公开(公告)号：US20060223800A1

公开(公告)日：2006-10-05

申请号：US11422338

申请日：2006-06-06

申请人： Stephen Garland ,  David Haigh ,  Deidre Mary Hickey ,  John Liddle ,  David Smith ,  Robert Ward ,  Jason Witherington

发明人： Stephen Garland ,  David Haigh ,  Deidre Mary Hickey ,  John Liddle ,  David Smith ,  Robert Ward ,  Jason Witherington

IPC分类号： A61K31/5377 ,  A61K31/496 ,  A61K31/4745 ,  C07D471/02

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。

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。

公开(公告)号：US07109199B2

公开(公告)日：2006-09-19

申请号：US10381292

申请日：2001-09-19

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： C07D487/04 ,  C07D471/04 ,  A61K31/4162 ,  A61P3/10

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 heterocyclyl and the alkyl moieties may each independently be unsubstituted or substituted; and R2 is unsubstituted aryl or unsubstituted or substituted or substituted heteroaryl. Additionally the present invention includes 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 芳基和烯基部分可各自独立地为未取代或取代的未取代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独立地为未取代或取代的; R 2是未取代的芳基或未取代或取代或取代的杂芳基。 另外本发明包括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。

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。

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

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。

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.

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。

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。

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。