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1. 发明授权

US08309720B2 Process for the preparation of substituted pyrimidine derivatives 有权
标题翻译：制备取代嘧啶衍生物的方法
公开(公告)号：US08309720B2
公开(公告)日：2012-11-13
申请号：US12459229
申请日：2009-06-29
申请人： Sergio Cesco-Cancian , Hongfeng Chen , Jeffrey S. Grimm , Neelakandha S. Mani , Christopher M. Mapes , David C. Palmer , Daniel J. Pippel , Kirk L. Sorgi , Tong Xiao
发明人： Sergio Cesco-Cancian , Hongfeng Chen , Jeffrey S. Grimm , Neelakandha S. Mani , Christopher M. Mapes , David C. Palmer , Daniel J. Pippel , Kirk L. Sorgi , Tong Xiao
IPC分类号： C07D211/06 , C07D211/30
CPC分类号： C07D401/12 , C07C211/22 , C07C211/26 , C07D211/22 , C07D211/26
摘要： The present invention is directed to processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine H4 receptor modulators, and to intermediates in H4 modulator synthesis.
摘要翻译：本发明涉及制备用作合成组胺H 4受体调节剂的中间体的取代嘧啶衍生物的方法，以及H4调节剂合成中的中间体。

2. 发明申请

US20100004450A1 Process for the preparation of substituted pyrimidine derivatives 有权
标题翻译：制备取代嘧啶衍生物的方法
公开(公告)号：US20100004450A1
公开(公告)日：2010-01-07
申请号：US12459229
申请日：2009-06-29
申请人： Sergio Cesco-Cancian , Hongfeng Chen , Jeffrey S. Grimm , Neelakandha S. Mani , Christopher M. Mapes , David C. Palmer , Daniel J. Pippel , Kirk L. Sorgi , Tong Xiao
发明人： Sergio Cesco-Cancian , Hongfeng Chen , Jeffrey S. Grimm , Neelakandha S. Mani , Christopher M. Mapes , David C. Palmer , Daniel J. Pippel , Kirk L. Sorgi , Tong Xiao
IPC分类号： C07D401/12 , C07D211/22 , C07D211/26
CPC分类号： C07D401/12 , C07C211/22 , C07C211/26 , C07D211/22 , C07D211/26
摘要： The present invention is directed to processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine H4 receptor modulators, and to intermediates in H4 modulator synthesis.
摘要翻译：本发明涉及制备用作合成组胺H 4受体调节剂的中间体的取代嘧啶衍生物的方法，以及H4调节剂合成中的中间体。

3. 发明授权

US08168829B2 Synthesis of quaternary salt compounds 有权
标题翻译：季盐化合物的合成
公开(公告)号：US08168829B2
公开(公告)日：2012-05-01
申请号：US12256114
申请日：2008-10-22
申请人： David C. Palmer , Sergio Casco-Cancian , Tong Xiao , Kirk L. Sorgi , Armin Roessler , Anita Vladislavic , Roger Faessler
发明人： David C. Palmer , Sergio Casco-Cancian , Tong Xiao , Kirk L. Sorgi , Armin Roessler , Anita Vladislavic , Roger Faessler
IPC分类号： C07C211/00
CPC分类号： C07D333/36 , C07D209/42 , C07D295/135 , C07D307/14 , C07D307/68 , C07D307/85 , C07D309/04 , C07D309/14 , C07D311/58 , C07D311/92 , C07D313/08 , C07D333/70 , C07D335/02 , C07D405/12 , C07D407/12 , C07D409/12
摘要： The present invention is directed to a process, having a reduced environmental impact, for preparing phenylamino substituted quaternary salt compounds that are CCR2 antagonists.
摘要翻译：本发明涉及一种降低环境影响的方法，用于制备作为CCR2拮抗剂的苯基氨基取代的季盐化合物。

