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1. 发明申请

US20090105291A1 Phenylalanine Enamide Derivatives 失效
标题翻译：苯丙氨酸酰胺衍生物
公开(公告)号：US20090105291A1
公开(公告)日：2009-04-23
申请号：US12327311
申请日：2008-12-03
申请人： Stephen Brand , Stuart Bailey , Julien A. Brown , James A. Johnson , John R. Porter , John C. Head
发明人： Stephen Brand , Stuart Bailey , Julien A. Brown , James A. Johnson , John R. Porter , John C. Head
IPC分类号： A61K31/44 , C07D213/72 , C07D471/04 , A61K31/4545 , A61P29/00 , A61K31/4439 , A61K31/4375 , C07D401/02
CPC分类号： C07D213/81 , C04B35/632 , C07C229/10 , C07C229/46 , C07C233/81 , C07C233/82 , C07C323/30 , C07C2601/04 , C07C2603/94 , C07C2603/96 , C07D213/79 , C07D213/89 , C07D311/96 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04
摘要： Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a group Ar1 L2Ar2Alk- 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; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic 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：描述了式（1）的苯丙氨酸烯酰胺衍生物：其中R1是基团Ar1 L2Ar2Alk-，其中：Ar1是任选取代的芳族或杂芳族基团; L2是共价键或连接体原子或基团; Ar 2是任选取代的亚芳基或亚杂芳基; 并且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; X是-O-或-S-原子或-N（R 2） - 基团，其中：可以相同或不同的R x，R y和R z各自为氢原子或任选的取代基; 或R z是如先前定义的原子或基团，并且R x和R y连接在一起以形成任选取代的螺环连接的脂环族或杂环脂族基团; 及其盐，溶剂合物，水合物和N-氧化物。该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。

2. 发明授权

US07501437B2 Phenylalanine enamide derivatives 失效
标题翻译：苯丙氨酸烯酰胺衍生物
公开(公告)号：US07501437B2
公开(公告)日：2009-03-10
申请号：US11692612
申请日：2007-03-28
申请人： Stephen Brand , Stuart Bailey , Julien A. Brown , James A. Johnson , John R. Porter , John C. Head
发明人： Stephen Brand , Stuart Bailey , Julien A. Brown , James A. Johnson , John R. Porter , John C. Head
IPC分类号： C07D471/04 , A61K31/4375
CPC分类号： C07D213/81 , C04B35/632 , C07C229/10 , C07C229/46 , C07C233/81 , C07C233/82 , C07C323/30 , C07C2601/04 , C07C2603/94 , C07C2603/96 , C07D213/79 , C07D213/89 , C07D311/96 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04
摘要： Phenylalanine 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 in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic 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：描述式（1）的苯丙氨酸烯酰胺衍生物：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亚杂芳基; 并且Alk是其中R是羧酸（-CO 2 H）或其衍生物或生物试剂的链; X是-O-或-S-原子或-N（R 2） - 基团，其中：可以相同或不同的R x，R y和R z各自为氢原子或任选的取代基; 或R z是如先前定义的原子或基团，并且R x和R y连接在一起以形成任选取代的螺环连接的脂环族或杂环脂族基团; 及其盐，溶剂合物，水合物和N-氧化物。该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。

