Abstract

An oral pharmaceutical composition comprising (a) a specific fatty acid derivative, (b) a specific sweetening agent and (c) a pharmaceutically acceptable oily vehicle, and an oily liquid formulation comprising thereof is provided

IPC Classes  ?

• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
• A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
• A61K 31/5575 - Eicosanoids, e.g. leukotrienes having a cyclopentane ring, e.g. prostaglandin E2, prostaglandin F2-alpha

Abstract

Provided is an anti-human VAP-1 monoclonal antibody having high specificity. The monoclonal antibody may have a combination of a heavy chain variable region of SEQ ID NO. 1 and a light chain variable region of SEQ ID NO. 2; a combination of a heavy chain variable region of SEQ ID NO. 3 and a light chain variable region of SEQ ID NO. 4; a combination of a heavy chain variable region of SEQ ID NO. 5 and a light chain variable region of SEQ ID NO. 6; or an antibody binding fragment thereof. An immunoassay method using an anti-human VAP-1 monoclonal antibody according to the invention and a kit for use in the immunoassay are also provided.

IPC Classes  ?

• C07K 16/40 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against enzymes
• G01N 33/573 - ImmunoassayBiospecific binding assayMaterials therefor for enzymes or isoenzymes

Abstract

Provided are a method and a pharmaceutical composition for treating cancer using a compound having VAP-1 inhibitory activity or a pharmaceutically acceptable salt thereof. Also provided are combination use of the compound having VAP-1 inhibitory activity or a pharmaceutically acceptable salt thereof and an anti-CTLA-4 antibody, and combination use of the compound having VAP-1 inhibitory activity or a pharmaceutically acceptable salt thereof, an anti-CTLA-4 antibody and an anti-PD-1 antibody.

IPC Classes  ?

• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61P 35/00 - Antineoplastic agents

Abstract

The object of the present invention is to provide a pharmaceutical composition for treating cerebral infarction. The present invention provides a pharmaceutical composition for treating cerebral infarction comprising a compound of formula (I) or a pharmaceutically acceptable salt. In formula (I), m is an integer of 1 or 2, n is an integer of 2 or 3, and A is dialkylamino or a certain ring structure containing at least one nitrogen atom.

IPC Classes  ?

• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• A61K 31/4409 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond

Abstract

Provided is a pharmaceutical composition for treating geographic atrophy associated with age-related macular degeneration, which contains a 15-ketoprostaglandin compound. A 15-ketoprostaglandin compound, such as isopropyl unoprostone, is effective for the treatment of geographic atrophy and can prevent the visual obscuration associated with geographic atrophy.

IPC Classes  ?

• A61K 31/5575 - Eicosanoids, e.g. leukotrienes having a cyclopentane ring, e.g. prostaglandin E2, prostaglandin F2-alpha
• A61K 9/08 - Solutions
• A61P 27/02 - Ophthalmic agents

Abstract

Disclosed is a method for manufacturing a fatty acid derivative represented by formula (I): which comprises the step of, reacting a compound of formula (II): with a co-oxidizer under the presence of an azaadamantane-N-oxyl derivative. According to the method, the desired fatty acid derivative can be synthesized without special equipment, by using an easy-available inexpensive co-oxidizer and generation of the undesired by-product is suppressed.

IPC Classes  ?

• C07D 309/12 - Oxygen atoms only hydrogen atoms and one oxygen atom directly attached to ring carbon atoms, e.g. tetrahydropyranyl ethers

Abstract

Disclosed is a method for manufacturing a fatty acid derivative represented by formula (I): which comprises the step of, reacting a compound of formula (II): with a co-oxidizer under the presence of an azaadamantane-N-oxyl derivative. According to the method, the desired fatty acid derivative can be synthesized by using an easy-available inexpensive co-oxidizer without special equipment, and generation of the undesired by-product is suppressed.

IPC Classes  ?

• C07F 7/08 - Compounds having one or more C—Si linkages

Abstract

A method for manufacturing a fatty acid derivative represented by formula (I) is provided: 1 is which includes the step of reacting a compound of formula (II): 1 is 2 is with a co-oxidizer under the presence of an azaadamantane-N-oxyl derivative.

