公开(公告)号：US5726192A

公开(公告)日：1998-03-10

申请号：US464728

申请日：1995-08-08

申请人： William Edward Bondinell ,  James Francis Callahan ,  William Francis Huffman ,  Richard McCulloch Keenan ,  Brian Walter Metcalf ,  James Samanen ,  Tobias Oregon Yellin

发明人： William Edward Bondinell ,  James Francis Callahan ,  William Francis Huffman ,  Richard McCulloch Keenan ,  Brian Walter Metcalf ,  James Samanen ,  Tobias Oregon Yellin

IPC分类号： A61K31/195 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/425 ,  A61K31/428 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4418 ,  A61K38/00 ,  A61P7/02 ,  A61P9/00 ,  C07D213/56 ,  C07D213/73 ,  C07D213/75 ,  C07D235/30 ,  C07D277/64 ,  C07D417/12 ,  C07K5/02 ,  C07K5/087 ,  C07K5/09 ,  C07K5/11 ,  C07D213/02

CPC分类号： C07D213/73 ,  C07D213/56 ,  C07D235/30 ,  C07D277/64 ,  C07D417/12 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/0812 ,  C07K5/0815 ,  C07K5/0817 ,  A61K38/00

摘要： This invention relates to compounds of the formula: W--Z--(CR'R.sup.10).sub.r --U--(CR'.sub.2).sub.s --V--A wherein: ##STR1## A is W is R'R"N--; Z is Het; U and V independently are absent or present as CO, CR'.sub.2, C(.dbd.CR'.sub.2), S(O).sub.r, O, NR', CR'OR', CR'(OR")CR'.sub.2, CR'.sub.2 CR'(OR"), C(O)CR'.sub.2, CR'.sub.2 C(O), CONR', NR'CO, OC(O), C(O)O, C(S)O, OC(S), C(S)NR', NR'C(S), S(O).sub.r NR', NR'S(O).sub.r, N.dbd.N, NR'NR', NR'CR'.sub.2, NR'CR'.sub.2, CR'.sub.2 O, OCR'.sub.2, .sup.c.tbd.c, CR'.dbd.CR', or CR'(NR'R")C(O); each r independently is 0 to 3; s is 0 to 2; each R' independently is H, C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-4 alkyl, or Ar--C.sub.0-4 alkyl; each R" independently is R', --C(O)R', or --C(O)OR.sup.15 ; R.sup.10 is as H, C.sub.1-4 alkyl, or --NR'R'; each R.sup.15 independently is C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-4 alkyl, or AR--C.sub.0-4 alkyl; R.sup.2 is present once or twice as C.sub.1-4 alkyl, J--CO.sub.2 R', CONR', SR', NR'R", C.sub.1-4 alkoxy, hydroxy, CN, CF.sub.3, halo, or ##STR2## with the proviso that at least one R.sup.2 is J--CO.sub.2 R; J is a single bond, --OCR'.sub.2 --, --NR'CR'.sub.2 --, CR'.sub.2 --CR'.sub.2 --, --CR'.sub.2 --, --CR'.dbd.CR', or --C(O)NR'CR'.sub.2 --; and each R.sup.14 independently is C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-4 alkyl, Ar--C.sub.0-4 alkyl, C(O)R', CN, NO.sub.2, SO.sub.2 R', or C(O)OR.sup.15 ; or a pharmaceutically acceptable salt thereof.

