专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO1997042152A1 VITAMIN D ANALOGS AND METHODS OF PREPARING THESE COMPOUNDS 审中-公开
标题翻译：维生素D类似物和制备这些化合物的方法
公开(公告)号：WO1997042152A1
公开(公告)日：1997-11-13
申请号：PCT/EP1997002429
申请日：1997-05-02
申请人： DUPHAR INTERNATIONAL RESEARCH B.V. , HALKES, Sebastian , VAN DE VELDE, Jan, Paul , KANZLER, Silvia , REISCHL, Wolfgang
发明人： DUPHAR INTERNATIONAL RESEARCH B.V.
IPC分类号： C07C33/38
CPC分类号： C07C33/38 , C07C2602/08
摘要： The invention relates to vitamin D analogs of general formula (I) wherein: R1 is a hydrogen atom or a substituent selected from the group consisting of hydroxy, CH2OH, CH2CH2OH, CH2CH2CH2OH, OCH3, OCH2OH, OCH2CH2OH and OCH2CH2CH2OH; R2 is a hydrogen atom or a substituent selected from the group consisting of OCH3, OCH2OH, CHm(CH2OH)n(CH2CH2OH)p, (CH2)qOH and O(CH2)rOH; wherein: m is 0 or 1, p, q and n are 0-3, r is 1-3 and m+n+p=3; with the proviso that R1 and/or R2 contain at least one OH group; R3 is a straight or branched, saturated or unsaturated aliphatic hydrocarbon of 6-13 C atoms which may be substituted with one or more substituents from the group hydroxy or fluoro. The invention further relates to methods of preparing these compounds, a pharmaceutical composition containing these compounds and to their use in pharmacotherapy and cosmetics.
摘要翻译：本发明涉及通式（I）的维生素D类似物，其中：R 1是氢原子或选自羟基，CH 2 OH，CH 2 CH 2 OH，CH 2 CH 2 CH 2 OH，OCH 3，OCH 2 OH，OCH 2 CH 2 OH和OCH 2 CH 2 CH 2 OH的取代基; R2是氢原子或选自OCH3，OCH2OH，CHm（CH2OH）n（CH2CH2OH）p，（CH2）qOH和O（CH2）rOH的取代基; 其中：m为0或1，p，q和n为0-3，r为1-3，m + n + p = 3; 条件是R1和/或R2含有至少一个OH基团; R3是6-13个碳原子的直链或支链饱和或不饱和脂族烃基，其可以被一个或多个羟基或氟取代基取代。本发明还涉及制备这些化合物的方法，含有这些化合物的药物组合物及其在药物治疗和化妆品中的用途。

2. 发明申请

WO1997036893A1 PIPERAZINE AND PIPERIDINE COMPOUNDS 审中-公开
标题翻译：哌嗪和哌啶化合物
公开(公告)号：WO1997036893A1
公开(公告)日：1997-10-09
申请号：PCT/EP1997001461
申请日：1997-03-20
申请人： DUPHAR INTERNATIONAL RESEARCH B.V. , FEENSTRA, Roelof, Willem , KRUSE, Cornelis, Gerrit , TULP, Martinus, Theodorus, Maria , KUIPERS, Wilma , LONG, Stephen, Kenneth
发明人： DUPHAR INTERNATIONAL RESEARCH B.V.
IPC分类号： C07D405/04
CPC分类号： C07D263/58 , C07D209/08 , C07D215/12 , C07D265/36 , C07D307/79 , C07D311/18 , C07D317/66 , C07D319/08 , C07D319/18 , C07D321/10 , C07D327/06 , C07D333/54 , C07D405/04 , C07D407/10 , C07D409/10 , C07D413/10
摘要： The invention relates to a group of new piperazine and piperidine compounds having interesting pharmacological properties. It has been found that compounds of formula (a) wherein A represents a heterocyclic group of 5-7 ring atoms wherein 1-3 heteroatoms from the group O, N and S are present; R1 is hydrogen or fluoro; R2 is C1-4-alkyl, C1-4-alkoxy or an oxo group, and p is 0, 1 or 2; Z represents carbon or nitrogen, and the dotted line is a single bond when Z is nitrogen, and a single or double bond when Z is carbon; R3 and R4 independently are hydrogen or C1-4-alkyl; n has the value 1 or 2; R5 is halogen, hydroxy, C1-4-alkoxy or C1-4-alkyl, and q is 0, 1, 2 or 3; Y is phenyl, furanyl or thienyl, which groups may be substituted with 1-3 substituents of the group hydroxy, halogen, C1-4-alkoxy, C1-4-alkyl, cyano, aminocarbonyl, mono- or di-C1-4-alkylaminocarbonyl; and salts thereof show high affinity for both the dopamine D2 and serotonin 5-HT1A receptors.
摘要翻译：本发明涉及具有感兴趣的药理学性质的一组新的哌嗪和哌啶化合物。已经发现，其中A表示5-7个环原子的杂环基的式（a）化合物，其中存在1-3个来自O，N和S基团的杂原子; R1是氢或氟; R 2是C 1-4 - 烷基，C 1-4 - 烷氧基或氧代基，p是0,1或2; Z表示碳或氮，当Z为氮时，虚线为单键，Z为碳时为单键或双键; R3和R4独立地是氢或C1-4烷基; n的值为1或2; R5是卤素，羟基，C1-4烷氧基或C1-4烷基，q是0,1,2或3; Y是苯基，呋喃基或噻吩基，它们可以被1-3个羟基，卤素，C 1-4 - 烷氧基，C 1-4 - 烷基，氰基，氨基羰基，单 - 或二-C 1-4 - 烷基氨基; 其盐对多巴胺D2和5-羟色胺5-HT 1A受体表现出高亲和力。

