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1.发明申请公开(公告)号：US20080200553A1
公开(公告)日：2008-08-21
申请号：US12102446
申请日：2008-04-14
Applicant: Heinz-Werner KLEEMANN
Inventor： Heinz-Werner KLEEMANN
IPC: A61K31/155 , C07C279/02 , A61P9/10 , A61P35/00
CPC classification number: C07C381/00 , Y10S514/821
Abstract: Pentafluorosulfanylbenzoylguanidines of the formula I and II in which R1 to R4 have the meanings stated in the claims, are suitable as antiarrhythmic medicaments with a cardioprotective component for the prophylaxis of infarction and treatment of infarction and for the treatment of angina pectoris. They also inhibit preventively the pathophysiological processes associated with the development of ischemia-induced damage, especially in the triggering of ischemia-induced cardiac arrhythmias.
Abstract translation: 其中R 1至R 4具有权利要求中所述含义的式I和II的五氟硫烷基苯甲酰基胍适合作为具有用于预防梗死和治疗梗死和用于治疗心绞痛的心脏保护组分的抗心律失常药物。 它们还预防性地抑制与缺血诱导的损伤的发展相关的病理生理过程，特别是在引发缺血诱发的心律失常中。
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2.发明申请PENTAFLUOROSULFANYLBENZOYLGUANIDINES, PROCESS FOR THEIR PREPARATION, USE AS A MEDICAMENT OR DIAGNOSTIC AID, AND MEDICAMENT COMPRISING SAME 有权二苯并呋喃基苯甲酰胺，其制备方法，用作药物或诊断辅助药物，以及包含其的药物公开(公告)号：US20080146673A1
公开(公告)日：2008-06-19
申请号：US11972954
申请日：2008-01-11
Applicant: Heinz-Werner KLEEMANN
Inventor： Heinz-Werner KLEEMANN
IPC: A61K31/155 , C07C277/08 , A01N1/02 , A61P9/10 , A61P41/00 , A61P39/00
CPC classification number: C07C381/00
Abstract: Pentafluorosulfanylbenzoylguanidines of formula I wherein R1 to R4 have the meanings stated in the claims, are suitable, for example, as antiarrhythmic medicaments with a cardioprotective component for the prophylaxis of infarction and treatment of infarction and for the treatment of angina pectoris. They also inhibit preventively the pathophysiological processes associated with the development of ischemia-induced damage, especially in the triggering of ischemia-induced cardiac arrhythmias.
Abstract translation: 其中R 1至R 4具有权利要求中所述含义的式I的五氟硫烷基苯甲酰基胍适用于例如具有用于预防梗塞和治疗梗塞和用于治疗心绞痛的心脏保护组分的抗心律失常药物。 它们还预防性地抑制与缺血诱导的损伤的发展相关的病理生理过程，特别是在引发缺血诱发的心律失常中。
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3.发明申请ACYLAMINO-SUBSTITUTED CYCLIC CARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS 有权ACYLAMINO取代的环状羧酸衍生物及其作为药物的用途公开(公告)号：US20120264790A1
公开(公告)日：2012-10-18
申请号：US13461264
申请日：2012-05-01
Applicant: Josef PERNERSTORFER , Heinz-Werner KLEEMANN , Matthias SCHAEFER , Alena SAFAROVA , Marcel PATEK
Inventor： Josef PERNERSTORFER , Heinz-Werner KLEEMANN , Matthias SCHAEFER , Alena SAFAROVA , Marcel PATEK
IPC: C07C61/40 , C07D231/12 , A61K31/415 , C07D213/82 , A61K31/44 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P7/02 , A61P29/00 , A61P19/02 , A61P13/12 , A61P11/00 , A61P11/06 , A61P37/00 , A61P37/08 , A61P35/04 , A61P3/00 , A61P17/06 , A61P25/00 , A61P17/04 , A61P27/02 , A61P25/18 , A61P25/28 , A61P5/00 , A61P5/16 , A61P17/02 , A61P35/00 , A61K31/196
