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19 条记录 (耗时 0.016 秒)

    Compounds useful in treating sickle cell anemia
    11.
    发明公开
    Compounds useful in treating sickle cell anemia 失效
    Verbindungen von Nutzen bei der Behandlung vom Herrickschen Syndrom。

    公开(公告)号：EP0240256A2

    公开(公告)日：1987-10-07

    申请号：EP87302643.9

    申请日：1987-03-26

    申请人： Merck & Co., Inc. ,  UNIVERSITY OF PITTSBURGH

    发明人： Abraham, Donald J. ,  Cragoe, Edward J., Jr. ,  Woltersdorf, Otto W., Jr.

    IPC分类号： C07C59/90 ,  C07C62/38 ,  C07C233/46 ,  C07C235/32 ,  C07C235/70 ,  C07C205/27 ,  C07C205/49

    CPC分类号： C07C205/54 ,  C07C45/46 ,  C07C49/835 ,  C07C59/74 ,  C07C59/90 ,  C07C59/92 ,  C07C65/30 ,  C07C205/32 ,  C07C205/33 ,  C07C49/825

    摘要： The present invention is directea to compounds or the formula (I) useful as anti-sickling agents and to pharmaceutical compositions of these compounds wherein formula


    V is selected from:

    which R, is ethyl, propyl or isopropyl;

    in which R 2 is H or lower alkyl;
    in which
    R 3 is lower alkyl;

    W is selected from:


    . A 2 is (CH 2 )n 2 -C(CH 3 ) 2 , -C(CH 2 ) 3 - and n 2 = 1 to 5; X is 0 or 1;

    R3 is HO- or

    A3 is -(CH 2 )n 3 or -C(CH 2 ) 3 - and
    n 3 = 1 to 5;
    m is 0 or 1;
    and
    Y is H, Cl or OCH 3 ;
    Z is H or Cl;
    provided that

    (i) when W is
    and Y and Z are Cl;
    (ii) when W is
    Y and Z are Cl, with the proviso that when R 2 is C 2 H 5 , R 2 is H and X is O, n 2 is 2 to 5;
    (iii) When W is
    with the proviso that when R3 is OH, Y is H or Cl and m is 1, n 3 = 4 or 5; (iv) when W is
    and Y and Z are Cl.

    摘要翻译： 本发明涉及可用作抗镰刀剂的式（I）化合物和这些化合物的药物组合物，其中式（I）： V选自CHEM，其中R 1是乙基，丙基或 异丙基; 其中R2为H或低级烷基的CHEM; 其中R 3为低级烷基; （d） - @ -CH = CH 2; W选自：（a）其中A 1是（CH 2）n1，-C（CH 2）3和n1 = 2,4或5的HO-@ -Al-O- 其中R 2为H，低级烷基，苄基，CH 2 OH; H

    Substituted 6-Phenethyl-and phenylethenyl-3,4,5,6-tetrahydro-4-hydroxytetraydropyran-2-ones in the4-R trans stereoisomeric forms and the corresponding dihydroxy acids, process for preparing and pharmaceutical composition comprising them
    14.
    发明公开
    Substituted 6-Phenethyl-and phenylethenyl-3,4,5,6-tetrahydro-4-hydroxytetraydropyran-2-ones in the4-R trans stereoisomeric forms and the corresponding dihydroxy acids, process for preparing and pharmaceutical composition comprising them 失效
    取代的6-苯乙基，和苯基乙烯基-3,4,5,6-四氢-4-羟基 - 四氢吡喃-2-酮茚4 R反式用于容纳它们的制备和药物组合物，立体异构体形式和相应的二羟基羧酸，过程。

    公开(公告)号：EP0024348A1

    公开(公告)日：1981-03-04

    申请号：EP80104807.5

    申请日：1980-08-14

    申请人： Merck & Co., Inc.

    发明人： Willard, Alvin K. ,  Cragoe, Edward J., Jr. ,  Novello, Frederick C. ,  Hoffman, William F.

    IPC分类号： C07D309/30 ,  A61K31/365 ,  C07C59/48 ,  C07C69/73

    CPC分类号： C07D309/30 ,  C07C67/347 ,  C07C69/738

    摘要： 6-Phenyl-, phenalkyl- and phenylethenyl-4-hydroxytetrahydropyran-2-ones in the 4- R trans stereoisomeric forms having the structure
    wherein

    A is H or methyl;
    E is a direct bond, -CH 2 -, -CH 2 -CH 2 -, -CH 2 -CH 2 -CH 2 - or-CH-CH-; and R 1 , R 2 and R 3 have several meanings, and the corresponding dihydroxy acids in which the lactone ring is hydrolytically opened, and the pharmaceutically acceptable salts of said dihydroxy acids, and the lower alkyl and the phenyl, dimethylamino or acetylamino-substituted lower alkyl esters of said dihydroxy acids; and processes for preparing them. These compounds are potent inhibitors of cholesterol synthesis by the enzyme hydroxymethyl glutaryl coenzyme A reductase.

    摘要翻译： 6 - 苯基，苯烷基和苯基乙烯基-4-羟基四氢吡喃-2-酮在具有结构其中A是H或甲基的4-反式 - [R立体异构体形式; E是直接键，-CH 2 - ，-CH 2 CH 2 - ，-CH 2 -CH-CH2-CH2-或-CH = CH-; 和R1，R2和R3具有多种含义，和相应的二羟基羧酸，其中内酯环水解开通，并且说二羟基酸的药学上可接受的盐，以及低级烷基和苯基，二甲基氨基或乙酰氨基取代的低级烷基酯 的说二羟基羧酸; 及其制备方法它们。 这些化合物是通过酶羟甲基胆固醇合成的有效抑制剂戊二酰辅酶A还原酶。

    Pharmaceutical compositions containing 4-((6,7-Dihalogen-2,3-dihydro-1-oxo-1H-inden-5-yl)-oxy) butanoic acid compounds
    17.
    发明公开
    Pharmaceutical compositions containing 4-((6,7-Dihalogen-2,3-dihydro-1-oxo-1H-inden-5-yl)-oxy) butanoic acid compounds 失效
    4 - （（6,7-二卤代-2,3-二氢-1-氧代-1H-茚-5-基） - 氧基） - 丁酸酯 - 维生素A的Pharmazeutische Zusammensetzungen。

    公开(公告)号：EP0047011A1

    公开(公告)日：1982-03-10

    申请号：EP81106827.9

    申请日：1981-09-01

    申请人： Merck & Co., Inc.

    发明人： Cragoe, Edward J., Jr. ,  Woltersdorf, Otto W., Jr.

    IPC分类号： C07C59/90 ,  C07C69/712 ,  C07C51/373 ,  C07C67/14 ,  A61K31/215

    CPC分类号： C07C59/90

    摘要： The invention relates to compounds of the formula
    wherein X 1 and X 2 are halo;

    R is lower alkyl of from 1 to 6 carbon atoms;
    R' is hydrogen, lower alkyl of 1 to 4 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, lowercycloalkylloweralkyl of 4 to 7 carbon atoms and phenyl;
    R 2 is hydrogen or lower alkyl of 1 to 6 carbon atoms, and carboxy lower alkyl of 2 to 6 carbon atoms; and the pharmaceutically acceptable salts thereof and a process for preparing the same. Those compounds are suitable for the treatment and prevention of injury to the gray matter of the brain and to the spinal chord due to accidents, ischemic stroke, cardiac arrest, arrested breathing, Reye's syndrome and hydrocephalus.

    摘要翻译： 本发明涉及式CHEM的化合物，其中X 1和X 2都是卤素; R是1至6个碳原子的低级烷基; R 1是氢，1至4个碳原子的低级烷基，3至6个碳原子的环烷基，4至7个碳原子的低级环烷基低级烷基和苯基; R 2是氢或1-6个碳原子的低级烷基和2-6个碳原子的羧基下通气; 及其药学上可接受的盐及其制备方法。 那些化合物适合于治疗和预防由于事故，缺血性卒中，心脏骤停，呼吸停止，Reye综合征和脑积水引起的脑灰质和脊髓损伤。

    3-Amino-5-substituted-6-halo-N-(3,4-dihydro- or 4,4-disubstituted-6-substituted-1,3,5-triazin-2-yl)-2-pyrazinecarboxamides, process for preparing and pharmaceutical compositions containing the same
    18.
    发明公开
    3-Amino-5-substituted-6-halo-N-(3,4-dihydro- or 4,4-disubstituted-6-substituted-1,3,5-triazin-2-yl)-2-pyrazinecarboxamides, process for preparing and pharmaceutical compositions containing the same 失效
    3-氨基-5-取代的6-卤代 - N-（3,4-二氢 - 或4,4二取代的6-取代-1,3,5-三嗪-2-基）吡嗪羧酰胺，处理为他们的 制备方法和含有它们的药物组合物。

    公开(公告)号：EP0043139A1

    公开(公告)日：1982-01-06

    申请号：EP81105094.7

    申请日：1981-07-01

    申请人： Merck & Co., Inc.

    发明人： Woltersdorf, Otto W., Jr. ,  Smith, Robert L. ,  Cragoe, Edward J., Jr. ,  De Solms, Jane S.

