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81. 发明申请

US20160230155A1 MODIFIED SULFAMIDASE AND PRODUCTION THEREOF 有权
标题翻译：改性磺化酶及其生产
公开(公告)号：US20160230155A1
公开(公告)日：2016-08-11
申请号：US14806504
申请日：2015-07-22
申请人： SWEDISH ORPHAN BIOVITRUM AB (PUBL)
发明人： Charlotta BERGHARD , Erik NORDLING , Stefan Svensson GELIUS , Agneta TJERNBERG
IPC分类号： C12N9/14 , C12N9/96
CPC分类号： C12N9/14 , A61K38/00 , C12N9/96 , C12Y310/01001
摘要： Disclosed herein are a modified sulfamidase, a composition comprising a modified sulfamidase, as well as methods for preparing a modified sulfamidase and therapeutic use of such a sulfamidase. In particular, the present disclosure relates to a modified sulfamidase comprising substantially no epitopes for glycan recognition receptors, thereby enabling transportation of said sulfamidase across the blood brain barrier of a mammal, wherein said sulfamidase has catalytic activity in the brain of said mammal.
摘要翻译：本文公开了修饰的磺酰胺酶，包含改性的磺酰胺酶的组合物，以及制备修饰的磺酰胺酶的方法和这种磺酰胺酶的治疗用途。具体地说，本公开内容涉及基本上不含聚糖识别受体的表位的修饰的磺酰胺酶，从而使所述磺酰胺酶能够跨过哺乳动物的血脑屏障传递，其中所述的磺酰胺酶在所述哺乳动物的脑中具有催化活性。

82. 发明授权

US08986682B2 Method to increase the absorption of unsaturated fatty acids by human infants 有权
标题翻译：增加人类不饱和脂肪酸吸收的方法
公开(公告)号：US08986682B2
公开(公告)日：2015-03-24
申请号：US13278682
申请日：2011-10-21
申请人： Olle Hernell , Birgitta Olsson , Patrik Strömberg , Lennart Svensson , Kristina Timdahl , Mårten Vågerö , Maria Öhman
发明人： Olle Hernell , Birgitta Olsson , Patrik Strömberg , Lennart Svensson , Kristina Timdahl , Mårten Vågerö , Maria Öhman
IPC分类号： A61P27/02 , C12N9/20 , A23C9/20 , A23L1/03 , A23L1/29 , A61K38/46 , A23C9/12
CPC分类号： A61K38/465 , A23C9/1216 , A23C9/206 , A23L29/06 , A23L33/12 , A23L33/40 , A23V2002/00 , C12Y301/01003 , A23V2200/08 , A23V2250/54 , A23V2300/50
摘要： The present invention relates to a method to increase the absorption by a human infant of at least one unsaturated fatty acid, said method comprising the enteral administration to said infant of recombinant human bile-salt-stimulated lipase (rhBSSL). In another aspect the invention also relates to a method to improve the visual and/or cognitive development of a human infant, said method comprising the enteral administration to said infant of rhBSSL. Such methods have particular utility for preterm human infants, particular those in medical need of increasing their absorption of or availability to such unsaturated fatty acids. In further aspects, the invention relates to kits, packaged-pharmaceutical-products, recombinant human bile-salt-stimulated lipase and pharmaceutical compositions, in each case useful for increasing the absorption by a human infant of at least one unsaturated fatty acid, or for increasing the visual and/or cognitive development of a human infant.
摘要翻译：本发明涉及一种增加人类婴幼儿至少一种不饱和脂肪酸吸收的方法，所述方法包括向所述婴儿重组人胆汁盐刺激的脂肪酶（rhBSSL）进行肠内施用。在另一方面，本发明还涉及一种改善人类婴儿的视觉和/或认知发育的方法，所述方法包括对所述婴儿的rhBSSL的肠内施用。这些方法对于早产儿的婴儿具有特别的用途，特别是在医学上需要增加其对这种不饱和脂肪酸的吸收或可用性的这些方法。在另外的方面，本发明涉及试剂盒，包装的药物产品，重组人胆汁盐刺激的脂肪酶和药物组合物，在每种情况下都可用于增加人类婴幼儿至少一种不饱和脂肪酸的吸收，或用于增加人类婴儿的视觉和/或认知发育。