CPC classification number: C07C235/54 , C07C231/00 , C07C231/02 , C07C235/42 , C07C235/84 , C07C255/50 , C07C255/54 , C07C255/57 , C07C307/10 , C07C317/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/22 , C07C2602/50 , C07D213/16 , C07D213/64 , C07D213/69 , C07D213/81 , C07D213/82 , C07D231/12 , C07D231/18 , C07D305/04 , C07D305/06 , C07D305/08 , C07D309/04 , C07D309/08 , C07D309/14 , C07D313/04 , C07D317/06 , C07D317/68 , C07D317/72 , C07D333/16 , C07D333/32 , C07D335/02 , C07D335/14 , C07D335/18 , C07D493/10
Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
Abstract translation: 本发明涉及式I化合物，其中A，Y，Z，R20至R22和R50具有权利要求中所示的含义，它们是有价值的药物活性化合物。 具体来说，它们是由溶血磷脂酸（LPA）激活的内皮分化基因受体2（Edg-2，EDG2）的抑制剂，也被称为LPA1受体，可用于治疗动脉粥样硬化，心肌的疾病 梗死和心力衰竭。 本发明还涉及制备式I化合物的方法，其用途和包含它们的药物组合物。
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公开(公告)号：US20100016272A1
公开(公告)日：2010-01-21
申请号：US12486117
申请日：2009-06-17
Applicant: Hartmut STROBEL , Paulus WOHLFART , Heinz-Werner KLEEMANN , Gerhard ZOLLER , David William WILL
Inventor： Hartmut STROBEL , Paulus WOHLFART , Heinz-Werner KLEEMANN , Gerhard ZOLLER , David William WILL
IPC: A61K31/4709 , C07D401/06 , C07D267/10 , A61K31/496 , A61K31/553 , A61K31/397 , A61P25/00 , A61P9/00 , A61P3/00
CPC classification number: C07D213/56 , C07D213/64 , C07D213/73 , C07D213/75 , C07D215/12 , C07D233/64 , C07D233/68 , C07D239/26 , C07D277/30 , C07D277/46 , C07D333/24 , C07D333/60 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/06 , C07D417/12
Abstract: The present invention relates to heteroarylacrylamides of the formula I, in which Het, X, Ra, Rb, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
Abstract translation: 本发明涉及式I的杂芳基丙烯酰胺，其中Het，X，Ra，Rb，R 1，R 2和R 3具有权利要求中所示的含义，其调节内皮一氧化氮（NO）合酶的转录并且是有价值的药理学 活性化合物。 具体地，式I化合物上调酶内皮NO合成酶的表达，并且可以在需要增加所述酶的表达或增加的NO水平或降低的NO水平的标准化的条件下应用。 本发明还涉及制备式I化合物的方法，包括它们的药物组合物，以及式I化合物在制备用于刺激内皮NO合成酶表达或用于 治疗包括心血管疾病如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全等各种疾病。
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5.发明申请Ortho-substituted pentafluorosulfanylbenzenes, process for their preparation and their use as valuable synthetic intermediates 有权正构取代的五氟硫基苯，其制备方法及其作为有价值的合成中间体的用途公开(公告)号：US20080091031A1
公开(公告)日：2008-04-17
申请号：US11955501
申请日：2007-12-13
Applicant: Heinz-Werner KLEEMANN , Remo WECK
Inventor： Heinz-Werner KLEEMANN , Remo WECK
IPC: C07D209/44 , C07C235/00 , C07C255/58 , C07C63/04 , C07C69/76
CPC classification number: C07C381/00
Abstract: Pentafluorosulfanyl-benzenes according to Formula (I): a process for their preparation and their use as valuable synthetic intermediates for preparing, for example, medicaments, diagnostic aids, liquid crystals, polymers, pesticides, herbicides, fungicides, nematicides, parasiticides, insecticides, acaricides and arthropodicides.
