公开(公告)号：US20070161632A1

公开(公告)日：2007-07-12

申请号：US11686023

申请日：2007-03-14

申请人： Guido Bold ,  Hans-Georg Capraro ,  Giorgio Caravatti ,  Peter Traxler

发明人： Guido Bold ,  Hans-Georg Capraro ,  Giorgio Caravatti ,  Peter Traxler

IPC分类号： A61K31/5377 ,  A61K31/519 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The invention relates to 7H-pyrrolo[2,3-d]pyrimidine derivatives of formula I wherein the symbols and substituents are as defined in the description, to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives—alone or in combination with one or more other pharmaceutically active compounds—for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumour.

摘要翻译： 本发明涉及式I的7H-吡咯并[2,3-d]嘧啶衍生物，其中符号和取代基如说明书中所定义，其制备方法，包含该衍生物的药物组合物及其用途 衍生物 - 单独或与一种或多种其它药学活性化合物组合 - 用于制备用于治疗特别是增殖性疾病如肿瘤的药物组合物。

公开(公告)号：US07091224B2

公开(公告)日：2006-08-15

申请号：US10494591

申请日：2002-11-07

申请人： Guido Bold ,  Pascal Furet ,  Paul W Manley

发明人： Guido Bold ,  Pascal Furet ,  Paul W Manley

IPC分类号： A61K31/44 ,  C07D211/72

CPC分类号： C07D213/64 ,  C07D213/70

摘要： The invention relates to anthranilic acid amide derivatives of formula (I), wherein R1 represents H or lower alkyl, R2 represents H or lower alkyl, R3 represents perfluoro lower alkyl, and X is O or S, or an N-oxide or a tautomer thereof, to salts of such anthranilic acid amides, their N-oxides and their tautomers; processes for the preparation thereof, the application thereof for the treatment of the human or animal body, the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment especially of a neoplastic disease, such as a tumor disease, of retinopathy or age—related macular degeneration; a method for the treatment of such a disease in animals, especially in humans, and the use of such a compound—alone or in combination with one or more other pharmaceutically active compounds—for the manufacture of a pharmaceutical preparation for the treatment of a neoplastic disease, of retinopathy or age-related macular degeneration.

摘要翻译： 本发明涉及式（I）的邻氨基苯甲酰胺衍生物，其中R 1代表H或低级烷基，R 2代表H或低级烷基，R 3 表示全氟低级烷基，X是O或S，或其N-氧化物或互变异构体，与邻氨基苯甲酸酰胺的盐，它们的N-氧化物及其互变异构体; 其制备方法，其用于治疗人或动物体的应用，其单独使用或与一种或多种其它药学活性化合物组合用于特别是肿瘤性疾病如肿瘤疾病的治疗 ，视网膜病变或年龄相关性黄斑变性; 用于治疗动物，特别是人类中的这种疾病的方法，以及使用这样的化合物 - 单独或与一种或多种其它药学活性化合物组合 - 用于制备用于治疗肿瘤的药物制剂 视网膜病变或年龄相关性黄斑变性疾病。

公开(公告)号：US20060074112A1

公开(公告)日：2006-04-06

申请号：US11254897

申请日：2005-10-20

申请人： Karl-Heinz Altmann ,  Guido Bold ,  Pascal Furet ,  Paul Manley ,  Jeanette Wood ,  Stefano Ferrari ,  Francesco Hofmann ,  Jurgen Mestan ,  Andreas Huth ,  Martin Kruger ,  Dieter Seidelmann ,  Andreas Menrad ,  Martin Haberey ,  Karl-Heinz Thierauch

发明人： Karl-Heinz Altmann ,  Guido Bold ,  Pascal Furet ,  Paul Manley ,  Jeanette Wood ,  Stefano Ferrari ,  Francesco Hofmann ,  Jurgen Mestan ,  Andreas Huth ,  Martin Kruger ,  Dieter Seidelmann ,  Andreas Menrad ,  Martin Haberey ,  Karl-Heinz Thierauch

