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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

US06603041B2 Bicyclic enamide derivatives 失效
标题翻译：双环烯酰胺衍生物
公开(公告)号：US06603041B2
公开(公告)日：2003-08-05
申请号：US09947107
申请日：2001-09-05
申请人： Timothy John Norman , John Robert Porter , John Clifford Head , Andrew James Ratcliffe
发明人： Timothy John Norman , John Robert Porter , John Clifford Head , Andrew James Ratcliffe
IPC分类号： C07C6112
CPC分类号： C07D471/04 , A61K31/4375
摘要： Enamide derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk- in which Ar1 is an optionally substituted aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom or group, Ar2 is an optionally substituted arylene or heteroarylene group and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; X is an O or S atom or the group NR30 group; j and k is each zero or the integer 1 or 2 provided that the sum of j and k is zero or the integer 1 or 2; Cy1 is an optionally substituted cycloaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The componds 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 including the inappropriate growth or migration of cells.
摘要翻译：描述了式（1）的酰胺衍生物：其中R1是Ar1L2Ar2Alk-基团，其中Ar1是任选取代的芳族或杂芳族基团，L2是共价键或连接原子或基团，Ar 2是任选取代的亚芳基或杂亚芳基， Alk是链-CH 2 -CH（R） - ， - CH = C（R） - 或其中R是羧酸（-CO 2 H）或其衍生物或生物试剂; R 2是氢原子或C 1-6烷基基团; X是O或S原子或NR30基团; j和k各自为零或整数1或2，条件是j和k的和为零或整数1或2; Cy1是任选取代的脂环族，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。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症性疾病，或疾病包括细胞不适当的生长或迁移。

3. 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。

4. 发明授权

US06953798B1 β-alanine derivates 失效
标题翻译： β-丙氨酸衍生物
公开(公告)号：US06953798B1
公开(公告)日：2005-10-11
申请号：US09450999
申请日：1999-11-29
申请人： John Robert Porter , John Clifford Head , Graham John Warrellow , Sarah Catherine Archibald
发明人： John Robert Porter , John Clifford Head , Graham John Warrellow , Sarah Catherine Archibald
IPC分类号： A61K31/197 , A61K31/40 , A61K31/4406 , A61K31/455 , A61K31/497 , A61K31/506 , A61K31/53 , A61P1/00 , A61P3/10 , A61P7/04 , A61P11/06 , A61P17/06 , A61P29/00 , A61P37/02 , A61P37/06 , C07C233/80 , C07C233/83 , C07D207/16 , C07D207/48 , C07D213/56 , C07D213/81 , C07D213/82 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D403/12 , A61K31/444 , A61P19/10
CPC分类号： C07D213/81 , C07C233/80 , C07C2601/14 , C07D207/16 , C07D213/56 , C07D213/82 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D417/14
摘要： Alkanoic acid derivatives of formula (1) are described: Ar1(Alka)rL1Ar2CH(R1)C(Ra)(Ra′)R (1) Ar1 is an optionally substituted aromatic or heteroarotic group; L1 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted phenylene or nitrogen-containing six-membered heteroarylene group; R is a carboxylic acid (—CO2H) or a derivative thereof; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of α4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
摘要翻译：描述式（1）的烷酸衍生物：<？in-line-formula description =“In-line formula”end =“lead”？> Ar <1> 其中，R 1，R 2，R 2，R 1，R 2，（R））（R i）（R 1）R（1）<βin-line-formula description =“In-line formula”end =“tail”？> Ar < 是任选取代的芳族或杂芳族基团; L 1是共价键或连接原子或基团; Ar 2是任选取代的亚苯基或含氮六元杂亚芳基; R是羧酸（-CO 2 H）或其衍生物; 及其盐，溶剂合物，水合物和N-氧化物。该化合物能够抑制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。

5. 发明授权

US06555562B1 Phenylalanine derivatives 失效
标题翻译：苯丙氨酸衍生物
公开(公告)号：US06555562B1
公开(公告)日：2003-04-29
申请号：US09258522
申请日：1999-02-26
申请人： Sarah Catherine Archibald , John Clifford Head , Graham John Warrellow , John Robert Porter
发明人： Sarah Catherine Archibald , John Clifford Head , Graham John Warrellow , John Robert Porter
IPC分类号： A61K3144
CPC分类号： C07D213/81 , C07C233/87 , C07C235/60 , C07C237/30 , C07C323/62 , C07D213/61
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; Ar is an optionally substituted aromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of alpha4 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; Ar是任选取代的芳族基团;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。

