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1. 发明授权

US06610700B2 Enamine derivatives 失效
标题翻译：使用衍生物
公开(公告)号：US06610700B2
公开(公告)日：2003-08-26
申请号：US09835656
申请日：2001-04-16
申请人： Timothy John Norman , John Robert Porter , Brian Woodside Hutchinson , Andrew James Ratcliffe , John Clifford Head , Rikki Peter Alexander , Barry John Langham , Graham John Warrellow , Sarah Catherine Archibald , Janeen Marsha Linsley
发明人： Timothy John Norman , John Robert Porter , Brian Woodside Hutchinson , Andrew James Ratcliffe , John Clifford Head , Rikki Peter Alexander , Barry John Langham , Graham John Warrellow , Sarah Catherine Archibald , Janeen Marsha Linsley
IPC分类号： A61K31435
CPC分类号： C07D213/81 , C07C229/36 , C07C2601/10 , C07D217/22 , C07D471/04
摘要： Enamine derivatives of formula (1) are described: wherein R1 is a group Ar1 L2Ar2Alk- in which Ar1 is an aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom or group, Ar2 is an arylene or heteroarylene group and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; Cy is a cycloaliphatic or heterocycloaliphatic ring in which X is a N atom or a C(Rw) group; Rx is a oxo, thioxo, or imino group; Rw and Rz is each a hydrogen atom or optional substituent; provided that Cy is not a cyclobutenedione group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.
摘要翻译：描述了式（1）的胺衍生物：其中R1是Ar1，其中Ar1是芳族或杂芳基，L2是共价键或连接原子或基团，Ar2是亚芳基或亚杂芳基，Alk是链-CH 2 -CH（R） - ， - CH = C（R） - ，其中R是羧酸或其衍生物或生物试剂; R 2是氢原子或C 1-6烷基; Cy是脂环族或杂环脂族环，其中X是N原子或C（Rw）基团; Rx是氧代，硫代或亚氨基; Rw和Rz各自是氢原子或任选的取代基;条件是Cy不是环丁烯二酮基团;并且盐，溶剂合物，水合物和N-氧化物。化合物能够抑制整联蛋白与其配体的结合，并且可用于预防和治疗免疫或炎性疾病或涉及细胞不适当生长或迁移的病症。

2. 发明授权

US06780874B2 Enamine derivatives 失效
标题翻译：使用衍生物
公开(公告)号：US06780874B2
公开(公告)日：2004-08-24
申请号：US10458234
申请日：2003-06-10
申请人： Timothy John Norman , John Robert Porter , Brian Woodside Hutchinson , Andrew James Ratcliffe , John Clifford Head , Rikki Peter Alexander , Barry John Langham , Graham John Warrellow , Sarah Catherine Archibald , Janeen Marsha Linsley
发明人： Timothy John Norman , John Robert Porter , Brian Woodside Hutchinson , Andrew James Ratcliffe , John Clifford Head , Rikki Peter Alexander , Barry John Langham , Graham John Warrellow , Sarah Catherine Archibald , Janeen Marsha Linsley
IPC分类号： A61K31435
CPC分类号： C07D213/81 , C07C229/36 , C07C2601/10 , C07D217/22 , C07D471/04
摘要： Enamine derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk- in, which Ar1 is an aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom or group, Ar2 is an arylene or heteroarylene group and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; Cy is a cycloaliphatic or heterocycloaliphatic ring in which X is a N atom or a C(Rw) group; Rx is a oxo, thioxo, or imino group; Rw and Rz is each a hydrogen atom or optional substituent; provided that Cy is not a cyclobutenedione group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.
摘要翻译：描述式（1）的胺衍生物：其中R 1是Ar 1，Ar 2，Ar 2，其中Ar 1是芳族或杂芳族基团，L 2是共价键或连接原子或基团，Ar 2是亚芳基或亚杂芳基，Alk是链-CH 2 -CH（R） - ， - CH = C（R） - ，其中R是羧酸或 R 2是氢原子或C 1-6烷基; Cy是其中X是N原子或C（R））基团的脂环族或杂环脂族环; R x是氢原子或C 1-6烷基; 是氧代，硫代或亚氨基; R w和R z各自为氢原子或任选的取代基; 只要Cy不是环丁烯二酮基团; 和其盐，溶剂合物，水合物和N-氧化物。化合物能够抑制整联蛋白与其配体的结合，并且可用于预防和治疗免疫或炎性疾病或涉及不适当生长或迁移的疾病细胞。

