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1. 发明授权

US5478851A Dioxothiazolidine compounds 失效
标题翻译：二恶唑烷化合物
公开(公告)号：US5478851A
公开(公告)日：1995-12-26
申请号：US50175
申请日：1993-04-30
申请人： Barrie C. C. Cantello , David Haigh , Richard M. Hindley
发明人： Barrie C. C. Cantello , David Haigh , Richard M. Hindley
IPC分类号： A61K31/425 , A61K31/426 , A61K31/44 , A61P3/06 , A61P3/08 , A61P3/10 , C07D277/20 , C07D277/34 , C07D417/12
CPC分类号： C07D417/12 , C07D277/34
摘要： It has now been discovered that certain novel amide substituted thiazolidinedione derivatives show improved blood-glucose lowering activity and are therefore of potential use in the treatment and/or prophylaxis of hyperglycaemia and are of particular use in the treatment of Type II diabetes.
摘要翻译： PCT No.PCT / GB91 / 01833 Sec。 371日期：1993年04月30日 102（e）日期1993年4月30日PCT 1991年10月18日PCT公布。出版物WO92 / 07850 日期：1992年5月14日。现在已经发现，某些新的酰胺取代的噻唑烷二酮衍生物显示改善的血糖降低活性，因此在治疗和/或预防高血糖中具有潜在的用途，并且特别用于治疗类型 II型糖尿病

2. 发明授权

US5075300A Novel compounds 失效
标题翻译：新型化合物
公开(公告)号：US5075300A
公开(公告)日：1991-12-24
申请号：US398490
申请日：1989-08-25
申请人： Richard M. Hindley , David Haigh , Peter T. Duff
发明人： Richard M. Hindley , David Haigh , Peter T. Duff
IPC分类号： C07D277/20 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/496 , A61K31/505 , A61P3/06 , A61P3/08 , A61P9/00 , C07D263/58 , C07D277/34 , C07D417/12
CPC分类号： C07D417/12
摘要： A compound of formula (I): ##STR1## or a tautomeric form thereof and/or a pharamaceutically acceptable salt thereof, and/or a pharmaceutically acceptable solvate thereof, wherein:A.sup.1 represents a substituted or unsubstituted aromatic heterocyclyl group;A.sup.2 represents a benzene ring having in total up to five substituents;X represents O, S or NR.sup.1 l wherein R.sup.1 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;Y represents O or S providing that Y does not represent O when X represents NR.sup.1 ;R.sup.2 and R.sup.3 each represent hydrogen, or R.sup.2 and R.sup.3 together represent a bond; andn represents an integer in the range of from 2 to 6; a process for preparing such a compound; a pharmaceutical composition comprising such a compound; and the use of such a compound and a composition in medicine.

3. 发明授权

US5478850A Thiazolidinedione derivatives 失效
标题翻译：噻唑烷二酮衍生物
公开(公告)号：US5478850A
公开(公告)日：1995-12-26
申请号：US50116
申请日：1993-04-30
申请人： Richard M. Hindley , David Haigh , Graham P. Cottam
发明人： Richard M. Hindley , David Haigh , Graham P. Cottam
IPC分类号： A61K31/425 , A61K31/426 , A61P3/06 , A61P3/08 , A61P3/10 , C07D277/20 , C07D277/34 , C07D417/12
CPC分类号： C07D417/12 , C07D277/34
摘要： ##STR1## A compound of formula (I) or a tautomeric form thereof and/or a pharmaceutically acceptable salt thereof, and/or a pharmaceutically acceptable solvate thereof, wherein R
1 and R
2 each independently represent an alkyl group, a substituted or unsubstituted aryl group or an aralkyl group being substituted or unsubstituted in the aryl or alkyl moiety; or R
1 together with R
2 represents a linking group, the linking group consisting of an optionally substituted methylene group and either a further optionally substituted methylene group or an O or S atom, optional substituents for the said methylene groups being selected from alkyl, aryl or aralkyl or substituents of adjacent methylene groups together with the carbon atoms to which they are attached form a substituted or unsubstituted phenylene group; R
3 and R
4 each represent hydrogen, or R
3 and R
4 together represent a bond; A
1 represents a benzene ting having in total up to three optional substituents; X represents O or S; and n represents an integer in the range of from 2 to 6; a process for preparing such a compound, a pharmaceutical composition containing such a compound and the use of such a compound and composition in medicine.
摘要翻译： PCT No.PCT / GB91 / 01835 Sec。 371日期：1993年04月30日 102（e）日期1993年4月30日PCT 1991年10月18日PCT公布。出版物WO92 / 07839 （I）式（I）化合物或其互变异构形式和/或其药学上可接受的盐，和/或其药学上可接受的溶剂合物，其中R 1和R 2各自独立地表示烷基，取代或未取代的芳基或在芳基或烷基部分被取代或未取代的芳烷基; 或R 1与R 2一起表示连接基团，连接基团由任选取代的亚甲基和进一步任选取代的亚甲基或O或S原子组成，所述亚甲基的任选取代基选自烷基，芳基或芳烷基或相邻亚甲基的取代基与它们所连接的碳原子一起形成取代或未取代的亚苯基; R3和R4各自表示氢，或R3和R4一起表示键; A1代表总共具有三个任选的取代基的苯; X表示O或S; n表示2〜6的整数，制备这种化合物的方法，含有这种化合物的药物组合物以及这种化合物和组合物在医药中的用途。