IPC Classes  ?

• C07D 307/30 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms

Abstract

The present invention relates to a method and a pharmaceutical composition for suppressing immunity, in each of wherein a fatty acid derivative represented by general formula (I) is utilized. The present invention also relates to a method and a pharmaceutical composition for treating inflammatory diseases, allergic diseases and autoimmune diseases, in each of wherein the fatty acid derivative is utilized.

IPC Classes  ?

• A61K 31/5575 - Eicosanoids, e.g. leukotrienes having a cyclopentane ring, e.g. prostaglandin E2, prostaglandin F2-alpha
• A61P 17/00 - Drugs for dermatological disorders
• A61P 17/14 - Drugs for dermatological disorders for baldness or alopecia
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 37/02 - Immunomodulators
• A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
• A61P 37/08 - Antiallergic agents
• C07C 69/734 - Ethers
• C07D 317/30 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 319/06 - 1,3-DioxanesHydrogenated 1,3-dioxanes not condensed with other rings

Abstract

The invention holds a prescribed amount of a drug solution and applies same to skin or mucosa without waste. The invention is equipped with a grip (10) for grasping, a neck part (12) that is continuous with the grip (10) and is elastically deformable, and a head part (13) that is continuous with the neck part (12) and has a slit (14) for holding a supplied drug solution, and is configured to apply the drug solution as the neck part (12) is being elastically deformed by pressing the head part (13) on the skin or mucosa.

IPC Classes  ?

• A61M 35/00 - Devices for applying media, e.g. remedies, on the human body
• A45D 34/04 - Appliances specially adapted for applying liquid, e.g. using roller or ball

Abstract

Disclosed is an aqueous ophthalmic composition comprising (a) a fatty acid derivative such as a prostaglandin derivative, (b) a polyoxyethylene sorbitan fatty acid ester, (c) an edetic acid compound, (d) a boric acid and a salt of a boric acid, (e) a pharmaceutically acceptable aqueous carrier, and (f) no more than 0.005w/v% of benzalkonium chloride. The composition is stable and has good anti-microbial properties.

IPC Classes  ?

• A61K 31/5575 - Eicosanoids, e.g. leukotrienes having a cyclopentane ring, e.g. prostaglandin E2, prostaglandin F2-alpha
• A61K 9/08 - Solutions
• A61K 47/04 - Non-metalsCompounds thereof
• A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
• A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
• A61P 27/02 - Ophthalmic agents

Abstract

Provided is a pharmaceutical composition comprising a specific fatty acid derivative as an active ingredient for treating macular edema in a mammalian subject. The composition of the present invention can effectively treat macular edema in a non-invasive manner.

IPC Classes  ?

• A61K 31/5575 - Eicosanoids, e.g. leukotrienes having a cyclopentane ring, e.g. prostaglandin E2, prostaglandin F2-alpha
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

The present application provides an ophthalmic composition comprising a fatty acid derivative for the treatment of a retinal disease in a patient, characterized in that at least two drops at a time of the composition are instilled to an eye of the patient at least twice a day. The present application also provides a method for treating a retinal disease using said ophthalmic composition.

IPC Classes  ?

• A61K 31/5575 - Eicosanoids, e.g. leukotrienes having a cyclopentane ring, e.g. prostaglandin E2, prostaglandin F2-alpha
• A61B 3/12 - Objective types, i.e. instruments for examining the eyes independent of the patients perceptions or reactions for looking at the eye fundus, e.g. ophthalmoscopes
• A61K 9/08 - Solutions
• A61K 47/16 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen
• A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• A61P 27/02 - Ophthalmic agents

Abstract

Disclosed is a method for stabilizing a pharmaceutically active bi-cyclic compound of formula (I): comprising the step of: admixing the same with a polyol and/or a fatty acid ester other than glyceride and a composition obtained by the method. In addition a soft gelatin capsule formulation of the compound of formula (I) obtained by incorporating the compound in a soft gelatin capsule shell comprising gelatin and a polyol plasticizer.

