Abstract: The present invention provides novel prostaglandins D, that is, 13,14-dihydro-15-keto-PGDs, which have an excellent sedative and sleep-inducing activity, and so they are useful for tranquilizer and/or soporifics.

Abstract: A method for improvement of excretion of nonprotein nitrogen into the intestines which comprises administering, to a subject in need of such improvement, a prostanoic acid derivative in an amount effective in improving excretion of nonprotein nitrogen into the intestines.

Abstract: The invention relates to carbacyclins of general Formula I ##STR1## wherein R.sub.1 is the residue CH.sub.2 OH or ##STR2## with R.sub.2 meaning a hydrogen atom, an alkyl, cycloalkyl, aryl residue, a ##STR3## or heterocyclic residue, or R.sub.1 is the residue ##STR4## with R.sub.3 meaning an alkanoyl or alkanesulfonyl residue of respectively 1-10 carbon atoms or the residue R.sub.2, orR.sub.1 is the residue ##STR5## wherein m is the number 1 or 2, X is an oxygen atom or a CH.sub.2 -group,A is a trans--CH.dbd.CH- or --.tbd.C--group,W is a free or functionally modified hydroxymethylene group wherein the OH-group can be in the .alpha.- or .beta.- position,n is the number 1, 2, or 3,D is a straight-chain alkylene group of 1-5 carbon atoms,E is a --C.tbd.C---bond or a --CR.sub.6 =CR.sub.7 --group wherein R.sub.6 and R.sub.7 are different from each other and mean a hydrogen atom or an alkyl group of 1-5 carbon atoms or a hydrogen atom or a halogen atom, preferably chlorine,R.sub.

Abstract: A liquid composition for nasal administration of polypeptide/s containing ammonium tartrate and a buffer together with optional adiuvants.

Abstract: An emulsion of lipid containing a prostaglandin analogue of the formula (1): ##STR1## wherein R.sup.1 is an alkanoyl group, R.sup.2 is a hydrogen atom or an alkyl group, each of R.sup.3 and R.sup.4 is a hydrogen atom or a protective group for an alcohol, R.sup.5 is an alkyl group which may have a substituent, and is a single bond or a double bond.

Abstract: A method of repelling Musca domestica L. (Diptera Muscidae) or Aedes aegyptae for a finite period of time from a three-dimensional space inhabitable by Musca domestica L. (Diptera Muscidae) or Aedes aegyptae consisting essentially of the step of exposing a three-dimensional space to an effective Musca domestica L. (Diptera Muscidae) or Aedes aegyptae - repelling concentration and quantity of a cyclopentanone derivative composition of matter selected from the group of the mixtures:(i) methyl jasmonate,(ii) HEDIONE.RTM., and(iii) KHARISMAL.TM..

Abstract: 2-Substituted-2-cyclopentenones represented by the formula (I): ##STR1## wherein A is a hydroxyl group or ##STR2## and B is a hydrogen atom or A and B are bonded together to form one bonding arm;R.sup.1 represents a substituted or unsubstituted hydrocarbon group having 1 to 10 carbon atoms;R.sup.2 represents a substituted or unsubstituted aliphatic hydrocarbon group having 1 to 10 carbon atoms;R.sup.3 represents a substituted or unsubstituted aliphatic hydrocarbon group having 1 to 10 carbon atoms; wherein,when R.sup.3 is a single bond bonded to the cyclopentene skeleton, X represents a hydrogen atom, a hydroxyl group or a protected hydroxyl group; andwhen R.sup.3 is a double bond bonded to the pentene skeleton, X represents a bonding arm constituting a part of said double bond; andm and n independently represent 0, 1 or 2.

Abstract: The invention is related to the novel compounds that have anti-oxident and anti-cancer activities. These compounds can protect (i) vital organs including the brain and the heart, (ii) skin cells, (iii) circulating cells such as red blood cells and white blood cells from physical, chemical and biological injuries either by pre-administration or post-administration. These compounds can be used to protect (iv) organs during transplant surgery by administering to a donar before removal of the organ and by administering to a receipient after transplantation. (v) These compounds can also protect red blood cells from the attack of malarial parasites. (vi) These compounds can be themselves be administered to cancer patients as low side-effect anti-cancer agents. They can also be administered to (vii) potentiate efficacy of existing other chemotherapeutic agents and (viii) to reduce side-effects of existing other chemotherapeutic agents.