3. 发明授权

US4889553A Herbicides 失效
标题翻译：除草剂
公开(公告)号：US4889553A
公开(公告)日：1989-12-26
申请号：US50733
申请日：1987-05-15
申请人： Graham P. Rowson , John C. Head , Jurgen Westermann , Martin Kruger , Friedrich Arndt , Richard Rees
发明人： Graham P. Rowson , John C. Head , Jurgen Westermann , Martin Kruger , Friedrich Arndt , Richard Rees
IPC分类号： A01N43/653 , A01N43/66 , A01N43/68 , A01N43/76 , A01N43/78 , A01N43/82 , A01N43/824 , A01N47/24 , A01N47/38 , A01N51/00 , C07D249/12 , C07D249/14 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D409/06 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12
CPC分类号： C07D401/04 , A01N43/653 , A01N43/66 , A01N43/68 , A01N43/76 , A01N43/78 , A01N43/82 , A01N47/24 , A01N47/38 , A01N51/00 , C07D249/12 , C07D249/14 , C07D401/12 , C07D403/04 , C07D403/12 , C07D409/06 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12
摘要： Herbicidal triazole sulphonamides of the formula: ##STR1## and salts thereof, where: R.sup.1 represents hydrogen or a substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, aralkyl, acyl, alkoxycarbonyl, aminocarbonyl, sulphonyl or heterocyclic group;R.sup.2 represents hydrogen, halo, cyano, hydroxy, mercapto, a substituted or unsubstituted alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, acyl, alkoxycarbonyl, aminocarbonyl, aryl or amino group, or a heterocyclic group;R.sup.3 represents a substituted or unsubstituted heterocyclic, benzheterocyclic, aryl or aralkyl group; andR.sup.4 represents hydrogen, a substituted or unsubstituted alkyl, alkenyl, alkynyl, acyl, aroyl, alkylsulphonyl, alkoxycarbonyl, aminocarbonyl, aralkyl, or a group of the formula: ##STR2## where R.sup.1 and R.sup.2 are as defined hereinbefore, processes for their preparation and compositions containing them.
摘要翻译：式（I）的除草三唑磺酰胺及其盐，其中：R1表示氢或取代或未取代的烷基，烯基，炔基，环烷基，芳基，芳烷基，酰基，烷氧基羰基，氨基羰基，磺酰基或杂环基; R 2表示氢，卤素，氰基，羟基，巯基，取代或未取代的烷基，烯基，炔基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，酰基，烷氧基羰基，氨基羰基，芳基或氨基或杂环基。 R3表示取代或未取代的杂环，苯并杂环，芳基或芳烷基; R 4代表氢，取代或未取代的烷基，烯基，炔基，酰基，芳酰基，烷基磺酰基，烷氧基羰基，氨基羰基，芳烷基或下式的基团：其中R 1和R 2如上所定义，用于制备和含有它们的组合物。

4. 发明申请

US20090186914A1 Phenylalanine Enamide Derivatives 失效
公开(公告)号：US20090186914A1
公开(公告)日：2009-07-23
申请号：US12415546
申请日：2009-03-31
申请人： Stephen Brand , Stuart Bailey , Julien A. Brown , James A. Johnson , John R. Porter , John C. Head
发明人： Stephen Brand , Stuart Bailey , Julien A. Brown , James A. Johnson , John R. Porter , John C. Head
IPC分类号： A61K31/438 , C07D215/14 , A61K31/47 , A61P11/06 , A61P29/00
CPC分类号： C07D213/81 , C04B35/632 , C07C229/10 , C07C229/46 , C07C233/81 , C07C233/82 , C07C323/30 , C07C2601/04 , C07C2603/94 , C07C2603/96 , C07D213/79 , C07D213/89 , C07D311/96 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04
摘要： Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a group Ar1 L2Ar2Alk- 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; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic 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.

5. 发明授权

US07122556B2 Phenylalanine enamide derivatives 失效
标题翻译：苯丙氨酸烯酰胺衍生物
公开(公告)号：US07122556B2
公开(公告)日：2006-10-17
申请号：US10947032
申请日：2004-09-22
申请人： Stephen Brand , Stuart Bailey , Julien A. Brown , James A. Johnson , John R. Porter , John C. Head
发明人： Stephen Brand , Stuart Bailey , Julien A. Brown , James A. Johnson , John R. Porter , John C. Head
IPC分类号： C07D471/04 , A61K31/4375
CPC分类号： C07D213/81 , C04B35/632 , C07C229/10 , C07C229/46 , C07C233/81 , C07C233/82 , C07C323/30 , C07C2601/04 , C07C2603/94 , C07C2603/96 , C07D213/79 , C07D213/89 , C07D311/96 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04
摘要： Phenylalanine 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 in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic 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：描述了式（1）的苯丙氨酸烯酰胺衍生物：其中R 1是基团Ar 1，L 2，Ar 2， > Alk-其中：Ar 1是任选取代的芳族或杂芳族基团; L 2是共价键或连接原子或基团; Ar 2是任选取代的亚芳基或杂亚芳基; 和Alk是其中R是羧酸（-CO 2 H 2 H）或其衍生物或生物固体的链; X是-O-或-S-原子或-N（R 2）基团，其中：R x，R y和 R“可以相同或不同，各自为氢原子或任选的取代基; 或R z是如前所定义的原子或基团，并且R x和R y连接在一起形成任选取代的螺环连接的脂环族或杂环脂族基团及其盐，溶剂合物，水合物和N-氧化物。该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。