4. 发明申请

US20080171870A1 PROCESS FOR THE PREPARATION OF PIPERAZINYL AND DIAZEPANYL BENZAMIDE DERIVATIVES 有权
标题翻译：制备哌嗪和二氮茚衍生物衍生物的方法
公开(公告)号：US20080171870A1
公开(公告)日：2008-07-17
申请号：US11953262
申请日：2007-12-10
申请人： Anusuya Choudhury , Jeffrey S. Grimm , Kirk L. Sorgi , David Palmer , Jing Liu
发明人： Anusuya Choudhury , Jeffrey S. Grimm , Kirk L. Sorgi , David Palmer , Jing Liu
IPC分类号： C07D413/00 , C07D295/00
CPC分类号： C07D413/10 , C07D241/04 , C07D401/10 , C07D403/10 , Y02P20/55
摘要： The present invention is directed to a novel process for the preparation of piperazinyl and diazepanyl benzamide derivatives, useful for the treatment of disorders and conditions mediated by a histamine receptor, preferably the H3 receptor.
摘要翻译：本发明涉及用于制备哌嗪基和二氮杂环庚烷基苯甲酰胺衍生物的新方法，其可用于治疗由组胺受体介导的病症和病症，优选H3受体。

5. 发明授权

US07893257B2 Process for the preparation of piperazinyl and diazepanyl benzamide derivatives 有权
标题翻译：制备哌嗪基和二氮杂环庚烷基苯甲酰胺衍生物的方法
公开(公告)号：US07893257B2
公开(公告)日：2011-02-22
申请号：US11953262
申请日：2007-12-10
申请人： Anusuya Choudhury , Jeffrey S. Grimm , Kirk L. Sorgi , David Palmer , Jing Liu
发明人： Anusuya Choudhury , Jeffrey S. Grimm , Kirk L. Sorgi , David Palmer , Jing Liu
IPC分类号： C07D413/10
CPC分类号： C07D413/10 , C07D241/04 , C07D401/10 , C07D403/10 , Y02P20/55
摘要： The present invention is directed to a novel process for the preparation of piperazinyl and diazepanyl benzamide derivatives, useful for the treatment of disorders and conditions mediated by a histamine receptor, preferably the H3 receptor.
摘要翻译：本发明涉及用于制备哌嗪基和二氮杂环庚烷基苯甲酰胺衍生物的新方法，其可用于治疗由组胺受体介导的病症和病症，优选H3受体。

6. 发明授权

US08680273B2 Process for the preparation of piperazinyl and diazepanyl benzamide derivatives 有权
标题翻译：制备哌嗪基和二氮杂环庚烷基苯甲酰胺衍生物的方法
公开(公告)号：US08680273B2
公开(公告)日：2014-03-25
申请号：US12987370
申请日：2011-01-10
申请人： Anusuya Choudhury , Jeffrey S. Grimm , Kirk L. Sorgi , David Palmer , Jing Liu
发明人： Anusuya Choudhury , Jeffrey S. Grimm , Kirk L. Sorgi , David Palmer , Jing Liu
IPC分类号： C07D241/04
CPC分类号： C07D413/10 , C07D241/04 , C07D401/10 , C07D403/10 , Y02P20/55
摘要： The present invention is directed to a novel process for the preparation of piperazinyl and diazepanyl benzamide derivatives, useful for the treatment of disorders and conditions mediated by a histamine receptor, preferably the H3 receptor.
摘要翻译：本发明涉及用于制备哌嗪基和二氮杂环庚烷基苯甲酰胺衍生物的新方法，其可用于治疗由组胺受体介导的病症和病症，优选H3受体。

7. 发明申请

US20110105752A1 PROCESS FOR THE PREPARATION OF PIPERAZINYL AND DIAZEPANYL BENZAMIDE DERIVATIVES 有权
标题翻译：制备哌嗪和二氮茚衍生物衍生物的方法
公开(公告)号：US20110105752A1
公开(公告)日：2011-05-05
申请号：US12987370
申请日：2011-01-10
申请人： Anusuya Choudhury , Jeffrey S. Grimm , Kirk L. Sorgi , David Palmer , Jing Liu
发明人： Anusuya Choudhury , Jeffrey S. Grimm , Kirk L. Sorgi , David Palmer , Jing Liu
IPC分类号： C07D241/04
CPC分类号： C07D413/10 , C07D241/04 , C07D401/10 , C07D403/10 , Y02P20/55
摘要： The present invention is directed to a novel process for the preparation of piperazinyl and diazepanyl benzamide derivatives, useful for the treatment of disorders and conditions mediated by a histamine receptor, preferably the H3 receptor.
摘要翻译：本发明涉及用于制备哌嗪基和二氮杂环庚烷基苯甲酰胺衍生物的新方法，其可用于治疗由组胺受体介导的病症和病症，优选H3受体。

