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1. 发明授权

US06069257A Process for the production of tetrazolylbenzopyrans 失效
标题翻译：生产四唑基苯并吡喃的方法
公开(公告)号：US06069257A
公开(公告)日：2000-05-30
申请号：US341200
申请日：1999-07-06
申请人： Robert Gordon Giles , Norman John Lewis , Paul Oxley , John Kirby Quick
发明人： Robert Gordon Giles , Norman John Lewis , Paul Oxley , John Kirby Quick
IPC分类号： A61K31/351 , C07D405/04
CPC分类号： C07D405/04
摘要： A process for preparing certain substituted benzopyran compounds of formula (I) ##STR1## is disclosed.
摘要翻译： PCT No.PCT / EP97 / 07341 Sec。 371日期：1999年7月6日 102（e）1999年7月6日PCT 1997年12月30日PCT PCT。公开号WO98 / 30559 日期：1998年7月16日公开了制备式（I）的某些取代的苯并吡喃化合物的方法。

2. 发明授权

US07351832B2 Process for the preparation of thiazolidinedione derivatives 失效
标题翻译：噻唑烷二酮衍生物的制备方法
公开(公告)号：US07351832B2
公开(公告)日：2008-04-01
申请号：US11550506
申请日：2006-10-18
申请人： Robert Gordon Giles , Norman John Lewis , John Kirby Quick
发明人： Robert Gordon Giles , Norman John Lewis , John Kirby Quick
IPC分类号： C07D417/12
CPC分类号： C07D417/12
摘要： A process for preparing a compound of formula (I): or a tautomeric form thereof or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein: A1 represents a substituted or unsubstituted aromatic heterocyclyl group; R1 represents a hydrogen atom, an alkyl group, an acyl group, an aralkyl group, wherein the aryl moiety may be substituted or unsubstituted, or a substituted or unsubstituted aryl group; A2 represents a benzene ring having in total up to five substituents; and n represents an integer in the range of from 2 to 6, which process comprises catalytically reducing a compound of formula (II): wherein A1, R1, A2 and n are as defined in relation to formula (I), characterised in that the reduction reaction is carried out using a hydrogen pressure above 20 psi; and thereafter if required forming a pharmaceutically acceptable salt and/or a pharmaceutically acceptable solvate of the compound of formula (I).
摘要翻译：制备式（I）化合物或其互变异构体或其药学上可接受的盐或其药学上可接受的溶剂合物的方法，其中：A 1表示取代或未取代的芳族杂环基 ; R 1表示氢原子，烷基，酰基，芳烷基，其中芳基部分可以是取代或未取代的，或取代或未取代的芳基; 代表一个总共有五个取代基的苯环; 并且n表示2至6的整数，该方法包括催化还原式（II）的化合物：其中A 1，R 2， SUP> 2和n如关于式（I）所定义，其特征在于还原反应使用高于20psi的氢气压力进行; 然后如果需要，形成式（I）化合物的药学上可接受的盐和/或药学上可接受的溶剂化物。

3. 发明授权

US07091359B2 Process for the preparation of thiazolidinedione derivatives 失效
标题翻译：噻唑烷二酮衍生物的制备方法
公开(公告)号：US07091359B2
公开(公告)日：2006-08-15
申请号：US10288072
申请日：2002-11-04
申请人： Robert Gordon Giles , Norman John Lewis , John Kirby Quick
发明人： Robert Gordon Giles , Norman John Lewis , John Kirby Quick
IPC分类号： C07D277/04
CPC分类号： C07D417/12
摘要： A process for preparing a compound of formula (I) or a tautomeric form thereof or a pharmaceutically acceptable salt thereof, wherein: A1 represents a substituted or unsubstituted aromatic heterocyclyl group; R1 represents a hydrogen atom, an alkyl group, an acyl group, an aralkyl group, wherein the aryl moiety may be substituted or unsubstituted, or a substituted or unsubstituted aryl group; A2 represents a benzene ring having in total up to five substituents; and n represents an integer in the range of from 2 to 6, which process comprises catalytically reducing a compound of formula (II): wherein A1, R1, A2 and n are as defined in relation to formula (I), characterized in that the reduction reaction is carried out using a hydrogen pressure above 20 psi; and thereafter if required forming a pharmaceutically acceptable salt and/or a pharmaceutically acceptable solvate of the compound of formula (I).
摘要翻译：一种制备式（I）化合物或其互变异构体或其药学上可接受的盐的方法，其中：A 1表示取代或未取代的芳族杂环基; R 1表示氢原子，烷基，酰基，芳烷基，其中芳基部分可以是取代或未取代的，或取代或未取代的芳基; 代表一个总共有五个取代基的苯环; 并且n表示2至6的整数，该方法包括催化还原式（II）的化合物：其中A 1，R 2， SUP> 2和n如关于式（I）所定义，其特征在于还原反应使用高于20psi的氢气压力进行; 然后如果需要，形成式（I）化合物的药学上可接受的盐和/或药学上可接受的溶剂化物。

