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21. 发明授权

US3788947A Microbiological reduction of10(11)unsaturated prostaglandins 失效
标题翻译：微生物减少10（11）不饱和前列腺素
公开(公告)号：US3788947A
公开(公告)日：1974-01-29
申请号：US3788947D
申请日：1972-10-05
申请人： SEARLE & CO
发明人： HSU C , JIU J , MIZUBA S
IPC分类号： C07C67/00 , C07C401/00 , C07C405/00 , C12P31/00 , C12D1/02
CPC分类号： C12P31/00 , C07C405/00 , Y10S435/822 , Y10S435/838 , Y10S435/849 , Y10S435/873 , Y10S435/911 , Y10S435/913 , Y10S435/915 , Y10S435/917 , Y10S435/918 , Y10S435/925 , Y10S435/929 , Y10S435/931 , Y10S435/933
摘要： THE PRESENT INVENTION RELATES TO FERMENTATIVE REDUCTION OF THE 10(11) DOUBLE BOND OF PGA-TYPE PROSTAGLANDINS. MORE PARTICULARLY, THE INVENTION PROVIDES A PROCESS FOR SELECTIVE 10(1) DOUBLE BOND REDUCTION OF PGA2 BY FUNGI OF GENERA CUNNINGHAMELLA, MUCOR, POLYPORUS, SPHAEROPSIS, STEMPHYLIUM, CLADOSPORIUM, HORMODENDRUM, EPICOCCIUM, FUSARIUM, GLIOCLADIUM, DACTYLIUM, CEPHALOSPORIUM, ASPERGILLUS, AND PENCILLIUM. THE SAME TRANSFORMATION IS ACCOMPLISHED BY BACTERIA OF GENERA BACILLUS, EN TEROBACTER, ESCHERICHIA, AND PROTEUS.

22. 发明授权

US3773622A Method for preparing 2-substituted-4-hydroxy-cyclopentane-1,3-diones 失效
标题翻译：制备2-取代-4-羟基 - 环戊烷-1,3-二酮的方法
公开(公告)号：US3773622A
公开(公告)日：1973-11-20
申请号：US3773622D
申请日：1972-09-29
申请人： WISCONSIN ALUMNI RES FOUND
发明人： SIH C
IPC分类号： C12P7/38 , C07C45/00 , C07C49/493 , C07C67/00 , C07C405/00 , C12P7/00 , C12P7/62 , C12P31/00 , C12D13/00
CPC分类号： C12P31/00 , C07C405/00 , Y10S435/911 , Y10S435/912 , Y10S435/913 , Y10S435/919 , Y10S435/93 , Y10S435/931 , Y10S435/933 , Y10S435/94 , Y10S435/942 , Y10S435/944 , Y10S435/945
摘要： A method for preparing optically active 2-substituted-4-hydroxycyclopentane-1,3-diones by subjecting 2-substituted cyclopentane1,3,4-trione or 2-substituted-3-alkoxy-2-cyclopentene-1,4-dione to the fermentative enzymatic action of microorganisms of the orders Endomycetales, Mucorales, Moliliales and Eurotiales.

23. 发明授权

US3725469A Prostanoic acid derivatives 失效
标题翻译：普鲁卡因酸衍生物
公开(公告)号：US3725469A
公开(公告)日：1973-04-03
申请号：US3725469D
申请日：1970-03-23
申请人： UPJOHN CO
发明人： NELSON J
IPC分类号： C07C405/00 , C12P31/00 , C07C61/36
CPC分类号： C07C405/00 , C12P31/00 , Y10S514/927 , Y10S514/929
摘要： WHEREIN R1 is hydrogen or a pharmacologically acceptable cation, essentially free of pyrogens, antigens, proteins, enzymes, cellular material, and other organic acids or salts thereof. These compounds are useful as vasodepressors and antisecretory agents.

This invention is a group of compounds of the formula:
摘要翻译：本发明是一组下式的化合物：

24. 发明授权

US3691216A Pge2 methyl ester and pge2 methyl ester diacetate 失效
标题翻译： PGE2甲基酯和PGE2甲基酯
公开(公告)号：US3691216A
公开(公告)日：1972-09-12
申请号：US3691216D
申请日：1971-02-12
申请人： SUNE BERGSTROM , JAN SJOVALL
发明人： BERGSTROM SUNE , SJOVALL JAN
IPC分类号： B01J23/42 , C07C405/00 , C12P31/00 , C07C69/74
CPC分类号： C12P31/00 , B01J23/42 , C07C405/00 , C07C405/0016 , Y10S514/935
摘要： The prostaglandins PGE2 methyl ester and PGE2 methyl ester diacetate are disclosed. These novel compounds are useful for a variety of pharmacological purposes, including use as smooth muscle stimulants and as cardiovascular agents.

