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1. 发明申请

WO1998006708A1 CRYTALLINE FORM OF 4-[5-METHYL-3-PHENYLISOXAZOL-4-YL]BENZENESULFONAMIDE 审中-公开
标题翻译： 4- [5-甲基-3-苯基恶唑-4-基]苯甲酰胺的结晶形式
公开(公告)号：WO1998006708A1
公开(公告)日：1998-02-19
申请号：PCT/US1997015126
申请日：1997-08-12
申请人： G.D. SEARLE & CO. , TALLEY, John, J. , MEDICH, John, R. , MCLAUGHLIN, Kathleen, T. , GAUD, Henry, T. , YONAN, Edward, E.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D261/08
CPC分类号： H01L23/4006 , C07D261/08 , H01L23/427 , H01L2924/0002 , H01L2924/00
摘要： A stable crystalline form of 4-[5-methyl-3-phenylisoxazol-4-yl]benzenesulfonamide is described. This crystal structure, designated Form B, is more stable, has favorable handling properties and is characterized by its melting point, x-ray and other physical characterizations.
摘要翻译：描述了4- [5-甲基-3-苯基异恶唑-4-基]苯磺酰胺的稳定结晶形式。这种晶体结构称为B型，更稳定，具有良好的操作性能，其特点是熔点，X射线等物理特性。

2. 发明申请

WO2008063213A2 USES AND COMPOSITIONS FOR TREATMENT OF PSORIATIC ARTHRITIS 审中-公开
标题翻译：用于治疗精神障碍的用途和组合物
公开(公告)号：WO2008063213A2
公开(公告)日：2008-05-29
申请号：PCT/US2007/008820
申请日：2007-04-10
申请人： ABBOTT BIOTECHNOLOGY LTD. , MEDICH, John, R. , WONG, Robert, L. , PERDOK, Renee, J. , SASSO, Eric, H. , HOFFMAN, Rebecca, S. , MEASE, Phillip, J. , RITCHLIN, Christopher, T.
发明人： MEDICH, John, R. , WONG, Robert, L. , PERDOK, Renee, J. , SASSO, Eric, H. , HOFFMAN, Rebecca, S. , MEASE, Phillip, J. , RITCHLIN, Christopher, T.
IPC分类号： A61K39/395 , G01N33/68 , A61K39/09 , A61K39/145 , A61P37/00 , A61P19/02
CPC分类号： C07K16/241 , A61K2039/505 , A61K2039/545 , A61K2039/55 , C07K2317/21 , C07K2317/565 , C07K2317/76 , G01N2800/102
摘要： The invention provides methods, uses and compositions for the treatment of psoriatic arthritis. The invention describes methods and uses for treating psoriatic arthritis, wherein a TNFα inhibitor, such as a human TNFα antibody, or antigen-binding portion thereof, is used to psoriatic arthritis in a subject. Also described are methods for determining the efficacy of a TNFα inhibitor for treatment of psoriatic arthritis in a subject.
摘要翻译：本发明提供了用于治疗牛皮癣关节炎的方法，用途和组合物。本发明描述了治疗牛皮癣关节炎的方法和用途，其中TNFα抑制剂如人TNFα抗体或其抗原结合部分用于受试者的银屑病关节炎。还描述了确定TNFα抑制剂治疗受试者银屑病关节炎的功效的方法。

3. 发明申请

WO2008154543A3 METHODS FOR TREATING JUVENILE IDIOPATHIC ARTHRITIS 审中-公开
标题翻译：治疗轻度发育不良症的方法
公开(公告)号：WO2008154543A3
公开(公告)日：2009-04-23
申请号：PCT/US2008066438
申请日：2008-06-10
申请人： ABBOTT BIOTECH LTD , MEDICH JOHN R , PAULSON SUSAN K , NOERTERSHEUSER PETER A
发明人： MEDICH JOHN R , PAULSON SUSAN K , NOERTERSHEUSER PETER A
IPC分类号： G01N33/53 , C07K16/00
CPC分类号： A61K39/3955 , A61K9/0019 , A61K31/155 , A61K31/519 , A61K2039/505 , C07K16/241 , C07K2317/21
摘要： The invention provides methods and compositions for the treatment of juvenile idiopathic arthritis (JIA) where a TNFa inhibitor, such as a human TNFa antibody, or antigen-binding portion thereof, is used to treat JIA. In particular, the invention is directed to methods and compositions relating to a fixed dosing regimen for treating JIA with a TNFa inhibitor.
摘要翻译：本发明提供了用于治疗青少年特发性关节炎（JIA）的方法和组合物，其中使用TNFα抑制剂，例如人TNFα抗体或其抗原结合部分来治疗JIA。特别地，本发明涉及与用TNFα抑制剂治疗JIA的固定给药方案相关的方法和组合物。