83. 发明授权

US08410113B2 (2R)-1-(3-chloro-2-pyrazinyl)-2-methylpiperazine and salts thereof 失效
标题翻译：（2R）-1-（3-氯-2-吡嗪基）-2-甲基哌嗪及其盐
公开(公告)号：US08410113B2
公开(公告)日：2013-04-02
申请号：US13234555
申请日：2011-09-16
申请人： Magnus Cernerud , Helena Lundström , Claes Löfström , Margit Pelcman , Alexander Paptchikhine , Emma Andersson , Alf Nygren , Bruce Fleck
发明人： Tom Fleck , Magnus Cernerud , Helena Lundström , Claes Löfström , Margit Pelcman , Alexander Paptchikhine , Emma Andersson , Alf Nygren
IPC分类号： C07D241/02 , C07D403/00
CPC分类号： C07D401/14 , C07D401/12
摘要： The present invention relates to a process for the preparation of compounds which are therapeutically active in the central nervous system.In one aspect, the invention relates to a process for the preparation of compounds of the general formula (I): wherein HA is a pharmaceutically acceptable acid and R1-R4 are each independently selected from the group consisting of hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, and di-C1-C6-alkylamino-C2-C6-alkoxy. The invention also relates to the use of said compound to manufacture a medicament for the treatment of a serotonin-related disorder.
摘要翻译：本发明涉及一种制备在中枢神经系统中具有治疗活性的化合物的方法。一方面，本发明涉及制备通式（I）的化合物的方法：其中HA是药学上可接受的酸，R 1 -R 4各自独立地选自氢，卤素，C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基和二-C 1 -C 6烷基氨基-C 2 -C 6 - 烷氧基。本发明还涉及所述化合物在制备用于治疗5-羟色胺相关病症的药物中的用途。

84. 发明授权

US08304387B2 Therapeutic formulations of keratinocyte growth factor 有权
标题翻译：角质形成细胞生长因子的治疗剂型
公开(公告)号：US08304387B2
公开(公告)日：2012-11-06
申请号：US11302033
申请日：2005-12-12
申请人： Michael J. Treuheit , Vasumathi Dharmavaram , Judith Purtell , Suzanne E. Roy
发明人： Michael J. Treuheit , Vasumathi Dharmavaram , Judith Purtell , Suzanne E. Roy
IPC分类号： A61K38/18 , A61K38/00 , A61P1/04 , A61P17/02
CPC分类号： A61K9/19 , A61K38/1825 , A61K47/183 , A61K47/26 , C07K14/50
摘要： The present invention provides long-term stable formulations of lyophilized keratinocyte growth factor and methods for making a lyophilized composition comprising keratinocyte growth factor.
摘要翻译：本发明提供了冻干角化细胞生长因子的长期稳定制剂和制备包含角化细胞生长因子的冻干组合物的方法。

85. 发明申请

US20120004241A1 SUCCINATE SALT OF (2R)-METHYL-1-PIPERAZINE 审中-公开
标题翻译：（2R） - 甲基-1-哌嗪的连续盐
公开(公告)号：US20120004241A1
公开(公告)日：2012-01-05
申请号：US13234510
申请日：2011-09-16
申请人： Tom Fleck , Bruce Fleck , Magnus Cernerud , Helena Lundström , Claes Löfström , Margit Pelcman , Alexander Paptchikhine , Emma Andersson , Alf Nygren
发明人： Tom Fleck , Bruce Fleck , Magnus Cernerud , Helena Lundström , Claes Löfström , Margit Pelcman , Alexander Paptchikhine , Emma Andersson , Alf Nygren
IPC分类号： A61K31/496 , A61P25/00 , C07D401/14
CPC分类号： C07D401/14 , C07D401/12
摘要： The present invention relates to a process for the preparation of compounds which are therapeutically active in the central nervous system.In one aspect, the invention relates to a process for the preparation of compounds of the general formula (I): wherein HA is a pharmaceutically acceptable acid and R1-R4 are each independently selected from the group consisting of hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, and di-C1-C6-alkylamino-C2-C6-alkoxy.The invention also relates to the use of said compound to manufacture a medicament for the treatment of a serotonin-related disorder.
摘要翻译：本发明涉及一种制备在中枢神经系统中具有治疗活性的化合物的方法。一方面，本发明涉及制备通式（I）化合物的方法：其中HA是药学上可接受的酸，R 1 -R 4各自独立地选自氢，卤素，C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基和二-C 1 -C 6烷基氨基-C 2 -C 6 - 烷氧基。本发明还涉及所述化合物在制备用于治疗5-羟色胺相关病症的药物中的用途。