摘要翻译： PCT No.PCT / US93 / 12530 Sec。 371日期：1995年8月8日 102（e）日期1995年8月8日PCT提交1993年12月22日PCT公布。 第WO94 / 14775号​​公报 日期：1994年7月7日本发明涉及下式的化合物：WZ-（CR'R10）rU-（CR'2）sV-A其中：不存在或作为CO，CR'2，C（= CR'2），S（O）r，O，NR'，CR'OR'，CR'（OR“）CR'2，CR'2CR'（OR”），C（O）CR'2， CR（O），CONR'，NR'CO，OC（O），C（O）O，C（S）O，OC（S），C（S）NR'，NR'C（S） S（O）rNR'，NR'（O）r，N = N，NR'NR'，NR'CR'2，NR'CR'2，CR'2O，OCR'2，c 3BOND c，CR'= CR '或CR'（NR'R“）C（O）; 每个r独立为0至3; s为0〜2; 每个R'独立地为H，C 1-4烷基，C 3-7环烷基-C 0-4烷基或Ar-C 0-4烷基; 每个R“独立地是R'，-C（O）R'或-C（O）OR 15; R 10为H，C 1-4烷基或-NR'R'; 每个R 15独立地为C 1-4烷基，C 3-7环烷基-C 0-4烷基或AR-C 0-4烷基; R2存在一次或两次作为C 1-4烷基，J-CO 2 R'，CONR'，SR'，NR'R“，C 1-4烷氧基，羟基，CN，CF 3，卤素或”IMAGE“，条件是至少 一个R2是J-CO2R; J是单键，-OCR'2-，-NR'CR'2-，CR'2-CR'2-，-CR'2-，-CR'= CR'或-C（O）NR' CR'2-; 并且每个R 14独立地为C 1-4烷基，C 3-7环烷基-C 0-4烷基，Ar-C 0-4烷基，C（O）R'，CN，NO 2，SO 2 R'或C（O）OR 15; 或其药学上可接受的盐。

公开(公告)号：US6028087A

公开(公告)日：2000-02-22

申请号：US10238

申请日：1998-01-21

申请人： William Edward Bondinell ,  James Francis Callahan ,  William Francis Huffman ,  Richard McCulloch Keenan ,  Brian Walter Metcalf ,  James Samanen ,  Tobias Oregon Yellin

发明人： William Edward Bondinell ,  James Francis Callahan ,  William Francis Huffman ,  Richard McCulloch Keenan ,  Brian Walter Metcalf ,  James Samanen ,  Tobias Oregon Yellin

IPC分类号： A61K38/00 ,  C07D213/56 ,  C07D213/73 ,  C07D417/12 ,  C07K5/083 ,  C07K5/09 ,  A61K31/44

CPC分类号： C07D213/73 ,  C07D213/56 ,  C07D417/12 ,  C07K5/0806 ,  C07K5/0815 ,  C07K5/0817 ,  A61K38/00

摘要： Compounds of the formula (I):W--Z--(CR'R.sup.10).sub.r --U--(CR'.sub.2).sub.s --V--A (I)wherein:A is ##STR1## W is .sup.N ; Z is (CH.sub.2).sub.1-2 ;U and V independently are present as CO, CR'.sub.2, C(.dbd.CR'.sub.2), S(O).sub.r, O, NR', CR'OR', CR'(OR")CR'.sub.2, CR'.sub.2 CR'(OR"), C(O)CR'.sub.2, CR'.sub.2 C(O), CONR', NR'CO, OC(O), C(O)O, C(S)O, OC(S), C(S)NR', NR'C(S), S(O).sub.r NR', NR'S(O).sub.r, N.dbd.N, NR'NR', NR'CR'.sub.2, NR'CR'.sub.2, CR'.sub.2 O, OCR'.sub.2, C.tbd.C, CR'.dbd.CR', or CR'(NR'R")C(O);each r independently is 0 to 3;s is 0 to 2;each R' independently is H, C.sub.1-4 alkyl, C.sub.3-7 cycloalky-C.sub.0-4 alkyl, or Ar-C.sub.0-4 alkyl;each R" independently is R', --C(O)R', or --C(O)OR.sup.15 ;R.sup.10 is H, C.sub.1-4 alkyl, or --NR'R';each R.sup.15 independently is C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-4 alkyl, or Ar-C.sub.0-4 alkyl;R.sup.2 is present once or twice as C.sub.1-4 alkyl, J--CO.sub.2 R', CONR', SR', NR'R", C .sub.1-4 alkoxy, hydroxy, CN, CF.sub.3, halo, or ##STR2## with the proviso that at least one R.sup.2 is J--CO.sub.2 R; and J is a single bond, --OCR'.sub.2 --, --NR'CR'.sub.2 --, CR'.sub.2 --CR'.sub.2 --, --CR'.sub.2 --, --CR'.dbd.CR', or --C(O)NR'CR'.sub.2 --;each R.sup.14 independently is C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-4 alkyl, Ar-C.sub.0-4 alkyl, C(O)R', CN, NO.sub.2, SO.sub.2 R', or C(O)OR.sup.15 ;or a pharmaceutically acceptable salt thereof, are effective for inhibiting platelet aggregation.

