Abstract: The invention relates to compounds capable of inhibiting the visual cycle and/or dark adaptation and their use for treatment and prevention of non-degenerative retinal diseases with specific emphasis on the prevention and treatment of diabetic retinopathy, retinopathy of prematurity, branch retinal vein occlusion, central retinal vein occlusion, open-angle glaucoma, veovascular glaucoma, and other diseases of the retinal and/or optic nerve where an imbalance between metabolic demand and blood supply contribute to the development of tissue damage. The invention furthermore relates to pharmaceutical compositions comprising such compounds.

Abstract: Process for heterogeneously catalyzed preparation of carboxylic acid derivatives using a reactor system comprising at least one reservoir vessel V, feed lines, at least one pump and a reaction vessel R, characterized in that a permanent gas flow through the reaction vessel R is applied through a gas feed line, and in which a reaction chamber in which the heterogeneous catalyst is not introduced in tightly packed form is delimited by at least two filters such that both the mass flow and the gas flow are passed through the reaction chamber.

Abstract: A compound of formula (I) for use in the treatment of a disease of the immune system; wherein R is an optionally-substituted alkyl, alkenyl, alkynyl, aryl, arylalkyl or alkylaryl moiety having from 1 to 50 carbon atoms; R1 is an optionally-substituted alkyl, alkenyl, alkynyl, aryl, arylalkyl or alkylaryl moiety having from 1 to 40 carbon atoms; each of R2, R3 and R4 is independently selected from an optionally-substituted alkylene, alkenylene, alkynylene, arylene, arylalkylene or alkylarylene moiety having from 1 to 40 carbon atoms; each of X, Y and Z is independently selected from an optionally-substituted alkylene, alkenylene, alkenylene, arylene, alkylarylene, cycloalkylene, ketone, ester, amide, imide, imine, thioether, ether, thioester and thioketone; and P is selected from hydrogen, an alkyl group, a sugar residue, or a metal, phosphonium or ammonium species; wherein at least one of X, Y and Z includes a moiety selected from cyclopropyl, C=A, C-AH and C—OR5; wherein R5 is alkyl or haloalkyl, and A is O,

Abstract: The invention relates to novel resolvin compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel resolvin compounds of the invention.

Abstract: The invention features methods for the preparation of naturally occurring trihydroxy polyunsaturated eicosanoids and their structural analogs. The invention further provides new derivatives and analogs of trihydroxy polyunsaturated eicosanoids that can be prepared according to these methods. The invention also provides compositions and methods using trihydroxy polyunsaturated eicosanoid derivatives for the prevention, amelioration and treatment of a variety of diseases or conditions associated with inflammation or inflammatory response, autoimmune diseases, rheumatoid arthritis, cardiovascular diseases, or abnormal cell proliferation or cancer.

Abstract: The present invention relates to enantiomeric forms of hepoxilin analogs of Formula I-VIII, pharmaceutical compositions thereof, a method for the separation of said enantiomeric forms of hepoxilin analogs comprising applying said hepoxilin to a chiral phase HPLC column and eluting said hepoxilin with an alkane and alcohol solvent mixture. Said enantiomeric forms of hepoxilin analogs of Formula I-VIII were found to be useful in controlling the biological effects of PPAR mediated transcriptional control for the treatment of diseases such as cancer, thromboxane-mediated diseases and for modulating intracellular calcium concentration.

Abstract: Provided is a plant growth regulator having for an active ingredient thereof an ?-ketol fatty acid derivative represented by the following general formula (1)

Abstract: This invention provides new lipoxin analogs, compositions containing analogs, and methods of using these compounds and compositions for treating and preventing oral inflammation, including gingivitis, periodontitis, and other forms of periodontal disease. The invention also provides for methods of treating and preventing oral inflammation, including gingivitis, periodontitis, and other forms of periodontal disease with compositions containing COX-2 inhibitors. Further, the invention provides methods for preventing systemic diseases beyond theoral cavity that are related to periodontal disease using the composition containing lipoxin analogs, COX-2 inhibitors, or both.

Abstract: Disclosed herein are compounds represented by a formula: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.

Abstract: A compound of formula (I) for use in the treatment of a disease of the immune system; wherein R is an optionally-substituted alkyl, alkenyl, alkynyl, aryl, arylalkyl or alkylaryl moiety having from 1 to 50 carbon atoms; R1 is an optionally-substituted alkyl, alkenyl, alkynyl, aryl, arylalkyl or alkylaryl moiety having from 1 to 40 carbon atoms; each of R2, Wand R4 is independently selected from an optionally-substituted alkylene, alkenylene, alkynylene, arylene, arylalkylene or alkylarylene moiety having from 1 to 40 carbon atoms; each of X, Y and Z is independently selected from an optionally-substituted alkylene, alkenylene, alkenylene, arylene, alkylarylene, cycloalkylene, ketone, ester, amide, imide, imine, thioether, ether, thioester and thioketone; and P is selected from hydrogen, an alkyl group, a sugar residue, or a metal, phosphonium or ammonium species; wherein at least one of X, Y and Z includes a moiety selected from cyclopropyl, C=A, C-AH and C-OR5; wherein R5 is alkyl or haloalkyl, and A is O, S

Abstract: The present invention relates to enantiomeric forms of hepoxilin analogs of Formula I-VIII, pharmaceutical compositions thereof, a method for the separation of said enantiomeric forms of hepoxilin analogs comprising applying said hepoxilin to a chiral phase HPLC column and eluting said hepoxilin with an alkane and alcohol solvent mixture. Said enantiomeric forms of hepoxilin analogs of Formula I-VIII were found to be useful in controlling the biological effects of PPAR mediated transcriptional control for the treatment of diseases such as cancer, thromboxane-mediated diseases and for modulating intracellular calcium concentration.

Abstract: The invention concerns novel polyunsaturated compounds of formula (I) wherein: R1 represents a R?1, -A-R?1 group, R?1 being selected from —COOH, —COOR3, —CONH2, —CONHR3, —CONR3, R4, —CHO, —CH2OH, —CH2OR5, and A represents a C2-C16 alkylene, alkenylene or alkynylene; R2 represents: an optionally substituted aryl group or an optionally substituted heteroaryl group; a sugar residue or, a fatty acid residue optionally branched and/or substituted preferably at the chain terminus and particularly by hydroxy, acetoxy radical or by an optionally protected amino radical; a —OC—(CH2)n CO-tocopheryl (alpha, beta or gamma or delta) group, with 2 $m(F) n $m(F) 10; a —R?2—O—R6 group, wherein R?2 is an optionally substituted arylene group or an optionally substituted heteroarylene group, and R6 represents a hydrogen atom, a straight or branched optionally substituted C1-C16 alkyl, a straight or branched optionally substituted C2-C16 alkenyl, or a straight or branched C2-C16 alkynyl group, an optionally substituted tocophery

Abstract: A method for or treating xerosis by applying a prostaglandin D receptor selective agonist to a mammal.

Abstract: A method of treating atopy-evoked pruritic symptoms by administering a prostaglandin derivative.

Abstract: Long-chain esters of retinol are prepared via a chemoenzymatic process from short-chain retinyl esters and an appropriate long-chain acid or ester in the presence of an enzyme. Use of various additives enhance the yield of the desired ester and facilitated its purification.

Abstract: Long-chain esters of retinol are prepared via a chemoenzymatic process from short-chain retinyl esters and an appropriate long-chain acid or ester in the presence of an enzyme. Use of various additives enhance the yield of the desired ester and facilitated its purification.

Abstract: This invention relates to a method of reducing an irritating or adverse side effect associated with the topical use of an active ophthalmic drug comprising incorporating an effective amount of a cyclodextrin or cyclodextrin derivative into a formulation to complex the active drug such that the concentration of the free active drug is reduced below a tolerable threshold, and incorporating an effective amount of a viscosity increasing agent in said formulation such that the bioavailability of said drug is high enough to be therapeutically effective, wherein the cyclodextrin or cyclodextrin derivative is not required to solubilize the active drug. Another aspect of this invention relates to topical ophthalmic formulations comprising an active drug, a cyclodextrin or cyclodextrin derivative, and a viscosity-enhancing agent, in effective amounts as stated above.

Abstract: A sleep-inducing preparation which comprises as an effective ingredient a prostaglandin derivative represented by the formula: wherein X is a halogen atom, Y is a group represented by (CH2)m, a cis-vinylene group or a phenylene group, Z is an ethylene group, a trans-vinylene group, OCH2 or S(O)nCH2, R1 is a C3-10 cycloalkyl group, a C3-10 cycloalkyl group substituted with C1-4 alkyl group(s), a C4-13 cycloalkylalkyl 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, m is an integer of 1 to 3, and n is 0, 1 or 2, a pharmaceutically acceptable salt thereof or a hydrate thereof.

Abstract: A prostaglandin derivative represented by the formula: wherein X is a halogen atom, n is an integer of 1 to 5, R1 is a C3-10 cycloalkyl group, a C3-10 cycloalkyl group substituted with C1-4 alkyl group(s), a C4-13 cycloalkylalkyl group, a C5-10 alkyl group, a C5-10 alkenyl group, a C5-10 alkynyl group or a bridged cyclic hydrocarbon group, and R2 is a hydrogen atom, a C1-10 alkyl group or a C3-10 cycloalkyl group, or a pharmaceutically acceptable salt thereof.

