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    Isoxazol-3(2H)-one analogs as therapeutic agents
    1.
    发明授权
    Isoxazol-3(2H)-one analogs as therapeutic agents 有权
    异恶唑-3（2H） - 酮类似物作为治疗剂

    公开(公告)号：US08415378B2

    公开(公告)日：2013-04-09

    申请号：US12755010

    申请日：2010-04-06

    申请人： Jonas Boström ,  Leifeng Cheng ,  Tomas Fex ,  Michael Karle ,  Daniel Pettersen ,  Peter Schell

    发明人： Jonas Boström ,  Leifeng Cheng ,  Tomas Fex ,  Michael Karle ,  Daniel Pettersen ,  Peter Schell

    IPC分类号： A01N43/40 ,  A01N43/80 ,  A61K31/445 ,  A61K31/42 ,  C07D401/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D421/00 ,  C07D261/00 ,  C07D307/02 ,  C07D315/00 ,  C07D407/00

    CPC分类号： C07D413/04

    摘要： or a pharmaceutically suitable salt thereof, wherein, R1 and R2 independently are hydrogen, deuterium, aryl, hetero aryl, C1-C8 alkyl, optionally being substituted with one or more substituents independently being R3, R3 is an aryl, hetero aryl, fluorine(s), a C1-C6 alkyl containing one or more fluorine, a C1-C6 alkyl containing one or more deuterium, a C1-C6 alkyl containing hydroxy, the aryl and heteroaryl optionally being substituted with one or more halogen, a fluorinated alkoxy, a fluorinated alkyl, a sulfonyl, one or more deuterium, a C1-6 alkyl, a C1-6 alkoxy, a nitrile, or R3 is a C1-6 alkyl optionally substituted with one or more of the following groups: COOR4, OCOR4, CONR5R6, NR5COR6, OR4; wherein, R4 is a C1-10 alkyl optionally substituted with one or more fluorine, deuterium, alkoxy, arylcarboxylate, alkyl carboxylate; R5 and R6 are independently selected from hydrogen, alkyl or they may together form a 4-8 membered carbon ring; or R1 and R2 form a 3-10 membered carbon ring optionally comprising O or N and optionally substituted with a C1-10 alkyl or aryl, hetero aryl optionally substituted with R3.

    摘要翻译： 或其药学上合适的盐，其中R 1和R 2独立地是氢，氘，芳基，杂芳基，任选被一个或多个取代基独立地被R 3取代的C 1 -C 8烷基，R 3是芳基，杂芳基，氟（ 含有一个或多个氟的C 1 -C 6烷基，含有一个或多个氘的C 1 -C 6烷基，含羟基的C 1 -C 6烷基，任选被一个或多个卤素取代的芳基和杂芳基，氟化烷氧基， 氟化烷基，磺酰基，一个或多个氘，C 1-6烷基，C 1-6烷氧基，腈或R 3是任选被一个或多个下列基团取代的C 1-6烷基：COOR 4，OCOR 4， CONR5R6，NR5COR6，OR4; 其中，R4为任选被一个或多个氟，氘，烷氧基，芳基羧酸酯，羧酸烷基酯取代的C 1-10烷基; R 5和R 6独立地选自氢，烷基或它们可以一起形成4-8元碳环; 或R 1和R 2形成任选地包含O或N并任选被C 1-10烷基或芳基取代的3-10元碳环，任选被R 3取代的杂芳基。

    Solid- and solution-phase synthesis of heparin and other glycosaminoglycans
    3.
    发明申请
    Solid- and solution-phase synthesis of heparin and other glycosaminoglycans 审中-公开

