Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.

Abstract: A prostaglandin derivative represented by the formula: wherein X is a halogen atom in the &agr;- or &bgr;-position, Y is an ethylene group, a vinylene group or an ethynylene group, A is a group represented by the formula: O(CH2)n, S(O)p(CH2)n, O(CH2)qO(CH2)r, O(CH2)qS(O)p(CH2)r, S(O)p(CH2)qS(O)p(CH2)r or S(O)p(CH2)qO(CH2)r (wherein n is an integer of 1 to 5, p is 0, 1 or 2, q is an integer of 1 to 3, and r is 0 or 1), R1 is a C3-10 cycloalkyl group, a C1-4 alkyl-C3-10 cycloalkyl group, a C3-10 cycloalkyl-C1-4 alkyl group, a C5-10 alkyl group, a C5-10 alkenyl group, a C5-10 alkynyl group or a bridged cyclic hydrocarbon group, R2 is a hydrogen atom, a C1-10 alkyl group or a C3-10 cycloalkyl group, and m is 0, 1 or 2], a pharmaceutically acceptable salt thereof or a hydrate thereof. The present invention is to provide novel PG derivatives having an excellent PGD2-like agonistic activity and a sleep-inducing action.

Abstract: The invention is a novel series of cyclic amino acids which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.

Abstract: 15-fluoro substituted analogs of PGF2&agr; and methods of their use in treating glaucoma and ocular hypertension are disclosed.

Abstract: A magnetic recording medium and method for forming the magnetic recording medium are described. The magnetic recording medium includes a magnetic layer formed on a non-magnetic support, and a lubricant layer over the magnetic layer. The lubricant layer includes a compound selected from the group consisting of hydrocarbyl-substituted cyclopentanes, hydrocarbyl-substituted cyclopentenes, hydrocarbyl-substituted cyclopentadienes, and mixtures or derivatives thereof. The lubricant layer also may be used on a magnetic head for reading and writing information on a magnetic recording medium. The magnetic recording medium and the magnetic head may be used to manufacture computer disk drives, compact disk drives, audio equipment, and video equipment.

Abstract: 15-Fluoro substituted analogs of PGF2&agr; and methods of their use in treating glaucoma and ocular hypertension are disclosed.

Abstract: The present invention relates to methods, compositions, devices and kits for the prevention and treatment of prostate disorders in mammals, including, but not limited to, benign prostatic hypertrophy, carcinoma of the prostate, prostadynia, prostatitis, and chronic prostatitis. The present invention provides methods for preventing and treating prostate disorders in mammals by administration of a therapeutic compound to mucosal membranes in the lower urinary tract of the mammal. The present invention also provides devices for administering a therapeutic compound to mucosal membranes in the lower urinary tract of the mammal.

Abstract: The invention provides novel compounds of the Formula (I) that stimulate rates of glucose oxidation in myocardial cells.

Abstract: A method is provided for making an enantiomerically pure of the formula: in which R and R′ represent C1?C10 alkyl, C2?C10 alkenyl or C3?C10 cycloalkyl and the wedges signify (S)- or (R)-stereochemistry, the substituents in compound (II) being trans. Conjugate addition is carried out between an organometallic nucleophile that provides a group R as defined above and (R)-4-acetoxycyclopent-2-en-1-one, (S)-4-acetoxycyclopent-2-en-1-one or a similar compound in which acetoxy is replaced by another leaving group to give, e.g.

Abstract: The invention relates to the use of derivatives of E-type prostaglandins as EP2 agonists, in general, and, in particular as ocular hypotensives.

Abstract: The present invention relates to small molecules according to the formula [I]: 1

Abstract: The invention relates to a process for preparing substituted cyclopentane derivatives represented by the formula (I) wherein R1, R2, R3, R4, X and Y are as described in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to a process for purifying the compound of formula (Ia) and novel crystalline forms of the compound of formula (Ia).

Abstract: Compositions and methods for the treatment of dry eye and related diseases utilizing 6-keto-PGF1&agr; and its analogs are disclosed.