4. 发明授权

US5869495A Heterocyclic compounds as pharmaceutical 失效
标题翻译：杂环化合物作为药物
公开(公告)号：US5869495A
公开(公告)日：1999-02-09
申请号：US458335
申请日：1995-06-02
申请人： David Haigh , John Thomas Sime
发明人： David Haigh , John Thomas Sime
IPC分类号： C07D239/42 , A61K31/41 , A61K31/42 , A61K31/422 , A61K31/423 , A61K31/44 , A61K31/4402 , A61K31/496 , A61K31/505 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/12 , C07D213/74 , C07D263/58 , C07D277/38 , C07D413/12
CPC分类号： C07D213/74 , C07D263/58 , C07D413/12
摘要： A compound of Formula (I) ##STR1## or a tautomeric form thereof and/or a pharmaceutically acceptable salt thereof, and/or a pharmaceutically acceptable solvate thereof, whereinA.sup.1, A.sup.2, A.sup.3, R.sup.2, X, Y and n are as defined herein; a pharmaceutical composition comprising such a compound and the use of such a compound or composition in medicine.
摘要翻译：式（I）化合物A1X（CH2）nOA2A3Y.R2（I）或其互变异构形式和/或其药学上可接受的盐，和/或其药学上可接受的溶剂化物，其中A1，A2，A3，R2，X ，Y和n如本文所定义; 包含这种化合物的药物组合物和这种化合物或组合物在医药中的用途。

5. 发明授权

US07304087B2 1-acyl-pyrrolidine derivatives for the treatment of viral infections 失效
标题翻译： 1-酰基 - 吡咯烷衍生物用于治疗病毒感染
公开(公告)号：US07304087B2
公开(公告)日：2007-12-04
申请号：US10531884
申请日：2003-10-22
申请人： David Haigh , Charles David Hartley , Peter David Howes , Deborah Lynette Jackson , Pritom Shah , Martin John Slater
发明人： David Haigh , Charles David Hartley , Peter David Howes , Deborah Lynette Jackson , Pritom Shah , Martin John Slater
IPC分类号： A61K31/4025 , C07D405/04 , C07D207/08
CPC分类号： C07D401/04 , C07D207/16 , C07D403/04 , C07D409/04 , C07D413/04 , C07D417/04
摘要： Anti-viral agents of Formula (I) wherein: A represents hydroxy; D represents aryl or heteroaryl; E represents hydrogen, C1-6alkyl, aryl, heteroaryl or heterocyclyl; G represents hydrogen or optionally substituted C1-6alkyl; J represents C1-6alkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl; and salts, solvates and esters thereof; provided that when A is esterified to form —OR where R is selected from straight or branched chain alkyl, aralkyl, aryloxyalkyl, or aryl, then R is other than tert-butyl; processes for their preparation, pharmaceutical compositions comprising them, and methods of using them in HCV treatment are provided.
摘要翻译：式（I）的抗病毒剂

