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1. 发明申请

WO1996038142A1 1H-4(5)-SUBSTITUTED IMIDAZOLE DERIVATIVES 审中-公开
标题翻译： 1H-4（5） - 取代的咪唑衍生物
公开(公告)号：WO1996038142A1
公开(公告)日：1996-12-05
申请号：PCT/US1996007873
申请日：1996-05-29
申请人： GLIATECH, INC. , PHILLIPS, James, G. , TEDFORD, Clark, E. , CHATURVEDI, Nishith, C.
发明人： GLIATECH, INC.
IPC分类号： A61K31/415
CPC分类号： C07D233/56 , A61K31/417 , A61K31/4174 , A61K31/4178 , C07D233/64 , C07D403/12 , C07D405/12
摘要： The present invention provides, in its principal aspect, compounds of general formula (1.0) or a pharmaceutically acceptable salt or hydrate thereof, wherein: where A is -NHCO-, -N(CH3)-CO-, -NHCH2-, -N(CH3)-CH2-, -CH=CH-, -COCH2-, -CH2CH2-, -CH(OH)CH2-, or -CC-; X is H, CH3, NH2, NH(CH3), N(CH3)2, OH, OCH3, or SH; R2 is hydrogen or a methyl or ethyl group; R3 is hydrogen or a methyl or ethyl group; n is 0, 1, 2, 3, 4, 5, or 6; and R1 is selected from the group consisting of (a) C3 to C8 cycloalkyl; (b) phenyl or substituted phenyl; (d) heterocyclic; (e) decahydronaphthalene and (f) octahydroindene; or R1 and X may be taken together to denote a 5,6 or 6,6 saturated bicyclic ring structure when X is NH, O, or S. The individual stereoisomers of compounds of structural formula (1.0) above, as well as mixtures thereof, are also contemplated as falling within the scope of the present invention. The compounds of the present invention have H3 histamine receptor antagonist activity. This invention also provides pharmaceutical compositions comprising a pharmaceutically acceptable carrier in combination with an effective amount of a compound of formula 1.0. The present invention also provides a method of treating conditions in which antagonism of histamine H3 receptors may be of therapeutic importance.
摘要翻译：本发明在其主要方面提供了通式（1.0）的化合物或其药学上可接受的盐或水合物，其中：A是-NHCO - ， - N（CH 3）-CO - ， - NHCH 2 - ， - N （CH 3）-CH 2 - ， - CH = CH - ， - COCH 2 - ， - CH 2 CH 2 - ， - CH（OH）CH 2 - 或-CC-; X是H，CH 3，NH 2，NH（CH 3），N（CH 3）2，OH，OCH 3或SH; R2是氢或甲基或乙基; R3是氢或甲基或乙基; n是0，1，2，3，4，5或6; 并且R 1选自（a）C 3至C 8环烷基; （b）苯基或取代的苯基; （d）杂环; （e）十氢萘和（f）八氢茚; 或者当X是NH，O或S时，R 1和X可以一起表示5,6或6,6饱和的双环结构。上述结构式（1.0）化合物的各个立体异构体以及它们的混合物也被认为落入本发明的范围内。本发明化合物具有H3组胺受体拮抗剂活性。本发明还提供药物组合物，其包含药学上可接受的载体与有效量的式1.0化合物的组合。本发明还提供了治疗组胺H 3受体的拮抗作用具有治疗意义的病症的方法。

2. 发明申请

WO2003097668A3 NOVEL PROCESS FOR PRODUCTION OF THE SOMATOSTATIN ANALOG, OCTREOTIDE 审中-公开
公开(公告)号：WO2003097668A3
公开(公告)日：2003-11-27
申请号：PCT/IN2003/000160
申请日：2003-04-16
申请人： CHATURVEDI, Nishith, C. , BERI, Suresh , YEOLE, Ravindra, D. , DE SOUZA, Noel, J.
发明人： CHATURVEDI, Nishith, C. , BERI, Suresh , YEOLE, Ravindra, D. , DE SOUZA, Noel, J.
IPC分类号： C07K1/06
摘要： The present invention relates to a process for commercial production of octreotide using solution peptide chemistry and inexpensive amino acid derivatives. Thus the hexapeptide (Boc) D-Phe-Cys(Acm)-Phe-D-Trp-Lys(Boc)-Thr-OMe is synthesised by condensation of two tripeptide fragments, saponified and condensed with Cys(Acm)-Thr-OL to give the linear octapeptide alcohol. The linear peptide alcohol is treated with iodine, after removal of Boc groups, to give the cyclic peptide octreotide. The linear octapeptide alcohol can alternately be made by condensation of the protected hexapeptide acid with the dipeptide Cys(Acm)-Thr-OMe, followed by reduction with sodium borohydride.

