The present invention relates to 5-thia- .omega. -substituted phenyl--prostaglandin E derivatives of the formula (I) (see formula I) (wherein, all the symbols are as defined in the specification), process for producing them and pharmaceutical compositions comprising them as active ingredient. The compounds of the formula (I) can bind to PGE2 receptors (especially, subtype EP4) strongly, so they are expected to be useful for prevention and/or treatment of immunological diseases (autoimmune diseases such as amyotrophic lateral sclerosis (ALS), multiple sclerosis, Sjoegren's syndrome, chronic rheumarthrosis and systemic lupus erythematosus etc., and rejection after organ transplantation etc.), asthma, abnormal bone formation, neuronal cell death, lung failure, liver damage, acute hepatitis, nephritis, renal insufficiency, hypertension, myocardiac ischemia, systemic inflammatory response syndrome, ambustion pain, sepsis, hemophagous syndrome, macrophage activation syndrome, Still's disease, Kawasaki disease, burn, systemic granulomatosis, ulcerative colitis, Crohn's disease, hypercytokinemia at dialysis, multiple organ failure, and shock etc. Further, it is thought that EP4 subtype receptor relates to sleeping disorder and blood platelet aggregation, so the compounds of the present invention are expected to be useful for the prevention and/or treatment of such diseases.

5-thia-omega-substituted phenyl-prostaglandin e derivatives, process for producing the same and drugs containing the same as the active ingredient

The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula (I), wherein hatched lines represent the α configuration, a triangle represents the β configuration and a dotted line represents the presence or absence of a double bond; A and B are independently selected from the group consisting of O, S and CH2 provided that at least one of A or B is S; D represents a covalent bond or CH2, O, S or NH; X is CO2R, CONR2, CH2OR, P(O)(OR)2, CONRSO2R SONR2 or Y is O, OH, OCOR2, halogen or cyano; Z is CH?2? or a covalent bond; R is H or R?2; R1? is H, R2, phenyl, or COR?2; R2 is C?1-C5 lower alkyl and R3 is C1-C5 n-alkyl, C3-C7 cycloalkyl, phenyl, furanyl, thienyl, or substituted derivatives thereof, wherein the substituents may be selected from the group consisting of C1-C5 alkyl, halogen, CF3, CN, NO2, CO2R and OR.

3, 7 or 3 and 7 thia or oxa prostanoic acid derivatives as agents for lowering intraocular pressure

Certain prostaglandin analogues are useful in the treatment of glaucoma and ocular hypertension. Also disclosed are ophthalmic, pharmaceutical compositions comprising such prostaglandin analogues.

Use of certain prostaglandin analogues to treat glaucoma and ocular hypertension

A sleep inducing agent comprising, as an active component, a prostaglandin derivative represented by formula (1), wherein X represents a halogen atom, Y represents a group represented by (CH2)m, a cis-vinylene group or a phenylene group, Z represents an ethylene group, a trans-vinylene group, OCH2 or S(O)nCH2, R is a C3-10 cycloalkyl group, a C3-10 cycloalkyl group substituted with a C1-4 alkyl group, a C4-13 cycloalkylalkyl group, a C5-10 alkyl group, a C5-10 alkenyl group, an C5-10 alkynyl group or a bridged cyclic hydrocarbon group, R represents a hydrogen atom, a C1-10 alkyl group or a C3-10 cycloalkyl, m is an integer of 1 to 3, and n is 0, 1 or 2, or a pharmaceutically acceptable salt or hydrate thereof.

Sleep inducing agent

A method for preventing or treating xerosis which comprises applying a prostaglandin D receptor selective agonist to a mammal.

Pharmaceuticals for xerosis

A prostaglandin derivative represented by general formula (I), a salt thereof, and a medicinal composition containing the same as the active ingredient for lowering the ocular tension. In said formula, R1 represents hydrogen, C1-C10 alkyl or C3-C10 cycloalkyl; R2 represents C3-C10 cycloalkyl optionally substituted by methyl, C1-C3 alkyl substituted by C3-C10 cycloalkyl, or C5-C10 branched alkyl or alkenyl; X represents .alpha.- or ~- chloro; and A represents ethylene, vinylene or ethynylene. This compound is useful as an ocular tension depressant which is free from side effects of, e.g., transient increased tension or is extremely reduced in these side effects.

Prostaglandin derivative, salt thereof, and use thereof

Object: to provide a novel prostaglandin E1 which is excellent in drug efficacy while reduced in adverse reactions as compared with conventional ones. Constitution: a PGE1 analogue represented by general formula (I) and its salt, wherein A represents vinylene or ethynylene; R1 represents hydrogen, C?1? to C6 alkyl or aryl; and R?2? represents C?5? to C10 branched aliphatic hydrocarbyl.

Prostaglandin e1 analogue

A prostaglandin E1 analog represented by formula (I), wherein R1 represents hydrogen or C?1?-C6 alkyl; and X represents oxygen and R?2? represents (a) or (b); or alternatively, X represents sulfur and R2 represents (c). This compound has a potent and persistent platelet aggregation inhibitor activity and is useful for treating various thrombotic diseases typified by peripheral circulatory disturbance.

Prostaglandin e1 analog

To produce a prostaglandin E in a short time and in a high yield while minimizing the formation of isomers. A process for producing a prostaglandin E represented by general formula (I) wherein A represents an arbitrary group not participating in the reaction; B represents vinylene or ethynylene; R?4 and R5? may be the same or different from each other and each represents hydrogen or a protective group for a hydroxyl group; and R?6 and R7? represent each an arbitrary group not participating in the reaction, which comprises reacting an allyl ester of a prostaglandin E represented by general formula (II) wherein R?1 and R2? may be the same or different from each other and each represents hydrogen or lower alkyl; R3 represents hydrogen, lower alkyl, alkenyl or aryl; and R?4, R5, R6, R7?, A and B are each as defined above, with one or two compounds selected from the group consisting of bases and formic acid in the presence of a complex compound or a complex salt of 0-valent or divalent palladium atom.

Process for producing prostaglandin e.

PURPOSE:To provide a platelet aggregation-inhibiting agent containing a prostaglandin E1 analogue as an active ingredient, excellent in its medicinal effect, good in durability, and not inducing the diarrhea of adverse action. CONSTITUTION:The platelet aggregation-inhibiting agent contains a compound of the formula (R is H, 1-6C alkyl) or its salt, e.g. (2E,16RS)16,20- dimethyl-2,3,13,14,18,18,19,19-octadehydro-prostaglandin E1-methyl ester as an active ingredient. The agent can be prepared in the form of tablets, granules, capsules. solution, emulsion, injection, suppositories or pessaries. The agent is administered at a dose of 0.1-100mug once to three times a day. The agent is useful for treating and preventing thrombotic diseases, and further useful for treating peripheral arterial obstruction because of its having an angiectatic action.

Platelet aggregation-inhibiting agent

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