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1. 发明申请

US20110021480A1 17-beta HSD1 and STS Inhibitors 失效
标题翻译： 17-beta HSD1和STS抑制剂
公开(公告)号：US20110021480A1
公开(公告)日：2011-01-27
申请号：US12892351
申请日：2010-09-28
申请人： Josef Messinger , Heinrich-Hubert Thole , Bettina Husen , Michael Weske , Pasi Koskimies , Lila Pirkkala
发明人： Josef Messinger , Heinrich-Hubert Thole , Bettina Husen , Michael Weske , Pasi Koskimies , Lila Pirkkala
IPC分类号： A61K31/58 , C07J41/00 , C07D295/185 , C07D277/46 , C07D317/58 , C07D213/40 , C07D209/14 , A61K31/566 , A61K31/565 , A61P35/00 , A61P15/00 , A61P13/00 , A61P17/08 , A61P17/10 , A61P3/10 , A61P19/02 , A61P21/04 , A61P25/28 , A61P11/06 , A61P17/02
CPC分类号： C07J43/00
摘要： Substituted steroid compounds which represent selective inhibitors of 17β-hydroxysteroid dehydrogenase type I (17β-HSD1) and, in addition, which may represent inhibitors of the steroid sulfatase, salts thereof, pharmaceutical preparations containing these compounds, and a process for the preparation of these compounds. Also disclosed is a therapeutic method of using such substituted steroid compounds, particularly in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17β-hydroxysteroid dehydrogenase type I and/or steroid sulfatase enzymes and/or requiring lowering of the endogenous 17β-estradiol concentration.
摘要翻译：代表17＆bgr-羟基类固醇脱氢酶I型选择性抑制剂（17＆bgr-HSD1）的替代类固醇化合物，另外还可以代表类固醇硫酸酯酶的抑制剂，其盐，含有这些化合物的药物制剂及其制备方法的这些化合物。还公开了使用这种取代的类固醇化合物的治疗方法，特别是在治疗，抑制，预防或预防类固醇激素依赖性疾病或病症例如类固醇激素依赖性疾病或需要抑制17β-羟基类固醇脱氢酶I 和/或类固醇硫酸酯酶和/或需要降低内源性17β-雌二醇浓度。

2. 发明授权

US07820690B2 Method of treating or inhibiting a non-digestive tract derived abdominal disorder associated with pain using a 5-HT, receptor antagonist 有权
标题翻译：使用5-HT受体拮抗剂治疗或抑制与疼痛相关的非消化道的腹部疾病的方法
公开(公告)号：US07820690B2
公开(公告)日：2010-10-26
申请号：US11080546
申请日：2005-03-16
申请人： Holger Sann
发明人： Holger Sann
IPC分类号： A61K31/437
CPC分类号： A61K31/4184
摘要： A method of treating or inhibiting non-digestive tract derived abdominal disorders associated with pain, in particular interstitial cystitis, chronic pelvic pain syndrome and/or abdominal pain associated with endometriosis, in a patient in need thereof, by administering to the patient a pharmaceutically effective amount of a 5-HT3 receptor antagonist, in particular cilansetron, or a pharmacologically compatible derivative thereof, such as a salt and/or a solvates.
摘要翻译：一种在有需要的患者中治疗或抑制与消化道衍生的腹部疾病有关的疼痛，特别是间质性膀胱炎，与子宫内膜异位症相关的慢性盆腔疼痛综合征和/或腹部疼痛的方法，通过向患者施用药学上有效的 5-HT 3受体拮抗剂的量，特别是西兰司琼或其药理学上相容的衍生物，例如盐和/或溶剂合物。