3. 发明申请

WO1994004683A1 BORDETELLA BRONCHISEPTICA VACCINE 审中-公开
公开(公告)号：WO1994004683A1
公开(公告)日：1994-03-03
申请号：PCT/NL1993000161
申请日：1993-07-28
申请人： DUPHAR INTERNATIONAL RESEARCH B.V. , SAVELKOUL, Paul, H., M. , GAASTRA, Willem
发明人： DUPHAR INTERNATIONAL RESEARCH B.V.
IPC分类号： C12N15/31
CPC分类号： C07K14/235 , A61K39/00
摘要： The present invention is concerned with a vaccine for combating B. bronchiseptica infection in susceptible animals (such as dogs and swine), containing proteins or polypeptides typical of the fimbrial protein of B. bronchiseptica, or containing recombinant polynucleotides having as part thereof a polynucleotide coding for said protein or polypeptide, and also is concerned with the preparation of said proteins, polypeptides and polynucleotides.
摘要翻译：本发明涉及用于在易感动物（例如狗和猪）中对抗支气管扩张支原体感染的疫苗，其包含典型的支气管炎支原体蛋白的蛋白质或多肽，或含有重组多核苷酸，其具有作为其部分的多核苷酸编码对于所述蛋白质或多肽，并且还涉及所述蛋白质，多肽和多核苷酸的制备。

