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1. 发明授权

US08222246B2 Substituted isoxazoles 有权
标题翻译：取代的异恶唑
公开(公告)号：US08222246B2
公开(公告)日：2012-07-17
申请号：US12748524
申请日：2010-03-29
申请人： Bernd Buettelmann , Stephen Deems Gabriel , Steven Paul Hanlon , Roland Jakob-Roetne , Matthew C. Lucas , Paul Spurr , Andrew Thomas , Pius Waldmeier
发明人： Bernd Buettelmann , Stephen Deems Gabriel , Steven Paul Hanlon , Roland Jakob-Roetne , Matthew C. Lucas , Paul Spurr , Andrew Thomas , Pius Waldmeier
IPC分类号： C07D413/02 , A61K31/44
CPC分类号： C07D413/12 , C07D413/14
摘要： The present invention is concerned with novel hydroxy-methyl isoxazole derivatives of formula I wherein R1, R2 and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A α5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as pharmaceuticals.
摘要翻译：本发明涉及式I的新型羟基 - 甲基异恶唑衍生物，其中R 1，R 2和R 3如本文所述，以及其药学上可接受的盐和酯。本发明的活性化合物对GABA Aα5受体具有亲和性和选择性。此外，本发明涉及制备式I的活性化合物，含有它们的药物组合物及其作为药物的用途。

2. 发明申请

US20100256127A1 SUBSTITUTED ISOXAZOLES 有权
标题翻译：取代的ISOXAZOLES
公开(公告)号：US20100256127A1
公开(公告)日：2010-10-07
申请号：US12748524
申请日：2010-03-29
申请人： Bernd Buettelmann , Stephen Deems Gabriel , Steven Paul Hanlon , Roland Jakob-Roetne , Matthew C. Lucas , Paul Spurr , Andrew Thomas , Pius Waldmeier
发明人： Bernd Buettelmann , Stephen Deems Gabriel , Steven Paul Hanlon , Roland Jakob-Roetne , Matthew C. Lucas , Paul Spurr , Andrew Thomas , Pius Waldmeier
IPC分类号： A61K31/465 , C07D413/12 , C07D417/14 , A61K31/541 , C07D413/14 , A61K31/5377 , A61P25/28
CPC分类号： C07D413/12 , C07D413/14
摘要： The present invention is concerned with novel hydroxy-methyl isoxazole derivatives of formula I wherein R1, R2 and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A α5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as pharmaceuticals.
摘要翻译：本发明涉及式I的新型羟基 - 甲基异恶唑衍生物，其中R 1，R 2和R 3如本文所述，以及其药学上可接受的盐和酯。本发明的活性化合物对GABA Aα5受体具有亲和性和选择性。此外，本发明涉及制备式I的活性化合物，含有它们的药物组合物及其作为药物的用途。

3. 发明申请

US20090143589A1 Preparation of dihydropyrrol derivatives as intermediates 审中-公开
标题翻译：制备二氢吡咯啉衍生物作为中间体
公开(公告)号：US20090143589A1
公开(公告)日：2009-06-04
申请号：US12313988
申请日：2008-11-26
申请人： Christophe Pfleger , Paul Spurr , Rene Trussardi , Pius Waldmeier , Shaoning Wang
发明人： Christophe Pfleger , Paul Spurr , Rene Trussardi , Pius Waldmeier , Shaoning Wang
IPC分类号： C07D471/04
CPC分类号： C07D209/44 , C07D471/04
摘要： The invention is concerned with a new scalable process for the preparation of compounds of formula I comprising a new process for the preparation of the key intermediate, a dihydropyrrole derivative formula II or a salt thereof.
摘要翻译：本发明涉及用于制备式I化合物的新的可伸缩方法，其包括制备关键中间体的新方法，式II的二氢吡咯衍生物或其盐。

4. 发明申请

US20120041205A1 PREPARATION OF DIHYDROPYRROL DERIVATIVES AS INTERMEDIATES 审中-公开
标题翻译：作为中间体的二氢吲哚衍生物的制备
公开(公告)号：US20120041205A1
公开(公告)日：2012-02-16
申请号：US13278718
申请日：2011-10-21
申请人： Christophe Pfleger , Paul Spurr , Rene Trussardi , Pius Waldmeier , Shaoning Wang
发明人： Christophe Pfleger , Paul Spurr , Rene Trussardi , Pius Waldmeier , Shaoning Wang
IPC分类号： C07D471/04 , C07D209/44
CPC分类号： C07D209/44 , C07D471/04
摘要： The invention is concerned with a new scalable process for the preparation of compounds of formula I comprising a new process for the preparation of the key intermediate, a dihydropyrrole derivative formula II or a salt thereof.
摘要翻译：本发明涉及用于制备式I化合物的新的可伸缩方法，其包括制备关键中间体的新方法，式II的二氢吡咯衍生物或其盐。