6. 发明授权

US07645770B2 Phenylalanine enamide derivatives 失效
标题翻译：苯丙氨酸烯酰胺衍生物
公开(公告)号：US07645770B2
公开(公告)日：2010-01-12
申请号：US12327311
申请日：2008-12-03
申请人： Stephen Brand , Stuart Bailey , Julien A. Brown , James A. Johnson , John R. Porter , John C. Head
发明人： Stephen Brand , Stuart Bailey , Julien A. Brown , James A. Johnson , John R. Porter , John C. Head
IPC分类号： C07D471/04 , A61K31/4375
CPC分类号： C07D213/81 , C04B35/632 , C07C229/10 , C07C229/46 , C07C233/81 , C07C233/82 , C07C323/30 , C07C2601/04 , C07C2603/94 , C07C2603/96 , C07D213/79 , C07D213/89 , C07D311/96 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04
摘要： Phenylalanine 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; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic 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：描述式（1）的苯丙氨酸烯酰胺衍生物：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亚杂芳基; 并且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; X是-O-或-S-原子或-N（R 2） - 基团，其中：可以相同或不同的R x，R y和R z各自为氢原子或任选的取代基; 或R z是如先前定义的原子或基团，并且R x和R y连接在一起以形成任选取代的螺环连接的脂环族或杂环脂族基团; 及其盐，溶剂合物，水合物和N-氧化物。该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

US5622977A Tri-substituted (aryl or heteroaryl) derivatives and pharmaceutical compositions containing the same 失效
标题翻译：三取代（芳基或杂芳基）衍生物和含有它们的药物组合物
公开(公告)号：US5622977A
公开(公告)日：1997-04-22
申请号：US474214
申请日：1995-06-07
申请人： Graham J. Warrellow , Ewan C. Boyd , Rikki P. Alexander , John C. Head
发明人： Graham J. Warrellow , Ewan C. Boyd , Rikki P. Alexander , John C. Head
IPC分类号： C07C43/235 , C07C59/72 , A61K31/44 , C07D213/04 , C07D405/10 , C07D409/10
CPC分类号： C07C43/235 , C07C59/72
摘要： Compounds of the general formula (1) ##STR1## are described wherein Y is halogen or --OR.sup.1, where R.sup.1 is a substituted or unsubstituted alkyl; X is --O--, --S-- or --N(R.sup.8)--, where R.sup.8 is hydrogen or alkyl; R.sup.2 is substituted or unsubstituted alkyl, alkenyl, cycloalkyl or cycloalkenyl; R.sup.3 is hydrogen, halogen or --OR.sup.9, where R.sup.9 is hydrogen or substituted or unsubstituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl, or formyl, carboxamido or thiocarboxamido; R.sup.4 and R.sup.5, which may be the same or different, are each --(CH.sub.2).sub.n Ar, where Ar is a monocyclic or bicyclic aryl group or monocyclic or bicyclic heteroaryl and n is integer of 0 to 3; R.sup.6 is hydrogen or substituted or unsubstituted alkyl; R.sup.7 is hydrogen or substituted or unsubstituted alkyl; and the salts, solvates, hydrates and N-oxides thereof. Compounds according to the invention are potent, selective and orally active PDE IV inhibitors and are useful in the prophylaxis and treatment of asthma and other diseases.
摘要翻译：其中Y为卤素或-OR 1，其中R 1为取代或未取代的烷基; X是-O - ， - S-或-N（R 8） - ，其中R 8是氢或烷基; R2是取代或未取代的烷基，烯基，环烷基或环烯基; R3是氢，卤素或-OR9，其中R9是氢或取代或未取代的烷基，烯基，烷氧基烷基或烷酰基，或甲酰基，甲酰氨基或硫代羧酰胺基; R 4和R 5可以相同或不同，各自为 - （CH 2）n Ar，其中Ar为单环或双环芳基或单环或双环杂芳基，n为0至3的整数; R6是氢或取代或未取代的烷基; R7是氢或取代或未取代的烷基; 及其盐，溶剂合物，水合物和N-氧化物。根据本发明的化合物是有效的，选择性和口服活性的PDE IV抑制剂，并且可用于预防和治疗哮喘和其它疾病。

