The present invention provides a transdermal patch having a high skin permeation amount of mirogabalin. A transdermal patch according to the present invention is characterized by comprising: a support; and an adhesive layer that is integrally laminated on one surface of the support and contains an adhesive agent and a salt of mirogabalin which is precipitated as a crystal in the adhesive agent and is a salt formed with an acid having a pKa value of less than 3.5. The transdermal patch is also characterized in that the content of the salt of mirogabalin in the adhesive layer is preferably 2-60 mass%. As a result, the transdermal patch has a high skin permeation amount of mirogabalin.
NATIONAL UNIVERSITY CORPORATION KOBE UNIVERSITY (Japan)
Inventor
Sawabe Toshihiro
Odahara Ikko
Hasagawa Takeshi
Nozu Kandai
Sakakibara Nana
Abstract
The present invention provides a method for improving renal function, and a compound for regulating the expression and function of CUBN and can be used in the method for improving renal function. Renal function was successfully improved using a CUBN inhibitor.
Provided is an adhesive patch having excellent percutaneous absorption of selexipag. The adhesive patch of the present invention is characterized by including a backing and an adhesive layer that is integrally laminated on one surface of the backing and includes selexipag and an acrylic adhesive. In the adhesive layer, selexipag and an acrylic adhesive are used in combination to provide an adhesive patch having excellent percutaneous absorption of selexipag. The adhesive patch can percutaneously administer selexipag as a drug.
Provided is an adhesive patch which enables excellent percutaneous absorption of selexipag. An adhesive patch according to the present invention is characterized by comprising a support and an adhesive layer that is integrally laminated on one surface of the support and that contains selexipag and an acrylic adhesive. By using selexipag and the acrylic adhesive in combination in the adhesive layer, it is possible to provide an adhesive patch which enables excellent percutaneous absorption of selexipag. This adhesive patch makes it possible to percutaneously administer selexipag as a drug.
Provided is a nintedanib-containing solid dispersion in which the amount of impurities originating from nintedanib contained therein is low. The present invention provides a solid dispersion containing the components (a) and (b) indicated below. (a) Nintedanib, a pharmaceutically acceptable salt thereof, or a solvate of such substances; (b) at least one component selected from the group consisting of sugar alcohols, hypromellose esters, (meth)acrylic acid-based polymers, hardened oils, carnauba waxes, polyalkylene glycols, and sucrose fatty acid esters.
222 receptor antagonist or the like. The present invention is a compound represented by general formula (I) (all symbols in the formula are defined in the description), a pharmaceutically acceptable salt thereof, or a solvate thereof.
C07D 215/08 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms with acylated ring nitrogen atom
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
A61K 31/5517 - 1,4-Benzodiazepines, e.g. diazepam condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61K 31/554 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 3/12 - Drugs for disorders of the metabolism for electrolyte homeostasis
A61P 5/10 - Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
C07D 225/06 - Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with one six-membered ring
C07D 267/14 - Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
C07D 281/10 - Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
C07D 401/12 - 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 linked by a chain containing hetero atoms as chain links
C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 409/12 - 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 chain containing hetero atoms as chain links
C07D 413/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
An adhesive preparation containing bisoprolol includes a backing and a pressure-sensitive adhesive layer formed on one side of the backing. The pressure-sensitive adhesive layer contains a polymer prepared through copolymerization of monomer components including a hydroxyl group-containing monomer and an alkyl (meth)acrylate monomer (component (A)), a polymer prepared through copolymerization of monomer components including a methyl methacrylate monomer and a butyl methacrylate monomer (component (B)), and bisoprolol (component (C)).
Provided is a novel therapeutic agent for glaucoma, which has an sGC-activating activity. A therapeutic agent for glaucoma or an ocular hypotensive agent, which contains, as an active ingredient, a compound represented by formula (I-a) or formula (I-b) and having a LogD value of 1.5 to 2.5 exclusive or a pharmaceutically acceptable salt of the compound. [In formulae (I-a) and (I-b), each symbol is as defined in the description.]
C07C 255/59 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton the carbon skeleton being further substituted by singly-bound oxygen atoms
A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
A61K 31/277 - NitrilesIsonitriles having a ring, e.g. verapamil
A61K 31/382 - Heterocyclic compounds having sulfur as a ring hetero atom having six-membered rings, e.g. thioxanthenes
C07C 229/38 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to acyclic carbon atoms and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
C07D 311/68 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulfur atoms in position 2 or 4 with nitrogen atoms directly attached in position 4
C07D 333/16 - Radicals substituted by singly bound hetero atoms other than halogen by oxygen atoms
Provided is an adhesive preparation containing bisoprolol that has the high dermal permeability of bisoprolol and an ability to maintain good adhesiveness. An adhesive preparation containing bisoprolol includes a support body and an adhesive agent layer formed on one surface of the support body, said adhesive agent layer containing the following components (A)-(C) component (A), a polymer formed by copolymerizing monomer components, which include a (meth)acrylate alkyl ester monomer and a hydroxy group-containing monomer; component (B), a polymer formed by copolymerizing monomer components, which include a methyl methacrylate monomer and a butyl methacrylate monomer; and component (C), bisoprolol.