5. 发明授权

US08293916B2 Diazole derivatives 失效
标题翻译：二唑衍生物
公开(公告)号：US08293916B2
公开(公告)日：2012-10-23
申请号：US12613089
申请日：2009-11-05
申请人： Bernd Buettelmann , Simona Maria Ceccarelli , Georg Jaeschke , Sabine Kolczewski , Richard Hugh Philip Porter , Paul Spurr , Eric Vieira
发明人： Bernd Buettelmann , Simona Maria Ceccarelli , Georg Jaeschke , Sabine Kolczewski , Richard Hugh Philip Porter , Paul Spurr , Eric Vieira
IPC分类号： A61K31/4439 , C07D401/04 , C07D401/06 , C07D401/14
CPC分类号： C07D401/06 , C07D401/14
摘要： The present invention relates to diazole derivatives of the general formula wherein A, E, R1, R2 and R3 are as defined in application and pharmaceutical compositions containing them. The invention also relates to use of such compounds for the treatment of diseases mediated by the metabotropic glutamate receptors (mGluR), such as anxiety, chronic and acute pain, protection against liver damage, urinary incontinence, obesity, Fragile-X and autism, Alzheimer's disease, epilepsy, schizophrenia, ischemia, Huntington's chorea, amyotrophic lateral sclerosis (ALS), dementia caused by AIDs, and Parkinson's disease.
摘要翻译：本发明涉及通式的二唑衍生物，其中A，E，R 1，R 2和R 3如申请中所定义，含有它们的药物组合物。本发明还涉及这种化合物用于治疗由代谢型谷氨酸受体（mGluR）介导的疾病的用途，例如焦虑，慢性和急性疼痛，防止肝损伤，尿失禁，肥胖，脆性-X和自闭症，阿尔茨海默病疾病，癫痫，精神分裂症，局部缺血，亨廷顿舞蹈病，肌萎缩性侧索硬化（ALS），AID引起的痴呆和帕金森病。

6. 发明申请

US20100048569A1 DIAZOLE DERIVATIVES 失效
标题翻译：二唑衍生物
公开(公告)号：US20100048569A1
公开(公告)日：2010-02-25
申请号：US12613089
申请日：2009-11-05
申请人： Bernd Buettelmann , Simona Maria Ceccarelli , Georg Jaeschke , Sabine Kolczewski , Richard Hugh Philip Porter , Paul Spurr , Eric Vieira
发明人： Bernd Buettelmann , Simona Maria Ceccarelli , Georg Jaeschke , Sabine Kolczewski , Richard Hugh Philip Porter , Paul Spurr , Eric Vieira
IPC分类号： A61K31/5377 , C07D401/02 , A61K31/4439 , C07D413/14 , A61P25/00
CPC分类号： C07D401/06 , C07D401/14
摘要： The present invention relates to diazole derivatives of the general formula wherein A, E, R1, R2 and R3 are as defined in application and pharmaceutical compositions containing them. The invention also relates to use of such compounds for the treatment of diseases mediated by the metabotropic glutamate receptors (mGluR), such as anxiety, chronic and acute pain, protection against liver damage, urinary incontinence, obesity, Fragile-X and autism, Alzheimer's disease, epilepsy, schizophrenia, ischemia, Huntington's chorea, amyotrophic lateral sclerosis (ALS), dementia caused by AIDs, and Parkinson's disease.
摘要翻译：本发明涉及通式的二唑衍生物，其中A，E，R 1，R 2和R 3如申请中所定义，含有它们的药物组合物。本发明还涉及这种化合物用于治疗由代谢型谷氨酸受体（mGluR）介导的疾病的用途，例如焦虑，慢性和急性疼痛，防止肝损伤，尿失禁，肥胖，脆性-X和自闭症，阿尔茨海默病疾病，癫痫，精神分裂症，局部缺血，亨廷顿舞蹈病，肌萎缩性侧索硬化（ALS），AID引起的痴呆和帕金森病。

7. 发明授权

US07459563B2 Process for the preparation of isonicotinic acid derivatives 有权
标题翻译：制备异烟酸衍生物的方法
公开(公告)号：US07459563B2
公开(公告)日：2008-12-02
申请号：US11259880
申请日：2005-10-27
申请人： Paul Spurr
发明人： Paul Spurr
IPC分类号： C07D213/46
CPC分类号： C07D213/79
摘要： The present invention relates to a process for the manufacture of compounds of formula Ia or Ib and pharmaceutically acceptable additional salts thereof, wherein R is lower alkyl. The compounds of formula Ia or Ib are valuable intermediate products for the manufacture of compounds that are pharmaceutically active as adenosine A2a receptor antagonist or metabotropic Glutamate receptor 2 antagonist. Such compounds are important in the regulation of many aspects of cellular metabolism and in the modulation of different central nervous system activities.
摘要翻译：本发明涉及制备式Ia或Ib化合物及其药学上可接受的另外的盐的方法，其中R是低级烷基。式Ia或Ib的化合物是制备作为腺苷A2a受体拮抗剂或代谢型谷氨酸受体2拮抗剂具有药学活性的化合物的有价值的中间产物。这些化合物在调节细胞代谢的许多方面以及调节不同的中枢神经系统活性中是重要的。

