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    • 5. 发明申请
    • PHOSPHOSUCCINIC ACID DERIVATIVES AND THEIR USE AS MEDICAMENTS
    • PHOSPHONOBERNSTEINSÄUREDERIVATE及其作为药物
    • WO1995000522A1
    • 1995-01-05
    • PCT/EP1994001980
    • 1994-06-17
    • BOEHRINGER MANNHEIM GMBHTSAKLAKIDIS, ChristosESSWEIN, AngelikaZIMMERMANN, GerdBAUSS, Frieder
    • BOEHRINGER MANNHEIM GMBH
    • C07F09/38
    • C07F9/655345C07F9/3808C07F9/3826C07F9/383C07F9/3882C07F9/572C07F9/59C07F9/6533C07F9/65515C07F9/6552
    • Compounds have formula (I), in which R , R may represent independently from each other hydrogen, lower alkyl, cycloalkyl or arylmethyl; R , R may represent independently from each other hydrogen, lower alkyl, or one of the groups -OR or -NR R , or they may form together with the atoms to which they are bound a five- to seven-membered carbocyclic ring or an heterocyclic ring containing one or two heteroatoms; R stands for lower alkenyl, cycloalkyl, cycloalkenyl, monocyclic arylalkyl, bicyclic aryl, biaryl or a group having formulae (a): R -X-alk- or (b), or forms together with R and the carbon atom to which it is bound a possibly substituted five- to seven-membered carbocyclic or heterocyclic ring; R stands for hydrogen, lower alkyl or arylmethyl; R , R represent independently from each other hydrogen or lower alkyl or form together with the nitrogen atom to which they are bound a five- or six-membered heterocyclic ring; R stands for hydrogen, lower alkyl, lower alkenyl, cycloalkyl, cycloalkenyl, mono- or bicyclic aryl, biaryl; R stands for a group having formula (a); X stands for a valence dash, oxygen or sulphur; Q stands for oxygen, sulphur or nitrogen; alk stands for a valence dash, a methylene chain, a saturated or unsaturated alkylene chain with 2-6 carbon atoms; n equals 0-3, m equals 0-2 and p equals 0-5. Also disclosed is a process for preparing said compounds and medicaments containing the same used for treating calcium metabolism disturbances.
    • 式(I)的化合物,其中R <1>,R <2>可以是氢,低级烷基,环烷基或彼此独立地芳甲基; [R <3>,R <4>各自独立地是氢,低级烷基,或以下基团之一-OR <6>,或-NR可以是<7> - [R <8>,或连同原子它们所连接 可形成五至七元碳环或含有一到两个杂原子的杂环; [R <5>低级链烯基,环烷基,环烯基,单环芳基烷基,二环芳基,联芳基或式的基团(一):R <9> -X-烷 - 或(b)指,或者与R一起<4> 和的碳原子其所连接形成任选经取代的五到形成七元碳环或杂环; [R <6>是氢,低级烷基或芳基甲基; [R <7> - [R <8>各自独立地表示氢或低级烷基,或一起与氮原子到它们所连接,形成五至六元杂环; [R <9>是氢,低级烷基,低级烯基,环烷基,环烯基,单环或双环芳基,联芳基,R <10>为式(a)的装置; X的化合价键,代表氧或硫; Q是氧,硫或氮; alk是价键,亚甲基,一个饱和或不饱和的亚烷基链与2 - 6个碳原子的装置; N = 0-3; M = 0-2且p = 0-5的装置,其制备方法和含有这些化合物,钙代谢紊乱的治疗的药物组合物的方法。
    • 6. 发明申请
    • NEW BARBITURIC ACID DERIVATIVES, PROCESSES FOR THEIR PRODUCTION AND PHARMACEUTICAL AGENTS CONTAINING THESE COMPOUNDS
    • 新型巴比妥酸衍生物及其生产方法及含有这些化合物的药物代理
    • WO1997023465A1
    • 1997-07-03
    • PCT/EP1996005766
    • 1996-12-20
    • BOEHRINGER MANNHEIM GMBHBOSIES, ElmarESSWEIN, AngelikaGRAMS, FrankKRELL, Hans-WilliMENTA, Ernesto
    • BOEHRINGER MANNHEIM GMBH
    • C07D239/62
    • C07D401/04C07D239/62
    • Compounds of formula (I) in which X, Y and Z are independently of one another oxygen, sulphur or NH; R1 represents a group W-V: W is a valence dash or a straight-chained or branched C1-C8 alkyl or a C2-C8 alkenyl group which is optionally once or several times substituted, V is an optionally substituted monocycle or bicycle which can contain one or several heteroatoms, or W-V is a C1-C20 alkyl group which can be interrupted by heteroatoms, one or several carbon atoms are optionally substituted; R2 and R3 represent hydrogen or one of the two represents lower alkyl or lower acyl; R4 and R5 denote independently of each other for A-D, wherein A represents a dash alkyl, alkenyl, acyl, alkylsulfonyl, sulfonyl, alkylaminocarbonyl, aminocarbonyl, alkoxycarbonyl, oxy-carbonyl, alkylaminothiocarbonyl, aminothio-carbonyl which is optionally once or several times substituted; D represents a hydrogen, monocycle or bicycle, the monocycle or bicycle is optionally once or several times interrupted by heteroatoms and the monocycle or bicycle is once or several times substituted, or R4 and R5 together with the adjacent N atom form a ring; pharmacologically acceptable salts and prodrugs thereof and optically active forms, processes for their production and pharmaceutical agents which contain these compounds having a matrix metalloprotease-inhibitory action.
    • 其中X,Y和Z彼此独立地为氧,硫或NH的式(I)化合物; R 1表示基团W V:W是价键或直链或支链C 1 -C 8烷基或任选被一次或多次取代的C 2 -C 8烯基,V是任选取代的单环或自行车,其可以含有一个 或几个杂原子,或WV是可以被杂原子中断的C1-C20烷基,一个或几个碳原子任选被取代; R2和R3代表氢或二者之一代表低级烷基或低级酰基; R 4和R 5彼此独立地表示A-D,其中A代表烷基,烯基,酰基,烷基磺酰基,磺酰基,烷基氨基羰基,氨基羰基,烷氧基羰基,氧羰基,烷基氨基硫代羰基,氨基硫代羰基,其任选被一次或多次取代; D代表氢,单环或自行车,单环或自行车任选被杂原子中断一次或多次,单环或自行车被一次或多次取代,或者R4和R5与相邻的N原子形成环; 其药理学上可接受的盐和前药以及光学活性形式,其制备方法和含有这些具有基质金属蛋白酶抑制作用的化合物的药剂。
    • 8. 发明申请
    • NEW OXAZOLIDINONE DERIVATIVES, PROCESS FOR PREPARING THE SAME AND MEDICAMENTS THAT CONTAIN THESE COMPOUNDS
    • 新的恶唑烷酮衍生物,方法为生产和药物含有它们的
    • WO1997003072A1
    • 1997-01-30
    • PCT/EP1996002939
    • 1996-07-04
    • BOEHRINGER MANNHEIM GMBHTSAKLAKIDIS, ChristosSCHÄFER, WolfgangDÖRGE, LieselFRIEBE, Walter-GunarESSWEIN, Angelika
    • BOEHRINGER MANNHEIM GMBH
    • C07D413/14
    • C07D413/14
    • New oxazolidinone derivatives are disclosed, as well as a process for preparing the same and medicaments that contain these substances. The disclosed compounds have general formula (I), in which X, Y and Q independently represent nitrogen or CH; W stands for hydrogen or NR R ; Z stands for nitrogen, CH or C-OH; A, E and G independently represent the valence dash or an alkylene chain -(CH2)n-; B stands for a valence dash and, when Z equals N, it may also stand for a carbonyl group; D stands for a side chain having the form -(CHR )m-COO- or =CR -COO-; n equals 1 to 5; m equals 0.1; R , R independently represent hydrogen, lower alkyl or aryl, or form together a carbocyclic five- or six-membered ring; R stands for hydrogen or a group -OR or -NR R ; R stands for hydrogen or a group -OR ; R stands for hydrogen, lower alkyl, aryl or arylalkyl; R stands for hydrogen, lower alkyl or arylalkyl; R stands for hydrogen, lower alkyl, arylalkyl, acyl, alkylsulphonyl or arylsulphonyl.
    • 本发明涉及新的恶唑烷酮衍生物,其制备方法和含有这些物质的药物组合物。 本发明涉及通式(I)中的X,Y和Q彼此独立地表示氮或CH的化合物; W是氢或NR <0> - [R <00>基; Z是氮,CH或C-OH; A,E和G彼此独立地化合价破折号或亚烷基链的 - 平均(CH 2)N-; 乙价破折号和用于Z为等于N的情况下,也意味着羰基; D是形式的侧链 - (CHR <3>)M-COO-或= CR <3>为-COO-; N = 1-5烷基; m为= 0.1; [R <1>,R <2>独立地是氢,低级烷基或芳基,或一起形成碳环五元或六元环; [R <3>是氢或基团-OR <5>或-NR <6> - [R <7>基; [R <4>是氢或基团-OR <5>基; [R <5>是氢,低级烷基,芳基或芳基烷基; [R <6>是氢,低级烷基或芳基烷基; ,R <7>是氢,低级烷基,芳烷基,酰基,烷基磺酰基或芳基磺酰。