3. 发明申请

US20100034797A1 Lipase Variants for Pharmaceutical Use 有权
标题翻译：药用脂肪酶变体
公开(公告)号：US20100034797A1
公开(公告)日：2010-02-11
申请号：US12519868
申请日：2007-12-12
申请人： Allan Svendsen , Michael Skjoet , Deborah Yaver , Lars Lehman Hylling Christensen , Signe Eskildsen Larsen , Nina Lundin , Michael Lamsa , Peter Colin Gregory
发明人： Allan Svendsen , Michael Skjoet , Deborah Yaver , Lars Lehman Hylling Christensen , Signe Eskildsen Larsen , Nina Lundin , Michael Lamsa , Peter Colin Gregory
IPC分类号： A61K38/54 , C12N9/20 , C12Q1/34 , A61K38/46
CPC分类号： A61K38/465 , A61K38/47 , A61K38/48 , C12N9/20
摘要： The pharmaceutical use of lipases related to the Thermomyces lanuginosus (Humicola lanuginosa) lipase comprising amino acids 1-269 of SEQ ID NO: 2, optionally in combination with a protease and/or an amylase. Examples of medical indications are: Treatment of digestive disorders, pancreatic exocrine insufficiency (PEI), pancreatitis, cystic fibrosis, diabetes type I, and/or diabetes type II. The lipases of the invention have, e.g., an improved digestion performance in vitro, an improved activity at a pH in the neutral range, an improved stability at low pH, an are stable against protease-degradation, and/or are stable in the presence of pepsin and bile salts. The invention also relates to methods of determining digestion performance in vitro of lipases, as well as to certain novel variants of the lipase of T. lanuginosus.
摘要翻译：与包含SEQ ID NO：2的氨基酸1-269的Thermomyces lanuginosus（Humicola lanuginosa）脂肪酶相关的脂肪酶的药物用途，任选地与蛋白酶和/或淀粉酶组合。医学适应症的例子有：消化系统疾病，胰腺外分泌功能不全（PEI），胰腺炎，囊性纤维化，I型糖尿病和/或II型糖尿病的治疗。本发明的脂肪酶具有例如体外改进的消化性能，在中性范围内的pH值改善的活性，在低pH下的改进的稳定性，对蛋白酶降解是稳定的，和/或在存在时是稳定的的胃蛋白酶和胆汁盐。本发明还涉及确定脂肪酶的体外消化性能的方法以及T.lanuginosus的脂肪酶的某些新颖变体。

4. 发明授权

US07534903B2 Use of amidomethyl-substituted 2-(4-sulfonylamino)-3-hydroxy-3,4-dihydro-2H-chromen-6-yl-compounds in the treatment of cardiac arrhythmia and other disease states 有权
标题翻译：酰胺甲基取代的2-（4-磺酰基氨基）-3-羟基-3,4-二氢-2H-色烯-6-基化合物在治疗心律失常和其他疾病状态中的应用
公开(公告)号：US07534903B2
公开(公告)日：2009-05-19
申请号：US12016798
申请日：2008-01-18
申请人： David Sykes , Brian Moloney , Lester Marrison , Dieter Ziegler , Michael Mlinaric , Christiane Boecker , Reinhard Brueckner , Michael Weske , Klaus Witte , Yvan Fischer
发明人： David Sykes , Brian Moloney , Lester Marrison , Dieter Ziegler , Michael Mlinaric , Christiane Boecker , Reinhard Brueckner , Michael Weske , Klaus Witte , Yvan Fischer
IPC分类号： C07D311/00 , A01N43/08
CPC分类号： C07D407/12 , C07D311/68
摘要： The use of compounds corresponding to formula I: in which R1, R2, R3, R4, R5 and R6 have the meanings given in the description for treating cardiac arrhythmias and other disease states.
摘要翻译：使用对应于式I的化合物：其中R1，R2，R3，R4，R5和R6具有描述中给出的用于治疗心律失常和其他疾病状态的含义。

5. 发明申请

US20080255075A1 SUBSTITUTED ESTRATRIENE DERIVATIVES AS 17BETA HSD INHIBITORS 有权
标题翻译：作为17BETA HSD抑制剂的取代的ESTRATRIENE衍生物
公开(公告)号：US20080255075A1
公开(公告)日：2008-10-16
申请号：US11947025
申请日：2007-11-29
申请人： Josef MESSINGER , Uwe Schoen , Heinrich-Hubert Thole , Bettina Husen , Pasi Koskimies , Mikko Unkila
发明人： Josef MESSINGER , Uwe Schoen , Heinrich-Hubert Thole , Bettina Husen , Pasi Koskimies , Mikko Unkila
IPC分类号： A61K31/58 , C07J43/00 , A61P35/00
CPC分类号： C07J43/00
摘要： Substituted estratriene compounds of formula (I) useful in therapy, especially in the treatment or inhibition of a steroid hormone dependent disorder requiring the inhibition of a 17β-hydroxysteroid dehydrogenase (17β-HSD) type 1, type 2 and/or type 3 enzyme, as well as their salts, pharmaceutical compositions containing such compounds and processes for preparing such compounds.
摘要翻译：可用于治疗，特别是治疗或抑制需要抑制17β-羟类固醇脱氢酶（17β-HSD）1型，2型和/或3型酶的类固醇激素依赖性病症的式（I）化合物的取代雌三烯化合物，以及它们的盐，含有这些化合物的药物组合物和制备这些化合物的方法。