IPC分类号： C07D213/56 ,  A61K31/44 ,  C07D233/54

CPC分类号： A61K31/415 ,  A61K31/44 ,  A61K31/47 ,  C07D213/38 ,  C07D213/56 ,  C07D213/64 ,  C07D213/89 ,  C07D215/12 ,  C07D233/54 ,  C07D405/12

摘要： Described are compunds of formula (I), wherein W is O or S; X is NR8; Y is CR9R10—(CH2)n wherein R9 and R10 are independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is SO2; R1 is aryl; R2 is a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms with the exception that R2 cannot represent 2-phthalimidyl, and in case of Y═SO2 cannot represent 2,1,3-benzothiadiazol-4-yl; any of R3, R4, R5 and R6, independently of the other, is H or a substituent other than hydrogen; and R7 and R8, independently of each, other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g. of a neoplastic disease, such as a tumor disease, of retinopathy and age-related macular degeneration.

摘要翻译： 描述的是式（I）的化合物，其中W是O或S; X是NR 8; Y是CR 9 R 10其中R 9是（CH 2）n - 和R 10彼此独立地为氢或低级烷基，n为0〜3的整数。 或Y为SO 2; R 1是芳基; R 2是包含一个或多个环氮原子的单环或双环杂芳基，除了R 2不能表示2-邻苯二甲酰亚氨基，并且在Y-SO的情况下 2不能表示2,1,3-苯并噻二唑-4-基; R 3，R 4，R 5和R 6中的任何一个独立地是H或 除氢以外的取代基; R 7和R 8分别独立地为H或低级烷基; 或N-氧化物或其药学上可接受的盐在制备用于治疗对VEGF受体酪氨酸激酶活性的抑制作出反应的肿瘤疾病的药物产品中的用途。 式（I）化合物可用于治疗，例如， 的肿瘤疾病，如肿瘤疾病，视网膜病变和年龄相关性黄斑变性。

公开(公告)号：US06686347B2

公开(公告)日：2004-02-03

申请号：US09964025

申请日：2001-09-26

申请人： Guido Bold ,  Janet Dawson King ,  Jörg Frei ,  Richard Heng ,  Paul William Manley ,  Bernhard Wietfeld ,  Jeanette Marjorie Wood

发明人： Guido Bold ,  Janet Dawson King ,  Jörg Frei ,  Richard Heng ,  Paul William Manley ,  Bernhard Wietfeld ,  Jeanette Marjorie Wood

IPC分类号： A61K3133

CPC分类号： C07D401/06 ,  A61K31/501 ,  A61K31/502 ,  C07D401/14

摘要： The invention relates to the treatment of an inflammatory disease, especially an inflammatory rheumatoid or rheumatic disease, and/or pain with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, the substituents being defined in the specification; as well as to new phthalazine derivatives; processes for the preparation thereof; the application thereof in a process for the treatment of the human or animal body; the use thereof for the treatment of a disease, especially a disease caused by ocular neovascularization, such as age-related macula degeneration or diabetic retinopathy, or other diseases that respond to the inhibition of tyrosine kinases, such as a proliferative disease; a method for the treatment of such disease in mammals; and the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment especially of a disease as mentioned above.

摘要翻译： 本发明涉及治疗炎症性疾病，特别是炎性类风湿病或风湿性疾病，和/或具有式I的VEGF受体酪氨酸激酶的活性抑制剂的疼痛，所述取代基在本说明书中定义;以及 新的酞嗪衍生物; 制备方法; 其用于治疗人或动物体的过程中的应用; 其用于治疗疾病，特别是由眼睛新生血管形成引起的疾病，例如年龄相关性黄斑变性或糖尿病性视网膜病，或其它对酪氨酸激酶（例如增殖性疾病）的抑制作用的疾病; 哺乳动物治疗这种疾病的方法; 以及这种化合物用于制造特别是上述疾病的药物制剂的用途。