4. 发明申请

WO2008154543A2 METHODS FOR TREATING JUVENILE IDIOPATHIC ARTHRITIS 审中-公开
标题翻译：治疗轻度发育不良症的方法
公开(公告)号：WO2008154543A2
公开(公告)日：2008-12-18
申请号：PCT/US2008/066438
申请日：2008-06-10
申请人： ABBOTT BIOTECHNOLOGY LTD. , MEDICH, John, R. , PAULSON, Susan, K. , NOERTERSHEUSER, Peter, A.
发明人： MEDICH, John, R. , PAULSON, Susan, K. , NOERTERSHEUSER, Peter, A.
IPC分类号： A61K39/395
CPC分类号： A61K39/3955 , A61K9/0019 , A61K31/155 , A61K31/519 , A61K2039/505 , C07K16/241 , C07K2317/21
摘要： The invention provides methods and compositions for the treatment of juvenile idiopathic arthritis (JIA) where a TNFα inhibitor, such as a human TNFα antibody, or antigen-binding portion thereof, is used to treat JIA. In particular, the invention is directed to methods and compositions relating to a fixed dosing regimen for treating JIA with a TNFα inhibitor.
摘要翻译：本发明提供了用于治疗青少年特发性关节炎（JIA）的方法和组合物，其中使用TNFα抑制剂，例如人TNFα抗体或其抗原结合部分来治疗JIA。特别地，本发明涉及与用TNFα抑制剂治疗JIA的固定给药方案相关的方法和组合物。

5. 发明申请

WO2008063213A3 USES AND COMPOSITIONS FOR TREATMENT OF PSORIATIC ARTHRITIS 审中-公开
标题翻译：用于治疗精神障碍的用途和组合物
公开(公告)号：WO2008063213A3
公开(公告)日：2009-04-02
申请号：PCT/US2007008820
申请日：2007-04-10
申请人： ABBOTT BIOTECH LTD , MEDICH JOHN R , WONG ROBERT L , PERDOK RENEE J , SASSO ERIC H , HOFFMAN REBECCA S , MEASE PHILLIP J , RITCHLIN CHRISTOPHER T
发明人： MEDICH JOHN R , WONG ROBERT L , PERDOK RENEE J , SASSO ERIC H , HOFFMAN REBECCA S , MEASE PHILLIP J , RITCHLIN CHRISTOPHER T
IPC分类号： A61K38/00
CPC分类号： C07K16/241 , A61K2039/505 , A61K2039/545 , A61K2039/55 , C07K2317/21 , C07K2317/565 , C07K2317/76 , G01N2800/102
摘要： The invention provides methods, uses and compositions for the treatment of psoriatic arthritis. The invention describes methods and uses for treating psoriatic arthritis, wherein a TNFa inhibitor, such as a human TNFa antibody, or antigen-binding portion thereof, is used to psoriatic arthritis in a subject. Also described are methods for determining the efficacy of a TNFa inhibitor for treatment of psoriatic arthritis in a subject.
摘要翻译：本发明提供了用于治疗牛皮癣关节炎的方法，用途和组合物。本发明描述了治疗牛皮癣关节炎的方法和用途，其中TNFα抑制剂如人TNFα抗体或其抗原结合部分用于受试者的银屑病关节炎。还描述了确定TNFα抑制剂治疗受试者银屑病关节炎的功效的方法。

