3,5-Substituted benzoylguanidines, process for their preparation, their
use as a medicament of diagnostic and medicament containing them
    2.
    发明授权
    3,5-Substituted benzoylguanidines, process for their preparation, their use as a medicament of diagnostic and medicament containing them 失效
    3,5-取代的苯甲酰胍,其制备方法,它们作为含有它们的诊断药物和药物的用途

    公开(公告)号:US5373024A

    公开(公告)日:1994-12-13

    申请号:US15926

    申请日:1993-02-10

    摘要: Benzoylguanidines of the formula I ##STR1## are described where R(1) is R(4)--SO.sub.m or R(5)R(6)N--SO.sub.z --, where R(4) and R(5) are alk(en)yl or --C.sub.n H.sub.2n --R(7), and where R(7) is a cycloalkyl or phenyl, where R(5) also has the meaning of H, and R(6) is H or C.sub.1 -C.sub.4 -alkyl, R(2) is hydrogen, halogen, alkyl, O--(CH.sub.2).sub.m C.sub.p F.sub.2p+1, --X--R(10), where X is O, S or NR(11), R(10) is H, (cyclo)alkyl(methyl) or --C.sub.n H.sub.2n --R(12) where R(12) is phenyl, and R(3) is defined, inter alia, as R(1), and their pharmaceutically tolerable salts.The compounds I are obtained by reaction of compounds of the formula II ##STR2## with guanidine, in which L is a leaving group which can be easily nucleophilically substituted.Compounds I are outstandingly suitable as antiarrythmic pharmaceuticals having a cardioprotective component for infarct prophylaxis and infarct treatment and for the treatment of angina pectoris, where they also preventively inhibit or greatly reduce the pathophysiological processes during the formation of ischemically induced damage. They are moreover distinguished by strong inhibitory action on the proliferation of cells. They can therefore be used as antiatherosclerotics, agents against late-onset diabetic complications, cancers, and fibrotic diseases such as pulmonary fibrosis, fibrosis of the liver or fibrosis of the kidneys.They are effective inhibitors of the cellular sodium/proton antiporter (Na.sup.+ /H.sup.+ exchanger).

    摘要翻译: 其中R(1)为R(4)-SOm或R(5)R(6)N-SOz-,其中R(4)和R(5)为 烷基(烯)或-C n H 2n-R(7),其中R(7)为环烷基或苯基,其中R(5)也为H,R(6)为H或C 1 -C 4 - 烷基,R(2)为氢,卤素,烷基,O-(CH2)mCpF2p + 1,-XR(10)其中X为O,S或NR(11),R(10)为H,(环) 烷基(甲基)或-CnH2n-R(12)其中R(12)为苯基,R(3)特别定义为R(1)及其药学上可耐受的盐。 化合物I通过式II化合物(II)与胍反应而获得,其中L是可容易地亲核取代的离去基团。 化合物I非常适合作为具有用于梗死预防和梗塞治疗的心脏保护组分和用于治疗心绞痛的抗焦虑药物,其中它们还预防性地抑制或大大降低在缺血诱导的损伤形成期间的病理生理过程。 此外,它们通过对细胞增殖的强抑制作用而不同。 因此,它们可以用作抗动脉粥样硬化,抗晚发性糖尿病并发症,癌症和纤维化疾病如肺纤维化,肝纤维化或肾纤维化的药物。 它们是细胞钠/质子反转录酶(Na + / H +交换剂)的有效抑制剂。

    SGK1 AS DIAGNOSTIC AND THERAPEUTIC TARGET
    3.
    发明申请
    SGK1 AS DIAGNOSTIC AND THERAPEUTIC TARGET 审中-公开
    SGK1作为诊断和治疗目标

    公开(公告)号:US20120149765A1

    公开(公告)日:2012-06-14

    申请号:US13315850

    申请日:2011-12-09

    申请人: Florian Lang

    发明人: Florian Lang

    CPC分类号: C12Q1/485

    摘要: The invention relates to the utilization of a substance for diagnostic determination of sgk1 (serum and glucocorticoid dependent kinase 1) and to the utilization of an active agent in order to influence sgk1 for therapeutic treatment of diseases associated with disordered activity of the tissue factor and to a diagnostic kit related to such substances or such active agents.