Abstract: 11-epi PGF.sub.2 alpha esters are employed in treating glaucoma or ocular hypertension.

Abstract: 3-Methoximinopropionic esters of the formula ##STR1## where the radicals R (m=1 to 5) are each hydrogen, halogen, cyano, nitro, alkyl, cycloalkyl, alkenyl, alkoxy, haloalkyl, haloalkoxy, unsubstituted or substituted phenyl, unsubstituted or substituted phenoxy, unsubstituted or substituted benzyl or unsubstituted or substituted benzyloxy, or the group ##STR2## is naphthyl, and X is methyleneoxy, oxymethylene, ethylene, ethenylene, thiomethylene or oxygen, and fungicides containing these compounds.

Abstract: The present invention relates to novel isomers of PGAs, PGDs, PGEs, PGFs, 6-keto-PGE.sub.1 s, 6-keto-PGF.sub.1 s, PGI.sub.2 s, 6,9.alpha.-nitrilo-PGI.sub.1 s and 6,9.alpha.-methano-PGI.sub.2 s, having a specific steric configuration, which are replaced by an alkyl (C.sub.1 to C.sub.8)-substituted cycloalkyl (C.sub.4 to C.sub.7) group in (1S,S) form, in (1S,R) form or in cis form at the 15-, 16- or 17-position of the PG skeleton, and, alkyl esters thereof, non-toxic salts thereof, non-toxic acid addition salts thereof and cyclodextrin clathrates thereof, possessing more potent PG-like pharmacological activity than other isomers.

Abstract: The present invention provides new compounds, 13,14-dihydro-15-keto-PGFs, and vassopressors containing them, which raise blood pressure without substantial ephemeral depression of blood pressure, trachea or enteron contraction effect inherent in usual PGFs.

Abstract: A method for treatment of a hepatobiliary disease which comprises administering, to a subject in need of such treatment, a 15-ketoprostaglandin compound in an amount effective in treatment of the hepatobiliary disease.

Abstract: A preventive and therapeutic agent for hepatitis, comprising a fat emulsion containing a compound having prostaglandin E.sub.1 activities.

Abstract: Tetraenyl Prostanoic Acid derivatives which are useful as prodrugs for the treatment of peptic ulcer disease and are represented by the following general formula ##STR1## are disclosed.

Abstract: The instant invention is novel uses of known cyclic amino acids. Such compounds as gabapentin are used for treating neurodegenerative disorders, perinatal asphyxia, status epilepticus, Alzheimer's Hungington's, Parkinson's, and Amyotrophic Lateral Sclerosis.

Abstract: A 9-chloroprostane of the formula ##STR1## wherein the 9-chlorine atom can be in the .alpha. or .beta.-position and R.sub.1, R.sub.4, R.sub.5, A, B, W, D and E are as described hereinafter which are useful as medical agents.

Abstract: Novel compounds have the formula (I) ##STR1## where ##STR2## represents one of the divalent cyclic groups ##STR3## the letters a and b indicating in each case the points of attachment of the substituents R.sup.1 and CV(R.sup.2)-NV'R, respectively; R.sup.1 is a group --(CH.sub.2).sub.b --(A).sub.a --(CH.sub.2).sub.c --B--CH.sub.2 --CO.sub.2 R' in which A and B are each separately oxygen or sulphur, a is 0, b is 0 and c is an integer from 3 to 10, or a is 1, b is 0 or an integer from 1 to 7 and c is an integer from 2 to 9 with the sum of b and c being from 2 to 9, and CO.sub.2 R' is a carboxy group or an amide, ester or salt derivative thereof; V and V' either each separately is hydrogen or together are the second bond of a carbon-nitrogen double bond; R.sup.2 is hydrogen, an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by an aromatic group directly or through an oxygen or sulphur atom; and R is a group --OR.sup.3, --OR.sup.4, --D--R.sup.3, --N.dbd. R.sup.5 or --NW.G.

Abstract: Amethod for inducing decrease in potassium ion concentration in the blood which comprises administering, to a subject having an increased potassium ion concentration in the blood, a prostanoic acid derivative in an amount effective in inducing decrease in potassium ion concentration in the blood wherein said concentration is increased or for improving extracorporeal excretion of potassium ion in the blood which comprises administering, to a subject having an increased potassium ion concentration in the blood, a prostanoic acid derivative in an amount effective in improving extracorporeal excretion of potassium ion concentration is increased.

