| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 181 | Pgf tetraols and alkanoyl esters | US28295272 | 1972-08-23 | US3852337A | 1974-12-03 | BERGSTROM S; SJOVALL J |
| There are disclosed compounds of the formula:
WHEREIN Y is -CH2CH2- or trans-CH CH-, and both X and Z are CH2CH2-, or wherein Y is trans-CH CH-, X is cis-CH CH-, and Z is -CH2CH2- or cis-CH CH-, wherein R is hydrogen or lower alkanoyl, and wherein * indicates attachment of -OR to the ring in alpha or beta configuration. These novel compounds are useful for a variety of pharmacological purposes, including use as smooth muscle stimulants. |
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| 182 | Process for producing prostaglandins | US35871073 | 1973-05-09 | US3843467A | 1974-10-22 | SKARNES R; HOWARD L |
| 1. A PROCESS FOR THE BIOSYNTHESIS OF PROSTAGLANDINS, COMPRISING THE STEPS OF (A9 GROWING THE BACTERIUM PSEUDOMONAS AERUGINOSA IN THE PRESENCE OF OXYGEN IN A CULTURE MEDIUM ESSENTIALLY FREE OF FATTY ACIDS AND CONTAINING AVAILABLE NITROGEN AND CARBON THEREBY TO FOM PROSTAGLANDINS; AND (B) ISOLATING THE PRODUCT PROSTAGLANDING THUS FORMED.
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| 183 | Pge3 esters and alkanoates | US36767873 | 1973-06-06 | US3839409A | 1974-10-01 | BERGSTROM S; SJOVALL J |
| 1. A COMPOUND OF THE FORMULA:
1-(O=),2-(R3-OOC-(CH2)3-CH=CH-CH2-),3-(CH3-(CH2)4- CH(-O-R2)-CH=CH-),4-(R2-O-)CYCLOPENTANE WHEREIN R3 IS HYDROCARBYL OF ONE TO 13 CARBON ATOMS, INCLUSIVE, AND R2 IS HYDROGEN OR LOWER ALKANOYL. |
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| 184 | Pgf1beta | US3796741D | 1972-07-03 | US3796741A | 1974-03-12 | BERGSTROM S; SJOVALL J |
| THE PROTASGLANDIN PGF1B, AND ITS SALTS, ESTERS, AND ALKANOATES ARE DISCLOSED. THESE NOVEL COMPOUNDS ARE USEFUL FOR A VARIETY OF PHARMACOLOGICAL PURPOSES, INCLUDING USE AS SMOOTH MUSCLE STIMULANTS AND AS CARDIOVASCULAR AGENTS.
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| 185 | Dihydro-pgf1beta | US3796740D | 1972-07-03 | US3796740A | 1974-03-12 | BERGSTROM S; SJOVALL J |
| THE PROSTAGLANDIN DIHYDRO-PGF1B, AND ITS SATLS, ESTERS, AND ALKONATES ARE DISCLOSED. THESE NOVEL COMPOUNDS ARE USEFUL FOR A VARIETY OF PHARMACOLOGICAL PURPOSES, INCLUDING USE AS SMOOTH MUSCLE STIMULTANTS AND AS CARDIOVASCULAR AGENTS.
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| 186 | Method for preparing 2-substituted-4-hydroxy-cyclopentane-1,3-diones | US3773622D | 1972-09-29 | US3773622A | 1973-11-20 | SIH C |
| 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.
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| 187 | Preparation of prostaglandins | US3579425D | 1969-08-29 | US3579425A | 1971-05-18 | DORP DAVID ADRIAAN VAN; BEERTHUIS ROELOF KAREL; NUGTEREN DIEDERIK HENDRIK; VONKEMAN HENDRIK |
| THE SPECIFICATION DISCLOSES A PROCESS FOR PREPARING PROSTAGLANDINS WHICH COMPRISES INCUBATING, UNDER AEROBIC CONDITIONS, A MIXTURE COMPRISING A PROSTAGLANDIN-SYNTHESIZING ENZYME SYSTEM PREPARED FROM ANIMAL TISSUE, GLUTHAHIONE, AND AN ALL-CIS POLYUNSATURATED CARBOXYLIC ACID OF THE FORMULA
CH3(CH2)N(CH=CHCH2)P(CH2)QCOOH WHEREIN N IS A NUMBER FROM 0 TO 5, P IS A NUMBER FROM 3 TO 5, AND Q IS A NUMBER FROM 0 TO 8, WITH THE PROVISO THAT THE SUM OF N+3P+Q IS FROM 16 TO 20 AND THAT WHEN P IS 3 THEN N IS A NUMBER FROM 3 TO 5. THE ENZYME SYSTEM IS OBTAINED FROM LIVING ANIMAL ORGAN CELLS, E.G., THYMUS, IRIS, GENITAL GLANDS AND THE LIKE. |
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| 188 | Microbiological conversion of unsaturated fatty acids | US34587064 | 1964-02-19 | US3290226A | 1966-12-06 | BEAL III PHILIP F; FONKEN GUNTHER S; PIKE JOHN E |
| 189 | Processes for the preparation of optically active cyclopentenones and cyclopentenones prepared therefrom | US11334336 | 2006-01-18 | US08546114B2 | 2013-10-01 | Yu-Chih Yeh; Ming-Kun Hsu; Shih-Yi Wei |
| The present invention relates to novel processes for preparing optically active Cyclopentenones of Formula (R)-1, which are useful for the preparation of Prostaglandins and analogs thereof. The invention also relates to novel Cyclopentenones prepared from the processes. | ||||||
| 190 | Purification and Separation Treatment Assembly (PASTA) for Biological Products | US13286193 | 2011-11-29 | US20120142047A1 | 2012-06-07 | Sarfaraz K. Niazi |
| An assembly capable of capturing and purifying expressed biological products during or at the end of a bioreaction cycle is disclosed wherein a binding resin is kept separated from the contents of the bioreactor allowing capturing, harvesting and purification of biological products in a bioreactor; the invention additionally provides means of removing undesirable metabolic products as well as provides for efficient loading of chromatography columns. | ||||||
| 191 | Protein having PGE2 synthase activity and use thereof | US10182233 | 2000-08-25 | US07169580B1 | 2007-01-30 | Ichiro Kudo; Makoto Murakami; Sachiko Oh-ishi |
| 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. | ||||||
| 192 | Method for producing highly unsaturated fatty acids and lipid containing same | US11232037 | 2005-09-22 | US20060014268A1 | 2006-01-19 | Osamu Suzuki; Kazuhisa Ono; Seiko Shigeta; Tsunehiro Aki; Kengo Akimoto |
| A method for producing highly unsaturated fatty acids comprising culturing a microorganism, belonging to the genus Mortierella and having resistance to a carbon source, in a medium having a carbon source concentration of at least 4% by weight, and collecting highly unsaturated fatty acids from the cultured products. Culturing the microorganism for about a week gives at least about 7 g/L of highly unsaturated fatty acids. | ||||||
| 193 | Microbiological reduction of prostacyclin intermediate products with a 15-keto group | US176927 | 1994-01-03 | US5403724A | 1995-04-04 | Karl Petzoldt; Helmut Dahl; Werner Skuballa |
| A process for production of 15-alpha-hydroxyprostaglandin intermediates of formula I ##STR1## wherein X is CH.sub.2,A is trans --CH.dbd.CH--B is ethylenedioxy or 2,2-dimethylpropylenedioxy,R.sub.1 is benzoyl, andR.sub.2 is ##STR2## by treating a ketone of formula II ##STR3## wherein A, B, X, R.sub.1 and R.sub.2 have the meanings indicated above, with a culture of Candida solani (NCYC 41) and isolating the resulting 15-alpha-hydroxyprostaglandin intermediate. | ||||||