3. 发明授权

US06455539B2 Squaric acid derivates 失效
标题翻译：方酸衍生物
公开(公告)号：US06455539B2
公开(公告)日：2002-09-24
申请号：US09742038
申请日：2000-12-21
申请人： Barry John Langham , Rikki Peter Alexander , John Clifford Head , Janeen Marsha Linsley , John Robert Porter , Sarah Catherine Archibald , Graham John Warrellow
发明人： Barry John Langham , Rikki Peter Alexander , John Clifford Head , Janeen Marsha Linsley , John Robert Porter , Sarah Catherine Archibald , Graham John Warrellow
IPC分类号： C07C22914
CPC分类号： C07D471/04 , C07C229/34 , C07C229/36 , C07C2601/04
摘要： Squaric acid derivatives of formula (1) are described: wherein R1 is a group Ar1Ar2Alk- in which Ar1 is an optionally substituted aromatic or heteroaromatic group; Ar2 is an optionally substituted phenylene or nitrogen-containing six-membered heteroarylene group; and Alk is a chain —CH2—CH(R)—, —CH═C(R)—, in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6 alkyl group; L1 is a covalent bond or a linker atom or group; n is zero or the integer 1; Alk1 is an optionally substituted aliphatic chain; R3 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloaliphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group: and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.
摘要翻译：描述式（1）的方酸衍生物：其中R1是Ar1Ar2Alk-基团，其中Ar1是任选取代的芳族或杂芳族基团; Ar2是任选取代的亚苯基或含氮六元杂亚芳基; 并且Alk是链-CH 2 -CH（R） - ， - CH = C（R） - ，其中R是羧酸（-CO 2 H）或其衍生物或生物固体; R 2是氢原子或C1- 6烷基; L1是共价键或连接原子或基团; n为零或整数1; Alk1为任选取代的脂族链; R3为氢原子或任选取代的杂脂肪族，脂环族，杂环脂族，多环脂族，杂多环脂族，芳族或杂芳族基团：及其盐，溶剂合物，水合物和N-氧化物。化合物能够抑制整联蛋白与其配体的结合，并且可用于预防和治疗免疫或炎性疾病或涉及细胞不适当的生长或迁移。

