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1. 发明授权

US06689904B2 Bridged tricyclic analogs of 2-(carboxycyclopropyl)glycine 失效
标题翻译： 2-（羧基环丙基）甘氨酸的桥连三环类似物
公开(公告)号：US06689904B2
公开(公告)日：2004-02-10
申请号：US10185445
申请日：2002-06-27
申请人： Alexander Alexei Greenfield , John Anthony Butera
发明人： Alexander Alexei Greenfield , John Anthony Butera
IPC分类号： C07C6112
CPC分类号： C07D493/08 , C07C229/50 , C07C2603/64
摘要： This invention provides processes for preparing a group of novel bridged tricyclic compounds having the formula: wherein X is (CH2)n, O, S, SO, SO2 or CR1R2; n is 1 or 2; and R1 and R2 are, independently, hydrogen, halogen, hydroxy, alkyl of one to six carbon atoms, alkoxy of one to six carbon atoms, or R1 and R2, taken together with the carbon to which they are attached, form cycloalkyl of three to six carbon atoms, an alkylidene of up to six carbon atoms or a carbonyl.
摘要翻译：本发明提供了制备一组具有下式的新型桥连三环化合物的方法：其中X是（CH 2）n，O，S，SO，SO 2或CR 1 R 2; n为1或2; R 1和R 2独立地是氢，卤素，羟基，1至6个碳原子的烷基，1至6个碳原子的烷氧基或R 1和R 2与它们所连接的碳形成3至6个碳原子的环烷基，最多6个碳原子的亚烷基或羰基。

2. 发明授权

US06700014B2 Process for extracting oleanolic acid from plant material 失效
标题翻译：从植物材料中提取齐墩果酸的方法
公开(公告)号：US06700014B2
公开(公告)日：2004-03-02
申请号：US10024978
申请日：2001-12-19
申请人： Gerold Jerz
发明人： Gerold Jerz
IPC分类号： C07C6112
CPC分类号： C07J63/00
摘要： A process for extracting oleanolic acid from plant material is disclosed. Dried plant material is provided and an extraction process is carried out with a non-halogenated polar to medium polar solvent. The resulting solution that contains oleanolic acid is separated from the plant material and the solvent is removed using cooling, vacuum-evaporation or other techniques. A precipitate is formed that contains mostly oleanolic acid. Subsequent purification steps to provide highly purified oleanolic acid include washing techniques, re-crystallization techniques or the use of chromatography.
摘要翻译：公开了从植物材料中提取齐墩果酸的方法。提供干燥植物材料，并用非卤化的极性至中等极性溶剂进行萃取过程。将所得到的含有齐墩果酸的溶液与植物材料分离，并使用冷却，真空蒸发或其它技术除去溶剂。形成大部分含有齐墩果酸的沉淀物。提供高度纯化的齐墩果酸的后续纯化步骤包括洗涤技术，重结晶技术或色谱法的使用。

3. 发明授权

US06222068B1 Nitrocubanes 失效
标题翻译：硝基异氰酸酯
公开(公告)号：US06222068B1
公开(公告)日：2001-04-24
申请号：US08228245
申请日：1994-04-14
申请人： Abdollah Bashir-Hashemi
发明人： Abdollah Bashir-Hashemi
IPC分类号： C07C6112
CPC分类号： C07C205/55 , C07C205/10 , C07C2603/90
摘要： An efficient direct functionalization of nitrocubanes has been achieved by irradiation of a solution in an oxalyl halide to yield halogenated and halocarbonylated derivatives of nitrocubanes.
摘要翻译：已经通过在草酰卤中的溶液照射产生氮化碳的卤代和卤代羰基化衍生物来实现氮代烷的有效直接官能化。

4. 发明授权

US06689905B2 Stereoisomers of 3-aminotricyclo[2.2.1.0(2.6)]heptane-1,3-dicarboxylic acid 失效
标题翻译： 3-氨基三环[2.2.1.0（2.6）]庚烷-1,3-二羧酸的立体异构体
公开(公告)号：US06689905B2
公开(公告)日：2004-02-10
申请号：US10185466
申请日：2002-06-27
申请人： Reinhardt Bernhard Baudy , Jean Yi-ching Sze , Jonathan Laird Gross
发明人： Reinhardt Bernhard Baudy , Jean Yi-ching Sze , Jonathan Laird Gross
IPC分类号： C07C6112
CPC分类号： C07C229/50 , C07B2200/07 , C07C227/32 , C07C2603/64
摘要： This invention provides a process for the preparation of all four stereoisomers of formula I or a pharmaceutically acceptable salt thereof which may be represented by the following structures:
摘要翻译：本发明提供了制备式I的所有四种立体异构体或其药学上可接受的盐的方法，其可以由以下结构表示：