6. 发明授权

US07427611B2 Amidomethyl-substituted 1-(carboxyalkyl)-cyclopentyl-carbonylamino-benzazepine-N-acetic acid compounds, process and intermediate products for their preparation and pharmaceutical compositions containing them 有权
标题翻译：甲基取代的1-（羧基烷基） - 环戊基 - 羰基氨基 - 苯并氮杂-N-乙酸化合物，其制备方法和中间产物以及含有它们的药物组合物
公开(公告)号：US07427611B2
公开(公告)日：2008-09-23
申请号：US11404775
申请日：2006-04-17
申请人： Dagmar Hoeltje , Yvan Fischer , Dieter Ziegler , Michael Weske , Katrin Michaelis , Yasmin Karimi-Nejad , Josef Messinger , Axel Pahl , Constanze Hoefer , Hrissanthi Ikonomidou , Lechoslaw Turski
发明人： Dagmar Hoeltje , Yvan Fischer , Dieter Ziegler , Michael Weske , Katrin Michaelis , Yasmin Karimi-Nejad , Josef Messinger , Axel Pahl , Constanze Hoefer , Hrissanthi Ikonomidou , Lechoslaw Turski
IPC分类号： C07D223/16 , A61K38/05 , A61P9/12
CPC分类号： C07D223/16 , C07D401/12 , C07K5/0222 , C07K5/06139
摘要： Compounds having neutral endopeptidase (NEP) and/or human soluble endopeptidase (hSEP) inhibitory activity corresponding to the formula I, wherein the substituents R1, R2, R3 and R4 have the meanings given in the description and also pharmaceutical compositions containing these compounds, in particular pharmaceutical compositions suitable for treating or inhibiting cardiovascular diseases, sexual dysfunction and/or adverse conditions associated with apoptosis.
摘要翻译：具有对应于式I的中性内肽酶（NEP）和/或人可溶内肽酶（hSEP）抑制活性的化合物，其中取代基R 1，R 2，R SUP > 3和R 4具有说明书中给出的含义，并且还含有这些化合物的药物组合物，特别是适用于治疗或抑制心血管疾病，性功能障碍和/或不利条件的药物组合物与凋亡相关。

7. 发明授权

US07273860B2 Method and pharmaceutical compositions for treating or inhibiting renal dysfunctions, diseases or disorders, particularly in diabetic patients 失效
标题翻译：用于治疗或抑制肾功能异常，疾病或病症，特别是糖尿病患者的方法和药物组合物
公开(公告)号：US07273860B2
公开(公告)日：2007-09-25
申请号：US10988847
申请日：2004-11-16
申请人： Dirk Thormaehlen , Berthold Hocher , Harald Waldeck
发明人： Dirk Thormaehlen , Berthold Hocher , Harald Waldeck
IPC分类号： A61K31/55
CPC分类号： A61K31/55
摘要： Treatment and/or inhibition of renal dysfunction, disease or disorder in larger mammals, and particularly in humans, especially in human patients suffering from diabetes, using benzazepine-N-acetic acid derivatives which contain an oxo-group in the α-position to the nitrogen atom and are substituted in position 3 by a 1-(carboxyalkyl)cyclopentylcarbonylamino radical, and/or salts or biolabile esters or physiologically acceptable solvates thereof, and production of pharmaceutical compositions and products suitable for treatment and/or inhibition of renal dysfunction, disease or disorder, particularly in diabetic patients, but also in patients with syndrome X or in patients with a renal dysfunction, disease and/or disorder, which patients are additionally hypertensive, obese, hyperglycemic and/or subject to a metabolic disorder.
摘要翻译：在大型哺乳动物，特别是人，特别是患有糖尿病的人类患者中，使用含有氧代基的苯并氮杂-N-乙酸衍生物，在α位置的治疗和/或抑制肾功能障碍，疾病或病症氮原子，并且在3位上被1-（羧基烷基）环戊基羰基氨基取代，和/或其盐或生物不稳定酯或其生理学上可接受的溶剂合物，以及适于治疗和/或抑制肾功能障碍的药物组合物和产品的生产或障碍，特别是在糖尿病患者中，而且在患有综合征X或患有肾功能障碍，疾病和/或障碍的患者中，该患者另外是高血压，肥胖，高血糖和/或经历代谢紊乱。