| 194 | Prostacyclin, methods of using and method of making | US795524 | 1977-05-10 | US4539333A | 1985-09-03 | Salvador Moncada |
| Prostacyclin, its salts, biosynthesis and synthesis thereof, pharmaceutical formulations containing them, and their use in medicine. | ||||||
| 195 | 16-Amino-postaglandin derivatives, their acid addition salts, and a process for the preparation thereof | US332840 | 1981-12-21 | US4372973A | 1983-02-08 | Gabor Ambrus; Eva Toth-Sarudy; Gyorgy Cseh; Istvan Barta; Gyula Horvath |
| The invention relates to new 16-amino-prostaglandin derivatives of general formula I, ##STR1## wherein C-15 and C-16 may have either S or R configuration, Z stands for a hydrogen atom or a lower alkyl group, and their acid addition salts. These compounds can be prepared by removing the ester group and the p-nitrocarbobenzyloxy protective group of a 9.alpha., 11.alpha., 15-trihydroxy-16-p-nitrobenzyloxycarbonylamido-5-cis,13-trans-prostadienoic acid derivative of general formula XII--wherein C-15 and C-16 may have either S or R configuration and Z stands for a lower alkyl group--in an optional sequence with the limitation that in those compounds of general formula I where Z stands for a lower alkyl group solely the p-nitrocarbobenzyloxy group is removed, and the resulting product of general formula I is optionally converted with an organic or inorganic acid into a salt.The new prostaglandin derivatives of the invention have valuable therapeutical properties, and can be applied as abortive or oxytocic agents. | ||||||
| 196 | Microbiological reduction of 15-ketoprostaglandin intermediates | US100571 | 1979-12-05 | US4247635A | 1981-01-27 | Klaus Kieslich; Bernd Raduchel; Werner Skubalia; Helmut Vorbruggen; Helmut Dahl |
| A process for the preparation of a 15 .alpha.-hydroxyprostaglandin intermediate of the formula ##STR1## wherein R.sub.1 is phenoxymethyl, phenoxymethyl substituted on the phenyl moiety by halogen or trifluoromethyl, or alkyl of 1-5 carbon atoms, andR.sub.2 is hydrogen, acetyl, benzoyl or p-phenylbenzoyl,which comprises stereospecifically microbiologically reducing a corresponding 15-ketone of the formula ##STR2## with a strain of the microorganism Kloeckera, Saccharomyces or Hansenula. | ||||||
| 197 | 19 Hydroxy prostaglandins | US955005 | 1978-10-26 | USRE30287E | 1980-05-27 | Arthur F. Marx; Jean Doodewaard |
| Novel 18 -, 19 - and 20 -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 of 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- 19- and 20-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. | ||||||
| 198 | Prostaglandin derivatives | US831949 | 1977-09-09 | US4190670A | 1980-02-26 | Arthur F. Marx; Jean Doodewaard |
| 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. | ||||||
| 199 | 18 OR 19 Hydroxy prostaglandins | US561895 | 1975-03-25 | US4054595A | 1977-10-18 | Arthur Friedrich Marx; Jean Doodewaard |
| Novel 18 -, 19 - and 20 -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=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=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 of 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 -, 19 - and 20 -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. | ||||||
| 200 | Racemic fluoro-substituted PGB.sub.2 analogs | US530429 | 1974-12-06 | US3993687A | 1976-11-23 | William P. Schneider |
| This invention is racemic PGE.sub.2 .alpha., racemic PGF.sub.2.sub..alpha., racemic PGF.sub.2 .beta., racemic PGA.sub.2, racemic PGB.sub.2, analogs of those, and processes for making them. These compounds are useful for a variety of pharmacological purposes, including anti-ulcer, inhibition of platelet aggregation, increase of nasal patency, abortion, and wound healing. | ||||||
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