86. 发明授权

US08030316B2 Malate salt of (2R)-methyl-1-{3-[2-(3-pyridinyloxy)ethoxy]-2-pyrazinyl}piperazine 有权
标题翻译：（2R） - 甲基-1- {3- [2-（3-吡啶氧基）乙氧基] -2-吡嗪基}哌嗪的苹果酸盐
公开(公告)号：US08030316B2
公开(公告)日：2011-10-04
申请号：US12817833
申请日：2010-06-17
申请人： Tom Fleck , Bruce Fleck, legal representative , Magnus Cernerud , Helena Lundström , Claes Löfström , Margit Pelcman , Alexander Paptchikhine , Emma Andersson , Alf Nygren
发明人： Tom Fleck , Magnus Cernerud , Helena Lundström , Claes Löfström , Margit Pelcman , Alexander Paptchikhine , Emma Andersson , Alf Nygren
IPC分类号： A61K31/4965
CPC分类号： C07D401/14 , C07D401/12
摘要： The present invention relates to a process for the preparation of compounds which are therapeutically active in the central nervous system.In one aspect, the invention relates to a process for the preparation of compounds of the general formula (I): wherein HA is a pharmaceutically acceptable acid and R1-R4 are each independently selected from the group consisting of hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, and di-C1-C6-alkylamino-C2-C6-alkoxy. The invention also relates to the use of said compound to manufacture a medicament for the treatment of a serotonin-related disorder.
摘要翻译：本发明涉及一种制备在中枢神经系统中具有治疗活性的化合物的方法。一方面，本发明涉及制备通式（I）化合物的方法：其中HA是药学上可接受的酸，R 1 -R 4各自独立地选自氢，卤素，C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基和二-C 1 -C 6烷基氨基-C 2 -C 6 - 烷氧基。本发明还涉及所述化合物在制备用于治疗5-羟色胺相关病症的药物中的用途。

87. 发明申请

US20110082107A1 INHIBITORS OF 11-BETA-HYDROXY STEROID DEHYDROGENASE TYPE 1 审中-公开
标题翻译： 11-羟基甾体脱氢酶1型抑制剂
公开(公告)号：US20110082107A1
公开(公告)日：2011-04-07
申请号：US12898279
申请日：2010-10-05
申请人： Martin Henriksson , Evert Homan , Lars Johansson , Jerk Vallgarda , Meredith Williams , Eric A. Bercot , Christopher H. Fotsch , Aiwen Li , Guolin Cai , Randall W. Hungate , Chester Chenguang Yuan , Christopher Tegley , David J.St. Jean, JR. , Nianhe Han , Qi Huang , Qingyian Liu , Michael D. Bartberger , George A. Moniz , Matthew J. Frizzle
发明人： Martin Henriksson , Evert Homan , Lars Johansson , Jerk Vallgarda , Meredith Williams , Eric A. Bercot , Christopher H. Fotsch , Aiwen Li , Guolin Cai , Randall W. Hungate , Chester Chenguang Yuan , Christopher Tegley , David J.St. Jean, JR. , Nianhe Han , Qi Huang , Qingyian Liu , Michael D. Bartberger , George A. Moniz , Matthew J. Frizzle
IPC分类号： A61K31/695 , C07D277/54 , A61K31/426 , C07D413/06 , A61K31/5377 , C07D277/60 , A61K31/428 , C07D417/06 , C07D417/12 , A61K31/55 , A61K31/4439 , C07D413/14 , A61K31/454 , C07D497/10 , A61K31/438 , C07F7/18 , A61P3/00 , A61P25/28 , A61P35/00
CPC分类号： C07D417/06 , C07D263/34 , C07D263/48 , C07D275/03 , C07D277/42 , C07D277/54 , C07D277/60 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D513/10 , C07F7/1804
摘要： The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.
摘要翻译：本发明涉及具有式（I），（II），（III）或（IV）的化合物：其中R1，R2，R3，R4，R5，R6，R7，X和Z如本文所定义，涉及包含该化合物的药物组合物，以及该化合物用于治疗与人类11-羟基类固醇脱氢酶1型酶相关的病症的用途和用于制备作用于人类11- 羟类固醇脱氢酶1型酶。

88. 发明授权

US07820675B2 Benzofuran compounds 失效
标题翻译：苯并呋喃化合物
公开(公告)号：US07820675B2
公开(公告)日：2010-10-26
申请号：US11018019
申请日：2004-12-20
申请人： Gary Johansson , Peter Brandt , Björn M. Nilsson
发明人： Gary Johansson , Peter Brandt , Björn M. Nilsson
IPC分类号： A61P3/04 , A61K31/18 , A61K31/47 , A61K31/495 , A61K31/496 , C07D295/04 , C07D487/06 , C07D241/04 , C07D215/38 , C07D217/22 , C07D403/04 , C07D405/04
CPC分类号： C07D307/79 , C07D307/82 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/12 , C07D409/14 , C07D453/02 , C07D487/08 , C07D495/04
摘要： The present invention relates to compounds of formula (I): wherein P, R3, W1, and W2 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds for the preparation of a medicament against 5-HT6 receptor-related disorders.
摘要翻译：本发明涉及式（I）化合物：其中P，R 3，W 1和W 2如本文所述，包含该化合物的药物组合物，其制备方法以及该化合物用于制备抗5-HT 6受体相关疾病的药物。