    IPC分类号： C07D403/12 ,  A61K31/53

    CPC分类号： C07D403/12 ,  C07D251/10

    摘要： This invention relates to 3-amino-5-substituted-6- haloN-(3,4-dihydro- or 4,4-disubstituted-6-substituted- 1,3,5-triazin-2-yl)-2-pyrazinecarboxamides. The invention also relates to processes for preparing those compounds of the formula of the tautomeric form thereof
    wherein

    R is hydrogen,, C 1 - 5 alkyl, C 2-5 alkenyl or C 3-6 cycloalkyl;
    R 1 is hydrogen, C 1-5 alkyl, C 2 - 5 alkenyl or C 3-6 cycloalkyl;
    R 2 is hydrogen, or C 1-5 alkyl;
    R 3 is hydrogen, or Ci-5 alkyl;
    R 2 and R 3 can be joined with the carbon atom to which they are attached to form a 3-7 membered carbon ring;
    X is halo
    Y is OH, SH, C 1-5 alkoxy, C 1-5 alkylthio and NR 4 R 5 wherein R 4 is hydrogen or C 1-5 alkyl and R 5 is hydrogen, C 1-5 alkyl, CN, CONH 2 , CNH 2 , N0 2 or NH 2 and the pharmaceutical acid addition salts thereof.

    The compounds are eukalemic/saluretic agents useful in the treatment of edema and hypertension.

    摘要翻译： 本发明涉及3-氨基-5-取代的6-卤代-N-（3,4-二氢 - 或4,4二取代的6-取代的-1,3,5-三嗪-2-基）-2- -pyrazinecarboxamides。 因此本发明涉及一种用于制备的互变异构形式的式Ⅰ化合物或其 worin R是氢,, C 1-5烷基，C 2-5链烯基或C 3-6环烷基; [R <1>是氢，C 1-5烷基，C 2-5链烯基或C 3-6环烷基; [R <2>为氢，或C1-5烷基; [R <3>为氢，或C1-5烷基; [R <2>和R <3>可与碳原子连接到它们所连接以形成3-7元碳环; X是卤素，Y是OH，SH，C 1-5烷氧基，C 1-5烷硫基和NR <4> - [R <5> worinř<4>是氢或C 1-5烷基且R <5>为氢，C1-5 烷基，CN，CONH 2，CNH 2，NO 2或NH 2 NH和它们的药物的酸加成盐。 的化合物在水肿和高血压的治疗中有用的保钾/促尿食盐排泄剂。

    Novel substituted pyrazinyl-1,2,4-oxadiazoles, processes for preparing the same and a pharmaceutical composition containing the same
    19.
    发明公开
    Novel substituted pyrazinyl-1,2,4-oxadiazoles, processes for preparing the same and a pharmaceutical composition containing the same 失效
    吡嗪基取代的-1,2,4-恶二唑，处理用于其制备方法和含有其的药物制剂。

    公开(公告)号：EP0040422A1

    公开(公告)日：1981-11-25

    申请号：EP81103800.9

    申请日：1981-05-18

    申请人： Merck & Co., Inc.

    发明人： Bock, Mark G. ,  Cragoe, Edward J., Jr. ,  Smith, Robert L.

    IPC分类号： C07D413/04 ,  A61K31/495

    CPC分类号： C07D241/26

    摘要： Novel substituted pyrazinyl-1,2,4-oxadiazoles of the formulas
    are disclosed wherein

    R is hydrogen or lower alkyl (C 1-5 ),
    R 1 is hydrogen or lower alkyl (C 1-5 ),
    R 2 is hydrogen or lower alkyl (C 1-5 ),
    R 3 is hydrogen or lower alkyl (C 1-5 ),
    R and R' can be joined to form an alkylene group of from 2-4 i carbon atoms,
    R 4 is lower alkyl (C 1-5 )
    X is halo, cyano or phenyl, and
    Y- is chloride, bromide or iodide, or a suitable anion.

    Processing for preparing the same are also described. The compounds are useful in the treatment of edema and hypertension.

    摘要翻译： 新颖substituiertem吡嗪基-1,2,4-恶二唑式... ...被游离缺失盘... worin ... R是氢或低级烷基（C 1-5），... - [R <1>是氢或低级烷基（C 1-5 ）... [R <2>是氢或低级烷基（C 1-5），... - [R <3>是氢或低级烷基（C 1-5），...，R和R <1>可以被连接以形成在亚烷基的基团 从2-4个碳原子，...... [R <4>是低级烷基（C 1-5）... X是卤素，氰基或苯基，和... Y < - >是氯化物，溴化物或碘化物，或适宜的阴离子。 ...被如此描述制备相同的处理。 的化合物在水肿和高血压的治疗中是有用的。