5. 发明授权

US06596900B2 Fused bicyclic or tricyclic amino acids 失效
标题翻译：稠合双环或三环氨基酸
公开(公告)号：US06596900B2
公开(公告)日：2003-07-22
申请号：US10124210
申请日：2002-04-16
申请人： David Clive Blakemore , Justin Stephen Bryans , Sophie Caroline Williams
发明人： David Clive Blakemore , Justin Stephen Bryans , Sophie Caroline Williams
IPC分类号： C07C6112
CPC分类号： C07C45/292 , C07C45/30 , C07C45/67 , C07C45/676 , C07C45/68 , C07C45/69 , C07C49/427 , C07C49/433 , C07C229/28 , C07C2602/18 , C07C2602/20 , C07C2602/22 , C07C2602/24
摘要： The compounds of the instant invention are bicyclic or tricyclic amino acids useful in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, arthritis, neuropathological disorders, sleep disorders, visceral pain disorders, and gastrointestinal disorders. Processes for the preparation of the final products and intermediates useful in the process are included. Pharmaceutical compositions containing one or more of the compounds are also included.
摘要翻译：本发明的化合物是可用于治疗癫痫，微弱发作，运动功能减退，颅内疾病，神经变性疾病，抑郁症，焦虑症，恐慌症，疼痛，关节炎，神经病理学障碍，睡眠障碍，内脏疼痛障碍的双环或三环氨基酸，和胃肠道疾病。包括制备在该方法中有用的最终产物和中间体的方法。还包括含有一种或多种化合物的药物组合物。

6. 发明授权

US06740778B2 Method for the preparation of oleanolic acid and/or maslinic acid 失效
标题翻译：齐墩果酸和/或马斯酸的制备方法
公开(公告)号：US06740778B2
公开(公告)日：2004-05-25
申请号：US10359586
申请日：2003-02-07
申请人： Noriyasu Kuno , Gou Shinohara
发明人： Noriyasu Kuno , Gou Shinohara
IPC分类号： C07C6112
CPC分类号： C07J63/008
摘要： The present invention relates to a method for preparing oleanolic acid and/or maslinic acid and physiologically acceptable salts thereof, which comprises the steps of extracting olive plant and/or products obtained in the olive oil-manufacturing processes with water and/or an organic solvent and then concentrating and/or fractionating/purifying the resulting extract.
摘要翻译：本发明涉及一种制备齐墩果酸和/或马斯酸及其生理上可接受的盐的方法，其包括以下步骤：用橄榄油制备方法获得的橄榄油和/或有机溶剂然后浓缩和/或分馏/纯化所得萃取物。

7. 发明授权

US06632962B2 Caspase inhibitors and uses thereof 失效
标题翻译：胱天蛋白酶抑制剂及其用途
公开(公告)号：US06632962B2
公开(公告)日：2003-10-14
申请号：US09834052
申请日：2001-04-03
申请人： Julian M. C. Golec , Paul Charifson , Guy Brenchley
发明人： Julian M. C. Golec , Paul Charifson , Guy Brenchley
IPC分类号： C07C6112
CPC分类号： C07D213/81 , C07C233/83 , C07C235/52 , C07C237/36 , C07C255/57 , C07D207/34 , C07D209/42 , C07D213/82 , C07D277/56 , C07D307/68 , C07D333/38
摘要： This invention provides novel compounds that are effective as inhibitors of caspase and cellular apoptosis. The invention also provides methods for using the compounds to treat caspase-mediated diseases in mammals. The compounds have the general formula I: wherein X is F or Cl; R1 is COOH, COO(alkyl), or an isostere thereof; and R2 is an aryl group.
摘要翻译：本发明提供了作为半胱天冬酶抑制剂和细胞凋亡有效的新型化合物。本发明还提供了使用该化合物治疗哺乳动物中半胱天冬酶介导的疾病的方法。化合物具有通式I：其中X是F或Cl; 其中，COOH，COO（烷基）或其等同物; 并且R <2 是芳基

8. 发明授权

US06603041B2 Bicyclic enamide derivatives 失效
标题翻译：双环烯酰胺衍生物
公开(公告)号：US06603041B2
公开(公告)日：2003-08-05
申请号：US09947107
申请日：2001-09-05
申请人： Timothy John Norman , John Robert Porter , John Clifford Head , Andrew James Ratcliffe
发明人： Timothy John Norman , John Robert Porter , John Clifford Head , Andrew James Ratcliffe
IPC分类号： C07C6112
CPC分类号： C07D471/04 , A61K31/4375
摘要： Enamide derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk- in which Ar1 is an optionally substituted aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom or group, Ar2 is an optionally substituted arylene or heteroarylene group and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; X is an O or S atom or the group NR30 group; j and k is each zero or the integer 1 or 2 provided that the sum of j and k is zero or the integer 1 or 2; Cy1 is an optionally substituted cycloaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The componds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders including the inappropriate growth or migration of cells.
摘要翻译：描述了式（1）的酰胺衍生物：其中R1是Ar1L2Ar2Alk-基团，其中Ar1是任选取代的芳族或杂芳族基团，L2是共价键或连接原子或基团，Ar 2是任选取代的亚芳基或杂亚芳基， Alk是链-CH 2 -CH（R） - ， - CH = C（R） - 或其中R是羧酸（-CO 2 H）或其衍生物或生物试剂; R 2是氢原子或C 1-6烷基基团; X是O或S原子或NR30基团; j和k各自为零或整数1或2，条件是j和k的和为零或整数1或2; Cy1是任选取代的脂环族，杂环脂族，芳族或杂芳族基团;及其盐，溶剂合物，水合物和N-氧化物。化合物能够抑制整联蛋白与其配体的结合，并且可用于预防和治疗免疫或炎症性疾病，或疾病包括细胞不适当的生长或迁移。

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