6. 发明授权

US5827865A Heterocyclic compounds as pharmaceutical 失效
标题翻译：杂环化合物作为药物
公开(公告)号：US5827865A
公开(公告)日：1998-10-27
申请号：US460162
申请日：1995-06-02
申请人： David Haigh , John Thomas Sime
发明人： David Haigh , John Thomas Sime
IPC分类号： C07D213/74 , C07D263/58 , A61K31/44
CPC分类号： C07D213/74 , C07D263/58
摘要： Compounds of Formula (I) A.sup.1 --X--(CH.sub.2).sub.n --O--A.sup.2 --A.sup.3 --Y.R.sup.2(I) or a tautomeric form thereof and/or a pharmaceutically acceptable salt thereof, and/or a pharmaceutically acceptable solvate thereof, wherein A.sup.1, A.sup.2, A.sup.3, R.sup.2, X, Y and n are as defined herein; a pharmaceutical composition comprising such a compound and the use of such a compound or composition in medicine as described.
摘要翻译：式（I）化合物A1-X-（CH2）nO-A2-A3-Y.R2（Ⅰ）或其互变异构形式和/或其药学上可接受的盐，和/或其药学上可接受的溶剂合物，其中A1 ，A2，A3，R2，X，Y和n如本文所定义; 包含这种化合物的药物组合物和在所述药物中使用这种化合物或组合物。

7. 发明申请

US20090227600A1 4-(PYRAZINE-2-YL) -PYRROLIDINE -2-CARBOXYLIC ACID COMPOUNDS AND DERIVATIVES THEREOF AS HEPATITIS C VIRUS INHIBITORS 审中-公开
标题翻译： 4-（吡嗪-2-基） - 吡咯烷-2-羧酸化合物及其作为丙型肝炎病毒抑制剂的衍生物
公开(公告)号：US20090227600A1
公开(公告)日：2009-09-10
申请号：US11577940
申请日：2005-10-24
申请人： Rossella Guidetti , David Haigh , Charles David Hartley , Peter David Howes , Fabrizio Nerozzi , Stephen Allan Smith
发明人： Rossella Guidetti , David Haigh , Charles David Hartley , Peter David Howes , Fabrizio Nerozzi , Stephen Allan Smith
IPC分类号： A61K31/497 , C07D417/14 , A61P31/12
CPC分类号： C07D417/14
摘要： Anti-viral agents of Formula (Ia) wherein: A represents hydroxy; B represents C(O)R3 wherein R3 is 4-tert-butyl-3-methoxyphenyl; D represents 1,3-thiazol-2-yl or 5-methyl-1,3-thiazol-2-yl; E represents pyrazin-2-yl; G represents 1,3-thiazol-2-ylmethyl, 1,3-thiazol-4-ylmethyl, 1,2-thiazol-3-ylmethyl, or 1H-pyrazol-1-ylmethyl; and salts, solvates and esters thereof; provided that when A is esterified to form —OR where R is selected from straight or branched chain alkyl, aralkyl, aryloxyalkyl, or aryl, then R is other than tert-butyl, processes for their preparation and their use in HCV treatment are provided.
摘要翻译：式（Ia）的抗病毒剂，其中：A表示羟基; B表示C（O）R 3，其中R 3是4-叔丁基-3-甲氧基苯基; D代表1,3-噻唑-2-基或5-甲基-1,3-噻唑-2-基; E表示吡嗪-2-基; G表示1,3-噻唑-2-基甲基，1,3-噻唑-4-基甲基，1,2-噻唑-3-基甲基或1H-吡唑-1-基甲基; 及其盐，溶剂化物和酯; 条件是当A被酯化形成-OR时，其中R选自直链或支链烷基，芳烷基，芳氧基烷基或芳基，则R不是叔丁基，提供其制备方法及其在HCV治疗中的用途。

