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1. 发明授权

US07442717B2 Substituted 2-aminoimidazoles, process for their preparation, their use as medicament or diagnostic aid 失效
标题翻译：取代的2-氨基咪唑，其制备方法，用作药物或诊断辅助剂
公开(公告)号：US07442717B2
公开(公告)日：2008-10-28
申请号：US10771185
申请日：2004-02-03
申请人： Uwe Heinelt , Hans-Jochen Lang , Armin Hofmeister , Klaus Wirth , Hans-Willi Jansen
发明人： Uwe Heinelt , Hans-Jochen Lang , Armin Hofmeister , Klaus Wirth , Hans-Willi Jansen
IPC分类号： A61K31/4168 , C07D233/88
CPC分类号： C07D233/50
摘要： Novel substituted 2-aminoimidazoles of formula I, process for their preparation, their use as medicament or diagnostic aid, and medicament containing them. The compounds of this type are useful in the prevention or treatment of various disorders and can be employed inter alia for renal disorders such as acute or chronic renal failure, for disorders of biliary function, for respiratory disorders such as snoring or sleep apneas or for stroke
摘要翻译：式I的新型取代的2-氨基咪唑，其制备方法，它们作为药物或诊断助剂的用途以及含有它们的药物。这种类型的化合物可用于预防或治疗各种疾病，并且可以特别用于肾脏疾病如急性或慢性肾衰竭，胆汁功能障碍，呼吸障碍如打鼾或睡眠呼吸暂停或中风

2. 发明授权

US06825231B2 Substituted norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics, and a medicament comprising them 失效
标题翻译：取代的降冰片基氨基衍生物，其制备方法，它们作为药物或诊断剂的用途，以及包含它们的药物
公开(公告)号：US06825231B2
公开(公告)日：2004-11-30
申请号：US09734008
申请日：2000-12-12
申请人： Uwe Heinelt , Hans-Jochen Lang , Heinz-Werner Kleemann , Jan-Robert Schwark , Klaus Wirth , Hans-Willi Jansen
发明人： Uwe Heinelt , Hans-Jochen Lang , Heinz-Werner Kleemann , Jan-Robert Schwark , Klaus Wirth , Hans-Willi Jansen
IPC分类号： A61K31335
CPC分类号： C07C317/32 , C07B2200/07 , C07C211/38 , C07C211/49 , C07C215/30 , C07C217/58 , C07C217/60 , C07C217/62 , C07C229/38 , C07C237/30 , C07C255/58 , C07C257/18 , C07C311/37 , C07C323/32 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2603/68
摘要： The application discloses substituted norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics and a medicament comprising them Substituted norbornylamino derivatives having exo-configured nitrogen and an endo-fused five-membered ring of the formula I, or having exo-configured nitrogen and an exo-fused five-membered ring of the formula I a in which R1, R2, R3, R4, R5, A, B, S1, and S2 are as defined in the claims, are highly suitable for use as antihypertensive agents, for reducing or preventing ischemically induced damage, for use as medicaments for surgical interventions for the treatment of ischemias of the nervous system, of stroke and cerebral edema, of shock, of impaired respiratory drive, for the treatment of snoring, as laxatives, as agents against ectoparasites, for the prevention of the formation of biliary calculus, as antiatherosclerotics, as agents against late diabetic complications, carcinomatous disorders, fibrotic disorders, endothelial dysfunction, and organ hypertrophies and hyperplasias. They are inhibitors of the cellular sodium/proton antiporter. They have an influence on serum lipoproteins and can therefore be used for the prophylaxis and regression of atherosclerotic changes.
摘要翻译：本申请公开了取代的降冰片烷基氨基衍生物，其制备方法，它们作为药物或诊断剂的用途，以及包含它们的药物具有外部构型的氮的取代的降冰片烷基氨基衍生物和式I的内部稠合的五元环，或具有外部配置的氮和R 1，R 2，R 3，R 4，R 5，A，B，S 1和S 2如权利要求中所定义的式I ain的外部稠合的五元环非常适合用作抗高血压剂，用于减少或预防缺血性损伤，用作外科手术治疗神经系统缺血，中风和脑水肿，休克，呼吸驱动受损，用于治疗打鼾的药物，作为泻药，作为药物外寄生虫，用于预防胆汁结石的形成，作为抗动脉粥样硬化，作为晚期糖尿病并发症的药剂，癌性疾病，纤维化疾病，en 上皮功能障碍，器官肥厚和增生。它们是细胞钠/质子逆转录酶的抑制剂。它们对血清脂蛋白有影响，因此可用于预防和消除动脉粥样硬化变化。

