专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

US20070270463A1 NOVEL PRODUCT, METHOD AND INTERMEDIATES FOR THE PREPARATION OF AZETIDINE DERIVATIVES 失效
标题翻译：用于制备AZETIDINE衍生物的新产品，方法和中间体
公开(公告)号：US20070270463A1
公开(公告)日：2007-11-22
申请号：US11689588
申请日：2007-03-22
申请人： Stephane Mutti , Michel Lavigne , Luc Grondard , Joel Malpart , Joerg Rieke-Zapp , Veronique Crocq-Stuerga
发明人： Stephane Mutti , Michel Lavigne , Luc Grondard , Joel Malpart , Joerg Rieke-Zapp , Veronique Crocq-Stuerga
IPC分类号： A61K31/47 , A61P25/14 , A61P25/28 , A61P3/04 , C07D215/38
CPC分类号： C07D205/04 , C07D401/12
摘要： The present invention relates to a novel method for the preparation of azetidine derivatives such as N-{1-[bis(4-chlorophenyl)methyl]azetidin-3-yl}-N-quinol-6-ylmethylsulfonamide and the dihydrochloride thereof and N-{1-[bis(4-chlorophenyl)methyl]azetidin-3-yl}-N-(3,5-difluorophenyl)methylsulfonamide.
摘要翻译：本发明涉及一种制备氮杂环丁烷衍生物如N- {1- [双（4-氯苯基）甲基]氮杂环丁烷-3-基} -N-喹啉-6-基甲基磺酰胺及其二盐酸盐和N - {1- [双（4-氯苯基）甲基]氮杂环丁烷-3-基} -N-（3,5-二氟苯基）甲基磺酰胺。

2. 发明授权

US07687493B2 Product, method and intermediates for the preparation of azetidine derivatives 失效
标题翻译：用于制备氮杂环丁烷衍生物的产品，方法和中间体
公开(公告)号：US07687493B2
公开(公告)日：2010-03-30
申请号：US11689588
申请日：2007-03-22
申请人： Stephane Mutti , Michel Lavigne , Luc Grondard , Joel Malpart , Joerg Rieke-Zapp , Veronique Crocq-Stuerga
发明人： Stephane Mutti , Michel Lavigne , Luc Grondard , Joel Malpart , Joerg Rieke-Zapp , Veronique Crocq-Stuerga
IPC分类号： A61K31/00
CPC分类号： C07D205/04 , C07D401/12
摘要： The present invention relates to a novel method for the preparation of azetidine derivatives such as N-{1-[bis(4-chlorophenyl)methyl]azetidin-3-yl}-N-quinol-6-ylmethylsulfonamide and the dihydrochloride thereof and N-{1-[bis(4-chlorophenyl)methyl]azetidin-3-yl}-N-(3,5-difluorophenyl)methylsulfonamide.
摘要翻译：本发明涉及一种制备氮杂环丁烷衍生物如N- {1- [双（4-氯苯基）甲基]氮杂环丁烷-3-基} -N-喹啉-6-基甲基磺酰胺及其二盐酸盐和N - {1- [双（4-氯苯基）甲基]氮杂环丁烷-3-基} -N-（3,5-二氟苯基）甲基磺酰胺。

3. 发明授权

US07179909B2 Process for the manufacture of a product of the thiazolo [3,4,5-de] [4,1]benzothiazepine type 失效
标题翻译：制备噻唑并[3,4,5-de] [4,1]苯并硫氮杂类产物的方法
公开(公告)号：US07179909B2
公开(公告)日：2007-02-20
申请号：US11005224
申请日：2004-12-06
申请人： Stephane Mutti , Joel Malpart , Michel Lavigne , Michel Cheve
发明人： Stephane Mutti , Joel Malpart , Michel Lavigne , Michel Cheve
IPC分类号： C07D513/06
CPC分类号： C07C271/28
摘要： Novel processes for the preparation of a compound of the thiazolo[3,4,5-de] [4,1]benzothiazepine type and in particular of 2-imino-9-trifluoromethyl-4,5-dihydro-2H,7H-thiazolo[3,4,5-de] [4,1]benzothiazepine 6,6-dioxide methanesulfonate and (R,S)-2-imino-9-trifluoromethyl-4,5-dihydro-2H,7H-thiazolo[3,4,5-de] [4,1]benzothiazepine 6-oxide and its enantiomers and their pharmaceutically acceptable salts.
摘要翻译：制备噻唑并[3,4,5-de] [4,1]苯并硫氮杂类化合物，特别是2-亚氨基-9-三氟甲基-4,5-二氢-2H- 7H-噻唑的化合物的新方法 [3,4,5-de] [4,1]苯并硫氮杂六甲醚甲磺酸盐和（R，S）-2-亚氨基-9-三氟甲基-4,5-二氢-2H- 7H-噻唑并[ 4,5-de] [4,1]苯并硫氮杂_6-氧化物及其对映体及其药学上可接受的盐。

