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1. 发明授权

US07381823B2 Process for preparing cyclohexanediacetic acid monoamide 失效
标题翻译：环己烷二乙酸单酰胺的制备方法
公开(公告)号：US07381823B2
公开(公告)日：2008-06-03
申请号：US10599009
申请日：2005-03-17
申请人： Bruno Danieli , Pietro Delogu , Sabrina De Rosa , Lorenza Fugazza
发明人： Bruno Danieli , Pietro Delogu , Sabrina De Rosa , Lorenza Fugazza
IPC分类号： C07D221/20 , C07C53/134
CPC分类号： C07D221/20
摘要： A new process is described for synthesising cyclohexanediacetic acid monoamide, a key compound in the synthesis of grabapentin precursors. The process of the invention is characterised by reacting cyclohexanone with cynoacetamide and immediately after, with a suitable malonic acid ester. A new intermediate (5-cyano-2,4-dioxo-3-azaspiro[5,5]undecane-1-carboxylic acid ester) is obtained which is convertible, under mild reaction conditions, into cyclohexanediacetic acid monoamide.
摘要翻译：描述了合成环己烷二乙酸单酰胺的新方法，其是在加巴喷丁前体的合成中的关键化合物。本发明的方法的特征在于使环己酮与鲸蜡醇乙酰胺反应，并立即与合适的丙二酸酯反应。得到新的中间体（5-氰基-2,4-二氧代-3-氮杂螺[5,5]十一碳烷-1-羧酸酯），其在温和的反应条件下可转化成环己烷二乙酸单酰胺。

2. 发明授权

US08664395B2 Purification 4-aza-androst-1-ene-17-oic acid from 4-aza-androstan-17-oic acid 有权
标题翻译：从4-氮杂 - 雄甾烷-17-酸酸中纯化4-氮杂 - 雄甾-1-烯-17-酸
公开(公告)号：US08664395B2
公开(公告)日：2014-03-04
申请号：US13257865
申请日：2009-04-02
申请人： Mauro Bonetti , Sabrina De Rosa
发明人： Mauro Bonetti , Sabrina De Rosa
IPC分类号： C07D221/18 , A61K31/435
CPC分类号： C07J73/005
摘要： The present invention relates to a process of separation of 4-aza-androst-1-ene-17-oic acid from 4-aza-androstan-17-oic acid, which brings to 4-aza-androst-1-ene-17-oic containing less than 0.05% w/w of 4-aza-androstan-17-oic acid, with high yield and productivity. In particular, the present invention relates to a process for the separation of 4-aza-androstan-17-oic acid from 4-aza-androst-1-ene-17-oic acid, comprising the steps of treating the crude 4-aza-androst-1-ene-17-oic acid with formic acid and recovering the purified 4-aza-androst-1-ene-17-oic acid containing 4-aza-androstan-17-oic acid in w/w % less than 0.05%.
摘要翻译：本发明涉及从4-氮杂 - 雄甾烷-17-酸分离4-氮杂 - 雄甾-1-烯-17-酸的方法，其使4-氮杂 - 雄甾-1-烯-17-酸含有小于0.05％w / w的4-氮杂 - 雄甾烷-17-酸的2-羟基苯甲酸，产率高，生产率高。特别地，本发明涉及从4-氮杂 - 雄甾-1-烯-17-酸酸分离4-氮杂 - 雄甾烷-17-酸的方法，包括以下步骤：将粗制4-氮杂 - 雄甾-1-烯-17-酸与甲酸反应，并回收纯化的含有4-氮杂 - 雄甾烷-17-酸的4-氮杂 - 雄甾-1-烯-17-酸，w / w％ 0.05％。

3. 发明申请

US20070208175A1 PROCESS FOR PREPARING CYCLOHEXANEDIACETIC ACID MONOAMIDE 失效
标题翻译：制备环己酸单丁酰胺的方法
公开(公告)号：US20070208175A1
公开(公告)日：2007-09-06
申请号：US10599009
申请日：2005-03-17
申请人： Bruno Danieli , Pietro Delogu , Sabrina de Rosa , Lorenza Fugazza
发明人： Bruno Danieli , Pietro Delogu , Sabrina de Rosa , Lorenza Fugazza
IPC分类号： C07D227/093
CPC分类号： C07D221/20
摘要： A new process is described for synthesising cyclohexanediacetic acid monoamide, a key compound in the synthesis of grabapentin precursors. The process of the invention is characterised by reacting cyclohexanone with cynoacetamide and immediately after, with a suitable malonic acid ester. A new intermediate (5-cyano-2,4-dioxo-3-azaspiro[5,5]undecane-1-carboxylic acid ester) is obtained which is convertible, under mild reaction conditions, into cyclohexanediacetic acid monoamide.
摘要翻译：描述了合成环己烷二乙酸单酰胺的新方法，其是在加巴喷丁前体的合成中的关键化合物。本发明的方法的特征在于使环己酮与鲸蜡醇乙酰胺反应，并立即与合适的丙二酸酯反应。得到新的中间体（5-氰基-2,4-二氧代-3-氮杂螺[5,5]十一碳烷-1-羧酸酯），其在温和的反应条件下可转化成环己烷二乙酸单酰胺。

