摘要:
3,4,5-Substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic and medicament containing them Benzoylguanidines of the formula I ##STR1## where R(1) is R(4)--SO.sub.m or R(5)R(6)N--SO.sub.2 --, where R(4) and R(5) are alk(en)yl, --C.sub.n H.sub.2n --R(7), and where R(7) is cycloalkyl or phenyl, where R(5) is also H, R(6) is H or C.sub.1 --C.sub.4 --alkyl, R(2) is hydrogen, (cyclo)-alk(en)(yn)yl, aryl and hetaryl, R(3) is defined as R(2) and their pharmaceutically tolerable salts are described.
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。
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:
Novel difluorophenyldiacylhydrazide derivatives of the formula I, in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in claim 1, are kinase inhibitors and can be used for the treatment of diseases and complaints such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in any type of fibroses, inflammatory processes, tumours and tumour diseases
摘要:
Novel oxadiazole derivatives of the formula (I), in which R, R′, Y, X1, X2 and X3 have the meanings indicated in claim 1, are kinase inhibitors and can be used for the treatment of diseases and conditions such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, in general in all types of fibroses, inflammatory processes, tumours and tumour diseases.
摘要:
Novel 3-aminoindazoles of the formula (I) are SGK inhibitors and can be used for the treatment of SGK-induced diseases and conditions, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and renal diseases, generally in fibrosis and inflammatory processes of any type.
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:
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.
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:
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.