Quinuclidine compounds and drugs containing the same as the active ingredient
    3.
    发明授权
    Quinuclidine compounds and drugs containing the same as the active ingredient 失效
    奎宁环化合物和含有与活性成分相同的药物

    公开(公告)号:US06599917B1

    公开(公告)日:2003-07-29

    申请号:US10088554

    申请日:2002-03-19

    IPC分类号: A61K31439

    CPC分类号: C07D453/02

    摘要: The present invention provides an excellent squalene synthesizing enzyme inhibitor. Specifically, it provides a compound (I) represented by the following formula, a salt thereof or a hydrate of them. In which R1 represents (1) hydrogen atom or (2) hydroxyl group; HAr represents an aromatic heterocycle which may be substituted with 1 to 3 groups; Ar represents an optionally substituted aromatic ring; W represents a chain represented by (1) —CH2—CH2— which may be substituted, (2) —CH═CH— which may be substituted, (3) —C≡C—, (4) —NH—CO—, (5) —CO—NH—, (6) —NH—CH2—, (7) —CH2—NH—, (8) —CH2—CO—, (9) —CO—CH2—, (10) —NH—S(O)l—, (11) —S(O)l—NH—, (12) —CH2—S(O)— or (13) —S(O)l—CH2— (l denotes 0, 1 or 2); and X represents a chain represented by (1) a single bond, (2) an optionally substituted C1-6 alkylene chain, (3) an optionally substituted C2-6 alkenylene chain, (4) an optionally substituted C2-6 alkynylene chain, (5) a formula —Q— (wherein Q represents oxygen atom, sulfur atom, CO or N(R2) (wherein R2 represents a C1-6 alkyl group or a C1-6 alkoxy group)), (6) —NH—CO—, (7) —CO—NH—, (8) —NH—CH2—, (9) —CH2—NH—, (10) —CH2—CO—, (11) —CO—CH2—, (12) —NH—S(O)m—, (13) —S(O)m—NH—, (14) —CH2—S(O)m—, (15) —S(O)m—CH2— (wherein m denotes 0, 1 or 2) or (16) —(CH2)n—O— (wherein n denotes an integer from 1 to 6).

    摘要翻译: 本发明提供优良的角鲨烯合成酶抑制剂。 具体地说,它提供由下式表示的化合物(I),其盐或它们的水合物。其中R1表示(1)氢原子或(2)羟基; HAr表示可被1〜3个基团取代的芳香族杂环; Ar表示任选取代的芳环; W表示可被取代的(1)-CH 2 -CH 2 - 表示的链,(2)可以被取代的-CH = CH-,(3)-C = C-,(4)-NH-CO-, (5)-CO-NH-,(6)-NH-CH2-,(7)-CH2-NH-,(8)-CH2-CO-,(9)-CO-CH2-,(10)-NH -S(O)1 - ,(11)-S(O)1 -NH-,(12)-CH 2 -S(O) - 或(13)-S(O) 1或2); 并且X表示由(1)单键表示的链,(2)任选取代的C 1-6亚烷基链,(3)任选取代的C 2-6亚烯基链,(4)任选取代的C 2-6亚炔基链, (5)式-Q-(其中Q表示氧原子,硫原子,CO或N(R2)(其中R2表示C1-6烷基或C1-6烷氧基)),(6)-NH- CO-,(7)-CO-NH-,(8)-NH-CH2-,(9)-CH2-NH-,(10)-CH2-CO-,(11)-CO-CH2-, )-NH-S(O)m - ,(13)-S(O)m -NH-,(14)-CH 2 -S(O)m - ,(15)-S(O)m -CH 2 - 其中m表示0,1或2)或(16) - (CH2)nO-(其中n表示1至6的整数)。

    Radiation polymerization of cationic monomer in aqueous alcohol
    7.
    发明授权
    Radiation polymerization of cationic monomer in aqueous alcohol 失效
    阳离子单体在含水醇中的辐射聚合

    公开(公告)号:US4354907A

    公开(公告)日:1982-10-19

    申请号:US118967

    申请日:1980-02-05

    CPC分类号: C08F20/34

    摘要: A process for the production of water-soluble, substantially solid, cationic polymers comprises the step of irradiating an aqueous solution with ionizing radiation, the aqueous solution comprising at least 50% by weight of one, or two or more of specific type of amino ester or esters optionally being accompanied by acrylamide, and at least 0.1% by weight of a specific type of alcohol as an agent for inhibiting water-insolubility of the resulting polymer.The amino esters have the generic formula ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group; R.sub.2 represents a hydrogen atom or an alkyl group having 1-4 carbon atoms; R.sub.3 and R.sub.4 each represents an alkyl group having 1-4 carbon atoms and x.sup.(-) represents an anion; or from the combination of at least one of said amino esters and acrylamide.The alcohols have the formula ##STR2## wherein X', Y' and Z' each represents a hydrogen atom or a hydroxyl group, providing at least one of said X', Y' and Z' is OH; and L, m and n each represents a natural number; and include isopropyl alcohol, isobutyl alcohol, sec. butyl alcohol, glycerine and propylene glycol.

    摘要翻译: 制备水溶性,基本上固体的阳离子聚合物的方法包括用电离辐射照射水溶液的步骤,所述水溶液包含至少50重量%的一种或两种或更多种特定类型的氨基酯 或任选地伴随丙烯酰胺的酯,以及至少0.1重量%的特定类型的醇作为抑制所得聚合物的水不溶性的试剂。 氨基酯具有通式“IMAGE”,其中R 1表示氢原子或甲基; R2表示氢原子或具有1-4个碳原子的烷基; R3和R4各自表示具有1-4个碳原子的烷基,x( - )表示阴离子; 或至少一种所述氨基酯和丙烯酰胺的组合。 醇具有式“其中X',Y'和Z”各自表示氢原子或羟基,提供所述X',Y'和Z'中的至少一个是OH; L,m和n各自表示自然数; 并包括异丙醇,异丁醇, 丁醇,甘油和丙二醇。