摘要翻译： 式（I）的化合物：W-Z-（CR'R10）r-U-（CR'2）s-V-A（I）其中：A是W是+ E，crc N + EE; Z是（CH 2）1-2; U和V独立地作为CO，CR'2，C（= CR'2），S（O）r，O，NR'，CR'OR'，CR'（OR“）CR'2，CR' （OR），C（O）CR'2，CR'2C（O），CONR'，NR'CO，OC（O），C（O）O，C（O） ），C（S）NR'，NR'C（S），S（O）rNR'，NR'S（O）r，N = N，NR'NR'，NR'CR'2，NR'CR'2， CR'2O，OCR'2，C 3BOND C，CR'= CR'或CR'（NR'R“）C（O）; 每个r独立为0至3; s为0〜2; 每个R'独立地为H，C 1-4烷基，C 3-7环烷基-C 0-4烷基或Ar-C 0-4烷基; 每个R“独立地是R'，-C（O）R'或-C（O）OR 15; R 10是H，C 1-4烷基或-NR'R'; 每个R 15独立地为C 1-4烷基，C 3-7环烷基-C 0-4烷基或Ar-C 0-4烷基; R 2存在一次或两次作为C 1-4烷基，J-CO 2 R'，CONR'，SR'，NR'R“，C 1-4烷氧基，羟基，CN，CF 3，卤素，或条件是至少一个R 2 是J-CO2R; 并且J是单键，-OCR'2 - ，-NR'CR'2 - ，CR'2-CR'2，-CR'2-，-CR'= CR'或-C（O）NR 'CR'2-; 每个R 14独立地是C 1-4烷基，C 3-7环烷基-C 0-4烷基，Ar-C 0-4烷基，C（O）R'，CN，NO 2，SO 2 R'或C（O）OR 15; 或其药学上可接受的盐对抑制血小板聚集是有效的。

公开(公告)号：US5665753A

公开(公告)日：1997-09-09

申请号：US702528

申请日：1996-09-03

申请人： James Simpson Frazee ,  John Gerald Gleason ,  Brian Walter Metcalf

发明人： James Simpson Frazee ,  John Gerald Gleason ,  Brian Walter Metcalf

IPC分类号： C07D233/54 ,  C07D233/68 ,  A01N43/52 ,  A61K31/415 ,  C07D233/64 ,  C07D235/04

CPC分类号： C07D233/64 ,  C07D233/68

摘要： The present invention relates to a series of novel imidazole substituted hydroxamic acid derivatives, and compositions useful thereof as inhibitors of matrix degrading metalloproteinases, in particular collagenase.

摘要翻译： PCT No.PCT / US95 / 02606 Sec。 371日期1996年9月3日 102（e）日期1996年9月3日PCT 1995年3月3日PCT PCT。 公开号WO95 / 23790 日期1995年9月8日本发明涉及一系列新的咪唑取代的异羟肟酸衍生物，以及作为基质降解金属蛋白酶抑制剂，特别是胶原酶的组合物。