Abstract: The use of compounds of formula I as topical agents to combat the disorders of the skin produced by photodamage which disorders include: wrinkling, elastosis and premature aging is described. Compounds of formula I are ##STR1## wherein n represents 1 or 2, Z represents--SR, wherein R represents lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkoxy-lower-alkyl, lower-alkanoyl-lower-alkyl, hydroxy-lower-alkyl, halo-lower-alkyl, lower-carbalkoxy-lower alkyl, mono-lower-alkylamino, di-lower-alkylamino, mono-lower-alkylamido, or di-lower-alkylamidoand pharmaceutically acceptable salts thereof.

Abstract: The present invention provides novel prostaglandins D, that is, 13,14-dihydro-15-keto-PGDs, which have an excellent sedative and sleep-inducing activity, and so they are useful for tranquilizer and/or soporifics.

Abstract: The use of compounds of formula I as topical agents to combat the disorders of the skin produced by photodamage which disorders include: wrinklin, elastosis and premature aging is described. Compounds of formula I are ##STR1## wherein n represents 1 or 2, Z represents --S(O)R, wherein R represents lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkoxy-lower-alkyl, lower-alkanoyl-lower-alkyl, hydroxy-lower-alkyl, halo-lower-alkyl, lower-carbalkoxy-lower-alkyl, lower-alkoxy, hydroxy, mono-lower-alkyl amino or di-lower-alkylaminoand pharmaceutically acceptable salts thereof.

Abstract: A method of combatting insects comprising contacting insects with an insecticidally effective amount of L-2-amino-4-[(hydroxy) (methyl) phosphinyl]-butyryl-L-alanyl-L-alanine.

Abstract: Oxime ethers of the general formula ##STR1## where R.sup.1 and R.sup.2 are hydrogen or alkyl,R.sup.3 is hydrogen, halogen, cyano, aryl or aryloxy, the aromatic ring being unsubstituted or substituted, or R.sup.3 is heteroaryl, adamantyl, fluorenyl or cycloalkyl or cycloalkenyl, these radicals being unsubstituted or substituted,X is saturated or unsaturated C.sub.1 -C.sub.12 -alkylene which is unsubstituted or substituted, andn is 0 or 1,and fungicides containing these compounds.

Abstract: Novel 1,3-diaryl cyclopentanes of the following general formula were prepared. ##STR1## These compounds were found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and as such useful in the treatment or amelioration of various diseases or disorders mediate by the PAF, for example, hypotension, inflammation, nephritis, stroke and other cardiovascular disorders, asthma, allergic and skin diseases, peptic or stomach ulcer, shock, lung edema, psoriasis, adult respiratory distress syndrome, pain including dental pain, and aggregation of platelets.

Abstract: The invention provides fungicidal compositions which comprise a carrier and, as active ingredient, a compound of the general formula ##STR1##

Abstract: Compounds of the formula (I): ##STR1## exhibit anti-cholingeric and calcium antagonistic action and are used for treating pollakiuria and incontinence in humans and animals.

Abstract: 2-Acylaminoalkyl-3-[1-(carboxycycloalkylcarbamoyl)cycloalkyl]propanoic acid derivatives (which may also be viewed as glutaramide derivatives) are useful in the treatment of hypertension, heart failure and renal insufficiency, based upon their inhibition of zinc-dependent, neutral endopiptidase.

Abstract: Certain 9,11-diacyl prostaglandins and their use for lowering intraocular pressure are disclosed herein.

Abstract: A series of novel spiro-substituted glutaramide derivatives have been prepared, including the pharmaceutically acceptable salts thereof and bioprecursors therefor, wherein the spiro-substituent completes a 5- or 6-membered carbocycyclic ring and is located at the carbon atom adjacent to the carbamoyl group. These particular compounds are inhibitors of the neutral endopeptidase E.C.3.4.24.11 enzyme and are therefore useful in therapy as diuretic agents for the treatment of hypertension, heart failure, renal insufficiency and other disorders. Methods for preparing these compounds from known starting materials are provided.

Abstract: The present invention is concerned with methods for the treatment and diagnosis of pulmonary hypertension which comprise the administration of an effective amount of a compound of formula (I) ##STR1## wherein X is hydrogen or methyl;Y is --O-- or --CH.sub.2 --;R is --C(R.sup.1)(R.sup.2)CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.3 wherein R.sup.1 and R.sup.2, which may be the same or different, are selected from hydrogen and halogen; andthe dotted line represents an optional double bond; andpharmaceutically acceptable salts and acid derivatives thereof.Medicaments and diagnostic aids for use in the methods of the invention are also within the scope of the invention.

