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WO/1981/001002A1 |
Prostaglandin and prostacyclin compounds which are fluorine substituted in any one or more of the following positions, 4, 4; 7, 7; 10, 10; and 5.
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WO/1980/001381A1 |
Novel bicyclo (2,2,1) heptanes and hept-2Z-enes are substituted at the 5-position by a 6-carboxyhex-2-enyl group or a modification thereof, and at the 6-position by an aldoxime or ketoxime group which is O-substituted by an aliphatic hyd...
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WO/1980/001382A1 |
Novel bicyclo (2,2,1) heptanes and hept-2-enes are substituted at the 5-position by a 6-carboxyhex-2-enyl group or a modification thereof, and at the 6-position by a grouping -C(R)=N-NHCO-(NH)a-R' in which R is hydrogen, an aliphatic hyd...
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JP2024012261A |
[Problem] Highly purified pharmaceutical grade hexanoic acid, 6-(nitrooxy)-, (1S,2E)-3- that is substantially free of the impurity 15-(6-chlorohexanoyl) ester of bimatoprost. [(1R,2R,3S,5R)-2-[(2Z)-7-(ethylamino)-7-oxo-2-hepten-1-yl]-3
,...
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JP2024009896A |
[Problem] Compound 6-(nitrooxy)-hexanoic acid (1S,2E)-3-[(1R,2R,3S,5R)-2-[(2Z)-7-(ethylamino)-7-oxo-2 -Hepten-1-yl]-3,5-dihydroxycyclopentyl]-1-(2-phenylethyl)-2-
propen-1-yl ester (I) is provided. [Solution] Compound (I) is efficiently ...
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JP2023165632A |
To provide more efficient and selective methods for preparing carbaprostacyclin analogues, and intermediates.The present invention provides a racemic or optically active compound represented by the following formula (where Y is -CH2OP or...
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JP7368381B2 |
This invention relates generally to the synthesis of Δ12-Prostaglandin J product using stereoretentive ruthenium olefin metathesis catalysts supported by dithiolate ligands. Δ12-Prostaglandin J products were generated with excellent se...
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JP7365349B2 |
The present invention relates to a process for preparing the Hexanoic acid, 6-(nitrooxy)-, (1S,2E)-3-[(1R,2R,3S,5R)-2-[(2Z)-7-(ethylamino)-7-oxo-2-hept
en-1-yl]-3,5-dihydroxycyclopentyl]-1-(2-phenylethyl)-2-prope
n-1-yl ester of formula ...
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JP7292255B2 |
Preparation of the compounds of general formula I, among them misoprostol where R represents a straight‐ or branched‐chain C1-4 alkyl group by cuprate coupling of the vinyl cuprate of general formula II prepared by reacting the vinyl...
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JP2023054794A |
To provide a purification method for tafluprost that is simple and efficient and enables scale-up.A tafluprost purification method includes the step of purifying a crude product of tafluprost by silica gel column chromatography, to colle...
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JP2023031276A |
To provide a method for efficiently preparing high purity Carboprost or Carboprost Tromethamine, which can significantly reduce the formation of impurities or isomers including 15(R)-epimer and trans isomer, and can also effectively remo...
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JP2023502893A |
The present invention provides a pharmaceutical composition for preventing or treating a disease, disorder or condition associated with Nurr1, comprising a prostaglandin analogue or a pharmaceutically acceptable salt thereof as an active...
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JP7205482B2 |
The present invention relates to a novel production method of a novel prostaglandin derivative or a pharmaceutically acceptable salt thereof useful as a medicament, and an intermediate therefor. According to the present invention, a prod...
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JP7192999B1 |
An object of the present invention is to provide a simple, efficient, and scalable method for purifying tafluprost. The present invention relates to a method for purifying tafluprost, comprising the steps of purifying crude tafluprost by...
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JP7164901B2 |
The present invention relates to processes for preparing latanoprostene bunod comprising reacting latanoprost acid with 1,4-butanediol dinitrate, as well as a silylated intermediate and a dimeric by-product thereof. The present invention...
