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1. 发明申请

US20050014804A1 Tetrazole and oxadiazolone substituted beta-amino acid derivatives 失效
标题翻译：四唑和恶二唑酮取代的β-氨基酸衍生物
公开(公告)号：US20050014804A1
公开(公告)日：2005-01-20
申请号：US10795760
申请日：2004-03-08
申请人： Nancy Barta , Norman Colbry , Raymond Hudack , Kristin Lin , Jacob Schwarz , Andrew Thorpe , David Wustrow , Zhijian Zhu
发明人： Nancy Barta , Norman Colbry , Raymond Hudack , Kristin Lin , Jacob Schwarz , Andrew Thorpe , David Wustrow , Zhijian Zhu
IPC分类号： A61K31/41 , A61K31/4245 , C07D257/04 , C07D271/06 , C07D271/07 , C07D271/12
CPC分类号： C07D257/04 , C07D271/07
摘要： This invention relates to novel tetrazole and oxadiazalone β-amino acids derivatives of the formula wherein G is wherein R1 through R4 are defined as in the specification, pharmaceutical compositions containing them and their use for the treatment of various central nervous system and other disorders. The cyclopropyl β-amino acids derivatives of this invention exhibit activity as alpha2delta ligands (α2δ ligands). Such compounds have affinity for the α2δ subunit of a calcium channel.
摘要翻译：本发明涉及下式的新型四唑和恶二唑类β-氨基酸衍生物，其中G为其中R 1至R 4如本说明书所定义，含有它们的药物组合物及其用于治疗各种中枢神经系统等障碍。本发明的环丙基β-氨基酸衍生物表现出作为α2delta配体（α2delta配体）的活性。这些化合物对钙离子通道的α2delta亚基具有亲和力。

2. 发明申请

US20060154972A1 Amino acids with affinity for the alpha-2-delta-protein 有权
公开(公告)号：US20060154972A1
公开(公告)日：2006-07-13
申请号：US11375318
申请日：2006-03-14
申请人： Nancy Barta , Jacob Schwarz , Andrew Thorpe , David Wustrow
发明人： Nancy Barta , Jacob Schwarz , Andrew Thorpe , David Wustrow
IPC分类号： A61K31/44 , A61K31/198 , A61K31/277
CPC分类号： C07C229/08 , A61K31/195 , A61K31/198 , C07C229/28 , C07C229/34 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , Y02A50/415
摘要： This invention relates to certain β-amino acids that bind to the alpha-2-delta (α2δ) subunit of a calcium channel. These compounds and their pharmaceutically acceptable salts are useful in the treatment of a variety of psychiatric, pain and other disorders.

3. 发明申请

US20050245519A1 Substituted morpholine compounds for the treatment of central nervous system disorders 失效
标题翻译：用于治疗中枢神经系统疾病的取代吗啉化合物
公开(公告)号：US20050245519A1
公开(公告)日：2005-11-03
申请号：US11119210
申请日：2005-04-29
申请人： Nancy Barta , Shelly Glase , David Gray , Gregory Reichard , Lloyd Simons , Weijan Xu
发明人： Nancy Barta , Shelly Glase , David Gray , Gregory Reichard , Lloyd Simons , Weijan Xu
IPC分类号： A61K31/537 , A61K31/5377 , C07D265/30 , C07D413/02 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06
CPC分类号： C07D265/30 , C07D413/06 , C07D413/12 , C07D417/06
摘要： This invention relates to compounds of the formulae I wherein R1-R8, A, X, and Z are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system disorders.
摘要翻译：本发明涉及式I化合物，其中R 1〜Z 8，A，X和Z如说明书中所定义，含有它们的药物组合物及其用途在治疗中枢神经系统疾病。

4. 发明授权

US06372911B1 Process for preparing &bgr;-hydroxycarbamates and their conversion to oxazolidinones 失效
标题翻译：制备β-羟基氨基甲酸酯及其转化为恶唑烷酮的方法
公开(公告)号：US06372911B1
公开(公告)日：2002-04-16
申请号：US09482799
申请日：2000-01-13
申请人： Nancy Barta , Robert D. Larsen , Daniel R. Sidler , Steven A. Weissman
发明人： Nancy Barta , Robert D. Larsen , Daniel R. Sidler , Steven A. Weissman
IPC分类号： C07D41312
CPC分类号： C07D413/12 , C07C271/16 , C07D211/18 , C07D263/38
摘要： A process for preparing a &bgr;-hydroxy carbamate product is disclosed. The process comprises reacting an olefin compound containing at least one carbon-carbon double bond with a carbamate in an aqueous solvent and in the presence of a base, an osmium catalyst, a co-oxidant selected from a halohydantoin, a haloisocyanuric acid, and an alkali metal salt of a haloisocyanuric acid, and optionally an asymmetric ligand, to form a reaction mixture containing the &bgr;-hydroxy carbamate product. The process optionally further comprises treating the &bgr;-hydroxy carbamate product with additional base to form an oxazolidinone. The oxazolidinones are useful as chiral auxiliary agents and as intermediates for the formation of pharmaceutically active substances such as alpha 1 a adrenergic receptor antagonists. A process for preparing nitrogen-functionalized derivatives of the oxazolidinones is also disclosed.
摘要翻译：公开了一种制备β-羟基氨基甲酸酯产物的方法。该方法包括使含有至少一个碳 - 碳双键的烯烃化合物与氨基甲酸酯在水溶剂中反应，并在碱，锇催化剂，选自卤代乙内酰脲，卤代异氰脲酸和卤代异氰尿酸的碱金属盐和任选的不对称配体，以形成含有β-羟基氨基甲酸酯产物的反应混合物。该方法任选地还包括用另外的碱处理β-羟基氨基甲酸酯产物以形成恶唑烷酮。恶唑烷酮可用作手性助剂，也可用作形成药物活性物质如α1肾上腺素能受体拮抗剂的中间体。还公开了制备恶唑烷酮的氮官能化衍生物的方法。

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