4. 发明申请

WO1998013029A1 ORAL DELAYED IMMEDIATE RELEASE FORMULATION AND METHOD OF PREPARATION THEREFOR 审中-公开
标题翻译：口服延迟立即释放配方及其制备方法
公开(公告)号：WO1998013029A1
公开(公告)日：1998-04-02
申请号：PCT/EP1997005234
申请日：1997-09-18
申请人： DUPHAR INTERNATIONAL RESEARCH B.V. , VAN BALKEN, Paulus, Maria , ELBERS, Jules, Alex, Cornelis , FRIJLINK, Henderik, Willem , PHILIPS, Wienman, Emerald
发明人： DUPHAR INTERNATIONAL RESEARCH B.V.
IPC分类号： A61K09/28
CPC分类号： A61K39/145 , A61K9/282 , A61K9/2866 , A61K9/4808 , A61K39/00 , A61K39/12
摘要： The invention relates to an Oral Delayed Immediate Release formulation comprising a compressed core containing one or more active substances surrounded with a coating, wherein release of active substance from the core is caused by rupture of the coating after a definite lag-time, said core comprising one or more immediate release carriers and having no substantial swelling properties upon exposure to gastrointestinal fluids. The invention further relates to formulations containing an Immediate Release formulation combined with one or more Oral Delayed Immediate Release formulations with different lag-times and to a method of preparing an Oral Delayed Immediate Release formulation. The Oral Delayed Immediate Release formulation may be used for the application of active substances whenever a certain lag-time before release is advantageous, such as in the case of anti-asthmatics, anti-emetics, cardiotonics, vasodilators, anti-vertigo and anti-ménière compounds, anti-hypertensives, sedatives, anti-depressants, anti-anxiety compounds, cortico-steroids, general anti-inflammatory compounds, anti-inflammatory compounds for gastrointestinal use, anti-ulceratives, analgetics, anti-aritmics, anti-rheumatics, anti-arthritic compounds and anti-angina compounds. The Oral Delayed Immediate Release formulation may also be used for the application of biological active compounds such as proteins, peptides, enzymes, vaccines and oligonucleotides.
摘要翻译：本发明涉及一种口服延迟的立即释放制剂，其包含含有被涂层包围的一种或多种活性物质的压缩核心，其中活性物质从核心中释放是由确定滞后时间之后的涂层破裂引起的，所述核心包含一种或多种立即释放载体，并且在暴露于胃肠液体时没有显着的溶胀特性。本发明还涉及含有立即释放制剂与一种或多种具有不同滞后时间的口服延迟立即释放制剂组合的制剂以及制备口服延迟立即释放制剂的方法。口服延迟即时释放制剂可以用于活性物质的应用，每当释放前的某个滞后时间是有利的，例如在抗哮喘，抗排毒，强心剂，血管扩张剂，抗眩晕和抗眩晕药物的情况下，化合物，抗高血压药，镇静剂，抗抑郁药，抗焦虑药，皮质类固醇，一般抗炎化合物，消化道用抗炎化合物，抗溃疡药，止痛剂，抗神经药，抗风湿药，抗关节炎化合物和抗心绞痛化合物。口服延迟即时释放制剂也可用于生物活性化合物如蛋白质，肽，酶，疫苗和寡核苷酸的应用。

5. 发明申请

WO1995019963A1 NEW PHARMACOTHERAPEUTICALLY ACTIVE COMPOUNDS 审中-公开
标题翻译：新药物活性化合物
公开(公告)号：WO1995019963A1
公开(公告)日：1995-07-27
申请号：PCT/NL1995000031
申请日：1995-01-23
申请人： DUPHAR INTERNATIONAL RESEARCH B.V. , KUTNER, Andrzej , ZHAO, Hong , FITAK, Hanna , CHODYN'SKI, Michael , HALKES, Sebastianus, J. , WILSON, Stephen, R. , VAN DEL VELDE, Jan-Paul
发明人： DUPHAR INTERNATIONAL RESEARCH B.V.
IPC分类号： C07C403/08
CPC分类号： C07C403/08 , C07B2200/07 , C07C45/30 , C07C401/00 , C07C2601/14 , C07C2601/16 , C07F9/532 , C07C47/19
摘要： The invention relates to a compound of general formula (I), wherein R1, R2, R4, R5 and R6 are each individually hydrogen atoms or methyl groups; R3 represents a methyl group or a methylene group; R7 and R8 are each individually straight or branched alkyl groups having 1 to 4 carbon atoms or cycloalkyl groups having 3 to 6 carbon atoms; Z is a hydrogen atom or a hydroxy group; n is an integer from 0 to 3; and the (a) bonds represent single or double carbon - carbon bonds; with the provisos: (1) that no cumulated double bonds are present in the molecule; (2) that either R3-C10, C5-C6 and C7-C8 or C10-C5, C6-C7 and C8-C9 form double bonds, with which optionally present additional double bonds are conjugated; and (3) that R3 represents a methyl group if R3-C10 is a single bond, and a methylene group if R3-C10 is a double bond. The invention also relates to a method of preparing this compound and to its use for the treament and/or prevention of certain disorders and diseases.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1，R 2，R 4，R 5和R 6各自为氢原子或甲基; R3表示甲基或亚甲基; R 7和R 8各自为具有1至4个碳原子的直链或支链烷基或具有3至6个碳原子的环烷基; Z是氢原子或羟基; n为0〜3的整数。（a）债券代表单一或双重碳 - 碳键; 条件是：（1）分子中不存在累积双键; （2）R3-C10，C5-C6和C7-C8或C10-C5，C6-C7和C8-C9形成双键，任选地存在额外的双键被共轭; 和（3）如果R3-C10是单键，则R3表示甲基，如果R3-C10是双键，则表示亚甲基。本发明还涉及一种制备该化合物的方法及其用于治疗和/或预防某些疾病和疾病的用途。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式