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1. 发明授权

US06583156B1 4-Quinolinemethanol derivatives as purine receptor antagonists (1) 失效
标题翻译：嘌呤受体拮抗剂4-喹啉甲醇衍生物（1）
公开(公告)号：US06583156B1
公开(公告)日：2003-06-24
申请号：US09786471
申请日：2001-05-16
申请人： Roger John Gillespie , Joanne Lerpiniere , Suneel Gaur , David Reginald Adoms , Lars Jacob Stray Knutsen , Simon Edward Ward
发明人： Roger John Gillespie , Joanne Lerpiniere , Suneel Gaur , David Reginald Adoms , Lars Jacob Stray Knutsen , Simon Edward Ward
IPC分类号： A61K3147
CPC分类号： C07D215/38 , A61K31/47 , A61K31/4709 , C07D215/14 , C07D215/18 , C07D215/22 , C07D215/26 , C07D215/36 , C07D215/48 , C07D401/04 , C07D401/06 , C07D405/04 , C07D405/06 , C07D409/04 , C07D409/06
摘要： Use a compound of formula (I) wherein: R1 is hydrogen or alkyl; R2 and R3 are independently selected from hydrogen, alkyl, aryl and heterocyclyle or together may form a ring or R1 and R2 or R3 together may form an oxygen-containing, optionally fused ring pharmaceutically acceptable salts or prodrugs thereof, with the proviso that where R1 and R4 to R9 are hydrogen, R2 or R3 is not 3-methoxy-4-benzyloxyphenyl or 2-dimethylaminoethoxymethyl, in the manufacture of a medicament for the treatment or prevention of a disorder in which the blocking of purine receptors, particularly adenosine receptors and more particularly A2A receptors, may be beneficial. Said disorders are neurodegenerative disorders or movement disorders selected from Parkinson's disease or progressive supernuclear palsy, Huntington's disease, multiple system atrophy, corticobasal degeneration, Wilson's disease, Hallerrorden-Spatz disease, progressive pallidal atrophy, Dopa-responsive dystonia-Parkinsonism, spasticity, Alzheimer's disease or other disorders of the basal ganglia which result in dyskinesias.
摘要翻译：使用式（I）的化合物，其中：R 1是氢或烷基; R2和R3独立地选自氢，烷基，芳基和杂环基，或一起可以形成环，或者R 1和R 2或R 3一起可以形成含氧的，任选稠合的药学上可接受的盐或前药，条件是其中R 1 并且R 4至R 9为氢，R 2或R 3不为3-甲氧基-4-苄氧基苯基或2-二甲基氨基乙氧基甲基，用于制备用于治疗或预防其中阻断嘌呤受体，特别是腺苷受体和更具体地，A2A受体可能是有益的。所述病症是选自帕金森氏病或进行性无核麻痹，亨廷顿氏病，多发性系统萎缩，皮质基底变性，威尔逊氏病，哈勒德 - 斯坦茨病，进行性苍白萎缩症，多巴反应性肌张力障碍 - 帕金森综合征，痉挛状态，阿尔茨海默病的神经变性疾病或运动障碍或导致运动障碍的基底节神经节的其他疾病。

2. 发明授权

US06608085B1 4-quinolinemethanol derivatives as purine receptor antagonists (II) 失效
标题翻译： 4-喹啉甲醇衍生物作为嘌呤受体拮抗剂（II）
公开(公告)号：US06608085B1
公开(公告)日：2003-08-19
申请号：US09786472
申请日：2001-05-09
申请人： Roger John Gillespie , Joanne Lerpiniere , Paul Richard Giles , David Reginald Adams , Lars Jacob Stray Knutsen , Ian Anthony Cliffe
发明人： Roger John Gillespie , Joanne Lerpiniere , Paul Richard Giles , David Reginald Adams , Lars Jacob Stray Knutsen , Ian Anthony Cliffe
IPC分类号： A61K314709
CPC分类号： A61K31/47
摘要： Use of a compound of formula (I) as defined herein, or a pharmaceutically acceptable salt or prodrug thereof, in the manufacture of a medicament for the treatment or prevention of a disorder in which the blocking of purine receptors, particularly adenosine receptors and more particularly A2a receptors, may be beneficial, such as a movement disorder, for example, Parkinson's Disease or progressive supemuclear palsy, Huntingtons disease, multiple system atrophy, corticobasal degeneration, Wilsons disease, Hallerrorder-Spatz disease, progressive pallidal atrophy, Dopa-responsive dystonia-Parkinsonism, spasticity, Alzheimer's disease or other disorders of the basal ganglia which result in dyskinesias.
摘要翻译：本文定义的式（I）化合物或其药学上可接受的盐或前药在制备用于治疗或预防其中阻断嘌呤受体，特别是腺苷受体，尤其是腺苷受体的病症的药物中的用途 A2a受体可能是有益的，例如运动障碍，例如帕金森氏病或进行性超核性麻痹，亨廷顿病，多系统萎缩，皮质基底变性，威尔逊病，哈勒勒斯特氏病，进行性苍白萎缩，多巴反应性肌张力障碍 - 帕金森综合征，痉挛性，阿尔茨海默病或基底神经节的其他障碍，导致运动障碍。

