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    Beta-hairpin peptidomimetics as CXC4 antagonists
    61.
    发明授权
    Beta-hairpin peptidomimetics as CXC4 antagonists 有权
    β-发夹肽模拟物作为CXC4拮抗剂

    公开(公告)号：US09079939B2

    公开(公告)日：2015-07-14

    申请号：US14124508

    申请日：2012-06-06

    申请人： Daniel Obrecht ,  Frank Otto Gombert ,  Johann Zimmermann

    发明人： Daniel Obrecht ,  Frank Otto Gombert ,  Johann Zimmermann

    IPC分类号： C07K7/08 ,  A61K38/00 ,  C07K7/64 ,  C07K1/04

    CPC分类号： C07K7/08 ,  A61K38/00 ,  C07K1/047 ,  C07K7/64

    摘要： β-Hairpin peptidomimetics of the general formula cyclo(-Tyr1-His2-Xaa3-Cys4-Ser5-Ala6-Xaa7-Xaa8-Arg9-Tyr10-Cys11-Tyr12-Xaa13-Xaa14-DPro15-Pro16-), disulfide bond between Cys4 and Cys11, and pharmaceutically acceptable salts thereof, with Xaa3, Xaa7, Xaa8, Xaa13 and Xaa14 being amino acid residues of certain types which are defined in the description and the claims, have favorable pharmacological properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immunosuppression; or during apheresis collections of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

    摘要翻译： （-Tyr1-His2-Xaa3-Cys4-Ser5-Ala6-Xaa7-Xaa8-Arg9-Tyr10-Cys11-Tyr12-Xaa13-Xaa14-DPro15-Pro16-）的通式肽模拟物，Cys4之间的二硫键 和Cys11及其药学上可接受的盐与在说明书和权利要求书中定义的某些类型的氨基酸残基的Xaa3，Xaa7，Xaa8，Xaa13和Xaa14具有有利的药理学性质并可用于预防健康的HIV感染 个体或减慢和停止感染患者的病毒进展; 或由CXCR4受体活性介导或产生癌症; 或其中免疫性疾病介导或由CXCR4受体活性产生; 或用于治疗免疫抑制; 或在外周血干细胞的分离采集期间和/或作为诱导干细胞动员以调节组织修复的试剂。 这些肽模拟物可以通过基于混合固相和溶液相合成策略的方法制造。

    BETA-HAIRPIN PEPTIDOMIMETICS AS CXC4 ANTAGONISTS
    62.
    发明申请
    BETA-HAIRPIN PEPTIDOMIMETICS AS CXC4 ANTAGONISTS 有权
    作为CXC4拮抗剂的BETA-HAIRPIN PEPTIDOMIMITICS

    公开(公告)号：US20140213509A1

    公开(公告)日：2014-07-31

    申请号：US14124508

    申请日：2012-06-06

    申请人： Daniel Obrecht ,  Frank Otto Gombert ,  Johann Zimmermann

    发明人： Daniel Obrecht ,  Frank Otto Gombert ,  Johann Zimmermann

    IPC分类号： C07K7/08 ,  C07K1/04

    CPC分类号： C07K7/08 ,  A61K38/00 ,  C07K1/047 ,  C07K7/64

    摘要： β-Hairpin peptidomimetics of the general formula cyclo(-Tyr1-His2-Xaa3-Cys4-Ser5-Ala6-Xaa7-Xaa8-Arg9-Tyr10-Cys11-Tyr12-Xaa13-Xaa14-DPro15-Pro16-), disulfide bond between Cys4 and Cys11, and pharmaceutically acceptable salts thereof, with Xaa3, Xaa7, Xaa8, Xaa13 and Xaa14 being amino acid residues of certain types which are defined in the description and the claims, have favorable pharmacological properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immunosuppression; or during apheresis collections of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

    摘要翻译： （-Tyr1-His2-Xaa3-Cys4-Ser5-Ala6-Xaa7-Xaa8-Arg9-Tyr10-Cys11-Tyr12-Xaa13-Xaa14-DPro15-Pro16-）的通式肽模拟物，Cys4之间的二硫键 和Cys11及其药学上可接受的盐与在说明书和权利要求书中定义的某些类型的氨基酸残基的Xaa3，Xaa7，Xaa8，Xaa13和Xaa14具有有利的药理学性质并可用于预防健康的HIV感染 个体或减慢和停止感染患者的病毒进展; 或由CXCR4受体活性介导或产生癌症; 或其中免疫性疾病介导或由CXCR4受体活性产生; 或用于治疗免疫抑制; 或在外周血干细胞的分离采集期间和/或作为诱导干细胞动员以调节组织修复的试剂。 这些肽模拟物可以通过基于混合固相和溶液相合成策略的方法制造。