Abstract translation: 根据式（I）的五氟硫烷基 - 苯：其制备方法及其用作制备例如药物，诊断助剂，液晶，聚合物，农药，除草剂，杀真菌剂，杀线虫剂，杀寄生虫剂，杀虫剂， 杀螨剂和节肢动物杀虫剂。
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Patent Agency Ranking
公开(公告)号：US20130109715A1
公开(公告)日：2013-05-02
申请号：US13715111
申请日：2012-12-14
Applicant: Oliver PLETTENBURG , Katrin LORENZ , Matthias LOEHN , John WESTON , Heinz-Werner KLEEMANN
Inventor： Oliver PLETTENBURG , Katrin LORENZ , Matthias LOEHN , John WESTON , Heinz-Werner KLEEMANN
IPC: C07D417/12 , C07D409/12 , C07D405/12 , C07D217/24 , C07D217/02
CPC classification number: C07D417/12 , C07D217/02 , C07D217/22 , C07D217/24 , C07D405/12 , C07D409/12
Abstract: The invention relates to 6-substituted isoquinoline and isoquinolinone derivatives of the formula (I) t,21useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
Abstract translation: 本发明涉及式（I）t，21的6-取代异喹啉和异喹啉酮衍生物，其用于治疗和/或预防与肌球蛋白轻链磷酸酶的Rho-激酶和/或Rho-激酶介导的磷酸化相关的疾病，以及 含有这些化合物的组合物。
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7.发明申请USE OF INHIBITORS OF THE CELLULAR NA+/H+ EXCHANGER (NHE) FOR PREPARING A MEDICAMENT FOR NORMALIZING SERUM LIPIDS 审中-公开细胞NA + / H +交换子（NHE）的抑制剂用于制备用于正常化血清脂质的药物公开(公告)号：US20090143473A1
公开(公告)日：2009-06-04
申请号：US12364703
申请日：2009-02-03
Applicant: Hans Jochen LANG , Hans-Willi JANSEN , Jan-Robert SCHWARK , Heinz-Werner KLEEMANN , Oliver JUNG , Hans-Ludwig SCHAFER , Wolfgang LINZ , Werner KRAMER , Bernward SCHOLKENS , Eugen FALK
Inventor： Hans Jochen LANG , Hans-Willi JANSEN , Jan-Robert SCHWARK , Heinz-Werner KLEEMANN , Oliver JUNG , Hans-Ludwig SCHAFER , Wolfgang LINZ , Werner KRAMER , Bernward SCHOLKENS , Eugen FALK
IPC: A61K31/165 , A61P7/00
CPC classification number: A61K31/00 , A61K31/155 , A61K31/166 , A61K31/22 , A61K31/365 , A61K2300/00
Abstract: Use of inhibitors of the cellular Na+/H+ exchanger (NHE) for the production of a medicament for the normalization of serum lipids.The active compounds identified as inhibitors of the cellular Na+/H+ exchanger (NHE) are used for the production of a medicament for the normalization of serum lipids.They are used for the production of a medicament for lowering the blood lipid level and illnesses caused thereby, as well as the endothelial dysfunction syndrome and illness caused thereby.