8. 发明授权

US07241770B2 Hydronopol derivatives as agonists on human ORL1 receptors 有权
标题翻译：水诺酮衍生物作为人类ORL1受体的激动剂
公开(公告)号：US07241770B2
公开(公告)日：2007-07-10
申请号：US11007255
申请日：2004-12-09
申请人： Matthias Mentzel , Dania B. Reiche , Reinhard Brückner , Samuel David , Bartholomeus J. Van Steen , Uwe Schön , Daniel Jasserand , Ulf Preuschoff
发明人： Matthias Mentzel , Dania B. Reiche , Reinhard Brückner , Samuel David , Bartholomeus J. Van Steen , Uwe Schön , Daniel Jasserand , Ulf Preuschoff
IPC分类号： A61K31/438 , C07D471/10
CPC分类号： C07D471/10
摘要： The invention relates to a group of hydronopol derivatives which are agonists on human ORL1 (nociceptin) receptors. The invention also relates to the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these novel hydronopol derivatives as an active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which ORL1 receptors are involved.The invention relates to compounds of the general formula (1) wherein the symbols have the meanings as given in the description.
摘要翻译：本发明涉及作为人类ORL1（伤害感受素）受体的激动剂的一组水诺酮衍生物。本发明还涉及这些化合物的制备，含有药理学活性量的这些新型水葫芦醇衍生物中的至少一种作为活性成分的药物组合物，以及这些药物组合物用于治疗其中涉及ORL1受体。本发明涉及通式（1）的化合物，其中符号具有说明书中给出的含义。

9. 发明申请

US20060234994A1 Method and device for concentrating and stabilizing conjugated estrogens from mare urine 失效
标题翻译：从母马尿中浓缩和稳定结合性雌激素的方法和装置
公开(公告)号：US20060234994A1
公开(公告)日：2006-10-19
申请号：US11451472
申请日：2006-06-13
申请人： Juergen Ahnsorge , Ivan Ban , Heinz-Helmer Rasche
发明人： Juergen Ahnsorge , Ivan Ban , Heinz-Helmer Rasche
IPC分类号： A61K31/56 , C07J1/00
CPC分类号： C07J1/00 , C07J75/00
摘要： A method and apparatus for concentrating and stabilizing conjugated estrogens from pregnant mare urine on solid adsorbent supports to obtain a starting material for pharmaceuticals that contain a natural mixture of conjugated estrogen mixtures on cartridges in the vicinity of the horses. The adsorbent cartridges can be loaded at the site of urine collection so it is unnecessary to transport large volumes of urine to a central processing point. The loading process can take continuously over a period of weeks until the column is saturated. The effluent urine remains at the site where facilities for its disposal are available. Only the loaded cartridge is transported, and transport can occur at longer intervals of up to several weeks. The stability of the conjugated estrogens on the adsorber assures there is no risk of decomposition.
摘要翻译：用于从固体吸附剂载体上浓缩和稳定来自怀孕母马的结合雌激素的方法和装置，以获得在马附近的药筒上含有共轭雌激素混合物的天然混合物的药物起始材料。吸收剂盒可以装载在尿液收集部位，因此不需要将大量的尿液运送到中央处理点。加载过程可以持续几周，直到色谱柱饱和。流出的尿液保留在可处置设施的场所。只有装载的墨盒才能运输，运输可能会在更长的间隔内进行，最长可达数周。共轭雌激素对吸附剂的稳定性确保没有分解的危险。

10. 发明授权

US07081451B2 Method and apparatus for concentrating and stabilizing conjugated estrogens from mare urine 失效
公开(公告)号：US07081451B2
公开(公告)日：2006-07-25
申请号：US10112040
申请日：2002-04-01
申请人： Juergen Ahnsorge , Ivan Ban , Heinz-Helmer Rasche
发明人： Juergen Ahnsorge , Ivan Ban , Heinz-Helmer Rasche
IPC分类号： A61K31/56
CPC分类号： C07J1/00 , C07J75/00
摘要： A method and apparatus for concentrating and stabilizing conjugated estrogens from pregnant mare urine on solid adsorbent supports to obtain a starting material for pharmaceuticals that contain a natural mixture of conjugated estrogens as active ingredient. The apparatus is suitable for decentralized concentration and stabilization of conjugated estrogen mixtures on cartridges in the vicinity of the horses. The adsorber cartridges can be loaded at the site of urine collection so it is unnecessary to transport large volumes of urine to a central processing point. The loading process can take continuously over a period of weeks until the column is saturated. The effluent urine remains at the site where facilities for its disposal are available. Only the loaded cartridge is transported, and transport can occur at longer intervals of up to several weeks. The stability of the conjugated estrogens on the adsorber assures there is no risk of decomposition.

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