4. 发明授权

US06632947B2 Process for the preparation of substituted thiazolidinedione 失效
标题翻译：制备取代噻唑烷二酮的方法
公开(公告)号：US06632947B2
公开(公告)日：2003-10-14
申请号：US10005686
申请日：2001-11-08
申请人： Robert Gordon Giles , Norman John Lewis , Stephen Moore , Colin Ripley Pool , John Kirby Quick , Michael Urquhart
发明人： Robert Gordon Giles , Norman John Lewis , Stephen Moore , Colin Ripley Pool , John Kirby Quick , Michael Urquhart
IPC分类号： C07D27704
CPC分类号： C07D417/06 , C07D277/34 , C07D417/10 , C07D417/12 , C07D417/14
摘要： A process for preparing a compound of formula (I, I) or a tautomeric form thereof or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof, wherein: J represents O or S; T represents a substituted or unsubstituted aryl group and T1 is O or S; which process comprises reducing a compound of formula (II, II) or a tautomeric form thereof or a salt thereof or a solvate thereof, wherein T and T1 are as defined in relation to formula (I), with a complex hydride reducing agent or a source of a complex hydride reducing agent; and thereafter, as required, preparing a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate of the compound of formula (I) or a tautomeric form thereof.
摘要翻译：制备式（I，I）化合物或其互变异构体或其药学上可接受的盐或其药学上可接受的溶剂化物的方法，其中：J表示O或S; T表示取代或未取代的芳基，并且T为H或S; 该方法包括还原式（II，II）化合物或其互变异构形式或其盐或其溶剂合物，其中T和T 如式（I），与复合氢化物还原剂或复合氢化物还原剂的来源; 然后根据需要制备式（I）化合物或其互变异构体的药学上可接受的盐或药学上可接受的溶剂合物。

5. 发明授权

US6048983A Process for the preparation of benzopyran compounds 失效
标题翻译：苯并吡喃化合物的制备方法
公开(公告)号：US6048983A
公开(公告)日：2000-04-11
申请号：US242094
申请日：1999-02-08
申请人： Robert Gordon Giles , Paul Oxley
发明人： Robert Gordon Giles , Paul Oxley
IPC分类号： B01J31/24 , C07B61/00 , C07C231/02 , C07C231/10 , C07C233/80 , C07C235/56 , C07D405/04 , C07D257/00
CPC分类号： C07D405/04 , C07C231/10
摘要： A process for preparing certain substituted benzopyran compounds is disclosed.
摘要翻译： PCT No.PCT / EP97 / 04328 Sec。 371日期1999年2月8日 102（e）1999年2月8日PCT PCT 1997年8月5日PCT公布。第WO98 / 06718号公报日期：1998年2月19日公开了制备某些取代的苯并吡喃化合物的方法。

6. 发明授权

US06806280B1 Polymorph of 5-[4-[2-(n-methyl-n(2-pyridyl)amino)ethoxy]benzyl]-thiazolidine-2,4-dione, maleic acid salt 失效
标题翻译： 5- [4- [2-（正 - 甲基 - （（2-吡啶基）氨基）乙氧基]苄基] - 噻唑烷-2,4-二酮的马来酸盐
公开(公告)号：US06806280B1
公开(公告)日：2004-10-19
申请号：US10048123
申请日：2001-12-03
申请人： Paul David James Blackler , Christine Marie Browne , Timothy G. Coakley , Robert Gordon Giles , Gillian Morrissey
发明人： Paul David James Blackler , Christine Marie Browne , Timothy G. Coakley , Robert Gordon Giles , Gillian Morrissey
IPC分类号： A61K3144
CPC分类号： C07D417/12
摘要： A polymorphic form of 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]-thiazolidine-2, 4-dione, maleic acid salt (the “Polymorph”) characterized in that it provides: (i) an infra red spectrum containing peaks at 1763, 912, 856 and 709 cm−1; and/or (ii) a Raman spectrum containing peaks at 1762, 1284, 912 and 888 cm−1; and/or (iii) a solid-state 13C nuclear magnetic resonance spectrum containing peaks at 111.0, 113.6, 119.8, 129.1, 130.9, 131.8, 134.7, 146.5, 152.7, 157.5, 169.5, 171.0, 178.7 ppm; and/or (v) an X-ray powder diffraction (XRPD) pattern which gives calculated lattice spacings at 5.87, 5.30, 4.69, 4.09, 3.88, 3.61, 3.53 and 3.46 Angstroms; a process for preparing such a compound, a pharmaceutical composition containing such a compound and the use of such a compound in medicine.
摘要翻译： 5- [4- [2-（N-甲基-N-（2-吡啶基）氨基）乙氧基]苄基] - 噻唑烷-2,4-二酮，马来酸盐（“多晶型”）的多晶型形式，其特征在于它提供：（i）在1763,912,856和709cm -1处含有峰的红外光谱; 和/或（ii）在1762,1284,912和888cm -1处含有峰的拉曼光谱; 和/或（iii）包含111.0,113.6,119.8,129.1,130.9,131.8,134.7,146.5,152.7,157.5,169.5,171.0,178.7ppm的峰的固态13 C核磁共振光谱; 和/或（v）X射线粉末衍射（XRPD）图，其计算出的晶格间距为5.87,5.30,4.69,4.09,38.88,3.61,3.53和3.46埃; 制备这种化合物的方法，含有这种化合物的药物组合物和这种化合物在医药中的用途。