公开(公告)号：US4039549A

公开(公告)日：1977-08-02

申请号：US664991

申请日：1976-03-08

申请人： Brian Walter Metcalf ,  Michel Jung

发明人： Brian Walter Metcalf ,  Michel Jung

IPC分类号： C07C237/00 ,  C07D211/76 ,  C07C103/183 ,  C07C103/28 ,  C07D207/26

CPC分类号： C07C237/00

摘要： Novel compounds of the following general formula are useful pharmacologic agents: ##STR1## R is selected from hydrogen, alkylcarbonyl wherein the alkyl moiety contains from 1 to 4 carbon atoms, alkoxycarbonyl wherein the alkoxy moiety contains from 1 to 4 carbon atoms and may be a straight or branched, and ##STR2## wherein R.sub.10 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl and .rho.-hydroxybenzyl; R.sub.2 is selected from hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, a lower alkylamino group wherein the alkyl moiety contains from 1 to 4 carbon atoms, and ##STR3## wherein R.sub.4 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl, and .rho.-hydroxybenzyl; R.sub.3 is selected from hydrogen, chlorine, bromine, and iodine; [A] is selected from ##STR4## AND --CH=CH-- wherein R.sub.1 is selected from hydrogen, lower alkyl of from 1 to 4 carbon atoms, phenyl and substituted phenyl wherein the substituents on the substituted phenyl may be attached at the ortho, meta or para positions of the phenyl ring and are selected from halogen, lower alkoxy of from 1 to 4 carbon atoms, and lower alkyl of from 1 to 4 carbon atoms; n is an integer of from 1 to 5; and the lactams of said compounds wherein [A] represents ##STR5## R and R.sub.1 represent hydrogen and n is the integer 2 or 3 and pharmaceutically acceptable salts and individual optical isomers thereof.

摘要翻译： 以下通式的新型化合物是有用的药理学药剂：R选自氢，烷基部分含有1至4个碳原子的烷基羰基，其中烷氧基部分含有1至4个碳原子，可以是 直链或支链，和其中R10选自氢，1-4个碳原子的直链或支链低级烷基，苄基和对羟基苄基; R2选自羟基，1至8个碳原子的直链或支链烷氧基，其中烷基部分含有1至4个碳原子的低级烷基氨基，和其中R 4选自氢，直链或 具有1至4个碳原子的支链低级烷基，苄基和rho-羟基苄基; R3选自氢，氯，溴和碘; [A]选自和-CH = CH-，其中R 1选自氢，1至4个碳原子的低级烷基，苯基和取代的苯基，其中取代的苯基上的取代基可以在邻位， 苯环的间位或对位，并且选自卤素，1至4个碳原子的低级烷氧基和1至4个碳原子的低级烷基; n为1〜5的整数， 和所述化合物的内酰胺，其中[A]表示R并且R 1表示氢，n是整数2或3及其药学上可接受的盐和单独的光学异构体。

公开(公告)号：US4100349A

公开(公告)日：1978-07-11

申请号：US812266

申请日：1977-07-01

申请人： Brian Walter Metcalf ,  Michel Jung

发明人： Brian Walter Metcalf ,  Michel Jung

IPC分类号： C07D233/54 ,  C07D233/64 ,  C07D233/68 ,  C07D233/88

CPC分类号： C07D233/64 ,  C07D233/68 ,  C07D233/88 ,  Y10S514/826 ,  Y10S514/849

摘要： Novel acetylenic derivatives of amines of the following general structure ##STR1## wherein R is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched or ##STR2## wherein R.sub.3 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; each of R.sub.1 and R.sub.2 is hydrogen, halogen selected from fluorine, chlorine, bromine and iodine or a straight or branched lower alkyl group of from 1 to 4 carbon atoms and may be the same or different with the proviso that when both R.sub.1 and R.sub.2 are halogen R.sub.1 and R.sub.2 are the same; and pharmaceutically acceptable salts and individual optical isomers thereof.

