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1. 发明授权

US08691864B2 Agents useful for reducing amyloid precursor protein and treating dementia and methods of use thereof 失效
标题翻译：可用于降低淀粉样蛋白前体蛋白和治疗痴呆的药剂及其使用方法
公开(公告)号：US08691864B2
公开(公告)日：2014-04-08
申请号：US13559186
申请日：2012-07-26
申请人： Nigel H. Greig , Karen T. Y. Shaw , Qiang-Sheng Yu , Harold W. Holloway , Tada Utsuki , Timothy T. Soncrant , Donald K. Ingram , Arnold Brossi , Anthony Giordano , Gordon Powers , Diane M. Davidson , Michael Sturgess
发明人： Nigel H. Greig , Karen T. Y. Shaw , Qiang-Sheng Yu , Harold W. Holloway , Tada Utsuki , Timothy T. Soncrant , Donald K. Ingram , Arnold Brossi , Anthony Giordano , Gordon Powers , Diane M. Davidson , Michael Sturgess
IPC分类号： A61K31/40
CPC分类号： C07D487/04 , A61K31/325 , A61K31/343 , A61K31/345 , A61K31/381 , A61K31/382 , A61K31/403 , A61K31/405 , A61K31/407 , C07D209/16 , C07D209/34 , C07D209/36 , C07D209/38 , C07D277/82 , C07D453/04 , C07D471/04 , C07D487/08 , C07D491/04 , C07D495/04
摘要： The present invention provides compounds and methods of administering compounds to a subject that can reduce βAPP production and that is not toxic in a wide range of dosages. The present invention also provides non-carbamate compounds and methods of administering such compounds to a subject that can reduce βAPP production and that is not toxic in a wide range of dosages. It has been discovered that either the racemic or enantiomerically pure non-carbamate compounds can be used to decrease βAPP production.
摘要翻译：本发明提供了向受试者施用化合物和方法，所述方法可以减少和产生APP，并且在广泛的剂量范围内是无毒的。本发明还提供了非氨基甲酸酯化合物和向受试者施用此类化合物的方法，所述方法可以减少APP生产并且在广泛剂量范围内不具有毒性。已经发现外消旋或对映体纯的非氨基甲酸酯化合物可用于减少和生产APP生产。

2. 发明申请

US20130035363A1 Thalidomide Analogs 有权
标题翻译：沙利度胺类似物
公开(公告)号：US20130035363A1
公开(公告)日：2013-02-07
申请号：US13648625
申请日：2012-10-10
申请人： Nigel H. Greig , Harold Holloway , Arnold Brossi , Xiaoxiang Zhu , Tony Giordano , Qian-sheng Yu , William D. Figg
发明人： Nigel H. Greig , Harold Holloway , Arnold Brossi , Xiaoxiang Zhu , Tony Giordano , Qian-sheng Yu , William D. Figg
IPC分类号： A61K31/4035 , A61P3/04 , A61P19/02 , A61P31/04 , A61P1/00 , A61P35/00 , A61P25/00 , A61P25/28 , A61P25/16 , A61P7/04 , A61P27/02 , A61P29/00 , A61P1/04
CPC分类号： H04M1/72522 , C07D209/44 , G06F3/01 , G06F3/0346 , H04M2250/12 , H04M2250/22 , H04M2250/74
摘要： Thalidomide analogs that modulate tumor necrosis factor alpha (TNFα) activity and angiogenesis are disclosed. In particularly disclosed embodiments, the thalidomide analogs are isosteric sulfur-containing analogs. Also disclosed are methods of treating a subject with the analogs.
摘要翻译：公开了调节肿瘤坏死因子α（TNFα）活性和血管生成的沙利度胺类似物。在特别公开的实施方案中，沙利度胺类似物是等熵含硫类似物。还公开了用类似物治疗受试者的方法。