公开(公告)号：US06514974B2

公开(公告)日：2003-02-04

申请号：US09859858

申请日：2001-05-17

申请人： Guido Bold ,  Jörg Frei ,  Peter Traxler ,  Karl-Heinz Altmann ,  Helmut Mett ,  David Raymond Stover ,  Jeanette Marjorie Wood

发明人： Guido Bold ,  Jörg Frei ,  Peter Traxler ,  Karl-Heinz Altmann ,  Helmut Mett ,  David Raymond Stover ,  Jeanette Marjorie Wood

IPC分类号： A61K3150

CPC分类号： C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04

摘要： The invention relates to compounds of formula I, wherein r is 0 to 2, n is 0 to 2; m is 0 to 4; R1 and R2 (i) are in each case a lower alkyl, or (ii) together form a bridge in subformula I* or (iii) together form a bridge in subformula I** wherein one or two of the ring members T1, T2, T3, and T4 are nitrogen, and the remainder are in each case CH; A, B, D, and E are N or CH, wherein not more than 2 of these radicals are N; G is lower alkylene, acyloxy- or hydroxy-lower alkylene, —CH2—O—, —CH2—S—, —CH2—NH—, oxa, thia, or imino; Q is methyl; R is H or lower alkyl; X is imino, oxa, or thia; Y is aryl, pyridyl, or (un)substituted cycloalkyl; and Z is mono- or disubstited amino, halogen, alkyl, substituted alkyl, hydroxy, etherified or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-disubstituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, phenyl-lower alkylthio, alkylphenylthio, phenylsulfinyl, phenyl-lower alkylsulfinyl, alkylphenylsulfinyl, phenylsulfonyl, phenyl-lower alkylsulfonyl, or alkylphenylsulfony; and wherein the bonds characterized by a wavy line are either single or double bonds; or an N-oxide of said compound with the stipulation that, if Y is pyridyl or unsubstituted cycloalkyl, X is imino, and the remaining radicals are as defined, then G is selected from the group comprising lower alkylene, —CH2—O—, —CH2—S—, oxa and thia; or a salt thereof. The compounds inhibit angiogenesis.

摘要翻译： 本发明涉及式I化合物，其中r为0至2，n为0至2; m为0〜4; R1和R2（i）在每种情况下都是低级烷基，或（ii）一起在子式I *中形成桥，或（iii）一起形成子式I **中的桥，其中一个或两个环成员T1，T2 ，T3和T4是氮，余数分别为CH; A，B，D和E是N或CH，其中不多于2个这些基团是N; G是低级亚烷基，酰氧基或羟基 - 低级亚烷基，-CH 2 -O-，-CH 2 -S-，-CH 2 -NH-，氧杂，硫杂或亚氨基; Q是甲基; R为H或低级烷基; X是亚氨基，氧杂或硫杂; Y是芳基，吡啶基或（未）取代的环烷基; 羟基，醚化或酯化的羟基，硝基，氰基，羧基，酯化的羧基，烷酰基，氨基甲酰基，N-单或N，N-二取代的氨基甲酰基，脒基， 胍基，巯基，磺基，苯硫基，苯基 - 低级烷硫基，烷基苯硫基，苯基亚磺酰基，苯基 - 低级烷基亚磺酰基，烷基苯基亚磺酰基，苯基磺酰基，苯基 - 低级烷基磺酰基或烷基苯基磺酰基。 并且其中以波浪线表征的键是单键或双键; 或所述化合物的N-氧化物，其规定如果Y是吡啶基或未取代的环烷基，则X是亚氨基，剩余的基团如所定义，则G选自低级亚烷基，-CH 2 -O-， -CH 2 -S-，氧杂和硫杂; 或其盐。 该化合物抑制血管发生。