4. 发明申请

US20050165002A1 Process for the manufacture of a product of the thiazolo [3,4,5-de] [4,1]benzothiazepine type 失效
标题翻译：制备噻唑并[3,4,5-de] [4,1]苯并硫氮杂类产物的方法
公开(公告)号：US20050165002A1
公开(公告)日：2005-07-28
申请号：US11005224
申请日：2004-12-06
申请人： Stephane Mutti , Joel Malpart , Michel Lavigne , Michel Cheve
发明人： Stephane Mutti , Joel Malpart , Michel Lavigne , Michel Cheve
IPC分类号： C07C271/28 , A61K31/554 , C07D498/04
CPC分类号： C07C271/28
摘要： Novel processes for the preparation of a compound of the thiazolo[3,4,5-de][4,1]benzothiazepine type and in particular of 2-imino-9-trifluoromethyl-4,5-dihydro-2H,7H-thiazolo[3,4,5-de][4,1]benzothiazepine 6,6-dioxide methanesulfonate and (R,S)-2-imino-9-trifluoromethyl-4,5-dihydro-2H,7H-thiazolo[3,4,5-de][4,1]benzothiazepine 6-oxide and its enantiomers and their pharmaceutically acceptable salts.
摘要翻译：制备噻唑并[3,4,5-de] [4,1]苯并硫氮杂类化合物，特别是2-亚氨基-9-三氟甲基-4,5-二氢-2H- 7H-噻唑的化合物的新方法 [3,4,5-de] [4,1]苯并硫氮杂六甲醚甲磺酸盐和（R，S）-2-亚氨基-9-三氟甲基-4,5-二氢-2H- 7H-噻唑并[ 4,5-de] [4,1]苯并硫氮杂_6-氧化物及其对映体及其药学上可接受的盐。

5. 发明授权

US06384272B2 Method for preparing aspartylcyclohexyla laninamide 有权
标题翻译：天冬氨酰环己基氨基磺酰胺的制备方法
公开(公告)号：US06384272B2
公开(公告)日：2002-05-07
申请号：US09729011
申请日：2000-12-04
申请人： Robert Stammler , Christophe Daubie , Michel Lavigne
发明人： Robert Stammler , Christophe Daubie , Michel Lavigne
IPC分类号： C07C22900
CPC分类号： C07K5/06113
摘要： Disclosure is a method for preparing &agr;-aspartyl-&bgr;-cyclohexylalaninamide, comprising carrying out a first step of amide formation of an &agr;-aspartyl phenylamine ester of general formula (II) wherein: R is a C1-C4 alkyl radical, and then performing a catalytic hydrogenation of the resulting &agr;-aspartyl phenylalaninamide ammonium salt, optionally released previously from its salt, and optionally transforming it into an addition acis salt.
摘要翻译：公开是制备α-天冬氨酰基-β-环己基丙氨酰胺的方法，包括进行通式（II）的α-天冬氨酰苯基胺酰胺形成的第一步骤，其中：R是C1-C4烷基，然后进行所得α-天冬氨酰苯丙氨酰胺铵盐的催化氢化，任选先前从其盐中释放，并任选地将其转化成加成盐。

6. 发明授权

US06759555B2 Process for the preparation of combretastatins 失效
标题翻译：制备考布他汀的方法
公开(公告)号：US06759555B2
公开(公告)日：2004-07-06
申请号：US10410547
申请日：2003-04-09
申请人： Stéphane Mutti , Michel Lavigne , Irina Malejonock , Jean-Paul Casimir
发明人： Stéphane Mutti , Michel Lavigne , Irina Malejonock , Jean-Paul Casimir
IPC分类号： A61K31135
CPC分类号： C07C213/02 , C07C217/84 , C07C237/08 , Y02P20/55
摘要： The present invention provides novel processes for the preparation of combretastatins or stilbene compounds of formulae (I) and (III) wherein A is NH2 or and PG is a protecting group. The disclosed and claimed processes include (1) Wittig condensation between a nitromethoxybenzaldehyde and a trimethoxybenzylphosphonium salt or between a trimethoxybenzaldehyde and a nitromethoxybenzylphosphonium salt to provide an intermediate compound of formula (I) wherein A is NO2, and subsequent iron powder reduction to provide a compound of formula (I) wherein A is NH2; (2) Wittig condensation of the same precursor aldehydes and phosphonium salts wherein NO2 is replaced by NH2 to provide a compound of formula (I) wherein A is NH2; and (3) a process for condensation of a compound of formula (I) wherein A is NH2 with a doubly protected serinamide to provide an intermediate of formula (III), and subsequent hydrolysis to provide a compound of formula (I) wherein A is —NH—C(═O)CH(NH2)CH2OH, or the pharmaceutically acceptable salts thereof. Also claimed is a compound of formula (III).
摘要翻译：本发明提供了制备式（I）和（III）的考布他汀或芪化合物的新方法，其中A是NH 2，PG是保护基。公开和要求保护的方法包括（1）硝基甲氧基苯甲醛和三甲氧基苄基鏻盐或三甲氧基苯甲醛和硝基甲氧基苄基鏻盐之间，以提供其中A为NO 2的式（I）的中间体化合物，随后的铁粉还原以提供其中A为NH 2的式（I）化合物; （2）相同的前体醛和鏻盐的Wittig缩合，其中NO 2被NH 2代替，得到其中A是NH 2的式（I）化合物; （3）将式（I）化合物（其中A是NH 2）与双重保护的丝氨酰胺缩合以提供式（III）的中间体，随后水解以提供式（I）化合物的方法，其中A为 -NH-C（= O）CH（NH 2）CH 2 OH，或其药学上可接受的盐。还要求的是式（III）的化合物。