8. 发明授权

US08278446B2 Process for preparing substituted diaminopyrimidine oximes 有权
标题翻译：制备取代的二氨基嘧啶肟的方法
公开(公告)号：US08278446B2
公开(公告)日：2012-10-02
申请号：US11766257
申请日：2007-06-21
申请人： Hongfeng Chen , Peter J. Connolly , Kirk L. Sorgi , Anusuya Choudhury , Christopher N. Nilsen
发明人： Hongfeng Chen , Peter J. Connolly , Kirk L. Sorgi , Anusuya Choudhury , Christopher N. Nilsen
IPC分类号： C07D239/48 , C07D239/50 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14
CPC分类号： C07D239/48 , C07D401/12 , C07D403/12 , C07D407/12 , C07D413/04 , C07D417/12
摘要： The present invention is directed to a process for chemoselective substitution on a halopyrimidine carboxaldehyde having multiple reactive sites and subsequent stereoselective oxime formation.
摘要翻译：本发明涉及一种在具有多个反应位点和随后的立体选择性肟形成的卤代嘧啶甲醛上进行化学选择性取代的方法。

9. 发明授权

US5977302A Liquid phase process for the preparation of GnRH peptides 有权
标题翻译：用于制备GnRH肽的液相方法
公开(公告)号：US5977302A
公开(公告)日：1999-11-02
申请号：US195049
申请日：1998-11-18
申请人： David C. Palmer , Ahmed Abdel-Magid , Michael S. Breslav , Urs P. Eggmann , Bruce Harris , Mark L. Haslego , Kirk L. Sorgi
发明人： David C. Palmer , Ahmed Abdel-Magid , Michael S. Breslav , Urs P. Eggmann , Bruce Harris , Mark L. Haslego , Kirk L. Sorgi
IPC分类号： C07K5/09 , C07K5/103 , C07K5/107 , C07K7/23 , C07K7/06
CPC分类号： C07K5/0815 , C07K5/101 , C07K5/1013 , C07K5/1016 , C07K7/23 , Y02P20/55
摘要： A liquid phase process for preparing GnRH peptide analogs of the formula:G-AA.sub.1 -(A)D-Phe-AA.sub.3 -AA.sub.4 -(R.sub.2)-AA.sub.5 -AA.sub.6 AA.sub.7 -AA.sub.8 -Pro-AA.sub.10 -NH.sub.2Formula 1which comprises:(a) reacting a peptide of the formula:T-(R.sub.2)AA.sub.5 -AA.sub.6 -Xwhere T is (P.sub.2)AA4 orP.sub.2 and X is AA.sub.7 --OH or is --OH, with a peptide of the formula:X'-AA.sub.8 -Pro-AA.sub.10 -NH.sub.2or acid-addition salt form thereof, where X' is AA.sub.7 when X is absent and X' selected from P-Ala, Gly, GABA, the D- and L- isomers of Ala, amino isobutyric acid, 6-amino-hexanoic acid, Ser, Thr, His, Tyr, Asn, and Gln' is absent when X is AA.sub.7 --OH;in a liquid reaction medium in the presence of a peptide coupling reagent and a strong organic amine base to obtain a product of the formula:T-(R.sub.2)AA.sub.5 -AA.sub.6 -AA.sub.7 -AA.sub.8 -Pro-AA.sub.10 -NH.sub.2(b) removing the P.sub.2 protecting group at the N-terminus, and(c) reacting the product of step (b) or an acid addition salt thereof, with a peptide of the formula:G-AA.sub.1 -(R.sub.1)D-Phe-AA.sub.3 -T'or acid-addition salt form thereof, where T' is AA.sub.4 --OH when T is absent and is absent when T is P2-AA.sub.4, in a liquid reaction medium to obtain a GnRH peptide of the formula:G-AA.sub.1 -(A)D-Phe-AA.sub.3 -AA.sub.4 -(R.sub.2)AA.sub.5 -AA.sub.6 -AA.sub.7 -AA.sub.8 -Pro-AA.sub.10 -NH.sub.2.
摘要翻译：用于制备下式的GnRH肽类似物的液相方法：G-AA1-（A）D-Phe-AA3-AA4-（R2）-AA5-AA6AA7-AA8-Pro-AA10-NH2式1，其包含：（a ）使下式的肽与下式的肽反应：其中T是（P2）AA4或P2，X是AA7-OH或-OH的式（T-（R2）AA5-AA6-X）肽与下式的肽反应：X'-AA8-Pro -AA10-NH2或其酸加成盐形式，其中当X不存在时X'为AA 7，X'选自P-Ala，Gly，GABA，Ala的D-和L-异构体，氨基异丁酸，当X是AA7-OH时，氨基己酸，Ser，Thr，His，Tyr，Asn和Gln'不存在; 在液体反应介质中，在肽偶联剂和强有机胺碱的存在下，得到下式的产物：（（R 2）AA 5 -A AA 6 -A AA 7 -A AA 8 -Pro-AA 10 -NH 2（b） P2保护基团，和（c）使步骤（b）的产物或其酸加成盐与下式的肽反应：G-AA1-（R1）D-Phe-AA3-T' 或其酸加成盐形式，其中当T不存在时T'为AA4-OH，当T为P2-AA4时不存在，在液体反应介质中得到G-AA1 - （A）的GnRH肽， D-Phe-AA3-AA4-（R2）AA5-AA6-AA7-AA8-Pro-AA10-NH2。

