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1. 发明授权

US08399483B2 Quinoxaline and quinoline derivatives as kinase inhibitors 有权
标题翻译：喹喔啉和喹啉衍生物作为激酶抑制剂
公开(公告)号：US08399483B2
公开(公告)日：2013-03-19
申请号：US12809394
申请日：2008-12-17
申请人： Daniel Rees Allen , George Martin Buckley , Roland Bürli , John Richard Davenport , Natasha Kinsella , Christopher James Lock , Christopher Lowe , Stephen Robert Mack , William Ross Pitt , Andrew James Ratcliffe , Marianna Dilani Richard , Verity Margaret Sabin , Andrew Sharpe , Laura Jane Tait , Graham John Warrellow , Sophie Caroline Williams
发明人： Daniel Rees Allen , George Martin Buckley , Roland Bürli , John Richard Davenport , Natasha Kinsella , Christopher James Lock , Christopher Lowe , Stephen Robert Mack , William Ross Pitt , Andrew James Ratcliffe , Marianna Dilani Richard , Verity Margaret Sabin , Andrew Sharpe , Laura Jane Tait , Graham John Warrellow , Sophie Caroline Williams
IPC分类号： A61K31/47
CPC分类号： C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/14 , C07D473/34 , C07D473/36
摘要： A series of heteroaryl-substituted quinoxaline and quinoline derivatives, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions, said substituted derivatives having the general formula
摘要翻译：因此，作为PI3激酶的选择性抑制剂的一系列杂芳基取代的喹喔啉和喹啉衍生物在医学中是有益的，例如在治疗炎性，自身免疫，心血管，神经退行性，代谢性，肿瘤学，伤害性感受性或眼科疾病中，所述具有通式的取代衍生物

2. 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。

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

US6093696A Tyrosine derivatives 失效
标题翻译：酪氨酸衍生物
公开(公告)号：US6093696A
公开(公告)日：2000-07-25
申请号：US86421
申请日：1998-05-29
申请人： John Clifford Head , Sarah Catherine Archibald , Graham John Warrellow
发明人： John Clifford Head , Sarah Catherine Archibald , Graham John Warrellow
IPC分类号： A61K38/00 , A61P1/00 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P29/00 , A61P43/00 , C07D277/06 , C07K5/02 , C07K5/06 , C07K5/078 , A61K31/425 , A61K38/05
CPC分类号： C07K5/06139 , C07D277/06 , C07K5/0202 , C07K5/0205 , C07K5/021 , C07K5/06191 , A61K38/00
摘要： Tyrosine derivatives of formula (1) are described: ##STR1## in which R is (1) a group R.sup.1 X.sup.1 -- where R.sup.1 is an optionally substituted alkyl or aromatic group, and X.sup.1 is a covalent bond or a --(CH.sub.2).sub.n -- [where n is an integer 1 or 2], --C(O)--, --CH.sub.2 C(O)--, --NHC(O)--, --CH.sub.2 NHC(O)--, or --SO.sub.2 -- group, or (2) a group (Hal.sup.1).sub.3 CSO.sub.2 --, where Hal.sup.1 is a fluorine or chlorine atom;R.sup.2 and R.sup.3, which may be the same or different, is each a hydrogen or halogen atom or an alkyl, alkoxy, hydroxyl or nitro group;Alk is an alkylene chain;m is zero or an integer 1;R.sup.4 is a hydrogen atom or a methyl group;R.sup.5 is a group --(CH.sub.2).sub.p CO.sub.2 R.sup.8 where p is zero or an integer 1 and R.sup.8 is a hydrogen atom or an alkyl group;R.sup.6 is a hydrogen atom or an alkyl group;Y is a sulphur atom or a --S(O).sub.q -- group where q is an integer 1 or 2;X.sup.2 is a --C(O)--, --C(O)O--, --CONH-- or --S(O).sub.2 -- group;R.sup.7 is an optionally substituted alkyl group or an aryl or aralkyl group;and the salts, solvates and hydrates thereof.The compounds are able to inhibit the binding of .alpha..sub.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）的酪氨酸衍生物：其中R是（1）R1X1基团，其中R1是任选取代的烷基或芳族基团，并且X 1是共价键或 - （CH 2）n - [其中n是整数1或2]，-C（O） - ， - CH 2 C（O） - ， - NHC（O） - ， - CH 2 NHC（O） - 或-SO 2 - 基，或（2） 3CSO2-，其中Hal1是氟或氯原子; R 2和R 3可以相同或不同，各自为氢或卤素原子或烷基，烷氧基，羟基或硝基; Alk是亚烷基链; m为零或整数1; R4是氢原子或甲基; R5是 - （CH2）pCO2R8基团，其中p为0或整数1，R8为氢原子或烷基; R6是氢原子或烷基; Y是硫原子或-S（O）q-基，其中q是整数1或2; X2是-C（O） - ， - C（O）O-，-CONH-或-S（O）2 - 基团; R7是任选取代的烷基或芳基或芳烷基; 及其盐，溶剂化物和水合物。这些化合物能够抑制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。

9. 发明授权

US5962483A Trisubstituted phenyl derivatives and processes for their preparation 失效
标题翻译：三取代苯基衍生物及其制备方法
公开(公告)号：US5962483A
公开(公告)日：1999-10-05
申请号：US8173
申请日：1998-01-16
申请人： Graham John Warrellow , Valerie Anne Cole , Rikki Peter Alexander
发明人： Graham John Warrellow , Valerie Anne Cole , Rikki Peter Alexander
IPC分类号： C07D239/26 , A01N43/40 , A01N43/48 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/495 , A61K31/505 , A61P11/08 , A61P29/00 , A61P43/00 , C07C41/20 , C07C43/235 , C07C43/247 , C07C59/72 , C07C67/303 , C07C67/343 , C07C69/734 , C07C69/736 , C07C209/10 , C07C209/68 , C07C211/52 , C07C237/08 , C07C253/30 , C07C255/32 , C07C255/37 , C07C319/20 , C07C323/09 , C07C323/20 , C07C323/62 , C07C327/38 , C07D213/30 , C07D213/34 , C07D213/56 , C07D213/57 , C07D213/61 , C07D213/73 , C07D237/08 , C07D241/12 , C07D213/02 , C07D239/24
CPC分类号： C07D213/30 , C07C255/37 , C07D213/73 , C07D237/08 , C07D241/12 , C07C2101/08
摘要： Compounds of general formula (1) ##STR1## are described wherein Y is a halogen atom or a group --OR.sup.1, where R.sup.1 is an optionally substituted alkyl group; X is --O--, --S-- or --N(R.sup.7)--, where R.sup.7 is a hydrogen atom or an alkyl group; R.sup.2 is an optionally substituted cycloalkyl or cycloalkenyl group; R.sup.3 and R.sup.4, which may be the same or different, is each a hydrogen atom or an alkyl, --CO.sub.2 R.sup.8 (where R.sup.8 is a hydrogen atom or an alkyl, aryl, or aralkyl group), --CONR.sup.9 R.sup.10 (where R.sup.9 and R.sup.10 which may be the same or different is each a hydrogen atom or an alkyl, aryl or aralkyl group), --CSNR.sup.9 R.sup.10, --CN, --CH.sub.2 CN group; Z is --(CH.sub.2).sub.n -- (where n is zero or an integer 1, 2 or 3; R.sup.5 is an optionally substituted monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; R.sup.6 is a hydrogen atom or a hydroxyl group; and the salts, solvates, hydrates, prodrugs and N-oxides thereof. Compounds according to the invention are potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of diseases such as asthma where an unwanted inflammatory response or muscular spasm is present.
摘要翻译：其中Y为卤素原子或-OR1基团，其中R 1为任意取代的烷基; X是-O - ， - S-或-N（R 7） - ，其中R 7是氢原子或烷基; R2是任选取代的环烷基或环烯基; R 3和R 4可以相同或不同，分别为氢原子或烷基-CO 2 R 8（其中R 8为氢原子或烷基，芳基或芳烷基），-CONR 9 R 10（其中R 9和R 10可以各自为氢原子或烷基，芳基或芳烷基），-CSNR 9 R 10，-CN，-CH 2 CN基团; Z是 - （CH 2）n - （其中n是0或整数1,2或3; R 5是任选地含有一个或多个选自氧，硫或氮原子的杂原子的任选取代的单环或双环芳基; R 6是氢原子或羟基;以及其盐，溶剂合物，水合物，前药和N-氧化物根据本发明的化合物是有效和选择性的磷酸二酯酶IV型抑制剂，并且可用于预防和治疗诸如哮喘的疾病，其中存在不希望的炎性反应或肌肉痉挛。

10. 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。

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