7. 发明授权

US6150541A 4,10-.beta.-diacetoxy- 2.alpha.-benzoyloxy-5.beta.,20-epoxy-1-hydroxy-9-oxo-19-norcyclopropa[g]t ax-11-en-13.alpha.-yl (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate dihydrate and its process of preparation 失效
标题翻译： 4,10-β-二乙酰氧基-2α-苯甲酰氧基-5β，20-环氧-1-羟基-9-氧代-19-降胆固醇[g] tax-11-en-13α-基（2R，3S） - 3-叔丁氧基羰基氨基-2-羟基-3-苯基丙酸酯二水合物及其制备方法
公开(公告)号：US6150541A
公开(公告)日：2000-11-21
申请号：US367387
申请日：1998-06-10
申请人： Eric Didier , Michel Lavigne , Jean-Rene Authelin
发明人： Eric Didier , Michel Lavigne , Jean-Rene Authelin
IPC分类号： C07D305/14
CPC分类号： C07D305/14
摘要： The present invention is directed to 4,10.beta.-diacetoxy-2.alpha.-benzoyloxy-5.beta.,20-epoxy-1-hydroxy-9-oxo-19-norcyclopropa(g)tax-11-en-13.alpha.-yl (2r,3s)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate dihydrate and a process for its preparation.
摘要翻译：本发明涉及4,10β-二乙酰氧基-2α-苯甲酰氧基-5β，20-环氧-1-羟基-9-氧代-19-降胆固醇（g）tax-11-en-13α-基（ 2r，3s）-3-叔丁氧基羰基氨基-2-羟基-3-苯基丙酸酯二水合物及其制备方法。

8. 发明授权

US06180759B2 Process for the preparation of azacycloalkylakanoyl pseudotetrapeptides 失效
标题翻译：制备氮杂环烷基烷酰基假四肽的方法
公开(公告)号：US06180759B2
公开(公告)日：2001-01-30
申请号：US09544680
申请日：2000-04-07
申请人： James J. Mencel , Robert Stammler , Christophe Daubie , Michel Lavigne , Benoit J. Vanasse , Robert C. Liu , Patrick Leon , Geoffrey A. D'Netto , Adam W. Sledeski
发明人： James J. Mencel , Robert Stammler , Christophe Daubie , Michel Lavigne , Benoit J. Vanasse , Robert C. Liu , Patrick Leon , Geoffrey A. D'Netto , Adam W. Sledeski
IPC分类号： C07C22718
CPC分类号： C07D211/34 , C07K5/021 , C07K5/06113 , Y02P20/55
摘要： This invention is directed to a process for preparing a pseudotetrapeptide of formula I or a salt or prodrug thereof wherein is optionally nitrogen protected azaheterocyclyl; is a single or double bond; q is 1-5; B is alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, aralkyl, alkylaryl, or alkylaralkyl; Q2 is H or a carboxylic acid protecting group; J is —H, alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, substituted aryl, aralkyl, substituted aralkyl; L is OR1, or NR1R2, where R1 and R2 are independently —H, alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, aralkyl, alkylaryl or alkylaralkyl; and p is 1 or 2 which comprises the coupling of two dipeptides or psuedopeptides.
摘要翻译：本发明涉及制备式I的假四肽或其盐或前药的方法，其中任选地氮保护氮杂环基;是单键或双键; q为1-5; B是烷基，环烷基，环烷基烷基，烷基环烷基，烷基环烷基烷基，芳基，芳烷基，烷基芳基或烷基烷基; Q2是H或羧酸保护基; J是-H，烷基，环烷基，环烷基烷基，烷基环烷基，烷基环烷基烷基，芳基，取代的芳基，芳烷基，取代的芳烷基; L是OR 1或NR 1 R 2，其中R 1和R 2独立地是-H，烷基，环烷基，环烷基烷基，烷基环烷基，烷基环烷基烷基，芳基，芳烷基，烷基芳基或烷基烷基; 并且p是1或2，其包括两个二肽或伪多肽的偶联。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式