    公开(公告)号：US20050187381A1

    公开(公告)日：2005-08-25

    申请号：US11040834

    申请日：2005-01-21

    申请人： Peter Seeberger ,  Hernan Orgueira ,  Peter Schell

    发明人： Peter Seeberger ,  Hernan Orgueira ,  Peter Schell

    IPC分类号： C07H3/04 ,  C07H3/06 ,  C08B37/00 ,  C07H5/04

    CPC分类号： C07H3/06 ,  C07H3/04 ,  C08B37/0075

    摘要： Described is a modular, general synthetic strategy for the preparation in solution and on a solid support of heparin, heparin-like glycosaminoglycans, glycosaminoglycans and non-natural analogs of each of them. Additionally, the modular strategy provides the basis for the preparation of combinatorial libraries and parallel libraries of defined glycosaminoglycan oligosaccharides. The defined glycosaminoglycan structures may be used in high-throughput screening experiments to identify carbohydrate sequences that regulate a host of recognition and signal-transduction processes. The determination of specific sequences involved in receptor binding holds great promise for the development of molecular tools which will allow modulation of processes underlying viral entry, angiogenesis, kidney diseases and diseases of the central nervous system. Notably, the present invention enables the automated synthesis of glycosaminoglycans in much the same fashion that peptides and oligonucleotides are currently assembled.

    Pyrazole Derivatives as Cb1 Modulators
    4.
    发明申请
    Pyrazole Derivatives as Cb1 Modulators 审中-公开
    吡唑衍生物作为Cb1调节剂

    公开(公告)号：US20080287517A1

    公开(公告)日：2008-11-20

    申请号：US11996115

    申请日：2006-07-17

    申请人： Leifeng Cheng ,  Maria Jonforsen ,  Peter Schell

    发明人： Leifeng Cheng ,  Maria Jonforsen ,  Peter Schell

    IPC分类号： A61K31/415 ,  C07D231/14 ,  A61P9/00 ,  A61P3/00 ,  A61P25/00 ,  A61P37/00

    CPC分类号： C07D231/14 ,  C07D401/12

    摘要： The present invention relates to compounds of formula I wherein R1 represents a group R5O— in which R5 represents a C3-7alkyl group substituted by one or more fluoro or R5 represents a C3-7alkylsulphonyl group which is optionally substituted by one or more fluoro; R2 represents a C1-4alkyl group, hydroxy, fluoro, chloro or cyano wherein each R2 is independently selected when n is >1; R3 represents a) cyclohexyl optionally substituted by one or more of the following: hydroxy, fluoro, amino, mono or diC1-3alkylamino, carboxy or a C1-4alkoxycarbonyl group b) piperidino substituted by one or more hydroxy c) unsubstituted piperidino but only when one of the following applies: R4 represents cyano or R1 represents 3-fluoropropylsulphonyloxy or R1 represents 3,3,3-trifluoropropoxy or R1 represents 3-fluoropropoxy or R2 is methyl d) phenyl substituted by one or more of the following: hydroxy, halo or a C1-4alkyl group e) pyridyl substituted by a C1-4alkyl group or f) a C4-9alkyl group; R4 represents cyano or methyl; and n is 1, 2 or 3 and pharmaceutically acceptable salts thereof and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.

    摘要翻译： 本发明涉及式I化合物，其中R 1表示基团R 5 O-，其中R 5表示C 1 -C 6烷基， 被一个或多个氟或R 5取代的3-7个烷基表示任选被一个或多个氟取代的C 3-7烷基磺酰基; R 2表示C 1-4烷基，羟基，氟，氯或氰基，其中当n是>时独立地选择每个R 2， 1; R 3表示a）任选被以下一个或多个取代的环己基：羟基，氟，氨基，单或二-C 1-3烷基氨基，羧基或C 代表3-氟丙基磺酰氧基或R 1代表3,3,3-三氟丙氧基或R 1代表3-氟丙氧基或R 2是 甲基d）被一个或多个下列基团取代的苯基：羟基，卤素或C 1-4烷基; e）被C 1-4烷基取代的吡啶基 或f）C 4-9烷基; R 4代表氰基或甲基; 和n为1,2或3及其药学上可接受的盐及其制备方法，它们在治疗肥胖症，精神病学和神经障碍中的应用，以及其治疗用途的方法和含有它们的药物组合物。

