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公开(公告)号：US6166060A
公开(公告)日：2000-12-26
申请号：US948801
申请日：1997-10-10
IPC分类号： C07D233/58 , A61K31/415 , A61K31/417 , A61K31/4178 , A61K31/47 , A61P1/00 , A61P9/00 , A61P25/00 , A61P25/18 , A61P25/28 , A61P29/00 , A61P37/08 , C07D233/54 , C07D233/60 , C07D233/64 , C07D401/12 , C07D403/12 , C07D405/12 , A61K31/4174
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 the general formula: ##STR1## when A is --NHCO--, --N(CH.sub.3)--CO--, --NHCH.sub.2 --, --N(CH.sub.3)--CH.sub.2 --, --CH.dbd.CH--, --COCH.sub.2 --, CH.sub.2 CH.sub.2 --, --CH(OH)CH.sub.2 -- or --C.tbd.C--;X can be H, CH.sub.3, NH.sub.2, NH(CH.sub.3),N(CH.sub.3).sub.2, OH, OCH.sub.3, SH,R.sub.2 is hydrogen or a methyl or ethyl group;R.sub.3 is hydrogen or a methyl or ethyl group;n is 0, 1, 2, 3, 4, 5 or 6;R.sub.1 is selected from the group consisting of (a) alkyl; (b) C.sub.3 to C.sub.8 cycloalkyl; (c) phenyl or substituted phenyl; (d) heteroocyclic; and (f) decahydronaphthalene or octahydroindane; andWhen R.sub.1 and X taken together denote a 5, 6 or 6, 6 saturated bicyclic ring structure, X can be NH, O, S, SO.sub.2,When X is constrained in a 5, 6 or 6, 6, saturated bicyclic ring structure, then for example, when X.dbd.NH, R.sub.1 and X taken together mean an octahydroindole ring structure directly attached to A.
摘要翻译： 本发明在其主要方面提供了以下通式的化合物：当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-C X可以是H，CH 3，NH 2，NH（CH 3），N（CH 3）2，OH，OCH 3，SH，R 2是氢或甲基或乙基; R3是氢或甲基或乙基; n为0，1，2，3，4，5或6; R1选自（a）烷基; （b）C3至C8环烷基; （c）苯基或取代的苯基; （d）杂环; 和（f）十氢萘或八氢化茚; 当R 1和X一起表示5,6或6,6个饱和双环结构时，X可以是NH，O，S，SO 2，当X被约束在5,6或6,6饱和双环结构中时 ，那么例如当X = NH时，R 1和X一起表示直接连接到A的八氢吲哚环结构。
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公开(公告)号：US07098219B2
公开(公告)日：2006-08-29
申请号：US09919347
申请日：2001-07-31
申请人： Noel John de Souza , Mahesh Vithalbhai Patel , Shrikant V Gupte , Dilip J Upadhyay , Milind Chintaman Shukla , Nishith C Chaturvedi , Satish B Bhawsar , Sheela Chandresekharan Nair , Mohammed A Jafri , Habil Fakhruddin Khorakiwala
发明人： Noel John de Souza , Mahesh Vithalbhai Patel , Shrikant V Gupte , Dilip J Upadhyay , Milind Chintaman Shukla , Nishith C Chaturvedi , Satish B Bhawsar , Sheela Chandresekharan Nair , Mohammed A Jafri , Habil Fakhruddin Khorakiwala
IPC分类号： C07D471/04 , C07D471/02 , A61K31/44 , A61K31/47
CPC分类号： C07D215/233 , A61K45/06 , C07D401/04 , C07D401/14 , C07D413/12 , C07D455/04 , C07D471/04 , C07D471/08
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.
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公开(公告)号：US06987167B2
公开(公告)日：2006-01-17
申请号：US10153555
申请日：2002-05-22
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 synthesized 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），皂化并与Cys（Acm）-Thr-OL 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。
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公开(公告)号：US06448282B1
公开(公告)日：2002-09-10
申请号：US09631189
申请日：2000-08-02
IPC分类号： A61K31417
CPC分类号： C07D233/56 , A61K31/417 , A61K31/4174 , A61K31/4178 , C07D233/64
摘要： The present invention provides, in its principal aspect, compounds of the general formula: where A is —NHCO—, —N(CH3)—CO—, —NHCH2—, —N(CH3)—CH2—, —COCH2—, —CH2CH2—, or —CH(OH)CH2—, X is H, CH3, NH2, NH(CH3), N(CH3)2, OCH3, or SH; R2 is hydrogen or a methyl or ethyl group; R3 is hydrogen or a methyl or ehtyl group; n is 0, 1, 2, 3, 4, 5 or 6; R1 is selected from the group consisting of (a) alkyl; (b) C3 to C8 cycloalkyl; (c) phenyl or substituted phenyl; (d) heterocyclic; (e) decahydronaphthalene and (f) octahydroindane; or R1 and X may be taken together to denote a 5,6 or 6,6 saturated bicycle ring structure. 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 of therapeutic importance.
摘要翻译： 本发明主要由下列通式表示：其中A是-NHCO - ， - N（CH 3）-CO - ， - NHCH 2 - ， - N（CH 3）-CH 2 - ， - COCH 2 - ， - CH 2 CH 2 - 或-CH（OH）CH 2 - ，X是H，CH 3，NH 2，NH（CH 3），N（CH 3）2，OCH 3或SH; R 2是氢或甲基或乙基; R 3是氢或 甲基或庚基; n为0,1,2,3,4,5或6; R 1选自（a）烷基; （b）C3至C8环烷基; （c）苯基或取代的苯基; （d）杂环; （e）十氢萘和（f）八氢化茚; 或R 1和X可以一起表示5,6或6,6饱和自由基环结构。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。
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