Abstract: Compounds I-III wherein U is CH, O, or S; Z is mono- or di-substituted carbon; R is (CH2)nCO2H, (CH2)nSO3H, (CH2)nPO3H2, (CH2)nNO2, CH(SCH3)3, esters; R1 is H, hydroxyalkyl, aminoalkyl, alkoxyalkyl; RR1 is O; n is 0-4; R2, R3 is H, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkyl; R4 is (CH2)nOH, (CH2)nNH2, substituted alkyl were prepd. as neuraminidase inhibitors. Thus, (1R,3R,4R,1′S)-(−)-(1′-acetylamino-2 ′-ethyl)butyl-4-(aminoimino)methylaminocyclopentan-1-carboxylic acid was prepd. and tested in vitro as neuraminidase inhibitor (IC50<1.mu.M).

Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.

Abstract: An improved method is described for making 9-deoxy-PGF1-type compounds. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds.

Abstract: The invention relates to the use of an oxidation inhibitor, i.e. active carbon, for ambient air in industrial manufacturing, especially in the processing of prostane derivatives, whereby the oxidation inhibitor removes ozone from the process air before contact with said prostane derivatives. The concentration of decomposition products is reduced.

Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.

Abstract: The present invention provides a simplified and convenient process for the preparation of an optically active enone such as 7,7-dimethyl-6,8-dioxabicyclo-[3,3,0]oct-3-en-2-one. The invention further provides novel optically active intermediate compounds.

Abstract: A liquid chromatography-electrospray ionization mass spectrometry method is capable of separating and identifying different prostaglandin isomers, including PGD2 and PGE2. Unlike traditional gas chromatography methods, little sample preparation and no derivatization are required. The chromatography is performed under acidic conditions that are optimal for separating the isomers. A basic sheath flow liquid is added to the chromatographic eluent, resulting in high ionization efficiency when the electrospray ionization is performed in negative ion mode. Additionally, by altering the energy at which the ionization is performed, tandem mass spectra of the two isomers can be made to differ as a result of the different relative energies of the two isomers.

Abstract: The invention relates to compositions and methods for the treatment of dry eye and related diseases utilizing 6-keto-PGF1&agr; and its analogs, according to formula (I); wherein A,B,D,Q9, Q11, R1, X and Y have the meanings given in the description. Some of these compounds are novel.

Abstract: The invention provides novel prostaglandin analogs. In particular, the present invention relates to compounds having a structure according to formula (I) wherein R1, R2, R3, R4, R5, R6, W, X, Z, a, b, p and q are defined below. This invention also includes optical isomers, diastereomers and enantiomers of formula (I), and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using these compounds or the compositions containing them.

Abstract: An improved method is described for making 9-deoxy-PGF1-type compounds. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds.

Abstract: Described is a bioprocess for the high-yield production of food flavor-acceptable jasmonic acid and methyl jasmonate, as well as a novel jasmonic acid isomer produced thereby and organoleptic uses thereof.

Abstract: The invention concerns compounds of formula (I): in which: R1 to R4, identical or different, represent hydrogen, alkyl or aryl, themselves substituted if required, R1 and R2 together further capable of representing a bridge —(CH2)m in which m is a whole number from 1 to 5, or a bridge X representing a linear combination of m hydrocarbon groups, m being as defined above and comprising, if required, at least a heteroatom such as O, N or S, or a bridge X representing a linear combination of p heteroatoms O, N and/or S, in which p is a whole number from 1 to 3; A1 and A2 represent —COOH, —SO3H or —PO3H2 radicals, or their derivatives such as esters or amides, or only one of A1 or A2 has these meanings, when R1 and R2 represent a single bond between the carbons in positions 3 and 4, the other of these groups being a hydrogen atom; Y represents a chain —(CH2)n—, n being zero or a whole number from 1 to 5, or represents a linear combination of n hydrocarbon group

Abstract: Disclosed as endothelin converting enzyme inhibitors are the compounds of the formula wherein the variables have the meanings as defined hereinbefore.

Abstract: The invention provides novel prostaglandin analogs. In particular, the present invention relates to compounds having a structure according to formula (I) wherein R1, R2, R3, R4, R5, R6, W, X, Z, a, b, p and q are defined below. This invention also includes optical isomers, diastereomers and enantiomers of formula (I), and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using these compounds or the compositions containing them.

Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma a therapeutically effective amount of a 3, 7 or 3 and 7 thia or oxa prostanoic acid derivative.

