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. 发明公开

EP0055999A2 Vitamin D3 失效
标题翻译：维生素D3。
公开(公告)号：EP0055999A2
公开(公告)日：1982-07-14
申请号：EP82200223.4
申请日：1980-02-14
申请人： TEIJIN LIMITED
发明人： Nishikawa, Osamu , Ishimaru, Kenji , Takeshita, Toru , Tsuruta, Hideki
IPC分类号： C07C172/00 , A61K31/59
CPC分类号： C07J17/00 , C07J9/00
摘要： The novel 25-hydroxy-24-oxocholecalciferol of formula [1]
the novel 1, 25-dihydroxy-24-oxocholecalciferol of formula [2]
process for their preparation, and their use in pharmaceutically active compositions.
摘要翻译：式[1]的新型25-羟基-24-氧代胆钙化甾醇[2]其制备方法的新型1,25-二羟基-24-氧代胆钙化甾醇的方法及其在药物活性组合物中的用途。

2. 发明公开

EP0055999A3 Vitamin D3 失效
标题翻译：维他命D3
公开(公告)号：EP0055999A3
公开(公告)日：1982-09-01
申请号：EP82200223
申请日：1980-02-14
申请人： TEIJIN LIMITED
发明人： Nishikawa, Osamu , Ishimaru, Kenji , Takeshita, Toru , Tsuruta, Hideki
IPC分类号： C07C172/00 , A61K31/59
CPC分类号： C07J17/00 , C07J9/00
摘要： The novel 25-hydroxy-24-oxocholecalciferol of formula [1]
the novel 1, 25-dihydroxy-24-oxocholecalciferol of formula [2]
process for their preparation, and their use in pharmaceutically active compositions.

3. 发明公开

EP0028484A1 Process for the preparation of active-type vitamin D3 compounds and of the cholesta-5,7-diene precursors, and products so obtained 失效
标题翻译：由此获得一种用于生产活性的维生素D 3化合物和胆甾-5,7-二烯前体和产物的过程。
公开(公告)号：EP0028484A1
公开(公告)日：1981-05-13
申请号：EP80303732.4
申请日：1980-10-22
申请人： TEIJIN LIMITED
发明人： Nishikawa, Osamu , Ishimaru, Kenji , Takeshita, Toru , Tsuruta, Hideki
IPC分类号： C07C172/00 , C07J9/00
CPC分类号： C07J9/00 , Y02P20/55 , Y02P20/582
摘要： The present invention relates to a novel process for the preparation of active-type vitamin D 3 compounds and their intermediates. In accordance with the present invention, a large amount of an active-type vitamin D 3 compound, for example 1α-hydroxycholecalciferol, 1α,25-dihydrox- ycholecalciferol and the like, is efficiently prepared with high industrial advantage by a novel process which comprises (i) reacting hydroxycholesta-5-enes having the hydroxyl groups protected with lower alkoxycarbonyl groups as a starting material with an allylic brominating agent and a dehydrobrominating agent to prepare the corresponding hydroxycholesta-5,7-dienes, (ii) exposing the hydroxycholesta-5,7-dienes to ultraviolet irradiation or to a combination of the irradiation with thermal isomerization to obtain a mixture of the unreacted hydroxycholesta-5,7-dienes and previtamin D 3 compounds or a mixture of the unreacted hydroxycholesta-5,7-dienes and the protected active-type vitamin D, compounds, (iii) separating the mixture into the unreacted hydroxycholesta-5,7-dienes and previtamin D 3 compounds or the protected active-type vitamin D 3 compounds, (iv) recycling the unreacted hydroxycholesta-5,7-dienes for reuse and (v) thermally isomerizing the remaining compounds and/or splitting off the protective groups. The process of the invention is of very high industrial value, capable of simple operation and adaptable to large scale commercial production.

4. 发明公开

EP0013082A1 Process for producing steroid compounds having an oxogroup in the side chain 失效
标题翻译：一种用于具有在侧链上具有酮基类固醇的制备方法。
公开(公告)号：EP0013082A1
公开(公告)日：1980-07-09
申请号：EP79302717.8
申请日：1979-11-29
申请人： TEIJIN LIMITED
发明人： Nishikawa, Osamu , Ishimaru, Kenji , Takeshita, Toru , Tsuruta, Hideki
IPC分类号： C07J9/00 , C07F3/06
CPC分类号： C07J9/005 , C07J9/00 , Y02P20/55
摘要： A process for producing a steroid compound having an oxo group in the side chain, which comprises condensing an acid halide having a steroid skeleton with an organozinc compound at a halocarbonyl group of the acid halide in an inert organic medium in the presence of a catalytic amound of an ether capable of forming a complex with the organozinc compound and, if desired, hydrolyzing the product. The process gives the steroid compound in a high yield, and often in an almost quantitative yield. The steroid compound can be an important intermediate for the production of vitamin D 3 analogs, such as active forms of vitamin D 3 .

