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    Certain macrocyclic lactam derivatives
    1.
    发明授权
    Certain macrocyclic lactam derivatives 失效
    某些大环内酰胺衍生物

    公开(公告)号：US5426103A

    公开(公告)日：1995-06-20

    申请号：US077975

    申请日：1993-06-15

    申请人： Lawrence J. MacPherson ,  James L. Stanton

    发明人： Lawrence J. MacPherson ,  James L. Stanton

    IPC分类号： A61K31/395 ,  A61K38/00 ,  A61K38/55 ,  A61P1/00 ,  A61P1/12 ,  A61P3/00 ,  A61P5/38 ,  A61P9/00 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P25/00 ,  A61P25/04 ,  A61P27/02 ,  A61P27/06 ,  A61P27/16 ,  A61P43/00 ,  C07D225/02 ,  C07D267/00 ,  C07D285/00 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07K1/113 ,  C07K5/06 ,  C07K5/078 ,  C07K14/81 ,  C07D281/00

    CPC分类号： C07D401/12 ,  C07D225/02 ,  C07K5/06139 ,  A61K38/00

    摘要： The invention relates to macrocyclic lactam derivatives of formula I ##STR1## wherin R is hydrogen or acyl; m is an integer from 4 to 9 inclusive; n is 1 or 2; p is zero, 1 or 2; X is --CONH-- or --NHCO--; Y is S, O or CH.sub.2 ; R.sub.1 is --COOH; or R.sub.1 is ##STR2## in which R.sub.2 is hydrogen, lower alkyl, aryl-lower alkyl, amino-lower alkyl, hydroxy-lower alkyl, acyloxy-lower alkyl, lower alkoxy-lower alkyl, mercapto-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, or carboxy-lower alkyl, R.sub.3 is hydrogen or lower alkyl, and q is zero or an integer from 1 to 5 inclusive; or R.sub.1 is ##STR3## in which R.sub.4 is hydrogen, lower alkyl, lower alkoxy, hydroxy or acyloxy, and r is 1 or 2; or R.sub.1 is ##STR4## in which s is 1 or 2; or R.sub.1 is ##STR5## in which R.sub.5 and R.sub.6 independently represent hydrogen, lower alkyl, C.sub.5 - or C.sub.6 -cycloalkyl, (hydroxy-, acyloxy or lower alkoxy-) lower alkyl, carbocyclic or heterocyclic monocyclic aryl, or (hydroxy-, acyloxy- or alkoxy-) lower alkyloxy-lower alkyl; or R.sub.5 and R.sub.6 together with the nitrogen to which they are attached represent pyrrolidino, piperidino, morpholino, piperazino or N-alkylpiperazino; and macrocyclic sulfur and oxygen containing lactam ring isomers in which a CH.sub.2 group of (CH.sub.2).sub.m in formula I is is replaced by O or S, and Y represents CH.sub.2 ; and pharmaceutically acceptable prodrug esters of any above said compound with a free carboxyl group; and pharmaceutically acceptable salts of any said compounds with a free acid or basic salt forming group; pharmaceutical compositions comprising said compounds; methods for the preparation of said compounds and for the preparation of intermediates; and methods of treating disorders in mammals which are responsive to the inhibition of neutral endopeptidases by administration of said compounds to mammals in need of such treatment.