    Novel Compounds 737
    5.
    发明申请
    Novel Compounds 737 审中-公开
    新型化合物737

    公开(公告)号：US20090023704A1

    公开(公告)日：2009-01-22

    申请号：US12104469

    申请日：2008-04-17

    申请人： Leifeng Cheng ,  Sara Holmqvist ,  Florian Raubacher ,  Peter Schell

    发明人： Leifeng Cheng ,  Sara Holmqvist ,  Florian Raubacher ,  Peter Schell

    IPC分类号： C07D473/04 ,  A61K31/522 ,  A61P1/00

    CPC分类号： C07D473/04 ,  C07D473/06 ,  C07F7/1804

    摘要： The present invention relates to novel xanthine compounds of the general formula (I) wherein R1, R2, R3 and R4 are as defined, having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS).

    摘要翻译： 本发明涉及通式（I）的新颖的黄嘌呤化合物，其中R 1，R 2，R 3和R 4如上定义，具有正变构GABA B受体（GBR）调节剂作用，制备所述化合物的方法及其用途 ，任选地与GABAB激动剂组合，用于抑制短暂的食管下括约肌松弛，用于治疗胃食管反流疾病，以及治疗功能性胃肠道疾病和肠易激综合征（IBS）。

    Solid- and solution-phase synthesis of heparin and other glycosaminoglycans
    6.
    发明授权
    Solid- and solution-phase synthesis of heparin and other glycosaminoglycans 有权
    固相和溶液相合成肝素和其他糖胺聚糖

    公开(公告)号：US06846917B2

    公开(公告)日：2005-01-25

    申请号：US10054724

    申请日：2002-01-22

    申请人： Peter H. Seeberger ,  Hernan Orgueira ,  Peter Schell

    发明人： Peter H. Seeberger ,  Hernan Orgueira ,  Peter Schell

    IPC分类号： C07H3/04 ,  C07H3/06 ,  C08B37/00 ,  C07H13/02 ,  C07H5/04

    CPC分类号： C07H3/06 ,  C07H3/04 ,  C08B37/0075

    摘要： Described is a modular, general synthetic strategy for the preparation in solution and on a solid support of heparin, heparin-like glycosaminoglycans, glycosaminoglycans and non-natural analogs of each of them. Additionally, the modular strategy provides the basis for the preparation of combinatorial libraries and parallel libraries of defined glycosaminoglycan oligosaccharides. The defined glycosaminoglycan structures may be used in high-throughput screening experiments to identify carbohydrate sequences that regulate a host of recognition and signal-transduction processes. The determination of specific sequences involved in receptor binding holds great promise for the development of molecular tools which will allow modulation of processes underlying viral entry, angiogenesis, kidney diseases and diseases of the central nervous system. Notably, the present invention enables the automated synthesis of glycosaminoglycans in much the same fashion that peptides and oligonucleotides are currently assembled.

    摘要翻译： 描述了一种模块化的，一般的合成策略，用于制备溶液和固体支持肝素，肝素样糖胺聚糖，糖胺聚糖和它们各自的非天然类似物。 此外，模块化策略为制备组合文库和定义的糖胺聚糖寡糖的平行文库提供了基础。 所定义的糖胺聚糖结构可用于高通量筛选实验以鉴定调节宿主识别和信号转导过程的碳水化合物序列。 涉及受体结合的具体序列的确定对于分子工具的开发具有很大的希望，这将允许调节病毒进入，血管生成，肾脏疾病和中枢神经系统疾病的过程。 值得注意的是，本发明能够以与肽和寡核苷酸当前组装的大致相同的方式自动合成糖胺聚糖。

    ISOXAZOL-3(2H)-ONE ANALOGS AS THERAPEUTIC AGENTS
    7.
    发明申请
    ISOXAZOL-3(2H)-ONE ANALOGS AS THERAPEUTIC AGENTS 有权
    ISOXAZOL-3（2H） - 作为治疗剂的模拟物

    公开(公告)号：US20100261755A1

    公开(公告)日：2010-10-14

    申请号：US12755010

    申请日：2010-04-06

    申请人： Jonas BOSTRÖM ,  Leifeng Cheng ,  Tomas Fex ,  Michael Karle ,  Daniel Pettersen ,  Peter Schell