10. 发明授权

US06235876B1 Liquid phase process for the preparation of GNRH peptides 有权
标题翻译：用于制备GNRH肽的液相方法
公开(公告)号：US06235876B1
公开(公告)日：2001-05-22
申请号：US09350231
申请日：1999-07-08
申请人： David C. Palmer , Ahmed Abdel-Magid , Urs P. Eggmann , Bruce Harris , Kirk L. Sorgi
发明人： David C. Palmer , Ahmed Abdel-Magid , Urs P. Eggmann , Bruce Harris , Kirk L. Sorgi
IPC分类号： C07K704
CPC分类号： C07K5/0815 , C07K5/101 , C07K5/1013 , C07K5/1016 , C07K7/23 , Y02P20/55
摘要： A liquid phase process for preparing GnRH peptide analogs of the formula: G-AA1-(A)D-Phe-AA3-AA4-(R2-AA5-AA6-AA7-AA8-Pro-AA10-NH2 Formula 1 which comprises: (a) reacting a peptide of the formula: T-(R2)AA5-AA6-X where T is (P2) AA4 orP2 and X is AA7-OH or is —OH, with a peptide of the formula: X′-AA8-Pro-AA10-NH2 or acid-addition salt form thereof, where X′ is AA7 when X is absent and X′ is absent when X is AA7-OH; in a liquid reaction medium in the presence of a peptide coupling reagent and a strong organic amine base to obtain a product of the formula: T-(R2)AA5-AA6-AA7-AA8-Pro-AA10-NH2 (b) removing the P2 protecting group at the N-terminus, and (c) reacting the product of step (b) or an acid addition salt thereof, with a peptide of the formula: G-AA1-(R1)D-Phe-AA3-T′ or acid-addition salt form thereof, where T′ is AA4-OH when T is absent and is absent when T is P2-AA4, in a liquid reaction medium to obtain a GnRH peptide of the formula: G-AA1-(A)D-Phe-AA3-AA4-(R2)AA5-AA6-AA7-AA8-Pro-AA10-NH2.
摘要翻译：用于制备下式的GnRH肽类似物的液相方法：其包括：（a）使下式的肽与其中T是（P2）AA4或P2，X是AA7-OH或-OH的肽反应，式：或其酸加成盐形式，其中当X不存在时X'为AA 7，X为AA 7 -OH时X'不存在; 在液体反应介质中，在肽偶联剂和强有机胺碱存在下，得到下式的产物：（b）在N末端除去P2保护基，和（c）使步骤（b）或其酸加成盐与下式的肽或其酸加成盐形式，当T不存在时T'为AA4-OH，当T为P2-AA4时不存在，在液体反应中培养基以获得下式的GnRH肽：

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