8. 发明申请

US20050043390A1 4-(6-membered)-heteroaryl acyl pyrrolidine derivatives as hcv inhibitors 失效
标题翻译： 4-（6-元） - 杂芳基酰基吡咯烷衍生物作为hcv抑制剂
公开(公告)号：US20050043390A1
公开(公告)日：2005-02-24
申请号：US10494127
申请日：2002-10-30
申请人： Gianpaolo Bravi , Rossella Guidetti , David Haigh , Charles Hartley , Peter Howes , Deborah Jackson , Victoria Lovegrove , Pritom Shah , Martin Slater , Katrina Wareing
发明人： Gianpaolo Bravi , Rossella Guidetti , David Haigh , Charles Hartley , Peter Howes , Deborah Jackson , Victoria Lovegrove , Pritom Shah , Martin Slater , Katrina Wareing
IPC分类号： A61K31/4439 , A61K31/497 , A61K31/498 , A61K31/501 , A61K31/506 , A61P1/16 , A61P31/12 , A61P31/14 , C07D401/14 , C07D403/04 , C07D409/14 , C07D417/14 , A61K31/4025 , A61K31/401 , C07D43/02
CPC分类号： C07D401/14 , C07D403/04 , C07D409/14 , C07D417/14
摘要： Novel anti-viral agents of Formula wherein: A represents OR1, NR1R2, or R1 wherein R1 and R2 are hydrogen, C1-6alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; or R1 and R2 together with the nitrogen atom to which they are attached form a 5 or 6 membered saturated cyclic group; B represents C(O)R3 wherein R3 is C1-6alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; C represents C1-6alkyl, aryl, heteroaryl or heterocyclyl; D represents a saturated or unsaturated optionally substituted 6-membered heterocyclic ring; E represents hydrogen or C1-6-alkyl; F represents hydrogen, C1-6alkyl, aryl or heteroaryl; and G represents hydrogen, C1-6alkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl; and salts, solvates and esters thereof, processes for their preparation and methods of using them in HCV treatment are provided.
摘要翻译：新型的式的抗病毒剂其中：A表示OR 1，NR 1 R 2或R 1，其中R 1和R 2是氢，C 1-6烷基，芳基，杂芳基，芳基烷基或杂芳基烷基; 或R 1和R 2与它们所连接的氮原子一起形成5或6元饱和环状基团; B表示C（O）R 3，其中R 3是C 1-6烷基，芳基，杂芳基，芳烷基或杂芳基烷基; C代表C 1-6烷基，芳基，杂芳基或杂环基; D表示饱和或不饱和的任选取代的6元杂环; E表示氢或C 1-6 - 烷基; F表示氢，C 1-6烷基，芳基或杂芳基; 和G表示氢，C 1-6烷基，杂环基烷基，芳基烷基或杂芳基烷基; 提供其盐，溶剂合物和酯，其制备方法及其用于HCV治疗的方法。