89. 发明授权

US07534794B2 Certain arylaliphatic and heteroaryl-aliphatic piperazinyl pyrazines and their use in the treatment of serotonin-related diseases 失效
标题翻译：某些芳基脂族和杂芳基 - 脂族哌嗪基吡嗪及其在治疗5-羟色胺相关疾病中的应用
公开(公告)号：US07534794B2
公开(公告)日：2009-05-19
申请号：US10269670
申请日：2002-10-11
申请人： Björn Nilsson , Jan Tejbrant , Benjamin Pelcman , Erik Ringberg , Markus Thor , Jonas Nilsson , Mattias Jönsson
发明人： Björn Nilsson , Jan Tejbrant , Benjamin Pelcman , Erik Ringberg , Markus Thor , Jonas Nilsson , Mattias Jönsson
IPC分类号： A61K31/50 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00
CPC分类号： C07D401/12 , C07D241/18 , C07D241/20 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D491/04
摘要： The invention relates to compounds of the general formula (I): wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO2—, —NH—, (ii) a C1-4-alkyl- or C1-6-acyl-substituted nitrogen atom or (iii) a C1-8-alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is —C(R4)(R5)—, —OC(R4)(R5)—, —N(R6)C(R4)(R5)—, —N(R6)—, —O—, —S— or —SO2—; R is optionally substituted C3-8-cycloalkyl, aryl or heteroaryl; R1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group —[C(R4)(R5)]xN(R2a)(R3a)]; R2a, R3a, R4, R5, R6 and x are as defined in the claims, and n is 0 or 1; and pharmaceutically acceptable salts, hydrates and prodrug forms thereof. The compounds may be prepared by per se conventional methods and can be used for treating a human or animal subject suffering from a serotonin-related disorder, such as eating disorders, especially obesity, memory disorders, schizophrenia, mood disorders, anxiety disorders, pain, sexual dysfunctions, and urinary disorders The invention also relates to such use as well as to pharmaceutical compositions comprising a compound of formula (I).
摘要翻译：本发明涉及通式（I）的化合物：其中Ar为任选取代的芳基或杂芳基; A是（ⅰ）-O - ， - S - ， - SO 2 - ， - NH - ，（ⅱ）C 1-4 - 烷基 - 或C 1-6 - 酰基取代的氮原子或（ⅲ）亚烷基链或具有2至8个链原子的杂亚烷基链，其任选地包含至少一个不饱和键，并且其可以被取代和/或含有桥以形成具有3-8个环成员的饱和或部分或完全不饱和的环; B是-C（R 4）（R 5） - ， - OC（R 4）（R 5） - ， - N（R 6）或-SO 2 - ; R是任选取代的C 3-8 - 环烷基，芳基或杂芳基; R1是（i）饱和或不饱和的氮杂环或氨基氮杂环或饱和的二氮环或氨基二氮环，其具有4至7个环成员，或具有7至10个环成员的饱和氨基氮杂双环，氮杂双环或二氮杂双环，其任选地环在一个或多个位置被取代，或基团 - [C（R 4）（R 5）] x N（R 2a）（R 3a）]; R2a，R3a，R4，R5，R6和x如权利要求中所定义，n为0或1; 及其药学上可接受的盐，水合物和前药形式。化合物可以通过本身的常规方法制备，并且可以用于治疗患有5-羟色胺相关病症的人或动物受试者，例如进食障碍，特别是肥胖，记忆障碍，精神分裂症，情绪障碍，焦虑症，疼痛，性功能障碍和尿失调本发明还涉及这样的用途以及包含式（I）化合物的药物组合物。

90. 发明申请

US20080293694A1 New compounds 失效
标题翻译：新化合物
公开(公告)号：US20080293694A1
公开(公告)日：2008-11-27
申请号：US12075979
申请日：2008-03-13
申请人： Johan Angbrant , Peter Brandt , Rune Ringom , Bengt Lindqvist
发明人： Johan Angbrant , Peter Brandt , Rune Ringom , Bengt Lindqvist
IPC分类号： A61K31/4745 , C07D471/06 , C07D487/06 , A61K31/55 , A61K8/49 , A61P3/04
CPC分类号： C07D471/06 , C07D487/06
摘要： The present invention relates to novel compounds of formula (I): wherein R1, R2, R3, R4, and R5 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds for the preparation of a medicament against 5-HT6 receptor-related disorders.
摘要翻译：本发明涉及新的式（I）化合物：其中R 1，R 2，R 3，R 4和R 5如本文所述，包含该化合物的药物组合物，其制备方法以及使用用于制备抗5-HT 6受体相关病症的药物的化合物。

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