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1. 发明申请

WO1993025539A1 NOVEL PIPERZINYL-BIS(ALKYLAMINO)PYRIMIDINE DERIVATIVES AND PROCESS FOR PREPARING SAME 审中-公开
标题翻译：新型哌嗪基（ALKYLAMINO）吡嗪衍生物及其制备方法
公开(公告)号：WO1993025539A1
公开(公告)日：1993-12-23
申请号：PCT/HU1993000034
申请日：1993-06-08
申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. , MAHO, Sándor , TUBA, Zoltán , SANTA, Csaba , BALOGH, Gábor , CZAJLIKNÉ, Csizér, Éva , LOVASNÉ, Marsai, Mária , GALIK, György
发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.
IPC分类号： C07D239/50
CPC分类号： C07D239/42 , C07D239/48 , C07D239/50 , C07D491/10 , C07J43/003
摘要： The invention relates to novel piperazinyl-bis(alkylamino)pyrimidine derivatives of formula (I), wherein two of X, Y and Z mean a nitrogen atom each and the third one is a methine group; R and R represent, independently from each other, a primary amino group bearing as substituent a branched-chain C4-8alkyl, -alkenyl or -alkynyl group, or a C4-10cycloalkyl group comprising 1 to 3 ring(s) and being optionally substituted by C1-3alkyl group(s); or R and R stand together for a spiro-heterocyclic secondary amino group containing at most 10 carbon atoms and optionally at least one oxygen atom as an additional heteroatom; or one of R and R means an unsubstituted heterocyclic secondary amino group containing 4 to 7 carbon atoms and the other one is an above-identified primary amino group, an above-identified spiro-heterocyclic secondary amino group, or a heterocyclic secondary amino group containing 4 to 7 carbon atoms and substituted by C1-4-alkyl group(s); and n is 1 or 2, as well as their acid addition salts. The compounds of formula (I) are preferably prepared from diaminomonochloropyrimidine compounds and a corresponding piperazine component. The compounds of formula (I) have a pharmacological activity in themselves; it is more important, however, that they can be used as substituents in the preparation of lipid peroxidation-inhibiting substances.
摘要翻译：本发明涉及式（I）的新型哌嗪基 - 双（烷基氨基）嘧啶衍生物，其中X，Y和Z中的两个分别表示氮原子，第三个是次甲基; R 1和R 2彼此独立地表示带有支链C4-8烷基， - 烯基或 - 炔基的取代基的伯氨基或包含1〜3个环的C 4-10环烷基（ s）并任选被C 1-3烷基取代; 或R 1和R 2一起形成含有至多10个碳原子和任选的至少一个氧原子作为另外的杂原子的螺杂环仲氨基; 或者R 1和R 2中的一个是指含有4至7个碳原子的未取代的杂环仲氨基，另一个是上述的伯氨基，上述的螺杂环仲氨基或含有4-7个碳原子并被C 1-4 - 烷基取代的杂环仲氨基; 和n为1或2，以及它们的酸加成盐。式（I）化合物优选由二氨基多氯嘧啶化合物和相应的哌嗪组分制备。式（I）化合物本身具有药理活性; 然而，更重要的是它们可以用作脂质过氧化抑制物质的制备中的取代基。

2. 发明申请

WO1995000532A1 17-HALOGENO-4-AZAANDROSTENE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF 审中-公开
标题翻译： 17-卤代-4-氮杂环丁烷衍生物及其制备方法
公开(公告)号：WO1995000532A1
公开(公告)日：1995-01-05
申请号：PCT/HU1993000040
申请日：1993-06-24
申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. , TUBA, Zoltán , HORVATH, Judit , SZÉLES, János , LOVASNÉ MARSAI, Mária , BALOGH, Gábor
发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.
IPC分类号： C07J73/00
CPC分类号： C07J73/005
摘要： The invention relates to novel 4-azaandrostene derivatives of general formula (I), wherein R represents hydrogen or a C1-3alkyl group; X represents chlorine, bromine or iodine; and the - &cir& _- &cir& _- &cir& _- &cir& _ bond line represents a single or double bond.
摘要翻译：本发明涉及通式（I）的新型4-氮杂雄甾烯衍生物，其中R代表氢或C1-3烷基; X表示氯，溴或碘; 而 - ＆cir＆_-＆cir＆_-＆cir＆_-＆cir＆_ bond line代表单一或双重债券。

3. 发明申请

WO1994007909A1 NOVEL 17'beta'-SUBSTITUTED 4-AZAANDROSTANE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME 审中-公开
标题翻译：新型17β-衍生的4-AZAANDROSTANE衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：WO1994007909A1
公开(公告)日：1994-04-14
申请号：PCT/HU1993000058
申请日：1993-10-01
申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. , TUBA, Zoltán , HORVATH, Judit , KOLLAR, László , LOVASNÉ, Marsai, Mária , BALOGH, Gábor , CSEHI, Attila , JAVOR, András , HAJOS, György , SZPORNY, László
发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.
IPC分类号： C07J73/00
CPC分类号： C07J73/005
摘要： The invention relates to novel 17 beta -substituted 4-azaandrostane derivatives of general Formula (I), wherein R means hydrogen or a C1-3alkyl group; R and R are the same or different and stand for hydrogen or a C1-4alkyl group with the proviso that both can mean hydrogen only in the case when n is higher than 5; or R and R together mean an alpha , omega -alkylene group containing 5 to 7 carbon atoms, the terminal carbon atoms of said alkylene group being bound to the same ring carbon atom; n is 4, 5, 6 or 7; and - &cir& _- &cir& _- &cir& _ bond line represents a single or double bond. Furthermore, the invention relates to pharmaceutical composition containing these compounds as well as a process for the preparation of the compounds of general Formula (I). The compounds of general Formula (I) exert a 5 alpha -reductase enzyme-inhibiting effect and therefore, they are useful for treating all diseases, where the aim is to reduce the tissue dihydrotestosterone level, such as the benign prostatic hyperplasia, acne, seborrhoea, female hirsutism or androgenic alopecia.
摘要翻译：本发明涉及通式（I）的新型17β-取代的4-氮杂雄甾烷衍生物，其中R表示氢或C 1-3烷基; R 1和R 2相同或不同，代表氢或C 1-4烷基，条件是只有在n高于5的情况下，两者均可表示氢; 或R 1和R 2一起表示含有5至7个碳原子的α，ω-亚烷基，所述亚烷基的末端碳原子与相同的环碳原子结合; n为4,5,6或7; 和 - ＆cir＆_-＆cir＆_-＆cir＆_ bond line代表单一或双重债券。此外，本发明涉及含有这些化合物的药物组合物以及制备通式（I）化合物的方法。通式（I）的化合物发挥5α-还原酶抑制作用，因此它们可用于治疗所有疾病，其目的是减少组织二氢睾酮水平，例如良性前列腺增生，痤疮，皮脂溢，女性多毛症或雄激素性脱发。

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