摘要翻译： 具有以下通用结构的胺的新型炔属衍生物，其中R是氢，烷基部分具有1至4个碳原子并且是直链或支链的烷氧基羰基，其中烷氧基部分具有1至4个碳原子，且为 直链或支链或者其中R3是氢，1-4个碳原子的直链或支链低级烷基，苄基或对羟基苄基; R 1和R 2各自为氢，选自氟，氯，溴和碘的卤素或具有1至4个碳原子的直链或支链低级烷基，并且可以相同或不同，条件是当R 1和R 2均为 卤素R1和R2相同; 及其药学上可接受的盐和单独的光学异构体。

公开(公告)号：US3960927A

公开(公告)日：1976-06-01

申请号：US559544

申请日：1975-03-18

申请人： Brian Walter Metcalf ,  Michel Jung

发明人： Brian Walter Metcalf ,  Michel Jung

IPC分类号： A61K31/16 ,  A61K31/195 ,  A61K31/21 ,  A61P25/00 ,  C07C67/00 ,  C07C227/00 ,  C07C229/30 ,  C07C231/00 ,  C07C233/47 ,  C07C237/00 ,  C07C237/12 ,  C07C237/16 ,  C07C237/20 ,  C07C237/22 ,  C07C271/22 ,  C07D207/267 ,  C07D211/76 ,  C07C101/00 ,  C07C101/28

CPC分类号： C07C237/00 ,  Y10S514/909

摘要： Novel compounds of the following general formula are useful pharmacologic agents: ##EQU1## R is selected from hydrogen, alkylcarbonyl wherein the alkyl moiety contains from 1 to 4 carbon atoms, alkoxycarbonyl wherein the alkoxy moiety contains from 1 to 4 carbon atoms and may be straight or branched, and ##EQU2## wherein R.sub.10 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl and p-hydroxybenzyl; R.sub.2 is selected from hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, a lower alkylamino group wherein the alkyl moiety contains from 1 to 4 carbon atoms, and ##EQU3## wherein R.sub.4 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl, and p-hydroxybenzyl; R.sub.3 is selected from hydrogen, chlorine, bromine, and iodine; [A] is selected from ##EQU4## AND --CH=CH-- wherein R.sub.1 is selected from hydrogen, lower alkyl of from 1 to 4 carbon atoms, phenyl and substituted phenyl wherein the substituents on the substituted phenyl may be attached at the ortho, meta or para positions of the phenyl ring and are selected from halogen, lower alkoxy of from 1 to 4 carbon atoms, and lower alkyl of from 1 to 4 carbon atoms; n is an integer of from 1 to 5; and the lactams of said compounds wherein [A] represents ##EQU5## R and R.sub.1 represent hydrogen and n is the integer 2 or 3 and pharmaceutically acceptable salts and individual optical isomers thereof.

摘要翻译： 以下通式的新型化合物是有用的药物：O PARALLEL R3-CH = CH-CH- [A] -C-R2 | NHRR选自氢，烷基羰基，其中烷基部分含有1至4个碳原子， 烷氧基羰基，其中烷氧基部分含有1至4个碳原子并且可以是直链或支链的，并且其中R 10选自氢，1-4个碳原子的直链或支链低级烷基， 原子，苄基和对羟基苄基; R2选自羟基，1至8个碳原子的直链或支链烷氧基，其中烷基部分含有1至4个碳原子的低级烷基氨基，以及-NH-CH-COOH | R4，其中R4选自 氢，1至4个碳原子的直链或支链低级烷基，苄基和对羟基苄基; R3选自氢，氯，溴和碘; [A]选自R 1 |（-CH-）n和-CH = CH-，其中R 1选自氢，1至4个碳原子的低级烷基，苯基和取代的苯基，其中取代的苯基上的取代基可以是 连接在苯环的邻位，间位或对位，并且选自卤素，1至4个碳原子的低级烷氧基和1至4个碳原子的低级烷基; n为1〜5的整数， 和所述化合物的内酰胺，其中[A]表示R 1 |（-CH-）n; R和R 1表示氢，n是整数2或3及其药学上可接受的盐和单独的光学异构体。