Provided is an adhesive preparation containing bisoprolol that has the high dermal permeability of bisoprolol and an ability to maintain good adhesiveness. An adhesive preparation containing bisoprolol includes a support body and an adhesive agent layer formed on one surface of the support body, said adhesive agent layer containing the following components (A)-(C) component (A), a polymer formed by copolymerizing monomer components, which include a (meth)acrylate alkyl ester monomer and a hydroxy group-containing monomer; component (B), a polymer formed by copolymerizing monomer components, which include a methyl methacrylate monomer and a butyl methacrylate monomer; and component (C), bisoprolol.
A compound represented by general formula (1)
2 alkyl groups; X represents a hydrogen atom or a halogen atom; V represents an oxygen atom or a methylene chain; and R represents a group selected from the formulae below:
A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
C07C 229/46 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
C07C 229/38 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to acyclic carbon atoms and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
C07C 255/59 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton the carbon skeleton being further substituted by singly-bound oxygen atoms
C07C 255/54 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and etherified hydroxy groups bound to the carbon skeleton
C07D 277/24 - Radicals substituted by oxygen atoms
C07D 333/16 - Radicals substituted by singly bound hetero atoms other than halogen by oxygen atoms
C07D 333/20 - Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms
Provided are compounds that are useful as prophylactic or therapeutic agents for various diseases involving T-type calcium channels, such as hypertension, arrhythmia, pain and cancer, said compounds having antagonistic activity against T-type calcium channels, being highly stable in the body, and being low risk in terms of genotoxicity and the like. The present invention provides compounds represented by general formula (I), and pharmaceutically acceptable salts or solvates thereof. [In general formula (I): R1 represents -NH(C=O)-V-R3, -(C=O)NH-V-R3, or the like; V represents a single bond, methylene, or -C(CH3)2O-; R2 represents an optionally-substitutable C1-6 alkyl group or the like; X represents a hydrogen atom, an oxygen atom, a hydroxyl group, a methyl group or a methylene group; A represents -NR6-, -O-CH2-, or -S-CH2-; n represents the number of methylene chains, and is an integer of 0, 1 or 2; and the dotted line represents a single or double bond].
C07D 451/02 - Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamineCyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropaneCyclic acetals thereof
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
Provided is a novel compound having an excellent suppression action against arrhythmia including atrial fibrillation and being useful as a pharmaceutical product having a separated antiviral effect. A compound indicated by general formula (I), a pharmacologically acceptable salt thereof, or a solvate of these (in the formula, the dotted line indicates a single bond and double bonds, R1 indicates a C1-6 alkyl group that may have a substituent, Q indicates an oxygen atom, a sulfur atom, or NR5, R2 indicates -(C=0)-R6, -CHR6R7, or -CH2OR8, and R3 and R4 are the same or different and indicate an amino group, an azide group, or -X-R9, provided that least either R3 or R4 is an amino group.)
C07C 233/41 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
A61K 31/166 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
A61K 31/27 - Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, e.g. meprobamate, carbachol, neostigmine
A61K 31/341 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
C07C 233/79 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
C07C 247/14 - Compounds containing azido groups with azido groups bound to carbon atoms of rings other than six-membered aromatic rings
C07C 271/24 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring
C07D 207/335 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
C07D 277/28 - Radicals substituted by nitrogen atoms
C07D 307/52 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
C07D 333/20 - Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms
C07D 333/22 - Radicals substituted by doubly bound hetero atoms, or by two hetero atoms other than halogen singly bound to the same carbon atom
Provided is an angiotensin II receptor antagonist that has favorable percutaneous absorbability. Also provided is a pharmaceutical composition that contains the angiotensin II receptor antagonist. A tert-butylamine salt or diethylamine salt that is an angiotensin II receptor antagonist, and a pharmaceutical composition that contains the tert-butylamine salt or the diethylamine salt.
The present invention provides a medical drug containing a compound represented by general formula (1), a pharmaceutically acceptable salt thereof, or a solvate of the compound or salt. The following are provided: the compound represented by general formula (1) (In the formula, Ar is an aryl group or a 5-6 membered ring type heteroaryl group containing a nitrogen atom, oxygen atom or sulfur atom; Y is a hydrogen atom, a C1-C6 alkyl group, or the like; A is a C1-C3 alkylene chain optionally substituted with two C1-C2 alkyl groups; X is a hydrogen atom or a halogen atom; V is an oxygen atom or a methylene chain; and R is a group selected from among formulae); the pharmaceutically acceptable salt thereof; or a solvate of the compound or salt.
