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    Carboxyalkyl derivatives useful as inhibitors of enkephalinase and ace
    3.
    发明授权
    Carboxyalkyl derivatives useful as inhibitors of enkephalinase and ace 失效
    可用作脑啡肽酶抑制剂的羧甲基烷基衍生物

    公开(公告)号：US5472959A

    公开(公告)日：1995-12-05

    申请号：US348778

    申请日：1994-12-01

    申请人： Alan M. Warshawsky ,  Gary A. Flynn

    发明人： Alan M. Warshawsky ,  Gary A. Flynn

    IPC分类号： A61K31/535 ,  A61K31/54 ,  A61K31/55 ,  A61K38/00 ,  A61P7/10 ,  A61P9/00 ,  A61P9/12 ,  A61P25/04 ,  A61P25/28 ,  A61P43/00 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D507/00 ,  C07D513/04 ,  C07K5/078

    CPC分类号： C07K5/06139 ,  A61K38/00

    摘要： The invention relates to compounds of the formula ##STR1## wherein B.sub.1 and B.sub.2 are each independently hydrogen; hydroxy; --OR.sub.2 wherein R.sub.2 is a C.sub.1 -C.sub.4 alkyl or an Ar--Y group wherein Ar is aryl and Y is a hydrogen or C.sub.1 -C.sub.4 alkyl; or, where B.sub.1 and B.sub.2 are attached to adjacent carbon atoms, B.sub.1 and B.sub.2 can be taken together with said adjacent carbons to form a benzene ring or methylenedioxy;A is a bond, methylene or oxygen, sulfur, NR.sub.4 or NCOR.sub.5 wherein R.sub.4 is hydrogen, a C.sub.1 -C.sub.4 alkyl or an Ar--Y-- group and R.sub.5 is --CF.sub.3, a C.sub.1 -C.sub.10 alkyl or an Ar--Y-- group; R.sub.3 is hydrogen or --CH.sub.2 OC(O)C(CH.sub.3).sub.3 ; R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl or --CH.sub.2 OC(O)--C(CH.sub.3).sub.3 ; and n is an integer 1 to 3,that are useful as inhibitors of enkephalinase and ACE.

    摘要翻译： 本发明涉及下式化合物：其中B1和B2各自独立地为氢; 羟基; -OR 2，其中R 2是C 1 -C 4烷基或Ar-Y基团，其中Ar是芳基，Y是氢或C 1 -C 4烷基; 或者其中B1和B2连接到相邻的碳原子上，可以将B1和B2与所述相邻的碳原子一起形成苯环或亚甲二氧基; A是键，亚甲基或氧，硫，NR 4或NCOR 5，其中R 4是氢，C 1 -C 4烷基或Ar-Y-基，R 5是-CF 3，C 1 -C 10烷基或Ar-Y-基团; R3是氢或-CH2OC（O）C（CH3）3; R1是氢，C1-C4烷基或-CH2OC（O）-C（CH3）3; 且n为1〜3的整数，可用作脑啡肽酶和ACE的抑制剂。

    Process for 3.beta.-aminoazetidin-2-ones
    4.
    发明授权
    Process for 3.beta.-aminoazetidin-2-ones 失效
    3 {62-氨基氮杂环丁烷-2-酮的方法

    公开(公告)号：US4127568A

    公开(公告)日：1978-11-28

    申请号：US775240

    申请日：1977-03-07

    申请人： Robin D. G. Cooper ,  Gary A. Koppel ,  Lawrence J. McShane

    发明人： Robin D. G. Cooper ,  Gary A. Koppel ,  Lawrence J. McShane

    IPC分类号： C07D205/08 ,  C07D205/085 ,  C07D498/04 ,  C07D507/00

    CPC分类号： C07D205/085

    摘要： 1-[.alpha.-(Carboxy)-4-hydroxybenzyl]-3.beta.-aminoazetidin-2-one esters are prepared by converting 2-acyl-3,3-dialkyl-7-oxo-.alpha.-[4-(benzyloxy)phenyl]-4-thia-2,6-diazabicyclo[3.2.0]-heptane-6-acetic acid esters with mercuric acetate in an aqueous organic solvent mixture, e.g., in aqueous methanol, to 7-oxo-3-phenyl-.alpha.-[4-(benzyloxy)phenyl]-4-oxa-2,6-diazabicyclo[3.2.0]hept-2-ene-1-acetic acid esters and the latter are reacted with PCl.sub.5 and pyridine to provide the monocyclic 1-[.alpha.-(carboxy)-4-benzyloxybenzyl]-3.beta.-(.alpha.-chlorobenzylideneamino)-4-chloroazetidin-2-one esters. Reduction of the dichloro azetidin-2-one with an organo tin hydride and azobisisobutyronitrile affords the deschloro, 1-[.alpha.-(carboxy)-4-benzyloxybenzyl]-3.beta.-benzylideneaminoazetidin-2-one ester. The latter is hydrolyzed and the 4-benzyloxy group is cleaved via catalytic hydrogenolysis to yield an ester of 1-[.alpha.-(carboxy)-4-hydroxybenzyl]-3.beta.-aminoazetidin-2-one. The 3.beta.-amino ester is useful for the preparation of the antibiotic FR 1923 (nocardicin).