7. 发明授权

US06815457B1 Thiazolidinedione derivative and its use as antidiabetic 失效
标题翻译：噻唑烷二酮衍生物及其用作抗糖尿病药
公开(公告)号：US06815457B1
公开(公告)日：2004-11-09
申请号：US10030323
申请日：2002-05-15
申请人： Paul David James Blackler , Robert Gordon Giles , Michael Sasse
发明人： Paul David James Blackler , Robert Gordon Giles , Michael Sasse
IPC分类号： C07D41712
CPC分类号： C07D417/12
摘要： A polymorphic form of 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]-benzyl]thiazolidine-2,4-dione, maleic acid salt (the “Polymorph”) characterized in that it: (i) provides an infra red spectrum containing peaks at 1360, 1326, 1241, 714 and 669 cm−1; and/or (ii) provides a Raman spectrum containing peaks at 1581, 768, 670, 271 and 226 cm−1; and/or (iii) provides a solid-state nuclear magnetic resonance spectrum containing peaks at chemical shifts substantially as set out in Table I; and/or (iv) provides an X-ray powder diffraction (XRPD) pattern containing peaks substantially as set out in Table II; a process for preparing such a compound, a pharmaceutical composition containing such a compound and the use of such a compound in medicine.

8. 发明授权

US07358366B2 Thiazolidinedione derivative and its use as antidiabetic 失效
标题翻译：噻唑烷二酮衍生物及其用作抗糖尿病药
公开(公告)号：US07358366B2
公开(公告)日：2008-04-15
申请号：US11458471
申请日：2006-07-19
申请人： Paul David James Blackler , Robert Gordon Giles , Stephen Moore , Michael John Sasse
发明人： Paul David James Blackler , Robert Gordon Giles , Stephen Moore , Michael John Sasse
IPC分类号： C07D417/12
CPC分类号： C07D417/12
摘要： A polymorphic form of 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione, maleic acid salt (the “Polymorph”) characterised in that it provides: (i) an infra red spectrum containing peaks at 1752, 1546, 1154, 621, and 602 cm−1; and/or (ii) a Raman spectrum containing peaks at 1751, 1243 and 602 cm−1; and/or (iii) a solid-state nuclear magnetic resonance spectrum containing peaks at 111.9, 114.8, 119.6, 129.2, 134.0, 138.0, 144.7, 153.2, 157.1, 170.7, 172.0, and 175.0 ppm; and/or (iv) an X-ray powder diffraction (XRPD) pattern which gives calculated lattice spacings of 6.46, 5.39, 4.83, 4.68, 3.71, 3.63, 3.58, and 3.48 Angstroms; a process for preparing such a compound, a pharmaceutical composition containing such a compound and the use of such a compound in medicine.
摘要翻译： 5- [4- [2-（N-甲基-N-（2-吡啶基）氨基）乙氧基]苄基]噻唑烷-2,4-二酮，马来酸盐（“多晶型”）的多晶形式，其特征在于它提供：（i）在1752,1546,1154,621和602cm -1处含有峰的红外光谱; 和/或（ii）在1751,1243和602cm -1处含有峰的拉曼光谱; 和/或（iii）在111.9,114.8,119.6,129.2,134.0,138.0,144.7,153.2,157.1,170.7,172.0和175.0ppm处含有峰的固态核磁共振光谱; 和/或（iv）X射线粉末衍射（XRPD）图案，其给出计算的晶格间距为6.46,5.39,4.83,4.68,3.73,3.63,3.58和3.48埃; 制备这种化合物的方法，含有这种化合物的药物组合物和这种化合物在医药中的用途。

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