Abstract: Oleamide is an endogenous fatty acid primary amide that possesses sleep-inducing properties in animals and has been shown to effect seratonergic systems and block gap junction communication in a structurally specific manner. Certain agents can serve both as an oleamide agonist and as an inhibitor of fatty acid amide hydrolase. Fatty acid amide hydrolase is responsible for the rapid inactivation of oleamide in vivo. The structural features of oleamide required for inhibition of gap junction-mediated chemical and electrical transmission in rat glial cells are defined. Effective inhibitors fall into two classes of fatty acid primary amides of which oleamide and arachidonamide are the prototypical members. Of these two, oleamide constitutes the most effective and its structural requirements for inhibition of the gap junction are well defined.

Abstract: A drug for prevention and therapy of diseases caused by fibrinoid formation or thrombus formation, as well as a model animal of fibrinoid formation or thrombus formation in the lung is disclosed. The drug for preventing and treating diseases caused by fibrinoid formation or thrombus formation in the lung according to the present invention comprises an inhibitor of interleukin 6 as an effective ingredient. The model animal of the diseases caused by fibrinoid formation or thrombus formation in the lung is a rat in which fibrinoid formation or thrombus formation actually occurs by induction with interleukin 6.

Abstract: An optically active bisoxazoline compound of the formula [I]: ##STR1## wherein R.sub.1 represents alkyl group, cycloalkyl group, aralkyl group, phenyl group which may be substituted or alkoxy group and two geminal alkyl groups may be joined together to form a cyclic structure;R.sub.2 represents alkyl group, cycloalkyl group, aralkyl group, phenyl group which may be substituted;R.sub.3 represents hydrogen atom, (C2-C4)alkyl group or cycloalkyl group; andthe asterisk * represents an asymmetric carbon atom.

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.

Abstract: Compounds of the formula: ##STR1## wherein R.sup.2 and X are as described, are disclosed. The compounds are useful for treating dermatological disorders which are accompanied by epithelial lesions, e.g., acne and psoriasis, as well as malignant and premalignant epithelial lesions, tumours and precancerous changes of the mucous membrane in the mouth, tongue, larynx, oesophagus, bladder, cervix and colon.

Abstract: This invention relates to the synthesis of vegetable and synthetic oil adducts and to the adduct products having the formula ##STR1##

Abstract: Object: To provide novel prostaglandin E.sub.1 analogues which have more excellent pharmaceutical effects, longer duration of the effects and less side-effects than the prior art prostaglandin E.sub.1 's.Constitution: A PGE.sub.1 analogue represented by the formula: ##STR1## (wherein A is a vinylene group or an ethynylene group, R.sup.1 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or an allyl group, R.sup.2 is a branched aliphatic hydrocarbon group having 5 to 10 carbon atoms), or a salt thereof.

Abstract: Compounds of the general structure ##STR1## are disclosed, wherein X is O, C.sub.n, NH, or S, wherein n is 1, 2, 3 or 4; R1 is OH, CH.sub.3, CH.sub.2 OH, N.sub.3 or CH.sub.2 N.sub.3 ; R3 is H or CH.sub.3 ; R5 is Y-R2, wherein Y is a six-carbon chain optionally containing up to three double or triple bonds or a mixture of double and triple bonds up to a maximum of three; R2 is C.sub.1 -C.sub.10 alkyl OH, C.sub.1 -C.sub.10 alkyl N.sub.3 or COOR4, wherein R4 is H, a branched or unbranched C.sub.1 -C.sub.10 alkyl (including substituted alkyl radicals), cycloalkyl, preferably C.sub.5 or C.sub.6 cycloalkyl, or a five- or six-membered aryl radical (including substituted aryl radicals), i.e. R2 is COOH or an ester of R4; R6 is a seven-carbon chain optionally containing up to three double or triple bonds or a mixture of double and triple bonds up to a maximum of three; and . . . . . . indicates a single, double or triple bond.

Abstract: Process for the stereospecific synthesis of leukotriene B.sub.4 (LTB.sub.4) of 6Z, 8E, 10E configuration of formula ##STR1## in which a dibenzoate triether is prepared which is subjected to a reductive elimination according to the diagram ##STR2## so as to obtain a triether which is converted in order to obtain the leukotriene B.sub.4.

Abstract: The invention relates to homo-prostaglandin derivatives. More particularly, the present invention concerns 1a-homo derivatives of naturally occurring and synthetic prostaglandins, the corresponding bis- and trishomo-prostaglandin compounds, and their 1-esters and salts. The homo-prostaglandin compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma.

Abstract: This invention is directed to a method for stereoselectively preparing a syn-dihydroxylated compound comprising reacting a 3-hydroxyket-1-one and a sterically hindered dialkylated borane to form a complex at about -50.degree. C. to about 0.degree. C., and reducing the complex with hydride at about -25.degree. C. to about 50.degree. C.