8. 发明授权

US5608070A Enantioselective process for the preparation of chiral triaryl derivatives and chiral intermediates for use therein 失效
标题翻译：用于制备手性三芳基衍生物和手性中间体的对映选择性方法
公开(公告)号：US5608070A
公开(公告)日：1997-03-04
申请号：US361439
申请日：1994-12-21
申请人： Rikki P. Alexander , Graham J. Warrellow , John C. Head , Ewan C. Boyd , John R. Porter
发明人： Rikki P. Alexander , Graham J. Warrellow , John C. Head , Ewan C. Boyd , John R. Porter
IPC分类号： C07D233/64 , C07D213/30 , C07D213/32 , C07D213/55 , C07D213/56 , C07D401/06 , C07D409/06 , C07D417/06 , C07D417/14 , C07D417/00
CPC分类号： C07D213/30 , C07D417/06 , C07D417/14
摘要： An enantioselective multi-stage process is described which uses as a starting material an .alpha.,.beta.-unsaturated olefin of formula (1):Ar--CH.dbd.C(R.sup.4)COAux (1)where Ar and R.sup.4, which may be the same or different, is each a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; and Aux is the residue of a chiral (R- or S-) auxiliary.In the process, the olefin is converted to a chiral triarylethane which is of use in medicine.
摘要翻译：描述了使用式（1）的α，β-不饱和烯烃作为原料的对映选择性多阶段方法：Ar-CH = C（R 4）COAux（1）其中Ar和R 4可以相同或各自是任选含有一个或多个选自氧，硫或氮原子的杂原子的单环或双环芳基; Aux是手性（R-或S-）辅助物的残基。在此过程中，烯烃被转化为在医学上有用的手性三芳基乙烷。

9. 发明授权

US07786177B2 Phenylalanine enamide derivatives 失效
标题翻译：苯丙氨酸烯酰胺衍生物
公开(公告)号：US07786177B2
公开(公告)日：2010-08-31
申请号：US12415546
申请日：2009-03-31
申请人： Stephen Brand , Stuart Bailey , Julien A. Brown , James A. Johnson , John R. Porter , John C. Head
发明人： Stephen Brand , Stuart Bailey , Julien A. Brown , James A. Johnson , John R. Porter , John C. Head
IPC分类号： C07D215/14 , A61K31/47 , A61K31/438 , A61P11/06 , A61P29/00
CPC分类号： C07D213/81 , C04B35/632 , C07C229/10 , C07C229/46 , C07C233/81 , C07C233/82 , C07C323/30 , C07C2601/04 , C07C2603/94 , C07C2603/96 , C07D213/79 , C07D213/89 , C07D311/96 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04
摘要： Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a group Ar1 L2Ar2Alk- 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; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic 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：描述了式（1）的苯丙氨酸烯酰胺衍生物：其中R1是基团Ar1 L2Ar2Alk-，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亚杂芳基; 并且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; X是-O-或-S-原子或-N（R 2） - 基团，其中：可以相同或不同的R x，R y和R z各自为氢原子或任选的取代基; 或R z是如先前定义的原子或基团，并且R x和R y连接在一起以形成任选取代的螺环连接的脂环族或杂环脂族基团; 及其盐，溶剂合物，水合物和N-氧化物。该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。

10. 发明授权

US07531549B2 Phenylalanine enamide derivatives 失效
标题翻译：苯丙氨酸烯酰胺衍生物
公开(公告)号：US07531549B2
公开(公告)日：2009-05-12
申请号：US11533117
申请日：2006-09-19
申请人： Stephen Brand , Stuart Bailey , Julien A. Brown , James A. Johnson , John R. Porter , John C. Head
发明人： Stephen Brand , Stuart Bailey , Julien A. Brown , James A. Johnson , John R. Porter , John C. Head
IPC分类号： C07D211/82 , C07D471/10 , A61K31/4747
CPC分类号： C07D213/81 , C04B35/632 , C07C229/10 , C07C229/46 , C07C233/81 , C07C233/82 , C07C323/30 , C07C2601/04 , C07C2603/94 , C07C2603/96 , C07D213/79 , C07D213/89 , C07D311/96 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04
摘要： Phenylalanine 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; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic 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：描述式（1）的苯丙氨酸烯酰胺衍生物：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是共价键或连接体原子或基团; Ar 2是任选取代的亚芳基或亚杂芳基; 并且Alk是一条链<？in-line-formula description =“In-line Formulas”end =“lead”？> - CH2-CH（R） - ，-CH-C（R） - 或<？ -formulae description =“In-line Formulas”end =“tail”？>其中R是羧酸（-CO 2 H）或其衍生物或生物试剂; X是-O-或-S-原子或-N（R 2） - 基团，其中：可以相同或不同的R x，R y和R z各自为氢原子或任选的取代基; 或R z是如先前定义的原子或基团，并且R x和R y连接在一起以形成任选取代的螺环连接的脂环族或杂环脂族基团; 及其盐，溶剂合物，水合物和N-氧化物。该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。

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