    摘要翻译: 本发明涉及用于sgk1(血清和糖皮质激素依赖性激酶1)的诊断测定的物质的利用和活性剂的利用,以影响sgk1用于治疗与组织因子的无序活性相关的疾病的治疗,以及 与这些物质或这种活性剂相关的诊断试剂盒。

    Mandelic hydrazides
    7.
    发明授权
    Mandelic hydrazides 失效
    扁豆酰肼

    公开(公告)号:US07776920B2

    公开(公告)日:2010-08-17

    申请号:US12279227

    申请日:2007-01-18

    IPC分类号: C07C243/38 A61K31/166

    CPC分类号: C07C243/38

    摘要: Novel mandelic hydrazides of the formula (I), in which R1-R11 have the meanings indicated in claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and complaints, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in fibroses and inflammatory processes of any type.

    摘要翻译: 式(I)的新型扁桃酸酰肼,其中R 1 -R 11具有权利要求1所述的含义,是SGK抑制剂,可用于治疗SGK诱发的疾病和投诉,例如糖尿病,肥胖症,代谢综合征 血脂异常),全身和肺高血压,心血管疾病和肾脏疾病,通常在任何类型的纤维和炎症过程中。

    Strap for snowboard boots or bindings

    公开(公告)号:US07766364B2

    公开(公告)日:2010-08-03

    申请号:US12392583

    申请日:2009-02-25

    IPC分类号: A63C9/00 A63C9/06

    摘要: A binding or boot strap is provided that allows a rider to easily, rapidly and/or effectively tighten and/or loosen the strap about his or her boot. The strap includes a boot-engaging strap portion that engages with an engagement strap coupleable to the boot, as may be the case with boots used for step-in bindings, or to the binding, as may be the case with strap-type bindings. An arrangement for facilitating tightening/loosening of the two strap pieces so that a rider can slip his or her foot into or out from the boot or fasten the boot to or loosen it from a snowboard binding is also provided. In one embodiment, this arrangement includes a tightening element, such as for example a cord, lace or strap, suitably coupled to one or both strap portions such that a rider can pull on the tightening element to move the strap pieces relative to each other and tighten the strap. The tightening arrangement may be configured with a mechanical advantage whereby the force applied to the tightening element results in a greater force applied to the strap. To take up any excess amount of tightening element after the strap has been tightened, a retraction device, such as a self-winding spool, may be utilized. To separate the strap from the boot or binding, a hook and catch arrangement may be employed.

    LACE SYSTEM FOR FOOTWEAR
    10.
    发明申请
    LACE SYSTEM FOR FOOTWEAR 审中-公开
    鞋类系统

    公开(公告)号:US20090019734A1

    公开(公告)日:2009-01-22

    申请号:US12233070

    申请日:2008-09-18

    IPC分类号: A43B5/04

    摘要: A snowboard boot incorporating techniques for making the process of tightening and loosening the laces of a snowboard boot more convenient for the wearer is disclosed. The snowboard boot may be provided with at least two independent lacing zones, the tensions of which are separately adjustable by the wearer. The zones may be secured by pulling on two laces, each of which tightens one of the two independent lacing zones. This arrangement allows the wearer to simultaneously tighten each zone, providing the wearer with the “feel” as though he or she is tightening a conventional single lacing zone snowboard boot. The laces may be simultaneously, yet independently secured by a lace lock at the upper and/or forward region of the snowboard boot. Slack may be created to facilitate loosening of the snowboard boot and easy removal of a foot from the snowboard boot by unhooking the lace from the lace guide without a corresponding distance of lace traveling through the lace lock. A release strap, graspable by the wearer, facilitates unhooking the lace.

    摘要翻译: 公开了一种包含用于使紧固和松动对于穿着者更方便的滑雪板护套的鞋带的过程的滑雪靴。 滑雪靴可以设置有至少两个独立的鞋带区,其张力可由穿着者单独调节。 这些区域可以通过拉两个鞋带来固定,每个鞋带收紧两个独立鞋带区中的一个。 这种布置允许佩戴者同时收紧每个区域,为佩戴者提供“感觉”,就好像他或她正在收紧传统的单一系带区滑雪靴。 鞋带可以同时地,但是通过在滑雪板靴的上部和/或前部区域处的花边锁独立地固定。 可以创建松弛以便于滑雪靴的松动,并且通过从蕾丝引导件脱钩花边而不使蕾丝行进通过花边锁的相应距离,从而容易地从雪靴靴中移除脚。 由佩戴者掌握的释放带有助于脱钩蕾丝。