25. 发明授权

US3598858A Pge2 and pge3 失效
标题翻译： PGE2和PGE3
公开(公告)号：US3598858A
公开(公告)日：1971-08-10
申请号：US3598858D
申请日：1962-06-20
申请人： SUNE BERGSTROM , JAN SJOVALL
发明人： BERGSTROM SUNE , SJOVALL JAN
IPC分类号： B01J23/42 , C07C405/00 , C12P31/00 , C07C69/74
CPC分类号： C12P31/00 , B01J23/42 , C07C405/00 , C07C405/0016 , Y10S514/935
摘要： PGE2, PGE3, THEIR SALTS AND ESTERS FREE OF ANTIGENS AND PYROGENS. PGE TYPE COMPOUNDS EXHIBIT BLOOD PRESSURE LOWERING AND SMOOTH MUSCLE STIMULATING PROPERTIES.
摘要翻译：公开了前列腺素PGF2α和PGF2β及其盐，酯和链烷酸酯。这些新型化合物可用于各种药理学目的，包括用作平滑肌兴奋剂和用作心血管药物。

26. 发明授权

US09346738B2 Process for the preparation of treprostinil and derivatives thereof 有权
标题翻译：制备曲前列环素及其衍生物的方法
公开(公告)号：US09346738B2
公开(公告)日：2016-05-24
申请号：US14401826
申请日：2013-05-22
申请人： SciPharm SàRL
发明人： Nareshkumar Jain , Michael Kirkup , Michael Marella , Sanjeevani Ghone
IPC分类号： C07C59/115 , C07C51/377 , C07C47/565 , C07C47/575 , C07F7/18 , C07C59/72 , C12P31/00 , C12P41/00
CPC分类号： C07C51/377 , C07C47/565 , C07C47/575 , C07C59/72 , C07C2603/14 , C07F7/18 , C07F7/1804 , C07F7/1892 , C12P31/00 , C12P41/002 , C12P41/004
摘要： A method for the preparation of treprostinil and its derivatives is described. In contrast to prior art, this method utilizes an easily scalable enzymatic resolution of a key intermediate for making these compounds. Another significant improvement of the described method over prior methods is the regioselective Claisen rearrangement of a 5-allyloxy-benzaldehyde precursor, which is facilitated by a bromo substituent in 2-position.
摘要翻译：描述了曲前列素及其衍生物的制备方法。与现有技术相反，该方法利用关键中间体易于扩展的酶分解来制备这些化合物。所述方法与现有方法的另一重大改进是5-烯丙氧基 - 苯甲醛前体的区域选择性Claisen重排，其由2-位的溴取代基促进。

27. 发明授权

US07605144B2 Enzyme catalyzed therapeutic compounds 失效
标题翻译：酶催化治疗化合物
公开(公告)号：US07605144B2
公开(公告)日：2009-10-20
申请号：US10681418
申请日：2003-10-07
申请人： H. Michael Shepard , Ming Fai Chan , Michael P. Groziak
发明人： H. Michael Shepard , Ming Fai Chan , Michael P. Groziak
IPC分类号： A61K31/70 , C07H19/10 , C12Q1/66 , C12P29/00 , C12P31/00
CPC分类号： C07H19/06
摘要： This invention provides novel compounds selected from the group consisting of a 1,5-substituted pyrimidine derivative or analog and substituted furano-pyrimidone analogs. The compounds are useful to treat or prevent diseases such as cancer.
摘要翻译：本发明提供了选自1,5-取代的嘧啶衍生物或类似物和取代的呋喃 - 嘧啶酮类似物的新化合物。该化合物可用于治疗或预防诸如癌症的疾病。

28. 发明授权

US07169580B1 Protein having PGE2 synthase activity and use thereof 失效
公开(公告)号：US07169580B1
公开(公告)日：2007-01-30
申请号：US10182233
申请日：2000-08-25
申请人： Ichiro Kudo , Makoto Murakami , Sachiko Oh-ishi
发明人： Ichiro Kudo , Makoto Murakami , Sachiko Oh-ishi
IPC分类号： C12P31/00 , C12N9/02 , A61K31/19
CPC分类号： C12N9/90 , A61K38/00
摘要： A single protein which is the substance of the PGE2 synthesis activity in brain soluble fractions of LPS administered rats has been purified and identified. The protein has an activity of synthesizing PGE2 from PGH2, and further, has an activity of synthesizing PGE2 from arachidonic acid in combination with COX.

29. 发明授权

US4711842A Method for production of biologically active substances 失效
标题翻译：生物活性物质生产方法
公开(公告)号：US4711842A
公开(公告)日：1987-12-08
申请号：US589832
申请日：1984-03-15
申请人： Tadayoshi Taniyama , Koichi Yoshida
发明人： Tadayoshi Taniyama , Koichi Yoshida
IPC分类号： C12N15/02 , C07K14/525 , C07K14/545 , C12N5/10 , C12N5/16 , C12P21/00 , C12P31/00 , C12N15/00
CPC分类号： C07K14/525 , C07K14/545 , C12N5/163
摘要： A method of producing biologically active substances using a hybrid cell line obtained by fusing (1) a human tumor cell line which does not grow in a medium containing aminopterin or/and azaserine or cell line derived therefrom with (2) a human non-tumor macrophage. The human tumor macrophage cell line may be either a thymidine kinase-deficient cell line of U-937 or a thymidine kinase-deficient cell line of THP-1, the non-tumor macrophage may be alveolar macrophage, splenic macrophage, peripheral blood monocyte, peritoneal macrophage, hepatic macrophage, placental macrophage, or thymic macrophage, and the biologically active substance produced is a tumoricidal substance or interleukin-1.
摘要翻译：使用通过将（1）在含有氨基蝶呤或/和重氮丝氨酸或其衍生物的细胞系的培养基中不生长的人肿瘤细胞系与（2）人类非肿瘤融合而得到的杂交细胞系的生产活性物质的制造方法巨噬细胞人肿瘤巨噬细胞系可能是U-937的胸苷激酶缺陷型细胞系或THP-1的胸苷激酶缺陷型细胞系，非肿瘤巨噬细胞可能是肺泡巨噬细胞，脾巨噬细胞，外周血单核细胞，腹膜巨噬细胞，肝巨噬细胞，胎盘巨噬细胞或胸腺巨噬细胞，产生的生物活性物质是杀肿瘤物质或白介素-1。

30. 发明授权

US4190670A Prostaglandin derivatives 失效
公开(公告)号：US4190670A
公开(公告)日：1980-02-26
申请号：US831949
申请日：1977-09-09
申请人： Arthur F. Marx , Jean Doodewaard
发明人： Arthur F. Marx , Jean Doodewaard
IPC分类号： C07C405/00 , C07F1/00 , C07F1/08 , C12P31/00 , C07C177/00
CPC分类号： C12P31/00 , C07C405/00 , C07F1/00 , C07F1/08
摘要： Novel 18.xi.-, 19.xi.- and 20.xi.-hydroxy-prostaglandin derivatives of the formula I ##STR1## wherein the dotted line in the position 8-12 indicates the optional presence of a double bond, the waved lines in position 15 indicate that the hydroxyl group and the group R.sub.4 are either in .alpha.- or .beta.-position and Z represents a --CH.sub.2 CH.sub.2 -- or a cis --CH.dbd.CH-- group, and wherein R represents one of the groups: ##STR2## (wherein the waved lines indicate that the hydroxyl groups are either in .alpha.- or .beta.-position and R.sub.1 represents a hydrogen atom, a methyl or ethyl group), R.sub.2 represents either an oxygen atom or a hydrogen atom and an .alpha.- or .beta.-hydroxyl group, R.sub.3 represents a hydrogen atom or a hydroxyl group and R.sub.4 represents a hydrogen atom or a methyl group, with the proviso that when simultaneously, R.sub.1, R.sub.3 and R.sub.4 each represents a hydrogen atom, R.sub.2 represents an oxygen atom, a double bond is in 8-12 position and the 15-hydroxyl group is in position .alpha., R does not represent the group (b), but that when in addition to these conditions, Z represents a cis --CH.dbd.CH-- group and the 8-12 position is saturated, R either represents the groups (b) or (c); and the pharmaceutically acceptable salts and esters thereof, novel process for their preparation by selective microbiological hydroxylation of compounds formula II ##STR3## wherein the dotted line in the position 10-11 indicates the optional presence of a double bond in case the 8-12 position is saturated and the other symbols are as defined hereinabove, by means of microorganisms of the Division of Eumycota or, as far as the introduction of a hydroxyl group in the 18- or 19-position is concerned, of the Family of Streptomycetaceae, and, if desired, conversion of the 18.xi.-, 19.xi.- and 20.xi.-hydroxy-prostaglandin derivatives thus obtained into pharmaceutically acceptable salts and esters thereof, and pharmaceutical compositions containing at least one of the novel hydroxy-prostaglandin derivatives of formula I.

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