    BETA-HAIRPIN PEPTIDOMIMETICS
    63.
    发明申请
    BETA-HAIRPIN PEPTIDOMIMETICS 有权

    公开(公告)号：US20130189363A1

    公开(公告)日：2013-07-25

    申请号：US13814398

    申请日：2010-08-05

    申请人： Daniel Obrecht ,  Frank Otto Gombert ,  John Anthony Robinson ,  Krystyna Patora-Komisarska

    发明人： Daniel Obrecht ,  Frank Otto Gombert ,  John Anthony Robinson ,  Krystyna Patora-Komisarska

    IPC分类号： C07K7/54

    CPC分类号： C07K7/54 ,  A01N47/44 ,  C07K7/64

    摘要： β-Hairpin peptidomimetics of the general formula Cyclo (-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13-Xaa14-), enantiomers and pharmaceutically acceptable salts thereof, with Xaa1-Xaa14 being amino acid residues of certain types which are defined in the description and the claims, have anti-infective activity, e.g. to selectively inhibit the growth of or to kill microorganisms such as Bacillus subtilis and/or Shigella boydii. They can be used as medicaments to treat or prevent infections or as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

    摘要翻译： 通式为Xaa1（-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13-Xaa14-）的β-发夹肽模拟物，其对映异构体和药学上可接受的盐， -Xaa14是在说明书和权利要求书中定义的某些类型的氨基酸残基，具有抗感染活性，例如， 选择性地抑制枯草芽孢杆菌和/或志贺氏志贺氏杆菌等生长或杀死微生物。 它们可用作治疗或预防感染的药物，或用作食品，化妆品，药​​物或其他含营养材料的消毒剂。 这些肽模拟物可以通过基于混合固相和溶液相合成策略的方法制造。

    PIPERIDINE/PIPERAZINE DERIVATIVES
    64.
    发明申请
    PIPERIDINE/PIPERAZINE DERIVATIVES 有权
    哌啶/哌嗪衍生物

    公开(公告)号：US20100216809A1

    公开(公告)日：2010-08-26

    申请号：US12663009

    申请日：2008-06-05

    申请人： Jean-Pierre André Marc Bongartz ,  Lieven Meerpoel ,  Gustaaf Maria Boeckx ,  Guy Rosalia Eugeen Van Lommen ,  Christophe Francis Robert Buyck ,  Daniel Obrecht ,  Philipp Ermert ,  Anatol Luther

    发明人： Jean-Pierre André Marc Bongartz ,  Lieven Meerpoel ,  Gustaaf Maria Boeckx ,  Guy Rosalia Eugeen Van Lommen ,  Christophe Francis Robert Buyck ,  Daniel Obrecht ,  Philipp Ermert ,  Anatol Luther

    IPC分类号： A61K31/506 ,  A61K31/496 ,  A61K31/454 ,  C07D403/10 ,  C07D413/10 ,  C07D513/04 ,  C07D487/04 ,  C07D401/10 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P1/16

    CPC分类号： C07D513/04 ,  C07D231/12 ,  C07D239/26 ,  C07D239/42 ,  C07D249/08 ,  C07D249/12 ,  C07D271/06 ,  C07D271/10 ,  C07D271/107 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D487/04

    摘要： The invention further relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —NRx—C(═O)—; —Z—C(═O)—; —Z—NRx—C(═O)—; —S(═O)p-; C(═S)—; —NRx—C(═S)—; —Z—C(═S)—; —Z—NRx—C(═S)—; —O—C(═O)—; —C(═O)—C(═O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5-or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxlyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzo-dioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-membered aromatic heterocycle may optionally be substituted; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.

    摘要翻译： 本发明还涉及式（I）的DGAT抑制剂，其包括其任何立体化学异构形式，其中A表示CH或N; 在A代表碳原子的情况下，虚线代表任意键; X表示-NR x -C（= O） - ; -Z-C（= O） - ; -Z-NRx-C（= O） - ; -S（= O）p-; C（═S） - ; -NR x -C（= S） - ; -Z-C（= S） - ; -Z-NRx-C（= S） - ; -O-C（= O） - ; -C（= O）-C（= O） - ; R1表示含有至少2个杂原子的5元单环杂环; 6元芳族单环杂环; 或含有至少2个与苯基，环己基或5或6元杂环稠合的杂原子的5元杂环; 其中每个所述杂环可任选被取代; R2表示R3; R 3表示C 3-6环烷基，苯基，萘基，2,3-二氢-1,4-苯并二氧杂环己烯基，1,3-苯并二恶唑基，2,3-二氢苯并呋喃基或含1或2个N原子的6元芳族杂环，其中所述C3 6-环烷基，苯基，萘基，2,3-二氢-1,4-苯并二恶基，1,3-苯并二恶唑基，2,3-二氢苯并呋喃基或6-元芳香杂环可以任选被取代; 其N-氧化物，其药学上可接受的盐或其溶剂合物。 本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及用作所述化合物的药物。

    CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS
    68.
    发明申请
    CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS 有权
    一致的约束，全合成大环化合物

    公开(公告)号：US20120270881A1

    公开(公告)日：2012-10-25

    申请号：US13508531

    申请日：2010-08-03

    申请人： Daniel Obrecht ,  Philipp Ermert ,  Said Oumouch ,  Franck Lach ,  Anatol Luther ,  Karsten Marx ,  Kerstin Möhle

    发明人： Daniel Obrecht ,  Philipp Ermert ,  Said Oumouch ,  Franck Lach ,  Anatol Luther ,  Karsten Marx ,  Kerstin Möhle

    IPC分类号： C07D273/02 ,  C07D273/00 ,  A61K31/4985 ,  A61K31/437 ,  A61P1/00 ,  A61P19/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61K31/407 ,  A61P25/06

    CPC分类号： C07D498/04 ,  A61K31/407 ,  A61K31/437 ,  A61K31/4985 ,  C07D497/18 ,  C07D498/18

    摘要： Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of formulae Ia and Ib are constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. These macrocycles Ia and Ib are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being the agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), ion channels and signal transduction pathways. In particular, these macrocycles act as antagonists of the motilin receptor, the FP receptor and the purinergic receptors P2Y1, as modulators of the serotonin receptor of subtype 5-HT2B, as blockers of the voltage-gated potassium channel Kv1.3 and as inhibitors of the β-catenin-dependent “canonical” Wnt pathway. Thus they are showing great potential as medicaments for a variety of diseases.

    摘要翻译： 构型限制，式Ia和Ib的空间限定的12-30元大环环系由三个不同的分子部分构成：模板A，构象调节剂B和桥C.这些大环Ia和Ib容易通过平行合成或组合化学 溶液或固相。 它们被设计为与多种特异性生物靶标类型相互作用，其实例是对G蛋白偶联受体（GPCR），离子通道和信号转导通路的激动或拮抗活性。 特别地，这些大环化合物作为拮抗剂作为拮抗剂，作为5-HT2B亚型的5-羟色胺受体的调节剂作为电压门控钾通道Kv1.3的阻断剂，作为抑制剂，作为拮抗剂受体，FP受体和嘌呤能受体P2Y1 连接蛋白依赖的规范Wnt通路。 因此，它们作为各种疾病的药物具有巨大的潜力。

    Template-fixed peptidomimetics as inhibitors of serine proteases
    69.
    发明授权
    Template-fixed peptidomimetics as inhibitors of serine proteases 有权
    模板固定的肽模拟物作为丝氨酸蛋白酶的抑制剂

    公开(公告)号：US07417024B2

    公开(公告)日：2008-08-26

    申请号：US10498468

    申请日：2001-12-11

    申请人： Daniel Obrecht ,  John Anthony Robinson ,  Anne Descours

    发明人： Daniel Obrecht ,  John Anthony Robinson ,  Anne Descours

    IPC分类号： A61K38/08 ,  A61K38/10 ,  C07K7/06 ,  C07K7/08 ,  C07K7/64

    CPC分类号： C07K7/06 ,  A61K38/00 ,  C07K7/08 ,  C07K7/64

    摘要： Template-fixed β-hairpin peptidomimetics of the general formulae (I), wherein Z is a template-fixed chain of 7 to 11 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or of certain types which, as the remaining symbols in the above formulae, are defined in the description and the claims, and salts thereof, have the property to inhibit proteases, in particular serine proteases. These β-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

    摘要翻译： 通式（I）的模板固定的β-发夹肽模拟物，其中Z是7至11个α-氨基酸残基的模板固定链，其取决于其在链中的位置（从N-末端氨基开始计数 酸）是Gly或Pro，或某些类型，其作为上述式中的其余符号在说明书和权利要求书及其盐中定义，并具有抑制蛋白酶，特别是丝氨酸蛋白酶的性质。 这些β-发夹肽模拟物可以通过基于混合固相和溶液相合成策略的方法制备。