3. 发明申请

US20140199417A1 Antihistamines Combined with Dietary Supplements for Improved Health 有权
标题翻译：抗组胺药联合膳食补充剂改善健康
公开(公告)号：US20140199417A1
公开(公告)日：2014-07-17
申请号：US14124748
申请日：2012-06-08
申请人： Lars Jacob Stray Knutsen , Judi Lois Knutsen
发明人： Lars Jacob Stray Knutsen , Judi Lois Knutsen
IPC分类号： A61K31/4415 , A23L2/52 , A61K31/4045 , A61K36/84 , A61K31/4402 , A61K31/405
CPC分类号： A61K31/4415 , A23L2/52 , A61K31/4045 , A61K31/405 , A61K31/4402 , A61K31/495 , A61K31/56 , A61K36/84 , A61K45/06 , A61K2300/00
摘要： The present invention provides combinations comprising a sedating antihistamine and selected indole-based natural products such as L-tryptophan, 5-hydroxytryptophan and melatonin, along with pharmaceutically acceptable calcium and magnesium salts and selected B vitamins. These combinations are useful in providing a medicament for improving sleep in mammals, especially humans.
摘要翻译：本发明提供了包含镇静抗组胺药和选择的基于吲哚的天然产物如L-色氨酸，5-羟色氨酸和褪黑激素以及药学上可接受的钙和镁盐以及选择的B族维生素的组合。这些组合可用于提供用于改善哺乳动物，特别是人类的睡眠的药物。

4. 发明授权

US06197788B1 (−)-mefloquine to block puringergic receptors and to treat movement or neurodegenerative disorders 失效
标题翻译：（ - ） - 美氟喹阻断风湿能受体并治疗运动或神经退行性疾病
公开(公告)号：US06197788B1
公开(公告)日：2001-03-06
申请号：US09355205
申请日：1999-09-27
申请人： Allan Fletcher , Lars Jacob Stray Knutsen , Richard H. P. Porter , Scott Murray Weiss , Robin Shepherd
发明人： Allan Fletcher , Lars Jacob Stray Knutsen , Richard H. P. Porter , Scott Murray Weiss , Robin Shepherd
IPC分类号： A61K3147
CPC分类号： A61K31/4709
摘要： The present invention relates to the use of (±)-R*,S*)-alpha-2-piperidnyl-2,8-bis(trifluoromethyl)-4-quinolinemthanol and in particular (−)-(11S,2′R)-alpha-2-piperidnyl-2,8-bis(trifluoromethyl)-4-quinolinemthanol in the treatment of disorders in which the reduction of purinergic neurotransmission could be beneficial. The invention relates in particular to adenosine receptors, and particularly adenosine A2a receptors and to the treatment of movement disorders such as Parkinson's disease.
摘要翻译：本发明涉及（）-R *，S *）-α-2-哌啶基-2,8-双（三氟甲基）-4-喹啉甲醇，特别是（ - ） - （11S，2'R） α-2-哌啶基-2,8-双（三氟甲基）-4-喹啉麻酚治疗嘌呤能神经传递减少可能有益的疾病。本发明特别涉及腺苷受体，特别是腺苷A2a受体以及运动障碍如帕金森病的治疗

5. 发明授权

US5683989A Treatment of ischemias by administration of 2,N.sup.6 -substituted adenosines 失效
标题翻译：通过施用2，N6取代的腺苷治疗缺血
公开(公告)号：US5683989A
公开(公告)日：1997-11-04
申请号：US504811
申请日：1995-07-20
申请人： Jesper Lau , Lars Jacob Stray Knutsen , Malcolm Sheardown , Anker Jon Hansen
发明人： Jesper Lau , Lars Jacob Stray Knutsen , Malcolm Sheardown , Anker Jon Hansen
IPC分类号： C07H19/16 , A61K31/70 , C07H19/167
CPC分类号： C07H19/16
摘要： The present invention relates to compounds of formula I ##STR1## wherein X is amino, C.sub.1-6 -alkylamino, di-C.sub.1-6 -alkylamino; R.sup.1 is H, straight or branched C.sub.1-6 -alkyl or trifluoromethyl; R.sup.4 is H or straight or branched C.sub.1-6 -alkyl; or R.sup.1 and R.sup.4 together form a cyclobutyl, cyclopentyl or cyclohexyl ring; Y is O, S, SO.sub.2, N--H or N-alkyl; R.sup.5 is selected from optionally substituted heterocycles; R.sup.6 is hydrogen, benzoyl or C.sub.1-6 -alkanoyl and R.sup.7 is hydrogen, benzoyl or C.sub.1-6 -alkanoyl; or a pharmaceutically acceptable salt thereof. The compounds have been found useful for treating central nervous system and cardiovascular ailments.
摘要翻译：本发明涉及式Ⅰ化合物其中X为氨基，C 1-6 - 烷基氨基，二-C 1-6 - 烷基氨基， R1是H，直链或支链C 1-6 - 烷基或三氟甲基; R4是H或直链或支链C 1-6 - 烷基; 或R 1和R 4一起形成环丁基，环戊基或环己基环; Y是O，S，SO 2，N-H或N-烷基; R5选自任选取代的杂环; R6是氢，苯甲酰基或C1-6-烷酰基，R7是氢，苯甲酰基或C1-6-烷酰基; 或其药学上可接受的盐。已经发现这些化合物可用于治疗中枢神经系统和心血管疾病。

6. 发明授权

US5672588A Purine derivatives 失效
标题翻译：嘌呤衍生物
公开(公告)号：US5672588A
公开(公告)日：1997-09-30
申请号：US521077
申请日：1995-08-28
申请人： Lars Jacob Stray Knutsen , Jesper Lau
发明人： Lars Jacob Stray Knutsen , Jesper Lau
IPC分类号： C07H19/16 , A61K31/70
CPC分类号： A61K31/7076 , C07H19/16 , Y10S514/929
摘要： A compound of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein X is hydrogen, amino, halogen, hydroxy, lower alkoxy or lower alkyl and R.sup.1 is ##STR2## wherein Y is methylene or a valence bond, R.sup.2 and R.sup.5 is H or lower, straight or branched alkyl, R.sup.3 is H or lower alkyl, or R.sup.2 and R.sup.3 can together form a cyclobutyl, cyclopentyl, cyclohexyl or phenyl ring, Z is oxygen, methylene, sulphur, sulphonyl or a valence bond, R.sup.4 is H, lower alkyl, aralkyl, a mono or bicyclic aromatic system optionally substituted with various groups. The compounds have been found useful for treating central nervous system ailments.
摘要翻译：式（I）化合物或其药学上可接受的盐：其中X是氢，氨基，卤素，羟基，低级烷氧基或低级烷基，R 1是其中Y是亚甲基或价数键，R2和R5是H或更低的直链或支链烷基，R3是H或低级烷基，或R2和R3可以一起形成环丁基，环戊基，环己基或苯环，Z是氧，亚甲基，硫，磺酰基或价键，R 4是H，低级烷基，芳烷基，任选被各种基团取代的单或二环芳族体系。已经发现这些化合物可用于治疗中枢神经系统疾病。

7. 发明授权

US09700548B2 Antihistamines combined with dietary supplements for improved health 有权
公开(公告)号：US09700548B2
公开(公告)日：2017-07-11
申请号：US14124748
申请日：2012-06-08
申请人： Lars Jacob Stray Knutsen , Judi Lois Knutsen
发明人： Lars Jacob Stray Knutsen , Judi Lois Knutsen
IPC分类号： A61K31/4402 , A61K45/06 , A61K31/4415 , A61K31/56 , A61K31/495 , A61K31/4045 , A23L2/52 , A61K31/405 , A61K36/84
CPC分类号： A61K31/4415 , A23L2/52 , A61K31/4045 , A61K31/405 , A61K31/4402 , A61K31/495 , A61K31/56 , A61K36/84 , A61K45/06 , A61K2300/00
摘要： The present invention provides combinations comprising a sedating antihistamine and selected indole-based natural products such as L-tryptophan, 5-hydroxytryptophan and melatonin, along with pharmaceutically acceptable calcium and magnesium salts and selected B vitamins. These combinations are useful in providing a medicament for improving sleep in mammals, especially humans.

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