4. 发明授权

US06740654B2 Squaric acid derivatives 失效
标题翻译：方酸衍生物
公开(公告)号：US06740654B2
公开(公告)日：2004-05-25
申请号：US09899488
申请日：2001-07-05
申请人： Barry John Langham , Rikki Peter Alexander , John Clifford Head , Janeen Marsha Linsley , John Robert Porter , Sarah Catherine Archibald , Graham John Warrellow
发明人： Barry John Langham , Rikki Peter Alexander , John Clifford Head , Janeen Marsha Linsley , John Robert Porter , Sarah Catherine Archibald , Graham John Warrellow
IPC分类号： C07D23514
CPC分类号： C07D495/04 , C07D235/30
摘要： Squaric acid derivatives of formula (1) are described: wherein Het is an optionally substituted bicyclic fused ring heteroaromatic group; L2 is a covalent bond or an atom or group —O—, —S—, —C(O)—, —C(S)—, —S(O)—, —S(O)2, —N(R8)— or —C(R8)(R8a)—; Ar2 is an optionally substituted aromatic or heteroaromatic group; Alk is a chain in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R1 is a hydrogen atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group; Alk1 is an optionally substituted aliphatic chain; n is zero or the integer 1; R2 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloalphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group other than a 2,6-naphthyridin-1-yl, isoquinolin-1-yl, 2,7-naphthyridin-1-yl or quinazolin-4-yl group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.
摘要翻译：描述式（1）的方酸衍生物：其中Het是任选取代的双环稠环杂芳族基团; L 2是共价键或-O - ， - S - ， - C（O） - ， -C（S） - ， - S（O） - ， - S（O）2，-N（R 8） - 或-C（R 8）（R 8a） - ; Ar 2 >是任选取代的芳族或杂芳族基团; Alk是一种链霉素，其中R是羧酸（-CO 2 H）或其衍生物或生物试剂; R 1是氢原子或C 1-6烷基; L 1，是共价键或连接原子或基团; Alk 1是任选取代的脂族链; n是0或整数1; R 2是氢原子或任选取代的杂脂肪族，脂环族，杂脂族，多环烷基，除2,6-二氮杂萘-1-基，异喹啉-1-基，2,7-萘啶-1-基或喹唑啉-4-基之外的杂多环脂族，芳族或杂芳族基;以及盐，溶剂合物，水合物和 N-氧化物。化合物能够抑制整联蛋白与其配体的结合并且可用于预防和治疗免疫或炎性疾病或涉及细胞不适当生长或迁移的病症。

5. 发明授权

US06403608B1 3-Substituted isoquinolin-1-yl derivatives 失效
标题翻译： 3-取代的异喹啉-1-基衍生物
公开(公告)号：US06403608B1
公开(公告)日：2002-06-11
申请号：US09867060
申请日：2001-05-29
申请人： Barry John Langham , Rikki Peter Alexander , John Clifford Head , Janeen Marsha Linsley , John Robert Porter , Sarah Catherine Archibald , Graham John Warrellow
发明人： Barry John Langham , Rikki Peter Alexander , John Clifford Head , Janeen Marsha Linsley , John Robert Porter , Sarah Catherine Archibald , Graham John Warrellow
IPC分类号： C07D21708
CPC分类号： C07D401/12 , C07D217/22 , C07D217/24 , C07D417/12 , C07D487/08
摘要： 3-Substituted isoquinoline containing squaric acids of formula (1) are described: wherein Ar1 is a 3-substituted isoquinolin-1-yl group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted aromatic or heteroaromatic chain; Alk is a chain in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R1 is a hydrogen atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group; Alk1 is an optionally substituted aliphatic chain; n is zero or the integer 1; R2 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloalphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disordes or disorders involving the inappropriate growth or migration of cells.
摘要翻译：描述了含有式（1）的方酸的3-取代的异喹啉：其中Ar1是3-取代的异喹啉-1-基; L2是共价键或连接原子或基团; Ar2是任选取代的芳族或杂芳族链; Alk是其中R是羧酸（-CO 2 H）或其衍生物或生物试剂的链霉素; R 1是氢原子或C 1-6烷基; L 1是共价键或连接原子或基团; Alk1是任选取代的脂族链; n为零或整数1; R 2为氢原子或任选取代的杂脂族，脂环族，杂环脂族，多环芳族，杂多环脂族，芳族或杂芳族基团;及其盐，溶剂合物，水合物和N-氧化物。能够抑制整联蛋白与其配体的结合，并且可用于预防和治疗涉及细胞不适当生长或迁移的免疫或炎症性紊乱或紊乱。