6. 发明申请

WO2007120651A3 USES AND COMPOSITIONS FOR TREATMENT OF JUVENILE RHEUMATOID ARTHRITIS 审中-公开
标题翻译：用于治疗妊娠高血压病的药物和组合物
公开(公告)号：WO2007120651A3
公开(公告)日：2008-07-31
申请号：PCT/US2007008826
申请日：2007-04-10
申请人： ABBOTT BIOTECH LTD , MEDICH JOHN R , RUPERTO NICOLINO , MARTINI ALBERTO , LOVELL DANIEL J , GIANNINI EDWARD H
发明人： MEDICH JOHN R , RUPERTO NICOLINO , MARTINI ALBERTO , LOVELL DANIEL J , GIANNINI EDWARD H
IPC分类号： A61K39/395
CPC分类号： C07K16/241 , A61K2039/505 , C07K2317/21
摘要： The invention provides methods, uses and compositions for the treatment of juvenile rheumatoid arthritis (JRA). The invention describes methods and uses for treating JRA, wherein a TNFa inhibitor, such as a human TNFa antibody, or antigenbinding portion thereof, is used to prevent flare-ups associated with JRA. Also described are methods for determining the efficacy of a TNFa inhibitor for treatment of JRA in a subject.
摘要翻译：本发明提供了用于治疗少年类风湿性关节炎（JRA）的方法，用途和组合物。本发明描述了用于治疗JRA的方法和用途，其中使用TNFα抑制剂，例如人TNFα抗体或其抗原结合部分，以防止与JRA相关的爆发。还描述了确定TNFα抑制剂治疗受试者中JRA的功效的方法。

7. 发明申请

WO1997003947A1 PROCESS FOR THE PREPARATION OF ETHYL 3S-[[4-[[4-(AMINOIMINOMETHYL)PHENYL]AMINO]-1,4-DIOXOBUTYL]AMINO]-4-PENTYNOATE 审中-公开
标题翻译：乙基3S- [[4 - [[4-（氨基亚氨基）苯基]氨基] -1,4-二氧代丁基]氨基] -4-戊酸的制备方法
公开(公告)号：WO1997003947A1
公开(公告)日：1997-02-06
申请号：PCT/US1996010658
申请日：1996-07-12
申请人： G.D. SEARLE & CO. , BABIAK, Kevin, A. , BABU, Srinivasan , BEHLING, James, R. , BOYS, Mark, L. , CAIN-JANICKI, Kimberly, J. , DOUBLEDAY, Wendell, W. , FARID, Payman , HAGEN, Timothy, J. , HALLINAN, E., Ann , HANSEN, Donald, W., Jr. , KORTE, Donald, E. , MC LAUGHLIN, Kathleen, T. , MEDICH, John, R. , NUGENT, Sean, T. , ORLOVSKI, Vlasdislav , PARK, Jung, M. , PETERSON, Karen, B. , PILIPAUSKAS, Daniel, R. , PITZELE, Barnett, S. , TSYMBALOV, Sofya , STAHL, Glenn, L.
发明人： G.D. SEARLE & CO.
IPC分类号： C07C249/12
CPC分类号： C07C227/12 , C07C227/34 , C07C257/18
摘要： The present invention relates to a novel process for the preparation of ethyl 3S-[[4-[[4-(aminoiminomethyl)-phenyl]amino]-1,4-dioxobutyl]amino]-4-pentynoate and pharmaceutically acceptable acid addition salt thereof which comprises treating (trimethylsilyl)acetylene sequentially with n-butyllitium and 4-formylmorpholine followed by acid hydrolysis to give 3-(trimethylsilyl)-2-propynal; treating 3-(trimethylsilyl)-2-propynal with lithium bis(trimethylsilyl)amide to give in situ N,3-bis(trimethylsilyl)-2-propyn-1-imine; condensation of N,3-bis(trimethylsilyl)-2-propyn-1-imine with lithium t-butyl acetate to give (+/-)1,1-dimethylethyl 3-amino-5-(trimethylsilyl)-4-pentynoate; treating (+/-)1,1-dimethylethyl 3-amino-5-(trimethylsilyl)-4-pentynoate- with p-toluenesulfonic acid to give (+/-)1,1-dimethylethyl 3-amin-5-(trimethylsilyl)-4-pentynoate, mono p-toluenesulfonic acid salt, treatment of resulting salt with ethanol in the presence of p-toluenesulfonic acid to give (+/-)ethyl 3-amino-5-(trimethylsilyl)-4-pentynoate; desilylation of (+/-)ethyl 3-amino-5-(trimethylsilyl)-4-pentynoate to give in situ (+/-)ethyl 3-amino-4-pentynoate; resolution of (+/-)ethyl 3-amino-4-pentynoate using (R)-(-)-mandelic acid and treatment of the resolved product with gaseous hydrochloric acid to give ethyl 3S-amino-4-pentynoate, monohydrochloride; coupling the ethyl 3S-amino-4-pentynoate, monohydrochloride to 4-[[4-(aminoiminomethyl)phenyl]amino]-4-oxobutanoic acid, monohydrochloride in the presence of isobutyl chloroformate and N-methylmorpholine to give ethyl 3S-[[4-[[4-(aminoiminomehtyl)phenyl]amino]-1,4-dioxobutyl]amino]-4-pentynoate, monohydrochloride.
摘要翻译：本发明涉及制备3S - [[4 - [[4-（氨基亚氨基甲基） - 苯基]氨基] -1,4-二氧代丁基]氨基] -4-戊酸乙酯和药学上可接受的酸加成盐的新方法其包括依次用正丁基鎓和4-甲酰基吗啉处理（三甲基甲硅烷基）乙炔，然后酸水解，得到3-（三甲基甲硅烷基）-2-丙炔醛; 用双（三甲基甲硅烷基）氨基锂处理3-（三甲基甲硅烷基）-2-丙炔醛，得到原位N，3-二（三甲基甲硅烷基）-2-丙炔-1-亚胺; N，3-二（三甲基甲硅烷基）-2-丙炔-1-亚胺与乙酸叔丁酯的缩合得到3-氨基-5-（三甲基甲硅烷基）-4-戊炔酸（+/-）1,1-二甲基乙酯; 用对甲苯磺酸处理（+/-）3-氨基-5-（三甲基甲硅烷基）-4-戊酸乙酯（+/-）1,1-二甲基乙基酯，得到3-氨基-5-（三甲基甲硅烷基）-4-戊酸酯，单对甲苯磺酸盐，在对甲苯磺酸存在下用乙醇处理所得的盐，得到（+/-）3-氨基-5-（三甲基甲硅烷基）-4-戊酸乙酯; （+/-）乙基3-氨基-5-（三甲基甲硅烷基）-4-戊酸乙酯脱甲硅烷基，得到原位（+/-）3-氨基-4-戊酸乙酯; 使用（R） - （ - ） - 扁桃酸分解（+/-）乙基3-氨基-4-戊炔酸，并用气态盐酸处理分离产物，得到3S-氨基-4-戊酸乙酯，一盐酸盐; 将3S-氨基-4-戊酸乙酯，一盐酸盐在氯甲酸异丁酯和N-甲基吗啉存在下，将4 - [[4-（氨基亚氨基甲基）苯基]氨基] -4-氧代丁酸单盐酸盐偶合，得到3S- [ 4 - [[4-（氨基亚氨基甲基）苯基]氨基] -1,4-二氧代丁基]氨基] -4-戊酸乙酯，一盐酸盐。