    摘要翻译： 本发明涉及式I的大环内酰胺衍生物，其中R是氢或酰基; m为4〜9的整数， n为1或2; p为零，1或2; X是-CONH-或-NHCO-; Y是S，O或CH2; R1是-COOH; 或R 1为其中R 2为氢，低级烷基，芳基 - 低级烷基，氨基 - 低级烷基，羟基 - 低级烷基，酰氧基 - 低级烷基，低级烷氧基 - 低级烷基，巯基 - 低级烷基，低级烷基 - （ 硫代，亚磺酰基或磺酰基） - 低级烷基或羧基 - 低级烷基，R 3为氢或低级烷基，q为0或1至5的整数（包括端值） 或R 1为其中R 4为氢，低级烷基，低级烷氧基，羟基或酰氧基，R为1或2; 或R1为，其中s为1或2; 或R 1为，其中R 5和R 6独立地表示氢，低级烷基，C5-或C6-环烷基，（羟基 - ，酰氧基或低级烷氧基 - ）低级烷基，碳环或杂环单环芳基，或（羟基 - ，酰氧基 - 或烷氧基 - ）低级烷氧基 - 低级烷基; 或R 5和R 6与它们所连接的氮一起代表吡咯烷基，哌啶子基，吗啉代，哌嗪子基或N-烷基哌嗪基; 和其中式I中（CH 2）m的CH 2基团被O或S替代并且Y表示CH 2的大环硫和含氧内酰胺环异构体; 和任何上述所述化合物与游离羧基的药学上可接受的前药酯; 和任何所述化合物与游离酸或碱式盐形成基团的药学上可接受的盐; 包含所述化合物的药物组合物; 制备所述化合物和制备中间体的方法; 以及通过向需要这种治疗的哺乳动物施用所述化合物来治疗哺乳动物疾病的方法，所述疾病对中性内肽酶的抑制有反应。

    Certain macrocyclic lactam derivatives
    2.
    发明授权
    Certain macrocyclic lactam derivatives 失效
    某些大环乳酸衍生物

    公开(公告)号：US5244889A

    公开(公告)日：1993-09-14

    申请号：US798684

    申请日：1991-11-26

    申请人： Lawrence J. MacPherson ,  James L. Stanton

    发明人： Lawrence J. MacPherson ,  James L. Stanton

    IPC分类号： A61K31/395 ,  A61K38/00 ,  A61K38/55 ,  A61P1/00 ,  A61P1/12 ,  A61P3/00 ,  A61P5/38 ,  A61P9/00 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P25/00 ,  A61P25/04 ,  A61P27/02 ,  A61P27/06 ,  A61P27/16 ,  A61P43/00 ,  C07D225/02 ,  C07D267/00 ,  C07D285/00 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07K1/113 ,  C07K5/06 ,  C07K5/078 ,  C07K14/81

    CPC分类号： C07D401/12 ,  C07D225/02 ,  C07K5/06139 ,  A61K38/00

    摘要： The invention relates to macrocyclic lactam derivatives of formula I ##STR1## wherein R is hydrogen or acyl; m is an integer from 4 to 9 inclusive; n is 1 or 2; p is zero, 1 or 2; X is --CONH-- or --NHCO--; Y is S, O or CH.sub.2 ; R.sub.1 is --COOH; or R.sub.1 is ##STR2## in which R.sub.2 is hydrogen, lower alkyl, aryl-lower alkyl, amino-lower alkyl, hydroxy-lower alkyl, acyloxy-lower alkyl, lower alkoxy-lower alkyl, mercapto-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, or carboxy-lower alkyl, R.sub.3 is hydrogen or lower alkyl, and q is zero or an integer from 1 to 5 inclusive; or R.sub.1 is ##STR3## in which R.sub.4 is hydrogen, lower alkyl, lower alkoxy, hydroxy or acyloxy, and r is 1 or 2; or R.sub.1 is ##STR4## in which s is 1 or 2; or R.sub.1 is ##STR5## in which R.sub.5 and R.sub.6 independently represent hydrogen, lower alkyl, C.sub.5 - or C.sub.6 -cycloalkyl, (hydroxy-, acyloxy or lower alkoxy-) lower alkyl, carbocyclic or heterocyclic monocyclic aryl, or (hydroxy-, acyloxy- or alkoxy-) lower alkyloxy-lower alkyl; or R.sub.5 and R.sub.6 together with the nitrogen to which they are attached represent pyrrolidino, piperidino, morpholino, piperazino or N-alkylpiperazino; and macrocyclic sulfur and oxygen containing lactam ring isomers in which a CH.sub.2 group of (CH.sub.2).sub.m in formula I is replaced by O or S, and Y represents CH.sub.2 ; and pharmaceutically acceptable prodrug esters of any above said compound with a free carboxyl group; and pharmaceutically acceptable salts of any said compounds with a free acid or basic salt forming group; pharmaceutical compositions comprising said compounds; methods for the preparation of said compounds and for the preparation of intermediates; and methods of treating disorders in mammals which are responsive to the inhibition of neutral endopeptidases by administration of said compounds to mammals in need of such treatment.