    发明人： Jonas BOSTRÖM ,  Leifeng Cheng ,  Tomas Fex ,  Michael Karle ,  Daniel Pettersen ,  Peter Schell

    IPC分类号： A61K31/454 ,  C07D401/04 ,  A61P1/16 ,  A61P9/10 ,  A61P7/04

    CPC分类号： C07D413/04

    摘要： or a pharmaceutically suitable salt thereof, wherein, R1 and R2 independently are hydrogen, deuterium, aryl, hetero aryl, C1-C8 alkyl, optionally being substituted with one or more substituents independently being R3, R3 is an aryl, hetero aryl, fluorine(s), a C1-C6 alkyl containing one or more fluorine, a C1-C6 alkyl containing one or more deuterium, a C1-C6 alkyl containing hydroxy, the aryl and heteroaryl optionally being substituted with one or more halogen, a fluorinated alkoxy, a fluorinated alkyl, a sulfonyl, one or more deuterium, a C1-6 alkyl, a C1-6 alkoxy, a nitrile, or R3 is a C1-6 alkyl optionally substituted with one or more of the following groups: COOR4, OCOR4, CONR5R6, NR5COR6, OR4; wherein, R4 is a C1-10 alkyl optionally substituted with one or more fluorine, deuterium, alkoxy, arylcarboxylate, alkyl carboxylate; R5 and R6 are independently selected from hydrogen, alkyl or they may together form a 4-8 membered carbon ring; or R1 and R2 form a 3-10 membered carbon ring optionally comprising O or N and optionally substituted with a C1-10 alkyl or aryl, hetero aryl optionally substituted with R3.

    摘要翻译： 或其药学上合适的盐，其中R 1和R 2独立地是氢，氘，芳基，杂芳基，任选被一个或多个取代基独立地被R 3取代的C 1 -C 8烷基，R 3是芳基，杂芳基，氟（ 含有一个或多个氟的C 1 -C 6烷基，含有一个或多个氘的C 1 -C 6烷基，含羟基的C 1 -C 6烷基，任选被一个或多个卤素取代的芳基和杂芳基，氟化烷氧基， 氟化烷基，磺酰基，一个或多个氘，C 1-6烷基，C 1-6烷氧基，腈或R 3是任选被一个或多个下列基团取代的C 1-6烷基：COOR 4，OCOR 4， CONR5R6，NR5COR6，OR4; 其中，R4为任选被一个或多个氟，氘，烷氧基，芳基羧酸酯，羧酸烷基酯取代的C 1-10烷基; R 5和R 6独立地选自氢，烷基或它们可以一起形成4-8元碳环; 或R 1和R 2形成任选地包含O或N并任选被C 1-10烷基或芳基取代的3-10元碳环，任选被R 3取代的杂芳基。

    Diazinane Compounds
    8.
    发明申请
    Diazinane Compounds 审中-公开
    二嗪烷化合物

    公开(公告)号：US20090088439A1

    公开(公告)日：2009-04-02

    申请号：US12238937

    申请日：2008-09-26

    申请人： Leifeng Cheng ,  Maria Jonforsen ,  Peter Schell

    发明人： Leifeng Cheng ,  Maria Jonforsen ,  Peter Schell

    IPC分类号： A61K31/4985 ,  C07D475/02 ,  A61P1/04

    CPC分类号： C07D475/02

    摘要： The present invention relates to novel compounds of the general formula (I) wherein R1, R2, R3 and R4 are as defined, having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS).

    摘要翻译： 本发明涉及通式（I）的新化合物，其中R 1，R 2，R 3和R 4如上定义，具有正变构GABA B受体（GBR）调节剂作用，制备所述化合物的方法及其用途， 任选地与GABAB激动剂组合，用于抑制短暂的食管下括约肌松弛，用于治疗胃食管反流疾病，以及治疗功能性胃肠道疾病和肠易激综合征（IBS）。