5. 发明授权

EP0028484B1 Process for the preparation of active-type vitamin D3 compounds and of the cholesta-5,7-diene precursors, and products so obtained 失效
标题翻译：制备活性型维生素D3化合物和氯化镁-5,7-二苯醚前体以及所得产品的方法
公开(公告)号：EP0028484B1
公开(公告)日：1985-08-14
申请号：EP80303732.4
申请日：1980-10-22
申请人： TEIJIN LIMITED
发明人： Nishikawa, Osamu , Ishimaru, Kenji , Takeshita, Toru , Tsuruta, Hideki
IPC分类号： C07C172/00 , C07J9/00
CPC分类号： C07J9/00 , Y02P20/55 , Y02P20/582

6. 发明授权

EP0044541B1 Aminocarboxylic acids, amino alcohols, or the derivatives thereof, processes for production thereof, and pharmaceutical composition, containing at least one of these compounds 失效
标题翻译：氨基羧酸，氨基醇或其衍生物，其生产方法和药物组合物，至少含有这些化合物之一
公开(公告)号：EP0044541B1
公开(公告)日：1983-09-21
申请号：EP81105629.0
申请日：1981-07-17
申请人： TEIJIN LIMITED
发明人： Takeshita, Toru , Hoshina, Kenji , Ohtsu, Akira , Naruchi, Tatsuyuki
IPC分类号： C07C101/34 , C07C101/30 , C07C97/10 , C07C103/32 , C07C101/28 , C07C101/04 , A61K31/195 , A61K31/135
CPC分类号： C07C229/34 , A61K31/135 , C07C225/18 , C07C233/51 , C07C2601/14 , Y10S514/927 , Y10S514/928

7. 发明公开

EP0044541A1 Aminocarboxylic acids, amino alcohols, or the derivatives thereof, processes for production thereof, and pharmaceutical composition, containing at least one of these compounds 失效
标题翻译：氨基羧酸，氨基醇，它们的衍生物，它们的制备方法和含有这些化合物中的至少一种药物制剂。
公开(公告)号：EP0044541A1
公开(公告)日：1982-01-27
申请号：EP81105629.0
申请日：1981-07-17
申请人： TEIJIN LIMITED
发明人： Takeshita, Toru , Hoshina, Kenji , Ohtsu, Akira , Naruchi, Tatsuyuki
IPC分类号： C07C101/34 , C07C101/30 , C07C97/10 , C07C103/32 , C07C101/28 , C07C101/04 , A61K31/195 , A61K31/135
CPC分类号： C07C229/34 , A61K31/135 , C07C225/18 , C07C233/51 , C07C2601/14 , Y10S514/927 , Y10S514/928
摘要： A compound represented by the following formula
wherein R 1 represents a hydrogen atom, an acyl group or an alkoxycarbonyl group; X 1 represents an alkylene group having 3 to 6 carbon atoms, a 1,4-cyclohexylene group, or a 1,4-phenylene group, the alkylene group may be substituted by an alkyl group having 1 to 6 carbon atoms, and the 1,4-phenylene group may be substituted by 1 or 2 substituents selected from halogen atoms and alkoxy groups having 1 to 6 carbon atoms; R 2 represents a hydrogen atom or a hydroxyl group and R 3 represents hydrogen atom, or R 2 and R 3 together may form an oxo group (=0), and when X 1 is other than the 1,4-phenylene group, R 2 represents a hydrogen atom and R 3 represents a bond between the carbon atom to which R 3 is bonded and that carbon atom of X 1 which is adjacent to said carbon atom; X 2 represents an alkylene group having 1 to 5 carbon atoms which may be substituted by an alkyl group having 1 to 6 carbon atoms or an amino group; and R 4 represents the group -COOR 5 , -CH 2 OR 6 or -CONR 7 R 8 in which R 5 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, R 6 represents a hydrogen atom or an acyl group having 1 to 6 carbon atoms, and R 7 and R B are identical or different and represent a hydrogen atom or an alkyl group having 1 to 6 carbon atoms or taken together may form a 5- or 6- membered ring;

or an acid addition salts of said compound wherein R 1 represents a hydrogen atom or X 2 represents an alkylene group having an amino group, or a salts of said compound wherein R 5 represents a hydrogen atom.