公开(公告)号：US6140317A

公开(公告)日：2000-10-31

申请号：US117056

申请日：1998-07-22

申请人： Peter Traxler ,  Jorg Frei ,  Guido Bold

发明人： Peter Traxler ,  Jorg Frei ,  Guido Bold

IPC分类号： A61K31/00 ,  A61K31/505 ,  A61K31/519 ,  A61K31/529 ,  A61P17/00 ,  A61P17/06 ,  A61P35/00 ,  A61P35/02 ,  A61P43/00 ,  C07D487/04 ,  A01N43/00 ,  A61K31/50 ,  C07D239/00 ,  C07D491/00 ,  C07F5/02

CPC分类号： C07D487/04

摘要： There are described compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2 are as defined in the description, Q is heterocyclyl boned via a ring nitrogen atom and having the formula IA ##STR2## wherein R.sub.3 and R.sub.4 and m and n are as defined in the description, the ring marked A is a heterocyclyl having 5 to 9 ring atoms and having at least one saturated bond, it being possible for a further ring hetero atom selected from O and S to be present in addition to the bonding nitrogen atom, the ring system marked B is a free or benzo-, thieno-, furo-, pyrrolo- or dihydropyrrolo-fused carbocyclic ring having from 5 to 9 carbon atoms that is fused to the ring A and may be unsaturated, partially saturated or fully saturated, and the bond marked by a parallel dotted line between the ring systems marked A and B is either a single bond or a double bond, and a salt thereof where at least one salt-forming group is present. The compounds are inhibitors of protein kinases and have, for example, antitumour activity.

摘要翻译： PCT No.PCT / EP97 / 00127 Sec。 371日期：1998年7月22日 102（e）日期1998年7月22日PCT 1997年1月13日PCT PCT。 公开号WO97 / 27199 日期：1997年7月31日描述式I化合物，其中R 1和R 2如说明书中所定义，Q是经由环氮原子并具有式IA的杂环基，其中R 3和R 4以及m和n如 描述中，标记为A的环是具有5至9个环原子并且具有至少一个饱和键的杂环基，除了键合氮原子之外，还可以存在另外选自O和S的环杂原子，所述环 标记为B的系统是具有5至9个碳原子的游离或苯并，噻吩并 - 二氢吡咯并 - 稠合的碳环，其与环A稠合并且可以是不饱和的，部分饱和的或完全饱和的，以及 标记为A和B的环状体系之间的平行虚线标记的键是单键或双键，以及其中存在至少一个成盐基团的盐。 这些化合物是蛋白激酶的抑制剂，并且具有例如抗肿瘤活性。

公开(公告)号：US5981533A

公开(公告)日：1999-11-09

申请号：US930904

申请日：1997-10-03

申请人： Peter Traxler ,  Pascal Furet ,  Guido Bold ,  Jorg Frei ,  Marc Lang

发明人： Peter Traxler ,  Pascal Furet ,  Guido Bold ,  Jorg Frei ,  Marc Lang

IPC分类号： C07D231/38 ,  A61K31/505 ,  A61P35/00 ,  A61P43/00 ,  C07D487/04

CPC分类号： C07D487/04

摘要： 4-Amino-1H-pyrazolo[3,4-d]pyrimidine derivatives of formula I ##STR1## wherein the symbols are as defined in claim 1, and intermediates for their manufacture are described.The compounds of formula I inhibit especially the tyrosine kinase activity of the receptor for epidermal growth factor and can be used, for example, in the case of epidermal hyperproliferation (psoriasis) and as anti-tumor agents.

摘要翻译： PCT No.PCT / EP96 / 01263。 371日期1997年10月3日第 102（e）日期1997年10月3日PCT 1996年3月22日PCT公布。 公开号WO96 / 31510PC。 日期：19964年10月10日 - 描述了式I的氨基-1H-吡唑并[3,4-d]嘧啶衍生物，其中符号如权利要求1中所定义，其中描述其制备方法。 式I的化合物特别地抑制表皮生长因子受体的酪氨酸激酶活性，并且可以用于例如表皮过度增生（牛皮癣）和作为抗肿瘤剂的情况。