3. 发明申请

US20110021594A1 Agents Useful for Reducing Amyloid Precursor Protein and Treating Dementia and Methods of Use Thereof 有权
标题翻译：可用于降低淀粉样蛋白前体蛋白和治疗痴呆的药剂及其使用方法
公开(公告)号：US20110021594A1
公开(公告)日：2011-01-27
申请号：US12841888
申请日：2010-07-22
申请人： Nigel H. Greig , Karen T.Y. Shaw , Qiang-Sheng Yu , Harold W. Holloway , Tada Utsuki , Timothy T. Soncrant , Donald K. Ingram , Arnold Brossi , Anthony Giordano , Gordon Powers , Diane Davidson , Michael Sturgess
发明人： Nigel H. Greig , Karen T.Y. Shaw , Qiang-Sheng Yu , Harold W. Holloway , Tada Utsuki , Timothy T. Soncrant , Donald K. Ingram , Arnold Brossi , Anthony Giordano , Gordon Powers , Diane Davidson , Michael Sturgess
IPC分类号： A61K31/407 , A61P25/28
CPC分类号： C07D487/04 , A61K31/325 , A61K31/343 , A61K31/345 , A61K31/381 , A61K31/382 , A61K31/403 , A61K31/405 , A61K31/407 , C07D209/16 , C07D209/34 , C07D209/36 , C07D209/38 , C07D277/82 , C07D453/04 , C07D471/04 , C07D487/08 , C07D491/04 , C07D495/04
摘要： The present invention provides compounds and methods of administering compounds to a subject that can reduce βAPP production and that is not toxic in a wide range of dosages. The present invention also provides non-carbamate compounds and methods of administering such compounds to a subject that can reduce βAPP production and that is not toxic in a wide range of dosages. It has been discovered that either the racemic or enantiomerically pure non-carbamate compounds can be used to decrease βAPP production.
摘要翻译：本发明提供了向受试者施用化合物和方法，所述方法可以减少和产生APP，并且在广泛的剂量范围内是无毒的。本发明还提供了非氨基甲酸酯化合物和向受试者施用此类化合物的方法，所述方法可以减少APP生产并且在广泛剂量范围内不具有毒性。已经发现外消旋或对映体纯的非氨基甲酸酯化合物可用于减少和生产APP生产。

4. 发明授权

US3946041A 6-(3,4-Methylenedioxy-6-benzylalkylaminoethylphenylacetyl)benzoic acid alkyl ester derivatives 失效
标题翻译： 6-（3,4-亚甲二氧基-6-苄基烷基氨基乙基苯基乙酰基）苯甲酸烷基酯衍生物
公开(公告)号：US3946041A
公开(公告)日：1976-03-23
申请号：US386668
申请日：1973-08-08
申请人： Arnold Brossi , Wilhelm Kloetzer , Sidney Teitel
发明人： Arnold Brossi , Wilhelm Kloetzer , Sidney Teitel
IPC分类号： C07D317/60 , C07D317/68
CPC分类号： C07D317/60
摘要： The present invention relates to the preparation of novel rheadan-type alkaloids and to novel intermediates useful in the preparation thereof. The process utilizes as starting materials a known class of alkaloids of the narcotine or of the hydrastine type. Certain of the said novel intermediates are also pharmaceutically useful in and of themselves. Additionally, certain of the novel intermediates can be converted into other type alkaloids which are also pharmaceutically useful.
摘要翻译：本发明涉及新型r头型生物碱的制备及其制备中可用的新型中间体。该方法利用了已知类型的氨基酸或hydrastine类型的生物碱作为起始物质。所述新型中间体中的某些也在其本身也是有用的。此外，某些新型中间体可以转化为其它类似的生物碱，其也是药学上可用的。

5. 发明授权

US5175342A Esters of 3-demethylthiocolchicine and n-acyl analogs 失效
标题翻译： 3-脱甲基硫代秋水仙素和N-酰基类似物的酯
公开(公告)号：US5175342A
公开(公告)日：1992-12-29
申请号：US686853
申请日：1991-04-18
申请人： Arnold Brossi
发明人： Arnold Brossi
IPC分类号： C07C323/41
CPC分类号： C07C323/41
摘要： The present invention relates to esters of 3-demethylthiocolchicine and N-acyl analogs thereof having the following formula: ##STR1## wherein R is O-CO-alkyl, O-CO-CH.sub.2 Oalkyl, O-CO-Phenyl, O-COOalkyl; the alkyl group having from 1 to 4 carbon atoms and the Ac group representing acetyl and its higher homologs, benzoyl, alkoxyacetyl, or haloacetyl.The invention further relates to processes for preparing these ester compounds, pharmaceutical compositions thereof and methods for treating diseases such as gout, Mediterranean fever and liver disorders.
摘要翻译：本发明涉及3-脱甲基硫代秋水仙碱及其N-酰基类似物的具有下式的酯：其中R是O-CO-烷基，O-CO-CH2O烷基，O-CO-苯基，O-COO烷基; 具有1至4个碳原子的烷基和Ac基团代表乙酰基及其较高同系物，苯甲酰基，烷氧基乙酰基或卤代乙酰基。本发明进一步涉及制备这些酯化合物的方法，其药物组合物和治疗诸如痛风，地中海热和肝病等疾病的方法。