9. 发明授权

US5589492A Heterocyclic compounds and their use in the treatment of Type-II diabetes 失效
标题翻译：杂环化合物及其在治疗II型糖尿病中的应用
公开(公告)号：US5589492A
公开(公告)日：1996-12-31
申请号：US318615
申请日：1994-12-12
申请人： David Haigh
发明人： David Haigh
IPC分类号： C07D213/74 , C07D263/58 , C07D413/12 , C07D417/12 , A61K31/42 , A61K31/44
CPC分类号： C07D213/74 , C07D263/58 , C07D413/12 , C07D417/12
摘要： A compound of the formula A.sup.1 --X--(CH.sub.2).sub.n --O--A.sup.2 --A.sup.3 --CO.R.sup.2 (I) or a tautomeric form thereof and/or a pharmaceutically acceptable salt thereof, and/or a pharmaceutically acceptable solvate thereof, wherein: A.sup.1 represents a substituted or unsubstituted aromatic heterocyclyl group; A.sup.2 represents a benzene ring having three optional substituents; A.sup.3 represents a moiety of formula --(CH.sub.2).sub.m --CHR.sup.1 -- wherein R.sup.1 represents a halogen atom or a moiety of formula S(O).sub.p A.sup.4 wherein A.sup.4 represents hydrogen, substituted or unsubstituted alkyl, aryl, aralkyl, alkylcarbonyl or an aromatic heterocyclyl group and p represents zero or an integer 1 or 2 and m represents zero or an integer in the range of from 1 to 5, or A.sup.3 represents a moiety of formula --CH.dbd.CR.sup.1 -- wherein R.sup.1 is as defined above; R.sup.2 represents OR.sup.3 wherein R.sup.3 represents hydrogen, alkyl, aryl or aralkyl, or R.sup.2 represents --NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 each independently represent hydrogen or alkyl or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached form a heterocyclic ring; X represents O, S or NR wherein R 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; and n represents an integer in the range of from 2 to 6; a process for the preparation of such a compound, a pharmaceutical composition comprising such a compound and the use of such a compound and composition in medicine.
摘要翻译： PCT No.PCT / GB93 / 00735 Sec。 371日期1994年12月12日第 102（e）日期1994年12月12日PCT提交1993年4月7日PCT公布。出版物WO93 / 21166 日期：1993年10月28日分子式为A1-X-（CH2）nO-A2-A3-CO.R2（Ⅰ）化合物或其互变异构形式和/或其药学上可接受的盐，和/或其药学上可接受的溶剂合物其中：A1表示取代或未取代的芳族杂环基; A2表示具有三个任选取代基的苯环; A3表示式 - （CH2）m-CHR1的部分，其中R1表示卤素原子或式S（O）pA4的部分，其中A4表示氢，取代或未取代的烷基，芳基，芳烷基，烷基羰基或芳族杂环基并且p表示0或整数1或2，m表示0或1至5的整数，或A3表示式-CH = CR 1的部分，其中R 1如上所定义; R 2表示OR 3，其中R 3表示氢，烷基，芳基或芳烷基，或R 2表示-NR 4 R 5，其中R 4和R 5各自独立地表示氢或烷基或R 4和R 5与它们所连接的氮原子一起形成杂环; X表示O，S或NR，其中R表示氢原子，烷基，酰基，芳基部分可以被取代或未取代的芳烷基，或取代或未取代的芳基; n表示2〜6的整数，制备这种化合物的方法，包含这种化合物的药物组合物和在药物中使用这种化合物和组合物。

10. 发明授权

US07297792B2 Pyrazolopyridines and pyrazolopyridazines as antidiabetics 失效
标题翻译：吡唑并吡啶类和吡唑并吡啶类作为抗糖尿病药
公开(公告)号：US07297792B2
公开(公告)日：2007-11-20
申请号：US11422338
申请日：2006-06-06
申请人： Stephen Garland , David Haigh , Deidre Mary Bernadette Hickey , John Liddle , David Glynn Smith , Robert William Ward , Jason Witherington
发明人： Stephen Garland , David Haigh , Deidre Mary Bernadette Hickey , John Liddle , David Glynn Smith , Robert William Ward , Jason Witherington
IPC分类号： C07D413/00
CPC分类号： C07D471/04 , C07D213/85 , C07D487/04
摘要： The present invention includes compound of formula (I), or a derivative thereof, wherein Y is CH or N; R1 is unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted cycloalkenyl, unsubstituted or substituted aryl, aralkyl wherein the aryl and the alkyl moieties may each independently be unsubstituted or substituted, aralkenyl wherein the aryl, and alkenyl moieties may each independently be unsubstituted or substituted, unsubstituted or substituted heterocyclyl, or heterocyclylalkyl wherein the heterocyclcyl and the alkyl moieties may each inedepently be unsubstituted or substituted; and R2 is unsubstituted aryl or unsubstituted or substituted or substituted heteroaryl. Additionally the present invention inlcudes 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：本发明包括式（I）化合物或其衍生物，其中Y为CH或N; R 1是未取代或取代的烷基，未取代或取代的环烷基，未取代或取代的烯基，未取代或取代的环烯基，未取代或取代的芳基，芳烷基，其中芳基和烷基部分各自独立地为未取代或取代的芳基和烯基部分可以各自独立地是未取代的或取代的，未取代的或取代的杂环基或杂环基烷基，其中杂环基和烷基部分各自是未取代的或取代的; R 2是未取代的芳基或未取代或取代或取代的杂芳基。另外本发明涉及制备这种化合物的方法，含有这种化合物的药物组合物，以及这种化合物在医药中的用途。

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