Abstract translation: 使用细胞Na + / H +交换剂（NHE）的抑制剂来制备用于血清脂质标准化的药物。 鉴定为细胞Na + / H +交换体（NHE）的抑制剂的活性化合物用于制备用于血清脂质标准化的药物。 它们用于制备用于降低由此引起的血脂水平和疾病以及由此引起的内皮功能障碍综合征和疾病的药物。
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8.发明申请METHODS FOR THE IMPROVEMENT OF MEMORY AND NEUROLOGICAL FUNCTION COMPRISING THE ADMINISTRATION OF COMPOSITIONS THAT ACT AS INHIBITORS OF THE SODIUM PROTON (NA+ /H+ ) EXCHANGER, SUBTYPE 5 (NHE-5) 审中-公开改进存储器和神经功能的方法，包括作为钠原子（NA + / H +）交换剂，第5类（NHE-5）交换剂的抑制剂的组合物的管理，公开(公告)号：US20080234317A1
公开(公告)日：2008-09-25
申请号：US12046920
申请日：2008-03-12
Applicant: Heinz-Werner KLEEMANN , Hans-Jochen LANG , Uwe HEINELT , Armin HOFMEISTER , Holger GAUL , Ulrich Hendrich SCHROEDER , Klaus REYMANN
Inventor： Heinz-Werner KLEEMANN , Hans-Jochen LANG , Uwe HEINELT , Armin HOFMEISTER , Holger GAUL , Ulrich Hendrich SCHROEDER , Klaus REYMANN
CPC classification number: A61K31/47
Abstract: The present invention comprises the use of pharmaceutical compositions that are effective in the inhibition of the Na+/H+ exchanger, subtype 5 (NHE-5) as inhibitors of cellular NHE-5 enhance long term potentiation (LTP) and are therefore effective in the treatment of memory impairments, dementing disorders, and for improving memory. Particularly suitable for the treatment of neurodegenerative disorders, memory impairments and dementing disorders, and for improving memory, are the following NHE-5 inhibitors of the formula I Wherein the R1-R8 substituents are further defined herein:
Abstract translation: 本发明包括使用有效抑制作为细胞NHE抑制剂的第5型（NHE-5）型的Na + / H + -5增强长期增强（LTP），因此有效治疗记忆障碍，痴呆症和改善记忆。 特别适用于治疗神经变性疾病，记忆障碍和痴呆病症以及改善记忆力，是下列式I的NHE-5抑制剂，其中R1-R8取代基在本文中进一步定义：
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9.发明申请ORTHO-SUBSTITUTED PENTAFLUOROSULFANYL BENZENES, METHOD FOR THE PRODUCTION THEREOF AND THEIR USE AS SYNTHESIS INTERMEDIATES 失效ORTHO替代的PENTAFLUOROSULFANYL BENZENES，其生产方法及其作为合成中间体的用途公开(公告)号：US20070259943A1
公开(公告)日：2007-11-08
申请号：US11684259
申请日：2007-03-09
Applicant: Heinz-Werner KLEEMANN , Remo WECK
Inventor： Heinz-Werner KLEEMANN , Remo WECK
IPC: A61K31/216 , A61K31/10 , A61K31/192 , C07C317/14 , C07D209/44 , A61K31/4015 , A61K31/215
CPC classification number: C07C381/00
Abstract: This invention relates to novel substituted pentafluorosulfanylbenzenes of the formula I: and/or salts thereof as claimed, for use as a synthetic intermediates for preparing medicaments, diagnostic aids, liquid crystals, pesticides, herbicides, fungicides, nematicides, parasiticides, insecticides, acaricides, arthropodicides and polymers.
Abstract translation: 本发明涉及用作制备药物，诊断助剂，液晶，农药，除草剂，杀真菌剂，杀线虫剂，杀寄生物剂，杀虫剂，杀螨剂等的合成中间体的式I的取代五氟硫烷基苯和/或其盐。 杀虫剂和聚合物。
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10.发明申请公开(公告)号：US20110306670A1
公开(公告)日：2011-12-15
申请号：US13217515
申请日：2011-08-25
Applicant: Heinz-Werner KLEEMANN
Inventor： Heinz-Werner KLEEMANN
IPC: A61K31/166 , A61P9/06 , A61P9/10 , C07C233/64 , C07C69/76
CPC classification number: C07C381/00 , Y10S514/821
Abstract: Pentafluorosulfanylbenzoylguanidines of the formula I and II in which R1 to R4 have the meanings stated in the claims, are suitable as antiarrhythmic medicaments with a cardioprotective component for the prophylaxis of infarction and treatment of infarction and for the treatment of angina pectoris.They also inhibit preventively the pathophysiological processes associated with the development of ischemia-induced damage, especially in the triggering of ischemia-induced cardiac arrhythmias.
Abstract translation: 其中R 1至R 4具有权利要求中所述含义的式I和II的五氟硫烷基苯甲酰基胍适合作为具有用于预防梗死和治疗梗死和用于治疗心绞痛的心脏保护组分的抗心律失常药物。 它们还预防性地抑制与缺血诱导的损伤的发展相关的病理生理过程，特别是在引发缺血诱发的心律失常中。
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