C07C 229/38 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to acyclic carbon atoms and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
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 11/00 - Drugs for disorders of the respiratory system
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07C 229/46 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
C07C 255/54 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and etherified hydroxy groups bound to the carbon skeleton
C07C 255/59 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton the carbon skeleton being further substituted by singly-bound oxygen atoms
C07D 277/24 - Radicals substituted by oxygen atoms
C07D 333/16 - Radicals substituted by singly bound hetero atoms other than halogen by oxygen atoms
C07D 333/20 - Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms
C07D 333/56 - Radicals substituted by oxygen atoms
The present invention relates to a bisoprolol-containing adhesive patch that is provided with: a support body; and an adhesive layer that contains bisoprolol and an adhesive and that is stacked on one surface of the support body. The bisoprolol-containing adhesive patch is characterized by the halogen atom content within the adhesive layer being 0.01-100 weight ppm. The present invention makes it possible to minimize decreases in adhesive strength, discoloration, and the like in a bisoprolol-containing adhesive patch during storage thereof.
The present invention pertains to a bisoprolol-containing patch preparation containing a support body and an adhesive layer laminated to one surface of the support body and containing an adhesive agent and free bisoprolol, the stress relaxation percentage of the adhesive layer being 20-90%, and the shear stress of the adhesive layer being 1.0-6.5 N/30 mm width. The bisoprolol-containing patch preparation has suppressed peeling during use, has superior skin adhesiveness, and suppresses skin irritation during delamination. As the adhesive agent, a rubber-based adhesive is preferable, and a polyisobutylene and/or styrene-isoprene-styrene block copolymer is more preferable.
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
The present invention relates to: a bisoprolol-containing adhesive patch which comprises a supporting body and an adhesive layer that is formed on at least one surface of the supporting body and contains bisoprolol, and wherein the adhesive layer has a moisture content of 10,000 ppm or less; and a package of a bisoprolol-containing adhesive patch, which is obtained by sealing the bisoprolol-containing adhesive patch in a bag that has resistance to water vapor permeation. A bisoprolol-containing adhesive patch according to the present invention achieves excellent long-term stability of bisoprolol that is contained in the adhesive layer. In addition, a package of a bisoprolol-containing adhesive patch according to the present invention has excellent usability and portability.
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
The present invention relates to a bisoprolol-containing adhesive patch that is provided with: an adhesive patch body that comprises a support body and an adhesive layer that contains bisoprolol and that is formed on one surface of the support body; and a peeling liner that is temporarily attached to the adhesive surface of the adhesive layer of the adhesive patch body. The peel force between the adhesive layer and the peeling liner is equal to or less than 0.07 N/24 mm width. This bisoprolol-containing adhesive patch minimizes the adhesion thereof to the inner surface of a packaging material, can be extracted with extreme ease at the time of use, and has good peeling liner peelability at the time of use.
A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
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 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
Provided is a medicinal agent comprising a compound represented by general formula (1), a pharmaceutically acceptable salt of the compound or a solvate of the compound or the pharmaceutically acceptable salt. A compound represented by general formula (1) (wherein A represents a C1-C3 linear alkylene group in which one methylene group may be substituted by O or S; n represents an integer of 3 to 5; X1 and X2 independently represent CH or N; W1 and W2 independently represent a carboxyl group or a tetrazolyl group; V represents a C1-C8 linear or branched alkylene group in which one methylene group may be substituted by O or S; and R represents a substituted phenyl group or the like), a pharmaceutically acceptable salt of the compound, or a solvate of the compound or the pharmaceutically acceptable salt.
C07C 229/50 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups and carboxyl groups bound to carbon atoms being part of the same condensed ring system
A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
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 31/353 - 3,4-Dihydrobenzopyrans, e.g. chroman, catechin
A61K 31/357 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
A61K 31/36 - Compounds containing methylenedioxyphenyl groups, e.g. sesamin
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/382 - Heterocyclic compounds having sulfur as a ring hetero atom having six-membered rings, e.g. thioxanthenes
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
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
C07D 307/82 - Benzo [b] furansHydrogenated benzo [b] furans 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 carbon atoms of the hetero ring
C07D 311/04 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring
C07D 311/58 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulfur atoms in position 2 or 4
The purpose of the present invention is to provide a packaging structure for patches which achieves a package body wherefrom patches can be removed easily. A packaging structure (100) for patches includes a first and a second base member (120, 130) having peripheral edge parts that are laminated together, and contains a patch. The first and second base members (120, 130) have a first, a second, a third, and a fourth edge (121-124, 131-134). At least one of the first and second base members (120, 130) has a first, a second and a third opening part (125-127, 135-137). The first, second, and third opening parts (125-127, 135-137) serve as guides to ensure opening occurs along the internal peripheral edges (120c1, 120c2, 120c4, 130c1, 130c2, 130c4) of a sealing part (120c, 130c).