3. 发明授权

US06737423B2 Substituted heterocyclo-norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics, and medicaments comprising them 失效
标题翻译：取代的杂环降冰片基氨基衍生物，其制备方法，它们作为药物或诊断剂的用途，以及包含它们的药物
公开(公告)号：US06737423B2
公开(公告)日：2004-05-18
申请号：US10020241
申请日：2001-12-18
申请人： Uwe Heinelt , Hans-Jochen Lang , Klaus Wirth , Hans-Willi Jansen
发明人： Uwe Heinelt , Hans-Jochen Lang , Klaus Wirth , Hans-Willi Jansen
IPC分类号： C07D21338
CPC分类号： C07D207/335 , C07D213/38 , C07D231/12 , C07D231/16 , C07D233/56 , C07D233/64 , C07D237/08 , C07D239/26 , C07D241/12 , C07D249/08 , C07D261/18 , C07D277/28 , C07D307/52 , C07D333/20 , C07D333/44
摘要： Substituted heterocyclo-norbornylaminoderivatives having: a) an exo-configuration nitrogen and an endo-fused five-membered ring or six-membered ring of the formula (I) or b) an exo-configuration nitrogen and an exo-fused five-membered ring or six-membered ring of the formula (I a), wherein Rn, Het, A, B and T have the meanings given in the claims. These compounds have a variety of uses. They can be used as antihypertensives, for the reduction or prevention of is chemically induced damage, as pharmaceuticals for surgical interventions, for the treatment of ischemia of the nervous system, including stroke and cerebral edema, for the treatment of ischemia due to shock and disturbed respiratory drive, for the treatment of snoring, as a laxative, as an agent against ectoparasites, for the prevention of gallstone formation, as an antiatherosclerotic, as an agent against diabetic late complications, cancers, fibrotic disorders, endothelial dysfunction, organ hypertrophy, and organ hyperplasia. The compounds of the invention are inhibitors of the cellular sodium-proton antiporter. Additonally, the compounds of the invention influence the serum lipoproteins and can therefore be used for the prophylaxis and the regression of atherosclerotic changes.
摘要翻译：取代的杂环降冰片基氨基衍生物具有：a）外配构型氮和式（I）的内联稠合五元环或六元环，或b）外配构氮和外稠合五元环或式（Ⅰa）的六元环，其中Rn，Het，A，B和T具有权利要求中给出的含义。这些化合物具有多种用途。它们可用作抗高血压药物，用于减少或预防化学诱导的损伤，作为手术干预的药物，用于治疗神经系统缺血，包括中风和脑水肿，用于治疗由于休克和受干扰的局部缺血呼吸驱动，用作治疗打鼾，作为泻药，作为对外寄生虫的药物，用于预防胆结石形成，作为抗动脉粥样硬化，作为抗糖尿病晚期并发症，癌症，纤维化病症，内皮功能障碍，器官肥大的药剂，以及器官增生。本发明的化合物是细胞钠 - 质子逆转录酶的抑制剂。此外，本发明的化合物影响血清脂蛋白，因此可用于预防和消除动脉粥样硬化变化。

4. 发明授权

US08067614B2 N-substituted (benzoimidazol-2-yl)phenylamines, processes for their preparation, their use as a medicament or diagnostic aid, and a medicament comprising them 失效
标题翻译： N-取代的（苯并咪唑-2-基）苯胺，其制备方法，它们作为药物或诊断助剂的用途，以及包含它们的药物
公开(公告)号：US08067614B2
公开(公告)日：2011-11-29
申请号：US12722634
申请日：2010-03-12
申请人： Uwe Heinelt , Hans-Jochen Lang , Armin Hofmeister , Klaus Wirth , Martin Hug
发明人： Uwe Heinelt , Hans-Jochen Lang , Armin Hofmeister , Klaus Wirth , Martin Hug
IPC分类号： A61K31/4184 , C07D235/30
CPC分类号： C07D235/30
摘要： This invention is directed to the compound of formula (I), compositions containing said compounds to inhibit the sodium-proton exchanger of subtype 3 (NHE3) which are useful in the prevention or treatment of various disorders in a patient suffering from a disease state, such as, renal disorders including acute or chronic renal failure, disorders of biliary function and for respiratory disorders such as snoring or sleep apnea or for stroke.
摘要翻译：本发明涉及式（I）化合物，含有抑制亚型3（NHE3）的钠 - 质子交换剂的所述化合物的组合物，其可用于预防或治疗患有疾病状态的患者中的各种疾病，例如包括急性或慢性肾衰竭，胆汁功能障碍和呼吸系统疾病如打鼾或睡眠呼吸暂停或中风的肾脏疾病。

