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1. 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。

2. 发明申请

US20090112004A1 SYNTHESIS OF QUATERNARY SALT COMPOUNDS 有权
标题翻译：季铵化合物的合成
公开(公告)号：US20090112004A1
公开(公告)日：2009-04-30
申请号：US12256114
申请日：2008-10-22
申请人： David C. Palmer , Sergio Casco-Cancian , Tong Xiao , Kirl L. Sorgi , Armin Roessler , Anita Vladislavic , Roger Faessler
发明人： David C. Palmer , Sergio Casco-Cancian , Tong Xiao , Kirl L. Sorgi , Armin Roessler , Anita Vladislavic , Roger Faessler
IPC分类号： C07D309/12 , C07C235/56 , C07C233/66
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。

3. 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。

4. 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。

5. 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。

6. 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：

7. 发明申请

US20120283433A1 NOVEL PROCESSES FOR THE PREPARATION OF CYCLOPROPYL-AMIDE DERIVATIVES 审中-公开
标题翻译：制备环丙基酰胺衍生物的新方法
公开(公告)号：US20120283433A1
公开(公告)日：2012-11-08
申请号：US13542821
申请日：2012-07-06
申请人： Neelakandha S. Mani , David C. Palmer , Chennagiri R. Pandit , Mayra B. Reyes , Tong Xiao , Sergio Cesco-Cancian
发明人： Neelakandha S. Mani , David C. Palmer , Chennagiri R. Pandit , Mayra B. Reyes , Tong Xiao , Sergio Cesco-Cancian
IPC分类号： C07D413/10
CPC分类号： C07D295/192
摘要： The present invention is directed to novel processes for the preparation of cyclopropyl-amide derivatives, useful for the treatment of disorders and conditions mediated by the histamine receptor.
摘要翻译：本发明涉及用于制备环丙基 - 酰胺衍生物的新方法，其用于治疗由组胺受体介导的病症和病症。

8. 发明申请

US20120029191A1 NOVEL PROCESSES FOR THE PREPARATION OF CYCLOPROPYL-AMIDE DERIVATIVES 审中-公开
公开(公告)号：US20120029191A1
公开(公告)日：2012-02-02
申请号：US13270924
申请日：2011-10-11
申请人： Neelakandha S. Mani , David C. Palmer , Chennagiri R. Pandit , Mayra B. Reyes , Tong Xiao , Sergio Cesco-Cancian
发明人： Neelakandha S. Mani , David C. Palmer , Chennagiri R. Pandit , Mayra B. Reyes , Tong Xiao , Sergio Cesco-Cancian
IPC分类号： C07D413/10
CPC分类号： C07D295/192
摘要： The present invention is directed to novel processes for the preparation of cyclopropyl-amide derivatives, useful for the treatment of disorders and conditions mediated by the histamine receptor.

9. 发明授权

US08063206B2 Processes for the preparation of cyclopropyl-amide derivatives 有权
标题翻译：制备环丙基 - 酰胺衍生物的方法
公开(公告)号：US08063206B2
公开(公告)日：2011-11-22
申请号：US12840134
申请日：2010-07-20
申请人： Neelakandha S. Mani , David C. Palmer , Chennagiri R. Pandit , Mayra B. Reyes , Tong Xiao , Sergio Cesco-Cancian
发明人： Neelakandha S. Mani , David C. Palmer , Chennagiri R. Pandit , Mayra B. Reyes , Tong Xiao , Sergio Cesco-Cancian
IPC分类号： C07D413/10
CPC分类号： C07D295/192
摘要： The present invention is directed to novel processes for the preparation of cyclopropyl-amide derivatives, useful for the treatment of disorders and conditions mediated by the histamine receptor.
摘要翻译：本发明涉及用于制备环丙基 - 酰胺衍生物的新方法，其用于治疗由组胺受体介导的病症和病症。

10. 发明申请

US20100286391A1 NOVEL PROCESSES FOR THE PREPARATION OF CYCLOPROPYL-AMIDE DERIVATIVES 有权
标题翻译：制备环丙基酰胺衍生物的新方法
公开(公告)号：US20100286391A1
公开(公告)日：2010-11-11
申请号：US12840134
申请日：2010-07-20
申请人： Neelakandha S. Mani , David C. Palmer , Chennagiri R. Pandit , Mayra B. Reyes , Tong Xiao , Sergio Cesco-Cancian
发明人： Neelakandha S. Mani , David C. Palmer , Chennagiri R. Pandit , Mayra B. Reyes , Tong Xiao , Sergio Cesco-Cancian
IPC分类号： C07D413/10 , C07D401/10
CPC分类号： C07D295/192
摘要： The present invention is directed to novel processes for the preparation of cyclopropyl-amide derivatives, useful for the treatment of disorders and conditions mediated by the histamine receptor.
摘要翻译：本发明涉及用于制备环丙基 - 酰胺衍生物的新方法，其用于治疗由组胺受体介导的病症和病症。

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