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JP2022544092A |
The present invention provides hexanoic acid,6-(nitrooxy)-,(1S,2E)-3-[(1R,2R,3S,5R)-2-[(2Z)-7-( Ethylamino)-7-oxo-2-hepten-1-yl]-3,5-dihydroxycyclopentyl]-1
-(2-phenylethyl)-2-propen-1-yl ester. According to the present invention, bimato...
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JP7109029B2 |
The present invention provides an industrially desirable novel cyclopentenone derivative, and a production method therefor. The novel compounds (the compounds represented by formula (II) and stereoisomers thereof) provided by the inventi...
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JP7050673B2 |
The subject of the invention is a process for the preparation of Latanoprostene bunod of formula (I) with a purity higher than 95% where chromatography is used applying normal phase gravity silica gel column chromatography where the used...
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JP7019920B2 |
The present invention provides a method for introducing substituents into the α-position and the β-position of an α,β-unsaturated ketone, which not only can be used for the synthesis of a prostaglandin by a three-component coupling p...
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JP2021524862A |
The present invention is a novel biologically active compound in clinical chemistry, in particular prostaglandin F.2αRegarding amide derivatives of. These compounds are low cytotoxic and can stimulate the formation of endogenous nitroge...
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JP6862448B2 |
The subject of the invention is a novel process for the preparation of Carboprost tromethamine salt where alkylation the enone of the general formula (II) is carried out in the presence of a chiral auxiliary in aprotic solvent with a Gri...
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JP6809987B2 |
A method for manufacturing a fatty acid derivative represented by formula (I) is provided: wherein Z1 is wherein R3 is a protecting group for a hydroxy group; which includes the step of reacting a compound of formula (II): wherein Z2 is ...
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JP2020164527A |
To provide prostaglandins that are substantially free of 5,6-trans isomer.A composition contains a prostaglandin derivative. A composition contains travoprost free acid, in which the 5,6-trans isomer content is less than 0.1% and the 15...
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JP2020090500A |
To provide isomerically or chemically pure prostaglandins.A latanoprost composition comprises latanoprost having at least a chemical purity of 99.95% and an isomeric purity of 99.92%, and C15S-cis isomer of latanoprost in an amount up to...
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JP6693859B2 |
The subject of the invention is process for the preparation of the prostaglandin amides of the general formula I, where in the formula the bonds marked with dotted lines may be single or double bonds, in the case of double bounds at posi...
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JP6675653B2 |
The present invention relates to a novel prostaglandin derivative having an alkynyl group on É-chain, particularly, a novel prostaglandin derivative having a double bond at the 2-position and an alkynyl group on the É-chain and a medic...
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JP6659563B2 |
The subject of the invention is a process for the preparation of high purity prostaglandin acid of the general formula II wherein the bonds marked with dotted lines represent single or double bonds wherein the double bonds may be cis- or...
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JP6654757B2 |
Prostaglandin conjugates and derivatives and methods for their use to treat glaucoma and/or lower intraocular pressure are disclosed. Additionally, ophthalmic pharmaceutical compositions useful in the treatment of eye diseases such as gl...
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JP6643308B2 |
This invention provides a novel method for the preparation of 2,3-disubstituted -4-oxy-cyclopentan1-one compounds that are useful for the synthesis of prostaglandins and prostaglandin analogs of industrial relevance. The method comprises...
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JP6633497B2 |
The present invention provides a method for the purification of a prostaglandin by supercritical fluid chromatography, said method comprising the use of a stationary phase and a mobile phase comprising carbon dioxide, provided that when ...
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JP2019513808A |
A method for preparing bimatoprost, which comprises reacting the compound of formula (III) with ethylamine in the presence of a suitable solvent; and b) deprotecting the compound obtained in step a) to obtain bimatoprost. Provided. In th...