6. 发明授权

US5171750A Substituted phenserines as specific inhibitors of acetylcholinesterase 失效
标题翻译：取代的苯西林作为乙酰胆碱酯酶的特异性抑制剂
公开(公告)号：US5171750A
公开(公告)日：1992-12-15
申请号：US765746
申请日：1991-09-26
申请人： Arnold Brossi , Malgarzota Brzostowska , Stanley I. Rapoport , Nigel Greig , Xiao-shu He
发明人： Arnold Brossi , Malgarzota Brzostowska , Stanley I. Rapoport , Nigel Greig , Xiao-shu He
IPC分类号： C07D487/04 , C07D491/04 , C07D491/048
CPC分类号： C07D487/04 , C07D491/04
摘要： The present invention relates to substituted phenylcarbamate or naphthylcarbamate tricyclic compounds which provide highly potent and selective cholinergic agonist and blocking activity and their use as pharmaceutical agents. The invention further relates to improvements in therapy relative to cholinergic diseases such as glacuoma, Myasthenia Gravis, Alzheimer's disease and to improvements in therapy and organophosphate poisoning. The invention further provides for a selective acetylcholinesterase and butyrylcholinesterase agents and a method for inhibiting these esterases.
摘要翻译：本发明涉及提供高效和选择性胆碱能激动剂和阻断活性的取代的苯基氨基甲酸酯或萘基氨基甲酸三环化合物及其作为药剂的用途。本发明还涉及治疗相对于胆碱能疾病如冰川，重症肌无力，阿尔茨海默病以及治疗和有机磷酸盐中毒方面的改进。本发明进一步提供选择性乙酰胆碱酯酶和丁酰胆碱酯酶及其抑制这些酯酶的方法。

7. 发明授权

US5011951A Synthesis of artemisininelactol derivatives 失效
标题翻译：青蒿素衍生物的合成
公开(公告)号：US5011951A
公开(公告)日：1991-04-30
申请号：US316282
申请日：1989-02-27
申请人： Peter Buchs , Arnold Brossi
发明人： Peter Buchs , Arnold Brossi
IPC分类号： C07D493/20
CPC分类号： C07D493/20
摘要： A process for the epimerization of .alpha.- to .beta.-ethyletherartemisininelactol (arteether) or preparation of arteether, useful in the treatment of malaria, from artemisininelactol, comprises reacting starting material in a solvent including an acid catalyst, the reaction of artemisininelactol also including an etherifying ethyl moiety, and isolating the product.

8. 发明授权

US4533675A Carbamates of colchicine for treatment of gout 失效
标题翻译：用于治疗痛风的秋水仙碱的氨基转移酶
公开(公告)号：US4533675A
公开(公告)日：1985-08-06
申请号：US601314
申请日：1984-04-17
申请人： Arnold Brossi , Peter Kerekes
发明人： Arnold Brossi , Peter Kerekes
IPC分类号： A61K31/24 , C07C271/06 , C07C125/065 , C07C125/067
CPC分类号： A61K31/24 , C07C271/06
摘要： The present invention consists of derivatives of colchicine and thiocolchicine which are carbamates of the same and are illustrated by the formula below: ##STR1## where either X.sub.1 or X.sub.2 is a hydroxy group and the other a lower alkoxy group and R.sub.1 can be H or an alkyl, R.sub.2 an alkyl, alkenyl or aryl which may be substituted and R.sub.3 is either OCH.sub.3 or SCH.sub.3 ; alkyl and alkoxy=C.sub.1 -C.sub.6 ; aryl=monoaryl.These compounds are not only new but have exhibited antitumor activity binding to tubulin protein and tests against P388 lymphocytic leukemia and also active against gouty arthritis. Further, they are far less toxic than colchicine.
摘要翻译：本发明由秋水仙素和硫代秋水仙素的衍生物组成，它们是氨基甲酸酯的衍生物，它们由下式表示：其中X1或X2是羟基，另一个是低级烷氧基，R1可以是H或烷基，R 2为可被取代的烷基，烯基或芳基，R 3为OCH 3或SCH 3; 烷基和烷氧基= C1-C6; 芳基=单芳基。这些化合物不仅是新的，而且具有结合微管蛋白的抗肿瘤活性和针对P388淋巴细胞性白血病的抗肿瘤活性，并且对抗痛风性关节炎也是有效的。此外，它们比秋水仙碱毒性低得多。