8. 发明申请

WO1991017145A1 PROCESS FOR PREPARATION OF 1,5-(ALKYLIMINO)-1,5-DIDEOXY-D-GLUCITOL AND DERIVATIVES THEREOF 审中-公开
标题翻译：制备1,5-（阿霉素）-1,5-二脱氧-D-葡萄糖苷及其衍生物的方法
公开(公告)号：WO1991017145A1
公开(公告)日：1991-11-14
申请号：PCT/US1991002986
申请日：1991-05-01
申请人： G.D. SEARLE & CO. , BEHLING, James, R. , FARID, Payman , KHANNA, Ish , MEDICH, John, R. , PRUNIER, Mike , SCAROS, Mike , WEIER, Richard, M.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D211/46
CPC分类号： C07D493/10 , C07D211/46 , C07D307/20
摘要： Process for the preparation of 1,5-(alkylimino)-1,5-dideoxy-D-glucitol and derivatives thereof. Described is a process for the preparation of 1,5-(n-butylimino)-1,5-dideoxy-D-glucitol and similar compounds and to the use of an adsorption hydrogenation protocol.
摘要翻译：制备1,5-（烷基亚氨基）-1,5-二脱氧-D-葡萄糖醇及其衍生物的方法。描述了制备1,5-（正丁基亚氨基）-1,5-二脱氧-D-葡萄糖醇和类似化合物以及使用吸附氢化方案的方法。

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