    Biochemical oxidation system and process
    3.
    发明授权
    Biochemical oxidation system and process 失效
    生化氧化系统及工艺

    公开(公告)号：US06299776B1

    公开(公告)日：2001-10-09

    申请号：US08996380

    申请日：1997-12-23

    申请人： John R. McWhirter ,  James L. Stanton ,  Paul M. Kubera

    发明人： John R. McWhirter ,  James L. Stanton ,  Paul M. Kubera

    IPC分类号： C02F302

    CPC分类号： C02F3/121 ,  C02F3/26 ,  C02F3/345 ,  C02F3/348 ,  C02F2103/10 ,  C02F2305/06 ,  C22B3/18 ,  C22B11/04 ,  Y02P10/234 ,  Y02W10/15 ,  Y10S423/17 ,  Y10S435/818 ,  Y10S435/822

    摘要： A biochemical oxidation system and process is disclosed for the removal of insoluble sulfides from metal ores. A liquid mixture of an ore slurry and of a liquid biochemical oxidation medium is flowed through a plurality of covered overflow tanks connected in series. The liquid mixture is continuously aerated in an aeration chamber formed in the tanks with a mixture of a purified oxygen gas and a purified carbon dioxide gas as introduced into the aeration chamber. A substantially sulfide-free liquid mixture is discharged from a last tank into a clarifier in which at least a portion of the biochemical oxidation medium is separated from the liquid mixture for recirculation into the tanks.

    摘要翻译： 公开了用于从金属矿石中除去不溶性硫化物的生物化学氧化体系和方法。 矿浆和液体生化氧化介质的液体混合物流过串联连接的多个覆盖溢流槽。 将液体混合物在形成于容器中的曝气室中，与纯化的氧气和纯化的二氧化碳气体混合进入曝气室中。 将基本上无硫化物的液体混合物从最后一个罐排放到澄清池中，在该澄清池中至少一部分生物化学氧化介质与液体混合物分离以再循环进入罐中。

    Certain benzopyran and benzothiopyran derivatives
    6.
    发明授权
    Certain benzopyran and benzothiopyran derivatives 失效

    公开(公告)号：US5155130A

    公开(公告)日：1992-10-13

    申请号：US595153

    申请日：1990-10-10

    申请人： James L. Stanton ,  Yoshitaka Satoh ,  Alan J. Hutchison

    发明人： James L. Stanton ,  Yoshitaka Satoh ,  Alan J. Hutchison

    IPC分类号： C07D311/58 ,  C07D335/06

    CPC分类号： C07D335/06 ,  C07D311/58

    摘要： The invention relates to the compounds of the formula ##STR1## wherein each R independently represents hydrogen, lower alkyl, halogen, trifluoromethyl, lower alkoxy, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryloxy, carbocyclic or heterocyclic aryl-lower alkyloxy, carbocyclic or heterocyclic aryl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyloxy, or C.sub.3 -C.sub.7 -cycloalkyloxy; R.sub.1 represents hydrogen, lower alkyl or carbocyclic aryl; R.sub.2 represents hydrogen or lower alkyl; Y represents oxygen (O), sulfur (S), sulfinyl or sulfonyl; n represents 1, 2 or 3; A represents a direct bond or lower alkylene; Z represents ##STR2## wherein R.sub.3 represents hydrogen or acyl; R.sub.4 represents lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryl-lower alkyl, or C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl; or Z represents ##STR3## wherein X represents oxygen or sulfur, R.sub.3 represents hydrogen, acyl, lower alkoxycarbonyl, aminocarbonyl, mono- or di-lower alkylaminocarbonyl, lower alkenylaminocarbonyl, lower alkynylaminocarbonyl, carbocyclic or heterocyclic aryl-lower alkylaminocarbonyl, carbocyclic or heterocyclic arylamino-carbonyl; C.sub.3 -C.sub.7 -cycloalkylaminocarbonyl, or C.sub.3 -C.sub.7 -cycloalkyl-lower alkylaminocarbonyl; R.sub.5 represents lower alkyl, lower alkoxycarbonyl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, amino, mono- or di-lower alkylamino, lower alkenylamino, lower alkynylamino, carbocyclic or heterocyclic aryl-lower alkylamino, carbocyclic or heterocyclic arylamino, C.sub.3 -C.sub.7 -cycloalkylamino, C.sub.3 -C.sub.7 -cycloalkyl-lower alkylamino, lower alkoxycarbonyl-lower alkylamino, or lower alkoxy; R.sub.6 and R.sub.7 independently represent hydrogen or lower alkyl; and pharmaceutically acceptable salts thereof; which are useful as 5-lipoxygenase inhibitors.