IPC Classes  ?

• A61K 9/64 - Organic coatings containing proteins or derivatives thereof
• A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline

Abstract

Provided are a method for screening a drug which is efficacious in treating dry eye with a dry eye severity level 3 or higher that is defined in 2007 report of the International Dry Eye Workshop and/or keratoconjunctival disorders, and a pharmaceutical composition comprising said drug. Also provided is a method for treating dry eye with a dry eye severity level 3 or higher that is defined in 2007 report of the International Dry Eye Workshop and/or keratoconjunctival disorders by using the aforesaid drug.

IPC Classes  ?

• G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing
• A61K 38/00 - Medicinal preparations containing peptides
• A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
• A61P 27/02 - Ophthalmic agents
• G01N 33/15 - Medicinal preparations

Abstract

Disclosed is a composition for topical administration to eyes, which is intended to be used for the treatment of ocular hypertension and glaucoma, and which contains latanoprost as an active ingredient and additionally contains (a) a polyol and/or a sugar alcohol, (b) a nonionic surfactant and (c) an edetic acid compound. In the composition, the amount of a preservative agent used can be significantly reduced compared to those in conventional compositions, and therefore the occurrence of adverse side effects caused by the preservative agent can be prevented. The composition can be stored stably at room temperature for a long period.

IPC Classes  ?

• A61K 31/216 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
• A61K 9/08 - Solutions
• A61K 31/5575 - Eicosanoids, e.g. leukotrienes having a cyclopentane ring, e.g. prostaglandin E2, prostaglandin F2-alpha
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
• A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
• A61P 27/02 - Ophthalmic agents
• A61P 27/06 - Antiglaucoma agents or miotics

Abstract

Disclosed is a method for preparing a prostaglandin derivative of formula (A): which comprises reacting an aldehyde represented by formula (1): with a 2-oxoalkyl phosphonate in a reaction solvent under the presence of alkali hydroxide as sole base. By carrying out the reaction using an alkali hydroxide as sole base in the reaction system, the desired prostaglandin derivative can be obtained by simple procedures and with high yield.

IPC Classes  ?

• C07D 309/12 - Oxygen atoms only hydrogen atoms and one oxygen atom directly attached to ring carbon atoms, e.g. tetrahydropyranyl ethers

Abstract

Disclosed is a method for preparing a prostaglandin derivative of formula (A): which comprises reacting an aldehyde represented by formula (1): with a 2-oxoalkyl phosphonate in a reaction solvent under the presence of alkali hydroxide as sole base. By carrying out the reaction using an alkali hydroxide as sole base in the reaction system, the desired prostaglandin derivative can be obtained by simple procedures and with high yield.

IPC Classes  ?

• C07D 309/12 - Oxygen atoms only hydrogen atoms and one oxygen atom directly attached to ring carbon atoms, e.g. tetrahydropyranyl ethers
• C07F 7/18 - Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages

Abstract

Disclosed is a method for preparing a prostaglandin derivative of formula (A): which comprises reacting an aldehyde represented by formula (1): with a 2-oxoalkyl phosphonate in a reaction solvent under the presence of alkali hydroxide as sole base. By carrying out the reaction using an alkali hydroxide as sole base in the reaction system, the desired prostaglandin derivative can be obtained by simple procedures and with high yield.

IPC Classes  ?

• C07D 307/85 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
• C07C 57/26 - Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms containing rings other than six-membered aromatic rings
• C07C 69/608 - Esters of carboxylic acids having a carboxyl group bound to an acyclic carbon atom and having a ring other than a six-membered aromatic ring in the acid moiety

Abstract

Provided is a pharmaceutical composition comprising: a) a prostaglandin compound; (b) a sugar alcohol; (c) a polyol; and (d) a pharmaceutically acceptable carrier. The composition of the present invention can be stored stably even in a polyethylene container. In addition, the composition of the present invention can be stored stably for a long term even if it comprises only a small amount of a preserving agent.

IPC Classes  ?

• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin

Abstract

The present invention provides a novel benzene derivative or thiophene derivative useful as a VAP-1 inhibitor, or a medicament for the prophylaxis or treatment of a VAP-1 associated disease and the like, namely, a compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
• C07D 233/88 - Nitrogen atoms, e.g. allantoin
• C07D 239/42 - One nitrogen atom
• C07D 241/20 - Nitrogen atoms
• C07D 241/24 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• C07D 265/36 - 1,4-OxazinesHydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
• C07D 333/36 - Nitrogen atoms
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 487/08 - Bridged systems
• C07C 281/06 - Compounds containing any of the groups e.g. semicarbazides
• A61K 31/175 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine having the group , N—C(O)—N=N— or , e.g. carbonohydrazides, carbazones, semicarbazides, semicarbazonesThioanalogues thereof
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

Disclosed is a pharmaceutical composition for the treatment of dry eye and/or corneal/conjunctival disorders. The pharmaceutical composition comprises a human serum albumin as an active ingredient, wherein the human serum albumin is produced by using a recombinant yeast produced by transforming an yeast with a gene encoding the human serum albumin. Also disclosed is a method for the treatment of dry eye and/or corneal/conjunctival disorders, which comprises administering an effective amount of a human serum albumin to a patient who needs the treatment of dry eye and/or corneal/conjunctival disorders, wherein the human serum albumin is produced by using a recombinant yeast produced by transforming an yeast with a gene encoding the human serum albumin.

IPC Classes  ?

• A61K 38/00 - Medicinal preparations containing peptides
• A61P 27/02 - Ophthalmic agents
• C12N 15/09 - Recombinant DNA-technology
• C12P 21/02 - Preparation of peptides or proteins having a known sequence of two or more amino acids, e.g. glutathione

Abstract

The present invention provides a novel thiazole derivative useful as a VAP-1 inhibitor, a pharmaceutical agent for the prophylaxis or treatment of VAP-1 associated diseases and the like. A compound represented by the formula (I): wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• C07D 277/46 - Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
• C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• A61K 31/426 - 1,3-Thiazoles
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings

Abstract

Disclosed is a pharmaceutical composition effective for the treatment of cataract. Specifically disclosed is a pharmaceutical composition for the treatment of cataract which comprises a VAP-1 inhibitor as an active ingredient, particularly a pharmaceutical composition for the treatment of cataract which comprises a compound represented by the formula (I) or the like as an active ingredient. R1-NH-X-Y-Z (I) wherein each of the symbols is as defined in the description.

IPC Classes  ?

• A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
• A61K 31/426 - 1,3-Thiazoles
• A61P 27/12 - Ophthalmic agents for cataracts
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• C07D 277/20 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
• C07D 277/46 - Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof

Abstract

Provided is a pharmaceutical composition comprising a 11-deoxy-prostaglandin compound represented by formula (I): and a fatty acid ester. By mixing the compound of formula (I) and a fatty acid ester, the compound of formula (I) will be stabilized.

IPC Classes  ?

• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 31/5575 - Eicosanoids, e.g. leukotrienes having a cyclopentane ring, e.g. prostaglandin E2, prostaglandin F2-alpha

Abstract

Disclosed is a composition effective for an ophthalmic disease associated with hypoxia or ischemia, which comprises a VAP-1 inhibitor as an active ingredient. Also disclosed is an angiogenesis inhibitor which can prevent a morbid angiogenesis associated with hypoxia or ischemia.

IPC Classes  ?

• A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
• A61K 31/426 - 1,3-Thiazoles
• A61P 27/02 - Ophthalmic agents

Abstract

Disclosed is a composition for ameliorating an optic nerve disorder, which comprises a prostaglandin F2&agr; compound represented by the formula (1) as an active ingredient. Also disclosed is use of the composition. (1) wherein A represents -COOH or a pharmaceutically acceptable salt, ester or amide thereof; B represents a bond, a lower alkylene, or an oxygen; and R1 represents a hydrogen, a halogen or a lower alkyl unsubstituted or substituted by a halogen.

IPC Classes  ?