公开(公告)号：US3959356A

公开(公告)日：1976-05-25

申请号：US559547

申请日：1975-03-18

申请人： Brian Walter Metcalf ,  Michel Jung

发明人： Brian Walter Metcalf ,  Michel Jung

IPC分类号： A61K31/16 ,  A61K31/195 ,  A61K31/21 ,  A61K31/215 ,  A61K31/22 ,  C07C67/00 ,  C07C229/30 ,  C07C231/00 ,  C07C231/12 ,  C07C233/47 ,  C07C237/12 ,  C07C237/16 ,  C07C237/20 ,  C07C237/22 ,  C07C239/00 ,  C07C271/22 ,  C07D207/267 ,  C07D211/76 ,  C07F7/08 ,  C07C101/00 ,  C07C101/28

CPC分类号： C07F7/0818 ,  Y02P20/55 ,  Y10S514/96 ,  Y10S514/962

摘要： Novel compounds of the following general formula are useful pharmacologic agents: ##EQU1## R is selected from hydrogen, alkylcarbonyl wherein the alkyl moiety contains from 1 to 4 carbon atoms, alkoxy-carbonyl wherein the alkoxy moiety contains from 1 to 4 carbon atoms and may be straight or branched, and ##EQU2## wherein R.sub.10 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl and p-hydroxybenzyl; R.sub.2 is selected from hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, a lower alkylamino group wherein the alkyl moiety contains from 1 to 4 carbon atoms, and ##EQU3## wherein R.sub.4 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl, and p-hydroxybenzyl; [A] is selected from ##EQU4## AND --CH=CH-- wherein R.sub.1 is selected from hydrogen, lower alkyl of from 1 to 4 carbon atoms, phenyl and substituted phenyl wherein the substituents on the substituted phenyl may be attached at the ortho, meta or para positions of the phenyl ring and are selected from halogen, lower alkoxy of from 1 to 4 carbon atoms, and lower alkyl of from 1 to 4 carbon atoms; n is an integer of from 1 to 5; and the lactams of said compounds wherein [A] represents ##EQU5## R and R.sub.1 represent hydrogen and n is the integer 2 or 3; and pharmaceutically acceptable salts and individual optical isomers thereof.

摘要翻译： 以下通式的新化合物是有用的药理学药剂：O PARALLEL HC 3BOND C-CH- [A] -C-R2 | NHR R选自氢，烷基部分含有1至4个碳原子的烷基羰基，烷氧基 - 羰基，其中烷氧基部分含有1至4个碳原子并且可以是直链或支链的，并且其中R 10选自氢，1-4个碳原子的直链或支链低级烷基， 原子，苄基和对羟基苄基; R2选自羟基，1至8个碳原子的直链或支链烷氧基，其中烷基部分含有1至4个碳原子的低级烷基氨基，以及-NH-CH-COOH | R4，其中R4选自 氢，1至4个碳原子的直链或支链低级烷基，苄基和对羟基苄基; [A]选自R 1 |（-CH-）n和-CH = CH-，其中R 1选自氢，1至4个碳原子的低级烷基，苯基和取代的苯基，其中取代的苯基上的取代基可以是 连接在苯环的邻位，间位或对位，并且选自卤素，1至4个碳原子的低级烷氧基和1至4个碳原子的低级烷基; n为1〜5的整数， 和所述化合物的内酰胺，其中[A]表示R 1 |（-CH-）n R，R 1表示氢，n为整数2或3; 及其药学上可接受的盐和单独的光学异构体。

公开(公告)号：US3946060A

公开(公告)日：1976-03-23

申请号：US559545

申请日：1975-03-18

申请人： Brian Walter Metcalf ,  Michel Jung

发明人： Brian Walter Metcalf ,  Michel Jung

IPC分类号： C07F7/10 ,  C07F7/08

CPC分类号： C07F7/0818

摘要： Novel compounds of the following general formula are useful pharmacologic agents and are useful as intermediates for the preparation of pharmacologically useful compounds. ##EQU1## wherein R.sub.1 is selected from a lower alkyl group having from 1 to 4 carbon atoms, R.sub.2 is selected from hydrogen and phenyl; and R.sub.3 is selected from phenyl and trialkylmethyl; and acid addition salts thereof.