6. 发明授权

US06545013B2 2,7-naphthyridine derivatives 失效
标题翻译： 2,7-萘啶衍生物
公开(公告)号：US06545013B2
公开(公告)日：2003-04-08
申请号：US09867016
申请日：2001-05-29
申请人： Barry John Langham , Rikki Peter Alexander , John Clifford Head , Janeen Marsha Linsley , John Robert Porter , Sarah Catherine Archibald , Graham John Warrellow
发明人： Barry John Langham , Rikki Peter Alexander , John Clifford Head , Janeen Marsha Linsley , John Robert Porter , Sarah Catherine Archibald , Graham John Warrellow
IPC分类号： A61K31435
CPC分类号： C07D471/04 , Y10S977/904
摘要： 2,7-Naphthyridine containing squaric acids of formula (1) are described: wherein Ar1 is an optionally substituted 2,7-naphthridin-1-yl group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted aromatic or heteroaromatic chain; Alk is a chain —CH2CH(R)—, —CH═C(R)—, in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R1 is a hydrogen atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group; Alk1 is an optionally substituted aliphatic chain; n is zero or the integer 1; R2 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloalphatic, heteropoly-cycloaliphatic, aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.
摘要翻译：描述了含有式（1）的方酸的2,7-萘啶：其中Ar1是任选取代的2,7-萘啶-1-基; L2是共价键或连接原子或基团; Ar 2是任选取代的芳族或杂芳族链; Alk是其中R是羧酸（-CO 2 H）或其衍生物或生物试剂的链; R 1是氢原子或C 1-6烷基; L 1是共价键或连接原子或基团; Alk1是任选取代的脂族链; n是0或整数1; R2是氢原子或任选取代的杂脂族，脂环族，杂脂族，多环芳族，杂多环脂族，芳族或杂芳族基团;以及盐，溶剂合物，水合物和化合物能够抑制整联蛋白与其配体的结合，并且可用于预防和治疗涉及细胞不适当生长或迁移的免疫或炎性疾病或病症。

7. 发明授权

US06518283B1 Squaric acid derivatives 失效
标题翻译：方酸衍生物
公开(公告)号：US06518283B1
公开(公告)日：2003-02-11
申请号：US09579317
申请日：2000-05-25
申请人： Barry John Langham , Rikki Peter Alexander , John Clifford Head , Janeen Marsha Linsley , John Robert Porter , Sarah Catherine Archibald , Graham John Warrellow
发明人： Barry John Langham , Rikki Peter Alexander , John Clifford Head , Janeen Marsha Linsley , John Robert Porter , Sarah Catherine Archibald , Graham John Warrellow
IPC分类号： A61K31445
CPC分类号： C07D213/79 , C07B2200/07 , C07C229/34 , C07C229/36 , C07C233/55 , C07C233/81 , C07C235/16 , C07C235/56 , C07C235/64 , C07C235/84 , C07C237/40 , C07C255/57 , C07C271/22 , C07C271/28 , C07C271/58 , C07C2601/04 , C07C2603/18 , C07D213/81 , C07D215/42 , C07D217/22 , C07D239/34 , C07D239/42 , C07D241/42 , C07D241/44 , C07D295/135 , C07D333/70 , C07D471/04 , C40B40/00
摘要： Squaric acid Derivatives of formula (1) are described: wherein R1 is an integrin binding group; R2 is a hydrogen atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group; n is zero or the integer 1; Alk1 is an optionally substituted aliphatic chain; R3 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group: and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune of inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.
摘要翻译：式（1）的方酸描述：其中R1是整联蛋白结合基团; R2是氢原子或C1-6烷基; L1是共价键或连接原子或基团; n是0或整数1; Alk1是任选取代的脂族链; R3是氢原子或任选取代的杂脂族，脂环族，杂脂族，多环脂族，多杂环脂族，芳族或杂芳族基团：及其盐，溶剂合物，水合物和N-氧化物。抑制整联蛋白与其配体的结合，并且可用于预防和治疗炎症性疾病或涉及细胞不适当生长或迁移的疾病的免疫。