• A61K 31/5575 - Eicosanoids, e.g. leukotrienes having a cyclopentane ring, e.g. prostaglandin E2, prostaglandin F2-alpha
• A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
• A61P 27/02 - Ophthalmic agents
• A61P 43/00 - Drugs for specific purposes, not provided for in groups

Abstract

Disclosed are: a compound represented by the formula (I) or a pharmaceutically acceptable salt thereof, which is useful as a VAP-1 inhibitor; a pharmaceutical composition; a pharmaceutical agent for the prevention or treatment of a VAP-1-related disease such as macular edema and a disease associated with the increase in vascular permeability; and others. (I) wherein each symbol is as defined in the description.

IPC Classes  ?

• C07D 277/20 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
• A61K 31/426 - 1,3-Thiazoles
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• A61P 3/04 - AnorexiantsAntiobesity agents
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 7/10 - Antioedematous agentsDiuretics
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• A61P 9/12 - Antihypertensives
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 11/02 - Nasal agents, e.g. decongestants
• A61P 11/04 - Drugs for disorders of the respiratory system for throat disorders
• A61P 11/06 - Antiasthmatics
• A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
• A61P 17/02 - Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
• A61P 17/04 - Antipruritics
• A61P 17/06 - Antipsoriatics
• A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
• A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 27/02 - Ophthalmic agents
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 31/04 - Antibacterial agents
• A61P 37/02 - Immunomodulators
• A61P 37/08 - Antiallergic agents
• A61P 43/00 - Drugs for specific purposes, not provided for in groups
• C07D 277/44 - Acylated amino or imino radicals
• C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Goods & Services

(1) Chemical preparations for use in the manufacture of pharmaceutical preparations for ophthalmic, otic, nasal, blood and liver diseases, allergic rhinitis and respiratory diseases, and diseases of the gastro-intestinal tract, the central nervous system and cardiovascular system; Ophthalmic pharmaceutical preparations. (1) Medical services, namely, medical and scientific research services in the ophthalmic, otic, nasal, blood and liver diseases fields, allergic rhinitis and respiratory diseases fields, and in the field of diseases of the gastro-intestinal tract, the central nervous system and the cardiovascular system; medical testing services, namely, evaluation of ophthalmic, otic, nasal, blood and liver diseases, allergic rhinitis and respiratory diseases, and diseases of the gastro-intestinal tract, the central nervous system and the cardiovascular system; consultancy services relating to medical and health matters; medical monitoring, testing, inspection, imaging and diagnostic services; information, advisory, and consultancy services, all relating to the aforementioned services

Goods & Services

(1) Ophthalmic pharmaceutical preparations (2) Chemical preparations for use in the manufacture of pharmaceuticals for ophthalmic, otic, nasal, blood and liver diseases, allergic rhinitis and respiratory diseases, and diseases of the gastro-intestinal tract, the central nervous system and cardiovascular system (1) Medical services, namely, medical and scientific research services in the ophthalmic, otic, nasal, blood and liver diseases fields, allergic rhinitis and respiratory diseases fields, and in the field of diseases of the gastro-intestinal tract, the central nervous system and the cardiovascular system; medical testing services, namely, evaluation of ophthalmic, otic, nasal, blood and liver diseases, allergic rhinitis and respiratory diseases, and diseases of the gastro-intestinal tract, the central nervous system and the cardiovascular system; consultancy services relating to medical and health matters; medical monitoring, testing, inspection, imaging and diagnostic services; information, advisory, and consultancy services, all relating to the aforementioned services

Abstract

Disclosed is an aqueous composition which comprises a 15-keto-prostaglandin compound as an active ingredient and contains a polyoxyethylene castor oil derivative. The solubility of the 15-keto-PG compound in water can be improved by the addition of the polyoxyethylene castor oil derivative. The aqueous composition preferably further contains a quaternary ammonium-type cationic surfactant as a preservative. The composition shows a potent antibacterial effect on the contamination of normal flora occurring in eyes such as Staphylococcus aureus and is useful as an ophthalmic composition such as an eye drop.

IPC Classes  ?