9. 发明授权

US4065473A Intermediates in the preparation of 2,3,4,5-tetrahydro-1H-3-benzazepines 失效
标题翻译：中间体制备2,3,4,5-四氢-1H-3-苯并吖庚因
公开(公告)号：US4065473A
公开(公告)日：1977-12-27
申请号：US588985
申请日：1975-06-20
申请人： Arnold Brossi , Benjamin Pecherer , Robert Sunbury
发明人： Arnold Brossi , Benjamin Pecherer , Robert Sunbury
IPC分类号： C07D209/48 , C07D491/056 , C07D317/44
CPC分类号： C07D209/48 , C07D491/056 , Y10S514/87 , Y10S514/96 , Y10S514/962
摘要： A process for the preparation of heterocyclic compounds containing one nitrogen atom and novel 2,3,4,5-tetrahydro-1H-3-benzazepines prepared by this process are disclosed. The resulting heterocyclic compounds, including the novel 2,3,4,5-tetrahydro-1H-3-benzazepine derivatives, exhibit analgesic, appetite suppressant, and anti-edema activity.
摘要翻译：公开了制备含有一个氮原子的杂环化合物的方法和通过该方法制备的新的2,3,4,5-四氢-1H-3-苯并氮杂。所得的杂环化合物，包括新的2,3,4,5-四氢-1H-3-苯并氮杂衍生物显示出止痛，食欲抑制和抗水肿活性。

10. 发明授权

US08258172B2 Agents useful for reducing amyloid precursor protein and treating dementia and methods of use thereof 有权
标题翻译：可用于降低淀粉样蛋白前体蛋白和治疗痴呆的药剂及其使用方法
公开(公告)号：US08258172B2
公开(公告)日：2012-09-04
申请号：US12841888
申请日：2010-07-22
申请人： Nigel H. Greig , Karen T. Y. Shaw , Qiang-Sheng Yu , Harold W. Holloway , Tada Utsuki , Timothy T. Soncrant , Donald K. Ingram , Arnold Brossi , Anthony Giordano , Gordon Powers , Diane M. Davidson , Michael Sturgess
发明人： Nigel H. Greig , Karen T. Y. Shaw , Qiang-Sheng Yu , Harold W. Holloway , Tada Utsuki , Timothy T. Soncrant , Donald K. Ingram , Arnold Brossi , Anthony Giordano , Gordon Powers , Diane M. Davidson , Michael Sturgess
IPC分类号： A61K31/40
CPC分类号： C07D487/04 , A61K31/325 , A61K31/343 , A61K31/345 , A61K31/381 , A61K31/382 , A61K31/403 , A61K31/405 , A61K31/407 , C07D209/16 , C07D209/34 , C07D209/36 , C07D209/38 , C07D277/82 , C07D453/04 , C07D471/04 , C07D487/08 , C07D491/04 , C07D495/04
摘要： The present invention provides compounds and methods of administering compounds to a subject that can reduce βAPP production and that is not toxic in a wide range of dosages. The present invention also provides non-carbamate compounds and methods of administering such compounds to a subject that can reduce βAPP production and that is not toxic in a wide range of dosages. It has been discovered that either the racemic or enantiomerically pure non-carbamate compounds can be used to decrease βAPP production.
摘要翻译：本发明提供了向受试者施用化合物和方法，所述方法可以减少和产生APP，并且在广泛的剂量范围内是无毒的。本发明还提供了非氨基甲酸酯化合物和向受试者施用此类化合物的方法，所述方法可以减少APP生产并且在广泛剂量范围内不具有毒性。已经发现外消旋或对映体纯的非氨基甲酸酯化合物可用于减少和生产APP生产。

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