5. 发明授权

US06686384B2 Substituted benzimidazoles, processes for their preparation, their use as medicaments, and medicaments comprising them 失效
标题翻译：取代的苯并咪唑，其制备方法，它们作为药物的用途，以及包含它们的药物
公开(公告)号：US06686384B2
公开(公告)日：2004-02-03
申请号：US10000028
申请日：2001-12-04
申请人： Armin Hofmeister , Uwe Heinelt , Hans-Jochen Lang , Markus Bleich , Klaus Wirth , Michael Gekle
发明人： Armin Hofmeister , Uwe Heinelt , Hans-Jochen Lang , Markus Bleich , Klaus Wirth , Michael Gekle
IPC分类号： A61K314184
CPC分类号： C07D235/30
摘要： The invention relates to the use of compounds of formula I for the production of a medicament for the treatment of illnesses which can be influenced by inhibition of the Na+/H+ exchanger, and to a medicament comprising them: in which R1 to R9 have the meanings shown in the claims.
摘要翻译：本发明涉及式I化合物用于制备可受Na + / H +交换剂的抑制影响的疾病的药物的用途，以及包含它们的药物的用途：其中R 1至R 9具有以下含义：如权利要求中所示。

6. 发明授权

US07790742B2 Substituted 4-phenyltetrahydroisoquinolines, pharmaceutical compositions thereof, methods for their preparation and therapeutic use 有权
标题翻译：取代的4-苯基四氢异喹啉，其药物组合物，其制备方法和治疗用途
公开(公告)号：US07790742B2
公开(公告)日：2010-09-07
申请号：US11680668
申请日：2007-03-01
申请人： Hans-Jochen Lang , Uwe Heinelt , Klaus Wirth , Thomas Licher , Armin Hofmeister
发明人： Hans-Jochen Lang , Uwe Heinelt , Klaus Wirth , Thomas Licher , Armin Hofmeister
IPC分类号： C07D217/00 , A61K31/47
CPC分类号： C07D405/12 , C07D217/14 , C07D401/12
摘要： The present invention relates to substituted 4-phenyltetrahydroisoquinoline compounds of the structure of formula I and pharmaceutical compositions comprising them wherein the R groups are herein defined. These are excellent inhibitors of the sodium-hydrogen exchanger (NHE), in particular of the sodium-hydrogen exchanger of subtype 3 (NHE3). As such these compounds are useful in the treatment of various disorders of the renal and respiratory systems such as acute or chronic renal failure, pulmonary complications, biliary function disorders, respiratory disorders such as snoring or sleep apneas and cardiovascular/central nervous system disorders such as stroke. More specifically, the present invention relates to substituted 4-phenyl-tetrahydroisoquinolines, derivatives thereof and compositions containing them formulated in combination with other compounds which also regulate the intracellular pH environment such as inhibitors of carbonic anhydrase and inhibitors of the transport systems that carry bicarbonate ions, such as of the sodium-bicarbonate co-transporter (NBC) or the sodium-dependent chloride-bicarbonate exchanger.
摘要翻译：本发明涉及式I结构的取代的4-苯基四氢异喹啉化合物和包含它们的药物组合物，其中本文定义了R基团。这些是钠 - 氢交换器（NHE），特别是亚型3（NHE3）的钠 - 氢交换器的优异抑制剂。因此，这些化合物可用于治疗肾脏和呼吸系统的各种疾病，例如急性或慢性肾衰竭，肺并发症，胆汁功能障碍，呼吸系统疾病如打鼾或睡眠呼吸暂停和心血管/中枢神经系统疾病，例如行程。更具体地，本发明涉及取代的4-苯基 - 四氢异喹啉，其衍生物和含有它们的组合物，其与调节细胞内pH环境的其它化合物配制，例如碳酸酐酶抑制剂和携带碳酸氢根离子的运输系统的抑制剂，例如碳酸氢钠共转运体（NBC）或钠依赖性氯化碳 - 碳酸氢盐交换剂。

7. 发明申请

US20050054705A1 N-substituted (benzoimidazol-2-yl) phenylamines, process for their preparation, their use as medicament or diagnostic aid, and medicament comprising them 审中-公开
标题翻译： N-取代（苯并咪唑-2-基）苯胺，其制备方法，它们作为药物或诊断助剂的用途，以及包含它们的药物
公开(公告)号：US20050054705A1
公开(公告)日：2005-03-10
申请号：US10770654
申请日：2004-02-03
申请人： Uwe Heinelt , Hans-Jochen Lang , Armin Hofmeister , Klaus Wirth , Martin Hug
发明人： Uwe Heinelt , Hans-Jochen Lang , Armin Hofmeister , Klaus Wirth , Martin Hug
IPC分类号： C07D235/30 , A61K31/4184
CPC分类号： C07D235/30
摘要： This invention is directed to the compound of formula (I), compositions containing said compounds to inhibit the sodium-proton exchanger of subtype 3 (NHE3) which are useful in the prevention or treatment of various disorders in a patient suffering from a disease state, such as, renal disorders including acute or chronic renal failure, disorders of biliary function and for respiratory disorders such as snoring or sleep apnea or for stroke.
摘要翻译：本发明涉及式（I）化合物，含有抑制亚型3（NHE3）的钠 - 质子交换剂的所述化合物的组合物，其可用于预防或治疗患有疾病状态的患者中的各种疾病，例如包括急性或慢性肾衰竭，胆汁功能障碍和呼吸系统疾病如打鼾或睡眠呼吸暂停或中风的肾脏疾病。