公开(公告)号：US5912352A

公开(公告)日：1999-06-15

申请号：US866558

申请日：1997-05-30

申请人： Alexander Fassler ,  Guido Bold ,  Hans-Georg Capraro ,  Heinz Steiner

发明人： Alexander Fassler ,  Guido Bold ,  Hans-Georg Capraro ,  Heinz Steiner

IPC分类号： C07C241/02 ,  C07C253/16 ,  C07C255/44 ,  C07C281/02 ,  C07C281/04 ,  C07D213/42 ,  C07D213/54 ,  C07D213/55 ,  C07D257/04 ,  C07D277/22 ,  C07D277/30 ,  C07D213/02

CPC分类号： C07D213/42 ,  C07C253/16 ,  C07C255/44 ,  C07C281/02 ,  C07C281/04 ,  C07D213/54 ,  C07D213/55 ,  C07D257/04 ,  C07D277/30 ,  C07B2200/07 ,  Y02P20/55

摘要： The invention relates to a novel process for the preparation of compounds of formula I ##STR1## wherein R.sub.1 is hydrogen or a suitable amino-protecting group,R.sub.2 is unsubstituted or substituted alkyl,R.sub.3 is hydrogen, aryl, heterocyclyl, unsubstituted or substituted alkyl or unsubstituted or substituted cycloalkyl,R.sub.4, independently of R.sub.1, is hydrogen or a suitable amino-protecting group andm is a number from 1 to 7; and wherein further suitable protecting groups for functional groups may be present; which compounds are antivirally active or can be used as starting materials for pharmaceutically active, especially antiviral compounds.The precursor is an oxo compound,which is in turn prepared by hydrogenation with a suitable complex hydride or with hydrogen in the presence of a suitable catalyst and acyl migration starting from a hydrazone,which is in turn preferably prepared from a nitrile via an imino compound by means of hydrogenation and reaction with a hydrazine derivative,which is prepared from an aldehyde by reaction with a reactive derivative of a carboxylic acid in the presence of a cyanide salt;and the novel intermediates required therefor.

摘要翻译： 本发明涉及一种制备式I化合物的新方法，其中R 1为氢或适当的氨基保护基，R 2为未取代或取代的烷基，R 3为氢，芳基，杂环基，未取代或取代的烷基或未取代或取代的 环烷基，独立于R 1的R 4是氢或合适的氨基保护基，m是1至7的数; 并且其中可以存在其它合适的官能团保护基团; 哪些化合物是抗病毒活性的或可以用作药物活性的起始原料，特别是抗病毒化合物。 前体是氧代化合物，其又通过在合适的催化剂存在下用合适的络合氢化物或氢气氢化制备，并且从腙开始进行酰基迁移，其又优选通过亚氨基化合物由腈制备 通过氢化和与肼衍生物反应，肼衍生物通过与氰化物的存在下与羧酸的反应性衍生物反应由醛制备; 和所需的新型中间体。

公开(公告)号：US5663200A

公开(公告)日：1997-09-02

申请号：US545170

申请日：1995-10-19

申请人： Guido Bold ,  Hans-Georg Capraro ,  Alexander Fassler ,  Marc Lang ,  Shripad Subray Bhagwat ,  Satish Chandra Khanna ,  Janis Karlis Lazdins ,  Jurgen Mestan

发明人： Guido Bold ,  Hans-Georg Capraro ,  Alexander Fassler ,  Marc Lang ,  Shripad Subray Bhagwat ,  Satish Chandra Khanna ,  Janis Karlis Lazdins ,  Jurgen Mestan

