/06

    摘要： There is disclosed compounds and pharmaceutical compositions having a xanthine core and one or two hydrocarbon side chains bonded to a ring nitrogen atom, wherein the hydrocarbon side chains are independently a straight chain hydrocarbon having at least one double bond in a carbon chain length of from about 4 to about 18 carbon atoms in length, wherein multiple double bonds are separated from each other by at least three carbon atoms, and wherein the hydrocarbon chain may be substituted by a hydroxyl, halo or dimethylamino group and/or interrupted by an oxygen atom. The compounds lower elevated levels of unsaturated, non-arachidonate phosphatidic acid (PA) and diacylglycerol (DAG) derived from said PA within seconds of the primary stimulus and their contact with cells. The modulatory effect depends on the nature of the target cell and the stimulus applied.

    摘要翻译： 公开了具有与环氮原子键合的黄嘌呤核和一个或两个烃侧链的化合物和药物组合物，其中烃侧链独立地为具有至少一个双键的碳链长度为约 4至约18个碳原子，其中多个双键彼此分开至少三个碳原子，并且其中烃链可以被羟基，卤素或二甲基氨基取代和/或被氧原子中断。 该化合物在主要刺激的几秒钟内和与细胞接触的情况下，降低了源自所述PA的不饱和，非花生四烯酸磷脂酸（PA）和二酰基甘油（DAG）的升高水平。 调节作用取决于靶细胞的性质和应用的刺激。

    Substituted aminoalkyl xanthine compounds
    12.
    发明授权
    Substituted aminoalkyl xanthine compounds 失效
    取代的氨基烷基黄嘌呤化合物

    公开(公告)号：US5340813A

    公开(公告)日：1994-08-23

    申请号：US973804

    申请日：1992-11-09

    申请人： J. Peter Klein ,  Gail Underiner ,  Alistair Leigh

    发明人： J. Peter Klein ,  Gail Underiner ,  Alistair Leigh

    IPC分类号： C07D251/00 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/505 ,  A61K31/517 ,  A61K31/52 ,  A61K31/522 ,  A61P1/00 ,  A61P1/16 ,  A61P3/00 ,  A61P7/00 ,  A61P9/00 ,  A61P13/02 ,  A61P15/00 ,  A61P17/00 ,  A61P31/00 ,  A61P37/00 ,  A61P43/00 ,  C07D213/64 ,  C07D239/54 ,  C07D239/62 ,  C07D239/72 ,  C07D471/02 ,  C07D473/04 ,  C07D473/06 ,  C07D473/08 ,  C07D473/10 ,  C07D473/30

    CPC分类号： A61K31/522 ,  A61K31/52 ,  C07D473/04

    摘要： Compounds of the formula ##STR1## wherein each of one or two R is independently ##STR2## wherein n is an integer from 4 to 18, each R.sub.1 ' and R.sub.2 ' is independently H, alkyl (1-4C) or alkenyl (1-4C); and R.sub.3 ' and R.sub.4 ' are independently H or CH.sub.3 ; and wherein the alkyl or alkenyl may be substituted by a hydroxyl, halo or dimethylamino group and/or interrupted by an oxygen atom, H or alkyl (1-4C), including resolved enantiomers and/or diastereomers and mixtures thereof. Preferably, n is from 6 to 10, R.sub.1 ' and R.sub.2 ' are independently H or methyl and R.sub.3 ' and R.sub.4 ' are H. In particular, the compounds lower elevated levels of unsaturated, non-arachidonate phosphatidic acid (PA) and diacylglycerol (DAG) derived from said PA within seconds of the primary stimulus and their contact with said cells. The modulatory effect depends on the nature of the target cell and the stimulus applied.

    摘要翻译： 式1的化合物，其中一个或两个R各自独立地为其中n为4至18的整数，每个R 1'和R 2'独立地为H，烷基（1-4C）或链烯基（ 1-4C）; 且R 3'和R 4'独立地为H或CH 3; 并且其中所述烷基或链烯基可以被羟基，卤素或二甲基氨基取代和/或被氧原子H或烷基（1-4C）中断，包括拆分的对映异构体和/或非对映异构体及其混合物。 优选地，n为6至10，R 1'和R 2'独立地为H或甲基，且R 3'和R 4'为H.特别地，该化合物降低不饱和，非花生四烯酸酯磷脂酸（PA）和二酰基甘油 DAG），其在主刺激的几秒钟内从所述PA衍生并与所述细胞接触。 调节作用取决于靶细胞的性质和应用的刺激。

    Substituted amino alkyl compounds
    13.
    发明授权
    Substituted amino alkyl compounds 失效
    取代的氨基烷基化合物

    公开(公告)号：US5817662A

    公开(公告)日：1998-10-06

    申请号：US468656

    申请日：1995-06-06

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

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

    IPC分类号： A61K31/522 ,  A61K31/52

    CPC分类号： A61K31/522 ,  Y10S424/824 ,  Y10S424/825

    摘要： Compounds and pharmaceutical compositions thereof comprise the formula: (R)j-(core moiety), including resolved enantiomers and/or diastereomers, hydrates, salts, solvates and mixtures thereof, wherein J is an integer from one to three, the core moiety is non-cyclic or comprises at least one, five- to seven-membered ring structure, R may be selected from the group consisting of hydrogen, halogen, hydroxyl, amino, substituted or unsubstituted benzyl, alkyl (C.sub.1-6) or alkenyl (C.sub.1-6), and at least one R has the formula I: ##STR1## wherein n is an integer from four to eighteen; each R'.sub.1 and R'.sub.2 is independently hydrogen, alkyl (C.sub.1-4) or alkenyl (C.sub.1-4), the alkyl or alkenyl groups being preferably substituted by a halogen, hydroxyl, ketone or dimethylamino group and/or may be interrupted by an oxygen or hydrogen atom or an alkyl (C.sub.1-4) group; and each R'.sub.3 and R'.sub.4 is independently hydrogen or methyl. Preferably, n is an integer from six to ten, R'.sub.1 and R'.sub.2 are independently hydrogen or methyl and R'.sub.3 and R'.sub.4 are hydrogen. The compounds are useful in treating or preventing, for example, sepsis syndrome, hematopoietic or organ toxicity, baldness, hair loss or allopecia caused by cytotoxic therapies, and progression of an inflammatory or autoimmune disease.

    摘要翻译： 化合物及其药物组合物包含式（R）j-（核心部分），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，其中J为1至3的整数，核心部分为 非环状或包含至少一个五元至七元环结构，R可以选自氢，卤素，羟基，氨基，取代或未取代的苄基，烷基（C 1-6）或烯基（C 1 -6），并且至少一个R具有式I：其中n是从4到18的整数; 每个R'1和R'2独立地是氢，烷基（C1-4）或烯基（C1-4），烷基或烯基优选被卤素，羟基，酮或二甲基氨基取代和/或可被中断 通过氧或氢原子或烷基（C 1-4）基团; 并且每个R'3和R'4独立地是氢或甲基。 优选地，n是6至10的整数，R'1和R'2独立地是氢或甲基，R'3和R'4是氢。 该化合物可用于治疗或预防例如败血症综合症，造血或器官毒性，秃发，由细胞毒性治疗引起的脱发或脱发，以及炎性或自身免疫性疾病的进展。

    Substituted amino alkyl compounds
    14.
    发明授权
    Substituted amino alkyl compounds 失效
    取代的氨基烷基化合物

    公开(公告)号：US5889011A

    公开(公告)日：1999-03-30

    申请号：US884037

    申请日：1997-06-27

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

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

    IPC分类号： A61K31/522 ,  C07D473/00 ,  A61K31/52

    CPC分类号： A61K31/522 ,  Y10S424/824 ,  Y10S424/825

    摘要： Compounds and pharmaceutical compositions thereof comprise the formula:(R)j- (core moiety),including resolved enantiomers and/or diastereomers, hydrates, salts, solvates and mixtures thereof, wherein J is an integer from one to three, the core moiety is non-cyclic or comprises at least one, five- to seven-membered ring structure, R may be selected from the group consisting of hydrogen, halogen, hydroxyl, amino, substituted or unsubstituted benzyl, alkyl (C.sub.1-6) or alkenyl (C.sub.1-6), and at least one R has the formula I: ##STR1## wherein n is an integer from four to eighteen; each R'.sub.1 and R'.sub.2 is independently hydrogen, alkyl (C.sub.1-4) or alkenyl (C.sub.1-4), the alkyl or alkenyl groups being preferably substituted by a halogen, hydroxyl, ketone or dimethylamino group and/or may be interrupted by an oxygen or hydrogen atom or an alkyl (C.sub.1-4) group; and each R'.sub.3 and R'.sub.4 is independently hydrogen or methyl. Preferably, n is an integer from six to ten, R'.sub.1 and R'.sub.2 are independently hydrogen or methyl and R'.sub.3 and R'.sub.4 are hydrogen. The compounds are useful in treating or preventing, for example, sepsis syndrome, hematopoietic or organ toxicity, baldness, hair loss or allopecia caused by cytotoxic therapies, and progression of an inflammatory or autoimmune disease.

    摘要翻译： 化合物及其药物组合物包含式（R）j-（核心部分），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，其中J为1至3的整数，核心部分为 非环状或包含至少一个五元至七元环结构，R可以选自氢，卤素，羟基，氨基，取代或未取代的苄基，烷基（C 1-6）或烯基（C 1 -6），并且至少一个R具有式I：其中n是从4到18的整数; 每个R'1和R'2独立地是氢，烷基（C1-4）或烯基（C1-4），烷基或烯基优选被卤素，羟基，酮或二甲基氨基取代和/或可被中断 通过氧或氢原子或烷基（C 1-4）基团; 并且每个R'3和R'4独立地是氢或甲基。 优选地，n是6至10的整数，R'1和R'2独立地是氢或甲基，R'3和R'4是氢。 该化合物可用于治疗或预防例如败血症综合症，造血或器官毒性，秃发，由细胞毒性治疗引起的脱发或脱发，以及炎性或自身免疫性疾病的进展。

    Amine substituted compounds
    16.
    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。

    Amine substituted xanthinyl compounds
    17.
    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
    18.
    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。