• A61K 31/5575 - Eicosanoids, e.g. leukotrienes having a cyclopentane ring, e.g. prostaglandin E2, prostaglandin F2-alpha
• A61K 9/08 - Solutions
• A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
• A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
• A61P 27/02 - Ophthalmic agents

Abstract

Disclosed is a method for preparing a prostaglandin derivative of formula (A): which comprises reacting an aldehyde represented by formula (1): with a 2-oxoalkyl phosphonate in a reaction solvent under the presence of alkali hydroxide as sole base. By carrying out the reaction using an alkali hydroxide as sole base in the reaction system, the desired prostaglandin derivative can be obtained by simple procedures and with high yield.

IPC Classes  ?

• C07D 307/93 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems condensed with a ring other than six-membered
• C07D 311/94 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
• C07C 405/00 - Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins

Abstract

The present invention discloses a soft gelatin capsule formulation of a 15-keto-prostaglandin compound, which comprises: a soft gelatin capsule shell comprising gelatin and sugar alcohol as a plasticizer, and a mixture comprising a 15-keto-prostaglandin compound and a pharmaceutically acceptable vehicle which is filled in the shell. By encapsulating the 15-keto-prostaglandin compound in the specified soft gelatin capsule shell, stability of the compound is significantly improved.

IPC Classes  ?

• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 31/5575 - Eicosanoids, e.g. leukotrienes having a cyclopentane ring, e.g. prostaglandin E2, prostaglandin F2-alpha

Abstract

Disclosed is a method for stabilizing a pharmaceutically active bi-cyclic compound of formula (I), comprising the step of : admixing the same with a polyol and/or a fatty acid ester other than glyceride and a composition obtained by the method. In addition a soft gelatin capsule formulation of the compound of formula (I) obtained by incorporating the compound in a soft gelatin capsule shell comprising gelatin and a polyol plasticizer.

IPC Classes  ?

• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline

Abstract

Disclosed is a method for preparing a
prostaglandin derivative of formula (A):
(see formula A)
which comprises reacting an aldehyde represented by
formula (1):
(see formula 1)
with a 2-oxoalkyl phosphonate in a reaction solvent under
the presence of alkali hydroxide as sole base. By carrying
out the reaction using an alkali hydroxide as sole base in
the reaction system, the desired prostaglandin derivative
can be obtained by simple procedures and with high yield.

IPC Classes  ?

• C07C 405/00 - Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins
• C07D 307/93 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems condensed with a ring other than six-membered
• C07D 311/94 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings

Abstract

The present invention is directed to a
pharmaceutical composition comprising a 11-deoxy-prostaglandin
compound represented by formula (I):
(see formula I)
and a fatty acid ester. By mixing the compound of
formula (I) and a fatty acid ester, the compound of
formula (I) will be stabilized.

IPC Classes  ?

• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 31/5575 - Eicosanoids, e.g. leukotrienes having a cyclopentane ring, e.g. prostaglandin E2, prostaglandin F2-alpha

Abstract

Disclosed are prostaglandin derivatives which are: 7- [(1R,2R,3R,5S)-2-(4,4-difluoro-3-hydroxyoctyl) -5-hydroxy-3-(2-tetrahydropyranyloxy)cyclopentyl]heptanoic acid, benzyl 7-[(1R,2R,3R,5S)-2-(4,4-difluoro-3-hydroxy octyl)-5-hydroxy-3-(2-tetrahydropyranyloxy)cyclopentyl] heptanate, benzyl 7- [(2R,4aR,5R,7aR) -2- (1,1-difluoropentyl)-2-hydroxy-6-oxooctahydro cyclopenta[b]pyran-5-yl]heptanate, methyl 7-[(1R,2S,3R,5S) -2-(t-butyldimethylsilyl-oxy methyl)- 5-hydroxy -3-(2-tetrahydropyranyloxy) cyclopentyl] heptanate; or methyl 7-[(1R,2S,3R,5S)-5-acetoxy-2-(t-butyl dimethylsilyloxymethyl)-3-(2-tetrahydropyranyloxy) cyclopentyl]heptanate.

IPC Classes  ?