IPC分类号： C07D295/12 ,  A61K31/075 ,  A61K31/16 ,  A61K31/165 ,  A61K31/275 ,  A61K31/325 ,  A61K31/35 ,  A61K31/351 ,  A61K31/352 ,  A61K31/395 ,  A61K31/425 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/47 ,  A61K31/495 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/695 ,  A61K38/05 ,  A61P31/12 ,  A61P31/18 ,  C07C237/22 ,  C07C255/60 ,  C07C271/22 ,  C07C311/19 ,  C07C311/42 ,  C07C317/50 ,  C07D207/12 ,  C07D207/16 ,  C07D207/26 ,  C07D207/28 ,  C07D209/18 ,  C07D209/42 ,  C07D211/40 ,  C07D211/46 ,  C07D211/48 ,  C07D211/60 ,  C07D211/62 ,  C07D213/30 ,  C07D213/65 ,  C07D213/81 ,  C07D213/82 ,  C07D277/06 ,  C07D277/20 ,  C07D277/40 ,  C07D277/56 ,  C07D295/155 ,  C07D295/215 ,  C07D307/20 ,  C07D307/33 ,  C07D309/04 ,  C07D309/12 ,  C07D311/24 ,  C07D317/60 ,  C07D401/04 ,  C07K5/00 ,  A61K31/215 ,  C07C271/20

CPC分类号： C07D207/26 ,  A61K31/47 ,  A61K31/495 ,  C07C255/60 ,  C07C271/22 ,  C07C311/19 ,  C07C311/42 ,  C07C317/50 ,  C07D207/28 ,  C07D209/42 ,  C07D211/46 ,  C07D211/62 ,  C07D213/30 ,  C07D213/82 ,  C07D277/06 ,  C07D277/40 ,  C07D295/155 ,  C07D307/20 ,  C07D309/04 ,  C07D309/12 ,  C07D311/24 ,  C07D317/60 ,  C07C2101/14 ,  C07C2102/10

摘要： Antiretroviral compounds (which are effective, for example, against HIV) of the formula I ##STR1## in which R.sub.1 is an acyl radical lower-alkoxyl-lower-alkanoyl whose lower alkoxy radical is unsubstituted or is substituted by halogen, phenyl, lower alkoxy or a heterocyclic radical selected from piperidinyl, pyrrolidinyl, tetrahydropyranyl, tetrahydrofuranyl, thiazolidinyl, thiazolyl, indolyl or 4H-1-benzopyranyl which is unsubstituted or substituted by oxo, hydroxyl, amine, lower alkyl, lower-alkoxycarbonyl and/or phenyl-lower-alkoxycarbonyl; lower alkanoyl which is unsubstituted or is substituted by one of the said unsubstituted or substituted heterocyclic radicals; arylcarbonyl or heterocyclylcarbonyl which are substituted by heterocyclyl or heterocyclyl-lower-alkyl; phenyl-lower-alkanoyl which is substituted by hydroxyl and lower alkyl; or arylsulfonyl;or the residue of an amino acid which is defined in accordance with the description (and which may be acylated on the amino nitrogen by one of the abovementioned acyl radicals);R.sub.2 and R.sub.3 are in each case cyclohexyl, cyclohexenyl, phenyl, naphthyl or tetrahydronaphthyl which are unsubstituted or substituted by lower alkyl, phenyl, cyanophenyl, phenyl-lower-alkyl, halogen, halo-lower-alkyl, cyano, hydroxyl, lower alkoxy, phenyl-lower-alkoxyl, pyridyl-lower-alkoxy, lower-alkoxy-lower-alkoxy, lower-alkoxycarbonyl-lower-alkoxy, carboxyl-lower-alkoxy, hydroxyl-lower-alkoxy, carbamoyl-lower-alkoxy, cyano-lower-alkoxy, and phenyl-lower-alkanesulfonyl which is unsubstituted or substituted by halogen;R.sub.4 is lower alkyl, cyclohexyl or phenyl; and R.sub.5 is lower alkyl; and n is 1 or 2, or salts thereof, are novel.