    摘要翻译： 通过将2-酰基-3,3-二烷基-7-氧代-α-[4-（苄氧基）苯基 ] -4-硫杂-2,6-二氮杂双环[3.2.0] - 庚烷-6-乙酸酯与乙酸汞在含水有机溶剂混合物（例如甲醇水溶液）中加入到7-氧代-3-苯基-α - [4-（苄氧基）苯基] -4-氧杂-2,6-二氮杂双环[3.2.0]庚-2-烯-1-乙酸酯，后者与PCl5和吡啶反应，得到单环1- -3α-（α-羧基）-4-苄氧基苄基]-3β-（α-氯亚苄基氨基）-4-氯氮杂环丁-2-酮酯。 用有机锡氢化物和偶氮二异丁腈还原二氯氮杂环丁烷-2-酮，得到脱氯，1- [α-（羧基）-4-苄氧基苄基]-3β-亚苄基氨基氮杂环丁-2-酮酯。 后者被水解，4-苄氧基通过催化氢解裂解，得到1- [α-（羧基）-4-羟基苄基]-3β-氨基吖丁啶-2-酮的酯。 3β-氨基酯可用于制备抗生素FR1923（诺卡霉素）。

    6-Unsubstituted-7-oxo-4-oxa-diazabicyclo(3.2.0)hept-2-ene derivatives
    8.
    发明授权
    6-Unsubstituted-7-oxo-4-oxa-diazabicyclo(3.2.0)hept-2-ene derivatives 失效
    6-取代-7-氧代-4-氧杂 - 二氮杂双环（3.2.0）庚-2-烯衍生物

    公开(公告)号：US4564473A

    公开(公告)日：1986-01-14

    申请号：US520097

    申请日：1983-08-04

    申请人： Dieter Habich

    发明人： Dieter Habich

    IPC分类号： C07D499/74 ,  C07D331/02 ,  C07D498/04 ,  C07D499/00 ,  C07D499/06 ,  C07D507/00

    CPC分类号： C07D331/02 ,  C07D499/00

    摘要： A compound of the formula ##STR1## in which R is hydrogen, or optionally substituted alkyl, alkenyl, alkinyl, aralkyl, aryl, heteroaryl, heteroaralkyl, aryloxyalkyl, heteroaryloxyalkyl, alkoxyalkyl, arylthioalkyl, heteroarylthioalkyl, alkylthioalkyl, alkoxy, aryloxy, alkylthio or arylthio.The compounds are prepared by novel processes and are suitable as intermediates for .beta.-lactam antibiotics.

    摘要翻译： 芳基，杂芳基，杂芳烷基，芳氧基烷基，杂芳基氧基烷基，烷氧基烷基，芳基硫代烷基，杂芳硫基烷基，烷硫基烷基，烷氧基，芳氧基，烷硫基或芳基硫基的化合物，其中R为氢或任选取代的烷基， 。 该化合物通过新方法制备，并且适合作为β-内酰胺抗生素的中间体。

    BIOLOGICALLY ACTIVE MOLECULES, CONJUGATES THEREOF, AND THERAPEUTIC USES
    10.
    发明申请
    BIOLOGICALLY ACTIVE MOLECULES, CONJUGATES THEREOF, AND THERAPEUTIC USES 有权

    公开(公告)号：US20220332729A1

    公开(公告)日：2022-10-20

    申请号：US17733974

    申请日：2022-04-29

    申请人： REGENERON PHARMACEUTICALS, INC.

    发明人： Thomas NITTOLI

    IPC分类号： C07D507/00 ,  A61K47/68 ,  A61K31/5365

    摘要： The present disclosure relates to linker compounds that are useful in covalently linking biologically active molecules with Ligands. The disclosed compounds also relate to biologically active molecules and Ligand conjugates, wherein the biologically active molecule is linked to the Ligand through a linker. The disclosure further provides compositions comprising biologically active molecule-ligand conjugates, methods of modifying abnormal cell growth and methods of treatment using the conjugates or the compositions.