8. 发明申请

US20050009864A1 Substituted 4-phenyltetrahydroisoquinolinium, process for their preparation, their use as a medicament, and medicament containing them 审中-公开
公开(公告)号：US20050009864A1
公开(公告)日：2005-01-13
申请号：US10866843
申请日：2004-06-14
申请人： Armin Hofmeister , Uwe Heinelt , Hans-Jochen Lang , Markus Bleich , Klaus Wirth , Michael Gekle
发明人： Armin Hofmeister , Uwe Heinelt , Hans-Jochen Lang , Markus Bleich , Klaus Wirth , Michael Gekle
IPC分类号： C07D217/18 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , A61K31/47 , C07D217/02
CPC分类号： C07D401/12 , C07D217/18 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The invention relates to compounds of the formula I in which R1 to R9 are as defined herein. In one embodiment, these compounds may be used as antihypertensives, for reducing or preventing ischemia-induced damage, as medicaments for surgical intervention for the treatment of ischemias of the nervous system, of stroke and of cerebral edema, of shock, of impaired respiratory drive, for the treatment of snoring, as laxative, as agent against ectoparasites, to prevent the formation of gallstones, as antiatherosclerotics, agents against late complications of diabetes, cancers, fibrotic disorders, endothelial dysfunction, organ hypertrophies and hyperplasias. In one embodiment, the compounds may be inhibitors of the cellular sodium-proton antiporter and influence serum lipoproteins and thus be used for the prophylaxis and for the regression of atherosclerotic lesions.

9. 发明授权

US07868003B2 Substituted 4-phenyltetrahydroisoquinolines, pharmaceutical compositions comprising them and therapeutic methods for their use 有权
标题翻译：取代的4-苯基四氢异喹啉，包含它们的药物组合物及其使用的治疗方法
公开(公告)号：US07868003B2
公开(公告)日：2011-01-11
申请号：US11776041
申请日：2007-07-11
申请人： Uwe Heinelt , Hans-Jochen Lang , Klaus Wirth , Thomas Licher , Armin Hofmeister
发明人： Uwe Heinelt , Hans-Jochen Lang , Klaus Wirth , Thomas Licher , Armin Hofmeister
IPC分类号： C07D217/12 , A61K31/47
CPC分类号： C07D401/10 , C07D217/18
摘要： The invention relates to substituted 4-phenyltetrahydroisoquinolines of formula I wherein R1-R8, N, W, X and Z are defined herein. These compounds and pharmaceutical compositions comprising them are useful in the treatment of respiratory disorders, sleep apnea, kidney disorders, high blood pressure, hypertension, disorders of the central nervous system and the like.
摘要翻译：本发明涉及式I的取代的4-苯基四氢异喹啉，其中R1-R8，N，W，X和Z如本文所定义。这些化合物和包含它们的药物组合物可用于治疗呼吸障碍，睡眠呼吸暂停，肾脏疾病，高血压，高血压，中枢神经系统疾病等。

10. 发明申请

US20060160873A1 Substituted thiophenes: compositions, processes of making, and uses in disease treatment and diagnosis 有权
公开(公告)号：US20060160873A1
公开(公告)日：2006-07-20
申请号：US11385331
申请日：2006-03-21
申请人： Hans-Jochen Lang , Uwe Heinelt , Armin Hofmeister , Klaus Wirth , Michael Gekle , Markus Bleich
发明人： Hans-Jochen Lang , Uwe Heinelt , Armin Hofmeister , Klaus Wirth , Michael Gekle , Markus Bleich
IPC分类号： A61K31/4178
CPC分类号： C07D409/12 , A61K31/4184 , A61K31/454
摘要： Substituted thiophenes, processes for their preparation, their use as medicament or diagnostic agent. The substituted thiophene derivatives have the following backbone structure: Medicaments comprising compounds of this type are of use for preventing or treating various disorders, such as, respiratory disorders and snoring, acute and chronic disorders, disorders induced by ischemic and/or reperfusion events and by proliferative or fibrotic events, disorders of the central nervous system and lipid metabolism, diabetes, blood coagulation and infection by parasites.

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