8. 发明授权

US06531597B2 Process for preparation of 2-phenyl acetic acid derivatives 有权
标题翻译： 2-苯基乙酸衍生物的制备方法
公开(公告)号：US06531597B2
公开(公告)日：2003-03-11
申请号：US10041123
申请日：2002-01-08
申请人： Fabienne Hoffmann-Emery , Michelangelo Scalone , Paul Spurr
发明人： Fabienne Hoffmann-Emery , Michelangelo Scalone , Paul Spurr
IPC分类号： C07D41300
CPC分类号： C07D213/75 , C07C29/40 , C07C41/26 , C07C51/12 , C07D239/48 , C07C57/30 , C07C57/58 , C07C59/64 , C07C63/14 , C07C61/40 , C07C33/46 , C07C33/20 , C07C43/23
摘要： The present invention is a process for the preparation of a compound of formula The compounds of formula I are valuable intermediates for the manufacture of therapeutically active compounds.
摘要翻译：本发明是制备下式化合物的方法式I化合物是制备治疗活性化合物的有价值的中间体。

9. 发明授权

US5578728A Process for the preparation of a benzo(a)quinolizione derivative 失效
标题翻译：制备苯并（a）喹嗪酮衍生物的方法
公开(公告)号：US5578728A
公开(公告)日：1996-11-26
申请号：US327159
申请日：1994-10-21
申请人： Paul Spurr
发明人： Paul Spurr
IPC分类号： A61K31/435 , A61P25/20 , C07D455/06
CPC分类号： C07D455/06
摘要： The invention is concerned with a process for the preparation of a benzo[a]quinolizinone derivative of the formula ##STR1## by reacting a compound of the formula ##STR2## wherein X is halogen and Ph is phenyl, with carbon monoxide in the presence of a carbonylation catalyst and in the presence of (S)-3-ethoxypyrrolidine or a lower alkanol or water; where a lower alkyl ester of the 10-chloro-6,7-dihydro-4-oxo-3 -phenyl-4H-benzo[a]quinolizine-1-carboxylic acid has been obtained, converting this into the corresponding free acid; and, where the 10-chloro-6,7-dihydro-4-oxo-3-phenyl-4H-benzo[a]quinolizine-1-carboxylic acid has been obtained, reacting a reactive derivative thereof with (S)-3-ethoxypyrrolidine. The compound of formula I is useful for the treatment or prophylaxis of sleep disorders.
摘要翻译：本发明涉及制备式I的苯并[a]喹嗪酮衍生物的方法，其中式Ⅰ的化合物其中X为卤素且Ph为苯基的式Ⅰbb与一氧化碳在在（S）-3-乙氧基吡咯烷或低级链烷醇或水的存在下，存在羰基化催化剂; 其中得到10-氯-6,7-二氢-4-氧代-3-苯基-4H-苯并[a]喹嗪-1-羧酸的低级烷基酯，将其转化为相应的游离酸; 并且其中已经获得了10-氯-6,7-二氢-4-氧代-3-苯基-4H-苯并[a]喹嗪-1-羧酸，使其反应性衍生物与（S）-3- 乙氧基吡咯烷。式I化合物可用于治疗或预防睡眠障碍。

10. 发明授权

US5902738A Enzymatic acylation 失效
标题翻译：酶酰化
公开(公告)号：US5902738A
公开(公告)日：1999-05-11
申请号：US829280
申请日：1997-03-31
申请人： Bernard Orsat , Paul Spurr , Beat Wirz
发明人： Bernard Orsat , Paul Spurr , Beat Wirz
IPC分类号： C12N9/20 , C07C35/18 , C12P7/40 , C12P7/62 , C12P7/64 , C12P23/00 , C12P7/02 , C07C67/02 , C12N11/02
CPC分类号： C12P7/62 , C12P23/00
摘要： A process for making a compound of formula ##STR1## wherein R signifies a C.sub.1-23 -alkyl group or a C.sub.2-23 -alkenyl group containing 1 to 3 double bonds, comprising the steps of (a) reacting a compound of formula ##STR2## with an acylating agent which is in a mixture comprising (i) an organic solvent and (ii) a lipase which is present in suspension, so as to form the compound of formula I; and (b) recovering the compound of formula I is provided for. The process can be used to make (11Z,13Z)-7,10-dihydro-10-hydroxy-retinyl acetate, an starting material for the production of vitamin A acetate.
摘要翻译：一种制备下式化合物的方法，其中R表示C1-23-烷基或含1〜3个双键的C2-23链烯基，包括以下步骤：（a）使式的化合物与酰化剂反应，是在（i）有机溶剂和（ii）存在于悬浮液中的脂肪酶的混合物中，以形成式I化合物; 和（b）回收式I化合物。该方法可用于制备（11Z，13Z）-7,10-二氢-10-羟基 - 视黄基乙酸酯，一种生产维生素A乙酸酯的原料。

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