6. 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。

7. 发明授权

US06329362B1 Cinnamic acid derivatives 失效
标题翻译：肉桂酸衍生物
公开(公告)号：US06329362B1
公开(公告)日：2001-12-11
申请号：US09270408
申请日：1999-03-16
申请人： Sarah Catherine Archibald , John Clifford Head , Graham John Warrellow , John Robert Porter
发明人： Sarah Catherine Archibald , John Clifford Head , Graham John Warrellow , John Robert Porter
IPC分类号： A61K3103
CPC分类号： C07D213/82 , A61K38/00 , C07C233/81 , C07K5/06139 , C07K5/06191 , Y10S514/826 , Y10S514/858 , Y10S514/863 , Y10S514/866 , Y10S514/885 , Y10S514/886 , Y10S514/887
摘要： Compounds of formula (1) are described: wherein L1 is a covalent bond or a linker atom or group; R is a carboxylic acid (—CO2H) or a derivative threof; R6 and R7 which may be the same or different is each an atom or group —L2(Alk2)tL3R12 in which L2, L3, Alk2 and t are as previously defined and R12 is a hydrogen or halogen atom or an —OR9, —NR9R10, —NO2, —CN, —CO2R9, —CONR9R10, —COR9, —N(R9)COR10, —N(R9)CSR10, —SO2N(R9)(R10), —N(R9)SO2R9, —N(R9)CON(R10)(R11), —N(R9)CSN(R10)(R11), —N(R9)SO2N(R10)(R11), or an optionally substituted aliphatic, heteroaliphatic, cycloaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group provided that R6 and R7 are not both hydrogen atoms and when R7 is a hydrogen atom then R4 and R5 is each a hydrogen or halogen atom or an alkyl, alkoxy or nitro group; and the salts, solvates, hydrates and N-oxides thereof, for use in modulating cell adhesion. The compounds are able to inhibit the binding of alpha 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）的化合物：其中L 1是共价键或连接原子或基团; R是羧酸（-CO 2 H）或衍生物; R 6和R 7可以相同或不同，各自为原子或基团-L2（Alk2）tL3R12，其中L2，L3，Alk2和t如前定义，R12是氢或卤素原子或-OR9，-NR9R10，-NO2，-CN，-CO2R9，-CONR9R10，-COR9 ，-N（R9）COR10，-N（R9）CSR10，-SO2N（R9）（R10），-N（R9）SO2R9，-N（R9）CON（R10）（R11）（R 10）（R 11），-N（R 9）SO 2 N（R 10）（R 11）或任选取代的脂族，杂脂族，脂环族，杂脂族，芳族或杂芳族基团，条件是R 6和R 7不是氢原子，氢原子然后R4和R5各自为氢或卤素原子或烷基，烷氧基或硝基; 和其盐，溶剂合物，水合物和N-氧化物，用于调节细胞粘附。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。

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

US06469025B1 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：US06469025B1
公开(公告)日：2002-10-22
申请号：US09920206
申请日：2001-08-01
申请人： John Clifford Head , Catherine McKay , John Robert Porter
发明人： John Clifford Head , Catherine McKay , John Robert Porter
IPC分类号： C07D21722
CPC分类号： C07D401/12 , C07D217/22 , C07D401/14 , C07D413/12
摘要： Squaric acid derivatives of formula (1) are described: wherein 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 substitued heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloaliphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group; Alk is a chain —CH2CH(R)—, —CH═C(R)—, in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; Ar2 is an optionally substituted aromatic or heteroaromatic linking group; L2 is a covalent bond or a linker atom or group; R16 is the group —L3(Alk2)tL4R20 in which L3 and L4 which may be the same or different is each a covalent bond or a linker atom or group, t is zero or the integer 1, Alk2 is an optionally substituted aliphatic or heteroaliphatic chain and R20 is an optionally substituted aromatic or heteroaromatic group; 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 including the inappropriate growth or migration of cells.
摘要翻译：描述式（1）的方酸衍生物：其中R1是氢原子或C1-6烷基; L1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，多环脂族，杂多环脂族，芳族或杂芳族基团; Alk是其中R是羧酸（-CO 2 H）或其衍生物或生物试剂的链; Ar 2是任选取代的芳族或杂芳族连接基团; L2是共价键或连接原子或基团; R16是基团-L3（Alk2）tL4R20，其中L3和L4可以相同或不同，各自是共价键或连接基原子或基团，t为零或整数1，Alk2为任选取代的脂族或杂脂族链，R20为任选取代的芳族或杂芳族基团;化合物能够抑制整联蛋白与其结合并且可用于预防和治疗免疫或炎性疾病或包括细胞的不适当生长或迁移的病症。

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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