    Hetero-benzazepine derivatives and their pharmaceutical use
    8.
    发明授权
    Hetero-benzazepine derivatives and their pharmaceutical use 失效
    异苯并吖嗪衍生物及其药物用途

    公开(公告)号：US4477464A

    公开(公告)日：1984-10-16

    申请号：US465694

    申请日：1983-02-10

    申请人： Joel Slade ,  James L. Stanton

    发明人： Joel Slade ,  James L. Stanton

    IPC分类号： C07D243/12 ,  C07D267/14 ,  C07D281/10 ,  A61K31/55 ,  C07D513/04

    CPC分类号： C07D281/10 ,  C07D243/12 ,  C07D267/14

    摘要： Disclosed are variously substituted 3-(carboxymethylamino)-(1,5-benzothiazepin-4-one, 1,5-benzoxazepin-4-one and 1,5-benzodiazepin-4-one)-5-alkanoic acids and derivatives as angiotensin-converting enzyme inhibitors and antihypertensive agents. Their synthesis, pharmaceutical compositions thereof, and methods of threatment utilizing such compounds are included.

    摘要翻译： 公开了各种取代的3-（羧甲基氨基） - （1,5-苯并硫氮杂-4-酮，1,5-苯并氧杂吖庚因-4-酮和1,5-苯并二氮杂-4-酮）-5-链烷酸及其衍生物作为血管紧张素 转化酶抑制剂和抗高血压药。 包括它们的合成，其药物组合物和利用这些化合物的威胁方法。

    Antihypertensive 5-amino-4-hydroxyvaleryl derivatives substituted by sulphur-containing groups
    9.
    发明授权
    Antihypertensive 5-amino-4-hydroxyvaleryl derivatives substituted by sulphur-containing groups 失效
    由含硫基取代的抗高血压5-氨基-4-羟基戊酰基衍生物

    公开(公告)号：US4758584A

    公开(公告)日：1988-07-19

    申请号：US011183

    申请日：1987-02-05

    申请人： Peter Buhlmayer ,  James L. Stanton ,  Walter Fuhrer ,  Richard Goschke ,  Vittorio Rasetti ,  Heinrich Rueger

    发明人： Peter Buhlmayer ,  James L. Stanton ,  Walter Fuhrer ,  Richard Goschke ,  Vittorio Rasetti ,  Heinrich Rueger

    IPC分类号： C07D233/54 ,  C07D401/12 ,  C07D417/12 ,  C07K5/02 ,  A61K37/64 ,  C07K5/08

    CPC分类号： C07D233/64 ,  C07D401/12 ,  C07D417/12 ,  C07K5/0227 ,  Y10S530/86

    摘要： Compounds of the formula ##STR1## in which R.sub.1 represents acyl substituted by a thio, sulphinyl or sulphonyl group, A represents an optionally N-alkylated .alpha.-amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, tricycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, tricycloalkyl, tricycloalkyl-lower alkyl, aryl, aryl-lower alkyl, optionally substituted carbamoyl, optionally substituted amino, optionally substituted hydroxy, optionally substituted mercapto, sulphinyl or sulphonyl, and R.sub.6 represents substituted amino, and salts of such compounds having salt-forming groups, inhibit the blood pressure-increasing action of the enzyme renin and can be used as anti-hypertensives.