摘要翻译： 抗逆转录病毒化合物（其有效的，例如针对HIV）具有式I的低级烷酰基，其低级烷酰基未被取代或被卤素，苯基，低级烷氧基或选自哌啶基，吡咯烷基 四氢呋喃基，噻唑烷基，噻唑基，吲哚基或4H-1-苯并吡喃基，其未被取代或被氧代，羟基，胺，低级烷基，低级烷氧基羰基和/或苯基 - 低级 - 烷氧基羰基取代; 低级烷酰基，其未被取代或被所述未取代或取代的杂环基之一取代; 被杂环基或杂环基 - 低级烷基取代的芳基羰基或杂环基羰基; 被羟基和低级烷基取代的苯基 - 低级 - 烷酰基; 或芳基磺酰基; 或根据描述定义的氨基酸的残基（并且可以通过上述酰基之一在氨基氮上酰化）; 苯基，氰基苯基，苯基 - 低级 - 烷基，卤素，卤代低级烷基，氰基，羟基，低级烷氧基，低级烷氧基，低级烷氧基，低级烷氧基， 低级烷氧基，低级烷氧基 - 低级烷氧基，低级烷氧基 - 低级 - 烷氧基，低级烷氧基 - 低级 - 烷氧基，羧基 - 低级 - 烷氧基，羟基 - 低级 - 烷氧基，氨基甲酰基 - 低级烷氧基， 烷氧基和未被卤素取代的苯基 - 低级烷基磺酰基; R4是低级烷基，环己基或苯基; R5为低级烷基; n为1或2，或其盐为新颖的。

公开(公告)号：US5051413A

公开(公告)日：1991-09-24

申请号：US452995

申请日：1989-12-18

申请人： Christof Angst ,  Derek E. Brundish ,  John G. Dingwall ,  Graham E. Fagg ,  Hans Allgeier ,  Guido Bold ,  Rudolf Duthaler ,  Roland Heckendorn ,  Antonio Togni

发明人： Christof Angst ,  Derek E. Brundish ,  John G. Dingwall ,  Graham E. Fagg ,  Hans Allgeier ,  Guido Bold ,  Rudolf Duthaler ,  Roland Heckendorn ,  Antonio Togni

IPC分类号： C07F9/30 ,  C07F9/32 ,  C07F9/38 ,  C07F9/40 ,  C07F9/48

CPC分类号： C07F9/4825 ,  C07F9/302 ,  C07F9/3217 ,  C07F9/3826 ,  C07F9/4015

摘要： The invention relates to unsaturated amino acids of the formula I ##STR1## in which R.sup.1 represents hydroxy or etherified hydroxy, R.sup.2 represents hydrogen, alkyl, hydroxy or etherified hydroxy, R.sup.3 represents hydrogen, alkyl, haloalkyl, hydroxyalkyl, lower alkoxyalkyl, arylalkyl, lower alkenyl, halogen or aryl, R.sup.4 represents hydrogen, alkyl or aryl, R.sup.5 represents hydrogen or alkyl, R.sup.6 represents carboxy or esterified or amidated carboxy, R.sup.7 represents amino or amino substituted by alkyl or acyl, A represents unsubstituted or alkyl-substituted .alpha.,.omega.-alkylene having from 1 to 3 carbon atoms or represents a bond, and B represents methylene or a bond, with the proviso that A is other than a bond when B represents a bond, and salts thereof. They can be manufactured, for example, in accordance with the Michaelis-Arbuzov reaction and can be used as pharmacologically active substances.

摘要翻译： 本发明涉及式I（I）的不饱和氨基酸，其中R 1表示羟基或醚化羟基，R 2表示氢，烷基，羟基或醚化羟基，R 3表示氢，烷基，卤代烷基，羟基烷基，低级烷氧基烷基， 芳基烷基，低级烯基，卤素或芳基，R 4表示氢，烷基或芳基，R 5表示氢或烷基，R 6表示羧基或酯化或酰胺化羧基，R 7表示氨基或被烷基或酰基取代的氨基，A表示未取代或烷基取代 具有1至3个碳原子的α，ω-亚烷基或表示键，并且B表示亚甲基或键，条件是当B表示键时A不是键，以及其盐。 它们可以例如根据Michaelis-Arbuzov反应制造，并且可以用作药理活性物质。