Abstract: Disclosed is an intraocular pressure reducing method and composition wherein 9,15-diacyl prostaglandins are contained in a pharmaceutically acceptable excipient for topical application on the surface of the eye.

Abstract: Prostaglandin analogues exhibiting activity at thromboxane receptor sites have been prepared.

Abstract: The instant invention is a novel use of known cyclic amino acids. Such compounds, including gabapentin, are useful for treating major and minor forms of depression.

Abstract: Seco-mevinic acid derivatives are provided which has the structure ##STR1## including all stereoisomers thereof, wherein Z is ##STR2## R is H, alkali metal or lower alkyl, R.sup.1 is H, lower alkyl, aryl, lower alkoxy, cycloalkyl, heteroaryl, aralkyl, heteroaralkyl or heterocyclic; R.sup.2 is lower alkyl, cycloalkyl or aralkyl, and X is O or NR.sup.5 wherein R.sup.5 is H or lower alkyl, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis. New intermediates for preparing the above seco-mevinic acid derivatives are also provided.

Abstract: The invention relates to 6-oxo-prostaglandin E.sub.1 derivatives of formula I, ##STR1## in which R.sup.1 means the radical COOR.sup.2 with R.sup.2 meaning a hydrogen atom, C.sub.1 -C.sub.10 alkyl, a C.sub.5 -C.sub.6 cycloalkyl or a C.sub.6 -C.sub.10 aryl group or a heterocyclic radical, or the radical CONHSO.sub.2 R.sup.5 as C.sub.1-10 alkyl, C.sub.5-6 cycloalkyl or C.sub.6-10 aryl,A means an E-configuration CH.dbd.CH or a --C.dbd.C group,W means a free or functionally modified hydroxymethylene group or a free or functionally modified group, and the OH group in each case can be in the alpha or beta position,D means a straight-chain or branched-chain alkylene group with 1-5 C atoms,E means a --C.dbd.C group or a C.sub.2 -C.sub.4 alkenylene group,R.sup.3 means C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.10 cycloalkyl or an optionally substituted C.sub.6 -C.sub.10 aryl group or a heterocyclic group,R.sup.4 means a free or functionally modified hydroxy group, and if R.sup.

Abstract: The invention relates to a means of reducing or maintaining intraocular pressure, and, more particularly, to a method and composition for reducing or maintaining intraocular pressure involving the administration of a composition containing prostaglandin F.sub.3.alpha. in a pharmaceutically acceptable carrier.

Abstract: Novel compounds have a formula (I) ##STR1## wherein ##STR2## represents a bicyclo [2,2,1] hept-2Z-ene, bicyclo [2,2,1]heptane, 7-oxa-bicyclo [2,2,1] hept-2Z-ene, 7-oxa-bicyclo [2,2,1] heptane, bicyclo [2,2,2] oct-2Z-ene or bicyclo [2,2,2] octane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group ANR.sup.2 R, a 6,6-dimethyl-bicyclo [3,1,1] heptane substituted at the 2-position by the group R.sup.1 and at the 3-position by the group ANR.sup.2 R or at the 2-position by the group ANR.sup.2 R and at the 3-position by the group R.sup.1, a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R.sup.1 and at the 5-position by the group ANR.sup.2 R or a 1-hydroxyclopentane substituted at the 2-position by the group R.sup.1 and at the 2-position by the group ANR.sup.2 R, R.sup.

Abstract: The invention relates to 9-halo-15-cycloalkyl prostaglandin derivatives of Formula I ##STR1## wherein R.sub.1 is hydrogen or methyl,R.sub.2 is fluorine or chlorine,n is 0 or 1,and, if R.sub.1 is hydrogen, the salts thereof with physiologically compatible bases or the cyclodextrin clathrates thereof, processes for their preparation, and their pharmaceutical usage.

Abstract: Disclosed are novel 3-hydroxy-3-methylglutarylcoenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by the formula ##STR1## and the corresponding ring-opened hydroxy acids and esters derived therefrom and pharmaceutically acceptable salts thereof.Pharmaceutical compositions containing said compounds and method of inhibiting the biosynthesis of cholesterol therewith are also disclosed.

Abstract: The present invention relates to ocular hypotensive agents which contains 13,14-dihydro-15-keto-prostagrandins, which shows no transient ocular hypertensive response that PGs usually show.