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JP6487410B2 |
The subject of the invention is process for the preparation of the prostaglandin amides of the general formula I, where in the formula the bonds marked with dotted lines may be single or double bonds, in the case of double bounds at posi...
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JP2018536017A |
The present disclosure includes prodrugs and derivatives of prostaglandins, carbonic anhydrase inhibitors, kinase inhibitors, β-adrenergic receptor antagonists and other drugs for the treatment of eye disorders, and such prodrugs and de...
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JP2018104435A |
To provide latanoprost which is chemically and/or isomerically pure.For example, a latanoprost composition is obtained by a method for purification of latanoprost by supercritical fluid chromatography using a stationary phase and a mobil...
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JP6306067B2 |
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JP2017222708A |
To provide a novel fatty acid derivative, and provide the use of an effective amount of a fatty acid derivative for treating schizophrenia in a mammalian subject.The present invention provides a pharmaceutical composition for treating sc...
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JP6193230B2 |
The present invention provides a novel fatty acid derivative. The present invention also provides a method for treating schizophrenia in a mammalian subject, which comprises administering to the subject in need thereof an effective amoun...
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JP6174040B2 |
The crystalline compound of formula (III) having the melting point of 129.5-134.5° C. is disclosed.
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JP6087147B2 |
The present invention provides a method for the purification of a prostaglandin by supercritical fluid chromatography, said method comprising the use of a stationary phase and a mobile phase comprising carbon dioxide, provided that when ...
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JP2016193930A |
To provide intermediates for preparations of derivatives of prostaglandins substantially free of the 5,6-trans isomer.A crystalline compound is selected from a group consisting of compounds represented by the formulas in the figure or th...
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JP2016533329A |
In some embodiments, the present invention is Δ12-PGJ3New derivatives and Δ12-PGJ3And a modular synthetic pathway for obtaining derivatives thereof. In some embodiments, Δ12-PGJ3Derivatives of are useful as chemotherapeutic agents. Th...
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JP6013412B2 |
Novel processes for the preparation of a compound of Formula I-2 substantially free of the 5,6- trans isomer: wherein R 2 , R 3 and R 4 are as defined in the specification are provided. Novel intermediates for the preparations of isomer ...
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JP5962657B2 |
The present invention provides a compound of which active form is represented by a formula (A). and which can be injected into a joint cavity which is an affected part of disorders and can be accumulated in the joint cavity to exert the ...
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JP2016094471A |
To provide a new crystalline form of 7-[3,5-dihydroxy-2-(3-hydroxy-5-phenyl-pent-1-enyl)-cyclopen
tyl]-N-ethyl-hept-5-enamide (bimatoprost).The present invention provides a new crystalline form of 7-[3,5-dihydroxy-2-(3-hydroxy-5-phenyl-p...
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JP5921439B2 |
The present invention provides a new crystalline form of bimatoprost, designated as crystalline form II. This new crystalline form is the most stable form known to date of bimatoprost. Moreover, it has been found that bimatoprost crystal...
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JP5885271B2 |
Provided herein, inter alia, are prodrugs of bimatoprost, methods of using the same and compositions including the same.
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JP2015205912A |
To develop a novel compound which can be delivered effectively and efficiently to a site of action in a certain state (e.g., disease) for preventing, reducing, or treating the state in a biological subject while minimizing side effects.T...
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JP5795354B2 |
A process for the preparation of prostaglandin compounds having the formula (I); wherein A is selected from the group consisting Of C1-C6 alkyl; C7-C16 aralkyl wherein the aryl group is optionally substituted with one to three substituen...
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JP2015129146A |
To provide a novel production method for prostamide.A production method for prostamide comprises the following steps of: (a) producing a second intermediate of a formula II by the reaction of a first intermediate of a formula I and DIBAL...
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JP2015120693A |
To provide new processes for preparing and purifying lubiprostone.A process involves 1,4-conjugate addition of a higher order cuprate compound to a protected cyclopentenone intermediate as an important preparation step. Obtained lubipros...
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