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    Process for preparing 3-alkenylidene-1,1-bisphosphonates
    12.
    发明授权
    Process for preparing 3-alkenylidene-1,1-bisphosphonates 失效
    制备3-亚烯基-1,1-二膦酸盐的方法

    公开(公告)号：US5103036A

    公开(公告)日：1992-04-07

    申请号：US699047

    申请日：1991-05-13

    Applicant: David R. Magnin ,  Richard B. Sulsky

    Inventor： David R. Magnin ,  Richard B. Sulsky

    IPC: B01J31/24 ,  C07B61/00 ,  C07F9/40

    CPC classification number: C07F9/4025

    Abstract: A process is provided for preparing a 3-alkenylidene-1,1-bisphosphonate which is an intermediate for preparing an inhibitor of the enzyme squalene synthetase which is useful as an inhibitor of cholesterol biosynthesis, or which bisphosphonate itself is useful as an inhibitor of cholesterol biosynthesis. The process involves the palladium catalyzed coupling of an allylic ester with a tetraester of a methylenebisphosphonate to form a 3-alkenylidene-1,1-bisphosphonate containing an alkene moiety located .gamma., .delta. to the phosphonates.

    .alpha.-phosphonocarboxylate squalene synthetase inhibitors
    18.
    发明授权
    .alpha.-phosphonocarboxylate squalene synthetase inhibitors 失效
    α-膦酰基角鲨烯合成酶抑制剂

    公开(公告)号：US5312814A

    公开(公告)日：1994-05-17

    申请号：US987831

    申请日：1992-12-09

    Applicant: Scott A. Biller ,  David R. Magnin

    Inventor： Scott A. Biller ,  David R. Magnin

    IPC: A61K31/66 ,  A61P3/06 ,  A61P31/04 ,  A61P35/00 ,  C07F9/38 ,  C07F9/40 ,  A61K31/73

    CPC classification number: C07F9/4056 ,  C07F9/3808 ,  C07F9/3826 ,  C07F9/3882 ,  C07F9/4006 ,  C07F9/4015

    Abstract: .alpha.- Phosphonocarboxylate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.1 is a lipophilic group which contains at least 7 carbons and is substituted alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted arylalkyl or optionally substituted aryl;Z is H, halogen, hydroxy, hydroxyalkyl or lower alkyl;R.sup.2 and R.sup.3 are independently H, metal ion or other pharmaceutically acceptable cation, or a prodrug ester;R.sup.4 is H, metal ion or other pharmaceutically acceptable cation, lower alkyl, lower alkenyl, arylalkyl, aryl or a prodrug ester.

    Abstract translation: 提供α-磷酸羧酸酯化合物，其抑制酶角鲨烯合成酶，从而抑制胆固醇生物合成。 这些化合物具有式“IMAGE”，其中R 1是含有至少7个碳原子并且是取代的烷基，任选取代的环烷基，任选取代的环烷基烷基，任选取代的烯基，任选取代的炔基，任选取代的芳烷基或任选取代的芳基的亲油基团; Z是H，卤素，羟基，羟烷基或低级烷基; R2和R3独立地为H，金属离子或其它药学上可接受的阳离子，或前药酯; R4是H，金属离子或其它药学上可接受的阳离子，低级烷基，低级烯基，芳烷基，芳基或前药酯。

    Bisphosphonate squalene synthetase inhibitors and method
    19.
    发明授权
    Bisphosphonate squalene synthetase inhibitors and method 失效
    二硫代磷酸酯合成酶抑制剂及方法

    公开(公告)号：US5157027A

    公开(公告)日：1992-10-20

    申请号：US699429

    申请日：1991-05-13

    Applicant: Scott A. Biller ,  David R. Magnin

    Inventor： Scott A. Biller ,  David R. Magnin

    IPC: A61K31/66 ,  A61P3/06 ,  A61P9/10 ,  C07F9/38 ,  C07F9/40

    CPC classification number: C07F9/4025 ,  C07F9/3839

    Abstract: Compounds which are inhibitors of cholesterol biosynthesis (by inhibiting de novo squalene biosynthesis), and thus are useful as hypocholesterolemic agents and antiatherosclerotic agents are provided which have the structure ##STR1## and analogs thereof, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are H, lower alkyl, a metal ion or a prodrug ester;R.sup.5 is H, halogen or lower alkyl;Zq is substituted alkenyl, substituted alkynyl, mixed alkenyl-alkynyl or substituted phenylalkyl or, phenylalkenyl or phenylalkynyl, or alkyl, including all stereoisomers thereof.New methods for using such compounds to inhibit cholesterol biosynthesis are also provided.

    3,5-dihydroxypentanoic acid derivatives useful as antihypercholesterolemic agents and method for preparing same
    20.
    发明授权
    3,5-dihydroxypentanoic acid derivatives useful as antihypercholesterolemic agents and method for preparing same 失效
    可用作抗高血胆固醇药的3,5-二羟基戊酸衍生物及其制备方法

    公开(公告)号：US5106992A

    公开(公告)日：1992-04-21

    申请号：US516867

    申请日：1990-04-30

    Applicant: David R. Magnin ,  Eric M. Gordon

    Inventor： David R. Magnin ,  Eric M. Gordon

    IPC: C07D277/06 ,  C07D417/06

    CPC classification number: C07D417/06 ,  C07D277/06

    Abstract: 3,5-Dihydroxypentanoic acid derivatives are provided which are 6-hydroxy-8-(2,2-dimethyl-1-oxybutoxy-2-methyl)-substituted-thiazolidine derivatives and have the structure ##STR1## wherein Z is ##STR2## R.sup.6 is an alkali metal, lower alkyl or H; R.sup.1 and R.sup.2 are the same or different and are H, lower alkyl or aryl; X is S, O, ##STR3## or a single bond; R.sup.7 is lower alkyl; R.sup.3 is lower alkyl or aryl; R.sup.4 and R.sup.5 are the same or different and are H or lower alkyl; and --- represents a single bond or a double bond, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis, and also as antifungal agents.In addition, novel intermediates for use in preparing the above mevinic acid derivatives are also provided.

    Abstract translation: 提供了3,5-二羟基戊酸衍生物，它是6-羟基-8-（2,2-二甲基-1-氧丁氧基-2-甲基） - 取代 - 噻唑烷衍生物，具有结构，其中Z是< R6是碱金属，低级烷基或H; R1和R2相同或不同，为H，低级烷基或芳基; X是S，O，或单键; R7是低级烷基; R3是低级烷基或芳基; R4和R5相同或不同，为H或低级烷基; 和---表示单键或双键，并且是HMG CoA还原酶抑制剂，因此可用作抗高胆固醇血症药物和治疗动脉粥样硬化，并且还可用作抗真菌剂。 此外，还提供了用于制备上述甲酸衍生物的新型中间体。

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