Abstract: This invention provides a fervescence composition containing 15-keto-PHEs separated from any substantial activity such as decrease of blood pressure.

Abstract: Compounds and their use for lowering intraocular pressure are disclosed herein.

Abstract: 11-Haloprostane derivatives of general Formula I ##STR1## wherein X is F, Cl or Br,R.sub.1 is the residue CH.sub.2 OH or ##STR2## wherein R.sub.2 means a hydrogen atom, an alkyl, cycloalkyl, aryl, phenacyl or heterocyclic residue,A is a --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH--group,B is a --CH.sub.2 --CH.sub.2 -- or trans--CH.dbd.CH-- or a --C.tbd.C--group,W is an ethylenedioxymethylene group or a hydroxymethylene group,D and E together mean a direct bond orD is a C.sub.1-10 -alkylene group,E is an oxygen or sulfur atom, a direct bond, a --C.tbd.C--bond or a --CR.sub.6 .dbd.CR.sub.7 -group with R.sub.6 and R.sub.7 meaning a hydrogen atom, a chlorine atom or an alkyl group,R.sub.4 is a hydroxy group,R.sub.5 is a hydrogen atom, an alkyl, a cycloalkyl, an aryl or a heterocyclic group, andthe salts thereof with physiologically compatible bases, processes for their preparation, and use thereof as agents inhibiting gastric acid secretion.

Abstract: Prostaglandin derivatives having an oxo group at specified positions in the .alpha. side chain have a variety of physiological effects, notably a strong anti-ulcer activity accompanied by a limited ability to inhibit blood platelet aggregation.

Abstract: Compounds of the formula ##STR1## wherein A is a carbocyclic, saturated or unsaturated ring; R.sup.1 is hydrogen or alkyl; R and R.sup.4 are each alkyl, cycloalkyl, benzyl or a readily hydrolyzable ester group; Y is a bond or a straight or branch alkylene; R.sup.2 is hydrogen, aryl, heterocyclic, R.sup.6 CONR.sup.5, R.sup.7 NR.sup.5 CO, R.sup.7 NR.sup.5 SO.sub.2 --or R.sup.8 SO.sub.2 NR.sup.5 --where R.sup.5 is hydrogen, alkyl or aralkyl; R.sup.6 is alkyl, aryl, aralkyl, heterocyclic, heterocyclyalkyl or a group of the formula ##STR2## where R.sup.9 is hydrogen, hydroxy, alkoxy, alkyl, hydroxyalkyl, aralkyl, alkylene, heterocyclic, heterocyclylalkyl, R.sup.12 CONH--, R.sup.12 SO.sub.2 NH-- or (R.sup.13).sub.2 N--; R.sup.10 and R.sup.11 are each hydrogen or alkyl; or R.sup.10 is hydrogen and R.sup.11 is aminoalkyl, imidazolylmethyl, aryl, aralkyl, aralkoxyalkoxy, hydroxyalkyl or methylthioalkyl; or R.sup.10 and R.sup.

Abstract: The invention also relates to carbacyclin derivatives of general formula I' ##STR1## wherein R.sub.9 is an alkyl group of 1-10 carbon atoms or the group --C.dbd.C--(CH.sub.2).sub.m --R.sub.6 whereinm is 1 to 16 andR.sub.6 is hydroxy on amino.

Abstract: The compounds of formula I, ##STR1## where the substituents have various significances, and physiologically acceptable hydrolyzable derivatives thereof having the hydroxy group in the 2 position of the 3-aminopropoxy side chain in esterified form, are useful as cardioselective .beta.-adrenoceptor blocking agents.

Abstract: An L-dopa derivative represented by formula (I) ##STR1## wherein one of R.sup.1 and R.sup.2 denotes a hydrogen atom and the other denotes a group of formula R--CO-- in which R denotes an alkyl, alkenyl, optionally substituted cycloalkyl, optionally substituted phenyl, optionally substituted aralkyl, lower alkoxy or optionally substituted aralkyloxy group,and its acid addition salt. The compounds are useful in the medical field, especially in the treatment of a series of diseases called Parkinson's disease or Parkinsonism.

Abstract: 2-Acylaminoalkyl-3-[1-(carboxycycloalkylcarbamoyl)cycloalkyl]propanoic acid derivatives (which may also be viewed as glutaramide derivatives) are useful in the treatment of hypertension, heart failure and renal insufficiency, based upon their inhibition of zinc-dependant, neutral endopiptidase.