Abstract: The present invention is directed to novel methods of prostanoid synthesis. Specifically, the invention is directed to the addition of alpha chains to prostanoids using cis-alkenylstannane intermediates.

Abstract: 5-Membered ring compounds represented by general formula (I), optically active isomers thereof or salts of the same. These compounds have physiological activities including a carcinostatic effect. In said formula the bond shown by the dotted line in the 5-membered ring represents that this 5-membered ring may be either a cyclopentene ring having a double bond or a saturated cyclopentane ring, and when the 5-membered ring is a cyclopentene ring, X is OR1, Y is ═O and Z is H, and when it is a cyclopentane ring, X is ═O, Y is OR2 and Z is OR3, (wherein R1 is R4 or —(CO)—R5; R2 is H, —R6 or —(CO)—R7; and R3 is H, R8 or (CO)—R9 (wherein R4, R5, R6, R7, R8 and R9 are the same or different and each represents an aliphatic, aromatic or aliphatic aromatic group, and R5, R7 and R9 may be each H), provided that the case where R2═R3═H is excluded); and W represents a residue obtained by eliminating SH from an SH-containing compound.

Abstract: A method of treating glaucoma or ocular hypertension in a patient, which comprises administering to the patient a pharmaceutically effective amount of a compound of formula I:

Abstract: A compound of the formula: wherein R1 and R2 each represents a lower alkyl, or R1 and R2 may be bonded together to form a ring; X represents a spacer of which the number of atoms constituting the principal chain is 1 to 15; Y represents an acyl, or a hydroxy, an amino or an aromatic group, each of which may be substituted; and ring A represents a 5- to 8-membered ring which may be further substituted apart from —X—Y, or a salt thereof is useful as a pharmaceutical composition for preventing or treating disease related to mitochondrial dysfunction.

Abstract: A composition which comprises human mesenchymal stem cells which have the potential to differentiate into cells of more than one connective tissue type and a composition which induces cells from the mesenchymal stem cell population to differentiate into the adipogenic lineage, and a process for inducing such differentiation. The composition for inducing such differentiation comprises a glucocorticoid, a compound which stimulates cAMP production or inhibits cAMP degradation (such as a phosphodiesterase inhibitor), and/or a compound which upregulates peroxisome proliferator activated receptor &ggr; (PPAR &ggr;) expression and/or increases its binding affinity to its DNA binding site. The process can further include isolating the adipocytes from remaining hMSCs.

Abstract: A hydroxy-1-alkyne is reacted with a tin hydride compound, and the obtained (E,Z)-hydroxyvinylstannanes are separated to give the (E)-substance which is further converted to a vinylcopper complex shown by followed by the conjugate addition reaction with an &agr;, &bgr;-unsaturated cyclopentenone, and the deprotecting reaction is subsequently carried out to prepare a prostaglandin or an intermediate of prostaglandins easily, efficiently and industrially favorably.

Abstract: The present invention provides 11,15-O-dialkyl prostaglandin E derivatives of formula (I) (wherein all symbols are as described in Specification), or non-toxic salts thereof or cyclodextrin clathrates thereof, processes for the preparation thereof and pharmaceutical compositions containing them as active ingredient. A compound of formula (I) binds strongly and acts on EP3 receptor which is a subtype of PGE2 receptor and therefore is useful for prevention and/or treatment of liver diseases, kidney diseases, pancreatitis, myocardial infarction etc.

Abstract: The novel 13,14-dihydro-15-keto prostaglandins E of the invention have remarkable preventive effects against ulcers. Further, the novel 13,14-dihydro-15-keto-prostaglandins E of the invention have an advantage that they have none of side effects which prostaglandin E intrinsically has, or can remarkably reduce such effects of the prostaglandin E. Therefore, the novel 13,14-dihydro-15-keto prostaglandins E of the invention are effective for animal and human use for treatment and prevention of ulcers, such as duodenal ulcer and gastric ulcer.

Abstract: A method for preventing adverse effects associated with the use of a medical device in a patient by introducing into the patient a device of which at least a portion includes a prophylactic or therapeutic amount of a nitric oxide adduct. The nitric oxide adduct can be present in a matrix coating on a surface of the medical device; can be coated per se on a surface of the medical device; can be directly or indirectly bound to reactive sites on a surface of the medical device; or at least a portion of the medical device can be formed of a material, such as a polymer, which includes the nitric oxide adduct. Also disclosed is a method for preventing adverse effects associated with the use of a medical device in a patient by introducing the device during a medical procedure and before or during said procedure locally administering a nitric oxide adduct to the site of contact of said device with any internal tissue.

Abstract: (wherein R1 is OH etc.; X is Cl, F; R2 is H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl which may be substituted; n is 0-4.), non-toxic salts thereof or cyclodextrin clathrates thereof can strongly bind on EP2 subtype receptor. Therefore, they are useful for the prevention and/or treatment of immunological diseases (autoimmune diseases, post-transplantation graft rejection etc.), asthma, abnormal bone formation, neuronal cell death, hepatopathy, abortion, premature birth or retina neuropathy (e.g. glaucoma) etc.

Abstract: The invention relates to 9-halogen-(Z) prostane derivatives of formula I in which Z represents the radicals Hal represents a chlorine or fluorine atom in the alpha or beta position, R1 represents the radical with R2 meaning a hydrogen atom, an alkyl, cycloalkyl, aryl or heterocyclic radical or R1 represents the radical with R3 meaning an acid radical or the radical R2 and A represents a —CH2—CH2—, a trans-CH═CH or —C≡C group, W represents a free or a functionally modified group, and the respective OH groups can be in the alpha or beta position, D and E together represent a direct bond or D represents a straight-chain alkylene group with 1-10 C atoms, a branched-chain alkylene group with 2-10 C atoms or an annular alkylene group with 3-10 C atoms, which optionally can be substituted by fluorine atoms, and E represents an oxygen or sulfur atom, a direct bond, a C≡C bond or a

Abstract: Formula (I) compounds: wherein R1 is alkyl substituted by fluorine(s); R2 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR3R4, in which R3, R4 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl subsituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R3 and R4, taken together is a saturated heterocyclic ring or amino acid residue; and non-toxic salts and acid addition salts thereof.

Abstract: A compound represented by the following formula [I] or an optically active substance or a salt thereof. (In the formula, a bond shown by a dotted line in the five-membered ring means that said five-membered ring may be any of a cyclopentene ring having a double bond and a cyclopentane ring where said bond is saturated and, in the case of a cyclopentene ring, X is OH, Y is ═O and Z is H while, in the case of a cyclopentane ring, X is ═O, Y is OH and Z is OH. R is a residue after removal of an SH group from the SH-containing compound.

Abstract: 14-Aza analogs of PGF.sub.2.alpha., PGD.sub.2, and PGE.sub.2 and methods of their use in treating glaucoma and ocular hypertension are disclosed.

Abstract: The present invention relates to a compound represented by the following general formula (1) ##STR1## (wherein X represents O, S, SO, SO.sub.2, or NH, Y is a substituted or unsubstituted hydrocarbon residue containing 1 through 6 carbon atoms and having an overall molecular weight of not less than 15 and not more than 400, and the hydrocarbon residue, when the residue is ring, may contain one or two hetero-atoms in the ring, and Z is a carboxyl group, a group derived therefrom or an aliphatic hydrocarbon residue having from 1 to 4 carbon atoms which may be substituted or unsabstituted) or a pharmacologically acceptable salt thereof (excluding (1R,2S)-2-[(2R)-(2-acetyl-amino-2-carboxyethyl)thiomethyl]-3-oxo-1-cyclope ntane-carboxylic acid (cystacyclin)), a method for production thereof and a medicinal use thereof. The compound of the present invention is useful as a neuron differentiation accelerator.

Abstract: A shell and tube heat exchanger reactor with forced circulation is used to improve heat and mass transfer for exothermic liquid--liquid, gas-liquid and gas-liquid-solid reactions. Enhanced productivity and selectivity are obtained.

Abstract: It has been surprisingly discovered that the disadvantages of the lengthy literature procedures to synthesize 13,14-dihydro prostaglandin A, E, and F derivatives can be overcome using a novel Methyl 7-(2-hydroxy-5-(2-(2-oxiranyl)ethyl)-4-(1,1,2,2 tetramethyl-1-silapropoxy)cyclopentyl) heptanoate intermediate, which can be synthesized from commercially available Methyl 7-[3-(R)-hydroxy-5-oxo-1-cyclopent-1-yl] heptanoate. This novel intermediate can be coupled with oxygen, carbon, sulfur, and nitrogen nucleophiles, in the presence of a base or a Lewis acid, in a ring-opening process to provide 13,14-dihydro prostaglandin A, E, and F derivatives.

Abstract: The invention provides novel PGF analogs. In particular, the present invention relates to compounds having a structure according to the following formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, and Z are as defined. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof.The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using theses compounds or the compositions containing them.

Abstract: A 3,7-dithiaprostanoic acid derivative of the formula (I) ##STR1## (wherein, R.sup.1 is OH, C1.about.6 alkyloxy, NR.sup.6 R.sup.7 (R.sup.6, R.sup.7 are H, C1.about.6 alkyl.); R.sup.2 is H, OH; R.sup.3 is single bond, C1.about.6 alkylene; R.sup.4 is (i) C1.about.8 alkyl substituted by C1.about.6 alkyloxy, halogen etc., (ii) phenyloxy, C3.about.7 cycloalkyloxy, (iii) furyl, furyloxy, thienyl, thienyloxy, naphthyl, naphthyloxy, phthalanyl, phthalanyloxy, (iv) phenyl, phenyloxy, C3.about.7 cycloalkyl, C3.about.7 cycloalkyloxy substituted by C1.about.6 alkyl etc., (v) furyl, furyloxy, thienyl, thienyloxy, naphthyl, naphthyloxy, phthalanyl, phthalanyloxy substituted by C1.about.6 alkyl etc.; R.sup.5 is H, C1.about.6 alkyl.) can bind PGE.sub.2 receptor (particularly, EP4 subtype receptor) strongly. So, they are useful for the prevention and/or treatment of immunological diseases (autoimmune diseases, rejection after organ transplantation etc.

Abstract: A substituted cyclopentene derivative of formula (V): whereinX.sup.1 is (.alpha.-OZ.sup.a, .beta.-H) or (.alpha.-H, .beta.-OZ.sup.a), X.sup.3 is (.alpha.-OZ.sup.d, .beta.-H), (.alpha.-H, .beta.-OZ.sup.d), or oxygen atom, each of Z.sup.a and Z.sup.d, which may be the same or different, is a hydrogen atom or a protective radical for a hydroxyl radical;U is a radical selected from the group consisting of CR.sup.1 HCH.sub.2, CR.sup.1 .dbd.CH and C.tbd.C,whereinR.sup.1 is a hydrogen atom, halogen atom, substituted silyl radical represented by SiR.sup.9 R.sup.10 R.sup.11 or substituted stannyl radical represented by SnR.sup.14 R.sup.15 R .sup.16,m is an integer of 0 to 6;X.sup.2 is CH.dbd.CH or C.tbd.C,p is an integer of 0 or 1, each of n and q is an integer of 0 to 5; andZ.sup.1 is a hydrogen atom, COOR.sup.y, CN, OH, OCOR.sup.2, CONR.sup.b R.sup.c or NR.sup.d R.sup.e.

Abstract: A pharmaceutical compound of the formula: ##STR1## in which n is 1 or 2, R.sup.1 is --CO.sub.2 H, R.sup.2 is hydrogen or C.sub.1-4 alkyl andR.sup.3 is hydrogen, C.sub.1-10 alkyl, C.sub.2-10 alkenyl, optionally substituted phenyl, optionally substituted phenyl-C.sub.1-4 alkyl, optionally substituted phenyl C.sub.2-10 alkenyl,(optionally substituted phenyl).sub.2 -C.sub.1-4 alkyl, optionally substituted C.sub.3-7 cycloalkyl, optionally substituted C.sub.3-7 cycloalkyl-C.sub.1-4 alkyl or optionally substituted C.sub.3-7 cycloalkyl-C.sub.2-10 alkenyl, orR.sup.2 and R.sup.3, together with the carbon atom to which they are attached, form an optionally substituted C.sub.4-7 cycloalkyl group;or a salt or ester thereof other than the compounds .gamma.-propylidene-L-glutamic acid, .gamma.-ethylidene-L-glutamic acid and .gamma.-methylidene-L-glutamic acid.

Abstract: A prostaglandin having formula (I), (II), or (III): ##STR1## a process of production thereof, and inhibitors of cell migration caused by chemokines containing (I) or (II) as an active ingredient.