8. 发明授权

US06677339B2 Phenylalanine derivatives 失效
标题翻译：苯丙氨酸衍生物
公开(公告)号：US06677339B2
公开(公告)日：2004-01-13
申请号：US09927874
申请日：2001-08-10
申请人： John Clifford Head , John Robert Porter , Graham John Warrellow , Sarah Catherine Archibald , Brian Woodside Hutchinson
发明人： John Clifford Head , John Robert Porter , Graham John Warrellow , Sarah Catherine Archibald , Brian Woodside Hutchinson
IPC分类号： C07D21302
CPC分类号： C07D213/81 , C07D213/89 , C07D251/30 , C07D251/46 , C07D401/12 , C07D409/12 , C07D413/12
摘要： Phenylalanine derivatives of formula (1) are described: in which: Ar1 is an aromatic or heteroaromatic group; L1 is a linker atom or group; R is a carboxylic acid or a derivative thereof; Ar2 is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of &agr;4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
摘要翻译：描述了式（1）的苯丙氨酸衍生物：其中：Ar 1是芳族或杂芳族基团; L 1是连接原子或基团; R是羧酸或其衍生物; Ar 2是任选取代的芳族或杂芳族基团;以及其盐，溶剂合物，水合物和N-氧化物。化合物能够抑制α4整联蛋白与其配体的结合，并且可用于预防和治疗免疫或炎性疾病。

9. 发明授权

US06348463B1 Phenylalanine derivatives 失效
标题翻译：苯丙氨酸衍生物
公开(公告)号：US06348463B1
公开(公告)日：2002-02-19
申请号：US09406560
申请日：1999-09-27
申请人： John Clifford Head , John Robert Porter , Graham John Warrellow , Sarah Catherine Archibald , Brian Woodside Hutchinson
发明人： John Clifford Head , John Robert Porter , Graham John Warrellow , Sarah Catherine Archibald , Brian Woodside Hutchinson
IPC分类号： C07D23924
CPC分类号： C07D213/81 , C07D213/89 , C07D251/30 , C07D251/46 , C07D401/12 , C07D409/12 , C07D413/12
摘要： Phenylalanine derivatives of formula (1) are described: in which: Ar1 is an aromatic or heteroaromatic group; L1 is a linker atom or group; R is a carboxylic acid or a derivative thereof; Ar2 is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of &agr;4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
摘要翻译：描述了式（1）的苯丙氨酸衍生物：其中：Ar1是芳族或杂芳族基团; L1是连接原子或基团; R是羧酸或其衍生物; Ar2是任选取代的芳族或杂芳族基团;和其盐，溶剂合物，水合物和N-氧化物。化合物能够抑制α4整联蛋白与其配体的结合，并且可用于预防和治疗免疫或炎症性疾病。

10. 发明授权

US06362204B1 Phenylalanine derivatives 失效
标题翻译：苯丙氨酸衍生物
公开(公告)号：US06362204B1
公开(公告)日：2002-03-26
申请号：US09317081
申请日：1999-05-20
申请人： John Clifford Head , Sarah Catherine Archibald , Graham John Warrellow , John Robert Porter
发明人： John Clifford Head , Sarah Catherine Archibald , Graham John Warrellow , John Robert Porter
IPC分类号： A61K314439
CPC分类号： C07D213/82 , A61K38/00 , C07K5/06139
摘要： Phenylalanine derivatives of formula (1) are described: wherein R is a carboxylic acid or a derivative thereof; L1 is a linker atom or group; and R5 is a group —L2(CH2)tR6 in which L2 is a —N(R7)CO— or —N(R7)CS— group. The compounds are able to inhibit the binding &agr;4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
摘要翻译：描述了式（1）的苯丙氨酸衍生物：其中R是羧酸或其衍生物; L1是连接原子或基团; R5是其中L2是-N（R7）CO的基团-L2（CH2）tR6 - 或-N（R7）CS-基团。化合物能够抑制结合α4整联蛋白与其配体，并且可用于预防和治疗免疫或炎症性疾病。

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