3. 发明申请

WO03097668A2 NOVEL PROCESS FOR PRODUCTION OF THE SOMATOSTATIN ANALOG, OCTREOTIDE 审中-公开
标题翻译：生产SOMATOSTATIN ANALOG，OCTREOTIDE的新工艺
公开(公告)号：WO03097668A2
公开(公告)日：2003-11-27
申请号：PCT/IN0300160
申请日：2003-04-16
申请人： CHATURVEDI NISHITH C , BERI SURESH , YEOLE RAVINDRA D , DE SOUZA NOEL J
发明人： CHATURVEDI NISHITH C , BERI SURESH , YEOLE RAVINDRA D , DE SOUZA NOEL J
IPC分类号： C07K5/087 , C07K5/097 , C07K14/655 , C07K1/06 , C07K1/107 , C07K1/113 , C07K5/09 , C07K7/06
CPC分类号： C07K5/0821 , C07K5/0812 , C07K14/6555
摘要： The present invention relates to a process for commercial production of octreotide using solution peptide chemistry and inexpensive amino acid derivatives. Thus the hexapeptide (Boc) D-Phe-Cys(Acm)-Phe-D-Trp-Lys(Boc)-Thr-OMe is synthesised by condensation of two tripeptide fragments, saponified and condensed with Cys(Acm)-Thr-OL to give the linear octapeptide alcohol. The linear peptide alcohol is treated with iodine, after removal of Boc groups, to give the cyclic peptide octreotide. The linear octapeptide alcohol can alternately be made by condensation of the protected hexapeptide acid with the dipeptide Cys(Acm)-Thr-OMe, followed by reduction with sodium borohydride.
摘要翻译：本发明涉及使用溶液肽化学和便宜的氨基酸衍生物商业生产奥曲肽的方法。因此，通过两个三肽片段的缩合合成六肽（Boc）D-Phe-Cys（Acm）-Phe-D-Trp-Lys（Boc）-Thr-OMe），将其与Cys（Acm）-Thr-OL皂化和缩合得到线性八肽醇。线性肽醇用碘处理后除去Boc基团，得到环肽奥曲肽。线性八肽醇可以交替地通过保护的六肽酸与二肽Cys（Acm）-Thr-OMe的缩合，然后用硼氢化钠还原来制备。

4. 发明申请

WO0209758A3 INHIBITORS OF CELLULAR EFFLUX PUMPS OF MICROBES 审中-公开
标题翻译：微生物细胞流出物的抑制剂
公开(公告)号：WO0209758A3
公开(公告)日：2002-12-27
申请号：PCT/IN0100139
申请日：2001-07-31
申请人： DE SOUZA NOEL J , PATEL MAHESH V , GUPTE SHRIKANT V , UPADHYAY DILIP J , SHUKLA MILIND C , CHATURVEDI NISHITH C , BHAWSAR SATISH B , NAIR SHEELA C , JAFRI MOHAMMED A , KHORAKIWALA HABIL F , WOCKHARDT LTD
发明人： DE SOUZA NOEL J , PATEL MAHESH V , GUPTE SHRIKANT V , UPADHYAY DILIP J , SHUKLA MILIND C , CHATURVEDI NISHITH C , BHAWSAR SATISH B , NAIR SHEELA C , JAFRI MOHAMMED A , KHORAKIWALA HABIL F
IPC分类号： A61K45/06 , A61P31/00 , C07D215/22 , C07D215/233 , C07D401/04 , C07D401/14 , C07D413/12 , C07D455/04 , C07D471/04 , C07D471/08 , C07D519/00
CPC分类号： A61K31/546 , A61K31/65 , A61K31/7048 , A61K45/06 , C07D215/233 , C07D401/04 , C07D401/14 , C07D413/12 , C07D455/04 , C07D471/04 , C07D471/08 , A61K2300/00
摘要： Compounds are described which are efflux pump inhibitors of cellular efflux pumps of microbes. Also described are methods of preparing such compounds, methods of using such efflux pump inhibitor compounds and pharmaceutical compositions which include such compounds.
摘要翻译：描述了作为微生物细胞外排泵的外排泵抑制剂的化合物。还描述了制备这些化合物的方法，使用这种外排泵抑制剂化合物的方法和包含这些化合物的药物组合物。

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