The compound represented by the above formula or its pharmaceutically acceptable salt is useful as an anti-ulcer agent.
The present invention also provides a process for producing the compound or its pharmaceutically acceptable salt, which comprises acylating a protected derivative at the amino group of a corresponding acid halide with a corresponding substituted benzene in the presence of a Lewis acid; or reducing a corresponding compound in the presence of an inert solvent under conditions which induce reduction of the carbonyl group of said corresponding compound without substantially reducing the phenylene group of said corresponding compound; or dehydrating a corresponding compound.
摘要翻译：由下式 worin R1 darstellt的氢原子的酰基或烷氧羰基所示的化合物; 具有3至6个碳原子的亚烷基基团的X1 darstellt，1,4-亚环己基或1,4-亚苯基，该亚烷基基团可以通过在具有1至6个碳原子的烷基substituiertem，和1， 1,4-亚苯基可以被具有1至6个碳原子选自卤素原子1个或2个取代基和烷氧基取代; R2 darstellt氢原子或羟基基团和R3 darstellt氢原子，或R2和R3一起可以形成于（= O）氧代基团，并且当X1比1,4-亚苯基等，R 2 darstellt氢原子和 R3 darstellt的碳原子其中R 3之间的键结合并做X1所有其相邻于所述碳原子的碳原子; 在具有1至5个碳原子可被在具有1至6个碳原子，或氨基烷基取代的亚烷基X2 darstellt; 并且R 4表示基团-COOR 5，-CH2OR6或-CONR 7 R 8，其中R 5 darstellt氢原子或烷基具有1至6个碳原子基团，R6表示具有1至6个碳原子的氢原子或酰基，和R 7和 R相同或不同，表示氢原子或烷基具有1至6个碳原子基团或一起可以形成5-或6-元环; 或worin R1表示具有氨基的亚烷基的氢原子或X2 darstellt，或worin R5 darstellt氢原子的所述化合物的盐，所述化合物的酸加成盐。由上述式或药学上可接受的盐表示的化合物及其可用作抗溃疡剂是有用的。因此，本发明提供了用于生产所述化合物或其药学上可接受的盐及其，该方法包括酰化在氨基与在路易斯酸的存在下，相应substituiertem苯相应的酰卤的被保护的衍生物的方法; 或减少在惰性溶剂中的诱导减少。所述的相应的化合物的羰基而基本上不减少所述相应化合物的亚苯基条件下在存在相应的A化合物; 或脱水相对应的化合物。

8. 发明授权

EP0092004B1 Novel vitamin D3 derivatives, processes for preparation thereof, and antigens comprising said derivatives to be used for preparation of antibodies for immunochemical assay and antibodies prepared therefrom 失效
标题翻译：新维生素D3衍生物，其制备方法和包含用于制备用于免疫化学测定的抗体的所述衍生物的抗体和其制备的抗体
公开(公告)号：EP0092004B1
公开(公告)日：1985-10-30
申请号：EP82302015.1
申请日：1982-04-20
申请人： TEIJIN LIMITED
发明人： Oshida, Jun-ichi , Nishikawa, Osamu , Ishimaru, Kenji , Tsuruta, Hideki , Takeshita, Toru , Yamamoto, Itaru
IPC分类号： C07C172/00 , C07K17/00 , C07J9/00 , G01N33/82
CPC分类号： C07J9/00 , G01N33/82

9. 发明公开

EP0092004A1 Novel vitamin D3 derivatives, processes for preparation thereof, and antigens comprising said derivatives to be used for preparation of antibodies for immunochemical assay and antibodies prepared therefrom 失效
标题翻译：，它们的制备方法和含有这些衍生物根据需要用于制备抗体的免疫化学试验方法维生素D3衍生物和由其抗体制备的抗原。
公开(公告)号：EP0092004A1
公开(公告)日：1983-10-26
申请号：EP82302015.1
申请日：1982-04-20
申请人： TEIJIN LIMITED
发明人： Oshida, Jun-ichi , Nishikawa, Osamu , Ishimaru, Kenji , Tsuruta, Hideki , Takeshita, Toru , Yamamoto, Itaru
IPC分类号： C07C172/00 , C07K17/00 , C07J9/00 , G01N33/82
CPC分类号： C07J9/00 , G01N33/82
摘要： he present invention relates to novel vitamin D 3 derivatives which have a carboxyl group or its ester group at the 22-position, processes for the preparation thereof, and antigens, which comprise said vitamin D 3 derivative and an immunogenic carrier material, to be used for the preparation of antibodies for enzymeimmunoassay or radioimmunoassay and antibodies obtained therefrom.
The determination of such activated vitamin D 3 compounds as 25-hydroxy vitamin D 3 , 24,25-dihydroxy vitamin D., etc. can be made satisfactorily according to the present invention.
摘要翻译：本发明涉及一种具有羧基，或在22位上的酯基团新的维生素D3衍生物，其制备工艺，和抗原，其包含所述维生素D3衍生物和免疫原性载体物质，所用的制备抗体酶联或放射免疫测定法和抗体的从那里得到。的调查活性型维生素D 3化合物为25-羟基维生素D3，24,25-二羟基维生素D3等的确定能满意地制成gemäß到了本发明。

10. 发明授权

EP0015122B1 New 25-hydroxy-24-oxocholestane derivatives and preparation thereof 失效
标题翻译：新型25-羟基-24-氧代醇衍生物及其制备方法
公开(公告)号：EP0015122B1
公开(公告)日：1983-09-14
申请号：EP80300426.6
申请日：1980-02-14
申请人： TEIJIN LIMITED
发明人： Nishikawa, Osamu , Ishimaru, Kenji , Takeshita, Toru , Tsuruta, Hideki
IPC分类号： C07J9/00
CPC分类号： C07J17/00 , C07J9/00

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