Provided is a novel compound which has antagonistic activity against a T-type calcium channel and is useful as a medicine. The compound is represented by general formula (I) (wherein n, indicating the number of nitrogen atoms contained in the fused 6-membered aromatic ring, is 0, 1, or 2; p, indicating the number of nitrogen atoms contained in the 6-membered aromatic ring, is 0 or 1; X represents an oxygen atom, -SO2-, or -N(R9)-; and R1 to R5 each represents a hydrogen atom or a substituent). Also provided is a medicine containing the compound.
C07D 235/12 - Radicals substituted by oxygen atoms
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
C07D 235/14 - Radicals substituted by nitrogen atoms
C07D 235/16 - 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 401/06 - 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 linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/12 - 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 linked by a chain containing hetero atoms as chain links
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Disclosed is an adhesive patch which effectively inhibits the occurrence of oozing or squeezing out of the adhesive layer component from the exposed area of the adhesive layer of the adhesive patch during storage, and also inhibits the occurrence of oozing of bisoprolol or salts of same from the adhesive layer thereby preventing reduction of drug content. A backing material, a release liner and an adhesive layer respectively, along with the entire adhesive patch, are shaped into a planar rectangle wherein the corners of the adhesive patch are formed into convex shapes on the rear surface on the backing material side. Further, the adhesive patch has a central part and edges wherein the corners of the rectangular shape of the central part can also be formed into convex shapes, and furthermore it can be provided with built-up articulated sections between two or more adjacent convex parts wherein the thickness of the adhesive patch is thinner than the thickness of the adhesive layer at each convex part. If the release liner is provided with a split at the back, the split should not traverse the convex parts.
Disclosed is a matrix-type transdermal preparation which contains a thiazide diuretic agent. Specifically disclosed is a matrix-type transdermal preparation which contains the following components (A), (B) and (C). (A) a thiazide diuretic agent or a thiazide-mimetic agent (B) one or more nonionic surfactants selected from among saturated fatty acid mono- or di-alkanolamides, alkyl glycosides, alkyl thioglycosides and polyoxyethylene alkyl ethers (C) an acrylic adhesive which contains a copolymer containing a (meth)acrylate ester that has a hydroxyl group or a carboxyl group in a side chain of a monomer constituent unit
A61K 31/549 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
A61K 47/08 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen
A61K 47/16 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen
A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
25.
PERCUTANEOUS ABSORPTION ENHANCER AND TRANSDERMAL PREPARATION USING THE SAME
Disclosed is a percutaneous absorption enhancer which has an excellent percutaneous absorption enhancing effect for a wide range of drugs, while exhibiting excellent compatibility with adhesive base agents. A transdermal preparation using the percutaneous absorption enhancer is also disclosed. The percutaneous absorption enhancer contains a sulfosuccinate ester or a salt thereof, and an alkyl glycoside or an alkyl thioglycoside.
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
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
A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
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
26.
METHOD FOR PRODUCING 9-HYDROXYMETHYL-CYCLOHEPTA[B]PYRIDINE-3-CARBOXYLATE ESTER DERIVATIVE
Disclosed is a method for commercially producing a 9-hydroxymethyl-cyclohepta[b]pyridine-3-carboxylate ester derivative. Specifically disclosed is a method for producing a 9-hydroxymethyl-cyclohepta[b]pyridine-3-carboxylate ester derivative represented by formula (1), which is characterized by reducing an epoxy derivative represented by general formula (3). (In the formula (3), R1 represents a halogen atom, a lower alkyl group or a lower alkoxy group; and R2 represents a lower alkyl group.) (In the formula (1), R1 and R2 are as defined above.)
A device for the administration of bisoprolol having a support; and a pressure-sensitive adhesive layer containing bisoprolol which is layered on one face of the support; wherein the maximum speed of releasing bisoprolol within 24 hours immediately after the application to the skin is 30 騜g/cm2/h or less and the speed of releasing bisoprolol at the point 24 hours after the application to the skin is 10 騜g/cm2/h or less. This transdermal administration device shows a relived skin irritation at the application and, in particular, at the peeling and enables the continuous administration of a therapeutically or preventively effective amount of bisoprolol to the living body.
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
patents