• C07C 405/00 - Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins
• C07F 7/18 - Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages

Abstract

Disclosed are prostaglandin derivatives which are: 7- [(1R,2R,3R,5S)-2-(4,4-difluoro-3-hydroxyoctyl)-5- hydroxy-3-(2-tetrahydropyranyloxy)cyclopentyl]heptanoic acid, benzyl 7- [(1R,2R,3R,5S)-2-(4,4-difluoro-3-hydroxy octyl)-5-hydroxy-3-(2-tetrahydropyranyloxy)cyclopentyl] heptanate, benzyl 7- [(2R,4aR,5R,7aR)-2-(1,1- difluoropentyl)-2-hydroxy-6-oxooctahydro cyclopenta[b]pyran-5-yl]heptanate, methyl 7-[(1R,2S,3R,5S)- 2-(t-butyldimethylsilyl-oxy methyl)- 5-hydroxy-3-(2- tetrahydropyranyloxy) cyclopentyl] heptanate; or methyl 7-[(1R,2S,3R,5S)-5-acetoxy-2-(t-butyl dimethylsilyloxymethyl)-3-(2-tetrahydropyranyloxy) cyclopentyl]heptanate.

IPC Classes  ?

• C07D 309/12 - Oxygen atoms only hydrogen atoms and one oxygen atom directly attached to ring carbon atoms, e.g. tetrahydropyranyl ethers

Abstract

The present invention discloses a soft gelatin capsule formulation of a 15-
keto-prostaglandin compound, which comprises: a soft gelatin capsule shell
comprising gelatin and sugar alcohol as a plasticizer, and a mixture
comprising a 15-keto-prostaglandin compound and a pharmaceutically acceptable
vehicle which is filled in the shell. By encapsulating the 15-keto-
prostaglandin compound in the specified soft gelatin capsule shell, stability
of the compound is significantly improved.

IPC Classes  ?

• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 31/5575 - Eicosanoids, e.g. leukotrienes having a cyclopentane ring, e.g. prostaglandin E2, prostaglandin F2-alpha

Abstract

The present invention is directed to a method for
stabilizing a pharmaceutically active bi-cyclic compound of
formula (I):
(see formula I)
comprising the step of: admixing the same with a polyol
and/or a fatty acid ester other than glyceride and a
composition obtained by the method. In
addition the
invention provides a soft gelatin capsule formulation of
the compound of formula (I) obtained by incorporating the
compound in a soft gelatin capsule shell comprising gelatin
and a polyol plasticizer.

IPC Classes  ?

• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 31/558 - Eicosanoids, e.g. leukotrienes having heterocyclic rings containing oxygen as the only ring hetero atom, e.g. thromboxanes
• A61P 1/10 - Laxatives

Abstract

Disclosed are prostaglandin derivatives which are: 7- [(1R,2R,3R,5S)-2-(4,4-difluoro-3-hydroxyoctyl)-5-hydroxy-3-(2- tetrahydropyranyloxy)cyclopentyl] heptanoic acid, benzyl 7- [(1R,2R,3R,5S)-2-(4,4-difluoro-3-hydroxy octyl)-5-hydroxy-3-(2-tetrahydropyranyloxy)cyclopentyl] heptanate, benzyl 7-[(2R,4aR,5R,7aR)-2-(1,1-difluoropentyl)-2-hydroxy-6-oxooctahydro cyclopenta[b]pyran-5-yl]heptanate, methyl 7-[(1R,2S,3R,5S)-2-(t-butyldimethylsilyl-oxy methyl) -5-hydroxy-3-(2-tetrahydropyranyloxy) cyclopentyl] heptanate; or methyl 7-[(1R,2S,3R,5S)-5-acetoxy-2-(t-butyl dimethylsilyloxymethyl)-3-(2-tetrahydropyranyloxy) cyclopentyl]heptanate.

IPC Classes  ?

• C07C 405/00 - Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins
• C07D 309/12 - Oxygen atoms only hydrogen atoms and one oxygen atom directly attached to ring carbon atoms, e.g. tetrahydropyranyl ethers
• C07D 311/94 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
• C07F 7/18 - Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages