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WO/1991/001302A1 |
9-fluor-postaglandine derivates are disclosed, having the formula (I), in which R?1� represents the groups (a), (b), COOR?4� or CONHR?5�; R?2� and R?3� represent each a hydrogen atom or a free or functionally transformed hydrox...
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WO/1990/014329A1 |
Compounds of formula (I) in which the residues have the following meanings: a is (II) or (III); R?1¿ is CH¿2?OH, CH¿3?, CF¿3?, COOR?5¿ with R?5¿ or, A is a trans, trans-CH=CH-CH=CH- or tetramethylene group; B is an alkylene group w...
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WO/1990/012576A1 |
A liquid composition comprising prostaglandin and a polyoxyethylene-polyoxypropylene copolymer having a molecular weight of 1,000 to 20,000. The stability of the prostaglandin can be remarkably improved by the use of the above-specified ...
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WO/1990/011276A1 |
The invention concerns a process for producing optically active bicyclo [3.3.0]-octane derivatives of formula (I), characterized in that 3-cyclopentylpropine derivatives of formula (II) in which X and R?1¿ have the meanings given are re...
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WO/1990/011275A1 |
The invention concerns 20-alkyl-3-oxa-isocarbacyclines of formula(I), in which p = 1 to 3, R?1¿ is a hydrogen atom or an alkyl group with 1 to 5 C atoms, R?2¿ is an alkyl group with 2 to 5 C atoms, their salts with physiologically acce...
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WO/1990/006917A1 |
This invention relates to novel optically active thromboxane A2 inhibiting 7-[3- [1-[[(phenylamino)thioxomethyl]hydrazono]ethyl]-bicyclo[2,2,
1]hept-2-yl]- heptenoic acids and to methods for their manufacture.
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WO/1990/005720A1 |
Process for producing carbacyclins of formula (I) wherein R1 is a straight-chain or branched C1-C7 alkyl group, a straight-chain or branched C2-C7 alkenyl group or a straight-chain or branched C2-C7 alkinyl group, and R2 and R3 can be th...
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WO/1990/002728A2 |
The invention concerns 6-oxo-9-fluor-prostaglandin derivatives of formula (I) in which R1 is a COOR2 or CONHSO2R2 residue in which R2 is a C5 to C6 cycloalkyl group or a C6 to C12 aryl group or a 5- or 6-membered heterocyclic residue, or...
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WO/1990/002553A1 |
The invention relates to ophthalmological compositions for topical treatment of glaucoma or ocular hypertension comprising an effective intraocular pressure reducing amount of a prostaglandin derivative of PGA, PGB, PGD, PGE or PGF, in w...
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WO/1990/002740A1 |
2-oxa-bicyclo[2.2.1]heptane derivatives according to formula (I) and their enantiomers, where for example A represents -(CH2)n-, (E)-CH=CH- or (Z)-CH=CH-, -C=C, -O- or -S-; B represents hydrogen, C1-C10 alkyl, -OR2, halogen, C=N, -N3, -C...
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WO/1989/003384A1 |
Use of derivatives of a diastereomer of prostaglandin F2alpha, viz. 11 epi, for the manufacture of compositions for the treatment of glaucoma or ocular hypertension.
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WO/1989/001470A1 |
The invention concerns a process for producing E/Z mixtures of 2-(bicyclo[3.3.0]octane-3-ylidene) acetic acid derivatives of formula (I) in which either the E or the Z moiety predominates.
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WO/1989/000990A1 |
The invention concerns carbacycline derivatives of formula (I), where Y1 is the residue -CH2-X-(CH2)n-R1 or the residue (a), n = 1 or 3, R1 is the residue (b), the residue (c), -COCH3, COOR2, where R2 is hydrogen or possibly alkyl with 1...
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WO/1989/000559A1 |
9-Halogen-(Z)-prostane derivatives have the formula (I), where Z is one of the residues (a) or (b), Hal is a chorine or fluorine atom in the alpha or beta position, R1 is the residue CH2OH or (c) where R2 is a hydrogen atom or an alkyl, ...
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WO/1988/010252A1 |
Novel prostaglandins of formula (IA) and (IB) are described wherein: n = 2, 3; m = 4, 5, 6, 7; p = 5, 6, 7, Y, when X = H, -NH2, represents -NH-NH2, -CH2NH2, -NRR', wherein R and R' may be the same or different, each representing: H, a l...
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WO/1988/007037A1 |
6-Oxoprostaglandin-E, derivatives having the formula (I), in which R1 signifies the residue COOR2 where R2 signifies a hydrogen atom, a C1-10 alkyl, a C5-6 cycloalkyl, a C6-C10 aryl group, a heterocyclic residue or the residue CONHSO2R5 ...
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WO/1988/007050A1 |
Process for the production of (+)-bicyclo-[3.3.0]octane-3-on-2-carboxylic acid steroid esters having the formula (I), in which X represents oxygen or the -O-(CH2)n-O- or the -O-CH2-C(CH3)2-CH2-O- residue; n represents 2 or 3; R2 represen...
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WO/1988/005042A1 |
Therapeutical compositions containing products obtained from the addition of thiols to prostaglandines or analogues of prostaglandines. These compositions have an antitumoral activity.
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WO/1988/003527A1 |
Process for the production of alpha-hydroxy-bicyclo[3.3.0]octane derivatives of formula (I), where A is the double-bound residue -O-X-O-, X having the notation of a straight or branched-chain alkalin with 1-7 C atoms or the residue =CH-(...
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WO/1988/003570A1 |
Process for the manufacture of (-)-oxabicyclo[3.3.0]octanolones of formula (-)-I, where R is hydrogen or the residue (a), in which R1 has the notation of a hydrogen, alkyl with 1-7 C atoms, or phenyl. The process is characterized in that...
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WO/1988/003567A1 |
Process for the production of optically active (+)-bicyclo[3.3.0]octanol derivatives of formula (+)-I, in which R1 and R2 represent jointly an oxygen atom or the double-bond residue -O-X-O-, with X as a straight or branched-chain alkylen...
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WO/1988/003568A1 |
Process for the production of 3alpha-hydroxy-prostacyclin intermediates of formula (+)-I, where A is the residue -CH2- or >CH-COOR, B is oxygen or the double-bond residue -O-X-O- with X as a straight or branched-chain alkylene with 1-7 C...
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WO/1988/003526A1 |
Process for manufacturing cis-bicyclo[3.3.0]octane-2-aldehydes of formula (I), in which R1 and R2 jointly represent the double-bound residue -O-X-O-, with X as straight or branched-chain alkylene with 1-7 C-atoms or R1 and R2 accordingly...
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WO/1987/005294A1 |
Cyclodextrinclathrates of carbacycline analogs have general formula (I) in which: R1 is an atom of hydrogen or a straight chain or branched alkyl rest with up to 10 C atoms, A is a trans-CH=CH or -C=C group, W is a free or functionally t...
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WO/1987/004428A2 |
Novel compounds have formula (I) where (chi) represents one of the divalent cyclic groups (alpha), (beta), (psi), (delta), (epsilon), (phi), (gamma), (eta), (iota), (xi). The letters a and b indicating in each case the points of attachme...
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WO/1987/004427A2 |
A process for the preparation of a compound of formula (I), wherein X and X' each represents hydrogen or together represent a bridging group -CH2-, -CH2-CH2- or -O-; R1 is a 6-carboxyhex-2-enyl group or a modification thereof in which th...
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WO/1987/003582A1 |
A process for producing (5-chlor-3-hydroxy-cyclopentyl)acetaldehyde having the formula (II), in which R represents a benzyl rest, a tertiary butyl-dimethyl-silyl rest or a tertiary butyl-diphenylsilyl rest. The process is characterized b...
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WO/1987/003283A1 |
Carbacycline derivatives of general formula (I), in which Y1 is the residue of Formula (II), R9 is the residue -(CH2)m-R6 or the residue -(CH2)m-o- ADZ1-(CH2)m-p BDx- ADZ2-(CH2)m-q BDy-R6, m = 2-20; o, p and q <= 19; x, y = 0, 1 or 2; Z1...
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WO/1987/002360A1 |
Isocarbacyclin derivatives represented by formula (I) wherein R1 represents a straight, branched or cyclic alkyl group having 5 to 10 carbon atoms, an alkenyl group or an alkynyl group, and R2 and R3 each represents a hydrogen atom or a ...
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WO/1987/001696A1 |
Novel prostacyclins represented by general formula (I), wherein R1 represents -CO2R5 or -CONR6R7, A represents (i) -CH=CH-CH2CH2- or (ii) -CH2CH2-O-CH2-, B represents -C=C-, R2 represents alkyl, cycloalkyl, alkenyl, alkynyl, phenyl or ph...
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WO/1986/005488A1 |
9-Halogen-15-cycloalkyl-prostaglandine derivates of formula (I), wherein R1 signifies hydrogen or methyl, R2 signifies fluorine or chlorine, n signifies 0 or 1, and, if R1 signifies hydrogen, their salts with physiologically tolerable ba...
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WO/1986/004330A1 |
A process for preparing 16-substituted DELTA7-prostaglandin E's of the compounds represented by general formula (I), ADwherein R1 represents COOR2, CH2OR3 or COCH2OR3 (wherein R2 represents H, substituted or unsubstituted C1 - C10 alkyl,...
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WO/1986/004234A2 |
Compounds having thromboxane antagonist activity are of use in the treatment of hormone-dependent neoplasias for example oestrogen-dependent neoplasias. Thromboxane antagonists of particular value are compounds of formula (I) wherein for...
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WO/1986/002923A1 |
A process for preparing bicyclo AD3.3.0 BDoctenes represented by general formula (II), wherein R11 represents H, a mono-equivalent cation or R1, Romega' represents Romega, and R21 represents H or R2, from a thiol compound represented by ...
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WO/1986/000895A1 |
Carbacycline derivatives of formula (I) are disclosed, wherein: n is 1 or 3, R1 is the rest having the formula (II), the rest having the formula (III), -COCH3, the rest COOR2 wherein R2 is hydrogen or alkyl with 1 to 10 atoms of carbon o...
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WO/1985/005452A1 |
Process for the determination of small quantities of drugs, body substances or other chemical compounds in a biological material, characterized in that the compound to be determined and its deuterised analogue are bound to an antibody in...
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WO/1985/004875A1 |
New derivatives 15(R+S)-fluorine-11,15-didesoxyprostaglandin E1 of general formula (I) where R' is ethyl, methyl, hydrogen, sodium; R2 or R3 is hydrogen or fluorine. The derivatives have a high antiaggregative activity of long duration.
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WO/1985/004656A1 |
9-halogen-prostane having the formula (I) wherein Hal represents a chlorine or fluorine atom in position alpha or beta; R1 represents the rest CH2OH or the formula (A) with R2 representing a hydrogen atom, an alkyl, cycloalkyl, aryl or h...
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WO/1985/003936A1 |
7-thiaprostaglandin E1's represented by formula (I): (wherein R1 represents H, C1 to C10 alkyl, C2 to C20 alkenyl, substituted or unsubstituted phenyl, substituted or unsubstituted C3 to C10 cycloalkyl, substituted or unsubstituted pheny...
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WO/1985/003935A1 |
6-substituted prostaglandin E1's represented by formula (I), (wherein R1 represents H, C1 to C10 alkyl, substituted or unsubstituted phenyl, substituted or unsubstituted C3 to C10 cycloalkyl, substituted or unsubstituted phenyl(C1 to C2)...
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WO/1985/003706A1 |
Novel punaglandins AD5-(2,3-diacetoxy-6-methoxycarbonyl hexylidene)-2-chloro-4-)2,5-octadienyl)-4-hydroxy-2-cyclopen
tenone, or 5-(2,3-diacetoxy-6-methoxycarbonylhexy-lidene)-2-chloro-4-(2
-octenyl)-4-hydroxy-2-cyclopentenone BD are isol...
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WO/1985/002841A1 |
9-halogen-DELTA2-prostaglandine derivatives having the general formula (I), wherein Hal may be a fluorine or chlorine atom in alpha or beta position; R1 may be the rest OR2, R2 being a hydrogen atom, an alkyl, a cycloalkyl, an aryl or a ...
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WO/1985/002187A1 |
20-alkyl-7-oxoprostacycline derivatives having the general formula (I) wherein R1 is either the rest OR3, R3 representing hydrogen or alkyl comprising from 1 to 10 atoms of carbon optionally substituted by halogen, phenyl, alkoxy having ...
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WO/1985/001728A1 |
A process for preparing prostaglandin D2's in good yields, which comprises treating 7-hydroxyPGF2alpha's with thiocarbonylimidazole or an analogue thereof, subjecting the product to deoxidation of the hydroxy group in position 7, convers...
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WO/1985/000367A1 |
11-halogene-prostane derivatives of the general formula (I), wherein X is F, Cl or Br; R1 is CH2OH or (II) wherein R2 is a hydrogen atom, a rest of alkyl, cycloalkyl, aryl, phenacyl or heterocyclic rest; A is a group -CH2-CH2- or cis -CH...
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WO/1984/004917A1 |
7-Fluoroprostaglandins represented by formula (I), wherein R1 represents H or C1-10 alkyl, R2, R3, and R4 each represents H or the same or different protective group, and R5 represents C3-7, straight-chain, branched or cyclic alkyl.
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WO/1984/002902A1 |
Novel prostacyclines represented by the formula (I), wherein ---- between 2- and 3-positions represents that the bond between these positions is a single or double bond, G represents -CO2R5 or -CONR6R7, wherein R5 represents H, C1-C10 al...
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WO/1983/004021A1 |
New 2,3,4-trinor-1,5-inter-m-phenylene-PGI2 derivatives (wherein A stands for carboxy, cyano, tetrazolyl or -COOR3 or -CONR1R2; R3 is C1-4 alkyl or an equivalent of a pharmacologically acceptable cation: R1 and R2 each stands for hydroge...
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WO/1983/003248A1 |
Carbacycline derivatives having the formula I wherein R1 is the residue CH2OH or$(1,)$ -C-OR2, R2 representing a hydrogen atom, an alkyl, cycloalkyl, aryl, $(1,)$CH2 -C-aryl residue or a heterocyclic residue, or R1 is the residue $(1,)$-...
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WO/1983/002273A1 |
Novel compounds have a formula (I)$(10,)$wherein$(6,)$represents a bicyclo AD2,2,1 BD hept-2Z-ene, bicyclo AD2,2,1 BD heptane, 7-oxa-bicyclo AD2,2,1 BD hept-2Z-ene, 7-oxa-bicyclo AD2,2,1 BD heptane, bicyclo AD 2,2,2 BD oct-2Z-ene or bicy...
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