摘要翻译： 以下通式的新型化合物是有用的药理学试剂，可用作制备药理学有用化合物的中间体。 （R1）3-Si-C3BOND C-CH2-N = C-R2 | R3其中R1选自具有1至4个碳原子的低级烷基，R2选自氢和苯基; 并且R 3选自苯基和三烷基甲基; 及其酸加成盐。

公开(公告)号：US4103089A

公开(公告)日：1978-07-25

申请号：US812268

申请日：1977-07-01

申请人： Brian Walter Metcalf ,  Michel Jung

发明人： Brian Walter Metcalf ,  Michel Jung

IPC分类号： C07D233/54 ,  C07D233/64 ,  C07D233/68 ,  C07D233/88

CPC分类号： C07D233/64 ,  C07D233/68 ,  C07D233/88

摘要： Novel acetylene and vinyl derivatives of amino acids of the following general structure ##STR1## wherein R is --CH.dbd.CH.sub.2 or C.tbd.CH; R.sub.1 is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.11 R.sub.12 wherein each of R.sub.11 and R.sub.12 is hydrogen or a straight or branched lower alkyl group of from 1 to 4 carbon atoms, ##STR2## wherein R.sub.5 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.2 is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched or ##STR3## wherein R.sub.6 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; each of R.sub.3 and R.sub.4 is hydrogen, halogen selected from fluorine, chlorine, bromine and iodine, or a straight or branched lower alkyl of from 1 to 4 carbon atoms and may be the same or different with the proviso that when both R.sub.3 and R.sub.4 are halogen R.sub.3 and R.sub.4 are the same; with the proviso that when R is --CH.dbd.CH.sub.2, R.sub.1 is hydroxy and R.sub.2 is hydrogen; and pharmaceutically acceptable salts thereof.

摘要翻译： 新颖的乙炔和乙烯基衍生物的氨基酸具有以下通用结构其中R是-CH = CH 2或C 3 CH 3; R1是羟基，1至8个碳原子的直链或支链烷氧基，-NR11R12，其中R11和R12各自为氢或1至4个碳原子的直链或支链低级烷基，其中R5为 氢，1至4个碳原子的直链或支链低级烷基，苄基或对羟基苄基; R2是氢，烷基羰基，其中烷基部分具有1至4个碳原子，并且是直链或支链的烷氧基羰基，其中烷氧基部分具有1至4个碳原子并且是直链或支链或者其中R6是氢，直链 或具有1至4个碳原子的支链低级烷基，苄基或对羟基苄基; R 3和R 4各自为氢，选自氟，氯，溴和碘的卤素，或具有1至4个碳原子的直链或支链低级烷基，并且可以相同或不同，条件是当R 3和R 4均为 卤素R3和R4相同; 条件是当R为-CH = CH 2时，R 1为羟基，R 2为氢; 及其药学上可接受的盐。

公开(公告)号：US4088667A

公开(公告)日：1978-05-09

申请号：US812065

申请日：1977-07-01

申请人： Patrick J. Casara ,  Michel Jung ,  Brian Walter Metcalf

发明人： Patrick J. Casara ,  Michel Jung ,  Brian Walter Metcalf

IPC分类号： A61K31/695 ,  A61P31/04 ,  C07D233/54 ,  C07F7/08 ,  C07F7/12 ,  C07F7/10

CPC分类号： C07D233/64 ,  C07F7/0818

摘要： Novel compounds of the formula ##STR1## wherein each of R and R.sub.1 is a lower alkyl group of from 1 to 4 carbon atoms, R.sub.3 is an alkyl group and a process employing said compounds.

摘要翻译： 新颖的式（IMAGE）化合物，其中R 1和R 1各自为1至4个碳原子的低级烷基，R 3为烷基和使用所述化合物的方法。