    摘要翻译： 式（I）的化合物，其中R 1表示被硫代，亚磺酰基或磺酰基取代的酰基，A表示任选N-烷基化的α-氨基酸残基，其N-末端与R1和C-末端键合 基团-NR 2 - ，R 2表示氢或低级烷基，R 3表示氢，低级烷基，任选醚化或酯化的羟基 - 低级烷基，环烷基，环烷基 - 低级烷基，双环烷基 - 低级烷基，三环烷基 - 低级烷基，芳基或芳基 - 低级烷基，R4代表羟基或醚化或酯化的羟基，R5代表低级烷基，任选醚化或酯化羟基 - 低级烷基，环烷基，环烷基 - 低级烷基，双环烷基，双环烷基 - 低级烷基，三环烷基，三环烷基 - 低级烷基，芳基，芳基 - 低级烷基，任选取代的氨基甲酰基，任选取代的氨基，任选取代的羟基，任选取代的巯基，亚磺酰基或磺酰基，R 6代表取代的氨基， 具有盐形成基团，抑制了肾素素的增压作用，可用作抗高血压药。

    Gamma-r-glutamoyl derivatives
    10.
    发明授权
    Gamma-r-glutamoyl derivatives 失效
    γ-氨基磺酰衍生物

    公开(公告)号：US4678800A

    公开(公告)日：1987-07-07

    申请号：US621302

    申请日：1984-06-15

    申请人： James L. Stanton ,  Gary M. Ksander

    发明人： James L. Stanton ,  Gary M. Ksander

    IPC分类号： C07D209/42 ,  C07D209/12 ,  A61K31/40

    CPC分类号： C07D209/42

    摘要： A compound of the formula ##STR1## wherein R.sub.1 and R.sub.6 independently represent hydroxy, C.sub.1 -C.sub.4 -alkoxy, substituted C.sub.1 -C.sub.4 - alkoxy, amino, or substituted amino, R.sub.2 represents hydrogen, C.sub.1 -C.sub.4 -alkyl, or C.sub.2 -C.sub.4 -alkenyl, R.sub.3 represents cyclo-C.sub.3 -C.sub.6 -alkyl, phenyl, phenyl substituted by C.sub.1 -C.sub.4 -alkyl, halogen, nitro, or C.sub.1 -C.sub.4 -alkoxy, or cyclo-C.sub.3 -C.sub.6 -alkyl fused with benzene, or wherein R.sub.2 and R.sub.3 are connected and together with the adjacent --CH-group and the adjacent N-atom form a saturated or partially saturated, monocyclic, five- or six-membered heterocyclic group or form a saturated or partially saturated, bicyclic heterocyclic group containing five or six atoms per ring, R.sub.4 represents hydrogen or C.sub.1 -C.sub.4 -alkyl, and R.sub.5 represents an acyl group, are useful as antihypertensive and cardioactive agents. The invention also relates to processes for preparing the compounds of the formula I and to pharmaceutical compositions.

    摘要翻译： 式（I）的化合物，其中R 1和R 6独立地表示羟基，C 1 -C 4 - 烷氧基，取代的C 1 -C 4 - 烷氧基，氨基或取代的氨基，R 2表示氢，C 1 -C 4烷基或C 2 C 4 - 烯基，R 3表示环-C 3 -C 6烷基，苯基，被C 1 -C 4 - 烷基，卤素，硝基或C 1 -C 4 - 烷氧基取代的苯基，或与苯稠合的环-C 3 -C 6烷基，或 其中R2和R3与相邻的-CH-基团和相邻的N-原子一起形成饱和或部分饱和的单环，五元或六元杂环基团或形成饱和或部分饱和的双环杂环基团，其含有 每个环五个或六个原子，R4代表氢或C1-C4-烷基，R5代表酰基，可用作抗高血压和心脏活性剂。 本发明还涉及制备式I化合物和药物组合物的方法。