4. 发明授权

US06245742B1 Peptide antagonists of cellular mitogenesis and motogenesis and their therapeutic use 失效
标题翻译：细胞有丝分裂和机制的肽拮抗剂及其治疗用途
公开(公告)号：US06245742B1
公开(公告)日：2001-06-12
申请号：US08930616
申请日：1997-10-15
申请人： Carlo Battistini , Patrizia Giordano , Sabrina De Rosa , Fabio Corradi , Paolo Comoglio , Alberto Bardelli
发明人： Carlo Battistini , Patrizia Giordano , Sabrina De Rosa , Fabio Corradi , Paolo Comoglio , Alberto Bardelli
IPC分类号： A61K3800
CPC分类号： C07K5/0827 , C07K5/0202 , C07K5/1016 , C07K5/1027 , C07K14/71
摘要： The present invention relates to peptides and peptidomimetic compounds and pharmaceutical compositions containing them as useful pharmacological agents in the control or treatment of proliferative diseases such as cancer, against tumor growing and/or tumoral metastasis, and psoriasis and in the control or treatment of inflammatory, allergic, autoimmune, viral, and cardiovascular diseases. These new compounds have the unique property to inhibit the recognition of several phosphotyrosine containing motifs within all the cellular receptors and cytosolic transducers by a wide spectrum of SH2 domains contained in cytosolic transducers and other effector proteins laying along different pathways of the signal transduction process and with a particularly high affinity for the SH2 domain of the adaptor transducer Grb2, a key element along the pathway to mitogenesis and motogenesis, this last activity leading to invasiveness and to metastasis. The invention also relates to methods for production of the compounds and methods of treatment employing the compounds.
摘要翻译：本发明涉及肽和拟肽化合物和药物组合物，其含有它们作为控制或治疗增殖性疾病如癌症，抗肿瘤生长和/或肿瘤转移以及牛皮癣以及控制或治疗炎症，过敏性，自身免疫性，病毒性和心血管疾病。这些新化合物具有独特的性质，可以通过广泛的SH2结构域抑制所有细胞受体和细胞溶质转导体中识别的含有多种含磷酸酪氨酸基序，这些SH2结构域包含在信号转导过程不同途径的细胞溶质转导和其他效应蛋白中，对于适应器传感器Grb2的SH2结构域特别高的亲和力，Grb2是沿着有丝分裂和发育的途径的关键因素，这是导致侵袭和转移的最后一个活动。本发明还涉及化合物的制备方法和使用该化合物的处理方法。

5. 发明申请

US20120029196A1 PURIFICATION 4-AZA-ANDROST-1-ENE-17-OIC ACID FROM 4-AZA-ANDROSTAN-17-OIC ACID 有权
标题翻译：来自4-AZA-ANDROSTAN-17-OIC酸的4-AZA-ANDROST-1-ENE-17-OIC酸的纯化
公开(公告)号：US20120029196A1
公开(公告)日：2012-02-02
申请号：US13257865
申请日：2009-04-02
申请人： Mauro Bonetti , Sabrina De Rosa
发明人： Mauro Bonetti , Sabrina De Rosa
IPC分类号： C07D221/18
CPC分类号： C07J73/005
摘要： The present invention relates to a process of separation of 4-aza-androst-1-ene-17-oic acid from 4-aza-androstan-17-oic acid, which brings to 4-aza-androst-1-ene-17-oic containing less than 0.05% w/w of 4-aza-androstan-17-oic acid, with high yield and productivity. In particular, the present invention relates to a process for the separation of 4-aza-androstan-17-oic acid from 4-aza-androst-1-ene-17-oic acid, comprising the steps of treating the crude 4-aza-androst-1-ene-17-oic acid with formic acid and recovering the purified 4-aza-androst-1-ene-17-oic acid containing 4-aza-androstan-17-oic acid in w/w % less than 0.05%.
摘要翻译：本发明涉及从4-氮杂 - 雄甾烷-17-酸分离4-氮杂 - 雄甾-1-烯-17-酸的方法，其使4-氮杂 - 雄甾-1-烯-17-酸含有小于0.05％w / w的4-氮杂 - 雄甾烷-17-酸的2-羟基苯甲酸，产率高，生产率高。特别地，本发明涉及从4-氮杂 - 雄甾-1-烯-17-酸酸分离4-氮杂 - 雄甾烷-17-酸的方法，包括以下步骤：将粗制4-氮杂 - 雄甾-1-烯-17-酸与甲酸反应，并回收纯化的含有4-氮杂 - 雄甾烷-17-酸的4-氮杂 - 雄甾-1-烯-17-酸，w / w％ 0.05％。

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